公开(公告)号：US5652235A

公开(公告)日：1997-07-29

申请号：US641311

申请日：1996-04-30

申请人： Meng-Hsin Chen ,  Ravi P. Nargund ,  David B. R. Johnston ,  Arthur A. Patchett ,  James R. Tata ,  Lihu Yang

发明人： Meng-Hsin Chen ,  Ravi P. Nargund ,  David B. R. Johnston ,  Arthur A. Patchett ,  James R. Tata ,  Lihu Yang

IPC分类号： A61K31/435 ,  A61K31/438 ,  A61K31/445 ,  A61K31/47 ,  A61K38/00 ,  A61K38/04 ,  A61P3/00 ,  A61P19/10 ,  A61P43/00 ,  C07D221/20 ,  C07D401/10 ,  C07D471/10 ,  C07D491/10 ,  C07D491/107 ,  C07D495/10 ,  C07D495/20 ,  C07D519/00 ,  C07K1/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K14/00 ,  A61K31/55 ,  A61K31/44

CPC分类号： C07D401/10 ,  C07D471/10 ,  C07D491/10 ,  C07D495/10 ,  C07K5/021 ,  C07K5/06034 ,  C07K5/06147 ,  C07K5/06191 ,  A61K38/00 ,  Y02P20/55

摘要： There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.

摘要翻译： 已经公开了鉴定为促进人和动物中生长激素释放的螺哌啶和同系物的某些新化合物。 这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小 儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。 还公开了含有作为其活性成分的螺环化合物的生长激素释放组合物。

公开(公告)号：US5578593A

公开(公告)日：1996-11-26

申请号：US146848

申请日：1993-11-03

申请人： Meng-Hsin Chen ,  David B. R. Johnston ,  Ravi P. Nargund ,  Arthur A. Patchett ,  James R. Tata ,  Lihu Yang

发明人： Meng-Hsin Chen ,  David B. R. Johnston ,  Ravi P. Nargund ,  Arthur A. Patchett ,  James R. Tata ,  Lihu Yang

IPC分类号： A61K38/00 ,  C07D401/10 ,  C07D471/10 ,  C07D491/10 ,  C07D495/10 ,  C07D519/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  A61K31/55 ,  A61K31/44 ,  C07D401/00 ,  C07D471/00

CPC分类号： C07D401/10 ,  C07D471/10 ,  C07D491/10 ,  C07D495/10 ,  C07K5/021 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06147 ,  C07K5/06191 ,  A61K38/00 ,  Y10S514/825

摘要： There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.

摘要翻译： 已经公开了鉴定为促进人和动物中生长激素释放的螺哌啶和同系物的某些新化合物。 这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小 儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。 还公开了含有作为其活性成分的螺环化合物的生长激素释放组合物。

公开(公告)号：US5536716A

公开(公告)日：1996-07-16

申请号：US147226

申请日：1993-11-03

申请人： Meng-Hsin Chen ,  David B. R. Johnston ,  Ravi P. Nargund ,  Arthur A. Patchett ,  James R. Tata ,  Lihu Yang

发明人： Meng-Hsin Chen ,  David B. R. Johnston ,  Ravi P. Nargund ,  Arthur A. Patchett ,  James R. Tata ,  Lihu Yang

IPC分类号： A61K38/00 ,  C07D401/10 ,  C07D471/10 ,  C07D491/10 ,  C07D495/10 ,  C07D519/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  A61K31/55 ,  A61K31/44 ,  C07D401/04 ,  C07D451/00

CPC分类号： C07D401/10 ,  C07D471/10 ,  C07D491/10 ,  C07D495/10 ,  C07K5/021 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06147 ,  C07K5/06191 ,  A61K38/00 ,  Y10S514/825

摘要： There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.

摘要翻译： 已经公开了鉴定为促进人和动物中生长激素释放的螺哌啶和同系物的某些新化合物。 这种性质可以用于促进食用动物的生长，使食用肉制品的生产更有效，并且在人类中，用于治疗以生长激素分泌不足为特征的生理或医学病症，例如生长激素缺乏的身材矮小 儿童，并且治疗通过生长激素的合成代谢作用改善的医疗状况。 还公开了含有作为其活性成分的螺环化合物的生长激素释放组合物。

公开(公告)号：US06410548B1

公开(公告)日：2002-06-25

申请号：US09781373

申请日：2001-02-12

申请人： Ravi P. Nargund ,  Zhixiong Ye ,  Brenda L. Palucki ,  Raman K. Bakshi ,  Arthur A. Patchett ,  Leonardus H. T. Van Der Ploeg

发明人： Ravi P. Nargund ,  Zhixiong Ye ,  Brenda L. Palucki ,  Raman K. Bakshi ,  Arthur A. Patchett ,  Leonardus H. T. Van Der Ploeg

IPC分类号： A61K31438

摘要： Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.

公开(公告)号：US06350760B1

公开(公告)日：2002-02-26

申请号：US09585111

申请日：2000-06-01

申请人： Raman K. Bakshi ,  Khaled J. Barakat ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Arthur A. Patchett ,  Iyassu Sebhat ,  Zhixiong Ye ,  Leonardus H. T. Van Der Ploeg

发明人： Raman K. Bakshi ,  Khaled J. Barakat ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Arthur A. Patchett ,  Iyassu Sebhat ,  Zhixiong Ye ,  Leonardus H. T. Van Der Ploeg

IPC分类号： A61K3144

CPC分类号： C07D231/12 ,  A61K31/4725 ,  A61K31/4985 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： Certain novel substituted piperidine compounds 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. Also provided are methods of treating sexual dysfunction with a compound that is a selective agonist of MC-4R over any other human melanocortin receptor.

摘要翻译： 某些新的取代的哌啶化合物是人类黑皮质素受体的激动剂，特别是人黑素皮质素-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。 还提供了使用作为MC-4R的选择性激动剂的化合物超过任何其它人类黑皮质素受体来治疗性功能障碍的方法。

公开(公告)号：US06767915B2

公开(公告)日：2004-07-27

申请号：US10343040

申请日：2003-01-27

申请人： Raman K. Bakshi ,  Khaled J. Barakat ,  Yingjie Lai ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Min K. Park ,  Iyassu K. Sebhat ,  Zhixiong Ye ,  Arthur A. Patchett

发明人： Raman K. Bakshi ,  Khaled J. Barakat ,  Yingjie Lai ,  Ravi P. Nargund ,  Brenda L. Palucki ,  Min K. Park ,  Iyassu K. Sebhat ,  Zhixiong Ye ,  Arthur A. Patchett

IPC分类号： A61K31445

CPC分类号： C07D211/62 ,  A61K31/445 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  C07D211/20 ,  C07D211/24 ,  C07D211/26 ,  C07D401/06 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D487/08 ,  C07D491/08

摘要： Certain novel 4-substituted piperidine compounds 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-取代的哌啶化合物是人类黑皮质素受体的激动剂，特别是人黑素皮质素-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。

公开(公告)号：US06294534B1

公开(公告)日：2001-09-25

申请号：US09329814

申请日：1999-06-10

申请人： Ravi P. Nargund ,  Brenda L. Palucki ,  Zhixiong Ye ,  Raman K. Bakshi ,  Arthur A. Patchett ,  Leonardus H. T. Van Der Ploeg

发明人： Ravi P. Nargund ,  Brenda L. Palucki ,  Zhixiong Ye ,  Raman K. Bakshi ,  Arthur A. Patchett ,  Leonardus H. T. Van Der Ploeg

IPC分类号： A61K3144

CPC分类号： C07K5/06139 ,  A61K38/00 ,  C07K5/06191

摘要： Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.

公开(公告)号：US20110201615A1

公开(公告)日：2011-08-18

申请号：US13125319

申请日：2009-10-19

申请人： Liangqin Guo ,  Jian Liu ,  Ravi P. Nargund ,  Alexander Pasternak ,  Lihu Yang ,  Zhixiong Ye

发明人： Liangqin Guo ,  Jian Liu ,  Ravi P. Nargund ,  Alexander Pasternak ,  Lihu Yang ,  Zhixiong Ye

IPC分类号： A61K31/501 ,  C07D471/04 ,  A61K31/437 ,  C07D401/14 ,  A61K31/506 ,  A61P3/00 ,  A61P9/12

CPC分类号： C07D471/04

摘要： Beta-carboline derivatives of structural formula (I) are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.

摘要翻译： 结构式（I）的β-咔啉衍生物是生长抑素亚型受体3（SSTR3）的选择性拮抗剂，可用于治疗2型糖尿病和通常与该疾病相关的病症，包括高血糖症，胰岛素抵抗， 肥胖，脂质障碍和高血压。 这些化合物也可用于治疗抑郁症和焦虑症。

公开(公告)号：US20160251407A1

公开(公告)日：2016-09-01

申请号：US15025912

申请日：2014-10-02

申请人： Songnian LIN ,  Lin YAN ,  Ahmet KEKEC ,  Yuping ZHU ,  David N. HUNTER ,  Pei HUO ,  Danqing FENG ,  Ravi P. NARGUND ,  Christopher R. MOYES ,  Zhiqiang ZHAO ,  Brenda PIPIK ,  Dimitri PISSARNITSKI ,  Joseph L. DUFFY ,  Erin N. GUIDRY ,  MERCK SHARP & DOHME CORP.

发明人： Songnian Lin ,  Lin Yan ,  Ahmet Kekec ,  Yuping Zhu ,  David N. Hunter ,  Pei Huo ,  Danqing Feng ,  Ravi P. Nargund ,  Christopher R. Moyes ,  Zhiqiang Zhao ,  Brenda Pipik ,  Dmitri Pissarnitski ,  Joseph L. Duffy ,  Erin Guidry

IPC分类号： C07K14/62 ,  A61K38/28 ,  A61K47/48

CPC分类号： A61K47/61 ,  A61K38/28 ,  A61K47/549 ,  A61K47/64 ,  C07K14/62

摘要： Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.

摘要翻译： 胰岛素缀合物包含共价连接到具有两个臂的至少一个双齿连接体的胰岛素分子，每个臂独立地连接到包含糖的配体，并且其中至少一个连接体的配体是岩藻糖。 胰岛素缀合物显示药代动力学（PK）和/或药效学（PD）谱，其对糖类如葡萄糖或α-甲基甘露糖的全身浓度有反应，即使在不存在外源多价的情况下施用于有需要的受试者时 糖结合分子如Con A.

公开(公告)号：US08293777B2

公开(公告)日：2012-10-23

申请号：US12629419

申请日：2009-12-02

申请人： Michael Man-Chu Lo ,  Amjad Ali ,  Ravi P. Nargund

发明人： Michael Man-Chu Lo ,  Amjad Ali ,  Ravi P. Nargund

IPC分类号： A61K31/34 ,  A61K31/41 ,  C07D249/00 ,  C07D409/02

CPC分类号： C07D403/10 ,  C07D235/08 ,  C07D257/04 ,  C07D409/06

摘要： A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is Y is selected from the group consisting of R1 is selected from the group consisting of —O—C1-6 alkyl, —O-aryl, —O-heteroaryl, —O—C3-8 cycloalkyl, —C1-6 alkyl, -aryl, -heteroaryl, and —C3-8 cycloalkyl; R2 and R3 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.

摘要翻译： 具有其中R为血管紧张素受体拮抗剂活性基团且Y为Y的结构的化合物选自R 1选自-O-C 1-6烷基，-O-芳基，-O- 杂芳基，-O-C 3-8环烷基，-C 1-6烷基， - 芳基， - 杂芳基和-C 3-8环烷基; R2和R3独立地选自氢和C 1-4烷基，或其药学上可接受的盐或水合物，其可用于治疗高血压。