| US 7,429,579 B2 | ||
| Tetrahydrobenzazepine derivatives useful as modulators of dopamine D3 receptors (antipsychotic agents) | ||
| Michael Stewart Hadley, Harlow (United Kingdom); Andrew Lightfoot, Harlow (United Kingdom); Gregor James MacDonald, Harlow (United Kingdom); and Geoffrey Stemp, Stevenage (United Kingdom) | ||
| Assigned to SmithKline Beecham, PLC, Brentford, Middlesex (United Kingdom) | ||
| Appl. No. 10/416,377 PCT Filed Nov. 12, 2001, PCT No. PCT/EP01/13140 § 371(c)(1), (2), (4) Date Nov. 11, 2003, PCT Pub. No. WO02/40471, PCT Pub. Date May 23, 2002. |
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| Claims priority of application No. 0027784.8 (GB), filed on Nov. 14, 2000; and application No. 0031082.1 (GB), filed on Dec. 20, 2000. | ||
| Prior Publication US 2004/0171606 A1, Sep. 02, 2004 | ||
| Int. Cl. A61P 25/18 (2006.01); A61K 31/55 (2006.01); C07D 223/16 (2006.01) | ||
| U.S. Cl. 514—217.01 [540/594] | 8 Claims |
1. A compound of formula (I)
![]() wherein
R2 is C1-4alkylthio, C1-4alkylsulfonyl, C1-4alkylsulfonyloxy, C1-4alkylsulfonylC1-4alkyl, arylsulfonyl, arylsulfonyloxy, arylsulfonylC1-4alkyl, C1-4alkylsulfonamido, C1-4alkylamido, C1-4alkylsulfonamidoC1-4alkyl, C1-4alkylamidoC1-4alkyl, arylsulfonamido, arylcarboxamido, arylsulfonamidoC1-4alkyl, arylcarboxamidoC1-4alkyl, aroyl, aroylC1-4alkyl, or arylC1-4alkanoyl group; or
a group R5OCO(CH2)p, R5CON(R6)(CH2)p, R5R6NCO(CH2)p or R5R6NSO2(CH2)p, in which p is zero or an integer from 1 to 4, and each of R5 and R6 independently are hydrogen or a C1-4alkyl group, or, in groups R5CON(R6)(CH2)p, R5R6NCO(CH2)p and R5R6NSO2(CH2)p, R5CONR6 or R5R6N together form a 4-, 5-, 6- or 7-membered azacyclic group optionally containing one additional O, N or S atom in the azacycle
and having 3-8 carbon atoms; or
a group Ar3—Z, wherein Ar3 is an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring and Z is
a bond, O, S, SO2, or CH2;
R7 is quinolinyl, unsubstituted or substituted by one or more substituents selected from the group consisting of halo, hydroxyl,
oxo, cyano, nitro, C1-4alkyl, C1-4alkoxy, C1-4alkylenedioxy, C1-4alkanoyl, C1-4alkylsulfonyl, C1-4alkylsulfonyloxy, C1-4alkylsulfinyl, C1-4alkylthio, R13SO2N(R14)—, R13R14NSO2—, R13R14N, R13R14NCO—, or R13CON(R14)— where in each of R13 and R14 independently are hydrogen or C1-4alkyl, or R13R14 together form a C3-6 alkylene chain;
R10 is H or C1-4alkyl;
or a salt thereof.
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