Amido spirocyclic amide and sulfonamide derivatives

Amido spirocyclic amide and sulfonamide derivatives

  • CN 104,520,290 A
  • Filed: 03/01/2013
  • Published: 04/15/2015
  • Est. Priority Date: 03/02/2012
  • Status: Active Application
First Claim
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1. a formula I:

  • Wherein;

    R is 8-, 9-or 10-unit bicyclic heteroaryl that (a) comprises a heteroatoms and 1,2 or 3 the extra atom N being selected from N, S and O, wherein said bicyclic heteroaryl is unsubstituted or one or more substituting groups through being selected from the group that is made up of deuterium, amino, alkylamino, dialkyl amido, alkyl, halo, cyano group, haloalkyl, hydroxyl, hydroxyalkyl and alkoxyl group replace, and one or more atom N of wherein said bicyclic heteroaryl are optionally N oxide compound;

    OrB heterocycloalkyl ring that 5-or the 6-unit of () and phenyl or monocycle heteroaryl-condensed 5-or 6-unit nitrogen is connected, wherein said phenyl or heteroaryl are unsubstituted or one or more substituting groups replacements through being selected from the group be made up of deuterium, amino, alkylamino, dialkyl amido, alkyl, halo, cyano group, haloalkyl, hydroxyl, hydroxyalkyl and alkoxyl group;

    AndR 1h ,-(C 1-4alkylidene group) 0-1c (O) R a,-(C 1-4alkylidene group) 0-1cO 2r a,-(C 1-4alkylidene group) 0-1s (O) R a, –

    (C 1-4alkylidene group) 0-1sO 2r a, –

    C (O) NH (R a), –

    C (O) N (R a) 2huo –

    C (O) C (O) NH (R a);

    Wherein each R abe independently (1) to be unsubstituted or through one or more R mthe alkyl that substituting group replaces, Wherein each R mindependently be selected from deuterium, hydroxyl ,-NR br c, alkoxyl group, cyano group, halo ,-C (O) alkyl ,-CO 2alkyl ,-CONR br c,-S (O) alkyl ,-SO 2alkyl ,-SO 2nR br c, aryl, heteroaryl, cycloalkyl, Heterocyclylalkyl, phenoxy group and-O-alkyl-OH;

    Wherein R bh or alkyl;

    R ch, alkyl, alkoxyalkyl, haloalkyl ,-C (O) alkyl ,-CO 2alkyl, –

    SO 2alkyl ,-C (O) NH 2or C (O) H;

    And R minterior each aryl, heteroaryl, cycloalkyl and Heterocyclylalkyl are unsubstituted or replace through being independently selected from following one or more substituting groups;

    alkyl, haloalkyl, hydroxyl ,-NR br c, alkoxyl group, halogenated alkoxy, cyano group, halo, oxo ,-C (O) alkyl ,-CO 2alkyl ,-C (O)-Heterocyclylalkyl ,-CONR br c,-S (O) alkyl ,-SO 2alkyl ,-SO 2-haloalkyl ,-SO 2nR br c, aryl, heteroaryl, cycloalkyl and Heterocyclylalkyl;

    Or two substituting groups form the heteroaryl, cycloalkyl or the heterocycloalkyl ring that condense together;

    Wherein each alkyl or alkoxyl group are unsubstituted or through phenyl, –

    NR br c, Heterocyclylalkyl, heteroaryl or-C (O) alkyl replace;

    With Each aryl, heteroaryl, cycloalkyl and Heterocyclylalkyl are unsubstituted or replace through alkyl, halo Huo –

    C (O) alkyl;

    (2) to be unsubstituted separately or through one or more R gthe phenyl that substituting group replaces, cycloalkyl, heteroaryl or Heterocyclylalkyl;

    Wherein each R gindependently be selected from alkyl, haloalkyl, hydroxyl ,-NR br c, alkoxyl group, halogenated alkoxy, cyano group, halo, oxo ,-C (O) alkyl ,-CO 2alkyl ,-C (O)-Heterocyclylalkyl ,-CONR br c,-S (O) alkyl ,-SO 2alkyl ,-SO 2-haloalkyl ,-SO 2nR br c, aryl, heteroaryl, cycloalkyl and Heterocyclylalkyl;

    Or two R gsubstituting group forms the phenyl, heteroaryl, cycloalkyl or the heterocycloalkyl ring that condense together;

    Wherein each alkyl or alkoxyl group are unsubstituted or Jing –

    NR br c, Heterocyclylalkyl, heteroaryl or-C (O) alkyl replace;

    With Each aryl, heteroaryl, cycloalkyl and Heterocyclylalkyl are unsubstituted or through alkyl, halo ,-CO 2wan Ji Huo –

    C (O) alkyl replaces;

    Or (3)–

    NR xR y

    Wherein R xh or alkyl;

    And R yh, alkyl, alkoxyalkyl, haloalkyl ,-C (O) alkyl ,-CO 2wan Ji Huo –

    SO 2alkyl;

    R 2and R 3respective is independently H or deuterium;

    And N is 1 or 2;

    Or its steric isomer, or the pharmacologically acceptable salts of this compound or steric isomer.

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