The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 04, 2001

Filed:

Oct. 04, 2000
Applicant:
Inventors:

Nigel Stephen Watson, Stevenage, GB;

Martin Pass, Stevenage, GB;

Vipulkumar Patel, Stevenage, GB;

Assignee:

Glaxo Group Limited, Greenford, GB;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D / ; A61K 3/144 ;
U.S. Cl.
CPC ...
C07D / ; A61K 3/144 ;
Abstract

The invention relates to a novel class of amide derivatives which act as thrombin inhibitors as described by formula (I), where R,and R,, independently represent a group (a) or R,and R,together form a C,heterocycloalkyl or heterocycloalkenyl group which may be optionally substituted by C,alkyl, C,alkoxy, halogen, carboxylic acid or a C,carboxylic acid ester group; R,represents hydrogen, C,alkyl, halogen, or C,alkoxy; R,, R,and R,independently represent hydrogen, or halogen; R,represents hydrogen or C,alkyl; R,represents hydrogen, C,cycloalkyl, C,cycloalkenyl, C,heterocycloalkyl, C,heterocycloalkenyl, aryl or heteroaryl, which groups are optionally substituted by one or more groups selected from halogen, hydroxy, CN, C,alkyl, C,alkoxy, C,acyloxy, NR,R,, NHCOR,, NHSO,R,, COR,, CO,R,, CONR,R,, and SO,NHR,; X represents a bond, a C,alkyl chain, or a C,alkenyl chain, where one or two nitrogen, oxygen, or sulfur atoms may be optionally contained within each chain, and the chains are optionally substituted by one or more groups selected from halogen, hydroxy, CN, C,alkyl, C,alkoxy, C,acyloxy, NR,R,, NHCOR,, NHSO,R,, COR,, CO,R,, CONR,R,, and SO,NHR,; R,-R,represent hydrogen, C,alkyl, or R,and R,or R,and R,form a C,heterocycloalkyl ring, or R,additionally may represent trifluoromethyl; and pharmaceutically acceptable derivatives or solvates thereof, to processes for their preparation; and their use in the treatment of clinical conditions susceptible to amelioration by administration of a thrombin inhibitor.


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