JP2001247564A - Heteroaryl-substituted pyrrole derivative - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a compound capable of suppressing the formation of inflammatory cytokine. SOLUTION: The objective compound is expressed by general formula (I) A is pyrrole ring; R1 is a (substituted)aryl or a (substituted)heteroaryl; R2 is a (substituted)heteroaryl; R3 is a group expressed by general formula X-R4 [X is single bond, a (substituted)alkylene, a (substituted)alkenylene or a (substituted)alkynylene; and R4 is a substituted cycloalkyl, a substituted aryl, a (substituted)heterocyclyl, a (substituted)heteroaryl or NRaRb (Ra and Rb are each H, an alkyl, an alkenyl, an alkynyl, an aralkyl or an alkylsulfonyl)]; the atoms on the pyrrole ring bonded with R1 and R3 are each adjacent to the atom on the pyrrole ring bonded with R2} or its pharmacologically permissible salts, esters or other derivatives.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

[0001] The present invention relates to a heteroaryl-substituted pyrrole derivative useful as a pharmaceutical. More specifically, interleukin (IL) -1, IL-6, IL
-8, antipyretic, analgesic, and anti-inflammatory agents, which have an inhibitory effect on the production of inflammatory cytokines such as tumor necrosis factor (TNF), autoimmune diseases such as rheumatoid arthritis, bone diseases such as osteoporosis, and other cytokines involved The present invention relates to a heteroaryl-substituted pyrrole derivative useful as a therapeutic agent for diseases.

[0002]

2. Description of the Related Art Conventionally, nonsteroidal anti-inflammatory drugs (NSA)
ID) has antipyretic, analgesic, and anti-inflammatory actions as its main pharmacological actions, which are based on the inhibition of prostaglandin (PG) biosynthesis by cyclooxygenase inhibition, and is widely used in various inflammatory and painful diseases. It has been. For rheumatoid arthritis and the like, NSAIDs are used for symptomatic treatment, and immunomodulators (DMARDs) are used for causal treatment.

[0003] Conventional NSAIDs cause gastrointestinal disorders such as gastric ulcer due to their mechanism of action, and have problems in long-term continuous use. In addition, DMARD has not yet stably expressed a clear drug effect. In recent years, active substances collectively referred to as cytokines produced by immunocompetent cells have been found. Interleukin (IL)
-1, IL-6, IL-8, tumor necrosis factor (TNF) and the like are called inflammatory cytokines, and activate arachidonic acid metabolism, which is a PG production system, leukocyte migration, induction of acute phase proteins, Various functions as inflammatory mediators such as activation of osteoclasts have been elucidated, and these inflammatory cytokine production inhibitors have a new generation of antipyretic, analgesic, and anti-inflammatory properties by a different mechanism of action. It is expected to be used as a therapeutic agent for inflammatory agents, autoimmune diseases such as rheumatoid arthritis, bone diseases such as osteoporosis, and other diseases in which the cytokine is involved.

[0004] As the heteroaryl compounds having the action of suppressing the production of these inflammatory cytokines, for example, the following compounds are specifically disclosed.
There is a demand for the development of compounds that are more excellent in pharmacokinetics and safety.

[0005]

Embedded image

[0006]

DISCLOSURE OF THE INVENTION The present inventors have conducted intensive studies over many years on the synthesis of compounds capable of suppressing the production of the above-mentioned inflammatory cytokines and their pharmacological actions. And found that a compound in which three consecutive atoms on the 1H-pyrrole ring were substituted has an excellent inflammatory cytokine production inhibitory action,
The present invention has been completed.

[0007]

The present invention relates to (1) a compound having the following general formula (I), or a pharmaceutically acceptable salt, ester or other derivative thereof:

[0008]

Embedded image In the formula, A represents a pyrrole ring; R ¹ is an aryl group; an aryl group substituted with a group selected from substituent group α, substituent group β, substituent group γ, and substituent group δ; A heteroaryl group; or a heteroaryl group substituted with a group selected from a substituent group α, a substituent group β, a substituent group γ, and a substituent group δ, and R ² has at least one nitrogen atom heteroaryl group; or a substituent group alpha, substituent group beta, substituted with a group selected from substituent group γ and substituent group [delta], the nitrogen atom shown a heteroaryl group having at least one, R ³ is in the general formula -X-R ⁴ [wherein, X represents a single bond, a lower alkylene group, substituted with a group selected from substituent group α is a lower alkylene group, lower alkenylene group, selected from substituent group α A lower alkenylene group, a lower alkynylene group, or a A lower alkynylene group substituted with a group selected from the substituent group α,
⁴ is a cycloalkyl group which may be substituted with a group selected from substituent group α and substituent group δ, and is substituted with a group selected from substituent group β and substituent group γ; α
And an aryl group which may be substituted with a group selected from the substituent group δ and is substituted with a group selected from the substituent group β and the substituent group γ; selected from the substituent group α and the substituent group δ A heterocyclyl group substituted with a group selected from the substituent group β and the substituent group γ; a heterocyclyl group substituted with a group selected from the substituent group α and the substituent group δ A heterocyclyl group having at least one nitrogen atom which may be substituted with a group selected from substituent group α and substituent group δ, and a group selected from substituent group β and substituent group γ A heteroaryl group substituted with
A heteroaryl group having at least one nitrogen atom, which may be substituted with a group selected from the substituent group α and the substituent group δ; or a group having the general formula —NR ^a R ^b (wherein
R ^a and R ^b are the same or different and each represent a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an aralkyl group, or a lower alkylsulfonyl group. ) Is shown. ] Is shown.

However, the atoms on the pyrrole ring to which R ¹ and R ³ are bonded are respectively adjacent to the atoms on the pyrrole ring to which R ² is bonded. ｝.

[Substituent group α] hydroxyl group, nitro group, cyano group, halogen atom, lower alkoxy group, halogeno lower alkoxy group, alkylthio group, halogeno lower alkylthio group [substituent group β] —group having —NR ^c R ^d (Wherein, R ^c and R ^d are the same or different and are each a hydrogen atom,
It represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an aralkyl group, or a lower alkylsulfonyl group, or forms a heterocyclyl group together with the nitrogen atom to which R ^c and R ^d are bonded. ) [Substituent group γ] Lower alkyl group substituted by a group having -NR ^c R ^d (wherein R ^c and R ^d have the same meanings as described above) [Substituent group δ] Lower alkyl group Lower alkenyl group, lower alkynyl group, aralkyl group, cycloalkyl group, lower alkyl group substituted with a group selected from substituent group α, lower alkenyl group substituted with a group selected from substituent group α, An alkynyl group substituted with a group selected from the substituent group α.

Among these, preferred compounds include
(2) a compound wherein R ¹ is an aryl group; or an aryl group substituted with a group selected from substituent group α, substituent group β, substituent group γ and substituent group δ, (3) R ¹ Is phenyl or naphthyl, or phenyl or naphthyl substituted with a group selected from substituent group α, substituent group β, substituent group γ and substituent group δ, (4) R
^1, phenyl, or a substituent group alpha ^1, Substituent group beta ^1, compound is phenyl substituted with a group selected from substituent group gamma ¹ and Substituent group [delta] ^1, is (5) R ^1, A compound that is phenyl or phenyl substituted with a group selected from the following substituent groups: (Substituent groups: halogen atom, halogeno lower alkyl group,
(Halogeno lower alkoxy group) (6) R ¹ is phenyl, 4-fluorophenyl, 3
A compound which is -fluorophenyl, 3-chlorophenyl, 3,4-difluorophenyl, 3,4,5-trifluorophenyl, 3-chloro-4-fluorophenyl, 3-difluoromethoxyphenyl or 3-trifluoromethylphenyl; (7) R ² is a 5- or 6-membered aromatic heterocyclic group containing one or two nitrogen atoms; or a group selected from substituent group α, substituent group β, substituent group γ and substituent group δ Containing one or two nitrogen atoms substituted with
A compound which is a 6- to 6-membered aromatic heterocyclic group, (8) R
(9) R ² is a compound wherein ² is pyridyl, pyrimidinyl, or pyridyl or pyrimidinyl substituted with a group selected from substituent group α, substituent group β, substituent group γ, and substituent group δ; A compound which is 4-pyridyl, 4-pyrimidinyl, or 4-pyridyl or 4-pyrimidinyl substituted with a group selected from substituent group α, substituent group β, substituent group γ, and substituent group δ, (10 ) R
² is 4-pyridyl, 4-pyrimidinyl, or 4-pyridyl substituted at the 2-position with one group selected from substituent group α, substituent group β, substituent group γ and substituent group δ, or compounds which are 4-pyrimidinyl, is (11) R ^2, 4
-Pyridyl, 4-pyrimidinyl, or a compound which is 4-pyridyl or 4-pyrimidinyl substituted at the 2-position with one group selected from the following substituent groups (Substituent groups: methoxy, amino, methylamino, Benzylamino, α-methylbenzylamino.) (12) R ⁴ may be substituted with a group selected from substituent group α and substituent group δ, and selected from substituent group β and substituent group γ. A cycloalkyl group having 3 to 7 carbon atoms, which is substituted with a group selected from the group consisting of a substituent group α and a substituent group δ; Phenyl or naphthyl substituted with a selected group; may be substituted with a group selected from a substituent group α and a substituent group δ, and a substituent group β and a substituent group γ
A 4- to 12-membered non-aromatic heterocyclic group containing one or two sulfur, oxygen and / or nitrogen atoms substituted with a group selected from the group consisting of: a substituent group α and a substituent group δ A 4- to 12-membered non-aromatic heterocyclic group optionally containing one nitrogen atom and further containing one oxygen atom, sulfur atom or nitrogen atom, which may be substituted with And one or two sulfur atoms, oxygen atoms, and / or a group selected from the substituent group β and the group selected from the substituent group γ.
Or a 5- or 6-membered aromatic heterocyclic group containing a nitrogen atom; a 5- or 6-membered aromatic group containing 1 or 2 nitrogen atoms which may be substituted with a group selected from the substituent group α and the substituent group δ A compound having a group heterocyclic group; or -NR ^a R ^b (where R ^a and R ^b have the same meanings as described above), (1
3) X is a single bond; an alkylene group having 1 to 6 carbon atoms; an alkylene group having 1 to 6 carbon atoms substituted with a group selected from the substituent group α; alkenylene having 2 to 6 carbon atoms Group; substituted with a group selected from substituent group α,
A compound which is an alkenylene group having 2 to 6 carbon atoms; an alkynylene group having 2 to 6 carbon atoms; or an alkynylene group having 2 to 6 carbon atoms, which is substituted with a group selected from the substituent group α. X is a single bond; an alkylene group having 1 to 4 carbon atoms; an alkylene group having 1 to 4 carbon atoms substituted with a group selected from the substituent group α;
Alkenylene groups; alkenylene groups having 2 to 4 carbon atoms, substituted with groups selected from substituent group α; alkynylene groups having 2 to 4 carbon atoms; or groups selected from substituent group α. (15) X is substituted with a single bond; an alkenylene group having 2 to 4 carbon atoms; or a group selected from a substituent group α. compound alkenylene group having 2 to 4 carbon atoms, (16) R ³ is represented by the following general formula (II)
A group having:

[0012]

Embedded image [In the formula, m represents 0 or 1, n represents 1 or 2, R ⁵ , R ⁶ , R ⁷ , R ⁸ and R ⁹ are the same or different and are a hydrogen atom, a substituent group α , Substituent group β, substituent group γ
And one group selected from substituent group δ, and one of D and E is> NR ¹⁰ (R ¹⁰ is a hydrogen atom, substituent group γ
And one group selected from the substituent group δ. The other is> CR ¹¹ R ¹² (R ¹¹ and R ¹² are one group selected from a hydrogen atom, a substituent group α, a substituent group β, a substituent group γ and a substituent group δ And R)
⁶ may together with R ⁵ or R ⁷ represent a single bond; R ¹⁰ and R ¹¹ together form a lower alkylene group or a substituent group α, a substituent group β, a substituent It may form a lower alkylene group substituted by a group selected from group γ and substituent group δ. A compound having the formula:
(17) a compound wherein m is 1 and n is 1;
8) compounds wherein E is> NR ¹⁰ and D is> CR ¹¹ R ¹² ; (19) one of R ⁵ and R ⁷ together with R ⁶ represents a single bond; Atom, substituent group α,
One group selected from the substituent group γ and the substituent group δ, wherein R ⁸ , R ⁹ and R ¹² are the same or different and are a hydrogen atom, a substituent group α, a substituent group γ and a substituent One group selected from the group δ, wherein R ¹⁰ and R ¹¹ are the same or different and are one group selected from a hydrogen atom, a substituent group α, a substituent group γ and a substituent group δ Or R ¹⁰
And R ¹¹ together form a lower alkylene group, or a lower alkylene group substituted with a group selected from substituent group α, substituent group β, substituent group γ, and substituent group δ. Compound (20) wherein R ¹⁰ and R ¹¹ together
A straight-chain alkylene group having 3 to 4 carbon atoms, or a straight-chain alkylene group having 3 to 4 carbon atoms substituted with a group selected from the group of substituents α, β, γ and δ A compound forming an alkylene group, (21) R ⁷ , R ⁸ and R ⁹
Is a hydrogen atom, and R ¹⁰ and R ¹¹ are taken together to form a straight-chain alkylene group having 3 to 4 carbon atoms, or a substituent group α, a substituent group β, a substituent group γ, and A compound forming a straight-chain alkylene group having 3 to 4 carbon atoms substituted with a group selected from group δ, and (22) a compound represented by the following general formula (1-1) or general formula (1-3) :

[0013]

Embedded image And a pharmacologically acceptable salt, ester or other derivative thereof.

[Substituent group α ¹ ] halogen atom, lower alkoxy group, halogeno lower alkoxy group [Substituent group β ¹ ] —a group having —NR ^c R ^d (wherein one of R ^c and R ^d is a hydrogen atom Or a lower alkyl group, and the other is a hydrogen atom, a lower alkyl group or an aralkyl group.) [Substituent group γ ¹ ] amino lower alkyl group, lower alkylamino lower alkyl group, di (lower alkyl) amino lower alkyl group Aralkylamino lower alkyl group [substituent group δ ¹ ] lower alkyl group, halogeno lower alkyl group, hydroxy lower alkyl group, and nitro lower alkyl group.

Further, in the compound of the above (1),
(2) to (6); (7) to (11); (12);
Compounds satisfying a combination of requirements arbitrarily selected from the five groups consisting of (13) and (15); (16) to (21); and (22) are also suitable.

Among these, particularly preferred compounds include (23) compounds selected from the following, or pharmacologically acceptable salts, esters or other derivatives thereof: 4- (3-amino) Propyl) -2- (4-Fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (3-acetylaminopropyl) -2- (4-fluorophenyl) -3- (pyridine- 4-yl) -1H
-Pyrrole 2- (4-fluorophenyl) -4- (3-methylaminopropyl) -3- (pyridin-4-yl) -1H-
Pyrrole [5- (4-fluorophenyl) -4- (pyridine-
4-yl) -1H-pyrrol-3-yl]-(pyridin-4-yl) methanol 4- (1-acetyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4 -Fluorophenyl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (1,2,3,6-tetrahydropyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (piperidine-
4-yl) -3- (pyridin-4-yl) -1H-pyrrole 3- (4-fluorophenyl) -1- (piperidin-
4-yl) -2- (pyridin-4-yl) -1H-pyrrole 1- (1-acetylpiperidin-4-yl) -3-
(4-Fluorophenyl) -2- (pyridin-4-yl) -1H-pyrrole.3- (4-fluorophenyl) -1- [1- (2-nitroethyl) piperidin-4-yl] -2- ( Pyridin-4-yl) -1H-pyrrole 3- (4-fluorophenyl) -1- [3- (morpholin-1-yl) propyl] -2- (pyridin-4-yl) -1H-pyrrole3 -(4-Fluorophenyl) -1- (piperidine-
3-yl) -2- (pyridin-4-yl) -1H-pyrrole 1- (azetidin-3-yl) -3- (4-fluorophenyl) -2- (pyridin-4-yl) -1H- Pyrrole 4- (3-dimethylaminopropyl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H
-Pyrrole 2- (4-fluorophenyl) -4- [3- (piperidin-1-yl) propyl] -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl)- 4- [3- (1-Methylpiperazin-4-yl) propyl] -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-methyl-
1,2,3,6-tetrahydropyridin-4-yl)-
3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-methylpiperidin-4-yl) -3- (pyridin-4-yl)-
1H-pyrrole 3- (4-fluorophenyl) -2- (pyridine-4
-Yl) -1- (2,2,6,6-tetramethylpiperidin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (quinuclidin-2-en-3-yl)
-1H-pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (quinuclidin-3-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (4-hydroxypiperidin-4-yl) -3- (pyridin-4-yl)- 1H-pyrrole 3- (4-fluorophenyl) -2- (pyridine-4
-Yl) -1- (quinuclidin-3-yl) -1H-pyrrole 1- (4-aminocyclohexyl) -3- (4-fluorophenyl) -2- (pyridin-4-yl) -1H-
Pyrrole3- (4-fluorophenyl) -2- (2-methylaminopyrimidin-4-yl) -1- (piperidin-4-
Yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (8-methyl-
8-azabicyclo [3.2.1] oct-2-ene-3
-Yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (8-methyl-
8-Azabicyclo [3.2.1] octan-3-yl)
-3- (pyridin-4-yl) -1H-pyrrole 4- (8-azabicyclo [3.2.1] oct-2-
(En-3-yl) -2- (4-fluorophenyl) -3
-(Pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (1,2,3,6-tetrahydro-2,
2,6,6-tetramethylpyridin-4-yl) -1H
-Pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (2,2,6,6-tetramethylpiperidin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (2-methyl-
1,2,3,6-tetrahydropyridin-4-yl)-
3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (6-methyl-
1,2,3,6-tetrahydropyridin-4-yl)-
3- (pyridin-4-yl) -1H-pyrrole. 4- (1-ethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl)-
3- (pyridin-4-yl) -1H-pyrrole. 4- (1-ethylpiperidin-4-yl) -2- (4
-Fluorophenyl) -3- (pyridin-4-yl)-
1H-pyrrole 2- (4-fluorophenyl) -4- (1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-propyl-1,2,3,6-tetrahydropyridin-4-yl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-phenethyl-1,2,3,6-tetrahydropyridin-4-yl) -3- ( Pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,8,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,6,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 4- (1,6-dimethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3 -(Pyridin-4-yl) -1H-pyrrole 4- (1,2-dimethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- ( Pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,2,
6,6-pentamethyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl)-
1H-pyrrole 4- (3-dimethylamino-1-propen-1-yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (4-amino Butyl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (1-ethyl-6-methyl-1,2,3,6-tetrahydropyridine-4- Yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (1-ethyl-2-methyl-1,2,3,6-tetrahydropyridine-4- Yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 1- (3-dimethylaminopropyl) -3- (4-fluorophenyl) -2- (pyridine- 4-yl) -1H
-Pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,6,7,8,8a-octahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole -4- (6-allyl-1-methyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4- Fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (2-allyl-1-methyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4- Fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (6-benzyl-1-methyl-1,2,3,6-
Tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (2-benzyl-1-methyl-1,2,3,6-
Tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (6-methyl-
1-propyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (2-methyl-
1-propyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,3 4,
6,7,9a-Hexahydro-2H-quinolidine-8-
Yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,3,4,
6,9,9a-Hexahydro-2H-quinolidine-8-
Yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3
5,8,8a-Hexahydroindolizin-7-yl)
-3- (2-Methylaminopyrimidin-4-yl) -1
H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,6,8a-Hexahydroindolizin-7-yl)
-3- (2-Methylaminopyrimidin-4-yl) -1
H-pyrrole 2- (3,4-difluorophenyl) -4- (1,
2,3,5,8,8a-Hexahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole2- (3,4-difluorophenyl) -4- (1,
2,3,5,6,8a-hexahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole Il)-
2- (3-trifluoromethylphenyl) -1H-pyrrole 4- (1,2,3,5,6,8a-hexahydroindolizin-7-yl) -3- (pyridin-4-yl)-
2- (3-trifluoromethylphenyl) -1H-pyrrole 2- (3-fluorophenyl) -4- (1,2,3
5,8,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (3-fluorophenyl) -4- (1,2,3
5,6,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (3-chlorophenyl) -4- (1,2,3,
5,8,8a-Hexahydroindolizin-7-yl)
-3- (Pyridin-4-yl) -1H-pyrrole 2- (3-chlorophenyl) -4- (1,2,3
5,6,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 4- (1,2,3,5,8,8a-hexahydroindolizin-7-yl) -2-phenyl-3- (pyridine-4 -Yl) -1H-pyrrole 4- (1,2,3,5,6,8a-hexahydroindolizin-7-yl) -2-phenyl-3- (pyridin-4-yl) -1H-pyrrole .

Among the compounds listed in (23), more preferred are (24) compounds selected from the following, or pharmacologically acceptable salts, esters or other derivatives thereof: 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (1,2,3,6-tetrahydropyridin-4-yl) -1H-pyrrole 3- (4-fluorophenyl) -1- (piperidine-
4-yl) -2- (pyridin-4-yl) -1H-pyrrole 3- (4-fluorophenyl) -1- [3- (morpholin-1-yl) propyl] -2- (pyridin-4- Yl) -1H-pyrrole 4- (8-azabicyclo [3.2.1] oct-2-
(En-3-yl) -2- (4-fluorophenyl) -3
-(Pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (6-methyl-
1,2,3,6-tetrahydropyridin-4-yl)-
3- (pyridin-4-yl) -1H-pyrrole. 4- (1-ethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl)-
3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridine -4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-propyl-1,2,3,6-tetrahydropyridin-4-yl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-phenethyl-1,2,3,6-tetrahydropyridin-4-yl) -3- ( Pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,6,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 4- (1,6-dimethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3 -(Pyridin-4-yl) -1H-pyrrole 4- (1,2-dimethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- ( 4- (1-ethyl-6-methyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole Pyridin-4-yl) -1H-pyrrole 4- (1-ethyl-2-methyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- ( Pyridin-4-yl) -1H-pyrrole Orofeniru) -4- (6-methyl -
1-propyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (2-methyl-
1-propyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,3 4,
6,7,9a-Hexahydro-2H-quinolidine-8-
Yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (3,4-difluorophenyl) -4- (1,
2,3,5,6,8a-hexahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole 4- (1,2,3,5,6,8a-hexahydroindolizin-7-yl) -3- (pyridin-4- Il)-
2- (3-trifluoromethylphenyl) -1H-pyrrole Another object of the present invention is to provide a compound according to any one of the above (1) to (24), which is pharmaceutically acceptable. It is to provide a medicine containing a salt or a derivative as an active ingredient. The compound having the general formula (I) has a formula of any one of the following general formulas (I-1) to (I-5):

[0018]

Embedded image (Wherein, R ^1, R ² and R ³ are as defined above.) The above formula (I), in the definition of R ^1, "aryl group", and "Substituent group alpha, substituents “Aryl group” of the group β, an aryl group substituted with a group selected from the substituent group γ and the substituent group δ, and “selected from the substituent group α and the substituent group δ in the definition of R ^4. "Aryl group" of the "aryl group substituted with a group selected from the substituent group β and the substituent group γ"
Is, for example, phenyl, naphthyl, phenanthryl,
It represents an aromatic hydrocarbon group having 6 to 14 carbon atoms such as anthracenyl, and is preferably phenyl or naphthyl, and most preferably phenyl.

The "aryl group" may be condensed with a cycloalkyl group having 3 to 10 carbon atoms, and examples of such a group include 5-indanyl.

In the definition of R ¹ , “aryl group substituted with a group selected from substituent group α, substituent group β, substituent group γ and substituent group δ” is preferably a substituent group α Represents an aryl group substituted with 1 to 4 groups selected from a substituent group β, a substituent group γ, and a substituent group δ; more preferably, a substituent group α, a substituent group β, An aryl group substituted with 1 to 3 groups selected from group γ and substituent group δ. Preferred examples include 4-fluorophenyl,
3-fluorophenyl, 4-chlorophenyl, 3-chlorophenyl, 3,4-difluorophenyl, 3,4-dichlorophenyl, 3,4,5-trifluorophenyl,
3-chloro-4-fluorophenyl, 3-difluoromethoxyphenyl, 3-trifluoromethoxyphenyl,
Groups such as 3-trifluoromethylphenyl can be mentioned.

In the definition of R ⁴ , “aryl which may be substituted with a group selected from substituent group α and substituent group δ, and is substituted by a group selected from substituent group β and substituent group γ” The `` group '' may be preferably substituted with 1 to 2 groups selected from substituent group α and substituent group δ,
An aryl group substituted with one group selected from substituent group β and substituent group γ. Preferred examples include 2-aminophenyl, 3-aminophenyl, 4-aminophenyl, 2-aminomethylphenyl, 3-aminomethylphenyl, 4-aminomethylphenyl, 2- (2-aminoethyl) phenyl, -(2-aminoethyl) phenyl,
4- (2-aminoethyl) phenyl, 2-methylaminophenyl, 3-methylaminophenyl, 4-methylaminophenyl, 2- (dimethylamino) phenyl, 3-
(Dimethylamino) phenyl, 4- (dimethylamino)
Phenyl, 2-methylaminomethylphenyl, 3-methylaminomethylphenyl, 4-methylaminomethylphenyl, 2- (dimethylaminomethyl) phenyl, 3-
(Dimethylaminomethyl) phenyl, 4- (dimethylaminomethyl) phenyl, 3-amino-4-fluorophenyl, 3-amino-5-fluorophenyl, 2-aminomethyl-4-fluorophenyl, 3-amino-5 Chlorophenyl, 2-aminomethyl-3-chlorophenyl,
Examples include groups such as 3-amino-5-difluoromethoxyphenyl and 2-aminomethyl-3-trifluoromethoxyphenyl.

In the definition of R ¹ , “heteroaryl group” and “heteroaryl group substituted with a group selected from substituent group α, substituent group β, substituent group γ and substituent group δ” "heteroaryl group", and, in the definition of R ^4, is selected from "may be substituted with a group selected from substituent group α and substituent group [delta], substituent group β and substituent group γ The `` heteroaryl group '' of the `` heteroaryl group substituted with a group '' is, for example, furyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, tetrazolyl, thiadiazolyl, pyridyl, pyridazinyl, pyrimidinyl, Represents a 5- to 7-membered aromatic heterocyclic group containing 1 to 3 sulfur atoms, oxygen atoms and / or nitrogen atoms, such as pyrazinyl; Preferably, furyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl,
It is a 5- or 6-membered aromatic heterocyclic group containing one or two sulfur atoms, oxygen atoms and / or nitrogen atoms, such as pyranyl, pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl.

R ¹ is more preferably furyl,
Thienyl, pyridyl or pyrimidinyl.

R ⁴ more preferably contains at least one nitrogen atom, such as pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl and further comprises a sulfur atom A 5- or 6-membered aromatic heterocyclic group optionally containing one oxygen atom or nitrogen atom, even more preferably nitrogen such as imidazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, pyridyl or pyrimidinyl. A 5- or 6-membered aromatic heterocyclic group containing one or two atoms, particularly preferably pyridyl or pyrimidinyl.

The above “heteroaryl group” may be condensed with another cyclic group (for example, an aryl group, a cyclic group such as a cycloalkyl group having 3 to 10 carbon atoms),
Such groups include, for example, indolyl, benzofuranyl, benzothienyl, quinolyl, isoquinolyl, quinazolinyl, tetrahydroquinolyl, tetrahydroisoquinolyl, and the like.

In the definition of R ¹ , “heteroaryl group substituted with a group selected from substituent group α, substituent group β, substituent group γ and substituent group δ” is preferably a substituent group α represents a heteroaryl group substituted with 1 to 3 groups selected from a substituent group β, a substituent group γ, and a substituent group δ. More preferably, the substituent group α and the substituent group β And a heteroaryl group substituted with one or two groups selected from substituent group γ and substituent group δ. A preferred example is 5
-Fluoro-2-furyl, 4-chloro-2-thienyl,
Groups such as 5-difluoromethoxy-3-furyl, 5-trifluoromethoxy-3-thienyl, and 5-fluoro-2-oxazolyl can be mentioned.

In the definition of R ⁴ , “a heterocyclic group which may be substituted with a group selected from the substituent group α and the substituent group δ, and is substituted by a group selected from the substituent group β and the substituent group γ” The `` aryl group '' may be preferably substituted with one group selected from substituent group α and substituent group δ,
It is a heteroaryl group substituted with one group selected from substituent group β and substituent group γ. A preferred example is
5-amino-2-furyl, 5-aminomethyl-2-furyl, 5-methylaminomethyl-2-furyl, 5-dimethylaminomethyl-2-furyl, 5-amino-2-thienyl, 5-aminomethyl- 2-thienyl, 5-methylaminomethyl-2-thienyl, 5-dimethylaminomethyl-
2-thienyl, 5-amino-2-oxazolyl, 5-aminomethyl-2-oxazolyl, 2-amino-4-pyridyl, 2-amino-4-pyrimidinyl, 2-methylamino-4-pyridyl, 2-methylamino -4-pyrimidinyl, 2-benzylamino-4-pyridyl, 2-benzylamino-4-pyrimidinyl, 2- (α-methylbenzylamino) -4-pyridyl, 2- (α-methylbenzylamino) -4-pyrimidinyl , 5-amino-4-fluoro-2-furyl, 5-aminomethyl-4-fluoro-2-
Furyl, 5-amino-4-fluoro-2-thienyl, 5
-Aminomethyl-4-fluoro-2-thienyl, 4-amino-5-difluoromethoxy-2-furyl, 4-aminomethyl-5-difluoromethoxy-2-furyl, 4-
Amino-5-difluoromethoxy-2-thienyl, 4-
Groups such as aminomethyl-5-difluoromethoxy-2-thienyl can be mentioned.

In the definition of R ² , “heteroaryl group having at least one nitrogen atom” and “substituted group selected from substituent group α, substituent group β, substituent group γ and substituent group δ” been, heteroaryl group "having at least one" nitrogen atom of the heteroaryl group "having at least one nitrogen atom, and" a group selected from substituent group α and substituent group δ in the definition of R ⁴ The `` heteroaryl group having at least one nitrogen atom '' which may be substituted with `` heteroaryl group having at least one nitrogen atom '' is pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl,
It contains at least one nitrogen atom, such as isothiazolyl, triazolyl, tetrazolyl, thiadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, and further contains one or two sulfur, oxygen and / or nitrogen atoms. And a 5- to 7-membered aromatic heterocyclic group. Preferably it contains one nitrogen atom, such as pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl,
It is a 5- or 6-membered aromatic heterocyclic group which may further contain one sulfur atom, oxygen atom or nitrogen atom, and more preferably, such as imidazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, pyridinyl or pyrimidinyl. And a 5- or 6-membered aromatic heterocyclic group containing one or two nitrogen atoms, particularly preferably pyridyl or pyrimidinyl.

For R ² it is optimally 4-pyridyl or 4-pyrimidinyl.

In the definition of R ² , “heteroaryl group having at least one nitrogen atom substituted with a group selected from substituent group α, substituent group β, substituent group γ and substituent group δ” And preferably represents a group substituted with 1 to 3 groups selected from a substituent group α, a substituent group β, a substituent group γ, and a substituent group δ. More preferably, the substituent group α, a group of substituents β, a group substituted with one or two groups selected from a group of substituents γ and a group of substituents δ, even more preferably
Substituent group α, substituent group β, substituent group γ and a group substituted with one group selected from substituent group δ, particularly preferably, substituent group α, substituent group β, 4-pyridyl or 4-pyrimidinyl substituted at the 2-position with one group selected from substituent group γ and substituent group δ, most preferably selected from substituent group β and substituent group γ Is 4-pyridyl or 4-pyrimidinyl substituted at the 2-position with one group. Preferred examples include 2-amino-4-pyridyl, 2-amino-4-pyrimidinyl, 2-methylamino-4-pyridyl, 2-methylamino-4-pyrimidinyl, 2-methoxy-4-pyridinyl, Methoxy-4-
Pyrimidinyl, 2-benzylamino-4-pyridyl, 2
Groups such as -benzylamino-4-pyrimidinyl, 2- (α-methylbenzylamino) -4-pyridyl, and 2- (α-methylbenzylamino) -4-pyrimidinyl.

The “heteroaryl group having at least one nitrogen atom which may be substituted with a group selected from the substituent group α and the substituent group δ” in the definition of R ⁴ is preferably a substituent A heteroaryl group having at least one nitrogen atom, which may be substituted with one or two groups selected from the group α and the substituent group δ, more preferably the substituent group α and the substituent A heteroaryl group having at least one nitrogen atom which may be substituted with one group selected from the group δ. A preferred example is 2-
Methyl-4-pyridyl, 2-ethyl-4-pyridyl, 2
-Benzyl-4-pyridyl, 2-phenethyl-4-pyridyl, 2-fluoro-4-pyridyl, 2,6-difluoro-4-pyridyl, 2,3,5,6-tetrafluoro-
Groups such as 4-pyridyl can be mentioned.

In the definition of X, the "lower alkylene group" in the "lower alkylene group" and the "lower alkylene group substituted with a group selected from the substituent group α" are methylene, ethylene, trimethylene, propylene, Tetramethylene, 1-methyltrimethylene, 2-methyltrimethylene, 1,1-dimethylethylene, pentamethylene,
It represents a linear or branched alkylene group having 1 to 6 carbon atoms such as 1,1-dimethyltrimethylene and hexamethylene. Preferably, it is a straight-chain or branched-chain alkylene group having 1 to 4 carbon atoms, more preferably, a straight-chain or branched-chain alkylene group having 1 to 3 carbon atoms. , Ethylene or trimethylene.

In the definition of X, the "lower alkenylene group" of the "lower alkenylene group" and the "lower alkenylene group substituted with a group selected from the substituent group α" are as follows:
A linear or branched alkenylene group having 2 to 6 carbon atoms such as vinylene, 1-methylvinylene, propenylene, 1-butenylene, 2-butenylene, 1-pentenylene, 2-pentenylene and the like; It is a straight-chain or branched-chain alkenylene group having 2 to 4 carbon atoms, more preferably vinylene, propenylene or butenylene, and particularly preferably vinylene or propenylene.

In the definition of X, “lower alkynylene group” and “lower alkynylene group” of “lower alkynylene group substituted with a group selected from substituent group α” include
A linear or branched alkynylene group having 2 to 6 carbon atoms, preferably a linear or branched alkynylene group having 2 to 4 carbon atoms, more preferably ethynylene, propynylene, -Butynylene or 2-butynylene, particularly preferably ethynylene or propynylene.

The "cycloalkyl group" in the definition of [Substituent group δ] and the "Substituent group α in the definition of R ⁴
And a cycloalkyl group which may be substituted with a group selected from the substituent group δ, and a cycloalkyl group substituted with a group selected from the substituent group β and the substituent group γ, Propyl, cyclobutyl, cyclopentyl,
A cycloalkyl group having 3 to 7 carbon atoms such as cyclohexyl and cycloheptanyl;
From 6 to 6 cycloalkyl groups.

In the definition of R ⁴ , “may be substituted with a group selected from substituent group α and substituent group δ, and substituted with a group selected from substituent group β and substituent group γ. The “heterocyclyl group” of the “heterocyclyl group” is a 4- to 14-membered non-aromatic heterocyclic group having 1 or 2 or more ring structures and having 1 to 3 sulfur atoms, oxygen atoms and / or nitrogen atoms. Is shown. It preferably represents a 4- to 12-membered non-aromatic heterocyclic group containing 1 or 2 sulfur atoms, oxygen atoms and / or nitrogen atoms (preferably a 4- to 10-membered non-aromatic heterocyclic group), More preferably, it is a 4- to 12-membered non-aromatic heterocyclic group (preferably 4- to 10-membered) which contains one nitrogen atom and may further contain one oxygen atom, sulfur atom or nitrogen atom. An aromatic heterocyclic group), such groups include, for example, azetidinyl, pyrrolidinyl, pyrrolinyl, imidazolidinyl, imidazolinyl, pyrazolidinyl, pyrazolinyl, oxazolidinyl, thiazolidinyl, piperidyl, tetrahydropyridyl, dihydropyridyl, piperazinyl, morpholinyl, morpholinyl, morpholinyl, morpholinyl Homopiperidyl, quinuclidinyl, quinuclidienyl, octahydroindolidinyl, hexa Mud indolizidine sulfonyl, octahydroquinazolin glue isoxazolidinyl, hexahydroxoplatinate glue isoxazolidinyl, 8-azabicyclo [3.2.1] octanyl, 8-azabicyclo [3.2.1] octenyl, 9
Azabicyclo [3.3.1] nonenyl and 9-azabicyclo [3.3.1] nonenyl can be exemplified. Of these, piperidyl, tetrahydropyridyl, homopiperidyl, quinuclidinyl, quinuclidienyl, octahydroindolizinyl, hexahydroindolizinyl,
Octahydroquinolidinyl, hexahydroquinolidinyl, 8-azabicyclo [3.2.1] octanyl, 8-
Azabicyclo [3.2.1] octenyl, 9-azabicyclo [3.3.1] nonanyl and 9-azabicyclo [3.3.1] nonenyl are preferred and include tetrahydropyridyl, quinuclidienyl, hexahydroindolidinyl, hexa Hydroquinolizinyl, 8-azabicyclo [3.2.1] octenyl and 9-azabicyclo [3.
3.1] Nonenyl is more preferred, and tetrahydropyridyl, hexahydroindolidinyl and hexahydroquinolizinyl are even more preferred.

The above "heterocyclyl group" may be condensed with an aryl group or a heteroaryl group. Examples of such a group include tetrahydroquinolinyl,
Groups such as tetrahydroisoquinolinyl, chromanyl, indolinyl, and isoindolinyl can be mentioned.

In the definition of R ⁴ , “heterocyclyl group having at least one nitrogen atom which may be substituted with a group selected from substituent group α and substituent group δ”, “at least one nitrogen atom Heterocyclyl group having "
Refers to “containing one nitrogen atom in the above“ heterocyclyl group ”and further containing one oxygen atom, sulfur atom or nitrogen atom.
And a 4- to 12-membered non-aromatic heterocyclic group which may be contained therein. Preferably, it contains one nitrogen atom,
An oxygen atom, a sulfur atom or a nitrogen-containing 4 to 10-membered non-aromatic heterocyclic group which may contain one atom, such as azetidinyl, pyrrolidinyl, pyrrolinyl, imidazolidinyl, imidazolinyl, pyrazolidinyl, Pyrazolinyl, oxazolidinyl, thiazolidinyl, piperidyl, tetrahydropyridyl, dihydropyridyl, piperazinyl, morpholinyl, thiomorpholinyl, homopiperidyl, quinuclidinyl, quinuclidienyl, octahydroindolinidinyl, hexahydroindolinidinyl, octahydroquinolinidinyl, hexahydroquinolinidinyl 8-azabicyclo [3.2.1] octanyl, 8-azabicyclo [3.2.1] octenyl, 9-
Azabicyclo [3.3.1] nonenyl and 9-azabicyclo [3.3.1] nonenyl can be exemplified. Of these, piperidyl, tetrahydropyridyl, homopiperidyl, quinuclidinyl, quinuclidienyl, octahydroindolizinyl, hexahydroindolizinyl,
Octahydroquinolidinyl, hexahydroquinolidinyl, 8-azabicyclo [3.2.1] octanyl, 8-
Azabicyclo [3.2.1] octenyl, 9-azabicyclo [3.3.1] nonanyl and 9-azabicyclo [3.3.1] nonenyl are preferred and include tetrahydropyridyl, quinuclidienyl, hexahydroindolidinyl, hexa Hydroquinolizinyl, 8-azabicyclo [3.2.1] octenyl and 9-azabicyclo [3.
3.1] Nonenyl is more preferred, and tetrahydropyridyl, hexahydroindolidinyl and hexahydroquinolizinyl are even more preferred.

The “heterocyclyl group having at least one nitrogen atom” may be condensed with an aryl group or a heteroaryl group. Examples of such a group include tetrahydroquinolinyl and tetrahydroiso. Groups such as quinolinyl, indolinyl and isoindolinyl can be mentioned.

R ^a , R ^b , R ^c , R ^d and “lower alkyl group” in the definition of [substituent group δ]; “group having -NR ^c R ^d in the definition of [substituent group γ] (formula Medium, R ^c and R ^d
Is as defined above. )), “Lower alkyl group” of “lower alkyl group”; and “lower alkyl group of“ lower alkyl group substituted with group selected from substituent group α ”in the definition of [substituent group δ]. "Means methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, s-butyl, tert-butyl, n-pentyl,
Isopentyl, 2-methylbutyl, neopentyl, 1-
Ethylpropyl, n-hexyl, isohexyl, 4-methylpentyl, 3-methylpentyl, 2-methylpentyl, 1-methylpentyl, 3,3-dimethylbutyl,
2,2-dimethylbutyl, 1,1-dimethylbutyl,
1,2-dimethylbutyl, 1,3-dimethylbutyl,
And represents a linear or branched alkyl group having 1 to 6 carbon atoms such as 2,3-dimethylbutyl and 2-ethylbutyl. Preferably, it is an alkyl group having 1 to 4 carbon atoms,
More preferably, it is methyl, ethyl or propyl, particularly preferably methyl or ethyl.

R ^a , R ^b , R ^c , R ^d and “lower alkenyl group” in the definition of [substituent group δ]; and “substituent group α in the definition of [substituent group δ]. The lower alkenyl group of the "lower alkenyl group substituted with a group" means vinyl, 2-propenyl, 1-methyl-2-propenyl, 2-methyl-2-propenyl, 2-ethyl-2-
Propenyl, 2-butenyl, 1-methyl-2-butenyl, 2-methyl-2-butenyl, 1-ethyl-2-butenyl, 3-butenyl, 1-methyl-3-butenyl, 2-
Methyl-3-butenyl, 1-ethyl-3-butenyl, 2
-Pentenyl, 1-methyl-2-pentenyl, 2-methyl-2-pentenyl, 3-pentenyl, 1-methyl-3
-Pentenyl, 2-methyl-3-pentenyl, 4-pentenyl, 1-methyl-4-pentenyl, 2-methyl-4
-Pentenyl, 2-hexenyl, 3-hexenyl, 4-
And represents a linear or branched alkenyl group having 2 to 6 carbon atoms such as hexenyl and 5-hexenyl. Preferably,
An alkenyl group having 2 to 4 carbon atoms, more preferably an alkenyl group having 2 or 3 carbon atoms.

R ^a , R ^b , R ^c , R ^d and “lower alkynyl group” in the definition of [substituent group δ]; and “substituent group α in the definition of [substituent group δ]. The lower alkynyl group of the "lower alkynyl group substituted with a group" is ethynyl, 2-propynyl, 1-methyl-2-propynyl, 2-butynyl, 1-methyl-2-butynyl,
-Ethyl-2-butynyl, 3-butynyl, 1-methyl-
3-butynyl, 2-methyl-3-butynyl, 1-ethyl-3-butynyl, 2-pentynyl, 1-methyl-2-pentynyl, 3-pentynyl, 1-methyl-3-pentynyl, 2-methyl-3- Pentynyl, 4-pentynyl, 1
Represents a straight-chain or branched-chain alkynyl group having 2 to 6 carbon atoms, such as -methyl-4-pentynyl, 2-methyl-4-pentynyl, 2-hexynyl, 3-hexynyl, 4-hexynyl and 5-hexynyl. . Preferably, it has 2 carbon atoms.
It is an alkynyl group having 2 to 3 carbon atoms, and more preferably an alkynyl group having 2 or 3 carbon atoms.

The “aralkyl group” in the definitions of R ^a , R ^b , R ^c , R ^d and [substituent group δ] is a group in which the above “aryl group” is bonded to the above “lower alkyl group”, Such groups include, for example, benzyl, indenylmethyl, phenanthrenylmethyl, anthracenylmethyl, α-naphthylmethyl, β-naphthylmethyl, diphenylmethyl, triphenylmethyl, α-naphthyldiphenylmethyl, 9- -Anthrylmethyl, piperonyl, 1-
Phenethyl, 2-phenethyl, 1-naphthylethyl, 2
-Naphthylethyl, 1-phenylpropyl, 2-phenylpropyl, 3-phenylpropyl, 1-naphthylpropyl, 2-naphthylpropyl, 3-naphthylpropyl,
1-phenylbutyl, 2-phenylbutyl, 3-phenylbutyl, 4-phenylbutyl, 1-naphthylbutyl,
2-naphthylbutyl, 3-naphthylbutyl, 4-naphthylbutyl, 1-phenylpentyl, 2-phenylpentyl, 3-phenylpentyl, 4-phenylpentyl, 5
-Phenylpentyl, 1-naphthylpentyl, 2-naphthylpentyl, 3-naphthylpentyl, 4-naphthylpentyl, 5-naphthylpentyl, 1-phenylhexyl, 2-phenylhexyl, 3-phenylhexyl, 4
-Phenylhexyl, 5-phenylhexyl, 6-phenylhexyl, 1-naphthylhexyl, 2-naphthylhexyl, 3-naphthylhexyl, 4-naphthylhexyl, 5-naphthylhexyl, and 6-naphthylhexyl. Of these, benzyl, phenanthrenylmethyl, anthracenylmethyl, α-naphthylmethyl, β-naphthylmethyl, diphenylmethyl, triphenylmethyl, 9-anthrylmethyl, piperonyl,
1-phenethyl, 2-phenethyl, 1-phenylpropyl, 2-phenylpropyl, 3-phenylpropyl, 1
-Phenylbutyl, 2-phenylbutyl, 3-phenylbutyl and 4-phenylbutyl are preferred.

The aryl part of the “aralkyl group” is 1 to 3 selected from the above “substituent group α”, “substituent group β”, “substituent group γ” and “substituent group δ”. And such substituted aralkyl groups include, for example, 2-fluorobenzyl,
Fluorobenzyl, 4-fluorobenzyl, 2-chlorobenzyl, 3-chlorobenzyl, 4-chlorobenzyl,
2-bromobenzyl, 3-bromobenzyl, 4-bromobenzyl, 3,5-difluorobenzyl, 2,5-difluorophenethyl, 2,6-difluorobenzyl, 2,
4-difluorophenethyl, 3,5-dibromobenzyl, 2,5-dibromophenethyl, 2,6-dichlorobenzyl, 2,4-dichlorophenethyl, 2,3,6-trifluorobenzyl, 2,3,4-triphenyl Fluorophenethyl, 3,4,5-trifluorobenzyl, 2,5,6
-Trifluorophenethyl, 2,4,6-trifluorobenzyl, 2,3,6-tribromophenethyl, 2,
3,4-tribromobenzyl, 3,4,5-tribromophenethyl, 2,5,6-trichlorobenzyl, 2,
4,6-trichlorophenethyl, 1-fluoro-2-naphthylmethyl, 2-fluoro-1-naphthylethyl, 3
-Fluoro-1-naphthylmethyl, 1-chloro-2-naphthylethyl, 2-chloro-1-naphthylmethyl, 3-
Bromo-1-naphthylethyl, 3,8-difluoro-1
-Naphthylmethyl, 2,3-difluoro-1-naphthylethyl, 4,8-difluoro-1-naphthylmethyl,
5,6-difluoro-1-naphthylethyl, 3,8-dichloro-1-naphthylmethyl, 2,3-dichloro-1-
Naphthylethyl, 4,8-dibromo-1-naphthylmethyl, 5,6-dibromo-1-naphthylethyl, 2,3
6-trifluoro-1-naphthylmethyl, 2,3,4-
Trifluoro-1-naphthylethyl, 3,4,5-trifluoro-1-naphthylmethyl, 4,5,6-trifluoro-1-naphthylethyl, 2,4,8-trifluoro-1-naphthylmethyl, Bis (2-fluorophenyl)
Methyl, 3-fluorophenylphenylmethyl, bis (4-fluorophenyl) methyl, 4-fluorophenylphenylmethyl, bis (2-chlorophenyl) methyl, bis (3-chlorophenyl) methyl, bis (4-chlorophenyl) methyl, -Chlorophenylphenylmethyl, 2-bromophenylphenylmethyl, 3-bromophenylphenylmethyl, bis (4-bromophenyl)
Methyl, bis (3,5-difluorophenyl) methyl,
Bis (2,5-difluorophenyl) methyl, bis (2,6-difluorophenyl) methyl, 2,4-difluorophenylphenylmethyl, bis (3,5-dibromophenyl) methyl, 2,5-dibromophenylphenylmethyl , 2,6-dichlorophenylphenylmethyl,
Bis (2,4-dichlorophenyl) methyl, bis (2
Aralkyl groups substituted by halogen atoms such as 3,6-trifluorophenyl) methyl; 2-trifluoromethylbenzyl, 3-trifluoromethylphenethyl,
-Trifluoromethylbenzyl, 2-trichloromethylphenethyl, 3-dichloromethylbenzyl, 4-trichloromethylphenethyl, 2-tribromomethylbenzyl, 3-dibromomethylphenethyl, 4-dibromomethylbenzyl, 3,5-bistrifluoromethyl Phenethyl, 2,5-bistrifluoromethylbenzyl, 2,6
-Bistrifluoromethylphenethyl, 2,4-bistrifluoromethylbenzyl, 3,5-bistribromomethylphenethyl, 2,5-bisdibromomethylbenzyl, 2,6-bisdichloromethylmethylphenethyl,
2,4-bisdichloromethylbenzyl, 2,3,6-tristrifluoromethylphenethyl, 2,3,4-tristrifluoromethylbenzyl, 3,4,5-tristrifluoromethylphenethyl, 2,5,6 -Tristrifluoromethylbenzyl, 2,4,6-tristrifluoromethylphenethyl, 2,3,6-tristribromobromobenzyl, 2,3,4-trisdibromomethylphenethyl, 3,4,5-tristri Bromomethylbenzyl, 2,5,6-trisdichloromethylmethylphenethyl, 2,4,6-trisdichloromethylbenzyl, 1-
Trifluoromethyl-2-naphthylethyl, 2-trifluoromethyl-1-naphthylmethyl, 3-trifluoromethyl-1-naphthylethyl, 1-trichloromethyl-
2-naphthylmethyl, 2-dichloromethyl-1-naphthylethyl, 3-tribromomethyl-1-naphthylmethyl, 3,8-bistrifluoromethyl-1-naphthylethyl, 2,3-bistrifluoromethyl-1-naphthyl Methyl, 4,8-bistrifluoromethyl-1-naphthylethyl, 5,6-bistrifluoromethyl-1-naphthylmethyl, 3,8-bistrichloromethyl-1-naphthylethyl, 2,3-bisdichloromethyl-1 -Naphthylmethyl, 4,8-bisdibromomethyl-1-naphthylethyl, 5,6-bistribromomethyl-1-naphthylmethyl, 2,3,6-tristrifluoromethyl-1-
Naphthylethyl, 2,3,4-tristrifluoromethyl-1-naphthylmethyl, 3,4,5-tristrifluoromethyl-1-naphthylethyl, 4,5,6-tristrifluoromethyl-1-naphthylmethyl , 2,4,8
-Tristrifluoromethyl-1-naphthylmethyl, bis (4-trifluoromethylphenyl) methyl, 4-trifluoromethylphenylphenylmethyl, bis (2-
Trichloromethylphenyl) methyl, bis (3-trichloromethylphenyl) methyl, bis (4-trichloromethylphenyl) methyl, 2-tribromomethylphenylphenylmethyl, 3-tribromomethylphenylphenylmethyl, bis (4-tribromo Methylphenyl) methyl, bis (3,5-bistrifluoromethylphenyl)
Methyl, bis (2,5-bistrifluoromethylphenyl) methyl, bis (2,6-bistrifluoromethylphenyl) methyl, 2,4-bistrifluoromethylphenylphenylmethyl, bis (3,5-bistrifluorobromophenyl) Methyl, 2,5-bistribromomethylphenylphenylmethyl, 2,6-bistrichloromethylphenylphenylmethyl, bis (2,4-bistrichloromethylphenyl) methyl, bis (2,3,6-tristrifluoromethylphenyl) ) Aralkyl groups substituted with halogeno lower alkyl groups such as methyl; 2-methylbenzyl, 3-methylbenzyl, 4-methylbenzyl, 2-methylphenethyl, 4-methylphenethyl,
-Ethylbenzyl, 3-propylphenethyl, 4-ethylbenzyl, 2-butylphenethyl, 3-pentylbenzyl, 4-pentylphenethyl, 3,5-dimethylbenzyl, 2,5-dimethylphenethyl, 2,6-dimethylbenzyl, 2,4-dimethylphenethyl, 3,5-dibutylbenzyl, 2,5-dipentylphenethyl, 2,6
-Dipropylbenzyl, 2,4-dipropylphenethyl, 2,3,6-trimethylbenzyl, 2,3,4-trimethylphenethyl, 3,4,5-trimethylbenzyl, 2,4,6-trimethylbenzyl, , 5,6-trimethylphenethyl, 2,3,6-tributylphenethyl, 2,3,4-tripentylbenzyl, 3,4,5-
Tributylphenethyl, 2,5,6-tripropylbenzyl, 2,4,6-tripropylphenethyl, 1-methyl-2-naphthylmethyl, 2-methyl-1-naphthylethyl, 3-methyl-1-naphthylmethyl, 1-ethyl-
2-naphthylethyl, 2-propyl-1-naphthylmethyl, 3-butyl-1-naphthylethyl, 3,8-dimethyl-1-naphthylmethyl, 2,3-dimethyl-1-naphthylethyl, 4,8-dimethyl -1-naphthylmethyl,
5,6-dimethyl-1-naphthylethyl, 3,8-diethyl-1-naphthylmethyl, 2,3-dipropyl-1-
Naphthylmethyl, 4,8-dipentyl-1-naphthylethyl, 5,6-dibutyl-1-naphthylmethyl, 2,
3,6-trimethyl-1-naphthylmethyl, 2,3,4
-Trimethyl-1-naphthylethyl, 3,4,5-trimethyl-1-naphthylmethyl, 4,5,6-trimethyl-1-naphthylmethyl, 2,4,8-trimethyl-1-
Naphthylmethyl, bis (2-methylphenyl) methyl,
3-methylphenylphenylmethyl, bis (4-methylphenyl) methyl, 4-methylphenylphenylmethyl, bis (2-ethylphenyl) methyl, bis (3-ethylphenyl) methyl, bis (4-ethylphenyl) methyl, 2-propylphenylphenylmethyl, 3-propylphenylphenylmethyl, bis (4-propylphenyl) methyl, bis (3,5-dimethylphenyl) methyl, bis (2,5-dimethylphenyl) methyl, bis (2,6 -Dimethylphenyl) methyl, 2,4-dimethylphenylphenylmethyl, bis (3,5-dipropylphenyl) methyl, 2,5-dipropylphenylphenylmethyl, 2,6-diethylphenylphenylmethyl,
Bis (2,4-diethylphenyl) methyl, bis (2
An aralkyl group substituted with a lower alkyl group such as 3,6-trimethylphenyl) methyl; 2-methoxybenzyl, 3-methoxybenzyl, 4-methoxybenzyl,
-Methoxyphenethyl, 2-ethoxyphenethyl, 3-
Propoxybenzyl, 4-ethoxyphenethyl, 2-butoxybenzyl, 3-pentoxyphenethyl, 4-pentoxybenzyl, 3,5-dimethoxyphenethyl, 2,
5-dimethoxybenzyl, 2,6-dimethoxyphenethyl, 2,4-dimethoxybenzyl, 3,5-dibutoxyphenethyl, 2,5-dipentoxybenzyl, 2,6-
Dipropoxyphenethyl, 2,4-dipropoxybenzyl, 2,3,6-trimethoxyphenethyl, 2,3,4
-Trimethoxybenzyl, 3,4,5-trimethoxyphenethyl, 2,5,6-trimethoxybenzyl, 2,
4,6-trimethoxyphenethyl, 2,3,6-tributoxybenzyl, 2,3,4-tripentoxyphenethyl, 3,4,5-tributoxybenzyl, 2,5,6-
Tripropoxyphenethyl, 2,4,6-tripropoxybenzyl, 1-methoxy-2-naphthylmethyl, 2-
Methoxy-1-naphthylmethyl, 3-methoxy-1-naphthylethyl, 1-ethoxy-2-naphthylmethyl, 2
-Propoxy-1-naphthylmethyl, 3-butoxy-1
-Naphthylethyl, 3,8-dimethoxy-1-naphthylmethyl, 2,3-dimethoxy-1-naphthylmethyl,
4,8-dimethoxy-1-naphthylethyl, 5,6-dimethoxy-1-naphthylmethyl, 3,8-diethoxy-
1-naphthylmethyl, 2,3-dipropoxy-1-naphthylethyl, 4,8-dipentoxy-1-naphthylmethyl, 5,6-dibutoxy-1-naphthylmethyl, 2,
3,6-trimethoxy-1-naphthylethyl, 2,3
4-trimethoxy-1-naphthylmethyl, 3,4,5-
Trimethoxy-1-naphthylmethyl, 4,5,6-trimethoxy-1-naphthylethyl, 2,4,8-trimethoxy-1-naphthylmethyl, bis (2-methoxyphenyl) methyl, 3-methoxyphenylphenylmethyl, bis (4-methoxyphenyl) methyl, 4-methoxyphenylphenylmethyl, bis (2-ethoxyphenyl) methyl, bis (3-ethoxyphenyl) methyl, bis (4
-Ethoxyphenyl) methyl, 2-propoxyphenylphenylmethyl, 3-propoxyphenylphenylmethyl, bis (4-propoxyphenyl) methyl, bis (3,5-dimethoxyphenyl) methyl, bis (2,5
-Dimethoxyphenyl) methyl, bis (2,6-dimethoxyphenyl) methyl, 2,4-dimethoxyphenylphenylmethyl, bis (3,5-dipropoxyphenyl)
Methyl, 2,5-dipropoxyphenylphenylmethyl, 2,6-diethoxyphenylphenylmethyl, bis (2,4-diethoxyphenyl) methyl, bis (2
An aralkyl group substituted with a lower alkoxy group such as 3,6-trimethoxyphenyl) methyl; 2-aminophenethyl, 3-aminobenzyl, 4-aminophenethyl,
3,5-diaminobenzyl, 2,5-diaminophenethyl, 2,6-diaminobenzyl, 2,4-diaminophenethyl, 2,3,6-triaminobenzyl, 2,3,4
-Triaminophenethyl, 3,4,5-triaminobenzyl, 2,5,6-triaminophenethyl, 2,4,6
-Triaminobenzyl, 1-amino-2-naphthylmethyl, 2-amino-1-naphthylethyl, 3-amino-1
-Naphthylmethyl, 3,8-diamino-1-naphthylmethyl, 2,3-diamino-1-naphthylethyl, 4,8
-Diamino-1-naphthylmethyl, 5,6-diamino-
1-naphthylmethyl, 2,3,6-triamino-1-naphthylethyl, 2,3,4-triamino-1-naphthylmethyl, 3,4,5-triamino-1-naphthylmethyl, 4,5,6- Triamino-1-naphthylethyl,
2,4,8-triamino-1-naphthylmethyl, bis (2-aminophenyl) methyl, 3-aminophenylphenylmethyl, bis (4-aminophenyl) methyl,
-Aminophenylphenylmethyl, bis (3,5-diaminophenyl) methyl, bis (2,5-diaminophenyl) methyl, bis (2,6-diaminophenyl) methyl, 2,4-diaminophenylphenylmethyl, bis ( An aralkyl group substituted with an amino group such as (2,3,6-triaminophenyl) methyl; 2-nitrophenethyl, 3-nitrobenzyl, 4-nitrobenzyl, 4-nitrophenethyl, 3,5-dinitrobenzyl, 2,5-
Dinitrophenethyl, 2,6-dinitrobenzyl, 2,
4-dinitrophenethyl, 2,3,6-trinitrobenzyl, 2,3,4-trinitrophenethyl, 3,4,5
-Trinitrobenzyl, 2,5,6-trinitrophenethyl, 2,4,6-trinitrobenzyl, 1-nitro-
2-naphthylmethyl, 2-nitro-1-naphthylethyl, 3-nitro-1-naphthylmethyl, 3,8-dinitro-1-naphthylmethyl, 2,3-dinitro-1-naphthylethyl, 4,8-dinitro -1-naphthylmethyl,
5,6-dinitro-1-naphthylmethyl, 2,3,6-
Trinitro-1-naphthylethyl, 2,3,4-trinitro-1-naphthylmethyl, 3,4,5-trinitro-
1-naphthylmethyl, 4,5,6-trinitro-1-naphthylethyl, 2,4,8-trinitro-1-naphthylmethyl, bis (2-nitrophenyl) methyl, 3-nitrophenylphenylmethyl, bis (4 -Nitrophenyl)
Methyl, 4-nitrophenylphenylmethyl, bis (3,5-dinitrophenyl) methyl, bis (2,5-
An aralkyl group substituted with a nitro group such as dinitrophenyl) methyl, bis (2,6-dinitrophenyl) methyl, 2,4-dinitrophenylphenylmethyl, bis (2,3,6-trinitrophenyl) methyl; And 2-
Cyanophenethyl, 3-cyanobenzyl, 4-cyanobenzyl, 4-cyanobenzyldiphenylmethyl, 4-cyanophenethyl, 3,5-dicyanobenzyl, 2,5-
Dicyanophenethyl, 2,6-dicyanobenzyl, 2,
4-dicyanophenethyl, 2,3,6-tricyanobenzyl, 2,3,4-tricyanophenethyl, 3,4,5
-Tricyanobenzyl, 2,5,6-tricyanophenethyl, 2,4,6-tricyanobenzyl, 1-cyano-
2-naphthylmethyl, 3-cyano-1-naphthylmethyl, 3,8-dicyano-1-naphthylmethyl, 2,3-
Dicyano-1-naphthylethyl, 4,8-dicyano-1
-Naphthylmethyl, 5,6-dicyano-1-naphthylmethyl, 2,3,6-tricyano-1-naphthylethyl,
2,3,4-tricyano-1-naphthylmethyl, 3,
4,5-tricyano-1-naphthylmethyl, 4,5,6
-Tricyano-1-naphthylethyl, 2,4,8-tricyano-1-naphthylmethyl, bis (2-cyanophenyl) methyl, 3-cyanophenylphenylmethyl, bis (4-cyanophenyl) methyl, 4-cyanophenyl Phenylmethyl, bis (3,5-dicyanophenyl) methyl, bis (2,5-dicyanophenyl) methyl, bis (2,6-dicyanophenyl) methyl, 2,4-dicyanophenylphenylmethyl, bis (2,3 Aralkyl groups substituted with a cyano group such as (6,6-tricyanophenyl) methyl.

It is preferably an unsubstituted aralkyl group or an aralkyl group substituted with a halogen atom, a lower alkyl group or a lower alkoxy group, and more preferably an unsubstituted aralkyl group or a halogen atom or a lower alkyl group. It is a substituted aralkyl group, most preferably an unsubstituted aralkyl group.

The “lower alkylsulfonyl group” in the definition of R ^a , R ^b , R ^c and R ^d is the above “lower alkyl”
Represents a group to which sulfonyl (—SO ₂ —) is bonded. Preferably, it is a linear or branched alkylsulfonyl group having 1 to 4 carbon atoms, more preferably, methylsulfonyl, ethylsulfonyl, propylsulfonyl, isopropylsulfonyl, butylsulfonyl, and particularly preferably, Methylsulfonyl, ethylsulfonyl and propylsulfonyl.

The heterocyclyl group formed by R ^c and R ^d together with the nitrogen atom to which they are bonded is defined as “heterocyclyl group having at least one nitrogen atom” in the above “nitrocyclyl group”. Represents a group bonded to
Such groups include, for example, 1-azetidinyl, 1
-Pyrrolidinyl, 1-pyrrolinyl, 1-imidazolidinyl, 1-imidazolinyl, 1-pyrazolidinyl, 1-pyrazolinyl, 3-oxazolidinyl, 3-thiazolidinyl, 1-piperidyl, tetrahydropyridin-1-yl, dihydropyridin-1-yl, 1- Piperazinyl,
4-morpholinyl, 4-thiomorpholinyl, 1-homopiperidyl, 8-azabicyclo [3.2.1] octane-
8-yl, 8-azabicyclo [3.2.1] octene-
8-yl, 9-azabicyclo [3.3.1] nonane-9
-Yl, 9-azabicyclo [3.3.1] nonene-9-
Ill.

These groups may be condensed with an aryl group or a heteroaryl group. Examples of such a group include tetrahydroquinolin-1-yl and tetrahydroisoquinolin-2-yl. Groups can be mentioned.

The "halogen atom" in the definition of [Substituent group α] includes a fluorine atom, a chlorine atom, a bromine atom and an iodine atom.
It is a chlorine atom.

The "lower alkoxy group" in the definition of [substituent group α] indicates a group in which an oxygen atom is bonded to the above "lower alkyl group". Preferably, it is a linear or branched alkoxy group having 1 to 4 carbon atoms, more preferably methoxy, ethoxy, propoxy, isopropoxy, butoxy, and particularly preferably methoxy, ethoxy, propoxy. It is.

The “halogeno lower alkoxy group” in the definition of [Substituent group α] is a group in which one or more hydrogen atoms of the above “lower alkoxy group” are substituted with the above “halogen atom”. . Preferably, it has 1 to 4 carbon atoms.
Halogeno lower alkoxy groups, more preferably difluoromethoxy, trifluoromethoxy, 2,2,2
-Trifluoroethoxy, particularly preferably difluoromethoxy.

The “lower alkylthio group” in the definition of [Substituent group α] indicates a group in which a sulfur atom is bonded to the above “lower alkyl group”. Preferably, it is a linear or branched alkylthio group having 1 to 4 carbon atoms, more preferably, methylthio, ethylthio, propylthio, isopropylthio, butylthio, and particularly preferably, methylthio, ethylthio, propylthio. It is.

The “halogeno lower alkylthio group” in the definition of [Substituent group α] is a group in which one or more hydrogen atoms of the above “lower alkylthio group” are substituted by the above “halogen atom”. . It is preferably a halogeno lower alkylthio group having 1 to 4 carbon atoms, more preferably difluoromethylthio, trifluoromethylthio,
2,2,2-trifluoroethylthio.

Among the groups defined as “substituent group α”, a preferred group of groups is “substituent group α ¹ ”, which comprises a halogen atom, a lower alkoxy group and a halogeno lower alkoxy group.

A group defined as "substituent group β"
A preferred group of groups is “substituent group β ¹And this
Is -NR^cR^dA group having the formula (wherein, R^cAnd R^dOne of them is
Represents a hydrogen atom or a lower alkyl group, the other being a hydrogen atom,
Indicates a lower alkyl group or an aralkyl group. ).

A group defined as "substituent group γ"
A preferred group of groups is “substituent group γ ¹And this
Is an amino lower alkyl group, a lower alkylamino lower
Alkyl group, di (lower alkyl) amino lower alkyl group,
And an aralkylamino lower alkyl group.

In the definition of “substituent group γ ¹ ”, “amino lower alkyl group”, “lower alkylamino lower alkyl group”, “di (lower alkyl) amino lower alkylamino group” and “aralkylamino lower alkyl group” Is a group in which one or more hydrogen atoms of the “lower alkyl group” have —NR ^c R ^d in the definition of the “substituent group β ¹ ” (where one of R ^c and R ^d is hydrogen) And the other is a hydrogen atom, a lower alkyl group or an aralkyl group). Preferably, the alkyl moiety is a group having 1 to 4 carbon atoms, more preferably, aminomethyl, 2-aminoethyl, 3-aminopropyl, methylaminomethyl,
(Methylamino) ethyl, 3- (methylamino) propyl, ethylaminomethyl, 2- (ethylamino) ethyl, 3- (ethylamino) propyl, dimethylaminomethyl, 2- (dimethylamino) ethyl, 3- (dimethyl Amino) propyl, diethylaminomethyl, 2- (diethylamino) ethyl, 3- (diethylamino) propyl, benzylaminomethyl, 2- (benzylamino) ethyl, and 3- (benzylamino) propyl.

A group defined as "substituent group δ"
That is, a preferable group of groups is “substituent group δ ¹And this
Represents a lower alkyl group, a halogeno lower alkyl group,
Xy lower alkyl groups and nitro lower alkyl groups.
You.

The “halogeno lower alkyl group” in the definition of the “substituent group δ ¹ ” means ^one of the above “lower alkyl groups”
Or two or more hydrogen atoms are the aforementioned “halogen atoms”
Represents a group substituted with It is preferably a halogenoalkyl group having 1 to 4 carbon atoms, more preferably trifluoromethyl, trichloromethyl, difluoromethyl, dichloromethyl, dibromomethyl, fluoromethyl, 2,2,2
2-trichloroethyl, 2,2,2-trifluoroethyl, 2-bromoethyl, 2-chloroethyl, 2-fluoroethyl, 2,2-dibromoethyl, and more preferably, trifluoromethyl, trichloromethyl, Difluoromethyl, fluoromethyl, most preferably
Trifluoromethyl.

The “hydroxy lower alkyl group” in the definition of the “substituent group δ ¹ ” refers to a group in which one or more hydrogen atoms of the above “lower alkyl group” are substituted with the above “hydroxyl group”. . It is preferably a hydroxyalkyl group having 1 to 4 carbon atoms, more preferably hydroxymethyl, 2-hydroxyethyl, or 3-hydroxypropyl.

The “nitro lower alkyl group” in the definition of the “substituent group δ ¹ ” refers to a group in which one or more hydrogen atoms of the above “lower alkyl group” are substituted with a nitro group. It is preferably a nitroalkyl group having 1 to 4 carbon atoms, and more preferably nitromethyl, 2-nitroethyl, or 3-nitropropyl.

X may be a “single bond”, and R ⁴ may be substituted with a group selected from the substituent group α and the substituent group δ. A heterocyclyl group substituted with a selected group '' or a `` heterocyclyl group having at least one nitrogen atom, which may be substituted with a group selected from substituent group α and substituent group δ '', R ³ is preferably represented by the following general formula (I)
I):

[0063]

Embedded image [In the formula, m represents 0 or 1, n represents 1 or 2, R ⁵ , R ⁶ , R ⁷ , R ⁸ and R ⁹ are the same or different and are a hydrogen atom, a substituent group α , Substituent group β, substituent group γ
And one group selected from substituent group δ, and one of D and E is> NR ¹⁰ (R ¹⁰ is a hydrogen atom, substituent group γ
And one group selected from the substituent group δ. The other is> CR ¹¹ R ¹² (R ¹¹ and R ¹² are one group selected from a hydrogen atom, a substituent group α, a substituent group β, a substituent group γ and a substituent group δ And R)
⁶ may together with R ⁵ or R ⁷ represent a single bond; R ¹⁰ and R ¹¹ together form a lower alkylene group or a substituent group α, a substituent group β, a substituent It may form a lower alkylene group substituted by a group selected from group γ and substituent group δ. ] It is a group which has.

In the general formula (II), preferably,
One of R ⁵ and R ⁷ together with R ⁶ represents a single bond;
The other is a hydrogen atom, one group selected from a substituent group α, a substituent group γ and a substituent group δ (preferably a hydrogen atom, a lower alkyl group or an aralkyl group, more preferably,
A hydrogen atom, an alkyl group having 1 to 4 carbon atoms, benzyl or phenethyl).

R ⁸ , R ⁹ , R ¹⁰ , R ¹¹ and R ¹² are each independently selected from a hydrogen atom, a substituent group α, a substituent group β, a substituent group γ and a substituent group δ When the group is represented by one, it is preferably one group selected from a hydrogen atom, a substituent group γ and a substituent group δ. More preferably, it is a hydrogen atom, a lower alkyl group or an aralkyl group, even more preferably, a hydrogen atom, an alkyl group having 1 to 4 carbon atoms,
Benzyl or phenethyl.

R ¹⁰ and R ¹¹ are substituted with a “lower alkylene group” formed together and a group selected from “substituent group α, substituent group β, substituent group γ and substituent group δ”. The lower alkylene group "of methylene, ethylene, trimethylene, propylene, tetramethylene, 1-methyltrimethylene, 2-methyltrimethylene, 1,1-dimethylethylene, pentamethylene, 1,
And represents a linear or branched alkylene group having 1 to 6 carbon atoms, such as 1-dimethyltrimethylene, 2,2-dimethyltrimethylene, 1,2-dimethyltrimethylene, and hexamethylene. Preferably, it is a linear or branched alkylene group having 3 to 6 carbon atoms, more preferably, a linear or branched alkylene group having 3 to 4 carbon atoms, even more preferably, 3 From 4 to 4 straight-chain alkylene groups.

In the general formula (II), suitable groups
(A) a group in which m is 1 and n is 1;
R^FiveAnd R⁷One of R⁶Shows a single bond with
A group in which the other is a hydrogen atom, (c) R⁷, R⁸And R⁹
Are the same or different, a hydrogen atom, a substituent group α,
One group selected from the substituent group γ and the substituent group δ
Group, (d) R^Ten, R¹¹And R¹²Is a hydrogen atom, a substituent group
α, one group selected from substituent group γ and substituent group δ
(E) R^TenAnd R¹¹But together, carbon
A linear alkylene group of 3 or 4 or a substituent group α,
Groups selected from the substituent group β, the substituent group γ, and the substituent group δ
Forms a straight-chain alkylene group having 3 or 4 carbon atoms
And (f) R⁷, R⁸And R⁹But each
Is a hydrogen atom, R^TenAnd R¹¹But together,
A straight-chain alkylene group having 3 to 4 carbon atoms or a group of substituents
selected from α, substituent group β, substituent group γ and substituent group δ
C3 or C4 linear alkylene substituted with a group
The group forming the group can be mentioned, and it is even more preferable.
(F) m is 1; n is 1;
But> CR¹¹R¹²E is> NR ^TenGroup
And (g) m is 1; n is 1; D is> CR¹¹
R¹²E is> NR ^TenAnd R⁸, R⁹, R¹¹Passing
And R¹²And at least one group is a group of substituents α,
One group selected from the substituent group γ and the substituent group δ
Groups.

Further, in the definition of R ³ , a general formula: -X
In group with -R ^4, X is a "lower alkenylene group" or "substituted with a group selected from Substituent group α was lower alkenylene group", R ⁴ is, "Substituent group α and substituents May be substituted with a group selected from group δ,
A heterocyclyl group substituted with a group selected from the substituent group β and the substituent group γ ”or“ the substituent group α and the substituent group δ
A group that is a "heterocyclyl group having at least one nitrogen atom, which may be substituted with a group selected from" is also preferable, and examples of such a group include 2-pyrrolidinyl and 1-methyl-2-. Pyrrolidinyl, 1-ethyl-
2-pyrrolidinyl, 1-propyl-2-pyrrolidinyl,
2-piperidinyl, 1-methyl-2-piperidinyl, 1
And groups such as -ethyl-2-piperidinyl and 1-propyl-2-piperidinyl.

The “ester or other derivative thereof” refers to a functional group (for example, hydroxyl group,
A compound obtained by modifying an amino group, an imino group, a sulfonamide group, etc.) with a protecting group or the like according to a conventional method.

"Ester" refers to the compound (I) of the present invention.
Can be an ester, which means an ester. Examples of such an ester include an ester of a hydroxyl group, and each ester residue is a `` general protecting group '' or `` in vivo. Esters which are "protecting groups that can be cleaved by biological methods such as hydrolysis."

"General protecting group" refers to a protecting group that can be cleaved by a chemical method such as hydrogenolysis, hydrolysis, electrolysis, or photolysis.

As the “general protecting group” for the “ester of hydroxyl group”, preferably, formyl, acetyl, propionyl, butyryl, isobutyryl, pentanoyl, pivaloyl, valeryl, isovaleryl, octanoyl, nonanoyl, decanoyl, 3-decanoyl, Methylnonanoyl, 8-methylnonanoyl, 3-ethyloctanoyl, 3,7-dimethyloctanoyl, undecanoyl, dodecanoyl,
Tridecanoyl, tetradecanoyl, pentadecanoyl, hexadecanoyl, 1-methylpentadecanoyl,
Alkanoyl groups such as 14-methylpentadecanoyl, 13,13-dimethyltetradecanoyl, heptadecanoyl, 15-methylhexadecanoyl, octadecanoyl, 1-methylheptadecanoyl, nonadecanoyl, eicosanoyl, henicosanoyl, chloroacetyl,
Halogenated alkylcarbonyl groups such as dichloroacetyl, trichloroacetyl, trifluoroacetyl, lower alkoxyalkylcarbonyl groups such as methoxyacetyl, acryloyl, propioloyl, methacryloyl, crotonoyl, isocrotonoyl, (E) -2-methyl-2-butenoyl An “aliphatic acyl group” such as an unsaturated alkylcarbonyl group (preferably a lower aliphatic acyl group having 1 to 6 carbon atoms); benzoyl, α
Arylcarbonyl groups such as -naphthoyl and β-naphthoyl, halogenated arylcarbonyl groups such as 2-bromobenzoyl, 4-chlorobenzoyl and 2,4,6-trifluorobenzoyl, 2,4,6 A lower alkylated arylcarbonyl group such as trimethylbenzoyl and 4-toluoyl, a lower alkoxylated arylcarbonyl group such as 4-anisoyl, and a nitrated aryl such as 4-nitrobenzoyl and 2-nitrobenzoyl. Arylcarbonyl group such as carbonyl group, 2- (methoxycarbonyl) benzoyl or arylated aryl group such as 4-phenylbenzoyl.
“Aromatic acyl group” such as carbonyl group; methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl,
A lower alkoxycarbonyl group such as butoxycarbonyl, s-butoxycarbonyl, t-butoxycarbonyl and isobutoxycarbonyl; a halogen or tri-lower alkylsilyl group such as 2,2,2-trichloroethoxycarbonyl and 2-trimethylsilylethoxycarbonyl; An “alkoxycarbonyl group” such as a substituted lower alkoxycarbonyl group; tetrahydropyran-2-yl;
"Tetrahydropyranyl or tetrahydrothiopyranyl such as 3-bromotetrahydropyran-2-yl, 4-methoxytetrahydropyran-4-yl, tetrahydrothiopyran-2-yl, 4-methoxytetrahydrothiopyran-4-yl A "tetrahydrofuranyl or tetrahydrothiofuranyl group" such as tetrahydrofuran-2-yl, tetrahydrothiofuran-2-yl;
Tri-lower alkylsilyl groups such as trimethylsilyl, triethylsilyl, isopropyldimethylsilyl, t-butyldimethylsilyl, methyldiisopropylsilyl, methyldi-t-butylsilyl, triisopropylsilyl, diphenylmethylsilyl, diphenylbutylsilyl, diphenylisopropylsilyl, phenyl A "silyl group" such as a tri-lower alkylsilyl group substituted with one or two aryl groups such as diisopropylsilyl; methoxymethyl, 1,1-dimethyl-1-methoxymethyl,
Ethoxymethyl, propoxymethyl, isopropoxymethyl, butoxymethyl, lower alkoxymethyl groups such as t-butoxymethyl, lower alkoxylated lower alkoxymethyl groups such as 2-methoxyethoxymethyl, 2,
"Alkoxymethyl group" such as halogeno lower alkoxymethyl such as 2,2-trichloroethoxymethyl, bis (2-chloroethoxy) methyl; 1-ethoxyethyl;
“Substituted ethyl group” such as lower alkoxylated ethyl group such as 1- (isopropoxy) ethyl, ethyl halide group such as 2,2,2-trichloroethyl; benzyl, α
Lower alkyl group substituted with 1 to 3 aryl groups such as naphthylmethyl, β-naphthylmethyl, diphenylmethyl, triphenylmethyl, α-naphthyldiphenylmethyl, 9-anthrylmethyl, 4-methyl Benzyl, 2,4,6-trimethylbenzyl, 3,4,5-trimethylbenzyl, 4-methoxybenzyl, 4-methoxyphenyldiphenylmethyl, 2-nitrobenzyl,
1 to 3 aryls in which the aryl ring is substituted by lower alkyl, lower alkoxy, nitro, halogen, cyano groups such as -nitrobenzyl, 4-chlorobenzyl, 4-bromobenzyl, 4-cyanobenzyl An "aralkyl group" such as a lower alkyl group substituted with a group; an "alkenyloxycarbonyl group" such as vinyloxycarbonyl or allyloxycarbonyl; benzyloxycarbonyl,
The aryl ring is substituted with one or two lower alkoxy or nitro groups such as -methoxybenzyloxycarbonyl, 3,4-dimethoxybenzyloxycarbonyl, 2-nitrobenzyloxycarbonyl, 4-nitrobenzyloxycarbonyl; "Aralkyloxycarbonyl group" which may be mentioned.

The term "protecting group that can be cleaved in vivo by a biological method such as hydrolysis" means that it is cleaved in a human body by a biological method such as hydrolysis to produce a free acid or a salt thereof. It refers to a protecting group, and whether such a derivative is administered by intravenous injection to experimental animals such as rats and mice,
It can be determined by examining the body fluid of the subsequent animal and detecting the base compound or a pharmacologically acceptable salt thereof.

The “protecting group that can be cleaved in vivo by a biological method such as hydrolysis” as the “ester of a hydroxyl group” is preferably formyloxymethyl, acetoxymethyl, dimethylaminoacetoxymethyl, Propionyloxymethyl, butyryloxymethyl, pivaloyloxymethyl, valeryloxymethyl, isovaleryloxymethyl, hexanoyloxymethyl, 1-formyloxyethyl, 1-acetoxyethyl, 1-propionyloxyethyl, 1- Butyryloxyethyl, 1-
Pivaloyloxyethyl, 1-valeryloxyethyl,
1-isovaleryloxyethyl, 1-hexanoyloxyethyl, 1-formyloxypropyl, 1-acetoxypropyl, 1-propionyloxypropyl, 1-butyryloxypropyl, 1-pivaloyloxypropyl, 1-vale Ryloxypropyl, 1-isovaleryloxypropyl, 1-hexanoyloxypropyl, 1-
Acetoxybutyl, 1-propionyloxybutyl, 1
Such as -butyryloxybutyl, 1-pivaloyloxybutyl, 1-acetoxypentyl, 1-propionyloxypentyl, 1-butyryloxypentyl, 1-pivaloyloxypentyl, 1-pivaloyloxyhexyl 1-("lower aliphatic acyl" oxy) "lower alkyl group", cyclopentylcarbonyloxymethyl, cyclohexylcarbonyloxymethyl, 1-cyclopentylcarbonyloxyethyl, 1-cyclohexylcarbonyloxyethyl, 1-cyclopentylcarbonyloxypropyl, 1- Cyclohexylcarbonyloxypropyl, 1-cyclopentylcarbonyloxybutyl, 1
1- such as -cyclohexylcarbonyloxybutyl
1- (acyloxy) "lower alkyl group" such as ("cycloalkyl" carbonyloxy) "lower alkyl group", 1-("aromatic acyl" oxy) "lower alkyl group" such as benzoyloxymethyl; methoxycarbonyl Oxymethyl, ethoxycarbonyloxymethyl, propoxycarbonyloxymethyl, isopropoxycarbonyloxymethyl, butoxycarbonyloxymethyl, isobutoxycarbonyloxymethyl, pentyloxycarbonyloxymethyl, hexyloxycarbonyloxymethyl, cyclohexyloxycarbonyloxymethyl, cyclohexyloxy Carbonyloxy (cyclohexyl) methyl, 1- (methoxycarbonyloxy) ethyl, 1- (ethoxycarbonyloxy) ethyl, 1-
(Propoxycarbonyloxy) ethyl, 1- (isopropoxycarbonyloxy) ethyl, 1- (butoxycarbonyloxy) ethyl, 1- (isobutoxycarbonyloxy) ethyl, 1- (t-butoxycarbonyloxy) ethyl, 1- ( Pentyloxycarbonyloxy)
Ethyl, 1- (hexyloxycarbonyloxy) ethyl, 1- (cyclopentyloxycarbonyloxy) ethyl, 1- (cyclopentyloxycarbonyloxy)
Propyl, 1- (cyclohexyloxycarbonyloxy) propyl, 1- (cyclopentyloxycarbonyloxy) butyl, 1- (cyclohexyloxycarbonyloxy) butyl, 1- (cyclohexyloxycarbonyloxy) ethyl, 1- (ethoxycarbonyloxy) propyl , 1- (methoxycarbonyloxy) propyl, 1- (ethoxycarbonyloxy) propyl, 1
-(Propoxycarbonyloxy) propyl, 1- (isopropoxycarbonyloxy) propyl, 1- (butoxycarbonyloxy) propyl, 1- (isobutoxycarbonyloxy) propyl, 1- (pentyloxycarbonyloxy) propyl, 1- ( Hexyloxycarbonyloxy) propyl, 1- (methoxycarbonyloxy) butyl, 1- (ethoxycarbonyloxy) butyl, 1- (propoxycarbonyloxy) butyl, 1-
(Isopropoxycarbonyloxy) butyl, 1- (butoxycarbonyloxy) butyl, 1- (isobutoxycarbonyloxy) butyl, 1- (methoxycarbonyloxy) pentyl, 1- (ethoxycarbonyloxy)
(Lower alkoxycarbonyloxy) alkyl groups such as pentyl, 1- (methoxycarbonyloxy) hexyl, 1- (ethoxycarbonyloxy) hexyl;
(5-phenyl-2-oxo-1,3-dioxolene-
4-yl) methyl, [5- (4-methylphenyl) -2
-Oxo-1,3-dioxolen-4-yl] methyl,
[5- (4-methoxyphenyl) -2-oxo-1,3
-Dioxolen-4-yl] methyl, [5- (4-fluorophenyl) -2-oxo-1,3-dioxolene-
4-yl] methyl, [5- (4-chlorophenyl) -2
-Oxo-1,3-dioxolen-4-yl] methyl,
(2-oxo-1,3-dioxolen-4-yl) methyl, (5-methyl-2-oxo-1,3-dioxolen-4-yl) methyl, (5-ethyl-2-oxo-1,
3-dioxolen-4-yl) methyl, (5-propyl-2-oxo-1,3-dioxolen-4-yl) methyl, (5-isopropyl-2-oxo-1,3-dioxolen-4-yl) "Carbonyloxyalkyl groups" such as methyl, oxodioxorenylmethyl groups such as (5-butyl-2-oxo-1,3-dioxolen-4-yl) methyl; phthalidyl, dimethylphthalidyl, dimethoxyphthalic; “Phthalidyl group” such as jill: the above “lower aliphatic acyl group”: the above “aromatic acyl group”: “half ester salt residue of succinic acid”: “phosphate ester residue”: “ester of amino acid or the like” "Forming residue": carbamoyl group: carbamoyl group substituted with 1 to 2 lower alkyl groups: and 1-carboxy group such as pivaloyloxymethyloxycarbonyl It can be exemplified acyloxy) alkyloxycarbonyl group ", preferably a" carbonyloxy alkyl group ".

"Other derivatives" means, when the compound (I) of the present invention has an amino group, an imino group and / or a sulfonamide group, other than the above-mentioned "ester" and the following "pharmacologically acceptable salts". Derivatives are shown because they can be derivatives. Such derivatives include, for example,
The amino group, imino group and / or sulfonamide group of the compound (I) may have the above-mentioned "aliphatic acyl group"
Alternatively, an amide derivative to which the above-mentioned “aromatic acyl group” is bonded may be mentioned.

"Pharmacologically acceptable salts thereof" means that the compound (I) of the present invention is reacted with an acid when it has a basic group such as an amino group, When the compound has an acidic group as described above, it can be converted into a salt by reacting it with a base.

The salt based on a basic group is preferably
Inorganic acid salts such as hydrohalides such as hydrochloride, hydrobromide and hydroiodide, nitrates, perchlorates, sulfates and phosphates; methanesulfonate, trifluoromethanesulfonate Salt, lower alkane sulfonate such as ethane sulfonate, benzene sulfonate, aryl sulfonate such as p-toluene sulfonate, acetate, malate, fumarate, succinic acid Organic salts such as salts, citrates, ascorbates, tartrates, oxalates, and maleates; and amino acid salts such as glycine, lysine, arginine, ornithine, glutamate, and aspartate. Can be mentioned.

On the other hand, the salt based on an acidic group is preferably an alkali metal salt such as a sodium salt, a potassium salt or a lithium salt; an alkaline earth metal salt such as a calcium salt or a magnesium salt; an aluminum salt; Metal salts such as salts; inorganic salts such as ammonium salts, t-octylamine salts, dibenzylamine salts, morpholine salts, glucosamine salts, phenylglycine alkyl ester salts, ethylenediamine salts, N-methylglucamine salts, guanidine salts,
Diethylamine salt, triethylamine salt, dicyclohexylamine salt, N, N'-dibenzylethylenediamine salt, chloroprocaine salt, procaine salt, diethanolamine salt, N-benzylphenethylamine salt, piperazine salt, tetramethylammonium salt, tris (hydroxymethyl) amino Amine salts such as organic salts such as methane salts; and amino acid salts such as glycine salts, lysine salts, arginine salts, ornithine salts, glutamates, and aspartates.

The compound having the general formula (I) of the present invention is
By leaving in the air or recrystallizing,
In some cases, water may be absorbed, adsorbed water may be formed, or a hydrate may be formed. Such a hydrate is also included in the present invention.

The compound having the general formula (I) of the present invention may include a geometric isomer (cis, trans isomer) and an optical isomer based on an asymmetric center in the molecule. In the compounds of the present invention, these isomers and mixtures of these isomers are all represented by a single formula, that is, the general formula (I). Accordingly, the present invention includes all these isomers and mixtures of these isomers.

Specific examples of the compound having the general formula (I) of the present invention include the compounds shown in Tables 1 and 2 below.

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[Table 1] Table 1 --------------------------------- Compound number R ¹ R ^Two R ^Three −−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−− 1-1 Ph 4-Pyr H _Two N-CH _Two 1-2 Ph 4-Pyr H _Two N- (CH _Two ) _Two 1-3 Ph 4-Pyr H _Two N- (CH _Two ) _Three 1-4 Ph 4-Pyr H _Two N- (CH _Two ) _Four 1-5 Ph 4-Pyr MeNH-CH _Two 1-6 Ph 4-Pyr MeNH- (CH _Two ) _Two 1-7 Ph 4-Pyr MeNH- (CH _Two ) _Three 1-8 Ph 4-Pyr MeNH- (CH _Two ) _Four 1-9 Ph 4-Pyr EtNH-CH _Two 1-10 Ph 4-Pyr EtNH- (CH _Two ) _Two 1-11 Ph 4-Pyr EtNH- (CH _Two ) _Three 1-12 Ph 4-Pyr EtNH- (CH _Two ) _Four 1-13 Ph 4-Pyr Me _Two N-CH _Two 1-14 Ph 4-Pyr Me _Two N- (CH _Two ) _Two 1-15 Ph 4-Pyr Me _Two N- (CH _Two ) _Three 1-16 Ph 4-Pyr Me _Two N- (CH _Two ) _Four 1-17 Ph 4-Pyr 1-Azt-CH _Two 1-18 Ph 4-Pyr 1-Azt- (CH _Two ) _Two 1-19 Ph 4-Pyr 1-Azt- (CH _Two ) _Three 1-20 Ph 4-Pyr 1-Azt- (CH _Two ) _Four 1-21 Ph 4-Pyr 1-Pyrd-CH _Two 1-22 Ph 4-Pyr 1-Pyrd- (CH _Two ) _Two 1-23 Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 1-24 Ph 4-Pyr 1-Pyrd- (CH _Two ) _Four 1-25 Ph 4-Pyr 1-Pip-CH _Two 1-26 Ph 4-Pyr 1-Pip- (CH _Two ) _Two 1-27 Ph 4-Pyr 1-Pip- (CH _Two ) _Three 1-28 Ph 4-Pyr 1-Pip- (CH _Two ) _Four 1-29 Ph 4-Pyr 1-Mor-CH _Two 1-30 Ph 4-Pyr 1-Mor- (CH _Two ) _Two 1-31 Ph 4-Pyr 1-Mor- (CH _Two ) _Three 1-32 Ph 4-Pyr 1-Mor- (CH _Two ) _Four 1-33 Ph 4-Pyr 1-Tmor-CH _Two 1-34 Ph 4-Pyr 1-Tmor- (CH _Two ) _Two 1-35 Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 1-36 Ph 4-Pyr 1-Tmor- (CH _Two ) _Four 1-37 Ph 4-Pyr 1-Piz-CH _Two 1-38 Ph 4-Pyr 1-Piz- (CH _Two ) _Two 1-39 Ph 4-Pyr 1-Piz- (CH _Two ) _Three 1-40 Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-41 Ph 4-Pyr 1-Piz- (CH _Two ) _Four 1-42 Ph 4-Pyr 3-Azt 1-43 Ph 4-Pyr 1-Me-3-Azt 1-44 Ph 4-Pyr 1-Bn-3-Azt 1-45 Ph 4-Pyr 3-Pyrd 1- 46 Ph 4-Pyr 1-Me-3-Pyrd 1-47 Ph 4-Pyr 3-Pip 1-48 Ph 4-Pyr 4-Pip 1-49 Ph 4-Pyr 4- (3,4-deH-Pip) 1-50 Ph 4-Pyr 1-Me-4-Pip 1-51 Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 1-52 Ph 4-Pyr 1-Et-4-Pip 1-53 Ph 4-Pyr 1-Bn-4-Pip 1-54 Ph 4-Pyr 3-Hpip 1-55 Ph 4-Pyr 1-Me-3-Hpip 1-56 Ph 4-Pyr 4-Hpip 1- 57 Ph 4-Pyr 1-Me-4-Hpip 1-58 Ph 4-Pyr 2-Mor 1-59 Ph 4-Pyr 1-Me-2-Mor 1-60 Ph 4-Pyr 2-Tmor 1-61 Ph 4-Pyr 1-Me-2-Tmor 1-62 Ph 4-Pyr 1-Piz 1-63 Ph 4-Pyr 4-Me-1-Piz 1-64 Ph 4-Pyr 2-Piz 1-65 Ph 4- Pyr 4-Pyr 1-66 Ph 4-Pyr 3-Pyr 1-67 Ph 4-Pyr 2-Pyr 1-68 Ph 4-Pyr 4-Pym 1-69 Ph 4-Pyr 5-Pym 1-70 Ph 4- Pyr 2-Pym 1-71 Ph 4-Pyr 3-Azt-CH _Two 1-72 Ph 4-Pyr 1-Me-3-Azt-CH _Two 1-73 Ph 4-Pyr 3-Pyrd-CH _Two 1-74 Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 1-75 Ph 4-Pyr 4-Pip-CH _Two 1-76 Ph 4-Pyr 1-Me-4-Pip-CH _Two 1-77 Ph 4-Pyr 3-Hpip-CH _Two 1-78 Ph 4-Pyr 1-Me-3-Hpip-CH _Two 1-79 Ph 4-Pyr 4-Hpip-CH _Two 1-80 Ph 4-Pyr 1-Me-4-Hpip-CH _Two 1-81 Ph 4-Pyr 2-Mor-CH _Two 1-82 Ph 4-Pyr 1-Me-2-Mor-CH _Two 1-83 Ph 4-Pyr 2-Tmor-CH _Two 1-84 Ph 4-Pyr 1-Me-2-Tmor-CH _Two 1-85 Ph 4-Pyr 1-Piz-CH _Two 1-86 Ph 4-Pyr 4-Me-1-Piz-CH _Two 1-87 Ph 4-Pyr 2-Piz-CH _Two 1-88 Ph 4-Pyr 4-Pyr-CH _Two 1-89 Ph 4-Pyr 3-Pyr-CH _Two 1-90 Ph 4-Pyr 2-Pyr-CH _Two 1-91 Ph 4-Pyr 4-Pym-CH _Two 1-92 Ph 4-Pyr 5-Pym-CH _Two 1-93 Ph 4-Pyr 2-Pym-CH _Two 1-94 Ph 4-Pyr H _Two N-CH _Two CH = CH 1-95 4-F-Ph 4-Pyr H _Two N-CH _Two 1-96 4-F-Ph 4-Pyr H _Two N- (CH _Two ) _Two 1-97 4-F-Ph 4-Pyr H _Two N- (CH _Two ) _Three 1-98 4-F-Ph 4-Pyr H _Two N- (CH _Two ) _Four 1-99 4-F-Ph 4-Pyr MeNH-CH _Two 1-100 4-F-Ph 4-Pyr MeNH- (CH _Two ) _Two 1-101 4-F-Ph 4-Pyr MeNH- (CH _Two ) _Three 1-102 4-F-Ph 4-Pyr MeNH- (CH _Two ) _Four 1-103 4-F-Ph 4-Pyr EtNH-CH _Two 1-104 4-F-Ph 4-Pyr EtNH- (CH _Two ) _Two 1-105 4-F-Ph 4-Pyr EtNH- (CH _Two ) _Three 1-106 4-F-Ph 4-Pyr EtNH- (CH _Two ) _Four 1-107 4-F-Ph 4-Pyr Me _Two N-CH _Two 1-108 4-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Two 1-109 4-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 1-110 4-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Four 1-111 4-F-Ph 4-Pyr 1-Azt-CH _Two 1-112 4-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Two 1-113 4-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 1-114 4-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Four 1-115 4-F-Ph 4-Pyr 1-Pyrd-CH _Two 1-116 4-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Two 1-117 4-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 1-118 4-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Four 1-119 4-F-Ph 4-Pyr 1-Pip-CH _Two 1-120 4-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Two 1-121 4-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 1-122 4-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Four 1-123 4-F-Ph 4-Pyr 1-Mor-CH _Two 1-124 4-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Two 1-125 4-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 1-126 4-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Four 1-127 4-F-Ph 4-Pyr 1-Tmor-CH _Two 1-128 4-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Two 1-129 4-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 1-130 4-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Four 1-131 4-F-Ph 4-Pyr 1-Piz-CH _Two 1-132 4-F-Ph 4-Pyr 1-Piz- (CH _Two ) _Two 1-133 4-F-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 1-134 4-F-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-135 4-F-Ph 4-Pyr 4-Bn-1-Piz- (CH _Two ) _Three 1-136 4-F-Ph 4-Pyr 3-Azt 1-137 4-F-Ph 4-Pyr 1-Me-3-Azt 1-138 4-F-Ph 4-Pyr 1-Bn-3-Azt 1-139 4-F-Ph 4-Pyr 3-Pyrd 1-140 4-F-Ph 4-Pyr 1-Me-3-Pyrd 1-141 4-F-Ph 4-Pyr 3-Pip 1-142 4 -F-Ph 4-Pyr 4-Pip 1-143 4-F-Ph 4-Pyr 4- (3,4-deH-Pip) 1-144 4-F-Ph 4-Pyr 1-Me-4-Pip 1-145 4-F-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 1-146 4-F-Ph 4-Pyr 1-Et-4-Pip 1-147 4-F -Ph 4-Pyr 1-Bn-4-Pip 1-148 4-F-Ph 4-Pyr 3-Hpip 1-149 4-F-Ph 4-Pyr 1-Me-3-Hpip 1-150 4-F -Ph 4-Pyr 4-Hpip 1-151 4-F-Ph 4-Pyr 1-Me-4-Hpip 1-152 4-F-Ph 4-Pyr 2-Mor 1-153 4-F-Ph 4- Pyr 1-Me-2-Mor 1-154 4-F-Ph 4-Pyr 2-Tmor 1-155 4-F-Ph 4-Pyr 1-Me-2-Tmor 1-156 4-F-Ph 4- Pyr 1-Piz 1-157 4-F-Ph 4-Pyr 4-Me-1-Piz 1-158 4-F-Ph 4-Pyr 2-Piz 1-159 4-F-Ph 4-Pyr 4-Pyr 1-160 4-F-Ph 4-Pyr 3-Pyr 1-161 4-F-Ph 4-Pyr 2-Pyr 1-162 4-F-Ph 4-Pyr 4-Pym 1-163 4-F-Ph 4-Pyr 5-Pym 1-164 4-F-Ph 4-Pyr 2-Pym 1-165 4-F-Ph 4-Pyr 3-Azt-CH _Two 1-166 4-F-Ph 4-Pyr 1-Me-3-Azt-CH _Two 1-167 4-F-Ph 4-Pyr 3-Pyrd-CH _Two 1-168 4-F-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 1-169 4-F-Ph 4-Pyr 4-Pip-CH _Two 1-170 4-F-Ph 4-Pyr 1-Me-4-Pip-CH _Two 1-171 4-F-Ph 4-Pyr 3-Hpip-CH _Two 1-172 4-F-Ph 4-Pyr 1-Me-3-Hpip-CH _Two 1-173 4-F-Ph 4-Pyr 4-Hpip-CH _Two 1-174 4-F-Ph 4-Pyr 1-Me-4-Hpip-CH _Two 1-175 4-F-Ph 4-Pyr 2-Mor-CH _Two 1-176 4-F-Ph 4-Pyr 1-Me-2-Mor-CH _Two 1-177 4-F-Ph 4-Pyr 2-Tmor-CH _Two 1-178 4-F-Ph 4-Pyr 1-Me-2-Tmor-CH _Two 1-179 4-F-Ph 4-Pyr 1-Piz-CH _Two 1-180 4-F-Ph 4-Pyr 4-Me-1-Piz-CH _Two 1-181 4-F-Ph 4-Pyr 2-Piz-CH _Two 1-182 4-F-Ph 4-Pyr 4-Pyr-CH _Two 1-183 4-F-Ph 4-Pyr 3-Pyr-CH _Two 1-184 4-F-Ph 4-Pyr 2-Pyr-CH _Two 1-185 4-F-Ph 4-Pyr 4-Pym-CH _Two 1-186 4-F-Ph 4-Pyr 5-Pym-CH _Two 1-187 4-F-Ph 4-Pyr 2-Pym-CH _Two 1-188 3-F-Ph 4-Pyr H _Two N-CH _Two 1-189 3-F-Ph 4-Pyr H _Two N- (CH _Two ) _Two 1-190 3-F-Ph 4-Pyr H _Two N- (CH _Two ) _Three 1-191 3-F-Ph 4-Pyr H _Two N- (CH _Two ) _Four 1-192 3-F-Ph 4-Pyr MeNH-CH _Two 1-193 3-F-Ph 4-Pyr MeNH- (CH _Two ) _Two 1-194 3-F-Ph 4-Pyr MeNH- (CH _Two ) _Three 1-195 3-F-Ph 4-Pyr MeNH- (CH _Two ) _Four 1-196 3-F-Ph 4-Pyr EtNH-CH _Two 1-197 3-F-Ph 4-Pyr EtNH- (CH _Two ) _Two 1-198 3-F-Ph 4-Pyr EtNH- (CH _Two ) _Three 1-199 3-F-Ph 4-Pyr EtNH- (CH _Two ) _Four 1-200 3-F-Ph 4-Pyr Me _Two N-CH _Two 1-201 3-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Two 1-202 3-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 1-203 3-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Four 1-204 3-F-Ph 4-Pyr 1-Azt-CH _Two 1-205 3-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Two 1-206 3-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 1-207 3-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Four 1-208 3-F-Ph 4-Pyr 1-Pyrd-CH _Two 1-209 3-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Two 1-210 3-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 1-211 3-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Four 1-212 3-F-Ph 4-Pyr 1-Pip-CH _Two 1-213 3-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Two 1-214 3-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 1-215 3-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Four 1-216 3-F-Ph 4-Pyr 1-Mor-CH _Two 1-217 3-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Two 1-218 3-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 1-219 3-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Four 1-220 3-F-Ph 4-Pyr 1-Tmor-CH _Two 1-221 3-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Two 1-222 3-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 1-223 3-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Four 1-224 3-F-Ph 4-Pyr 1-Piz-CH _Two 1-225 3-F-Ph 4-Pyr 1-Piz- (CH _Two ) _Two 1-226 3-F-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 1-227 3-F-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-228 3-F-Ph 4-Pyr 1-Piz- (CH _Two ) _Four 1-229 3-F-Ph 4-Pyr 3-Azt 1-230 3-F-Ph 4-Pyr 1-Me-3-Azt 1-231 3-F-Ph 4-Pyr 1-Bn-3-Azt 1-232 3-F-Ph 4-Pyr 3-Pyrd 1-233 3-F-Ph 4-Pyr 1-Me-3-Pyrd 1-234 3-F-Ph 4-Pyr 3-Pip 1-235 3 -F-Ph 4-Pyr 4-Pip 1-236 3-F-Ph 4-Pyr 4- (3,4-deH-Pip) 1-237 3-F-Ph 4-Pyr 1-Me-4-Pip 1-238 3-F-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 1-239 3-F-Ph 4-Pyr 1-Et-4-Pip 1-240 3-F -Ph 4-Pyr 1-Bn-4-Pip 1-241 3-F-Ph 4-Pyr 3-Hpip 1-242 3-F-Ph 4-Pyr 1-Me-3-Hpip 1-243 3-F -Ph 4-Pyr 4-Hpip 1-244 3-F-Ph 4-Pyr 1-Me-4-Hpip 1-245 3-F-Ph 4-Pyr 2-Mor 1-246 3-F-Ph 4- Pyr 1-Me-2-Mor 1-247 3-F-Ph 4-Pyr 2-Tmor 1-248 3-F-Ph 4-Pyr 1-Me-2-Tmor 1-249 3-F-Ph 4- Pyr 1-Piz 1-250 3-F-Ph 4-Pyr 4-Me-1-Piz 1-251 3-F-Ph 4-Pyr 2-Piz 1-252 3-F-Ph 4-Pyr 4-Pyr 1-253 3-F-Ph 4-Pyr 3-Pyr 1-254 3-F-Ph 4-Pyr 2-Pyr 1-255 3-F-Ph 4-Pyr 4-Pym 1-256 3-F-Ph 4-Pyr 5-Pym 1-257 3-F-Ph 4-Pyr 2-Pym 1-258 3-F-Ph 4-Pyr 3-Azt-CH _Two 1-259 3-F-Ph 4-Pyr 1-Me-3-Azt-CH _Two 1-260 3-F-Ph 4-Pyr 3-Pyrd-CH _Two 1-261 3-F-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 1-262 3-F-Ph 4-Pyr 4-Pip-CH _Two 1-263 3-F-Ph 4-Pyr 1-Me-4-Pip-CH _Two 1-264 3-F-Ph 4-Pyr 3-Hpip-CH _Two 1-265 3-F-Ph 4-Pyr 1-Me-3-Hpip-CH _Two 1-266 3-F-Ph 4-Pyr 4-Hpip-CH _Two 1-267 3-F-Ph 4-Pyr 1-Me-4-Hpip-CH _Two 1-268 3-F-Ph 4-Pyr 2-Mor-CH _Two 1-269 3-F-Ph 4-Pyr 1-Me-2-Mor-CH _Two 1-270 3-F-Ph 4-Pyr 2-Tmor-CH _Two 1-271 3-F-Ph 4-Pyr 1-Me-2-Tmor-CH _Two 1-272 3-F-Ph 4-Pyr 1-Piz-CH _Two 1-273 3-F-Ph 4-Pyr 4-Me-1-Piz-CH _Two 1-274 3-F-Ph 4-Pyr 2-Piz-CH _Two 1-275 3-F-Ph 4-Pyr 4-Pyr-CH _Two 1-276 3-F-Ph 4-Pyr 3-Pyr-CH _Two 1-277 3-F-Ph 4-Pyr 2-Pyr-CH _Two 1-278 3-F-Ph 4-Pyr 4-Pym-CH _Two 1-279 3-F-Ph 4-Pyr 5-Pym-CH _Two 1-280 3-F-Ph 4-Pyr 2-Pym-CH _Two 1-281 3,4-diF-Ph 4-Pyr H _Two N-CH _Two 1-282 3,4-diF-Ph 4-Pyr H _Two N- (CH _Two ) _Two 1-283 3,4-diF-Ph 4-Pyr H _Two N- (CH _Two ) _Three 1-284 3,4-diF-Ph 4-Pyr H _Two N- (CH _Two ) _Four 1-285 3,4-diF-Ph 4-Pyr MeNH-CH _Two 1-286 3,4-diF-Ph 4-Pyr MeNH- (CH _Two ) _Two 1-287 3,4-diF-Ph 4-Pyr MeNH- (CH _Two ) _Three 1-288 3,4-diF-Ph 4-Pyr MeNH- (CH _Two ) _Four 1-289 3,4-diF-Ph 4-Pyr EtNH-CH _Two 1-290 3,4-diF-Ph 4-Pyr EtNH- (CH _Two ) _Two 1-291 3,4-diF-Ph 4-Pyr EtNH- (CH _Two ) _Three 1-292 3,4-diF-Ph 4-Pyr EtNH- (CH _Two ) _Four 1-293 3,4-diF-Ph 4-Pyr Me _Two N-CH _Two 1-294 3,4-diF-Ph 4-Pyr Me _Two N- (CH _Two ) _Two 1-295 3,4-diF-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 1-296 3,4-diF-Ph 4-Pyr Me _Two N- (CH _Two ) _Four 1-297 3,4-diF-Ph 4-Pyr 1-Azt-CH _Two 1-298 3,4-diF-Ph 4-Pyr 1-Azt- (CH _Two ) _Two 1-299 3,4-diF-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 1-300 3,4-diF-Ph 4-Pyr 1-Azt- (CH _Two ) _Four 1-301 3,4-diF-Ph 4-Pyr 1-Pyrd-CH _Two 1-302 3,4-diF-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Two 1-303 3,4-diF-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 1-304 3,4-diF-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Four 1-305 3,4-diF-Ph 4-Pyr 1-Pip-CH _Two 1-306 3,4-diF-Ph 4-Pyr 1-Pip- (CH _Two ) _Two 1-307 3,4-diF-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 1-308 3,4-diF-Ph 4-Pyr 1-Pip- (CH _Two ) _Four 1-309 3,4-diF-Ph 4-Pyr 1-Mor-CH _Two 1-310 3,4-diF-Ph 4-Pyr 1-Mor- (CH _Two ) _Two 1-311 3,4-diF-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 1-312 3,4-diF-Ph 4-Pyr 1-Mor- (CH _Two ) _Four 1-313 3,4-diF-Ph 4-Pyr 1-Tmor-CH _Two 1-314 3,4-diF-Ph 4-Pyr 1-Tmor- (CH _Two ) _Two 1-315 3,4-diF-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 1-316 3,4-diF-Ph 4-Pyr 1-Tmor- (CH _Two ) _Four 1-317 3,4-diF-Ph 4-Pyr 1-Piz-CH _Two 1-318 3,4-diF-Ph 4-Pyr 1-Piz- (CH _Two ) _Two 1-319 3,4-diF-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 1-320 3,4-diF-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-321 3,4-diF-Ph 4-Pyr 1-Piz- (CH _Two ) _Four 1-322 3,4-diF-Ph 4-Pyr 3-Azt 1-323 3,4-diF-Ph 4-Pyr 1-Me-3-Azt 1-324 3,4-diF-Ph 4-Pyr 1 -Bn-3-Azt 1-325 3,4-diF-Ph 4-Pyr 3-Pyrd 1-326 3,4-diF-Ph 4-Pyr 1-Me-3-Pyrd 1-327 3,4-diF -Ph 4-Pyr 3-Pip 1-328 3,4-diF-Ph 4-Pyr 4-Pip 1-329 3,4-diF-Ph 4-Pyr 4- (3,4-deH-Pip) 1- 330 3,4-diF-Ph 4-Pyr 1-Me-4-Pip 1-331 3,4-diF-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 1-332 3 , 4-diF-Ph 4-Pyr 1-Et-4-Pip 1-333 3,4-diF-Ph 4-Pyr 1-Bn-4-Pip 1-334 3,4-diF-Ph 4-Pyr 3 -Hpip 1-335 3,4-diF-Ph 4-Pyr 1-Me-3-Hpip 1-336 3,4-diF-Ph 4-Pyr 4-Hpip 1-337 3,4-diF-Ph 4- Pyr 1-Me-4-Hpip 1-338 3,4-diF-Ph 4-Pyr 2-Mor 1-339 3,4-diF-Ph 4-Pyr 1-Me-2-Mor 1-340 3,4 -diF-Ph 4-Pyr 2-Tmor 1-341 3,4-diF-Ph 4-Pyr 1-Me-2-Tmor 1-342 3,4-diF-Ph 4-Pyr 1-Piz 1-343 3 , 4-diF-Ph 4-Pyr 4-Me-1-Piz 1-344 3,4-diF-Ph 4-Pyr 2-Piz 1-345 3,4-diF-Ph 4-Pyr 4-Pyr 1- 346 3,4-diF-Ph 4-Pyr 3-Pyr 1-347 3,4-diF-Ph 4-Pyr 2-Pyr 1-348 3,4-diF-Ph 4-Pyr 4-Pym 1-349 3 , 4-diF-Ph 4-Pyr 5-Pym 1-350 3,4-diF-Ph 4-Pyr 2-Pym 1-351 3,4-diF-Ph 4-Pyr 3-Azt-CH _Two 1-352 3,4-diF-Ph 4-Pyr 1-Me-3-Azt-CH _Two 1-353 3,4-diF-Ph 4-Pyr 3-Pyrd-CH _Two 1-354 3,4-diF-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 1-355 3,4-diF-Ph 4-Pyr 4-Pip-CH _Two 1-356 3,4-diF-Ph 4-Pyr 1-Me-4-Pip-CH _Two 1-357 3,4-diF-Ph 4-Pyr 3-Hpip-CH _Two 1-358 3,4-diF-Ph 4-Pyr 1-Me-3-Hpip-CH _Two 1-359 3,4-diF-Ph 4-Pyr 4-Hpip-CH _Two 1-360 3,4-diF-Ph 4-Pyr 1-Me-4-Hpip-CH _Two 1-361 3,4-diF-Ph 4-Pyr 2-Mor-CH _Two 1-362 3,4-diF-Ph 4-Pyr 1-Me-2-Mor-CH _Two 1-363 3,4-diF-Ph 4-Pyr 2-Tmor-CH _Two 1-364 3,4-diF-Ph 4-Pyr 1-Me-2-Tmor-CH _Two 1-365 3,4-diF-Ph 4-Pyr 1-Piz-CH _Two 1-366 3,4-diF-Ph 4-Pyr 4-Me-1-Piz-CH _Two 1-367 3,4-diF-Ph 4-Pyr 2-Piz-CH _Two 1-368 3,4-diF-Ph 4-Pyr 4-Pyr-CH _Two 1-369 3,4-diF-Ph 4-Pyr 3-Pyr-CH _Two 1-370 3,4-diF-Ph 4-Pyr 2-Pyr-CH _Two 1-371 3,4-diF-Ph 4-Pyr 4-Pym-CH _Two 1-372 3,4-diF-Ph 4-Pyr 5-Pym-CH _Two 1-373 3,4-diF-Ph 4-Pyr 2-Pym-CH _Two 1-374 3-Cl-Ph 4-Pyr H _Two N-CH _Two 1-375 3-Cl-Ph 4-Pyr H _Two N- (CH _Two ) _Two 1-376 3-Cl-Ph 4-Pyr H _Two N- (CH _Two ) _Three 1-377 3-Cl-Ph 4-Pyr H _Two N- (CH _Two ) _Four 1-378 3-Cl-Ph 4-Pyr MeNH-CH _Two 1-379 3-Cl-Ph 4-Pyr MeNH- (CH _Two ) _Two 1-380 3-Cl-Ph 4-Pyr MeNH- (CH _Two ) _Three 1-381 3-Cl-Ph 4-Pyr MeNH- (CH _Two ) _Four 1-382 3-Cl-Ph 4-Pyr EtNH-CH _Two 1-383 3-Cl-Ph 4-Pyr EtNH- (CH _Two ) _Two 1-384 3-Cl-Ph 4-Pyr EtNH- (CH _Two ) _Three 1-385 3-Cl-Ph 4-Pyr EtNH- (CH _Two ) _Four 1-386 3-Cl-Ph 4-Pyr Me _Two N-CH _Two 1-387 3-Cl-Ph 4-Pyr Me _Two N- (CH _Two ) _Two 1-388 3-Cl-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 1-389 3-Cl-Ph 4-Pyr Me _Two N- (CH _Two ) _Four 1-390 3-Cl-Ph 4-Pyr 1-Azt-CH _Two 1-391 3-Cl-Ph 4-Pyr 1-Azt- (CH _Two ) _Two 1-392 3-Cl-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 1-393 3-Cl-Ph 4-Pyr 1-Azt- (CH _Two ) _Four 1-394 3-Cl-Ph 4-Pyr 1-Pyrd-CH _Two 1-395 3-Cl-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Two 1-396 3-Cl-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 1-397 3-Cl-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Four 1-398 3-Cl-Ph 4-Pyr 1-Pip-CH _Two 1-399 3-Cl-Ph 4-Pyr 1-Pip- (CH _Two ) _Two 1-400 3-Cl-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 1-401 3-Cl-Ph 4-Pyr 1-Pip- (CH _Two ) _Four 1-402 3-Cl-Ph 4-Pyr 1-Mor-CH _Two 1-403 3-Cl-Ph 4-Pyr 1-Mor- (CH _Two ) _Two 1-404 3-Cl-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 1-405 3-Cl-Ph 4-Pyr 1-Mor- (CH _Two ) _Four 1-406 3-Cl-Ph 4-Pyr 1-Tmor-CH _Two 1-407 3-Cl-Ph 4-Pyr 1-Tmor- (CH _Two ) _Two 1-408 3-Cl-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 1-409 3-Cl-Ph 4-Pyr 1-Tmor- (CH _Two ) _Four 1-410 3-Cl-Ph 4-Pyr 1-Piz-CH _Two 1-411 3-Cl-Ph 4-Pyr 1-Piz- (CH _Two ) _Two 1-412 3-Cl-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 1-413 3-Cl-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-414 3-Cl-Ph 4-Pyr 1-Piz- (CH _Two ) _Four 1-415 3-Cl-Ph 4-Pyr 3-Azt 1-416 3-Cl-Ph 4-Pyr 1-Me-3-Azt 1-417 3-Cl-Ph 4-Pyr 1-Bn-3-Azt 1-418 3-Cl-Ph 4-Pyr 3-Pyrd 1-419 3-Cl-Ph 4-Pyr 1-Me-3-Pyrd 1-420 3-Cl-Ph 4-Pyr 3-Pip 1-421 3 -Cl-Ph 4-Pyr 4-Pip 1-422 3-Cl-Ph 4-Pyr 4- (3,4-deH-Pip) 1-423 3-Cl-Ph 4-Pyr 1-Me-4-Pip 1-424 3-Cl-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 1-425 3-Cl-Ph 4-Pyr 1-Et-4-Pip 1-426 3-Cl -Ph 4-Pyr 1-Bn-4-Pip 1-427 3-Cl-Ph 4-Pyr 3-Hpip 1-428 3-Cl-Ph 4-Pyr 1-Me-3-Hpip 1-429 3-Cl -Ph 4-Pyr 4-Hpip 1-430 3-Cl-Ph 4-Pyr 1-Me-4-Hpip 1-431 3-Cl-Ph 4-Pyr 2-Mor 1-432 3-Cl-Ph 4- Pyr 1-Me-2-Mor 1-433 3-Cl-Ph 4-Pyr 2-Tmor 1-434 3-Cl-Ph 4-Pyr 1-Me-2-Tmor 1-435 3-Cl-Ph 4- Pyr 1-Piz 1-436 3-Cl-Ph 4-Pyr 4-Me-1-Piz 1-437 3-Cl-Ph 4-Pyr 2-Piz 1-438 3-Cl-Ph 4-Pyr 4-Pyr 1-439 3-Cl-Ph 4-Pyr 3-Pyr 1-440 3-Cl-Ph 4-Pyr 2-Pyr 1-441 3-Cl-Ph 4-Pyr 4-Pym 1-442 3-Cl-Ph 4-Pyr 5-Pym 1-443 3-Cl-Ph 4-Pyr 2-Pym 1-444 3-Cl-Ph 4-Pyr 3-Azt-CH _Two 1-445 3-Cl-Ph 4-Pyr 1-Me-3-Azt-CH _Two 1-446 3-Cl-Ph 4-Pyr 3-Pyrd-CH _Two 1-447 3-Cl-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 1-448 3-Cl-Ph 4-Pyr 4-Pip-CH _Two 1-449 3-Cl-Ph 4-Pyr 1-Me-4-Pip-CH _Two 1-450 3-Cl-Ph 4-Pyr 3-Hpip-CH _Two 1-451 3-Cl-Ph 4-Pyr 1-Me-3-Hpip-CH _Two 1-452 3-Cl-Ph 4-Pyr 4-Hpip-CH _Two 1-453 3-Cl-Ph 4-Pyr 1-Me-4-Hpip-CH _Two 1-454 3-Cl-Ph 4-Pyr 2-Mor-CH _Two 1-455 3-Cl-Ph 4-Pyr 1-Me-2-Mor-CH _Two 1-456 3-Cl-Ph 4-Pyr 2-Tmor-CH _Two 1-457 3-Cl-Ph 4-Pyr 1-Me-2-Tmor-CH _Two 1-458 3-Cl-Ph 4-Pyr 1-Piz-CH _Two 1-459 3-Cl-Ph 4-Pyr 4-Me-1-Piz-CH _Two 1-460 3-Cl-Ph 4-Pyr 2-Piz-CH _Two 1-461 3-Cl-Ph 4-Pyr 4-Pyr-CH _Two 1-462 3-Cl-Ph 4-Pyr 3-Pyr-CH _Two 1-463 3-Cl-Ph 4-Pyr 2-Pyr-CH _Two 1-464 3-Cl-Ph 4-Pyr 4-Pym-CH _Two 1-465 3-Cl-Ph 4-Pyr 5-Pym-CH _Two 1-466 3-Cl-Ph 4-Pyr 2-Pym-CH _Two 1-467 Ph 2-NH _Two -4-Pym H _Two N-CH _Two 1-468 Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Two 1-469 Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 1-470 Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Four 1-471 Ph 2-NH _Two -4-Pym MeNH-CH _Two 1-472 Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Two 1-473 Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 1-474 Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Four 1-475 Ph 2-NH _Two -4-Pym EtNH-CH _Two 1-476 Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Two 1-477 Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 1-478 Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Four 1-479 Ph 2-NH _Two -4-Pym Me _Two N-CH _Two 1-480 Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Two 1-481 Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 1-482 Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Four 1-483 Ph 2-NH _Two -4-Pym 1-Azt-CH _Two 1-484 Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Two 1-485 Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 1-486 Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Four 1-487 Ph 2-NH _Two -4-Pym 1-Pyrd-CH _Two 1-488 Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Two 1-489 Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 1-490 Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Four 1-491 Ph 2-NH _Two -4-Pym 1-Pip-CH _Two 1-492 Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Two 1-493 Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 1-494 Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Four 1-495 Ph 2-NH _Two -4-Pym 1-Mor-CH _Two 1-496 Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Two 1-497 Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 1-498 Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Four 1-499 Ph 2-NH _Two -4-Pym 1-Tmor-CH _Two 1-500 Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Two 1-501 Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 1-502 Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Four 1-503 Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 1-504 Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Two 1-505 Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 1-506 Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-507 Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Four 1-508 Ph 2-NH _Two -4-Pym 3-Azt 1-509 Ph 2-NH _Two -4-Pym 1-Me-3-Azt 1-510 Ph 2-NH _Two -4-Pym 1-Bn-3-Azt 1-511 Ph 2-NH _Two -4-Pym 3-Pyrd 1-512 Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 1-513 Ph 2-NH _Two -4-Pym 3-Pip 1-514 Ph 2-NH _Two -4-Pym 4-Pip 1-515 Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 1-516 Ph 2-NH _Two -4-Pym 1-Me-4-Pip 1-517 Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 1-518 Ph 2-NH _Two -4-Pym 1-Et-4-Pip 1-519 Ph 2-NH _Two -4-Pym 1-Bn-4-Pip 1-520 Ph 2-NH _Two -4-Pym 3-Hpip 1-521 Ph 2-NH _Two -4-Pym 1-Me-3-Hpip 1-522 Ph 2-NH _Two -4-Pym 4-Hpip 1-523 Ph 2-NH _Two -4-Pym 1-Me-4-Hpip 1-524 Ph 2-NH _Two -4-Pym 2-Mor 1-525 Ph 2-NH _Two -4-Pym 1-Me-2-Mor 1-526 Ph 2-NH _Two -4-Pym 2-Tmor 1-527 Ph 2-NH _Two -4-Pym 1-Me-2-Tmor 1-528 Ph 2-NH _Two -4-Pym 1-Piz 1-529 Ph 2-NH _Two -4-Pym 4-Me-1-Piz 1-530 Ph 2-NH _Two -4-Pym 2-Piz 1-531 Ph 2-NH _Two -4-Pym 4-Pyr 1-532 Ph 2-NH _Two -4-Pym 3-Pyr 1-533 Ph 2-NH _Two -4-Pym 2-Pyr 1-534 Ph 2-NH _Two -4-Pym 4-Pym 1-535 Ph 2-NH _Two -4-Pym 5-Pym 1-536 Ph 2-NH _Two -4-Pym 2-Pym 1-537 Ph 2-NH _Two -4-Pym 3-Azt-CH _Two 1-538 Ph 2-NH _Two -4-Pym 1-Me-3-Azt-CH _Two 1-539 Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 1-540 Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 1-541 Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 1-542 Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 1-543 Ph 2-NH _Two -4-Pym 3-Hpip-CH _Two 1-544 Ph 2-NH _Two -4-Pym 1-Me-3-Hpip-CH _Two 1-545 Ph 2-NH _Two -4-Pym 4-Hpip-CH _Two 1-546 Ph 2-NH _Two -4-Pym 1-Me-4-Hpip-CH _Two 1-547 Ph 2-NH _Two -4-Pym 2-Mor-CH _Two 1-548 Ph 2-NH _Two -4-Pym 1-Me-2-Mor-CH _Two 1-549 Ph 2-NH _Two -4-Pym 2-Tmor-CH _Two 1-550 Ph 2-NH _Two -4-Pym 1-Me-2-Tmor-CH _Two 1-551 Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 1-552 Ph 2-NH _Two -4-Pym 4-Me-1-Piz-CH _Two 1-553 Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 1-554 Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 1-555 Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 1-556 Ph 2-NH _Two -4-Pym 2-Pyr-CH _Two 1-557 Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 1-558 Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 1-559 Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 1-560 4-F-Ph 2-NH _Two -4-Pym H _Two N-CH _Two 1-561 4-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Two 1-562 4-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 1-563 4-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Four 1-564 4-F-Ph 2-NH _Two -4-Pym MeNH-CH _Two 1-565 4-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Two 1-566 4-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 1-567 4-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Four 1-568 4-F-Ph 2-NH _Two -4-Pym EtNH-CH _Two 1-569 4-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Two 1-570 4-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 1-571 4-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Four 1-572 4-F-Ph 2-NH _Two -4-Pym Me _Two N-CH _Two 1-573 4-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Two 1-574 4-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 1-575 4-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Four 1-576 4-F-Ph 2-NH _Two -4-Pym 1-Azt-CH _Two 1-577 4-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Two 1-578 4-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 1-579 4-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Four 1-580 4-F-Ph 2-NH _Two -4-Pym 1-Pyrd-CH _Two 1-581 4-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Two 1-582 4-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 1-583 4-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Four 1-584 4-F-Ph 2-NH _Two -4-Pym 1-Pip-CH _Two 1-585 4-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Two 1-586 4-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 1-587 4-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Four 1-588 4-F-Ph 2-NH _Two -4-Pym 1-Mor-CH _Two 1-589 4-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Two 1-590 4-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 1-591 4-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Four 1-592 4-F-Ph 2-NH _Two -4-Pym 1-Tmor-CH _Two 1-593 4-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Two 1-594 4-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 1-595 4-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Four 1-596 4-F-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 1-597 4-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Two 1-598 4-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 1-599 4-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-600 4-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Four 1-601 4-F-Ph 2-NH _Two -4-Pym 3-Azt 1-602 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 1-603 4-F-Ph 2-NH _Two -4-Pym 1-Bn-3-Azt 1-604 4-F-Ph 2-NH _Two -4-Pym 3-Pyrd 1-605 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 1-606 4-F-Ph 2-NH _Two -4-Pym 3-Pip 1-607 4-F-Ph 2-NH _Two -4-Pym 4-Pip 1-608 4-F-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 1-609 4-F-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 1-610 4-F-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 1-611 4-F-Ph 2-NH _Two -4-Pym 1-Et-4-Pip 1-612 4-F-Ph 2-NH _Two -4-Pym 1-Bn-4-Pip 1-613 4-F-Ph 2-NH _Two -4-Pym 3-Hpip 1-614 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip 1-615 4-F-Ph 2-NH _Two -4-Pym 4-Hpip 1-616 4-F-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip 1-617 4-F-Ph 2-NH _Two -4-Pym 2-Mor 1-618 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Mor 1-619 4-F-Ph 2-NH _Two -4-Pym 2-Tmor 1-620 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor 1-621 4-F-Ph 2-NH _Two -4-Pym 1-Piz 1-622 4-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 1-623 4-F-Ph 2-NH _Two -4-Pym 2-Piz 1-624 4-F-Ph 2-NH _Two -4-Pym 4-Pyr 1-625 4-F-Ph 2-NH _Two -4-Pym 3-Pyr 1-626 4-F-Ph 2-NH _Two -4-Pym 2-Pyr 1-627 4-F-Ph 2-NH _Two -4-Pym 4-Pym 1-628 4-F-Ph 2-NH _Two -4-Pym 5-Pym 1-629 4-F-Ph 2-NH _Two -4-Pym 2-Pym 1-630 4-F-Ph 2-NH _Two -4-Pym 3-Azt-CH _Two 1-631 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Azt-CH _Two 1-632 4-F-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 1-633 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 1-634 4-F-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 1-635 4-F-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 1-636 4-F-Ph 2-NH _Two -4-Pym 3-Hpip-CH _Two 1-637 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip-CH _Two 1-638 4-F-Ph 2-NH _Two -4-Pym 4-Hpip-CH _Two 1-639 4-F-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip-CH _Two 1-640 4-F-Ph 2-NH _Two -4-Pym 2-Mor-CH _Two 1-641 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Mor-CH _Two 1-642 4-F-Ph 2-NH _Two -4-Pym 2-Tmor-CH _Two 1-643 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor-CH _Two 1-644 4-F-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 1-645 4-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz-CH _Two 1-646 4-F-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 1-647 4-F-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 1-648 4-F-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 1-649 4-F-Ph 2-NH _Two -4-Pym 2-Pyr-CH _Two 1-650 4-F-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 1-651 4-F-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 1-652 4-F-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 1-653 3-F-Ph 2-NH _Two -4-Pym H _Two N-CH _Two 1-654 3-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Two 1-655 3-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 1-656 3-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Four 1-657 3-F-Ph 2-NH _Two -4-Pym MeNH-CH _Two 1-658 3-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Two 1-659 3-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 1-660 3-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Four 1-661 3-F-Ph 2-NH _Two -4-Pym EtNH-CH _Two 1-662 3-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Two 1-663 3-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 1-664 3-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Four 1-665 3-F-Ph 2-NH _Two -4-Pym Me _Two N-CH _Two 1-666 3-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Two 1-667 3-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 1-668 3-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Four 1-669 3-F-Ph 2-NH _Two -4-Pym 1-Azt-CH _Two 1-670 3-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Two 1-671 3-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 1-672 3-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Four 1-673 3-F-Ph 2-NH _Two -4-Pym 1-Pyrd-CH _Two 1-674 3-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Two 1-675 3-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 1-676 3-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Four 1-677 3-F-Ph 2-NH _Two -4-Pym 1-Pip-CH _Two 1-678 3-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Two 1-679 3-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 1-680 3-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Four 1-681 3-F-Ph 2-NH _Two -4-Pym 1-Mor-CH _Two 1-682 3-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Two 1-683 3-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 1-684 3-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Four 1-685 3-F-Ph 2-NH _Two -4-Pym 1-Tmor-CH _Two 1-686 3-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Two 1-687 3-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 1-688 3-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Four 1-689 3-F-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 1-690 3-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Two 1-691 3-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 1-692 3-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-693 3-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Four 1-694 3-F-Ph 2-NH _Two -4-Pym 3-Azt 1-695 3-F-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 1-696 3-F-Ph 2-NH _Two -4-Pym 1-Bn-3-Azt 1-697 3-F-Ph 2-NH _Two -4-Pym 3-Pyrd 1-698 3-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 1-699 3-F-Ph 2-NH _Two -4-Pym 3-Pip 1-700 3-F-Ph 2-NH _Two -4-Pym 4-Pip 1-701 3-F-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 1-702 3-F-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 1-703 3-F-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 1-704 3-F-Ph 2-NH _Two -4-Pym 1-Et-4-Pip 1-705 3-F-Ph 2-NH _Two -4-Pym 1-Bn-4-Pip 1-706 3-F-Ph 2-NH _Two -4-Pym 3-Hpip 1-707 3-F-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip 1-708 3-F-Ph 2-NH _Two -4-Pym 4-Hpip 1-709 3-F-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip 1-710 3-F-Ph 2-NH _Two -4-Pym 2-Mor 1-711 3-F-Ph 2-NH _Two -4-Pym 1-Me-2-Mor 1-712 3-F-Ph 2-NH _Two -4-Pym 2-Tmor 1-713 3-F-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor 1-714 3-F-Ph 2-NH _Two -4-Pym 1-Piz 1-715 3-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 1-716 3-F-Ph 2-NH _Two -4-Pym 2-Piz 1-717 3-F-Ph 2-NH _Two -4-Pym 4-Pyr 1-718 3-F-Ph 2-NH _Two -4-Pym 3-Pyr 1-719 3-F-Ph 2-NH _Two -4-Pym 2-Pyr 1-720 3-F-Ph 2-NH _Two -4-Pym 4-Pym 1-721 3-F-Ph 2-NH _Two -4-Pym 5-Pym 1-722 3-F-Ph 2-NH _Two -4-Pym 2-Pym 1-723 3-F-Ph 2-NH _Two -4-Pym 3-Azt-CH _Two 1-724 3-F-Ph 2-NH _Two -4-Pym 1-Me-3-Azt-CH _Two 1-725 3-F-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 1-726 3-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 1-727 3-F-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 1-728 3-F-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 1-729 3-F-Ph 2-NH _Two -4-Pym 3-Hpip-CH _Two 1-730 3-F-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip-CH _Two 1-731 3-F-Ph 2-NH _Two -4-Pym 4-Hpip-CH _Two 1-732 3-F-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip-CH _Two 1-733 3-F-Ph 2-NH _Two -4-Pym 2-Mor-CH _Two 1-734 3-F-Ph 2-NH _Two -4-Pym 1-Me-2-Mor-CH _Two 1-735 3-F-Ph 2-NH _Two -4-Pym 2-Tmor-CH _Two 1-736 3-F-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor-CH _Two 1-737 3-F-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 1-738 3-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz-CH _Two 1-739 3-F-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 1-740 3-F-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 1-741 3-F-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 1-742 3-F-Ph 2-NH _Two -4-Pym 2-Pyr-CH _Two 1-743 3-F-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 1-744 3-F-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 1-745 3-F-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 1-746 3,4-diF-Ph 2-NH _Two -4-Pym H _Two N-CH _Two 1-747 3,4-diF-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Two 1-748 3,4-diF-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 1-749 3,4-diF-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Four 1-750 3,4-diF-Ph 2-NH _Two -4-Pym MeNH-CH _Two 1-751 3,4-diF-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Two 1-752 3,4-diF-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 1-753 3,4-diF-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Four 1-754 3,4-diF-Ph 2-NH _Two -4-Pym EtNH-CH _Two 1-755 3,4-diF-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Two 1-756 3,4-diF-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 1-757 3,4-diF-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Four 1-758 3,4-diF-Ph 2-NH _Two -4-Pym Me _Two N-CH _Two 1-759 3,4-diF-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Two 1-760 3,4-diF-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 1-761 3,4-diF-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Four 1-762 3,4-diF-Ph 2-NH _Two -4-Pym 1-Azt-CH _Two 1-763 3,4-diF-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Two 1-764 3,4-diF-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 1-765 3,4-diF-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Four 1-766 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pyrd-CH _Two 1-767 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Two 1-768 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 1-769 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Four 1-770 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pip-CH _Two 1-771 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Two 1-772 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 1-773 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Four 1-774 3,4-diF-Ph 2-NH _Two -4-Pym 1-Mor-CH _Two 1-775 3,4-diF-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Two 1-776 3,4-diF-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 1-777 3,4-diF-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Four 1-778 3,4-diF-Ph 2-NH _Two -4-Pym 1-Tmor-CH _Two 1-779 3,4-diF-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Two 1-780 3,4-diF-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 1-781 3,4-diF-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Four 1-782 3,4-diF-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 1-783 3,4-diF-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Two 1-784 3,4-diF-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 1-785 3,4-diF-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-786 3,4-diF-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Four 1-787 3,4-diF-Ph 2-NH _Two -4-Pym 3-Azt 1-788 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 1-789 3,4-diF-Ph 2-NH _Two -4-Pym 1-Bn-3-Azt 1-790 3,4-diF-Ph 2-NH _Two -4-Pym 3-Pyrd 1-791 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 1-792 3,4-diF-Ph 2-NH _Two -4-Pym 3-Pip 1-793 3,4-diF-Ph 2-NH _Two -4-Pym 4-Pip 1-794 3,4-diF-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 1-795 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 1-796 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 1-797 3,4-diF-Ph 2-NH _Two -4-Pym 1-Et-4-Pip 1-798 3,4-diF-Ph 2-NH _Two -4-Pym 1-Bn-4-Pip 1-799 3,4-diF-Ph 2-NH _Two -4-Pym 3-Hpip 1-800 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip 1-801 3,4-diF-Ph 2-NH _Two -4-Pym 4-Hpip 1-802 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip 1-803 3,4-diF-Ph 2-NH _Two -4-Pym 2-Mor 1-804 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-2-Mor 1-805 3,4-diF-Ph 2-NH _Two -4-Pym 2-Tmor 1-806 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor 1-807 3,4-diF-Ph 2-NH _Two -4-Pym 1-Piz 1-808 3,4-diF-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 1-809 3,4-diF-Ph 2-NH _Two -4-Pym 2-Piz 1-810 3,4-diF-Ph 2-NH _Two -4-Pym 4-Pyr 1-811 3,4-diF-Ph 2-NH _Two -4-Pym 3-Pyr 1-812 3,4-diF-Ph 2-NH _Two -4-Pym 2-Pyr 1-813 3,4-diF-Ph 2-NH _Two -4-Pym 4-Pym 1-814 3,4-diF-Ph 2-NH _Two -4-Pym 5-Pym 1-815 3,4-diF-Ph 2-NH _Two -4-Pym 2-Pym 1-816 3,4-diF-Ph 2-NH _Two -4-Pym 3-Azt-CH _Two 1-817 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-3-Azt-CH _Two 1-818 3,4-diF-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 1-819 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 1-820 3,4-diF-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 1-821 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 1-822 3,4-diF-Ph 2-NH _Two -4-Pym 3-Hpip-CH _Two 1-823 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip-CH _Two 1-824 3,4-diF-Ph 2-NH _Two -4-Pym 4-Hpip-CH _Two 1-825 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip-CH _Two 1-826 3,4-diF-Ph 2-NH _Two -4-Pym 2-Mor-CH _Two 1-827 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-2-Mor-CH _Two 1-828 3,4-diF-Ph 2-NH _Two -4-Pym 2-Tmor-CH _Two 1-829 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor-CH _Two 1-830 3,4-diF-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 1-831 3,4-diF-Ph 2-NH _Two -4-Pym 4-Me-1-Piz-CH _Two 1-832 3,4-diF-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 1-833 3,4-diF-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 1-834 3,4-diF-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 1-835 3,4-diF-Ph 2-NH _Two -4-Pym 2-Pyr-CH _Two 1-836 3,4-diF-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 1-837 3,4-diF-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 1-838 3,4-diF-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 1-839 3-Cl-Ph 2-NH _Two -4-Pym H _Two N-CH _Two 1-840 3-Cl-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Two 1-841 3-Cl-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 1-842 3-Cl-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Four 1-843 3-Cl-Ph 2-NH _Two -4-Pym MeNH-CH _Two 1-844 3-Cl-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Two 1-845 3-Cl-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 1-846 3-Cl-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Four 1-847 3-Cl-Ph 2-NH _Two -4-Pym EtNH-CH _Two 1-848 3-Cl-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Two 1-849 3-Cl-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 1-850 3-Cl-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Four 1-851 3-Cl-Ph 2-NH _Two -4-Pym Me _Two N-CH _Two 1-852 3-Cl-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Two 1-853 3-Cl-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 1-854 3-Cl-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Four 1-855 3-Cl-Ph 2-NH _Two -4-Pym 1-Azt-CH _Two 1-856 3-Cl-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Two 1-857 3-Cl-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 1-858 3-Cl-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Four 1-859 3-Cl-Ph 2-NH _Two -4-Pym 1-Pyrd-CH _Two 1-860 3-Cl-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Two 1-861 3-Cl-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 1-862 3-Cl-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Four 1-863 3-Cl-Ph 2-NH _Two -4-Pym 1-Pip-CH _Two 1-864 3-Cl-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Two 1-865 3-Cl-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 1-866 3-Cl-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Four 1-867 3-Cl-Ph 2-NH _Two -4-Pym 1-Mor-CH _Two 1-868 3-Cl-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Two 1-869 3-Cl-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 1-870 3-Cl-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Four 1-871 3-Cl-Ph 2-NH _Two -4-Pym 1-Tmor-CH _Two 1-872 3-Cl-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Two 1-873 3-Cl-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 1-874 3-Cl-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Four 1-875 3-Cl-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 1-876 3-Cl-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Two 1-877 3-Cl-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 1-878 3-Cl-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-879 3-Cl-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Four 1-880 3-Cl-Ph 2-NH _Two -4-Pym 3-Azt 1-881 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 1-882 3-Cl-Ph 2-NH _Two -4-Pym 1-Bn-3-Azt 1-883 3-Cl-Ph 2-NH _Two -4-Pym 3-Pyrd 1-884 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 1-885 3-Cl-Ph 2-NH _Two -4-Pym 3-Pip 1-886 3-Cl-Ph 2-NH _Two -4-Pym 4-Pip 1-887 3-Cl-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 1-888 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 1-889 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 1-890 3-Cl-Ph 2-NH _Two -4-Pym 1-Et-4-Pip 1-891 3-Cl-Ph 2-NH _Two -4-Pym 1-Bn-4-Pip 1-892 3-Cl-Ph 2-NH _Two -4-Pym 3-Hpip 1-893 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip 1-894 3-Cl-Ph 2-NH _Two -4-Pym 4-Hpip 1-895 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip 1-896 3-Cl-Ph 2-NH _Two -4-Pym 2-Mor 1-897 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-2-Mor 1-898 3-Cl-Ph 2-NH _Two -4-Pym 2-Tmor 1-899 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor 1-900 3-Cl-Ph 2-NH _Two -4-Pym 1-Piz 1-901 3-Cl-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 1-902 3-Cl-Ph 2-NH _Two -4-Pym 2-Piz 1-903 3-Cl-Ph 2-NH _Two -4-Pym 4-Pyr 1-904 3-Cl-Ph 2-NH _Two -4-Pym 3-Pyr 1-905 3-Cl-Ph 2-NH _Two -4-Pym 2-Pyr 1-906 3-Cl-Ph 2-NH _Two -4-Pym 4-Pym 1-907 3-Cl-Ph 2-NH _Two -4-Pym 5-Pym 1-908 3-Cl-Ph 2-NH _Two -4-Pym 2-Pym 1-909 3-Cl-Ph 2-NH _Two -4-Pym 3-Azt-CH _Two 1-910 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-3-Azt-CH _Two 1-911 3-Cl-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 1-912 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 1-913 3-Cl-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 1-914 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 1-915 3-Cl-Ph 2-NH _Two -4-Pym 3-Hpip-CH _Two 1-916 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip-CH _Two 1-917 3-Cl-Ph 2-NH _Two -4-Pym 4-Hpip-CH _Two 1-918 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip-CH _Two 1-919 3-Cl-Ph 2-NH _Two -4-Pym 2-Mor-CH _Two 1-920 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-2-Mor-CH _Two 1-921 3-Cl-Ph 2-NH _Two -4-Pym 2-Tmor-CH _Two 1-922 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor-CH _Two 1-923 3-Cl-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 1-924 3-Cl-Ph 2-NH _Two -4-Pym 4-Me-1-Piz-CH _Two 1-925 3-Cl-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 1-926 3-Cl-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 1-927 3-Cl-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 1-928 3-Cl-Ph 2-NH _Two -4-Pym 2-Pyr-CH _Two 1-929 3-Cl-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 1-930 3-Cl-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 1-931 3-Cl-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 1-932 Ph 2-MeNH-4-Pym H _Two N-CH _Two 1-933 Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Two 1-934 Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 1-935 Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Four 1-936 Ph 2-MeNH-4-Pym MeNH-CH _Two 1-937 Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Two 1-938 Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 1-939 Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Four 1-940 Ph 2-MeNH-4-Pym EtNH-CH _Two 1-941 Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Two 1-942 Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 1-943 Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Four 1-944 Ph 2-MeNH-4-Pym Me _Two N-CH _Two 1-945 Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Two 1-946 Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 1-947 Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Four 1-948 Ph 2-MeNH-4-Pym 1-Azt-CH _Two 1-949 Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Two 1-950 Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 1-951 Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Four 1-952 Ph 2-MeNH-4-Pym 1-Pyrd-CH _Two 1-953 Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Two 1-954 Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 1-955 Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Four 1-956 Ph 2-MeNH-4-Pym 1-Pip-CH _Two 1-957 Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Two 1-958 Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 1-959 Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Four 1-960 Ph 2-MeNH-4-Pym 1-Mor-CH _Two 1-961 Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Two 1-962 Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 1-963 Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Four 1-964 Ph 2-MeNH-4-Pym 1-Tmor-CH _Two 1-965 Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Two 1-966 Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 1-967 Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Four 1-968 Ph 2-MeNH-4-Pym 1-Piz-CH _Two 1-969 Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Two 1-970 Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 1-971 Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-972 Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Four 1-973 Ph 2-MeNH-4-Pym 3-Azt 1-974 Ph 2-MeNH-4-Pym 1-Me-3-Azt 1-975 Ph 2-MeNH-4-Pym 1-Bn-3-Azt 1-976 Ph 2-MeNH-4-Pym 3-Pyrd 1-977 Ph 2-MeNH-4-Pym 1-Me-3-Pyrd 1-978 Ph 2-MeNH-4-Pym 3-Pip 1-979 Ph 2-MeNH-4-Pym 4-Pip 1-980 Ph 2-MeNH-4-Pym 4- (3,4-deH-Pip) 1-981 Ph 2-MeNH-4-Pym 1-Me-4-Pip 1-982 Ph 2-MeNH-4-Pym 1-Me-4- (3,4-deH-Pip) 1-983 Ph 2-MeNH-4-Pym 1-Et-4-Pip 1-984 Ph 2- MeNH-4-Pym 1-Bn-4-Pip 1-985 Ph 2-MeNH-4-Pym 3-Hpip 1-986 Ph 2-MeNH-4-Pym 1-Me-3-Hpip 1-987 Ph 2- MeNH-4-Pym 4-Hpip 1-988 Ph 2-MeNH-4-Pym 1-Me-4-Hpip 1-989 Ph 2-MeNH-4-Pym 2-Mor 1-990 Ph 2-MeNH-4- Pym 1-Me-2-Mor 1-991 Ph 2-MeNH-4-Pym 2-Tmor 1-992 Ph 2-MeNH-4-Pym 1-Me-2-Tmor 1-993 Ph 2-MeNH-4- Pym 1-Piz 1-994 Ph 2-MeNH-4-Pym 4-Me-1-Piz 1-995 Ph 2-MeNH-4-Pym 2-Piz 1-996 Ph 2-MeNH-4-Pym 4-Pyr 1-997 Ph 2-MeNH-4-Pym 3-Pyr 1-998 Ph 2-MeNH-4-Pym 2-Pyr 1-999 Ph 2-MeNH-4-Pym 4-Pym 1-1000 Ph 2-MeNH- 4-Pym 5-Pym 1-1001 Ph 2-MeNH-4-Pym 2-Pym 1-1002 Ph 2-MeNH-4-Pym 3-Azt-CH _Two 1-1003 Ph 2-MeNH-4-Pym 1-Me-3-Azt-CH _Two 1-1004 Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 1-1005 Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 1-1006 Ph 2-MeNH-4-Pym 4-Pip-CH _Two 1-1007 Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 1-1008 Ph 2-MeNH-4-Pym 3-Hpip-CH _Two 1-1009 Ph 2-MeNH-4-Pym 1-Me-3-Hpip-CH _Two 1-1010 Ph 2-MeNH-4-Pym 4-Hpip-CH _Two 1-1011 Ph 2-MeNH-4-Pym 1-Me-4-Hpip-CH _Two 1-1012 Ph 2-MeNH-4-Pym 2-Mor-CH _Two 1-1013 Ph 2-MeNH-4-Pym 1-Me-2-Mor-CH _Two 1-1014 Ph 2-MeNH-4-Pym 2-Tmor-CH _Two 1-1015 Ph 2-MeNH-4-Pym 1-Me-2-Tmor-CH _Two 1-1016 Ph 2-MeNH-4-Pym 1-Piz-CH _Two 1-1017 Ph 2-MeNH-4-Pym 4-Me-1-Piz-CH _Two 1-1018 Ph 2-MeNH-4-Pym 2-Piz-CH _Two 1-1019 Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 1-1020 Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 1-1021 Ph 2-MeNH-4-Pym 2-Pyr-CH _Two 1-1022 Ph 2-MeNH-4-Pym 4-Pym-CH _Two 1-1023 Ph 2-MeNH-4-Pym 5-Pym-CH _Two 1-1024 Ph 2-MeNH-4-Pym 2-Pym-CH _Two 1-1025 4-F-Ph 2-MeNH-4-Pym H _Two N-CH _Two 1-1026 4-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Two 1-1027 4-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 1-1028 4-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Four 1-1029 4-F-Ph 2-MeNH-4-Pym MeNH-CH _Two 1-1030 4-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Two 1-1031 4-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 1-1032 4-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Four 1-1033 4-F-Ph 2-MeNH-4-Pym EtNH-CH _Two 1-1034 4-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Two 1-1035 4-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 1-1036 4-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Four 1-1037 4-F-Ph 2-MeNH-4-Pym Me _Two N-CH _Two 1-1038 4-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Two 1-1039 4-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 1-1040 4-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Four 1-1041 4-F-Ph 2-MeNH-4-Pym 1-Azt-CH _Two 1-1042 4-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Two 1-1043 4-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 1-1044 4-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Four 1-1045 4-F-Ph 2-MeNH-4-Pym 1-Pyrd-CH _Two 1-1046 4-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Two 1-1047 4-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 1-1048 4-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Four 1-1049 4-F-Ph 2-MeNH-4-Pym 1-Pip-CH _Two 1-1050 4-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Two 1-1051 4-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 1-1052 4-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Four 1-1053 4-F-Ph 2-MeNH-4-Pym 1-Mor-CH _Two 1-1054 4-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Two 1-1055 4-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 1-1056 4-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Four 1-1057 4-F-Ph 2-MeNH-4-Pym 1-Tmor-CH _Two 1-1058 4-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Two 1-1059 4-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 1-1060 4-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Four 1-1061 4-F-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 1-1062 4-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Two 1-1063 4-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 1-1064 4-F-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-1065 4-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Four 1-1066 4-F-Ph 2-MeNH-4-Pym 3-Azt 1-1067 4-F-Ph 2-MeNH-4-Pym 1-Me-3-Azt 1-1068 4-F-Ph 2- MeNH-4-Pym 1-Bn-3-Azt 1-1069 4-F-Ph 2-MeNH-4-Pym 3-Pyrd 1-1070 4-F-Ph 2-MeNH-4-Pym 1-Me-3 -Pyrd 1-1071 4-F-Ph 2-MeNH-4-Pym 3-Pip 1-1072 4-F-Ph 2-MeNH-4-Pym 4-Pip 1-1073 4-F-Ph 2-MeNH- 4-Pym 4- (3,4-deH-Pip) 1-1074 4-F-Ph 2-MeNH-4-Pym 1-Me-4-Pip 1-1075 4-F-Ph 2-MeNH-4- Pym 1-Me-4- (3,4-deH-Pip) 1-1076 4-F-Ph 2-MeNH-4-Pym 1-Et-4-Pip 1-1077 4-F-Ph 2-MeNH- 4-Pym 1-Bn-4-Pip 1-1078 4-F-Ph 2-MeNH-4-Pym 3-Hpip 1-1079 4-F-Ph 2-MeNH-4-Pym 1-Me-3-Hpip 1-1080 4-F-Ph 2-MeNH-4-Pym 4-Hpip 1-1081 4-F-Ph 2-MeNH-4-Pym 1-Me-4-Hpip 1-1082 4-F-Ph 2- MeNH-4-Pym 2-Mor 1-1083 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Mor 1-1084 4-F-Ph 2-MeNH-4-Pym 2-Tmor 1- 1085 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Tmor 1-1086 4-F-Ph 2-MeNH-4-Pym 1-Piz 1-1087 4-F-Ph 2-MeNH- 4-Pym 4-Me-1-Piz 1-1088 4-F-Ph 2-MeNH-4-Pym 2-Piz 1-1089 4-F-Ph 2-MeNH-4-Pym 4-Pyr 1-1090 4 -F-Ph 2-MeNH-4-Pym 3-Pyr 1-1091 4-F-Ph 2-MeNH-4-Pym 2-Pyr 1-1092 4-F-Ph 2-MeNH-4-Pym 4-Pym 1-1093 4-F-Ph 2-MeNH- 4-Pym 5-Pym 1-1094 4-F-Ph 2-MeNH-4-Pym 2-Pym 1-1095 4-F-Ph 2-MeNH-4-Pym 3-Azt-CH _Two 1-1096 4-F-Ph 2-MeNH-4-Pym 1-Me-3-Azt-CH _Two 1-1097 4-F-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 1-1098 4-F-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 1-1099 4-F-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 1-1100 4-F-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 1-1101 4-F-Ph 2-MeNH-4-Pym 3-Hpip-CH _Two 1-1102 4-F-Ph 2-MeNH-4-Pym 1-Me-3-Hpip-CH _Two 1-1103 4-F-Ph 2-MeNH-4-Pym 4-Hpip-CH _Two 1-1104 4-F-Ph 2-MeNH-4-Pym 1-Me-4-Hpip-CH _Two 1-1105 4-F-Ph 2-MeNH-4-Pym 2-Mor-CH _Two 1-1106 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Mor-CH _Two 1-1107 4-F-Ph 2-MeNH-4-Pym 2-Tmor-CH _Two 1-1108 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Tmor-CH _Two 1-1109 4-F-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 1-1110 4-F-Ph 2-MeNH-4-Pym 4-Me-1-Piz-CH _Two 1-1111 4-F-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 1-1112 4-F-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 1-1113 4-F-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 1-1114 4-F-Ph 2-MeNH-4-Pym 2-Pyr-CH _Two 1-1115 4-F-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 1-1116 4-F-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 1-1117 4-F-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 1-1118 3-F-Ph 2-MeNH-4-Pym H _Two N-CH _Two 1-1119 3-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Two 1-1120 3-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 1-1121 3-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Four 1-1122 3-F-Ph 2-MeNH-4-Pym MeNH-CH _Two 1-1123 3-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Two 1-1124 3-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 1-1125 3-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Four 1-1126 3-F-Ph 2-MeNH-4-Pym EtNH-CH _Two 1-1127 3-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Two 1-1128 3-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 1-1129 3-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Four 1-1130 3-F-Ph 2-MeNH-4-Pym Me _Two N-CH _Two 1-1131 3-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Two 1-1132 3-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 1-1133 3-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Four 1-1134 3-F-Ph 2-MeNH-4-Pym 1-Azt-CH _Two 1-1135 3-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Two 1-1136 3-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 1-1137 3-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Four 1-1138 3-F-Ph 2-MeNH-4-Pym 1-Pyrd-CH _Two 1-1139 3-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Two 1-1140 3-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 1-1141 3-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Four 1-1142 3-F-Ph 2-MeNH-4-Pym 1-Pip-CH _Two 1-1143 3-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Two 1-1144 3-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 1-1145 3-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Four 1-1146 3-F-Ph 2-MeNH-4-Pym 1-Mor-CH _Two 1-1147 3-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Two 1-1148 3-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 1-1149 3-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Four 1-1150 3-F-Ph 2-MeNH-4-Pym 1-Tmor-CH _Two 1-1151 3-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Two 1-1152 3-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 1-1153 3-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Four 1-1154 3-F-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 1-1155 3-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Two 1-1156 3-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 1-1157 3-F-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-1158 3-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Four 1-1159 3-F-Ph 2-MeNH-4-Pym 3-Azt 1-1160 3-F-Ph 2-MeNH-4-Pym 1-Me-3-Azt 1-1161 3-F-Ph 2- MeNH-4-Pym 1-Bn-3-Azt 1-1162 3-F-Ph 2-MeNH-4-Pym 3-Pyrd 1-1163 3-F-Ph 2-MeNH-4-Pym 1-Me-3 -Pyrd 1-1164 3-F-Ph 2-MeNH-4-Pym 3-Pip 1-1165 3-F-Ph 2-MeNH-4-Pym 4-Pip 1-1166 3-F-Ph 2-MeNH- 4-Pym 4- (3,4-deH-Pip) 1-1167 3-F-Ph 2-MeNH-4-Pym 1-Me-4-Pip 1-1168 3-F-Ph 2-MeNH-4- Pym 1-Me-4- (3,4-deH-Pip) 1-1169 3-F-Ph 2-MeNH-4-Pym 1-Et-4-Pip 1-1170 3-F-Ph 2-MeNH- 4-Pym 1-Bn-4-Pip 1-1171 3-F-Ph 2-MeNH-4-Pym 3-Hpip 1-1172 3-F-Ph 2-MeNH-4-Pym 1-Me-3-Hpip 1-1173 3-F-Ph 2-MeNH-4-Pym 4-Hpip 1-1174 3-F-Ph 2-MeNH-4-Pym 1-Me-4-Hpip 1-1175 3-F-Ph 2- MeNH-4-Pym 2-Mor 1-1176 3-F-Ph 2-MeNH-4-Pym 1-Me-2-Mor 1-1177 3-F-Ph 2-MeNH-4-Pym 2-Tmor 1- 1178 3-F-Ph 2-MeNH-4-Pym 1-Me-2-Tmor 1-1179 3-F-Ph 2-MeNH-4-Pym 1-Piz 1-1180 3-F-Ph 2-MeNH- 4-Pym 4-Me-1-Piz 1-1181 3-F-Ph 2-MeNH-4-Pym 2-Piz 1-1182 3-F-Ph 2-MeNH-4-Pym 4-Pyr 1-1183 3 -F-Ph 2-MeNH-4-Pym 3-Pyr 1-1184 3-F-Ph 2-MeNH-4-Pym 2-Pyr 1-1185 3-F-Ph 2-MeNH-4-Pym 4-Pym 1-1186 3-F-Ph 2-MeNH- 4-Pym 5-Pym 1-1187 3-F-Ph 2-MeNH-4-Pym 2-Pym 1-1188 3-F-Ph 2-MeNH-4-Pym 3-Azt-CH _Two 1-1189 3-F-Ph 2-MeNH-4-Pym 1-Me-3-Azt-CH _Two 1-1190 3-F-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 1-1191 3-F-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 1-1192 3-F-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 1-1193 3-F-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 1-1194 3-F-Ph 2-MeNH-4-Pym 3-Hpip-CH _Two 1-1195 3-F-Ph 2-MeNH-4-Pym 1-Me-3-Hpip-CH _Two 1-1196 3-F-Ph 2-MeNH-4-Pym 4-Hpip-CH _Two 1-1197 3-F-Ph 2-MeNH-4-Pym 1-Me-4-Hpip-CH _Two 1-1198 3-F-Ph 2-MeNH-4-Pym 2-Mor-CH _Two 1-1199 3-F-Ph 2-MeNH-4-Pym 1-Me-2-Mor-CH _Two 1-1200 3-F-Ph 2-MeNH-4-Pym 2-Tmor-CH _Two 1-1201 3-F-Ph 2-MeNH-4-Pym 1-Me-2-Tmor-CH _Two 1-1202 3-F-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 1-1203 3-F-Ph 2-MeNH-4-Pym 4-Me-1-Piz-CH _Two 1-1204 3-F-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 1-1205 3-F-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 1-1206 3-F-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 1-1207 3-F-Ph 2-MeNH-4-Pym 2-Pyr-CH _Two 1-1208 3-F-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 1-1209 3-F-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 1-1210 3-F-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 1-1211 3,4-diF-Ph 2-MeNH-4-Pym H _Two N-CH _Two 1-1212 3,4-diF-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Two 1-1213 3,4-diF-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 1-1214 3,4-diF-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Four 1-1215 3,4-diF-Ph 2-MeNH-4-Pym MeNH-CH _Two 1-1216 3,4-diF-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Two 1-1217 3,4-diF-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 1-1218 3,4-diF-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Four 1-1219 3,4-diF-Ph 2-MeNH-4-Pym EtNH-CH _Two 1-1220 3,4-diF-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Two 1-1221 3,4-diF-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 1-1222 3,4-diF-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Four 1-1223 3,4-diF-Ph 2-MeNH-4-Pym Me _Two N-CH _Two 1-1224 3,4-diF-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Two 1-1225 3,4-diF-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 1-1226 3,4-diF-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Four 1-1227 3,4-diF-Ph 2-MeNH-4-Pym 1-Azt-CH _Two 1-1228 3,4-diF-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Two 1-1229 3,4-diF-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 1-1230 3,4-diF-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Four 1-1231 3,4-diF-Ph 2-MeNH-4-Pym 1-Pyrd-CH _Two 1-1232 3,4-diF-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Two 1-1233 3,4-diF-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 1-1234 3,4-diF-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Four 1-1235 3,4-diF-Ph 2-MeNH-4-Pym 1-Pip-CH _Two 1-1236 3,4-diF-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Two 1-1237 3,4-diF-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 1-1238 3,4-diF-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Four 1-1239 3,4-diF-Ph 2-MeNH-4-Pym 1-Mor-CH _Two 1-1240 3,4-diF-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Two 1-1241 3,4-diF-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 1-1242 3,4-diF-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Four 1-1243 3,4-diF-Ph 2-MeNH-4-Pym 1-Tmor-CH _Two 1-1244 3,4-diF-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Two 1-1245 3,4-diF-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 1-1246 3,4-diF-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Four 1-1247 3,4-diF-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 1-1248 3,4-diF-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Two 1-1249 3,4-diF-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 1-1250 3,4-diF-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-1251 3,4-diF-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Four 1-1252 3,4-diF-Ph 2-MeNH-4-Pym 3-Azt 1-1253 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-3-Azt 1-1254 3,4 -diF-Ph 2-MeNH-4-Pym 1-Bn-3-Azt 1-1255 3,4-diF-Ph 2-MeNH-4-Pym 3-Pyrd 1-1256 3,4-diF-Ph 2- MeNH-4-Pym 1-Me-3-Pyrd 1-1257 3,4-diF-Ph 2-MeNH-4-Pym 3-Pip 1-1258 3,4-diF-Ph 2-MeNH-4-Pym 4 -Pip 1-1259 3,4-diF-Ph 2-MeNH-4-Pym 4- (3,4-deH-Pip) 1-1260 3,4-diF-Ph 2-MeNH-4-Pym 1-Me -4-Pip 1-1261 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-4- (3,4-deH-Pip) 1-1262 3,4-diF-Ph 2-MeNH- 4-Pym 1-Et-4-Pip 1-1263 3,4-diF-Ph 2-MeNH-4-Pym 1-Bn-4-Pip 1-1264 3,4-diF-Ph 2-MeNH-4- Pym 3-Hpip 1-1265 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-3-Hpip 1-1266 3,4-diF-Ph 2-MeNH-4-Pym 4-Hpip 1- 1267 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-4-Hpip 1-1268 3,4-diF-Ph 2-MeNH-4-Pym 2-Mor 1-1269 3,4-diF -Ph 2-MeNH-4-Pym 1-Me-2-Mor 1-1270 3,4-diF-Ph 2-MeNH-4-Pym 2-Tmor 1-1271 3,4-diF-Ph 2-MeNH- 4-Pym 1-Me-2-Tmor 1-1272 3,4-diF-Ph 2-MeNH-4-Pym 1-Piz 1-1273 3,4-diF-Ph 2-MeNH-4-Pym 4-Me -1-Piz 1-1274 3,4-diF-Ph 2-MeNH-4-Pym 2-Piz 1-1275 3,4-diF-Ph 2-MeNH-4-Pym 4-Pyr 1-1276 3,4 -diF-Ph 2-MeNH -4-Pym 3-Pyr 1-1277 3,4-diF-Ph 2-MeNH-4-Pym 2-Pyr 1-1278 3,4-diF-Ph 2-MeNH-4-Pym 4-Pym 1-1279 3,4-diF-Ph 2-MeNH-4-Pym 5-Pym 1-1280 3,4-diF-Ph 2-MeNH-4-Pym 2-Pym 1-1281 3,4-diF-Ph 2-MeNH -4-Pym 3-Azt-CH _Two 1-1282 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-3-Azt-CH _Two 1-1283 3,4-diF-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 1-1284 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 1-1285 3,4-diF-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 1-1286 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 1-1287 3,4-diF-Ph 2-MeNH-4-Pym 3-Hpip-CH _Two 1-1288 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-3-Hpip-CH _Two 1-1289 3,4-diF-Ph 2-MeNH-4-Pym 4-Hpip-CH _Two 1-1290 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-4-Hpip-CH _Two 1-1291 3,4-diF-Ph 2-MeNH-4-Pym 2-Mor-CH _Two 1-1292 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-2-Mor-CH _Two 1-1293 3,4-diF-Ph 2-MeNH-4-Pym 2-Tmor-CH _Two 1-1294 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-2-Tmor-CH _Two 1-1295 3,4-diF-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 1-1296 3,4-diF-Ph 2-MeNH-4-Pym 4-Me-1-Piz-CH _Two 1-1297 3,4-diF-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 1-1298 3,4-diF-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 1-1299 3,4-diF-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 1-1300 3,4-diF-Ph 2-MeNH-4-Pym 2-Pyr-CH _Two 1-1301 3,4-diF-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 1-1302 3,4-diF-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 1-1303 3,4-diF-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 1-1304 3-Cl-Ph 2-MeNH-4-Pym H _Two N-CH _Two 1-1305 3-Cl-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Two 1-1306 3-Cl-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 1-1307 3-Cl-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Four 1-1308 3-Cl-Ph 2-MeNH-4-Pym MeNH-CH _Two 1-1309 3-Cl-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Two 1-1310 3-Cl-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 1-1311 3-Cl-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Four 1-1312 3-Cl-Ph 2-MeNH-4-Pym EtNH-CH _Two 1-1313 3-Cl-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Two 1-1314 3-Cl-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 1-1315 3-Cl-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Four 1-1316 3-Cl-Ph 2-MeNH-4-Pym Me _Two N-CH _Two 1-1317 3-Cl-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Two 1-1318 3-Cl-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 1-1319 3-Cl-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Four 1-1320 3-Cl-Ph 2-MeNH-4-Pym 1-Azt-CH _Two 1-1321 3-Cl-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Two 1-1322 3-Cl-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 1-1323 3-Cl-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Four 1-1324 3-Cl-Ph 2-MeNH-4-Pym 1-Pyrd-CH _Two 1-1325 3-Cl-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Two 1-1326 3-Cl-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 1-1327 3-Cl-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Four 1-1328 3-Cl-Ph 2-MeNH-4-Pym 1-Pip-CH _Two 1-1329 3-Cl-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Two 1-1330 3-Cl-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 1-1331 3-Cl-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Four 1-1332 3-Cl-Ph 2-MeNH-4-Pym 1-Mor-CH _Two 1-1333 3-Cl-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Two 1-1334 3-Cl-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 1-1335 3-Cl-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Four 1-1336 3-Cl-Ph 2-MeNH-4-Pym 1-Tmor-CH _Two 1-1337 3-Cl-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Two 1-1338 3-Cl-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 1-1339 3-Cl-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Four 1-1340 3-Cl-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 1-1341 3-Cl-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Two 1-1342 3-Cl-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 1-1343 3-Cl-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-1344 3-Cl-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Four 1-1345 3-Cl-Ph 2-MeNH-4-Pym 3-Azt 1-1346 3-Cl-Ph 2-MeNH-4-Pym 1-Me-3-Azt 1-1347 3-Cl-Ph 2- MeNH-4-Pym 1-Bn-3-Azt 1-1348 3-Cl-Ph 2-MeNH-4-Pym 3-Pyrd 1-1349 3-Cl-Ph 2-MeNH-4-Pym 1-Me-3 -Pyrd 1-1350 3-Cl-Ph 2-MeNH-4-Pym 3-Pip 1-1351 3-Cl-Ph 2-MeNH-4-Pym 4-Pip 1-1352 3-Cl-Ph 2-MeNH- 4-Pym 4- (3,4-deH-Pip) 1-1353 3-Cl-Ph 2-MeNH-4-Pym 1-Me-4-Pip 1-1354 3-Cl-Ph 2-MeNH-4- Pym 1-Me-4- (3,4-deH-Pip) 1-1355 3-Cl-Ph 2-MeNH-4-Pym 1-Et-4-Pip 1-1356 3-Cl-Ph 2-MeNH- 4-Pym 1-Bn-4-Pip 1-1357 3-Cl-Ph 2-MeNH-4-Pym 3-Hpip 1-1358 3-Cl-Ph 2-MeNH-4-Pym 1-Me-3-Hpip 1-1359 3-Cl-Ph 2-MeNH-4-Pym 4-Hpip 1-1360 3-Cl-Ph 2-MeNH-4-Pym 1-Me-4-Hpip 1-1361 3-Cl-Ph 2- MeNH-4-Pym 2-Mor 1-1362 3-Cl-Ph 2-MeNH-4-Pym 1-Me-2-Mor 1-1363 3-Cl-Ph 2-MeNH-4-Pym 2-Tmor 1- 1364 3-Cl-Ph 2-MeNH-4-Pym 1-Me-2-Tmor 1-1365 3-Cl-Ph 2-MeNH-4-Pym 1-Piz 1-1366 3-Cl-Ph 2-MeNH- 4-Pym 4-Me-1-Piz 1-1367 3-Cl-Ph 2-MeNH-4-Pym 2-Piz 1-1368 3-Cl-Ph 2-MeNH-4-Pym 4-Pyr 1-1369 3 -Cl-Ph 2-MeNH-4-Pym 3-Pyr 1-1370 3-Cl-Ph 2-MeNH-4-Pym 2-Pyr 1-1371 3-Cl-Ph 2-MeNH-4-Pym 4-Pym 1-1372 3-Cl-Ph 2-MeNH-4-Pym 5-Pym 1-1373 3-Cl-Ph 2-MeNH-4-Pym 2-Pym 1-1374 3-Cl-Ph 2-MeNH -4-Pym 3-Azt-CH _Two 1-1375 3-Cl-Ph 2-MeNH-4-Pym 1-Me-3-Azt-CH _Two 1-1376 3-Cl-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 1-1377 3-Cl-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 1-1378 3-Cl-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 1-1379 3-Cl-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 1-1380 3-Cl-Ph 2-MeNH-4-Pym 3-Hpip-CH _Two 1-1381 3-Cl-Ph 2-MeNH-4-Pym 1-Me-3-Hpip-CH _Two 1-1382 3-Cl-Ph 2-MeNH-4-Pym 4-Hpip-CH _Two 1-1383 3-Cl-Ph 2-MeNH-4-Pym 1-Me-4-Hpip-CH _Two 1-1384 3-Cl-Ph 2-MeNH-4-Pym 2-Mor-CH _Two 1-1385 3-Cl-Ph 2-MeNH-4-Pym 1-Me-2-Mor-CH _Two 1-1386 3-Cl-Ph 2-MeNH-4-Pym 2-Tmor-CH _Two 1-1387 3-Cl-Ph 2-MeNH-4-Pym 1-Me-2-Tmor-CH _Two 1-1388 3-Cl-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 1-1389 3-Cl-Ph 2-MeNH-4-Pym 4-Me-1-Piz-CH _Two 1-1390 3-Cl-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 1-1391 3-Cl-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 1-1392 3-Cl-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 1-1393 3-Cl-Ph 2-MeNH-4-Pym 2-Pyr-CH _Two 1-1394 3-Cl-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 1-1395 3-Cl-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 1-1396 3-Cl-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 1-1397 3-Cl-4-F-Ph 4-Pyr H _Two N- (CH _Two ) _Three 1-1398 3-Cl-4-F-Ph 4-Pyr MeNH- (CH _Two ) _Three 1-1399 3-Cl-4-F-Ph 4-Pyr EtNH- (CH _Two ) _Three 1-1400 3-Cl-4-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 1-1401 3-Cl-4-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 1-1402 3-Cl-4-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 1-1403 3-Cl-4-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 1-1404 3-Cl-4-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 1-1405 3-Cl-4-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 1-1406 3-Cl-4-F-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 1-1407 3-Cl-4-F-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-1408 3-Cl-4-F-Ph 4-Pyr 3-Azt 1-1409 3-Cl-4-F-Ph 4-Pyr 1-Me-3-Azt 1-1410 3-Cl-4-F -Ph 4-Pyr 3-Pyrd 1-1411 3-Cl-4-F-Ph 4-Pyr 1-Me-3-Pyrd 1-1412 3-Cl-4-F-Ph 4-Pyr 4-Pip 1- 1413 3-Cl-4-F-Ph 4-Pyr 4- (3,4-deH-Pip) 1-1414 3-Cl-4-F-Ph 4-Pyr 1-Me-4-Pip 1-1415 3 -Cl-4-F-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 1-1416 3-Cl-4-F-Ph 4-Pyr 1-Piz 1-1417 3-Cl -4-F-Ph 4-Pyr 4-Me-1-Piz 1-1418 3-Cl-4-F-Ph 4-Pyr 4-Pyr 1-1419 3-Cl-4-F-Ph 4-Pyr 3 -Pyr 1-1420 3-Cl-4-F-Ph 4-Pyr 4-Pym 1-1421 3-Cl-4-F-Ph 4-Pyr 5-Pym 1-1422 3-Cl-4-F-Ph 4-Pyr 3-Pyrd-CH _Two 1-1423 3-Cl-4-F-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 1-1424 3-Cl-4-F-Ph 4-Pyr 4-Pip-CH _Two 1-1425 3-Cl-4-F-Ph 4-Pyr 1-Me-4-Pip-CH _Two 1-1426 3-Cl-4-F-Ph 4-Pyr 2-Piz-CH _Two 1-1427 3-Cl-4-F-Ph 4-Pyr 4-Pyr-CH _Two 1-1428 3-Cl-4-F-Ph 4-Pyr 3-Pyr-CH _Two 1-1429 3-Cl-4-F-Ph 4-Pyr 4-Pym-CH _Two 1-1430 3-Cl-4-F-Ph 4-Pyr 5-Pym-CH _Two 1-1431 3-Cl-4-F-Ph 4-Pyr 2-Pym-CH _Two 1-1432 3,4,5-triF-Ph 4-Pyr H _Two N- (CH _Two ) _Three 1-1433 3,4,5-triF-Ph 4-Pyr MeNH- (CH _Two ) _Three 1-1434 3,4,5-triF-Ph 4-Pyr EtNH- (CH _Two ) _Three 1-1435 3,4,5-triF-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 1-1436 3,4,5-triF-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 1-1437 3,4,5-triF-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 1-1438 3,4,5-triF-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 1-1439 3,4,5-triF-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 1-1440 3,4,5-triF-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 1-1441 3,4,5-triF-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 1-1442 3,4,5-triF-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-1443 3,4,5-triF-Ph 4-Pyr 3-Azt 1-1444 3,4,5-triF-Ph 4-Pyr 1-Me-3-Azt 1-1445 3,4,5-triF -Ph 4-Pyr 3-Pyrd 1-1446 3,4,5-triF-Ph 4-Pyr 1-Me-3-Pyrd 1-1447 3,4,5-triF-Ph 4-Pyr 4-Pip 1- 1448 3,4,5-triF-Ph 4-Pyr 4- (3,4-deH-Pip) 1-1449 3,4,5-triF-Ph 4-Pyr 1-Me-4-Pip 1-1450 3 , 4,5-triF-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 1-1451 3,4,5-triF-Ph 4-Pyr 1-Piz 1-1452 3,4 , 5-triF-Ph 4-Pyr 4-Me-1-Piz 1-1453 3,4,5-triF-Ph 4-Pyr 4-Pyr 1-1454 3,4,5-triF-Ph 4-Pyr 3 -Pyr 1-1455 3,4,5-triF-Ph 4-Pyr 4-Pym 1-1456 3,4,5-triF-Ph 4-Pyr 5-Pym 1-1457 3,4,5-triF-Ph 4-Pyr 3-Pyrd-CH _Two 1-1458 3,4,5-triF-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 1-1459 3,4,5-triF-Ph 4-Pyr 4-Pip-CH _Two 1-1460 3,4,5-triF-Ph 4-Pyr 1-Me-4-Pip-CH _Two 1-1461 3,4,5-triF-Ph 4-Pyr 2-Piz-CH _Two 1-1462 3,4,5-triF-Ph 4-Pyr 4-Pyr-CH _Two 1-1463 3,4,5-triF-Ph 4-Pyr 3-Pyr-CH _Two 1-1464 3,4,5-triF-Ph 4-Pyr 4-Pym-CH _Two 1-1465 3,4,5-triF-Ph 4-Pyr 5-Pym-CH _Two 1-1466 3,4,5-triF-Ph 4-Pyr 2-Pym-CH _Two 1-1467 3-CF _Three -Ph 4-Pyr H _Two N- (CH _Two ) _Three 1-1468 3-CF _Three -Ph 4-Pyr MeNH- (CH _Two ) _Three 1-1469 3-CF _Three -Ph 4-Pyr EtNH- (CH _Two ) _Three 1-1470 3-CF _Three -Ph 4-Pyr Me _Two N- (CH _Two ) _Three 1-1471 3-CF _Three -Ph 4-Pyr 1-Azt- (CH _Two ) _Three 1-1472 3-CF _Three -Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 1-1473 3-CF _Three -Ph 4-Pyr 1-Pip- (CH _Two ) _Three 1-1474 3-CF _Three -Ph 4-Pyr 1-Mor- (CH _Two ) _Three 1-1475 3-CF _Three -Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 1-1476 3-CF _Three -Ph 4-Pyr 1-Piz- (CH _Two ) _Three 1-1477 3-CF _Three -Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-1478 3-CF _Three -Ph 4-Pyr 3-Azt 1-1479 3-CF _Three -Ph 4-Pyr 1-Me-3-Azt 1-1480 3-CF _Three -Ph 4-Pyr 3-Pyrd 1-1481 3-CF _Three -Ph 4-Pyr 1-Me-3-Pyrd 1-1482 3-CF _Three -Ph 4-Pyr 4-Pip 1-1483 3-CF _Three -Ph 4-Pyr 4- (3,4-deH-Pip) 1-1484 3-CF _Three -Ph 4-Pyr 1-Me-4-Pip 1-1485 3-CF _Three -Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 1-1486 3-CF _Three -Ph 4-Pyr 1-Piz 1-1487 3-CF _Three -Ph 4-Pyr 4-Me-1-Piz 1-1488 3-CF _Three -Ph 4-Pyr 4-Pyr 1-1489 3-CF _Three -Ph 4-Pyr 3-Pyr 1-1490 3-CF _Three -Ph 4-Pyr 4-Pym 1-1491 3-CF _Three -Ph 4-Pyr 5-Pym 1-1492 3-CF _Three -Ph 4-Pyr 3-Pyrd-CH _Two 1-1493 3-CF _Three -Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 1-1494 3-CF _Three -Ph 4-Pyr 4-Pip-CH _Two 1-1495 3-CF _Three -Ph 4-Pyr 1-Me-4-Pip-CH _Two 1-1496 3-CF _Three -Ph 4-Pyr 2-Piz-CH _Two 1-1497 3-CF _Three -Ph 4-Pyr 4-Pyr-CH _Two 1-1498 3-CF _Three -Ph 4-Pyr 3-Pyr-CH _Two 1-1499 3-CF _Three -Ph 4-Pyr 4-Pym-CH _Two 1-1500 3-CF _Three -Ph 4-Pyr 5-Pym-CH _Two 1-1501 3-CF _Three -Ph 4-Pyr 2-Pym-CH _Two 1-1502 3-CHF _Two O-Ph 4-Pyr H _Two N- (CH _Two ) _Three 1-1503 3-CHF _Two O-Ph 4-Pyr MeNH- (CH _Two ) _Three 1-1504 3-CHF _Two O-Ph 4-Pyr EtNH- (CH _Two ) _Three 1-1505 3-CHF _Two O-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 1-1506 3-CHF _Two O-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 1-1507 3-CHF _Two O-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 1-1508 3-CHF _Two O-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 1-1509 3-CHF _Two O-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 1-1510 3-CHF _Two O-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 1-1511 3-CHF _Two O-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 1-1512 3-CHF _Two O-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-1513 3-CHF _Two O-Ph 4-Pyr 3-Azt 1-1514 3-CHF _Two O-Ph 4-Pyr 1-Me-3-Azt 1-1515 3-CHF _Two O-Ph 4-Pyr 3-Pyrd 1-1516 3-CHF _Two O-Ph 4-Pyr 1-Me-3-Pyrd 1-1517 3-CHF _Two O-Ph 4-Pyr 4-Pip 1-1518 3-CHF _Two O-Ph 4-Pyr 4- (3,4-deH-Pip) 1-1519 3-CHF _Two O-Ph 4-Pyr 1-Me-4-Pip 1-1520 3-CHF _Two O-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 1-1521 3-CHF _Two O-Ph 4-Pyr 1-Piz 1-1522 3-CHF _Two O-Ph 4-Pyr 4-Me-1-Piz 1-1523 3-CHF _Two O-Ph 4-Pyr 4-Pyr 1-1524 3-CHF _Two O-Ph 4-Pyr 3-Pyr 1-1525 3-CHF _Two O-Ph 4-Pyr 4-Pym 1-1526 3-CHF _Two O-Ph 4-Pyr 5-Pym 1-1527 3-CHF _Two O-Ph 4-Pyr 3-Pyrd-CH _Two 1-1528 3-CHF _Two O-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 1-1529 3-CHF _Two O-Ph 4-Pyr 4-Pip-CH _Two 1-1530 3-CHF _Two O-Ph 4-Pyr 1-Me-4-Pip-CH _Two 1-1531 3-CHF _Two O-Ph 4-Pyr 2-Piz-CH _Two 1-1532 3-CHF _Two O-Ph 4-Pyr 4-Pyr-CH _Two 1-1533 3-CHF _Two O-Ph 4-Pyr 3-Pyr-CH _Two 1-1534 3-CHF _Two O-Ph 4-Pyr 4-Pym-CH _Two 1-1535 3-CHF _Two O-Ph 4-Pyr 5-Pym-CH _Two 1-1536 3-CHF _Two O-Ph 4-Pyr 2-Pym-CH _Two 1-1537 3-Cl-4-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 1-1538 3-Cl-4-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 1-1539 3-Cl-4-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 1-1540 3-Cl-4-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 1-1541 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 1-1542 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 1-1543 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 1-1544 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 1-1545 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 1-1546 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 1-1547 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-1548 3-Cl-4-F-Ph 2-NH _Two -4-Pym 3-Azt 1-1549 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 1-1550 3-Cl-4-F-Ph 2-NH _Two -4-Pym 3-Pyrd 1-1551 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 1-1552 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Pip 1-1553 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 1-1554 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 1-1555 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 1-1556 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Piz 1-1557 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 1-1558 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Pyr 1-1559 3-Cl-4-F-Ph 2-NH _Two -4-Pym 3-Pyr 1-1560 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Pym 1-1561 3-Cl-4-F-Ph 2-NH _Two -4-Pym 5-Pym 1-1562 3-Cl-4-F-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 1-1563 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 1-1564 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 1-1565 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 1-1566 3-Cl-4-F-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 1-1567 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 1-1568 3-Cl-4-F-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 1-1569 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 1-1570 3-Cl-4-F-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 1-1571 3-Cl-4-F-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 1-1572 3,4,5-triF-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 1-1573 3,4,5-triF-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 1-1574 3,4,5-triF-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 1-1575 3,4,5-triF-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 1-1576 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 1-1577 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 1-1578 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 1-1579 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 1-1580 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 1-1581 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 1-1582 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-1583 3,4,5-triF-Ph 2-NH _Two -4-Pym 3-Azt 1-1584 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 1-1585 3,4,5-triF-Ph 2-NH _Two -4-Pym 3-Pyrd 1-1586 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 1-1587 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Pip 1-1588 3,4,5-triF-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 1-1589 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 1-1590 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 1-1591 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Piz 1-1592 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 1-1593 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Pyr 1-1594 3,4,5-triF-Ph 2-NH _Two -4-Pym 3-Pyr 1-1595 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Pym 1-1596 3,4,5-triF-Ph 2-NH _Two -4-Pym 5-Pym 1-1597 3,4,5-triF-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 1-1598 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 1-1599 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 1-1600 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 1-1601 3,4,5-triF-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 1-1602 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 1-1603 3,4,5-triF-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 1-1604 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 1-1605 3,4,5-triF-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 1-1606 3,4,5-triF-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 1-1607 3-CF _Three -Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 1-1608 3-CF _Three -Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 1-1609 3-CF _Three -Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 1-1610 3-CF _Three -Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 1-1611 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 1-1612 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 1-1613 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 1-1614 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 1-1615 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 1-1616 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 1-1617 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-1618 3-CF _Three -Ph 2-NH _Two -4-Pym 3-Azt 1-1619 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Me-3-Azt 1-1620 3-CF _Three -Ph 2-NH _Two -4-Pym 3-Pyrd 1-1621 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 1-1622 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Pip 1-1623 3-CF _Three -Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 1-1624 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Me-4-Pip 1-1625 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 1-1626 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Piz 1-1627 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Me-1-Piz 1-1628 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Pyr 1-1629 3-CF _Three -Ph 2-NH _Two -4-Pym 3-Pyr 1-1630 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Pym 1-1631 3-CF _Three -Ph 2-NH _Two -4-Pym 5-Pym 1-1632 3-CF _Three -Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 1-1633 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 1-1634 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 1-1635 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 1-1636 3-CF _Three -Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 1-1637 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 1-1638 3-CF _Three -Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 1-1639 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 1-1640 3-CF _Three -Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 1-1641 3-CF _Three -Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 1-1642 3-CHF _Two O-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 1-1643 3-CHF _Two O-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 1-1644 3-CHF _Two O-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 1-1645 3-CHF _Two O-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 1-1646 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 1-1647 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 1-1648 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 1-1649 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 1-1650 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 1-1651 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 1-1652 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-1653 3-CHF _Two O-Ph 2-NH _Two -4-Pym 3-Azt 1-1654 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 1-1655 3-CHF _Two O-Ph 2-NH _Two -4-Pym 3-Pyrd 1-1656 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 1-1657 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Pip 1-1658 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 1-1659 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 1-1660 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 1-1661 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Piz 1-1662 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 1-1663 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Pyr 1-1664 3-CHF _Two O-Ph 2-NH _Two -4-Pym 3-Pyr 1-1665 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Pym 1-1666 3-CHF _Two O-Ph 2-NH _Two -4-Pym 5-Pym 1-1667 3-CHF _Two O-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 1-1668 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 1-1669 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 1-1670 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 1-1671 3-CHF _Two O-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 1-1672 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 1-1673 3-CHF _Two O-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 1-1674 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 1-1675 3-CHF _Two O-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 1-1676 3-CHF _Two O-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 1-1677 3-Cl-4-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 1-1678 3-Cl-4-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 1-1679 3-Cl-4-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 1-1680 3-Cl-4-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 1-1681 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 1-1682 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 1-1683 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 1-1684 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 1-1685 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 1-1686 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 1-1687 3-Cl-4-F-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-1688 3-Cl-4-F-Ph 2-MeNH-4-Pym 3-Azt 1-1689 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Me-3-Azt 1- 1690 3-Cl-4-F-Ph 2-MeNH-4-Pym 3-Pyrd 1-1691 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd 1-1692 3 -Cl-4-F-Ph 2-MeNH-4-Pym 4-Pip 1-1693 3-Cl-4-F-Ph 2-MeNH-4-Pym 4- (3,4-deH-Pip) 1- 1694 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Me-4-Pip 1-1695 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Me-4- ( (1,3-deH-Pip) 1-1696 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Piz 1-1697 3-Cl-4-F-Ph 2-MeNH-4-Pym 4 -Me-1-Piz 1-1698 3-Cl-4-F-Ph 2-MeNH-4-Pym 4-Pyr 1-1699 3-Cl-4-F-Ph 2-MeNH-4-Pym 3-Pyr 1-1700 3-Cl-4-F-Ph 2-MeNH-4-Pym 4-Pym 1-1701 3-Cl-4-F-Ph 2-MeNH-4-Pym 5-Pym 1-1702 3-Cl -4-F-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 1-1703 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 1-1704 3-Cl-4-F-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 1-1705 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 1-1706 3-Cl-4-F-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 1-1707 3-Cl-4-F-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 1-1708 3-Cl-4-F-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 1-1709 3-Cl-4-F-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 1-1710 3-Cl-4-F-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 1-1711 3-Cl-4-F-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 1-1712 3,4,5-triF-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 1-1713 3,4,5-triF-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 1-1714 3,4,5-triF-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 1-1715 3,4,5-triF-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 1-1716 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 1-1717 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 1-1718 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 1-1719 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 1-1720 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 1-1721 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 1-1722 3,4,5-triF-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-1723 3,4,5-triF-Ph 2-MeNH-4-Pym 3-Azt 1-1724 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Me-3-Azt 1- 1725 3,4,5-triF-Ph 2-MeNH-4-Pym 3-Pyrd 1-1726 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd 1-1727 3 , 4,5-triF-Ph 2-MeNH-4-Pym 4-Pip 1-1728 3,4,5-triF-Ph 2-MeNH-4-Pym 4- (3,4-deH-Pip) 1- 1729 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Me-4-Pip 1-1730 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Me-4- ( 3,4-deH-Pip) 1-1731 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Piz 1-1732 3,4,5-triF-Ph 2-MeNH-4-Pym 4 -Me-1-Piz 1-1733 3,4,5-triF-Ph 2-MeNH-4-Pym 4-Pyr 1-1734 3,4,5-triF-Ph 2-MeNH-4-Pym 3-Pyr 1-1735 3,4,5-triF-Ph 2-MeNH-4-Pym 4-Pym 1-1736 3,4,5-triF-Ph 2-MeNH-4-Pym 5-Pym 1-1737 3,4 , 5-triF-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 1-1738 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 1-1739 3,4,5-triF-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 1-1740 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 1-1741 3,4,5-triF-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 1-1742 3,4,5-triF-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 1-1743 3,4,5-triF-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 1-1744 3,4,5-triF-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 1-1745 3,4,5-triF-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 1-1746 3,4,5-triF-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 1-1747 3-CF _Three -Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 1-1748 3-CF _Three -Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 1-1749 3-CF _Three -Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 1-1750 3-CF _Three -Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 1-1751 3-CF _Three -Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 1-1752 3-CF _Three -Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 1-1753 3-CF _Three -Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 1-1754 3-CF _Three -Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 1-1755 3-CF _Three -Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 1-1756 3-CF _Three -Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 1-1757 3-CF _Three -Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-1758 3-CF _Three -Ph 2-MeNH-4-Pym 3-Azt 1-1759 3-CF _Three -Ph 2-MeNH-4-Pym 1-Me-3-Azt 1-1760 3-CF _Three -Ph 2-MeNH-4-Pym 3-Pyrd 1-1761 3-CF _Three -Ph 2-MeNH-4-Pym 1-Me-3-Pyrd 1-1762 3-CF _Three -Ph 2-MeNH-4-Pym 4-Pip 1-1763 3-CF _Three -Ph 2-MeNH-4-Pym 4- (3,4-deH-Pip) 1-1764 3-CF _Three -Ph 2-MeNH-4-Pym 1-Me-4-Pip 1-1765 3-CF _Three -Ph 2-MeNH-4-Pym 1-Me-4- (3,4-deH-Pip) 1-1766 3-CF _Three -Ph 2-MeNH-4-Pym 1-Piz 1-1767 3-CF _Three -Ph 2-MeNH-4-Pym 4-Me-1-Piz 1-1768 3-CF _Three -Ph 2-MeNH-4-Pym 4-Pyr 1-1769 3-CF _Three -Ph 2-MeNH-4-Pym 3-Pyr 1-1770 3-CF _Three -Ph 2-MeNH-4-Pym 4-Pym 1-1771 3-CF _Three -Ph 2-MeNH-4-Pym 5-Pym 1-1772 3-CF _Three -Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 1-1773 3-CF _Three -Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 1-1774 3-CF _Three -Ph 2-MeNH-4-Pym 4-Pip-CH _Two 1-1775 3-CF _Three -Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 1-1776 3-CF _Three -Ph 2-MeNH-4-Pym 2-Piz-CH _Two 1-1777 3-CF _Three -Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 1-1778 3-CF _Three -Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 1-1779 3-CF _Three -Ph 2-MeNH-4-Pym 4-Pym-CH _Two 1-1780 3-CF _Three -Ph 2-MeNH-4-Pym 5-Pym-CH _Two 1-1781 3-CF _Three -Ph 2-MeNH-4-Pym 2-Pym-CH _Two 1-1782 3-CHF _Two O-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 1-1783 3-CHF _Two O-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 1-1784 3-CHF _Two O-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 1-1785 3-CHF _Two O-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 1-1786 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 1-1787 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 1-1788 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 1-1789 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 1-1790 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 1-1791 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 1-1792 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-1793 3-CHF _Two O-Ph 2-MeNH-4-Pym 3-Azt 1-1794 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Me-3-Azt 1-1795 3-CHF _Two O-Ph 2-MeNH-4-Pym 3-Pyrd 1-1796 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd 1-1797 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Pip 1-1798 3-CHF _Two O-Ph 2-MeNH-4-Pym 4- (3,4-deH-Pip) 1-1799 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Me-4-Pip 1-1800 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Me-4- (3,4-deH-Pip) 1-1801 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Piz 1-1802 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Me-1-Piz 1-1803 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Pyr 1-1804 3-CHF _Two O-Ph 2-MeNH-4-Pym 3-Pyr 1-1805 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Pym 1-1806 3-CHF _Two O-Ph 2-MeNH-4-Pym 5-Pym 1-1807 3-CHF _Two O-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 1-1808 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 1-1809 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 1-1810 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 1-1811 3-CHF _Two O-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 1-1812 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 1-1813 3-CHF _Two O-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 1-1814 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 1-1815 3-CHF _Two O-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 1-1816 3-CHF _Two O-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 1-1817 Ph 2-NH _Two -4-Pyr H _Two N- (CH _Two ) _Three 1-1818 Ph 2-NH _Two -4-Pyr MeNH- (CH _Two ) _Three 1-1819 Ph 2-NH _Two -4-Pyr EtNH- (CH _Two ) _Three 1-1820 Ph 2-NH _Two -4-Pyr Me _Two N- (CH _Two ) _Three 1-1821 Ph 2-NH _Two -4-Pyr 1-Azt- (CH _Two ) _Three 1-1822 Ph 2-NH _Two -4-Pyr 1-Pyrd- (CH _Two ) _Three 1-1823 Ph 2-NH _Two -4-Pyr 1-Pip- (CH _Two ) _Three 1-1824 Ph 2-NH _Two -4-Pyr 1-Mor- (CH _Two ) _Three 1-1825 Ph 2-NH _Two -4-Pyr 1-Tmor- (CH _Two ) _Three 1-1826 Ph 2-NH _Two -4-Pyr 1-Piz- (CH _Two ) _Three 1-1827 Ph 2-NH _Two -4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-1828 Ph 2-NH _Two -4-Pyr 3-Azt 1-1829 Ph 2-NH _Two -4-Pyr 1-Me-3-Azt 1-1830 Ph 2-NH _Two -4-Pyr 3-Pyrd 1-1831 Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd 1-1832 Ph 2-NH _Two -4-Pyr 4-Pip 1-1833 Ph 2-NH _Two -4-Pyr 4- (3,4-deH-Pip) 1-1834 Ph 2-NH _Two -4-Pyr 1-Me-4-Pip 1-1835 Ph 2-NH _Two -4-Pyr 1-Me-4- (3,4-deH-Pip) 1-1836 Ph 2-NH _Two -4-Pyr 1-Piz 1-1837 Ph 2-NH _Two -4-Pyr 4-Me-1-Piz 1-1838 Ph 2-NH _Two -4-Pyr 4-Pyr 1-1839 Ph 2-NH _Two -4-Pyr 3-Pyr 1-1840 Ph 2-NH _Two -4-Pyr 4-Pym 1-1841 Ph 2-NH _Two -4-Pyr 5-Pym 1-1842 Ph 2-NH _Two -4-Pyr 3-Pyrd-CH _Two 1-1843 Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd-CH _Two 1-1844 Ph 2-NH _Two -4-Pyr 4-Pip-CH _Two 1-1845 Ph 2-NH _Two -4-Pyr 1-Me-4-Pip-CH _Two 1-1846 Ph 2-NH _Two -4-Pyr 2-Piz-CH _Two 1-1847 Ph 2-NH _Two -4-Pyr 4-Pyr-CH _Two 1-1848 Ph 2-NH _Two -4-Pyr 3-Pyr-CH _Two 1-1849 Ph 2-NH _Two -4-Pyr 4-Pym-CH _Two 1-1850 Ph 2-NH _Two -4-Pyr 5-Pym-CH _Two 1-1851 Ph 2-NH _Two -4-Pyr 2-Pym-CH _Two 1-1852 4-F-Ph 2-NH _Two -4-Pyr H _Two N- (CH _Two ) _Three 1-1853 4-F-Ph 2-NH _Two -4-Pyr MeNH- (CH _Two ) _Three 1-1854 4-F-Ph 2-NH _Two -4-Pyr EtNH- (CH _Two ) _Three 1-1855 4-F-Ph 2-NH _Two -4-Pyr Me _Two N- (CH _Two ) _Three 1-1856 4-F-Ph 2-NH _Two -4-Pyr 1-Azt- (CH _Two ) _Three 1-1857 4-F-Ph 2-NH _Two -4-Pyr 1-Pyrd- (CH _Two ) _Three 1-1858 4-F-Ph 2-NH _Two -4-Pyr 1-Pip- (CH _Two ) _Three 1-1859 4-F-Ph 2-NH _Two -4-Pyr 1-Mor- (CH _Two ) _Three 1-1860 4-F-Ph 2-NH _Two -4-Pyr 1-Tmor- (CH _Two ) _Three 1-1861 4-F-Ph 2-NH _Two -4-Pyr 1-Piz- (CH _Two ) _Three 1-1862 4-F-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-1863 4-F-Ph 2-NH _Two -4-Pyr 3-Azt 1-1864 4-F-Ph 2-NH _Two -4-Pyr 1-Me-3-Azt 1-1865 4-F-Ph 2-NH _Two -4-Pyr 3-Pyrd 1-1866 4-F-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd 1-1867 4-F-Ph 2-NH _Two -4-Pyr 4-Pip 1-1868 4-F-Ph 2-NH _Two -4-Pyr 4- (3,4-deH-Pip) 1-1869 4-F-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip 1-1870 4-F-Ph 2-NH _Two -4-Pyr 1-Me-4- (3,4-deH-Pip) 1-1871 4-F-Ph 2-NH _Two -4-Pyr 1-Piz 1-1872 4-F-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz 1-1873 4-F-Ph 2-NH _Two -4-Pyr 4-Pyr 1-1874 4-F-Ph 2-NH _Two -4-Pyr 3-Pyr 1-1875 4-F-Ph 2-NH _Two -4-Pyr 4-Pym 1-1876 4-F-Ph 2-NH _Two -4-Pyr 5-Pym 1-1877 4-F-Ph 2-NH _Two -4-Pyr 3-Pyrd-CH _Two 1-1878 4-F-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd-CH _Two 1-1879 4-F-Ph 2-NH _Two -4-Pyr 4-Pip-CH _Two 1-1880 4-F-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip-CH _Two 1-1881 4-F-Ph 2-NH _Two -4-Pyr 2-Piz-CH _Two 1-1882 4-F-Ph 2-NH _Two -4-Pyr 4-Pyr-CH _Two 1-1883 4-F-Ph 2-NH _Two -4-Pyr 3-Pyr-CH _Two 1-1884 4-F-Ph 2-NH _Two -4-Pyr 4-Pym-CH _Two 1-1885 4-F-Ph 2-NH _Two -4-Pyr 5-Pym-CH _Two 1-1886 4-F-Ph 2-NH _Two -4-Pyr 2-Pym-CH _Two 1-1887 3-F-Ph 2-NH _Two -4-Pyr H _Two N- (CH _Two ) _Three 1-1888 3-F-Ph 2-NH _Two -4-Pyr MeNH- (CH _Two ) _Three 1-1889 3-F-Ph 2-NH _Two -4-Pyr EtNH- (CH _Two ) _Three 1-1890 3-F-Ph 2-NH _Two -4-Pyr Me _Two N- (CH _Two ) _Three 1-1891 3-F-Ph 2-NH _Two -4-Pyr 1-Azt- (CH _Two ) _Three 1-1892 3-F-Ph 2-NH _Two -4-Pyr 1-Pyrd- (CH _Two ) _Three 1-1893 3-F-Ph 2-NH _Two -4-Pyr 1-Pip- (CH _Two ) _Three 1-1894 3-F-Ph 2-NH _Two -4-Pyr 1-Mor- (CH _Two ) _Three 1-1895 3-F-Ph 2-NH _Two -4-Pyr 1-Tmor- (CH _Two ) _Three 1-1896 3-F-Ph 2-NH _Two -4-Pyr 1-Piz- (CH _Two ) _Three 1-1897 3-F-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-1898 3-F-Ph 2-NH _Two -4-Pyr 3-Azt 1-1899 3-F-Ph 2-NH _Two -4-Pyr 1-Me-3-Azt 1-1900 3-F-Ph 2-NH _Two -4-Pyr 3-Pyrd 1-1901 3-F-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd 1-1902 3-F-Ph 2-NH _Two -4-Pyr 4-Pip 1-1903 3-F-Ph 2-NH _Two -4-Pyr 4- (3,4-deH-Pip) 1-1904 3-F-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip 1-1905 3-F-Ph 2-NH _Two -4-Pyr 1-Me-4- (3,4-deH-Pip) 1-1906 3-F-Ph 2-NH _Two -4-Pyr 1-Piz 1-1907 3-F-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz 1-1908 3-F-Ph 2-NH _Two -4-Pyr 4-Pyr 1-1909 3-F-Ph 2-NH _Two -4-Pyr 3-Pyr 1-1910 3-F-Ph 2-NH _Two -4-Pyr 4-Pym 1-1911 3-F-Ph 2-NH _Two -4-Pyr 5-Pym 1-1912 3-F-Ph 2-NH _Two -4-Pyr 3-Pyrd-CH _Two 1-1913 3-F-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd-CH _Two 1-1914 3-F-Ph 2-NH _Two -4-Pyr 4-Pip-CH _Two 1-1915 3-F-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip-CH _Two 1-1916 3-F-Ph 2-NH _Two -4-Pyr 2-Piz-CH _Two 1-1917 3-F-Ph 2-NH _Two -4-Pyr 4-Pyr-CH _Two 1-1918 3-F-Ph 2-NH _Two -4-Pyr 3-Pyr-CH _Two 1-1919 3-F-Ph 2-NH _Two -4-Pyr 4-Pym-CH _Two 1-1920 3-F-Ph 2-NH _Two -4-Pyr 5-Pym-CH _Two 1-1921 3-F-Ph 2-NH _Two -4-Pyr 2-Pym-CH _Two 1-1922 3,4-diF-Ph 2-NH _Two -4-Pyr H _Two N- (CH _Two ) _Three 1-1923 3,4-diF-Ph 2-NH _Two -4-Pyr MeNH- (CH _Two ) _Three 1-1924 3,4-diF-Ph 2-NH _Two -4-Pyr EtNH- (CH _Two ) _Three 1-1925 3,4-diF-Ph 2-NH _Two -4-Pyr Me _Two N- (CH _Two ) _Three 1-1926 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Azt- (CH _Two ) _Three 1-1927 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Pyrd- (CH _Two ) _Three 1-1928 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Pip- (CH _Two ) _Three 1-1929 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Mor- (CH _Two ) _Three 1-1930 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Tmor- (CH _Two ) _Three 1-1931 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Piz- (CH _Two ) _Three 1-1932 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-1933 3,4-diF-Ph 2-NH _Two -4-Pyr 3-Azt 1-1934 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Me-3-Azt 1-1935 3,4-diF-Ph 2-NH _Two -4-Pyr 3-Pyrd 1-1936 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd 1-1937 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Pip 1-1938 3,4-diF-Ph 2-NH _Two -4-Pyr 4- (3,4-deH-Pip) 1-1939 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip 1-1940 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Me-4- (3,4-deH-Pip) 1-1941 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Piz 1-1942 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz 1-1943 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Pyr 1-1944 3,4-diF-Ph 2-NH _Two -4-Pyr 3-Pyr 1-1945 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Pym 1-1946 3,4-diF-Ph 2-NH _Two -4-Pyr 5-Pym 1-1947 3,4-diF-Ph 2-NH _Two -4-Pyr 3-Pyrd-CH _Two 1-1948 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd-CH _Two 1-1949 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Pip-CH _Two 1-1950 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip-CH _Two 1-1951 3,4-diF-Ph 2-NH _Two -4-Pyr 2-Piz-CH _Two 1-1952 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Pyr-CH _Two 1-1953 3,4-diF-Ph 2-NH _Two -4-Pyr 3-Pyr-CH _Two 1-1954 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Pym-CH _Two 1-1955 3,4-diF-Ph 2-NH _Two -4-Pyr 5-Pym-CH _Two 1-1956 3,4-diF-Ph 2-NH _Two -4-Pyr 2-Pym-CH _Two 1-1957 3-Cl-Ph 2-NH _Two -4-Pyr H _Two N- (CH _Two ) _Three 1-1958 3-Cl-Ph 2-NH _Two -4-Pyr MeNH- (CH _Two ) _Three 1-1959 3-Cl-Ph 2-NH _Two -4-Pyr EtNH- (CH _Two ) _Three 1-1960 3-Cl-Ph 2-NH _Two -4-Pyr Me _Two N- (CH _Two ) _Three 1-1961 3-Cl-Ph 2-NH _Two -4-Pyr 1-Azt- (CH _Two ) _Three 1-1962 3-Cl-Ph 2-NH _Two -4-Pyr 1-Pyrd- (CH _Two ) _Three 1-1963 3-Cl-Ph 2-NH _Two -4-Pyr 1-Pip- (CH _Two ) _Three 1-1964 3-Cl-Ph 2-NH _Two -4-Pyr 1-Mor- (CH _Two ) _Three 1-1965 3-Cl-Ph 2-NH _Two -4-Pyr 1-Tmor- (CH _Two ) _Three 1-1966 3-Cl-Ph 2-NH _Two -4-Pyr 1-Piz- (CH _Two ) _Three 1-1967 3-Cl-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-1968 3-Cl-Ph 2-NH _Two -4-Pyr 3-Azt 1-1969 3-Cl-Ph 2-NH _Two -4-Pyr 1-Me-3-Azt 1-1970 3-Cl-Ph 2-NH _Two -4-Pyr 3-Pyrd 1-1971 3-Cl-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd 1-1972 3-Cl-Ph 2-NH _Two -4-Pyr 4-Pip 1-1973 3-Cl-Ph 2-NH _Two -4-Pyr 4- (3,4-deH-Pip) 1-1974 3-Cl-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip 1-1975 3-Cl-Ph 2-NH _Two -4-Pyr 1-Me-4- (3,4-deH-Pip) 1-1976 3-Cl-Ph 2-NH _Two -4-Pyr 1-Piz 1-1977 3-Cl-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz 1-1978 3-Cl-Ph 2-NH _Two -4-Pyr 4-Pyr 1-1979 3-Cl-Ph 2-NH _Two -4-Pyr 3-Pyr 1-1980 3-Cl-Ph 2-NH _Two -4-Pyr 4-Pym 1-1981 3-Cl-Ph 2-NH _Two -4-Pyr 5-Pym 1-1982 3-Cl-Ph 2-NH _Two -4-Pyr 3-Pyrd-CH _Two 1-1983 3-Cl-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd-CH _Two 1-1984 3-Cl-Ph 2-NH _Two -4-Pyr 4-Pip-CH _Two 1-1985 3-Cl-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip-CH _Two 1-1986 3-Cl-Ph 2-NH _Two -4-Pyr 2-Piz-CH _Two 1-1987 3-Cl-Ph 2-NH _Two -4-Pyr 4-Pyr-CH _Two 1-1988 3-Cl-Ph 2-NH _Two -4-Pyr 3-Pyr-CH _Two 1-1989 3-Cl-Ph 2-NH _Two -4-Pyr 4-Pym-CH _Two 1-1990 3-Cl-Ph 2-NH _Two -4-Pyr 5-Pym-CH _Two 1-1991 3-Cl-Ph 2-NH _Two -4-Pyr 2-Pym-CH _Two 1-1992 Ph 2-MeNH-4-Pyr H _Two N- (CH _Two ) _Three 1-1993 Ph 2-MeNH-4-Pyr MeNH- (CH _Two ) _Three 1-1994 Ph 2-MeNH-4-Pyr EtNH- (CH _Two ) _Three 1-1995 Ph 2-MeNH-4-Pyr Me _Two N- (CH _Two ) _Three 1-1996 Ph 2-MeNH-4-Pyr 1-Azt- (CH _Two ) _Three 1-1997 Ph 2-MeNH-4-Pyr 1-Pyrd- (CH _Two ) _Three 1-1998 Ph 2-MeNH-4-Pyr 1-Pip- (CH _Two ) _Three 1-1999 Ph 2-MeNH-4-Pyr 1-Mor- (CH _Two ) _Three 1-2000 Ph 2-MeNH-4-Pyr 1-Tmor- (CH _Two ) _Three 1-2001 Ph 2-MeNH-4-Pyr 1-Piz- (CH _Two ) _Three 1-2002 Ph 2-MeNH-4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-2003 Ph 2-MeNH-4-Pyr 3-Azt 1-2004 Ph 2-MeNH-4-Pyr 1-Me-3-Azt 1-2005 Ph 2-MeNH-4-Pyr 3-Pyrd 1-2006 Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd 1-2007 Ph 2-MeNH-4-Pyr 4-Pip 1-2008 Ph 2-MeNH-4-Pyr 4- (3,4-deH-Pip) 1-2009 Ph 2-MeNH-4-Pyr 1-Me-4-Pip 1-2010 Ph 2-MeNH-4-Pyr 1-Me-4- (3,4-deH-Pip) 1-2011 Ph 2- MeNH-4-Pyr 1-Piz 1-2012 Ph 2-MeNH-4-Pyr 4-Me-1-Piz 1-2013 Ph 2-MeNH-4-Pyr 4-Pyr 1-2014 Ph 2-MeNH-4- Pyr 3-Pyr 1-2015 Ph 2-MeNH-4-Pyr 4-Pym 1-2016 Ph 2-MeNH-4-Pyr 5-Pym 1-2017 Ph 2-MeNH-4-Pyr 3-Pyrd-CH _Two 1-2018 Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd-CH _Two 1-2019 Ph 2-MeNH-4-Pyr 4-Pip-CH _Two 1-2020 Ph 2-MeNH-4-Pyr 1-Me-4-Pip-CH _Two 1-2021 Ph 2-MeNH-4-Pyr 2-Piz-CH _Two 1-2022 Ph 2-MeNH-4-Pyr 4-Pyr-CH _Two 1-2023 Ph 2-MeNH-4-Pyr 3-Pyr-CH _Two 1-2024 Ph 2-MeNH-4-Pyr 4-Pym-CH _Two 1-2025 Ph 2-MeNH-4-Pyr 5-Pym-CH _Two 1-2026 Ph 2-MeNH-4-Pyr 2-Pym-CH _Two 1-2027 4-F-Ph 2-MeNH-4-Pyr H _Two N- (CH _Two ) _Three 1-2028 4-F-Ph 2-MeNH-4-Pyr MeNH- (CH _Two ) _Three 1-2029 4-F-Ph 2-MeNH-4-Pyr EtNH- (CH _Two ) _Three 1-2030 4-F-Ph 2-MeNH-4-Pyr Me _Two N- (CH _Two ) _Three 1-2031 4-F-Ph 2-MeNH-4-Pyr 1-Azt- (CH _Two ) _Three 1-2032 4-F-Ph 2-MeNH-4-Pyr 1-Pyrd- (CH _Two ) _Three 1-2033 4-F-Ph 2-MeNH-4-Pyr 1-Pip- (CH _Two ) _Three 1-2034 4-F-Ph 2-MeNH-4-Pyr 1-Mor- (CH _Two ) _Three 1-2035 4-F-Ph 2-MeNH-4-Pyr 1-Tmor- (CH _Two ) _Three 1-2036 4-F-Ph 2-MeNH-4-Pyr 1-Piz- (CH _Two ) _Three 1-2037 4-F-Ph 2-MeNH-4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-2038 4-F-Ph 2-MeNH-4-Pyr 3-Azt 1-2039 4-F-Ph 2-MeNH-4-Pyr 1-Me-3-Azt 1-2040 4-F-Ph 2- MeNH-4-Pyr 3-Pyrd 1-2041 4-F-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd 1-2042 4-F-Ph 2-MeNH-4-Pyr 4-Pip 1- 2043 4-F-Ph 2-MeNH-4-Pyr 4- (3,4-deH-Pip) 1-2044 4-F-Ph 2-MeNH-4-Pyr 1-Me-4-Pip 1-2045 4 -F-Ph 2-MeNH-4-Pyr 1-Me-4- (3,4-deH-Pip) 1-2046 4-F-Ph 2-MeNH-4-Pyr 1-Piz 1-2047 4-F -Ph 2-MeNH-4-Pyr 4-Me-1-Piz 1-2048 4-F-Ph 2-MeNH-4-Pyr 4-Pyr 1-2049 4-F-Ph 2-MeNH-4-Pyr 3 -Pyr 1-2050 4-F-Ph 2-MeNH-4-Pyr 4-Pym 1-2051 4-F-Ph 2-MeNH-4-Pyr 5-Pym 1-2052 4-F-Ph 2-MeNH- 4-Pyr 3-Pyrd-CH _Two 1-2053 4-F-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd-CH _Two 1-2054 4-F-Ph 2-MeNH-4-Pyr 4-Pip-CH _Two 1-2055 4-F-Ph 2-MeNH-4-Pyr 1-Me-4-Pip-CH _Two 1-2056 4-F-Ph 2-MeNH-4-Pyr 2-Piz-CH _Two 1-2057 4-F-Ph 2-MeNH-4-Pyr 4-Pyr-CH _Two 1-2058 4-F-Ph 2-MeNH-4-Pyr 3-Pyr-CH _Two 1-2059 4-F-Ph 2-MeNH-4-Pyr 4-Pym-CH _Two 1-2060 4-F-Ph 2-MeNH-4-Pyr 5-Pym-CH _Two 1-2061 4-F-Ph 2-MeNH-4-Pyr 2-Pym-CH _Two 1-2062 3-F-Ph 2-MeNH-4-Pyr H _Two N- (CH _Two ) _Three 1-2063 3-F-Ph 2-MeNH-4-Pyr MeNH- (CH _Two ) _Three 1-2064 3-F-Ph 2-MeNH-4-Pyr EtNH- (CH _Two ) _Three 1-2065 3-F-Ph 2-MeNH-4-Pyr Me _Two N- (CH _Two ) _Three 1-2066 3-F-Ph 2-MeNH-4-Pyr 1-Azt- (CH _Two ) _Three 1-2067 3-F-Ph 2-MeNH-4-Pyr 1-Pyrd- (CH _Two ) _Three 1-2068 3-F-Ph 2-MeNH-4-Pyr 1-Pip- (CH _Two ) _Three 1-2069 3-F-Ph 2-MeNH-4-Pyr 1-Mor- (CH _Two ) _Three 1-2070 3-F-Ph 2-MeNH-4-Pyr 1-Tmor- (CH _Two ) _Three 1-2071 3-F-Ph 2-MeNH-4-Pyr 1-Piz- (CH _Two ) _Three 1-2072 3-F-Ph 2-MeNH-4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-2073 3-F-Ph 2-MeNH-4-Pyr 3-Azt 1-2074 3-F-Ph 2-MeNH-4-Pyr 1-Me-3-Azt 1-2075 3-F-Ph 2- MeNH-4-Pyr 3-Pyrd 1-2076 3-F-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd 1-2077 3-F-Ph 2-MeNH-4-Pyr 4-Pip 1- 2078 3-F-Ph 2-MeNH-4-Pyr 4- (3,4-deH-Pip) 1-2079 3-F-Ph 2-MeNH-4-Pyr 1-Me-4-Pip 1-2080 3 -F-Ph 2-MeNH-4-Pyr 1-Me-4- (3,4-deH-Pip) 1-2081 3-F-Ph 2-MeNH-4-Pyr 1-Piz 1-2082 3-F -Ph 2-MeNH-4-Pyr 4-Me-1-Piz 1-2083 3-F-Ph 2-MeNH-4-Pyr 4-Pyr 1-2084 3-F-Ph 2-MeNH-4-Pyr 3 -Pyr 1-2085 3-F-Ph 2-MeNH-4-Pyr 4-Pym 1-2086 3-F-Ph 2-MeNH-4-Pyr 5-Pym 1-2087 3-F-Ph 2-MeNH- 4-Pyr 3-Pyrd-CH _Two 1-2088 3-F-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd-CH _Two 1-2089 3-F-Ph 2-MeNH-4-Pyr 4-Pip-CH _Two 1-2090 3-F-Ph 2-MeNH-4-Pyr 1-Me-4-Pip-CH _Two 1-2091 3-F-Ph 2-MeNH-4-Pyr 2-Piz-CH _Two 1-2092 3-F-Ph 2-MeNH-4-Pyr 4-Pyr-CH _Two 1-2093 3-F-Ph 2-MeNH-4-Pyr 3-Pyr-CH _Two 1-2094 3-F-Ph 2-MeNH-4-Pyr 4-Pym-CH _Two 1-2095 3-F-Ph 2-MeNH-4-Pyr 5-Pym-CH _Two 1-2096 3-F-Ph 2-MeNH-4-Pyr 2-Pym-CH _Two 1-2097 3,4-diF-Ph 2-MeNH-4-Pyr H _Two N- (CH _Two ) _Three 1-2098 3,4-diF-Ph 2-MeNH-4-Pyr MeNH- (CH _Two ) _Three 1-2099 3,4-diF-Ph 2-MeNH-4-Pyr EtNH- (CH _Two ) _Three 1-2100 3,4-diF-Ph 2-MeNH-4-Pyr Me _Two N- (CH _Two ) _Three 1-2101 3,4-diF-Ph 2-MeNH-4-Pyr 1-Azt- (CH _Two ) _Three 1-2102 3,4-diF-Ph 2-MeNH-4-Pyr 1-Pyrd- (CH _Two ) _Three 1-2103 3,4-diF-Ph 2-MeNH-4-Pyr 1-Pip- (CH _Two ) _Three 1-2104 3,4-diF-Ph 2-MeNH-4-Pyr 1-Mor- (CH _Two ) _Three 1-2105 3,4-diF-Ph 2-MeNH-4-Pyr 1-Tmor- (CH _Two ) _Three 1-2106 3,4-diF-Ph 2-MeNH-4-Pyr 1-Piz- (CH _Two ) _Three 1-2107 3,4-diF-Ph 2-MeNH-4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-2108 3,4-diF-Ph 2-MeNH-4-Pyr 3-Azt 1-2109 3,4-diF-Ph 2-MeNH-4-Pyr 1-Me-3-Azt 1-2110 3,4 -diF-Ph 2-MeNH-4-Pyr 3-Pyrd 1-2111 3,4-diF-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd 1-2112 3,4-diF-Ph 2- MeNH-4-Pyr 4-Pip 1-2113 3,4-diF-Ph 2-MeNH-4-Pyr 4- (3,4-deH-Pip) 1-2114 3,4-diF-Ph 2-MeNH- 4-Pyr 1-Me-4-Pip 1-2115 3,4-diF-Ph 2-MeNH-4-Pyr 1-Me-4- (3,4-deH-Pip) 1-2116 3,4-diF -Ph 2-MeNH-4-Pyr 1-Piz 1-2117 3,4-diF-Ph 2-MeNH-4-Pyr 4-Me-1-Piz 1-2118 3,4-diF-Ph 2-MeNH- 4-Pyr 4-Pyr 1-2119 3,4-diF-Ph 2-MeNH-4-Pyr 3-Pyr 1-2120 3,4-diF-Ph 2-MeNH-4-Pyr 4-Pym 1-2121 3 , 4-diF-Ph 2-MeNH-4-Pyr 5-Pym 1-2122 3,4-diF-Ph 2-MeNH-4-Pyr 3-Pyrd-CH _Two 1-2123 3,4-diF-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd-CH _Two 1-2124 3,4-diF-Ph 2-MeNH-4-Pyr 4-Pip-CH _Two 1-2125 3,4-diF-Ph 2-MeNH-4-Pyr 1-Me-4-Pip-CH _Two 1-2126 3,4-diF-Ph 2-MeNH-4-Pyr 2-Piz-CH _Two 1-2127 3,4-diF-Ph 2-MeNH-4-Pyr 4-Pyr-CH _Two 1-2128 3,4-diF-Ph 2-MeNH-4-Pyr 3-Pyr-CH _Two 1-2129 3,4-diF-Ph 2-MeNH-4-Pyr 4-Pym-CH _Two 1-2130 3,4-diF-Ph 2-MeNH-4-Pyr 5-Pym-CH _Two 1-2131 3,4-diF-Ph 2-MeNH-4-Pyr 2-Pym-CH _Two 1-2132 3-Cl-Ph 2-MeNH-4-Pyr H _Two N- (CH _Two ) _Three 1-2133 3-Cl-Ph 2-MeNH-4-Pyr MeNH- (CH _Two ) _Three 1-2134 3-Cl-Ph 2-MeNH-4-Pyr EtNH- (CH _Two ) _Three 1-2135 3-Cl-Ph 2-MeNH-4-Pyr Me _Two N- (CH _Two ) _Three 1-2136 3-Cl-Ph 2-MeNH-4-Pyr 1-Azt- (CH _Two ) _Three 1-2137 3-Cl-Ph 2-MeNH-4-Pyr 1-Pyrd- (CH _Two ) _Three 1-2138 3-Cl-Ph 2-MeNH-4-Pyr 1-Pip- (CH _Two ) _Three 1-2139 3-Cl-Ph 2-MeNH-4-Pyr 1-Mor- (CH _Two ) _Three 1-2140 3-Cl-Ph 2-MeNH-4-Pyr 1-Tmor- (CH _Two ) _Three 1-2141 3-Cl-Ph 2-MeNH-4-Pyr 1-Piz- (CH _Two ) _Three 1-2142 3-Cl-Ph 2-MeNH-4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 1-2143 3-Cl-Ph 2-MeNH-4-Pyr 3-Azt 1-2144 3-Cl-Ph 2-MeNH-4-Pyr 1-Me-3-Azt 1-2145 3-Cl-Ph 2- MeNH-4-Pyr 3-Pyrd 1-2146 3-Cl-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd 1-2147 3-Cl-Ph 2-MeNH-4-Pyr 4-Pip 1- 2148 3-Cl-Ph 2-MeNH-4-Pyr 4- (3,4-deH-Pip) 1-2149 3-Cl-Ph 2-MeNH-4-Pyr 1-Me-4-Pip 1-2150 3 -Cl-Ph 2-MeNH-4-Pyr 1-Me-4- (3,4-deH-Pip) 1-2151 3-Cl-Ph 2-MeNH-4-Pyr 1-Piz 1-2152 3-Cl -Ph 2-MeNH-4-Pyr 4-Me-1-Piz 1-2153 3-Cl-Ph 2-MeNH-4-Pyr 4-Pyr 1-2154 3-Cl-Ph 2-MeNH-4-Pyr 3 -Pyr 1-2155 3-Cl-Ph 2-MeNH-4-Pyr 4-Pym 1-2156 3-Cl-Ph 2-MeNH-4-Pyr 5-Pym 1-2157 3-Cl-Ph 2-MeNH- 4-Pyr 3-Pyrd-CH _Two 1-2158 3-Cl-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd-CH _Two 1-2159 3-Cl-Ph 2-MeNH-4-Pyr 4-Pip-CH _Two 1-2160 3-Cl-Ph 2-MeNH-4-Pyr 1-Me-4-Pip-CH _Two 1-2161 3-Cl-Ph 2-MeNH-4-Pyr 2-Piz-CH _Two 1-2162 3-Cl-Ph 2-MeNH-4-Pyr 4-Pyr-CH _Two 1-2163 3-Cl-Ph 2-MeNH-4-Pyr 3-Pyr-CH _Two 1-2164 3-Cl-Ph 2-MeNH-4-Pyr 4-Pym-CH _Two 1-2165 3-Cl-Ph 2-MeNH-4-Pyr 5-Pym-CH _Two 1-2166 3-Cl-Ph 2-MeNH-4-Pyr 2-Pym-CH _Two 1-2167 Ph 4-Pym H _Two N- (CH _Two ) _Three 1-2168 Ph 4-Pym MeNH- (CH _Two ) _Three 1-2169 Ph 4-Pym EtNH- (CH _Two ) _Three 1-2170 Ph 4-Pym Me _Two N- (CH _Two ) _Three 1-2171 Ph 4-Pym 1-Azt- (CH _Two ) _Three 1-2172 Ph 4-Pym 1-Pyrd- (CH _Two ) _Three 1-2173 Ph 4-Pym 1-Pip- (CH _Two ) _Three 1-2174 Ph 4-Pym 1-Mor- (CH _Two ) _Three 1-2175 Ph 4-Pym 1-Tmor- (CH _Two ) _Three 1-2176 Ph 4-Pym 1-Piz- (CH _Two ) _Three 1-2177 Ph 4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-2178 Ph 4-Pym 3-Azt 1-2179 Ph 4-Pym 1-Me-3-Azt 1-2180 Ph 4-Pym 3-Pyrd 1-2181 Ph 4-Pym 1-Me-3-Pyrd 1- 2182 Ph 4-Pym 4-Pip 1-2183 Ph 4-Pym 4- (3,4-deH-Pip) 1-2184 Ph 4-Pym 1-Me-4-Pip 1-2185 Ph 4-Pym 1-Me -4- (3,4-deH-Pip) 1-2186 Ph 4-Pym 1-Piz 1-2187 Ph 4-Pym 4-Me-1-Piz 1-2188 Ph 4-Pym 4-Pyr 1-2189 Ph 4-Pym 3-Pyr 1-2190 Ph 4-Pym 4-Pym 1-2191 Ph 4-Pym 5-Pym 1-2192 Ph 4-Pym 3-Pyrd-CH _Two 1-2193 Ph 4-Pym 1-Me-3-Pyrd-CH _Two 1-2194 Ph 4-Pym 4-Pip-CH _Two 1-2195 Ph 4-Pym 1-Me-4-Pip-CH _Two 1-2196 Ph 4-Pym 2-Piz-CH _Two 1-2197 Ph 4-Pym 4-Pyr-CH _Two 1-2198 Ph 4-Pym 3-Pyr-CH _Two 1-2199 Ph 4-Pym 4-Pym-CH _Two 1-2200 Ph 4-Pym 5-Pym-CH _Two 1-2201 Ph 4-Pym 2-Pym-CH _Two 1-2202 4-F-Ph 4-Pym H _Two N- (CH _Two ) _Three 1-2203 4-F-Ph 4-Pym MeNH- (CH _Two ) _Three 1-2204 4-F-Ph 4-Pym EtNH- (CH _Two ) _Three 1-2205 4-F-Ph 4-Pym Me _Two N- (CH _Two ) _Three 1-2206 4-F-Ph 4-Pym 1-Azt- (CH _Two ) _Three 1-2207 4-F-Ph 4-Pym 1-Pyrd- (CH _Two ) _Three 1-2208 4-F-Ph 4-Pym 1-Pip- (CH _Two ) _Three 1-2209 4-F-Ph 4-Pym 1-Mor- (CH _Two ) _Three 1-2210 4-F-Ph 4-Pym 1-Tmor- (CH _Two ) _Three 1-2211 4-F-Ph 4-Pym 1-Piz- (CH _Two ) _Three 1-2212 4-F-Ph 4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-2213 4-F-Ph 4-Pym 3-Azt 1-2214 4-F-Ph 4-Pym 1-Me-3-Azt 1-2215 4-F-Ph 4-Pym 3-Pyrd 1-2216 4 -F-Ph 4-Pym 1-Me-3-Pyrd 1-2217 4-F-Ph 4-Pym 4-Pip 1-2218 4-F-Ph 4-Pym 4- (3,4-deH-Pip) 1-2219 4-F-Ph 4-Pym 1-Me-4-Pip 1-2220 4-F-Ph 4-Pym 1-Me-4- (3,4-deH-Pip) 1-2221 4-F -Ph 4-Pym 1-Piz 1-2222 4-F-Ph 4-Pym 4-Me-1-Piz 1-2223 4-F-Ph 4-Pym 4-Pyr 1-2224 4-F-Ph 4- Pym 3-Pyr 1-2225 4-F-Ph 4-Pym 4-Pym 1-2226 4-F-Ph 4-Pym 5-Pym 1-2227 4-F-Ph 4-Pym 3-Pyrd-CH _Two 1-2228 4-F-Ph 4-Pym 1-Me-3-Pyrd-CH _Two 1-2229 4-F-Ph 4-Pym 4-Pip-CH _Two 1-2230 4-F-Ph 4-Pym 1-Me-4-Pip-CH _Two 1-2231 4-F-Ph 4-Pym 2-Piz-CH _Two 1-2232 4-F-Ph 4-Pym 4-Pyr-CH _Two 1-2233 4-F-Ph 4-Pym 3-Pyr-CH _Two 1-2234 4-F-Ph 4-Pym 4-Pym-CH _Two 1-2235 4-F-Ph 4-Pym 5-Pym-CH _Two 1-2236 4-F-Ph 4-Pym 2-Pym-CH _Two 1-2237 3-F-Ph 4-Pym H _Two N- (CH _Two ) _Three 1-2238 3-F-Ph 4-Pym MeNH- (CH _Two ) _Three 1-2239 3-F-Ph 4-Pym EtNH- (CH _Two ) _Three 1-2240 3-F-Ph 4-Pym Me _Two N- (CH _Two ) _Three 1-2241 3-F-Ph 4-Pym 1-Azt- (CH _Two ) _Three 1-2242 3-F-Ph 4-Pym 1-Pyrd- (CH _Two ) _Three 1-2243 3-F-Ph 4-Pym 1-Pip- (CH _Two ) _Three 1-2244 3-F-Ph 4-Pym 1-Mor- (CH _Two ) _Three 1-2245 3-F-Ph 4-Pym 1-Tmor- (CH _Two ) _Three 1-2246 3-F-Ph 4-Pym 1-Piz- (CH _Two ) _Three 1-2247 3-F-Ph 4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-2248 3-F-Ph 4-Pym 3-Azt 1-2249 3-F-Ph 4-Pym 1-Me-3-Azt 1-2250 3-F-Ph 4-Pym 3-Pyrd 1-2251 3 -F-Ph 4-Pym 1-Me-3-Pyrd 1-2252 3-F-Ph 4-Pym 4-Pip 1-2253 3-F-Ph 4-Pym 4- (3,4-deH-Pip) 1-2254 3-F-Ph 4-Pym 1-Me-4-Pip 1-2255 3-F-Ph 4-Pym 1-Me-4- (3,4-deH-Pip) 1-2256 3-F -Ph 4-Pym 1-Piz 1-2257 3-F-Ph 4-Pym 4-Me-1-Piz 1-2258 3-F-Ph 4-Pym 4-Pyr 1-2259 3-F-Ph 4- Pym 3-Pyr 1-2260 3-F-Ph 4-Pym 4-Pym 1-2261 3-F-Ph 4-Pym 5-Pym 1-2262 3-F-Ph 4-Pym 3-Pyrd-CH _Two 1-2263 3-F-Ph 4-Pym 1-Me-3-Pyrd-CH _Two 1-2264 3-F-Ph 4-Pym 4-Pip-CH _Two 1-2265 3-F-Ph 4-Pym 1-Me-4-Pip-CH _Two 1-2266 3-F-Ph 4-Pym 2-Piz-CH _Two 1-2267 3-F-Ph 4-Pym 4-Pyr-CH _Two 1-2268 3-F-Ph 4-Pym 3-Pyr-CH _Two 1-2269 3-F-Ph 4-Pym 4-Pym-CH _Two 1-2270 3-F-Ph 4-Pym 5-Pym-CH _Two 1-2271 3-F-Ph 4-Pym 2-Pym-CH _Two 1-2272 3,4-diF-Ph 4-Pym H _Two N- (CH _Two ) _Three 1-2273 3,4-diF-Ph 4-Pym MeNH- (CH _Two ) _Three 1-2274 3,4-diF-Ph 4-Pym EtNH- (CH _Two ) _Three 1-2275 3,4-diF-Ph 4-Pym Me _Two N- (CH _Two ) _Three 1-2276 3,4-diF-Ph 4-Pym 1-Azt- (CH _Two ) _Three 1-2277 3,4-diF-Ph 4-Pym 1-Pyrd- (CH _Two ) _Three 1-2278 3,4-diF-Ph 4-Pym 1-Pip- (CH _Two ) _Three 1-2279 3,4-diF-Ph 4-Pym 1-Mor- (CH _Two ) _Three 1-2280 3,4-diF-Ph 4-Pym 1-Tmor- (CH _Two ) _Three 1-2281 3,4-diF-Ph 4-Pym 1-Piz- (CH _Two ) _Three 1-2282 3,4-diF-Ph 4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-2283 3,4-diF-Ph 4-Pym 3-Azt 1-2284 3,4-diF-Ph 4-Pym 1-Me-3-Azt 1-2285 3,4-diF-Ph 4-Pym 3 -Pyrd 1-2286 3,4-diF-Ph 4-Pym 1-Me-3-Pyrd 1-2287 3,4-diF-Ph 4-Pym 4-Pip 1-2288 3,4-diF-Ph 4- Pym 4- (3,4-deH-Pip) 1-2289 3,4-diF-Ph 4-Pym 1-Me-4-Pip 1-2290 3,4-diF-Ph 4-Pym 1-Me-4 -(3,4-deH-Pip) 1-2291 3,4-diF-Ph 4-Pym 1-Piz 1-2292 3,4-diF-Ph 4-Pym 4-Me-1-Piz 1-2293 3 , 4-diF-Ph 4-Pym 4-Pyr 1-2294 3,4-diF-Ph 4-Pym 3-Pyr 1-2295 3,4-diF-Ph 4-Pym 4-Pym 1-2296 3,4 -diF-Ph 4-Pym 5-Pym 1-2297 3,4-diF-Ph 4-Pym 3-Pyrd-CH _Two 1-2298 3,4-diF-Ph 4-Pym 1-Me-3-Pyrd-CH _Two 1-2299 3,4-diF-Ph 4-Pym 4-Pip-CH _Two 1-2300 3,4-diF-Ph 4-Pym 1-Me-4-Pip-CH _Two 1-2301 3,4-diF-Ph 4-Pym 2-Piz-CH _Two 1-2302 3,4-diF-Ph 4-Pym 4-Pyr-CH _Two 1-2303 3,4-diF-Ph 4-Pym 3-Pyr-CH _Two 1-2304 3,4-diF-Ph 4-Pym 4-Pym-CH _Two 1-2305 3,4-diF-Ph 4-Pym 5-Pym-CH _Two 1-2306 3,4-diF-Ph 4-Pym 2-Pym-CH _Two 1-2307 3-Cl-Ph 4-Pym H _Two N- (CH _Two ) _Three 1-2308 3-Cl-Ph 4-Pym MeNH- (CH _Two ) _Three 1-2309 3-Cl-Ph 4-Pym EtNH- (CH _Two ) _Three 1-2310 3-Cl-Ph 4-Pym Me _Two N- (CH _Two ) _Three 1-2311 3-Cl-Ph 4-Pym 1-Azt- (CH _Two ) _Three 1-2312 3-Cl-Ph 4-Pym 1-Pyrd- (CH _Two ) _Three 1-2313 3-Cl-Ph 4-Pym 1-Pip- (CH _Two ) _Three 1-2314 3-Cl-Ph 4-Pym 1-Mor- (CH _Two ) _Three 1-2315 3-Cl-Ph 4-Pym 1-Tmor- (CH _Two ) _Three 1-2316 3-Cl-Ph 4-Pym 1-Piz- (CH _Two ) _Three 1-2317 3-Cl-Ph 4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-2318 3-Cl-Ph 4-Pym 3-Azt 1-2319 3-Cl-Ph 4-Pym 1-Me-3-Azt 1-2320 3-Cl-Ph 4-Pym 3-Pyrd 1-2321 3 -Cl-Ph 4-Pym 1-Me-3-Pyrd 1-2322 3-Cl-Ph 4-Pym 4-Pip 1-2323 3-Cl-Ph 4-Pym 4- (3,4-deH-Pip) 1-2324 3-Cl-Ph 4-Pym 1-Me-4-Pip 1-2325 3-Cl-Ph 4-Pym 1-Me-4- (3,4-deH-Pip) 1-2326 3-Cl -Ph 4-Pym 1-Piz 1-2327 3-Cl-Ph 4-Pym 4-Me-1-Piz 1-2328 3-Cl-Ph 4-Pym 4-Pyr 1-2329 3-Cl-Ph 4- Pym 3-Pyr 1-2330 3-Cl-Ph 4-Pym 4-Pym 1-2331 3-Cl-Ph 4-Pym 5-Pym 1-2332 3-Cl-Ph 4-Pym 3-Pyrd-CH _Two 1-2333 3-Cl-Ph 4-Pym 1-Me-3-Pyrd-CH _Two 1-2334 3-Cl-Ph 4-Pym 4-Pip-CH _Two 1-2335 3-Cl-Ph 4-Pym 1-Me-4-Pip-CH _Two 1-2336 3-Cl-Ph 4-Pym 2-Piz-CH _Two 1-2337 3-Cl-Ph 4-Pym 4-Pyr-CH _Two 1-2338 3-Cl-Ph 4-Pym 3-Pyr-CH _Two 1-2339 3-Cl-Ph 4-Pym 4-Pym-CH _Two 1-2340 3-Cl-Ph 4-Pym 5-Pym-CH _Two 1-2341 3-Cl-Ph 4-Pym 2-Pym-CH _Two 1-2342 Ph 2-MeO-4-Pym H _Two N- (CH _Two ) _Three 1-2343 Ph 2-MeO-4-Pym MeNH- (CH _Two ) _Three 1-2344 Ph 2-MeO-4-Pym EtNH- (CH _Two ) _Three 1-2345 Ph 2-MeO-4-Pym Me _Two N- (CH _Two ) _Three 1-2346 Ph 2-MeO-4-Pym 1-Azt- (CH _Two ) _Three 1-2347 Ph 2-MeO-4-Pym 1-Pyrd- (CH _Two ) _Three 1-2348 Ph 2-MeO-4-Pym 1-Pip- (CH _Two ) _Three 1-2349 Ph 2-MeO-4-Pym 1-Mor- (CH _Two ) _Three 1-2350 Ph 2-MeO-4-Pym 1-Tmor- (CH _Two ) _Three 1-2351 Ph 2-MeO-4-Pym 1-Piz- (CH _Two ) _Three 1-2352 Ph 2-MeO-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-2353 Ph 2-MeO-4-Pym 3-Azt 1-2354 Ph 2-MeO-4-Pym 1-Me-3-Azt 1-2355 Ph 2-MeO-4-Pym 3-Pyrd 1-2356 Ph 2-MeO-4-Pym 1-Me-3-Pyrd 1-2357 Ph 2-MeO-4-Pym 4-Pip 1-2358 Ph 2-MeO-4-Pym 4- (3,4-deH-Pip) 1-2359 Ph 2-MeO-4-Pym 1-Me-4-Pip 1-2360 Ph 2-MeO-4-Pym 1-Me-4- (3,4-deH-Pip) 1-2361 Ph 2- MeO-4-Pym 1-Piz 1-2362 Ph 2-MeO-4-Pym 4-Me-1-Piz 1-2363 Ph 2-MeO-4-Pym 4-Pyr 1-2364 Ph 2-MeO-4- Pym 3-Pyr 1-2365 Ph 2-MeO-4-Pym 4-Pym 1-2366 Ph 2-MeO-4-Pym 5-Pym 1-2367 Ph 2-MeO-4-Pym 3-Pyrd-CH _Two 1-2368 Ph 2-MeO-4-Pym 1-Me-3-Pyrd-CH _Two 1-2369 Ph 2-MeO-4-Pym 4-Pip-CH _Two 1-2370 Ph 2-MeO-4-Pym 1-Me-4-Pip-CH _Two 1-2371 Ph 2-MeO-4-Pym 2-Piz-CH _Two 1-2372 Ph 2-MeO-4-Pym 4-Pyr-CH _Two 1-2373 Ph 2-MeO-4-Pym 3-Pyr-CH _Two 1-2374 Ph 2-MeO-4-Pym 4-Pym-CH _Two 1-2375 Ph 2-MeO-4-Pym 5-Pym-CH _Two 1-2376 Ph 2-MeO-4-Pym 2-Pym-CH _Two 1-2377 4-F-Ph 2-MeO-4-Pym H _Two N- (CH _Two ) _Three 1-2378 4-F-Ph 2-MeO-4-Pym MeNH- (CH _Two ) _Three 1-2379 4-F-Ph 2-MeO-4-Pym EtNH- (CH _Two ) _Three 1-2380 4-F-Ph 2-MeO-4-Pym Me _Two N- (CH _Two ) _Three 1-2381 4-F-Ph 2-MeO-4-Pym 1-Azt- (CH _Two ) _Three 1-2382 4-F-Ph 2-MeO-4-Pym 1-Pyrd- (CH _Two ) _Three 1-2383 4-F-Ph 2-MeO-4-Pym 1-Pip- (CH _Two ) _Three 1-2384 4-F-Ph 2-MeO-4-Pym 1-Mor- (CH _Two ) _Three 1-2385 4-F-Ph 2-MeO-4-Pym 1-Tmor- (CH _Two ) _Three 1-2386 4-F-Ph 2-MeO-4-Pym 1-Piz- (CH _Two ) _Three 1-2387 4-F-Ph 2-MeO-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-2388 4-F-Ph 2-MeO-4-Pym 3-Azt 1-2389 4-F-Ph 2-MeO-4-Pym 1-Me-3-Azt 1-2390 4-F-Ph 2- MeO-4-Pym 3-Pyrd 1-2391 4-F-Ph 2-MeO-4-Pym 1-Me-3-Pyrd 1-2392 4-F-Ph 2-MeO-4-Pym 4-Pip 1- 2393 4-F-Ph 2-MeO-4-Pym 4- (3,4-deH-Pip) 1-2394 4-F-Ph 2-MeO-4-Pym 1-Me-4-Pip 1-2395 4 -F-Ph 2-MeO-4-Pym 1-Me-4- (3,4-deH-Pip) 1-2396 4-F-Ph 2-MeO-4-Pym 1-Piz 1-2397 4-F -Ph 2-MeO-4-Pym 4-Me-1-Piz 1-2398 4-F-Ph 2-MeO-4-Pym 4-Pyr 1-2399 4-F-Ph 2-MeO-4-Pym 3 -Pyr 1-2400 4-F-Ph 2-MeO-4-Pym 4-Pym 1-2401 4-F-Ph 2-MeO-4-Pym 5-Pym 1-2402 4-F-Ph 2-MeO- 4-Pym 3-Pyrd-CH _Two 1-2403 4-F-Ph 2-MeO-4-Pym 1-Me-3-Pyrd-CH _Two 1-2404 4-F-Ph 2-MeO-4-Pym 4-Pip-CH _Two 1-2405 4-F-Ph 2-MeO-4-Pym 1-Me-4-Pip-CH _Two 1-2406 4-F-Ph 2-MeO-4-Pym 2-Piz-CH _Two 1-2407 4-F-Ph 2-MeO-4-Pym 4-Pyr-CH _Two 1-2408 4-F-Ph 2-MeO-4-Pym 3-Pyr-CH _Two 1-2409 4-F-Ph 2-MeO-4-Pym 4-Pym-CH _Two 1-2410 4-F-Ph 2-MeO-4-Pym 5-Pym-CH _Two 1-2411 4-F-Ph 2-MeO-4-Pym 2-Pym-CH _Two 1-2412 3-F-Ph 2-MeO-4-Pym H _Two N- (CH _Two ) _Three 1-2413 3-F-Ph 2-MeO-4-Pym MeNH- (CH _Two ) _Three 1-2414 3-F-Ph 2-MeO-4-Pym EtNH- (CH _Two ) _Three 1-2415 3-F-Ph 2-MeO-4-Pym Me _Two N- (CH _Two ) _Three 1-2416 3-F-Ph 2-MeO-4-Pym 1-Azt- (CH _Two ) _Three 1-2417 3-F-Ph 2-MeO-4-Pym 1-Pyrd- (CH _Two ) _Three 1-2418 3-F-Ph 2-MeO-4-Pym 1-Pip- (CH _Two ) _Three 1-2419 3-F-Ph 2-MeO-4-Pym 1-Mor- (CH _Two ) _Three 1-2420 3-F-Ph 2-MeO-4-Pym 1-Tmor- (CH _Two ) _Three 1-2421 3-F-Ph 2-MeO-4-Pym 1-Piz- (CH _Two ) _Three 1-2422 3-F-Ph 2-MeO-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-2423 3-F-Ph 2-MeO-4-Pym 3-Azt 1-2424 3-F-Ph 2-MeO-4-Pym 1-Me-3-Azt 1-2425 3-F-Ph 2- MeO-4-Pym 3-Pyrd 1-2426 3-F-Ph 2-MeO-4-Pym 1-Me-3-Pyrd 1-2427 3-F-Ph 2-MeO-4-Pym 4-Pip 1- 2428 3-F-Ph 2-MeO-4-Pym 4- (3,4-deH-Pip) 1-2429 3-F-Ph 2-MeO-4-Pym 1-Me-4-Pip 1-2430 3 -F-Ph 2-MeO-4-Pym 1-Me-4- (3,4-deH-Pip) 1-2431 3-F-Ph 2-MeO-4-Pym 1-Piz 1-2432 3-F -Ph 2-MeO-4-Pym 4-Me-1-Piz 1-2433 3-F-Ph 2-MeO-4-Pym 4-Pyr 1-2434 3-F-Ph 2-MeO-4-Pym 3 -Pyr 1-2435 3-F-Ph 2-MeO-4-Pym 4-Pym 1-2436 3-F-Ph 2-MeO-4-Pym 5-Pym 1-2437 3-F-Ph 2-MeO- 4-Pym 3-Pyrd-CH _Two 1-2438 3-F-Ph 2-MeO-4-Pym 1-Me-3-Pyrd-CH _Two 1-2439 3-F-Ph 2-MeO-4-Pym 4-Pip-CH _Two 1-2440 3-F-Ph 2-MeO-4-Pym 1-Me-4-Pip-CH _Two 1-2441 3-F-Ph 2-MeO-4-Pym 2-Piz-CH _Two 1-2442 3-F-Ph 2-MeO-4-Pym 4-Pyr-CH _Two 1-2443 3-F-Ph 2-MeO-4-Pym 3-Pyr-CH _Two 1-2444 3-F-Ph 2-MeO-4-Pym 4-Pym-CH _Two 1-2445 3-F-Ph 2-MeO-4-Pym 5-Pym-CH _Two 1-2446 3-F-Ph 2-MeO-4-Pym 2-Pym-CH _Two 1-2447 3,4-diF-Ph 2-MeO-4-Pym H _Two N- (CH _Two ) _Three 1-2448 3,4-diF-Ph 2-MeO-4-Pym MeNH- (CH _Two ) _Three 1-2449 3,4-diF-Ph 2-MeO-4-Pym EtNH- (CH _Two ) _Three 1-2450 3,4-diF-Ph 2-MeO-4-Pym Me _Two N- (CH _Two ) _Three 1-2451 3,4-diF-Ph 2-MeO-4-Pym 1-Azt- (CH _Two ) _Three 1-2452 3,4-diF-Ph 2-MeO-4-Pym 1-Pyrd- (CH _Two ) _Three 1-2453 3,4-diF-Ph 2-MeO-4-Pym 1-Pip- (CH _Two ) _Three 1-2454 3,4-diF-Ph 2-MeO-4-Pym 1-Mor- (CH _Two ) _Three 1-2455 3,4-diF-Ph 2-MeO-4-Pym 1-Tmor- (CH _Two ) _Three 1-2456 3,4-diF-Ph 2-MeO-4-Pym 1-Piz- (CH _Two ) _Three 1-2457 3,4-diF-Ph 2-MeO-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-2458 3,4-diF-Ph 2-MeO-4-Pym 3-Azt 1-2459 3,4-diF-Ph 2-MeO-4-Pym 1-Me-3-Azt 1-2460 3,4 -diF-Ph 2-MeO-4-Pym 3-Pyrd 1-2461 3,4-diF-Ph 2-MeO-4-Pym 1-Me-3-Pyrd 1-2462 3,4-diF-Ph 2- MeO-4-Pym 4-Pip 1-2463 3,4-diF-Ph 2-MeO-4-Pym 4- (3,4-deH-Pip) 1-2464 3,4-diF-Ph 2-MeO- 4-Pym 1-Me-4-Pip 1-2465 3,4-diF-Ph 2-MeO-4-Pym 1-Me-4- (3,4-deH-Pip) 1-2466 3,4-diF -Ph 2-MeO-4-Pym 1-Piz 1-2467 3,4-diF-Ph 2-MeO-4-Pym 4-Me-1-Piz 1-2468 3,4-diF-Ph 2-MeO- 4-Pym 4-Pyr 1-2469 3,4-diF-Ph 2-MeO-4-Pym 3-Pyr 1-2470 3,4-diF-Ph 2-MeO-4-Pym 4-Pym 1-2471 3 , 4-diF-Ph 2-MeO-4-Pym 5-Pym 1-2472 3,4-diF-Ph 2-MeO-4-Pym 3-Pyrd-CH _Two 1-2473 3,4-diF-Ph 2-MeO-4-Pym 1-Me-3-Pyrd-CH _Two 1-2474 3,4-diF-Ph 2-MeO-4-Pym 4-Pip-CH _Two 1-2475 3,4-diF-Ph 2-MeO-4-Pym 1-Me-4-Pip-CH _Two 1-2476 3,4-diF-Ph 2-MeO-4-Pym 2-Piz-CH _Two 1-2477 3,4-diF-Ph 2-MeO-4-Pym 4-Pyr-CH _Two 1-2478 3,4-diF-Ph 2-MeO-4-Pym 3-Pyr-CH _Two 1-2479 3,4-diF-Ph 2-MeO-4-Pym 4-Pym-CH _Two 1-2480 3,4-diF-Ph 2-MeO-4-Pym 5-Pym-CH _Two 1-2481 3,4-diF-Ph 2-MeO-4-Pym 2-Pym-CH _Two 1-2482 3-Cl-Ph 2-MeO-4-Pym H _Two N- (CH _Two ) _Three 1-2483 3-Cl-Ph 2-MeO-4-Pym MeNH- (CH _Two ) _Three 1-2484 3-Cl-Ph 2-MeO-4-Pym EtNH- (CH _Two ) _Three 1-2485 3-Cl-Ph 2-MeO-4-Pym Me _Two N- (CH _Two ) _Three 1-2486 3-Cl-Ph 2-MeO-4-Pym 1-Azt- (CH _Two ) _Three 1-2487 3-Cl-Ph 2-MeO-4-Pym 1-Pyrd- (CH _Two ) _Three 1-2488 3-Cl-Ph 2-MeO-4-Pym 1-Pip- (CH _Two ) _Three 1-2489 3-Cl-Ph 2-MeO-4-Pym 1-Mor- (CH _Two ) _Three 1-2490 3-Cl-Ph 2-MeO-4-Pym 1-Tmor- (CH _Two ) _Three 1-2491 3-Cl-Ph 2-MeO-4-Pym 1-Piz- (CH _Two ) _Three 1-2492 3-Cl-Ph 2-MeO-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 1-2493 3-Cl-Ph 2-MeO-4-Pym 3-Azt 1-2494 3-Cl-Ph 2-MeO-4-Pym 1-Me-3-Azt 1-2495 3-Cl-Ph 2- MeO-4-Pym 3-Pyrd 1-2496 3-Cl-Ph 2-MeO-4-Pym 1-Me-3-Pyrd 1-2497 3-Cl-Ph 2-MeO-4-Pym 4-Pip 1- 2498 3-Cl-Ph 2-MeO-4-Pym 4- (3,4-deH-Pip) 1-2499 3-Cl-Ph 2-MeO-4-Pym 1-Me-4-Pip 1-2500 3 -Cl-Ph 2-MeO-4-Pym 1-Me-4- (3,4-deH-Pip) 1-2501 3-Cl-Ph 2-MeO-4-Pym 1-Piz 1-2502 3-Cl -Ph 2-MeO-4-Pym 4-Me-1-Piz 1-2503 3-Cl-Ph 2-MeO-4-Pym 4-Pyr 1-2504 3-Cl-Ph 2-MeO-4-Pym 3 -Pyr 1-2505 3-Cl-Ph 2-MeO-4-Pym 4-Pym 1-2506 3-Cl-Ph 2-MeO-4-Pym 5-Pym 1-2507 3-Cl-Ph 2-MeO- 4-Pym 3-Pyrd-CH _Two 1-2508 3-Cl-Ph 2-MeO-4-Pym 1-Me-3-Pyrd-CH _Two 1-2509 3-Cl-Ph 2-MeO-4-Pym 4-Pip-CH _Two 1-2510 3-Cl-Ph 2-MeO-4-Pym 1-Me-4-Pip-CH _Two 1-2511 3-Cl-Ph 2-MeO-4-Pym 2-Piz-CH _Two 1-2512 3-Cl-Ph 2-MeO-4-Pym 4-Pyr-CH _Two 1-2513 3-Cl-Ph 2-MeO-4-Pym 3-Pyr-CH _Two 1-2514 3-Cl-Ph 2-MeO-4-Pym 4-Pym-CH _Two 1-2515 3-Cl-Ph 2-MeO-4-Pym 5-Pym-CH _Two 1-2516 3-Cl-Ph 2-MeO-4-Pym 2-Pym-CH _Two 1-2517 4-F-Ph 4-Pyr H _Two N-CH _Two CH = CH 1-2518 4-F-Ph 4-Pyr MeNH-CH _Two CH = CH 1-2519 4-F-Ph 4-Pyr Me _Two N-CH _Two CH = CH 1-2520 4-F-Ph 4-Pyr 3-Pip-CH _Two 1-2521 4-F-Ph 4-Pyr 1-Me-3-Pip-CH _Two 1-2522 4-F-Ph 4-Pyr 2-Me-4-Pip 1-2523 4-F-Ph 4-Pyr 2,2,6,6-tetraMe-4-Pip 1-2524 4-F-Ph 4-Pyr 1-Ac-4-Pip 1-2525 4-F-Ph 4-Pyr 1-Ac-4- (3,4-deH-Pip) 1-2526 4-F-Ph 4-Pyr 4-OH -4-Pip 1-2527 4-F-Ph 4-Pyr 4-OH-1-Me-4-Pip 1-2528 4-F-Ph 4-Pyr AcNH- (CH _Two ) _Three 1-2529 4-F-Ph 4-Pyr 4-NH _Two -cHx 1-2530 4-F-Ph 4-Pyr 4-Pyr-CH (OH) 1-2531 4-F-Ph 4-Pyr 3-Pyr-CH (OH) 1-2532 4-F-Ph 4- Pyr 2-Pyr-CH (OH) 1-2533 4-F-Ph 4-Pyr CF _Three CONH- (CH _Two ) _Three 1-2534 4-F-Ph 4-Pyr BzNH- (CH _Two ) _Three 1-2535 4-F-Ph 4-Pyr 2,4,6-triF-BzNH-CH _Two 1-2536 4-F-Ph 4-Pyr MeSO _Two NH- (CH _Two ) _Three 1-2537 4-F-Ph 4-Pyr 1-NO _Two (CH _Two ) _Two -4-Pip 1-2538 4-F-Ph 4-Pyr 2,3,5,6-tetraF-4-Pyr 1-2539 4-F-Ph 4-Pyr 3-Qun 1-2540 4-F-Ph 4-Pyr 3- (2,3-deH-Qun) 1-2541 4-F-Ph 4-Pyr 3-ABO 1-2542 4-F-Ph 4-Pyr 8-Me-3-ABO 1-2543 4 -F-Ph 4-Pyr 3- (2,3-deH-ABO) 1-2544 4-F-Ph 4-Pyr 8-Me-3- (2,3-deH-ABO) 1-2545 4-F -Ph 4-Pyr 3-ABN 1-2546 4-F-Ph 4-Pyr 9-Me-3-ABN 1-2547 4-F-Ph 4-Pyr 3- (2,3-deH-ABN) 1- 2548 4-F-Ph 4-Pyr 9-Me-3- (2,3-deH-ABN) 1-2549 4-F-Ph 2-NH _Two -4-Pym H _Two N-CH _Two CH = CH 1-2550 4-F-Ph 2-NH _Two -4-Pym MeNH-CH _Two CH = CH 1-2551 4-F-Ph 2-NH _Two -4-Pym Me _Two N-CH _Two CH = CH 1-2552 4-F-Ph 2-NH _Two -4-Pym 3-Pip-CH _Two 1-2553 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pip-CH _Two 1-2554 4-F-Ph 2-NH _Two -4-Pym 2-Me-4-Pip 1-2555 4-F-Ph 2-NH _Two -4-Pym 2,2,6,6-tetraMe-4-Pip 1-2556 4-F-Ph 2-NH _Two -4-Pym 1-Ac-4-Pip 1-2557 4-F-Ph 2-NH _Two -4-Pym 1-Ac-4- (3,4-deH-Pip) 1-2558 4-F-Ph 2-NH _Two -4-Pym 4-OH-4-Pip 1-2559 4-F-Ph 2-NH _Two -4-Pym 4-OH-1-Me-4-Pip 1-2560 4-F-Ph 2-NH _Two -4-Pym AcNH- (CH _Two ) _Three 1-2561 4-F-Ph 2-NH _Two -4-Pym 4-NH _Two -cHx 1-2562 4-F-Ph 2-NH _Two -4-Pym 3-Qun 1-2563 4-F-Ph 2-NH _Two -4-Pym 3- (2,3-deH-Qun) 1-2564 4-F-Ph 2-NH _Two -4-Pym 3-ABO 1-2565 4-F-Ph 2-NH _Two -4-Pym 8-Me-3-ABO 1-2566 4-F-Ph 2-NH _Two -4-Pym 3- (2,3-deH-ABO) 1-2567 4-F-Ph 2-NH _Two -4-Pym 8-Me-3- (2,3-deH-ABO) 1-2568 4-F-Ph 2-NH _Two -4-Pym 3-ABN 1-2569 4-F-Ph 2-NH _Two -4-Pym 9-Me-3-ABN 1-2570 4-F-Ph 2-NH _Two -4-Pym 3- (2,3-deH-ABN) 1-2571 4-F-Ph 2-NH _Two -4-Pym 9-Me-3- (2,3-deH-ABN) 1-2572 4-F-Ph 2-MeNH-4-Pym H _Two N-CH _Two CH = CH 1-2573 4-F-Ph 2-MeNH-4-Pym MeNH-CH _Two CH = CH 1-2574 4-F-Ph 2-MeNH-4-Pym Me _Two N-CH _Two CH = CH 1-2575 4-F-Ph 2-MeNH-4-Pym 3-Pip-CH _Two 1-2576 4-F-Ph 2-MeNH-4-Pym 1-Me-3-Pip-CH _Two 1-2577 4-F-Ph 2-MeNH-4-Pym 2-Me-4-Pip 1-2578 4-F-Ph 2-MeNH-4-Pym 2,2,6,6-tetraMe-4-Pip 1-2579 4-F-Ph 2-MeNH-4-Pym 1-Ac-4-Pip 1-2580 4-F-Ph 2-MeNH-4-Pym 1-Ac-4- (3,4-deH- Pip) 1-2581 4-F-Ph 2-MeNH-4-Pym 4-OH-4-Pip 1-2582 4-F-Ph 2-MeNH-4-Pym 4-OH-1-Me-4-Pip 1-2583 4-F-Ph 2-MeNH-4-Pym AcNH- (CH _Two ) _Three 1-2584 4-F-Ph 2-MeNH-4-Pym 4-NH _Two -cHx 1-2585 4-F-Ph 2-MeNH-4-Pym 3-Qun 1-2586 4-F-Ph 2-MeNH-4-Pym 3- (2,3-deH-Qun) 1-2587 4 -F-Ph 2-MeNH-4-Pym 3-ABO 1-2588 4-F-Ph 2-MeNH-4-Pym 8-Me-3-ABO 1-2589 4-F-Ph 2-MeNH-4- Pym 3- (2,3-deH-ABO) 1-2590 4-F-Ph 2-MeNH-4-Pym 8-Me-3- (2,3-deH-ABO) 1-2591 4-F-Ph 2-MeNH-4-Pym 3-ABN 1-2592 4-F-Ph 2-MeNH-4-Pym 9-Me-3-ABN 1-2593 4-F-Ph 2-MeNH-4-Pym 3- ( (2,3-deH-ABN) 1-2594 4-F-Ph 2-MeNH-4-Pym 9-Me-3- (2,3-deH-ABN) 1-2595 4-F-Ph 2-BnNH- 4-Pyr 4-Pip 1-2596 4-F-Ph 2-BnNH-4-Pyr 4- (3,4-deH-Pip) 1-2597 4-F-Ph 2-BnNH-4-Pym 4-Pip 1-2598 4-F-Ph 2-BnNH-4-Pym 4- (3,4-deH-Pip) 1-2599 4-F-Ph 2- (α-Me-BnNH) -4-Pyr 4-Pip 1-2600 4-F-Ph 2- (α-Me-BnNH) -4-Pyr 4- (3,4-deH-Pip) 1-2601 4-F-Ph 2- (α-Me-BnNH)- 4-Pym 4-Pip 1-2602 4-F-Ph 2- (α-Me-BnNH) -4-Pym 4- (3,4-deH-Pip) 1-2603 3-Cl-Ph 2-BnNH- 4-Pyr 4-Pip 1-2604 3-Cl-Ph 2-BnNH-4-Pyr 4- (3,4-deH-Pip) 1-2605 3-Cl-Ph 2-BnNH-4-Pym 4-Pip 1-2606 3-Cl-Ph 2-BnNH-4-Pym 4- (3,4-deH-Pip) 1-2607 3-Cl-Ph 2- (α-Me-BnNH) -4-Pyr 4-Pip 1-2608 3-Cl-Ph 2- (α-Me-BnNH) -4-Pyr 4- (3,4-deH-Pip) 1-2609 3- Cl-Ph 2- (α-Me-BnNH) -4-Pym 4-Pip 1-2610 3-Cl-Ph 2- (α-Me-BnNH) -4-Pym 4- (3,4-deH-Pip ) 1-2611 3-CF _Three -Ph 2-BnNH-4-Pyr 4-Pip 1-2612 3-CF _Three -Ph 2-BnNH-4-Pyr 4- (3,4-deH-Pip) 1-2613 3-CF _Three -Ph 2-BnNH-4-Pym 4-Pip 1-2614 3-CF _Three -Ph 2-BnNH-4-Pym 4- (3,4-deH-Pip) 1-2615 3-CF _Three -Ph 2- (α-Me-BnNH) -4-Pyr 4-Pip 1-2616 3-CF _Three -Ph 2- (α-Me-BnNH) -4-Pyr 4- (3,4-deH-Pip) 1-2617 3-CF _Three -Ph 2- (α-Me-BnNH) -4-Pym 4-Pip 1-2618 3-CF _Three -Ph 2- (α-Me-BnNH) -4-Pym 4- (3,4-deH-Pip) 1-2619 4-F-Ph 4-Pyr 2-NH _Two -4-Pym 1-2620 4-F-Ph 4-Pyr 2-MeNH-4-pym 1-2621 4-F-Ph 4-Pyr 2-NH _Two -4-Pyr 1-2622 4-F-Ph 4-Pyr 2-MeNH-4-pyr −−−−−−−−−−−−−−−−−−−−−−−−−−−−− −−−−−−− Table 1 (continued) −−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−− Compound No. R ¹ R ^Two R ^Three −−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−− 1-2623 4-F-Ph 4-Pyr H _Two N-CH _Two C (Me) _Two CH _Two 1-2624 4-F-Ph 4-Pyr MeNH-CH _Two C (Me) _Two CH _Two 1-2625 4-F-Ph 4-Pyr EtNH-CH _Two C (Me) _Two CH _Two 1-2626 4-F-Ph 4-Pyr Me _Two N-CH _Two C (Me) _Two CH _Two 1-2627 4-F-Ph 4-Pyr 3- (3,4-deH-Pip) 1-2628 4-F-Ph 4-Pyr 1-Me-3- (3,4-deH-Pip) 1- 2629 4-F-Ph 4-Pyr 1-Et-4- (3,4-deH-Pip) 1-2630 4-F-Ph 4-Pyr 1-Pr-4- (3,4-deH-Pip) 1-2631 4-F-Ph 4-Pyr 1-Pr-4-Pip 1-2632 4-F-Ph 4-Pyr 1-iPr-4- (3,4-deH-Pip) 1-2633 4-F -Ph 4-Pyr 1-iPr-4-Pip 1-2634 4-F-Ph 4-Pyr 1-Bu-4- (3,4-deH-Pip) 1-2635 4-F-Ph 4-Pyr 1 -tBu-4- (3,4-deH-Pip) 1-2636 4-F-Ph 4-Pyr 1-Pn-4- (3,4-deH-Pip) 1-2637 4-F-Ph 4- Pyr 1-Hx-4- (3,4-deH-Pip) 1-2638 4-F-Ph 4-Pyr 1-Hp-4- (3,4-deH-Pip) 1-2639 4-F-Ph 4-Pyr 1-Oc-4- (3,4-deH-Pip) 1-2640 4-F-Ph 4-Pyr 1-Nn-4- (3,4-deH-Pip) 1-2641 4-F -Ph 4-Pyr 1-cPr-4- (3,4-deH-Pip) 1-2642 4-F-Ph 4-Pyr 1-cPn-4- (3,4-deH-Pip) 1-2643 4 -F-Ph 4-Pyr 1-cHx-4- (3,4-deH-Pip) 1-2644 4-F-Ph 4-Pyr 1-Bn-4- (3,4-deH-Pip) 1- 2645 4-F-Ph 4-Pyr 1-Phet-4- (3,4-deH-Pip) 1-2646 4-F-Ph 4-Pyr 1- (3-Ph-Pr) -4- (3, 4-deH-Pip) 1-2647 4-F-Ph 4-Pyr 1- (4-Ph-Bu) -4- (3,4-deH-Pip) 1-2648 4-F-Ph 4-Pyr 1 -Allyl-4- (3,4-deH-Pip) 1-2649 4-F-Ph 4-Pyr 1-Propargyl-4- (3,4-deH-Pip) 1-2650 4-F-Ph 4- Pyr 2,2,6,6, -tetraMe-4- (3,4-deH-Pi p) 1-2651 4-F-Ph 4-Pyr 1,2,2,6,6, -pentaMe-4- (3,4-deH-Pip) 1-2652 4-F-Ph 4-Pyr 1, 2,2,6,6, -pentaMe-4-Pip) 1-2653 4-F-Ph 4-Pyr 7- (1,2,3,5,6,8a-hexaH-Ind) 1-2654 4- F-Ph 4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 1-2655 4-F-Ph 4-Pyr 7-octaH-Ind 1-2656 4-F-Ph 4 -Pyr 8- (1,3,4,6,7,9a-hexaH-2H-Qui) 1-2657 4-F-Ph 4-Pyr 8- (1,3,4,6,9,9a-hexaH -2H-Qui) 1-2658 4-F-Ph 4-Pyr 8-octaH-Qui 1-2659 4-F-Ph 4-Pyr 2,2-diMe-4- (3,4-deH-PiP) 1 -2660 4-F-Ph 4-Pyr 1,2,2-triMe-4- (3,4-deH-PiP) 1-2661 4-F-Ph 4-Pyr 2,2-diMe-4- (4 , 5-deH-PiP) 1-2662 4-F-Ph 4-Pyr 1,2,2-triMe-4- (4,5-deH-PiP) 1-2663 4-F-Ph 4-Pyr 2, 6-diMe-4- (3,4-deH-PiP) 1-2664 4-F-Ph 4-Pyr 1,2,6-triMe-4- (3,4-deH-PiP) 1-2665 4- F-Ph 4-Pyr 2-Me-4- (3,4-deH-Pip) 1-2666 4-F-Ph 4-Pyr 1,2-diMe-4- (3,4-deH-Pip) 1 -2667 4-F-Ph 4-Pyr 1-Et-2-Me-4- (3,4-deH-Pip) 1-2668 4-F-Ph 4-Pyr 1-Pr-2-Me-4- (3,4-deH-Pip) 1-2669 4-F-Ph 4-Pyr 1-Bu-2-Me-4- (3,4-deH-Pip) 1-2670 4-F-Ph 4-Pyr 1-Phet-2-Me-4- (3,4-deH-Pip) 1-2671 4-F-Ph 4-Pyr 2-Et-4- (3,4-deH-Pip) 1-2672 4- F-Ph 4-Pyr 1-Me-2-Et-4- (3,4-deH-Pip) 1-2673 4-F-Ph 4-Pyr 1,2-diEt-4- (3,4-deH-Pip) 1-2674 4-F-Ph 4-Pyr 1-Pr-2-Et-4- ( 3,4-deH-Pip) 1-2675 4-F-Ph 4-Pyr 1-Bu-2-Et-4- (3,4-deH-Pip) 1-2676 4-F-Ph 4-Pyr 1 -Phet-2-Et-4- (3,4-deH-Pip) 1-2677 4-F-Ph 4-Pyr 2-Pr-4- (3,4-deH-Pip) 1-2678 4-F -Ph 4-Pyr 1-Me-2-Pr-4- (3,4-deH-Pip) 1-2679 4-F-Ph 4-Pyr 1-Et-2-Pr-4- (3,4- deH-Pip) 1-2680 4-F-Ph 4-Pyr 1,2-diPr-4- (3,4-deH-Pip) 1-2681 4-F-Ph 4-Pyr 1-Bu-2-Pr -4- (3,4-deH-Pip) 1-2682 4-F-Ph 4-Pyr 1-Phet-2-Pr-4- (3,4-deH-Pip) 1-2683 4-F-Ph 4-Pyr 2-Bu-4- (3,4-deH-Pip) 1-2684 4-F-Ph 4-Pyr 1-Me-2-Bu-4- (3,4-deH-Pip) 1- 2685 4-F-Ph 4-Pyr 1-Et-2-Bu-4- (3,4-deH-Pip) 1-2686 4-F-Ph 4-Pyr 1-Pr-2-Bu-4- ( 3,4-deH-Pip) 1-2687 4-F-Ph 4-Pyr 1,2-diBu-4- (3,4-deH-Pip) 1-2688 4-F-Ph 4-Pyr 1-Phet -2-Bu-4- (3,4-deH-Pip) 1-2689 4-F-Ph 4-Pyr 2-Allyl-4- (3,4-deH-Pip) 1-2690 4-F-Ph 4-Pyr 1-Me-2-Allyl-4- (3,4-deH-Pip) 1-2691 4-F-Ph 4-Pyr 1-Et-2-Allyl-4- (3,4-deH- Pip) 1-2692 4-F-Ph 4-Pyr 1-Pr-2-Allyl-4- (3,4-deH-Pip) 1-2693 4-F-Ph 4-Pyr 1-Bu-2-Allyl -4- (3,4-deH-Pip) 1-2694 4-F-Ph 4-Pyr 1-Phet-2-Al lyl-4- (3,4-deH-Pip) 1-2695 4-F-Ph 4-Pyr 2-Bn-4- (3,4-deH-Pip) 1-2696 4-F-Ph 4-Pyr 1-Me-2-Bn-4- (3,4-deH-Pip) 1-2697 4-F-Ph 4-Pyr 1-Et-2-Bn-4- (3,4-deH-Pip) 1 -2698 4-F-Ph 4-Pyr 1-Pr-2-Bn-4- (3,4-deH-Pip) 1-2699 4-F-Ph 4-Pyr 1-Bu-2-Bn-4- (3,4-deH-Pip) 1-2700 4-F-Ph 4-Pyr 1-Phet-2-Bn-4- (3,4-deH-Pip) 1-2701 4-F-Ph 4-Pyr 2-Phet-4- (3,4-deH-Pip) 1-2702 4-F-Ph 4-Pyr 1-Me-2-Phet-4- (3,4-deH-Pip) 1-2703 4- F-Ph 4-Pyr 1-Et-2-Phet-4- (3,4-deH-Pip) 1-2704 4-F-Ph 4-Pyr 1-Pr-2-Phet-4- (3,4 -deH-Pip) 1-2705 4-F-Ph 4-Pyr 1-Bu-2-Phet-4- (3,4-deH-Pip) 1-2706 4-F-Ph 4-Pyr 1,2- diPhet-4- (3,4-deH-Pip) 1-2707 4-F-Ph 4-Pyr 2-Me-4- (4,5-deH-Pip) 1-2708 4-F-Ph 4-Pyr 1,2-diMe-4- (4,5-deH-Pip) 1-2709 4-F-Ph 4-Pyr 1-Et-2-Me-4- (4,5-deH-Pip) 1-2710 4-F-Ph 4-Pyr 1-Pr-2-Me-4- (4,5-deH-Pip) 1-2711 4-F-Ph 4-Pyr 1-Bu-2-Me-4- (4 , 5-deH-Pip) 1-2712 4-F-Ph 4-Pyr 1-Phet-2-Me-4- (4,5-deH-Pip) 1-2713 4-F-Ph 4-Pyr 2- Et-4- (4,5-deH-Pip) 1-2714 4-F-Ph 4-Pyr 1-Me-2-Et-4- (4,5-deH-Pip) 1-2715 4-F- Ph 4-Pyr 1,2-diEt-4- (4,5-deH-Pip) 1-2716 4-F-Ph 4-Pyr 1 -Pr-2-Et-4- (4,5-deH-Pip) 1-2717 4-F-Ph 4-Pyr 1-Bu-2-Et-4- (4,5-deH-Pip) 1- 2718 4-F-Ph 4-Pyr 1-Phet-2-Et-4- (4,5-deH-Pip) 1-2719 4-F-Ph 4-Pyr 2-Pr-4- (4,5- deH-Pip) 1-2720 4-F-Ph 4-Pyr 1-Me-2-Pr-4- (4,5-deH-Pip) 1-2721 4-F-Ph 4-Pyr 1-Et-2 -Pr-4- (4,5-deH-Pip) 1-2722 4-F-Ph 4-Pyr 1,2-diPr-4- (4,5-deH-Pip) 1-2723 4-F-Ph 4-Pyr 1-Bu-2-Pr-4- (4,5-deH-Pip) 1-2724 4-F-Ph 4-Pyr 1-Phet-2-Pr-4- (4,5-deH- Pip) 1-2725 4-F-Ph 4-Pyr 2-Bu-4- (4,5-deH-Pip) 1-2726 4-F-Ph 4-Pyr 1-Me-2-Bu-4- ( 4,5-deH-Pip) 1-2727 4-F-Ph 4-Pyr 1-Et-2-Bu-4- (4,5-deH-Pip) 1-2728 4-F-Ph 4-Pyr 1 -Pr-2-Bu-4- (4,5-deH-Pip) 1-2729 4-F-Ph 4-Pyr 1,2-diBu-4- (4,5-deH-Pip) 1-2730 4 -F-Ph 4-Pyr 1-Phet-2-Bu-4- (4,5-deH-Pip) 1-2731 4-F-Ph 4-Pyr 2-Allyl-4- (4,5-deH- Pip) 1-2732 4-F-Ph 4-Pyr 1-Me-2-Allyl-4- (4,5-deH-Pip) 1-2733 4-F-Ph 4-Pyr 1-Et-2-Allyl -4- (4,5-deH-Pip) 1-2734 4-F-Ph 4-Pyr 1-Pr-2-Allyl-4- (4,5-deH-Pip) 1-2735 4-F-Ph 4-Pyr 1-Bu-2-Allyl-4- (4,5-deH-Pip) 1-2736 4-F-Ph 4-Pyr 1-Phet-2-Allyl-4- (4,5-deH- Pip) 1-2737 4-F-Ph 4-Pyr 2-Bn-4- (4,5-deH-Pip) 1-273 8 4-F-Ph 4-Pyr 1-Me-2-Bn-4- (4,5-deH-Pip) 1-2739 4-F-Ph 4-Pyr 1-Et-2-Bn-4- ( 4,5-deH-Pip) 1-2740 4-F-Ph 4-Pyr 1-Pr-2-Bn-4- (4,5-deH-Pip) 1-2741 4-F-Ph 4-Pyr 1 -Bu-2-Bn-4- (4,5-deH-Pip) 1-2742 4-F-Ph 4-Pyr 1-Phet-2-Bn-4- (4,5-deH-Pip) 1- 2743 4-F-Ph 4-Pyr 2-Phet-4- (4,5-deH-Pip) 1-2744 4-F-Ph 4-Pyr 1-Me-2-Phet-4- (4,5- deH-Pip) 1-2745 4-F-Ph 4-Pyr 1-Et-2-Phet-4- (4,5-deH-Pip) 1-2746 4-F-Ph 4-Pyr 1-Pr-2 -Phet-4- (4,5-deH-Pip) 1-2747 4-F-Ph 4-Pyr 1-Bu-2-Phet-4- (4,5-deH-Pip) 1-2748 4-F -Ph 4-Pyr 1,2-diPhet-4- (4,5-deH-Pip) 1-2749 4-F-Ph 2-NH _Two -4-Pym H _Two N-CH _Two C (Me) _Two CH _Two 1-2750 4-F-Ph 2-NH _Two -4-Pym MeNH-CH _Two C (Me) _Two CH _Two 1-2751 4-F-Ph 2-NH _Two -4-Pym EtNH-CH _Two C (Me) _Two CH _Two 1-2752 4-F-Ph 2-NH _Two -4-Pym Me _Two N-CH _Two C (Me) _Two CH _Two 1-2753 4-F-Ph 2-NH _Two -4-Pym 3- (3,4-deH-Pip) 1-2754 4-F-Ph 2-NH _Two -4-Pym 1-Me-3- (3,4-deH-Pip) 1-2755 4-F-Ph 2-NH _Two -4-Pym 1-Et-4- (3,4-deH-Pip) 1-2756 4-F-Ph 2-NH _Two -4-Pym 1-Pr-4- (3,4-deH-Pip) 1-2757 4-F-Ph 2-NH _Two -4-Pym 1-Pr-4-Pip 1-2758 4-F-Ph 2-NH _Two -4-Pym 1-iPr-4- (3,4-deH-Pip) 1-2759 4-F-Ph 2-NH _Two -4-Pym 1-iPr-4-Pip 1-2760 4-F-Ph 2-NH _Two -4-Pym 1-Bu-4- (3,4-deH-Pip) 1-2761 4-F-Ph 2-NH _Two -4-Pym 1-tBu-4- (3,4-deH-Pip) 1-2762 4-F-Ph 2-NH _Two -4-Pym 1-Pn-4- (3,4-deH-Pip) 1-2763 4-F-Ph 2-NH _Two -4-Pym 1-Hx-4- (3,4-deH-Pip) 1-2764 4-F-Ph 2-NH _Two -4-Pym 1-Hp-4- (3,4-deH-Pip) 1-2765 4-F-Ph 2-NH _Two -4-Pym 1-Oc-4- (3,4-deH-Pip) 1-2766 4-F-Ph 2-NH _Two -4-Pym 1-Nn-4- (3,4-deH-Pip) 1-2767 4-F-Ph 2-NH _Two -4-Pym 1-cPr-4- (3,4-deH-Pip) 1-2768 4-F-Ph 2-NH _Two -4-Pym 1-cPn-4- (3,4-deH-Pip) 1-2769 4-F-Ph 2-NH _Two -4-Pym 1-cHx-4- (3,4-deH-Pip) 1-2770 4-F-Ph 2-NH _Two -4-Pym 1-Bn-4- (3,4-deH-Pip) 1-2771 4-F-Ph 2-NH _Two -4-Pym 1-Phet-4- (3,4-deH-Pip) 1-2772 4-F-Ph 2-NH _Two -4-Pym 1- (3-Ph-Pr) -4- (3,4-deH-Pip) 1-2773 4-F-Ph 2-NH _Two -4-Pym 1- (4-Ph-Bu) -4- (3,4-deH-Pip) 1-2774 4-F-Ph 2-NH _Two -4-Pym 1-Allyl-4- (3,4-deH-Pip) 1-2775 4-F-Ph 2-NH _Two -4-Pym 1-Propargyl-4- (3,4-deH-Pip) 1-2776 4-F-Ph 2-NH _Two -4-Pym 2,2,6,6, -tetraMe-4- (3,4-deH-Pip) 1-2777 4-F-Ph 2-NH _Two -4-Pym 1,2,2,6,6, -pentaMe-4- (3,4-deH-Pip) 1-2778 4-F-Ph 2-NH _Two -4-Pym 1,2,2,6,6, -pentaMe-4-Pip) 1-2779 4-F-Ph 2-NH _Two -4-Pym 7- (1,2,3,5,6,8a-hexaH-Ind) 1-2780 4-F-Ph 2-NH _Two -4-Pym 7- (1,2,3,5,8,8a-hexaH-Ind) 1-2781 4-F-Ph 2-NH _Two -4-Pym 7-octaH-Ind 1-2782 4-F-Ph 2-NH _Two -4-Pym 8- (1,3,4,6,7,9a-hexaH-2H-Qui) 1-2783 4-F-Ph 2-NH _Two -4-Pym 8- (1,3,4,6,9,9a-hexaH-2H-Qui) 1-2784 4-F-Ph 2-NH _Two -4-Pym 8-octaH-Qui 1-2785 4-F-Ph 2-NH _Two -4-Pym 2,2-diMe-4- (3,4-deH-PiP) 1-2786 4-F-Ph 2-NH _Two -4-Pym 1,2,2-triMe-4- (3,4-deH-PiP) 1-2787 4-F-Ph 2-NH _Two -4-Pym 2,2-diMe-4- (4,5-deH-PiP) 1-2788 4-F-Ph 2-NH _Two -4-Pym 1,2,2-triMe-4- (4,5-deH-PiP) 1-2789 4-F-Ph 2-NH _Two -4-Pym 2,6-diMe-4- (3,4-deH-PiP) 1-2790 4-F-Ph 2-NH _Two -4-Pym 1,2,6-triMe-4- (3,4-deH-PiP) 1-2791 4-F-Ph 2-NH _Two -4-Pym 2-Me-4- (3,4-deH-Pip) 1-2792 4-F-Ph 2-NH _Two -4-Pym 1,2-diMe-4- (3,4-deH-Pip) 1-2793 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Me-4- (3,4-deH-Pip) 1-2794 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Me-4- (3,4-deH-Pip) 1-2795 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Me-4- (3,4-deH-Pip) 1-2796 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Me-4- (3,4-deH-Pip) 1-2797 4-F-Ph 2-NH _Two -4-Pym 2-Et-4- (3,4-deH-Pip) 1-2798 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Et-4- (3,4-deH-Pip) 1-2799 4-F-Ph 2-NH _Two -4-Pym 1,2-diEt-4- (3,4-deH-Pip) 1-2800 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Et-4- (3,4-deH-Pip) 1-2801 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Et-4- (3,4-deH-Pip) 1-2802 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Et-4- (3,4-deH-Pip) 1-2803 4-F-Ph 2-NH _Two -4-Pym 2-Pr-4- (3,4-deH-Pip) 1-2804 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Pr-4- (3,4-deH-Pip) 1-2805 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Pr-4- (3,4-deH-Pip) 1-2806 4-F-Ph 2-NH _Two -4-Pym 1,2-diPr-4- (3,4-deH-Pip) 1-2807 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Pr-4- (3,4-deH-Pip) 1-2808 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Pr-4- (3,4-deH-Pip) 1-2809 4-F-Ph 2-NH _Two -4-Pym 2-Bu-4- (3,4-deH-Pip) 1-2810 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Bu-4- (3,4-deH-Pip) 1-2811 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Bu-4- (3,4-deH-Pip) 1-2812 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Bu-4- (3,4-deH-Pip) 1-2813 4-F-Ph 2-NH _Two -4-Pym 1,2-diBu-4- (3,4-deH-Pip) 1-2814 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Bu-4- (3,4-deH-Pip) 1-2815 4-F-Ph 2-NH _Two -4-Pym 2-Allyl-4- (3,4-deH-Pip) 1-2816 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Allyl-4- (3,4-deH-Pip) 1-2817 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Allyl-4- (3,4-deH-Pip) 1-2818 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Allyl-4- (3,4-deH-Pip) 1-2819 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Allyl-4- (3,4-deH-Pip) 1-2820 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Allyl-4- (3,4-deH-Pip) 1-2821 4-F-Ph 2-NH _Two -4-Pym 2-Bn-4- (3,4-deH-Pip) 1-2822 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Bn-4- (3,4-deH-Pip) 1-2823 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Bn-4- (3,4-deH-Pip) 1-2824 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Bn-4- (3,4-deH-Pip) 1-2825 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Bn-4- (3,4-deH-Pip) 1-2826 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Bn-4- (3,4-deH-Pip) 1-2827 4-F-Ph 2-NH _Two -4-Pym 2-Phet-4- (3,4-deH-Pip) 1-2828 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Phet-4- (3,4-deH-Pip) 1-2829 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Phet-4- (3,4-deH-Pip) 1-2830 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Phet-4- (3,4-deH-Pip) 1-2831 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Phet-4- (3,4-deH-Pip) 1-2832 4-F-Ph 2-NH _Two -4-Pym 1,2-diPhet-4- (3,4-deH-Pip) 1-2833 4-F-Ph 2-NH _Two -4-Pym 2-Me-4- (4,5-deH-Pip) 1-2834 4-F-Ph 2-NH _Two -4-Pym 1,2-diMe-4- (4,5-deH-Pip) 1-2835 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Me-4- (4,5-deH-Pip) 1-2836 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Me-4- (4,5-deH-Pip) 1-2837 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Me-4- (4,5-deH-Pip) 1-2838 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Me-4- (4,5-deH-Pip) 1-2839 4-F-Ph 2-NH _Two -4-Pym 2-Et-4- (4,5-deH-Pip) 1-2840 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Et-4- (4,5-deH-Pip) 1-2841 4-F-Ph 2-NH _Two -4-Pym 1,2-diEt-4- (4,5-deH-Pip) 1-2842 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Et-4- (4,5-deH-Pip) 1-2843 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Et-4- (4,5-deH-Pip) 1-2844 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Et-4- (4,5-deH-Pip) 1-2845 4-F-Ph 2-NH _Two -4-Pym 2-Pr-4- (4,5-deH-Pip) 1-2846 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Pr-4- (4,5-deH-Pip) 1-2847 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Pr-4- (4,5-deH-Pip) 1-2848 4-F-Ph 2-NH _Two -4-Pym 1,2-diPr-4- (4,5-deH-Pip) 1-2849 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Pr-4- (4,5-deH-Pip) 1-2850 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Pr-4- (4,5-deH-Pip) 1-2851 4-F-Ph 2-NH _Two -4-Pym 2-Bu-4- (4,5-deH-Pip) 1-2852 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Bu-4- (4,5-deH-Pip) 1-2853 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Bu-4- (4,5-deH-Pip) 1-2854 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Bu-4- (4,5-deH-Pip) 1-2855 4-F-Ph 2-NH _Two -4-Pym 1,2-diBu-4- (4,5-deH-Pip) 1-2856 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Bu-4- (4,5-deH-Pip) 1-2857 4-F-Ph 2-NH _Two -4-Pym 2-Allyl-4- (4,5-deH-Pip) 1-2858 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Allyl-4- (4,5-deH-Pip) 1-2859 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Allyl-4- (4,5-deH-Pip) 1-2860 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Allyl-4- (4,5-deH-Pip) 1-2861 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Allyl-4- (4,5-deH-Pip) 1-2862 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Allyl-4- (4,5-deH-Pip) 1-2863 4-F-Ph 2-NH _Two -4-Pym 2-Bn-4- (4,5-deH-Pip) 1-2864 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Bn-4- (4,5-deH-Pip) 1-2865 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Bn-4- (4,5-deH-Pip) 1-2866 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Bn-4- (4,5-deH-Pip) 1-2867 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Bn-4- (4,5-deH-Pip) 1-2868 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Bn-4- (4,5-deH-Pip) 1-2869 4-F-Ph 2-NH _Two -4-Pym 2-Phet-4- (4,5-deH-Pip) 1-2870 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Phet-4- (4,5-deH-Pip) 1-2871 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Phet-4- (4,5-deH-Pip) 1-2872 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Phet-4- (4,5-deH-Pip) 1-2873 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Phet-4- (4,5-deH-Pip) 1-2874 4-F-Ph 2-NH _Two -4-Pym 1,2-diPhet-4- (4,5-deH-Pip) 1-2875 4-F-Ph 2-MeNH-4-Pym H _Two N-CH _Two C (Me) _Two CH _Two 1-2876 4-F-Ph 2-MeNH-4-Pym MeNH-CH _Two C (Me) _Two CH _Two 1-2877 4-F-Ph 2-MeNH-4-Pym EtNH-CH _Two C (Me) _Two CH _Two 1-2878 4-F-Ph 2-MeNH-4-Pym Me _Two N-CH _Two C (Me) _Two CH _Two 1-2879 4-F-Ph 2-MeNH-4-Pym 3- (3,4-deH-Pip) 1-2880 4-F-Ph 2-MeNH-4-Pym 1-Me-3- (3, 4-deH-Pip) 1-2881 4-F-Ph 2-MeNH-4-Pym 1-Et-4- (3,4-deH-Pip) 1-2882 4-F-Ph 2-MeNH-4- Pym 1-Pr-4- (3,4-deH-Pip) 1-2883 4-F-Ph 2-MeNH-4-Pym 1-Pr-4-Pip 1-2884 4-F-Ph 2-MeNH- 4-Pym 1-iPr-4- (3,4-deH-Pip) 1-2885 4-F-Ph 2-MeNH-4-Pym 1-iPr-4-Pip 1-2886 4-F-Ph 2- MeNH-4-Pym 1-Bu-4- (3,4-deH-Pip) 1-2887 4-F-Ph 2-MeNH-4-Pym 1-tBu-4- (3,4-deH-Pip) 1-2888 4-F-Ph 2-MeNH-4-Pym 1-Pn-4- (3,4-deH-Pip) 1-2889 4-F-Ph 2-MeNH-4-Pym 1-Hx-4 -(3,4-deH-Pip) 1-2890 4-F-Ph 2-MeNH-4-Pym 1-Hp-4- (3,4-deH-Pip) 1-2891 4-F-Ph 2- MeNH-4-Pym 1-Oc-4- (3,4-deH-Pip) 1-2892 4-F-Ph 2-MeNH-4-Pym 1-Nn-4- (3,4-deH-Pip) 1-2893 4-F-Ph 2-MeNH-4-Pym 1-cPr-4- (3,4-deH-Pip) 1-2894 4-F-Ph 2-MeNH-4-Pym 1-cPn-4 -(3,4-deH-Pip) 1-2895 4-F-Ph 2-MeNH-4-Pym 1-cHx-4- (3,4-deH-Pip) 1-2896 4-F-Ph 2- MeNH-4-Pym 1-Bn-4- (3,4-deH-Pip) 1-2897 4-F-Ph 2-MeNH-4-Pym 1-Phet-4- (3,4-deH-Pip) 1-2898 4-F-Ph 2-MeNH-4-Pym 1- (3-Ph-Pr) -4- (3,4-deH-Pip) 1-2899 4-F-Ph 2-MeNH-4- Pym 1- (4-Ph-Bu) -4- (3,4-deH- Pip) 1-2900 4-F-Ph 2-MeNH-4-Pym 1-Allyl-4- (3,4-deH-Pip) 1-2901 4-F-Ph 2-MeNH-4-Pym 1-Propargyl -4- (3,4-deH-Pip) 1-2902 4-F-Ph 2-MeNH-4-Pym 2,2,6,6, -tetraMe-4- (3,4-deH-Pip) 1 -2903 4-F-Ph 2-MeNH-4-Pym 1,2,2,6,6, -pentaMe-4- (3,4-deH-Pip) 1-2904 4-F-Ph 2-MeNH- 4-Pym 1,2,2,6,6, -pentaMe-4-Pip) 1-2905 4-F-Ph 2-MeNH-4-Pym 7- (1,2,3,5,6,8a- hexaH-Ind) 1-2906 4-F-Ph 2-MeNH-4-Pym 7- (1,2,3,5,8,8a-hexaH-Ind) 1-2907 4-F-Ph 2-MeNH- 4-Pym 7-octaH-Ind 1-2908 4-F-Ph 2-MeNH-4-Pym 8- (1,3,4,6,7,9a-hexaH-2H-Qui) 1-2909 4-F -Ph 2-MeNH-4-Pym 8- (1,3,4,6,9,9a-hexaH-2H-Qui) 1-2910 4-F-Ph 2-MeNH-4-Pym 8-octaH-Qui 1-2911 4-F-Ph 2-MeNH-4-Pym 2,2-diMe-4- (3,4-deH-PiP) 1-2912 4-F-Ph 2-MeNH-4-Pym 1,2 , 2-triMe-4- (3,4-deH-PiP) 1-2913 4-F-Ph 2-MeNH-4-Pym 2,2-diMe-4- (4,5-deH-PiP) 1- 2914 4-F-Ph 2-MeNH-4-Pym 1,2,2-triMe-4- (4,5-deH-PiP) 1-2915 4-F-Ph 2-MeNH-4-Pym 2,6 -diMe-4- (3,4-deH-PiP) 1-2916 4-F-Ph 2-MeNH-4-Pym 1,2,6-triMe-4- (3,4-deH-PiP) 1- 2917 4-F-Ph 2-MeNH-4-Pym 2-Me-4- (3,4-deH-Pip) 1-2918 4-F-Ph 2-MeNH-4-Pym 1,2-diMe-4 -(3,4-de H-Pip) 1-2919 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Me-4- (3,4-deH-Pip) 1-2920 4-F-Ph 2-MeNH- 4-Pym 1-Pr-2-Me-4- (3,4-deH-Pip) 1-2921 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Me-4- (3, 4-deH-Pip) 1-2922 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Me-4- (3,4-deH-Pip) 1-2923 4-F-Ph 2- MeNH-4-Pym 2-Et-4- (3,4-deH-Pip) 1-2924 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Et-4- (3,4- deH-Pip) 1-2925 4-F-Ph 2-MeNH-4-Pym 1,2-diEt-4- (3,4-deH-Pip) 1-2926 4-F-Ph 2-MeNH-4- Pym 1-Pr-2-Et-4- (3,4-deH-Pip) 1-2927 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Et-4- (3,4- deH-Pip) 1-2928 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Et-4- (3,4-deH-Pip) 1-2929 4-F-Ph 2-MeNH- 4-Pym 2-Pr-4- (3,4-deH-Pip) 1-2930 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Pr-4- (3,4-deH- Pip) 1-2931 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Pr-4- (3,4-deH-Pip) 1-2932 4-F-Ph 2-MeNH-4- Pym 1,2-diPr-4- (3,4-deH-Pip) 1-2933 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Pr-4- (3,4-deH- Pip) 1-2934 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Pr-4- (3,4-deH-Pip) 1-2935 4-F-Ph 2-MeNH-4- Pym 2-Bu-4- (3,4-deH-Pip) 1-2936 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Bu-4- (3,4-deH-Pip) 1-2937 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Bu-4- (3,4-deH-Pi p) 1-2938 4-F-Ph 2-MeNH-4-Pym 1-Pr-2-Bu-4- (3,4-deH-Pip) 1-2939 4-F-Ph 2-MeNH-4- Pym 1,2-diBu-4- (3,4-deH-Pip) 1-2940 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Bu-4- (3,4-deH- Pip) 1-2941 4-F-Ph 2-MeNH-4-Pym 2-Allyl-4- (3,4-deH-Pip) 1-2942 4-F-Ph 2-MeNH-4-Pym 1-Me -2-Allyl-4- (3,4-deH-Pip) 1-2943 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Allyl-4- (3,4-deH-Pip) 1-2944 4-F-Ph 2-MeNH-4-Pym 1-Pr-2-Allyl-4- (3,4-deH-Pip) 1-2945 4-F-Ph 2-MeNH-4-Pym 1 -Bu-2-Allyl-4- (3,4-deH-Pip) 1-2946 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Allyl-4- (3,4-deH- Pip) 1-2947 4-F-Ph 2-MeNH-4-Pym 2-Bn-4- (3,4-deH-Pip) 1-2948 4-F-Ph 2-MeNH-4-Pym 1-Me -2-Bn-4- (3,4-deH-Pip) 1-2949 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Bn-4- (3,4-deH-Pip) 1-2950 4-F-Ph 2-MeNH-4-Pym 1-Pr-2-Bn-4- (3,4-deH-Pip) 1-2951 4-F-Ph 2-MeNH-4-Pym 1 -Bu-2-Bn-4- (3,4-deH-Pip) 1-2952 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Bn-4- (3,4-deH- Pip) 1-2953 4-F-Ph 2-MeNH-4-Pym 2-Phet-4- (3,4-deH-Pip) 1-2954 4-F-Ph 2-MeNH-4-Pym 1-Me -2-Phet-4- (3,4-deH-Pip) 1-2955 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Phet-4- (3,4-deH-Pip) 1-2956 4-F-Ph 2-MeNH-4-Pym 1- Pr-2-Phet-4- (3,4-deH-Pip) 1-2957 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Phet-4- (3,4-deH-Pip ) 1-2958 4-F-Ph 2-MeNH-4-Pym 1,2-diPhet-4- (3,4-deH-Pip) 1-2959 4-F-Ph 2-MeNH-4-Pym 2- Me-4- (4,5-deH-Pip) 1-2960 4-F-Ph 2-MeNH-4-Pym 1,2-diMe-4- (4,5-deH-Pip) 1-2961 4- F-Ph 2-MeNH-4-Pym 1-Et-2-Me-4- (4,5-deH-Pip) 1-2962 4-F-Ph 2-MeNH-4-Pym 1-Pr-2- Me-4- (4,5-deH-Pip) 1-2963 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Me-4- (4,5-deH-Pip) 1-2964 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Me-4- (4,5-deH-Pip) 1-2965 4-F-Ph 2-MeNH-4-Pym 2-Et- 4- (4,5-deH-Pip) 1-2966 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Et-4- (4,5-deH-Pip) 1-2967 4- F-Ph 2-MeNH-4-Pym 1,2-diEt-4- (4,5-deH-Pip) 1-2968 4-F-Ph 2-MeNH-4-Pym 1-Pr-2-Et- 4- (4,5-deH-Pip) 1-2969 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Et-4- (4,5-deH-Pip) 1-2970 4- F-Ph 2-MeNH-4-Pym 1-Phet-2-Et-4- (4,5-deH-Pip) 1-2971 4-F-Ph 2-MeNH-4-Pym 2-Pr-4- (4,5-deH-Pip) 1-2972 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Pr-4- (4,5-deH-Pip) 1-2973 4-F- Ph 2-MeNH-4-Pym 1-Et-2-Pr-4- (4,5-deH-Pip) 1-2974 4-F-Ph 2-MeNH-4-Pym 1,2-diPr-4- (4,5-deH-Pip) 1-2975 4-F-Ph 2-MeNH-4-Pym 1-Bu -2-Pr-4- (4,5-deH-Pip) 1-2976 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Pr-4- (4,5-deH-Pip) 1-2977 4-F-Ph 2-MeNH-4-Pym 2-Bu-4- (4,5-deH-Pip) 1-2978 4-F-Ph 2-MeNH-4-Pym 1-Me-2 -Bu-4- (4,5-deH-Pip) 1-2979 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Bu-4- (4,5-deH-Pip) 1- 2980 4-F-Ph 2-MeNH-4-Pym 1-Pr-2-Bu-4- (4,5-deH-Pip) 1-2981 4-F-Ph 2-MeNH-4-Pym 1,2 -diBu-4- (4,5-deH-Pip) 1-2982 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Bu-4- (4,5-deH-Pip) 1- 2983 4-F-Ph 2-MeNH-4-Pym 2-Allyl-4- (4,5-deH-Pip) 1-2984 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Allyl -4- (4,5-deH-Pip) 1-2985 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Allyl-4- (4,5-deH-Pip) 1-2986 4 -F-Ph 2-MeNH-4-Pym 1-Pr-2-Allyl-4- (4,5-deH-Pip) 1-2987 4-F-Ph 2-MeNH-4-Pym 1-Bu-2 -Allyl-4- (4,5-deH-Pip) 1-2988 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Allyl-4- (4,5-deH-Pip) 1- 2989 4-F-Ph 2-MeNH-4-Pym 2-Bn-4- (4,5-deH-Pip) 1-2990 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Bn -4- (4,5-deH-Pip) 1-2991 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Bn-4- (4,5-deH-Pip) 1-2992 4 -F-Ph 2-MeNH-4-Pym 1-Pr-2-Bn-4- (4,5-deH-Pip) 1-2993 4-F-Ph 2-MeNH-4-Pym 1-Bu-2 -Bn-4- (4,5-deH-Pip) 1-2994 4-F-Ph 2- MeNH-4-Pym 1-Phet-2-Bn-4- (4,5-deH-Pip) 1-2995 4-F-Ph 2-MeNH-4-Pym 2-Phet-4- (4,5- deH-Pip) 1-2996 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Phet-4- (4,5-deH-Pip) 1-2997 4-F-Ph 2-MeNH- 4-Pym 1-Et-2-Phet-4- (4,5-deH-Pip) 1-2998 4-F-Ph 2-MeNH-4-Pym 1-Pr-2-Phet-4- (4, 5-deH-Pip) 1-2999 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Phet-4- (4,5-deH-Pip) 1-3000 4-F-Ph 2- MeNH-4-Pym 1,2-diPhet-4- (4,5-deH-Pip) 1-3001 4-F-Ph 2-NH _Two -4-Pyr H _Two N-CH _Two C (Me) _Two CH _Two 1-3002 4-F-Ph 2-NH _Two -4-Pyr MeNH-CH _Two C (Me) _Two CH _Two 1-3003 4-F-Ph 2-NH _Two -4-Pyr EtNH-CH _Two C (Me) _Two CH _Two 1-3004 4-F-Ph 2-NH _Two -4-Pyr Me _Two N-CH _Two C (Me) _Two CH _Two 1-3005 4-F-Ph 2-NH _Two -4-Pyr 3- (3,4-deH-Pip) 1-3006 4-F-Ph 2-NH _Two -4-Pyr 1-Me-3- (3,4-deH-Pip) 1-3007 4-F-Ph 2-NH _Two -4-Pyr 1-Et-4- (3,4-deH-Pip) 1-3008 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-4- (3,4-deH-Pip) 1-3009 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-4-Pip 1-3010 4-F-Ph 2-NH _Two -4-Pyr 1-iPr-4- (3,4-deH-Pip) 1-3011 4-F-Ph 2-NH _Two -4-Pyr 1-iPr-4-Pip 1-3012 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-4- (3,4-deH-Pip) 1-3013 4-F-Ph 2-NH _Two -4-Pyr 1-tBu-4- (3,4-deH-Pip) 1-3014 4-F-Ph 2-NH _Two -4-Pyr 1-Pn-4- (3,4-deH-Pip) 1-3015 4-F-Ph 2-NH _Two -4-Pyr 1-Hx-4- (3,4-deH-Pip) 1-3016 4-F-Ph 2-NH _Two -4-Pyr 1-Hp-4- (3,4-deH-Pip) 1-3017 4-F-Ph 2-NH _Two -4-Pyr 1-Oc-4- (3,4-deH-Pip) 1-3018 4-F-Ph 2-NH _Two -4-Pyr 1-Nn-4- (3,4-deH-Pip) 1-3019 4-F-Ph 2-NH _Two -4-Pyr 1-cPr-4- (3,4-deH-Pip) 1-3020 4-F-Ph 2-NH _Two -4-Pyr 1-cPn-4- (3,4-deH-Pip) 1-3021 4-F-Ph 2-NH _Two -4-Pyr 1-cHx-4- (3,4-deH-Pip) 1-3022 4-F-Ph 2-NH _Two -4-Pyr 1-Bn-4- (3,4-deH-Pip) 1-3023 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-4- (3,4-deH-Pip) 1-3024 4-F-Ph 2-NH _Two -4-Pyr 1- (3-Ph-Pr) -4- (3,4-deH-Pip) 1-3025 4-F-Ph 2-NH _Two -4-Pyr 1- (4-Ph-Bu) -4- (3,4-deH-Pip) 1-3026 4-F-Ph 2-NH _Two -4-Pyr 1-Allyl-4- (3,4-deH-Pip) 1-3027 4-F-Ph 2-NH _Two -4-Pyr 1-Propargyl-4- (3,4-deH-Pip) 1-3028 4-F-Ph 2-NH _Two -4-Pyr 2,2,6,6, -tetraMe-4- (3,4-deH-Pip) 1-3029 4-F-Ph 2-NH _Two -4-Pyr 1,2,2,6,6, -pentaMe-4- (3,4-deH-Pip) 1-3030 4-F-Ph 2-NH _Two -4-Pyr 1,2,2,6,6, -pentaMe-4-Pip) 1-3031 4-F-Ph 2-NH _Two -4-Pyr 7- (1,2,3,5,6,8a-hexaH-Ind) 1-3032 4-F-Ph 2-NH _Two -4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 1-3033 4-F-Ph 2-NH _Two -4-Pyr 7-octaH-Ind 1-3034 4-F-Ph 2-NH _Two -4-Pyr 8- (1,3,4,6,7,9a-hexaH-2H-Qui) 1-3035 4-F-Ph 2-NH _Two -4-Pyr 8- (1,3,4,6,9,9a-hexaH-2H-Qui) 1-3036 4-F-Ph 2-NH _Two -4-Pyr 8-octaH-Qui 1-3037 4-F-Ph 2-NH _Two -4-Pyr 2,2-diMe-4- (3,4-deH-PiP) 1-3038 4-F-Ph 2-NH _Two -4-Pyr 1,2,2-triMe-4- (3,4-deH-PiP) 1-3039 4-F-Ph 2-NH _Two -4-Pyr 2,2-diMe-4- (4,5-deH-PiP) 1-3040 4-F-Ph 2-NH _Two -4-Pyr 1,2,2-triMe-4- (4,5-deH-PiP) 1-3041 4-F-Ph 2-NH _Two -4-Pyr 2,6-diMe-4- (3,4-deH-PiP) 1-3042 4-F-Ph 2-NH _Two -4-Pyr 1,2,6-triMe-4- (3,4-deH-PiP) 1-3043 4-F-Ph 2-NH _Two -4-Pyr 2-Me-4- (3,4-deH-Pip) 1-3044 4-F-Ph 2-NH _Two -4-Pyr 1,2-diMe-4- (3,4-deH-Pip) 1-3045 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Me-4- (3,4-deH-Pip) 1-3046 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Me-4- (3,4-deH-Pip) 1-3047 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Me-4- (3,4-deH-Pip) 1-3048 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Me-4- (3,4-deH-Pip) 1-3049 4-F-Ph 2-NH _Two -4-Pyr 2-Et-4- (3,4-deH-Pip) 1-3050 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Et-4- (3,4-deH-Pip) 1-3051 4-F-Ph 2-NH _Two -4-Pyr 1,2-diEt-4- (3,4-deH-Pip) 1-3052 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Et-4- (3,4-deH-Pip) 1-3053 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Et-4- (3,4-deH-Pip) 1-3054 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Et-4- (3,4-deH-Pip) 1-3055 4-F-Ph 2-NH _Two -4-Pyr 2-Pr-4- (3,4-deH-Pip) 1-3056 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Pr-4- (3,4-deH-Pip) 1-3057 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Pr-4- (3,4-deH-Pip) 1-3058 4-F-Ph 2-NH _Two -4-Pyr 1,2-diPr-4- (3,4-deH-Pip) 1-3059 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Pr-4- (3,4-deH-Pip) 1-3060 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Pr-4- (3,4-deH-Pip) 1-3061 4-F-Ph 2-NH _Two -4-Pyr 2-Bu-4- (3,4-deH-Pip) 1-3062 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Bu-4- (3,4-deH-Pip) 1-3063 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Bu-4- (3,4-deH-Pip) 1-3064 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Bu-4- (3,4-deH-Pip) 1-3065 4-F-Ph 2-NH _Two -4-Pyr 1,2-diBu-4- (3,4-deH-Pip) 1-3066 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Bu-4- (3,4-deH-Pip) 1-3067 4-F-Ph 2-NH _Two -4-Pyr 2-Allyl-4- (3,4-deH-Pip) 1-3068 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Allyl-4- (3,4-deH-Pip) 1-3069 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Allyl-4- (3,4-deH-Pip) 1-3070 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Allyl-4- (3,4-deH-Pip) 1-3071 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Allyl-4- (3,4-deH-Pip) 1-3072 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Allyl-4- (3,4-deH-Pip) 1-3073 4-F-Ph 2-NH _Two -4-Pyr 2-Bn-4- (3,4-deH-Pip) 1-3074 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Bn-4- (3,4-deH-Pip) 1-3075 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Bn-4- (3,4-deH-Pip) 1-3076 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Bn-4- (3,4-deH-Pip) 1-3077 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Bn-4- (3,4-deH-Pip) 1-3078 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Bn-4- (3,4-deH-Pip) 1-3079 4-F-Ph 2-NH _Two -4-Pyr 2-Phet-4- (3,4-deH-Pip) 1-3080 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Phet-4- (3,4-deH-Pip) 1-3081 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Phet-4- (3,4-deH-Pip) 1-3082 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Phet-4- (3,4-deH-Pip) 1-3083 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Phet-4- (3,4-deH-Pip) 1-3084 4-F-Ph 2-NH _Two -4-Pyr 1,2-diPhet-4- (3,4-deH-Pip) 1-3085 4-F-Ph 2-NH _Two -4-Pyr 2-Me-4- (4,5-deH-Pip) 1-3086 4-F-Ph 2-NH _Two -4-Pyr 1,2-diMe-4- (4,5-deH-Pip) 1-3087 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Me-4- (4,5-deH-Pip) 1-3088 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Me-4- (4,5-deH-Pip) 1-3089 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Me-4- (4,5-deH-Pip) 1-3090 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Me-4- (4,5-deH-Pip) 1-3091 4-F-Ph 2-NH _Two -4-Pyr 2-Et-4- (4,5-deH-Pip) 1-3092 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Et-4- (4,5-deH-Pip) 1-3093 4-F-Ph 2-NH _Two -4-Pyr 1,2-diEt-4- (4,5-deH-Pip) 1-3094 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Et-4- (4,5-deH-Pip) 1-3095 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Et-4- (4,5-deH-Pip) 1-3096 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Et-4- (4,5-deH-Pip) 1-3097 4-F-Ph 2-NH _Two -4-Pyr 2-Pr-4- (4,5-deH-Pip) 1-3098 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Pr-4- (4,5-deH-Pip) 1-3099 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Pr-4- (4,5-deH-Pip) 1-3100 4-F-Ph 2-NH _Two -4-Pyr 1,2-diPr-4- (4,5-deH-Pip) 1-3101 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Pr-4- (4,5-deH-Pip) 1-3102 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Pr-4- (4,5-deH-Pip) 1-3103 4-F-Ph 2-NH _Two -4-Pyr 2-Bu-4- (4,5-deH-Pip) 1-3104 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Bu-4- (4,5-deH-Pip) 1-3105 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Bu-4- (4,5-deH-Pip) 1-3106 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Bu-4- (4,5-deH-Pip) 1-3107 4-F-Ph 2-NH _Two -4-Pyr 1,2-diBu-4- (4,5-deH-Pip) 1-3108 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Bu-4- (4,5-deH-Pip) 1-3109 4-F-Ph 2-NH _Two -4-Pyr 2-Allyl-4- (4,5-deH-Pip) 1-3110 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Allyl-4- (4,5-deH-Pip) 1-3111 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Allyl-4- (4,5-deH-Pip) 1-3112 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Allyl-4- (4,5-deH-Pip) 1-3113 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Allyl-4- (4,5-deH-Pip) 1-3114 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Allyl-4- (4,5-deH-Pip) 1-3115 4-F-Ph 2-NH _Two -4-Pyr 2-Bn-4- (4,5-deH-Pip) 1-3116 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Bn-4- (4,5-deH-Pip) 1-3117 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Bn-4- (4,5-deH-Pip) 1-3118 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Bn-4- (4,5-deH-Pip) 1-3119 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Bn-4- (4,5-deH-Pip) 1-3120 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Bn-4- (4,5-deH-Pip) 1-3121 4-F-Ph 2-NH _Two -4-Pyr 2-Phet-4- (4,5-deH-Pip) 1-3122 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Phet-4- (4,5-deH-Pip) 1-3123 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Phet-4- (4,5-deH-Pip) 1-3124 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Phet-4- (4,5-deH-Pip) 1-3125 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Phet-4- (4,5-deH-Pip) 1-3126 4-F-Ph 2-NH _Two -4-Pyr 1,2-diPhet-4- (4,5-deH-Pip) 1-3127 4-F-Ph 2-MeNH-4-Pyr H _Two N-CH _Two C (Me) _Two CH _Two 1-3128 4-F-Ph 2-MeNH-4-Pyr MeNH-CH _Two C (Me) _Two CH _Two 1-3129 4-F-Ph 2-MeNH-4-Pyr EtNH-CH _Two C (Me) _Two CH _Two 1-3130 4-F-Ph 2-MeNH-4-Pyr Me _Two N-CH _Two C (Me) _Two CH _Two 1-3131 4-F-Ph 2-MeNH-4-Pyr 3- (3,4-deH-Pip) 1-3132 4-F-Ph 2-MeNH-4-Pyr 1-Me-3- (3, 4-deH-Pip) 1-3133 4-F-Ph 2-MeNH-4-Pyr 1-Et-4- (3,4-deH-Pip) 1-3134 4-F-Ph 2-MeNH-4- Pyr 1-Pr-4- (3,4-deH-Pip) 1-3135 4-F-Ph 2-MeNH-4-Pyr 1-Pr-4-Pip 1-3136 4-F-Ph 2-MeNH- 4-Pyr 1-iPr-4- (3,4-deH-Pip) 1-3137 4-F-Ph 2-MeNH-4-Pyr 1-iPr-4-Pip 1-3138 4-F-Ph 2- MeNH-4-Pyr 1-Bu-4- (3,4-deH-Pip) 1-3139 4-F-Ph 2-MeNH-4-Pyr 1-tBu-4- (3,4-deH-Pip) 1-3140 4-F-Ph 2-MeNH-4-Pyr 1-Pn-4- (3,4-deH-Pip) 1-3141 4-F-Ph 2-MeNH-4-Pyr 1-Hx-4 -(3,4-deH-Pip) 1-3142 4-F-Ph 2-MeNH-4-Pyr 1-Hp-4- (3,4-deH-Pip) 1-3143 4-F-Ph 2- MeNH-4-Pyr 1-Oc-4- (3,4-deH-Pip) 1-3144 4-F-Ph 2-MeNH-4-Pyr 1-Nn-4- (3,4-deH-Pip) 1-3145 4-F-Ph 2-MeNH-4-Pyr 1-cPr-4- (3,4-deH-Pip) 1-3146 4-F-Ph 2-MeNH-4-Pyr 1-cPn-4 -(3,4-deH-Pip) 1-3147 4-F-Ph 2-MeNH-4-Pyr 1-cHx-4- (3,4-deH-Pip) 1-3148 4-F-Ph 2- MeNH-4-Pyr 1-Bn-4- (3,4-deH-Pip) 1-3149 4-F-Ph 2-MeNH-4-Pyr 1-Phet-4- (3,4-deH-Pip) 1-3150 4-F-Ph 2-MeNH-4-Pyr 1- (3-Ph-Pr) -4- (3,4-deH-Pip) 1-3151 4-F-Ph 2-MeNH-4- Pyr 1- (4-Ph-Bu) -4- (3,4-deH- Pip) 1-3152 4-F-Ph 2-MeNH-4-Pyr 1-Allyl-4- (3,4-deH-Pip) 1-3153 4-F-Ph 2-MeNH-4-Pyr 1-Propargyl -4- (3,4-deH-Pip) 1-3154 4-F-Ph 2-MeNH-4-Pyr 2,2,6,6, -tetraMe-4- (3,4-deH-Pip) 1 -3155 4-F-Ph 2-MeNH-4-Pyr 1,2,2,6,6, -pentaMe-4- (3,4-deH-Pip) 1-3156 4-F-Ph 2-MeNH- 4-Pyr 1,2,2,6,6, -pentaMe-4-Pip) 1-3157 4-F-Ph 2-MeNH-4-Pyr 7- (1,2,3,5,6,8a- hexaH-Ind) 1-3158 4-F-Ph 2-MeNH-4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 1-3159 4-F-Ph 2-MeNH- 4-Pyr 7-octaH-Ind 1-3160 4-F-Ph 2-MeNH-4-Pyr 8- (1,3,4,6,7,9a-hexaH-2H-Qui) 1-3161 4-F -Ph 2-MeNH-4-Pyr 8- (1,3,4,6,9,9a-hexaH-2H-Qui) 1-3162 4-F-Ph 2-MeNH-4-Pyr 8-octaH-Qui 1-3163 4-F-Ph 2-MeNH-4-Pyr 2,2-diMe-4- (3,4-deH-PiP) 1-3164 4-F-Ph 2-MeNH-4-Pyr 1,2 , 2-triMe-4- (3,4-deH-PiP) 1-3165 4-F-Ph 2-MeNH-4-Pyr 2,2-diMe-4- (4,5-deH-PiP) 1- 3166 4-F-Ph 2-MeNH-4-Pyr 1,2,2-triMe-4- (4,5-deH-PiP) 1-3167 4-F-Ph 2-MeNH-4-Pyr 2,6 -diMe-4- (3,4-deH-PiP) 1-3168 4-F-Ph 2-MeNH-4-Pyr 1,2,6-triMe-4- (3,4-deH-PiP) 1- 3169 4-F-Ph 2-MeNH-4-Pyr 2-Me-4- (3,4-deH-Pip) 1-3170 4-F-Ph 2-MeNH-4-Pyr 1,2-diMe-4 -(3,4-de H-Pip) 1-3171 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Me-4- (3,4-deH-Pip) 1-3172 4-F-Ph 2-MeNH- 4-Pyr 1-Pr-2-Me-4- (3,4-deH-Pip) 1-3173 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Me-4- (3, 4-deH-Pip) 1-3174 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Me-4- (3,4-deH-Pip) 1-3175 4-F-Ph 2- MeNH-4-Pyr 2-Et-4- (3,4-deH-Pip) 1-3176 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Et-4- (3,4- deH-Pip) 1-3177 4-F-Ph 2-MeNH-4-Pyr 1,2-diEt-4- (3,4-deH-Pip) 1-3178 4-F-Ph 2-MeNH-4- Pyr 1-Pr-2-Et-4- (3,4-deH-Pip) 1-3179 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Et-4- (3,4- deH-Pip) 1-3180 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Et-4- (3,4-deH-Pip) 1-3181 4-F-Ph 2-MeNH- 4-Pyr 2-Pr-4- (3,4-deH-Pip) 1-3182 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Pr-4- (3,4-deH- Pip) 1-3183 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Pr-4- (3,4-deH-Pip) 1-3184 4-F-Ph 2-MeNH-4- Pyr 1,2-diPr-4- (3,4-deH-Pip) 1-3185 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Pr-4- (3,4-deH- Pip) 1-3186 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Pr-4- (3,4-deH-Pip) 1-3187 4-F-Ph 2-MeNH-4- Pyr 2-Bu-4- (3,4-deH-Pip) 1-3188 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Bu-4- (3,4-deH-Pip) 1-3189 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Bu-4- (3,4-deH-Pi p) 1-3190 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2-Bu-4- (3,4-deH-Pip) 1-3191 4-F-Ph 2-MeNH-4- Pyr 1,2-diBu-4- (3,4-deH-Pip) 1-3192 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Bu-4- (3,4-deH- Pip) 1-3193 4-F-Ph 2-MeNH-4-Pyr 2-Allyl-4- (3,4-deH-Pip) 1-3194 4-F-Ph 2-MeNH-4-Pyr 1-Me -2-Allyl-4- (3,4-deH-Pip) 1-3195 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Allyl-4- (3,4-deH-Pip) 1-3196 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2-Allyl-4- (3,4-deH-Pip) 1-3197 4-F-Ph 2-MeNH-4-Pyr 1 -Bu-2-Allyl-4- (3,4-deH-Pip) 1-3198 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Allyl-4- (3,4-deH- Pip) 1-3199 4-F-Ph 2-MeNH-4-Pyr 2-Bn-4- (3,4-deH-Pip) 1-3200 4-F-Ph 2-MeNH-4-Pyr 1-Me -2-Bn-4- (3,4-deH-Pip) 1-3201 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Bn-4- (3,4-deH-Pip) 1-3202 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2-Bn-4- (3,4-deH-Pip) 1-3203 4-F-Ph 2-MeNH-4-Pyr 1 -Bu-2-Bn-4- (3,4-deH-Pip) 1-3204 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Bn-4- (3,4-deH- Pip) 1-3205 4-F-Ph 2-MeNH-4-Pyr 2-Phet-4- (3,4-deH-Pip) 1-3206 4-F-Ph 2-MeNH-4-Pyr 1-Me -2-Phet-4- (3,4-deH-Pip) 1-3207 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Phet-4- (3,4-deH-Pip) 1-3208 4-F-Ph 2-MeNH-4-Pyr 1- Pr-2-Phet-4- (3,4-deH-Pip) 1-3209 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Phet-4- (3,4-deH-Pip ) 1-3210 4-F-Ph 2-MeNH-4-Pyr 1,2-diPhet-4- (3,4-deH-Pip) 1-3211 4-F-Ph 2-MeNH-4-Pyr 2- Me-4- (4,5-deH-Pip) 1-3212 4-F-Ph 2-MeNH-4-Pyr 1,2-diMe-4- (4,5-deH-Pip) 1-3213 4- F-Ph 2-MeNH-4-Pyr 1-Et-2-Me-4- (4,5-deH-Pip) 1-3214 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2- Me-4- (4,5-deH-Pip) 1-3215 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Me-4- (4,5-deH-Pip) 1-3216 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Me-4- (4,5-deH-Pip) 1-3217 4-F-Ph 2-MeNH-4-Pyr 2-Et- 4- (4,5-deH-Pip) 1-3218 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Et-4- (4,5-deH-Pip) 1-3219 4- F-Ph 2-MeNH-4-Pyr 1,2-diEt-4- (4,5-deH-Pip) 1-3220 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2-Et- 4- (4,5-deH-Pip) 1-3221 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Et-4- (4,5-deH-Pip) 1-3222 4- F-Ph 2-MeNH-4-Pyr 1-Phet-2-Et-4- (4,5-deH-Pip) 1-3223 4-F-Ph 2-MeNH-4-Pyr 2-Pr-4- (4,5-deH-Pip) 1-3224 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Pr-4- (4,5-deH-Pip) 1-3225 4-F- Ph 2-MeNH-4-Pyr 1-Et-2-Pr-4- (4,5-deH-Pip) 1-3226 4-F-Ph 2-MeNH-4-Pyr 1,2-diPr-4- (4,5-deH-Pip) 1-3227 4-F-Ph 2-MeNH-4-Pyr 1-Bu -2-Pr-4- (4,5-deH-Pip) 1-3228 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Pr-4- (4,5-deH-Pip) 1-3229 4-F-Ph 2-MeNH-4-Pyr 2-Bu-4- (4,5-deH-Pip) 1-3230 4-F-Ph 2-MeNH-4-Pyr 1-Me-2 -Bu-4- (4,5-deH-Pip) 1-3231 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Bu-4- (4,5-deH-Pip) 1- 3232 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2-Bu-4- (4,5-deH-Pip) 1-3233 4-F-Ph 2-MeNH-4-Pyr 1,2 -diBu-4- (4,5-deH-Pip) 1-3234 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Bu-4- (4,5-deH-Pip) 1- 3235 4-F-Ph 2-MeNH-4-Pyr 2-Allyl-4- (4,5-deH-Pip) 1-3236 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Allyl -4- (4,5-deH-Pip) 1-3237 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Allyl-4- (4,5-deH-Pip) 1-3238 4 -F-Ph 2-MeNH-4-Pyr 1-Pr-2-Allyl-4- (4,5-deH-Pip) 1-3239 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2 -Allyl-4- (4,5-deH-Pip) 1-3240 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Allyl-4- (4,5-deH-Pip) 1- 3241 4-F-Ph 2-MeNH-4-Pyr 2-Bn-4- (4,5-deH-Pip) 1-3242 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Bn -4- (4,5-deH-Pip) 1-3243 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Bn-4- (4,5-deH-Pip) 1-3244 4 -F-Ph 2-MeNH-4-Pyr 1-Pr-2-Bn-4- (4,5-deH-Pip) 1-3245 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2 -Bn-4- (4,5-deH-Pip) 1-3246 4-F-Ph 2- MeNH-4-Pyr 1-Phet-2-Bn-4- (4,5-deH-Pip) 1-3247 4-F-Ph 2-MeNH-4-Pyr 2-Phet-4- (4,5- deH-Pip) 1-3248 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Phet-4- (4,5-deH-Pip) 1-3249 4-F-Ph 2-MeNH- 4-Pyr 1-Et-2-Phet-4- (4,5-deH-Pip) 1-3250 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2-Phet-4- (4, 5-deH-Pip) 1-3251 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Phet-4- (4,5-deH-Pip) 1-3252 4-F-Ph 2- MeNH-4-Pyr 1,2-diPhet-4- (4,5-deH-Pip) 1-3253 Ph 4-Pyr 7- (1,2,3,5,6,8a-hexaH-Ind) 1- 3254 Ph 4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 1-3255 3-F-Ph 4-Pyr 7- (1,2,3,5,6,8a- hexaH-Ind) 1-3256 3-F-Ph 4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 1-3257 3-Cl-Ph 4-Pyr 7- (1, 2,3,5,6,8a-hexaH-Ind) 1-3258 3-Cl-Ph 4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 1-3259 3,4 -diF-Ph 4-Pyr 7- (1,2,3,5,6,8a-hexaH-Ind) 1-3260 3,4-diF-Ph 4-Pyr 7- (1,2,3,5, 8,8a-hexaH-Ind) 1-3261 3-CF _Three -Ph 4-Pyr 7- (1,2,3,5,6,8a-hexaH-Ind) 1-3262 3-CF _Three -Ph 4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 1-3263 4-F-Ph 4-Pyr 2-Pyrd-CH = CH- 1-3264 4-F- Ph 4-Pyr 1-Me-2-Pyrd-CH = CH- 1-3265 4-F-Ph 4-Pyr 1-Et-2-Pyrd-CH = CH- 1-3266 4-F-Ph 4-Pyr 1-Pr-2-Pyrd-CH = CH- 1-3267 4-F-Ph 4-Pyr 2-Pip-CH = CH- 1-3268 4-F-Ph 4-Pyr 1-Me-2-Pip- CH = CH- 1-3269 4-F-Ph 4-Pyr 1-Et-2-Pip-CH = CH- 1-3270 4-F-Ph 4-Pyr 1-Pr-2-Pip-CH = CH- 1-3271 Ph 4-Pyr 2-Pyrd-CH = CH- 1-3272 Ph 4-Pyr 1-Me-2-Pyrd-CH = CH- 1-3273 Ph 4-Pyr 1-Et-2-Pyrd-CH = CH- 1-3274 Ph 4-Pyr 1-Pr-2-Pyrd-CH = CH- 1-3275 Ph 4-Pyr 2-Pip-CH = CH- 1-3276 Ph 4-Pyr 1-Me-2- Pip-CH = CH- 1-3277 Ph 4-Pyr 1-Et-2-Pip-CH = CH- 1-3278 Ph 4-Pyr 1-Pr-2-Pip-CH = CH- 1-3279 3-F -Ph 4-Pyr 2-Pyrd-CH = CH- 1-3280 3-F-Ph 4-Pyr 1-Me-2-Pyrd-CH = CH- 1-3281 3-F-Ph 4-Pyr 1-Et -2-Pyrd-CH = CH- 1-3282 3-F-Ph 4-Pyr 1-Pr 2-Pyrd-CH = CH- 1-3283 3-F-Ph 4-Pyr 2-Pip-CH = CH -1-3284 3-F-Ph 4-Pyr 1-Me-2-Pip-CH = CH- 1-3285 3-F-Ph 4-Pyr 1-Et-2-Pip-CH = CH- 1-3286 3-F-Ph 4-Pyr 1-Pr-2-Pip-CH = CH- 1-3287 3-Cl-Ph 4-Pyr 2-Pyrd-CH = CH- 1-3288 3-Cl-Ph 4-Pyr 1-Me-2-Pyrd-CH = CH- 1-3289 3-Cl-Ph 4-Pyr 1-Et- 2-Pyrd-CH = CH- 1-3290 3-Cl-Ph 4-Pyr 1-Pr-2-Pyrd-CH = CH- 1-3291 3-Cl-Ph 4-Pyr 2-Pip-CH = CH- 1-3292 3-Cl-Ph 4-Pyr 1-Me-2-Pip-CH = CH- 1-3293 3-Cl-Ph 4-Pyr 1-Et-2-Pip-CH = CH- 1-3294 3 -Cl-Ph 4-Pyr 1-Pr-2-Pip-CH = CH- 1-3295 3,4-diF-Ph 4-Pyr 2-Pyrd-CH = CH- 1-3296 3,4-diF-Ph 4-Pyr 1-Me-2-Pyrd-CH = CH- 1-3297 3,4-diF-Ph 4-Pyr 1-Et-2-Pyrd-CH = CH- 1-3298 3,4-diF-Ph 4-Pyr 1-Pr-2-Pyrd-CH = CH- 1-3299 3,4-diF-Ph 4-Pyr 2-Pip-CH = CH- 1-3300 3,4-diF-Ph 4-Pyr 1 -Me-2-Pip-CH = CH- 1-3301 3,4-diF-Ph 4-Pyr 1-Et-2-Pip-CH = CH- 1-3302 3,4-diF-Ph 4-Pyr 1 -Pr-2-Pip-CH = CH- 1-3303 3-CF _Three -Ph 4-Pyr 2-Pyrd-CH = CH- 1-3304 3-CF _Three -Ph 4-Pyr 1-Me-2-Pyrd-CH = CH- 1-3305 3-CF _Three -Ph 4-Pyr 1-Et-2-Pyrd-CH = CH- 1-3306 3-CF _Three -Ph 4-Pyr 1-Pr-2-Pyrd-CH = CH- 1-3307 3-CF _Three -Ph 4-Pyr 2-Pip-CH = CH- 1-3308 3-CF _Three -Ph 4-Pyr 1-Me-2-Pip-CH = CH- 1-3309 3-CF _Three -Ph 4-Pyr 1-Et-2-Pip-CH = CH- 1-3310 3-CF _Three -Ph 4-Pyr 1-Pr-2-Pip-CH = CH- ----------------------------------- −−

[0084]

[Table 2]

[0085]

Embedded image

[0086]

[Table 3] Table 2-------------------------------------Compound number R ¹ R ^Two R ^Three −−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−− 2-1 Ph 4-Pyr H _Two N-CH _Two 2-2 Ph 4-Pyr H _Two N- (CH _Two ) _Two 2-3 Ph 4-Pyr H _Two N- (CH _Two ) _Three 2-4 Ph 4-Pyr H _Two N- (CH _Two ) _Four 2-5 Ph 4-Pyr MeNH-CH _Two 2-6 Ph 4-Pyr MeNH- (CH _Two ) _Two 2-7 Ph 4-Pyr MeNH- (CH _Two ) _Three 2-8 Ph 4-Pyr MeNH- (CH _Two ) _Four 2-9 Ph 4-Pyr EtNH-CH _Two 2-10 Ph 4-Pyr EtNH- (CH _Two ) _Two 2-11 Ph 4-Pyr EtNH- (CH _Two ) _Three 2-12 Ph 4-Pyr EtNH- (CH _Two ) _Four 2-13 Ph 4-Pyr Me _Two N-CH _Two 2-14 Ph 4-Pyr Me _Two N- (CH _Two ) _Two 2-15 Ph 4-Pyr Me _Two N- (CH _Two ) _Three 2-16 Ph 4-Pyr Me _Two N- (CH _Two ) _Four 2-17 Ph 4-Pyr 1-Azt-CH _Two 2-18 Ph 4-Pyr 1-Azt- (CH _Two ) _Two 2-19 Ph 4-Pyr 1-Azt- (CH _Two ) _Three 2-20 Ph 4-Pyr 1-Azt- (CH _Two ) _Four 2-21 Ph 4-Pyr 1-Pyrd-CH _Two 2-22 Ph 4-Pyr 1-Pyrd- (CH _Two ) _Two 2-23 Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 2-24 Ph 4-Pyr 1-Pyrd- (CH _Two ) _Four 2-25 Ph 4-Pyr 1-Pip-CH _Two 2-26 Ph 4-Pyr 1-Pip- (CH _Two ) _Two 2-27 Ph 4-Pyr 1-Pip- (CH _Two ) _Three 2-28 Ph 4-Pyr 1-Pip- (CH _Two ) _Four 2-29 Ph 4-Pyr 1-Mor-CH _Two 2-30 Ph 4-Pyr 1-Mor- (CH _Two ) _Two 2-31 Ph 4-Pyr 1-Mor- (CH _Two ) _Three 2-32 Ph 4-Pyr 1-Mor- (CH _Two ) _Four 2-33 Ph 4-Pyr 1-Tmor-CH _Two 2-34 Ph 4-Pyr 1-Tmor- (CH _Two ) _Two 2-35 Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 2-36 Ph 4-Pyr 1-Tmor- (CH _Two ) _Four 2-37 Ph 4-Pyr 1-Piz-CH _Two 2-38 Ph 4-Pyr 1-Piz- (CH _Two ) _Two 2-39 Ph 4-Pyr 1-Piz- (CH _Two ) _Three 2-40 Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-41 Ph 4-Pyr 1-Piz- (CH _Two ) _Four 2-42 Ph 4-Pyr 3-Azt 2-43 Ph 4-Pyr 1-Me-3-Azt 2-44 Ph 4-Pyr 1-Bn-3-Azt 2-45 Ph 4-Pyr 3-Pyrd 2- 46 Ph 4-Pyr 1-Me-3-Pyrd 2-47 Ph 4-Pyr 3-Pip 2-48 Ph 4-Pyr 4-Pip 2-49 Ph 4-Pyr 4- (3,4-deH-Pip) 2-50 Ph 4-Pyr 1-Me-4-Pip 2-51 Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 2-52 Ph 4-Pyr 1-Et-4-Pip 2-53 Ph 4-Pyr 1-Bn-4-Pip 2-54 Ph 4-Pyr 3-Hpip 2-55 Ph 4-Pyr 1-Me-3-Hpip 2-56 Ph 4-Pyr 4-Hpip 2- 57 Ph 4-Pyr 1-Me-4-Hpip 2-58 Ph 4-Pyr 2-Mor 2-59 Ph 4-Pyr 1-Me-2-Mor 2-60 Ph 4-Pyr 2-Tmor 2-61 Ph 4-Pyr 1-Me-2-Tmor 2-62 Ph 4-Pyr 1-Piz 2-63 Ph 4-Pyr 4-Me-1-Piz 2-64 Ph 4-Pyr 2-Piz 2-65 Ph 4- Pyr 4-Pyr 2-66 Ph 4-Pyr 3-Pyr 2-67 Ph 4-Pyr 2-Pyr 2-68 Ph 4-Pyr 4-Pym 2-69 Ph 4-Pyr 5-Pym 2-70 Ph 4- Pyr 2-Pym 2-71 Ph 4-Pyr 3-Azt-CH _Two 2-72 Ph 4-Pyr 1-Me-3-Azt-CH _Two 2-73 Ph 4-Pyr 3-Pyrd-CH _Two 2-74 Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 2-75 Ph 4-Pyr 4-Pip-CH _Two 2-76 Ph 4-Pyr 1-Me-4-Pip-CH _Two 2-77 Ph 4-Pyr 3-Hpip-CH _Two 2-78 Ph 4-Pyr 1-Me-3-Hpip-CH _Two 2-79 Ph 4-Pyr 4-Hpip-CH _Two 2-80 Ph 4-Pyr 1-Me-4-Hpip-CH _Two 2-81 Ph 4-Pyr 2-Mor-CH _Two 2-82 Ph 4-Pyr 1-Me-2-Mor-CH _Two 2-83 Ph 4-Pyr 2-Tmor-CH _Two 2-84 Ph 4-Pyr 1-Me-2-Tmor-CH _Two 2-85 Ph 4-Pyr 1-Piz-CH _Two 2-86 Ph 4-Pyr 4-Me-1-Piz-CH _Two 2-87 Ph 4-Pyr 2-Piz-CH _Two 2-88 Ph 4-Pyr 4-Pyr-CH _Two 2-89 Ph 4-Pyr 3-Pyr-CH _Two 2-90 Ph 4-Pyr 2-Pyr-CH _Two 2-91 Ph 4-Pyr 4-Pym-CH _Two 2-92 Ph 4-Pyr 5-Pym-CH _Two 2-93 Ph 4-Pyr 2-Pym-CH _Two 2-94 Ph 4-Pyr H _Two N-CH _Two CH = CH 2-95 4-F-Ph 4-Pyr H _Two N-CH _Two 2-96 4-F-Ph 4-Pyr H _Two N- (CH _Two ) _Two 2-97 4-F-Ph 4-Pyr H _Two N- (CH _Two ) _Three 2-98 4-F-Ph 4-Pyr H _Two N- (CH _Two ) _Four 2-99 4-F-Ph 4-Pyr MeNH-CH _Two 2-100 4-F-Ph 4-Pyr MeNH- (CH _Two ) _Two 2-101 4-F-Ph 4-Pyr MeNH- (CH _Two ) _Three 2-102 4-F-Ph 4-Pyr MeNH- (CH _Two ) _Four 2-103 4-F-Ph 4-Pyr EtNH-CH _Two 2-104 4-F-Ph 4-Pyr EtNH- (CH _Two ) _Two 2-105 4-F-Ph 4-Pyr EtNH- (CH _Two ) _Three 2-106 4-F-Ph 4-Pyr EtNH- (CH _Two ) _Four 2-107 4-F-Ph 4-Pyr Me _Two N-CH _Two 2-108 4-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Two 2-109 4-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 2-110 4-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Four 2-111 4-F-Ph 4-Pyr 1-Azt-CH _Two 2-112 4-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Two 2-113 4-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 2-114 4-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Four 2-115 4-F-Ph 4-Pyr 1-Pyrd-CH _Two 2-116 4-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Two 2-117 4-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 2-118 4-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Four 2-119 4-F-Ph 4-Pyr 1-Pip-CH _Two 2-120 4-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Two 2-121 4-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 2-122 4-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Four 2-123 4-F-Ph 4-Pyr 1-Mor-CH _Two 2-124 4-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Two 2-125 4-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 2-126 4-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Four 2-127 4-F-Ph 4-Pyr 1-Tmor-CH _Two 2-128 4-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Two 2-129 4-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 2-130 4-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Four 2-131 4-F-Ph 4-Pyr 1-Piz-CH _Two 2-132 4-F-Ph 4-Pyr 1-Piz- (CH _Two ) _Two 2-133 4-F-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 2-134 4-F-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-135 4-F-Ph 4-Pyr 4-Bn-1-Piz- (CH _Two ) _Three 2-136 4-F-Ph 4-Pyr 3-Azt 2-137 4-F-Ph 4-Pyr 1-Me-3-Azt 2-138 4-F-Ph 4-Pyr 1-Bn-3-Azt 2-139 4-F-Ph 4-Pyr 3-Pyrd 2-140 4-F-Ph 4-Pyr 1-Me-3-Pyrd 2-141 4-F-Ph 4-Pyr 3-Pip 2-142 4 -F-Ph 4-Pyr 4-Pip 2-143 4-F-Ph 4-Pyr 4- (3,4-deH-Pip) 2-144 4-F-Ph 4-Pyr 1-Me-4-Pip 2-145 4-F-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 2-146 4-F-Ph 4-Pyr 1-Et-4-Pip 2-147 4-F -Ph 4-Pyr 1-Bn-4-Pip 2-148 4-F-Ph 4-Pyr 3-Hpip 2-149 4-F-Ph 4-Pyr 1-Me-3-Hpip 2-150 4-F -Ph 4-Pyr 4-Hpip 2-151 4-F-Ph 4-Pyr 1-Me-4-Hpip 2-152 4-F-Ph 4-Pyr 2-Mor 2-153 4-F-Ph 4- Pyr 1-Me-2-Mor 2-154 4-F-Ph 4-Pyr 2-Tmor 2-155 4-F-Ph 4-Pyr 1-Me-2-Tmor 2-156 4-F-Ph 4- Pyr 1-Piz 2-157 4-F-Ph 4-Pyr 4-Me-1-Piz 2-158 4-F-Ph 4-Pyr 2-Piz 2-159 4-F-Ph 4-Pyr 4-Pyr 2-160 4-F-Ph 4-Pyr 3-Pyr 2-161 4-F-Ph 4-Pyr 2-Pyr 2-162 4-F-Ph 4-Pyr 4-Pym 2-163 4-F-Ph 4-Pyr 5-Pym 2-164 4-F-Ph 4-Pyr 2-Pym 2-165 4-F-Ph 4-Pyr 3-Azt-CH _Two 2-166 4-F-Ph 4-Pyr 1-Me-3-Azt-CH _Two 2-167 4-F-Ph 4-Pyr 3-Pyrd-CH _Two 2-168 4-F-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 2-169 4-F-Ph 4-Pyr 4-Pip-CH _Two 2-170 4-F-Ph 4-Pyr 1-Me-4-Pip-CH _Two 2-171 4-F-Ph 4-Pyr 3-Hpip-CH _Two 2-172 4-F-Ph 4-Pyr 1-Me-3-Hpip-CH _Two 2-173 4-F-Ph 4-Pyr 4-Hpip-CH _Two 2-174 4-F-Ph 4-Pyr 1-Me-4-Hpip-CH _Two 2-175 4-F-Ph 4-Pyr 2-Mor-CH _Two 2-176 4-F-Ph 4-Pyr 1-Me-2-Mor-CH _Two 2-177 4-F-Ph 4-Pyr 2-Tmor-CH _Two 2-178 4-F-Ph 4-Pyr 1-Me-2-Tmor-CH _Two 2-179 4-F-Ph 4-Pyr 1-Piz-CH _Two 2-180 4-F-Ph 4-Pyr 4-Me-1-Piz-CH _Two 2-181 4-F-Ph 4-Pyr 2-Piz-CH _Two 2-182 4-F-Ph 4-Pyr 4-Pyr-CH _Two 2-183 4-F-Ph 4-Pyr 3-Pyr-CH _Two 2-184 4-F-Ph 4-Pyr 2-Pyr-CH _Two 2-185 4-F-Ph 4-Pyr 4-Pym-CH _Two 2-186 4-F-Ph 4-Pyr 5-Pym-CH _Two 2-187 4-F-Ph 4-Pyr 2-Pym-CH _Two 2-188 3-F-Ph 4-Pyr H _Two N-CH _Two 2-189 3-F-Ph 4-Pyr H _Two N- (CH _Two ) _Two 2-190 3-F-Ph 4-Pyr H _Two N- (CH _Two ) _Three 2-191 3-F-Ph 4-Pyr H _Two N- (CH _Two ) _Four 2-192 3-F-Ph 4-Pyr MeNH-CH _Two 2-193 3-F-Ph 4-Pyr MeNH- (CH _Two ) _Two 2-194 3-F-Ph 4-Pyr MeNH- (CH _Two ) _Three 2-195 3-F-Ph 4-Pyr MeNH- (CH _Two ) _Four 2-196 3-F-Ph 4-Pyr EtNH-CH _Two 2-197 3-F-Ph 4-Pyr EtNH- (CH _Two ) _Two 2-198 3-F-Ph 4-Pyr EtNH- (CH _Two ) _Three 2-199 3-F-Ph 4-Pyr EtNH- (CH _Two ) _Four 2-200 3-F-Ph 4-Pyr Me _Two N-CH _Two 2-201 3-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Two 2-202 3-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 2-203 3-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Four 2-204 3-F-Ph 4-Pyr 1-Azt-CH _Two 2-205 3-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Two 2-206 3-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 2-207 3-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Four 2-208 3-F-Ph 4-Pyr 1-Pyrd-CH _Two 2-209 3-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Two 2-210 3-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 2-211 3-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Four 2-212 3-F-Ph 4-Pyr 1-Pip-CH _Two 2-213 3-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Two 2-214 3-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 2-215 3-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Four 2-216 3-F-Ph 4-Pyr 1-Mor-CH _Two 2-217 3-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Two 2-218 3-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 2-219 3-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Four 2-220 3-F-Ph 4-Pyr 1-Tmor-CH _Two 2-221 3-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Two 2-222 3-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 2-223 3-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Four 2-224 3-F-Ph 4-Pyr 1-Piz-CH _Two 2-225 3-F-Ph 4-Pyr 1-Piz- (CH _Two ) _Two 2-226 3-F-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 2-227 3-F-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-228 3-F-Ph 4-Pyr 1-Piz- (CH _Two ) _Four 2-229 3-F-Ph 4-Pyr 3-Azt 2-230 3-F-Ph 4-Pyr 1-Me-3-Azt 2-231 3-F-Ph 4-Pyr 1-Bn-3-Azt 2-232 3-F-Ph 4-Pyr 3-Pyrd 2-233 3-F-Ph 4-Pyr 1-Me-3-Pyrd 2-234 3-F-Ph 4-Pyr 3-Pip 2-235 3 -F-Ph 4-Pyr 4-Pip 2-236 3-F-Ph 4-Pyr 4- (3,4-deH-Pip) 2-237 3-F-Ph 4-Pyr 1-Me-4-Pip 2-238 3-F-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 2-239 3-F-Ph 4-Pyr 1-Et-4-Pip 2-240 3-F -Ph 4-Pyr 1-Bn-4-Pip 2-241 3-F-Ph 4-Pyr 3-Hpip 2-242 3-F-Ph 4-Pyr 1-Me-3-Hpip 2-243 3-F -Ph 4-Pyr 4-Hpip 2-244 3-F-Ph 4-Pyr 1-Me-4-Hpip 2-245 3-F-Ph 4-Pyr 2-Mor 2-246 3-F-Ph 4- Pyr 1-Me-2-Mor 2-247 3-F-Ph 4-Pyr 2-Tmor 2-248 3-F-Ph 4-Pyr 1-Me-2-Tmor 2-249 3-F-Ph 4- Pyr 1-Piz 2-250 3-F-Ph 4-Pyr 4-Me-1-Piz 2-251 3-F-Ph 4-Pyr 2-Piz 2-252 3-F-Ph 4-Pyr 4-Pyr 2-253 3-F-Ph 4-Pyr 3-Pyr 2-254 3-F-Ph 4-Pyr 2-Pyr 2-255 3-F-Ph 4-Pyr 4-Pym 2-256 3-F-Ph 4-Pyr 5-Pym 2-257 3-F-Ph 4-Pyr 2-Pym 2-258 3-F-Ph 4-Pyr 3-Azt-CH _Two 2-259 3-F-Ph 4-Pyr 1-Me-3-Azt-CH _Two 2-260 3-F-Ph 4-Pyr 3-Pyrd-CH _Two 2-261 3-F-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 2-262 3-F-Ph 4-Pyr 4-Pip-CH _Two 2-263 3-F-Ph 4-Pyr 1-Me-4-Pip-CH _Two 2-264 3-F-Ph 4-Pyr 3-Hpip-CH _Two 2-265 3-F-Ph 4-Pyr 1-Me-3-Hpip-CH _Two 2-266 3-F-Ph 4-Pyr 4-Hpip-CH _Two 2-267 3-F-Ph 4-Pyr 1-Me-4-Hpip-CH _Two 2-268 3-F-Ph 4-Pyr 2-Mor-CH _Two 2-269 3-F-Ph 4-Pyr 1-Me-2-Mor-CH _Two 2-270 3-F-Ph 4-Pyr 2-Tmor-CH _Two 2-271 3-F-Ph 4-Pyr 1-Me-2-Tmor-CH _Two 2-272 3-F-Ph 4-Pyr 1-Piz-CH _Two 2-273 3-F-Ph 4-Pyr 4-Me-1-Piz-CH _Two 2-274 3-F-Ph 4-Pyr 2-Piz-CH _Two 2-275 3-F-Ph 4-Pyr 4-Pyr-CH _Two 2-276 3-F-Ph 4-Pyr 3-Pyr-CH _Two 2-277 3-F-Ph 4-Pyr 2-Pyr-CH _Two 2-278 3-F-Ph 4-Pyr 4-Pym-CH _Two 2-279 3-F-Ph 4-Pyr 5-Pym-CH _Two 2-280 3-F-Ph 4-Pyr 2-Pym-CH _Two 2-281 3,4-diF-Ph 4-Pyr H _Two N-CH _Two 2-282 3,4-diF-Ph 4-Pyr H _Two N- (CH _Two ) _Two 2-283 3,4-diF-Ph 4-Pyr H _Two N- (CH _Two ) _Three 2-284 3,4-diF-Ph 4-Pyr H _Two N- (CH _Two ) _Four 2-285 3,4-diF-Ph 4-Pyr MeNH-CH _Two 2-286 3,4-diF-Ph 4-Pyr MeNH- (CH _Two ) _Two 2-287 3,4-diF-Ph 4-Pyr MeNH- (CH _Two ) _Three 2-288 3,4-diF-Ph 4-Pyr MeNH- (CH _Two ) _Four 2-289 3,4-diF-Ph 4-Pyr EtNH-CH _Two 2-290 3,4-diF-Ph 4-Pyr EtNH- (CH _Two ) _Two 2-291 3,4-diF-Ph 4-Pyr EtNH- (CH _Two ) _Three 2-292 3,4-diF-Ph 4-Pyr EtNH- (CH _Two ) _Four 2-293 3,4-diF-Ph 4-Pyr Me _Two N-CH _Two 2-294 3,4-diF-Ph 4-Pyr Me _Two N- (CH _Two ) _Two 2-295 3,4-diF-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 2-296 3,4-diF-Ph 4-Pyr Me _Two N- (CH _Two ) _Four 2-297 3,4-diF-Ph 4-Pyr 1-Azt-CH _Two 2-298 3,4-diF-Ph 4-Pyr 1-Azt- (CH _Two ) _Two 2-299 3,4-diF-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 2-300 3,4-diF-Ph 4-Pyr 1-Azt- (CH _Two ) _Four 2-301 3,4-diF-Ph 4-Pyr 1-Pyrd-CH _Two 2-302 3,4-diF-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Two 2-303 3,4-diF-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 2-304 3,4-diF-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Four 2-305 3,4-diF-Ph 4-Pyr 1-Pip-CH _Two 2-306 3,4-diF-Ph 4-Pyr 1-Pip- (CH _Two ) _Two 2-307 3,4-diF-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 2-308 3,4-diF-Ph 4-Pyr 1-Pip- (CH _Two ) _Four 2-309 3,4-diF-Ph 4-Pyr 1-Mor-CH _Two 2-310 3,4-diF-Ph 4-Pyr 1-Mor- (CH _Two ) _Two 2-311 3,4-diF-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 2-312 3,4-diF-Ph 4-Pyr 1-Mor- (CH _Two ) _Four 2-313 3,4-diF-Ph 4-Pyr 1-Tmor-CH _Two 2-314 3,4-diF-Ph 4-Pyr 1-Tmor- (CH _Two ) _Two 2-315 3,4-diF-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 2-316 3,4-diF-Ph 4-Pyr 1-Tmor- (CH _Two ) _Four 2-317 3,4-diF-Ph 4-Pyr 1-Piz-CH _Two 2-318 3,4-diF-Ph 4-Pyr 1-Piz- (CH _Two ) _Two 2-319 3,4-diF-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 2-320 3,4-diF-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-321 3,4-diF-Ph 4-Pyr 1-Piz- (CH _Two ) _Four 2-322 3,4-diF-Ph 4-Pyr 3-Azt 2-323 3,4-diF-Ph 4-Pyr 1-Me-3-Azt 2-324 3,4-diF-Ph 4-Pyr 1 -Bn-3-Azt 2-325 3,4-diF-Ph 4-Pyr 3-Pyrd 2-326 3,4-diF-Ph 4-Pyr 1-Me-3-Pyrd 2-327 3,4-diF -Ph 4-Pyr 3-Pip 2-328 3,4-diF-Ph 4-Pyr 4-Pip 2-329 3,4-diF-Ph 4-Pyr 4- (3,4-deH-Pip) 2- 330 3,4-diF-Ph 4-Pyr 1-Me-4-Pip 2-331 3,4-diF-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 2-332 3 , 4-diF-Ph 4-Pyr 1-Et-4-Pip 2-333 3,4-diF-Ph 4-Pyr 1-Bn-4-Pip 2-334 3,4-diF-Ph 4-Pyr 3 -Hpip 2-335 3,4-diF-Ph 4-Pyr 1-Me-3-Hpip 2-336 3,4-diF-Ph 4-Pyr 4-Hpip 2-337 3,4-diF-Ph 4- Pyr 1-Me-4-Hpip 2-338 3,4-diF-Ph 4-Pyr 2-Mor 2-339 3,4-diF-Ph 4-Pyr 1-Me-2-Mor 2-340 3,4 -diF-Ph 4-Pyr 2-Tmor 2-341 3,4-diF-Ph 4-Pyr 1-Me-2-Tmor 2-342 3,4-diF-Ph 4-Pyr 1-Piz 2-343 3 , 4-diF-Ph 4-Pyr 4-Me-1-Piz 2-344 3,4-diF-Ph 4-Pyr 2-Piz 2-345 3,4-diF-Ph 4-Pyr 4-Pyr 2- 346 3,4-diF-Ph 4-Pyr 3-Pyr 2-347 3,4-diF-Ph 4-Pyr 2-Pyr 2-348 3,4-diF-Ph 4-Pyr 4-Pym 2-349 3 , 4-diF-Ph 4-Pyr 5-Pym 2-350 3,4-diF-Ph 4-Pyr 2-Pym 2-351 3,4-diF-Ph 4-Pyr 3-Azt-CH _Two 2-352 3,4-diF-Ph 4-Pyr 1-Me-3-Azt-CH _Two 2-353 3,4-diF-Ph 4-Pyr 3-Pyrd-CH _Two 2-354 3,4-diF-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 2-355 3,4-diF-Ph 4-Pyr 4-Pip-CH _Two 2-356 3,4-diF-Ph 4-Pyr 1-Me-4-Pip-CH _Two 2-357 3,4-diF-Ph 4-Pyr 3-Hpip-CH _Two 2-358 3,4-diF-Ph 4-Pyr 1-Me-3-Hpip-CH _Two 2-359 3,4-diF-Ph 4-Pyr 4-Hpip-CH _Two 2-360 3,4-diF-Ph 4-Pyr 1-Me-4-Hpip-CH _Two 2-361 3,4-diF-Ph 4-Pyr 2-Mor-CH _Two 2-362 3,4-diF-Ph 4-Pyr 1-Me-2-Mor-CH _Two 2-363 3,4-diF-Ph 4-Pyr 2-Tmor-CH _Two 2-364 3,4-diF-Ph 4-Pyr 1-Me-2-Tmor-CH _Two 2-365 3,4-diF-Ph 4-Pyr 1-Piz-CH _Two 2-366 3,4-diF-Ph 4-Pyr 4-Me-1-Piz-CH _Two 2-367 3,4-diF-Ph 4-Pyr 2-Piz-CH _Two 2-368 3,4-diF-Ph 4-Pyr 4-Pyr-CH _Two 2-369 3,4-diF-Ph 4-Pyr 3-Pyr-CH _Two 2-370 3,4-diF-Ph 4-Pyr 2-Pyr-CH _Two 2-371 3,4-diF-Ph 4-Pyr 4-Pym-CH _Two 2-372 3,4-diF-Ph 4-Pyr 5-Pym-CH _Two 2-373 3,4-diF-Ph 4-Pyr 2-Pym-CH _Two 2-374 3-Cl-Ph 4-Pyr H _Two N-CH _Two 2-375 3-Cl-Ph 4-Pyr H _Two N- (CH _Two ) _Two 2-376 3-Cl-Ph 4-Pyr H _Two N- (CH _Two ) _Three 2-377 3-Cl-Ph 4-Pyr H _Two N- (CH _Two ) _Four 2-378 3-Cl-Ph 4-Pyr MeNH-CH _Two 2-379 3-Cl-Ph 4-Pyr MeNH- (CH _Two ) _Two 2-380 3-Cl-Ph 4-Pyr MeNH- (CH _Two ) _Three 2-381 3-Cl-Ph 4-Pyr MeNH- (CH _Two ) _Four 2-382 3-Cl-Ph 4-Pyr EtNH-CH _Two 2-383 3-Cl-Ph 4-Pyr EtNH- (CH _Two ) _Two 2-384 3-Cl-Ph 4-Pyr EtNH- (CH _Two ) _Three 2-385 3-Cl-Ph 4-Pyr EtNH- (CH _Two ) _Four 2-386 3-Cl-Ph 4-Pyr Me _Two N-CH _Two 2-387 3-Cl-Ph 4-Pyr Me _Two N- (CH _Two ) _Two 2-388 3-Cl-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 2-389 3-Cl-Ph 4-Pyr Me _Two N- (CH _Two ) _Four 2-390 3-Cl-Ph 4-Pyr 1-Azt-CH _Two 2-391 3-Cl-Ph 4-Pyr 1-Azt- (CH _Two ) _Two 2-392 3-Cl-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 2-393 3-Cl-Ph 4-Pyr 1-Azt- (CH _Two ) _Four 2-394 3-Cl-Ph 4-Pyr 1-Pyrd-CH _Two 2-395 3-Cl-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Two 2-396 3-Cl-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 2-397 3-Cl-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Four 2-398 3-Cl-Ph 4-Pyr 1-Pip-CH _Two 2-399 3-Cl-Ph 4-Pyr 1-Pip- (CH _Two ) _Two 2-400 3-Cl-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 2-401 3-Cl-Ph 4-Pyr 1-Pip- (CH _Two ) _Four 2-402 3-Cl-Ph 4-Pyr 1-Mor-CH _Two 2-403 3-Cl-Ph 4-Pyr 1-Mor- (CH _Two ) _Two 2-404 3-Cl-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 2-405 3-Cl-Ph 4-Pyr 1-Mor- (CH _Two ) _Four 2-406 3-Cl-Ph 4-Pyr 1-Tmor-CH _Two 2-407 3-Cl-Ph 4-Pyr 1-Tmor- (CH _Two ) _Two 2-408 3-Cl-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 2-409 3-Cl-Ph 4-Pyr 1-Tmor- (CH _Two ) _Four 2-410 3-Cl-Ph 4-Pyr 1-Piz-CH _Two 2-411 3-Cl-Ph 4-Pyr 1-Piz- (CH _Two ) _Two 2-412 3-Cl-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 2-413 3-Cl-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-414 3-Cl-Ph 4-Pyr 1-Piz- (CH _Two ) _Four 2-415 3-Cl-Ph 4-Pyr 3-Azt 2-416 3-Cl-Ph 4-Pyr 1-Me-3-Azt 2-417 3-Cl-Ph 4-Pyr 1-Bn-3-Azt 2-418 3-Cl-Ph 4-Pyr 3-Pyrd 2-419 3-Cl-Ph 4-Pyr 1-Me-3-Pyrd 2-420 3-Cl-Ph 4-Pyr 3-Pip 2-421 3 -Cl-Ph 4-Pyr 4-Pip 2-422 3-Cl-Ph 4-Pyr 4- (3,4-deH-Pip) 2-423 3-Cl-Ph 4-Pyr 1-Me-4-Pip 2-424 3-Cl-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 2-425 3-Cl-Ph 4-Pyr 1-Et-4-Pip 2-426 3-Cl -Ph 4-Pyr 1-Bn-4-Pip 2-427 3-Cl-Ph 4-Pyr 3-Hpip 2-428 3-Cl-Ph 4-Pyr 1-Me-3-Hpip 2-429 3-Cl -Ph 4-Pyr 4-Hpip 2-430 3-Cl-Ph 4-Pyr 1-Me-4-Hpip 2-431 3-Cl-Ph 4-Pyr 2-Mor 2-432 3-Cl-Ph 4- Pyr 1-Me-2-Mor 2-433 3-Cl-Ph 4-Pyr 2-Tmor 2-434 3-Cl-Ph 4-Pyr 1-Me-2-Tmor 2-435 3-Cl-Ph 4- Pyr 1-Piz 2-436 3-Cl-Ph 4-Pyr 4-Me-1-Piz 2-437 3-Cl-Ph 4-Pyr 2-Piz 2-438 3-Cl-Ph 4-Pyr 4-Pyr 2-439 3-Cl-Ph 4-Pyr 3-Pyr 2-440 3-Cl-Ph 4-Pyr 2-Pyr 2-441 3-Cl-Ph 4-Pyr 4-Pym 2-442 3-Cl-Ph 4-Pyr 5-Pym 2-443 3-Cl-Ph 4-Pyr 2-Pym 2-444 3-Cl-Ph 4-Pyr 3-Azt-CH _Two 2-445 3-Cl-Ph 4-Pyr 1-Me-3-Azt-CH _Two 2-446 3-Cl-Ph 4-Pyr 3-Pyrd-CH _Two 2-447 3-Cl-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 2-448 3-Cl-Ph 4-Pyr 4-Pip-CH _Two 2-449 3-Cl-Ph 4-Pyr 1-Me-4-Pip-CH _Two 2-450 3-Cl-Ph 4-Pyr 3-Hpip-CH _Two 2-451 3-Cl-Ph 4-Pyr 1-Me-3-Hpip-CH _Two 2-452 3-Cl-Ph 4-Pyr 4-Hpip-CH _Two 2-453 3-Cl-Ph 4-Pyr 1-Me-4-Hpip-CH _Two 2-454 3-Cl-Ph 4-Pyr 2-Mor-CH _Two 2-455 3-Cl-Ph 4-Pyr 1-Me-2-Mor-CH _Two 2-456 3-Cl-Ph 4-Pyr 2-Tmor-CH _Two 2-457 3-Cl-Ph 4-Pyr 1-Me-2-Tmor-CH _Two 2-458 3-Cl-Ph 4-Pyr 1-Piz-CH _Two 2-459 3-Cl-Ph 4-Pyr 4-Me-1-Piz-CH _Two 2-460 3-Cl-Ph 4-Pyr 2-Piz-CH _Two 2-461 3-Cl-Ph 4-Pyr 4-Pyr-CH _Two 2-462 3-Cl-Ph 4-Pyr 3-Pyr-CH _Two 2-463 3-Cl-Ph 4-Pyr 2-Pyr-CH _Two 2-464 3-Cl-Ph 4-Pyr 4-Pym-CH _Two 2-465 3-Cl-Ph 4-Pyr 5-Pym-CH _Two 2-466 3-Cl-Ph 4-Pyr 2-Pym-CH _Two 2-467 Ph 2-NH _Two -4-Pym H _Two N-CH _Two 2-468 Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Two 2-469 Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 2-470 Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Four 2-471 Ph 2-NH _Two -4-Pym MeNH-CH _Two 2-472 Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Two 2-473 Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 2-474 Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Four 2-475 Ph 2-NH _Two -4-Pym EtNH-CH _Two 2-476 Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Two 2-477 Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 2-478 Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Four 2-479 Ph 2-NH _Two -4-Pym Me _Two N-CH _Two 2-480 Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Two 2-481 Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 2-482 Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Four 2-483 Ph 2-NH _Two -4-Pym 1-Azt-CH _Two 2-484 Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Two 2-485 Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 2-486 Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Four 2-487 Ph 2-NH _Two -4-Pym 1-Pyrd-CH _Two 2-488 Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Two 2-489 Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 2-490 Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Four 2-491 Ph 2-NH _Two -4-Pym 1-Pip-CH _Two 2-492 Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Two 2-493 Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 2-494 Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Four 2-495 Ph 2-NH _Two -4-Pym 1-Mor-CH _Two 2-496 Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Two 2-497 Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 2-498 Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Four 2-499 Ph 2-NH _Two -4-Pym 1-Tmor-CH _Two 2-500 Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Two 2-501 Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 2-502 Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Four 2-503 Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 2-504 Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Two 2-505 Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 2-506 Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-507 Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Four 2-508 Ph 2-NH _Two -4-Pym 3-Azt 2-509 Ph 2-NH _Two -4-Pym 1-Me-3-Azt 2-510 Ph 2-NH _Two -4-Pym 1-Bn-3-Azt 2-511 Ph 2-NH _Two -4-Pym 3-Pyrd 2-512 Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 2-513 Ph 2-NH _Two -4-Pym 3-Pip 2-514 Ph 2-NH _Two -4-Pym 4-Pip 2-515 Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 2-516 Ph 2-NH _Two -4-Pym 1-Me-4-Pip 2-517 Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 2-518 Ph 2-NH _Two -4-Pym 1-Et-4-Pip 2-519 Ph 2-NH _Two -4-Pym 1-Bn-4-Pip 2-520 Ph 2-NH _Two -4-Pym 3-Hpip 2-521 Ph 2-NH _Two -4-Pym 1-Me-3-Hpip 2-522 Ph 2-NH _Two -4-Pym 4-Hpip 2-523 Ph 2-NH _Two -4-Pym 1-Me-4-Hpip 2-524 Ph 2-NH _Two -4-Pym 2-Mor 2-525 Ph 2-NH _Two -4-Pym 1-Me-2-Mor 2-526 Ph 2-NH _Two -4-Pym 2-Tmor 2-527 Ph 2-NH _Two -4-Pym 1-Me-2-Tmor 2-528 Ph 2-NH _Two -4-Pym 1-Piz 2-529 Ph 2-NH _Two -4-Pym 4-Me-1-Piz 2-530 Ph 2-NH _Two -4-Pym 2-Piz 2-531 Ph 2-NH _Two -4-Pym 4-Pyr 2-532 Ph 2-NH _Two -4-Pym 3-Pyr 2-533 Ph 2-NH _Two -4-Pym 2-Pyr 2-534 Ph 2-NH _Two -4-Pym 4-Pym 2-535 Ph 2-NH _Two -4-Pym 5-Pym 2-536 Ph 2-NH _Two -4-Pym 2-Pym 2-537 Ph 2-NH _Two -4-Pym 3-Azt-CH _Two 2-538 Ph 2-NH _Two -4-Pym 1-Me-3-Azt-CH _Two 2-539 Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 2-540 Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 2-541 Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 2-542 Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 2-543 Ph 2-NH _Two -4-Pym 3-Hpip-CH _Two 2-544 Ph 2-NH _Two -4-Pym 1-Me-3-Hpip-CH _Two 2-545 Ph 2-NH _Two -4-Pym 4-Hpip-CH _Two 2-546 Ph 2-NH _Two -4-Pym 1-Me-4-Hpip-CH _Two 2-547 Ph 2-NH _Two -4-Pym 2-Mor-CH _Two 2-548 Ph 2-NH _Two -4-Pym 1-Me-2-Mor-CH _Two 2-549 Ph 2-NH _Two -4-Pym 2-Tmor-CH _Two 2-550 Ph 2-NH _Two -4-Pym 1-Me-2-Tmor-CH _Two 2-551 Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 2-552 Ph 2-NH _Two -4-Pym 4-Me-1-Piz-CH _Two 2-553 Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 2-554 Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 2-555 Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 2-556 Ph 2-NH _Two -4-Pym 2-Pyr-CH _Two 2-557 Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 2-558 Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 2-559 Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 2-560 4-F-Ph 2-NH _Two -4-Pym H _Two N-CH _Two 2-561 4-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Two 2-562 4-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 2-563 4-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Four 2-564 4-F-Ph 2-NH _Two -4-Pym MeNH-CH _Two 2-565 4-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Two 2-566 4-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 2-567 4-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Four 2-568 4-F-Ph 2-NH _Two -4-Pym EtNH-CH _Two 2-569 4-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Two 2-570 4-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 2-571 4-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Four 2-572 4-F-Ph 2-NH _Two -4-Pym Me _Two N-CH _Two 2-573 4-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Two 2-574 4-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 2-575 4-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Four 2-576 4-F-Ph 2-NH _Two -4-Pym 1-Azt-CH _Two 2-577 4-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Two 2-578 4-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 2-579 4-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Four 2-580 4-F-Ph 2-NH _Two -4-Pym 1-Pyrd-CH _Two 2-581 4-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Two 2-582 4-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 2-583 4-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Four 2-584 4-F-Ph 2-NH _Two -4-Pym 1-Pip-CH _Two 2-585 4-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Two 2-586 4-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 2-587 4-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Four 2-588 4-F-Ph 2-NH _Two -4-Pym 1-Mor-CH _Two 2-589 4-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Two 2-590 4-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 2-591 4-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Four 2-592 4-F-Ph 2-NH _Two -4-Pym 1-Tmor-CH _Two 2-593 4-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Two 2-594 4-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 2-595 4-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Four 2-596 4-F-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 2-597 4-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Two 2-598 4-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 2-599 4-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-600 4-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Four 2-601 4-F-Ph 2-NH _Two -4-Pym 3-Azt 2-602 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 2-603 4-F-Ph 2-NH _Two -4-Pym 1-Bn-3-Azt 2-604 4-F-Ph 2-NH _Two -4-Pym 3-Pyrd 2-605 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 2-606 4-F-Ph 2-NH _Two -4-Pym 3-Pip 2-607 4-F-Ph 2-NH _Two -4-Pym 4-Pip 2-608 4-F-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 2-609 4-F-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 2-610 4-F-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 2-611 4-F-Ph 2-NH _Two -4-Pym 1-Et-4-Pip 2-612 4-F-Ph 2-NH _Two -4-Pym 1-Bn-4-Pip 2-613 4-F-Ph 2-NH _Two -4-Pym 3-Hpip 2-614 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip 2-615 4-F-Ph 2-NH _Two -4-Pym 4-Hpip 2-616 4-F-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip 2-617 4-F-Ph 2-NH _Two -4-Pym 2-Mor 2-618 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Mor 2-619 4-F-Ph 2-NH _Two -4-Pym 2-Tmor 2-620 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor 2-621 4-F-Ph 2-NH _Two -4-Pym 1-Piz 2-622 4-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 2-623 4-F-Ph 2-NH _Two -4-Pym 2-Piz 2-624 4-F-Ph 2-NH _Two -4-Pym 4-Pyr 2-625 4-F-Ph 2-NH _Two -4-Pym 3-Pyr 2-626 4-F-Ph 2-NH _Two -4-Pym 2-Pyr 2-627 4-F-Ph 2-NH _Two -4-Pym 4-Pym 2-628 4-F-Ph 2-NH _Two -4-Pym 5-Pym 2-629 4-F-Ph 2-NH _Two -4-Pym 2-Pym 2-630 4-F-Ph 2-NH _Two -4-Pym 3-Azt-CH _Two 2-631 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Azt-CH _Two 2-632 4-F-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 2-633 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 2-634 4-F-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 2-635 4-F-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 2-636 4-F-Ph 2-NH _Two -4-Pym 3-Hpip-CH _Two 2-637 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip-CH _Two 2-638 4-F-Ph 2-NH _Two -4-Pym 4-Hpip-CH _Two 2-639 4-F-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip-CH _Two 2-640 4-F-Ph 2-NH _Two -4-Pym 2-Mor-CH _Two 2-641 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Mor-CH _Two 2-642 4-F-Ph 2-NH _Two -4-Pym 2-Tmor-CH _Two 2-643 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor-CH _Two 2-644 4-F-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 2-645 4-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz-CH _Two 2-646 4-F-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 2-647 4-F-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 2-648 4-F-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 2-649 4-F-Ph 2-NH _Two -4-Pym 2-Pyr-CH _Two 2-650 4-F-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 2-651 4-F-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 2-652 4-F-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 2-653 3-F-Ph 2-NH _Two -4-Pym H _Two N-CH _Two 2-654 3-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Two 2-655 3-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 2-656 3-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Four 2-657 3-F-Ph 2-NH _Two -4-Pym MeNH-CH _Two 2-658 3-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Two 2-659 3-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 2-660 3-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Four 2-661 3-F-Ph 2-NH _Two -4-Pym EtNH-CH _Two 2-662 3-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Two 2-663 3-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 2-664 3-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Four 2-665 3-F-Ph 2-NH _Two -4-Pym Me _Two N-CH _Two 2-666 3-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Two 2-667 3-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 2-668 3-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Four 2-669 3-F-Ph 2-NH _Two -4-Pym 1-Azt-CH _Two 2-670 3-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Two 2-671 3-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 2-672 3-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Four 2-673 3-F-Ph 2-NH _Two -4-Pym 1-Pyrd-CH _Two 2-674 3-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Two 2-675 3-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 2-676 3-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Four 2-677 3-F-Ph 2-NH _Two -4-Pym 1-Pip-CH _Two 2-678 3-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Two 2-679 3-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 2-680 3-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Four 2-681 3-F-Ph 2-NH _Two -4-Pym 1-Mor-CH _Two 2-682 3-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Two 2-683 3-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 2-684 3-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Four 2-685 3-F-Ph 2-NH _Two -4-Pym 1-Tmor-CH _Two 2-686 3-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Two 2-687 3-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 2-688 3-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Four 2-689 3-F-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 2-690 3-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Two 2-691 3-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 2-692 3-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-693 3-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Four 2-694 3-F-Ph 2-NH _Two -4-Pym 3-Azt 2-695 3-F-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 2-696 3-F-Ph 2-NH _Two -4-Pym 1-Bn-3-Azt 2-697 3-F-Ph 2-NH _Two -4-Pym 3-Pyrd 2-698 3-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 2-699 3-F-Ph 2-NH _Two -4-Pym 3-Pip 2-700 3-F-Ph 2-NH _Two -4-Pym 4-Pip 2-701 3-F-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 2-702 3-F-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 2-703 3-F-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 2-704 3-F-Ph 2-NH _Two -4-Pym 1-Et-4-Pip 2-705 3-F-Ph 2-NH _Two -4-Pym 1-Bn-4-Pip 2-706 3-F-Ph 2-NH _Two -4-Pym 3-Hpip 2-707 3-F-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip 2-708 3-F-Ph 2-NH _Two -4-Pym 4-Hpip 2-709 3-F-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip 2-710 3-F-Ph 2-NH _Two -4-Pym 2-Mor 2-711 3-F-Ph 2-NH _Two -4-Pym 1-Me-2-Mor 2-712 3-F-Ph 2-NH _Two -4-Pym 2-Tmor 2-713 3-F-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor 2-714 3-F-Ph 2-NH _Two -4-Pym 1-Piz 2-715 3-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 2-716 3-F-Ph 2-NH _Two -4-Pym 2-Piz 2-717 3-F-Ph 2-NH _Two -4-Pym 4-Pyr 2-718 3-F-Ph 2-NH _Two -4-Pym 3-Pyr 2-719 3-F-Ph 2-NH _Two -4-Pym 2-Pyr 2-720 3-F-Ph 2-NH _Two -4-Pym 4-Pym 2-721 3-F-Ph 2-NH _Two -4-Pym 5-Pym 2-722 3-F-Ph 2-NH _Two -4-Pym 2-Pym 2-723 3-F-Ph 2-NH _Two -4-Pym 3-Azt-CH _Two 2-724 3-F-Ph 2-NH _Two -4-Pym 1-Me-3-Azt-CH _Two 2-725 3-F-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 2-726 3-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 2-727 3-F-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 2-728 3-F-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 2-729 3-F-Ph 2-NH _Two -4-Pym 3-Hpip-CH _Two 2-730 3-F-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip-CH _Two 2-731 3-F-Ph 2-NH _Two -4-Pym 4-Hpip-CH _Two 2-732 3-F-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip-CH _Two 2-733 3-F-Ph 2-NH _Two -4-Pym 2-Mor-CH _Two 2-734 3-F-Ph 2-NH _Two -4-Pym 1-Me-2-Mor-CH _Two 2-735 3-F-Ph 2-NH _Two -4-Pym 2-Tmor-CH _Two 2-736 3-F-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor-CH _Two 2-737 3-F-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 2-738 3-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz-CH _Two 2-739 3-F-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 2-740 3-F-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 2-741 3-F-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 2-742 3-F-Ph 2-NH _Two -4-Pym 2-Pyr-CH _Two 2-743 3-F-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 2-744 3-F-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 2-745 3-F-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 2-746 3,4-diF-Ph 2-NH _Two -4-Pym H _Two N-CH _Two 2-747 3,4-diF-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Two 2-748 3,4-diF-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 2-749 3,4-diF-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Four 2-750 3,4-diF-Ph 2-NH _Two -4-Pym MeNH-CH _Two 2-751 3,4-diF-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Two 2-752 3,4-diF-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 2-753 3,4-diF-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Four 2-754 3,4-diF-Ph 2-NH _Two -4-Pym EtNH-CH _Two 2-755 3,4-diF-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Two 2-756 3,4-diF-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 2-757 3,4-diF-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Four 2-758 3,4-diF-Ph 2-NH _Two -4-Pym Me _Two N-CH _Two 2-759 3,4-diF-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Two 2-760 3,4-diF-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 2-761 3,4-diF-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Four 2-762 3,4-diF-Ph 2-NH _Two -4-Pym 1-Azt-CH _Two 2-763 3,4-diF-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Two 2-764 3,4-diF-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 2-765 3,4-diF-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Four 2-766 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pyrd-CH _Two 2-767 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Two 2-768 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 2-769 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Four 2-770 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pip-CH _Two 2-771 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Two 2-772 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 2-773 3,4-diF-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Four 2-774 3,4-diF-Ph 2-NH _Two -4-Pym 1-Mor-CH _Two 2-775 3,4-diF-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Two 2-776 3,4-diF-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 2-777 3,4-diF-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Four 2-778 3,4-diF-Ph 2-NH _Two -4-Pym 1-Tmor-CH _Two 2-779 3,4-diF-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Two 2-780 3,4-diF-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 2-781 3,4-diF-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Four 2-782 3,4-diF-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 2-783 3,4-diF-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Two 2-784 3,4-diF-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 2-785 3,4-diF-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-786 3,4-diF-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Four 2-787 3,4-diF-Ph 2-NH _Two -4-Pym 3-Azt 2-788 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 2-789 3,4-diF-Ph 2-NH _Two -4-Pym 1-Bn-3-Azt 2-790 3,4-diF-Ph 2-NH _Two -4-Pym 3-Pyrd 2-791 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 2-792 3,4-diF-Ph 2-NH _Two -4-Pym 3-Pip 2-793 3,4-diF-Ph 2-NH _Two -4-Pym 4-Pip 2-794 3,4-diF-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 2-795 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 2-796 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 2-797 3,4-diF-Ph 2-NH _Two -4-Pym 1-Et-4-Pip 2-798 3,4-diF-Ph 2-NH _Two -4-Pym 1-Bn-4-Pip 2-799 3,4-diF-Ph 2-NH _Two -4-Pym 3-Hpip 2-800 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip 2-801 3,4-diF-Ph 2-NH _Two -4-Pym 4-Hpip 2-802 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip 2-803 3,4-diF-Ph 2-NH _Two -4-Pym 2-Mor 2-804 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-2-Mor 2-805 3,4-diF-Ph 2-NH _Two -4-Pym 2-Tmor 2-806 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor 2-807 3,4-diF-Ph 2-NH _Two -4-Pym 1-Piz 2-808 3,4-diF-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 2-809 3,4-diF-Ph 2-NH _Two -4-Pym 2-Piz 2-810 3,4-diF-Ph 2-NH _Two -4-Pym 4-Pyr 2-811 3,4-diF-Ph 2-NH _Two -4-Pym 3-Pyr 2-812 3,4-diF-Ph 2-NH _Two -4-Pym 2-Pyr 2-813 3,4-diF-Ph 2-NH _Two -4-Pym 4-Pym 2-814 3,4-diF-Ph 2-NH _Two -4-Pym 5-Pym 2-815 3,4-diF-Ph 2-NH _Two -4-Pym 2-Pym 2-816 3,4-diF-Ph 2-NH _Two -4-Pym 3-Azt-CH _Two 2-817 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-3-Azt-CH _Two 2-818 3,4-diF-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 2-819 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 2-820 3,4-diF-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 2-821 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 2-822 3,4-diF-Ph 2-NH _Two -4-Pym 3-Hpip-CH _Two 2-823 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip-CH _Two 2-824 3,4-diF-Ph 2-NH _Two -4-Pym 4-Hpip-CH _Two 2-825 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip-CH _Two 2-826 3,4-diF-Ph 2-NH _Two -4-Pym 2-Mor-CH _Two 2-827 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-2-Mor-CH _Two 2-828 3,4-diF-Ph 2-NH _Two -4-Pym 2-Tmor-CH _Two 2-829 3,4-diF-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor-CH _Two 2-830 3,4-diF-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 2-831 3,4-diF-Ph 2-NH _Two -4-Pym 4-Me-1-Piz-CH _Two 2-832 3,4-diF-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 2-833 3,4-diF-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 2-834 3,4-diF-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 2-835 3,4-diF-Ph 2-NH _Two -4-Pym 2-Pyr-CH _Two 2-836 3,4-diF-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 2-837 3,4-diF-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 2-838 3,4-diF-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 2-839 3-Cl-Ph 2-NH _Two -4-Pym H _Two N-CH _Two 2-840 3-Cl-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Two 2-841 3-Cl-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 2-842 3-Cl-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Four 2-843 3-Cl-Ph 2-NH _Two -4-Pym MeNH-CH _Two 2-844 3-Cl-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Two 2-845 3-Cl-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 2-846 3-Cl-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Four 2-847 3-Cl-Ph 2-NH _Two -4-Pym EtNH-CH _Two 2-848 3-Cl-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Two 2-849 3-Cl-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 2-850 3-Cl-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Four 2-851 3-Cl-Ph 2-NH _Two -4-Pym Me _Two N-CH _Two 2-852 3-Cl-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Two 2-853 3-Cl-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 2-854 3-Cl-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Four 2-855 3-Cl-Ph 2-NH _Two -4-Pym 1-Azt-CH _Two 2-856 3-Cl-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Two 2-857 3-Cl-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 2-858 3-Cl-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Four 2-859 3-Cl-Ph 2-NH _Two -4-Pym 1-Pyrd-CH _Two 2-860 3-Cl-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Two 2-861 3-Cl-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 2-862 3-Cl-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Four 2-863 3-Cl-Ph 2-NH _Two -4-Pym 1-Pip-CH _Two 2-864 3-Cl-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Two 2-865 3-Cl-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 2-866 3-Cl-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Four 2-867 3-Cl-Ph 2-NH _Two -4-Pym 1-Mor-CH _Two 2-868 3-Cl-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Two 2-869 3-Cl-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 2-870 3-Cl-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Four 2-871 3-Cl-Ph 2-NH _Two -4-Pym 1-Tmor-CH _Two 2-872 3-Cl-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Two 2-873 3-Cl-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 2-874 3-Cl-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Four 2-875 3-Cl-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 2-876 3-Cl-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Two 2-877 3-Cl-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 2-878 3-Cl-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-879 3-Cl-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Four 2-880 3-Cl-Ph 2-NH _Two -4-Pym 3-Azt 2-881 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 2-882 3-Cl-Ph 2-NH _Two -4-Pym 1-Bn-3-Azt 2-883 3-Cl-Ph 2-NH _Two -4-Pym 3-Pyrd 2-884 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 2-885 3-Cl-Ph 2-NH _Two -4-Pym 3-Pip 2-886 3-Cl-Ph 2-NH _Two -4-Pym 4-Pip 2-887 3-Cl-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 2-888 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 2-889 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 2-890 3-Cl-Ph 2-NH _Two -4-Pym 1-Et-4-Pip 2-891 3-Cl-Ph 2-NH _Two -4-Pym 1-Bn-4-Pip 2-892 3-Cl-Ph 2-NH _Two -4-Pym 3-Hpip 2-893 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip 2-894 3-Cl-Ph 2-NH _Two -4-Pym 4-Hpip 2-895 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip 2-896 3-Cl-Ph 2-NH _Two -4-Pym 2-Mor 2-897 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-2-Mor 2-898 3-Cl-Ph 2-NH _Two -4-Pym 2-Tmor 2-899 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor 2-900 3-Cl-Ph 2-NH _Two -4-Pym 1-Piz 2-901 3-Cl-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 2-902 3-Cl-Ph 2-NH _Two -4-Pym 2-Piz 2-903 3-Cl-Ph 2-NH _Two -4-Pym 4-Pyr 2-904 3-Cl-Ph 2-NH _Two -4-Pym 3-Pyr 2-905 3-Cl-Ph 2-NH _Two -4-Pym 2-Pyr 2-906 3-Cl-Ph 2-NH _Two -4-Pym 4-Pym 2-907 3-Cl-Ph 2-NH _Two -4-Pym 5-Pym 2-908 3-Cl-Ph 2-NH _Two -4-Pym 2-Pym 2-909 3-Cl-Ph 2-NH _Two -4-Pym 3-Azt-CH _Two 2-910 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-3-Azt-CH _Two 2-911 3-Cl-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 2-912 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 2-913 3-Cl-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 2-914 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 2-915 3-Cl-Ph 2-NH _Two -4-Pym 3-Hpip-CH _Two 2-916 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-3-Hpip-CH _Two 2-917 3-Cl-Ph 2-NH _Two -4-Pym 4-Hpip-CH _Two 2-918 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-4-Hpip-CH _Two 2-919 3-Cl-Ph 2-NH _Two -4-Pym 2-Mor-CH _Two 2-920 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-2-Mor-CH _Two 2-921 3-Cl-Ph 2-NH _Two -4-Pym 2-Tmor-CH _Two 2-922 3-Cl-Ph 2-NH _Two -4-Pym 1-Me-2-Tmor-CH _Two 2-923 3-Cl-Ph 2-NH _Two -4-Pym 1-Piz-CH _Two 2-924 3-Cl-Ph 2-NH _Two -4-Pym 4-Me-1-Piz-CH _Two 2-925 3-Cl-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 2-926 3-Cl-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 2-927 3-Cl-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 2-928 3-Cl-Ph 2-NH _Two -4-Pym 2-Pyr-CH _Two 2-929 3-Cl-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 2-930 3-Cl-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 2-931 3-Cl-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 2-932 Ph 2-MeNH-4-Pym H _Two N-CH _Two 2-933 Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Two 2-934 Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 2-935 Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Four 2-936 Ph 2-MeNH-4-Pym MeNH-CH _Two 2-937 Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Two 2-938 Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 2-939 Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Four 2-940 Ph 2-MeNH-4-Pym EtNH-CH _Two 2-941 Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Two 2-942 Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 2-943 Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Four 2-944 Ph 2-MeNH-4-Pym Me _Two N-CH _Two 2-945 Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Two 2-946 Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 2-947 Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Four 2-948 Ph 2-MeNH-4-Pym 1-Azt-CH _Two 2-949 Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Two 2-950 Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 2-951 Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Four 2-952 Ph 2-MeNH-4-Pym 1-Pyrd-CH _Two 2-953 Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Two 2-954 Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 2-955 Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Four 2-956 Ph 2-MeNH-4-Pym 1-Pip-CH _Two 2-957 Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Two 2-958 Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 2-959 Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Four 2-960 Ph 2-MeNH-4-Pym 1-Mor-CH _Two 2-961 Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Two 2-962 Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 2-963 Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Four 2-964 Ph 2-MeNH-4-Pym 1-Tmor-CH _Two 2-965 Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Two 2-966 Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 2-967 Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Four 2-968 Ph 2-MeNH-4-Pym 1-Piz-CH _Two 2-969 Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Two 2-970 Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 2-971 Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-972 Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Four 2-973 Ph 2-MeNH-4-Pym 3-Azt 2-974 Ph 2-MeNH-4-Pym 1-Me-3-Azt 2-975 Ph 2-MeNH-4-Pym 1-Bn-3-Azt 2-976 Ph 2-MeNH-4-Pym 3-Pyrd 2-977 Ph 2-MeNH-4-Pym 1-Me-3-Pyrd 2-978 Ph 2-MeNH-4-Pym 3-Pip 2-979 Ph 2-MeNH-4-Pym 4-Pip 2-980 Ph 2-MeNH-4-Pym 4- (3,4-deH-Pip) 2-981 Ph 2-MeNH-4-Pym 1-Me-4-Pip 2-982 Ph 2-MeNH-4-Pym 1-Me-4- (3,4-deH-Pip) 2-983 Ph 2-MeNH-4-Pym 1-Et-4-Pip 2-984 Ph 2- MeNH-4-Pym 1-Bn-4-Pip 2-985 Ph 2-MeNH-4-Pym 3-Hpip 2-986 Ph 2-MeNH-4-Pym 1-Me-3-Hpip 2-987 Ph 2- MeNH-4-Pym 4-Hpip 2-988 Ph 2-MeNH-4-Pym 1-Me-4-Hpip 2-989 Ph 2-MeNH-4-Pym 2-Mor 2-990 Ph 2-MeNH-4- Pym 1-Me-2-Mor 2-991 Ph 2-MeNH-4-Pym 2-Tmor 2-992 Ph 2-MeNH-4-Pym 1-Me-2-Tmor 2-993 Ph 2-MeNH-4- Pym 1-Piz 2-994 Ph 2-MeNH-4-Pym 4-Me-1-Piz 2-995 Ph 2-MeNH-4-Pym 2-Piz 2-996 Ph 2-MeNH-4-Pym 4-Pyr 2-997 Ph 2-MeNH-4-Pym 3-Pyr 2-998 Ph 2-MeNH-4-Pym 2-Pyr 2-999 Ph 2-MeNH-4-Pym 4-Pym 2-1000 Ph 2-MeNH- 4-Pym 5-Pym 2-1001 Ph 2-MeNH-4-Pym 2-Pym 2-1002 Ph 2-MeNH-4-Pym 3-Azt-CH _Two 2-1003 Ph 2-MeNH-4-Pym 1-Me-3-Azt-CH _Two 2-1004 Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 2-1005 Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 2-1006 Ph 2-MeNH-4-Pym 4-Pip-CH _Two 2-1007 Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 2-1008 Ph 2-MeNH-4-Pym 3-Hpip-CH _Two 2-1009 Ph 2-MeNH-4-Pym 1-Me-3-Hpip-CH _Two 2-1010 Ph 2-MeNH-4-Pym 4-Hpip-CH _Two 2-1011 Ph 2-MeNH-4-Pym 1-Me-4-Hpip-CH _Two 2-1012 Ph 2-MeNH-4-Pym 2-Mor-CH _Two 2-1013 Ph 2-MeNH-4-Pym 1-Me-2-Mor-CH _Two 2-1014 Ph 2-MeNH-4-Pym 2-Tmor-CH _Two 2-1015 Ph 2-MeNH-4-Pym 1-Me-2-Tmor-CH _Two 2-1016 Ph 2-MeNH-4-Pym 1-Piz-CH _Two 2-1017 Ph 2-MeNH-4-Pym 4-Me-1-Piz-CH _Two 2-1018 Ph 2-MeNH-4-Pym 2-Piz-CH _Two 2-1019 Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 2-1020 Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 2-1021 Ph 2-MeNH-4-Pym 2-Pyr-CH _Two 2-1022 Ph 2-MeNH-4-Pym 4-Pym-CH _Two 2-1023 Ph 2-MeNH-4-Pym 5-Pym-CH _Two 2-1024 Ph 2-MeNH-4-Pym 2-Pym-CH _Two 2-1025 4-F-Ph 2-MeNH-4-Pym H _Two N-CH _Two 2-1026 4-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Two 2-1027 4-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 2-1028 4-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Four 2-1029 4-F-Ph 2-MeNH-4-Pym MeNH-CH _Two 2-1030 4-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Two 2-1031 4-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 2-1032 4-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Four 2-1033 4-F-Ph 2-MeNH-4-Pym EtNH-CH _Two 2-1034 4-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Two 2-1035 4-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 2-1036 4-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Four 2-1037 4-F-Ph 2-MeNH-4-Pym Me _Two N-CH _Two 2-1038 4-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Two 2-1039 4-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 2-1040 4-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Four 2-1041 4-F-Ph 2-MeNH-4-Pym 1-Azt-CH _Two 2-1042 4-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Two 2-1043 4-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 2-1044 4-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Four 2-1045 4-F-Ph 2-MeNH-4-Pym 1-Pyrd-CH _Two 2-1046 4-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Two 2-1047 4-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 2-1048 4-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Four 2-1049 4-F-Ph 2-MeNH-4-Pym 1-Pip-CH _Two 2-1050 4-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Two 2-1051 4-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 2-1052 4-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Four 2-1053 4-F-Ph 2-MeNH-4-Pym 1-Mor-CH _Two 2-1054 4-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Two 2-1055 4-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 2-1056 4-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Four 2-1057 4-F-Ph 2-MeNH-4-Pym 1-Tmor-CH _Two 2-1058 4-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Two 2-1059 4-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 2-1060 4-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Four 2-1061 4-F-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 2-1062 4-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Two 2-1063 4-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 2-1064 4-F-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-1065 4-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Four 2-1066 4-F-Ph 2-MeNH-4-Pym 3-Azt 2-1067 4-F-Ph 2-MeNH-4-Pym 1-Me-3-Azt 2-1068 4-F-Ph 2- MeNH-4-Pym 1-Bn-3-Azt 2-1069 4-F-Ph 2-MeNH-4-Pym 3-Pyrd 2-1070 4-F-Ph 2-MeNH-4-Pym 1-Me-3 -Pyrd 2-1071 4-F-Ph 2-MeNH-4-Pym 3-Pip 2-1072 4-F-Ph 2-MeNH-4-Pym 4-Pip 2-1073 4-F-Ph 2-MeNH- 4-Pym 4- (3,4-deH-Pip) 2-1074 4-F-Ph 2-MeNH-4-Pym 1-Me-4-Pip 2-1075 4-F-Ph 2-MeNH-4- Pym 1-Me-4- (3,4-deH-Pip) 2-1076 4-F-Ph 2-MeNH-4-Pym 1-Et-4-Pip 2-1077 4-F-Ph 2-MeNH- 4-Pym 1-Bn-4-Pip 2-1078 4-F-Ph 2-MeNH-4-Pym 3-Hpip 2-1079 4-F-Ph 2-MeNH-4-Pym 1-Me-3-Hpip 2-1080 4-F-Ph 2-MeNH-4-Pym 4-Hpip 2-1081 4-F-Ph 2-MeNH-4-Pym 1-Me-4-Hpip 2-1082 4-F-Ph 2- MeNH-4-Pym 2-Mor 2-1083 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Mor 2-1084 4-F-Ph 2-MeNH-4-Pym 2-Tmor 2- 1085 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Tmor 2-1086 4-F-Ph 2-MeNH-4-Pym 1-Piz 2-1087 4-F-Ph 2-MeNH- 4-Pym 4-Me-1-Piz 2-1088 4-F-Ph 2-MeNH-4-Pym 2-Piz 2-1089 4-F-Ph 2-MeNH-4-Pym 4-Pyr 2-1090 4 -F-Ph 2-MeNH-4-Pym 3-Pyr 2-1091 4-F-Ph 2-MeNH-4-Pym 2-Pyr 2-1092 4-F-Ph 2-MeNH-4-Pym 4-Pym 2-1093 4-F-Ph 2-MeNH- 4-Pym 5-Pym 2-1094 4-F-Ph 2-MeNH-4-Pym 2-Pym 2-1095 4-F-Ph 2-MeNH-4-Pym 3-Azt-CH _Two 2-1096 4-F-Ph 2-MeNH-4-Pym 1-Me-3-Azt-CH _Two 2-1097 4-F-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 2-1098 4-F-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 2-1099 4-F-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 2-1100 4-F-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 2-1101 4-F-Ph 2-MeNH-4-Pym 3-Hpip-CH _Two 2-1102 4-F-Ph 2-MeNH-4-Pym 1-Me-3-Hpip-CH _Two 2-1103 4-F-Ph 2-MeNH-4-Pym 4-Hpip-CH _Two 2-1104 4-F-Ph 2-MeNH-4-Pym 1-Me-4-Hpip-CH _Two 2-1105 4-F-Ph 2-MeNH-4-Pym 2-Mor-CH _Two 2-1106 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Mor-CH _Two 2-1107 4-F-Ph 2-MeNH-4-Pym 2-Tmor-CH _Two 2-1108 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Tmor-CH _Two 2-1109 4-F-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 2-1110 4-F-Ph 2-MeNH-4-Pym 4-Me-1-Piz-CH _Two 2-1111 4-F-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 2-1112 4-F-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 2-1113 4-F-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 2-1114 4-F-Ph 2-MeNH-4-Pym 2-Pyr-CH _Two 2-1115 4-F-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 2-1116 4-F-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 2-1117 4-F-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 2-1118 3-F-Ph 2-MeNH-4-Pym H _Two N-CH _Two 2-1119 3-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Two 2-1120 3-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 2-1121 3-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Four 2-1122 3-F-Ph 2-MeNH-4-Pym MeNH-CH _Two 2-1123 3-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Two 2-1124 3-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 2-1125 3-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Four 2-1126 3-F-Ph 2-MeNH-4-Pym EtNH-CH _Two 2-1127 3-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Two 2-1128 3-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 2-1129 3-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Four 2-1130 3-F-Ph 2-MeNH-4-Pym Me _Two N-CH _Two 2-1131 3-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Two 2-1132 3-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 2-1133 3-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Four 2-1134 3-F-Ph 2-MeNH-4-Pym 1-Azt-CH _Two 2-1135 3-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Two 2-1136 3-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 2-1137 3-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Four 2-1138 3-F-Ph 2-MeNH-4-Pym 1-Pyrd-CH _Two 2-1139 3-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Two 2-1140 3-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 2-1141 3-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Four 2-1142 3-F-Ph 2-MeNH-4-Pym 1-Pip-CH _Two 2-1143 3-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Two 2-1144 3-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 2-1145 3-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Four 2-1146 3-F-Ph 2-MeNH-4-Pym 1-Mor-CH _Two 2-1147 3-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Two 2-1148 3-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 2-1149 3-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Four 2-1150 3-F-Ph 2-MeNH-4-Pym 1-Tmor-CH _Two 2-1151 3-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Two 2-1152 3-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 2-1153 3-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Four 2-1154 3-F-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 2-1155 3-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Two 2-1156 3-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 2-1157 3-F-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-1158 3-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Four 2-1159 3-F-Ph 2-MeNH-4-Pym 3-Azt 2-1160 3-F-Ph 2-MeNH-4-Pym 1-Me-3-Azt 2-1161 3-F-Ph 2- MeNH-4-Pym 1-Bn-3-Azt 2-1162 3-F-Ph 2-MeNH-4-Pym 3-Pyrd 2-1163 3-F-Ph 2-MeNH-4-Pym 1-Me-3 -Pyrd 2-1164 3-F-Ph 2-MeNH-4-Pym 3-Pip 2-1165 3-F-Ph 2-MeNH-4-Pym 4-Pip 2-1166 3-F-Ph 2-MeNH- 4-Pym 4- (3,4-deH-Pip) 2-1167 3-F-Ph 2-MeNH-4-Pym 1-Me-4-Pip 2-1168 3-F-Ph 2-MeNH-4- Pym 1-Me-4- (3,4-deH-Pip) 2-1169 3-F-Ph 2-MeNH-4-Pym 1-Et-4-Pip 2-1170 3-F-Ph 2-MeNH- 4-Pym 1-Bn-4-Pip 2-1171 3-F-Ph 2-MeNH-4-Pym 3-Hpip 2-1172 3-F-Ph 2-MeNH-4-Pym 1-Me-3-Hpip 2-1173 3-F-Ph 2-MeNH-4-Pym 4-Hpip 2-1174 3-F-Ph 2-MeNH-4-Pym 1-Me-4-Hpip 2-1175 3-F-Ph 2- MeNH-4-Pym 2-Mor 2-1176 3-F-Ph 2-MeNH-4-Pym 1-Me-2-Mor 2-1177 3-F-Ph 2-MeNH-4-Pym 2-Tmor 2- 1178 3-F-Ph 2-MeNH-4-Pym 1-Me-2-Tmor 2-1179 3-F-Ph 2-MeNH-4-Pym 1-Piz 2-1180 3-F-Ph 2-MeNH- 4-Pym 4-Me-1-Piz 2-1181 3-F-Ph 2-MeNH-4-Pym 2-Piz 2-1182 3-F-Ph 2-MeNH-4-Pym 4-Pyr 2-1183 3 -F-Ph 2-MeNH-4-Pym 3-Pyr 2-1184 3-F-Ph 2-MeNH-4-Pym 2-Pyr 2-1185 3-F-Ph 2-MeNH-4-Pym 4-Pym 2-1186 3-F-Ph 2-MeNH- 4-Pym 5-Pym 2-1187 3-F-Ph 2-MeNH-4-Pym 2-Pym 2-1188 3-F-Ph 2-MeNH-4-Pym 3-Azt-CH _Two 2-1189 3-F-Ph 2-MeNH-4-Pym 1-Me-3-Azt-CH _Two 2-1190 3-F-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 2-1191 3-F-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 2-1192 3-F-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 2-1193 3-F-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 2-1194 3-F-Ph 2-MeNH-4-Pym 3-Hpip-CH _Two 2-1195 3-F-Ph 2-MeNH-4-Pym 1-Me-3-Hpip-CH _Two 2-1196 3-F-Ph 2-MeNH-4-Pym 4-Hpip-CH _Two 2-1197 3-F-Ph 2-MeNH-4-Pym 1-Me-4-Hpip-CH _Two 2-1198 3-F-Ph 2-MeNH-4-Pym 2-Mor-CH _Two 2-1199 3-F-Ph 2-MeNH-4-Pym 1-Me-2-Mor-CH _Two 2-1200 3-F-Ph 2-MeNH-4-Pym 2-Tmor-CH _Two 2-1201 3-F-Ph 2-MeNH-4-Pym 1-Me-2-Tmor-CH _Two 2-1202 3-F-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 2-1203 3-F-Ph 2-MeNH-4-Pym 4-Me-1-Piz-CH _Two 2-1204 3-F-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 2-1205 3-F-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 2-1206 3-F-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 2-1207 3-F-Ph 2-MeNH-4-Pym 2-Pyr-CH _Two 2-1208 3-F-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 2-1209 3-F-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 2-1210 3-F-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 2-1211 3,4-diF-Ph 2-MeNH-4-Pym H _Two N-CH _Two 2-1212 3,4-diF-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Two 2-1213 3,4-diF-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 2-1214 3,4-diF-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Four 2-1215 3,4-diF-Ph 2-MeNH-4-Pym MeNH-CH _Two 2-1216 3,4-diF-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Two 2-1217 3,4-diF-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 2-1218 3,4-diF-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Four 2-1219 3,4-diF-Ph 2-MeNH-4-Pym EtNH-CH _Two 2-1220 3,4-diF-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Two 2-1221 3,4-diF-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 2-1222 3,4-diF-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Four 2-1223 3,4-diF-Ph 2-MeNH-4-Pym Me _Two N-CH _Two 2-1224 3,4-diF-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Two 2-1225 3,4-diF-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 2-1226 3,4-diF-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Four 2-1227 3,4-diF-Ph 2-MeNH-4-Pym 1-Azt-CH _Two 2-1228 3,4-diF-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Two 2-1229 3,4-diF-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 2-1230 3,4-diF-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Four 2-1231 3,4-diF-Ph 2-MeNH-4-Pym 1-Pyrd-CH _Two 2-1232 3,4-diF-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Two 2-1233 3,4-diF-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 2-1234 3,4-diF-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Four 2-1235 3,4-diF-Ph 2-MeNH-4-Pym 1-Pip-CH _Two 2-1236 3,4-diF-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Two 2-1237 3,4-diF-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 2-1238 3,4-diF-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Four 2-1239 3,4-diF-Ph 2-MeNH-4-Pym 1-Mor-CH _Two 2-1240 3,4-diF-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Two 2-1241 3,4-diF-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 2-1242 3,4-diF-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Four 2-1243 3,4-diF-Ph 2-MeNH-4-Pym 1-Tmor-CH _Two 2-1244 3,4-diF-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Two 2-1245 3,4-diF-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 2-1246 3,4-diF-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Four 2-1247 3,4-diF-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 2-1248 3,4-diF-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Two 2-1249 3,4-diF-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 2-1250 3,4-diF-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-1251 3,4-diF-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Four 2-1252 3,4-diF-Ph 2-MeNH-4-Pym 3-Azt 2-1253 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-3-Azt 2-1254 3,4 -diF-Ph 2-MeNH-4-Pym 1-Bn-3-Azt 2-1255 3,4-diF-Ph 2-MeNH-4-Pym 3-Pyrd 2-1256 3,4-diF-Ph 2- MeNH-4-Pym 1-Me-3-Pyrd 2-1257 3,4-diF-Ph 2-MeNH-4-Pym 3-Pip 2-1258 3,4-diF-Ph 2-MeNH-4-Pym 4 -Pip 2-1259 3,4-diF-Ph 2-MeNH-4-Pym 4- (3,4-deH-Pip) 2-1260 3,4-diF-Ph 2-MeNH-4-Pym 1-Me -4-Pip 2-1261 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-4- (3,4-deH-Pip) 2-1262 3,4-diF-Ph 2-MeNH- 4-Pym 1-Et-4-Pip 2-1263 3,4-diF-Ph 2-MeNH-4-Pym 1-Bn-4-Pip 2-1264 3,4-diF-Ph 2-MeNH-4- Pym 3-Hpip 2-1265 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-3-Hpip 2-1266 3,4-diF-Ph 2-MeNH-4-Pym 4-Hpip 2- 1267 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-4-Hpip 2-1268 3,4-diF-Ph 2-MeNH-4-Pym 2-Mor 2-1269 3,4-diF -Ph 2-MeNH-4-Pym 1-Me-2-Mor 2-1270 3,4-diF-Ph 2-MeNH-4-Pym 2-Tmor 2-1271 3,4-diF-Ph 2-MeNH- 4-Pym 1-Me-2-Tmor 2-1272 3,4-diF-Ph 2-MeNH-4-Pym 1-Piz 2-1273 3,4-diF-Ph 2-MeNH-4-Pym 4-Me -1-Piz 2-1274 3,4-diF-Ph 2-MeNH-4-Pym 2-Piz 2-1275 3,4-diF-Ph 2-MeNH-4-Pym 4-Pyr 2-1276 3,4 -diF-Ph 2-MeNH -4-Pym 3-Pyr 2-1277 3,4-diF-Ph 2-MeNH-4-Pym 2-Pyr 2-1278 3,4-diF-Ph 2-MeNH-4-Pym 4-Pym 2-1279 3,4-diF-Ph 2-MeNH-4-Pym 5-Pym 2-1280 3,4-diF-Ph 2-MeNH-4-Pym 2-Pym 2-1281 3,4-diF-Ph 2-MeNH -4-Pym 3-Azt-CH _Two 2-1282 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-3-Azt-CH _Two 2-1283 3,4-diF-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 2-1284 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 2-1285 3,4-diF-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 2-1286 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 2-1287 3,4-diF-Ph 2-MeNH-4-Pym 3-Hpip-CH _Two 2-1288 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-3-Hpip-CH _Two 2-1289 3,4-diF-Ph 2-MeNH-4-Pym 4-Hpip-CH _Two 2-1290 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-4-Hpip-CH _Two 2-1291 3,4-diF-Ph 2-MeNH-4-Pym 2-Mor-CH _Two 2-1292 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-2-Mor-CH _Two 2-1293 3,4-diF-Ph 2-MeNH-4-Pym 2-Tmor-CH _Two 2-1294 3,4-diF-Ph 2-MeNH-4-Pym 1-Me-2-Tmor-CH _Two 2-1295 3,4-diF-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 2-1296 3,4-diF-Ph 2-MeNH-4-Pym 4-Me-1-Piz-CH _Two 2-1297 3,4-diF-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 2-1298 3,4-diF-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 2-1299 3,4-diF-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 2-1300 3,4-diF-Ph 2-MeNH-4-Pym 2-Pyr-CH _Two 2-1301 3,4-diF-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 2-1302 3,4-diF-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 2-1303 3,4-diF-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 2-1304 3-Cl-Ph 2-MeNH-4-Pym H _Two N-CH _Two 2-1305 3-Cl-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Two 2-1306 3-Cl-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 2-1307 3-Cl-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Four 2-1308 3-Cl-Ph 2-MeNH-4-Pym MeNH-CH _Two 2-1309 3-Cl-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Two 2-1310 3-Cl-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 2-1311 3-Cl-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Four 2-1312 3-Cl-Ph 2-MeNH-4-Pym EtNH-CH _Two 2-1313 3-Cl-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Two 2-1314 3-Cl-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 2-1315 3-Cl-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Four 2-1316 3-Cl-Ph 2-MeNH-4-Pym Me _Two N-CH _Two 2-1317 3-Cl-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Two 2-1318 3-Cl-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 2-1319 3-Cl-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Four 2-1320 3-Cl-Ph 2-MeNH-4-Pym 1-Azt-CH _Two 2-1321 3-Cl-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Two 2-1322 3-Cl-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 2-1323 3-Cl-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Four 2-1324 3-Cl-Ph 2-MeNH-4-Pym 1-Pyrd-CH _Two 2-1325 3-Cl-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Two 2-1326 3-Cl-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 2-1327 3-Cl-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Four 2-1328 3-Cl-Ph 2-MeNH-4-Pym 1-Pip-CH _Two 2-1329 3-Cl-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Two 2-1330 3-Cl-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 2-1331 3-Cl-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Four 2-1332 3-Cl-Ph 2-MeNH-4-Pym 1-Mor-CH _Two 2-1333 3-Cl-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Two 2-1334 3-Cl-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 2-1335 3-Cl-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Four 2-1336 3-Cl-Ph 2-MeNH-4-Pym 1-Tmor-CH _Two 2-1337 3-Cl-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Two 2-1338 3-Cl-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 2-1339 3-Cl-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Four 2-1340 3-Cl-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 2-1341 3-Cl-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Two 2-1342 3-Cl-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 2-1343 3-Cl-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-1344 3-Cl-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Four 2-1345 3-Cl-Ph 2-MeNH-4-Pym 3-Azt 2-1346 3-Cl-Ph 2-MeNH-4-Pym 1-Me-3-Azt 2-1347 3-Cl-Ph 2- MeNH-4-Pym 1-Bn-3-Azt 2-1348 3-Cl-Ph 2-MeNH-4-Pym 3-Pyrd 2-1349 3-Cl-Ph 2-MeNH-4-Pym 1-Me-3 -Pyrd 2-1350 3-Cl-Ph 2-MeNH-4-Pym 3-Pip 2-1351 3-Cl-Ph 2-MeNH-4-Pym 4-Pip 2-1352 3-Cl-Ph 2-MeNH- 4-Pym 4- (3,4-deH-Pip) 2-1353 3-Cl-Ph 2-MeNH-4-Pym 1-Me-4-Pip 2-1354 3-Cl-Ph 2-MeNH-4- Pym 1-Me-4- (3,4-deH-Pip) 2-1355 3-Cl-Ph 2-MeNH-4-Pym 1-Et-4-Pip 2-1356 3-Cl-Ph 2-MeNH- 4-Pym 1-Bn-4-Pip 2-1357 3-Cl-Ph 2-MeNH-4-Pym 3-Hpip 2-1358 3-Cl-Ph 2-MeNH-4-Pym 1-Me-3-Hpip 2-1359 3-Cl-Ph 2-MeNH-4-Pym 4-Hpip 2-1360 3-Cl-Ph 2-MeNH-4-Pym 1-Me-4-Hpip 2-1361 3-Cl-Ph 2- MeNH-4-Pym 2-Mor 2-1362 3-Cl-Ph 2-MeNH-4-Pym 1-Me-2-Mor 2-1363 3-Cl-Ph 2-MeNH-4-Pym 2-Tmor 2- 1364 3-Cl-Ph 2-MeNH-4-Pym 1-Me-2-Tmor 2-1365 3-Cl-Ph 2-MeNH-4-Pym 1-Piz 2-1366 3-Cl-Ph 2-MeNH- 4-Pym 4-Me-1-Piz 2-1367 3-Cl-Ph 2-MeNH-4-Pym 2-Piz 2-1368 3-Cl-Ph 2-MeNH-4-Pym 4-Pyr 2-1369 3 -Cl-Ph 2-MeNH-4-Pym 3-Pyr 2-1370 3-Cl-Ph 2-MeNH-4-Pym 2-Pyr 2-1371 3-Cl-Ph 2-MeNH-4-Pym 4-Pym 2-1372 3-Cl-Ph 2-MeNH-4-Pym 5-Pym 2-1373 3-Cl-Ph 2-MeNH-4-Pym 2-Pym 2-1374 3-Cl-Ph 2-MeNH -4-Pym 3-Azt-CH _Two 2-1375 3-Cl-Ph 2-MeNH-4-Pym 1-Me-3-Azt-CH _Two 2-1376 3-Cl-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 2-1377 3-Cl-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 2-1378 3-Cl-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 2-1379 3-Cl-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 2-1380 3-Cl-Ph 2-MeNH-4-Pym 3-Hpip-CH _Two 2-1381 3-Cl-Ph 2-MeNH-4-Pym 1-Me-3-Hpip-CH _Two 2-1382 3-Cl-Ph 2-MeNH-4-Pym 4-Hpip-CH _Two 2-1383 3-Cl-Ph 2-MeNH-4-Pym 1-Me-4-Hpip-CH _Two 2-1384 3-Cl-Ph 2-MeNH-4-Pym 2-Mor-CH _Two 2-1385 3-Cl-Ph 2-MeNH-4-Pym 1-Me-2-Mor-CH _Two 2-1386 3-Cl-Ph 2-MeNH-4-Pym 2-Tmor-CH _Two 2-1387 3-Cl-Ph 2-MeNH-4-Pym 1-Me-2-Tmor-CH _Two 2-1388 3-Cl-Ph 2-MeNH-4-Pym 1-Piz-CH _Two 2-1389 3-Cl-Ph 2-MeNH-4-Pym 4-Me-1-Piz-CH _Two 2-1390 3-Cl-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 2-1391 3-Cl-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 2-1392 3-Cl-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 2-1393 3-Cl-Ph 2-MeNH-4-Pym 2-Pyr-CH _Two 2-1394 3-Cl-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 2-1395 3-Cl-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 2-1396 3-Cl-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 2-1397 3-Cl-4-F-Ph 4-Pyr H _Two N- (CH _Two ) _Three 2-1398 3-Cl-4-F-Ph 4-Pyr MeNH- (CH _Two ) _Three 2-1399 3-Cl-4-F-Ph 4-Pyr EtNH- (CH _Two ) _Three 2-1400 3-Cl-4-F-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 2-1401 3-Cl-4-F-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 2-1402 3-Cl-4-F-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 2-1403 3-Cl-4-F-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 2-1404 3-Cl-4-F-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 2-1405 3-Cl-4-F-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 2-1406 3-Cl-4-F-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 2-1407 3-Cl-4-F-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-1408 3-Cl-4-F-Ph 4-Pyr 3-Azt 2-1409 3-Cl-4-F-Ph 4-Pyr 1-Me-3-Azt 2-1410 3-Cl-4-F -Ph 4-Pyr 3-Pyrd 2-1411 3-Cl-4-F-Ph 4-Pyr 1-Me-3-Pyrd 2-1412 3-Cl-4-F-Ph 4-Pyr 4-Pip 2- 1413 3-Cl-4-F-Ph 4-Pyr 4- (3,4-deH-Pip) 2-1414 3-Cl-4-F-Ph 4-Pyr 1-Me-4-Pip 2-1415 3 -Cl-4-F-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 2-1416 3-Cl-4-F-Ph 4-Pyr 1-Piz 2-1417 3-Cl -4-F-Ph 4-Pyr 4-Me-1-Piz 2-1418 3-Cl-4-F-Ph 4-Pyr 4-Pyr 2-1419 3-Cl-4-F-Ph 4-Pyr 3 -Pyr 2-1420 3-Cl-4-F-Ph 4-Pyr 4-Pym 2-1421 3-Cl-4-F-Ph 4-Pyr 5-Pym 2-1422 3-Cl-4-F-Ph 4-Pyr 3-Pyrd-CH _Two 2-1423 3-Cl-4-F-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 2-1424 3-Cl-4-F-Ph 4-Pyr 4-Pip-CH _Two 2-1425 3-Cl-4-F-Ph 4-Pyr 1-Me-4-Pip-CH _Two 2-1426 3-Cl-4-F-Ph 4-Pyr 2-Piz-CH _Two 2-1427 3-Cl-4-F-Ph 4-Pyr 4-Pyr-CH _Two 2-1428 3-Cl-4-F-Ph 4-Pyr 3-Pyr-CH _Two 2-1429 3-Cl-4-F-Ph 4-Pyr 4-Pym-CH _Two 2-1430 3-Cl-4-F-Ph 4-Pyr 5-Pym-CH _Two 2-1431 3-Cl-4-F-Ph 4-Pyr 2-Pym-CH _Two 2-1432 3,4,5-triF-Ph 4-Pyr H _Two N- (CH _Two ) _Three 2-1433 3,4,5-triF-Ph 4-Pyr MeNH- (CH _Two ) _Three 2-1434 3,4,5-triF-Ph 4-Pyr EtNH- (CH _Two ) _Three 2-1435 3,4,5-triF-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 2-1436 3,4,5-triF-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 2-1437 3,4,5-triF-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 2-1438 3,4,5-triF-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 2-1439 3,4,5-triF-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 2-1440 3,4,5-triF-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 2-1441 3,4,5-triF-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 2-1442 3,4,5-triF-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-1443 3,4,5-triF-Ph 4-Pyr 3-Azt 2-1444 3,4,5-triF-Ph 4-Pyr 1-Me-3-Azt 2-1445 3,4,5-triF -Ph 4-Pyr 3-Pyrd 2-1446 3,4,5-triF-Ph 4-Pyr 1-Me-3-Pyrd 2-1447 3,4,5-triF-Ph 4-Pyr 4-Pip 2- 1448 3,4,5-triF-Ph 4-Pyr 4- (3,4-deH-Pip) 2-1449 3,4,5-triF-Ph 4-Pyr 1-Me-4-Pip 2-1450 3 , 4,5-triF-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 2-1451 3,4,5-triF-Ph 4-Pyr 1-Piz 2-1452 3,4 , 5-triF-Ph 4-Pyr 4-Me-1-Piz 2-1453 3,4,5-triF-Ph 4-Pyr 4-Pyr 2-1454 3,4,5-triF-Ph 4-Pyr 3 -Pyr 2-1455 3,4,5-triF-Ph 4-Pyr 4-Pym 2-1456 3,4,5-triF-Ph 4-Pyr 5-Pym 2-1457 3,4,5-triF-Ph 4-Pyr 3-Pyrd-CH _Two 2-1458 3,4,5-triF-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 2-1459 3,4,5-triF-Ph 4-Pyr 4-Pip-CH _Two 2-1460 3,4,5-triF-Ph 4-Pyr 1-Me-4-Pip-CH _Two 2-1461 3,4,5-triF-Ph 4-Pyr 2-Piz-CH _Two 2-1462 3,4,5-triF-Ph 4-Pyr 4-Pyr-CH _Two 2-1463 3,4,5-triF-Ph 4-Pyr 3-Pyr-CH _Two 2-1464 3,4,5-triF-Ph 4-Pyr 4-Pym-CH _Two 2-1465 3,4,5-triF-Ph 4-Pyr 5-Pym-CH _Two 2-1466 3,4,5-triF-Ph 4-Pyr 2-Pym-CH _Two 2-1467 3-CF _Three -Ph 4-Pyr H _Two N- (CH _Two ) _Three 2-1468 3-CF _Three -Ph 4-Pyr MeNH- (CH _Two ) _Three 2-1469 3-CF _Three -Ph 4-Pyr EtNH- (CH _Two ) _Three 2-1470 3-CF _Three -Ph 4-Pyr Me _Two N- (CH _Two ) _Three 2-1471 3-CF _Three -Ph 4-Pyr 1-Azt- (CH _Two ) _Three 2-1472 3-CF _Three -Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 2-1473 3-CF _Three -Ph 4-Pyr 1-Pip- (CH _Two ) _Three 2-1474 3-CF _Three -Ph 4-Pyr 1-Mor- (CH _Two ) _Three 2-1475 3-CF _Three -Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 2-1476 3-CF _Three -Ph 4-Pyr 1-Piz- (CH _Two ) _Three 2-1477 3-CF _Three -Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-1478 3-CF _Three -Ph 4-Pyr 3-Azt 2-1479 3-CF _Three -Ph 4-Pyr 1-Me-3-Azt 2-1480 3-CF _Three -Ph 4-Pyr 3-Pyrd 2-1481 3-CF _Three -Ph 4-Pyr 1-Me-3-Pyrd 2-1482 3-CF _Three -Ph 4-Pyr 4-Pip 2-1483 3-CF _Three -Ph 4-Pyr 4- (3,4-deH-Pip) 2-1484 3-CF _Three -Ph 4-Pyr 1-Me-4-Pip 2-1485 3-CF _Three -Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 2-1486 3-CF _Three -Ph 4-Pyr 1-Piz 2-1487 3-CF _Three -Ph 4-Pyr 4-Me-1-Piz 2-1488 3-CF _Three -Ph 4-Pyr 4-Pyr 2-1489 3-CF _Three -Ph 4-Pyr 3-Pyr 2-1490 3-CF _Three -Ph 4-Pyr 4-Pym 2-1491 3-CF _Three -Ph 4-Pyr 5-Pym 2-1492 3-CF _Three -Ph 4-Pyr 3-Pyrd-CH _Two 2-1493 3-CF _Three -Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 2-1494 3-CF _Three -Ph 4-Pyr 4-Pip-CH _Two 2-1495 3-CF _Three -Ph 4-Pyr 1-Me-4-Pip-CH _Two 2-1496 3-CF _Three -Ph 4-Pyr 2-Piz-CH _Two 2-1497 3-CF _Three -Ph 4-Pyr 4-Pyr-CH _Two 2-1498 3-CF _Three -Ph 4-Pyr 3-Pyr-CH _Two 2-1499 3-CF _Three -Ph 4-Pyr 4-Pym-CH _Two 2-1500 3-CF _Three -Ph 4-Pyr 5-Pym-CH _Two 2-1501 3-CF _Three -Ph 4-Pyr 2-Pym-CH _Two 2-1502 3-CHF _Two O-Ph 4-Pyr H _Two N- (CH _Two ) _Three 2-1503 3-CHF _Two O-Ph 4-Pyr MeNH- (CH _Two ) _Three 2-1504 3-CHF _Two O-Ph 4-Pyr EtNH- (CH _Two ) _Three 2-1505 3-CHF _Two O-Ph 4-Pyr Me _Two N- (CH _Two ) _Three 2-1506 3-CHF _Two O-Ph 4-Pyr 1-Azt- (CH _Two ) _Three 2-1507 3-CHF _Two O-Ph 4-Pyr 1-Pyrd- (CH _Two ) _Three 2-1508 3-CHF _Two O-Ph 4-Pyr 1-Pip- (CH _Two ) _Three 2-1509 3-CHF _Two O-Ph 4-Pyr 1-Mor- (CH _Two ) _Three 2-1510 3-CHF _Two O-Ph 4-Pyr 1-Tmor- (CH _Two ) _Three 2-1511 3-CHF _Two O-Ph 4-Pyr 1-Piz- (CH _Two ) _Three 2-1512 3-CHF _Two O-Ph 4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-1513 3-CHF _Two O-Ph 4-Pyr 3-Azt 2-1514 3-CHF _Two O-Ph 4-Pyr 1-Me-3-Azt 2-1515 3-CHF _Two O-Ph 4-Pyr 3-Pyrd 2-1516 3-CHF _Two O-Ph 4-Pyr 1-Me-3-Pyrd 2-1517 3-CHF _Two O-Ph 4-Pyr 4-Pip 2-1518 3-CHF _Two O-Ph 4-Pyr 4- (3,4-deH-Pip) 2-1519 3-CHF _Two O-Ph 4-Pyr 1-Me-4-Pip 2-1520 3-CHF _Two O-Ph 4-Pyr 1-Me-4- (3,4-deH-Pip) 2-1521 3-CHF _Two O-Ph 4-Pyr 1-Piz 2-1522 3-CHF _Two O-Ph 4-Pyr 4-Me-1-Piz 2-1523 3-CHF _Two O-Ph 4-Pyr 4-Pyr 2-1524 3-CHF _Two O-Ph 4-Pyr 3-Pyr 2-1525 3-CHF _Two O-Ph 4-Pyr 4-Pym 2-1526 3-CHF _Two O-Ph 4-Pyr 5-Pym 2-1527 3-CHF _Two O-Ph 4-Pyr 3-Pyrd-CH _Two 2-1528 3-CHF _Two O-Ph 4-Pyr 1-Me-3-Pyrd-CH _Two 2-1529 3-CHF _Two O-Ph 4-Pyr 4-Pip-CH _Two 2-1530 3-CHF _Two O-Ph 4-Pyr 1-Me-4-Pip-CH _Two 2-1531 3-CHF _Two O-Ph 4-Pyr 2-Piz-CH _Two 2-1532 3-CHF _Two O-Ph 4-Pyr 4-Pyr-CH _Two 2-1533 3-CHF _Two O-Ph 4-Pyr 3-Pyr-CH _Two 2-1534 3-CHF _Two O-Ph 4-Pyr 4-Pym-CH _Two 2-1535 3-CHF _Two O-Ph 4-Pyr 5-Pym-CH _Two 2-1536 3-CHF _Two O-Ph 4-Pyr 2-Pym-CH _Two 2-1537 3-Cl-4-F-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 2-1538 3-Cl-4-F-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 2-1539 3-Cl-4-F-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 2-1540 3-Cl-4-F-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 2-1541 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 2-1542 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 2-1543 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 2-1544 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 2-1545 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 2-1546 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 2-1547 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-1548 3-Cl-4-F-Ph 2-NH _Two -4-Pym 3-Azt 2-1549 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 2-1550 3-Cl-4-F-Ph 2-NH _Two -4-Pym 3-Pyrd 2-1551 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 2-1552 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Pip 2-1553 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 2-1554 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 2-1555 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 2-1556 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Piz 2-1557 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 2-1558 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Pyr 2-1559 3-Cl-4-F-Ph 2-NH _Two -4-Pym 3-Pyr 2-1560 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Pym 2-1561 3-Cl-4-F-Ph 2-NH _Two -4-Pym 5-Pym 2-1562 3-Cl-4-F-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 2-1563 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 2-1564 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 2-1565 3-Cl-4-F-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 2-1566 3-Cl-4-F-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 2-1567 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 2-1568 3-Cl-4-F-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 2-1569 3-Cl-4-F-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 2-1570 3-Cl-4-F-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 2-1571 3-Cl-4-F-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 2-1572 3,4,5-triF-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 2-1573 3,4,5-triF-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 2-1574 3,4,5-triF-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 2-1575 3,4,5-triF-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 2-1576 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 2-1577 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 2-1578 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 2-1579 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 2-1580 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 2-1581 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 2-1582 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-1583 3,4,5-triF-Ph 2-NH _Two -4-Pym 3-Azt 2-1584 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 2-1585 3,4,5-triF-Ph 2-NH _Two -4-Pym 3-Pyrd 2-1586 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 2-1587 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Pip 2-1588 3,4,5-triF-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 2-1589 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 2-1590 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 2-1591 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Piz 2-1592 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 2-1593 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Pyr 2-1594 3,4,5-triF-Ph 2-NH _Two -4-Pym 3-Pyr 2-1595 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Pym 2-1596 3,4,5-triF-Ph 2-NH _Two -4-Pym 5-Pym 2-1597 3,4,5-triF-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 2-1598 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 2-1599 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 2-1600 3,4,5-triF-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 2-1601 3,4,5-triF-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 2-1602 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 2-1603 3,4,5-triF-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 2-1604 3,4,5-triF-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 2-1605 3,4,5-triF-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 2-1606 3,4,5-triF-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 2-1607 3-CF _Three -Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 2-1608 3-CF _Three -Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 2-1609 3-CF _Three -Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 2-1610 3-CF _Three -Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 2-1611 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 2-1612 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 2-1613 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 2-1614 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 2-1615 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 2-1616 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 2-1617 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-1618 3-CF _Three -Ph 2-NH _Two -4-Pym 3-Azt 2-1619 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Me-3-Azt 2-1620 3-CF _Three -Ph 2-NH _Two -4-Pym 3-Pyrd 2-1621 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 2-1622 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Pip 2-1623 3-CF _Three -Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 2-1624 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Me-4-Pip 2-1625 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 2-1626 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Piz 2-1627 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Me-1-Piz 2-1628 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Pyr 2-1629 3-CF _Three -Ph 2-NH _Two -4-Pym 3-Pyr 2-1630 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Pym 2-1631 3-CF _Three -Ph 2-NH _Two -4-Pym 5-Pym 2-1632 3-CF _Three -Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 2-1633 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 2-1634 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 2-1635 3-CF _Three -Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 2-1636 3-CF _Three -Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 2-1637 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 2-1638 3-CF _Three -Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 2-1639 3-CF _Three -Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 2-1640 3-CF _Three -Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 2-1641 3-CF _Three -Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 2-1642 3-CHF _Two O-Ph 2-NH _Two -4-Pym H _Two N- (CH _Two ) _Three 2-1643 3-CHF _Two O-Ph 2-NH _Two -4-Pym MeNH- (CH _Two ) _Three 2-1644 3-CHF _Two O-Ph 2-NH _Two -4-Pym EtNH- (CH _Two ) _Three 2-1645 3-CHF _Two O-Ph 2-NH _Two -4-Pym Me _Two N- (CH _Two ) _Three 2-1646 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Azt- (CH _Two ) _Three 2-1647 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Pyrd- (CH _Two ) _Three 2-1648 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Pip- (CH _Two ) _Three 2-1649 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Mor- (CH _Two ) _Three 2-1650 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Tmor- (CH _Two ) _Three 2-1651 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Piz- (CH _Two ) _Three 2-1652 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-1653 3-CHF _Two O-Ph 2-NH _Two -4-Pym 3-Azt 2-1654 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Me-3-Azt 2-1655 3-CHF _Two O-Ph 2-NH _Two -4-Pym 3-Pyrd 2-1656 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd 2-1657 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Pip 2-1658 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4- (3,4-deH-Pip) 2-1659 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Me-4-Pip 2-1660 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Me-4- (3,4-deH-Pip) 2-1661 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Piz 2-1662 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Me-1-Piz 2-1663 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Pyr 2-1664 3-CHF _Two O-Ph 2-NH _Two -4-Pym 3-Pyr 2-1665 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Pym 2-1666 3-CHF _Two O-Ph 2-NH _Two -4-Pym 5-Pym 2-1667 3-CHF _Two O-Ph 2-NH _Two -4-Pym 3-Pyrd-CH _Two 2-1668 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Me-3-Pyrd-CH _Two 2-1669 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Pip-CH _Two 2-1670 3-CHF _Two O-Ph 2-NH _Two -4-Pym 1-Me-4-Pip-CH _Two 2-1671 3-CHF _Two O-Ph 2-NH _Two -4-Pym 2-Piz-CH _Two 2-1672 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Pyr-CH _Two 2-1673 3-CHF _Two O-Ph 2-NH _Two -4-Pym 3-Pyr-CH _Two 2-1674 3-CHF _Two O-Ph 2-NH _Two -4-Pym 4-Pym-CH _Two 2-1675 3-CHF _Two O-Ph 2-NH _Two -4-Pym 5-Pym-CH _Two 2-1676 3-CHF _Two O-Ph 2-NH _Two -4-Pym 2-Pym-CH _Two 2-1677 3-Cl-4-F-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 2-1678 3-Cl-4-F-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 2-1679 3-Cl-4-F-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 2-1680 3-Cl-4-F-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 2-1681 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 2-1682 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 2-1683 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 2-1684 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 2-1685 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 2-1686 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 2-1687 3-Cl-4-F-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-1688 3-Cl-4-F-Ph 2-MeNH-4-Pym 3-Azt 2-1689 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Me-3-Azt 2- 1690 3-Cl-4-F-Ph 2-MeNH-4-Pym 3-Pyrd 2-1691 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd 2-1692 3 -Cl-4-F-Ph 2-MeNH-4-Pym 4-Pip 2-1693 3-Cl-4-F-Ph 2-MeNH-4-Pym 4- (3,4-deH-Pip) 2- 1694 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Me-4-Pip 2-1695 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Me-4- ( 3,4-deH-Pip) 2-1696 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Piz 2-1697 3-Cl-4-F-Ph 2-MeNH-4-Pym 4 -Me-1-Piz 2-1698 3-Cl-4-F-Ph 2-MeNH-4-Pym 4-Pyr 2-1699 3-Cl-4-F-Ph 2-MeNH-4-Pym 3-Pyr 2-1700 3-Cl-4-F-Ph 2-MeNH-4-Pym 4-Pym 2-1701 3-Cl-4-F-Ph 2-MeNH-4-Pym 5-Pym 2-1702 3-Cl -4-F-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 2-1703 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 2-1704 3-Cl-4-F-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 2-1705 3-Cl-4-F-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 2-1706 3-Cl-4-F-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 2-1707 3-Cl-4-F-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 2-1708 3-Cl-4-F-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 2-1709 3-Cl-4-F-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 2-1710 3-Cl-4-F-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 2-1711 3-Cl-4-F-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 2-1712 3,4,5-triF-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 2-1713 3,4,5-triF-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 2-1714 3,4,5-triF-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 2-1715 3,4,5-triF-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 2-1716 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 2-1717 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 2-1718 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 2-1719 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 2-1720 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 2-1721 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 2-1722 3,4,5-triF-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-1723 3,4,5-triF-Ph 2-MeNH-4-Pym 3-Azt 2-1724 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Me-3-Azt 2- 1725 3,4,5-triF-Ph 2-MeNH-4-Pym 3-Pyrd 2-1726 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd 2-1727 3 , 4,5-triF-Ph 2-MeNH-4-Pym 4-Pip 2-1728 3,4,5-triF-Ph 2-MeNH-4-Pym 4- (3,4-deH-Pip) 2- 1729 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Me-4-Pip 2-1730 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Me-4- ( 3,4-deH-Pip) 2-1731 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Piz 2-1732 3,4,5-triF-Ph 2-MeNH-4-Pym 4 -Me-1-Piz 2-1733 3,4,5-triF-Ph 2-MeNH-4-Pym 4-Pyr 2-1734 3,4,5-triF-Ph 2-MeNH-4-Pym 3-Pyr 2-1735 3,4,5-triF-Ph 2-MeNH-4-Pym 4-Pym 2-1736 3,4,5-triF-Ph 2-MeNH-4-Pym 5-Pym 2-1737 3,4 , 5-triF-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 2-1738 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 2-1739 3,4,5-triF-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 2-1740 3,4,5-triF-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 2-1741 3,4,5-triF-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 2-1742 3,4,5-triF-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 2-1743 3,4,5-triF-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 2-1744 3,4,5-triF-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 2-1745 3,4,5-triF-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 2-1746 3,4,5-triF-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 2-1747 3-CF _Three -Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 2-1748 3-CF _Three -Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 2-1749 3-CF _Three -Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 2-1750 3-CF _Three -Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 2-1751 3-CF _Three -Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 2-1752 3-CF _Three -Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 2-1753 3-CF _Three -Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 2-1754 3-CF _Three -Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 2-1755 3-CF _Three -Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 2-1756 3-CF _Three -Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 2-1757 3-CF _Three -Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-1758 3-CF _Three -Ph 2-MeNH-4-Pym 3-Azt 2-1759 3-CF _Three -Ph 2-MeNH-4-Pym 1-Me-3-Azt 2-1760 3-CF _Three -Ph 2-MeNH-4-Pym 3-Pyrd 2-1761 3-CF _Three -Ph 2-MeNH-4-Pym 1-Me-3-Pyrd 2-1762 3-CF _Three -Ph 2-MeNH-4-Pym 4-Pip 2-1763 3-CF _Three -Ph 2-MeNH-4-Pym 4- (3,4-deH-Pip) 2-1764 3-CF _Three -Ph 2-MeNH-4-Pym 1-Me-4-Pip 2-1765 3-CF _Three -Ph 2-MeNH-4-Pym 1-Me-4- (3,4-deH-Pip) 2-1766 3-CF _Three -Ph 2-MeNH-4-Pym 1-Piz 2-1767 3-CF _Three -Ph 2-MeNH-4-Pym 4-Me-1-Piz 2-1768 3-CF _Three -Ph 2-MeNH-4-Pym 4-Pyr 2-1769 3-CF _Three -Ph 2-MeNH-4-Pym 3-Pyr 2-1770 3-CF _Three -Ph 2-MeNH-4-Pym 4-Pym 2-1771 3-CF _Three -Ph 2-MeNH-4-Pym 5-Pym 2-1772 3-CF _Three -Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 2-1773 3-CF _Three -Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 2-1774 3-CF _Three -Ph 2-MeNH-4-Pym 4-Pip-CH _Two 2-1775 3-CF _Three -Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 2-1776 3-CF _Three -Ph 2-MeNH-4-Pym 2-Piz-CH _Two 2-1777 3-CF _Three -Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 2-1778 3-CF _Three -Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 2-1779 3-CF _Three -Ph 2-MeNH-4-Pym 4-Pym-CH _Two 2-1780 3-CF _Three -Ph 2-MeNH-4-Pym 5-Pym-CH _Two 2-1781 3-CF _Three -Ph 2-MeNH-4-Pym 2-Pym-CH _Two 2-1782 3-CHF _Two O-Ph 2-MeNH-4-Pym H _Two N- (CH _Two ) _Three 2-1783 3-CHF _Two O-Ph 2-MeNH-4-Pym MeNH- (CH _Two ) _Three 2-1784 3-CHF _Two O-Ph 2-MeNH-4-Pym EtNH- (CH _Two ) _Three 2-1785 3-CHF _Two O-Ph 2-MeNH-4-Pym Me _Two N- (CH _Two ) _Three 2-1786 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Azt- (CH _Two ) _Three 2-1787 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Pyrd- (CH _Two ) _Three 2-1788 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Pip- (CH _Two ) _Three 2-1789 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Mor- (CH _Two ) _Three 2-1790 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Tmor- (CH _Two ) _Three 2-1791 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Piz- (CH _Two ) _Three 2-1792 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-1793 3-CHF _Two O-Ph 2-MeNH-4-Pym 3-Azt 2-1794 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Me-3-Azt 2-1795 3-CHF _Two O-Ph 2-MeNH-4-Pym 3-Pyrd 2-1796 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd 2-1797 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Pip 2-1798 3-CHF _Two O-Ph 2-MeNH-4-Pym 4- (3,4-deH-Pip) 2-1799 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Me-4-Pip 2-1800 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Me-4- (3,4-deH-Pip) 2-1801 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Piz 2-1802 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Me-1-Piz 2-1803 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Pyr 2-1804 3-CHF _Two O-Ph 2-MeNH-4-Pym 3-Pyr 2-1805 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Pym 2-1806 3-CHF _Two O-Ph 2-MeNH-4-Pym 5-Pym 2-1807 3-CHF _Two O-Ph 2-MeNH-4-Pym 3-Pyrd-CH _Two 2-1808 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Me-3-Pyrd-CH _Two 2-1809 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Pip-CH _Two 2-1810 3-CHF _Two O-Ph 2-MeNH-4-Pym 1-Me-4-Pip-CH _Two 2-1811 3-CHF _Two O-Ph 2-MeNH-4-Pym 2-Piz-CH _Two 2-1812 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Pyr-CH _Two 2-1813 3-CHF _Two O-Ph 2-MeNH-4-Pym 3-Pyr-CH _Two 2-1814 3-CHF _Two O-Ph 2-MeNH-4-Pym 4-Pym-CH _Two 2-1815 3-CHF _Two O-Ph 2-MeNH-4-Pym 5-Pym-CH _Two 2-1816 3-CHF _Two O-Ph 2-MeNH-4-Pym 2-Pym-CH _Two 2-1817 Ph 2-NH _Two -4-Pyr H _Two N- (CH _Two ) _Three 2-1818 Ph 2-NH _Two -4-Pyr MeNH- (CH _Two ) _Three 2-1819 Ph 2-NH _Two -4-Pyr EtNH- (CH _Two ) _Three 2-1820 Ph 2-NH _Two -4-Pyr Me _Two N- (CH _Two ) _Three 2-1821 Ph 2-NH _Two -4-Pyr 1-Azt- (CH _Two ) _Three 2-1822 Ph 2-NH _Two -4-Pyr 1-Pyrd- (CH _Two ) _Three 2-1823 Ph 2-NH _Two -4-Pyr 1-Pip- (CH _Two ) _Three 2-1824 Ph 2-NH _Two -4-Pyr 1-Mor- (CH _Two ) _Three 2-1825 Ph 2-NH _Two -4-Pyr 1-Tmor- (CH _Two ) _Three 2-1826 Ph 2-NH _Two -4-Pyr 1-Piz- (CH _Two ) _Three 2-1827 Ph 2-NH _Two -4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-1828 Ph 2-NH _Two -4-Pyr 3-Azt 2-1829 Ph 2-NH _Two -4-Pyr 1-Me-3-Azt 2-1830 Ph 2-NH _Two -4-Pyr 3-Pyrd 2-1831 Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd 2-1832 Ph 2-NH _Two -4-Pyr 4-Pip 2-1833 Ph 2-NH _Two -4-Pyr 4- (3,4-deH-Pip) 2-1834 Ph 2-NH _Two -4-Pyr 1-Me-4-Pip 2-1835 Ph 2-NH _Two -4-Pyr 1-Me-4- (3,4-deH-Pip) 2-1836 Ph 2-NH _Two -4-Pyr 1-Piz 2-1837 Ph 2-NH _Two -4-Pyr 4-Me-1-Piz 2-1838 Ph 2-NH _Two -4-Pyr 4-Pyr 2-1839 Ph 2-NH _Two -4-Pyr 3-Pyr 2-1840 Ph 2-NH _Two -4-Pyr 4-Pym 2-1841 Ph 2-NH _Two -4-Pyr 5-Pym 2-1842 Ph 2-NH _Two -4-Pyr 3-Pyrd-CH _Two 2-1843 Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd-CH _Two 2-1844 Ph 2-NH _Two -4-Pyr 4-Pip-CH _Two 2-1845 Ph 2-NH _Two -4-Pyr 1-Me-4-Pip-CH _Two 2-1846 Ph 2-NH _Two -4-Pyr 2-Piz-CH _Two 2-1847 Ph 2-NH _Two -4-Pyr 4-Pyr-CH _Two 2-1848 Ph 2-NH _Two -4-Pyr 3-Pyr-CH _Two 2-1849 Ph 2-NH _Two -4-Pyr 4-Pym-CH _Two 2-1850 Ph 2-NH _Two -4-Pyr 5-Pym-CH _Two 2-1851 Ph 2-NH _Two -4-Pyr 2-Pym-CH _Two 2-1852 4-F-Ph 2-NH _Two -4-Pyr H _Two N- (CH _Two ) _Three 2-1853 4-F-Ph 2-NH _Two -4-Pyr MeNH- (CH _Two ) _Three 2-1854 4-F-Ph 2-NH _Two -4-Pyr EtNH- (CH _Two ) _Three 2-1855 4-F-Ph 2-NH _Two -4-Pyr Me _Two N- (CH _Two ) _Three 2-1856 4-F-Ph 2-NH _Two -4-Pyr 1-Azt- (CH _Two ) _Three 2-1857 4-F-Ph 2-NH _Two -4-Pyr 1-Pyrd- (CH _Two ) _Three 2-1858 4-F-Ph 2-NH _Two -4-Pyr 1-Pip- (CH _Two ) _Three 2-1859 4-F-Ph 2-NH _Two -4-Pyr 1-Mor- (CH _Two ) _Three 2-1860 4-F-Ph 2-NH _Two -4-Pyr 1-Tmor- (CH _Two ) _Three 2-1861 4-F-Ph 2-NH _Two -4-Pyr 1-Piz- (CH _Two ) _Three 2-1862 4-F-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-1863 4-F-Ph 2-NH _Two -4-Pyr 3-Azt 2-1864 4-F-Ph 2-NH _Two -4-Pyr 1-Me-3-Azt 2-1865 4-F-Ph 2-NH _Two -4-Pyr 3-Pyrd 2-1866 4-F-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd 2-1867 4-F-Ph 2-NH _Two -4-Pyr 4-Pip 2-1868 4-F-Ph 2-NH _Two -4-Pyr 4- (3,4-deH-Pip) 2-1869 4-F-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip 2-1870 4-F-Ph 2-NH _Two -4-Pyr 1-Me-4- (3,4-deH-Pip) 2-1871 4-F-Ph 2-NH _Two -4-Pyr 1-Piz 2-1872 4-F-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz 2-1873 4-F-Ph 2-NH _Two -4-Pyr 4-Pyr 2-1874 4-F-Ph 2-NH _Two -4-Pyr 3-Pyr 2-1875 4-F-Ph 2-NH _Two -4-Pyr 4-Pym 2-1876 4-F-Ph 2-NH _Two -4-Pyr 5-Pym 2-1877 4-F-Ph 2-NH _Two -4-Pyr 3-Pyrd-CH _Two 2-1878 4-F-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd-CH _Two 2-1879 4-F-Ph 2-NH _Two -4-Pyr 4-Pip-CH _Two 2-1880 4-F-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip-CH _Two 2-1881 4-F-Ph 2-NH _Two -4-Pyr 2-Piz-CH _Two 2-1882 4-F-Ph 2-NH _Two -4-Pyr 4-Pyr-CH _Two 2-1883 4-F-Ph 2-NH _Two -4-Pyr 3-Pyr-CH _Two 2-1884 4-F-Ph 2-NH _Two -4-Pyr 4-Pym-CH _Two 2-1885 4-F-Ph 2-NH _Two -4-Pyr 5-Pym-CH _Two 2-1886 4-F-Ph 2-NH _Two -4-Pyr 2-Pym-CH _Two 2-1887 3-F-Ph 2-NH _Two -4-Pyr H _Two N- (CH _Two ) _Three 2-1888 3-F-Ph 2-NH _Two -4-Pyr MeNH- (CH _Two ) _Three 2-1889 3-F-Ph 2-NH _Two -4-Pyr EtNH- (CH _Two ) _Three 2-1890 3-F-Ph 2-NH _Two -4-Pyr Me _Two N- (CH _Two ) _Three 2-1891 3-F-Ph 2-NH _Two -4-Pyr 1-Azt- (CH _Two ) _Three 2-1892 3-F-Ph 2-NH _Two -4-Pyr 1-Pyrd- (CH _Two ) _Three 2-1893 3-F-Ph 2-NH _Two -4-Pyr 1-Pip- (CH _Two ) _Three 2-1894 3-F-Ph 2-NH _Two -4-Pyr 1-Mor- (CH _Two ) _Three 2-1895 3-F-Ph 2-NH _Two -4-Pyr 1-Tmor- (CH _Two ) _Three 2-1896 3-F-Ph 2-NH _Two -4-Pyr 1-Piz- (CH _Two ) _Three 2-1897 3-F-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-1898 3-F-Ph 2-NH _Two -4-Pyr 3-Azt 2-1899 3-F-Ph 2-NH _Two -4-Pyr 1-Me-3-Azt 2-1900 3-F-Ph 2-NH _Two -4-Pyr 3-Pyrd 2-1901 3-F-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd 2-1902 3-F-Ph 2-NH _Two -4-Pyr 4-Pip 2-1903 3-F-Ph 2-NH _Two -4-Pyr 4- (3,4-deH-Pip) 2-1904 3-F-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip 2-1905 3-F-Ph 2-NH _Two -4-Pyr 1-Me-4- (3,4-deH-Pip) 2-1906 3-F-Ph 2-NH _Two -4-Pyr 1-Piz 2-1907 3-F-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz 2-1908 3-F-Ph 2-NH _Two -4-Pyr 4-Pyr 2-1909 3-F-Ph 2-NH _Two -4-Pyr 3-Pyr 2-1910 3-F-Ph 2-NH _Two -4-Pyr 4-Pym 2-1911 3-F-Ph 2-NH _Two -4-Pyr 5-Pym 2-1912 3-F-Ph 2-NH _Two -4-Pyr 3-Pyrd-CH _Two 2-1913 3-F-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd-CH _Two 2-1914 3-F-Ph 2-NH _Two -4-Pyr 4-Pip-CH _Two 2-1915 3-F-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip-CH _Two 2-1916 3-F-Ph 2-NH _Two -4-Pyr 2-Piz-CH _Two 2-1917 3-F-Ph 2-NH _Two -4-Pyr 4-Pyr-CH _Two 2-1918 3-F-Ph 2-NH _Two -4-Pyr 3-Pyr-CH _Two 2-1919 3-F-Ph 2-NH _Two -4-Pyr 4-Pym-CH _Two 2-1920 3-F-Ph 2-NH _Two -4-Pyr 5-Pym-CH _Two 2-1921 3-F-Ph 2-NH _Two -4-Pyr 2-Pym-CH _Two 2-1922 3,4-diF-Ph 2-NH _Two -4-Pyr H _Two N- (CH _Two ) _Three 2-1923 3,4-diF-Ph 2-NH _Two -4-Pyr MeNH- (CH _Two ) _Three 2-1924 3,4-diF-Ph 2-NH _Two -4-Pyr EtNH- (CH _Two ) _Three 2-1925 3,4-diF-Ph 2-NH _Two -4-Pyr Me _Two N- (CH _Two ) _Three 2-1926 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Azt- (CH _Two ) _Three 2-1927 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Pyrd- (CH _Two ) _Three 2-1928 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Pip- (CH _Two ) _Three 2-1929 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Mor- (CH _Two ) _Three 2-1930 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Tmor- (CH _Two ) _Three 2-1931 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Piz- (CH _Two ) _Three 2-1932 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-1933 3,4-diF-Ph 2-NH _Two -4-Pyr 3-Azt 2-1934 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Me-3-Azt 2-1935 3,4-diF-Ph 2-NH _Two -4-Pyr 3-Pyrd 2-1936 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd 2-1937 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Pip 2-1938 3,4-diF-Ph 2-NH _Two -4-Pyr 4- (3,4-deH-Pip) 2-1939 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip 2-1940 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Me-4- (3,4-deH-Pip) 2-1941 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Piz 2-1942 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz 2-1943 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Pyr 2-1944 3,4-diF-Ph 2-NH _Two -4-Pyr 3-Pyr 2-1945 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Pym 2-1946 3,4-diF-Ph 2-NH _Two -4-Pyr 5-Pym 2-1947 3,4-diF-Ph 2-NH _Two -4-Pyr 3-Pyrd-CH _Two 2-1948 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd-CH _Two 2-1949 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Pip-CH _Two 2-1950 3,4-diF-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip-CH _Two 2-1951 3,4-diF-Ph 2-NH _Two -4-Pyr 2-Piz-CH _Two 2-1952 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Pyr-CH _Two 2-1953 3,4-diF-Ph 2-NH _Two -4-Pyr 3-Pyr-CH _Two 2-1954 3,4-diF-Ph 2-NH _Two -4-Pyr 4-Pym-CH _Two 2-1955 3,4-diF-Ph 2-NH _Two -4-Pyr 5-Pym-CH _Two 2-1956 3,4-diF-Ph 2-NH _Two -4-Pyr 2-Pym-CH _Two 2-1957 3-Cl-Ph 2-NH _Two -4-Pyr H _Two N- (CH _Two ) _Three 2-1958 3-Cl-Ph 2-NH _Two -4-Pyr MeNH- (CH _Two ) _Three 2-1959 3-Cl-Ph 2-NH _Two -4-Pyr EtNH- (CH _Two ) _Three 2-1960 3-Cl-Ph 2-NH _Two -4-Pyr Me _Two N- (CH _Two ) _Three 2-1961 3-Cl-Ph 2-NH _Two -4-Pyr 1-Azt- (CH _Two ) _Three 2-1962 3-Cl-Ph 2-NH _Two -4-Pyr 1-Pyrd- (CH _Two ) _Three 2-1963 3-Cl-Ph 2-NH _Two -4-Pyr 1-Pip- (CH _Two ) _Three 2-1964 3-Cl-Ph 2-NH _Two -4-Pyr 1-Mor- (CH _Two ) _Three 2-1965 3-Cl-Ph 2-NH _Two -4-Pyr 1-Tmor- (CH _Two ) _Three 2-1966 3-Cl-Ph 2-NH _Two -4-Pyr 1-Piz- (CH _Two ) _Three 2-1967 3-Cl-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-1968 3-Cl-Ph 2-NH _Two -4-Pyr 3-Azt 2-1969 3-Cl-Ph 2-NH _Two -4-Pyr 1-Me-3-Azt 2-1970 3-Cl-Ph 2-NH _Two -4-Pyr 3-Pyrd 2-1971 3-Cl-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd 2-1972 3-Cl-Ph 2-NH _Two -4-Pyr 4-Pip 2-1973 3-Cl-Ph 2-NH _Two -4-Pyr 4- (3,4-deH-Pip) 2-1974 3-Cl-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip 2-1975 3-Cl-Ph 2-NH _Two -4-Pyr 1-Me-4- (3,4-deH-Pip) 2-1976 3-Cl-Ph 2-NH _Two -4-Pyr 1-Piz 2-1977 3-Cl-Ph 2-NH _Two -4-Pyr 4-Me-1-Piz 2-1978 3-Cl-Ph 2-NH _Two -4-Pyr 4-Pyr 2-1979 3-Cl-Ph 2-NH _Two -4-Pyr 3-Pyr 2-1980 3-Cl-Ph 2-NH _Two -4-Pyr 4-Pym 2-1981 3-Cl-Ph 2-NH _Two -4-Pyr 5-Pym 2-1982 3-Cl-Ph 2-NH _Two -4-Pyr 3-Pyrd-CH _Two 2-1983 3-Cl-Ph 2-NH _Two -4-Pyr 1-Me-3-Pyrd-CH _Two 2-1984 3-Cl-Ph 2-NH _Two -4-Pyr 4-Pip-CH _Two 2-1985 3-Cl-Ph 2-NH _Two -4-Pyr 1-Me-4-Pip-CH _Two 2-1986 3-Cl-Ph 2-NH _Two -4-Pyr 2-Piz-CH _Two 2-1987 3-Cl-Ph 2-NH _Two -4-Pyr 4-Pyr-CH _Two 2-1988 3-Cl-Ph 2-NH _Two -4-Pyr 3-Pyr-CH _Two 2-1989 3-Cl-Ph 2-NH _Two -4-Pyr 4-Pym-CH _Two 2-1990 3-Cl-Ph 2-NH _Two -4-Pyr 5-Pym-CH _Two 2-1991 3-Cl-Ph 2-NH _Two -4-Pyr 2-Pym-CH _Two 2-1992 Ph 2-MeNH-4-Pyr H _Two N- (CH _Two ) _Three 2-1993 Ph 2-MeNH-4-Pyr MeNH- (CH _Two ) _Three 2-1994 Ph 2-MeNH-4-Pyr EtNH- (CH _Two ) _Three 2-1995 Ph 2-MeNH-4-Pyr Me _Two N- (CH _Two ) _Three 2-1996 Ph 2-MeNH-4-Pyr 1-Azt- (CH _Two ) _Three 2-1997 Ph 2-MeNH-4-Pyr 1-Pyrd- (CH _Two ) _Three 2-1998 Ph 2-MeNH-4-Pyr 1-Pip- (CH _Two ) _Three 2-1999 Ph 2-MeNH-4-Pyr 1-Mor- (CH _Two ) _Three 2-2000 Ph 2-MeNH-4-Pyr 1-Tmor- (CH _Two ) _Three 2-2001 Ph 2-MeNH-4-Pyr 1-Piz- (CH _Two ) _Three 2-2002 Ph 2-MeNH-4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-2003 Ph 2-MeNH-4-Pyr 3-Azt 2-2004 Ph 2-MeNH-4-Pyr 1-Me-3-Azt 2-2005 Ph 2-MeNH-4-Pyr 3-Pyrd 2-2006 Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd 2-2007 Ph 2-MeNH-4-Pyr 4-Pip 2-2008 Ph 2-MeNH-4-Pyr 4- (3,4-deH-Pip) 2-2009 Ph 2-MeNH-4-Pyr 1-Me-4-Pip 2-2010 Ph 2-MeNH-4-Pyr 1-Me-4- (3,4-deH-Pip) 2-2011 Ph 2- MeNH-4-Pyr 1-Piz 2-2012 Ph 2-MeNH-4-Pyr 4-Me-1-Piz 2-2013 Ph 2-MeNH-4-Pyr 4-Pyr 2-2014 Ph 2-MeNH-4- Pyr 3-Pyr 2-2015 Ph 2-MeNH-4-Pyr 4-Pym 2-2016 Ph 2-MeNH-4-Pyr 5-Pym 2-2017 Ph 2-MeNH-4-Pyr 3-Pyrd-CH _Two 2-2018 Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd-CH _Two 2-2019 Ph 2-MeNH-4-Pyr 4-Pip-CH _Two 2-2020 Ph 2-MeNH-4-Pyr 1-Me-4-Pip-CH _Two 2-2021 Ph 2-MeNH-4-Pyr 2-Piz-CH _Two 2-2022 Ph 2-MeNH-4-Pyr 4-Pyr-CH _Two 2-2023 Ph 2-MeNH-4-Pyr 3-Pyr-CH _Two 2-2024 Ph 2-MeNH-4-Pyr 4-Pym-CH _Two 2-2025 Ph 2-MeNH-4-Pyr 5-Pym-CH _Two 2-2026 Ph 2-MeNH-4-Pyr 2-Pym-CH _Two 2-2027 4-F-Ph 2-MeNH-4-Pyr H _Two N- (CH _Two ) _Three 2-2028 4-F-Ph 2-MeNH-4-Pyr MeNH- (CH _Two ) _Three 2-2029 4-F-Ph 2-MeNH-4-Pyr EtNH- (CH _Two ) _Three 2-2030 4-F-Ph 2-MeNH-4-Pyr Me _Two N- (CH _Two ) _Three 2-2031 4-F-Ph 2-MeNH-4-Pyr 1-Azt- (CH _Two ) _Three 2-2032 4-F-Ph 2-MeNH-4-Pyr 1-Pyrd- (CH _Two ) _Three 2-2033 4-F-Ph 2-MeNH-4-Pyr 1-Pip- (CH _Two ) _Three 2-2034 4-F-Ph 2-MeNH-4-Pyr 1-Mor- (CH _Two ) _Three 2-2035 4-F-Ph 2-MeNH-4-Pyr 1-Tmor- (CH _Two ) _Three 2-2036 4-F-Ph 2-MeNH-4-Pyr 1-Piz- (CH _Two ) _Three 2-2037 4-F-Ph 2-MeNH-4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-2038 4-F-Ph 2-MeNH-4-Pyr 3-Azt 2-2039 4-F-Ph 2-MeNH-4-Pyr 1-Me-3-Azt 2-2040 4-F-Ph 2- MeNH-4-Pyr 3-Pyrd 2-2041 4-F-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd 2-2042 4-F-Ph 2-MeNH-4-Pyr 4-Pip 2- 2043 4-F-Ph 2-MeNH-4-Pyr 4- (3,4-deH-Pip) 2-2044 4-F-Ph 2-MeNH-4-Pyr 1-Me-4-Pip 2-2045 4 -F-Ph 2-MeNH-4-Pyr 1-Me-4- (3,4-deH-Pip) 2-2046 4-F-Ph 2-MeNH-4-Pyr 1-Piz 2-2047 4-F -Ph 2-MeNH-4-Pyr 4-Me-1-Piz 2-2048 4-F-Ph 2-MeNH-4-Pyr 4-Pyr 2-2049 4-F-Ph 2-MeNH-4-Pyr 3 -Pyr 2-2050 4-F-Ph 2-MeNH-4-Pyr 4-Pym 2-2051 4-F-Ph 2-MeNH-4-Pyr 5-Pym 2-2052 4-F-Ph 2-MeNH- 4-Pyr 3-Pyrd-CH _Two 2-2053 4-F-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd-CH _Two 2-2054 4-F-Ph 2-MeNH-4-Pyr 4-Pip-CH _Two 2-2055 4-F-Ph 2-MeNH-4-Pyr 1-Me-4-Pip-CH _Two 2-2056 4-F-Ph 2-MeNH-4-Pyr 2-Piz-CH _Two 2-2057 4-F-Ph 2-MeNH-4-Pyr 4-Pyr-CH _Two 2-2058 4-F-Ph 2-MeNH-4-Pyr 3-Pyr-CH _Two 2-2059 4-F-Ph 2-MeNH-4-Pyr 4-Pym-CH _Two 2-2060 4-F-Ph 2-MeNH-4-Pyr 5-Pym-CH _Two 2-2061 4-F-Ph 2-MeNH-4-Pyr 2-Pym-CH _Two 2-2062 3-F-Ph 2-MeNH-4-Pyr H _Two N- (CH _Two ) _Three 2-2063 3-F-Ph 2-MeNH-4-Pyr MeNH- (CH _Two ) _Three 2-2064 3-F-Ph 2-MeNH-4-Pyr EtNH- (CH _Two ) _Three 2-2065 3-F-Ph 2-MeNH-4-Pyr Me _Two N- (CH _Two ) _Three 2-2066 3-F-Ph 2-MeNH-4-Pyr 1-Azt- (CH _Two ) _Three 2-2067 3-F-Ph 2-MeNH-4-Pyr 1-Pyrd- (CH _Two ) _Three 2-2068 3-F-Ph 2-MeNH-4-Pyr 1-Pip- (CH _Two ) _Three 2-2069 3-F-Ph 2-MeNH-4-Pyr 1-Mor- (CH _Two ) _Three 2-2070 3-F-Ph 2-MeNH-4-Pyr 1-Tmor- (CH _Two ) _Three 2-2071 3-F-Ph 2-MeNH-4-Pyr 1-Piz- (CH _Two ) _Three 2-2072 3-F-Ph 2-MeNH-4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-2073 3-F-Ph 2-MeNH-4-Pyr 3-Azt 2-2074 3-F-Ph 2-MeNH-4-Pyr 1-Me-3-Azt 2-2075 3-F-Ph 2- MeNH-4-Pyr 3-Pyrd 2-2076 3-F-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd 2-2077 3-F-Ph 2-MeNH-4-Pyr 4-Pip 2- 2078 3-F-Ph 2-MeNH-4-Pyr 4- (3,4-deH-Pip) 2-2079 3-F-Ph 2-MeNH-4-Pyr 1-Me-4-Pip 2-2080 3 -F-Ph 2-MeNH-4-Pyr 1-Me-4- (3,4-deH-Pip) 2-2081 3-F-Ph 2-MeNH-4-Pyr 1-Piz 2-2082 3-F -Ph 2-MeNH-4-Pyr 4-Me-1-Piz 2-2083 3-F-Ph 2-MeNH-4-Pyr 4-Pyr 2-2084 3-F-Ph 2-MeNH-4-Pyr 3 -Pyr 2-2085 3-F-Ph 2-MeNH-4-Pyr 4-Pym 2-2086 3-F-Ph 2-MeNH-4-Pyr 5-Pym 2-2087 3-F-Ph 2-MeNH- 4-Pyr 3-Pyrd-CH _Two 2-2088 3-F-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd-CH _Two 2-2089 3-F-Ph 2-MeNH-4-Pyr 4-Pip-CH _Two 2-2090 3-F-Ph 2-MeNH-4-Pyr 1-Me-4-Pip-CH _Two 2-2091 3-F-Ph 2-MeNH-4-Pyr 2-Piz-CH _Two 2-2092 3-F-Ph 2-MeNH-4-Pyr 4-Pyr-CH _Two 2-2093 3-F-Ph 2-MeNH-4-Pyr 3-Pyr-CH _Two 2-2094 3-F-Ph 2-MeNH-4-Pyr 4-Pym-CH _Two 2-2095 3-F-Ph 2-MeNH-4-Pyr 5-Pym-CH _Two 2-2096 3-F-Ph 2-MeNH-4-Pyr 2-Pym-CH _Two 2-2097 3,4-diF-Ph 2-MeNH-4-Pyr H _Two N- (CH _Two ) _Three 2-2098 3,4-diF-Ph 2-MeNH-4-Pyr MeNH- (CH _Two ) _Three 2-2099 3,4-diF-Ph 2-MeNH-4-Pyr EtNH- (CH _Two ) _Three 2-2100 3,4-diF-Ph 2-MeNH-4-Pyr Me _Two N- (CH _Two ) _Three 2-2101 3,4-diF-Ph 2-MeNH-4-Pyr 1-Azt- (CH _Two ) _Three 2-2102 3,4-diF-Ph 2-MeNH-4-Pyr 1-Pyrd- (CH _Two ) _Three 2-2103 3,4-diF-Ph 2-MeNH-4-Pyr 1-Pip- (CH _Two ) _Three 2-2104 3,4-diF-Ph 2-MeNH-4-Pyr 1-Mor- (CH _Two ) _Three 2-2105 3,4-diF-Ph 2-MeNH-4-Pyr 1-Tmor- (CH _Two ) _Three 2-2106 3,4-diF-Ph 2-MeNH-4-Pyr 1-Piz- (CH _Two ) _Three 2-2107 3,4-diF-Ph 2-MeNH-4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-2108 3,4-diF-Ph 2-MeNH-4-Pyr 3-Azt 2-2109 3,4-diF-Ph 2-MeNH-4-Pyr 1-Me-3-Azt 2-2110 3,4 -diF-Ph 2-MeNH-4-Pyr 3-Pyrd 2-2111 3,4-diF-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd 2-2112 3,4-diF-Ph 2- MeNH-4-Pyr 4-Pip 2-2113 3,4-diF-Ph 2-MeNH-4-Pyr 4- (3,4-deH-Pip) 2-2114 3,4-diF-Ph 2-MeNH- 4-Pyr 1-Me-4-Pip 2-2115 3,4-diF-Ph 2-MeNH-4-Pyr 1-Me-4- (3,4-deH-Pip) 2-2116 3,4-diF -Ph 2-MeNH-4-Pyr 1-Piz 2-2117 3,4-diF-Ph 2-MeNH-4-Pyr 4-Me-1-Piz 2-2118 3,4-diF-Ph 2-MeNH- 4-Pyr 4-Pyr 2-2119 3,4-diF-Ph 2-MeNH-4-Pyr 3-Pyr 2-2120 3,4-diF-Ph 2-MeNH-4-Pyr 4-Pym 2-2121 3 , 4-diF-Ph 2-MeNH-4-Pyr 5-Pym 2-2122 3,4-diF-Ph 2-MeNH-4-Pyr 3-Pyrd-CH _Two 2-2123 3,4-diF-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd-CH _Two 2-2124 3,4-diF-Ph 2-MeNH-4-Pyr 4-Pip-CH _Two 2-2125 3,4-diF-Ph 2-MeNH-4-Pyr 1-Me-4-Pip-CH _Two 2-2126 3,4-diF-Ph 2-MeNH-4-Pyr 2-Piz-CH _Two 2-2127 3,4-diF-Ph 2-MeNH-4-Pyr 4-Pyr-CH _Two 2-2128 3,4-diF-Ph 2-MeNH-4-Pyr 3-Pyr-CH _Two 2-2129 3,4-diF-Ph 2-MeNH-4-Pyr 4-Pym-CH _Two 2-2130 3,4-diF-Ph 2-MeNH-4-Pyr 5-Pym-CH _Two 2-2131 3,4-diF-Ph 2-MeNH-4-Pyr 2-Pym-CH _Two 2-2132 3-Cl-Ph 2-MeNH-4-Pyr H _Two N- (CH _Two ) _Three 2-2133 3-Cl-Ph 2-MeNH-4-Pyr MeNH- (CH _Two ) _Three 2-2134 3-Cl-Ph 2-MeNH-4-Pyr EtNH- (CH _Two ) _Three 2-2135 3-Cl-Ph 2-MeNH-4-Pyr Me _Two N- (CH _Two ) _Three 2-2136 3-Cl-Ph 2-MeNH-4-Pyr 1-Azt- (CH _Two ) _Three 2-2137 3-Cl-Ph 2-MeNH-4-Pyr 1-Pyrd- (CH _Two ) _Three 2-2138 3-Cl-Ph 2-MeNH-4-Pyr 1-Pip- (CH _Two ) _Three 2-2139 3-Cl-Ph 2-MeNH-4-Pyr 1-Mor- (CH _Two ) _Three 2-2140 3-Cl-Ph 2-MeNH-4-Pyr 1-Tmor- (CH _Two ) _Three 2-2141 3-Cl-Ph 2-MeNH-4-Pyr 1-Piz- (CH _Two ) _Three 2-2142 3-Cl-Ph 2-MeNH-4-Pyr 4-Me-1-Piz- (CH _Two ) _Three 2-2143 3-Cl-Ph 2-MeNH-4-Pyr 3-Azt 2-2144 3-Cl-Ph 2-MeNH-4-Pyr 1-Me-3-Azt 2-2145 3-Cl-Ph 2- MeNH-4-Pyr 3-Pyrd 2-2146 3-Cl-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd 2-2147 3-Cl-Ph 2-MeNH-4-Pyr 4-Pip 2- 2148 3-Cl-Ph 2-MeNH-4-Pyr 4- (3,4-deH-Pip) 2-2149 3-Cl-Ph 2-MeNH-4-Pyr 1-Me-4-Pip 2-2150 3 -Cl-Ph 2-MeNH-4-Pyr 1-Me-4- (3,4-deH-Pip) 2-2151 3-Cl-Ph 2-MeNH-4-Pyr 1-Piz 2-2152 3-Cl -Ph 2-MeNH-4-Pyr 4-Me-1-Piz 2-2153 3-Cl-Ph 2-MeNH-4-Pyr 4-Pyr 2-2154 3-Cl-Ph 2-MeNH-4-Pyr 3 -Pyr 2-2155 3-Cl-Ph 2-MeNH-4-Pyr 4-Pym 2-2156 3-Cl-Ph 2-MeNH-4-Pyr 5-Pym 2-2157 3-Cl-Ph 2-MeNH- 4-Pyr 3-Pyrd-CH _Two 2-2158 3-Cl-Ph 2-MeNH-4-Pyr 1-Me-3-Pyrd-CH _Two 2-2159 3-Cl-Ph 2-MeNH-4-Pyr 4-Pip-CH _Two 2-2160 3-Cl-Ph 2-MeNH-4-Pyr 1-Me-4-Pip-CH _Two 2-2161 3-Cl-Ph 2-MeNH-4-Pyr 2-Piz-CH _Two 2-2162 3-Cl-Ph 2-MeNH-4-Pyr 4-Pyr-CH _Two 2-2163 3-Cl-Ph 2-MeNH-4-Pyr 3-Pyr-CH _Two 2-2164 3-Cl-Ph 2-MeNH-4-Pyr 4-Pym-CH _Two 2-2165 3-Cl-Ph 2-MeNH-4-Pyr 5-Pym-CH _Two 2-2166 3-Cl-Ph 2-MeNH-4-Pyr 2-Pym-CH _Two 2-2167 Ph 4-Pym H _Two N- (CH _Two ) _Three 2-2168 Ph 4-Pym MeNH- (CH _Two ) _Three 2-2169 Ph 4-Pym EtNH- (CH _Two ) _Three 2-2170 Ph 4-Pym Me _Two N- (CH _Two ) _Three 2-2171 Ph 4-Pym 1-Azt- (CH _Two ) _Three 2-2172 Ph 4-Pym 1-Pyrd- (CH _Two ) _Three 2-2173 Ph 4-Pym 1-Pip- (CH _Two ) _Three 2-2174 Ph 4-Pym 1-Mor- (CH _Two ) _Three 2-2175 Ph 4-Pym 1-Tmor- (CH _Two ) _Three 2-2176 Ph 4-Pym 1-Piz- (CH _Two ) _Three 2-2177 Ph 4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-2178 Ph 4-Pym 3-Azt 2-2179 Ph 4-Pym 1-Me-3-Azt 2-2180 Ph 4-Pym 3-Pyrd 2-2181 Ph 4-Pym 1-Me-3-Pyrd 2- 2182 Ph 4-Pym 4-Pip 2-2183 Ph 4-Pym 4- (3,4-deH-Pip) 2-2184 Ph 4-Pym 1-Me-4-Pip 2-2185 Ph 4-Pym 1-Me -4- (3,4-deH-Pip) 2-2186 Ph 4-Pym 1-Piz 2-2187 Ph 4-Pym 4-Me-1-Piz 2-2188 Ph 4-Pym 4-Pyr 2-2189 Ph 4-Pym 3-Pyr 2-2190 Ph 4-Pym 4-Pym 2-2191 Ph 4-Pym 5-Pym 2-2192 Ph 4-Pym 3-Pyrd-CH _Two 2-2193 Ph 4-Pym 1-Me-3-Pyrd-CH _Two 2-2194 Ph 4-Pym 4-Pip-CH _Two 2-2195 Ph 4-Pym 1-Me-4-Pip-CH _Two 2-2196 Ph 4-Pym 2-Piz-CH _Two 2-2197 Ph 4-Pym 4-Pyr-CH _Two 2-2198 Ph 4-Pym 3-Pyr-CH _Two 2-2199 Ph 4-Pym 4-Pym-CH _Two 2-2200 Ph 4-Pym 5-Pym-CH _Two 2-2201 Ph 4-Pym 2-Pym-CH _Two 2-2202 4-F-Ph 4-Pym H _Two N- (CH _Two ) _Three 2-2203 4-F-Ph 4-Pym MeNH- (CH _Two ) _Three 2-2204 4-F-Ph 4-Pym EtNH- (CH _Two ) _Three 2-2205 4-F-Ph 4-Pym Me _Two N- (CH _Two ) _Three 2-2206 4-F-Ph 4-Pym 1-Azt- (CH _Two ) _Three 2-2207 4-F-Ph 4-Pym 1-Pyrd- (CH _Two ) _Three 2-2208 4-F-Ph 4-Pym 1-Pip- (CH _Two ) _Three 2-2209 4-F-Ph 4-Pym 1-Mor- (CH _Two ) _Three 2-2210 4-F-Ph 4-Pym 1-Tmor- (CH _Two ) _Three 2-2211 4-F-Ph 4-Pym 1-Piz- (CH _Two ) _Three 2-2212 4-F-Ph 4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-2213 4-F-Ph 4-Pym 3-Azt 2-2214 4-F-Ph 4-Pym 1-Me-3-Azt 2-2215 4-F-Ph 4-Pym 3-Pyrd 2-2216 4 -F-Ph 4-Pym 1-Me-3-Pyrd 2-2217 4-F-Ph 4-Pym 4-Pip 2-2218 4-F-Ph 4-Pym 4- (3,4-deH-Pip) 2-2219 4-F-Ph 4-Pym 1-Me-4-Pip 2-2220 4-F-Ph 4-Pym 1-Me-4- (3,4-deH-Pip) 2-2221 4-F -Ph 4-Pym 1-Piz 2-2222 4-F-Ph 4-Pym 4-Me-1-Piz 2-2223 4-F-Ph 4-Pym 4-Pyr 2-2224 4-F-Ph 4- Pym 3-Pyr 2-2225 4-F-Ph 4-Pym 4-Pym 2-2226 4-F-Ph 4-Pym 5-Pym 2-2227 4-F-Ph 4-Pym 3-Pyrd-CH _Two 2-2228 4-F-Ph 4-Pym 1-Me-3-Pyrd-CH _Two 2-2229 4-F-Ph 4-Pym 4-Pip-CH _Two 2-2230 4-F-Ph 4-Pym 1-Me-4-Pip-CH _Two 2-2231 4-F-Ph 4-Pym 2-Piz-CH _Two 2-2232 4-F-Ph 4-Pym 4-Pyr-CH _Two 2-2233 4-F-Ph 4-Pym 3-Pyr-CH _Two 2-2234 4-F-Ph 4-Pym 4-Pym-CH _Two 2-2235 4-F-Ph 4-Pym 5-Pym-CH _Two 2-2236 4-F-Ph 4-Pym 2-Pym-CH _Two 2-2237 3-F-Ph 4-Pym H _Two N- (CH _Two ) _Three 2-2238 3-F-Ph 4-Pym MeNH- (CH _Two ) _Three 2-2239 3-F-Ph 4-Pym EtNH- (CH _Two ) _Three 2-2240 3-F-Ph 4-Pym Me _Two N- (CH _Two ) _Three 2-2241 3-F-Ph 4-Pym 1-Azt- (CH _Two ) _Three 2-2242 3-F-Ph 4-Pym 1-Pyrd- (CH _Two ) _Three 2-2243 3-F-Ph 4-Pym 1-Pip- (CH _Two ) _Three 2-2244 3-F-Ph 4-Pym 1-Mor- (CH _Two ) _Three 2-2245 3-F-Ph 4-Pym 1-Tmor- (CH _Two ) _Three 2-2246 3-F-Ph 4-Pym 1-Piz- (CH _Two ) _Three 2-2247 3-F-Ph 4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-2248 3-F-Ph 4-Pym 3-Azt 2-2249 3-F-Ph 4-Pym 1-Me-3-Azt 2-2250 3-F-Ph 4-Pym 3-Pyrd 2-2251 3 -F-Ph 4-Pym 1-Me-3-Pyrd 2-2252 3-F-Ph 4-Pym 4-Pip 2-2253 3-F-Ph 4-Pym 4- (3,4-deH-Pip) 2-2254 3-F-Ph 4-Pym 1-Me-4-Pip 2-2255 3-F-Ph 4-Pym 1-Me-4- (3,4-deH-Pip) 2-2256 3-F -Ph 4-Pym 1-Piz 2-2257 3-F-Ph 4-Pym 4-Me-1-Piz 2-2258 3-F-Ph 4-Pym 4-Pyr 2-2259 3-F-Ph 4- Pym 3-Pyr 2-2260 3-F-Ph 4-Pym 4-Pym 2-2261 3-F-Ph 4-Pym 5-Pym 2-2262 3-F-Ph 4-Pym 3-Pyrd-CH _Two 2-2263 3-F-Ph 4-Pym 1-Me-3-Pyrd-CH _Two 2-2264 3-F-Ph 4-Pym 4-Pip-CH _Two 2-2265 3-F-Ph 4-Pym 1-Me-4-Pip-CH _Two 2-2266 3-F-Ph 4-Pym 2-Piz-CH _Two 2-2267 3-F-Ph 4-Pym 4-Pyr-CH _Two 2-2268 3-F-Ph 4-Pym 3-Pyr-CH _Two 2-2269 3-F-Ph 4-Pym 4-Pym-CH _Two 2-2270 3-F-Ph 4-Pym 5-Pym-CH _Two 2-2271 3-F-Ph 4-Pym 2-Pym-CH _Two 2-2272 3,4-diF-Ph 4-Pym H _Two N- (CH _Two ) _Three 2-2273 3,4-diF-Ph 4-Pym MeNH- (CH _Two ) _Three 2-2274 3,4-diF-Ph 4-Pym EtNH- (CH _Two ) _Three 2-2275 3,4-diF-Ph 4-Pym Me _Two N- (CH _Two ) _Three 2-2276 3,4-diF-Ph 4-Pym 1-Azt- (CH _Two ) _Three 2-2277 3,4-diF-Ph 4-Pym 1-Pyrd- (CH _Two ) _Three 2-2278 3,4-diF-Ph 4-Pym 1-Pip- (CH _Two ) _Three 2-2279 3,4-diF-Ph 4-Pym 1-Mor- (CH _Two ) _Three 2-2280 3,4-diF-Ph 4-Pym 1-Tmor- (CH _Two ) _Three 2-2281 3,4-diF-Ph 4-Pym 1-Piz- (CH _Two ) _Three 2-2282 3,4-diF-Ph 4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-2283 3,4-diF-Ph 4-Pym 3-Azt 2-2284 3,4-diF-Ph 4-Pym 1-Me-3-Azt 2-2285 3,4-diF-Ph 4-Pym 3 -Pyrd 2-2286 3,4-diF-Ph 4-Pym 1-Me-3-Pyrd 2-2287 3,4-diF-Ph 4-Pym 4-Pip 2-2288 3,4-diF-Ph 4- Pym 4- (3,4-deH-Pip) 2-2289 3,4-diF-Ph 4-Pym 1-Me-4-Pip 2-2290 3,4-diF-Ph 4-Pym 1-Me-4 -(3,4-deH-Pip) 2-2291 3,4-diF-Ph 4-Pym 1-Piz 2-2292 3,4-diF-Ph 4-Pym 4-Me-1-Piz 2-2293 3 , 4-diF-Ph 4-Pym 4-Pyr 2-2294 3,4-diF-Ph 4-Pym 3-Pyr 2-2295 3,4-diF-Ph 4-Pym 4-Pym 2-2296 3,4 -diF-Ph 4-Pym 5-Pym 2-2297 3,4-diF-Ph 4-Pym 3-Pyrd-CH _Two 2-2298 3,4-diF-Ph 4-Pym 1-Me-3-Pyrd-CH _Two 2-2299 3,4-diF-Ph 4-Pym 4-Pip-CH _Two 2-2300 3,4-diF-Ph 4-Pym 1-Me-4-Pip-CH _Two 2-2301 3,4-diF-Ph 4-Pym 2-Piz-CH _Two 2-2302 3,4-diF-Ph 4-Pym 4-Pyr-CH _Two 2-2303 3,4-diF-Ph 4-Pym 3-Pyr-CH _Two 2-2304 3,4-diF-Ph 4-Pym 4-Pym-CH _Two 2-2305 3,4-diF-Ph 4-Pym 5-Pym-CH _Two 2-2306 3,4-diF-Ph 4-Pym 2-Pym-CH _Two 2-2307 3-Cl-Ph 4-Pym H _Two N- (CH _Two ) _Three 2-2308 3-Cl-Ph 4-Pym MeNH- (CH _Two ) _Three 2-2309 3-Cl-Ph 4-Pym EtNH- (CH _Two ) _Three 2-2310 3-Cl-Ph 4-Pym Me _Two N- (CH _Two ) _Three 2-2311 3-Cl-Ph 4-Pym 1-Azt- (CH _Two ) _Three 2-2312 3-Cl-Ph 4-Pym 1-Pyrd- (CH _Two ) _Three 2-2313 3-Cl-Ph 4-Pym 1-Pip- (CH _Two ) _Three 2-2314 3-Cl-Ph 4-Pym 1-Mor- (CH _Two ) _Three 2-2315 3-Cl-Ph 4-Pym 1-Tmor- (CH _Two ) _Three 2-2316 3-Cl-Ph 4-Pym 1-Piz- (CH _Two ) _Three 2-2317 3-Cl-Ph 4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-2318 3-Cl-Ph 4-Pym 3-Azt 2-2319 3-Cl-Ph 4-Pym 1-Me-3-Azt 2-2320 3-Cl-Ph 4-Pym 3-Pyrd 2-2321 3 -Cl-Ph 4-Pym 1-Me-3-Pyrd 2-2322 3-Cl-Ph 4-Pym 4-Pip 2-2323 3-Cl-Ph 4-Pym 4- (3,4-deH-Pip) 2-2324 3-Cl-Ph 4-Pym 1-Me-4-Pip 2-2325 3-Cl-Ph 4-Pym 1-Me-4- (3,4-deH-Pip) 2-2326 3-Cl -Ph 4-Pym 1-Piz 2-2327 3-Cl-Ph 4-Pym 4-Me-1-Piz 2-2328 3-Cl-Ph 4-Pym 4-Pyr 2-2329 3-Cl-Ph 4- Pym 3-Pyr 2-2330 3-Cl-Ph 4-Pym 4-Pym 2-2331 3-Cl-Ph 4-Pym 5-Pym 2-2332 3-Cl-Ph 4-Pym 3-Pyrd-CH _Two 2-2333 3-Cl-Ph 4-Pym 1-Me-3-Pyrd-CH _Two 2-2334 3-Cl-Ph 4-Pym 4-Pip-CH _Two 2-2335 3-Cl-Ph 4-Pym 1-Me-4-Pip-CH _Two 2-2336 3-Cl-Ph 4-Pym 2-Piz-CH _Two 2-2337 3-Cl-Ph 4-Pym 4-Pyr-CH _Two 2-2338 3-Cl-Ph 4-Pym 3-Pyr-CH _Two 2-2339 3-Cl-Ph 4-Pym 4-Pym-CH _Two 2-2340 3-Cl-Ph 4-Pym 5-Pym-CH _Two 2-2341 3-Cl-Ph 4-Pym 2-Pym-CH _Two 2-2342 Ph 2-MeO-4-Pym H _Two N- (CH _Two ) _Three 2-2343 Ph 2-MeO-4-Pym MeNH- (CH _Two ) _Three 2-2344 Ph 2-MeO-4-Pym EtNH- (CH _Two ) _Three 2-2345 Ph 2-MeO-4-Pym Me _Two N- (CH _Two ) _Three 2-2346 Ph 2-MeO-4-Pym 1-Azt- (CH _Two ) _Three 2-2347 Ph 2-MeO-4-Pym 1-Pyrd- (CH _Two ) _Three 2-2348 Ph 2-MeO-4-Pym 1-Pip- (CH _Two ) _Three 2-2349 Ph 2-MeO-4-Pym 1-Mor- (CH _Two ) _Three 2-2350 Ph 2-MeO-4-Pym 1-Tmor- (CH _Two ) _Three 2-2351 Ph 2-MeO-4-Pym 1-Piz- (CH _Two ) _Three 2-2352 Ph 2-MeO-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-2353 Ph 2-MeO-4-Pym 3-Azt 2-2354 Ph 2-MeO-4-Pym 1-Me-3-Azt 2-2355 Ph 2-MeO-4-Pym 3-Pyrd 2-2356 Ph 2-MeO-4-Pym 1-Me-3-Pyrd 2-2357 Ph 2-MeO-4-Pym 4-Pip 2-2358 Ph 2-MeO-4-Pym 4- (3,4-deH-Pip) 2-2359 Ph 2-MeO-4-Pym 1-Me-4-Pip 2-2360 Ph 2-MeO-4-Pym 1-Me-4- (3,4-deH-Pip) 2-2361 Ph 2- MeO-4-Pym 1-Piz 2-2362 Ph 2-MeO-4-Pym 4-Me-1-Piz 2-2363 Ph 2-MeO-4-Pym 4-Pyr 2-2364 Ph 2-MeO-4- Pym 3-Pyr 2-2365 Ph 2-MeO-4-Pym 4-Pym 2-2366 Ph 2-MeO-4-Pym 5-Pym 2-2367 Ph 2-MeO-4-Pym 3-Pyrd-CH _Two 2-2368 Ph 2-MeO-4-Pym 1-Me-3-Pyrd-CH _Two 2-2369 Ph 2-MeO-4-Pym 4-Pip-CH _Two 2-2370 Ph 2-MeO-4-Pym 1-Me-4-Pip-CH _Two 2-2371 Ph 2-MeO-4-Pym 2-Piz-CH _Two 2-2372 Ph 2-MeO-4-Pym 4-Pyr-CH _Two 2-2373 Ph 2-MeO-4-Pym 3-Pyr-CH _Two 2-2374 Ph 2-MeO-4-Pym 4-Pym-CH _Two 2-2375 Ph 2-MeO-4-Pym 5-Pym-CH _Two 2-2376 Ph 2-MeO-4-Pym 2-Pym-CH _Two 2-2377 4-F-Ph 2-MeO-4-Pym H _Two N- (CH _Two ) _Three 2-2378 4-F-Ph 2-MeO-4-Pym MeNH- (CH _Two ) _Three 2-2379 4-F-Ph 2-MeO-4-Pym EtNH- (CH _Two ) _Three 2-2380 4-F-Ph 2-MeO-4-Pym Me _Two N- (CH _Two ) _Three 2-2381 4-F-Ph 2-MeO-4-Pym 1-Azt- (CH _Two ) _Three 2-2382 4-F-Ph 2-MeO-4-Pym 1-Pyrd- (CH _Two ) _Three 2-2383 4-F-Ph 2-MeO-4-Pym 1-Pip- (CH _Two ) _Three 2-2384 4-F-Ph 2-MeO-4-Pym 1-Mor- (CH _Two ) _Three 2-2385 4-F-Ph 2-MeO-4-Pym 1-Tmor- (CH _Two ) _Three 2-2386 4-F-Ph 2-MeO-4-Pym 1-Piz- (CH _Two ) _Three 2-2387 4-F-Ph 2-MeO-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-2388 4-F-Ph 2-MeO-4-Pym 3-Azt 2-2389 4-F-Ph 2-MeO-4-Pym 1-Me-3-Azt 2-2390 4-F-Ph 2- MeO-4-Pym 3-Pyrd 2-2391 4-F-Ph 2-MeO-4-Pym 1-Me-3-Pyrd 2-2392 4-F-Ph 2-MeO-4-Pym 4-Pip 2- 2393 4-F-Ph 2-MeO-4-Pym 4- (3,4-deH-Pip) 2-2394 4-F-Ph 2-MeO-4-Pym 1-Me-4-Pip 2-2395 4 -F-Ph 2-MeO-4-Pym 1-Me-4- (3,4-deH-Pip) 2-2396 4-F-Ph 2-MeO-4-Pym 1-Piz 2-2397 4-F -Ph 2-MeO-4-Pym 4-Me-1-Piz 2-2398 4-F-Ph 2-MeO-4-Pym 4-Pyr 2-2399 4-F-Ph 2-MeO-4-Pym 3 -Pyr 2-2400 4-F-Ph 2-MeO-4-Pym 4-Pym 2-2401 4-F-Ph 2-MeO-4-Pym 5-Pym 2-2402 4-F-Ph 2-MeO- 4-Pym 3-Pyrd-CH _Two 2-2403 4-F-Ph 2-MeO-4-Pym 1-Me-3-Pyrd-CH _Two 2-2404 4-F-Ph 2-MeO-4-Pym 4-Pip-CH _Two 2-2405 4-F-Ph 2-MeO-4-Pym 1-Me-4-Pip-CH _Two 2-2406 4-F-Ph 2-MeO-4-Pym 2-Piz-CH _Two 2-2407 4-F-Ph 2-MeO-4-Pym 4-Pyr-CH _Two 2-2408 4-F-Ph 2-MeO-4-Pym 3-Pyr-CH _Two 2-2409 4-F-Ph 2-MeO-4-Pym 4-Pym-CH _Two 2-2410 4-F-Ph 2-MeO-4-Pym 5-Pym-CH _Two 2-2411 4-F-Ph 2-MeO-4-Pym 2-Pym-CH _Two 2-2412 3-F-Ph 2-MeO-4-Pym H _Two N- (CH _Two ) _Three 2-2413 3-F-Ph 2-MeO-4-Pym MeNH- (CH _Two ) _Three 2-2414 3-F-Ph 2-MeO-4-Pym EtNH- (CH _Two ) _Three 2-2415 3-F-Ph 2-MeO-4-Pym Me _Two N- (CH _Two ) _Three 2-2416 3-F-Ph 2-MeO-4-Pym 1-Azt- (CH _Two ) _Three 2-2417 3-F-Ph 2-MeO-4-Pym 1-Pyrd- (CH _Two ) _Three 2-2418 3-F-Ph 2-MeO-4-Pym 1-Pip- (CH _Two ) _Three 2-2419 3-F-Ph 2-MeO-4-Pym 1-Mor- (CH _Two ) _Three 2-2420 3-F-Ph 2-MeO-4-Pym 1-Tmor- (CH _Two ) _Three 2-2421 3-F-Ph 2-MeO-4-Pym 1-Piz- (CH _Two ) _Three 2-2422 3-F-Ph 2-MeO-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-2423 3-F-Ph 2-MeO-4-Pym 3-Azt 2-2424 3-F-Ph 2-MeO-4-Pym 1-Me-3-Azt 2-2425 3-F-Ph 2- MeO-4-Pym 3-Pyrd 2-2426 3-F-Ph 2-MeO-4-Pym 1-Me-3-Pyrd 2-2427 3-F-Ph 2-MeO-4-Pym 4-Pip 2- 2428 3-F-Ph 2-MeO-4-Pym 4- (3,4-deH-Pip) 2-2429 3-F-Ph 2-MeO-4-Pym 1-Me-4-Pip 2-2430 3 -F-Ph 2-MeO-4-Pym 1-Me-4- (3,4-deH-Pip) 2-2431 3-F-Ph 2-MeO-4-Pym 1-Piz 2-2432 3-F -Ph 2-MeO-4-Pym 4-Me-1-Piz 2-2433 3-F-Ph 2-MeO-4-Pym 4-Pyr 2-2434 3-F-Ph 2-MeO-4-Pym 3 -Pyr 2-2435 3-F-Ph 2-MeO-4-Pym 4-Pym 2-2436 3-F-Ph 2-MeO-4-Pym 5-Pym 2-2437 3-F-Ph 2-MeO- 4-Pym 3-Pyrd-CH _Two 2-2438 3-F-Ph 2-MeO-4-Pym 1-Me-3-Pyrd-CH _Two 2-2439 3-F-Ph 2-MeO-4-Pym 4-Pip-CH _Two 2-2440 3-F-Ph 2-MeO-4-Pym 1-Me-4-Pip-CH _Two 2-2441 3-F-Ph 2-MeO-4-Pym 2-Piz-CH _Two 2-2442 3-F-Ph 2-MeO-4-Pym 4-Pyr-CH _Two 2-2443 3-F-Ph 2-MeO-4-Pym 3-Pyr-CH _Two 2-2444 3-F-Ph 2-MeO-4-Pym 4-Pym-CH _Two 2-2445 3-F-Ph 2-MeO-4-Pym 5-Pym-CH _Two 2-2446 3-F-Ph 2-MeO-4-Pym 2-Pym-CH _Two 2-2447 3,4-diF-Ph 2-MeO-4-Pym H _Two N- (CH _Two ) _Three 2-2448 3,4-diF-Ph 2-MeO-4-Pym MeNH- (CH _Two ) _Three 2-2449 3,4-diF-Ph 2-MeO-4-Pym EtNH- (CH _Two ) _Three 2-2450 3,4-diF-Ph 2-MeO-4-Pym Me _Two N- (CH _Two ) _Three 2-2451 3,4-diF-Ph 2-MeO-4-Pym 1-Azt- (CH _Two ) _Three 2-2452 3,4-diF-Ph 2-MeO-4-Pym 1-Pyrd- (CH _Two ) _Three 2-2453 3,4-diF-Ph 2-MeO-4-Pym 1-Pip- (CH _Two ) _Three 2-2454 3,4-diF-Ph 2-MeO-4-Pym 1-Mor- (CH _Two ) _Three 2-2455 3,4-diF-Ph 2-MeO-4-Pym 1-Tmor- (CH _Two ) _Three 2-2456 3,4-diF-Ph 2-MeO-4-Pym 1-Piz- (CH _Two ) _Three 2-2457 3,4-diF-Ph 2-MeO-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-2458 3,4-diF-Ph 2-MeO-4-Pym 3-Azt 2-2459 3,4-diF-Ph 2-MeO-4-Pym 1-Me-3-Azt 2-2460 3,4 -diF-Ph 2-MeO-4-Pym 3-Pyrd 2-2461 3,4-diF-Ph 2-MeO-4-Pym 1-Me-3-Pyrd 2-2462 3,4-diF-Ph 2- MeO-4-Pym 4-Pip 2-2463 3,4-diF-Ph 2-MeO-4-Pym 4- (3,4-deH-Pip) 2-2464 3,4-diF-Ph 2-MeO- 4-Pym 1-Me-4-Pip 2-2465 3,4-diF-Ph 2-MeO-4-Pym 1-Me-4- (3,4-deH-Pip) 2-2466 3,4-diF -Ph 2-MeO-4-Pym 1-Piz 2-2467 3,4-diF-Ph 2-MeO-4-Pym 4-Me-1-Piz 2-2468 3,4-diF-Ph 2-MeO- 4-Pym 4-Pyr 2-2469 3,4-diF-Ph 2-MeO-4-Pym 3-Pyr 2-2470 3,4-diF-Ph 2-MeO-4-Pym 4-Pym 2-2471 3 , 4-diF-Ph 2-MeO-4-Pym 5-Pym 2-2472 3,4-diF-Ph 2-MeO-4-Pym 3-Pyrd-CH _Two 2-2473 3,4-diF-Ph 2-MeO-4-Pym 1-Me-3-Pyrd-CH _Two 2-2474 3,4-diF-Ph 2-MeO-4-Pym 4-Pip-CH _Two 2-2475 3,4-diF-Ph 2-MeO-4-Pym 1-Me-4-Pip-CH _Two 2-2476 3,4-diF-Ph 2-MeO-4-Pym 2-Piz-CH _Two 2-2477 3,4-diF-Ph 2-MeO-4-Pym 4-Pyr-CH _Two 2-2478 3,4-diF-Ph 2-MeO-4-Pym 3-Pyr-CH _Two 2-2479 3,4-diF-Ph 2-MeO-4-Pym 4-Pym-CH _Two 2-2480 3,4-diF-Ph 2-MeO-4-Pym 5-Pym-CH _Two 2-2481 3,4-diF-Ph 2-MeO-4-Pym 2-Pym-CH _Two 2-2482 3-Cl-Ph 2-MeO-4-Pym H _Two N- (CH _Two ) _Three 2-2483 3-Cl-Ph 2-MeO-4-Pym MeNH- (CH _Two ) _Three 2-2484 3-Cl-Ph 2-MeO-4-Pym EtNH- (CH _Two ) _Three 2-2485 3-Cl-Ph 2-MeO-4-Pym Me _Two N- (CH _Two ) _Three 2-2486 3-Cl-Ph 2-MeO-4-Pym 1-Azt- (CH _Two ) _Three 2-2487 3-Cl-Ph 2-MeO-4-Pym 1-Pyrd- (CH _Two ) _Three 2-2488 3-Cl-Ph 2-MeO-4-Pym 1-Pip- (CH _Two ) _Three 2-2489 3-Cl-Ph 2-MeO-4-Pym 1-Mor- (CH _Two ) _Three 2-2490 3-Cl-Ph 2-MeO-4-Pym 1-Tmor- (CH _Two ) _Three 2-2491 3-Cl-Ph 2-MeO-4-Pym 1-Piz- (CH _Two ) _Three 2-2492 3-Cl-Ph 2-MeO-4-Pym 4-Me-1-Piz- (CH _Two ) _Three 2-2493 3-Cl-Ph 2-MeO-4-Pym 3-Azt 2-2494 3-Cl-Ph 2-MeO-4-Pym 1-Me-3-Azt 2-2495 3-Cl-Ph 2- MeO-4-Pym 3-Pyrd 2-2496 3-Cl-Ph 2-MeO-4-Pym 1-Me-3-Pyrd 2-2497 3-Cl-Ph 2-MeO-4-Pym 4-Pip 2- 2498 3-Cl-Ph 2-MeO-4-Pym 4- (3,4-deH-Pip) 2-2499 3-Cl-Ph 2-MeO-4-Pym 1-Me-4-Pip 2-2500 3 -Cl-Ph 2-MeO-4-Pym 1-Me-4- (3,4-deH-Pip) 2-2501 3-Cl-Ph 2-MeO-4-Pym 1-Piz 2-2502 3-Cl -Ph 2-MeO-4-Pym 4-Me-1-Piz 2-2503 3-Cl-Ph 2-MeO-4-Pym 4-Pyr 2-2504 3-Cl-Ph 2-MeO-4-Pym 3 -Pyr 2-2505 3-Cl-Ph 2-MeO-4-Pym 4-Pym 2-2506 3-Cl-Ph 2-MeO-4-Pym 5-Pym 2-2507 3-Cl-Ph 2-MeO- 4-Pym 3-Pyrd-CH _Two 2-2508 3-Cl-Ph 2-MeO-4-Pym 1-Me-3-Pyrd-CH _Two 2-2509 3-Cl-Ph 2-MeO-4-Pym 4-Pip-CH _Two 2-2510 3-Cl-Ph 2-MeO-4-Pym 1-Me-4-Pip-CH _Two 2-2511 3-Cl-Ph 2-MeO-4-Pym 2-Piz-CH _Two 2-2512 3-Cl-Ph 2-MeO-4-Pym 4-Pyr-CH _Two 2-2513 3-Cl-Ph 2-MeO-4-Pym 3-Pyr-CH _Two 2-2514 3-Cl-Ph 2-MeO-4-Pym 4-Pym-CH _Two 2-2515 3-Cl-Ph 2-MeO-4-Pym 5-Pym-CH _Two 2-2516 3-Cl-Ph 2-MeO-4-Pym 2-Pym-CH _Two 2-2517 4-F-Ph 4-Pyr H _Two N-CH _Two CH = CH 2-2518 4-F-Ph 4-Pyr MeNH-CH _Two CH = CH 2-2519 4-F-Ph 4-Pyr Me _Two N-CH _Two CH = CH 2-2520 4-F-Ph 4-Pyr 3-Pip-CH _Two 2-2521 4-F-Ph 4-Pyr 1-Me-3-Pip-CH _Two 2-2522 4-F-Ph 4-Pyr 2-Me-4-Pip 2-2523 4-F-Ph 4-Pyr 2,2,6,6-tetraMe-4-Pip 2-2524 4-F-Ph 4-Pyr 1-Ac-4-Pip 2-2525 4-F-Ph 4-Pyr 1-Ac-4- (3,4-deH-Pip) 2-2526 4-F-Ph 4-Pyr 4-OH -4-Pip 2-2527 4-F-Ph 4-Pyr 4-OH-1-Me-4-Pip 2-2528 4-F-Ph 4-Pyr AcNH- (CH _Two ) _Three 2-2529 4-F-Ph 4-Pyr 4-NH _Two -cHx 2-2530 4-F-Ph 4-Pyr 4-Pyr-CH (OH) 2-2531 4-F-Ph 4-Pyr 3-Pyr-CH (OH) 2-2532 4-F-Ph 4- Pyr 2-Pyr-CH (OH) 2-2533 4-F-Ph 4-Pyr CF _Three CONH- (CH _Two ) _Three 2-2534 4-F-Ph 4-Pyr BzNH- (CH _Two ) _Three 2-2535 4-F-Ph 4-Pyr 2,4,6-triF-BzNH-CH _Two 2-2536 4-F-Ph 4-Pyr MeSO _Two NH- (CH _Two ) _Three 2-2537 4-F-Ph 4-Pyr 1-NO _Two (CH _Two ) _Two -4-Pip 2-2538 4-F-Ph 4-Pyr 2,3,5,6-tetraF-4-Pyr 2-2539 4-F-Ph 4-Pyr 3-Qun 2-2540 4-F-Ph 4-Pyr 3- (2,3-deH-Qun) 2-2541 4-F-Ph 4-Pyr 3-ABO 2-2542 4-F-Ph 4-Pyr 8-Me-3-ABO 2-2543 4 -F-Ph 4-Pyr 3- (2,3-deH-ABO) 2-2544 4-F-Ph 4-Pyr 8-Me-3- (2,3-deH-ABO) 2-2545 4-F -Ph 4-Pyr 3-ABN 2-2546 4-F-Ph 4-Pyr 9-Me-3-ABN 2-2547 4-F-Ph 4-Pyr 3- (2,3-deH-ABN) 2- 2548 4-F-Ph 4-Pyr 9-Me-3- (2,3-deH-ABN) 2-2549 4-F-Ph 2-NH _Two -4-Pym H _Two N-CH _Two CH = CH 2-2550 4-F-Ph 2-NH _Two -4-Pym MeNH-CH _Two CH = CH 2-2551 4-F-Ph 2-NH _Two -4-Pym Me _Two N-CH _Two CH = CH 2-2552 4-F-Ph 2-NH _Two -4-Pym 3-Pip-CH _Two 2-2553 4-F-Ph 2-NH _Two -4-Pym 1-Me-3-Pip-CH _Two 2-2554 4-F-Ph 2-NH _Two -4-Pym 2-Me-4-Pip 2-2555 4-F-Ph 2-NH _Two -4-Pym 2,2,6,6-tetraMe-4-Pip 2-2556 4-F-Ph 2-NH _Two -4-Pym 1-Ac-4-Pip 2-2557 4-F-Ph 2-NH _Two -4-Pym 1-Ac-4- (3,4-deH-Pip) 2-2558 4-F-Ph 2-NH _Two -4-Pym 4-OH-4-Pip 2-2559 4-F-Ph 2-NH _Two -4-Pym 4-OH-1-Me-4-Pip 2-2560 4-F-Ph 2-NH _Two -4-Pym AcNH- (CH _Two ) _Three 2-2561 4-F-Ph 2-NH _Two -4-Pym 4-NH _Two -cHx 2-2562 4-F-Ph 2-NH _Two -4-Pym 3-Qun 2-2563 4-F-Ph 2-NH _Two -4-Pym 3- (2,3-deH-Qun) 2-2564 4-F-Ph 2-NH _Two -4-Pym 3-ABO 2-2565 4-F-Ph 2-NH _Two -4-Pym 8-Me-3-ABO 2-2566 4-F-Ph 2-NH _Two -4-Pym 3- (2,3-deH-ABO) 2-2567 4-F-Ph 2-NH _Two -4-Pym 8-Me-3- (2,3-deH-ABO) 2-2568 4-F-Ph 2-NH _Two -4-Pym 3-ABN 2-2569 4-F-Ph 2-NH _Two -4-Pym 9-Me-3-ABN 2-2570 4-F-Ph 2-NH _Two -4-Pym 3- (2,3-deH-ABN) 2-2571 4-F-Ph 2-NH _Two -4-Pym 9-Me-3- (2,3-deH-ABN) 2-2572 4-F-Ph 2-MeNH-4-Pym H _Two N-CH _Two CH = CH 2-2573 4-F-Ph 2-MeNH-4-Pym MeNH-CH _Two CH = CH 2-2574 4-F-Ph 2-MeNH-4-Pym Me _Two N-CH _Two CH = CH 2-2575 4-F-Ph 2-MeNH-4-Pym 3-Pip-CH _Two 2-2576 4-F-Ph 2-MeNH-4-Pym 1-Me-3-Pip-CH _Two 2-2577 4-F-Ph 2-MeNH-4-Pym 2-Me-4-Pip 2-2578 4-F-Ph 2-MeNH-4-Pym 2,2,6,6-tetraMe-4-Pip 2-2579 4-F-Ph 2-MeNH-4-Pym 1-Ac-4-Pip 2-2580 4-F-Ph 2-MeNH-4-Pym 1-Ac-4- (3,4-deH- Pip) 2-2581 4-F-Ph 2-MeNH-4-Pym 4-OH-4-Pip 2-2582 4-F-Ph 2-MeNH-4-Pym 4-OH-1-Me-4-Pip 2-2583 4-F-Ph 2-MeNH-4-Pym AcNH- (CH _Two ) _Three 2-2584 4-F-Ph 2-MeNH-4-Pym 4-NH _Two -cHx 2-2585 4-F-Ph 2-MeNH-4-Pym 3-Qun 2-2586 4-F-Ph 2-MeNH-4-Pym 3- (2,3-deH-Qun) 2-2587 4 -F-Ph 2-MeNH-4-Pym 3-ABO 2-2588 4-F-Ph 2-MeNH-4-Pym 8-Me-3-ABO 2-2589 4-F-Ph 2-MeNH-4- Pym 3- (2,3-deH-ABO) 2-2590 4-F-Ph 2-MeNH-4-Pym 8-Me-3- (2,3-deH-ABO) 2-2591 4-F-Ph 2-MeNH-4-Pym 3-ABN 2-2592 4-F-Ph 2-MeNH-4-Pym 9-Me-3-ABN 2-2593 4-F-Ph 2-MeNH-4-Pym 3- ( 2,3-deH-ABN) 2-2594 4-F-Ph 2-MeNH-4-Pym 9-Me-3- (2,3-deH-ABN) 2-2595 4-F-Ph 2-BnNH- 4-Pyr 4-Pip 2-2596 4-F-Ph 2-BnNH-4-Pyr 4- (3,4-deH-Pip) 2-2597 4-F-Ph 2-BnNH-4-Pym 4-Pip 2-2598 4-F-Ph 2-BnNH-4-Pym 4- (3,4-deH-Pip) 2-2599 4-F-Ph 2- (α-Me-BnNH) -4-Pyr 4-Pip 2-2600 4-F-Ph 2- (α-Me-BnNH) -4-Pyr 4- (3,4-deH-Pip) 2-2601 4-F-Ph 2- (α-Me-BnNH)- 4-Pym 4-Pip 2-2602 4-F-Ph 2- (α-Me-BnNH) -4-Pym 4- (3,4-deH-Pip) 2-2603 3-Cl-Ph 2-BnNH- 4-Pyr 4-Pip 2-2604 3-Cl-Ph 2-BnNH-4-Pyr 4- (3,4-deH-Pip) 2-2605 3-Cl-Ph 2-BnNH-4-Pym 4-Pip 2-2606 3-Cl-Ph 2-BnNH-4-Pym 4- (3,4-deH-Pip) 2-2607 3-Cl-Ph 2- (α-Me-BnNH) -4-Pyr 4-Pip 2-2608 3-Cl-Ph 2- (α-Me-BnNH) -4-Pyr 4- (3,4-deH-Pip) 2-2609 3- Cl-Ph 2- (α-Me-BnNH) -4-Pym 4-Pip 2-2610 3-Cl-Ph 2- (α-Me-BnNH) -4-Pym 4- (3,4-deH-Pip ) 2-2611 3-CF _Three -Ph 2-BnNH-4-Pyr 4-Pip 2-2612 3-CF _Three -Ph 2-BnNH-4-Pyr 4- (3,4-deH-Pip) 2-2613 3-CF _Three -Ph 2-BnNH-4-Pym 4-Pip 2-2614 3-CF _Three -Ph 2-BnNH-4-Pym 4- (3,4-deH-Pip) 2-2615 3-CF _Three -Ph 2- (α-Me-BnNH) -4-Pyr 4-Pip 2-2616 3-CF _Three -Ph 2- (α-Me-BnNH) -4-Pyr 4- (3,4-deH-Pip) 2-2617 3-CF _Three -Ph 2- (α-Me-BnNH) -4-Pym 4-Pip 2-2618 3-CF _Three -Ph 2- (α-Me-BnNH) -4-Pym 4- (3,4-deH-Pip) 2-2619 4-F-Ph 4-Pyr 2-NH _Two -4-Pym 2-2620 4-F-Ph 4-Pyr 2-MeNH-4-pym 2-2621 4-F-Ph 4-Pyr 2-NH _Two -4-Pyr 2-2622 4-F-Ph 4-Pyr 2-MeNH-4-pyr ------------------------------------------- −−−−−−− Table 2 (continued) −−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−− Compound No. R ¹ R ^Two R ^Three −−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−−− 2-2623 4-F-Ph 4-Pyr H _Two N-CH _Two C (Me) _Two CH _Two 2-2624 4-F-Ph 4-Pyr MeNH-CH _Two C (Me) _Two CH _Two 2-2625 4-F-Ph 4-Pyr EtNH-CH _Two C (Me) _Two CH _Two 2-2626 4-F-Ph 4-Pyr Me _Two N-CH _Two C (Me) _Two CH _Two 2-2627 4-F-Ph 4-Pyr 3- (3,4-deH-Pip) 2-2628 4-F-Ph 4-Pyr 1-Me-3- (3,4-deH-Pip) 2- 2629 4-F-Ph 4-Pyr 1-Et-4- (3,4-deH-Pip) 2-2630 4-F-Ph 4-Pyr 1-Pr-4- (3,4-deH-Pip) 2-2631 4-F-Ph 4-Pyr 1-Pr-4-Pip 2-2632 4-F-Ph 4-Pyr 1-iPr-4- (3,4-deH-Pip) 2-2633 4-F -Ph 4-Pyr 1-iPr-4-Pip 2-2634 4-F-Ph 4-Pyr 1-Bu-4- (3,4-deH-Pip) 2-2635 4-F-Ph 4-Pyr 1 -tBu-4- (3,4-deH-Pip) 2-2636 4-F-Ph 4-Pyr 1-Pn-4- (3,4-deH-Pip) 2-2637 4-F-Ph 4- Pyr 1-Hx-4- (3,4-deH-Pip) 2-2638 4-F-Ph 4-Pyr 1-Hp-4- (3,4-deH-Pip) 2-2639 4-F-Ph 4-Pyr 1-Oc-4- (3,4-deH-Pip) 2-2640 4-F-Ph 4-Pyr 1-Nn-4- (3,4-deH-Pip) 2-2641 4-F -Ph 4-Pyr 1-cPr-4- (3,4-deH-Pip) 2-2642 4-F-Ph 4-Pyr 1-cPn-4- (3,4-deH-Pip) 2-2643 4 -F-Ph 4-Pyr 1-cHx-4- (3,4-deH-Pip) 2-2644 4-F-Ph 4-Pyr 1-Bn-4- (3,4-deH-Pip) 2- 2645 4-F-Ph 4-Pyr 1-Phet-4- (3,4-deH-Pip) 2-2646 4-F-Ph 4-Pyr 1- (3-Ph-Pr) -4- (3, 4-deH-Pip) 2-2647 4-F-Ph 4-Pyr 1- (4-Ph-Bu) -4- (3,4-deH-Pip) 2-2648 4-F-Ph 4-Pyr 1 -Allyl-4- (3,4-deH-Pip) 2-2649 4-F-Ph 4-Pyr 1-Propargyl-4- (3,4-deH-Pip) 2-2650 4-F-Ph 4- Pyr 2,2,6,6, -tetraMe-4- (3,4-deH-Pi p) 2-2651 4-F-Ph 4-Pyr 1,2,2,6,6, -pentaMe-4- (3,4-deH-Pip) 2-2652 4-F-Ph 4-Pyr 1, 2,2,6,6, -pentaMe-4-Pip) 2-2653 4-F-Ph 4-Pyr 7- (1,2,3,5,6,8a-hexaH-Ind) 2-2654 4- F-Ph 4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 2-2655 4-F-Ph 4-Pyr 7-octaH-Ind 2-2656 4-F-Ph 4 -Pyr 8- (1,3,4,6,7,9a-hexaH-2H-Qui) 2-2657 4-F-Ph 4-Pyr 8- (1,3,4,6,9,9a-hexaH -2H-Qui) 2-2658 4-F-Ph 4-Pyr 8-octaH-Qui 2-2659 4-F-Ph 4-Pyr 2,2-diMe-4- (3,4-deH-PiP) 2 -2660 4-F-Ph 4-Pyr 1,2,2-triMe-4- (3,4-deH-PiP) 2-2661 4-F-Ph 4-Pyr 2,2-diMe-4- (4 , 5-deH-PiP) 2-2662 4-F-Ph 4-Pyr 1,2,2-triMe-4- (4,5-deH-PiP) 2-2663 4-F-Ph 4-Pyr 2, 6-diMe-4- (3,4-deH-PiP) 2-2664 4-F-Ph 4-Pyr 1,2,6-triMe-4- (3,4-deH-PiP) 2-2665 4- F-Ph 4-Pyr 2-Me-4- (3,4-deH-Pip) 2-2666 4-F-Ph 4-Pyr 1,2-diMe-4- (3,4-deH-Pip) 2 -2667 4-F-Ph 4-Pyr 1-Et-2-Me-4- (3,4-deH-Pip) 2-2668 4-F-Ph 4-Pyr 1-Pr-2-Me-4- (3,4-deH-Pip) 2-2669 4-F-Ph 4-Pyr 1-Bu-2-Me-4- (3,4-deH-Pip) 2-2670 4-F-Ph 4-Pyr 1-Phet-2-Me-4- (3,4-deH-Pip) 2-2671 4-F-Ph 4-Pyr 2-Et-4- (3,4-deH-Pip) 2-2672 4- F-Ph 4-Pyr 1-Me-2-Et-4- (3,4-deH-Pip) 2-2673 4-F-Ph 4-Pyr 1,2-diEt-4- (3,4-deH-Pip) 2-2674 4-F-Ph 4-Pyr 1-Pr-2-Et-4- ( 3,4-deH-Pip) 2-2675 4-F-Ph 4-Pyr 1-Bu-2-Et-4- (3,4-deH-Pip) 2-2676 4-F-Ph 4-Pyr 1 -Phet-2-Et-4- (3,4-deH-Pip) 2-2677 4-F-Ph 4-Pyr 2-Pr-4- (3,4-deH-Pip) 2-2678 4-F -Ph 4-Pyr 1-Me-2-Pr-4- (3,4-deH-Pip) 2-2679 4-F-Ph 4-Pyr 1-Et-2-Pr-4- (3,4- deH-Pip) 2-2680 4-F-Ph 4-Pyr 1,2-diPr-4- (3,4-deH-Pip) 2-2681 4-F-Ph 4-Pyr 1-Bu-2-Pr -4- (3,4-deH-Pip) 2-2682 4-F-Ph 4-Pyr 1-Phet-2-Pr-4- (3,4-deH-Pip) 2-2683 4-F-Ph 4-Pyr 2-Bu-4- (3,4-deH-Pip) 2-2684 4-F-Ph 4-Pyr 1-Me-2-Bu-4- (3,4-deH-Pip) 2- 2685 4-F-Ph 4-Pyr 1-Et-2-Bu-4- (3,4-deH-Pip) 2-2686 4-F-Ph 4-Pyr 1-Pr-2-Bu-4- ( 3,4-deH-Pip) 2-2687 4-F-Ph 4-Pyr 1,2-diBu-4- (3,4-deH-Pip) 2-2688 4-F-Ph 4-Pyr 1-Phet -2-Bu-4- (3,4-deH-Pip) 2-2689 4-F-Ph 4-Pyr 2-Allyl-4- (3,4-deH-Pip) 2-2690 4-F-Ph 4-Pyr 1-Me-2-Allyl-4- (3,4-deH-Pip) 2-2691 4-F-Ph 4-Pyr 1-Et-2-Allyl-4- (3,4-deH- Pip) 2-2692 4-F-Ph 4-Pyr 1-Pr-2-Allyl-4- (3,4-deH-Pip) 2-2693 4-F-Ph 4-Pyr 1-Bu-2-Allyl -4- (3,4-deH-Pip) 2-2694 4-F-Ph 4-Pyr 1-Phet-2-Al lyl-4- (3,4-deH-Pip) 2-2695 4-F-Ph 4-Pyr 2-Bn-4- (3,4-deH-Pip) 2-2696 4-F-Ph 4-Pyr 1-Me-2-Bn-4- (3,4-deH-Pip) 2-2697 4-F-Ph 4-Pyr 1-Et-2-Bn-4- (3,4-deH-Pip) 2 -2698 4-F-Ph 4-Pyr 1-Pr-2-Bn-4- (3,4-deH-Pip) 2-2699 4-F-Ph 4-Pyr 1-Bu-2-Bn-4- (3,4-deH-Pip) 2-2700 4-F-Ph 4-Pyr 1-Phet-2-Bn-4- (3,4-deH-Pip) 2-2701 4-F-Ph 4-Pyr 2-Phet-4- (3,4-deH-Pip) 2-2702 4-F-Ph 4-Pyr 1-Me-2-Phet-4- (3,4-deH-Pip) 2-2703 4- F-Ph 4-Pyr 1-Et-2-Phet-4- (3,4-deH-Pip) 2-2704 4-F-Ph 4-Pyr 1-Pr-2-Phet-4- (3,4 -deH-Pip) 2-2705 4-F-Ph 4-Pyr 1-Bu-2-Phet-4- (3,4-deH-Pip) 2-2706 4-F-Ph 4-Pyr 1,2- diPhet-4- (3,4-deH-Pip) 2-2707 4-F-Ph 4-Pyr 2-Me-4- (4,5-deH-Pip) 2-2708 4-F-Ph 4-Pyr 1,2-diMe-4- (4,5-deH-Pip) 2-2709 4-F-Ph 4-Pyr 1-Et-2-Me-4- (4,5-deH-Pip) 2-2710 4-F-Ph 4-Pyr 1-Pr-2-Me-4- (4,5-deH-Pip) 2-2711 4-F-Ph 4-Pyr 1-Bu-2-Me-4- (4 , 5-deH-Pip) 2-2712 4-F-Ph 4-Pyr 1-Phet-2-Me-4- (4,5-deH-Pip) 2-2713 4-F-Ph 4-Pyr 2- Et-4- (4,5-deH-Pip) 2-2714 4-F-Ph 4-Pyr 1-Me-2-Et-4- (4,5-deH-Pip) 2-2715 4-F- Ph 4-Pyr 1,2-diEt-4- (4,5-deH-Pip) 2-2716 4-F-Ph 4-Pyr 1 -Pr-2-Et-4- (4,5-deH-Pip) 2-2717 4-F-Ph 4-Pyr 1-Bu-2-Et-4- (4,5-deH-Pip) 2- 2718 4-F-Ph 4-Pyr 1-Phet-2-Et-4- (4,5-deH-Pip) 2-2719 4-F-Ph 4-Pyr 2-Pr-4- (4,5- deH-Pip) 2-2720 4-F-Ph 4-Pyr 1-Me-2-Pr-4- (4,5-deH-Pip) 2-2721 4-F-Ph 4-Pyr 1-Et-2 -Pr-4- (4,5-deH-Pip) 2-2722 4-F-Ph 4-Pyr 1,2-diPr-4- (4,5-deH-Pip) 2-2723 4-F-Ph 4-Pyr 1-Bu-2-Pr-4- (4,5-deH-Pip) 2-2724 4-F-Ph 4-Pyr 1-Phet-2-Pr-4- (4,5-deH- Pip) 2-2725 4-F-Ph 4-Pyr 2-Bu-4- (4,5-deH-Pip) 2-2726 4-F-Ph 4-Pyr 1-Me-2-Bu-4- ( 4,5-deH-Pip) 2-2727 4-F-Ph 4-Pyr 1-Et-2-Bu-4- (4,5-deH-Pip) 2-2728 4-F-Ph 4-Pyr 1 -Pr-2-Bu-4- (4,5-deH-Pip) 2-2729 4-F-Ph 4-Pyr 1,2-diBu-4- (4,5-deH-Pip) 2-2730 4 -F-Ph 4-Pyr 1-Phet-2-Bu-4- (4,5-deH-Pip) 2-2731 4-F-Ph 4-Pyr 2-Allyl-4- (4,5-deH- Pip) 2-2732 4-F-Ph 4-Pyr 1-Me-2-Allyl-4- (4,5-deH-Pip) 2-2733 4-F-Ph 4-Pyr 1-Et-2-Allyl -4- (4,5-deH-Pip) 2-2734 4-F-Ph 4-Pyr 1-Pr-2-Allyl-4- (4,5-deH-Pip) 2-2735 4-F-Ph 4-Pyr 1-Bu-2-Allyl-4- (4,5-deH-Pip) 2-2736 4-F-Ph 4-Pyr 1-Phet-2-Allyl-4- (4,5-deH- Pip) 2-2737 4-F-Ph 4-Pyr 2-Bn-4- (4,5-deH-Pip) 2-273 8 4-F-Ph 4-Pyr 1-Me-2-Bn-4- (4,5-deH-Pip) 2-2739 4-F-Ph 4-Pyr 1-Et-2-Bn-4- ( 4,5-deH-Pip) 2-2740 4-F-Ph 4-Pyr 1-Pr-2-Bn-4- (4,5-deH-Pip) 2-2741 4-F-Ph 4-Pyr 1 -Bu-2-Bn-4- (4,5-deH-Pip) 2-2742 4-F-Ph 4-Pyr 1-Phet-2-Bn-4- (4,5-deH-Pip) 2- 2743 4-F-Ph 4-Pyr 2-Phet-4- (4,5-deH-Pip) 2-2744 4-F-Ph 4-Pyr 1-Me-2-Phet-4- (4,5- deH-Pip) 2-2745 4-F-Ph 4-Pyr 1-Et-2-Phet-4- (4,5-deH-Pip) 2-2746 4-F-Ph 4-Pyr 1-Pr-2 -Phet-4- (4,5-deH-Pip) 2-2747 4-F-Ph 4-Pyr 1-Bu-2-Phet-4- (4,5-deH-Pip) 2-2748 4-F -Ph 4-Pyr 1,2-diPhet-4- (4,5-deH-Pip) 2-2749 4-F-Ph 2-NH _Two -4-Pym H _Two N-CH _Two C (Me) _Two CH _Two 2-2750 4-F-Ph 2-NH _Two -4-Pym MeNH-CH _Two C (Me) _Two CH _Two 2-2751 4-F-Ph 2-NH _Two -4-Pym EtNH-CH _Two C (Me) _Two CH _Two 2-2752 4-F-Ph 2-NH _Two -4-Pym Me _Two N-CH _Two C (Me) _Two CH _Two 2-2753 4-F-Ph 2-NH _Two -4-Pym 3- (3,4-deH-Pip) 2-2754 4-F-Ph 2-NH _Two -4-Pym 1-Me-3- (3,4-deH-Pip) 2-2755 4-F-Ph 2-NH _Two -4-Pym 1-Et-4- (3,4-deH-Pip) 2-2756 4-F-Ph 2-NH _Two -4-Pym 1-Pr-4- (3,4-deH-Pip) 2-2757 4-F-Ph 2-NH _Two -4-Pym 1-Pr-4-Pip 2-2758 4-F-Ph 2-NH _Two -4-Pym 1-iPr-4- (3,4-deH-Pip) 2-2759 4-F-Ph 2-NH _Two -4-Pym 1-iPr-4-Pip 2-2760 4-F-Ph 2-NH _Two -4-Pym 1-Bu-4- (3,4-deH-Pip) 2-2761 4-F-Ph 2-NH _Two -4-Pym 1-tBu-4- (3,4-deH-Pip) 2-2762 4-F-Ph 2-NH _Two -4-Pym 1-Pn-4- (3,4-deH-Pip) 2-2763 4-F-Ph 2-NH _Two -4-Pym 1-Hx-4- (3,4-deH-Pip) 2-2764 4-F-Ph 2-NH _Two -4-Pym 1-Hp-4- (3,4-deH-Pip) 2-2765 4-F-Ph 2-NH _Two -4-Pym 1-Oc-4- (3,4-deH-Pip) 2-2766 4-F-Ph 2-NH _Two -4-Pym 1-Nn-4- (3,4-deH-Pip) 2-2767 4-F-Ph 2-NH _Two -4-Pym 1-cPr-4- (3,4-deH-Pip) 2-2768 4-F-Ph 2-NH _Two -4-Pym 1-cPn-4- (3,4-deH-Pip) 2-2769 4-F-Ph 2-NH _Two -4-Pym 1-cHx-4- (3,4-deH-Pip) 2-2770 4-F-Ph 2-NH _Two -4-Pym 1-Bn-4- (3,4-deH-Pip) 2-2771 4-F-Ph 2-NH _Two -4-Pym 1-Phet-4- (3,4-deH-Pip) 2-2772 4-F-Ph 2-NH _Two -4-Pym 1- (3-Ph-Pr) -4- (3,4-deH-Pip) 2-2773 4-F-Ph 2-NH _Two -4-Pym 1- (4-Ph-Bu) -4- (3,4-deH-Pip) 2-2774 4-F-Ph 2-NH _Two -4-Pym 1-Allyl-4- (3,4-deH-Pip) 2-2775 4-F-Ph 2-NH _Two -4-Pym 1-Propargyl-4- (3,4-deH-Pip) 2-2776 4-F-Ph 2-NH _Two -4-Pym 2,2,6,6, -tetraMe-4- (3,4-deH-Pip) 2-2777 4-F-Ph 2-NH _Two -4-Pym 1,2,2,6,6, -pentaMe-4- (3,4-deH-Pip) 2-2778 4-F-Ph 2-NH _Two -4-Pym 1,2,2,6,6, -pentaMe-4-Pip) 2-2779 4-F-Ph 2-NH _Two -4-Pym 7- (1,2,3,5,6,8a-hexaH-Ind) 2-2780 4-F-Ph 2-NH _Two -4-Pym 7- (1,2,3,5,8,8a-hexaH-Ind) 2-2781 4-F-Ph 2-NH _Two -4-Pym 7-octaH-Ind 2-2782 4-F-Ph 2-NH _Two -4-Pym 8- (1,3,4,6,7,9a-hexaH-2H-Qui) 2-2783 4-F-Ph 2-NH _Two -4-Pym 8- (1,3,4,6,9,9a-hexaH-2H-Qui) 2-2784 4-F-Ph 2-NH _Two -4-Pym 8-octaH-Qui 2-2785 4-F-Ph 2-NH _Two -4-Pym 2,2-diMe-4- (3,4-deH-PiP) 2-2786 4-F-Ph 2-NH _Two -4-Pym 1,2,2-triMe-4- (3,4-deH-PiP) 2-2787 4-F-Ph 2-NH _Two -4-Pym 2,2-diMe-4- (4,5-deH-PiP) 2-2788 4-F-Ph 2-NH _Two -4-Pym 1,2,2-triMe-4- (4,5-deH-PiP) 2-2789 4-F-Ph 2-NH _Two -4-Pym 2,6-diMe-4- (3,4-deH-PiP) 2-2790 4-F-Ph 2-NH _Two -4-Pym 1,2,6-triMe-4- (3,4-deH-PiP) 2-2791 4-F-Ph 2-NH _Two -4-Pym 2-Me-4- (3,4-deH-Pip) 2-2792 4-F-Ph 2-NH _Two -4-Pym 1,2-diMe-4- (3,4-deH-Pip) 2-2793 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Me-4- (3,4-deH-Pip) 2-2794 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Me-4- (3,4-deH-Pip) 2-2795 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Me-4- (3,4-deH-Pip) 2-2796 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Me-4- (3,4-deH-Pip) 2-2797 4-F-Ph 2-NH _Two -4-Pym 2-Et-4- (3,4-deH-Pip) 2-2798 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Et-4- (3,4-deH-Pip) 2-2799 4-F-Ph 2-NH _Two -4-Pym 1,2-diEt-4- (3,4-deH-Pip) 2-2800 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Et-4- (3,4-deH-Pip) 2-2801 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Et-4- (3,4-deH-Pip) 2-2802 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Et-4- (3,4-deH-Pip) 2-2803 4-F-Ph 2-NH _Two -4-Pym 2-Pr-4- (3,4-deH-Pip) 2-2804 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Pr-4- (3,4-deH-Pip) 2-2805 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Pr-4- (3,4-deH-Pip) 2-2806 4-F-Ph 2-NH _Two -4-Pym 1,2-diPr-4- (3,4-deH-Pip) 2-2807 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Pr-4- (3,4-deH-Pip) 2-2808 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Pr-4- (3,4-deH-Pip) 2-2809 4-F-Ph 2-NH _Two -4-Pym 2-Bu-4- (3,4-deH-Pip) 2-2810 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Bu-4- (3,4-deH-Pip) 2-2811 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Bu-4- (3,4-deH-Pip) 2-2812 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Bu-4- (3,4-deH-Pip) 2-2813 4-F-Ph 2-NH _Two -4-Pym 1,2-diBu-4- (3,4-deH-Pip) 2-2814 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Bu-4- (3,4-deH-Pip) 2-2815 4-F-Ph 2-NH _Two -4-Pym 2-Allyl-4- (3,4-deH-Pip) 2-2816 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Allyl-4- (3,4-deH-Pip) 2-2817 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Allyl-4- (3,4-deH-Pip) 2-2818 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Allyl-4- (3,4-deH-Pip) 2-2819 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Allyl-4- (3,4-deH-Pip) 2-2820 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Allyl-4- (3,4-deH-Pip) 2-2821 4-F-Ph 2-NH _Two -4-Pym 2-Bn-4- (3,4-deH-Pip) 2-2822 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Bn-4- (3,4-deH-Pip) 2-2823 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Bn-4- (3,4-deH-Pip) 2-2824 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Bn-4- (3,4-deH-Pip) 2-2825 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Bn-4- (3,4-deH-Pip) 2-2826 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Bn-4- (3,4-deH-Pip) 2-2827 4-F-Ph 2-NH _Two -4-Pym 2-Phet-4- (3,4-deH-Pip) 2-2828 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Phet-4- (3,4-deH-Pip) 2-2829 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Phet-4- (3,4-deH-Pip) 2-2830 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Phet-4- (3,4-deH-Pip) 2-2831 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Phet-4- (3,4-deH-Pip) 2-2832 4-F-Ph 2-NH _Two -4-Pym 1,2-diPhet-4- (3,4-deH-Pip) 2-2833 4-F-Ph 2-NH _Two -4-Pym 2-Me-4- (4,5-deH-Pip) 2-2834 4-F-Ph 2-NH _Two -4-Pym 1,2-diMe-4- (4,5-deH-Pip) 2-2835 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Me-4- (4,5-deH-Pip) 2-2836 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Me-4- (4,5-deH-Pip) 2-2837 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Me-4- (4,5-deH-Pip) 2-2838 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Me-4- (4,5-deH-Pip) 2-2839 4-F-Ph 2-NH _Two -4-Pym 2-Et-4- (4,5-deH-Pip) 2-2840 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Et-4- (4,5-deH-Pip) 2-2841 4-F-Ph 2-NH _Two -4-Pym 1,2-diEt-4- (4,5-deH-Pip) 2-2842 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Et-4- (4,5-deH-Pip) 2-2843 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Et-4- (4,5-deH-Pip) 2-2844 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Et-4- (4,5-deH-Pip) 2-2845 4-F-Ph 2-NH _Two -4-Pym 2-Pr-4- (4,5-deH-Pip) 2-2846 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Pr-4- (4,5-deH-Pip) 2-2847 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Pr-4- (4,5-deH-Pip) 2-2848 4-F-Ph 2-NH _Two -4-Pym 1,2-diPr-4- (4,5-deH-Pip) 2-2849 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Pr-4- (4,5-deH-Pip) 2-2850 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Pr-4- (4,5-deH-Pip) 2-2851 4-F-Ph 2-NH _Two -4-Pym 2-Bu-4- (4,5-deH-Pip) 2-2852 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Bu-4- (4,5-deH-Pip) 2-2853 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Bu-4- (4,5-deH-Pip) 2-2854 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Bu-4- (4,5-deH-Pip) 2-2855 4-F-Ph 2-NH _Two -4-Pym 1,2-diBu-4- (4,5-deH-Pip) 2-2856 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Bu-4- (4,5-deH-Pip) 2-2857 4-F-Ph 2-NH _Two -4-Pym 2-Allyl-4- (4,5-deH-Pip) 2-2858 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Allyl-4- (4,5-deH-Pip) 2-2859 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Allyl-4- (4,5-deH-Pip) 2-2860 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Allyl-4- (4,5-deH-Pip) 2-2861 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Allyl-4- (4,5-deH-Pip) 2-2862 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Allyl-4- (4,5-deH-Pip) 2-2863 4-F-Ph 2-NH _Two -4-Pym 2-Bn-4- (4,5-deH-Pip) 2-2864 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Bn-4- (4,5-deH-Pip) 2-2865 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Bn-4- (4,5-deH-Pip) 2-2866 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Bn-4- (4,5-deH-Pip) 2-2867 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Bn-4- (4,5-deH-Pip) 2-2868 4-F-Ph 2-NH _Two -4-Pym 1-Phet-2-Bn-4- (4,5-deH-Pip) 2-2869 4-F-Ph 2-NH _Two -4-Pym 2-Phet-4- (4,5-deH-Pip) 2-2870 4-F-Ph 2-NH _Two -4-Pym 1-Me-2-Phet-4- (4,5-deH-Pip) 2-2871 4-F-Ph 2-NH _Two -4-Pym 1-Et-2-Phet-4- (4,5-deH-Pip) 2-2872 4-F-Ph 2-NH _Two -4-Pym 1-Pr-2-Phet-4- (4,5-deH-Pip) 2-2873 4-F-Ph 2-NH _Two -4-Pym 1-Bu-2-Phet-4- (4,5-deH-Pip) 2-2874 4-F-Ph 2-NH _Two -4-Pym 1,2-diPhet-4- (4,5-deH-Pip) 2-2875 4-F-Ph 2-MeNH-4-Pym H _Two N-CH _Two C (Me) _Two CH _Two 2-2876 4-F-Ph 2-MeNH-4-Pym MeNH-CH _Two C (Me) _Two CH _Two 2-2877 4-F-Ph 2-MeNH-4-Pym EtNH-CH _Two C (Me) _Two CH _Two 2-2878 4-F-Ph 2-MeNH-4-Pym Me _Two N-CH _Two C (Me) _Two CH _Two 2-2879 4-F-Ph 2-MeNH-4-Pym 3- (3,4-deH-Pip) 2-2880 4-F-Ph 2-MeNH-4-Pym 1-Me-3- (3, 4-deH-Pip) 2-2881 4-F-Ph 2-MeNH-4-Pym 1-Et-4- (3,4-deH-Pip) 2-2882 4-F-Ph 2-MeNH-4- Pym 1-Pr-4- (3,4-deH-Pip) 2-2883 4-F-Ph 2-MeNH-4-Pym 1-Pr-4-Pip 2-2884 4-F-Ph 2-MeNH- 4-Pym 1-iPr-4- (3,4-deH-Pip) 2-2885 4-F-Ph 2-MeNH-4-Pym 1-iPr-4-Pip 2-2886 4-F-Ph 2- MeNH-4-Pym 1-Bu-4- (3,4-deH-Pip) 2-2887 4-F-Ph 2-MeNH-4-Pym 1-tBu-4- (3,4-deH-Pip) 2-2888 4-F-Ph 2-MeNH-4-Pym 1-Pn-4- (3,4-deH-Pip) 2-2889 4-F-Ph 2-MeNH-4-Pym 1-Hx-4 -(3,4-deH-Pip) 2-2890 4-F-Ph 2-MeNH-4-Pym 1-Hp-4- (3,4-deH-Pip) 2-2891 4-F-Ph 2- MeNH-4-Pym 1-Oc-4- (3,4-deH-Pip) 2-2892 4-F-Ph 2-MeNH-4-Pym 1-Nn-4- (3,4-deH-Pip) 2-2893 4-F-Ph 2-MeNH-4-Pym 1-cPr-4- (3,4-deH-Pip) 2-2894 4-F-Ph 2-MeNH-4-Pym 1-cPn-4 -(3,4-deH-Pip) 2-2895 4-F-Ph 2-MeNH-4-Pym 1-cHx-4- (3,4-deH-Pip) 2-2896 4-F-Ph 2- MeNH-4-Pym 1-Bn-4- (3,4-deH-Pip) 2-2897 4-F-Ph 2-MeNH-4-Pym 1-Phet-4- (3,4-deH-Pip) 2-2898 4-F-Ph 2-MeNH-4-Pym 1- (3-Ph-Pr) -4- (3,4-deH-Pip) 2-2899 4-F-Ph 2-MeNH-4- Pym 1- (4-Ph-Bu) -4- (3,4-deH- Pip) 2-2900 4-F-Ph 2-MeNH-4-Pym 1-Allyl-4- (3,4-deH-Pip) 2-2901 4-F-Ph 2-MeNH-4-Pym 1-Propargyl -4- (3,4-deH-Pip) 2-2902 4-F-Ph 2-MeNH-4-Pym 2,2,6,6, -tetraMe-4- (3,4-deH-Pip) 2 -2903 4-F-Ph 2-MeNH-4-Pym 1,2,2,6,6, -pentaMe-4- (3,4-deH-Pip) 2-2904 4-F-Ph 2-MeNH- 4-Pym 1,2,2,6,6, -pentaMe-4-Pip) 2-2905 4-F-Ph 2-MeNH-4-Pym 7- (1,2,3,5,6,8a- hexaH-Ind) 2-2906 4-F-Ph 2-MeNH-4-Pym 7- (1,2,3,5,8,8a-hexaH-Ind) 2-2907 4-F-Ph 2-MeNH- 4-Pym 7-octaH-Ind 2-2908 4-F-Ph 2-MeNH-4-Pym 8- (1,3,4,6,7,9a-hexaH-2H-Qui) 2-2909 4-F -Ph 2-MeNH-4-Pym 8- (1,3,4,6,9,9a-hexaH-2H-Qui) 2-2910 4-F-Ph 2-MeNH-4-Pym 8-octaH-Qui 2-2911 4-F-Ph 2-MeNH-4-Pym 2,2-diMe-4- (3,4-deH-PiP) 2-2912 4-F-Ph 2-MeNH-4-Pym 1,2 , 2-triMe-4- (3,4-deH-PiP) 2-2913 4-F-Ph 2-MeNH-4-Pym 2,2-diMe-4- (4,5-deH-PiP) 2- 2914 4-F-Ph 2-MeNH-4-Pym 1,2,2-triMe-4- (4,5-deH-PiP) 2-2915 4-F-Ph 2-MeNH-4-Pym 2,6 -diMe-4- (3,4-deH-PiP) 2-2916 4-F-Ph 2-MeNH-4-Pym 1,2,6-triMe-4- (3,4-deH-PiP) 2- 2917 4-F-Ph 2-MeNH-4-Pym 2-Me-4- (3,4-deH-Pip) 2-2918 4-F-Ph 2-MeNH-4-Pym 1,2-diMe-4 -(3,4-de H-Pip) 2-2919 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Me-4- (3,4-deH-Pip) 2-2920 4-F-Ph 2-MeNH- 4-Pym 1-Pr-2-Me-4- (3,4-deH-Pip) 2-2921 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Me-4- (3, 4-deH-Pip) 2-2922 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Me-4- (3,4-deH-Pip) 2-2923 4-F-Ph 2- MeNH-4-Pym 2-Et-4- (3,4-deH-Pip) 2-2924 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Et-4- (3,4- deH-Pip) 2-2925 4-F-Ph 2-MeNH-4-Pym 1,2-diEt-4- (3,4-deH-Pip) 2-2926 4-F-Ph 2-MeNH-4- Pym 1-Pr-2-Et-4- (3,4-deH-Pip) 2-2927 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Et-4- (3,4- deH-Pip) 2-2928 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Et-4- (3,4-deH-Pip) 2-2929 4-F-Ph 2-MeNH- 4-Pym 2-Pr-4- (3,4-deH-Pip) 2-2930 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Pr-4- (3,4-deH- Pip) 2-2931 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Pr-4- (3,4-deH-Pip) 2-2932 4-F-Ph 2-MeNH-4- Pym 1,2-diPr-4- (3,4-deH-Pip) 2-2933 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Pr-4- (3,4-deH- Pip) 2-2934 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Pr-4- (3,4-deH-Pip) 2-2935 4-F-Ph 2-MeNH-4- Pym 2-Bu-4- (3,4-deH-Pip) 2-2936 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Bu-4- (3,4-deH-Pip) 2-2937 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Bu-4- (3,4-deH-Pi p) 2-2938 4-F-Ph 2-MeNH-4-Pym 1-Pr-2-Bu-4- (3,4-deH-Pip) 2-2939 4-F-Ph 2-MeNH-4- Pym 1,2-diBu-4- (3,4-deH-Pip) 2-2940 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Bu-4- (3,4-deH- Pip) 2-2941 4-F-Ph 2-MeNH-4-Pym 2-Allyl-4- (3,4-deH-Pip) 2-2942 4-F-Ph 2-MeNH-4-Pym 1-Me -2-Allyl-4- (3,4-deH-Pip) 2-2943 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Allyl-4- (3,4-deH-Pip) 2-2944 4-F-Ph 2-MeNH-4-Pym 1-Pr-2-Allyl-4- (3,4-deH-Pip) 2-2945 4-F-Ph 2-MeNH-4-Pym 1 -Bu-2-Allyl-4- (3,4-deH-Pip) 2-2946 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Allyl-4- (3,4-deH- Pip) 2-2947 4-F-Ph 2-MeNH-4-Pym 2-Bn-4- (3,4-deH-Pip) 2-2948 4-F-Ph 2-MeNH-4-Pym 1-Me -2-Bn-4- (3,4-deH-Pip) 2-2949 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Bn-4- (3,4-deH-Pip) 2-2950 4-F-Ph 2-MeNH-4-Pym 1-Pr-2-Bn-4- (3,4-deH-Pip) 2-2951 4-F-Ph 2-MeNH-4-Pym 1 -Bu-2-Bn-4- (3,4-deH-Pip) 2-2952 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Bn-4- (3,4-deH- Pip) 2-2953 4-F-Ph 2-MeNH-4-Pym 2-Phet-4- (3,4-deH-Pip) 2-2954 4-F-Ph 2-MeNH-4-Pym 1-Me -2-Phet-4- (3,4-deH-Pip) 2-2955 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Phet-4- (3,4-deH-Pip) 2-2956 4-F-Ph 2-MeNH-4-Pym 1- Pr-2-Phet-4- (3,4-deH-Pip) 2-2957 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Phet-4- (3,4-deH-Pip ) 2-2958 4-F-Ph 2-MeNH-4-Pym 1,2-diPhet-4- (3,4-deH-Pip) 2-2959 4-F-Ph 2-MeNH-4-Pym 2- Me-4- (4,5-deH-Pip) 2-2960 4-F-Ph 2-MeNH-4-Pym 1,2-diMe-4- (4,5-deH-Pip) 2-2961 4- F-Ph 2-MeNH-4-Pym 1-Et-2-Me-4- (4,5-deH-Pip) 2-2962 4-F-Ph 2-MeNH-4-Pym 1-Pr-2- Me-4- (4,5-deH-Pip) 2-2963 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Me-4- (4,5-deH-Pip) 2-2964 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Me-4- (4,5-deH-Pip) 2-2965 4-F-Ph 2-MeNH-4-Pym 2-Et- 4- (4,5-deH-Pip) 2-2966 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Et-4- (4,5-deH-Pip) 2-2967 4- F-Ph 2-MeNH-4-Pym 1,2-diEt-4- (4,5-deH-Pip) 2-2968 4-F-Ph 2-MeNH-4-Pym 1-Pr-2-Et- 4- (4,5-deH-Pip) 2-2969 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Et-4- (4,5-deH-Pip) 2-2970 4- F-Ph 2-MeNH-4-Pym 1-Phet-2-Et-4- (4,5-deH-Pip) 2-2971 4-F-Ph 2-MeNH-4-Pym 2-Pr-4- (4,5-deH-Pip) 2-2972 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Pr-4- (4,5-deH-Pip) 2-2973 4-F- Ph 2-MeNH-4-Pym 1-Et-2-Pr-4- (4,5-deH-Pip) 2-2974 4-F-Ph 2-MeNH-4-Pym 1,2-diPr-4- (4,5-deH-Pip) 2-2975 4-F-Ph 2-MeNH-4-Pym 1-Bu -2-Pr-4- (4,5-deH-Pip) 2-2976 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Pr-4- (4,5-deH-Pip) 2-2977 4-F-Ph 2-MeNH-4-Pym 2-Bu-4- (4,5-deH-Pip) 2-2978 4-F-Ph 2-MeNH-4-Pym 1-Me-2 -Bu-4- (4,5-deH-Pip) 2-2979 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Bu-4- (4,5-deH-Pip) 2- 2980 4-F-Ph 2-MeNH-4-Pym 1-Pr-2-Bu-4- (4,5-deH-Pip) 2-2981 4-F-Ph 2-MeNH-4-Pym 1,2 -diBu-4- (4,5-deH-Pip) 2-2982 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Bu-4- (4,5-deH-Pip) 2- 2983 4-F-Ph 2-MeNH-4-Pym 2-Allyl-4- (4,5-deH-Pip) 2-2984 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Allyl -4- (4,5-deH-Pip) 2-2985 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Allyl-4- (4,5-deH-Pip) 2-2986 4 -F-Ph 2-MeNH-4-Pym 1-Pr-2-Allyl-4- (4,5-deH-Pip) 2-2987 4-F-Ph 2-MeNH-4-Pym 1-Bu-2 -Allyl-4- (4,5-deH-Pip) 2-2988 4-F-Ph 2-MeNH-4-Pym 1-Phet-2-Allyl-4- (4,5-deH-Pip) 2- 2989 4-F-Ph 2-MeNH-4-Pym 2-Bn-4- (4,5-deH-Pip) 2-2990 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Bn -4- (4,5-deH-Pip) 2-2991 4-F-Ph 2-MeNH-4-Pym 1-Et-2-Bn-4- (4,5-deH-Pip) 2-2992 4 -F-Ph 2-MeNH-4-Pym 1-Pr-2-Bn-4- (4,5-deH-Pip) 2-2993 4-F-Ph 2-MeNH-4-Pym 1-Bu-2 -Bn-4- (4,5-deH-Pip) 2-2994 4-F-Ph 2- MeNH-4-Pym 1-Phet-2-Bn-4- (4,5-deH-Pip) 2-2995 4-F-Ph 2-MeNH-4-Pym 2-Phet-4- (4,5- deH-Pip) 2-2996 4-F-Ph 2-MeNH-4-Pym 1-Me-2-Phet-4- (4,5-deH-Pip) 2-2997 4-F-Ph 2-MeNH- 4-Pym 1-Et-2-Phet-4- (4,5-deH-Pip) 2-2998 4-F-Ph 2-MeNH-4-Pym 1-Pr-2-Phet-4- (4, 5-deH-Pip) 2-2999 4-F-Ph 2-MeNH-4-Pym 1-Bu-2-Phet-4- (4,5-deH-Pip) 2-3000 4-F-Ph 2- MeNH-4-Pym 1,2-diPhet-4- (4,5-deH-Pip) 2-3001 4-F-Ph 2-NH _Two -4-Pyr H _Two N-CH _Two C (Me) _Two CH _Two 2-3002 4-F-Ph 2-NH _Two -4-Pyr MeNH-CH _Two C (Me) _Two CH _Two 2-3003 4-F-Ph 2-NH _Two -4-Pyr EtNH-CH _Two C (Me) _Two CH _Two 2-3004 4-F-Ph 2-NH _Two -4-Pyr Me _Two N-CH _Two C (Me) _Two CH _Two 2-3005 4-F-Ph 2-NH _Two -4-Pyr 3- (3,4-deH-Pip) 2-3006 4-F-Ph 2-NH _Two -4-Pyr 1-Me-3- (3,4-deH-Pip) 2-3007 4-F-Ph 2-NH _Two -4-Pyr 1-Et-4- (3,4-deH-Pip) 2-3008 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-4- (3,4-deH-Pip) 2-3009 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-4-Pip 2-3010 4-F-Ph 2-NH _Two -4-Pyr 1-iPr-4- (3,4-deH-Pip) 2-3011 4-F-Ph 2-NH _Two -4-Pyr 1-iPr-4-Pip 2-3012 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-4- (3,4-deH-Pip) 2-3013 4-F-Ph 2-NH _Two -4-Pyr 1-tBu-4- (3,4-deH-Pip) 2-3014 4-F-Ph 2-NH _Two -4-Pyr 1-Pn-4- (3,4-deH-Pip) 2-3015 4-F-Ph 2-NH _Two -4-Pyr 1-Hx-4- (3,4-deH-Pip) 2-3016 4-F-Ph 2-NH _Two -4-Pyr 1-Hp-4- (3,4-deH-Pip) 2-3017 4-F-Ph 2-NH _Two -4-Pyr 1-Oc-4- (3,4-deH-Pip) 2-3018 4-F-Ph 2-NH _Two -4-Pyr 1-Nn-4- (3,4-deH-Pip) 2-3019 4-F-Ph 2-NH _Two -4-Pyr 1-cPr-4- (3,4-deH-Pip) 2-3020 4-F-Ph 2-NH _Two -4-Pyr 1-cPn-4- (3,4-deH-Pip) 2-3021 4-F-Ph 2-NH _Two -4-Pyr 1-cHx-4- (3,4-deH-Pip) 2-3022 4-F-Ph 2-NH _Two -4-Pyr 1-Bn-4- (3,4-deH-Pip) 2-3023 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-4- (3,4-deH-Pip) 2-3024 4-F-Ph 2-NH _Two -4-Pyr 1- (3-Ph-Pr) -4- (3,4-deH-Pip) 2-3025 4-F-Ph 2-NH _Two -4-Pyr 1- (4-Ph-Bu) -4- (3,4-deH-Pip) 2-3026 4-F-Ph 2-NH _Two -4-Pyr 1-Allyl-4- (3,4-deH-Pip) 2-3027 4-F-Ph 2-NH _Two -4-Pyr 1-Propargyl-4- (3,4-deH-Pip) 2-3028 4-F-Ph 2-NH _Two -4-Pyr 2,2,6,6, -tetraMe-4- (3,4-deH-Pip) 2-3029 4-F-Ph 2-NH _Two -4-Pyr 1,2,2,6,6, -pentaMe-4- (3,4-deH-Pip) 2-3030 4-F-Ph 2-NH _Two -4-Pyr 1,2,2,6,6, -pentaMe-4-Pip) 2-3031 4-F-Ph 2-NH _Two -4-Pyr 7- (1,2,3,5,6,8a-hexaH-Ind) 2-3032 4-F-Ph 2-NH _Two -4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 2-3033 4-F-Ph 2-NH _Two -4-Pyr 7-octaH-Ind 2-3034 4-F-Ph 2-NH _Two -4-Pyr 8- (1,3,4,6,7,9a-hexaH-2H-Qui) 2-3035 4-F-Ph 2-NH _Two -4-Pyr 8- (1,3,4,6,9,9a-hexaH-2H-Qui) 2-3036 4-F-Ph 2-NH _Two -4-Pyr 8-octaH-Qui 2-3037 4-F-Ph 2-NH _Two -4-Pyr 2,2-diMe-4- (3,4-deH-PiP) 2-3038 4-F-Ph 2-NH _Two -4-Pyr 1,2,2-triMe-4- (3,4-deH-PiP) 2-3039 4-F-Ph 2-NH _Two -4-Pyr 2,2-diMe-4- (4,5-deH-PiP) 2-3040 4-F-Ph 2-NH _Two -4-Pyr 1,2,2-triMe-4- (4,5-deH-PiP) 2-3041 4-F-Ph 2-NH _Two -4-Pyr 2,6-diMe-4- (3,4-deH-PiP) 2-3042 4-F-Ph 2-NH _Two -4-Pyr 1,2,6-triMe-4- (3,4-deH-PiP) 2-3043 4-F-Ph 2-NH _Two -4-Pyr 2-Me-4- (3,4-deH-Pip) 2-3044 4-F-Ph 2-NH _Two -4-Pyr 1,2-diMe-4- (3,4-deH-Pip) 2-3045 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Me-4- (3,4-deH-Pip) 2-3046 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Me-4- (3,4-deH-Pip) 2-3047 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Me-4- (3,4-deH-Pip) 2-3048 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Me-4- (3,4-deH-Pip) 2-3049 4-F-Ph 2-NH _Two -4-Pyr 2-Et-4- (3,4-deH-Pip) 2-3050 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Et-4- (3,4-deH-Pip) 2-3051 4-F-Ph 2-NH _Two -4-Pyr 1,2-diEt-4- (3,4-deH-Pip) 2-3052 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Et-4- (3,4-deH-Pip) 2-3053 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Et-4- (3,4-deH-Pip) 2-3054 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Et-4- (3,4-deH-Pip) 2-3055 4-F-Ph 2-NH _Two -4-Pyr 2-Pr-4- (3,4-deH-Pip) 2-3056 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Pr-4- (3,4-deH-Pip) 2-3057 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Pr-4- (3,4-deH-Pip) 2-3058 4-F-Ph 2-NH _Two -4-Pyr 1,2-diPr-4- (3,4-deH-Pip) 2-3059 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Pr-4- (3,4-deH-Pip) 2-3060 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Pr-4- (3,4-deH-Pip) 2-3061 4-F-Ph 2-NH _Two -4-Pyr 2-Bu-4- (3,4-deH-Pip) 2-3062 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Bu-4- (3,4-deH-Pip) 2-3063 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Bu-4- (3,4-deH-Pip) 2-3064 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Bu-4- (3,4-deH-Pip) 2-3065 4-F-Ph 2-NH _Two -4-Pyr 1,2-diBu-4- (3,4-deH-Pip) 2-3066 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Bu-4- (3,4-deH-Pip) 2-3067 4-F-Ph 2-NH _Two -4-Pyr 2-Allyl-4- (3,4-deH-Pip) 2-3068 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Allyl-4- (3,4-deH-Pip) 2-3069 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Allyl-4- (3,4-deH-Pip) 2-3070 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Allyl-4- (3,4-deH-Pip) 2-3071 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Allyl-4- (3,4-deH-Pip) 2-3072 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Allyl-4- (3,4-deH-Pip) 2-3073 4-F-Ph 2-NH _Two -4-Pyr 2-Bn-4- (3,4-deH-Pip) 2-3074 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Bn-4- (3,4-deH-Pip) 2-3075 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Bn-4- (3,4-deH-Pip) 2-3076 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Bn-4- (3,4-deH-Pip) 2-3077 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Bn-4- (3,4-deH-Pip) 2-3078 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Bn-4- (3,4-deH-Pip) 2-3079 4-F-Ph 2-NH _Two -4-Pyr 2-Phet-4- (3,4-deH-Pip) 2-3080 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Phet-4- (3,4-deH-Pip) 2-3081 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Phet-4- (3,4-deH-Pip) 2-3082 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Phet-4- (3,4-deH-Pip) 2-3083 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Phet-4- (3,4-deH-Pip) 2-3084 4-F-Ph 2-NH _Two -4-Pyr 1,2-diPhet-4- (3,4-deH-Pip) 2-3085 4-F-Ph 2-NH _Two -4-Pyr 2-Me-4- (4,5-deH-Pip) 2-3086 4-F-Ph 2-NH _Two -4-Pyr 1,2-diMe-4- (4,5-deH-Pip) 2-3087 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Me-4- (4,5-deH-Pip) 2-3088 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Me-4- (4,5-deH-Pip) 2-3089 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Me-4- (4,5-deH-Pip) 2-3090 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Me-4- (4,5-deH-Pip) 2-3091 4-F-Ph 2-NH _Two -4-Pyr 2-Et-4- (4,5-deH-Pip) 2-3092 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Et-4- (4,5-deH-Pip) 2-3093 4-F-Ph 2-NH _Two -4-Pyr 1,2-diEt-4- (4,5-deH-Pip) 2-3094 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Et-4- (4,5-deH-Pip) 2-3095 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Et-4- (4,5-deH-Pip) 2-3096 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Et-4- (4,5-deH-Pip) 2-3097 4-F-Ph 2-NH _Two -4-Pyr 2-Pr-4- (4,5-deH-Pip) 2-3098 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Pr-4- (4,5-deH-Pip) 2-3099 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Pr-4- (4,5-deH-Pip) 2-3100 4-F-Ph 2-NH _Two -4-Pyr 1,2-diPr-4- (4,5-deH-Pip) 2-3101 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Pr-4- (4,5-deH-Pip) 2-3102 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Pr-4- (4,5-deH-Pip) 2-3103 4-F-Ph 2-NH _Two -4-Pyr 2-Bu-4- (4,5-deH-Pip) 2-3104 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Bu-4- (4,5-deH-Pip) 2-3105 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Bu-4- (4,5-deH-Pip) 2-3106 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Bu-4- (4,5-deH-Pip) 2-3107 4-F-Ph 2-NH _Two -4-Pyr 1,2-diBu-4- (4,5-deH-Pip) 2-3108 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Bu-4- (4,5-deH-Pip) 2-3109 4-F-Ph 2-NH _Two -4-Pyr 2-Allyl-4- (4,5-deH-Pip) 2-3110 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Allyl-4- (4,5-deH-Pip) 2-3111 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Allyl-4- (4,5-deH-Pip) 2-3112 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Allyl-4- (4,5-deH-Pip) 2-3113 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Allyl-4- (4,5-deH-Pip) 2-3114 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Allyl-4- (4,5-deH-Pip) 2-3115 4-F-Ph 2-NH _Two -4-Pyr 2-Bn-4- (4,5-deH-Pip) 2-3116 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Bn-4- (4,5-deH-Pip) 2-3117 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Bn-4- (4,5-deH-Pip) 2-3118 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Bn-4- (4,5-deH-Pip) 2-3119 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Bn-4- (4,5-deH-Pip) 2-3120 4-F-Ph 2-NH _Two -4-Pyr 1-Phet-2-Bn-4- (4,5-deH-Pip) 2-3121 4-F-Ph 2-NH _Two -4-Pyr 2-Phet-4- (4,5-deH-Pip) 2-3122 4-F-Ph 2-NH _Two -4-Pyr 1-Me-2-Phet-4- (4,5-deH-Pip) 2-3123 4-F-Ph 2-NH _Two -4-Pyr 1-Et-2-Phet-4- (4,5-deH-Pip) 2-3124 4-F-Ph 2-NH _Two -4-Pyr 1-Pr-2-Phet-4- (4,5-deH-Pip) 2-3125 4-F-Ph 2-NH _Two -4-Pyr 1-Bu-2-Phet-4- (4,5-deH-Pip) 2-3126 4-F-Ph 2-NH _Two -4-Pyr 1,2-diPhet-4- (4,5-deH-Pip) 2-3127 4-F-Ph 2-MeNH-4-Pyr H _Two N-CH _Two C (Me) _Two CH _Two 2-3128 4-F-Ph 2-MeNH-4-Pyr MeNH-CH _Two C (Me) _Two CH _Two 2-3129 4-F-Ph 2-MeNH-4-Pyr EtNH-CH _Two C (Me) _Two CH _Two 2-3130 4-F-Ph 2-MeNH-4-Pyr Me _Two N-CH _Two C (Me) _Two CH _Two 2-3131 4-F-Ph 2-MeNH-4-Pyr 3- (3,4-deH-Pip) 2-3132 4-F-Ph 2-MeNH-4-Pyr 1-Me-3- (3, 4-deH-Pip) 2-3133 4-F-Ph 2-MeNH-4-Pyr 1-Et-4- (3,4-deH-Pip) 2-3134 4-F-Ph 2-MeNH-4- Pyr 1-Pr-4- (3,4-deH-Pip) 2-3135 4-F-Ph 2-MeNH-4-Pyr 1-Pr-4-Pip 2-3136 4-F-Ph 2-MeNH- 4-Pyr 1-iPr-4- (3,4-deH-Pip) 2-3137 4-F-Ph 2-MeNH-4-Pyr 1-iPr-4-Pip 2-3138 4-F-Ph 2- MeNH-4-Pyr 1-Bu-4- (3,4-deH-Pip) 2-3139 4-F-Ph 2-MeNH-4-Pyr 1-tBu-4- (3,4-deH-Pip) 2-3140 4-F-Ph 2-MeNH-4-Pyr 1-Pn-4- (3,4-deH-Pip) 2-3141 4-F-Ph 2-MeNH-4-Pyr 1-Hx-4 -(3,4-deH-Pip) 2-3142 4-F-Ph 2-MeNH-4-Pyr 1-Hp-4- (3,4-deH-Pip) 2-3143 4-F-Ph 2- MeNH-4-Pyr 1-Oc-4- (3,4-deH-Pip) 2-3144 4-F-Ph 2-MeNH-4-Pyr 1-Nn-4- (3,4-deH-Pip) 2-3145 4-F-Ph 2-MeNH-4-Pyr 1-cPr-4- (3,4-deH-Pip) 2-3146 4-F-Ph 2-MeNH-4-Pyr 1-cPn-4 -(3,4-deH-Pip) 2-3147 4-F-Ph 2-MeNH-4-Pyr 1-cHx-4- (3,4-deH-Pip) 2-3148 4-F-Ph 2- MeNH-4-Pyr 1-Bn-4- (3,4-deH-Pip) 2-3149 4-F-Ph 2-MeNH-4-Pyr 1-Phet-4- (3,4-deH-Pip) 2-3150 4-F-Ph 2-MeNH-4-Pyr 1- (3-Ph-Pr) -4- (3,4-deH-Pip) 2-3151 4-F-Ph 2-MeNH-4- Pyr 1- (4-Ph-Bu) -4- (3,4-deH- Pip) 2-3152 4-F-Ph 2-MeNH-4-Pyr 1-Allyl-4- (3,4-deH-Pip) 2-3153 4-F-Ph 2-MeNH-4-Pyr 1-Propargyl -4- (3,4-deH-Pip) 2-3154 4-F-Ph 2-MeNH-4-Pyr 2,2,6,6, -tetraMe-4- (3,4-deH-Pip) 2 -3155 4-F-Ph 2-MeNH-4-Pyr 1,2,2,6,6, -pentaMe-4- (3,4-deH-Pip) 2-3156 4-F-Ph 2-MeNH- 4-Pyr 1,2,2,6,6, -pentaMe-4-Pip) 2-3157 4-F-Ph 2-MeNH-4-Pyr 7- (1,2,3,5,6,8a- hexaH-Ind) 2-3158 4-F-Ph 2-MeNH-4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 2-3159 4-F-Ph 2-MeNH- 4-Pyr 7-octaH-Ind 2-3160 4-F-Ph 2-MeNH-4-Pyr 8- (1,3,4,6,7,9a-hexaH-2H-Qui) 2-3161 4-F -Ph 2-MeNH-4-Pyr 8- (1,3,4,6,9,9a-hexaH-2H-Qui) 2-3162 4-F-Ph 2-MeNH-4-Pyr 8-octaH-Qui 2-3163 4-F-Ph 2-MeNH-4-Pyr 2,2-diMe-4- (3,4-deH-PiP) 2-3164 4-F-Ph 2-MeNH-4-Pyr 1,2 , 2-triMe-4- (3,4-deH-PiP) 2-3165 4-F-Ph 2-MeNH-4-Pyr 2,2-diMe-4- (4,5-deH-PiP) 2- 3166 4-F-Ph 2-MeNH-4-Pyr 1,2,2-triMe-4- (4,5-deH-PiP) 2-3167 4-F-Ph 2-MeNH-4-Pyr 2,6 -diMe-4- (3,4-deH-PiP) 2-3168 4-F-Ph 2-MeNH-4-Pyr 1,2,6-triMe-4- (3,4-deH-PiP) 2- 3169 4-F-Ph 2-MeNH-4-Pyr 2-Me-4- (3,4-deH-Pip) 2-3170 4-F-Ph 2-MeNH-4-Pyr 1,2-diMe-4 -(3,4-de H-Pip) 2-3171 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Me-4- (3,4-deH-Pip) 2-3172 4-F-Ph 2-MeNH- 4-Pyr 1-Pr-2-Me-4- (3,4-deH-Pip) 2-3173 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Me-4- (3, 4-deH-Pip) 2-3174 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Me-4- (3,4-deH-Pip) 2-3175 4-F-Ph 2- MeNH-4-Pyr 2-Et-4- (3,4-deH-Pip) 2-3176 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Et-4- (3,4- deH-Pip) 2-3177 4-F-Ph 2-MeNH-4-Pyr 1,2-diEt-4- (3,4-deH-Pip) 2-3178 4-F-Ph 2-MeNH-4- Pyr 1-Pr-2-Et-4- (3,4-deH-Pip) 2-3179 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Et-4- (3,4- deH-Pip) 2-3180 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Et-4- (3,4-deH-Pip) 2-3181 4-F-Ph 2-MeNH- 4-Pyr 2-Pr-4- (3,4-deH-Pip) 2-3182 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Pr-4- (3,4-deH- Pip) 2-3183 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Pr-4- (3,4-deH-Pip) 2-3184 4-F-Ph 2-MeNH-4- Pyr 1,2-diPr-4- (3,4-deH-Pip) 2-3185 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Pr-4- (3,4-deH- Pip) 2-3186 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Pr-4- (3,4-deH-Pip) 2-3187 4-F-Ph 2-MeNH-4- Pyr 2-Bu-4- (3,4-deH-Pip) 2-3188 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Bu-4- (3,4-deH-Pip) 2-3189 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Bu-4- (3,4-deH-Pi p) 2-3190 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2-Bu-4- (3,4-deH-Pip) 2-3191 4-F-Ph 2-MeNH-4- Pyr 1,2-diBu-4- (3,4-deH-Pip) 2-3192 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Bu-4- (3,4-deH- Pip) 2-3193 4-F-Ph 2-MeNH-4-Pyr 2-Allyl-4- (3,4-deH-Pip) 2-3194 4-F-Ph 2-MeNH-4-Pyr 1-Me -2-Allyl-4- (3,4-deH-Pip) 2-3195 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Allyl-4- (3,4-deH-Pip) 2-3196 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2-Allyl-4- (3,4-deH-Pip) 2-3197 4-F-Ph 2-MeNH-4-Pyr 1 -Bu-2-Allyl-4- (3,4-deH-Pip) 2-3198 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Allyl-4- (3,4-deH- Pip) 2-3199 4-F-Ph 2-MeNH-4-Pyr 2-Bn-4- (3,4-deH-Pip) 2-3200 4-F-Ph 2-MeNH-4-Pyr 1-Me -2-Bn-4- (3,4-deH-Pip) 2-3201 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Bn-4- (3,4-deH-Pip) 2-3202 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2-Bn-4- (3,4-deH-Pip) 2-3203 4-F-Ph 2-MeNH-4-Pyr 1 -Bu-2-Bn-4- (3,4-deH-Pip) 2-3204 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Bn-4- (3,4-deH- Pip) 2-3205 4-F-Ph 2-MeNH-4-Pyr 2-Phet-4- (3,4-deH-Pip) 2-3206 4-F-Ph 2-MeNH-4-Pyr 1-Me -2-Phet-4- (3,4-deH-Pip) 2-3207 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Phet-4- (3,4-deH-Pip) 2-3208 4-F-Ph 2-MeNH-4-Pyr 1- Pr-2-Phet-4- (3,4-deH-Pip) 2-3209 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Phet-4- (3,4-deH-Pip ) 2-3210 4-F-Ph 2-MeNH-4-Pyr 1,2-diPhet-4- (3,4-deH-Pip) 2-3211 4-F-Ph 2-MeNH-4-Pyr 2- Me-4- (4,5-deH-Pip) 2-3212 4-F-Ph 2-MeNH-4-Pyr 1,2-diMe-4- (4,5-deH-Pip) 2-3213 4- F-Ph 2-MeNH-4-Pyr 1-Et-2-Me-4- (4,5-deH-Pip) 2-3214 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2- Me-4- (4,5-deH-Pip) 2-3215 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Me-4- (4,5-deH-Pip) 2-3216 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Me-4- (4,5-deH-Pip) 2-3217 4-F-Ph 2-MeNH-4-Pyr 2-Et- 4- (4,5-deH-Pip) 2-3218 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Et-4- (4,5-deH-Pip) 2-3219 4- F-Ph 2-MeNH-4-Pyr 1,2-diEt-4- (4,5-deH-Pip) 2-3220 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2-Et- 4- (4,5-deH-Pip) 2-3221 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Et-4- (4,5-deH-Pip) 2-3222 4- F-Ph 2-MeNH-4-Pyr 1-Phet-2-Et-4- (4,5-deH-Pip) 2-3223 4-F-Ph 2-MeNH-4-Pyr 2-Pr-4- (4,5-deH-Pip) 2-3224 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Pr-4- (4,5-deH-Pip) 2-3225 4-F- Ph 2-MeNH-4-Pyr 1-Et-2-Pr-4- (4,5-deH-Pip) 2-3226 4-F-Ph 2-MeNH-4-Pyr 1,2-diPr-4- (4,5-deH-Pip) 2-3227 4-F-Ph 2-MeNH-4-Pyr 1-Bu -2-Pr-4- (4,5-deH-Pip) 2-3228 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Pr-4- (4,5-deH-Pip) 2-3229 4-F-Ph 2-MeNH-4-Pyr 2-Bu-4- (4,5-deH-Pip) 2-3230 4-F-Ph 2-MeNH-4-Pyr 1-Me-2 -Bu-4- (4,5-deH-Pip) 2-3231 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Bu-4- (4,5-deH-Pip) 2- 3232 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2-Bu-4- (4,5-deH-Pip) 2-3233 4-F-Ph 2-MeNH-4-Pyr 1,2 -diBu-4- (4,5-deH-Pip) 2-3234 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Bu-4- (4,5-deH-Pip) 2- 3235 4-F-Ph 2-MeNH-4-Pyr 2-Allyl-4- (4,5-deH-Pip) 2-3236 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Allyl -4- (4,5-deH-Pip) 2-3237 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Allyl-4- (4,5-deH-Pip) 2-3238 4 -F-Ph 2-MeNH-4-Pyr 1-Pr-2-Allyl-4- (4,5-deH-Pip) 2-3239 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2 -Allyl-4- (4,5-deH-Pip) 2-3240 4-F-Ph 2-MeNH-4-Pyr 1-Phet-2-Allyl-4- (4,5-deH-Pip) 2- 3241 4-F-Ph 2-MeNH-4-Pyr 2-Bn-4- (4,5-deH-Pip) 2-3242 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Bn -4- (4,5-deH-Pip) 2-3243 4-F-Ph 2-MeNH-4-Pyr 1-Et-2-Bn-4- (4,5-deH-Pip) 2-3244 4 -F-Ph 2-MeNH-4-Pyr 1-Pr-2-Bn-4- (4,5-deH-Pip) 2-3245 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2 -Bn-4- (4,5-deH-Pip) 2-3246 4-F-Ph 2- MeNH-4-Pyr 1-Phet-2-Bn-4- (4,5-deH-Pip) 2-3247 4-F-Ph 2-MeNH-4-Pyr 2-Phet-4- (4,5- deH-Pip) 2-3248 4-F-Ph 2-MeNH-4-Pyr 1-Me-2-Phet-4- (4,5-deH-Pip) 2-3249 4-F-Ph 2-MeNH- 4-Pyr 1-Et-2-Phet-4- (4,5-deH-Pip) 2-3250 4-F-Ph 2-MeNH-4-Pyr 1-Pr-2-Phet-4- (4, 5-deH-Pip) 2-3251 4-F-Ph 2-MeNH-4-Pyr 1-Bu-2-Phet-4- (4,5-deH-Pip) 2-3252 4-F-Ph 2- MeNH-4-Pyr 1,2-diPhet-4- (4,5-deH-Pip) 2-3253 Ph 4-Pyr 7- (1,2,3,5,6,8a-hexaH-Ind) 2- 3254 Ph 4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 2-3255 3-F-Ph 4-Pyr 7- (1,2,3,5,6,8a- hexaH-Ind) 2-3256 3-F-Ph 4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 2-3257 3-Cl-Ph 4-Pyr 7- (1, 2,3,5,6,8a-hexaH-Ind) 2-3258 3-Cl-Ph 4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 2-3259 3,4 -diF-Ph 4-Pyr 7- (1,2,3,5,6,8a-hexaH-Ind) 2-3260 3,4-diF-Ph 4-Pyr 7- (1,2,3,5, 8,8a-hexaH-Ind) 2-3261 3-CF _Three -Ph 4-Pyr 7- (1,2,3,5,6,8a-hexaH-Ind) 2-3262 3-CF _Three -Ph 4-Pyr 7- (1,2,3,5,8,8a-hexaH-Ind) 2-3263 4-F-Ph 4-Pyr 2-Pyrd-CH = CH- 2-3264 4-F- Ph 4-Pyr 1-Me-2-Pyrd-CH = CH- 2-3265 4-F-Ph 4-Pyr 1-Et-2-Pyrd-CH = CH- 2-3266 4-F-Ph 4-Pyr 1-Pr-2-Pyrd-CH = CH- 2-3267 4-F-Ph 4-Pyr 2-Pip-CH = CH- 2-3268 4-F-Ph 4-Pyr 1-Me-2-Pip- CH = CH- 2-3269 4-F-Ph 4-Pyr 1-Et-2-Pip-CH = CH- 2-3270 4-F-Ph 4-Pyr 1-Pr-2-Pip-CH = CH- 2-3271 Ph 4-Pyr 2-Pyrd-CH = CH- 2-3272 Ph 4-Pyr 1-Me-2-Pyrd-CH = CH- 2-3273 Ph 4-Pyr 1-Et-2-Pyrd-CH = CH- 2-3274 Ph 4-Pyr 1-Pr-2-Pyrd-CH = CH- 2-3275 Ph 4-Pyr 2-Pip-CH = CH- 2-3276 Ph 4-Pyr 1-Me-2- Pip-CH = CH- 2-3277 Ph 4-Pyr 1-Et-2-Pip-CH = CH- 2-3278 Ph 4-Pyr 1-Pr-2-Pip-CH = CH- 2-3279 3-F -Ph 4-Pyr 2-Pyrd-CH = CH- 2-3280 3-F-Ph 4-Pyr 1-Me-2-Pyrd-CH = CH- 2-3281 3-F-Ph 4-Pyr 1-Et -2-Pyrd-CH = CH- 2-3282 3-F-Ph 4-Pyr 1-Pr-2-Pyrd-CH = CH- 2-3283 3-F-Ph 4-Pyr 2-Pip-CH = CH -2-3284 3-F-Ph 4-Pyr 1-Me-2-Pip-CH = CH- 2-3285 3-F-Ph 4-Pyr 1-Et-2-Pip-CH = CH- 2-3286 3-F-Ph 4-Pyr 1-Pr-2-Pip-CH = CH- 2-3287 3-Cl-Ph 4-Pyr 2-Pyrd-CH = CH- 2-3288 3-Cl-Ph 4-Pyr 1-Me-2-Pyrd-CH = CH- 2-3289 3-Cl-Ph 4-Pyr 1-Et- 2-Pyrd-CH = CH- 2-3290 3-Cl-Ph 4-Pyr 1-Pr-2-Pyrd-CH = CH- 2-3291 3-Cl-Ph 4-Pyr 2-Pip-CH = CH- 2-3292 3-Cl-Ph 4-Pyr 1-Me-2-Pip-CH = CH- 2-3293 3-Cl-Ph 4-Pyr 1-Et-2-Pip-CH = CH- 2-3294 3 -Cl-Ph 4-Pyr 1-Pr-2-Pip-CH = CH- 2-3295 3,4-diF-Ph 4-Pyr 2-Pyrd-CH = CH- 2-3296 3,4-diF-Ph 4-Pyr 1-Me-2-Pyrd-CH = CH- 2-3297 3,4-diF-Ph 4-Pyr 1-Et-2-Pyrd-CH = CH- 2-3298 3,4-diF-Ph 4-Pyr 1-Pr-2-Pyrd-CH = CH- 2-3299 3,4-diF-Ph 4-Pyr 2-Pip-CH = CH- 2-3300 3,4-diF-Ph 4-Pyr 1 -Me-2-Pip-CH = CH- 2-3301 3,4-diF-Ph 4-Pyr 1-Et-2-Pip-CH = CH- 2-3302 3,4-diF-Ph 4-Pyr 1 -Pr-2-Pip-CH = CH- 2-3303 3-CF _Three -Ph 4-Pyr 2-Pyrd-CH = CH- 2-3304 3-CF _Three -Ph 4-Pyr 1-Me-2-Pyrd-CH = CH- 2-3305 3-CF _Three -Ph 4-Pyr 1-Et-2-Pyrd-CH = CH- 2-3306 3-CF _Three -Ph 4-Pyr 1-Pr-2-Pyrd-CH = CH- 2-3307 3-CF _Three -Ph 4-Pyr 2-Pip-CH = CH- 2-3308 3-CF _Three -Ph 4-Pyr 1-Me-2-Pip-CH = CH- 2-3309 3-CF _Three -Ph 4-Pyr 1-Et-2-Pip-CH = CH- 2-3310 3-CF _Three -Ph 4-Pyr 1-Pr-2-Pip-CH = CH- ----------------------------------- −−

[0087]

[Table 4] In the above table, "ABN" is 9-azabicyclo [3.3.1].
Represents nonanyl, and "deH-ABN" is dehydro [9-azabi
Cyclo [3.3.1] nonanyl] (i.e., 9-Azabi
Black [3.3.1] nonenyl), and “ABO” is 8-
Azabicyclo [3.2.1] octanyl, and “deH-
“ABO” is dehydro [8-azabicyclo [3.2.1]
Tanil] (ie, 8-azabicyclo [3.2.1]
Octenyl), “Ac” indicates acetyl, and “Ally”
`` l '' represents allyl, `` Azt '' represents azetidinyl,
“Bn” indicates benzyl, “Bu” indicates butyl, and “tB
"u" indicates t-butyl, "Bz" indicates benzoyl,
“Et” indicates ethyl, “Hp” indicates heptyl, and “Hp
“ip” indicates homopiperidinyl, “Hx” indicates hexyl
Where "cHx" indicates cyclohexyl and "Ind" indicates India
Indicates lysinyl, `` Me '' indicates methyl, and `` Mor ''
Represents rufolinyl, “Nn” represents nonyl, and “Oc” represents
Indicates octyl, “Ph” indicates phenyl, and “Phet” indicates phenyl.
Propargyl indicates propargyl
"Pip" indicates piperidyl, and "deH-Pip" indicates
Lopiperidyl (ie, tetrahydropyridyl),
“Piz” indicates piperazinyl, “Pn” indicates pentyl
`` CPn '' indicates cyclopentyl, and `` Pr ''
`` IPr '' indicates isopropyl, and `` cPr '' indicates isopropyl.
Represents propyl, "Pym" represents pyrimidinyl,
"Pyr" represents pyridyl, "Pyrd" represents pyrrolidinyl
`` Qui '' indicates quinolizinyl, and `` Qun '' indicates quinuclidinyl
Indicates lysinyl, "deH-Qun" is dehydroquinuclidini
(I.e., quinuclidienyl) and "Tmor"
Shows morpholinyl. In Tables 1 and 2 above,
Examples of the compound include exemplified compound numbers 1-1 to 1-3.
2, 1-35, 1-38, 1-40, 1-42, 1-4
3, 1-45 to 1-52, 1-65 to 1-67, 1
-71 to 1-76, 1-88 to 1-90, 1-94
To 1-126, 1-129, 1-132, 1-134
To 1-137, 1-139 to 1-146, 1-15
9 to 1-161, 1-165 to 1-170, 1-1
82 to 1-184, 1-188 to 1-219, 1-
222, 1-225, 1-227, 1-229, 1-2
30, 1-232 to 1-239, 1-252 to 1-
254, 1-258 to 1-263, 1-275 to 1
-277, 1-281 to 1-312, 1-315, 1
-318, 1-320, 1-322, 1-323, 1-
325 to 1-332, 1-345 to 1-347, 1
-351 to 1-356, 1-368 to 1-370,
1-374 to 1-405, 1-408, 1-411,
1-413, 1-415, 1-416, 1-418 ~
1-425, 1-438 to 1-440, 1-444
To 1-449, 1-461 to 1-463, 1-467
To 1-498, 1-501, 1-504, 1-50
6, 1-508, 1-509, 1-511 to 1-51
8, 1-531 to 1-533, 1-537 to 1-5
42, 1-554 to 1-556, 1-560 to 1-
591, 1-594, 1-597, 1-599, 1-6
01, 1-602, 1-604 to 1-611, 1-6
24 to 1-626, 1-630 to 1-635, 1-
647 to 1-649, 1-653 to 1-684, 1
-687, 1-690, 1-692, 1-694, 1-
695, 1-697 to 1-704, 1-717 to 1
-719, 1-723 to 1-728, 1-740 to
1-742, 1-746 to 1-777, 1-780,
1-783, 1-785, 1-787, 1-788, 1
-790 to 1-797, 1-810 to 1-812,
1-816 to 1-821, 1-833 to 1-83
5, 1-839 to 1-870, 1-873, 1-87
6, 1-878, 1-880, 1-881, 1-883
1-890, 1-903 to 1-905, 1-90
9 to 1-914, 1-926 to 1-928, 1-9
32 to 1-963, 1-966, 1-969, 1-9
71, 1-973, 1-974, 1-976 to 1-9
83, 1-996 to 1-998, 1-1002 to 1
-1007, 1-1010 to 1-1021, 1-10
25 to 1-1056, 1-11059, 1-1062,
1-1064, 1-1066, 1-1067, 1-10
69 to 1-1076, 1-189 to 1-109
1, 1-1095 to 1-1100, 1-112 to
1-1114, 1-1118 to 1-1149, 1-1
152, 1-1155, 1-1157, 1-1159,
1-1160, 1-1162 to 1-1169, 1-1
182 to 1-1184, 1-1188 to 1-119
3, 1-1205 through 1-1207, 1-211 through
1-1242, 1-1245, 1-1248, 1-12
50, 1-125, 1-1253, 1-1255 to
1-1262, 1-1275 to 1-1277, 1-1
281 to 1-1286, 1-1298 to 1-130
0, 1-1304 to 1-1335, 1-1338, 1
-1341, 1-1343, 1-1345, 1-134
6, 1-1348 through 1-1355, 1-1368 through
1-1370, 1-1374 to 1-1379, 1-1
391 to 1-1393, 1-139 to 1-140
5, 1-1407 to 1-1415, 1-1418, 1
-1419, 1-1422 to 1-1425, 1-14
27, 1-1428, 1-1432 to 1-1440,
1-1442 to 1-1450, 1-1453, 1-1
454, 1-1457 to 1-1460, 1-146
2, 1-1463, 1-1467 to 1-1475, 1
-1477 to 1-1485, 1-1488, 1-14
89, 1-1492 to 1-1495, 1-1497,
1-1498, 1-1502 to 1-1510, 1-1
512 to 1-1520, 1-1523, 1-152
4, 1-1527 to 1-1530, 1-1532, 1
-1533, 1-1537 to 1-1545, 1-15
47 to 1-1555, 1-1558, 1-1559,
1-1562 to 1-1565, 1-1567, 1-1
568, 1-1572 to 1-1580, 1-1582
To 1-1590, 1-1593, 1-194, 1-1
597 to 1-1600, 1-1602, 1-160
3, 1-1607 through 1-1615, 1-1617 through
1-1625, 1-1628, 1-1629, 1-16
32 to 1-1635, 1-1637, 1-1636,
1-1644 to 1-1650, 1-1655 to 1-
1660, 1-1663, 1-1664, 1-1667
1 to 1670, 1-1672, 1-167, 1-
1677 to 1-1685, 1-1687 to 1-16
95, 1-1698, 1-1699, 1-1702 through
1-1705, 1-1707, 1-1708, 1-17
12 to 1-1720, 1-1722 to 1-173
0, 1-1733, 1-1732, 1-1737 to 1
-1740, 1-1742, 1-1743, 1-174
7 to 1-1755, 1-1775 to 1-1765,
1-1768, 1-1776, 1-1772 to 1-1
775, 1-1777, 1-1778, 1-1780
1-1-1790, 1-1792 to 1-1800, 1-
1803, 1-1804, 1-1807 to 1-181
0, 1-1818, 1-1818, 1-1817 to 1
-1825, 1-1828 to 1-1835, 1-18
38, 1-1839, 1-1842 to 1-1845,
1-1847, 1-1848, 1-1852 to 1-1
860, 1-1862 to 1-1870, 1-187
3, 1-1874, 1-1877 to 1-1880, 1
-1882, 1-1883, 1-1888 to 1-18
95, 1-1899 to 1-1905, 1-1908,
1-1909, 1-1912 to 1-1915, 1-1
917, 1-1918, 1-1922 to 1-193
0, 1-1932 to 1-1940, 1-1943, 1
-1944, 1-1947 to 1-1950, 1-19
52, 1-1953, 1-1957 to 1-1965,
1-1967 to 1-1975, 1-1978, 1-1
979, 1-182 to 1-185, 1-198
7, 1-188, 1-1992 through 1-2000, 1
-2002 to 1-2010, 1-2013, 1-20
14, 1-22017 to 1-220, 1-2202,
1-2022, 1-22027 to 1-235, 1-2
037 to 1-204, 1-2048, 1-204
9, 1-2052 through 1-255, 1-2205, 1
-2058, 1-2206 to 1-2070, 1-20
72 to 1-2080, 1-2083, 1-2084,
1-2087 to 1-2090, 1-2092, 1-2
093, 1-2209 to 1-2105, 1-2107
To 1-2115, 1-2118, 1-2119, 1-
2122 to 1-2125, 1-2127, 1-212
8, 1-2132 through 1-2140, 1-2142 through
1-2150, 1-2153, 1-2154, 1-21
57 to 1-2160, 1-2162, 1-2163,
1-2167 to 1-2175, 1-2177 to 1-
2185, 1-2188, 1-2189, 1-2192
To 1-2195, 1-2197, 1-2198, 1-
2202 to 1-2210, 1-2212 to 1-22
20, 1-2223, 1-2224, 1-2227 through
1-2230, 1-2232, 1-2233, 1-22
37 to 1-2245, 1-2247 to 1-225
5, 1-2258, 1-2259, 1-2262 to 1
-2265, 1-2267, 1-2268, 1-227
2 to 1-2280, 1-2282 to 1-2290,
1-2293, 1-2294, 1-2297 through 1-2
300, 1-2302, 1-2303, 1-2307
To 1-2315, 1-2317 to 1-2325, 1-
2328, 1-2329, 1-2332 to 1-233
5, 1-2337, 1-2338, 1-2342 through 1
-2350, 1-2352 to 1-2360, 1-23
63, 1-2364, 1-2367 through 1-2370,
1-2372, 1-2373, 1-2377 through 1-2
385, 1-2387 through 1-2395, 1-239
8, 1-2399, 1-2402 through 1-2405, 1
-2407, 1-2408, 1-2412 to 1-24
20, 1-2422 to 1-2430, 1-2433,
1-2434, 1-237 to 1-2440, 1-2
442, 1-2443, 1-247 to 1-245
5, 1-2457 to 1-2465, 1-2468, 1
-2469, 1-2472 to 1-2475, 1-24
77, 1-2478, 1-2482 to 1-2490,
1-2492 to 1-2500, 1-2503, 1-2
504, 1-2507 to 1-2510, 1-251
2, 1-2513, 1-2517 through 1-2529, 1
-2539 to 1-2594, 1-2623 to 1-3
322, 2-1 to 2-32, 2-35, 2-38, 2
-40, 2-42, 2-43, 2-45 to 2-52,
2-65 to 2-67, 2-71 to 2-76, 2-8
8 to 2-90, 2-94 to 2-126, 2-12
9, 2-132, 2-134 to 2-137, 2-13
9 to 2-146, 2-159 to 2-161, 2-1
65 to 2-170, 2-182 to 2-184, 2-
188 to 2-219, 2-222, 2-225, 2-
227, 2-229, 2-230, 2-232 to 2-
239, 2-252 to 2-254, 2-258 to 2
-263, 2-275 to 2-277, 2-281 to
2-312, 2-315, 2-318, 2-320, 2
-322, 2-323, 2-325 to 2-332, 2
-345 to 2-347, 2-351 to 2-356,
2-368 to 2-370, 2-374 to 2-40
5, 2-408, 2-411, 2-413, 2-41
5, 2-416, 2-418 to 2-425, 2-43
8 to 2-440, 2-444 to 2-449, 2-4
61 to 2-463, 2-467 to 2-498, 2-
501, 2-504, 2-506, 2-508, 2-5
09, 2-511 to 2-518, 2-531 to 2-
533, 2-537 to 2-542, 2-554 to 2
-556, 2-560 to 2-591, 2-594, 2
-597, 2-599, 2-601, 2-602, 2-
604 to 2-611, 2-624 to 2-626, 2
-630 to 2-635, 2-647 to 2-649,
2-653 to 2-684, 2-687, 2-690,
2-692, 2-694, 2-695, 2-697 or later
2-704, 2-717 to 2-719, 2-723
2-728, 2-740 to 2-742, 2-746
To 2-777, 2-780, 2-783, 2-78
5, 2-787, 2-788, 2-790 to 2-79
7, 2-810 to 2-812, 2-816 to 2-8
21, 2-833 to 2-835, 2-839 to 2-
870, 2-873, 2-876, 2-878, 2-8
80, 2-881, 2-883 to 2-890, 2-9
03 to 2-905, 2-909 to 2-914, 2-
926 to 2-928, 2-932 to 2-963, 2
-966, 2-969, 2-971, 2-973, 2-
974, 2-976 to 2-983, 2-996 to 2
−998, 2-1002 to 2-1007, 2-101
9 to 2-1021, 2-1025 to 2-1056,
2-1059, 2-1062, 2-1064, 2-10
66, 2-1067, 2-1069 to 2-1076,
2-1089 to 2-1091, 2-1095 to 2-
1100, 2-1112 to 2-1114, 2-111
8 to 2-1149, 2-1152, 2-1155, 2
-1157, 2-1159, 2-1160, 2-116
2 to 2-1169, 2-1182 to 2-1184,
2-1188 to 2-1193, 2-1205 to 2-
1207, 2-1211 to 2-1242, 2-124
5, 2-1248, 2-1250, 2-1252, 2-
1253, 2-1255 to 2-1262, 2-127
5 to 2-1277, 2-1281 to 2-1286,
2-1298 to 2-1300, 2-1304 to 2-
1335, 2-1338, 2-1341, 2-134
3, 2-1345, 2-1346, 2-1348 or 2
-1355, 2-1368 to 2-1370, 2-13
74 to 2-1379, 2-1391 to 2-139
3, 2-1397 to 2-1405, 2-1407 to
2-1415, 2-1418, 2-1419, 2-14
22 to 2-1425, 2-1427, 2-1428,
2-1432 to 2-1440, 2-1442 to 2-
1450, 2-1453, 2-1454, 2-1457
2-1460, 2-1462, 2-1463, 2-
1467 to 2-1475, 2-1377 to 2-14
85, 2-1488, 2-1489, 2-1492 or later
2-1495, 2-1497, 2-1498, 2-15
02 to 2-1510, 2-1512 to 2-152
0, 2-1523, 2-1524, 2-1527 or 2
-1530, 2-1532, 2-1533, 2-153
7 to 2-1545, 2-1547 to 2-1555,
2-1558, 2-1559, 2-1562 to 2-1
565, 2-1567, 2-1568, 2-1572
2-1580, 2-1582 to 2-1590, 2-
1593, 2-194, 2-1597 to 2-160
0, 2-1602, 2-1603, 2-1607 to 2
-1615, 2-1617 to 2-1625, 2-16
28, 2-1629, 2-1632 to 2-1635,
2-1637, 2-1638, 2-1642 to 2-1
650, 2-1652 to 2-1660, 2-166
3, 2-1664, 2-1667 to 2-1670, 2,
-1672, 2-1673, 2-1677 to 2-16
85, 2-1687 to 2-1695, 2-1698,
2-1699, 2-1702 to 2-1705, 2-1
707, 2-1708, 2-1712 to 2-172
0, 2-1722 to 2-1730, 2-1733, 2
-1734, 2-1737 to 2-1740, 2-17
42, 2-1743, 2-1747 to 2-1755,
2-1775 to 2-1765, 2-1768, 2-1
769, 2-1772 to 2-1775, 2-177
7, 2-1778, 2-1780 to 2-1790, 2,
-1792 to 2-1800, 2-1803, 2-18
04, 2-1807 to 2-1810, 2-1812,
2-1813, 2-1817 to 2-1825, 2-1
827 to 2-1835, 2-1838, 2-183
9, 2-1842 to 2-1845, 2-1847, 2
-1848, 2-1852 to 2-1860, 2-18
62 to 2-1870, 2-1873, 2-1874,
2-1877 to 2-1880, 2-1882, 2-1
883, 2-1887 to 2-1895, 2-1897
2-1905, 2-1908, 2-1909, 2-
1912 to 2-1915, 2-1917, 2-191
8, 2-1922 to 2-1930, 2-1936 to
2-1940, 2-1943, 2-1944, 2-19
47 to 2-1950, 2-1952, 2-1953,
2-1957 to 2-1965, 2-1957 to 2-
1975, 2-1978, 2-1979, 2-1982
To 2-1985, 2-1987, 2-1988, 2-
1992 to 2-2000, 2-2002 to 2-20
10, 2-2013, 2-2014, 2-2017 to
2-2020, 2-2022, 2-2023, 2-20
27 to 2-2035, 2-2037 to 2-204
5, 2-2048, 2-2049, 2-2052 or 2
-2055, 2-2057, 2-2058, 2-206
2 to 2-2070, 2 to 2072 to 2-2080,
2-2083, 2-2084, 2-2087 to 2-2
090, 2-2092, 2-2093, 2-2097
2-2105, 2-2107 to 2-2115, 2-
2118, 2-2119, 2-2122 to 2-212
5, 2-2127, 2-2128, 2-2132 and 2
-2140, 2-2142 to 2-2150, 2-21
53, 2-2154, 2-2157 to 2-2160,
2-2162, 2-2163, 2-2167 to 2-2
175, 2-2177 to 2-2185, 2-218
8, 2-2189, 2-2192 to 2-2195, 2
-2197, 2-2198, 2-2202 to 2-22
10, 2-2212 to 2-2220, 2-2223,
2-2224, 2-2227 to 2-2230, 2-2
232, 2-2233, 2-2237 to 2-224
5, 2-2247 to 2-2255, 2-2258, 2
-2259, 2-2262 to 2-2265, 2-22
67, 2-2268, 2-2272 to 2-2280,
2-2282 to 2-2290, 2-2293, 2-2
294, 2-2297 to 2-2300, 2-230
2, 2-2303, 2-2307 to 2-2315, 2
-2317 to 2-2325, 2-2328, 2-23
29, 2-2332 to 2-2335, 2-2337,
2-2338, 2-2342 to 2-2350, 2-2
352 to 2-2360, 2-2363, 2-236
4, 2-2367 to 2-2370, 2-2372, 2
-2373, 2-2377 to 2-2385, 2-23
87 to 2-2395, 2-2398, 2-2399,
2-2402 to 2-2405, 2-2407, 2-2
408, 2-2412 to 2-2420, 2-2422
2-2430, 2-2433, 2-2434, 2-
2437 to 2-2440, 2-2442, 2-244
3, 2-2247 to 2-2455, 2-2457 to
2-2465, 2-2468, 2-2469, 2-24
72 to 2-2475, 2-2577, 2-2478,
2-2482 to 2-2490, 2-2492 to 2-
2500, 2-2503, 2-2504, 2-2507
2-2510, 2-2512, 2-2513, 2-
2517 to 2-2529, 2-2539 to 2-25
94, and compounds of 1-2623 to 1-3322
And more preferred compounds are exemplified.
Compound numbers 1-2 to 1-4, 1-6 to 1-8, 1-
11, 1-14 to 1-16, 1-18 to 1-20,
1-22 to 1-24, 1-26 to 1-28, 1-3
0 to 1-32, 1-35, 1-42, 1-43, 1-
45 to 1-52, 1-65, 1-66, 1-71 to
1-75, 1-89, 1-94, 1-96 to 1-9
8, 1-100 to 1-102, 1-105, 1-10
8 to 1-110, 1-112 to 1-114, 1-1
16 to 1-118, 1-120 to 1-122, 1-
124 to 1-126, 1-129, 1-136, 1-
137, 1-139 to 1-146, 1-159, 1-
160, 1-165 to 1-169, 1-183, 1-
189 to 1-191, 1-193 to 1-195, 1
-198, 1-201 to 1-203, 1-205 to
1-207, 1-209 to 1-211, 1-213
To 1-215, 1-217 to 1-219, 1-22
2, 1-229, 1-230, 1-232 to 1-23
9, 1-252, 1-253, 1-258 to 1-26
2, 1-276, 1-282 to 1-284, 1-28
6 to 1-288, 1-291, 1-294 to 1-2
96, 1-298 to 1-300, 1-302 to 1-
304, 1-306 to 1-308, 1-310 to 1
-312, 1-315, 1-322, 1-323, 1-
325 to 1-332, 1-345, 1-346, 1-
351 to 1-355, 1-369, 1-375 to 1
-377, 1-379 to 1-381, 1-384, 1
-387 to 1-389, 1-391 to 1-393,
1-395 to 1-397, 1-399 to 1-40
1, 1-403 to 1-405, 1-408, 1-41
5, 1-416, 1-418 to 1-425, 1-43
8, 1-439, 1-444 to 1-448, 1-46
2, 1-468 to 1-470, 1-472 to 1-4
74, 1-477, 1-480 to 1-482, 1-4
84 to 1-486, 1-488 to 1-490, 1-
492 to 1-494, 1-496 to 1-498, 1
-501, 1-508, 1-509, 1-511 to 1
-518, 1-531, 1-532, 1-537 to 1
-541, 1-555, 1-561 to 1-563, 1
-565 to 1-567, 1-570, 1-573 to
1-575, 1-577 to 1-579, 1-581
1-583, 1-585 to 1-587, 1-589
1-591, 1-594, 1-601, 1-60
2, 1-604 to 1-611, 1-624, 1-62
5, 1-630 to 1-634, 1-648, 1-65
4 to 1-656, 1-658 to 1-660, 1-6
63, 1-666 to 1-668, 1-670 to 1-
672, 1-674 to 1-676, 1-678 to 1
-680, 1-682 to 1-684, 1-687, 1
-694, 1-695, 1-697 to 1-704, 1
-717, 1-718, 1-723 to 1-727, 1
-741, 1-747 through 1-749, 1-751 through
1-753, 1-756, 1-759 to 1-761,
1-763 to 1-765, 1-767 to 1-76
9, 1-771 to 1-773, 1-775 to 1-7
77, 1-780, 1-787, 1-788, 1-79
0 to 1-797, 1-810, 1-811, 1-81
6 to 1-820, 1-834, 1-840 to 1-8
42, 1-844 to 1-846, 1-849, 1-8
52 to 1-854, 1-856 to 1-858, 1-
860 to 1-862, 1-864 to 1-866, 1
-868 to 1-870, 1-873, 1-880, 1
-881, 1-883 to 1-890, 1-903, 1
-904, 1-909 to 1-913, 1-927, 1
-933 to 1-935, 1-937 to 1-939,
1-942, 1-945 to 1-947, 1-949
1-951, 1-953 to 1-955, 1-957
To 1-959, 1-961 to 1-963, 1-96
6, 1-973, 1-974, 1-976 to 1-98
3, 1-996, 1-997, 1-1002 to 1-1
006, 1-1020, 1-102 to 1-102
8, 1-1030 to 1-1032, 1-1035, 1
-1038 to 1-1040, 1-1042 to 1-1
044, 1-1046 to 1-1048, 1-1050
1 to 1052, 1-1054 to 1-1056, 1
-1059, 1-1066, 1-1067, 1-106
9 to 1-1076, 1-1089, 1-1090, 1
-1095 to 1-1099, 1-1113, 1-11
19 to 1-1121, 1-1123 to 1-112
5, 1-1128, 1-1131 to 1-1133, 1
-1135 to 1-1137, 1-1139 to 1-1
141, 1-1143 to 1-1145, 1-1147
To 1-1149, 1-1152, 1-1159, 1-
1160, 1-1162 to 1-1169, 1-118
2, 1-1183, 1-1188 to 1-1192, 1
-1206, 1-1212 to 1-1214, 1-12
16 to 1-1218, 1-1221, 1-1224no
1-12-126, 1-1228 to 1-1230, 1-
1232 to 1-1234, 1-1236 to 1-12
38, 1-1240 to 1-1242, 1-1245,
1-1252, 1-1253, 1-1255 to 1-1
262, 1-1275, 1-1276, 1-128
To 1-1285, 1-1299, 1-1305 to 1-
1307, 1-1309 to 1-1131, 1-131
4, 1-1317 through 1-1319, 1-1321 through
1-1323, 1-1325 to 1-1327, 1-1
329 to 1-133, 1-1333 to 1-133
5, 1-1338, 1-1345, 1-1346, 1-
1348 to 1-1355, 1-1368, 1-136
9, 1-1374 to 1-1378, 1-1392, 1
-1397 to 1-1405, 1-1408 to 1-1
415, 1-1418, 1-1419, 1-1422
1-14-124, 1-1428, 1-1432 to 1-
1440, 1-1443 to 1-1450, 1-145
3, 1-1454, 1-1457 to 1-1459, 1
-1463, 1-1467 to 1-1475, 1-14
78 to 1-1485, 1-1488, 1-1489,
1-1492 to 1-1494, 1-1498, 1-1
502 to 1-1510, 1-1513 to 1-152
0, 1-1523, 1-1524, 1-1527 to 1
-1529, 1-1533, 1-1-1537 to 1-15
45, 1-1548 to 1-1555, 1-1558,
1-1559, 1-1562 through 1-1564, 1-1
568, 1-1572 to 1-1580, 1-1583
To 1590, 1-1593, 1-1594, 1-
1597 to 1-1599, 1-1603, 1-160
7 to 1-1615, 1-1618 to 1-1625,
1-1628, 1-1629, 1-1632 to 1-1
634, 1-1638, 1-1642 to 1-165
0, 1-1653 to 1-1660, 1-1663, 1
-1664, 1-1667 to 1-1669, 1-16
73, 1-1677 to 1-1684, 1-1688
1-1695, 1-1698, 1-1699, 1-1
702 to 1-1704, 1-1708, 1-1712
To 1-1720, 1-1723 to 1-1730, 1
-1733, 1-1734, 1-1737 to 1-17
39, 1-1743, 1-1747 to 1-1755,
1-1758 to 1-1765, 1-1768, 1-1
769, 1-1772 to 1-1774, 1-177
8, 1-1780 to 1-1790, 1-1793 to
1-1800, 1-1803, 1-1804, 1-18
07 to 1-1809, 1-1818, 1-1817
1-11825, 1-1828 to 1-1835, 1-
1838, 1-1839, 1-1842 to 1-184
4, 1-1848, 1-1852 to 1-1860, 1
-1863 to 1-1870, 1-1873, 1-18
74, 1-1877 to 1-1879, 1-1883,
1-18887 to 1-1895, 1-1899 to 1-
1905, 1-1908, 1-1909, 1-1912
To 1-1914, 1-1918, 1-1922 to 1
-1930, 1-1933 to 1-1940, 1-19
43, 1-1944, 1-1947 to 1-1949,
1-1953, 1-1957 to 1-1965, 1-1
968 to 1-1975, 1-1978, 1-197
9, 1-182 to 1-184, 1-188, 1
-1992 to 1-2000, 1-203 to 1-2
010, 1-2013, 1-2014, 1-2017
1-2019, 1-2022, 1-22020 to 1-
2035, 1-22038 to 1-2040, 1-204
8, 1-2049, 1-2052 through 1-2054, 1
-2058, 1-2206 to 1-2070, 1-20
73 to 1-2080, 1-2083, 1-2084,
1-2087 to 1-289, 1-2093, 1-2
097 to 1-2105, 1-2108 to 1-211
5, 1-2118, 1-2119, 1-2122 through 1
-2124, 1-2128, 1-2132 to 1-21
40, 1-2143 to 1-2150, 1-2153,
1-2154, 1-2157 through 1-2159, 1-2
163, 1-2167 to 1-2175, 1-2178
To 1-2185, 1-2188, 1-2189, 1-
2192 to 1-2194, 1-2198, 1-220
2 to 1-2210, 1-2213 to 1-2220,
1-2223, 1-2224, 1-2227 to 1-2
229, 1-2233, 1-2237 to 1-224
5, 1-2248 to 1-2255, 1-2258, 1
-2259, 1-2262 to 1-2264, 1-22
68, 1-2272 to 1-2280, 1-2283
To 1-2290, 1-2293, 1-2294, 1-2
297 to 1-2299, 1-2303, 1-2307
To 1-2315, 1-2318 to 1-2325, 1
-2328, 1-2329, 1-2332 to 1-23
34, 1-2338, 1-2342 through 1-2350,
1-2353 to 1-2360, 1-2363, 1-2
364, 1-2367 through 1-2369, 1-237
3, 1-2377 through 1-2385, 1-2388 through
1-2395, 1-2398, 1-2399, 1-24
02 to 1-2404, 1-2408, 1-2241
To 1-2420, 1-2423 to 1-2430, 1-
2433, 1-2434, 1-237 to 1-243
9, 1-2443, 1-247 to 1-2455, 1
-2458 to 1-2465, 1-2468, 1-24
69, 1-2472 to 1-2474, 1-2478,
1-2482 to 1-2490, 1-2493 to 1-
2500, 1-2503, 1-2504, 1-2507
1-2509, 1-2513, 1-2517 through 1
-2526, 1-2528, 1-2529, 1-253
9 to 1-2554, 1-2556 to 1-2558,
1-2560 to 1-2577, 1-2579 to 1-
2581, 1-2584 to 1-2594, 1-262
6, 1-2629 to 1-2643, 1-2645, 1
-2648 to 1-2651, 1-2653 to 1-2
748, 1-2779, 1-2780, 1-22782,
1-2781, 1-2905, 1-2906, 1-29
08, 1-2909, 1-3031, 1-3032, 1
-3157, 1-3158, 1-3253 to 1-33
22, 2-2 to 2-4, 2-6 to 2-8, 2-1
1, 2-14 to 2-16, 2-18 to 2-20, 2
-22 to 2-24, 2-26 to 2-28, 2-30
To 2-32, 2-35, 2-42, 2-43, 2-4
5 to 2-52, 2-65, 2-66, 2-71 to 2
-75, 2-89, 2-94, 2-96 to 2-98,
2-100 to 2-102, 2-105, 2-108
2-110, 2-112 to 2-114, 2-116
To 2-118, 2-120 to 2-122, 2-12
4 to 2-126, 2-129, 2-136, 2-13
7, 2-139 to 2-146, 2-159, 2-16
0, 2-165 to 2-169, 2-183, 2-18
9 to 2-191, 2-193 to 2-195, 2-1
98, 2-201 to 2-203, 2-205 to 2-
207, 2-209 to 2-211, 2-213 to 2
-215, 2-217 to 2-219, 2-222, 2
-229, 2-230, 2-232 to 2-239, 2
-252, 2-253, 2-258 to 2-262, 2
-276, 2-282 to 2-284, 2-286 to
2-288, 2-291, 2-294 to 2-296,
2-298 to 2-300, 2-302 to 2-30
4, 2-306 to 2-308, 2-310 to 2-3
12, 2-315, 2-322, 2-323, 2-32
5 to 2-332, 2-345, 2-346, 2-35
1 to 2-355, 2-369, 2-375 to 2-3
77, 2-379 to 2-381, 2-384, 2-3
87 to 2-389, 2-391 to 2-393, 2-
395 to 2-397, 2-399 to 2-401, 2
-403 to 2-405, 2-408, 2-415, 2
-416, 2-418 to 2-425, 2-438, 2
-439, 2-444 to 2-448, 2-462, 2
-468 to 2-470, 2-472 to 2-474,
2-478, 2-480 to 2-482, 2-484
2-486, 2-488 to 2-490, 2-492
To 2-494, 2-496 to 2-498, 2-50
1, 2-508, 2-509, 2-511 to 2-51
8, 2-531, 2-532, 2-537 to 2-54
1, 2-555, 2-561 to 2-563, 2-56
5 to 2-567, 2-570, 2-573 to 2-5
75, 2-577 to 2-579, 2-581 to 2-
583, 2-585 to 2-587, 2-589 to 2
−591, 2-594, 2-601, 2-602, 2-
604 to 2-611, 2-624, 2-625, 2-
630 to 2-634, 2-648, 2-654 to 2
-656, 2-658 to 2-660, 2-663, 2
-666 to 2-668, 2-670 to 2-672,
2-674 to 2-676, 2-678 to 2-68
0, 2-682 to 2-684, 2-687, 2-69
4, 2-695, 2-697 to 2-704, 2-71
7, 2-718, 2-723 to 2-727, 2-74
1, 2-747 to 2-749, 2-751 to 2-7
53, 2-756, 2-759 to 2-761, 2-7
63 to 2-765, 2-767 to 2-769, 2-
771 to 2-773, 2-775 to 2-777, 2
-780, 2-787, 2-788, 2-790 to 2
-797, 2-810, 2-811, 2-816 or 2
-820, 2-834, 2-840 to 2-842,2
-844 to 2-846, 2-849, 2-852 to
2-854, 2-856 to 2-858, 2-860
2-862, 2-864 to 2-866, 2-868
To 2-870, 2-873, 2-880, 2-88
1, 2-883 to 2-890, 2-903, 2-90
4, 2-909 to 2-913, 2-927, 2-93
3 to 2-935, 2-937 to 2-939, 2-9
42, 2-945 to 2-947, 2-949 to 2-
951, 2-953 to 2-955, 2-957 to 2
-959, 2-961 to 2-963, 2-966, 2
-973, 2-974, 2-976 to 2-983, 2,
-996, 2-997, 2-1002 to 2-100
6, 2-1020, 2-1026 to 2-1028, 2
-1030 to 2-1032, 2-1035, 2-10
38 to 2-1040, 2 to 1042 to 2-104
4, 2-1046 to 2-1048, 2-1050 to
2-1052, 2-1054 to 2-1056, 2-1
059, 2-1066, 2-1067, 2-1069
2-1076, 2-1089, 2-1090, 2-1
095 to 2-1099, 2-1113, 2-1119
2-1121, 2-1123 to 2-1125, 2
-1128, 2-1131 to 2-1133, 2-11
35 to 2-1137, 2-1139 to 2-114
1, 2-1143 to 2-1145, 2-1147 to
2-1149, 2-1152, 2-1159, 2-11
60, 2-1162 to 2-1169, 2-1182,
2-1183, 2-1188 to 2-1192, 2-1
206, 2-1212 to 2-1214, 2-1216
2-1218, 2-1221, 2-1224 to 2
-1226, 2-1228 to 2-1230, 2-12
32 to 2-1234, 2-1236 to 2-123
8, 2-1240 to 2-1242, 2-1245, 2
-1252, 2-1253, 2-1255 to 2-12
62, 2-1275, 2-1276, 2-1281 to
2-1285, 2-1299, 2-1305 to 2-1
307, 2-1309 to 2-1131, 2-131
4, 2-1317 to 2-1319, 2-1321 to
2-1323, 2-1325 to 2-1327, 2-1
329 to 2-1331, 2-1333 to 2-133
5, 2-1338, 2-1345, 2-1346, 2-
1348 to 2-1355, 2-1368, 2-136
9, 2-1374 to 2-1378, 2-1392,
-1397 to 2-1405, 2-1408 to 2-1
415, 2-1418, 2-1419, 2-1422
2-1424, 2-1428, 2-1432 to 2-
1440, 2-1443 to 2-1450, 2-145
3, 2-1454, 2-1457 to 2-1449, 2,
-1463, 2-1467 to 2-1475, 2-14
78 to 2-1485, 2-1488, 2-1489,
2-1492 to 2-1494, 2-1498, 2-1
502 to 2-1510, 2-1513 to 2-152
0, 2-1523, 2-1524, 2-1527 or 2
-1529, 2-1533, 2-1537 to 2-15
45, 2-1548 to 2-1555, 2-1558,
2-1559, 2-1562 to 2-1564, 2-1
568, 2-1572 to 2-1580, 2-1584
2-1590, 2-1593, 2-1594, 2-
1597 to 2-1599, 2-1603, 2-160
7 to 2-1615, 2-1618 to 2-1625,
2-1628, 2-1629, 2-1632 to 2-1
634, 2-1638, 2-1642 to 2-165
0, 2-1653 to 2-1660, 2-1663, 2
-1664, 2-1667 to 2-1669, 2-16
73, 2-1677 to 2-1685, 2-1688
2-1695, 2-1698, 2-1699, 2-1
702 to 2-1704, 2-1708, 2-1712
To 2-1720, 2-1723 to 2-1730, 2
-1733, 2-1734, 2-1737 to 2-17
39, 2-1743, 2-1747 to 2-1755,
2-1758 to 2-1765, 2-1768, 2-1
769, 2-1772 to 2-1774, 2-177
8, 2-1782 to 2-1790, 2-1793 to
2-1800, 2-1803, 2-1804, 2-18
07 to 2-1809, 2-1813, 2-1817
2-1825, 2-1828 to 2-1835, 2-
1838, 2-1839, 2-1842 to 2-184
4, 2-1848, 2-1852 to 2-1860, 2
-1863 to 2-1870, 2-1873, 2-18
74, 2-1877 to 2-1879, 2-1883,
2-1887 to 2-1895, 2-1898 to 2-
1905, 2-1908, 2-1909, 2-1912
2-1914, 2-1918, 2-1922 to 2
-1930, 2-1933 to 2-1940, 2-19
43, 2-1944, 2-1947 to 2-1949,
2-1953, 2-1957 to 2-1965, 2-1
968 to 2-1975, 2-1978, 2-197
9, 2-1982 to 2-1984, 2-1988, 2
-1992 to 2-2000, 2-2003 to 2-2
010, 2-2013, 2-2014, 2-2017
2-2019, 2-2020, 2-2020 to 2-
2035, 2-2038 to 2-2045, 2-204
8, 2-2049, 2-2205 to 2-2954, 2
-2058, 2-2062 to 2-2070, 2-20
73 to 2-2080, 2-2083, 2-2084,
2-2087 to 2-2089, 2-2093, 2-2
097 to 2-2105, 2-2108 to 2-211
5, 2-2118, 2-2119, 2-2122 and 2
-2124, 2-2128, 2-2132 to 2-21
40, 2-2143 to 2-2150, 2-2153,
2-2154, 2-2157 to 2-2159, 2-2
163, 2-2167 to 2-2175, 2-2178
2-2185, 2-2188, 2-2189, 2-
2192 to 2-2194, 2-2198, 2-220
2 to 2-2210, 2-2213 to 2-2220,
2-2223, 2-2224, 2-2227 to 2-2
229, 2-2233, 2-2237 to 2-224
5, 2-2248 to 2-2255, 2-2258, 2
-2259, 2-2262 to 2-2264, 2-22
68, 2-2272 to 2-2280, 2-2283
2-2290, 2-2293, 2-2294, 2-2
297 to 2-2299, 2-2303, 2-2307
2-2315, 2-2318 to 2-2325, 2
-2328, 2-2329, 2-2332 to 2-23
34, 2-2338, 2-2342 to 2-2350,
2-2353 to 2-2360, 2-2363, 2-2
364, 2-2367 to 2-2369, 2-237
3, 2-2377 through 2-2385, 2-2388 through
2-2395, 2-2398, 2-2399, 2-24
02 to 2-2404, 2-2408, 2-2412
2-2420, 2-2423 to 2-2430, 2-
2433, 2-2434, 2-2437 to 2-243
9, 2-2443, 2-2247 to 2-2455,2
-2458 to 2-2465, 2-2468, 2-24
69, 2-2472 to 2-2474, 2-2478,
2-2482 to 2-2490, 2-2493 to 2-
2500, 2-2503, 2-2504, 2-2507
2-2509, 2-2513, 2-2517 to 2
-2522, 2-2524 to 2-2526, 2-25
28, 2-2529, 2-2538 to 2-2554,
2-2556 to 2-2558, 2-2560 to 2-
2577, 2-2579 to 2-2581, 2-258
3 to 2-259, and 2-3253 to 2-33
22 compounds, and more preferably,
Exemplified compound numbers 1-3, 1-7, 1-11, 1-15,
1-19, 1-23, 1-27, 1-31, 1-35,
1-42, 1-45, 1-47 to 1-51, 1-6
5, 1-71, 1-73, 1-89, 1-94, 1-9
7, 1-98, 1-101, 1-105, 1-109,
1-113, 1-117, 1-121, 1-125, 1
-129, 1-136, 1-139, 1-141 to 1
-146, 1-159, 1-165, 1-167, 1-
183, 1-190, 1-194, 1-198, 1-2
02, 1-206, 1-210, 1-214, 1-21
8, 1-222, 1-229, 1-232, 1-234
To 1-238, 1-252, 1-258, 1-26
0, 1-276, 1-283, 1-287, 1-29
1, 1-295, 1-299, 1-303, 1-30
7, 1-311, 1-315, 1-322, 1-32
5, 1-327 to 1-331, 1-345, 1-35
1, 1-353, 1-369, 1-376, 1-38
0, 1-384, 1-388, 1-392, 1-39
6, 1-400, 1-404, 1-408, 1-41
5, 1-418, 1-420 to 1-424, 1-43
8, 1-444, 1-446, 1-462, 1-46
9, 1-473, 1-477, 1-481, 1-48
5, 1-489, 1-493, 1-497, 1-50
1, 1-508, 1-511, 1-513 to 1-51
7, 1-531, 1-537, 1-539, 1-55
5, 1-562, 1-566, 1-570, 1-57
4, 1-578, 1-582, 1-586, 1-59
0, 1-594, 1-601, 1-604, 1-606
To 1-610, 1-624, 1-630, 1-63
2, 1-648, 1-655, 1-659, 1-66
3, 1-667, 1-671, 1-675, 1-67
9, 1-683, 1-687, 1-694, 1-69
7, 1-699 to 1-703, 1-717, 1-72
3, 1-725, 1-741, 1-748, 1-75
2, 1-756, 1-760, 1-764, 1-76
8, 1-772, 1-776, 1-780, 1-78
7, 1-790, 1-792 to 1-796, 1-81
0, 1-816, 1-818, 1-834, 1-84
1, 1-845, 1-849, 1-853, 1-85
7, 1-861, 1-865, 1-869, 1-87
3, 1-880, 1-883, 1-885 to 1-88
9, 1-903, 1-909, 1-911, 1-92
7, 1-934, 1-938, 1-942, 1-94
6, 1-950, 1-954, 1-958, 1-96
2, 1-966, 1-973, 1-976, 1-978
To 1-982, 1-996, 1-1002, 1-10
04, 1-1020, 1-1027, 1-1031, 1
-1035, 1-1039, 1-1043, 1-104
7, 1-1051, 1-1055, 1-11059, 1-
1066, 1-1069, 1-1071 to 1-107
5, 1-1089, 1-1095, 1-1097, 1-
1113, 1-1120, 1-1124, 1-112
8, 1-1132, 1-1136, 1-1140, 1-
1144, 1-1148, 1-1152, 1-115
9, 1-1162, 1-1164 to 1-1168, 1
-1182, 1-1188, 1-1190, 1-120
6, 1-1213, 1-1217, 1-1221, 1-
1225, 1-1229, 1-1233, 1-123
7, 1-1241, 1-1245, 1-1252, 1-
1255, 1-1257 to 1-1261, 1-127
5, 1-1281, 1-1283, 1-1299, 1-
1306, 1-1310, 1-1314, 1-131
8, 1-1322, 1-1326, 1-1330, 1-
1334, 1-1338, 1-1345, 1-134
8, 1-1350 to 1-1354, 1-1368, 1
-1374, 1-1376, 1-1392, 1-139
7 to 1-1405, 1-1408, 1-1410, 1
-1412 to 1-1415, 1-1418, 1-14
22, 1-1428, 1-1432 to 1-1440,
1-1443, 1-1445, 1-147 to 1-1
450, 1-1453, 1-1457, 1-1463,
1-1467 to 1-1475, 1-1478, 1-1
480, 1-1482 to 1-1485, 1-148
8, 1-1492, 1-1498, 1-1502 to 1
-1510, 1-1513, 1-1515, 1-151
7 to 1-1520, 1-1523, 1-1527, 1
-1533, 1-1537 to 1-1545, 1-15
48, 1-1550, 1-1552 to 1-1555,
1-1558, 1-1562, 1-1568, 1-15
72 to 1-1580, 1-1584, 1-1585,
1-1587 to 1-1590, 1-1593, 1-1
597, 1-1603, 1-1607 to 1-161
5, 1-1616, 1-1620, 1-1622 to 1
-1625, 1-1628, 1-1632, 1-163
8, 1-1642 to 1-1650, 1-11653, 1
-1655, 1-1657 to 1-1660, 1-16
63, 1-1667, 1-1673, 1-1677 through
1-1685, 1-1688, 1-1690, 1-16
92 to 1-1695, 1-1698, 1-1702,
1-1708, 1-1712 to 1-1720, 1-1
723, 1-1725, 1-1727 to 1-173
0, 1-1733, 1-1737, 1-1743, 1-
1747 to 1-1755, 1-1758, 1-176
0, 1-1762 to 1-1765, 1-1768, 1
-1772, 1-1778, 1-1780 to 1-17
90, 1-1793, 1-1795, 1-1797 to
1-1800, 1-1803, 1-1807, 1-18
13, 1-1817 to 1-1825, 1-1828,
1-1830, 1-1832 to 1-1835, 1-1
838, 1-1842, 1-1848, 1-1852
1-1860, 1-1863, 1-1865, 1-1
867 to 1-1870, 1-1873, 1-187
7, 1-1883, 1-1888 to 1-1895, 1
-1898, 1-1900, 1-1902 to 1-19
05, 1-1908, 1-1912, 1-1918, 1
-1922 to 1-1930, 1-1933, 1-19
35, 1-1937 to 1-1940, 1-1943,
1-1947, 1-1953, 1-1957 to 1-1
965, 1-1968, 1-1970, 1-1972
1-11-1975, 1-1978, 1-182, 1-1
988, 1-1992 to 1-2000, 1-200
3, 1-2005, 1-2007 to 1-2010, 1
-2013, 1-22017, 1-2022, 1-202
7 to 1-2035, 1-2038, 1-2040, 1
−2042 to 1-2048, 1-2048, 1-20
52, 1-2205, 1-2206 to 1-2070,
1-2073, 1-2075, 1-20777 through 1-2
080, 1-2083, 1-2087, 1-2093,
1-2209 to 1-2105, 1-2108, 1-2
110, 1-2112 to 1-2115, 1-211
8, 1-2122, 1-2128, 1-2132 to 1
-2140, 1-2143, 1-2145, 1-214
7 to 1-2150, 1-2153, 1-2157, 1
-2163, 1-2167 to 1-2175, 1-21
78, 1-2180, 1-2182 to 1-2185,
1-2188, 1-2192, 1-2198, 1-22
02 to 1-2210, 1-2213, 1-2215,
1-2217 to 1-2220, 1-2223, 1-2
227, 1-2233, 1-2237 to 1-224
5, 1-2248, 1-2250, 1-2225 to 1
-2255, 1-2258, 1-2262, 1-226
8, 1-2272 to 1-2280, 1-2283, 1
-2285, 1-2287 to 1-2290, 1-22
93, 1-2297, 1-2303, 1-2307 through
1-2315, 1-2318, 1-2320, 1-23
22 to 1-2325, 1-2328, 1-2332,
1-2338, 1-2342 through 1-2350, 1-2
353, 1-2355, 1-2357 to 1-236
0, 1-2363, 1-2367, 1-2373, 1-
2377 to 1-2385, 1-2388, 1-239
0, 1-2392 to 1-2395, 1-2398, 1
-2402, 1-2408, 1-2412 to 1-24
20, 1-2423, 1-2425, 1-2427 through
1-2430, 1-2433, 1-237, 1-24
43, 1-2247 to 1-2455, 1-2458,
1-2460, 1-2462 to 1-2465, 1-2
468, 1-2472, 1-2478, 1-2482ino
To 1-2490, 1-2493, 1-2495, 1-2
497 to 1-2500, 1-2503, 1-250
7, 1-2513, 1-2517 through 1-2520, 1
-2522 to 1-2524, 1-2525, 1-25
28, 1-2529, 1-2539 through 1-2541,
1-2543, 1-2545, 1-2547, 1-25
49 to 1-2552, 1-2554, 1-2556,
1-2557, 1-2560 through 1-2564, 1-2
566, 1-2568, 1-2570, 1-2572
To 1-2575, 1-2577, 1-2579, 1-2
580, 1-258 to 1-2587, 1-258
9, 1-2591, 1-2593, 1-2629, 1-
2630, 1-2632, 1-2645, 1-265
0, 1-2651, 1-2653, 1-2654, 1-
2656, 1-2657, 1-2665 to 1-266
7, 1-2707 to 1-2709, 1-2779, 1
-2780, 1-2782, 1-2783, 1-290
5, 1-2906, 1-2908, 1-2909, 1-
3031, 1-3032, 1-3157, 1-315
8, 1-3253 to 1-3322, 2-3, 2-7,
2-11, 2-15, 2-19, 2-23, 2-27,
2-31, 2-35, 2-42, 2-45, 2-47no
2-51, 2-65, 2-71, 2-73, 2-8
9, 2-94, 2-97, 2-101, 2-105,
-109, 2-113, 2-117, 2-121, 2-
125, 2-129, 2-136, 2-139, 2-1
41 to 2-145, 2-159, 2-165, 2-1
67, 2-183, 2-190, 2-194, 2-19
8, 2-202, 2-206, 2-210, 2-21
4, 2-218, 2-222, 2-229, 2-23
2, 2-234 to 2-238, 2-252, 2-25
8, 2-260, 2-276, 2-283, 2-28
7, 2-291, 2-295, 2-299, 2-30
3, 2-307, 2-311, 2-315, 2-32
2, 2-325, 2-327 to 2-331, 2-34
5, 2-351, 2-353, 2-369, 2-37
6, 2-380, 2-384, 2-388, 2-39
2, 2-396, 2-400, 2-404, 2-40
8, 2-415, 2-418, 2-420 to 2-42
4, 2-438, 2-444, 2-446, 2-46
2, 2-469, 2-473, 2-478, 2-48
1, 2-485, 2-489, 2-493, 2-49
7, 2-501, 2-508, 2-511, 2-513
To 2-517, 2-531, 2-537, 2-53
9, 2-555, 2-562, 2-566, 2-57
0, 2-574, 2-578, 2-582, 2-58
6, 2-590, 2-594, 2-601, 2-60
4, 2-606 to 2-610, 2-624, 2-63
0, 2-632, 2-648, 2-655, 2-65
9, 2-663, 2-667, 2-671, 2-67
5, 2-679, 2-683, 2-687, 2-69
4, 2-697, 2-699 to 2-703, 2-71
7, 2-723, 2-725, 2-741, 2-74
8, 2-752, 2-756, 2-760, 2-76
4, 2-768, 2-772, 2-776, 2-78
0, 2-787, 2-790, 2-792 to 2-79
6, 2-810, 2-816, 2-818, 2-83
4, 2-841, 2-845, 2-849, 2-85
3, 2-857, 2-861, 2-865, 2-86
9, 2-873, 2-880, 2-883, 2-885
To 2-889, 2-903, 2-909, 2-91
1, 2-927, 2-934, 2-938, 2-94
2, 2-946, 2-950, 2-954, 2-95
8, 2-962, 2-966, 2-973, 2-97
6, 2-978 to 2-982, 2-996, 2-10
02, 2-1004, 2-1020, 2-1027, 2
-1031, 2-1035, 2-1039, 2-104
3, 2-1047, 2-1051, 2-1055, 2-
1059, 2-1066, 2-1069, 2-1071
To 2-1075, 2-1089, 2-1095, 2-
1097, 2-1113, 2-1120, 2-112
4, 2-1128, 2-1132, 2-1136, 2-
1140, 2-1144, 2-1148, 2-115
2, 2-1159, 2-1162, 2-1164 to 2
-1168, 2-1182, 2-1188, 2-119
0, 2-1206, 2-1213, 2-1217, 2-
1221, 2-1225, 2-1229, 2-123
3, 2-1237, 2-1241, 2-1245, 2-
1252, 2-1255, 2-1257 to 2-126
1, 2-1275, 2-1281, 2-1283, 2-
1299, 2-1306, 2-1310, 2-131
4, 2-1318, 2-1322, 2-1326, 2-
1330, 2-1334, 2-1338, 2-134
5, 2-1348, 2-1350 to 2-1354, 2
-1368, 2-1374, 2-1376, 2-139
2, 2-1397 to 2-1405, 2-1408, 2
-1410, 2-1412 to 2-1415, 2-14
18, 2-1422, 2-1428, 2-1432 to
2-1440, 2-1443, 2-1445, 2-14
47 to 2-1450, 2-1453, 2-1457,
2-1463, 2-1467 to 2-1475, 2-1
478, 2-1480, 2-1482 to 2-148
5, 2-1488, 2-1492, 2-1498, 2-
1502 to 2-1510, 2-1513, 2-151
5, 2-1517 to 2-1520, 2-1523, 2
-1527, 2-1533, 2-1537 to 2-15
45, 2-1548, 2-1550, 2-1552 or later
2-1555, 2-1558, 2-1562, 2-15
68, 2-1572-2-1580, 2-1583,
2-1585, 2-1587 to 2-1590, 2-1
593, 2-1597, 2-1603, 2-1607
2-1615, 2-1618, 2-1620, 2-1
622 to 2-1625, 2-1628, 2-163
2, 2-1638, 2-1642 to 2-1650, 2
-1653, 2-1655, 2-1657 to 2-16
60, 2-1663, 2-1667, 2-1673, 2
-1677 to 2-1685, 2-1688, 2-16
90, 2-1692 to 2-1695, 2-1698,
2-1702, 2-1708, 2-1712 to 2-1
720, 2-1723, 2-1725, 2-1727
2-1730, 2-1733, 2-1737, 2-1
743, 2-1747 to 2-1755, 2-175
8, 2-1760, 2-1762 to 2-1765, 2
-1768, 2-1772, 2-1778, 2-178
2 to 2-1790, 2-1793, 2-179,2
-1797 to 2-1800, 2-1803, 2-18
07, 2-1813, 2-1817 to 2-1825,
2-1828, 2-1830, 2-1833 to 2-1
835, 2-1838, 2-1842, 2-1848,
2-1852 to 2-1860, 2-1863, 2-1
865, 2-1867 to 2-1870, 2-187
3, 2-1877, 2-1883, 2-187 to 2
-1895, 2-1898, 2-1900, 2-190
2 to 2-1905, 2-1908, 2-1912, 2
-1918, 2-1922 to 2-1930, 2-19
33, 2-1935, 2-1937 to 2-1940,
2-1943, 2-1947, 2-1953, 2-19
57 to 2-1965, 2-1968, 2-1970,
2-1972 to 2-1975, 2-1978, 2-1
982, 2-1988, 2-1992 to 2-200
0, 2-2003, 2-2005, 2-2007 or 2
-2010, 2-2013, 2-2017, 2-202
3, 2-2027 to 2-2035, 2-2038, 2
-2040, 2-2042 to 2-2045, 2-20
48, 2-2052, 2-2058, 2-2062 to
2-2070, 2-2073, 2-2075, 2-20
77 to 2-2080, 2-2083, 2-2087,
2-2093, 2-2097 to 2-2105, 2-2
108, 2-2110, 2-2112 to 2-211
5, 2-2118, 2-2122, 2-2128, 2-
2132 to 2-2140, 2-2143, 2-214
5, 2-2147 to 2-2150, 2-2153, 2
-2157, 2-2163, 2-2167 to 2-21
75, 2-2178, 2-2180, 2-2182 to
2-2185, 2-2188, 2-2192, 2-21
98, 2-2202 to 2-2210, 2-2213,
2-2215, 2-2217 to 2-2220, 2-2
223, 2-2227, 2-2233, 2-2237
2-2245, 2-2248, 2-2250, 2-2
252 to 2-2255, 2-2258, 2-226
2, 2-2268, 2-2272 to 2-2280, 2
-2283, 2-2285, 2-2287 to 2-22
90, 2-2293, 2-2297, 2-2303, 2
-2307 to 2-2315, 2-2318, 2-23
20, 2-2322 to 2-2325, 2-2328,
2-2332, 2-2338, 2-2342 to 2-2
350, 2-2353, 2-2355, 2-2357
2-2360, 2-2363, 2-267, 2-2
373, 2-2377 to 2-2385, 2-238
8, 2-2390, 2-2392 to 2-2395, 2
-2398, 2-2402, 2-2408, 2-241
2 to 2-2420, 2-2423, 2-2425, 2
-2427 to 2-2430, 2-2433, 2-24
37, 2-2443, 2-247 to 2-2455,
2-2458, 2-2460, 2-2462 to 2-2
465, 2-2468, 2-2472, 2-2478,
2-2482 to 2-2490, 2-2493, 2-2
495, 2-2497 to 2-2500, 2-250
3, 2-2507, 2-2513, 2-2517 or 2
-2520, 2-2522, 2-2524, 2-252
5, 2-2528, 2-2529, 2-2539 or 2
-2541, 2-2543, 2-2545, 2-254
7, 2-2549 to 2-2552, 2-2554, 2
-2556, 2-2557, 2-2560 to 2-25
64, 2-2566, 2-2568, 2-2570, 2
-2572 to 2-2575, 2-2577, 2-25
79, 2-2580, 2-2581 to 2-2587,
2-2589, 2-2591, 2-2593, and 2
The compounds of -3253 to 2-3322 can be mentioned.
Wear.

Particularly preferred compounds include the following compounds: 4- (3-aminopropyl) -2- (4-fluorophenyl) -3- (pyridin-4-yl)- 1H-pyrrole 4- (3-acetylaminopropyl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H
-Pyrrole 2- (4-fluorophenyl) -4- (3-methylaminopropyl) -3- (pyridin-4-yl) -1H-
Pyrrole • [5- (4-fluorophenyl) -4- (pyridine-
4-yl) -1H-pyrrol-3-yl]-(pyridin-4-yl) methanol 4- (1-acetyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4 -Fluorophenyl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (1,2,3,6-tetrahydropyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (piperidine-
4-yl) -3- (pyridin-4-yl) -1H-pyrrole 3- (4-fluorophenyl) -1- (piperidin-
4-yl) -2- (pyridin-4-yl) -1H-pyrrole 1- (1-acetylpiperidin-4-yl) -3-
(4-Fluorophenyl) -2- (pyridin-4-yl) -1H-pyrrole. 3- (4-fluorophenyl) -1- [1- (2-nitroethyl) piperidin-4-yl] -2- ( Pyridin-4-yl) -1H-pyrrole 3- (4-fluorophenyl) -1- [3- (morpholin-1-yl) propyl] -2- (pyridin-4-yl) -1H-pyrrole3 -(4-Fluorophenyl) -1- (piperidine-
3-yl) -2- (pyridin-4-yl) -1H-pyrrole 1- (azetidin-3-yl) -3- (4-fluorophenyl) -2- (pyridin-4-yl) -1H- Pyrrole 4- (3-dimethylaminopropyl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H
-Pyrrole 2- (4-fluorophenyl) -4- [3- (piperidin-1-yl) propyl] -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl)- 4- [3- (1-Methylpiperazin-4-yl) propyl] -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-methyl-
1,2,3,6-tetrahydropyridin-4-yl)-
3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-methylpiperidin-4-yl) -3- (pyridin-4-yl)-
1H-pyrrole 3- (4-fluorophenyl) -2- (pyridine-4
-Yl) -1- (2,2,6,6-tetramethylpiperidin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (quinuclidin-2-en-3-yl)
-1H-pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (quinuclidin-3-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (4-hydroxypiperidin-4-yl) -3- (pyridin-4-yl)- 1H-pyrrole 3- (4-fluorophenyl) -2- (pyridine-4
-Yl) -1- (quinuclidin-3-yl) -1H-pyrrole 1- (4-aminocyclohexyl) -3- (4-fluorophenyl) -2- (pyridin-4-yl) -1H-
Pyrrole3- (4-fluorophenyl) -2- (2-methylaminopyrimidin-4-yl) -1- (piperidin-4-
Yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (8-methyl-
8-azabicyclo [3.2.1] oct-2-ene-3
-Yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (8-methyl-
8-Azabicyclo [3.2.1] octan-3-yl)
-3- (pyridin-4-yl) -1H-pyrrole-4- (8-azabicyclo [3.2.1] oct-2
-En-3-yl) -2- (4-fluorophenyl)-
3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (1,2,3,6-tetrahydro-2,
2,6,6-tetramethylpyridin-4-yl) -1H
-Pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (2,2,6,6-tetramethylpiperidin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (2-methyl-
1,2,3,6-tetrahydropyridin-4-yl)-
3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (6-methyl-
1,2,3,6-tetrahydropyridin-4-yl)-
3- (pyridin-4-yl) -1H-pyrrole. 4- (1-ethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl)-
3- (pyridin-4-yl) -1H-pyrrole. 4- (1-ethylpiperidin-4-yl) -2- (4
-Fluorophenyl) -3- (pyridin-4-yl)-
1H-pyrrole 2- (4-fluorophenyl) -4- (1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-propyl-1,2,3,6-tetrahydropyridin-4-yl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-phenethyl-1,2,3,6-tetrahydropyridin-4-yl) -3- ( Pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,8,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,6,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 4- (1,6-dimethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3 -(Pyridin-4-yl) -1H-pyrrole 4- (1,2-dimethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- ( Pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,2,
6,6-pentamethyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl)-
1H-pyrrole 4- (3-dimethylamino-1-propen-1-yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (4-amino Butyl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (1-ethyl-6-methyl-1,2,3,6-tetrahydropyridine-4- Yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (1-ethyl-2-methyl-1,2,3,6-tetrahydropyridine-4- Yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 1- (3-dimethylaminopropyl) -3- (4-fluorophenyl) -2- (pyridine- 4-yl) -1H
-Pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,6,7,8,8a-octahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole -4- (6-allyl-1-methyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4- Fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (2-allyl-1-methyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4- Fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (6-benzyl-1-methyl-1,2,3,6-
Tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (2-benzyl-1-methyl-1,2,3,6-
Tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (6-methyl-
1-propyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (2-methyl-
1-propyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,3 4,
6,7,9a-Hexahydro-2H-quinolidine-8-
Yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,3,4,
6,9,9a-Hexahydro-2H-quinolidine-8-
Yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3
5,8,8a-Hexahydroindolizin-7-yl)
-3- (2-Methylaminopyrimidin-4-yl) -1
H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,6,8a-Hexahydroindolizin-7-yl)
-3- (2-Methylaminopyrimidin-4-yl) -1
H-pyrrole 2- (3,4-difluorophenyl) -4- (1,
2,3,5,8,8a-Hexahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole2- (3,4-difluorophenyl) -4- (1,
2,3,5,6,8a-hexahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole Il)-
2- (3-trifluoromethylphenyl) -1H-pyrrole 4- (1,2,3,5,6,8a-hexahydroindolizin-7-yl) -3- (pyridin-4-yl)-
2- (3-trifluoromethylphenyl) -1H-pyrrole 2- (3-fluorophenyl) -4- (1,2,3
5,8,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (3-fluorophenyl) -4- (1,2,3
5,6,8a-Hexahydroindolizin-7-yl)
-3- (Pyridin-4-yl) -1H-pyrrole 2- (3-chlorophenyl) -4- (1,2,3
5,8,8a-Hexahydroindolizin-7-yl)
-3- (Pyridin-4-yl) -1H-pyrrole 2- (3-chlorophenyl) -4- (1,2,3
5,6,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 4- (1,2,3,5,8,8a-hexahydroindolizin-7-yl) -2-phenyl-3- (pyridine-4 -Yl) -1H-pyrrole 4- (1,2,3,5,6,8a-hexahydroindolizin-7-yl) -2-phenyl-3- (pyridin-4-yl) -1H-pyrrole .

The combinations of the substituents (R ¹ , R ² and R ³ ) specifically shown in Tables 1 and 2 are represented by formulas (I-2), (I-4) and (I-4). -5) can also be applied.

[0090]

BEST MODE FOR CARRYING OUT THE INVENTION The compound (I) of the present invention can be produced according to the following method. <Method A> In the method A, the compounds having the general formula (I)
This is a method for producing a compound having the general formula (I-1).

[0091]

Embedded image (In the above formula, R ¹ , R ² and R ³ have the same meanings as described above.) In the step 1a, the aminonitrile compound (1a) and α, β
A step of producing a pyrrolidine compound (3a) by reacting with an unsaturated aldehyde compound (2a);
This is performed according to the method detailed in 3823.

In the step 2a, the pyrrolidine compound (3a)
Is a method for producing a pyrrole derivative (I-1) of the present invention by performing a hydrogen cyanide reaction and a dehydration reaction, and is carried out according to the method described in detail in EP 733823. <Method B>, <Method C>, <Method D> and <Method E>

[0093]

Embedded image (In the above formula, R ¹ , R ² and R ³ have the same meanings as described above.) Method B, Method C, Method D and Method E are each represented by the general formula (I-
2) A method for producing a compound having (I-3), (I-4) and (I-5), wherein the steps 1b, 1c, 1d and 1e are steps 1a and Steps 2b, 2c, 2d and 2
Step e is performed similarly to step 2a. Among the compounds (I-1) of the present invention, those in which R ³ is aminomethyl, aminoethyl, aminopropyl or aminopropenyl can also be produced by the following Method F. <F method>

[0094]

Embedded image (In the above formula, R ¹ and R ² are as defined above, and R ¹³
Represents a hydrogen atom, the above “lower alkyl group” or the above “aralkyl group”. The third step is a step of reacting an α, β-unsaturated compound (4) with an isonitrile compound (5) to produce a pyrrolecarboxylic acid derivative (6). For example, R. Di Santo
et al., Synthetic Communications, 25 (6), 795-802
It is carried out according to the method described on page (1995).

The fourth step is a step of producing a hydroxymethyl compound (7) by reducing the pyrrole carboxylic acid derivative (6). Using RFNystrom et al.,
Performed according to the method detailed in J. Am. Chem. Soc., 71 , 3245 (1945).

The fifth step is a step of oxidizing the hydroxymethyl compound (7) to produce the aldehyde compound (8). For example, using a oxidizing agent such as chromic acid, manganese dioxide, dimethylsulfoxide, etc. Bartel & FB
It is performed according to the method detailed in ohlmann, Tetrahedron Lett., 685 (1985).

The sixth step is a step for producing an oxime compound (9) by reacting the aldehyde compound (8) with hydroxyamine, and is carried out according to a conventional method.

The seventh step is a step of producing the compound (I-1a) of the present invention by reducing the oxime compound (9), for example, by catalytic reduction or reduction with diborane [PNRylander & DRSteele] , Engelhald
Ind.Tech.Bull., 3 , 19 (1962), JASecrist, III &
MWLogue, J. Org. Chem., 37, 335 (1972). ].

The eighth step is a step of producing a nitroolefin compound (10) by performing dehydration condensation (aldol condensation) of the aldehyde compound (8) and nitromethane. For example, DEWorall, Org. , 413 (1
941).

In the ninth step, the nitroolefin compound (1
0) to produce the compound (I-1b) of the present invention. For example, SIMurahashi et al., Bull.
m. Soc. Jpn., 63 , 1252 (1990).

The tenth step is a step for producing a cyanoolefin compound (11) from the aldehyde compound (8). In this step, for example, the same aldol condensation reaction or Wittig reaction as employed in the eighth step [The Organic Chemistry of Phosphorous, Elsevier
(1967)] or Wittig-Horner reaction [L. Ho.
rner et al., Chem. Ber., 95 , 581 (1962)].

The eleventh step is a step for producing a cyanoethyl compound (12) by reducing the double bond of the cyanoolefin compound (11).
t al., J. Org.Chem., 52 , 1686 (1987), T. Hudlicky
, J. Org. Chem., 52, 4641 (1987).

In the twelfth step, the cyanoethyl compound (1
Compound (I-1c) of the present invention by reducing the cyano group of 2)
Is, for example, using lithium aluminum hydride and diisobutyl aluminum hydride, NMYoon & HC Brown, J. Am. Chem. Soc., 90 , 2927
(1968), J. Meinweld et al., J. Org. Chem., 29 , 2914.
(1964).

In the thirteenth step, the cyano group of the compound (I-1) is reduced by reducing the cyano group of the cyanoolefin compound (11).
This is a step of manufacturing d), and is performed in the same manner as in the twelfth step.

Compound (I-1a) and compound (I-1)
b), the amino groups of compound (I-1c) and compound (I-1d) are alkylated, acylated and / or
Alternatively, a compound having an amino group substituted with a nitrogen atom can be synthesized by sulfonylation. In compound (I-1) of the present invention, R ³ may be substituted with a group selected from substituent group α and substituent group δ, and R ³ is selected from substituent group β and substituent group γ. A heterocyclyl group substituted with a group selected from the group consisting of: a heterocyclyl group having at least one nitrogen atom, which may be substituted by a group selected from the substituent group α and the substituent group δ; or a general formula:
_{CH (OH) - (CH 2} ) k -R 4 ( wherein, R ⁴ have the same meanings as defined above, -CH (OH) - (CH 2) k - is substituted with a hydroxyl group in the definition of X A compound having a lower alkylene group and k represents 0 or an integer of 1 to 5) can also be produced by the following Method G. <G method>

[0106]

Embedded image (In the above formula, R ¹ , R ² , R ⁴ and k have the same meanings as described above, and R ¹⁴ is the same or different and each is a hydrogen atom, the “lower alkyl group” or the “aralkyl group” In the definition of R ⁴ , the cyclic group B may be “substituted with a group selected from the substituent group α and the substituent group δ, and selected from the substituent group β and the substituent group γ. A group corresponding to a `` heterocyclyl group substituted by a group selected from the group consisting of a group selected from substituent groups α and δ, and a heterocyclyl group having at least one nitrogen atom '' The fourteenth step is a step of producing a di-substituted pyrrole compound (13) by decarboxylation of the carboxylic acid compound (6a).
In this step, a method commonly used in organic synthetic chemistry of heating under acidic, alkaline, or neutral conditions (N.Yo
shida et al., Yakugaku Zasshi, 93 (5), 584-598 (1973
Year)) can be adopted.

In the fifteenth step, the disubstituted pyrrole compound (1
The silyl compound (1) is obtained by silylating the nitrogen atom at position 1 of 3).
This is the step of manufacturing 4).

In the sixteenth step, the silyl compound (14) obtained in the fifteenth step is converted into a brominating agent (for example,
N-bromosuccinimide) to give a bromopyrrole compound (15), and then, in a seventeenth step, the compound (15) is lithiated and then reacted with a heterocyclyl ketone (16) to give a hydroxyheterocyclyl compound (17) And in the eighteenth step, tetrabutylammonium fluoride (TBAF)
The compound (I-1e) of the present invention can be produced by deprotection (desilylation) by the method described above.

The reactions from the fifteenth step to the eighteenth step are as follows:
Brian L. Bray et al., J. Org.Chem., 55 , 6317-6318 (19
1990).

The nineteenth step is a step of producing an unsaturated heterocyclyl compound (18) by subjecting the hydroxyheterocyclyl compound (17) to a dehydration reaction. This dehydration reaction is usually performed in the presence of an acid catalyst such as sulfuric acid, a solid catalyst such as alumina, or a halogenating agent such as thionyl chloride. [These reactions are, for example, GHColeman &
HF Johnstone, Org. Synth., I, 183 (1941), RLSaw
yer & DWAndrus, Org.Synth., III, 276 (1955), and JSLomas et al., Tetrahedron Lett., 599 (1971)
In detail. ]. In addition, the dehydration reaction in this step is a reaction using trialkylsilane such as triethylsilane, tripropylsilane, and tributylsilane, and trifluoroacetic acid [for example, Francis A. Carey & Henry S. Tre.
mper, J. Am. Chem. Soc., 91, 2967-2972 (1969)].

The twentieth step is a step for producing a compound (I-1f) of the present invention by removing the protecting group (silyl group) of the unsaturated heterocyclyl compound (18). Is done.

In the twenty-first step, compound (I-1f) of the present invention is prepared.
This is a step of producing the compound (I-1g) of the present invention by reducing the double bond in the cyclic group B, and carried out in the same manner as in the eleventh step.

In the 22nd step, the bromopyrrole compound (1
This is a step of producing a hydroxy compound (20) using 5) and the aldehyde compound (19), and is carried out in the same manner as in the seventeenth step.

In the twenty third step, the hydroxy compound (20)
To remove the protecting group (silyl group) of the compound of the present invention (I-
1h), which is carried out in the same manner as in the eighteenth step.

In the above compound (I-1h), K
Is an integer of 1 to 5, for the compound:
By performing a dehydration reaction in the same manner as in the nineteenth step, a corresponding alkenylene derivative can be obtained.

In general, the compound (I) of the present invention
Can be produced by introducing an R ³ group into a pyrrole compound having an R ¹ group and an R ² group. Can be. <H method>

[0117]

Embedded image (In the above formula, R ¹ , R ² , R ³ and R ¹⁴ have the same meanings as described above, and L represents a leaving group.

The term "leaving group" in the definition of L is usually
Represents a group leaving as a nucleophilic residue, for example, a halogen atom such as fluorine, chlorine, bromine or iodine; a trihalogenomethyloxy group such as trichloromethoxy; a lower alkane such as methanesulfonyloxy or ethanesulfonyloxy A sulfonyloxy group; a halogeno lower alkanesulfonyloxy group such as trifluoromethanesulfonyloxy and pentafluoroethanesulfonyloxy; and an arylsulfonyloxy group such as benzenesulfonyloxy, p-toluenesulfonyloxy and p-nitrobenzenesulfonyloxy. be able to. It is preferably a halogen atom, particularly preferably a bromine atom. In the 24th step, the bromopyrrole compound (15) is added to the first
As in the 7th step, this is a step of producing a compound (22) by reacting with the compound (21) after lithiation, and for example, carried out according to the method detailed in WO99 / 01449.

The 25th step is a step for producing the compound (I-1) of the present invention by removing the protecting group (silyl group) of the compound (22), and is carried out in the same manner as the 18th step. . In the compound (I) of the present invention, R ³ has the general formula -X
-R group [wherein with ⁴ a, R ⁴ a is in the definition of R ^4, may be substituted with a group selected from Substituent group α and Substituent group [delta], Substituent group β and substituents A heterocyclyl group substituted with a group selected from group γ; a heterocyclyl group having at least one nitrogen atom, which may be substituted with a group selected from substituent group α and substituent group δ; —NR ^a R ^b (wherein R ^a and R ^b have the same meanings as described above), and represent a group bonded to the X group via a nitrogen atom. ] Can also be produced by the following method I. <Method I>

[0120]

Embedded image (In the above formula, the cyclic group ^{A, R 1, R 2,} R 4 a, L and X
Is as defined above. The 26th step comprises the step of reacting the compound (23) with the amine compound (24)
By reacting the door, by replacing the group L based on R ⁴ a, it is a step for preparing a compound of the present invention (Ia). This reaction is usually carried out in a solvent in the presence or absence of a base, for example, methanol,
Alcohols such as ethanol, propanol and isopropanol; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran and dioxane; dimethylformamide, dimethylacetamide;
Aprotic polar solvents such as dimethyl sulfoxide;
Nitriles such as acetonitrile; esters such as methyl acetate and ethyl acetate; aromatic hydrocarbons such as benzene, toluene and xylene; pentane, hexane;
Aliphatic hydrocarbons such as heptane can be mentioned.

Examples of the base used include, for example, sodium methoxide, sodium ethoxide, potassium-t
Alkali metal alkoxides such as butoxide; alkali metal hydrides such as sodium hydride and lithium hydride; alkali metal hydroxides such as sodium hydroxide and potassium hydroxide; alkalis such as sodium carbonate and potassium carbonate. Metal carbonates; amines such as triethylamine, tributylamine, pyridine, picoline, 1,8-diazabicyclo [5.4.0] -7-undecene.

The compounds of the present invention in (Ia), R ⁴ a
(Ia ′) wherein is an amino group (—NH ₂ ) can also be produced via an azide compound (25).

The 27th step is a step of reacting the compound (23) with sodium azide in the presence of a solvent to produce an azide compound (25).

Examples of the solvent used include halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride and dichloroethane; ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran and dioxane; dimethylformamide, dimethylacetamide Aprotic polar solvents such as dimethylsulfoxide; nitriles such as acetonitrile;
Esters such as methyl acetate and ethyl acetate; aromatic hydrocarbons such as benzene, toluene and xylene; aliphatic hydrocarbons such as pentane, hexane and heptane; and mixed solvents thereof.

The twenty-eighth step is a step of reducing the azide compound (25) to produce the compound (Ia ') of the present invention. This step is performed, for example, by EJCorey et al., Synthesis,
It is carried out according to the catalytic reduction method detailed in 590 (1975). In the compound (I) of the present invention, R ² is NR ^c R
Compound (Ib), which is a heteroaryl group having at least one nitrogen atom substituted with ^d , can also be produced by the following Method J. <J method>

[0126]

Embedded image [In the above formula, the cyclic groups A, R ¹ , R ³ , R ^c and R ^d have the same meanings as described above, L ′ represents a leaving group, and a group —R ^{2 ′} —
L ′ is a “heteroaryl group having at least one nitrogen atom” having a leaving group (group L ′) (for example, 2-methanesulfonylpyrimidin-4-yl, 2-methanesulfonylpyridin-4-yl and the like) ), And the “heteroaryl group having at least one nitrogen atom” is R ²
And the same group as the "heteroaryl group having at least one nitrogen atom" in the definition of.

The leaving group in the definition of L 'is the same as the leaving group in the definition of L, or methanesulfonyl,
Ethanesulfonyl, propanesulfonyl, a lower alkylsulfonyl group such as butanesulfonyl, preferably a lower alkylsulfonyl group, more preferably
Methanesulfonyl. In a twenty-ninth step, a compound (2)
6) is reacted with an amine compound (27) to convert the leaving group into NR ^c R ^d , thereby obtaining the compound (I) of the present invention.
This is the step of manufacturing b). This step is performed in the same manner as in the 26th step. Further, among the compounds (I) of the present invention, the compound wherein R ³ is a group containing a pyridine ring can be produced by subjecting the corresponding tetrahydropyridine compound to a dehydrogenation reaction (the following “Step 30”). The dehydrogenation reaction can be performed using palladium-carbon, G.
Performed according to the method detailed in Wieslaw et al., J. Med. Chem., 28, 311-317 (1985).

[0128]

Embedded image Compounds serving as starting materials in the above methods A to J, ie, compounds (1a), (1b), (1c), (1
d), (1e), (2a), (2b), (2c), (2
d), (2e), (4), (5), (6a), (1
6), (19), (21), (24) and (27)
It is a compound known per se or a compound which can be easily obtained by treating a known compound according to a known method (eg, the method described in WO97 / 5877), and a compound (23) ) And (26) can be easily synthesized from known compounds by performing the same reaction as in the above methods A to E.

In particular, among the compounds (16), a 4-oxopiperidine compound [(35) below] can also be produced by the following <Method K>. <K method>

[0130]

Embedded image [Wherein R ⁵ , R ⁷ , R ⁸ , R ⁹ , R ¹⁰ , R ¹¹ and R ¹²
Has the same meaning as described above, and R ¹⁵ and R ¹⁶ are the same or different and represent the above “lower alkyl group” or the above “aralkyl group”. In the <Method K>, first, the unsaturated ester compound (2
An amino ester compound (30) is produced by adding an amine compound (29) to 8) (Step 31), and another unsaturated ester compound [compound (31)] is added thereto. The diester compound (32) is obtained (the 32nd step). Next, the compound (32) is subjected to a Dieckmann reaction (step 33) to obtain a ketoester compound [compound (33) and / or compound (34)]. 4-oxopiperidine compound (35)
Is manufactured (34th step).

In the thirty-fifth step, the unsaturated ester compound (2
This is a step of producing a diester compound (32) by reacting 8) with an aminoester compound (36), and is carried out in the same manner as in the 32nd step. Compound (32)
Wherein R ¹⁰ and R ¹¹ are taken together to form a lower alkylene group, or a lower alkylene group substituted with a group selected from substituent group α, substituent group β, substituent group γ and substituent group δ. When a compound forming a group is produced, this step is preferably employed.

The reactions employed in the above-mentioned steps 31 to 35 are described in UMTeotino, J. Org. Chem., 27, 1406.
(1962);

Further, in the 4-oxopiperidine compound (35), R ¹⁰ and R ¹¹ together form a lower alkylene group or a substituent group α, a substituent group β, a substituent group γ, The compound (35a) forming a lower alkylene group substituted with a group selected from the group δ can also be produced by the method shown in <Method L> below. <L method>

[0134]

Embedded image [Wherein R ¹⁷ and R ¹⁸ are the same or different,
Wherein indicates the "lower alkyl group" or the "aralkyl group", R ¹⁹ and R ^20, same or different, and represent the "lower alkyl group", or, R ¹⁹ and R ^20, together , The above-mentioned “lower alkylene group”;
¹⁰ and R ¹¹ form together, a "lower alkylene group" or a "lower alkylene substituted with a group selected from substituent group α, substituent group β, substituent group γ and substituent group δ. "Ki" and consent. ] In each step of the L method, O. Pollet et al., Heterocycles, 43, 1391 (1996)
Or Anet et al., Austral. J. scient. Res., <A> 3, 6
The reaction can be carried out according to the reaction described in detail in 35-640 (1950).

After completion of each of the above reactions, the target compound is collected from the reaction mixture according to a conventional method.

For example, the reaction mixture is appropriately neutralized, and if there is any insoluble matter, it is removed by filtration. Then, an immiscible organic solvent such as water and ethyl acetate is added. An organic layer containing the compound is separated, dried over anhydrous magnesium sulfate or the like, and then obtained by distilling off the solvent.

If necessary, the obtained target compound may be prepared by a conventional method.
For example, recrystallization, reprecipitation, or a method commonly used for separation and purification of organic compounds, for example, adsorption column chromatography using a carrier such as silica gel, alumina, and magnesium-silica gel type florisil; Sephadex LH-20 (manufactured by Pharmacia), Amberlite XAD-11 (manufactured by Rohm and Haas),
A method using a synthetic adsorbent such as distribution column chromatography using a carrier such as Diaion HP-20 (manufactured by Mitsubishi Chemical Corporation), a method using ion exchange chromatography,
Alternatively, separation and purification can be performed by appropriately combining a normal phase / reverse phase column chromatography method with silica gel or alkylated silica gel (preferably high performance liquid chromatography) and eluting with a suitable eluent. . Since the heteroaryl-substituted pyrrole derivative of the present invention exhibits an excellent inflammatory cytokine production inhibitory action,
It is effective as a medicine (particularly, an agent for preventing or treating a disease mediated by inflammatory cytokines). Such drugs include, for example, analgesic / anti-inflammatory agents, antiviral agents, and rheumatoid arthritis, osteoarthritis, allergic diseases, asthma, sepsis, psoriasis, osteoporosis, autoimmune diseases (eg, systemic lupus erythematosus) , Ulcerative colitis, Crohn's disease, etc.), diabetes, nephritis, hepatitis, tumor, ischemic heart disease, Alzheimer's disease, arteriosclerosis prophylactic or therapeutic agent, especially analgesic / anti-inflammatory agent, And prophylactic or therapeutic agents for rheumatoid arthritis, osteoarthritis, allergic diseases, sepsis, psoriasis, osteoporosis, ulcerative colitis, diabetes, hepatitis, and arteriosclerosis.

The administration form of the compound of the present invention having the general formula (I), a pharmaceutically acceptable salt or derivative thereof includes:
For example, oral administration such as tablets, capsules, granules, powders or syrups, or parenteral administration such as injections or suppositories can be mentioned. These preparations are manufactured by a known method using additives such as excipients, lubricants, binders, disintegrants, stabilizers, flavoring agents, and diluents.

Here, as the excipient, for example, sugar derivatives such as lactose, sucrose, glucose, mannitol and sorbitol; corn starch, potato starch, α-
Starch derivatives such as starch, dextrin, carboxymethyl starch; cellulose derivatives such as crystalline cellulose, low-substituted hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxymethylcellulose, carboxymethylcellulose calcium, internally cross-linked sodium carboxymethylcellulose; gum arabic; dextran; Organic excipients such as pullulan; and silicate derivatives such as light silicic anhydride, synthetic aluminum silicate, magnesium metasilicate aluminate; phosphates such as calcium phosphate; carbonates such as calcium carbonate; And inorganic excipients such as sulfates.

Examples of the lubricant include metal stearates such as stearic acid, calcium stearate and magnesium stearate; talc; colloidal silica; waxes such as veegum and gay wax; boric acid: adipic acid; Sodium sulfate, DL-leucine; fatty acid sodium salt; lauryl sulfate such as sodium lauryl sulfate, magnesium lauryl sulfate; silicic acids such as silicic anhydride, silicic acid hydrate; And the above-mentioned starch derivatives.

Examples of the binder include polyvinylpyrrolidone, macrogol and the same compounds as the above-mentioned excipients.

Examples of the disintegrant include the same compounds as the above-mentioned excipients and chemically modified starch and cellulose such as croscarmellose sodium, sodium carboxymethyl starch and crosslinked polyvinylpyrrolidone.

As the stabilizer, for example, methyl paraben,
Paraoxybenzoic acid esters such as propylparaben; alcohols such as chlorobutanol, benzyl alcohol and phenylethyl alcohol; benzalkonium chloride; phenols such as phenol and cresol; thimerosal; dehydroacetic acid; and sorbic acid. be able to.

Examples of the flavoring agent include, for example, commonly used sweeteners, sour agents, flavors and the like.

The amount of the compound having the general formula (I) of the present invention, or a pharmaceutically acceptable salt or derivative thereof, varies depending on the condition, age, administration method and the like. 0.1m per day
g (preferably 0.5 mg), with an upper limit of 2000 m
g (preferably 500 mg) is desirably administered once or several times depending on the condition. In the case of intravenous administration, the lower limit is 0.1 per day for adults.
01 mg (preferably 0.05 mg), with an upper limit of 2 mg
It is desirable to administer 00 mg (preferably 50 mg) once or in several divided doses according to the symptoms. Hereinafter, the present invention will be described in more detail with reference to Examples, Reference Examples, Formulation Examples, and Test Examples, but the present invention is not limited thereto.

[0146]

【Example】

[0147]

Example 1 4- (3-aminopropyl) -2- (4
-Fluorophenyl) -3- (pyridin-4-yl)-
1H-pyrrole (Exemplary Compound No. 1-97) 1) 4-ethoxycarbonyl-2- (4-fluorophenyl)
Eniru) -3- (pyrid down-4-yl)-1H-Pillow
Le 1.53N butyllithium / hexane solution 36 ml (5
4.7 mmol) in 240 ml of tetrahydrofuran and then at -45 ° C. 15.90 g of α- (p-toluenesulfonyl) -4-fluorobenzylisonitrile.
(54.7 mmol) in tetrahydrofuran solution 120
ml was added. After stirring at the same temperature for 10 minutes, 25.00 g (273 mmol) of 95% lithium bromide was added, and
Stir for 0 minutes and add 3- (4-pyridyl) acrylic acid
A solution of 8.73 g (49.2 mmol) of ethyl ester in 120 ml of tetrahydrofuran was added. After stirring at the same temperature for 1 hour, the reactor was taken out of the cooling bath and further stirred for 1 hour.
500 ml of water was added, and the mixture was extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The obtained solid was washed with diethyl ether to obtain 13.61 g of the title compound as a pale yellow powder (89% yield).

¹ H-nuclear magnetic resonance spectrum (500 MH
z, CDCl ₃ ) δ ppm: 8.84 (1H, br.s), 8.51 (2
H, d, J = 7Hz), 7.58 (1H, d, J = 3Hz), 7.21 (2H, d, J = 6
Hz), 7.11 (2H, dd, J = 9Hz, 5Hz), 6.97 (2H, t, J = 9H
z), 4.18 (2H, quartet, J = 7Hz), 1.20 (3H, t, J = 7H
z). 2) 2- (4-fluorophenyl) -4-hydroxy
12.56 g of 4-ethoxycarbonyl-2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole obtained in methyl-3- (pyridin -4-yl) -1H-pyrrole 1) (40.47 mmol) was dissolved in 630 ml of tetrahydrofuran, and a 1M diisobutylaluminum hydride / toluene solution 12
1.4 ml (121.4 mmol) was slowly added dropwise. After completion of the dropwise addition, the reactor was taken out of the cooling bath and stirred for 5 hours. After adding a saturated ammonium chloride aqueous solution, the mixture was extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous magnesium sulfate and concentrated under reduced pressure to obtain the title compound (10.80 g) as a pale orange powder (yield: 99%).

¹ H-nuclear magnetic resonance spectrum (500 MH
z, CDCl ₃ ) δ ppm: 10.52 (1H, br.s), 8.46
(2H, d, J = 6Hz), 7.31 (2H, d, J = 6Hz), 7.26 (2H, dd,
J = 9Hz, 5Hz), 6.98 (2H, t, J = 9Hz), 6.95 (1H, d, J = 3
Hz), 4.50 (2H, s), 3.49 (1H, br.s). 3) 2- (4-fluorophenyl) -4-formyl-
3- (pyridin-4-i le)-1H-obtained in pyrrole 2) 2- (4-fluorophenyl) -4-hydroxymethyl-3- (pyridin-4-yl)-1H-pyrrole 10.73 g ( 40 mmol) was dissolved in 120 ml of dimethyl sulfoxide, and manganese dioxide was dissolved in 118.00.
After adding g (440 mmol) and stirring at 50 ° C. overnight, the reaction mixture was filtered, water was added to the filtrate, and the mixture was extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous magnesium sulfate and concentrated under reduced pressure, and the obtained solid was washed with diethyl ether to obtain 7.35 g of the title compound as a brown powder (yield 69%).

¹ H-nuclear magnetic resonance spectrum (500 MH
z, CDCl ₃ -CD ₃ OD) δ ppm: 9.76 (1H, s),
8.48 (2H, d, J = 6Hz), 7.59 (1H, s), 7.26 (2H, d, J =
6Hz), 7.19 (2H, dd, J = 9Hz, 6Hz), 7.01 (2H, t, J = 9H
z). 4) 3-[[2- (4-fluorophenyl) -3-
(Pyridin-4-yl) -1H-pyrrole] -4-i
786 mg of acrylonitrile 55% sodium hydride (18.02 mmol)
l) were suspended in tetrahydrofuran (60 ml) and stirred under ice-cooling with diethyl phosphonoacetonitrile (2.92 ml, 1).
8.02 mmol) in 16 ml of tetrahydrofuran
And stirred at room temperature for 1.5 hours.
4.00 g of (4-fluorophenyl) -4-formyl-3- (pyridin-4-yl) -1H-pyrrole (15.
(02 mmol) in a tetrahydrofuran suspension (30 ml) was added, followed by stirring at room temperature for 1 hour. Water was added to the reaction solution, and the mixture was extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The obtained solid was washed with diethyl ether to give the title compound (2.94 g) as a pale-brown powder (yield 68%).

The ¹ H-nuclear magnetic resonance spectrum (500 MH
_{z, CDCl 3 -DMSO-d 6} ) δppm: 11.30 (1H,
br.s), 8.57 (2H, d, J = 6Hz), 7.24 (1H, d, J = 4Hz),
7.21 (1H, d, J = 17Hz), 7.19 (2H, dd, J = 9Hz, 5Hz),
7.13 (2H, d, J = 6Hz), 6.97 (2H, d, J = 9Hz), 5.39 (1H,
d, J = 17Hz). 5) 4- (2-cyanoethyl) -2- (4-fluoro
Phenyl) -3- (pyrimidin Jin-4-yl)-1H-pyro
Obtained in Lumpur 4) 3 - [[2- (4-fluorophenyl) -3
-(Pyridin-4-yl) -1H-pyrrole] -4-yl] acrylonitrile 2.94 g (10.16 mmol
l) in 20 ml of tetrahydrofuran and 20 m of methanol
and 10% palladium on carbon 2.94
g was added and stirred at room temperature for 8 hours under a hydrogen atmosphere. The reaction mixture was filtered, the filtrate was concentrated under reduced pressure, and the residue was washed with a mixture of 30 ml of diethyl ether and 30 ml of ethanol to obtain 1.80 g of the title compound as a pale orange powder (yield 61%).

The ¹ H-nuclear magnetic resonance spectrum (500 MH
z, CDCl ₃ ) δ ppm: 8.55 (2H, d, J = 6 Hz), 8.2
7 (1H, br.s), 7.13 (2H, dd, J = 9Hz, 5Hz), 7.12 (2H,
d, J = 6Hz), 6.98 (2H, t, J = 9Hz), 6.89 (1H, d, J = 3H
z), 2.88 (2H, t, J = 7Hz), 2.43 (2H, t, J = 7Hz). 6) 4- (3-aminopropyl) -2- (4-fluoro
Rofeniru) -3- (Pi lysine-4-yl)-1H-pin
469 mg of roll lithium aluminum hydride (12.36
mmol) in 150 ml of tetrahydrofuran,
4- (2-cyanoethyl)-obtained in 5) under stirring at room temperature.
2- (4-fluorophenyl) -3- (pyridine-4-
Il) -1H-pyrrole 1.80 g (6.18 mmo
100 ml of tetrahydrofuran solution of 1) was slowly added dropwise, followed by stirring at 60 ° C. for 30 minutes. After cooling to room temperature, water 2
5 ml and 0.5 ml of a 15% aqueous sodium hydroxide solution were gradually added, followed by filtration, and the filtrate was concentrated under reduced pressure. The operation of adding toluene to the residue, concentrating under reduced pressure, and performing azeotropic dehydration was repeated three times to obtain 1.71 g of the title compound as a white powder (yield 94%).

Melting point: 198-199 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.16 (1H, br.s), 8.46 (2H, d, J
= 6Hz), 7.18 (2H, dd, J = 9Hz, 6Hz), 7.13 (2H, d, J = 6H
z), 7.11 (2H, t, J = 9Hz), 6.74 (1H, d, J = 3Hz), 2.49
(2H, t, J = 7Hz), 2.41 (2H, t, J = 8Hz), 1.48 (2H, qui
ntet, J = 8Hz).

[0154]

Example 2 2- (4-fluorophenyl) -3-
(Pyridin-4-yl) -4- (3-trifluoroace
(Tylaminopropyl ) -1H-pyrrole (Exemplary Compound No. 1-2533) 4- (3-aminopropyl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole (Example) 685 mg (2.32 mmol)
Was dissolved in 70 ml of tetrahydrofuran, 3.3 ml (23.2 mmol) of trifluoroacetic anhydride was added, and the mixture was stirred at room temperature for 30 minutes. Then, 200 ml of a saturated aqueous sodium hydrogen carbonate solution was added, and the mixture was extracted with ethyl acetate. The organic layer was washed with water, concentrated under reduced pressure, and subjected to silica gel column chromatography (solvent; hexane: ethyl acetate = 1: 1) to obtain 280 mg of the title compound as a white powder (yield 31%).

Melting point: 229-230 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 10.09 (1H, br.s), 8.49 (2H, d, J = 6H
z), 7.93 (1H, br.s), 7.18 (2H, dd, J = 9Hz, 5Hz), 7.1
3 (2H, d, J = 6Hz), 6.94 (2H, t, J = 9Hz), 6.74 (1H, d,
J = 3Hz), 3.29 (2H, dd, J = 13Hz, 7Hz), 2.56 (2H, t, J
= 8Hz), 1.74 (2H, quintet, J = 8Hz).

[0156]

Example 3 4- (3-acetylaminopropyl)-
2- (4-Furuorofe) -3- (pyridin-4
Yl) -1H-pyrrole (Exemplary Compound No. 1-252)
8) The same reaction as in Example 2 was performed using acetic anhydride instead of trifluoroacetic anhydride to obtain the title compound as a pale yellow powder (yield: 99%).

Melting point: 218-220 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, DMSO
−d ₆ ) δ ppm: 11.19 (1H, br.s), 8.46 (2H, d, J
= 6Hz), 7.77 (1H, br.t, J = 5Hz), 7.18 (2H, dd, J = 9Hz,
5Hz), 7.15-7.08 (4H, m), 6.77 (1H, d, 2Hz), 2.99
(2H, dd, J = 13Hz, 7Hz), 2.39 (2H, t, 8Hz), 1.75 (3
H, s), 1.53 (2H, quintet, J = 7Hz).

[0158]

Example 4 2- (4-fluorophenyl) -4-
(3-methylamino-propyl Le) -3- (pyridin-4
Yl) -1H-pyrrole (Exemplary Compound No. 1-101) 1) 4- [3- (t-butoxycarbonylamino) p
Propyl] -2- (4-off Ruorofeniru) -3- (pyridinium
(Gin-4-yl) -1H-pyrrole Di-tert-butyl dicarbonate was used instead of trifluoroacetic anhydride, and methanol was used instead of tetrahydrofuran to carry out the same reaction as in Example 2 to give the title compound Was obtained as a white powder (yield 68%).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.51 (2H, d, J = 6 Hz), 8.2
6 (1H, br.s), 7.15-7.12 (4H, m), 6.96 (2H, t, J = 9H
z), 6.75 (1H, d, J = 3Hz), 4.45 (1H, br.s), 3.12-3.09
(2H, m), 2.54 (2H, t, J = 8Hz), 1.67-1.63 (2H, m),
1.43 (9H, s). 2) 2- (4-fluorophenyl) -4- (3-methyl
Ruaminopropyl) -3- (pyridin-4-yl) -1
154 mg of H-pyrrole lithium aluminum hydride was suspended in 8 ml of tetrahydrofuran, and the 4- [3-
(T-butoxycarbonylamino) propyl] -2-
400 mg (1.01 mmol) of (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole
After heating under reflux for 2 hours, the same treatment as in Example 1-6) was carried out to obtain 300 mg of the title compound as a white powder (yield: 96%).

Melting point: 193-198 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.51 (2H, d, J = 6Hz), 8.34 (1H, br.
s), 7.17-7.12 (4H, m), 6.96 (2H, t, J = 9Hz), 6.74 (1
H, d, J = 3Hz), 2.57 (2H, t, J = 7Hz), 2.54 (2H, t, J = 7
Hz), 2.38 (3H, s), 1.69 (2H, quintet, J = 7Hz).

[0161]

Example 5 4-aminomethyl-2- (4-fluoro
Phenyl) -3- (pyrimidin Jin-4-yl)-1H-pyro
Lumpur dihydrochloride (Compound No. 1-95 dihydrochloride) 1) 5- (4-Fluorophenyl) -4- (pyridin
4-yl)-1H-pin roll-3-carboxaldehyde aldehyde
Hyd O-methyloxime 2- (4-fluorophenyl) -obtained in Example 1-3)
0.85 g (3.2 mmol) of 4-formyl-3- (pyridin-4-yl) -1H-pyrrole was added to methanol 17
Then, 0.83 g (9.58 mmol) of O-methylhydroxylamine hydrochloride and 1.56 ml (11.2 mmol) of triethylamine were added, and the mixture was heated under reflux for 30 minutes. Water was added, followed by extraction with ethyl acetate. The organic layer was washed with water, concentrated under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent: ethyl acetate) to obtain 728 mg of the title compound as a slightly yellow powder (yield 77).
%).

Melting point: 242-248 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.88 (1H, br.s), 8.54 (0.2H, d,
J = 6Hz), 8.49 (1.8H, d, J = 6Hz), 7.88 (0.9H, s), 7.7
6 (0.1H, s), 7.34 (0.9H, s), 7.25-7.12 (6H, m), 6.9
8 (0.1H, s), 3.92 (0.4H, s), 3.71 (2.6H, s). 2) 4-aminomethyl-2- (4-fluorophenyl )
) -3- (pyridin-4 -yl) -1H-pyrrole
5- (4-Fluorophenyl) -4- (pyridin-4-yl) -1H-pyrrole-3-carboxaldehyde obtained in dihydrochloride 1) 497 mg (1.68 m)
mol) was dissolved in 10 ml of methanol, 10 ml of a 10% aqueous hydrochloric acid solution and 0.50 g of 10% palladium-carbon were added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 2 hours, and then filtered. The filtrate was concentrated under reduced pressure, and the residue was sequentially washed with diisopropyl ether and diethyl ether to give the title compound 39
1 mg was obtained as a yellow-orange powder (68% yield).

Melting point: 235-240 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, CD ₃ O
D) δ ppm: 11.85 (1H, br.s), 8.65 (2H, d, J = 7H
z), 7.81 (2H, d, J = 7Hz), 7.32 (2H, dd, J = 9Hz, 5Hz),
7.24 (1H, d, J = 3Hz), 7.14 (2H, t, J = 9Hz), 4.22 (2
H, s).

[0164]

Example 6 2- (4-fluorophenyl) -3-
(Pyridin-4-yl) -4- (2,4,6-trifur
(Orobenzoylaminomethyl ) -1H-pyrrole (Exemplary Compound No. 1-2535) 4-aminomethyl-2- (4-fluorophenyl) -3
162 mg (0.476 mmol) of-(pyridin-4-yl) -1H-pyrrole dihydrochloride (the compound of Example 5)
l) was suspended in 3.3 ml of tetrahydrofuran, and 265 μl (1.905 mmol) of triethylamine and 2,2 were added.
96 mg of 4,6-trifluorobenzoyl chloride
(0.493 mmol) was added, and the mixture was stirred at room temperature for 4 hours. Then, water was added, and the mixture was extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous sodium sulfate, concentrated under reduced pressure, and the residue was washed with diethyl ether to give the title compound (78 mg) as a pale-yellow powder (yield 38%).

Melting point: 243-245 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.41 (1H, br.s), 8.99 (1H, br.
t, J = 5Hz), 8.46 (2H, d, J = 6Hz), 7.29-7.19 (4H, m),
7.19-7.13 (4H, m), 6.94 (1H, d, J = 3Hz), 4.27 (2H,
d, J = 5Hz).

[0166]

Example 7 2- (4-fluorophenyl) -3-
(Pyridin-4-yl) -4- (2,3,5,6-tet
Lafluoropyridin -4-yl) -1H-pyrrole (Exemplary Compound No. 1-2538) 1) 2- (4-fluorophenyl) -3- (pyridine
4-yl)-1H-4-ethoxycarbonyl obtained in pin roll Example 1-1) -2-
15.00 g of (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole (48.3 mmol)
l) was dissolved in a mixture of 90 ml of acetic acid, 30 ml of sulfuric acid and 60 ml of water and stirred at 100 ° C. for 16 hours. After cooling to room temperature, a 10% aqueous sodium hydroxide solution was added to make the mixture alkaline, and the mixture was extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous sodium sulfate and concentrated under reduced pressure to obtain 11.40 g of the title compound as a slightly red powder (yield: 99%).

¹ H-nuclear magnetic resonance spectrum (500 MH
z, CDCl ₃ ) δ ppm: 9.78 (1H, br.s), 8.42 (2
H, d, J = 7Hz), 7.37 (2H, dd, J = 9Hz, 5Hz), 7.22 (2H,
d, J = 6Hz), 7.06 (2H, t, J = 9Hz), 6.90 (1H, t, J = 3H
z), 6.47 (1H, t, J = 3Hz). 2) 2- (4-fluorophenyl) -3- (pyridine
-4-yl) -1- triisopropylsilyl-1H-pi
11.30 g of 2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole obtained in Roll 1) (4
7.4 mmol) was dissolved in 300 ml of tetrahydrofuran, 31 ml (47.4 mmol) of a 1.57N butyllithium / hexane solution was added at −78 ° C., and the mixture was stirred for 10 minutes. At the same temperature, 13.4 ml of triisopropylsilyl triflate ( 49.8 mmol) was added. Further, the reactor was removed from the cooling bath and stirred at room temperature for 30 minutes. 200 ml of water and 300 ml of a saturated aqueous solution of sodium hydrogen carbonate were added to the reaction solution, and the mixture was extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous sodium sulfate and concentrated under reduced pressure to give 18.70 g of the title compound as a red-purple oil. Obtained (yield: quantitative).

¹ H-nuclear magnetic resonance spectrum (500 MH
z, DMSO-d ₆ ) δ ppm: 8.25 (2H, d, J = 6 Hz),
7.39 (2H, dd, J = 9Hz, 6Hz), 7.28 (2H, t, J = 9Hz), 7.
00 (1H, d, J = 3Hz), 6.91 (2H, d, J = 7Hz), 6.71 (1H,
d, J = 3Hz), 1.15-1.05 (3H, m), 0.98 (18H, d, J = 8H
z). 3) 4-bromo-2- (4-fluorophenyl) -3
-(Pyridin-4-yl ) -1-triisopropylsilyl
2- (4-Fluorophenyl) -3- (pyridin-4-yl) -1-triisopropylsilyl-1H obtained from 1H-pyrrole 2)
Dissolve 18.70 g (47.4 mmol) of pyrrole in 300 ml of tetrahydrofuran, gradually add a suspension of 8.61 g (47.4 mmol) of N-bromosuccinimide in 100 ml of tetrahydrofuran at -78 ° C, After stirring for 1 hour, the reactor was taken out of the cooling bath, and stirred for 1 hour at room temperature. The filtrate was concentrated under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent; hexane: ethyl acetate = 2: 1) to obtain 9.57 g of the title compound as pale yellow prism-like crystals (yield 43%).

The ¹ H-nuclear magnetic resonance spectrum (500 MH
z, DMSO-d ₆ ) δ ppm: 8.36 (2H, d, J = 6 Hz),
7.34 (2H, dd, J = 9Hz, 6Hz), 7.18 (2H, t, J = 9Hz), 7.
12 (1H, s), 7.04 (2H, d, J = 6Hz), 1.16-1.08 (3H, m),
0.99 (18H, d, J = 8Hz). 4) 2- (4-fluorophenyl) -3- (pyridine
-4-yl) -4- ( 2,3,5,6-tetrafluoro
4-bromo-2- (4-fluorophenyl) obtained by pyridin-4-yl) -1H-pyrrole 3)
650 mg (1.37 mmol of 3- (pyridin-4-yl) -1-triisopropylsilyl-1H-pyrrole
l) was dissolved in 15 ml of tetrahydrofuran,
1.54Nt-butyllithium / pentane solution 1.8
After stirring for 10 minutes, 165 μl (1.51 mmol) of pentafluoropyridine was added.
Was added and the reactor was removed from the cooling bath and stirred for 30 minutes.
70 ml of water and 50 ml of saturated sodium bicarbonate are added to the reaction solution.
And extracted with ethyl acetate. The organic layer was washed with water, concentrated under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent; hexane: ethyl acetate = 4: 1) to give the title compound (346 mg) as pale yellow. Powder (yield 6
5%).

Melting point:> 300 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CD ₃ O
D) δppm: 8.34 (2H, d, J = 8Hz), 7.32 (1H, s),
7.30 (2H, dd, J = 11Hz, 7Hz), 7.09 (2H, t, J = 11Hz),
7.06 (2H, d, J = 8Hz).

[0171]

Example 8 (±)-[5- (4-fluorophenyl)
) -4- (pyridin-4 -yl) -1H-pyrrole-
3-yl]-(pyridin-4-yl) methanol (Exemplary Compound No. 1-2530) 1) (±)-[5- (4-fluorophenyl) -4-
(Pyridin-4-yl) -1-triisopropylsilyl
-1H-pyrrol-3-yl]-(pyridin-4 -i
G) methanol (compound of the following structural formula)

[0172]

Embedded image The reaction was carried out in the same manner as in Example 7-4) using 4-formylpyridine instead of pentafluoropyridine, and the title compound was obtained as a pale yellow oil (yield: 56%).

The ¹ H-nuclear magnetic resonance spectrum (500 MH
z, CD ₃ OD) δ ppm: 8.39 (2H, d, J = 7 Hz), 8.21
(2H, d, J = 6Hz), 7.38 (2H, d, J = 7Hz), 7.29 (2H, dd,
J = 9Hz, 6Hz), 7.17 (2H, d, J = 6Hz), 7.03 (2H, t, J = 9
Hz), 6.67 (1H, s), 5.82 (1H, s), 1.14-1.05 (3H, m),
1.01 (9H, d, J = 7Hz), 1.00 (9H, d, J = 7Hz). 2) (±)-[5- (4-fluorophenyl) -4-
(Pyridin-4-yl) -1H-pyrrol-3-yl]
[5- (4-Fluorophenyl) -4- (pyridin-4-yl) -1-triisopropylsilyl-1 obtained in-(pyridin-4-yl) methanol 1)
148 mg (0.295 mmol) of [H-pyrrol-3-yl]-(pyridin-4-yl) methanol is dissolved in 3 ml of tetrahydrofuran, and 0.59 ml of a 1 M tetrabutylammonium fluoride / tetrahydrofuran solution is dissolved.
(0.59 mmol) and the mixture was stirred at room temperature for 10 minutes. Water was added to the reaction solution, and the mixture was acidified with a 1N aqueous hydrochloric acid solution and extracted with ethyl acetate. The aqueous layer was made alkaline with potassium carbonate and extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous sodium sulfate and concentrated under reduced pressure, and solidified by adding isopropanol to the oily residue to obtain 83 mg of the title compound as a white powder (yield: 82%).

Melting point: 202-205 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.39 (1H, br.s), 8.43 (2H, d, J
= 6Hz), 8.41 (2H, d, J = 6Hz), 7.26-7.21 (4H, m), 7.18
(2H, dd, J = 9Hz, 6Hz), 7.13 (2H, t, J = 9Hz), 6.55 (1
H, d, J = 3Hz), 5.77 (1H, d, J = 5Hz), 5.54 (1H, d, J =
4Hz).

[0175]

Example 9 4- (1-acetyl-1,2,3,6-
Tetrahydropyridin- 4-yl) -2- (4-fluoro
L-phenyl) -3- (pyridin-4-yl) -1H -pi
Roll (Exemplified Compound No. 1-2525) 1) 4- (1-benzyl-4-hydroxypiperidine )
-4-yl) -2- (4 -fluorophenyl) -3-
(Pyridin-4-yl) -1-triisopropyl silyl
The reaction was carried out in the same manner as in Example 7-4) using 1-benzylpiperidin-4-one instead of -1H-pyrrolepentafluoropyridine , and the title compound was obtained as white needle crystals (yield 61%). ).

¹ H-nuclear magnetic resonance spectrum (500 MH
z, CD ₃ OD) δ ppm: 8.21 (2H, d, J = 6 Hz), 7.35
-7.15 (9H, m), 6.93 (2H, t, J = 9Hz), 6.90 (1H, s),
3.49 (2H, s), 2.58-2.41 (4H, br.m), 2.00-1.91 (2H,
br.m), 1.83-1.74 (2H, br.m), 1.20-1.10 (3H, m), 1.0
6 (18H, d, J = 7Hz). 2) 2- (4-fluorophenyl) -4- (4-hydrido
Roxypiperidin-4- yl) -3- (pyridine-4-
Yl) -1-triisopropylsilyl -1H- pin roll 1) 4- (1-benzyl-4-hydroxy-pyridin-yl) -2- (4-fluorophenyl) -3-
0.58 g (1.00 mmol) of (pyridin-4-yl) -1-triisopropylsilyl-1H-pyrrole was dissolved in 15 ml of methanol, and 0.58 g of 10% palladium-carbon was added. Stirred for hours. The reaction solution was filtered, and the filtrate was concentrated under reduced pressure to obtain 483 mg of the title compound as a white amorphous solid (yield 98).
%).

The ¹ H-nuclear magnetic resonance spectrum (500 MH
z, CD ₃ OD) δ ppm: 8.22 (2H, d, J = 7 Hz), 7.27
(2H, d, J = 6Hz), 7.21 (2H, dd, J = 9Hz, 6Hz), 6.94 (2
(H, t, J = 9Hz), 6.92 (1H, s), 2.98-2.90 (2H, m), 2.76
-2.68 (2H, m), 1.93-1.84 (2H, m), 1.77-1.69 (2H, m
m), 1.20-1.11 (3H, m), 1.07 (18H, d, J = 7Hz). . 3) 4- (1-Acetyl-1,2,3,6-tetrahi
Dropyridin-4-yl ) -2- (4-fluorophenyl
Le) -3- (pyridin-4-yl)-1H-pyro chromatography to give Le 2) 2- (4-fluorophenyl) -4- (4-
(Hydroxypiperidin-4-yl) -3- (pyridine-
3.58 g (7.25 mmol) of 4-yl) -1-triisopropylsilyl-1H-pyrrole was dissolved in 40 ml of dichloromethane, and 1.4 ml of triethylsilane (8.
70 mmol) and 2.25 ml of trifluoroacetic acid (2
9.0 mmol), and the mixture was stirred at room temperature for 5 hours. Then, a saturated aqueous sodium hydrogen carbonate solution was added, and the mixture was extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous sodium sulfate and concentrated under reduced pressure to obtain 3.90 g of a dehydrated product as a yellow amorphous solid.

Next, the whole amount was dissolved in 80 ml of tetrahydrofuran, and 0.76 ml of acetic anhydride (8.0 mm
ol) and 2.25 ml of triethylamine (16.0 mm
ol) and stirred at room temperature for 20 minutes, followed by 1M tetrabutylammonium fluoride / tetrahydrofuran solution 1
6 ml (16.0 mmol) was added and stirred for 10 minutes. 150 ml of saturated aqueous sodium hydrogen carbonate solution
And extracted with ethyl acetate. The organic layer was washed with water, 1N hydrochloric acid aqueous solution was added, and the mixture was separated to collect an aqueous layer. The aqueous layer was washed with ethyl acetate, made alkaline with potassium carbonate, and extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous sodium sulfate and concentrated under reduced pressure to give the title compound (1.78 g).
Was obtained as a slightly brown powder (yield 68%).

Melting point: 262-264 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.43 (1H, br.s), 8.48-8.44 (2H,
m), 7.20-7.09 (6H, m), 6.96 (0.5H, d, J = 3Hz), 6.94
(0.5H, d, J = 3Hz), 5.32-5.29 (0.5H, br.m), 5.29-5.2
5 (0.5H, br.m), 3.92-3.88 (1H, m), 3.87-3.84 (1H,
m), 3.50 (1H, t, J = 6Hz), 3.46 (1H, t, J = 6Hz), 2.22-
2.17 (1H, br.m), 2.16-2.11 (1H, br.m), 2.00 (1.5H, br.m)
s), 1.96 (1.5H, s).

[0180]

Example 10 2- (4-fluorophenyl) -3-
(Pyridin-4-yl) -4- (1,2,3,6-tet
Lahydropyridin-4-yl) -1H-pyrrole dihydrochloride
Salt (Exemplary Compound No. 1-143 dihydrochloride) 4- (1-acetyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl)-
249 mg (0.689 mmol) of 3- (pyridin-4-yl) -1H-pyrrole (the compound of Example 9) was dissolved in a mixture of 2.5 ml of methanol and 2.5 ml of water, and a 4N hydrogen chloride / dioxane solution was used. 2.43 ml (9.
646 mmol), and the mixture was heated under reflux for 11 hours, concentrated under reduced pressure, and the residual solid was washed with hot isopropanol to obtain 216 mg of the title compound as a pale yellow powder (80% yield).

Melting point: 290-295 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, CD ₃ O
D) δ ppm: 11.63 (1H, br.s), 8.54 (2H, d, J = 7H
z), 7.74 (2H, d, J = 7Hz), 7.29 (2H, dd, J = 9Hz, 5Hz),
7.14 (2H, t, J = 9Hz), 7.06 (1H, d, J = 2Hz), 5.51-5.4
7 (1H, br.m), 3.72 (2H, d, J = 3Hz), 3.42 (2H, t, J = 6
Hz), 2.66-2.55 (2H, br.m).

[0182]

Example 11 2- (4-fluorophenyl) -4-
(Piperidin-4-yl ) -3- (pyridine-4-i
1) -H -pyrrole (Exemplified Compound No. 1-142) 2- (4-fluorophenyl) -3- (pyridine-4-
Yl) -4- (1,2,3,6-tetrahydropyridin-4-yl) -1H-pyrrole dihydrochloride (Example 10
120 mg (0.306 mmol) was dissolved in 10 ml of methanol, and 10% palladium-carbon 120
After stirring for 1 hour at room temperature under a hydrogen atmosphere,
Filtered. The filtrate was concentrated under reduced pressure and water was added to the residue.
Add 1N aqueous sodium hydroxide to make it alkaline,
The deposited precipitate was collected by filtration to give the title compound (84 mg) as a slightly red powder (yield: 85%).

Melting point: 265-267 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.17 (1H, br.s), 8.48 (2H, d, J
= 6Hz), 7.20-7.04 (6H, m), 6.73 (1H, d, J = 3Hz), 2.88
(2H, d, J = 12Hz), 2.46 (1H, tt, J = 12Hz, 4Hz), 2.38
(2H, t, J = 12Hz), 1.58 (2H, d, J = 13Hz), 1.35 (2H, dd
t, J = 13Hz, 12Hz, 4Hz).

[0184]

Example 12 1- (1-benzylpiperidine-4-
Yl) -3- (4-full Orofeniru) -2- (pyrid
N-4-yl) -1H-pyrrole (Exemplified Compound No. 2-
147) 1) 1-benzyl-4- (pyridin-4-yl) methyl
Lenaminopiperidine (compound of the following structural formula)

[0185]

Embedded image 3.95 ml of 4-formylpyridine (42.01 mmol
l) was dissolved in 5 ml of ethanol, and 8.57 ml (42.01 mmol) of 4-amino-1-benzylpiperidine was dissolved.
After heating under reflux for 1 hour, the solvent was distilled off under reduced pressure to obtain 11.78 g of the title compound as a pale brown powder (yield: quantitative).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.68 (2H, d, J = 6 Hz), 8.3
0 (1H, s), 7.60 (2H, d, J = 6Hz), 7.38-7.22 (5H, m),
3.56 (2H, s), 3.37-3.27 (1H, m), 3.00-2.90 (2H, m),
2.23-2.10 (2H, m), 1.96-1.83 (2H, m), 1.79-1.60 (2
H, m). 2) (±) -α- (1-benzylpiperidine-4-i
) Amino-.alpha.-(pyridinium Jin-4-yl) acetonitrile
1-benzyl-4 was obtained by Le 1) (pyridin-4-yl)
11.73 g of methyleneaminopiperidine (42.00 m
mol) and 95% trimethylsilyl cyanide 9.22m
1 (65.67 mmol), stirred at 100 ° C. for 3 hours, and then cooled to room temperature. 100 ml of methanol was added to the reaction solution, and the mixture was stirred for 30 minutes. The solvent was distilled off under reduced pressure to obtain 12.87 g of the title compound as a brown oil (yield: quantitative).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.67 (2H, d, J = 6 Hz), 7.5
0 (2H, d, J = 6Hz), 7.37-7.22 (5H, m), 4.85 (1H, s),
3.53 (2H, s), 2.98-2.77 (4H, m), 2.33-1.44 (5H,
m). 3) 1- (1-benzylpiperidin-4-yl) -3
- (4-fluoro-phenylcarbamoyl) -2- (pyridin-4-y
Α)-(1-benzylpiperidin-4-yl) obtained in 1 ) -H-pyrrole 2)
Amino-α- (pyridin-4-yl) acetonitrile 1
4.25 g (46.51 mmol) and 6.98 g of 3- (4-fluorophenyl) acrolein (46.51 m
mol) was dissolved in 145 ml of N, N-dimethylacetamide, and 1.29 g (9.30 mmol) of potassium carbonate was dissolved.
Was added and stirred at room temperature for 5 hours. Water was added to the reaction solution, and the mixture was extracted with ethyl acetate. The organic layer was washed with water and concentrated under reduced pressure. 150 ml of ethylene glycol was added to the residue, and the mixture was stirred at 180 ° C. for 1 hour. After cooling to room temperature, a saturated aqueous sodium hydrogen carbonate solution was added, and the mixture was extracted with ethyl acetate. The organic layer is washed with water, concentrated under reduced pressure, and the residue is subjected to silica gel column chromatography (solvent; hexane: ethyl acetate = 1: 3).
To give 10.31 g of the title compound as a pale brown powder (yield 49%).

Melting point: 132-139 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.61 (2H, d, J = 6Hz), 7.37-7.23 (5H,
m), 7.13 (2H, d, J = 6Hz), 7.03 (2H, dd, J = 9Hz, 5Hz),
6.96 (1H, d, J = 3Hz), 6.87 (2H, t, J = 9Hz), 6.38 (1
(H, d, J = 3Hz), 3.87-3.80 (1H, m), 3.50 (2H, s), 2.97
(2H, d, J = 12Hz), 2.12-1.56 (6H, m).

[0189]

Example 13 3- (4-fluorophenyl) -1-
(Piperidin-4-yl ) -2- (pyridine-4-i
1) -H -pyrrole (Exemplified Compound No. 2-142) 1- (1-benzylpiperidin-4-yl) -3- (4
-Fluorophenyl) -2- (pyridin-4-yl)-
A debenzylation reaction was carried out using 1H-pyrrole (the compound of Example 12) in the same manner as in Example 9-2) to obtain the title compound as a white powder (yield 30%).

Melting point: 191 ° -192 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.62 (2H, d, J = 6Hz), 7.15 (2H, d, J =
6Hz), 7.04 (2H, dd, J = 9Hz, 5Hz), 6.97 (1H, d, J = 3H
z), 6.88 (2H, t, J = 9Hz), 6.39 (1H, d, J = 3Hz), 3.97-
3.86 (1H, m), 3.17 (2H, d, J = 12Hz), 2.58 (2H, dt,
J = 12Hz, 3Hz), 1.98-1.82 (4H, m).

[0191]

Example 14 3- (4-fluorophenyl) -1-
(1-methylpiperidin -4-yl) -2- (pyridine
-4-yl) -1H-pyrrole (exemplary compound number 2-1)
44) 3- (4-Fluorophenyl) -1- (piperidine-4
-Yl) -2- (pyridin-4-yl) -1H-pyrrole (compound of Example 13) and N- (t-butoxycarbonyl) ation reaction in the same manner as in Examples 4-1) and 2). The reduction reaction was performed to obtain the title compound as a white powder (total yield of two steps: 55%).

Melting point: 187-189 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.62 (2H, d, J = 6Hz), 7.14 (2H, d, J =
6Hz), 7.04 (2H, dd, J = 9Hz, 5Hz), 6.96 (1H, d, J = 3H
z), 6.87 (2H, t, J = 9Hz), 6.39 (1H, d, J = 3Hz), 3.87-
3.77 (1H, m), 2.93 (2H, d, J = 12Hz), 2.29 (3H, s),
2.13-1.85 (6H, m).

[0193]

Example 15 1- (1-acetylpiperidine-4-
Yl) -3- (4-full Orofeniru) -2- (pyrid
N-4-yl) -1H-pyrrole (Exemplified Compound No. 2-
2524) 3- (4-Fluorophenyl) -1- (piperidine-4
The same reaction as in Example 3 was carried out using -yl) -2- (pyridin-4-yl) -1H-pyrrole (the compound of Example 13) to obtain the title compound as a white powder (yield 98). %).

Melting point: 223-224 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.64 (2H, d, J = 6Hz), 7.15 (2H, d, J =
6Hz), 7.04 (2H, dd, J = 9Hz, 5Hz), 6.88 (2H, t, J = 9H
z), 6.87 (1H, d, J = 3Hz), 6.41 (1H, d, J = 3Hz), 4.84
4.74 (1H, m), 4.05 (1H, dt, J = 12Hz, 4Hz), 3.95-3.8
3 (1H, m), 3.08-2.97 (1H, m), 2.58-2.48 (1H, m), 2.
13 (3H, s), 2.04-1.78 (4H, m).

[0195]

Example 16 3- (4-fluorophenyl) -1-
[1- (2-Nitoroechi Le) piperidin-4-yl] -
2- (pyridin-4-yl) -1H-pyrrole (Exemplary Compound No. 2-2537) 3- (4-fluorophenyl) -1- (piperidine-4
-Yl) -2- (pyridin-4-yl) -1H-pyrrole (compound of Example 13) 300 mg (0.93 mmol)
l) was dissolved in 6 ml of ethanol, 186 mg (1.40 mmol) of acetic acid 2-nitroethyl ester was added, the mixture was stirred at room temperature for 30 minutes, and the solvent was distilled off under reduced pressure. A saturated aqueous sodium hydrogen carbonate solution was added to the residue, and the mixture was extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The obtained solid was washed with diethyl ether to obtain 280 mg of the title compound as a white powder (yield: 76%).

Melting point: 172-173 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.61 (2H, d, J = 6Hz), 7.13 (2H, d, J =
6Hz), 7.04 (2H, dd, J = 9Hz, 5Hz), 6.93 (1H, d, J = 3H
z), 6.87 (2H, t, J = 9Hz), 6.39 (1H, d, J = 3Hz), 4.47
(2H, t, J = 6Hz), 3.82 (1H, dt, J = 12Hz, 4Hz), 3.03-
2.92 (4H, m), 2.16-1.85 (6H, m).

[0197]

Example 17 3- (4-fluorophenyl) -1-
[3- (morpholin-1 -yl) propyl] -2- (pi
Lysin-4-yl) -1H-pyrrole (Exemplified Compound No. 2-125) In place of 4-amino-1-benzylpiperidine, 1-
The same reaction as in Examples 12-1), 2) and 3) was successively carried out using (3-aminopropyl) morpholine as a starting material to obtain the title compound as slightly brown needle-like crystals (total yield: 13). %).

Melting point: 111-112 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.59 (2H, d, J = 6Hz), 7.18 (2H, d, J =
6Hz), 7.06 (2H, dd, J = 9Hz, 5Hz), 6.89 (2H, t, J = 9H
z), 6.84 (1H, d, J = 3Hz), 6.34 (1H, d, J = 3Hz), 3.96
(2H, t, J = 7Hz), 3.64 (2H, t, J = 5Hz), 2.33-2.22 (4
H, m), 2.20 (2H, t, J = 7Hz), 1.72 (2H, quintet, J = 7H
z).

[0199]

Example 18 (±) -3- (4-fluorophenyl)
-)- 2- (pyridin-4 -yl) -1- (pyrrolidine
-3-yl) -1H-pyrrole (exemplary compound number 2-1)
39) 1) (±) -1- [1- (t-butoxycarbonyl)
Pyrrolidin-3-yl] -3- (4-fluorophenyl
) -2- (pyridin-4-yl)-1H-place of (± of pyrrole 4-amino-1-benzylpiperidine)
Using -3-amino-1- (t-butoxycarbonyl) pyrrolidine as a starting material, the same reaction as in Examples 12-1), 2) and 3) was carried out sequentially to give the title compound as a brown amorphous solid. (Total yield 31%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.63 (2H, d, J = 6 Hz), 7.1
7 (2H, d, J = 6Hz), 7.03 (2H, dd, J = 9Hz, 5Hz), 6.93
6.84 (3H, m), 6.41 (1H, d, J = 3Hz), 4.70-4.55 (1H,
m), 3.80-3.36 (4H, m), 2.30-2.12 (2H, m), 1.47 (9H,
s). 2) (±) -3- (4-fluorophenyl) -2-
(Pyridin-4-yl) -1- 1- (pyrrolidin-3-i
) -1H-pyrrole (±) -1- [1- (t-butoxycarbonyl) pyrrolidin-3-yl] -3- (4-fluorophenyl) -2- (pyridin-4-yl) obtained in 1). 1.) 1.96 g (4.81 mmol) of 1H-pyrrole in 10 ml of ethanol
And 4N-hydrogen chloride / dioxane solution 6.01 m
1 (24.05 mmol) was added and stirred at 50 ° C. for 30 minutes. The solvent was distilled off under reduced pressure, a saturated aqueous sodium hydrogen carbonate solution was added to the residue, and the mixture was extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure to obtain 1.29 g of the title compound as a pale yellow powder (yield: 8).
7%).

Melting point: 145 ° -147 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.61 (2H, d, J = 6Hz), 7.16 (2H, d, J =
6Hz), 7.05 (2H, dd, J = 9Hz, 5Hz), 7.00 (1H, d, J = 3H
z), 6.88 (2H, t, J = 9Hz), 6.39 (1H, d, J = 3Hz), 4.61-
4.53 (1H, m), 3.30-3.17 (2H, m), 3.10-2.97 (2H,
m), 2.28-2.18 (2H, m), 2.11-2.01 (2H, m).

[0202]

Example 19 (±) -3- (4-Fluorophenyl)
Ru) -1- (piperidin- 3-yl) -2- (pyridine
-4-yl) -1H-pyrrole (exemplary compound number 2-1)
41) (±) -3-amino-1- (t-butoxycarbonyl)
Instead of pyrrolidine, (±) -3-amino-1- (t-
The same reaction as in Examples 18-1) and 2) was successively performed using butoxycarbonyl) piperidine as a starting material to obtain the title compound as a white powder (total yield: 21).
%).

Melting point: 189-191 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.61 (2H, d, J = 6Hz), 7.15 (2H, d, J =
6Hz), 7.04 (2H, dd, J = 9Hz, 5Hz), 6.93 (1H, d, J = 3H
z), 6.87 (2H, t, J = 9Hz), 6.38 (1H, d, J = 3Hz), 3.93
(1H, tt, J = 11Hz, 4Hz), 3.20-3.12 (1H, m), 3.05-2.9
6 (1H, m), 2.83 (1H, t, J = 11Hz), 2.58 (1H, dt, J = 12
Hz, 3Hz), 2.17-2.08 (1H, m), 1.90-1.76 (2H, m), 1.5
8-1.43 (1H, m).

[0204]

Example 20 3- (4-fluorophenyl) -1-
(Piperidin-4-yl ) methyl-2- (pyridine-4
-Yl) -1H-pyrrole (Exemplary Compound No. 2-16)
9) Example 1 using 4-aminomethyl-1- (t-butoxycarbonyl) piperidine as a starting material instead of 3-amino-1- (t-butoxycarbonyl) pyrrolidine
The same reaction as in 8-1) and 2) was sequentially performed to obtain the title compound as a white powder (total yield: 4%).

Melting point: 174-176 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.59 (2H, d, J = 6Hz), 7.15 (2H, d, J =
6Hz), 7.06 (2H, dd, J = 9Hz, 5Hz), 6.88 (2H, t, J = 9H
z), 6.79 (1H, d, J = 3Hz), 6.34 (1H, d, J = 3Hz), 3.75
(2H, d, J = 7Hz), 3.05-2.95 (2H, m), 2.45 (2H, dt, J
= 12Hz, 2Hz), 1.62-1.52 (1H, m), 1.46-1.38 (2H, m),
1.05-0.93 (2H, m).

[0206]

Example 21 1- (azetidin-3-yl) -3-
(4-Fluorophenyl ) -2- (pyridine-4-i
1) -H-pyrrole dihydrochloride (Exemplified Compound No. 2-
136 dihydrochloride) 1) 1- (1-diphenylmethylazetidine-3-i)
Le) -3- (4-fluoride Rofeniru) -2- (pyridine
-4-yl) -1H-pyrrole As in Examples 12-1), 2) and 3) using 3-amino-1-diphenylmethylazetidine as a starting material instead of 4-amino-1-benzylpiperidine Were sequentially performed to obtain the title compound as a pale brown powder (total yield: 20%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.56 (2H, d, J = 6 Hz), 7.4
3-7.18 (11H, m), 7.07-7.02 (4H, m), 6.88 (2H, t, J =
9Hz), 6.43 (1H, d, J = 3Hz), 4.74-4.66 (1H, m), 4.41
(1H, s), 3.58-3.52 (2H, m), 3.34-3.28 (2H, m). 2) 1- (azetidin-3-yl) -3- (4-fur
(Orophenyl) -2- ( pyridin-4-yl) -1H-
1- (1-Diphenylmethylazetidine-3) obtained from pyrrole dihydrochloride 1)
-Yl) -3- (4-fluorophenyl) -2- (pyridin-4-yl) -1H-pyrrole 1.20 g (2.6
1 mmol) in ethanol 12 ml, concentrated hydrochloric acid 0.45 ml and 20% palladium hydroxide-carbon 0.1%.
2 g was added and the mixture was stirred at 50 ° C. for 20 hours under a hydrogen atmosphere.
After cooling to room temperature, the mixture was filtered, the filtrate was concentrated under reduced pressure, and the obtained solid was washed with diethyl ether to obtain 0.91 g of the title compound as a pale yellow amorphous solid (yield 95).
%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, DMSO-d ₆ ) δ ppm: 9.84-9.64 (1H, br.
s), 9.58-9.37 (1H, br.s), 9.80 (2H, d, J = 6Hz), 7.94
(1H, d, J = 3Hz), 7.64 (2H, d, J = 6Hz), 7.25 (2H, t,
J = 9Hz), 7.20-7.07 (4H, m), 7.62 (1H, d, J = 3Hz), 5.
19-5.08 (1H, m), 4.43-4.23 (4H, m).

[0209]

Example 22 1- (3-aminopropyl) -3-
(4-fluorophenyl) -2- (pyridine-4-i
1) -H -pyrrole (Exemplified Compound No. 2-97) 1) 1- (3-benzyloxypropyl) -3- (4
-Fluorophenyl) -2- (pyridin-4-yl)-
The same reaction as in Examples 12-1), 2) and 3) was sequentially performed using 3-benzyloxypropylamine as a starting material instead of 1H-pyrrole 4-amino-1-benzylpiperidine, to give the title compound. Obtained as a brown oil (total yield 3
4%).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.55 (2H, d, J = 6 Hz), 7.3
8-7.23 (5H, m), 7.16 (2H, d, J = 6Hz), 7.07 (2H, dd,
J = 9Hz, 5Hz), 6.89 (2H, t, J = 9Hz), 6.81 (1H, d, J = 3
Hz), 6.34 (1H, d, J = 3Hz), 4.41 (2H, s), 4.03 (2H,
t, J = 7Hz), 3.36 (2H, t, J = 7Hz), 1.86 (2H, quintet,
J = 7Hz). 2) 3- (4-fluorophenyl) -1- (3-hydrido
Roxypropyl) -2- (pyridin-4-yl) -1H
-1- (3-benzyloxypropyl) -3- obtained in pyrrole 1)
A debenzylation reaction was carried out in the same manner as in Example 9-2) using (4-fluorophenyl) -2- (pyridin-4-yl) -1H-pyrrole to obtain the title compound as a white powder. Rate 55%).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.59 (2H, d, J = 6 Hz), 7.1
9 (2H, d, J = 6Hz), 7.05 (2H, dd, J = 9Hz, 5Hz), 6.89
(2H, t, J = 9Hz), 6.87 (1H, d, J = 3Hz), 6.36 (1H, d,
J = 3Hz), 4.05 (2H, t, J = 7Hz), 3.55 (2H, t, J = 7Hz),
1.80 (2H, quintet, J = 7Hz). 3) 3- (4-fluorophenyl) -2- (pyridine
-4-yl) -1- [3- (p-toluenesulfonylthio )
Xy) propyl] -1H-pyrrole 3- (4-fluorophenyl) -1- (3-
(Hydroxypropyl) -2- (pyridin-4-yl)-
1.64 g (5.53 mmol) of 1H-pyrrole was dissolved in 16 ml of dichloromethane, 1.99 g (6.09 mmol) of p-toluenesulfonic anhydride and 0.85 ml (6.09 mmol) of triethylamine were added, and the mixture was added at room temperature for 2 hours. Stirred. The solvent was distilled off under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent; hexane: ethyl acetate = 1: 1) to obtain 1.33 g of the title compound as a yellow powder (yield 53%).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.57 (2H, d, J = 6 Hz), 7.7
4 (2H, d, J = 8Hz), 7.35 (2H, d, J = 8Hz), 7.10 (2H, d,
J = 6Hz), 7.03 (2H, dd, J = 9Hz, 5Hz), 6.88 (2H, t, J
= 9Hz), 6.71 (1H, d, J = 3Hz), 6.29 (1H, d, J = 3Hz), 3.
98 (2H, t, J = 7Hz), 3.89 (2H, t, J = 7Hz), 2.46 (3H,
s), 1.84 (2H, quintet, J = 7Hz). 4) 1- (3-azidopropyl) -3- (4-fluoro
Rofeniru) -2- (Pi lysine-4-yl)-1H-pin
1.33 g of 3- (4-fluorophenyl) -2- (pyridin-4-yl) -1- [3- (p-toluenesulfonyloxy) propyl] -1H-pyrrole obtained in roll 3)
(2.95 mmol) in 13 ml of dimethyl sulfoxide
And dissolved in sodium azide 0.38 g (5.90 mm
ol) and stirred at 70 ° C. for 1 hour. Water was added to the reaction solution, and the mixture was extracted with dichloromethane. The organic layer was washed with water, concentrated under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent; hexane: ethyl acetate = 1: 1) to give 100 mg of the title compound as pale Obtained as a brown powder (yield 11
%).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.16 (2H, d, J = 6 Hz), 7.1
7 (2H, d, J = 6Hz), 7.07 (2H, dd, J = 9Hz, 5Hz), 6.89
(2H, t, J = 9Hz), 6.83 (1H, d, J = 3Hz), 6.37 (1H, d,
J = 3Hz), 4.00 (2H, t, J = 7Hz), 3.18 (2H, t, J = 7Hz),
1.78 (2H, quintet, J = 7Hz). 5) 1- (3-aminopropyl) -3- (4-fluoro
Rofeniru) -2- (Pi lysine-4-yl)-1H-pin
1- (3-azidopropyl) -3- (4-fluorophenyl) -2- (pyridin-4-yl) -1H obtained in roll 4)
-100 mg (0.31 mmol) of pyrrole was dissolved in 2 ml of ethanol, 20 mg of 10% palladium-carbon was added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 1 hour. The reaction solution was filtered, and the filtrate was concentrated under reduced pressure, and the obtained solid was washed with diethyl ether to give the title compound (43 mg) as a pale-yellow powder (yield 47%).

Melting point: 219-222 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.61 (2H, d, J = 6Hz), 7.74-7.40 (2H,
br.s), 7.27 (2H, d, J = 6Hz), 7.12-7.00 (5H, m), 6.38
(1H, d, J = 3Hz), 3.97 (2H, t, J = 7Hz), 2.60 (2H, t,
J = 7Hz), 1.73 (2H, quintet, J = 7Hz).

[0215]

Example 23 2- (4-fluorophenyl) -3-
(Pyridin-4-yl) -4- [3- (thiomorpholine
-1-yl) propyl] -1H-pyrrole (Exemplified Compound No. 1-129) 1) 3-[[2- (4-fluorophenyl) -3-
(Pyridin-4-yl) -1H-pyrrole] -4-i
L] Acrylic acid ethyl ester The same reaction as in Example 1-4) was performed using diethylphosphonoacetate ethyl ester instead of diethylphosphonoacetonitrile to obtain the title compound as a brown powder (yield: 60%). .

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.64 (1H, br.s), 8.56 (2
H, d, J = 6Hz), 7.54 (1H, d, J = 16Hz), 7.16 (2H, d, J =
6Hz), 7.16-7.13 (3H, m), 6.99 (2H, t, J = 9Hz), 6.07
(1H, d, J = 16Hz), 4.20 (2H, quartet, J = 7Hz), 1.28
(3H, t, J = 7Hz). 2) 4- (2-ethoxycarbonylethyl) -2-
(4-Fluorophenyl) -3- (pyridine-4-i
3-[[2- (4-fluorophenyl) -3] obtained in 1 ) 1H-pyrrole.
Example 1 using-(pyridin-4-yl) -1H-pyrrole] -4-yl] acrylic acid ethyl ester
A reduction reaction was carried out in the same manner as in 5) to give the title compound as a pale-brown powder (yield 73%).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.51 (2H, d, J = 4 Hz), 8.3
3 (1H, br.s), 7.15 (2H, d, J = 4Hz), 7.16-7.12 (2H,
m), 6.96 (2H, t, J = 9Hz), 6.74 (1H, d, J = 3Hz), 4.11
(2H, quartet, J = 7Hz), 2.85 (2H, t, J = 8Hz), 2.50 (2
H, t, J = 8Hz), 1.23 (3H, t, J = 7Hz). 3) 2- (4-fluorophenyl) -4- (3-hydrido
Roxypropyl) -3- (pyridin-4-yl) -1H
-4- (2-ethoxycarbonylethyl) -2 obtained from pyrrole 2)
A reduction reaction was carried out in the same manner as in Example 1-6) using-(4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole and lithium aluminum hydride to give the title compound as a pale brown powder (Yield 91
%).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.51 (2H, d, J = 5 Hz), 8.2
3 (1H, br.s), 7.17-7.12 (4H, m), 7.00 (2H, t, J = 9H
z), 6.75 (1H, d, J = 3Hz), 3.65 (2H, t, J = 6Hz), 2.61
(2H, t, J = 8Hz), 1.79-1.72 (2H, m), 1.61 (1H, br.
s). 4) 2- (4-fluorophenyl) -3- (pyridine
-4-yl) -4- [3- (p-toluenesulfonylthio )
Xy) propyl] -1H-pyrrole 2- (4-fluorophenyl) -4- (3-
(Hydroxypropyl) -3- (pyridin-4-yl)-
Using 1H-pyrrole, p-
The toluenesulfonylation reaction was performed to obtain the title compound as a pale yellow powder (yield: 71%).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.49 (2H, d, J = 6 Hz), 8.2
0 (1H, br.s), 7.59 (2H, d, J = 8Hz), 7.33 (2H, d, J = 8
Hz), 7.12 (2H, dd, J = 9Hz, 5Hz), 7.08 (2H, d, J = 6H
z), 6.96 (2H, t, J = 9Hz), 6.69 (1H, d, J = 3Hz), 4.00
(2H, t, J = 6Hz), 2.56 (2H, t, J = 8Hz), 2.44 (3H, s),
1.81-1.74 (2H, m). 5) 2- (4-fluorophenyl) -3- (pyridine
-4-yl) -4- [3- (thiomorpholin-1-i
) Propyl]-1H-pyrrole 2- (4-fluorophenyl obtained in 4)) -3- (pyridin-4-yl) -4- [3- (p-toluenesulfonyloxy) propyl]-1H-pyrrole 450mg
(1.07 mmol) was dissolved in 50 ml of acetonitrile, 163 mg (1.18 mmol) of potassium carbonate and 122 μl (1.29 mmol) of thiomorpholine were added, and the mixture was heated under reflux overnight. After cooling the reaction to room temperature,
Water was added and extracted with ethyl acetate. The organic layer was washed with water and concentrated under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent; ethyl acetate: methanol = 95: 5) to obtain 340 mg of the title compound as a pale yellow powder (yield 83%).

Melting point: 205-207 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.51 (2H, d, J = 6Hz), 8.20 (1H, br.
s), 7.14 (2H, dd, J = 9Hz, 5Hz), 7.13 (2H, d, J = 6Hz),
6.96 (2H, t, J = 9Hz), 6.72 (1H, d, J = 3Hz), 2.65 (8
H, s), 2.50 (2H, t, J = 8Hz), 2.35 (2H, t, J = 8Hz), 1.
66 (2H, quintet, J = 8Hz).

[0221]

Embodiment 244- [3- (1-benzylpiperazine
-4-yl) propyl] -2- (4-fluorophenyl)
) -3- (pyridin-4-yl) -1H-pillow Le
(Exemplary Compound No. 1-135) 1-benzylpiperazine is used in place of thiomorpholine
And the reaction was carried out in the same manner as in Example 23-5).
The compound was obtained as a white powder (yield 52%).

Melting point: 153 ° -154 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.50 (2H, d, J = 5Hz), 8.28 (1H, br.
s), 7.31 (4H, d, J = 4Hz), 7.28-7.22 (1H, m), 7.13 (2
H, dd, J = 9Hz, 5Hz), 7.13 (2H, d, J = 5Hz), 6.96 (2H,
t, J = 9Hz), 6.72 (1H, d, J = 2Hz), 3.50 (2H, s), 2.50
(2H, t, J = 8Hz), 2.44 (8H, br.s), 2.34 (2H, t, J = 8H
z), 1.69 (2H, quintet, J = 8Hz).

[0223]

Example 25 2- (4-fluorophenyl) -4-
[3- (Piperazin-1 -yl) propyl] -3- (pi
Lysin -4-yl) -1H-pyrrole (Exemplary Compound No. 1-133) 4- [3- (1-benzylpiperazin-4-yl) propyl] -2- (4-fluorophenyl) -3- (pyridine- A debenzylation reaction was carried out in the same manner as in Example 9-2) using (4-yl) -1H-pyrrole (the compound of Example 24) to obtain the title compound as a white powder (yield 9).
8%).

Melting point: 162-164 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.51 (2H, d, J = 6Hz), 8.20 (1H, br.
s), 7.14 (2H, dd, J = 9Hz, 5Hz), 7.14 (2H, d, J = 6Hz),
6.96 (2H, t, J = 9Hz), 6.73 (1H, d, J = 2Hz), 2.87 (4
H, t, J = 5Hz), 2.51 (2H, t, J = 8Hz), 2.36 (4H, br.
s), 2.32 (2H, t, J = 8Hz), 1.70 (2H, quintet, J = 8H
z).

[0225]

Example 26 4- (3-dimethylaminopropyl)
2- (4-Furuorofu Eniru) -3- (pyridin -4
-Yl) -1H-pyrrole (Exemplary Compound No. 1-10)
9) The reaction was carried out in the same manner as in Example 23-5) using dimethylamine instead of thiomorpholine to obtain the title compound as a white powder (yield 66%).

Melting point: 177-179 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.51 (2H, d, J = 5Hz), 8.24 (1H, br.
s), 7.15-7.13 (2H, m), 7.14 (2H, d, J = 5Hz), 6.96 (2
H, t, J = 9Hz), 6.74 (1H, d, J = 2Hz), 2.52 (2H, t, J = 8
Hz), 2.28 (2H, t, J = 8Hz), 2.19 (6H, s), 1.74-1.59
(2H, m).

[0227]

Example 27 2- (4-fluorophenyl) -4-
[3- (morpholin-1 -yl) propyl] -3- (pi
Lysin-4-yl) -1H-pyrrole (Exemplary Compound No. 1-125) Example 2 using morpholine instead of thiomorpholine
The reaction was carried out in the same manner as in 3-5) to give the title compound as a pale-yellow powder (yield 45%).

Melting point: 182-183 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.62 (1H, br.s), 8.50 (2H, d, J = 5H
z), 7.17-7.12 (2H, m), 7.14 (2H, d, J = 5Hz), 6.96 (2
H, t, J = 9Hz), 6.73 (1H, d, J = 3Hz), 3.70-3.68 (4H,
m), 2.53 (2H, t, J = 8Hz), 2.41-2.34 (4H, m), 2.33 (2
H, t, J = 8Hz), 1.68 (2H, quintet, J = 8Hz).

[0229]

Working Example 28 2- (4-Fluorophenyl) -4-
[3- (Piperidin-1 -yl) propyl] -3- (pi
Lysin-4-yl) -1H-pyrrole (Exemplary Compound No. 1-121) Example 2 using piperidine instead of thiomorpholine
The reaction was carried out in the same manner as in 3-5) to give the title compound as a pale-yellow powder (yield 63%).

Melting point: 195-197 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.50 (2H, d, J = 6Hz), 8.19 (1H, br.
s), 7.14 (2H, dd, J = 9Hz, 6Hz), 6.96 (2H, t, J = 9Hz),
6.74 (1H, d, J = 2Hz), 2.50 (2H, t, J = 8Hz), 2.40-2.3
0 (4H, m), 1.75-1.55 (8H, m), 1.43-1.42 (2H, m).

[0231]

Working Example 29 2- (4-Fluorophenyl) -4-
[3- (1-Mechirupipe Rajin-4-yl) propyl]
-3- (Pyridin-4-yl) -1H-pyrrole (Exemplary Compound No. 1-134) The reaction was carried out in the same manner as in Example 23-5) using 1-methylpiperazine instead of thiomorpholine to give the title compound Was obtained as a pale yellow powder (yield 64%).

Melting point: 190-192 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.65 (1H, br.s), 8.49 (2H, d, J = 6H
z), 7.16-7.12 (2H, m), 7.14 (2H, d, J = 6Hz), 6.95 (2
H, t, J = 9Hz), 6.73 (1H, d, J = 3Hz), 2.52 (2H, t, J = 8
Hz), 2.53-2.36 (8H, m), 2.36 (2H, t, J = 8Hz), 2.28
(3H, s), 1.70 (2H, quintet, J = 8Hz).

[0233]

Example 30 1- (3-dimethylaminopropyl)
3- (4-Furuorofu Eniru) -2- (pyridin -4
-Yl) -1H-pyrrole (Exemplary Compound No. 2-10)
9) The same reaction as in Examples 12-1), 2) and 3) was sequentially performed using 3-dimethylaminopropylamine as a starting material instead of 4-amino-1-benzylpiperidine, and the title compound was converted to white. Obtained as a powder (total yield 9
%).

Melting point: 93-95 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.59 (2H, d, J = 6Hz), 7.18 (2H, d, J =
6Hz), 7.07 (2H, dd, J = 9Hz, 6Hz), 6.89 (2H, t, J = 9H
z), 6.84 (1H, d, J = 3Hz), 6.35 (1H, d, J = 3Hz), 3.93
(2H, t, J = 7Hz), 2.14 (2H, t, J = 7Hz), 2.11 (6H, s),
1.71 (2H, quintet, J = 7Hz).

[0235]

Example 31 2- (4-fluorophenyl) -3,
4-bis (pyridin-4 -yl) -1H-pyrrole (Exemplary Compound No. 1-159) 2- (4-fluorophenyl) -3- (pyridine-4-
Yl) -4- (1,2,3,6-tetrahydropyridin-4-yl) -1H-pyrrole dihydrochloride (Example 10
Compound (450 mg) (1.15 mmol) was suspended in a mixture of 25 ml of xylene and 2 ml of methanol.
0% palladium-carbon 450 mg and sodium carbonate 3
After adding 20 mg (2.30 mmol) and heating under reflux for 4 hours, the mixture was filtered. The filtrate was concentrated under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent; ethyl acetate: methanol: isopropylamine = 10: 1: 1) to obtain 192 mg of the title compound as a pale yellow powder (yield 53%). ).

Melting point: 325-330 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.87 (1H, br.s), 8.47 (2H, d, J
= 6Hz), 8.35 (2H, d, J = 6Hz), 7.39 (1H, d, J = 3Hz), 7.
21 (2H, dd, J = 9Hz, 5Hz), 7.16 (2H, t, J = 9Hz), 7.08
(2H, d, J = 6Hz), 7.03 (2H, d, J = 6Hz).

[0237]

Example 32 2- (4-fluorophenyl) -4-
(1-methyl-1,2,3,6 -tetrahydropyridine
-4-yl) -3- (pyridin-4-yl) -1H -pi
Roll (Exemplified Compound No. 1-145) 1) 2- (4-fluorophenyl) -4- (4- hydr)
Proxy 1-Mechirupipe lysine-4-yl) -3- (Hoon
Lysine-4-yl) -1-triisopropyl silyl -1
The reaction was carried out in the same manner as in Example 7-4) using 1-methylpiperidin-4-one instead of H-pyrrolepentafluoropyridine to obtain the title compound as a slightly brown powder (yield 47).
%).

¹ H-nuclear magnetic resonance spectrum (500 MH
z, CD ₃ OD) δ ppm: 8.22 (2H, d, J = 6 Hz), 7.27
(2H, d, J = 6Hz), 7.21 (2H, dd, J = 9Hz, 5Hz), 6.94 (2
H, t, J = 9Hz), 6.92 (1H, s), 2.56-2.42 (4H, br.m),
2.22 (3H, s), 2.00-1.91 (2H, br.m), 1.84-1.78 (2H,
br.m), 1.20-1.11 (3H, m), 1.06 (18H, d, J = 7Hz). 2) 2- (4-fluorophenyl) -4- (1-methyl
Le-1,2,3,6-te tiger-tetrahydropyridine-4-Yi
Le) -3- (pyridin-4-yl)-1H-obtained in pyrrole 1) 2- (4-fluorophenyl) -4- (4-
(Hydroxy-1-methylpiperidin-4-yl) -3-
Dehydration reaction using triethylsilane / trifluoroacetic acid in the same manner as in Example 9-3) using (pyridin-4-yl) -1-triisopropylsilyl-1H-pyrrole,
And a desilyl reaction (deprotection reaction) using tetrabutylammonium fluoride to obtain the title compound as a slightly yellow powder (yield 91%).

Melting point: 230-232 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.36 (1H, br.s), 8.45 (2H, d, J
= 6Hz), 7.19-7.14 (6H, m), 6.90 (1H, d, J = 3Hz), 5.24
-5.21 (1H, br.m), 2.78-2.75 (2H, br.m), 2.40 (2H,
t, J = 5Hz), 2.18 (3H, s), 2.20-2.13 (2H, br.m).

[0240]

Working Example 33 2- (4-Fluorophenyl) -4-
(1-Methylpiperidin -4-yl) -3- (pyridine
-4-yl) -1H-pyrrole (exemplary compound number 1-1)
44) 2- (4-Fluorophenyl) -4- (1-methyl-
1,2,3,6-tetrahydropyridin-4-yl)-
A reduction reaction was carried out using 3- (pyridin-4-yl) -1H-pyrrole (the compound of Example 32) in the same manner as in Example 11 to obtain the title compound as a white powder (yield: 85).
%).

Melting point: 284-285 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.20 (1H, br.s), 8.48 (2H, d, J
= 6Hz), 7.19-7.16 (4H, m), 7.10 (2H, t, J = 9Hz), 6.76
(1H, d, J = 2Hz), 2.73 (2H, d, J = 12Hz), 2.35 (1H, t
t, J = 12Hz, 4Hz), 2.12 (3H, s), 1.77 (2H, t, J = 12H
z), 1.61 (2H, d, J = 12Hz), 1.51 (2H, ddt, J = 13Hz, 12
Hz, 4Hz).

[0242]

Working Example 34 3- (4-Fluorophenyl) -2-
(Pyridin-4-yl) -1- (2,2,6,6-tet
La methylpiperidin-4-yl)-1H-pyrrole (Compound No. 2-2523) 4-amino-1-starting material 4-amino-2,2,6,6-tetramethylpiperidine in place of benzyl piperidine And the same reaction as in Examples 12-1), 2) and 3) was carried out sequentially to obtain the title compound as a white powder (total yield: 12%).

Melting point: 118-119 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.62 (2H, d, J = 6Hz), 7.18 (2H, d, J =
6Hz), 7.07 (2H, dd, J = 9Hz, 6Hz), 6.89 (1H, d, J = 3H
z), 6.88 (2H, t, J = 9Hz), 6.39 (1H, d, J = 3Hz), 4.43-
4.38 (1H, m), 1.86 (2H, dd, J = 13Hz, 3Hz), 1.55-1.3
8 (3H, m), 1.15 (6H, s), 1.05 (6H, s).

[0244]

Example 35 2- (4-fluorophenyl) -3-
(Pyridin-4-yl) -4- (quinuclidine-2-e
N-3-yl) -1H-pyrrole (exemplary compound number 1-
2540) 1) (±) -2- (4-fluorophenyl) -4-
(3-Hydroxyquinuclidin -3-yl) -3- (pi
Lysin-4-yl) -1-triisopropylsilyl- 1
Quinuclidine-3-in place of H -pyrrolepentafluoropyridine
The reaction was carried out in the same manner as in Example 7-4) using ON to give the title compound as a slightly brown powder (yield 37%).

The ¹ H-nuclear magnetic resonance spectrum (500 MH
z, DMSO-d ₆ ) δ ppm: 8.25 (2H, d, J = 6 Hz),
7.25 (2H, d, J = 6Hz), 7.26-7.16 (2H, br.m), 7.08 (2
H, t, J = 9Hz), 6.80 (1H, s), 4.82 (1H, s), 2.81 (1H,
d, J = 14Hz), 2.72-2.64 (1H, br.m), 2.59 (1H, d, J =
15Hz), 2.60-2.50 (2H, br.m), 2.46-2.37 (1H, br.m),
2.03-1.91 (2H, br.m), 1.49-1.37 (2H, br.m), 1.26-1.
17 (1H, br.m), 1.15-1.05 (3H, m), 1.03-0.95 (18H,
m). 2) 2- (4-fluorophenyl) -3- (pyridine
4-yl) -4- (g Nukurijin-2-en-3-y
) -1H-pyrrole (±) -2- (4-fluorophenyl) -4 obtained in 1)
-(3-hydroxyquinuclidin-3-yl) -3-
24 ml of formic acid was added to 1.20 g (2.31 mmol) of (pyridin-4-yl) -1-triisopropylsilyl-1H-pyrrole, the mixture was stirred at 90 ° C. for 3 hours, and then cooled to room temperature. Water was added to the reaction solution, and the pH was adjusted to 10 or more by further adding a 10% aqueous sodium hydroxide solution, followed by extraction with ethyl acetate. The organic layer was washed with water, dried over anhydrous sodium sulfate, concentrated under reduced pressure, and the obtained solid was washed with a 1: 1 mixture of ethyl acetate-diethyl ether to give 568 mg of the title compound as a slightly brown powder. Was obtained (yield 71%).

Melting point: 246-248 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.48 (1H, br.s), 8.47 (2H, d, J
= 6Hz), 7.19-7.14 (4H, m), 7.11 (2H, t, J = 9Hz), 7.00
(1H, d, J = 2Hz), 5.86 (1H, s), 2.77 (2H, ddd, J = 13H
z, 9Hz, 5Hz), 2.61-2.56 (1H, br.m), 2.40-2.31 (2H,
m), 1.58-1.49 (2H, br.m), 1.43-1.34 (2H, br.m).

[0247]

Example 36 (±) -2- (4-fluorophenyl)
) -3- (pyridin-4 -yl) -4- (quinuclidi
N-3-yl) -1H-pyrrole (exemplary compound number 1-
2539) 2- (4-Fluorophenyl) -3- (pyridine-4-
Yl) -4- (quinuclidin-2-en-3-yl)-
A reduction reaction was carried out using 1H-pyrrole (the compound of Example 35) in the same manner as in Example 11 to obtain the title compound as a white powder (yield: 82%).

Melting point: 239-241 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.25 (1H, br.s), 8.47 (2H, d, J
= 6Hz), 7.18-7.07 (6H, m), 6.93 (1H, d, J = 2Hz), 2.98
-2.90 (1H, m), 2.89-2.76 (2H, br.m), 2.74-2.58 (4H,
br.m), 1.73-1.64 (1H, br.m), 1.54-1.46 (2H, br.
m), 1.42-1.33 (1H, br.m), 1.26-1.17 (1H, br.m).

[0249]

Working Example 37 2- (4-Fluorophenyl) -4-
(4-hydroxy-piperidine-Jin-4-yl) -3- (pyridinium
Zin-4-yl) -1H-pyrrole (Exemplary Compound No. 1)
-2526) 2- (4-Fluorophenyl)-obtained in Example 9-2)
4- (4-hydroxypiperidin-4-yl) -3-
675 mg (1.37 mmol) of (pyridin-4-yl) -1-triisopropylsilyl-1H-pyrrole was dissolved in 14 ml of tetrahydrofuran, and a 1 M tetrabutylammonium fluoride / tetrahydrofuran solution was used.
73 ml (2.73 mmol) was added, and the mixture was stirred at room temperature for 30 minutes. The solvent was distilled off under reduced pressure, water was added, and the precipitated solid was collected by filtration and washed with ethyl acetate to give the title compound 363.
mg was obtained as a white powder (79% yield).

Melting point: 197-199 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.16 (1H, br.s), 8.42 (2H, d, J
= 6Hz), 7.32 (2H, d, J = 6Hz), 7.04-7.01 (4H, m), 6.79
(1H, d, J = 2Hz), 4.45 (1H, s), 2.78-2.70 (2H, m),
2.55-2.45 (2H, overlap with DMSO-d ₆ residual proton), 1.63-1.4
8 (4H, m).

[0251]

Working Example 38 2- (4-Fluorophenyl) -4-
(3-methanesulfonylaminopropyl ) -3- (pyri
Zin-4-yl) -1H-pyrrole (Exemplary Compound No. 1)
-2536) 290 mg (0.982 mmol) of 4- (3-aminopropyl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole (the compound of Example 1)
l) was dissolved in 5 ml of pyridine, 188 mg (1.08 mmol) of methanesulfonic anhydride was added, and the mixture was allowed to stand overnight. Water was added to the reaction solution, and the precipitate was collected by filtration and washed with ethyl acetate to give the title compound (208 mg) as a pale-brown powder (yield 57%).

Melting point: 210-214 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.52 (2H, d, J = 6Hz), 8.23 (1H, br.
s), 7.15-7.12 (4H, m), 6.97 (2H, t, J = 9Hz), 6.76 (1
H, d, J = 2Hz), 4.15 (1H, br.s), 3.13-3.09 (2H, m),
2.89 (3H, s), 2.61 (2H, t, J = 7Hz), 1.72 (2H, quinte
t, J = 7Hz).

[0253]

Working Example 39 (±) -3- (4-Fluorophenyl)
) -2- (pyridin-4 -yl) -1- (quinuclidine
N-3-yl) -1H-pyrrole (Exemplified Compound No. 2-
2539) Instead of 4-amino-1-benzylpiperidine (±)
Using -3-aminoquinuclidine as a starting material, the same reactions as in Examples 12-1), 2) and 3) were successively performed to obtain the title compound as a pale brown powder (total yield: 2).
5%).

Melting point: 229-230 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.61 (2H, d, J = 6Hz), 7.16 (2H, d, J =
6Hz), 7.13 (1H, d, J = 3Hz), 7.04 (2H, dd, J = 9Hz, 5H
z), 6.87 (2H, t, J = 9Hz), 6.42 (1H, d, J = 3Hz), 4.24
4.15 (1H, m), 3.33-3.23 (1H, m), 3.22-3.05 (2H,
m), 2.98-2.79 (2H, m), 2.78-2.67 (1H, m), 1.95-1.81
(2H, m), 1.71-1.58 (1H, m), 1.56-1.37 (2H, m).

[0255]

Example 40 (±) -3- (4-Fluorophenyl)
1)-(piperidin- 3-yl) methyl-2- (pi
Lysin -4-yl) -1H-pyrrole (Exemplary Compound No. 2-2520) (±) -3-amino-1- (t-butoxycarbonyl)
Instead of pyrrolidine, (±) -3-aminomethyl- (1
(T-Butoxycarbonyl) piperidine was used as a starting material, and the same reaction as in Examples 18-1) and 2) was sequentially performed to obtain the title compound as a white powder (total yield: 7%).

Melting point: 134-135 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.59 (2H, d, J = 6Hz), 7.16 (2H, d, J =
6Hz), 7.06 (2H, dd, J = 9Hz, 5Hz), 6.88 (2H, t, J = 9H
z), 6.79 (1H, d, J = 3Hz), 6.34 (1H, d, J = 3Hz), 3.74
(2H, d, J = 8Hz), 2.94-2.87 (1H, m), 2.83-2.73 (1H,
m), 2.46 (1H, dd, J = 12Hz, 3Hz), 2.13 (1H, dd, J = 12H
(z, 10Hz), 1.75-1.51 (3H, m), 1.40-1.28 (1H, m), 0.9
8-0.85 (1H, m).

[0257]

Example 41 cis-1- (4-aminocyclohexene
Sil) -3- (4-full Orofeniru) -2- (pyrid
N-4-yl) -1H-pyrrole (Exemplified Compound No. 2-
2529) (±) -3-Amino-1- (t-butoxycarbonyl)
The same reaction as in Examples 18-1) and 2) was sequentially performed using cis-4- (t-butoxycarbonylamino) cyclohexylamine as a starting material instead of pyrrolidine to obtain the title compound as a pale brown powder. (Total yield 10%) Melting point: 163-164 ° C ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.61 (2H, d, J = 6Hz), 7.14 (2H, d, J =
6Hz), 7.05 (2H, dd, J = 9Hz, 5Hz), 7.03 (1H, d, J = 3H
z), 6.87 (2H, t, J = 9Hz), 6.83 (1H, d, J = 3Hz), 3.82
(1H, tt, J = 12Hz, 4Hz), 3.29-3.22 (1H, m), 2.22-2.0
7 (2H, m), 1.82-1.41 (6H, m).

[0258]

Working Example 42 3- (4-Fluorophenyl) -2-
(2-methylamino-pyrimidine-4-yl) -1- (Hoon
Peridin-4-yl) -1H-pyrrole (Exemplary Compound No. 2-1072) 1) 1- (1- Benzylpiperidin -4-yl) -3
- (4-fluoro-phenylcarbamoyl) -2- (2-Mechiruchiopi
Example 12 using 4-formyl-2-methylthiopyrimidine as a starting material instead of ( limidin-4-yl) -1H-pyrrole 4-formylpyridine.
The same reaction as in -1), 2) and 3) was successively performed to obtain the title compound as a brown oil (total yield: 34%).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.21 (1H, d, J = 5 Hz), 7.3
9-7.24 (5H, m), 7.16 (2H, dd, J = 9Hz, 5Hz), 7.06 (1
H, d, J = 3Hz), 6.96 (2H, t, J = 9Hz), 6.57 (1H, d, J =
5Hz), 6.27 (1H, d, J = 3Hz), 4.83-4.73 (1H, m), 3.54
(2H, s), 3.02 (2H, d, J = 9Hz), 2.75 (2H, t, J = 6Hz),
2.46 (2H, t, J = 6Hz), 2.13-1.96 (2H, m). 2) 1- (1-benzylpiperidin-4-yl) -3
- (4-fluoro-phenylcarbamoyl) -2- (2-methanesulfonate
1- (1-benzylpiperidin-4-yl) obtained in 1), nilpyrimidin-4-yl) -1H-pyrrole
3.50 g of -3- (4-fluorophenyl) -2- (2-methylthiopyrimidin-4-yl) -1H-pyrrole
(7.63 mmol) in 35 ml of ethyl acetate,
2. 69-75% by weight m-chloroperbenzoic acid under ice-cooling
After 51 g (15.26 mmol) was added little by little and the mixture was stirred at room temperature for 2 days, a 10% aqueous sodium thiosulfate solution was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer is washed with water, concentrated under reduced pressure, and the residue is subjected to silica gel column chromatography (solvent; dichloromethane: methanol = 9:
By subjecting it to 1), 2.48 g of the title compound was obtained as a light brown amorphous solid (yield 66%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.35 (1H, d, J = 5 Hz), 7.6
3-7.56 (2H, m), 7.47-7.38 (3H, m), 7.29-7.24 (1H,
m), 7.22 (2H, dd, J = 9Hz, 5Hz), 7.05 (2H, t, J = 9H
z), 6.90 (2H, d, J = 5Hz), 6.29 (1H, d, J = 3Hz), 5.43-
5.33 (1H, m), 4.46 (2H, s), 3.56-3.27 (4H, m), 3.03
-2.86 (2H, m), 2.93 (3H, s), 2.26-2.14 (1H, m), 2.1
0-2.01 (1H, m). 3) 1- (1-benzylpiperidin-4-yl) -3
- (4-fluoro-phenylcarbamoyl) -2- (2-methylamino
1- (1-benzylpiperidin-4-yl) obtained by pyrimidin-4-yl) -1H-pyrrole 2)
-3- (4-Fluorophenyl) -2- (2-methanesulfonylpyrimidin-4-yl) -1H-pyrrole
13 ml of a 2M methylamine / tetrahydrofuran solution was added to 19 g (2.43 mmol), and 100 ° C.
For 30 hours. The solvent was concentrated under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent; hexane: ethyl acetate = 1: 2) to give the title compound (260 mg) as a yellow amorphous solid (yield 24%).

¹ H-nuclear magnetic resonance spectrum (500 MH
z, CDCl ₃ ) δ ppm: 8.03 (1H, d, J = 5 Hz), 7.4
2-7.23 (5H, m), 7.18 (2H, dd, J = 9Hz, 5Hz), 7.00 (1
H, d, J = 3Hz), 6.94 (2H, t, J = 9Hz), 6.26 (1H, d, J =
3Hz), 6.23 (1H, d, J = 5Hz), 5.14-5.04 (1H, m), 4.82-
4.68 (1H, m), 3.53 (2H, s), 3.10-2.95 (5H, m), 2.12
-1.96 (6H, m). 4) 3- (4-fluorophenyl) -2- (2-methyl
Ruaminopyrimidin-4 -yl) -1- (piperidine-
4- (yl) -1H-pyrrole 1- (1-benzylpiperidin-4-yl) obtained in 3)
A debenzylation reaction was carried out in the same manner as in Example 9-2) using -3- (4-fluorophenyl) -2- (2-methylaminopyrimidin-4-yl) -1H-pyrrole to give the title compound. Obtained as a pale yellow powder (39% yield).

Melting point: 189-191 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.05 (1H, d, J = 5Hz), 7.19 (2H, dd, J
= 9Hz, 5Hz), 7.00 (1H, d, J = 3Hz), 6.95 (2H, t, J = 9H
z), 6.28 (1H, d, J = 3Hz), 6.24 (1H, d, J = 5Hz), 5.14-
5.04 (1H, m), 4.96-4.81 (1H, m), 3.24 (2H, d, J = 12H
z), 3.04 (3H, d, J = 5Hz), 2.70 (2H, dt, J = 12Hz, 2H
z), 2.14 (2H, d, J = 12Hz), 1.91 (2H, dq, J = 12Hz, 4H
z).

[0263]

Example 43 (±) -2- (4-fluorophenyl)
) -4- (8-Methyl- 8-azabicyclo [3.2.
1] oct-2-en-3-yl) -3- (pyridine down -
4-yl) -1H-pyrrole (exemplary compound number 1-25)
44) 1) 2- (4-Fluorophenyl) -4- (3-hydrido)
Roxy-8-methyl-8 -azabicyclo [3.2.1]
Octan-3-yl) -3- (pyridin-4-i le) -
The reaction was carried out in the same manner as in Example 7-4) using 8-methyl-8-azabicyclo [3.2.1] octan-3-one instead of 1-triisopropylsilyl-1H-pyrrolepentafluoropyridine , An isomer mixture of the title compound was obtained as a light brown powder (yield 49%).

This isomer mixture was subjected to alumina column chromatography (solvent; ethyl acetate: methanol = 1).
0: 1) to separate into isomer A (Rf value 0.45, light brown powder) and isomer B (Rf value 0.40, light brown powder) (weight ratio: A: B = 85). : 90). Isomer A ¹ H-nuclear magnetic resonance spectrum (500 MHz, CD ₃ O
D) δppm: 8.21 (2H, d, J = 6Hz), 7.26 (2H, d, J =
6Hz), 7.17 (2H, dd, J = 9Hz, 5Hz), 6.92 (2H, t, J = 9H
z), 6.84 (1H, s), 3.14-3.06 (1H, br.m), 2.28-2.15
(4H, m), 2.20 (3H, s), 1.95-1.84 (4H, br.m), 1.19-
1.09 (3H, m), 1.05 (18H, d, J = 7Hz). Isomer B ¹ H-nuclear magnetic resonance spectrum (500 MHz, CD ₃ O
D) δppm: 8.22 (2H, d, J = 6Hz), 7.27 (2H, d, J =
6Hz), 7.18 (2H, dd, J = 9Hz, 5Hz), 6.93 (2H, t, J = 9H
z), 6.85 (1H, s), 3.38 (1H, br.s), 2.41 (3H, s), 2.
38-2.27 (4H, m), 2.06-1.95 (4H, br.m), 1.20-1.10
(3H, m), 1.06 (18H, d, J = 7Hz). 2) (±) -2- (4-fluorophenyl) -4-
(8-methyl-8-Azabi cyclo [3.2.1] oct
2-en-3-yl) -3- (pyridin-4-i le)
1 -H-pyrrole 1) 2- (4-fluorophenyl) -4- (3-
Hydroxy-8-methyl-8-azabicyclo [3.2.
1] Example 9- using octane-3-yl) -3- (pyridin-4-yl) -1-triisopropylsilyl-1H-pyrrole (mixture of isomer A and isomer B)
In the same manner as in 3), a dehydration reaction using triethylsilane / trifluoroacetic acid and a desilyl reaction (deprotection reaction) using tetrabutylammonium fluoride were performed to obtain the title compound as a white powder (yield). 83%).

Melting point: 243-245 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CD ₃ O
D) δppm: 8.39 (2H, d, J = 7Hz), 7.25 (2H, d, J =
6Hz), 7.16 (2H, dd, J = 9Hz, 5Hz), 6.99 (2H, t, J = 9H
z), 6.83 (1H, s), 5.45 (1H, br.d, J = 6Hz), 3.28-3.24
(1H, br.m), 3.22 (1H, t, J = 6Hz), 2.68 (1H, br.d,
J = 16Hz), 2.37 (3H, s), 2.20-2.11 (1H, br.m), 2.09-
1.99 (1H, m), 1.90-1.80 (2H, br.m), 1.69-1.61 (1H,
m).

[0266]

Working Example 44 2- (4-Fluorophenyl) -4-
(8-methyl-8-aza bicyclo [3.2.1] oct
N-3-yl) -3- (pyridin-4-yl) -1H-
Pyrrole (Exemplary Compound No. 1-2542) (±) -2- (4-fluorophenyl) -4- (8-methyl-8-azabicyclo [3.2.1] oct-2-en-3-yl)- 3- (pyridin-4-yl) -1H-
A reduction reaction was carried out using pyrrole (the compound of Example 43) in the same manner as in Example 11 to obtain the title compound as a white powder (yield 57%).

Melting point: 233-234 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.13 (1H, br.s), 8.49 (2H, d, J =
6Hz), 7.14-7.05 (6H, m), 6.76 (1H, d, J = 3Hz), 3.03-
2.85 (3H, br.m), 2.16-2.07 (2H, m), 2.04 (3H, s),
1.98-1.90 (2H, m), 1.45-1.36 (2H, m), 1.24-1.14 (2
H, m).

[0268]

Example 45 (±) -4- (8-Azabicyclo)
[3.2.1] Oct-2- en-3-yl) -2-
(4-Fluorophenyl) -3- (pyridine-4-i
Le)-1H-pyrrole (Compound No. 1-2543) 8-benzyl-8-instead of 1-benzyl-4-one-azabicyclo [3.2.1] octan-3
In the same manner as in Examples 9-1), 2) and 3) using on as a starting material, a coupling reaction, a debenzylation reaction,
The dehydration reaction and the desilyl reaction were sequentially performed to obtain the title compound as a slightly yellow powder (yield 35%).

Melting point: 212-213 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.32 (1H, br.s), 8.45 (2H, d, J =
6Hz), 7.17-7.07 (6H, m), 6.81 (1H, d, J = 3Hz), 5.45
(1H, d, J = 6Hz), 3.53-3.46 (1H, m), 3.38-3.32 (1H,
m), 2.55-2.48 (1H, br.m), 1.86-1.69 (3H, m), 1.66-
1.55 (1H, m), 1.52-1.44 (1H, m).

[0270]

Embodiment 464- (8-Azabicyclo [3.2.
1] Octan-3-yl) -2- (4-fluorophenyl)
) -3- (pyridin-4-yl) -1H-pillow Le
(Exemplified Compound No. 1-2541) (±) -4- (8-azabicyclo [3.2.1] oct)
-2-en-3-yl) -2- (4-fluorophenyl)
) -3- (pyridin-4-yl) -1H-pyrrole
(Compound of Example 45) in the same manner as in Example 11.
Original reaction was performed to obtain the title compound as a white powder.
(74% yield).

Melting point: 235-237 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.14 (1H, br.s), 8.48 (2H, d, J =
6Hz), 7.15-7.05 (6H, m), 6.73 (1H, d, J = 2Hz), 3.18-
3.15 (2H, m), 2.86-2.78 (1H, m), 2.05-1.96 (2H, m),
1.63-1.56 (2H, m), 1.50-1.43 (2H, m), 1.17-1.08 (2
H, m).

[0272]

Working Example 47 2- (4-Fluorophenyl) -3-
(Pyridin-4-yl) -4- (1,2,3,6-tet
Rahidoro 2,2,6,6-tetramethyl pyridinium down -4
-Yl ) -1H-pyrrole (Exemplary Compound No. 1-265)
0) 2,2 instead of 1-benzylpiperidin-4-one
Using 6,6-tetramethylpiperidin-4-one as a starting material, a coupling reaction, a dehydration reaction and a desilyl reaction were sequentially performed in the same manner as in Examples 9-1) and 3).
The title compound was obtained as a white powder (50% yield).

Melting point: 258-259 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.37 (1H, br.s), 8.42 (2H, d, J =
6Hz), 7.19-7.09 (6H, m), 6.86 (1H, d, J = 2Hz), 5.04-
5.02 (1H, br.m), 1.93 (2H, s), 1.25-1.15 (1H, br.m)
s), 1.04 (6H, s), 0.94 (6H, s).

[0274]

Working Example 48 2- (4-Fluorophenyl) -3-
(Pyridin-4-yl) -4- (2,2,6,6-tet
La methylpiperidin-4-yl)-1H-pyrrole (Compound No. 1-2523) 2- (4-fluorophenyl) -3- (pyridin-4
Yl) -4- (1,2,3,6-tetrahydro-2,
2,6,6-tetramethylpyridin-4-yl) -1H
Example 11 using pyrrole (the compound of Example 47)
A reduction reaction was carried out in the same manner as in the above to give the title compound as a white powder (yield 77%).

Melting point: 242-243 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.18 (1H, br.s), 8.47 (2H, d, J =
6Hz), 7.21-7.15 (4H, m), 7.11 (2H, t, J = 9Hz), 6.70
(1H, d, J = 2Hz), 2.95 (1H, tt, J = 13Hz, 3Hz), 1.50 (2
H, dd, J = 13Hz, 3Hz), 1.09 (2H, t, J = 13Hz), 1.01 (6
H, s), 0.96 (6H, s).

[0276]

Example 49 (±) -2- (4-Fluorophenyl)
) -4- (2-Methyl- 1,2,3,6-tetrahydride
Ropirijin 4-yl) -3- (pyridin-4-i le)
-1H-pyrrole (Exemplified Compound No. 1-2707) Instead of 1-benzylpiperidin-4-one, (±)-
Using 1-benzyl-2-methylpiperidin-4-one as a starting material, a coupling reaction, debenzylation reaction, dehydration reaction and desilyl reaction were carried out in the same manner as in Examples 9-1), 2) and 3). Sequentially, a mixture of the title compound and its isomer (the compound of Example 50) was obtained. This mixture was subjected to silica gel column chromatography (solvent; ethyl acetate: isopropylamine = 25: 1) to give the title compound (Rf value 0.50) as a white powder (yield 3%).

Melting point: 178-180 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, CD ₃ O
D) δppm: 8.36 (2H, d, J = 6Hz), 7.24 (2H, d, J =
6Hz), 7.17 (2H, dd, J = 9Hz, 6Hz), 7.00 (2H, t, J = 9H
z), 6.85 (1H, s), 5.40-5.35 (1H, br.m), 3.46-3.38
(1H, m), 3.36-3.28 (1H, m), 2.96-2.88 (1H, m), 2.23
-2.15 (1H, m), 2.06-1.97 (1H, m), 1.14 (3H, d, J = 6
Hz).

[0278]

Example 50 (±) -2- (4-fluorophenyl)
) -4- (6-Methyl- 1,2,3,6-tetrahydride
Ropirijin 4-yl) -3- (pyridin-4-i le)
-1H-pyrrole (Exemplified Compound No. 1-2665) The title compound (Rf value: 0.45) was obtained as a white powder by silica gel column chromatography performed in Example 49 (yield: 5%).

Melting point: 201-204 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, CD ₃ O)
D) δppm: 8.36 (2H, d, J = 6Hz), 7.24 (2H, d, J =
6Hz), 7.18 (2H, dd, J = 9Hz, 6Hz), 7.00 (2H, t, J = 9H
z), 6.86 (1H, s), 5.24-5.20 (1H, m), 3.48-3.40 (1H,
m), 3.16-3.09 (1H, m), 2.90-2.82 (1H, m), 2.37-2.2
7 (1H, m), 2.18-2.10 (1H, m), 1.05 (3H, d, J = 7H
z).

[0280]

Example 51 (±) -2- (4-fluorophenyl)
) -4- (2-methylpiperidin Perijin 4-yl) -3-
(Pyridin-4-yl) -1H-pyrrole (Exemplary Compound No. 1-2522) (±) -2- (4-fluorophenyl) -4- (6-methyl-1,2,3,6-tetrahydropyridine- A reduction reaction was performed in the same manner as in Example 11 using 4-yl) -3- (pyridin-4-yl) -1H-pyrrole (the compound of Example 50) to obtain the title compound as a pale yellow powder ( Yield 83%).

Melting point: 198-205 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.53 (2H, d, J = 4Hz), 8.33 (0.5H, br.
s), 8.31 (0.5H, br.s), 7.14 (2H, d, J = 4Hz), 7.11 (2
H, dd, J = 9Hz, 5Hz), 6.95 (2H, t, J = 9Hz), 6.79 (0.5
H, d, J = 3Hz), 6.74 (0.5H, d, J = 3Hz), 3.25-2.63 (4
H, m), 1.74-1.43 (5H, m), 1.11 (1.5H, d, J = 7Hz), 1.
07 (1.5H, d, J = 7Hz).

[0282]

Working Example 52 4- (1-Ethyl-1,2,3,6-
Tetrahydropyridin- 4-yl) -2- (4-fluoro
L-phenyl) -3- (pyridin-4-yl) -1H -pi
Roll (Exemplified Compound No. 1-2629) Coupling reaction similar to Examples 9-1) and 3) using 1-ethylpiperidin-4-one as a starting material instead of 1-benzylpiperidin-4-one , A dehydration reaction and a desilyl reaction were sequentially performed to obtain the title compound as a pale yellow powder (yield 55%).

Melting point: 234-236 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.36 (1H, br.s), 8.45 (2H, d, J =
6Hz), 7.18-7.08 (6H, m), 6.90 (1H, d, J = 3Hz), 5.26-
5.22 (1H, br.m), 2.84-2.79 (2H, br.m), 2.45 (2H, t,
J = 6Hz), 2.34 (2H, quartet, J = 8Hz), 2.18-2.12 (2H,
br.m), 0.99 (3H, t, J = 8Hz).

[0284]

Working Example 53 4- (1-ethylpiperidin-4-i)
) -2- (4-fluoride Rofeniru) -3- (pyridine
-4-yl) -1H-pyrrole (exemplary compound number 1-1)
46) 4- (1-Ethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3
-(Pyridin-4-yl) -1H-pyrrole (Example 5
The compound of formula (2) was subjected to a reduction reaction in the same manner as in Example 11 to give the title compound as a white powder (yield: 95).
%).

Melting point: 262-263 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.19 (1H, br.s), 8.48 (2H, d, J =
6Hz), 7.18-7.07 (6H, m), 6.76 (1H, d, J = 2Hz), 2.87-
2.79 (2H, br.m), 2.37 (1H, tt, J = 12Hz, 4Hz), 2.26
(2H, quartet, J = 7Hz), 1.80-1.71 (2H, br.m), 1.66-1.
59 (2H, br.m), 1.55-1.43 (2H, m), 0.96 (3H, t, J = 7H
z).

[0286]

Working Example 54 2- (4-Fluorophenyl) -4-
(1-Isopropyl- 1,2,3,6-tetrahydropi
Lysin-4-yl) -3- (pyridin-4-yl ) -1
H-Pyrrole (Exemplified Compound No. 1-2632) In the same manner as in Examples 9-1) and 3) using 1-isopropylpiperidin-4-one as a starting material instead of 1-benzylpiperidin-4-one, Ring reaction,
The dehydration reaction and the desilyl reaction were sequentially performed to obtain the title compound as a slightly yellow powder (yield 42%).

Melting point: 237-240 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.35 (1H, br.s), 8.45 (2H, d, J =
6Hz), 7.18-7.08 (6H, m), 6.88 (1H, d, J = 3Hz), 5.28-
5.24 (1H, br.m), 2.94-2.89 (2H, br.m), 2.64 (1H, se
ptet, J = 6Hz), 2.49 (2H, t, J = 6Hz), 2.15-2.09 (2H,
br.m), 0.96 (6H, d, J = 6Hz).

[0288]

Example 55 2- (4-fluorophenyl) -4-
(L-isopropyl piperazinyl lysine-yl) -3- (Hoon
Lysin -4-yl) -1H-pyrrole (Exemplary Compound No. 1-2633) 2- (4-fluorophenyl) -4- (1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl)- A reduction reaction was carried out using 3- (pyridin-4-yl) -1H-pyrrole (the compound of Example 54) in the same manner as in Example 11 to obtain the title compound as white needle crystals (yield: 80%). ).

Melting point: 264-266 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.18 (1H, br.s), 8.48 (2H, d, J =
6Hz), 7.17-7.06 (6H, m), 6.76 (1H, s), 2.77-2.70 (2
H, br.m), 2.63 (1H, septet, J = 6Hz), 2.35 (1H, tt, J
= 12Hz, 4Hz), 2.06-1.97 (2H, m), 1.67-1.60 (2H, br.
m), 1.52-1.40 (2H, m), 0.92 (6H, d, J = 6Hz).

[0290]

Working Example 56 2- (4-fluorophenyl) -4-
(1-propyl-1,2,3,6 -tetrahydropyridi
-4-yl) -3- (pyridin-4-yl) -1H-
Pyrrole (Exemplified Compound No. 1-2630) Coupling reaction in the same manner as in Examples 9-1) and 3) using 1-propylpiperidin-4-one as a starting material instead of 1-benzylpiperidin-4-one. , A dehydration reaction and a desilyl reaction were sequentially performed to obtain the title compound as a white powder (yield: 46%).

Melting point: 236-238 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.36 (1H, br.s), 8.45 (2H, d, J =
6Hz), 7.18-7.08 (6H, m), 6.90 (1H, d, J = 3Hz), 5.26-
5.23 (1H, m), 2.84-2.79 (2H, m), 2.44 (2H, t, J = 5H
z), 2.25 (2H, t, J = 8Hz), 2.17-2.11 (2H, br.m), 1.43
(2H, t, quartet, J = 8Hz, 8Hz), 0.84 (3H, t, J = 8H
z).

[0292]

Example 57 4- (1-benzyl-1,2,3,6
-Tetrahydropyridin -4-yl) -2- (4-fur
Orofeniru) -3- (pyridin-4-yl) - 1H-
Pyrrole (Exemplified Compound No. 1-2644) 4- (1-benzyl-4-hydroxypiperidin-4-yl) -2- (4-fluorophenyl) -3- (pyridine-4) obtained in Example 9-1) Example 9-3) using (-yl) -1-triisopropylsilyl-1H-pyrrole
The dehydration reaction and the desilyl reaction were sequentially performed in the same manner as in the above, to give the title compound as a slightly yellow powder (yield 88%).

Melting point: 217-219 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.37 (1H, br.s), 8.45 (2H, d, J =
6Hz), 7.34-7.21 (5H, m), 7.18-7.08 (6H, m), 6.90 (1
H, d, J = 3Hz), 5.23-5.21 (1H, br.m), 3.50 (2H, s),
2.86-2.81 (2H, br.m), 2.48 (2H, t, J = 6Hz), 2.18-2.1
2 (2H, br.m).

[0294]

Working Example 58 2- (4-Fluorophenyl) -4-
(1-phenethyl- 1,2,3,6-tetrahydropyri
Zin-4-yl) -3- (pyridin-4-yl) -1H
- Similar to the pyrrole (Compound No. 1-2645) 1-1-phenethyl-4-one in place of benzyl piperidin-4-one used as starting material in Example 9-1) and 3), the coupling The reaction, dehydration reaction and desilyl reaction were sequentially performed to obtain the title compound as a slightly brown powder (yield 46%).

Melting point: 219-221 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.37 (1H, br.s), 8.45 (2H, d, J =
6Hz), 7.29-7.09 (11H, m), 6.90 (1H, d, J = 3Hz), 5.28
-5.24 (1H, br.m), 2.95-2.89 (2H, br.m), 2.76-2.69
(2H, m), 2.57-2.51 (4H, m), 2.19-2.12 (2H, br.m).

[0296]

Example 59 (±) -2- (4-fluorophenyl)
) -4- ( 1,2,3,5,8,8a-hexahydro
Indolizin-7-yl) -3- (pyridine-4- i
) -1H-pyrrole (Exemplary Compound No. 1-2654) Instead of 1-benzylpiperidin-4-one, (±)-
Example 9-Using 1,2,3,5,6,7,8,8a-octahydroindolizin-7-one as a starting material
A coupling reaction, a dehydration reaction, and a desilyl reaction were sequentially performed in the same manner as in 1) and 3) to obtain a mixture of the title compound and its isomer (the compound of Example 60). This mixture was subjected to silica gel column chromatography (solvent; ethyl acetate: methanol: isopropylamine = 10: 1:
1) to give the title compound (Rf value 0.50) as a white powder (yield 24%).

Melting point: 220-222 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, CD ₃ O
D) δppm: 8.36 (2H, d, J = 6Hz), 7.24 (2H, d, J =
6Hz), 7.17 (2H, dd, J = 9Hz, 6Hz), 7.00 (2H, t, J = 9H
z), 6.85 (1H, s), 5.41-5.37 (1H, m), 3.47-3.40 (1H,
m), 3.18-3.12 (1H, m), 2.84-2.77 (1H, m), 2.40-2.2
6 (2H, m), 2.23-2.11 (2H, m), 2.05-1.97 (1H, m), 1.
90-1.75 (2H, m), 1.46-1.36 (1H, m).

[0298]

Working Example 60 (±) -2- (4-Fluorophenyl)
) -4- ( 1,2,3,5,6,8a-hexahydro
Indolizin-7-yl) -3- (pyridine-4- i
L ) -1H-pyrrole (Exemplary Compound No. 1-2653) The title compound (Rf value 0.40) was obtained as a slightly yellow powder by silica gel column chromatography performed in Example 59 (yield 27%).

Melting point: 188-190 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, CD ₃ O
D) δppm: 8.37 (2H, d, J = 6Hz), 7.23 (2H, d, J =
6Hz), 7.18 (2H, dd, J = 9Hz, 5Hz), 7.00 (2H, t, J = 9H
z), 6.86 (1H, s), 5.34-5.30 (1H, br.m), 3.38-3.30
(1H, m), 2.99-2.86 (2H, m), 2.82-2.73 (2H, m), 2.40
-2.31 (1H, m), 2.25-2.16 (1H, m), 1.97-1.86 (2H,
m), 1.84-1.73 (1H, m), 1.48-1.38 (1H, m).

[0300]

Example 61 (±) -4- (1,6-dimethyl-
2,3,6 Tetorahi Doropirijin 4-yl) -
2- (4-fluorophenyl) -3- (pyridine- 4-
Il) -1H-pyrrole (exemplary compound number 1-266)
6) Instead of 1-benzylpiperidin-4-one, (±)-
Using 1,2-dimethylpiperidin-4-one as a starting material, a coupling reaction, a dehydration reaction and a desilyl reaction were sequentially performed in the same manner as in Examples 9-1) and 3) to give the title compound and its isomers (Compound of Example 62) was obtained. The mixture is subjected to silica gel column chromatography (solvent; ethyl acetate: isopropylamine = 9).
9: 1) to give the title compound (Rf value 0.40) as a pale yellow powder (yield 10%).

Melting point: 208-209 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl ₃
) Δ ppm: 8.47 (2H, d, J = 6Hz), 8.29-8.10 (1H, b
rs), 7.17 (2H, d, J = 6Hz), 7.13 (2H, dd, J = 9Hz, 5H
z), 6.97 (2H, t, J = 9Hz), 6.83 (1H, d, J = 3Hz), 5.19
(1H, s), 2.90-2.83 (1H, m), 2.55-2.32 (2H, m), 2.3
7 (3H, s), 2.17-2.07 (2H, m), 1.05 (3H, d, J = 7Hz).

[0302]

Example 62 (±) -4- (1,2-dimethyl-
2,3,6 Tetorahi Doropirijin 4-yl) -
2- (4-fluorophenyl) -3- (pyridine- 4-
Il) -1H-pyrrole (exemplary compound number 1-270)
8) The title compound (Rf value 0.30) was obtained as a pale yellow powder by silica gel column chromatography performed in Example 61 (yield 14%).

Melting point: 198-201 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl ₃
) Δppm: 8.47 (2H, d, J = 6Hz), 8.33 (1H, br.s),
7.17 (2H, d, J = 6Hz), 7.12 (2H, dd, J = 9Hz, 5Hz), 6.
97 (2H, t, J = 9Hz), 6.82 (1H, d, J = 3Hz), 5.40 (1H,
s), 3.22-3.18 (1H, m), 2.95-2.91 (1H, m), 2.57-2.46
(1H, m), 2.34 (3H, s), 2.27-2.23 (1H, m), 2.11-2.0
9 (1H, m), 1.08 (3H, d, J = 6Hz).

[0304]

Working Example 63 2- (4-Fluorophenyl) -4-
(1,2,2,6,6- pentamethyl-1,2,3,6
- tetrahydropyridin-4-yl) -3- (Pi lysine
-4-yl) -1H-pyrrole (exemplary compound number 1-2)
651) 1, 2,2 instead of 1-benzylpiperidin-4-one
Using 2,6,6-pentamethylpiperidin-4-one as a starting material, a coupling reaction, a dehydration reaction, and a desilyl reaction were sequentially performed in the same manner as in Examples 9-1) and 3) to give the title compound. Obtained as a white powder (yield 69
%).

Melting point: 264-268 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.38 (1H, br.s), 8.43 (2H, d, J =
6Hz), 7.20-7.09 (6H, m), 6.88 (1H, d, J = 3Hz), 4.88
(1H, s), 2.18 (3H, s), 2.07 (2H, s), 1.01 (6H, s),
0.90 (6H, s).

[0306]

Working Example 64 2- (4-Fluorophenyl) -4-
(1,2,2,6,6- pentamethylpiperidine-4-
Yl) -3- (pyridin-4-yl)-1H-pin roll <br/> (Compound No. 1-2652) 2- (4-fluorophenyl) -4- (1,2,2,
6,6-pentamethyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl)-
A reduction reaction was carried out in the same manner as in Example 11 using 1H-pyrrole (the compound of Example 63) to obtain the title compound as a white powder (yield: 82%).

Melting point: 248-250 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.19 (1H, br.s), 8.47 (2H, d, J =
6Hz), 7.21-7.15 (4H, m), 7.11 (2H, t, J = 9Hz), 6.73
(1H, d, J = 2Hz), 2.91-2.82 (1H, m), 2.14 (3H, s), 1.
54-1.47 (2H, m), 1.36 (2H, t, J = 13Hz), 1.01 (6H,
s), 0.86 (6H, s).

[0308]

Working Example 65 2- (4-Fluorophenyl) -3-
(Pyridin-4-yl) -4- (1,2,3,6-tet
Lahydropyridin -5-yl) -1H-pyrrole (Exemplary Compound No. 1-2627) Example 9-1 using 1-benzylpiperidin-3-one as a starting material instead of 1-benzylpiperidin-4-one. The coupling reaction, debenzylation reaction, dehydration reaction, and desilyl reaction were sequentially performed in the same manner as in (2) and (3) to obtain the title compound as a slightly brown powder (yield 12%).

Melting point: 230-233 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (500 MHz, CD ₃ O
D) δppm: 8.36 (2H, d, J = 6Hz), 7.24 (2H, d, J =
6Hz), 7.18 (2H, dd, J = 9Hz, 6Hz), 7.01 (2H, t, J = 9H
z), 6.82 (1H, s), 5.55-5.50 (1H, br.m), 3.36-3.30
(2H, m), 2.90 (2H, t, J = 6Hz), 2.16-2.09 (2H, br.
m).

[0310]

Example 66 4- (3-Dimethylamino-1-pro
Pen-1-yl) -2- (4-fluorophenyl) -3
-(Pyridin-4-yl) -1H-pyrrole (Exemplary Compound No. 1-2519) 1) 2- (4-fluorophenyl) -4- (3- hydrido)
Roxy-1-propen- 1-yl) -3- (pyridine-
4-yl) -1H-pyrrole 3-[[2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole] -4-yl] acryl obtained in Example 23-1). Acid ethyl ester 3.88
g (12.5 mmol) was dissolved in 120 ml of dichloromethane, and 27.6 ml of a 1M diisobutylaluminum hydride / dichloromethane solution was stirred under cooling at −78 ° C.
(27.6 mmol) was slowly added dropwise. Thereafter, the mixture was stirred at the same temperature for 3 hours, and the reaction mixture was added to a saturated aqueous solution of sodium hydrogen carbonate, followed by filtration. The filtrate was extracted with dichloromethane, the organic layer was washed with water, dried over anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure. The residue was subjected to silica gel column chromatography (solvent; hexane: ethyl acetate = 1: 1).
9) to give 3.42 g of the title compound as a light brown powder (93% yield) ¹ H-nuclear magnetic resonance spectrum (400 MHz, CD ₃ O).
D) δ ppm: 8.41 (2H, d, J = 6Hz), 7.23 (2H, d, J =
6Hz), 7.20 (2H, dd, J = 9Hz, 5Hz), 7.08 (1H, s), 7.01
(2H, t, J = 9Hz), 6.39 (1H, d, J = 16Hz), 5.98 (1H, d
t, J = 16Hz, 6Hz), 4.09 (2H, dd, J = 6Hz, 1Hz). 2) 3-[[2- (4-fluorophenyl) -3-
(Pyridin-4-yl) -1H-pyrrole] -4-i
Le] was obtained in an acrylic aldehyde 1) 2- (4-fluorophenyl) -4- (3-
Hydroxy-1-propen-1-yl) -3- (pyridin-4-yl) -1H-pyrrole 1.63 g (5.54)
mmol) in 80 ml of dimethyl sulfoxide,
Add 16.32 g of activated manganese dioxide and add at room temperature
Stirred for hours. Ethyl acetate was added to the reaction mixture, followed by filtration. Water was added to the filtrate, and the mixture was extracted with ethyl acetate. After the organic layer was washed with water and dried over anhydrous magnesium sulfate, the solvent was distilled off under reduced pressure, and the residue was washed with dichloromethane to obtain 1.36 g of the title compound as a pale brown powder (yield: 84).
%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CD ₃ OD-CDCl ₃ ) δ ppm: 9.42 (1H, d, J
= 8Hz), 8.51 (2H, d, J = 6Hz), 7.49 (1H, s), 7.45 (1H,
d, J = 16Hz), 7.27 (2H, d, J = 6Hz), 7.22 (2H, dd, J = 9
Hz, 5Hz), 7.01 (2H, t, J = 9Hz), 6.39 (1H, dd, J = 16H
z, 8Hz). 3) 4- (3-dimethylamino-1-propene-1-
Yl) -2- (4-full Orofeniru) -3- (pyrid
Down-4-yl)-1H-obtained in pyrrole 2) 3 - [[2- (4-fluorophenyl) -3
-(Pyridin-4-yl) -1H-pyrrole] -4-yl] acrylaldehyde 700 mg (2.38 mmol
1) and 1.95 g (23.8 m) of dimethylamine hydrochloride
mol) in methanol-tetrahydrofuran (1: 1)
The mixture was dissolved in 110 ml of the mixture, 226 mg (3.59 mmol) of sodium cyanotrihydroborate was further added, and the mixture was stirred at room temperature for 19 hours. The reaction mixture was added to a saturated aqueous solution of sodium hydrogen carbonate, and extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous magnesium sulfate, concentrated under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent; ethyl acetate: methanol: isopropylamine = 20: 1: 1) to give the title compound 429.
mg was obtained as a white powder (56% yield).

Melting point: 196-198 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, CD ₃ OD)
−CDCl ₃ ) δ ppm: 8.42 (2H, d, J = 6 Hz), 7.23
(2H, d, J = 6Hz), 7.20 (2H, dd, J = 9Hz, 5Hz), 7.09 (1
H, s), 6.98 (2H, t, J = 9Hz), 6.35 (1H, d, J = 16Hz),
5.88 (1H, dt, J = 16Hz, 7Hz), 3.04 (2H, d, J = 7Hz), 2.
27 (6H, s).

[0313]

Working Example 67 4- (4-aminobutyl) -2- (4
-Fluorophenyl) -3- (pyridin-4-yl)-
1H-pyrrole (Exemplified Compound No. 1-98) 1) 4- (3-cyanopropyl) -2- (4-fluoro
Rofeniru) -3- (Pi lysine-4-yl)-1H-pin
Roll 2- (4-fluorophenyl) obtained in Example 23-4)
3.04 g (7.26 mmol) of -3- (pyridin-4-yl) -4- [3- (p-toluenesulfonyloxy) propyl] -1H-pyrrole is dissolved in 60 ml of N, N-dimethylformamide, and further dissolved. Potassium cyanide 5
68 mg (8.72 mmol) were added,
Stirred for hours. After the reaction mixture was cooled to room temperature, a saturated aqueous solution of sodium hydrogencarbonate was added,
Extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous magnesium sulfate, concentrated under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent; hexane: ethyl acetate = 2: 1) to give the title compound (0.94 g) as pale yellow Obtained as a powder (42% yield).

The ¹ H-nuclear magnetic resonance spectrum (500 MH
z, CDCl ₃ ) δ ppm: 8.53 (2H, d, J = 6 Hz), 8.25
(1H, br.s), 7.13 (2H, dd, J = 9Hz, 5Hz), 7.12 (2H,
d, J = 6Hz), 6.97 (2H, t, J = 9Hz), 6.75 (1H, d, J = 3H
z), 2.70 (2H, t, J = 7Hz), 2.28 (2H, t, J = 7Hz), 1.76
(2H, quintet, J = 7Hz). 2) 4- (4-aminobutyl) -2- (4-fluoro
Phenyl) -3- (pyrimidin Jin-4-yl)-1H-pyro
Lumpur lithium aluminum hydride 468 mg (12.32
mmol) in 100 ml of tetrahydrofuran,
While stirring at room temperature, 0.94 g of the 4- (3-cyanopropyl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole obtained in 1) (3.08)
(mmol) of tetrahydrofuran was added dropwise. After heating to 60 ° C. and stirring for 3 hours, the mixture was cooled to room temperature, and 0.47 ml of a 15% aqueous sodium hydroxide solution and 20 ml of water were gradually added. The reaction mixture was filtered, the filtrate was concentrated under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent; ethyl acetate: isopropylamine = 25: 1) to obtain 410 mg of the title compound as a slightly red powder ( Yield 43%).

Melting point: 185-187 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDC
l ₃ ) δ ppm: 10.02 (1H, br.s), 8.49 (2H, d, J = 4H
z), 7.19 (2H, dd, J = 9Hz, 5Hz), 7.14 (2H, d, J = 4Hz),
6.94 (2H, t, J = 9Hz), 6.72 (1H, d, J = 2Hz), 2.65 (2
H, t, J = 7Hz), 2.51 (2H, d, J = 7Hz), 2.46-2.08 (2H,
m), 1.52-1.46 (4H, m).

[0316]

Working Example 68 1- (2-Dimethylaminoethyl)-
3- (4-Furuorofe) -2- (pyridin-4
Il) -1H-pyrrole (Exemplified Compound No. 2-108) Same as in Examples 12-1), 2) and 3) using 2-dimethylaminoethylamine as a starting material instead of 4-amino-1-benzylpiperidine Were sequentially performed to obtain the title compound as a slightly brown powder (yield: 8).
%).

Melting point: 70-73 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDC
l ₃ ) δppm: 8.60 (2H, d, J = 6Hz), 7.19 (2H, d, J
= 6Hz), 7.07 (2H, dd, J = 9Hz, 5Hz), 6.89 (2H, t, J = 9H
z), 6.88 (1H, d, J = 3Hz), 6.36 (1H, d, J = 3Hz), 3.96
(2H, t, J = 7Hz), 2.48 (2H, t, J = 7Hz), 2.15 (6H,
s).

[0318]

Working Example 69 1- (2,2-Dimethyl-3-dimethyl)
Ruaminopropyl) -3- (4-fluorophenyl)-
2- (pyridin-4-yl) -1H-pyrrole (Exemplary Compound No. 2-2626) Instead of 4-amino-1-benzylpiperidine, 2,2
The same reaction as in Examples 12-1), 2) and 3) was successively performed using -dimethyl-3-dimethylaminopropylamine as a starting material to obtain the title compound as a white powder (yield 21%). .

Melting point: 101-103 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDC
l ₃ ) δppm: 8.58 (2H, d, J = 6Hz), 7.14 (2H, d, J
= 6Hz), 7.04 (2H, dd, J = 9Hz, 5Hz), 6.88 (2H, t, J = 9H
z), 6.84 (1H, d, J = 3Hz), 6.32 (1H, d, J = 3Hz), 3.90
(2H, s), 2.22 (6H, s), 2.00 (2H, s), 0.64 (6H,
s).

[0320]

Embodiment 701- (8-Azabicyclo- [3.2.
1] Octan-3-yl ) -3- (4-Fluorophenyl)
) -2- (pyridin-4-yl) -1H-pyro Rule
(Exemplified Compound No. 2-2541) Instead of 4-amino-1-benzylpiperidine, 3-A
Mino-8-benzyl-8-azabicyclo [3.2.1]
Example 12-1) using octane as a starting material,
Perform the same reaction as in 2) and 3) sequentially to give the title compound
The N-benzyl form of was obtained. Then, using this, Example 9
Perform debenzylation reaction in the same manner as in -2),
Was obtained as a white powder (yield 90%).

Melting point: 204-205 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDC
l ₃ ) δppm: 8.60 (2H, d, J = 6Hz), 7.14 (2H, d, J
= 6Hz), 7.02 (2H, dd, J = 9Hz, 5Hz), 6.88 (1H, d, J = 3H
z), 6.86 (2H, t, J = 9Hz), 6.38 (1H, d, J = 3Hz), 4.36
4.25 (1H, m), 3.67-3.53 (2H, m), 2.51-2.39 (2H,
m), 1.90-1.67 (4H, m), 1.57-1.47 (2H, m).

[0322]

Example 71 (±) -3- (4-Fluorophenyl)
Le) -1- (2-methylpiperidin Perijin 4-yl) -2-
(Pyridin-4-yl) -1H-pyrrole (Exemplified Compound No. 2-2522) Instead of 4-amino-1-benzylpiperidine, (±)
Examples 12-1), 2) and 3) using -4-amino-1-benzyl-2-methylpiperidine as starting material
Were successively performed to obtain an N-benzyl compound of the title compound. Then, the compound was subjected to a debenzylation reaction in the same manner as in Example 9-2) to give the title compound as a white powder (yield: 24%).

Melting point: 173-175 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDC
l ₃ ) δppm: 8.61 (2H, d, J = 5Hz), 7.15 (1H, d, J
= 5Hz), 7.14 (1H, d, J = 5Hz), 7.07-7.03 (2H, m), 7.00
(0.5H, d, J = 3Hz), 6.95 (0.5H, d, J = 3Hz), 6.88 (2H,
t, J = 9Hz), 6.38 (1H, d, J = 3Hz), 4.30-4.26 (0.5H,
m), 4.00-3.91 (0.5H, m), 3.47-3.39 (0.5H, m), 3.17-
3.15 (0.5H, m), 2.98-2.88 (1H, m), 2.66-2.61 (1H,
m), 2.06-1.76 (4H, m), 1.11 (1.5H, d, J = 7Hz), 1.08
(1.5H, d, J = 7Hz).

[0324]

Working Example 72 3- (4-Fluorophenyl) -2-
(2-methylamino-pyrimidin Jin-4-yl) -1- (piperazinyl
Lysin -4-yl) -1H-pyrrole (Exemplary Compound No. 2-2042) 1) 1- (1-benzylpiperidin-4-yl) -3
- (4-fluoro-phenylcarbamoyl) -2- (2-Furuoropiri
Reaction similar to Example 12-1), 2) and 3) using 2-fluoropyridine-4-carboxaldehyde as a starting material instead of (zin- 4-yl) -1H-pyrrolepyridine -4-carboxaldehyde Was sequentially performed to obtain the title compound as a pale brown powder (yield 49%).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.20 (1H, d, J = 5 Hz), 7.37
-7.24 (5H, m), 7.04 (2H, dd, J = 9Hz, 5Hz), 7.02-6.96
(2H, m), 6.90 (2H, t, J = 9Hz), 6.75 (1H, s), 6.37
(1H, d, J = 3Hz), 3.89-3.78 (1H, m), 3.52 (2H, s), 3.
01-2.96 (2H, m), 2.12-1.96 (4H, m), 1.94-1.86 (2H, m
m). 2) 1- (1-benzylpiperidin-4-yl) -3
- (4-fluoro-phenylcarbamoyl) -2- (2-methylamino
1- (1-Benzylpiperidin-4-yl) obtained in 1) pyridin-4-yl) -1H-pyrrole
-3- (4-Fluorophenyl) -2- (2-fluoropyridin-4-yl) -1H-pyrrole 1.50 g
(3.49 mmol) in tetrahydrofuran solution 30 m
1 and 2M methylamine / tetrahydrofuran solution 50
ml (100 mmol) and stirred at 150 ° C. for 28 hours in an autoclave. The solvent was distilled off from the reaction mixture under reduced pressure, ethyl acetate and water were added to the residue, and the mixture was separated, and the organic layer was collected. This was dried over anhydrous magnesium sulfate, concentrated under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent; dichloromethane: methanol = 20: 1) to give 1.83 g of the title compound as a pale brown amorphous solid. (60% yield).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.10 (1H, d, J = 5 Hz), 7.35
-7.23 (5H, m), 7.12 (2H, dd, J = 9Hz, 5Hz), 6.92 (1H,
d, J = 3Hz), 6.88 (2H, t, J = 9Hz), 6.48 (1H, d, J = 5H
z), 6.37 (1H, d, J = 3Hz), 6.20 (1H, s), 4.66-4.57 (1
H, m), 3.93-3.84 (1H, m), 3.51 (2H, s), 2.99-2.91
(2H, m), 2.84 (3H, d, J = 5Hz), 2.06-1.85 (6H, m). 3) 3- (4-fluorophenyl) -2- (2-methyl
Ruaminopyridin-4- yl) -1- (piperidine-4
-Yl) -1H-pyrrole 1- (1-benzylpiperidin-4-yl) obtained in 2)
A debenzylation reaction was carried out in the same manner as in Example 9-2) using -3- (4-fluorophenyl) -2- (2-methylaminopyridin-4-yl) -1H-pyrrole to give the title compound. Obtained as a white powder (52% yield).

Melting point: 165-167 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDC
l ₃ ) δppm: 8.12 (1H, d, J = 5Hz), 7.13 (2H, dd,
J = 9Hz, 5Hz), 6.93 (1H, d, J = 3Hz), 6.88 (2H, t, J = 9H
z), 6.49 (1H, dd, J = 5Hz, 1Hz), 6.38 (1H, d, J = 3Hz),
6.21 (1H, d, J = 1Hz), 4.65-4.55 (1H, m), 4.02-3.97
(1H, m), 3.16 (2H, br.d, J = 12Hz), 2.85 (3H, d, J = 5
Hz), 2.60 (2H, dt, J = 12Hz, 3Hz), 1.99-1.81 (4H,
m).

[0328]

Working Example 73 2- (4-Fluorophenyl) -3-
[2- (1 (S) --phenyl ethylamino) pyridine -
4-yl] -4- (1,2,3,6 Tetorahido Ropiri
Zin-4-yl) -1H-pyrrole (Exemplary Compound No. 1)
-2600) 1) 4-Bromo-2- (4-fluorophenyl) -3
- (2-Furuoropiriji down-4-yl) -1-triiso
Example 1 using 3- (2-fluoropyridin-4-yl) acrylic acid ethyl ester as a starting material instead of propylsilyl-1H-pyrrole 3- (4-pyridyl) acrylic acid ethyl ester
-1), 7-1), 7-2) and 7-3), a pyrrole ring formation reaction, a decarboxylation reaction, a silylation reaction, and a bromination reaction were sequentially performed to give the title compound as a pale yellow powder. (48% yield).

¹ H-nuclear magnetic resonance spectrum (400 MH
z, DMSO-d ₆ ) δ ppm: 8.05 (1H, d, J = 5 Hz),
7.38 (2H, dd, J = 9Hz, 5Hz), 7.20 (2H, t, J = 9Hz), 7.1
5 (1H, s), 7.01-6.97 (1H, m), 6.78 (1H, s), 1.20-1.
07 (3H, m), 0.99 (18H, d, J = 7Hz). 2) 4- (1-allyloxycarbonyl-1,2,2
3,6 tetrahydropyridyl Jin-4-yl) -2- (4
- fluorophenyl) -3- (2-Furuoropiriji down -
4-yl) -1H-pyrrole 4-bromo-2- (4-fluorophenyl) -3- (pyridin-4-yl) -1-triisopropylsilyl-1
Instead of H-pyrrole, 4-bromo-2- obtained in 1)
(4-Fluorophenyl) -3- (2-fluoropyridin-4-yl) -1-triisopropylsilyl-1H-
Coupling reaction, dehydration reaction and desilyl reaction of pyrrole in the same manner as in Examples 9-1) and 9-3) using 1-allyloxycarbonylpiperidin-4-one instead of 1-benzylpiperidin-4-one. The reaction was sequentially performed to obtain the title compound as a white powder (yield: 6%).

The ¹ H-nuclear magnetic resonance spectrum (500 MH
z, CDCl ₃ ) δ ppm: 8.42-8.31 (1H, br.s), 8.0
9 (1H, d, J = 5Hz), 7.15 (2H, dd, J = 9Hz, 5Hz), 7.04-
6.97 (3H, m), 6.82 (1H, s), 6.77 (1H, s), 6.00-5.89
(1H, m), 5.63-5.39 (1H, m), 5.31 (1H, d, J = 16Hz),
5.21 (1H, d, J = 11Hz), 4.62 (2H, d, J = 5Hz), 4.04-3.9
6 (2H, br.s), 3.63-3.52 (2H, br.s), 2.29-2.12 (2H, br.s)
m). 3) 4- (1-allyloxycarbonyl-1,2,2,
3,6 tetrahydropyridyl Jin-4-yl) -2- (4
- fluorophenyl) -3- [2- (1 (S ) - off E D
Ruethylamino) pyridin-4-yl] -1H-pillow
Obtained in Le 2) 4- (1-allyloxycarbonyl-1,
2,3,6-tetrahydropyridin-4-yl) -2-
360 mg of (4-fluorophenyl) -3- (2-fluoropyridin-4-yl) -1H-pyrrole (0.85
mmol) and 3.6 m of 1 (S) -phenylethylamine
1 (28.3 mmol) and 0.36 ml of concentrated hydrochloric acid
After stirring, the mixture was stirred at 150 ° C. for 10 hours. A saturated aqueous sodium hydrogen carbonate solution was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The extract is washed with water, dried over anhydrous magnesium sulfate, concentrated under reduced pressure, and the residue is subjected to silica gel column chromatography (solvent; hexane: ethyl acetate =
1: 1) to give 229 mg of the title compound as a brown amorphous solid (49% yield).

¹ H-nuclear magnetic resonance spectrum (500 MH
z, CDCl ₃ ) δ ppm: 8.20-8.12 (1H, br.s), 7.9
6 (1H, d, J = 5Hz), 7.25 (4H, s), 7.22-7.16 (1H, m),
7.04 (2H, dd, J = 9Hz, 5Hz), 6.89 (2H, t, J = 9Hz), 6.7
4 (1H, s), 6.44 (1H, d, J = 4Hz), 6.10 (1H, s), 6.00
-5.89 (1H, m), 5.54-5.33 (1H, m), 5.32 (1H, d, J = 16
Hz), 5.22 (1H, d, J = 11Hz), 5.05 (1H, br.d, J = 6Hz),
4.62 (2H, d, J = 5Hz), 4.54-4.46 (1H, m), 3.93-3.83
(2H, m), 3.50-3.38 (2H, m), 2.20-2.05 (2H, m), 1.48
(3H, d, J = 7Hz). 4) 2- (4-fluorophenyl) -3- [2- (1
(S) -phenylethylamino) pyridin-4-yl]
-4- (1,2,3,6-tetrahydropyridine -4-
Yl) -1H-pyrrole 4- (1-allyloxycarbonyl-1,
2,3,6-tetrahydropyridin-4-yl) -2-
229 mg (0.44 mmol) of (4-fluorophenyl) -3- [2- (1 (S) -phenylethylamino) pyridin-4-yl] -1H-pyrrole were added to dioxane-
Dissolved in 2.5 ml of a water (10: 1) mixture, 55 μl (0.66 mmol) of pyrrolidine and 5 mg (0.00) of tetrakis (triphenylphosphine) palladium (0)
44 mmol) and stirred at 0 ° C. for 10 minutes. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The extract was washed with water and concentrated under reduced pressure. The residue was subjected to silica gel column chromatography (solvent; ethyl acetate: methanol: isopropylamine = 10: 1: 1) to obtain 41 mg of the title compound as a slightly brown amorphous solid (yield 21).
%).

The ¹ H-nuclear magnetic resonance spectrum (500 MH
z, CDCl ₃ ) δ ppm: 8.19-8.01 (1H, br.s), 7.9
6 (1H, d, J = 5Hz), 7.26 (4H, s), 7.24-7.18 (1H, m),
7.06 (2H, dd, J = 9Hz, 5Hz), 6.89 (2H, t, J = 9Hz), 6.7
4 (1H, s), 6.47 (1H, d, J = 4Hz), 6.15 (1H, s), 5.47
(1H, d, J = 3Hz), 5.05 (1H, br.d, J = 6Hz), 4.60-4.52
(1H, m), 3.31-3.26 (2H, m), 2.94-2.84 (2H, m), 2.13
-2.07 (2H, m), 1.48 (3H, d, J = 7Hz).

[0333]

Working Example 74 4- (1-t-butyl-1,2,3,3)
6-tetrahydropyridinyl di emissions-4-yl) -2- (4-off
Fluorophenyl) -3- (pyridin-4-yl) -1H
- 1-t-instead of pyrrole (Compound No. 1-2635) 1-benzyl-4-one
Coupling reaction using butylpiperidin-4-one as a starting material in the same manner as in Examples 9-1) and 9-3),
The dehydration reaction and the desilyl reaction were sequentially performed to obtain the title compound as a pale yellow powder (yield: 20%).

Melting point: 242-244 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl _{3
-DMSO-d 6) δppm: 9.72} (1H, br.s), 8.46
(2H, d, J = 6Hz), 7.19 (2H, d, J = 6Hz), 7.16 (2H, dd,
J = 9Hz, 5Hz), 6.94 (2H, t, J = 9Hz), 6.81 (1H, d, J = 3H
z), 5.46 (1H, s), 3.19-3.11 (2H, m), 2.66-2.58 (2H,
m), 2.26-2.18 (2H, m), 1.10 (9H, s).

[0335]

Working Example 75 2- (4-Fluorophenyl) -4-
(1-octyl-1,2,3,6 -tetrahydropyridi
-4-yl) -3- (pyridin-4-yl) -1H-
Pyrrole (Exemplified Compound No. 1-2639) Coupling in the same manner as in Examples 9-1) and 9-3) using 1-octylpiperidin-4-one as a starting material instead of 1-benzylpiperidin-4-one. The reaction, dehydration reaction and desilyl reaction were sequentially performed to obtain the title compound as a white powder (yield 26%).

Melting point: 173-175 ° C. ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDC
l ₃ ) δ ppm: 8.47 (2H, d, J = 6 Hz), 8.29 (1H, br.
s), 7.17 (2H, d, J = 6Hz), 7.12 (2H, dd, J = 9Hz, 5Hz),
6.96 (2H, t, J = 9Hz), 6.82 (1H, d, J = 3Hz), 5.45 (1
H, s), 2.99 (2H, br.d, J = 3Hz), 2.56 (2H, t, J = 6Hz),
2.39 (2H, t, J = 8Hz), 2.28-2.23 (2H, m), 1.55-1.48
(2H, m), 1.31-1.22 (10H, m), 0.88 (3H, t, J = 7Hz).

[0337]

Example 76 (±) -4- (1-ethyl-6-methyl
Le-1,2,3,6-te tiger-tetrahydropyridine-4-Yi
) -2- (4-fluorophenyl) -3- (pyridinium Jin
-4-yl) -1H-pyrrole (exemplary compound number 1-2)
667) Instead of 1-benzylpiperidin-4-one, (±)-
Using 1-ethyl-2-methylpiperidin-4-one as a starting material, a coupling reaction, a dehydration reaction, and a desilyl reaction were sequentially performed in the same manner as in Examples 9-1) and 9-3) to give the title compound. Its isomer (compound of Example 77)
To obtain a mixture. This mixture was subjected to silica gel column chromatography (solvent; ethyl acetate: isopropylamine = 50: 1) to give the title compound (Rf 0.2
0) was obtained as a pale yellow powder (33% yield).

Melting point: 210-212 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDC
l ₃ ) δ ppm: 8.47 (2H, d, J = 6 Hz), 8.31 (1H, br.
s), 7.17 (2H, d, J = 6Hz), 7.13 (2H, dd, J = 9Hz, 5Hz),
6.97 (2H, t, J = 9Hz), 6.82 (1H, s), 5.27 (1H, s),
3.09-3.00 (1H, m), 2.97-2.88 (1H, m), 2.84-2.73 (1
H, m), 2.48-2.24 (3H, m), 2.22-2.11 (1H, m), 1.09
(3H, t, J = 7Hz), 1.04 (3H, d, J = 7Hz).

[0339]

Example 77 (±) -4- (1-ethyl-2-methyl)
Le-1,2,3,6-te tiger-tetrahydropyridine-4-Yi
) -2- (4-fluorophenyl) -3- (pyridinium Jin
-4-yl) -1H-pyrrole (exemplary compound number 1-2)
709) By silica gel column chromatography performed in Example 76, the title compound (Rf value: 0.15) was obtained as a pale orange powder (yield: 46%).

Melting point: 218-220 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDC
l ₃ ) δ ppm: 8.47 (2H, d, J = 6 Hz), 8.32 (1H, br.
s), 7.17 (2H, d, J = 6Hz), 7.12 (2H, dd, J = 9Hz, 5Hz),
6.96 (2H, t, J = 9Hz), 6.82 (1H, s), 5.44 (1H, s),
3.16-2.99 (2H, m), 2.90-2.79 (1H, m), 2.76-2.64 (1
H, m), 2.51-2.32 (2H, m), 2.03-1.98 (1H, m), 1.08
(3H, t, J = 7Hz), 1.01 (3H, d, J = 6Hz).

[0341]

Example 78 (±) -2- (4-fluorophenyl)
) -4- ( 1,2,3,5,6,7,8,8a-oct
Motor hydro indolizin-7-yl) -3- (pyridine down -
4-yl) -1H-pyrrole (Exemplary Compound No. 1-26)
55) (±) -2- (4-fluorophenyl) -4- (1,
2,3,5,8,8a-Hexahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole (the compound of Example 59) was subjected to a reduction reaction in the same manner as in Example 11 to obtain the title compound as a white powder (yield). 52%).

Melting point: 263-265 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, DMSO
−d ₆ ) δ ppm: 11.20 (1H, br.s), 8.48 (2H, d, J
= 6Hz), 7.18-7.12 (4H, m), 7.09 (2H, t, J = 9Hz), 6.76
(1H, d, J = 2Hz), 2.98-2.92 (1H, m), 2.92-2.86 (1H,
br.t, J = 8Hz), 2.46 (1H, tt, J = 13Hz, 3Hz), 1.98-1.4
5 (9H, m), 1.30-1.14 (2H, m).

[0343]

Example 79 (±) -4- (6-allyl-1-methyl)
Le-1,2,3,6-te tiger-tetrahydropyridine-4-Yi
) -2- (4-fluorophenyl) -3- (pyridinium Jin
-4-yl) -1H-pyrrole (exemplary compound number 1-2)
690) Instead of 1-benzylpiperidin-4-one, (±)-
Using 2-allyl-1-methylpiperidin-4-one as a starting material, a coupling reaction, a dehydration reaction, and a desilyl reaction were sequentially performed in the same manner as in Examples 9-1) and 9-3) to give the title compound. Its isomer (compound of Example 80)
To obtain a mixture. This mixture was subjected to silica gel column chromatography (solvent; ethyl acetate: isopropylamine = 100: 1) to give the title compound (Rf value 0.4
0) was obtained as a pale yellow powder (20% yield).

Melting point: 218-220 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.48 (2H, d, J = 6Hz), 8.39 (1H, br.
s), 7.17 (2H, d, J = 6Hz), 7.11 (2H, dd, J = 9Hz, 5Hz),
6.96 (2H, t, J = 9Hz), 6.83 (1H, d, J = 3Hz), 5.66-5.5
8 (1H, m), 5.34 (1H, s), 4.96 (1H, d, J = 10Hz), 4.90
(1H, d, J = 17Hz), 2.89-2.87 (1H, m), 2.71-2.67 (1
H, m), 2.46-2.43 (2H, m), 2.37 (3H, s), 2.35-2.32
(1H, m), 2.12-2.07 (2H, m).

[0345]

Working Example 80 (±) -4- (2-Allyl-1-methyl)
Le-1,2,3,6-te tiger-tetrahydropyridine-4-Yi
) -2- (4-fluorophenyl) -3- (pyridinium Jin
-4-yl) -1H-pyrrole (exemplary compound number 1-2)
732) By silica gel column chromatography performed in Example 79, the title compound (Rf value: 0.35) was obtained as a pale yellow powder (yield: 18%).

Melting point: 178-180 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.47 (2H, d, J = 6Hz), 8.38 (1H, br.
s), 7.17 (2H, d, J = 6Hz), 7.12 (2H, dd, J = 9Hz, 5Hz),
6.96 (2H, t, J = 9Hz), 6.82 (1H, d, J = 3Hz), 5.77-5.6
9 (1H, m), 5.39 (1H, s), 5.03 (1H, d, J = 4Hz), 5.00
(1H, s), 3.19-3.15 (1H, m), 2.99-2.95 (1H, m), 2.5
7-2.41 (1H, m), 2.36 (3H, s), 2.36-2.31 (1H, m), 2.
24-2.09 (3H, m).

[0347]

Example 81 (±) -4- (6-benzyl-1-me
Tyl-1,2,3,6- tetrahydropyridine-4-i
) -2- (4-fluorophenyl) -3- (Pi lysine
-4-yl) -1H-pyrrole (exemplary compound number 1-2)
696) Instead of 1-benzylpiperidin-4-one, (±)-
Using 2-benzyl-1-methylpiperidin-4-one as a starting material, a coupling reaction, a dehydration reaction, and a desilyl reaction were sequentially performed in the same manner as in Examples 9-1) and 9-3) to give the title compound. A mixture with the isomer (the compound of Example 82) was obtained. This mixture was subjected to silica gel column chromatography (solvent; ethyl acetate: isopropylamine = 100: 1) to give the title compound (Rf value 0.38) as a pale-yellow powder (yield 11%).

Melting point: 198-200 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.45 (2H, d, J = 6Hz), 8.28 (1H, br.
s), 7.20-7.12 (3H, m), 7.09 (2H, d, J = 6Hz), 7.10-7.
07 (2H, m), 6.97-6.91 (4H, m), 6.76 (1H, d, J = 3Hz),
5.24 (1H, s), 3.13-3.10 (1H, m), 2.94-2.89 (2H,
m), 2.51 (3H, s), 2.49-2.35 (3H, m), 2.11-2.05 (1
H, m).

[0349]

Example 82 (±) -4- (2-benzyl-1-me
Tyl-1,2,3,6- tetrahydropyridine-4-i
) -2- (4-fluorophenyl) -3- (Pi lysine
-4-yl) -1H-pyrrole (exemplary compound number 1-2)
738) By silica gel column chromatography performed in Example 81, the title compound (Rf value: 0.33) was obtained as a pale yellow powder (yield: 4%).

Melting point: 198-199 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.55 (1H, br.s), 8.43 (2H, d, J = 6H
z), 7.23 (2H, t, J = 7Hz), 7.16 (2H, t, J = 7Hz), 7.12
(2H, d, J = 6Hz), 7.10-7.05 (4H, m), 6.94 (2H, t, J = 9
Hz), 6.72 (1H, d, J = 3Hz), 5.40 (1H, s), 3.20-3.17
(1H, m), 3.08-3.04 (2H, m), 2.81-2.78 (1H, m), 2.46
(3H, s), 2.43-2.38 (1H, m), 2.10-2.00 (2H, m).

[0351]

Working Example 83 (−)-2- (4-Fluorophenyl)
) -4- ( 1,2,3,5,6,8a-hexahydro
Indolizin-7-yl) -3- (pyridine-4- i
) -1H-pyrrole (Exemplified Compound No. 1-2653) (±) -2- (4-fluorophenyl) -4- (1,
2,3,5,6,8a-hexahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole (the compound of Example 60) was fractionated by HPLC using an optically active column under the following conditions, and the title compound (retention time 4.51 minutes) Was obtained as a pale yellow powder (recovery 94
%).

Melting point: 204-205 ° C. (decomposition) [α] ²⁷ _D- 50.67 # (C = 0.975, methanol) <HPLC conditions> Column: CHIRALPAK AD (manufactured by Daicel Chemical Industries, Ltd., inner diameter 0) .46 cm, length 25 cm) Mobile phase: n-hexane / ethanol = 80/20 Flow rate: 1.0 ml / min. Temperature: 40 ° C. Detection: 254 nm (UV).

[0353]

Working Example 84 (+)-2- (4-Fluorophenyl)
) -4- ( 1,2,3,5,6,8a-hexahydro
Indolizin-7-yl) -3- (pyridine-4- i
L ) -1H-pyrrole (Exemplary Compound No. 1-2653) In the fractionation by HPLC performed in Example 83, the title compound (retention time: 6.23 minutes) was obtained as a pale yellow powder (recovery rate: 95%). .

Melting point: 207-210 ° C. (decomposition) [α] ²⁴ _D +46.59 (C = 0.920, methanol) <HPLC conditions> As described in Example 83.

[0355]

Working Example 85 (±) -2- (4-Fluorophenyl)
) -4- (6-Methyl- 1-propyl-1,2,3,
6-tetrahydropyridin-4-yl) -3- (Pi lysine
N-4-yl) -1H-pyrrole (exemplary compound number 1-
2668) Instead of 1-benzylpiperidin-4-one, (±)-
Using 2-methyl-1-propylpiperidin-4-one as a starting material, a coupling reaction, a dehydration reaction, and a desilyl reaction were sequentially performed in the same manner as in Examples 9-1) and 9-3) to give the title compound. A mixture with the isomer (the compound of Example 86) was obtained. This mixture was subjected to silica gel column chromatography (solvent; ethyl acetate: isopropylamine = 100: 1) to give the title compound (Rf value 0.35) as a white powder (yield 6%).

Melting point: 214-215 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.47 (2H, d, J = 6Hz), 8.22 (1H, br.
s), 7.17 (2H, d, J = 6Hz), 7.13 (2H, dd, J = 9Hz, 5Hz),
6.97 (2H, t, J = 9Hz), 6.83 (1H, s), 5.27 (1H, s),
3.07-2.98 (1H, m), 2.97-2.89 (1H, m), 2.68-2.56 (1
H, m), 2.47-2.39 (1H, m), 2.37-2.23 (2H, m), 2.20-
2.10 (1H, m), 1.62-1.43 (2H, m), 1.04 (3H, d, J = 7H
z), 0.90 (3H, t, J = 7Hz).

[0357]

Working Example 86 (±) -2- (4-Fluorophenyl)
) -4- (2-Methyl- 1-propyl-1,2,3,
6-tetrahydropyridin-4-yl) -3- (Pi lysine
N-4-yl) -1H-pyrrole (exemplary compound number 1-
2710) The title compound (Rf value 0.32) was obtained as a white powder by silica gel column chromatography performed in Example 85 (yield 8%).

Melting point: 210-218 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.47 (2H, d, J = 6Hz), 8.23 (1H, br.
s), 7.17 (2H, d, J = 6Hz), 7.12 (2H, dd, J = 9Hz, 5Hz),
6.96 (2H, t, J = 9Hz), 6.82 (1H, s), 5.43 (1H, s),
3.16-3.01 (2H, m), 2.89-2.82 (1H, m), 2.58-2.50 (1
H, m), 2.42-2.30 (2H, m), 2.00-1.92 (1H, m), 1.57-
1.45 (2H, m), 1.01 (3H, d, J = 6Hz), 0.90 (3H, t, J = 7
Hz).

[0359]

Working Example 87 (±) -2- (4-Fluorophenyl)
) -4- ( 1,3,4,6,7,9a-hexahydro
-2H-quinolizin-8-yl) -3- (pyridine- 4
-Yl ) -1H-pyrrole (Exemplary Compound No. 1-265)
6) Instead of 1-benzylpiperidin-4-one, (±)-
Coupling reaction, dehydration reaction and desilyl reaction were sequentially performed in the same manner as in Examples 9-1) and 9-3) using octahydroquinolizin-2-one as a starting material, and the title compound and its isomer ( (Compound of Example 88). This mixture was subjected to silica gel column chromatography (solvent; ethyl acetate: isopropylamine = 10).
0: 1) to give the title compound (Rf value 0.35) as a pale-yellow powder (yield 6%).

Melting point: 223-224 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.47 (2H, d, J = 6Hz), 8.30 (1H, br.
s), 7.17 (2H, d, J = 6Hz), 7.12 (2H, dd, J = 9Hz, 5Hz),
6.96 (2H, t, J = 9Hz), 6.83 (1H, d, J = 3Hz), 5.13 (1
H, s), 2.88-2.81 (2H, m), 2.67-2.56 (1H, m), 2.45-
2.43 (1H, m), 2.40-2.35 (1H, m), 2.17-2.07 (2H, m),
1.76-1.73 (1H, m), 1.69-1.64 (2H, m), 1.44-1.41 (1
H, m), 1.34-1.18 (2H, m).

[0361]

Working Example 88 (±) -2- (4-Fluorophenyl)
) -4- ( 1,3,4,6,9,9a-hexahydro
-2H-quinolizin-8-yl) -3- (pyridine- 4
-Yl ) -1H-pyrrole (Exemplary Compound No. 1-265)
7) By silica gel column chromatography performed in Example 87, the title compound (Rf value: 0.30) was obtained as a pale yellow powder (yield: 19%).

Melting point: 228-234 ° C. ¹ H-nuclear magnetic resonance spectrum (500 MHz, CDCl
₃ ) δppm: 8.47 (2H, d, J = 6Hz), 8.28 (1H, br.
s), 7.17 (2H, d, J = 6Hz), 7.12 (2H, dd, J = 9Hz, 5Hz),
6.96 (2H, t, J = 9Hz), 6.81 (1H, d, J = 3Hz), 5.42 (1
H, s), 3.30-3.25 (1H, m), 2.98-2.95 (1H, m), 2.77-
2.73 (1H, m), 2.14-1.99 (5H, m), 1.74-1.65 (3H, m),
1.31-1.21 (2H, m).

[0363]

Working Example 89 (±) -2- (4-Fluorophenyl)
) -4- ( 1,2,3,5,8,8a-hexahydro
Indolizine-7-yl) -3- (2-Mechiruami Bruno pin
Limidin-4-yl) -1H-pyrrole (Exemplified Compound No. 1-2906) 4-bromo-2- (4-fluorophenyl) -3- (pyridin-4-yl) -1-triisopropylsilyl-1
4-bromo-2- (4-fluorophenyl) -3- (2-methylaminopyrimidine-4 instead of H-pyrrole
-Yl) -1-triisopropylsilyl-1H-pyrrole was replaced with (±) -1,2,3,5,6,7,8,8a-octahydroindolizine instead of 1-benzylpiperidin-4-one Using -7-one as a starting material, a coupling reaction, a dehydration reaction and a desilyl reaction were sequentially performed in the same manner as in Examples 9-1) and 3) to give the title compound and its isomer (the compound of Example 90). To obtain a mixture. This mixture is subjected to silica gel column chromatography (solvent; ethyl acetate: methanol: isopropylamine = 2).
00: 20: 1) and the title compound (Rf value 0.5
5) was obtained as a light brown amorphous solid (yield 15%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CD ₃ OD) δ ppm: 8.08 (1H, d, J = 5 Hz), 7.3
0 (2H, dd, J = 9Hz, 5Hz), 7.02 (2H, t, J = 9Hz), 6.82
(1H, s), 6.49 (1H, d, J = 5Hz), 5.57-5.51 (1H, m), 3.
53-3.45 (1H, m), 3.21-3.11 (1H, m), 2.90-2.81 (1H,
m), 2.80 (3H, s), 2.47-2.28 (2H, m), 2.26-2.13 (2
H, m), 2.07-1.96 (1H, m), 1.91-1.73 (2H, m), 1.49-
1.37 (1H, m).

[0365]

Working Example 90 (±) -2- (4-Fluorophenyl)
) -4- ( 1,2,3,5,6,8a-hexahydro
Indolizine-7-yl) -3- (2-Mechiruami Bruno pin
(Limidin-4-yl) -1H-pyrrole (Exemplary Compound No. 1-2905) The title compound (Rf value: 0.50) was obtained as a pale brown amorphous solid by silica gel column chromatography performed in Example 89 ( Yield 12%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CD ₃ OD) δ ppm: 8.09 (1H, d, J = 5 Hz), 7.3
0 (2H, dd, J = 9Hz, 5Hz), 7.02 (2H, t, J = 9Hz), 6.83
(1H, s), 6.46 (1H, d, J = 5Hz), 5.48-5.42 (1H, m), 3.
47-3.38 (1H, m), 3.03-2.75 (4H, m), 2.81 (3H, s),
2.46-2.36 (1H, m), 2.29-2.20 (1H, m), 2.03-1.87 (2
H, m), 1.83-1.75 (1H, m), 1.54-1.43 (1H, m).

[0367]

Working Example 91 (±) -2- (3,4-difluorofuran)
Enyl ) -4- ( 1,2,3,5,8,8a-hexahi
Droindolizin-7-yl) -3- (pyridine -4-
Il) -1H-pyrrole (exemplary compound number 1-326)
0) 4-bromo-2- (4-fluorophenyl) -3- (pyridin-4-yl) -1-triisopropylsilyl-1
4-bromo-2- (3,4-difluorophenyl) -3- (pyridin-4-yl) -1 in place of H-pyrrole
-Triisopropylsilyl-1H-pyrrole with (±) -1, instead of 1-benzylpiperidin-4-one
Example 9-1) using 2,3,5,6,7,8,8a-octahydroindolizin-7-one as a starting material
Coupling reaction, dehydration reaction and desilyl reaction were sequentially performed in the same manner as in (3) and (3) to obtain a mixture of the title compound and its isomer (the compound of Example 92). This mixture was subjected to silica gel column chromatography (solvent; ethyl acetate: methanol: isopropylamine = 100: 10:
1) to give the title compound (Rf value 0.66) as a pale pink powder (yield 29%).

Melting point: 215-217 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, DMSO
−d ₆ ) δ ppm: 11.48 (1H, br.s), 8.48 (2H, d, J
= 6Hz), 7.37-7.28 (1H, m), 7.21-7.10 (1H, m), 7.14
(2H, d, J = 6Hz), 6.96 (1H, d, J = 3Hz), 6.93-6.86 (1H,
m), 5.27-5.20 (1H, m), 3.33-3.23 (1H, m), 3.05-2.9
7 (1H, m), 2.65-2.56 (1H, m), 2.30-2.22 (1H, m), 2.
12-1.93 (3H, m), 1.91-1.81 (1H, m), 1.75-1.57 (2H,
m), 1.33-1.20 (1H, m).

[0369]

Working Example 92 (±) -2- (3,4-difluorofuran)
Enyl ) -4- ( 1,2,3,5,6,8a-hexahi
Droindolizin-7-yl) -3- (pyridine -4-
Yl) -1H-pyrrole (exemplary compound number 1-325)
9) The title compound (Rf value: 0.31) was obtained as a pale pink powder by silica gel column chromatography performed in Example 91 (yield: 23%).

Melting point: 187-190 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, DMSO
−d ₆ ) δ ppm: 11.48 (1H, br.s), 8.47 (2H, d, J
= 6Hz), 7.39-7.29 (1H, m), 7.21-7.10 (1H, m), 7.14
(2H, d, J = 6Hz), 6.96 (1H, d, J = 3Hz), 6.94-6.87 (1H,
m), 5.18-5.13 (1H, m), 3.10-3.02 (1H, m), 2.89-2.8
2 (1H, m), 2.79-2.71 (1H, m), 2.63-2.45 (2H, m), 2.
30-2.20 (1H, m), 2.06-1.97 (1H, m), 1.78-1.53 (3H,
m), 1.22-1.10 (1H, m).

[0371]

Embodiment 93 (±) -4- (1,2,3,5,8,
8a- hexahydroisochromeno in Dorijin 7-yl) -3-
(Pyridin-4-yl) -2- (3-trifluoromethyl
Ruphenyl) -1H-pyrrole (exemplary compound number 1-3)
262) 4-Bromo-2- (4-fluorophenyl) -3- (pyridin-4-yl) -1-triisopropylsilyl-1
4-Bromo-3- (pyridine-
4-yl) -2- (3-trifluoromethyl) -1-triisopropylsilyl-1H-pyrrole was replaced with (±) -1,2,2 instead of 1-benzylpiperidin-4-one.
Using 3,5,6,7,8,8a-octahydroindolizin-7-one as a starting material, a coupling reaction, a dehydration reaction and a desilyl reaction were sequentially performed in the same manner as in Examples 9-1) and 3). This gave a mixture of the title compound and its isomer (the compound of Example 94). This mixture was subjected to silica gel column chromatography (solvent; ethyl acetate: methanol: isopropylamine = 100: 10: 1) to give the title compound (Rf value 0.65) as a pale-brown powder (yield 26%). ).

Melting point: 220-223 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, DMSO
−d ₆ ) δ ppm: 11.62 (1H, br.s), 8.49 (2H, d, J
= 6Hz), 7.54-7.35 (4H, m), 7.16 (2H, d, J = 6Hz), 7.02
(1H, d, J = 3Hz), 5.29-5.21 (1H, m), 3.35-3.24 (1H,
m), 3.06-2.98 (1H, m), 2.65-2.56 (1H, m), 2.34-2.24
(1H, m), 2.13-1.94 (3H, m), 1.92-1.82 (1H, m), 1.7
5-1.58 (2H, m), 1.34-1.21 (1H, m).

[0373]

Embodiment 94 (±) -4- (1, 2, 3, 5, 6,
8a- hexahydroisochromeno in Dorijin 7-yl) -3-
(Pyridin-4-yl) -2- (3-trifluoromethyl
Ruphenyl) -1H-pyrrole (exemplary compound number 1-3)
261) The title compound (Rf value 0.31) was obtained as a pale brown powder by silica gel column chromatography performed in Example 93 (yield 17%).

Melting point: 189-191 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, DMSO
−d ₆ ) δ ppm: 11.63 (1H, br.s), 8.48 (2H, d, J
= 6Hz), 7.55-7.37 (4H, m), 7.15 (2H, d, J = 6Hz), 7.02
(1H, d, J = 3Hz), 5.19-5.14 (1H, m), 3.12-3.03 (1H,
m), 2.91-2.82 (1H, m), 2.80-2.71 (1H, m), 2.64-2.45
(2H, m), 2.33-2.21 (1H, m), 2.09-1.98 (1H, m), 1.7
8-1.53 (3H, m), 1.21-1.10 (1H, m).

[0375]

Example 95 (±) -2- (3-fluorophenyl)
) -4- ( 1,2,3,5,8,8a-hexahydro
Indolizin-7-yl) -3- (pyridine-4- i
1) -H -pyrrole (exemplary compound number 1-3256) 4-bromo-2- (4-fluorophenyl) -3- (pyridin-4-yl) -1-triisopropylsilyl-1
4-bromo-2- (3-fluorophenyl) -3- (pyridin-4-yl) -1-triisopropylsilyl-1H-pyrrole in place of H-pyrrole, and 1-benzylpiperidin-4-one (±) -1, 2, 3,
5,6,7,8,8a-octahydroindolizine-7
Examples 9-1) and 3) using -one as a starting material
A coupling reaction, a dehydration reaction and a desilyl reaction were sequentially performed in the same manner as described above, and the title compound and its isomer (Example 96)
With the compound of formula (1). This mixture was subjected to silica gel column chromatography (solvent; ethyl acetate: isopropylamine = 30: 1) to give the title compound (Rf
0.25) was obtained as a pale pink powder (17% yield).

Melting point: 199 ° -203 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.49 (2H, d, J = 6Hz), 8.30 (1H, br.
s), 7.23-7.18 (3H, m), 6.96-6.82 (4H, m), 5.50-5.47
(1H, m), 3.53-2.96 (1H, m), 3.20 (1H, t, J = 9Hz),
2.79 (1H, d, J = 17Hz), 2.32-2.08 (4H, m), 2.00-1.67
(3H, m), 1.48-1.33 (1H, m).

[0377]

Working Example 96 (±) -2- (3-Fluorophenyl)
) -4- ( 1,2,3,5,6,8a-hexahydro
Indolizin-7-yl) -3- (pyridine-4- i
L ) -1H-pyrrole (Exemplified Compound No. 1-3255) The title compound (Rf value 0.10) was obtained as a pale brown powder by silica gel column chromatography carried out in Example 95 (yield 12%).

Melting point: 178-181 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.50 (2H, d, J = 6Hz), 8.34 (1H, br.
s), 7.26-7.18 (3H, m), 6.95-6.84 (4H, m), 5.42 (1H,
s), 3.23-3.17 (1H, m), 3.02-2.82 (2H, m), 2.78-2.6
1 (2H, m), 2.42-2.30 (1H, m), 2.16-2.04 (1H, m), 1.
95-1.68 (3H, m), 1.44-1.32 (1H, m).

[0379]

Working Example 97 (±) -2- (3-Chlorophenyl)
-4- ( 1,2,3,5,8,8a-hexahydroin
Dorijin-7-yl) -3- (pyridin-4-i le) -
1H-pyrrole (Exemplified Compound No. 1-3258) 4-bromo-2- (4-fluorophenyl) -3- (pyridin-4-yl) -1-triisopropylsilyl-1
4-bromo-2- (3-chlorophenyl) -3- (pyridin-4-yl) -1-triisopropylsilyl-1H-pyrrole is used instead of H-pyrrole, and 1-benzylpiperidin-4-one is used instead of 1-benzylpiperidin-4-one. (±) -1, 2, 3,
5,6,7,8,8a-octahydroindolizine-7
Examples 9-1) and 3) using -one as a starting material
A coupling reaction, a dehydration reaction and a desilyl reaction were sequentially performed in the same manner as described above to give the title compound and its isomer (Example 98)
With the compound of formula (1). This mixture was subjected to silica gel column chromatography (solvent; ethyl acetate: isopropylamine = 30: 1) to give the title compound (Rf
0.25) was obtained as a pale pink powder (18% yield).

Melting point: 197-201 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.49 (2H, d, J = 6Hz), 8.32 (1H, br.
s), 7.25-7.13 (5H, m), 6.96 (1H, d, J = 7Hz), 6.85 (1
(H, d, J = 3Hz), 5.50-5.47 (1H, m), 3.54-3.45 (1H, m),
3.20 (1H, t, J = 9Hz), 2.79 (1H, d, J = 16Hz), 2.31-2.
07 (4H, m), 2.00-1.67 (3H, m), 1.48-1.33 (1H, m).

[0381]

Working Example 98 (±) -2- (3-chlorophenyl)
-4- ( 1,2,3,5,6,8a-hexahydroin
Dorijin-7-yl) -3- (pyridin-4-i le) -
1H-Pyrrole (Exemplified Compound No. 1-3257) The title compound (Rf value 0.10) was obtained as a light brown powder by silica gel column chromatography carried out in Example 97 (yield 16%).

Melting point: 193-195 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.50 (2H, d, J = 6Hz), 8.42 (1H, br.
s), 7.25-7.13 (5H, m), 6.96 (1H, d, J = 7Hz), 6.85 (1
(H, d, J = 3Hz), 5.42 (1H, s), 3.26-3.17 (1H, m), 3.02
-2.82 (2H, m), 2.78-2.60 (2H, m), 2.42-2.30 (1H,
m), 2.16-2.03 (1H, m), 1.95-1.65 (3H, m), 1.45-1.32
(1H, m).

[0383]

Example 99 (±) -4- (1,2,3,5,8,
8a- hexahydroisochromeno in Dorijin 7-yl) -2-off
Eniru -3- (pyridin-4-yl)-1H-pin roll <br/> (Compound No. 1-3254) 4-bromo-2- (4-fluorophenyl) -3- (pyridin-4-yl) -1-triisopropylsilyl-1
4-bromo-2-phenyl-3 in place of H-pyrrole
-(Pyridin-4-yl) -1-triisopropylsilyl-1H-pyrrole was converted to 1-benzylpiperidin-4-
(±) -1,2,3,5,6,7,8,
Using 8a-octahydroindolizin-7-one as a starting material, a coupling reaction, a dehydration reaction, and a desilyl reaction were sequentially performed in the same manner as in Examples 9-1) and 3) to give the title compound and its isomer ( (Compound of Example 100). The mixture is subjected to silica gel column chromatography (solvent; ethyl acetate: isopropylamine =
30: 1) to give the title compound (Rf value 0.24) as a pale brown powder (yield 14%).

Melting point: 201-204 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.46 (2H, d, J = 6Hz), 8.28 (1H, br.
s), 7.30-7.13 (7H, m), 6.84 (1H, d, J = 3Hz), 5.50-5.
47 (1H, m), 3.54-3.45 (1H, m), 3.50 (1H, t, J = 9Hz),
2.79 (1H, d, J = 17Hz), 2.32-2.07 (4H, m), 2.00-1.67
(3H, m), 1.48-1.33 (1H, m).

[0385]

Example 100 (±) -4- (1, 2, 3, 5,
6,8a- Hekisahidoroi Ndorijin-7-yl) -2
-Phenyl-3- (pyridin-4-yl) -1H- pyro
Give Lumpur (Compound No. 1-3253) The title compound by silica gel column chromatography performed in Example 99 a (Rf value 0.11) as a pale brown powder (10% yield).

Melting point: 180-183 ° C. (decomposition) ¹ H-nuclear magnetic resonance spectrum (400 MHz, CDCl
₃ ) δppm: 8.47 (2H, d, J = 6Hz), 8.34 (1H, br.
s), 7.30-7.13 (7H, m), 6.84 (1H, d, J = 3Hz), 5.44 (1
H, s), 3.27-3.18 (1H, m), 3.02-2.82 (2H, m), 2.78-
2.60 (2H, m), 2.43-2.30 (1H, m), 2.17-2.06 (1H, m),
1.95-1.65 (3H, m), 1.45-1.32 (1H, m).

[0387]

[Reference example]

[0388]

[Reference Example 1] 4-bromo-2- (4-fluorophenyl)
) -3- (2-Methylaminopyrimidin -4-yl)
-1-triisopropylsilyl-1H-pyrrole 1) 2- (4-fluorophenyl) -3- (2-methyl
Example 1 using 3- (2-methylthiopyrimidin-4-yl) acrylic acid ethyl ester as a starting material instead of ruthiopyrimidin-4- yl) -1H-pyrrole 3- (4-pyridyl) acrylic acid ethyl ester
-1) (pyrrole ring form) and Example 7-1) (decarboxylation)
Was carried out sequentially to give the title compound as a white powder (yield 37%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.41 (1H, br.s), 8.24 (1
H, d, J = 5Hz), 7.42 (1H, dd, J = 9Hz, 5Hz), 7.10 (2H,
t, J = 9Hz), 6.88 (1H, t, J = 3Hz), 6.84 (1H, d, J = 5H
z), 6.81 (1H, t, J = 3Hz), 2.33 (3H, s). 2) 2- (4-fluorophenyl) -3- (2-meta
2-sulfonylpyrimidin -4-yl) -1H-pyrrole 1-)-(4-fluorophenyl) -3- (2-
An oxidation reaction was carried out using methylthiopyrimidin-4-yl) -1H-pyrrole in the same manner as in Example 42-2) to obtain the title compound as a pale yellow powder (yield 81%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ -DC ₃ OD) δ ppm: 8.58 (1H, d, J
= 6Hz), 7.50 (2H, dd, J = 9Hz, 6Hz), 7.47 (1H, d, J = 6
Hz), 7.16 (2H, t, J = 9Hz), 6.90 (1H, d, J = 3Hz), 6.84
(1H, d, J = 3Hz), 3.05 (3H, s). 3) 2- (4-fluorophenyl) -3- (2-methyl
2- (4-Fluorophenyl) -3- (2-) obtained from laminopyrimidin-4 -yl) -1H-pyrrole 2)
Methylamination reaction was carried out in the same manner as in Example 42-3) using methanesulfonylpyrimidin-4-yl) -1H-pyrrole to obtain the title compound as a pale brown amorphous solid (yield: quantitative). ).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.37 (1H, br.s), 8.08 (1
H, d, J = 5Hz), 7.44 (2H, dd, J = 9Hz, 6Hz), 7.08 (2H,
t, J = 9Hz), 6.85 (1H, t, J = 3Hz), 6.75 (1H, t, J = 3H)
z), 6.47 (1H, d, J = 5Hz), 4.90 (1H, br.quartet, J = 5H
z), 2.87 (3H, d, J = 5Hz). 4) 2- (4-fluorophenyl) -3- (2-methyl
Ruaminopyrimidin-4 -yl) -1-triisopropyl
2- (4-fluorophenyl) -3- (2-) obtained with luciryl-1H-pyrrole 3)
Triisopropylsilylation reaction was carried out using methylaminopyrimidin-4-yl) -1H-pyrrole in the same manner as in Example 7-2) to obtain the title compound as a white powder (yield: 82%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 7.92 (1H, d, J = 5 Hz), 7.3
6 (2H, dd, J = 9Hz, 6Hz), 7.06 (2H, t, J = 9Hz), 6.90
(1H, d, J = 3Hz), 6.89 (1H, d, J = 3Hz), 5.93 (1H, d,
J = 5Hz), 4.80 (1H, br.quartet, J = 5Hz), 2.83 (3H, d,
J = 5Hz), 1.15-0.92 (21H, m). 5) 3- [2- (Nt-butoxycarbonyl-N-
Methylamino) pyrimidine down-yl] -2- (4-off
(Fluorophenyl) -1-triisopropylsilyl- 1H
- (4-Fluorophenyl) -3- (2-
Example 4-1) using methylaminopyrimidin-4-yl) -1-triisopropylsilyl-1H-pyrrole
Nt-butoxycarbonylation reaction is carried out in the same manner as
The title compound was obtained as a colorless oil (yield 90%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.24 (1H, d, J = 5 Hz), 7.3
6 (2H, dd, J = 9Hz, 5Hz), 7.09 (2H, t, J = 9Hz), 6.95
(1H, d, J = 3Hz), 6.90 (1H, d, J = 3Hz), 6.28 (1H, d,
J = 5Hz), 3.20 (3H, s), 1.51 (9H, s), 1.15-0.94 (21H,
m). 6) 4-bromo-3- [2- (Nt-butoxycal)
Boniru -N- Mechiruami Roh) pyrimidin-4-yl] -
2- (4-fluorophenyl) -1- Toriisopu propyl
3- [2- (Nt-butoxycarbonyl-) obtained with silyl-1H-pyrrole 5)
N-methylamino) pyrimidin-4-yl] -2- (4
-Fluorophenyl) -1-triisopropylsilyl-
The bromination reaction was carried out in the same manner as in Example 7-3) using 1H-pyrrole to obtain the title compound as a pale brown amorphous solid (yield 79%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.42 (1H, d, J = 5 Hz), 7.2
8 (2H, dd, J = 9Hz, 5Hz), 7.00 (2H, t, J = 9Hz), 6.93
(1H, s), 6.78 (1H, d, J = 5Hz), 3.13 (3H, s), 1.49
(9H, s), 1.15-0.93 (21H, m). 7) 4-bromo-2- (4-fluorophenyl) -3
- (2-Mechiruaminopi Rimijin 4-yl)-1H-
4-bromo-3- [2- (Nt-butoxycarbonyl-N-methylamino) pyrimidin-4-yl] -2- (4-fluorophenyl) -1-triisopropylsilyl- obtained by pyrrole 6) 472 mg of 1H-pyrrole (0.782
mmol) in 10 ml of tetrahydrofuran,
0.98 ml of N HCl / dioxane solution (3.91 m
mol) was added and the mixture was stirred at 50 ° C for 3 hours. After adding water to the reaction solution and neutralizing with a saturated aqueous solution of sodium hydrogen carbonate,
The mixture was extracted with ethyl acetate, the organic layer was concentrated under reduced pressure, and the residue was subjected to silica gel column chromatography (solvent; hexane: ethyl acetate = 7: 3) to give the title compound (202 mg).
Was obtained as a light brown amorphous solid (74% yield).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.66 (1H, br.s), 8.21 (1
H, d, J = 5Hz), 7.26 (2H, dd, J = 9Hz, 5Hz), 7.01 (2H,
t, J = 9Hz), 6.88 (1H, d, J = 3Hz), 6.61 (1H, d, J = 5H
z), 4.96 (1H, br.quartet, J = 5Hz), 2.86 (3H, d, J = 5H
z). 8) 4-bromo-2- (4-fluorophenyl) -3
- (2-Mechiruaminopi Rimijin 4-yl) -1-Doo
4-bromo-2- (4-fluorophenyl) obtained with liisopropylsilyl-1H-pyrrole 7)
-3- (2-Methylaminopyrimidin-4-yl) -1
A triisopropylsilylation reaction was carried out using H-pyrrole in the same manner as in Example 7-2) to obtain the title compound as a pale brown amorphous solid (yield 67%).

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.04 (1H, d, J = 5 Hz), 7.3
0 (2H, dd, J = 9Hz, 6Hz), 6.98 (2H, t, J = 9Hz), 6.91
(1H, s), 6.32 (1H, br.s), 4.85 (1H, br.quartet, J =
4Hz), 2.82 (3H, d, J = 4Hz), 1.15-0.92 (21H, m).

[0397]

Reference Example 2 4-bromo-2-phenyl-3- (pyri
Zin-4-yl) -1 -triisopropylsilyl-1H
Example 1-1) (pyrrole ring formation), Example 7 using α- (p-toluenesulfonyl) benzylisonitrile as a starting material instead of -pyrrole α- (p-toluenesulfonyl) -4-fluorobenzylisonitrile Reactions corresponding to -1) (decarboxylation), Example 7-2) (triisopropylsilylation) and Example 7-3) (bromination) were sequentially performed to obtain the title compound as a pale purple powder.

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.35 (2H, d, J = 6 Hz), 7.3
6-7.30 (1H, m), 7.28-7.21 (4H, m), 7.03 (2H, d, J = 6
Hz), 6.94 (1H, s), 1.15-1.02 (21H, m).

[0399]

Reference Example 3 4-Bromo-2- (3-chlorophenyi
) -3- (pyridin-4 -yl) -1-triisopro
Example 1-1) using pyrryl-1H-pyrrole α- (p-toluenesulfonyl) -4-fluorobenzylisonitrile instead of α- (p-toluenesulfonyl) -3-chlorobenzylisonitrile as a starting material Ring formation), Example 7
Reactions corresponding to -1) (decarboxylation), Example 7-2) (triisopropylsilylation) and Example 7-3) (bromination) were sequentially performed to obtain the title compound as a pale purple powder.

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.40 (2H, d, J = 6 Hz), 7.3
3-7.29 (2H, m), 7.18 (1H, t, J = 8Hz), 7.09 (1H, d, J
= 8Hz), 7.03 (2H, d, J = 6Hz), 6.95 (1H, s), 1.12-0.99
(21H, m).

[0401]

[Reference Example 4] 4-bromo-2- (3-fluorophenyl)
) -3- (pyridin- 4-yl) -1-triisopro
Example 1-1) using pyrryl-1H-pyrrole α- (p-toluenesulfonyl) -4-fluorobenzylisonitrile instead of α- (p-toluenesulfonyl) -3-fluorobenzylisonitrile as a starting material Ring formation), reactions corresponding to Example 7-1) (decarboxylation), Example 7-2) (triisopropylsilylation) and Example 7-3) (bromination) were sequentially performed to give the title compound. Obtained as a pale purple powder.

The ¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.39 (2H, d, J = 6 Hz), 7.2
2 (1H, dd, J = 8Hz, 6Hz), 7.07-7.01 (4H, m), 6.98-6.9
4 (2H, m), 1.14-0.98 (21H, m).

[0403]

Reference Example 5 4-bromo-2- (3,4-difluoro
Phenyl) -3- (pyrimidin Jin-4-yl) -1-Torii
Example 1 using α- (p-toluenesulfonyl) -3,4-difluorobenzylisonitrile as a starting material instead of isopropylsilyl-1H-pyrrole α- (p-toluenesulfonyl) -4-fluorobenzylisonitrile 1) (pyrrole ring formation),
Reactions corresponding to Example 7-1) (decarboxylation), Example 7-2) (triisopropylsilylation) and Example 7-3) (bromination) were sequentially performed to give the title compound as a pale purple powder. Obtained.

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.42 (2H, d, J = 6 Hz), 7.1
2-6.93 (3H, m), 7.02 (2H, d, J = 6Hz), 6.94 (1H, s),
1.18-0.94 (21H, m).

[0405]

Reference Example 6 4-bromo-2- (3-trifluoromethyl
Tylphenyl) -3- ( pyridin-4-yl) -1-to
Example 1 using α- (p-toluenesulfonyl) -3-trifluoromethylbenzylisonitrile as a starting material instead of riisopropylsilyl- 1H-pyrrole α- (p-toluenesulfonyl) -4-fluorobenzylisonitrile Reactions corresponding to 1) (pyrrole ring formation), Example 7-1) (decarboxylation), Example 7-2) (triisopropylsilylation) and Example 7-3) (bromination) were sequentially performed. The title compound was obtained as a pale purple powder.

¹ H-nuclear magnetic resonance spectrum (400 MH
z, CDCl ₃ ) δ ppm: 8.39 (2H, d, J = 6 Hz), 7.6
4-7.57 (2H, m), 7.40-7.33 (2H, m), 7.00 (2H, d, J = 6
Hz), 6.98 (1H, s), 1.15-0.94 (21H, m).

[0407]

[Formulation Examples] The preparations of the present invention containing the compound having the above general formula (I) or a pharmaceutically acceptable salt, ester or other derivative thereof as an active ingredient can be produced, for example, by the following method.

[0408]

Formulation Example 1 Powder 5 g of the compound of Example 2, 895 g of lactose and 100 g of corn starch were mixed with a blender.
A powder is obtained.

[0409]

Formulation Example 2 Granules 5 g of the compound of Example 5, 865 g of lactose and 100 g of low-substituted hydroxypropylcellulose were mixed, and then mixed with 10% aqueous solution of hydroxypropylcellulose 30
Add 0 g and knead. This is granulated using an extrusion granulator and dried to obtain a granule.

[0410]

Formulation Example 3 Capsule 5 g of the compound of Example 6, lactose 115 g, corn starch 58 g and magnesium stearate
After mixing 2 g using a V-type mixer, 180 mg is filled into No. 3 capsules to obtain capsules.

[0411]

Formulation Example 4 Tablets 5 g of the compound of Example 83, 90 g of lactose, 34 g of corn starch, 20 g of crystalline cellulose and 1 g of magnesium stearate are mixed in a blender, and the mixture is compressed with a tablet machine to give tablets.

[0412]

[Test example]

[0413]

[Test Example 1] Human whole blood IL-1β and TNFα production
Inhibition test (in vitro) The method of Hartman et al. (DAHartman, SJ Ochalski a
nd RPCarlson; Theeffects of antiinflammatory and
antiallergic drugs on cytokine release after stim
ulation of human whole blood by lipopolysaccharide
and zymosanA: Inflamm. Res., 44, 269 (1995)).

[0414] Peripheral blood was collected from healthy volunteers in the presence of heparin. 1000 μl of whole blood is added to an eppendorf tube to which 2 μl of a dimethyl sulfoxide solution of a test compound has been added in advance, and lipopolysaccharide (LPS) (derived from E. coli O26: B6, Dif
After adding 10 μl (final concentration: 10 μg / ml), the mixture was mixed well and cultured at 37 ° C. for 6 hours under the conditions of 5% CO ₂ . After completion of the culture, the reaction was stopped by cooling to 4 ° C., and immediately centrifuged at 14,000 rpm for 5 minutes to separate and collect the supernatant plasma. IL- produced and released in plasma
1β and TNFα were measured with an enzyme-linked immunosorbent assay (ELISA) kit (Cayman and Genzyme). The inhibition rate was determined from the amount of cytokine production in the presence and absence of the test compound. Based on these average suppression rates, the IC ₅₀ value was determined by the least squares method.

[0415] (In the above table, compound A and compound B each represent a compound having the following formula.)

[0416]

Embedded image As shown in Table 3 above, in this test, the compound of the present invention showed an excellent cytokine production inhibitory action.

[0417]

Test Example 2 TNFα Production Inhibition Test (in Vivo) The method of Ochalski et al. (SJ Ochalski, DAHartma)
n, MTBelfast, TLWalter, KBGlaser and RPCar
lson; Inhibition of endotoxin-induced hypothermia
and serum TNF-α levels in CD-1 mice by various ph
armacologicalagents: Agents Actions 39, C52-C54 (199
3) Performed according to).

The production of TNFα was induced by intravenous injection of LPS into mice. Balb / c mice (male, 5 to 7 weeks old, weighing 22) fasted overnight from the day before the experiment.
g of LPS (derived from E. coli O26: B6, Difc) using a physiological saline solution to adjust to 0.045 mg / ml in the tail vein of Charles River Japan
o company) was administered at a rate of 10 ml / kg body weight. One hour later, the mouse was opened under anesthesia with ether, and blood was collected from the abdominal vena cava. For blood collection, a 1 ml disposable syringe with a 23G needle attached and an inner wall wetted with heparin was used. After blood collection, the blood was immediately transferred to a 1.5 ml Eppendorf tube, and centrifuged at 14,000 rpm at 4 ° C. to separate plasma. This plasma is TNF
Stored at −20 ° C. until measurement of α.

The amount of TNFα was measured by enzyme immunoassay (ELI).
SA) kit (mouse TNFα ELISA K
IT, Genzyme).

The test compound was suspended in a 0.5% tragacanth solution and orally administered at a ratio of 10 ml / kg of body weight 30 minutes before the injection of LPS. A minimum of 3 doses per test compound were administered to 5 mice each. The average inhibition rate for the control group was calculated for each dose.

In this test, the compound of the present invention showed an excellent inhibitory action on TNFα production.

[0422]

Test Example 3 IL-1β Production Inhibition Test (in Vivo) The method of Griffith et al. (Richard J. Griffiths, Ethan J. Sta
m, James T. Downs and Ivan G. Otterness; ATP Induces
the Release of IL-1 from LPS-Primed Cells In Vivo:
J. Immunol., 154, 2821-2828 (1995)).

By intraperitoneally injecting mice with LPS and adenosine triphosphate (ATP), IL-
Induction of 1β was induced. Ba fasted overnight from the day before the experiment
LPS prepared in abdominal cavity of a lb / c mouse (male, 5 to 7 weeks old, around 22 g, Charles River Japan) using a physiological saline solution to a concentration of 0.0045 mg / ml.
(E. coli O26: derived from B6, Difco) was administered at a rate of 10 ml / kg body weight. Two hours later, 0.5 ml of ATP adjusted to 6.03 mg / ml using a physiological saline solution was intraperitoneally administered. 0.5 hours after ATP administration, 3 ml of washing PBS (heparin:
10 U / ml, PMSF: 0.25 mM, leupep
sin: 1 μg / ml, pepstatin: 1 μg /
ml, containing 1 mM EDTA) was injected intraperitoneally and the peritoneal cavity was washed. A 1 ml disposable syringe equipped with a 21G needle was used for collecting the washing solution. After the collection, the washing solution from the peritoneal cavity was immediately transferred to a 1.5 ml Eppendorf tube, and centrifuged at 4 ° C. and 7,500 rpm to separate the supernatant. This supernatant is
Stored at -20 ° C until measurement of L-1β.

The amount of IL-1β was measured by enzyme immunoassay (EL
ISA) kit (mouse ELISA KIT, G
test compound was suspended in 0.5% tragacanth solution, and 10 ml 30 minutes before LPS injection.
Oral administration was performed at a rate of 1 kg / body weight. A minimum of 3 doses per test compound were administered to 5 mice each. The average inhibition rate for the control group was calculated for each dose.

In this test, the compound of the present invention showed an excellent inhibitory action on IL-1β production.

[0426]

[Test Example 4] Adjuvant arthritis onset suppression test (in vivo) Method of Winder et al. (Arthritis Rheum., 12, 472-482, 196)
It was carried out according to 9).

Heat-killed cells of Mycobacterium butyricum (D
Ifco Laboratories, lot 679123) was refined in an agate mortar, and suspended in dry and heat-sterilized liquid paraffin (Wako Pure Chemical Industries, Ltd., first grade) to a concentration of 2 mg / ml, followed by ultrasonication. An adjuvant was made. This adjuvant (100 μg / 0.05 ml / paw of heat-killed cells) in the right hind footpad skin of a female Lewis rat (9 weeks old, weighing about 190 g, Charles River Japan Co., Ltd.)
Was injected to induce arthritis.

The test compound was suspended in a 0.5% aqueous solution of sodium carboxymethylcellulose, and was suspended daily from the day of injection of adjuvant (Day 0: Day 0) to Day 20.
Oral administration was performed at a rate of 5 ml / kg.

[0429] 3,5,7,1 after injection of adjuvant
On days 0, 13, 15, 18 and 21 the volumes of the right foot (the foot injected with adjuvant) and the left foot (the foot not injected) were measured and the swelling volume (hind foot volume of the adjuvant-injected animal-hind foot foot of the healthy group). Volume) was calculated. Rat foot volume measurement device (Plesthymometer, Ugo Basile) for foot volume measurement
Was used to measure from the hairline of the hind limb to the tip of the foot in the tank of the measuring device.

Further, the swelling inhibition rate of the test compound-administered group relative to the test compound-untreated control group on day 21 was calculated by the following equation.

Swelling inhibition rate (%) = {1− (swelling volume of test compound administration group) / (swelling volume of control group)} × 100 In this test, the compound of the present invention exhibited excellent inhibitory action against adjuvant arthritis. Indicated.

[0432]

[Test Example 5] Anti-collagen antibody-induced arthritis suppression test
In this test, a mouse anti-collagen antibody-induced arthritis model was employed.

An anti-collagen antibody solution (4 mg / ml, cocktail for arthritis, manufactured by Immune Biology Laboratories) was injected into the tail vein of Balb / c mice (male, 5-6 weeks old, Charles River Japan Co., Ltd.). 0.5 ml was administered, and 3 days later, 0.1 ml of a lipopolysaccharide solution (0.5 mg / ml, Arthritis cocktail manufactured by Immune Biological Laboratories, Inc.) was intraperitoneally administered to induce arthritis.

The test compound was suspended in a 0.5% tragacanth solution for 7 days from the day when the anti-collagen antibody solution was administered.
It was orally administered once a day at a rate of 10 ml / kg. still,
The control group received a 0.5% tragacanth solution instead of the test compound suspension.

After the administration of the test compound (or tragacanth solution) was completed, the degree of swelling was scored for each limb according to the following criteria.

0: Normal (no swelling is observed at all) 1: Swelling is observed at one finger 2: Swelling is observed at two or more fingers 3: The entire limb is swollen.

For each individual, the sum of the scores of the limbs was used as the solid swelling score, and the score of each individual in the test compound administration group relative to the average of the control group scores was calculated as follows:
The inhibition rate was calculated, and the inhibition activity of the test compound was determined based on the calculated inhibition rate.

In this test, the compound of the present invention showed an excellent anti-collagen antibody-induced arthritis development inhibitory action.

[0439]

[Test Example 6] Anti-collagen antibody-induced arthritis treatment test
(In vivo) In this test, a mouse anti-collagen antibody-induced arthritis model was adopted.

An anti-collagen antibody solution (4 mg / ml, Arthritis cocktail manufactured by Immune Biology Laboratories) was injected into the tail vein of Balb / c mice (male, 5-6 weeks old, Charles River Japan Co., Ltd.). 0.5 ml was administered, and 3 days later, 0.1 ml of a lipopolysaccharide solution (0.5 mg / ml, Arthritis cocktail manufactured by Immune Biological Laboratories, Inc.) was intraperitoneally administered to induce arthritis.

7 days after the administration of the anti-collagen antibody solution
One day later, the degree of swelling was scored according to the criteria shown in Test Example 5, and mice with a score of 3 for both hind limbs were selected, and a therapeutic test was performed using these mice.

The test compound was suspended in a 0.5% tragacanth solution, and once a day at 10 ml / day for 3 days from the date of the above selection.
Oral administration was performed at a rate of kg. The control group received a 0.5% tragacanth solution instead of the test compound suspension.

After the administration of the test compound (or tragacanth solution) was completed, the degree of swelling of both hind limbs was scored again according to the criteria shown in Test Example 5. The inhibition rate was calculated from the score of each individual in the test compound administration group with respect to the average value of the scores in the control group, and thereby the inhibitory activity of the test compound was determined.

In this test, the compound of the present invention showed an excellent anti-collagen antibody-induced arthritis therapeutic effect.

[0445]

Industrial Applicability The compound of the present invention has an excellent inhibitory action on inflammatory cytokine production (in particular, an inhibitory action on IL-1β and TNFα production), has good oral absorbability, and has low toxicity. So it is useful as a medicament, for example,
Analgesic / anti-inflammatory agent, antiviral agent, rheumatoid arthritis, osteoarthritis, allergic disease, asthma, sepsis,
As a preventive or therapeutic agent for psoriasis, osteoporosis, autoimmune diseases (eg, systemic lupus erythematosus, ulcerative colitis, Crohn's disease, etc.), diabetes, nephritis, hepatitis, tumor, ischemic heart disease, Alzheimer's disease, arteriosclerosis Useful and
In particular, it is useful as an analgesic / anti-inflammatory agent and a preventive or therapeutic agent for rheumatoid arthritis, osteoarthritis, allergic disease, sepsis, psoriasis, osteoporosis, ulcerative colitis, diabetes, hepatitis, arteriosclerosis. .

Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat II (Reference) A61K 31/496 A61K 31/496 31/506 31/506 31/5377 31/5377 31/541 31/541 31/55 31 / 55 A61P 1/16 A61P 1/16 3/10 3/10 7/00 7/00 9/10 9/10 101 101 11/06 11/06 13/12 13/12 17/06 17/06 19 / 02 19/02 19/10 19/10 25/28 25/28 29/00 29/00 31/12 31/12 35/00 35/00 37/00 37/00 37/02 37/02 C07D 401/14 C07D 401/14 403/04 403/04 403/14 403/14 453/02 453/02 455/02 455/02 487/04 137 487/04 137 152 152 (72) Inventor Akira Nakao Hiroshi Shinagawa-ku, Tokyo 1-58 2-cho, Sankyo Co., Ltd. (72) Inventor Shigeru Ushiyama 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 1-72 Sanko Co., Ltd. (72) Inventor Ryuichi Shimozato Hiromachi, Shinagawa-ku, Tokyo No. 1-258 in Sankyo Co., Ltd. (72) Inventor Nobuyuki Okawa 1-2-58 Hiromachi, Shinagawa-ku, Tokyo F-term in Sankyo Co., Ltd. 4C050 AA01 BB04 CC04 EE01 GG01 HH04 4C0 63 AA01 AA03 BB01 BB07 CC12 CC14 CC19 CC31 CC54 CC64 DD04 EE01 4C064 AA06 CC01 DD03 EE01 FF01 GG10 GG12 GG13 4C086 AA01 AA02 AA03 BC17 BC28 BC42 BC73 BC88 GA07 GA08 MA01 MA04 NA14 ZA08 ZAZZAZZAZAZAZAZAZAZAZAA ZB07 ZB11 ZB13 ZB26 ZB33 ZC35

Claims (25)

[Claims] 1. A compound having the following general formula (I), or a pharmacologically acceptable salt, ester or other derivative thereof: In the formula, A represents a pyrrole ring; R ¹ is an aryl group; an aryl group substituted with a group selected from a substituent group α, a substituent group β, a substituent group γ, and a substituent group δ; A heteroaryl group; or a heteroaryl group substituted with a group selected from substituent group α, substituent group β, substituent group γ, and substituent group δ, wherein R ² has at least one nitrogen atom heteroaryl group; or a substituent group alpha, substituent group beta, substituted with a group selected from substituent group γ and substituent group [delta], the nitrogen atom shown a heteroaryl group having at least one, R ³ is in the general formula -X-R ⁴ [wherein, X represents a single bond, a lower alkylene group, substituted with a group selected from substituent group α is a lower alkylene group, lower alkenylene group, selected from substituent group α Lower alkenylene group, lower alkynylene group, Substituent group α
A lower alkynylene group substituted with a group selected from the group consisting of: R ⁴ may be substituted with a group selected from a substituent group α and a substituent group δ, and a substituent group β and a substituent group γ A cycloalkyl group substituted with a group selected from the group consisting of: a cycloalkyl group which may be substituted with a group selected from the substituent group α and the substituent group δ, and a group selected from the substituent group β and the substituent group γ A substituted aryl group; a heterocyclyl group which may be substituted with a group selected from substituent group α and substituent group δ, and is substituted by a group selected from substituent group β and substituent group γ; A heterocyclyl group having at least one nitrogen atom which may be substituted with a group selected from the group α and the group δ; substituted with a group selected from the group α and the group δ; May be replaced by a group selected from the substituent group β and the substituent group γ. Heteroaryl group;
A heteroaryl group having at least one nitrogen atom, which may be substituted with a group selected from the substituent group α and the substituent group δ; or a group having the general formula —NR ^a R ^b (wherein
R ^a and R ^b are the same or different and each represent a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an aralkyl group, or a lower alkylsulfonyl group. ) Is shown. ] Is shown. However, the atom on the pyrrole ring to which R ¹ and R ³ are bonded is
Each is adjacent to the atom on the pyrrole ring to which R ² is attached. ｝ [Substituent group α] a hydroxyl group, a nitro group, a cyano group, a halogen atom, a lower alkoxy group, a halogeno lower alkoxy group,
An alkylthio group, a halogeno lower alkylthio group [substituent group β] —a group having —NR ^c R ^d (where R ^c and R ^d are the same or different and are each a hydrogen atom,
It represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an aralkyl group, or a lower alkylsulfonyl group, or forms a heterocyclyl group together with the nitrogen atom to which R ^c and R ^d are bonded. ) [Substituent group γ] Lower alkyl group substituted by a group having -NR ^c R ^d (wherein R ^c and R ^d have the same meanings as described above) [Substituent group δ] Lower alkyl group Lower alkenyl group, lower alkynyl group, aralkyl group, cycloalkyl group, lower alkyl group substituted with a group selected from substituent group α, lower alkenyl group substituted with a group selected from substituent group α, An alkynyl group substituted with a group selected from the substituent group α. 2. The method according to claim 1, wherein R ¹ is an aryl group; or an aryl group substituted with a group selected from the group consisting of a substituent group α, a group of substituents β, a group of substituents γ and a group of substituents δ. A compound or a pharmacologically acceptable salt, ester or other derivative thereof. 3. The method according to claim 1, wherein R ¹ is phenyl,
Naphthyl, or a compound which is phenyl or naphthyl substituted with a group selected from substituent group α, substituent group β, substituent group γ and substituent group δ, or a pharmacologically acceptable salt, ester or other thereof. Derivatives. 4. The method of claim 1, wherein R ¹ is phenyl,
Or a substituent group α ¹ , a substituent group β ¹ , a compound which is phenyl substituted with a group selected from the substituent group γ ¹ and the substituent group δ ¹ or a pharmaceutically acceptable salt, ester or other Derivatives. [Substituent group α ¹ ] halogen atom, lower alkoxy group, halogeno lower alkoxy group [Substituent group β ¹ ] —a group having —NR ^c R ^d (where one of R ^c and R ^d is a hydrogen atom or lower alkyl) Represents a hydrogen atom, a lower alkyl group or an aralkyl group.) [Substituent group γ ¹ ] amino lower alkyl group, lower alkylamino lower alkyl group, di (lower alkyl) amino lower alkyl group, aralkylamino Lower alkyl group [Substituent group δ ¹ ] Lower alkyl group, halogeno lower alkyl group, hydroxy lower alkyl group, nitro lower alkyl group 5. The method of claim 1, wherein R ¹ is phenyl,
Or a compound which is phenyl substituted with a group selected from the following substituent groups, or a pharmacologically acceptable salt, ester or other derivative thereof. [Substituent groups] a halogen atom, a halogeno lower alkyl group,
A halogeno lower alkoxy group. 6. The method of claim 1, wherein R ¹ is phenyl,
4-fluorophenyl, 3-fluorophenyl, 3-chlorophenyl, 3,4-difluorophenyl, 3,4
A compound which is 5-trifluorophenyl, 3-chloro-4-fluorophenyl, 3-difluoromethoxyphenyl or 3-trifluoromethylphenyl, or a pharmaceutically acceptable salt, ester or other derivative thereof. 7. A method selected from claims 1 to 6.
In one of the terms, R ^TwoHas one or two nitrogen atoms
A 5- or 6-membered aromatic heterocyclic group containing
Groups selected from the substituent group β, the substituent group γ, and the substituent group δ
5-6 containing one or two nitrogen atoms substituted with
Or a pharmacologically acceptable compound that is a membered aromatic heterocyclic group
Salts, esters or other derivatives. 8. A method selected from claims 1 to 6.
In one of the terms, R ^TwoBut pyridyl, pyrimidiny
Or substituent group α, substituent group β, substituent group γ and substitution
Pyridyl substituted with a group selected from group δ or
Compounds that are pyrimidinyl or pharmacologically acceptable thereof
Salts, esters or other derivatives. 9. A method selected from claim 1 to claim 6.
In one of the terms, R ^TwoIs 4-pyridyl, 4-pyridyl
Midinyl, or substituent group α, substituent group β, substituent group γ and
And 4-pyridyl substituted with a group selected from substituent group δ
Or a compound which is 4-pyrimidinyl, or its pharmacology
Salts, esters or other derivatives that are acceptable. 10. The method according to claim 1, wherein R ² is 4-pyridyl, 4-pyrimidinyl, or a substituent group α, a substituent group β, or a substituent group γ.
And 4-pyridyl or 4-pyrimidinyl substituted at the 2-position with one group selected from the substituent group δ, or a pharmacologically acceptable salt, ester or other derivative thereof. 11. The method according to claim 1, wherein R ² is ² -pyridyl, 4-pyrimidinyl, or a 2-membered group selected from the following substituent groups. Is a substituted 4-pyridyl or 4-pyrimidinyl, or a pharmaceutically acceptable salt, ester or other derivative thereof. [Substituent groups] methoxy, amino, methylamino, benzylamino, α-methylbenzylamino 12. The method according to claim 1, wherein R ⁴ may be substituted with a group selected from the group of substituents α and δ. A cycloalkyl group having 3 to 7 carbon atoms substituted with a group selected from the group β and the substituent group γ; a cycloalkyl group which may be substituted with a group selected from the substituent group α and the substituent group δ; Phenyl or naphthyl substituted with a group selected from group β and group γ; group α and group δ
May be substituted with a group selected from
And a 4- to 12-membered non-aromatic heterocyclic group containing one or two sulfur atoms, oxygen atoms and / or nitrogen atoms, substituted with a group selected from substituent group γ; substituent group α and substituent A 4- to 12-membered non-aromatic heterocyclic group optionally containing one nitrogen atom and further containing one oxygen atom, sulfur atom or nitrogen atom, which may be substituted with a group selected from group δ One or two sulfur atoms, which may be substituted with a group selected from the substituent group α and the substituent group δ, and are substituted with a group selected from the substituent group β and the substituent group γ; A 5- or 6-membered aromatic heterocyclic group containing an oxygen atom and / or a nitrogen atom; 5 containing 1 or 2 nitrogen atoms which may be substituted with a group selected from the substituent group α and the substituent group δ
Or ^a 6-membered aromatic heterocyclic group; or -NR ^a R ^b (wherein R ^a
And R ^b are as defined above. Or a pharmacologically acceptable salt, ester or other derivative thereof. 13. The method according to claim 1, wherein X is a single bond; an alkylene group having 1 to 6 carbon atoms; and X is substituted with a group selected from the substituent group α. An alkylene group having 1 to 6 carbon atoms;
To 6 alkenylene groups; alkenylene groups having 2 to 6 carbon atoms, substituted with groups selected from substituent group α;
A alkynylene group having 2 to 6 carbon atoms; or a compound which is an alkynylene group having 2 to 6 carbon atoms, which is substituted with a group selected from the substituent group α, or a pharmacologically acceptable salt thereof,
Esters or other derivatives. 14. The method according to claim 1, wherein X is a single bond; an alkylene group having 1 to 4 carbon atoms; and X is substituted with a group selected from the substituent group α. An alkylene group having 1 to 4 carbon atoms;
And 4 to 4 alkenylene groups; alkenylene groups having 2 to 4 carbon atoms substituted with a group selected from the substituent group α;
A alkynylene group having 2 to 4 carbon atoms; or a compound which is a alkynylene group having 2 to 4 carbon atoms, which is substituted with a group selected from the substituent group α, or a pharmaceutically acceptable salt thereof,
Esters or other derivatives. 15. The method according to any one of claims 1 to 12, wherein X is a single bond; an alkenylene group having 2 to 4 carbon atoms; or a group selected from the substituent group α. Or a pharmacologically acceptable salt, ester or other derivative thereof, which is an alkenylene group having 2 to 4 carbon atoms. 16. The method according to claim 1, wherein R ³ is a group represented by the following general formula (II):
A group having: [In the formula, m represents 0 or 1, n represents 1 or 2, R ⁵ , R ⁶ , R ⁷ , R ⁸ and R ⁹ are the same or different and are a hydrogen atom, a substituent group α , Substituent group β, substituent group γ
And one group selected from substituent group δ, and one of D and E is> NR ¹⁰ (R ¹⁰ is a hydrogen atom, substituent group γ
And one group selected from the substituent group δ. The other is> CR ¹¹ R ¹² (R ¹¹ and R ¹² are one group selected from a hydrogen atom, a substituent group α, a substituent group β, a substituent group γ and a substituent group δ And R)
⁶ may together with R ⁵ or R ⁷ represent a single bond; R ¹⁰ and R ¹¹ together form a lower alkylene group or a substituent group α, a substituent group β, a substituent It may form a lower alkylene group substituted by a group selected from group γ and substituent group δ. Or a pharmacologically acceptable salt, ester or other derivative thereof. 17. The method of claim 16, wherein m is 1.
A compound in which n is 1, or a pharmaceutically acceptable salt, ester or other derivative thereof. 18. The method according to claim 16, wherein
A compound wherein E is> NR ¹⁰ and D is> CR ¹¹ R ¹² , or a pharmaceutically acceptable salt, ester or other derivative thereof. 19. The method according to claim 16, wherein one of R ⁵ and R ⁷ is R ⁶
And a single bond; the other is a hydrogen atom, a group selected from substituent group α, substituent group γ and substituent group δ, wherein R ⁸ , R ⁹ and R ¹² are The same or different, a hydrogen atom, a substituent group α, a substituent group γ and a substituent group δ
R ¹⁰ and R ¹¹ are the same or different and each are a hydrogen atom, a substituent group α, a substituent group γ
And one group selected from substituent group δ, or R ¹⁰ and R ¹¹ together form a lower alkylene group,
Or a compound forming a lower alkylene group substituted with a group selected from the substituent group α, the substituent group β, the substituent group γ, and the substituent group δ, or a pharmaceutically acceptable salt, ester or other thereof. Derivatives. 20. The method according to claim 16, wherein R ¹⁰ and R ¹¹ together form a straight-chain alkylene group having 3 to 4 carbon atoms or a group of substituents. a compound having a straight-chain alkylene group having 3 or 4 carbon atoms and substituted by a group selected from α, substituent group β, substituent group γ and substituent group δ, or a pharmaceutically acceptable salt thereof , Esters or other derivatives. 21. The method according to claim 16, wherein R ⁷ , R ⁸ and R ⁹ are each a hydrogen atom, and R ¹⁰ and R ¹¹ are taken together. A straight-chain alkylene group having 3 to 4 carbon atoms, or a straight-chain alkylene group having 3 to 4 carbon atoms, which is substituted with a group selected from the group of substituents α, β, γ and δ. A compound forming a chain alkylene group or a pharmacologically acceptable salt, ester or other derivative thereof. 22. The method according to claim 1, wherein the compound is represented by the following general formula (1-1) or general formula (1-3): Or a pharmacologically acceptable salt, ester or other derivative thereof. 23. The compound according to claim 1, wherein the compound is selected from the following or a pharmacologically acceptable salt, ester or other derivative thereof: 4- (3-aminopropyl) -2- (4-fluorophenyl)- 3- (pyridin-4-yl) -1H-pyrrole • 4- (3-acetylaminopropyl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H
-Pyrrole 2- (4-fluorophenyl) -4- (3-methylaminopropyl) -3- (pyridin-4-yl) -1H-
Pyrrole [5- (4-fluorophenyl) -4- (pyridine-
4-yl) -1H-pyrrol-3-yl]-(pyridin-4-yl) methanol 4- (1-acetyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4 -Fluorophenyl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (1,2,3,6-tetrahydropyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (piperidine-
4-yl) -3- (pyridin-4-yl) -1H-pyrrole 3- (4-fluorophenyl) -1- (piperidin-
4-yl) -2- (pyridin-4-yl) -1H-pyrrole 1- (1-acetylpiperidin-4-yl) -3-
(4-Fluorophenyl) -2- (pyridin-4-yl) -1H-pyrrole.3- (4-fluorophenyl) -1- [1- (2-nitroethyl) piperidin-4-yl] -2- ( Pyridin-4-yl) -1H-pyrrole 3- (4-fluorophenyl) -1- [3- (morpholin-1-yl) propyl] -2- (pyridin-4-yl) -1H-pyrrole3 -(4-Fluorophenyl) -1- (piperidine-
3-yl) -2- (pyridin-4-yl) -1H-pyrrole 1- (azetidin-3-yl) -3- (4-fluorophenyl) -2- (pyridin-4-yl) -1H- Pyrrole 4- (3-dimethylaminopropyl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H
-Pyrrole 2- (4-fluorophenyl) -4- [3- (piperidin-1-yl) propyl] -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl)- 4- [3- (1-Methylpiperazin-4-yl) propyl] -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-methyl-
1,2,3,6-tetrahydropyridin-4-yl)-
3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-methylpiperidin-4-yl) -3- (pyridin-4-yl)-
1H-pyrrole 3- (4-fluorophenyl) -2- (pyridine-4
-Yl) -1- (2,2,6,6-tetramethylpiperidin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (quinuclidin-2-en-3-yl)
-1H-pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (quinuclidin-3-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (4-hydroxypiperidin-4-yl) -3- (pyridin-4-yl)- 1H-pyrrole 3- (4-fluorophenyl) -2- (pyridine-4
-Yl) -1- (quinuclidin-3-yl) -1H-pyrrole 1- (4-aminocyclohexyl) -3- (4-fluorophenyl) -2- (pyridin-4-yl) -1H-
Pyrrole3- (4-fluorophenyl) -2- (2-methylaminopyrimidin-4-yl) -1- (piperidin-4-
Yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (8-methyl-
8-azabicyclo [3.2.1] oct-2-ene-3
-Yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (8-methyl-
8-Azabicyclo [3.2.1] octan-3-yl)
-3- (pyridin-4-yl) -1H-pyrrole 4- (8-azabicyclo [3.2.1] oct-2-
(En-3-yl) -2- (4-fluorophenyl) -3
-(Pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (1,2,3,6-tetrahydro-2,
2,6,6-tetramethylpyridin-4-yl) -1H
-Pyrrole 2- (4-fluorophenyl) -3- (pyridine-4
-Yl) -4- (2,2,6,6-tetramethylpiperidin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (2-methyl-
1,2,3,6-tetrahydropyridin-4-yl)-
3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (6-methyl-
1,2,3,6-tetrahydropyridin-4-yl)-
3- (pyridin-4-yl) -1H-pyrrole. 4- (1-ethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl)-
3- (pyridin-4-yl) -1H-pyrrole. 4- (1-ethylpiperidin-4-yl) -2- (4
-Fluorophenyl) -3- (pyridin-4-yl)-
1H-pyrrole 2- (4-fluorophenyl) -4- (1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-propyl-1,2,3,6-tetrahydropyridin-4-yl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-phenethyl-1,2,3,6-tetrahydropyridin-4-yl) -3- ( Pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,8,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,6,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 4- (1,6-dimethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3 -(Pyridin-4-yl) -1H-pyrrole 4- (1,2-dimethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- ( Pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,2,
6,6-pentamethyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl)-
1H-pyrrole 4- (3-dimethylamino-1-propen-1-yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (4-amino Butyl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (1-ethyl-6-methyl-1,2,3,6-tetrahydropyridine-4- Yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (1-ethyl-2-methyl-1,2,3,6-tetrahydropyridine-4- Yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 1- (3-dimethylaminopropyl) -3- (4-fluorophenyl) -2- (pyridine- 4-yl) -1H
-Pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,6,7,8,8a-octahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole -4- (6-allyl-1-methyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4- Fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (2-allyl-1-methyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4- Fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (6-benzyl-1-methyl-1,2,3,6-
Tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 4- (2-benzyl-1-methyl-1,2,3,6-
Tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (6-methyl-
1-propyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (2-methyl-
1-propyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,3 4,
6,7,9a-Hexahydro-2H-quinolidine-8-
Yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,3,4,
6,9,9a-Hexahydro-2H-quinolidine-8-
Yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3
5,8,8a-Hexahydroindolizin-7-yl)
-3- (2-Methylaminopyrimidin-4-yl) -1
H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,6,8a-Hexahydroindolizin-7-yl)
-3- (2-Methylaminopyrimidin-4-yl) -1
H-pyrrole 2- (3,4-difluorophenyl) -4- (1,
2,3,5,8,8a-Hexahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole2- (3,4-difluorophenyl) -4- (1,
2,3,5,6,8a-hexahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole Il)-
2- (3-trifluoromethylphenyl) -1H-pyrrole 4- (1,2,3,5,6,8a-hexahydroindolizin-7-yl) -3- (pyridin-4-yl)-
2- (3-trifluoromethylphenyl) -1H-pyrrole 2- (3-fluorophenyl) -4- (1,2,3
5,8,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (3-fluorophenyl) -4- (1,2,3
5,6,8a-Hexahydroindolizin-7-yl)
-3- (Pyridin-4-yl) -1H-pyrrole 2- (3-chlorophenyl) -4- (1,2,3
5,8,8a-Hexahydroindolizin-7-yl)
-3- (Pyridin-4-yl) -1H-pyrrole 2- (3-chlorophenyl) -4- (1,2,3
5,6,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 4- (1,2,3,5,8,8a-hexahydroindolizin-7-yl) -2-phenyl-3- (pyridine-4 -Yl) -1H-pyrrole 4- (1,2,3,5,6,8a-hexahydroindolizin-7-yl) -2-phenyl-3- (pyridin-4-yl) -1H-pyrrole . 24. The compound according to claim 1, wherein the compound is selected from the following, or a pharmacologically acceptable salt, ester or other derivative thereof: 2- (4-fluorophenyl) -3- (pyridine-4)
-Yl) -4- (1,2,3,6-tetrahydropyridin-4-yl) -1H-pyrrole 3- (4-fluorophenyl) -1- (piperidine-
4-yl) -2- (pyridin-4-yl) -1H-pyrrole 3- (4-fluorophenyl) -1- [3- (morpholin-1-yl) propyl] -2- (pyridin-4- Yl) -1H-pyrrole 4- (8-azabicyclo [3.2.1] oct-2-
(En-3-yl) -2- (4-fluorophenyl) -3
-(Pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (6-methyl-
1,2,3,6-tetrahydropyridin-4-yl)-
3- (pyridin-4-yl) -1H-pyrrole. 4- (1-ethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl)-
3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-isopropyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridine -4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-propyl-1,2,3,6-tetrahydropyridin-4-yl)
-3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1-phenethyl-1,2,3,6-tetrahydropyridin-4-yl) -3- ( Pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,2,3,
5,6,8a-Hexahydroindolizin-7-yl)
-3- (pyridin-4-yl) -1H-pyrrole 4- (1,6-dimethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3 -(Pyridin-4-yl) -1H-pyrrole 4- (1,2-dimethyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- ( 4- (1-ethyl-6-methyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- (pyridin-4-yl) -1H-pyrrole Pyridin-4-yl) -1H-pyrrole 4- (1-ethyl-2-methyl-1,2,3,6-tetrahydropyridin-4-yl) -2- (4-fluorophenyl) -3- ( Pyridin-4-yl) -1H-pyrrole Orofeniru) -4- (6-methyl -
1-propyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (2-methyl-
1-propyl-1,2,3,6-tetrahydropyridin-4-yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (4-fluorophenyl) -4- (1,3 4,
6,7,9a-Hexahydro-2H-quinolidine-8-
Yl) -3- (pyridin-4-yl) -1H-pyrrole 2- (3,4-difluorophenyl) -4- (1,
2,3,5,6,8a-hexahydroindolizine-7
-Yl) -3- (pyridin-4-yl) -1H-pyrrole 4- (1,2,3,5,6,8a-hexahydroindolizin-7-yl) -3- (pyridin-4- Il)-
2- (3-trifluoromethylphenyl) -1H-pyrrole 25. A medicament comprising the compound according to any one of claims 1 to 24 or a pharmacologically acceptable salt, ester or other derivative thereof as an active ingredient.