专利号:US-4743694-A 优先权日:1986-04-11 标 题 :Diastereocontrolled synthesis of 2-amino alcohols 发明人:CLAREMON DAVID A 权利人:MERCEK & CO INC 摘要:The addition of organolithium to dimethylhydrazones of certain ethers of a-hydroxyaldehydes results in the synthesis of threo- or erythro- intermediates readily convertible to threo- or erythro-2-amino alcohols.
专利号:US-6867202-B1 优先权日:1997-06-25 标 题 :Treatment of insulin resistance 发明人:CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL 权利人:PFIZER 摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.
专利号:US-2005239808-A1 优先权日:2002-05-10 标题 :Active substances for the treatment, diagnosis and prophylaxis of diseases in which abnormal protein structures occur 发明人:SCHRADER THOMAS; RIESNER DETLEV; RZEPECKI PETRA; NAGEL-STEGER LUITGARD; WEHNER MARK; KIRSTEN CHRISTIAN; MOLT OLIVER; ZADMARD REZA; ASCHERMANN KATJA 权利人:SCHRADER THOMAS; RIESNER DETLEV; RZEPECKI PETRA; NAGEL-STEGER LUITGARD; WEHNER MARK; KIRSTEN CHRISTIAN; MOLT OLIVER; ZADMARD REZA; ASCHERMANN KATJA 摘要:The invention on hand refers to diseases associated with abnormal protein structures, including Alzheimer's disease, Creutzfeldt-Jakob's disease, BSE and other prion-associated diseases. It is the task of the invention on hand to provide new active agents preventing the formation of amyloid plaques and to dissolve existing plaques, such agents being convenient for therapy, diagnosis and prophylaxis of diseases that are associated with abnormal protein structures. This task is performed in terms of the current invention by heterocyclic or aromatic agents with a rigid structure and a donor-acceptor-donor pattern (DAD), the latter being formed by donors and acceptors of hydrogen bridge linkages which comply with the β-sheet structure of the peptide or protein and thus fit as binding partners. The heterocyclic or aromatic agents are available at least as dimers. They recognise peptides and proteins with a β-sheet structure, form stable complexes with them and inhibit their aggregation to β-amyloid plaques. Furthermore, the new active agents are able to dissolve β-amyloid plaques that already exist. Another task of the current invention is to provide methods for the synthesis of said heterocyclic or aromatic compounds.
专利号:US-7312343-B2 优先权日:2004-06-02 标 题:Synthesis of α-amino-β-alkoxy-carboxylic acid esters 发明人:SCHMID RUDOLF; ZUTTER ULRICH 权利人:HOFFMANN LA ROCHE 摘要:Compounds of formula I n nand a process for the preparation of such compounds are disclosed.
专利号:US-8703991-B2 优先权日:2008-11-04 标 题 :Synthesis of (phenylalkyloxy)phenyl-oxobutanoic acids 发明人:WIRTH DAVID D; HUDSPETH JAMES P 权利人:WIRTH DAVID D; HUDSPETH RICHARD; WELLSTAT THERAPEUTICS CORP 摘要:A method for synthesizing (phenylalkyloxy)phenyl-oxobutanoic acid compounds is described. The corresponding (phenylalkyloxy)acylphenyl compound is halogenated, giving the alpha haloketone. The halide is displaced by the anion of a di-alkyl malonate to give a substituted malonic ester. Hydrolysis of the ester and decarboxylation of the diacid gives the desired product.
专利号:US-7550510-B2 优先权日:2001-07-06 标 题 :Solid phase synthesis of arylretinamides 发明人:CURLEY JR ROBERT W; MERSHON SERENA M; BARNETT DEREK W; CLAGETT-DAME MARGARET; CHAPMAN JASON S 权利人:WISCONSIN ALUMNI RES FOUND 摘要:A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride; adding pyridine and a select arylamine to the resulting mixture; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.