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1.Open chain prolyl urea-related modulators of androgen receptor function 有权
标题翻译: 开链脯氨酰脲相关调节剂的雄激素受体功能公开(公告)号:US07632858B2
公开(公告)日:2009-12-15
申请号:US10712456
申请日:2003-11-13
IPC分类号: C07D207/12 , A61K31/4015 , A61P35/00
CPC分类号: C07D207/16 , C07D401/12
摘要: The invention provides for a pharmaceutical composition capable of modulating the androgen receptor comprising a compound of formula I wherein R1, R2, R3, X, Y, Z and G 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.
摘要翻译: 本发明提供能够调节包含式I化合物的雄激素受体的药物组合物,其中R 1,R 2,R 3,X,Y,Z和G如本文所述。 还提供了使用这些化合物治疗核激素受体相关病症(如与年龄相关的疾病,例如肌肉减少症)的方法,并且还提供含有这些化合物的药物组合物。
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2.Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof 失效
标题翻译: 二肽基肽酶IV抑制剂的生产方法和化合物及其中间体公开(公告)号:US07705033B2
公开(公告)日:2010-04-27
申请号:US12181216
申请日:2008-07-28
申请人: Truc Chi Vu , David B. Brzozowski , Rita Fox , Jollie Duaine Godfrey, Jr. , Ronald L. Hanson , Sergei V. Kolotuchin , John A. Mazzullo , Ramesh N. Patel , Jianji Wang , Kwok Wong , Jurong Yu , Jason J. Zhu , David R. Magnin , David J. Augeri , Lawrence G. Hamann
发明人: Truc Chi Vu , David B. Brzozowski , Rita Fox , Jollie Duaine Godfrey, Jr. , Ronald L. Hanson , Sergei V. Kolotuchin , John A. Mazzullo , Ramesh N. Patel , Jianji Wang , Kwok Wong , Jurong Yu , Jason J. Zhu , David R. Magnin , David J. Augeri , Lawrence G. Hamann
IPC分类号: A61K31/403 , C07D209/52
CPC分类号: C07C69/757 , C07C62/06 , C07C69/635 , C07C69/675 , C07C229/28 , C07C271/22 , C07C2603/74 , C07D207/22 , C07D209/52
摘要: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
摘要翻译: 提供了用于制备二肽基肽酶IV的环丙基稠合吡咯烷基抑制剂的方法和化合物。
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3.Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof 有权
标题翻译: 二肽基肽酶IV抑制剂的生产方法和化合物及其中间体公开(公告)号:US08278462B2
公开(公告)日:2012-10-02
申请号:US12712958
申请日:2010-02-25
申请人: Truc Chi Vu , David B. Brzozowski , Rita Fox , Jollie Duaine Godfrey, Jr. , Ronald L. Hanson , Sergei V. Kolotuchin , John A. Mazzullo , Ramesh N. Patel , Jianji Wang , Kwok Wong , Jurong Yu , Jason J. Zhu , David R. Magnin , David J. Augeri , Lawrence G. Hamann
发明人: Truc Chi Vu , David B. Brzozowski , Rita Fox , Jollie Duaine Godfrey, Jr. , Ronald L. Hanson , Sergei V. Kolotuchin , John A. Mazzullo , Ramesh N. Patel , Jianji Wang , Kwok Wong , Jurong Yu , Jason J. Zhu , David R. Magnin , David J. Augeri , Lawrence G. Hamann
IPC分类号: C07D209/52
CPC分类号: C07C69/757 , C07C62/06 , C07C69/635 , C07C69/675 , C07C229/28 , C07C271/22 , C07C2603/74 , C07D207/22 , C07D209/52
摘要: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
摘要翻译: 提供了用于制备二肽基肽酶IV的环丙基稠合吡咯烷基抑制剂的方法和化合物。
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4.
公开(公告)号:US20130012723A1
公开(公告)日:2013-01-10
申请号:US13601477
申请日:2012-08-31
申请人: Truc Chi Vu , David B. Brzozowski , Rita Fox , Jollie Duaine Godfrey, JR. , Ronald L. Hanson , Sergei V. Kolotuchin , John A. Mazzullo , Ramesh N. Patel , Jianji Wang , Kwok Wong , Jurong Yu , Jason J. Zhu , David R. Magnin , David J. Augeri , Lawrence G. Hamann
发明人: Truc Chi Vu , David B. Brzozowski , Rita Fox , Jollie Duaine Godfrey, JR. , Ronald L. Hanson , Sergei V. Kolotuchin , John A. Mazzullo , Ramesh N. Patel , Jianji Wang , Kwok Wong , Jurong Yu , Jason J. Zhu , David R. Magnin , David J. Augeri , Lawrence G. Hamann
IPC分类号: C07D209/52 , C12N1/21 , C12N1/19 , C07D207/22
CPC分类号: C07C69/757 , C07C62/06 , C07C69/635 , C07C69/675 , C07C229/28 , C07C271/22 , C07C2603/74 , C07D207/22 , C07D209/52
摘要: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
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5.METHODS AND COMPOUNDS FOR PRODUCING DIPEPTIDYL PEPTIDASE IV INHIBITORS AND INTERMEDIATES THEREOF 失效
标题翻译: 用于生产二磷酸酯酶IV抑制剂的方法和化合物及其中间体公开(公告)号:US20090018311A1
公开(公告)日:2009-01-15
申请号:US12181216
申请日:2008-07-28
申请人: Truc Chi Vu , David B. Brzozowski , Rita Fox , Jollie Duaine Godfrey, JR. , Ronald L. Hanson , Sergei V. Kolotuchin , John A. Mazzullo , Ramesh N. Patel , Jianji Wang , Kwok Wong , Jurong Yu , Jason J. Zhu , David R. Magnin , David J. Augeri , Lawrence G. Hamann
发明人: Truc Chi Vu , David B. Brzozowski , Rita Fox , Jollie Duaine Godfrey, JR. , Ronald L. Hanson , Sergei V. Kolotuchin , John A. Mazzullo , Ramesh N. Patel , Jianji Wang , Kwok Wong , Jurong Yu , Jason J. Zhu , David R. Magnin , David J. Augeri , Lawrence G. Hamann
IPC分类号: C07K1/02 , C07D207/22 , C07D209/52 , C07C209/08 , C12N1/21 , C07C51/09
CPC分类号: C07C69/757 , C07C62/06 , C07C69/635 , C07C69/675 , C07C229/28 , C07C271/22 , C07C2603/74 , C07D207/22 , C07D209/52
摘要: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
摘要翻译: 提供了用于制备二肽基肽酶IV的环丙基稠合吡咯烷基抑制剂的方法和化合物。
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6.Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method 有权
标题翻译: 二丙基稠合吡咯烷基二肽基肽酶IV抑制剂及方法公开(公告)号:US06395767B2
公开(公告)日:2002-05-28
申请号:US09788173
申请日:2001-02-16
申请人: Jeffrey A. Robl , Richard B. Sulsky , David J. Augeri , David R. Magnin , Lawrence G. Hamann , David A. Betebenner
发明人: Jeffrey A. Robl , Richard B. Sulsky , David J. Augeri , David R. Magnin , Lawrence G. Hamann , David A. Betebenner
IPC分类号: C07D20907
CPC分类号: C07C271/22 , C07C2603/74 , C07D209/52 , C07D401/06 , C07D403/06
摘要: Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where x is 0 or 1 and y is 0 or 1 (provided that x=1 when y=0 and x=0 when y=1); n is 0 or 1; X is H or CN; and wherein R1, R2, R3 and R4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor *or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.
摘要翻译: 提供二肽基肽酶IV(DP 4)抑制化合物,其具有0或1并且y为0或1(当y = 0时X = 1,当y = 1时x = 0); n为0或1; X是H或CN;并且其中R 1,R 2,R 3和R 4如本文所述。还提供了用于治疗糖尿病和相关疾病,特别是II型糖尿病和本文所列的其它疾病的方法,使用这种DP 4抑制剂 *或这种DP 4抑制剂与一种或多种其它抗糖尿病药如二甲双胍,格列本脲,曲格列酮,吡格列酮,罗格列酮和/或胰岛素和/或降血脂药和/或抗肥胖剂中的一种或多种的组合,以及 /或其他治疗剂。
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7.Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method 有权
标题翻译: 二丙基稠合吡咯烷基二肽基肽酶IV抑制剂及方法公开(公告)号:USRE44186E1
公开(公告)日:2013-04-30
申请号:US13308658
申请日:2011-12-01
申请人: Jeffrey A. Robl , Richard B. Sulsky , David J. Augeri , David R. Magnin , Lawrence G. Hamann , David A. Betebenner
发明人: Jeffrey A. Robl , Richard B. Sulsky , David J. Augeri , David R. Magnin , Lawrence G. Hamann , David A. Betebenner
IPC分类号: C07D209/02 , A61K31/403
CPC分类号: C07C271/22 , C07C2603/74 , C07D209/52 , C07D401/06 , C07D403/06
摘要: Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where x is 0 or 1 and y is 0 or 1 (provided that x=1 when y=0 and x=0 when y=1); n is 0 or 1; X is H or CN; and wherein R1, R2, R3 and R4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor *or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.
摘要翻译: 提供二肽基肽酶IV(DP 4)抑制化合物,其具有下式,其中x为0或1,y为0或1(当y = 0时x = 1,y = 1时x = 0); n为0或1; X是H或CN; 并且其中R 1,R 2,R 3和R 4如本文所述。 还提供了一种用于治疗糖尿病和相关疾病,特别是II型糖尿病和本文所列的其它疾病的方法,其使用这种DP 4抑制剂*或这种DP 4抑制剂与一种或多种其它抗糖尿病药如二甲双胍的组合 ,格列本脲,曲格列酮,吡格列酮,罗格列酮和/或胰岛素和/或降血脂药和/或抗肥胖剂和/或其它治疗剂中的一种或多种。
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8.METHODS AND COMPOUNDS FOR PRODUCING DIPEPTIDYL PEPTIDASE IV INHIBITORS AND INTERMEDIATES THEREOF 有权
标题翻译: 用于生产二磷酸酯酶IV抑制剂的方法和化合物及其中间体公开(公告)号:US20100274025A1
公开(公告)日:2010-10-28
申请号:US12712958
申请日:2010-02-25
申请人: Truc Chi Vu , David B. Brzozowski , Rita Fox , Jollie Duaine Godfrey, JR. , Ronald L. Hanson , Sergei V. Kolotuchin , John A. Mazzullo , Ramesh N. Patel , Jianji Wang , Kwok Wong , Jurong Yu , Jason J. Zhu , David R. Magnin , David J. Augeri , Lawrence G. Hamann
发明人: Truc Chi Vu , David B. Brzozowski , Rita Fox , Jollie Duaine Godfrey, JR. , Ronald L. Hanson , Sergei V. Kolotuchin , John A. Mazzullo , Ramesh N. Patel , Jianji Wang , Kwok Wong , Jurong Yu , Jason J. Zhu , David R. Magnin , David J. Augeri , Lawrence G. Hamann
IPC分类号: C07D209/52 , C07D207/22 , C07C57/28 , C12N1/19 , C12N1/21
CPC分类号: C07C69/757 , C07C62/06 , C07C69/635 , C07C69/675 , C07C229/28 , C07C271/22 , C07C2603/74 , C07D207/22 , C07D209/52
摘要: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
摘要翻译: 提供了用于制备二肽基肽酶IV的环丙基稠合吡咯烷基抑制剂的方法和化合物。
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9.Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof 有权
标题翻译: 二肽基肽酶IV抑制剂的生产方法和化合物及其中间体公开(公告)号:US07420079B2
公开(公告)日:2008-09-02
申请号:US10716012
申请日:2003-11-18
申请人: Truc Chi Vu , David B. Brzozowski , Rita Fox , Jollie Duaine Godfrey, Jr. , Ronald L. Hanson , Sergei V. Kolotuchin , John A. Mazzullo , Ramesh N. Patel , Jianji Wang , Kwok Wong , Jurong Yu , Jason J. Zhu , David R. Magnin , David J. Augeri , Lawrence G. Hamann
发明人: Truc Chi Vu , David B. Brzozowski , Rita Fox , Jollie Duaine Godfrey, Jr. , Ronald L. Hanson , Sergei V. Kolotuchin , John A. Mazzullo , Ramesh N. Patel , Jianji Wang , Kwok Wong , Jurong Yu , Jason J. Zhu , David R. Magnin , David J. Augeri , Lawrence G. Hamann
IPC分类号: C07C69/52 , C07C229/02
CPC分类号: C07C69/757 , C07C62/06 , C07C69/635 , C07C69/675 , C07C229/28 , C07C271/22 , C07C2603/74 , C07D207/22 , C07D209/52
摘要: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
摘要翻译: 提供了用于制备二肽基肽酶IV的环丙基稠合吡咯烷基抑制剂的方法和化合物。
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10.4-amino-1H-pyrimidin-2-one based compounds, compositions comprising them and methods of their use 有权
标题翻译: 4-氨基-1H-嘧啶-2-酮基化合物,包含它们的组合物及其使用方法公开(公告)号:US08093245B2
公开(公告)日:2012-01-10
申请号:US11954421
申请日:2007-12-12
申请人: David J. Augeri , Marianne Carlsen , Kenneth G. Carson , Qinghong Fu , Alexander Heim-Riether , Theodore C. Jessop , James E. Tarver , Jerry A. Taylor
发明人: David J. Augeri , Marianne Carlsen , Kenneth G. Carson , Qinghong Fu , Alexander Heim-Riether , Theodore C. Jessop , James E. Tarver , Jerry A. Taylor
IPC分类号: C07D239/47 , C07D403/04 , A61K31/506
CPC分类号: C07D239/47 , C07D239/54 , C07D403/04 , C07D403/08 , C07D403/12 , C07D405/12 , C07D409/14 , C07D417/12 , C07D471/04
摘要: 4-Amino-1H-pyrimidin-2-one-based compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of various diseases and disorders are disclosed. Particular compounds are of formula I:
摘要翻译: 公开了4-氨基-1H-嘧啶-2-酮基化合物,包含它们的组合物及其用于治疗,预防和治疗各种疾病和病症的方法。 特定的化合物具有式I:
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