5-HT.sub.4 agonists and antagonists
First Claim
Patent Images
1. A compound of formula I:
- ##STR7## wherein;
A-D is C═
N or N--C═
O;
n is 1, 2, 3, 4, or 5;
R is hydrogen, halo, C1 -C4 alkyl, hydroxy, C1 -C4 alkoxy, C1 -C4 alkylthio, cyano, trifluoromethyl, carboxamido, mono or di(C1 -C4 alkyl) carboxamido;
R1 is hydrogen, C1 -C6 alkyl, C3 -C6 cycloalkyl, or substituted C3 -C6 cycloalkyl;
R2 and R3 taken together form a bridge of 1 to 4 methylene units;
X is OR4 or NR4 R5 ;
R4 is hydrogen, C1 -C6 alkyl, C3 -C6 cycloalkyl, substituted C3 -C6 cycloalkyl, phenyl, substituted phenyl, (C1 -C6 alkyl)CO, benzoyl, substituted benzoyl, tricyclo[3.3.1.13,7 ]decan-1-oyl, or S(O)2 R6 ;
R5 is hydrogen or R4 and R5 together with the nitrogen to which they are attached form a 1-pyrrolidinyl, 1-piperazinyl, 1,2,3,4-tetrahydro-2-isoquinolinyl, 2,3-dihydro-1-indolinyl, 4-morpholinyl, 1-piperidinyl, 1-hexamethyleneiminyl, or phthalimidyl ring;
R6 is C1 -C6 alkyl, C3 -C6 cycloalkyl, substituted C3 -C6 cycloalkyl, phenyl, or substituted phenyl;
or a pharmaceutically acceptable salt thereof provided that when A-D is C═
N and X is OR4, then R4 is phenyl substituted 1 to 3 times with a halogen.
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Abstract
Compounds of formula I: ##STR1## are used as antagonists and partial agonists for the serotonin receptor 5-HT4 and provide therapeutic methods for treatment of disorders caused by or affected by dysfunction of the 5-HT4 receptor.
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Citations
12 Claims
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1. A compound of formula I:
- ##STR7## wherein;
A-D is C═
N or N--C═
O;n is 1, 2, 3, 4, or 5; R is hydrogen, halo, C1 -C4 alkyl, hydroxy, C1 -C4 alkoxy, C1 -C4 alkylthio, cyano, trifluoromethyl, carboxamido, mono or di(C1 -C4 alkyl) carboxamido; R1 is hydrogen, C1 -C6 alkyl, C3 -C6 cycloalkyl, or substituted C3 -C6 cycloalkyl; R2 and R3 taken together form a bridge of 1 to 4 methylene units; X is OR4 or NR4 R5 ; R4 is hydrogen, C1 -C6 alkyl, C3 -C6 cycloalkyl, substituted C3 -C6 cycloalkyl, phenyl, substituted phenyl, (C1 -C6 alkyl)CO, benzoyl, substituted benzoyl, tricyclo[3.3.1.13,7 ]decan-1-oyl, or S(O)2 R6 ; R5 is hydrogen or R4 and R5 together with the nitrogen to which they are attached form a 1-pyrrolidinyl, 1-piperazinyl, 1,2,3,4-tetrahydro-2-isoquinolinyl, 2,3-dihydro-1-indolinyl, 4-morpholinyl, 1-piperidinyl, 1-hexamethyleneiminyl, or phthalimidyl ring; R6 is C1 -C6 alkyl, C3 -C6 cycloalkyl, substituted C3 -C6 cycloalkyl, phenyl, or substituted phenyl;
or a pharmaceutically acceptable salt thereof provided that when A-D is C═
N and X is OR4, then R4 is phenyl substituted 1 to 3 times with a halogen. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
- ##STR7## wherein;
Specification