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。

Phenylalkan(en)oic acids with leukotriene B4 antagonistic activity
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.
信息查询
0/0