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1. 发明授权

US08202876B2 Compounds and compositions as protein kinase inhibitors 有权
标题翻译：化合物和组合物作为蛋白激酶抑制剂
公开(公告)号：US08202876B2
公开(公告)日：2012-06-19
申请号：US12444129
申请日：2007-09-24
申请人： Pamela Albaugh , Gregory B. Chopiuk , Qiang Ding , Shenlin Huang , Zuosheng Liu , Shifeng Pan , Pingda Ren , Xia Wang , Xing Wang , Yongping Xie , Chengzhi Zhang , Qiong Zhang , Guobao Zhang , Daniel Poon , Paul Renhowe , Martin Sendzik
发明人： Pamela Albaugh , Gregory B. Chopiuk , Qiang Ding , Shenlin Huang , Zuosheng Liu , Shifeng Pan , Pingda Ren , Xia Wang , Xing Wang , Yongping Xie , Chengzhi Zhang , Qiong Zhang , Guobao Zhang , Daniel Poon , Paul Renhowe , Martin Sendzik
IPC分类号： C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D231/00 , C07D403/02 , A01N43/56 , A61K31/415
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D417/14
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases.
摘要翻译：本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Abl，ARG，BCR异常活化的疾病或病症 -Abl，BRK，EphB，Fms，Fyn，KDR，c-Kit，LCK，PDGF-R，b-Raf，c-Raf，SAPK2，Src，Tie2和TrkB激酶。

2. 发明申请

US20110178126A1 PYRAZOLYLBENZOTHIAZOLE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 有权
标题翻译：吡唑并苯并噻唑衍生物及其作为治疗剂的用途
公开(公告)号：US20110178126A1
公开(公告)日：2011-07-21
申请号：US12910744
申请日：2010-10-22
申请人： Zaihui Zhang , Timothy S. Daynard , Shisen Wang , Xinyao Du , Gregory B. Chopiuk , Jun Yan , Jianxin Chen , Serguei V. Sviridov
发明人： Zaihui Zhang , Timothy S. Daynard , Shisen Wang , Xinyao Du , Gregory B. Chopiuk , Jun Yan , Jianxin Chen , Serguei V. Sviridov
IPC分类号： A61K31/454 , C07D277/62 , C07D417/14 , C07D261/20 , A61K31/426 , A61K31/4439 , A61P35/00
CPC分类号： C07D417/04 , A61K31/428 , A61K31/655 , A61K31/675 , C07D231/12 , C07D233/56 , C07D249/08 , C07D413/04 , C07D417/14 , C07D513/04 , A61K2300/00
摘要： Pharmaceutical compositions and compounds are provided. The compounds of the invention have use as therapeutic agents, e.g., they demonstrate anti-proliferative, anti-inflammatory, anti-angiogenic, anti-migration activities. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of, e.g., anti-inflammatory, renal, and hyperproliferative disorders. The compounds of the invention are pyrazolylbenzothiazole derivatives of the following formula (1) wherein X, R1, R2, R3 and R4 are described herein.
摘要翻译：提供药物组合物和化合物。本发明的化合物可用作治疗剂，例如它们表现出抗增殖，抗炎，抗血管生成，抗迁移活性。在本发明的一个实施方案中，提供了与生理上可接受的载体组合的化合物的制剂。药物制剂可用于治疗，例如抗炎，肾和过度增殖性疾病。本发明的化合物是下式（1）的吡唑基苯并噻唑衍生物，其中X，R1，R2，R3和R4如本文所述。

3. 发明授权

US08445694B2 Hydrazonopyrazole derivatives and their use as therapeutics 有权
标题翻译：肼吡唑衍生物及其作为治疗剂的用途
公开(公告)号：US08445694B2
公开(公告)日：2013-05-21
申请号：US12977794
申请日：2010-12-23
申请人： Zaihui Zhang , Timothy S. Daynard , Mikhail A. Chafeev , Shisen Wang , Gregory B. Chopiuk , Serguei V. Sviridov
发明人： Zaihui Zhang , Timothy S. Daynard , Mikhail A. Chafeev , Shisen Wang , Gregory B. Chopiuk , Serguei V. Sviridov
IPC分类号： C07D231/38 , A61K31/415
CPC分类号： C07D417/12 , A61K31/415 , A61K31/4155 , A61K31/655 , C07D231/04 , C07D231/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/04
摘要： Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
摘要翻译：提供药物组合物和化合物。本发明化合物表现出抗增殖活性，并可能促进缺乏细胞周期和死亡正常调节的细胞凋亡。在本发明的一个实施方案中，提供了与生理上可接受的载体组合的化合物的药物组合物。该药物组合物可用于治疗过度增殖性疾病，该疾病包括肿瘤生长，淋巴组织增生性疾病，血管生成。本发明的化合物是取代的吡唑和吡唑啉。

4. 发明授权

US07847101B2 Pyrazolylbenzothiazole derivatives and their use as therapeutic agents 有权
标题翻译：吡唑基苯并噻唑衍生物及其用作治疗剂
公开(公告)号：US07847101B2
公开(公告)日：2010-12-07
申请号：US10521948
申请日：2003-07-23
申请人： Zaihui Zhang , Timothy S. Daynard , Shisen Wang , Xinyao Du , Gregory B. Chopiuk , Jun Yan , Jianxin Chen , Serguei V. Sviridov
发明人： Zaihui Zhang , Timothy S. Daynard , Shisen Wang , Xinyao Du , Gregory B. Chopiuk , Jun Yan , Jianxin Chen , Serguei V. Sviridov
IPC分类号： A61K31/428 , C07D413/14 , C07D417/14 , C07D417/04
CPC分类号： C07D417/04 , A61K31/428 , A61K31/655 , A61K31/675 , C07D231/12 , C07D233/56 , C07D249/08 , C07D413/04 , C07D417/14 , C07D513/04 , A61K2300/00
摘要： Pharmaceutical pyrazolybenzothiazole compositions of formula (1) are provided. The compositions may be pharmaceutically acceptable salts. R1, R2 and R3 at each occurrence are independently selected from amino, aminosulfinyl, aminosulfonyl, aryl, azido, halogen, heteroalkyl, heteroaryl, hydrazinyl, hydrocarbyl, hydrogen, hydroxyl, nitro, nitroso, phosphate, phosphinate, phosphonate, phosphonium, phosphorothioate, phosphoryl, sulfamoyl, sulfate, sulfinic acid, sulfonamido, sulfonate, sulfonic acid, sulfonyl, sulfoxido, thiol, thioureido, and ureido, and R4 is selected from hydrogen, heteroalkyl, heteroaryl, and hydrocarbyl.
摘要翻译：提供式（1）的药物吡唑并苯并噻唑组合物。组合物可以是药学上可接受的盐。 R1，R2和R3各自独立地选自氨基，氨基亚磺酰基，氨基磺酰基，芳基，叠氮基，卤素，杂烷基，杂芳基，肼基，烃基，氢，羟基，硝基，亚硝基，磷酸根，次膦酸根，膦酸根，鏻，硫代磷酸酯，磷酰基，氨磺酰基，硫酸根，亚磺酸，亚磺酰氨基，磺酸根，磺酸，磺酰基，亚砜基，硫醇，硫脲基和脲基，R 4选自氢，杂烷基，杂芳基和烃基。

5. 发明授权

US07022702B2 Antiproliferative 1,2,3-thiadiazole compounds 失效
公开(公告)号：US07022702B2
公开(公告)日：2006-04-04
申请号：US10144203
申请日：2002-05-10
申请人： Zaihui Zhang , Gregory B. Chopiuk , Timothy S. Daynard , Shisen Wang
发明人： Zaihui Zhang , Gregory B. Chopiuk , Timothy S. Daynard , Shisen Wang
IPC分类号： A61K31/433 , C07D285/06
CPC分类号： A61K31/433 , C07D285/06
摘要： Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are 1,2,3-thiadiazoles having the structure: and including stereoisomers, solvates, and pharmaceutically acceptable salts thereof, wherein each of R1, R22 , R3 and R4 is independently selected from hydrogen, R5R6, and R7, R5 is selected from alkyl, heteroalkyl, aryl and heteroaryl; R6 is selected from (R5)n-alkylene, (R5)n-heteroalkylene, (R5)n-arylene and (R5)n-heteroarylene; R7 is selected from (R6)n-alkylene, (R6)n-heteroalkylene, (R6)n-arylene, and (R6)n-heteroarylene; and n is selected from 0, 1, 2, 3, 4 and 5, where R1 and R2 may together form a heterocyclic structure including the nitrogen to which they are both attached, and R3 and R4 may together form a heterocyclic structure including the nitrogen to which they are both attached; and each of L1 and L2 is independently selected from -A1-A2-A3- where each of Al, A2, and A3 is independently selected from a direct bond, alkylene, heteroalkylene, arylene and heteroarylene.

6. 发明申请

US20110237783A1 HYDRAZONOPYRAZOLE DERIVATIVES AND THEIR USE AS THERAPEUTICS 有权
标题翻译：水合唑衍生物及其用作治疗药物
公开(公告)号：US20110237783A1
公开(公告)日：2011-09-29
申请号：US12977794
申请日：2010-12-23
申请人： Zaihui Zhang , Timothy S. Daynard , Mikhail A. Chafeev , Shisen Wang , Gregory B. Chopiuk , Serguei V. Sviridov
发明人： Zaihui Zhang , Timothy S. Daynard , Mikhail A. Chafeev , Shisen Wang , Gregory B. Chopiuk , Serguei V. Sviridov
IPC分类号： C07D231/38 , C07D401/02 , C07D417/02 , C07D403/02 , C07D215/02 , C07F9/6503 , C07D401/14 , C07D217/00 , C07D413/02
CPC分类号： C07D417/12 , A61K31/415 , A61K31/4155 , A61K31/655 , C07D231/04 , C07D231/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/04
摘要： Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
摘要翻译：提供药物组合物和化合物。本发明化合物表现出抗增殖活性，并可能促进缺乏细胞周期和死亡正常调节的细胞凋亡。在本发明的一个实施方案中，提供了与生理上可接受的载体组合的化合物的药物组合物。该药物组合物可用于治疗过度增殖性疾病，该疾病包括肿瘤生长，淋巴组织增生性疾病，血管生成。本发明的化合物是取代的吡唑和吡唑啉。

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