专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-8598153-B2 优先权日:2006-09-22 标题 :Method of treatment using fatty acid synthesis inhibitors 发明人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN 权利人:SINGH SHEO B; TOTA MICHAEL R; WANG JUN; MERCK SHARP & DOHME 摘要:The present invention relates to natural products that possess fatty acid synthesis inhibitor activity and can be used to treat and prevent diseases such as obesity, cancer, diabetes, fungal infections, Mycobacterium tuberculosis infections, malarial infections and other apicomplexan protozoal diseases.
专利号:US-2022402908-A1 优先权日:2019-07-08 标题 :Cxcr6 inhibitors and methods of use 发明人:PEDDIBHOTLA SATYAMAHESHWAR; HERSHBERGER PAUL M; KIRBY RICHARD JASON; MALANY SIOBHAN; SMITH LAYTON H; MALONEY PATRICK R; SESSIONS HAMPTON; DIVLIANSKA DANIELA; PINKERTON ANTHONY B 权利人:SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INST 摘要:Provided herein are small molecule inhibitors of CXCR6 receptor, compositions comprising the compounds, and methods of using the compounds and compositions. The compounds are 9-azbicyclo[3.3.1]nonane or 9-diazbicyclo[3.3.1]nonane derivatives, whose synthesis is also described. Also provided are method of treating a disease or condition (such as, cancer) mediated by CXCR6/CXCL16 signaling pathway in a mammal.
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-9018249-B2 优先权日:2011-09-13 标题 :SGLT inhibitors 发明人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR 权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD 摘要:The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).
专利号:EP-1551403-B1 优先权日:2002-10-10 标 题 :5-substituted 2h-pyrazone-3-carboxylic acid derivatives as antilipolytic agents for the treatment of metabolic-related disorders such as dyslipidemia 发明人:SEMPLE GRAEME; AVERBUJ CLAUDIA; SKINNER PHILIP; GHARBAOUI TAWFIK; SHIN YOUNG-JUN 权利人:ARENA PHARM INC 摘要:The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R2 is H, halogen, C1-12 alkyl or C1-12 haloalkyl; and R3 is C3-6 cycloalkyl, C1-12 alkyl, C1-12 haloalkyl, C3-6 cycloalkyl-C1-4-alkylene, aryl-C1-4-alkylene or heteroaryl-C1-4-alkylene, wherein said aryl-C1-4-alkylene and heteroaryl-C1-4-alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for pharmaceutical compositions in combination with other active agents, for example, those agents belonging to the class of alpha-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, thiazolidinedione and the like.
1: Vázquez C, Encalada R, Jiménez-Galicia I, Gómez-Escobedo R, Rivera G, Nogueda-Torres B, Saavedra E. Repurposing the Antidiabetic Drugs Glyburide, Gliquidone, and Glipizide in Combination with Benznidazole for Trypanosoma cruzi Infection. Pharmaceuticals (Basel). 2024 Dec 27;18(1):21. doi: 10.3390/ph18010021. 2: Yang C, Li Q, Hu F, Liu Y, Wang K. Inhibition of Cardiac Kv4.3/KChIP2 Channels by Sulfonylurea Drug Gliquidone. Mol Pharmacol. 2024 Feb 15;105(3):224-232. doi: 10.1124/molpharm.123.000787. 21(3):e41. doi: 10.5808/gi.23035. Epub 2023 Sep 27. 4: Huang L, Zhang X, Luo L, Mu H, Li W, Wang R. Effects of high-altitude environment on pharmacokinetic parameters of gliquidone in rats. Zhejiang Da Xue Xue Bao Yi Xue Ban. 2022 Aug 1;51(4):389-396. English. doi: 10.3724/zdxbyxb-2022-0129.
合成参考文献
参考文献:10.1107/s1600536811016680 摘要:Gelbrich T, Haddow MF, Griesser UJ. Gliquidone. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1343.