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    Pyrazole compounds
    8.
    发明授权
    Pyrazole compounds 失效
    吡唑化合物

    公开(公告)号：US07612201B2

    公开(公告)日：2009-11-03

    申请号：US10536899

    申请日：2003-12-18

    申请人： Mandy Christine Beswick ,  Martin James Drysdale ,  Brian William Dymock ,  Edward McDonald

    发明人： Mandy Christine Beswick ,  Martin James Drysdale ,  Brian William Dymock ,  Edward McDonald

    IPC分类号： C07D231/38 ,  C07D401/04 ,  C07D403/04 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    CPC分类号： C07D231/38 ,  A61K31/415 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： Compounds of formula (IA) or (IB) or a salt, N-oxide, hydrate or solvate thereof are inhibitors of HSP90, and are of value in the treatment of diseases responsive to HSP90 inhibition such as cancers. In the formulae, Ar is an aryl, aryl(C1-C6 alkyl), aryl(C1-C6 alkyl), heteroaryl, heteroarylaryl(C1-C6 alkyl), or heteroarylaryl(C1-C6 alkyl) group, any of which being optionally substituted in the aryl or heteroaryl part thereof; R1, is hydrogen or optionally substituted C1-C6 alkyl; R2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and ring A is a non aromatic carbocyclic or heterocyclic ring wherein (i) a ring carbon is optionally substituted, and/or (ii) a ring nitrogen is optionally substituted by a group of formula -(Alk1)p (Cyc)n-(Alk3)m-(Z)r (Alk2)s Q where Alk1, Alk2 and Alk3 are optionally substituted C1-C3 alkyl, Cyc is an optionally substituted carbocyclic or heterocyclic radical; m, n, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C═O)—, —S02-, —C(═O)O—, —OC(═O)—, —NW—, —C(═O)NRA-, —NRAC(═O)—, —SO2NRA—, or —NRASO2— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical.

    摘要翻译： 式（IA）或（IB）化合物或其盐，N-氧化物，水合物或溶剂合物是HSP90的抑制剂，并且在治疗对HSP90抑制作用的疾病如癌症的治疗中具有价值。 在式中，Ar是芳基，（C 1 -C 6烷基），芳基（C 1 -C 6烷基），杂芳基，杂芳基芳基（C 1 -C 6烷基）或杂芳基芳基（C 1 -C 6烷基） 在其芳基或杂芳基部分取代; R1是氢或任选取代的C 1 -C 6烷基; R 2是氢，任选取代的环烷基，环烯基，C 1 -C 6烷基，C 1 -C 6烯基或C 1 -C 6炔基; 或羧基，羧酰胺或羧基酯基团; 环A是非芳族碳环或杂环，其中（i）环碳任选被取代，和/或（ii）环氮任选地被式 - （Alk1）p（Cyc）n-（ Alk3）m-（Z）r（Alk2）sQ其中Alk1，Alk2和Alk3是任选取代的C 1 -C 3烷基，Cyc是任选取代的碳环或杂环基; m，n，p，r和s独立地为0或1，Z为-O - ， - S - ， - （CO） - ， - SO2-，-C - ，-NW-， - C（ - O）NRA - ， - NRAC（-O） - ， - SO2NRA-或-NRASO2-，其中RA是氢或C1-C6烷基，Q是氢或任选取代的碳环 或杂环基。

    Enzyme Inhibitors
    9.
    发明申请
    Enzyme Inhibitors 有权
    酶抑制剂

    公开(公告)号：US20090247507A1

    公开(公告)日：2009-10-01

    申请号：US12158339

    申请日：2006-12-21

    申请人： Vassilios Bavetsias ,  Edward McDonald ,  Spyridon Linardopoulos

    发明人： Vassilios Bavetsias ,  Edward McDonald ,  Spyridon Linardopoulos

    IPC分类号： A61K31/551 ,  C07D471/04 ,  A61P37/02 ,  A61P35/00 ,  C12N9/99 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/496

    CPC分类号： C07D471/04

    摘要： Compounds of formula (I), are aurora kinase inhibitors: wherein X is —N—, —CH2—N—, —CH2—CH—, or —CH—; R1 is a radical of formula (IA) wherein Z is —CH2—, —NH—, -0-, —S(O)— —S—, —S(O)2 or a divalent monocyclic carbocyclic or heterocyclic radical having 3-7 ring atoms; Alk is an optionally substituted divalent C1-C6 alkylene radical; A is hydrogen or an optionally substituted monocyclic carbocyclic or heterocyclic ring having 5-7 ring atoms; r, s and t are independently 0 or 1, provided that when A is hydrogen then at least one of r and s is 1; R2 is halogen, —CN, —CF3, —OCH3, or cyclopropyl; and R3 is a radical of formula (IB) wherein Q is hydrogen or an optionally substituted phenyl or monocyclic heterocyclic ring with 5 or 6 ring atoms; Z&It;1> is —S—, —S(O)—, —S(O)2—, —O—, —SO2NH—, —NHSO2—, NHC(═O)NH, —NH(C═S)NH—, Or —N(R4)—wherein R4 is hydrogen, C1-C3 alkyl, cycloalkyl, or benzyl; and Alk&It;1> and Alk&It;2> are, independently, optionally substituted divalent C1-C3 alkylene radicals; and m, n and p are independently 0 or 1. Data supplied from the esp@cenet datatbase—Worldwide d77

    摘要翻译： 式（I）化合物是极光激酶抑制剂：其中X是-N-，-CH 2 -N，-CH 2 -CH-或-CH-; R1是式（IA）的基团，其中Z是-CH 2 - ， - NH - ， - O - ， - S（O）-S - ， - S（O）2或具有3价的二价单环碳环或杂环基 -7环原子; Alk是任选取代的二价C 1 -C 6亚烷基; A是氢或任选取代的具有5-7个环原子的单环碳环或杂环; r，s和t独立地为0或1，条件是当A为氢时，r和s中的至少一个为1; R2是卤素，-CN，-CF3，-OCH3或环丙基; 并且R 3是式（IB）的基团，其中Q是氢或具有5或6个环原子的任选取代的苯基或单环杂环; （O） - ， - S（O）2 - ， - O - ， - SO 2 NH-，-NHSO 2 - ，NHC（-O）NH，-NH（CS）NH- 或-N（R4） - 其中R4是氢，C1-C3烷基，环烷基或苄基; 和Alk＆It; 1>和Alk＆It; 2>独立地是任选取代的二价C1-C3亚烷基; m，n和p独立为0或1.从esp @ cenet datatbase-Worldwide d77提供的数据

    Substituted 5-membered ring compounds and their use
    10.
    发明申请
    Substituted 5-membered ring compounds and their use 失效
    取代的5元环化合物及其用途

    公开(公告)号：US20060235058A1

    公开(公告)日：2006-10-19

    申请号：US10561969

    申请日：2004-06-24

    申请人： Kwai Cheung ,  Brian Dymock ,  Edward McDonald ,  Martin Drysdale

    发明人： Kwai Cheung ,  Brian Dymock ,  Edward McDonald ,  Martin Drysdale

    IPC分类号： A61K31/4196 ,  A61K31/4192 ,  C07D249/04 ,  C07D249/08 ,  A61K31/41

    CPC分类号： A61K31/4196 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/433

    摘要： Compound of a compound of formula (1) or a salt, N-oxide, hydrate or solvate thereof, in the preparation of a composition for inhibition of HSP90 activity: wherein ring A is an aromatic or non-aromatic carbocyclic or heterocyclic ring having 5 ring atoms, for example 1,2,3-triazolyl or a 1,2,4-triazolyl or a tetrazolyl ring; and R1 R2 R3 are as defined in the specification are inhibitors of HSP90 and therefore of use in the treatment of, for example, cancers, viral disease, inflammatory diseases such as rheumatoid arthritis, asthma, multiple sclerosis, Type I diabetes, lupus, psoriasis and inflammatory bowel disease; cystic fibrosis angiogenesis-related disease such as diabetic retinopathy, haemangiomas, and endometriosis; or for protection of normal cells against chemotherapy-induced toxicity; or diseases where failure to undergo apoptosis is an underlying factor, or protection from hypoxia-ischemic injury due to elevation of Hsp70 in the heart and brain; scrapie /CJD, Huntingdon's and Alzheimer's disease.

    摘要翻译： 式（1）化合物或其盐，N-氧化物，水合物或溶剂化物的化合物在制备抑制HSP90活性的组合物中的用途：其中环A是具有5个或更多个碳原子的芳族或非芳族碳环或杂环 环原子，例如1,2,3-三唑基或1,2,4-三唑基或四唑基环; 和R 1 R 2 R 3 R 3如本说明书中所定义的是HSP90的抑制剂，因此用于治疗，例如， 癌症，病毒性疾病，炎性疾病如类风湿性关节炎，哮喘，多发性硬化，I型糖尿病，狼疮，牛皮癣和炎症性肠病; 囊性纤维化血管生成相关疾病如糖尿病性视网膜病变，血管瘤和子宫内膜异位症; 或用于保护正常细胞免受化疗诱导的毒性; 或未能进行细胞凋亡的疾病是潜在的因素，或由于心脏和脑中Hsp70的升高而保护缺氧缺血性损伤; 瘙痒病/ CJD，亨廷顿氏症和阿尔茨海默病。