发明公开
EP0652208A1 Phenylalkan(en)oic acids with leukotriene B4 antagonistic activity
失效
苯基(en)-Sauren mit白三烯B4拮抗剂Wirkung。
- 专利标题: Phenylalkan(en)oic acids with leukotriene B4 antagonistic activity
- 专利标题(中): 苯基(en)-Sauren mit白三烯B4拮抗剂Wirkung。
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申请号: EP94118144.8申请日: 1990-05-16
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公开(公告)号: EP0652208A1公开(公告)日: 1995-05-10
- 发明人: Konno, Mitoshi, Ono Pharmaceutical Co.,Ltd. , Nakae, Takahiko, Ono Pharmaceutical Co.,Ltd. , Hamanaka, Nobuyuki, Ono Pharmaceutical Co.,Ltd.
- 申请人: ONO PHARMACEUTICAL CO., LTD.
- 申请人地址: 1-5, Doshomachi 2-chome Chuo-ku Osaka-shi Osaka JP
- 专利权人: ONO PHARMACEUTICAL CO., LTD.
- 当前专利权人: ONO PHARMACEUTICAL CO., LTD.
- 当前专利权人地址: 1-5, Doshomachi 2-chome Chuo-ku Osaka-shi Osaka JP
- 代理机构: Henkel, Feiler, Hänzel & Partner
- 优先权: JP164213/89 19890627; JP310545/89 19891201; JP1799/90 19900109
- 主分类号: C07C233/54
- IPC分类号: C07C233/54 ; A61K31/16 ; C07D209/08 ; C07D277/42 ; C07C323/19 ; C07C235/16 ; C07C311/21 ; C07C235/20 ; C07C235/34 ; C07C235/78 ; C07C59/68
摘要:
The phenylalkan(en)oic acids of the formula:
wherein A is
i) ―NHCO―,
ii) ―O―
iii) ―NHSO₂―,
iv) ―CO―
v) ―CH₂― or
vi) ―CH(OH)―;
W is C1-13 alkylene;
R¹ is
i) hydrogen,
ii) C1-4 alkyl,
iii) ―COOH,
iv) saturated or unsaturated, 4-7 membered mono-cyclic hetero ring containing one nitrogen as a hetero atom or saturated or unsaturated, 4-7 membered mono-cyclic hetero ring containing one nitrogen as a hetero atom substituted by an oxo group,
v)
vi) ―CH₂OH;
A, taken together with W and R¹, is
i)
ii)
iii) ―N―(SO₂R⁶)₂,
iv)
or
v)
two R² are, same or different,
i) hydrogen,
ii) C1-4 alkyl or
iii) 4-7 membered, saturated or unsaturated, mono-cyclic hetero ring containing two or three of nitrogen and sulfur in total,
or two R², taken together with a nitrogen to which they are attached, form saturated or unsaturated
i) 7-14 membered, bi-or tri-cyclic hetero ring containing one nitrogen as a hetero atom, or
ii) 4-7 membered, mono-cyclic hetero ring containing two or three of nitrogen and oxygen in total ;
Y is ethylene or vinylene;
D is
i) ―Z―B or
ii)
Z is C3-11 alkylene or alkenylene
B is
or
Z, taken together with B, is C3-22 alkyl;
R³ is
i) hydrogen,
ii) halogen,
III) C1-8 alkyl, alkoxy or alkylthio, or
iv) C2-8 alkenyl, alkenyloxy or alkenylthio;
n is 1-3;
R⁴ is C1-7 alkylene;
R⁵ is
i) C1-12 alkyl,
ii) C2-12 alkenyl,
iii) C5-7 cycloalkyl or
iv) phenethyl or phenethyl wherein the ring is substituted by one C1-4 alkoxy;
two R⁶ are, same or different,
i) C1-7 alkyl,
ii) benzyl or
iii) phenyl or phenyl wherein the ring is substituted by one C1-4 alkyl; and
Two R⁷ are, same or different, C1-4 alkyl;
with the proviso that
―A―W―R¹ should bind to 4- carbon in benzene ring, and
and non-toxic salts thereof,
possess an antagonism on leukotriene B₄, and therefore, are useful for the prevention and treatment of several diseases induced by leukotriene B₄.
wherein A is
i) ―NHCO―,
ii) ―O―
iii) ―NHSO₂―,
iv) ―CO―
v) ―CH₂― or
vi) ―CH(OH)―;
W is C1-13 alkylene;
R¹ is
i) hydrogen,
ii) C1-4 alkyl,
iii) ―COOH,
iv) saturated or unsaturated, 4-7 membered mono-cyclic hetero ring containing one nitrogen as a hetero atom or saturated or unsaturated, 4-7 membered mono-cyclic hetero ring containing one nitrogen as a hetero atom substituted by an oxo group,
v)
vi) ―CH₂OH;
A, taken together with W and R¹, is
i)
ii)
iii) ―N―(SO₂R⁶)₂,
iv)
or
v)
two R² are, same or different,
i) hydrogen,
ii) C1-4 alkyl or
iii) 4-7 membered, saturated or unsaturated, mono-cyclic hetero ring containing two or three of nitrogen and sulfur in total,
or two R², taken together with a nitrogen to which they are attached, form saturated or unsaturated
i) 7-14 membered, bi-or tri-cyclic hetero ring containing one nitrogen as a hetero atom, or
ii) 4-7 membered, mono-cyclic hetero ring containing two or three of nitrogen and oxygen in total ;
Y is ethylene or vinylene;
D is
i) ―Z―B or
ii)
Z is C3-11 alkylene or alkenylene
B is
or
Z, taken together with B, is C3-22 alkyl;
R³ is
i) hydrogen,
ii) halogen,
III) C1-8 alkyl, alkoxy or alkylthio, or
iv) C2-8 alkenyl, alkenyloxy or alkenylthio;
n is 1-3;
R⁴ is C1-7 alkylene;
R⁵ is
i) C1-12 alkyl,
ii) C2-12 alkenyl,
iii) C5-7 cycloalkyl or
iv) phenethyl or phenethyl wherein the ring is substituted by one C1-4 alkoxy;
two R⁶ are, same or different,
i) C1-7 alkyl,
ii) benzyl or
iii) phenyl or phenyl wherein the ring is substituted by one C1-4 alkyl; and
Two R⁷ are, same or different, C1-4 alkyl;
with the proviso that
―A―W―R¹ should bind to 4- carbon in benzene ring, and
and non-toxic salts thereof,
possess an antagonism on leukotriene B₄, and therefore, are useful for the prevention and treatment of several diseases induced by leukotriene B₄.
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