Phenoxy- and phenoxyalkyl-piperidines as antiviral agents
    113.
    发明授权
    Phenoxy- and phenoxyalkyl-piperidines as antiviral agents 失效
    苯氧基和苯氧基烷基 - 哌啶作为抗病毒剂

    公开(公告)号:US5364865A

    公开(公告)日:1994-11-15

    申请号:US998498

    申请日:1992-12-30

    申请人: Guy D. Diana

    发明人: Guy D. Diana

    CPC分类号: C07D401/14 C07D413/14

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## Y is a bond or lower alkylene; R.sub.2 and R.sub.3 are independently hydrogen, lower-alkyl or halogen;R.sub.4 is ##STR3## R.sub.5 is hydrogen, lower-alkyl or halogen; R.sub.6 is hydrogen, lower-alkyl or halogen;R.sub.7 is hydrogen or lower-alkyl;R.sub.8 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.9 is lower-alkyl;R.sub.10 is lower-alkyl, trifluoromethyl or difluoromethyl;or pharmaceutically acceptable acid addition salts thereof are useful as antiviral agents.

    摘要翻译: 其中R 1选自Y的结构式为的化合物是下式的键或低级亚烷基; R2和R3独立地是氢,低级烷基或卤素; R4是氢,低级烷基或卤素; R6是氢,低级烷基或卤素; R7是氢或低级烷基; R8是氢,低级烷基或三氟甲基; R9为低级烷基; R10为低级烷基,三氟甲基或二氟甲基; 或其药学上可接受的酸加成盐可用作抗病毒剂。

    1-acylpiperidine compounds
    114.
    发明授权
    1-acylpiperidine compounds 失效
    1-酰基哌啶化合物

    公开(公告)号:US5310743A

    公开(公告)日:1994-05-10

    申请号:US929186

    申请日:1992-08-11

    摘要: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.3 is carbonyl, oxo-lower-alkylene, oxo(aza)-lower-alkylene or an alkylene radical which is optionally substituted by phenyl, hydroxymethyl, optionally esterified or amidated carboxyl or, in higher than the .alpha. position, by hydroxyl, and its salts have substance-P-antagonistic properties and can be used as pharmaceutically active substances in pharmaceuticals for the treatment of disorders in whose development substance P plays an essential part.

    摘要翻译: 式I的1-酰基哌啶化合物其中R 1是任选取代的芳烷基,芳氧基烷基,杂芳烷基,芳酰基,杂芳酰基,环烷基羰基,芳烷酰基,杂芳基烷酰基,芳烷氧基羰基或芳基氨基甲酰基或α-氨基的酰基 酸,其任选被低级烷酰基或氨基甲酰基 - 低级 - 烷酰基N-取代,R 2是环烷基或任选取代的芳基或杂芳基,R 3是氢,烷基,氨基甲酰基或任选被羧基或酯化的烷酰基或烯酰基 或酰胺化的羧基,R 4是任选取代的芳基或任选部分氢化的杂芳基,X 1是亚甲基,亚乙基,直链,任选的缩酮化羰基或任选醚化的羟基亚甲基,X 2是亚烷基,羰基或直链, X 3是羰基,氧代 - 低级 - 亚烷基,氧代(氮杂) - 低级 - 亚烷基或任选被苯基取代的亚烷基, 羟甲基,任选酯化或酰胺化的羧基,或高于α位置的羟基,其盐具有物质P-拮抗性质,可用作药物中的药物活性物质,用于治疗其发育物质P所起的障碍 一个重要的部分。