Derivatives of 5-aminopyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine, pharmaceutical composition based on thereof, using and methods for preparing intermediate compounds

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention describes novel derivatives of 5-aminopyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine of the general formula: wherein R means furanyl, possibly substituted pyrrolyl, possibly substituted pyridyl, possibly substituted phenyl or (C4-C6)-cycloalkenyl; X means (C2-C6)-alkylene or -C(O)CH2-; Y means the following groups: -N(R2)CH2CH2N(R3)-, -OCH2CH2N(R2)- wherein R2 and R3 mean hydrogen atom or (C1-C6)-alkyl, -O-, -S-, -CH2S-, -(CH2)2-NH- or compound of the formula: wherein Q means or R4 means hydrogen atom or (C1-C6)-alkyl, or two R at one carbon atom form group =O; Z means phenyl comprising from 1 to 5 of different substitutes, phenylalkyl or heteroaryl, diphenylmethyl and other values; or Z and Y in common can form substituted piperidinyl or substituted phenyl also possessing activity of antagonist of A2a adenosine receptors. Also, invention relates to a pharmaceutical composition based on these compounds, using novel compounds for preparing medicinal agents in treatment, for example, Parkinson's disease, and two methods for synthesis of intermediate compounds of formulae (II) and (IIIa) .

EFFECT: improved methods of synthesis, valuable medicinal properties of compounds and pharmaceutical composition.

17 cl, 17 tbl, 29 ex

 

The text descriptions are given in facsimile form.

1. Derivatives of 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-C]pyrimidine of the General formula

where R is furanyl, unsubstituted or substituted (C1-C6)-alkyl, halogen or nitro; pyrrolyl, unsubstituted or substituted (C1-C6)-alkyl; pyridyl, phenyl, unsubstituted or substituted by halogen; or (C4-C6)-cycloalkenyl;

X means (C2 -C6-alkylene or-C(O)CH2-;

Y represents-N(R2)CH2CH2N(R3)-, -Och2CH2N(R2)-, where R2and R3independently selected from the group comprising hydrogen and (C1-C6)-alkyl;

-O-, -S-, -CH2S-, -(CH2)2-NH - or

where Q means

or

m and n independently equals 2-3;

R4means hydrogen and (C1-C6)-alkyl, or two substituent R4at the same carbon atom form a group =O;

Z means R5-phenyl, where R5means from 1 to 5 substituents independently selected from the group comprising hydrogen, halogen, (C1-C6)-alkyl, hydroxyl, (C1-C6-alkoxy, -CN, di-((C1-C6)-alkyl)-amino, -CF3, -OCF3, acetyl, -NO2, hydroxy-(C1-C6-alkoxy, (C1-C6)-alkoxy-(C1-C6-alkoxy, di-((C1-C6)-alkoxy) (C1-C6-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkoxy-(C1-C6-alkoxy, carboxy-(C1-C6-alkoxy, (C1-C6-alkoxycarbonyl-(C1-C6-alkoxy, (C 3-C6-cycloalkyl-(C1-C6-alkoxy, di-((C1-C6)-alkyl)-amino-(C1-C6-alkoxyl, morpholinyl, (C1-C6)-alkyl-SO2-, (C1-C6)-alkyl-SO-(C1-C6-alkoxyl, tetrahydropyranyloxy, (C1-C6-alkylsulphonyl-(C1-C6-alkoxy, (C1-C6-alkoxycarbonyl, (C1-C6)-alkylcarboxylic-(C1-C6-alkoxyl, -SO2NH2phenoxyl,

where R2has the above value, the radical of the formula

or adjacent substituents R5together are-O-CH2-O-, -O-CH2-CH2-O-, -O-CF2-O-, or-O-CF2-CF2-O -, and form a loop together with the carbon atoms to which they are attached;

phenyl-(C1-C6)-alkyl, unsubstituted or substituted by halogen or (C1-C6-alkoxyl on the phenyl fragment;

diphenylmethyl;

heteroaryl, selected from the group comprising a pyridyl, unsubstituted or substituted (C1-C6)-alkyl, CF3or halogen; pyrimidinyl, unsubstituted or substituted (C1-C6)-alkyl, (C1-C6-alkoxyl, CF3, halogen or amino; pyrazinyl, benzopyranyl or benzimidazolyl;

R6-C(O)-, R6-SO2-, R6-OC(O)-,

where R6means (C1-C6)-alkyl, phenyl, unsubstituted or substituted (C1-C6)-alkyl, halogen or (C1-C6-alkoxyl; phenyl-(C1-C6)-alkyl, unsubstituted or substituted by halogen or (C1-C6-alkoxyl; thienyl, pyridyl, (C3-C6-cycloalkyl, (C1-C6)-alkyl-OC(O)-NH-(C1-C6)-alkyl-, di((C1-C6)-alkyl)-aminomethyl or

R7-N(R8)-C(O)- or R7-N(R8)-C(S)-, where R7means (C1-C6)-alkyl, phenyl-(C1-C6)-alkyl or phenyl, unsubstituted or substituted by halogen;

R8means hydrogen;

or R7and R8together represent -(CH2)p-A-(CH2)qwhere p and q are independently 2 or 3 and a represents-O-, and form a loop together with the nitrogen atom to which they are attached;

the radical of the formula

phenyl-CH(OH) -, or phenyl-C(=NOR2)-, where R2has the above values;

or if Q means

Z also means phenylamino or pyridylamino;

provided that when Y represents a group-O-, then Z may not mean b is silovoy group;

or Z and Y together imply

or its N-oxide,

where R9means hydrogen or (C1-C6-alkoxy; and R10means hydrogen;

where R10means halogen;

where R10means hydrogen, (C1-C6-alkoxyl, -OCF3or-S(O)0-2(C1-C6)-alkyl;

where R11means H, (C1-C6)-alkyl, phenyl, benzyl, (C2-C6)-alkenyl, (C1-C6)-alkoxy-(C1-C6)-alkyl;

and their pharmaceutically acceptable salts.

2. Derivatives of 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-C]pyrimidine according to claim 1, where R is furanyl, unsubstituted or substituted (C1-C6)-alkyl, halogen or nitro.

3. Derivatives of 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-C]pyrimidine according to claim 1, where X means (C2-C6-alkylen.

4. Derivatives of 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-C]pyrimidine according to claim 1, where the Y means

5. Derivatives of 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-C]pyrimidine according to claim 4, where Q means

or

and m and n equal to 2, a R4means N.

6. Derivatives of 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-C]pyrimidine according to claim 1, where Z means R5-phenyl, where R5has the above values; heteroaryl, selected from the group comprising a pyridyl, unsubstituted or substituted (C1-C6)-alkyl, CF3or halogen, pyrimidinyl, unsubstituted or substituted (C1-C6)-alkyl, (C1-C6-alkoxyl, CF3, halogen or amino, pyrazinyl, benzopyranyl or benzimidazolyl; R6-C(O)- or R6-SO2-where R6has the above values.

7. Derivatives of 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-C]pyrimidine according to claim 6, where R5means H, halogen, (C1-C6)-alkyl, (C1-C6-alkoxy, hydroxy-(C1-C6-alkoxy or (C1-C6)-alkoxy-(C1-C6-alkoxyl; heteroaryl, selected from the group comprising a pyridyl, unsubstituted or substituted (C1-C6)-alkyl or halogen, pyrimidinyl, unsubstituted or substituted (C1-C6)-alkyl, (C1-C6-alkoxyl or halogen, and R6means phenyl, nezam the seal or substituted (C 1-C6)-alkyl, halogen or (C1-C6-alkoxyl.

8. Derivatives of 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-C]pyrimidine according to claim 1, where x is the group-CH2-CH2-, and R and Z-Y are as indicated in the table below:

Z-Y-R

9. Derivative of 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-C]pyrimidine according to claim 1, having the formula

10. Derivative of 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-C]pyrimidine according to claim 1, having the formula

11. Pharmaceutical composition having activity of the receptor antagonist of the adenosine A2Acontaining the active ingredient and pharmaceutically acceptable carrier, wherein the active substance contains a compound according to claim 1 in a therapeutically effective amount.

12. The pharmaceutical composition according to claim 11, characterized in that it further comprises 1-3 other agents suitable for the treatment of Parkinson's disease.

13. The use of compounds according to claim 1 for the preparation of drugs for the treatment of depression, cognitive disorders, neurodegenerative diseases or stroke.

14. The application indicated in paragraph 13, and in the case of preparation of medicines for the treatment of neurodegenerative diseases, representing Parkinson's disease, to omnitele use 1-3 other agents, suitable for the treatment of Parkinson's disease.

15. The method of obtaining the intermediate 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-C]pyrimidine of formula II

where R is furanyl, unsubstituted or substituted (C1-C6)-alkyl, halogen or nitro; pyrrolyl, unsubstituted or substituted (C1-C6)-alkyl; pyridyl, unsubstituted or substituted by halogen; or (C4-C6)-cycloalkenyl;

in which the compound of formula IX

where R has the above meaning,

is subjected to a dehydration rearrangement.

16. The method according to item 15, wherein the compound of formula IX is obtained by (1) the interaction of 2-amino-4,6-dihydroxypyrimidine formula VI

with POCl3in dimethylformamide,

(2) the interaction of the obtained 2-amino-4,6-dichloropyrimidine-5-carboxaldehyde formula VII

with a hydrazide of the formula H2N-NH-C(O)-R, where R is specified in clause 15 of the value

(3) and the interaction of the obtained product of formula VIII

where R is specified in clause 15 of the value, hydrazinehydrate.

17. The method of obtaining the intermediate 7-bromoalkyl-5-amino-2-(R-substituted)-Pirat is about-[4,3-e]-1,2,4-triazolo[1,5-C]pyrimidine of formula IIIa

where R is furanyl, unsubstituted or substituted (C1-C6)-alkyl, halogen or nitro; pyrrolyl, unsubstituted or substituted (C1-C6)-alkyl; pyridyl, unsubstituted or substituted by halogen; or (C4-C6)-cycloalkenyl;

in which (1) the chloride of the formula VIII

where R has the above meaning,

subjected to interaction with hydroxyethylhydrazine formula HO-(CH2)r-NHNH2where r is 2-6,

(2) the resulting compound of formula X,

where R has the above meaning,

is subjected to a dehydration rearrangement with receiving tricyclic intermediate of formula XI

where R has the above meaning,

(3) translated into bromide of the formula IIIa.



 

Same patents:

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

16 cl, 2 tbl

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7 cl, 1 dwg, 24 ex

FIELD: organic chemistry, medicine.

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EFFECT: valuable medicinal properties of derivatives.

10 cl, 6 sch, 41 ex

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EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

13 cl, 1 tbl, 67 ex

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EFFECT: valuable properties of compound.

1 ex

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

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EFFECT: improved preparing method and treatment, valuable properties of compounds.

20 cl, 5 tbl, 149 ex

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< / BR>
where Z denotes a group of General formula II

< / BR>
where A, B, X, Z, R1-R10have the meanings indicated in the claims, as well as the way they are received and drug based on these compounds

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EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.

6 tbl, 82 ex

FIELD: pharmaceutical industry and technology, pharmacy, medicine, phytotherapy.

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EFFECT: improved preparing method.

5 tbl, 2 dwg, 1 ex

FIELD: medicine.

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EFFECT: enhanced effectiveness in reducing static and motor speech functions disorders and motor and emotional disorders.

8 tbl

FIELD: medicine, phytotherapy, pharmaceutical industry, pharmacy.

SUBSTANCE: invention proposes an agent possessing the nootropic anti-hypoxic activity. Agent represents common dropwort (Filipendula vulgaris Moech) above-ground part extract and elicits the nootropic and anti-hypoxic activity. Common dropwort (Filipendula vulgaris Moech) above-ground part extract is effective as the nootropic and anti-hypoxic agent.

EFFECT: valuable medicinal properties of agent.

2 tbl

FIELD: medicine, neurology, psychiatry.

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EFFECT: higher efficiency of therapy.

2 ex, 3 tbl

FIELD: organic chemistry, medicine, pharmacy.

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EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.

4 cl, 4 sch, 13 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to using compounds of the general formula (I): and their pharmaceutically acceptable acid-additive salts. Compounds are used for preparing medicinal agents used in treatment diseases and state associated with system of adenosine receptors A2A, such as Alzheimer's disease, Parkinson's diseases, Huntington's syndrome, schizophrenia, anxiety state, pain, depression, narcomania to such substances as amphetamine, cocaine, opioides, ethyl alcohol, nicotine, cannabinoids, or in treatment of hypoxia, ischemia, epileptic attack. Also, proposed compounds exert neuroprotective effect and can be used as sedative, antipsychotic or anti-epileptic agents.

EFFECT: valuable medicinal properties of compounds.

18 cl, 1 tbl, 49 ex

FIELD: organic chemistry, steroids.

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

30 cl, 2 tbl, 5 dwg, 16 ex

FIELD: medicine, phytotherapy, pharmaceutical industry.

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EFFECT: valuable medicinal properties of agent.

2 tbl

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of pyridineamides of the general formula (I): wherein one among X or Y means -N= and another means -CR7=; R1, R2, R3, R5, R6 and R7 mean independently hydrogen atom or (C1-C6)-alkyl; R4 means halogen-(C1-C6)-alkyl or unsubstituted phenyl or phenyl substituted with one or some substitutes chosen from group consisting of (C1-C6)-alkyl, halogen atom, halogen-(C1-C6)-alkyl, (C1-C6)-alkoxy-group and cyano-group, and to their pharmaceutically acceptable salts. Indicated compounds possess inhibitory effect with respect to monoaminoxidase B activity and can be used as a medicinal agent in treatment of diseases mediated by monoaminoxidase B inhibitors, in particular, Alzheimer's disease or Parkinson's disease or feeble-mindedness.

EFFECT: valuable medicinal properties of compounds and drug.

12 cl, 1 tbl, 16 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention describes a combination containing: (a) inhibitor of signal transduction chosen from inhibitor of tyrosinase receptor PDGF (thrombocyte growth factor) and active substance that decreases activity of epidermal growth factor (EGF), and (b) derivative of epotilone of the formula (I) given in the invention description wherein A represents oxygen atom (O) or ntn wherein rn means hydrogen atom or (lower)-alkyl; R means hydrogen atom or (lower)-alkyl; Z means O or a bond, and optionally at least one pharmaceutically acceptable carrier. Also, invention relates to a combination designated for simultaneous, separated or successive using, in particular, for the development retention or treatment of proliferative disease, to a pharmaceutical composition comprising such combination, using such combination in preparing a drug designated for the development retention or treatment of proliferative diseases, package or product containing such combination used as a combined medicinal agent, and to a method for treatment of warm-blooded animal. The combination exceeds effect of each components of its.

EFFECT: enhanced and valuable medicinal properties of combination and pharmaceutical composition.

14 cl, 2 ex

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