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1. 发明申请

US20060247210A1 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：US20060247210A1
公开(公告)日：2006-11-02
申请号：US10521948
申请日：2003-07-23
申请人： Zaihui Zhang , Timothy Daynard , Shisen Wang , Xinyao Du , Gregory Chopiuk , Jun Yan , Jianxin Chen , Serguei Sviridov
发明人： Zaihui Zhang , Timothy Daynard , Shisen Wang , Xinyao Du , Gregory Chopiuk , Jun Yan , Jianxin Chen , Serguei Sviridov
IPC分类号： A61K31/675 , A61K31/428 , A61K31/655 , C07D417/02
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。 R 1，R 2，R 3和R 3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，磷酸酯，次膦酸酯，膦酸酯，鏻，硫代磷酸酯，磷酰基，氨磺酰，硫酸根，亚磺酸，亚磺酰氨基，磺酸，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。

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

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。

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

US07196083B2 Heteropolycyclic inhibitors of protein kinases 失效
标题翻译：蛋白激酶的杂多环抑制剂
公开(公告)号：US07196083B2
公开(公告)日：2007-03-27
申请号：US10310600
申请日：2002-12-04
申请人： Zaihui Zhang , Xinyao Du , Serguei Sviridov , Greg Chopiuk
发明人： Zaihui Zhang , Xinyao Du , Serguei Sviridov , Greg Chopiuk
IPC分类号： A61K31/53
CPC分类号： C07D487/04 , C07D513/04
摘要： A method of inhibiting tumor growth is provided, comprising administering an effective dose of a compound of the formula wherein, independently at each occurrence, w is C or N, v and x are N with H substitution as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as needed to fulfill open valence sites, with the proviso that each of w, v, x, y and z is not simultaneously C; the ring formed from v, w, x, y and z may be saturated or unsaturated; and R1, R2, R3 and R4 are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R1, R2, R3 and R4 may join together to form a 5, 6 or 7-membered carbocyclic ring or a 5, 6 or 7-membered heterocyclic ring containing at least one atom selected from nitrogen, oxygen and sulfur.
摘要翻译：提供了一种抑制肿瘤生长的方法，包括施用有效剂量的下式的化合物

6. 发明授权

US06514972B2 Heteropolycyclic inhibitors of protein kinases 失效
标题翻译：蛋白激酶的杂多环抑制剂
公开(公告)号：US06514972B2
公开(公告)日：2003-02-04
申请号：US09900073
申请日：2001-07-06
申请人： Zaihui Zhang , Xinyao Du , Serguei Sviridov , Greg Chopiuk
发明人： Zaihui Zhang , Xinyao Du , Serguei Sviridov , Greg Chopiuk
IPC分类号： C07D48704
CPC分类号： C07D487/04 , C07D513/04
摘要： A compound of the formula wherein, independently at each occurrence, v, w, and x are selected from C, N, O, and S, with H substitution as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as needed to fulfill open valence sites, with the proviso that each of w, v, x, y and z is not simultaneously C; the ring formed from v, w, x, y and z may be saturated or unsaturated; and R1, R2, R3 and R4 are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R1, R2, R3 and R4 may join together to form a 5, 6 or 7-membered carbocyclic or heterocyclic ring, with the proviso that each of R1, R2, R3 and R4 is not simultaneously hydrogen. Pharmaceutical compositions of said compounds, and methods of use in the treatment of biological conditions including cellular hyperproliferation, are disclosed.
摘要翻译：在每次出现时，v，w和x独立地选自C，N，O和S的化合物，根据需要进行H取代以实现开价值位点; y和z选自N和C，根据需要进行H取代以满足开价值位置，条件是w，v，x，y和z中的每一个不同时为C; 由v，w，x，y和z形成的环可以是饱和或不饱和的; 并且R 1，R 2，R 3和R 4选自氢，烷基，芳基，烷芳基，芳烷基，杂烷基和杂芳基; 其中R 1，R 2，R 3和R 4中的任何相邻的两个可以连接在一起以形成5,6或7-元碳环或杂环，条件是R 1，R 2，R 3和R 4中的每一个不是同时氢。公开了所述化合物的药物组合物，以及用于治疗包括细胞过度增殖的生物学条件的方法。

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