专利号:US-9359333-B2 优先权日:2013-01-14 标 题 :Efficient process for the preparation of Lapatinib and salts thereof by means of new intermediates 发明人:FONTANA FRANCESCO; PAIO ALFREDO 权利人:F I S —FABBRICA ITALIANA SINT S P A; F I S —FABBRICA ITALIANA SINT 摘要:The present invention refers to a new efficient process for the synthesis of the active pharmaceutical ingredient Lapatinib and salts thereof. n In particular, the present synthesis is carried out employing new intermediates in which the amine function is protected by a group cleavable in basic milieu that provides a higher overall yield of the synthesis process.
专利号:US-12304894-B2 优先权日:2019-04-17 标题 :Derivatives of adamantyl oxadiazoles and pharmaceutically acceptable solvates, hydrates and salts thereof, pharmaceutical composition comprising same, synthesis method, suitable for use as effective and selective inhibitors of the reductase activity of the enzyme 11-beta dehydrogenase type 1 (11β-HSD1) 发明人:FARDELLA BELLO CARLOS ENRIQUE; LAGOS ARÉVALO CARLOS FERNANDO; VECCHIOLA CÃ?RDENAS ANDREA PAOLA; ALLENDE SANZANA FIDEL ALEJANDRO; DIETHELM VARELA BENJAMIN MANUEL; RECABARREN GAJARDO GONZALO IVAN; GONZÃ?LEZ CISTERNA PABLO MARCELO 权利人:UNIV PONTIFICIA CATOLICA CHILE 摘要:The present invention relates to compounds derived from adamantyl oxadiazoles and the pharmaceutically acceptable solvates, hydrates and salts of same. These compounds are suitable for use as effective and selective inhibitors of the reductase activity of the enzyme 11-beta dehydrogenase type 1 (11β-HSD1), as well as in the production of a drug for treating conditions and diseases such as high blood pressure, obesity, dyslipidaemia, type 2 diabetes, insulin resistance, glaucoma, metabolic syndrome, cognitive disorders, osteoporosis, immune disorders, depression and other conditions. Also provided is a pharmaceutical composition comprising the compounds and a method for preparing said composition.
专利号:US-10150111-B2 优先权日:2016-09-06 标题 :Method for catalytic synthesis of cinnamic acid with catalyst recycle
专利号:US-8338565-B2 优先权日:2008-08-20 标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha 发明人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P 权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP 摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.
专利号:US-2018326410-A1 优先权日:2016-09-06 标题 :Method for catalytic synthesis of cinnamic acid with catalyst recycle
专利号:WO-2018219107-A1 优先权日:2017-05-27 标题:Engineered polypeptides and their applications in synthesis of beta-hydroxy-alpha-amino acids