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1.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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2.发明申请公开(公告)号：US20050215553A1
公开(公告)日：2005-09-29
申请号：US11009249
申请日：2004-12-10
IPC分类号： A61K31/50 , A61K31/501 , A61K31/5377 , A61P1/02 , A61P3/14 , A61P9/00 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/02 , A61P29/00 , A61P31/00 , A61P35/00 , C07B61/00 , C07D237/04 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07K5/06 , G01N33/53
CPC分类号： C07K5/06026 , C07B2200/11 , C07D237/04 , C40B40/00
摘要： The present invention discloses and claims hexahydropyridazine-3-carboxylic acid hydrazides and hydrazones of formula (I) as inhibitors of proteases and kinases, and methods of using said compounds of formula (I) for the prevention or treatment of certain cardiovascular, central nervous system, inflammatory, and bone diseases as well as infectious diseases and certain cancers. Combinatorial libraries of the compounds of formula (I), pharmaceutical compositions, and methods for the preparation of combinatorial libraries and the compounds of formula (I) are also disclosed and claimed.
摘要翻译： 本发明公开并要求具有式（I）的六氢哒嗪-3-羧酸酰肼和腙作为蛋白酶和激酶的抑制剂，以及使用所述式（I）化合物预防或治疗某些心血管，中枢神经系统的方法 ，炎症和骨疾病以及传染病和某些癌症。 还公开并要求保护式（I）化合物的组合文库，药物组合物和制备组合文库和式（I）化合物的方法。
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3.发明授权Substituted pyrazoles, compositions containing these, method of production and use 有权取代的吡唑，含有这些的组合物，生产和使用方法公开(公告)号：US07989439B2
公开(公告)日：2011-08-02
申请号：US12437618
申请日：2009-05-08
申请人： Kirsten Bjergarde , Mark Dodson , Jacques Mauger , Anil Nair , Marcel Patek , Michel Tabart
发明人： Kirsten Bjergarde , Mark Dodson , Jacques Mauger , Anil Nair , Marcel Patek , Michel Tabart
IPC分类号： A61K31/535
CPC分类号： C07C273/18 , C07D231/38 , C07C275/38
摘要： The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.
摘要翻译： 本公开涉及式（I）的化合物及其盐; 其中Ar，L，A，X，R 1，R 2，R 3，R 4a，R 4b和R 5如本公开所定义; 包含所述化合物的组合物，其制备方法，其中间体及其用途，特别是作为药物。
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4.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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5.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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6.发明授权Hexahydropyridazine-3-carboxylic acid derivatives, pharmaceutical compositions containing same and methods of preparation 失效六氢哒嗪-3-羧酸衍生物，含有它们的药物组合物和制备方法公开(公告)号：US07034022B2
公开(公告)日：2006-04-25
申请号：US10979679
申请日：2004-11-02
IPC分类号： A01N43/58 , A61K31/50 , A61K31/501 , C07D237/00 , C07D237/02
CPC分类号： C07D401/12 , C07D237/04 , C07D403/12 , C07D409/12 , C07D413/12
摘要： The present invention discloses and claims compounds of formula (I) as inhibitors of proteases and kinases, method using said compounds of formula (I) for the prevention or treatment of certain cardiovascular, central nervous system, inflammatory, and bone diseases as well as infectious diseases and certain cancers. Combinatorial libraries of compounds of formula (I), pharmaceutical compositions and methods for preparation of combinatorial libraries and compounds of formula (I) are also disclosed and claimed.
摘要翻译： 本发明公开并要求作为蛋白酶和激酶抑制剂的式（I）化合物，使用所述式（I）化合物用于预防或治疗某些心血管，中枢神经系统，炎症和骨疾病以及感染性 疾病和某些癌症。 式（I）化合物的组合文库，药物组合物和制备组合文库和式（I）化合物的方法也被公开并要求保护。
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7.发明申请Hexahydropyridazine-3-carboxylic acid derivatives, pharmaceutical compositions containing same and methods of preparation 失效六氢哒嗪-3-羧酸衍生物，含有它们的药物组合物和制备方法公开(公告)号：US20050171346A1
公开(公告)日：2005-08-04
申请号：US10979679
申请日：2004-11-02
IPC分类号： A61K31/50 , A61K31/501 , A61K31/506 , A61P1/02 , A61P3/14 , A61P9/00 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07D237/04 , C07D401/12 , C07D403/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D43/02 , C07D237/02
CPC分类号： C07D401/12 , C07D237/04 , C07D403/12 , C07D409/12 , C07D413/12
摘要： The present invention discloses and claims compounds of formula (I) as inhibitors of proteases and kinases, method using said compounds of formula (I) for the prevention or treatment of certain cardiovascular, central nervous system, inflammatory, and bone diseases as well as infectious diseases and certain cancers. Combinatorial libraries of compounds of formula (I), pharmaceutical compositions and methods for preparation of combinatorial libraries and compounds of formula (I) are also disclosed and claimed.
摘要翻译： 本发明公开并要求作为蛋白酶和激酶抑制剂的式（I）化合物，使用所述式（I）化合物用于预防或治疗某些心血管，中枢神经系统，炎症和骨疾病以及感染性 疾病和某些癌症。 式（I）化合物的组合文库，药物组合物和制备组合文库和式（I）化合物的方法也被公开并要求保护。
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8.发明授权Substituted pyrazoles, compositions containing these, method of production and use 失效取代的吡唑，含有这些的组合物，生产和使用方法公开(公告)号：US08410286B2
公开(公告)日：2013-04-02
申请号：US13156915
申请日：2011-06-09
申请人： Kirsten Bjergarde , Mark Dodson , Jacques Mauger , Anil Nair , Marcel Patek , Michel Tabart
发明人： Kirsten Bjergarde , Mark Dodson , Jacques Mauger , Anil Nair , Marcel Patek , Michel Tabart
IPC分类号： C07D231/10 , C07D231/12
CPC分类号： C07C273/18 , C07D231/38 , C07C275/38
摘要： The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.
摘要翻译： 本公开涉及式（I）的化合物及其盐; 其中Ar，L，A，X，R 1，R 2，R 3，R 4a，R 4b和R 5如本公开所定义; 包含所述化合物的组合物，其制备方法，其中间体及其用途，特别是作为药物。
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公开(公告)号：US20110237801A1
公开(公告)日：2011-09-29
申请号：US13156947
申请日：2011-06-09
申请人： Kirsten BJERGARDE , Mark DODSON , Jacques MAUGER , Anil NAIR , Marcel PATEK , Michel TABART
发明人： Kirsten BJERGARDE , Mark DODSON , Jacques MAUGER , Anil NAIR , Marcel PATEK , Michel TABART
IPC分类号： C07D401/12 , C07D231/38 , C07F7/10
CPC分类号： C07C273/18 , C07D231/38 , C07C275/38
摘要： The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.
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10.发明申请SUBSTITUTED PYRAZOLES, COMPOSITIONS CONTAINING THESE, METHOD OF PRODUCTION AND USE 失效取代的吡唑，包含这些的组合物，生产和使用方法公开(公告)号：US20110237641A1
公开(公告)日：2011-09-29
申请号：US13156915
申请日：2011-06-09
申请人： Kirsten BJERGARDE , Mark DODSON , Jacques MAUGER , Anil NAIR , Marcel PATEK , Michel TABART
发明人： Kirsten BJERGARDE , Mark DODSON , Jacques MAUGER , Anil NAIR , Marcel PATEK , Michel TABART
IPC分类号： A61K31/415 , C07D231/38 , C12N9/99 , A61P35/00
CPC分类号： C07C273/18 , C07D231/38 , C07C275/38
摘要： The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.
摘要翻译： 本公开涉及式（I）的化合物及其盐; 其中Ar，L，A，X，R 1，R 2，R 3，R 4a，R 4b和R 5如本公开所定义; 包含所述化合物的组合物，其制备方法，其中间体及其用途，特别是作为药物。
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