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161. 发明授权

EP1056710B1 DITERPENE DERIVATIVES AND ANTI-INFLAMMATORY ANALGESIC AGENTS COMPRISING THE SAME 有权
标题翻译： ENTZÜNDUNGSHEMMENDESCHMERZMITTEL DIEE ENTHALTEN的DITERPENDERIVATE
公开(公告)号：EP1056710B1
公开(公告)日：2003-12-10
申请号：EP99901968.0
申请日：1999-01-25
申请人： Sae Han Pharm. Co., Ltd. , Suh, Young Ger
发明人： SUH, Young Ger , CHOI, Young Hoon , LEE, Hye Kyung , KIM, Young Ho , PARK, Hyoung Sup
IPC分类号： C07C63/44 , C07C57/40 , C07C233/00 , C07C311/00 , A61K31/19 , A61K31/16
CPC分类号： C07C69/14 , C07C57/40 , C07C57/42 , C07C62/06 , C07C62/32 , C07C62/34 , C07C69/608 , C07C233/58 , C07C243/36 , C07C259/08 , C07C311/51 , C07C2603/26 , C07D261/04

162. 发明公开

EP1318156A1 Novel asymmetric phosphine ligand 有权
标题翻译：新不对称磷膦配体
公开(公告)号：EP1318156A1
公开(公告)日：2003-06-11
申请号：EP02293055.6
申请日：2002-12-10
申请人： Takasago International Corporation
发明人： Matsumura, Kazuhiko, c/o Takasaga Int. Corp , Saito, Takao, c/o Takasaga Int. Corp
IPC分类号： C07F9/6568 , C07F9/50 , C07F15/04 , C07F15/00 , B01J31/24 , C07B53/00
CPC分类号： C07F15/04 , B01J31/2295 , B01J31/2433 , B01J31/2476 , B01J2231/645 , B01J2531/821 , B01J2531/822 , B01J2531/824 , B01J2531/827 , B01J2531/847 , C07B53/00 , C07B2200/07 , C07C231/18 , C07F9/5027 , C07F9/65683 , C07C233/58
摘要： A novel phosphine compound having excellent properties (chemical selectivity, enantioselectivity, catalytic activity) as a catalyst for asymmetric syntheses, especially asymmetric hydrogenation. A phosphine-phospholane compound represented by the following general formula:
wherein R 1 represents hydrogen atom, a linear or branched alkyl group having 1 to 4 carbon atoms; R 2 represents hydrogen atom, or OR 21 , R 21 represents an alkyl group having 1 to 4 carbon atoms, a represents an integer of 1 to 2, b represents an integer of 1 to 3, sum of a and b represents an integer of 2 to 3, provided that at least one of R 1 and R 2 is not hydrogen atoms; R 3 , R 4 , R 5 and R 6 are the same or different, and each represents hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or an alkoxy group having 1 to 6 carbon atoms, and R 3 and R 4 , R 4 and R 5 , and/or R 5 and R 6 may be combined to form a ring which may contain at least one oxygen atoms; and R 7 and R 8 are the same or different, and each represents a linear or branched alkyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms, a perfluoroalkyl group, a phenyl group, a phenyl group having at least one substituents each selected from the group consisting of an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms which is substituted by one or more halogen atoms, an alkoxy group having 1 to 6 carbon atoms, and a halogen atom, an aralkyl group having 7 to 12 carbon atoms, or a ring-substituted aralkyl group.)
摘要翻译：具有优异特性（化学选择性，对映体选择性，催化活性）作为不对称合成催化剂，特别是不对称氢化的新型膦化合物。由以下通式表示的膦 - 磷脂化合物：其中R 1表示氢原子，具有1至4个碳原子的直链或支链烷基的 R 2表示氢原子，或OR 21，R 21表示碳原子数1〜4的烷基，a表示1〜2的整数，b表示1〜3的整数，并且b表示2〜3的整数，条件是R 1和R 2中的至少一个不是氢原子; R 3，R 4，R 5和R 6相同或不同，分别表示氢原子，碳原子数1〜6的烷基或碳原子数1〜6的烷氧基原子，R 3和R 4，R 4和R 5和/或R 5和R 6可以组合形成可以含有至少一个氧原子的环 ; R 7和R 8相同或不同，表示碳原子数1〜6的直链或支链烷基，碳原子数3〜7的环烷基，全氟烷基，苯基，具有至少一个选自碳原子数1〜6的烷基，碳原子数1〜6的烷基，被一个以上卤素原子取代的烷基的苯基，具有1〜 6个碳原子，卤素原子，碳原子数为7〜12的芳烷基或环取代的芳烷基）

163. 发明公开

EP1146037A4 PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE AMINO ALCOHOLS 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VON OPTISCH AKTIVEN AMINO-ALKOHOLEN
公开(公告)号：EP1146037A4
公开(公告)日：2002-07-17
申请号：EP00900418
申请日：2000-01-18
申请人： NIPPON SODA CO
发明人： KATAYAMA EIJI , SATO DAISUKE , OOKA HIROHITO , INOUE TSUTOMU
IPC分类号： C07C231/18 , C07C233/58 , C07C269/06 , C07C271/08 , C07C271/12 , C07C303/40 , C07C311/51 , C07D209/48 , C07D231/12 , C07D233/64 , C07D277/24
CPC分类号： C07D209/48 , C07B2200/07 , C07C231/18 , C07C269/06 , C07C303/40 , C07C311/51 , C07C233/58 , C07C271/08 , C07C271/12
摘要： 3 process for the preparation of optically active β-amino alcohols represented by the general formula (2): Ra-C*H(OH)-C*H(Rb)-Rc, [wherein Ra and Rc are each independently hydrogen, optionally substituted alkyl, or the like; Rb is one member selected from among groups represented by the following general formulae: (3) R1CO(R2)N-, (4) R1CO(R1'CO)N-, (5) R1CO(R1'SO2)N-, (6) R1SO2(R2)N- (wherein R1, R1' and R2 are each independently hydrogen, optionally substituted alkyl, or the like, or alternatively R1 and R2 or R1 and R1' may be united to form a five- to eight-membered nitrogenous heterocycle); and C* is an asymmetric carbon atom], characterized by reacting a racemic α-aminocarbonyl compound represented by the general formula (1): Ra-CO-CH(Rb)-Rc (wherein Ra, Rb and Rc are each as defined above) with hydrogen or a hydrogen donor in the presence of an optically active transition metal compound and a base.
摘要翻译： 3制备由通式（2）表示的光学活性β-氨基醇的方法：Ra-C * H（OH）-C * H（Rb）-Rc，其中Ra和Rc各自独立地为氢，任选取代烷基等; （3）R1CO（R2）N-，（4）R1CO（R1'CO）N - ，（5）R1CO（R1'SO2）N-，R3是选自下列通式表示的基团之一：（6）R 1 SO 2（R 2）N-（其中R 1，R 1和R 2各自独立地为氢，任选取代的烷基等，或者R 1和R 2或R 1和R 1'可以团合以使5-8 含氮杂环）; 和C *是不对称碳原子，其特征在于使由通式（1）表示的外消旋的α-氨基羰基化合物：Ra-CO-CH（Rb）-Rc（其中Ra，Rb和Rc各自如上定义）与氢或氢供体在光学活性的过渡金属化合物和碱的存在下反应。

164. 发明公开

EP1090908A3 Cyclobutane derivatives as inhibitors of protein farnesyltransferase 失效
标题翻译：环丁烷衍生物抑制蛋白 - 法呢基转移酶
公开(公告)号：EP1090908A3
公开(公告)日：2001-05-16
申请号：EP00124275.9
申请日：1996-04-18
申请人： ABBOTT LABORATORIES
发明人： Arendsen, David L. , Baker, William R. , Fakhoury, Stephen A. , Fung, K.L. Anthony , Garvey, David S. , McClellan, William J. , O'Connor, Stephen J. , Prasad, Rajnandan N. , Rockway, Todd W. , Rosenberg, Saul H. , Stein, Herman H. , Shen, Wang , Stout, David M. , Sullivan, Gerard M. , Augeri, David J.
IPC分类号： C07C233/60 , C07D333/20 , C07C233/58 , C07C233/59 , C07C235/40 , A61K31/19 , A61K31/215 , A61K31/38 , A61K31/16
CPC分类号： C07C235/82 , C07C233/58 , C07C233/59 , C07C233/60 , C07C235/40 , C07C2601/04 , C07D333/20
摘要： The present invention provides a compound of formula (II) or a pharmaceutically acceptable salt thereof, which is useful for inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.
摘要翻译：本发明提供式（II）化合物或其药学上可接受的盐，其可用于抑制蛋白质法呢基转移酶和癌基因蛋白Ras的法呢基化，制备本发明化合物的方法除了可用于这些方法，药物组合物，以及使用这些化合物的方法。

165. 发明公开

EP1053242A1 DICARBAMOYLFUNKTIONALISIERTE METALLKOMPLEXE 审中-公开
公开(公告)号：EP1053242A1
公开(公告)日：2000-11-22
申请号：EP99906215.1
申请日：1999-02-02
申请人： TARGOR GmbH
发明人： FRITZE, Cornelia , ERKER, Gerhard , DUDA, Lothar
IPC分类号： C07F7/00 , C07C237/24 , C08F10/00 , C07F17/00
CPC分类号： C07F17/00 , C07C233/58 , C07C2601/10 , C07C2601/14 , C07C2603/74 , C07F7/006 , C08F10/00 , C08F4/64
摘要： The invention relates to novel dicarbamoyl-substituted metal complexes and to their use in the polymerisation of olefins.
摘要翻译：本发明涉及新的二氨基甲酰基取代的金属配合物及其在烯烃聚合中的用途。

166. 发明授权

EP0721938B1 Nouveaux composés (hétéro)cycliques alkylés, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent 失效
标题翻译：烷基（杂）环衍生物，它们的制备方法和含有它们的药物组合物
公开(公告)号：EP0721938B1
公开(公告)日：1999-12-08
申请号：EP96400051.7
申请日：1996-01-10
申请人： ADIR ET COMPAGNIE
发明人： Lesieur, Daniel , Fourmaintraux, Eric , Depreux, Patrick , Delagrange, Philippe , Renard, Pierre , Guardiola-Lemaître, Béatrice
IPC分类号： C07C233/02 , C07C233/58 , C07C327/40 , C07C275/24 , C07C335/12 , C07D333/58 , C07D209/16 , A61K31/38 , A61K31/17 , A61K31/40
CPC分类号： C07C233/08 , C07C233/05 , C07C233/58 , C07C2601/02 , C07C2601/04 , C07C2602/10 , C07D307/81 , C07D333/58

167. 发明授权

EP0783480B1 PROCESSES FOR THE PREPARATION OF CYCLOPROPANECARBOXYLIC ACID AND DERIVATIVES THEREOF 无效
标题翻译：维多利亚州自然保护联合国环境规划署
公开(公告)号：EP0783480B1
公开(公告)日：1999-12-01
申请号：EP95932531.7
申请日：1995-09-18
申请人： EASTMAN CHEMICAL COMPANY
发明人： LIANG, Shaowo , PRICE, Timothy, Warren
IPC分类号： C07C61/04 , C07C51/235
CPC分类号： C07C231/02 , C07C51/235 , C07C2601/02 , C07C61/04 , C07C233/58
摘要： Disclosed is a process for the preparation of cyclopropanecarboxylic acid by the non-catalytic, oxidation of cyclopropanecarboxaldehyde using molecular oxygen as the oxidant. Also disclosed are processes for the preparation of amides, esters and acid chlorides from cyclopropanecarboxylic acid.
摘要翻译：本发明提供了制备环丙烷甲酰胺的方法，其包括以下步骤：（1）在200-260℃的温度和10至100巴绝对压力下，在反应器中将环丙烷羧酸与氨接触，不存在两者都是催化剂和溶剂，形成环丙烷甲酰胺的熔体; （2）在高于环丙烷甲酰胺熔点的温度下排空反应器，以降低压力至大气压，并从环丙烷甲酰胺中除去过量的氨和反应水; 和（3）从反应器中获得基本上不含水和氨的环丙烷甲酰胺。

168. 发明公开

EP0897747A1 NITRATION OR CARBOXYLATION CATALYSTS 失效
标题翻译： NITRIERUNGS- ODER CARBOXYLIERUNGSKATALYSATOREN
公开(公告)号：EP0897747A1
公开(公告)日：1999-02-24
申请号：EP98900216.7
申请日：1998-01-13
申请人： Daicel Chemical Industries, Ltd. , Ishii, Yasutaka
发明人： ISHII, Yasutaka , NAKANO, Tatsuya , SAKAGUCHI, Satoshi
IPC分类号： B01J31/02 , B01J31/26 , C07C201/08 , C07C51/10 , C07C61/28 , C07C211/35 , C07C265/10 , C07C205/55 , C07C62/06 , C07C271/24 , C07B43/02 , C07B41/08
CPC分类号： C07C45/36 , B01J31/006 , B01J31/0247 , B01J31/2208 , B01J2231/70 , B01J2531/16 , B01J2531/72 , B01J2531/842 , B01J2531/845 , C07B41/08 , C07B43/02 , C07C51/10 , C07C67/12 , C07C69/757 , C07C205/04 , C07C205/05 , C07C205/06 , C07C205/18 , C07C205/55 , C07C211/35 , C07C211/37 , C07C215/42 , C07C229/50 , C07C233/10 , C07C233/14 , C07C233/23 , C07C233/41 , C07C233/52 , C07C233/58 , C07C233/62 , C07C235/40 , C07C235/82 , C07C237/24 , C07C265/10 , C07C271/24 , C07C2603/74 , C07C49/78 , C07C61/29 , C07C61/135
摘要： In the presence of an imide compound (e.g., N-hydroxyphthalimide) shown by the following formula (1):
wherein R 1 and R 2 represent a hydrogen atom, a halogen atom, an alkyl group, an aryl group and a cycloalkyl group, and R 1 and R 2 may bond together to form a double bond, or an aromatic or non-aromatic ring, and Y is an O or OH, and n denotes 1 to 3;
a substrate is allowed to contact with at least one reactant selected from (i) a nitrogen oxide and (ii) a mixture of carbon monoxide and oxygen to be introduced with at least one functional group selected from a nitro group and a carboxyl group. The nitrogen oxide includes, for example, a compound represented by the formula N x O y (e.g., N 2 O 3 , NO 2 ). The substrate includes, for example, a compound having a methine carbon atom (e.g., adamantane), a compound having a methyl group or a methylene group at an adjacent moiety of an aromatic ring. According to such reaction, the substrate can be efficiently nitrated or carboxylated even in a mild or moderate condition.
摘要翻译：在下式（1）所示的酰亚胺化合物（例如N-羟基邻苯二甲酰亚胺）存在下，其中R 1和R 2表示氢原子，卤素原子，烷基，芳基和环烷基，R 1和R 2可以键合在一起形成双键，或芳族或非芳香环，Y是O或OH，n表示1至3; 允许底物与选自（i）氮氧化物和（ii）一氧化碳和氧气的混合物中的至少一种反应物接触，以将至少一种选自硝基和羧基的官能团引入。氮氧化物包括例如由式N x O y表示的化合物（例如，N 2 O 3，NO 2）。底物包括例如具有次甲基碳原子的化合物（例如金刚烷），在芳环的相邻部分具有甲基或亚甲基的化合物。根据这种反应，即使在温和或中等条件下，底物也能被有效地硝化或羧化。

169. 发明授权

EP0668855B1 SUBSTITUTED CYCLOPENTANE COMPOUNDS FOR USE AS CHELATING AGENTS 失效
标题翻译：替代品CYCLOPENTAN-VERBINDUNGEN ZUR VERWENDUNG ALS CHELATBILDER
公开(公告)号：EP0668855B1
公开(公告)日：1998-06-24
申请号：EP93924758.1
申请日：1993-11-12
申请人： AMERSHAM INTERNATIONAL plc
发明人： ORCHARD, Pamela Joan , COOPER, Stephen, Randolph
IPC分类号： C07C233/58 , C07C31/27 , C07C309/66 , C07C323/52 , C07C69/708 , C07C43/162 , C07C255/13 , C07C323/62 , C07C259/06
CPC分类号： C07C255/13 , C07C31/274 , C07C43/162 , C07C69/708 , C07C233/58 , C07C259/06 , C07C323/52 , C07C323/62 , C07C2601/08
摘要： The invention provides as new compounds cis-cis-cis-tetrasubstituted cyclopentane compounds which are expected to be useful as chelating agents for alkaline earths, transition, lanthanide and actinide metal ions. The compounds have formula (I). Each of the groups X , X , X and X comprises at least one potential ligand donor group, or one of the groups X or Z may comprise a group which may permit attachment to a biologically active molecule or insoluble support.
摘要翻译： PCT No.PCT / GB93 / 02335 Sec。 371日期：1995年5月12日 102（e）日期1995年5月12日PCT提交1993年11月12日PCT公布。公开号WO94 / 11339 日期1994年5月26日本发明提供了预期可用作碱土金属，过渡金属，镧系元素和锕系金属离子螯合剂的新化合物顺式 - 顺式 - 四取代环戊烷化合物。该化合物具有式（I）。基团X1，X2，X3和X4中的每一个包含至少一个潜在的配体供体基团，或者X或Z基团之一可以包含可以附着于生物活性分子或不溶性载体的基团。公式（I）

170. 发明公开

EP0783480A1 PROCESSES FOR THE PREPARATION OF CYCLOPROPANECARBOXYLIC ACID AND DERIVATIVES THEREOF 无效
标题翻译：用于生产环丙烷及其衍生物
公开(公告)号：EP0783480A1
公开(公告)日：1997-07-16
申请号：EP95932531.0
申请日：1995-09-18
申请人： EASTMAN CHEMICAL COMPANY
发明人： LIANG, Shaowo , PRICE, Timothy, Warren
IPC分类号： C07B61 , C07C51 , C07C61 , C07C67 , C07C69 , C07C231 , C07C233
CPC分类号： C07C231/02 , C07C51/235 , C07C2601/02 , C07C61/04 , C07C233/58
摘要： Disclosed is a process for the preparation of cyclopropanecarboxylic acid by the non-catalytic, oxidation of cyclopropanecarboxaldehyde using molecular oxygen as the oxidant. Also disclosed are processes for the preparation of amides, esters and acid chlorides from cyclopropanecarboxylic acid.

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