US 2003/0153579 A1Published application

Carboxylic acid derivative and a pharmaceutical composition containing the derivative as active ingredient

AssigneeOno Pharmaceutical Co., Ltd.

InventorsHisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima

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Abstract

A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) 1 (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.

Claims8

Dependent claims

A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I)

967
(wherein A1 is C1˜4 alkylene or C2˜4 alkenylene,
A2 is —O— or —S—,
A3 is CH or N,
n is 1˜5,
R1 is
(i) hydrogen,
(ii) C1˜8 alkyl,
(iii) halogen,
(iv) C1˜4 alkoxy,
(v) nitro,
(vi) trihalomethyl,
(vii) trihalomethoxy,
(viii) trihalomethylthio,
(ix) cyano,
(x) C1˜4 alkylthio,
(xi) NR5R6 (wherein R5 and R6 are each independently, hydrogen or C1˜4 alkyl),
(xii) carbocyclic ring or
(xiii) hetero ring,
R1 is
(i) hydrogen,
(ii) C1˜4 alkyl,
(iii) halogen or
(iv) trihalomethyl,
Cyc1 is
968
Cyc2 is
(i) carbocyclic ring or
(ii) hetero ring,
R3 is
(i) hydrogen,
(ii) C1˜8 alkyl,
(iii) halogen,
(iv) C1˜4 alkoxy,
(v) nitro,
(vi) trihalomethyl,
(vii) trihalomethoxy,
(viii) trihalomethylthio,
(ix) cyano or
(x) C1˜4 alkylthio,
R1 is
969
or
(ii) 2,4-thiazolidindion-5-yl,
A4 is
(i) bond,
(ii) C1˜4 alkylene,
(iii) —C1˜4 alkylene-O— or
(iv) —C1˜4 alkylene-S—,
R7, R8 and R9 are each independently hydrogen or C1˜4 alkyl, with the proviso that
(1) R4 is attached to 2- or 3-position and
(2) when R4 is attached to 3-position, A4 is bond or methylene, A3 is CH and Cyc1 is benzene, then A1 is methylene, ethylene or vinylene.), its non-toxic salt or hydrate thereof as active ingredient.

49 more elements

A carboxylic acid derivative of formula (I)

970
(wherein A1 is C1˜4 alkylene or C2˜4 alkenylene,
A2 is —O— or —S—,
A3 is CH or N,
n is 1˜5,
R1 is
(i) hydrogen,
(ii) C1˜8 alkyl,
(iii) halogen,
(iv) C1˜4 alkoxy,
(v) nitro,
(vi) trihalomethyl,
(vii) trihalomethoxy,
(viii) trihalomethylthio,
(ix) cyano,
(x) C1˜4 alkylthio,
(xi) NR5R6 (wherein R5 and R6 are each independently hydrogen or C1˜4 alkyl),
(xii) carbocyclic ring or
(xiii) hetero ring,
R2 is
(i) hydrogen,
(ii) C1˜4 alkyl,
(iii) halogen or
(iv) trihalomethyl,
Cyc1 is
971
Cyc2 is
(i) a carbocyclic ring or
(ii) a hetero ring,
R3 is
(i) hydrogen,
(ii) C1˜8 alkyl,
(iii) halogen,
(iv) C1˜4 alkoxy,
(v) nitro,
(vi) trihalomethyl,
(vii) trihalomethoxy,
(viii) trihalomethylthio,
(ix) cyano or
(x) C1˜4 alkylthio,
R4 is
972
or
(ii) 2,4-thiazolidindion-5-yl,
A4 is
(i) a bond,
(ii) C1˜4 alkylene,
(iii) —C1˜4 alkylene-o— or
(iv) —C1˜4 alkylene-S—,
R7, R1 and R9 are each independently hydrogen or C1˜4 alkyl, with the proviso that
(1) R4 is attached to 2- or 3-position and
(2) when R4 is attached to 3-position, A4 is a bond or methylene, A3 is CH and Cyc1 is benzene, A1 is methylene, ethylnene or vinylene.).

49 more elements

Dependencies are inferred from the claim text.

Facts

Application: 10/251,805Filed 23 Sep 2002
Priority: JP 10-05844410 Mar 1998
Published: 14 Aug 2003
Term ends: Not estimatedThe source records don’t support an estimate.

Classification19 codes

C07D 213/30
Radicals substituted by singly-bound oxygen or sulphur atoms: oxygen atoms
A61K 31/00
Medicinal preparations containing organic active ingredients
C07C 59/66
Containing six-membered aromatic rings: the non-carboxylic part of the ether containing six-membered aromatic rings
C07C 59/68
The non-carboxylic part of the ether containing six-membered aromatic rings: the oxygen atom of the ether group being bound to a non-condensed…

Family

Application09/623,913Division · filed 11 Sep 2000
Application10/251,805Division · filed 23 Sep 2002
US 6,506,757 B1Related patent
US 7,037,914 B2Related patent
US 2003/0153579 A1This patent

From the US filing history. Foreign family members aren’t listed.