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1. 发明申请

WO2009023211A1 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
标题翻译：调节HSP90活性的三唑化合物
公开(公告)号：WO2009023211A1
公开(公告)日：2009-02-19
申请号：PCT/US2008/009667
申请日：2008-08-13
申请人： SYNTA PHARMACEUTICALS CORP. , YING, Weiwen , SUN, Lijun , KOYA, Keizo , CHIMMANAMADA, Dinesh, U. , ZHANG, Shijie , PRZEWLOKA, Teresa , LI, Hao
发明人： YING, Weiwen , SUN, Lijun , KOYA, Keizo , CHIMMANAMADA, Dinesh, U. , ZHANG, Shijie , PRZEWLOKA, Teresa , LI, Hao
IPC分类号： C07F9/6518 , C07F9/6558 , A61K31/4196 , A61K31/5355
CPC分类号： A61K31/675 , C07D209/04 , C07D249/08 , C07D403/04 , C07F9/65182 , C07F9/65583 , C07F9/65586
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
摘要翻译：本发明涉及取代的三唑化合物和包含取代的三唑化合物的组合物。本发明还涉及在有需要的受试者中抑制Hsp90的活性的方法和在有需要的受试者中预防或治疗过度增殖性疾病如癌症的方法，其包括向受试者施用本发明的取代的三唑化合物，或包含这种化合物的组合物。

2. 发明申请

WO2008136976A2 COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS 审中-公开
标题翻译：治疗增殖性疾病的化合物
公开(公告)号：WO2008136976A2
公开(公告)日：2008-11-13
申请号：PCT/US2008/005512
申请日：2008-04-28
申请人： SYNTA PHARMACEUTICALS CORP. , KOYA, Keizo , YING, Weiwen , PRZEWLOKA, Teresa , SUN, Lijun
发明人： KOYA, Keizo , YING, Weiwen , PRZEWLOKA, Teresa , SUN, Lijun
IPC分类号： C07C259/18 , C07C391/00 , C07C395/00 , A61K31/166 , A61P35/00
CPC分类号： C07C391/00 , A61K31/165 , A61K31/18 , A61K45/06 , C07C259/20 , C07C2601/02
摘要： Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
摘要翻译：公开了使用本发明化合物治疗患有增殖性病症（例如癌症）的受试者的化合物和方法，以及治疗对Hsp70诱导和/或自然杀伤细胞诱导有反应的病症的方法。还公开了包含本发明化合物和药学上可接受的载体的药物组合物。

3. 发明申请

WO2007139955A3 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
公开(公告)号：WO2007139955A3
公开(公告)日：2007-12-06
申请号：PCT/US2007/012524
申请日：2007-05-25
申请人： SYNTA PHARMACEUTICALS CORP. , CHAE, Junghyun , DEMKO, Zachary , YING, Weiwen , DU, Zhenjian , FOLEY, Kevin , JAMES, David , PRZEWLOKA, Teresa , SONG, Minghu , ZHANG, Shijie , NG, Howard, P. , LI, Hao , CHIMMANAMADA, Dinesh, U. , SUN, Lijun , KOYA, Keizo , ZHOU, Dan , QIN, Shuzhen , LEE, Chi-wan
发明人： CHAE, Junghyun , DEMKO, Zachary , YING, Weiwen , DU, Zhenjian , FOLEY, Kevin , JAMES, David , PRZEWLOKA, Teresa , SONG, Minghu , ZHANG, Shijie , NG, Howard, P. , LI, Hao , CHIMMANAMADA, Dinesh, U. , SUN, Lijun , KOYA, Keizo , ZHOU, Dan , QIN, Shuzhen , LEE, Chi-wan
IPC分类号： A61K31/4196 , A61P31/00 , C07D249/12 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/04 , C07D417/04
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

4. 发明申请

WO2003047516A2 PYRIMIDINE COMPOUNDS 审中-公开
标题翻译：嘧啶化合物
公开(公告)号：WO2003047516A2
公开(公告)日：2003-06-12
申请号：PCT/US2002/038161
申请日：2002-11-27
申请人： SYNTA PHARMACEUTICALS CORPORATION , ONO, Mitsunori , SUN, Lijun , PRZEWLOKA, Teresa , ZHANG, Shijie , KOSTIK, Elena , YING, Weiwen , WADA, Yumiko , KOYA, Keizo , WU, Yaming , ZHOU, Dan , TATSUTA, Noriaki
发明人： ONO, Mitsunori , SUN, Lijun , PRZEWLOKA, Teresa , ZHANG, Shijie , KOSTIK, Elena , YING, Weiwen , WADA, Yumiko , KOYA, Keizo , WU, Yaming , ZHOU, Dan , TATSUTA, Noriaki
IPC分类号： A61K
CPC分类号： C07D239/48 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D401/14 , C07D403/12
摘要： This invention features pyrimidine compounds of formula (I): R 1 is formula (II), aryl, or heteroaryl; each of R 2 and R 4 , independently, is R c , halogen, nitro, cyano, isothionitro, SR c , or OR c ; or R 2 and R 4 , taken together, is carbonyl; R 3 is R c , alkenyl, alkynyl, OR c , OC(O)R c , S0 2 R c , S(O)R c , S(0 2 )NR c R d , SR c , NR c R d , NR c COR d , NR c C(O)OR d , NR c C(O)NR c R d , NR c S0 2 R d , COR c , C(O)OR c , or C(O)NR c R d ; R 5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(0 2 ), or NR c ; Y is a covalent bond, CH 2 , C(O), C=N-R c , C=N-OR c , C=N-SR c , O, S, S(O), S(0 2 ), or NR c ; Z is N or CH; one of U and V is N, and the other is CR c ; and W is O, S, S(O), S(0 2 ), NR c , or NC(O)R c ; in which each of R a and R b , independently, is H, alkyl, aryl, heteroaryl; and each of R c and R d , independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl. The compounds are useful for treating IL-12 overproduction related diseases (e.g., rheumatoid arthritis, sepsis, Crohn's disease, multiple sclerosis, psoriasis, or insulin-dependent diabetes mellitus).
摘要翻译：本发明的特征是式（I）的嘧啶化合物：R1是式（II），芳基或杂芳基; 每个R 2和R 4独立地为R c，卤素，硝基，氰基，异硫氰酸根，SR c， sup>或OR ^{c ; 或者R 2和R 4合在一起为羰基; R 3是R c，烯基，炔基，OR c，OC（O）R c，S 0，（O）R c，S（O 2）NR c，其中R 1，R 2， R c，NR c，NR c，NR c，NR c，NR c，NR c R c，（O）OR d，NR c C（O）NR s，C（O）NR c， R c，R c，R c，R c，R c，R c，R c，R c，R c，R c， C（O）OR c或C（O）NR c R d; R 5是H或烷基; n是0,1,2,3,4,5或6; X是O，S，S（O），S（O 2）或NR C; Y是共价键，CH 2，C（O），C = NR c，C = N-OR c，C = N -S（O）S，S（O），S（O 2）或NR C; Z是N或CH; U和V中的一个是N，另一个是CR ^{c ; 和W是O，S，S（O），S（O 2），NR C或NC（O）R C; 其中R a和R b各自独立地为H，烷基，芳基，杂芳基; 并且每个R c和R d独立地为H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基。该化合物可用于治疗IL-12过量产生相关疾病（例如类风湿性关节炎，败血症，克罗恩氏病，多发性硬化症，牛皮癣或胰岛素依赖性糖尿病）。}}

5. 发明申请

WO2006089177A2 COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS 审中-公开
标题翻译：用于治疗增生性疾病的化合物
公开(公告)号：WO2006089177A2
公开(公告)日：2006-08-24
申请号：PCT/US2006/005761
申请日：2006-02-16
申请人： SYNTA PHARMACEUTICALS CORP. , SUN, Lijun , BORELLA, Christopher , LI, Hao , JIANG, Jun , CHEN, Shoujun , KOYA, Keizo , INOUE, Takayo , DU, Zhenjian , FOLEY, Kevin , WU, Yaming , ZHANG, Mei , YING, Weiwen
发明人： SUN, Lijun , BORELLA, Christopher , LI, Hao , JIANG, Jun , CHEN, Shoujun , KOYA, Keizo , INOUE, Takayo , DU, Zhenjian , FOLEY, Kevin , WU, Yaming , ZHANG, Mei , YING, Weiwen
IPC分类号： C07D261/08 , C07D413/04 , A61K31/42 , A61P35/00
CPC分类号： C07D413/14 , A61K31/42 , A61K31/426 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/675 , A61K45/06 , C07D261/08 , C07D413/04 , C07D413/10 , C07F9/653
摘要： The invention relates to compounds of structural formula (I); or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein R a , R b , and R 2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
摘要翻译：本发明涉及结构式（I）的化合物; 或其药学上可接受的盐，溶剂化物，包合物和前药，其中R a，R b和R 2均在本文中定义。这些化合物抑制微管蛋白聚合和/或靶向脉管系统，并且可用于治疗增殖性疾病，例如癌症。

6. 发明申请

WO2004035740A2 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2004035740A2
公开(公告)日：2004-04-29
申请号：PCT/US2003/032546
申请日：2003-10-14
申请人： SYNTA PHARMACEUTICALS CORP. , SUN, Lijun , ONO, Mitsunori , WADA, Yumiko , YING, Weiwen , PRZEWLOKA, Teresa , KOSTIK, Elena
发明人： SUN, Lijun , ONO, Mitsunori , WADA, Yumiko , YING, Weiwen , PRZEWLOKA, Teresa , KOSTIK, Elena
IPC分类号： C12N
CPC分类号： C07D473/34 , C07D473/16 , C07D473/18
摘要： This invention features a compound of formula (I): R 1 is aryl or heteroaryl; each of R 2 and R 4 , independently, is H, halogen, CN, alkyl, OR a , or NR a R b ; R 3 is H, halogen, CN, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, OR a , OC(O)R a , OC(O)NR a R b , NR a R b , NR a C(O)R b , NR a S(O)R b , NR a S(O)2R b , NR a C(O)NR b R c NR a C(S)NR b R ° , NR a C(NR b )NR c R d , NR a C(O)OR b , S(O)NTR a R t , S(O) 2 NR S R b , S(O)R a , S(O) 2 R a , C(O)R a , C(O)OR a , or C(O)NR a R l ; R 5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; A is 0, S, S(O), S(O) 2 , or NW; B is N or CR C ; X is 0, S, S(O), S(O) 2 , NR, or C(O); Y is a covalent bond, C(O), C=NR a, O, S, S(O), S(O) 2 , or NW; Z is N or CH; each of U and V, independently, is N or CR; and W is 0, S, or NR ' ; in which each of R a , R b , R e , and R d , independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; R e is H, alkyl, aryl, acyl, or sufonyl; and R f is H, alkyl., aryl, acyl, sulfonyl, alkoxyl, amino, ester, amide, CN, or halogen. The compound is useful for treating an interleukin- 12 overproduction-related disorder.
摘要翻译：本发明的特征在于式（I）的化合物：R 1是芳基或杂芳基; R 2和R 4各自独立地是H，卤素，CN，烷基，OR a或NR a R b; R 3是H，卤素，CN，烷基，烯基，炔基，芳基，杂芳基，环基，杂环基，OR a，OC（O）R a，OC（O）NR a R b，NR NR a C（O）R b，NR a S（O）R b，NR a S（O）2 R b，NR a， C（O）NR b R c C（S）NR b，NR a C（NR b）NR c R d， NR a C（O）OR b，S（O）NTR a R t，S（O）2 NR s R b，S（O）R a， O）2 R a，C（O）R a，C（O）OR a或C（O）NR a R 1; R 5是H或烷基; n是0，1，2，3，4，5或6; A为0，S，S（O），S（O）2或NW; B为N或CR ; X为0，S，S（O），S（O）2，NR或C（O）; Y是共价键，C（O），C = NR a，O，S，S（O），S（O）2或NW; Z是N或CH; U和V各自独立地是N或CR; 且W为0，S或NR'; 其中R a，R b，R e和R d各自独立地是H，烷基，芳基，杂芳基，环基或杂环基; R e是H，烷基，芳基，酰基或磺酰基; 并且R f是H，烷基，芳基，酰基，磺酰基，烷氧基，氨基，酯，酰胺，CN或卤素。该化合物可用于治疗白细胞介素-12过度生产相关疾病。

7. 发明申请

WO2008097640A3 TRIAZOLE COMPOUNDS THAT ARE USEFUL IN THE TREATMENT OF PROLIFERATIVE DISORDERS, SUCH AS CANCER 审中-公开
公开(公告)号：WO2008097640A3
公开(公告)日：2008-08-14
申请号：PCT/US2008/001693
申请日：2008-02-08
申请人： SYNTA PHARMACEUTICALS CORP. , CHIMMANAMADA, Dinesh, U. , BURLISON, Joseph, A. , YING, Weiwen , SUN, Lijun , SCHWEIZER, Stefan, Michael , ZHANG, Shijie , DEMKO, Zachary , JAMES, David , PRZEWLOKA, Teresa
发明人： CHIMMANAMADA, Dinesh, U. , BURLISON, Joseph, A. , YING, Weiwen , SUN, Lijun , SCHWEIZER, Stefan, Michael , ZHANG, Shijie , DEMKO, Zachary , JAMES, David , PRZEWLOKA, Teresa
IPC分类号： C07D249/08 , C07D249/10 , C07D249/12 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D417/14 , A61K31/4196 , A61P35/00
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to the use of a substituted triazole compound of the invention, or a composition comprising such a compound in the preparation of a medicament for preventing or treating hyperprolif erative disorders, such as cancer, in a subject in need thereof.

8. 发明申请

WO2007139967A3 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
公开(公告)号：WO2007139967A3
公开(公告)日：2007-12-06
申请号：PCT/US2007/012543
申请日：2007-05-25
申请人： SYNTA PHARMACEUTICALS CORP. , YING, Weiwen , PRZEWLOKA, Teresa , CHAE, Junghyun , ZHANG, Shijie , LI, Hao , DU, Zhenjian , JAMES, David , CHIMMANAMADA, Dinesh, U. , NG, Howard, P. , FOLEY, Kevin , DEMKO, Zachary , SUN, Lijun , ZHOU, Dan , QIN, Shuzhen
发明人： YING, Weiwen , PRZEWLOKA, Teresa , CHAE, Junghyun , ZHANG, Shijie , LI, Hao , DU, Zhenjian , JAMES, David , CHIMMANAMADA, Dinesh, U. , NG, Howard, P. , FOLEY, Kevin , DEMKO, Zachary , SUN, Lijun , ZHOU, Dan , QIN, Shuzhen
IPC分类号： C07D249/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/14 , C07D487/04 , A61K31/4196 , A61P35/00
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

9. 发明申请

WO2007139952A2 SYNTHESIS OF TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
标题翻译：调节HSP90活性的三唑化合物的合成
公开(公告)号：WO2007139952A2
公开(公告)日：2007-12-06
申请号：PCT/US2007/012520
申请日：2007-05-25
申请人： SYNTA PHARMACEUTICALS CORP. , LEE, Chi-wan , JAMES, David , ZHANG, Shijie , YING, Weiwen , CHIMMANAMADA, Dinesh, U. , CHAE, Junghyun , PRZEWLOKA, Teresa
发明人： LEE, Chi-wan , JAMES, David , ZHANG, Shijie , YING, Weiwen , CHIMMANAMADA, Dinesh, U. , CHAE, Junghyun , PRZEWLOKA, Teresa
CPC分类号： C07D403/04 , C07D249/12 , C07D249/14 , C07D401/04 , C07D401/10 , C07D403/10 , C07D413/04 , C07D417/04
摘要： The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) with an oxidizing agent, thereby producing a compound of formula (IA). The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: (IB) or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: (HB) in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula: (IIIB).
摘要翻译：本发明提供抑制Hsp90活性的三唑化合物的新方法。本发明的一个实施方案涉及制备由以下结构式表示的三唑化合物或互变异构体，药学上可接受的盐，溶剂合物或包合物或其前药的方法，其包括以下步骤：a）使酰胺由以下结构式表示：用硫化试剂形成硫代酰胺; b）使步骤a）的硫代酰胺与肼反应形成腙酰胺; c）使步骤b）的腙与羰基化或硫代羰基化试剂反应。在一个实施方案中，本发明是合成式（IA）化合物或互变异构体，其药学上可接受的盐，溶剂合物或包合物或其前药的方法，包括使式（IIA）化合物与氧化剂，从而制备式（IA）化合物。本发明还涉及由以下结构式：（IB）或互变异构体，其药学上可接受的盐，溶剂合物或包合物或其前药代表的化合物或其互变异构体的制备方法。该方法包括使由以下结构式：（HB）表示的第一起始化合物在汞盐存在下与由以下结构式：（IIIB）表示的第二起始化合物反应的步骤。

10. 发明申请

WO2006055760A1 TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY 审中-公开
公开(公告)号：WO2006055760A1
公开(公告)日：2006-05-26
申请号：PCT/US2005/041779
申请日：2005-11-17
申请人： SYNTA PHARMACEUTICALS CORP. , YING, Weiwen , JAMES, David , ZHANG, Shijie , PRZEWLOKA, Teresa , CHAE, Junghyun , CHIMMANAMADA, Dinesh, U. , LEE, Chi-Wan , KOSTIK, Elena , NG, Howard, P. , FOLEY, Kevin , DU, Zhenjian , BARSOUM, James
发明人： YING, Weiwen , JAMES, David , ZHANG, Shijie , PRZEWLOKA, Teresa , CHAE, Junghyun , CHIMMANAMADA, Dinesh, U. , LEE, Chi-Wan , KOSTIK, Elena , NG, Howard, P. , FOLEY, Kevin , DU, Zhenjian , BARSOUM, James
IPC分类号： C07D249/12 , C07D401/04 , C07D405/04 , C07D403/04 , A61K31/4196 , A61P35/00
CPC分类号： C07D249/08 , A61K31/4196 , C07D249/12 , C07D401/04 , C07D403/04 , C07D403/10 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D473/00 , C07D473/34
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

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