Yamanouchi Pharmaceutical Company Ltd.

Other

Takashi Fujikura

Kunihiro Niigata

Toichi Takenaka

Shinichi Hashimoto

Kazuo Imai

Akihiro Tanaka

Ryuji Tsuzuki

Takeyuki Yatsu

Masaki Yokota

Yuzo Matsumoto

Noriki Ito

Masaharu Asano

Kazuo Honda

Tadao Kojima

Masuo Murakami

Kozo Takahashi

Yasuo Isomura

Masaru Iwanami

Shinji Usuda

Kazuharu Tamazawa

Shiro Tachikawa

Kohji Nakano

Ryuichiro Hara

Yoshihisa Nozaki

Masayuki Shibasaki

Masato Ichihara

Soichi Kagami

Yukiko Fukunaga

Yuji Kawashima

Masharu Asano

A compound of the formula (I) or its salt and a process for producing the compounds; The compounds have the effect to dilate neophrovascular tracts; ##STR1## Wherein ##STR2## represents the formula ##STR3## (wherein R.sup.4 is a hydrogen atom or lower alkylsulfonyl); R.sup.1 is hydrogen, lower alkyl, hydroxyl, halogen, amino, or lower acylamino;

Substituted tetrahydroisoquinoline compounds, and process for producing

Pharmaceutical composition of certain dihydropyridine compounds and salts thereof are provided which exhibit both Ca.sup.2+ -antagonistic and adrenergic beta-receptor blocking activities and therefore are useful for the treatment of ischemic heart diseases and hypertension. The pharmaceutical compositions contains either 4-(2-hydroxy-3-phenoxy-propylamino)-butyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate or 6-(2-hydroxy-3-phenoxypropylamino) hexyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate or their pharmaceutically acceptable salts.

Dihydropyridine composition

Pharmaceutical compositions are provided for the treatment of disorders in a subject, such as hypertension, congestive heart failure, angina pectoris, lower urinary tract dysfunction and prostatic hypertrophy. The compositions when administered to a subject produce an .alpha.-adrenergic blocking action and contain as an active ingredient sulfamoyl-substituted phenethylamine derivatives, such as optically active 5-2-[ 2-(2-ethoxyphenoxy)ethylamino] -2-methylethyl-2-methoxybenzenesulfonamide 2-methoxybenzenesulfonamide, and a pharmaceutically acceptable carrier.

Sulfamoyl-substituted phenethylamine derivatives, their preparation, and

Pharmaceutical compositions are provided for the treatment of disorders in a subject, such as hypertension, congestive heart failure, angina pectoris, lower urinary tract dysfunction and prostatic hypertrophy. The compositions when administered to a subject produce an .alpha.-adrenergic blocking action and contain as an active ingredient sulfamoyl-substituted phenethylamine derivatives, such as optically active 5-2-[2-(2-ethoxyphenoxy)ethylamino]-2-methylethyl-2-methoxybenzenesulfonam ide, and a pharmaceutically acceptable carrier.

Sulfamoyl substituted phenethylamine intermediates

This invention provides certain novel substituted tetrahydroisoquinoline opticulisomers of the formula: ##STR1## wherein A represents the formula ##STR2## wherein R is hydrogen or halogen; R.sup.1 is hydrogen, lower alkyl, hydroxyl, halogen, amino, or lower acylamino;

This invention provides the single species (-)-(S)-4-(3,4-dihydroxyphenyl)-7, 8-dihydroxy-1,2,3,4-tetrahydroisoquinoline hydrochloride hydrate, which is useful as a nephrovascular dilator.

Substituted 4,5,6,7-tetrahydrothiens[2,3-C]pyridine compounds

Phenethylamine derivatives shown by the general formula ##STR1## wherein Ro represents a lower alkyl group; R.sub.1 represents a lower alkyl group or a lower alkoxy group; R.sub.2 represents hydrogen atom or a hydroxyl group; R.sub.3 and R.sub.4 each represents hydrogen atom or a lower alkyl group; R.sub.5 represents hydrogen atom or a lower alkoxy group; X represents oxygen atom or a methylene group; m is an integer of 1-3; and n is an integer of 0-2 and the acid addition salts thereof. These compounds exhibit a strong .alpha.-adrenergic blocking action and are useful as an antihypertensive agent.

Phenethylamine derivatives

Dihydropyridine compounds and salts thereof are provided which exhibit both Ca.sup.2+ -antagonistic and adrenergic beta-receptor blocking activities and therefore are useful for the treatment of ischemic heart diseases and hypertension. The compounds have the formula ##STR1## wherein A represents a straight or branched carbon chain alkylene group having 1 to 10 carbon atoms which may be interrupted by an oxygen atom(s); R.sup.1 and R.sup.4, which may be the same or different, each represents a lower alkyl group; R.sup.2 represents an amino group, ##STR2## R.sup.3 represents a straight or branched carbon chain alkyl group having 1 to 10 carbon atoms which may be interrupted by an oxygen atom(s), or ##STR3## R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, a nitro group, a halogen atom, a trifluoromethyl group, a cyano group, a lower alkyl group, a lower alkoxy group or a lower alkenyloxy group; R.sup.7 represents a hydrogen atom, a cyano group, a halogen atom, a lower alkoxy group or a lower alkanoyl group; R.sup.8 and R.sup.9, which may be the same or different, each represents a lower alkyl group or an aralkyl group; and n represents an integer of 1 to 2: these symbols, hereafter, have the same significances.

Dihydropyridine compounds which process both calcium (2+)-antagonistic

A compound of the formula (I) or its salt and a process for producing the compounds. The compounds have the effect of dilating neophrovascular tracts; ##STR1## wherein ##STR2## represents the formula ##STR3## wherein R.sup.4 is a hydrogen atom or lower alkylsulfonyl;

Substituted tetrahydroisoquinoline compounds and method containing them

A compound of the formula (I) or its salt and a process for producing the compounds; The compounds have the effect to dilate neophrovascular tracts; ##STR1## wherein ##STR2## represents the formula ##STR3## (wherein R.sup.4 is a hydrogen atom or lower alkylsulfonyl); R.sup.1 is hydrogen, lower alkyl, hydroxyl, halogen, amino, or lower acylamino;

Production of

Phenethylamine derivatives shown by the general formula ##STR1## wherein Ro represents a lower alkyl group; R.sub.1 represents a lower alkyl group or a lower alkoxy group, R.sub.2 represents hydrogen atom or a hydroxyl group; R.sub.3 and R.sub.4 each represents hydrogen atom or a lower alkyl group; R.sub.5 represents hydrogen atom or a lower alkoxy group; X represents oxygen atom or a methylene group; m is an integer of 1-3; and n is an integer of 0-2 and the acid addition salts thereof. These compounds exhibit a strong .alpha.-adrenergic blocking action and are useful as an antihypertensive agent.

Phenethylamine derivative compositions and use

Novel 1,4-dihydropyridine derivatives and salts thereof are provided, which can be represented by the formula ##STR1## wherein, Y represents an oxygen atom or a sulfur atom; A represents an alkylene group, an alkenylene group or an alkynylene group; and R.sup.7 and R.sup.8 can represent individual groups or may be combined together with a nitrogen atom(s) to form a pyrrole ring, a piperidine ring, a morpholine ring or a piperazine ring or azepine ring which may be substituted with a lower alkyl group or an aralkyl group. Pharmaceutical compositions containing the derivatives and their use for imparting calcium antagonistic activity are also provided.

1,4-dihydropyridine derivatives

Novel sulfamoyl-substituted phenethylamine derivatives which exhibit .alpha.-adrenergic blocking action and are useful as an antihypertensive agent and an agent for the treatment of congestive heart failure.

Use of sulfamoyl-substituted phenethylamine derivatives in treatment of

Novel compounds of the following formula (I) and their salts: A compound of the formula (I) ##STR1## These compounds are expected to be useful for renin inhibitors. Thus, the compounds are useful medical agents, in particular, anti-hypertensive agents.

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Saitama, Japan

Takashi Fujikura