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    PURINE COMPOUNDS AS HSP90 PROTEIN INHIBITORS FOR THE TREATMENT OF CANCER
    2.
    发明公开
    PURINE COMPOUNDS AS HSP90 PROTEIN INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
    嘌呤化合物AS HSP90蛋白抑制剂用于癌症的治疗

    公开(公告)号：EP2004648A1

    公开(公告)日：2008-12-24

    申请号：EP06779505.4

    申请日：2006-09-20

    申请人： Vernalis (R&D) Limited ,  Cancer Research Technology Limited ,  The Institute of Cancer Research

    发明人： BROUGH, Paul ,  DRYSDALE, Martin ,  BARRIL-ALONSO, Xavier

    IPC分类号： C07D473/40 ,  C07D473/36 ,  C07D473/28 ,  A61K31/52 ,  A61P35/00

    CPC分类号： C07D473/40 ,  C07D473/30 ,  C07D473/36

    摘要： Compounds of formula (I) are inhibitors of HSP90, and of utility in the treatment of, for example, cancers: wherein ring A is an aryl or heteroaryl ring or ring system; R1 is hydrogen, fluoro, chloro, bromo, or a radical of formula (1A): -X-AIk1 -(Z)m-(Alk2)n-Q (IA) wherein X is a bond, -O-, -S- -S(O)-, -SO2-, or -NH-, Z is -O-, -S-, -(C=O)-, -(C=S)-, -S(O)-, -SO2-, -NRA-, or, in either orientation -C(=O)O-, -C(=O)NRA-, -C(=S)NRA-, -SO2NRA-, -NRAC(=O)-, or -NRASO2- wherein RA is hydrogen or C1-C6 alkyl in which one or more hydrogens is optionally substituted by fluorine; AIk1 and AIk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m and n are independently 0 or 1 , and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is cyano (-CN), fluoro, chloro, bromo, methyl, ethyl, -OH, -CH2OH, -C(=O)NH2, -C(=O)H, -C(=O)CH3, or -NH2; R3 and R4 are independently selected from hydrogen, fluoro, chloro, bromo, cyano (-CN), C1C3alkyl optionally substituted with one or more fluorine substituents, C1C3alkoxy optionally substituted with one or more fluorine substituents, -CH=CH2, -C=CH, cyclopropyl and -NH2, or R3 and R4 together represent a carbocyclic or heterocyclic ring fused to ring A, or methylenedioxy (-OCH2O-) or ethylenedioxy (-OCH2CH2O-) in either of which one or more hydrogens are optionally replaced by fluorine; Si is hydrogen, or a substituent as defined in the specification.

    Fused heterocyclic compounds, their production and use
    6.
    发明公开
    Fused heterocyclic compounds, their production and use 失效
    熔融杂环化合物，它们的生产和使用

    公开(公告)号：EP0518033A1

    公开(公告)日：1992-12-16

    申请号：EP92106621.3

    申请日：1992-04-16

    申请人： TAKEDA CHEMICAL INDUSTRIES, LTD.

    发明人： Naka, Takehiko ,  Inada, Yoshiyuki

    IPC分类号： C07D471/04 ,  C07D495/04 ,  C07D487/04 ,  C07D403/14 ,  C07D405/14 ,  C07D403/10 ,  C07D473/28 ,  C07D401/06 ,  A61K31/435 ,  A61K31/505 ,  A61K31/41

    CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D471/04 ,  C07D473/30 ,  C07D487/04 ,  C07D495/04

    摘要： Fused heterocyclic compounds of the formula (I):

    wherein R¹ is an optionally substituted hydrocarbon residue which may be attached through a hetero atom; R² is a group capable of forming an anion or a group convertible thereinto; R³ is an optionally substituted aromatic hydrocarbon or heterocyclic residue which contains at least one hetero atom; X is a direct bond or a spacer having an atomic length of two or less between the R³ group and the ring W group; W is an optionally substituted aromatic hydrocarbon or heterocyclic residue which contains at least one hetero atom;
    a,c and d are independently selected from the group consisting of one or two optionally substituted carbon atoms and one or two optionally substituted hetero atoms; b and e are independently selected from the group consisting of one optionally substituted carbon atom and one optionally substituted nitrogen atom; the dotted line is a bond to form one double bond; n is an integer of 1 or 2 and when a, which is an optionally substituted carbon atom, is taken together with R¹, the following group:

    may form a ring group; provided that when

    is a benzimidazole, thieno[3,4-d]imidazole, or thieno[2,3-d]imidazole ring, at least one of the group:

    and R³ is an optionally substituted heterocyclic residue ; and the pharmaceutically acceptable salts thereof, have potent angiotensinII antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.

    摘要翻译： 式（I）的稠合杂环化合物：其中R 1是可通过杂原子连接的任选取代的烃残基; R 2是能够形成阴离子或可转化为其的基团的基团; R 3是含有至少一个杂原子的任选取代的芳烃或杂环残基; X是在R 3基团和环W基团之间原子长度等于或小于2的直接键或间隔基; W是含有至少一个杂原子的任选取代的芳族烃或杂环残基; a，c和d独立地选自一个或两个任选取代的碳原子和一个或两个任选取代的杂原子; b和e独立地选自一个任选取代的碳原子和一个任选取代的氮原子; 虚线是形成一个双键的键; n是1或2的整数，并且当任意取代的碳原子a与R 1一起时，下列基团可以形成环基团; 条件是当为苯并咪唑，噻吩并[3,4-d]咪唑或噻吩并[2,3-d]咪唑环时，至少一个基团：和R 3是任选取代的杂环残基; 及其药学上可接受的盐具有有效的血管紧张素II拮抗活性和抗高血压活性，因此可用作治疗循环系统疾病如高血压疾病，心脏疾病（例如高血压，心力衰竭，心肌梗塞等），中风， 脑卒中，肾炎等