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45 条记录 (耗时 0.035 秒)

    Diazacycloalkanedione derivatives
    33.
    发明授权
    Diazacycloalkanedione derivatives 失效
    二氮杂环烷二酮衍生物

    公开(公告)号：US06642225B2

    公开(公告)日：2003-11-04

    申请号：US09968389

    申请日：2001-10-02

    申请人： Rainer Albert ,  Janet Dawson ,  Claus Ehrhardt ,  Sompong Wattanasin ,  Gabriele Weitz-Schmidt ,  Karl Welzenbach

    发明人： Rainer Albert ,  Janet Dawson ,  Claus Ehrhardt ,  Sompong Wattanasin ,  Gabriele Weitz-Schmidt ,  Karl Welzenbach

    IPC分类号： C07D24100

    CPC分类号： C07D401/06 ,  A61K31/4965 ,  A61K31/551 ,  C07D241/08 ,  C07D243/08 ,  C07D401/12

    摘要： Compounds of formula I wherein R is carboxy, esterified carboxy or amidated carboxy; R1 and R3 are independently lower alkyl, (hydroxy, lower alkoxy, amino, acylamino, mono- or di-lower alkylamino or mercapto)-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, cycloalkyl, aryl, biaryl, (cycloalkyl, aryl or biaryl)-lower alkyl, or (carboxy, esterified carboxy or amidated carboxy)-lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, arylaminocarbonyl, or aryl-(oxy, thio or amino); n is 1 or 2; Y is lower-alkylene or lower alkenylene; and pharmaceutically acceptable salts thereof; which are useful as LFA-1 antagonists.

    摘要翻译： 式I化合物，其中R是羧基，酯化的羧基或酰胺化的羧基; R 1和R 3独立地是低级烷基，（羟基，低级烷氧基，氨基，酰氨基，一或二低级烷基氨基或巯基） - 低级烷基，低级烷基 - （ （环烷基，芳基或联芳基） - 低级烷基，或（羧基，酯化的羧基或酰胺基羧基） - 低级烷基; R2是氢，低级烷基，环烷基， 芳基，联芳基，芳基氨基羰基或芳基 - （氧基，硫代或氨基）; n为1或2; Y为低级亚烷基或低级亚烯基;及其药学上可接受的盐; 其作为LFA-1拮抗剂是有用的。

    Substituted 2-oxo-1,4-diazacycloalkanes
    34.
    发明授权
    Substituted 2-oxo-1,4-diazacycloalkanes 失效
    取代的2-氧代-1,4-二氮杂环烷烃

    公开(公告)号：US06399599B1

    公开(公告)日：2002-06-04

    申请号：US09686511

    申请日：2000-10-11

    申请人： Rainer Albert ,  Josef G. Meingassner ,  Sompong Wattanasin ,  Gabriele Weitz-Schmidt ,  Karl Welzenbach ,  Ulrich Hommel ,  Claus Ehrhardt ,  Didier Roche ,  Joerg Kallen

    发明人： Rainer Albert ,  Josef G. Meingassner ,  Sompong Wattanasin ,  Gabriele Weitz-Schmidt ,  Karl Welzenbach ,  Ulrich Hommel ,  Claus Ehrhardt ,  Didier Roche ,  Joerg Kallen

    IPC分类号： C07D40106

    CPC分类号： C07K5/06034 ,  A61K38/00 ,  C07D243/08 ,  C07K5/02 ,  C07K5/06078

    摘要： Compounds of formula I wherein n is 1, 2 or 3; R1 is H, C1-4alkyl, aryl, or aryl-C1-4alkyl; Y is C1-4alkylene, —CO—C1-4alkylene, —CO—C2-5alkenylene, —CO—NH—, —CO—C1-3alkylene-NH—, or —CO—O—; R2 is an aromatic or heteroaromatic residue, each being optionally substituted by CF3, halogen, OH, C1-4alkoxy, amino, mono- or di-C1-4alkyl substituted amino, phenyl, benzyl or C1-4alkyl optionally substituted by amino; R3is the side chain present on the C&agr; of an &agr;-amino acid; R4 is biphenylyl, benzyl, hydroxy-benzyl, &agr;- or &bgr;-naphthyl-methyl, 5,6,7,8-tetrahydro-&bgr;-naphthyl-methyl or indolyl-methyl, each being optionally substituted on the ring by CF3, halogen, OH, C1-4alkoxy, amino, mono- or di-C1-4alkyl substituted amino, phenyl, benzyl or C1-4alkyl optionally substituted by amino; and X is —CN, —NR5R6 or —O—R8 wherein R5 is H, C1-6alkyl, aryl or aryl-C1-4alkyl; R6 is H or C1-6alkyl; and R8 is H, C1-4alkyl, aryl or aryl-C1-4alkyl; in free form or in salt form; which are useful in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1, -ICAM-2 or -ICAM-3 interactions.

    摘要翻译： 其中n为1,2或3的式I化合物; R 1是H，C 1-4烷基，芳基或芳基-C 1-4烷基; Y是C1-4亚烷基，-CO-C1-4亚烷基，-CO-C2-5亚烯基，-CO-NH-，-CO-C1-3亚烷基-NH-或-CO-O-; R 2是芳族或杂芳族残基，其各自任选被CF 3，卤素，OH，C 1-4烷氧基，氨基，单或二C 1-4烷基取代的氨基，苯基，苄基或任选被氨基取代的C 1-4烷基取代; R3是存在于α-氨基酸的Calpha上的侧链; R4是联苯基，苄基，羟基 - 苄基，α-或β-萘基 - 甲基，5,6,7,8-四氢-β-萘基 - 甲基或吲哚基 - 甲基，其各自在环上被CF 3任选取代，卤素 ，OH，C 1-4烷氧基，氨基，单或二-C 1-4烷基取代的氨基，苯基，苄基或任选被氨基取代的C 1-4烷基; 并且X是-CN，-NR 5 R 6或-O-R 8，其中R 5是H，C 1-6烷基，芳基或芳基-C 1-4烷基; R6是H或C1-6烷基; 且R 8为H，C 1-4烷基，芳基或芳基-C 1-4烷基; 以游离形式或盐形式; 其可用于预防或治疗由LFA-1 / ICAM-1，-ICAM-2或-ICAM-3相互作用介导的疾病或疾病。