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41. 发明公开

EP1932844A1 BRIDGED CYCLIC AMINE COMPOUND AND PEST CONTROL AGENT 有权
标题翻译： QUERVERNETZTE CYCLISCHE AMINVERBINDUNGEN UND MITTEL ZURSCHÄDLINGSBEKÄMPFUNG
公开(公告)号：EP1932844A1
公开(公告)日：2008-06-18
申请号：EP06811460.2
申请日：2006-10-06
申请人： NIPPON SODA CO., LTD.
发明人： HAMAMOTO, Isami , TAKAHASHI, Jun , YANO, Makio , KAWAGUCHI, Masahiro , HANAI, Daisuke , IWASA, Takao
IPC分类号： C07D451/14 , A01N43/42 , A01N43/56 , A01N43/58 , A01N43/78 , A01N43/824 , A01N43/90 , A01P7/02 , A01P7/04 , C07D471/04 , C07D491/08
CPC分类号： C07D221/22 , A01N43/40 , A01N43/42 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/76 , A01N43/78 , A01N43/80 , A01N43/82 , A01N43/90 , C07D211/54 , C07D211/58 , C07D221/24 , C07D237/08 , C07D241/16 , C07D401/04 , C07D401/12 , C07D417/04
摘要： Cyclic amine compounds represented by formula (1)

or salts thereof or N-oxides thereof, wherein Cy 1 represents an unsubstituted or substituted aromatic ring; X represents oxygen, sulfur, unsubstituted or substituted nitrogen, sulfinyl, or sulfonyl; R 1 a and R 2 a , R 1 a and R 4 a , R 2 a and R 3 a , or R 3 and R 4 a form saturated rings together; R 1 a , R 1 b , R 2 a , R 2 b , R 3 a , R 3 b , R 4 a , R 4 b , and R 5 which do not form the saturated rings are each independently hydrogen, hydroxyl, halogen, unsubstituted or substituted amino, nitro, or an organic group; Cy 2 represents an unsubstituted or substituted aromatic ring with a proviso that Cy 2 is an unsubstituted or substituted heteroaromatic ring when R 1 a and R 2 a form a saturated ring together and Cy 1 is an unsubstituted or substituted phenyl, and Cy 2 is a substituted pyridin-2-yl having one or more cyano as a substituent when Cy 1 is an unsubstituted or substituted phenyl and Cy 2 is a pyridin-2-yl.
摘要翻译：由式（1）表示的环胺化合物或其盐或其N-氧化物，其中Cy 1表示未取代或取代的芳环; X表示氧，硫，未取代或取代的氮，亚磺酰基或磺酰基; R 1 a和R 2 a，R 1 a和R 4 a，R 2 a和R 3 a，或R 3和R 4 a形成饱和的环; 不形成饱和环的R 1a，R 1b，R 2a，R b，R 3 a，R 3 b，R 4 a，R 4 b和R 5各自独立地为氢，羟基，卤素，未取代或取代的氨基，硝基或有机基团; Cy 2表示未取代或取代的芳环，条件是当R 1 a和R 2 a一起形成饱和环时，Cy 2为未取代或取代的杂芳环，Cy 1为未取代或取代的苯基，Cy 2为当Cy 1是未取代或取代的苯基且Cy 2是吡啶-2-基时，具有一个或多个氰基作为取代基的取代的吡啶-2-基。

43. 发明公开

EP1873150A1 Fluorinated indoleamides useful as ligands of the ORL-1 receptor 审中-公开
标题翻译： Fluorierte Indolamide als Ligandenfürden ORL-1 Rezeptor
公开(公告)号：EP1873150A1
公开(公告)日：2008-01-02
申请号：EP06116414.1
申请日：2006-06-30
申请人： NIKEM RESEARCH S.R.L.
发明人： Ronzoni, Silvano , Gagliardi, Stefania
IPC分类号： C07D401/06 , C07D401/14 , C07D491/08 , A61K31/454 , A61K31/439 , A61P29/00
CPC分类号： C07D401/06 , C07D401/14 , C07D491/08
摘要： New ligands for the ORL-1 receptor are described, useful for antagonising the activity of said receptors in a patient in need thereof, and for preventing and treating illnesses dependent on the activation of this receptor. The new compounds conform to structural formula (I)

In formula (I) inter alia, at least one of the two R 4 substituents is a fluorine atom and at least one among R2 and R3 is a group -(CH 2 ) n -CONR a R b , where R1, R2, R3, R4, n, R a , R b are defined in the description.
摘要翻译：描述了ORL-1受体的新配体，其可用于拮抗有需要的患者中所述受体的活性，并且用于预防和治疗依赖于该受体活化的疾病。新化合物符合结构式（I）在式（I）中，特别地，两个R 4取代基中的至少一个是氟原子，R2和R3中的至少一个是基团 - （CH 2）n -CONR R b，其中R 1，R 2，R 3，R 4，n，R a，R b在说明书中定义。

44. 发明公开

EP1848694A1 HETEROCYCLIC SUBSTITUTED PHENYL METHANONES AS INHIBITORS OF THE GLYCINE TRANSPORTER 1 有权转让
标题翻译： HETEROCYCLSCHE取代的甘氨酸1的抑制剂苯甲
公开(公告)号：EP1848694A1
公开(公告)日：2007-10-31
申请号：EP06706475.8
申请日：2006-01-30
申请人： F. Hoffmann-Roche AG
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger, David , PINARD, Emmanuel
IPC分类号： C07D209/44 , C07D403/04 , C07D471/04 , C07D209/08 , C07D231/56 , C07D235/06 , C07D417/04 , C07D401/04 , C07D409/04 , C07D487/04 , C07D209/88 , C07D405/04 , C07D491/08 , C07D498/08 , C07D413/04
CPC分类号： C07D471/04 , C07D209/08 , C07D209/44 , C07D209/46 , C07D209/88 , C07D231/56 , C07D235/06 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07D487/04 , C07D491/08
摘要： The present invention relates to compounds of general formula (I) wherein (i) is an aromatic or partially aromatic bicyclic amine, which may contain one or two additional N-atoms, selected from the group consisting of (a), (b), (c), (d), (e), (f), (g), (h) and to pharmaceutically acceptable acid addition salts thereof.

45. 发明公开

EP1716153A2 METHODS, COMPOSITIONS, AND APPARATUSES FOR FORMING MACROCYCLIC COMPOUNDS 失效
标题翻译：方法，组合物和装置用于形成大环CONNECTIONS
公开(公告)号：EP1716153A2
公开(公告)日：2006-11-02
申请号：EP05812865.3
申请日：2005-02-17
申请人： Johnson, Thomas E. , Fowler, Billy T.
发明人： Johnson, Thomas E. , Fowler, Billy T.
IPC分类号： C07D491/08
CPC分类号： C07D291/08 , C07D313/00 , C07D323/00
摘要： This invention relates to methods, compositions, and apparatuses for producing macrocyclic compounds. First, one or more reactants are provided in a reaction medium, which are capable of forming the macrocyclic compound through a desired reaction pathway that includes at least cyclization, and which are further capable of forming undesired oligomers through a undesired reaction pathway that includes undesirable oligomerization. Oligomerization of such reactions in the reaction medium is modulated to reduce formation of undesired oligomers and/or to reduce separation of the undesired oligomers from the reaction medium, relative to a corresponding unmodulated oligomerization reaction, thereby maximizing yields of the macrocyclic compound. The macrocyclic compound so formed is then recovered from the reaction medium. Preferably, the macrocyclic compound spontaneously separates from the reaction medium via phase separation. More preferably, the macrocyclic compound spontaneous precipitates from the reaction medium and therefore can be easily recovered by simple filtration.

46. 发明公开

EP1522542A1 THERAPEUTIC OR PREVENTIVE AGENT FOR NAUSEA/VOMITING 审中-公开
标题翻译：治疗BZW PROPHYLAKTISCHES MITTEL GEGENÜBELKEIT/ ERBRECHEN
公开(公告)号：EP1522542A1
公开(公告)日：2005-04-13
申请号：EP03741305.1
申请日：2003-07-10
申请人： TORAY INDUSTRIES, INC.
发明人： KAWAI, Koji , SAITO, Akiyoshi , SUZUKI, Tomohiko , HASEBE, Ko , SUZUKI, Tsutomu
IPC分类号： C07D491/18 , C07D491/22 , C07D491/08 , A61K45/00 , A61K31/485 , A61P1/08 , A61P25/00
CPC分类号： A61K31/485 , C07D491/18
摘要： The present invention provides a therapeutic or prophylactic agent for preventing nausea and vomiting. The agent includes a morphinan derivative represented by general formula (I):
or a pharmacologically acceptable acid addition salt thereof as an active ingredient,
(where R 1 represents, for example, a cyclopropylmethyl group, R 2 and R 3 represent, for example, a hydroxy or methoxy group, R 4 and R 5 together form, for example, an -O- bond, R 6 represents, for example, a hydrogen atom, Q represents a substituted or unsubstituted group represented by, for example, the following formula:
where X represents, for example, NH or NMe).
The compounds of the present invention can be widely used as medicines against vomiting caused by emetic drugs. In particular, the compounds of the present invention are useful as therapeutic or prophylactic agents for preventing nausea and vomiting caused by µ-agonists represented by morphine.
摘要翻译：本发明提供了用于预防恶心和呕吐的治疗或预防剂。该试剂包括由通式（I）表示的吗啡喃衍生物：或其药理学上可接受的酸加成盐作为活性成分（其中R 1表示例如环丙基甲基，R 2和 R 3表示例如羟基或甲氧基，R 4和R 5一起形成例如-O-键，R 6表示例如氢原子，Q 表示由例如下式表示的取代或未取代的基团：其中X表示例如NH或NMe的。本发明的化合物可广泛用作抗呕吐药物引起的呕吐药物。特别地，本发明的化合物可用作预防恶心和呕吐引起的恶心和呕吐的治疗或预防剂。

47. 发明公开

EP1451154A2 INHIBITORS OF CYTOSOLIC PHOSPHOLIPASE A2 有权转让
标题翻译：抑制剂胞浆磷脂酶A2
公开(公告)号：EP1451154A2
公开(公告)日：2004-09-01
申请号：EP02786829.8
申请日：2002-12-02
申请人： Wyeth
发明人： MCKEW, John, Caedmon , TAM, Steve, Yik-Kai , CLARK, James, Donald , LEE, Katherine, Lin , CHEN, Lihren , THAKKER, Paresh , SUM, Fuk-Wah , BEHNKE, Mark, Leo , HU, Baihua
IPC分类号： C07D209/14 , A61K31/404 , A61P43/00 , C07D403/12 , C07D401/12 , C07D491/10 , C07D417/12 , C07D405/12 , C07D409/12 , C07D491/08 , C07D417/14
CPC分类号： C07D401/12 , C07D209/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/08 , C07D491/10
摘要： This invention provides substituted indole compounds of the general formula: (I) and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.

48. 发明公开

EP1370546A2 NOVEL AMINES AS HISTAMINE-3 RECEPTOR LIGANDS AND THEIR THERAPEUTIC APPLICATIONS 审中-公开
标题翻译：胺衍生物作为组胺-3受体配体和它们的治疗应用
公开(公告)号：EP1370546A2
公开(公告)日：2003-12-17
申请号：EP02715079.6
申请日：2002-03-11
申请人： Abbott Laboratories
发明人： COWART, Marlon, D. , BENNANI, Youssef, L. , FAGHIH, Ramin , GFESSER, Gregory, A. , BLACK, Lawrence, A.
IPC分类号： C07D307/79 , C07D307/81 , C07D333/54 , C07D405/06 , C07D405/04 , C07D409/04 , C07D407/04 , C07D417/04 , A61K31/343 , A61K31/4427 , A61P9/00 , A61P11/06 , A61P25/00 , C07D413/04 , C07D409/10 , C07D521/00 , C07D491/10 , C07D491/08
CPC分类号： C07D307/79 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/81 , C07D333/54 , C07D405/04 , C07D405/06 , C07D407/04 , C07D409/04 , C07D409/10 , C07D413/04 , C07D417/04 , C07D491/08 , C07D491/10
摘要： Compounds of formula (I), or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.

49. 发明授权

EP0560055B1 Immuno-suppressing enepyranose derivatives 失效
标题翻译：免疫抑制烯吡喃糖衍生物
公开(公告)号：EP0560055B1
公开(公告)日：2002-08-28
申请号：EP93101822.0
申请日：1993-02-05
申请人： ISHIHARA SANGYO KAISHA, LTD.
发明人： Mizukoshi, Sadanori, c/o Ishihara Sangyo Kaisha , Kato, Fuminori, c/o Ishihara Sangyo Kaisha , Tsukamoto, Masamitsu, c/o Ishihara Sangyo Kaisha , Kon, Kenji, c/o Ishihara Sangyo Kaisha
IPC分类号： C07H3/08 , C07H3/10 , A61K31/70 , C07H13/04 , C07H13/06 , C07H13/08 , C07H13/10 , C07H13/12 , C07H15/04 , C07H15/207 , C07D491/08
CPC分类号： C07H13/04 , C07H3/08 , C07H3/10 , C07H7/02 , C07H11/00 , C07H13/06 , C07H13/08 , C07H13/12 , C07H15/04 , C07H15/18 , C07H15/207

50. 发明授权

EP0645391B1 Benzamide derivatives 失效
标题翻译： Benzamidderivate
公开(公告)号：EP0645391B1
公开(公告)日：2001-11-21
申请号：EP94111783.0
申请日：1994-07-28
申请人： Eisai Co., Ltd.
发明人： Miyazawa, Shuhei , Hoshino, Yorihisa , Shibata, Hisashi , Hirota, Kazuo , Kameyama, Takaaki , Abe, Shinya , Yamanaka, Takashi
IPC分类号： C07D498/08 , C07D451/14 , C07D471/08 , C07D211/58 , C07D451/04 , C07D221/24 , C07D207/14 , C07D491/08 , C07D451/02 , C07D471/18 , A61K31/46
CPC分类号： C07D451/02 , C07D207/14 , C07D211/58 , C07D221/24 , C07D451/04 , C07D451/14 , C07D471/08 , C07D491/08 , C07D498/08

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