专利号:US-7230101-B1 优先权日:2002-08-28 标 题:Synthesis of methotrexate-containing heterodimeric molecules 发明人:MURTHI KRISHNA K; SMITH CHASE C 权利人:GPC BIOTECH INC 摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:
专利号:US-2021130409-A1 优先权日:2017-09-01 标 题 :Method for the Solid-Phase Synthesis of Cyclic Pentapeptides 发明人:ZHENGGUO JIANG; LUCIANO FORNI; ROBERTSON ALAN 权利人:Alsonex Pty Ltd 摘要:A method for the synthesis of a cyclic ornithine-proline-D-cyclohexylalanine-tryptophan-arginine pentapeptide of Formula A; n n n n n n n n n n n n wherein R 1 and R 2 are, independently, —H, or —C(O)R 3 where R 3 is —CH 2 Ph, —CH 2 CH 2 Ph, —CHâ•?CHPh, —C(NHAC)CH 2 Ph;n nthe method comprising the steps of;n nforming a linear proline-D-cyclohexylalanine-tryptophan-arginine-ornithine pentapeptide of Formula B, attached to a polymeric resin;n n n n n n n n n n n n n n n n n wherein R 1 is as for Formula A, RES indicates the polymeric resin, and P 1 and P 2 are protecting groups;n ncyclising the linear pentapeptide of Formula B to form a cyclic pentapeptide of Formula C, attached to the polymeric resin;n n n n n n n n n n n n n n n cleaving the cyclic peptide of Formula C from the resin providing a cleaved cyclic pentapeptide having a free amine group of an ornithine residue;n noptionally substituting the free amine group of the ornithine residue of the cleaved cyclic peptide;n nremoving the protecting groups P 1 and P 2 , to providethe cyclic peptide of Formula A.
专利号:US-8546532-B2 优先权日:2008-04-17 标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders 发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS 权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC 摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
专利号:US-6117974-A 优先权日:1991-10-02 标题:Libraries of backbone-cyclized peptidomimetics 发明人:GILON CHAIM; HORNIK VERED 权利人:PEPTOR LTD; YISSUM RES DEV CO 摘要:Libraries of novel backbone-cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units used in the synthesis of these backbone-cyclized peptide analogs are N(((-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N(((-functionalized) amino acids are incorporated into a library of peptide sequences, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by libraries of backbone-cyclized bradykinin analogs, somatostatin analogs, BPI analogs and Substance P analogs having biological activity. Further embodiments of the invention are Interleukin-6 receptor derived peptides having ring structures involving backbone cyclization.
专利号:US-2015148524-A1 优先权日:2012-07-06 标题:Amino acid analogues and methods for their synthesis 发明人:WANG ZHEN; ROBINSON ANDREA; SPICCIA NICOLAS DANIEL; JACKSON WILLIAM ROY 权利人:UNIV MONASH 摘要:A method for the synthesis of an amino acid analogue or a salt, solvate, derivative, isomer or tautomer thereof comprising the steps of: (i) subjecting an amino acid containing a metathesisable group to metathesis with a compound containing a complementary metathesisable group of formula (I) or (II): (Formulae (I), (II)) wherein R 1 and R 2 are independently selected from H and substituted or unsubstituted C 1 to C 4 alkyl; each R 3 is either absent or independently selected from a heteroatom, a substituted or unsubstituted C 1 to C 20 alkyl, and a substituted or unsubstituted C 1 to C 20 alkyl group interrupted by one or more heteroatoms; and each X is independently selected from H and an effector molecule; in the presence of a reagent to catalyse the metathesis to form a dicarba bridge between the amino acid containing a metathesisable group and the compound containing a complementary metathesisable group; and (ii) reducing the dicarba bridge to form a saturated dicarba bridge, wherein the reagent used to catalyse step (i) also catalyses step (ii).
专利号:US-2006052577-A1 优先权日:2001-02-06 标题:Methods of synthesis of polymers and copolymers from natural products 发明人:SWIFT GRAHAM; WESTMORELAND DAVID G; HUGHES KATHLEEN 权利人:SWIFT GRAHAM; WESTMORELAND DAVID G; HUGHES KATHLEEN 摘要:Described are polymers and copolymers containing sorbitol, citric acid, starch, aspartic acid, succinic anhydride, adipic acid mixtures thereof, methods of their synthesis and their uses.
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合成参考文献
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