Provided is a heterocyclic derivative showing a thyroid hormone Î² receptor agonist action, which is effective for the prophylaxis or treatment of the diseases relating to the action. A compound represented by the formula [I]: [structure] wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, and a medicament containing the compound as an active ingredient.

Claims

19 · 2 independent · depth 6

19 granted claims

›1.independentA compound represented by the formula:+17

›2.↳ 1The compound according to claim 1, wherein the substituent of the optionally substituted alkyl for A is the same or different 1-3 groups selected from…d2+4

The compound according to claim 1, wherein the substituent of the optionally substituted alkyl for A is the same or different 1-3 groups selected fromnaryl optionally substituted by 1-3 groups selected from alkyl, halogen, alkoxy, alkanoyl, and cyano;a heterocyclic group optionally substituted by 1-3 groups selected from alkyl, halogen, alkoxy, alkanoyl, and cyano;heteroaryl optionally substituted by 1-3 groups selected from alkyl, halogen, alkoxy, alkanoyl, and cyano;cycloalkyl optionally substituted by 1-3 groups selected from alkyl, halogen, alkoxy, alkanoyl, and cyano;hydroxy;alkoxy;halogen;amino group optionally substituted by 1 or 2 alkyl; andoxo,the substituent of the optionally substituted aryl, optionally substituted carbocyclic group, optionally substituted heterocyclic group and optionally substituted heteroaryl group for A is the same or different 1-3 groups selected fromalkyl optionally substituted by hydroxy, alkoxy, cycloalkyl or halogen;alkenyl optionally substituted by alkoxy or cycloalkyl;cycloalkyl optionally substituted by alkyl, alkoxy or cycloalkyl;alkoxy optionally substituted by alkoxy, cycloalkyl or halogen;cycloalkyloxy optionally substituted by alkyl, alkoxy or cycloalkyl;halogen;cyano;hydroxy;oxo;heterocycle;alkylsulfonyl; andmono or dialkylcarbamoyl,the substituent of the optionally substituted amino for A is the same or different 1 or 2 alkyl optionally substituted by alkoxy, cycloalkyl or halogen;alkenyl optionally substituted by alkoxy or cycloalkyl;cycloalkyl optionally substituted by alkyl, alkoxy or cycloalkyl;alkanoyl optionally substituted by alkoxy, cycloalkyl or halogen; oraryl optionally substituted by alkyl, alkoxy or cycloalkyl,the substituent of the optionally substituted carbamoyl for A is the same or different 1 or 2 alkyl optionally substituted by aryl,the substituent of the optionally substituted alkyl for R6 or R7 is alkoxy, hydroxy or halogen, andthe substituent of the optionally substituted methylene for X is alkoxy or hydroxy, or a pharmacologically acceptable salt thereof.

›4.↳ 1The compound according to claim 1, wherein A is an optionally substituted carbocyclic group, or a pharmacologically acceptable salt thereof.d2+1

›5.↳ 1The compound according to claim 1, wherein A is optionally substituted aryl, or a pharmacologically acceptable salt thereof.d2

›7.↳ 1The compound according to claim 1, wherein A is optionally substituted alkyl, or a pharmacologically acceptable salt thereof.d2

›8.↳ 1The compound according to claim 1, wherein A is optionally substituted heterocyclic group, or a pharmacologically acceptable salt thereof.d2

›9.↳ 1The compound according to claim 1, wherein A is optionally substituted heteroaryl, or a pharmacologically acceptable salt thereof.d2

›10.↳ 1The compound according to claim 1, wherein X is methylene, or a pharmacologically acceptable salt thereof.d2

›11.↳ 1The compound according to claim 1, wherein R1 and R2 are the same group, or a pharmacologically acceptable salt thereof.d2

›12.↳ 1The compound according to claim 1, wherein R1 and R2 are the same or different and each is alkyl, or a pharmacologically acceptable salt thereof.d2

›13.↳ 1The compound according to claim 1, wherein R1 and R3 are bonded to form carbocycle or heterocycle, or a pharmacologically acceptable salt thereof.d2

›14.↳ 1The compound according to claim 1, wherein R8 is hydroxy, or a pharmacologically acceptable salt thereof.d2

›16.↳ 1A pharmaceutical composition comprising:nthe compound according to claim 1, or a pharmacologically acceptable salt thereof, as an active ingredient; a…d2

›15.independent(4-{[5-Hydroxy-6-(2-naphthyl)pyridin-2-yl]methyl}-3,5-dimethylphenoxy)acetic acid;n{4-[(6-cyclopentyl-5-hydroxypyridin-2-yl)methyl]-2,3,5-trimethylphe…

(4-{[5-Hydroxy-6-(2-naphthyl)pyridin-2-yl]methyl}-3,5-dimethylphenoxy)acetic acid;n{4-[(6-cyclopentyl-5-hydroxypyridin-2-yl)methyl]-2,3,5-trimethylphenoxy}acetic acid;{4-[(6-cyclohexyl-5-hydroxypyridin-2-yl)methyl]-2,3,5-trimethylphenoxy}acetic acid;{2-bromo-4- [(6-cyclohexyl-5-hydroxypyridin-2-yl)methyl]-3,5-dimethylphenoxy}acetic acid;3-({4-[(5-hydroxy-6-phenylpyridin-2-yl)methyl]-3,5-dimethylphenyl}amino)-3-oxopropanoic acid;3-({4-[(6-cyclohexyl-5-hydroxypyridin-2-yl)methyl]-3,5-dimethylphenyl}amino)-3-oxopropanoic acid;3-[(4-{[5-hydroxy-6-(2-naphthyl)pyridin-2-yl]methyl}-3,5-dimethylphenoxy)methyl]-1,2,4-oxadiazol-5(4H)-one;3-[(4- {[5-hydroxy-6-(5,6,7,8-tetrahydronaphthalen-2-yl)pyridin-2-yl]methyl }-3,5-dimethylphenoxy)methyl]-1,2,4-oxadiazol-5(4H)-one;3-({4-[(6-cycloheptyl-5-hydroxypyridin-2-yl)methyl]-3,5-dimethylphenyl}amino)-3-oxopropanoic acid;N-[2-chloro-4-(6-cyclohexyl-5-hydroxy-pyridin-2-ylmethyl)-3,5-dimethyl-phenyl]amino-3-oxopropanoic acid;3-[(2-fluoro-4-{[6-(2-fluoro-3-methylphenyl)-5-hydroxypyridin-2-yl]methyl}-3,5-dimethylphenoxy)methyl]-1,2,4-oxadiazol-5(4H)-one;{4-[(6-cyclohexyl-4-fluoro-5-hydroxypyridin-2-yl)methyl]-2,3,5-trimethylphenoxy}acetic acid;{4-[(6-cyclohexyl-3-fluoro-5-hydroxypyridin-2-yl)methyl]-2,3,5-trimethylphenoxy}acetic acid;{4-[(6-cycloheptyl-5-hydroxypyridin-2-yl)methyl]-2,3,5-trimethylphenoxy}acetic acid;3-({4-[(6-cycloheptyl-5-hydroxypyridin-2-yl)methyl]-2-fluoro-3,5-dimethylphenyl}amino)-3-oxopropanoic acid;{4-[6-(3-fluoro-phenyl)-5-hydroxy-pyridin-2-ylmethyl]-2,3,5-trimethyl-phenoxy}acetic acid;(4-{[6-(3-chlorophenyl)-5-hydroxypyridin-2-yl]methyl}-2,3,5-trimethylphenoxy)acetic acid;3-{2-fluoro-4-[5-hydroxy-6-(2,3,4-trifluoro-phenyl)-pyridin-2-ylmethyl]-3,5-dimethyl-phenoxymethyl}-1,2,4-oxadiazol-5(4H)-one;3-[(2-fluoro-4-{[5-hydroxy-6-(3-pyrrolidin-1-ylphenyl)pyridin-2-yl]methyl}-3,5-dimethylphenoxy)methyl]-1,2,4-oxadiazol-5(4H)-one;2-{4-[(5-hydroxy-6-phenylpyridin-2-yl)methyl]-3,5-dimethylphenyl}-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile;3-{2-fluoro-4-[5-hydroxy-6-(3-propoxy-phenyl)-pyridin-2-ylmethyl]-3,5-dimethyl-phenoxymethyl}-1,2,4-oxadiazol-5(4H)-one;[3,5-dibromo-2-fluoro-4-(5-hydroxy-6-phenyl-pyridin-2-ylmethyl)-phenoxy]acetic acid;(5-ethyl-4-{[6-(3-fluorophenyl)-5-hydroxypyridin-2-yl]methyl}-2,3-dimethylphenoxy)acetic acid, or a pharmacologically acceptable salt thereof.

Classifications

4 codes

IPC · International Patent Classification

Section A — Human necessities

A61K31/675

Section C — Chemistry; metallurgy

C07D211/72

USPC · US Patent Classification

546/290514/345

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Heidi Reese

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Type	Document	Date
related publication	US 20120129812 A1	24 May 2012

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