Kyowa Hakko Kogyo Co., Ltd.

Satoru Nagamura

Hiromitsu Saito

Eiji Kobayashi

Katsushige Gomi

Akira Asai

Hiroshi Sano

Nobuo Hanai

Motoo Yamasaki

Yutaka Kanda

Makoto Morimoto

Toshiyuki Suzawa

Nobuyoshi Amishiro

So Ohta

Youichi Uosaki

Akihiko Okamoto

Mitsutaka Kino

Toshimitsu Takiguchi

Tadashi Kinoshita

Hidenori Aoki

The present invention relates to a toxin conjugate in which a residue derived from a compound having an affinity for a target cell is bound to a toxin through a spacer comprising polyalkylene glycol and dipeptide.

Toxin conjugates

A staurosporine derivative with anti-cancer activity and anti-bacterial activity is produced by acidifying a solution containing staurosporine to isomerize staurosporine to its desired derivative, whereby the derivative is recovered from the acidified solution.

Production of staurosporine derivative using acid isomerization

Method of purifying K-252a

DC-89 derivatives

Pyrrolo-indole derivatives

Novel DC-89 derivatives represented by general formula (I): ##STR1## wherein X represents Cl or Br; R.sup.1 represents hydrogen, CONR.sup.2 R.sup.3 (in which R.sup.2 and R.sup.3 independently represent hydrogen, a straight-chain or branched alkyl group having 1 to 4 carbon atoms or phenyl group), ##STR2## (in which n represents an integer of 4 to 7), ##STR3## (in which R.sup.4 represents oxygen, N--CH.sub.3 or N--CH.sub.2 CH.sub.2 NH.sub.2), ##STR4## (in which R.sup.5 R.sup.6 and R.sup.7 independently represent a straight-chain or branched alkyl group having 1 to 4 carbon atoms); and ##STR5## (in which Y represents hydrogen or CO.sub.2 CH.sub.3); provided that when R.sup.1 is hydrogen, CONR.sup.2 R.sup.3 or SiR.sup.5 R.sup.6 R.sup.7, ##STR6## and pharmaceutically acceptable salts thereof have an excellent anti-tumor activity and are expected to be useful as anti-tumor compositions.

DC-89 derivatives represented by the formula: ##STR1## wherein X represents hydrogen or CO.sub.2 CH.sub.3 ; and ##STR2## wherein Z represents Cl or Br; R represents hydrogen, CONR.sup.1 R.sup.2 (in which R.sup.1 and R.sup.2 independently represent hydrogen, a straight-chain or branched alkyl group having 1 to 4 carbon atoms or phenyl) or ##STR3## (in which n represents an integer of 0 to 4; R.sup.3 represents CH.sub.2, ##STR4## oxygen, N--CH.sub.3, or N--CH.sub.2 CONR.sup.1 R.sup.2 in which R.sup.1 and R.sup.2 have the same significances as defined above); and W represents hydrogen or ##STR5## (in which W.sup.1 and W.sup.2 independently represent hydrogen or OR.sup.2 in which R.sup.4 represents a straight-chain or branched alkyl group having 1 to 4 carbon atoms or a straight-chain or branched alkenyl group having 2 to 4 carbon atoms, and pharmaceutically acceptable salts thereof have an excellent anti-tumor and antibacterial activity and are expected to be useful as anti-tumor compositions and antibacterial compositions.

Novel DC-89 derivatives as shown below have an excellent anti-tumor activity, and thus are useful as anti-tumor agent ##STR1## wherein L represents chlorine or bromine; R represents ##STR2## (wherein n represents an integer of 4 to 7) or ##STR3## (wherein Y represents oxygen or N--M).

DC-89 derivatives as anti-tumor agents

Novel DC-89 derivatives have an excellent anti-tumor activity, and thus are useful as anti-tumor agent.

DC-88A derivatives represented by the general formula: ##STR1## wherein X represents hydrogen or CO.sub.2 R.sup.1 (in which R.sup.1 represents hydrogen, a straight-chain or branched alkyl having 1 to 4 carbon atoms, allyl, or benzyl); and ##STR2## have an excellent anti-tumor activity and are useful as anti-tumor agents.

Pyrroloindole derivatives

Pyrroloindole derivatives related to DC-88A compound

Growing community of inventors

Hofu, Japan

Satoru Nagamura