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1.发明授权Cyclic urea compounds, preparation thereof and pharmaceutical use thereof as kinase inhibitors 失效环状尿素化合物，其制备及其作为激酶抑制剂的药物用途公开(公告)号：US07825115B2
公开(公告)日：2010-11-02
申请号：US11972314
申请日：2008-01-10
申请人： Marcel Patek , Anil Nair , Augustin Hittinger , Conception Nemecek , Daniel Bond , Greg Harlow , Herve Bouchard , Jacques Mauger , Jean-Luc Malleron , Mark Palermo , Fahad Al-Obeidi , Thomas Faitg , Hartmut Strobel , Sven Ruf , Kurt Ritter , Youssef El-Ahmad , Dominique Lesuisse , Didier Bénard
发明人： Marcel Patek , Anil Nair , Augustin Hittinger , Conception Nemecek , Daniel Bond , Greg Harlow , Herve Bouchard , Jacques Mauger , Jean-Luc Malleron , Mark Palermo , Fahad Al-Obeidi , Thomas Faitg , Hartmut Strobel , Sven Ruf , Kurt Ritter , Youssef El-Ahmad , Dominique Lesuisse , Didier Bénard
IPC分类号： C07D401/06 , C07D403/06 , A61K31/41
CPC分类号： C07D401/06 , C07D401/14
摘要： The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
摘要翻译： 本公开涉及式I的环脲化合物：如本文所定义，其制备方法，包含其的药物组合物及其作为蛋白激酶上的抑制剂的药物用途。 因此，式I化合物可用于预防或治疗能够通过抑制蛋白激酶如实体瘤的活性而被调节的生理障碍。
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2.发明申请NOVEL PYRROLO(2,3-b) PYRIDINE DERIVATIVES, THE PREPARATION AND THE PHARMACEUTICAL USE THEREOF IN THE FORM OF KINASE INHIBITORS 失效新型吡咯（2,3-b）吡啶衍生物，其在激酶抑制剂形式中的制备及其药物应用公开(公告)号：US20090233956A1
公开(公告)日：2009-09-17
申请号：US12410135
申请日：2009-03-24
申请人： Sylvie Wentzler , Youssef El-Ahmad , Bruno Filoche-Romme , Conception Nemecek , Corinne Venot , Augustin Hittinger
发明人： Sylvie Wentzler , Youssef El-Ahmad , Bruno Filoche-Romme , Conception Nemecek , Corinne Venot , Augustin Hittinger
IPC分类号： A61K31/437 , C07D401/14
CPC分类号： C07D471/04
摘要： Novel compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R, R1, R2, R3, R4, R5, and R6 have the meanings given in the description, pharmaceutical compositions comprising said compounds and use thereof as protein kinase inhibitors.
摘要翻译： 式（I）的新型化合物或其药学上可接受的盐，其中R，R 1，R 2，R 3，R 4，R 5和R 6具有说明书中给出的含义，包含所述化合物的药物组合物及其作为蛋白激酶抑制剂的用途。
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3.发明授权Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors 失效环状尿素衍生物，其制备方法及其作为激酶抑制剂的药物用途公开(公告)号：US07354933B2
公开(公告)日：2008-04-08
申请号：US10770382
申请日：2004-02-02
申请人： Marcel Patek , Anil Nair , Augustin Hittinger , Conception Nemecek , Daniel Bond , Greg Harlow , Herve Bouchard , Jacques Mauger , Jean-Luc Malleron , Mark Palermo , Fahad Al-Obeidi , Thomas Faitg , Hartmut Strobel , Sven Ruf , Kurt Ritter , Youssef El-Ahmad , Dominique Lesuisse , Didier Bénard
发明人： Marcel Patek , Anil Nair , Augustin Hittinger , Conception Nemecek , Daniel Bond , Greg Harlow , Herve Bouchard , Jacques Mauger , Jean-Luc Malleron , Mark Palermo , Fahad Al-Obeidi , Thomas Faitg , Hartmut Strobel , Sven Ruf , Kurt Ritter , Youssef El-Ahmad , Dominique Lesuisse , Didier Bénard
IPC分类号： C07D401/06 , C07D403/06 , A61K31/41
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
摘要翻译： 本发明涉及式I的环脲化合物：如本文所定义。 本发明还涉及其制备方法，包含其的药物组合物及其药物用途，作为蛋白激酶上的抑制剂。 因此，通过抑制蛋白激酶（例如实体瘤）的活性来预防或治疗能够调节的生理障碍是有用的。
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4.发明申请Heterocycle-Substituted Cyclic Urea Derivatives, Preparation Thereof And Pharmaceutical Use Thereof As Kinase Inhibitors 审中-公开杂环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：US20070259891A1
公开(公告)日：2007-11-08
申请号：US11627505
申请日：2007-01-26
申请人： Hartmut Strobel , Sven Ruf , Dominique Lesuisse , Conception Nemecek , Stefan Guessregen , Anne Lebrun , Kurt Ritter , Jean-Luc Malleron
发明人： Hartmut Strobel , Sven Ruf , Dominique Lesuisse , Conception Nemecek , Stefan Guessregen , Anne Lebrun , Kurt Ritter , Jean-Luc Malleron
IPC分类号： A61K31/4439 , A61K31/4709 , A61K31/506 , A61P11/06 , A61P17/00 , A61P21/00 , A61P3/00 , A61P35/00 , A61P37/08 , A61P9/00 , C07D215/00 , C07D401/02 , C07D401/14
CPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The disclosure relates to compounds of formula (I): wherein Y, Y1, Yo, R1, R2, R2′, p, R3, R3′, A, B 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： 本公开涉及式（I）的化合物：其中Y，Y 1，Y 1，R 1，R 2，R 2，p ，R 3，R 3'，A，B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作为蛋白质的用途 激酶抑制剂。
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公开(公告)号：US06897207B2
公开(公告)日：2005-05-24
申请号：US10177804
申请日：2002-06-21
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： A61K20060101 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/4985 , A61K31/5355 , A61K31/5377 , A61K31/541 , A61P20060101 , A61P9/00 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/08 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P27/14 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D241/00 , C07D471/04 , C07D487/04 , C07D519/00 , A61K31/33 , A61K31/66 , C07D417/02
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：和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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6.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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7.发明授权6-aryl/heteroalkyloxy benzothiazole and benzimidazole derivatives, method for preparing same, application thereof as drugs, pharmaceutical compositions and novel use in particular as C-MET inhibitors 失效6-芳基/杂烷氧基苯并噻唑和苯并咪唑衍生物，其制备方法，作为药物的用途，药物组合物和特别用作C-MET抑制剂的新用途公开(公告)号：US08188078B2
公开(公告)日：2012-05-29
申请号：US12761973
申请日：2010-04-16
IPC分类号： A61K31/535 , C07D417/12 , C07D277/82
CPC分类号： C07D235/30 , C07D235/32 , C07D277/82 , C07D417/12
摘要： The disclosure relates to compounds of formula (I): wherein A, W, R, R5, and R6 are as defined in the disclosure, or a salt thereof, and to their use as drugs, in particular as c-Met inhibitors.
摘要翻译： 本公开涉及式（I）的化合物：其中A，W，R，R 5和R 6如本公开内容中所定义，或其盐，以及它们作为药物，特别是作为c-Met抑制剂的用途。
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![NOVEL IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE IN PARTICULAR AS MET INHIBITORS](/abs-image/US/2011/10/20/US20110257171A1/abs.jpg.150x150.jpg)
8.发明申请NOVEL IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE IN PARTICULAR AS MET INHIBITORS 审中-公开新型咪唑并[1,2-A]吡啶衍生物，其制备方法，作为药物，药物组合物和特别用作抑制剂的新用途公开(公告)号：US20110257171A1
公开(公告)日：2011-10-20
申请号：US13003604
申请日：2009-07-16
IPC分类号： A61K31/437 , A61P9/00 , A61P7/04 , A61P3/00 , A61P37/08 , A61P11/06 , A61P7/02 , A61P25/00 , A61P9/10 , A61P17/06 , A61P19/02 , A61P3/10 , A61P21/00 , A61P35/00 , A61P35/04 , C07D413/14 , A61K31/5377 , C07D471/04
CPC分类号： C07D277/82 , C07D471/04
摘要： The invention relates to the novel products of formula (I): in which: Ra is H, Hal, aryl or heteroaryl, which are optionally substituted; Rb is H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc is alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd is 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是任选取代的H，Hal，芳基或杂芳基; Rb是H，Rc，-COORc-CO-Rc或-CO-NRcRd; 其中R c是烷基，环烷基，杂环烷基，芳基和杂芳基，全部被取代; Rd为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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9.发明授权Pyrrolo(2,3-b) pyridine derivatives, the preparation and the pharmaceutical use thereof in the form of kinase inhibitors 失效吡咯（2,3-b）吡啶衍生物，其制备方法及其在激酶抑制剂形式中的用途公开(公告)号：US07968566B2
公开(公告)日：2011-06-28
申请号：US12410135
申请日：2009-03-24
申请人： Sylvie Wentzler , Youssef El-Ahmad , Bruno Filoche-Romme , Conception Nemecek , Corinne Venot , Augustin Hittinger
发明人： Sylvie Wentzler , Youssef El-Ahmad , Bruno Filoche-Romme , Conception Nemecek , Corinne Venot , Augustin Hittinger
IPC分类号： C07D401/14 , A61K31/437
CPC分类号： C07D471/04
摘要： Novel compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R, R1, R2, R3, R4, R5, and R6 have the meanings given in the description, pharmaceutical compositions comprising said compounds and use thereof as protein kinase inhibitors.
摘要翻译： 式（I）的新型化合物或其药学上可接受的盐，其中R，R 1，R 2，R 3，R 4，R 5和R 6具有说明书中给出的含义，包含所述化合物的药物组合物及其作为蛋白激酶抑制剂的用途。
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10.发明授权Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors 失效环状尿素衍生物，其制备方法及其作为激酶抑制剂的药物用途公开(公告)号：US07759379B2
公开(公告)日：2010-07-20
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 , Hervé 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 , Hervé Bouchard
IPC分类号： C07D239/02 , A61K31/505 , A61P43/00
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R1，R2，L1，X，R3，A，R4，R4'，R4“，R4”'，R5，Y和L2如本文所定义， 作为蛋白激酶抑制剂的用途，以及治疗包括其施用的疾病的方法。
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