Sankyo Company, Limited

Mitsuru Kataoka

Yasuhiro Morisawa

Hiroyuki Koike

Noritoshi Kitano

Toshiaki Matsuzawa

Yasuteru Iijima

Yuichiro Yabe

Kiyoshi Konishi

Tatsuo Kokubu

Kunio Hiwada

Hidekuni Takahagi

Fujio Saito

Tomihisa Yokoyama

Masaharu Fukami

Takeshi Oshima

Sadao Ishihara

Shinsaku Kobayashi

Hiroshi Mizuno

Mitsuo Sugiyama

Shigeki Miyake

Seiji Kumakura

Toshiaki Mastuzawa

Hitoshi Nagahori

Yasuo Simoji

Nitroxyalkylamide derivatives

Oligopeptides of formula (I): ##STR1## where R.sup.1 -R.sup.5 are various organic groups, and A represents a group of formula --NH-- or --(CH.sub.2).sub.n --, in which n represents an integer of from 1 to 3, have renin-inhibitory activity and are particularly suitable for oral administration. They may be prepared by condensing their component amino acids or lower oligopeptides using conventional peptide synthesis reactions.

New renin-inhibitory oligopeptides, their preparation and their use

Compounds of formula (I): ##STR1## [in which: R.sup.1 is heterocyclic group having 5 or 6 ring atoms, or --NR.sup.7 R.sup.8, where R.sup.7 is alkyl and R.sup.8 is optionally substituted phenyl, optionally substituted phenylalkyl or cycloalkyl; R.sup.2 is optionally substituted phenyl or naphthyl; R.sup.3 is thiazolyl; R.sup.4 is cyclohexyl or isopropyl; R.sup.5 is alkyl; and R.sup.6 is alkyl] and salts thereof have renin-inhibitory and, hence, hypotensive activities and are of value in the diagnosis and treatment of hypertension induced by failures in the renin-angiotensin system. They may be prepared by reacting together appropriate amino acids or derivatives thereof.

Peptides having renin inhibitory activity, their preparation and use

Compounds of formula (I): ##STR1## A is a carbon-carbon bond or C.sub.1 -C.sub.3 alkylene; B is imino group or C.sub.1 -C.sub.2 alkylene; R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, heterocyclic or optionally substituted amino; R.sup.2 is optionally substituted phenyl or optionally substituted naphthyl; R.sup.3 is thiazolyl, isoxazolyl or imidazolyl; R.sup.4 is isopropyl or cyclohexyl; R.sup.5 and R.sup.6 are C.sub.1 -C.sub.4 alkyl, or, together with the carbon atom to which they are attached, C.sub.3 -C.sub.7 cycloalkyl; R.sup.7 is hydrogen, optionally substituted C.sub.1 -C.sub.6 alkyl group; and R.sup.8 is hydrogen or C.sub.1 -C.sub.4 alkyl. These compounds have renin-inhibitory and, hence, hypotensive activities. The invention also provides a method for the treatment or prophylaxis of hypertension induced by failures in the renin-angiotensin system.

Renin-inhibitory oligopeptides, their preparation and use

Pharmaceutical compositions and methods for treatment of eye disorders employ ocular hypotensive compounds of the formula (I) ##STR1## wherein R.sup.1 is selected from hydrogen, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy; each R.sup.2 is selected from hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro or carboxy; R.sup.3 is selected from amino, mono-substituted amino, and di-substituted amino; A and B each represents C.sub.1 -C.sub.6 alkylene, X represents --NH-- or --CH.sub.2 -- and n is 1, 2 or 3; and pharmaceutically acceptable salts or esters thereof.

Ocular hypotensive agents

Pharmaceutical compositions and methods for treatment of eye disorders employ ocular hypotensive compounds of the formula (I); ##STR1## (wherein: R.sup.1 is selected from hydrogen, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy;

Occular hypotensive agents

Compounds of formula (I): ##STR1## (wherein Q is oxygen or sulfur, the dotted line is a single or double bond, A is alkylene, and R.sup.1 -R.sup.5 are a variety of atoms or organic groups) have excellent ability to potentiate myocardial contractivity and a variety of other properties, and can be used to treat cardiac disorders.

Pyridazinone derivatives, their preparation and use

Compounds of formula (I): ##STR1## (in which: R.sup.1 is hydrogen or alkl; R.sup.2 is a variety of groups or atoms; R.sup.3 is optionally substituted hydroxy or --(NH).sub.n --NR.sup.5 R.sup.6, wherein R.sup.5 and R.sup.6 are a variety of groups or atoms, preferably alkyl substituted by heterocyclic, and n is 0 or 1; Q is oxygen or sulfur; and A is a C.sub.1 -C.sub.6 alkylene group) have valuable cardiotionic activity and may be used for the treatment of cardiac disorders. They may be prepared from corresponding compounds containing a benzene ring with a group --QH at the 1-position and a group --CO--CHR.sup.1 --NH--COOR.sup.7 at the 4-position by ring closure and introduction of the group of formula --A--CO--R.sup.3 in any order.

1,2,4-triazinone derivatives, their preparation and use

1,1,2-Triiodo-1-propene and 1-bromo-1,2-diiodo-1-propene derivatives having a formyloxy, alkanoyloxy, alkoxycarbonyloxy, alkoxycarbonylalkoxy, phenoxycarbonylalkoxy or benzyloxycarbonylalkoxy group at the 3-position are valuable anti-fungal and preservative agents having good heat and light stability.

Trihaloallyl derivatives having anti-fungal activities

A variety of organic materials susceptible to fungal attack (especially wood and wood-based materials) can be protected from such attack and fungi growing on such materials can be eradicated by treating them, e.g. by applying to the surfaces or impregnating, with one or more compounds of formula (I): ##STR1## (wherein X represents a halogen atom and R represents a hydroxy group, an alkoxy gorup, a substituted or unsubstituted phenoxy group, an amino group, a mono- or di- alkylamino group, a phenylamino or benzylamino group which is unsubstituted or has one or two substituents on the benzene ring of the phenyl or benzyl moiety, or a 3-halo-2,3-diiodoallyloxy group). An anti-fungal composition contains one or more of these compounds in admixture with a carrier or adjuvant.

Method of preserving organic materials from fungal attack and a

Iodopropargyl derivatives, their use and preparation

Pyridine derivatives having the formula ##STR1## wherein R.sub.1 is an alkyl group having 1 to 3 carbon atoms; R.sub.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms; R.sub.3 is hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 3 or 4 carbon atoms, an alkyl group having 1 or 2 carbon atoms and hydroxy as a substituent, an alkanoyl group having 1 to 18 carbon atoms, an alkenoyl group having 3 to 11 carbon atoms, an aromatic acyl group having 6 or 10 carbon atoms in the aromatic ring and optionally alkyl, alkoxy, acetylamino, cyano or halogen as a substituent, a heterocyclic acyl group, an alkylcarbamoyl group having 1 to 4 carbon atoms in the alkyl moiety, an allylcarbamoyl group or hydroxy group; n is an integer of 0 to 2 inclusive; and, when n is 2, R.sub.1 's may be the same or different; provided that when R.sub.2 is said alkyl group having 1 to 3 carbon atoms, R.sub.3 is said alkyl group having 1 to 4 carbon atoms. They are highly effective in the treatment of coccidiosis.

Pyridine derivatives and their use as anticoccidial agents

Pyridine derivatives having the formula ##STR1## wherein R.sub.1 represents hydrogen atom, amino group or a group ##STR2## in which R.sub.5 and R.sub.6 may be the same or different and each represents an alkyl group of 1 to 4 carbon atoms or R.sub.5 is hydrogen atom and R.sub.6 represents an alkyl group of 1 to 4 carbon atoms, an alkenyl group of 3 or 4 carbon atoms or a benzyl group optionally substituted with halogen, cyano, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms;

Pyridine sulfonamides and their use as anticoccidial agents

Anticoccidial compositions which comprise as active ingredient pyridine derivatives having the formula ##STR1## wherein R.sub.1 is hydrogen atom, a halomethyl group or methyl group;

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Tokyo, Japan

Mitsuru Kataoka