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41.发明授权公开(公告)号：US06180642B2
公开(公告)日：2001-01-30
申请号：US09520318
申请日：2000-03-07
IPC分类号： A61K31495
CPC分类号： C07D519/00
摘要： There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
摘要翻译： 公开了式（I）化合物及其药学上可接受的盐，其可用作GnRH的拮抗剂，因此可用于治疗男性和女性中各种性激素相关和其他病症。
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公开(公告)号：US6156772A
公开(公告)日：2000-12-05
申请号：US312192
申请日：1999-05-14
IPC分类号： A61K45/06 , C07D401/12 , C07D401/14 , C07D491/08 , A01N43/40 , A01N43/38 , C07D209/02 , C07D401/00 , C07D405/00
CPC分类号： C07D401/12 , A61K45/06 , C07D401/14 , C07D491/08
摘要： There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
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公开(公告)号：US10442819B2
公开(公告)日：2019-10-15
申请号：US15532549
申请日：2015-12-01
申请人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig Gibeau , Tesfaye Biftu , Purakkattle Biju , Lei Chen , Joshua Close , Peter H. Fuller , Xianhai Huang , Min K. Park , Valdimir Simov , David J. Witter , Hongjun Zhang
发明人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig Gibeau , Tesfaye Biftu , Purakkattle Biju , Lei Chen , Joshua Close , Peter H. Fuller , Xianhai Huang , Min K. Park , Valdimir Simov , David J. Witter , Hongjun Zhang
IPC分类号： A61K31/351 , A61K31/4353 , A61K31/5355 , A61K31/551 , C07D471/04 , C07D471/14 , C07D498/08 , C07D471/08 , C07D498/04 , C07D498/10 , A01N43/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
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公开(公告)号：US07696177B2
公开(公告)日：2010-04-13
申请号：US11922055
申请日：2006-06-09
CPC分类号： C07D405/10 , C07D205/08 , C07H7/033 , C07H7/04 , C07H7/06 , C07H15/18 , C07H15/203
摘要： This invention provides cholesterol absorption inhibitors of Formula (I), and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.
摘要翻译： 本发明提供式（I）的胆固醇吸收抑制剂及其药学上可接受的盐和酯。 该化合物可用于降低血浆胆固醇水平，特别是低密度脂蛋白胆固醇，以及用于治疗和预防动脉粥样硬化和动脉粥样硬化疾病事件。
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公开(公告)号：US20060128963A1
公开(公告)日：2006-06-15
申请号：US10560290
申请日：2004-07-16
申请人： Heather Sings , Feroze Ujjainwalla
发明人： Heather Sings , Feroze Ujjainwalla
IPC分类号： C07D403/02 , C07D401/02 , C07D211/60
CPC分类号： C07D401/06 , C07D401/14
摘要： Certain novel piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
摘要翻译： 某些新的哌啶衍生物是人类黑皮质素受体的激动剂，特别是人黑皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。
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公开(公告)号：US07012084B2
公开(公告)日：2006-03-14
申请号：US10468517
申请日：2002-02-25
IPC分类号： A61K31/445 , C07D211/06
CPC分类号： C07D413/06 , C07D211/26 , C07D211/28 , C07D211/62 , C07D413/14
摘要： Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
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公开(公告)号：US20060035935A1
公开(公告)日：2006-02-16
申请号：US11239721
申请日：2005-09-30
申请人： Mark Goulet , Ravi Nargund , Iyassu Sebhat , Feroze Ujjainwalla , Thomas Walsh , Daniel Warner , Zhixiong Ye , Jonathan Young , Raman Bakshi
发明人： Mark Goulet , Ravi Nargund , Iyassu Sebhat , Feroze Ujjainwalla , Thomas Walsh , Daniel Warner , Zhixiong Ye , Jonathan Young , Raman Bakshi
IPC分类号： A61K31/454 , C07D417/02 , C07D413/02 , C07D403/02 , C07D401/02
CPC分类号： C07D491/08 , A61K31/445 , C07D211/62 , C07D211/64 , C07D401/06 , C07D401/14 , C07D413/06 , C07D413/14
摘要： Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
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公开(公告)号：US5998432A
公开(公告)日：1999-12-07
申请号：US276029
申请日：1999-03-25
IPC分类号： C07D519/00 , A61K31/435 , C07D471/04
CPC分类号： C07D519/00
摘要： There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
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公开(公告)号：US08742110B2
公开(公告)日：2014-06-03
申请号：US13810946
申请日：2011-08-12
申请人： Joseph L. Duffy , Jianming Bao , Debra L. Ondeyka , Sriram Tyagarajan , Patrick Shao , Feng Ye , Revathi Katipally , Aaron Zwicker , Edward C. Sherer , Michael A. Plotkin , Remond Moningka , Zahid Hussain , Harold B. Wood , Feroze Ujjainwalla , F. Anthony Romero , Paul E. Finke , Yi Zang , Weiguo Liu
发明人： Joseph L. Duffy , Jianming Bao , Debra L. Ondeyka , Sriram Tyagarajan , Patrick Shao , Feng Ye , Revathi Katipally , Aaron Zwicker , Edward C. Sherer , Michael A. Plotkin , Remond Moningka , Zahid Hussain , Harold B. Wood , Feroze Ujjainwalla , F. Anthony Romero , Paul E. Finke , Yi Zang , Weiguo Liu
IPC分类号： C07D215/00 , C07D229/00 , A61K31/44 , A61K31/397
CPC分类号： C07D498/10 , C07D519/00
摘要： Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
摘要翻译： 结构式（I）的取代的螺环胺是生长抑素亚型受体5（SSTR5）的选择性拮抗剂，可用于治疗，控制或预防对SSTR5的拮抗作用有响应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍 ，肥胖症，动脉粥样硬化，代谢综合征，抑郁症和焦虑症。
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50.发明授权公开(公告)号：US07700778B2
公开(公告)日：2010-04-20
申请号：US11239770
申请日：2005-09-30
IPC分类号： C07D401/06 , A61K31/454 , A61K31/451
CPC分类号： C07D413/06 , C07D211/26 , C07D211/28 , C07D211/62 , C07D413/14
摘要： Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
摘要翻译： 某些新的4-取代的N-酰化哌啶衍生物是人类黑皮质素受体的激动剂，特别是人黑皮质素-4受体（MC-4R）的选择性激动剂。 因此，它们可用于治疗，控制或预防对MC-4R的激活反应的疾病和病症，例如肥胖，糖尿病，性功能障碍，包括勃起功能障碍和女性性功能障碍。
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