1,4-substituted derivative of a cyclic amine, the means of obtaining it, the drug, which has antagonistic to serotonin effect, a method of treating diseases, for which effective antagonism to serotonin

 

Describes 1,4-substituted derivatives of cyclic amine of the formula (1), where a, b, C, D are the same or different and each of them Metin or nitrogen, provided that at least two of them Metin, communicationrepresents a single or double bond; T-Metin or nitrogen; Y and Z are the same or different and each represents Metin, nitrogen,orprovided that at least one nitrogen; R1-R6have different values; n = 0 or 1, 2, 3; m = 0 or an integer from 1 to 6; p = 1, 2, 3. Describes two methods of preparing compounds of the formula (X) drug, possess antagonistic to serotonin effect, and a method of treating diseases, for which effective antagonism to serotonin. The technical result is to new compounds that are antagonistic to serotonin and can be used for treating, mitigating and preventing spastic paralysis or muscle relaxant Central action to mitigate myotonia. 5 C. and 21 C.p. f-crystals, 7 PL.

Text description of the Noe-derived cyclic amine, represented by formula (I)or its pharmacologically acceptable salt, where a, b, C and D are the same or different from each other and each of them Metin or nitrogen, provided that at least two of them Metin;
link

represents a single or double bond;
T - Metin or nitrogen;
Y and Z, equal or different from each other and each of them Metin, nitrogen, a group of the formula

or a group of the formula

provided that at least one nitrogen;
R1and R2the same or different from each other and each of them is hydrogen, halogen, hydroxy, lower alkylsulfonyl, halogen-substituted lower alkylsulfonyl, 1-hydroxy-1-(methoxyphenyl) methyl, methoxyprogesterone, 1,3-propanesultone-2-yl, lower hydroxypiperidine, lower hydroxyethylaminomethyl, halogen-substituted lower acylaminoalkyl, lower dehalogenation acylaminoalkyl, lower imidazolylalkyl, lower pyrrolidineethanol, lower hydroxypiperidine, amino, optionally substituted stands, ethyl, isopropyl, dimethylamino, nitro, n is alkoxy, lower alkylsulfonyl, N-lower alkylamidopolyamine, lower acylamino, aminoalkyl, methylaminomethyl, N-methyl lower acyl-aminoalkyl, lower acyl-aminoalkyl, phenyl, substituted by fluorine, phenylcarbonylamino substituted by fluorine, lower alkylsulfonate, gidroksilaminami, (2-pyrrolidone-1-yl)methyl, (2-piperidin-1-yl)methyl, pyridyl, thiazolyl, 1-methylpropyl, benzyl, substituted methoxy, pyridylethyl, optionally substituted methoxy, titlelabel, pyrrolidinyloxy, piperidinyloxy, optionally substituted stands, ethyl, acetyl, pyrrolidinyl, imidazolylalkyl, triazolylmethyl, cycloalkylcarbonyl, optionally substituted stands, dimetilan, ureido-lower alkyl, (succinimido-1-yl)lower alkyl, amido, carbarnoyl, optionally substituted stands, ethyl, propylene, isobutyl, tert-bootrom, cyclopropyl, carbarnoyl-lower alkyl, tetramethylaniline, thiocarbamoyl-lower alkyl, formyl, pyrrolidinones, pyridylcarbonyl, thiazolidinones, halogen-substituted lower alkyl, (2-imidazolidine-1-yl)methyl, (2,4-imidazolidinedione-3-yl)methyl, (2-oxazolidin-3-yl)methyl, (glutarimide-1-yl)methyl, optionally substituted by chlorine, methoxy, dimethylamino pyridylcarboxylic, pirici, 1-hydroxy-lower cycloalkyl, (2,4-thiazolidinedione-3-yl) methyl, 4-piperidinyl, substituted acetyl, stands, ethyl, N-methyl aminosulfonyl, carboxy-lower alkyl or lower acylaminoalkyl, or alternative R1and R2together can form trimethylene, substituted hydroxy, thiazole, dioxymethylene, the rest of aminothiazole;
R3is hydrogen, halogen, lower alkyl, hydroxy, hydroxy-lower alkyl, lower alkoxy, formyl;
R4is hydrogen, lower alkyl, hydroxy-lower alkyl, fortunelately, forbindelser;
R5- lower alkyl, lower acyl, lower alkoxycarbonyl or a group of the formula
-Q1-(CH2)s-Q2-R6,
where Q1and Q2both single bond or one of them represents a single bond and the other is oxygen, the carbonyl group of the formula
-NHCO-
or a group of the formula

where R7hydroxy, lower alkyl or halogen;
s = 0 or an integer from 1 to 6;
R6is phenyl, optionally substituted by one or more substituents selected from the following: halogen, C1-C6-alkoxy, HE, CN, hydroxy-C1-C6-alkyl, hydroxy-C1-C6-alkoxy, CF3C1- 1-C6-alkanolamine, C1-C6-alkylamino, hydroxyamino-C1-C6-alkyl, amino-C1-C6-alkyl, C1-C6-alkanolamine-C1-C6-alkyl, halogen-(C1-C6-alkanolamine-C1-C6-alkyl, C1-C6-alkylsulfonamides-C1-C6-alkyl, carbarnoyl, C1-C6-alkyl-carbarnoyl-C1-C6-alkyl, aminosulfonyl, di-C1-C6-alkylamino-C1-C6-alkoxy or C1-C3-alkylenedioxy;
R6- pyridyl, optionally substituted by one or more substituents selected from the following: C1-C6-alkoxy, CN, hydroxy-C1-C6-alkyl, halogen;
R6- thienyl, optionally substituted C1-C6-alkoxy;
R6- thiazolyl, optionally substituted C1-C6-alkyl, C1-C6-alkoxy, CN;
R6- indolyl, benzothiazolyl, pyrazinyl, pyrazolyl, optionally substituted with halogen;
R6- phthalimido;
n = 0 or 1, 2, 3;
m = 0 or an integer from 1 to 6;
p = 1, 2, 3,
provided that the 1,4-substituted derivative of the cyclic amine is not one of the following compounds

where R5b- H, benzyl, etoxycarbonyl

where R5A- H, och3, etoxycarbonyl

2. 1,4-Substituted derivative of a cyclic amine under item 1 or its pharmacologically acceptable salt, in which a, b, C and D are the same or different from each other and at least one nitrogen.

3. 1,4-Substituted derivative of a cyclic amine of the formula (I) under item 1 or its pharmacologically acceptable salt, where T and Z is nitrogen atoms; a, b, C, D, and Y carbon atoms; R4is hydrogen; R5- 4-florfenicol; n and m = 0; p = 2; R1and R2taken together and are associated with atoms b and C, form a residue of thiazole, aminothiazole or dioxymethylene or, taken together and are associated with atoms a and b, form a fragment of trimethylene, substituted hydroxy-group.

4. 1,4-Substituted derivative of a cyclic amine under item 1, represented by formula (II)

or its hydrochloride, hydrobromide, oxalate,
where R is the Deputy chosen from the following:





5. 1,4-Substituted derivative of a cyclic amine under item 1 or 4 or its hydrochloride, hydrobromide, oxalate, where m = 0 and p = 2.

6. 1, 4-Substituted derivative of a cyclic amine on PP.1, 4 and 5 or the hydrochloride, hydrobromide, oxalate, where Y - Metin, Z is nitrogen.

7. 1,4-Substituted derivative of a cyclic amine on PP.1, 4-6 formula (III)

or its hydrochloride, hydrobromide, oxalate,
where the relationship represented by the formula

R1- R5defined in paragraph 1.

8. 1,4-Substituted derivative of a cyclic amine on PP.1, 4-7 formula (IV)

or its hydrochloride, hydrobromide, oxalate,
where the relationship represented by the formula

R1, R2, R3, R4, R6, Q1, Q2and s is defined in paragraph 1.

9. 1,4-Substituted derivative of a cyclic amine under item 8 of the formula (V)

or its hydrochloride, hydrobromide, oxalate,
where R1- R4, R6and s is defined in paragraph 1.

10. 1,4-Substituted derivative of a cyclic amine under item 8 of the formula (VI)

or its hydrochloride, hydrobromide, oxalate,
where R1- R4, R6 is Eski acceptable salt, which traveler is a compound selected from the following compounds:
(1) 1-[1-(4-forfinal)piperidine-4-yl]indoline,
(2) 1-[1-(4-terbisil)piperidine-4-yl]indoline,
(3) 1-(1-finetipped-4-yl)indolin,
(4) 1-[1-(4-bromophenetole)piperidine-4-yl]indoline,
(5) 1-[1-(3-chlorphenyl)piperidine-4-yl]indoline,
(6) 1-[1-(-4-chlorphenyl)piperidine-4-yl]indoline,
(7) 1-[1-(2-florfenicol)piperidine-4-yl]indoline,
(8) 1-[1-(3-florfenicol)piperidine-4-yl]indoline,
(9) 1-[1-(4-florfenicol)piperidine-4-yl]indoline,
(10) 1-[1-(2,4-divertenti)piperidine-4-yl]indoline,
(11) 1-[1-(3,4-divertenti)piperidine-4-yl]indoline,
(12) 1-[1-(5,5-divertenti)piperidine-4-yl]indoline,
(13) 1-[1-(4-florfenicol)piperidine-4-yl]indoline,
(14) 1-{1-[2-(4-forfinal)propyl]piperidine-4-yl}indoline,
(15) 1-[1-(4-florfenicol)piperidine-4-yl]indoline,
(16) 1-[1-(4-florfenicol)piperidine-4-yl]methylindolin,
(17) 1-{2-[1-(4-florfenicol)piperidine-4-yl]ethyl}of indolin,
(18) 1-[1-(4-methoxyphenethyl)piperidine-4-yl]indoline,
(19) 1-[1-(3-methoxyphenethyl)piperidine-4-yl]indoline,
(20) 1-[1-(4-hydroxyphenethyl)piperidine-4-yl]indoline,
(21) 1-[1-(4-cyanophenyl)piperidine-4-yl]indoline,
(22) 1-[1-(3-hydroxymethylene)piperidine-4-yl]indoline,
(23) 1-[1-(4-hydroxymethylene)piperidine-4-yl]indoline,
(24) 1-{1-[4-1-{1-[4-(2-hydroxyethoxy)phenethyl]piperidine-4-yl}indoline,
(27) 1-[1-(4-triptoreline)piperidine-4-yl]indoline,
(28) 1-[1-(4-methanesulfonylaminoethyl) piperidine-4-yl]indoline,
(29) 1-[1-(4-nitrophenyl)piperidine-4-yl]indoline,
(30) 1-[1-(4-AMINOPHENYL)piperidine-4-yl]indoline,
(31) 1-[1-(4-methylsulfonylmethane)piperidine-4-yl]indoline and 1-{1-[4-bis (methylsulphonyl)aminopentyl]piperidine-4-yl}indoline,
(32) 1-[1-(4-acetamidophenyl)piperidine-4-yl]indoline,
(33) 1-[1-(4-ethylaminomethyl)piperidine-4-yl]indoline,
(34) 1-[1-(4-hydroxyaminobuteroyl)piperidine-4-yl]indoline,
(35) 1-[1-(4-aminomethylphenol)piperidine-4-yl]indoline,
(36) 1-[1-(4-acetamidophenyl)piperidine-4-yl]indoline,
(37) 1-[1-(4-chloroacetoacetate)piperidine-4-yl]indoline,
(38) 1-[1-(4-methanesulfonylaminoethyl)piperidine-4-yl]indoline,
(39) 1-[1-(4-propenolatomethyl)piperidine-4-yl]-3-methylindolin,
(40) 1-[1-(4-carbamoylmethyl)piperidine-4-yl]indoline,
(41) 1-[1-(4-1M-isopropylcyclopentadienyl)piperidine-4-yl]indoline,
(42) 1-[1-(4-sulfamoylbenzoyl)piperidine-4-yl]indoline,
(43) 1-{3-[(2-hydroxyethoxy)phenethyl]piperidine-4-yl}indoline,
(44) 1-{1-[4-(2-dimethylaminoethoxy)phenethyl]piperidine-4-yl}indoline
(45) 1-{1-[3,4-di(hydroxymethyl)phenethyl]piperidine-4-yl)indolin,
(46) 1-{1-[3,4-(methylenedioxy)phenethyl]episuldonium)ethyl]piperidine-4-yl}indoline,
(49) 1-{1-[2-(4-pyridyl)ethyl]piperidine-4-yl)indolin,
(50) 1-{1-[2-(2-pyridyl)ethyl]piperidine-4-yl)indolin,
(51) 1-{1-[2-(3-pyridyl)ethyl]piperidine-4-yl}indoline,
(52) 1-{1-[2-(2-methoxy-5-pyridyl)ethyl]piperidine-4-yl}indoline,
(53) 1-{1-[2-(3-methoxypyridine-5-yl)ethyl]piperidine-4-yl}indoline,
(54) 1-{1-[2-(2-cyano-5-yl)ethyl]piperidine-4-yl}indoline,
(55) 1-{1-[2-(2-hydroxymethylpropane-5-yl)ethyl]piperidine-4-yl}indoline,
(56) 1-{1-[2-(3-hydroxymethylpropane-5-yl)ethyl]piperidine-4-yl}indoline,
(57) 1-[1-(2,6-debtor-3-pyridylmethyl)piperidine-4-yl]indoline,
(58) 1-{1-[2-(2-thienyl)ethyl]piperidine-4-yl}indoline,
(59) 1-{1-[2-(3-thienyl)ethyl]piperidine-4-yl}indoline,
(60) 1-[1-(2-triazolylmethyl)piperidine-4-yl]indoline,
(61) 1-[1-(4-methyl-5-thiazoleacetic)piperidine-4-yl]indoline,
(62) 1-{1-[(indol-3-yl)ethyl]piperidine-4-yl}indoline,
(63) 1-{1-[2-(6-benzothiazolyl)ethyl]piperidine-4-yl}indoline,
(64) 1-[1-(5-methoxy-2-thienyl)ethylpiperidine-4-yl]indoline,
(65) 1-[1-(2-methoxy-5-thiazolyl)ethylpiperidine-4-yl]indoline,
(66) 1-[1-(2-cyano-5-thiazolyl)ethylpiperidine-4-yl]indoline,
(67) 1-(1-personalityparade-4-yl)indolin,
(68) 1-{1-[2-(4-bromopyrazole-1-yl)ethyl]piperidine-4-yl}indoline,
(69) 1-{1-[3-(4-pertenece)propyl]piperidine-4-yl}indoline,
(70) 1-{1-[3-(4-hydroxymethylene)propyl]piperidine-4-yl}indoline,
(Jolin,
(73) 1-{1-[4-(4-forfinal)-4-hydroxybutyl]piperidine-4-yl}indoline
(74) 1-[1-(phthalimido-1-yl)ethylpiperidine-4-yl]indoline,
(75) 1-[1-(4-perbenzoic)ethylpiperidine-4-yl]indoline,
(76) 1-{1-[1-(3,4-acid)propan-2-yl]piperidine-4-yl}indoline,
(77) 1-{1-[(1,4-benzodioxan-2-yl)methyl]piperidine-4-yl}indoline,
(78) 1-{1-[3-(3,4-methylenedioxyphenoxy)propyl]piperidine-4-yl}indoline,
(79) 1-[1-(4-florfenicol)-3-methylpiperidin-4-yl]indoline,
(80) 1-(1-benzyl-3-hydroxyethylpiperazine-4-yl)indolin,
(81) 1-[1-(4-florfenicol)-3-hydroxyethylpiperazine-4-yl]indoline,
(82) 1-[1-(4-florfenicol)-3-hydroxyethylpiperazine-4-yl]indoline,
(83) 1-[2-(4-acetamidomethyl)ethyl]-4-(indan-1-yl)-piperidine-1-oxide,
(84) 1-[1-ethyl-3-(4-forfinancial)piperidine-4-yl]indoline,
(85) 1-[1-ethyl-3-(4-forbindelser)piperidine-4-yl]indoline,
(86) 1-[1-ethyl-3-(4-forbindelser)piperidine-4-yl]indoline,
(87) 1-(1-acetylpiperidine-4-yl)indolin-7-carbaldehyde,
(88) 1-[1-(4-tert-butoxycarbonyl)piperidine-4-yl]-6-bromoindoline,
(89) 1-[1-(4-tert-butoxycarbonyl)piperidine-4-yl] -6-hydroxymethylcytosine,
(90) 1-[1-(4-tert-butoxycarbonyl)piperidine-4-yl]-6-aminomethylation,
(91) 1-(1-benzylpiperidine-4-yl)-6-bromoindoline,
(92) 1-(1-benzylpiperidine-4-yl)-6-floridain,
(93) 1-(1-benzylpiperidine-yl)-6-aminomethylation,
(96) 1-(1-benzylpiperidine-4-yl)-6-acetamidomethyl,
(97) 1-[1-(4-methoxyphenethyl)piperidine-4-yl]-6-acetamidomethyl,
(98) 1-[1-(4-chlorphenyl)piperidine-4-yl]-6-acetamidomethyl,
(99) 1-[1-(4-florfenicol)piperidine-4-yl]-5-methoxyindole,
(100) 1-[1-(4-florfenicol)piperidine-4-yl]-6-bromoindoline,
(101) 1-[1-(4-florfenicol)piperidine-4-yl]-6-bromoindoline,
(102) 1-[1-(4-florfenicol)piperidine-4-yl]-6-chloroindole,
(103) 1-[1-(4-florfenicol)piperidine-4-yl]-6-floridain,
(104) 1-[1-(4-florfenicol)piperidine-4-yl]-6-hydroxyindole,
(105) 1-[1-(4-florfenicol)piperidine-4-yl]-4-methoxyindole,
(106) 1-[1-(4-florfenicol)piperidine-4-yl]-6-methoxyindole,
(107) 1-[1-(4-florfenicol)piperidine-4-yl]-7-methoxyindole,
(108) 1-[1-(4-florfenicol)piperidine-4-yl]-6,7-dimethoxyindole,
(109) 1-[1-(4-florfenicol)piperidine-4-yl]-6-nitroindoline,
(110) 1-[1-(4-florfenicol)piperidine-4-yl]-6-aminoindole,
(111) 1-[1-(4-florfenicol)piperidine-4-yl]-6-methyleneindoline,
(112) 1-[1-(4-florfenicol)piperidine-4-yl]-6-ethylaminomethyl,
(113) 1-[1-(4-florfenicol)piperidine-4-yl]-6-isopropylaminoethyl,
(114) 1-[1-(4-florfenicol)piperidine-4-yl]-6-dimethylaminoethyl,
(115) 1-[1-(4-florfenicol)piperidine-4-yl]-6-acetamidobenzoic,
(116) 1-[1-(4-florfenicol)piperidine-4-yl]-6-methanesulfonyl uridin-4-yl]-6-propanesulfinamide,
(119) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(4-forbindelseshandtering)indolin,
(120) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(N-methylmethanesulfonamide)indolin,
(121) 1-[1-(4-florfenicol)piperidine-4-yl]-6-hydroxyisoquinoline,
(122) 1-[1-(4-florfenicol)piperidine-4-yl]-6-methanesulfonamido,
(123) 1-[1-(4-florfenicol)piperidine-4-yl]-7-hydroxyisoquinoline,
(124) 1-[1-(4-florfenicol)piperidine-4-yl]-6-cyanoindole,
(125) 1-[1-(4-florfenicol)piperidine-4-yl]-6-carbamimidoyl,
(126) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(1-pyrrolidinone)indolin,
(127) 1-[1-(4-florfenicol)piperidine-4-yl]-6-acetylindole,
(128) 1-[1-(4-florfenicol)piperidine-4-yl]-6-methanesulfonamido,
(129) 1-[1-(4-florfenicol)piperidine-4-yl]-6-thiocarbamoylation,
(130) 1-[1-(4-florfenicol)piperidine-4-yl]-6-formylindole,
(131) 1-[1-(4-florfenicol)piperidine-4-yl]-6-gidroksiiminobetulonovoi,
(132) 1-[1-(4-florfenicol)piperidine-4-yl]-6-aminomethylation,
(133) 1-[1-(4-florfenicol)piperidine-4-yl]-6-acetamidomethyl,
(134) 1-[1-(2-florfenicol)piperidine-4-yl]-6-acetamidomethyl,
(135) 1-[1-(3-florfenicol)piperidine-4-yl)-6-acetamidomethyl,
(136) 1-[1-(4-florfenicol)piperidine-4-yl]-6-hydroxymethylcytosine,
(137) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(1-hydroxide-4-yl] -6-(1-hydroxy-1-methylethyl)indolin,
(140) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(1-hydroxycyclopent)indolin,
(141) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(1-hydroxycyclopent)indolin,
(142) 1-[1-(4-florfenicol)piperidine-4-yl]-6-chlorothalidone,
(143) 1-[1-(4-florfenicol)piperidine-4-yl]-6-formationally,
(144) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(1-foradil)indolin,
(145) 1-[1-(4-florfenicol)piperidine-4-yl]-6-cyanopyridine,
(146) 1-[1-(4-florfenicol)piperidine-4-yl]-6-carboxymethylation,
(147) 1-[1-(4-florfenicol)piperidine-4-yl]-6-carbamoylmethyl,
(148) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(methylcarbamoylmethyl)indolin,
(149) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(ethylcarboxylate)indolin,
(150) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(n-propylgallate)indolin,
(151) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(isopropylaminomethyl)indolin,
(152) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(isobutylbarbituric)indolin,
(153) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(tert-butylcarbamoyl)indolin,
(154) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(cyclopropanecarbonyl)indolin,
(155) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(tetramethylaniline)indolin,
(156) 1-[1-(4-florfenicol)piperidine-4-yl]-6-propiomelanocortin,
(157) 1-[1-(4-florfenicol)piperidine-4-I) 1-[1-(4-florfenicol)piperidine-4-yl] -6-cyclopropanecarboxaldehyde,
(160) 1-[1-(4-florfenicol)piperidine-4-yl] -6-methylsulfonylmethan,
(161) 1-[1-(4-florfenicol)piperidine-4-yl]-6-ureidopenicillin,
(162) 1-[1-(4-florfenicol)piperidine-4-yl]-6-S-methylaminoethanol,
(163) 1-[1-(4-florfenicol)piperidine-4-yl] -6-S-methylacetanilide,
(164) 1-[1-(4-florfenicol)piperidine-4-yl] -6-M-methylsulfonylmethan,
(165) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(1-acetamidomethyl)indolin,
(166) 1-[1-(4-florfenicol)piperidine-4-yl]-6-acetamidoacrylic,
(167) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[(piperidine-4-yl)methyl]indoline,
(168) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[(1-acetylpiperidine-4-yl)methyl]indoline,
(169) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[(1-ethylpiperazin-4-yl)methyl]indoline,
(170) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[(1-methylpiperidin-4-yl)methyl]indoline,
(171) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-pyridyl)indolin,
(172) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-thiazolyl)indolin,
(173) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(1-methylpyrrole-2-yl)indolin,
(174) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(2-pyridyl)methyl]indoline,
(175) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-(2-pyridyl)-methyl]indoline,
(176) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(3-pyridyl)methyl]indoline,
(177) 1-[1-(4-florfenicol)indolin,
(179) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(4-pyridylmethyl)indolin,
(180) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-pyridylcarbonyl)indolin,
(181) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(2-pyridyl)ethyl]indolin,
(182) 1-[1-(4-florfenicol)piperidine-4-yl]-6-[1-(2-pyridyl)-ethyl]indolin,
(183) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(3-pyridylcarbonyl)indolin,
(184) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(2-methoxypyridine-3-yl)methyl] indoline,
(185) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-(2-methoxypyridine-3-yl)methyl]indoline,
(186) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(2-methoxypyridine-6-yl)methyl]indoline,
(187) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-(2-methoxypyridine-6-yl)methyl]indoline,
(188) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(2-methoxypyridine-5-yl)methyl]indoline,
(189) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-(2-methoxypyridine-5-yl)methyl]indoline,
(190) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(2-pyridone-5-yl)methyl]indoline,
(191) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(2-dimethylaminopyridine-5-yl)methyl]indoline,
(192) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(2-chloropyridin-5-yl)methyl]indoline,
(193) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(2-thiazolyl)-1-hydroxymethyl]indolin,
(194) 1-[1-(4-ferrocenyl]indolin,
(196) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-(5-thiazolyl)-1-hydroxymethyl]indolin,
(197) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(pyrimidine-2-yl)methyl]indoline,
(198) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(pyrimidine-5-yl)methyl]indoline,
(199) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[1-hydroxy-1-(2-pyrrolyl)methyl]indoline,
(200) 1-[1-(4-florfenicol)piperidine-4-yl] -6-N,N-dimethylaminomethylene,
(201) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(4-forfinal)indolin,
(202) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-pyrrolidone-1-yl)methylindoline,
(203) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-piperidin-1-yl)methylindoline,
(204) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(succinimido-1-yl)methylindoline,
(205) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(glutarimide-1-yl)methylindoline,
(206) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-imidazolidinyl)methylindolin,
(207) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(2,4-imidazolidinedione-3-yl)methylindoline,
(208) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-oxazolidin-3-yl)methylindoline,
(209) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(2,4-thiazolidinedione-3-yl)methylindoline,
(210) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(pyrrol-1-yl)methylindoline,
(211) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(imidazol-1-yl)methylindoline,
(212) 1-[1-(4-florfenicol)piperidine-4-yl]orinetal)piperidine-4-yl]-6-(1,2,4-triazole-2-yl)methylindoline,
(214) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-thiazolyl)methylindolin,
(215) 1-[1-(4-florfenicol)piperidine-4-yl]-3-methylindolin,
(216) (217) 1-[1-(4-florfenicol)piperidine-4-yl]-5-chloro-6-aminoindole,
(217) (218) 1-[1-(4-florfenicol)piperidine-4-yl] -5-chloro-6-methanesulfonylaminoethyl,
(218) 1-[1-(4-florfenicol)piperidine-4-yl]-5-chloro-6-methoxyindole,
(219) 1-[1-(2,4-divertenti)piperidine-4-yl]-6-aminoindole,
(220) 1-[1-(2,4-divertenti)piperidine-4-yl] -6-methanesulfonylaminoethyl,
(221) 1-[1-(2,4-divertenti)piperidine-4-yl]-6-acetamidobenzoic,
(222) 1-[1-(2,4-divertenti)piperidine-4-yl]-6-bromoindoline,
(223) 1-[1-(2,4-divertenti)piperidine-4-yl]-6-acetamidomethyl,
(224) 1-[1-(2,4-divertenti)piperidine-4-yl]-6-carbamoylmethyl,
(225) 1-{ 1-[3-(4-florfenicol)propyl] piperidine-4-yl} -6-acetamidomethyl,
(226) 1-{ 1-[4-(4-florfenicol)butyl]piperidine-4-yl}-6-acetamidomethyl,
(227) 1-[1-(4-methoxyphenethyl)piperidine-4-yl]-6-methoxyindole,
(228) 1-[1-(4-methoxyphenethyl)piperidine-4-yl]-6-floridain,
(229) 1-[1-(4-sulfamoylbenzoyl)piperidine-4-yl]-6-methoxyindole,
(230) 1-[1-(4-forfinancial)piperidine-4-yl]-6-bromoindoline,
(231) 1-[1-(4-forfinancial)piperidine-4-yl]-6-acetamidomethyl,
(232) 1-{1-[2-(6-benzothiazolyl)ethyl]piperidine-the one-4-yl]-6-aminothiazole-[5,4-f]indolin,
(235) 1-[1-(4-florfenicol)piperidine-4-yl]-7-hydroxy(4A, 7a)cyclohexanedione and 1-[1-(4-florfenicol)piperidine-4-yl]-4-hydroxy-(3b, 6A)-cyclohexanedione,
(236) 1-(1-methylpiperidin-4-yl)-6-(4-forbindelseshandtering)indolin,
(237) 1-(1-ethylpiperazin-4-yl)-6-(4-forbindelseshandtering)indolin,
(238) 1-(1-ethylpiperidine)-4-(4-forfinal)indolin,
(239) 1-[1-(4-florfenicol)piperidine-4-yl]indan,
(240) 1-[1-(4-methoxyphenethyl)piperidine-4-yl]indan,
(241) 1-{4-[2-(4-forfinal)ethyl]piperazine-1-yl}-6-methoxyindol,
(242) 1-(4-ethylpiperazin-1-yl)-6-methoxyindol,
(243) 7-[4-hydroxy-1-(4-florfenicol)piperidine-4-yl] -5,6-dihydro-7H-pyridine,
(244) 7-[1-(4-florfenicol)piperidine-4-ilidene]-5,6-dihydropyridines,
(245) 7-[1-(4-florfenicol)piperidine-4-yl]-5,6-dihydro-7H-pyridine,
(246) 7-[4-(4-florfenicol)piperazine-1-yl]-5,6-dihydro-7H-pyridine,
(247) 1-[1-(4-florfenicol)piperidine-4-yl]-6-chloro-7-azaindole,
(248) 1-[1-(4-florfenicol)piperidine-4-yl]-7-azaindole,
(249) 1-[1-(4-florfenicol)piperidine-4-yl]-6-fluoro-7-azaindole,
(250) 1-[1-(2,4-divertenti)piperidine-4-yl]-6-chloro-7-azaindole,
(251) 1-[1-(4-methoxyphenethyl)piperidine-4-yl]-6-chloro-7-azaindole,
(252) 1-[1-(4-florfenicol)piperidine-4-yl]-6-azaindole,
(253) 5-[1-(4-florfenicol)piperidine-4-ilidene] -7-methyl-5,6-dihydrocyclopenta,
(25 is ridin-4-yl}-7-methoxy-1,2,3,4-tetrahydroquinolin,
(256) 1-{ 1-[2-(4-forfinal)ethyl]piperidine-4-yl}-7-methoxy-1,2,3,4-tetrahydroquinolin,
(257) 1-[1-(4-cyanopropyl)piperidine-4-yl] -7-methoxy-1,2,3,4-tetrahydroquinolin,
(258) 1-{ 1-[2-(2-thienyl)ethyl] piperidine-4-yl}-7-methoxy-1,2,3,4-tetrahydroquinolin,
(259) 1-{1-[2-(4-forfinal)ethyl]piperidine-4-yl}-7,8-dimethoxy-1,2,3,4-tetrahydroquinolin,
(260) 1-{ 1-[2-(4-forfinal)ethyl] piperidine-4-yl} -7,8-methylenedioxy-1,2,3,4-tetrahydroquinolin,
(261) 1-{ 1-[2-(4-forfinal)ethyl] piperidine-4-yl} -7-methoxy-8-methyl-1,2,3,4-tetrahydroquinolin,
(262) 1-{ 1-[2-(4-forfinal)-2-oxoethyl] piperidine-4-yl} -7-methoxy-1,2,3,4-tetrahydroquinolin,
(263) 1-{ 1-[2-(4-forfinal)-2-hydroxyethyl]piperidine-4-yl}-7-methoxy-1,2,3,4-tetrahydroquinolin,
(264) 1-{ 1-[2-(4-forfinal)-2-feratel] piperidine-4-yl} -7-methoxy-1,2,3,4-tetrahydroquinolin,
(265) 1-[2-(4-forfinal)ethyl]-4-(6-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)piperidine,
(266) 1-[2-(4-forfinal)ethyl] -4-[6-(2-hydroxy)ethoxy-1,2,3,4-tetrahydronaphthalen-1-yl]piperidine,
(267) 1-{ 4-[2-(4-forfinal)ethyl]piperazine-1-yl)-7-methoxy-1,2,3,4-tetrahydronaphthalen,
(268) 1-{ 4-[2-(4-forfinal)-2-oxoethyl] piperazine-1-yl} -7-methoxy-1,2,3,4-tetrahydronaphthalen,
(269) 1-(4-florfenicol)-4-(2-methoxybenzaldehyde-9-yl)-piperazine,
(270) 5-{ 4-[2-(4-forfinal)ethyl]piperazine-1-yl}-5,6,7,8-tetrahydroisoquinoline,
(271) 1-Linda,
(273) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(N-isopropylaminomethyl)indole,
(274) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(1-methylpyrrole-2-yl)indole,
(275) 1-[1-(4-acetamidophenyl)piperidine-4-yl]indole,
(276) 1-[1-(4-florfenicol)piperidine-4-yl]-6-cyanoindole,
(277) 1-[1-(4-florfenicol)-3-methylpiperidin-4-yl]indole,
(278) 1-[1-(4-florfenicol)homopiperazin-4-yl]-6-methoxyindole,
(279) 1-[1-(4-florfenicol)pyrrolidin-3-yl]-6-methoxyindole,
(280) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(ethylcarboxylate)indole,
(281) 1-[1-(4-florfenicol)piperidine-4-yl]-6-[N-(cyclopropanecarbonyl)methyl]indole,
(282) 1-[1-(4-florfenicol)piperidine-4-yl]-6-[N-(isobutylamino)methyl] indole,
(283) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(n-propylgallate)indole,
(284) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(tetramethylaniline)indole,
(285) 1-[1-(2,4-divertenti)piperidine-4-yl]-6-carbamoylmethyl,
(286) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-hydroxyethyl)carbamoylmethyl,
(287) 1-[1-(-4-florfenicol)piperidine-4-yl]-6-dimethylcarbamoyl,
(288) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(4-hydroxypiperidine-1-ylcarbonyl)indole,
(289) 1-1-(4-florfenicol)piperidine-4-yl]-6-[bis(2-hydroxyethyl)carbamoylmethyl]indole,
(290) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(1,3-d) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(carbamoylmethyl)carbamoylmethyl,
(293) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-dimethylaminoethyl)carbamoylmethyl,
(294) 1-[1-(4-florfenicol)piperidine-4-yl] -6-cyanomethaemoglobin,
(295) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-methoxyethyl)carbamoylmethyl,
(296) (310) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(2-foradil)-carbamoylmethyl,
(297) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[2-(ethylcarbamate)ethyl]indole,
(298) 1-[1-(4-florfenicol)piperidine-4-yl]-6-[2-(pyrrolidin-1-yl)ethyl]carbamoylmethyl,
(299) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[2-(morpholine-4-yl)ethyl] carbamoylmethyl,
(300) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(pyridin-4-yl)-methylcarbamoylmethyl,
(301) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[2-(pyridin-2-yl)ethyl]carbamoylmethyl,
(302) 1-[1-(4-florfenicol)piperidine-4-yl]-6-methylcarbamoylmethyl,
(303) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(2-methoxypyridine-5-ylcarbonyl)indole,
(304) 1-[1-(4-florfenicol)piperidine-4-yl] -6-[(2-methoxypyridine-5-yl)hydroxymethyl]indole,
(305) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(1-hydroxypropyl)indole,
(306) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(1-hydroxy-1-methylethyl)indolin,
(307) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(3-hydroxypropyl)indole,
(308) 1-[1-(4-florfenicol)piperidine-4-yl]-6-methanesulfonamido,
(311) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(3-chlorpropyl)-sulfonamidemetformin,
(312) 1-[1-(4-perfectil)piperidine-4-yl] -6-(1,3-propanesultone-2-yl)methylindole,
(313) 1-[1-(4-florfenicol)piperidine-4-yl]-6-propionylthiocholine,
(314) 3-chloro-1-[1-(4-florfenicol)piperidine-4-yl]-6-acetamidomethyl,
(315) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(4-hydroxyethylaminomethyl)indole,
(316) 1-[1-(4-florfenicol)piperidine-4-yl]-6-hydroxyethoxyethyl,
(317) 1-[1-(4-florfenicol)piperidine-4-yl]-6-methanesulfonamido,
(318) 1-[1-(2,6-debtor-3-pyridylmethyl)piperidine-4-yl]indole,
(319) 1-[1-(4-florfenicol)piperidine-4-yl]-6-Florinda,
(320) 1-[1-(4-florfenicol)piperidine-4-yl]thiazolo[5,4-f]-indole,
(321) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(N-methylmethanesulfonamide)indole,
(322) 1-[1-(4-florfenicol)piperidine-4-yl]-6-methanesulfonamido,
(323) 1-[1- (4-florfenicol)piperidine-4-yl]-6-carbamimidoyl,
(324) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(N-methylcarbamoylmethyl)indole,
(325) 1-[1-(4-florfenicol)piperidine-4-yl]-6-acetamidophenol,
(326) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(1,2-dihydroxypropane-3-yl)carbamoylmethyl,
(327) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(pyridin-2-yl)-methylcarbamoylmethyl,
(328) 1-[1-(2-florfenicol)piperidine-4-yl]-6-methylcarbamoylmethyl)piperidine-4-yl]-6-ethylcarbodiimide,
(331) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(1-ethylpiperazin-4-yl)methylcarbamoylmethyl,
(332) 1-[1-(2-florfenicol)piperidine-4-yl]-6-(2-hydroxyethyl)carbamoylmethyl,
(333) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(1,3-dioxolane-2-ylmethyl)carbamoylmethyl,
(334) 1-[1-(2-florfenicol)piperidine-4-yl]-6-aminomethylphenol,
(335) 1-[1-(4-chlorphenyl)piperidine-4-yl]-6-acetamidomethyl,
(336) 1-[1-(3-florfenicol)piperidine-4-yl]-6-acetamidomethyl,
(337) 1-[1-(4-methoxyphenethyl)piperidine-4-yl]-6-acetamidomethyl
(338) 1-[1-(2-florfenicol)piperidine-4-yl]-6-acetamidomethyl,
(339) 1-[1-(4-perfectil)piperidine-4-yl] -6-(2,4-imidazolidinedione-3-yl)methylindole,
(340) 1-[1-(4-florfenicol)piperidine-4-yl]-6-isobutylamino,
(341) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-imidazolidinyl)methylindol,
(342) 1-{1-[4-(4-forfinal)butyl]piperidine-4-yl}-6-acetamidomethyl,
(343) 1-[1-(2,4-divertenti)piperidine-4-yl]-6-acetamidomethyl,
(344) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(2-pyrrolidone-1-yl)methylindole,
(345) 1-[1-(4-florfenicol)piperidine-4-yl]-G-N-methylacetanilide,
(346) 1-{1-[3-(4-forfinal)propyl]piperidine-4-yl}-6-acetamidomethyl,
(347) 1-[1-(4-florfenicol)piperidine-4-yl]-6-N-methylaminoethanol
(348) 1-[1-(4-florfenicol)piperidin the ol,
(350) 1-[1-(4-florfenicol)piperidine-4-yl]-6-hydroxyacetylamino,
(351) 1-[1-(4-florfenicol)piperidine-4-yl]-6-diferecutremurator,
(352) 1-[1-(4-florfenicol)piperidine-4-yl]-6-fioricetmedication,
(353) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(3-chloropropylamine)methylindol,
(354) 1-[1-(4-florfenicol)piperidine-4-yl] -6-imidazolidinylideneamino,
(355) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(3-hydroxypropylamino)methylindol,
(356) 1-[1-(4-florfenicol)piperidine-4-yl] -3-formyl-6-acetamidomethyl,
(357) 1-[1-(4-florfenicol)piperidine-4-yl] -3-hydroxymethyl-6-acetamidomethyl,
(358) 1-[1-(4-florfenicol)piperidine-4-yl]-6-characaterization,
(359) 1-[1-(4-florfenicol)piperidine-4-yl]-6-bromoacetonitrile,
(360) 1-[1- (4-florfenicol) piperidine-4-yl]-6-(N,N-dimethylaminoacetyl)methylindol,
(361) 1-[1-(4-florfenicol)piperidine-4-yl]-6-[(piperidinyl)acetamido]methylindol,
(362) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(3-bromopropylamine)methylindol,
(363) 1-[1-(4-florfenicol)piperidine-4-yl] -6-(3-N,N-dimethylaminopropionic)aminomethylphenol,
(364) 1-[1-(4-florfenicol)piperidine-4-yl]-6-[3-(piperidine-1-yl)propionamido]methylindol,
(365) 1-[1-(2-florfenicol)piperidine-4-yl]-6-propionylthiocholine,
(366) 1-[1-(2-florfenicol)PI is Jindal,
(368) 1-[1-(2-florfenicol)piperidine-4-yl]-6-hydroxyacetylamino,
(369) 1-[1-(4-florfenicol)piperidine-4-yl] -6-methoxycarbonylaminophenyl,
(370) 1-[1-(4-florfenicol)piperidine-4-yl] -6-N,N-dimethylaminocarbonylmethyl,
(371) 1-{1-[2-(3-pyridyl)ethyl]piperidine-4-yl}-6-acetamidomethyl,
(372) 1-{ 4-[(1-hydroxyethyl)phenethyl] piperidine-4-yl} -6-acetamidomethyl,
(373) 1-[1-(4-bromophenetole)piperidine-4-yl]-6-acetamidomethyl,
(374) 1-[1-(2-florfenicol)piperidine-4-yl]-6-formylindole,
(375) 1-[1-(2-florfenicol)piperidine-4-yl]-6-hydroxymethylene,
(376) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(1-hydroxyacyl)indole,
(377) 1-[1-(4-florfenicol)piperidine-4-yl]-6-freedomlolita,
(378) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(3-methylurea)methylindol and
(379) 1-[1-(4-florfenicol)piperidine-4-yl]-6-(3-methylurea)methylindole) are studied.

12. 1,4-Substituted derivative of a cyclic amine under item 1 or its pharmacologically acceptable salt for the treatment of diseases, for which effective antagonism to serotonin.

13. 1,4-Substituted derivative of a cyclic amine under item 1, in which the connection
in the formula (I)
is a single bond, represented by formula (XXI)

where As, In the Noe-derived cyclic amine under item 1, in which in the formula (I) m = 0, is represented by the formula (XXII)

where a, b, C, D, Z, n, m, p, R1- R5defined in paragraph 1,
or its hydrochloride, hydrobromide, oxalate.

15. 1,4-Substituted derivative of a cyclic amine under item 1, in which in the formula (I) m = 1, 2,
or its hydrochloride, hydrobromide, oxalate.

16. 1,4-Substituted derivative of a cyclic amine under item 15, selected from the following compounds:
1-[1-(4-florfenicol)piperidine-4-yl]methylindolin,
1-{2-[1-(4-florfenicol)piperidine-4-yl]ethyl}of indolin and
1-[(1-ethylpiperazin-4-yl)methyl]-3-(4-methoxybenzyl)indoline,
or its pharmacologically acceptable salt.

17. 1,4-Substituted derivative of a cyclic amine under item 1 of the formula (XXIII)

where a, b, C, D, Z, n, m, p, R1- R5defined in paragraph 1,
or its pharmacologically acceptable salt.

18. 1,4-Substituted derivative (XXIII) a cyclic amine under item 17, selected from the following compounds:
7-[1-(4-florfenicol)piperidine-4-ilidene]-5,6-dihydropyridines
5-[1-(4-florfenicol)piperidine-4-ilidene] -7-methyl-5,6-dihydrocyclopenta, or its pharmacologically acceptable salt.

19. 1,4-Substituted derivative of a cyclic amine under item 1, in which the connection

or its pharmacologically acceptable salt.

20. The drug, which has antagonistic to serotonin activity, containing as the active substance 1,4-substituted derivative of a cyclic amine under item 1 or its pharmacologically acceptable salt.

21. Means on p. 20 for the treatment, reduction and prevention of diseases for which effective antagonism to serotonin.

22. Means on p. 21, where the disease is spastic paralysis.

23. Means on p. 20, which represents a muscle relaxant.

24. The method of obtaining 1,4-substituted derivative of a cyclic amine of formula (X)

where the relationship represented by the formula

A, b, C, D, R1- R5, n and p are defined in paragraph 1,
which involves removal of the protective groups of the 1,4-substituted derivative of a cyclic amine of formula (IX)

where the relationship represented by the formula

A, b, C, D, R1- R4, n and p are defined in paragraph 1;
Pr.G represents hydrogen or a protective group,
and then the realization of interaction that is derived from L-R5(where R5defined in paragraph 1, L - go engagement condensed cyclic amine of formula (VII)

where the relationship represented by the formula

A, b, C, D, R1, R2, R3and n are defined in paragraph 1,
with a cyclic ketone of formula (VIII)

where R4, p, and Pr.G defined above,
in the presence of a reducing agent to obtain 1,4-substituted derivative (X) cyclic amine, destruction of derived, if necessary, the protective group and then the implementation of its interaction with L-R5.

26. A method of treating diseases, for which effective antagonism to serotonin, which includes an introduction to the patient an effective dose of 1,4-substituted derivative of a cyclic amine under item 1 or its pharmacologically acceptable salt.

Priority points and features:
31.03.1997 on PP.1-19 excluding compounds in which the connection

represents a double bond, R1and R2the same or different from each other and each represents a lower alkylsulfonyl, halogen-substituted lower alkylsulfonyl, 1-hydroxy-1-(methoxyphenyl)methyl, methoxyprogesterone, 1,3-propanesultone-2-yl, lower hydroxydiphenylamine acylaminoalkyl, R3- formyl, n = 3;
26.12.1997 on PP.20 - 26;
31.03.1998 on p. 1-19 (excluded above link).

 

Same patents:

The invention relates to 2-(iminomethyl)aminoaniline derivative of General formula I, And where the aromatic residue of the formula Ia, R1and R2independently H, halogen, HE, linear or branched C1-C6alkyl, linear or branched C1-C6alkoxyl, R3-H, linear or branched C1-C6alkyl, or-COR4where R4-C1-C6alkyl or the residue IC, linear or branched C1-C6the five-membered alkyl or a heterocycle containing 1-4 heteroatoms selected from O, S, N, and in particular: thiophene, furan, pyrrole or thiazole, carbon atoms which is unsubstituted or substituted by one or more groups selected from linear or branched C1-C6of alkyl, C1-C6alkoxyl or halogen; X is-CO-N(R3)-X'-, -NH-CO-X'-, -CH=,-CO -, or a bond, and X' represents -(CH2)n- where n = 0-6; Y means Y'-, -Y'-NH-CO-, -CO-Y', Y'-CO-, -N(R3)-Y'-, -Y,-N(R3)-, Y'-CH2-N(R3)-CO-, -Y'-O-, -Y'-O-Y' - or a bond, and Y' is -(CH2)n- where n = 0-6; Неt-pyrrole, pyrrolidine, furan, thiophene, imidazole, imidazoline, oxazole, isoxazol, oxazoline, isoxazole, thiazole, thiazoline, thiazolidine, thiazolidine, azetidine, piperidine, imidazolidine, they

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The invention relates to a derivative of 1,2,4-thiadiazole, substituted in the 5-position of General formula I, in which X Is N; R1- C1-6alkyl; R2is hydrogen, R3, R4and R5each independently selected from hydrogen; trifloromethyl;is Ar2, Ar2CH2or Het2; AG2is phenyl; Het2is a monocyclic heterocycle selected from thiadiazolyl, pyridinyl, pyrimidinyl or pyrazinyl, their N-oxide forms, the pharmaceutically acceptable acid additive salts and stereochemical isomeric forms

The invention relates to organic chemistry, namely to new derivatives of benzoperylene

The invention relates to the derivatives of pyrrolidine formula I

< / BR>
where R1- H, C1-C6alkyl; phenyl, possibly substituted; biphenyl, possibly substituted; 1H, 5H - pyrido [3,2,1-ij] chinolin; phenyl WITH1-C6alkyl, optionally substituted; biphenyl WITH1-C6alkyl, optionally substituted; biphenylcarboxylic; terphenyl; naphthyl, optionally substituted; Z denotes-S-, -O-, -och2-, -N(R16), where R16- H, C1-C6alkyl, C3-C8cycloalkyl1-C6alkyl, panels1-C6alkyl, a chemical bond; X1means-CO-, -(CH2)r-CO-N(R17), where R17means H, C1-C6alkyl (where r = 0 or 1), -CH2NHSO2-, -(CH2)s-N (R18)-CO- (where R18- N, s=1-3), - CH2NHCОСН2O-, -CH2N (R19Of PINES = CH- (where R19- H, -CH2OCH2-, -CH2-N (R20)-CH2- (where R20- H, C1-C6alkyl, C1-C6alkylsulphonyl, phenylcarbinol)1-C5alkylen,2-C4albaniles, a chemical bond; X2- phenylene, optionally substituted hydroxy, theoffender, purandar, piperidinyl,< / BR>
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R2and R3each - H; and R4- phenyl, possibly substituted with halogen; R5- phenyl, possibly substituted; a cycle of G is phenyl,3-C7cycloalkyl, pyridyl, thienyl; loop J is phenyl; L is phenyl; p=0-2;----- means the presence or absence of chemical bonding;displays a CIS - or TRANS-configuration D relative to E; provided that X1means-CH2NHCО-, X2means 1,4-phenylene and X3means a chemical bond or a C1-C5alkylen, when the carbon atom bound CD and adjacent carbon atom in the cycle are connected by a simple relation and V1does not mean a chemical bond, when X1means-CH2O-; and pharmaceutically acceptable salt or hydrate of the compound

The invention relates to a method for the preparations of thiazolidinediones of the formula III, where a denotes CH=CH or S, W is O; X Is S, O or NR2where the remainder R2is hydrogen or C1-C6by alkyl; Y is CH or N; R is naphthyl, thienyl or phenyl, which optionally one - or twofold substituted C1-C3the alkyl, CF3C1-C3alkoxygroup, F, Cl or bromine; R1is hydrogen, C1-C6alkyl and n = 1-3, by restoring the compounds of formula IV metal aluminum in proton solvent

The invention relates to new derivatives of 2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole of the formula I, in which R1means a hydrogen atom, a C1-4alkyl group or phenyl group which may be substituted by 1 to 3 substituents selected from the group consisting of halogen atom, hydroxy-group, nitro group, WITH1-4alkoxygroup, (C1-4alkyl) amino and di(C1-4alkyl)amino group; or a group of formula (a) Z means a hydrogen atom or a C1-4alkoxygroup, R0means a group of the formula Alk-NR4R5where Alk is alkalinous group having a straight or branched C1-6chain, one of R2and R3is amino and the other is an amino group or a 5-6-membered saturated heterocyclic group containing one or two atom(s) of nitrogen and/or oxygen and attached via its nitrogen atom, and the specified heterocyclic group may be substituted WITH1-4alkyl group, phenyl group or kalogeropoulou group, or the last of the R2and R3is a group of the formula - SR

The invention relates to new bicyclic to carboxamide formula (i) in which (1) X represents N and (a) Z is =CR1-CR2and Y is N, Z is =CR1and Y represents O, S or NR4or (C) Z is = CR1-N= and Y represents CR2or (2), X represents NR4Z represents CR1= and Y is N, Q is O, R1and R2are СОR6, C(= NOR6R13, alkyl-C(=NOR6R13, NR8R9, CF3or R6, R3is1-6alkoxygroup, R4represents H or alkyl, R5is heteroaryl, optionally substituted with halogen, alkyl, CONR11R12, CF3or CN, aryl, substituted with halogen; R6represents H, alkyl, cycloalkyl, aryl, heteroaryl, heterocycle, arylalkyl, heteroaromatic or heteroseksualci, R7represents alkyl, hydroxy, OR10, NR8R9CN, CO2H, CO2R10, CONR11R12, R8and R9represent H or alkyl, or NR8R9represents a heterocyclic ring, optionally substituted by R14, R10represents an alkyl, heterocycle, R11and R12represent H or alkyl, and the salts

The invention relates to organic chemistry, namely to new derivatives of benzoperylene

The invention relates to new substituted pyrazolylborate General formula (I) in which R1-R6have the meanings given in the description of the invention

The invention relates to piperazine derivatives of the formula I, in which R1denotes a substituted radicals CN or Hal indole-3-ilen residue, R2denotes unsubstituted 2-oxo-2H-1-benzopyran-6-yl or 2-oxo-2H-1-benzopyran-4-yl

The invention relates to novel azole compounds having antifungal activity, their preparation and application

The invention relates to 1,4-disubstituted the piperazines of General formula I, the method of production thereof, containing compositions and their use for the clinical treatment of painful conditions, increased pain sensitivity and/or inflammatory conditions in which the pathophysiological role of C-fibers, causing neurogenic pain or inflammation
The invention relates to an improved process for the preparation of doxazosin, which is known antihypertensive agent used in hypertension and prostate cancer

The invention relates to new imidazole derivative of General formula (1), where n1is an integer from 1 to 3, a represents hydrogen, linear or branched C1-C10-alkyl, which may be optionally substituted C3-C7-cycloalkyl or lower alkoxy, or a radical selected from the group shown in the formula of the invention, Y represents a radical selected from the group described in the claims, or to his new pharmaceutically acceptable salts
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