NITROANILINE-BASED ALKYLATING AGENT, AND USE OF THE SAME AS PRODRUG

Title:

NITROANILINE-BASED ALKYLATING AGENT, AND USE OF THE SAME AS PRODRUG

Document Type and Number:

Japanese Patent JP2010265272

Kind Code:

A

Abstract:

To provide a series of non-symmetric mustards, the non-symmetrical mustards suitable for the use as prodrugs for GDEPT (gene dependent enzyme-prodrug therapy) and cell ablation therapy in conjunction with nitroreductase enzymes as hypoxia-selective cytotoxins and as anti-cancer agents, and a method for synthesizing them.

The non-symmetrical mustards are expressed by formula (I) [wherein, X is one of NO2, CN or SO2R1; Y is OR2, NHCOR2, CONH(CH2)2CO2Me, CONH(CH2)3N morpholide, CONHR2or the like; and A and B are each independently a halogen, OSO2R4, OSO2NH2or the like].

Inventors:

DENNY WILLIAM ALEXANDER
ATWELL GRAHAM J
YANG SHANGJIN
WILSON WILLIAM ROBERT
PATTERSON ADAM VORN

Application Number:

JP2010136139A

Publication Date:

November 25, 2010

Filing Date:

June 15, 2010

Export Citation:

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Assignee:

OAKLAND UNISERVICES LTD

International Classes:

C07C237/30; A61K31/166; A61K31/5375; A61P35/00; A61P43/00; C07C231/12; C07C303/30; C07C309/66; C07C311/39; C07D263/04; C07D295/13; C07D317/28

Attorney, Agent or Firm:

Norihiko Hibi
Einosuke Kishimoto
Akira Watanabe

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