3-(HETEROARYL-OXY)-2-ALKYL-1-AZA-BICYCLOALKYL DERIVATIVES AS ALPHA. 7-NACHR LIGANDS FOR THE TREATMENT OF CNS DISEASES
    2.
    发明申请
    3-(HETEROARYL-OXY)-2-ALKYL-1-AZA-BICYCLOALKYL DERIVATIVES AS ALPHA. 7-NACHR LIGANDS FOR THE TREATMENT OF CNS DISEASES 审中-公开
    3-(异丁氧基)-2-烷基-1-氮杂双环己基衍生物作为ALPHA。 用于治疗CNS疾病的7-NACHR配偶

    公开(公告)号:US20140057921A1

    公开(公告)日:2014-02-27

    申请号:US14068004

    申请日:2013-10-31

    Applicant: NOVARTIS AG

    CPC classification number: C07D453/02 C07D487/08

    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula (I) wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals in the prevention and treatment of psychotic and neurodegenerative disorders. The claimed compounds act as nicotinic acetylcholine receptors (NACHR) ligands.

    Abstract translation: 本发明涉及式(I)的1-氮杂 - 双环烷基衍生物,其中取代基如说明书中所定义,其制备方法,它们作为药物用于预防和治疗精神病和神经变性疾病。 所要求的化合物作为烟碱乙酰胆碱受体(NACHR)配体。

    1-AZA-BICYCLO[3.3.1]NONANES
    6.
    发明申请
    1-AZA-BICYCLO[3.3.1]NONANES 审中-公开
    1-AZA-BICYCLO [3.3.1] NONANES

    公开(公告)号:US20150087650A1

    公开(公告)日:2015-03-26

    申请号:US14558776

    申请日:2014-12-03

    Applicant: NOVARTIS AG

    CPC classification number: C07D471/08

    Abstract: The present invention relates to 1-aza-bicy-cloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R′); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.

    Abstract translation: 本发明涉及式(I)的1-氮杂 - 双环烷基衍生物; 其中取代基如本说明书中所定义,其制备方法,它们作为药物的用途以及包含它们的药物组合物。 式(I),其中A表示O或N(R'); Y表示一组式,或其中左键连接至A基团,右键连接至R基团; R代表取代或未取代的C 5 -C 10芳基,取代或未取代的杂-C 5 -C 10芳基,基团N(R 1)(R 4)或基团N(R 2)(CH 3 R 4)。 R代表氢,C1-C4烷基或CF3; R 2表示氢,C 1 -C 4烷基或CF 3; R3表示氢,C1-C4烷基或CF3; R4表示取代或未取代的C5-C10芳基或取代或未取代的C5-C10杂芳基; 在游离碱或酸加成盐形式。

    1-AZA-BICYCLO[3.3.1] NON-4-YL)-[5-(1H-INDOL-5-YL)-HETEROARYL]-AMINES AS CHOLINERGIC LIGANDS OF THE N-ACHR FOR THE TREATMENT OF PSYCHOTIC AND NEURODEGENERATIVE DISORDERS
    10.
    发明申请
    1-AZA-BICYCLO[3.3.1] NON-4-YL)-[5-(1H-INDOL-5-YL)-HETEROARYL]-AMINES AS CHOLINERGIC LIGANDS OF THE N-ACHR FOR THE TREATMENT OF PSYCHOTIC AND NEURODEGENERATIVE DISORDERS 审中-公开
    1-AZA-BICYCLO [3.3.1] NON-4-YL) - [5-(1H-吲哚-5-YL)-HETEROARYL] - 胺作为N-ACHR用于治疗心脏病和神经病变疾病的CHOLINERGG配体

    公开(公告)号:US20140256940A1

    公开(公告)日:2014-09-11

    申请号:US14285942

    申请日:2014-05-23

    Applicant: NOVARTIS AG

    CPC classification number: C07D471/08 A61K31/429

    Abstract: The present invention related to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5, represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate, Y represents one of the following groups: (Ia) in free base or acid addition salt form, to processes for their production, to pharmaceutical compositions comprising them and their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and neurodegenerative disorders.

    Abstract translation: 本发明涉及式(I)化合物,其中n代表0,1,2,3,4或5相互独立地表示羟基,氰基,硝基,卤素,烷基,烷氧基烷基羰基,烷氧基羰基,烷基胺,二烷基胺, 烷基羰基胺,烷基氨基甲酸酯,Y代表以下基团之一:游离碱或酸加成盐形式的(Ia),其制备方法,包含它们的药物组合物及其在制备用于治疗和/或 延迟精神病和神经退行性疾病的进展。

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