Title:
【発明の名称】アメトプテリン(メトトレキセート)のプロドラッグ、中間生成物、製造方法およびそれらを含有する組成物
Document Type and Number:
Japanese Patent JPH06501240
Kind Code:
A
Abstract:
The synthesis of gem-diphosphonic amethopterin(methotrexate) analogues, and their use as pharmaceutical compositions for various therapeutical applications, are described. In particular, an association of the pro-drug concept with the pharmacological vectorization of antineoplastic agents for bone carcinomata, using diphosphonic acids, is desired. The gem-diphosphonic amethopterin(methotrexate) and 10-N-deaza amethopterin compounds have the form of an amethopterin pro-drug of which the gem-diphosphonic grouping is connected to the pteroylglutamic grouping by a peptide linkage. These compounds are particularly useful in cancerological pharmaceutical compositions particularly intended for treating tumours or metastases, especially those to bone, and/or in rheumatological pharmaceutical compositions particularly intended for treating resistant psoriatic rheumatism, polymyositis, Reiter's disease and rheumatoid arthritis.
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Inventors:
Georges Sturz
Application Number:
JP50875891A
Publication Date:
February 10, 1994
Filing Date:
April 23, 1991
Export Citation:
Assignee:
Université de Bretagne, Occidental
International Classes:
A61K31/519; A61K31/675; A61K47/48; C07D475/06; A61K31/505; C07F9/40; C07F9/6561; (IPC1-7): C07F9/6561; A61K31/505; A61K31/675; C07D475/06
Attorney, Agent or Firm:
Shusaku Yamamoto