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公开(公告)号：US07880004B2
公开(公告)日：2011-02-01
申请号：US11521035
申请日：2006-09-14
IPC分类号： A61K31/444 , A61K31/437 , C07D471/04 , C07D213/64
CPC分类号： C07D213/75 , C07D471/04
摘要： The invention is directed to compounds that are useful for the treatment of cancer having the following Formula:
摘要翻译： 本发明涉及可用于治疗具有下式的癌症的化合物：
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公开(公告)号：US07439246B2
公开(公告)日：2008-10-21
申请号：US11292358
申请日：2005-12-01
申请人： Robert M. Borzilleri , Zhong Chen , Tram N. Huynh , Wayne Vaccaro , Xiao-Tao Chen , Kyoung S. Kim , Zhen-wei Cai
发明人： Robert M. Borzilleri , Zhong Chen , Tram N. Huynh , Wayne Vaccaro , Xiao-Tao Chen , Kyoung S. Kim , Zhen-wei Cai
IPC分类号： C07D471/02 , A61K31/519
CPC分类号： C07D487/04 , C07D471/04 , C07D495/04
摘要： In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.
摘要翻译： 通常，本发明包括式I和II的化合物，包括其药学上可接受的盐。 本发明的化合物可用作蛋白激酶抑制剂，因此可用于治疗癌症和其它蛋白激酶介导的疾病。
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公开(公告)号：US07102002B2
公开(公告)日：2006-09-05
申请号：US11152650
申请日：2005-06-14
申请人： Zhen-wei Cai , Louis J. Lombardo , Rajeev S. Bhide , Ligang Qian , Donna D. Wei , Stephanie Barbosa
发明人： Zhen-wei Cai , Louis J. Lombardo , Rajeev S. Bhide , Ligang Qian , Donna D. Wei , Stephanie Barbosa
IPC分类号： C07D487/04 , A61K31/53 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
摘要翻译： 本发明提供式I化合物及其药学上可接受的盐。 式I化合物抑制生长因子受体如VEGFR-2和FGFR-1的酪氨酸激酶活性，从而使其成为抗癌剂。 式I化合物还可用于治疗与通过生长因子受体操作的信号转导途径相关的其它疾病。
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公开(公告)号：US20060009454A1
公开(公告)日：2006-01-12
申请号：US11152650
申请日：2005-06-14
申请人： Zhen-wei Cai , Louis Lombardo , Rajeev Bhide , Ligang Qian , Donna Wei , Stephanie Barbosa
发明人： Zhen-wei Cai , Louis Lombardo , Rajeev Bhide , Ligang Qian , Donna Wei , Stephanie Barbosa
IPC分类号： A61K31/53 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
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公开(公告)号：US20060211695A1
公开(公告)日：2006-09-21
申请号：US11292358
申请日：2005-12-01
申请人： Robert Borzilleri , Zhong Chen , Tram Huynh , Wayne Vaccaro , Xiao-Tao Chen , Kyoung Kim , Zhen-wei Cai
发明人： Robert Borzilleri , Zhong Chen , Tram Huynh , Wayne Vaccaro , Xiao-Tao Chen , Kyoung Kim , Zhen-wei Cai
IPC分类号： A61K31/53 , A61K31/52 , A61K31/519 , C07D498/02 , C07D487/02 , C07D473/02
CPC分类号： C07D487/04 , C07D471/04 , C07D495/04
摘要： In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.
摘要翻译： 通常，本发明包括式I和II的化合物，包括其药学上可接受的盐。 本发明的化合物可用作蛋白激酶抑制剂，因此可用于治疗癌症和其它蛋白激酶介导的疾病。
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6.发明申请Processes and intermediates useful for preparing fused heterocyclic kinase inhibitors 失效用于制备稠合杂环激酶抑制剂的方法和中间体公开(公告)号：US20050288289A1
公开(公告)日：2005-12-29
申请号：US11165875
申请日：2005-06-24
申请人： Gerard Crispino , Stephanie Barbosa , Junying Fan , Zhen-wei Cai
发明人： Gerard Crispino , Stephanie Barbosa , Junying Fan , Zhen-wei Cai
IPC分类号： A61K31/53 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention is directed to intermediates that are useful for preparing pyrrolotriazines, and processes for preparing such intermediates.
摘要翻译： 本发明涉及可用于制备吡咯并三嗪的中间体，以及制备这种中间体的方法。
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7.发明授权Processes and intermediates useful for preparing fused heterocyclic kinase inhibitors 失效用于制备稠合杂环激酶抑制剂的方法和中间体公开(公告)号：US07432373B2
公开(公告)日：2008-10-07
申请号：US11165875
申请日：2005-06-24
申请人： Gerard Crispino , Stephanie Barbosa , Junying Fan , Zhen-wei Cai
发明人： Gerard Crispino , Stephanie Barbosa , Junying Fan , Zhen-wei Cai
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention is directed to intermediates that are useful for preparing pyrrolotriazines, and processes for preparing such intermediates.
摘要翻译： 本发明涉及可用于制备吡咯并三嗪的中间体，以及制备这种中间体的方法。
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公开(公告)号：US06521759B2
公开(公告)日：2003-02-18
申请号：US09839751
申请日：2001-04-20
申请人： Kyoung S. Kim , S. David Kimball , Zhen-wei Cai , David B. Rawlins , Raj N. Misra , Michael A. Poss , Kevin R. Webster , John T. Hunt , Wen-Ching Han
发明人： Kyoung S. Kim , S. David Kimball , Zhen-wei Cai , David B. Rawlins , Raj N. Misra , Michael A. Poss , Kevin R. Webster , John T. Hunt , Wen-Ching Han
IPC分类号： C07D41712
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D417/12 , C07D417/14
摘要： The present invention describes compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, m and n are as defined in the specification. The compounds of formula I are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, chemotherapy-induced alopecia, and cardiovascular disease.
摘要翻译： 本发明描述了式I的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，m和n如说明书中所定义。 式I的化合物是蛋白激酶抑制剂，可用于治疗增殖性疾病，例如癌症，炎症和关节炎。 它们也可用于治疗阿尔茨海默病，化学疗法诱发的脱发和心血管疾病。
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公开(公告)号：US6040321A
公开(公告)日：2000-03-21
申请号：US176239
申请日：1998-10-21
申请人： Kyoung S. Kim , S. David Kimball , Zhen-wei Cai , David B. Rawlins , Raj N. Misra , Michael A. Poss , Kevin R. Webster , John T. Hunt , Wen-Ching Han
发明人： Kyoung S. Kim , S. David Kimball , Zhen-wei Cai , David B. Rawlins , Raj N. Misra , Michael A. Poss , Kevin R. Webster , John T. Hunt , Wen-Ching Han
IPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/497 , A61K31/506 , A61P1/04 , A61P9/00 , A61P9/10 , A61P9/14 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/10 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/06 , A61P43/00 , C07D263/00 , C07D277/00 , C07D277/42 , C07D277/44 , C07D277/54 , C07D417/12 , C07D417/14 , A61K31/425
CPC分类号： C07D417/14 , C07D417/12
摘要： Compounds of the formula ##STR1## and pharmaceuticaly acceptable salts thereof. As used in formula I, and throughout the specification, the symbols have the following meanings:R.sub.1 and R.sub.2 are independently hydrogen, fluorine or alkyl;R.sub.3 is aryl or heteroarylR.sub.4 is hydrogen, alkyl, cycloalkyl, aryl, cycloalkylalkyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl; orCO-alkyl,CONH-alkyl,COO-alkyl,SO.sub.2 -alkyl,C(NCN)NH-alkyl,C(NNO.sub.2)NH-alkyl,C(NH)NH-alkyl,C(NH)NHCO-alkyl,C(NOR.sub.6)NH-alkyl,R.sub.5 is hydrogen or alkyl;R.sub.6 is hydrogen, alkyl, cycloalkyl, aryl, cycloalkylakyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;m is an integer of 0 to 2; andn is an integer of 1 to 3.The compounds of formula I are protein kinase inhibitors and are useful in the treatment and prevention of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, viral diseases and fungal diseases.
摘要翻译： 式的化合物及其药学上可接受的盐。 如式I所用，在整个说明书中，符号具有以下含义：R 1和R 2独立地为氢，氟或烷基; R 3是芳基或杂芳基R 4是氢，烷基，环烷基，芳基，环烷基烷基，芳基烷基，杂芳基，杂芳基烷基，杂环烷基，杂环烷基烷基; 或（C 1 -C 10）烷基，C 1 -C 6烷基，CO 2 - 烷基，SO 2 - 烷基，C（NCN）NH-烷基，C （NOR6）NH-烷基，R5是氢或烷基; R 6是氢，烷基，环烷基，芳基，环烷基烷基，芳基烷基，杂芳基，杂芳基烷基，杂环烷基或杂环烷基烷基; m为0〜2的整数; 并且n是1至3的整数。式I化合物是蛋白激酶抑制剂，可用于治疗和预防增殖性疾病，例如癌症，炎症和关节炎。 它们也可用于治疗神经变性疾病如阿尔茨海默病，心血管疾病，病毒性疾病和真菌性疾病。
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公开(公告)号：US20070117802A1
公开(公告)日：2007-05-24
申请号：US11521035
申请日：2006-09-14
申请人： Robert Borzilleri , Zhen-wei Cai , Donna Wei , John Tokarski
发明人： Robert Borzilleri , Zhen-wei Cai , Donna Wei , John Tokarski
IPC分类号： A61K31/53 , A61K31/519 , C07D487/04 , C07D491/02
CPC分类号： C07D213/75 , C07D471/04
摘要： The invention is directed to compounds that are useful for the treatment of cancer having the following Formula:
摘要翻译： 本发明涉及可用于治疗具有下式的癌症的化合物：
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