₆ receptors, methods of producing and using said compounds. RU patent 2384581.

RussianPatents.com

Substituted 2-amino-3-sulfonyl-tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines-antagonists of serotonin 5-ht₆ receptors, methods of producing and using said compounds. RU patent 2384581.

Substituted 2-amino-3-sulfonyl-tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines-antagonists of serotonin 5-ht<sub>6</sub> receptors, methods of producing and using said compounds. RU patent 2384581.

FIELD: chemistry.

SUBSTANCE: invention relates to novel antagonists of serotonin 5-HT₆ receptors - substituted 2-amino-3-sulfonyl-6,7,8,9-tetrahydro-pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines of general formula 1 and substituted 2-amino-3-sulfonyl-5,6,7,8-tetrahydro-pyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of general formula 2 or their pharmaceutically acceptable salts and/or hydrates, method of producing said compounds and pharmaceutical compositions, medicinal agents and treatment method. In compounds of formula 1 and general formula 2 , Ar is phenyl which is possibly substituted with halogen atoms, or a 6-member nitrogen-containing heteroaryl; R¹ is a hydrogen atom, C₁-C₃alkyl which is possibly substituted with phenyl, C₁-C₅alkoxycarbonyl; R² is a hydrogen atom, halogen or C₁-C₃alkyl; R₁ ³ and R₂ ³ are optionally identical substitutes selected from a hydrogen atom, optionally substituted C₁-C₃alkyl or R₁ ³ and R₂ ³ together with the nitrogen atom with which they are bonded form a nitrogen-containing 6-member saturated heteroaryl optionally substituted with C₁-C₅alkoxycarbonyl, where the said heteroaryl has 1-2 heteroatoms selected from nitrogen.

EFFECT: compounds can be used to prevent and treat diseases of the central nervous system, pathogenesis of which is associated with 5-HT₆ receptors for enhancing mental capacity.

14 cl, 3 tbl, 19 dwg, 16 ex

IPC classes for russian patent Substituted 2-amino-3-sulfonyl-tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines-antagonists of serotonin 5-ht₆ receptors, methods of producing and using said compounds. RU patent 2384581. (RU 2384581):

C07D471/14 - Ortho-condensed systems

A61P25/28 - for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

A61P25/24 - Antidepressants

A61P25/22 - Anxiolytics

A61P25/18 - Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

A61K31/519 -

Another patents in same IPC classes:

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Invention refers to method for prevention of mirtazapin sublimation from a pharmaceutical preparative form containing solid enantiomer pure form of mirtazapin, by making the preparative forms by addition of at least one pharmaceutically acceptable adjuvant to the solid form of mirtazapin enantiomer. The enantiomer pure form is pharmaceutically acceptable, nonsublumating and solid salt of S- or R-mirtazapin. There are also described nonsublumating salts of S-mirtazapin and the pharmaceutical preparative form of the latter.

Method of obtaining enantiomerically pure mirtazapine / 2352566
Invention relates to method of obtaining mirtazapine enantiomer, containing less than 10% of other enantiomer, which includes reaction of closing cycle of compound of formula , where X represents leaving group, said stage includes processing with acid, by means of which mirtazapine with enantiomer excess is obtained by closing cycle R- or S-enantiomer of formula (II) compound by processing with polyphosporic acid in absence of solvent or combination of polyphosphoric acid and N-methylpyrrolidinol or DMF.

Heterocyclel ester substituted imidazoquinolines / 2351598
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Quinolone analogues / 2349586
Present invention pertains to new compounds with formula (1): and to their pharmaceutical salts, where B, X, A or V are not present, if Z1, Z2, Z3 or Z4 respectively represent N, and independently H, halogen atom, azido, R2, CH2R2, SR2, OR2 or NR1R2, when Z1, Z2, Z3 or Z4 represent C. In each NR1R2, R1 and R2 together with N there can be formation of an optionally substituted piperidine, pyrrolidine, piperazine or morpholine ring. Z1 represents N and Z2, Z3 and Z4 represent C, or Z1 and Z3 represent N and Z2 and Z4 represent C. W together with N and Z form an optionally substituted thiazole, imidazole or pyrimidine ring, which is condensed with an optionally substituted ring, chosen from a group consisting of: or . U represents NR1R2, NR1-(CR1 2)n-NR3R4, where in NR3R4, R3 and R4 together with N there can be formation of an optionally substituted piperidine, pyrrolidine, piperazine or morpholine ring. R1 and R3 independently represent H or C1-6alkyl. Each R2 represents H or C1-10alkyl, each optionally substituted with a halogen atom, or C3-6cycloalkyl, aryl, heteroaryl or pyridine, pyrrolidine, piperazine or morpholine ring, where each ring is optionally substituted; or R2 is optionally substituted with piperidine, pyrrolidine, pyridine, piperazine, pyrazine, morpholine or benzimidazole. R2 represents H or C1-10alkyl. Each R5 represents a substitute in any position in ring W, and is H, OR2, amino, alkoxy, amido, halogen atom or cyano; or R5 represents C1-6alkyl, -CONHR1-, each optionally substituted with a halogen atom; or two adjacent R5 are linked with formation of a 5-6-member ring, an optionally substituted heterocyclic ring, chosen piperidine, pyrrolidine, piperazine or morpholine ring. n equals 1-6, and each optionally substituted part can be substituted with one or more halogens, OR2, NR1R2 , carbamate, C1-10alkyl, each optionally substituted with a halogen atom, C=O, cyano, nitro, COR2, NR2COR2, sulphonyl amides, NR2SOOR2; SR2, SOR2, COOR2, CONR2 2, OCOR2, OCOOR2 or OCONR2 2. The invention also relates to pharmaceutical compositions, to the method of suppressing proliferation of cells and/or weakening cell proliferative breakdown, to the method of reducing microbe titre and/or weakening microbe infection, to the method of inducing death of cells and/or inducing apoptosis, to compounds, chosen from a group, to pharmaceutical compositions, as well as to the method of producing compounds with formula (1).

Pyridopyrrolizine and pyridoindolizine derivatives / 2342386
Described are novel pyridopyrrolizine and pyridoindolizine derivatives of general formula I and their pharmaceutically acceptable salts and hydrates, where A is C1-3alkyl; Ar stands for naphtyl or phenyl optionally substituted with one or two groups, selected from halogen, C1-6alkyl or C1-6alkyl haloid; Q stands for COOH; one of X1, X2, X3 or X4 stands for nitrogen, others are independently selected from CH and C-Rg, where Rg stands for C1-6alkyl or S(O)nC1-6alkyl, where n=0, 2; Y1 stands for S or C(O); Y2 stands for (CRdRe)m, where Rd and Re - hydrogen, m is integer 1 or 2; R1, R2, R3 stands for hydrogen, pharmaceutical composition, containing them, and method of treatment of diseases, mediated by prostaglandin D2.

Benzamide derivatives as oxytocin agonists and vasopressin antagonists / 2340617
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Antitumor lamellarin analogs / 2328500
Invention relates to the novel compounds with the common formula III: where, if X is selected from the group containing NH and S, R1, R2, R3, R4, R5, R6, R7, R8 and R9, each independently is selected from the group containing H, OH, OR', substituted or unsubstituted aryl, where substitutes independently correspond to H, OH, C1-C12alkoxy; where, if X means O, R1, R2, R3, R4, R5, R6, R7 and R8, each independently, selected from the group containing H, OH, OR', SH, SR', SOR', SO2R', OSO2R', NHR', N(R') CO2R', OC(=O)R'; and R9 independently selected from the group containing H, OR', unsubstituted or substituted with aminogroup or halogen C2-C12 alkenyl, unsubstituted C2- C12 alkenyl, unsubstituted thienyl and halogen; where each of the R' groups are independently selected from the group containing H, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted aryl; where substitutes are independently selected from the group containing halogen, OH, CN, C1-C12 alkoxy, phenyl; and the dotted line represents the simple or double bind; or its pharmaceutically compatible salt or complex ether. Other novel lamellarin analogs are described.

Substituted pyrazoles, pharmaceutical composition based on thereof, using pharmaceutical composition and method for inhibition of cathepsin s activity / 2317988
Invention describes novel substituted pyrazoles of the general formula (I): wherein values of radicals Ar, Ar2, W, G, R5-R8, RZ and n are given in the invention claim. Also, invention relates to a pharmaceutical composition based on these compounds, using this pharmaceutical composition for manufacturing agent designated for treatment of asthma, and a method for inhibition of activity of cathepsin S. Compounds indicated above can be used in medicine.

Compound comprising 1-(2-methylpropyl)-1h-imidazo[4,5-c][1,5]naphthyridine-4-amine, pharmaceutical composition based on its and method for stimulation of cytokine biosynthesis in animal body / 2312867
Invention relates to compound comprising 1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridine-4-amine or pharmaceutically acceptable salt of this compound and pharmaceutical composition used for stimulation of biosynthesis of cytokine based on abovementioned compound Also, invention claims a method for stimulation of biosynthesis of cytokines in animal body involving administration in animal body of above described compound or its salt. Invention provides preparing a novel compound possessing useful biological properties.

Imidazo-condensed compounds and pharmaceutical composition containing thereof / 2310657
Invention describes novel imidazo-condensed compounds of the general formula (I): wherein Z represents nitrogen atom (N); Z1 represents N whein a bond between C5 and Z1 represents a simple bond, and Z1 represents carbon atom (C) when a bond between C5 and Z1 represents a double bond; R1 represents hydrogen atom; R2 represents (C1-C6)-alkyl, (C1-C6)-hydroxyalkyl, phenyl-(C1-C4)-alkyl substituted with halogen atom, ((C1-C4)-alkyl)-SO2, (C1-C6)-alkyl, (C5-C6)-cycloalkyl possibly substituted with hydroxy-group, phenyl substituted with halogen atom, heterocyclyl possibly substituted and chosen from group consisting of tetrahydropyranyl, (N-methylsulfonyl)piperidinyl or tetrahydro-1,1-dioxide-2H-thiopyranyl; A is absent or represents -O-; a bond between C5 and Z1 is a simple or double bond; a bond between C8 and C9 is a simple or double bond; Y represents phenyl substituted with halogen atom, or their pharmaceutically acceptable salts possessing inhibitory activity with respect to p38 MAP kinase, and pharmaceutical composition containing thereof. Proposed compounds can be used, for example, in treatment/or prophylaxis of such diseases as rheumatic arthritis, fever and reduced bone resorption.

Benzo[d] isoxazole-3 daao inhibitors / 2384574
Invention relates to novel compounds of formula IA and their pharmaceutically acceptable salts. Claimed compounds have inhibitory effect on DAAO. In formula IA , A denotes hydrogen; Z denotes O; R1 is selected from a hydrogen atom, hydroxy or methoxy; R2 is selected from a hydrogen atom, F, Cl, hydroxy, methoxy and methyl; or R1 is selected from a hydrogen atom, F, hydroxy and methoxy; and R2 is selected from a hydrogen atom, Cl, hydroxy, methoxy and methyl; R3 is selected from C1-C6alkyl, hydroxy, methoxy, halogen, cyano, CH2-CH2-phenyl and OCH2-phenyl; R4a is selected from C1-C6alkyl, hydroxy, methoxy and halogen. The invention also relates to use of compounds in which R3a denotes hydrogen, C1-C6alkyl, hydroxy, methoxy, halogen, cyano, CH2-CH2-phenyl, O-CH2-phenyl, NH-CO-O-CH2-phenyl, R4a denotes H, C1-C6alkyl, hydroxy, methoxy, halogen, NH-CO-O-CH2-phenyl, for making a medicinal agent.

Agent and method for prevention and treatment of patients with alzheimer's disease / 2384343
Method for prevention and treatment of the patients with Alzheimer's disease implies application of preparation "Semax 1% nasal drops" in a daily dosage 18-20 mg introduced 3 drops into each nasal passage 6-7 times a day.

6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines, having pde9a inhibition properties / 2383546
Invention relates to novel compounds of formula (I) and their pharmaceutically acceptable salts which have PDE9A inhibition properties. In formula (I) R1 represents alkyl with 1-8 carbon atoms or cycloalkyl with 5-6 carbon atoms which, if necessary, can have up to three substitutes independently selected from: alkyl with 1-6 carbon atoms, hydroxy, halogen and trifluoromethyl, where the alkyl with 1-6 carbon atoms, if necessary, can be substituted with 1-3 substitutes independently selected from halogen and trifluoromethyl, R2 represents phenyl or aromatic mono- or bicyclic heteroaryl with 5-10 atoms in the ring and up to 5 heteroatoms selected from: sulphur, oxygen and/or nitrogen, where phenyl is substituted with 1-3 substitutes, and the heteroaryl, if necessary, can be substituted with 1-3 substitutes in each case independently selected from: alkyl with 1-6 carbon atoms, alkoxy with 1-6 carbon atoms, trifluoromethyl, trifluoromethoxy, amino, hydroxyl and halogen.

Pharmaceutical composition in form of solution for injections of ethylmethylhydroxypyridine succinate and pyridoxin, method of its obtaining and method of treatment / 2383331
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Derivatives of tetrahydrocarbazoles, method of obtaining them and pharmaceutical compositions containing them / 2382770
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Novel chroman-2-one derivatives and use thereof as monoamine neuromediator reuptake inhibitors / 2382040
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Donepezil salts applicable for preparing pharmaceutical compositions / 2382032
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Morpholine type cinnamide derivative / 2381225
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Pharmaceutical composition of choline alphocerate expressing nootropic activity and cholinomimetic action, method for making thereof / 2380095
Invention concerns chemical-pharmaceutical industry, more specifically to a pharmaceutical composition expressing nootropic activity and cholinomimetic action. There is offered original pharmaceutical composition containing choline alphoscerate as an active ingredient in therapeutically effective amount and pharmaceutically acceptable carriers, differing that as pharmaceutically acceptable carriers it contains macrogol (polyethylene glycol 400) and povidone (Plasdone or collidone). There is also offered method for making thereof that enables making a high-yield end product. The pharmaceutical composition produced by the declared method exhibits minimum by-effects, improved bioavailability and prolonged storage stability.

Thiomorpholine compound and method for making thereof / 2379305
There is described thiomorpholine compound presented by formula (I) wherein the ring A represents benzene ring; the ring B represents benzene ring; R1 represents hydrogen atom, R2 represents C1-6-alkyl group; R3a and R3b are identical or different, each representing hydrogen atom or C1-6-alkyl group, and n represents an integer equal to 2, or its pharmaceutically acceptable salt. There is also described method for making the compound of formula (1), a pharmaceutical composition and application of the compound of formula (1) for making a medical product used for treatment and prevention of the disease chosen from inflammation, allergic diseases, pain, migraine, neuralgia, itch, cough, central nervous system diseases, alimentary organ diseases, nausea, vomiting and urological disorders.

Application of flibanserin for treating premenstrual and other sexual disorders in women / 2384333
Invention is related to application of therapeutically effective amount of flibanserin or its pharmacologically acceptable acid addition salts to produce a medicine for treating premenstrual disorders. The daily dosage of flibanserin is 0.1 to 400 mg a day.

Substituted 2-amino-3-sulfonyl-tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines-antagonists of serotonin 5-ht6 receptors, methods of producing and using said compounds. RU patent 2384581.

Substituted 2-amino-3-sulfonyl-tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines-antagonists of serotonin 5-ht₆ receptors, methods of producing and using said compounds. RU patent 2384581.