专利号:US-8598153-B2 优先权日:2006-09-22 标题 :Method of treatment using fatty acid synthesis inhibitors 发明人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN 权利人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN; MERCK SHARP & DOHME 摘要:The present invention relates to natural products that possess fatty acid synthesis inhibitor activity and can be used to treat and prevent diseases such as obesity, cancer, diabetes, fungal infections, Mycobacterium tuberculosis infections, malarial infections and other apicomplexan protozoal diseases.
专利号:WO-2008022467-A1 优先权日:2006-08-25 标 题 :2-substituted azain doles and 2 substituted thienopyrroles, their precursors and novel processes for the preparation thereof 发明人:LAUTENS MARK; YUEN JOSEPHINE; FANG YUANQING 权利人:LAUTENS MARK; YUEN JOSEPHINE; FANG YUANQING 摘要:The present invention relates generally to processes for the chemical synthesis of azaindole and thienopyrrole compounds, in particular azaindole and thienopyrrole compounds that are substituted at the 2-position of the azaindole or thienopyrrole ring, and optionally at additional locations of the azaindole or thienopyrrole ring such as the 1- and/or 3-position, compounds prepared by such processes, and synthetic precursors of such processes. More particularly, the present invention relates to the preparation of 2- substituted azaindoles from an ortho-gem-dihalovinylaminopyridine or from an ortho- gem-dihalovinylaminopyridine N-oxide compound and an organoboron reagent using a palladium metal pre-catalyst, base and a ligand. The present invention also relates to the preparation of 2-substituted thienopyrroles from an ortho-gem-dihalovinylthiophene compound and an organoboron reagent using a palladium metal pre-catalyst, base and a ligand. The present invention also relates to processes for the production of ortho-gem- dihalovinylaminopyridines which are useful as starting materials in the production of 2- substituted azaindoles, and novel compounds prepared by the processes. The present invention also relates to processes for the production of ortho-gem-dihalovinylthiophenes which are useful as starting materials in the production of 2-substituted thienopyrroles, and novel compounds prepared by the processes. Formulae (V) and (VII).
专利号:EP-1501503-B1 优先权日:2002-05-09 标 题:Substantially pure solid form of the enol tautomer of 3-indolypyruvic acid for use in the treatment of central nervous system disturbances 发明人:POLITI VINCENZO; SELLA ANTONIO; BARTOLINI BARBARA; MARGONELLI ANDREA; SOMMA FRANCESCA; CORNIELLO CRISTINA 权利人:POLIFARMA SPA 摘要:The enol tautomer of 3-indolylpyruvic acid in stable and pure form, as well as alkali and alkali-earth salts thereof are produced by synthesis process. The enol tautomer comprises only the geometric isomer (Z) and it is the only one tautomeric form having relevant pharmacological effects. The compounds obtained exhibited relevant biochemical and pharmacological properties in pathological situations like anxiety, depression, behaviour disturbances, neuronal degenerations, etc.
专利号:RU-2198875-C2 优先权日:1997-05-15 标 题:Methods of synthesis of pyridine-2-carboxaldehyde thiosemicarbazones and intermediate pyridine-2-carboxaldehydes
专利号:CN-119638694-A 优先权日:2018-11-16 标 题 :Improved synthesis of key intermediates for KRAS G12C inhibitor compounds
专利号:CN-114728960-B 优先权日:2019-11-14 标 题:Improved synthesis of KRAS G12C inhibitor compounds
摘要:Walker, J. C. L., Science of Synthesis: Knowledge Updates, (2024) 3, 210. 参考文献:10.1208/pt020314 摘要:Krishna G, Hodnick WF, Lang W, Lin X, Karra S, Mao J, Almassian B. Pharmaceutical development and manufacturing of a parenteral formulation of a novel antitumor agent, VNP40101M. AAPS PharmSciTech. 2001 Aug 26;2(3):E14.