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21. 发明申请

WO2005099824A1 1-GLYOXYLAMIDE INDOLIZINES FOR TREATING LUNG AND OVARIAN CANCER 审中-公开
标题翻译： 1-GLYOXYLAMIDE INDOLIZINES FOR TRANTING LUNG AND OVARIAN CANCER
公开(公告)号：WO2005099824A1
公开(公告)日：2005-10-27
申请号：PCT/US2005/009519
申请日：2005-03-22
申请人： SYNTHA PHARMACEUTICALS, CORP. , LI, Hao , KOYA, Keizo , SUN, Lijun , ONO, Mitsunori
发明人： LI, Hao , KOYA, Keizo , SUN, Lijun , ONO, Mitsunori
IPC分类号： A61P35/00
CPC分类号： A61K31/437 , A61K31/4745
摘要： A method of treating a subject having lung cancer or ovarian cancer, comprising administering to the subject an effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt, solvate, or polymorph thereof: Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z 1 and Z 2 are independently=O, =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 )-, -O-, -S-, -S(O)-, -S(O) 2 -, -C(=O)-, -C(=O)-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：一种治疗患有肺癌或卵巢癌的受试者的方法，其包括向所述受试者施用有效量的由结构式（I）表示的化合物或其药学上可接受的盐，溶剂化物或多晶型物：环A是取代或未取代的，任选地与芳基稠合。 Z 1和Z 2独立地为= O，= S，= N-OR 12或= NR 12，R 1和R 2独立地为-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基团，芳基或取代的芳基，条件是R1和R2不同时为-H。或者，-NR 1 R 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。 R3是取代或未取代的芳基或取代或未取代的脂族基团。 X是共价键，-C（R4R5） - ， - N（R4） - ， - O - ， - S - ， - S（O） - ， - S（O），-C（= O）-N（R 4） - 或-N（R 4）-C（= O） - 。 R 4和R 5独立地为-H或取代或未取代的脂族基团。 R 12是-H或取代或未取代的烷基。

22. 发明申请

WO2005000404A3 HETEROCYCLIC COMPOUNDS FOR PREVENTING AND TREATING DISORDERS ASSOCIATED WITH EXCESSIVE BONE LOSS 审中-公开
标题翻译：用于预防和治疗与过量骨质流失相关的病症的杂环化合物
公开(公告)号：WO2005000404A3
公开(公告)日：2005-09-15
申请号：PCT/US2004017064
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： A61K31/5375 , A61P20060101 , A61P1/00 , C07D239/48 , C07D251/18 , C07D251/52 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D473/16
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 R1, R2, R3, R4, R5, 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“）的嘧啶化合物：式（I）及其药学上可接受的盐，溶剂合物，包合物和前药，其中R 1，R 2， 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量骨损失相关的病症，包括但不限于牙周病，非恶性骨病（例如骨质疏松症，骨佩吉特病，成骨不全，纤维发育不良和原发性甲状旁腺功能亢进症），雌激素缺乏症，炎性骨丢失，骨恶性肿瘤，关节炎，石骨症和某些癌症相关病症（例如恶性肿瘤（HCM）高钙血症，多发性骨髓瘤的溶骨性骨病变和乳腺癌和其他转移性癌症的溶骨性骨转移）。

23. 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）。

24. 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。

25. 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）。}}

26. 发明申请

WO2009123704A2 PROCESS FOR PREPARING BIS(THIOHYDRAZIDE AMIDES) 审中-公开
标题翻译：制备BIS（硫代肼酰胺）的方法
公开(公告)号：WO2009123704A2
公开(公告)日：2009-10-08
申请号：PCT/US2009/001996
申请日：2009-03-31
申请人： SYNTA PHARMACEUTICALS CORP. , CHEN, Shoujun , JIANG, Jun , SUN, Lijun , KOYA, Keizo
发明人： CHEN, Shoujun , JIANG, Jun , SUN, Lijun , KOYA, Keizo
IPC分类号： C07C327/56 , C07D213/86 , C07D213/87
CPC分类号： C07C327/56 , C07C2601/02 , C07D213/86 , C07D213/87
摘要： Disclosed herein are methods of preparing a bis(thio-hydrazide amides) compounds of the following structural formula: wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 13 are defined herein.
摘要翻译：本文公开了制备以下结构式的双（硫代酰肼酰胺）化合物的方法：其中R 1，R 2，R 4， R 3，R 4，R 5，R 6和R 13是在此定义。

27. 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。

28. 发明申请

WO2008024303A3 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：WO2008024303A3
公开(公告)日：2008-11-27
申请号：PCT/US2007018378
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 , C07C243/28 , C07C255/42 , C07C257/20 , C07C261/04 , C07C307/04 , C07C311/49 , C07C337/06 , C07D207/34 , C07D263/48 , C07D271/10 , C07D307/38 , C07F9/02
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 of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variabables are as defined in the claims, 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），（III），（IV），（VII），（X），（XI），（XII），（XIII）和（XIV）的化合物，其中可变量如权利要求以及使用本发明化合物治疗患有增殖性疾病（例如癌症）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。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。

29. 发明申请

WO2008024301A3 BIS(THIOHYDRAZIDE AMIDES) FOR USE IN PREVENTING OR DELAYING THE RECURRENCE OF MELANOMA 审中-公开
标题翻译： BIS（THIOHYDRAZIDE AMIDES）用于防止或延迟梅毒的恢复
公开(公告)号：WO2008024301A3
公开(公告)日：2008-07-10
申请号：PCT/US2007018357
申请日：2007-08-20
申请人： SYNTA PHARMACEUTICALS CORP , WILLIAMS MARTIN , MCLEOD MATTHEW , KOYA KEIZO
发明人： WILLIAMS MARTIN , MCLEOD MATTHEW , KOYA KEIZO
IPC分类号： A61K31/16 , A61K31/337 , A61P35/00 , A61P35/04
CPC分类号： A61K31/16 , A61K31/337 , A61K2300/00
摘要： Disclosed herein are methods of preventing or delaying the recurrence of melanoma in a subject with bis(thio-hydrazide amides) represented by a formula selected from Structural Formulas (I)-(IX) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these bis(thio-hydrazide amides) and compositions comprising these bis(thiohydrazide)amides and one or more anti cancer agent.
摘要翻译：本文公开的是用选自结构式（I） - （IX）或其药学上可接受的盐的式（II）表示的双（硫代酰肼）酰胺）来预防或延迟受试者黑素瘤复发的方法，包含这些双硫代酰肼）和包含这些双（硫代酰肼）酰胺和一种或多种抗癌剂的组合物。

30. 发明申请

WO2008024302A8 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：WO2008024302A8
公开(公告)日：2008-05-08
申请号：PCT/US2007018362
申请日：2007-08-20
申请人： SYNTA PHARMACEUTICALS CORP , SUN LIJUN , KOYA KEIZO , CHEN SHOUJUN , DEMKO ZACHARY , XIA ZHI-QIANG
发明人： SUN LIJUN , KOYA KEIZO , CHEN SHOUJUN , DEMKO ZACHARY , XIA ZHI-QIANG
IPC分类号： C07D213/86 , A61K31/16 , A61K31/165 , C07C243/24 , C07C327/00 , C07D207/416 , C07D231/08 , C07D237/04 , C07D277/50 , C07D303/48 , C07D307/66 , C07D307/68 , C07D309/30 , C07D333/36 , C07D333/38
CPC分类号： C07C327/56 , C07C243/24 , C07C255/56 , C07C255/58 , C07C337/02 , C07C337/06 , C07C2601/02 , C07C2601/14 , C07D207/34 , C07D213/81 , C07D213/86 , C07D231/08 , C07D237/04 , C07D277/50 , C07D303/48 , C07D307/66 , C07D307/68 , C07D309/38 , C07D333/36 , C07D333/38
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，以及用于治疗响应于Hsp70诱导和/或自然杀伤诱导的病症的方法。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。

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