Mitsui Toatsu Kagaku Kabushiki Kaisha

Mitsui Toatsu Chemicals, Incorporated

Mitsui Petrochemical Industries, Ltd.

Takashi Nishina

Nobuyuki Fukazawa

Hajime Iizuka

Takuo Nakano

Tsutomu Katakami

Joji Kamiya

Yasuhito Tanaka

Akira Awaya

Keiichi Yokoyama

Mikio Kumakura

Takumi Kitahara

Hiroyasu Ohno

Koji Kato

Kazuyuki Watanabe

Isao Shirakawa

Sakae Saruta

This invention relates to pyridazinone derivatives of the general formula: ##STR1## [wherein R.sup.1 stands for a hydrogen atom or a lower alkyl group; R.sup.2 for a hydrogen atom or a lower alkyl group; and A for (i) a ring selected from a benzene ring, a furan ring, a thiophene ring and a pyridine ring (on which ring 1-3 substituents or atoms selected from amino groups, nitro groups, lower alkanoylamino groups, hydroxyl groups, lower alkanoyloxy groups, sulfamoyl groups and halogen atoms may be present), or (ii) a grouping of the formula: ##STR2## (wherein R.sup.3 stands for a hydrogen atom, a lower alkyl group, a phenyl(lower)alkyl, a hydroxyphenyl(lower)alkyl group, a lower alkylmercapto(lower)alkyl group, a benzylmercapto(lower)alkyl group, a guanidino(lower)alkyl group, a nitroguanidino(lower)alkyl group, an indolyl(lower)alkyl group, a carbamoyl(lower)alkyl group or a carboxy(lower)alkyl group, R.sup.4 for a hydrogen atom or a lower alkyl group, R.sup.5 for a hydrogen atom, a lower alkyl group, a lower alkanoyl group, a benzoyl or a benzyloxycarbonyl group, and R.sup.3 and R.sup.4 may be combined to form a grouping of the formula: ##STR3## which forms a ring), or (iii) a grouping of the formula: ##STR4## (wherein R.sup.6, R.sup.7 and R.sup.8 each stand for a hydrogen atom or a lower alkyl group, B is an oxygen atom or a sulfur atom, R.sup.9 stands for a hydrogen atom or a lower alkanoyl group, and n is 0 or 1)].

6-acylaminophenyl-5-alkyl-4,5-dihydro-3(2H)-pyridazinone compounds

Disclosed herein is an antihypertensive preparation containing, as an active component, a novel quinazoline derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sup.100 means a hydrogen atom or methoxy group, R.sup.200 and R.sup.300 denote individually a hydrogen atom or lower alkoxy group, R.sup.400 is a hydrogen atom or amino group, l stands for 2 or 3, and Het is a specific hetero ring group.

Quinazoline compounds and antihypertensives

Pyridazinone derivatives

This invention relates to benzothiazepine derivatives of the general formula ##STR1## where K is hydrogen or a --CH.sub.2 COOR.sub.2 group where R.sub.2 is hydrogen or a lower alkyl group, Z is hydrogen or phenyl except when both K and Z are hydrogen, and Y is hydrogen, a --CHR.sub.3 --COOR.sub.1 group, an alkanoyl group or a --COO(CH.sub.2).sub.n R.sub.4 group where R.sub.1 is hydrogen or a lower alkyl group, R.sub.3 is hydrogen, an alkyl group, an alkylphenyl group or an aryl-lower alkyl group, R.sub.4 is an aryl group and n is a whole number of 1 to 10, and to their methods of preparation. The benzothiazepine derivatives of this invention, including their salts, have a powerful inhibitory effect on the angiotensin converting enzyme and exert a marked depressor effect in such models of hypertension as spontaneously occurring hypertensive rats and the like, so that they are useful as drugs for the treatment of hypertension and other cardiovascular diseases. In addition, these compounds are also useful as intermediates for the synthesis of coronary dilators, psychotropic drugs and the like.

Benzothiazepine derivatives and their methods of preparation

6-(Substituted phenyl)-4,5-dihydro-3(2H)-pyridazinone compounds possessing strong platelet aggregation inhibiting activity and blood pressure depressing activity, having the general formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2 is hydrogen, lower alkyl, lower alkylthio or the grouping R.sup.5 --NH-- where R.sup.5 is lower alkyl; R.sup.3 is phenyl, pyridyl, benzyl, lower alkyl or a substituted phenyl group carrying at any desired position on the benzene ring thereof the grouping: ##STR2## where R.sup.1 has the same meaning as given above; R.sup.4 is hydrogen or halogen; n is 0 or 1; and when both R.sup.2 and R.sup.3 are lower alkyl groups, R.sup.2 and R.sup.3 may be combined together with the bridging member ##STR3## between them to form the structure: ##STR4## where m is 2 or 3, as well as physiologically acceptable acid-addition salts thereof, and processes for preparing them.

Process for preparing 6-(substituted

6-(Substituted phenyl)-4,5-dihydro-3(2H)-pyridazinone compounds possessing strong platelet aggregation inhibiting activity and blood pressure depressing activity, having the general formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2 is hydrogen, lower alkyl, lower alkylthio or the grouping R.sup.5 --NH-- where R.sup.5 is lower alkyl; R.sup.3 is phenyl, pyridyl, benzyl, lower alkyl or a substituted phenyl group carrying at any desired position on the benzene ring thereof the grouping: ##STR2## where R.sup.1 has the same meaning as given above; R.sup.4 is hydrogen or halogen; n is 0 or 1; and when both R.sup.2 and R.sup.3 are lower alkyl groups, R.sup.2 and R.sup.3 may be combined together with the bridging member ##STR3## where m is 2 or 3, as well as physiologically acceptable acid-addition salts thereof, and processes for preparing them.

6-(Substituted phenyl)-4,5-dihydro-3(2H)-pyridazinone compounds

Growing community of inventors

Mobara, Japan

Takashi Nishina