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1. 发明申请

WO2010039236A1 COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES 审中-公开
标题翻译：用于炎症和免疫相关用途的化合物
公开(公告)号：WO2010039236A1
公开(公告)日：2010-04-08
申请号：PCT/US2009/005406
申请日：2009-10-01
申请人： SYNTA PHARMACEUTICALS CORP. , BOHNERT, Gary , XIA, Zhiqiang , CHEN, Shoujun , SUN, Lijun
发明人： BOHNERT, Gary , XIA, Zhiqiang , CHEN, Shoujun , SUN, Lijun
IPC分类号： C07D211/96 , C07D401/04 , C07D401/14 , C07D417/04 , C07D417/14 , A61K31/435 , A61K31/495 , A61P29/00 , A61P37/00
CPC分类号： C07D401/04 , A61K31/497 , A61K45/06 , C07D211/96 , C07D401/14 , C07D417/04 , C07D417/14
摘要： The invention relates to certain compounds or pharmaceutically acceptable salts thereof, including derivatives of tetrahydropyridine, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
摘要翻译：本发明涉及某些化合物或其药学上可接受的盐，包括四氢吡啶的衍生物，其可用作免疫抑制剂并用于治疗和预防炎性病症，过敏性疾病和免疫疾病。

2. 发明申请

WO2009105257A1 COMPOUNDS FOR TREATING 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：WO2009105257A1
公开(公告)日：2009-08-27
申请号：PCT/US2009/001102
申请日：2009-02-20
申请人： SYNTA PHARMACEUTICALS CORP. , PRZEWLOKA, Teresa , SUN, Lijun
发明人： PRZEWLOKA, Teresa , SUN, Lijun
IPC分类号： C07C327/56 , C07D295/30 , A61K31/495 , A61K31/5375 , A61K31/16 , A61P35/00
CPC分类号： C07C327/56 , C07D295/30
摘要： Disclosed are compounds of Formula (I) 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：公开了式（I）的化合物和使用本发明化合物治疗患有增殖性疾病如癌症的受试者的方法，以及用于治疗对Hsp70诱导和/或自然杀伤诱导反应的病症的方法。此外，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

WO2008024303A2 COMPOUNDS FOR TREATING 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：WO2008024303A2
公开(公告)日：2008-02-28
申请号：PCT/US2007/018378
申请日：2007-08-20
申请人： SYNTA PHARMACEUTICALS CORP. , CHEN, Shoujun , KOYA, Keizo , DEMKO, Zachary , SUN, Lijun
发明人： CHEN, Shoujun , KOYA, Keizo , DEMKO, Zachary , SUN, Lijun
IPC分类号： C07C327/56 , A61K31/16 , A61P35/00 , C07C307/04 , C07C311/49 , C07C311/51
CPC分类号： C07C327/56 , A61K31/16 , A61K31/166 , A61K31/18 , A61K31/277 , A61K31/341 , A61K31/40 , A61K31/4245 , A61K31/664 , C07C243/28 , C07C243/34 , C07C255/66 , C07C257/22 , C07C261/04 , C07C281/06 , C07C307/04 , C07C311/49 , C07C311/51 , C07C311/55 , C07C337/06 , C07C2601/02 , C07D207/34 , C07D207/36 , C07D233/74 , C07D263/48 , C07D271/10 , C07D271/113 , C07D307/66 , C07F9/228 , C07F9/4423 , C07F9/4496 , C07F9/46
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疾病如癌症的受试者的化合物和方法，以及用于治疗对Hsp70诱导和/或自然杀伤诱导反应的病症的方法。此外，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。

4. 发明申请

WO2006053109A1 HETEROARYL COMPOUNDS 审中-公开
标题翻译：杂环化合物
公开(公告)号：WO2006053109A1
公开(公告)日：2006-05-18
申请号：PCT/US2005/040706
申请日：2005-11-10
申请人： SYNTA PHARMACEUTICALS CORP. , SUN, Lijun , ZHANG, Shijie , KOYA, Keizo , CHIMMANAMADA, Dinesh , LI, Hao , JAMES, David , KOSTIK, Elena
发明人： SUN, Lijun , ZHANG, Shijie , KOYA, Keizo , CHIMMANAMADA, Dinesh , LI, Hao , JAMES, David , KOSTIK, Elena
IPC分类号： C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , A61K31/44 , A61K31/506 , A61K31/53 , A61P3/10 , A61P17/06 , A61P19/02 , A61P25/28 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , A61K31/5375 , A61K31/541
CPC分类号： C07D213/75 , C07D213/77 , C07D239/47 , C07D239/48 , C07D239/50 , C07D239/56 , C07D251/42 , C07D251/52 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D491/10
摘要： This invention relates to compounds of formula (I) their compositions and methods of use thereof. The compounds (and compositions) are useful in modulating IL-12 production and processes mediated by IL-12.
摘要翻译：本发明涉及式（I）化合物的组合物及其使用方法。化合物（和组合物）可用于调节由IL-12介导的IL-12产生和过程。

5. 发明申请

WO2005046603A2 PYRIDINE COMPOUNDS 审中-公开
标题翻译：吡啶化合物
公开(公告)号：WO2005046603A2
公开(公告)日：2005-05-26
申请号：PCT/US2004/037476
申请日：2004-11-10
申请人： SYNTA PHARMACEUTICALS, CORP. , ONO, Mitsunori , SUN, Lijun , WADA, Yumiko , PRZEWLOKA, Teresa , LI, Hao , NG, Howard, P. , DEMKO, Zachary
发明人： ONO, Mitsunori , SUN, Lijun , WADA, Yumiko , PRZEWLOKA, Teresa , LI, Hao , NG, Howard, P. , DEMKO, Zachary
IPC分类号： A61K
CPC分类号： C07D413/12 , C04B35/632 , C07D213/77 , C07D401/12 , C07D405/12
摘要： This invention features compounds of formula (I): pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia , IL-12-related diseases and disorders.
摘要翻译：本发明的特征在于式（I）化合物：化合物的药物组合物，以及使用该化合物治疗特别是IL-12相关疾病和病症的方法。

6. 发明申请

WO2005000404A2 HETEROCYCLIC COMPOUNDS FOR PREVENTING AND TREATING DISORDERS ASSOCIATED WITH EXCESSIVE BONE LOSS 审中-公开
标题翻译：用于预防和治疗与骨质疏松相关的疾病的异种化合物
公开(公告)号：WO2005000404A2
公开(公告)日：2005-01-06
申请号：PCT/US2004/017064
申请日：2004-05-28
申请人： SYNTA PHARMACEUTICALS, CORP. , ONO, Mitsunori , SUN, Lijun , WADA, Yumiko , KOYA, Keizo , NAGAI, Masazumi
发明人： ONO, Mitsunori , SUN, Lijun , WADA, Yumiko , KOYA, Keizo , NAGAI, Masazumi
IPC分类号： A61P
CPC分类号： C07D413/14 , C07D239/48 , C07D251/18 , C07D251/52 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/12 , C07D473/16
摘要： This invention relates to pyrimidine compounds of formula (I), formula (I')’ and formula (I’’): formula (I) and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , U, V, W, X, Y, Z, and n are defined herein. This invention also relates to compositions comprising these compounds and methods for using them. The compounds and compositions of this invention are useful to treat or prevent disorders associated with excessive bone loss, including, without limitation periodontal disease, non-malignant bone disorders (such as osteoporosis, Paget's disease of bone, osteogenesis imperfecta, fibrous dysplasia, and primary hyperparathyroidism) estrogen deficiency, inflammatory bone loss, bone malignancy, arthritis, osteopetrosis, and certain cancer-related disorders (such as hypercalcernia of malignancy (HCM), osteolytic bone lesions of multiple myeloma and osteolytic bone metastases of breast cancer and other metastatic cancers).
摘要翻译：本发明涉及式（I），式（I'）'和式（I“）：式（I）的嘧啶化合物及其药学上可接受的盐，溶剂化物，包合物和前药，其中R1，R2，R3， R4，R5，U，V，W，X，Y，Z和n在本文中定义。本发明还涉及包含这些化合物的组合物和使用它们的方法。本发明的化合物和组合物可用于治疗或预防与过度骨质流失相关的疾病，包括但不限于牙周病，非恶性骨病（如骨质疏松症，骨Paget氏病，成骨不全，纤维性发育异常和原发性甲状旁腺功能亢进），雌激素缺乏症，炎性骨质流失，骨恶性肿瘤，关节炎，骨质疏松症和某些癌症相关疾病（如恶性高钙血症（HCM），多发性骨髓瘤溶骨性骨病变以及乳腺癌和其他转移性癌症溶骨性骨转移）。

7. 发明申请

WO2004064826A1 BIS (THIO-HYDRAZIDE AMIDE) COMPOUNDS FOR TREATING MULTI-DRUG RESISTANT CANCER 审中-公开
标题翻译： BIS（THIO-HYDRAZIDE AMIDE）化合物用于治疗多种耐药性癌症
公开(公告)号：WO2004064826A1
公开(公告)日：2004-08-05
申请号：PCT/US2004/001089
申请日：2004-01-15
申请人： SYNTA PHARMACEUTICALS CORP. , KOYA, Keizo , SUN, Lijun , WU, Yaming , KORBUT, Timoty , ZHOU, Dan , DU, Zhenjian , CHEN, Shoujun , TATSUTA, Noriaki , LIANG, Guiqing , ONO, Mitsunori
发明人： KOYA, Keizo , SUN, Lijun , WU, Yaming , KORBUT, Timoty , ZHOU, Dan , DU, Zhenjian , CHEN, Shoujun , TATSUTA, Noriaki , LIANG, Guiqing , ONO, Mitsunori
IPC分类号： A61K31/165
CPC分类号： A61K31/165 , A61K31/16 , A61K31/277
摘要： One embodiment of the present invention is a method of treating a subject with a multi-drug resistant cancer. The method comprises administering to the subject an effective amount of a compound represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group, or, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. R 1 -R 4 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R 1 and R 3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R 2 and R 4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Preferably R 1 and R 2 are the same and R 3 and R 4 are the same. R 5 -R 6 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. Z is =O or =S.
摘要翻译：本发明的一个实施方案是用多药耐药性癌症治疗受试者的方法。该方法包括向受试者施用有效量的由结构式（I）表示的化合物：Y是共价键或取代或未取代的直链烃基，或Y与两个> C = Z基团一起连接至其是键合的，是取代或未取代的芳基。 R 1 -R 4独立地为-H，脂族基团，取代的脂族基团，芳基或取代的芳基，或者R 1和R 3与它们所键合的碳原子和氮原子一起，和/或R 2和R 4 与它们所键合的碳原子和氮原子一起形成任选地与芳环稠合的非芳族杂环。优选地，R 1和R 2相同，并且R 3和R 4相同。 R5-R6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 Z = 0或= S。

8. 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。

9. 发明申请

WO2009038775A1 SUBSTITUTED BENZOIMIDAZOLYL-PYRAZINE COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES 审中-公开
标题翻译：用于炎症和免疫相关用途的替代苯甲酰甲霜灵 - 吡嗪化合物
公开(公告)号：WO2009038775A1
公开(公告)日：2009-03-26
申请号：PCT/US2008/010920
申请日：2008-09-19
申请人： SYNTA PHARMACEUTICALS CORP. , CHEN, Shoujun , JIANG, Jun , ZHANG, Junyi , SUN, Lijun
发明人： CHEN, Shoujun , JIANG, Jun , ZHANG, Junyi , SUN, Lijun
IPC分类号： A01N43/50 , A61K31/415
CPC分类号： C07D403/04 , C07D413/14
摘要： This invention relates to certain biologically active chemical compounds, namely benzoimidazolyl-pyrazine derivatives or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
摘要翻译：本发明涉及某些生物活性化合物，即苯并咪唑基 - 吡嗪衍生物或其药学上可接受的盐，溶剂合物，包合物或前药。这些化合物可用作免疫抑制剂并用于治疗和预防炎性病症，过敏性疾病和免疫疾病。

10. 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。

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