专利号:US-12319677-B2 优先权日:2019-09-25 标 题:Process for the production of 5-(4-((2S,5S)-5-(4-chlorobenzyl)-2-methyl-morpholino)piperidin-1-yl)-1H-1,2,4-triazol-3-amine 发明人:WITKOWSKI GRZEGORZ; MAGDYCZ MARTA; TYSZKIEWICZ MAGDALENA; ZAKRZEWSKI MARCIN; PIKUL STANISÅ?AW 权利人:MOLECURE S A 摘要:The present invention relates to a process for the synthesis of 5-(4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)piperidin-1-yl)-1H-1,2,4-triazol-3-amine in two hydrated crystalline forms and in one anhydrous crystalline form. The present invention further relates to methyl (Z)-4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)-N-cyanopiperidine-1-carbimidothioate which is an intermediate in this process.
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:WO-2023191400-A1 优先权日:2022-04-01 标题:Ethyl piperidine triazolo triazine derivatives, synthesis method therefor, and pharmaceutical composition containing same for prevention or treatment of cancer 发明人:JI SEUNGHEE; BYUN JOONSEOK; KIM JIWON; KIM DOYOUNG; KIM SEOHYUN; LEE JONGHYUN; JUNG SEUNGHEE; CHOI JONGRYOUL; KO DONG-HYUN; KIM DONGKYU; SON SEO HYUN; KANG JI YOON; JANG HYU JEONG; AHN SANG YEOP; KIM JI YONG; LEE SEO JIN 权利人:HK INNO N CORP; FUTURE MEDICINE CO LTD 摘要:The present invention relates to an ethyl piperidine triazolo triazine derivative, a synthesis method therefor, and a pharmaceutical composition including same for the prevention or treatment of cancer. Acting as an antagonist on an adenosine A2A receptor (A2AR), the derivative can exhibit efficacy for the prevention or treatment of various A2AR-related diseases, specifically, various cancers. When used in combination therapy with an immune checkpoint inhibitor, the derivative is expected to exhibit a remarkable synergistic effect in terms of anticancer activity.
专利号:US-11608340-B2 优先权日:2014-11-17 标 题 :Nanomaterial compositions, synthesis, and assembly 发明人:CHEN QIAN; YU HONGCHUAN; CHEN YUPENG 权利人:RHODE ISLAND HOSPITAL 摘要:Compositions or an assembly of a series of biomimetic compounds include chemical structures that mimic or structurally resemble a nucleic acid base pair. Complexes of nanotubes and agents are useful to deliver agents into the cells or bodily tissues of individuals for therapeutic and diagnostic purposes. Exemplary compounds include those of Formula (I), (III), (V) or (VII), or of Formula (II), (IV), (VI) or (VIII).
专利号:WO-0009116-A1 优先权日:1998-08-14 标 题:Grp receptor ligands 发明人:XIANG JIA-NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 权利人:SMITHKLINE BEECHAM CORP; XIANG JIA NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV 摘要:Novel GRP receptor antagonists are provided. Methods of using the present compounds to antagonize GRP receptors are also provided. The present invention further involves the synthesis of the present compounds.
专利号:US-2009291955-A1 优先权日:2005-11-15 标题 :Azacyclohexane Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase 发明人:CRANE SHELDON N; ROBICHAUD JOEL STEPHANE; LEGER SERGE; RAMTOHUL YEEMAN K 权利人:CRANE SHELDON N; ROBICHAUD JOEL STEPHANE; LEGER SERGE; RAMTOHUL YEEMAN K 摘要:Azacyclohexane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
[参考文献]: D Z Hung, Et Al. Dermatitis Caused By Dimethyl Cyanocarbonimidodithioate. J Toxicol Clin Toxicol. 1992;30(3):351-8.
合成参考文献
摘要:Shimada, K., Science of Synthesis Knowledge Updates, (2010) 1, 417. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 271. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 235.