专利号:EP-0946499-B1 优先权日:1996-11-22 标 题 :N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:WU JING; TUNG JAY S; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; EID CLARK NORMAN; AUDIA JAMES E 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta -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 beta -amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions. Said compounds are represented by formula (I), wherein R<1> is selected from the group consisting of: a) alkyl, alkenyl, alkaryl, alkcycloalkyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl and heterocyclic; b) a substituted phenyl group of formula (II), wherein R is alkylene of from 1 to 8 carbon atoms, m is an integer equal to 0 or 1, and c) 1- or 2-naphthyl substituted at the 5, 6, 7 and/or 8 positions, R<2> is selected from the group consisting of hydrogen, alkyl of from 1 to 4 carbon atoms, alkylalkoxy of from 1 to 4 carbon atoms, alkylthioalkoxy of from 1 to 4 carbon atoms; and R<3> and R<3'> are independently selected from the group consisting of: (a) hydrogen, (b) alkyl, (c) -(R<7>)n(W)p, wherein R<7> is an alkylene group, W is selected from the group consisting of (i) formula (A); (ii) heteroaryl; and (iii) N-heterocyclic, and n is an integer equal to 0 or 1, and p is an integer equal to 1 to 3; (d) -CH( phi )CH2C(O)O-Q where Q is selected from the group consisting of alkyl, aryl, heteroaryl and heterocyclic; X' is hydrogen, hydroxy or fluoro; X'' is hydrogen, hydroxy or fluoro, or X' and X'' together form an oxo group, Z is selected from the group consisting of a bond covalently linking R<1> to -CX'X''-, oxygen and sulfur.
专利号:US-6849650-B2 优先权日:1998-02-27 标 题:Heterocyclic 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; PORTER WARREN J; NISSEN JEFFREY S; LATIMER LEE H; AUDIA JAMES E; DROSTE JAMES 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:EP-0951464-B1 优先权日:1996-11-22 标题:N-(aryl/heteroarylacetyl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:WU JING; THORSETT EUGENE D; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; JOHN VARGHESE; FANG LAWRENCE Y; AUDIA JAMES E 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta -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 beta -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:EP-0951466-B1 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 发明人:WU JING; TUNG JAY S; THORSETT EUGENE D; PLEISS MICHAEL A; NISSEN JEFFREY S; NEITZ JEFFREY; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; DROSTE JAMES J; HENRY STEVEN S; MCDANIEL STACEY L; SCOTT WILLIAM L; STUCKY RUSSELL D 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds for Formula (I) wherein the substituents are as defined in the claims 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-6262302-B1 优先权日:1996-11-22 标题:N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:WU JING; TUNG JAY S; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; EID CLARK N; AUDIA JAMES E 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits beta-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-6333351-B1 优先权日:1996-11-22 标题:N-(aryl/heteroarylacetyl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:WU JING; THORSETT EUGENE D; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; JOHN VARGHESE; FANG LAWRENCE Y; AUDIA JAMES E 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits beta-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
[参考文献]: Andreas Aemissegger, Et Al. Synthesis And Application Of An Azobenzene Amino Acid As A Light-Switchable Turn Element In Polypeptides. Nat Protoc. 2007;2(1):161-7.
合成参考文献
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