Derivatives of 7-aryl-3,9-diazabicyclo(3,3,1)non-6-ene-rhenin inhibitors

FIELD: chemistry.

SUBSTANCE: derivatives of 7-aryl-3,9-diazabicyclo(3.3.1)non-6-ene of general formula I , general formula I, where X and W or both represent -CH-, or one of them represents -CH-, and the other -N. V represents -A-(CH2)s-, -(CH2)s-A-, -A-(CH2)v-B- or -CH2-A-(CH2)3-B-; A and B represent-O- U -phenyl, possibly 1-3 substituted with halogen, alkyl, alkoxy, CF3, CF3O - or alkylcarbonyl, or pyridyl, monosubstituted with cyanogroup. T represents -CONR1-, -(CH2)pOCO- or -(CH2)pN(R1)CO- Q-alkylene; M - hydrogen, phenyl, possibly substituted, benzo[1,3]dioxol, possibly substituted, or pyridyl; L represents -R3, -COR3, -COOR3, -CONR2R3 or -SO2R3; R1 - hydrogen, alkyl, C3-7 cycloalkyl, pyrrolidinyl, benzo[b]thienyl, chinoxalinyl, phenylalkyl, thienylalkyl or tetrazolylalkyl, possibly substituted. m=1, n=0 or m=0, n=1, p - integer 1-4, s - integer 2-5, v - integer 2-4, optically pure enantiomers, mixtures of enantiomers, pharmaceutically acceptable salts and complexes with solvents, possessing activity of phenin inhibitors.

EFFECT: efficient application in medicine for treatment of cardio-vascular diseases and renal failure.

8 cl, 743 ex

 

The text descriptions are given in facsimile form.

1. Compounds of General formula I

in which

X and W both represent a group-CH - or one of them represents a group-CH-and the other is a nitrogen atom;

V denotes-A-(CH2)s-, -(CH2)s-A-, -A-(CH2)v-B - or-CH2"And CH2-CH2-CH2- - ;

A and b represent-O-;

U denotes phenyl, optionally substituted by 1-3 substituents, independently selected from the group comprising halogen, (ness.)alkyl, (ness.)alkoxy, trifluoromethyl, triptoreline or (ness.)alkylsulphonyl;

or U denotes pyridyl, monosubstituted by cyano;

T denotes-CONR1-, -(CH2)pOCO -, or -(CH2)pN(R1)CO-;

Q denotes (ness.)alkylen;

M denotes a hydrogen atom, phenyl, optionally substituted by 1-3 substituents, independently selected from the group comprising hydroxyl, halogen, (ness.)alkyl, hydroxy(ness.)alkyl, (ness.)alkoxy, trifluoromethyl and thrift is methoxy; benzo[1,3]dioxol, optionally monosubstituted by halogen; or pyridyl;

L denotes-R3, -COR3, -COOR3, -CONR2R3or-SO2R3;

R1denotes a hydrogen atom, (ness.)alkyl or cycloalkyl;

R3denotes a hydrogen atom, (ness.)alkyl, cycloalkyl, pyrrolidinyl; benzo[b]thienyl; honokalani; phenyl(ness.)alkyl, (halo-phenyl)-(ness.)alkyl; thienyl(ness.)alkyl or tetrazolyl(ness.)alkyl; where these groups may be unsubstituted or mono-, di - or tizamidine by hydroxyl, -OCOR2, -COOR2, cyano, -CONR2R2'- WITH-morpholine-4-yl or-NH2provided that the carbon atom bound at most to one heteroatom in case this carbon atom is sp3-hybridized;

R2and R2' independently denote a hydrogen atom or (ness.)alkyl,

m represents the integer 1, and n denotes an integer of 0 or n denotes an integer of 1 and m represents the integer 0;

p denotes an integer of 1, 2, 3 or 4;

s denotes the integer 2, 3, 4, or 5; and

v denotes the integer 2, 3 or 4;

and optically pure enantiomers, mixtures of enantiomers, such as racemates, diastereoisomer, a mixture of diastereoisomers, diastereoisomeric of the racemates, mixtures diastereoisomeric racemate and mesoform; there are also pharmaceutically acceptable salts and complexes with solvents, when this concept "(ness.)alkyl", "(ness.)alkoxy", "(ness.)alkylene", and "cycloalkyl" have the following meanings:

"(ness.)alkyl", alone or in combination with other groups, means saturated remotemachine and branched groups containing from one to seven carbon atoms, which may be optionally substituted by halogen atoms;

"(ness.)alkoxy" refers to the group R-O in which R denotes (ness.)alkyl;

"(ness.)alkylen", alone or in combination with other groups, denotes remotemachine and branched groups containing olefinic bond and containing from two to seven carbon atoms, which may be optionally substituted by halogen atoms;

"cycloalkyl" alone or in combination refers to saturated cyclic hydrocarbon ring system containing from 3 to 7 carbon atoms.

2. Compounds of General formula I according to claim 1, in which X, W, V, U, T, Q, L and M have the meanings indicated in claim 1, and n represents 0, m represents 1, and optically pure enantiomers, mixtures of enantiomers, such as racemates, diastereoisomer, a mixture of diastereoisomers, diastereoisomeric of the racemates, mixtures diastereoisomeric racemate and mesoform; and pharmaceutically acceptable salts and complexes with solvents.

3. Compounds of General formula I according to claim 1, in to the ora X, W, V, U, L, M, m, and n have the meanings indicated in claim 1, and T denotes-CONR1; Q represents methylene; and optically pure enantiomers, mixtures of enantiomers, such as racemates, diastereoisomer, a mixture of diastereoisomers, diastereoisomeric of the racemates, mixtures diastereoisomeric racemate and mesoform; and pharmaceutically acceptable salts and complexes with solvents.

4. Compounds of General formula I according to claim 1, in which X, W, U, L, T, Q, M, m, and n have the meanings indicated in claim 1, and V denotes-CH2CH2O-, -CH2CH2CH2O -, or-OCH2CH2O-; and optically pure enantiomers, mixtures of enantiomers, such as racemates, diastereoisomer, a mixture of diastereoisomers, diastereoisomeric of the racemates, mixtures diastereoisomeric racemate and mesoform; and pharmaceutically acceptable salts and complexes with solvents.

5. Compounds of General formula I according to claim 1, in which V, U, T, Q, M, L, m and n have the meanings indicated in claim 1, and X and W represent a group-CH-, and optically pure enantiomers, mixtures of enantiomers, such as racemates, diastereoisomer, a mixture of diastereoisomers, diastereoisomeric of the racemates, mixtures diastereoisomeric racemate and mesoform; and pharmaceutically acceptable salts and complexes with solvents.

6. Compounds of General formula I according to claim 1, in which X, W, V, Q, T, M, L, m and n have the meanings indicated in claim 1, and U denotes m the but, di - or tizamidine phenyl, where the substituents are halogen atoms, (ness.)alkyl or (ness.)alkoxy, and optically pure enantiomers, mixtures of enantiomers, such as racemates, diastereoisomer, a mixture of diastereoisomers, diastereoisomeric of the racemates, mixtures diastereoisomeric racemate and mesoform; and pharmaceutically acceptable salts and complexes with solvents.

7. Compounds according to claim 1, selected from the group including

(1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3-(2-thiophene-2-ylacetic)-3,9-diazabicyclo[3.3.1]non-6-ene-6-ymetray ether (2-methoxyphenyl)acetic acid;

(1R*,5S*)-3-[2-(4-chlorophenyl)acetyl]-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-ymetray ether (2-methoxyphenyl)acetic acid;

(1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3-(cinoxacin-2-carbonyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-ymetray ether (2-methoxyphenyl)acetic acid;

[2-(2-chlorophenyl)ethyl]methylamide (1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(1R*,5S*)-3-(benzo[b]thiophene-3-carbonyl)-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl} -3,9-diazabicyclo[3.3.1]non-6-ene-6-ymetray ether (2-methoxyphenyl)acetic acid;

(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-ileti the new ether (2-methoxyphenyl)acetic acid;

(1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3-phenylmethanesulfonyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-eletrolytic (2-methoxyphenyl)acetic acid;

[2-(4-methoxyphenyl)ethyl]methylamide (1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-pertenece)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(1R*,5S*)-3-[2-(4-chlorophenyl)acetyl]-7-{6-[3-(2-methoxybenzyloxy)propoxy]pyridin-3-yl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-ymetray ether (2-methoxyphenyl)acetic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2,5-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

[2-(4-chlorophenyl)ethyl]methylamide (1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

[2-(3-chlorophenyl)ethyl]methylamide (1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

ethylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

[2-(3-methoxyphenyl)ethyl]methylamide (1R*,5S*)-3-acetyl-7-{4-[3-(2-what ethoxybenzoate)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3-methyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-ymetray ether (2-methoxyphenyl)acetic acid;

[2-(3,4-acid)ethyl]methylamide (1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2,3,5-trimethylphenol)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2,5-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dimethylphenoxy)ethyl]phenyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine ((1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(1R*,5S*)-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-ymetray ether (2-methoxyphenyl)acetic acid;/p>

N-((1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-ylmethyl)-2-(2-methoxyphenyl)-N-methylacetamide;

methylphenethylamine ((1R*,5S*)-3-acetyl-7-{4-[2-(2-tert-butyl-4-methylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2,5-divergence)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methyl(3-phenylpropyl)amide of(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2,3-dichlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2-acetylphenol)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

[2-(2-methoxyphenyl)ethyl]methylamide(1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

benzylmethylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2-methoxybenzyloxy)propoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2,5-divergence)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethylamine (1R*,5S*)-3-acetyl-7-[4-(2-o-tolylacetic)phenyl]-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methylphenethyl is d (1R*,5S*)-3-acetyl-7-{4-[2-(3-isopropylphenoxy)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2-chlorophenoxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(1R*,5S*)-5-[7-{4-[2-(2-bromo-5-pertenece)ethyl]phenyl}-6-(methylphenylcarbinol)-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl]-5-oxopentanoic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

2,2,2-trichloro-1,1-dimethylethylamine ether (1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid;

5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

methyl ester 5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acids;

(2 Chlorobenzyl)cyclopropylamine (1R,5S)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-Diaz is bicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1S,5R)-3-((1S,4R)-4-hydroxypyrrolidine-2-carbonyl)-7-{4-[3-(2,3,6-tryptophanate)propyl] phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-(4-carbamoylmethyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

resizetopreferred (1R*,5S*)-3-(4-carbamoylmethyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)ethylamide (1R*,5S*)-3-(4-carbamoylmethyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2-terbisil)amide of (1R*,5S*)-3-(4-carbamoylmethyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(3-trifloromethyl)amide of (1R*,5S*)-3-(4-carbamoylmethyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2-methylbenzyl)amide of (1R*,5S*)-3-(4-carbamoylmethyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropylacetylene (1R*,5S*)-3-(4-carbamoylmethyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

[2-(2-chlorophenyl)ethyl]cyclopropylamine (1R*,5S*)-3-(4-carbamoylmethyl)-7-{4-[3-(2,3,6-trip is orphenochs)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(3,5-dimethoxybenzyl)amide of (1R*,5S*)-3-(4-carbamoylmethyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(3R*)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acid and (3S*)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3R*)-5-((1R*,5S*)-6-(benzylcarbamoyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl} -3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3S*)-5-((1R*,5S*)-6-(benzylcarbamoyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3R*)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamate]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3S*)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamate]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3R*)-5-((1R*,5S*)-6-[cyclopropyl(2-terbisil)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3S*)-5-((1R*,5S*)-6-[cyclopropyl(2-terbisil)to rebamol]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acid;

(3R*)-5-((1R*,5S*)-6-[cyclopropyl(3-trifloromethyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3S*)-5-((1R*,5S*)-6-[cyclopropyl(3-trifloromethyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3R*)-5-((1R*,5S*)-6-[cyclopropyl(2-methylbenzyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3S*)-5-((1R*,5S*)-6-[cyclopropyl(2-methylbenzyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3R*)-5-((1R*,5S*)-6-{cyclopropyl[2-(4-methoxyphenoxy)ethyl]carbarnoyl}-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3S*)-5-((1R*,5S*)-6-{cyclopropyl[2-(4-methoxyphenoxy)ethyl]carbarnoyl}-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3R*)-5-((1R*,5S*)-6-[cyclopropyl(2-m-tolylacetic)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3S*)-5-((1R*,5S*)-6-[cyclopropyl(2-m-tolylacetic)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-the h-3-yl)-3-hydroxy-5-oxopentanoic acid;

(3R*)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropanecarbonyl}-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3S*)-5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropanecarbonyl}-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3R*)-5-((1R*,5S*)-6-[cyclopropyl(3,5-dimethoxybenzyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(3S*)-5-((1R*,5S*)-6-[cyclopropyl(3,5-dimethoxybenzyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-3-hydroxy-5-oxopentanoic acids;

(2 Chlorobenzyl)ethylamide (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(3,5-dimethoxybenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

5-((1R*,5S*)-6-(benzylcarbamoyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamate]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-6-[cyclopropyl(2-terbisil)carbarnoyl]-7-{4-[3-(2,3,6-tryptohan the XI)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-6-[cyclopropyl(3-trifloromethyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-6-[cyclopropyl(2-methylbenzyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-6-{[2-(2-chlorophenyl)ethyl]cyclopropanecarbonyl}-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-6-[cyclopropyl(3,5-dimethoxybenzyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-6-[cyclopropyl(2-n-triletal)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

methyl ester 5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamate]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acids;

methyl ester 5-((1R*,5S*)-6-[cyclopropyl(2-terbisil)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acids;

methyl ester 5-((1R*,5S*)-6-[cyclopropyl(3,5-dimethoxybenzyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acids;

5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamate]-7-{4-[3(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

5-((1R*,5S*)-6-[cyclopropyl(2-terbisil)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

5-((1R*,5S*)-6-[cyclopropyl(2-methylbenzyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

5-((1R*,5S*)-6-[cyclopropyl(3,5-dimethoxybenzyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

(2R*,3S*)-4-((1R*,5S*)-6-[cyclopropyl(2-methylbenzyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,3-dihydroxy-4-oxomalonate acids;

(2S*,3R*)-4-((1R*,5S*)-6-[cyclopropyl(2-methylbenzyl)carbarnoyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,3-dihydroxy-4-oxomalonate acids;

5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-[cyclopropyl(2-terbisil)carbarnoyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-5-oxopentanoic acid;

5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-{cyclopropyl[2-(3-methylphenoxy)ethyl]carbarnoyl}-3,9-diazabicyclo[3.3.1]-non-6-EN-3-yl}-5-oxopentanoic acid;

5-[(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-(cyclopropanecarbonyl)-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl]-5-oxopentanoic acid;

5-((1R*,5S*)-7-{4-[3-(2-bromo-5-torfin the XI)propyl]phenyl}-6-{[2-(2-chlorophenyl)ethyl]cyclopropanecarbonyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-{[2-(2,3-differenl)ethyl]cyclopropanecarbonyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-{[2-(2-were)ethyl]cyclopropanecarbonyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-{[2-(4-were)ethyl]cyclopropanecarbonyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-[cyclopropyl(3,5-dimethoxybenzyl)carbarnoyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-5-oxopentanoic acid;

methyl ester 5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-[cyclopropyl(3,5-dimethoxybenzyl)carbarnoyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-5-oxopentanoic acids;

5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-[cyclopropyl(2-terbisil)carbarnoyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-2,2-dimethyl-5-oxopentanoic acid;

5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-[cyclopropyl(2-methylbenzyl)carbarnoyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-2,2-dimethyl-5-oxopentanoic acid;

5-[(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-(cyclopropanecarbonyl)-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl]-2,2-dimethyl-5-oxopentanoic acid;

5-((1R*,5S*)-7-{4-[3-(2-bromo-5-perfe is hydroxy)propyl]phenyl}-6-{[2-(4-were)ethyl]cyclopropanecarbonyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-[cyclopropyl(3,5-dimethoxybenzyl)carbarnoyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-2,2-dimethyl-5-oxopentanoic acid;

(2R*,3S*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-[cyclopropyl(3,5-dimethoxybenzyl)carbarnoyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-2,3-dihydroxy-4-oxomalonate acid and (2S*,3R*)-4-{(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-[cyclopropyl(3,5-dimethoxybenzyl)carbarnoyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-2,3-dihydroxy-4-oxomalonate acids;

5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[2-(2,3,5-trimethylphenol)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-6-[(3-trifloromethyl)cyclopropanecarbonyl]-7-{4-[2-(2,3,5-trimethylphenol)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-6-[(2-methylbenzyl)cyclopropanecarbonyl]-7-{4-[2-(2,3,5-trimethylphenol)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamate]-7-{4-[2-(2,3,5-trimethylphenol)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

5-((1R*,5S*)-6-[cyclopropyl(2-terbisil)carbarnoyl]-7-{4-[2-(2,3,5-trimethylphenol)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)the filing]phenyl}-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-5-oxopentanoic acid;

5-{(1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-2,2-dimethyl-5-oxopentanoic acid;

(2 Chlorobenzyl)cyclopropylamino 5-{(1R*,5S*)-4-[3-(2-bromo-5-pertenece)propyl]phenyl}-3-(4-carbamoylmethyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

methyl ester 5-((1R*,5S*)-6-(benzylcarbamoyl)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acids;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl(2-methylbenzyl)carbarnoyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-5-oxopentanoic acid;

5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl(3,5-dimethoxybenzyl)carbarnoyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-5-oxopentanoic acid;

5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

5-((1R*,5S*)-6-[(2-Chlorobenzyl)ethylcarbamate]-7-{4-[2-(2-chloro-4,5-is immiltenali)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

5-{(1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-[cyclopropyl(2-terbisil)carbarnoyl]-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl}-2,2-dimethyl-5-oxopentanoic acid;

5-((1R*,5S*)-6-[cyclopropyl(3,5-dimethoxybenzyl)carbarnoyl]-7-{4-[2-(2,3,5-trimethylphenol)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-6-[cyclopropyl(2-n-triletal)carbarnoyl]-7-{4-[2-(2,3,5-trimethylphenol)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-6-{cyclopropyl[2-(2-hydroxyethyl)benzyl]carbarnoyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acid;

5-((1R*,5S*)-6-(cyclopropanecarbonyl)-7-{4-[2-(2,3,5-trimethylphenol)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-2,2-dimethyl-5-oxopentanoic acid;

(2 Chlorobenzyl)ethylamide (1R*,5S*)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

3-dimethylamide-6-[(2-Chlorobenzyl)cyclopropylamino] (1R*,5S*)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylic acid;

3-diethylamide-6-[(2-Chlorobenzyl)cyclopropylamino] (1R*,5S*)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3,6-dicarboxylic acid;

methyl ester of (1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]the dryer is l}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboxylic acid;

ethyl ester of (1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-3-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-methanesulfonyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-econsultancy-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

ethyl ester of 5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-5-oxopentanoic acids;

4-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-yl)-4-oxomalonate acid;

ethyl ester of 3-[((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-carbonyl)amino]propionic acid;

ethyl ether (rat.)4-[((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-carbonyl)amino]butyric acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-(3-carbamoylbiphenyl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-(2-HYDR shall Xianity)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R,5S)-3-((3R)-3-hydroxybutyryl)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-((1R*,2S*)-2-hydroxycyclohexanone)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid and (2-Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-((1S*,2R*)-2-hydroxycyclohexanone)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-9-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-yl)-5-oxopentanoic acid;

ethyl ester of 5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-yl)-5-oxopentanoic acids;

methyl ester 5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-yl)-5-oxopentanoic acids;

(3R*)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-yl)-3-hydroxy-5-oxopentanoic acid and (3S*)-5-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropylamino the yl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-yl)-3-hydroxy-5-oxopentanoic acid;

5-({1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-yl)-2,2-dimethyl-5-oxopentanoic acid;

4-((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-yl)-4-oxomalonate acid;

9-dimethylamide-6-[(2-Chlorobenzyl)cyclopropylamino](1R*,5S*)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6,9-dicarboxylic acid;

methyl ester of (1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid;

ethyl ester of (1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carboxylic acid;

ethyl ester of 3-[(1R*,5S*)-(6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)amino]propionic acid;

ethyl ester of 4-[((1R*,5S*-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)amino]butyric acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-formyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

3-[((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-thrift is Hinoki)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-EN-3-carbonyl)amino]propionic acid;

3-[((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)amino]propionic acid;

4-[((1R*,5S*)-6-[(2-Chlorobenzyl)cyclopropanecarbonyl]-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-9-carbonyl)amino]butyric acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2,3,6-tryptophanate)ethyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-9-(4-carbamoylmethyl)-7-{4-[2-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-9-(3-carbamoylbiphenyl)-7-{4-[2-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-9-(2-hydroxyacyl)-7-{4-[2-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R,5S)-9-((3S)-3-hydroxybutyryl)-7-{4-[2-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-9-methanesulfonyl-7-{4-[2-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-9-econsultancy-7-{4-[2-(2,3,6-tryptophanate)propyl]FeNi is}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2-fluoro-5-methoxybenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(3-methoxybenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(3,4-dimethoxybenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2-chloro-3-trifloromethyl)cyclopropylamine(1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

benzo[1,3]dioxol-5-almatyconservprom (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2-chloro-6-terbisil)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2-bromobenzyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2,3-dimethylbenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(3,5-diferensial)amide of (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid is;

cyclopropyl(2,3-dichlorobenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(3-cryptomaterial)amide of (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl} -3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(3-methylbenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(3 chlorbenzyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl-(3,5-dimethoxybenzyl)amide of (1R*,5S*)-7-{4-[3-(2-bromo-5-pertenece)propyl]phenyl}-3-(4-carbamoylmethyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-(5-morpholine-4-yl-5-oxopentanoic)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-(2-tetrazol-1-ylacetic)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-(5-oxo-5-piperazine-1-ilistener)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R,5S)-3-((2S)-2-amino-3-hydroxypropionic)-7-{4-[3-(2,3,6-cryptorf is hydroxy)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid and (2-Chlorobenzyl)cyclopropylamine (1S,5R)-3-((2S)-2-amino-3-hydroxypropionic)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R,5S)-3-((2S)-2-aminopropionic)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid and (2-Chlorobenzyl)cyclopropylamine (1S,5R)-3-((2S)-2-aminopropionic)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2,3-dichlorobenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2,3-dimethylbenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2-chloro-3-trifloromethyl)cyclopropylamine(1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl} -3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2-bromobenzyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)ethylamide (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(6 chlorobenzo[1,3]dioxol-5-ylmethyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[non-6-ene-6-carboxylic acid;

cyclopropyl(3,5-dimethoxybenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(3-methoxybenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2,3-dichlorobenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-pertenece)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2-chloro-3-trifloromethyl)cyclopropylamine(1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-pertenece)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(3 chlorbenzyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(3-methylbenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2-fluoro-5-methoxybenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2,3-dichlorobenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[3-(2-chloro-3,6-divergence)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-to benovoy acid;

(2-chloro-3-trifloromethyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(3,4-dimethoxybenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(3-cryptomaterial)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2-chloro-3-trifloromethyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2,3-dichlorobenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2,3-dimethylbenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2,3-dimethylbenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2,4,5-trichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2,3-dimethylbenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2,3-dichlorobenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2-bromo-5-pertenece)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]n the n-6-ene-6-carboxylic acid;

(2-bromobenzyl)cyclopropylamine (1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-4,5-dimethylphenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2,3-dichlorobenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2,3-dichlorophenoxy)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

cyclopropyl(2,3-dimethylbenzyl)amide of (1R*,5S*)-3-acetyl-7-{4-[2-(2-chloro-5-pertenece)ethoxy]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1R,5S)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid;

(2 Chlorobenzyl)cyclopropylamine (1S,5R)-7-{4-[3-(2,3,6-tryptophanate)propyl]phenyl}-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxylic acid.

8. The connection according to one of claims 1 to 7, intended for use as drugs having activity of renin inhibitors.



 

Same patents:

FIELD: organic chemistry, medicine, oncology.

SUBSTANCE: invention relates to condensed heterocyclic succinamide compounds of the formula (I): , their pharmaceutically acceptable salts, solvates or isomers wherein G represents mono- or polycyclic aryl or heterocyclic group substituted possibly at one or more positions; L represents a bond, -(CR7R7')n (wherein n = 1; R7 and R7' represents independently hydrogen atom (H), alkyl or substituted alkyl) or -CH2-NH-; Z1 represents oxygen atom (O); Z2 represents O; A1 and A2 represent -CR7 or in common with R7 from group W is a heterocyclic ring wherein oxygen represents a heteroatom; Y represents -O-, -SO-, -N(V2)-, -CH2-N(V2)-, -CO-N-(alkyl)-, -CH2-S-, -CH2-SO2-; V2 represents hydrogen atom, alkyl, arylalkyl, -CO-alkyl, -CO-O-aryl, -CO-O-arylalkyl; W represents -CR7R7'-CR7R7'-, -CR7R7'-C=O, -NR9-, -CR7R7'-, -N=CR8-, -N=N, -NR9-NR9'-, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo- or substituted heterocyclo-group, aryl or substituted aryl wherein if W doesn't mean -NR9-CR7R7'-, -N=CR8-, -N=N, -NR9-NR9'- or heterocyclo- or substituted heterocyclo-group then Y must mean -O-, -CH2-S-, -SO-, -CH2-SO2-, -N-(V2)- or -CH2-N-(V2)-; Q1 and Q2 represent hydrogen atom (H). Also, invention describes a method for synthesis of intermediate compounds in synthesis of compounds of the formula (I), using the latter for preparing agents modeling function of the nuclear hormone receptors. Compounds of the formula (I) can be used in treatment of prostate cancer.

EFFECT: improved method of synthesis, valuable medicinal properties of compounds.

8 cl, 11 tbl, 463 ex

The invention relates to a method for production of new chemical compounds having pesticidal activity

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to a method for preparing derivatives of taxane, namely 13-(N-Boc-β-isobutylisoserinyl)-14-β-hydroxybaccatin III-1,14-carbonate of the formula (I): from 10-desacetylbaccatin III for nine stages. Invention provides the effective method for preparing valuable biologically active compound from the more available parent raw.

EFFECT: improved preparing method.

11 cl, 2 tbl, 8 ex

FIELD: organic chemistry, chemical technology, medicine, oncology, pharmacy.

SUBSTANCE: invention relates to new derivative of taxane of the formula (I):

that elicits strong antitumor effect. Also, invention relates to intermediates substances, a method for preparing compound of the formula (I), a method for preparing 1,14-β-hydroxy-1,14-carbonate-baccatin III-derivatives substituted with isoserine residue at position 3 and to pharmaceutical composition based on compounds of the formula (I). Invention provides preparing new derivative of taxane that elicits higher activity and reduced toxicity as compared with paclitaxel.

EFFECT: improved preparing method, enhanced and valuable medicinal properties of compound.

10 cl, 7 tbl, 6 ex

The invention relates to compositions for coatings, in particular for re-finishing cars, to a method of curing compositions for coatings

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The invention relates to a method for production of new chemical compounds having pesticidal activity

The invention relates to 7-examinerlawrence heterocyclic Amida - analogues of prostaglandins, which are receptor antagonists AND thromboxane a2(THA2or combined receptor antagonists AND thromboxane a2(thromboxane synthetase inhibitors, and are used, for example, in the treatment of thrombotic disease and/or vascular spasm: have a long duration of action

FIELD: chemistry.

SUBSTANCE: description is given of new diazabicyclic aryl derivatives, with general formula I: its enantiomers, or mixture of enantiomers, or its adjoining pharmaceutical salt, where X and Y independently represent CR2, CR3 or N, where R2 is hydrogen, C1-6alkyl or halogen; and R3 is hydrogen or halogen; and R1 is hydrogen or halogen, CF3, NO2 or phenyl, possibly substituted, group with formula phenyl-Z-(C1-6alkyl)m-, phenyl -C≡C- or pyridyl -Z-(C1-6alkyl)m-, where m equals 0 or 1; Z - O or S, where phenyl and pyridyl are possibly substituted, or R1 and R3 , together with carbon atoms to which they are bonded, form a benzocondensed aromatic carbocyclic ring, which can be substituted. The new compounds are cholinergic ligands of nicotinic acetylcholine receptors.

EFFECT: compounds can be useful for treating such diseases or disorders related to the cholinergic system of the central nervous system, peripheral nervous system etc.

11 cl, 3 ex, 1 tbl

FIELD: organic chemistry.

SUBSTANCE: invention relates to novel individual compounds of series 2,5a-methano[1,4]diazepino[1,7-a]-quinoxaline-5-carboxylates, namely, to isopropyl-12-aroyl-2-hydroxy-1,6-dioxo-4-(3-pyridinyl)-7-phenyl-1,3,6,7-tetrahydro-2,5a-methano[1,4]diazepino[1,7-a]-quinoxaline-5-carboxylates of the formula (1) wherein Ar means phenyl or p-methoxyphenyl, and to a method for their synthesis. Method for synthesis of compound of the formula (1) involves interaction of 3-aroyl-5-phenylpyrrolo[1,2-a]-quinoxaline-1,2,4(5H)-triones with isopropyl-3-amino-3-(3-pyridinyl)-2-propenoate in an inert aprotonic solvent medium and the following isolation of end substances. The proposed method provides synthesis of novel compounds of the formula (1) possessing antibacterial effect with high yield and selectivity.

EFFECT: improved method of synthesis.

4 cl, 1 tbl, 3 ex

FIELD: organic chemistry, chemical technology, medicine.

SUBSTANCE: invention relates to new biarylcarboxamides of the general formula (I): wherein A means compound of the formula (II): ; D means oxygen atom (O) or sulfur atom (S); E means a simple bond, oxygen atom, sulfur atom or NH; Ar1 means 5-membered heteroaromatic ring comprising one nitrogen atom (N) and one sulfur atom (S) or one oxygen atom (O), or one S atom, or one N atom; or 6-membered aromatic ring, or heteroaromatic ring comprising one N atom; Ar2 means 5-membered heteroaromatic ring comprising one S atom or on O atom, or one N atom and one O atom, or one N atom; or 6-membered aromatic ring or heteroaromatic ring comprising one N atom; or 9-membered condensed heteroaromatic ring system comprising one O atom, or 10-membered condensed aromatic ring system, or heteroaromatic ring system comprising one N atom wherein aromatic ring Ar2 is possibly substituted with one or two substitutes taken among halogen atom, (C1-C4)-alkyl, cyano-group (-CN), nitro group (-NO2), NR1R2, OR3, trihalogen-(C1-C4)-alkyl, (C1-C4)-acylamino-, hydroxy-, morpholino-, amino-, methylamino-group, amino-(C1-C4)-alkyl and hydroxymethyl but if Ar1-phenyl and Ar2 represent quinolinyl group then Ar2 is substituted with one or two (C1-C4)-alkyls, -CN, -NO2, NR1R2, OR3 wherein R1, R2 and R3 mean (C1-C4)-alkyl and compound of the formula (III) doesn't represent .

EFFECT: improved preparing and treatment methods.

33 cl, 69 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to new individual compounds of azapentacycloeicosanes class. Invention describes 20-aroyl-12-hydroxy-17,17-dimethyl-3-phenyl3,10,13-triazapentacyclo[10.7.1.01,10.O4,9.O14,19]eicosa-4,6,14(19)-2,11,15-triones of the formula:

wherein R means hydrogen atom; Ar means phenyl; or R means benzyl and Ar means p-methoxyphenyl group. Also, the invention describes a method for preparing these compounds. Invention provides preparing new compounds that can be used as the parent substances for synthesis of new heterocyclic systems.

EFFECT: improved preparing method, valuable chemical properties of compounds.

4 cl, 1 tbl, 3 ex

The invention relates to a single-stage process for the preparation of new chemical compounds - cyclocarbonate

The invention relates to organic chemistry, specifically to a method for producing cyclic nitramines

The invention relates to new compounds which can be used as inhibitors of matrix metalloprotease, in particular interstitial collagenases, and which is effective for the treatment of painful condition caused by excessive activity of matrix metalloprotease
The invention relates to the selection of triethylenediamine, which is used as a catalyst in obtaining polyurethane foam and which is a hardener of epoxy resins and vulcanizer polyester oils

FIELD: chemistry.

SUBSTANCE: description is given of new diazabicyclic aryl derivatives, with general formula I: its enantiomers, or mixture of enantiomers, or its adjoining pharmaceutical salt, where X and Y independently represent CR2, CR3 or N, where R2 is hydrogen, C1-6alkyl or halogen; and R3 is hydrogen or halogen; and R1 is hydrogen or halogen, CF3, NO2 or phenyl, possibly substituted, group with formula phenyl-Z-(C1-6alkyl)m-, phenyl -C≡C- or pyridyl -Z-(C1-6alkyl)m-, where m equals 0 or 1; Z - O or S, where phenyl and pyridyl are possibly substituted, or R1 and R3 , together with carbon atoms to which they are bonded, form a benzocondensed aromatic carbocyclic ring, which can be substituted. The new compounds are cholinergic ligands of nicotinic acetylcholine receptors.

EFFECT: compounds can be useful for treating such diseases or disorders related to the cholinergic system of the central nervous system, peripheral nervous system etc.

11 cl, 3 ex, 1 tbl

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