发明名称 D-PROLINE DERIVATIVES
摘要 This invention refers to D-proline formulas which are: R SH, benzyl or phenyl, which is optionally substituted by hydroxy or lower alcoxy group or formula R1 hydrogen or halogen, X -(CH2)n-, -CH(R2)(CH2)n-, -CH2O(CH2)n-, -CH2NH-, benzyl, -C(R2)=CH-, -CH2CH(OH)- or tyazol-2,5-diil, Y -S-S-, -(CH2)n-, -O-, -NH-, -N(R2)-, -CH=CH-, -NHC(O)NH-, -N(R2)C(O)N(R2)-, -N[CH2C6H3(OCH3)2]-, -N(CH2C6H5)-, -N(CH2C6H5)C(O)N(CH2C6H5)-, -N(alcoxyalkyl)-, -N(cycloalkyl-metyl)-, 2,6-pyridil, 2,5-furanil, 2,5-thienil, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,4-cyclohexyl, 1,2-naphthyl, 1,4-naphthyl, 1,5-naftyl, 1,6-naphthyl, biphenylene or 1,2-phenylene, 1,3-phenylene i 1,4-phenylene, whereas phenyl groups are supstituted optionally by 1-4 supstituents, that are chosen among halogenes, lower alkyl-, lower alcoxy-, hidroxy-, carboxy-, -COO-lower alkyl-, nitrilo-, 5-tetrazole-, (2-carboxy acid-pirolidine-1-or)-2-oxo-etoxy-, N-hidroxycarbamidoile-, 5-oxo-[1,2,4]oksadiazolil, 2-okso[1,2,3,5]- oxatyadiazolyl-, 5-thioxo-[1,2,4]oxadiazolil i 5-terc-butylsulphaniy-[1,2,4]oxadiazolil-group, X' -(CH2)n-, -(CH2)nCH(R2)-, -(CH2)nOCH2-, -NHCH2-, benzyl, -CH=C(R2)-, -CH(OH)CH2- or tiazole-2,5-diil, R2 low alkyl, lower alcoxy or benzyl and n 0-3, and other pharmaceutically acceptable salts and mono - and diesters. D-prolines formules I-A and I-B can be applied in the healing and prevention of all sorts of central and system amiloidose.
申请公布号 YU47698(A) 申请公布日期 2001.07.10
申请号 YU19980000476 申请日期 1998.10.28
申请人 F.HOFFMANN-LA ROCHE AG. 发明人 HERTEL, CORNELIA;HOFFMANN, TORSTEN;JAKOB-ROETNE, ROLAND;NORCROSS, ROGER DAVID
分类号 C07K5/078;A61K31/00;A61K31/40;A61K31/401;A61K31/4015;A61K38/08;A61P3/00;A61P3/10;A61P9/04;A61P9/10;A61P25/00;A61P25/28;A61P43/00;C07D207/16;C07D207/22;C07D207/277;C07D401/14;C07D403/06;C07D403/12;C07D403/14;C07D405/14;C07D409/14;C07D413/14;C07D417/14;C07D419/14;C07D521/00 主分类号 C07K5/078
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