Shrenik K. Shah - Metuchen NJ, US Quang T. Truong - Metuchen NJ, US Hongbo Qi - Edison NJ, US William K. Hagmann - Westfield NJ, US
Assignee:
Merck & Co., Inc. - Rahway NJ
International Classification:
C07C 211/00 A01N 33/00
US Classification:
514579, 564336
Abstract:
Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, including alcohol and nicotine addiction, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
Substituted Imidazoles As Cannabinoid Receptor Modulators
Paul E. Finke - Milltown NJ, US Sander G. Mills - Scotch Plains NJ, US Christopher W. Plummer - Keasbey NJ, US Shrenik K. Shah - Metuchen NJ, US Quang T. Truong - Edison NJ, US
Assignee:
Merck & Co., Inc. - Rahway NJ
International Classification:
A61K 31/55 C07D 405/00 C07D 413/00
US Classification:
51421709, 51423518, 514326, 544141, 546210
Abstract:
The use of compounds of the present invention as antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor particularly in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB1) receptor. The invention is concerned with the use of these novel compounds to selectively antagonize the Cannabinoid-1 (CB1) receptor. As such, compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith.
Substituted Imidazoles As Cannabinoid Receptor Modulators
Paul Finke - Milltown NJ, US Sander Mills - Scotch Plains NJ, US Christopher Plummer - Keasbey NJ, US Shrenik Shah - Metuchen NJ, US Quang Truong - Edison NJ, US
International Classification:
A61K031/4439 A61K031/4172 A61K031/4178
US Classification:
514/341000, 514/397000, 514/400000
Abstract:
The use of compounds of the present invention as antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor particularly in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB1) receptor. The invention is concerned with the use of these novel compounds to selectively antagonize the Cannabinoid-1 (CB1) receptor. As such, compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith. Novel compounds of structural formula (I) are also claimed.
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.
Oxadiazole Beta Carboline Derivatives As Antidiabetic Compounds
Liangqin Guo - Edison NJ, US William K. Hagmann - Westfield NJ, US Shuwen He - Edison NJ, US Zhong Lai - Scotch Plains NJ, US Jian Liu - Edison NJ, US Ravi P. Nargund - East Brunswick NJ, US Shrenik K. Shah - Metuchen NJ, US Quang T. Truong - Morganville NJ, US
Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin sub-type 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.
Poly(Amide) Polymers For The Delivery Of Oligonucleotides
Stephanie E. Barrett - Perkasie PA, US Steven L. Colletti - Princeton Junction NJ, US Robert M. Garbaccio - Lansdale PA, US Erin N. Guidry - Cranford NJ, US Robert A. Kowtoniuk - Glenside PA, US Jing Liao - Livingston NJ, US Craig A. Parish - Tenafly NJ, US Rubina G. Parmar - Harleysville PA, US Tao Pei - Holmdel NJ, US Kevin M. Schlosser - North Wales PA, US David M. Tellers - Lansdale PA, US Sandra C. Tobias - Lansdale PA, US Quang T. Truong - Morganville NJ, US Jacob H. Waldman - Metuchen NJ, US Weimin Wang - Churchville PA, US J. Michael Williams - Hillsborough NJ, US
International Classification:
A61K 47/48
US Classification:
525 542, 525426
Abstract:
The present invention provides poly(amide) polymers, polyconjugates, compositions and methods for the delivery of oligonucleotides for therapeutic purposes.
Novel Tetragalnac Containing Conjugates And Methods For Delivery Of Oligonucleotides
- Cambridge MA, US Steven COLLETTI - West Point PA, US Vadim DUDKIN - West Point PA, US Norihiro IKEMOTO - Rahway NJ, US Hongbiao LIAO - Rahway NJ, US Craig PARISH - Rahway NJ, US Tao PEI - Rahway NJ, US Anthony SHAW - West Point PA, US Quang TRUONG - Rahway NJ, US Lijun WANG - Whitehouse Station NJ, US Yu YUAN - Orlando FL, US Man ZHU - Rahway NJ, US
International Classification:
C12N 15/113
Abstract:
Disclosed herein is a modular composition comprising 1) an oligonucleotide; 2) one or more tetraGalNAc ligands of Formula (I), which may be the same or different; optionally, 3) one or more linkers, which may be the same or different; and optionally, 4) one or more targeting ligands, solubilizing agents, pharmacokinetics enhancing agents, lipids, and/or masking agents.
C2-Carbocyclic Iminothiazine Dioxides As Bace Inhibitors, Compositions, And Their Use
- Rahway NJ, US Jared N. Cumming - Garwood NJ, US Shuwen He - Fanwood NJ, US Brandon M. Taoka - Hoboken NJ, US Quang T. Truong - Morganville NJ, US
Assignee:
Merck Sharp & Dohme Corp. - Rahway NJ
International Classification:
C07D 487/04 C07D 471/04
Abstract:
In its many embodiments, the present invention provides certain C2-carbocyclic iminothiazine dioxide compounds, including compounds Formula (I); or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R, R, ring A, R, m, ring B, RB, n, ring C, Rand p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.