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公开(公告)号:US08642576B2
公开(公告)日:2014-02-04
申请号:US13597364
申请日:2012-08-29
申请人: Mark E. Salvati , Heather Finlay , Bang-Chi Chen , Lalgudi S. Harikrishnan , Ji Jiang , James A. Johnson , Muthoni G. Kamau , R. Michael Lawrence , Jianqing Li , John Lloyd , Michael M. Miller , Zulan Pi , Jennifer X. Qiao , Richard A. Rampulla , Jacques Y. Roberge , Tammy C. Wang , Yufeng Wang , Wu Yang
发明人: Mark E. Salvati , Heather Finlay , Bang-Chi Chen , Lalgudi S. Harikrishnan , Ji Jiang , James A. Johnson , Muthoni G. Kamau , R. Michael Lawrence , Jianqing Li , John Lloyd , Michael M. Miller , Zulan Pi , Jennifer X. Qiao , Richard A. Rampulla , Jacques Y. Roberge , Tammy C. Wang , Yufeng Wang , Wu Yang
IPC分类号: A61K31/166 , A61K31/137 , A61K31/426 , A61K31/4468 , A61K31/505 , A61K31/695 , A61K31/5375 , A61K31/17 , C07C275/26 , C07C233/73 , C07C37/02 , C07C41/01
CPC分类号: C07C275/26 , C07C211/29 , C07C215/08 , C07C217/58 , C07C229/36 , C07C229/38 , C07C233/09 , C07C233/13 , C07C233/18 , C07C233/56 , C07C233/60 , C07C233/66 , C07C233/73 , C07C233/78 , C07C235/20 , C07C235/34 , C07C235/48 , C07C235/74 , C07C237/06 , C07C237/08 , C07C251/38 , C07C255/13 , C07C255/57 , C07C255/60 , C07C271/16 , C07C271/20 , C07C271/44 , C07C275/24 , C07C311/04 , C07C311/17 , C07C317/44 , C07C323/57 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/08 , C07D207/10 , C07D207/16 , C07D207/26 , C07D207/273 , C07D207/325 , C07D207/38 , C07D209/18 , C07D209/20 , C07D209/42 , C07D209/48 , C07D211/38 , C07D211/58 , C07D213/38 , C07D213/40 , C07D213/82 , C07D231/14 , C07D231/40 , C07D239/26 , C07D249/04 , C07D249/06 , C07D249/08 , C07D249/14 , C07D257/04 , C07D257/06 , C07D261/04 , C07D261/08 , C07D261/14 , C07D261/18 , C07D263/34 , C07D271/06 , C07D271/10 , C07D271/113 , C07D277/48 , C07D277/58 , C07D277/60 , C07D285/06 , C07D285/135 , C07D295/155 , C07D303/48 , C07D307/22 , C07D307/24 , C07D307/33 , C07D307/68 , C07D307/79 , C07D307/85 , C07D311/58 , C07D317/46 , C07D319/20 , C07D333/20 , C07D333/24 , C07D333/38 , C07D333/68 , C07D333/70 , C07D471/04 , C07F7/081
摘要: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
摘要翻译: 其中A,B,C和R 1的化合物在此描述。
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公开(公告)号:US20120322761A1
公开(公告)日:2012-12-20
申请号:US13597364
申请日:2012-08-29
申请人: Mark E. Salvati , Heather Finlay , Bang-Chi Chen , Lalgudi S. Harikrishnan , Ji Jiang , James A. Johnson , Muthoni G. Kamau , R. Michael Lawrence , Jianqing Li , John Lloyd , Michael M. Miller , Zulan Pi , Jennifer X. Qiao , Richard A. Rampulla , Jacques Y. Roberge , Tammy C. Wang , Yufeng Wang , Wu Yang
发明人: Mark E. Salvati , Heather Finlay , Bang-Chi Chen , Lalgudi S. Harikrishnan , Ji Jiang , James A. Johnson , Muthoni G. Kamau , R. Michael Lawrence , Jianqing Li , John Lloyd , Michael M. Miller , Zulan Pi , Jennifer X. Qiao , Richard A. Rampulla , Jacques Y. Roberge , Tammy C. Wang , Yufeng Wang , Wu Yang
IPC分类号: C07C275/26 , C07C233/73 , C07C37/02 , C07C41/01 , C07C215/08 , A61K31/166 , A61K31/137 , C07D277/48 , A61K31/426 , C07D211/58 , A61K31/4468 , C07D239/26 , A61K31/505 , C07C41/24 , C07F7/10 , A61K31/695 , C07D295/135 , A61K31/5375 , C07D207/10 , A61K31/40 , A61P25/28 , A61P9/10 , A61P7/02 , A61P9/00 , A61P3/06 , A61P3/00 , A61P9/12 , A61K31/17
CPC分类号: C07C275/26 , C07C211/29 , C07C215/08 , C07C217/58 , C07C229/36 , C07C229/38 , C07C233/09 , C07C233/13 , C07C233/18 , C07C233/56 , C07C233/60 , C07C233/66 , C07C233/73 , C07C233/78 , C07C235/20 , C07C235/34 , C07C235/48 , C07C235/74 , C07C237/06 , C07C237/08 , C07C251/38 , C07C255/13 , C07C255/57 , C07C255/60 , C07C271/16 , C07C271/20 , C07C271/44 , C07C275/24 , C07C311/04 , C07C311/17 , C07C317/44 , C07C323/57 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/08 , C07D207/10 , C07D207/16 , C07D207/26 , C07D207/273 , C07D207/325 , C07D207/38 , C07D209/18 , C07D209/20 , C07D209/42 , C07D209/48 , C07D211/38 , C07D211/58 , C07D213/38 , C07D213/40 , C07D213/82 , C07D231/14 , C07D231/40 , C07D239/26 , C07D249/04 , C07D249/06 , C07D249/08 , C07D249/14 , C07D257/04 , C07D257/06 , C07D261/04 , C07D261/08 , C07D261/14 , C07D261/18 , C07D263/34 , C07D271/06 , C07D271/10 , C07D271/113 , C07D277/48 , C07D277/58 , C07D277/60 , C07D285/06 , C07D285/135 , C07D295/155 , C07D303/48 , C07D307/22 , C07D307/24 , C07D307/33 , C07D307/68 , C07D307/79 , C07D307/85 , C07D311/58 , C07D317/46 , C07D319/20 , C07D333/20 , C07D333/24 , C07D333/38 , C07D333/68 , C07D333/70 , C07D471/04 , C07F7/081
摘要: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
摘要翻译: 其中A,B,C和R 1的化合物在此描述。
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3.Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function 有权
标题翻译: 稠合的杂环琥珀酰亚胺化合物及其类似物,核激素受体功能的调节剂公开(公告)号:US07655689B2
公开(公告)日:2010-02-02
申请号:US11338587
申请日:2006-03-20
申请人: Mark E. Salvati , James Aaron Balog , Dacia A. Pickering , Sören Giese , Aberra Fura , Wenying Li , Ramesh N. Patel , Ronald L. Hanson , Toomas Mitt , Jacques Y. Roberge , James R. Corte , Steven H. Spergel , Richard A. Rampulla , Raj N. Misra , Hai-Yun Xiao
发明人: Mark E. Salvati , James Aaron Balog , Dacia A. Pickering , Sören Giese , Aberra Fura , Wenying Li , Ramesh N. Patel , Ronald L. Hanson , Toomas Mitt , Jacques Y. Roberge , James R. Corte , Steven H. Spergel , Richard A. Rampulla , Raj N. Misra , Hai-Yun Xiao
IPC分类号: C07D209/00 , A01N43/38
CPC分类号: C07D487/18
摘要: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
摘要翻译: 稠合的环状化合物,使用这些化合物治疗核激素受体相关病症如癌症和免疫疾病的方法,以及含有这些化合物的药物组合物。
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4.Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function 失效
标题翻译: 稠合的杂环琥珀酰亚胺化合物及其类似物,核激素受体功能的调节剂公开(公告)号:US07517904B2
公开(公告)日:2009-04-14
申请号:US11176810
申请日:2005-07-07
申请人: Mark E. Salvati , James Aaron Balog , Dacia A. Pickering , Sören Giese , Aberra Fura , Wenying Li , Ramesh N. Patel , Ronald L. Hanson , Toomas Mitt , Jacques Y. Roberge , James R. Corte , Steven H. Spergel , Richard A. Rampulla , Raj N. Misra , Hai-Yun Xiao
发明人: Mark E. Salvati , James Aaron Balog , Dacia A. Pickering , Sören Giese , Aberra Fura , Wenying Li , Ramesh N. Patel , Ronald L. Hanson , Toomas Mitt , Jacques Y. Roberge , James R. Corte , Steven H. Spergel , Richard A. Rampulla , Raj N. Misra , Hai-Yun Xiao
IPC分类号: A61K31/407 , A61K31/34 , C07D491/08
CPC分类号: C07D487/18 , A61K31/00 , A61K31/403 , A61K31/407 , A61K31/655 , A61K31/675 , A61K45/06 , C07B2200/11 , C07D401/08 , C07D471/08 , C07D487/08 , C07D491/08 , C07D491/18 , C07D491/22 , C07D495/08 , C07D495/18 , C07D519/00 , C40B40/00 , A61K2300/00
摘要: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
摘要翻译: 稠合的环状化合物,使用这些化合物治疗核激素受体相关病症如癌症和免疫疾病的方法,以及含有这些化合物的药物组合物。
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5.Alkylene bridged sultam compounds useful as modulators of nuclear hormone receptor function 有权
标题翻译: 可用作核激素受体功能的调节剂的亚烷基桥连的苏丹化合物公开(公告)号:US07468439B2
公开(公告)日:2008-12-23
申请号:US11850070
申请日:2007-09-05
申请人: Weifang Shan , James Aaron Balog , Andrew James Nation , Ashvinikumar V. Gavai , Wen-Ching Han , Mark E. Salvati
发明人: Weifang Shan , James Aaron Balog , Andrew James Nation , Ashvinikumar V. Gavai , Wen-Ching Han , Mark E. Salvati
IPC分类号: C07D275/04 , A61K31/425
CPC分类号: C07D275/06
摘要: Disclosed are sultam compounds of Formula (I) or a pharmaceutically-acceptable salt thereof. Also disclosed are methods of using such compounds in the treatment of at least one nuclear hormone receptor-associated condition, such as, for example, cancer and immune disorders, and at least one pharmaceutical composition comprising such compounds.
摘要翻译: 公开了式(I)的磺胺化合物或其药学上可接受的盐。 还公开了使用这些化合物治疗至少一种核激素受体相关病症例如癌症和免疫病症的方法,以及至少一种包含这些化合物的药物组合物。
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6.
公开(公告)号:US07087636B2
公开(公告)日:2006-08-08
申请号:US10322276
申请日:2002-12-18
IPC分类号: A61K31/40 , C07D487/02
CPC分类号: C07D209/74 , C07D209/76 , C07D231/54 , C07D275/06
摘要: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
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公开(公告)号:US06992102B2
公开(公告)日:2006-01-31
申请号:US10685020
申请日:2003-10-14
申请人: Lawrence Hamann , David Augeri , Chongqing Sun , Jeffrey A. Robl , Mark E. Salvati , Tammy Wang
发明人: Lawrence Hamann , David Augeri , Chongqing Sun , Jeffrey A. Robl , Mark E. Salvati , Tammy Wang
IPC分类号: A61K31/40 , C07D207/00
CPC分类号: C07D207/16 , C07D471/04 , C07D487/04 , C07D513/04
摘要: The invention provides compounds of the formula I wherein the substitutents are as described herein.Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia, and also provided are pharmaceutical compositions containing such compounds.
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8.
公开(公告)号:US06897321B2
公开(公告)日:2005-05-24
申请号:US10639272
申请日:2003-08-12
申请人: Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xia , Rulin Zhao
发明人: Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xia , Rulin Zhao
IPC分类号: C07D487/18 , A61K20060101 , A61K31/427 , A61K31/454 , A61P20060101 , C07D20060101 , C07D263/32 , C07D417/12 , C07D417/14 , C07D521/00 , C07D263/30
CPC分类号: C07D417/12 , A61K31/427 , A61K31/454 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/14
摘要: The present invention relates to new, efficient processes for the preparation of 5-(-2-oxyazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9, R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.
摘要翻译: 本发明涉及制备式I的5-( - 2-氧杂唑基烷硫基)-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的,有效的方法,其中:R是烷基,芳基或杂芳基; R 1,R 2,R 3,R 4和R 5均为 各自独立地为氢,烷基,芳基或杂芳基; R 6和R 7各自独立地为氢,烷基,芳基,杂芳基,卤素,羟基或烷氧基; R 8是氢,烷基,芳基,杂芳基,CONR 9,R 10,COR 11或COOR, SUP> 12 SUP> R 9,R 10,R 11和R 12各自独立地为氢,烷基或芳基; m等于0到5; 且n等于0至5,这是细胞周期蛋白依赖性激酶(cdks)的新型有效抑制剂。 本发明还涉及新的关键中间体化合物,式III'的季铵盐和式IX的2-恶唑基烷基衍生物。
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公开(公告)号:US08304403B2
公开(公告)日:2012-11-06
申请号:US12797760
申请日:2010-06-10
申请人: Mark E. Salvati , Heather Finlay , Bang-Chi Chen , Lalgudi S. Harikrishnan , Ji Jiang , James A. Johnson , Muthoni G. Kamau , R. Michael Lawrence , Jianqing Li , John Lloyd , Michael M. Miller , Zulan Pi , Jennifer X. Qiao , Richard A. Rampulla , Jacques Y. Roberge , Tammy C. Wang , Yufeng Wang , Wu Yang
发明人: Mark E. Salvati , Heather Finlay , Bang-Chi Chen , Lalgudi S. Harikrishnan , Ji Jiang , James A. Johnson , Muthoni G. Kamau , R. Michael Lawrence , Jianqing Li , John Lloyd , Michael M. Miller , Zulan Pi , Jennifer X. Qiao , Richard A. Rampulla , Jacques Y. Roberge , Tammy C. Wang , Yufeng Wang , Wu Yang
IPC分类号: A61K31/695 , A61K31/17 , A61K31/165 , A61K31/426 , A61K31/4468 , A61K31/50 , A61K31/535 , C07C273/00 , C07D277/20 , C07D211/98 , C07D239/02 , C07D205/08
CPC分类号: C07C275/26 , C07C211/29 , C07C215/08 , C07C217/58 , C07C229/36 , C07C229/38 , C07C233/09 , C07C233/13 , C07C233/18 , C07C233/56 , C07C233/60 , C07C233/66 , C07C233/73 , C07C233/78 , C07C235/20 , C07C235/34 , C07C235/48 , C07C235/74 , C07C237/06 , C07C237/08 , C07C251/38 , C07C255/13 , C07C255/57 , C07C255/60 , C07C271/16 , C07C271/20 , C07C271/44 , C07C275/24 , C07C311/04 , C07C311/17 , C07C317/44 , C07C323/57 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/08 , C07D207/10 , C07D207/16 , C07D207/26 , C07D207/273 , C07D207/325 , C07D207/38 , C07D209/18 , C07D209/20 , C07D209/42 , C07D209/48 , C07D211/38 , C07D211/58 , C07D213/38 , C07D213/40 , C07D213/82 , C07D231/14 , C07D231/40 , C07D239/26 , C07D249/04 , C07D249/06 , C07D249/08 , C07D249/14 , C07D257/04 , C07D257/06 , C07D261/04 , C07D261/08 , C07D261/14 , C07D261/18 , C07D263/34 , C07D271/06 , C07D271/10 , C07D271/113 , C07D277/48 , C07D277/58 , C07D277/60 , C07D285/06 , C07D285/135 , C07D295/155 , C07D303/48 , C07D307/22 , C07D307/24 , C07D307/33 , C07D307/68 , C07D307/79 , C07D307/85 , C07D311/58 , C07D317/46 , C07D319/20 , C07D333/20 , C07D333/24 , C07D333/38 , C07D333/68 , C07D333/70 , C07D471/04 , C07F7/081
摘要: Compounds of formula Ia and Ib and wherein A, B, C and R1 are described herein.
摘要翻译: 式Ia和Ib化合物,其中A,B,C和R 1在本文中描述。
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公开(公告)号:US07888376B2
公开(公告)日:2011-02-15
申请号:US11559930
申请日:2006-11-15
申请人: Mark E. Salvati , Heather Finlay , Lalgudi S. Harikrishnan , Ji Jiang , James A. Johnson , Muthoni G. Kamau , R. Michael Lawrence , Michael M. Miller , Jennifer X. Qiao , Tammy C. Wang , Yufeng Wang , Wu Yang
发明人: Mark E. Salvati , Heather Finlay , Lalgudi S. Harikrishnan , Ji Jiang , James A. Johnson , Muthoni G. Kamau , R. Michael Lawrence , Michael M. Miller , Jennifer X. Qiao , Tammy C. Wang , Yufeng Wang , Wu Yang
IPC分类号: C07D213/56 , A61K31/44
CPC分类号: C07D417/06 , C07D213/40 , C07D213/61 , C07D277/28 , C07D401/04 , C07D401/12 , C07D405/06 , C07D405/12 , C07D417/12
摘要: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
摘要翻译: 其中A,B,C和R 1的化合物在此描述。
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