RussianPatents.com

Polymorphic modification in n-{5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-2-fluoro-phenyl}-n-methyl-acetamide (versions), containing it pharmaceutical composition (versions), medication, method of obtaining said polymorphic modification (versions) and method of treatment and/or prevention of nervous disorders. RU patent 2413729.

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention describes novel polymorphic modification N-{5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-2-fluoro-phenyl}-N-methyl-acetamide, methods of its obtaining, its application as medication, its application for preparation of medication and pharmaceutical compositions, including novel polymorphic modification.

EFFECT: obtaining novel polymorphic modification for preparation of medication and pharmaceutical compositions.

30 cl, 2 tbl, 24 ex, 7 dwg

IPC classes for russian patent Polymorphic modification in n-{5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-2-fluoro-phenyl}-n-methyl-acetamide (versions), containing it pharmaceutical composition (versions), medication, method of obtaining said polymorphic modification (versions) and method of treatment and/or prevention of nervous disorders. RU patent 2413729. (RU 2413729):

C07D487/04 - Ortho-condensed systems

A61P25/22 - Anxiolytics

A61P25/20 - Hypnotics; Sedatives

A61P25/08 - Antiepileptics; Anticonvulsants

A61K31/519 -

Another patents in same IPC classes:

Pyrazole derivatives and use thereof as receptor tyrosine kinase inhibitors / 2413727
Present invention relates to novel pyrazole derivatives of formula (I) or pharmaceutically acceptable salts thereof, having tyrosine kinase Trk inhibiting properties and used for treating or preventing malignant growths accompanied by high level of Trk, to a method of producing said derivatives, use thereof to prepare a medicinal agent, pharmaceutical compositions based on said derivatives, a method of inhibiting Trk activity and a method of obtaining antiproliferative action. where A denotes a single bond or C1-2alkylene; where the said C1-2alkylene can be optionally substituted with one R22; ring C is a phenyl or a 5-6-member heterocyclic ring with 1-2 heteroatoms selected from N or S. Values of R1-R7, R22 and n are given in the formula of invention.

Acetylenyl-pyrazole-pyrimidine derivatives as mglur2 antagonists / 2412943
Invention relates to novel acetylenyl-pyrazole-pyrimidine derivatives of general formula (I), having mGluR2 (metabotropic glutamate receptor) antogonist properties). In compounds of general formula (I): either E and J denote N, G denotes C and L denotes N, M denotes CH, or M denotes N, L denotes CH; or L and G denote N, E denotes C, and J and M denote CH; or J, G and L denote N, E denotes C, and M denotes CH; or E and L denote N, J and M denote CH, and G denotes C; R1 denotes H, halogen, CF3, CHF2 or C1-6alkyl; R2 denotes H, halogen, C1-6-alkyl, C1-6-alkoxy, CF3 or CHF2, wherein R1=R2≠H; R3 denotes H; -C(CH3)2OH; linear C1-4-alkyl or C3-4-cycloalkyl, which are possibly substituted with one or more substitutes selected from a group comprising 1-3 F and 1-2 OH; A is selected from a group comprising phenyl or a 5- or 6-member heteroaryl having in the ring 1-2 heteroatoms selected from nitrogen, sulphur or nitrogen and sulphur in the 5-member ring, and 1-2 nitrogen atoms i the 6-member ring, and possibly substituted with 1-3 Ra; Ra denotes halogen; hydroxy; cyano; CF3; NReRf; C1-C6-alkyl, possibly substituted amino or hydroxy; ; C1-6-alkoxy; C3-4-cycloalkyl; CO-NRbRc, SO2-NRbRc; or SO2-Rd-; Rb and RC can be identical or different and are selected from a group comprising H; normal or branched C1-6-alkyl, possibly substituted with one or more substitutes selected from a group comprising F, cyano, hydroxy, C1-6-alkoxy, -NH-C(O)-O-C1-6-alkyl, amino, (C1-6-alkyl)amino, di(C1-6-alkyl)amino, heterocycloalkyl having 6 ring atoms, from which 1-2 heteroatoms are selected from nitrogen or nitrogen and oxygen, or a 6-member heteroaryl with one nitrogen heteroatom in the ring; or a 6-membeer heteroaryl with one nitrogen heteroatom in the ring; or Rb and Rc, together with the nitrogen atom with which they are bonded, can form a heterocyclic ring having 6 members in the ring, from which 1-2 atoms are selected from nitrogen and/or oxygen, and which can be substituted with C1-6-alkyl; Rd denotes OH or C1-6-alkyl; Re and Rf denote H, C1-6-alkyl, possibly substituted hydroxy, -C(O)- C1-6-alkyl; S(O)2-C1-6-alkyl.

Salts of 9-(2-morpholinoethyl)-2-(4-fluorophenyl)imidazo [1,2-a]benzimidazole and salts of 9-aminoethyl-substituted -(4-fluorophenyl)imidazo [1,2-a]benzimidazole, having analgesic action / 2412187
Invention relates to novel compounds of the 2,9-disubstituted imidazo[1,2-a]benzimidazole family, specifically to water-soluble salts of 9-aminoethyl-substituted 2-(4-fluorophenyl)imidazo[1,2-a]benzimidazole of general formula I:

Pyrazolepyrimidines / 2412186
Compounds can be used to treat tumourous diseases, such as solid tumours, breast, lung, large intestine or prostate gland tumours. In compounds of formula

Novel piperazine compound and use thereof as hcv polymerase inhibitor / 2412171
Invention relates to a compound of formula [I-D1] or pharmaceutically acceptable salt thereof,

Compounds and compositions as proteinkinase inhibitors / 2411242
Invention refers to new compounds of formula I and to their pharmaceutically acceptable salts exhibiting inhibitory activity in relation to kinases chosen from Abl, Bcr-Abl, Bmx, BTK, b-RAF, c-RAF, CSK, cSRC, Fes, FGER3, Elt3, 1KKα, 1KKβ, JNK1α1, JNK2α2, Lck, Met, MKK4, MKK6, p70S6K, PAK2, PDGFRα, PKA, PKCα, PKD2, ROCK-II, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SAPK4, SGK, Syk, Tie2 and TrkB. In compounds of formula I , n is equal to 1, m is equal to 0, Y1 is chosen from N and CR5, and R5 represents hydrogen, Y2 represents O, R1 represents hydrogen, R2 is chosen from hydrogen and C1-C6alkyl, R3 is chosen from a group including hydrogen, C1-C6alkyl, C1-C6alkoxy, R4 is chosen from NR5C(O)R6 and -C(O)NR5R6 where R5 is chosen from hydrogen and C1-C6 alkyl, and R6 represents phenyl optionally substituted with 1-3 radicals chosen of a group including NR3R3, halogen-substituted C1-C6alkyl, C5-C6heteroaryl(C0-C4)alkyl where heteroaryl contains 1-2 heteroatoms chosen from N and O, C5-C6heterocyclo(C0-C4)alkyl, where heterocyclyl contains 1-2 heteroatoms of N, and C5-C6heterocyclo(C0-C4)alkoxy where heterocyclyl contains 1-2 heteroatoms of N, and any heteroaryl or heterocyclyl contained in R6 is optionally substituted by 1-3 radicals independently chosen from a group including C1-C6alkyl and hydroxy(C1-C6)alkyl.

1-(2-isopropoxyethyl)-2-thioxo-1,2,3,5-tetrahydro-pyrrolo[3,2-d]pyrimidin-4-one and pharmaceutically acceptable salts thereof / 2409578
Invention relates to a novel chemical compound - 1-(2-isopropoxyethyl)-2-thioxo-1,2,3,5-tetrahydro-pyrrolo [3,2-d]pyrimidin-4-one and pharmaceutically acceptable salts thereof, a pharmaceutical composition containing said compounds and use thereof. Disclosed compound has myeloperoxidase enzyme inhibiting properties.

Triazole derivatives / 2409570
Described are novel derivatives of genera formula (1) (where A denotes an oxygen or sulphur atom, -CH2- or -NH- group; R1 denotes C1-6alkyl group, possibly substituted ; R1A denotes a hydrogen atom or a C1-6 alkyl group; or these two radicals together with a carbon atom to which they are bonded form a cyclic C3-6 alkyl group; R2 denotes a C1-6 alkyl group or a C3-6 cycloalkyl group; R3 denotes an aryl group or a heteroaryl group, which can be substituted; R4 denotes a hydrogen atom; R5 denotes C1-6 alkyl group, aryl or heteroaryl group, which can be substituted), a pharmaceutical composition containing said derivatives and intermediate compounds. Said compounds (1) can inhibit bonding between SIP and its receptor Edg-1 (SIP1).

Pyrazolone derivatives / 2407737
Invention relates to compounds of formula

Imidazopyrazines as tyrosine kinase inhibitors / 2405784
Present invention refers to new imidazopyrazines of formula where Q1 and R1 have the values specified in the patent claim, and to their pharmaceutically acceptable salts showing IGF-1R enzyme inhibiting activity and applicable for treatment and/or prevention of various diseases and conditions which are sensitive to tyrosine kinase inhibition.

Anti-vomit nk-1 antagonist metabolites / 2404969
Invention relates to compounds of general formula (I) , where R is methyl and R1 is 4-methyl-oxy-piperazin-1-yl; or R is CH2OH and R1 is 4-methyl-piperzin-1-yl or 4-methyl-4-oxy-piperazin-1-yl; and to pharmaceutically acceptable acid addition salts thereof, as well as to a medicinal agent based on said compounds, having NK-1 receptor antagonist activity and to use of said compounds in treating NK-1 receptor associated diseases.

Substituted 8-sulphonyl-2,3,4,5-tetrahydro-1h-gamma-carbolines, ligands, pharmaceutical composition, synthesis method and use thereof / 2404180
Invention relates to novel substituted 8-sulphonyl-2,3,4,5-tetrahydro-1H-γ-carbolines of general formula 1 or pharmaceutically acceptable salts thereof, which are ligands with a wider range of simultaneous activity towards alpha adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors, sigma receptors, norepiniphrine receptors and serotonin receptors. In compounds of general formula 1 R1 is an amino group substitute selected from hydrogen; C1-C3alkyl optionally substituted with phenyl; C1-C4alkyloxycarbonyl; R2 is a cyclic system substitute selected from hydrogen, C1-C3alkyl optionally substituted with phenyl, pyridin-(3- or 4-yl), (6-methylpyridin-3-yl); C1-C3alkenyl substituted with phenyl; or optionally substituted phenylsulphonyl; R3 is an optionally halogen-substituted phenyl, six member aromatic azaheterocycle, mono- or di-C1-C3alkylamino group, phenylamino group which is optionally substituted with halogen atoms on the phenyl ring, or a substituted six member azaheterocycle containing an additional nitrogen atom, substituted with C1-C3alkyl.

Diarylmetyhylpyperazine derivatives, their obtaining and application / 2404172
There are described compound of formula, its pharmaceutically acceptable salt or their mixture, enentiomerically pure 4-{(R)-(3-aminophenyl)[4-(4-fluorobenzyl)pyperazin-1-yl]-N,N-diethylbenzamide or its pharmaceutically acceptable salt. Also described are method of anxiety therapy, method of pain therapy and method of depression therapy in animal.

Substituted 4-phenyltetrahydroisoquinolines, preparation method, application as medicinal agents, and also medicinal agents containing them / 2398766
Invention refers to new compounds of formula I , where: R1, R2, R3 and R4 independently from each other mean hydrogen, F, CI, Br, I; R5 designates hydrogen, alkyl with 1, 2, 3, 4, 5 or 6 C atoms, or cycloalkyl with 3, 4, 5 or 6 C atoms; R6 designates hydrogen; R7 and R8 independently from each other mean hydrogen, W means CrH2r or CsH2S-2; and one or more CH2-groups in C2H2r and CsH2s-2 can be substituted with NR17, oxygen or S; R17 means hydrogen, alkyl with 1, 2, 3 or 4 C atoms; r means 1, 2, 3, 4, 5 or 6; s means 2, 3 or 4; X designates-with C(O)- or -S(O)2-; Z means -C(O)- or a bond; and also to their pharmaceutically acceptable salts and trifluoroacetates. The invention also concerns application of the compounds of formula I, and also to a pharmaceutical composition.

Anxiolytic and cerebroprotective agent reducing inclination to alcohol / 2393855
Invention refers to medicine, particularly to pharmacology and concerns application of derivatives of gamma-aminobutyric acid in the form of 4-amino-3-phenyl butane acid salts of general formula

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

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 / 2384581
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.

4-(sulphanilpyrimidine-4-ylmethyl)morpholine derivatives as gaba-receptor ligands for treating anxiety, depression and epilepsy / 2382033
Invention refers to compound of formula I wherein X represents -S- or -NH-; R1 represents C1-12alkyl, C2-12alkenyl, phenyl C1-12alkel, phenyl C2-12alkenyl or phenyl-O-C1-12alkyl and wherein said phenyl groups are optionally substituted with one or two assistants chosen from the group consisting of lower C1-7alkyl, C C1-7alkoxy and halogen C1-7alkyl; R2 represents hydrogen, lower C1-7alkyl or C3-6cycloalkyl; R3/R4 together with N-atom whereto attached, form nonaromatic 5,6-members heterocyclic ring system which optionally contains in addition to N-atom one additional heteroatom chosen from the group, consisting of O or N and where the ring system is optionally substituted group lower C1-7alkyl, lower C1-7alkoxy, -NR2, -CONR2; or R3/R4 together with N-atom whereto attached, can form heterocyclic ring system which contains at least two rings and which optionally contains one or two additional heteroatoms chosen from group, consisting of N and O; R represents hydrogen or lower C1-7alkyl; R5 represents hydrogen or lower C1-7alkyl; or to pharmaceutically acceptable additive salts with acid of this compound. The invention also concerns a medical product.

Quinoline as allosteric enhencer of gaba-b receptors / 2378256
Present invention relates to compounds of formula (I) , where R1 is hydrogen, C1-C7 alkyl; R2 is C1-C7 alkyl, aryl, C1-C7 haloalkyl or C3-C8 cycloalkyl; R3, R4 each independently represents hydrogen, halogen, C1-C7 alkoxy, C1-C7 alkylsuphonyl; R5 is hydrogen, halogen, C1-C7 alkyl, C1-C7 haloalkoxy, or aryloxy, or is -NR7R8, where R7 and R8 represent C1-C7 alkyls, or R7 and R8 together with the nitrogen atom to which they are bonded can form a 4-7-member heterocycloalkyl group, which can be substituted with one or more substitutes selected from a group consisting of halogen, C1-C7 alkyl, C1-C7 alkoxy, hydroxyl, phenyl and di(C1-C7)alkylamino; R6 is hydrogen or together with R5 can form a 5- or 6-member heterocycloalkyl group which can be substituted with one or more halogens; and their pharmaceutically acceptable salts of acid compound, except the range of compounds given in paragraph 1 of the formula of invention. The invention also relates to medicine based on said compounds, with activity of allosteric enhancer of GABA-B receptors and use of compounds of the formula to prepare medicines used in treating central nervous system disorders, including anxiety and depression.

Pharmaceutical composition based on ladasten / 2376986
Invention relates to field of medicine, in particular to pharmaceutics, and concerns pharmaceutical compositions, which contain as active substance therapeutically effective quantity of ladasten, and as target additives - starch, stearic acid and/or its salt or ludipress and stearic acid and/or its salt with definite ratio of said components. Composition is made in form of pills, contains optimal quantity of target additives, which allows to obtain easy swallowed pills. Pills meet all requirements of State Pharmacopoeia XI edition.

Substituted 3,5-diamino-4-sulfonyl-pyrazoles and 2-amino-3-sulfonyl-pyrazolo-[1,5-a]pyrimidines-antagonists of serotonin 5-ht<sub>6</sub> receptors, methods for their production and use

Substituted 3,5-diamino-4-sulfonyl-pyrazoles and 2-amino-3-sulfonyl-pyrazolo-[1,5-a]pyrimidines-antagonists of serotonin 5-ht₆ receptors, methods for their production and use / 2376291
Invention is related to antagonists of serotonin 5-HT6 receptors of common formula 1 and their pharmaceutically acceptable salts and/or hydrates, pharmaceutical compositions, dosage forms and methods of production. Invention also includes new compounds of formula 1.1. In formulae 1 and 1.1 , Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur and heteroatom; R1 represents atom of hydrogen, unnecessarily substituted C1-C5 alkyl; Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur as heteroatom; R1 represents atom of hydrogen, which is unnecessarily substituted C1-C5 alkyl; R2 1,R2 2, R3 1, R3 2 independently from each other represent atom of hydrogen or substituent of aminogroup, selected from unnecessarily substituted C1-C4 alkyl, unnecessarily substituted phenyl, or R3 1 and R3 2 together with atom of nitrogen, to which they are bound, create unnecessarily substituted saturated 6-member heterocycle, possibly containing atom of nitrogen in cycle; or R1 together with atom of nitrogen, to which it is bound, and R2 1 and R2 2 together with atom of nitrogen, to which they are bound, create substituted pyrimidine cycle. In formula 1.1 R4, R5 and R6 independently from each other represent atom of hydrogen, unnecessarily substituted C1-C3 alkyl or phenyl.

Application of lavandar oil for prevention and treatment of neorasthenia, somatoform disorder and other stress-induced diseases / 2406521
There is claimed method of prevention and treatment of neurasthenia, somatoform disorder of post-traumatic stress, in which patient intakes perorally lavender oil in form of capsule and means of the same purpose in form of capsule, which contains lavender oil, introduced perorally.