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-10329264-B2 优先权日:2015-07-31 标题 :Process for the preparation of isocarboxazid 发明人:DE FAVERI CARLA; HUBER FLORIAN ANTON MARTIN; ANTOLINI NICOLA 权利人:LUNDBECK PHARMACEUTICALS ITALY S P A 摘要:This invention relates to a novel chemical process for the synthesis of N′-benzyl-5-methylisoxazole-3-carbohydrazide (Isocarboxazid) which comprises reacting 5-methyl-3-isoxazole carboxylic acid ester with benzylhydrazine or a salt thereof in an aprotic organic solvent and in the presence of an organic base.
专利号:WO-0019994-A9 优先权日:1998-10-02 标题 :Estrogen receptor ligands 发明人:KATZENELLENBOGEN JOHN A; KATZENELLENBOGEN BENITA S; FINK BRIAN E; STAUFFER SHAUN R; MORTENSEN DEBORAH S; SATTIGERI VISWAJANANI JITENDRA; HUANG YING 权利人:UNIV ILLINOIS 摘要:This invention provides non-steroidal estrogen receptor ligands having a modular structure that is amenable to solid phase synthesis and the application of combinatorial synthetic methods to prepare these estrogen receptor ligands. ER ligands of this invention consist of a core scaffold that is a carbocyclic or heterocyclic-5-member ring that has two double bonds or a 6-member aromatic ring. A plurality of selected substituents are bonded to the ring substantially independently of other substituents. The modular structure of these compounds allows for synthesis of a very large numer of substituent structural variations, substituent combinations and substituent positioning on the core. The structural variants of the ER ligands of this invention exhibit a spectrum of selective affinities for ERα and ERβ and a spectrum of agonist/antagonist properties.
专利号:US-10226449-B2 优先权日:2013-12-20 标 题:Heterocyclic modulators of lipid synthesis and combinations thereof 发明人:HEUER TIMOTHY SEAN; OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREGORY; OHOL-GUPTA YAMINI; O'FARRELL MARIE 权利人:3 V BIOSCIENCES INC 摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
专利号:US-9428502-B2 优先权日:2012-07-03 标题:Heterocyclic modulators of lipid synthesis 发明人:OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; WAGMAN ALLAN S 权利人:3-V BIOSCIENCES INC 摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.
专利号:US-2024239799-A1 优先权日:2021-04-02 标 题:(s)-1-(5-((pyridin-3-yl)thio)pyrazin-2-yl)-4'h,6'h-spiro[piperidine-4,5'-pyrrolo [1,2-b]pyrazol]-4'-amine derivatives and similar compounds as shp2 inhibitors for the treatment of e.g. cancer 发明人:DI FABIO ROMANO; MONTALBETTI CHRISTIAN; PETROCCHI ALESSIA; GRILLO ALESSANDRO; RANDAZZO PIETRO; ROSSETTI ILARIA; CIAMMAICHELLA ALINA 权利人:C N C C S S C A R L COLLEZIONE NAZ DEI COMPOSTI CHIMICI E CENTRO SCREENING; IRBM S P A 摘要:The present invention relates to compounds of formula (I). The compounds of the formula (I) are e.g. (S)-1-(5-((pyridin-3-yl)thio) pyrazin-2-yl)-41H,6′H-spiro[piperidine-4,5′-pyrrolo[1,2-b]pyrazol]-41-amine derivatives and similar compounds. The present invention also relates to the compounds of formula (I) for use as Src homology phosphotyrosine phosphatase 2 (SHP2) inhibitors in methods of treatment of e.g. cancer, cardiovascular diseases, immunological disorders, autoimmune disorders, fibrosis, ocular disorders, systemic lupus erythematosus, diabetes, neutropenia, and combinations thereof. The present invention also relates to pharmaceutical compositions containing said compounds and to their methods of synthesis.
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