专利号:US-9321728-B2 优先权日:2012-04-25 标题:Beta-alanine derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical composition comprising same as active ingredient 发明人:AHN JIN HEE; PAGIRE H S; RHEE SANG DAL; KIM KI YOUNG; JUNG WON HOON; BAE MYUNG-AE; SONG JIN SOOK; KIM KWANG-ROK; KWAK HYUN JUNG 权利人:KOREA RES INST CHEM TECH; HANDOK PHARMACEUTICALS CO LTD 摘要:The present invention relates to a beta-alanine derivative, pharmaceutically acceptable salts thereof, and a pharmaceutical composition including the same as an active ingredient. The novel beta-alanine derivative and pharmaceutically acceptable salts thereof according to the present invention may effectively inhibit the activity of DGAT1, which is an enzyme serving as a catalyst in the final step of the synthesis of neutral lipids, to thereby be effectively used as a pharmaceutical composition for preventing or treating various lipid metabolism-related disorders selected from the group consisting of obesity, dyslipidemia, fatty liver, insulin resistance syndrome, and hepatitis.
专利号:US-5081138-A 优先权日:1986-12-17 标题:3-hetero-substituted-n-benzyl-indoles and prevention of leucotriene synthesis therewith 发明人:GILLARD JOHN W; MORTON HOWARD E; FORTIN REJEAN; GUINDON YVAN 权利人:MERCK FROSST CANADA INC 摘要:Compounds having the formula: are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
专利号:US-6989384-B2 优先权日:2000-06-14 标题:Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis 发明人:HUA YE; LUU HIEP THE; CHAN FORA P; JOHNSON JR THEODORE O; REICH SIEGFRIED HEINZ; SKALITZKY DONALD JAMES; YANG YI; HENDRICKSON THOMAS F; CHU SHAO SONG; EASTMAN BRIAN WALTER 权利人:AGOURON PHARMA 摘要:Compounds of the formula: n nwhere the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:US-2024327418-A1 优先权日:2021-08-04 标 题 :Multi-target inhibitor targeting hdac and nad synthesis and use of multi-target inhibitor
专利号:WO-2023231948-A1 优先权日:2022-05-30 标 题:Isr inhibitors, method for preparing same, and use thereof 发明人:ZHANG HUIBIN; ZHOU JINPEI; WANG LIXUN; PEI YIFENG 权利人:UNIV CHINA PHARMA 摘要:Disclosed are a class of ISR inhibitors, a method for preparing same, and use thereof. The present invention belongs to the technical field of biopharmaceutics. The compound of the present invention is a compound having a structure of formula (I) or formula (II), a stereoisomer thereof, a geometric isomer thereof, a tautomer thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, a hydrate thereof or a solvate thereof. The compound provided by the present invention can effectively bind to elF2B, has a good ability to inhibit ATF4, and can well restore protein synthesis upon ISR stimulation. Therefore, the compound of the present invention can be used as an ISR inhibitor for treating various related diseases.
专利号:WO-2023011416-A1 优先权日:2021-08-04 标题:Multi-target inhibitor targeting hdac and nad synthesis and use of multi-target inhibitor
参考文献:10.1038/ncb3255 摘要:Lin R, Elf S, Shan C, Kang HB, Ji Q, Zhou L, Hitosugi T, Zhang L, Zhang S, Seo JH, Xie J, Tucker M, Gu TL, Sudderth J, Jiang L, Mitsche M, DeBerardinis RJ, Wu S, Li Y, Mao H, Chen PR, Wang D, Chen GZ, Hurwitz SJ, Lonial S, Arellano ML, Khoury HJ, Khuri FR, Lee BH, Lei Q, Brat DJ, Ye K, Boggon TJ, He C, Kang S, Fan J, Chen J. 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. Nat Cell Biol. 2015 Nov;17(11):1484–96. 摘要:Journal of Medicinal Chemistry., 15(659), 1972