S-triazine derivative and remedy for estrogen-dependent disease containing said derivative as effective component
AssigneeZenyaku Kogyo Kabushiki Kaisha
InventorsHideshi Kobayashi, Toshihiko Komatsu, Seiichi Fukuda, Yoshio Tsuchida, Masanobu Kato, Shinichi Yaguchi, Naohito Ogose, Hajime Ono, Yasuhiro Izumisawa, Masayuki Takahashi, Tsutomu Nakagane
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Abstract
s-Triazine (1,3,5-triazine) is chemically modified to obtain s-triazine derivative effective for prevention and treatment of estrogen-dependent diseases.
Claims12
An s-triazine compound having the formula (1) or a pharmaceutically-acceptable acid addition salt thereof:
- ##STR6## wherein:
- (1) when R.sub.1 and R.sub.2 are independent of each other or R.sub.3 and R.sub.4 are independent of each other, or both;
- R.sub.1 and R.sub.3 are each lower alkyl;
- R.sub.2 and R.sub.4 are each lower alkyl or phenyl which is unsubstituted or substituted with halogen, nitro or amino;
- with the proviso that at least one of R.sub.2 or R.sub.4 is phenyl which is unsubstituted or substituted with halogen, nitro or amino;
- (2) when R.sub.1 and R.sub.2 or R.sub.3 and R.sub.4, or both, are, respectively, coupled with an neighboring nitrogen atom to form a cyclic amino group;
- NR.sub.1 R.sub.2 is 1-pyrrolidinyl;
- piperidino which is unsubstituted or substituted with phenyl;
- 1-piperazinyl which is unsubstituted or substituted with lower alkyl or phenyl;
- morpholino;
- or thiomorpholino;
- NR.sub.3 R.sub.4 is 1-aziridinyl which is unsubstituted or substituted with lower alkyl;
- 1-pyrrolidinyl which is unsubstituted or substituted with lower alkoxycarbonyl;
- piperidino which is unsubstituted or mono- or di-substituted with hydroxy, hydroxyl lower alkyl, lower alkoxycarbonyl, lower alkyl, cyano, phenyl or ethylenedioxy;
- 1-piperazinyl which is unsubstituted or substituted with lower alkyl, benzyl, phenyl which is unsubstituted or substituted with halogen, nitro or amino, pyridyl or pyrimidinyl;
- morpholino which is unsubstituted or mono- or di-substituted with lower alkyl;
- 3-thiazolidinyl;
- thiomorpholino;
- 1-imidazolyl which is unsubstituted or mono- or di-substituted with lower alkyl;
- or 1, 2, 4-triazole-1-yl.
A pharmaceutical composition for inhibiting aromatase enzymes, which comprises an effective amount of one or more s-triazine compounds having the formula (I) or a pharmaceutically-acceptable acid addition salt thereof:
- ##STR7## wherein:
- (1) when R.sub.1 and R.sub.2 are independent of each other or R.sub.3 and R.sub.4 are independent of each other, or both;
- R.sub.1 and R.sub.3 are each lower alkyl;
- R.sub.2 and R.sub.4 are each lower alkyl or phenyl which is unsubstituted or substituted with halogen, nitro or amino;
- with the proviso that at least one of R.sub.2 or R.sub.4 is phenyl which is unsubstituted or substituted with halogen, nitro or amino;
- (2) when R.sub.1 and R.sub.2 or R.sub.3 and R.sub.4, or both are, respectively, coupled with an neighboring nitrogen atom to form a cyclic amino group;
- NR.sub.1 R.sub.2 is 1-pyrrolidinyl;
- piperidino which is unsubstituted or substituted with phenyl;
- 1-piperazinyl which is unsubstituted or substituted with lower alkyl or phenyl;
- morpholino;
- or thiomorpholino;
- NR.sub.3 R.sub.4 is 1-aziridinyl which is unsubstituted or substituted with lower alkyl;
- 1-pyrrolidinyl which is unsubstituted or substituted with lower alkoxycarbonyl;
- piperidino which is unsubstituted or mono- or di-substituted with hydroxy, hydroxyl lower alkyl, lower alkoxycarbonyl, lower alkyl, cyano, phenyl or ethylenedioxy;
- 1-piperazinyl which is unsubstituted or substituted with lower alkyl, benzyl, phenyl which is unsubstituted or substituted with halogen, nitro or amino, pyridyl or pyrimidinyl;
- morpholino which is unsubstituted or mono- or di-substituted with lower alkyl;
- 3-thiazolidinyl;
- thiomorpholino;
- 1-imidazolyl which is unsubstituted or mono- or di-substituted with lower alkyl;
- or 1, 2, 4-triazole-1-yl and a pharmaceutically acceptable diluent or carrier.
Dependencies are inferred from the claim text.