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72 条记录 (耗时 0.046 秒)

    Pyrimidine derivatives as selective inhibitors of COX-2
    44.
    发明授权
    Pyrimidine derivatives as selective inhibitors of COX-2 失效

    公开(公告)号：US07056928B2

    公开(公告)日：2006-06-06

    申请号：US10486001

    申请日：2002-08-05

    申请人： Malcolm C Carter ,  Alan Naylor ,  Jeremy J Payne ,  Neil A Pegg

    发明人： Malcolm C Carter ,  Alan Naylor ,  Jeremy J Payne ,  Neil A Pegg

    IPC分类号： C07D239/42 ,  A61K31/505

    CPC分类号： C07D239/42

    摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable salts thereof, in which: R1 and R2 are independently selected from H, or C1-6alkyl; R3 is selected from the group consisting of C1-6alkyl, NH2 and R6CONH; R4 is H or C1-6alkyl; R5 is selected from the group consisting of CH2F, CHF2, CF3CH2, CF3CHF and CF3CF2; A is a 5- or 6-membered aryl, or a 5- or 6-membered aryl substituted by one or more R7; R6 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkyl, phenyl, HO2CC1-6alkyl, C1-6alkylOCOC1-6alkyl, C1-6alkylOCO, H2NC1-6alkyl, C1-6alkylOCONHC1-6alkyl and C1-6alkylCONHC1-6alkyl; R7 is selected from the group consisting of halogen, C1-6alkyl, C1-6alkyl substituted by one or more F, C1-6alkoxy, C1-6alkoxy substitued by one or more F, SO2NH2 or SO2C1-6alkyl; and n is 1 to 4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.

    Pyrimidine derivatives useful as selective COX-2 inhibitors
    45.
    发明授权
    Pyrimidine derivatives useful as selective COX-2 inhibitors 失效

    公开(公告)号：US07026327B2

    公开(公告)日：2006-04-11

    申请号：US10477547

    申请日：2002-05-23

    申请人： Alan Naylor ,  Jeremy John Payne ,  Neil Anthony Pegg

    发明人： Alan Naylor ,  Jeremy John Payne ,  Neil Anthony Pegg

    IPC分类号： C07D239/34 ,  C07D401/12 ,  A61K31/505

    CPC分类号： C07D239/34 ,  A61K31/505 ,  C07D401/12

    摘要： The invention provides the compounds of formula (I) in which: R1 is selected from the group consisting of H, C1-6alkyl, C1-2alkyl substituted by one to five fluorine atoms, C3-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl, C4-12bridged cycloalkyl, A(CR4R5)n and B(CR4R5)n; R2 is C1-2alkyl substituted by one to five fluorine atoms; R3 is selected from the group consisting of C1-6alkyl, NH2 and R7CONH; R4 and R5 are independently selected from H or C1-6alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by one or more R6; R6 is selected from the group consisting of halogen, C1-6alkyl, C1-6alkyl substituted by one more fluorine atoms, C1-6alkoxy, C1-6alkoxy substituted by one or more F, NH2SO2 and C1-6alkylSO2; B is selected from the group consisting of where defines the point of attachment of the ring; R7 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkyl, phenyl, HO2CC1-6alkyl, C1-6alkylOCOC1-6alkyl, C1-6alkylOCO, H2NC1-6alkyl, C1-6alkylOCONHC1-6alkyl and C1-6alkylCONHC1-6alkyl; and n is 0 to 4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of variety of conditions and diseases.

    Pyrimidine derivatives
    47.
    发明授权
    Pyrimidine derivatives 失效
    嘧啶衍生物

    公开(公告)号：US06780869B1

    公开(公告)日：2004-08-24

    申请号：US10130516

    申请日：2002-05-16

    申请人： Richard Howard Green ,  Charles David Hartley ,  Alan Naylor ,  Jeremy John Payne ,  Neil Anthony Pegg

    发明人： Richard Howard Green ,  Charles David Hartley ,  Alan Naylor ,  Jeremy John Payne ,  Neil Anthony Pegg

    IPC分类号： C07D23942

    CPC分类号： C07D239/42

    摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof, in which: R1 and R2 are independently selected from H, C1-6 alkyl, C2-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl or C4-12bridged cycloalkane; and R3 is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of pain, fever, inflammation and a variety of conditions and diseases.

    摘要翻译： 本发明提供式（I）化合物及其药学上可接受的衍生物，其中：R 1和R 2独立地选自H，C 1-6烷基，C 2-6烯基，C 3-6炔基，C 3-10环烷基C 0 C6烷基或C4-12桥连环烷烃; 和R 3是C 1-6烷基或NH 2。式（I）的化合物是COX-2的有效和选择性抑制剂，并且可用于治疗疼痛，发烧，炎症和多种病症和疾病。

    Pyrazolopyridines
    48.
    发明授权
    Pyrazolopyridines 失效
    吡唑并吡啶类

    公开(公告)号：US06498166B1

    公开(公告)日：2002-12-24

    申请号：US09890925

    申请日：2001-08-30

    申请人： Ian Baxter Campbell ,  Paul Francis Lambeth ,  Alan Naylor ,  Neil Anthony Pegg

    发明人： Ian Baxter Campbell ,  Paul Francis Lambeth ,  Alan Naylor ,  Neil Anthony Pegg

    IPC分类号： A61K31437

    CPC分类号： C07D471/04

    摘要： The invention provides the compounds of formula (I) wherein: R0 and R1 are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R2 is halogen, CN, CONR4R5, CO2H, CO2C1-6alkyl, or NHSO2R4; R3 is C1-6alkyl or NH2; and R4 and R5 are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups (selected from halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms), or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring; and pharmaceutically acceptable derivatives thereof. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.

    摘要翻译： 本发明提供式（I）化合物，其中：R 0和R 1独立地选自H，卤素，C 1-6烷基，C 1-6烷氧基或被一个或多个氟原子取代的C 1-6烷氧基; R 2是卤素，CN，CONR 4 R 5 ，CO 2 H，CO 2 C 1-6烷基或NHSO 2 R 4; R 3是C 1-6烷基或NH 2; R 4和R 5独立地选自H，C 1-6烷基，苯基，被一个或多个原子或基团取代的苯基（选自卤素，C 1-6烷基，C 1-6烷氧基或被一个或多个氟原子取代的C 1-6烷氧基）， 或与它们所连接的氮原子一起形成饱和的4至8元环; 其药学上可接受的衍生物。式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，多种病症和疾病的炎症。

    2,3-Diaryl-pyrazolo[1,5-b]pyridazines derivatives, their preparation and their use as cyclooxygenase 2(COX-2) inhibitors
    49.
    发明授权
    2,3-Diaryl-pyrazolo[1,5-b]pyridazines derivatives, their preparation and their use as cyclooxygenase 2(COX-2) inhibitors 失效
    2,3-二芳基 - 吡唑并[1,5-b]哒嗪衍生物，其制备及其作为环氧合酶2（COX-2）抑制剂的用途

    公开(公告)号：US06451794B1

    公开(公告)日：2002-09-17

    申请号：US09508029

    申请日：2000-06-13

    申请人： Paul John Beswick ,  Ian Baxter Campbell ,  Neil Mathews ,  Alan Naylor

    发明人： Paul John Beswick ,  Ian Baxter Campbell ,  Neil Mathews ,  Alan Naylor

    IPC分类号： A61K314985

    CPC分类号： C07D487/04 ,  A61K31/50 ,  Y02P20/55

    摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl, substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H, or C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.

    摘要翻译： 本发明提供式（I）化合物及其药学上可接受的衍生物，其中：R 0是卤素，C 1-6烷基，C 1-6烷氧基，被一个或多个氟原子取代的C 1-6烷氧基或O（CH 2）n NR 4 R 5; R 1和R 2独立地选自被一个或多个氟原子取代的H，C 1-6烷基，C 1-6烷基，C 1-6烷氧基，C 1-6羟烷基，SC 1-6烷基，C（O）H，C（O）C 1-6烷基 （C 1-6烷基磺酰基），被一个或多个氟原子取代的C 1-6烷氧基，O（CH 2）n CO 2 C 1-6烷基，O（CH 2）nSC 1-6烷基，（CH 2）n NR 4 R 5，（CH 2）nSC 1-6烷基或C（O）NR 4 R 5; 条件是当R 0在4-位且是卤素时，R 1和R 2中的至少一个是C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，O（CH 2）n CO 2 C 1-6烷基，O（CH 2） ）nSC1-6烷基，（CH2）nNR4R5或（CH2）nSC1-6烷基，C（O）NR4R5; R3是C1-6烷基或NH2; R 4和R 5独立地选自H或C 1-6烷基，或与它们所连接的氮原子一起形成4-8元饱和环; n为1-4。 式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，各种病症和疾病的炎症。