专利号:WO-2014011120-A1 优先权日:2012-07-13 标 题 :Endoperoxides, synthesis and uses thereof for the treatment of neoplastic diseases such as cancer 发明人:TAN NGUAN SOON; CHIBA SHUNSUKE 权利人:UNIV NANYANG TECH 摘要:The present invention generally relates to processes and methods for the synthesis of endoperoxide compounds. More specifically, the invention relates to a method for preparing endoperoxide compounds starting from an aryl imine of formula (I) in the presence of a metallic catalyst and oxygen. The present invention also relates to endoperoxide compounds of formula (III) and their pharmaceutically acceptable salts thereof, useful for therapy. All substituents are defined herein. Also disclosed are methods of treating cancer using the compounds of formula (III).
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:US-2022363662-A1 优先权日:2021-04-20 标题 :Compounds as lxr agonists 发明人:PUJALA BRAHMAM; SATHE BALAJI DASHRATH; DANODIA ABHINANDAN; GUPTA ASHU; SONI SANJEEV; KUMAR VIVEK; ANSARI AMANTULLAH; KHAN FARHA; SARKAR ARINDAM; PAYGHAN PAVAN V 权利人:INTEGRAL BIOSCIENCES PRIVATED LTD 摘要:The present invention generally discloses compounds having LXR (the liver X receptor) agonistic activity, to the use of such compounds in the treatment of various disorders such as proliferative disorders, Alzheimer's disease, inflammatory diseases, and diseases characterized by defects in cholesterol and lipid metabolism. Specifically, the present invention discloses compound of formula (IA) which exhibit LXR agonist activity, specifically to LXRβ. The invention also discloses method of synthesis of said compounds, method of using said compounds, pharmaceutical compositions comprising said compounds and method of using thereof.
专利号:EP-3070087-B1 优先权日:2011-08-05 标题 :Intermediates for the synthesis of cyclic p1 linkers as factor xia inhibitors
专利号:EP-3070087-A1 优先权日:2011-08-05 标 题 :Intermediates for the synthesis of cyclic p1 linkers as factor xia inhibitors
专利号:WO-2007104696-A1 优先权日:2006-03-15 标题 :Antimalarial agents having polyaromatic structure 发明人:CAMPIANI GIUSEPPE; GEMMA SANDRA; FATTORUSSO CATERINA; KUKREJA GAGAN; JOSHI BHUPENDRA PRASAD; TAGLIALATELA SCAFATI ORAZIO; SAVINI LUISA; DE ANGELIS MERI; FATTORUSSO ERNESTO 权利人:SIGMA TAU IND FARMACEUTI; CAMPIANI GIUSEPPE; GEMMA SANDRA; FATTORUSSO CATERINA; KUKREJA GAGAN; JOSHI BHUPENDRA PRASAD; TAGLIALATELA SCAFATI ORAZIO; SAVINI LUISA; DE ANGELIS MERI; FATTORUSSO ERNESTO 摘要:Antimalarial agents having a novel pharmacophore of formula (I) are herein described. These polycyclic compounds are able to inhibit chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum (Pf). Furthermore, the synthesis of these compounds involves few steps from commercial products with low cost of production.