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Heterocyclic substituted Indan derivatives as antagonists of dopamine D2 Receptors and serotonin 2a

机译:杂环取代的Indan衍生物作为多巴胺D2受体和血清素2a的拮抗剂

摘要

Refers to substituted Heterocyclic indan Derivatives of formula Ia where J is s, so, SO2, CH2, where NR10 R10 is H, alkyl of C1 - C6 C (= o) c1-c6 alkyl, - C (= o) or alqulo C1 - C6; M is CH, CH N; g n; M is 1 to 6; X is o, NR1, where R3 is R10, C (= o), Choh, chor3, among others; r1 is H, Halo, cyano, C1 - C6 alkyl substituted with one to three Fluorine Atoms.C1-c6 alkoxy optionally substituted with one to three Fluorine ATOMS, among other r1; R2 is under the condition that R2 cannot form a Heterocyclic ring is present when R1, R4 and R5 are h, Halo, cyano, aminoalquilo c1-c6 alkoxy, C1 - C6, R6, R7, among others; R8 and R9 are h, alkyl of C1 - C6, OPC Ionalmente replaced with one to three Fluorine Atoms; and when R11 is present is selected, orR13 NR13, which is defined as R10 (CH2) W, where W is 1 to 6; n is 1 to 3; Z is 1 to 3; R11 is H, alkyl of C1 - C6 C1 - C6 alkyl - SO2 -, among others.Preferred compounds are n {2 - [6 - (4 - (benzo [d] isotiazol ilpiperazin - 3 - 1 - il) ethyl] - 1 - indan il} acetamide; (S) - (+) - N - (5 - [2 - [4 - (benzo [d] - 3 - ilpiperazin isotiazol - 1 - il) ethyl] - 2 - indan il} acetamide; (R) - n {(-) - 5 - [2 - [4 - (benzo [d] isotiazol ilpiperazin - - 3 - 1 - il) ethyl] - 2 - indan il} propionamide; among others. It also relates to a Pharmaceutical Composition and a process for Preparation.These compounds are antagonists of dopamine D2 and serotonin 2a receptor (5HT2A) being useful in the treatment of Schizophrenia and other disorders of the CNS
机译:指式Ia的取代杂环茚满衍生物,其中J为s,因此为SO2,CH2,其中NR10 R10为H,C1-C6 C(= o)c1-c6烷基,-C(= o)或α1的烷基-C6; M为CH,CH为N; n M为1至6; X是o,NR1,其中R3是R10,C(= o),Choh,chor3等; r1是H,卤素,氰基,被1-3个氟原子取代的C1-C6烷基。除其他r1外,C1-c6烷氧基任选被1-3个氟原子取代。当R 1,R 4和R 5为h,卤素,氰基,氨基芳基C 1 -C 6烷氧基,C 1 -C 6,R 6,R 7等时,R 2的条件是R 2不能形成杂环。 R8和R9是h,C1-C6的烷基,被一到三个氟原子取代的OPC离子基;当R11存在时,或R13 NR13定义为R10(CH2)W,其中W为1至6; n为1至3; Z为1至3; R 11是H,C 1 -C 6 C 1 -C 6烷基-SO 2-的烷基,优选的化合物是n {2-[6-(4-(苯并[d]异噻唑ilpiperazin-3-1-il)乙基]- 1-茚满il}乙酰胺;(S)-(+)-N-(5-[2-[4-(苯并[d]-3-哌嗪异噻唑-1-il)乙基]]-2-茚满il}乙酰胺;(R)-n {(-)-5-[2-[4-(苯并[d]异噻唑唑哌嗪--3-1-il)乙基]-2-茚满il}丙酰胺;等等。这些化合物是多巴胺D2和血清素2a受体(5HT2A)的拮抗剂,可用于治疗精神分裂症和其他中枢神经系统疾病

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