专利号:US-6683189-B1 优先权日:1996-02-26 标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support 发明人:DERVAN PETER B; BAIRD ELDON 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
专利号:US-11945838-B2 优先权日:2018-12-20 标 题:Method for synthesis of protein amphiphiles 发明人:BRITTO Sandanaraj Selvaraj; REDDY Mullapudi Mohan 权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES 摘要:The present invention discloses a novel cost effective method for synthesis of protein/peptide amphiphiles irrespective of functional and structural classification of proteins useful in designing a vaccine candidate from antigenic protein. The protein modification of the present invention is universal and hence any protein/peptide can be converted into amphiphilic proteins/peptides.
专利号:EP-4092127-A1 优先权日:2021-05-18 标题:Enzyme-catalytic method for the direct stereoselective synthesis of gamma-(acyloxy) carboxylic acids 发明人:PARVE JAAN; KUDRJASHOVA MARINA; GATHERGOOD NICHOLAS; PARVE OMAR 权利人:TALLINN UNIV OF TECHNOLOGY 摘要:The present invention is a method for the stereoselective straightforward synthesis of gamma-acyloxy carboxylic acids of novel structure starting from racemic gamma-hydroxy carboxylic acid salts that are obtained by alkaline hydrolysis of the racemic gamma-lactones. The salt is acylated by enzyme catalysis in an organic solvent containing an acyl donor and an immobilised lipase, on stirring at room temperature (ca 20 °C) until reaching the conversion rate required. After that, the reaction mixture is acidified and extracted and the product treated with catalytic amount of para-toluenesulfonic acid in toluene during the time required for the relactonisation of the unreacted salt enantiomer. Thereafter, the target gamma-acyloxy carboxylic acid formed from one enantiomer of the starting compound and relactonised gamma-lactone formed from the other, unreacted enantiomer of the starting compound are isolated using a routine separation method, such as distillation, extraction with NaHCO3 water solution followed by acidification or column chromatography.
专利号:WO-9312076-A1 优先权日:1991-12-13 标题:Reagents for automated synthesis of peptide analogs 发明人:WEBB THOMAS ROY 权利人:CORVAS INT INC 摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.
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-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
参考文献:10.1245/s10434-010-0956-9 摘要:Iwasaki Y, Sunaga N, Tomizawa Y, Imai H, Iijima H, Yanagitani N, Horiguchi K, Yamada M, Mori M. Epigenetic inactivation of the thyroid hormone receptor beta1 gene at 3p24.2 in lung cancer. Ann Surg Oncol. 2010 Aug;17(8):2222–8. doi: 10.1245/s10434-010-0956-9. 参考文献:10.1007/s11596-010-0115-3 摘要:Shou Z, Shen L, Xiong P. Assessing the validity of a novel model of vertebral artery type of cervical syndrome induced by injecting sclerosing agent next to transverse process of cervical vertebra. J Huazhong Univ Sci Technolog Med Sci. 2010 Feb;30(1):85–8. doi: 10.1007/s11596-010-0115-3. 参考文献:10.1007/s00249-011-0726-z 摘要:Idiong G, Won A, Ruscito A, Leung BO, Hitchcock AP, Ianoul A. Investigating the effect of a single glycine to alanine substitution on interactions of antimicrobial peptide latarcin 2a with a lipid membrane. Eur Biophys J. 2011 Sep;40(9):1087–100. doi: 10.1007/s00249-011-0726-z. 参考文献:10.1007/s00128-011-0360-6 摘要:Yi X, Kim E, Jo H, Han T, Jung J. A Comparative Study on Toxicity Identification of Industrial Effluents Using Daphnia magna. Bulletin of Environmental Contamination and Toxicology. 2011 Jul 15;87(3):319. doi: 10.1007/s00128-011-0360-6. 参考文献:10.1007/s00726-011-0975-2 摘要:Danger G, Charlot S, Boiteau L, Pascal R. Activation of carboxyl group with cyanate: peptide bond formation from dicarboxylic acids. Amino Acids. 2012 Jun;42(6):2331–41. doi: 10.1007/s00726-011-0975-2.