首页> 外国专利> INDOLE DERIVATIVES AS HISTAMINE H3 RECEPTOR INHIBITORS FOR TREATMENT OF COGNITIVE DISORDERS AND DISORDERS OF SLEEP, OBESITY AND OTHER DISORDERS OF THE CENTRAL NERVOUS SYSTEM

INDOLE DERIVATIVES AS HISTAMINE H3 RECEPTOR INHIBITORS FOR TREATMENT OF COGNITIVE DISORDERS AND DISORDERS OF SLEEP, OBESITY AND OTHER DISORDERS OF THE CENTRAL NERVOUS SYSTEM

机译:吲哚衍生物作为组氨酸H3受体抑制剂可治疗中枢神经系统的认知障碍和睡眠障碍,肥胖症和其他疾病

摘要

1. The compound of the formula:! ! in which the spacer is! ! Y represents CH or N, provided that if Y represents CH, then n is 0-2; if Y is N, then n is 2-4; ! if Y is CH, then R1 and R2, taken together, are - (CH2) a-NR11- (CH2) 2-, where a is 1-2, which together with Y forms a piperidine or pyrrolidine ring, which is optional substituted by 1-3 groups selected from a fluorine atom, fluoroalkyl, (C1-C4) alkyl, alkoxyl, aryl, (C3-C7) cycloalkyl, heterocycloalkyl groups containing 1-2 heteroatoms selected from (O, S) and ( C1-C5) alkyl-O- (C1-C5) alkyl; and! if Y is N, then R1 and R2 independently represent a (C1-C5) alkyl or (C3-C6) cycloalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a 5-7 membered heterocyclic a ring system with 0-1 additional heteroatom selected from O and S, which is optionally substituted with 1-3 (C1-C5) alkyl, fluoroalkyl or (C3-C6) cycloalkyl groups, or R1 and R2, taken together, are - (CH2) a-NR11- (CH2) 2-, where a is 2-3, which together with Y forms a piperazine or homopiperazine ring, which, neo optionally substituted by 1-3 groups selected from a fluorine atom, fluoroalkyl, (C1-C4) alkyl, alkoxy, aryl, (C3-C7) cycloalkyl, heterocycloalkyl group containing 1-2 heteroatoms selected from (O, S), and (C1-C5) alkyl-O- (C1-C5) alkyl; ! R3 represents 0-2 groups selected from a halogen atom, (C1-C6) alkyl, (C1-C6) alkoxyl, (C3-C7) cycloalkyl, (C3-C7) cycloalkyl- (C1-C6) alkyl, heterocycloalkyl groups containing 1-3 heteroatoms selected from (O, S) and (C1-C3) alkyl-O- (C1-C5) alkyl�
机译:1.公式的化合物:! !垫片在其中! ! Y代表CH或N,如果Y代表CH,则n为0-2;如果Y为N,则n为2-4; !如果Y为CH,则R1和R2加在一起为-(CH2)a-NR11-(CH2)2-,其中a为1-2,其与Y一起形成哌啶或吡咯烷环,其可任选地被取代1-3个选自氟原子,氟烷基,(C1-C4)烷基,烷氧基,芳基,(C3-C7)环烷基,含有1-2个选自(O,S)和(C1-C5的杂原子的杂环烷基的基团)烷基-O-(C 1 -C 5)烷基;和!如果Y为N,则R 1和R 2独立地代表(C 1 -C 5)烷基或(C 3 -C 6)环烷基,或R 1和R 2与它们所连接的氮原子一起形成5-7元杂环a。具有0-1个选自O和S的额外杂原子的环系统,它们任选被1-3个(C1-C5)烷基,氟代烷基或(C3-C6)环烷基或R1和R2共同取代-( CH2)a-NR11-(CH2)2-,其中a为2-3,与Y一起形成哌嗪或高哌嗪环,它们可被1-3个选自氟原子,氟烷基的基团新取代(C1 -C4)烷基,烷氧基,芳基,(C3-C7)环烷基,含有1-2个选自(O,S)和(C1-C5)烷基-O-(C1-C5)烷基的杂原子的杂环烷基; ! R 3表示选自卤素原子,(C 1 -C 6)烷基,(C 1 -C 6)烷氧基,(C 3 -C 7)环烷基,(C 3 -C 7)环烷基-(C 1 -C 6)烷基,含有以下的杂环烷基的0-2基团。 1-3个选自(O,S)和(C1-C3)烷基-O-(C1-C5)烷基的杂原子。

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