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: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-2023151034-A1 优先权日:2020-03-17 标题:Peptidomimetic n5-methyl-n2-(nonanoyl-l-leucyl)-l-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds as inhibitors of norovirus and coronavirus replication 发明人:JACOBSON IRINA C; LEE SAM SK; PIZARRO NOVOA JUAN CARLOS 权利人:COCRYSTAL PHARMA INC 摘要:Peptidomimetic N5-methyl-N2-(nonanoyl-L-leucyl)-L-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds for use in methods of inhibiting the replication of noroviruses and coronaviruses in a biological sample or patient, for use in reducing the amount of noroviruses or coronaviruses in a biological sample or patient, and for use in treating norovirus and coronavirus in a patient, comprising administering to said biological sample or patient a safe and effective amount of a compound represented by formulae I or II, or a pharmaceutically acceptable salt thereof. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. page 99 to page 271; examples 1 to 3; compounds A1 to A104 and B1 to B66; tables A to E).
专利号:US-7629488-B2 优先权日:2005-03-14 标 题 :Process for the preparation of opioid modulators 发明人:CAI CHAOZHONG; HE WEI 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to novel processes for the preparation of opioid modulators (agonists and antagonists) and intermediates in their synthesis. The opioid modulators are useful for the treatment and prevention of as pain and gastrointestinal disorders.
专利号:CN-111909067-A 优先权日:2020-08-28 标题 :A kind of organic total synthesis method of D-penicillamine
专利号:CN-111909067-B 优先权日:2020-08-28 标 题:A kind of organic total synthesis method of D-penicillamine
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合成参考文献
摘要:Fowler, L. S.; Sutherland, A., Science of Synthesis Knowledge Updates, (2010) 3, 136. 摘要:Primer, D. N.; Molander, G. A., Science of Synthesis, (2019) , 313.