Ethyl 2,4-Dihydroxy-6-Methylnicotinate置于氢氧化钾,乙醇,Potassium Acetate,钯,三氯氧磷体系中,化学反应生成 6-甲基烟酸 参考文献:Kooyman; Wibaut,Recueil Des Travaux Chimiques Des Pays-Bas,1946,Vol. 65,P. 10,13 标题:Kooyman; Wibaut,Recueil Des Travaux Chimiques Des Pays-Bas,1946,Vol. 65,P. 10,13
专利号:US-7151112-B1 优先权日:2001-09-04 标题:Pharmaceutical uses and synthesis of nicotinamides 发明人:CUTSHALL NEIL S; JEFFREY SCOTT C 权利人:UCB SA 摘要:This invention is directed to methods of using a compound of the formula n nand pharmaceutically acceptable salts thereof, wherein n, X, R 1 and R 2 are disclosed herein, for treating inflammatory events in an animal subject.
专利号:US-9676783-B2 优先权日:2008-10-22 标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds 发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN 权利人:ARRAY BIOPHARMA INC 摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
专利号:US-2009215080-A1 优先权日:2005-10-13 标题:Methods for identification of inhibitors of enzyme activity 发明人:SINHA SUKANTO; CHILCOTE TAMIE JO 权利人:ACTIVESITE PHARMACEUTICALS 摘要:The invention discloses compositions and methods of synthesis to create novel ligands and drugs and identifying such compounds as inhibitors of enzyme targets for use in the treatment of clinical disorders, including cancer, infectious diseases, parasitic infestations, neurological disorders, reproductive disorders, inflammatory disorders, circulatory disorders, and metabolic disorders.
专利号:US-5169935-A 优先权日:1990-06-20 标 题:Method of making peptides 发明人:HOEGER CARL A; THEOBALD PAULA G; PORTER JOHN S; RIVIER JEAN E F 权利人:SALK INST FOR BIOLOGICAL STUDI 摘要:Methods for making peptides of a suitable length for solid phase synthesis, which peptides include in their sequence a pair of residues of a different character which have acylated side chains and a residue which has an N-alkylated side chain. A peptide intermediate is constructed on the resin using commercially available starting materials. The N-terminus can be acylated by removing the alpha -amino protecting group and acylating under standard conditions. First primary amino protecting groups included in those residues to be acylated are removed, and acylation is effected, preferably by using a carboxypyridine or a similar heterocyclic acylating agent. Following such side chain acylation, a second protecting group included in the residue to be N-alkylated is removed, and the N-alkylation reaction is carried out while the peptide remains on the resin using a borohydride and an appropriate aldehyde or ketone. Following cleavage from the resin and removal of any protecting groups still remaining, the peptide is appropriately purified, thus requiring only a single purification to be carried out while forming a synthetic peptide including residues for which the modified amino acids are not readily commercially available.
专利号:US-5968736-A 优先权日:1992-10-01 标 题 :Methods for recording the reaction history of a solid support 发明人:STILL W CLARK; WIGLER MICHAEL H; OHLMEYER MICHAEL H J; DILLARD LAWRENCE W; READER JOHN C 权利人:COLD SPRING HARBOR LAB; UNIV COLUMBIA 摘要:Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detached from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.
专利号:US-9217012-B2 优先权日:2009-04-08 标题 :Inhibitors of protein tyrosine phosphatases 发明人:ZHANG ZHONG-YIN; ZHANG SHENG 权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP 摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.