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1. 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。

2. 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）。}}

3. 发明申请

WO2005046604A3 HETEROARYL-HYDRAZONE COMPOUNDS 审中-公开
公开(公告)号：WO2005046604A3
公开(公告)日：2005-05-26
申请号：PCT/US2004/037479
申请日：2004-11-10
申请人： SYNTA PHARMACEUTICALS, CORP. , ONO, Mitsunori , SUN, Lijun , WADA, Yumiko , KOSTIK, Elena , NG, Howard, P.
发明人： ONO, Mitsunori , SUN, Lijun , WADA, Yumiko , KOSTIK, Elena , NG, Howard, P.
IPC分类号： A61K31/497
摘要： This invention relates to compounds having a formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, hydrate, prodrug or polymorph thereof wherein X is -C(R g )=N-A. The invention also relates to methods of treating IL-12 verproduction-related disorders, methods of treating or preventing disorders related with excessive bone loss, methods for inhibiting osteoclast formation, and methods for treating or preventing a disorder associated with excessive bone resorption.

4. 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.

5. 发明申请

WO2007094819A2 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：WO2007094819A2
公开(公告)日：2007-08-23
申请号：PCT/US2006/032199
申请日：2006-08-17
申请人： SYNTA PHARMACEUTICALS CORP. , YING, Weiwen , JAMES, Davis , PRZEWLOKA, Teresa , KOSTIK, Elena , CHAE, Junghyun , NG, Howard, P. , DU, Zhenjian , BARSOUM, James , CHIMMANAMADA, Dinesh, U. , LEE, Chi-wan , FOLEY, Kevin , ZHANG, Shije
发明人： YING, Weiwen , JAMES, Davis , PRZEWLOKA, Teresa , KOSTIK, Elena , CHAE, Junghyun , NG, Howard, P. , DU, Zhenjian , BARSOUM, James , CHIMMANAMADA, Dinesh, U. , LEE, Chi-wan , FOLEY, Kevin , ZHANG, Shije
CPC分类号： C07D249/08 , C07D403/10 , C07D403/12 , C07D413/12
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。

6. 发明申请

WO2004082606A3 FUSED PYRROLE COMPOUNDS 审中-公开
公开(公告)号：WO2004082606A3
公开(公告)日：2004-09-30
申请号：PCT/US2004/007469
申请日：2004-03-11
申请人： SYNTA PHARMACEUTICALS CORP. , ONO, Mitsunori , SUN, Lijun , XIA, Zhi, Qiang , KOSTIK, Elena , KOYA, Keizo , WU, Yaming , NAGAI, Masazumi
发明人： ONO, Mitsunori , SUN, Lijun , XIA, Zhi, Qiang , KOSTIK, Elena , KOYA, Keizo , WU, Yaming , NAGAI, Masazumi
IPC分类号： C07D487/04
摘要： This invention relates to fused pyrrole compounds of Formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein V 1 , V 2 , V 3 , V 4 , R 1 , R 2 , R 3 , W 1 and W 2 are as defined herein. The compounds of this invention may be used to prevent or treat cancer, inflammatory disorders, autoimmune diseases and other conditions involving PDE4 or elevated levels of cytokines. The invention also provides methods of using the compounds to treat or prevent such disorders and pharmaceutical compositions containing the compounds.

7. 发明申请

WO2006053227A2 IL-12 MODULATORY COMPOUNDS 审中-公开
标题翻译： IL-12调节化合物
公开(公告)号：WO2006053227A2
公开(公告)日：2006-05-18
申请号：PCT/US2005/040952
申请日：2005-11-10
申请人： SYNTA PHARMACEUTICALS CORP. , SUN, Lijun , KOSTIK, Elena , PRZEWLOKA, Teresa , NG, Howard, P. , CHIMMANAMADA, Dinesh , DEMKO, Zachary
发明人： SUN, Lijun , KOSTIK, Elena , PRZEWLOKA, Teresa , NG, Howard, P. , CHIMMANAMADA, Dinesh , DEMKO, Zachary
IPC分类号： A61K31/5377
CPC分类号： C07D403/12 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/48 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention relates to heterocyclic compounds, compositions including the compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.
摘要翻译：本发明涉及杂环化合物，包括该化合物的组合物及其使用方法及其制备方法。化合物（和组合物）尤其用于调节由IL-12介导的IL-12产生和过程。

8. 发明申请

WO2007050980A2 PROCESS FOR PREPARING MESYLATE SALTS OF IL-12 INHIBITORY COMPOUNDS 审中-公开
标题翻译：制备IL-12抑制化合物的甲磺酸盐的方法
公开(公告)号：WO2007050980A2
公开(公告)日：2007-05-03
申请号：PCT/US2006/042211
申请日：2006-10-27
申请人： SYNTA PHARMACEUTICALS CORP. , KOSTIK, Elena , SUN, Lijun , KOYA, Keizo , BOULAS, Pierre, L.
发明人： KOSTIK, Elena , SUN, Lijun , KOYA, Keizo , BOULAS, Pierre, L.
IPC分类号： C07D239/48
CPC分类号： C07D401/12 , C07D213/64 , C07D213/77 , C07D239/48 , C07D251/42 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D491/10
摘要： This invention relates to a method of preparing mesylate salts of compounds that inhibit IL-12, IL-23 and/or IL-27 production.
摘要翻译：本发明涉及制备抑制IL-12，IL-23和/或IL-27产生的化合物的甲磺酸盐的方法。

9. 发明申请

WO2006053112A1 PROCESS FOR PREPARING TRISUBSTITUTED PYRIMIDINE COMPOUNDS 审中-公开
标题翻译：制备三唑啉化合物的方法
公开(公告)号：WO2006053112A1
公开(公告)日：2006-05-18
申请号：PCT/US2005/040712
申请日：2005-11-10
申请人： SYNTA PHARMACEUTICALS CORP. , ZHANG, Shijie , KOSTIK, Elena , SUN, Lijun
发明人： ZHANG, Shijie , KOSTIK, Elena , SUN, Lijun
IPC分类号： C07D417/04 , C07D413/04 , C07D409/04 , C07D405/04 , C07D401/04 , A61K31/506 , A61K31/5375 , A61P19/02
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14
摘要： Disclosed herein is a regioselective synthesis of compounds represented by formula (I): or a salt, solvate, clathrate, or prodrug thereof, wherein X, Y, R 2 , R 3 , R 4 , R 7 , R 8 , R 9 , R 10 , m and n are defined as within.
摘要翻译：本文所公开的是由式（I）表示的化合物的区域选择性合成：或其盐，溶剂化物，包合物或前药，其中X，Y，R 2，R 3， R 4，R 7，R 8，R 9，R 10， >，m和n定义为内。

10. 发明申请

WO2005112938A3 DISALT INHIBITORS OF IL-12 PRODUCTION 审中-公开
公开(公告)号：WO2005112938A3
公开(公告)日：2005-12-01
申请号：PCT/US2005/012578
申请日：2005-04-13
申请人： SYNTA PHARMACEUTICALS CORP. , KOSTIK, Elena , SUN, Lijun
发明人： KOSTIK, Elena , SUN, Lijun
IPC分类号： C07D403/04
摘要： This invention relates to disalt nitrogen-heteroaryl inhibitors of IL-12 production, and related methods and pharmaceutical compositions.

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