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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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2.发明申请公开(公告)号：US20080312214A1
公开(公告)日：2008-12-18
申请号：US12197760
申请日：2008-08-25
IPC分类号： A61K31/55 , A61K31/4439 , A61K31/4015 , A61P25/22 , A61P25/24 , A61P25/28
CPC分类号： C07D401/14 , C07D207/26 , C07D207/267 , C07D401/12 , C07D403/12
摘要： Methods for treating a mammal suffering from glucocorticoid-related diseases and conditions, comprising administering to the mammal an effective amount of a selective inhibitor of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme activity, wherein the inhibitor is a compound of formula (I): or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Methods of inhibiting 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. Methods of treating neuronal degeneration, dysfunction, acute psychosis, anxiety, dementia, depression, non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
摘要翻译： 用于治疗患有糖皮质激素相关疾病和病症的哺乳动物的方法，包括向哺乳动物施用有效量的11-β-羟基类固醇脱氢酶1型酶活性的选择性抑制剂，其中所述抑制剂是式（I）的化合物： 或其药学上可接受的盐，前药，前药的盐或其组合。 抑制11-β-羟基类固醇脱氢酶1型酶的方法。 治疗由过度糖皮质激素作用介导的神经元变性，功能障碍，急性精神病，焦虑，痴呆，抑郁症，非胰岛素依赖型2型糖尿病，胰岛素抵抗，肥胖症，脂质疾病，代谢综合征和其他疾病和病症的方法。
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3.发明授权公开(公告)号：US08993632B2
公开(公告)日：2015-03-31
申请号：US13469021
申请日：2012-05-10
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 , Jeffrey J. Rohde , Qi Shuai , James T. Link , Jyoti R. Patel , Jurgen Dinges , Bryan K. Sorensen , Hong Yong , Vince S. Yeh , Ravi Kurukulasuriya
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 , Jeffrey J. Rohde , Qi Shuai , James T. Link , Jyoti R. Patel , Jurgen Dinges , Bryan K. Sorensen , Hong Yong , Vince S. Yeh , Ravi Kurukulasuriya
IPC分类号： A61K31/16 , C07C233/11 , A61K31/165 , A61K31/195 , A61K31/44 , A61K31/45 , A61K31/5377 , C07C233/52 , C07C233/58 , C07C233/63 , C07C237/24 , C07C311/46 , C07D207/277 , C07D211/78 , C07D213/56 , C07D231/12 , C07D261/08 , C07D333/24
CPC分类号： A61K31/498 , A61K31/165 , A61K31/195 , A61K31/196 , A61K31/381 , A61K31/4015 , A61K31/415 , A61K31/44 , A61K31/4409 , A61K31/45 , A61K31/451 , A61K31/5377 , C07C233/11 , C07C233/52 , C07C233/58 , C07C233/63 , C07C237/24 , C07C311/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D207/277 , C07D211/78 , C07D213/56 , C07D231/12 , C07D261/08 , C07D333/24
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：US20130059829A1
公开(公告)日：2013-03-07
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： A61K31/5375 , A61K31/55 , A61K31/551 , A61K31/397 , A61K31/16 , A61P25/28 , A61P25/24 , A61P25/18 , A61P25/22 , A61K31/496 , A61P25/00
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.
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5.发明授权公开(公告)号：US08198331B2
公开(公告)日：2012-06-12
申请号：US12390286
申请日：2009-02-20
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 , Jeffrey J. Rohde , Qi Shuai , James T. Link , Jyoti R. Patel , Jurgen Dinges , Bryan K. Sorensen , Hong Yong , Vince S. Yeh , Ravi Kurukulasuriya
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 , Jeffrey J. Rohde , Qi Shuai , James T. Link , Jyoti R. Patel , Jurgen Dinges , Bryan K. Sorensen , Hong Yong , Vince S. Yeh , Ravi Kurukulasuriya
IPC分类号： A61K31/16
CPC分类号： A61K31/498 , A61K31/165 , A61K31/195 , A61K31/196 , A61K31/381 , A61K31/4015 , A61K31/415 , A61K31/44 , A61K31/4409 , A61K31/45 , A61K31/451 , A61K31/5377 , C07C233/11 , C07C233/52 , C07C233/58 , C07C233/63 , C07C237/24 , C07C311/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D207/277 , C07D211/78 , C07D213/56 , C07D231/12 , C07D261/08 , C07D333/24
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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6.发明申请GEMINALLY SUBSTITUTED CYANOETHYLPYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS 有权作为JANUS KINASE抑制剂的GEMYALLY取代的氰基乙基吡唑啉吡啶公开(公告)号：US20160272632A1
公开(公告)日：2016-09-22
申请号：US14778046
申请日：2014-03-19
申请人： Matthew Lloyd CHILDERS , Peter FULLER , David GUERIN , Jason David KATZ , Qinglin PU , Mark E. SCOTT , Christopher E. THOMPSON , Michelle MARTINEZ , Danielle FALCONE , Luis TORRES , Yongqi DENG , Ravi KURUKULASURIYA , Hongbo ZENG , Yunfeng BAI , Norman KONG , Yumei LIU , MERCK SHARP & DOHME CORP.
发明人： Matthew Lloyd Childers , Peter Fuller , David Guerin , Jason David Katz , Qinglin Pu , Mark E. Scott , Christopher F. Thompson , Michelle Martinez , Danielle Falcone , Luis Torres , Yongqi Deng , Ravi Kurukulasuriya , Hongbo Zeng , Yunfeng Bai , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为JAK抑制剂的式（I）化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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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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8.发明授权公开(公告)号：US07737137B2
公开(公告)日：2010-06-15
申请号：US12197760
申请日：2008-08-25
申请人： Michael E. Brune , Peer B. Jacobson , Jeffrey J. Rohde , Jiahong Wang , Steven Fung , Ravi Kurukulasuriya , David J. Madar , James T. Link , Vince S. Yeh
发明人： Michael E. Brune , Peer B. Jacobson , Jeffrey J. Rohde , Jiahong Wang , Steven Fung , Ravi Kurukulasuriya , David J. Madar , James T. Link , Vince S. Yeh
CPC分类号： C07D401/14 , C07D207/26 , C07D207/267 , C07D401/12 , C07D403/12
摘要： Methods for treating a mammal suffering from glucocorticoid-related diseases and conditions, comprising administering to the mammal an effective amount of a selective inhibitor of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme activity, wherein the inhibitor is a compound of formula (I): or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Methods of inhibiting 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. Methods of treating neuronal degeneration, dysfunction, acute psychosis, anxiety, dementia, depression, non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
摘要翻译： 用于治疗患有糖皮质激素相关疾病和病症的哺乳动物的方法，包括向哺乳动物施用有效量的11-β-羟基类固醇脱氢酶1型酶活性的选择性抑制剂，其中所述抑制剂是式（I）的化合物： 或其药学上可接受的盐，前药，前药的盐或其组合。 抑制11-β-羟基类固醇脱氢酶1型酶的方法。 治疗由过度糖皮质激素作用介导的神经元变性，功能障碍，急性精神病，焦虑，痴呆，抑郁症，非胰岛素依赖型2型糖尿病，胰岛素抵抗，肥胖症，脂质疾病，代谢综合征和其他疾病和病症的方法。
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公开(公告)号：USRE41135E1
公开(公告)日：2010-02-16
申请号：US12179405
申请日：2008-07-24
IPC分类号： C07C233/57 , C07C233/64
CPC分类号： C07D207/277 , C07C233/11 , C07C233/52 , C07C233/58 , C07C233/63 , C07C237/24 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D211/78 , C07D213/56 , C07D231/12 , C07D261/08 , C07D333/24
摘要： The present invention relates to compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
摘要翻译： 本发明涉及作为11-β-羟基类固醇脱氢酶1型酶的抑制剂的化合物。 本发明还涉及用于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，代谢综合征和其它疾病和病症的11-β-羟基类固醇脱氢酶1型酶抑制剂的用途，所述疾病和病症由 过度的糖皮质激素作用。
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公开(公告)号：US20150258074A1
公开(公告)日：2015-09-17
申请号：US14431485
申请日：2013-09-26
申请人： Kevin J. WILSON , David J. WITTER , Matthew H. DANIELS , Angie R. ANGELES , Phieng SILIPHAIVANH , David L. SLOMAN , Brendan O'BOYLE , Danielle FALCONE , Catherine WHITE , Ron FERGUSON , Wei ZHOU , Kathryn LIPFORD , Umar Faruk MANSOOR , Salem FEVRIRE , Xianhai HUANG , Ravi KURUKULASURIYA , Judson E. RICHARD , Shuyi TANG , Christopher BOYCE , Joseph KOZLOWSKI , Raman Kumar BAKSHI , Ganesh Babu UNAKARAN , Merck Sharp & Dohme Corp.
发明人： Kevin J. Wilson , David J. Witter , Matthew H. Daniels , Angie R. Angeles , Phieng Siliphaivanh , David Sloman , Brendan O'Boyle , Danielle Falcone , Catherine White , Ron Ferguson , Wei Zhou , Kathryn Lipford , Umar Faruk Mansoor , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Judson E. Richard , Shuyi Tang , Christopher Boyce , Joseph Kozlowski , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC分类号： A61K31/437 , A61K45/06 , A61K31/4545 , C07D471/04
CPC分类号： A61K31/437 , A61K31/4545 , A61K45/06 , C07D471/04
摘要： Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0).
摘要翻译： 公开了具有吡唑并吡啶基结构的式（1.0）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1.0）化合物治疗癌症的方法。
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