Banyu Pharmaceutical Co. Ltd

Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai

Tetsuji Miyano

Kunio Suzuki

Susumu Nakagawa

Ryosuke Ushijima

Nobuo Harada

Hamao Umezawa

Takaaki Aoyagi

Hiroshi Fukatsu

Kohtaro Funaishi

A process for preparing a 2-carbamoylocxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:

Process for preparing 2-carbamoyloxyalkyl-1,4-dihydropyridine derivatives

A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:

Certain intermediate 3-carbamoyloxyalkyl propiolic acid derivatives

3-amino-3-carbamoyloxyalkylacrylic acid intermediates to dihydropyridines

Novel compounds having vasodilation and hypotensive effects are represented by the formula ##STR1## where R.sup.1 is halogen, nitro, cyano or lower alkoxy; each of R.sup.2 and R.sup.3 is lower alkyl, lower haloalkyl, lower alkoxyalkyl, aralkyloxyalkyl, aryloxyalkyl, lower alkenoxyalkyl, N,N-di-lower alkylaminoalkyl, N-lower alkyl-N-aralkylaminoalkyl, piperidylalkyl, 4-lower alkyl piperazinylalkyl, norpholinoalkyl or 1-pyrrolidinylalkyl; R.sup.4 is lower alkyl; A is lower alkylene; and R.sup.5 is hydrogen, lower alkyl, cycloalkyl of 3 to 7 carbon atoms, or aryl unsubstituted or substituted by one or two substituents selected from halogen, nitro, lower alkyl, lower alkoxy, di-lower alkylamino and cyano. Also disclosed are processes for their preparation.

2-Substituted or unsubstituted aminocarbonyloxyalkyl-1,4-dihydropyridines

A process for producing new pepstatins having anti-pepsin activity by cultivating a pepstatin producing strain in a nutrient medium containing assimilable carbon sources and nitrogen sources, and extracting the new pepstatins from the cultivated broth or medium.

Process for the production of new pepstatins having anti-pepsin activity

Halo-fusaric acid amides having the formula ##SPC1## Wherein X represents halogen or hydrogen, Y represents halogen and R.sub.1 and R.sub.2 are same or different and represent hydrogen or a lower alkyl group (C.sub.1-4) which are characterized by significant activity in the treatment of hypertension.

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Nagoya, Japan

Tetsuji Miyano