公开(公告)号：US09475811B2

公开(公告)日：2016-10-25

申请号：US14558776

申请日：2014-12-03

Applicant: NOVARTIS AG

Inventor： Dominik Feuerbach ,  Werner Müller ,  Bernard Lucien Roy ,  Thomas Troxler ,  Konstanze Hurth ,  Mathias Frederiksen

IPC: C07D471/08

CPC classification number: C07D471/08

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 and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); 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.

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

Inventor： Dominik FEUERBACH ,  Werner Müller ,  Bernard Lucien ROY ,  Thomas TROXLER ,  Konstanze HURTH ,  Mathias FREDERIKSEN

IPC: C07D471/08

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。