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Tetracycline derivatives and methods of use thereof

a technology of tetracycline and derivatives, applied in the field of tetracycline derivatives, can solve the problems of synthetic tetracyclines with substantially less or effective antimicrobial activity, and achieve the effect of not having antimicrobial activity

Inactive Publication Date: 2005-11-03
TETRAGENEX PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention relates to novel tetracycline derivatives, methods for producing them, and methods of using them. The invention provides new tetracycline derivatives that have improved antimicrobial properties and can be used to treat various medical conditions such as inflammation and bone disorders. The invention also provides new methods for producing and using these new tetracycline derivatives."

Problems solved by technology

Changes to the basic ring system or replacement of the substituents at positions 1-4 and 10-12, however, generally lead to synthetic tetracyclines with substantially less or effectively no antimicrobial activity.

Method used

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  • Tetracycline derivatives and methods of use thereof
  • Tetracycline derivatives and methods of use thereof
  • Tetracycline derivatives and methods of use thereof

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Embodiment Construction

[0016] Compounds disclosed herein are derivatives of tetracycline, which exhibit antimicrobial and / or anti-cancer activity.

[0017] In a preferred embodiment, the present invention relates to a treatment for inhibiting microbial or tumor growth which comprises adding to a subject in need of said treatment an effective amount of a tetracycline composition or salt thereof, comprising a general formula:

wherein R is selected from CH2N(RaRb) or [0018] RaRb are C1 to C6 alkyl; [0019] Rc and Rd are (CH2)n CHRe, n is 0 or 1 and Re is H, C1 to C6 alkyl, or NH2, and X is NH, S, or CH2; [0020] R1 is H or OH; [0021] R2 is H, OH, ═O, or OCOR8, where R8 is C1 to C6 alkyl, or alternatively, R2 is N(R9)2, where R9 is hydrogen or C1 to C6 lower alkyl, or R9 CO, with the proviso that when R2 is keto or N(R9)2, then R3 and R4 are H or CH3, and R3 and R4 are not both CH3 or H; [0022] 5a hydrogen is α or β; [0023] R3 and R4 are H, CH3 or F, with the proviso that when R3 is CH3, then R4 is H or F, and...

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Abstract

A treatment for inhibiting microbial or tumor growth is disclosed, which comprises adding to a subject in need of treatment an effective amount of one or more tetracycline derivatives.

Description

FIELD OF INVENTION [0001] The present invention relates to novel tetracycline derivatives, methods for producing the novel derivatives and methods of using these derivatives. BACKGROUND OF THE INVENTION [0002] The compound tetracycline, exhibits the following general structure [0003] The numbering system of the ring nucleus is as follows: [0004] Tetracycline as well as the 5-OH (Terramycin) and 7-Cl (Aureomycin) derivatives exist in nature, and are well known antibiotics. Natural tetracycline may be modified without losing their antibiotic properties, although certain elements of the structure must be retained. The modifications that may and may not be made to the basic tetracycline structure have been reviewed by Mitscher in The Chemistry of Tetracyclines, Chapter 6, Marcel Dekker, Publishers, New York (1978). According to Mitscher, the substituents at positions 5-9 of the tetracycline ring system may be modified without the complete loss of antibiotic properties. Changes to the ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/65A61K31/655A61P31/04A61P35/00C07C235/84C07C237/26
CPCA61K31/65C07C2103/46C07C237/26C07C2603/46A61P31/04A61P35/00
Inventor HLAVKA, JOSEPH J.ABLIN, RICHARD J.
Owner TETRAGENEX PHARMA