Fibrinogen receptor antagonists

  • US 5,441,952 A
  • Filed: 04/05/1993
  • Issued: 08/15/1995
  • Est. Priority Date: 04/05/1993
  • Status: Expired due to Fees
First Claim
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1. A fibrinogen receptor antagonist of the following formula:

  • ##STR23## wherein G is ##STR24## X is 3-piperidinyl;

    Y isC1-8 alkylene;

    Z is--(CH2)m --, --C.tbd.C--CH2 -- ##STR25## wherein m is 0-6;

    R5 ishydrogenC 1-6 alkyl,C0-6 alkylcarboxy C0-6 alkyl,C0-6 alkyloxy C0-6 alkyl,hydroxy C0-6 alkyl,aryl C0-6 alkyl, orhalogen;

    R6 ishydrogen,C1-8 alkyl,aryl C0-6 alkyl,C3-8 cycloalkyl C0-6 alkyl,C0-6 alkylcarboxy C0-6 alkyl, carboxy C0-6alkyl,C1-4 alkyloxy C0-6 alkyl, orhydroxy C0-6 alkyl, provided that any of which groups may be substituted or unsubstituted independently with R1 or R2, and provided that, when two R6 groups are attached to the same carbon, they may be the same or different;

    R7 ishydrogen, fluorineC1-8 alkyl,C3-8 cycloalkyl,aryl C0-6 alkyl,C0-6 alkylamino C0-6 alkyl,C0-6 dialkylamino C0-6 alkyl,C1-8 alkylsulfonylamino C0-6 alkyl,aryl C0-6 alkylsulfonylamino C0-6 alkyl,C1-8 alkyloxycarbonylamino C0-8 -alkyl,aryl C0-8 alkyloxycarbonylamino C0-8 alkyl,C1-8 alkylcarbonylamino C0-6 alkyl,aryl C0-6 alkylcarbonylamino C0-6 alkyl,C0-8 alkylaminocarbonylamino C0-6 alkyl,aryl C0-8 alkylaminocarbonylamino C0-6 alkyl,C1-6 alkylsulfonyl C0-6 alkyl,aryl C0-6 alkylsulfonyl C0-6 alkyl,C1-6 alkylcarbonyl C0-6 alkylaryl C0-6 alkylcarbonyl C0-6 alkyl,C1-6 alkylthiocarbonylamino C0-6 alkyl, oraryl C0-6 alkylthiocarbonylamino C0-6 alkyl wherein groups may be unsubstituted or substituted with one or more substituents selected from R1 and R2, and provided that when two R7 groups are attached to the same carbon atom, they may be the same or different;

    R8 ishydroxy,C1-8 alkyloxy,aryl C0-6 alkyloxy,C1-8 alkylcarbonyloxy C1-4 alkyloxy,aryl C1-8 alkylcarbonyloxy C1-4 alkyloxy, oran L- or D-amino acid joined by an amide linkage and wherein the carboxylic acid moiety of said amino acid is as the free acid or is esterified by C1-6 alkyl; and

    R9 ishydrogen, C1-8 alkyl,;

    phenyl or phenyl C1-3 alkyl.

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