Nippon Chemiphar Co., Ltd.

Naoya Moritoh

Mitsuo Masaki

Haruhiko Shinozaki

Toshiro Kamishiro

Koichi Hashimoto

Masaru Satoh

Toshihiro Takahashi

Hiromitsu Takeda

Mituo Masaki

Novel alkylenediamine derivatives effectively employable glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5 R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.

Alkylenediamine derivatives

Amino-alcohol derivatives of the formula, ##STR1## where R.sub.1 is a straight or branched alkyl group having 3 to 8 carbon atoms, R.sub.2 and R.sub.3 are each a lower alkyl group, or R.sub.2 and R.sub.3 form a 5- to 7-membered ring together with the adjacent nitrogen atom which may have an oxygen atom attached thereto, R.sub.4 is a hydrogen atom or a lower alkyl group, R.sub.5 is a hydrogen atom or a lower alkyl group, X is a hydrogen or halogen atom or a lower alkyl or lower alkoxy group, and n is an integer of 2 or 3, and acid addition salts thereof, are effectively useful as medicines and agricultural chemicals. Processes are also disclosed for preparing such compounds.

Amino-alcohol derivatives and processes for their preparation

Novel alkylenediamine derivatives effectively employable as glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5, R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.

A novel process for the preparation of 2-(10,11-dihydro-10-oxodibenzo[b, f]thiepin-2-yl)propionic acid which shows high anti-inflammatory and analgetic action is disclosed. The process starts from a propiophenone derivative having the formula (II): ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group, which is once converted into a haloacetal compound via a halo-ketone compound, and then converted into the desired dibenzothiepin derivative through a combination of rearrangement, hydrolysis and ring closure in variable sequences.

Process for the preparation of dibenzothiepin derivative

A novel quinaldinamide derivative having the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents a lower alkyl group or R.sup.1 and R.sup.2 are combined together with the adjacent nitrogen atom to form a 5-7 membered ring; and X represents the hydrogen atom, a lower alkyl group or a lower alkoxy group, and its acid-addition salt, which show prominent central muscle relaxant effect, namely rigidity relieving effect on anemic decerebrated rigidity.

Quinaldinamide derivatives

1,3-Oxazolidine-one derivatives of the following formula ##STR1## where R is straight or branched alkyl of C.sub.3 -C.sub.8, X is hydrogen, halogen, lower alkyl or lower alkoxy and n is 4, 5 or 6, or their acid addition salts are effective for medicinal and agricultural use.

Growing community of inventors

Kuki, Japan

Naoya Moritoh