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公开(公告)号:US07504512B2
公开(公告)日:2009-03-17
申请号:US10820097
申请日:2004-04-07
申请人: David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William McClellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
发明人: David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William McClellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
IPC分类号: C07C211/00 , A61K31/445
CPC分类号: C07D207/27 , A61K31/18 , A61K31/4015 , A61K31/44 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C311/51 , C07C323/30 , C07C323/37 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D203/26 , C07D207/06 , C07D209/08 , C07D209/52 , C07D209/54 , C07D211/22 , C07D211/74 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/78 , C07D215/12 , C07D221/20 , C07D231/12 , C07D235/08 , C07D235/26 , C07D239/26 , C07D249/04 , C07D263/32 , C07D263/56 , C07D263/58 , C07D277/56 , C07D277/64 , C07D295/205 , C07D295/26 , C07D317/60 , C07D333/28 , C07D333/56 , C07D333/70 , C07D417/12 , C07D451/02
摘要: N-Benzoyl arylsulfonamides having the formula are BCL-X1 inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-X1 inhibiting compositions and methods of promoting apoptosis in a mammal.
摘要翻译: 具有下式的N-苯甲酰基芳基磺酰胺是BCL-X1抑制剂,可用于促进凋亡。 还公开了BCL-X1抑制组合物和促进哺乳动物细胞凋亡的方法。
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公开(公告)号:US20090137585A1
公开(公告)日:2009-05-28
申请号:US12364987
申请日:2009-02-03
申请人: David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William Mcclellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
发明人: David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William Mcclellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
IPC分类号: A61K31/445 , C07D211/60 , C07D241/04 , A61K31/5375 , A61P35/00 , A61K31/495 , C07D413/02
CPC分类号: C07D207/27 , A61K31/18 , A61K31/4015 , A61K31/44 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C311/51 , C07C323/30 , C07C323/37 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D203/26 , C07D207/06 , C07D209/08 , C07D209/52 , C07D209/54 , C07D211/22 , C07D211/74 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/78 , C07D215/12 , C07D221/20 , C07D231/12 , C07D235/08 , C07D235/26 , C07D239/26 , C07D249/04 , C07D263/32 , C07D263/56 , C07D263/58 , C07D277/56 , C07D277/64 , C07D295/205 , C07D295/26 , C07D317/60 , C07D333/28 , C07D333/56 , C07D333/70 , C07D417/12 , C07D451/02
摘要: N-Benzoyl arylsulfonamides having the formula are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
摘要翻译: 具有下式的N-苯甲酰基芳基磺酰胺是BCL-X1抑制剂,可用于促进凋亡。 还公开了BCL-X1抑制组合物和促进哺乳动物细胞凋亡的方法。
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公开(公告)号:US06720338B2
公开(公告)日:2004-04-13
申请号:US09957276
申请日:2001-09-20
申请人: David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William McClellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
发明人: David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William McClellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
IPC分类号: A61K31445
CPC分类号: C07D207/27 , A61K31/18 , A61K31/4015 , A61K31/44 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C311/51 , C07C323/30 , C07C323/37 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D203/26 , C07D207/06 , C07D209/08 , C07D209/52 , C07D209/54 , C07D211/22 , C07D211/74 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/78 , C07D215/12 , C07D221/20 , C07D231/12 , C07D235/08 , C07D235/26 , C07D239/26 , C07D249/04 , C07D263/32 , C07D263/56 , C07D263/58 , C07D277/56 , C07D277/64 , C07D295/205 , C07D295/26 , C07D317/60 , C07D333/28 , C07D333/56 , C07D333/70 , C07D417/12 , C07D451/02
摘要: N-Benzoyl arylsulfonamides having the formula: are BCL-X1 inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-X1 inhibiting compositions and methods of promoting apoptosis in a mammal.
摘要翻译: 具有下式的N-苯甲酰基芳基磺酰胺是BCL-X1抑制剂,可用于促进细胞凋亡。 还公开了BCL-X1抑制组合物和促进哺乳动物细胞凋亡的方法。
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公开(公告)号:US07754886B2
公开(公告)日:2010-07-13
申请号:US12364987
申请日:2009-02-03
申请人: David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J Hajduk , Aaron R Kunzer , William J. Mcclellan , David D. Nettesheim , Thorsten K. Oost , Andrew M. Petros , Saul Howard Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
发明人: David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J Hajduk , Aaron R Kunzer , William J. Mcclellan , David D. Nettesheim , Thorsten K. Oost , Andrew M. Petros , Saul Howard Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
IPC分类号: C07C211/00 , A61K31/445
CPC分类号: C07D207/27 , A61K31/18 , A61K31/4015 , A61K31/44 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C311/51 , C07C323/30 , C07C323/37 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D203/26 , C07D207/06 , C07D209/08 , C07D209/52 , C07D209/54 , C07D211/22 , C07D211/74 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/78 , C07D215/12 , C07D221/20 , C07D231/12 , C07D235/08 , C07D235/26 , C07D239/26 , C07D249/04 , C07D263/32 , C07D263/56 , C07D263/58 , C07D277/56 , C07D277/64 , C07D295/205 , C07D295/26 , C07D317/60 , C07D333/28 , C07D333/56 , C07D333/70 , C07D417/12 , C07D451/02
摘要: N-Benzoyl arylsulfonamides having the formula are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
摘要翻译: 具有下式的N-苯甲酰基芳基磺酰胺是BCL-X1抑制剂,可用于促进凋亡。 还公开了BCL-X1抑制组合物和促进哺乳动物细胞凋亡的方法。
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公开(公告)号:US08940902B2
公开(公告)日:2015-01-27
申请号:US13554698
申请日:2012-07-20
申请人: R. Scott Bitner , Kaitlin E. Browman , Michael E. Brune , Yixian Chen , Jurgen Dinges , Karla Drescher , Peer Jacobson , Hwan-soo Jae , Ravi Kurukulasuriya , James T. Link , David J. Madar , Jyoti R. Patel , Marina A. Pliushchev , Jeffrey J. Rohde , Lynne E. Rueter , Qi Shuai , Bryan K. Sorensen , Jiahong Wang , Karsten M. Wicke , Martin Winn , Dariusz Wodka , Vince Yeh , Hong Yong
发明人: R. Scott Bitner , Kaitlin E. Browman , Michael E. Brune , Yixian Chen , Jurgen Dinges , Karla Drescher , Peer Jacobson , Hwan-soo Jae , Ravi Kurukulasuriya , James T. Link , David J. Madar , Jyoti R. Patel , Marina A. Pliushchev , Jeffrey J. Rohde , Lynne E. Rueter , Qi Shuai , Bryan K. Sorensen , Jiahong Wang , Karsten M. Wicke , Martin Winn , Dariusz Wodka , Vince Yeh , Hong Yong
IPC分类号: C07D211/74 , A61K31/44 , A61K31/495
CPC分类号: C07D403/12 , A61K31/44 , A61K31/495 , C07D207/267 , C07D401/12 , C07D401/14
摘要: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-β-hydroxysteroid dehydrogenase Type 1 enzyme activity.
摘要翻译: 一种治疗患有与老化和神经变性相关的糖尿病中枢神经系统紊乱和缺陷的患者的方法,包括注意力缺陷障碍,注意力缺陷多动障碍(ADHD),阿尔茨海默病(AD),轻度认知障碍 老年性痴呆,艾滋病痴呆,神经退行性疾病,抑郁症和精神分裂症,包括向需要这种治疗的患者施用有效量的11-羟基类固醇脱氢酶1型酶活性的选择性抑制剂。
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6.Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) 审中-公开
标题翻译: 药物组合物作为二肽基肽酶-IV(DPP-IV)的抑制剂公开(公告)号:US20050215603A1
公开(公告)日:2005-09-29
申请号:US10795622
申请日:2004-03-08
申请人: Irini Akritopoulou-Zanze , Daria Darczak , Jurgen Dinges , Stevan Djuric , Ethan Hoff , Hana Kopecka , Jyoti Patel , Zhonghua Pei , Qi Shuai , Kathy Sarris , Hing Sham , Paul Wiedeman
发明人: Irini Akritopoulou-Zanze , Daria Darczak , Jurgen Dinges , Stevan Djuric , Ethan Hoff , Hana Kopecka , Jyoti Patel , Zhonghua Pei , Qi Shuai , Kathy Sarris , Hing Sham , Paul Wiedeman
IPC分类号: A61K31/427 , C07D405/06 , C07D413/06 , C07D417/02 , C07D417/06
CPC分类号: C07D417/06 , C07D405/06 , C07D413/06
摘要: The present invention relates to compounds of formula (I), which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
摘要翻译: 本发明涉及抑制二肽基肽酶IV(DPP-IV)的式(I)化合物,其可用于预防或治疗糖尿病,特别是II型糖尿病,以及高血糖症,X综合症,高胰岛素血症,肥胖症, 动脉粥样硬化和各种免疫调节疾病。
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公开(公告)号:US20050209249A1
公开(公告)日:2005-09-22
申请号:US11075319
申请日:2005-03-08
申请人: Irini Akritopoulou-Zanze , Daria Darczak , Jurgen Dinges , Stevan Djuric , Ethan Hoff , Hana Kopecka , Jyoti Patel , Zhonghua Pei , Qi Shuai , Kathy Sarris , Hing Sham , Paul Wiedeman
发明人: Irini Akritopoulou-Zanze , Daria Darczak , Jurgen Dinges , Stevan Djuric , Ethan Hoff , Hana Kopecka , Jyoti Patel , Zhonghua Pei , Qi Shuai , Kathy Sarris , Hing Sham , Paul Wiedeman
IPC分类号: A61K31/454 , A61K31/496 , C07D207/09 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/06 , C07D417/14
CPC分类号: C07D417/14 , C07D207/09 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/06
摘要: The present invention relates to compounds of formula (I), which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
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公开(公告)号:US20150065508A1
公开(公告)日:2015-03-05
申请号:US14226615
申请日:2014-03-26
申请人: R. Scott Bitner , Kaitlin E. Browman , Michael E. Brune , Steven Fung , Peer B. Jacobson , Lynne E. Rueter , Marina I. Strakhova , Jiahong Wang , Jyoti R. Patel , Qi Shuai , James T. Link , Jeffrey J. Rohde , Jurgen Dinges , Bryan K. Sorensen , Martin Winn , Hong Yong , Vince S. Yeh
发明人: R. Scott Bitner , Kaitlin E. Browman , Michael E. Brune , Steven Fung , Peer B. Jacobson , Lynne E. Rueter , Marina I. Strakhova , Jiahong Wang , Jyoti R. Patel , Qi Shuai , James T. Link , Jeffrey J. Rohde , Jurgen Dinges , Bryan K. Sorensen , Martin Winn , Hong Yong , Vince S. Yeh
IPC分类号: C07C235/14 , C07C235/22 , C07C271/28 , C07D295/088 , C07D207/48 , C07D257/04 , C07D401/04 , C07D261/08 , C07C237/24 , C07C311/46
CPC分类号: C07C235/14 , A61K31/165 , A61K31/19 , A61K31/4439 , C07C235/22 , C07C237/24 , C07C271/28 , C07C311/46 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D207/48 , C07D257/04 , C07D261/08 , C07D295/088 , C07D401/04
摘要: The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
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9.
公开(公告)号:US08716345B2
公开(公告)日:2014-05-06
申请号:US13530422
申请日:2012-06-22
申请人: R. Scott Bitner , Kaitlin E. Browman , Michael E. Brune , Steven Fung , Peer B. Jacobson , Lynne E. Rueter , Marina I. Strakhova , Jiahong Wang , Jyoti R. Patel , Qi Shuai , James T. Link , Jeffrey J. Rohde , Jurgen Dinges , Bryan K. Sorensen , Martin Winn , Hong Yong , Vince S. Yeh
发明人: R. Scott Bitner , Kaitlin E. Browman , Michael E. Brune , Steven Fung , Peer B. Jacobson , Lynne E. Rueter , Marina I. Strakhova , Jiahong Wang , Jyoti R. Patel , Qi Shuai , James T. Link , Jeffrey J. Rohde , Jurgen Dinges , Bryan K. Sorensen , Martin Winn , Hong Yong , Vince S. Yeh
IPC分类号: A61K31/16 , C07C239/00
CPC分类号: C07C235/14 , A61K31/165 , A61K31/19 , A61K31/4439 , C07C235/22 , C07C237/24 , C07C271/28 , C07C311/46 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D207/48 , C07D257/04 , C07D261/08 , C07D295/088 , C07D401/04
摘要: The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
摘要翻译: 本发明涉及11-β-羟基类固醇脱氢酶1型酶的抑制剂及其在治疗非胰岛素依赖性2型糖尿病,胰岛素抵抗,肥胖症,脂质障碍,代谢综合征,中枢神经系统疾病和疾病中的用途,以及 与过量糖皮质激素有关的病症。
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公开(公告)号:US20090054426A1
公开(公告)日:2009-02-26
申请号:US12195937
申请日:2008-08-21
申请人: R. Scott Bitner , Kaitlin E. Browman , Michael E. Brune , Yixian Chen , Jurgen Dinges , Karla Drescher , Peer Jacobson , Hwan-soo Jae , Ravi Kurukulasuriya , James T. Link , David J. Madar , Jyoti R. Patel , Marina A. Pliushchev , Jeffrey J. Rohde , Lynne E. Rueter , Qi Shuai , Bryan K. Sorensen , Jiahong Wang , Karsten M. Wicke , Martin Winn , Dariusz Wodka , Vince Yeh , Hong Yong
发明人: R. Scott Bitner , Kaitlin E. Browman , Michael E. Brune , Yixian Chen , Jurgen Dinges , Karla Drescher , Peer Jacobson , Hwan-soo Jae , Ravi Kurukulasuriya , James T. Link , David J. Madar , Jyoti R. Patel , Marina A. Pliushchev , Jeffrey J. Rohde , Lynne E. Rueter , Qi Shuai , Bryan K. Sorensen , Jiahong Wang , Karsten M. Wicke , Martin Winn , Dariusz Wodka , Vince Yeh , Hong Yong
IPC分类号: A61K31/496 , A61P25/00 , A61K31/5375 , A61K31/445 , A61K31/16
CPC分类号: C07D403/12 , A61K31/44 , A61K31/495 , C07D207/267 , C07D401/12 , C07D401/14
摘要: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-β-hydroxysteroid dehydrogenase Type 1 enzyme activity.
摘要翻译: 一种治疗患有与老化和神经变性相关的糖尿病中枢神经系统紊乱和缺陷的患者的方法,包括注意力缺陷障碍,注意力缺陷多动障碍(ADHD),阿尔茨海默病(AD),轻度认知障碍 老年性痴呆,艾滋病痴呆,神经变性,抑郁和精神分裂症,包括向需要这种治疗的患者施用有效量的11-β-羟基类固醇脱氢酶1型酶活性的选择性抑制剂。
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