Title:
第Xa因子阻害剤としてのフェニル誘導体
Document Type and Number:
Japanese Patent JP2005501075
Kind Code:
A
Abstract:
Bicyclic benzene derivatives (I) are new. Bicyclic benzene derivatives of formula (I) and their derivatives, solvates and stereoisomers are new. D = (un)saturated 3-4C alkylene, optionally by 1-3 C atoms replaced by heteroatoms (by 1-3 N, 1-2 O and/or 1-2 S) and optionally substituted by 1-3 halo, A, (C(R)2)nQ, OR', N(R')2, NO2, CN, COOR', CON(R')2, NR'COA, NR'SO2A, COR', SO2NR' and SOmA and optionally with one CH2 group replaced by CO; R1 = H, halo, A, OR', N(R')2, CN, COOR', CON(R')2 or (C(R)2)nQ; R' = H, A or (C(R)2)nQ; R = H or A; Q = Ar, Het or cycloalkyl; W = C(R')2, (C(R')2)2, OC(R')2 or NR'C(R')2; X = CONR', CONR'CR2, C(R)2NR' or C(R)2NR'C(R)2; Y = alkylene, cycloalkylene, Het-diyl or Ar-diyl; T = mono- or bicyclic heterocyclyl with 1-4 N, O and/or S atoms and substituted by 1-3 oxo groups and 0-3 halo, A, (C(R)2)nQ, OR', N(R')2, NO2, CN, COOR', CON(R')2, NR'COA, NR'SO2A, COR', SO2NR' and SOmA; A = 1-6C alkyl in which 1-2 CH2 groups can be replaced by O, S and/or CH=CH and 1-7 H atoms can be replaced by F; Ar = phenyl, naphthyl or biphenylyl optionally substituted by 1-3 halo, A, OR', N(R')2, NO2, CN, COOR', CON(R')2, NR'COA, NR'SO2A, COR', SO2NR' and SOmA; Het = mono- or bicyclic heterocyclyl with 1-4 N, O and/or S atoms optionally substituted by 1-3 oxo, halo, A, (C(R)2)nQ', OR', NR'2, NO2, CN, COOR', CON(R')2, NR'COA, NR'SO2A, COR', SO2NR' and SOmA; Q' = Ar, Het' or cycloalkyl; Het' = mono- or bicyclic heterocyclyl with 1-2 N, O and/or S atoms optionally substituted by 1-2 oxo, halo, A, OR', N(R')2, NO2, CN, COOR', CON(R')2, NR'COA, NR'SO2A, COR', SO2NR' and SOmA; and n, m = 0-2. Independent claims are also included for: (1) preparation of (I); (2) a kit comprising a compound (I) and another drug in separate packs; and (3) intermediates of formula (VI). R'' = H or Me; and n' = 3-5.
Inventors:
Dolsh Dieter
Cezanne, Bertram
Zakura Kydis, Christos
Medellsky, Werner
Glitz, johannes
Burns, christopher
Cezanne, Bertram
Zakura Kydis, Christos
Medellsky, Werner
Glitz, johannes
Burns, christopher
Application Number:
JP2003518540A
Publication Date:
January 13, 2005
Filing Date:
July 12, 2002
Export Citation:
Assignee:
Merck Patent Gesellschaft mit beschraenkter Haftung
International Classes:
A61K31/439; A61K31/451; A61K31/4525; A61K31/453; A61K31/454; A61K31/4709; A61K31/4725; A61K31/496; A61K31/497; A61K31/498; A61K31/501; A61K31/513; A61K31/5377; A61K31/55; A61P7/02; A61P9/00; A61P9/10; A61P25/06; A61P29/00; A61P35/00; A61P35/04; C07D211/76; C07D401/12; C07D405/12; C07D413/12; C07D417/12; C07D453/06; (IPC1-7): C07D211/76; A61K31/439; A61K31/451; A61K31/4525; A61K31/453; A61K31/454; A61K31/4709; A61K31/4725; A61K31/496; A61K31/497; A61K31/498; A61K31/501; A61K31/513; A61K31/5377; A61K31/55; A61P7/02; A61P9/00; A61P9/10; A61P25/06; A61P29/00; A61P35/00; A61P35/04; C07D401/12; C07D405/12; C07D413/12; C07D417/12; C07D453/06
Attorney, Agent or Firm:
Kiyoji Kuzuwa