Asahi Kasei Kogyo Kabushiki Kaisha

Toyo Jozo Company, Ltd.

Yuji Kogami

Daisuke Mochizuki

Tatsuro Fujiwara

Naomi Aono

Asako Watanabe

2,3-dihydrobenzofuran derivatives, method for producing the same, and

Disclosed are a 2,3-dihydrobenzofuran derivative represented by formula (1) or a salt thereof, a method for producing the same, and use thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; n is an integer of from 2 to 6; A represents a carbonyl group or a sulfonyl group; R.sup.2 represents a hydrogen atom, a halogen atom, a lower alkyl group (which is unsubstituted or substituted with at least one halogen atom), a lower alkoxy group, a hydroxyl group, a nitro group or a cyano group; and * represents an asymmetric carbon atom. A 2,3-dihydrobenzofuran derivative of the present invention or a salt thereof has a strong affinity for a serotonin 1A receptor, and, therefore, is useful for prevention and treatment of serotonergic neuron-related diseases, such as anxiety, depression, high blood pressure, emeses (including emeses induced by motion sickness, space sickness and dizziness, etc.) and the like.

2,3-dihydrobenzofuran derivatives

9-Dihydro-9-O-alkyldesmycosin derivatives and their salts are disclosed. The 9-dihydro-9-O-alkyldesmycosin derivatives are represented by the following formula (I), ##STR1## --wherein X represents an --O-- mycinose or a di-lower alkylamino group, R.sup.1 represents a hydrogen atom or a lower alkanoyl group, R.sup.2 represents a lower alkyl group, a cycloalkyl-lower group, or phenyl-lower alkyl group which may have a substituent, and R.sup.3 represents a hydrogen atom or a hydroxyl group. The compounds and the salts are useful as an antimicrobial agent. Unlike known desmycosin derivatives, the compounds give a high blood concentration by oral administration.

9-dihydro-9-O-alkyldesmycosin derivatives

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Shizuoka, Japan

Yuji Kogami