http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EA-000991-B1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_36089addd8e49e968b4c7e13c517dd1c |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D241-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D333-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-425 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D307-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D277-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4427 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D307-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-426 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-425 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-505 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-495 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D333-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D241-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-381 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-341 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-44 |
| filingDate | 1996-12-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0997d398c0b7c6ddc54d33e935ce2f75 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ce973498017ab49b2803801258147aa2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cb7db50e02d72bec0575458c08f5d610 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d361383c0cfb3f7d0753d17dc2626765 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d36a01cb8b16e0b902401f9b188fffdc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_10215783ebf8613011ddf05db8cdaa0b |
| publicationDate | 2000-08-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EA-000991-B1 |
| titleOfInvention | THIOL DERIVATIVES, possessing inhibitory activity against metallopeptidases |
| abstract | 1. A compound of formula wherein R is a mercapto group or a R4COS group convertible in the organism to mercapto group; R1 is a straight or branched chain C2-C4 alkyl group or an aryl or arylalkyl group having from 1 to 6 carbon atoms in the alkyl moiety, wherein the aryl is a phenyl or a 5 or 6 membered aromatic heterocycle with one or two heteroatoms, selected from the group, consising of nitrogen, oxygen and sulphur, optionally substituted with one or more substituents, the same or different, selected from the group consisting of halogen atoms, hydroxy groups, alkoxy, alkyl, alkylthio, alkylsulphonyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C1-C3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylainino groups, aminosulphonyl groups, mono- or dialkylamino or mono- or dialkylaminocarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R2 is a hydrogen atom, a straight or branched chain C1-C4alkyl or a benzyl group; R3 is a phenyl group substituted by a 5 or 6 membered aromatic heterocycle with one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulphur, moreover the phenyl and the heterocyclic groups optionally substituted with one or more substituents, the same or different, as indicated for R1; R4 is a straight or branched chain C1-C4alkyl group or a phenyl group; the carbon atoms marked with an asterisk are stereogenic centers; and pharmaceutically acceptable salts thereof. 2. A compound of formula I according to claim 1, wherein R3 is a phenyl group substituted in position 4 with a heterocyclic group. 3. A compound of formula I according to claim 2, wherein R1 represents an arylalkyl group optionally substituted with one or more substituents, the same or different, selected from the group, consisting of halogen atoms, hydroxy, alkyl or alkoxy groups. 4. A compound of formula I according to claim 3, wherein R1 represents a phenylalkyl group optionally substituted with one or more substituents, the same or different, selected from the group, consisting of halogen atoms, hydroxy, alkyl or alkoxy groups. 5. A compound of formula I according to claim 1 in the form of a salt of an alkali metal, selected from the group, consisting of sodium, lithium and potassium. 6. A process for the preparation of a compound of formula I according to claim 1, comprising the reaction between a compound of formula wherein R and R1 have the above reported meanings; and a phenylalanine derivative of formula wherein R2 and R3 have the above reported meanings. 7. A pharmaceutical composition, containing a therapeutically effective amount of a compound of formula I according to claim 1 in admixture with a carrier, acceptable for pharmaceutical use. 8. A pharmaceutical composition according to claim 7 for the treatment of cardiovascular diseases. 9. A method for the treatment of cardiovascular diseases comprising the administration of a therapeutically effective amount of a compound of formula I according to claim 1. 10. A compound, selected from the group consisting of: N-(3-phenylcarbonylthio-2-phenylmethylpropionyl)-4-(2-thiazolyl)-L-phenylalanine methyl ester; N-(3-phenylcarbonylthio-2-phenylmethylpropionyl)-4-(2-pyridyl)-L-phenylalanine methyl ester; N-(3-phenylcarbonylthio-2-phenylmethylpropionyl)-4-(3-pyridyl)-L-phenylalanine benzyl ester; N-(3-phenylcarbonylthio-2-phenylmethylpropionyl)-4-(2-furyl)-L-phenylalanine methyl ester; N-(3-phenylcarbonylthio-2-phenylmethylpropionyl)-4-(5-pyrimidinyl)-L-phenylalanine ethyl ester; N-(3-phenylcarbonylthio-2-phenylmethylpropionyl)-4-(2-pyrazinyl)-L-phenylalanine methyl ester; N-(3-phenylcarbonylthio-2-phenylmethylpropionyl)-4-(2-thienyl)-L-phenylalanine methyl ester; N-(3-phenylcarbonylthio-2-phenylmethylpropionyl)-4-(3-thienyl)-L-phenylalanine methyl ester; N-(3-phenylcarbonylthio-2-phenylmethylpropionyl)-4-(3-furyl)-L-phenylalanine methyl ester; N-[3-phenylcarbonylthio-2-(3-pyridylmethyl)propionyl]-4-(2-thiazolyl)-L-phenylalanine methyl ester; N-(3-mercapto-2-phenylmethylpropionyl)-4-(2-thiazolyl)-L-phenylalanine; N-(3-mercapto-2-phenylmethylpropionyl)-4-(2-pyridyl)-L-phenylalanine; N-(3-mercapto-2-phenylmethylpropionyl)-4-(3-pyridyl)-L-phenylalanine; N-(3-mercapto-2-phenylmethylpropionyl)-4-(2-furyl)-L-phenylalanine; N-(3-mercapto-2-phenylmethylpropionyl)-4-(5-pyrimidinyl)-L-phenylalanine; N-(3-mercapto-2-phenylmethylpropionyl)-4-(2-pyrazinyl)-L-phenylalanine; N-(3-mercapto-2-phenylmethylpropionyl)-4-(2-thienyl)-L-phenylalanine; N-(3-mercapto-2-phenylmethylpropionyl)-4-(3-thienyl)-L-phenylalanine; N-(3-mercapto-2-phenylmethylpropionyl)-4-(3-furyl)-L-phenylalanine; N-[3-mercapto-2-(3-pyridylmethyl)propionyl]-4-(2-thiazolyl)-L-phenylalanine; N-[3-acetylthio-2-(3-methoxyphenyl)methylpropionyl]-4-(2-thiazolyl)-L-phenylalanine methyl ester; N-[3-acetylthio-2-(2-fluorophenyl)methylpropionyl]-4-(2-thiazolyl)-L-phenylalanine methyl ester; N-[3-phenylcarbonylthio-2-(2-thienyl)methylpropionyl]-4-(2-thiazolyl)-L-phenylalanine methyl ester; N-[2-(2-furyl)methyl-3-phenylcarbonylthiopropionyl]-4-(2-thiazolyl)-L-phenylalanine methyl ester; N-[2-(3-methyl-5-isoxazolyl)methyl-3-phenylcarbonylthiopropionyl]-4-(2-thiazolyl)-L- phenylalanine methyl ester; N-[3-mercapto-2-(3-methoxyphenyl)methylpropionyl]-4-(2-thiazolyl)-L-phenylalanine; N-[3-mercapto-2-(3-thienyl)methylpropionyl]-4-(2-thiazolyl)-L-phenylalanine; N-[3-mercapto-2-(3-methyl-5-isoxazolyl)methylpropionyl]-4-(2-thiazolyl)-L-phenylalanine; N-[2-(2-fluorophenyl)methyl-3-mercaptopropionyl]-4-(2-thiazolyl)-L-phenylalanine; N-[2-(2-furyl)methyl-3-mercaptopropionyl]-4-(2-thiazolyl)-L-phenylalanine; and the stereoisomers (2S) or (2R) thereof. |
| priorityDate | 1995-12-28-04:00^^<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: 212.