专利号:US-4105651-A 优先权日:1976-03-15 标 题:Purification of enkephalin, an endogenous composition in the human body and synthesis of same 发明人:HUGHES JOHN 权利人:US HEALTH EDUCATION & WELFARE 摘要:The purification of an endogenous composition isolated from mammalian brain tissue and termed enkephalin ('in the head'). Enkephalin is recovered from brain tissue by acetone solution and purified by means of column and thin layer chromatography. The composition which is a mixture of two pentapeptides, namely, (a) H-Tyr-Gly-Gly-Phe-Met-OH and (b) H-Tyr-Gly-Gly-Phe-Leu-OH wherein the ratio of a:b is from 3:1 to 4:1 has been found to be a non-addictive narcotic and an opiate agonist. n The synthesis of the pentapeptide composition from the known structure above is accomplished by conventional solution techniques of protection of the amino groups, such as t-butyloxycarbonyl, benzyloxycarbonyl, and t-amyloxycarbonyl, or the solid phase peptide synthesis of R. Bruce Merrifield using a polymeric support and the same or similar amine protecting groups.
专利号:US-11571456-B2 优先权日:2017-05-23 标题 :Process for the linear synthesis of gram-positive class II bacteriocins and compositions and uses thereof 发明人:BÉDARD FRANÇOIS; BIRON ÉRIC; HAMMAMI RIADH; FLISS ISMAIL 权利人:UNIV LAVAL 摘要:A process for the linear synthesis of a gram-positive class II bacteriocin or a variant thereof is disclosed herein. The process comprises the stepwise addition of selected amino acids to a solid support; pseudoproline positioning and reopening; and cleavage of the gram-positive class II bacteriocin or the variant thereof from the solid support to provide a linear gram-positive class II bacteriocin or variant thereof; and in situ disulfide bond formation. Various applications and uses of the synthetic bacteriocins are also disclosed. The synthetic process can also be used to synthesize variants of bacteriocins by the selective substitution of one or more amino acids and/or additions and/or deletions of selected amino acids.
专利号:US-2023337702-A1 优先权日:2017-05-23 标 题 :Process for the linear synthesis of gram-positive class ii bacteriocins and compositions and uses thereof 发明人:BÉDARD FRANÇOIS; BIRON ÉRIC; HAMMAMI RIADH; FLISS ISMAIL; RENAUD ARIANE; DALLAIRE LAURENT 权利人:UNIV LAVAL 摘要:A process for the linear synthesis of a gram-positive class II bacteriocin or a variant thereof is disclosed herein. The process comprises the stepwise addition of selected amino acids to a solid support; pseudoproline positioning and reopening; and cleavage of the gram-positive class II bacteriocin or the variant thereof from the solid support to provide a linear gram-positive class II bacteriocin or variant thereof; and in situ disulfide bond formation. Various applications and uses of the synthetic bacteriocins are also disclosed. The synthetic process can also be used to synthesize variants of bacteriocins by the selective substitution of one or more amino acids and/or additions and/or deletions of selected amino acids.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-4794150-A 优先权日:1987-03-11 标题:Synthesis of peptide analogs 发明人:STEEL SAMUEL 权利人:STEEL SAMUEL 摘要:A novel polymeric disc, wafer or similarly shaped resin for carrying out the synthsis of peptide analogs via solid phase peptide synthesis techniques is provided. The polymeric disc or wafer of the invention may be made out of those resin materials presently used in bead form in solid phase peptide synthesis, such as, benzhydrylamine resins, Boc-aminoacyl-4-(oxymethyl)-phenyacetamidomethyl (Pam) resin, polyamide resins and chloromethyl resins. The disc or wafer of the invention should, preferably, have a thickness of 200-400 μm and may be of any suitable length or width. A process for the synthsis of peptide analogs utilizing the polymeric disc or wafer of the present invention is also disclosed.
专利号:US-2017165371-A1 优先权日:2017-02-22 标 题:Novel synthesis of potential ester prodrugs 发明人:GOLDBERG JOEL STEVEN 权利人:GOLDBERG JOEL STEVEN 摘要:Esters prodrugs that cross the blood brain barrier can be ideal drugs for treatment of diseases of the central nervous system because the cerebral spinal fluid contains an abundance of esterases. The prodrug can be hydrolyzed into an active drug and a metabolite such as cholesterol that is known to be non-toxic and is familiar to the central nervous system. This invention describes a modification of the Fischer-Speier or Fischer esterification reaction in which one reagent is lipophilic and the other reagent is hydrophilic. The reaction occurs in a heterogeneous mixture. The preferred catalyst is 1.0 M hydrochloric acid and the preferred solvent is acetone. The presence of ester synthesis was confirmed by the hydroxamic acid-ferric perchlorate reaction. The synthesis can be conducted without chemical scaffolds and without protecting functional groups.
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