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11. 发明申请

US20090227583A1 2-AMINOQUINOLINES 失效
标题翻译： 2-氨基喹啉
公开(公告)号：US20090227583A1
公开(公告)日：2009-09-10
申请号：US12394072
申请日：2009-02-27
申请人： Sabine Kolczewski , Claus Riemer , Olivier Roche , Lucinda Steward , Juergen Wichmann , Thomas Woltering
发明人： Sabine Kolczewski , Claus Riemer , Olivier Roche , Lucinda Steward , Juergen Wichmann , Thomas Woltering
IPC分类号： A61K31/5377 , C07D215/38 , C07D417/12 , A61K31/47 , A61K31/4709 , C07D413/12 , C07D401/12 , A61K31/506 , A61K31/496 , A61P25/22 , A61P25/24 , A61P25/00
CPC分类号： C07D215/38 , C07D401/04 , C07D401/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein A, R1, R2, R3, R4, and R5 are as described herein, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonistsand are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
摘要翻译：本发明涉及其中A，R 1，R 2，R 3，R 4和R 5如本文所述的式（I）化合物，含有它们的药物组合物及其制备方法。这些化合物是5-HT5A受体拮抗剂，可用于预防和/或治疗抑郁症，焦虑障碍，精神分裂症，恐慌症，广场恐怖症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆，饮食行为障碍，性功能障碍，睡眠障碍，药物滥用，运动障碍如帕金森病，精神病或胃肠道疾病。

12. 发明申请

US20090209529A1 4,5-DIHYDRO-OXAZOL-2-YL AMINE DERIVATIVES 有权
标题翻译： 4,5-二氢 - 氧杂-2-氨基胺衍生物
公开(公告)号：US20090209529A1
公开(公告)日：2009-08-20
申请号：US12369782
申请日：2009-02-12
申请人： Matteo Andreini , Emanuele Gabellieri , Wolfgang Guba , Guido Marconi , Robert Narquizian , Eoin Power , Massimiliano Travagli , Thomas Woltering , Wolfgang Wostl
发明人： Matteo Andreini , Emanuele Gabellieri , Wolfgang Guba , Guido Marconi , Robert Narquizian , Eoin Power , Massimiliano Travagli , Thomas Woltering , Wolfgang Wostl
IPC分类号： A61K31/421 , C07D263/28 , C07D413/10 , A61K31/506 , A61K31/4439 , A61K31/538
CPC分类号： C07D263/28 , C07D413/10
摘要： The present invention relates to a compounds of formula I wherein R1, R1′, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (β-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
摘要翻译：本发明涉及式I化合物，其中R 1，R 1'，R 2，R 3，R 4，X，Ar和m如说明书和权利要求中所定义，及其药学上活性的酸加成盐。本发明的化合物具有Asp2（β-分泌酶，BACE1或Memapsin-2）抑制活性，并且可用于治疗特征在于升高的β-淀粉样蛋白水平或β-淀粉样蛋白沉积物，特别是阿尔茨海默氏病的疾病。

13. 发明申请

US20080081907A1 2-AMINOQUINOLINE DERIVATIVES 失效
标题翻译： 2-氨基喹啉衍生物
公开(公告)号：US20080081907A1
公开(公告)日：2008-04-03
申请号：US11859045
申请日：2007-09-21
申请人： Sabine Kolczewski , Claus Riemer , Lucinda Steward , Juergen Wichmann , Thomas Woltering
发明人： Sabine Kolczewski , Claus Riemer , Lucinda Steward , Juergen Wichmann , Thomas Woltering
IPC分类号： C07D405/14 , C07D215/38 , C07D401/02 , C07D413/14 , C07D417/14 , C07D409/02 , C07D405/02
CPC分类号： C07D215/38 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein X, Y, Ar1, and Ar2 are as defined in the specification.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中X，Y，Ar 1和Ar 2如本说明书中所定义。

14. 发明申请

US20070167460A1 Acetylenyl-pyrazolo-pyrimidine derivatives 有权
标题翻译：乙酰基 - 吡唑并嘧啶衍生物
公开(公告)号：US20070167460A1
公开(公告)日：2007-07-19
申请号：US11726807
申请日：2007-03-23
申请人： Silvia McArthur , Erwin Goetschi , Wylie Palmer , Juergen Wichmann , Thomas Woltering
发明人： Silvia McArthur , Erwin Goetschi , Wylie Palmer , Juergen Wichmann , Thomas Woltering
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： 035 The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufacture of such compounds, pharmaceutical compositions containing them, and methods for treating CNS disorders.
摘要翻译： 035本发明涉及式（I）化合物：其中R 1至R 3，A，M，L，E，G和J定义如说明和权利要求。本发明还涉及制备这些化合物的方法，含有它们的药物组合物和治疗CNS障碍的方法。

15. 发明申请

US20070072879A1 Novel compounds as metabotropic glutamate receptor antagonists 失效
标题翻译：新型化合物作为代谢型谷氨酸受体拮抗剂
公开(公告)号：US20070072879A1
公开(公告)日：2007-03-29
申请号：US11524135
申请日：2006-09-20
申请人： Silvia McArthur , Erwin Goetschi , Juergen Wichmann , Thomas Woltering
发明人： Silvia McArthur , Erwin Goetschi , Juergen Wichmann , Thomas Woltering
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention relates to compounds of formula (I) wherein A, E G, J, L, M, R1, R2, and R3 are as defined in the specification and claims. The invention also relates to pharmaceutical compositions containing such compounds and methods for preparing the compounds and compositions. The compounds are metabotropic glutamate receptor antagonists and are useful for the treatment of a variety of CNS disorders.
摘要翻译：本发明涉及式（I）的化合物，其中A，EG，J，L，M，R 1，R 2和R 3， SUP>如说明书和权利要求中所定义。本发明还涉及含有这些化合物的药物组合物和用于制备化合物和组合物的方法。化合物是代谢型谷氨酸受体拮抗剂，可用于治疗各种CNS疾病。

16. 发明申请

US20060183756A1 Pyrrazolo-pyrimidine derivatives 失效
标题翻译：吡唑并嘧啶衍生物
公开(公告)号：US20060183756A1
公开(公告)日：2006-08-17
申请号：US11348105
申请日：2006-02-06
申请人： Silvia Gatti McArthur , Erwin Goetschi , Juergen Wichmann , Thomas Woltering
发明人： Silvia Gatti McArthur , Erwin Goetschi , Juergen Wichmann , Thomas Woltering
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to pyrrazolo-pyrimidine derivatives of formula (I): wherein R1 to R4 and A are as defined in the specification, a process for the manufacture thereof, their use for treating or preventing metabotropic glutamate receptors mediated disorders, their use for the preparation of medicaments for treating such disorders and pharmaceutical compositions containing said derivatives.
摘要翻译：本发明涉及式（I）的吡唑并嘧啶衍生物：其中R 1至R 4和A如说明书中所定义，其制备方法，它们用于治疗或预防代谢型谷氨酸受体介导的病症，其用于制备用于治疗这种病症的药物的用途和含有所述衍生物的药物组合物。

17. 发明申请

US20050234048A1 Glutamate receptor antagonists 失效
公开(公告)号：US20050234048A1
公开(公告)日：2005-10-20
申请号：US11146693
申请日：2005-06-07
申请人： Geo Adam , Alexander Alanine , Erwin Goetschi , Vincent Mutel , Thomas Woltering
发明人： Geo Adam , Alexander Alanine , Erwin Goetschi , Vincent Mutel , Thomas Woltering
IPC分类号： A61K31/55 , A61K31/551 , A61K31/5513 , A61P1/08 , A61P3/08 , A61P9/08 , A61P13/02 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/34 , A61P25/36 , A61P27/02 , A61P29/02 , A61P43/00 , C07D243/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/10 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/08 , C07D409/14 , C07D413/10 , C07D417/02 , C07D417/04 , C07D417/06 , C07D417/10 , C07D417/14 , C07D43/14
CPC分类号： C07D401/04 , C07D243/12 , C07D403/10 , C07D405/06 , C07D413/10 , C07D417/06 , C07D417/10
摘要： The present invention is a compound of formula wherein X is an ethynediyl group, R1, R2 and R3 are as defined in the specification.

18. 发明申请

US20050130992A1 Pyrazolo-pyridine 失效
标题翻译：吡唑并吡啶
公开(公告)号：US20050130992A1
公开(公告)日：2005-06-16
申请号：US10948970
申请日：2004-09-24
申请人： Juergen Wichmann , Thomas Woltering
发明人： Juergen Wichmann , Thomas Woltering
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The present invention relates to novel pyrazolo- and imidazo-pyrimidine derivatives of formula I wherein A, D, E, L, M, Q, R1, R2 and R3 are as defined hereinabove. The present invention also relates to a process for their preparation, a pharmaceutical composition containing said derivatives and a method of treating or preventing acute or chronic neurological disorder comprising administering to a patient in need of such treatment a pharmaceutical composition comprising a therapeutically effective amount of at least one such derivatives. These disorders include acute and chronic disorders
摘要翻译：本发明涉及式I的新型吡唑并咪唑并嘧啶衍生物，其中A，D，E，L，M，Q，R 1，R 2和R 2 ＆lt; SUP＆gt; 3＆gt;如上文所定义。本发明还涉及其制备方法，含有所述衍生物的药物组合物和治疗或预防急性或慢性神经障碍的方法，包括向需要这种治疗的患者施用药物组合物，其包含治疗有效量的至少一个此类衍生物。这些疾病包括急性和慢性疾病

19. 发明申请

US20050049243A1 Pharmaceutical composition comprising an AChE inhibitor and a mGluR2 antagonist 有权
标题翻译：包含AChE抑制剂和mGluR2拮抗剂的药物组合物
公开(公告)号：US20050049243A1
公开(公告)日：2005-03-03
申请号：US10896494
申请日：2004-07-22
申请人： Theresa Ballard , Silvia McArthur , Erwin Goetschi , Juergen Wichmann , Thomas Woltering
发明人： Theresa Ballard , Silvia McArthur , Erwin Goetschi , Juergen Wichmann , Thomas Woltering
IPC分类号： A61K31/4535 , A61K31/473 , A61K31/55 , A61K31/551 , A61K31/662 , A61K31/7068 , A61K45/06 , A61K31/5513
CPC分类号： A61K45/06 , A61K31/4535 , A61K31/473 , A61K31/55 , A61K31/551 , A61K31/662 , A61K31/7068 , A61K2300/00
摘要： The present invention relates to a pharmaceutical composition comprising an inhibitor of acetylcholinesterase (AChE inhibitor) and a metabotropic glutamate receptor 2 antagonist (mGluR2 antagonist) and a pharmaceutically acceptable excipient. The invention also relates to a method of treating and/or preventing acute and/or chronic neurological disorders comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said AChE inhibitor and mGluR2 antagonist as well as a kit comprising said AChE inhibitor and mGluR2 antagonist. In particular, the mGluR2 antagonist relates to the compound of formula I wherein, R1, R2, R3, X and Y are described hereinabove. The combination of the AChE inhibitor and mGluR2 antagonist is useful for treating and/or preventing chronic neurological disorders. These disorders include Alzheimer's disease and mild cognitive impairment.
摘要翻译：本发明涉及包含乙酰胆碱酯酶（AChE抑制剂）抑制剂和代谢型谷氨酸受体2拮抗剂（mGluR2拮抗剂）和药学上可接受的赋形剂的药物组合物。本发明还涉及治疗和/或预防急性和/或慢性神经障碍的方法，包括向需要这种治疗和/或预防的患者施用治疗有效量的所述AChE抑制剂和mGluR2拮抗剂以及试剂盒包括所述AChE抑制剂和mGluR2拮抗剂。特别地，mGluR2拮抗剂涉及式I化合物，其中R 1，R 2，R 3，X和Y如上所述。 AChE抑制剂和mGluR2拮抗剂的组合可用于治疗和/或预防慢性神经障碍。这些疾病包括阿尔茨海默病和轻度认知障碍。

20. 发明授权

US08815881B2 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds 有权
标题翻译： 1,4,5,6-四氢 - 嘧啶-2-基胺化合物
公开(公告)号：US08815881B2
公开(公告)日：2014-08-26
申请号：US13196933
申请日：2011-08-03
申请人： David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Benoit Hornsperger , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
发明人： David Banner , Emanuele Gabellieri , Wolfgang Guba , Hans Hilpert , Benoit Hornsperger , Roland Humm , Harald Mauser , Alexander V. Mayweg , Robert Narquizian , Emmanuel Pinard , Mark Rogers-Evans , Thomas Woltering , Wolfgang Wostl
IPC分类号： C07D239/22 , A61K31/513
CPC分类号： C07D417/12 , A61K31/513 , C07D239/22 , C07D239/70 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
摘要翻译：本发明涉及下式化合物或其药学上可接受的盐：其中R 1至R 9如下所述。这些化合物是BACE2抑制剂，可用作治疗和/或预防性治疗诸如糖尿病，特别是2型糖尿病和其它代谢疾病的药物。

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