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    PYRIMIDINE DERIVATIVES
    3.
    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.

    17β-carbothioate 17α-arylcarbonyloxyloxy androstane derivative as anti-inflammatory agents
    4.
    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。

    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：US07074802B2

    公开(公告)日：2006-07-11

    申请号：US10477819

    申请日：2002-05-23

    申请人： Jennifer Doughty, legal representative ,  Charles David Hartley ,  Alan Naylor ,  Jeremy John Payne ,  Neil Anthony Pegg

    发明人： Richard Howard Doughty, deceased

    IPC分类号： C07D239/42 ,  A61K31/505

    CPC分类号： C07D239/42

    摘要： The invention thus 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, C2-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl and C4-12bridged cycloalkyl; R3 is selected from the group consisting of C1-6alkyl, NH2 and R5CONH; R4 is selected from the group consisting of CH2F, CHF2, CF3CH2, CF3CHF and CF3CF2; and R5 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. 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： 因此，本发明提供式（I）化合物及其药学上可接受的盐，其中：R 1和R 2独立地选自H，C C 1-6烷基，C 2-6链烯基，C 3-6亚炔基，C 3-10环烷基C 0-6个烷基和C 4-12-12桥连环烷基; R 3选自C 1-6烷基，NH 2和R 5 CONH; R 4选自CH 2，CH 2，CH 3，CH 3，CH 3，CH 3， 2，CF 3 CHF和CF 3 3 CF 2; 和R 5选自H，C 1-6烷基，C 1-6烷氧基，C 1 C 1-6烷基，C 1-6烷基，苯基，HO 2 C 1-6烷基，C 1-6 C 1-6烷基，C 1-6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 烷基，C 1-6烷基，C 1-6烷基和C 1-6烷基CONHC 1-6烷基。 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。

    Pyrimidine derivatives useful as selective COX-2 inhibitors
    6.
    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
    7.
    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。

    Anti-inflammatory androstane derivatives
    8.
    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。

    Novel Anti-Inflammatory Androstane Derivatives
    10.
    发明申请
    Novel Anti-Inflammatory Androstane Derivatives 审中-公开
    新型抗炎安慰剂衍生物

    公开(公告)号：US20080317833A1

    公开(公告)日：2008-12-25

    申请号：US12199991

    申请日：2008-08-28

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

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

    IPC分类号： A61K31/56 ,  A61K9/70 ,  A61K9/127 ,  A61K9/12 ,  A61K9/14 ,  A61K9/20

    CPC分类号： C07J31/006

    摘要： There are provided according to the invention pharmaceutical compositions 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, wherein said heteroaryl is a 5 member heterocyclic aromatic ring containing 1-3 hetero atoms selected from N and S, or a 5 member heterocyclic aromatic ring containing 2-3 hetero atoms selected from N, O and S, or a 6 member heterocyclic aromatic ring containing 1-3 hetero atoms selected from N, O and S; 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; or a physiologically acceptably salt or solvate thereof; and another therapeutically active agent; in admixture with one or more physiologically acceptable diluents or carriers.

    摘要翻译： 根据本发明提供药物组合物，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，其中所述杂芳基是含有1-3个选自N和S的杂原子的5元杂环芳族环或含有 2-3个选自N，O和S的杂原子，或含有1-3个选自N，O和S的杂原子的6元杂环芳环; 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; ＆lt; img id =“CUSTOM-CHARACTER-00001”he =“3.13mm”wi =“11.60mm”file =“US20080317833A1-20081225-P00001.TIF”img-content =“character”img-format =“tif”/ >表示单键或双键; 或其生理上可接受的盐或溶剂合物; 和另一种治疗活性剂; 与一种或多种生理上可接受的稀释剂或载体混合。