专利号:US-12247037-B2 优先权日:2018-12-12 标题:1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4h-benzo[f][1,2,4]triazolo[4,3-A][1,4]diazepine derivatives and related compounds as vasopressin antagonists for the treatment of neuro-psychological disorders 发明人:BRANDT GARY 权利人:NEUMORA THERAPEUTICS INC 摘要:The present invention relates to 1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives and related compounds of Formula (I): wherein A, B, G, R1, R1b, RiC, R2 and X are as defined herein. The present compounds are vasopressin receptor antagonists (in particular of the Via receptor) for the treatment of neuro-psychological disorders, such as e.g. autism, anxiety, stress-related disorders, depression, schizophrenia or bipolar disorder. The present description discloses the synthesis of exemplary compounds, as well as pharmacological data thereof (e.g. pages 71 to 246; examples 1 to 49; tables 1 to 5). An exemplary compound is e.g. 8-chloro-1-(2-(5-fluoropyridin-2-yl)-2,6-diazaspiro[3.3]heptan-6-yl)-5-methyl-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine (example 1, compound no. 1).
专利号:US-2009275727-A1 优先权日:1998-03-24 标题:Peptide turn mimetics 发明人:CASSIDY PETER J; ALEWOOD PAUL FRANCIS; VERNALL ANDREA JOY 权利人:MIMETICA PTY LTD 摘要:This invention provides novel compounds useful for the synthesis of peptide mimetics, and describes the use of these compounds for the synthesis of novel reverse turn mimetics. The reverse turn mimetics of the invention have the general structure X wherein the variables are as defined herein.
专利号:US-2012190648-A1 优先权日:2009-07-23 标 题:Fluorinated cyclopropane analogs of glutamic acid 发明人:JUBAULT PHILIPPE; QUIRION JEAN-CHARLES; LEMONNIER GERALD; LION CEDRIC 权利人:JUBAULT PHILIPPE; QUIRION JEAN-CHARLES; LEMONNIER GERALD; LION CEDRIC 摘要:The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer or a mixture in all proportions of stereoisomers thereof, in particular a mixture of enantiomers, such as a racemic mixture, wherein R represents a (C 1 -C 6 )alkyl or (C 1 -C 6 )alkenyl group, optionally substituted by one or more groups chosen among an halogen atom, OR a , SR b , NR c R d , PO(OR e )(OR f ), CO 2 R g , SO 2 R h SO 3 R 1 , P0(0H)(CH(0H)R k ), CN, N 3 and NH—C(â•?NH)NH2, with R a , R b , R c and R d , representing, independently of each other, an hydrogen atom, a (C 1 -C 6 )alkyl group or a —CO—(C 1 -C 6 )alkyl group, R e , R f , R g , R h and R1 representing, independently of each other, an hydrogen atom or a (C 1 -C 6 )alkyl group, and R k representing an aryl or heteroaryl group, said group being optionally substituted by one or more groups selected from an halogen atom and NO 2 , as well as to the use thereof and to a process for preparing such a compound, to a pharmaceutical composition containing it and to synthesis intermediates.
专利号:US-9351974-B2 优先权日:2011-11-10 标题 :Substituted pteridinones for the treatment of cancer 发明人:JIN MEIZHONG; KADALBAJOO MRIDULA; LI AN-HU; MULVIHILL MARK J; SIU KAM W; STEINIG ARNO G; WANG JING 权利人:OSI PHARMACEUTICALS LLC 摘要:Compounds of Formula I, as shown below and defined herein: n npharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.
专利号:US-8518885-B2 优先权日:2008-02-06 标题 :Heterocyclic peptide ketoamides 发明人:POWERS JAMES C; GLASS JONATHAN D; OVAT ASLI; LI ZHAOZHAO 权利人:POWERS JAMES C; GLASS JONATHAN D; OVAT ASLI; LI ZHAOZHAO; GEORGIA TECH RES INST; UNIV EMORY 摘要:A novel class of peptide α-ketoamides useful for selectively inhibiting calpains, selectively inhibiting cysteine proteases, and generally inhibiting all cysteine proteases, having the formula M-AA 2 -AA 1 -CO—NH—(CH 2 ) n —R 3 . Processes for the synthesis of peptidyl α-ketoamide derivatives. Compositions and methods for inhibiting cysteine proteases, inhibiting calpains, and treating disease caused by cysteine proteases and calpains are provided.
参考标题:1,1-Dioxonaphtho[1,2-B]Thiophene-2-Methyloxycarbonyl (α-Nsmoc) And 3,3-Dioxonaphtho[2,1-B]Thiophene-2-Methyloxycarbonyl (β-Nsmoc) Amino-Protecting Groups 作者:Louis A. Carpino,Adel Ali Abdel-Maksoud,Dumitru Ionescu,E. M. E. Mansour,Mohamed A. Zewail |发布日期:2007.3.1 摘要:Mechanistically Similar To That Previously Established For The Bsmoc Derivative In That The Reaction Is Initiated By Michael Addition To The β-Carbon Atom Of The α,β-Unsaturated Sulfone System. Application Of α- And β-Nsmoc Amino Acids To The Solid-Phase Synthesis Of Two Model Peptides Was Examined. An Advantage Of The α-Nsmoc System Over The Long-Known Bsmoc System Proved To Be The Milder Conditions Needed For