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1. 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。

2. 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.

3. 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。

4. 发明申请

WO2008033494A3 PURIFICATION OF BIS(THIOHYDRAZIDE AMIDES) 审中-公开
公开(公告)号：WO2008033494A3
公开(公告)日：2008-03-20
申请号：PCT/US2007/019987
申请日：2007-09-14
申请人： SYNTA PHARMACEUTICALS CORP. , CHEN, Shoujun , XIA, Zhi-Qiang , KOSTIK, Elena , KOYA, Keizo , SUN, Lijun
发明人： CHEN, Shoujun , XIA, Zhi-Qiang , KOSTIK, Elena , KOYA, Keizo , SUN, Lijun
IPC分类号： C07C327/56
摘要： Disclosed herein is a method for the purification of bis(thiohydrazide amide) compounds of formula I, wherein R 1 , R 2 , R 3 , R 4 , R 7 , R 8 , Z and Y are defined herein, by dissolving the compound in a solvent selected from the group consisting of tetrahydrofuran-acetone, tetrahydrofuran-acetonitrile, tetrahydrofuran, acetone, acetonitrile, tetrahydrofuran-ethanol and acetone-ethanol and precipitating the compound with water.

5. 发明申请

WO2006009940A1 BIS(THIO-HYDRAZIDE AMIDE) SALTS FOR TREATMENT OF CANCERS 审中-公开
标题翻译： BIS（THIO-HYDRAZIDE AMIDE）用于治疗癌症的药物
公开(公告)号：WO2006009940A1
公开(公告)日：2006-01-26
申请号：PCT/US2005/021642
申请日：2005-06-20
申请人： SYNTA PHARMACEUTICALS CORP. , KOSTIK, Elena , VAGHEFI, Farid , LIANG, Guiqing , KOYA, Keizo , SUN, Lijun , TATSUTA, Noriaki , CHEN, Shoujun , INOUE, Takayo , XIA, Zhi-Qiang
发明人： KOSTIK, Elena , VAGHEFI, Farid , LIANG, Guiqing , KOYA, Keizo , SUN, Lijun , TATSUTA, Noriaki , CHEN, Shoujun , INOUE, Takayo , XIA, Zhi-Qiang
IPC分类号： C07C327/56
CPC分类号： C07D305/14 , C07C327/56 , C07C2601/02
摘要： Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I) Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl 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. Z is -O or -S. M + is a pharmaceutically acceptable monovalent cation and M 2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.
摘要翻译：公开了由结构式（I）表示的双（硫代酰肼酰胺）二盐，Y是共价键或取代或未取代的直链烃基。 [R <子

6. 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）。}}

7. 发明申请

WO2004054507A2 INDOLIZINE COMPOUNDS 审中-公开
标题翻译：吲哚化合物
公开(公告)号：WO2004054507A2
公开(公告)日：2004-07-01
申请号：PCT/US2003/039303
申请日：2003-12-10
申请人： SYNTA PHARMACEUTICALS CORP. , ONO, Mitsunori , PRZEWLOKA, Teresa , JAMES, David , CHIMMANAMADA, Dinesh , LU, Rongzhen , NAGAI, Masazumi , KOYA, Keizo , SUN, Lijun
发明人： ONO, Mitsunori , PRZEWLOKA, Teresa , JAMES, David , CHIMMANAMADA, Dinesh , LU, Rongzhen , NAGAI, Masazumi , KOYA, Keizo , SUN, Lijun
IPC分类号： A61K
CPC分类号： C07D471/04
摘要： This invention relates to compounds of Formula (I) wherein Ring A, X, Y, Z, R 1 , R 2 and R 3 are defined herein. These compounds are useful for treating and preventing cancer, inflammatory disorders, autoimmune diseases and other conditions involving PDE4 or elevated levels of cytokines. This invention also relates to pharmaceutical compositions comprising at least one compound of Formula (I) and methods for treating and preventing cancer, inflammatory disorders, autoimmune diseases and other conditions involving PDE4 or elevated levels of cytokines.
摘要翻译：本发明涉及式（I）的化合物，其中环A，X，Y，Z，R 1，R 2和R 3在本文中定义。这些化合物可用于治疗和预防癌症，炎性疾病，自身免疫性疾病和其他涉及PDE4的病症或升高的细胞因子水平。本发明还涉及包含至少一种式（I）化合物和用于治疗和预防癌症，炎症性疾病，自身免疫性疾病和涉及PDE4或升高的细胞因子水平的其它病症的方法的药物组合物。

8. 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。

9. 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）。

10. 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。

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