您的位置: 首页 > 农业专利 > 详情页

DERIVES DE 1,3-BENZOXAZOLYLE SERVANT D'INHIBITEURS DE KINASE
专利权人:
MERCK PATENT GMBH
发明人:
STAEHLE, WOLGANG,JONCZYK, ALFRED,RAUTENBERG, WILFRIED
申请号:
EP04764704.5
公开号:
EP1664039B1
申请日:
2004.09.01
申请国别(地区):
EP
年份:
2014
代理人:
摘要:
2-(4-Substituted anilino)-1,3-benzoxazole derivatives (I) and their salts, derivatives, solvates and stereoisomers (including mixtures in all proportions) are new. Benzoxazoles of formula (I) and their salts, derivatives, solvates and stereoisomers (including mixtures in all proportions) are new. [Image] R 1>; - R 3>;R, halo, CN, NO 2, NHR, NRR, NHCOR, NHSO 2R, OR, COR, CONHR, CF 3, OCF 3, SCF 3, SO 3R, SO 2R, SO 2NR or COOR; R : H; or A, Ar, Het, (CH 2) qAr or (CH 2) qHet (all optionally substituted (os) by 1-4 R 4>; groups); A : 1-14C linear, branched or cyclic alkyl (optionally having 1 or 2 CH 2 groups replaced by O, S and/or CH=CH and os by 1-7 F and/or Cl); A : phenyl, naphthyl or biphenyl (all os by 1-3 of A, halo, OH, OA, CN, NO 2, NH 2, NHA, NA 2, NHCOA, SCF 3, SO 2A, COOH, COOA, CONH 2, CONHA, CONA 2, NHSO 2A, SO 2NH 2, SO 2NHA, SO 2NA 2, CHO or COA); Het : mono- or bicyclic, saturated, unsaturated or aromatic heterocycle containing 1-4 of N, O and/or S (os by 1-3 of =O, halo, A, -(CH 2) bAr, -(CH 2) b-cycloalkyl, OH, OA, NH 2, NHA, NA 2, NO 2, CN, COOH, COOA, CONH 2, CONHA, CONA 2, NHCOA, NHCONH 2, NHSO 2A, CHO, COA, SO 2NH 2 and/or S(O) gA); R 4>;halo, OH, CN, NO 2, CF 3, OCF 3, SCF 3, SO 2A or OA; X : O, S, SO 2NH or NH; Y : phenyl or monocyclic heteroaryl with 1-4 N, O and/or S atoms; b : 0-4; g : 0-2; n, m, p, q : 1-4. An independent claim is included for the preparation of (I). ACTIVITY : Cytostatic; ophthalmological; antidiabetic; antiinflammatory; osteopathic; antiarthritic; antipsoriatic; antirheumatic; dermatological; antiallergic; gynecological; vulnerary; immunosuppressive; immunostimulant; antiarteriosclerotic; anti-HIV. MECHANISM OF ACTION : Kinase inhibitor. (5-Chloro-7-nitro-benzoxazol-2-yl)-(4-(pyridin-4-ylsulfanyl)-phenyl)-amine (Ia) had IC 5 0 310 nM for inhibition of TIE-2.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
相关发明人
相关专利

意 见 箱

匿名:登录

个人用户登录

找回密码

第三方账号登录

忘记密码

个人用户注册

必须为有效邮箱
6~16位数字与字母组合
6~16位数字与字母组合
请输入正确的手机号码

信息补充