US 6,610,692 B1Granted

Thrombin inhibitors

AssigneeMerck & Co., Inc.

InventorsPhilip E. Sanderson, Bruce D. Dorsey, Terry A. Lyle, Matthew G. Stanton, Donnette Staas, Adel M. Naylor-Olsen, Craig Coburn, Matthew M. Morrissette

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Abstract

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY or O; c is CY2 or N; d is CY3 or N; e is CY4 or N; f is CY5 or N; g is CY6 or N; Y4, Y5, and Y6 are independently hydrogen, C1-4 alkyl, or halogen; Y1 and Y2 are independently hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy, and Y3 is hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, —CN, NH2, OH or C1-4 alkoxy; A is and W, W1, R1, R3, R4, R5, X and Z are defined in the specification.

Claims7

Dependent claims

A compound of the formula

or a pharmaceutically acceptable salt thereof, wherein
b is NY1 or O;
c is CY2 or N;
d is CY3 or N;
e is CY4 or N;
f is CY5 or N;
g is CY6 or N, provided that 1) when e and f are N, g is CY6, 2) when e and g are N, f is CY5, and 3) when f and g are N, e is CY4;
Y1, Y2, Y3, Y4, Y5, and Y6 are independently selected from the group consisting of hydrogen, C1-4 alkyl, NH2 and Cl;
A is
X is selected from the group consisting of hydrogen and halogen;
R3 is selected from the group consisting of hydrogen and C1-4 alkyl;
W is selected from the group consisting of hydrogen, R2, R2SO2, R2CH2SO2, and
where m is 0-3, and
R2 is selected from the group consisting of hydrogen, C1-7 alkyl unsubstituted or substituted with phenyl, naphthyl or C3-7 cycloalkyl.

11 more elements

Dependencies are inferred from the claim text.

Facts

Application: 09/429,741Filed 28 Oct 1999 · us provisional application
Priority: 30 Oct 1998
Granted: 26 Aug 2003
Term ends: Not estimatedThe source records don’t support an estimate.

Classification12 codes

C07D 401/12
Containing two hetero rings: linked by a chain containing hetero atoms as chain links
A61P 7/00
Drugs for disorders of the blood or the extracellular fluid
A61P 7/02
Drugs for disorders of the blood or the extracellular fluid: antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A61P 43/00
Drugs for specific purposes, not provided for in groups a61p1/00-a61p41/00