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US 5,494,921 AGranted
Fibrinogen receptor antagonists
AssigneeMerck & Co., Inc.
InventorsMelissa S. Egbertson, George D. Hartman, Laura A. Birchenough
Life of this patent
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Abstract
Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##
Claims8
A compound having the formula ##STR67## and pharmaceutically acceptable salts thereof, and esters thereof, wherein X is ##STR68## M is chosen from ##STR69## Y is chosen from ##STR70## m and n, wherein m is independently selected for Y and M, are integers independently chosen from 0-6;
- B is chosen from:
- ##STR71## wherein R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently chosen from:
- hydrogen,
- flourine,
- C.sub.1-8 alkyl,
- hydroxyl,
- hydroxy C.sub.1-6 alkyl,
- carboxy C.sub.0-6 alkyl,
- C.sub.1-6 alkyloxy C.sub.0-6 alkyl,
- C.sub.1-6 alkylcarbonyl C.sub.0-6 alkyl,
- C.sub.3-8 cycloalkyl C.sub.0-6 alkyl,
- aryl C.sub.0-6 alkylcarbonyl C.sub.0-6 alkyl,
- aryl C.sub.0-6 alkyl,
- C.sub.1-6 alkylcarbonyloxy C.sub.0-6 alkyl,
- C.sub.0-6 alkylamino C.sub.0-6 alkyl,
- aryl C.sub.0-6 alkylamino C.sub.0-6 alkyl,
- C.sub.0-6 dialkylamino C.sub.0-6 alkyl,
- aryl C.sub.0-6 alkylcarbonyloxy C.sub.0-6 alkyl,
- C.sub.1-8 alkylsulfonylamino C.sub.0-6 alkyl,
- C.sub.1-6 alkylaminocarbonyloxy C.sub.0-6 alkyl,
- aryl C.sub.0-6 alkylaminocarbonyloxy C.sub.0-6 alkyl,
- aryl C.sub.0-6 alkylsulfonylamino C.sub.0-6 alkyl,
- C.sub.1-8 alkyloxycarbonyalmino C.sub.0-8 alkyl,
- aryl C.sub.0-8 alkyloxycarbonylamino C.sub.0-8 alkyl,
- C.sub.1-8 alkyicarbonylamino C.sub.0-6 alkyl,
- aryl C.sub.0-6 alkylcarbonylamino C.sub.0-6 alkyl,
- C.sub.0-8 alkylaminocarbonyl C.sub.0-6 alkyl,
- aryl C.sub.0-8 alkylaminocarbonyl C.sub.0-6 alkyl,
- C.sub.1-8 alkylaminocarbonylamino C.sub.0-6 alkyl,
- aryl C.sub.0-8 alkylaminocarbonylamino C.sub.0-6 alkyl,
- C.sub.0-8 alkylaminosulfonylamino C.sub.0-6 alkyl,
- aryl C.sub.0-8 alkylaminosulfonylamino C.sub.0-6 alkyl,
- C.sub.1-6 alkylsulfonyl C.sub.0-6 alkyl,
- aryl C.sub.0-6 alkylsulfonyl C.sub.0-6 alkyl,
- aryl C.sub.0-6 alkylcarbonyl C.sub.0-6 alkyl,
- C.sub.1-6 alkylthiocarbonylamino C.sub.0-6 alkyl,
- aryl C.sub.0-6 alkylthiocarbonylamino C.sub.0-6 alkyl,
- wherein alkyl groups may be unsubstituted or substituted with one or more substituents selected from
- hydrogen,
- C.sub.1-10 alkyl,
- aryl C.sub.0-8 alkyl,
- oxo,
- thio,
- amino C.sub.0-8 alkyl, C.sub.1-3 acylamino C.sub.0-8 alkyl,
- C.sub.1-6 alkylamino C.sub.0-8 alkyl,
- C.sub.1-6 dialkylamino C.sub.0-8 alkyl,
- C.sub.1-4 alkoxy C.sub.0-6 alkyl,
- carboxy C.sub.0-6 alkyl, C.sub.1-3 alkoxycarbonyl C.sub.0-6 alkyl,
- carboxy C.sub.0-6 alkyloxy and
- hydroxy C.sub.0-6 alkyl;
- wherein R.sup.9 and R.sup.10 are independently chosen from:
- hydrogen, with the proviso that R.sup.9 and R.sup.10 cannot both be hydrogen,
- C.sub.1-8 alkyisulfonylamino C.sub.0-6 alkyl,
- aryl C.sub.0-6 alkylsulfonylamino C.sub.0-6 alkyl,
- C.sub.0-8 alkylaminosulfonylamino C.sub.0-6 alkyl,
- aryl C.sub.0-8 alkylaminosulfonylamino C.sub.0-6 alkyl,
- wherein alkyl groups may be unsubstituted or substituted with one or more substituents selected from
- hydrgen,
- C.sub.1-10 alkyl,
- aryl C.sub.0-8 alkyl,
- oxo,
- thio,
- amino C.sub.0-8 alkyl, C.sub.1-3 acylamino C.sub.0-8 alkyl,
- C.sub.1-6 alkylamino C.sub.0-8 alkyl,
- C.sub.1-6 dialkylamino C.sub.0-8 alkyl,
- C.sub.1-4 alkoxy C.sub.0-6 alkyl,
- carboxy C.sub.0-6 alkyl, C.sub.1-3 alkoxycarbonyl C.sub.0-6 alkyl,
- carboxy C.sub.0-6 alkyloxy and
- hydroxy C.sub.o-6 alkyl;
- and
- R.sup.11 is chosen from:
- hydroxy,
- C.sub.1-8 alkyloxy,
- aryl C.sub.0-6 alkyloxy,
- C.sub.1-8 alkylcarbonyloxy C.sub.1-4 alkyloxy,
- aryl C.sub.1-8 alkylcarbonyloxy C.sub.1-4 alkyloxy.
73 more elements
Dependencies are inferred from the claim text.