Sankyo Company, Limited

Keiichi Matsuda

Takeshi Oshima

Takafumi Kohama

Isao Kaneko

Takeshi Kagasaki

Yoshiya Amemiya

Ryuzo Enokita

Shunji Naruto

Takemichi Nakamura

Yuichi Sugano

Tomiichiro Oda

Atsusuke Terada

Isao Kawamoto

Shigeru Ushiyama

Rokuro Endo

Atsusuke Trada

Novel benzene derivatives are provided of the general formula (I): ##STR1## [wherein R.sup.1 represents an amino group, a substituted amino group, a protected amino group, or a nitro group; R.sup.2 represents an amino group, a substituted amino group, a protected amino group, a hydroxy group, a substituted hydroxy group, or a protected hydroxy group; R.sup.3 represents an amino group, a substituted amino, a heterocyclyl group having a ring nitrogen atom as the point of binding, or a substituted heterocyclyl group having a ring nitrogen atom as the point of binding; m is 0 to 2; n is 0 to 6; with the proviso that when m is 0, then n represents an integer from 2 to 6] and salts thereof. Compounds of formula (I) except those wherein R.sup.1 is a nitro group have activity in promoting production of nerve growth factor. Compounds of formula (I) wherein R.sup.1 is a nitro group are intermediates for compounds of formula (I) wherein R.sup.1 is an amino group.

Benzene derivatives having NGF production-promoting activity

A compound of the formula (I): ##STR1## wherein R.sup.1 is an unsubstituted or substituted amino group, a protected amino group, or a nitro group; R.sup.2 is an unsubstituted or substituted amino group, a protected amino group, an unsubstituted or substituted hydroxy group or a protected hydroxy group; R.sup.3 is an unsubstituted or substituted amino group, m is 0 to 2; n is 0 to 6; with the proviso that when m is 0, then n is an integer from 2 to 6, and pharmaceutically acceptable salts thereof. Compounds of formula (I) except those wherein R.sup.1 is a nitro group have activity in promoting the production of nerve growth factor.

New compounds, which we have named the 'Leustroducsins' have the formula (I): ##STR1## in which R represents a 5-methylhexanoyloxy group, a 6-methyloctanoyloxy group or a 7-methyloctanoyloxy group, and salts thereof, and may be prepared by fermentation using a microorganism of the genus Streptomyces, especially a strain of the species Streptomyces platensis, such as strain SANK 60191 (FERM BP-3288). These compounds may be used for the treatment or prophylaxis of: adverse reactions resulting from cancer chemotherapy or radiotherapy; infections; cancer; cerebral dysfunction; and fungal infections.

Process to prepare leustroducsins

Compounds, named the 'Leustroducsins', their preparation and their

Compounds of formula (I): ##STR1## (wherein n is 0 or 1, R.sup.1 and R.sup.2 are hydrogen or alkyl, one of A.sup.1 and A.sup.2 is --Z--Y and the other is --W--COOH, where W and Z are alkenylene or alkylene and Y is imidazolyl or pyridyl, and the broken lines represent two single bonds or one single bond and one double bond) and their salts, esters and amides have the ability to inhibit the synthesis of thromboxane A.sub.2 and hence are useful in the treatment of prophylaxis of thrombotic conditions. They may be prepared by introducing an imidazolyl or pyridyl group into the corresponding compound in which Y is replaced by an active group or atom.

Thianaphthene derivatives

Compounds of formula (I): ##STR1## (wherein n is 0, 1 or 2 and R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.6, X, Y and Z are a variety of groups and atoms) have the ability to inhibit the synthesis of thromboxane A.sub.2 and hence are useful in the treatment or prophylaxis of thrombotic conditions.

Imidazole derivatives as inhibitors of TXA.sub.2 synthesis

Compounds of formula (I): ##STR1## (wherein n is 0 or 1, R.sup.1 and R.sup.2 are hydrogen or alkyl, one of A.sup.1 and A.sup.2 is --Z--Y and the other is --W--COOH, where W and Z are alkenylene or alkylene and Y is imidazolyl or pyridyl, and the broken lines represent two single bonds or one single bond and one double bond) and their salts, esters and amides have the ability to inhibit the synthesis of thromboxane A.sub.2 and hence are useful in the treatment or prophylaxis of thrombotic conditions. They may be prepared by introducing an imidazolyl or pyridyl group into the corresponding compound in which Y is replaced by an active group or atom.

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Tokyo, Japan

Keiichi Matsuda