Jeremy I. Levin - New City NY Aranapakam M. Venkatesan - Rego Park NY Derek C. Cole - New City NY James M. Chen - Bedminister NJ Jamie M. Davis - Nyack NY George T. Grosu - Pearl River NY
Compounds of the formula are useful in treating disease conditions mediated by TNF-, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohns disease and degenerative cartilage loss.
N-Hydroxy-2-(Alkyl,Aryl Or Heteroaryl Sulfanyl, Sulfinyl Or Sulfonyl) 3-Substituted Alkyl, Aryl Or Heteroarylamides As Matrix Metalloproteinase Inhibitors
Matrix metalloproteinases (MMps) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF- converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF- from membrane bound TNF- precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF- converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection. The compounds of this invention are represented by the formula where R , R , R and R are described herein.
N-Hydroxy-2-(Alkyl, Aryl, Or Heteroaryl Sulfanyl, Sulfinyl Or Sulfonyl)-3-Substituted Alkyl, Aryl Or Heteroarylamides As Matrix Metalloproteinase Inhibitors
Aranapakam Mudumbai Venkatesan - Rego Park NY George Theodore Grosu - Pearl River NY Jamie Marie Davis - Nyack NY Jannie Lea Baker - White Plains NY Jeremy Ian Levin - New City NY
Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF- from membrane bound TNF- precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (is) and TNF- converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection having the formula wherein R and R form a heterocyclic ring and A is S, S(O), or S(O)2, and R and R are defined herein.
Alkynyl Containing Hydroxamic Acid Compounds As Matrix Metalloproteinase And Tace Inhibitors
Jeremy I. Levin - New City NY Aranapakam M. Venkatesan - Rego Park NY Derek C. Cole - New City NY James M. Chen - Stoddard Court NJ Jamie M. Davis - Nyack NY George T. Grosu - Pearl River NY
Assignee:
Wyeth Holdings Corporation - Madison NJ
International Classification:
C07D21172
US Classification:
546290, 514345, 514352, 514353
Abstract:
Compounds of the formula are useful in treating disease conditions mediated by TNF-, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohns disease and degenerative cartilage loss.
Benzofuranyl-And Benzothienyl-Piperazinyl Quinolines And Methods Of Their Use
Aranapakam Mudumbai Venkatesan - Regopark NY, US Osvaldo Dos Santos - Kew Garden NY, US Magda Asselin - Mahwah NJ, US George Theodore Grosu - Pearl River NY, US Deborah A. Evrard - Hamilton Square NJ, US Richard Eric Mewshaw - King of Prussia PA, US Kristin Meagher - Novi MI, US
Assignee:
Wyeth - Madison NJ
International Classification:
C07D 405/12 C07D 409/12 A61K 31/496
US Classification:
544363, 51425306
Abstract:
Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such compounds are disclosed. Methods of using benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such composition in the treatment and/or prevention of serotonin-related disorders, such as depression and anxiety, are also disclosed. In addition, processes for the preparation of benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives are disclosed. Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives of Formula I are disclosed:.
Piperazine-Piperidine Antagonists And Agonists Of The 5-Ht Receptor
Magda Asselin - Mahwah NJ, US George Theodore Grosu - Pearl River NY, US Annmarie Louise Sabb - Pennington NJ, US Wayne Everett Childers - New Hope PA, US Lisa Marie Havran - Florence NJ, US Zhongqi Shen - Plainsboro NJ, US James Jacob Bicksler - Titusville NJ, US Dan Chaekoo Chong - Plainsboro NJ, US
The present invention relates to novel piperazine-piperidine compounds. The compounds are useful as 5-HT1A binding agents, particularly as 5-HT1A receptor antagonists and agonists. These compounds are useful in treating central nervous system disorders, such as cognition disorders, anxiety disorders, depression and sexual dysfunction. The invention relates to compounds and pharmaceutically acceptable salts of formula (I′):.
Benzofuranyl- And Benzothienyl- Piperazinyl Quinolines And Methods Of Their Use
Aranapakam Mudumbai Venkatesan - Regopark NY, US Osvaldo Dos Santos - Kew Garden NY, US Magda Asselin - Mahwah NJ, US George Theodore Grosu - Pearl River NY, US Deborah A. Evrard - Hamilton Square NJ, US Richard Eric Mewshaw - King of Prussia PA, US Kristin Meagher - Novi MI, US
Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such compounds are disclosed. Methods of using benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such composition in the treatment and/or prevention of serotonin-related disorders, such as depression and anxiety, are also disclosed. In addition, processes for the preparation of benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives are disclosed.
3-Substituted-1H-Pyrrolo[2,3-B]Pyridine And 3-Substituted-1H-Pyrrolo[3,2-B]Pyridine Compounds, Their Use As Mtor Kinase And Pi3 Kinase Inhibitors, And Their Syntheses
Gary Harold Birnberg - Tuxedo Park NY, US Gloria Jean MacEwan - Monroe NY, US Matthew Gregory Bursavich - Salt Lake City UT, US Sabrina Lombardi - New Haven CT, US Nan Zhang - Bayside NY, US Adam Matthew Gilbert - Congers NY, US George Theordore Grosu - Pearl River NY, US Natasja Brooijmans - New York NY, US Thai Hiep Nguyen - Fair Lawn NJ, US