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1. 发明授权

US08410272B2 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：US08410272B2
公开(公告)日：2013-04-02
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： A61K31/437 , C07D513/04
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 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。

2. 发明授权

US07875728B2 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：US07875728B2
公开(公告)日：2011-01-25
申请号：US10497046
申请日：2002-10-18
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： C07D231/14 , 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。

3. 发明授权

US07288556B2 Antiproliferative 1,2,3-thiadiazole compounds 有权
标题翻译：抗增殖性1,2,3-噻二唑化合物
公开(公告)号：US07288556B2
公开(公告)日：2007-10-30
申请号：US11218969
申请日：2005-09-02
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： C07D285/06 , A61K31/41
CPC分类号： A61K31/433 , C07D285/06
摘要： This invention is directed to methods of using compounds having the structure: and including stereoisomers, solvates, and pharmaceutically acceptable salts thereof, wherein each of R1, R2, R3 and R4 is independently selected from hydrogen, R5, R6, 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 A1, A2, and A3 is independently selected from a direct bond, alkylene, heteroalkylene, arylene and heteroarylene. These compounds are useful in treating hyperproliferative disorders and inducing apoptosis.
摘要翻译：本发明涉及使用具有以下结构的化合物的方法：其包括立体异构体，溶剂化物和药学上可接受的盐，其中R 1，R 2，R 2， SO 3和R 4独立地选自氢，R 5，R 6和R 7， / SUP>; R 5选自烷基，杂烷基，芳基和杂芳基; R 6选自（R 5）N 1 - 亚烷基，（R 5）亚磺酰基，（R 5） - 亚芳基和（R 5）5 - 亚杂芳基。 R 7选自（R 6）N - 亚烷基，（R 6）亚磺酰基，（R 6） - 亚芳基和（R 6） - 亚 - 亚芳基 ; 并且n选自0,1,2,3,4和5，其中R 1和R 2可以一起形成杂环结构，包括它们是氮的杂环结构两个连接的R 3和R 4可以一起形成包括它们都连接的氮的杂环结构; 并且L 1和L 2各自独立地选自-A1-A2-A3-，其中A1，A2和A3各自独立地选自直接键，亚烷基，杂亚烷基，亚芳基和亚杂芳基。这些化合物可用于治疗过度增殖性疾病和诱导凋亡。

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