专利号:US-2025129050-A1 优先权日:2022-01-26 标 题 :Synthesis of a kif18a inhibitor 发明人:CAILLE SEBASTIEN; GREENE DANIEL GERARD; CORBETT MICHAEL THOMAS; WEI CAROLYN 权利人:AMGEN INC 摘要:The present invention relates to improved preparation of a KIF18A inhibitor having the chemical structure Compound (1), or a salt thereof Compound (la); wherein HA is as defined herein; and key intermediates thereof, i.e., Compound (2a), Compound (3a), Compound (5) or a salt thereof, and Compound (6a) or a hydrate thereof, of the formulae: Compound (2a); Compound (3a); Compound (5) or a salt thereof; and Compound (6a) or a hydrate thereof, preferably Compound (6a-1). The present invention further relates to solid form of Compound (6a), preferably the crystalline hydrate form of Compound (6a-1).
专利号:US-2011053983-A1 优先权日:2008-04-23 标 题:(5r)-1,5-diaryl-4,5-dihydro-1h-pyrazole-3-carboxamidine derivatives having cb1-antagonistic activity 发明人:LANGE JOSEPHUS H M; DEN HARTOG ARNOLD P; VAN VLIET BERNARD J 权利人:LANGE JOSEPHUS H M; DEN HARTOG ARNOLD P; VAN VLIET BERNARD J 摘要:Embodiments of the invention relate to (5R)-1,5-diaryl-4,5-dihydro-1H-pyrazole-3-carboxamidine derivatives as cannabinoid-CB 1 receptor antagonists, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said dihydropyrazole derivatives, to methods for the preparation of these intermediates, pharmaceutical compositions containing one or more of these dihydropyrazole derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders involving cannabinoid receptors. The compounds of embodiments of the invention are compounds of formula (I) wherein the symbols have the meanings given in the specification.
专利号:US-2011172274-A1 优先权日:2008-06-16 标 题 :Fluoro-substituted 3,4-diaryl-4,5-dihydro-1h-pyrazole-1-carboxamidine derivatives having cb1-antagonistic activity 发明人:LANGE JOSEPHUS H M; VLIET VAN BERNARD J 权利人:LANGE JOSEPHUS H M; VLIET VAN BERNARD J 摘要:This invention concerns fluorinated 3,4-diaryl-4,5-dihydro-1H-pyrazole-1-carboxamidine derivatives as cannabinoid-CB 1 receptor antagonists, methods for preparing these compounds, novel intermediates useful for the synthesis of said compounds, methods for the preparation of these intermediates, pharmaceutical compositions containing one or more of these dihydropyrazole derivatives as active ingredient, as well as the use of these pharmaceutical compositions for the treatment of obesity and obesity-related cardiovascular disorders, drug addiction, cognition deficits, liver fibrosis and inflammatory disorders. The compounds have the general formula (I) n n n n n n n n n n wherein the symbols have the meanings given in the specification.
专利号:US-11279687-B2 优先权日:2010-09-03 标题:Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; YUEN PO-WAI 权利人:VALO HEALTH INC; GENENTECH INC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An embodiment of the invention is the provision of a compound of Formula IIIA.
专利号:US-8404670-B2 优先权日:2009-02-11 标题:Histamine H3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:JP-2025505892-A 优先权日:2022-01-26 标 题 :Synthesis of KIF18A inhibitors
参考文献:10.1007/s00044-020-02677-3 摘要:Hwang N, Ban H, Chen J, Ma J, Liu H, Lam P, Kulp J, Menne S, Chang J, Guo J, Du Y. Synthesis of 4-oxotetrahydropyrimidine-1(2H)-carboxamides derivatives as capsid assembly modulators of hepatitis B virus. Medicinal Chemistry Research. 2021 Jan 11;30(2):459–72. doi: 10.1007/s00044-020-02677-3.