US 2013/0261128 A1Published application

Continuous arycyclic compound

AssigneeMitsubishi Tanabe Pharma Corporation

InventorsOsamu Sakurai, Kunio Saruta, Norimitsu Hayashi, Takashi Goi, Kenji Morokuma, Hidekazu Tsujishima, Hiroaki Sawamoto, Hiroaki Shitama, Ritsuo Imashiro

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Abstract

This is to provide a continuous arycyclic compound having a DGAT1 inhibitory activity, and useful for prophylaxis and/or treatment of obesity or hyperlipidemia caused by obesity, hypertriglyceridemia, lipid metabolism disorder, fatty liver, hypertension, arteriosclerosis, diabetes, etc., as well as to provide a DGAT1 inhibitor comprising the continuous arycyclic compound or a pharmaceutically acceptable salt thereof as an effective ingredient. Disclosed is the continuous arycyclic compound is represented by the formula: wherein the substituents in the formula are the same as defined in the specification, or a pharmaceutically acceptable salt thereof.

Claims13

Dependent claims

A continuous arycyclic compound represented by the formula:

wherein Alk represents a linear C1-6 alkylene group, a branched C1-6 alkylene group or a C1-6 alkylene group having a ring structure;
where a part of the carbon atoms constituting the ring structure may be optionally substituted by an oxygen atom, a nitrogen atom or a sulfur atom, in Ring X,
X1 represents N or CRX1,
X2 represents N or CRX2,
X3 represents N or CRX3,
X4 represents N or CRX4,
where RX1, RX2, RX3 and RX4 each independently represents a hydrogen atom;
a linear or branched C1-6 alkyl group which may be substituted by a halogen atom(s);
a C3-7 alkyl group having a ring structure which may be substituted by a halogen atom(s);
a linear or branched C1-6 alkoxy group;
a halogen atom or a cyano group,
in Ring Y,
Y1 represents N or CRY1,
Y2 represents N or CRY2,
Y3 represents N or CRY3,
Y4 represents N or CRY4,
RY1, RY2, RY3 and RY4 each independently represents a hydrogen atom;
a linear or branched C1-6 alkyl group which may be substituted by a halogen atom(s);
a C3-7 alkyl group having a ring structure which may be substituted by a halogen atom(s);
a linear or branched C1-6 alkoxy group;
a halogen atom or a cyano group,
in Ring Z,
RZ represents a linear or branched C1-6 alkyl group which may be substituted by a halogen atom(s) or C3-7 alkyl group having a ring structure which may be substituted by a halogen atom(s),
or a pharmaceutically acceptable salt thereof.

21 more elements

A continuous arycyclic compound which is any one of the following compounds:

2,2-dimethyl-3-(4-{5-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-2-yl}phenoxy)-propanoic acid;
2,2-dimethyl-3-(4-{5-[5-(2,2,2-trifluoro-1,1-dimethylethyl)-1H-imidazol-2-yl]pyridin-2-yl}phenoxy)propanoic acid;
2,2-dimethyl-3-(4-{4-methyl-5-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-2-yl}-phenoxy)propanoic acid;
2,2-dimethyl-3-[4-(5-{5-[1-(trifluoromethyl)cyclopropyl]-1H-imidazol-2-yl}pyridin-2-yl)phenoxy)propanoic acid;
2,2-dimethyl-3-(4-{5-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyrazin-2-yl}phenoxy)-propanoic acid;
1-[(3-methyl-4-{5-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-2-yl]phenoxy)-methyl}cyclobutanecarboxylic acid;
3-(4-{5-[5-(3,3-difluorocyclobutyl)-1H-imidazol-2-yl]pyridin-2-yl}phenoxy)-2,2-dimethylpropanoic acid;
2,2-dimethyl-3-({4-methyl-6′-[5-(trifluoromethyl)-1H-imidazol-2-yl]-3,3′-bipyridin-6-yl}oxy)propanoic acid;
2,2-dimethyl-3-({4′-methyl-5-[5-(trifluoromethyl)-1H-imidazol-2-yl]-2,3′-bipyridin-6′-yl}oxy)propanoic acid;
2,2-dimethyl-3-[(4-methyl-5-{4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl}pyridin-2-yl)oxy]propanoic acid;
2,2-dimethyl-3-[(6-methyl-5-{4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl}pyridin-2-yl)oxy]propanoic acid;
3-[(5-{3-fluoro-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl}pyridin-2-yl)oxy]-2,2-dimethylpropanoic acid;
2,2-dimethyl-3-[(5-{4-[4-(trifluoromethyl)-1H-imidazol-2-yl]phenyl}pyrazin-2-yl)-oxy]propanoic acid;
2,2-dimethyl-3-[(4-methyl-5-{3-methyl-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]-phenyl}pyridin-2-yl)oxy]propanoic acid;
3-[(5-{3-fluoro-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl}-4-methylpyridin-2-yl)oxy]-2,2-dimethylpropanoic acid;
2,2-dimethyl-3-[4-[5-[4-(trifluoromethyl)-1H-imidazol-2-yl]-2-pyridyl]phenoxy]-propanoic acid;
3-[(5-{3-chloro-4-[4-(trifluoromethyl)-1H-imidazol-2-yl]phenyl}-4-methylpyridin-2-yl)oxy]-2,2-dimethylpropanoic acid;
3-{[5-(3-fluoro-4-{5-[1-(trifluoromethyl)cyclopropyl]-1H-imidazol-2-yl}phenyl)-4-methylpyridin-2-yl]oxy}-2,2-dimethylpropanoic acid;
2,2-dimethyl-3-[(4-methyl-5-{5-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyrazin-2-yl}pyridin-2-yl)oxy]propanoic acid;
and
3-[(5-{4-[5-(cyclopropylmethyl)-1H-imidazol-2-yl]-3-fluorophenyl}-4-methylpyridin-2-yl)oxy]-2,2-dimethylpropanoic acid;
1-[({4-methyl-6′-[5-(trifluoromethyl)-1H-imidazol-2-yl]-3,3′-bipyridin-6-yl]oxy)methyl}cyclobutanecarboxylic acid;
1-{[(5-{3-fluoro-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl}-4-methylpyridin-2-yl)oxy]methyl}cyclobutanecarboxylic acid;
1-[({5′-chloro-4-methyl-6′-[5-(trifluoromethyl)-1H-imidazol-2-yl]-3,3′-bipyridin-6-yl]oxy)methyl}cyclobutanecarboxylic acid;
1-{[(5-{3-chloro-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl}-4-methylpyridin-2-yl)oxy]methyl}cyclopropanecarboxylic acid;
1-{[(5-{3-chloro-4-[5-(trifluoromethyl)-1H-imidazol-2-yl]phenyl}-4-methylpyridin-2-yl)oxy]methyl}cyclobutanecarboxylic acid,
or a pharmaceutically acceptable salt thereof.

24 more elements

Dependencies are inferred from the claim text.

Facts

Application: 13/994,543Filed 16 Dec 2011
Priority: 17 Dec 2010
Published: 3 Oct 2013
Term ends: Not estimatedThe source records don’t support an estimate.

Classification24 codes

C07D 401/04
Containing two hetero rings: directly linked by a ring-member-to-ring-member bond
A61P 1/16
Drugs for disorders of the alimentary tract or the digestive system: for liver or gallbladder disorders, e.g. hepatoprotective agents,…
A61P 3/00
Drugs for disorders of the metabolism
A61P 3/04
Drugs for disorders of the metabolism: anorexiants; Antiobesity agents