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    • 2. 发明专利
    • AT459704T
    • 2010-03-15
    • AT05773198
    • 2005-05-25
    • TOULOUSE INST NAT POLYTECH
    • ZITOUNI ABDELGHANISABOU NASSERDINEMATHIEU FLORENCELEBRIHI AHMED
    • C12N1/20A01N43/24A61K31/357A61P31/00A61P31/04A61P31/12A61P35/00C07D309/10C07D407/12C07D407/14C07D493/14C07D493/22C07D519/00C07H15/252C12P15/00C12P17/02C12R1/04
    • The actinomycetes strain SaccharothrixSA 103 (CNCM I-3160) (A) and its mutants (A') are new, where (A') are obtained by selective mutation of (A) while retaining its ability to produce new or known active compound(s) (I) selected from mutactimycins and aldgamycins. Independent claims are also included for: (1) selection of (A)/(A'), by contacting a biological sample potentially containing (A)/(A') with a suitable selection medium, then isolating (A)/(A'); (2) production of a culture broth from a culture of (A)/(A'), by culturing (A)/(A') in a nutrient broth and optionally separating the broth (specifically by centrifugation, filtration and/or pasteurization); (3) culture broths obtained by the process; (4) production of an active concentrate from the culture broths by: (a) extracting the broth with an organic solvent; (b) optionally dehydrating the organic phase and/or drying under vacuum; and (c) optionally resuspending the obtained concentrate, preferably filtering the concentrate and repeating steps (a) and (b); (5) active concentrates obtained by the process; (6) production of active compounds (specifically mutactimycins such as mutactimycin P11, PR, G or F or aldgamycins such as aldgamycin G, H or P10b) from the concentrates by HPLC, preferably preceded by thin layer chromatography and/or low pressure liquid chromatography; (7) new active compounds obtained by the process, selected from mutactimycin PR of formula (Ia), mutactimycin F of formula (Ib), mutactimycin G of formula (Ic), aldgamycin G of formula (Id) (with the exception of the specific stereoisomer of formula (Id')), aldgamycin H of formula (Ie), aldgamycin P10b of formula (If) and their acid addition salts, isomers, enantiomers and diastereomers (including mixtures). [Image] [Image] [Image] ACTIVITY : Antibiotic; Cardiant; Antiinflammatory; Auditory; Tuberculostatic; Antileprotic; Virucide; Anti-HIV; Hepatotropic; Neuroprotective; Cytostatic. Mutactimycin PR (Ia) had MIC values of 50 mu g/ml against Staphylococcus aureusCIP 53156 and Micrococcus luteusATCC 9314, 40 mu g/ml against Klebsiella pneumoniaeCIP 82.91, and 75 mu g/ml against Bacillus subtilisATCC 6633. MECHANISM OF ACTION : None given.
    • 3. 发明专利
    • DE602005019723D1
    • 2010-04-15
    • DE602005019723
    • 2005-05-25
    • TOULOUSE INST NAT POLYTECH
    • ZITOUNI ABDELGHANISABOU NASSERDINEMATHIEU FLORENCELEBRIHI AHMED
    • C12N1/20A01N43/24A61K31/357A61P31/00A61P31/04A61P31/12A61P35/00C07D309/10C07D407/12C07D407/14C07D493/14C07D493/22C07D519/00C07H15/252C12P15/00C12P17/02C12R1/04
    • The actinomycetes strain SaccharothrixSA 103 (CNCM I-3160) (A) and its mutants (A') are new, where (A') are obtained by selective mutation of (A) while retaining its ability to produce new or known active compound(s) (I) selected from mutactimycins and aldgamycins. Independent claims are also included for: (1) selection of (A)/(A'), by contacting a biological sample potentially containing (A)/(A') with a suitable selection medium, then isolating (A)/(A'); (2) production of a culture broth from a culture of (A)/(A'), by culturing (A)/(A') in a nutrient broth and optionally separating the broth (specifically by centrifugation, filtration and/or pasteurization); (3) culture broths obtained by the process; (4) production of an active concentrate from the culture broths by: (a) extracting the broth with an organic solvent; (b) optionally dehydrating the organic phase and/or drying under vacuum; and (c) optionally resuspending the obtained concentrate, preferably filtering the concentrate and repeating steps (a) and (b); (5) active concentrates obtained by the process; (6) production of active compounds (specifically mutactimycins such as mutactimycin P11, PR, G or F or aldgamycins such as aldgamycin G, H or P10b) from the concentrates by HPLC, preferably preceded by thin layer chromatography and/or low pressure liquid chromatography; (7) new active compounds obtained by the process, selected from mutactimycin PR of formula (Ia), mutactimycin F of formula (Ib), mutactimycin G of formula (Ic), aldgamycin G of formula (Id) (with the exception of the specific stereoisomer of formula (Id')), aldgamycin H of formula (Ie), aldgamycin P10b of formula (If) and their acid addition salts, isomers, enantiomers and diastereomers (including mixtures). [Image] [Image] [Image] ACTIVITY : Antibiotic; Cardiant; Antiinflammatory; Auditory; Tuberculostatic; Antileprotic; Virucide; Anti-HIV; Hepatotropic; Neuroprotective; Cytostatic. Mutactimycin PR (Ia) had MIC values of 50 mu g/ml against Staphylococcus aureusCIP 53156 and Micrococcus luteusATCC 9314, 40 mu g/ml against Klebsiella pneumoniaeCIP 82.91, and 75 mu g/ml against Bacillus subtilisATCC 6633. MECHANISM OF ACTION : None given.