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1.发明授权2-imino-3-alkylbenzothiazoline derivatives bearing a heterocyclic substituent on the alkyl group, their preparation and medicinal products containing them. 失效在烷基上带有杂环取代基的2-亚氨基-3-烷基苯并噻唑啉衍生物及其制备物和含有它们的药用产品。
公开(公告)号：US5260297A
公开(公告)日：1993-11-09
申请号：US815220
申请日：1991-12-31
IPC分类号： C07D277/82 , C07D417/06 , C07D417/12 , A61K31/44 , A61K31/445 , A61K31/495
CPC分类号： C07D417/06 , C07D277/82 , C07D417/12
摘要： Compounds of formula: ##STR1## in which R.sub.1 represents a substituted 1-piperazinyl, substituted 1,2,3,6-tetrahydro-1-pyridyl or substituted piperidino radical, R.sub.2 represents a polyfluoroalkoxy or a polyfluoroalkyl radical and n is equal to 2 or 3, the salts of these compounds with an acid, processes for preparing them and medicinal products containing them.
摘要翻译： 其中R1表示取代的1-哌嗪基，取代的1,2,3,6-四氢-1-吡啶基或取代的哌啶子基的式：其中R 2表示多氟烷氧基或多氟烷基，n等于2 或3，这些化合物与酸的盐，其制备方法和含有它们的药用产品。
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2.发明授权2-alkyliminobenzothiazoline derivatives, processes for preparing them and medicinal products containing them 失效2-烷基亚氨基苯并噻唑啉衍生物，其制备方法和含有它们的药用产品
公开(公告)号：US5068238A
公开(公告)日：1991-11-26
申请号：US545822
申请日：1990-06-29
IPC分类号： A61K31/425 , A61K31/428 , A61P25/08 , A61P25/26 , C07D277/82
CPC分类号： C07D277/82
摘要： Compounds of formula: ##STR1## R.sub.1 represents a polyfluoroalkoxy radical, R.sub.2 represents an alkylthioalkyl, alkylsulphinylalkyl or alkylsulphonylalkyl radical, andR.sub.3 represents an alkyl radical,as well as the salts of these compounds with an inorganic or organic acid, processes for preparing them and medicinal products containing them.
摘要翻译： 下式化合物：（I）R 1表示多氟烷氧基，R 2表示烷硫基烷基，烷基亚磺酰基烷基或烷基磺酰基烷基，R 3表示烷基，以及这些化合物与无机酸或有机酸的盐， 准备他们和含有它们的药用产品。
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3.发明申请DERIVATIVES OF 6-(6-NH-SUBSTITUTED-TRIAZOLOPYRIDAZINE-SULFANYL) BENZOTHIAZOLES AND BENZIMIDAZOLES, PREPARATION THEREOF, USE THEREOF AS DRUGS, AND USE THEREOF AS MET INHIBITORS 审中-公开6-（6-NH-取代的三唑基亚氨基 - 磺酰基）苯并噻唑和苯并咪唑的衍生物，其制备方法及其作为药物的用途，以及作为抑制剂的用途公开(公告)号：US20120040987A1
公开(公告)日：2012-02-16
申请号：US13147297
申请日：2010-02-04
IPC分类号： A61K31/5025 , C07D277/82 , A61P35/00 , A61P21/00 , A61P3/10 , A61P17/06 , A61P27/02 , A61P19/02 , A61P25/00 , A61P11/06 , A61P7/02 , A61P3/00 , A61P37/08 , A61P35/04 , C07D487/04
CPC分类号： C07D277/82 , C07D487/04
摘要： The invention relates to novel products of the formula (I) where: (II) is a single or double bond; Rb is a hydrogen or fluorine atom; Ra is a NH-Rc radical in which Rc is an optionally substituted heterocycloalkyl, aryl, heteroaryl or -alkylcycloalkyl radical; X is S, SO, or SO2; A is NH or S; W is H, alkyl, or COR with R being cycloalkyl; alkyl; alkoxy; O-phenyl; —O— (CH2)n-phenyl with n=1 to 4; or NR1R2 with R1 being H or alk and R2 is H, cycloalkyl or alkyl; or R1, R2 form a cycle together with N optionally containing O, S, N and/or NH; all of said radicals being optionally substituted; wherein said products can be in any isomer or salt form, and can be used as drugs, in particular as MET inhibitors.
摘要翻译： 本发明涉及式（I）的新产物，其中：（II）是单键或双键; Rb是氢或氟原子; R a是NH-R c基团，其中R c是任选取代的杂环烷基，芳基，杂芳基或 - 烷基环烷基; X是S，SO或SO 2; A是NH或S; W是H，烷基或COR，其中R是环烷基; 烷基; 烷氧基 O-苯基; -O-（CH 2）n - 苯基，n = 1〜4; 或NR1R2，其中R1是H或alk，R2是H，环烷基或烷基; 或R 1，R 2与任选地含有O，S，N和/或NH的N一起形成一个循环; 所有这些基团任选被取代; 其中所述产物可以是任何异构体或盐形式，并且可以用作药物，特别是作为MET抑制剂。
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4.发明申请NOVEL TRIAZOLO(4,3-A)PYRIDINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE, IN PARTICULAR AS MET INHIBITORS 审中-公开新型三唑（4,3-A）吡啶衍生物，其制备方法，作为药物，药物组合物和新药使用，特别是作为抑制剂公开(公告)号：US20110263594A1
公开(公告)日：2011-10-27
申请号：US13054663
申请日：2009-07-16
IPC分类号： A61K31/437 , C07D413/14 , A61K31/5377 , A61P9/00 , A61P7/04 , A61P3/00 , A61P37/00 , A61P11/06 , A61P7/02 , A61P25/00 , A61P9/10 , A61P17/06 , A61P29/00 , A61P3/10 , A61P21/00 , A61P35/00 , A61P35/04 , C07D471/04
CPC分类号： A61K31/428 , A61K31/437 , A61K31/496 , A61K31/5377 , C07D471/04
摘要： The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.
摘要翻译： 本发明涉及式（I）的新产物：其中：R a表示任选取代的H，Hal，芳基或杂芳基; Rb表示H，Rc，-COORc-CO-Rc或-CO-NRcRd; 其中R c代表烷基，环烷基，杂环烷基，芳基和杂芳基，全部任意取代; Rd表示H，烷基或环烷基; 这些产品是所有异构体形式和盐，作为药物，特别是作为MET抑制剂。
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5.发明申请Substituted Cyclic Urea Derivatives, Preparation Thereof And Pharmaceutical Use Thereof As Kinase Inhibitors 审中-公开取代的环状尿素衍生物，其制备方法及其药物用途作为激酶抑制剂公开(公告)号：US20080021029A1
公开(公告)日：2008-01-24
申请号：US11627515
申请日：2007-01-26
申请人： Hartmut Strobel , Sven Ruf , Dominique Lesuisse , Conception Nemecek , Youssef El-Ahmad , Jacques Mauger , Stefan Guessregen , Kurt Ritter , Jean-Luc Malleron
发明人： Hartmut Strobel , Sven Ruf , Dominique Lesuisse , Conception Nemecek , Youssef El-Ahmad , Jacques Mauger , Stefan Guessregen , Kurt Ritter , Jean-Luc Malleron
IPC分类号： A61K31/506 , A61K31/4709 , A61K31/5377 , A61P11/06 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P3/00 , A61P3/10 , A61P35/00 , A61P37/08 , A61P7/00 , C07D215/58 , C07D401/02 , C07D413/14 , C12N9/99
CPC分类号： C07D401/06 , C07D409/14
摘要： The disclosure relates to the novel compounds of formula (I): wherein R1, R2, R2′, R3, R3′, p, A, B, Y, Y1, and Y2 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and use thereof as protein kinase inhibitors.
摘要翻译： 本公开涉及新的式（I）化合物：其中R 1，R 2，R 2，R 3，R 3， p，A，B，Y，Y 1和Y 2具有本说明书中给出的含义及其盐，包含所述化合物的药物组合物及其用途为 蛋白激酶抑制剂。
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6.发明授权Pyrrole derivatives, their preparation and pharmaceutical compositions containing them 失效吡咯衍生物，其制备方法和含有它们的药物组合物公开(公告)号：US06207675B1
公开(公告)日：2001-03-27
申请号：US09319773
申请日：1999-06-11
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： The invention concerns pyrrole derivatives of general formula (I) useful for treatment and prevention of diseases in which are involved viruses of the herpes family and/or cytokines in particular TNF&agr;.
摘要翻译： 本发明涉及通式（I）的吡咯衍生物，其用于治疗和预防涉及疱疹家族病毒和/或细胞因子特别是TNFα的疾病。
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7.发明授权Benzimidazole and benzothiazole derivatives, method for preparing same, use thereof as drugs, pharmaceutical compositions and novel use especially as c-MET inhibitors 失效苯并咪唑和苯并噻唑衍生物，其制备方法，作为药物的用途，药物组合物和新型用途，特别是作为c-MET抑制剂公开(公告)号：US08110571B2
公开(公告)日：2012-02-07
申请号：US12054719
申请日：2008-03-25
申请人： Conception Nemecek , Francois Clerc
发明人： Conception Nemecek , Francois Clerc
IPC分类号： A01N43/52 , A61K31/415
CPC分类号： C07D235/30 , C07D277/82
摘要： This invention relates to benzimidazole and benzothiazole compounds of formula (I) to methods of preparing such compounds, pharmaceutical compositions comprising such compounds, and to methods of treatment comprising administering of such compounds.
摘要翻译： 本发明涉及式（I）的苯并咪唑和苯并噻唑化合物与制备这些化合物的方法，包含这些化合物的药物组合物以及包括给予这些化合物的治疗方法。
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公开(公告)号：US07943616B2
公开(公告)日：2011-05-17
申请号：US10995103
申请日：2004-11-23
申请人： Paul J. Cox , Tahir N. Majid , Justine Yeun Quai Lai , Andrew D. Morley , Shelley Amendola , Stephanie D. Deprets , Christopher Edlin , Charles J. Gardner , Dorothea Kominos , Brian L. Pedgrift , Frank Halley , Timothy A. Gillespy , Michael Edwards , Francois F. Clerc , Conception Nemecek , Olivier Houille , Dominique Damour , Herve Bouchard , Daniel N. A. Bezard , Chantal Carrez
发明人： Paul J. Cox , Tahir N. Majid , Justine Yeun Quai Lai , Andrew D. Morley , Shelley Amendola , Stephanie D. Deprets , Christopher Edlin , Charles J. Gardner , Dorothea Kominos , Brian L. Pedgrift , Frank Halley , Timothy A. Gillespy , Michael Edwards , Francois F. Clerc , Conception Nemecek , Olivier Houille , Dominique Damour , Herve Bouchard , Daniel N. A. Bezard , Chantal Carrez
IPC分类号： C07D487/04 , A61K31/5025 , A61P29/00 , A61P35/00 , A61P19/02
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04
摘要： The invention is directed to physiologically active compounds of general formula (I):— and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译： 本发明涉及通式（I）的生理活性化合物： - 含有这些化合物的组合物; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物，以及式（I）范围内的新化合物。 这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。
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9.发明申请Cyclic Urea Derivatives, Preparation Thereof And Pharmaceutical Use Thereof As Kinase Inhibitors 失效循环脲衍生物，其制备方法及其药物用途作为激酶抑制剂公开(公告)号：US20080004300A1
公开(公告)日：2008-01-03
申请号：US11627518
申请日：2007-01-26
申请人： Hartmut Strobel , Sven Ruf , Dominique Lesuisse , Conception Nemecek , Youssef El-Ahmad , Stefan Guessregen , Anne Lebrun , Kurt Ritter , Didier Benard , Augustin Hittinger , Herve Bouchard
发明人： Hartmut Strobel , Sven Ruf , Dominique Lesuisse , Conception Nemecek , Youssef El-Ahmad , Stefan Guessregen , Anne Lebrun , Kurt Ritter , Didier Benard , Augustin Hittinger , Herve Bouchard
IPC分类号： A61K31/505 , A61P43/00 , C07D239/02
CPC分类号： C07D403/04
摘要： The invention relates to compounds of formula (I): in which R1, R2, L1, X, R3, A, R4, R4′, R4″, R4″′, R5, Y and L2 are as herein defined, salts and prodrugs thereof, to their use as protein kinase inhibitors, and to methods of treating diseases comprising adminstration thereof.
摘要翻译： 本发明涉及式（I）化合物：其中R 1，R 2，L 1，X，R 3，A，R 4，R 4， R 4，R 4，R 5，Y和L 2如本文所定义，其盐和前药，用作蛋白激酶 抑制剂，以及治疗疾病的方法，包括给药。
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公开(公告)号：US20070238734A1
公开(公告)日：2007-10-11
申请号：US11608977
申请日：2006-12-11
IPC分类号： A61K31/495 , A61P35/00
CPC分类号： A61K31/495
摘要： The present invention concerns compounds of general formula (I): in which the substituents are as described herein.
摘要翻译： 本发明涉及通式（I）的化合物：其中取代基如本文所述。
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