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    8-quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors
    1.
    发明授权
    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：US07019136B2

    公开(公告)日：2006-03-28

    申请号：US10937639

    申请日：2004-09-09

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

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

    IPC分类号： C07D239/02

    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）化合物：R 1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，或任选地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， 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，任选地被一个或多个选自卤素，氰基，羟基，烷基，羟烷基，烷氧基烷基，烷硫基 烷基，烷氧基，烷硫基，烯基，烷氧基羰基，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
    2.
    发明授权
    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：US06919337B2

    公开(公告)日：2005-07-19

    申请号：US10644328

    申请日：2003-08-20

    申请人： Gurdip Bhalay ,  Stephen Paul Collingwood ,  Robin Alec Fairhurst ,  Sylvie Felicite Gomez ,  Ret Naef ,  David Andrew Sandham

    发明人： Gurdip Bhalay ,  Stephen Paul Collingwood ,  Robin Alec Fairhurst ,  Sylvie Felicite Gomez ,  Ret Naef ,  David Andrew Sandham

    IPC分类号： C07D473/04 ,  C07D473/06 ,  A61K31/5355 ,  A61P15/10 ,  C07D473/02

    CPC分类号： 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。

    Organic Compounds
    6.
    发明申请
    Organic Compounds 有权
    有机化合物

    公开(公告)号：US20090221578A1

    公开(公告)日：2009-09-03

    申请号：US12096332

    申请日：2006-12-07

    申请人： David Andrew Sandham

    发明人： David Andrew Sandham

    IPC分类号： A61K31/5377 ,  C07D413/10 ,  A61P11/00

    CPC分类号： C07D209/10

    摘要： There are provided according to the invention compounds of formula (I) in free or salt form, wherein R1, R2, R4, R5, R6, D, X, W, m and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.

    摘要翻译： 根据本发明，提供游离或盐形式的式（I）化合物，其中R 1，R 2，R 4，R 5，R 6，D，X，W，m和n如说明书中所述， ，以及作为药物的用途。

    COMBINATIONS OF STEROIDS AND METHYLXANTHINE COMPOUNDS
    10.
    发明申请
    COMBINATIONS OF STEROIDS AND METHYLXANTHINE COMPOUNDS 审中-公开
    STEROIDS和甲基噻嗪化合物的组合

    公开(公告)号：US20090018109A1

    公开(公告)日：2009-01-15

    申请号：US12279854

    申请日：2007-02-22

    申请人： David Andrew Sandham

    发明人： David Andrew Sandham

    IPC分类号： A61K31/56 ,  A61P11/00

    CPC分类号： A61K31/522 ,  A61K31/56 ,  A61K45/06

    摘要： There is provided a medicament comprising a combination of a methylxanthine compound of formula I and a steroid of formula II and their use as pharmaceuticals, in particular for the treatment of inflammatory or obstructive airways diseases.

    摘要翻译： 提供了包含式I的甲基黄嘌呤化合物和式II的类固醇及其作为药物的用途，特别是用于治疗炎性或阻塞性气道疾病的组合的药物。