New! View global litigation for patent families

EP2590929A1 - Aryloxy-alkylene substituted hydroxyphenyl hexynoic acids, methods for the production thereof and use of the same as medicament - Google Patents

Aryloxy-alkylene substituted hydroxyphenyl hexynoic acids, methods for the production thereof and use of the same as medicament

Info

Publication number
EP2590929A1
EP2590929A1 EP20110733622 EP11733622A EP2590929A1 EP 2590929 A1 EP2590929 A1 EP 2590929A1 EP 20110733622 EP20110733622 EP 20110733622 EP 11733622 A EP11733622 A EP 11733622A EP 2590929 A1 EP2590929 A1 EP 2590929A1
Authority
EP
Grant status
Application
Patent type
Prior art keywords
described
ci
example
alkyl
formula
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP20110733622
Other languages
German (de)
French (fr)
Inventor
Stefanie Keil
Elisabeth Defossa
Viktoria Dietrich
Siegfried Stengelin
Andreas Herling
Guido Haschke
Thomas Klabunde
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sanofi SA
Original Assignee
Sanofi SA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/54Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40Unsaturated compounds
    • C07C59/58Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/64Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/65One oxygen atom attached in position 3 or 5
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring

Abstract

The invention relates to aryloxy-alkylene substituted hydroxyphenyl hexynoic acid derivatives of formula (I) and to their physiologically compatible salts. The compounds are suitable for, for example, the treatment of diabetes, because they cause an increased insulin release by activating the GPR40 receptor.

Description

description

Aryloxy-alkylene-substituted hydroxy-phenyl-hexinsäuren, processes for their

Preparation and their use as medicaments

The invention relates to aryloxy-alkylene-substituted hydroxy-phenyl-hexinsäurederivate, and their physiologically acceptable salts. There are structurally similar compounds in the prior art (see Eisai WO2002 / 100812) as well as their use as PPAR agonists or antagonists.

The invention had the object of providing compounds which display a therapeutically utilizable effect. Next, the task was to find new compounds which are useful in the treatment of hyperglycemia and diabetes. Next, the task was to find new compounds that activate the GPR40 receptor and are useful in the treatment of hyperglycemia and diabetes.

The invention therefore relates to compounds of the formula I,

wherein represents (Ci-C 6) -alkyl, (C 3 -C 6) -cycloalkyl, (Ci-C 3) alkylene (C3-C6) cycloalkyl, wherein said (Ci-C 6) alkyl radical, the (C 3 -C 6) cycloalkyl and (Ci-C 3) -alkylene- (C 3 -C 6) -cycloalkyl in each case one or more times may be substituted with F; R2, R3 are independently H, F, Cl, Br, CN, CO- (Ci-C 6) -alkyl, (Ci-C 6) -alkyl or O- (Ci-C 6) -alkyl, where the CO (Ci-C 6) -alkyl (Ci-C 6) -alkyl and O- (Ci-Ce) -AI kyl radical may be singly or multiply substituted with F, respectively;

R4, R5, R6, R7, R8, R9, R10, R1 1 is independently H, (Ci-C 6) alkyl,

(Ci-C 3) -alkylene- (C 3 -C 6) cycloalkyl, (C 3 -C 6) -cycloalkyl, (C 6 -C 0) aryl), OH, O- (Ci-C6) -alkyl, O- (Ci -C 3) -alkyl kylen- (C6-Cio) aryl), O- (Ci -C 3) -alkyl kylen- (C 3 -C 6) - cycloalkyl, O- ( C 3 -C 6) cycloalkyl, (Ci-C 3) alkylene-OH, (Ci-C 3) -alkylene-O- (Ci- C6) alkyl, (Ci-C 3) -alkylene-O - (Ci-C 3) alkylene- (C 3 -C 6) cycloalkyl, (dC 3) - alkylene-O- (C 3 -C 6) cycloalkyl, wherein said (CrC 6) -AI alkyl radical, the (Ci-C3) - alkylene- (C 3 -C 6) cycloalkyl radical, the (C 3 -C 6) -Cycloal alkyl radical, which O- (Ci-C 6) - alkyl radical O- (Ci -C 3) alkylene- (C 6 -C 0) aryl) radical, the cycloalkyl radical O- (dC 3) -alkylene- (C 3 -C 6) O- (C 3 -C 6) - cycloalkylene alkyl rest, the (dC 3) rest -alkylene-OH, of (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, the (Ci-C 3) -alkylene-O- ( Ci-C3) - alkylene- (C 3 -C 6) -cycloal alkyl radical and the (Ci-C 3) -alkylene-O- (C 3 -C 6) - alkyl cycloalkylene radical in each case one or polysubstituted with F could be; q, r independently of one another 0, 1;

, R13, R14 are independently H, F, Cl, Br, I, NO 2, CN, O- (Ci-C 6) -alkyl, (Ci-C 6) -alkyl, (Ci-C 3) alkylene (C 3 -C 6) cycloalkyl, SO 2 -CH 3, SO 2 -NH 2, SO 2 - NH (Ci-C 6) -alkyl, SO 2 -N ((Ci-C 6) alkyl) 2 , CONH 2, CONH (Ci-C 6) -alkyl, CON ((Ci-C 6) -alkyl) 2, SF 5, (C 6 -C 0) aryl, (C 3 -C 0) -cycloalkyl or a 4 bis12- membered heterocycle, wherein the O- (d-C6) alkyl, the (Ci-Ce) -alkyl radical, the (Ci-C 3) -alkylene- (C 3 -C 6) cycloalkyl, SO 2 -NH (Ci-C 6) -alkyl, SO 2 -N ((Ci-C 6) alkyl) 2 group, the CONH (Ci-C 6) -alkyl and CON ((d- C6) alkyl) 2 radical in each case may be substituted with one or multiple F and wherein the (C6-Cio) aryl, the (C3-Cio) cycloalkyl radical and the 4 bis12- membered heterocycle each substituted one to 3 times may be with

F, Cl, Br, I, OH, CF 3, CHF 2, CH 2 F, NO 2, CN, OCF 3, OCHF 2, 0- (Ci-C6) alkyl, (Ci-C 6) alkyl, NH 2, NH (Ci-C 6) -alkyl, N ((Ci-C 6) alkyl) 2> SO 2 -CH 3, SO 2 -NH 2, SO 2 -NH (Ci-C 6) alkyl , SO 2 -N ((Ci-C 6) -alkyl) 2, COOH, COO- (Ci-C 6) -alkyl, CONH 2, CONH (Ci-C 6) -alkyl, CON ((CC 6) - alkyl) 2, or SF 5;

A (C 6 -Cio) aryl, (C 3 -C 0) cycloalkyl or a 4 to 12-membered

heterocycle; and their physiologically tolerated salts.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings:

R1 CH 3; R2, R3 are independently H, F, Cl, Br, CN, CO- (Ci-C 6) -alkyl, (Ci-C 6) -alkyl or O- (Ci-C 6) -alkyl, where the CO (Ci-C 6) -alkyl (Ci-C 6) -alkyl and O- (d-C6) -alkyl radical can in each case be mono or polysubstituted by F; R4, R5, R6, R7, R8, R9, R10, R1 1 is independently H, (Ci-C 6) alkyl,

(Ci-C 3) -alkylene- (C 3 -C 6) cycloalkyl, (C 3 -C 6) -cycloalkyl, (C 6 -C 0) aryl), OH, O- (Ci-C6) -alkyl, O- (Ci -C 3) -alkyl kylen- (C 6 -C 0) aryl), O- (Ci -C 3) -alkyl kylen- (C 3 -C 6) - cycloalkyl, O - (C 3 -C 6) cycloalkyl, (dC 3) -alkylene-OH, (Ci-C 3) -alkylene-O- (Ci- C6) alkyl, (Ci-C 3) -alkylene-O - (Ci-C 3) alkylene- (C 3 -C 6) cycloalkyl, (dC 3) - alkylene-O- (C 3 -C 6) cycloalkyl, wherein said (Ci-C 6) alkyl radical, the (dC 3) -

Alkylene (C 3 -C 6) cycloalkyl radical, the (C 3 -C 6) -cycloalkyl, the O- (Ci-C 6) - alkyl radical O- (Ci-C 3) alkylene- (C 6 -C 0) aryl) radical, the cycloalkyl radical O- (dC 3) -alkylene- (C 3 -C 6) cycloalkyl O- (C 3 -C 6) (Ci-C 3) - alkylene-OH group, the (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, the (Ci-C 3) alkylene-0- (Ci-C3) - alkylene- (C 3 -C 6) cycloalkyl and (Ci-C 3) alkylene-0- (C 3 -C 6) - cycloalkyl may be mono or polysubstituted with F, respectively; q, r independently of one another 0, 1;

R12, R13, R14 are independently H, F, Cl, Br, I, NO 2, CN, O- (Ci-C 6) alkyl,

(Ci-C 6) -alkyl, (Ci-C 3) -alkylene- (C 3 -C 6) cycloalkyl, SO 2 -CH 3, SO 2 -NH 2, SO 2 - NH (Ci-C 6) alkyl, SO 2 -N ((Ci-C 6) alkyl) 2, CONH 2, CONH (Ci-C 6) alkyl,

CON ((Ci-C 6) -alkyl) 2, SF 5, (C 6 -C 0) aryl, (C 3 -C 0) cycloalkyl or a 4 bis12- membered heterocycle, wherein (O- Ci of C6) alkyl, the (Ci-C6) alkyl, the (Ci-C 3) -alkylene- (C 3 -C 6) cycloalkyl, SO 2 -NH (Ci-C 6) alkyl, SO 2 -N ((Ci-C 6) alkyl) 2 group, the CONH (Ci-C 6) -alkyl and CON ((d- Ce) alkyl) 2 radical in each case be mono or polysubstituted with F can, and wherein the (C6-Cio) aryl, the (C 3 -Cio) cycloalkyl and 4 bis12- membered heterocycle in each case can be up to 3-fold substituted with

F, Cl, Br, I, OH, CF 3, CHF 2, CH 2 F, NO 2, CN, OCF 3, OCHF 2, O- (d- C6) alkyl, (Ci-C 6) alkyl , NH 2, NH (Ci-C 6) -alkyl, N ((Ci-C 6) -alkyl) 2, SO 2 -CH 3, SO 2 -NH 2, SO 2 -NH (Ci-C 6) - alkyl, SO 2 -N ((Ci-C 6) alkyl) 2,

COOH, COO- (Ci-C 6) -alkyl, CONH 2, CONH (Ci-C 6) -alkyl, CON ((d- C6) alkyl) 2, or SF 5;

A (C 6 -Cio) aryl, (C 3 -C 0) cycloalkyl or a 4 to 12-membered

heterocycle; and their physiologically tolerated salts.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings: R1

R2, R3 H; R4, R5 independently of one another H, (Ci-C6) alkyl;

R6, R7 independently of one another H, (Ci-C 6) -alkyl, (Ci-C 3) -alkylene- (C 3 -C 6) cycloalkyl

(C 3 -C 6) -cycloalkyl, phenyl, OH, O- (Ci-C 6) -alkyl, O- (Ci-C 3) alkylene-phenyl, O- (Ci -C 3) -alkyl kylen- (C 3 -C 6) -cycloal -alkyl, O- (C 3 -C 6) -cycloal alkyl, (Ci -C 3) -alkyl kylen- OH; (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, (Ci-C 3) alkylene-O- (Ci-C 3) alkylene- (C 3 - C 6) alkyl -cycloal , (Ci -C 3) -alkylene-O- (C 3 -C 6) alkyl -cycloal;

R8, R9 independently of one another H, (d-C6) alkyl;

R10, R1 1 is independently H, (d-C6) alkyl; q, r independently of one another 0, 1;

R12, R13 independently of one another H, F, CI, Br, I, CN, O- (Ci-C 6) -alkyl, (d- C 6) alkyl, wherein the O- (Ci-C 6) alkyl radical and the (Ci-C 6) alkyl radical in each case one or more times may be substituted with F;

R14 H;

A is phenyl, pyridyl; and their physiologically tolerated salts.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings:

R1 CH 3; R2, R3 H;

R4, R5 independently of one another H, (d-C6) alkyl;

R6, R7 independently of one another H, (Ci-C 6) -alkyl, (Ci-C 3) alkylene (C3-C6) cycloalkyl,

(C 3 -C 6) -cycloalkyl, phenyl, OH, O- (Ci-C 6) -alkyl, O- (Ci-C 3) alkylene-phenyl, O- (Ci -C 3) -alkyl kylen- (C 3 -C 6) -cycloal -alkyl, O- (C 3 -C 6) -cycloal alkyl, (Ci -C 3) -alkyl kylen- OH; (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, (Ci-C 3) alkylene-O- (Ci-C 3) alkylene- (C 3 - C 6) alkyl -cycloal , (Ci -C 3) -alkylene-O- (C 3 -C 6) alkyl -cycloal;

R8, R9 independently of one another H, (d-C6) alkyl;

R10, R1 1 is independently H, (d-C6) alkyl; q, r independently of one another 0, 1;

R12, R13 independently of one another H, F, CI, Br, I, CN, O- (Ci-C 6) alkyl, (d-

C 6) alkyl, wherein the O- (Ci-C 6) -alkyl and (Ci-C 6) -alkyl radical may be substituted with F in each case one or more times;

R14 H;

A is phenyl; and their physiologically tolerated salts.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings:

R1 CH 3; R2, R3 H;

R4, R5 independently of one another H, (Ci-C6) alkyl; independently of one another H, (Ci-C6) alkyl, (Ci-C3) -alkylene- (C3-C6) cycloalkyl (C 3 -C 6) -cycloalkyl, phenyl, OH, O- (Ci-C 6) - alkyl, O- (Ci-C 3) alkylene-phenyl, O- (Ci -C 3) -alkyl kylen- (C 3 -C 6) -cycloal -alkyl, O- (C 3 -C 6) alkyl -cycloal , (Ci -C 3) -alkyl kylen- OH; (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, (Ci-C 3) alkylene-O- (Ci-C 3) alkylene- (C 3 - C 6) alkyl -cycloal , (Ci -C 3) -alkylene-O- (C 3 -C 6) alkyl -cycloal;

R8, R9 independently of one another H, (d-C6) alkyl; R10, R1 1 is independently H, (d-C6) alkyl; n, p, q, r are independently 0, 1;

R12, R13 independently of one another H, F, CI, Br, I, CN, O- (Ci-C 6) alkyl, (d-

C 6) alkyl, wherein the O- (Ci-C 6) -alkyl and (Ci-C 6) -alkyl radical may be substituted with F in each case one or more times;

R14 H;

A is pyridyl; and their physiologically tolerated salts.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings: R 1 CH 3;

R2, R3 H; R4, R5 independently of one another H, (Ci-C6) alkyl;

R6, R7 independently of one another H, (Ci-C 6) -alkyl, (Ci-C 3) alkylene (C3-C6) cycloalkyl,

(C 3 -C 6) -cycloalkyl, phenyl, OH, O- (Ci-C 6) -alkyl, O- (Ci-C 3) alkylene-phenyl,

O- (Ci -C 3) -alkyl kylen- (C 3 -C 6) -cycloal -alkyl, O- (C 3 -C 6) -cycloal alkyl, (Ci -C 3) -alkyl kylen- OH; (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, (Ci-C 3) alkylene-O- (Ci-C 3) alkylene- (C 3 - C 6) alkyl -cycloal , (Ci -C 3) -alkylene-O- (C 3 -C 6) alkyl -cycloal; R8, R9 independently of one another H, (d-C6) alkyl;

R10, R1 1 is independently H, (d-C6) alkyl; n, p, q, r are independently 0, 1;

R12, R13 independently of one another H, F, CI, Br, I, CN, O- (Ci-C 6) alkyl, (d-

C 6) alkyl, wherein the O- (Ci-C 6) -alkyl and (Ci-C 6) -alkyl radical may be substituted with F in each case one or more times; R14 H;

A pyrazinyl; and their physiologically tolerated salts.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings: R 1 CH 3;

R2, R3 H; R4, R5 independently of one another H, (d-C6) alkyl;

R6, R7 independently of one another H, (Ci-C 6) -alkyl, (Ci-C 3) alkylene (C3-C6) cycloalkyl,

(C 3 -C 6) -cycloalkyl, phenyl, OH, O- (Ci-C 6) -alkyl, O- (Ci-C 3) alkylene-phenyl, O- (Ci -C 3) -alkyl kylen- (C 3 -C 6) -cycloal -alkyl, O- (C 3 -C 6) -cycloal alkyl, (Ci -C 3) -alkyl kylen- OH; (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, (Ci-C 3) alkylene-O- (Ci-C 3) alkylene- (C 3 - C 6) alkyl -cycloal , (Ci -C 3) -alkylene-O- (C 3 -C 6) alkyl -cycloal;

R8, R9 independently of one another H, (d-C6) alkyl;

R10, R1 1 is independently H, (d-C6) alkyl; q, r independently of one another 0, 1;

R12, R13 independently of one another H, F, CI, Br, I, CN, O- (Ci-C 6) alkyl, (d-

C 6) alkyl, wherein the O- (Ci-C 6) -alkyl and (Ci-C 6) -alkyl radical may be substituted with F in each case one or more times;

R14 H;

A is phenyl, pyridyl, pyrazinyl; and their physiologically tolerated salts.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings:

R1 CH 3;

R2, R3 H; R4, R5 independently of one another H, (Ci-C6) alkyl;

R6, R7 independently of one another H, (Ci-C 6) -alkyl, (Ci-C 3) alkylene (C3-C6) cycloalkyl,

(C 3 -C 6) -cycloalkyl, phenyl, -OH, O- (Ci-C 6) -alkyl, O- (Ci-C 3) alkylene-phenyl, (Ci-C 3) alkylene-OH; (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, (Ci-C 3) -alkylene-O- (Ci-

C 3) alkylene- (C 3 -C 6) cycloalkyl;

R8, R9 independently of one another H, (Ci-C6) alkyl; R10, R1 1 is independently H, (Ci-C 6) alkyl; q, r independently of one another 0, 1;

R12, R13 independently of one another H, F, Cl, Br, I, CN, O- (Ci-C 6) alkyl, (d-

C 6) alkyl, wherein the O- (Ci-C 6) -alkyl and (Ci-C 6) -alkyl radical may be substituted with F in each case one or more times;

R14 H;

A is phenyl, 2-pyridyl, 3-pyridyl, 2-pyrazinyl; and their physiologically tolerated salts.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings:

q, r independently of one another 0, 1; wherein the sum of q and r is equal to 0 and all other groups and numbers in the general definition of

are compounds of formula I or as defined in one of the specified embodiments of the invention or definitions of structural elements.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings:

q, r independently of one another 0, 1; wherein the sum of q and r is equal to 1 and all other groups and numbers in the general definition of the compounds of formula I or in one of the specified embodiments of the invention or definitions of structural elements are defined. A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings:

q, r independently of one another 0, 1; wherein the sum of q and r is equal to 2 and all other groups and numbers in the general definition of the compounds of formula I or in one of the specified embodiments of the invention or definitions of structural elements are defined.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings:

A is phenyl or a 5 to 6-membered heterocycle;

and all other groups and numbers as in the general definition of

are compounds of formula I or as defined in one of the specified embodiments of the invention or definitions of structural elements.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings:

A is phenyl or a 6-membered heterocycle;

and all other groups and numbers in the general definition of the compounds of formula I or in one of the specified embodiments of the invention or definitions of structural elements are defined.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings:

A is phenyl or a 6-membered nitrogen-containing heterocycle;

and all other groups and numbers in the general definition of the compounds of formula I or in one of the specified embodiments of the invention or definitions of structural elements are defined. A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings:

A is phenyl;

and all other groups and numbers as in the general definition of

are compounds of formula I or as defined in one of the specified embodiments of the invention or definitions of structural elements.

A further embodiment relates to compounds of formula I, wherein one or more radicals have the following meanings:

A is a 6-membered nitrogen-containing heterocycle;

and all other groups and numbers as in the general definition of

are compounds of formula I or as defined in one of the specified embodiments of the invention or definitions of structural elements. If radicals or substituents occur more than once in the compounds of the formulas I, they may all, independently of one another have the stated meaning and be identical or different.

The alkyl and alkynyl radicals in the radicals R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R1 1, R12 and R13 may be either straight-chain or branched.

The invention relates to compounds of formula I in the form of their salts, racemates, racemic mixtures and pure enantiomers and the diastereomers thereof and mixtures thereof.

The invention further relates both stereoisomer mixtures of the formula I and the pure stereoisomers of the formula I, and diastereomer mixtures of the formula I and the pure diastereomers. The separation of mixtures, for example by chromatographic means.

The present invention encompasses all possible tautomeric forms of the

Compounds of the formula I. Pharmaceutically acceptable salts are particularly suitable for medical applications because of their greater solubility in water compared with the starting or base compounds. These salts must have a pharmaceutically acceptable anion or cation.

Salts with a pharmaceutically unacceptable anion likewise belong within the framework of the invention as useful intermediates for preparing or purifying pharmaceutically acceptable salts and / or for use in nontherapeutic, for example in-vitro applications.

The compounds of the invention may also exist in different polymorphic forms, for example as amorphous and crystalline polymorphic forms. All polymorphic forms of the compounds of the invention belong within the framework of the invention and are a further aspect of the invention.

Below, all references to "compound (s) of formula I" refer to compound (s) of formula I as described above, and their salts and solvates as described herein.

An alkyl radical means a straight or branched hydrocarbon chain is understood to mean, for example methyl, ethyl, iso-propyl, tert-butyl, hexyl. The alkyl radicals may be substituted one or more times as described above. Heterocycle or heterocyclic radical rings and ring systems are understood which contain other than carbon or heteroatoms, such as nitrogen, oxygen or sulfur. Furthermore, ring systems belong to this definition, which the heterocycle or the heterocyclic radical is fused to a further ring system. The heterocycle or the heterocyclic group may be saturated, partially saturated or aromatic.

The invention also includes solvates, hydrates and alcohol adducts of compounds of the formula I.

The compound (s) of formula I may also be administered in combination with other active ingredients.

The amount of a compound according to formula I which is necessary in order to

to achieve the desired biological effect depends on a number of factors, for example the specific compound chosen, the intended

Use, the mode of administration and the clinical condition of the patient. In general, the daily dose is in the range from 0.3 mg to 100 mg (typically from 3 mg and 50 mg) per day per kilogram of body weight, for example 3-10 mg / kg / day. An intravenous dose may, for example, in the range of 0.3 mg to 1, 0 mg / kg, which can suitably be administered as infusion of 10 ng to 100 ng per kilogram per minute. Suitable infusion solutions for these purposes may, for example, from 0.1 ng to 100 mg, typically from 1 ng to 100 mg, per milliliter. Single doses may contain from 1 mg to 10 g of the active ingredient, for example. Thus, ampoules for injections, for example, from 1 mg to 100 mg, and orally administrable individual dose formulations, such as tablets or capsules, can, for example from 1, 0 to 1000 mg, typically from 10 to 600 mg. For the therapy of the abovementioned conditions, the compounds of formula I can themselves be used as the compound, but they are preferably with an acceptable carrier in the form of a pharmaceutical composition. The carrier must, of course, be acceptable in the sense that he and the other

compatible components of the composition and is not harmful for the patient. The carrier may be a solid or a liquid or both and is preferably formulated with the compound as single dose,

for example a tablet, which can contain wt .-% of the active ingredient of 0.05% to 95 wt. Further pharmaceutically active substances may likewise be present, including other compounds of formula I. The pharmaceutical compositions of the invention can be prepared by one of the known

pharmaceutical methods are prepared which essentially consist in that the constituents are mixed with pharmacologically acceptable carriers and / or excipients.

Inventive pharmaceutical compositions are those which are suitable (for example sublingual) for oral, rectal, topical, peroral and parenteral (eg subcutaneous, intramuscular, intradermal or intravenous) administration, although the most suitable mode of administration in each individual case on the nature and severity of the treated is dependent status and the nature of the compound used according to formula I. Coated formulations and coated slow-release in the context of the invention. acid- and gastric juice-resistant formulations are preferred. Suitable enteric coatings include cellulose acetate phthalate, Poylvinylacetatphthalat,

Hydroxypropylmethylcellulose phthalate and anionic polymers of methacrylic acid and methyl methacrylate.

Suitable pharmaceutical compounds for oral administration may be in separate units, such as capsules, cachets,

Lozenges or tablets, each containing a predetermined amount of the compound according to formula I contain; as powders or granules; as a solution or a suspension in an aqueous or non-aqueous liquid; or as an oil-in-water or water-in-oil emulsion. by any suitable pharmaceutical method These compositions may, as already mentioned, be prepared, which comprises a step, (which may consist of one or more additional ingredients consist) in which the active ingredient and the carrier are brought into contact. In general, the compositions are prepared by uniform and homogeneous mixing of the active ingredient with a liquid and / or finely divided solid carrier, after which the product is shaped if necessary. So can

For example, a tablet can be prepared by mixing a powder or granules of the compound compressing or molding, optionally with one or more accessory ingredients. Compressed tablets can be produced by tableting the compound in free-flowing form such as a powder or granules, optionally mixed with a binder, lubricant, inert diluent and / or one (or more) are surface-active / dispersing agents in a suitable machine. Molded tablets may be made by molding the pulverulent compound, moistened with an inert liquid diluent in a suitable machine.

Pharmaceutical compositions suitable for peroral (sublingual)

Administration are suitable include lozenges which contain a compound of formula I with a flavoring, normally sucrose and gum arabic or tragacanth, and pastilles which comprise the compound in an inert base such as gelatin and glycerol or sucrose and gum arabic.

Suitable pharmaceutical compositions for parenteral administration comprise preferably sterile aqueous preparations of a compound according to formula I, which are preferably isotonic with the blood of the intended recipient. These preparations are preferably administered intravenously, although administration can also take place subcutaneously, intramuscularly or intradermally as an injection. These preparations can preferably be produced by subjecting the compound is mixed with water and the resulting solution is made isotonic with the blood sterile. Injectable compositions according to the invention generally contain from 0.1 to 5 wt .-% of active compound.

Pharmaceutical compositions suitable for rectal administration are preferably present as individual dose suppositories. These can be prepared by reacting a compound of formula I with one or more conventional solid carriers, for example cocoa butter are mixed, and shaping the resulting mixture in the form.

Suitable pharmaceutical compositions for topical use on the skin are preferably present as ointment, cream, lotion, paste, spray, aerosol or oil. As a carrier vaseline, lanolin, polyethylene glycols, alcohols and combinations of two or more of these substances can be used. The active ingredient is generally present in a concentration of 0.1 to 15 wt .-% of the composition, for example from 0.5 to 2%.

Transdermal administration is also possible. Suitable pharmaceutical compositions for transdermal uses can be present as individual patches which are suitable for long-term close contact with the epidermis of the patient. Such patches suitably contain the active compound in an optionally buffered aqueous solution, dissolved and / or dispersed in an adhesive or dispersed in a polymer. A suitable active ingredient concentration is about 1% to 35%, preferably about 3% to 15%. As one particular possibility, the active ingredient, such as, for example, in Pharmaceutical Research, 2 (6): described 318 (1986), be released by electrotransport or iontophoresis.

Further active ingredients for combination products are:

All antidiabetics which are mentioned in the Red List 2010, Chapter 12; all

Drugs for weight loss / appetite suppressants which are mentioned in the Red List 2010, Chapter 1; all diuretics that are listed in the Red List 2010, Chapter 36; all lipid-lowering agents which are mentioned in the Red List 2010, Chapter 58th You can use the

Compound of formula I according to the invention in particular for synergistic

Enhanced action are combined. The administration of the

Active ingredient combination can take place either by separate administration of the active ingredients to the patient or in the form of combination preparations in which several active compounds are present in one pharmaceutical preparation. If the administration of the active ingredients by separate administration of the active ingredients, these may be simultaneous or sequential. Most of the active ingredients listed below are in USP Dictionary of USAN and International Drug Names, US Pharmacopeia, Rockville 2006 is disclosed.

Antidiabetics include insulin and insulin derivatives, such as Lantus ® (see

www.lantus.com) or HMR 1964 or Levemir® (insulin detemir), Humalog (R) (insulin lispro), insulin Degludec, insulin aspart, poly-ethylene glycosidiertes (PEGylated) Insulin Lispro as described in WO2009152128, Humulin (R fast-acting insulins), VlAject ™, SuliXen (R), VlAject ™ or those as are described in WO2005005477 (Novo Nordisk), (see US 6,221, 633), inhalable insulins such. B.

Exubera ®, Nasulin ™, or oral insulins such. B. IN-105 (Nobex) or Oral-lyn ™ (Generex Biotechnology) or Technosphere (R) Insulin (MannKind) or cobalamin ™ oral insulin or ORMD-0801 or insulin precursors or insulin (insulin

precursor) as in WO2007128815, WO2007128817, WO2008034881

WO200804971 1, WO2008145721, WO20090341 17, WO2009060071,

WO2009133099 describes or insulins that can be administered transdermally; are in addition also includes such insulin derivatives represented by a

bifunctional linkers are bound to albumin as described for example in WO2009121884;

GLP-1 derivatives and GLP-1 agonists such as exenatide or special preparations thereof, as described for example in WO2008061355, WO2009080024, WO2009080032 are described, Liraglutide, Taspoglutide (R-1583), Albiglutide, Lixisenatide or those described in WO 98/08871 have been disclosed, WO2005027978, WO200603781 1, WO2006037810 of Novo Nordisk A / S, in WO 01/04156 by Zealand or in WO 00/34331 by Beaufour-Ipsen, pramlintide acetate (Symlin; amylin Pharmaceuticals), inhalable GLP-1 (MKC 253 of the company MannKind), AVE-0010, BIM-51077 (R-1583 ITM-077), PC-DAC: exendin-4 (an exendin-4 analog covalently bonded to recombinant human albumin), biotinylated exendin ( WO2009107900), a special formulation of exendin-4 as described in US2009238879, CVX 73, CVX-98 and-96 CVx (GLP-1 analogues, which are covalently bonded to a monoclonal antibody which has specific binding sites for the GLP- having 1 peptide), CNTO-736 (a GLP-1 analogue which at a domain is bound, which includes the Fc portion of an antibody), PGC-GLP-1 (GLP-1 bound to a nanocarrier) agonists or modulators as described for example in D. Chen et al., Proc. Natl. Acad. Be. US 104 (2007) described 943, such as in

WO2006124529, WO2007124461, WO2008062457, WO2008082274,

WO2008101017, WO2008081418, WO20081 12939, 12941 WO20081,

WO20081 13601, 16294 WO20081, WO20081 16648, 19238 WO20081,

WO2008148839, US2008299096, WO2008152403, WO2009030738,

WO2009030771, WO2009030774, WO2009035540, WO2009058734,

WO20091 1 1700, WO2009125424, WO2009129696, WO2009149148 are described, peptides such as Obinepitide (TM-30338), orally active GLP-1 analogs (eg NN9924 of Novo Nordisk), amylin receptor agonists such as for example, in

WO2007104789, are described in WO20090341 19, analogs of human GLP-1 as described in WO2007120899, WO2008022015, are WO2008056726 describes chimeric pegylated peptides that both GLP-1 - as Glucagonreste contain and how they described for example in WO2008101017, WO2009155257, WO2009155258 are glycosylated GLP-1 derivatives such as are described in WO2009153960, and orally effective hypoglycemic active ingredients.

Antidiabetics also include Gastrinanaloga such as TT-223rd

Further antidiabetic agents include poly- or monoclonal antibodies which are directed against, for example, interleukin-1 beta (IL-1 beta), such as XOMA 052.

Antidiabetic agents further include peptides to the human pro-island

Peptide can bind receptor (human pro-islet petide (HIP) receptor) as described for example in WO2009049222. Antidiabetics also include agonists of the glucose-dependent insulinotropic polypeptide (GIP) receptor as are described for example in WO2006121860.

Antidiabetics also include the glucose-dependent insulinotropic polypeptide (GIP) and analogous compounds as they are for example described in WO2010016944 WO2008021560, WO2010016935, WO2010016936, WO2010016938, WO2010016940.

Further included are analogues and derivatives of the human pancreatic polypeptide (human pancreatic polypeptides), for example as described in WO2009007714

are described. Antidiabetics also include encapsulated insulin-producing cells, such as porcine DiabeCell (R).

Antidiabetics also include analogs and derivatives of fibroblast growth factor 21 (FGF-21, fibroblast growth factor 21) as described for example in WO2009149171,

WO2010006214 described.

The orally effective hypoglycemic active ingredients include preferably

sulfonylureas,

biguanides,

meglitinides,

oxadiazolidinediones,

thiazolidinediones,

PPAR and RXR modulators,

Glucosidase inhibitors,

Inhibitors of glycogen phosphorylase,

Glucagon receptor antagonists,

glucokinase

Inhibitors of fructose-1, 6-bisphosphatase, modulators of the glucose transporter 4 (GLUT4),

Inhibitors of glutamine-fructose-6-phosphate amidotransferase (GFAT),

GLP-1 agonists,

Potassium channel openers, such as pinacidil, cromakalim, diazoxide, diazoxide choline salt or such as in RD Carr et al., Diabetes 52, 2003, 2513.2518, with JB Hansen et al, Current Medicinal Chemistry 11, 2004, 1595-1615, at TM Tagmose et al., J. Med. Chem. 47, 2004 3202-321 1 or MJ Coghlan et al., J. Med. Chem. 44, 2001 are described 1627-1653, or those described in WO 97 / 26265 and WO 99/03861 were disclosed by Novo Nordisk A / S,

Agents acting on the ATP-dependent potassium channel of the beta cells,

Inhibitors of dipeptidyl peptidase-IV (DPP-IV),

Insulin sensitizers,

Inhibitors of liver enzymes involved in the stimulation of gluconeogenesis and / or glycogenolysis,

Modulators of glucose uptake, of glucose transport and of

glucose reabsorption,

Modulators of the sodium-dependent glucose transporter 1 or 2 (SGLT1, SGLT2), inhibitors of 1 1 -beta-hydroxysteroid dehydrogenase-1 (1 1 beta-HSD1),

Inhibitors of protein tyrosine phosphatase 1 B (PTP-1 B),

Nicotinic receptor agonists,

Inhibitors of hormone-sensitive or endothelial lipases,

Inhibitors of acetyl-CoA carboxylase (ACC1 and / or ACC2) or

Inhibitors of GSK-3 beta.

Furthermore includes the compounds which alter lipid metabolism, such as antihyperlipidemic active ingredients and antilipidemic active ingredients,

HM GCoA- Red u ktase- 1 NHib itoren,

Farnesoid X receptor (FXR) modulators,

fibrates,

Cholesterinresorptionsinhibitoren,

CETP inhibitors,

bile acid,

MTP inhibitors, agonists of the estrogen receptor gamma (ERR agonist),

Sigma-1 receptor antagonist,

Antagonists of the somatostatin 5 receptor (SST5 receptor);

Compounds which reduce food intake, and

Compounds which increase thermogenesis.

In one embodiment of the invention, the compound of formula I is

Combination administered with insulin.

In another embodiment of the invention, the compound of formula I in combination with an insulin sensitizer such as PN-2034 or ISIS 13715 is administered 1.

In one embodiment, the compound of formula I in combination with an agent acting on the ATP-dependent potassium channel of the beta cells, such as

Sulfonylureas, such as tolbutamide, glibenclamide, glipizide, gliclazide or

Glimepiride or such formulations as are described for example in EP2103302 administered.

In one embodiment, the compound of formula I is administered in combination with a tablet containing both glimepiride, which is rapidly released and also contains metformin, which is released over a longer period (for example in US2007264331, WO2008050987, WO2008062273 described).

In one embodiment, the compound of formula I in combination with a biguanide, is administered such as metformin or one of its salts.

In a further embodiment, the compound of formula I in combination with a guanidine, such as benzylguanidine or a salt thereof, or guanidines such as are described in WO2009087395, is administered. In yet another embodiment, the compound of formula I in combination with a meglitinide, such as repaglinide, nateglinide or mitiglinide is administered.

In a further embodiment, the compound of formula I with a combination of mitiglinide with a glitazone, for example pioglitazone hydrochloride is administered.

In a further embodiment, the compound of the formula I is administered with a combination of mitiglinide with an alpha-glucosidase inhibitor.

In another embodiment, the compound of formula I in combination with antidiabetic compounds as administered in WO2007095462, WO2007101060, WO2007105650 are described.

In another embodiment, the compound of formula I in combination with antihypoglykamischen compounds, such as are described in WO2008020607 WO2007137008 administered.

In one embodiment, the compound of formula I in combination with a thiazolidinedione, such as troglitazone, ciglitazone, pioglitazone, rosiglitazone or in WO 97/41097 of Dr. Reddy's Research Foundation disclosed compounds, in particular 5 - [[4 - phenyl] methyl - [(3,4-dihydro-3-methyl-4-oxo-2-chinazolinylmethoxy]] -2,4-thiazolidinedione administered.

In one embodiment of the invention, the compound of formula I is

Combination with a PPAR gamma agonist such as, for example, rosiglitazone, pioglitazone, JTT-501, Gl 262570, R-483, CS-01 1 (Rivoglitazon), DRL-17564, DRF-2593

(Balaglitazon), INT-131, T-2384, or such as in WO2005086904

WO2007060992, WO2007100027, WO2007103252, WO2007122970,

WO2007138485, WO2008006319, WO2008006969, WO2008010238,

WO2008017398, WO2008028188, WO2008066356, WO2008084303,

WO2008089461 -WO2008089464, WO2008093639, WO2008096769, WO2008096820, WO2008096829, US2008194617, WO2008099944,

WO2008108602, WO2008109334, WO20081 10062, WO2008126731,

WO2008126732, WO2008137105, WO2009005672, WO2009038681,

WO2009046606, WO2009080821, WO2009083526, WO2009102226,

WO2009128558, are described in WO2009139340, is administered.

In one embodiment of the invention, the compound of formula I is

Combination with Competact ™, a fixed combination of pioglitazone hydrochloride with metformin hydrochloride administered.

In one embodiment of the invention, the compound of formula I is

Combination with Tandemact ™, a fixed combination of pioglitazone with

Glimepiride administered. In a further embodiment of the invention the compound of formula I in combination with a fixed combination of pioglitazone hydrochloride with an angiotensin II agonist, such as TAK-536, is administered.

In one embodiment of the invention, the compound of formula I is

Combination with a PPAR alpha agonists or mixed PPAR alpha / PPAR delta agonist such as, for example, GW9578, GW-590735, K-1 1 1, LY-674, KRP-101, DRF 10945, LY-518674, CP-900691, BMS-687453, BMS-71 1939 or those as are described in WO2001040207, WO2002096894, WO2005097076, WO2007056771

WO2007087448, WO2007089667, WO2007089557, WO2007102515,

WO2007103252, JP2007246474, WO20071 18963, WO20071 18964, WO2007126043, WO2008006043, WO2008006044, WO2008012470, WO2008035359,

WO2008087365, WO2008087366, WO2008087367, WO20081 17982, JP2009023975, WO2009033561, WO2009047240, WO2009072581, WO2009080248,

WO2009080242, WO2009149819, WO2009149820, WO2009147121,

WO2009153496, WO2010008299, WO2010014771 described administered. In one embodiment of the invention, the compound of formula I is

Combination with a mixed PPAR alpha / gamma agonist, such as

Naveglitazar, Aleglitazar, LY-510929, ONO-5129, E-3030, AVE 8042, AVE 8134, AVE 0847, CKD-501 (Lobeglitazon sulfate), MBX-213, KY-201, BMS-759509 or as described in WO 00 / 64888, WO 00/64876, WO03 / 020269, WO2004024726, WO2007099553, US2007276041, WO2007085135, WO2007085136, WO2007141423,

WO2008016175, WO2008053331, WO2008109697, WO2008109700,

WO2008108735, WO2009026657, WO2009026658, WO2009149819,

WO2009149820 or in JP Berger et al., TRENDS in Pharmacological Sciences 28 (5), 244-251, described in 2005, is administered.

In one embodiment of the invention, the compound of formula I is

Combination with a PPAR delta agonist such as GW-501516, or as are described in WO2006059744, WO2006084176, WO2006029699, WO2007039178 WO2007039172-, WO2007071766, WO2007101864, US2007244094

WO20071 19887, WO2007141423, US2008004281, WO2008016175,

WO2008066356, WO200807131 1, WO2008084962, US2008176861,

WO2009012650, US2009137671, WO2009080223, WO2009149819,

WO2009149820, are described in WO2010000353, is administered.

In one embodiment of the invention, the compound of formula I is

Combination with a pan-SPPARM (selective PPAR modulator alpha, gamma, delta), such as GFT-505, Indeglitazar or such as are described in WO2008035359, WO2009072581, administered.

In one embodiment, the compound of formula I in combination with metaglidasen or with MBX-2044 or other partial PPAR gamma is

Agonists / antagonists administered.

In one embodiment, the compound of formula I in combination with an α-glucosidase inhibitor, such as miglitol or acarbose, or such, as they are described for example in WO20071 14532, WO2007140230, US2007287674, US2008103201, WO2008065796, WO2008082017, US2009076129, administered.

In one embodiment, the compound of formula I in combination with an inhibitor of glycogen phosphorylase, such as, for example, PSN-357 or FR-258900 or those described in WO2003084922, WO2004007455, WO2005073229-31, is

WO2005067932, WO2008062739, WO2008099000, WO20081 13760,

WO20090161 18, WO20090161 19, WO2009030715, WO2009045830,

described WO2009045831, WO2009127723, administered.

In another embodiment, the compound of formula I in combination with an inhibitor of the interaction of the Leberglykogenphosphorylase with the protein PPP1 R3 (GL-subunit of glycogen-associated protein phosphatase 1 (PP1)), as described for example in WO2009030715, is administered.

In one embodiment, the compound of formula I in combination with

Glucagon receptor antagonists such as A-770077 or NNC-25-2504 or as described in WO2004100875, WO2005065680, WO2006086488, WO2007047177,

WO2007106181, WO20071 1, 1864, WO2007120270, WO2007120284,

WO2007123581, WO2007136577, WO2008042223, WO2008098244,

WO2009057784, WO2009058662, WO2009058734, WO20091 10520,

WO2009120530, WO2009140342, WO2010019828 describes administered.

In a further embodiment, the compound of formula I in combination with an antisense compound, for example, ISIS 325568 is administered, which inhibits the production of the glucagon receptor.

In one embodiment, the compound of formula I in combination with activators of glucokinase, such. B. LY-2121260 (WO2004063179), PSN-105, PSN 1 to 10, GKA-50 or those as such. As in WO2004072031, WO2004072066,

WO2005080360, WO2005044801, WO2006016194, WO2006058923,

WO20061 12549, WO2006125972, WO2007017549, WO2007017649,

WO2007007910, WO2007007040-42, WO2007006760-61, WO2007006814,

WO2007007886, WO2007028135, WO2007031739, WO2007041365,

WO2007041366, WO2007037534, WO2007043638, WO2007053345,

WO2007051846, WO2007051845, WO2007053765, WO2007051847,

WO2007061923, WO2007075847, WO2007089512, WO2007104034,

WO20071 17381, WO2007122482, WO2007125103, WO2007125105,

US2007281942, WO2008005914, WO2008005964, WO2008043701,

WO2008044777, WO2008047821, US2008096877, WO20080501 17,

WO2008050101, WO2008059625, US2008146625, WO2008078674,

WO2008079787, WO2008084043, WO2008084044, WO2008084872,

WO2008089892, WO2008091770, WO2008075073, WO2008084043,

WO2008084044, WO2008084872, WO2008084873, WO2008089892,

WO2008091770, JP2008189659, WO2008104994, WO20081 1 1473 WO20081 16107, WO20081 18718, WO2008120754, US2008280875, WO2008136428,

WO2008136444, WO2008149382, WO2008154563, WO2008156174,

WO2008156757, US2009030046, WO2009018065, WO2009023718,

WO2009039944, WO2009042435, WO2009046784, WO2009046802,

WO2009047798, WO2009063821, WO2009081782, WO2009082152,

WO2009083553, WO2009091014, US2009181981, WO2009092432,

WO2009099080, WO2009106203, WO2009106209, WO2009109270,

WO2009125873, WO2009127544, WO2009127546, WO2009128481,

WO2009133687, WO2009140624, WO2010013161, WO2010015849,

WO2010018800 describes administered.

In one embodiment, the compound of formula I in combination with an inhibitor of gluconeogenesis, such as z. As in FR-225654, WO2008053446

are described administered. In one embodiment, the compound of formula I in combination with inhibitors of fructose-1, 6-bisphosphatase (FBPase), such as MB-07729, CS-917 (MB-06322) or MB-07803 or those as are described in WO2006023515 is

WO2006104030, WO2007014619, WO2007137962, WO2008019309,

WO2008037628, WO2009012039, EP2058308, WO2009068467, WO2009068468 described administered.

In one embodiment, the compound of formula I in combination with modulators of glucose transporter 4 (GLUT4), such as. B. KST-48 (D.-O. Lee et al .: Arzneim.-Forsch. Drug Res. 54 (12), 835 (2004)) administered.

In one embodiment, the compound of formula I in combination with inhibitors of glutamine-fructose-6-phosphate amidotransferase (GFAT), as z. As are described in WO2004101528 administered.

In one embodiment, the compound of formula I in combination with inhibitors of dipeptidylpeptidase IV (DPP-IV) is such. B. vildagliptin (LAF-237), sitagliptin (MK-0431), sitagliptin phosphate, saxagliptin (BMS-4771 18), GSK-823093, PSN-9301, SYR-322, SYR-619, TA-6666, TS-021 , GRC-8200 (Melogliptin), GW-825964X, KRP-104, DP-893, ABT-341, ABT-279 or another salt thereof, S 40010, S-40755, PF-00734200, BI-1356, PHX -1149, DSP 7238, Alogliptin benzoate, linagliptin, Melogliptin, Carmegliptin or such compounds as described in

WO2003074500, WO2003106456, WO2004037169, WO200450658, WO2005037828, WO2005058901, WO2005012312, WO2005 / 012308, WO2006039325,

WO2006058064, WO2006015691, WO2006015701, WO2006015699,

WO2006015700, WO20060181 17, WO2006099943, WO2006099941, JP2006160733, WO2006071752, WO2006065826, WO2006078676, WO2006073167,

WO2006068163, WO2006085685, WO2006090915, WO2006104356,

WO2006127530, WO20061 1 1261, US2006890898, US2006803357, US2006303661, WO2007015767 (LY-2463665), WO2007024993, WO2007029086, WO2007063928, WO2007070434, WO2007071738, WO2007071576, WO2007077508,

WO2007087231, WO2007097931, WO2007099385, WO2007100374, WO20071 12347, WO20071 12669, WO20071 13226, WO20071 13634, WO20071 15821, WO20071 16092, US2007259900, EP1852108, US2007270492, WO2007126745, WO2007136603, WO2007142253, WO2007148185,

WO2008017670, US2008051452, WO2008027273, WO2008028662,

WO2008029217, JP2008031064, JP2008063256, WO2008033851, WO2008040974, WO2008040995, WO2008060488, WO2008064107, WO2008066070,

WO2008077597, JP2008156318, WO2008087560, WO2008089636, WO2008093960, WO2008096841, WO2008101953, WO20081 18848, 19005 WO20081,

WO20081 19208, WO2008120813, WO2008121506, WO2008130151,

WO2008131 149, WO2009003681, WO2009014676, WO2009025784,

WO2009027276, WO2009037719, WO2009068531, WO2009070314,

WO2009065298, WO2009082134, WO2009082881, WO2009084497,

WO2009093269, WO2009099171, WO2009099172, WO20091 1 1239,

WO20091 13423, WO20091 16067, US2009247532, WO2010000469, WO2010015664 described are administered.

In one embodiment, the compound of formula I in combination with Janumet ™, a fixed combination of sitagliptin phosphate with metformin is

Hydrochloride is administered.

In one embodiment, the compound of formula I in combination with Eucreas (R), a fixed combination of vildagliptin with metformin hydrochloride is administered. In another embodiment, the compound of formula I in combination with a fixed combination of Alogliptin benzoate is administered with pioglitazone.

In one embodiment, the compound of formula I is administered in combination with a fixed combination of a salt of sitagliptin with metformin hydrochloride. In one embodiment, the compound of formula I in combination with a combination of a DPP-IV inhibitor with omega-3 fatty acids or omega-3 fatty acid esters is, as described for example in WO2007128801, is administered. In one embodiment, the compound of formula I in combination with a combination of a DPP-IV inhibitor with metformin hydrochloride, for example in

WO2009121945 describes administered.

In one embodiment, the compound of formula I in combination with a combination of a DPP-IV inhibitor with a GPR 1 19 agonist, such as described in WO2009123992, is administered.

In one embodiment, the compound of formula I in combination with a combination of a DPP-IV inhibitor with Miglitol, as described for example in WO2009139362, is administered.

In one embodiment, the compound of formula I in combination with a fixed combination of a salt of sitagliptin is administered with metformin hydrochloride.

In one embodiment, the compound of formula I in combination with a fixed combination of Alopliptin benzoate is administered with pioglitazone hydrochloride.

In one embodiment, the compound of formula I in combination with an insulin secretion-enhancing substance, such. For example, KCP-265 (WO2003097064) or those as are described in WO2007026761, WO2008045484, US2008194617

WO2009109259, are described in WO2009109341, is administered.

In one embodiment, the compound of formula I in combination with agonists of the glucose-dependent insulinotropic receptor (GDIR) such. For example, APD-668 administered. In one embodiment of the invention, the compound of formula I is

Combination with an ATP-citrate lyase inhibitor, such as SB-204990.

In one embodiment, the compound of formula I in combination with modulators of the sodium-dependent glucose transporter 1 and / or 2 (SGLT1, SGLT2), as for example, KGA-2727, T-1095, SGL-0010, AVE 2268, SAR 7226, SGL -5,083, SGL-5085, SGL-5094, ISIS 388626, Sergliflozin, dapagliflozin or Remogliflozin Etanobat, CANAGLIFLOZIN or as such. As in WO2004007517, WO200452903,

WO200452902, PCT / EP2005 / 005959, WO2005085237, JP2004359630,

WO2005121 161, WO2006018150, WO2006035796, WO2006062224,

WO2006058597, WO2006073197, WO2006080577, WO2006087997,

WO2006108842, WO2007000445, WO2007014895, WO2007080170,

WO2007093610, WO20071261 17, WO2007128480, WO2007129668,

US2007275907, WO20071361 16, WO2007143316, WO2007147478,

WO2008001864, WO2008002824, WO2008013277, WO2008013280,

WO2008013321, WO2008013322, WO2008016132, WO200802001 1, JP2008031 161, WO2008034859, WO2008042688, WO2008044762, WO2008046497,

WO2008049923, WO2008055870, WO2008055940, WO2008069327,

WO2008070609, WO2008071288, WO2008072726, WO2008083200,

WO2008090209, WO2008090210, WO2008101586, WO2008101939,

WO20081 16179, WO20081 16195, US2008242596, US2008287529, WO2009026537,

WO2009049731, WO2009076550, WO2009084531, WO2009096503,

WO2009100936, WO2009121939, WO2009124638, WO2009128421,

WO2009135673, WO2010009197, WO2010018435, WO2010018438 or by AL Handion in Expert Opin. Ther. Patents (2005) 15 (1 1), 1531 -1540 are described administered.

In a further embodiment of the invention, the compound of formula I in combination with a fixed combination of an SGLT inhibitor with a DPP-IV inhibitor, as described in WO2009091082, is administered. In one embodiment, the compound of formula I in combination with a stimulator of glucose transport, as described for example in WO2008136392, WO2008136393, administered. In one embodiment, the compound of formula I in combination with inhibitors of 1 1 -beta-hydroxysteroid dehydrogenase-1 (1 1 beta-HSD1), such as is. B. BVT-2733, JNJ-25918646, INCB-13739, INCB-20817, DIO-92 ((-) - ketoconazole) or those as such. B. WO200190090-94, WO200343999, WO20041 12782,

WO200344000, WO200344009, WO20041 12779, WO20041 13310, WO2004103980, WO20041 12784, WO2003065983, WO2003104207, WO2003104208,

WO2004106294, WO200401 1410, WO2004033427, WO2004041264,

WO2004037251, WO2004056744, WO2004058730, WO2004065351,

WO2004089367, WO2004089380, WO2004089470-71, WO2004089896,

WO2005016877, WO2005063247, WO2005097759, WO2006010546,

WO2006012227, WO2006012173, WO2006017542, WO2006034804,

WO2006040329, WO2006051662, WO2006048750, WO2006049952,

WO2006048331, WO2006050908, WO2006024627, WO2006040329,

WO2006066109, WO2006074244, WO2006078006, WO2006106423,

WO2006132436, WO2006134481, WO2006134467, WO2006135795,

WO2006136502, WO2006138508, WO2006138695, WO2006133926,

WO2007003521, WO2007007688, US2007066584, WO2007029021,

WO2007047625, WO200705181 1, WO2007051810, WO2007057768,

WO2007058346, WO2007061661, WO2007068330, WO2007070506,

WO2007087150, WO2007092435, WO2007089683, WO2007101270,

WO2007105753, WO2007107470, WO2007107550, WO20071 1 1921

US2007207985, US2007208001, WO20071 15935, 18185 WO20071, WO200712241 1,

WO2007124329, WO2007124337, WO2007124254, WO2007127688,

WO2007127693, WO2007127704, WO2007127726, WO2007127763,

WO2007127765, WO2007127901, US2007270424, JP2007291075, WO2007130898, WO2007135427, WO2007139992, WO2007144394, WO2007145834.

WO2007145835, WO2007146761, WO2008000950, WO2008000951,

WO200800361 1, WO2008005910, WO2008006702, WO2008006703, WO200801 1453 WO2008012532, WO2008024497, WO2008024892, WO2008032164, WO2008034032, WO2008043544, WO2008044656,

WO2008046758, WO2008052638, WO2008053194, WO2008071 169,

WO2008074384, WO2008076336, WO2008076862, WO2008078725,

WO2008087654, WO2008088540, WO2008099145, WO2008101885,

WO2008101886, WO2008101907, WO2008101914, WO2008106128,

WO20081 10196, WO20081 19017, WO2008120655, WO2008127924,

WO2008130951, WO2008134221, WO2008142859, WO2008142986,

WO2008157752, WO2009001817, WO2009010416, WO2009017664,

WO2009020140, WO2009023180, WO2009023181, WO2009023664,

WO2009026422, WO2009038064, WO2009045753, WO2009056881,

WO2009059666, WO2009061498, WO2009063061, WO2009070497,

WO2009074789, WO2009075835, WO2009088997, WO2009090239,

WO2009094169, WO2009098501, WO2009100872, WO2009102428,

WO2009102460, WO2009102761, WO2009106817, WO2009108332,

WO20091 12691, 12845 WO20091, WO20091 14173, 17109 WO20091,

US2009264401, WO20091 18473, WO2009131669, WO2009132986,

WO2009134384, WO2009134387, WO2009134392, WO2009134400,

WO2009135581, WO2009138386, WO2010006940, WO2010010157,

WO2010010174, WO201001 1917 are described administered.

In one embodiment, the compound of formula I in combination with inhibitors of protein tyrosine phosphatase 1 B (PTP-1 B), as z. B.

WO2001 19830-31, WO2001 17516, WO2004506446, WO2005012295,

WO20051 16003, WO20051 16003, WO2006007959, DE 10 2004 060542.4, WO200700991 1, WO2007028145, WO2007067612-615, WO2007081755,

WO20071 15058, US2008004325, WO2008033455, WO2008033931,

WO2008033932, WO2008033934, WO2008089581, WO2008148744,

are described in WO2009032321, WO2009109999, WO2009109998, administered. In another embodiment, the compound of formula I in combination with stimulators tyrosine kinase B (Trk-B) is as such. As are described in WO2010014613 administered.

In one embodiment of the invention, the compound of formula I is

Combination with an agonist of GPR109A (HM74A receptor agonist; NAR agonist (nicotinic acid receptor agonists)), such as nicotinic acid or "extended release niacin" in conjunction with MK-0524A (laropiprant) or MK-0524 or those compounds as are described in WO2004041274 WO2006045565, WO2006045564,

WO2006069242, WO2006085108, WO20060851 12, WO20060851 13,

WO2006124490, WO20061 13150, WO2007002557, WO2007017261,

WO2007017262, WO2007017265, WO2007015744, WO2007027532,

WO2007092364, WO2007120575, WO2007134986, WO2007150025,

WO2007150026, WO2008016968, WO2008051403, WO2008086949,

WO2008091338, WO2008097535, WO2008099448, US2008234277, WO2008127591 described administered.

In another embodiment of the invention the compound of formula I in combination with a fixed combination of niacin is administered with simvastatin.

In another embodiment of the invention, the compound of formula I in combination with nicotinic acid or administered "extended release niacin" in conjunction with MK-0524A (laropiprant) is.

In a further embodiment of the invention, the compound of formula I in combination with nicotinic acid or "extended release niacin" is administered in conjunction with MK-0524A (laropiprant) and with simvastatin. In one embodiment of the invention, the compound of formula I is in

Combination with nicotinic acid or another Nicotinsäurerezeptoragonisten and a prostaglandin DP receptor antagonists such as those as described in WO2008039882, is administered.

In another embodiment of the invention the compound of formula I in combination with a fixed combination of niacin with meloxicam is, as described for example in WO2009149056, is administered.

In another embodiment of the invention, the compound of formula I in combination with an agonist of the GPR1 16, as they are for example described in WO2006067532 WO2006067531 administered.

In one embodiment, the compound of formula I in combination with modulators of GPR40, as described for example in WO2007013689, WO2007033002,

WO2007106469, US2007265332, WO2007123225, WO2007131619,

WO2007131620, WO2007131621, US2007265332, WO2007131622,

WO2007136572, WO2008001931, WO2008030520, WO2008030618,

WO2008054674, WO2008054675, WO2008066097, US2008176912,

WO2008130514, WO2009038204, WO2009039942, WO2009039943,

WO2009048527, WO2009054479, WO2009058237, WO20091 1 1056,

WO2010012650 describes administered.

In one embodiment, the compound of formula I in combination with modulators of the GPR1 19 (G-protein-coupled glucose-dependent insulinotropic receptor) is such as PSN-1 19-1, PSN-821, PSN-1 19-2, MBX -2982 or those as such. B. in WO2004065380, WO2005061489 (PSN-632408), WO2006083491,

WO2007003960-62 and WO2007003964, WO2007035355, WO20071 16229,

WO20071 16230, WO2008005569, WO2008005576, WO2008008887,

WO2008008895, WO2008025798, WO2008025799, WO2008025800,

WO2008070692, WO2008076243, WO200807692, WO2008081204, WO2008081205, WO2008081206, WO2008081207, WO2008081208, WO2008083238, WO2008085316, WO2008109702, WO2008130581, WO2008130584, WO2008130615, WO2008137435, WO2008137436, WO2009012275,

WO2009012277, WO2009014910, WO2009034388, WO2009038974,

WO2009050522, WO2009050523, WO2009055331, WO2009105715,

WO2009105717, WO2009105722, WO2009106561, WO2009106565,

WO20091 17421, WO2009125434, WO2009126535, WO2009129036,

US2009286812, WO2009143049, WO2009150144, WO2010001 166,

WO2010004343, WO2010004344, WO2010004345, WO2010004346,

WO2010004347, WO2010004348, WO2010008739, WO2010006191,

WO2010009183, WO2010009195, WO2010009207, WO2010009208,

WO2010014593 describes administered.

In a further embodiment, the compound of formula I in combination with modulators of GPR120, as described for example in EP1688138, WO2008066131,

WO2008066131, WO2008103500, WO2008103501, WO2008139879,

WO2009038204, WO2009147990, WO2010008831 described administered.

In another embodiment, the compound of formula I in combination with antagonists of the GPR105, as they are described for example in WO2009000087, WO2009070873, administered.

In another embodiment, the compound of formula I in combination with agonists of GPR43, as administered, for example, ESN-282nd In one embodiment, the compound of formula I in combination with

Inhibitors of hormone-sensitive lipase (HSL) and / or phospholipases such. B. in WO2005073199, WO2006074957, WO2006087309, WO20061 1 1321,

WO2007042178, WO20071 19837, WO2008122352, WO2008122357,

WO2009009287 describes administered. In one embodiment, the compound of formula I in combination with inhibitors of endothelial lipase, as z. As described in WO20071 10216 administered. In one embodiment, the compound of formula I in combination with a phospholipase A2 inhibitor such as Darapladib or A-002 or such, as described in WO2008048866, WO20080488867, US2009062369 administered.

In one embodiment, the compound of formula I in combination with myricitrin is administered a lipase inhibitor (WO20071 19827).

In one embodiment, the compound of formula I in combination with an inhibitor of glycogen synthase kinase-3 beta (GSK-3 beta), as z. B.

US2005222220, WO2005085230, WO20051 1 1018, WO2003078403,

WO2004022544, WO2003106410, WO2005058908, US2005038023,

WO2005009997, US2005026984, WO2005000836, WO2004106343, EP1460075, WO2004014910, WO2003076442, WO2005087727, WO20040461 17,

WO20070731 17, WO2007083978, WO2007120102, WO2007122634,

WO2007125109, WO20071251 10, US2007281949, WO2008002244,

WO2008002245, WO2008016123, WO2008023239, WO2008044700,

WO2008056266, WO2008057940, WO2008077138, EP1939191, EP1939192, WO2008078196, WO2008094992, WO20081 12642, 12651 WO20081,

WO20081 13469, WO2008121063, WO2008121064, EP-1992620, EP-1992621, EP1992624, EP-1992625, WO2008130312, WO2009007029, EP2020232,

WO2009017452, WO2009035634, WO2009035684, WO2009038385,

WO2009095787, WO2009095788, WO2009095789, WO2009095792,

WO2009145814, US2009291982, WO2009154697, WO2009156857,

WO2009156859, WO2009156860, WO2009156861, WO2009156863,

WO2009156864, WO2009156865, WO2010013168, WO2010014794 described. In one embodiment, the compound of formula I in combination with an inhibitor of phosphoenolpyruvate carboxykinase (PEPCK), as for example those as described in WO2004074288, is administered. In one embodiment, the compound of formula I in combination with an inhibitor of Phosphoinositidkinase-3 (PI3K) is, for example such as in WO2008027584, WO2008070150, WO2008125833, WO2008125835, WO2008125839

WO2009010530, WO2009026345, WO2009071888, WO2009071890,

WO2009071895 describes administered.

In one embodiment, the compound of formula I in combination with an inhibitor of the serum / glucocorticoid regulated kinase (SGK), such. B.

WO2006072354, WO2007093264, WO2008009335, WO2008086854,

WO2008138448 describes administered.

In one embodiment, the compound of formula I in combination with a modulator of glucocorticoid receptor, such. As in WO2008057855, WO2008057856, WO2008057857, WO2008057859, WO2008057862, WO2008059867,

WO2008059866, WO2008059865, WO2008070507, WO2008124665,

WO2008124745, WO2008146871, WO2009015067, WO2009040288,

WO2009069736, WO2009149139 describes administered.

In one embodiment, the compound of formula I in combination with a modulator of mineralocorticoid receptor (MR), as z. B. Drospirenone, or such as in WO2008104306 administered, WO20081 19918 are described.

In one embodiment, the compound of formula I in combination with an inhibitor of protein kinase C beta (PKC beta), as z. B. ruboxistaurin, or such as are described in WO2008096260, WO2008125945, administered. In one embodiment, the compound of formula I in combination with an inhibitor of protein kinase D is such. B. doxazosin (WO2008088006) administered.

In a further embodiment, the compound of formula I in combination with an activator / modulator of the AMP-activated protein kinase (AMPK), as z. As in WO2007062568, WO2008006432, WO2008016278, WO2008016730,

WO2008020607, WO2008083124, WO2008136642, WO2009019445,

WO2009019446, WO2009019600, WO2009028891, WO2009065131,

WO2009076631, WO2009079921, WO2009100130, WO2009124636,

WO2009135580, are described in WO2009152909, is administered.

In one embodiment, the compound of formula I in combination with an inhibitor of Ceramidkinase is as such. B. in WO20071 12914, WO2007149865 described administered.

In another embodiment, the compound of formula I in combination with an inhibitor of MAPK-interacting kinase 1 or 2 (MNK1 or 2), as they are described for example in WO2007104053, WO20071 15822, WO2008008547, WO2008075741, administered.

In one embodiment, the compound of formula I in combination with inhibitors of "Ι-kappaB kinase" (IKK inhibitors), as z. B. in WO2001000610, WO2001030774, WO2004022057, WO2004022553, WO2005097129,

WO20051 13544, US2007244140, WO2008099072, WO2008099073,

WO2008099073, WO2008099074, WO2008099075, WO2009056693,

WO2009075277, WO2009089042, WO2009120801 described administered.

In another embodiment, the compound of formula I in combination with inhibitors of NF-kappaB is (NFKB) Activation, as z. B. salsalate administered. In a further embodiment, the compound of formula I in combination with inhibitors of ASK-1 (apoptosis signal-regulating kinase 1) as z. B.

WO2008016131, are described in WO2009123986, is administered. In one embodiment of the invention, the compounds of formula I is in

Combination with an HMGCoA reductase inhibitor such as simvastatin, fluvastatin, pravastatin, lovastatin, atorvastatin, cerivastatin, rosuvastatin, pitavastatin, L-659699, BMS-644950, NCX-6560 or those as are described in US2007249583

WO2008083551, are described in WO2009054682, is administered.

In a further embodiment of the invention, the compound of formula I in combination with a farnesoid X is receptor (FXR) modulators, such as WAY 362450 or those described in WO2003099821, WO2005056554, WO2007052843, WO2007070796, WO2007092751, JP2007230909, WO2007095174, WO2007140174, WO2007140183 , WO2008000643, WO2008002573, WO2008025539,

WO2008025540, JP2008214222, JP2008273847, WO2008157270, US20082991 18, US2008300235, WO2009005998, WO2009012125, WO2009027264,

WO2009062874, US2009131409, US2009137554, US2009163552, WO2009127321, EP2128158 describes administered.

(Liver X receptor; LXR) In another embodiment of the invention the compound of formula I in combination with a ligand of the liver X receptor is, for example, in WO2007092965, WO2008041003, WO2008049047, WO2008065754

WO2008073825, US2008242677, WO2009020683, US2009030082, WO2009021868, US2009069373, WO2009024550, WO2009040289, WO2009086123,

WO2009086129, WO2009086130, WO2009086138, WO2009107387,

US2009247587, WO2009133692, WO2008138438, WO2009144961, administered WO2009150109 described. In one embodiment of the invention, the compound of formula I is

Combination with a fibrate, such as fenofibrate, clofibrate, bezafibrate, or such as are described in WO2008093655, is administered. In one embodiment of the invention, the compound of formula I is

Combination with fibrates, such as the choline salt of fenofibrate (SLV-348; Trilipix ™) administered.

In one embodiment of the invention, the compound of formula I is

Combination with fibrates, such as the choline salt of fenofibrate (Trilipix ™) and an HMGCoA reductase inhibitor, such as rosuvastatin administered. In a further embodiment of the invention the compound of formula I in combination with bezafibrate and diflunisal administered.

In a further embodiment of the invention the compound of formula I in combination with a fixed combination of fenofibrate or a salt thereof with simvastatin, rosuvastatin, fluvastatin, lovastatin, cerivastatin, pravastatin,

Pitavastatin or atorvastatin administered.

In a further embodiment of the invention, the compound of formula I in combination with Synordia (R), a fixed combination of fenofibrate with metformin.

In another embodiment of the invention, the compound of formula I in combination with a fixed combination of metformin is described with an MTP inhibitor such as in WO2009090210 administered.

In one embodiment of the invention, the compound of formula I is

Combination with a cholesterol such as ezetimibe, tiqueside, pamaqueside, FM-VP4 (sitostanol / campesterol ascorbyl phosphate; Forbes Medi-Tech, WO2005042692, WO2005005453), MD-0727 (Microbia Inc., WO2005021497,

WO2005021495) or with compounds as described in WO2002066464, WO2005000353 (Kotobuki Pharmaceutical Co. Ltd.), or WO2005044256 or WO2005062824

(Merck & Co.) or WO2005061451 and WO2005061452 (AstraZeneca AB) and WO2006017257 (Phenomix) or WO2005033100 (Lipideon Biotechnology AG) or as described in WO2002050060, WO2002050068, WO2004000803, WO2004000804,

WO2004000805, WO2004087655, WO2004097655, WO2005047248,

WO2006086562, WO2006102674, WO20061 16499, WO2006121861,

WO2006122186, WO2006122216, WO2006127893, WO2006137794,

WO2006137796, WO2006137782, WO2006137793, WO2006137797,

WO2006137795, WO2006137792, WO2006138163, WO2007059871,

US2007232688, WO2007126358, WO2008033431, WO2008033465,

WO2008052658, WO2008057336, WO2008085300, WO2008104875,

US2008280836, WO2008108486 describes administered.

In one embodiment of the invention, the compound of formula I is

Combination with a NPC1 L1 antagonists, such as those described in

WO2008033464, are described in WO2008033465, is administered.

In one embodiment of the invention, the compound of formula I is

Combination with Vytorin ™, a fixed combination of ezetimibe and simvastatin is administered. In one embodiment of the invention, the compound of formula I is

Combination with a fixed combination of ezetimibe with atorvastatin administered.

In one embodiment of the invention, the compound of formula I is

administered combination with a fixed combination of ezetimibe with fenofibrate.

In one embodiment of the invention, the further active ingredient is a

Diphenylazetidinone, such as described in US 6,992,067 or US 7,205,290.

In a further embodiment of the invention, the further active ingredient is a

Diphenylazetidinone derivative, as described for example in US 6,992,067 or US 7,205,290, combined with a statin such as simvastatin, fluvastatin, pravastatin, lovastatin, cerivastatin, atorvastatin, pitavastatin or rosuvastatin. In one embodiment of the invention, the compound of formula I is

Administered combination with a fixed combination of Lapaquistat, a Squalensynthase- inhibitor atorvastatin.

In a further embodiment of the invention the compound of formula I in combination with a conjugate consisting of the HMGCoA reductase inhibitor atorvastatin with the renin inhibitor aliskiren (WO2009090158) is administered. In one embodiment of the invention, the compound of formula I is

Combination with a CETP inhibitor, such as torcetrapib, JTT-705 or anacetrapib (Dalcetrapib) or those as are described in WO2006002342, WO2006010422

WO2006012093, WO2006073973, WO2006072362, WO2007088996,

WO2007088999, US2007185058, US20071851 13, US2007185154, US2007185182, WO2006097169, WO2007041494, WO2007090752, WO2007107243,

WO2007120621, US2007265252, US2007265304, WO2007128568, WO2007132906, WO2008006257, WO2008009435, WO2008018529, WO2008058961,

WO2008058967, WO2008059513, WO2008070496, WO20081 15442,

WO20081 1 1604, WO2008129951, WO2008141077, US20091 18287,

WO2009062371, are described in WO2009071509, is administered.

In one embodiment of the invention, the compound of formula I is

Combination with bile acid (inhibitors of intestinal

(Bile acid transporter (IBAT)) See, eg, US 6,245,744, US 6,221, 897 or

WOOO / 61568), such as HMR 1741 or those described in DE 10 2005 033099.1 and DE 10 2005 033100.9, DE 10 2006 053 635, DE 10 2006 053 637, WO2007009655-56, WO2008058628, WO2008058629, WO2008058630, WO2008058631 describes administered. In one embodiment, the compound of formula I in combination with

GPBAR1 agonists of the (G-protein-coupled bile-acid-receptor-1; TGR5), such as INT or 777 such as, for example, in US20060199795, WO20071 10237, WO2007127505, WO2008009407, WO2008067219, WO2008067222, FR2908310, WO2008091540, WO2008097976 , US2009054304, WO2009026241, WO2009146772,

WO2010014739, are described in WO2010014836, is administered. In one embodiment, the compound of formula I in combination with modulators of histone deacetylase, as for example ursodeoxycholic acid, as in

described WO200901 1420 administered.

In one embodiment, the compound of formula I in combination with inhibitors / modulators of the TRPM5 channel (TRP-Cation Channel M5), as they are for example described in WO2009038722 WO2008097504 administered.

In one embodiment, the compound of formula I in combination with inhibitors / modulators of TRPA1 channel (TRP-Cation-channel-A1), as they are described for example in US2009176883, WO2009089083, WO2009144548, administered.

In one embodiment, the compound of formula I in combination with inhibitors / modulators of the TRPV3 channel (TRP-Cation Channel V3), as they are described for example in WO2009084034, WO2009130560, administered.

In one embodiment of the invention, the compound of formula I is

Combination with a polymeric bile acid adsorber, such as cholestyramine, colesevelam hydrochloride, administered. In one embodiment of the invention, the compound of formula I is

Combination with colesevelam hydrochloride and metformin or a

Sulfonylurea or insulin administered.

In one embodiment of the invention, the compound of formula I is

administered combination with tocotrienol and insulin or an insulin derivative. In one embodiment of the invention, the compound of formula I is

Combination with a phytosterol-containing chewing gum (Reductol ™) administered.

In one embodiment of the invention, the compound of formula I is

Combination with an inhibitor of microsomal triglyceride transfer protein (MTTP inhibitor), such as implitapide, BMS-201038, R-103757, AS-1552133, SLX 4090, AEGR-733, JTT-130 or those described in WO2005085226, WO2005121091, WO2006010423, WO20061 13910, WO2007143164, WO2008049806,

WO2008049808, WO2008090198, WO2008100423, administered WO2009014674 described.

In a further embodiment of the invention, the compound of formula I in combination with a Kombinbation a Cholesterolabsorptionsinhibitors such as ezetimibe, and an inhibitor of triglyceride transfer protein (MTP) inhibitor, such as implitapide, as described in WO2008030382 or WO2008079398 administered.

In one embodiment of the invention, the compound of formula I is

Combination with a antihypertriglyceridämischen agent such as administered such as are described in WO2008032980.

In another embodiment of the invention the compound of formula I in combination with an antagonist of somatostatin 5 receptor (SST5

Receptor), such as those as described in WO2006094682 administered.

In one embodiment of the invention, the compound of formula I is

Combination with an ACAT inhibitor, such as avasimibe or SMP-797 KY-382 or those as are described in WO2008087029, WO2008087030, WO2008095189

WO2009030746, WO2009030747, WO2009030750, WO2009030752,

WO2009070130, WO2009081957, WO2009081957 described administered. In a further embodiment of the invention the compound of formula I in combination with an inhibitor of liver carnitine palmitoyltransferase-1 (L-CPT1), as described for example in WO2007063012, WO2007096251 (ST-3473), WO2008015081, US2008103182, WO2008074692, WO2008145596 , WO2009019199,

WO2009156479, are described in WO2010008473, is administered.

In another embodiment of the invention the compound of formula I in combination with an inhibitor of carnitine palmitoyltransferase-O-Il is (CPT2), as described for example in US2009270500, US2009270505, WO2009132978, WO2009132979

are described administered.

In a further embodiment of the invention the compound of formula I in combination with a modulator of serine palmitoyltransferase (SPT) is as given, for example, in WO2008031032, are described in WO2008046071, WO2008083280, WO2008084300.

In one embodiment of the invention, the compound of formula I is

Combination with a squalene synthetase inhibitor, such as BMS-188494, TAK-475 (Lapaquistat acetate) or as administered WO2009136396 described in WO2005077907, JP2007022943, WO2008003424, WO2008132846, WO2008133288.

In one embodiment of the invention, the compound of formula I is

Combination with ISIS-301012 (Mipomersen), an antisense oligonucleotide which is able to regulate the apolipoprotein B gene.

In one embodiment of the invention, the compound of formula I is

Combination with apolipoprotein (ApoB) SNALP, a therapeutic product containing (directed against the ApoB gene) an siRNA administered. In one embodiment of the invention, the compound of formula I is

Combination with a stimulator of the ApoA-1 gene, as described for example in WO2008092231, is administered. In one embodiment of the invention, the compound of formula I is

Combination with a modulator of the synthesis of apolipoprotein 0- III as .B. ISIS APOCIMRx administered.

In one embodiment of the invention, the compound of formula I is

Combination with an LDL receptor inducer (see US 6,342,512), such as

HMR1 171, HMR1586 or those as described in WO2005097738, WO2008020607 describes administered.

In another embodiment of the invention, the compound of formula I in combination with an HDL-cholesterol increasing agent is, for example such as are described in WO2008040651, WO2008099278, WO2009071099, WO2009086096

US2009247550 described administered.

In one embodiment of the invention, the compound of formula I is

Combination as described for example in WO2006072393, WO2008062830, WO2009100326 with an ABCA1 expression enhancer, administered.

In one embodiment of the invention, the compound of formula I is

Combination with a lipoprotein lipase modulator, such as Ibrolipim administered (NO-1886). In one embodiment of the invention, the compound of formula I is

Combination with a lipoprotein (a) antagonist, such as gemcabene (CI-1027) administered.

In one embodiment of the invention, the compound of formula I is

Combination with a lipase inhibitor, such as orlistat or cetilistat (ATL-962), administered. In one embodiment of the invention, the compound of formula I is

Combination with an adenosine A1 receptor agonist (adenosine A1 R), such as CVT 3619 or such as for example, in EP1258247, EP1375508, WO2008028590, WO2008077050, WO2009050199, WO2009080197, WO2009100827,

WO20091 12155 are described administered.

In one embodiment of the invention, the compound of formula I is

Combination with an adenosine A2B receptor agonist (adenosine A2B R), such as ATL-801 administered.

In another embodiment of the invention the compound of formula I in combination with a modulator of adenosine A2A and / or adenosine A3

Receptors, such as, in WO20071 1 1954, WO2007121918, WO2007121921

described WO2007121923, WO2008070661, WO2009010871, administered.

In a further embodiment of the invention the compound of formula I in combination with a ligand of the adenosine A1 / A2B receptors, such as in

WO2008064788, WO2008064789, WO2009080198, WO2009100827,

WO2009143992 describes administered.

In one embodiment of the invention, the compound of formula I is

Combination with an adenosine A2B receptor antagonist (adenosine A2B R), such as, in US2007270433, WO2008027585, WO2008080461, WO2009037463

WO2009037467, WO2009037468, WO20091 18759 describes administered.

In one embodiment, the compound of formula I in combination with inhibitors of acetyl-CoA carboxylase (ACC1 and / or ACC2), such as is. As such as in WO199946262, WO200372197, WO2003072197, WO2005044814,

WO2005108370, JP2006131559, WO200701 1809 WO200701 181 1, WO2007013691, WO2007095601 -603, WO20071 19833, WO2008065508, WO2008069500,

WO2008070609, WO2008072850, WO2008079610, WO2008088688,

WO2008088689, WO2008088692, US2008171761, WO2008090944, JP2008179621, US2008200461, WO2008102749, WO2008103382, WO2008121592, WO2009082346, US2009253725, JP2009196966, WO2009144554, WO2009144555, WO2010003624, WO2010002010 describes administered. In another embodiment, the compound of formula I in combination with modulators of microsomal acyl-CoA: glycerol-3-phosphate acyltransferase 3 (GPAT3 described in WO2007100789) or with modulators of microsomal acyl-CoA: glycerol-3-phosphate acyltransferase 4 (GPAT4 described in

WO2007100833) or with modulators of mitochondrial glycerol-3-phosphate-O- acyltransferase described in WO2010005922, is administered.

In another embodiment, the compound of formula I in combination with modulators of xanthine oxidoreductase (XOR) is administered. In another embodiment, the compound of formula I in combination with inhibitors of soluble epoxide hydrolase (sEH), such as, for example, in WO2008051873, WO2008051875, WO2008073623, WO2008094869, WO20081 12022

WO200901 1872, WO2009049154, WO2009049157, WO2009049165,

WO2009073772, WO2009097476, WO20091 1 1207, WO2009129508,

WO2009151800 describes administered.

In another embodiment, the compound of formula I in combination with CART modulators (see is "Cocaine-amphetamine-regulated transcript influences energy metabolism, anxiety and gastric emptying in mice" Asakawa, A. et al. Hormone and Metabolic Research (2001 ), 33 (9), 554-558);

NPY antagonists such as naphthalene-1 -sulfonsäure- {4 - [(4-amino-quinazolin-2- ylamino) methyl] -cyclohexylmethyl} -amide hydrochloride (CGP 71683A) or Velneperit or those as are described in WO20091 10510 ; NPY-5 receptor antagonists / -rezeptornnodulatoren such as L-152,804 or the compound "NPY-5-BY" from Banyu or as z. B. in WO2006001318, WO2007103295, WO2007125952, WO2008026563, WO2008026564, WO2008052769,

WO2008092887, WO2008092888, WO2008092891, WO2008129007,

WO2008134228, WO2009054434, WO2009095377, WO2009131096 are described;

NPY-4 receptor antagonists as such. As are described in WO2007038942; NPY-2 receptor antagonists / modulators as such. As in WO2007038943,

WO2009006185, US2009099199, US2009099243, US2009099244, WO2009079593, WO2009079597 are described;

Peptide YY 3-36 (PYY3-36) or analogous compounds, such as. For example, CJC-1682 (PYY3-36 conjugated with human serum albumin via Cys34), CJC-or 1643 (derivative of PYY3-36 which conjugates in vivo to serum albumin) or those described in WO2005080424, WO2006095166, WO2008003947, WO2009080608 are described; NPY-2 receptor agonists as described, for example, in WO2009080608; Derivatives of the peptide obestatin as are described in WO2006096847;

CB1 R (cannabinoid receptor 1) antagonists / inverse agonists, such as

Rimonabant, Surinabant (SR147778), SLV-319 (Ibipinabant), AVE-1625, Taranabant (MK-0364) or salts thereof, Otenabant (CP-945.598), Rosonabant, V-24343 or those compounds as described in z. For example, EP 0656354, WO 00/15609, WO2001 / 64632- 64634, WO 02/076949, WO2005080345, WO2005080328, WO2005080343,

WO2005075450, WO2005080357, WO200170700, WO2003026647-48,

WO200302776, WO2003040107, WO2003007887, WO2003027069, US6,509,367, WO200132663, WO2003086288, WO2003087037, WO2004048317, WO2004058145, WO2003084930, WO2003084943, WO2004058744, WO2004013120, WO2004029204, WO2004035566, WO2004058249, WO2004058255, WO2004058727, WO2004069838, US20040214837, US20040214855,

US20040214856, WO2004096209, WO2004096763, WO2004096794,

WO2005000809, WO2004099157, US20040266845, WO20041 10453,

WO2004108728, WO2004000817, WO2005000820, US20050009870,

WO200500974, WO20041 1 1033-34, 1038-39 WO20041, WO2005016286,

WO20050071 1 1, WO2005007628, US20050054679, WO2005027837,

WO2005028456, WO2005063761 -62, WO2005061509, WO2005077897,

WO2006018662, WO2006047516, WO2006060461, WO2006067428,

WO2006067443, WO2006087480, WO2006087476, WO2006100208,

WO2006106054, WO20061 1 1849 WO20061 13704, WO2007009705,

WO2007017124, WO2007017126, WO2007018459, WO2007018460,

WO2007016460, WO2007020502, WO2007026215, WO2007028849,

WO2007031720, WO2007031721, WO2007036945, WO2007038045,

WO2007039740, US20070015810, WO2007046548, WO2007047737,

WO2007057687, WO2007062193, WO2007064272, WO2007079681,

WO2007084319, WO2007084450, WO2007086080, ΕΡ1816125, US2007213302, WO2007095513, WO2007096764, US2007254863, WO20071 19001,

WO2007120454, WO2007121687, WO2007123949, US2007259934,

WO2007131219, WO2007133820, WO2007136571, WO2007136607,

WO2007136571, US7297710, WO2007138050, WO2007139464, WO2007140385, WO2007140439, WO2007146761, WO2007148061, WO2007148062,

US2007293509, WO2008004698, WO2008017381, US2008021031, WO2008024284, WO2008031734, WO2008032164, WO2008034032, WO2008035356,

WO2008036021, WO2008036022, WO2008039023, WO2998043544,

WO20080441 1 1, WO2008048648, ΕΡ1921072-Α1, WO2008053341, WO2008056377, WO2008059207, WO2008059335, WO2008062424, WO2008068423,

WO2008068424, WO2008070305, WO2008070306, WO2008074816,

WO2008074982, WO2008075012, WO2008075013, WO2008075019,

WO20080751 18, WO2008076754, WO2008081009, WO2008084057, ΕΡ1944295, US2008090809, US2008090810, WO2008092816, WO2008094473, WO2008094476, WO2008099076, WO2008099139, WO2008101995, US2008207704, WO2008107179, WO2008109027, WO20081 12674, WO20081 15705, WO20081 18414, WO20081 19999, WO200812000, WO2008121257, WO2008127585 , WO2008129157, WO2008130616, WO2008134300, US2008262066, US2008287505, WO2009005645, WO2009005646, WO2009005671, WO2009023292,

WO2009023653, WO2009024819, WO2009033125, EP2042175, WO2009053548- WO2009053553, WO2009054923, WO2009054929, WO2009059264,

WO2009073138, WO2009074782, WO2009075691, WO2009078498,

WO2009087285, WO2009074782, WO2009097590, WO2009097995,

WO2009097996, WO2009097998, WO2009097999, WO2009098000,

WO2009106708, US2009239909, WO20091 18473, US2009264436, US2009264476, WO2009130234, WO2009131814, WO2009131815, US2009286758,

WO2009141532, WO2009141533, WO2009153569, WO2010003760,

WO2010012437, WO2010019762 are described; Cannabinoid receptor 1 / cannabinoid receptor 2 (CB1 / CB2) modulating

Compounds such as delta-9 tetrahydrocannabivarin or such as described for example in WO2007001939, WO2007044215, WO2007047737, WO2007095513,

WO2007096764, WO20071 12399, WO20071 12402, WO2008122618,

WO2009007697, WO2009012227, WO2009087564, WO2009093018,

WO2009095752, WO2009120660, WO2010012964 are described;

Cannabinoid receptor 2 (CB2) modulating compounds such as such as described for example, in WO2008063625, WO2008157500, WO2009004171, WO2009032754

WO2009055357, WO2009061652, WO2009063495, WO2009067613,

WO20091 14566 are described;

Modulators of FAAH (fatty acid amide hydrolase) as described for example in WO2007140005, WO2008019357, WO2008021625, WO2008023720, WO2008030532,

WO2008129129, WO2008145839, WO2008145843, WO2008147553,

WO2008153752, WO200901 1904, WO2009048101, WO2009084970,

WO2009105220, WO2009109504, WO2009109743, WO20091 17444, WO2009127944, WO2009138416, WO2009151991, WO2009152025, WO2009154785, WO2010005572, are described in WO2010017079;

Inhibitors of fatty acid (fatty acid synthase; FAS) such as, for example, in

WO2008057585, WO2008059214, WO2008075064, WO2008075070,

WO2008075077, are described in WO2009079860;

Inhibitors of the LCE (long chain fatty acid elongase) / Long-Chain Fatty Acid-CoA ligase, as described for example, in WO2008120653, WO2009038021, WO2009044788

WO2009081789, are described in WO2009099086;

Vanilloid 1 receptor modulators (modulators of TRPV1), as described for example in

WO2007091948, WO2007129188, WO2007133637, WO2008007780,

WO2008010061, WO200800721 ​​1, WO2008010061, WO2008015335,

WO2008018827, WO2008024433, WO2008024438, WO2008032204,

WO2008050199, WO2008059339, WO2008059370, WO2008066664,

WO2008075150, WO2008090382, WO2008090434, WO2008093024,

WO2008107543, WO2008107544, WO20081 10863, WO2008125295,

WO2008125296, WO2008125337, WO2008125342, WO2008132600,

WO2008133973, WO2009010529, WO2009010824, WO2009016241,

WO2009023539, WO2009038812, WO2009050348, WO2009055629,

WO2009055749, WO2009064449, WO2009081222, WO2009089057,

WO2009109710WO20091 12677, WO20091 12678, WO20091 12679, WO2009121036, WO2009124551, WO2009136625, WO2010002209 are described;

Modulators, ligands, antagonists or inverse agonists of opioid receptors, such as GSK-982 or those as described for example, in WO2007047397, WO2008021849, WO2008021851, WO2008032156, WO2008059335, WO2008125348

WO2008125349, WO2008142454, WO2009030962, WO2009103552,

WO20091 15257 are described; Modulators of "orphan opioid (ORL-1) receptor" as described for example in US2008249122, WO2008089201;

Agonists of prostaglandin receptor, such as bimatoprost, or such

Compounds as disclosed in WO20071 1 1806;

MC4 receptor agonists (melanocortin-4 receptor agonists, MC4R agonists such as 1 -amino-1, 2,3,4-tetrahydro-naphthalene-2-carboxylic acid [2- (3a-benzyl-2-methyl-3-oxo- 2,3,3a, 4,6,7-hexahydro-pyrazolo [4,3-c] pyridin-5-yl) -1 - (4-chloro-phenyl) -2-oxo-ethyl] -amide; (WO 01/91752)) or LB53280, LB53279, LB53278 or THIQ, MB243, RY764, CHIR-785, PT-141 or those MK-0493 as described in WO2005060985,

WO2005009950, WO2004087159, WO2004078717, WO2004078716,

WO2004024720, US20050124652, WO2005051391, WO20041 12793,

WOUS20050222014, US20050176728, US20050164914, US20050124636,

US20050130988, US20040167201, WO2004005324, WO2004037797,

WO2004089307, WO2005042516, WO2005040109, WO2005030797,

US20040224901, WO200501921, WO200509184, WO2005000339, EP1460069, WO2005047253, WO2005047251, WO20051 18573, EP1538159, WO2004072076, WO2004072077, WO2006021655-57, WO2007009894, WO2007015162,

WO2007041061, WO2007041052, JP2007131570, EP-1842846, WO2007096186, WO2007096763, WO2007141343, WO2008007930, WO2008017852,

WO2008039418, WO2008087186, WO2008087187, WO2008087189,

WO2008087186-WO2008087190, WO2008090357, WO2008142319,

WO2009015867, WO200906141 1, US2009076029, US2009131465, WO2009071 101, US2009305960, WO2009144432, WO2009151383, WO2010015972 are described;

MC4 receptor modulators (melanocortin-4 receptor modulators) as described for example in WO2009010299, WO2009074157 are described;

Orexin receptor 1 antagonists (R OX1 antagonists), orexin receptor 2

Antagonists (OX2R antagonists) or mixed OX1 R / OX2R antagonists (for example 1 - (2-methyl-benzoxazol-6-yl) -3- [1, 5] naphthyridin-4-yl-urea hydrochloride (SB-334867- A) or those such as, for. example, in WO200196302, WO200185693, WO2004085403, WO2005075458, WO2006067224, WO2007085718, WO2007088276,

WO20071 16374, WO2007122591, WO2007126934, WO2007126935,

WO2008008517, WO2008008518, WO2008008551, WO2008020405,

WO2008026149, WO2008038251, US2008132490, WO2008065626,

WO2008078291, WO200808761 1, WO2008081399, WO2008108991,

WO2008107335, US2008249125, WO2008147518, WO2008150364,

WO2009003993, WO2009003997, WO200901 1775, WO2009016087,

WO2009020642, WO2009058238, US2009186920, US2009203736, WO2009092642, WO2009100994, WO2009104155, WO2009124956, WO2009133522,

WO2009156951, are described in WO2010017260);

Histamine H3 receptor antagonists / inverse agonists (for example 3-cyclohexyl-1 -. (4,4-dimethyl-1, 4,6,7-tetrahydro-imidazo [4,5-c] pyridin-5-yl) - propan-1 -one oxalic acid salt (WO 00/63208) or those described in WO200064884, WO2005082893, WO2005123716, US2005171 181 (for example, PF-00389027), WO2006107661, WO2007003804

WO2007016496, WO2007020213, WO2007049798, WO2007055418,

WO2007057329, WO2007062999, WO2007065820, WO2007068620,

WO2007068641, WO2007075629, WO2007080140, WO2007082840,

WO2007088450, WO2007088462, WO2007094962, WO2007099423,

WO2007100990, WO2007105053, WO2007106349, WO20071 10364,

WO20071 15938, WO2007131907, WO2007133561, US2007270440,

WO20071351 1 1, WO2007137955, US2007281923, WO2007137968,

WO2007138431, WO2007146122, WO2008005338, WO2008012010,

WO2008015125, WO2008045371, EP1757594, WO2008068173, WO2008068174, US20080171753, WO2008072703, WO2008072724, US2008188484, US2008188486, US2008188487, WO2008109333, WO2008109336, WO2008126886,

WO2008154126, WO2008151957, US2008318952, WO2009003003,

WO2009013195, WO2009036132, WO2009039431, WO2009045313,

WO2009058300, WO2009063953, WO2009067401, WO2009067405,

WO2009067406, US2009163464, WO2009100120, WO2009105206, WO2009121812, WO2009126782, WO201001 1653, WO201001 1657 are described);

Histamine H1 / histamine H3 modulators such. B. betahistine or its

dihydrochloride;

Modulators of the histamine H3 transporter or the histamine H3 / serotonin

Transportation as they are described for example in WO2008002816, WO2008002817, WO2008002818, WO2008002820;

Modulators of the vesicular monoamine transporter 2 (vesicular monoamine transporter 2 (VMAT2)) as described for example in WO2009126305;

Histamine H4 modulators such as those described for example in WO20071 17399, US2009156613;

CRF antagonists (for example [2-methyl-9- (2,4,6-trimethyl-phenyl) -9H-1, 3,9-triaza-fluoren-4-yl] -dipropyl-amine (WO 00/66585) or those CRF1 antagonists as described in

WO20071051 13, WO2007133756, WO2008036541, WO2008036579,

WO2008083070 are described WO2010015628, WO2010015655);

CRF BP antagonists (for example urocortin);

U-rocortin Agon ists;

Modulators of the beta-3 Adrenoceptors such as 1 - (4-chloro-3-methanesulfonylmethyl- phenyl) -2- [2- (2,3-dimethyl-1 H-indol-6-yloxy) ethylamino] ethanol hydrochloride ( WO 01/83451) or Solabegron (GW-427353) or N-5984 (KRP-204) or those described in JP20061 1 1553 WO2002038543, WO2002038544, WO2007048840-843

WO2008015558, EP1947103, WO2008132162 are described;

MSH (melanocyte-stimulating hormone) agonists; MCH (melanin-concentrating hormone) receptor antagonists (such as, for example, NBI-845, A-761, A-665798, A-798, ATC-0175, T-226296, T-71 (AMG-071, AMG-076 ), GW-856464, NGD-4715, ATC-0453, ATC-0759, GW-803430 or those compounds as are described in WO2005085200, WO2005019240, WO200401 1438, WO2004012648, WO2003015769, WO2004072025, WO2005070898, WO2005070925

WO2004039780, WO2004092181, WO2003033476, WO2002006245,

WO2002089729, WO2002002744, WO2003004027, FR2868780, WO2006010446, WO2006038680, WO2006044293, WO2006044174, JP2006176443, WO2006018280, WO2006018279, WO20061 18320, WO2006130075, WO2007018248,

WO2007012661, WO2007029847, WO2007024004, WO2007039462,

WO2007042660, WO2007042668, WO2007042669, US2007093508, US2007093509, WO2007048802, JP2007091649, WO2007092416; WO2007093363-366,

WO20071 14902, WO20071 14916, WO2007141200, WO2007142217,

US2007299062, WO2007146758, WO2007146759, WO2008001 160,

WO200801681 1, WO2008020799, WO2008022979, WO2008038692,

WO2008041090, WO2008044632, WO2008047544, WO2008061 109,

WO2008065021, WO2008068265, WO2008071646, WO2008076562, JP2008088120, WO2008086404, WO2008086409, US20082691 10, WO2008140239,

WO2009021740, US200901 1994, US2009082359, WO2009041567, WO2009076387, WO2009089482, WO2009103478, WO20091 19726, WO2009120655,

WO2009123194, WO2009137270, WO2009146365, WO2009154132 are described); CCK-A (CCK-1) agonists / modulators (for example {2- [4- (4-chloro-2,5-dimethoxy-phenyl) -5- (2-cyclohexyl-ethyl) -thiazol-2-ylcarbamoyl] -5,7-dinnethyl-indol-1 -yl} - acetic acid trifluoroacetic acid salt (WO 99/15525) or SR-146131 (WO 0244150) or SSR-125180) or such as, in WO20051 16034, WO2007120655

WO2007120688, WO2007120718, are described in WO2008091631;

Serotonin reuptake inhibitors (for example dexfenfluramine) or those as are described in WO2007148341, WO2008034142, WO2008081477, WO2008120761, WO2008141081, WO2008141082, WO2008145135, WO2008150848

WO2009043834, are described in WO2009077858; mixed serotonin / dopamine reuptake inhibitors (for example, bupropion) or those as are described in WO2008063673 or fixed combinations of bupropion with naltrexone or bupropion with zonisamide; mixed reuptake inhibitors such as DOV 21947 or those as are described in WO2009016214, WO2009016215, WO2009077584, WO2009098208

WO2009098209, WO2009106769, WO2009109517, WO2009109518,

are WO2009109519, WO2009109608, WO2009145357, WO2009149258 described; mixed serotonin and noradrenergic compounds (for example WO 00/71549);

5-HT receptor agonists, for example, 1 - (3-ethyl-benzofuran-7-yl) piperazine oxalic acid salt (WO 01/091 1 1); mixed dopamine / norepinephrine / acetylcholine reuptake inhibitors (such as tesofensine) or those as are described for example in WO20060851 18, WO2008150480;

Dopamine antagonists such as, for example, in WO2008079838, WO2008079839

WO2008079847, are described in WO2008079848;

Norepinephrine reuptake inhibitors, such as they are described for example in US2008076724, WO2009062318;

5-HT1 A receptor modulators as they are described for example in WO2009137732 WO2009006227, WO2009137679;

5-HT2A receptor antagonists as are described for example in WO2007138343; 5-HT2C receptor agonists (such as lorcaserin hydrochloride (APD-356) or BAT 933 or those described in WO200077010, WO200077001 -02, WO2005019180, WO2003064423, WO200242304, WO2005035533, WO2005082859, WO2006004937, US2006025601, WO2006028961, WO2006077025, WO200610351 1 ,

WO2007028132, WO2007084622, US2007249709; WO2007132841,

WO2007140213, WO2008007661, WO2008007664, WO2008009125,

WO2008010073, WO2008108445, WO2009063991, WO2009063992,

WO2009063993 are described WO2009079765);

5-HT6 receptor modulators, such as E-6837, BVT-74316, PF-3246799 or PRX- 07034 or such as, for example, in WO2005058858, WO2007054257, WO2007107373, WO2007108569, WO2007108742-744, WO2008003703, WO2008027073

WO2008034815, WO2008054288, EP1947085, WO2008084491, WO2008084492, WO2008092665, WO2008092666, WO2008101247, WO20081 10598,

WO20081 16831, 16833 WO20081, WO20081 17169, WO2008136017,

WO2008147812, EP2036888, WO2009013010, WO2009034581, WO2009053997, WO2009056632, WO20090731 18, WO20091 15515, WO2009135925,

WO2009135927, WO2010000456, WO2010012806, EP2145887 are described;

Agonists of the estrogen receptor gamma (ERR agonist), as described for example in

WO2007131005, are described in WO2008052709;

Agonists of the estrogen receptor alpha (ERR / ERR1 agonist) as they are described for example in WO2008109727;

Agonists of the estrogen receptor beta (ERRß agonists), for example, in

WO2009055734, WO2009100335, WO2009127686 are described; Sigma-1 receptor antagonists as are for example described in WO2009071657 WO2007098953, WO2007098961, WO2008015266, WO2008055932, WO2008055933; 3 muscarinic receptor (M3R) antagonists, such as, for example, in WO20071 10782

are described in WO2008041 184; Bombesin receptor agonists (BRS-3 agonists) as they are described for example in WO2008051404, WO2008051405, WO2008051406, WO200807331 1;

Galanin receptor antagonists; Growth hormone (for example human growth hormone or AOD-9604);

Growth hormone-releasing compounds (6-benzyloxy-1 - (2-diisopropylamino-ethylcarbamoyl) -3,4-dihydro-1 H-isoquinoline-2-carbonsäuretertiärbutylester (WO

01/85695));

Growth hormone secretagogue receptor antagonists (ghrelin antagonists) such as. B. A-778193 or those as are described in WO2005030734, WO2007127457

WO2008008286, are described in WO2009056707; Growth hormone secretagogue receptor modulators (ghrelin modulators) such as JMV-2959, JMV-3002, JMV-2810, JMV-2951 or those as described in WO2006012577 (eg YIL-781 or YIL-870), WO2007079239, WO2008092681, WO2008145749 , WO2008148853, WO2008148854, WO2008148856, WO2009047558,

WO2009071283, are described WO20091 15503;

TRH agonists (see, for example EP 0462884); uncoupling protein 2 or 3 modulators (such as in WO2009128583

described); chemical decoupler (eg, WO2008059023, WO2008059024, WO2008059025, WO2008059026); Leptin receptor agonists (see, eg, Lee, Daniel W .; Leinung, Matthew C; Rozhavskaya Arena, Marina;.. Grasso, Patricia leptin agonists as a potential approach to the treatment of obesity Drugs of the Future (2001), 26 (9) 873-881);

Leptin receptor modulators as described for example in WO2009019427, WO2009071658,

WO2009071668, WO2009071677, WO2009071678, WO200914721 1,

WO2009147216, WO2009147219, are described in WO2009147221; DA agonists (bromocriptine, bromocriptine mesylate, doprexin) or those as are described in US2009143390;

Lipase / amylase inhibitors (for example WO 00/40569, WO2008107184, WO2009049428, WO2009125819);

Inhibitors of diacylglycerol O-acyltransferases (DGATs) such. B. BAY-74-41 13 or such. As in US2004 / 0224997, WO2004094618, WO200058491, WO2005044250, WO2005072740, JP2005206492, WO2005013907, WO2006004200, WO200601 9020, WO2006064189, WO2006082952, WO2006120125, WO20061 13919,

WO2006134317, WO2007016538, WO2007060140, JP2007131584, WO2007071966, WO2007126957, WO2007137103, WO2007137107, WO2007138304,

WO200713831 1, WO2007141502, WO2007141517, WO2007141538,

WO2007141545, WO2007144571, WO200801 1130, WO200801 1 131,

WO2008039007, WO2008048991, WO2008067257, WO2008099221,

WO2008129319, WO2008141976, WO2008148840, WO2008148849,

WO2008148851, WO2008148868, WO200901 1285, WO2009016462,

WO2009024821, US2009076275, WO2009040410, WO2009071483,

WO2009081 195, WO20091 19534, WO2009126624, WO2009126861,

described WO2010007046, WO2010017040;

Inhibitors of Monoacylglycerolacyltransferase (2-acylglycerol O-acyltransferase; MG AT) as described for example in WO2008038768; Inhibitors of fatty acid synthase (FAS) as described, for example, C75 or those as described in WO2004005277, WO20080061 13; Inhibitors of stearoyl-CoA desaturase delta9 (SCD1) as described for example in

WO2007009236, WO2007044085, WO2007046867, WO2007046868,

WO20070501 124, WO2007056846, WO2007071023, WO2007130075,

WO2007134457, WO2007136746, WO2007143597, WO2007143823,

WO2007143824, WO2008003753, WO2008017161, WO2008024390,

WO2008029266, WO2008036715, WO2008043087, WO2008044767,

WO2008046226, WO2008056687, WO2008062276, WO2008064474,

WO2008074824, WO2008074832, WO2008074833, WO2008074834,

WO2008074835, WO2008089580, WO2008096746, WO2008104524,

WO20081 16898, US2008249100, WO2008120744, WO2008120759,

WO2008123469, WO2008127349, WO2008128335, WO2008135141,

WO2008139845, WO2008141455, US20080255130, US2008255161,

WO2008141455, WO2009010560, WO2009016216, WO2009012573,

WO2009024287, JP2009019013, WO2009037542, WO2009056556, WO2009060053, WO2009060054, WO2009070533, WO2009073973, WO2009103739,

WO20091 17659, WO20091 17676, US2009253693, US2009253738, WO2009124259, WO2009126123, WO2009126527, WO2009129625, WO2009137201,

WO2009150196, WO2009156484, WO2010006962, WO2010007482 are described; Inhibitors of Fatty Acid Desaturase-1 (deltaö desaturase), for example as described in

WO2008089310 are described;

Inhibitors of monoglyceride lipase (MGL) as are described in WO2008145842; hypoglycemic / hypertriglyceridämische indoline as in

WO2008039087, WO2009051 1 19 are described; Inhibitors of "Adipocyte fatty acid-binding protein aP2", such as BMS-309403 or those as are described in WO2009028248; activators of Adiponectinsekretion, as described for example in WO2006082978, WO2008105533, WO2008136173;

Promoters of Adiponectinproduktion, as described for example in WO2007125946, WO2008038712;

Adiponectine modified as described for example in WO2008121009;

Oxyntomodulin and analogs thereof (such as TKS-1225); Oleoyl-estrone or agonist or partial agonist the thyroid hormone receptor (thyroid hormone receptor agonists) such. B: KB-21 15 (Eprotirome), QRX-431 (Sobetirome) or DITPA or those as described in WO20058279, WO200172692, WO200194293, WO2003084915, WO2004018421, WO2005092316, WO2007003419,

WO2007009913, WO2007039125, WO20071 10225, WO20071 10226

WO2007128492, WO2007132475, WO2007134864, WO2008001959,

WO2008106213, JP2009155261 described or agonists of the thyroid hormone receptor beta (TR-beta), such as. B. described MB-1 or MB-07344 0781, or those described in WO2008062469, is administered.

In one embodiment of the invention, the compound of formula I is

Combination with a combination of Eprotirome administered with ezetimibe.

In one embodiment of the invention, the compound of formula I is

Combination with an inhibitor of the site-1 protease (S1 P), such as PF-429242, administered. In a further embodiment of the invention, the compound of formula I in combination with a modulator of the "trace amines-Associated-Receptor-1", (TAAR1) as they are described for example in US2008146523, WO2008092785 administered. In one embodiment of the invention, the compound of formula I is

Combination with an inhibitor of the growth factor receptor-bound protein 2

(GRB2), administered as described for example in WO2008067270.

In a further embodiment of the invention, the compound of formula I in combination with an RNAi (siRNA) therapeutic agent which is opposite PCSK9

(Proprotein convertase subtilisin / kexin type 9) is directed administered.

In one embodiment, the compound of formula I in combination with Omacor® or Lovaza ™ (omega-3 fatty acid esters; highly concentrated ethyl esters of eicosapentaenoic acid and docosahexaenoic acid) is administered.

In one embodiment, the compound of formula I is administered in combination with lycopene. In one embodiment of the invention, the compound of formula I is

Combination with an antioxidant such as OPC-141 17, AGI-1067 (Succinobucol), probucol, tocopherol, ascorbic acid, .beta.-carotene or selenium or those as described in WO2009135918, is administered. In one embodiment of the invention, the compound of formula I is

Combination with a vitamin such. Example, vitamin B6 or vitamin B12 administered.

In one embodiment, the compound of formula I in combination with more than one of the aforementioned compounds, for example in combination with a sulfonylurea and metformin, a sulfonylurea and acarbose, repaglinide and metformin (PrandiMet (TM)), insulin and a sulfonylurea, insulin and metformin, insulin and troglitazone, insulin and lovastatin, etc.. In a further embodiment, the compound of formula I in combination with an activator of soluble guanylate cyclase is (sGC) soluble guanylate cyclase () administered as they are described for example in WO2009032249.

In another embodiment, the compound of formula I in combination with an inhibitor of carbonic anhydrase type 2 (Carbonic anhydrase type 2), such as those as described in WO2007065948, WO2009050252 describes administered.

In another embodiment, the compound of formula I in combination with topiramate or a derivative thereof, as described in WO2008027557, US2009304789, administered.

In another embodiment, the compound of formula I in combination with a fixed combination of topiramate with phentermine (Qnexa ™) is administered. In a further embodiment, the compound of formula I in combination with an antisense compound, for example, ISIS 377131 is administered, which inhibits the production of the glucocorticoid receptor.

In another embodiment, the compound of formula I in combination with an aldosterone synthase inhibitor and an antagonist of the is

Glucocorticoid receptor, a cortisol synthesis inhibitor and / or an antagonist of the corticotropin-releasing factor (corticotropin releasing factor), such as described in EP1886695, WO20081 19744, administered. In one embodiment, the compound of formula I in combination with an agonist of the RUP3 receptor is such. B. in WO2007035355, WO2008005576 describes administered.

In another embodiment, the compound of formula I in combination with an activator of the gene (ATM) encodes protein kinase for the ataxia telangiectasia mutated such is. As chloroquine administered. In one embodiment, the compound of formula I in combination with a tau protein kinase 1 inhibitor is (TPK1 inhibitor), such as. B. WO20071 19463,

WO2009035159, WO2009035162 describes administered.

In one embodiment, the compound of formula I in combination with a "c-Jun N-terminal kinase" inhibitor (JNK inhibitor) is such. B. BI-78D3 or those described in WO2007125405, WO2008028860 described, WO20081 18626, administered . in one embodiment, the compound of formula I in combination with an endothelin-a receptor antagonist, such as. for example, avosentan (SPP-301) administered.

In one embodiment, the compound of formula I in combination with neutral endopeptidase inhibitors (NEP inhibitors), as for example in

WO2009138122, are described in WO2009135526, is administered.

In one embodiment, the compound of formula I in combination with modulators of the glucocorticoid receptor is (GR), such as KB-3305 or those compounds as such. As in WO 2005/090336, WO2006071609, WO2006135826, WO2007105766, WO2008120661, WO2009040288, WO2009058944,

WO2009108525, WO20091 1 1214 describes administered.

In one embodiment, the further active ingredient Varenicl ine tartrate, a partial agonist of the alpha 4-beta 2 nicotinic acetylcholine receptor is.

In one embodiment, the further active compound is an agonist of the alpha 7 nicotinic acetylcholine receptor as described for example in WO2009018551, WO2009071519, WO2009071576, WO2009071577 are described. In one embodiment, the further active ingredient is Trodusquemine. In one embodiment, the further active ingredient is a modulator of the SIRT1 enzyme and / or SIRT3 (a NAD + -dependent Proteindeacetylase); this drug may be appropriate in Fornnulierungen example, resveratrol, or those compounds as described in WO2007019416 (eg SRT-1720), WO2008073451, WO2008156866,

WO2008156869, WO2009026701, WO2009049018, WO2009058348,

are called WO2009061453, WO2009134973, WO2009146358, WO2010003048.

In one embodiment of the invention, the further active ingredient DM-71 is (N-acetyl-L-cysteine ​​with bethanechol).

In one embodiment, the compound of formula I in combination with anti- hypercholesterolemic acting compounds, as for example, in WO2004000803, WO2006000804, WO2004000805, WO2004087655, WO20051 13496 is

WO2007059871, WO2007107587, WO20071 1 1994, WO2008052658,

WO2008106600, WO20081 13796, US2008280836, WO20091 13952, are described US2009312302 administered.

In another embodiment, the compound of formula I in combination with inhibitors of SREBP (sterol regulatory element-binding protein) is, for example

Fatostatin or those as are described for example in WO2008097835, is administered.

In another embodiment, the compound of formula I in combination with a cyclic peptide agonist of the VPAC2 receptor, as described for example in

WO2007101 146, are described in WO2007133828, is administered.

In a further embodiment, the compound of formula I in combination with an agonist of the endothelin receptor, as described for example in WO20071 12069, is administered. In another embodiment, the compound of formula I in combination with ACP-020 is administered (bis (ethylmaltolato) oxovanadium-IV). In another embodiment, the compound of Fornnel I in Konnbination with tissue-selective androgen receptor modulators ( "tissue-selective androgen receptor modulators"; SARM) as administered, for example, in WO2007099200, WO2007137874 are described.

In a further embodiment, the compound of formula I in combination with an AGE (advanced glycation end-product) inhibitor such as, for example, in

JP2008024673 describes administered. In one embodiment of the invention, the further active ingredient is leptin;

See, eg, "Perspectives in the therapeutic use of leptin", Salvador, Javier; Gomez-Ambrosi, Javier; FRUHBECK, Gema, Expert Opinion on Pharmacotherapy (2001), 2 (10), 1615-1622. In another embodiment of the invention, the further active ingredient Metreleptin (recombinant methionyl leptin) is combined with pramlintide.

In a further embodiment of the invention, the further active ingredient is the tetrapeptide ISF 402nd

In one embodiment, the further active ingredient is dexamphetamine or

Amphetamine.

In one embodiment, the further active ingredient is fenfluramine or dexfenfluramine.

In yet another embodiment, the further active ingredient is sibutramine or such derivatives as are described in WO2008034142 is.

In one embodiment, the further active ingredient is mazindol or phentermine.

In another embodiment, the further active ingredient is Geniposidinsäure

(Geniposidic acid; WO2007100104) or derivatives thereof (JP2008106008). In another embodiment, the further active compound is an agonist of

Neuropeptide FF2 as described for example in WO2009038012.

In one embodiment, the further active ingredient is a nasally administered

Calcium channel blockers such as diltiazem, or those as described in US 7,138,107.

In one embodiment, the further active ingredient is an inhibitor of the sodium-calcium ion-exchange, for example those as described in WO2008028958, WO200808571. 1

In another embodiment, the further active ingredient is a blocker of

Calcium channels such as the CaV3.2 or CaV2.2 as in WO2008033431, WO2008033447, WO2008033356, WO2008033460, WO2008033464

WO2008033465, WO2008033468, WO2008073461 described.

In one embodiment, the further active ingredient is a modulator of a calcium channel such as those as described in WO2008073934, WO2008073936, WO2009107660.

In one embodiment, the further active ingredient is an inhibitor of

Calcium metabolism such as those as described in US2009124680.

In one embodiment, the other active ingredient is a blocker of the "T-type calcium channel" as described for example in WO2008033431, WO20081 10008, US2008280900

WO2008141446, US2009270338, WO2009146540, US2009325979, WO2009146539 described.

In one embodiment, the further active ingredient is an inhibitor of the KCNQ potassium channel 2 and -3, for example those as described in US2008027049, US2008027090. In one embodiment, the further active ingredient is a modulator of KCNN- potassium channel-1, -2 and -3 (modulators of SK1 -, SK2 and / or SK3 channel), for example those as described in US2009036475. In one embodiment, the further active ingredient is an inhibitor / blocker of the potassium Kv1 .3 ion channel such as those as described in WO2008040057, WO2008040058, WO2008046065, WO20090431 17th

In one embodiment, the further active ingredient is a potassium channel modulator such as those described in WO2008135447, WO2008135448, WO2008135591

WO2009099820 described.

In another embodiment, the further active ingredient is a

hyperpolarization activated and controlled by cyclic nucleotide potassium sodium channel inhibitor ( "hyperpolarization-activated cyclic nucleotide-gated (HCN) potassium-sodium channel inhibitor") such as those as described in US2009069296.

In another embodiment, the further active ingredient is an inhibitor of sodium-potassium 2-chloride (NKCCI) co-transporter, for example those as described in WO2009130735.

In another embodiment, the further active ingredient is an inhibitor of the voltage-guided sodium channel (voltage-gated sodium channel inhibitor), for example those as described in WO2009049180, WO2009049181.

In another embodiment, the further active ingredient is a modulator of the MCP-1 receptor (monocyte chemoattractant protein-1 (MCP-1)), for example those as described in WO2008014360, WO2008014381. In one embodiment, the further active ingredient is a modulator of

Somatostatin receptor 3 (SSTR3) such as those as described in WO200901 1836th In one embodiment, the further active ingredient is a modulator of

Somatostatin receptor 5 (SSTR5), such as those as described in WO2008019967

US2008064697, US2008249101, WO2008000692, US2008293756, WO2008148710 described. In one embodiment, the further active ingredient is a modulator of

Somatostatin receptor 2 (SSTR2), for example those as described in WO2008051272.

In one embodiment, the further active ingredient is a compound which is able to reduce the amount of the retinol-binding protein 4 (RBP4), such as those described, in WO2009051244 WO2009145286 are.

In one embodiment, the further active ingredient is an erythropoietin mimetic peptide, which acts as erythropoietin (EPO) receptor agonist. Such molecules are described for example in WO2008042800.

In another embodiment, the further active compound is an anorectic agent / hypoglycemic compound such as, for example, those as described in WO2008035305

WO2008035306, WO2008035686 described.

In one embodiment, the further active ingredient is an inducer of the

Liponsäuresynthetase such as those described in WO2008036966, WO2008036967 are described. In one embodiment, the further active ingredient is a stimulator of endothelial nitric oxide synthase (eNOS), such as those as described in WO2008058641

WO2008074413 described. In one embodiment, the further active ingredient is a modulator of the carbohydrate and / or lipid metabolism, such as those as described in WO2008059023

WO2008059024, WO2008059025, WO2008059026 are described.

In another embodiment, the further active ingredient is an angiotensin II receptor antagonist such as those as described in WO2008062905, WO2008067378, WO2008062905. In one embodiment, the further active compound is an agonist of the sphingosine-1 - phosphate receptor (S1 P), such as those as described in WO2008064315

WO2008074820. WO2008074821, WO2008135522, WO2009019167,

WO2009043013, WO2009080663, WO2009085847, WO2009151529,

WO2009151621, WO2009151626, WO2009154737 are described.

In one embodiment, the further active ingredient is an agent which the

Retarded gastric emptying, such as 4-hydroxyisoleucine (WO2008044770).

In one embodiment, the further active ingredient is inhibitor-1 (TPH1 inhibitor) which modulates gastrointestinal motility such as in WO2009014972 describes a tryptophan-5-hydroxylase.

In one embodiment, the further active compound is a muscle relaxant substance as described for example in WO2008090200.

In another embodiment, the further active ingredient is an inhibitor of

Monoamine oxidase B (MAO-B), such as those as described in WO2008092091

WO2009066152 described. In another embodiment, the further active ingredient is an inhibitor of

Monoamine oxidase A (MAO-A), for example those as described in WO2009030968. In another embodiment, the further active ingredient is an inhibitor of the binding of cholesterol and / or triglycerides in the SCP-2 protein (sterol carrier protein-2), for example those as described in US2008194658.

In another embodiment, the further active ingredient is a compound which binds to the beta-subunit of the trimeric GTP-binding protein, for example those as described in WO2008126920. In one embodiment, the further active ingredient is an inhibitor of

Harnsäureanionaustauschers-1 (urate-anion exchanger-inhibitor-1), as described for example in WO2009070740.

In one embodiment, the further active ingredient is a modulator of ATP transporter, as described for example in WO2009108657.

In another embodiment, the further active ingredient Lisofylline that prevents autoimmune damage to the insulin-producing cells. In yet another embodiment, the further active ingredient is described an extract of Bidens pilosa with the ingredient Cytopiloin as in EP1955701.

In one embodiment, the further active ingredient is an inhibitor of glucosylceramide synthase described for example in WO2008150486.

In a further embodiment of the invention, the further active ingredient is a

Glycosidase inhibitor such as in WO20091 17829, WO2009155753 described.

In another embodiment, the other active ingredient is an ingredient of Hoodia Gordonii plant as described in US2009042813, EP2044852. In one embodiment, the further active ingredient is an antidiabetic agent such as D-tagatose.

In one embodiment, the further active ingredient is a zinc complex of curcumin as described in WO2009079902.

In one embodiment, the further active ingredient is an inhibitor of the "cAMP response element binding protein" (CREB) is as described in WO2009143391. In another embodiment, the further active ingredient is an antagonist of the bradykinin B1 receptor as described in WO2009124746.

In another embodiment, the further active ingredient is a compound which is capable of diabetic peripheral neuropathy (DPN) to modulate. Such modulators are, for example FK-1706 or SB-509 or those described in WO1989005304, WO2009092129, WO2010002956 are described.

In one embodiment, the further active ingredient is a compound which is able to modulate the diabetic nephropathy. Such compounds are, for example, in WO2009089545, WO2009153261 described.

In one embodiment, the further active ingredient is an inhibitor (for example an anti-CD38 antibody) of CD38 as described in US2009196825.

In one embodiment, the further active ingredient is an inhibitor of the human

Fibroblast growth factor receptor 4 (human fibroblast growth factor receptor 4 (FGFR4)) as described for example in WO2009046141.

In a further embodiment of the invention, the further active ingredient is a beta cell protective compound such as 14-alpha-Lipolyl-andrographolide (AL-1). In yet another embodiment of the invention, the further active ingredient is the INGAP peptide (islet neogenesis associated protein), a peptide having the

Insulin production in patients with diabetes mellitus restores. In one embodiment of the invention, the further active ingredient is a modulator of CFTR (cystic fibrosis transmembrane conductance regulator) such as that described in

US2009246137, US2009264433, US2009264441, US2009264471, US2009264481, US2009264486, WO2010019239 described. In one embodiment of the invention, the further active ingredient is a compound which stimulates / modulates the release of insulin, such as those described in

WO2009109258, WO2009132739, US2009281057, WO2009157418 described. In one embodiment of the invention, the further active ingredient is an extract of Hippophae rhamnoides, as described for example in WO2009125071.

In one embodiment of the invention, the further active ingredient is a Huanglian and of Ku Ding Cha, as described for example in WO2009133458.

In another embodiment of the invention, the further active ingredient is an extract from root Cipadessa baccifera, as described in US2009238900.

In one embodiment of the invention, the further active Borapetoside A and / or C Borapetoside which from the plant SDH V, a species of are

Tinospora crispa, can be isolated as described for example in US2010016213.

In one embodiment, the compound of formula I in combination with bulking agents, preferably insoluble bulking agents (see for example, carob / Caromax ® (Zunft HJ; et al, Carob pulp preparation for treatment of hypercholesterolemia, ADVANCES IN THERAPY (2001 Sep-Oct). 18 (5), 230-6.) Caromax.RTM is a carob-containing product from. Nutrinova Nutrition Specialties & Food Ingredients GmbH, Industriepark Höchst, 65926 Frankfurt / Main)) administered. Combination with Caromax ® is possible in one preparation or by separate administration of compounds of the formula I and Caromax ®. Caromax.RTM ® can in this case in the form of food, such as administered in bakery products or muesli bars.

It is understood that any suitable combination of the invention

Compounds having one or more of the aforementioned compounds and optionally one or more further pharmacologically active substances is included in the scope of the present invention is considered to fall.

77

NO-1886 

80

81

PSN 632408 SYR-322

Solabegron lorcaserin hydrochloride 83

- H is lu- Gly T r P HE T hr

Leu-T yr Se r-Ser-Val-Asp S he

Glu lysed Gin Ala Ala L YS-G lu

T rp Ala 1 le P he

BIM-51077 TAK-536

E-6837 tesofensine

AVE 1625 (Proposed INN: dnnabant) TAK-475 (Lapaquistat acetate)

JMV-2810 JMV-2951

S-40755 LY-2463665

PF-429242 SLV-348 88

AMG 071 sobetirome

10

PSN 119-2 drospirenone

CVT-3619 INT-131

alpha-Lipolyl-andrographolide (AL-1) Fatostatin

PF-3246799

Furthermore, the following active ingredients for combination products are:

All anti-epileptic drugs that are listed in the Red List 2010, Chapter 15;

all antihypertensives, listed in the Red List 2010, Chapter 17;

all hypotensives that are listed in the Red List 2010, Chapter 19;

all anticoagulants which are listed in the Red List 2010, Chapter 20;

edium all Arteriosklerosem that are listed in the Red List 2010, Chapter 25;

all Betarezeptoren-, calcium channel blockers and inhibitors of the renin-angiotensin

Systems that are listed in the Red List 2010, Chapter 27;

all diuretics and circulation-promoting agents, the Red List 2010, Chapter

are called 36 and 37;

All withdrawal agents / agents for the treatment of addictive disorders that are listed in the Red List 2010, Chapter 39;

all coronary and gastrointestinal agents that are listed in the Red List 2010, Chapter 55 and 60;

all migraine drugs, neuropathy preparations and Parkinson agents that are listed in the Red List 2010, Chapter 61, 66 and 70th It is understood that any suitable combination of the invention

Compounds having one or more of the aforementioned compounds and optionally one or more further pharmacologically active substances is included in the scope of the present invention is considered to fall.

The examples listed below serve to illustrate the invention, but without limiting.

Table 1 :

The compounds were characterized as follows in more detail by LC / MS:

LC / MS methods

Method 1:

Column: Waters UPLC BEH C18 2.1 * 50 mm; 1 .7 pm

Solvent: H 2 O + 0.1% FA: AcN + 0.08% FA

Gradient: 95: 5 (0 min) to 5:95 (1 .1 min) to 5:95 (1 .7 min) to 95: 5 (1 .8 min) to 95: 5 (2 min)

Flow, temperature: 0.9 ml / min 55 ° C

Method 2:

Column: Waters UPLC BEH C18 2.1 * 50 mm; 1 .7 pm

Solvent: H 2 O + 0.05% FA: ACN + 0.035% FA

Gradient: 95: 5 (0 min) to 5:95 (1 .1 min) to 5:95 (1 .7 min) to 95: 5 (1 .8 min) to 95: 5 (2 min)

Flow, temperature: 0.9 ml / min 55 ° C

Method 3:

Column: YMC-Pack Jsphere H80 33 * 2.1, 4 pm

Solvent: H 2 O + 0.05% TFA: CH 3 OH + 0.05% TFA

Gradient: 98: 2 (1 min) to 5:95 (5.0 min) to 5:95 (6.25 min)

Flow, temperature: 1 .0 ml / min, RT

Method 4:

Column: Waters XBridge C18 4.6 * 50 mm; μηη 2.5

Solvent: H 2 O + 0.1% FA: ACN + 0.1% FA

Gradient: 97: 3 (0 min) to 40:60 (3.5 min) to 2:98 (4 min) to 2:98 (5 to 97: 3 (5.2 min) to 97: 3 (6.5 min)

Flow, temperature: 1 .3 ml / min 45 ° C

Method 5:

Column: Waters UPLC BEH C18 2.1 * 50 mm; 1 .7 pm

Solvent: H 2 O + 0.05% FA: ACN + 0.035% FA

Gradient: 98: 2 (0 min) to 5:95 (2 min) to 5:95 (2.6 min) to 95: 5 (2.7 to 95: 5 (3 min)

Flow, temperature: 0.9 ml / min 55 ° C Table 3:

49 427.88 ES + 1 428.27 [M + H] + 23.1 C23H22CIN05 A

50 441.91 ES + 1 442.18 [M + H] + 1:33 C24H24CIN05 A

51 481.98 1 ES- 480.1 [MH] - 1.27 C27H28CIN05 A

52 456.84 1 455.28 ES- [MH] - 1.32 C22H20CIF3O5 B

53 470.87 1 469.38 ES- [MH] - 1.38 C23H22CIF305 B

54 404.26 ES + 2 404.19 [M + H] + A 1.11 C19H18BrN04

55 359.81 ES + 4 360.21 [M + H] + 29.4 C19H18CIN04 A

56 339.39 ES + 2 340.26 [M + H] + 0.85 C20H21 NO4 A

57 338.40 ES + 1 339.32 [M + H] + 1.32 C21 H2204 A

58 352.43 1 351.34 ES- [MH] - 1.36 C22H2404 A

59 406.40 1 405.39 ES- [MH] - 1.37 C22H21 F304 A

60 427.81 ES + 1 428.21 [M + H] + A 1:36 C20H17CIF3NO4

61 372.85 1 371.32 ES- [MH] - 1.37 C21 H21CI04 A

62 394.51 1 393.34 ES- [MH] - A 1:43 C25H30O4

63 393.36 ES + 1 394.19 [M + H] + C20H18F3NO4 A 1:33

64 393.36 ES + 1 394.19 [M + H] + C20H18F3NO4 A 1:33

65 386.87 1 385.25 ES- [MH] - 1.38 C22H23CI04 A

66 420.43 1 419.29 ES- [MH] - 1.38 C23H23F304 A

67 366.46 1 365.23 ES- [MH] - 1.36 C23H2604 A

68 450.45 ES- 449.28 [MH] - 1.25 C24H25F305 C

69 475.38 ES + 476.19 [M + H] + 01.26 C22H19F6N04 D

70 475.38 ES + 1 476.12 [M + H] + 1:33 C22H19F6N04 D

71 475.38 ES + 1 476.18 [M + H] + 1:36 C22H19F6N04 D

72 420.43 1 419.28 ES- [MH] - 1.38 C23H23F304 A

73 360.80 1 ES- 359.2 [MH] - 1.25 C18H17CIN204 A

74 374.82 1 373.29 ES- [MH] - 1.28 C19H19CIN204 A

75 475.38 ES + 1 476.07 [M + H] + 1:36 C22H19F6N04 D

76 475.38 1 ES- 474.2 [MH] - 1.31 C22H19F6N04 D

77 475.38 ES + 1 476.11 [M + H] + 1:32 C22H19F6N04 D

78 339.39 ES + 1 340.13 [M + H] + 1:01 C20H21 NO4 A

79 407.39 ES + 2 408.06 [M + H] + 1:36 C21 H20F3NO4 A

80 441.83 2 440.07 ES- [MH] - 1.38 C21 H19CIF3N04 A

81 354.41 ES + 2 355.1 [M + H] + C20H22N2O4 1.23 A

82 340.38 ES + 2 341.07 [M + H] + C19H20N2O4 1.2 A

83 407.39 2 406.15 ES- [MH] - 1.32 C21 H20F3NO4 A

84 407.39 2 406.15 ES- [MH] - 1.35 C21 H20F3NO4 A

85 354.41 ES + 2 355.1 [M + H] + C20H22N2O4 1.24 A

86 509.83 2 508.09 ES- [MH] - A 1:40 C22H18CIF6N04

87 358.82 ES + 2 359.08 [M + H] + A 1:32 C20H19CIO4

88 358,82 ES 2 357.14 [MH] - 1.32 C20H19CIO4 A

89 340.38 ES + 2 341.12 [M + H] + C19H20N2O4 1.20 A

90 340.38 ES + 4 341.16 [M + H] + C19H20N2O4 4:05 A

91 393.36 ES + 2 394.17 [M + H] + C20H18F3NO4 1.29 A

92 458.55 5 459.25 ES + [M + H] + A 2.14 C29H30O5

93 419 147 5 421.24 ES + M + H] + A 2.12 C23H22F304

The activity of the compounds was tested as follows:

In vitro FLIPR assay with recombinant cells that express the GPCR GPR40 function examining assay using the FLIPR technology ( "Fluorescence Imaging Plate Reader", Molecular Devices Corp.) were performed. To this was agonist-induced changes in the intracellular concentration of Ca 2 + in recombinant HEK293 cells determined expressing the GPR40 GPCR (rat species).

For the investigations, cells (in 96-well microtiter plates 60000

seeded cells / well) and grown overnight. The medium was removed and the cells are incubated in buffer containing the fluorescent dye Fluo-fourth After this loading with dye, cells were washed,

Test substance is added and changes in intracellular Ca 2+ concentration measured in the FLIPR instrument. Results were expressed as percentage change shown relative to the control (0%: no test substance added; 100%: 10 μΜ

Reference agonist linoleic acid added) was used for calculation of dose / response curves and EC 5 o determined values.

Table 2: Biological Activity:

Example EC 50 [μΜ]

(Rat GPR40)

1 0:44

2 0:05

3 0:35

4 0.1 1

5 12:40

6 12:17

7 0.72

8 12:35

9 0.61

10 12:55

1 1 00:08

12 12:07

13 12:04

14 0.05 15 0.06

16 0.61

17 12:36

18 12:46

19 12:18

20 12:08

21 0.80

22 12:05

23 12:21

24 0.98

25 1 .99

26 12:05

27 12:05

28 12:05

29 12:17

30 12:14

31 0.64

32 0.77

33 1 .61

34 0.81

35 1 .09

36 1 .59

37 6:01

38 0.73

39 3.20

40 0.83

41 0.80

42 1 .78

43 2:03

44 5.10

45 6.85

46 8:49

47 8.74

48 7:50

49 0.15 50 0.55

51 2:40

52 0.99

53 12:20

54 0.63

55 0.60

56 3.1 1

57 0.09

58 12:09

59 12:10

60 12:05

61 12:06

62 0.66

63 12:07

64 0:08

65 0.1 1

66 12:21

67 0.28

68 12:43

69 12:20

70 12:59

71 1 .69

72 12:14

73 12:44

74 12:06

75 12:39

76 12:48

77 0.71

78 14:20

79 12:19

80 0.01

81 0.52

82 0.59 83 0.01

84 0.01

85 0.21

86 7.60

87 0.01

88 0.79

89 0.83

90 2.17

91 0.07

92 0.71

93 29.5

From the table it can be read that the compounds of the formula I activate the GPR40 receptor, and thus are very suitable for the treatment of hyperglycemia and diabetes. By the compounds of formula I, the

Insulin secretion increased (see Itoh et al., Nature 2003, 422, 173-176).

Due to the activation of the GPR40 receptor, the compounds of formula I for the treatment or prevention of further diseases may be employed.

The compounds of the present invention are particularly useful for the treatment and / or prevention of: The compounds of the present invention are particularly useful for the treatment and / or prevention of:

1 . - Disorders of fatty acid metabolism and glucose utilization disorders

- disorders in which insulin resistance is involved

2. Diabetes mellitus, especially type 2 diabetes, including the prevention of the sequelae associated therewith.

- Particular aspects in this connection are

- hyperglycemia, - improvement in insulin resistance,

- Improvement of glucose tolerance,

- Protection of the beta cells of the pancreas

- prevention of macro- and microvascular disorders

3. Various other conditions associated with the metabolic syndrome or

, Syndrome X may be associated as

- obesity (increased body mass index -BMI)

Increase in waist circumference (visceral adiposity)

- fatty liver (non-alcoholic fatty liver disease (NAFLD) and NASH)

- dyslipidemia (eg hypertriglyceridemia and / or low HDL)

- insulin resistance

- hypercoagulable

- hyperuricemia

- microalbuminuria

- thromboses, hypercoagulable and prothrombotic states (arterial and venous)

- High blood pressure

- heart failure, such as (but not limited) to

Myocardial infarction, hypertensive heart disease or cardiomyopathy memory impairment, mental defects, central nervous system disorders such as

- senile dementia

- Alzheimer's disease

- treatment decreased alertness or vigilance

- schizophrenia Gastrointestinal (GI) disorders

- Gl-dyskinesia (irritable bowel syndrome = irritable bowel syndrome (IDS) and

Irritable Bowel Syndrome (IBS), inflammatory bowel disease, irritable bowel syndrome and "nervous bowel") General preparation method

The compounds of formula I of the invention can be prepared according to the following reaction schemes:

Method A:

formula I

A compound of general formula A, wherein R4, R5, R6, R7, R8, R9, R10, R1 1, q and r have the meanings described above, with a phenol of general formula B wherein R1, R2 and R3 above

have meanings and R is an alkyl group such as methyl or ethyl, in the case that Y2 is a hydroxyl group under Mitsunobu conditions in the presence of, for example, triphenylphosphine and Diethyldiazodicarboxylate in an aprotic solvent such as dichloromethane to the compound of general formula C. In the case that Y2 is a halide such as bromide, or a leaving group such as mesylate or tosylate, the conversion to the compound of the general formula C takes place in the presence of a base such as cesium carbonate in a polar aprotic solvent such as dimethylformamide , In the event that a Y2

Hydroxyl group, the compound of the general formula C under Mitsunobu conditions in the presence of, for example, triphenylphosphine and

Diethyldiazodicarboxylate in an aprotic solvent such as dichloromethane, with a compound of the general formula D, wherein A, R12, R13 and R14 have the meanings described above and in the case that Y2 is a halide, such as fluoride, chloride or bromide, finds the conversion to the compound of the general formula C e reacted in a polar aprotic solvent such as dimethylformamide in the presence of a base such as sodium hydride, to compound of general formula. The

Compound of general formula I can alternatively also be obtained by first separating the compound of general formula A, wherein R4, R5, R6, R7, R8, R9, R10, R1 1, q and r have the meanings described above, either

Mitsunobu conditions for the case that Y1 represents a hydroxyl group, in the presence of, for example, triphenylphosphine and Diethyldiazodicarboxylate in an aprotic solvent such as dichloromethane, with a

Compound of general formula D, wherein A, R12, R13 and R14 have the meanings described above, and FG represents a hydroxyl group, or under the conditions of an aromatic nucleophilic substitution, for the case that Y1 represents a hydroxyl group, in a polar aprotic solvent such as for example, dimethylformamide or ethylene glycol in the presence of a base such as sodium hydride, with a compound of general formula D, wherein a, R12, R13 and R14 have the meanings described above, and FG means a fluorine, chlorine, or Bromtom for connection of the general formula F are reacted. In the event that Y1 is a halide such as bromide or

Leaving group such as mesylate or tosylate and FG represents a hydroxyl group, the conversion to the compound of the general formula F takes place in a polar aprotic solvent such as dimethylformamide in the presence of a base such as cesium or potassium carbonate. The compound of general formula F is then under Mitsunobu conditions in the presence of, for example, triphenylphosphine and Diethyldiazodicarboxylate in an aprotic solvent such as dichloromethane, with a phenol of general formula B wherein, have R2 and have the meanings described above, R1 R3 and R is a alkyl group such as methyl or ethyl, to give the compound of the general formula e. For the case that Y1 is a halide such as bromide, or a leaving group such as mesylate or tosylate, the conversion to the compound of the general formula is E in a polar aprotic solvent such as dimethylformamide in the presence of a base such as cesium carbonate instead of , Under the action of a base such as sodium or lithium hydroxide in a solvent mixture such as methanol, tetrahydrofuran and water of the esters of the general formula E is gepalten to give the free carboxylic acid of the general formula I.

According to this method, the examples of 1 - 51, 54-67, 72-74 and 78-93 produced. Method B:

A phenol of the general formula D, wherein A, R12, R13 and R14 have the meanings described above is reacted with epichlorohydrin in a polar solvent such as dimethylformamide in the presence of a base such as cesium carbonate to oxirane of the general formula G. The oxirane of the general formula G is reacted with a phenolic compound of the general formula B wherein have the meanings described above, R1, R2 and R3 and R is an alkyl group such as methyl or ethyl, in a polar solvent such as dimethylformamide in the presence of a base such as for example, 1, 4-diazabicyclo [2.2.2] undecene to give the compound of the general formula H. The alcohol moiety of the compound of general formula H is reacted with an alkylating agent RX wherein X is a leaving group such as bromide, iodide, mesylate or tosylate, and R is an alkyl group such as methyl or ethyl, in a polar solvent such as dimethylformamide in the presence of a base such as sodium hydride to give a compound of general formula I. Under the action of a base such as sodium hydroxide in a solvent mixture such as methanol, tetrahydrofuran and water of the esters of general formula I is cleaved to give the free carboxylic acid of the general formula Ib.

According to this method, the examples were prepared 52 and 53rd Method C:

A phenol of allgenneinen formula J wherein A, R12, R13 and R14 have the meanings described above is reacted with 2-hydroxymethyl-propane-1, 3-diol under Mitsunobu conditions in the presence of, for example, triphenylphosphine and Diisopropyldiazodicarboxylate in an aprotic solvent such as for example, dichloromethane to give the compound of the general formula K. Under the same conditions, the Vverbindung of the general formula K with a compound of general formula B wherein have the meanings described above, R1, R2 and R3 and R is an alkyl group such as methyl or ethyl, to give a compound of the general formula L. The alcohol moiety of the compound of general formula L is reacted with an alkylating agent RX wherein X is a leaving group such as bromide, iodide, mesylate or tosylate, and R is an alkyl group such as methyl or ethyl, in a polar

Solvent such as dimethylformamide such as sodium hydride in the presence of a base to give a compound of general formula M. Under the action of a base such as sodium hydroxide in a

Solvent mixture such as methanol, tetrahydrofuran and water of the esters of formula allgenneinen M is cleaved to give the free carboxylic acid of the general formula Ic.

According to this method, the example 68 was prepared.

learn D:

A phenolic compound of the general formula B wherein R1, R2 and R3 have the meanings described above and R is an alkyl group such as methyl or ethyl is reacted with an alkylating reagent of general formula N wherein X is a leaving group such as bromide, iodide, mesylate or tosylate means, in a polar solvent such as dimethylformamide in the presence of a base such as sodium hydride to a dimethyl acetal of the general formula O. The acetal is reacted as using an acid such as hydrochloric acid in an aprotic solvent, for example THF to give an aldehyde of the general formula P. The introduction of

Trifluoromethyl succeeds using trimethyl-trifluoromethyl-silane and tetra-n-butylammonium fluoride followed by cleavage of the

Trimethylsilyl group using an acid such as hydrochloric acid to give alcohols of the general formula Q. These are using

Fluoroaromatics of the general formula R in which A, R12, R13 and R14 have the abovementioned meaning, are reacted in a polar solvent such as dimethylformamide in the presence of a base such as sodium hydride to a compound of general formula S. Under the action of a base such as sodium hydroxide in a solvent mixture such as methanol, tetrahydrofuran and water of the esters of the general formula M is cleaved to give the free carboxylic acid of the general formula Id. According to this method Examples 69-71 and 75- were 77 produced. List of Abbreviations:

Ac acetyl

AcN acetonitrile

Bn benzyl

iBu isobutyl

tBu tert-butyl

BuLi n-butyllithium

TLC thin layer chromatography

DEAD diethylazodicarboxylate

DCI direct chemical ionization (in MS)

DCM dichloromethane

DMAP 4-N, N-dimethylaminopyridine

DMF N, N-dimethylformamide

DMSO dimethyl sulfoxide

EE ethyl acetate

ent enantiomer / enantiomerically

EI electron impact ionization (in MS)

eq equivalent

ESI electron spray ionization (in MS)

FA formic acid FG Functional group

Hal is halogen

HPLC high pressure, high performance liquid chromatography

LC-MS liquid chromatography-coupled mass spectroscopy m meta

me methyl

MeOH methanol

MS mass spectrometry

ms mesyl

NMR nuclear magnetic resonance spectroscopy

o ortho

p para

Pd / C palladium on carbon

iPr isopropyl

nPr n-propyl

rac Racemic / racemic mixture

Rf retention time (in DC)

RP reverse phase

TFA trifluoroacetic

THF tetrahydrofuran

Ts tosyl The following specific examples of the various methods will be described in detail.

EXPERIMENTAL SECTION

Example Synthesis according to method A:

example 1

3- 4- [3- (3-tert-butyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

example 1

3- (3-tert-butyl-phenoxy) -propan-1-ol

In a 50 ml three-necked flask 620 mg of 3-tert-butylphenol, 0.546 ml of 3-bromo-1-propanol and suspended 2:02 g of cesium carbonate in 10 ml acetonitrile. The

Reaction mixture for one hour at 60 ° C was stirred. to the cooled

Reaction mixture were add 50 ml of water and 50 ml ethyl acetate. The organic phase was separated, dried over MgSO 4 and concentrated in vacuo. 1 .1 g of 3- (3-tert-butyl-phenoxy) -propan-1-ol was obtained, this material was reacted further without further purification.

C13H20O2 (208.30), LCMS (ESI-pos): 209.2 (M + H +).

3- {4- [3- (3-tert-butyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäuremethylester

525 mg of 3- (3-tert-butyl-phenoxy) -propan-1-ol, 500 mg of 3- (4-Hydroxy-phenyl) -hex-4- ynoylsäuremethylester and 600 mg of triphenylphosphine were dissolved in 100 ml

Of dichloromethane. Under ice cooling, 00:31 ml of diethyl azodicarboxylate were added dropwise. Thereafter, the ice bath was removed and the reaction mixture stirred at room temperature for three hours. There were added an additional 600 mg of triphenylphosphine and 00:31 ml of diethyl azodicarboxylate and the reaction mixture 12 hours at room temperature, allowed to stand. To the reaction mixture 50 ml of water and 50 ml of ethyl acetate were to admit. The organic phase was separated, dried over MgSO 4 and concentrated in vacuo. The residue was 100% => ethyl acetate purified on silica gel with a solvent mixture of n-heptane / ethyl acetate as the linear gradient of n-heptane 100%. This gave 280 mg of 3- ynoylsäuremethylester {4- [3- (3-tert-butyl-phenoxy) -propoxy] -phenyl} -hex-4.

3- 4- [3- (3-tert-butyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

280 mg of 3- {4- [3- (3-tert-butyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäuremethylester were dissolved in a mixture of THF / MeOH / 2N NaOH = 1: 1: 1 (depending 5 ml) and stirred at room temperature. After 1 hour, was acidified by addition of 2N HCl to pH1. 50 ml of water was added and three times with 50 ml

Ethyl acetate. The combined organic phases were dried over MgSO4, then concentrated in vacuo and the residue chromatographed on

Kiesegel cleaned with a solvent mixture of n-heptane / ethyl acetate as a linear gradient, 100% n-heptane => 100% ethyl acetate. This gave 80 mg of 3- {4- [3- (3-tert-butyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäure. example 2

3- 4- [2- (3-tert-butyl-phenoxy) -ethoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 there was obtained from 3-tert-butylphenol, 2-bromo-1 -ethanol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2- (3-tert-butyl -phenoxy) -ethoxy] - phenyl} -hex-4-ynoylsäure.

example 3

3- 4- [4- (3-tert-butyl-phenoxy) -butoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 there was obtained from 3-tert-butylphenol, 4-bromo-1-butanol and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [4- (3-tert-butyl phenoxy) -butoxy] - phenyl} -hex-4-ynoylsäure.

example 4

3- 4- [3- (2-Chloro-4-trifluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 there was obtained from 2-chloro-4-trifluomethylphenol, 3-bromo-1 - propanol and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (2-Chloro -4- trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäure. example 5

3- 4- [3- (3,5-Bis-tnfluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 there was obtained from 3,5-Bis-trifluoromethyl-phenol, 3-bromo-1 - propanol and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (3 , 5-bis- trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäure.

example 6

3- 4- [3- (2-trifluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 there was obtained from 2-trifluoromethyl-phenol, 3-bromo-1-propanol and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (2-trifluoromethyl phenoxy ) -propoxy] -phenyl} -hex-4-ynoylsäure.

example 7

3- 4- [3- (2-Chloro-3-trifluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 there was obtained from 2-Chloro-3-trifluoromethyl-phenol, 3-bromo-1 - propanol and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (2 -chloro-3-trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäure. example 8

3- 4- [3- (6-trifluoromethyl-pyridin-3-yloxy) -propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 there was obtained from 6-Trifluoromethyl-pyridin-3-ol, 3-bromo-1 - propanol and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (6 - trifluoromethyl-pyridin-3-yloxy) -propoxy] -phenyl} -hex-4-ynoylsäure.

example 9

3- 4- [3- (2-Chloro-5-trifluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 there was obtained from 2-Chloro-5-trifluoromethyl-phenol, 3-bromo-1 - propanol and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (2 -chloro-5-trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäure.

example 10

3- 4- [2- (6-trifluoromethyl-pyridin-3-yloxy) -ethoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 there was obtained from 6-Trifluoromethyl-pyridin-3-ol, 2-bromo-1 -ethanol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2- (6 -Trifluoromethyl- pyridin-3-yloxy) -ethoxy] -phenyl} -hex-4-ynoylsäure.

Example 1 1 3- {4- [3- (4-Trifluoronnethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

3- (4-Trifluoronnethyl-phenoxy) -propan-1-ol

In a 50 ml three-necked flask, 750 mg 4-hydroxybenzotrifluoride, 0.63 ml of 3-propanol and 2.26 g of cesium carbonate in 10 ml of acetonitrile was suspended bromine -1. The reaction mixture was stirred for one hour at 60 ° C. to the cooled

Reaction mixture was added 50 ml of water and 50 ml ethyl acetate admit The organic phase was separated, dried over MgSO 4 and concentrated in vacuo. 1 .0 g was obtained 3- (4-trifluoromethyl-phenoxy) -propan-1-ol This material was further reacted without further purification.

C10H 11 F3O2 (220.19), LCMS (ESI-pos): 221 .2 (M + H +). 3- 4- [3- (4-trifluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäuremethylester

Cs 2 C0 3, MeCN

In a 100 ml 3-neck flask 1 .0 g of 3- (4-trifluoromethyl-phenoxy) -propan-1 - ol and submitted 1 .35 ml of diisopropylethylamine in 80 ml methylene chloride and cooled to 0 ° C. Then were added dropwise 0.71 ml of methanesulfonyl chloride.

Thereafter, the ice bath was removed and the reaction mixture stirred for one hour at room temperature. To the reaction mixture 50 ml of water and 50 ml of ethyl acetate were to admit. The organic phase was separated, dried over MgSO 4 and concentrated in vacuo. To give 1 .3 g of methanesulfonic acid 3- (4-trifluoromethyl-phenoxy) -propyl ester, this material was reacted further without further purification. In a 50 ml three-neck flask were 1 .23 g

Methanesulfonic acid 3- (4-trifluoromethyl-phenoxy) -propyl ester, 300 mg of 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester and 1 .34 g of cesium carbonate in 25 ml of acetonitrile was suspended. The reaction mixture was stirred for one hour at 60 ° C. To the cooled reaction mixture were added 50 ml of water and 50 ml

Ethyl acetate to admit. The organic phase was separated, dried over MgSO 4 and concentrated in vacuo. The residue was purified on Kiesegel with a solvent mixture of n-heptane / ethyl acetate as a linear gradient, 100% n-heptane => 100% ethyl acetate. This gave 45 mg of 3- {4- [3- (4-trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäuremethylester.

C23H 2 3F 3 O 4 (420.43), LCMS (ESI-pos): 421 .1 (M + H +). - {4- [3- (4-trifluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

45 mg 3- {4- [3- (4-trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4- ynoylsäuremethylester were dissolved in a mixture of THF / MeOH / 2N NaOH 1: 1: 1 (2 ml ) and stirred at room temperature. After 1 hour was

acidified addition of 2N HCl to pH1. 50 ml of water was added and extracted three times with 50 ml ethyl acetate. The combined organic phases were dried over MgSO 4, then concentrated in vacuo and the residue purified by RP-HPLC. This gave 40 mg of 3- {4- [3- (4-trifluoromethyl phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäure.

example 12

3- 4- (3-m-tolyloxy-propoxy) -phenyl1-hex-4-vnoylsäure

Analogously to Example 1 1 were obtained from commercially erhieltlichem 1 - (3-bromopropoxy) - 3-methyl-benzene and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- [4- (3-m- tolyloxy-propoxy ) -phenyl] -hex-4-ynoylsäure. example 13

3- 4- [3- (3-Chloro-phenoxy) -ethoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 1 were obtained from commercially erhieltlichem 2- (1 -Bromethoxy) -3- chlorobenzene and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (3-Chloro- phenoxy) -ethoxy] -phenyl} -hex-4-ynoylsäure.

example 14

3- [4- (2-m-tolyloxy-ethoxy) -phenyl1-hex-4-vnoylsäure

Analogously to Example 1 1 were obtained from commercially erhieltlichem 2- (1 -Bromethoxy) -3-methyl benzene and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- [4- (2-m-tolyloxy-ethoxy ) -phenyl] -hex-4-ynoylsäure. example 15

3- 4- [2- (3-trifluoromethyl-phenoxy) -ethoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 1 were obtained from commercially erhieltlichem 2- (1 -Bromethoxy) -3- (trifluoromethyl) benzene and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2- (3 -trifluoromethyl-phenoxy) -ethoxy] -phenyl} -hex-4-ynoylsäure.

example 16

3- 4- [2- (4-tert-butyl-phenoxy) -ethoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 1 were obtained from commercially erhieltlichem 1 -tert-butyl-4- (2-chloro-ethoxy) benzene and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2 - (4-tert-butyl-phenoxy) -ethoxy] -phenyl} -hex-4-ynoylsäure.

example 17

3- {4- [2-phenoxy-ethoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 1 were obtained from commercially erhieltlichem 2-bromo-phenyl ether and 3- (4-hydroxy-phenyl) {[2-ethoxy phenoxy] phenyl} 4- -hex-4-3- ynoylsäuremethylester -hex -4-ynoylsäure. example 18

3- 4- [2- (2-fluoro-phenoxy) -ethoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 1 were obtained from commercially erhieltlichem 2- (1 -Bromethoxy) -2-fluoro-benzene and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2- (2-fluoro- phenoxy) -ethoxy] -phenyl} -hex-4-ynoylsäure.

example 19

3- 4- [2- (2-chloro-phenoxy) -ethoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 1 were obtained from commercially erhieltlichem 2- (1 -Bromethoxy) -2-chlorobenzene and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2- (2-chloro-phenoxy ) -ethoxy] -phenyl} -hex-4-ynoylsäure.

example 20

3- [4- (2-o-tolyloxy-ethoxy) -phenyl1-hex-4-vnoylsäure

Analogously to Example 1 1 were obtained from commercially erhieltlichem 2- (1 -Bromethoxy) -2-methyl benzene and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- [4- (2-o-tolyloxy-ethoxy ) -phenyl] -hex-4-ynoylsäure. example 21

3- 4- [2- (2-methoxy-phenoxy) -ethoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 1 were obtained from commercially erhieltlichem 2- (1 -Bromethoxy) -2- methoxybenzene and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2- (2-methoxy- phenoxy) -ethoxy] -phenyl} -hex-4-ynoylsäure.

example 22

3- 4- [2- (2- (trifluoromethyl) phenoxy) -ethoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 1 were obtained from commercially erhieltlichem 2- (1 -Bromethoxy) -2- (trifluoromethyl) benzene and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2- (2 - (trifluoromethyl) phenoxy) -ethoxy] -phenyl} -hex-4-ynoylsäure.

example 23/24

3- {4 - [(S or R) -3- (4-trifluoromethyl-phenoxy) -butoxy1-phenyl) -hex-4-vnoylsäure and

3- {4 - [(R or S) -3- (4-trifluoromethyl-phenoxy) -butoxy1-phenyl) -hex-4-vnoylsäure

(S or R) -3- (4-trifluoromethyl-phenoxy) -butan-1-ol and (R or S) -3- (4-trifluoromethyl-phenoxy) -butan-1-ol

500 mg of 4-hydroxybenzotrifluoride, 0.70 ml of 1, 3-butanediol and 1 .62 g of resin bound triphenylphosphine were charged to a 100 ml round-bottomed flask in 20 ml of dichloromethane under argon and cooled to 0 ° C, at this temperature, 1 .21 ml of diisopropyl dissolved in 10 ml of dichloromethane, are slowly added dropwise. The ice-cooling was removed and the mixture is stirred overnight. The

Reaction mixture was filtered to remove the resin, washed with 50 ml of dimethylformamide, dichloromethane and methanol and the filtrate concentrated in vacuo. The residue was purified by chiral HPLC. 35 mg (S or R) was obtained -3- (4-trifluoromethyl-phenoxy) -butan-1-ol and 35 mg of (R or S) -3- (4-trifluoromethyl-phenoxy) -butan-1-ol. The absolute configuration was not determined. Furthermore, 165 mg of 3- (4-trifluoromethyl-phenoxy) -butan-1-ol were isolated.

3- (4-trifluoromethyl-phenoxy) -butan-1-ol: C11 H13F3O2 (392.38), chiral HPLC: AD / H 55 250 + 4.6 mm, eluent n-heptane: isopropanol = 50: 1, R t = 22,333 min and 23,212 rpm.

(R or S) - 3- (4-trifluoromethyl-phenoxy) -butan-1-ol: C11 H13F3O2 (392.38), chiral HPLC: AD / H 55 250 + 4.6 mm, eluent n-heptane: isopropanol = 50: 1, R t = 16,312 min. (S or R) - 3- (4-trifluoromethyl-phenoxy) -butan-1-ol: C11 H13F3O2 (392.38), chiral HPLC: AD / H 55 250 + 4.6 mm, eluent n-heptane: isopropanol = 50: 1, R t = 20 122 min.

example 23

3- 4 - [(S or R) -3- (4-trifluoromethyl-phenoxy) -butoxy1-phenyl) -hex-4-vnoylsäure

(S or R)

Analogously to Example 1 there was obtained from (S or R) - 3- (4-trifluoromethyl-phenoxy) -butan-1-ol and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [ (S or R) -3- (4-trifluoro-methyl-phenoxy) -butoxy] -phenyl} -hex-4-ynoylsäure.

example 24

3- 4 - [(R or S) -3- (4-trifluoromethyl-phenoxy) -butoxy1-phenyl) -hex-4-vnoylsäure

(R or S) Analogously to Example 1 there was obtained from (R or S) - 3- (4-trifluoromethyl-phenoxy) -butan-1-ol and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3 - {4 - [(R or S) -3- (4-trifluoro-methyl-phenoxy) -butoxy] -phenyl} -hex-4-ynoylsäure.

example 25

3- 4- [1-methyl-3- (4-trifluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 there was obtained from 3- (4-trifluoromethyl-phenoxy) -butan-1-ol and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [1-methyl-3- (4-trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäure.

example 26

- [4- (3-m-tolyloxy-butoxy) -phenyl1-hex-4-vnoylsäure

4-tert-butyl-diphenyl-silanyloxy) -butan-2-ol

In a 100 ml round bottom flask, 222 mg of sodium hydride was submitted (60% in mineral oil) in 20 ml of tetrahydrofuran. There were 1 .0g 1, 3-butanediol and 1 .42 ml of tert-butyldiphenylchlorosilane added at room temperature. The reaction mixture was stirred for one hour at room temperature, then allowed to stand overnight. 30 ml of water and 30 ml of ethyl acetate were then added to the reaction mixture. The organic phase was separated, the aqueous phase is extracted three times with 30 ml ethyl acetate. The combined organic phases were dried over MgSO 4 and concentrated in vacuo. The residue was purified on Kiesegel with a solvent mixture of n-heptane / ethyl acetate as a linear gradient, 100% n-heptane => 100% ethyl acetate. This gave 667 mg of 4- (tert-butyl-diphenyl-silanyloxy) -butan-2-ol.

C20H28O2S1 (328.53), LCMS (ESI-pos): 329.2 (M + H +).

3-m-tolyloxy-butan-1-ol

128.3 mg of m-cresol, 209.9 mg of 4- (tert-butyl-diphenyl-silanyloxy) -butan-2-ol and 125.7 mg of resin bound triphenylphosphine were initially charged in 5 ml of dichloromethane under argon. There were dropped 94.4 μΙ diisopropylazodicarboxylate and

heated reaction mixture under microwave irradiation for thirty minutes at 120 ° C. The reaction mixture was filtered from the resin and the filtrate was concentrated in vacuo. The residue was dissolved in 2 ml of tetrahydrofuran and 0.77 ml verstezt with tetra-N-Butylammoniumtrifluorid solution (1 M in tetrahydrofuran). The reaction mixture was stirred for three hours at room temperature, then allowed to stand overnight. The reaction mixture was concentrated in vacuo and the residue purified over RP-HPLC. This gave 41 .0 mg of 3-m-tolyloxy-butan-1-ol. C11 H 16O2 (180.25), LCMS (ESI-pos): 181 .2 (M + H +).

3- [4- (3-m-tolyloxy-butoxy) -phenyl1-hex-4-vnoylsäure

Analogously to Example 1 there was obtained from 3-m-tolyloxy-butan-1-ol and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- [4- (3-m-tolyloxy-butoxy) -phenyl ] -hex-4 ynoylsäure.

example 27

- [4 - ((R) -3-m-tolyloxy-butoxy) -phenyl1-hex-4-vnoylsäure

Analogously to Example 26 there was obtained from m-cresol, (R) -1, 3-butanediol and methyl 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- [4 - ((R) -3-m- tolyloxy-butoxy) -phenyl] -hex-4- ynoylsäure.

example 28

- [4 - ((S) -3-m-tolyloxy-butoxy) -phenyl1-hex-4-vnoylsäure

Analogously to Example 26 there was obtained from m-cresol, (S) -1, 3-butanediol and methyl 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- [4 - ((S) -3-m- tolyloxy-butoxy) -phenyl] -hex-4- ynoylsäure.

example 29

- 4 - [(R) -3- (2-trifluoromethyl-phenoxy) -butoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 26 there was obtained from 2-trifluoromethyl-phenol, (R) -1, 3-butanediol and methyl 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4 - [(R) -3- (2-trifluoromethyl- phenoxy) -butoxy] -phenyl} -hex-4-ynoylsäure. example 30

- {4 - [(S) -3- (2-trifluoromethyl-phenoxy) -butoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 26 there was obtained from 2-trifluoromethyl-phenol, (S) -1, 3-butanediol and methyl 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4 - [(S) -3- (2-trifluoromethyl- phenoxy) -butoxy] -phenyl} -hex-4-ynoylsäure.

example 31

3- 4 - [(R) -3- (2-chloro-4-trifluoromethyl-phenoxy) -butoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 26 there was obtained from 2-chloro-4-trifluoromethyl-phenol, (R) -1, 3-butanediol and methyl 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4 - [(R ) -3- (2-chloro-4-trifluoromethyl-phenoxy) -butoxy] -phenyl} -hex-4-ynoylsäure.

example 32

3- 4 - [(S) -3- (2-chloro-4-trifluoromethyl-phenoxy) -butoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 26 there was obtained from 2-chloro-4-trifluoromethyl-phenol, (S) -1, 3- butanediol and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4 - [(S ) -3- (2-chloro-4-trifluoromethyl-phenoxy) -butoxy] -phenyl} -hex-4-ynoylsäure. example 33

- {4- [3- (3-tert-butyl-phenoxy) -1-methyl-propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 1 to give 3-tert-butyl phenol-off, 1, 3-butanediol and methyl 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (3-tert-butyl phenoxy) -1 - methyl-propoxy] -phenyl} -hex-4-ynoylsäure.

example 34

example 34

3- 4- (3-Hydroxy-2-methyl-propoxy) -phenyl1-hex-4-vnoylsäuremethylester

500 mg of 3- (4-Hydroxy-phenyl) -hex-4-ynoylsäuremethylester, 1 .01 ml of 2-methyl-1, 3- propanediol, and 1 .20 g of resin bound triphenylphosphine in a 100 ml round-bottomed flask in 30 ml of dichloromethane under argon and cooled to 0 ° C. At this temperature, 0.91 ml of diisopropyl azodicarboxylate dissolved in 10 ml of dichloromethane, are slowly added dropwise. The ice-cooling was removed and the mixture is stirred for two days at room temperature. The reaction mixture was filtered to remove the resin washed three times with 50 ml of dichloromethane. The filtrate was washed with 30 ml 1 N HCl, dried over MgSO 4 and then in vacuo

concentrated. The residue was purified by RP-HPLC to give 486 mg of 3- [4- (3-hydroxy-2-methyl-propoxy) -phenyl] -hex-4-ynoylsäuremethylester.

C 7 H 22 O 4 (290.36), LCMS (ESI-pos): 291 .2 (M + H +).

3- {4- [2-methyl-3- (4-trifluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-

200 mg of 3- [4- (3-hydroxy-2-methyl-propoxy) -phenyl] -hex-4-ynoylsäuremethylester, 279 mg 4-hydroxybenzotrifluoride and 278 mg of resin bound triphenylphosphine in a 100 ml round-bottomed flask in 10 ml of dichloromethane under argon and cooled to 0 ° C. At this temperature, 271 μΙ were

Diisopropylazodicarboxylate dissolved in 10 ml of dichloromethane, are slowly added dropwise. The ice-cooling was removed and the reaction stirred for one day at room temperature. The reaction mixture was filtered from the resin three times with 50 ml

washed dichloromethane. The filtrate was concentrated in vacuum and the

Residue purified by RP-HPLC. To obtain 132 mg 3- {4- [2-methyl-3- (4-trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäuremethylester.

C 2 H 2 5F 3 O 4 (434.46), LCMS (ESI-pos): 435.3 (M + H +).

3- 4- [2-methyl-3- (4-trifluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

132 mg 3- {4- [2-methyl-3- (4-trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4- ynoylsäuremethylester were dissolved in a mixture of THF / MeOH / 2N NaOH = 1: 1: 1 (2 ml) and stirred at room temperature. After three hours, was acidified by addition of 2N HCl to pH1. 50 ml of water was added and extracted three times with 50 ml ethyl acetate. The combined organic phases were dried over MgSO 4 and then concentrated in vacuo. To obtain 126 mg 3- {4- [2-methyl-3- (4-trifluoromethyl-phenoxy) -propoxy] -phenyl} - hex-4-ynoylsäure.

example 35

3- 4- [3- (3-tert-butyl-phenoxy) -2-methyl-propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 34 there was obtained from 3-tert-butyl-phenol, 2-methyl-1, 3-propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (3 -tert-butyl phenoxy) -2-methyl-propoxy] -phenyl} -hex-4-ynoylsäure. example 36

3- 4- [3- (2-isopropyl-5-methyl-phenoxy) -2-methyl-propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 34 there was obtained from 2-isopropyl-5-methyl-phenol, 2-methyl-1, 3- propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (2-isopropyl-5-methyl-phenoxy) -2-methyl-propoxy] -phenyl} -hex-4-ynoylsäure.

example 37

3- {4- [3- (4-tert-butyl-2-chloro-phenoxy) -2-methyl-propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 34 there was obtained from 4-tert-butyl-2-chloro-phenol, 2-methyl-1, 3- propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [ 3- (4-tert-butyl-2-chloro-phenoxy) -2-methyl-propoxy] -phenyl} -hex-4-ynoylsäure.

example 38

3- 4- [2-methyl-3- (2-trifluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 34 there was obtained from 2-trifluoromethyl-phenol, 2-methyl-1, 3- propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2-methyl-3- (2-trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäure.

example 39

3- 4- [3- (5-isopropyl-2-methyl-phenoxy) -2-methyl-propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 34 there was obtained from 5-isopropyl-2-methyl-phenol, 2-methyl-1, 3- propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (5- isopropyl-2-methyl-phenoxy) -2-methyl-propoxy] -phenyl} -hex-4-ynoylsäure.

example 40

3- {4- [3- (4-Bromo-3-chloro-phenoxy) -2-methyl-propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 34 there was obtained from 4-bromo-3-chloro-phenol, 2-methyl-1, 3- propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (4-bromo-3-chloro-phenoxy) -2-methyl-propoxy] -phenyl} -hex-4-ynoylsäure.

example 41

3- 4- [2,2-dimethyl-3- (4-trifluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 34 there was obtained from 4-hydroxybenzotrifluoride, 2,2-dimethyl-1, 3- propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2,2-dimethyl- 3- (4-trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäure.

example 42

3- 4- [2- (4-trifluoromethyl-phenoxymethyl) -butoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 34 there was obtained from 4-hydroxybenzotrifluoride, 2-ethyl-1, 3- propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2- (4-trifluoromethyl-phenoxymethyl ) butoxy] phenyl} -hex-4-ynoylsäure.

example 43

3- {4- [2- (3-tert-butyl-phenoxymethyl) -butoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 34 there was obtained from 3-tert-butyl-phenol, 2-ethyl-1, 3-propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2- (3 -tert-butyl phenoxymethyl) -butoxy] -phenyl} -hex-4-ynoylsäure.

example 44

3- 4- [2- (4-trifluoromethyl-phenoxymethyl) -pentyloxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 34 there was obtained from 4-hydroxybenzotrifluoride, 2-propyl-1, 3- propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2- (4-trifluoromethyl-phenoxymethyl ) -pentyloxy] -phenyl} -hex-4-ynoylsäure.

example 45

- {4- [2- (3-tert-butyl-phenoxymethyl) -pentyloxy1-phenyl) -hex-4 -ynoylsäure

Analogously to Example 34 there was obtained from 3-tert-butyl-phenol, 2-propyl-1, 3-propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2- (3 -tert-butyl phenoxymethyl) -pentyloxy] -phenyl} -hex-4-ynoylsäure. example 46

3- 4- [2-phenyl-3- (4-tnfluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 34 there was obtained from 4-hydroxybenzotrifluoride, 2-phenyl-1, 3- propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2-phenyl-3- (4 -trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäure.

example 47

3- 4- [3- (3-tert-butyl-phenoxy) -2-phenyl-propoxy1-phenyl) -hex-4-vnoylsäure

Analogously to Example 34 there was obtained from 3-tert-butyl-phenol, 2-phenyl-1, 3-propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (3 -tert-butyl phenoxy) -2-phenyl-propoxy] -phenyl} -hex-4-ynoylsäure. example 48

3- {4- [2-benzyloxy-3- (2-chloro-4-trifluoromethyl-phenoxy) -propoxy1-phenyl) -hex-4- ynoylsäure

Analogously to Example 25 there was obtained from 3-chloro-4-hydroxybenzotrifluoride, 2-benzyloxy-1, 3-propanediol, and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [2- benzyloxy 3- (2-chloro-4-trifluoromethyl-phenoxy) -propoxy] -phenyl} -hex-4-ynoylsäure. example 49

3- {4- [3- (3-chloro-4-cvano-phenoxy) -2-hvdroxymethyl-propoxy1-phenyl) -hex-4- noylsäure

2-chloro-4- (3-Hydroxy-2-hvdroxymethyl-propoxy) -benzonitrile

5.0 g of 2-chloro-4-fluorobenzonitrile and 10.2 g of 2- (hydroxymethyl) -1, 3-propanediol, N-methylpyrrolidone were dissolved and cooled in an ice bath to 0 ° C in 230 ml. At this temperature, 1 .40 g of sodium hydride (55% dispersion in mineral oil) was added. The ice bath was removed and the reaction mixture stirred for twelve hours at room temperature. The mixture was then carefully added 80 ml of water and the mixture five times with portions of 80 ml of

Ethyl acetate. The combined organic phases were washed with 100 ml water, dried over MgSO 4 and then concentrated in vacuo. The residue was chromatographed on silica gel using the solvent mixture of n-heptane / ethyl acetate as a linear gradient, 100% n-heptane => 100% ethyl acetate cleaned. 3.0 g of 2-chloro-4- (3-hydroxy-2-hydroxymethyl-propoxy) -benzonitrile was obtained as a colorless oil.

H C11 NO3 12CI (241 .68) DC in ethyl acetate: R f = 0.27.

3- {4- [3- (3-chloro-4-cvano-phenoxy) -2-hvdroxymethyl-propoxy1-phenyl) -hex-4- noylsäure

Analogously to Example 1 there was obtained from 2-chloro-4- (3-hydroxy-2-hydroxymethyl-propoxy) -benzonitrile and 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester 3- {4- [3- (3-chloro-4-cyano-phenoxy) -2-hydroxymethyl-propoxy] -phenyl} -hex-4-ynoylsäure.

example 50

3- {4- [3- (3-chloro-4-cvano-phenoxy) -2-methoxynnethyl-propoxy1-phenyl) -hex-4- noylsäure

I Example 50

3- {4- [3- (3-chloro-4-cvano-phenoxy) -2-methoxynnethyl-propoxy1-phenyl) -hex-4- ynoylsäuremethylester

150 mg of 3- {4- [3- (3-chloro-4-cyano-phenoxy) -2-hydroxymethyl-propoxy] -phenyl} -hex-4- ynoylsäuremethylester and 0.1 1 ml of methyl iodide were dissolved in 3 ml of dimethylformamide and ice bath cooled to 0 ° C. At this temperature, 22.2 mg of sodium hydride (55% dispersion in mineral oil) was added. The ice bath was removed and the reaction mixture stirred for two hours at room temperature. Then cautiously 10 ml of water was added and the mixture extracted five times with portions of 10 ml ethyl acetate. The combined organic phases were washed with 40 ml water, dried over MgSO 4 and then concentrated in vacuo. To obtain 180 mg 3- {4- [3- (3-chloro-4-cyano-phenoxy) -2-methoxymethyl-propoxy] -phenyl} -hex-4-ynoylsäuremethylester, this material was reacted further without further purification.

C2 5 H26CINO 5 (455.94), LCMS (ESI-pos): 456.2 (M + H +).

3- {4- [3- (3-chloro-4-cvano-phenoxy) -2-methoxymethyl-propoxy1-phenyl) -hex-4- vnoylsäure

Analogously to Example 1 there was obtained from 3- {4- [3- (3-chloro-4-cyano-phenoxy) -2-methoxymethyl-propoxy] -phenyl} -hex-4-ynoylsäuremethylester 3- {4- [3- (3-chloro-4-cyano-phenoxy) -2-methoxymethyl-propoxy] -phenyl} -hex-4-ynoylsäure.

example 51

3- {4- [3- (3-chloro-4-cvano-phenoxy) -2-cvclopropylmethoxymethyl-propoxy1-phenyl) - hex-4-ynoylsäure

Analogously to Example 50 there was obtained from 3- {4- [3- (3-chloro-4-cyano-phenoxy) -2-hydroxymethyl-propoxy] -phenyl} -hex-4-ynoylsäuremethylester and

lodmethylcyclopropan 3- {4- [3- (3-chloro-4-cyano-phenoxy) -2-cyclopropylmethoxymethyl-propoxy] -phenyl} -hex-4-ynoylsäure.

Example Synthesis according to method B:

example 52

3- {4- [3- (2-chloro-4-trifluoromethyl-phenoxy) -2-hydroxy-propoxy1-phenyl) -hex-4- noylsäure

example 52

2- (2-chloro-4-thfluormethyl-phenoxymethyl) -oxirane

0:48 ml of epichlorohydrin, and 600 mg of 3-chloro-4-hydroxy-benzotrifluoride were dissolved in 50 ml of dimethylformamide and 2:49 g of cesium carbonate was added. The

Reaction mixture was heated two hours at 70 ° C. Carefully 50 ml of water was added then to the cooled reaction mixture and the mixture extracted three times with portions of 50 ml ethyl acetate. The combined organic phases were washed with 80 ml water, dried over MgSO 4 and then concentrated in vacuo. The residue was purified on silica gel with a solvent mixture of n-heptane / ethyl acetate as a linear gradient, 100% n-heptane => 100% ethyl acetate. This gave 550 mg of 2- (2-chloro-4-trifluoromethyl-phenoxymethyl) -oxirane.

CioH 8 ClF3 O2 (252.62), LCMS (ESI-pos): 235.0 (MH 2 O + H +).

3- {4- [3- (2-chloro-4-trifluoromethyl-phenoxy) -2-hydroxy-propoxy1-phenyl) -hex-4- ynoylsäuremethylester

434 mg of 2- (2-chloro-4-trifluoromethyl-phenoxymethyl) -oxirane, 250 mg of 3- (4-hydroxy-phenyl) -hex-4-ynoylsäuremethylester and 0:19 mL of 1, 4-diazabicyclo [2.2.2] octane were dissolved in 10 ml of N-methylpyrrolidone and heated to 80 ° C twenty hours. Subsequently, to the cooled reaction mixture is carefully added 50 ml of water and the mixture extracted three times with portions of 80 ml of

Ethyl acetate. The combined organic phases were washed with 100 ml water, dried over MgSO 4 and then concentrated in vacuo. The residue was chromatographed on silica gel using the solvent mixture of n-heptane / ethyl acetate as a linear gradient, 100% n-heptane => 100%

Ethyl acetate cleaned. To give 90 mg of 3- {4- [3- (2-chloro-4-trifluoromethyl-phenoxy) -2-hydroxy-propoxy] -phenyl} -hex-4-ynoylsäuremethylester.

C23H22CIF3O 5 (470.88), LCMS (ESI-pos): 471 .1 (M + H +), 493.1 (M + Na +). 3- {4- [3- (2-chloro-4-trifluoromethyl-phenoxy) -2-hydroxy-propoxy1-phenyl) -hex-4- vnoylsäure

Analogously to Example 1 there was obtained from 3- {4- [3- (2-chloro-4-trifluoromethyl-phenoxy) -2-hydroxy-propoxy] -phenyl} -hex-4-ynoylsäuremethylester 3- {4- [3- (2-chloro-4-trifluoromethyl-phenoxy) -2-hydroxy-propoxy] -phenyl} -hex-4-ynoylsäure.

example 53

3- {4- [3- (2-Chloro-4-trifluoromethyl-phenoxy) -2-methoxy-propoxy1-phenyl) -hex-4- noylsäure

Analogously to Example 51 there was obtained from 3- {4- [3- (2-chloro-4-trifluoromethyl-phenoxy) -2-hydroxy-propoxy] -phenyl} -hex-4-ynoylsäuremethylester 3- {4- [3- (2-chloro-4-trifluoromethyl-phenoxy) -2-methoxy-propoxy] -phenyl} -hex-4-ynoylsäure.

All other examples were each analog, according to the method indicated in Table 3. Production Process A, B, C or D, synthesized. The analysis of the compounds was carried out by LC / MS. The corresponding molecular peak or elimination products (see examples) could be detected in all examples by LC / MS.

Claims

claims:
1 . Compounds of the formula I,
I wherein
R1 (Ci-C 6) -alkyl, (C 3 -C 6) -cycloalkyl, (Ci-C 3) alkylene (C3-C6) cycloalkyl, wherein said (Ci-C 6) -alkyl cycloalkyl (C 3 -C 6) cycloalkyl, and the (dC 3) -alkylene- (C3-C6) can be one or polysubstituted with F, respectively;
R2, R3 are independently H, F, Cl, Br, CN, CO- (Ci-C 6) -alkyl, (Ci-C 6) -alkyl or O- (Ci-C 6) -alkyl, where the CO (Ci-C 6) -alkyl (Ci-C 6) -alkyl and O- (d-C6) -alkyl radical can in each case be mono or polysubstituted by F;
R4, R5, R6, R7, R8, R9, R10, R1 1 is independently H, (Ci-C 6) alkyl,
(Ci-C 3) -alkylene- (C 3 -C 6) cycloalkyl, (C 3 -C 6) -cycloalkyl, (C 6 -C 0) aryl), OH, O- (Ci-C 6) alkyl, O- (Ci-C 3) alkylene- (C 6 -C 0) aryl), O- (dC 3) -alkylene- (C 3 - C 6) cycloalkyl, O- (C 3 - C 6) cycloalkyl, (dC 3) -alkylene-OH, (dC 3) -alkylene- O- (Ci-C 6) alkyl, (Ci-C 3) alkylene-O- (Ci-C 3) alkylene- (C 3 -C 6) cycloalkyl, (dC 3) -alkylene-O- (C 3 -C 6) cycloalkyl, wherein said (Ci-C 6) alkyl radical, the (dC 3) - alkylene (C 3 -C 6) cycloalkyl radical, the (C 3 -C 6) -cycloalkyl, the O- (Ci-C 6) - alkyl radical 0- (Ci-C 3) alkylene (C 6 -Cio) aryl) rest> of 0- (Ci-C3) -alkylene- (C3-C6) cycloalkyl, the cycloalkyl O- (C3-C6), the (dC 3) alkylene- OH rest, the (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, the (Ci-C 3) alkylene-0- (Ci-C 3) alkylene- (C 3 -C 6 ) cycloalkyl and (Ci-C 3) alkylene-0- (C 3 -C 6) - cycloalkyl each may be substituted with one or multiple F; q, r independently of one another 0, 1;
R12, R13, R14 are independently H, F, Cl, Br, I, NO 2, CN, 0- (Ci-C 6) - alkyl, (Ci-C 6) -alkyl, (Ci-C 3) alkylene - (C 3 -C 6) cycloalkyl, SO 2 -CH 3, SO 2 -NH 2,
SO 2 -NH (Ci-C 6) -alkyl, SO 2 -N ((Ci-C 6) alkyl) 2, CONH 2, CONH (Ci-C 6) -alkyl, CON ((Ci-C 6) -alkyl) 2, SF 5, (C 6 -C 0) aryl, (C 3 -C 0) cycloalkyl or a 4 to 12 membered heterocycle, wherein the O- (Ci-C6) alkyl which (C1 C6) - alkyl radical, the (Ci-C 3) -alkylene- (C 3 -C 6) cycloalkyl, SO 2 -NH (Ci-C 6) - alkyl, SO 2 -N ((Ci-C 6) -alkyl) 2 group, the ((d-C6) alkyl) 2 radical CONH (Ci-C 6) -alkyl and CON may be respectively singly or multiply substituted by F, and wherein the (C6-Cio ) aryl, the (C 3 -Cio) cycloalkyl and 4 to 12-membered heterocycle each may be a one to 3 times substituted with
F, Cl, Br, I, OH, CF 3, CHF 2, CH 2 F, NO 2, CN, OCF 3, OCHF 2, O- (d-
C 6) alkyl, (Ci-C 6) -alkyl, NH 2, NH (Ci-C 6) -alkyl, N ((Ci-C 6) -alkyl) 2, SO 2 -CH 3, SO 2 - NH 2, SO 2 -NH (Ci-C 6) -alkyl, SO 2 -N ((Ci-C 6) -alkyl) 2, COOH, COO- (Ci-C 6) -alkyl, CONH 2, CONH ( Ci-C 6) alkyl,
CON ((Ci-C 6) alkyl) 2, or SF 5;
A (C 6 -Cio) aryl, (C 3 -C 0) cycloalkyl or a 4 to 12-membered
heterocycle; and their physiologically tolerated salts.
2. Compounds according to claim 1, characterized in that therein R1 represents CH 3;
R2, R3 are independently H, F, Cl, Br, CN, CO- (Ci-C 6) -alkyl, (Ci-C 6) -alkyl or O- (Ci-C 6) -alkyl, where the CO (Ci-C 6) -alkyl (Ci-C 6) -alkyl and O- (d-C6) -alkyl radical can in each case be mono or polysubstituted by F;
R4, R5, R6, R7, R8, R9, R10, R1 1 is independently H, (Ci-C 6) alkyl,
(Ci-C 3) -alkylene- (C 3 -C 6) cycloalkyl, (C 3 -C 6) -cycloalkyl, (C 6 -C 0) aryl), OH, O- (Ci-C 6) alkyl, O- (Ci-C 3) alkylene- (C 6 -C 0) aryl), O- (dC 3) -alkylene- (C 3 - C 6) cycloalkyl, O- (C 3 - C 6) cycloalkyl, (dC 3) -alkylene-OH, (dC 3) -alkylene- O- (Ci-C 6) alkyl, (Ci-C 3) alkylene-O- (Ci-C 3) alkylene- (C 3 -C 6) cycloalkyl, (dC 3) -alkylene-O- (C 3 -C 6) cycloalkyl, wherein said (Ci-C 6) alkyl radical, the (dC 3) - alkylene (C 3 -C 6) cycloalkyl radical, the (C 3 -C 6) -cycloalkyl, the O- (Ci-C 6) - alkyl radical O- (Ci-C 3) alkylene (C 6 -C 0) aryl) radical, the 3 -C 6) cycloalkyl O- (dC 3) -alkylene- (C 3 -C 6) cycloalkyl O- (C, the (dC 3) alkylene- OH radical, the (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, the (dC 3) -alkylene-O- (Ci-C 3) alkylene- (C 3 -C 6) cycloalkyl and (Ci-C 3) -alkylene-O- (C 3 -C 6) - cycloalkyl each may be substituted with one or multiple F; q, r independently of one another 0, 1;
R12, R13, R14 are independently H, F, Cl, Br, I, NO 2, CN, O- (Ci-C 6) -
Alkyl, (Ci-C 6) -alkyl, (Ci-C 3) -alkylene- (C 3 -C 6) cycloalkyl, SO 2 -CH 3, SO 2 -NH 2, SO 2 -NH (Ci-C 6) -alkyl, SO 2 -N ((Ci-C 6) alkyl) 2, CONH 2, CONH (Ci-C 6) -alkyl, CON ((Ci-C 6) -alkyl) 2, SF 5, (C 6 -C 0) aryl, (C 3 -C 0) cycloalkyl or a 4 to 12 membered heterocycle, wherein the O- (d-C6) alkyl, the (Ci-Ce) - alkyl radical ( Ci-C 3) -alkylene- (C 3 -C 6) cycloalkyl, SO 2 -NH (Ci-C 6) - alkyl, SO 2 -N ((Ci-C 6) radical alkyl) 2 the CONH (Ci-C 6) -alkyl and CON ((d-C6) alkyl) 2 radical in each case can be mono or polysubstituted by F and wherein the (C6-Cio) aryl, the (C 3 -Cio) cycloalkyl and 4 to 12-membered heterocycle may be a to 3-fold substituted by F, Cl, Br, I, OH, CF 3, CHF 2, CH 2 F, NO 2, CN, OCF 3, OCHF 2, O- (d- C6) alkyl, (Ci-C 6) -alkyl, NH 2, NH (Ci-C 6) -alkyl, N ((Ci-C 6) -alkyl) 2, SO 2 -CH 3, SO 2 -NH 2, SO 2 -NH (Ci-C 6) -alkyl, SO 2 -N ((Ci-C 6) -alkyl) 2, COOH, COO- (Ci-C 6) -Al alkyl, CONH 2, CONH (Ci-C 6) alkyl,
CON ((Ci-C 6) alkyl) 2, or SF 5;
A (C 6 -Cio) aryl, (C 3 -C 0) cycloalkyl or a 4 to 12-membered
heterocycle; and their physiologically tolerated salts.
3. Compounds according to claim 1 or 2, characterized in that the meanings are
R1 CH 3;
R2, R3 H;
R4, R5 independently of one another H, (d-C6) alkyl;
R6, R7 independently of one another H, (Ci-C 6) -alkyl, (Ci-C 3) -alkylene- (C 3 -C 6) - cycloalkyl, (C 3 -C 6) -cycloalkyl, phenyl, OH, O - (Ci-C 6) -alkyl, O- (Ci-C 3) - alkylene-phenyl, O- (Ci-C 3) -alkylene- (C 3 -C 6) -cycloalkyl, O- (C 3 - C 6) cycloalkyl (Ci-C 3) alkylene-OH; (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, (dC 3) -alkylene-O- (Ci-C 3) alkylene- (C 3 -C 6) cycloalkyl, (C -C 3) -alkylene-O- (C 3 -C 6) cycloalkyl;
R8, R9 independently of one another H, (d-C6) alkyl;
R10, R1 1 is independently H, (d-C6) alkyl; q, r independently of one another 0, 1; R12, R13 independently of one another H, F, Cl, Br, I, CN, O- (Ci-C 6) alkyl, (d-
C 6) alkyl, wherein the O- (Ci-C 6) -alkyl and (Ci-C 6) -alkyl radical may be substituted with F in each case one or more times;
R14 H;
A is phenyl, pyridyl, pyrazinyl; and their physiologically tolerated salts.
4. Compounds according to claim 1 or 2, characterized in that the meanings are
R1 CH 3; R2, R3 H;
R4, R5 independently of one another H, (d-C6) alkyl;
R6, R7 independently of one another H, (Ci-C 6) -alkyl, (Ci-C 3) -alkylene- (C 3 -C 6) - cycloalkyl, (C 3 -C 6) -cycloalkyl, phenyl, OH, O - (Ci-C 6) -alkyl, O- (Ci-C 3) -
Alkylene-phenyl, O- (Ci-C 3) -alkylene- (C 3 -C 6) -cycloalkyl, O- (C 3 -C 6) cycloalkyl, (Ci-C 3) alkylene-OH; (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, (dC 3) -alkylene-O- (Ci-C 3) alkylene- (C 3 -C 6) cycloalkyl, (C -C 3) -alkylene-O- (C 3 -C 6) cycloalkyl; R8, R9 independently of one another H, (d-C6) alkyl;
R10, R1 1 is independently H, (d-C6) alkyl; q, r independently of one another 0, 1;
R12, R13 independently of one another H, F, Cl, Br, I, CN, O- (Ci-C 6) alkyl, (d-
C 6) alkyl, wherein the O- (Ci-C 6) -alkyl and (Ci-C 6) -alkyl radical may be substituted with F in each case one or more times;
R14 H; A is phenyl, pyridyl; and their physiologically tolerated salts.
5. Compounds according to one or more of claims 1 to 3, characterized in that the meanings are
R1 CH 3;
R2, R3 H;
R4, R5 independently of one another H, (d-C6) alkyl; R6, R7 independently of one another H, (Ci-C 6) -alkyl, (Ci-C 3) -alkylene- (C 3 -C 6) - cycloalkyl, (C 3 -C 6) cycloalkyl, phenyl, -OH, O- (Ci-C 6) -alkyl, O- (Ci-C 3) - alkylene-phenyl, (dC 3) -alkylene-OH; (Ci-C 3) alkylene-O- (Ci-C 6) alkyl, (d- C3) alkylene-O- (Ci-C 3) alkylene- (C 3 -C 6) cycloalkyl; R8, R9 independently of one another H, (Ci-C 6) alkyl;
R10, R1 1 is independently H, (d-C6) alkyl; q, r independently of one another 0, 1;
R12, R13 independently of one another H, F, Cl, Br, I, CN, O- (Ci-C 6) alkyl, (d-
C 6) alkyl, wherein the O- (Ci-C 6) -alkyl and (Ci-C 6) -alkyl radical may be substituted with F in each case one or more times;
R14 H;
A is phenyl, 2-pyridyl, 3-pyridyl, 2-pyrazinyl; and their physiologically tolerated salts.
6. Compounds according to one or more of claims 1 to 5, for use as pharmaceuticals.
7. A medicament comprising one or more of the compounds according to one or more of claims 1 to. 5
8. A pharmaceutical composition according to claim 7, characterized in that it
contains at least one further active compound.
9. A pharmaceutical composition according to claim 8, characterized in that it comprises as further active ingredient one or more antidiabetics, hypoglycemic active ingredients, HMGCoA reductase inhibitors, Cholesterinresorptionsinhibitoren, PPAR gamma agonists, PPAR alpha agonists, PPAR alpha / gamma agonists, PPAR delta agonists, fibrates , MTP inhibitors, bile acid, CETP inhibitors, polymeric bile acid adsorbers, LDL receptor inducers, ACAT inhibitors, antioxidants, lipoprotein lipase inhibitors, ATP citrate lyase inhibitors, squalene synthetase inhibitors, lipoprotein (a) antagonists, HM74A receptor agonists, lipase inhibitors, insulins, sulfonylureas, biguanides, meglitinides,
Thiazolidinediones, α-glucosidase inhibitors which act on the ATP-dependent potassium channel of the beta cells agents, glycogen phosphorylase inhibitors, glucagon receptor antagonists, activators of glucokinase, inhibitors of
Gluconeogenesis, inhibitors of fructose-1, 6-bisphosphatase, modulators of glucose transporter 4, inhibitors of glutamine-fructose-6-phosphate amidotransferase, inhibitors of dipeptidylpeptidase IV, inhibitors of 1 1 -beta-hydroxysteroid dehydrogenase-1 inhibitors protein tyrosine phosphatase-1B, modulators of the sodium-dependent glucose transporter 1 or 2, inhibitors of hormone-sensitive lipase, inhibitors of acetyl-CoA carboxylase, inhibitors of phosphoenolpyruvate carboxykinase, inhibitors of glycogen synthase kinase-3 beta, inhibitors of protein kinase C beta, endothelin-A receptor antagonists, inhibitors of I kappaB kinase, modulators of the glucocorticoid receptor, CART agonists, NPY agonists, MC4 agonists, orexin agonists, H3 agonists, TNF agonists, CRF agonists, CRF BP antagonists, urocortin agonists, ß3- agonists, CB1 receptor antagonists, MSH (melanocyte-stimulating hormone) - agonists, CCK agonists, serotonin reuptake Inhibito reindeer, mixed serotonin and noradrenergic compounds, 5HT agonists, bombesin agonists, galanin antagonists, growth hormones, growth hormone-releasing compounds, TRH agonists, decoupling protein 2- or 3 modulators, leptin agonists, DA agonists, lipase / amylase includes inhibitors, PPAR modulators, RXR modulators or TR-.beta.-agonists or amphetamines.
10. A pharmaceutical composition according to claim 8, characterized in that it contains, as further active compound Metformin, Arcabose, glibenclamide, glimepiride, gliclazide, gliquidone, pioglitazone, rosiglitazone, exenatide, Miglitol, Vildagliptin, Sitagliptin, repaglinide, nateglinide or Mitiglinid.
1. 1 A pharmaceutical composition according to claim 8, characterized in that it contains, as further active compound Lixisenatide.
12. Compounds according to one or more of claims 1 to 5 for lowering blood sugar.
13. Compounds according to one or more of claims 1 to 5 for the treatment of diabetes.
14. Compounds according to one or more of claims 1 to 5 for increasing insulin release.
15. A method for producing a medicament comprising one or more of the compounds according to one or more of claims 1 to 5, characterized in that the active ingredient is mixed with a pharmaceutically suitable carrier and bringing this mixture into a form suitable for administration.
16. Set (kit) consisting of separate packs of
a) an effective amount of a compound of formula I according to one or more of claims 1 to 5 and
b) an effective amount of a further medicament active ingredient.
EP20110733622 2010-07-05 2011-07-05 Aryloxy-alkylene substituted hydroxyphenyl hexynoic acids, methods for the production thereof and use of the same as medicament Withdrawn EP2590929A1 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP10305732 2010-07-05
PCT/EP2011/061334 WO2012010413A1 (en) 2010-07-05 2011-07-05 Aryloxy-alkylene substituted hydroxyphenyl hexynoic acids, methods for the production thereof and use of the same as medicament
EP20110733622 EP2590929A1 (en) 2010-07-05 2011-07-05 Aryloxy-alkylene substituted hydroxyphenyl hexynoic acids, methods for the production thereof and use of the same as medicament

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP20110733622 EP2590929A1 (en) 2010-07-05 2011-07-05 Aryloxy-alkylene substituted hydroxyphenyl hexynoic acids, methods for the production thereof and use of the same as medicament

Publications (1)

Publication Number Publication Date
EP2590929A1 true true EP2590929A1 (en) 2013-05-15

Family

ID=43100553

Family Applications (1)

Application Number Title Priority Date Filing Date
EP20110733622 Withdrawn EP2590929A1 (en) 2010-07-05 2011-07-05 Aryloxy-alkylene substituted hydroxyphenyl hexynoic acids, methods for the production thereof and use of the same as medicament

Country Status (7)

Country Link
US (1) US20120004166A1 (en)
EP (1) EP2590929A1 (en)
JP (1) JP2013535410A (en)
KR (1) KR20130095255A (en)
CN (1) CN103080063A (en)
CA (1) CA2804110A1 (en)
WO (1) WO2012010413A1 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2507228B1 (en) 2009-11-30 2014-11-05 Eli Lilly and Company Novel spiropiperidine compounds
EP2590930B1 (en) * 2010-07-05 2015-02-25 Sanofi Spirocyclically substituted 1,3-propane dioxide derivatives, methods for the production thereof and use of the same as medicament
JP2013531000A (en) 2010-07-05 2013-08-01 サノフイ (2-aryloxy - acetylamino) - phenyl - propionic acid derivatives, their use as their preparation and pharmaceutical
CA2878625A1 (en) 2012-07-11 2014-01-16 Elcelyx Therapeutics, Inc. Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk
WO2014064215A1 (en) 2012-10-24 2014-05-01 INSERM (Institut National de la Santé et de la Recherche Médicale) TPL2 KINASE INHIBITORS FOR PREVENTING OR TREATING DIABETES AND FOR PROMOTING β-CELL SURVIVAL
WO2014069555A1 (en) * 2012-11-02 2014-05-08 株式会社成和化成 Propyl-phenyl-ether derivative and melanogenesis inhibitor, skin-lightening agent, antimicrobial agent, and cosmetic containing said propyl-phenyl-ether derivative
EP2963027A4 (en) 2013-02-28 2016-07-20 Sk Chemicals Co Ltd Tricyclic compound and use thereof
WO2014178892A8 (en) * 2013-05-03 2015-12-17 Oregon Health & Science University Use of sobetirome in the treatment of x-linked adrenolenoleukodystrophy
WO2015044379A1 (en) 2013-09-27 2015-04-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A dyrk1a polypeptide for use in preventing or treating metabolic disorders
CN105722841A (en) 2013-11-14 2016-06-29 卡迪拉保健有限公司 Novel Heterocyclic Compounds
EP3259246A1 (en) 2015-02-20 2017-12-27 Oregon Health & Science University Derivatives of sobetirome
EP3273981A1 (en) 2015-03-24 2018-01-31 INSERM - Institut National de la Santé et de la Recherche Médicale Method and pharmaceutical composition for use in the treatment of diabetes

Family Cites Families (982)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3972059A (en) 1973-12-28 1976-07-27 International Business Machines Corporation Dielectric diode, fabrication thereof, and charge store memory therewith
JPS6295494A (en) 1985-10-18 1987-05-01 Westinghouse Electric Corp Device and method of controlling trip of nuclear reactor
WO1997026265A1 (en) 1996-01-17 1997-07-24 Novo Nordisk A/S Fused 1,2,4-thiadiazine and fused 1,4-thiazine derivatives, their preparation and use
CN1190434C (en) 1996-12-31 2005-02-23 雷迪实验室有限公司 Novel heterocyclic compounds and process for its preparation, and pharmaceutical compositions containing them and their use in treatment of diabetes and related diseases
ES2283025T3 (en) 1996-08-30 2007-10-16 Novo Nordisk A/S GLP-1.1.
DE19726167B4 (en) 1997-06-20 2008-01-24 Sanofi-Aventis Deutschland Gmbh Insulin, process for its preparation and pharmaceutical preparation containing
RU2215004C2 (en) 1997-07-16 2003-10-27 Ново Нордиск А/С Condensed derivative of 1,2,4-thiadiazine, pharmaceutical composition and method for preparing medicine
RU2214418C2 (en) 1998-12-07 2003-10-20 Сосьете Де Консей Де Решерш Э Д'Аппликасьон Сьентифик Сас Glp-1 analogs
WO2000064876A1 (en) 1999-04-28 2000-11-02 Aventis Pharma Deutschland Gmbh Tri-aryl acid derivatives as ppar receptor ligands
KR100709498B1 (en) 1999-04-28 2007-04-20 사노피-아벤티스 도이칠란트 게엠베하 Di-aryl acid derivatives as PPAR receptor ligands
EP1194425B1 (en) 1999-06-23 2005-08-10 Aventis Pharma Deutschland GmbH Substituted benzimidazole
DE19929709C2 (en) 1999-06-24 2001-07-12 Lueder Gerking A process for the production of substantially continuous fine filaments and use of the apparatus for performing the method
EP1076066A1 (en) 1999-07-12 2001-02-14 Zealand Pharmaceuticals A/S Peptides for lowering blood glucose levels
EP1214060A2 (en) 1999-09-10 2002-06-19 Novo Nordisk A/S Method of inhibiting protein tyrosine phosphatase 1b and/or t-cell protein tyrosine phosphatase and/or other ptpases with an asp residue at position 48
DE19951360A1 (en) 1999-10-26 2001-05-03 Aventis Pharma Gmbh substituted indoles
CA2393190A1 (en) 1999-12-02 2001-06-07 Glaxo Group Limited Substituted oxazoles and thiazoles derivatives as hppar alpha activators
DE60107248D1 (en) 2000-06-22 2004-12-23 Pfizer New process for production of pyrazolopyrimidonen
EP1315751A2 (en) 2000-08-25 2003-06-04 Novo Nordisk A/S Two receptors of meiosis activating sterols designated sam1a and sam1b
ES2375491T3 (en) 2000-12-21 2012-03-01 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as inhibitors of prote? Na kinases.
RU2316537C2 (en) 2001-04-20 2008-02-10 ЭЙСАЙ Ар энл Ди МЕНЕДЖМЕНТ КО., ЛТД. Derivatives of carboxylic acid, their pharmaceutically acceptable salts or esters, medicinal agent and pharmaceutical composition based on thereof, their using and methods for treatment and prophylaxis of diseases
GB0113233D0 (en) 2001-05-31 2001-07-25 Glaxo Group Ltd Chemical compounds
RU2330846C2 (en) 2001-08-31 2008-08-10 Санофи-Авентис Дойчланд Гмбх Diarylcycloalkyl derivatives, method of their obtaining, and application as ppar-activators
KR20050044577A (en) 2001-11-22 2005-05-12 바이오비트럼 에이비 Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
EP1461327A1 (en) 2001-11-22 2004-09-29 Biovitrum Ab Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
CN1633428A (en) 2001-11-22 2005-06-29 比奥维特罗姆股份公司 Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
US7329683B2 (en) 2002-02-01 2008-02-12 Merck & Co., Inc. 11-β-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
DE60309848T2 (en) 2002-03-05 2007-05-16 Eli Lilly And Co., Indianapolis Purine derivatives as kinase inhibitors
CN1990486A (en) 2002-03-06 2007-07-04 赛诺菲-安万特公司 N-glycyl-pyrrolidine-2-nitrile and its use as DDP-IV enzyme inhibitor
FR2836915B1 (en) 2002-03-11 2008-01-11 Aventis Pharma Sa Aminoindazoles derivatives of, and process for the preparation of intermediates such process is as medicines and pharmaceutical compositions containing them
DE10215907A1 (en) 2002-04-11 2003-11-06 Aventis Pharma Gmbh Acyl-4-carboxyphenyl urea derivatives, processes for their preparation and their use
JPWO2003097064A1 (en) 2002-05-17 2005-09-15 協和醗酵工業株式会社 An agent for treating diabetes
WO2003104208A1 (en) 2002-06-10 2003-12-18 Merck & Co., Inc. 11-beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
DE10226462A1 (en) 2002-06-13 2003-12-24 Aventis Pharma Gmbh Fluorinated cycloalkyl-derivatised benzoylguanidines, processes for their preparation, their use as a medicament, and medicament containing them
EP1517907B1 (en) 2002-06-14 2011-01-12 Sanofi-Aventis Azabicyclo-octane and nonane derivatives with ddp-iv inhibiting activity
DE10231370B4 (en) 2002-07-11 2006-04-06 Sanofi-Aventis Deutschland Gmbh , Pharmaceuticals containing these compounds and processes for preparing these Thiophenglycosidderivate drug
CA2493374A1 (en) 2002-07-12 2004-01-22 Aventis Pharma Deutschland Gmbh Heterocyclically substituted benzoylureas, method for their production and their use as medicaments
KR20050025189A (en) 2002-07-27 2005-03-11 아스트라제네카 아베 Chemical compounds
JP2005534713A (en) 2002-08-07 2005-11-17 三菱ウェルファーマ株式会社 Dihydro pyrazolopyridine compound
DE10237722A1 (en) 2002-08-17 2004-08-19 Aventis Pharma Deutschland Gmbh Indole or benzimidazole derivatives to modulate kinase IkappaB
DE10237723A1 (en) 2002-08-17 2004-07-08 Aventis Pharma Deutschland Gmbh Use of IkappaB kinase inhibitors in the treatment of pain
JP4648703B2 (en) 2002-09-05 2011-03-09 アベンティス・ファーマ・ソシエテ・アノニム Novel aminoindazole derivatives and pharmaceutical compositions containing them as medicaments
CN100577660C (en) 2002-09-12 2010-01-06 霍夫曼-拉罗奇有限公司 N-substituted-1H-indol-5-propionic acid compounds as PPAR agonists used for the treatment of diabetes
WO2004033427A1 (en) 2002-10-11 2004-04-22 Astrazeneca Ab 1,4-disubstituted piperidine derivatives and their use as 11-betahsd1 inhibitors
JP4352001B2 (en) 2002-10-18 2009-10-28 メルク エンド カムパニー インコーポレーテッドMerck & Company Incoporated Beta for treatment or prevention of diabetes - amino heterocyclic dipeptidyl peptidase inhibitors
JP2006514614A (en) 2002-10-24 2006-05-11 ステリックス リミテッド 11β- hydroxysteroid dehydrogenase type 1 and type 2 inhibitor
WO2004041274A1 (en) 2002-11-05 2004-05-21 Arena Pharmaceuticals, Inc. Benzotriazoles and methods of prophylaxis or treatment of metabolic-related disorders thereof
JP2006514102A (en) 2002-11-07 2006-04-27 アストラゼネカ アクチボラグ 2-oxo - ethanesulfonamide derivatives
FR2847253B1 (en) 2002-11-19 2007-05-18 Aventis Pharma Sa New derivatives of pyridazinone was as medicines and pharmaceutical compositions containing them
WO2004050658A1 (en) 2002-12-03 2004-06-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Novel substituted imidazo-pyridinones and imidazo-pyridazeiones, the production and use thereof as medicaments
DE10258007B4 (en) 2002-12-12 2006-02-09 Sanofi-Aventis Deutschland Gmbh Aromatic Fluorglycosidderivate, containing these compounds, pharmaceutical compositions and methods for producing these drug
DE10258008B4 (en) 2002-12-12 2006-02-02 Sanofi-Aventis Deutschland Gmbh , Pharmaceuticals containing these compounds and methods for preparing heterocyclic Fluorglycosidderivate these drugs
DE60316841T2 (en) 2002-12-20 2008-07-17 Merck & Co., Inc. Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
WO2004056744A1 (en) 2002-12-23 2004-07-08 Janssen Pharmaceutica N.V. Adamantyl acetamides as hydroxysteroid dehydrogenase inhibitors
CA2509086C (en) 2003-01-06 2012-08-21 Eli Lilly And Company Substituted arylcyclopropylacetamides as glucokinase activators
JP2006516572A (en) 2003-01-14 2006-07-06 アリーナ ファーマシューティカルズ, インコーポレイテッド Prevention and treatment of disorders such as 1,2,3-trisubstituted aryl derivatives as metabolic modulators and 1,2,3 substituted heteroaryl derivatives and diabetes and hyperglycemia associated with these derivatives
JP2006517199A (en) 2003-01-24 2006-07-20 ノバルティス アクチエンゲゼルシャフト Amide derivatives and their 11-beta - use as inhibitors of hydroxysteroid dehydrogenase type 1
JP4757188B2 (en) 2003-02-11 2011-08-24 プロシディオン・リミテッドProsidion Limited Tri (cyclo) substituted amide compounds
WO2004072066A1 (en) 2003-02-11 2004-08-26 Prosidion Limited Tri(cyclo) substituted amide glucokinase activator compounds
KR100728425B1 (en) 2003-02-19 2007-06-13 에프. 호프만-라 로슈 아게 Sulfonamide substituted xanthine derivatives for use as pepck inhibitors
EP1460075A1 (en) 2003-03-21 2004-09-22 Sanofi-Synthélabo Substituted 8-Pyridinyl-6,7,8,9-Tetrahydropyrimido[1,2-a]Pyrimidin-4-one and 8-Phenyl-6-7,8,9-Tetrahydropyrimido[1,2-a]Pyrimidin-4-one derivatives
EP2239012A3 (en) 2003-04-11 2011-06-15 High Point Pharmaceuticals, LLC Substituted amide derivatives and pharmaceutical uses thereof
EP1615647B1 (en) 2003-04-11 2010-01-20 High Point Pharmaceuticals, LLC Pharmaceutical use of fused 1,2,4-triazoles
JP2006522745A (en) 2003-04-11 2006-10-05 ノボ ノルディスク アクティーゼルスカブNovo Nordisk Aktie Selsxab Pharmaceutical use of substituted 1,2,4-triazole
JP2006528687A (en) 2003-05-09 2006-12-21 メルク エンド カムパニー インコーポレーテッドMerck & Company Incoporated Compositions and methods of use comprising benzimidazole, such compounds
US7067529B2 (en) 2003-05-19 2006-06-27 Hoffmann-La Roche Inc. Glutamine fructose-y-phosphate amidotransferase (GFAT) inhibitors
US7090355B2 (en) 2003-05-19 2006-08-15 Superimaging, Inc. System and method for a transparent color image display utilizing fluorescence conversion of nano particles and molecules
EP1631558A1 (en) 2003-05-21 2006-03-08 Biovitrum Ab Inhibitors of 11-beta-hydroxy steroid dehydrogenase type i
CN1795181A (en) 2003-05-29 2006-06-28 麦克公司 Triazole derivatives as inhibitors of 11-beta hydroxysteroid dehydrogenase-1
WO2004106343A3 (en) 2003-05-30 2005-03-24 Mathias M Domostoj Agelastatin derivatives of antitumour and gsk-3beta-inhibiting alkaloids
JP2004359630A (en) 2003-06-06 2004-12-24 Kotobuki Seiyaku Kk Difluorodiphenylmethane derivative and its salt
WO2005000836A1 (en) 2003-06-13 2005-01-06 Janssen Pharmaceutica N.V. Substituted indazolyl(indolyl)maleimide derivatives as kinase inhibitors
CA2529406A1 (en) 2003-06-25 2004-12-29 Biovitrum Ab New use i
WO2004112779A1 (en) 2003-06-25 2004-12-29 Biovitrum Ab New use vii
WO2004113310A1 (en) 2003-06-25 2004-12-29 Biovitrum Ab Use of an inhibitor of 11-b-hydroxysteroid dehydrogenase type 1 compounds for promoting wound healing
WO2004112782A1 (en) 2003-06-25 2004-12-29 Biovitrum Ab New use v
EP1644411A2 (en) 2003-07-11 2006-04-12 Novo Nordisk A/S Stabilised insulin compositions
CA2534267A1 (en) 2003-07-25 2005-02-10 Sanofi-Aventis Deutschland Gmbh Novel cyanopyrrolidides, methods for the production thereof, and use of the same as medicaments
DE10333935A1 (en) 2003-07-25 2005-02-24 Aventis Pharma Deutschland Gmbh New bicyclic Cyanoheterocyclen, processes for their preparation and their use as medicaments
DE10334309A1 (en) 2003-07-28 2005-03-03 Aventis Pharma Deutschland Gmbh Substituted thiazol-Benzoisothiazoldioxidderivate, processes for their preparation and their use
US20050026984A1 (en) 2003-07-29 2005-02-03 Aventis Pharma S.A. Substituted thieno [2,3-c] pyrazoles and their use as medicinal products
US7008953B2 (en) 2003-07-30 2006-03-07 Agouron Pharmaceuticals, Inc. 3, 5 Disubstituted indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
JP5225679B2 (en) 2005-01-31 2013-07-03 田辺三菱製薬株式会社 Indole derivatives
JP2007501789A (en) 2003-08-07 2007-02-01 メルク エンド カムパニー インコーポレーテッドMerck & Company Incoporated 11-beta-pyrazolecarboxamide as inhibitors of hydroxysteroid dehydrogenases -1
WO2005027978A3 (en) 2003-09-19 2005-05-19 Novo Nordisk As Albumin-binding derivatives of therapeutic peptides
WO2005037828A1 (en) 2003-10-20 2005-04-28 Lg Life Sciences Ltd. Novel inhibitors of dpp-iv, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent
GB0325402D0 (en) 2003-10-31 2003-12-03 Astrazeneca Ab Compounds
US8008525B2 (en) 2003-11-26 2011-08-30 Takeda Pharmaceutical Company Limited Receptor function regulating agent
DE10359098A1 (en) 2003-12-17 2005-07-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg New 2- (piperazin-1-yl) - and 2 - ([1,4] diazepan-1-yl) imidazo [4,5-d] pyridazin-4-ones, their preparation and their use as medicaments
EP1557417B1 (en) 2003-12-19 2007-03-07 Sanofi-Aventis Substituted 8'-pyri(mi)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-a] pyrimidin-6-one derivatives
JP2007514794A (en) 2003-12-19 2007-06-07 メルク エンド カムパニー インコーポレーテッドMerck & Company Incoporated Cyclic guanidines, compositions comprising such compounds, and methods of use
EP1703908A4 (en) 2003-12-22 2009-07-08 Amgen Inc Aryl sulfonamide compounds and uses related thereto
WO2005061489A1 (en) 2003-12-24 2005-07-07 Prosidion Limited Heterocyclic derivatives as gpcr receptor agonists
EP1711184B1 (en) 2004-01-06 2007-07-18 Janssen Pharmaceutica N.V. (3-oxo-3,4-dihydro-quinoxalin-2-yl-amino)-benzamide derivatives and related compounds as glycogen phosphorylase inhibitors for the treatment of diabetes and obesity
CA2554522A1 (en) 2004-01-31 2005-08-11 Sanofi-Aventis Deutschland Gmbh 7-phenylamino-4-quinolone-3-carboxylic acid derivatives, methods for production and use thereof as medicaments
DE102004005172A1 (en) 2004-02-02 2005-08-18 Aventis Pharma Deutschland Gmbh Indazole derivatives as inhibitors of hormone-sensitive lipase
CA2554686A1 (en) 2004-02-18 2005-09-01 Astrazeneca Ab Compounds
ES2433466T3 (en) * 2004-02-27 2013-12-11 Amgen, Inc Compounds, pharmaceutical compositions and methods for use in treating metabolic disorders
DE102004010194A1 (en) 2004-03-02 2005-10-13 Aventis Pharma Deutschland Gmbh 4-benzimidazole-2-yl-pyridazin-3-one derivatives, their preparation and use in medicaments
JP4950657B2 (en) 2004-03-04 2012-06-13 キッセイ薬品工業株式会社 Fused heterocyclic derivatives, pharmaceutical compositions containing them and their pharmaceutical use
WO2005086904A3 (en) 2004-03-08 2005-11-24 Amgen Inc Therapeutic modulation of ppar (gamma) activity
DE102004012068A1 (en) 2004-03-12 2005-09-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg New alkyl-containing 5-Acylindolinone, their preparation and their use as medicaments
CN1938286A (en) 2004-03-29 2007-03-28 默克公司 Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
EP1586318A1 (en) 2004-04-05 2005-10-19 Neuropharma S.A.U. Thiadiazolidinones as GSK-3 inhibitors
US7608627B2 (en) 2004-04-05 2009-10-27 Takeda Pharmaceutical Company Limited 6-azaindole compound
US20070202179A1 (en) 2004-04-09 2007-08-30 FAULKNER Patrick Low Dose Pharmaceutical Products
RU2006143758A (en) 2004-05-12 2008-06-27 Авентис Фармасьютикалз Инк. (Us) By substantially pure 2 - {[2- (2-methylaminopyrimidin-4-yl) -1H-indole-5-carbonyl] -amino} -3- (phenylpyridine-2-ylamino) -propionic acid as an inhibitor of kinase 1Q
EP1604988A1 (en) 2004-05-18 2005-12-14 Sanofi-Aventis Deutschland GmbH Pyridazinone derivatives, methods for producing them and their use as pharmaceuticals
DE102004026532A1 (en) 2004-05-29 2006-01-05 Sanofi-Aventis Deutschland Gmbh Substituted oxazole Benzoisothiazoldioxidderivate, processes for their preparation and their use
DE102004028241B4 (en) 2004-06-11 2007-09-13 Sanofi-Aventis Deutschland Gmbh New fluoroglycoside pyrazoles, pharmaceutical compositions containing these compounds and manufacture of these drugs
WO2006012227A3 (en) 2004-06-24 2006-05-04 Chunhong He Amido compounds and their use as pharmaceuticals
JP2008504274A (en) 2004-06-24 2008-02-14 インサイト・コーポレイションIncyte Corporation Use as amide compounds and their pharmaceutically
DE102004034697A1 (en) 2004-07-17 2006-02-09 Sanofi-Aventis Deutschland Gmbh substituted diphenylamine or diphenylamine Salicylthiazole, processes for their preparation and their use
KR100926842B1 (en) 2004-07-28 2009-11-13 에프. 호프만-라 로슈 아게 Aryl-pyridine derivatives as 11-beta-hsd1 inhibitors
DE102004037554A1 (en) 2004-08-03 2006-03-16 Sanofi-Aventis Deutschland Gmbh Substituted 8-aminoalkylthio-xanthine, processes for their preparation and their use as medicaments
JP2008509146A (en) 2004-08-06 2008-03-27 メルク エンド カムパニー インコーポレーテッドMerck & Company Incoporated 11-beta - sulfonyl compounds as inhibitors of hydroxysteroid dehydrogenases -1
DE102004038269A1 (en) 2004-08-06 2006-03-16 Sanofi-Aventis Deutschland Gmbh Substituted bicyclic 8-piperidino xanthine, processes for their preparation and their use as medicaments
DE102004038270A1 (en) 2004-08-06 2006-03-16 Sanofi-Aventis Deutschland Gmbh Substituted bicyclic 8-amino-xanthine, processes for their preparation and their use as medicaments
DE102004038268A1 (en) 2004-08-06 2006-03-16 Sanofi-Aventis Deutschland Gmbh Substituted bicyclic 8-pyrrolidino-xanthine, processes for their preparation and their use as medicaments
WO2006018150A8 (en) 2004-08-11 2006-04-20 Boehringer Ingelheim Int D-xylopyranosyl-phenyl-substituited cyclene, medicaments containing said compounds, use thereof and method for the production thereof
EP1789396A1 (en) 2004-08-12 2007-05-30 Prosidion Limited Substituted phenylacetamides and their use as glucokinase activators
DE102004039507A1 (en) 2004-08-14 2006-03-02 Sanofi-Aventis Deutschland Gmbh Substituted 8-Aminoalkoxi-xanthine, processes for their preparation and their use as medicaments
RU2007102288A (en) 2004-08-18 2008-09-27 Мебабазис Терапеутикс, Инк. (Us) New thiazole inhibitors of fructose-1,6-bisphosphatase
CA2576839C (en) 2004-08-30 2013-07-02 Janssen Pharmaceutica N.V. N-2 adamantanyl-2-phenoxy-acetamide derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
CN101018790A (en) 2004-09-11 2007-08-15 塞诺菲-安万特德国有限公司 7-azaindoles and their use as PPAR agonists
ES2317305T3 (en) 2004-09-29 2009-04-16 F. Hoffmann-La Roche Ag Indazolona derivatives as inhibitors of 11b-HSD1.
WO2006035796A1 (en) 2004-09-29 2006-04-06 Kissei Pharmaceutical Co., Ltd. 1-(β-D-GLYCOPYRANOSYL)-3-SUBSTITUTED NITROGENOUS HETEROCYCLIC COMPOUND, MEDICINAL COMPOSITION CONTAINING THE SAME, AND MEDICINAL USE THEREOF
CN101031300A (en) 2004-10-01 2007-09-05 默克公司 Aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2006037811A3 (en) 2004-10-07 2006-12-07 Thomas Kruse Hansen Protracted exendin-4 compounds
WO2006037810A3 (en) 2004-10-07 2006-09-08 Thomas Kruse Hansen Protracted glp-1 compounds
US8138342B2 (en) 2004-10-12 2012-03-20 High Point Pharmacueticals, LLC 11β-hydroxysteroid dehydrogenase type 1 active spiro compounds
CA2584904A1 (en) 2004-10-22 2006-05-04 Smithkline Beecham Corporation Xanthine derivatives with hm74a receptor activity
WO2006045564A1 (en) 2004-10-22 2006-05-04 Smithkline Beecham Corporation Xanthine derivatives with hm74a receptor activity
EP1807072B1 (en) 2004-10-29 2009-01-07 Eli Lilly And Company Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
JP2008518903A (en) 2004-11-02 2008-06-05 ファイザー・インク The novel compounds of substituted and unsubstituted adamantyl amide
EP1666467A1 (en) 2004-11-08 2006-06-07 Evotec AG 11Beta-HSD1 Inhibitors
EP1659113A1 (en) 2004-11-08 2006-05-24 Evotec AG Inhibitors of 11beta-hydroxy steroid dehydrogenase type 1 (11beta-HSD1)
WO2006051662A1 (en) 2004-11-09 2006-05-18 Taisho Pharmaceutical Co., Ltd. Thiazole derivative
JP2006160733A (en) 2004-11-15 2006-06-22 Taisho Pharmaceut Co Ltd Medicine containing cyanofluoropyrrolidine derivative as active ingredient
CA2587800C (en) 2004-11-29 2012-06-12 Merck & Co., Inc. Fused aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2006059744A1 (en) 2004-11-30 2006-06-08 Nippon Chemiphar Co., Ltd. ACTIVATOR OF PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR δ
DE102004058449A1 (en) 2004-12-03 2006-06-14 Merck Patent Gmbh tetrahydropyran
KR101066882B1 (en) 2004-12-03 2011-09-26 트랜스테크 파르마, 인크. Heteroaromatic glucokinase activators
JP2008007405A (en) 2004-12-07 2008-01-17 Takeda Chem Ind Ltd Carboxamide derivative
WO2006065826A3 (en) 2004-12-15 2006-10-05 Joseph D Armstrong Iii Process to chiral beta amino acid derivatives by asymmetric hydrogenation
DE102004060542A1 (en) 2004-12-16 2006-07-06 Sanofi-Aventis Deutschland Gmbh Hydroxybiphenyl-carboxylic acids and derivatives, processes for their preparation and their use
WO2006066109A3 (en) 2004-12-17 2009-04-23 Nancy K Brennan Hydroxysteroid dehydrogenase inhibitors
EP1831178A2 (en) 2004-12-23 2007-09-12 Arena Pharmaceuticals, Inc. Fused pyrazole derivatives and uses thereof in methods of treatment of metabolic-related disorders
WO2006068163A1 (en) 2004-12-24 2006-06-29 Dainippon Sumitomo Pharma Co., Ltd. Bicyclic pyrrole derivatives
JP5065908B2 (en) 2004-12-24 2012-11-07 プロシディオン・リミテッドProsidion Limited G-protein coupled receptor agonists
KR20070091038A (en) 2004-12-24 2007-09-06 프로시디온 리미티드 G-protein coupled receptor(gpr116) agonists and use thereof for treating obesity and diabetes
US7635699B2 (en) 2004-12-29 2009-12-22 Bristol-Myers Squibb Company Azolopyrimidine-based inhibitors of dipeptidyl peptidase IV and methods
EP1846363B1 (en) 2005-01-05 2012-04-25 Abbott Laboratories Adamantyl derivatives as inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
DE102005001053A1 (en) 2005-01-07 2006-07-20 Merck Patent Gmbh Square acid derivatives
CA2592995C (en) 2005-01-07 2012-07-10 Hiroyuki Kakinuma 1-thio-d-glucitol derivatives
WO2006073167A1 (en) 2005-01-07 2006-07-13 Ono Pharmaceutical Co., Ltd. Pyrrolidine derivatives
DK1911756T3 (en) 2005-01-10 2010-02-08 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
DE102005002130A1 (en) 2005-01-17 2006-07-27 Sanofi-Aventis Deutschland Gmbh New substituted aminomethylene sulfonamides useful as hormone sensitive lipase inhibitors in medicaments for treatment and/or prevention of non-insulin dependent diabetes mellitus, diabetic syndrome or obesity
US7956061B2 (en) 2005-01-19 2011-06-07 Merck Sharp & Dohme Corp. Bicyclic pyrimidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
JP2008100916A (en) 2005-01-24 2008-05-01 Dainippon Sumitomo Pharma Co Ltd Indoles and pharmaceutical formulation containing the same
KR100929069B1 (en) 2005-02-03 2009-11-30 아이알엠 엘엘씨 The compounds and compositions as modulators Ppar
WO2006085685A1 (en) 2005-02-09 2006-08-17 Takeda Pharmaceutical Company Limited Pyrazole compound
EP1856090B1 (en) 2005-02-11 2009-10-14 Eli Lilly And Company Substituted thiophene derivatives as glucagon receptor antagonists, preparation and therapeutic uses
GB0503053D0 (en) 2005-02-14 2005-03-23 Smithkline Beecham Corp Chemical compounds
US20080221108A1 (en) 2005-02-14 2008-09-11 Richard Hatley Anthranilic Acid Derivatives As Hm74A Receptor Agonists
GB0503056D0 (en) 2005-02-14 2005-03-23 Smithkline Beecham Corp Chemical compounds
JP2008530174A (en) 2005-02-15 2008-08-07 ノボ ノルディスク アクティーゼルスカブNovo Nordisk Aktie Selsxab 3,4-dihydro -1h- isoquinoline-2-carboxylic acid 5-aminopyridin-2-yl ester
WO2006087997A1 (en) 2005-02-15 2006-08-24 Kissei Pharmaceutical Co., Ltd. 1-SUBSTITUTED-7-(β-D-GLYCOPYRANOSYLOXY)(AZA)INDOLE COMPOUND AND PHARMACEUTICAL CONTAINING THE SAME
CA2598934A1 (en) 2005-02-25 2006-08-31 Takeda Pharmaceutical Company Limited Pyridyl acetic acid compounds
JP4632817B2 (en) 2005-03-09 2011-02-23 株式会社リコー The lens barrel, a camera, a portable information terminal and the image input device
US20060203661A1 (en) 2005-03-11 2006-09-14 Ulead Systems,Inc. Rewritable media and management methods thereof
DE102005012873B4 (en) 2005-03-19 2007-05-03 Sanofi-Aventis Deutschland Gmbh Aminocarbonyl substituted 8-N-benzimidazoles, process for their preparation and their use as medicaments
DE102005012874A1 (en) 2005-03-19 2006-09-21 Sanofi-Aventis Deutschland Gmbh Amide substituted 8-N-benzimidazoles, process for their preparation and their use as medicaments
WO2006104030A1 (en) 2005-03-25 2006-10-05 Daiichi Sankyo Company, Limited Thiazole compound
CA2602248C (en) 2005-04-01 2011-06-28 Lg Life Sciences Ltd. Dipeptidyl peptidase-iv inhibiting compounds, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent
WO2006106423A8 (en) 2005-04-07 2007-11-08 Hengmiao Cheng Amino sulfonyl derivatives as inhibitors of human 11-.beta.-hydrosysteroid dehydrogenase
CA2603757A1 (en) 2005-04-13 2006-10-26 Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment
EP1874787B1 (en) 2005-04-15 2009-12-30 Boehringer Ingelheim International GmbH Glucopyranosyl-substituted (heteroaryloxy-benzyl)-benzene derivatives as sglt inhibitors
DE102005017605B4 (en) 2005-04-16 2007-03-15 Sanofi-Aventis Deutschland Gmbh Substituted 2-aminoalkylthio-benzimidazoles, process for their preparation and their use as medicaments
DE102005018389A1 (en) 2005-04-20 2006-10-26 Sanofi-Aventis Deutschland Gmbh Azole derivatives as inhibitors of lipases, and phospholipases
EP1873144B1 (en) 2005-04-20 2014-07-23 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
EP1883419A4 (en) 2005-05-06 2010-08-04 Bayer Pharmaceuticals Corp Glucagon-like peptide 1 (glp-1) receptor agonists and their pharmacological methods of use
ES2350852T3 (en) 2005-05-13 2011-01-27 Eli Lilly And Company glp-1 pegylated compounds.
EP1885726B1 (en) 2005-05-17 2016-12-14 Merck Sharp & Dohme Corp. Ortho-condensed 2-pyridinone derivatives as nicotinic acid receptor agonists for the treatment of dyslipidemia
EP1888066B1 (en) 2005-05-25 2012-01-11 Merck Sharp & Dohme Corp. Aminocyclohexanes as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
EP1891058A1 (en) 2005-05-27 2008-02-27 AstraZeneca AB Heteroaryl benzamide derivatives for use as glk activators in the treatment of diabetes
WO2006132436A1 (en) 2005-06-08 2006-12-14 Japan Tobacco Inc. Heterocyclic compound
US7579360B2 (en) 2005-06-09 2009-08-25 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
EP1893609B1 (en) 2005-06-16 2009-11-18 Pfizer, Inc. N-(pyridin-2-yl)-sulfonamide derivatives
WO2006134481A1 (en) 2005-06-16 2006-12-21 Pfizer Inc. Inhibitors of 11-beta hydroxysteroid dehydrogenase type 1
US7605289B2 (en) 2005-06-17 2009-10-20 Amgen, Inc. Benzamide derivatives and uses related thereto
WO2006133926A1 (en) 2005-06-17 2006-12-21 Carex Sa Pyrazole derivates as cannabinoid receptor modulators
US7572808B2 (en) 2005-06-17 2009-08-11 Bristol-Myers Squibb Company Triazolopyridine cannabinoid receptor 1 antagonists
CN101203502A (en) 2005-06-22 2008-06-18 霍夫曼-拉罗奇有限公司 ( 6-flu0r0-benz0[l, 3] dioxolyl) -morpholin-4-yl-methanones and their use as cbl ligands
EP1901731B1 (en) 2005-06-28 2011-03-02 Merck Sharp & Dohme Corp. Niacin receptor agonists, compositions containing such compounds and methods of treatment
WO2007000006A3 (en) 2005-06-29 2007-10-18 Plansee Se Halogen filament lamp comprising a dimming cover consisting of an mo alloy
WO2007000445A1 (en) 2005-06-29 2007-01-04 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituted benzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
JP5114395B2 (en) 2005-06-30 2013-01-09 プロシディオン・リミテッドProsidion Limited Gpcr agonist
CA2613236A1 (en) 2005-06-30 2007-01-11 Prosidion Limited G-protein coupled receptor agonists
JP4787321B2 (en) 2005-07-05 2011-10-05 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Pyridazine derivative
JP2009500377A (en) 2005-07-08 2009-01-08 ノボ・ノルデイスク・エー/エス Dicycloalkyl urea-type glucokinase activators
WO2007007688A1 (en) 2005-07-08 2007-01-18 Mochida Pharmaceutical Co., Ltd. 3,5-diamino-1,2,4-triazole derivative
EP1910350A1 (en) 2005-07-09 2008-04-16 AstraZeneca AB 2 -heterocyclyloxybenzoyl amino heterocyclyl compounds as modulators of glucokinase for the treatment of type 2 diabetes
JP4033409B1 (en) 2005-07-11 2008-01-16 田辺三菱製薬株式会社 Oxime derivatives and their preparation
JP5281287B2 (en) 2005-07-13 2013-09-04 Msd株式会社 Heterocyclic-substituted benzimidazole derivatives
WO2007006814A1 (en) 2005-07-14 2007-01-18 Novo Nordisk A/S Urea glucokinase activators
EP1912946B1 (en) 2005-07-20 2009-05-27 Eli Lilly And Company Pyridine derivatives as dipeptedyl peptidase inhibitors
EP1910359B1 (en) 2005-07-21 2009-11-18 F. Hoffmann-Roche AG PYRIDO [2 , 3-D]PYRIMIDINE-2 , 4-DIAMINE COMPOUNDS AS PTPlB INHIBITORS
WO2007015744A1 (en) 2005-07-21 2007-02-08 Incyte Corporation Disubstituted thienyl compounds and their use as pharmaceuticals
EP1912656A2 (en) 2005-07-28 2008-04-23 Boehringer Ingelheim International GmbH Methods for preventing and treating metabolic disorders and new pyrazole-o-glycoside derivatives
JP5084503B2 (en) 2005-07-29 2012-11-28 武田薬品工業株式会社 Cyclopropanecarboxylic acid compound
FR2889190A1 (en) 2005-08-01 2007-02-02 Merck Sante Soc Par Actions Si New imidazole carboxamides, useful to treat e.g. pathologies associated with the insulin resistance syndrome, are fructose-1,6-biphosphatase inhibitors
ES2267400B1 (en) 2005-08-04 2008-03-01 Universitat De Valencia pigment compositions in aqueous base for polychromatic marking laser inorganic materials.
US20100160286A1 (en) 2005-08-09 2010-06-24 Astrazeneca Uk Limited Ab Heteroarylcarbamoylbenzene derivatives for the treatment of diabetes
GB0516462D0 (en) 2005-08-10 2005-09-14 Smithkline Beecham Corp Novel compounds
US20100179128A1 (en) 2005-08-10 2010-07-15 Richard Jonathan Daniel Hatley Xanthine derivatives as selective hm74a agonists
WO2007024993A3 (en) 2005-08-26 2007-10-11 Jason M Cox Fused aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
CA2620570A1 (en) 2005-08-29 2007-03-08 Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment
CA2621227A1 (en) 2005-08-31 2007-03-08 Astellas Pharma Inc. Thiazole derivative
JP2007063225A (en) 2005-09-01 2007-03-15 Takeda Chem Ind Ltd Imidazopyridine compound
WO2007028145A3 (en) 2005-09-02 2007-10-11 Dara Biosciences Inc Agents and methods for reducing protein tyrosine phosphatase 1b activity in the central nervous system
US20080300251A1 (en) 2005-09-05 2008-12-04 Sattigeri Jitendra A Derivatives of 3-Azabicyclo[3.1.0] Hexane as Dipeptidyl Peptidase-IV Inhibitors
GB0518361D0 (en) 2005-09-08 2005-10-19 Univ Edinburgh Therapeutic compounds
US20070264331A1 (en) 2005-09-08 2007-11-15 Laboratorios Silanes, S.A De C.V. Stable pharmaceutical composition of immediate-release glimepiride and extended-release metformin
CA2621949A1 (en) 2005-09-14 2007-03-22 Amgen Inc. Conformationally constrained 3- (4-hydroxy-phenyl) - substituted-propanoic acids useful for treating metabolic disorders
EP1928874A1 (en) 2005-09-16 2008-06-11 AstraZeneca AB Heterobicyclic compounds as glucokinase activators
ES2326391T3 (en) 2005-09-16 2009-10-08 Arena Pharmaceuticals, Inc. Modulators of metabolism and treatment of disorders related thereto.
JP2009508963A (en) 2005-09-21 2009-03-05 インサイト・コーポレイションIncyte Corporation Its use as amide compounds and pharmaceutical compositions
KR20080048494A (en) 2005-09-29 2008-06-02 사노피-아벤티스 Phenyl-[1,2,4]-oxadiazol-5-one derivatives with phenyl group, processes for their preparation and their use as pharmaceuticals
EP2298779A1 (en) 2005-09-30 2011-03-23 Novartis AG Sulfonamide derivatives as glycokinase activators useful in the treatment of type 2 diabetes
CA2623686A1 (en) 2005-09-30 2007-04-12 Novartis Ag 3-cyclyl-2- (4-sulfamo yl-phenyl) -n-cyclyl-propionamide derivatives useful in the treatment of impaired glucose tolerance and diabetes
WO2007037534A9 (en) 2005-09-30 2007-05-31 Banyu Pharma Co Ltd 2-heteroaryl-substituted indole derivative
DE102005048897A1 (en) 2005-10-12 2007-04-19 Sanofi-Aventis Deutschland Gmbh Diacylindazol derivatives as inhibitors of lipases and phospholipases
WO2007047177A1 (en) 2005-10-13 2007-04-26 Merck & Co., Inc. Acyl indoles, compositions containing such compounds and methods of use
JP2009013065A (en) 2005-10-14 2009-01-22 Astellas Pharma Inc Condensed heterocyclic compound
WO2007047625A3 (en) 2005-10-20 2007-10-11 Merck & Co Inc Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
JP5137207B2 (en) 2005-11-01 2013-02-06 アレイ バイオファーマ、インコーポレイテッド Glucokinase activators
EP1960386A2 (en) 2005-11-01 2008-08-27 Janssen Pharmaceutica N.V. Substituted cycloalkylpyrrolones as allosteric modulators of glucokinase
WO2007051811A3 (en) 2005-11-01 2008-01-24 Henrik Sune Andersen Pharmaceutical use of substituted amides
US20090124598A1 (en) 2005-11-01 2009-05-14 Henrik Sune Andersen Pharmaceutical use of substituted amides
US20080293741A1 (en) 2005-11-03 2008-11-27 Matthew Colin Thor Fyfe Tricyclo Substituted Amides as Glucokinase Modulators
JP2009514836A (en) 2005-11-03 2009-04-09 プロシディオン・リミテッドProsidion Limited Tricyclo substituted amides
JP2009514835A (en) 2005-11-03 2009-04-09 プロシディオン・リミテッドProsidion Limited Tricyclo substituted amides
EP1948152B1 (en) 2005-11-09 2013-01-02 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
DK1951661T3 (en) 2005-11-17 2012-09-03 Lilly Co Eli Glucagon receptor antagonists, the preparation and therapeutic uses thereof
EP1951658B1 (en) 2005-11-17 2012-09-26 Eli Lilly & Company Glucagon receptor antagonists, preparation and therapeutic uses
EP1948614A2 (en) 2005-11-18 2008-07-30 Takeda San Diego, Inc. Glucokinase activators
WO2007057768A3 (en) 2005-11-18 2007-11-01 Hengmiao Cheng Sulfonyl derivatives
CN101312951A (en) 2005-11-21 2008-11-26 盐野义制药株式会社 Heterocyclic compound possessing ó± type 11 beta-hydroxy steroid dehydrogenase inhibiting activity
ES2516691T3 (en) 2005-11-22 2014-10-31 Eli Lilly & Company Glucagon receptor antagonists, preparation and therapeutic uses
JP5204662B2 (en) 2005-11-22 2013-06-05 アムジエン・インコーポレーテツド 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors
US7807702B2 (en) 2005-11-23 2010-10-05 Eli Lilly And Company Substituted thiophene carboxylic amide glucagon receptor antagonists, preparation and therapeutic uses
WO2007060992A1 (en) 2005-11-25 2007-05-31 Kaneka Corporation Agent for preventing or improving metabolic syndrome or insulin-resistance syndrome
WO2007063928A1 (en) 2005-11-30 2007-06-07 Toray Industries, Inc. Novel noncyclic amine carboxamide derivative and salt thereof
CN1978445B (en) 2005-12-02 2010-09-01 中国科学院上海药物研究所 Compound serving as human-derived adenoside mononucleoside activated protein kinase activator, and its preparing method and use
JP2009519933A (en) 2005-12-14 2009-05-21 アムゲン インコーポレイティッド Diaza heterocyclic sulfonamide derivatives and methods for their use
US7943615B2 (en) 2005-12-14 2011-05-17 Merck Sharp & Dohme Corp. Fused aminopiperidines as dipeptidyl peptidase-4 inhibitors for the treatment or prevention of diabetes
EP1801098A1 (en) 2005-12-16 2007-06-27 Merck Sante 2-Adamantylurea derivatives as selective 11B-HSD1 inhibitors
KR20150003157A (en) 2005-12-19 2015-01-08 트러스티즈 오브 터프츠 칼리지 Soft protease inhibitors and pro-soft forms thereof
WO2007075847A3 (en) 2005-12-20 2007-10-04 Jun Feng Glucokinase activators
EP1966193B1 (en) 2005-12-21 2010-09-29 F. Hoffmann-La Roche AG New salt and polymorph of dpp-iv inhibitor
US20090227612A1 (en) 2005-12-22 2009-09-10 Boonsaeng Park Aminopyrimidine Derivatives Inhibiting Protein Kinase Activity, Method For The Preparation Thereof And Pharmaceutical Composition Containing Same
US7943613B2 (en) 2005-12-22 2011-05-17 High Point Pharmaceuticals, Llc Compounds, their preparation and use
JP2009520763A (en) 2005-12-23 2009-05-28 ノバルティス アクチエンゲゼルシャフト Dpp-iv useful fused heterocyclic compounds as inhibitors
US20090156465A1 (en) 2005-12-30 2009-06-18 Sattigeri Jitendra A Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors
WO2007081755A3 (en) 2006-01-09 2007-11-01 Metabasis Therapeutics Inc Indole-benzimidazole and indazole inhibitors of tyrosine phosphatases
EP1976859A1 (en) 2006-01-11 2008-10-08 Boehringer Ingelheim International GmbH CRYSTALLINE FORM OF 1´-(1-METHYLETHYL)- 4´-[(2-FLUORO-4-METHOXYPHENYL)METHYL]-5´-METHYL-1H-PYRAZOL-3´-O-beta-D-GLUCOPYRANOSIDE, A METHOD FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS
CA2635211A1 (en) 2006-01-13 2007-08-02 Merck & Co., Inc. Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
JP2009523781A (en) 2006-01-18 2009-06-25 エヴォルヴァ エスアー Ppar regulators
CA2676444C (en) 2007-01-18 2013-07-30 Evolva Sa Prodrugs of substituted 1,3-dioxanes and their uses
EP1984370A4 (en) 2006-01-23 2010-03-31 Crystalgenomics Inc Imidazopyridine derivatives inhibiting protein kinase activity, method for the preparation thereof and pharmaceutical composition containing same
CN101007798B (en) 2006-01-24 2011-01-26 中国人民解放军军事医学科学院毒物药物研究所 Benzodioxole derivatives and their preparation method and medicinal uses
EP1978804B1 (en) 2006-01-25 2014-07-30 Merck Sharp & Dohme Corp. Aminocyclohexanes as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
CN101007804B (en) 2006-01-25 2011-05-11 中国人民解放军军事医学科学院毒物药物研究所 1,3-benzodioxole-2,2-dicarboxylic acid derivatives and their preparation method and medicinal uses
ES2378704T3 (en) 2006-01-27 2012-04-17 Array Biopharma, Inc. Glucokinase activators
WO2007134014A3 (en) 2006-05-05 2009-04-09 Sanjay Bhanot Compounds and methods for modulating expression of gcgr
CN101360743A (en) 2006-01-30 2009-02-04 Irm责任有限公司 Polycyclic 1, 2, 3, 4 -tetrahydro- isoquinoline derivatives and compositions comprising them as ppar modulators
EP1979355B1 (en) 2006-01-30 2010-08-18 Irm Llc Spiro imidazole derivatives as ppar modulators
JP2009525280A (en) 2006-01-30 2009-07-09 アイアールエム・リミテッド・ライアビリティ・カンパニーIrm,Llc The compounds and compositions as Ppar modulator
KR20080091503A (en) 2006-01-31 2008-10-13 인사이트 코포레이션 Amido compounds and their use as pharmaceuticals
US7632838B2 (en) 2006-02-07 2009-12-15 Wyeth 11-beta HSD1 inhibitors
EP1983993A4 (en) 2006-02-07 2010-09-22 Merck Sharp & Dohme Niacin receptor agonists, compositions containing such compounds and methods of treatment
EP1983972A4 (en) 2006-02-13 2012-01-25 Wellstat Therapeutics Corp Compounds for the treatment of metabolic disorders
DE102006006648A1 (en) 2006-02-14 2007-08-23 Merck Patent Gmbh Mandelsäurehydrazide
JP2009531291A (en) 2006-02-15 2009-09-03 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Glucopyranosyl-substituted benzonitrile derivatives, pharmaceutical compositions containing these compounds, methods for their use and manufacture
WO2007097931A3 (en) 2006-02-15 2007-11-22 Tesfaye Biftu Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
ES2327187T3 (en) 2006-02-27 2009-10-26 Cadila Healthcare Limited Carboxylic acid 1,3-dioxane.
WO2007101060A3 (en) 2006-02-28 2007-12-13 Wellstat Therapeutics Corp Compounds for the treatment of metabolic disorders
US7834178B2 (en) 2006-03-01 2010-11-16 Bristol-Myers Squibb Company Triazine 11-beta hydroxysteroid dehydrogenase type 1 inhibitors
WO2007099385A1 (en) 2006-03-01 2007-09-07 Glenmark Pharmaceuticals S.A. Dipeptidyl peptidase iv inhibitor compounds and compositions
US20070213311A1 (en) 2006-03-02 2007-09-13 Yun-Long Li Modulators of 11-beta hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same
WO2007100027A1 (en) 2006-03-02 2007-09-07 Daiichi Sankyo Company, Limited Optically active thiazolidinedione derivative
WO2007103719A3 (en) 2006-03-03 2008-01-24 Chunhong He MODULATORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
WO2007103252A3 (en) 2006-03-03 2008-03-06 Merck & Co Inc Novel crystalline forms of antidiabetic compounds
US20070270492A1 (en) 2006-03-06 2007-11-22 Avestha Gengraine Technologies Pvt. Ltd. Nananoic acid derivatives as dipeptidyl peptidase inhibitors
US20080051452A1 (en) 2006-03-06 2008-02-28 Avestha Gengraine Technologies Pvt. Ltd. Hexanoic acid derivatives as dipeptidyl peptidase inhibitors
JP2009132620A (en) 2006-03-07 2009-06-18 Astellas Pharma Inc Phenylthiazole derivative
JP5302012B2 (en) 2006-03-08 2013-10-02 タケダ カリフォルニア インコーポレイテッド Glucokinase activators
WO2007101864A3 (en) 2006-03-09 2007-10-25 Novo Nordisk As Compounds that modulate ppar activity, their preparation and use
WO2007104053A3 (en) 2006-03-09 2007-11-01 Gulzar Ahmed 8-heteroarylpurine mnk2 inhibitors for treating metabolic disorders
WO2007105650A1 (en) 2006-03-10 2007-09-20 Ajinomoto Co., Inc. 4-hydroxyisoleucine derivative and process for producing the derivative
CA2646430A1 (en) 2006-03-14 2007-09-20 Amgen Inc. Bicyclic carboxylic acid derivatives useful for treating metabolic disorders
WO2007104789A3 (en) 2006-03-15 2008-03-13 Thomas Kruse Hansen Amylin derivatives
RU2008140940A (en) 2006-03-16 2010-04-27 Астеллас Фарма Инк. (Jp) A triazole derivative or salt thereof
JP5243696B2 (en) 2006-03-17 2013-07-24 田辺三菱製薬株式会社 Benzene derivatives
WO2007107550A1 (en) 2006-03-21 2007-09-27 High Point Pharmaceuticals, Llc Adamantane derivatives for the treatment of the metabolic syndrome
CN101405270B (en) 2006-03-22 2013-01-16 霍夫曼-拉罗奇有限公司 Pyrazoles as 11-beta-HSD-1
WO2007111921A1 (en) 2006-03-23 2007-10-04 Amgen Inc. 1-phenylsulfonyl-diaza heterocyclic amide compounds and their uses as modulators of hydroxsteroid dehydrogenases
EP2001472A2 (en) 2006-03-23 2008-12-17 Merck and Co., Inc. Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
CN101437816B (en) 2006-03-24 2013-08-14 阿雷生物药品公司 2-aminopyridine analogs as glucokinase activators
FR2898894B1 (en) 2006-03-24 2008-06-06 Genfit Sa compounds derived from N- (phenethyl) benzamide substituted, preparation and uses
EP2173745A2 (en) 2007-03-23 2010-04-14 Array Biopharma, Inc. 2-aminopyridine analogs as glucokinase activators
FR2898892A1 (en) 2006-03-24 2007-09-28 Genfit Sa New poly-substituted N-(phenethyl)benzamide derivatives are peroxisome proliferator activated receptor activators useful to treat e.g. type-2 diabetes, insulin-resistance, metabolic disorders, atherosclerosis and cardiovascular diseases
JP2007291075A (en) 2006-03-27 2007-11-08 Sankyo Co Ltd New compound sterenin and method for producing the same
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
DE102006014688A1 (en) 2006-03-28 2007-10-04 Sanofi-Aventis New bicyclic pyrazolone or isoxazolone derivatives useful as endothelial lipase inhibitors, e.g. for treating disorders of fat metabolism or glucose utilization
CA2646962C (en) 2006-03-28 2011-06-21 Merck & Co., Inc. Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
GB0606429D0 (en) 2006-03-30 2006-05-10 Novartis Ag Organic compounds
RU2008143053A (en) 2006-03-31 2010-05-10 Новартис АГ (CH) Tiadiazolidinonovye inhibitors ptfazy
CN101410397A (en) 2006-03-31 2009-04-15 诺瓦提斯公司 Organic compounds
WO2007114532A1 (en) 2006-04-03 2007-10-11 Industry-Academic Cooperation Foundation Gyeongsang National University Novel chalcone derivatives, pharmaceutically acceptable salt, method for preparation and uses thereof
JP2009532454A (en) 2006-04-03 2009-09-10 マトリックス ラボラトリーズ リミテッドMatrix Laboratories Limited New dipeptidyl peptidase iv inhibitors and methods for their preparation, pharmaceutical compositions comprising a sequence the inhibitor
CN101050194B (en) 2006-04-05 2013-08-21 上海恒瑞医药有限公司 Derivative of bicyclo-octanes class, preparation method, and application of medicine
CA2646676A1 (en) 2006-04-06 2007-10-18 Prosidion Limited Heterocyclic gpcr agonists
CA2648074A1 (en) 2006-04-07 2007-10-18 High Point Pharmaceuticals, Llc 11.beta.-hydroxysteroid dehydrogenase type 1 active compounds
KR20090047391A (en) 2006-04-07 2009-05-12 데벨로겐 악틴게젤샤프트 Thienopyrimidines having mnk1/mnk2 inhibiting activity for pharmaceutical compositions
US7435833B2 (en) 2006-04-07 2008-10-14 Abbott Laboratories Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
JP2009533368A (en) 2006-04-11 2009-09-17 ノバルティス アクチエンゲゼルシャフト Organic compound
GB0607196D0 (en) 2006-04-11 2006-05-17 Prosidion Ltd G-protein coupled receptor agonists
CA2648642A1 (en) 2006-04-11 2007-10-25 Merck & Co., Inc. Niacin receptor agonists, compositions containing such compounds and methods of treatment
US7728146B2 (en) 2006-04-12 2010-06-01 Probiodrug Ag Enzyme inhibitors
WO2007120593A1 (en) 2006-04-12 2007-10-25 Wyeth Anilino-pyrimidine phenyl and benzothiophene analogs
EP2015769A4 (en) 2006-04-13 2013-12-25 Ipsen Pharma Pharmaceutical compositions of hglp-1, exendin-4 and analogs thereof
JP2007284090A (en) 2006-04-14 2007-11-01 Dic Plastics Inc Lid locking structure and container
WO2007119837A1 (en) 2006-04-14 2007-10-25 Ajinomoto Co., Inc. Lipase inhibitor
JP5232771B2 (en) 2006-04-18 2013-07-10 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap Increase in hdl-c, benzazepine as ppar- delta agent used for reduction and reduced cholesterol ldl-c - oxy - acid derivative
WO2007119887A1 (en) 2006-04-18 2007-10-25 Nippon Chemiphar Co., Ltd. ACTIVATING AGENT FOR PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR δ
WO2007120102A1 (en) 2006-04-19 2007-10-25 Astrazeneca Ab New substituted oxindole derivatives
US8288339B2 (en) 2006-04-20 2012-10-16 Amgen Inc. GLP-1 compounds
WO2007122970A1 (en) 2006-04-20 2007-11-01 Osaka University Ligand capable of binding to nuclear receptor
WO2007122482A1 (en) 2006-04-20 2007-11-01 Pfizer Products Inc. Fused phenyl amido heterocyclic compounds for the prevention and treatment of glucokinase-mediated diseases
US7842713B2 (en) 2006-04-20 2010-11-30 Pfizer Inc Fused phenyl amido heterocyclic compounds
ES2422165T3 (en) 2006-04-21 2013-09-09 Lilly Co Eli Ciclohexilimidazol lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
KR101055576B1 (en) 2006-04-21 2011-08-08 일라이 릴리 앤드 캄파니 11-beta-hydroxy-cyclohexyl-pyrazole as inhibitors of collagenase in the first steroid dehydrogenase-lactam derivative
ES2435115T3 (en) 2006-04-21 2013-12-18 Eli Lilly And Company Biphenylamide derivatives lactam as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
CA2646624C (en) 2006-04-24 2013-08-06 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
WO2007122634A3 (en) 2006-04-24 2007-12-21 Vituduki Narayana Iyeng Balaji Pyrimidinediones as tyrosine kinase inhibitors
US7816349B2 (en) 2006-04-24 2010-10-19 Eli Lilly And Company Substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
WO2007123225A1 (en) 2006-04-24 2007-11-01 Astellas Pharma Inc Oxadiazolidinedione compound
WO2007127704A1 (en) 2006-04-24 2007-11-08 Eli Lilly And Company Cyclohexyl substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
CN101454310B (en) 2006-04-25 2013-07-17 伊莱利利公司 Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
EP2016071B1 (en) 2006-04-25 2013-07-24 Eli Lilly And Company Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
DE602007007211D1 (en) 2006-04-25 2010-07-29 Lilly Co Eli Inhibitors of11-beta-hydroxysteroid dehydrogenase 1
WO2007122411A1 (en) 2006-04-26 2007-11-01 Astrazeneca Ab Diazepan-1-yl-sulfonyl derivatives for the treatment of metabolic syndrome
JP5225076B2 (en) 2006-04-27 2013-07-03 田辺三菱製薬株式会社 Pharmaceutical applications of the carboxylic acid derivative containing the thiazole ring
EP1849785A1 (en) 2006-04-28 2007-10-31 Neuropharma, S.A. N-(2-Thiazolyl)-amide derivatives as GSK-3 inhibitors
ES2354917T3 (en) 2006-04-28 2011-03-21 Transtech Pharma, Inc. Benzamidaglucoquinasa activators.
JP5225980B2 (en) 2006-04-28 2013-07-03 イーライ リリー アンド カンパニー 11-beta-Pierijiniru substituted pyrrolidinone as inhibitors of hydroxysteroid dehydrogenase 1
US7880012B2 (en) 2006-04-28 2011-02-01 Transtech Pharma, Inc. Benzamide glucokinase activators
EP2013163A1 (en) 2006-05-01 2009-01-14 Incyte Corporation Tetrasubstituted ureas as modulators of 11-beta hydroxyl steroid dehydrogenase type 1
JP2009167104A (en) 2006-05-02 2009-07-30 Taisho Pharmaceutical Co Ltd Phenyl 5-thio glycoside compound
JP2009167103A (en) 2006-05-02 2009-07-30 Taisho Pharmaceutical Co Ltd Pyrazolyl 5-thioglycoside compound
EP1854806A1 (en) 2006-05-02 2007-11-14 MPG Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Thioglycosides as pharmaceutically active agents
KR101452915B1 (en) 2006-05-04 2014-10-21 베링거 인겔하임 인터내셔날 게엠베하 Polymorphs
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
WO2007128801A1 (en) 2006-05-08 2007-11-15 Novartis Ag Combination of organic compounds
ES2548393T3 (en) 2006-05-09 2015-10-16 Novo Nordisk A/S Insulin derivative
ES2553154T3 (en) 2006-05-09 2015-12-04 Novo Nordisk A/S Insulin derivative
DE102006021872B4 (en) 2006-05-11 2008-04-17 Sanofi-Aventis 4,5-diphenyl-pyrimidinyl-oxy or mercapto substituted carboxylic acids, process for their preparation and their use as medicaments
DE102006021878A1 (en) 2006-05-11 2007-11-15 Sanofi-Aventis Phenylamino-benzoxazole substituted carboxylic acids, process for their preparation and their use as medicaments
DE102006021874B4 (en) 2006-05-11 2008-03-27 Sanofi-Aventis 4,5-diphenyl-pyrimidinyl-amino substituted carboxylic acids, process for their preparation and their use as medicaments
KR20090006847A (en) 2006-05-11 2009-01-15 사노피-아벤티스 4,5-diphenyl-pyrimidinyl substitued carboxylic acids, method for the production and use thereof as medicaments
US7851468B2 (en) 2006-05-15 2010-12-14 Cephalon, Inc. Substituted pyrazolo[3,4-d]pyrimidines
EP2021327B1 (en) 2006-05-15 2012-04-04 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
EP2019677B1 (en) 2006-05-16 2013-08-14 Merck Sharp & Dohme Corp. Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
JP2009537525A (en) 2006-05-16 2009-10-29 メルク エンド カムパニー インコーポレーテッドMerck & Company Incoporated Glucagon receptor antagonist compounds, compositions and methods of use comprising such compounds
WO2007137066A3 (en) 2006-05-17 2008-07-03 Incyte Corp HETEROCYCLIC INHIBITORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE I AND METHODS OF USING THE SAME
CA2651598A1 (en) 2006-05-18 2007-11-29 Wellstat Therapeutics Corporation Compounds for the treatment of metabolic disorders
RU2437876C2 (en) 2006-05-19 2011-12-27 Тайсо Фармасьютикал Ко., Лтд. C-phenyl glycitol compound for treating diabetes
WO2007135427A1 (en) 2006-05-23 2007-11-29 Astrazeneca Ab 1,4-disubstituted piperazine and 1,4-disubstituted azepane as 11 -beta-hydroxysteroid dehydrogenase 1 inhibitors
JP5230613B2 (en) 2006-05-23 2013-07-10 テラコス・インコーポレイテッド Glucose transporter inhibitors and methods of use thereof
CN101448836B (en) 2006-05-23 2011-12-14 霍夫曼-拉罗奇有限公司 Pyridine and pyrimidine derivatives
JP5105297B2 (en) 2006-05-25 2012-12-26 味の素株式会社 Ppar active control agent
RU2008150752A (en) 2006-05-26 2010-07-10 Новартис АГ (CH) Inhibitors of aldosterone synthase and / or 11-hydroxylase
CA2655665A1 (en) 2006-05-26 2007-12-06 Nestec S.A. Methods of use and nutritional compositions of touchi extract
EP2049518B1 (en) 2006-05-31 2011-08-31 Takeda San Diego, Inc. Indazole and isoindole derivatives as glucokinase activating agents.
KR101156367B1 (en) 2006-06-01 2012-06-13 에프. 호프만-라 로슈 아게 Thiazole derivatives
JP2009190971A (en) 2006-06-06 2009-08-27 Mitsubishi Tanabe Pharma Corp 2-cyanopyrrolidine derivative
FR2901792A1 (en) 2006-06-06 2007-12-07 Negma Lerads Soc Par Actions S DERIVATIVES OF PPARs ACTIVATOR, METHOD OF PREPARATION AND THERAPEUTIC
CA2655146C (en) 2006-06-08 2013-09-24 Amgen Inc. Benzamide derivatives and uses related thereto
US20070287674A1 (en) 2006-06-08 2007-12-13 Hej Research Institute Of Chemistry New treatment of diabetes mellitus
WO2007145834A3 (en) 2006-06-08 2008-04-03 Amgen Inc Benzamide derivatives and uses related thereto
WO2007146761A3 (en) 2006-06-12 2008-10-30 Neurogen Corp Diaryl pyrimidinones and related compounds
WO2008035359A3 (en) 2006-06-12 2008-05-15 Cadila Healthcare Ltd Oximinophenoxyalkanoic acid and phenylalkanoic acid derivatives
EP2038255A2 (en) 2006-06-16 2009-03-25 High Point Pharmaceuticals, LLC Pharmaceutical use of substituted piperidine carboxamides
WO2007149865A3 (en) 2006-06-19 2008-07-24 Scott A Summers Methods and compositions related to inhibition of ceramide synthesis
WO2007148185A3 (en) 2006-06-21 2008-03-13 John William Benbow Substituted 3 -amino- pyrrolidino-4 -lactams as dpp inhibitors
CA2656002A1 (en) 2006-06-23 2007-12-27 Incyte Corporation Purinone derivatives as hm74a agonists
DE102006028862A1 (en) 2006-06-23 2007-12-27 Merck Patent Gmbh 3-amino-imidazo [1,2-a] pyridine
JP5584466B2 (en) 2006-06-23 2014-09-03 インサイト コーポレイション Purinone derivatives as HM74a receptor agonist
KR20090024295A (en) 2006-06-27 2009-03-06 아스트라제네카 아베 Imidazol-pyrimidine derivatives for treatment of diseases related to glycogen synthase kinase (gsk3)
EP2046782A4 (en) 2006-06-27 2010-10-13 Astrazeneca Ab Imidazolylpyrimidine derivatives for treatment of diseases related to glycogen synthase kinase (gsk3)
EP2044057A2 (en) 2006-06-27 2009-04-08 Sanofi-Aventis Derivatives of ureas of piperidine or pyrrolidine, their preparation and their therapeutical use
EP2046791B1 (en) 2006-06-27 2010-03-24 Sanofi-Aventis Urea derivatives of tropane, their preparation and their therapeutic application
EP2743268A3 (en) 2006-06-27 2014-10-08 Takeda Pharmaceutical Company Limited Fused cyclic compounds as GPR40 receptor modulators
US20080004281A1 (en) 2006-06-28 2008-01-03 Kalypsys, Inc. Methods for the modulation of crp by the selective modulation of ppar delta
US7919598B2 (en) 2006-06-28 2011-04-05 Bristol-Myers Squibb Company Crystal structures of SGLT2 inhibitors and processes for preparing same
RU2434862C2 (en) 2006-06-29 2011-11-27 Тайсо Фармасьютикал Ко., Лтд. C-phenyl-1-thioglucitols
US20080004325A1 (en) 2006-06-29 2008-01-03 Wyeth PTP1B inhibitors
EP2044034B1 (en) 2006-07-05 2012-08-22 F. Hoffmann-La Roche AG Alkyl-pyridazine derivatives as inhibitors of 11 beta hydroxysteroid dehydrogenase type 1(11b-hsd 1)
CN101484440A (en) 2006-07-06 2009-07-15 艾尼纳制药公司 Modulators of metabolism and the treatment of disorders related thereto
US7910747B2 (en) 2006-07-06 2011-03-22 Bristol-Myers Squibb Company Phosphonate and phosphinate pyrazolylamide glucokinase activators
WO2008005910A3 (en) 2006-07-06 2008-03-20 Squibb Bristol Myers Co Pyridone/hydroxypyridine 11-beta hydroxysteroid dehydrogenase type i inhibitors
JP5194588B2 (en) 2006-07-06 2013-05-08 大正製薬株式会社 Diabetes prophylactic or therapeutic agent containing 1-thio -d- glucitol derivative as an active ingredient
US7888504B2 (en) 2006-07-06 2011-02-15 Bristol-Myers Squibb Company Glucokinase activators and methods of using same
DE602007006815D1 (en) 2006-07-06 2010-07-08 Arena Pharm Inc 4-AE5-methoxy-6- (2-methyl-6-ä1,2,4ütriazol-1-yl-pyridin-3-ylamino) -pyrimidin-4-yloxyü-piperidin-1-carboxylic acid isopropyl ester as a metabolic modulatore and treatment of diseases associated therewith
CN101100458A (en) 2006-07-07 2008-01-09 上海艾力斯医药科技有限公司 Bibenzimidazole derivative with PPARgamma exciting agent activity and application thereof
US7795291B2 (en) 2006-07-07 2010-09-14 Bristol-Myers Squibb Company Substituted acid derivatives useful as anti-atherosclerotic, anti-dyslipidemic, anti-diabetic and anti-obesity agents and method
US20080009534A1 (en) 2006-07-07 2008-01-10 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
FR2903404B1 (en) 2006-07-10 2008-08-22 Servier Lab New tetracyclic derivatives, method of preparing them and pharmaceutical compositions containing them
CA2657078A1 (en) 2006-07-13 2008-01-17 High Point Pharmaceuticals, Llc 11beta-hydroxysteroid dehydrogenase type 1 active compounds
EP1878721A1 (en) 2006-07-13 2008-01-16 Novo Nordisk A/S 4-Piperidylbenzamides as 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors
FR2903695B1 (en) 2006-07-13 2008-10-24 Merck Sante Soc Par Actions Si Use of imidazole derivatives AMPK activators, their process for the preparation and pharmaceutical compositions containing them
EP2043744A2 (en) 2006-07-13 2009-04-08 SmithKline Beecham Corporation Chemical compounds
WO2008008547A3 (en) 2006-07-14 2008-07-31 Eugene Y Rhee Balloon dilation for implantable prosthesis
JP5372318B2 (en) 2006-07-14 2013-12-18 パナソニック株式会社 Method for producing an electrochemical capacitor
DE102006033140A1 (en) 2006-07-18 2008-01-24 Merck Patent Gmbh Aminoindazolharnstoffderivate
EP2051977A2 (en) 2006-07-20 2009-04-29 Amgen Inc. SUBSTITUTED AZOLE AROMATIC HETEROCYCLES AS INHIBITORS OF LLbeta-HSD-1
GB0902845D0 (en) 2006-07-21 2009-04-08 Lupin Ltd Antidiabetic azabicyclo (3.1.0) hexan compounds
FR2903984B1 (en) 2006-07-24 2008-10-03 Genfit Sa Imidazolone derivatives of substituted, preparation and uses
JP2008031064A (en) 2006-07-27 2008-02-14 Astellas Pharma Inc Diacylpiperazine derivative
US7851617B2 (en) 2006-07-27 2010-12-14 Mitsubishi Tanabe Pharma Corporation Indole derivatives
WO2008012532A3 (en) 2006-07-27 2008-03-13 Astrazeneca Ab : pyridine-3-carboxamide compounds and their use for inhibiting 11-beta-hydroxysteroid dehydrogenase
RU2009106866A (en) 2006-07-27 2010-09-10 Чугаи Сейяку Кабусики Кайся (Jp) Spiroketal fused ring derivative and its use as an antidiabetic medicament
KR20090033494A (en) 2006-07-27 2009-04-03 추가이 세이야쿠 가부시키가이샤 Substituted spiroketal derivative and use thereof as drug for treating diabetes
US20080027014A1 (en) 2006-07-28 2008-01-31 Tanabe Seiyaku Co., Ltd. Novel SGLT inhibitors
WO2008016730A3 (en) 2006-08-02 2008-08-28 Targeted Molecular Diagnostics Compositions and methods for reducing cellular fat
CN101522623B (en) 2006-08-03 2013-06-12 塔夫茨大学信托人 Non-flushing niacin analogues, and methods of use thereof
WO2008016175A1 (en) 2006-08-03 2008-02-07 Nippon Chemiphar Co., Ltd. Activator for peroxisome proliferator activated receptor
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
CA2649044A1 (en) 2006-08-04 2008-02-07 Daiichi Sankyo Company, Limited Benzylphenyl glucopyranoside derivative
KR100826108B1 (en) 2006-08-04 2008-04-29 한국화학연구원 Furan-2-carboxylic acid?derivatives and process for the preparation thereof
WO2008019309A1 (en) 2006-08-04 2008-02-14 Metabasis Therapeutics, Inc. Novel inhibitors of fructose 1,6-bisphosphatase
EP1887006A1 (en) 2006-08-07 2008-02-13 Krka Polymorphic forms of rosiglitazone base
EP2057160A1 (en) 2006-08-08 2009-05-13 Boehringer Ingelheim International GmbH Pyrrolo [3, 2 -d]pyrimidines as dpp-iv inhibitors for the treatment of diabetes mellitus
WO2008022015A3 (en) 2006-08-11 2008-10-23 Tufts College Retro-inverso incretin analogues, and methods of use thereof
CA2656847A1 (en) 2006-08-15 2008-02-21 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituted cyclopropylbenzene derivatives, pharmaceutical compositions containing such compounds, their use as sglt inhibitors and process for their manufacture
WO2008021560A3 (en) 2006-08-17 2008-07-10 Amylin Pharmaceuticals Inc Dpp-iv resistant gip hybrid polypeptides with selectable properties
JP2009256208A (en) 2006-08-17 2009-11-05 Dainippon Sumitomo Pharma Co Ltd Phthalide derivative or pharmaceutically acceptable salt of the same
WO2008023239A1 (en) 2006-08-23 2008-02-28 Pfizer Products Inc. Pyrimidone compounds as gsk-3 inhibitors
US7727978B2 (en) 2006-08-24 2010-06-01 Bristol-Myers Squibb Company Cyclic 11-beta hydroxysteroid dehydrogenase type I inhibitors
WO2008024497A3 (en) 2006-08-25 2008-07-24 Vitae Pharmaceuticals Inc INHIBITORS OF 11β -HYDROXYSTEROID DEHYDROGENASE TYPE 1
WO2008029217A3 (en) 2006-08-29 2008-07-24 Naresh Chidurula Dipeptidyl peptidase iv inhibitors
KR101504769B1 (en) 2006-08-30 2015-03-20 페노믹스 코포레이션 Solid citrate and tartrate salt of the inhibitor, Dpp-ⅳ
WO2008025800A1 (en) 2006-08-30 2008-03-06 Biovitrum Ab (Publ) Pyrimidine compounds for treating gpr119 related disorders
WO2008028188A3 (en) 2006-09-01 2008-12-31 Richard M Harmon Demand aggregation for future items contingent upon threshold demand
CN101528738A (en) 2006-09-01 2009-09-09 沃泰克斯药物股份有限公司 5-(2-furyl)-1,3-thiazole derivatives useful as inhibitors of phosphatidylinositol 3-kinase
JP2008063256A (en) 2006-09-06 2008-03-21 Astellas Pharma Inc β-AMINO ACID DERIVATIVE
US7687526B2 (en) 2006-09-07 2010-03-30 Amgen Inc. Benzo-fused compounds for use in treating metabolic disorders
WO2008028662A1 (en) 2006-09-07 2008-03-13 Santhera Pharmaceuticals (Schweiz) Ag N-[1-(3-amino-4-phenyl-butyryl)-4-hydroxy-pyrrolidin-2-ylmethyl}-propionamide and related compounds as dpp-iv inhibitors for the treatment of type 2 diabetes mellitus
WO2008030520A1 (en) 2006-09-07 2008-03-13 Amgen Inc. Heterocyclic gpr40 modulators
JP2010503654A (en) 2006-09-12 2010-02-04 ファイザー・プロダクツ・インク Benzimidazolone derivatives
WO2008033934A1 (en) 2006-09-13 2008-03-20 The Institutes For Pharmaceutical Discovery, Llc Substituted heteroaryl carboxylic acid derivatives as ptb-1b inhibitors
WO2008033455A3 (en) 2006-09-13 2008-12-24 Inst For Pharm Discovery Inc Biphenyl and heteroaryl phenyl derivatives as protein tyrosine phosphatases inhibitors
WO2008033931A1 (en) 2006-09-13 2008-03-20 The Institutes For Pharmaceutical Discovery, Llc Para-xylylene carboxylic acids and isothiazolones useful as protein tyrosine phosphatases (ptps) in particular ptp-ib
ES2370873T3 (en) 2006-09-13 2011-12-23 Takeda Pharmaceutical Company Limited Using 2-6- (3-amino-piperidin-1-yl) -3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl-4-fluoro-benzonitrile for treatment diabetes, cancer, autoimmune disorders and HIV infection.
WO2008033932A3 (en) 2006-09-13 2008-05-02 Inst For Pharm Discovery Inc Biarylthiazole carboxylic acid derivatives as protein tyrosine phosphatase-ib inhibitors
US20100016274A1 (en) 2006-09-14 2010-01-21 Koppel Gary A Beta-lactam cannabinoid receptor modulators
WO2008034859A8 (en) 2006-09-21 2008-06-12 Boehringer Ingelheim Int Glucopyranosyl-substituted difluorobenzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
WO2008034881A1 (en) 2006-09-22 2008-03-27 Novo Nordisk A/S Protease resistant insulin analogues
CA2664037A1 (en) 2006-09-29 2008-04-03 F. Hoffmann-La Roche Ag Sulfonamide derivatives
US7781577B2 (en) 2006-09-29 2010-08-24 Lexicon Pharmaceuticals, Inc. Inhibitors of sodium glucose co-transporter 2 and methods of their use
WO2008039882A1 (en) 2006-09-30 2008-04-03 Sanofi-Aventis U.S. Llc A combination of niacin and a prostaglandin d2 receptor antagonist
DK2084182T3 (en) 2006-10-03 2013-11-04 Cadila Healthcare Ltd antidiabetic compounds
JP2010505828A (en) 2006-10-03 2010-02-25 メルク エンド カムパニー インコーポレーテッドMerck & Company Incoporated Glucagon receptor antagonist compounds, compositions containing such compounds, and methods of use
KR20090060426A (en) 2006-10-06 2009-06-12 반유 세이야꾸 가부시끼가이샤 2-pyridinecarboxamide derivative having gk-activating activity
WO2008044656A1 (en) 2006-10-06 2008-04-17 Taisho Pharmaceutical Co., Ltd. Imidazolidinone derivative
WO2008040995A9 (en) 2006-10-07 2008-12-31 Peakdale Molecular Ltd Indazoles for use as dpp-iv inhibitors
US8022061B2 (en) 2006-10-10 2011-09-20 Amgen Inc. N-aryl pyrazole compounds, compositions, and methods for their use
EP1911747A1 (en) 2006-10-11 2008-04-16 Laboratorios del Dr. Esteve S.A. Sulfonamide substituted pyrazoline compounds, their preparation and use as CB1 modulators
WO2008044700A1 (en) 2006-10-11 2008-04-17 Takeda Pharmaceutical Company Limited GSK-3β INHIBITOR
JPWO2008044762A1 (en) 2006-10-13 2010-02-18 中外製薬株式会社 Thioglucose spiro ketal derivatives, and their use as antidiabetic agents
US20080107725A1 (en) 2006-10-13 2008-05-08 Albano Antonio A Pharmaceutical Solid Dosage Forms Comprising Amorphous Compounds Micro-Embedded in Ionic Water-Insoluble Polymers
US7705005B2 (en) 2006-10-13 2010-04-27 Glaxo Group Limited Bicyclic heteroaromatic compounds
DE102006048728A1 (en) 2006-10-16 2008-04-17 Merck Patent Gmbh 3-amino-imidazo {1,2-a] pyridine
EP2080275A4 (en) 2006-10-16 2010-08-18 Vidyo Inc Systems and methods for signaling and performing temporal level switching in scalable video coding
EP2077267A4 (en) 2006-10-18 2010-04-07 Takeda Pharmaceutical Fused heterocyclic compound
EP2508524A3 (en) 2006-10-19 2012-10-24 Takeda Pharmaceutical Company Limited Indole compound
KR101118410B1 (en) 2006-10-19 2012-04-23 에프. 호프만-라 로슈 아게 Imidazolone and imidazolidinone derivatives as 11b-hsd1 inhibitors for diabetes
US20100204278A1 (en) 2006-10-20 2010-08-12 Beresis Richard T Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment
EP2086964A2 (en) 2006-10-23 2009-08-12 Astra Zeneca AB Benzoyl amino heterocyclyl compounds useful in the treatment of a disease mediated through glk
KR100812538B1 (en) 2006-10-23 2008-03-11 한올제약주식회사 Controlled release complex formulation comprising metformin and glimepiride
US20080103201A1 (en) 2006-10-26 2008-05-01 Wijayabandara Mirihanage Don J Novel alpha-Glucosidase inhibitor from Tabernaemontana dichotoma
CN101805299A (en) 2006-10-26 2010-08-18 阿斯利康(瑞典)有限公司 Benzoyl amino heterocyclyl compounds as glucokinase (glk) activators
WO2008049711A1 (en) 2006-10-27 2008-05-02 Novo Nordisk A/S Peptide extended insulins
CA2667550A1 (en) 2006-10-27 2008-05-02 Boehringer Ingelheim International Gmbh Crystalline form of 4-(.beta.-d-glucopyranos-1-yl)-1-methyl-2-[4-((s)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments
WO2008054674A3 (en) 2006-10-31 2009-04-16 Merck & Co Inc Antidiabetic bicyclic compounds
EP2079467B1 (en) 2006-10-31 2015-11-18 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
US8198311B2 (en) 2006-11-01 2012-06-12 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
EP2089389A2 (en) 2006-11-01 2009-08-19 Bristol-Myers Squibb Company Heterocyclic compounds as modulators of glucocorticoid receptor, ap-1, and/or nf-kappa-b activity
EP2094692B1 (en) 2006-11-01 2012-11-28 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, ap-1 and/or nf-kappab activity and use thereof
WO2008057862A3 (en) 2006-11-01 2008-10-16 Squibb Bristol Myers Co MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-ϰB ACTIVITY AND USE THEREOF
EP2078015B1 (en) 2006-11-01 2012-03-21 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, ap-1 and/or nf-kappab activity and use thereof
JP5552313B2 (en) 2006-11-01 2014-07-16 プロノヴァ・バイオファーマ・ノルゲ・アーエスPronova BioPharma Norge AS Lipid compounds
JP2010509231A (en) 2006-11-02 2010-03-25 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated Useful aminopyridine and aminopyrimidine as inhibitors of protein kinases
EP2077846B1 (en) 2006-11-02 2011-10-12 Piramal Life Sciences Limited Benzoxazepine compounds, their preparation and use
WO2009056881A1 (en) 2007-10-29 2009-05-07 Astrazeneca Ab Chemical compounds 313
US7964618B2 (en) 2006-11-03 2011-06-21 Astrazeneca Ab Chemical compounds
EP1918285A1 (en) 2006-11-03 2008-05-07 Merck Sante Diazepane-acetamide derivatives as selective 11beta-HSD1 inhibitors
JP2010508371A (en) 2006-11-06 2010-03-18 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Glucopyranosyl-substituted phenyl derivatives, pharmaceuticals and used and a manufacturing method thereof containing the compound
EP1921080B1 (en) 2006-11-07 2009-08-05 Sanofi-Aventis Subsitituted 8-piperidinyl-2-pyridinyl-pyrimido(1,2-a)pyrimidin-6-one and 8-piperidinyl-2-pyrimidinyl-pyrimido(1,2-a)pyrimidin-6-one derivatives
JP2010043001A (en) 2006-11-09 2010-02-25 Sanwa Kagaku Kenkyusho Co Ltd Glp-1 derivative and use thereof
KR101463724B1 (en) 2006-11-09 2014-11-21 베링거 인겔하임 인터내셔날 게엠베하 Combination therapy with SGLT-2 inhibitors and their pharmaceutial compositions
CA2669607A1 (en) 2006-11-14 2008-05-22 Santen Pharmaceutical Co., Ltd. Novel 1,2-dihydroquinoline derivative having (substituted phenyl or substituted heterocyclic) carbonyloxy lower alkyl group and ester-introduced phenyl group as substituents
WO2008060488A1 (en) 2006-11-14 2008-05-22 Merck & Co., Inc. Tricyclic heteroaromatic compounds as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
US7750048B2 (en) 2006-11-15 2010-07-06 Janssen Pharmaceutica Nv GPR40 agonists
WO2008059625A1 (en) 2006-11-17 2008-05-22 National University Corporation Kagawa University Utilization of the function of rare sugar as promoter for the migration of glucokinase from nucleus to cytoplasm
WO2008062273A3 (en) 2006-11-20 2009-04-23 Cadila Pharmaceuticals Ltd Solid oral dosage form having antidiabetic drug combination
EP2086975B1 (en) 2006-11-20 2012-03-14 Bristol-Myers Squibb Company 7,8-dihydro-1,6-naphthyridin-5(6h)-ones and related bicyclic compounds as inhibitors of dipeptidyl peptidase iv and methods
EP2096111A1 (en) 2006-11-20 2009-09-02 Japan Tobacco Inc. Pyrazoles and use thereof as drugs
WO2008061355A1 (en) 2006-11-24 2008-05-29 Matregen Corp. Glp-1 depot systems, and methods of manufacture and uses thereof
WO2008066070A1 (en) 2006-11-29 2008-06-05 Uha Mikakuto Co., Ltd. Dipeptidyl peptidase-iv inhibitor
JP4125768B2 (en) 2006-11-30 2008-07-30 公立大学法人大阪府立大学 α- glucosidase inhibitor
JPWO2008066097A1 (en) 2006-12-01 2010-03-11 アステラス製薬株式会社 Carboxylic acid derivatives
US8367708B2 (en) 2006-12-01 2013-02-05 Msd K.K. Phenyl-isoxazol-3-ol derivative
RU2444514C2 (en) 2006-12-02 2012-03-10 Сеул Нэшнл Юниверсити Индастри Фаундейшн Aryl compounds as ppar ligands and their application
US7943582B2 (en) 2006-12-04 2011-05-17 Mitsubishi Tanabe Pharma Corporation Crystalline form of 1-(β-D-glucopyransoyl)-4-methyl-3-[5-(4-fluorophenyl)-2- thienylmethyl]benzene hemihydrate
EP2099791B1 (en) 2006-12-04 2012-11-21 Janssen Pharmaceutica, N.V. Thienyl-containing glycopyranosyl derivatives as antidiabetics
ES2572189T3 (en) 2006-12-05 2016-05-30 Bayer Ip Gmbh Derivatives of 2,3-dihydro-imidazo [1,2-c] quinazoline substituted useful in treating hyperproliferative disorders and diseases associated with angiogenesis
EP2094683B1 (en) 2006-12-06 2011-10-12 GlaxoSmithKline LLC Bicyclic compounds and use as antidiabetics
EP2102170A2 (en) 2006-12-06 2009-09-23 Boehringer Ingelheim International GmbH Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE102006058236A1 (en) 2006-12-11 2008-06-12 Merck Patent Gmbh indolizine derivatives
WO2008071169A3 (en) 2006-12-11 2009-07-30 Uksh Schleswig Holstein Method for the production of specific inhibitors of 11-beta-hydroxysteroid dehydrogenase, in particular type 1 with basic nor-oleanan or nor-ursan frameworks
EP2112880A4 (en) 2006-12-14 2011-12-21 Merck Sharp & Dohme Acyl bipiperidinyl compounds, compositions containing such compounds and methods of treatment
US7902248B2 (en) 2006-12-14 2011-03-08 Hoffmann-La Roche Inc. Oxime glucokinase activators
EP2103607A4 (en) 2006-12-14 2011-01-05 Taisho Pharma Co Ltd 1-phenyl 1-thio-d-glucitol derivative
EP1932843A1 (en) 2006-12-14 2008-06-18 sanofi-aventis Sulfonyl-phenyl-2H-(1,2,4) oxadiazole-5-one derivatives, processes for their preparation and their use as pharmaceuticals
EP2213668A3 (en) 2006-12-18 2010-11-24 Novartis AG Imidazoles as aldosterone synthase inhibitors
CA2672286A1 (en) 2006-12-18 2008-06-26 Novartis Ag Organic compounds
WO2008077138A1 (en) 2006-12-19 2008-06-26 The Board Of Trustees Of The University Of Illinois 3-benzofuranyl-4-indolyl maleimides as potent gsk3 inhibitors for neurogenerative disorders
EP1939187A1 (en) 2006-12-20 2008-07-02 Sanofi-Aventis Substituted heteroaryl pyridopyrimidone derivatives
JP2010513488A (en) 2006-12-20 2010-04-30 メルク・シャープ・エンド・ドーム・コーポレイション Bipiperidinyl compounds, compositions and methods of treatment containing the compound
EP2091947A2 (en) 2006-12-20 2009-08-26 Takeda San Diego, Inc. Glucokinase activators
JPWO2008075741A1 (en) 2006-12-20 2010-04-15 国立大学法人 長崎大学 Antidiabetic agents and prophylactic agents
EP1935420A1 (en) 2006-12-21 2008-06-25 Merck Sante 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors
WO2008084303A1 (en) 2006-12-21 2008-07-17 Pfizer Products Inc. Compounds having both angiotensin ii receptor antagonism and ppary activating activities
EP2121666A1 (en) 2006-12-21 2009-11-25 AstraZeneca AB Novel crystalline compound useful as glk activator
US20130012485A1 (en) 2006-12-22 2013-01-10 Baeschlin Daniel Kaspar Organic compounds
KR20090096615A (en) 2006-12-25 2009-09-11 교린 세이야꾸 가부시키 가이샤 Glucokinase-activating substance
WO2008078725A1 (en) 2006-12-26 2008-07-03 Daiichi Sankyo Company, Limited Thiazepine derivative
EP2121580A2 (en) 2006-12-26 2009-11-25 Amgen Inc. N-cyclohexyl benzamides and benzeneacetamides as inhibitors of 11-beta-hydroxysteroid dehydrogenases
JP2008156318A (en) 2006-12-26 2008-07-10 Dainippon Sumitomo Pharma Co Ltd 1,3,4-oxadiazol-2-one derivative
US7795228B2 (en) 2006-12-28 2010-09-14 Theracos, Inc. Spiroheterocyclic glycosides and methods of use
EP1939192A1 (en) 2006-12-28 2008-07-02 Neuropharma S.A. Cyclopentanone derivatives, method of synthesis and uses thereof
US8012955B2 (en) 2006-12-28 2011-09-06 Rigel Pharmaceuticals, Inc. N-substituted-heterocycloalkyloxybenzamide compounds and methods of use
US7638541B2 (en) 2006-12-28 2009-12-29 Metabolex Inc. 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
EP1939191A1 (en) 2006-12-28 2008-07-02 Neuropharma S.A. Furan derivatives, method of synthesis and uses thereof
FR2910892A1 (en) 2006-12-29 2008-07-04 Genfit Sa New substituted 1,3-diphenylpropane derivatives are peroxisome proliferator-activated receptor agonist useful treat e.g. diabetic, dyslipidemia, cardiovascular disease, obesity, hypertension, inflammatory diseases and cerebral ischaemia
FR2910893A1 (en) 2006-12-29 2008-07-04 Genfit Sa New Phenylthiazolyl/phenyloxazolyl derivatives are peroxisome proliferator-activated receptor agonist useful to treat e.g. diabetic, dyslipidemia, cardiovascular disease, hypertension, inflammatory diseases and cerebral ischaemia
FR2910894A1 (en) 2006-12-29 2008-07-04 Genfit Sa New substituted 3-phenyl-1-(phenylthienyl)propan-1-one and 3-phenyl-1-(phenylfuranyl)propan-1-one derivatives are peroxisome proliferator-activated receptor agonist useful to treat e.g. diabetic, dyslipidemia, obesity and hypertension
US20100063302A1 (en) 2007-01-03 2010-03-11 Takano Co., Ltd. Cyclic sulfonium salt, method for production of cyclic sulfonium salt, and glycosidase inhibitor
DK2114931T3 (en) 2007-01-04 2012-02-13 Prosidion Ltd Piperidine GPCR agonists
EP2114933B1 (en) 2007-01-04 2011-09-07 Prosidion Ltd Piperidine gpcr agonists
GB0700122D0 (en) 2007-01-04 2007-02-14 Prosidion Ltd GPCR agonists
EP2114936A1 (en) 2007-01-04 2009-11-11 Prosidion Limited Piperidine gpcr agonists
CA2674455A1 (en) 2007-01-04 2008-07-10 Prosidion Limited Piperidine gpcr agonists
FR2911138B1 (en) 2007-01-05 2009-02-20 Sanofi Aventis Sa New derivatives of n, n'-2,4-dianilinopyrimidines, their preparation has as medicines, pharmaceutical compositions including such inhibitors ikk
FR2911137B1 (en) 2007-01-05 2009-02-20 Sanofi Aventis Sa New derivatives of 2,4-dianilinopyrimides, their preparation has as medicines, pharmaceutical compositions including such inhibitors ikk
JP2008169195A (en) 2007-01-05 2008-07-24 Hanmi Pharmaceutical Co Ltd Insulinotopic peptide drug combo using carrier material
FR2911139A1 (en) 2007-01-05 2008-07-11 Sanofi Aventis Sa New 2,4-diaminopyrimidine derivatives useful for treating inflammatory diseases, diabetes or cancer
FR2911140B1 (en) 2007-01-05 2009-02-20 Sanofi Aventis Sa New derivatives of 2-anilino-4-heteroaryl pyrimides, their preparation has as medicines, pharmaceutical compositions including such inhibitors ikk
US20090098130A1 (en) 2007-01-05 2009-04-16 Bradshaw Curt W Glucagon-like protein-1 receptor (glp-1r) agonist compounds
JP5367584B2 (en) 2007-01-08 2013-12-11 ソウル ナショナル ユニバーシティー インダストリー ファンデーション Peroxisome proliferator-activated receptor δ ligands thiazole compounds and medicaments containing the same, cosmetics and health food composition
WO2008084043A1 (en) 2007-01-09 2008-07-17 Novo Nordisk A/S Urea glucokinase activators
WO2008084873A1 (en) 2007-01-10 2008-07-17 Mitsubishi Tanabe Pharma Corporation Oxime derivative
JP5207981B2 (en) 2007-01-10 2013-06-12 田辺三菱製薬株式会社 Hydrazone derivatives
JP4328820B2 (en) 2007-01-10 2009-09-09 田辺三菱製薬株式会社 Pharmaceutical compositions
WO2008084044A1 (en) 2007-01-11 2008-07-17 Novo Nordisk A/S Urea glucokinase activators
WO2008087654A3 (en) 2007-01-16 2008-12-18 Cadila Healthcare Ltd PIPERIDINES AS INHIBITORS OF 11β-HYDROXYSTEROID DEHYDROGENASE TYPE 1
KR100848491B1 (en) 2007-01-16 2008-07-28 영진약품공업주식회사 2-thiazolidine derivatives having beta;-amino group, pharmaceutical acceptable salts and preparation process thereof
DE102007002260A1 (en) 2007-01-16 2008-07-31 Sanofi-Aventis Use of substituted Pyranonsäurederivaten for the preparation of medicaments for the treatment of metabolic syndrome
DE102007002717A1 (en) 2007-01-18 2008-07-24 Merck Patent Gmbh heterocyclic indazole derivatives
WO2008089463A3 (en) 2007-01-18 2008-09-12 Evolva Sa Substituted 1,3-dioxanes and their uses
WO2008088006A1 (en) 2007-01-19 2008-07-24 Shinji Yokoyama Ap2 inhibitor
WO2008091863A1 (en) 2007-01-23 2008-07-31 Kalypsys, Inc. Sulfonyl-substituted bicyclic compounds as ppar modulators for the treatment of non-alcoholic steatohepatitis
EP2120959A4 (en) 2007-01-23 2010-05-26 Reddys Lab Ltd Dr Methods and compositions for the treatment of insulin resistance, diabetes, and diabetes-associated dyslipidemia
CN101230058A (en) 2007-01-23 2008-07-30 上海恒瑞医药有限公司 Bicycle aza alkyl derivative, preparation method and use in medicine thereof
US8431713B2 (en) 2007-01-24 2013-04-30 Array Biopharma, Inc. 2-aminopyridine derivatives as glucokinase activators
WO2008090209A3 (en) 2007-01-26 2008-10-02 Boehringer Ingelheim Int Use of glucopyranosyloxy- pyrazoles for preventing and treating neurodegenerative disorders
JP2010516721A (en) 2007-01-26 2010-05-20 サノフィ−アベンティス Phenothiazine derivatives, their use as their preparation and pharmaceutical
DK2114971T3 (en) 2007-01-26 2015-08-31 Kaneq Pharma Inc Fused aromatic PTB-1B inhibitors
WO2008090210A1 (en) 2007-01-26 2008-07-31 Boehringer Ingelheim International Gmbh Methods for preventing and treating neurodegenerative disorders
US20100016396A1 (en) 2007-01-29 2010-01-21 Hiroshi Imoto Pyrazole compound
KR20080071476A (en) 2007-01-30 2008-08-04 주식회사 엘지생명과학 Novel dipeptidyl peptidase-iv inhibitors
EP2121613A2 (en) 2007-01-31 2009-11-25 Vertex Pharmaceuticals, Inc. 2-aminopyridine derivatives useful as kinase inhibitors
JP5161245B2 (en) 2007-02-07 2013-03-13 ファイザー・インク PKC inhibitors as a 3-amino - pyrrolo [3,4-c] pyrazole -5 (1H, 4H, 6H) carbaldehyde derivative
US8242151B2 (en) 2007-02-07 2012-08-14 Kyowa Hakko Kirin Co., Ltd. Tricyclic compounds
WO2008096820A1 (en) 2007-02-07 2008-08-14 Kyowa Hakko Kirin Co., Ltd. Biphenyl derivative
US20100260841A1 (en) 2007-02-08 2010-10-14 Paolini John F Method of Treating Atherosclerosis, Dyslipidemias and Related Conditions
CA2665048C (en) 2007-02-08 2011-11-08 Daiichi Sankyo Company, Limited Crystalline forms of thiazolidinedione compound and its manufacturing method
WO2008096769A1 (en) 2007-02-08 2008-08-14 Daiichi Sankyo Company, Limited Pharmaceutical compositions containing substituted cercosporamide derivatives
WO2008099448A1 (en) 2007-02-09 2008-08-21 Masayoshi Yamaguchi Preventive/therapeutic agent for diabetic diseases
KR101538810B1 (en) 2007-02-09 2015-07-22 메타베이시스 테라퓨틱스, 인크. Glucagon receptor antagonists of the
EP2118066A1 (en) 2007-02-09 2009-11-18 Takeda Pharmaceutical Company Limited Fused ring compounds as partial agonists of ppar-gamma
JP2010120851A (en) 2007-02-09 2010-06-03 Kyorin Pharmaceut Co Ltd Dimerized cyclo derivative
WO2008099145A1 (en) 2007-02-12 2008-08-21 Astrazeneca Ab Pyrazole derivatives as 11-beta-hsd1 inhibitors
US7951833B2 (en) 2008-02-04 2011-05-31 Astrazeneca Ab Crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]Benzoic acid 471
JP6017754B2 (en) 2007-02-15 2016-11-02 インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションIndiana University Research And Technology Corporation Glucagon / glp-1 receptor co-agonist
DE102007007751A1 (en) 2007-02-16 2008-08-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg New substituted Arylsulfonylglycine, their preparation and their use as medicaments
US7879807B2 (en) 2007-02-21 2011-02-01 Boehringer Ingelheim International Gmbh Tetrasubstituted glucopyranosylated benzene derivatives, medicaments containing such compounds, their use and process for their manufacture
DE102007008420A1 (en) 2007-02-21 2008-08-28 Merck Patent Gmbh benzimidazole derivatives
EP2121675A1 (en) 2007-02-22 2009-11-25 Irm Llc Thiazole derivatives as modulators of g protein-coupled receptors
US8394841B2 (en) 2007-02-22 2013-03-12 Irm Llc Compounds and methods for modulating G protein-coupled receptors
EP1961742A1 (en) 2007-02-22 2008-08-27 Novartis AG compounds of formula (I) as serine protease inhibitors
US20110003856A1 (en) 2007-02-23 2011-01-06 Soren Ebdrup N-adamantyl benzamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase
EP2146952A1 (en) 2007-02-23 2010-01-27 High Point Pharmaceuticals, LLC N-adamantyl benzamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase
EP2150526B1 (en) 2007-02-23 2017-09-20 vTv Therapeutics LLC N-adamantyl benzamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase
JP2010519242A (en) 2007-02-23 2010-06-03 ハイ ポイント ファーマシューティカルズ,リミティド ライアビリティ カンパニー Novel compounds
JP5486928B2 (en) 2007-02-26 2014-05-07 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β- cyclic urea and carbamate inhibitors of hydroxysteroid dehydrogenase 1
DE102007009494A1 (en) 2007-02-27 2008-08-28 Bayer Healthcare Ag New 1,6-naphthyridine or 8-azaquinazoline derivatives useful for treating aldosteronism, hypertension, cardiac insufficiency, myocardial infarct sequelae, liver cirrhosis, renal insufficiency and stroke
CA2679185A1 (en) 2007-02-28 2008-09-04 Advinus Therapeutics Private Limited 2,2,2-tri-substituted acetamide derivatives as glucokinase activators, their process and pharmaceutical application
US8258161B2 (en) 2007-03-02 2012-09-04 Merck Sharp & Dohme Corp. Crystalline salt form of an antidiabetic compound
US8034819B2 (en) 2007-03-07 2011-10-11 Kyorin Pharmaceutical Co., Ltd. Glucokinase activator
WO2008108602A1 (en) 2007-03-07 2008-09-12 Dong-A Pharm. Co., Ltd. Novel phenylpropionic acid derivatives as peroxisome proliferator-activated gamma receptor modulators, method of the same, and pharmaceutical composition comprising the same
US8053463B2 (en) 2007-03-08 2011-11-08 Plexxikon Inc. PPAR active compounds
CA2679314A1 (en) 2007-03-08 2008-09-12 Albireo Ab 2-substituted-3-phenylpropionic acid derivatives and their use in the treatment of inflammatory conditions
CA2679844A1 (en) 2007-03-08 2008-09-12 Plexxikon, Inc. Ppar active compounds
WO2008109702A1 (en) 2007-03-08 2008-09-12 Irm Llc Compounds and compositions as modulators of gpr119 activity
WO2008112642A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
KR20100015414A (en) 2007-03-09 2010-02-12 하이 포인트 파마슈티칼스, 엘엘씨 Indole- and benzimidazole amides as hydroxysteroid dehydrogenase inhibitors
ES2374335T3 (en) 2007-03-09 2012-02-15 Vertex Pharmaceuticals Incorporated aminopyrimidines useful as inhibitors of protein kinases.
CN101260103A (en) 2007-03-09 2008-09-10 上海艾力斯医药科技有限公司 Compound with portion PPARgamma excitant activity and application thereof
WO2008112941A1 (en) 2007-03-13 2008-09-18 Board Of Regents The University Of Texas System Composition and method for the treatment of diseases affected by a peptide receptor
DE102007012645A1 (en) 2007-03-16 2008-09-18 Bayer Healthcare Ag Substituted imidazo and triazolopyrimidines
DE102007012284A1 (en) 2007-03-16 2008-09-18 Boehringer Ingelheim Pharma Gmbh & Co. Kg New substituted Arylsulfonylglycine, their preparation and their use as medicaments
EP1972349A1 (en) 2007-03-21 2008-09-24 Biocompatibles UK Limited GLP-1 fusion peptides conjugated to polymer(s), their production and use
US8173645B2 (en) 2007-03-21 2012-05-08 Takeda San Diego, Inc. Glucokinase activators
WO2008116195A3 (en) 2007-03-22 2008-11-20 Bristol Myers Squibb Compositions comprising an sglt2 ingibitor for treating obesity
CN101686988B (en) 2007-03-22 2013-12-11 百时美施贵宝公司 Pharmaceutical formulations containing dapagliflozin propylene glycol hydrate
WO2008118848A1 (en) 2007-03-23 2008-10-02 Trustees Of Tufts College N-substituted peptidomimetic inhibitors of dipeptidylpeptidase iv
WO2008116294A1 (en) 2007-03-23 2008-10-02 Matregen Corp. Exendin analogs
JP2010521513A (en) 2007-03-23 2010-06-24 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Aza - pyridopyrimidinone derivatives
EP1975176A1 (en) 2007-03-27 2008-10-01 Biocompatibles UK Limited Novel glp-1 fusion peptides, their production and use
WO2008119005A1 (en) 2007-03-27 2008-10-02 Trustees Of Tufts College 3,4-dehydro-proline-containing inhibitors of dipeptidylpeptidase iv
US20100056600A1 (en) 2007-03-28 2010-03-04 Soren Ebdrup 11beta-hsd1 active compounds
WO2008117982A1 (en) 2007-03-28 2008-10-02 Crystal Genomics, Inc. Heterocyclic carboxylic acid derivatives and pharmaceutical composition for inhibiting lipid accumulation containing same
US20100120736A1 (en) 2007-03-29 2010-05-13 N.V. Organon Mineralocorticoid Receptor Antagonists
EP2142542A4 (en) 2007-03-30 2011-06-22 Astrazeneca Ab New imidazo [4,5-b] pyridine-7-carboxamides 704
WO2008121064A1 (en) 2007-03-30 2008-10-09 Astrazeneca Ab New imidazo[4,5-b]pyridine-6-halo-7-aryl/heteroaryl compounds 705
US7998992B2 (en) 2007-03-30 2011-08-16 Institute Of Medicinal Molecular Design, Inc. Oxazolidinone derivative having inhibitory activity on 11β-hydroxysteroid dehydrogenase type 1
WO2008121506A3 (en) 2007-03-30 2009-02-19 Stephen L Gwaltney Renin inhibitors
CN101274918A (en) 2007-03-30 2008-10-01 中国科学院上海药物研究所;国家新药筛选中心 Substitutive five membered heterocyclic compound, preparation and medical use thereof
JP2010138073A (en) 2007-03-30 2010-06-24 Nissan Chem Ind Ltd Picolinic acid amide
RU2492175C2 (en) 2007-04-02 2013-09-10 Теракос, Инк. Benzyl derivatives of glycosides and methods of their application
ES2529149T3 (en) 2007-04-03 2015-02-17 Mitsubishi Tanabe Pharma Corporation A combination of dipeptidyl peptidase IV inhibitor and a sweetener for use in the treatment of obesity
CN101279955B (en) 2007-04-03 2012-11-28 北京摩力克科技有限公司 N-substituted thiamorpholine derivate as DPP-IV inhibitor and medical use thereof
CA2682875A1 (en) 2007-04-05 2008-10-16 Sanofi-Aventis Imidazolidine carboxamide derivatives as lipase and phospholipase inhibitors
WO2008126731A1 (en) 2007-04-05 2008-10-23 Daiichi Sankyo Company, Limited Aryl derivatives
WO2008122357A1 (en) 2007-04-05 2008-10-16 Sanofi-Aventis 5-oxo-isoxazoles as inhibitors of lipases and phospholipases
WO2008126732A1 (en) 2007-04-05 2008-10-23 Daiichi Sankyo Company, Limited Fused bicyclic heteroaryl derivatives
EP2136811A1 (en) 2007-04-10 2009-12-30 Boehringer Ingelheim International GmbH Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US20100063282A1 (en) 2007-04-10 2010-03-11 Boehringer Ingelheim International Gmbh Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions, and Uses Thereof
EP2152081B1 (en) 2007-04-11 2012-10-24 High Point Pharmaceuticals, LLC Novel compounds
GB0707087D0 (en) 2007-04-12 2007-05-23 Piramed Ltd Pharmaceutical compounds
US20100130496A1 (en) 2007-04-12 2010-05-27 F. Hoffmann-La Roche Ag Pyrimidine derivatives as inhibitors of phosphatidylinositol-3-kinase
WO2008125945A3 (en) 2007-04-12 2009-03-12 Iriny Botrous 3-amido-pyrrolo [3, 4-c] pyrazole-5 (1h, 4h, 6h) carbaldehyde derivatives as inhibitors of protein kinase c
KR20100016431A (en) 2007-04-12 2010-02-12 디 인스티튜트 오브 캔서 리서치:로얄 캔서 하스피틀 Pharmaceutical compounds
CA2683915A1 (en) 2007-04-13 2008-10-23 Schering Corporation Pyrimidinedione derivatives and methods of use thereof
ES2446419T3 (en) 2007-04-16 2014-03-07 Amgen, Inc Modulators of GPR40 bifenilfenoxi, thiophenyl and substituted acids aminofenilpropanoico
WO2008130951A1 (en) 2007-04-17 2008-10-30 Bristol-Myers Squibb Company Fused heterocyclic 11-beta-hydroxysteroid dehydrogenase type i inhibitors
EP2146979A4 (en) 2007-04-18 2010-11-03 Astrazeneca Ab A new process for the manufacturing of the compound 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1h-indole-5-carbonitrile 701
US8030315B2 (en) 2007-04-19 2011-10-04 Dong-A Pharm. Co., Ltd. DPP-IV inhibitor including beta-amino group, preparation method thereof and pharmaceutical composition containing the same for preventing and treating diabetes or obesity
JP2010524941A (en) 2007-04-20 2010-07-22 シェーリング コーポレイションSchering Corporation Pyrimidinone derivatives and methods for their use
CN101687793B (en) 2007-04-20 2014-05-07 百时美施贵宝公司 Crystal forms of saxagliptin and processes for preparing same
CN102015677A (en) 2007-04-20 2011-04-13 先灵公司 Pyrimidinone derivatives and methods of use thereof
CN101686980A (en) 2007-04-20 2010-03-31 先灵公司 Tetrahydropyrido[4,3-d]pyrimidinone derivatives and methods of use thereof
EP2150109B1 (en) 2007-04-24 2012-09-19 High Point Pharmaceuticals, LLC Pharmaceutical use of substituted amides
EP2154131A4 (en) 2007-04-26 2011-09-21 Pharmafrontier Co Ltd G protein-coupled receptor inhibitor and pharmaceutical product
JP2010159210A (en) 2007-04-26 2010-07-22 Dainippon Sumitomo Pharma Co Ltd Condensed heterocyclic derivative
EP2149550A4 (en) 2007-04-27 2010-08-11 Takeda Pharmaceutical Nitrogen-containing five-membered heterocyclic compound
WO2008136393A1 (en) 2007-04-27 2008-11-13 Ajinomoto Co., Inc. Crystal of lactam compound, and method for production thereof
WO2008137436A1 (en) 2007-05-04 2008-11-13 Bristol-Myers Squibb Company [6,5]-bicyclic gpr119 g protein-coupled receptor agonists
WO2008137435A1 (en) 2007-05-04 2008-11-13 Bristol-Myers Squibb Company [6,6] and [6,7]-bicyclic gpr119 g protein-coupled receptor agonists
KR20080099174A (en) 2007-05-07 2008-11-12 주식회사 머젠스 Naphthoquinone-based pharmaceutical composition for treatment or prevention of diseases involving obesity, diabetes, metabolic syndrome, neuro-degenerative diseases and mitochondria dysfunction diseases
JP2010526807A (en) 2007-05-07 2010-08-05 メルク・シャープ・エンド・ドーム・コーポレイション Treatment with condensed aromatic compounds having anti-diabetic activity
DE102007022565A1 (en) 2007-05-14 2008-11-20 Merck Patent Gmbh heterocyclic indazole derivatives
EP1992620A1 (en) 2007-05-16 2008-11-19 Sanofi-Aventis Arylamide pyrimidone derivatives for the treatment of neurodegenerative diseases
EP1992621A1 (en) 2007-05-16 2008-11-19 Sanofi-Aventis Heteroarylamide-substituted pyrimidone derivatives for the treatment of neurodegenerative diseases
EP1992625A1 (en) 2007-05-16 2008-11-19 Sanofi-Aventis Arylamide pyrimidone compounds
EP1992624A1 (en) 2007-05-16 2008-11-19 Sanofi-Aventis Heteroarylamide pyrimidone compounds
US8236855B2 (en) 2007-05-17 2012-08-07 Case Western Reserve University Methods of treating metabolic disorders
WO2008142859A1 (en) 2007-05-18 2008-11-27 Kowa Company, Ltd. Novel spiro-oxindole compound and pharmaceutical containing the same
CN101754972A (en) 2007-05-18 2010-06-23 百时美施贵宝公司 Crystal structures of SGLT2 inhibitors and processes for preparing same
KR101376432B1 (en) 2007-05-18 2014-05-16 시오노기세이야쿠가부시키가이샤 NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVE HAVING 11 β-HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORY ACTIVITY
RU2498980C2 (en) 2007-05-29 2013-11-20 Сантен Фармасьютикал Ко., Лтд. Novel 1,2,3,4-tetrahydroquinoxaline derivative containing phenyl group as substitute, having sulphonic acid ester structure or sulphonic acid amide structure, and having glucocorticoid receptor binding activity
US7829664B2 (en) 2007-06-01 2010-11-09 Boehringer Ingelheim International Gmbh Modified nucleotide sequence encoding glucagon-like peptide-1 (GLP-1), nucleic acid construct comprising same for production of glucagon-like peptide-1 (GLP-1), human cells comprising said construct and insulin-producing constructs, and methods of use thereof
WO2008145721A3 (en) 2007-06-01 2009-03-12 Thomas Hoeg-Jensen N-terminal modification of polypeptides for protection against degradation by aminopeptidases
CN101687828A (en) 2007-06-04 2010-03-31 诺瓦提斯公司 Thiadiazole derivatives as antidiabetic agents
CA2689909C (en) 2007-06-08 2016-04-05 Ascendis Pharma As Long-acting polymeric prodrugs of exendin
US8299115B2 (en) 2007-06-08 2012-10-30 Debnath Bhuniya Pyrrole-2-carboxamide derivatives as glucokinase activators, their process and pharmaceutical application
US8222285B2 (en) 2007-06-11 2012-07-17 Bristol-Myers Squibb Company 1,3-dihydroxy substituted phenylamide glucokinase activators
EP2158214B1 (en) 2007-06-15 2011-08-17 Zealand Pharma A/S Glucagon analogues
JP2011502958A (en) 2007-06-19 2011-01-27 タケダ サン ディエゴ インコーポレイテッド Glucokinase activation indazole compound
WO2008156174A1 (en) 2007-06-21 2008-12-24 Taisho Pharmaceutical Co., Ltd. Pyrazinamide compound
EP2918586A1 (en) 2007-06-21 2015-09-16 Incyte Corporation Spirocycles as inhibitors of 11-beta hydroxyl steroid dehydrogenase type 1
EP2172453A4 (en) 2007-06-27 2010-12-22 Taisho Pharma Co Ltd COMPOUND HAVING 11 ß-HSD1 INHIBITORY ACTIVITY
EP2170883A1 (en) 2007-06-28 2010-04-07 Merck Frosst Canada Ltd. Substituted fused pyrimidines as antagonists of gpr105 activity
WO2009005672A1 (en) 2007-06-29 2009-01-08 Merck & Co., Inc. Antidiabetic azaindoles and diazaindoles
WO2009003681A1 (en) 2007-07-02 2009-01-08 Santhera Pharmaceuticals (Schweiz) Ag Dpp-iv inhibitors
EP2322620A3 (en) 2007-07-09 2011-08-31 Imperial Innovations Ltd. Analogs of human pancreatic polypeptide and their effects on feeding behaviour
DE102007032349A1 (en) 2007-07-11 2009-01-15 Bayer Healthcare Ag Imidazo, Pyrazolopyrazine and imidazotriazines and their use
WO2009009287A3 (en) 2007-07-12 2009-03-19 Deviris Inc Hormone sensitive lipase modulators and methods of use
WO2009012039A3 (en) 2007-07-13 2009-03-19 Metabasis Therapeutics Inc Crystalline polymorphs
WO2009010416A3 (en) 2007-07-17 2009-03-05 Hoffmann La Roche Inhibitors of 11b-hydroxysteroid dehydrogenase
WO2009012275A9 (en) 2007-07-17 2010-03-11 Bristol-Myers Squibb Company Pyridone gpr119 g protein-coupled receptor agonists
EP2178868A1 (en) 2007-07-18 2010-04-28 Novartis Ag Bicyclic heteroaryl compounds and their use as kinase inhibitors
CA2693169C (en) 2007-07-19 2016-01-12 Metabolex, Inc. N-linked heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders
WO2009014676A1 (en) 2007-07-23 2009-01-29 Merck & Co., Inc. Novel crystalline form of a dihydrochloride salt of a dipeptidyl peptidase-iv inhibitor
JP5215607B2 (en) 2007-07-23 2013-06-19 シーシーアイ株式会社 Peroxisome proliferator-activated receptor (PPAR) alpha ligand agent
WO2009015067A3 (en) 2007-07-25 2009-09-11 Boehringer Ingelheim International Gmbh Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
EP2184277B1 (en) 2007-07-25 2015-07-01 Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China Aryl pyrimidine derivatives, preparation methods and pharmaceutical uses thereof
EP2291373B1 (en) 2008-05-01 2013-09-11 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5301563B2 (en) 2008-05-01 2013-09-25 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β- hydroxy cyclic inhibitors of steroid dehydrogenase 1
CA2723034A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5696037B2 (en) 2008-05-01 2015-04-08 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β- hydroxy cyclic inhibitors of steroid dehydrogenase 1
US8329897B2 (en) 2007-07-26 2012-12-11 Vitae Pharmaceuticals, Inc. Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1
CN101808995A (en) 2007-07-27 2010-08-18 百时美施贵宝公司 Novel glucokinase activators and methods of using same
DE102007035333A1 (en) 2007-07-27 2009-01-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg New substituted Arylsulfonylglycine, their preparation and their use as medicaments
DE102007035334A1 (en) 2007-07-27 2009-01-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg New substituted Arylsulfonylglycine, their preparation and their use as medicaments
JP2010535200A (en) 2007-07-30 2010-11-18 アストラゼネカ・アクチエボラーグAstrazeneca Aktiebolag The new crystalline form of 2-hydroxy-3- [5- (morpholin-4-ylmethyl) pyridin-2-yl]-1h-indole-5-carbonitrile citrate
WO2009019600A3 (en) 2007-08-03 2009-12-30 Dr. Reddy's Laboratories Ltd. Modulation of endogenous ampk levels for the treatment of obesity
EP2183233A1 (en) 2007-08-03 2010-05-12 Betagenon AB Dithiazolidine and thiazolidine derivatives as anticancer agents
EP2020232A1 (en) 2007-08-03 2009-02-04 Zeltia, S.A. N-(1-thiazolyl)-amide derivatives for the treatment of obesity, diabetes and cardiovascular diseases
WO2009020140A1 (en) 2007-08-06 2009-02-12 Dainippon Sumitomo Pharma Co., Ltd. Adamantylurea derivative
FR2919869B1 (en) 2007-08-09 2009-09-25 Sanofi Aventis Sa New derivatives of n, n'-2,4-dianilinopyrimidines, their preparation has as medicines, pharmaceutical compositions including such inhibitors ikk
CA2695583A1 (en) 2007-08-13 2009-02-19 Metabasis Therapeutics, Inc. Novel activators of glucokinase
CA2696288A1 (en) 2007-08-15 2009-02-19 Schering Corporation 6-substituted sulfonyl azabicyclo[3.2.1]octanes useful to inhibit 11.beta.-hydroxysteroid dehydrogenase type-1
JP2010536749A (en) 2007-08-15 2010-12-02 シェーリング コーポレイションSchering Corporation 11β- Useful substituted bicyclic piperidinylmethyl sulfonamide and piperazinyl sulfonamides to inhibit hydroxysteroid dehydrogenase type I
EP2190820B1 (en) 2007-08-15 2013-04-10 Merck Sharp & Dohme Corp. Substituted azepine-sulfonamides useful to inhibit 11beta-hydroxysteroid dehydrogenase type-1
WO2009026346A1 (en) 2007-08-20 2009-02-26 Targegen Inc. Thiazolidine compounds, and methods of making and using same
JP5736098B2 (en) 2007-08-21 2015-06-17 アッヴィ・インコーポレイテッド The pharmaceutical composition for treating a central nervous system disorder
JP5313246B2 (en) 2007-08-21 2013-10-09 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. Dipeptidyl peptidase -iv heterocyclyl compounds as inhibitors for the treatment or prevention of diabetes
JP4809931B2 (en) 2007-08-23 2011-11-09 セラコス・インコーポレイテッドTheracos, Inc. Benzyl benzene derivatives and methods of use thereof
WO2009026657A8 (en) 2007-08-29 2009-05-28 Univ Sydney Flavonoid ppar agonists
WO2009026658A1 (en) 2007-08-29 2009-03-05 The University Of Sydney Ppar agonists
US20090105480A1 (en) 2007-08-30 2009-04-23 Ulrike Bromberger Process for the preparation of a dpp-iv inhibitor
US20090062369A1 (en) 2007-08-31 2009-03-05 Joaquim Trias Use of secretory phospholipase a2 (spla2) inhibitors to decrease spla2 levels
CN101796035B (en) 2007-08-31 2013-12-04 韩诺生物制约株式会社 1,3,5-triazine-2,4,6-triamine compound or pharmaceutical acceptable salt thereof, and pharmaceutical composition comprising the same
DE102007042154A1 (en) 2007-09-05 2009-03-12 Boehringer Ingelheim Pharma Gmbh & Co. Kg Arylsulfonylaminomethyphosphonsäure derivatives, their preparation and their use as medicaments
CN101868476B (en) 2007-09-05 2015-02-25 诺沃-诺迪斯克有限公司 Glucagon-like peptide-1 derivatives and their pharmaceutical use
EP2190873B1 (en) 2007-09-05 2015-07-22 Novo Nordisk A/S Truncated glp-1 derivatives and their therapeutical use
EP2190460B1 (en) 2007-09-05 2014-12-17 Novo Nordisk A/S Peptides derivatized with a-b-c-d- and their therapeutical use
EP2188299B1 (en) 2007-09-06 2017-10-25 Ohr Pharmaceutical, Inc. Compounds for treating diabetes
WO2009035540A3 (en) 2007-09-07 2009-09-24 Ipsen Pharma S.A.S. Analogues of exendin-4 and exendin-3
DE102007042754A1 (en) 2007-09-07 2009-03-12 Bayer Healthcare Ag Substituted 6-Phenylnikotinsäuren and their use
JP2010539152A (en) 2007-09-10 2010-12-16 プロシディオン・リミテッドProsidion Limited Compounds for the treatment of metabolic disorders
US8389514B2 (en) 2007-09-11 2013-03-05 Kyorin Pharmaceutical Co., Ltd. Cyanoaminoquinolones and tetrazoloaminoquinolones as GSK-3 inhibitors
EP2036923A1 (en) 2007-09-11 2009-03-18 Novo Nordisk A/S Improved derivates of amylin
EP2200635A1 (en) 2007-09-11 2010-06-30 Novo Nordisk A/S Mixture comprising an amylin peptide and a protracted insulin
EP2203459B1 (en) 2007-09-12 2016-03-16 Kyorin Pharmaceutical Co., Ltd. Spirocyclic aminoquinolones as gsk-3 inhibitors
US7659313B2 (en) 2007-09-13 2010-02-09 Gateway Health Alliances, Inc. Methods and related compositions using specific indanes to reduce weight and inhibit lipase, α-amylase and α-glucosidase activity in mammals
JP5371988B2 (en) 2007-09-14 2013-12-18 メタボリック ソリューションズ ディベロップメント カンパニー, エルエルシー Thiazolidinedione analogs for the treatment of high blood pressure
WO2009038204A1 (en) 2007-09-17 2009-03-26 Pharma Frontier Co., Ltd. Novel long-chain fatty acid derivative compound and g-protein-coupled receptor agonist containing the compound as active ingredient
WO2009038064A1 (en) 2007-09-19 2009-03-26 Institute Of Medicinal Molecular Design, Inc. Heterocyclic derivative having inhibitory activity on type-i 11β-hydroxysteroid dehydrogenase
CA2697551C (en) 2007-09-20 2013-03-12 Irm Llc Piperidine derivatives as modulators of gpr119 activity
GB2465132B (en) 2007-09-21 2012-06-06 Lupin Ltd Compounds as dipeptidyl peptidase IV (DPP IV) inhibitors
CA2699718C (en) 2007-09-21 2014-05-27 Array Biopharma Inc. Pyridin-2-yl-amino-1, 2, 4-thiadiazole derivatives as glucokinase activators for the treatment of diabetes mellitus
WO2009039944A1 (en) 2007-09-21 2009-04-02 Sanofi-Aventis Phenothiazine derivative having a double bond, method for the production thereof, and use thereof as a pharmaceutical
KR20100061692A (en) 2007-09-21 2010-06-08 사노피-아벤티스 (carboxylalkylene-phenyl)-phenyl-oxalamides, method for the production thereof, and use of same as a medicament
CA2700025A1 (en) 2007-09-21 2009-04-02 Sanofi-Aventis (cyclopropylphenyl)phenyloxamides, method for the production thereof, and use of same as a medicament
KR20090031122A (en) 2007-09-21 2009-03-25 주식회사 중외제약 Compounds containing indazole frameworks, preparing method thereof and pharmaceutical composition containing thereof
US8143280B2 (en) 2007-09-27 2012-03-27 Hoffmann-La Roche Inc. Glucocorticoid receptor antagonists
WO2009045831A1 (en) 2007-09-28 2009-04-09 Smithkline Beecham Corporation Glycogen phosphorylase inhibitor compound and pharmaceutical composition thereof
US20100305207A1 (en) 2007-09-28 2010-12-02 Pierette Banker Glycogen phosphorylase inhibitor compound and pharmaceutical composition thereof
US8119658B2 (en) 2007-10-01 2012-02-21 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
JP5580201B2 (en) 2007-10-08 2014-08-27 アドビヌス・セラピューティクス・プライベート・リミテッド Acetamide derivatives as glucokinase activators, their preparation and pharmaceutical applications
US8420642B2 (en) 2007-10-09 2013-04-16 Merck Patent Gmbh Pyridine derivatives useful as glucokinase activators
WO2009047240A1 (en) 2007-10-09 2009-04-16 Smithkline Beecham Corporation Indole derivatives useful as ppar activators
ES2403105T3 (en) 2007-10-09 2013-05-14 Merck Patent Gmbh Derivatives of N- (pyrazol-3-yl) -benzamide as glucokinase activators
JP5591706B2 (en) 2007-10-10 2014-09-17 アムジエン・インコーポレーテツド Substituted biphenyl gpr40 regulators
DE102007048716A1 (en) 2007-10-11 2009-04-23 Merck Patent Gmbh Imidazo [1,2-a] pyrimidine derivatives
WO2009046606A1 (en) 2007-10-11 2009-04-16 Shanghai Institute Of Materia Medica, Cas Pyrimidinyl-propionic acid derivatives and their use as ppar agonists
WO2009049222A1 (en) 2007-10-12 2009-04-16 Curedm, Inc. Compositions and methods of using the human proislet peptide receptor
GB0720389D0 (en) 2007-10-18 2008-11-12 Prosidion Ltd G-Protein Coupled Receptor Agonists
GB0720390D0 (en) 2007-10-18 2007-11-28 Prosidion Ltd G-Protein coupled receptor agonists
WO2009055331A3 (en) 2007-10-22 2009-07-30 Schering Corp Bicyclic heterocycle derivatives and their use as modulators of the activity of gpr119
CN101417999A (en) 2007-10-25 2009-04-29 上海恒瑞医药有限公司 Piperazines derivates, preparation method thereof and application thereof in medicine
EP2508503A1 (en) 2007-10-26 2012-10-10 Japan Tobacco, Inc. Spiro compounds and pharmaceutical use thereof
JP5542058B2 (en) 2007-10-29 2014-07-09 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. Antidiabetic tricyclic compound
EP2217701B9 (en) 2007-10-30 2015-02-18 Indiana University Research and Technology Corporation Glucagon antagonists
CA2702289A1 (en) 2007-10-30 2009-05-07 Indiana University Research And Technology Corporation Compounds exhibiting glucagon antagonist and glp-1 agonist activity
US8309580B2 (en) 2007-11-01 2012-11-13 Takeda Pharmaceutical Company Limited Heterocyclic compound
CA2704803C (en) 2007-11-05 2017-04-11 Denis Carniato 7-azaindole derivatives as selective 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors
WO2009061498A1 (en) 2007-11-07 2009-05-14 Vitae Pharmaceuticals, Inc. CYCLIC UREA INHIBITORS OF 11β -HYDROXYSTEROID DEHYDROGENASE 1
EP2217621B1 (en) 2007-11-08 2015-04-22 Novo Nordisk A/S Insulin derivative
JP5301456B2 (en) 2007-11-12 2013-09-25 Msd株式会社 Heteroaryloxy quinazoline derivatives
EP2058308A1 (en) 2007-11-12 2009-05-13 Merck Sante Benzimidazoledihydrothiadiazinone derivatives used as fructose-1,6-biphosphatase inhibitors and pharmaceutical compositions containing same.
EP2220048B1 (en) 2007-11-16 2017-01-25 Boehringer Ingelheim International GmbH Aryl- and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use
CA2705947C (en) 2007-11-16 2016-08-09 Rigel Pharmaceuticals, Inc. Carboxamide, sulfonamide and amine compounds for metabolic disorders
US20090221595A1 (en) 2007-11-26 2009-09-03 Nurit Perlman Crystalline form of sitagliptin
WO2009070497A1 (en) 2007-11-28 2009-06-04 Smithkline Beecham Corporation SEH AND 11 β-HSD1 INHIBITORS AND THEIR USE
WO2009069736A1 (en) 2007-11-28 2009-06-04 Kyowa Hakko Kirin Co., Ltd. Nitrogenated compound
CN101450963B (en) 2007-11-30 2012-03-14 中国科学院上海药物研究所 Gourd alkane type triterpene saponin compounds, medicament composition thereof as well as preparation method and application thereof
EP2227452A2 (en) 2007-11-30 2010-09-15 F. Hoffmann-La Roche AG Pyridine compounds
WO2009068531A3 (en) 2007-11-30 2010-09-10 Novartis Ag Adamantyl o-glucuronide derivatives as inhibitors of dipeptidyl peptidase iv for the treatment of diabetes
US7973051B2 (en) 2007-11-30 2011-07-05 Hoffman-La Roche Inc. Aminothiazoles as FBPase inhibitors for diabetes
WO2009071895A1 (en) 2007-12-04 2009-06-11 Ucb Pharma S.A. Fused thiazole and thiophene derivatives as kinase inhibitors
WO2009071890A1 (en) 2007-12-04 2009-06-11 Ucb Pharma S.A. Tricyclic kinase inhibitors
WO2009070873A1 (en) 2007-12-04 2009-06-11 Merck Frosst Canada Ltd. Substituted 2-naphthoic acids as antagonists of gpr105 activity
GB0723747D0 (en) 2007-12-04 2008-12-31 Ucb Pharma Sa Therapeutic agents
WO2009072581A1 (en) 2007-12-05 2009-06-11 Aska Pharmaceutical Co., Ltd. Lactam compound or salt thereof, and ppar activator
EP2229368A1 (en) 2007-12-11 2010-09-22 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11beta-hydroxysteroid dehydrogenase 1
ES2382579T3 (en) 2007-12-11 2012-06-11 Cadila Healthcare Limited Peptidomimetics glucagon antagonist activity and agonist of GLP-1
GB0724251D0 (en) 2007-12-12 2008-02-06 Univ Edinburgh Therapeutic compounds and their use
ES2553340T3 (en) 2007-12-12 2015-12-07 Rigel Pharmaceuticals, Inc. Carboxamide compounds, and amine sulfonamide for metabolic disorders
WO2009076550A1 (en) 2007-12-13 2009-06-18 Theracos, Inc. Benzylphenyl cyclohexane derivatives and methods of use
WO2009080032A1 (en) 2007-12-20 2009-07-02 Fertin Pharma A/S Compressed chewing gum comprising a systemically active small peptide
DE102007061757A1 (en) 2007-12-20 2009-06-25 Bayer Healthcare Ag Substituted 2-phenylpyrimidine-5-carboxylic acids and their use
WO2009080024A1 (en) 2007-12-20 2009-07-02 Fertin Pharma A/S Compressed chewing gum comprising an incretin mimetic
KR101133772B1 (en) 2007-12-20 2012-04-24 주식회사 엘지생명과학 Glucokinase activators and pharmaceutical compositions containing the same as an active ingredient
DE102007061756A1 (en) 2007-12-20 2009-06-25 Bayer Healthcare Ag Substituted 4-aminopyrimidine-5-carboxylic acids and their use
WO2009082134A3 (en) 2007-12-21 2009-09-24 Lg Life Sciences, Ltd. Dipeptidyl peptidase-iv inhibiting compounds, methods of preparing the same, and pharmaceutical compositions containing the same as active agent
WO2009080821A3 (en) 2007-12-21 2010-01-14 Giuliani International Limited Multitarget compounds active at a ppar and cannabinoid receptor
WO2009081782A1 (en) 2007-12-25 2009-07-02 Banyu Pharmaceutical Co., Ltd. N-pyrazole-2-pyridinecarboxamide derivative
KR20100101165A (en) 2007-12-26 2010-09-16 사노피-아벤티스 Cyclic pyridyl-n-(1,3,4)-thiadiazol-2-yl-benzene sulfonamides, processes for their preparation and their use as pharmaceuticals
CN101468988A (en) 2007-12-26 2009-07-01 上海恒瑞医药有限公司 Piperazine derivative, preparation thereof and use thereof in medicine
WO2009084531A1 (en) 2007-12-27 2009-07-09 Kissei Pharmaceutical Co., Ltd. Monosebacate of pyrazole derivative
WO2009084497A1 (en) 2007-12-28 2009-07-09 Dainippon Sumitomo Pharma Co., Ltd. Methyl-substituted piperidine derivative
WO2009083553A1 (en) 2007-12-31 2009-07-09 Rheoscience A/S Azine compounds as glucokinase activators
GB0800035D0 (en) 2008-01-02 2008-02-13 Glaxo Group Ltd Compounds
JP5451637B2 (en) 2008-01-07 2014-03-26 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β- hydroxysteroid dehydrogenase type 1 lactam inhibitors
EP2231687A4 (en) 2008-01-10 2012-11-14 Sun Pharma Advanced Res Co Ltd Novel derivatives of acyl cyanopyrrolidines
GB0800383D0 (en) 2008-01-10 2008-02-20 Univ Strathclyde Weight reducing compounds
CN101909629A (en) 2008-01-15 2010-12-08 伊莱利利公司 Crystalline (R)-2-(4-cyclopropanesulphonyl-phenyl)-N-pyrazin-2-yl-3-(tetrahydropyran-4-yl)-propionamide
JP5204849B2 (en) 2008-01-17 2013-06-05 田辺三菱製薬株式会社 Combination therapy consisting Sglt inhibitor and dpp4 inhibitors
US20100022590A1 (en) 2008-01-17 2010-01-28 Biovitrum Ab (Publ.) Novel compounds
JP5287730B2 (en) 2008-01-18 2013-09-11 アステラス製薬株式会社 Phenylacetamide derivatives
CA2712500A1 (en) 2008-01-24 2009-07-30 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US20090238879A1 (en) 2008-01-24 2009-09-24 Northwestern University Delivery scaffolds and related methods of use
DK2231640T3 (en) 2008-01-24 2012-07-16 Merck Patent Gmbh Beta-amino acid derivatives for the treatment of diabetes
JP5640208B2 (en) 2008-01-24 2014-12-17 パナセア バイオテック リミテッド Novel heterocyclic compound
CA2713367A1 (en) 2008-01-28 2009-09-17 Sanofi-Aventis Derivatives of tetrahydroquinoxaline urea, preparation thereof and therapeutic application thereof
EP2085400A1 (en) 2008-01-29 2009-08-05 Sanofi-Aventis Substituted heteroarylamide oxazepinopyrimidone derivatives
EP2090578A1 (en) 2008-01-29 2009-08-19 Sanofi-Aventis Substituted arylamide diazepinopyrimidone derivatives for the treatment of neurodegenerative diseases caused by abnormal activity of GSK3-beta
EP2090579A1 (en) 2008-01-29 2009-08-19 Sanofi-Aventis Substituted heteroarylamide diazepinopyrimidone derivatives
EP2085399A1 (en) 2008-01-29 2009-08-05 Sanofi-Aventis substituted arylamide oxazepinopyrimidone derivatives
WO2009096503A1 (en) 2008-01-31 2009-08-06 Daiichi Sankyo Company, Limited Benzyl phenyl glucopyranoside derivative
WO2009100130A1 (en) 2008-02-04 2009-08-13 Mercury Therapeutics, Inc. Ampk modulators
EP2239253B1 (en) 2008-02-06 2013-06-19 Daiichi Sankyo Company, Limited Novel phenylpyrrole derivative
WO2009099172A1 (en) 2008-02-07 2009-08-13 Takeda Pharmaceutical Company Limited Pharmaceutical product
WO2009099171A1 (en) 2008-02-07 2009-08-13 Takeda Pharmaceutical Company Limited Pharmaceutical product
CA2714532A1 (en) 2008-02-11 2009-08-20 Vitae Pharmaceuticals, Inc. 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
WO2009102226A1 (en) 2008-02-12 2009-08-20 Adamed Sp. Z O.O. Malonic acid salt of 5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]- 2,4-thiazolidinedione
US8263630B2 (en) 2008-02-12 2012-09-11 Bristol-Myers Squibb Company 1,2,3-triazoles as 11-beta hydroxysteroid dehydrogenase type I inhibitors
JP5538239B2 (en) 2008-02-12 2014-07-02 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Urea derivatives of benzomorphan and related skeleton, pharmaceutical and use thereof containing such compounds
JP2011511820A (en) 2008-02-13 2011-04-14 サノフィ−アベンティス Novel aromatic fluoro glycoside derivatives, agents and their use comprising the compounds
CA2715290A1 (en) 2008-02-15 2009-08-20 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CN102006870A (en) 2008-02-22 2011-04-06 Irm责任有限公司 Compounds and compositions as modulators of gpr119 activity
CA2716332A1 (en) 2008-02-22 2009-08-27 Irm Llc Compounds and compositions as modulators of gpr119 activity
US20110190263A1 (en) 2008-02-22 2011-08-04 Irm Llc Compounds and compositions as modulators of gpr119 activity
CA2716599A1 (en) 2008-02-25 2009-09-03 Lars Thore Burgdorf Glucokinase activators
KR100864584B1 (en) 2008-02-25 2008-10-24 성균관대학교산학협력단 Exendin derivative linked biotin, method for the preparation thereof and pharmaceutical composition comprising the same
GB0803494D0 (en) 2008-02-26 2008-04-02 Sterix Ltd Compound
US8383629B2 (en) 2008-02-27 2013-02-26 Vitae Pharmaceuticals, Inc. Inhibitors of 11β-hydroxysteroid dehydrogenase type 1
WO2009106561A1 (en) 2008-02-27 2009-09-03 Biovitrum Ab (Publ) Pyrazine compounds for treating gpr119 related disorders
WO2009106565A1 (en) 2008-02-27 2009-09-03 Biovitrum Ab (Publ) Agonists of gpr119
WO2009106209A1 (en) 2008-02-27 2009-09-03 Merck Patent Gmbh Carboxamide-heteroaryl derivatives for the treatment of diabetes
FR2928149B1 (en) 2008-02-29 2011-01-14 Sanofi Aventis Compounds derived from azetidines, their preparation and their therapeutic application
ES2475209T3 (en) 2008-03-01 2014-07-10 Merck Patent Gmbh Amides of 5-oxo-2,3,4,5-tetrahydro-benzo [b] oxepin-4-carboxlico and amides of 2,3-dihydrobenzo [b] oxepin-4-carboxlico treatment and prevention of diabetes types 1 and 2.
WO2009109998A1 (en) 2008-03-03 2009-09-11 Lupin Limited Novel protein tyrosine phosphatase - ib inhibitors
WO2009109999A1 (en) 2008-03-03 2009-09-11 Lupin Limited Novel protein tyrosine phosphatase - ib inhibitors
EP2247292B1 (en) 2008-03-05 2017-04-12 Merck Patent GmbH Pyridopyrazinones derivatives insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes
WO2009109259A1 (en) 2008-03-05 2009-09-11 Merck Patent Gmbh Pyrazinone derivatives as insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes
JP5586484B2 (en) 2008-03-05 2014-09-10 ナショナル ヘルス リサーチ インスティテューツ Pyrrolidine derivatives
KR101616140B1 (en) 2008-03-05 2016-04-27 다케다 야쿠힌 고교 가부시키가이샤 Heterocyclic compound
EP2260017A1 (en) 2008-03-06 2010-12-15 Amgen, Inc Conformationally constrained carboxylic acid derivatives useful for treating metabolic disorders
ES2567451T3 (en) 2008-03-07 2016-04-22 Vtv Therapeutics Llc Oxadiazoantraceno compounds for the treatment of diabetes
WO2009145814A9 (en) 2008-03-10 2010-05-14 Vertex Pharmaceuticals Incorporated Pyrimidines and pyridines useful as inhibitors of protein kinases
US20110009433A1 (en) 2008-03-10 2011-01-13 Dainippon Sumitomo Pharma Co., Ltd. Bicyclic pyrrole compound
GB0804685D0 (en) 2008-03-13 2008-04-16 Univ Edinburgh Therapeutic compounds and their use
CA2718038A1 (en) 2008-03-14 2009-09-17 Exelixis, Inc. Azabicyclo [3.2.1] octyl derivatives as 11 beta-hsd1 modulators
WO2009117421A3 (en) 2008-03-17 2010-01-07 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
JP5538356B2 (en) 2008-03-18 2014-07-02 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β- hydroxysteroid dehydrogenase type 1 inhibitors
FR2928836B1 (en) 2008-03-21 2011-08-26 Servier Lab DOSAGE FORM Scored a modified release of the active ingredient
KR101235934B1 (en) 2008-03-27 2013-02-21 일라이 릴리 앤드 캄파니 Glucagon receptor antagonists
US20090247532A1 (en) 2008-03-28 2009-10-01 Mae De Ltd. Crystalline polymorph of sitagliptin phosphate and its preparation
CN102026636B (en) 2008-03-31 2014-07-16 赛马拜制药公司 Oxymethylene aryl compounds and uses thereof
ES2563553T3 (en) 2008-04-01 2016-03-15 Novo Nordisk A/S Insulin-albumin conjugates
FR2929615B1 (en) 2008-04-02 2010-12-17 Tfchem Compounds C-aryl glycosides for the treatment of diabetes and obesity.
KR101775942B1 (en) 2008-04-03 2017-09-07 베링거 인겔하임 인터내셔날 게엠베하 DPP-IV Inhibitor combined with a further antidiabetic agent, tablets comprising such formulations, their use and process for their preparation
DE102008017590A1 (en) 2008-04-07 2009-10-08 Merck Patent Gmbh Glucopyranosidderivate
CA2720950A1 (en) 2008-04-07 2009-10-15 Irm Llc Compounds and compositions as modulators of gpr119 activity
WO2009125434A3 (en) 2008-04-07 2010-04-15 Cadila Healthcare Limited Oxime derivatives, process for their preparation, pharmaceutical composition containing the same and medicinal use thereof
JP5528348B2 (en) 2008-04-10 2014-06-25 武田薬品工業株式会社 Fused ring compounds and their applications
CN101998853B (en) 2008-04-11 2015-02-11 默克专利有限公司 Thienopyridone derivatives as AMP-activated protein kinase (AMPK) activators
EP2297129B1 (en) 2008-04-14 2013-07-24 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
WO2009128558A1 (en) 2008-04-15 2009-10-22 日本ケミファ株式会社 Activator for peroxisome proliferator-activated receptor
US8258134B2 (en) 2008-04-16 2012-09-04 Hoffmann-La Roche Inc. Pyridazinone glucokinase activators
EP2266983B1 (en) 2008-04-16 2013-06-05 Takeda Pharmaceutical Company Limited Nitrogenated 5-membered heterocyclic compound
US8354382B2 (en) 2008-04-16 2013-01-15 Kissei Pharmaceutical Co., Ltd. Hemifumarate of a pyrazole derivative
US7741327B2 (en) 2008-04-16 2010-06-22 Hoffmann-La Roche Inc. Pyrrolidinone glucokinase activators
DE102008019838A1 (en) 2008-04-19 2009-12-10 Boehringer Ingelheim International Gmbh New Arylsulfonylglycin derivatives, their preparation and their use as medicaments
CN102066335A (en) 2008-04-22 2011-05-18 阿斯利康(瑞典)有限公司 Substituted pyrimidin-5-carboxamides 281
CA2721750A1 (en) 2008-04-22 2009-10-29 Vitae Pharmaceuticals, Inc. Carbamate and urea inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CN101565408A (en) 2008-04-25 2009-10-28 国家新药筛选中心;中国科学院上海药物研究所 Receptor signal transduction positive modulator, preparation method and purpose thereof
RU2565070C2 (en) 2008-04-28 2015-10-20 Киорин Фармасьютикал Ко., Лтд. Cyclopentylacrylamide derivative
WO2009133099A3 (en) 2008-04-28 2010-04-29 Novo Nordisk A/S Insulin precursors for oral diabetes treatment
US8124636B2 (en) 2008-04-30 2012-02-28 Hoffmann-La Roche Inc. Imidazolidinone derivatives as 11B-HSD1 inhibitors
DK2280952T3 (en) 2008-05-05 2012-07-23 Merck Patent Gmbh Thienopyridinonderivater as AMP-activated protein kinase (AMPK) activators
ES2432383T3 (en) 2008-05-05 2013-12-03 Merck Patent Gmbh Thiazole derivatives nip-as inhibitors of 11-beta-hydroxysteroid dehydrogenase
WO2009135673A8 (en) 2008-05-09 2010-02-18 Andrea Balsari Compounds with glycidic structure active in the therapy of systemic and local inflammation
WO2009139340A1 (en) 2008-05-12 2009-11-19 武田薬品工業株式会社 Pyrazole compound
EP2288596B1 (en) 2008-05-13 2016-11-30 Boehringer Ingelheim International GmbH Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use
CN102026641A (en) 2008-05-14 2011-04-20 株式会社三和化学研究所 Pharmaceutical preparation comprising DPP-IV inhibitor and other diabetes therapeutic agent in concomitant or combined form
KR20110018366A (en) 2008-05-16 2011-02-23 다케다 샌디에고, 인코포레이티드 Glucokinase activators
CA2724294A1 (en) 2008-05-16 2009-11-19 Schering Corporation Glucagon receptor antagonists, compositions, and methods for their use
CA2724426A1 (en) 2008-05-19 2009-11-26 Schering Corporation Bicyclic heterocycle derivatives and use thereof as gpr119 modulators
US8188098B2 (en) 2008-05-19 2012-05-29 Hoffmann-La Roche Inc. GPR119 receptor agonists
US20090291982A1 (en) 2008-05-22 2009-11-26 Astrazeneca Ab New Substituted Oxindole Derivative 352
ES2423793T3 (en) 2008-05-26 2013-09-24 Genfit PPAR agonist compounds, preparation and uses for treating diabetes and / or dyslipidemia
WO2009154697A3 (en) 2008-05-28 2010-03-18 Massachusetts Institute Of Technology Disc-1 pathway activators in the control of neurogenesis
US20110086074A1 (en) 2008-06-02 2011-04-14 Dr. Reddy's Laboratories Ltd. Combinations of niacin and an oxicam
CA2725316A1 (en) 2008-06-02 2009-12-10 Banyu Pharmaceutical Co., Ltd. Novel isoxazole derivative
WO2009147121A1 (en) 2008-06-02 2009-12-10 Smithkline Beecham Corporation Carboxyl substituted indoles for use as ppar alpha modulators
WO2009149148A9 (en) 2008-06-03 2010-04-08 Trustees Of Tufts College Long-acting glp-1 derivatives, and methods of treating cardiac dysfunction
JP2011523561A (en) 2008-06-04 2011-08-18 アムジエン・インコーポレーテツド Fgf21 mutants and their use
WO2009149139A8 (en) 2008-06-06 2011-02-24 Boehringer Ingelheim International Gmbh Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
EP2288607B1 (en) 2008-06-09 2014-09-24 Sanofi Sulfonamides with heterocycle and oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals
CA2727373A1 (en) 2008-06-09 2009-12-17 Sanofi-Aventis Annelated n-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals
EP2288605B1 (en) 2008-06-09 2014-06-25 Sanofi Annelated pyrrolidin sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals
WO2009150144A1 (en) 2008-06-10 2009-12-17 Inovacia Ab New gpr119modulators
EP2288375B1 (en) 2008-06-13 2012-04-25 Eli Lilly And Company Pegylated insulin lispro compounds
DK2285786T3 (en) 2008-06-16 2013-11-04 Merck Patent Gmbh Quinoxalinedione derivatives
EP2300037B1 (en) 2008-06-17 2016-03-30 Indiana University Research and Technology Corporation Glucagon/glp-1 receptor co-agonists
CA2727161A1 (en) 2008-06-17 2009-12-23 Indiana University Research And Technology Corporation Glucagon analogs exhibiting enhanced solubility and stability physiological ph buffers
WO2009153960A1 (en) 2008-06-17 2009-12-23 大塚化学株式会社 Glycosylated glp-1 peptide
KR20110026481A (en) 2008-06-20 2011-03-15 메타볼렉스, 인코포레이티드 Aryl gpr119 agonists and uses thereof
JP5400878B2 (en) 2008-06-24 2014-01-29 アイアールエム・リミテッド・ライアビリティ・カンパニーIrm,Llc Compounds and methods for modulating G protein-coupled receptor
EP2138492A1 (en) 2008-06-26 2009-12-30 Sanofi-Aventis Substituted pyrimidin-4-one derivatives
EP2138485A1 (en) 2008-06-26 2009-12-30 sanofi-aventis Substituted N-Oxide pyrazine derivatives
EP2138498A1 (en) 2008-06-26 2009-12-30 sanofi-aventis Substituted tricyclic derivatives against neurodegenerative diseases
EP2138494A1 (en) 2008-06-26 2009-12-30 Sanofi-Aventis Substituted alkyl pyrimidin-4-one derivatives
EP2138495A1 (en) 2008-06-26 2009-12-30 sanofi-aventis Substituted pyrimido[2,1-a]isoquinolin-4-one derivatives
EP2138493A1 (en) 2008-06-26 2009-12-30 Sanofi-Aventis Substituted pyrimidone derivatives
EP2138488A1 (en) 2008-06-26 2009-12-30 sanofi-aventis 4-(pyridin-4-yl)-1H-[1,3,5]triazin-2-one derivatives as GSK3-beta inhibitors for the treatment of neurodegenerative diseases
GB0812031D0 (en) 2008-07-01 2008-08-06 7Tm Pharma As Thiazole derivatives
EP2650299A1 (en) 2008-07-03 2013-10-16 Ratiopharm GmbH Crystalline salts of sitagliptin
WO2010006214A1 (en) 2008-07-09 2010-01-14 Ambrx, Inc. Fgf-21 neutralizing antibodies and their uses
GB0812641D0 (en) 2008-07-10 2008-08-20 Prosidion Ltd Compounds
GB0812649D0 (en) 2008-07-10 2008-08-20 Prosidion Ltd Compounds
GB0812648D0 (en) 2008-07-10 2008-08-20 Prosidion Ltd Compounds
GB0812642D0 (en) 2008-07-10 2008-08-20 Prosidion Ltd Compounds
KR20110036609A (en) 2008-07-10 2011-04-07 프로시디온 리미티드 Piperidinyl gpcr agonists
JP2011527332A (en) 2008-07-10 2011-10-27 プロシディオン・リミテッドProsidion Limited Piperidine gpcr agonist
EP2331503B1 (en) 2008-07-11 2013-08-21 Irm Llc 4-phenoxymethylpiperidines as modulators of gpr119 activity
US8501940B2 (en) 2008-07-15 2013-08-06 Hoffmann-La Roche Inc. Tetrahydrocinnoline derivatives
EP2147910A1 (en) 2008-07-15 2010-01-27 Pronova BioPharma Norge AS Novel lipid compounds
WO2010009208A1 (en) 2008-07-16 2010-01-21 Schering Corporation Bicyclic heterocycle derivatives and methods of use thereof
EP2313395B1 (en) 2008-07-16 2012-12-19 Bristol-Myers Squibb Company Pyridone and pyridazone analogues as gpr119 modulators
CA2730610A1 (en) 2008-07-16 2010-01-21 Schering Corporation Bicyclic heterocycle derivatives and their use as gpcr modulators
CA2730593A1 (en) 2008-07-16 2010-01-21 Schering Corporation Bicyclic heterocycle derivatives and use thereof as gpr119 modulators
CN102112483A (en) 2008-07-17 2011-06-29 莱西肯医药有限公司 Solid forms of (2s, 3r, 4r, 5s, 6r)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(methylthio)tetrahydro-2h-pyran-3, 4, 5-triol and methods of their use
EP2324017B1 (en) 2008-07-25 2014-12-31 Boehringer Ingelheim International GmbH INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1
JP5846909B2 (en) 2008-07-25 2016-01-20 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 1,1'-di-adamantyl carboxylic acid, pharmaceutical and use thereof containing such compounds
WO2010011917A8 (en) 2008-07-25 2010-04-22 Glaxosmithkline Llc sEH AND 11β-HSD1 DUAL INHIBITORS
CN102137836B (en) 2008-07-28 2015-08-26 赛丹思科大学 Compounds for treating a metabolic disease
CA2732266A1 (en) 2008-07-28 2010-02-04 Emory University Treating various disorders using trkb agonists
JP2011529483A (en) 2008-07-29 2011-12-08 ファイザー・インク Fluorinated heteroaryl
JP2011529897A (en) 2008-07-30 2011-12-15 グラクソスミスクライン エルエルシー Use a compound
JP2011529903A (en) 2008-07-30 2011-12-15 オンコセラピー・サイエンス株式会社 Benzimidazole derivatives and glycogen synthase kinase-3β inhibitor containing the same
EP2149553B1 (en) 2008-08-01 2011-10-19 Centre National de la Recherche Scientifique 3', 6-substituted indirubins and their biological applications
WO2010014771A1 (en) 2008-08-01 2010-02-04 Ore Pharmaceuticals Inc. Romazarit for treating metabolic diseases
JP2011529955A (en) 2008-08-04 2011-12-15 アストラゼネカ アクチボラグ Therapeutic agent 414
EP2990037A1 (en) 2008-08-06 2016-03-02 Boehringer Ingelheim International GmbH Treatment for diabetes in patients inappropriate for metformin therapy
US8999940B2 (en) 2008-08-07 2015-04-07 Ipsen Pharma S.A.S. Analogues of glucose-dependent insulinotropic polypeptide (GIP) modified at N-terminal
KR20130133104A (en) 2008-08-07 2013-12-05 입센 파마 에스.에이.에스 Glucose-dependent insulinotropic polypeptide analogues
DK2320923T3 (en) 2008-08-07 2015-03-02 Ipsen Pharma Sas Truncated analogues of glucose-dependent insulinotropic polypeptide
WO2010016936A1 (en) 2008-08-07 2010-02-11 Ipsen Pharma S.A.S. Pharmaceutical compositions of analogues of glucose-dependent insulinotropic polypeptide
KR20110043686A (en) 2008-08-07 2011-04-27 입센 파마 에스.에이.에스 Analogues of glucose-dependent insulinotropic polypeptide
WO2010018438A3 (en) 2008-08-11 2011-01-20 Hetero Research Foundation Tetrazole glycosides
WO2010018435A1 (en) 2008-08-11 2010-02-18 Hetero Research Foundation Amide glycosides
WO2010019828A1 (en) 2008-08-13 2010-02-18 Metabasis Therapeutics, Inc. Glucagon receptor antagonists
CA2733646A1 (en) 2008-08-15 2010-02-18 Banyu Pharmaceutical Co., Ltd. Acetyl pyrrolidinyl indole derivative

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO2012010413A1 *

Also Published As

Publication number Publication date Type
CN103080063A (en) 2013-05-01 application
JP2013535410A (en) 2013-09-12 application
KR20130095255A (en) 2013-08-27 application
US20120004166A1 (en) 2012-01-05 application
WO2012010413A1 (en) 2012-01-26 application
CA2804110A1 (en) 2012-01-26 application

Similar Documents

Publication Publication Date Title
WO2007093364A1 (en) Azacyclyl-substituted aryldihydroisoquinolinones, process for their preparation and their use as medicaments
WO2007039177A2 (en) Phenyl- and pyridinyl- 1, 2 , 4 - oxadiazolone derivatives, processes for their preparation and their use as pharmaceuticals
WO2007039172A1 (en) Phenyl- and pyridyl-i, 2 , 4 -oxadiazolone derivatives with phenyl group, processes for their preparation and their use as pharmaceuticals
WO2007042178A1 (en) Diacyl indazol derivatives as lipase and phospholipase inhibitors
WO2011078370A1 (en) Novel parabanic acid derivative and drug having the same as active ingredient
WO2007131622A1 (en) Phenylamino-benzoxazole substituted carboxylic acids, method for their production and use thereof as medicaments
WO2007131620A1 (en) 4,5-diphenyl-pyrimidinyl-amino substituted carboxylic acids, method for the production and use thereof as medicaments
WO2007131619A1 (en) 4,5-diphenyl-pyrimidinyl-oxy or -mercapto substituted carboxylic acids, method for the production and use thereof as medicaments
WO2008017381A1 (en) Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, processes for preparing them, medicaments comprising these compounds, and their use
WO2007045392A1 (en) Triazolopyridine derivatives as inhibitors of lipases and phospholipases
WO2008089892A1 (en) Phenothiazin derivates, method for the production thereof and use thereof as pharmaceuticals
WO2007059871A1 (en) Hydroxy-substituted diphenylazetidinones for the treatment of hyperlipidaemia
WO2009039943A1 (en) (carboxylalkylene-phenyl)-phenyl-oxalamides, method for the production thereof, and use of same as a medicament
US20120004165A1 (en) Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
WO2007045393A1 (en) Carbamoylbenzotriazole derivatives as inhibitors of lipases and phospholipases
WO2009149820A1 (en) Annelated n-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals
WO2007039173A1 (en) Cyclic n-[1 ,3,4]-thiadiazol-2-yl-benzene sulfonamides, processes for their preparation and their use as pharmaceuticals
WO2007131621A1 (en) 4,5-diphenyl-pyrimidinyl substituted carboxylic acids, method for the production and use thereof as medicaments
WO2009039942A1 (en) (cyclopropyl-phenyl)-phenyl-oxalamides, method for the production thereof, and use of same as a medicament
WO2008058630A1 (en) Novel 1,4-benzothiepin-1,1-dioxide derivatives which are substituted with fluorine, method for producing the same, drugs containing said compounds and use thereof
WO2009149819A1 (en) Annelated pyrrolidin sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals
WO2007093366A1 (en) Novel aminoalcohol-substituted aryldihydroisoquinolinones, process for their preparation and their use as medicaments
WO2008058631A1 (en) Novel 1,4-benzothiepin-1,1-dioxide derivatives with improved properties, method for producing the same, drugs containing said compounds and use thereof
WO2014044738A1 (en) Benzoimidazole-carboxylic acid amide derivatives as apj receptor modulators
JP2006509734A (en) The novel bicyclic inhibitors of hormone-sensitive lipase

Legal Events

Date Code Title Description
AK Designated contracting states:

Kind code of ref document: A1

Designated state(s): AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

AX Request for extension of the european patent to

Countries concerned: BAME

17P Request for examination filed

Effective date: 20130205

18W Withdrawn

Effective date: 20130604