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Novel compounds as receptor modulators with therapeutic utility
专利权人:
ALLERGAN INC.
发明人:
HEIDELBAUGH TODD M.,NGUYEN PHONG X.
申请号:
NZ59996610
公开号:
NZ599966A
申请日:
2010.11.19
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
Disclosed are 1-(benzyl)azetidine-3-carboxylic acid and 3-benzylamino)cyclobutanecarboxylic acid derivatives as represented by the general formula (I), wherein: R1 is CH R2 is an aromatic heterocycle, a non-aromatic heterocycle, cycloalkyl, cycloalkenyl or aryl, each of which is optionally substituted with one or more alkyl groups R3 is O or S R4 is optionally substituted aryl R5 is H, halogen or alkoxy R6 is H R7 is H or alkyl R8 is H R9 is CH or N R10 is carboxylic acid a is 0, 1, 2 or 3 b is 0, 1, 2 or 3 c is 1 d is 0 or 1 e is 0 f is 1 g is 0 L is CH2, CH(alkyl) or O and with the proviso that when R3 is O or S and b is 0 or 1 then L is not O. Representative compounds of formula I include 1-{ 3-(3-furyl)-4-[(5-phenylpentyl)oxy]benzyl} azetidine-3-carboxylic acid, 1-{ 3-chloro-4-[(5-phenylpentyl)oxy]-5-(2-thienyl)benzyl} azetidine-3-carboxylic acid, 1-{ 4-[(5-phenylpentyl)oxy]-3-(1,3-thiazol-5-yl)benzyl} azetidine-3-carboxylic acid, 1-{ 4-[(5-phenylpentyl)oxy]-3-(1,3-thiazol-4-yl)benzyl} azetidine-3-carboxylic acid, 1-{ 3-cyclopent-1-en-1-yl-4-[(5-phenylpentyl)oxy]benzyl} azetidine-3-carboxylic acid, 1-{ 4-[(5-phenylpentyl)oxy]-3-(2-thienyl)benzyl} azetidine-3-carboxylic acid, 1-{ 4-[(5-phenylpentyl)oxy]-3-(1H-pyrazol-5-yl)benzyl} azetidine-3-carboxylic acid, 1-{ 4-[(5-phenylpentyl)oxy]-3-(1H-pyrazol-4-yl)benzyl} azetidine-3-carboxylic acid, 1-{ 4-[(5-phenylpentyl)oxy]-3-(3-thienyl)benzyl} azetidine-3-carboxylic acid, 1-{ 3-(2-furyl)-4-[(5-phenylpentyl)oxy]benzyl} azetidine-3-carboxylic acid, 1-{ 4-[(5-phenylpentyl)oxy]-3-(1,3-thiazol-2-yl)benzyl} azetidine-3-carboxylic acid, 1-{ 3-(1,3-oxazol-2-yl)-4-[(5-phenylpentyl)oxy]benzyl} azetidine-3-carboxylic acid, 1-{ 4-[(5-phenylpentyl)oxy]-3-(1H-pyrazol-1-yl)benzyl} azetidine-3-carboxylic acid and 3-({ 4-[(5-phenylpentyl)oxy]-3-(2-thienyl)benzyl} amino)cyclobutane-carboxylic acid. Further disclosed is a pharmaceutical composition comprising as an active ingredient a therapeutically effective amount of a compound as de
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