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31. 发明公开

EP1353898A2 COMPOUNDS TO TREAT ALZHEIMER'S DISEASE 审中-公开
标题翻译：化合物疾病ALZHEIMERISCHEN的治疗
公开(公告)号：EP1353898A2
公开(公告)日：2003-10-22
申请号：EP01952378.6
申请日：2001-06-29
申请人： Elan Pharmaceuticals, Inc. , Pharmacia & Upjohn Company
发明人： MAILLARD, Michel , HOM, Roy , GAILUNAS, Andrea , JAGODZINSKA, Barbara , FANG, Lawrence, Y. , JOHN, Varghese , FRESKOS, John, N. , PULLEY, Shon, R. , BECK, James, P. , TENBRINK, Ruth, E.
IPC分类号： C07C233/78 , C07D307/52 , C07D307/14 , C07D213/38 , C07D295/12 , C07D333/20 , C07C317/44 , C07D213/82 , C07C233/40 , A61K31/165 , A61K31/33 , A61P25/28
CPC分类号： C07D295/26 , C07C215/28 , C07C233/78 , C07C235/84 , C07C239/20 , C07C243/22 , C07C243/28 , C07C271/16 , C07C271/18 , C07C275/24 , C07C311/03 , C07C311/08 , C07C311/13 , C07C311/16 , C07C311/37 , C07C317/44 , C07C323/60 , C07D211/60 , C07D215/12 , C07D277/04 , C07D295/13 , C07D303/36 , C07D307/52 , C07D307/54 , C07D333/24 , Y02P20/55 , Y02P20/582
摘要： The present invention is substituted amines of formula (X) useful in treating Alzheimer's disease and other similar diseases.

32. 发明公开

EP1241160A1 Tetracycline derivatives and their use as antibiotic agents 审中-公开
标题翻译： Tetracyclinderivate und ihre Verwendung als Antibiotica
公开(公告)号：EP1241160A1
公开(公告)日：2002-09-18
申请号：EP01500065.6
申请日：2001-03-13
申请人： GLAXO GROUP LIMITED
发明人： The designation of the inventor has not yet been filed
IPC分类号： C07C237/20 , C07D295/185 , C07D307/14 , A61K31/65
CPC分类号： C07D295/185 , C07C237/26 , C07C2603/46 , C07D307/14
摘要： A compound of formula (I) and their use for the treatment of Gram-positive, Gram-negative and community acquired infections
wherein:

R represents hydrogen, halogen, C 1-6 alkyl or NRaRb;
R 1 represents hydrogen, C 1-6 alkyl or together R 1 and R 3 represent a CH 2 moiety;
R 2 represents hydrogen, -OC 1-6 alkyl, -O(O)C 1-6 alkyl or hydroxy;
R 3 represents hydrogen, hydroxy or together R 3 and R 1 represent a CH 2 moiety;
R 4 represents hydrogen or C 1-6 alkyl;
R 5 represents hydrogen, C 1-6 alkyl or C 1-6 alkoxycarbonyl;
X represents NRxRY or -OC 1-6 alkyl optionally substituted by one or more groups selected from hydroxy, methoxy, halogen, amino and trifluoromethyl;
Rx and Ry independently represent hydrogen, benzyl, C 3-6 cycloalkyl,C 3-6 alkenyl, C 3-6 alkynyl, C 1-6 alkyl optionally substituted by one or more groups selected from hydroxy, methoxy, halogen, NRaRb and trifluoromethyl, -C 1-6 alkylcycloalkyl, -C 1-6 alkylheterocycle, -C 1-6 alkylamino and -C 1-6 alkylthio or together Rx and Ry form a heterocycle;
and pharmaceutically acceptable derivatives and solvates thereof.
摘要翻译：式（I）化合物及其用于治疗革兰氏阳性，革兰氏阴性和社区获得性感染的用途，其中：R表示氢，卤素，C 1-6烷基或NR a R b; R 1表示氢，C 1-6烷基或一起R 1和R 3表示CH 2部分; R 2表示氢，-OC 1-6烷基，-O（O）C 1-6烷基或羟基; R 3表示氢，羟基或一起R 3和R 1表示CH 2部分; R 4表示氢或C 1-6烷基; R 5表示氢，C 1-6烷基或C 1-6烷氧基羰基; X代表NRxRY或任选被一个或多个选自羟基，甲氧基，卤素，氨基和三氟甲基的基团取代的-OC 1-6烷基; Rx和Ry独立地表示氢，苄基，C3-6环烷基，C3-6烯基，C3-6炔基，任选被一个或多个选自羟基，甲氧基，卤素，NR a R b和三氟甲基的基团取代的C 1-6烷基，-C 1-6烷基环烷基，-C 1 -6-烷基杂环，-C 1-6烷基氨基和-C 1-6烷硫基，或一起Rx和Ry形成杂环; 及其药学上可接受的衍生物和溶剂合物。

33. 发明公开

EP1123270A1 PREPARATION OF AMINES 有权
标题翻译：生产胺
公开(公告)号：EP1123270A1
公开(公告)日：2001-08-16
申请号：EP99958664.7
申请日：1999-10-22
申请人： EASTMAN CHEMICAL COMPANY
发明人： CLUBB, Clyde, Neal
IPC分类号： C07C209/26 , C07D307/14 , C07C213/02 , C07C211/17
CPC分类号： C07D307/12
摘要： Disclosed is a process for the preparation of an amine by contacting in a reaction zone a water-soluble aldehyde, water, ammonia and hydrogen in the presence of a supported ruthenium catalyst at elevated temperature and pressure. The process is particularly useful for the preparation of 3-(aminomethyl)tetrahydrofuran by contacting an aqueous solution of 3-formyltetrahydrofuran with ammonia and hydrogen at elevated temperature and pressure in the presence of a supported ruthenium catalyst. The use of a supported ruthenium catalyst has been found to avoid the problem of catalyst leaching encountered when a nickel catalyst is used.

34. 发明公开

EP1066251A1 VERFAHREN ZUR HERSTELLUNG VON 1,3-DISUBSTITUIERTEN 2-NITROGUANIDINEN 有权
标题翻译：用于生产1,3-二取代-2-硝基胍
公开(公告)号：EP1066251A1
公开(公告)日：2001-01-10
申请号：EP99913140.2
申请日：1999-02-04
申请人： Bayer Aktiengesellschaft
发明人： VAN LAAK, Kai , WOLLWEBER, Detlef
IPC分类号： C07C277/08 , C07C279/36 , C07D213/61 , C07D277/32 , C07D307/14
CPC分类号： C07D277/32 , C07D213/61 , C07D307/14
摘要： The invention relates to a method for the production of compounds of formula (I) by reacting compounds of formula (II), wherein Het, R?1, R2 and R4¿ have the meaning cited in the description, with a compound of formula (III) R5-NH2, wherein R5 has the meaning cited in the description.

35. 发明授权

EP0749418B1 L-N6 -(1-IMINOETHYL)LYSINE DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 失效
标题翻译： L-N6-（1-亚氨基乙基）赖氨酸 - 衍生物及其AS NO合酶 - 抑制剂
公开(公告)号：EP0749418B1
公开(公告)日：2000-08-30
申请号：EP95913969.2
申请日：1995-03-08
申请人： G.D. SEARLE & CO.
发明人： HALLINAN, E., Ann , TJOENG, Foe, S. , FOK, Kam, F. , HAGEN, Timothy, J. , TOTH, Mihaly, V. , TSYMBALOV, Sofya , PITZELE, Barnett, S.
IPC分类号： C07C257/14 , C07C279/18 , A61K31/155 , A61K31/195 , C07D333/22 , C07D307/14 , C07C317/28 , C07C323/41 , C07D333/20 , C07D233/54 , C07D317/28
CPC分类号： C07D233/64 , A61K31/155 , C07C257/14 , C07C259/06 , C07C279/18 , C07C317/40 , C07C323/41 , C07D257/04 , C07D263/32 , C07D307/14 , C07D317/28 , C07D317/38 , C07D319/12 , C07D333/20 , C07D333/22 , Y10S514/825 , Y10S514/866 , Y10S514/921
摘要： There is disclosed a novel amino glycol derivatives of L-N6-(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.

36. 发明公开

EP1008592A3 Cyclic amide derivatives which inhibit cathepsin K 有权
标题翻译：抑制组织蛋白酶K的环状酰胺衍生物
公开(公告)号：EP1008592A3
公开(公告)日：2000-08-02
申请号：EP99402811.6
申请日：1999-11-12
申请人： Fujirebio Kabushiki Kaisha
发明人： Hosoda, Akihiko , Kobayashi, Nobuo , Tanabe, Naoko , Koji, Tsuneo , Shibata, Masahiro , Sekine, Akihiro , Dozen, Masaharu
IPC分类号： C07D295/20 , A61K31/535 , C07C271/24 , A61K31/325 , C07D317/68 , A61K31/36 , A61K31/495 , C07D307/14 , C07D307/20 , C07D213/75 , A61P19/00
CPC分类号： C07D213/71 , C07C271/24 , C07C275/26 , C07C311/20 , C07C311/29 , C07C311/43 , C07C311/46 , C07C317/44 , C07C323/60 , C07C2601/14 , C07D211/46 , C07D211/58 , C07D213/75 , C07D223/10 , C07D223/12 , C07D231/40 , C07D243/08 , C07D277/48 , C07D277/68 , C07D277/82 , C07D295/215 , C07D307/14 , C07D307/33 , C07D307/52 , C07D309/20 , C07D317/28 , C07D317/46 , C07D317/58 , C07D317/66 , C07D317/68 , C07D317/72 , C07D319/06
摘要： A cyclic amide derivative of formula (I) : wherein R 1 represents a substituted alkyl group, a substituted alkenyl group, a substituted amino group, a substituted alkoxyl group, a substituted alkylthio group, a substituted carbamoyl group, a substituted sulfonamide group or a substituted amide group; the ring A represents a saturated cyclic alkyl group with 5 to 7 carbon atoms or a hetero-atom-containing saturated heterocyclic group with 3 to 6 carbon atoms; R 2 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group; R 3 represents a hydrogen atom, a group represented by the general formula R 4 O- or a group represented by the general formula R 5 (R 6 )N-wherein R 4 represents hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group; R 5 and R 6 may be the same or different and each represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group. The cyclic amide derivative of formula (I) have a strong and selective inhibitory action of a cathepsin K and a clinical efficacy when administered orally.
摘要翻译：式（I）的环酰胺衍生物：其中R1代表取代的烷基，取代的链烯基，取代的氨基，取代的烷氧基，取代的烷硫基，取代的氨基甲酰基，取代的磺酰胺基或取代的酰胺基团; 环A表示具有5至7个碳原子的饱和环状烷基或具有3至6个碳原子的含杂原子饱和杂环基; R2表示氢原子，取代或未取代的烷基，取代或未取代的芳烃基或取代或未取代的杂环基; R 3表示氢原子，通式R 4 O-表示的基团或通式R 5（R 6）N-表示的基团，其中R 4表示氢原子，取代或未取代的烷基，取代或未取代的芳族烃基或取代或未取代的杂环基; R5和R6可以相同或不同，且各自表示氢原子，取代或未取代的烷基，取代或未取代的芳族烃基或取代或未取代的杂环基。式（I）的环酰胺衍生物在口服给药时具有组织蛋白酶K的强选择性抑制作用和临床效力。

37. 发明公开

EP0675118A3 Biphenylderivatives, process for their preparation and their use as medicaments 失效
标题翻译： Biphenylderivate，Verfahren zu ihrer Herstellung und ihre Anwendung als Arzneimittel。
公开(公告)号：EP0675118A3
公开(公告)日：1997-09-03
申请号：EP95104208.4
申请日：1995-03-22
申请人： Eisai Co., Ltd.
发明人： Akasaka, Kozo , Yonaga, Masahiro , Kajiwara, Akiharu , Higurashi, Kunizo , Ueno, Kohshi , Nagato, Satoshi , Komatsu, Makoto , Kitazawa, Noritaka , Ueno, Masataka , Yamanishi, Yoshiharu , Machida, Yoshimasa , Komatsu, Yuki , Shimomura, Naoyuki , Minami, Norio , Shimizu, Toshikazu , Nagaoka, Atsushi
IPC分类号： C07D295/205 , C07D295/155 , C07D295/135 , C07D295/073 , C07D295/088 , C07D295/096 , C07D307/52 , C07D307/14 , C07D213/36 , C07D295/26 , A61K31/495
CPC分类号： C07D213/30 , C07C2601/02 , C07D213/26 , C07D213/38 , C07D213/50 , C07D213/70 , C07D295/02 , C07D295/073 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D295/205 , C07D295/26 , C07D307/14 , C07D307/52 , C07D319/06 , C07D339/08 , C07F7/1856
摘要： A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof:
wherein R 1 represents a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a lower alkyl group, a halogenated lower alkyl group, a lower alkoxy group, a halogenated lower alkoxy group, a lower alkoxyalkyl group, a lower alkoxyalkoxy group, an aryl group, an aralkyl group, a heteroaryl group, a heteroarylalkyl group, a halogenated heteroarylalkyl group, a cyano lower alkyl group, a hydroxy lower alkyl group, an amino lower alkyl group, a lower alkoxycarbonyl group, an aryloxycarbonyl group, a cyano group, a formyl group, a lower acyl group, an aralkylcarbonyl group, a cycloether group, an alkenyl group, an alkynyl group, a lower alkylsulfinyl group, a lower alkylsulfonyl group, a lower alkylaminosulfonyl group, an arylaminosulfonyl group, a lower alkylsulfonylamino group, a halogenated lower alkylsulfonylamino group or an arylsulfonylamino group; R 2 and R 3 may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a halogenated lower alkyl group, a lower alkoxy group, a halogenated lower alkoxy group or a cyano group; R 4 represents a hydrogen atom or a halogen atom; R 5 represents a hydrogen atom, a lower alkyl group, a halogenated lower alkyl group, a hydroxy lower alkyl group, a lower alkoxycarbonyl group or an aryloxycarbonyl group; and n is 0 or an integer of 1 to 3, which exhibits dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis.
摘要翻译：由下式（I）表示的联苯衍生物或其药理学上可接受的盐：其中R 1表示氢原子，卤素原子，羟基，氨基，低级烷基，卤代低级烷基，低级烷氧基，卤代低级烷氧基，低级烷氧基烷基，低级烷氧基烷氧基，芳基，芳烷基，杂芳基，杂芳基烷基，卤代杂芳基烷基，氰基低级烷基基团，羟基低级烷基，氨基低级烷基，低级烷氧基羰基，芳氧基羰基，氰基，甲酰基，低级酰基，芳烷基羰基，环醚基，链烯基，炔基低级烷基亚磺酰基，低级烷基磺酰基，低级烷基氨基磺酰基，芳基氨基磺酰基，低级烷基磺酰基氨基，卤代低级烷基磺酰基氨基或芳基磺酰基氨基; R 2和R 3可以相同或不同，各自表示氢原子，卤素原子，低级烷基，卤代低级烷基，低级烷氧基，卤代低级烷氧基或氰基; R 4表示氢原子或卤素原子; R 5表示氢原子，低级烷基，卤代低级烷基，羟基低级烷基，低级烷氧基羰基或芳氧基羰基; 并且表示多巴胺2受体拮抗作用和/或5-羟色胺2受体拮抗作用的n为0或1〜3的整数在临床上可用于治疗和改善精神障碍如脑血管障碍，老年痴呆，精神激素引起的侵袭行为，烦躁不安，del妄，幻觉，运动过度，精神分裂症，情绪障碍，抑郁，神经症，心理生理障碍和焦虑神经症。

38. 发明授权

EP0456112B1 Cyclohexenonoximether, Verfahren zu ihrer Herstellung und ihre Verwendung als Herbizide 失效
标题翻译：环己酮肟醚，其制备方法及其作为除草剂的使用过程。
公开(公告)号：EP0456112B1
公开(公告)日：1994-08-31
申请号：EP91107095.1
申请日：1991-05-02
申请人： BASF Aktiengesellschaft
发明人： Misslitz, Ulf, Dr. , Meyer, Norbert, Dr. , Kast, Juergen , Goetz, Norbert, Dr. , Harreus, Albrecht, Dr. , Wuerzer, Bruno, Dr. , Walter, Helmut, Dr. , Westphalen, Karl-Otto, Dr. , Gerber, Matthias, Dr.
IPC分类号： C07C215/50 , C07C251/54 , C07C323/29 , C07C323/47 , C07D307/42 , C07D307/14 , C07D309/20 , C07D333/16 , C07D317/28 , C07D409/12 , C07D407/12
CPC分类号： A01N43/14 , A01N35/10 , C07C239/20 , C07C2601/16 , C07D309/06 , C07D335/02

39. 发明授权

EP0355544B1 Substituierte Decalinamine, Verfahren zu deren Herstellung, sowie deren Verwendung in Schädlingsbekämpfungsmitteln 失效
标题翻译：替补Decalinamine，其制备方法，及其在农药的使用。
公开(公告)号：EP0355544B1
公开(公告)日：1994-01-26
申请号：EP89114521.1
申请日：1989-08-05
申请人： BAYER AG
发明人： Weissmueller, Joachim, Dr. , Dutzmann, Stefan, Dr.
IPC分类号： C07C211/38 , A01N33/04 , C07C217/08 , C07D307/14 , C07D317/28 , C07D295/033 , C07D265/30 , C07D295/073 , C07D211/14
CPC分类号： C07D317/28 , A01N33/04 , A01N43/08 , C07C211/38 , C07C217/08 , C07C2601/14 , C07C2602/28 , C07D295/033 , C07D295/073 , C07D307/14

40. 发明公开

EP0435840A3 Process for the preparation of 2-(2-furyl) ethanol amine 失效
标题翻译：制备2-（2-呋喃基）乙醇胺的方法
公开(公告)号：EP0435840A3
公开(公告)日：1991-11-21
申请号：EP90870146.9
申请日：1990-09-12
申请人： MONSANTO COMPANY
发明人： Smith, Lowell Richard
IPC分类号： C07D307/52 , C07D307/14
CPC分类号： C07D307/14 , C07D307/52
摘要： The invention disclosed herein relates to a process for producing heterocyclic ethanolamines, especially 2-(2-furyl)ethanolamine.
摘要翻译：本文公开的本发明涉及制备杂环乙醇胺，特别是2-（2-呋喃基）乙醇胺的方法。

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