Antipicornaviral agents
    41.
    发明授权
    Antipicornaviral agents 失效
    止痒病毒药

    公开(公告)号:US5523312A

    公开(公告)日:1996-06-04

    申请号:US312724

    申请日:1994-09-27

    CPC分类号: C07D413/06 C07D413/14

    摘要: Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.

    摘要翻译: 本文公开了用于对抗小核糖核酸病毒和预防或治疗小RNA病毒感染的化合物和药物组合物。 化合物具有下式:其中Het1选自恶唑基,异恶唑基,恶二唑基; Y是3〜9个碳原子的亚烷基桥; Het2是苯并呋喃基或吲哚基; R 1和R 2各自独立地选自氢,卤素,乙酰基,烷基,烯基,氨基,烷硫基,羟基,羟基烷基,烷氧基烷基,烷硫基烷基,烷基亚磺酰基烷基,烷基磺酰基烷基,烷氧基,硝基,羧基,烷氧基羰基,二烷基氨基烷基,烷基氨基烷基,氨基烷基,二氟甲基 ,三氟甲基或氰基; 并且R 3是恶唑基,恶二唑基,异恶唑基或被烷基,卤素,烷氧基烷基,环烷基,卤代烷基,羟基烷基,烷氧基,羟基,呋喃基,噻吩基或氟代烷基取代的任何一个。 其N-氧化物或其药学上可接受的酸加成盐。

    GPR40 agonists
    43.
    发明授权
    GPR40 agonists 有权
    GPR40激动剂

    公开(公告)号:US07750048B2

    公开(公告)日:2010-07-06

    申请号:US11939039

    申请日:2007-11-13

    IPC分类号: A61K31/192 C07C59/64

    摘要: The invention is directed to compounds of Formula (I) useful as GPR40 agonists. Pharmaceutical compositions and methods of treating one or more conditions including, but not limited to, insulin resistance, hyperglycemia, obesity, diabetes such as NIDDM, and other disorders related to lipid metabolism, energy homeostasis, and complications thereof, using compounds of the invention are also described.

    摘要翻译: 本发明涉及用作GPR40激动剂的式(I)化合物。 使用本发明化合物治疗一种或多种病症的药物组合物和方法,包括但不限于胰岛素抵抗,高血糖症,肥胖症,糖尿病如NIDDM,以及与脂质代谢相关的其它障碍,能量稳态及其并发症, 也描述。

    Substituted quinoline derivatives useful as antipiconaviral agents
    46.
    发明授权
    Substituted quinoline derivatives useful as antipiconaviral agents 失效
    可用作抗病毒药物的取代喹啉衍生物

    公开(公告)号:US5514692A

    公开(公告)日:1996-05-07

    申请号:US449463

    申请日:1995-05-24

    CPC分类号: C07D413/06 C07D413/14

    摘要: The invention discloses compounds of the formula ##STR1## wherein, Het.sub.1 is chosen from the group consisting of substituted or unsubstituted furyl, oxazolyl, isoxazolyl, oxadiazolyl, tetrazolyl, thiadiazolylY is an alkylene bridge of 3 to 9 carbon atoms.Het.sub.2 is quinolyl quinolyl substituted by R.sub.1 and R.sub.2 ;R.sub.1 and R.sub.2 are each individually chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.3 is alkyltetrazolyl, or substituted or unsubstituted heterocyclyl chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, isoxazolyl, isothiazolyl, furyl, triazolyl, tetrazolyl, thiophenyl the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof are effective antipicornaviral agents.

    摘要翻译: 本发明公开了下式化合物:其中Het1选自取代或未取代的呋喃基,恶唑基,异恶唑基,恶二唑基,四唑基,噻二唑基,Y为3至9个碳原子的亚烷基桥。 Het2是被R1和R2取代的喹啉基喹啉基; R 1和R 2各自独立地选自氢,卤素,烷基,烯基,氨基,烷硫基,羟基,羟基烷基,烷氧基烷基,烷硫基烷基,烷基亚磺酰基烷基,烷基磺酰基烷基,烷氧基,硝基,羧基,烷氧基羰基,二烷基氨基烷基,烷基氨基烷基,氨基烷基,二氟甲基, 或氰基; R3是烷基四唑基,或者是取代或未取代的选自苯并恶唑基,苯并噻唑基,噻二唑基,咪唑基,二氢咪唑基,恶唑基,噻唑基,恶二唑基,吡唑基,噻唑基,恶唑基,呋喃基,三唑基,四唑基,噻吩基,其N-氧化物或其药学上可接受的酸 其加成盐是有效的抗虫病毒药剂。

    1-cyclopropyl-4-pyridyl-quinolinones
    47.
    发明授权
    1-cyclopropyl-4-pyridyl-quinolinones 失效
    1-环丙基-4-吡啶基 - 喹啉酮

    公开(公告)号:US5330992A

    公开(公告)日:1994-07-19

    申请号:US967473

    申请日:1992-10-23

    CPC分类号: C07D401/04 C07D401/14

    摘要: Compounds of formula ##STR1## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Z where Z is hydroxy, chloro, lower-alkylamino or dilower-alkylamino;R.sub.3 and R.sub.4 are each individually hydrogen or fluoro; andAr is phenyl, an aromatic 5- or 6-membered heterocycle or any of these substituted at one or more positions with lower-alkyl, fluoro, chloro, hydroxy, amino, lower-alkylamino, dilower-alkylamino, carboxy, sulfonamido, lower alkylsulfonamido, methylenedioxy, trifluoroacetamido, lower-alkanoylamino, or carbamoyl; and their pharmaceutically acceptable acid addition salts are useful as anticancer agents.

    摘要翻译: 其中R 1是氢,低级烷基或三氟甲基的式IMAMA的化合物; R2是低级烷基,三氟甲基或CH2Z,其中Z是羟基,氯,低级烷基氨基或二元 - 烷基氨基; R3和R4各自为氢或氟; 并且Ar是苯基,芳族的5或6元杂环,或者它们在一个或多个位置被低级烷基,氟,氯,羟基,氨基,低级烷基氨基,二元 - 二烷基氨基,羧基,亚磺酰氨基,低级 烷基亚磺酰氨基,亚甲二氧基,三氟乙酰胺基,低级烷酰氨基或氨基甲酰基; 其药学上可接受的酸加成盐可用作抗癌剂。