专利号:US-7390801-B2 优先权日:1996-12-23 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:THORSETT EUGENE D; PLEISS MICHAEL A; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES A; REEL JON K; DRESSMAN BRUCE A; DROSTE JAMES J; HENRY STEVEN S; STUCKY RUSSELL D; PORTER WARREN J 权利人:ATHENA NEUROSCIENCES INC; 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 comprising 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-5077397-A 优先权日:1988-11-29 标题:Sialic acid derivative with active ester groups 发明人:YOSHIMURA SHOJI; TANAKA MAKOTO 权利人:KANTO ISHI PHARMA CO LTD 摘要:Sialic acid derivative with active ester groups expressed with the formula [I] ##STR1## Where R 1 denotes hydrogen or an acetyl group, R 2 denotes hydrogen or a lower alkyl group, R 3 denotes C 2 H 4 , C 3 H 6 or C 2 H 2 , R 4 denotes an hydroxyl group, the residue left after removing hydrogen from the alcohol portion of the active ester or alkyloxycarbonyloxy group, AC denotes an acetyl group, Ph denotes an phenyl group, and X denotes oxygen or sulfur. This sialic acid derivative has high reactivity because it has active ester groups in the molecules and can be used as a raw material or intermediate for synthesis of various sialic acid derivatives.
专利号:US-2002045747-A1 优先权日:1996-12-23 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
专利号:US-2002052359-A1 优先权日:1996-12-23 标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting B-amyloid peptide release and/or its synthesis by use of such compounds
专利号:US-2002173504-A1 优先权日:1996-12-23 标题 :Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting B-amyloid peptide release and/or its synthesis by use of such compounds
专利号:US-2004043977-A1 优先权日:1996-12-23 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
摘要:Farmatsevtichnii Zhurnal, (5)(39), 1987 参考文献:10.1016/j.bmcl.2010.01.098 摘要:Jha A, Mukherjee C, Prasad AK, Parmar VS, Vadaparti M, Das U, De Clercq E, Balzarini J, Stables JP, Shrivastav A, Sharma RK, Dimmock JR. Derivatives of aryl amines containing the cytotoxic 1,4-dioxo-2-butenyl pharmacophore. Bioorganic & Medicinal Chemistry Letters. 2010 Mar;20(5):1510–5. doi: 10.1016/j.bmcl.2010.01.098.