http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-047587-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c76ecadad74a1a35270b3e3a34d60f37 |
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| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D237-32 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-096 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D215-227 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D231-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D241-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D237-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D217-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-04 |
| filingDate | 2005-01-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2006-01-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-047587-A1 |
| titleOfInvention | HISTAMINE-3 RECEIVER MODULATORS |
| abstract | Pharmaceutical composition that understands them and uses. Claim 1: A compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein: R1 is selected from the group consisting of N3, OR4 and NR2R3; R2 and R3 are each independently selected from the group consisting of hydrogen; C1-8 alkyl optionally substituted with 1 to 4 halogens; C1-4 alkyl group optionally substituted with a substituent selected from the group consisting of OH, from one to four C1-4 alkyl, C3-7 cycloalkyl, C1-4 dialkylamino, C6-14 aryl optionally substituted with a halogen and optionally substituted with aryloxy C6-10 optionally substituted with one to two halogens, and 5-10 membered heteroaryl optionally substituted with a C6-10 aryl group and optionally substituted with one to three C1-4 alkyl groups; C3-7 cycloalkyl; C6-14 aryl; 3-8-membered heterocycloalkyl optionally substituted with one or more (C1-4) alkylcarbonyl groups; C6-10 arylsulfonyl optionally substituted with one or more C1-2 alkyl; 5-10 membered heteroaryl; and aryl (C6-14) -alkylene (C0-4) -O-alkyl (C0-4), where each C0-4 alkyl and each C0-4 alkylene is optionally substituted with one to four C1-4 alkyl; where R3 can also be selected from the group consisting of: arylcarbonyl (C6-14) -aryl (C6-14); 3-8-membered arylcarbonyl (C6-14) -heterocycloalkyl; (C3-8) cycloalkylcarbonyl (C6-14) aryl; C 3-8 cycloalkylcarbonyl-3-8 membered heterocycloalkyl; 3-8 membered heterocycloalkylcarbonyl (C6-14); and 3-8-membered heterocycloalkylcarbonyl-3-8-membered heterocycloalkyl; or R3 and R2 together with the nitrogen of the NR2R3 group form a first aliphatic ring of 5, 6 or 7 members, in which one of the carbons in the first aliphatic ring of 5, 6 or 7 members is optionally substituted by O, S , NR2 'or CO, and the first 5, 6 or 7 membered aliphatic ring is optionally fused to a C6-10 arylene and is optionally substituted on a ring carbon with a substituent selected from the group consisting of 5-10 membered heteroaryl optionally substituted with one or more halogens and optionally substituted with one or more C1-2 alkyl; C1-4 alkoxy optionally substituted with one or more C1-2 alkoxy and optionally substituted with one or more C1-4 dialkylaminocarbonyl; and one or two C1-4 alkyl optionally and independently substituted with one or more C1-2 alkoxy; where R2 'is: hydrogen; C1-8 alkyl optionally substituted with 1 to 4 halogens; 5-10 membered heteroaryl optionally substituted with a substituent selected from the group consisting of halogen, C1-4 alkyl, C1-2 alkoxy, C6-10 aryl, C1-4 alkylaminocarbonyl and cyano; a C1-4 alkyl group optionally substituted with a substituent selected from the group consisting of C1-2 alkoxycarbonyl, 5-10 membered heteroaryl optionally substituted with one or more C1-2 alkyl, one to four C1-4 alkyl, C3 cycloalkyl -7 and C6-14 aryl; C6-10 aryl optionally substituted with one or two C1-2 alkyl; C1-4 alkylcarbonyl; or aryl (C6-14) -alkylene (C0-4) -O-alkyl (C0-4), where each C0-4 alkyl and each C0-4 alkylene is optionally substituted with one to four C1-4 alkyl; R4 is: hydrogen; C1-8 alkyl optionally substituted with 1 to 4 halogens; C1-4 alkyl optionally substituted with a substituent selected from the group consisting of C3-7 cycloalkyl; 5-10 membered heteroaryl; and C6-14 aryl optionally substituted with a substituent selected from the group consisting of one, two or three halogens, cyano, one or two C1-2 alkoxy, di or trifluoroalkyl C1-2, C1-4 alkyl optionally substituted with C6-10 arylsulfonyl , 5-10 membered nitro and heteroaryl; 5-10 membered heteroaryl fused to a C6-10 arylene group that is optionally substituted with one or more halogens or one or more C1-2 alkoxy, where the 5-10 membered heteroaryl is optionally substituted with a substituent selected from the group consisting by: C6-10 aryl optionally substituted with one or more halogens, one or more C1-2 alkoxy or one or more C1-2 alkyl; C6-10 arylcarbonyl optionally substituted with one or more halogens; one or more halogens; from one to three C1-4 alkyl groups optionally substituted with one or more C6-10 aryl optionally and independently substituted with one or more halogens or one or more C1-2 alkoxy; di or trifluoroalkyl C1-2; from 1 to 2 C1-2 alkoxy groups; 3-8-membered heterocycloalkyl; 5-10 membered heteroarylamino; (C1-2) alkylaminocarbonyl-C1-2 alkylamino; C6-10 arylaminocarbonyl; C6-10 arylaminocarbonyl-C1-2 alkylamino optionally substituted with one or more halogens in the C6-10 arylaminocarbonyl aryl moiety; 5-10 membered heteroaryl optionally substituted with one or more C6-10 aryl or one or more C1-2 alkyl; C6-10 aryloxy optionally substituted with one or more C1-2 alkoxy or one or more halogens; and C1-4 dialkylamino; C6-14 aryl optionally substituted with one or more halogens and optionally substituted with one or more C6-10 aryloxy optionally and independently substituted with one to two halogens; aryl (C6-14) -alkylene- (C0-4) -O-alkyl (C0-4), where each C0-4 alkyl and each C0-4 alkylene is optionally substituted with one to four C1-4 alkyl; or C6-10 arylsulfonyl optionally substituted with C1-2 alkyl; R6 is hydrogen, C1-4 alkyl or halogen; R7 is hydrogen, SO2 (C1-10) alkyl -, C1-8 alkyl optionally substituted with 1 to 4 halogens, cycloalkyl (C3-7) -alkyl (C0-4), aryl (C6-14) -alkyl ( C0-4), 5-10 membered heteroaryl-(C0-4) alkyl, or (C6-14) -aryl (C0-4) -O- (C0-4) alkyl, where each C0-4 alkyl and each C0-4 alkylene is optionally substituted with one to four C1-4 alkyl; R10 is OH, halogen or hydrogen; R8 is CN, -CHR7'CR2''R3 '' 'or C (= NR12) -NR13R13', where R13 and R13 'are each independently hydrogen or C1-6 alkyl and R12 is hydrogen, C1-6 alkyl OH, O-C1-6 alkyl, NH2, NH-C1-6 alkyl or N (C1-6 alkyl) 2, or where C (= NR12) -NR13R13 ', represents a five-membered heteroaryl group, where R12 is O, NH or N-C1-6 alkyl, R13 and R13 'together represent N or CR13' 'linked by a double bond to the nitrogen of the group NR13R13', and R13 '' is hydrogen or C1-6 alkyl ; or when R8 is ortho to R6, R6 and R8 together with the carbons of the aromatic ring to which R6 and R8 are attached they can form a 5-membered carbocyclic ring; R2 '' is hydrogen, C1-8 alkyl optionally substituted with 1 to 4 halogens, cycloalkyl (C3-7) -alkyl (C0-4), aryl (C6-14) -alkyl (C0-4), heteroaryl of 5 -10-alkyl (C0-4) or aryl (C6-14) -alkylene (C0-4) -O-alkyl (C0-4), where each C0-4 alkyl and each C0-4 alkylene is optionally substituted with from one to four C1-4 alkyl; R3 '' is hydrogen, C1-8 alkyl optionally substituted with 1 to 4 halogens, C6-14 aryl, C6-14 arylcarbonyl (C6-14) aryl, (C6-14) arylcarbonyl 3-8 heterocycloalkyl members, C 3-8 cycloalkylcarbonyl (6-14), C 3-8 cycloalkylcarbonyl 3-8 membered heterocycloalkyl, 3-8 membered heterocycloalkyl, 3-8 membered heterocycloalkylcarbonyl (C6-14) or 3-8-membered heterocycloalkylcarbonyl-3-8-membered heterocycloalkyl; or R3 '' and R2 '' together with the nitrogen of the CHR7'NR2''R3 '' group form a second aliphatic ring of 5, 6 or 7 members, where one of the carbons in the second aliphatic ring of 5, 6 or 7 members is optionally substituted by O, S, NR11 or C = O, and the second aliphatic ring of 5, 6 or 7 members is optionally substituted with one or two C1-4alkyl or optionally substituted with OH, where R11 is hydrogen, C1-8 alkyl optionally substituted with 1 to 4 halogens, cycloalkyl (C3-7) -alkyl (C0-4), aryl (C6-14) -alkyl (C0-4), 5-10-membered heteroaryl-alkyl ( C0-4), or aryl (C6-14) -alkylene (C0-4) -O-alkyl (C0-4), where each C0-4 alkyl and each C0-4 alkylene is optionally substituted with one to four alkyl C1-4; and R7 'is hydrogen, C1-8 alkyl optionally substituted with 1 to 4 halogens, cycloalkyl (C-37) -alkyl (C0-4), aryl (C6-14) -alkyl (C0-4), heteroaryl of 5 -10 members (C0-4) alkyl, C6-14 aryl-C0-4 alkylene-C0-4 alkyl, where each C0-4 alkyl and each C0-4 alkylene is optionally substituted with from one to four C1-4 alkyl or SO2-C1-10 alkyl. |
| priorityDate | 2004-02-02-04:00^^<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: 71.