Carbamoyl-type benzofuran derivatives
AssigneeMitsubishi Tanabe Pharma Corporation
InventorsTakayuki Kawaguchi, Hidenori Akatsuka, Masamichi Morimoto, Tatsuya Watanabe, Toru Iijima, Jun Murakami
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Abstract
The present invention provides a carbamoyl-type benzofuran derivative of the formula [1]: wherein Ring Z is a group of the formula: etc.; A is a single bond, and the like; Y is a cycloalkanediyl group, etc.; R4 and R5 are the same or different and each is an optionally substituted lower alkyl group, etc.; R1 is a halogen atom, etc.; Ring B of the formula: is an optionally substituted benzene ring; and R3 is a hydrogen atom. etc., or a pharmaceutically acceptable salt thereof, which is useful as an FXa inhibitor.
Claims19
A carbamoyl-type benzofuran derivative of the formula [1]:
- wherein Ring Z is a group of the formula:
- A is a single bond or a group of the formula:
- —NH—;
- Y is a lower alkylene group, a cycloalkanediyl group, a phenyl group or a saturated heterocyclic group;
- R4 and R5 are the same or different and each is a hydrogen atom, an optionally substituted lower alkyl group or an optionally substituted saturated heterocyclic group, or R4 and R5 combine together at the ends to form an optionally substituted nitrogen-containing saturated heterocyclic group along with the adjacent nitrogen atom;
- R1 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a cyano group, or an amino group optionally substituted by 1 to 2 lower alkyl groups;
- Ring B of the formula:
- is an optionally substituted benzene ring;
- and
- R3 is a hydrogen atom or a lower alkyl group,
- or a pharmaceutically acceptable salt thereof.
A compound of the formula:
- wherein X is a group of the formula:
- —N═ or —CH═;
- A is a single bond or a group of the formula:
- —NH—;
- Y is a lower alkylene group, a cycloalkanediyl group, a phenyl group or a saturated heterocyclic group;
- R6 is a protecting group for carboxyl group;
- R1 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a cyano group, or an amino group optionally substituted by 1 to 2 lower alkyl groups;
- Ring B of the formula:
- is an optionally substituted benzene ring;
- and
- R3 is a hydrogen atom or a lower alkyl group.
A compound of the formula:
- wherein X is a group of the formula:
- —N═ or —CH═;
- A is a single bond or a group of the formula:
- —NH—;
- Y is a lower alkylene group, a cycloalkanediyl group, a phenyl group or a saturated heterocyclic group;
- R1 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a cyano group, or an amino group optionally substituted by 1 to 2 lower alkyl groups;
- Ring B of the formula:
- is an optionally substituted benzene ring;
- and R3 is a hydrogen atom or a lower alkyl group.
Methyl 2-{[(5 -chloropyridin-2-yl)amino]carbonyl}-3-[({trans-4-[(dimethylamino)carbonyl]cyclohexyl}carbonyl)amino]benzofuran-5-carboxylate;
- Methyl [2- {[(5-chloropyridin-2-yl)amino]carbonyl}-3-({[trans-4-(pyrrolidin- 1-ylcarbonyl)cyclohexyl]carbonyl}amino)benzofuran-5-yl]acetate;
- N2-(5-Chloropyridin-2-yl)-N5,N5-dimethyl-3 -({[trans-4-(morpholin-4-ylcarbonyl)cyclohexyl]carbonyl}amino)-benzofuran-2,5-dicarboxamide;
- N-(5-Chloropyridin-2-yl)-3-[(5-morpholin-4-yl -5-oxopentanoyl)amino]benzofuran-2-carboxamide;
- 2- {[(5-Chloropyridin-2-yl)amino]carbonyl}-3-[({trans-4-[(dimethylamino)carbonyl]cyclohexyl}carbonyl)amino]-benzofuran-5-carboxylic acid;
- N2-(5-Chloropyridin-2-yl)-3-[({trans-4-[(dimethylamino)carbonyl]cyclohexyl}carbonyl)amino]-N5,N5-dimethylbenzofuran-2,5-dicarboxamide;
- trans-N′-[2-{[(5-Chloropyridin-2-yl)amino]carbonyl}-5-morpholin-4-ylcarbonyl)benzofuran-3-yl]-N,N-dimethylcyclohexane- 1,4-dicarboxamide, or
- a pharmaceutically acceptable-salt thereof.
Dependencies are inferred from the claim text.