专利号:WO-2011090968-A1 优先权日:2010-01-22 标题:Post-synthetic chemical modification of rna at the 2'-position of the ribose ring via 'click' chemistry 发明人:ZEWGE DANIEL; GOSSELIN FRANCIS 权利人:MERCK SHARP & DOHME; ZEWGE DANIEL; GOSSELIN FRANCIS 摘要:This invention relates to the post-synthetic chemical modification of RNA at the 2'-position on the ribose ring via a copper catalyzed Huisgen cycloaddition ('click' chemistry: Kolb, Sharpless Drug Discovery Today 2003, 8, 1128). The invention 1) avoids complex, tedious multi-step syntheses of each desired modified ribonucleoside; 2) allows diverse chemical modifications using high-fidelity chemistry that is completely orthogonal to commonly used alkylamino, carboxylate and disulfide linker reactivities; 3) allows introduction of functional groups that are incompatible with modern automated solid-phase synthesis of RNA and subsequent cleavage-deprotection steps; 4) allows introduction of functional groups useful as targeting ligands; and 5) enables high-throughput structure-activity relationship studies on chemically modified RNA in 96-well format.
专利号:US-11173212-B2 优先权日:2017-09-28 标 题 :Supramolecular protein assemblies with advanced functions and synthesis thereof 发明人:BRITTO Sandanaraj Selvaraj; BHANDARI PAVANKUMAR JANARDHAN; REDDY Mullapudi Mohan 权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES 摘要:The present invention discloses stimuli-sensitive protein conjugate which can make supramolecular protein assemblies and methods for using the same. The present invention provides simple and rational process for construction of said stimuli-sensitive spherical protein assemblies through supramolecular chemical strategy.
专利号:WO-03000690-A1 优先权日:2001-06-25 标题:Synthesis of heterocyclic compounds employing microwave technology 发明人:MAJID TAHIR NADEEM; DEPRETS STEPHANIE D; PEDGRIFT BRIAN L 权利人:AVENTIS PHARMA INC; MAJID TAHIR NADEEM; DEPRETS STEPHANIE D; PEDGRIFT BRIAN L 摘要:This invention provides for processes for preparing compounds of the formula (I) comprising employing microwave energy.
专利号:US-5200546-A 优先权日:1991-09-30 标 题 :Phosphonoalkyl phenylalanine compounds suitably protected for use in peptide synthesis 发明人:BURKE JR TERRENCE R; LIM BENJAMIN B 权利人:US HEALTH 摘要:There are disclosed novel compounds of the formula: ##STR1## wherein, x is --CH 2 --, --CHF--, --CF 2 , --CHOH-- or --C(O)--; n R 6 is hydrogen, benzyl, pentafluorophenyl, nitrophenyl, 1-benzotriazolyl or 1-succinimidoyl; n Fmoc is 9-fluorenylmethyloxycarbonyl; and n * indicates a chiral carbon atom. n The Formula (I) compounds are useful in synthesizing peptides. There are also disclosed novel synthesis methods which include the step of hydrogenating a compound of the Formula ##STR2## wherein R 4 and R 5 are C 1-8 lower alkyl, to give a compound of the formula ##STR3## wherein R 4 and R 5 are as defined above. The compounds of formula (II) are useful as intermediates in preparing certain formula (I) compounds.
专利号:WO-2011047481-A1 优先权日:2009-10-23 标题 :Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:FORTIN REJEAN; LACHANCE NICOLAS; LI CHUN SING; TRANMER GEOFFREY 权利人:MERCK FROSST CANADA LTD; FORTIN REJEAN; LACHANCE NICOLAS; LI CHUN SING; TRANMER GEOFFREY 摘要:Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl- coenzyme. A delta-9 desaturase (SCDl) relative to other known stearoyl-coenzyme. A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. Formula (I).
专利号:US-2009176968-A1 优先权日:2006-06-20 标 题 :Preparation of Triazole Containing Metal Chelating Agents 发明人:MINDT THOMAS; SCHIBLI ROGER 权利人:SCHERRER INST PAUL 摘要:New chelating agents as well as their tricarbonyl complexes with technetium and rhenium and the use of these compounds in radiodiagnosis and radiotherapy are described. As a peculiarity of this invention, synthesis and coupling of the chelating systems to (bio)molecules is performed simultaneously. The new chelating agents are coupled to substances that accumulate in the diseased/targeted tissue.