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US08697744B2 Substituted 5,6-dihydro-4H-thiazolo[4,5-E]indazoles and their use as positive allosteric modulators of metabotropic glutamate receptors 失效
取代的5,6-二氢-4H-噻唑并[4,5-E]吲唑及其作为代谢型谷氨酸受体的正变构调节剂的用途

  • Patent Title: Substituted 5,6-dihydro-4H-thiazolo[4,5-E]indazoles and their use as positive allosteric modulators of metabotropic glutamate receptors
  • Patent Title (中): 取代的5,6-二氢-4H-噻唑并[4,5-E]吲唑及其作为代谢型谷氨酸受体的正变构调节剂的用途
  • Application No.: US12998955
    Application Date: 2010-01-12
  • Publication No.: US08697744B2
    Publication Date: 2014-04-15
  • Inventor: Christelle Boléa , Sylvain Celanire
  • Applicant: Christelle Boléa , Sylvain Celanire
  • Applicant Address: CH Geneva
  • Assignee: Addex Pharma S.A.
  • Current Assignee: Addex Pharma S.A.
  • Current Assignee Address: CH Geneva
  • Agency: Law Offices of Gerard Bilotto, P.C.
  • Agent Gerard Bilotto
  • Priority: GB0900404.5 20090112
  • International Application: PCT/EP2010/050304 WO 20100112
  • International Announcement: WO2010/079238 WO 20100715
  • Main IPC: A61K31/30
  • IPC: A61K31/30
Substituted 5,6-dihydro-4H-thiazolo[4,5-E]indazoles and their use as positive allosteric modulators of metabotropic glutamate receptors
Abstract:
The present invention relates to novel compounds of Formula (I), wherein X1, X2, Y, Z1, Z2, Z3, M and (A)m are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
Abstract(Chinese):

本发明涉及新的式（I）化合物，其中X 1，X 2，Y，Z 1，Z 2，Z 3，M和（A）m如式（I）所定义; 本发明化合物是代谢型谷氨酸受体的调节剂 - 亚型4（“mGluR4”），其可用于治疗或预防中枢神经系统疾病以及由mGluR4受体调节的其它障碍。 本发明还涉及药物组合物和这些化合物在制备药物中的用途，以及这些化合物用于预防和治疗涉及mGluR4的疾病的用途。

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