Heterocyclic compounds
First Claim
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1. A compound of formula I:
- ##STR17## W is S or O;
R8 is selected from the group consisting of hydrogen and C1 -C4 alkyl;
R10'"'"' is C2 -C5 alkynyl;
R11'"'"' is aryl or 5 to 6 member heterocyclic ring each of which is optionally substituted with one or more independently selected from the group consisting of halogen, --CN, C1-4 -alkyl, C1-4 -alkoxy, --OCF3, --CF3, --CONH2, --CSNH2 ;
--OH, --COR6'"'"', CH2 --OH, and --NH2 ;
G is selected from one of the following azacyclic or azabicyclic ring systems;
##STR18## or G is optionally substituted C3 -C8 cycloalkyl wherein the cycloalkyl substituents are selected from R1 and R2 ;
or optionally substituted C1-6 -alkyl wherein the substitution is --NR6 R7 ;
R6 and R7 independently are selected from the group consisting of hydrogen and C1-6 -alkyl;
or R6 and R7 together with the nitrogen atom optionally form a 4- to 6-member ring;
R1 and R2 independently are selected from the group consisting of hydrogen, C1-15 -alkyl, C2-5 -alkenyl, C2-5 -alkynyl, C1-10 -alkoxy, and C1-5 -alkyl substituted with one or more independently selected from the group consisting of --OH, --COR6'"'"', CH2 --OH, halogen, --NH2, carboxy, ##STR19## and phenyl;
R9 and R9 '"'"' are each independently selected from the group consisting of hydrogen, halogen, C1-4 -alkoxy, C1-4 -alkyl, --CN, --OCF3, --CONH2 and --CSNH2 ;
R6'"'"' is hydrogen, C1-6 -alkyl;
R3 is selected from the group consisting of hydrogen, C1-5 -alkyl, C2-5 -alkenyl and C2-5 -alkynyl;
n is 0, 1 or 2;
m is 0, 1 or 2;
p is 0, 1 or 2;
q is 1 or 2;
r is 0, 1 or 2;
. . is a single or double bond; and
pharmaceutically acceptable salts and solvates thereof.
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Abstract
The present invention provides heterocyclic compounds which are useful for modulating a muscarinic receptor.
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22 Claims
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1. A compound of formula I:
- ##STR17## W is S or O;
R8 is selected from the group consisting of hydrogen and C1 -C4 alkyl;R10'"'"' is C2 -C5 alkynyl; R11'"'"' is aryl or 5 to 6 member heterocyclic ring each of which is optionally substituted with one or more independently selected from the group consisting of halogen, --CN, C1-4 -alkyl, C1-4 -alkoxy, --OCF3, --CF3, --CONH2, --CSNH2 ;
--OH, --COR6'"'"', CH2 --OH, and --NH2 ;G is selected from one of the following azacyclic or azabicyclic ring systems;
##STR18## or G is optionally substituted C3 -C8 cycloalkyl wherein the cycloalkyl substituents are selected from R1 and R2 ;or optionally substituted C1-6 -alkyl wherein the substitution is --NR6 R7 ; R6 and R7 independently are selected from the group consisting of hydrogen and C1-6 -alkyl;
or R6 and R7 together with the nitrogen atom optionally form a 4- to 6-member ring;R1 and R2 independently are selected from the group consisting of hydrogen, C1-15 -alkyl, C2-5 -alkenyl, C2-5 -alkynyl, C1-10 -alkoxy, and C1-5 -alkyl substituted with one or more independently selected from the group consisting of --OH, --COR6'"'"', CH2 --OH, halogen, --NH2, carboxy, ##STR19## and phenyl;
R9 and R9 '"'"' are each independently selected from the group consisting of hydrogen, halogen, C1-4 -alkoxy, C1-4 -alkyl, --CN, --OCF3, --CONH2 and --CSNH2 ;R6'"'"' is hydrogen, C1-6 -alkyl; R3 is selected from the group consisting of hydrogen, C1-5 -alkyl, C2-5 -alkenyl and C2-5 -alkynyl; n is 0, 1 or 2; m is 0, 1 or 2; p is 0, 1 or 2; q is 1 or 2; r is 0, 1 or 2; . . is a single or double bond; and pharmaceutically acceptable salts and solvates thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 19, 20)
- ##STR17## W is S or O;
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15. A compound of formula II ##STR20## wherein R is selected from the group consisting of --OR4, --SR4, --SOR4, --SO2 R4, --Z--C3-10 -cycloalkyl, --Z--C4-12 -(cycloalkylalkyl) which is optionally substituted with straight or branched C1-6 -alkyl or R is selected from the group consisting of --OR5 Y, --SR5 Y, --OR5 ZY, --SR5 ZY, --OR5 ZR4, and --SR5 ZR4 ;
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R4 is selected from the group consisting of straight or branched C1-15 -alkyl, straight or branched C2-15 -alkenyl, straight or branched C2-15 -alkynyl and straight or branched C4-15-alkenynyl, each of which is optionally substituted with one or more independently selected from the group consisting of halogen(s), --CF3, --CN, Y and phenyl which is optionally substituted with one or more independently selected from the group consisting of --OH, halogen, --CN, straight or branched C1-4 -alkyl, straight or branched C1-4 -alkylthio, straight or branched C1-4 -alkoxy, --SCF3, --OCF3, --CONH2, --CSNH2, and CF3 ; Z is oxygen or sulphur; R5 is straight or branched C1-15 -alkylene, straight or branched C2-15 -alkenylene, straight or branched C2-15 -alkynylene or straight or branched C4-15-alkenynylene; Y is a 5 or 6 membered heterocyclic group optionally substituted with one or more independently selected from the group consisting of --OH, halogen, --NO2, --CN, straight or branched C1-4 -alkyl, straight or branched C1-4 -alkylthio, straight or branched C1-4 -alkoxy, --SCF3, --OCF3, --CF3, --CONH2 and --CSNH2 ;
or a pharmaceutically acceptable salt or solvate thereof. - View Dependent Claims (16, 17, 18, 21, 22)
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Specification