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US 8,785,631 B2Granted
Oxazolone derivative compounds having a 3-oxa-1-azaspiro[4.5] core
AssigneeSeikagaku Corporation
InventorsTsuneo Koji, Hisatomo Kunii, Nobuo Kobayashi
Life of this patent
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Abstract
Novel raw material compounds are provided that are useful for producing novel cycloalkane carboxamide derivatives having cathepsin K inhibitory action. An oxazolone derivative represented by formula (I): [wherein, R1 represents a substituted or unsubstituted alkyl group, substituted or unsubstituted alkenyl group, substituted or unsubstituted alkynyl group, substituted phenyl group, substituted or unsubstituted naphthyl group or substituted or unsubstituted heterocyclic group, and ring A represents a saturated cyclic alkylidene group having 6 to 7 carbon atoms].
Claims2
An oxazolone derivative of formula (I):
- wherein R1 represents an alkyl group of 1 or 2 carbon atoms substituted by a phenyl group, furanyl group, furanylcarbonylamino group or benzoylamino group;
- a cycloalkyl group of 5 or 6 carbon atoms;
- a cyclopentenyl group;
- an alkenyl group of 2 carbon atoms which is substituted by a furanyl group;
- a phenyl group which is substituted by a phenyl group, methoxy group, propylpiperazinyl group, dimethylaminomethyl group, morpholinylmethyl group or thiazolyl group which may be substituted by a methylpiperazinyl group or morpholinylpiperidinyl group;
- a naphthyl group;
- a furanyl group which may be substituted by a methyl group;
- a thienyl group which may be substituted by a methyl group or ethoxy group;
- a pyrrolyl group which may be substituted by a methyl group;
- a pyridinyl group which may be substituted by a hydroxyl group;
- a piperidinyl group which may be substituted by an ethoxycarbonyl group, propoxycarbonyl group or furanylcarbonyl group;
- a pyrazinyl group;
- an isoxazolyl group which may be substituted by a methyl group;
- a benzothiazolyl group;
- a benzodioxolyl group;
- a tetrahydrobenzofuranyl group;
- an indolyl group;
- or a benzothienyl group;
- and
- ring A represents an unsubstituted cyclohexylidene group.
17 more elements
An oxazolone derivative compound selected from the group consisting of:
- 2-(phenylmethyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(2-phenylethyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(4-biphenyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(2-naphthyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(1-naphthyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[(RS)-2,3-tetrahydrobenzofuran-2-yl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(2-furanyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(3-furanyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[2-(2-furanyl)ethenyl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-cyclohexyl-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(6-benzothiazolyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(2-thienyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(1,3-benzodioxol-5-yl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(2-pyridinyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(3-thienyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(3-ethoxy-2-thienyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[2-[(S)-1-phenylethyl]]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(2-pyrazinyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(5-methylisoxazol-4-yl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-cyclopentyl-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(5-methyl-2-thienyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(4-methoxyphenyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(3-methyl-2-thienyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(3-methyl-2-furanyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(3-pyridinyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(1-methyl-1H-pyrrol-2-yl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[(R)-1-phenylethyl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(1H-indol-5-yl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(1-cyclopentenyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(4-pyridinyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(1H-pyrrol-2-yl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(6-hydroxy-2-pyridinyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(2-hydroxy-3-pyridinyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(6-hydroxy-3-pyridinyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[2-(2-furanyl)ethyl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[1-[(2-propoxy)carbonyl]piperidin-4-yl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[1-(ethoxycarbonyl)piperidin-4-yl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[1-(2-furanylcarbonyl)piperidin-4-yl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[[(2-furanylcarbonyl)amino]methyl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[(benzoylamino)methyl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[[4-(1-propyl)piperazin-1-yl]phenyl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-(2-benzothienyl)-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[4-[(dimethylamino)methyl]phenyl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[4-(4-morpholinylmethyl)phenyl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one,
- 2-[4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]phenyl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one and
- 2-[4-[2-[4-(4-morpholinyl)-1-piperidinyl]-4-thiazolyl]phenyl]-3-oxa-1-azaspiro[4.5]dec-1-en-4-one.
43 more elements
Dependencies are inferred from the claim text.