4-苯基-4-羟基哌啶置于盐酸体系中,化学反应 24.0H,以68%的收率获得4-苯基-1,2,3,6-四氢吡啶 参考文献:Structure-activity Relationship Exploration Of Kv1.3 Blockers Based On Diphenoxylate 标题:Structure-activity Relationship Exploration Of Kv1.3 Blockers Based On Diphenoxylate 摘要:Diphenoxylate,A Well-Known Opioid Agonist And Anti-Diarrhoeal Agent,Was Recently Found To Block Kv1.3 Potassium Channels,Which Have Been Proposed As Potential Therapeutic Targets For A Range Of Autoimmune Diseases. The Molecular Basis For This Kv1.3 Blockade Was Assessed By The Selective Removal Of Functional Groups From The Structure Of Diphenoxylate As Well As A Number Of Other Structural Variations. Removal Of The Nitrile Functional Group And Replacement Of The C-4 Piperidinyl Substituents Resulted In Several Compounds With Submicromolar Ic50 Values. (C) 2012 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2012.09.080
专利信息
专利号:US-RE41998-E 优先权日:1990-02-26 标题 :Compositions and methods of treatment of sympathetically maintained pain 发明人:CAMPBELL JAMES N 权利人:ARCLON THERAPEUTICS INC 摘要:Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.
专利号:US-2011301143-A1 优先权日:2009-02-23 标题 :Heterocyclic derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN 权利人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN 摘要:Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, Câ•?CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.
专利号:WO-0010565-A1 优先权日:1998-08-18 标 题 :Growth hormone secretagogues 发明人:DODGE JEFFREY ALAN; HAUSER KENNETH LEE; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR CHARLES WILLIS III; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROBERT LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE 权利人:LILLY CO ELI; DODGE JEFFREY ALAN; HAUSER KENNETH LEE; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR CHARLES WILLIS III; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROBERT LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE 摘要:This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.
专利号:WO-2010007202-A1 优先权日:2008-07-17 标 题:Enzymatic synthesis of enantiomerically enriched derivatives of cis- and trans-cyclopentane-1,2-diamines
专利号:EP-2319825-A1 优先权日:2008-07-17 标 题 :Enzymatic synthesis of enantiomerically enriched derivatives of cis- and trans-cyclopentane-1,2-diamines
专利号:US-4546177-A 优先权日:1979-02-13 标题:1-(6-Hydroxy-4- or -7-methoxy-5-Benzofuranyl)-4-substituted-1,3-butanediones 发明人:GAMMILL RONALD B 权利人:UPJOHN CO 摘要:The present invention provides novel 1-(6-hydroxy-4- or 7-methoxy or 4,7-dimethoxy-5-benzofuranyl)-4-substituted-1,3-butanediones which are useful as intermediates in the synthesis of khellin and related anti-atherosclerotic furochromones.
摘要:Nairoukh, Z.; Ding, H.; Hu, M., Science of Synthesis: Dearomatizations, (2026) . 参考文献:10.1093/brain/awz176 摘要:Rosenblad C, Li Q, Pioli EY, Dovero S, Antunes AS, Agúndez L, Bardelli M, Linden RM, Henckaerts E, Björklund A, Bezard E, Björklund T. Vector-mediated l-3,4-dihydroxyphenylalanine delivery reverses motor impairments in a primate model of Parkinson's disease. Brain. 2019 Aug 01;142(8):2402–16.