专利号:US-6228988-B1 优先权日:1995-02-24 标题:Synthesis of hydroxamic acid derivatives 发明人:FLOYD CHRISTOPHER DAVID; LEWIS CHRISTOPHER NORMAN 权利人:BRITISH BIOTECH PHARM 摘要:The present invention describes processes for preparing desired synthetic products that comprise a covalently bonded hydroxamic acid group -CONHOH by forming a mixture of a liquid reaction medium and a solid phase reaction product that carries a plurality of moieties of formula (A1) or (B1):where X is a residual, non-hydroxamate partial structure of the desired synthetic product, P1 is hydrogen or an amino-protecting group, P2 is hydrogen or a hydroxyl protecting group, and the bond designated (a) covalently links the moieties (A1) or (B1) to the residue of a solid substrate; by cleaving the bond designated (a) in the resultant mixture; and by separating the resultant liquid reaction phase from the resultant reaction solids to recover the desired synthetic product.
专利号:US-12227522-B2 优先权日:2020-12-21 标题:Synthesis of structural analogs of largazole and associated compounds 发明人:WILLIAMS ROBERT M; KOTI SIVANAGIREDDY; DE SUBHADIP; SHELKE ANIL M; CERBONE RYAN E; YASUDA NOBUYOSHI 权利人:UNIV COLORADO STATE RES FOUND; CETYA THERAPEUTICS INC 摘要:Disclosed are various synthetic methods to prepare structural analogs of largazole and derivatives thereof. One structural analog is an amide isostere of largazole. Another structural analog replaces the thiazole ring of largazole with a pyridine moiety or an oxazole moiety. Also disclosed are various intermediate compounds obtained when preparing structural analogs of largazole and derivatives thereof, including macrocycle analogs having an alcohol functionality.
专利号:US-2005192265-A1 优先权日:2003-03-20 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6906056-B2 优先权日:1998-06-22 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 权利人:LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6093798-A 优先权日:1995-02-24 标题 :Synthesis of hydroxamic acid derivatives
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.