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    • 3. 发明授权
    • Substituted lactose and lactosamine derivatives as cell adhesion
inhibitors
    • 取代的乳糖和乳糖胺衍生物作为细胞粘附抑制剂
    • US5567683A
    • 1996-10-22
    • US270874
    • 1994-07-01
    • Mina A. NashedFalguni DasguptaSaeed A. AbbasJohn H. MusserDarwin S. Asa
    • Mina A. NashedFalguni DasguptaSaeed A. AbbasJohn H. MusserDarwin S. Asa
    • C07H5/04A61K31/7008A61K31/7024A61K31/7028A61K31/7034A61K31/7042A61K31/715A61P29/00A61P37/06A61P37/08C07H3/06C07H5/10C07H13/04C07H15/20C07H17/00A61K31/70A61K38/00A61K38/16
    • C07H3/06
    • Simple lactose or lactosamine related compounds which behave as ligands for the ELAM-1 and related receptors are described. These compounds are useful in the treatment of conditions characterized by excess inflammation. These compounds are of the formula ##STR1## wherein each R.sup.1 is independently H or lower alkyl (1-4C); R.sup.2 is H, lower alkyl (1-4C), alkylaryl or one or more additional saccharide residues;R.sup.3 and R.sup.4 are each independently H, alkyl(1-6C), aryl or R.sup.3 and R.sup.4, taken together, form a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ;wherein said five- or six-membered ring may further be substituted by one or more substituents selected from the group consisting of (CHOR.sup.1).sub.m H wherein m is 1-4, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NHCOR.sup.1, and SR.sup.1 ;Y is H, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NCOR.sup.1 or SR.sup.1 ; andX is --CHR.sup.5 (CHOR.sup.1).sub.2 CHR.sup.6 OR.sup.1 wherein R.sup.5 and R.sup.6 are each independently H, lower alkyl(1-4C) optionally substituted with one or more F, or result in a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ;said five- or six-membered ring optionally substituted with one substituent selected from the group consisting of R.sup.1, CH.sub.2 OR.sup.1, OR.sup.1, OOCR.sup.1, NR.sup.1.sub.2, NHCOR.sup.1, SR.sup.1 and F;or X is benzoyl or naphthoyl having 1-3 hydroxyl substituents,with the proviso that if X represents a hexose substituent R.sup.3 and R.sup.4, taken together, cannot provide a hexose substituent.
    • 描述了作为ELAM-1和相关受体的配体的简单的乳糖或乳糖胺相关化合物。 这些化合物可用于治疗以过量炎症为特征的病症。 这些化合物具有式“IMAGE”,其中每个R 1独立地是H或低级烷基(1-4C); R2是H,低级烷基(1-4C),烷基芳基或一个或多个另外的糖残基; R 3和R 4各自独立地为H,烷基(1-6C),芳基或R 3和R 4一起形成任选含有选自O,S和NR 1的杂原子的五元或六元环; 其中所述五元或六元环可以进一步被一个或多个选自(CHOR1)mH的取代基取代,其中m是1-4,OR1,OOCR1,NR12,NHCOR1和SR1; Y是H,OR1,OOCR1,NR12,NCOR1或SR1; 并且X是-CHR 5(CHOR 1)2 CHR 6OR 1,其中R 5和R 6各自独立地为H,任选地被一个或多个F取代的低级烷基(1-4C),或者产生任选含有选自以下的杂原子的五元或六元环 由O,S和NR1组成的组; 所述五元或六元环任选被一个选自由R 1,CH 2 OR 1,OR 1,OOCR 1,NR 12,NHCOR 1,SR 1和F的取代基取代; 或X是具有1-3个羟基取代基的苯甲酰基或萘甲酰基,条件是如果X表示己糖取代基R 3和R 4一起不能提供己糖取代基。
    • 10. 发明授权
    • Substituted indole-, indene-, pyranoindole- and
tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and
lipoxygenase
    • 取代的吲哚,茚,吡喃吲哚和四氢咔唑 - 链烷酸衍生物作为PLA2和脂氧合酶的抑制剂
    • US5229516A
    • 1993-07-20
    • US911434
    • 1992-07-10
    • John H. MusserAnthony F. Kreft, IIIAmedeo A. FailliChristopher A. DemersonUresh S. ShahJames A. Nelson
    • John H. MusserAnthony F. Kreft, IIIAmedeo A. FailliChristopher A. DemersonUresh S. ShahJames A. Nelson
    • C07C323/62C07D209/22C07D215/14C07D401/12C07D401/14C07D417/12C07D491/04
    • C07D401/12C07C323/62C07D209/22C07D215/14C07D401/14C07D417/12C07D491/04
    • There are disclosed compounds of the formulaA(CH.sub.2).sub.n O-BwhereinA is C.sub.4 -C.sub.8 alkyl, phenoxyethyl, phenoxyphenyl or a group having the formula ##STR1## wherein ##STR2## R.sup.1 is hydrogen, lower alkyl, phenyl or phenyl substituted with trifluoromethyl;R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring;R.sup.3 is hydrogen or lower alkyl;n is 1-2;B is ##STR3## wherein ##STR4## m is 0-3; R.sup.5 is ##STR5## or phenyl or phenyl substituted by halo, lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl;R.sup.6 is A(CH.sub.2).sub.n O-- or halo; with the proviso that when R.sup.6 is halo, R.sup.5 is ##STR6## R.sup.7 is lower alkyl; Y is --CH.sub.2 -- or --O--;R.sup.8 is lower alkyl or --(CH.sub.2).sub.m CO.sub.2 R.sup.3 ;R.sup.9 is ##STR7## or --CH.sub.2 R.sup.10 ; R.sup.10 is lower alkyl, phenyl, phenyl substituted with carboxy, halo, loweralkylthio or loweralkylsulfinyl, pyridyl, furanyl or quinolinyl;R.sup.11 is lower alkyl or phenyl;Z is hydrogen, lower alkyl or --N(CH.sub.3)OH;and the pharmacologically acceptable salts thereof, and their use in the treatment of inflammatory conditions, such as rheumatoid arthritis, ulcerative colitis, psoriasis and other immediate hypersensitivity reactions; in the treatment of leukotriene-mediated naso-bronchial obstructive air-passageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like; and as gastric cytoprotective agents.
    • 公开了式A(CH 2)n O-B的化合物,其中A是C 4 -C 8烷基,苯氧基乙基,苯氧基苯基或具有下式的基团:其中R 1是氢,低级烷基 ,苯基或被三氟甲基取代的苯基; R2是氢或低级烷基; 或R 1和R 2一起形成苯环; R3是氢或低级烷基; n为1-2; B是 其中 m是0-3; R 5为苯基或被卤素,低级烷硫基,低级烷基亚磺酰基或低级烷基磺酰基取代的苯基; R6是A(CH2)nO-或卤素; 条件是当R 6为卤素时,R 5为低级烷基; Y是-CH 2 - 或-O-; R8是低级烷基或 - (CH2)mCO2R3; R9是或-CH2R10; R 10为低级烷基,苯基,被羧基,卤素,低级烷硫基或低级烷基亚磺酰基取代的苯基,吡啶基,呋喃基或喹啉基; R11为低级烷基或苯基; Z是氢,低级烷基或-N(CH 3)OH; 及其药理学上可接受的盐及其在治疗炎性病症如类风湿性关节炎,溃疡性结肠炎,牛皮癣和其他立即超敏反应中的用途; 治疗白三烯介导的鼻支气管阻塞性通气条件,如过敏性鼻炎,过敏性支气管哮喘等; 和作为胃细胞保护剂。