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US 5,962,479 AGranted
Corticotropin releasing factor antagonists
AssigneePfizer Inc.
InventorYuhpyng Liang Chen
Life of this patent
Estimating the term…
Abstract
Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders. ##STR1##
Claims16
A compound of the formula ##STR18## or a pharmaceutically acceptable salt thereof, wherein A is --CR.sub.7 ;
- B is --NHCHR.sub.1 R.sub.2, or --OCHR.sub.1 R.sub.2 ;
- Z is O;
- R.sub.1 is C.sub.1 -C.sub.4 alkyl which may optionally contain one double or triple bond and which may optionally be substituted with one or two substituents selected independently from hydroxy and C.sub.1 -C.sub.4 alkoxy;
- R.sub.2 is C.sub.1 -C.sub.12 alkyl which may optionally contain one double or triple bond and which may optionally be substituted with from one to three C.sub.1 -C.sub.6 alkoxy;
- R.sub.3 is methyl;
- R.sub.4 is hydrogen, methoxy, amino, nitro, --NH(C.sub.1 -C.sub.4 alkyl), --N(CH.sub.3).sub.2,--COOCH.sub.3, or C.sub.1 -C.sub.4 alkyl one optionally substituted by hydroxy, C.sub.1 -C.sub.3 alkoxy, or chloro;
- R.sub.5 is phenyl or pyridyl, wherein each R.sub.5 is substituted with two or three substituents, independently selected from fluoro, chloro, C.sub.1 -C.sub.6 alkyl optionally containing one carbon--carbon double or triple bond, and C.sub.1 -C.sub.4 alkoxy, and wherein one of said substituents can be further selected from hydroxy, iodo, bromo, formyl, and trifluoromethyl, and wherein said C.sub.1 -C.sub.6 alkyl R.sub.5 group may optionally be substituted with one fluoro, hydroxy, or C.sub.1 -C.sub.2 alkoxy;
- and
- R.sub.7 is hydrogen or methyl.
6 more elements
A process for preparing a compound of the formula I, ##STR19## or a pharmaceutically acceptable salt thereof, wherein A is --CR.sub.7 ;
- B is --NHCHR.sub.1 R.sub.2, or --OCHR.sub.1 R.sub.2 ;
- Z is O;
- R.sub.1 is C.sub.1 -C.sub.6 alkyl which may optionally contain one double or triple bond and which may optionally be substituted with one or two substituents selected independently from hydroxy or C.sub.1 -C.sub.4 alkoxy;
- R.sub.2 is C.sub.1 -C.sub.12 alkyl which may optionally contain one double or triple bond and which may optionally be substituted with from one to three C.sub.1 -C.sub.6 alkoxy;
- R.sub.3 is methyl;
- R.sub.4 is hydrogen, methoxy, amino, nitro, --NH(C.sub.1 -C.sub.4 alkyl), --N(CH.sub.3).sub.2, --COO(C.sub.1 -C.sub.4 alkyl), or C.sub.1 -C.sub.4 one hydroxy, C.sub.1 -C.sub.3 alkoxy or chloro;
- R.sub.5 is phenyl or pyridyl and R.sub.5 is substituted with two or three substituents independently selected from fluoro, chloro, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.4 alkoxy, and wherein one of said substituents can further be selected from hydroxy, iodo, bromo, formyl, and trifluoromethyl, and wherein said C.sub.1 -C.sub.6 alkyl R.sub.5 group may optionally be substituted with one fluoro or hydroxy;
- and
- R.sub.7 is hydrogen or methyl;
- or a pharmaceutically acceptable salt of such compound;
- comprising reacting a compound of the formula ##STR20## wherein R.sub.19 is methyl or ethyl, D is chloro and A, Z, R.sub.4 and R.sub.5 are defined as above, with a compound of the formula BH, wherein B is defined as above, in the presence of a base;
- and then optionally converting the compound of formula I formed in such reaction into a pharmaceutically acceptable salt.
9 more elements
Dependencies are inferred from the claim text.