Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-04-17
1998-03-31
Marschel, Ardin H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
540450, 540451, 540467, 540471, 540472, 540473, 540476, 540477, 540482, 549 1, 549 9, 549 10, 514 1, 514 23, 514183, 514430, 514461, 514471, 514473, 514478, 514480, A61K 3700
Patent
active
057339244
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to novel DC107 derivatives having an antibacterial activity and an antitumor activity.
BACKGROUND ART
DC107 (leinamycin) is a compound produced by a microorganism belonging to the genus Streptomyces and disclosed in Japanese Published Unexamined Patent Application No. 112988/89. DC107 exhibits an antibacterial activity against various bacteria and also an antitumor activity and has a chemical structure represented by the formula (I) described below wherein R.sup.1, R.sup.2 and Z each represents a hydrogen atom, R.sup.3 bonds to Y to represent a single bond, and W represents an oxygen atom.
DISCLOSURE OF THE INVENTION
The present invention relates to the DC107 derivatives represented by the formula (I): ##STR2## or pharmacologically acceptable salts thereof, wherein R.sup.1 represents hydrogen, a lower alkoxyalkyl group, an aralkyloxyalkyl group, a lower alkoxyalkoxyalkyl group, a lower alkoxyalkoxyalkoxyalkyl group, an aralkyl group, a tetrahydropyranyl group, ##STR3## {wherein Q.sup.1 represents CH.sub.2, O, S, SO, SO.sub.2 or N--Q.sup.3 (wherein Q.sup.3 represents a substituted or unsubstituted aryl group or a lower alkoxycarbonyl group), and Q.sup.2 represents a lower alkyl group}, group, an aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic group, a lower alkoxy group, an alicyclic alkoxy group, a 9-fluorenylmethoxy, an aralkyloxy group, a substituted or unsubstituted aryloxy group, (CH.sub.2).sub.m R.sup.4A <wherein m represents an integer of from 1 to 6, R.sup.4A represents hydroxy, a lower alkoxy group, a carboxyl group, a lower alkoxycarbonyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted aralkyloxy group, NR.sup.4B COR.sup.4C {wherein R.sup.4B represents hydrogen or a lower alkyl group, and R.sup.4C represents hydrogen, a lower alkyl group, a lower alkoxy group, an aralkyloxy group, an aryl group, an aryloxy group, a 9-fluorenylmethoxy group, (CH.sub.2).sub.n NHCOR.sup.4D (wherein n represents an integer of from 1 to 6, R.sup.4D represents an alkyl group, a lower alkoxy group, an aralkyloxy group, an aryl group, an aryloxy group or a 9-fluorenylmethyloxy group) or CHR.sup.4E NHCOR.sup.4F (wherein R.sup.4E represents a lower alkyl group or a hydroxy lower alkyl group, and R.sup.4F has the same meaning as R.sup.4D)}> or CHR.sup.4G NHCOR.sup.4H (wherein R.sup.4G has the same meaning as R.sup.4E, and R.sup.4H has the same meaning as R.sup.4C)!; R.sup.2 represents hydrogen or COR.sup.5 (wherein R.sup.5 represents a lower alkyl group, an aralkyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group); R.sup.3 represents a lower alkyl group, a lower alkenyl group, a substituted or unsubstituted aralkyl group in which aryl may be substituted, a lower alkoxyalkyl group, an aralkyloxyalkyl group, a substituted or unsubstituted aryloxyalkyl group, a lower alkoxycarbonylalkyl group, a lower alkanoyloxyalkyl group, an alicyclic alkanoyloxyalkyl group or ##STR4## or R.sup.3 bonds to Y to represent a single bond; Y bonds to R.sup.3 to represent a single bond or bonds to Z to represent a single bond; Z represents hydrogen or bonds to Y to represent a single bond; W represents oxygen or NR.sup.6 (wherein R.sup.6 represents a hydroxyl group, a lower alkoxy group, a lower alkenyloxy group, an aralkyloxy group, a substituted or unsubstituted arylsulfonylamino group or a lower alkoxycarbonylamino group), with the proviso that the compound wherein R.sup.1, R.sup.2 and Z each represents hydrogen, R.sup.3 bonds to Y to represent a single bond, and W represents oxygen (DC107) is excluded.
In the present invention, the compounds represented by the formula (I) above are hereinafter referred to as compound (I). Other formula numbers are also applied to the corresponding compounds in the same manner.
In the definition of each of the groups in the formula (I), the alkyl group includes a straight
REFERENCES:
patent: 4999196 (1991-03-01), Nakano et al.
Chemical Abstracts, vol. 112, No. 11 (Mar. 12, 1990) 96887z.
Hara et al., J. Antibiot., vol. 42, No. 12 (1989) 1768-74.
Ashizawa Tadashi
Gomi Katsushige
Kakita Shingo
Kanda Yutaka
Murakata Chikara
Kyowa Hakko Kogyo Co. Ltd.
Marschel Ardin H.
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