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    INDAZOLES AS GLUCOCORTICOID RECEPTOR LIGANDS
    1.
    发明申请
    INDAZOLES AS GLUCOCORTICOID RECEPTOR LIGANDS 有权
    INDAZOLES作为GLUCOCORTICOID受体配体

    公开(公告)号：US20090074675A1

    公开(公告)日：2009-03-19

    申请号：US11910935

    申请日：2006-04-12

    Applicant: Colin David Eldred ,  David House ,  Graham George Adam Inglis ,  Simon John Fawcett MacDonald ,  Philip Alan Skone

    Inventor： Colin David Eldred ,  David House ,  Graham George Adam Inglis ,  Simon John Fawcett MacDonald ,  Philip Alan Skone

    IPC: A61K9/12 ,  C07D401/04 ,  A61K31/4439

    CPC classification number: C07D405/14 ,  C07D231/56 ,  C07D401/04 ,  C07D405/12

    Abstract: A compound of formula (I): wherein A1 represents 2,3-dihydro-1-benzofuran-7-yl, 5-fluoro-2-methoxy-phenyl or 5-fluoro-2-hydroxy-phenyl; X represents —C(R3)— or nitrogen; when X represents —C(R3)—, R2 represents hydrogen and R1 represents fluorine, R3 represents hydrogen or fluorine, when X represents —C(R3)— and R2 and R1 each represent hydrogen, R3 represents hydrogen, hydroxy, methoxy or fluorine, when X represents —C(R3)— and R2 represents hydroxy, methoxy, —CO2CH3 or —CO2CH2CH3, R1 and R3 each represent hydrogen, when X represents nitrogen, R1 and R2 each represent hydrogen; and Y represents H or methyl; or a physiologically functional derivative thereof.

    Abstract translation: 式（I）的化合物：其中A1表示2,3-二氢-1-苯并呋喃-7-基，5-氟-2-甲氧基 - 苯基或5-氟-2-羟基 - 苯基; X表示-C（R 3） - 或氮; 当X表示-C（R3） - 时，R2表示氢，R1表示氟，R3表示氢或氟，当X表示-C（R3） - 且R2和R1各自表示氢时，R3表示氢，羟基，甲氧基或氟 当X表示-C（R 3） - 且R 2表示羟基，甲氧基，-CO 2 CH 3或-CO 2 CH 2 CH 3时，R 1和R 3各自表示氢，当X表示氮时，R 1和R 2各自表示氢; Y表示H或甲基; 或其生理功能衍生物。

    1,7-Naphthyridines as Pde4 Inhibitors
    4.
    发明申请
    1,7-Naphthyridines as Pde4 Inhibitors 审中-公开
    1,7-萘乙酸作为Pde4抑制剂

    公开(公告)号：US20080146563A1

    公开(公告)日：2008-06-19

    申请号：US11908188

    申请日：2006-03-16

    Applicant: Colin David Eldred ,  John Edward Robinson

    Inventor： Colin David Eldred ,  John Edward Robinson

    IPC: A61K31/5377 ,  C07D221/04 ,  A61K31/4375 ,  A61K31/496 ,  A61P37/08 ,  A61P29/00 ,  C07D295/00

    CPC classification number: C07D471/04

    Abstract: There are provided according to the invention novel compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein R1 is selected from the group consisting of C1-4alkyl, C4-6cycloalkyl(CH2)m—, methoxyC2-4alkyl, HOCH2CH2—, R3(O)2S(CH2)2—, R5R4NCO(CH2)n—, and heterocyclyl(CH2)m— wherein any nitrogen heteroatom of the heterocyclyl radical may be unsubstituted or substituted by methyl; R2 is hydrogen or methyl; R3 is methyl or NH2; R4-5 independently represent methyl, m is 0, 1 or 2; and n is 1 or 2; or R1 and R2 together with the nitrogen atom to which they are attached may form a heterocyclyl ring, which may be unsubstituted or substituted by one or two substituents selected from the group consisting of; methyl, ═O and (CH3)2N—.

    Abstract translation: 根据本发明提供新的式（I）化合物及其药学上可接受的盐和溶剂合物：其中R 1选自C 1-4烷基， 烷基，C 4-6环烷基（CH 2 CH 2）m - ，甲氧基C 2-4烷基， （O）2 S 2（CH 2）2 - - - - （CH 2） R 2，R 5，R 5，R 5，N 2，N 2， 和杂环基（CH 2 CH 2）m - ，其中杂环基的任何氮杂原子可以是未取代的或被甲基取代; R 2是氢或甲基; R 3是甲基或NH 2; R 4-5独立地表示甲基，m是0,1或2; n为1或2; 或R 1和R 2与它们所连接的氮原子一起可以形成杂环基环，其可以是未取代的或被一个或两个选自以下的取代基取代： 组成; 甲基，-O和（CH 3）2 N - 。

    Chemical Compounds
    6.
    发明授权
    Chemical Compounds 失效
    化学化合物

    公开(公告)号：US06455510B1

    公开(公告)日：2002-09-24

    申请号：US09530573

    申请日：2000-06-15

    Applicant: Richard Peter Charles ,  Brian Cox ,  Colin David Eldred ,  Andrew Michael Kenneth Pennell

    Inventor： Richard Peter Charles ,  Brian Cox ,  Colin David Eldred ,  Andrew Michael Kenneth Pennell

    IPC: A61K3170

    CPC classification number: C07H19/16

    Abstract: A compound of formula (I) which is an agonist at the adenosine A1 receptor wherein R2 represents C1-3alkyl, halogen or hydrogen; R3 represents a fluorinated straight or branched alkyl group of 1-6 carbon atoms and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists at the adenosine A1 receptor.

    Abstract translation: 式（I）化合物，其为腺苷A1受体的激动剂，其中R2表示C1-3烷基，卤素或氢; R3表示1-6个碳原子的氟化直链或支链烷基及其盐和溶剂化物，特别是其生理上可接受的溶剂合物及其盐。 这些化合物是腺苷A1受体的激动剂。

    Indazoles as glucocorticoid receptor ligands
    8.
    发明授权
    Indazoles as glucocorticoid receptor ligands 有权
    吲哚类作为糖皮质激素受体配体

    公开(公告)号：US08093281B2

    公开(公告)日：2012-01-10

    申请号：US11910935

    申请日：2006-04-12

    Applicant: Colin David Eldred ,  David House ,  Graham George Adam Inglis ,  Simon John Fawcett MacDonald ,  Philip Alan Skone

    Inventor： Colin David Eldred ,  David House ,  Graham George Adam Inglis ,  Simon John Fawcett MacDonald ,  Philip Alan Skone

    IPC: A61K31/416 ,  C07D231/56

    CPC classification number: C07D405/14 ,  C07D231/56 ,  C07D401/04 ,  C07D405/12

    Abstract: A compound of formula (I): wherein A1 represents 2,3-dihydro-1-benzofuran-7-yl, 5-fluoro-2-methoxy-phenyl or 5-fluoro-2-hydroxy-phenyl; X represents —C(R3)— or nitrogen; when X represents —C(R3)—, R2 represents hydrogen and R1 represents fluorine, R3 represents hydrogen or fluorine, when X represents —C(R3)— and R2 and R1 each represent hydrogen, R3 represents hydrogen, hydroxy, methoxy or fluorine, when X represents —C(R3)— and R2 represents hydroxy, methoxy, —CO2CH3 or —CO2CH2CH3, R1 and R3 each represent hydrogen, when X represents nitrogen, R1 and R2 each represent hydrogen; and Y represents H or methyl; or a physiologically functional derivative thereof.

    Abstract translation: 式（I）的化合物：其中A1表示2,3-二氢-1-苯并呋喃-7-基，5-氟-2-甲氧基 - 苯基或5-氟-2-羟基 - 苯基; X表示-C（R 3） - 或氮; 当X表示-C（R3） - 时，R2表示氢，R1表示氟，R3表示氢或氟，当X表示-C（R3） - 且R2和R1各自表示氢时，R3表示氢，羟基，甲氧基或氟 当X表示-C（R 3） - 且R 2表示羟基，甲氧基，-CO 2 CH 3或-CO 2 CH 2 CH 3时，R 1和R 3各自表示氢，当X表示氮时，R 1和R 2各自表示氢; Y表示H或甲基; 或其生理功能衍生物。

    1,7-Naphthyridines
    9.
    发明申请
    1,7-Naphthyridines 审中-公开
    1,7-萘啶

    公开(公告)号：US20090270444A1

    公开(公告)日：2009-10-29

    申请号：US11718892

    申请日：2005-11-17

    Applicant: Colin David Eldred ,  John Edward Robinson ,  Alison Judith Steel

    Inventor： Colin David Eldred ,  John Edward Robinson ,  Alison Judith Steel

    IPC: A61K31/4375 ,  C07D471/04 ,  A61P37/08

    CPC classification number: C07D471/04

    Abstract: There are provided according to the invention novel compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein: R1 is phenyl which may be unsubstituted or substituted by one or two substituents selected from fluorine, chlorine, C1-2alkoxy-, —CN; phenyl fused to a 5-membered saturated ring containing one oxygen atom; pyridinyl which may be unsubstituted or substituted by one or two substituents selected from fluorine or chlorine; or C-linked pyrazolyl which may be unsubstituted or substituted by the substituent C1-2alkyl; R2 is C1-4alkyl; R3 is C1-2alkyl; and n is 0, 1 or 2.

    Abstract translation: 根据本发明，提供新的式（I）化合物及其药学上可接受的盐和溶剂化物，其中：R1是可以是未取代的或被一个或两个选自氟，氯，C 1-2烷氧基 - ， - CN; 与含有一个氧原子的5元饱和环稠合的苯基; 吡啶基，其可以是未取代的或被一个或两个选自氟或氯的取代基取代; 或C连接的吡唑基，其可以是未取代的或被取代基C 1-2烷基取代; R2是C1-4烷基; R3是C1-2烷基; n为0,1或2。

    Chemical compounds
    10.
    发明授权
    Chemical compounds 失效
    化合物

    公开(公告)号：US06740644B2

    公开(公告)日：2004-05-25

    申请号：US10373064

    申请日：2003-02-26

    Applicant: Colin David Eldred ,  Andrew Michael Kenneth Pennell

    Inventor： Colin David Eldred ,  Andrew Michael Kenneth Pennell

    IPC: A61K3170

    CPC classification number: C07H19/16 ,  Y02P20/55

    Abstract: A compound of formula (I), wherein R2 represents C1-3alkyl, halogen or hydrogen; R3 represents straight or branched alkyl group of 1-6 carbon atoms; with the proviso that, when R3 represents C1-3alkyl, R2 represents C1-3alkyl, R1 cannot represent phenyl optionally substituted by one or more substituents selected from halogen, C1-3alkyl, trifluoromethyl, nitro, cyano, —CO2Rc, —CONRcRd, —CORc, —SORe, —SO2Re, —SO3H, —SO2NRcRd, —ORc, —NHSO2Re, —NHCORc and —NRcRd; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists at the Adenosine A1 receptor.

    Abstract translation: 式（I）的化合物，其中R 2表示C 1-3烷基，卤素或氢; R 3表示1-6个碳原子的直链或支链烷基; 条件是当R 3表示C 1-3烷基时，R 2表示C 1-3烷基，R 1不能表示任选被一个或多个选自卤素，C 1-3烷基，三氟甲基，硝基， 氰基，-CO 2 R c，-CONR c R d，-COR c，-SOR e，-SO 2 R e，-SO 3 H，-SO 2 NR c R d， OR c，-NHSO 2 R e，-NHCOR c和-NR c R d; 特别是其生理上可接受的溶剂合物及其盐。 这些化合物是腺苷A1受体的激动剂。

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