Benzofuran derivatives useful as inhibitors of bone resorption

Details Benzofuran derivatives useful as inhibitors of bone resorption Benzofuran derivatives useful as inhibitors of bone resorption

1996-10-25

1999-01-12

Dentz, Bernard

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

514468, 514469, 549220, 549460, 549467, 549468, A61K 3134, C07D30781, C07D30780, C07D30779

Patent

active

058589953

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/JP95/00787 filed Apr. 21, 1995.


TECHNICAL FIELD

The present invention relates to a novel heterocyclic compound and a pharmaceutically acceptable salt thereof which are useful as a medicament.


BACKGROUND ART

In Japanese Patent Application Laid-open No.60-48924, No. 60-54379, etc., there are disclosed thionaphten-2-carboxylic acid derivatives and 3-phenyl-4H-1-benzopyran-4-one derivatives inhibiting bone resorption.


DISCLOSURE OF INVENTION

The present invention relates to a novel heterocyclic compound and a pharmaceutically acceptable salt thereof which are the inhibitors of bone resorption, the inhibitors of bone metastases and useful for the prophylactic and/or therapeutic treatment of bone disease characterized by abnormal bone metabolism such as osteoporosis (especially, postmenopausal osteoporosis); hyper-calcemia; hyperparathyroidism; Paget's bone diseases; osteolysis; hypercalcemia of malignancy with or without bone metastases; rheumatoid arthritis; periodontitis; osteoarthritis; ostealgia; osteopenia; cancer cachexia; or the like in a human being or an animal.
And further, the present invention relates to processes for the preparation of the heterocyclic derivatives, to a pharmaceutical composition comprising the same and to a method for the prophylactic and/or therapeutic treatment of above-mentioned diseases in a human being or an animal, and to a use of the heterocyclic derivatives and pharmaceutically acceptable salts thereof for the prophylactic and/or therapeutic treatment of above-mentioned diseases in human therapeutic treatment of above-mentioned diseases in human being or an animal.
The heterocyclic derivatives of this invention are new and can be represented by the following general formula (I): ##STR2## wherein R.sup.1 is hydrogen, lower alkyl, an acyl group, amino, acylamino, nitro, halogen or hydroxy(lower)alkyl which may have one or more suitable substituent(s), acyl(lower)alkyl, aryl, cyano, mono-(or di- or tri-)-halo (lower)alkyl, lower alkylthio or hydroxy(lower)alkyl which may have one or more suitable substituent(s), cyclo(lower)alkyl(lower)alkyl, halogen, an acyl group, acyl(lower)alkyl, acylamino, acylamino(lower)alkyl, acyl(lower)alkenyl, acyloxy(lower)alkyl, acyl(lower)alkylthio(lower)alkyl, amino(lower)alkyl, mono-(or di-)lower alkylamino, lower alkylthio(lower)alkyl, hydroxyimino(lower)alkyl which may have one or more suitable substituent(s), hydroxy(lower)alkyl which may have one or more suitable substituent(s), hydroxy(lower)alkylthio(lower)alkyl, cyano(lower)alkyl, mono-(or di-)lower alkoxy(lower)alkyl which may have one or more suitable substituent(s), lower alkyl substituted with aryl which may have one or more suitable substituent(s), mono-(or di-)lower alkylamino(lower)alkyl, lower alkyl substituted with heterocyclic group which may have one or more suitable substituent(s), heterocyclic group which may have one or more suitable substituent(s), heterocyclicthio, heterocyclicthio(lower),alkyl, heterocyclicoxy, heterocyclicoxy(lower)alkyl, heterocyclicaminoimino-(lower)alkyl, aryl, amino or nitro, ##STR3## or more suitable substituent(s) or lower alkenylene which may have one or more suitable substituent(s), ##STR4## (wherein R.sup.5 is hydrogen, lower alkyl or an acyl group) and m and n are each integer of 0 or 1.!, ##STR5## (wherein R.sup.6 is lower alkyl), Z is heterocyclic group which may have one or more suitable substituent(s), or aryl which may have one or more suitable substituent(s), pharmaceutically acceptable salt thereof.
The object compound (I) or a salt thereof can be prepared by the processes as illustrated in the following reaction schemes. ##STR6## wherein R.sup.1, R.sup.2, R.sup.3, X, Y, Z , --- and l are each as defined above, ##STR7## R' is hydrogen or lower alkyl, R" is leaving group, heterocyclic group which may have one or more suitable substituent(s), lower alkoxy(lower)alkyl, hydroxy(lower)alkyl, amino, heterocyclic group, carboxy(lower)alkyl, protected carboxy(lower)alkyl, lower alkyl substituted with ar

REFERENCES:
Erlenmeyer et al., Helv. Chim. Acta vol. 31, pp. 75-77, 1948.
Chemical Abstracts, vol. 112: 50495, 1990.
Palidowicz et al., J. Org. Chem., vol. 58, pp. 4802-4804, 1993.

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