The use of derivatives of aryl (or heteroaryl) asolitarynote in the preparation of medicines for treating disorders mediated by an excess of substance p

 

Proposed: a tool based on the derivatives of aryl (or heteroaryl) asolitarynote (part of which was formerly used as analgesics) or their salts for inhibiting substance P in the treatment of Central nervous system disorders selected from the group of: anxiety, depression, schizophrenia, manic-depressive psychosis, sexual dysfunction, addiction to narcotic drugs, disorder cognitive abilities, locomotive disorders in mammals, including man, in particular, on the basis of ()-5-{-[2-(dimethylamino)ethoxy] benzyl} -1-methyl-1H-pyrazole or its salts. The invention expands the Arsenal of tools specified destination. 1 C.p. f-crystals, 12 tab.

Description text in facsimile form (see graphic part)and

Claims

1. Means for inhibiting substance P in the treatment of a disorder of the Central nervous system selected from the group of: anxiety, depression, schizophrenia, manic-depressive psychosis, sexual dysfunction, addiction to narcotic drugs, disorder cognitive abilities, locomotive disorders in mammals, https://img.russianpatents.com/img_data/72/727315.gif">

where AG denotes phenyl or thienyl radical, unsubstituted or optionally substituted by 1, 2 or 3 identical or different substituents selected from the group consisting of fluorine, chlorine, bromine, methyl, trifloromethyl and methoxy;

R1 denotes a hydrogen atom, tsiklogeksilnogo group, N-methylpiperidino group, phenyl group, vinyl group or1-C4is an alkyl group;

R2 denotes a hydrogen atom or di(C1-C4alkyl)amino(C2-C3alkyl), (C1-C2alkyl)azaheterocyclic(C2-C3alkyl) or azaheterocyclic(C2-C3alkyl);

Het denotes a heterocyclic nitrogen-containing five-membered ring which contains one to three nitrogen atoms, unsubstituted or optionally substituted by 1 or 2 identical or different substituents selected from the group consisting of fluorine, chlorine, bromine, C1-C12alkyl group, a benzyl radical, a cyano(C2-C3alkyl) radical, carboxylic(C2-C3alkyl) radical, methoxycarbonyl(C2-C3alkyl) radical, hydroxy(C2-C3alkyl) radical, amino(C2-C3alkyl) radical, a di(C1

or one of its physiologically acceptable salts.

2. Means under item 1, where the compound of General formula (I) selected from the group consisting of

[1] 2-{-[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-imidazole,

[2] 2-{4-chloro--[2-(dimethylamino)ethoxy]--methylbenzyl}-1-methyl-1H-imidazole,

[3] 2-{4-chloro--[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-imidazole,

[4] 2-{3-chloro--[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-imidazole,

[5] 2-{4-chloro--[2-(dimethylamino)ethoxy]--methylbenzyl}-1-methyl-1H-imidazole,

[6] 2-{4-fluoro--[2-(dimethylamino)ethoxy]--methylbenzyl}-1-methyl-1H-imidazole,

[7] 2-{-[2-(dimethylamino)ethoxy]--methyl-3-(trifluoromethyl)benzyl}-1-methyl-1H-imidazole,

[8] 2-{3-chloro--[2-(dimethylamino)ethoxy]--methylbenzyl}-1-methyl-1H-imidazole,

[9] 2-{3-chloro--[2-(dimethylamino)ethoxy]--propylbenzyl}-1-methyl-1H-imidazole,

[10] 1-butyl-2-{4-chloro--[2-(dimethylamino)ethoxy]--methyl-4-methoxybenzyl}-1-methyl-1H-imidazole,

[12] 2-{3-chloro--methyl--[2-(N-pyrrolidyl)ethoxy]benzyl}-1-methyl-1H-imidazole,

[13] 2-{-[2-(dimethylamino)ethoxy]--propyl-3,4,5-trimethoxybenzyl}-1-dodecyl-1H-imidazole,

[14] 1-butyl-2-{-[2-(dimethylamino)ethoxy]-4-(trifluoromethyl)benzyl}-1H-imidazole,

[15] 1-methyl-2-{-methyl--[2-(N-piperidyl)ethoxy]-3-(trifluoromethyl)benzyl}-1H-imidazol

[16] 2-{-cyclohexyl-3,4-dichloro--[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-imidazole,

[17] 2-{3,4-dichloro--[2-(dimethylamino)ethoxy]--propylbenzyl}-1-methyl-1H-imidazole,

[18] 2-{3,4-dichloro--[2-(dimethylamino)ethoxy]--methylbenzyl}-1-methyl-1H-imidazole,

[19] 2-{3,4-dichloro--[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-imidazole,

[20] 2-{4-chloro--[2-(dimethylamino)ethoxy]--methylbenzyl}-1-[2-(N-piperidyl)ethyl]-1H-imidazole,

[21] 2-{4-chloro--[2-(dimethylamino)ethoxy]-

[23] 2-{4-chloro--[2-(dimethylamino)ethoxy]--(N-methyl-4-piperidyl)benzyl}-1-methyl-1H-imidazole,

[24] 1-benzyl-2-{-[2-(N-benzyl-N-methylamino)ethoxy]-4-Chlorobenzyl}-1H-imidazol

[25] 2-{4-chloro--[2-(dimethylamino)ethoxy]--methylbenzyl}-7-methyl-6,7,8,9-tetrahydro-1H-imidazole[1,5-a][1,4]diazepin,

[26] 2-{4-chloro--[2-(dimethylamino)ethoxy]benzyl}-7-methyl-6,7,8,9-tetrahydro-1H-imidazole[1,5-a][1,4]diazepin,

[27] 1-butyl-5-{-[2-(dimethylamino)ethoxy]benzyl}-1H-pyrazole,

[28] 5-{-(4-chlorophenyl)--[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[29] 1-butyl-5-{-[2-(dimethylamino)ethoxy]-3,4,5-trimethoxybenzyl}-1H-pyrazole

[30] 1-butyl-5-{4-chloro--[2-(dimethylamino)ethoxy]--methylbenzyl}-1H-pyrazole,

[31] 5-{-[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[32] 5-{-[2-(dimethylamino)ethoxy]--methylbenzyl}-1-methyl-1H-pyrazole,

[33] 5-{-[2-(dimethylene the hydroxy]benzyl}-1H-pyrazole,

[35] 1-methyl-5-{-[2-(N-morpholinyl)ethoxy]benzyl}-1H-pyrazole,

[36] 5-{-[2-(dimethylamino)ethoxy]--methyl-3,4,5-trimethoxybenzyl}-1-methyl-1H-pyrazole,

[37] 4-bromo-5-{-[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[38] 1,3-dimethyl-5-{-[2-(dimethylamino)ethoxy]--methylbenzyl}-1H-pyrazole,

[39] 1,3-dimethyl-5-{-[2-(dimethylamino)ethoxy]benzyl}-1H-pyrazole,

[40] 5-{-[2-(dimethylamino)ethoxy]-2-methylbenzyl}-1-methyl-1H-pyrazole,

[41] 4-chloro-5-{4-chloro--[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[42] 5-{4-chloro--[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[43] 5-{3-chloro--[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[44] 5-{-[2-(dimethylamino)ethoxy]-4-methylbenzyl}-1-methyl-1H-pyrazole,

[45] 5-{2-chloro--[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[46] 1-methyl-5-{-[2-(N-piperidyl)ethoxy]benzyl}-1H-pyrazole,

[47] 1-methyl-5-{-[2-(N-propyl-2-piperidyl)ethoxy]benzyl}-1H-pyrazole,

<232D/chr/945.gif">-[2-(N-methyl-2-pyrrolidyl)ethoxy]benzyl}-1H-pyrazole,

[50] 5-{-[2-(diisopropylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[51] 1-methyl-5-{-[2-(N-methyl-2-piperidyl)ethoxy]benzyl}-1H-pyrazole,

[52] 2-{4-chloro--[3-(dimethylamino)propoxy]--methylbenzyl}-1-methyl-1H-imidazole,

[53] 2-{3-chloro--[3-(dimethylamino)propoxy]benzyl}-1-methyl-1H-imidazole,

[54] 2-{4-chloro--[3-(dimethylamino)propoxy]--active compounds}-1-methyl-1H-imidazole,

[55] 2-{-butyl-3-chloro--[3-(dimethylamino)propoxy]benzyl}-1-methyl-1H-imidazole,

[56] 2-{-cyclohexyl-4-chloro--[3-(dimethylamino)propoxy]benzyl}-1-methyl-1H-imidazole,

[57] 2-{-[3-(dimethylamino)propoxy]-4-fluoro--methylbenzyl}-1-methyl-1H-imidazole,

[58] 2-{-[3-(dimethylamino)propoxy]--methyl-3-(trifluoromethyl)benzyl}-1-methyl-1H-imidazole,

[59] 2-{2-chloro--[3-(dimethylamino)propoxy]--methylbenzyl}-1-methyl-1H-imidazole,

[60] 2-{3-chloro--[3-(dimethylamino)propoxy]--methyl-3,4,5-trimethoxybenzyl}-1-methyl-1H-imidazole,

[62] 2-{-[3-(dimethylamino)propoxy]--methyl-4-methoxybenzyl}-1-methyl-1H-imidazole,

[63] 2-{4-chloro--[3-(dimethylamino)propoxy]benzyl}-1-methyl-1H-imidazole,

[64] 2-{-[3-(dimethylamino)propoxy]-3,4,5-trimethoxybenzyl}-1-methyl-1H-imidazole,

[65] 2-{-[3-(dimethylamino)propoxy]--methyl-4-(trifluoromethyl)benzyl}-1-methyl-1H-imidazole,

[66] 2-{-[3-(dimethylamino)propoxy]-3-(trifluoromethyl)benzyl}-1-methyl-1H-imidazole,

[67] 2-{-[3-(dimethylamino)propoxy]-4-(trifluoromethyl)benzyl}-1-methyl-1H-imidazole,

[68] 2-{-[3-(dimethylamino)propoxy]-4-methoxybenzyl}-1-methyl-1H-imidazole,

[69] 2-{-butyl--[3-(dimethylamino)propoxy]-3-(trifluoromethyl)benzyl}-1-methyl-1H-imidazole,

[70] 1-butyl-2-{4-chloro--[3-(dimethylamino)propoxy]--methylbenzyl}-1H-imidazole,

[71] 1-butyl-2-{-butyl--[3-(dimethylamino)propoxy]-3,4,5-Tr is methylamino)propoxy]benzyl}-1H-imidazole,

[73] 1-butyl-2-{-butyl-2,4-dichloro--[3-(dimethylamino)propoxy]benzyl}-1H-imidazole,

[74] 1-butyl-2-{-[3-(dimethylamino)propoxy]-4-(trifluoromethyl)benzyl}-1H-imidazole,

[75] 2-{4-chloro--[3-(N-piperidyl)propoxy]benzyl}-1-methyl-1H-imidazole,

[76] 1-methyl-2-{-methyl--[3-(N-piperidyl)propoxy]-4-(trifluoromethyl)benzyl}-1H-imidazole,

[77] 2-{-butyl-2-chloro--[3-(dimethylamino)propoxy]benzyl}-1-methyl-1H-imidazole,

[78] 2-{-butyl-3,4-dichloro--[3-(dimethylamino)propoxy]benzyl}-1-methyl-1H-imidazole,

[79] 2-{3,4-dichloro--[3-(dimethylamino)propoxy]--methylbenzyl}-1-methyl-1H-imidazole,

[80] 2-{3,4-dichloro--[3-(dimethylamino)propoxy]benzyl}-1-methyl-1H-imidazole,

[81] 2-{-cyclohexyl-3,4-dichloro--[3-(dimethylamino)propoxy]benzyl}-1-methyl-1H-imidazole,

[82] 2-{4-chloro--[3-(dimethylamino)propoxy]--methylbenzyl}--[2-(N-piperidyl)ethyl]-1H-imidazole,

[who yl)-propyl]-1H-imidazole,

[84] 2-{4-chloro--[3-(dimethylamino)propoxy]--(N-methyl-4-piperidyl)benzyl}-1-methyl-1H-imidazole,

[85] 1-butyl-5-{-[3-(dimethylamino)propoxy]benzyl}-1H-pyrazole,

[86] 1-butyl-5-{4-chloro--[3-(dimethylamino)propoxy]--methylbenzyl}-1H-pyrazole,

[87] 5-{-[3-(dimethylamino)propoxy]benzyl}-1-methyl-1H-pyrazole,

[88] 5-{-[3-(dimethylamino)propoxy]--methylbenzyl}-1-methyl-1H-pyrazole,

[89] 1,3-Dimethyl-5-{-[3-(dimethylamino)propoxy]--methylbenzyl}-1H-pyrazole,

[90] 1,3-dimethyl-5-{-[3-(dimethylamino)propoxy]benzyl}-1H-pyrazole,

[91] 5-{-[3-(dimethylamino)propoxy]-2-methylbenzyl}-1-methyl-1H-pyrazole,

[92] 5-chloro-5-{4-chloro--[3-(dimethylamino)propoxy]benzyl}-1-methyl-1H-pyrazole,

[93] 1-methyl-5-{-[3-(N-piperidyl)propoxy]benzyl}-1H-pyrazole,

[94] 1-methyl-5-{-[3-(N-pyrrolidyl)propoxy]benzyl}-1H-pyrazole,

[95] 4-{4-chloro--[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[96] 4-{4-chloro--[2-(N-propyl-2-piperidyl)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[98] 4-{4-chloro--[2-(N-methyl-2-piperidyl)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[99] 4-{4-chloro--[2-(N-ethyl-2-piperidyl)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[100] 4-{4-chloro--[2-(diisopropylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[101] 4-{4-chloro--[2-(N-methyl-2-pyrrolidyl)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[102] 4-{-[3-(dimethylamino)propoxy]benzyl}-1-methyl-1H-pyrazole,

[103] 4-{4-chloro--[3-(N-morpholinyl)propoxy]benzyl}-1-methyl-1H-pyrazole,

[104] 4-{4-chloro--[3-(N-pyrrolidyl)propoxy]benzyl}-1-methyl-1H-pyrazole,

[105] 2-(-hydroxybenzyl)-1H-imidazole,

[106] 2-(4-chloro--hydroxybenzyl)-1H-imidazole,

[107] 2-(4-chloro--hydroxybenzyl)-1-methyl-1H-imidazole,

[108] 2-(3-chloro--hydroxybenzyl)-1-methyl-1H-imidazole,

[109] 2-(4-fluoro--hydroxybenzyl)-1-methyl-1H-imidazole,

[110] 2-[-hydroxy-3-(trifluoromethyl)benzyl]-1-methyl-1H-imidazole,

[111] 2-[-hydroxy-3-(trifluoromethyl)benzyl

[113] 2-(3,4-dichloro--hydroxybenzyl)-1-methyl-1H-imidazole,

[114] 1-butyl-2-[-hydroxy-4-(trifluoromethyl)benzyl]-1H-imidazole,

[115] 1-butyl-2-(3,4-dichloro--hydroxybenzyl)-1H-imidazole,

[116] 1-butyl-2-(4-chloro--hydroxybenzyl)-1H-imidazole,

[117] 1-butyl-2-(-hydroxy-3,4,5-trimethoxybenzyl)-1H-imidazole,

[118] 1-dodecyl-2-(-hydroxy-3,4,5-trimethoxybenzyl)-1H-imidazole,

[119] 2-(-butyl-3-chloro--hydroxybenzyl)-1-methyl-1H-imidazole,

[120] 2-(3-chloro--hydroxy--methylbenzyl)-1-methyl-1H-imidazole,

[121] 2-(4-chloro--hydroxy--methylbenzyl)-1-methyl-1H-imidazole,

[122] 2-[4-chloro--hydroxy--(N-methyl-4-piperidyl)benzyl]-1-methyl-1H-imidazole,

[123] 2-(4-chloro--ethyl--hydroxybenzyl)-1-methyl-1H-imidazole,

[124] 2-(-butyl-4-chloro--hydroxybenzyl)-1-methyl-1H-imidazole,

[125] 2-(-cyclohexyl-4-chloro--methylbenzyl)-1-methyl-1H-imidazole,

[127] 2-(-butyl-2-chloro--hydroxybenzyl)-1-methyl-1H-imidazole,

[128] 2-[-hydroxy--methyl-3-(trifluoromethyl)benzyl]-1-methyl-1H-imidazole,

[129] 2-[-butyl--hydroxy-3-(trifluoromethyl)benzyl]-1-methyl-1H-imidazole,

[130] 2-[-cyclohexyl--hydroxy-3-(trifluoromethyl)benzyl]-1-methyl-1H-imidazole,

[131] 2-[-hydroxy--methyl-4-(trifluoromethyl)benzyl]-1-methyl-1H-imidazole,

[132] 2-(4-fluoro--hydroxy--methylbenzyl)-1-methyl-1H-imidazole,

[133] 2-(-hydroxy--methyl-4-methoxybenzyl)-1-methyl-1H-imidazole,

[134] 2-(3,4-dichloro--hydroxy--methylbenzyl)-1-methyl-1H-imidazole,

[135] 2-(-butyl-3,4-dichloro--hydroxybenzyl)-1-methyl-1H-imidazole,

[136] 2-(-cyclohexyl-3,4-dichloro--hydroxybenzyl)-1-methyl-1H-imidazole,

[137] 2-(-�/chr/945.gif">-hydroxy--methylbenzyl)-1H-imidazole,

[139] 1-butyl-2-(-butyl-4-chloro--hydroxybenzyl)-1H-imidazole,

[140] 1-butyl-2-[4-chloro--hydroxy--(N-methyl-4-piperidyl)benzyl]-1H-imidazole,

[141] 1-butyl-2-(-butyl--hydroxy-3,4,5-trimethoxybenzyl)-1H-imidazole,

[142] 1-butyl-2-(-butyl-2-chloro--hydroxybenzyl)-1H-imidazole,

[143] 1-butyl-2-[-ethyl--hydroxy-3-(trifluoromethyl)benzyl]-1H-imidazole,

[144] 1-butyl-2-(-butyl-2,4-dichloro--hydroxybenzyl)-1H-imidazole,

[145] 2-(4-chloro--hydroxy--methylbenzyl)-1-[2-(N-piperidyl)ethyl]-1H-imidazole,

[146] 2-(4-chloro--hydroxy--methylbenzyl)-1-(3-dimethylaminopropyl)-1H-imidazole,

[147] 2-(-butyl--hydroxy-3,4,5-trimethoxybenzyl)-1-dodecyl-1H-imidazole,

[148] 1-benzyl-2-[-butyl--hydroxy-3-(trifluoromethyl)benzyl]-1H-im the azole,

[150] 1-(2-cyanoethyl)-2-(4-chloro--hydroxybenzyl)-1H-imidazole,

[151] 1-(3-aminopropyl)-2-(4-chloro--hydroxybenzyl)-1H-imidazole,

[152] 3-[2-(3-chlorine--hydroxybenzyl)-1H-imidazol-1-yl]propanoic acid,

[153] 2-(4-chloro--hydroxybenzyl)-1-(3-hydroxypropyl)-1H-imidazole,

[154] 3-[2-(3-chlorine--hydroxybenzyl)-1H-imidazol-1-yl]methylpropanoate,

[155] 2-(-hydroxybenzyl)-1-(3-hydroxypropyl)-1H-imidazole,

[156] 2-(-hydroxy-4-methylbenzyl)-1-(3-hydroxypropyl)-1H-imidazole,

[157] 2-(-hydroxy-4-methoxybenzyl)-1-(3-hydroxypropyl)-1H-imidazole,

[158] 2-(3,4-dichloro--hydroxybenzyl)-1-(3-hydroxypropyl)-1H-imidazole,

[159] 3-{2-(-hydroxybenzyl)-1H-imidazol-1-yl}methylpropanoate,

[160] 2-(4-chloro--hydroxybenzyl)-1-(4-hydroxybutyl)-1H-imidazole,

[161] 1-(3-cyanopropyl)-2-(4-chloro--hydroxybenzyl)-1H-imidazole,

[162] 4-[2-(4-chlorine--hydroxybenzyl)-1H-imidazol-1-yl]-butane acid,

[163] 4-[2-(4-chlorine--)-1-�="https://img.russianpatents.com/chr/945.gif">-hydroxybenzyl)-1-methyl-1H-pyrazole,

[166] 5-(-hydroxy-3,4,5-trimethoxybenzyl)-1-methyl-1H-pyrazole,

[167] 1-butyl-5-(-hydroxy-3,4,5-trimethoxybenzyl)-1H-piraso,

[168] 4-bromo-5-(-hydroxybenzyl)-1-methyl-1H-pyrazole,

[169] 5-[-(4-chlorophenyl)--hydroxybenzyl]-1-methyl-1H-pyrazole,

[170] 1-butyl-5-(4-chloro--hydroxy--methylbenzyl)-1H-pyrazole,

[171] 5-(-hydroxy--methylbenzyl)-1-methyl-1H-pyrazole,

[172] 5-(-hydroxy--methyl-3,4,5-trimethoxybenzyl)-1-methyl-1H-pyrazole,

[173] 1,3-dimethyl-5-(-hydroxy--methylbenzyl)-1H-pyrazole,

[174] 1-butyl-5-(-hydroxy--vinylbenzyl)-1H-pyrazole,

[175] 1-butyl-5-(4-chloro--hydroxy--vinylbenzyl)-1H-pyrazole,

[176] 4-chloro-5-(-hydroxybenzyl)-1-methyl-1H-pyrazole,

[177] 5-(-hydroxy-2-methylbenzyl)-1-methyl-1H-pyrazole,

[178] 5-(3-chloro--hydro] 5-(2-chloro--hydroxybenzyl)-1-methyl-1H-pyrazole,

[181] 5-(-hydroxy-4-methoxybenzyl)-1-methyl-1H-pyrazole,

[182] 5-{-[2-(dimethylamino)ethoxy]-2-thienylmethyl}-1-methyl-1H-pyrazole,

[183] citrate 5-{-[2-(dimethylamino)ethoxy]-2-thienylmethyl}-1-methyl-1H-pyrazole,

[184] 5-{-[2-(dimethylamino)ethoxy]-3-thienylmethyl}-1-methyl-1H-pyrazole,

[185] 2-{-[2-(dimethylamino)ethoxy]-2-thienylmethyl}-1-methyl-1H-imidazol

[186] 5-{-[2-(dimethylamino)ethoxy]-3-methyl-2-thienylmethyl}-1-methyl-1 H-pyrazole,

[187] 5-{-[2-(dimethylamino)ethoxy]-5-methyl-2-thienylmethyl}-1-methyl-1H-pyrazole,

[188] 5-{5-bromo--[2-(dimethylamino)ethoxy]-2-thienylmethyl}-1-methyl-1H-pyrazole,

[189] 5-{4-bromo--[2-(dimethylamino)ethoxy]-2-thienylmethyl}-1-methyl-1H-pyrazole,

[190] 5-{-[2-(dimethylamino)ethoxy]--methyl-2-thienylmethyl}-1-methyl-1H-pyrazole,

[191] citrate 5-{-[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[192] (±)-5-{-[2-(dimethylamino)-1-(methyl)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[193] (±)-5-{

[195] (-)-5-{-[2-(dimethylamino)ethoxy]-2-thienylmethyl}-1-methyl-1H-pyrazole,

[196] citrate (+)-5-{-[2-(dimethylamino)ethoxy]-2-thienylmethyl}-1-methyl-1H-pyrazole,

[197] citrate (-)-5-{-[2-(dimethylamino)ethoxy]-2-thienylmethyl}-1-methyl-1H-pyrazole

[198] D-ditoluylmethane (+)-5-{-[2-(dimethylamino)ethoxy]-2-thienylmethyl}-1-methyl-1H-pyrazole

[199] L-ditoluylmethane (-)-5-{-[2-(dimethylamino)ethoxy]-2-thienylmethyl}-1-methyl-1H-pyrazole

[200] citrate (+)-5-{-[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[201] citrate (-)-5-{-[2-(dimethylamino)ethoxy]benzyl}-1-methyl-1H-pyrazole,

[202] 5-(-hydroxy-2-thienylmethyl)-1-methyl-1H-pyrazole,

[203] 5-(-hydroxy-3-methyl-2-thienylmethyl)-1-methyl-1H-pyrazole,

[204] 5-(-hydroxy-5-methyl-2-thienylmethyl)-1-methyl-1H-pyrazole,

[205] 5-(5-bromo--hydroxy-2-thienylmethyl)-1-methyl-1H-pyrazole,

[206] 5-(4-bromo--hydroxy-2-thienylmethyl)-1-methyl-1H-pyrazole,

[207] 5-(-hydroxy--methyl-2-thienylmethyl)-1-methyl

 

Same patents:

The invention relates to the field of medicine and concerns sedative medicinal composition of soft steps, including for Pediatrics

The invention relates to the field of medicine and related antidepressant and treatment of depression using known SFL and SYMPTOM

The invention relates to medicine, namely the creation of an analgesic, antipyretic and anti-inflammatory drugs

The invention relates to medicine, namely to drugs that improve blood circulation in the brain

The invention relates to new compounds of General formulas I, II, III

< / BR>
or their pharmaceutically acceptable salts, in which the dotted lines indicate optional double bonds; A is-CR7or N; - - NR1R2, -CR1R2R11, -C(= CR2R12R1, -NHCHR1R2, -ОСHR1R2, -SCHR1R2, -CHR2OR12,

-CHR2SR12, -C(S)R2or-C(O)R2N-ethyl-2,2,2-triptorelin; G is oxygen, sulfur, NH, NH3hydrogen, methoxy, ethoxy, triptoreline, methyl, ethyl, dimethoxy, NH2, NHCH3N(CH3)2or trifluoromethyl; Y Is N; Z is NH, O, S, -N(C1-C2alkyl) or-C(R13R14), where R13and R14independently of one another represent hydrogen, trifluoromethyl or methyl, or one of the elements of R13and R14is cyano and the other is hydrogen or stands; R1- C1-C6alkyl which may be optionally substituted by one or two substituents R8independently from each other selected from the group comprising hydroxy, fluorine, chlorine, bromine, iodine, CF3C1-C4alkoxy, -O-CO-(C1-C4alkyl), where (C1-C2- C1-C12alkyl, aryl or -(C1-C4alkylene)aryl, where aryl is phenyl, naphthyl; R3is methyl, ethyl, fluorine, chlorine, bromine, iodine, cyano, methoxy, OCF3, methylthio, methylsulphonyl, CH2HE or CH2OCH3; R4is hydrogen, C1-C4alkyl, fluorine, chlorine, bromine, iodine, C1-C4alkoxy, triptoreline, -CH2OCH3, -CH2OCH2CH3, -CH2CH2OCH3, -CF3, amino, nitro, -NH(C1-C4alkyl), -N(CH3)2, -NHCOCH3, -NHCONHCH3, hydroxy, -CO(C1-C4alkyl), -Cho, COOH, cyano, or-COO(C1-C4alkyl), where C1-C4the alkyl may be substituted by one Deputy chosen from the group comprising hydroxy, amino, -NHCOCH3, -NH(C1-C2alkyl), -N(C1-C2alkyl)2, fluorine, chlorine, cyano, nitro; R5is phenyl, naphthyl, pyridyl, pyrimidyl, where each of the above groups R5substituted with one to three substituents that are independently from each other selected from fluorine, chlorine, C1-C6the alkyl or C1-C6alkoxyl, or one Deputy chosen from the group comprising hydroxy, iodine, bromine, formyl, cyano, nitro, trifluoromethyl, amino, -(C1-C6these groups of R5may be optionally substituted with one hydroxy-group; R6is hydrogen or C1-C6alkyl; R7is hydrogen, methyl; R11is hydrogen, hydroxy, fluorine or methoxy; R12is hydrogen or C1-C4alkyl, and R16and R17independently of one another represent hydrogen, hydroxy, methyl, ethyl, methoxy or ethoxy, except that both R16and R17cannot both be methoxy or ethoxy; or R16and R17together form oxo (=O) group; provided that if G is an atom of oxygen, sulfur, NH or NCH3he is joined by a double bond to a five-membered ring of the formula III, and further provided that R6is absent when the nitrogen atom to which it is linked, is attached by a double bond to an adjacent carbon atom in the ring

The invention relates to a derivative tetrahydroisoquinoline formula (I), where X1and X2are hydrogen, halogen, alkoxy - or nitro-group; Y is oxygen or sulfur; R1is hydrogen, alkyl, phenylalkyl or CONHR' wherein R' is phenyl; R2and R3are the same or different from each other and are independently selected from the group consisting of hydrogen and alkyl; R4is hydrogen or lower alkyl

The invention relates to pharmacy and medicine and relates to a medicinal product for the treatment of opium addiction

The invention relates to medicine, to use rihanana as anti-convulsants, excelling activity reference drugs and does not cause allergic reactions
The invention relates to medicine, in particular to the gynecologist, and for the treatment of infertility

The invention relates to technologies for water treated by electrolysis in the cathode chamber and with the ability to suppress metastasis of cancer cells
The invention relates to pharmacy
The invention relates to pharmaceutical compositions, in particular to pharmaceutical compositions comprising an inhibitor illegitimates (ARI) and angiotensin-converting enzyme (ACE), which is applicable for the prevention and treatment of complications of diabetes

The invention relates to pharmaceuticals, to pharmaceutical compositions which possess improved antitumor effect or reduced(and) side(s) effect(s) consisting of the active substance having antitumor action, or a pharmaceutically acceptable salt thereof and a derivative of hydroxamic acids according to the formula or therapeutically applicable its acid salt additive

Pharmaceutical drug // 2213577
The invention relates to medicine

The invention relates to substituted 1-phenylpyrazol-3-carboxamide formula (Ia) in which R1xis in position 4 or 5 and denotes the group-T-CONRaRbin which T represents a direct bond or (C1-C7-alkylen; NRaRbdenotes a group selected from (a), (b), (C); R5and R6denote, independently of one another, hydrogen, (C1-C6)-alkyl, (C3-C8)-alkenyl or R5and R6together with the nitrogen atom to which they are linked, represent a heterocycle selected from pyrrolidine, piperidine, research, piperazine, substituted in position 4 by Deputy R9; R7denotes hydrogen, (C1-C4)-alkyl or benzyl; R8denotes hydrogen, (C1-C4)-alkyl, or R7and R8together with the carbon atom to which they are attached, form a (C3-C5-cycloalkyl; R9denotes hydrogen, (C1-C4)-alkyl, benzyl or a group-X-NR'5R'6in which R'5and R'6represent, independently from each other, (C1-C6)-alkyl; R10denotes hydrogen, (C1-C4)-alkyl; s= 0-3; t=0-3, provided that (s+t) in the same group greater than or equal to 1; the divalent radicals a and E together with the atom is which in addition, may be substituted by one or more (C1-C4-alkilani; R2xand R3xdenote, independently of one another, hydrogen, (C1-C6)-alkyl, (C3-C8-cycloalkyl, (C3-C8-cyclooctylmethyl provided that R2xand R3xdo not simultaneously denote hydrogen or R2xand R3xtogether form tetramethylene group; and their pharmaceutically acceptable salts
Up!