专利号:WO-2013057110-A1 优先权日:2011-10-19 标 题:Method for the synthesis of citric acid esters 发明人:ALTENBACH HANS-JOSEF; LANGE KARSTEN; NANDI SUKHENDU; IHIZANE RACHID; JAKOB BERND; SCHNEIDER MANFRED 权利人:BERGISCHE UNI WUPPERTAL; ALTENBACH HANS-JOSEF; LANGE KARSTEN; NANDI SUKHENDU; IHIZANE RACHID; JAKOB BERND; SCHNEIDER MANFRED 摘要:The present invention discloses a targeted synthesis method for the synthesis of asymmetric monoesters and/or symmetrical diesters of citric acid through acidic esterification by using boric acid or a boronic acid as a catalyst. The boric/boronic acid simultaneously acts as a catalyst, as well as a 'protecting group' for the tertiary carboxylic acid, and therefore specifically only the asymmetric monoesters or symmetrical diesters are created.
专利号:DE-102011054602-A1 优先权日:2011-10-19 标 题 :Process for the synthesis of citric acid esters
专利号:US-9169209-B2 优先权日:2011-05-04 标题:Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BAUMEISTER TIMM; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG 权利人:BAIR KENNETH W; BAUMEISTER TIMM; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC 摘要:The present invention relates to compounds and composition for inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
专利号:EP-2768795-A1 优先权日:2011-10-19 标题:Method for the synthesis of citric acid esters
专利号:US-7671085-B2 优先权日:2002-11-15 标 题 :Non-steroidal farnesoid X receptor modulators and methods for the use thereof 发明人:DOWNES MICHAEL R; EVANS RONALD M 权利人:SALK INST FOR BIOLOGICAL STUDI 摘要:The efficient regulation of cholesterol synthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR would be an important step in further deconvoluting FXR physiology. In accordance with the present invention, the identification of novel potent FXR activators is described. Two derivatives of invention compounds, bearing stilbene or biaryl moieties, contain members that are the most potent FXR agonists reported to date in cell-based assays. These compounds are useful as chemical tools to further define the physiological role of FXR as well as therapeutic leads for the treatment of diseases linked to cholesterol, bile acids and their metabolism and homeostasis.
专利号:US-9951062-B2 优先权日:2012-12-14 标 题 :Substituted 1 H-pyrrolo [2, 3-b] pyridine and 1 H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors 发明人:VANKAYALAPATI HARIPRASAD; YERRAMREDDY VENKATAKRISHNAREDDY; GANIPISETTY VENU BABU; TALLURI SURESHKUMAR; APPALANENI RAJENDRA P 权利人:ARRIEN PHARMACEUTICALS LLC 摘要:Compounds according to Formulas I, IA or IB: n nto pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and/or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes.