专利号:US-6271375-B1 优先权日:1997-06-30 标 题 :Ortho-metalation process for the synthesis of 2-substituted-1-(tetrazol-5-yl)benzenes 发明人:VILLA MARCO; ALLEGRINI PIETRO; ARRIGHI KATIUSCIA; PAIOCCHI MAURIZIO 权利人:ZAMBON SPA 摘要:A process of direct metalation of phenyltetrazoles useful for preparing compounds of formula (II) intermediates for the synthesis of angiotensin II antagonists is described.
专利号:US-9453044-B2 优先权日:2012-02-07 标题 :Method of synthesizing peptides, proteins and bioconjugates 发明人:LIU CHUAN FA; ZHAO JUNFENG 权利人:UNIV NANYANG TECH 摘要:The invention relates to the synthesis of peptides, proteins and related bioconjugates, and in particular, to such synthesis using a peptide ligation method whereby a C-terminal salicylaldehyde ester peptide is reacted with an aminoacyl-N-hydroxl peptide. The invention also relates to the synthesis of cyclic peptides, including serinyl- or threonyl-containing cyclic peptides. The invention further relates to a solid phase synthesis of C-terminal salicylaldehyde ester peptides.
专利号:US-7781488-B2 优先权日:2002-06-10 标 题:Post-cleavage sulfur deprotection for convergent protein synthesis by chemical ligation 发明人:BOTTI PAOLO; VILLAIN MATTEO; MANGANIELLO SONIA; GAERTNER HUBERT 权利人:AMYLIN PHARMACEUTICALS INC 摘要:The present invention provides a method and compositions for synthesizing an oligopeptide or polypeptide by convergent assembly of a plurality of pairs of oligopeptides in chemical ligation reactions. An important aspect of the present invention is an oligopeptide having a C-terminal disulfide-protected carboxythioester group that can be deprotected to spontaneously generate a free C-terminal thioester moiety. This allows a single precursor to participate in a succession of chemical ligation reactions, thereby making the convergent synthesis approach possible. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins, and improves the efficiency of native chemical ligation reactions, particularly where four or more peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.
专利号:WO-9519967-A1 优先权日:1994-01-21 标 题:A process for the preparation of 3-(substituted phenyl) pyrazole derivatives 发明人:BANSAL HARJINDER SINGH; BARNETT SUSAN PATRICIA; CHRYSTAL EWAN JAMES TURNER; ROGERS MICHAEL LOUIS 权利人:ZENECA LTD; BANSAL HARJINDER SINGH; BARNETT SUSAN PATRICIA; CHRYSTAL EWAN JAMES TURNER; ROGERS MICHAEL LOUIS 摘要:A process for the synthesis of a herbicide of general formula (I), wherein X is halogen or cyano; Y is H, alkyl, alkenyl or alkynyl, any of which may optionally be substituted, cyano, nitro, halogen, NR?10R11, OR10, SO¿pR10, CO2R?10, CONR10R11, NR10SO¿2R?11, COR10, C(NOR10)R11, OSO¿pR?10 or NR10COR11; R1¿ is hydrogen or alkyl, alkenyl, alkynyl, benzyl, cycloalkyl or cycloalkenyl, any of which may optionally be substituted; R2 is lower haloalkoxy; and R3 is halogen; from a compound of general formula (II), wherein X and Y are as defined above and R4 is lower alkyl; comprises the steps of: (i) reacting the compound of formula (II) with a hydrazine derivative; (ii) reacting the product with a compound R9-Z where R9 is a lower haloalkyl group and Z is a leaving group in the presence of a base; and (iii) halogenating the product to give a compound of formula (I).
专利号:WO-2024020091-A1 优先权日:2022-07-19 标 题 :Inhibitors of short-chain dehydrogenase activity for reducing glial fibrillary acidic protein levels 发明人:MARKOWITZ SANFORD; PIEPER ANDREW 权利人:UNIV CASE WESTERN RESERVE; THE US GOV AS REPRESENTED BY THE DEPARTMENT OF VETERAN AFFAIRS 摘要:A method of decreasing blood glial fibrillary acidic protein (GFAP) levels in a subject in need thereof includes administering to the subject a therapeutically effective amount of a 15-PGDH inhibitor. Astroglia cells are the major and perhaps most abundant cell types in the brain. In healthy brain, astrocytes help with providing structural and network support for neurons and interface with the brain vasculature, including the blood-brain-barrier. Functionally, astrocytes are involved with providing neurotrophic factors (such as glial derived neurotrophic factor (GDNF)), and cytokine/chemokine release that influences the global and local inflammatory response environments, as well as working closely with neurons involved in the glutamate-glutamine synthesis/recycling pathway.
专利号:US-7732605-B2 优先权日:2005-03-29 标题 :Synthesis of diketopiperazines 发明人:HAYASHI YOSHIO 权利人:NEREUS PHARMACEUTICALS INC 摘要:Disclosed herein are methods for synthesizing diketopiperazines with enantiomeric excess by inducing cyclization of an α-keto acid with an acid catalyst.
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