http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-086218-A1
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| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c16ddedf8b57a5d40033debc21ed5781 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_448df27628b9edec7a065b956ae02263 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5513 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-147 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 |
| filingDate | 2012-04-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1a1a993974b230a6f290ae2462f2e142 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_78a271d4c05621d78cac378af0239aa3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_540300f9803fba14b105d3f4683aee99 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1cd3dffb423aee88e13f11c676d6a2bd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0ada47581fc944d6c09559ca3063df8c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fa9fedf56b65f2ad2d4ba7c8de3fa582 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_604146b6a475d6ea51d3f62d5ee24708 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3045a3bc0dde752b522befe99fec12d2 |
| publicationDate | 2013-11-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-086218-A1 |
| titleOfInvention | TRICYCLE AND TETRACICLIC SYSTEMS WITH ACTIVITY ON THE CENTRAL AND VASCULAR NERVOUS SYSTEM |
| abstract | These molecular entities have GABAergic and modulating action of calcium channels, usable in the treatment of cardiovascular, cerebrovascular, neurodegenerative, neuropsychiatric and neurological diseases.Claim 1: Tricyclic and tetracyclic systems with activity on the central and vascular nervous system derived from diazepines with a 1,4-dihydropyridine ring fused to its structure, for use as drugs in medicine, of general formula (1) to (12) in its racemic modification and as each levogyric and dextrogyre enantiomer separately, where for compounds of general formula (1) to (12), R represents H, alkyl group (preferably alkyl groups of up to 8 straight or branched chain carbon atoms, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl and octyl, and the chain isomers of all of the above; as well as cyclic alkyl, and substituted alkyl, preferably substituted with halogen enos, vinyl and substituted vinyl; and cyclic alkyl chains, preferably the cyclohexyl group; R represents an aryl group (benzyl, naphthyl and substituted naphthyl or anthracil), the aryl and substituted aryl group, preferably represent unsubstituted phenyl or substituted by one and up to five substituents independently selected from -NO2, -NH2, -OH, F, Cl, Br, I, -CN, -OCH3, -N (CH3) 2, -CH3 -OCOCH3, -COOCH3, -OCF3, -SH, -NH (C = O) -CH3, -CHO, -C = NH , - C = NH-NH2, -C = NH-OH; R represents heteroaryl, substituted heteroaryl, where heteroaryl and substituted heteroaryl preferably refers to furfuryl, substituted furfuryl, pyrrolidyl, substituted pyrrolidyl, thiophenyl, substituted thiophenyl, pyridyl (2-pyridyl, 3-pyridyl and 4-pyridyl), substituted pyridyl, quinolinyl (2-quinolinyl, 3-quinolinyl, 4-quinolinyl), pyrazolyl; R represents a heteroaryl group, preferably pyrrole, thiophene and substituted phenyl furan, where the phenyl group may be substituted in turn with one or more substituents chosen from -CN, -C (C = O) -CH3, F, Cl, Br , NH2, NO2; for the compounds of the general formula (1), (2) and (3), R 1 represents H, alkyl group, straight or branched chain and alicyclic, preferably with a number of carbon atoms between 1 and 16; for the compounds of general formula (1), (2) and (3), R1 also represents OR 'where R' independently represents H, or its salts of Sodium (Na) and Potassium (K); alkyl groups of 1 and up to 24 carbon atoms, of straight or branched chains such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, sec-pentyl, tert-pentyl, neopentyl , hexyl, isohexyl, sec-hexyl, tert-hexyl, heptyl, octyl, nonyl, decyl, undecyl, dodecyl, and all positional, straight or branched chain isomers of all of the foregoing; - (CH2) n-O- (CH2) n-CH3; - (CH2) n-O- (CH2) n-O- (CH2) n-CH3 where n is equal to 1 and less than 8, - (CH2) n-CN, where n is a number between 1 and 8; R ’also represents lipid chains derived from mono and polyunsaturated fatty acids of up to 24 carbon atoms; R1 also represents -NHR ’, where R’ ’independently represents linear or branched alkyl groups of carbon chains of between 1 and up to 24 carbon atoms; - (CH2) n-O- (CH2) n-CH3; - (CH2) n-O- (CH2) n-O- (CH2) n-CH3 where n is a number between 1 and 8, - (CH2) n-CN, where n = 1-8; R 'also represents lipid chains derived from mono and polyunsaturated fatty acids of up to 24 carbon atoms; R1 also represents -NHR '' ', where R' '' independently represents - (CH2) n-NH2 where n is a number between 1 and 10, example and preferably -NH- (CH2) 6-NH2, -NH- ( CH2) 8-NH2; R1 also represents chains of the type -NH- (CH2) n-NH (C = O) -R3, where n is a number between 1 and 10 and R3 represents linear or branched alkyl groups, unsaturated alkyl moieties, of the type - (CH2 ) nC = C- (CH2) n-CH3, preferably of chain lengths of up to 18 carbon atoms, for example and preferably -NH- (CH2) 6-NH (C = O) -C11H23, -NH- (CH2 ) 6-NH (C = O) -C7H14-CH = CH-C8H17; for the compounds of general formula (1), (2) and (3), R1 also represents amino acid residues of the type -NH-CH (R4) -COOH, where R4 is the amino acid residues, preferably valine, phenylalanine, alanine, histidine, usine, tryptophan, cysteine, leucine, tyrosine, isoleucine, proline and methionine; R1 also represents small peptide chains of between 2 and up to 12 amino acids, obtained by combinations of some of them chosen independently; R1 also represents -NH-OH; -NH-NH2 -NH-NH- (C = O) -NH2; -NH-NH- (CS) -NH2; R1 also represents -NHR5, where R5 is a thiazole and substituted thiazole ring, 4-phenylthiazole or substituted 4-phenylthiazole; R5 also represents a phenyl and substituted phenyl substituent; for the compounds of the general formula (1), (2) and (3), R2 represents an alkyl or cycloalkyl group; alkyl groups can be straight or branched chain between 1 and up to 16 carbon atoms; groups - (CH2) n-NH2 and groups - (CH2) n-OH, where n is 1 and up to 8; for the compounds of general formula (1) to (12), cycle A is a 6-membered aromatic ring fused to the diazepine ring and represents a benzene or substituted benzene ring, forming a benzodiazepine, fused in such a way that implies a structure and all its position isomers and all possible tautomers; benzene fused to diazepine, represented as ring A, is in turn substituted by one and up to four substituents independently selected from OH, COOH, CH3, NO2, NH2, CHO (formyl group), halogens and combinations thereof; the benzene group fused to diazepine, represented by A, may also be substituted with carboxylic acid derivatives -C (C = O) -R6, where R6 represents O-alkyl, -O-aryl, NH2, -NH-alkyl, -NH-aryl; the benzene group fused to diazepine, represented by A, may also be substituted by a group -NH-C (C = O, S) -N (R7) 2, where R7 is an H, or small linear or branched alkyl group from 1 to 6 carbon atoms; the benzene group fused to diazepine, represented by A, may also be substituted by a group -NH- (C = O, S) -OR7, where R7 is an H, or small linear or branched alkyl group of 1 and up to 8 carbon atoms; for the compounds of general formula (1) to (12), cycle A is also a 6-membered heterocyclic ring fused to the diazepine ring and represents a substituted pyridine and pyridine ring, preferably with halogens, the pyridine ring may be fused to diazepine in such a way that it implies a structure and all its possible positional isomers and all possible tautomers; for the compounds of general formula (1) to (12), cycle A is also a 6-membered heterocyclic ring fused to the diazepine ring and represents an unsubstituted pyrimidine ring and substituted pyrimidine, where one or both of the nitrogen atoms of pyrimidine may be substituted by H, CH3, OH, SH and NH2 and their combinations independently selected; the carbon atoms of the pyrimidine may be independently substituted by one or more substituents selected from H or CH3; also OH, SH, NH2, -C = O, -C = S, -C = NH so that it implies a structure and all tautomeric forms and positional isomers and all tautomeric forms derived therefrom; for the compounds of general formula (1) to (12), when cycle A is a substituted pyrimidine ring, said pyrimidine ring may also be substituted at the positions corresponding to the carbons of the cycle, by a substituent R8, where R8 represents an alkyl group of 1 and 6 straight or branched chain carbon atoms, and preferably by a phenyl group unsubstituted or substituted by one and up to five substituents independently selected from -NO2, -NH2, -OH, F, Cl, Br , I, -CN - OCH3, -N (CH3) 2, -CH3, -OCOCH3, -COOCH3, -OCF3, -SH, -NH (C = O) -CH3, -CHO, -C = NH, -C = NH-NH2, -C = NH-OH in such a way that it implies a structure and all its possible positional isomers and all the tautomeric forms derived from them. |
| priorityDate | 2012-04-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 111.