Piperazine substituted aryl benzodiazepines
1-41-41 1-63-61-41-4222 1-61-6442445656256545241-61-63 1-62-61-41-41-44 1-61-65 6 1-67 1-61-68 9 1-61 2 1-61-677278989 Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N,...
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Format | Patent |
Language | English |
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10.06.2008
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Abstract | 1-41-41 1-63-61-41-4222 1-61-6442445656256545241-61-63 1-62-61-41-41-44 1-61-65 6 1-67 1-61-68 9 1-61 2 1-61-677278989 Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C) alkylene or hydroxy substituted (C) alkylene; X is oxygen or sulfur; Ris hydrogen, (C) fluroalkyl, (C) cycloalkyl, or (C) alkyl, wherein the (C) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCHCHOH, or -CN; Ris H, halogen, (C) fluoroalkyl, (C) cycloalkyl, OR, SR, NO, CN, COR, C(O)OR, CONRR, NRR, SONRR, NRCOR, NRSOR, optionally substituted aromatic, or (C) alkyl, wherein (C) alkyl is unsubstituted or substituted with a hydroxy group; Ris hydrogen (C) fluoroalkyl, (C) alkenyl, Ar, (C)alkyl-Ar, or (C) alkyl wherein (C) alkyly is unsubstituted or substituted with a phenyl; Ris hydrogen, (C) alkyl, (C) fluoroalkyl, or optionally substituted aromatic; Rand Rare independently hydrogen, (C) alkyl, or optionally substituted aromatic, Ris hydrogen, (C) alkyl, (C) fluoroalkyl, or optionally substituted aromatic; Rand Rare independently hydrogen, (C) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Zand Zare independently selected from hydrogen, halogen, (C) alkyl, (C) fluoroalkyl, OR, SR, NO, CN, COR, CONRR, NRR, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I) |
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AbstractList | 1-41-41 1-63-61-41-4222 1-61-6442445656256545241-61-63 1-62-61-41-41-44 1-61-65 6 1-67 1-61-68 9 1-61 2 1-61-677278989 Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C) alkylene or hydroxy substituted (C) alkylene; X is oxygen or sulfur; Ris hydrogen, (C) fluroalkyl, (C) cycloalkyl, or (C) alkyl, wherein the (C) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCHCHOH, or -CN; Ris H, halogen, (C) fluoroalkyl, (C) cycloalkyl, OR, SR, NO, CN, COR, C(O)OR, CONRR, NRR, SONRR, NRCOR, NRSOR, optionally substituted aromatic, or (C) alkyl, wherein (C) alkyl is unsubstituted or substituted with a hydroxy group; Ris hydrogen (C) fluoroalkyl, (C) alkenyl, Ar, (C)alkyl-Ar, or (C) alkyl wherein (C) alkyly is unsubstituted or substituted with a phenyl; Ris hydrogen, (C) alkyl, (C) fluoroalkyl, or optionally substituted aromatic; Rand Rare independently hydrogen, (C) alkyl, or optionally substituted aromatic, Ris hydrogen, (C) alkyl, (C) fluoroalkyl, or optionally substituted aromatic; Rand Rare independently hydrogen, (C) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Zand Zare independently selected from hydrogen, halogen, (C) alkyl, (C) fluoroalkyl, OR, SR, NO, CN, COR, CONRR, NRR, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I) |
Author | Rocco, Vincent Patrick Ruley, Kevin Michael Spinazze, Patrick Gianpietro LeHuerou, Yvan Pineiro-Nunez, Marta Maria Chen, Zhaogen Schaus, John Mehnert Tupper, David Edward Aicher, Thomas Daniel Martin, Fionna Mitchell |
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References | Rasmussen et al., Preclinical Pharmacology of FMPD [6-Fluoro-10-[3-(2-methoxyethyl)-4-methyl-piperazin-1-yl]-2-methyl-4H-3-thia-4,9-diaza-benzo[f]azulene]: A Potential Novel Antipsychotic with Lower Histamine H1 Receptor Affinity Than Olanzapine, The Journal of Pharmacology and Experimental Therapeutics, 2005, pp. 1265-1277, vol. 315, No. 3. Chakrabarti et al. (4115568) 19780900 Tehim et al. (5824676) 19981000 Fu (5602121) 19970200 Chakrabarti J K et al: "Effects of Conformationally Restricted 4-Piperazinyl-10h-Thienobenzod Iazepine Neuroleptics on Central Dopamingergic and Cholinergic Systems," Journal of Medicinal Chemistry, American Chemical Society. Washington, US, vol. 25, No. 10, Oct. 1, 1982, pp. 1133-1140. (0354781) 19900200 (WO 03082877) 20031000 (1016664) 20000700 |
References_xml | – year: 20031000 ident: WO 03082877 – year: 19780900 ident: 4115568 contributor: fullname: Chakrabarti et al. – year: 19981000 ident: 5824676 contributor: fullname: Tehim et al. – year: 19970200 ident: 5602121 contributor: fullname: Fu – year: 20000700 ident: 1016664 – year: 19900200 ident: 0354781 |
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