Indolizineacetic Acids and Their Therapeutic Use as Ligands of the CRTH2 Receptor
    1.
    发明申请
    Indolizineacetic Acids and Their Therapeutic Use as Ligands of the CRTH2 Receptor 审中-公开
    吲哚嗪乙酸及其作为CRTH2受体配体的治疗用途

    公开(公告)号:US20100093751A1

    公开(公告)日:2010-04-15

    申请号:US12520004

    申请日:2007-12-13

    CPC分类号: C07D471/04

    摘要: Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, inter alia, respiratory diseases: wherein R1 is fluoro, chloro, cyano or trifluoromethyl; R2 is hydrogen, fluoro or chloro; R3 is hydrogen, fluoro, chloro or trifluoromethyl; X is —CH2—, —S—, —S(═O)— or —S(═O)2—; one of Y and Y1 is hydrogen and the other is —C(═O)R4, or —S(═O)2R4, or —CR5R6OR7 or a heterocyclic group selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,5-oxadiazolyl, furazanyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,3-thiadiazolyl, 1,2,5-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,4-thiadiazolyl, tetrazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, 1,2,4-triazinyl and 1,3,5-triazinyl any of which may be optionally substituted; R4 is an optionally substituted cyclic amino group having 5, 6 or 7 ring atoms which is linked to the carbonyl or sulfonyl through a ring nitrogen; R5 and R6 are independently hydrogen, (C1C3)alkyl, cyclopropyl, or R5 and R6 taken together with the carbon atom to which they are attached form a 3-6 membered cycloalkyl ring; and R7 is optionally substituted (C1-C6)alkyl or (C3-C6)cycloalkyl,

    摘要翻译: 式(I)化合物是CRTH2配体,可用于治疗呼吸系统疾病,其中R1是氟,氯,氰基或三氟甲基; R2是氢,氟或氯; R3是氢,氟,氯或三氟甲基; X是-CH 2 - , - S - , - S(= O) - 或-S(= O)2 - ; Y和Y1之一是氢,另一个是-C(= O)R 4或-S(= O)2 R 4或-CR 5 R 6 OR 7或选自呋喃基,噻吩基,吡咯基,恶唑基,噻唑基,咪唑基,吡唑基 ,异恶唑基,异噻唑基,1,2,3-恶二唑基,1,2,4-恶二唑基,1,3,4-恶二唑基,1,2,5-恶二唑基,呋咱基,1,2,3-三唑基,1,2 ,4-三唑基,1,2,3-噻二唑基,1,2,5-噻二唑基,1,3,4-噻二唑基,1,2,4-噻二唑基,四唑基,吡啶基,哒嗪基,嘧啶基,吡嗪基,1,2 ,4-三嗪基和1,3,5-三嗪基,其中任何一个可以是任选取代的; R4是具有5,6或7个环原子的任选取代的环状氨基,其通过环氮连接到羰基或磺酰基; R5和R6独立地为氢,(C1C3)烷基,环丙基或R5和R6与它们所连接的碳原子一起形成3-6元环烷基环; 并且R 7是任选取代的(C 1 -C 6)烷基或(C 3 -C 6)环烷基,

    Quinolines and Their Therapeutic Use
    9.
    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

    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。