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Title:
メタロマトリックスプロテイナーゼによって活性化される腫瘍ターゲティング・プロドラッグ
Document Type and Number:
Japanese Patent JP2004531493
Kind Code:
A
Abstract:
A-(B)n-X (I) A-(B)n-Q (II) Structural Relationship of Example (8) to its Potential Metabolites Numbers in Parentheses denote examples in the specification A compound is of general formula (I) wherein (A) is a moiety comprising one of more of a heterocylcic ring, a carbocyclic ring and a fused ring system, the ring or ring system being essential for a biological activity of the compound by action at a nucleic acid or protein target (B) is a bivalent spacer molecule attached directly to the ring system n is an integer 0 or 1 and (X) is a monovalent moiety containing a amide bond that is cleavable by the action of a matrix metalloproteinase enzyme such as to produce a compound of formula (II) wherein the efficacy of the biological activity of the compound of formula (II) is increased over that of the compound of formula (I).

Inventors:
Mincher, david john
Turnbull, Agnes
Bibby, Michael Charles
Lord Man, Paul Michael
Application Number:
JP2002571533A
Publication Date:
October 14, 2004
Filing Date:
March 08, 2002
Export Citation:
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Assignee:
The Court of Napier University
BTG International Limited
Cancer Research Ventures Limited
International Classes:
A61K38/00; A61K47/48; A61P29/00; A61P31/12; A61P31/18; A61P31/22; A61P33/00; A61P33/02; A61P33/06; A61P35/00; A61P35/04; A61P43/00; C07C225/32; C07K7/06; (IPC1-7): C07K7/06; A61K38/00; A61K47/48; A61P29/00; A61P31/12; A61P31/18; A61P31/22; A61P33/00; A61P33/02; A61P33/06; A61P35/00; A61P35/04; A61P43/00; C07C225/32
Attorney, Agent or Firm:
Kazuo Shamoto
Tadashi Masui
Yasushi Kobayashi
Akio Chiba
Hiroyuki Tomita
Ken Matsumoto