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    PYRIMIDINE DERIVATIVES
    1.
    发明申请
    PYRIMIDINE DERIVATIVES 审中-公开

    公开(公告)号：US20100267755A1

    公开(公告)日：2010-10-21

    申请号：US10477546

    申请日：2002-05-23

    申请人： Gianpaolo Bravi ,  Malcolm Clive Carter ,  Richard Howard Green ,  Jennifer Margaret Doughty ,  Charles David Hartley ,  Alan Naylor ,  Martin Pass ,  Jeremy John Payne ,  Neil Anthony Pegg

    发明人： Gianpaolo Bravi ,  Malcolm Clive Carter ,  Richard Howard Green ,  Jennifer Margaret Doughty ,  Charles David Hartley ,  Alan Naylor ,  Martin Pass ,  Jeremy John Payne ,  Neil Anthony Pegg

    IPC分类号： A61K31/505 ,  A61P29/00 ,  C07D239/42 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/506

    CPC分类号： C07D239/42 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

    摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable salts thereof, in which: R1 and R2 are independently 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(CR7R8)n and B(CR7R8)n; R3 is selected from the group consisting of C1-6alkyl, NH2 and R10CONH; R4 is C1-2alkyl substituted by one to five fluorine atoms; R5 is selected from the group consisting of H, C1-4alkyl, C1-2alkyl substituted with one to five fluorine atoms, halogen and C3-10cycloalkylC0-6alkyl, with the proviso that when R6 is H R5 is not H. R6 is selected from the group consisting of H, C1-4alkyl, C1-2alkyl substituted with one to five fluorine atoms, halogen, C1-4alkoxy, CN, NO2, C1-6alkylOCO, NH2CO, C1-6alkylNHCO, NH2, C1-6alkylNH, (C1-6alkyl)2N, (C1-6alkyl)2NCO, C1-6alkylCONH, NH2SO2, C1-6alkylNHSO2, (C1-6alkyl)2NSO2, C1-6alkylSO2NH, ArSO2NH, C1-6alkylSO2, ArSO2, C3-10cycloalkylC0-6alkyl, C3-6alkenyl and C3-6alkynyl, with the proviso that when R5 is H R6 is not H. R7 and R8 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 R9; R9 is selected from the group consisting of hydroxy, 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; R10 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; B is selected from the group consisting of defines the point of attachment of the ring; 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 pain, fever and inflammation of a variety of conditions and diseases.

    Pyrimidine derivatives as selective inhibitors of COX-2
    3.
    发明授权
    Pyrimidine derivatives as selective inhibitors of COX-2 失效
    嘧啶衍生物作为COX-2的选择性抑制剂

    公开(公告)号：US06780870B2

    公开(公告)日：2004-08-24

    申请号：US10182788

    申请日：2002-07-31

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

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

    IPC分类号： C07D23942

    CPC分类号： C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    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, or C1-6alkyl; R3 is C1-6alkyl or NH2; R4 is H or C1-6alkyl; A is a 5- or 6-membered aryl, or a 5- or 6-membered aryl substituted by one or more R5; R5 is halogen, C1-6alkyl, C1-6alkyl substituted by one ore more F, C1-6alkoxy, C1-6alkoxy substituted by one or more F, SO2NH2 or SO2C1-6alkyl; and n is 1 to 4.

    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或C 1-6烷基; R 3是C 1-6烷基或NH 2; R 4是H或C 1-6烷基; A是5或6元芳基或被一个或多个R 5取代的5或6元芳基; R 5是卤素，C 1 -C 6烷基， 被一个或多个F，C 1-6烷氧基，被一个或多个F，SO 2 NH 2或SO 2 C 1-6烷基取代的C 1-6烷氧基取代的C 1-6烷基; andn是1到4。

    Pyrimidine derivatives useful as selective COX-2 inhibitors
    4.
    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
    5.
    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
    6.
    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。

    Heterocyclic compounds and methods for their use
    10.
    发明申请
    Heterocyclic compounds and methods for their use 有权
    杂环化合物及其使用方法

    公开(公告)号：US20150218180A1

    公开(公告)日：2015-08-06

    申请号：US14373357

    申请日：2013-01-25

    申请人： Thomas David McCarthy ,  Alan Naylor ,  Spinifex Pharmaceuticals Pty Ltd

    发明人： Thomas David McCarthy ,  Alan Naylor

    IPC分类号： C07D491/056 ,  C07D211/60 ,  C07D401/04 ,  C07D471/04

    CPC分类号： C07D491/056 ,  C07D211/60 ,  C07D401/04 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04

    摘要： The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to piperidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.

    摘要翻译： 本发明涉及可用于拮抗血管紧张素II型2型（AT2）受体的杂环化合物。 更具体地，本发明涉及哌啶化合物，含有它们的组合物及其在治疗或预防与AT2受体功能相关的病症或疾病的方法中的用途，包括神经性疼痛，炎性疼痛，与神经元超敏反应相关的病症，神经传导速度受损，细胞增殖紊乱 ，与骨吸收和骨形成之间的不平衡相关的疾病以及与异常神经再生相关的疾病。