JP2005126428A5 - - Google Patents

Claims (22)

Formula (I)

[Wherein, R represents a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted, and X represents a bond or a divalent chain hydrocarbon group which may be substituted. X ′ represents a bond or —N (R ⁵ ) — (R ⁵ represents a hydrogen atom, an optionally substituted hydrocarbon group, an esterified or amidated carboxyl group or an acyl group). , Y represents an optionally substituted divalent hydrocarbon group, Y ′ represents a bond or —C (═O) —, ring A represents an optionally substituted nitrogen-containing heterocyclic ring, Z ¹ and Z ³ each independently represent a bond or an optionally substituted divalent chain hydrocarbon group, Z ² represents a bond or —N (R ⁶ ) — (R ⁶ represents a hydrogen atom) Represents an optionally substituted hydrocarbon group or acyl group), and B represents a formula

(R ¹ and R ² are each independently a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally esterified or amidated carboxyl group, an acyl, A group or an optionally substituted amino group, R ³ represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally esterified or amidated carboxyl group or an acyl group, and R ⁴ represents substituted indicates also be a hydrocarbon group, Table by R ² and R ¹ or R ^4, R ³ may form a ring which may be optionally substituted combine with each other and R ⁴⁾ R ⁶ may be bonded to R ¹ , R ² , R ³ or R ⁴ to form an optionally substituted ring, and a represents 0, 1 or 2. Or a salt thereof. A prodrug of the compound of claim 1. R is a halogen atom, C _1-6 alkyl, C _2-6 alkenyl, C _2-6 alkynyl, optionally substituted amino, nitro, cyano, optionally substituted amidino and esterified or amidated The compound according to claim 1, which is an aryl group which may be substituted with a substituent selected from optional carboxyl. R is a halogen atom, C _1-6 alkyl, C _2-6 alkenyl, C _2-6 alkynyl, optionally substituted amino, nitro, cyano, optionally substituted amidino and esterified or amidated The compound according to claim 1, which is a heterocyclic group which may be substituted with a substituent selected from optionally carboxyl. The compound according to claim 1, wherein R is naphthyl optionally substituted with a halogen atom. The compound according to claim 1, wherein X is a bond, X ′ is a bond, Y is an optionally substituted C _1-3 alkylene, and Y ′ is —C (═O) —. The compound according to claim 6, wherein Y is C _1-3 alkylene substituted with a hydroxyl group. The compound according to claim 1, wherein Z ¹ and Z ² are a bond and Z ³ is optionally substituted C _1-3 alkylene. The compound according to claim 1, wherein ring A is an optionally substituted piperazine ring or an optionally substituted piperidine ring. Ring A is the formula

[Wherein, ring A ′ may further have a substituent. ] Or expression

The compound according to claim 1, which is a ring represented by the formula: wherein ring A "may further have a substituent. The compound according to claim 1, wherein R ⁵ is a hydrogen atom. The compound according to claim 1, wherein a is 2. N- (4-((4- (3-((6-chloro-2-naphthyl) sulfonyl) propanoyl) -1-piperazinyl) methyl) -3-methyl-1,3-thiazole-2 (3H) -ylidene ) -N-methylamine, 4-((4- (3-((6-chloro-2-naphthyl) sulfonyl) propanoyl) -1-piperazinyl) methyl) -3-methyl-1,3-thiazole-2 ( 3H) -imine, N- (5-((1- (3-((6-chloro-2-naphthyl) sulfonyl) propanoyl) -4-piperidinyl) methyl) -3-methyl-1,3-thiazole-2 (3H) -Ilidene) -N-methylamine, 5- (1- (3-((6-chloro-2-naphthyl) sulfonyl) propanoyl) -4-piperidinyl) -3-methyl-1,3-thiazole- 2 (3H) -imine, 2- (2-((1- (3-((6-chloro-2-naphthyl) sulfonyl) propanoyl) -4-piperidinyl) imino) -1,3-thiazole-3 (2H ) -Yl) A compound selected from the group consisting of ethanol or a salt thereof or a prodrug thereof. Formula (II)

[Wherein P ⁰ represents a hydrogen atom or an imino protecting group, and other symbols are as defined in claim 1. Or a salt thereof. A pharmaceutical comprising the compound according to claim 1 or the prodrug according to claim 2 . The medicine according to claim 15, which is an anticoagulant. The medicament according to claim 15, which is an activated blood coagulation factor X inhibitor. The medicament according to claim 15, which is a prophylactic / therapeutic agent for myocardial infarction, cerebral infarction, deep vein thrombosis, pulmonary thromboembolism or obstructive arteriosclerosis. The medicament according to claim 15, which is a prophylactic / therapeutic agent for secondary onset of economy class syndrome, thromboembolism during or after surgery, and deep vein thrombosis. Use of a compound according to claim 1 or a prodrug according to claim 2 for the manufacture of a medicament for inhibiting blood clotting. Use of a compound according to claim 1 or a prodrug according to claim 2 for the manufacture of a medicament for inhibiting activated blood coagulation factor X. Use of the compound according to claim 1 or the prodrug according to claim 2 for the manufacture of a medicament for the prevention / treatment of myocardial infarction, cerebral infarction, deep vein thrombosis, pulmonary thromboembolism or obstructive arteriosclerosis .