Triazolopyridine derivatives and their therapeutic use
    1.
    发明授权
    Triazolopyridine derivatives and their therapeutic use 失效
    三唑并吡啶衍生物及其治疗用途

    公开(公告)号:US08557797B2

    公开(公告)日:2013-10-15

    申请号:US13201716

    申请日:2010-02-16

    CPC classification number: C07D471/04

    Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of inter alia, diseases of the respiratory tract wherein; R1 is C1-C6 alkyl, C3-C6 cycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and R3 and R4 are independently H or C1-C6 alkyl, or R3 and R4 taken together with the nitrogen to which they are attached form a 6-membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is —O— or —S(O)p— wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C3-C6 divalent cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to R2NHC(═O)W—; W is a bond, —NH— or —C(RA)(RB), wherein RA and RB are independently H, methyl, ethyl, amino, hydroxyl or halo; and R2 is a radical as defined in the claims.

    Abstract translation: 式(I)化合物是p38MAP激酶的抑制剂,其可用作治疗特别是呼吸道疾病的抗炎剂,其中: R 1是C 1 -C 6烷基,C 3 -C 6环烷基,任选取代的苯基,任选被取代的5-或6-元单环杂芳基,或其中n是1或2的式(II)基团,R 3和R 4是 独立地是H或C 1 -C 6烷基,或者R 3和R 4与它们所连接的氮一起形成任选含有另外选自N和O的杂原子的6元杂环; Y是-O-或-S(O)p - ,其中p是0,1或2; A是任选取代的二价亚芳基或单环或双环亚杂芳基或具有5或6个环原子的C 3 -C 6二价亚环烷基或哌啶子基,其中环氮连接至R 2 NHC(= O)W - ; W是键,-NH-或-C(RA)(RB),其中RA和RB独立地是H,甲基,乙基,氨基,羟基或卤素; 并且R 2是如权利要求中所定义的基团。

    TRIAZOLOPYRIDINE DERIVATIVES AND THEIR THERAPEUTIC USE
    3.
    发明申请
    TRIAZOLOPYRIDINE DERIVATIVES AND THEIR THERAPEUTIC USE 失效
    三唑吡啶衍生物及其治疗用途

    公开(公告)号:US20120088763A1

    公开(公告)日:2012-04-12

    申请号:US13201716

    申请日:2010-02-16

    CPC classification number: C07D471/04

    Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of inter alia, diseases of the respiratory tract wherein; R1 is C1-C6 alkyl, C3-C6 cycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and R3 and R4 are independently H or C1-C6 alkyl, or R3 and R4 taken together with the nitrogen to which they are attached form a 6-membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is —O— or —S(O)p— wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C3-C6 divalent cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to R2NHC(═O)W—; W is a bond, —NH— or —C(RA)(RB), wherein RA and RB are independently H, methyl, ethyl, amino, hydroxyl or halo; and R2 is a radical as defined in the claims.

    Abstract translation: 式(I)化合物是p38MAP激酶的抑制剂,其可用作治疗特别是呼吸道疾病的抗炎剂,其中: R 1是C 1 -C 6烷基,C 3 -C 6环烷基,任选取代的苯基,任选被取代的5-或6-元单环杂芳基,或其中n是1或2的式(II)基团,R 3和R 4是 独立地是H或C 1 -C 6烷基,或者R 3和R 4与它们所连接的氮一起形成任选含有另外选自N和O的杂原子的6元杂环; Y是-O-或-S(O)p - ,其中p是0,1或2; A是任选取代的二价亚芳基,或单环或双环亚杂芳基或具有5或6个环原子的C 3 -C 6二价亚环烷基或哌啶子基,其中环氮连接至R 2 NHC(= O)W - ; W是键,-NH-或-C(RA)(RB),其中RA和RB独立地是H,甲基,乙基,氨基,羟基或卤素; 并且R 2是如权利要求中所定义的基团。

    Urea derivatives and their therapeutic use in the treatment of, inter alia, diseases of the respiratory tract
    4.
    发明授权
    Urea derivatives and their therapeutic use in the treatment of, inter alia, diseases of the respiratory tract 有权
    尿素衍生物及其治疗用途,特别是治疗呼吸道疾病

    公开(公告)号:US08916708B2

    公开(公告)日:2014-12-23

    申请号:US13701989

    申请日:2011-06-09

    CPC classification number: C07D471/04 C07D401/12

    Abstract: Compounds of formula (I) are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory wherein R1 is a radical of formula (IA) or (IB) or (IC): 10 Y is —O— or —S(O)p—wherein p is 0, 1 or 2; A is an optionally substituted cycloalkylene radical having 5, 6 or 7 ring atoms fused to a phenyl ring; and R2, R3b and R4b are as defined in the claims.

    Abstract translation: 式(I)化合物是p38MAPK抑制剂,其用作治疗特别是呼吸道疾病的抗炎剂,其中R1是式(IA)或(IB)或(IC)的基团:10Y 是-O-或-S(O)p - ,其中p是0,1或2; A是与苯环稠合的具有5,6或7个环原子的任选取代的亚环烷基; R2,R3b和R4b如权利要求中所定义。

    UREA DERIVATIVES AND THEIR THERAPEUTIC USE IN THE TREATMENT OF, INTER ALIA, DISEASES OF THE RESPIRATORY TRACT
    5.
    发明申请
    UREA DERIVATIVES AND THEIR THERAPEUTIC USE IN THE TREATMENT OF, INTER ALIA, DISEASES OF THE RESPIRATORY TRACT 有权
    尿素衍生物及其治疗,治疗,联合治疗呼吸道感染的治疗方法

    公开(公告)号:US20130143914A1

    公开(公告)日:2013-06-06

    申请号:US13701989

    申请日:2011-06-09

    CPC classification number: C07D471/04 C07D401/12

    Abstract: Compounds of formula (I) are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory wherein R1 is a radical of formula (IA) or (IB) or (IC): 10 Y is -0- or —S(0)p- wherein p is 0, 1 or 2; A is an optionally substituted cycloalkylene radical having 5, 6 or 7 ring atoms fused to a phenyl ring; and R2, R3b and R4b are as defined in the claims.

    Abstract translation: 式(I)化合物是p38MAPK抑制剂,其用作治疗特别是呼吸道疾病的抗炎剂,其中R1是式(IA)或(IB)或(IC)的基团:10Y 是-O-或-S(O)p - ,其中p是0,1或2; A是与苯环稠合的具有5,6或7个环原子的任选取代的亚环烷基; R2,R3b和R4b如权利要求中所定义。

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