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    Indolizine Derivatives as Ligands of the Crth2 Receptor
    2.
    发明申请
    Indolizine Derivatives as Ligands of the Crth2 Receptor 审中-公开
    吲哚啉衍生物作为Crth2受体的配体

    公开(公告)号：US20080306109A1

    公开(公告)日：2008-12-11

    申请号：US12065963

    申请日：2006-09-14

    申请人： George Hynd ,  Nicholas Charles Ray ,  Harry Finch ,  John Gary Montana ,  Michael Colin Cramp ,  Trevor Keith Harrison ,  Rosa Arienzo ,  Paul Blaney ,  Yann Griffon ,  David Middlemiss

    发明人： George Hynd ,  Nicholas Charles Ray ,  Harry Finch ,  John Gary Montana ,  Michael Colin Cramp ,  Trevor Keith Harrison ,  Rosa Arienzo ,  Paul Blaney ,  Yann Griffon ,  David Middlemiss

    IPC分类号： A61K31/44 ,  C07D455/02 ,  A61P43/00

    CPC分类号： C07D471/04

    摘要： Compounds of formula (I) are CRTH2 antagonists, useful in the treatment of, for example, asthma, chronic obstructive pulmonary disease, rhinitis, allergic airway syndrome, and allergic rhinobronchitis. Formula (I) wherein R1, R2. R3 and R4 each independently are hydrogen, C1-C6alkyl, fully or partially fluorinated C1-C6alkyl, halo, —S(O)nR10, —SO2N(R10)2, —N(R10)2, —C(O)N(R10)2, —NR10C(O)R9, —CO2R10, —C(O)R9, —NO2, —CN or —OR11; wherein each R9 is independently C1-C6alkyl, aryl, heteroaryl; R10 is independently hydrogen, C1-C6alkyl, aryl, or heteroaryl; R11 is hydrogen, C1-C6alkyl, fully or partially fluorinated C1-C6alkyl or a group —SO2R10; n is 0, 1 or 2; R5 is C1-C6alkyl, fully or partially fluorinated C1-C6alkyl, C1-C6alkenyl, C1-C6alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R6 is hydrogen, C1-C6alkyl or fully or partially fluorinated C1-C6alkyl; R7 and R8 are independently hydrogen or C1-C6alkyl, or R7 and R8 together with the atom to which they are attached form a cycloalkyl group; and X is —CHR6—, —S(O)n—, —C(O)—, —NR6SO2— or —SO2NR6- wherein n is 0, 1 or 2.

    摘要翻译： 式（I）化合物是CRTH2拮抗剂，可用于治疗例如哮喘，慢性阻塞性肺病，鼻炎，过敏性气道综合征和过敏性鼻炎支原体炎。 式（I）其中R1，R2。 完全或部分氟化的C 1 -C 6烷基，卤素，-S（O）n R 10，-SO 2 N（R 10）2，-N（R 10）2，-C（O）N（ R 10）2，-NR 10 C（O）R 9，-CO 2 R 10，-C（O）R 9，-NO 2，-CN或-OR 11; 其中每个R 9独立地是C 1 -C 6烷基，芳基，杂芳基; R 10独立地是氢，C 1 -C 6烷基，芳基或杂芳基; R 11是氢，C 1 -C 6烷基，完全或部分氟化的C 1 -C 6烷基或基团-SO 2 R 10; n为0,1或2; R 5是C 1 -C 6烷基，完全或部分氟化的C 1 -C 6烷基，C 1 -C 6烯基，C 1 -C 6炔基，任选取代的芳基或任选取代的杂芳基; R6是氢，C1-C6烷基或完全或部分氟化的C1-C6烷基; R 7和R 8独立地是氢或C 1 -C 6烷基，或者R 7和R 8与它们所连接的原子一起形成环烷基; 且X为-CHR 6 - ， - S（O）n - ， - C（O） - ， - NR 6 SO 2 - 或-SO 2 NR 6 - ，其中n为0,1或2。

    Quinolines and Their Therapeutic Use
    4.
    发明申请
    Quinolines and Their Therapeutic Use 有权
    喹啉及其治疗用途

    公开(公告)号：US20090156600A1

    公开(公告)日：2009-06-18

    申请号：US12066603

    申请日：2006-09-29

    申请人： Michael Colin Cramp ,  Rosa Arienzo ,  George Hynd ,  Peter Crackett ,  Yann Griffon ,  Trevor Keith Harrison ,  Nicholas Charles Ray ,  Harry Finch ,  John Gary Montana

    发明人： Michael Colin Cramp ,  Rosa Arienzo ,  George Hynd ,  Peter Crackett ,  Yann Griffon ,  Trevor Keith Harrison ,  Nicholas Charles Ray ,  Harry Finch ,  John Gary Montana

    IPC分类号： A61K31/5377 ,  C07D215/233 ,  A61P11/06 ,  C07D413/14 ,  A61K31/47

    CPC分类号： C07D215/233 ,  A61K31/47 ,  C07D215/12 ,  C07D215/18 ,  C07D215/20 ,  C07D215/227 ,  C07D215/36 ,  C07D215/48 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12

    摘要： Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component; in which: R1, R2, R3, R4 and R5 are independently hydrogen, C1-C6alkyl, C1-C6-fluoroalkyl, cyclopropyl, halo, —S(O)nR6, —SO2NR7R8, —NR7R8, —NR7C(O)R6, —CO2R7, —C(O)NR7R8, —C(O)R76, —NO2, —CN or a group —OR9; wherein each R6 is independently C1-C6alkyl, C1-C6-fluoroalkyl, cycloalkyl, aryl, or heteroaryl; R7, R8 are independently C1-C6alkyl, C1-C6-fluoroalkyl, cycloalkyl, cycloalkyl-(C1-C6alkyl)-, aryl, heteroaryl or hydrogen; R9 is hydrogen, C1-C6alkyl, C1-C6-fluoroalkyl, cycloalkyl, cylcoalkyl-(C1-C6alkyl)-, or a group —SO2R6; A is —CHR10—, —C(O)—, —S(O)n—, —O—, or —NR10— wherein n is an integer from 0-2 and R10 is hydrogen C1-C3alkyl, or C1-C6-fluoroalkyl group; B is a direct bond, or a divalent radical selected from —CH2—, —CH2CH2—, —CHR11—, —CR11R12—, —CH2CHR11—, CH2CR11R12—, —CHR11CHR12—, and divalent radicals of formula —(CR11R12)p-Z- wherein Z is attached to the ring carrying R1, R2 and R3; wherein R11 is C1-C3alkyl, cyclopropyl, C1-C6-fluoroalkyl; R12 is methyl or fluoromethyl; p is independently 1 or 2; and Z is —O—, —NH—, or —S(O)n—, wherein n is an integer from 0-2; X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, or sulfonic acid group, or a group of formula C(═O)NHSO2R6 or SO2NHC(═O)R6; and Y is aryl, heteroaryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group.

    摘要翻译： 式[1]化合物是CRTH2拮抗剂，可用于治疗具有炎性成分的病症; 其中：R1，R2，R3，R4和R5独立地是氢，C1-C6烷基，C1-C6-氟烷基，环丙基，卤素，-S（O）nR6，-SO2NR7R8，-NR7R8，-NR7C（O） -C（O）NR 7 R 8，-C（O）R 76，-NO 2，-CN或-OR 9基团; 其中每个R 6独立地为C 1 -C 6烷基，C 1 -C 6 - 氟烷基，环烷基，芳基或杂芳基; R 7，R 8独立地是C 1 -C 6烷基，C 1 -C 6氟代烷基，环烷基，环烷基 - （C 1 -C 6烷基） - ，芳基，杂芳基或氢; R 9是氢，C 1 -C 6烷基，C 1 -C 6 - 氟代烷基，环烷基，环烷基 - （C 1 -C 6烷基） - 或-SO 2 R 6基团; A是-CHR 10 - ， - C（O） - ， - S（O）n - ， - O-或-NR 10 - ，其中n是0-2的整数，R 10是氢C1-C3烷基或C1-C6 氟烷基 或选自-CH 2 - ， - CH 2 CH 2 - ， - CHR 11 - ， - CR 11 R 12 - ， - CH 2 CHR 11 - ，CH 2 CR 11 R 12 - ， - CHR 11 CHR 12 - - 的二价基团和式 - （CR11R12）pZ- 其中Z连接到携带R1，R2和R3的环上; 其中R11是C1-C3烷基，环丙基，C1-C6-氟代烷基; R12是甲基或氟甲基; p独立地为1或2; 和Z是-O - ， - NH-或-S（O）n - ，其中n是0-2的整数; X是羧酸，四唑，3-羟基异恶唑，异羟肟酸，次膦酸盐，膦酸盐，膦酰胺或磺酸基，或式C（-O）NHSO 2 R 6或SO 2 NHC（-O）R 6的基团; 并且Y是芳基，杂芳基，芳基稠合 - 杂环烷基，杂芳基 - 稠合 - 环烷基，杂芳基 - 稠合 - 杂环烷基或芳基稠合 - 环烷基。

    Quinolines and Their Therapeutic Use
    6.
    发明申请
    Quinolines and Their Therapeutic Use 有权
    喹啉及其治疗用途

    公开(公告)号：US20100144787A1

    公开(公告)日：2010-06-10

    申请号：US12531935

    申请日：2008-04-03

    申请人： John Gary Montana ,  Harry Finch ,  George Hynd ,  Michael Colin Cramp ,  Rosa Arienzo ,  Neville McLean

    发明人： John Gary Montana ,  Harry Finch ,  George Hynd ,  Michael Colin Cramp ,  Rosa Arienzo ,  Neville McLean

    IPC分类号： A61K31/4709 ,  C07D215/233 ,  C07D215/227 ,  C07D215/12 ,  A61P11/06 ,  A61P11/08 ,  A61P11/16 ,  A61P11/02

    CPC分类号： C07D401/10 ,  C07D215/227 ,  C07D215/233 ,  C07D413/10 ,  C07D417/10

    摘要： Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R1 is halogen or cyano; R2 is hydrogen or methyl; R3 and R4 are independently —OR6, C1-C6alkyl or C3-C6cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R5 is hydrogen or halogen; R6 is C1C6 alkyl or C3-C6 cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is —CH2—, —S—, or —O—; one of Y and Y1 is hydrogen and the other is OR6, —C(═O)R7, NR8SO2R6 or a heterocyclic group selected from those referred to in the specification; and R6, R7 and R8 are as defined in the specification.

    摘要翻译： 式（I）化合物是可用于治疗例如哮喘和COPD的CRTH2配体，其中：R1是卤素或氰基; R2是氢或甲基; R 3和R 4独立地为-OR 6，C 1 -C 6烷基或C 3 -C 6环烷基，后两个基团任选被一个或多个卤素原子取代; R5是氢或卤素; R6是C1C6烷基或C3-C6环烷基，其任一个任选被一个或多个卤素原子取代; X是-CH 2 - ， - S-或-O-; Y和Y1中的一个是氢，另一个是选自本说明书中提到的那些的OR 6，-C（= O）R 7，NR 8 SO 2 R 6或杂环基; R6，R7和R8如说明书中所定义。

    Quinolines and their therapeutic use
    8.
    发明授权
    Quinolines and their therapeutic use 有权
    喹啉及其治疗用途

    公开(公告)号：US08173812B2

    公开(公告)日：2012-05-08

    申请号：US12531935

    申请日：2008-04-03

    申请人： John Gary Montana ,  Harry Finch ,  George Hynd ,  Michael Colin Cramp ,  Rosa Arienzo ,  Neville McLean

    发明人： John Gary Montana ,  Harry Finch ,  George Hynd ,  Michael Colin Cramp ,  Rosa Arienzo ,  Neville McLean

    IPC分类号： C07D215/38 ,  A61K31/04

    CPC分类号： C07D401/10 ,  C07D215/227 ,  C07D215/233 ,  C07D413/10 ,  C07D417/10

    摘要： Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R1 is halogen or cyano; R2 is hydrogen or methyl; R3 and R4 are independently —OR6, C1-C6alkyl or C3-C6cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R5 is hydrogen or halogen; R6 is C1-C6 alkyl or C3-C6 cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is —CH2—, —S—, or —O—; one of Y and Y1 is hydrogen and the other is OR6, —C(═O)R7, NR8SO2R6 or a heterocyclic group selected from those referred to in the specification; and R6, R7 and R8 are as defined in the specification.

    摘要翻译： 式（I）化合物是可用于治疗例如哮喘和COPD的CRTH2配体，其中：R1是卤素或氰基; R2是氢或甲基; R 3和R 4独立地为-OR 6，C 1 -C 6烷基或C 3 -C 6环烷基，后两个基团任选被一个或多个卤素原子取代; R5是氢或卤素; R6是C1-C6烷基或C3-C6环烷基，其任一个任选被一个或多个卤素原子取代; X是-CH 2 - ， - S-或-O-; Y和Y1中的一个是氢，另一个是选自本说明书中提到的那些的OR 6，-C（= O）R 7，NR 8 SO 2 R 6或杂环基; R6，R7和R8如说明书中所定义。

    Quinolines and their therapeutic use
    9.
    发明授权
    Quinolines and their therapeutic use 有权
    喹啉及其治疗用途

    公开(公告)号：US08394830B2

    公开(公告)日：2013-03-12

    申请号：US13435242

    申请日：2012-03-30

    申请人： John Gary Montana ,  Harry Finch ,  George Hynd ,  Michael Colin Cramp ,  Rosa Arienzo ,  Neville McLean

    发明人： John Gary Montana ,  Harry Finch ,  George Hynd ,  Michael Colin Cramp ,  Rosa Arienzo ,  Neville McLean

    IPC分类号： A61K31/04

    CPC分类号： C07D401/10 ,  C07D215/227 ,  C07D215/233 ,  C07D413/10 ,  C07D417/10

    摘要： Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R1 is halogen or cyano; R2 is hydrogen or methyl; R3 and R4 are independently —OR6, C1-C6alkyl or C3-C6cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R5 is hydrogen or halogen; R6 is C1C6alkyl or C3-C6cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is —CH2—, —S—, or —O—; one of Y and Y1 is hydrogen and the other is OR6, —C(═O)R7, NR8SO2R6 or a heterocyclic group selected from those referred to in the specification; and R6, R7 and R8 are as defined in the specification.

    摘要翻译： 式（I）化合物是可用于治疗例如哮喘和COPD的CRTH2配体，其中：R1是卤素或氰基; R2是氢或甲基; R 3和R 4独立地为-OR 6，C 1 -C 6烷基或C 3 -C 6环烷基，后两个基团任选被一个或多个卤素原子取代; R5是氢或卤素; R6是C1C6烷基或C3-C6环烷基，其中任一个任选被一个或多个卤素原子取代; X是-CH 2 - ， - S-或-O-; Y和Y1中的一个是氢，另一个是选自本说明书中提到的那些的OR 6，-C（= O）R 7，NR 8 SO 2 R 6或杂环基; R6，R7和R8如说明书中所定义。

    Indoles and their therapeutic use
    10.
    发明授权
    Indoles and their therapeutic use 有权
    吲哚及其治疗用途

    公开(公告)号：US08394836B2

    公开(公告)日：2013-03-12

    申请号：US12746104

    申请日：2008-12-12

    申请人： George Hynd ,  John Gary Montana ,  Harry Finch ,  Rosa Arienzo ,  Barbara Avitabile-Woo ,  Mathias Domostoj

    发明人： George Hynd ,  John Gary Montana ,  Harry Finch ,  Rosa Arienzo ,  Barbara Avitabile-Woo ,  Mathias Domostoj

    IPC分类号： A61K31/4439 ,  C07D409/12 ,  C07D401/12

    CPC分类号： C07D209/12 ,  C07D209/04 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06 ,  C07D417/14

    摘要： Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. Wherein X is —SO2— or *—SO2NR3— wherein the bond marked with an asterisk is attached to Ar1; R1 is hydrogen, fluoro, chloro, CN or CF3; R2 is hydrogen, fluoro or chloro; R3 is hydrogen, C1C8alkyl or C3-C7cycloalkyl; Ar1 is phenyl or a 5- or 6-membered heteroaryl group selected from furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3-C7cycloalkyl, —O(C1-C4alkyl) or C1C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and Ar2 is phenyl or 5- or 6-membered heteroaryl group selected from pyrrolyl, furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3-C3-C7cycloalkyl, —O(C1-C4alkyl) or C1C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.

    摘要翻译： 式（I）的化合物是CRTH2受体的配体，特别用于治疗炎性病症。 其中X是-SO 2 - 或* -SO 2 NR 3 - ，其中用星号附着的键连接到Ar1上; R1是氢，氟，氯，CN或CF3; R2是氢，氟或氯; R3是氢，C1C8烷基或C3-C7环烷基; Ar 1是苯基或选自呋喃基，噻吩基，恶唑基，噻唑基，咪唑基，吡唑基，异恶唑基，异噻唑基，吡啶基，哒嗪基，嘧啶基和吡嗪基的5-或6-元杂芳基，其中苯基或杂芳基任选被一个 或更多个独立地选自氟，氯，CN，C 3 -C 7环烷基，-O（C 1 -C 4烷基）或C 1 -C 6烷基的取代基，后两个基团任选被一个或多个氟原子取代; 并且Ar 2是苯基或选自吡咯基，呋喃基，噻吩基，恶唑基，噻唑基，咪唑基，吡唑基，异恶唑基，异噻唑基，吡啶基，哒嗪基，嘧啶基和吡嗪基中的5-或6-元杂芳基，其中苯基或杂芳基任选被取代 通过一个或多个独立地选自氟，氯，CN，C 3 -C 3 -C 7环烷基，-O（C 1 -C 4烷基）或C 1 -C 6烷基的取代基，后两个基团任选被一个或多个氟原子取代。