CAS: 51285-13-3; N-Hydroxycyclopropanecarboximidamide

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57297-29-7 22926-85-8 70458-18-3

上下游产品

CAS号5500-21-0 环丙基腈

专利信息

专利号:US-5124460-A
优先权日:1991-05-06
标 题 :Enantioselective synthesis of 3-substituted 1-azabicyclo (2.2.1)heptanes
发明人：HUMPHREY GUY R
权利人:MERCK SHARP & DOHME
摘要:A process for preparing a substantially pure enantiomer of a compound formula (I) ##STR1## wherein X is O or S; and n R 2 represents hydrogen, --CF 3 , --OR 7 , --SR 7 , --NR 7 R 8 , --CN, --COOR 7 , --CONR 7 R 8 , or a saturated or unsaturated, substituted or unsubstituted hydrocarbon group, wherein R 7 and R 8 are independently selected from hydrogen and C 1-2 alkyl provided that --NR 7 R 8 is other than NH 2 ; n which process comprises cyclization of a compound of formula (10) or salt thereof: ##STR2## wherein X and R 2 are as defined in formula (I); and R 4 is a labile leaving group and optionally epimerizing the endo-diastereomer so prepared to produce the corresponding exo-diastereomer.

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:US-6399628-B1
优先权日:1996-11-22
标 题 :N-(aryl/heteroaryl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting alpha- amyloid peptide release and/or its synthesis by use of such compounds
发明人：AUDIA JAMES E; FOLMER BEVERLY K; JOHN VARGHESE; LATIMER LEE H; NISSEN JEFFREY S; REEL JON K; THORSETT EUGENE D; WHITESITT CELIA A
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-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-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-5134146-A
优先权日:1990-05-13
标题:Substituted oxadiazoles and thiadiazoles for use in the treatment of glaucoma
发明人：SHOWELL GRAHAM; LOTTI VICTOR
权利人:MERCK SHARP & DOHME
摘要:The use of compounds for formula (I): ##STR1## or a salt or prodrug thereof; wherein one of X, Y, or Z is an oxygen or sulphur atom and the other two are nitrogen atoms, and the dotted circle represents two double bonds thus forming a 1,3,4-oxadiazole, 1,2,4-oxadiazole, 1,3,4-thiadiazole or 1,2,4-thiadiazole nucleus; n R 1 represents a non-aromatic azacyclic or azabicyclic ring system selected from ##STR2## wherein the broken line represents an optional chemical bond; the substituents R 3 and R 4 may be present at any position, including the point of attachment to the oxa- or thia-diazole ring, and independently represent hydrogen, C 1-4 alkyl, halo, C 1-4 alkoxy, hydroxy or carboxy, or R 3 and R 4 together represent carbonyl; n the group R 5 represents hydrogen or C 1-4 alkyl; and n R 2 represents hydrogen, C 1-8 hydrogen, C 1-8 alkyl optionally substituted by hydroxy or fluoro, C 2-8 alkenyl, OR 7 , SR 7 , NR 7 R 8 , CN, CO 2 R 7 , CONR 7 R 8 OR NHCONHR 9 where R 9 is C 1-4 alkyl; wherein R 7 and R 8 independently represent hydrogen or saturated or unsaturated C 1-4 alkyl provided that, when R 7 and R 8 in NR 7 R 8 are both hydrogen, at least one of R 3 and R 4 is C 1-4 alkyl, n in the treatment of glaucoma, novel compounds having such use, formulations containing them and their synthesis.