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1. 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.

2. 发明申请

WO2003006428A1 TAXOL ENHANCER COMPOUNDS 审中-公开
标题翻译： TAXOL增强剂化合物
公开(公告)号：WO2003006428A1
公开(公告)日：2003-01-23
申请号：PCT/US2002/021714
申请日：2002-07-10
申请人： SBR PHARMACEUTICALS CORP. , KOYA, Keizo , SUN, Lijun , CHEN, Shoujun , TATSUTA, Noriaki , WU, Yaming , ONO, Mitsunori , XIA, Zhi-Qiang
发明人： KOYA, Keizo , SUN, Lijun , CHEN, Shoujun , TATSUTA, Noriaki , WU, Yaming , ONO, Mitsunori , XIA, Zhi-Qiang
IPC分类号： C07C327/56
CPC分类号： C07D307/68 , A45D2008/006 , A61K31/337 , A61K31/505 , A61K31/53 , A61K31/5377 , A61K47/58 , C07C327/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D209/44 , C07D213/83 , C07D261/18 , C07D333/38 , C07D333/68
摘要： One embodiment of the present invention is a compound represented by Structural Formula (I) wherein Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or -C(R 7 R 8 )-. R 1 is an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, or a substituted non-aromatic hetereocyclic group, R 2 -R 4 are independently -H, an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, a substituted non-aromatic hetereocyclic 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. R 5 -R 6 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R 7 and R 8 are each independently -H, an aliphatic or substituted aliphatic group, or R 7 is -H and R 8 is a substituted or unsubstituted aryl group, or, R 7 and R 8 , taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is =0 or =S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.
摘要翻译：本发明的一个实施方案是由结构式（I）表示的化合物，其中Y是取代或未取代的直链烃基的共价键。此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。优选Y为共价键或-C（R 7 R 8） - 。 R1是脂肪族基团，取代脂肪族基团，非芳香族杂环基团或取代的非芳香族杂环基团，R2-R4独立地是-H，脂肪族基团，取代的脂肪族基团，非芳香族的杂环基团，取代的非芳香族杂环基团，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与碳和氮原子一起形成与芳环稠合的非芳族杂环。 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。 R 7和R 8各自独立地为-H，脂族或取代的脂族基团，或者R 7为-H且R 8为取代或未取代的芳基，或者R 7和R 8一起为C 2 -C 6取代或未取代的亚烷基。 Z = 0或= S。还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。

3. 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）。}}

4. 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。

5. 发明申请

WO2006065842A2 5,6,7,8-TETRAHYDROQUINOLINES AND RELATED COMPOUNDS AND USES THEREOF 审中-公开
标题翻译： 5,6,7,8-四氢喹啉和相关化合物及其用途
公开(公告)号：WO2006065842A2
公开(公告)日：2006-06-22
申请号：PCT/US2005/045136
申请日：2005-12-13
申请人： SYNTA PHARMACEUTICALS CORP. , BORELLA, Christopher , FOLEY, Kevin , SUN, Lijun , CHIMMANAMADA, Dinesh, U. , LI, Hao , XIA, Zhi-Qiang , VO, Nha, Huu , BOHNERT, Gary , CHEN, Shoujun , WU, Yaming
发明人： BORELLA, Christopher , FOLEY, Kevin , SUN, Lijun , CHIMMANAMADA, Dinesh, U. , LI, Hao , XIA, Zhi-Qiang , VO, Nha, Huu , BOHNERT, Gary , CHEN, Shoujun , WU, Yaming
CPC分类号： C07D215/38 , C07D215/20 , C07D215/24 , C07D215/54 , C07D219/06 , C07D221/20 , C07D401/04 , C07D401/06 , C07D405/04 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D491/04
摘要： This invention relates to substituted 5,6,7,8-tetrahydroquinoline compounds, substituted dihydropyridine compounds, and substituted tricyclic compounds. The invention also relates to methods of preventing or treating metabolic disorders, such as diabetes mellitus, and conditions and complications associated with diabetes mellitus, comprising administering to a subject in need thereof a compound of the invention or a composition comprising such a compound. The invention further relates to methods of treating inflammatory bowel disease, comprising administering to a subject in need thereof a compound of the invention or a composition comprising such a compound.
摘要翻译：本发明涉及取代的5,6,7,8-四氢喹啉化合物，取代的二氢吡啶化合物和取代的三环化合物。本发明还涉及预防或治疗诸如糖尿病的代谢疾病以及与糖尿病相关的病症和并发症的方法，其包括向有需要的受试者施用本发明的化合物或包含这种化合物的组合物。本发明进一步涉及治疗炎症性肠病的方法，包括向有需要的受试者施用本发明化合物或包含这种化合物的组合物。

6. 发明申请

WO2003006430A1 TAXOL ENHANCER COMPOUNDS 审中-公开
标题翻译： TAXOL增强剂化合物
公开(公告)号：WO2003006430A1
公开(公告)日：2003-01-23
申请号：PCT/US2002/021717
申请日：2002-07-10
申请人： SBR PHARMACEUTICALS CORP. , KOYA, Keizo , SUN, Lijun , CHEN, Shoujun , TATSUTA, Noriaki , WU, Yaming , ONO, Mitsunori
发明人： KOYA, Keizo , SUN, Lijun , CHEN, Shoujun , TATSUTA, Noriaki , WU, Yaming , ONO, Mitsunori
IPC分类号： C07C327/56
CPC分类号： A61K47/48176 , A61K31/16 , A61K31/165 , A61K31/277 , A61K31/337 , A61K31/381 , A61K31/44 , A61K31/505 , A61K31/53 , A61K47/58 , C07C327/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D209/44 , C07D213/83 , C07D261/18 , C07D305/14 , C07D307/68 , C07D333/38 , C07D333/68 , C07D407/12
摘要： Disclosed is a compound represented by the Structural Formula (I); Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or -C(R 7 R 8 )-. R 1 and R 2 are independently an aryl group or a substituted aryl group, R 3 and R 4 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R 5 -R 6 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R 7 and R 8 are each independently -H, an aliphatic or substituted aliphatic group, or R 7 is -H and R 8 is a substituted or unsubstituted aryl group, or, R 7 and R 8 , taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is =O or =S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with taxol or an analog of taxol.
摘要翻译：公开了由结构式（I）表示的化合物; Y是共价键，亚苯基或取代或未取代的直链烃基。此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。优选Y为共价键或-C（R 7 R 8） - 。 R 1和R 2独立地是芳基或取代的芳基，R 3和R 4独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 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。 R 7和R 8各自独立地为-H，脂族或取代的脂族基团，或者R 7为-H且R 8为取代或未取代的芳基，或者R 7和R 8一起为C 2 -C 6取代或未取代的亚烷基。 Z = 0或= S。还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。还公开了通过向受试者施用结构式（I）的化合物与紫杉醇或紫杉醇的类似物组合治疗患有癌症的受试者的方法。

7. 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。

8. 发明申请

WO2008033449A2 COMPOUNDS FOR THE TREATMENT OF ANGIOGENESIS 审中-公开
标题翻译：用于治疗血液发生的化合物
公开(公告)号：WO2008033449A2
公开(公告)日：2008-03-20
申请号：PCT/US2007/019905
申请日：2007-09-13
申请人： SYNTA PHARMACEUTICALS CORP. , WU, Yaming , FOLEY, Kevin , BORELLA, Christopher
发明人： WU, Yaming , FOLEY, Kevin , BORELLA, Christopher
IPC分类号： A61K31/675 , A61K31/00 , A61K31/4192 , A61K31/42 , A61K31/422 , A61K31/425 , A61K31/427
CPC分类号： A61K31/00 , A61K31/4192 , A61K31/42 , A61K31/422 , A61K31/425 , A61K31/427 , A61K31/675
摘要： The invention relates to isoxazole, isothiazole, and triazole compounds that are useful for treating or inhibiting angiogenesis.
摘要翻译：本发明涉及可用于治疗或抑制血管发生的异恶唑，异噻唑和三唑化合物。

9. 发明申请

WO2010135914A1 NEW SPIROHETEROCYCLIC FURAN AND THIOFURAN DIONE DERIVATIVES 审中-公开
标题翻译：新的螺旋脂肪和呋喃酮衍生物
公开(公告)号：WO2010135914A1
公开(公告)日：2010-12-02
申请号：PCT/CN2010/000728
申请日：2010-05-21
申请人： SYNGENTA PARTICIPATIONS AG , SCHAETZER, Jürgen, Harry , PITTERNA, Thomas , LU, Long , WU, Yaming , RENOLD, Peter , PERRUCCIO, Francesca , CASSAYRE, Jérome, Yves , MUEGLEBACH, Michel
发明人： SCHAETZER, Jürgen, Harry , PITTERNA, Thomas , LU, Long , WU, Yaming , RENOLD, Peter , PERRUCCIO, Francesca , CASSAYRE, Jérome, Yves , MUEGLEBACH, Michel
IPC分类号： C07D491/107 , C07D495/10 , C07D211/94 , A01N43/42
CPC分类号： C07D491/10 , A01N43/90 , C07D211/94 , C07D495/10
摘要： Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.
摘要翻译：公开了用作农药的式（I）化合物，其中取代基如权利要求1所定义。

10. 发明申请

WO2012092827A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2012092827A1
公开(公告)日：2012-07-12
申请号：PCT/CN2011/085024
申请日：2011-12-30
申请人： SYNGENTA PARTICIPATIONS AG , JEANMART, Stephane André Marie , LU, Long , WU, Yaming , MAO, Lisheng , MUEHLEBACH, Michel
发明人： JEANMART, Stephane André Marie , LU, Long , WU, Yaming , MAO, Lisheng , MUEHLEBACH, Michel
IPC分类号： C07D207/36 , C07D307/12 , C07D317/34 , C07D401/12 , C07D405/12 , C07D409/12 , A01N43/36
CPC分类号： C07D401/06 , A01N43/16 , A01N43/36 , A01N43/40 , A01N47/06 , A01N47/40 , C07D211/26 , C07D211/34 , C07D211/94 , C07D309/06 , C07D335/02 , C07D403/06 , C07D405/06 , C07D407/06 , C07D409/06
摘要： Disclosed are cyclic dione derivatives represented by formula (I), wherein the substituents are as defined in the description. The preparation method, intermediate and use thereof are also provided.
摘要翻译：公开了由式（I）表示的环状二酮衍生物，其中取代基如说明书中所定义。还提供了其制备方法，中间体和用途。

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