公开(公告)号：US20070185172A1

公开(公告)日：2007-08-09

申请号：US11571894

申请日：2005-07-13

Applicant: David Sandham ,  Christopher Sharp ,  Simon Watson

Inventor： David Sandham ,  Christopher Sharp ,  Simon Watson

IPC: A61K31/41

CPC classification number: C07J1/00

Abstract: Compounds of formula I in free or salt form, wherein R1 and R2 have the meanings as indicated in the specification, are useful for treating inflammatory conditions, particularly inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract translation: 具有游离或盐形式的式I化合物，其中R 1和R 2 2具有说明书中所示的含义，可用于治疗炎性疾病，特别是炎性或阻塞性 气道疾病 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。

公开(公告)号：US20050054660A1

公开(公告)日：2005-03-10

申请号：US10937639

申请日：2004-09-09

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

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

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

CPC classification number: C07D239/545 ,  A61K31/522 ,  C07D473/04 ,  C07D473/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20070066607A1

公开(公告)日：2007-03-22

申请号：US10552023

申请日：2004-04-02

Applicant: Robin Fairhurst ,  David Sandham ,  David Beattie ,  Ian Bruce ,  Bernard Cuenoud ,  Reamonn Madden ,  Neil Taylor ,  Roger Taylor ,  Katharine Turner ,  Simon Watson

Inventor： Robin Fairhurst ,  David Sandham ,  David Beattie ,  Ian Bruce ,  Bernard Cuenoud ,  Reamonn Madden ,  Neil Taylor ,  Roger Taylor ,  Katharine Turner ,  Simon Watson

IPC: A61K31/541 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/496 ,  A61K31/4709 ,  C07D265/36 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

CPC classification number: C07D215/227 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds of formula I free or salt form, wherein —C—Y—, R1 and R2 are G have the meanings 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.

Abstract translation: 式I的游离或盐形式的化合物，其中-CY-，R 1和R 2是G具有说明书中指出的含义，可用于治疗 通过β2 - 肾上腺素受体的激活而被预防或缓解。 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。

公开(公告)号：US20060106214A1

公开(公告)日：2006-05-18

申请号：US11329889

申请日：2006-01-11

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

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

IPC: A61K31/522 ,  C07D473/04

CPC classification number: C07D239/545 ,  A61K31/522 ,  C07D473/04 ,  C07D473/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20060173181A1

公开(公告)日：2006-08-03

申请号：US11274030

申请日：2005-11-15

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

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

IPC: C07D473/04 ,  A61K31/522

CPC classification number: C07D239/545 ,  A61K31/522 ,  C07D473/04 ,  C07D473/06

Abstract: 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.

Abstract translation: 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。