C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 495/04 (2006.01) C07D 241/04 (2006.01) C07D 243/38 (2006.01) C07D 401/06 (2006.01) C07D 403/04 (2006.01) C07D 407/06 (2006.01) C07D 409/06 (2006.01) C07D 487/04 (2006.01) C07D 513/04 (2006.01)
Patent
CA 2479932
Described herein are antipyschotic compounds of formula (I) wherein, A is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; Alk is (C1-4) alkylene optionally substituted with OH, methoxy, ethoxy, or F; Ar is optionally substituted phenyl, naphthyl, monocyclic heteroaromatic, or bicyclic heteroaromatic; R1 is hydrogen or (C1-4) alkyl optionally substituted with OH, OR3, or OCH2CH2OH, wherein R3 is (C1-2) alkyl; R2 is H, (C1-6) alkyl, halogen, fluorinated (C1-6) alkyl, OR4, SR4, NO2, CN, COR4, CONR5R6, SO2NR5R6, NR5R6, NR5COR4, NR5SO2R4, or optionally substituted phenyl,wherein R4 is hydrogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, benzyl, or optionally substituted phenyl, R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; Z is one or two substituents independently selected from hydrogen, halogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, SO2NR8R9, NR8SO2R7, NR8R9, or optionally substituted phenyl, wherein R7 is hydrogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, benzyl, or optionally substituted phenyl, R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; and salts, solvates, and crystal 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). Also described are compounds useful as intermediates for the synthesis of the compounds of formula (I).
L'invention porte sur des composés antipsychotiques représentés par la formule (I) dans laquelle A est facultativement un noyau aromatique à 5 ou 6 membres à fusion benzo possédant entre zéro et trois hétéroatomes indépendamment choisis parmi N, O, et S; Alk est (C¿1-4?) alkylène facultativement substitué par OH, methoxy, ethoxy, ou F; Ar est phényl à substitution facultative, naphthyl, hétéroaromatique monocyclique, ou hétéroaromatique bicyclique; R?1¿ est hydrogène ou (C¿1-4?) alkyl facultativement substitué par OH, OR?3¿, ou OCH¿2?CH¿2?OH, R?3¿ est (C¿1-2?) alkyl; R?2¿ est H, (C¿1-6?) alkyl, halogène, (C¿1-6?) alkyl fluoré, OR?4¿, SR?4¿, NO¿2?, CN, COR?4¿, CONR?5¿R?6¿, SO¿2?NR?5¿R?6¿, NR?5¿R?6¿, NR?5¿COR?4¿, NR?5¿SO¿2?R?4¿, phényl à substitution facultative, R?4¿ est hydrogène, (C¿1-6?) alkyl, (C¿1-6?) alkyl fluoré, benzyl, ou phényl à substitution facultative, R?5¿ et R?6¿ sont indépendamment hydrogène, (C¿1-6?) alkyl, ou phényl à substitution facultative; Z est un ou deux substituants indépendamment choisis parmi hydrogène, halogène, (C¿1-6?) alkyl, (C¿1-6?) alkyl fluoré, OR?7¿, SR?7¿, NO¿2?, CN, COR?7¿, CONR?8¿R?9¿, SO¿2?NR?8¿R?9¿, NR?8¿SO¿2?R?7¿, NR?8¿R?9¿, ou phényl à substitution facultative, R?7¿ est hydrogène, (C¿1-6?) alkyl, (C¿1-6?) alkyl fluoré, benzyl, ou phényl à substitution facultative, R?8¿ et R?9¿ sont indépendamment hydrogène, (C¿1-6?) alkyl, ou phényl à substitution facultative; et des sels, des solvants et des formes cristallines de ces derniers. L'invention porte aussi sur l'utilisation de ces composés représentés par la formule (I) en tant qu'antagonistes du récepteur D¿2? de dopamine et en tant qu'agents utilisés dans le traitement de troubles psychotiques et bipolaires, et sur des préparations pharmaceutiques des composés de la formule (I). Elle a également trait à des composés utiles en tant que produits intermédiaires dans la synthèse des composés de la formule (I).
Aicher Thomas Daniel
Chen Ying
Chen Zhaogen
Faul Margaret Mary
Krushinski Joseph Herman Jr.
Eli Lilly And Company
Gowling Lafleur Henderson Llp
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