Benzenesulfonamide derivatives

Details Benzenesulfonamide derivatives Benzenesulfonamide derivatives

1994-06-30

1996-06-04

Bernhardt, Emily

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

544 59, 544161, 544383, 546159, 546171, 546223, 546239, 546240, 548193, 548194, 548542, 564 88, 564 89, 562833, C07D21158, C07D29526, C07D29528, C07C31129

Patent

active

055234640

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/JP92/01429 filed Nov. 5, 1992.


TECHNICAL FIELD

The present invention relates to benzenesulfonamide derivatives which are useful as therapeutic agents for osteoporosis.


BACKGROUND ART

J. Amer. Chem. Soc., 112, 7861 (1990) discloses compounds represented by Formula (A) ##STR2## wherein R.sup.c represents sulfonanilide. Further, EP 395093 discloses that compounds represented by Formula (A) wherein R.sup.c represents carbamoyl etc. are useful as therapeutic agents for osteoporosis.


DISCLOSURE OF THE INVENTION

According to the present invention, there can be provided benzenesulfonamide derivatives represented by Formula (I): ##STR3## in which R.sup.1 and R.sup.2 independently represent hydrogen or lower alkanoyl; and R.sup.3 and R.sup.4 independently represent hydrogen, lower alkyl, cycloalkyl, substituted or unsubstituted polycycloalkyl, substituted aryl, or a substituted or unsubstituted heterocyclic group, or R.sup.3 and R.sup.4 are combined together with the adjacent nitrogen atom to form a substituted or unsubstituted aliphatic heterocyclic group [hereinafter referred to as Compound (I); the same applies to the compounds of other formula numbers], or pharmaceutically acceptable salts thereof.
In the definitions of the groups in Formula (I), the lower alkyl means a straight-chain or branched alkyl group having 1 to 8 carbon atoms such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, neopentyl, hexyl, heptyl, and octyl. The lower alkanoyl means a straight-chain or branched alkanoyl group having 1 to 5 carbon atoms such as formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, and pivaloyl. The cycloalkyl means a cycloalkyl group having 3 to 8 carbon atoms such as cyclopropyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl. The polycycloalkyl means a saturated hydrocarbon group having (a) bridge(s) which is selected from the group consisting of compounds represented by the formula ##STR4## (in which Q.sup.1 represents hydrogen or lower alkyl; m represents 0 or 1; and n represents an integer of 0 to 5) such as tricyclo[3.3.1.1.sup.3,7 ]decyl and tricyclo[3.3.1.0.sup.3,7 ]-nonyl, and compounds represented by the formula ##STR5## (in which n has the same meaning as defined above) such as bicyclo[2.2.1]heptyl. The lower alkyl in the definition of Q.sup.1 has the same meaning as the above-defined lower alkyl.
The aryl means phenyl or naphthyl. The substituted aryl has 1 to 3 independently-selected substituents. The substituent includes, for example, lower alkyl, hydroxy, lower alkoxy, lower alkylthio, halogen, nitro, amino, lower alkanoyl, aroyl, carboxy, and lower alkoxycarbonyl. The alkyl moiety of the lower alkyl, the lower alkoxy, the lower alkylthio, and the lower alkoxycarbonyl has the same meaning as the above-defined lower alkyl. The lower alkanoyl and the aryl moiety of the aroyl have the same meanings as the above-defined lower alkanoyl and aryl, respectively. The halogen means fluorine, chlorine, bromine, and iodine atoms.
The heterocyclic group means an aromatic heterocyclic group such as pyridyl, quinolyl, and thiazolyl, or an aliphatic heterocyclic group such as pyrrolidinyl, piperidyl, piperidino, piperazinyl, morpholino, and thiomorpholino. The aliphatic heterocyclic group which is formed by combining R.sup.3 and R.sup.4 together with the adjacent nitrogen atom has the same meaning as the above-defined aliphatic heterocyclic group. The substituted heterocyclic group has 1 to 2 independently-selected substituents. The substituent includes, for example, lower alkyl, lower alkoxy, halogen, benzyl, and substituted or unsubstituted phenyl. The lower alkyl, the lower alkoxy, and the halogen have the same meanings as described above. The substituents of the substituted phenyl has the same meaning as the above-defined substituents for the aryl.
Examples of the pharmaceutically acceptable salts of Compounds (I) are acid addition salts with hydrochloric acid, hydrobromic acid, hydroiodic acid, nitric acid, phosphoric acid,

REFERENCES:
patent: 4879315 (1989-11-01), Magarian et al.
J. Am. Chem. Soc., vol. 12, No. 22 (1990) pp. 7861-7868.

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