C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/246, 260/266
C07D 295/18 (2006.01) C07D 295/15 (2006.01) C07D 295/192 (2006.01) C07D 403/12 (2006.01) C07D 413/12 (2006.01)
Patent
CA 1201121
ABSTRACT OF THE DISCLOSURE Novel aniline derivative and its salt represented by the general formula (1), Image (1) [wherein R0, R1 and R2 are the same or different and each are a hydrogen atom, a halogen atom, a nitro group, an amino group, a carboxy group, a cyano group, a hydroxy group, a sulfonamido group, a lower alkyl group, a lower alkoxycarbonyl group, a lower alkoxy group, a lower alkanoyl group, a lower alkylamino group, a lower alkylthio group, a lower alkanoylamino group or a group of the formula Image (wherein R5 and R6 are the same or different and each are a hydrogen atom, a lower alkyl group or a cycloalkyl group, or said R5 and R6 may form a 5- or 6-membered saturated heterocyclic group together with the nitrogen atom adjacent thereto, or further with or without a nitrogen atom or an oxygen atom); R3 is a cyano group, a nitro group, a halogen atom, a lower alkyl group or a lower alkoxy group; m is an integer of 1 to 3; R4 is a hydrogen atom or a lower alkyl group; A is a lower alkylene group; provided that when R3 is a lower alkoxy group, a halogen atom or a lower alkyl group; and when R0 is a hydrogen atom and further A is a methylene group, then R1 and R2 are the same or different and should not be hydrogen atoms, halogen atoms, lower alkyl groups or lower alkoxy groups; further when R3 is a lower alkoxy group, a halogen atom or a lower alkyl group, and R° is a halogen atom, a lower alkyl group or a lower alkoxy group and A is a methylene group, then any one of R1 or R2 is a hydrogen atom or another one should not be a halogen atom, a lower alkyl group or a lower alkoxy group.] Aniline derivative and its salt represented by the general formula (1) act directly to the heart, and has myocardial contraction activity (positive inotropic activity) and coronary blood flow increasing activity, and thus it is useful as cardiotonics for curing various heart diseases such as acute left venticular heart failure, cardiogenic shock, low output heart failure sydrome and the like. Specifically, aniline derivative and its salt represented by the general formula (1) of the present invention is characterized as its low toxicities to the heart, thus it has almost no heart beat increasing activity.
402347
Nakagawa Kazuyuki
Ogawa Hidenori
Tominaga Michiaki
Yang Yung-Hsiung
Fetherstonhaugh & Co.
Otsuka Pharmaceutical Co. Ltd.
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