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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 useful as selective COX-2 inhibitors
    3.
    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
    4.
    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。

    Pyrimidine derivatives as selective inhibitors of COX-2
    5.
    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。

    17β-carbothioate 17α-arylcarbonyloxyloxy androstane derivative as anti-inflammatory agents
    7.
    发明授权
    17β-carbothioate 17α-arylcarbonyloxyloxy androstane derivative as anti-inflammatory agents 失效
    17β-硫代硫酸钠17α-芳基羰氧基氧基雄甾烷衍生物作为抗炎剂

    公开(公告)号：US07498321B2

    公开(公告)日：2009-03-03

    申请号：US10343842

    申请日：2001-08-03

    申请人： Keith Biggadike ,  Paul Jones ,  Jeremy John Payne

    发明人： Keith Biggadike ,  Paul Jones ,  Jeremy John Payne

    IPC分类号： A61K31/58 ,  C07J3/00 ,  C07J17/00 ,  C07J33/00 ,  C07J43/00

    CPC分类号： C07J31/006

    摘要： There are provided according to the invention compounds of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(═O)-aryl or —C(═O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the α or β configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and——represents a single or a double bond; and salts and solvates thereof. There are also provided processes for preparing compounds of formula (I) and use of the compounds in therapy especially in the treatment of inflammatory and allergic conditions.

    摘要翻译： 根据本发明提供式（I）化合物，其中R 1表示C 1-6烷基或C 1-6卤代烷基; R 2表示-C（ - ） - 芳基或-C（-O） - 杂芳基; R3表示氢，甲基（其可以是α或β构型）或亚甲基; R4和R5相同或不同，各自表示氢或卤素; 和 - 表示单键或双键; 及其盐和溶剂合物。 还提供了制备式（I）化合物的方法和该化合物在治疗中的用途，特别是用于治疗炎性和过敏性疾病。

    Anti-inflammatory androstane derivatives
    9.
    发明授权
    Anti-inflammatory androstane derivatives 有权
    抗炎雄甾烷衍生物

    公开(公告)号：US07405206B2

    公开(公告)日：2008-07-29

    申请号：US10492813

    申请日：2002-10-17

    申请人： Keith Biggadike ,  Paul Jones ,  Jeremy John Payne

    发明人： Keith Biggadike ,  Paul Jones ,  Jeremy John Payne

    IPC分类号： A61K31/58 ,  A61K31/585 ,  C07J17/00

    CPC分类号： C07J31/006 ,  C07J17/00

    摘要： There are provided compounds of formula (I) wherein R1 represents O, S or NH; R2 represents —C(═O)-aryl or —C(═O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the α or β configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and represents a single or a double bond; and salts and solvates thereof; process for preparing them, compositions containing them and their use in therapy.

    摘要翻译： 提供式（I）化合物，其中R 1代表O，S或NH; R 2表示-C（ - ） - 芳基或-C（-O） - 杂芳基; R 3表示氢，甲基（其可以是α或β构型）或亚甲基; R 4和R 5相同或不同，各自表示氢或卤素; “img id =”CUSTOM-CHARACTER-00001“he =”2.79mm“wi =”7.03mm“file =”US07405206-20080729-P00001.TIF“alt =”custom character“img-content =”character“img- format =“tif”/>表示单键或双键; 其盐和溶剂合物; 制备它们的方法，含有它们的组合物及其在治疗中的用途。

    Anti-inflammatory androstane derivatives
    10.
    发明授权
    Anti-inflammatory androstane derivatives 有权
    抗炎雄甾烷衍生物

    公开(公告)号：US06537983B1

    公开(公告)日：2003-03-25

    申请号：US10066961

    申请日：2002-02-04

    申请人： Keith Biggadike ,  Paul Spencer Jones ,  Jeremy John Payne

    发明人： Keith Biggadike ,  Paul Spencer Jones ,  Jeremy John Payne

    IPC分类号： A61K3158

    CPC分类号： A61K9/0075 ,  A61K9/008 ,  A61K31/18 ,  A61K31/573 ,  A61K31/58 ,  A61K45/06 ,  C07J17/00 ,  C07J31/00 ,  C07J33/002 ,  C07J43/003 ,  A61K2300/00

    摘要： According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(═O)-aryl or —C(═O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the &agr; or &bgr; configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and {overscore (-----)} represents a single or a double bond; and salts and solvates thereof together with a long-acting &bgr;2-adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of inflammatory disorders of the respiratory tract over a period of 24 hours or more.

    摘要翻译： 根据本发明的一个方面，提供了一种用于通过吸入给药的药物制剂，其包含式（I）化合物，其中R 1表示C 1-6烷基或C 1-6卤代烷基; R 2表示-C（= O） - 芳基或 -C（= O） - 杂芳基; R 3表示氢，甲基（其可以是α或β构型）或亚甲基; R 4和R 5相同或不同，各自表示氢或卤素; 和（过量的（-----表示单键或双键;以及其与长效β2-肾上腺素受体激动剂的盐和溶剂合物），该制剂在治疗呼吸道炎症性疾病中具有治疗上有用的作用 24小时以上。