New cyclic diamine compounds containing them medicines and methods of treatment

 

The invention relates to new cyclic diamine compounds of the formula I, whererepresents an optionally substituted divalent residue of benzene, where the substituents are selected from unsubstituted lower alkyl groups, unsubstituted lower alkoxygroup, unsubstituted lower acyl group, a lower allylthiourea, lower alkylsulfonyl group, halogen atom, etc. or unsubstituted pyridine; Ar represents a phenyl group which may be substituted by one to four groups selected from unsubstituted lower alkyl group, the unsubstituted alkoxygroup, low allylthiourea, lower alkylsulfonyl group, and so on, optional substituted amino group, alkylenedioxy; X is-NH-, oxygen atom or sulfur atom; Y is a sulfur atom, sulfoxide or sulfon; Z represents a single bond or-NR2-; R2- the atom of hydrogen or unsubstituted lower alkyl group; l = 2 or 3; m = 2 or 3; n = 1, 2, or 3, or their salts, or their solvate. Pharmaceutical composition having ACAT-inhibiting action, containing the compound of formula I or its salt in an effective amount and a pharmaceutically acceptable carrier. A method of treating or preduprejdaet or aneurysm of the aorta by the patient, suffering from hyperlipemia, arteriosclerosis, cerebrovascular disorders, ischemic cardiopathy, ischemic enteropathy or aortic aneurysm, an effective amount of the compounds of formula I, or salts thereof, or MES. The technical result - the new cyclic diamine compounds having ACAT-inhibiting action. 6 C. and 5 C.p. f-crystals, 22 PL.

Description text in facsimile form (see graphic part).

Claims

1. The compound of formula (I) or its salt, or its MESwhererepresents an optionally substituted divalent residue of benzene, where the substituents are selected from unsubstituted lower alkyl groups, unsubstituted lower alkoxygroup, unsubstituted lower acyl group, a lower allylthiourea, lower alkylsulfonyl group, halogen atom, alkoxycarbonyl group, hydroxyalkyl group, halogenide alkyl group, alkoxyalkyl group, pyrazole, nitro, imidazole or unsubstituted pyridine; AG represents phenyl, pyridyloxy or pyramidalnou group, which neobyazatelnostyu, alkoxyalkyl, alkoxycarbonylmethyl, low allylthiourea, lower alkylsulfonyl group, lower alkylsulfonate, hydroxy-group, unsubstituted lower alloctype, nitro, di-(lower alkoxy)phosphoryloxy, optionally substituted amino, alkylenedioxy; X is-NH-, oxygen atom or sulfur atom;
Y is a sulfur atom, sulfoxide or sulfon;
Z is a single bond or-NR2-;
R2represents a hydrogen atom or optionally substituted lower alkyl group;
l = 2 or 3;
m = 2 or 3;
n = 1, 2, or 3.

2. The compound of formula (II) or its salt, or its MES

where

represents an optionally substituted divalent residue of benzene, where the substituents are selected from unsubstituted lower alkyl groups, unsubstituted lower alkoxygroup, unsubstituted lower acyl group, a lower allylthiourea, lower alkylsulfonyl group, halogen atom, alkoxycarbonyl group, hydroxyalkyl group, halogenide alkyl group, alkoxyalkyl group, pyrazole, nitro, imidazole or unsubstituted pyridine;
X is-NH-, oxygen atom or AOI phenyl group, which is optionally substituted with one to four groups selected from unsubstituted lower alkyl group, the unsubstituted alkoxygroup, alkoxyalkyl, alkoxycarbonylmethyl, low allylthiourea, lower alkylsulfonyl group, lower alkylsulfonate, hydroxy-group, unsubstituted lower alloctype, nitro, di-(lower alkoxy)phosphoryloxy, optionally substituted amino, alkylenedioxy, peredelnoj group, which is optionally substituted with one to four groups selected from unsubstituted lower alkyl group, the unsubstituted alkoxygroup,low allylthiourea, or pyrimidines group, which is optionally substituted lower alkylthiol;
R2is a hydrogen atom or optionally substituted lower alkyl group;
l = 2 or 3;
m = 2 or 3;
n = 1, 2, or 3.

3. The compound of formula (III) or its salt, or its MES:

where X is-NH-, oxygen atom or sulfur atom;
Y is an oxygen atom, a sulfur atom, sulfoxide or sulfon;
Z is a single bond or-NR2-;
AG' is a phenyl group which is optionally substituted with one to four groups selected from unsubstituted who Issa allylthiourea, lower alkylsulfonyl group, lower alkylsulfonate, hydroxy-group, unsubstituted lower alloctype, nitro, di-(lower alkoxy)phosphoryloxy, optionally substituted amino, alkylenedioxy; peredelnoj group, which is optionally substituted with one to four groups selected from unsubstituted lower alkyl group, the unsubstituted alkoxygroup, low ancilliary or pyrimidines group, which is optionally substituted lower alkylthiol;
R2is a hydrogen atom or optionally substituted lower alkyl group;
R3, R4and R5identical or different, represent a hydrogen atom, unsubstituted lower alkyl group, the unsubstituted alkoxygroup, optionally substituted lower acyl group, a lower allylthiourea, lower alkylsulfonyl group, halogen atom, alkoxycarbonyl group, hydroxyalkyl group, halogenide alkyl group, alkoxyalkyl group, a nitrogroup, or imidazole;
1 = 2 or 3;
m = 2 or 3;
n = 0, 1, 2, or 3.

4. The compound of formula (IV) or its salt, or its MES:

where

predstavljena bond or-NR2-;
AG' is a phenyl group which is optionally substituted from one to four unsubstituted lower alkyl groups, peredelnoj group, which is optionally substituted with one to four groups selected from unsubstituted lower alkyl groups, lower ancilliary;
R2represent a hydrogen atom or optionally substituted lower alkyl group;
R6and R7- hydrogen atoms;
1 = 2 or 3;
m = 2 or 3;
n = 0, 1, 2, or 3.

5. Pharmaceutical composition having ACAT-inhibiting action, containing the effective ingredient and a pharmaceutically acceptable carrier, characterized in that as an effective ingredient it contains a compound according to any one of paragraphs. 1-4, or salt, or MES in an effective amount.

6. The pharmaceutical composition according to p. 5, representing an ACAT inhibitor, an agent for suppressing transport of intracellular cholesterol, agent for reducing blood cholesterol or agent for suppressing the foaming of macrophages.

7. The pharmaceutical composition according to paragraphs.5 and 6, with ACAT-inhibiting action, used for the treatment and prevention of hyperlipemia, arteriosclerosis, cerebrovascular naru is p. 1-4, or its salt with ACAT-inhibiting action.

9. Connection on p. 8, representing an ACAT inhibitor, an agent for suppressing transport of intracellular cholesterol, agent for reducing blood cholesterol or agent for suppressing the foaming of macrophages for the treatment and prevention of hyperlipemia, arteriosclerosis, cerebrovascular disorders, ischemic cardiopathy, ischemic enteropathy or aortic aneurysm.

10. The method of treatment or prevention hyperlipemia, arteriosclerosis, cerebrovascular disorders, ischemic cardiopathy, ischemic enteropathy or aortic aneurysm by introducing a patient suffering from hyperlipemia, arteriosclerosis, cerebrovascular disorders, ischemic cardiopathy, ischemic enteropathy or aortic aneurysm, an effective amount of a compound according to any one of paragraphs.1 to 4, or its salt, or MES.

11. A method of treating or preventing under item 10, where the effective amount is entered as an ACAT inhibitor, an agent for suppressing the transport of intracellular cholesterol, agent for reducing blood cholesterol or agent for suppressing the foaming of macrophages.

 

Same patents:

The invention relates to new heterocyclic o-dicarbonitrile formula (I), where

< / BR>
The compounds obtained can be used to obtain hexatriene-fluorophores

The invention relates to a new 1.8-fused derivative of 2-Hinayana formula (I), where A, X, R1, R2, R3, R4, R5, R6such as defined in the claims

-converting enzyme)" target="_blank">

The invention relates to novel ortho-sulfonamidophenylhydrazine heteroaryl hydroxamic acids of the formula

< / BR>
where W and X are both carbon, T is nitrogen, U represents CR1where R1represents hydrogen, or alkyl containing 1-8 carbon atoms, R represents-N(CH2R5)-SO2Z, Q represents -(C=O)-NHOH, with

< / BR>
is a benzene ring, or is a heteroaryl ring of 5 to 6 atoms in the cycle, which may contain 0-2 heteroatoms selected from nitrogen, oxygen and sulfur, in addition to the heteroatom of nitrogen, denoted as W, where benzene or heteroaryl ring may optionally contain one or two substituent R1where permissible; Z is phenyl, which is optionally substituted by phenyl, alkyl with 1-8 carbon atoms, or a group OR2; R1represents halogen, alkyl with 1-8 carbon atoms, alkenyl with 2-6 carbon atoms, perfluoroalkyl from 1 to 4 carbon atoms, phenyl, optionally substituted by 1-2 groups OR2group-NO2group -(CH2)nZ, where Z is a phenyl which allows an alkyl with 1-8 carbon atoms, phenyl, optionally substituted with halogen, or heteroaryl radical containing 5 to 6 atoms in the cycle, including 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; R5represents hydrogen, alkyl with 1-8 carbon atoms, phenyl, or heteroaryl containing 5 to 6 atoms in the cycle, including 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; or their pharmaceutically acceptable salts

The invention relates to the field of organic chemistry, namely to new bicikliski derived pyrimidine

The invention relates to new benzoxazine and piridokshinom compounds of formula I, where part of the Q - condensed phenyl, or condensed pyridyl; Z1is hydrogen, halogen, C1-C6alkyl, phenyl, nitro, sulfonylamino or trifluoromethyl; Z2is hydrogen or halogen; X is hydrogen or oxygen; And - C1-C6-alkyl, C1-C6-alkylaryl or C1-C6-Alkylglucoside, where aryl and heterocyclyl described in the claims, n = 0 to 3; Y is the portion described in the claims, and their pharmaceutically acceptable salts, esters and proletarienne forms

The invention relates to new tricyclic pyrazole derivative or its pharmaceutically acceptable salt

The invention relates to compounds of formula (I):

< / BR>
where

-A= B-C= D - represents-CH=CH-CH=CH-group, in which 1 or 2 CH may be replaced by nitrogen;

Ar denotes phenyl or naphthyl, unsubstituted or one-, two - or three-fold substituted with H, Gal, Q, alkenyl with the number of C-atoms up to 6, Ph, OPh, NO2, NR4R5, NHCOR4, CF3, OCF3CN, OR4, COOR4, (CH2)nCOOR4, (CH2)nNR4R5, -N=C=O or NHCONR4R5phenyl or naphthyl;

R1, R2, R3each independently from each other, are absent or represent H, Gal, Q, CF3, NO2, NR4R5, CN, COOR4or CHCOR4;

R4, R5each independently of one another denote H or Q, or together also denote-CH2-(CH2)N-CH2-;

Q denotes alkyl with 1-6 C-atoms;

Ph denotes phenyl;

X denotes O or S;

Gal denotes F, Cl, Br or I;

"n" represents 1, 2 or 3;

and their salts, except 4-methyl-N-(2,1,3-benzothiadiazole - 5-yl)benzosulfimide, 4-nitro-N-(2,1,3-benzothiadiazole-5-yl)- benzosulfimide and 4-amino-N-(2,1,3-benzothiadiazole-5-yl)- benzolsulfonat

The invention relates to new derivatives isothiazolinones acid of the formula I, where R stands for a group-OR1or-SR2in which R1means alkyl with 1-6 carbon atoms, a substituted once residues selected from the group comprising halogenoalkanes with 1-6 carbon atoms and 1 to 5 halogen atoms, dialkylamino with 1-6 carbon atoms in each alkyl part, phenylalkyl with 1-4 carbon atoms in the CNS parts and pyrrolidinyloxyl with 1-4 carbon atoms in the CNS part, and twice by hydroxyl, or so, m and n is 2, R3means phenyl, R4means alkyl with 1-4 carbon atoms, R2means alkyl with 1-6 carbon atoms, or R2means phenylalkyl with 1-2 carbon atoms in the alkyl part, with the phenyl portion may be substituted with halogen

The invention relates to a new derivative of solidilin formula (I) where one of X, Y and Z represents C=O or C=S, and one of the remaining X, Y and Z denotes a group With=, and the other group C=S; R1, R2and R3are Deputy or X, Y and Z, or nitrogen atom and may be the same or different and denote hydrogen, halogen, hydroxy, nitro, etc., the group -(CH2)n-O - and may be joined through the nitrogen atom, or X, Y, Z, n is 1-4, Ar denotes a phenylene or naftilan, R4denotes hydrogen or forms a bond with group a, And denotes nitrogen or CR5, R5denotes hydrogen, halogen or forms a bond with R4In means O or S, when a is CR5and means that, when a is N, its tautomeric forms, stereoisomers, polymorphic forms, pharmaceutically acceptable salt and solvate

The invention relates to the derivatives of propanolamine formula (I) and their pharmaceutically acceptable salts, where R1and R2means phenyl, naphthyl, pyridyl, thienyl, pyrimidyl, thiazolyl, hinely, piperazinil, oxazolyl, which may be substituted with halogen, HE, NO2, NH2, COOH, etc., R3-R8mean hydrogen, hydroxyl, (C1-C8-alkoxy, NH2-THE OTHER9, -N(R9R10, R9-R10mean hydrogen or (C1-C8)alkyl, X is CH or N, Y represents CH or N, provided that the residues R1, R2X and Y are not simultaneously mean R1- phenyl, R2is phenyl, X is CH, Y is CH

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>
< / BR>
< / BR>
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 new heterocyclic compounds of the formula (I), where R1represents a group of formula (II), R is 2,4-dioxothiazolidine-5-ylmethylene group and others, And represents C1-6alkylenes group, A represents an oxygen atom, R4represents a substituted phenyl or pyridyl which may have a Deputy, R6represents a hydrogen atom or a C1-6alkyl group, D represents an oxygen atom or sulfur, E is a CH group or a nitrogen atom, or their pharmacologically acceptable salts

The invention relates to the derivatives of hintline formula I in which Z denotes-O-, -NH - or-S-; m = 1-5, integer, provided that when Z represents-NH-, m = 3 - 5; R1is hydrogen, C1-3alkoxy; R2is hydrogen; R3hydroxy, halogen, C1-3alkyl, C1-3-alkoxy, C1-3alkanoyloxy, trifluoromethyl or cyano; X1denotes-O-, -NR7, -NR8CO-, where R7and R8each is hydrogen, C1-3alkyl; R4choose one of the listed in paragraph 1 of the claims of the seven groups, except 4-(3,4,5-trimethoxyphenyl)-6,7-dimethoxyquinazoline, 4-(3-methoxybenzylthio)-6,7-dimethoxyquinazoline, 4-(3-chlorophenylthio)-6,7-dimethoxyquinazoline, 4-(3-chlorophenoxy)-6,7-dimethoxyquinazolin and 4-(3,4,5-trimethoxyaniline)-6,7-dimethoxyquinazolin, or their salts

The invention relates to the derivatives of hintline formula (I), where Y1represents-O-, -S-, -NR5CO-, where R5is hydrogen; R1represents hydrogen or C1-3alkoxy; R2represents hydrogen; m is an integer from 1 to 5; R3represents hydroxy, halogen, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl or cyano; R4is one of five groups, which is optionally substituted by Spiridonova, phenyl or aromatic heterocyclic group with 1-3 heteroatoms selected from O, N and S, or contains such a group; and their salts, to processes for their preparation and to pharmaceutical compositions containing a compound of the formula (I) or its pharmaceutically acceptable salt as an active ingredient

The invention relates to a method for producing derivatives of 2-aminothiazoline formula I, in which R1represents C1-5alkyl straight or branched chain, R2is1-3alkyl, by reacting the compounds of formula II in which R3represents phenyl which may be optionally mono-pentamidine independently chlorine, methoxy, ethoxy, phenoxy or nitro, with the compound of the formula III in which Y represents a leaving group, in a solvent and in the presence of a base

The invention relates to a derivative of benzamidine formula I, where R1denotes-C(=NH)-NH2; R2denotes H; R3refers to -[C(R5)2]m-СООR5, R3and X together represent well-CO-N-, form a 5-membered ring, with R3refers to - C = O, and X denotes N, R4means And, cycloalkyl, -[C(R5)2]mAr; X represents O, NR5or CH2Y represents O, NR5N[C(R5)2]m-Ar, N[C(R5)2]m-Het, - N[C(R5)2]m-СООR5W represents a bond, -SO2-, -CO - or-СОNR5-
Up!