专利号:US-3846399-A 优先权日:1969-04-10 标题:Process for controlled stepwise synthesis of polypeptides 发明人:HIRSCHMANN R; DENKEWALTER R 权利人:MERCK & CO INC 摘要:The invention disclosed herein relates to a novel process for the controlled, stepwise synthesis of polypeptides and proteins. More particularly, it is concerned with a process for the rapid and efficient preparation of polypeptides in which multiple sequential steps are carried out without isolation of intermediate peptides. This process for the controlled stepwise synthesis of polypeptides involves reacting a starting amino acid or peptide (or derivative thereof) with an N-carboxy amino acid anhydride (or derivative thereof) in an aqueous medium under conditions of controlled pH such that the only amino group present in appreciable concentration in reactive form during the course of the reaction is the amino group in the starting amino acid or peptide.
专利号:US-4629784-A 优先权日:1983-08-16 标 题:Synthesis of cyclopropane amino acids 发明人:STAMMER CHARLES H 权利人:UNIV GEORGIA RES FOUND 摘要:Cyclopropane ('Cyclopropyl') amino acids and peptides containing at least one cyclopropyl amino acid are disclosed. The processes for synthesizing cyclopropyl amino acids and peptides containing at least one cyclopropyl amino acid are also disclosed. Cyclopropyl amino acids are useful as enzyme inhibitors and as substitutes for natural amino acids in peptide hormones such as regulators of bodily functions to enhance bioactivity, to stabilize the peptide into which it is incorporated to cleavage by enzymes and to convert such peptides into enzyme inhibitors.
专利号:US-2025197441-A1 优先权日:2023-12-19 标题 :Safety-Catch Linkers for Solid Phase Peptide Synthesis 发明人:ALBERICIO PALOMERA FERNANDO; DE LA TORRE BEATRIZ GARCIA; NOKI SIKABWE; SANEII HOSSAIN 权利人:AAPPTEC LLC 摘要:A safety-catch linker for solid phase peptide synthesis (SPPS) is provided, having a chemical structure according to Formula I:wherein R1 and R2 are each independently selected from hydrogen and methyl; R3 is absent or phenyl; and n is 0 or 1. Also provided are methods of synthesizing the linker, methods of solid phase peptide synthesis (SPPS) of a target peptide employing the resin-bound linker, and kits for SPPS.
专利号:US-2008051323-A1 优先权日:2004-08-21 标 题 :Chloroquine drug compositions and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. n The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
专利号:US-2007060499-A1 优先权日:2005-09-15 标 题 :Chloroquine combination drugs and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
专利号:US-2007166281-A1 优先权日:2004-08-21 标题 :Chloroquine coupled antibodies and other proteins with methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents such as therapeutic antibodies or insulin, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the drug is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a drug directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing the drug for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and antibody or insulin to their site of action.
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合成参考文献
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