CAS: 1194-86-1; (R)-2-Amino-2-(Thiophen-3-yl)Acetic Acid

该化合物是一种氨基酸衍生物,其特点是与氨基酸结构的碳碳相连的硫苯环;该化合物的特点是氨基氨基酸组(-NH2),一个碳酸组(-COOH),以及硫苯酯,它有助于其独特的特性.它通常是白色到白晶体外的固体,在水中溶解,反映了氨基和氨基酸的功能组的极性.硫苯环具有独特的电子和消毒特性,影响其在生物系统中的再活动与互动.该化合物对制药研究和生物化学研究感兴趣,特别是考虑到其在...

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1194-87-2 38150-49-1 40512-57-0

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CAS号498-62-4 3-噻吩甲醛

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    专利信息


    专利号:US-7060818-B2
    优先权日:2003-02-21
    标题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process
    发明人:HORWITZ COLIN P; GHOSH ANINDYA
    权利人:UNIV CARNEGIE MELLON
    摘要:An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate. Following deprotection, the diamide diamine intermediate is reacted with an activated diacid, such as an activated malonate, oxalate or succinate derivative to form the macrocyclic tetraamido compound. The macrocyclic tetraamido compound may further be complexed with a transition metal.

    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:WO-9967219-A1
    优先权日:1998-06-22
    标 题:Compounds for inhibiting beta-amyloid peptide release and/or its synthesis
    发明人:AUDIA JAMES E; PORTER WARREN J; THOMPSON RICHARD C; WILKIE STEPHEN C; STACK DOUGLAS R; SHI QING
    权利人:ELAN PHARM INC; LILLY CO ELI; AUDIA JAMES E; PORTER WARREN J; THOMPSON RICHARD C; WILKIE STEPHEN C; STACK DOUGLAS R; SHI QING
    摘要:Compounds of formula (I), wherein W is a cyclic group of the type (2); (3); Y is represented by the formula (II); these compounds 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-6774125-B2
    优先权日:1998-06-22
    标 题:Deoxyamino acid 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:AUDIA JAMES E; THOMPSON RICHARD C; WILKIE STEPHEN C; BRITTON THOMAS C; PORTER WARREN J; HUFFMAN GEORGE W; LATIMER LEE H
    权利人:ELAN PHARM 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-6509331-B1
    优先权日:1998-06-22
    标题:Deoxyamino acid 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:AUDIA JAMES E; THOMPSON RICHARD C; WILKIE STEPHEN C; BRITTON THOMAS C; PORTER WARREN J; HUFFMAN GEORGE W; LATIMER LEE H
    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: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.

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    主要参考文献

    [参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.

    合成参考文献


    参考文献:10.1016/j.bmc.2010.05.077
    摘要:Ruda GF, Campbell G, Alibu VP, Barrett MP, Brenk R, Gilbert IH. Virtual fragment screening for novel inhibitors of 6-phosphogluconate dehydrogenase. Bioorganic & Medicinal Chemistry. 2010 Jul;18(14):5056–62. doi: 10.1016/j.bmc.2010.05.077.
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