Title:
【発明の名称】アミジノフェノール誘導体およびその誘導体を有効成分として含有する薬剤
Document Type and Number:
Japanese Patent JP2736952
Kind Code:
B2
Abstract:
Amidinophenol derivatives of the formula (I): wherein R<1> and R<2> are (i) H, (ii) C1-4 alkyl, (iii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO2, (vii) benzoyl, (viii) COOR<4>(in which R<4> is C1-3 alkyl); A is bond, C1-4 alkylene, -C(R<5>)=C(R<6>)- (in which R<5> and R<6> are H or C1-4 alkyl); R<3> is (i) CON(R<7>)(R<8>), (ii) CON(R<9>)-CH(R<7>)(R<8>) or (iii) (in which R<7> and R<8> are (1) H, (2) phenyl, (3) C7-10 phenylalkyl, (4) pheny or C7-10 phenylalkyl substituted by 1or 2 C1-4 alkyl, halogen or R<1><1>-COOR<1><2> (in which R<1><1> is bond, C1-8 alkylene, C2-8 alkenylene, C2-8 alkynylene; R<1><2> is H, C1-4 alkyl, C7-10 phenylalkyl, phenyl, allyl, propargyl), (5) C1-10 alkyl, (6) C2-10 alkenyl having 1 to 3 double bonds, (7) C2-10 alkynyl having 1 or 2 triple bonds, (8) R<11a>-COXR<1><2>(in which R<11a> is (a) bond, (b) C1-8 alkylene, (c) C2-8 alkylene in which 1 or 2 carbon atoms in the main chain are replaced by sulfur, or sulfur and phenylene, (d) C2-8 alkenylene, (e) C4-8 alkenylene in which 1 or 2 carbon atoms in the main chain are replaced by sulfur, or sulfur and phenylene, (f) C2-8 alkynylene, (g)C4-8 alkynylene in which 1 or 2 carbon atoms in the main chain are replaced by sulfur, or sulfur and phenylene; X is -O- or -NH-), (9) C1-4 alkyl substituted by a 7-14 membered, bi- or tri-cyclic hetero ring containing one N atom, (10) C3-7 cycloalkyl); R<9> is (1) H, (2) C1-8 alkyl, (3) C7-10 phenylalkyl, (4) C2-10 alkenyl having 1 to 3 double bonds, (5) C2-10 alkynyl having 1 or 2 triple bonds, (6) R<1><1>-COOR<1><2>, (7) C3-7 cycloalkyl; @ @ is 4-7 membered, mono-cyclic hetero ring containing 1 or 2 N atom; R<1><0> is H, C7-10 phenylalkyl or COOR<1><3>(in which R<1><3> is H, C1-4 alkyl or C7-10 phenylalkyl)); with the proviso that (i) both R<7> and R<8> do not represent hydrogen at the same time, and (ii) when at least one group in R<7>, R<8> and R<9> represents the group containing t-butyl ester, the other groups do not represent the group containing carboxy; or an acid addition salt thereof, have inhibitory activities on PLA2 and on various proteases such as trypsin, plasmin, thrombin, kallikrein, especially trypsin, and are useful for the prevention and/or the treatment of various inflammatory diseases, allergic diseases, disseminated intravascular coagulation, pancreatitis, severity in pancreatitis and multiple organ failure.
Inventors:
NAKAI HISAO
KAWAMURA MASANORI
MYAMOTO TSUMORU
KAWAMURA MASANORI
MYAMOTO TSUMORU
Application Number:
JP25217893A
Publication Date:
April 08, 1998
Filing Date:
September 16, 1993
Export Citation:
Assignee:
ONO YAKUHIN KOGYO KK
International Classes:
A61K31/235; A61K31/40; C07D295/18; A61K31/403; A61K31/404; A61K31/405; A61K31/495; A61P29/00; A61P37/08; A61P43/00; C07C257/18; C07C323/59; C07C323/62; C07C323/63; C07D205/04; C07D207/08; C07D207/16; C07D209/20; C07D223/04; C07D295/185; C07D295/192; (IPC1-7): C07C257/18; A61K31/235
Attorney, Agent or Firm:
Kunihisa Oya