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US 5,334,716 AGranted
Heterocyclic derivatives
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsSatoshi Okada, Kozo Sawada, Akio Kuroda, Shinya Watanabe, Hirokazu Tanaka
Life of this patent
Estimating the term…
Abstract
This invention relates to heterocyclic derivatives useful for treating or preventing testosteron 5.alpha.-reductase mediated diseases such as alopecia, ache, prostatism and the like, which can be represented by the following formula: ##STR1## to a process for their production, to a pharmaceutical composition containing the same and to uses thereof.
Claims12
A compound of the formula:
- ##STR15## wherein R.sup.1 is carboxy or pharmaceutically acceptable protected carboxy,
- R.sup.3 is phenyl substituted by lower alkyl, mono- or di- or triphenyl(lower)alkyl which may be substituted by one to four substituents selected from the group consisting of lower alkyl, halogen, cyano, carboxy, mono- or di- or triphenyl(lower)alkoxycarbonyl, mono- or di(lower)alkylcarbamoyl, phenylcarbamoyl, lower alkylphenylcarbamoyl, lower alkoxy, hydroxy(lower)alkyl, lower alkanoyloxy(lower)-alkyl, cyclo(lower)alkyl(lower)alkyl, lower alkenyl and lower alkynyl, lower alkylcarbamoyl(lower)alkyl, or lower alkylphenylcarbamoyl(lower)alkyl,
- R.sup.11 is hydrogen or lower alkyl,
- A is lower alkylene which may be substituted by oxo, or lower alkenylene,
- Q is carbonyl or lower alkylene, ##STR16## in which R.sup.4 is hydrogen or lower alkyl, and R.sup.5 is hydrogen, lower alkyl or Y--Z--R.sup.3,
- Y is bond or lower alkylene,
- Z is lower alkylene, lower alkenylene, ##STR17## in which R.sup.6 is hydrogen, lower alkyl, mono- or di- or triphenyl(lower)alkyl which may be substituted by lower alkyl, or lower alkoxycarbonyl,
- and pharmaceutically acceptable salts thereof.
5 more elements
A compound of the formula:
- ##STR22## wherein R.sup.1 is carboxy or pharmaceutically acceptable protected carboxy,
- R.sup.2 is hydrogen, lower alkyl or halogen,
- R.sup.3 is aryl or ar(lower)alkyl, each of which may have suitable substituent(s) selected from the group consisting of lower alkyl, halogen, cyano, carboxy, pharmaceutically acceptable esterified carboxy, pharmaceutically acceptable amidated carboxy, lower alkoxy, hydroxy(lower)alkyl, pharmaceutically acceptable protected hydroxy(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, lower alkenyl and lower alkynyl, carbamoyl (lower)alkyl, in which the carbamoyl moiety is substituted by suitable substituents, selected from the group consisting of lower alkyl and lower alkylaryl,
- R.sup.11 is hydrogen or lower alkyl,
- A is lower alkylene which may be substituted by oxo, or lower alkenylene,
- Q is carbonyl or lower alkylene, ##STR23## in which R.sup.4 is hydrogen or lower alkyl, and
- R.sup.5 is hydrogen, lower alkyl or Y--Z--R.sup.3,
- Y is bond or lower alkylene,
- Z is lower alkylene, lower alkenylene, ##STR24## in which R.sup.6 is hydrogen, lower alkyl, ar(lower)alkyl which may have suitable substituent(s) selected from the group consisting of lower alkyl, halogen, cyano, carboxy, pharmaceutically acceptable esterified carboxy, pharmaceutically acceptable amidated carboxy, lower alkoxy, hydroxy(lower)alkyl, pharmaceutically acceptable protected hydroxy(lower)alkyl, cyclo(lower)alkyl-(lower)alkyl, lower alkenyl and lower alkynyl, or
- a pharmaceutically acceptable amino protective group,
- and pharmaceutically acceptable salts thereof.
8 more elements
Dependencies are inferred from the claim text.