Nippon Kayaku Kabushiki Kaisha

Kazuhisa Narita

Akira Shiozawa

Hideo Sugimura

Hirotaka Yamamoto

Kazuo Ohtsuki

Yuh-ichiro Ichikawa

Tochiro Tatee

Yukihiro Sagawa

Shuji Kurashige

Takeji Sakasai

Kouwa Yamashita

Michio Ishikawa

Yukihiro Nishiyama

Masashi Nagai

Kenichi Matsubara

Takemitsu Nagahata

Takashi Takahira

Makoto Hosono

Yuka Sugawara

Chikara Komuro

Hiroshi Akaba

Masashi Iida

Giichi Izumi

Ichiro Koga

Katsuhiko Sakitama

Atsushi Okada

Sayuri Kato

Atsuro Inubushi

Masao Sakurai

Aya Ishikawa

Remedies/preventives (therapeutic or preventive agents) against frequent urination (pollakiuria)/urinary incontinence which contain as an active ingredient compound having a tropone structure or pharmacologically acceptable salt thereof and a novel compound having the tropone structure. The compounds having a tropone structure and having the above pharmacological effects are those represented by, for example, general (1):

Remedies/preventives for frequent urination/urinary incontinence and tropone derivatives

This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.

Process for the preparation of 6,7-diacyl-7-deacetylforskolin derivatives

This invention relates to cyclobutane derivatives represented by the following general formula (1) and physiologically acceptable salts thereof: ##STR1## wherein B represents a nucleic acid base derivative, R.sup.1 and R.sup.2 independently represent hydrogen atom, dialkylaminoacyl group, 1,4-dihydro-1-methylnicotinoyl group or substituted phosphoric acid group, provided that either one of R.sup.1 and R.sup.2 is a group other than hydrogen atom. The compounds of this invention exhibit a high oral absorbability and are metabolized in vivo into the compounds of formula (1a). Accordingly, the compounds of this invention are expectedly useful as antiviral agent.

Phenoxyphosphoryloxymethyl cyclobutyl purines

A chroman derivative represented by the following general formula [1]: ##STR1## wherein R.sub.1 represents cyano group, nitro group, halogenomethyl group or --SO.sub.2 --X group (X represents lower alkyl group having 1-6 carbon atoms or aryl group); R.sub.2 represents hydrogen atom or OA group (A represents hydrogen atom, nitro group, lower acyl group having 1-6 carbon atoms, arylcarbonyl group, lower alkylsulfonyl group having 1-6 carbon atoms, arylsulfonyl group, arylalkyl group, tetrahydropyranyl group, lower alkoxycarbonyl group having 1-6 carbon atoms, arylalkoxycarbonyl group or silyl derivative group); R.sub.3 singly represents a hydrogen atom; or R.sub.3 forms a bond jointly with R.sub.2 ; and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each represent hydrogen atom, vinyl group, formyl group, --Y--(OA).sub.n group (Y represents straight or branched chain alkylene group having 1-6 carbon atoms or lower alkenyl group having 1-6 carbon atoms, A is as defined above, and n represents an integer of 1-3. The compound of this invention is expected to be effectively usable as an agent for treatment of various symptoms due to the contraction of smooth muscles, for treatment of the diseases of the circulatory system and for treatment of epilepsy.

Certain chroman derivatives useful for treating symptoms caused by

This invention relates to a process for producing an optically active cyclobutylamine which comprises reacting a racemic modification of cyclobuthylamine represented by the following general formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 represent each a hydrogen atom or a protecting group; with an optically active N-acylphenylglycine to thereby give two corresponding diastereomeric salts, crystallizing the more difficultly soluble diastereomeric salt and isolating the corresponding optically active cyclobutylamine from the diastereomeric salt thus crystallized. The optically active substances of the compound of the above general formula [I] are useful as, for example, an intermediate in the synthesis of 9-[(1R, 2R, 3S)-2,3-bis(hydroxymethyl)-1-cyclobutyl]guanine which is expected as an antiviral agent.

Process for producing optically active cyclobutylamines

A process for producing an optically active aminoketone derivative having a central muscle relaxant activity is described wherein a racemic mixture of the aminoketone is reacted with optically active L-acetylphenylglycine and then isolating the optically active L-aminoketone from the diastereomeric salts formed by the reaction.

Process for producing an optically active aminoketone derivative

A new class of aminoketone derivatives according to the formula: ##STR1## and certain propiophenone derivatives in particular, corresponding to the formula: ##STR2## having central muscle relaxant activity.

Derivatives of an aminoketone

This invention relates to forskolin derivatives, their physiologically acceptable salts, and a process for producing these compounds. The forskolin derivative is represented by the general formula ##STR1## wherein; I. when R.sup.1 is hydrogen and R.sup.4 is vinyl, ethyl, or cyclopropyl,

Forskolin compounds

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Tokyo, Japan

Kazuhisa Narita