2-carbocyclic and 2-heterocyclic quinoline-4-carboxylic acids and salts thereof useful as immunosuppressive agents
First Claim
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1. A compound of Formula I ##STR27## or pharmaceutically acceptable salts or prodrug forms thereof wherein:
- A is selected from;
##STR28## X is --N(R7)--, --O--, --S--, or --CH═
CH--;
Y is --N--or --C(R8)--;
Z is --C(R8)(R9)--;
R1 and R2 are independently selected from H, Cl, Br, F, CF3, or C1 -C4 alkyl;
R3 is selected from hydrogen, C1 -C3 alkyl, --CN, --NR8 R9, --OR8, --SR8, --CF3, --OCF3, --SCF3 ;
R4 is selected from hydrogen, Cl, F, C1 -C3 alkyl, 13 OR8a, --CF3, --OCF3, --SR8a, --SCF3, --NR8 R9 ;
R5 is an aryl or heteroaryl selected from phenyl, thienyl, furyl, pyridinyl, thiazolyl, or oxazolyl, said aryl or heteroaryl being optionally substituted with 0-2 R11 ;
R6 and R6a are independently selected from hydrogen or C1 -C3 alkyl;
R7, R8, and R9 are independently selected from hydrogen or C1 -C3 alkyl;
R8a is C1 -C3 alkyl;
R8 and R9 can alternatively join to form --(CH2)4 --, --(CH2)5 --, --CH2 CH2 N(R10)CH2 CH2 --, or --CH2 CH2 OCH2 CH2 --;
R10 is hydrogen or methyl;
R11 is selected from hydrogen, Cl, F, C1 -C3 alkyl, --OR8a, --CF3, --OCF3, --SR8a, --SCF3, --NR8 R9.
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Abstract
This invention relates to 2-carbocyclic and 2-heterocyclic quinoline-4-carbocyclic acid compounds, and salts thereof, to pharmaceutical compositions comprising such compounds, and to methods of using such compounds for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, and chronic inflammatory diseases, including but not limited to psoriasis and rheumatoid arthritis, in a mammal.
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8 Claims
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1. A compound of Formula I ##STR27## or pharmaceutically acceptable salts or prodrug forms thereof wherein:
- A is selected from;
##STR28## X is --N(R7)--, --O--, --S--, or --CH═
CH--;
Y is --N--or --C(R8)--;Z is --C(R8)(R9)--; R1 and R2 are independently selected from H, Cl, Br, F, CF3, or C1 -C4 alkyl; R3 is selected from hydrogen, C1 -C3 alkyl, --CN, --NR8 R9, --OR8, --SR8, --CF3, --OCF3, --SCF3 ; R4 is selected from hydrogen, Cl, F, C1 -C3 alkyl, 13 OR8a, --CF3, --OCF3, --SR8a, --SCF3, --NR8 R9 ; R5 is an aryl or heteroaryl selected from phenyl, thienyl, furyl, pyridinyl, thiazolyl, or oxazolyl, said aryl or heteroaryl being optionally substituted with 0-2 R11 ; R6 and R6a are independently selected from hydrogen or C1 -C3 alkyl; R7, R8, and R9 are independently selected from hydrogen or C1 -C3 alkyl; R8a is C1 -C3 alkyl; R8 and R9 can alternatively join to form --(CH2)4 --, --(CH2)5 --, --CH2 CH2 N(R10)CH2 CH2 --, or --CH2 CH2 OCH2 CH2 --; R10 is hydrogen or methyl; R11 is selected from hydrogen, Cl, F, C1 -C3 alkyl, --OR8a, --CF3, --OCF3, --SR8a, --SCF3, --NR8 R9. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
- A is selected from;
Specification