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US 5,852,045 AGranted
Fibrinogen receptor antagonists
AssigneeMerck & Co., Inc.
InventorsBen C. Askew, George D. Hartman, Mark E. Duggan, Steven D. Young, John H. Hutchinson, John S. Wai, Melissa S. Egbertson, Laura M. Vassallo, Laura A. Libby, Amy E. Krause, Wasyl Halczenko, Nathan C. Ihle
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Abstract
Fibrinogen receptor antagonists having the structure, for example, of ##STR1## for example ##STR2##
Claims13
A compound having the formula ##STR184## or a pharmaceutically acceptable salt thereof, wherein X is
- an aromatic heterocyclic ring selected from the group consisting of:
- ##STR185## E is --CH-- or --N--;
- G is --CH-- or --N--;
- R.sup.8 is
- hydrogen,
- C.sub.1-8 alkyl,
- aryl,
- aryl C.sub.1-6 alkyl,
- hydroxy C.sub.1-6 alkyl,
- C.sub.1-6 alkylsulfonyl,
- C.sub.1-6 alkylsulfonyl C.sub.1-6 alkyl,
- aryl sulfonyl C.sub.1-6 alkyl,
- aryl sulfonyl,
- aryl C.sub.1-6 alkylsulfonyl, or
- aryl C.sub.1-6 alkylsulfonyl C.sub.1-6 alkyl;
- R.sup.10 is
- hydrogen
- --NHCOR.sup.2,
- --NH.sub.2,
- --NH.sub.2 SO.sub.2 R.sup.2, or
- --OH;
- R.sup.12 is
- --OR.sup.2,
- --OCH.sub.2 OCOR.sup.2, or
- --OCH.sub.2 OCON(R.sup.2).sub.2 ;
- and
- R.sup.2 is
- hydrogen,
- halogen,
- C.sub.1-10 alkyl,
- C.sub.3-8 cycloalkyl,
- aryl,
- aryl C.sub.1-8 alkyl,
- amino,
- amino C.sub.1-8 alkyl,
- C.sub.1-3 acylamino,
- C.sub.1-3 acylamino C.sub.1-8 alkyl,
- C.sub.1-6 alkylamino,
- C.sub.1-6 alkylamino C.sub.1-8 alkyl,
- C.sub.1-6 dialkylamino,
- C.sub.1-6 dialkylamino C.sub.1-8 alkyl,
- C.sub.1-4 alkoxy,
- C.sub.1-4 alkoxy C.sub.1-6 alkyl,
- carboxy,
- carboxy .sub.1-6 alkyl,
- C.sub.1-3 alkoxycarbonyl,
- C.sub.1-3 alkoxycarbonyl C.sub.1-6 alkyl,
- carboxy C.sub.1-6 alkyloxy,
- hydroxy, and
- hydroxy C.sub.1-6 alkyl.
47 more elements
A compound having the formula ##STR189## or a pharmaceutically acceptable salt thereof, wherein X is
- an aromatic heterocyclic ring selected from the group consisting of:
- ##STR190## E is --CH-- or --N--;
- G is --CH-- or --N--;
- R.sup.8 is ##STR191## R.sup.10 is hydrogen,
- --NHCOR.sup.2,
- --NH.sub.2,
- --NH.sub.2 SO.sub.2 R.sup.2, or
- --OH;
- R.sup.12 is
- --OR.sub.2,
- --OCH.sub.2 OCOR.sup.2, or
- --OCH.sub.2 OCON(R.sup.2).sub.2 ;
- and
- R.sup.2 is
- hydrogen,
- halogen,
- C.sub.1-10 alkyl,
- C.sub.3-8 cycloalkyl,
- aryl,
- aryl C.sub.1-8 alkyl,
- amino,
- amino C.sub.1-8 alkyl,
- C.sub.1-3 acylamino,
- C.sub.1-3 acylamino C.sub.1-8 alkyl,
- C.sub.1-6 alkylamino,
- C.sub.1-6 alkylamino C.sub.1-8 alkyl,
- C.sub.1-6 dialkylamino,
- C.sub.1-6 dialkylamino C.sub.1-8 alkyl,
- C.sub.1-4 alkoxy,
- C.sub.1-4 alkoxy C.sub.1-6 alkyl,
- carboxy,
- carboxy .sub.1-6 alkyl,
- C.sub.1-3 alkoxycarbonyl,
- C.sub.1-3 alkoxycarbonyl C.sub.1-6 alkyl,
- carboxy C.sub.1-6 alkyloxy,
- hydroxy, and
- hydroxy C.sub.1-6 alkyl.
34 more elements
A compound selected from the group consisting of
- N-1-4-(1-Imidazole)butyl!-2-piperidone-3-yl!acetyl-3(S)-(3-pyridyl)-.beta .-alanine ethyl ester,
- N-1-4-(1-imidazol)butyl!-2-piperidone-3-yl!acetyl-3(S)-(3-pyridyl)-.beta. -alanine, and
- N-1-(3-(1-Imidazole)propyl)-2-piperidone-3(R)-yl!acetyl-3(R)-(2-phenethyl) -.beta.-alanine
- or a pharmaceutically acceptable salt thereof.
1 more element
Dependencies are inferred from the claim text.