http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-050430-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_12a9e9ce63eb0bbf3658453fb50a6d9b |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-06139 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-06191 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 |
| filingDate | 2005-07-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9b417eae408f5893bc46537002953cdd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d36438eea74fd177a34e8914e7482c05 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cddc586cb7adb439b67a5421cdfb1893 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3e10c9f8ec37b8cf86800d4f6eba3880 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1cb585f065120375e0160e686e451052 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_61c9c5d71fbb04ec481c06c85eac8191 |
| publicationDate | 2006-10-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-050430-A1 |
| titleOfInvention | ANALOGS OF INHIBITING DIPEPTIDES OF HEPATITIS C |
| abstract | Claim 1: A compound of formula (1), wherein: n is 1 or 2; m is 1 or 2; R1 is C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl; wherein C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are optionally substituted in one to more replaceable positions with one to three halogen atoms; R2 is selected from -NH-R20, -O-R20, -S-R20, -SO-R20, -SO2-R20, -OCH2-R20, and -CH2O-R20, in which: R29 is aryl or Het, wherein aryl and Het are optionally substituted with R200, wherein R200 is one to four substituents each independently selected from H, halogen, cyano, C1-6 alkyl, C3-7 cycloalkyl, arylC1-6 alkyl- , aryl, Het, oxo, thioxo, -OR201, -SR201, -SOR201, -SO2R201, and -N (R202) R201, and - CON (R202) R201; wherein each of the alkyl, cycloalkyl, aryl and Het is further optionally substituted with R2000; R201 in each case is independently selected from H, C1-6 alkyl, aryl, C2-4 alkenyl, C2-4 alkynyl, -CO-C1-6 alkyl and -CO-O-C1-6 alkyl; wherein each of the alkyl and aryl is further optionally substituted with R2000; R202 is H or C1-6 alkyl; R2000 is one to three substituents each independently selected from halogen, R2003, aryl, Het, - OR2001, -SR2001, -SOR2001, -SO2R2001, cyano and -N (R2002) (R2001), in which aryl and Het each is optionally substituted with one, two or three substituents, each independently selected from C1-6 alkyl and -O-C1-6 alkyl; R2001 in each case is independently selected from aryl, arylC1-6- alkyl, -C (O) -R2003, -C (O) O-R2003, -CON (R2002) (R2004) and R2004; R2002 in each case is independently selected from H and C1-6 alkyl; R2003 in each case is independently selected from C 1-8 alkyl, C 3-7 cycloalkyl and C 3-7 cycloalkyl-C 1-4 alkyl, wherein C 3-7 cycloalkyl and C 3-7 cycloalkyl-C 1-4 alkyl are each optionally substituted. with one to three substituents, each independently selected from C1-3 alkyl; and R2004 in each case is independently selected from H and R2003; R3 is selected from: i) -C (O) OR31 in which R31 is C1-6 alkyl or aryl, wherein C1-6 alkyl is optionally substituted with one to three halogen substituents; ii) -C (O) NR32R33, wherein R32 and R33 are each independently selected from H, C1-6 alkyl, and Het; iii) -SovR34 in which v is 1 or 2 and R34 is selected from: C1-6 alkyl, aryl, Het, and NR32R33 in which R32 and R33 are as defined above; and iv) -C (O) -R35, wherein R35 is selected from C 1-8 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyl-C 1-4 alkyl, aryl, aryl C 1-6 alkyl, Het and Het- C1-6 alkyl, each of which is optionally substituted with one or more substituents, each independently selected from halogen, C1-6 alkyl, C3-7 cycloalkyl, aryl, Het, hydroxyl, -O-C1-6 alkyl, -S -C1-6 alkyl, -SO-C1-6 alkyl, -SO2-C1-6 alkyl, -O-aryl, -S-aryl, -SO-aryl and -SO2-aryl, in which the aryl part of -O- aryl, -S-aryl, -SO-aryl and -SO2-aryl are each optionally substituted with one or five halogen substituents; R 4 is C 1-6 alkyl, C 2-6 alkenyl, C 3-7 cycloalkyl, C 3-7 cycloalkyl-C 1-6 alkyl, aryl, Het, aryl C 1-4 alkyl, or Het C 1-4 alkyl; a) with C1-6 alkyl, C2-6 alkenyl, aryl, Het, C3-7 cycloalkyl- C1-6 alkyl, arylC1-4 alkyl-, and Het-C1-4 alkyl optionally substituted with one, two or three substituents , each independently selected from halogen, nitro, hydroxy, cyano, C1-6 alkyl, O-C1-6 alkyl, -O-aryl, -CO-NH2, -CO-NH-C1-4 alkyl, -CO-N (C1-alkyl -4) 2, -NH2, -NH-C1-4alkyl and -N (C1-4alkyl) 2, wherein C1-6alkyl and O-C1-6alkyl are optionally substituted with one to three halogen atoms; and b) the C3-7 cycloalkyl being optionally substituted with one or more substituents, each independently selected from nitro, halogen, hydroxy, cyano, -O-C1-6 alkyl, C2-4 alkenyl, -OCF3, -NH2, -NH- C 1-4 alkyl, -N (C 1-4 alkyl) 2, tri-C 1-6 alkyl silyl, R41, -C (= O) -R41, -C (= O) OR41, -C (= O) N (R42) R41, -SO2R41, and -OC (= O) -R41; in which R41 in each case is independently selected from: i) H, C3-7 cycloalkyl, C4-7 cycloalkenyl, Het or arylC1-4-O- alkyl; ii) aryl or aryloxy, each of which is optionally substituted with C1-6 alkyl; and iii) C1-8 alkyl optionally substituted with one or more substituents, each independently selected from -O- C1-6 alkyl, hydroxy, halogen, C2-10 alkenyl, C2-10 alkynyl, C3-7 cycloalkyl, C4-7 cycloalkenyl , aryl, Het, aryloxy, and arylC 1-4 alkyl-O-, wherein each of the aryl and aryloxy is optionally substituted with C 1-6 alkyl; and R42 is selected from H and C1-6 alkyl; or R4 is -N (RN2) (RN1), in which RN1 and RN2 are each independently selected from H, C1-6 alkyl, -O-C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl -, aryl and arylC 1-6 alkyl; wherein C1-6 alkyl, -O-C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl- C1-6- alkyl, aryl and arylC1-6 alkyl- are each optionally substituted with one or more substituents each independently selected from halogen, C1-6 alkyl, hydroxy, cyano, O- C1-6 alkyl, -NH2, -NH-C1-4 alkyl, -N (C1-4 alkyl) 2, -CO-NH2, -CO-NH-C1 alkyl -4, -CO-N (C1-4alkyl) 2, -COOH, and -COO-C1-6alkyl; or RN2 and RN1 are linked, together with the nitrogen to which they are attached, to form a monocyclic, saturated or unsaturated heterocycle of 3 to 7 members, optionally condensed with at least one other cycle to form a heterocycle and the heterocycle and heterocycle containing each one optionally one to three additional heteroatoms, each independently selected from N, S and O, and are optionally substituted with one or more substituents, each independently selected from halogen, C1-6 alkyl, hydroxy, cyano, O-C1-alkyl 6, -NH2, -NH-C1-4alkyl, -N (C1-4alkyl) 2, -CO-NH2, -CO- NH-C1-4alkyl, -CO-N (C1-4alkyl) 2, -COOH, and -COO-C 1-6 alkyl; in which Het as used herein is defined as a 3 to 7 membered heterocycle having 1 to 4 heteroatoms each independently selected from O, N and S, which can be saturated, unsaturated or aromatic, and which it is optionally condensed with at least one other cycle to form a 4 to 14 membered heteropolyclo, which has 1 to 5 heteroatoms where possible, each independently selected from O, N and S, the saturated, unsaturated or aromatic heteropolyclo being; with the proviso that: when n is 1; and m is 2; R1 is ethyl or ethenyl; and R2 is -O-R20, in which R20 is Het, in which Het is selected from a group of formulas (2); and wherein the Het is optionally substituted with R200, wherein R200 is one or two substituents each independently selected from methyl, methoxy, chloro, fluorine, hydroxy, phenyl, 4-methoxyphenyl, 4- (dimethylamino) phenyl, 4 - cyanophenyl, and a group selected from formulas (3); and R4 is cyclopropyl optionally substituted with propyl, cyclopropylmethyl or phenylmethyl; and R3 is -COOR31; then R31 is not 1,1-dimethylethyl; or a racemate, diastereoisomer, or its optical isomer, including one of its salts. |
| priorityDate | 2004-07-20-04:00^^<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: 45.