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:US-3839346-A 优先权日:1972-12-18 标 题:N-substituted pyridone and general method for preparing pyridones 发明人:GADEKAR S 权利人:AFFILIATED MED RES 摘要:1. A PROCESS FOR THE SYNTHESIS OF PYRIDONES OF THE FORMULA 1-A,2-(O=),3-R3,4-R4,5-R5,6-R6-1,2-DIHYDROPYRIDINE WHEREIN A IS AN AROMATIC RADICAL SELECTED FROM THE GROUP CONSISTING OF PHENYL, TOLYL, CHLOROPHENYL, TRIFLUOROMETHYLPHENYL, NAPHTHYL, PYRIDYL, FURYL, THIENYL, THIAZOLYL, PYRIMIDYL, QUINOLYL, IMIDAZOLYL; UP TO TWO OF THE TERMS R3, R4, R5 AND R6 ARE INDIVIDUALLY EACH HYDROGEN OR ALKYL UP TO 6 CARBON ATOMS, ARYL OR SUBSTITUTED ARYL RADICALS WHICH CONSISTS ESSENTIALLY OF THE STEPS OF REACTING A PYRIDONE OF THE FORMULA 2-(O=),3-R3,4-R4,5-R5,6-R6-1,2-DIHYDROPYRIDINE, OR ITS TAUTOMER, 2-(HO-),3-R3,4-R4,5-R5,6-R6-PYRIDINE IN WHICH R3, R4, R5 AND R6 ARE SET FORTH ABOVE, WITH A HALOGENATED COMPOUND OF THE FORMULA AX, WHEREIN X IS EITHER CHLORINE, BROMINE OR IODINE, AT TEMPERATURES RANGING BETWEEN THE MELTING POINT AND BOILING POINT OF SAID HALOGENATED COMPOUND, IN THE PRESENCE OF AN ALKALI METAL CARBONATE AND FINELY DIVIDED METALLIC COPPER.
专利号:EP-4588918-A1 优先权日:2024-01-18 标 题:Synthesis of (s)-1-(1-(3-chlorophenyl)-2-(dimethylamino)ethyl)- 4-(5-morpholino-1h-pyrrolo[2,3-b]pyridin-3-yl)pyridin-2(1h)-one
专利号:WO-2025067239-A1 优先权日:2023-09-26 标 题 :Kinesin kif18a inhibitor, and application thereof 发明人:XIAO YISONG; GU XIAOHUI; LAI KUNMIN; WANG MINGHUA; HU MIN 权利人:SHANGHAI APEIRON THERAPEUTICS COMPANY LTD 摘要:A KIF18 inhibitor, and a synthesis method therefor, capable of adjusting a KIF18A protein, so as to affect cell cycle and cell proliferation processes, in order to treat cancers and cancer-related diseases. Also provided are a pharmaceutical composition including the KIF18 inhibitor compound, and a method for treating KIF18A activity-related conditions.
参考文献:10.1126/sciadv.abf8711 摘要:Schuller M, Correy GJ, Gahbauer S, Fearon D, Wu T, Díaz RE, Young ID, Carvalho Martins L, Smith DH, Schulze-Gahmen U, Owens TW, Deshpande I, Merz GE, Thwin AC, Biel JT, Peters JK, Moritz M, Herrera N, Kratochvil HT; QCRG Structural Biology Consortium, Aimon A, Bennett JM, Brandao Neto J, Cohen AE, Dias A, Douangamath A, Dunnett L, Fedorov O, Ferla MP, Fuchs MR, Gorrie-Stone TJ, Holton JM, Johnson MG, Krojer T, Meigs G, Powell AJ, Rack JGM, Rangel VL, Russi S, Skyner RE, Smith CA, Soares AS, Wierman JL, Zhu K, O'Brien P, Jura N, Ashworth A, Irwin JJ, Thompson MC, Gestwicki JE, von Delft F, Shoichet BK, Fraser JS, Ahel I. Fragment binding to the Nsp3 macrodomain of SARS-CoV-2 identified through crystallographic screening and computational docking. Sci Adv. 2021 Apr;7(16).