首页> 外国专利> VITRONECTIN RECEPTOR ANTAGONISTS, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME AND USE THEREOF IN THE PREPARATION OF MEDICAMENTS FOR TREATMENT OF OSTEOPOROSIS AND INHIBITION OF ANGIOGENESIS

VITRONECTIN RECEPTOR ANTAGONISTS, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME AND USE THEREOF IN THE PREPARATION OF MEDICAMENTS FOR TREATMENT OF OSTEOPOROSIS AND INHIBITION OF ANGIOGENESIS

机译：葡萄胎蛋白受体拮抗剂，其制备方法，包含相同成分的药物组合物，及其在制备治疗骨质疏松和抑制血管生成的药物中的用途

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Benzodiazepine compounds (I) of formula (I'; R = H), and their salts, are new: R1 = 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 3-4C oxoalkenyl, 3-4C oxoalkynyl, 1-4C aminoalkyl, 3-4C aminoalkenyl, 3-4C aminoalkynyl, (all optionally substituted by one A and one or more R10 or R7), H or R7; A = 3-6C cycloalkyl, Het or Ar; R7 = COR8, COC(R')2R9, C(S)R8, S(O)mOR', S(O)mNR'R'', PO(OR'), PO(OR')2, NO2 or tetrazolyl; R8 = OR', NR'R'', NR'SO2R', NR'OR' or OC(R')2COOR'; R9 = OR', CN, S(O)rR', S(O)mN(R')2, COR', CON(R')2 or COOR'; R10 = 1-6C alkyl, 1-6C oxoalkyl, 2-6C alkenyl, 2-6C alkynyl, 1-6C alkyloxy, 1-6C alkylamino, S(O)r-(1-6C alkyl) (all optionally substituted by A), H, OH, NH2, S(O)rH, OR11, CN, NR'R11, NO2, CF3, S(O)rCF3, COOR' or CON(R')2; R11 = R', COR', CON(R')2, COOR', S(O)mR' or S(O)mN(R')2; R2 = a group of formula (a)-(i); W = (CHRg)a-U-(CHRg)b; U = bond, CO, C(Rg)2, C(=CRg2), S(O)k, O, NRg, CRgORg, CRg(ORk)C(Rg)2, C(Rg)2CRg(ORk), COC(Rg)2, C(Rg)2C(O), CONRi, NRiCO, OC(O), C(O)O, C(S)O, OC(S), C(S)NRg, NRgC(S), S(O)2NRg, NRgS(O)2, N=N, NRgNRg, NRgC(Rg)2, C(Rg)2NRg, C(Rg)2O, OC(Rg)2, CC or CRg=CRg; G = NRe, S or O; Rg = H, 1-6C alkyl (optionally substituted by Het, 3-7C cycloalkyl or Ar) or Het, 3-7C cycloalkyl or Ar; Rk = Rg, CORg or COORf; Ri = Rg or 1-6C alkyl (substituted by 1-3 halo, CN, N(Rg)2, ORg, SRg, COORg or CON(Rg)2); Rf = H, Ar, or 1-6C alkyl (optionally substituted by Ar); Re = Rg or (CH2)kCOORg; Rb, Rc = H, A, 1-6C alkyl (optionally substituted by A), halo, CF3, ORf, S(O)kRf, CORf, NO2, N(Rf)2, CON(Rf)2 or CH2N(Rf)2; or Rb+Rc complete a 5-6 membered aromatic or non-aromatic carbocyclic or heterocyclic ring (optionally mono- to tri- substituted by halo, CF3, 1-4C alkyl, ORf, S(O)kRf, CORf, COORf, OH, NO2, N(Rf)2, CON(Rf)2, CH2N(Rf)2 or methylenedioxy; Q = C-Ry, and one Q may also be N; R' = H, Ar, 3-6C cycloalkyl or 1-6C alkyl (optionally substituted by Ar or (3-6C cycloalkyl); R'' = R', COR' or COOR'; Ry = H, halo, ORg, SRg, CN, NRgRk, NO2, CF3, S(O)rCF3, COORg, CORg, CON(Rg)2 or 1-6C alkyl (optionally substituted by halo, ORg, SRg, CN, NRgR'', NO2, CF3, S(O)rR', COORg, CORg or CON(Rg)2); a, b, k, r, s = 0-2; m = 1 or 2; u, v = 0 or 1. Also defined is a variable R''' = H, A, 1-6C alkyl (optionally substituted by A), halo, CF3, ORf, S(O)kRf, CORf, NO2, N(Rf)2, CON(Rf)2 or CH2N(Rf)2 which is not shown in the formula. Also claimed is a composition comprising (I), a carrier, and optionally an antineoplastic agent or inhibitor of bone resorption. Intermediates (II) of formula (I'; R = 1-6C alkyl).

机译：式（I′; R ＝ H）的苯二氮卓化合物（I）及其盐是新的：R 1 ＝ 1-4C烷基，2-4C烯基，2-4C炔基，3-4C氧代烯基，3-4C氧代炔基， 1-4C氨基烷基，3-4C氨基烯基，3-4C氨基炔基（全部任选地被一个A和一个或多个R10或R7取代），H或R7; A ＝ 3-6C环烷基，Het或Ar; R7 = COR8，COC（R'）2R9，C（S）R8，S（O）mOR'，S（O）mNR'R''，PO（OR'），PO（OR'）2，NO2或四唑基; R8 = OR'，NR'R''，NR'SO2R'，NR'OR'或OC（R'）2COOR'; R9 ＝ OR′，CN，S（O）rR′，S（O）mN（R′）2，COR′，CON（R′）2或COOR′; R10 = 1-6C烷基，1-6C氧代烷基，2-6C烯基，2-6C炔基，1-6C烷氧基，1-6C烷基氨基，S（O）r-（1-6C烷基）（全部可选地被A取代），H，OH，NH2，S（O）rH，OR11，CN，NR'R11，NO2，CF3，S（O）rCF3，COOR'或CON（R'）2; R11 = R'，COR'，CON（R'）2，COOR'，S（O）mR'或S（O）mN（R'）2; R2 ＝一组式（a）-（i）; W =（CHRg）a-U-（CHRg）b; U =键，CO，C（Rg）2，C（= CRg2），S（O）k，O，NRg，CRgORg，CRg（ORk）C（Rg）2，C（Rg）2CRg（ORk），COC （Rg）2，C（Rg）2C（O），CONRi，NRiCO，OC（O），C（O）O，C（S）O，OC（S），C（S）NRg，NRgC（S），S（O）2NRg，NRgS（O）2，N = N，NRgNRg，NRgC（Rg）2，C（Rg）2NRg，C（Rg）2O，OC（Rg）2，CC或CRg = CRg; G = NRe，S或O; Rg ＝ H，1-6C烷基（任选被Het，3-7C环烷基或Ar取代）或Het，3-7C环烷基或Ar; Rk = Rg，CORg或COORf; Ri = Rg或1-6C烷基（被1-3个卤素，CN，N（Rg）2，ORg，SRg，COORg或CON（Rg）2取代）; Rf ＝ H，Ar或1-6C烷基（任选地被Ar取代）; Re = Rg或（CH2）kCOORg; Rb，Rc = H，A，1-6C烷基（可选被A取代），卤素，CF3，ORf，S（O）kRf，CORf，NO2，N（Rf）2，CON（Rf）2或CH2N（Rf ）2;或Rb + Rc完整形成5-6元的芳族或非芳族碳环或杂环（可选地被卤素，CF3、1-4C烷基，ORf，S（O）kRf，CORf，COORf，OH取代为单取代或三取代，NO 2，N（Rf）2，CON（Rf）2，CH 2 N（Rf）2或亚甲二氧基; Q = C-Ry，一个Q也可以是N; R'= H，Ar，3-6C环烷基或1 -6C烷基（可选地被Ar或（3-6C环烷基）取代; R''= R'，COR'或COOR'; Ry = H，卤素，ORg，SRg，CN，NRgRk，NO2，CF3，S（O rCF3，COORg，CORg，CON（Rg）2或1-6C烷基（可选被卤素，ORg，SRg，CN，NRgR''，NO2，CF3，S（O）rR'，COORg，CORg或CON（ Rg）2）; a，b，k，r，s = 0-2; m = 1或2; u，v = 0或1.还定义了变量R'''= H，A，1-6C烷基（任选被A取代），卤素，CF 3，ORf，S（O）kRf，CORf，NO 2，N（Rf）2，CON（Rf）2或CH 2 N（Rf）2，也未在公式中显示。要求保护的组合物包含（I），载体和任选的抗骨吸收剂或骨吸收抑制剂式（I′; R ＝ 1-6C烷基）的中间体（II）。

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公开/公告号IL129243A

专利类型
公开/公告日2004-07-25

原文格式PDF
申请/专利权人 SMITHKLINE BEECHAM CORPORATION;
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申请/专利号IL19970129243
发明设计人
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申请日1997-10-01
分类号C07D401/12;C07D401/14;C07D403/12;C07D403/14;C07D413/12;C07D413/14;C07D417/12;C07D417/14;C07D471/02;C07D491/02;C07F9/547;A61K31/395;A61K31/661;A61P9/00;A61P29/00;
国家 IL
入库时间 2022-08-21 23:10:38

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