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121. 发明公开

EP1071668A1 5-AMINOINDENO(1,2-C)PYRAZOL-4-ONES AS ANTI-CANCER AND ANTI-PROLIFERATIVE AGENTS 有权
标题翻译： 5- AMINOINDENO [1,2-c]吡唑-4-酮作为抗肿瘤和生长抑制剂
公开(公告)号：EP1071668A1
公开(公告)日：2001-01-31
申请号：EP99918695.0
申请日：1999-04-20
申请人： Du Pont Pharmaceuticals Company
发明人： NUGIEL, David, A. , CARINI, David, J. , YUE, Eddy, W. , DIMEO, Susan, V.
IPC分类号： C07D231/54 , A61K31/41 , C07D409/12 , C07D403/12 , C07D401/12 , C07D417/12 , C07D413/12 , C07D413/14
CPC分类号： C07D405/12 , C07D231/54 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/14 , C07D405/04 , C07D409/04 , C07D409/12 , C07D409/14
摘要： The present invention relates to the synthesis of a new class of indeno [1,2-c]pyrazol-4-ones of formula (I), that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits known as cyclines A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

122. 发明公开

EP0959080A1 Initiatoren für die radikalische Polymerisation 审中-公开
标题翻译： Initiatorenfürdie radikalische Polymerisation
公开(公告)号：EP0959080A1
公开(公告)日：1999-11-24
申请号：EP99107085.5
申请日：1999-04-12
申请人： BASF AKTIENGESELLSCHAFT
发明人： Königer, Rainer Dr. , Schwalm, Reinhold Dr. , Raether, Roman Benedikt Dr.
IPC分类号： C08F4/04 , C07D237/26 , C07D487/04 , C07D231/54 , C07D491/02 , C07D271/12 , C07F7/08 , C07C271/60
CPC分类号： C08F4/04 , C07D231/54 , C07D271/12 , C07D487/08 , C07F7/0814
摘要： Initiatoren für die radikalische Polymerisation, enthaltend als Strukturmerkmal das Diels-Alder-Addukt einer Azogruppe (-N=N-) an eine konjugierte Doppelbindung (Dien).
摘要翻译：自由基聚合引发剂，其特殊结构特征是偶氮基（-N = N-）与共轭双键（二烯）的狄尔斯 - 阿尔德加合物。

123. 发明公开

EP0923933A1 Substituted pyrazolyl benzenesulfonamides for use in the treatment of inflammation 失效
标题翻译： Substitutierte吡唑苯磺酰胺在炎症的治疗
公开(公告)号：EP0923933A1
公开(公告)日：1999-06-23
申请号：EP99101697.3
申请日：1994-11-14
申请人： G.D. SEARLE & CO.
发明人： Talley, John J , Penning, Thomas D. , Collins, Paul W. , Rogier, Donald J., Jr. , Malecha, James W. , Miyashiro, Julie M. , Bertenshaw, Stephen R. , Khanna, Ish K , Granets, Matthew J. , Rogers, Roland S. , Carter, Jeffery S. , Docter, Stephen H. , Yu, Stella S.
IPC分类号： A61K31/415
CPC分类号： C07D405/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D409/04 , C07D495/04
摘要： A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II:

wherein R 2 is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R 3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R 4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R 4 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R 2 and R 3 are not both hydrido; further provided that R 2 is not carboxyl or methyl when R 3 is hydrido and when R 4 is phenyl; further provided that R 4 is not triazolyl when R 2 is methyl;
further provided that R 4 is not aralkenyl when R 2 is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R 4 is not phenyl when R 2 is methyl and R 3 is carboxyl; and further provided that R 4 is not unsubstituted thienyl when R 2 is trifluoromethyl; or a pharmaceutically-acceptable salt thereof.

124. 发明授权

EP0683155B1 Tetrahydrobenz cd indoles with serotonin regulatory activity 失效
标题翻译： Tetrahydrobenzfluorene CD吲哚与血清素抑制活性
公开(公告)号：EP0683155B1
公开(公告)日：1998-07-01
申请号：EP95303268.7
申请日：1995-05-16
申请人： ELI LILLY AND COMPANY
发明人： Flaugh, Michael Edward
IPC分类号： C07D231/54 , A61K31/415
CPC分类号： C07D231/54

125. 发明授权

EP0713485B1 THIOCARBAMOYLVERBINDUNGEN ALS MIKROBIZIDE 失效
标题翻译：甲硫氨酸硼酸盐
公开(公告)号：EP0713485B1
公开(公告)日：1998-04-15
申请号：EP94926134.1
申请日：1994-07-29
申请人： BAYER AG
发明人： HEUER, Lutz , WACHTLER, Peter , KUGLER, Martin , SCHRAGE, Heinrich
IPC分类号： C07D231/20 , A01N43/56 , C07C69/716 , C07C69/738
CPC分类号： C07C69/716 , A01N47/38 , C07D231/20 , C07D231/54 , C07D231/56 , C07D405/04 , C07D409/04

126. 发明授权

EP0635996B1 PYRAZOLINE ZUM SCHUTZ VON KULTURPFLANZEN GEGENÜBER HERBIZIDEN 失效
标题翻译：吡唑啉用于保护作物除草剂AGAINST
公开(公告)号：EP0635996B1
公开(公告)日：1998-02-11
申请号：EP90917518.4
申请日：1990-11-26
申请人： Hoechst Schering AgrEvo GmbH
发明人： RÖSCH, Wolfgang , SOHN, Erich , BAUER, Klaus , BIERINGER, Hermann
IPC分类号： A01N25/32 , A01N43/56 , C07D231/06 , C07D231/54
CPC分类号： C07F7/1896 , A01N25/32 , C07D231/06 , C07D231/54 , C07F7/0812
摘要： Disclosed are compounds of formula (I) in which X, n, R?1, R2 and R3¿ are as defined in claim 1. Such compounds are suitable for use as antidotes against the phytotoxic side-effects of herbicides used on crops, without diminishing the effect of the herbicides against weeds.

127. 发明授权

EP0638071B1 HETEROCYCLIC CARBONIC ACID DERIVATIVES WHICH BIND TO RETINOID RECEPTORS (RAR) 失效
标题翻译：杂环羧酸羧酸衍生物RAR受体的结合MAY
公开(公告)号：EP0638071B1
公开(公告)日：1997-04-09
申请号：EP94903025.8
申请日：1993-12-20
申请人： Eisai Co., Ltd.
发明人： YOSHIMURA, Hiroyuki , NAGAI, Mitsuo , HIBI, Shigeki , KIKUCHI, Koichi , HISHINUMA, Ieharu , NAGAKAWA, Junichi , ASADA, Makoto , MIYAMOTO, Norimasa , HIDA, Takayuki , OGASAWARA, Aichi , YAMATSU, Isao
IPC分类号： C07D231/54 , A61K31/415 , C07D401/06 , A61K31/44 , C07D491/052 , C07D495/04 , C07D209/56 , C07D417/04 , C07D403/04 , C07D407/06 , C07D409/06
CPC分类号： C07D495/04 , C07D209/56 , C07D221/18 , C07D231/54 , C07D277/60 , C07D307/77 , C07D311/92 , C07D333/38 , C07D333/50 , C07D335/08 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/04 , C07D491/04
摘要： A heterocycle-containing carbonic acid derivative represented by general formula (I) or a physiologically acceptable salt thereof which exhibits an excellent preventive and therapeutic effect against various diseases linked to retinoic acid and an intermediate which is useful for the production of the heterocycle-containing carbonic acid derivative. B represents a heterocyclic group, D represents a phenyl group and A/E are as defined in the application.

128. 发明公开

EP0717736A4 POLAR-SUBSTITUTED HYDROCARBONS 失效
标题翻译：极地替代型KOHLENWASSERSTOFFE
公开(公告)号：EP0717736A4
公开(公告)日：1996-08-28
申请号：EP94926731
申请日：1994-09-12
申请人： NARHEX LTD
发明人： GROBELNY DAMIAN
IPC分类号： A61K38/00 , C07C243/18 , C07C243/28 , C07C243/32 , C07C243/34 , C07C251/80 , C07C255/13 , C07C255/24 , C07C271/20 , C07C271/22 , C07C281/02 , C07D207/14 , C07D207/40 , C07D207/416 , C07D209/48 , C07D211/28 , C07D211/58 , C07D211/72 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/75 , C07D213/80 , C07D215/14 , C07D231/04 , C07D231/54 , C07D237/04 , C07D237/30 , C07D237/32 , C07D239/04 , C07D243/10 , C07D245/02 , C07D255/02 , C07D257/04 , C07D265/06 , C07D265/30 , C07D295/13 , C07D295/26 , C07D303/36 , C07D307/12 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08 , C07D491/04 , C07D495/04 , C07D498/08 , C07D521/00 , C07F9/09 , C07F9/141 , C07F9/553 , C07F9/572 , C07F9/58 , C07F9/60 , C07F9/62 , C07F9/6506 , C07F9/6509 , C07F9/6558 , C07F9/6561 , C07F9/6574 , C07K5/06 , C07K5/078
CPC分类号： C07D237/04 , A61K38/00 , C07C243/18 , C07C243/28 , C07C243/32 , C07C243/34 , C07C251/80 , C07C255/13 , C07C255/24 , C07C271/20 , C07C271/22 , C07C281/02 , C07C2601/14 , C07C2601/16 , C07C2602/10 , C07C2603/24 , C07D207/14 , C07D207/416 , C07D209/48 , C07D211/28 , C07D211/58 , C07D211/72 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/75 , C07D213/80 , C07D215/14 , C07D231/04 , C07D231/12 , C07D231/54 , C07D233/56 , C07D237/30 , C07D237/32 , C07D239/04 , C07D243/10 , C07D245/02 , C07D249/08 , C07D255/02 , C07D257/04 , C07D265/06 , C07D265/30 , C07D295/13 , C07D295/26 , C07D303/36 , C07D307/12 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08 , C07D491/04 , C07D495/04 , C07F9/091 , C07F9/093 , C07F9/1411 , C07F9/1412 , C07F9/5532 , C07F9/5721 , C07F9/588 , C07F9/60 , C07F9/62 , C07F9/65067 , C07F9/650994 , C07F9/65583 , C07F9/65586 , C07F9/6561 , C07F9/65742 , C07F9/65744 , C07K5/06139 , C07K5/06191
摘要： The invention relates to retroviral protease inhibitors of the general formula (I): W-(A)n-B-(A*)m-V where W, A, B, A*, V, n and m are as defined herein, including related prodrugs of general formula (I) comprising a solubilising group which is labile in vivo.
摘要翻译：本发明涉及通式（I）的逆转录病毒蛋白酶抑制剂：W-（A）nB-（A *）mV其中W，A，B，A *，V，n和m如本文所定义，包括相关的前药的通式（I）包含在体内不稳定的增溶基团。

129. 发明公开

EP0700905A1 Tricyclische Pyrazol-Derivate 失效
标题翻译：三菌酸吡唑衍生物
公开(公告)号：EP0700905A1
公开(公告)日：1996-03-13
申请号：EP95112270.4
申请日：1995-08-04
申请人： F. HOFFMANN-LA ROCHE AG
发明人： Wichmann, Jürgen
IPC分类号： C07D231/54 , C07D231/56 , A61K31/415
CPC分类号： C07D231/54
摘要： Die Erfindung betrifft tricyclische Pyrazol-Derivate der allgemeinen Formel

worin

R¹ bis R⁴ je Wasserstoff, Hydroxy, Halogen, niederes Alkyl, niederes Alkoxy oder Phenyl;
R⁵ Wasserstoff oder niederes Alkyl;
R⁶ Wasserstoff, niederes Alkyl oder niederes Alkoxy;
X -(CR⁷R⁸) n - oder -CH=CH-;
R⁷ und R⁸ Wasserstoff oder niederes Alkyl und
n 1 oder 2 bedeuten,
sowie pharmazeutisch annehmbare Salze von basischen Verbindungen der allgemeinen Formel I.
Diese Verbindungen und Salze sind geeignet zur Anwendung als therapeutische Wirkstoffe, insbesondere zur Behandlung oder Verhütung von zentralnervösen Störungen, wie Depressionen, bipolaren Störungen, Angstzuständen, Schlaf- und Sexualstörungen, Psychosen, Schizophrenie, Migräne und andere mit Kopfschmerz oder Schmerz anderer Art verbundene Zustände, Persönlichkeitsstörungen oder obsessiv-compulsive Störungen, soziale Phobien oder panische Anfälle, mentale organische Störungen, mentale Störungen im Kindesalter, Aggressivität, altersbedingte Gedächtnisstörungen und Verhaltensstörungen, Sucht, Obesitas, Bulimie etc., Schädigungen des Nervensystems durch Trauma, Schlaganfall, neurodegenerative Erkrankungen etc., cardiovasculären Störungen, wie Bluthochdruck, Thrombose, Schlaganfall etc. und gastrointestinalen Störungen wie Dysfunktion der Motilität des Gastrointestinaltrakts.
摘要翻译：第9616号发行。第一大国相当于NO9503162A。 minoalkyl-substd。式（I）的三环吡唑及其盐是新的：R 1 -R 4 = H，OH，卤素，低级烷基或低级烷氧基; R 5 = H或低级烷基; R 6 = H，低级烷基或低级烷氧基; X =（CR 7 R 8）n或CH = CH; R 7，R 8 = H或低级烷基; n = 1或2。

130. 发明公开

EP0700390A1 INTERMEDIATES AND METHODS FOR THE SYNTHESIS OF ANTHRAPYRAZOLONE ANTICANCER AGENTS 失效
标题翻译：用于生产ANTHRAPYRAZOLONE抗恶性肿瘤药和中间体
公开(公告)号：EP0700390A1
公开(公告)日：1996-03-13
申请号：EP94915874.0
申请日：1994-04-29
申请人： THE DU PONT MERCK PHARMACEUTICAL COMPANY
发明人： ZHANG, Lin-Hua , AUERBACH, Joseph
IPC分类号： C07D231
CPC分类号： C07D231/54
摘要： This invention relates to compounds, including 5-chloro-2-[2-[[(4-methylphenyl)sulfonyl]oxy]ethyl]-7-[2,4,6-trimethylphenyl)methoxy]anthra[1,9-cd]pyrazol-6(2H)-one and analogs thereof, which are useful as intermediates for the synthesis of anthrapyrazolone anticancer agents, including losoxantrone. This invention also relates to methods for the synthesis of anthrapyrazolone anticancer agents, including losoxantrone.

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