专利号:US-6252082-B1 优先权日:1997-01-16 标 题 :Pyridone derivatives, their preparation and their use as synthesis intermediates 发明人:LASSALLE GILBERT; BELLEVERGUE PATRICE; BOURBIER JEAN-CLAUDE; GALTIER DANIEL; MARTIN VALERIE 权利人:SANOFI SYNTHELABO 摘要:The invention concerns compounds of formula (I)in which: R is -NO2 or -NHR3, R3 being hydrogen, -COR4 (R4 selected among (C1-C4) alkyl, aryl and aryl (C1-C4) alkyl, -COOR5 (R5 selected among (C1-C4) alkyl and aryl (C1-C4) alkyl), -CONHR6 or SO2R6 (R6 selected among (C1-C5) alkyl, aryl and aryl(C1-C4) alkyl), -SO2NR7R8 (R7 and R8 independently of each other represent hydrogen or (C1-C4) alkyl or form with the nitrogen atom a morpholine group), aryl (C1-C4) alkyl, R1 is a (C1-C4) alkyl group linear or branched, cyclo (C3-C8) alkyl, aryl optionally substituted, aryl (C1-C4) alkyl optionally substituted, heteroaryl, R2 is a hydrogen atom, a (C1-C4) alkyl or arylmethyl group, X is an oxygen or sulphur atom, a -CH2-, -SO2 or -NR1- group and Y is a hydrogen atom or (C1-C6) alkyl. The invention is applicable to synthesis intermediates.
专利号:WO-2010115869-A1 优先权日:2009-04-03 标 题 :Propofol phosphonyl derivatives, synthesis, and use in long acting formulations 发明人:GONNISSEN YVES RENE JOHANNA PAUL 权利人:SEPS PHARMA N V; GONNISSEN YVES RENE JOHANNA PAUL 摘要:This invention relates to compounds represented by the structural formula (I), and the salts and stereoisomers thereof, wherein: - L is a linker selected from the group consisting of -(CH 2 ) P -O-, a single bond, formula (IA), -(CH 2 ) 1-8 -O-X(O)-, and - p is an integer from 1 to 8, - each R 3 and each R 4 is independently selected from the group consisting of C 1-20 alkyl, C 3-12 alkyl, C 3-12 cycloalkyl-C 1-4 alkyl, saturated heterocyclyl and saturated heterocyclyl-C 1-4 alkyl, and - X and Y are each independently C or S(O), - Z is selected from the group consisting of O, S(O) and NR 5 , - W is selected from the group consisting of halogen, OH, S(O)H and O - M + wherein M + is a monovalent cation; and - R 5 is selected from the group consisting of hydrogen and C 1-10 alkyl. These compounds are useful pharmaceutical agents with improved oral bioavailability.
专利号:RU-2067585-C1 优先权日:1991-09-12 标 题 :Derivatives of 5-amino-4-hydroxyhexanoic acid and a method of their synthesis
参考文献:10.1007/s11030-024-10860-6 摘要:Jin Z, Zhang Y, Luo X, Geng M, Duan W, Xie Z, Zhang H. Design, synthesis, and evaluation of thiazolecarboxamide derivatives as stimulator of interferon gene inhibitors. Mol Divers. 2025 Feb;29(1):397–423. doi: 10.1007/s11030-024-10860-6.