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US 5,508,432 AGranted
Modulators of cholecystokinin
AssigneeGlaxo Wellcome Inc.
InventorsElizabeth E. Sugg, Milana Dezube, Gavin C. Hirst
Life of this patent
Estimating the term…
Abstract
CCK modulators, e.g. agonists or antagonists, of the following formula (I): ##STR1## or a base-addtion salt thereof.
Claims12
A compound of the following Formula (I):
- ##STR23## wherein:
- A is selected from
- --COOR.sup.1,
- --CONHR.sup.1,
- --CN,
- ---- tetrazolyl,
- --CONHSO.sub.2 R.sub.3,
- --CH.sub.2 OR.sup.1,
- --CH.sub.2 SR.sup.1,
- --P--O(OR.sup.1).sub.2 or
- --CO--NHOH;
- R.sup.1 is H or C.sub.1-6 alkyl;
- R.sup.2 is C.sub.1-6 alkyl, CF.sub.3, OH, or phenyl;
- R.sup.3 is OH, NH.sub.2, or CH.sub.3 ;
- R.sup.4 is CN, CO.sub.2 H or CF.sub.3 ;
- B is selected from
- --COCH(NHR.sup.5)--(CH.sub.2).sub.n --,
- --COCH.sub.2 (CH.sub.2).sub.n --,
- --CO--CH.dbd.CH--,
- --CO--phenylene, ortho, meta or para,
- --CH.sub.2 --(CH.sub.2).sub.n -- or
- --CH(COOR.sup.6)--CH.sub.2 --(CH.sub.2).sub.n --;
- where n is 0, 1 or 2;
- R.sup.5 is H, C.sub.1-6 alkyl, COR.sup.7 or CONHR.sup.8 ;
- R.sup.6 is H, C.sub.1-6 alkyl, t-butyl, benzyl, methyl, ethyl or phenyl;
- R.sup.7 is H, C.sub.1-6 alkyl, benzyl, C.sub.1-6 alkoxy, or benzyloxy;
- R.sup.8 is H, C.sub.1-6 alkyl, benzyl or phenyl;
- R.sup.9 is H or C.sub.1-6 alkyl;
- R.sup.10 is H or C.sub.1-6 alkyl;
- m is 1, 2, 3 or 4;
- G is --O--, --CH.sub.2 --, NR.sup.11, --CH.dbd.CH--;
- R.sup.11 is H or C.sub.1-6 alkyl;
- R.sup.12 is selected from
- C.sub.1-10 alkyl,
- C.sub.2-6 alkenyl,
- C.sub.3 -C.sub.10 cycloalkyl,
- C.sub.3 -C.sub.10 carbocyclic arylalkyl or
- C.sub.3 -C.sub.10 carbocyclic aryl having 1 or 2 substituents independently selected from the group consisting of
- hydroxyl,
- halogen
- --OSO.sub.3 R.sup.13,
- nitro,
- cyano,
- amino,
- C.sub.1-6 alkylamino,
- (C.sub.1-6 alkyl).sub.2 amino,
- C.sub.1-6 alkyl,
- halo C.sub.1-6 alkyl
- C.sub.1-6 alkoxy,
- C.sub.2 -C.sub.4 - alkanoyl,
- C.sub.1-6 alkoxy carbonyl, and
- phenoxy;
- R.sup.13 is H or C.sub.1-6 alkyl;
- p is 0, 1 or 2;
- D is selected from
- --NH--CO--,
- --CO--NR.sup.14 --,
- --(CH.sub.2).sub.r --NR.sup.14 -- or
- --NR.sup.13 --(CH.sub.2).sub.r --;
- r is 0, 1 or 2;
- R.sup.14 is H or C.sub.1-6 alkyl;
- R.sup.15 is H or C.sub.1-6 alkyl;
- q is 0 or 1;
- E is selected from
- --NH--CO--,
- --CO--NR.sup.17,
- --NH--CO--NR.sup.17 --,
- --O--CO--NR.sup.17,
- --SO.sub.2 --NR.sup.17 --or
- --(CH.sub.2).sub.r --NR.sub.17 --;
- R.sup.17 is H is C.sub.1-10 alkyl;
- R.sup.18 is selected from
- C.sub.3 -C.sub.10 carbocyclic arylalkyl,
- C.sub.3 -C.sub.10 carbocyclic aryl,
- C.sub.1-10 alkyl,
- C.sub.2-10 alkenyl or
- C.sub.3 -C.sub.10 mono, bi- or tri-cycloalkyl with zero to four substituents independently selected form the group consisting of:
- C.sub.1-10 alkyl,
- halogen,
- CN,
- --OR.sup.19,
- --SR.sup.19,
- --CO.sub.2 R.sup.19,
- --CF.sub.3,
- --NR.sup.19 R.sup.20,
- --(CH.sub.2).sub.s OR.sup.19 or
- --(CH.sub.2).sub.s COOR.sup.19 ;
- s is an integer from 0 to 6;
- R.sup.19 is H or C.sub.1-6 alkyl;
- and
- R.sup.20 is H or C.sub.1-6 alkyl;
- or a pharmaceutically acceptable base-addition salt thereof.
89 more elements
Dependencies are inferred from the claim text.