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:WO-2023275607-A1 优先权日:2021-07-02 标 题 :Synthesis of n,n-dialkyl, -dialkenyl, -dialkynl, and related cyclics, sulfamoyl fluoride compounds using hydrogen fluoride
专利号:US-6936600-B2 优先权日:1999-04-01 标题:Sorbitol dehrydrogenase inhibitors 发明人:CHU-MOYER MARGARET Y; MYLARI BANAVARA L; ZEMBROWSKI WILLIAM J 权利人:PFIZER 摘要:This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, n n nwherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula I and to processes for preparing those intermediates.
专利号:WO-9700872-A1 优先权日:1995-06-23 标题 :1,3,8-triaza- and 3,8-diaza-1-oxaspiro(4,5)decane derivatives 发明人:BERGER JACOB; CARTER DAVID SCOTT; FLIPPIN LEE ALLEN; WEINHARDT KLAUS KURT 权利人:HOFFMANN LA ROCHE 摘要:Heterocyclic compounds of Formula (I) in which n is 2, 3, 4, 5 or 6; t is 1, 2, 3 or 4; u is 0 or 1 (provided that t is not 1 when u is 0); X is O or N(R4), in which R4 is hydro, (C¿1-4 )alkyl, or aryl; Y and Z are independently C(O), C(S) or CH2 (provided that Y and Z are not both CH2); R 1, R2, and R3¿ are as defined in the specification; and their pharmaceutically acceptable salts and N-oxides, formulations containing them, their uses as therapeutic agents, and their synthesis. The compounds of this invention are selective 5-HT¿2 C receptor antagonists.
专利号:US-5739336-A 优先权日:1995-06-23 标题:1,3,8-triaza- and 3,8-diaza-1-oxaspiro 4,5! decane derivatives 发明人:WEINHARDT KLAUS K; BERGER JACOB; CARTER DAVID S; FLIPPIN LEE A 权利人:SYNTEX INC 摘要:Heterocyclic compounds of Formula I: I in which n is 2, 3, 4, 5 or 6; t is 1, 2, 3 or 4; u is 0 or 1 (provided that t is not 1 when u is 0); X is O or N(R4); Y and Z are independently C(O), C(S) or CH2 (provided that Y and Z are not both CH2); R1, R2, R3, and R4 are as defined in the specification; and their pharmaceutically acceptable salts and N-oxides, formulations containing them, their uses as therapeutic agents, and their synthesis.
参考文献:10.1055/s-0037-1610223 摘要:Pearson S, Fillery S, Goldberg K, Demeritt J, Eden J, Finlayson J, Patel A. Synthesis of Indole-Dihydroisoquinoline Sulfonyl Ureas via Three-Component Reactions. Synthesis. 2018 Aug 20;50(24):4963–81. doi: 10.1055/s-0037-1610223. 参考文献:10.1055/a-1509-5541 摘要:Renzi P, Azzi E, Lanfranco A, Moro R, Deagostino A. Visible Light as the Key for the Formation of Carbon–Sulfur Bonds in Sulfones, Thioethers, and Sulfonamides: An Update. Synthesis. 2021 Jul 07;53(19):3440–68. doi: 10.1055/a-1509-5541.