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    HETEROCYCLIC COMPOUNDS WITH AFFINITY TO MUSCARINIC RECEPTORS
    1.
    发明申请
    HETEROCYCLIC COMPOUNDS WITH AFFINITY TO MUSCARINIC RECEPTORS 审中-公开
    具有对肌肉受体的亲和性的杂环化合物

    公开(公告)号：WO2008129054A3

    公开(公告)日：2009-02-05

    申请号：PCT/EP2008054897

    申请日：2008-04-23

    Applicant: SOLVAY PHARM BV ,  STOIT AXEL ,  COOLEN HEIN K A C ,  KRUSE CORNELIS G ,  TERWEL LOUISE HEIR OF REINDERS

    Inventor： STOIT AXEL ,  COOLEN HEIN K A C ,  KRUSE CORNELIS G ,  TERWEL LOUISE HEIR OF REINDERS

    IPC: C07D401/04 ,  A61K31/439 ,  A61K31/4427 ,  A61K31/4439 ,  A61P25/28 ,  C07D401/14 ,  C07D413/04 ,  C07D453/02 ,  C07D471/08

    CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D453/02 ,  C07D471/08

    Abstract: The present invention relates to heterocyclic compounds of the formula (I) wherein - the heterocycle comprises two double bonds which may be present at several positions, represented by the dashed lines ( -- ); - the heterocycle contains two heteroatoms, - W being N or NH; - Y being CH, O or NH, wherein if Y is O, X1 is CH and X2 is the residue C-Z-R2 or C-R3, wherein Z is NH, O, or S; and if Y is CH or NH, one of X1 and X2 is CH or N, the other being the residue C-Z-R2 or C-R3, wherein Z is NH or S; - R1 is selected from the structures (a), (b) and (c): - R2 is selected from (C1-C10)alkyl, (C2-C10)alkenyl and (C2-C10)alkynyl, optionally independently substituted with one or more substituents selected from halogen, hydroxy, cyano, oxo, (C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkenyloxy, (C1-C6)alkenylthio, (C1-C4)alkoxy(C1-C4)alkoxy, (C5-C7)cycloalkyl, a 5-membered unsaturated heterocycle (optionally substituted with halogen), phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; or - R2 is an unbranched (C2-C8)alkyl substituted at the Za-symbol of a group with the formula (Ia) wherein if X1 is CH or N1 X1 is CH or N and X2a is C-Za-, or if X1 is C-Z-R2, X1a is C-Za- and X2a is CH or N; and the symbols Wa, Ya and Za and the substituent R1a have the same meanings as defined previously for the symbols W, Y and Z and the substituent R1, and are not independently selected, each of the symbols Wa, Ya and Za and the substituent R1 a representing identical symbols and substituents, respectively, as the symbols W, Y and Z and the substituent R1 in the other part of the structure of formula (I); - R3 is selected from (C4-C10) alkyl, (C2-C10) alkenyl and (C2-C10) alkynyl, optionally independently substituted with one or more substituents selected from halogen, hydroxy, cyano, (C1C6) alkoxy, (C1C6) alkylthio, (C1C6)alkenyloxy, (C1C6) alkenylthio, (C1-C4) alkoxy (C1-C4) alkoxy, (C5-C7) cycloalkyl, a 5-membered unsaturated heterocycle optionally substituted with halogen, phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to muscarinic receptors and may be used in the treatment, alleviation or prevention of muscarinic receptor mediated diseases and conditions.

    Abstract translation: 本发明涉及式（I）的杂环化合物，其中 - 杂环包含两个双键，其可以存在于由虚线（ - ）表示的几个位置。 - 杂环含有两个杂原子，-W为N或NH; - Y是CH，O或NH，其中如果Y是O，则X1是CH，X2是残基C-Z-R2或C-R3，其中Z是NH，O或S; 并且如果Y是CH或NH，则X1和X2之一是CH或N，另一个是残基C-Z-R2或C-R3，其中Z是NH或S; -R 1选自（C 1 -C 10）烷基，（C 2 -C 10）烯基和（C 2 -C 10）炔基，任选独立地被一个 （C1-C6）烷氧基，（C1-C6）烷氧基，（C1-C6）烯硫基，（C1-C4）烷氧基（C1- C4烷氧基，（C5-C7）环烷基，5元不饱和杂环（任选被卤素取代），苯基，苯氧基和苯硫基，其中苯基任选被卤素取代; 或 - R 2是在具有式（Ia）的基团的Za符号取代的未支化的（C 2 -C 8）烷基，其中如果X 1是CH或N 1是CH或N 1且X 2是C a Z a，或者如果X 1 是CZ-R2，X1a是C-Za，X2a是CH或N; 并且符号Wa，Ya和Za以及取代基R 1a具有与前面对符号W，Y和Z以及取代基R所定义的相同的含义，并且不是独立地选择，每个符号Wa，Ya和Za以及取代基 R1a分别表示与式（I）结构的另一部分中的符号W，Y和Z以及取代基R 1相同的符号和取代基; 羟基，氰基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷基，（C 2 -C 10） 烷基硫基，（C1C6）烯氧基，（C1C6）烯基硫代，（C1-C4）烷氧基（C1-C4）烷氧基，（C5-C7）环烷基，任选被卤素，苯基，苯氧基和苯硫基取代的5元不饱和杂环，其中 苯基任选被卤素取代; 或其药学上可接受的盐，溶剂合物或水合物。 本发明的化合物对毒蕈碱受体具有亲和力，可用于治疗，缓解或预防毒蕈碱受体介导的疾病和病症。

    2.
    发明专利
    未知

    公开(公告)号：BRPI0713631A2

    公开(公告)日：2012-10-23

    申请号：BRPI0713631

    申请日：2007-07-05

    Applicant: SOLVAY PHARM BV

    Inventor： STOIT AXEL ,  COOLEN HEIN K A C ,  VAN DER NEUT MARTINA A W ,  KRUSE CORNELIS G

    IPC: C07D471/04 ,  A61K31/40 ,  A61K31/445 ,  A61P25/16 ,  A61P25/28 ,  A61P25/30 ,  C07D487/04 ,  C07D519/00

    Abstract: The invention concerns azaindole derivatives having the general formula (I) wherein the symbols have the meanings given in the specification. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.

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