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1. 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）。}}

2. 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。

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

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。

5. 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.

6. 发明申请

WO2003022846A1 1-GLYOXLYLAMIDE INDOLIZINES FOR TREATING CANCER 审中-公开
标题翻译： 1-GLYOXLYLAMIDE INDOLIZINES FOR TRANTING CANCER
公开(公告)号：WO2003022846A1
公开(公告)日：2003-03-20
申请号：PCT/US2002/029154
申请日：2002-09-13
申请人： SBR PHARMACEUTICALS CORP. , KOYA, Keizo , SUN, Lijun , ONO, Mitsunori , YING, Weiwen , LI, Hao
发明人： KOYA, Keizo , SUN, Lijun , ONO, Mitsunori , YING, Weiwen , LI, Hao
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Disclosed is a compound represented by Structural Fonnula (I): Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z 1 and Z 2 are independently =0, =S, =N-OR 12 or =NR 12 ; R 1 and R 2 are independently -H, an aliphatic group, a substituted aliphatic group, an unsubstituted non-aromatic heterocylic group, a substituted non-aromatic heterocylic group, an aryl group or a substituted aryl group, provided that R 1 and R 2 are not both -H. Alternatively, -NR 1 R 2 , taken together, is a substituted or unsubstituted non-aromatic nitrogen-containing heterocyclic group or a substituted or unsubstituted nitrogen-containing heteroaryl group. R 3 is a substituted or unsubstituted aryl group or a substituted or unsubstituted aliphatic group. X is a covalent bond, -C(R 4 R 5 )-, -N(R 4 )-, -0-, -S-, -S(O)-, -S(0) 2 -, -C(=O)-, -C(=0)-N(R 4 )-, or N(R 4 )-C(=O)-. R 4 and R 5 are independently -H or a substituted or unsubstituted aliphatic group. R 12 is -H or a substituted or unsubstituted alkyl group.
摘要翻译：公开了由结构式（I）表示的化合物：环A是取代或未取代的，并任选地与芳基稠合。 Z> 1 <和Z> 2 <独立地= 0，= S，= N-OR> 12 <或= NR> 12 < R 1和R 2独立地是-H，脂族基团，取代的脂族基团，未取代的非芳族杂环基团，取代的非芳族杂环基团，芳基或取代的芳基，条件是 R＆gt; 1＆lt;和＆lt; 2＆gt;不同于-H。或者，-NR> 1 2一起是取代或未取代的非芳族含氮杂环基或取代或未取代的含氮杂芳基。 R 3是取代或未取代的芳基或取代或未取代的脂族基。 X是共价键，-C（R 5）5 - ， - （R 4） - ， - O - ， - S - ， - S（O） - ， - S（O） > - ， - （= O） - ， - （= O）-N（R 4） - 或N（R 4））C（= O） - 。 R 4和R 5独立地是-H或取代或未取代的脂族基团。 R 12为-H或取代或未取代的烷基。

7. 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.

8. 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。

9. 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。

10. 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.

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