PHTHALAZINONE DERIVATIVES
    4.
    发明申请
    PHTHALAZINONE DERIVATIVES 失效
    邻苯二酚衍生物

    公开(公告)号:US20090069303A1

    公开(公告)日:2009-03-12

    申请号:US12271308

    申请日:2008-11-14

    摘要: A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i) where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and (ii) where Q is O or S; RD is: wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C═O; RN2 is selected from H and optionally substituted C1-10 alkyl; RC3 and RC4 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRC1RC2. RC1 and RC2 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring; and when X is a single bond RN1 and RC2 may together with the N and C atoms to which they are bound, form an optionally substituted C5-7 heterocylic ring; and when X is CRC3RC4, RC2 and RC4 may together form an additional bond, such that there is a double bond between the atoms substituted by RC1 and RC3.

    摘要翻译: 式(I)的化合物:其中:A和B一起表示任选取代的稠合芳环; D选自:(i)其中Y1选自CH和N,Y2选自CH和N,Y3选自CH,CF和N; 和(ii)其中Q为O或S; RD是:其中RN1选自H和任选取代的C 1-10烷基; X选自单键NRN2,CRC3RC4和C-O; RN2选自H和任选取代的C 1-10烷基; RC3和RC4独立地选自H,R,C(-O)OR,其中R是任选取代的C 1-10烷基,任选取代的C 5-20芳基或任选取代的C 3-20杂环基; Y选自NRN3和CRC1RC2。 RC1和RC2独立地选自H,R,C(-O)OR,其中R是任选取代的C 1-10烷基,任选取代的C 5-20芳基或任选取代的C 3-20杂环基; RC1和RC2与它们所连接的碳原子一起可以形成任选取代的螺 - 稠合的C 5-7碳环或杂环; 当X是单键时,RN1和RC2可以与它们所结合的N和C原子一起形成任选被取代的C5-7杂环; 并且当X是CRC3RC4时,RC2和RC4可以一起形成附加键,使得在被RC1和RC3取代的原子之间存在双键。

    COMPOUNDS
    7.
    发明申请
    COMPOUNDS 审中-公开
    化合物

    公开(公告)号:US20100130473A1

    公开(公告)日:2010-05-27

    申请号:US11817134

    申请日:2006-02-24

    摘要: Compounds of formula (I): A-B—C and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of formula (i) where RN is H or Me; or B is a divalent C5 heterocyclic residue containing one or two ring heteroatoms; A is formula (ii) RA3 and RA5 are independently selected from halo, ORO and RAC, where RO is H or Me, and RAC is H or C1-4 alkyl; XA is selected from N and CRA4, where RA4 is selected from H, ORO, CH2OH, CO2H, NHSO2Me and NHCOMe; RA2 and RA6 are independently selected from H, halo and ORO; or RA3 and RA4 together with the carbon atoms to which they are attached, or RA2 and RA3 together with the carbon atoms to which they are attached, may form a C5-6 heterocylic or heteroaromatic ring, containing at least one nitrogen ring atom; where if X is not N, 1, 2, or 3 of RA2 to RA6 are not H; C is formula (iii) where X is selected from N and CH, Y is selected from N and CH, and Z is selected from N and CRC6; RC3 is selected from H, halo and an optionally substituted N-containing C5-7 heterocyclic group; RC5 is a group selected from formula (iv) which group may be selected by one or two C1-4 alkyl groups or a carboxy group; RC6 is H; or, when X and Y are N, RC5 and RC6 (when Z is CRC6) together with the carbon atoms to which they are attached may form a fused C6 aromatic ring selected from the group consisting of formula (v).

    摘要翻译: 式(I)化合物:A-B-C及其异构体,盐,溶剂合物,化学保护形式及其前药。其中:B选自式(ⅰ),其中RN为H或Me; 或B是含有一个或两个环杂原子的二价C5杂环残基; A是式(ⅱ)RA 3和RA 5独立地选自卤素,ORO和RAC,其中RO是H或Me,RAC是H或C 1-4烷基; XA选自N和CRA4,其中RA4选自H,ORO,CH2OH,CO2H,NHSO2Me和NHCOMe; RA2和RA6独立地选自H,卤素和ORO; 或RA3和RA4与它们所连接的碳原子一起,或RA2和RA3与它们所连接的碳原子一起可以形成含有至少一个氮环原子的C 5-6杂环或杂芳环; 其中如果X不是RA,RA6的N,1,2或3不是H; C是式(ⅲ),其中X选自N和CH,Y选自N和CH,Z选自N和CRC 6; RC3选自H,卤素和任选取代的含N的C 5-7杂环基; RC5是选自式(iv)的基团,该基团可以被一个或两个C 1-4烷基或羧基选择; RC6为H; 或者当X和Y为N时,RC5和RC6(当Z为CRC6时)与它们所连接的碳原子一起形成选自式(v)的稠合C 6芳环。

    Phthalazinone derivatives
    10.
    发明授权
    Phthalazinone derivatives 失效
    酞嗪衍生物

    公开(公告)号:US07470688B2

    公开(公告)日:2008-12-30

    申请号:US11550004

    申请日:2006-10-17

    摘要: A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i) where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and (ii) where Q is O or S; RD is: wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C═O; RN2 is selected from H and optionally substituted C1-10 alkyl; RC3 and RC4 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRC1RC2; RC1 and RC2 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring; and when X is a single bond RN1 and RC2 may together with the N and C atoms to which they are bound, form an optionally substituted C5-7 heterocyclic ring; and when X is CRC3RC4, RC2 and RC4 may together form an additional bond, such that there is a double bond between the atoms substituted by RC1 and RC3.

    摘要翻译: 式(I)的化合物:其中:A和B一起表示任选取代的稠合芳环; D选自:(i)其中Y1选自CH和N,Y2选自CH和N,Y3选自CH,CF和N; 和(ii)其中Q为O或S; RD是:其中RN1选自H和任选取代的C 1-10烷基; X选自单键NRN2,CRC3RC4和C-O; RN2选自H和任选取代的C 1-10烷基; RC3和RC4独立地选自H,R,C(-O)OR,其中R是任选取代的C 1-10烷基,任选取代的C 5-20芳基或任选取代的C 3-20杂环基; Y选自NRN3和CRC1RC2; RC1和RC2独立地选自H,R,C(-O)OR,其中R是任选取代的C 1-10烷基,任选取代的C 5-20芳基或任选取代的C 3-20杂环基; RC1和RC2与它们所连接的碳原子一起可以形成任选取代的螺 - 稠合的C 5-7碳环或杂环; 当X是单键时,RN1和RC2可以与它们所结合的N和C原子一起形成任选取代的C 5-7杂环; 并且当X是CRC3RC4时,RC2和RC4可以一起形成附加键,使得在被RC1和RC3取代的原子之间存在双键。