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    Pharmaceutical compounds
    2.
    发明授权
    Pharmaceutical compounds 失效
    药物化合物

    公开(公告)号：US08779132B2

    公开(公告)日：2014-07-15

    申请号：US12445154

    申请日：2007-10-12

    申请人： Miles Stuart Congreve ,  Lynsey Helen Fazal ,  Martyn Frederickson ,  Christopher William Murray ,  Michael Alistair O'Brien ,  Andrew James Woodhead ,  John Francis Lyons ,  Neil Thomas Thompson

    发明人： Miles Stuart Congreve ,  Lynsey Helen Fazal ,  Martyn Frederickson ,  Christopher William Murray ,  Michael Alistair O'Brien ,  Andrew James Woodhead ,  John Francis Lyons ,  Neil Thomas Thompson

    IPC分类号： C07D403/06 ,  A61K31/497

    CPC分类号： C07D403/06 ,  C07D209/08 ,  C07D209/44 ,  C07D215/08 ,  C07D215/14 ,  C07D217/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D491/08 ,  C07D491/10 ,  C07D491/107 ,  C07D491/18

    摘要： The invention provides a compound for use in medicine, the compound being a compound of the formula (VI0) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R1 is hydrogen, hydroxy, or O—Rz; R2a is hydroxy, methoxy or O—Rz; provided that at least one of R1 and R2a is O—Rz; Rz is Lp-Rp1; SO3H; a glucuronide residue; a mono-, di- or tripeptide residue; or Lp is a bond, C═O, (C═O)O, (C═O)NRp1 or S(O)xNRp1; x is 1 or 2; Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C═O or (C═O)O; and provided also that O—Rz does not contain an O—O moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group Rp1; and R3, R4a, R8 and R10 are defined in the claims. The compounds of formula (VI0) are pro-drugs of parent compounds wherein R1 and/or R2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.

    摘要翻译： 本发明提供了一种用于医药的化合物，该化合物为式（VI0）化合物或其盐，溶剂化物，互变异构体或N-氧化物：其中双环基团：选自结构C1，C5和C6： 其中n为0,1,2或3; R1是氢，羟基或O-Rz; R2a是羟基，甲氧基或O-Rz; 条件是R1和R2a中的至少一个是O-Rz; Rz是Lp-Rp1; SO3H; 葡萄糖苷酸残基; 单，二或三肽残基; 或Lp为键，C = O，（C = O）O，（C = O）NRp1或S（O）xNRp1; x为1或2; Rp1是氢或任选取代的含有0,1或2个碳环和0,1,2,3,4,5或6个碳 - 碳多重键的C1〜25烃基，条件是当Lp为 一个键，C = O或（C = O）O; 并且还提供O-Rz不含有O-O部分; 并且不包括其中R 1是羟基并且R 2a是甲氧基的化合物; Rp2和Rp3相同或不同，并且各自为基团Rp1; R3，R4a，R8和R10如权利要求中所定义。 式（VI0）化合物是其中R 1和/或R 2a是羟基的母体化合物的前药，其中母体化合物具有Hsp90抑制活性。

    PHARMACEUTICAL COMBINATIONS COMPRISING PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS
    4.
    发明申请
    PHARMACEUTICAL COMBINATIONS COMPRISING PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 失效
    包含作为蛋白激酶调节剂的吡唑衍生物的药物组合

    公开(公告)号：US20100166699A1

    公开(公告)日：2010-07-01

    申请号：US11993823

    申请日：2006-06-21

    申请人： Neil Thomas Thompson ,  Robert George Boyle ,  Ian Collins ,  Michelle Dawn Garrett ,  John Francis Lyons ,  Kyla Merriom Thompson

    发明人： Neil Thomas Thompson ,  Robert George Boyle ,  Ian Collins ,  Michelle Dawn Garrett ,  John Francis Lyons ,  Kyla Merriom Thompson

    IPC分类号： A61K38/20 ,  A61K31/497 ,  A61K39/395 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/565 ,  A61K31/566 ,  A61K38/21 ,  A61K33/24 ,  A61K31/4375 ,  A61K31/675 ,  A61K31/551 ,  A61P35/00

    CPC分类号： A61K45/06 ,  A61K31/415 ,  A61K31/454 ,  A61K2300/00

    摘要： The invention provides a combination comprising an ancillary compound (e.g. one, two or more ancillary compounds) and a compound of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are patient packs, pharmaceutical kits and packs and compositions containing the combinations, methods for preparing the combinations and their use in combination therapy as anticancer agents.

    摘要翻译： 本发明提供包含辅助化合物（例如一种，两种或多种辅助化合物）和具有​​蛋白激酶B抑制活性的式（I）化合物的组合的组合：其中A是含有1至7个碳原子的饱和烃连接基团 ，连接基团具有在R1和NR2R3之间延伸的5个原子的最大链长度，以及在E和NR 2 R 3之间延伸的4个原子的最大链长度，其中连接基团中的一个碳原子可以任选被氧或氮取代 原子; 并且其中连接基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是当存在的羟基不相对于NR 2 R 3基团位于碳原子a时， 存在时的氧代基相对于NR 2 R 3基团位于碳原子a; E是单环或双环碳环或杂环基; R是芳基或杂芳基; 并且R 2，R 3，R 4和R 5如权利要求中所定义。 还提供了包含组合的患者包装，药物盒和包装和组合，用于制备组合的方法及其在联合治疗中作为抗癌剂的用途。

    Pharmaceutical combinations
    5.
    发明授权
    Pharmaceutical combinations 有权
    药物组合

    公开(公告)号：US08277807B2

    公开(公告)日：2012-10-02

    申请号：US12445141

    申请日：2007-10-12

    申请人： Neil James Gallagher ,  John Francis Lyons ,  Neil Thomas Thompson ,  Stephen Murray Yule ,  Christopher William Murray

    发明人： Neil James Gallagher ,  John Francis Lyons ,  Neil Thomas Thompson ,  Stephen Murray Yule ,  Christopher William Murray

    IPC分类号： A61K31/404 ,  A61K31/4035 ,  A61K31/47 ,  A61K31/472 ,  A61K31/438 ,  A61K31/5377 ,  A61K39/395 ,  A61K31/4745

    CPC分类号： A61K45/06 ,  A61K31/403 ,  A61K31/4035 ,  A61K2300/00

    摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The combinations have activity as Hsp90 inhibitors.

    摘要翻译： 本发明提供包含（或基本上由）一种或多种辅助化合物和式（I）化合物或其盐，互变异构体，溶剂合物和N-氧化物的组合; 其中R1是羟基或氢; R2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任选取代的C 1-5烃氧基; R4选自氢; 其中n为0或1，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 卤素; 氰基; 羟基; 氨基; 和任选取代的单或二-C 1-5烃基 - 氨基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; 并且NR 5 R 6形成具有8至12个环成员的任选取代的双环杂环基，其中多达5个环成员是选自氧，氮和硫的杂原子。 这些组合具有作为Hsp90抑制剂的活性。

    PHARMACEUTICAL COMBINATIONS
    6.
    发明申请
    PHARMACEUTICAL COMBINATIONS 有权
    药物组合

    公开(公告)号：US20110105501A1

    公开(公告)日：2011-05-05

    申请号：US12445136

    申请日：2007-10-12

    申请人： Neil James Gallagher ,  John Francis Lyons ,  Neil Thomas Thompson ,  Stephen Murray Yule ,  Christopher William Murray

    发明人： Neil James Gallagher ,  John Francis Lyons ,  Neil Thomas Thompson ,  Stephen Murray Yule ,  Christopher William Murray

    IPC分类号： A61K31/4035 ,  A61K31/438 ,  A61K31/5377 ,  A61K31/496 ,  A61P31/12 ,  A61P35/00

    CPC分类号： C07D401/14 ,  A61K31/403 ,  A61K31/438 ,  A61K31/439 ,  A61K31/496 ,  A61K31/5375 ,  C07D209/08 ,  C07D209/44 ,  C07D215/08 ,  C07D401/04 ,  C07D471/04 ,  C07D471/10 ,  C07D491/08 ,  C07D491/10 ,  A61K2300/00

    摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The combinations have activity as Hsp90 and/or glycogen synthase kinase-3 and/or cyclin dependent kinase and/or aurora kinase inhibitors.

    摘要翻译： 本发明提供包含（或基本上由）一种或多种辅助化合物和式（I）化合物或其盐，互变异构体，溶剂合物和N-氧化物的组合; 其中R1是羟基或氢; R2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任选取代的C 1-5烃氧基; R4选自氢; 其中n为0或1，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 卤素; 氰基; 羟基; 氨基; 和任选取代的单或二-C 1-5烃基 - 氨基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; 并且NR 5 R 6形成具有8至12个环成员的任选取代的双环杂环基，其中多达5个环成员是选自氧，氮和硫的杂原子。 这些组合具有作为Hsp90和/或糖原合酶激酶-3和/或细胞周期蛋白依赖性激酶和/或极光激酶抑制剂的活性。

    PHARMACEUTICAL COMBINATIONS
    7.
    发明申请
    PHARMACEUTICAL COMBINATIONS 有权
    药物组合

    公开(公告)号：US20100092474A1

    公开(公告)日：2010-04-15

    申请号：US12445141

    申请日：2007-10-12

    申请人： Neil James Gallagher ,  John Francis Lyons ,  Neil Thomas Thompson ,  Stephen Murray Yule ,  Christopher William Murray

    发明人： Neil James Gallagher ,  John Francis Lyons ,  Neil Thomas Thompson ,  Stephen Murray Yule ,  Christopher William Murray

    IPC分类号： A61K31/404 ,  A61K31/4035 ,  A61K31/47 ,  A61K31/472 ,  A61K31/438 ,  A61K31/437 ,  A61K31/5377 ,  A61K39/395 ,  A61K31/4745 ,  A61P35/00

    CPC分类号： A61K45/06 ,  A61K31/403 ,  A61K31/4035 ,  A61K2300/00

    摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The combinations have activity as Hsp90 inhibitors.

    摘要翻译： 本发明提供包含（或基本上由）一种或多种辅助化合物和式（I）化合物或其盐，互变异构体，溶剂合物和N-氧化物的组合; 其中R1是羟基或氢; R2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任选取代的C 1-5烃氧基; R4选自氢; 其中n为0或1，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 卤素; 氰基; 羟基; 氨基; 和任选取代的单或二-C 1-5烃基 - 氨基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; 并且NR 5 R 6形成具有8至12个环成员的任选取代的双环杂环基，其中多达5个环成员是选自氧，氮和硫的杂原子。 这些组合具有作为Hsp90抑制剂的活性。

    PHARMACEUTICAL COMPOUNDS
    8.
    发明申请
    PHARMACEUTICAL COMPOUNDS 有权
    药物化合物

    公开(公告)号：US20090298818A1

    公开(公告)日：2009-12-03

    申请号：US12445163

    申请日：2007-10-12

    申请人： John Francis Lyons ,  Neil Thomas Thompson

    发明人： John Francis Lyons ,  Neil Thomas Thompson

    IPC分类号： A61K31/536 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/44 ,  A61K31/40

    CPC分类号： A61K31/4035 ,  A61K31/437 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  Y02A50/411 ,  A61K2300/00

    摘要： The invention provides the use of a compound for the manufacture of a medicament for the treatment of pain, wherein the compound is a compound of the formula (VI): or a salt, solvate, tautomer or N-oxide thereof; wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n, R1, R2a, R3, R4a, R8 and R10 are as defined in the claims.The invention also provides the use of a compound of the formula (VI) for the manufacture of a medicament for the prophylaxis or treatment of a fungal, protozoal, viral or parasitic disease state or condition (other than a disease state or condition due to Plasmodium falciparum) or for use in the prophylaxis or treatment of Ewing's sarcoma, atherosclerosis or lupus erythematosus.

    摘要翻译： 本发明提供化合物在制备用于治疗疼痛的药物中的用途，其中所述化合物是式（Ⅵ）化合物或其盐，溶剂化物，互变异构体或N-氧化物; 其中双环基团：选自结构C1，C5和C6：其中n，R1，R2a，R3，R4a，R8和R10如权利要求中所定义。 本发明还提供式（VI）化合物在制备用于预防或治疗真菌，原生动物，病毒或寄生虫病状态（除了由于疟原虫引起的疾病状态或病症之外）的药物的用途 恶性疟原虫）或用于预防或治疗尤文氏肉瘤，动脉粥样硬化或红斑狼疮。

    Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators
    10.
    发明授权
    Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators 失效
    包含吡唑衍生物作为蛋白激酶调节剂的药物组合

    公开(公告)号：US08541461B2

    公开(公告)日：2013-09-24

    申请号：US11993823

    申请日：2006-06-21

    申请人： Neil Thomas Thompson ,  Robert George Boyle ,  Ian Collins ,  Michelle Dawn Garrett ,  John Francis Lyons ,  Kyla Merriom Thompson

    发明人： Neil Thomas Thompson ,  Robert George Boyle ,  Ian Collins ,  Michelle Dawn Garrett ,  John Francis Lyons ,  Kyla Merriom Thompson

    IPC分类号： A61K31/415

    CPC分类号： A61K45/06 ,  A61K31/415 ,  A61K31/454 ,  A61K2300/00

    摘要： The invention provides a combination comprising an ancillary compound (e.g. one, two or more ancillary compounds) and a compound of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are patient packs, pharmaceutical kits and packs and compositions containing the combinations, methods for preparing the combinations and their use in combination therapy as anticancer agents.

    摘要翻译： 本发明提供包含辅助化合物（例如一种，两种或多种辅助化合物）和具有​​蛋白激酶B抑制活性的式（I）化合物的组合的组合：其中A是含有1至7个碳原子的饱和烃连接基团 ，连接基团具有在R1和NR2R3之间延伸的5个原子的最大链长度，以及在E和NR 2 R 3之间延伸的4个原子的最大链长度，其中连接基团中的一个碳原子可以任选被氧或氮取代 原子; 并且其中连接基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是当存在的羟基不相对于NR 2 R 3基团位于碳原子α时，条件是 存在时的氧代基位于相对于NR 2 R 3基团的碳原子α; E是单环或双环碳环或杂环基; R1是芳基或杂芳基; 并且R 2，R 3，R 4和R 5如权利要求中所定义。 还提供了包含组合的患者包装，药物盒和包装和组合，用于制备组合的方法及其在联合治疗中作为抗癌剂的用途。