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    8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors
    7.
    发明申请
    8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors 审中-公开
    8-喹啉黄嘌呤和8-异喹啉黄嘌呤衍生物作为PDE 5抑制剂

    公开(公告)号：US20060173181A1

    公开(公告)日：2006-08-03

    申请号：US11274030

    申请日：2005-11-15

    申请人： Gurdip Bhalay ,  Stephen Collingwood ,  Robin Fairhurst ,  Sylvie Gomez ,  Reto Naef ,  David Sandham

    发明人： Gurdip Bhalay ,  Stephen Collingwood ,  Robin Fairhurst ,  Sylvie Gomez ,  Reto Naef ,  David Sandham

    IPC分类号： C07D473/04 ,  A61K31/522

    CPC分类号： C07D239/545 ,  A61K31/522 ,  C07D473/04 ,  C07D473/06

    摘要： A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula —N(R6)R7, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R6 and R7 are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R6 and R7 is hydrogen and the other is acyl, or R6 and R7 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclyl group.

    摘要翻译： 式（I）R 1的化合物是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 2是氢，烷基，羟基烷基，烷基羰氧基烷基，烷氧基烷基， 烷基硫代烷基，烯基，环烷基烷基，杂环基烷基，芳烷基，其中其芳基环任选地与5元杂环基稠合，或任选被一个或多个选自烷氧基，氨基，烷基氨基，二烷基氨基，酰氨基，卤素，羟基， 氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基氨基或二烷基氨基磺酰基氨基，R 3是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 4是氢或烷基，R 0 任选地与5元杂环基稠合并且任选地被一个或多个选自卤素，氰基，羟基，烷基，羟基烷基，烷氧基烷基，烷硫基的取代基取代的喹啉基，异喹啉基或氧代二氢异喹啉基 烷基，烷氧基，烷硫基，烯基，烷氧基羰基，炔基，羧基，酰基，式-N（R 6）R 7的基团，任选地被一个或多个 选自卤素或烷氧基的取代基或具有5或6个环原子通过环碳原子连接到指定碳原子的杂芳基，R 6和R 7各自独立地 任选被羟基或烷氧基取代的氢或烷基或R 6和R 7中的一个是氢，另一个是酰基或R 6和 R 7与它们所连接的氮原子一起表示5-或6-元杂环基。

    8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors
    8.
    发明申请
    8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors 失效
    8-喹啉黄嘌呤和8-异喹啉黄嘌呤衍生物作为PDE 5抑制剂

    公开(公告)号：US20060106214A1

    公开(公告)日：2006-05-18

    申请号：US11329889

    申请日：2006-01-11

    申请人： Gurdip Bhalay ,  Stephen Collingwood ,  Robin Fairhurst ,  Sylvie Gomez ,  Reto Naef ,  David Sandham

    发明人： Gurdip Bhalay ,  Stephen Collingwood ,  Robin Fairhurst ,  Sylvie Gomez ,  Reto Naef ,  David Sandham

    IPC分类号： A61K31/522 ,  C07D473/04

    CPC分类号： C07D239/545 ,  A61K31/522 ,  C07D473/04 ,  C07D473/06

    摘要： A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsufonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula —N(R6)R7, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R6 and R7 are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R6 and R7 is hydrogen and the other is acyl, or R6 and R7 together with the nitrogen atom to which they are attached denote a 5- or 6- membered heterocyclyl group.

    摘要翻译： 式（I）R 1的化合物是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 2是氢，烷基，羟基烷基，烷基羰氧基烷基，烷氧基烷基， 烷基硫代烷基，烯基，环烷基烷基，杂环基烷基，芳烷基，其中其芳基环任选地与5元杂环基稠合，或任选被一个或多个选自烷氧基，氨基，烷基氨基，二烷基氨基，酰氨基，卤素，羟基， 氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基氨基或二烷基氨基磺酰基氨基，R 3是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 4是氢或烷基，R 0 任选地与5元杂环基稠合并且任选地被一个或多个选自卤素，氰基，羟基，烷基，羟基烷基，烷氧基烷基，烷基硫基的取代基取代的喹啉基，异喹啉基或氧代二氢异喹啉基 烷基，烷硫基，烯基，烷氧基羰基，炔基，羧基，酰基，式-N（R 6）R 7的基团，任选地被一个或多个 选自卤素或烷氧基的取代基或具有5或6个环原子通过环碳原子连接到指定碳原子的杂芳基，R 6和R 7各自独立地 任选被羟基或烷氧基取代的氢或烷基或R 6和R 7中的一个是氢，另一个是酰基或R 6和 R 7与它们所连接的氮原子一起表示5-或6-元杂环基。

    8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors
    9.
    发明申请
    8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors 失效
    8-喹啉黄嘌呤和8-异喹啉黄嘌呤衍生物作为PDE 5抑制剂

    公开(公告)号：US20050054660A1

    公开(公告)日：2005-03-10

    申请号：US10937639

    申请日：2004-09-09

    申请人： Gurdip Bhalay ,  Stephen Collingwood ,  Robin Fairhurst ,  Sylvie Gomez ,  Reto Naef ,  David Sandham

    发明人： Gurdip Bhalay ,  Stephen Collingwood ,  Robin Fairhurst ,  Sylvie Gomez ,  Reto Naef ,  David Sandham

    IPC分类号： C07D239/54 ,  C07D239/545 ,  C07D473/04 ,  C07D473/06 ,  C07D473/02 ,  A61K31/522

    CPC分类号： C07D239/545 ,  A61K31/522 ,  C07D473/04 ,  C07D473/06

    摘要： A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula —N(R6)R7, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R6 and R7 are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R6 and R7 is hydrogen and the other is acyl, or R6 and R7 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclyl group.

    摘要翻译： 式（I）R 1的化合物是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 2是氢，烷基，羟基烷基，烷基羰氧基烷基，烷氧基烷基，烷硫基烷基，烯基，环烷基烷基，杂环基烷基， 其芳基环任选地与5元杂环基稠合或任选被一个或多个选自烷氧基，氨基，烷基氨基，二烷基氨基，酰氨基，卤素，羟基，氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基氨基或二烷基氨基磺酰基氨基的取代基取代， R 3是氢或任选地被羟基，烷氧基或烷硫基取代的烷基，R 4是氢或烷基，R 5是任选地与5元杂环基稠合的喹啉基，异喹啉基或氧代二氢异喹啉基， 被一个或多个选自卤素，氰基，羟基，烷基，羟基烷基，烷氧基烷基，烷硫基烷基，烷氧基，烷硫基，烯基，烷氧基羰基 烷基，炔基，羧基，酰基，式-N（R 6）R 7的基团，任选地被一个或多个选自卤素或烷氧基的取代基取代的芳基或具有5或6个环原子的杂芳基， R 6和R 7各自独立地为氢或任选被羟基或烷氧基取代的烷基或R 6和R 7中的一个为氢，另一个为酰基 或R 6和R 7与它们所连接的氮原子一起表示5-或6-元杂环基。

    5-Hydroxy-Benzothiazole Derivatives Having Beta-2-Adrenoreceptor Agonist Activity
    10.
    发明申请
    5-Hydroxy-Benzothiazole Derivatives Having Beta-2-Adrenoreceptor Agonist Activity 有权
    具有β-2-肾上腺素受体激动剂活性的5-羟基 - 苯并噻唑衍生物

    公开(公告)号：US20080096940A1

    公开(公告)日：2008-04-24

    申请号：US11718829

    申请日：2005-11-28

    申请人： Robin Fairhurst

    发明人： Robin Fairhurst

    IPC分类号： A61K31/428 ,  C07D277/68 ,  A61P11/00

    CPC分类号： C07D277/68

    摘要： Compounds of formula (I) in free or salt or solvate form, wherein T has the meaning as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the β2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

    摘要翻译： 游离或盐或溶剂化物形式的式（I）化合物，其中T具有说明书中指出的含义，可用于治疗通过β2 - 肾上腺素受体激活而预防或缓解的病症 。 还描述了含有化合物的药物组合物和制备该化合物的方法。