Dopamine receptor ligands
First Claim
1. A compound of Formula I:
- ##STR30## wherein;
A and B independently are both benzene optionally substituted with 1 or 2 substituents selected independently from hydroxyl, halo, selected independently from hydroxyl, halo, C1-4 alkyl, amino, nitro, cyano, halo-substituted C1-4 alkyl, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkoxycarbonyl, C1-4 acyl, halo-substituted C1-4 acyl cyclo-C1-7 alkyl, thio-C1-4 alkylene, C1-4 alkylthio, halo-substituted C1-4 alkylthio, cyanothio, tetrazolyl, N-piperidinyl, N-piperazinyl, N-morpholinyl, acetamido, C1-4 alkylsulfonyl, halosulfonyl, halo-substituted C1-4 alkylsulfonyl, C1-4 alkylsulfoxyl, sulfonamido C1-4 alkylseleno, and OSO3 H;
X1 is selected from NH, N--C1-4 alkyl and N-acetyl,X2 is N=Y is selected from CH and N;
R1 represents C1-4 alkyl;
n is 0, 1 or 2;
q is 1 or 2;
R2 is C1-6 alkylene optionally incorporating an intervening or terminating heteroatom selected from N, O and S;
D is cyclohexane or benzene; and
E is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C1-4 alkyl and halogen-substituted C1-4 alkyl;
and acid addition salts, solvates or hydrates thereof.
1 Assignment
0 Petitions
Accused Products
Abstract
Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;
X1 is selected from CH2, O, NH, S, C═O, CH--OH, CH--N(C1-4 alkyl)2, C═CHCl, C═CHCN, N--C1-4 alkyl, N-acetyl, SO2 and SO;
X2 - - - is selected from N═, CH2 --, CH═, C(O)--, O--, and S--;
R1 represents C1-4 alkyl;
Y is selected from CH and N;
n is 0, 1 or 2;
q is 1 or 2;
R2 is C1-6 alkyl optionally incorporating a heteroatom selected from N, O and S;
D is cyclohexane or benzene; and
E is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C1-4 alkyl and halogen-substituted C1-4 alkyl;
and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
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Citations
20 Claims
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1. A compound of Formula I:
- ##STR30## wherein;
A and B independently are both benzene optionally substituted with 1 or 2 substituents selected independently from hydroxyl, halo, selected independently from hydroxyl, halo, C1-4 alkyl, amino, nitro, cyano, halo-substituted C1-4 alkyl, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkoxycarbonyl, C1-4 acyl, halo-substituted C1-4 acyl cyclo-C1-7 alkyl, thio-C1-4 alkylene, C1-4 alkylthio, halo-substituted C1-4 alkylthio, cyanothio, tetrazolyl, N-piperidinyl, N-piperazinyl, N-morpholinyl, acetamido, C1-4 alkylsulfonyl, halosulfonyl, halo-substituted C1-4 alkylsulfonyl, C1-4 alkylsulfoxyl, sulfonamido C1-4 alkylseleno, and OSO3 H;X1 is selected from NH, N--C1-4 alkyl and N-acetyl, X2 is N= Y is selected from CH and N; R1 represents C1-4 alkyl; n is 0, 1 or 2; q is 1 or 2; R2 is C1-6 alkylene optionally incorporating an intervening or terminating heteroatom selected from N, O and S; D is cyclohexane or benzene; and E is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C1-4 alkyl and halogen-substituted C1-4 alkyl; and acid addition salts, solvates or hydrates thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20)
- ##STR30## wherein;
Specification