专利号:US-2021284618-A1 优先权日:2016-08-12 标 题 :Furanochalcones as inhibitors of cyp1a1, cyp1a2 and cyp1b1 for cancer chemoprevention 发明人:BHARATE SANDIP BIBISHAN; SHARMA RAJNI; JOSHI PRASHANT; VISHWAKARMA RAM; CHAUDHURI BHABATOSH 权利人:COUNCIL SCIENT IND RES; DE MONTFORT UNIV 摘要:The present invention relates to the furanochalcone class of compounds of general formula A. The present invention particularly relates to the synthesis of furanochalcones and their CYP1A1, CYP1A2 and CYP1B1 inhibitory activity. In addition, the invention relates to the prevention or treatment of cancer caused by polyaromatic hydrocarbons (PAHs), 4-nitroquinoline-1-oxide, and N-nitroso-N-methylurea, heterocyclic amines, estrogen and 17β-estradiol, resulting from the inhibition of CYP1A1, CYP1A2 and CYP1B1 enzymes.
专利号:WO-2021038419-A1 优先权日:2019-08-23 标题 :Kinase inhibitors and methods of synthesis and treatment 发明人:ZAVORONKOVS ALEKSANDRS; IVANENKOV YAN; POLYKOVSKIY DANIIL; ALIPER ALEKSANDR 权利人:INSILICO MEDICINE IP LTD 摘要:Compounds that function as kinase inhibitors are provided. The kinase inhibitors can have any structure of the formulae provided herein, such as shown for Compounds 1-4. A pharmaceutical composition can include: the compound of one of the embodiments; and a pharmaceutically acceptable carrier having the compound. A method of inhibiting a kinase can include: providing the compound of one of the embodiments described herein to the kinase such that the kinase is inhibited. The methods can include inhibiting DDR1 and/or DDR2, and thereby providing a modulation or decrease in the activity of DDR1 and/or DDR2. This decrease in DDR1 and/or DDR2 activity can be used as therapy to treat conditions related to DDR1 and/or DDR2 activity, such as fibrosis, cancer, and others.
专利号:US-2013164265-A1 优先权日:2011-12-21 标题 :Skin care compositions 发明人:FLAVIN DANA; OBENLAND SIGRID 权利人:FLAVIN DANA; OBENLAND SIGRID 摘要:This invention provides compositions and methods of manufacturing such compositions that employ GRAS compounds which can act to promote the generation of stem, epidermal or other skin cells in the epidermis, activation of collagen synthesis, activation of hyaluronic acid synthesis, enhanced skin hydration, and dermal healing by stimulating stem cell and fibroblast migration to sites of needed repair. These compositions and methods are useful for rejuvenating the skin and for treating some skin-related aging or other dermal damaging conditions, including wrinkle reduction and treatment of minor dermal wounds.
专利号:US-2014328952-A1 优先权日:2011-12-21 标题:Topical compositions 发明人:FLAVIN DANA 权利人:FLAVIN DANA 摘要:This invention provides compositions and methods of manufacturing such compositions that employ GRAS compounds which can act to promote the generation of stem, epidermal or other skin cells in the epidermis, activation of collagen synthesis, activation of hyaluronic acid synthesis, enhanced skin hydration, and dermal healing by stimulating stem cell and fibroblast migration to sites of needed repair. These compositions and methods are useful for rejuvenating the skin and for treating some skin-related aging or other dermal damaging conditions, including wrinkle reduction and treatment of minor dermal wounds.
专利号:US-2023295141-A1 优先权日:2022-03-17 标 题:Fxr small molecule agonist, the preparation and use thereof 发明人:ZHAO YISHUANG; ZHANG ZHENWEI; WU GUOHUI; YANG SHENGSHENG 权利人:CASCADE PHARMACEUTICALS INC 摘要:The present invention discloses an FXR (farnesoid X receptor) small molecule agonist, the structure of which is shown in formula I, and a preparation method thereof. In the formula, the definition of each substituent is as described in the specification and claims. The compound of the present invention has advantages, such as high FXR agonistic activity, convenience in synthesis, easy availability of raw materials, and can be used as a medicine for the treatment of FXR-related diseases.
专利号:US-10829464-B2 优先权日:2016-11-23 标题 :Benzoheterocyclic alkylamine compounds and use thereof 发明人:LI JIAN; LAN LEFU; LI BAOLI; CHEN FEIFEI; NI SHUAISHUAI; LIU YIFU; WEI HANWEN; MAO FEI; ZHU JIN 权利人:UNIV EAST CHINA SCIENCE & TECH; SHANGHAI INST MATERIA MEDICA CAS 摘要:Disclosed are benzoheterocyclic alkylamine compounds, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, and a preparation method thereof, and use of the same in the manufacture of an antibacterial drug as an inhibitor of staphyloxanthin synthesis in Staphylococcus aureus .
参考标题:Palladium-Catalyzed Carbonylation Reaction Of Aryl Bromides With 2-Hydroxyacetophenones To Form Flavones 作者:Xiao-Feng Wu,Helfried Neumann,Matthias Beller |发布日期:2012.10.1 摘要:Flavone Of The Month: A General And Efficient Method For The Palladium‐catalyzed Carbonylative Synthesis Of Flavones Has Been Developed (See Scheme). Starting From Aryl Bromides And 2‐hydroxyacetophenones, The Corresponding Flavones Have Been Isolated In Good Yields.
合成参考文献
参考文献:10.1021/tx200080b 摘要:Amunom I, Dieter LJ, Tamasi V, Cai J, Conklin DJ, Srivastava S, Martin MV, Guengerich FP, Prough RA. Cytochromes P450 catalyze the reduction of α,β-unsaturated aldehydes. Chem Res Toxicol. 2011 Aug 15;24(8):1223–30.