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61. 发明授权

US07053086B2 4-heteroaryl-3-heteroarylidenyl-2-indolinones and their use as protein kinase inhibitors 失效
公开(公告)号：US07053086B2
公开(公告)日：2006-05-30
申请号：US10648810
申请日：2003-08-27
申请人： Peng Cho Tang , Chung Chen Wei , Ping Huang , Jingrong Cui
发明人： Peng Cho Tang , Chung Chen Wei , Ping Huang , Jingrong Cui
IPC分类号： C07D403/14 , A61K31/14
CPC分类号： C07D401/04 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D417/14 , C07D491/04
摘要： The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.

62. 发明申请

US20050176802A1 Pyrrole substituted 2-indolinone protein kinase inhibitors 有权
标题翻译：吡咯取代的2-二氢吲哚酮蛋白激酶抑制剂
公开(公告)号：US20050176802A1
公开(公告)日：2005-08-11
申请号：US11028477
申请日：2005-01-04
申请人： Peng Cho Tang , Todd Miller , Xiaoyuan Li , Li Sun , Chung Chen Wei , Shahrzad Shirazian , Congxin Liang , Tomas Vojkovsky , Asaad Nematalla , Michael Hawley
发明人： Peng Cho Tang , Todd Miller , Xiaoyuan Li , Li Sun , Chung Chen Wei , Shahrzad Shirazian , Congxin Liang , Tomas Vojkovsky , Asaad Nematalla , Michael Hawley
IPC分类号： C07D401/14 , A61K31/404 , A61K31/4178 , A61K31/4439 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P3/10 , A61P9/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D207/32 , C07D207/33 , C07D209/44 , C07D401/12 , C07D403/00 , C07D403/06 , C07D403/12 , C07D403/14 , C07D521/00 , C07D43/14
CPC分类号： C07D233/56 , C07D207/33 , C07D209/44 , C07D231/12 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14
摘要： The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
摘要翻译：本发明涉及吡咯取代的2-二氢吲哚酮化合物及其药学上可接受的盐，其调节蛋白激酶的活性，因此预期可用于预防和治疗与蛋白激酶相关的细胞病症例如癌症。

63. 发明授权

US06906093B2 Indolinone combinatorial libraries and related products and methods for the treatment of disease 失效
标题翻译：吲哚酮组合文库及相关产品及治疗方法
公开(公告)号：US06906093B2
公开(公告)日：2005-06-14
申请号：US09897755
申请日：2001-07-03
申请人： Peng Cho Tang , Li Sun , Gerald McMahon , Klaus Peter Hirth , Laura Kay Shawver
发明人： Peng Cho Tang , Li Sun , Gerald McMahon , Klaus Peter Hirth , Laura Kay Shawver
IPC分类号： C07D209/34 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D455/06 , C07D495/04 , G06F13/40 , A61K31/40 , C07D209/02
CPC分类号： C07D401/06 , C07D209/34 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D455/06 , C07D495/04 , G06F13/4045
摘要： The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
摘要翻译：本发明涉及能够调节酪氨酸激酶信号转导以调节，调节和/或抑制异常细胞增殖的有机分子。

64. 发明授权

US06696463B2 3-heteroarylidenyl-2-azaindolinones active as protein tyrosine kinase inhibitors 失效
标题翻译：作为蛋白酪氨酸激酶抑制剂有活性的3-杂芳基-2-氮杂吲哚酮
公开(公告)号：US06696463B2
公开(公告)日：2004-02-24
申请号：US09948106
申请日：2001-09-07
申请人： Peng Cho Tang , Li Sun , Gerald McMahon
发明人： Peng Cho Tang , Li Sun , Gerald McMahon
IPC分类号： C07D20942
CPC分类号： C07D209/34
摘要： The invention relates to 3-heteroarylidenyl-2-azaindolinone compounds of the formula: wherein, A is selected from the group consisting of nitrogen, oxygen and sulfur; only one of B, D, E, F or G is nitrogen; Z is selected from the group consisting of oxygen, sulfur and NR11; or physiologically acceptable salts thereof; and wherein the groups R1-R7 are defined herein. The 3-heteroarylidenyl-2-azaindolinone compounds of the preferred embodiments of the present invention have improved hydrosolubility and are expected to modulate the activity of protein tyrosine kinases. The 3-heteroarylidenyl-2-azaindolinone compounds of the preferred embodiments of the present invention should be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.
摘要翻译：本发明涉及下式的3-杂芳基-2-氮杂吲哚酮化合物：其中A选自氮，氧和硫; B，D，E，F或G中只有一个是氮;选择Z 由氧，硫和NR 11组成的组; 其生理上可接受的盐;并且其中基团R 1 -R 7在本文中定义。本发明优选实施方案的3-杂芳基-2-氮杂吲哚酮化合物具有改善的水溶性，并且预期调节蛋白酪氨酸激酶的活性。本发明优选实施方案的3-杂芳基-2-氮杂吲哚酮化合物可用于预防和治疗蛋白质酪氨酸激酶相关细胞病症如癌症。

65. 发明授权

US06683082B2 Bicyclic protein kinase inhibitors 失效
标题翻译：双环蛋白激酶抑制剂
公开(公告)号：US06683082B2
公开(公告)日：2004-01-27
申请号：US09819698
申请日：2001-03-29
申请人： Peng Cho Tang , Li Sun , Gerald McMahon
发明人： Peng Cho Tang , Li Sun , Gerald McMahon
IPC分类号： A61K31495
CPC分类号： C07D471/04 , C07D209/34
摘要： The present invention relates to novel 3-hetero-arylidene-2-indolinone compounds and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
摘要翻译：本发明涉及调节蛋白激酶活性的新型3-异亚烷基-2-二氢吲哚酮化合物及其生理上可接受的盐，因此预期可用于预防和治疗蛋白激酶相关的细胞病症例如癌症。

66. 发明授权

US06677368B2 4-aryl substituted indolinones 失效
标题翻译： 4-芳基取代的二氢吲哚酮
公开(公告)号：US06677368B2
公开(公告)日：2004-01-13
申请号：US10023488
申请日：2001-12-20
申请人： Jingrong Cui , Ruofei Zhang , Hong Shen , Ji Yu Chu , Fang-Jie Zhang , Marcel Koenig , Steven Huy Do , Xiaoyuan Li , Chung Chen Wei , Peng Cho Tang
发明人： Jingrong Cui , Ruofei Zhang , Hong Shen , Ji Yu Chu , Fang-Jie Zhang , Marcel Koenig , Steven Huy Do , Xiaoyuan Li , Chung Chen Wei , Peng Cho Tang
IPC分类号： A61K3140
CPC分类号： C07D403/14 , C07D209/34 , C07D401/14 , C07D403/06 , C07D417/14 , C07D487/04
摘要： The present invention relates to 4-arylindolinones, as well as pharmaceutical compositions thereof, capable of modulating protein kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. The present invention also relates to methods for treating protein kinase related disorders.
摘要翻译：本发明涉及能够调节蛋白激酶信号转导以调节，调节和/或抑制异常细胞增殖的4-芳基吲哚啉酮及其药物组合物。本发明还涉及治疗蛋白激酶相关病症的方法。

67. 发明授权

US06610688B2 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors 失效
标题翻译： 4-取代的7-氮杂 - 二氢吲哚-2-酮及其作为蛋白激酶抑制剂的用途
公开(公告)号：US06610688B2
公开(公告)日：2003-08-26
申请号：US09741737
申请日：2000-12-21
申请人： Congxin Liang , Li Sun , Chung Chen Wei , Peng Cho Tang , Gerald McMahon , Klaus Peter Hirth , Jingrong Cui
发明人： Congxin Liang , Li Sun , Chung Chen Wei , Peng Cho Tang , Gerald McMahon , Klaus Peter Hirth , Jingrong Cui
IPC分类号： C07D48704
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention relates to 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors. Particular 4-substituted 7-aza-indolin-2-ones disclosed herein are of Formula 1 and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, X, Y, and Z are defined herein. The invention further relates to pharmaceutical compositions and dosage forms comprising compounds of Formula 1 and to methods of their use for the treatment and/or prevention of diseases such as, but not limited to, cancer.
摘要翻译：本发明涉及4-取代的7-氮杂 - 二氢吲哚-2-酮及其作为蛋白激酶抑制剂的用途。本文公开的特定的4-取代的7-氮杂 - 二氢吲哚-2-酮是式1及其药学上可接受的盐，溶剂合物，包合物和前药，其中R1，R2，R3，R4，X，Y和Z如本文所定义。本发明还涉及包含式1化合物的药物组合物和剂型，以及它们用于治疗和/或预防疾病例如但不限于癌症的方法。

68. 发明授权

US06525072B1 Geometrically restricted 2-indolinone derivatives as modulators of protein kinase activity 失效
公开(公告)号：US06525072B1
公开(公告)日：2003-02-25
申请号：US09385974
申请日：1999-08-30
申请人： Peng Cho Tang , Todd Anthony Miller , Li Sun , Ngoc My Tran , Asaad Nematalla , Anh Thi Nguyen
发明人： Peng Cho Tang , Todd Anthony Miller , Li Sun , Ngoc My Tran , Asaad Nematalla , Anh Thi Nguyen
IPC分类号： C07D20934
CPC分类号： C07D209/34
摘要： The present invention relates to novel geometrically restricted 2-indolinones and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.

69. 发明授权

US06225346B1 Tyrphostin like compounds 失效
标题翻译：酪氨酸磷酸酯类化合物
公开(公告)号：US06225346B1
公开(公告)日：2001-05-01
申请号：US09372395
申请日：1999-08-10
申请人： Peng Cho Tang , Li Sun , Asaad S. Nematalla , Gerald McMahon
发明人： Peng Cho Tang , Li Sun , Asaad S. Nematalla , Gerald McMahon
IPC分类号： A61K31275
CPC分类号： C07C311/13 , C07C317/46 , C07D333/34
摘要： The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.
摘要翻译：本发明涉及能够调节酪氨酸信号转导以通过抑制一种或多种异常酪氨酸激酶活性来预防和治疗与特定酪氨酸激酶相关的细胞增殖性疾病或细胞分化障碍的分子。

70. 发明授权

US6004967A Psoriasis treatment with quinazoline compounds 失效
标题翻译：用喹唑啉化合物治疗牛皮癣
公开(公告)号：US6004967A
公开(公告)日：1999-12-21
申请号：US927442
申请日：1997-09-11
申请人： Gerald McMahon , Laura Shawver , Blair Narog , Peng Cho Tang , Klaus Peter Hirth
发明人： Gerald McMahon , Laura Shawver , Blair Narog , Peng Cho Tang , Klaus Peter Hirth
IPC分类号： A61K31/517 , A61K31/505
CPC分类号： A61K31/517
摘要： This invention is directed to methods and compositions for treating hyperproliferative skin disorders utilizing a quinazoline derivative as an active ingredient.
摘要翻译：本发明涉及利用喹唑啉衍生物作为活性成分治疗过度增生性皮肤病的方法和组合物。

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