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US 5,397,791 AGranted
Fibrinogen receptor antagonists
AssigneeMerck & Co., Inc.
InventorsGeorge D. Hartman, John D. Prugh, Wasyl Halczenko, Melissa Egbertson, Nathan Ihle
Life of this patent
Estimating the term…
Abstract
Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##
Claims8
A compound of formula I ##STR133## or a pharmaceutically acceptable salt thereof wherein:
- A and B are independently selected from the group consisting of C,O and S, wherein one of A or B is O or S, and
- D and E are independently selected from the group consisting of C, O and S, wherein one of D or E is O or S;
- X is ##STR134## Y is (CH.sub.2).sub.q, (CH.sub.2).sub.q (C.sub.4-10 cycloalkyl), (CH.sub.2).sub.q NR.sup.3 --CO(CH.sub.2).sub.q (CH.sub.2).sub.q CONR.sup.3 (CH.sub.2).sub.q, (CH.sub.2).sub.q --O--(CH.sub.2).sub.q, (CH.sub.2).sub.q --S(O.sub.n)--(CH.sub.2).sub.q, or (CH.sub.2).sub.q --SO.sub.2 --NR.sup.3 (CH.sub.2).sub.q --, (CH.sub.2).sub.q CO(CH.sub.2).sub.q, (CH.sub.2).sub.0-6 phenyl(CH.sub.2).sub.0-6, (CH.sub.2).sub.0-6 imidazolyl(CH.sub.2).sub.0-6, ##STR135## wherein q is an integer chosen from 0-8;
- Z and L are independently chosen from ##STR136## (CH.sub.2).sub.m SO.sub.2 (CH.sub.2).sub.n, (CH.sub.2).sub.m S(CH.sub.2).sub.n, (CH.sub.2).sub.m SO(CH.sub.2).sub.n, (CH.sub.2).sub.m SO.sub.2 NR.sup.3 (CH.sub.2).sub.n, (CH.sub.2).sub.m NR.sup.3 SO.sub.2 (CH.sub.2).sub.n, (CH.sub.2).sub.m CR.sup.3 .dbd.CR.sup.4 (CH.sub.2).sub.n, (CH.sub.2).sub.m C.tbd.C(CH.sub.2).sub.n, (CH.sub.2).sub.m, and (CH.sub.2).sub.m O(CH.sub.2).sub.n, where m and n are integers independently chosen from 0-6, and where R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, C.sub.1-10 alkyl, phenyl C.sub.0-8 alkyl, OXO, thio, amino C.sub.0-8 alkyl, C.sub.1-3 alkylcarbonylamino 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 .sub.0-6 alkyloxy, or hydroxy C.sub.0-6 alkyl, where m and n are integers independently chosen from 2-5;
- M is:
- ##STR137## wherein R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 are independently chosen from:
- hydrogen, fluorine, C.sub.1-8 alkyl, hydroxyl, hydroxy C.sub.1-6 alkyl, carboxy C.sub.0-6 alkyl, C.sub.1-6 alkyloxy, phenyl C.sub.0-6 alkyloxy, C.sub.1-6 alkylcarbonyl, phenyl C.sub.0-6 alkylcarbonyl, C.sub.1-6 alkylcarbonyloxy, phenyl C.sub.0-6 alkylcarbonyloxy, C.sub.1-6 alkylaminocarbonyloxy C.sub.0-6 alkyl, C.sub.3-8 cycloalkyl, phenyl C.sub.0-6 alkyl, C.sub.0-6 alkylamino C.sub.0-6 alkyl, C.sub.0-6 dialkylamino C.sub.0-6 alkyl, C.sub.1-8 alkylsulfonylamino C.sub.0-6 alkyl, phenyl C.sub.0-6 alkylsulfonylamino C.sub.0-6 alkyl, pyridyl C.sub.0-6 alkylsulfonylamino C.sub.0-6 alkyl, thienyl C.sub.0-6 alkylsulfonylamino C.sub.0-6 alkyl, naphthyl C.sub.0-6 alkylsulfonylamino C.sub.0-6 alkyl, pyryl C.sub.0-6 alkylsulfonylamino C.sub.0-6 alkyl, C.sub.1-8 alkyloxycarbonylamino CO.sub.0-8 -alkyl, C.sub.1-8 alkylcarbonylamino C.sub.0-6 alkyl, pyridyl C.sub.0-6 alkylcarbonylamino C.sub.0-6 alkyl, C.sub.0-8 alkylaminocarbonylamino C.sub.0-6 alkyl, phenyl C.sub.0-8 alkylaminocarbonylamino C.sub.0-6 alkyl, C.sub.0-8 alkylaminosulfonylamino C.sub.0-6 alkyl, C.sub.1-6 alkylsulfonyl C.sub.0-6 alkyl, C.sub.1-6 alkylcarbonyl C.sub.0-6 alkyl, phenyl C.sub.0-6 alkylcarbonyl C.sub. 0-6 alkyl, C.sub.1-6 alkylthiocarbonylamino C.sub.0-6 alkyl;
- and
- R.sup.12 is chosen from hydroxy, C.sub.1-8 alkyloxy, phenyl C.sub.0-6 alkyloxy, C.sub.1-8 alkylcarbonyloxy C.sub.1-4 alkyloxy, or a naturally occurring 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 C.sub.1-6 alkyl.
6 more elements
Dependencies are inferred from the claim text.