Derivatives of sapogenin, their synthesis, using and method based on their using

FIELD: organic chemistry, steroids.

SUBSTANCE: invention discloses derivatives of steroid sapogenins of the general formula (I): wherein R means alkylcarbonyl, alkoxycarbonyl substituted possibly with amino-group and others under condition that R is not acetyl and R is not ethoxycarbonyl if C3 is in S and C25 in R-configurations simultaneously; R is nor succinyl if C3 and C25 are in S-configuration simultaneously, or C3 R(α) or S(β), and C25 in R-configuration. Also, invention discloses using these compounds in treatment of cognitive dysfunction, noncognitive neurodegeneration, noncognitive neuromuscular degeneration and loss of receptors in absence of cognitive, nervous and neuromuscular insufficiency. Also, invention discloses methods for synthesis of these compounds, treatment and pharmaceutical composition containing thereof.

EFFECT: improved method of synthesis, valuable medicinal properties of compounds and pharmaceutical compositions.

30 cl, 2 tbl, 5 dwg, 16 ex

 

The text descriptions are given in facsimile form.

1. Compounds of General formula II

characterized in that the group R is selected from alkylcarboxylic or alkoxycarbonyl; where any alkyl group may be substituted amino group, alkoxycarbonylmethyl, monoalkylamines, dialkylamines, N-alkyl, N-alkoxycarbonylmethyl or a residue of carboxylic acid (-COOH), or any combination thereof; provided, that

R is not unsubstituted acetyl;

R is not unsubstituted etoxycarbonyl if C3 has S(β)-configuration, and C25 - R-configuration;

R is not succinyl if C3 has S(β)-configuration, and C25 - S-configuration or C3 has R(α)- or S(β)-configuration, and C25 - R-configuration; and

R is not propionyl, isobutyryl, butyryl, valeryl, isovaleryl, caproyl, isocaproic, diethylacetal, octanoyl, decanoyl, lauryl, myristyl, palmityl, stearyl, cinnamate when C25 has the R-configuration, and C3-S(β)-con is Horatio;

including, if the above conditions, all stereoisomers and racemic mixtures and their salts.

2. The compounds of formula II as defined in claim 1, characterized in that the group R is selected from lower alkylcarboxylic and lower alkoxycarbonyl, which can be substituted at the terminal residue of carboxylic acid (-COOH).

3. Compounds according to claim 1 or 2, characterized in that With25-methyl group is in the R-configuration.

4. Compounds according to claim 1 or 2, characterized in that C25-methyl group is in the S-configuration.

5. A compound selected from the group comprising: apisgelerin katilot, sarsasapogenin katilot, epicastasterone katilot, epicastasterone succinate, sarsasapogenin glycinate, epicastasterone glycinate, smilagenin glycinate, apisgelerin glycinate, sarsasapogenin alaninate, epicastasterone alaninate, smilagenin alaninate, apisgelerin alaninate, sarsasapogenin valint, epicastasterone valint, smilagenin valint, apisgelerin valint, sarsasapogenin isoleucine, epicastasterone isoleucine, smilagenin isoleucine, apisgelerin isoleucine, sarsasapogenin methionine, epicastasterone methionine, smilagenin methionine, apisgelerin methionine and their pharmaceutically acceptable salts.

6. Compounds according to claim 1 or 2, and their pharmacist is Cesky acceptable salt, designed for use as a medicine.

7. Compounds according to claim 3 and their pharmaceutically acceptable salts, intended for use as a medicine.

8. Compounds 4 and their pharmaceutically acceptable salts, intended for use as a medicine.

9. The method of synthesis of compounds of formula II as defined in any one of claims 1 to 5, comprising the reaction of compounds of formula II in which R=H, with a compound of the formula

L-R,

in which the group R is selected from alkylcarboxylic or alkoxycarbonyl, where any alkyl group may be substituted amino group, monoalkylamines, dialkylamines, the remainder of the carboxylic acid (-COOH) or any combination thereof, and L is removed by the group under conditions suitable for nucleophilic substitution.

10. The method according to claim 9, characterized in that the compound L-R is a carboxylic acid, anhydride or allalone.

11. The method of synthesis of a derivative of a steroid sapogenin formula II as defined in any one of claims 1 to 5, including the processing of selected steroid sapogenin etelcharge.com in the presence of a base to form a 3-ethoxycarbonyl derived.

12. The method according to claim 11, characterized in that the substrate is dry pyridine and dissolved in dry is m dichloromethane.

13. Synthesis apisgelerin of catilina of apisgelerin by reaction with etelcharge.com and base.

14. Synthesis sarsasapogenin of catilina of sarsasapogenin by reaction with etelcharge.com and base.

15. Synthesis epicastasterone of catilina of epicastasterone by reaction with etelcharge.com reagent and a base.

16. Synthesis epicastasterone succinate from epicastasterone by reaction with succinic anhydride reagent and a base.

17. The use of compounds as defined in any one of claims 1 to 5, or its acceptable from a medical point of view salts for the manufacture of drugs to increase the number of nicotinic and/or muscarinic receptors and/or dopamine receptors and/or adrenergic receptors or speed up their metabolism, or to enhance the function of nicotinic and/or muscarinic receptors and/or dopamine receptors and/or adrenergic receptors in man or animal.

18. The composition having activity against cognitive dysfunction in humans or animal containing an effective dose of a compound of General formula II as defined in any one of claims 1 to 5, or its pharmaceutically acceptable salt.

19. Pharmaceutical composition for treatment of cognitive dysfunction, containing a pharmacologically effective amount of one or more compounds of formula II, as they determine the Helena in any one of claims 1 to 5, or their pharmaceutically acceptable salts.

20. Food, food Supplement or beverage containing a pharmacologically effective amount of one or more compounds of the formula II as defined in any one of claims 1 to 5, or their pharmaceutically acceptable salts.

21. The composition having the property of enhancing cognitive function, containing a pharmacologically effective amount of one or more compounds from the group comprising: apisgelerin katilot, sarsasapogenin katilot, epicastasterone katilot, epicastasterone succinate, sarsasapogenin glycinate, epicastasterone glycinate, smilagenin glycinate, apisgelerin glycinate, sarsasapogenin alaninate, epicastasterone alaninate, smilagenin alaninate, apisgelerin alaninate, sarsasapogenin valint, epicastasterone valint, smilagenin valint, apisgelerin valint, sarsasapogenin isoleucine, epicastasterone isoleucine, smilagenin isoleucine, apisgelerin isoleucine, sarsasapogenin methionine, epicastasterone methionine, smilagenin methionine, apisgelerin methionine or their pharmaceutically acceptable salts.

22. Drug for treatment of cognitive dysfunction, containing one or more compounds from the group comprising: apisgelerin katilot, sarsasapogenin katilot, EPI is sarsasapogenin katilot, epicastasterone succinate, sarsasapogenin glycinate, epicastasterone glycinate, smilagenin glycinate, apisgelerin glycinate, sarsasapogenin alaninate, epicastasterone alaninate, smilagenin alaninate, apisgelerin alaninate, sarsasapogenin valint, epicastasterone valint, smilagenin valint, apisgelerin valint, sarsasapogenin isoleucine, epicastasterone isoleucine, smilagenin isoleucine, apisgelerin isoleucine, sarsasapogenin methionine, epicastasterone methionine, smilagenin methionine, apisgelerin methionine or their pharmaceutically acceptable salts.

23. Method for the treatment or prevention of cognitive dysfunction in a human or animal in need thereof, comprising the administration to a human or animal an effective dose of the compounds of General formula II as defined in any one of claims 1 to 5, or its pharmaceutically acceptable salt.

24. A method of treating cognitive dysfunction in a patient suffering from a disease selected from the group including: Alzheimer's disease, senile dementia type (DATE), age-associated memory loss (AAMI), dementia with calves levy or autism, including the introduction to the patient a pharmacologically effective amount of the compounds of formula II as defined in any one of claims 1 to 5.

25. Method of strengthening Kohn the tive functions in man or animal, includes introduction to the patient an effective amount of the compounds of formula II as defined in any one of claims 1 to 5.

26. The method according A.25, characterized in that the treatment is a non-therapeutic method applied to the normal subject for enhancing cognitive function in the subject.

27. The application of one or more compounds of the formula II as defined in any one of claims 1 to 5, or their pharmaceutically acceptable salts as an ingredient in the pharmaceutical composition, food, food Supplement or beverage in the treatment of Alzheimer's disease, the DATE, AAMI, syndrome of mild cognitive impairment (ISS) and autism.

28. Method of enhancing cognitive function in a patient suffering from age-associated cognitive dysfunction, comprising the administration to a patient a pharmacologically effective dose of the compounds of formula II as defined in any one of claims 1 to 5.

29. The method according to PP, 24, 25 or 27, characterized in that it is designed for the treatment of Alzheimer's disease or senile dementia in medical literature type.

30. The use of compounds of General formula II as defined in any one of claims 1 to 5, for the preparation of compositions for the treatment or prevention of cognitive dysfunction in humans and animals suffering from or susceptible to them.



 

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2 tbl

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12 cl, 1 tbl, 16 ex

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33 cl, 9 tbl, 3 dwg, 5 ex

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5 ex

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14 cl, 1 tbl, 25(29) ex

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9 cl, 9 dwg, 8 ex, 6 tbl

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19 cl, 9 tbl, 19 ex

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