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Staufosporine derivatives as inhibitors of receptor tyrosine kinase flt3 activity
Staufosporine derivatives as inhibitors of receptor tyrosine kinase flt3 activity
IPC classes for russian patent Staufosporine derivatives as inhibitors of receptor tyrosine kinase flt3 activity (RU 2337692):
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Invention relates to a spontaneously dispersing composition comprising N-benzoylstaurosporin, a hydrophilic component, a lipophilic component and a surface-active substance taken in the definite ratio of components. Also, invention relates to a method for treatment of the patient needing administration of N-benzoylstautosporin as a component of the spontaneously dispersing composition. The composition possesses the enhanced level of biological availability or diminished variability of the biological availability levels and effectiveness.

FIELD: medicine; pharmacology.

SUBSTANCE: invention concerns application of N-[(9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9N-diindolo [1,2,3-gh:3', 2', 1'-lm] pyrrolo[3,4-j][1,7]benzodiasonine-11-yl]-N-methylbenzamide of formula or its salts for production of pharmaceutical composition intended for treatment of diseases associated with uncontrolled activity of receptor tyrosine kinase FLT3, pharmaceutical preparation and product, containing connection of formula (II).

EFFECT: high efficiency of treatment.

6 cl, 1 tbl, 2 ex

 

The text descriptions are given in facsimile form.

1. The use of N-[(9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,N-vindaloo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazepin-11-yl]-N-methylbenzamide formula (VII)

or its salt to obtain a pharmaceutical composition intended for the treatment of diseases associated with uncontrolled activity of the receptor tyrosine kinase FLT3.

2. The use according to claim 1 for the treatment of leukemias and myelodysplastic syndromes.

3. The use according to claim 1 for the treatment of acute myeloid leukemia and myelodysplastic the x syndromes at high risk.

4. Pharmaceutical preparation for the treatment of leukemia, including N-[(9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,N-vindaloo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazepin-11-yl]-N-methylbenzamide formula (VII) in an effective amount.

5. The product, including packaging material and N-[(9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,N-vindaloo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazepin-11-yl]-N-methylbenzamide formula (VII) according to claim 1 or its pharmaceutically acceptable salts contained in the specified packaging material, and specified packaging material includes label instructions, in which it is reported that the compound of formula (VII) or its pharmaceutically acceptable salt should be introduced mammals suffering from diseases associated with uncontrolled activity of the receptor tyrosine kinase FLT3, in the amount of from 220 to 230 mg special treatment regimen for inhibiting the development of diseases associated with uncontrolled activity of the receptor tyrosine kinase FLT3.

6. The product according to claim 5, where the compound of formula VII is administered three times daily at a total dose of from 220 to 230 mg, and preferably at a dose of from 70 to 80 mg every introduction, for the treatment of leukemia, especially acute myeloid leukemia and myelodysplastic syndromes at high risk.

Priority items:

30.10.200 according to claims 1 to 4;

29.10.2002 on pp.5 and 6.

 
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