专利号:WO-9837078-A1 优先权日:1997-02-20 标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-10458995-B2 优先权日:2016-03-25 标 题 :Combinatorial synthesis and biomarker development 发明人:MOOLA MURALIDHAR REDDY 权利人:MOOLA MURALIDHAR REDDY 摘要:Provided herein are methods, kits, and compositions for use in the diagnosis and treatment of diseases. Peptoids recognized by Alzheimers disease specific antibodies are identified.
专利号:US-9920336-B2 优先权日:2012-12-31 标 题:Methods of producing 7-carbon chemicals from long chain fatty acids via oxidative cleavage 发明人:PEARLMAN PAUL S; CONRADIE ALEX VAN ECK; CHEN CHANGLIN; BOTES ADRIANA LEONORA 权利人:INVISTA NORTH AMERICA SARL 摘要:This document describes biochemical pathways for producing pimelic acid, 7-aminoheptanoic acid, 7-hydroxyheptanoic acid, heptamethylenediamine or 1,7-heptanediol by forming two terminal functional groups, comprised of carboxyl, amine or hydroxyl group, in a C7 aliphatic backbone substrate. These pathways, metabolic engineering and cultivation strategies described herein rely on the fatty acid synthesis pathway and oxidative cleavage of long chain acyl-[acp] intermediates by a monooxgenase (e.g., cytochrome P450) such as that encoded by BioI from microorganisms such as Bacillus subtillis.
专利号:US-9580731-B2 优先权日:2012-12-31 标 题:Methods of producing 7-carbon chemicals via c1 carbon chain elongation associated with coenzyme B synthesis 发明人:BOTES ADRIANA LEONORA; CONRADIE ALEX VAN ECK; CHEN CHANGLIN; PEARLMAN PAUL S 权利人:INVISTA NORTH AMERICA S Ã R L; INVISTA NORTH AMERICA SARL 摘要:This document describes biochemical pathways for producing pimelic acid, 7-aminoheptanoic acid, 7-hydroxyheptanoic acid, heptamethylenediamine or 1,7-heptanediol by forming one or two terminal functional groups, each comprised of carboxyl, amine or hydroxyl group, in a C7 aliphatic backbone substrate. These pathways, metabolic engineering and cultivation strategies described herein rely on the C1 elongation enzymes or homolog associated with coenzyme B biosynthesis.
专利号:US-9637764-B2 优先权日:2012-12-31 标题:Methods of producing 7-carbon chemicals via carbon chain elongation associated with cyclohexane carboxylate synthesis 发明人:BOTES ADRIANA LEONORA; CONRADIE ALEX VAN ECK; CHEN CHANGLIN; PEARLMAN PAUL S 权利人:INVISTA NORTH AMERICA S Ã R L; INVISTA NORTH AMERICA SARL 摘要:This document describes biochemical pathways for producing pimelic acid, 7-aminoheptanoic acid, 7-hydroxyheptanoic acid, heptamethylenediamine or 1,7-heptanediol by forming two terminal functional groups, comprised of carboxyl, amine or hydroxyl group, in a C7 aliphatic backbone substrate. These pathways, metabolic engineering and cultivation strategies described herein rely on the carbon chain elongation enzymes or homologs thereof associated with the cyclohexane carboxylate biosynthesis from Syntrophus aciditrophicus or 2-aminoadipate lysine biosynthesis.
专利号:CN-117070502-A 优先权日:2023-08-08 标 题 :A deacetylase mutant and its application in the synthesis of clethodim intermediates
参考文献:10.1007/s00726-023-03269-2 摘要:Sánchez M, Suárez L, Banda G, Barreiro-Alonso E, Rodríguez-Uña I, Rubín JM, Cantabrana B. Age-associated polyamines in peripheral blood cells and plasma in 20 to 70 years of age subjects. Amino Acids. 2023 Jun;55(6):789–98.