Raman K. Bakshi - Edison NJ, US Liangqin Guo - Edison NJ, US Qingmei Hong - Scotch Plains NJ, US Ravi P. Nargund - East Brunswick NJ, US Patrick G. Pollard - Oakhurst NJ, US Iyassu K. Sebhat - New York NY, US Feroze Ujjainwalla - Scotch Plains NJ, US Zhixiong Ye - Princeton NJ, US
Certain novel N-acylated piperazine 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.
Bicyclic Piperidine Derivatives As Melanocortin-4 Receptor Agonists
Certain novel bicyclic 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.
Acylated Spiropiperidine Derivatives As Melanocortin-4 Receptor Agonists
Liangqin Guo - Edison NJ, US Shuwen He - Edison NJ, US Tianying Jian - Westfield NJ, US Yingjie Lai - Edison NJ, US Jian Liu - Edison NJ, US Ravi P. Nargund - East Brunswick NJ, US Iyassu K. Sebhat - New York NY, US Feroze Ujjainwalla - Scotch Plains NJ, US Zhixiong Ye - Princeton NJ, US Jonathan R. Young - Kendall Park NJ, US
Assignee:
Merck & Co., Inc. - Rahway NJ
International Classification:
A61K 31/438 C07D 221/20 C07D 401/02
US Classification:
514278, 546 17, 546 18
Abstract:
Certain novel N-acylated spiropiperidine 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.
Acylated Spiropiperidine Derivatives As Melanocortin-4 Receptor Modulators
Raman K. Bakshi - Edison NJ, US James P. Dellureficio - Millington NJ, US Peter H. Dobbelaar - Morris Plains NJ, US Liangqin Guo - Edison NJ, US Shuwen He - Edison NJ, US Qingmei Hong - Scotch Plains NJ, US Ravi P. Nargund - East Brunswick NJ, US Zhixiong Ye - West Windsor NJ, US
Assignee:
Merck Sharp & Dohme Corp. - Rahway NJ
International Classification:
A61K 31/438 C07D 491/107
US Classification:
514278, 546 17, 544125, 5142328
Abstract:
Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands 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 modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
Acylated Piperidine Derivatives As Melanocortin 4-Receptor Agonists
Khaled Barakat - Brooklyn NY, US Liangqin Guo - Edison NJ, US Jian Liu - Edison NJ, US Ravi Nargund - East Brunswick NJ, US Iyassu Sebhat - New York NY, US Zhixiong Ye - Princeton NJ, US
Certain novel 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.
Beta Carboline Derivatives As Antidiabetic Compounds
Peter H. Dobbelaar - Morris Plains NJ, US Wu Du - Monroe Township NJ, US Liangqin Guo - Edison NJ, US William K. Hagmann - Westfield NJ, US Shuwen He - Edison NJ, US Tianying Jian - Westfield NJ, US Jian Liu - Edison NJ, US Ravi P. Nargund - East Brunswick NJ, US Alexander Pasternak - Princeton NJ, US Shrenik K. Shah - Metuchen NJ, US Quang T. Truong - Morganville NJ, US Zhixiong Ye - Princeton NJ, US Raman Bakshi - Edison NJ, US
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.
Amino Cyclopentyl Heterocyclic And Carbocyclic Modulators Of Chemokine Receptor Activity
Lihu Yang - Edison NJ, US Songnian Lin - Monroe NJ, US Gregori Morriello - Randolph NJ, US Liangqin Guo - Edison NJ, US Changyou Zhou - Plainsboro NJ, US
Compounds of the formulae (I) and (II): (wherein Q, X, E, G, G, R, R, R, R, Rand Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
Triazole Beta Carboline Derivatives As Anti-Diabetic Agents
Liangqin Guo - Edison NJ, US Jian Liu - Edison NJ, US Ravi P. Nargund - East Brunswick NJ, US Alexander Pasternak - Princeton NJ, US Lihu Yang - Edison NJ, US Zhixiong Ye - West Windsor NJ, US
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.
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