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    1,2,4-triazine-4-amine derivatives
    2.
    发明授权
    1,2,4-triazine-4-amine derivatives 有权
    1,2,4-三嗪-4-胺衍生物

    公开(公告)号：US08809525B2

    公开(公告)日：2014-08-19

    申请号：US13576798

    申请日：2011-02-07

    申请人： Miles Stuart Congreve ,  Stephen Philippe Andrews ,  Jonathan Stephen Mason ,  Christine Mary Richardson ,  Giles Albert Brown

    发明人： Miles Stuart Congreve ,  Stephen Philippe Andrews ,  Jonathan Stephen Mason ,  Christine Mary Richardson ,  Giles Albert Brown

    IPC分类号： C07D401/04 ,  C07D401/14 ,  A61K31/444 ,  A61P25/16 ,  C07D417/12 ,  C07D405/04 ,  C07D413/04 ,  C07D405/10 ,  C07D487/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D253/07

    CPC分类号： C07D401/04 ,  A61K31/4427 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/5386 ,  C07D253/07 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04

    摘要： According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cy2 group is optionally substituted by one or more R4c substituents; HetB represents a 3- to 10-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one or two rings and which HetB group is optionally substituted by one or more R4d substituents.

    摘要翻译： 根据本发明，提供式A1化合物，其可用于治疗通过抑制A1-A2b或特别是A2a受体而改善的病症或障碍，其中式A1化合物具有结构， 其中，A表示Cy1或HetA; Cy1表示5至14元芳族，完全饱和或部分不饱和的碳环系统，其包含一个，两个或三个环，该Cy1基团任选被一个或多个R 4a取代基取代; HetA表示5至14元杂环基，其可以是芳族的，完全饱和的或部分不饱和的，并且其含有一个或多个选自O，S和N的杂原子，该杂环基可以包含一个，两个或三个环， HetA基团任选被一个或多个R 4b取代基取代; B代表Cy2或HetB; Cy2表示包含一个或两个环的3-至10-元芳族，完全饱和或部分不饱和的碳环系，该Cy2基团任选被一个或多个R 4c取代基取代; HetB表示可以是芳族的，完全饱和的或部分不饱和的并且含有一个或多个选自O，S和N的杂原子的3-至10-元杂环基，该杂环基可以包含一个或两个环，并且HetB基团 任选地被一个或多个R 4d取代基取代。

    Pharmaceutical compounds
    4.
    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。

    Naphthalene derivatives
    9.
    发明授权
    Naphthalene derivatives 失效
    萘衍生物

    公开(公告)号：US07732622B2

    公开(公告)日：2010-06-08

    申请号：US12111989

    申请日：2008-04-30

    申请人： Miles Stuart Congreve ,  Gerard Martin Paul Giblin ,  Andrew McMurtrie Mason ,  Neil Derek Miller ,  Susan Roomans ,  Ann Louise Walker

    发明人： Miles Stuart Congreve ,  Gerard Martin Paul Giblin ,  Andrew McMurtrie Mason ,  Neil Derek Miller ,  Susan Roomans ,  Ann Louise Walker

    IPC分类号： C07D209/60 ,  A61K31/40

    CPC分类号： C07D209/66 ,  C07D209/64

    摘要： A compound of formula (I) wherein R1 and R3 are the same or different and represent ═O, hydrogen, C1-6alkyl, C1-6dialkyl, ═CHC1-C5alkyl, ═S, or a 5- or 6-membered aryl; R4 to R9 are the same or different and represent hydrogen, C1-6alkoxy, OCF3, OCH2CF3, O-cyclopropyl, OCH2-cyclopropyl, C1-C6alkyl, S-alkyl, NR210 where R10 is hydrogen or C1-6alkyl, halogen, NO2, OH, CH2OC1-C6alkyl, CH2OH, or CF3; Q1 is hydrogen, C1-6alkyl, C1-6dialkyl, C1-6alkoxy, NHAc, NR210 where R10 is hydrogen or C1-6alkyl, difluoro, fluoro, ═O, or OH; Q2, Q3, Q4 and Q5 are the same or different and represent hydrogen, C1-6alkoxy, OCF3, OCH2CF3, O-cyclopropyl, OCH2-cyclopropyl, C1-C6alkyl, S-alkyl, NR210 where R10 is hydrogen or C1-6alkyl, halogen, NO2, OH, CH2OC1-C6alkyl, CH2OH, or a 5- or 6-membered aryl; with the proviso that the compounds [4-(1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]-2-propionic acid, sodium salt and [4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetic acid are excluded; and pharmaceutically acceptable derivatives thereof.

    摘要翻译： 式（I）的化合物，其中R 1和R 3相同或不同并且表示≡O，氢，C 1-6烷基，C 1-6二烷基，= CHCl-C 5烷基，= S或5或6元芳基; R4至R9相同或不同，表示氢，C1-6烷氧基，OCF3，OCH2CF3，O-环丙基，OCH2-环丙基，C1-C6烷基，S-烷基，NR210，其中R10为氢或C1-6烷基，卤素， OH，CH 2 OC 1 -C 6烷基，CH 2 OH或CF 3; Q1是氢，C1-6烷基，C1-6二烷基，C1-6烷氧基，NHAc，NR210，其中R10是氢或C1-6烷基，二氟，氟，= O或OH; Q2，Q3，Q4和Q5相同或不同，表示氢，C1-6烷氧基，OCF3，OCH2CF3，O-环丙基，OCH2-环丙基，C1-C6烷基，S-烷基，NR210，其中R10是氢或C1-6烷基， 卤素，NO 2，OH，CH 2 OC 1 -C 6烷基，CH 2 OH或5或6元芳基; 条件是化合物[4-（1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基）苯基] -2-丙酸钠盐和[4-（4,9 - 二乙氧基-1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基）苯基]乙酸; 和它们的药用衍生物。