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    8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors
    12.
    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。

    Derivatives of 3-phenyl-n-(2-(4-benzyl)-piperidin-1-yl)-ethyl)-acrylamid with ccr-3-receptor antagonistic activity for use in the treatment of inflammations and allergic conditions
    16.
    发明授权
    Derivatives of 3-phenyl-n-(2-(4-benzyl)-piperidin-1-yl)-ethyl)-acrylamid with ccr-3-receptor antagonistic activity for use in the treatment of inflammations and allergic conditions 失效
    具有ccr-3-受体拮抗活性的3-苯基 - 正 - （2-（4-苄基） - 哌啶-1-基） - 乙基） - 丙烯酰胺的衍生物，用于治疗炎症和过敏性疾病

    公开(公告)号：US07259173B2

    公开(公告)日：2007-08-21

    申请号：US10478795

    申请日：2002-06-14

    申请人： Gurdip Bhalay ,  Clive Victor Walker

    发明人： Gurdip Bhalay ,  Clive Victor Walker

    IPC分类号： A61K31/445 ,  C07D211/14 ,  C07D211/18 ,  C07D211/48

    CPC分类号： C07D211/14 ,  C07D211/18 ,  C07D211/48

    摘要： This invention relates to organic compounds of formula I, in which Ar1 is unsubstituted phenyl substituted by one or more halogen atoms; Ar2 is unsubstituted phenyl or phenyl substituted by one or more substituents selected from the group consisting of halogen, cyano and C1-C8-alkoxy; R1 is hydrogen or methyl optionally substituted by hydroxy; R10 is hydrogen or hydroxy; and pharmaceutically acceptable salts thereof. Compositions containing them, methods for their preparation and their use as pharmaceuticals are also described.

    摘要翻译： 本发明涉及式I的有机化合物，其中Ar 1是被一个或多个卤素原子取代的未取代的苯基; Ar 2是未取代的苯基或被一个或多个选自以下的取代基取代的苯基：卤素，氰基和C 1 -C 8 - 烷氧基 R 1是氢或任选被羟基取代的甲基; R 10是氢或羟基; 及其药学上可接受的盐。 还描述了含有它们的组合物，其制备方法及其作为药物的用途。

    8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors
    17.
    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。

    N-(4-aryloxypiperidin-1-ylalkyl) cinnamic amides as CCR33 receptor antagonists
    18.
    发明授权
    N-(4-aryloxypiperidin-1-ylalkyl) cinnamic amides as CCR33 receptor antagonists 失效

    公开(公告)号：US07034042B2

    公开(公告)日：2006-04-25

    申请号：US10398533

    申请日：2001-10-08

    申请人： Gurdip Bhalay ,  Trevor J Howe ,  Darren M Le Grand

    发明人： Gurdip Bhalay ,  Trevor J Howe ,  Darren M Le Grand

    IPC分类号： A61K31/445 ,  C07D211/22

    CPC分类号： C07D211/46

    摘要： Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more substituents selected from halogen, cyano, nitro, and C1–C8-alkyl optionally substituted by cyano or halogen, Ar2 is phenyl optionally which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1–C8-alkyl, C1–C8-haloalkyl, C1–C8-alkoxy or C1–C8-alkoxycarbonyl, R1 is C1–C8-alkyl substituted by hydroxy, C1–C8-alkoxy, acyloxy, —N(R2)R3, halogen, carboxy, C1–C8-alkoxycarbonyl, phenyl-C1–C8-alkoxycarbonyl, —CON(R4)R5 or by a monovalent cyclic organic group, R2 and R?3 are each independently hydrogen or C1–C8-alkyl, or R2 is hydrogen and R3 is acyl or SO2R6, or R2 and R3 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen, C1–C8-alkyl optionally substituted by hydroxy or phenyl, or phenyl optionally substituted by C1–C8-alkyl, halogen, cyano or C1–C8-alkoxy, or R4 and R5 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R?6 is C1–C8-alkyl, C1–C8-haloalkyl, or phenyl optionally substituted by C1–C8-alkyl, and n is 1, 2, 3 or 4. The compounds are useful as pharmaceuticals.

    Pyrazine derivatives as enac blockers
    19.
    发明授权
    Pyrazine derivatives as enac blockers 有权
    吡嗪衍生物作为阻断剂

    公开(公告)号：US08372845B2

    公开(公告)日：2013-02-12

    申请号：US13232175

    申请日：2011-09-14

    申请人： Gurdip Bhalay ,  Lee Edwards ,  Catherine Howsham ,  Peter Hunt ,  Nichola Smith

    发明人： Gurdip Bhalay ,  Lee Edwards ,  Catherine Howsham ,  Peter Hunt ,  Nichola Smith

    IPC分类号： A61K31/497

    CPC分类号： C07D241/26 ,  C07D403/12 ,  C07D487/10

    摘要： Compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings as indicated in the specification, are useful for treating diseases mediated by blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

    摘要翻译： 式I化合物及其药学上可接受的盐和溶剂合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9和R10具有说明书中所示的含义，可用于治疗由 阻断上皮钠通道。 还描述了含有化合物的药物组合物和用于制备化合物的方法。