http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-036081-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_07b71571160c289fbf5fc680dfea513f |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2601-02 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D233-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D265-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D215-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D249-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C229-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-06 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/C07D417-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D231-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D285-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F7-1804 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C311-46 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K39-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C229-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K45-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5415 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D285-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D265-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C311-46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K48-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D521-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D215-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7105 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7088 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C229-64 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F7-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-21 |
| filingDate | 2002-06-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2004-08-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-036081-A1 |
| titleOfInvention | COMPOSITE OF 1,2-DIHYDROQUINOLINE, ITS USE TO PREPARE A PHARMACEUTICAL COMPOSITION, METHODS TO PREPARE IT AND N-RENTED 2-AMINOBENZOIC ACID OF UTILITY AS INTERMEDIARY IN SUCH METHODS |
| abstract | RNA virus inhibitor compounds of formula (1) in which: R1 is hydrogen, halogen, C1-4 alkyl, -OR11, -SR11, -NR10R11, aryl, -C (O) OH, -C ( O) NHR11, cyano or nitro; R2 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-6 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, nitro, cyano, halogen, -C (O) OR9, -C (O) R9, -C (O) NR9R10, -OR9, -SR9, -S (O) R12, -S (O) 2R9, -NR9R10, -OH protected, -N (R10) C (O) R9, -OC (O) NR9R10, -N (R10) C (O) NR9R10, -P (O) (OR9) 2, -SO2NR9R10, or -N (R10) SO2R9, said C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl being said , unsubstituted or substituted with one or more substituents independently selected from halogen, -OH, -SH, -NH2, -O-C1-4 alkyl, -S-C1-4 alkyl, -NR10R11, cyano, nitro, -CO2R10, -C (O) O-C1-4 alkyl, -CONR10R11, -CONH2, aryl and heteroaryl, and said cycloalkyl, heterocycloalkyl, aryl or heteroaryl being unsubstituted or substituted with one or more substituents independently selected from C1-6 alkyl, haloalkyl C1-6, halogen, -OH, -SH, -NH2, -O-C1-4 alkyl, -S-C1-4 alkyl, -N (C1-4 alkyl) (C1-4 alkyl), -NH (alkyl C1-4), cyano, nitro, -CO2H, -C (O) O-C1-4 alkyl, -CON (al C 1-4 alkyl) (C 1-4 alkyl), -CONH (C 1-4 alkyl) and -CONH2; R3 is hydrogen, halogen, cyano, C1-6 alkyl, -OH or -CO2H; each of R4, R5 and R6 are independently selected from the group consisting of hydrogen, halogen, cyano, C1-6 alkyl, -OH and -O-C1-4 alkyl; R7 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-6 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, nitro, cyano, halogen, -C (O) OR9, -C (O) R9, -C (O) NR9R10, -OR9, -SR9, -S (O) R12, -S (O) 2R12, -NR9R10, -OH protected, -N (R12) C (O) R9, -OC (O) NR9R10, -N (R12) C (O) NR9R10, -P (O) (OR9) 2, -SO2NR9R10, or -N (R10) SO2R12, said C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl being said , unsubstituted or substituted with one or more substituents independently selected from halogen, -OH, -SH, -NH2, -O-C1-4 alkyl, -S-C1-4 alkyl, -NR10R11, cyano, nitro, -CO2H, -C (O) O-C1-4 alkyl, -CONR10R11, -CONH2, aryl, heteroaryl, heterocycloalkyl, -C (O) aryl, -C (O) heterocycloalkyl and -C (O) heteroaryl, said aryl being heteroaryl , heterocycloalkyl, -C (O) aryl, -C (O) heterocycloalkyl or -C (O) heteroaryl unsubstituted or substituted with one or more substituents independently selected from C1-4 alkyl, C1-4 haloalkyl, halogen, -OH, -SH, -NH2, -O-C1-4 alkyl, -S-al C1-4 chyl, -N (C1-4 alkyl) (C1-4 alkyl), -NH (C1-4 alkyl), cyano and nitro; and said cycloalkyl, heterocycloalkyl, aryl or heteroaryl being unsubstituted or substituted with one or more substituents independently selected from C1-6 alkyl, C1-6 haloalkyl, halogen, -OH, -SH, -NH2, -O-C1-4 alkyl , -S-C1-4 alkyl, -N (C1-4 alkyl) (C1-4 alkyl), -NH (C1-4 alkyl), cyano, nitro, -CO2H, -C (O) O-C1-alkyl 4, -CON (C1-4 alkyl) (C1-4 alkyl), -CONH (C1-4 alkyl), and -CONH2; R8 is hydrogen, halogen, hydroxy or C1-4 alkyl; or R1 and R2 or R5 and R6 or R6 and R7 or R7 and R8 taken together are alkylenedioxy; W is hydrogen, -C (O) OR11, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, - (C1-6 alkyl) - (C3-6 cycloalkyl), - (C2 alkenyl -6) - (C3-6 cycloalkyl), - (C2-6 alkynyl) - (C3-6 cycloalkyl), - (C1-6 alkyl) -heterocycloalkyl, - (C2-6 alkenyl) -heterocycloalkyl, - (C2 alkynyl -6) -heterocycloalkyl, - (C1-6 alkyl) -aryl, (C2-6 alkenyl) -aryl, - (C2-6 alkynyl) -aryl, - (C1-6 alkyl) -heteroaryl, - (C2- alkenyl 6) -heteroaryl or - (C2-6 alkynyl) -heteroaryl, said C1-10 alkyl, C2-10 alkenyl and C2-10 alkynyl being unsubstituted or substituted with one or more substituents independently selected from halogen, cyano, -OH, -O-C1-4 alkyl, -SH, -S-C1-4 alkyl, -S (O) (C1-4 alkyl), -S (O) 2H and -S (O) 2 (C1-4 alkyl) ; said C3-6 cycloalkyl is unsubstituted or substituted with one or more substituents independently selected from halogen, cyano, C1-4 alkyl, -OH, -O-C1-4 alkyl, -SH, -S-C1-4 alkyl, - S (O) (C1-4 alkyl), -S (O) 2H and -S (O) 2 (C1-4 alkyl), and the cycloalkyl, heterocycloalkyl, aryl or heteroaryl moieties of said - (C1-6 alkyl) being ) - (C3-6 cycloalkyl), - (C2-6 alkenyl) - (C3-6 cycloalkyl), - (C2-6 alkynyl) - (C3-6 cycloalkyl), - (C1-6 alkyl) -heterocycloalkyl, - (C2-6 alkenyl) -heterocycloalkyl, - (C2-6 alkynyl) -heterocycloalkyl, - (C1-6 alkyl) -aryl, (C2-6 alkenyl) -aryl, - (C2-6 alkynyl) -aryl, - ( C1-6 alkyl) -heteroaryl, - (C2-6 alkenyl) -heteroaryl or - (C2-6 alkynyl) -heteroaryl, unsubstituted or substituted with one or more substituents independently selected from C1-6 alkyl, C1-6 haloalkyl, halogen, cyano, nitro, -OH, -NH2, -O-C1-4 alkyl, -N (C1-4 alkyl) (C1-4 alkyl) and -NH (C1-4 alkyl); X is O or S; Y is -OH or -SH; Z is hydrogen or C1-4 alkyl; wherein R 9 is independently selected from the group consisting of hydrogen, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 3-8 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1-6 alkyl-C 3-8 cycloalkyl , -C1-6-heterocycloalkyl, - (C1-6 alkyl) -aryl, and - (C1-6 alkyl) -heteroaryl, - (C2-6 alkenyl) - (C3-6 cycloalkyl), - (C2- alkenyl 6) -heterocycloalkyl, - (C2-6 alkenyl) -aryl, - (C2-6 alkenyl) -heteroaryl, - (C2-6 alkynyl) - (C3-6 cycloalkyl), - (C2-6 alkynyl) -heterocycloalkyl, - (C2-6 alkynyl) -aryl, and - (C2-6 alkynyl) -heteroaryl, said C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl, unsubstituted or substituted with one or more substituents independently selected from halogen, -OR11, -NR10R11, cyano, nitro, -CO2R11, -CONR10R11, -NR10CONR10R11, -OCONR10R11, -SO2NR10 and -COR11, and said cycloalkyl being, heterocycloalkyl, aryl or heteroaryl (including cycloalkyl, heterocyclic, heterocyclic, heterocyclic, arc heteroaryl of said -alq C1-6-C3-8 -cycloalkyl, -C1-6-heterocycloalkyl, - (C1-6-alkyl) -aryl, or - (C1-6-alkyl) -heteroaryl unsubstituted or substituted with one or more substituents independently selected from C1-4 alkyl, C1-4 haloalkyl, halogen, -OR11, -NR10R11, cyano, nitro, -CO2R11, -CONR10R11, -NR10CONR10R11, -OCONR10R11, -SO2NR10R11 and -COR11; each R10 is independently selected from hydrogen and C1-6 alkyl; each R 11 is independently selected from the group consisting of hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, -C 1-4 alkyl-C 3-8 cycloalkyl, -C 1-4 alkyl-heterocycloalkyl, -C1 alkyl -4-aryl or -C 1-4 alkyl-heteroaryl; said cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or heteroarylalkyl being unsubstituted or substituted with one or more substituents independently selected from C1-6 alkyl, C1-6 haloalkyl, halogen, -O-C1-6 alkyl, - O-C1-6 haloalkyl, cyano, -N (C1-6 alkyl) (C1-6 alkyl), -NH (C1-6 alkyl), -NH2, -CO2-C1-6 alkyl, -CO2H, -CON ( C1-6 alkyl) (C1-6 alkyl), -CONH (C1-6 alkyl) and -CONH2; or when present in either NR9R10 or NR10R11, each of R9 and R10 or each of R10 and R11, independently, taken together with the nitrogen to which they are attached represent a 3-6 membered ring that optionally contains another selected heteroatom between oxygen and nitrogen, said 3-6 membered ring being unsubstituted or substituted with one or more substituents independently selected from hydrogen, C1-6 alkyl, halogen, cyano, -O-C1-6 alkyl, -OH, -N ( C1-6 alkyl) (C1-6 alkyl), -NH (C1-6 alkyl), -NH2, -CO2H, -C (O) O-C1-6 alkyl, -C (O) C1-6 alkyl, - CON (C1-6 alkyl) (C1-6 alkyl), -CONH (C1-6 alkyl), -CONH2, C3-6 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C1-6 cycloalkyl-C1-6 alkyl, heterocycloalkyl-alkyl C1-6, aryl-C1-6 alkyl, and heteroaryl-C1-6 alkyl, and said cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or unsubstituted heteroarylalkyl being or substituted with one or more substituents independently selected from C 1-6 alkyl, C 1-6 haloalkyl, halogen, -O-C 1-6 alkyl, -O-C 1-6 haloalkyl, cyano, -N (C 1-6 alkyl) (alkyl C1-6), -NH (C1-6 alkyl), -NH2, -CO2-C1-6 alkyl, -CO2H, -CON (C1-6 alkyl) (C1-6 alkyl), -CONH (C1-6 alkyl ) and -CONH2; each R 12 is independently selected from the group consisting of hydrogen, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 3-8 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1-6 alkyl-C 3-8 cycloalkyl, - C 1-6 alkyl-heterocycloalkyl, -C 1-6 alkyl-aryl and -C 1-6 alkyl-heteroaryl, -C 2-6 alkenyl-C 3-8 cycloalkyl, C 2-6 alkenyl-heterocycloalkyl, C 2-6 aryl-alkenyl, -C2-6-alkenyl-heteroaryl, -C2-6 -alkyl-C3-8 -alkyl, C2-6-alkynyl-heterocycloalkyl, -C2-6 -alkyl-aryl and -C2-6 -alkyl-heteroaryl; said C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl being unsubstituted or substituted with one or more substituents independently selected from halogen, -OR13, -NR10R13, cyano, nitro, -CO2R13, -CONR10R13, -NR10CONR10R13, - OCONR10R13, -SO2NR10R13 and -COR13; and any of said cycloalkyl, heterocycloalkyl, aryl or heteroaryl being unsubstituted or substituted with one or more substituents independently selected from C1-4 alkyl, C1-4 haloalkyl, halogen, -OR13, -NR10R13, cyano, nitro, -CO2R13, - CONR10R13, -NR10CONR10R13, -OCONR10R13, -SO2NR10R13 and -COR13; each R 13 is independently selected from the group consisting of hydrogen, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 3-8 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1-6 alkyl-C 3-8 cycloalkyl, -C 1-6 alkyl-heterocycloalkyl, -C 1-6 alkyl-aryl and -C 1-6 alkyl-heteroaryl; with the proviso that when X is O, Y is OH and Z, R1, R2, R3, R4, R5, R6, R7 and R8 are hydrogen; W is not hydrogen, -CH3, -C2H5, -nC3H7, -nC4H9, -nC5H11, -nC6H13, -nC7H15, - (CH2) CH (CH3) 2, - (CH2) 2CH (CH3) 2, -CH2CH = CH2 , -CH2CH = CH (CH3), - (CH2) 3CN, - (CH2) 4CN, - (CH2) phenyl |
| priorityDate | 2001-06-07-04:00^^<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: 75.