Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1993-02-12
1995-09-19
Rizzo, Nicholas
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540509, C07D24324, A61K 3155
Patent
active
054515823
ABSTRACT:
Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein: R.sup.1 is H, certain optionally substituted C.sub.1.6 alkyl, or C.sub.3-7 cycloalkyl;
R.sup.2 is (CH.sub.2).sub.q -tetrazolyl optionally substituted in the tetrazole ring by C.sub.1-4 alkyl, (CH.sub.2).sub.q -imidazolyl (where q is 0, 1, 2 or 3), CONHSO.sub.2 R.sup.9, SO.sub.2 NHCOR.sup.9 (where R.sup.9 is C.sub.1-6 alkyl, optionally substituted aryl or trifluoromethyl). SO.sub.2 NHR.sup.10 (where R.sup.10 is a nitrogen containing heterocycle), cyclopropyl or (CH.sub.2), CO.sub.2 H, where n is 1 or 2;
R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ;
R.sup.4 is C.sub.1-7 straight or branched chain alkyl; and
x is 0, 1, 2 or 3;
are CCK and/or gastrin receptor antagonists. They and compositions thereof are useful in therapy.
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Chambers Mark S.
Fletcher Stephen R.
Matassa Victor G.
DiPrima Joseph F.
Merck Sharp & Dohme Ltd.
North Robert J.
Rizzo Nicholas
Winokur Melvin
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