Title:
ビトロネクチンレセプター拮抗物質
Document Type and Number:
Japanese Patent JP4491072
Kind Code:
B2
Abstract:
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).
Inventors:
Callahan, James Francis
Cousins, Russell Donovan
Keenan, Richard McCulloch
Kwon, Chet
Miller, William Henry
Udinkas, Irene Nijol
Cousins, Russell Donovan
Keenan, Richard McCulloch
Kwon, Chet
Miller, William Henry
Udinkas, Irene Nijol
Application Number:
JP51694298A
Publication Date:
June 30, 2010
Filing Date:
October 01, 1997
Export Citation:
Assignee:
GlaxoSmithKline LLC
International Classes:
C07D223/00; A61K31/415; C07D401/12; A61K31/44; A61K31/445; A61K31/47; A61K31/4704; A61K31/495; A61K31/52; A61K31/55; A61K31/551; A61K33/243; A61K45/06; A61P9/00; A61P9/10; A61P19/10; A61P29/00; A61P35/00; A61P43/00; C07D223/16; C07D233/56; C07D233/64; C07D235/18; C07D235/22; C07D243/14; C07D401/00; C07D401/14; C07D403/12; C07D413/12; C07D417/12; C07D487/00
Foreign References:
| WO1996000574A1 | ||||
| WO1996000730A1 | ||||
| WO1996006087A1 | ||||
| WO1996026190A1 |
Attorney, Agent or Firm:
Mitsuo Tanaka
Hiroshi Yamazaki
Tadayuki Motoyama
Kenji Tomita
Nishino Mitsuru
Mizuhara Masahiro
Hiroshi Yamazaki
Tadayuki Motoyama
Kenji Tomita
Nishino Mitsuru
Mizuhara Masahiro