Thiazoline derivatives
AssigneeTaisho Pharmaceutical Co., Ltd.
InventorsMasakazu Sato, Akira Manaka, Keiko Takahashi, Yutaka Kawashima, Katsuo Hatayama
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Abstract
A thiazoline derivative represented by the formula: ##STR1## [wherein R.sup.1 is cyano, carbamoyl, thiocarbamoyl, morpholinothiocarbonyl, alkylthioimidoyl, amidino, substituted amidino or imidazolin-2-yl, R.sup.2 is alkyl or aralkyl, R.sup.3 is hydrogen or alkyl, R.sup.4 is hydroxyl, alkoxy, substituted alkoxy or amino, l is an integer of 1 to 5] and salts thereof have fibrinogen receptor antagonism and cell adhesion factor antagonism, and are useful as therapeutic agents for ischemic diseases and atherosclerosis diseases, and metastasis inhibitory agents of tumors.
Claims1
A thiazoline derivative represented by the formula:
- ##STR70## [wherein R.sup.1 is (i) a cyano group,
- (ii) a carbamoyl group,
- (iii) a thiocarbamoyl group,
- (iv) a morpholinothiocarbonyl group,
- (v) an alkylthioimidoyl group having 2 to 7 carbon atoms,
- (vi) a group represented by the formula:
- ##STR71## (wherein R.sup.11 and R.sup.12 are each a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkoxycarbonyl group having 2 to 7 carbon atoms, a cycloalkyl group having 4 to 8 carbon atoms, a phenyl group, a phenyl group substituted by an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom, an aralkyl group, or an aralkyl group substituted by an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a trifluoromethyl group or a halogen atom),
- (vii) a group represented by the formula:
- ##STR72## (wherein R.sup.21 and R.sup.22 are each a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, m and n are each an integer of 1 to 3, and A is a methylene group, a carbonyl group, an ethylenedioxymethylene group, an oxygen atom, a sulfur atom, a sulfinyl group, a sulfonyl group or a group represented by the formula:
- <NR.sup.23
- (wherein R.sup.23 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a formyl group, an alkanoyl group having 2 to 7 carbon atoms, a phenyl group, a phenyl group substituted by an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, a nitro group, an alkanoyl group having 2 to 7 carbon atoms, a halogen atom or a trifluoromethyl group, a pyridyl group or a benzyl group)), or
- (viii) an imidazolin-2-yl group,
- R.sup.2 is an alkyl group having 1 to 10 carbon atoms or an aralkyl group,
- R.sup.3 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms,
- R.sup.4 is a hydroxyl group, an alkoxy group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms substituted by a phenyl group, a pyridyl group, a morpholino group, an alkanoyloxy group having 2 to 7 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, an N,N-dialkylaminocarbonyl group or an N,N-dialkylamino group, or an amino group, and l is an integer of 1 to 5] and a salt thereof.
Dependencies are inferred from the claim text.