http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-033642-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_880cc8535f892eca8121f608c316808c |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-021 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-06139 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-02 |
| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4427 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K5-078 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K5-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-454 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4035 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-403 |
| filingDate | 1999-12-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6e575660eb5b3557a3aac8c22c6b29e2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d6ea8f4e3641a1694749dddb000c18d1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c172fcb8311ba5a1ab8e54b7735dd0c5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e5fb6aefad9cb9db14a19d5c194946ae |
| publicationDate | 2004-01-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-033642-A1 |
| titleOfInvention | 3- (SUBSTITUTED THIO-AMIDO) USEFUL LACTAMAS AS INHIBITORS OF METALOPROTEINASES OF THE MATRIX, PHARMACEUTICAL COMPOSITION AND USES IN THE MANUFACTURE OF PHARMACEUTICAL COMPOSITIONS TO TREAT DISEASES |
| abstract | 3- (Substituted thio-amido) lactams of formula (1), useful as inhibitors of matrix metalloproteinases (MMP), wherein: q is 1 or 2; A is selected from the group consisting of -OH and -NRR '; where R and R 'are independently selected from the group consisting of hydrogen and C1-6 alkyl, or R and R', taken together with the nitrogen atom to which they are attached, form an N-morpholino, N-piperidino, N- pyrrolidino or N-isoindolyl; R1 is selected from the group consisting of hydrogen, C1-6 alkyl, - (CH2) a-CO2R5, - (CH2) aC (O) NH2, - (CH2) 4-NH2, - (CH2) 3-NH-C (NH) NH2, - (CH2) 2-S (O) b-CH3, -CH2-OH, -CH- (OH) CH3, - (CH2) d-Ar1 and -CH2-Ar2; where a is 1 or 2; b is 0, 1 or 2; d is an integer from 0 to 4; R5 is selected from the group consisting of hydrogen, C1-4 alkyl and benzyl; Ar1 is a radical selected from the group consisting of the moieties of formulas (2) and (3), where R6 is 1 to 2 substituents selected from the group consisting of hydrogen, halogen, C1-4 alkyl, hydroxy and C1- alkoxy 4; R7 is selected from the group consisting of hydrogen, halogen, C1-4 alkyl and C1-4 alkoxy; Ar2 is a radical selected from the group consisting of the moieties of formulas (4) and (5); R2 is a radical selected from the group consisting of C1-6 alkyl, - (CH2) g-Ar1 'and - (CH2) -Ar2'; where g is an integer from 1 to 4; Ar1 'is a radical selected from the group consisting of the moieties of formulas (6) and (7), where R6' is 1 to 2 substituents independently selected from the group consisting of hydrogen, halogen, C1-4 alkyl, hydroxy and C1-4 alkoxy; R7 'is selected from the group consisting of hydrogen, halogen, C1-4 alkyl and C1-4 alkoxy; Ar2 'is a radical independently selected from the group consisting of the moieties of formulas (4) and (5); R3 is selected from the group consisting of C1-6 alkyl, - (CH2) mW, - (CH2) p-Ar3, - (CH2) k-CO2R9, - (CH2) m-NR8'SO2-Y1 and - (CH2 ) mZQ, where m is an integer from 2 to 8; p is an integer from 0 to 10; k is an integer from 1 to 9; W is phthalimido; Ar3 is selected from the group consisting of the moieties of formulas (8) through (13), where R23 is 1 to 2 substituents independently selected from the group consisting of hydrogen, halogen, C1-4 alkyl and C1-4 alkoxy; R8 'is hydrogen or C1-6 alkyl; R9 is hydrogen or C1-6 alkyl; Y1 is selected from the group consisting of hydrogen, - (CH2) j-Ar4 and -N (R24) 2, where j is 0 or 1; R24 each time selected is independently hydrogen or C1-6 alkyl or are taken together with the nitrogen to which they are attached to form N-morpholino, N-piperidino, N-pyrrolidino or N-isoindolyl; Ar4 is a moiety of formula (14), wherein R25 is 1 to 3 substituents independently selected from the group consisting of hydrogen, halogen, C1-4 alkyl and C1-4 alkoxy; Z is selected from the group consisting of -O-, -NR8-, -C (O) NR8-, -NR8C (O) -, -NR8C (O) -NH-, -NR8C (O) O- and OC ( O) NH-, where R8 is hydrogen or C1-6 alkyl; Q is selected from the group consisting of hydrogen, - (CH2) n-Y2 and - (CH2) x-Y3, where n is an integer from 0 to 4; Y2 is selected from the group consisting of hydrogen, - (CH2) h-Ar5 and - (CH2) t-C (O) OR27; where Ar5 is selected from the group consisting of the moieties of formulas (9) and (15), where R26 is 1 to 3 substituents independently selected from the group consisting of hydrogen, halogen, C1-4 alkyl and C1-4 alkoxy; h is an integer from 0 to 6; t is an integer from 1 to 6; R27 is hydrogen or C1-6 alkyl; x is an integer from 2 to 4; Y3 is selected from the group consisting of -N (R28) 2, N-morpholino, N-piperidino, N-pyrrolidino and N-isoindolyl; where R28 each time taken is independently selected from the group consisting of hydrogen or C1-6 alkyl; R4 is selected from the group consisting of hydrogen, -C (O) R10, -C (O) - (CH2) qX and -SG, where R10 is selected from the group consisting of hydrogen, C1-4 alkyl, phenyl and benzyl ; q is 0, 1 or 2; X is selected from the group consisting of the residues of formulas (13), (16), (17), (18) and (19); where V is selected from the group consisting of a bond, -CH2-, -O-, -S (O) r-, -NR21- and -NC (O) R22-; where r is 0, 1 or 2; R21 is selected from the group consisting of hydrogen, C1-4 alkyl and benzyl; R22 is selected from the group consisting of hydrogen, -CF3, C1-10 alkyl, phenyl and benzyl; R11 is selected from the group consisting of hydrogen, C1-4 alkyl or benzyl; G is selected from the group consisting of formulas (20) to (26), where w is an integer from 1 to 3; R12 is selected from the group consisting of hydrogen, C1-6 alkyl, -CH2CH2-S (O) uCH3 and benzyl; u is 0, 1 or 2; R13 is selected from the group consisting of hydrogen, hydroxy, amino, C1-6 alkyl, N-methylamino, N, N-dimethylamino, .CO2R17 and -OC- (O) R18; where R17 is hydrogen, -CH2O-C (O) C (CH3) 3, C1-4 alkyl, benzyl or diphenylmethyl; R18 is hydrogen, C1-6 alkyl or phenyl; R14 is 1 or 2 substituents independently selected from the group consisting of hydrogen, C1-4 alkyl, C1-4 alkoxy or halogen; V1 is selected from the group consisting of -O-, -S- and -NH-; V2 is selected from the group consisting of -N- and -CH-; V3 is selected from the group consisting of a link and -C (O) -; V4 is selected from the group consisting of -O-, -S-, -NR19- and -NC (O) R20-; where R19 is hydrogen, C1-4 alkyl or benzyl; R20 is hydrogen, -CF3, C1-10 alkyl or benzyl; R15 is selected from the group consisting of hydrogen, C1-6 alkyl and benzyl; and R16 is selected from the group consisting of hydrogen and C1-4 alkyl; and its stereoisomers, pharmaceutically acceptable salts and hydrates. Pharmaceutical composition, as well as uses for the manufacture of pharmaceutical compositions to treat diseases that respond to the inhibition of matrix metalloproteinase. |
| priorityDate | 1998-12-31-04:00^^<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: 57.