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41. 发明申请

US20100120751A1 SPIRO-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENES 有权
标题翻译： SPIRO-5,6-二氢-4H-2,3,5,10B-四氮杂苯并[E]三烯
公开(公告)号：US20100120751A1
公开(公告)日：2010-05-13
申请号：US12613554
申请日：2009-11-06
申请人： Caterina Bissantz , Erwin Goetschi , Roland Jakob-Roetne , Raffaello Masciadri , Emmanuel Pinard , Hasane Ratni , Mark Rogers-Evans , Patrick Schnider
发明人： Caterina Bissantz , Erwin Goetschi , Roland Jakob-Roetne , Raffaello Masciadri , Emmanuel Pinard , Hasane Ratni , Mark Rogers-Evans , Patrick Schnider
IPC分类号： A61K31/5513 , C07D487/14 , A61P5/00
CPC分类号： C07D487/04 , C07D491/107 , C07D495/10
摘要： The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2, R3, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
摘要翻译：本发明涉及式I的螺 - 二氢四氮杂苯并薁，即螺-5,6-二氢-4H-2,3,5,10b-四氮杂 - 苯并[e]薁其中R1，R2，R3，X，Y， Z，m和n如本文所述。根据本发明的化合物作为V1a受体调节剂，并且可用作在痛经，男性或女性性功能障碍，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，焦虑症的周围和中心作用的治疗剂抑郁障碍，强迫症，孤独症谱系障碍，精神分裂症和侵略行为。

42. 发明申请

US20090143580A1 SUBSTITUTED PYRAZOLO [1,5-a] PYRIMIDINES AS METABOTROPIC GLUTAMATE ANTAGONISTS 失效
标题翻译：取代的吡唑并[1,5-a]吡啶类作为代谢型谷氨酸拮抗剂
公开(公告)号：US20090143580A1
公开(公告)日：2009-06-04
申请号：US12348962
申请日：2009-01-06
申请人： Silvia Gatti McArthur , Erwin Goetschi , Juergen Wichmann , Thomas Johannes Woltering
发明人： Silvia Gatti McArthur , Erwin Goetschi , Juergen Wichmann , Thomas Johannes Woltering
IPC分类号： C07D487/04 , C07D471/04
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）化合物，其中A，E G，J，L，M，R 1，R 2和R 3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。

43. 发明申请

US20070232583A1 Pyridine and pyrimidine derivatives as mGIuR2 antagonists 有权
标题翻译：吡啶和嘧啶衍生物作为mGIuR2拮抗剂
公开(公告)号：US20070232583A1
公开(公告)日：2007-10-04
申请号：US11726575
申请日：2007-03-22
申请人： Silvia Gatti McArthur , Erwin Goetschi , Juergen Wichmann , Thomas Johannes Woltering
发明人： Silvia Gatti McArthur , Erwin Goetschi , Juergen Wichmann , Thomas Johannes Woltering
IPC分类号： A61K31/513 , A61K31/506 , C07D405/14 , C07D403/02 , C07D409/14
CPC分类号： C07D239/30 , C07D213/61 , C07D213/64 , C07D213/79 , C07D213/81 , C07D213/84 , C07D239/28 , C07D239/34 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07F5/025
摘要： The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, X, Y, R1, R2, R3 and R4 are as defined in the description and claims.
摘要翻译：本发明涉及式（I）化合物，其制备方法，含有它们的药物组合物及其用于治疗CNS病症的用途：其中A，B，X，Y，R 1， R 2，R 3和R 4如在说明书和权利要求书中所定义。

44. 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。

45. 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。

46. 发明授权

US07163936B2 β-lactam compounds and process for producing the same 失效
标题翻译： β-内酰胺化合物及其制备方法
公开(公告)号：US07163936B2
公开(公告)日：2007-01-16
申请号：US10416334
申请日：2001-11-06
申请人： Makoto Sunagawa , Katsumi Kubota , Masanori Itoh , Erwin Goetschi
发明人： Makoto Sunagawa , Katsumi Kubota , Masanori Itoh , Erwin Goetschi
IPC分类号： A61K31/40 , C07D487/04
CPC分类号： C07D477/20 , C07D477/06
摘要： 1. A β-lactam compound of the formula [1]; wherein R1 is a lower alkyl, a lower alkyl substituted by a hydroxy; R2 is a hydrogen, a lower alkyl; X is O, S, NH; m and n are 0 to 4, Y1 is a halogen, cyano, a hydroxy, an amino, a lower alkyloxy, a lower alkylamino, a carboxy, a carbamoyl, a lower alkyl, etc., Y2 is hydrogen, an alkyl, cyano, —C(R3)═NR4 (wherein R3 and R4 are hydrogen, an amino, an alkyl, etc., or R3 and R4 may combine each other together with the nitrogen atom to form a 5- to 7-membered heterocyclic group), or a pharmaceutically acceptable salt thereof, or a non-toxic ester thereof, which has an excellent antibacterial activity against Gram-positive bacteria, especially against MRSA and MRCNS.
摘要翻译： 1.式[1]的β-内酰胺化合物; 其中R 1是低级烷基，被羟基取代的低级烷基; R 2是氢，低级烷基; X是O，S，NH; m和n为0〜4，Y 1为卤素，氰基，羟基，氨基，低级烷氧基，低级烷基氨基，羧基，氨基甲酰基，低级烷基等， Y 2是氢，烷基，氰基，-C（R 3） - NR 4（其中R 3 O） >和R 4是氢，氨基，烷基等，或R 3和R 4可以彼此结合，氮原子形成5-至7-元杂环基）或其药学上可接受的盐或其无毒性酯，其对革兰氏阳性细菌，特别是抗MRSA和MRCNS具有优异的抗菌活性。

47. 发明授权

US07151098B2 Glutamate receptor antagonists 失效
公开(公告)号：US07151098B2
公开(公告)日：2006-12-19
申请号：US11363351
申请日：2006-02-27
申请人： Geo Adam , Alexander Alanine , Erwin Goetschi , Vincent Mutel , Thomas Johannes Woltering
发明人： Geo Adam , Alexander Alanine , Erwin Goetschi , Vincent Mutel , Thomas Johannes Woltering
IPC分类号： C07D243/12 , C07D417/04 , C07D413/10 , A61K31/55
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.

48. 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。

49. 发明授权

US07018998B2 Glutamate receptor antagonists 失效
标题翻译：谷氨酸受体拮抗剂
公开(公告)号：US07018998B2
公开(公告)日：2006-03-28
申请号：US11146693
申请日：2005-06-07
申请人： Geo Adam , Alexander Alanine , Erwin Goetschi , Vincent Mutel , Thomas Johannes Woltering
发明人： Geo Adam , Alexander Alanine , Erwin Goetschi , Vincent Mutel , Thomas Johannes Woltering
IPC分类号： C07D243/12 , C07D417/04 , C07D413/10 , A61K31/55
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.
摘要翻译：本发明是下式的化合物，其中X是亚乙二基，R 1，R 2和R 3如本说明书中所定义。

50. 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.

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