http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-074814-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/Y02A50-30 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-553 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-551 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D407-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-052 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 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/A61P19-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D451-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 |
| filingDate | 2009-12-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d56cfddb782818dba7e2053d85697ccd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7f1e697155fc752ab353e3ceb4c96a0e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_83feb63e7ed92d806a0910df564d60a6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0572bd1fca1012d63b1e63e80b6bdc3f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8bf69d77c7a94c6e71c6eb401e0590dd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b095ed332dbbd56396842e55be05b6e4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e901f1b46428540019f17638449a4343 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_883b9e9cfde4994ad9983c1b95aa57ed |
| publicationDate | 2011-02-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-074814-A1 |
| titleOfInvention | PYRIMIDINES REPLACED AS ANTAGONISTS OF THE CCR2 RECEIVER AND USES OF THE SAME IN MEDICINES. |
| abstract | Novel antagonists for CCR2 (CC chemokine receptor 2) and its use to provide medications to treat conditions and diseases, especially lung diseases such as asthma and COPD. Claim 1: Compounds characterized in accordance with formula (1), wherein R1 is -L1-R7, wherein L1 is a linker selected from a bond or a group selected from -C1-2 alkylene and -alkenylene C1-2 optionally comprising one or more groups selected from -O-, -C (O) - and -NH- in the chain and which is optionally substituted with a group selected from -OH, -NH2, -C1-3 alkyl , C 1-6 alkyl and -CN, wherein R 7 is a ring selected from C 3-8 cycloalkyl, C 3-8 heterocyclyl, C 5-10 aryl, and C 5-10 heteroaryl, wherein the ring R7 is optionally substituted with one or more groups selected from -CF3, -O-CF3, -CN and -halogen, or in which the R7 ring is optionally substituted with one or more groups selected from -C1-6 alkyl, -O -C1-6 alkyl, -C5-10 aryl, -C5-10 heteroaryl, -C3-8 cycloalkyl, -C3-8 heterocyclyl, -C1-6 alkenyl and -C1-6 alkynyl, being optionally substituted with one or more groups selected cited between -OH, -NH2, -C1-3 alkyl, -O-C1-6 alkyl, -CN, -CF3, -OCF3, halogen y = O, or in which the R7 ring is optionally further substituted bi-valent at two neighboring atoms in the ring, such that an anelated ring is formed with one or more groups selected from -C 1-6 alkylene, C 2-6 alkenylene and C 4-6 alkenylene, where one or two carbon centers can optionally replaced by 1 or 2 heteroatoms selected from N, O and S, the bivalent group being optionally substituted with one or more groups selected from -OH, -NH2, C1-3 alkyl, -O-C1-6 alkyl, -CN, -CF3, -OCF3, halogen y = O; wherein R2 is selected from -H, -halogen, -CN, -O-C1-4alkyl, -C1-4alkyl, -CH = CH2, -C ::: CH, -CF3, -OCF3, -OCF2H and -OCFH2; wherein R3 is selected from -H, -methyl, -ethyl, -propyl, -i-propyl, -cyclopropyl, -OCH3 and -CN; wherein R4 and R5 are independently selected from an electron pair, -H and a group selected from -C1-6 alkyl, -NH2, -C3-8cycloalkyl, -C3-8 heterocyclyl, -C5-10 aryl, - C5-10 heteroaryl, and -C (O) -N (R8R8 '), where R8 and R8' are independently selected from -H and -C1-6 alkyl, and in which R4 and R5, if different from a pair of electrons or are -H, are optionally independently substituted with one or more groups selected from -halogen, -OH, -CF3, -CN, -C1-6 alkyl, -O-C1-6 alkyl, -O-C3 cycloalkyl- 8, -O-C3-8 heterocyclyl, -O-C5-10 aryl, -O-C5-10 heteroaryl, -C0-6-CN alkylene, -C0-4 alkylene-C1-4 alkyl, -C0-4 alkylene -O-C3-8 cycloalkyl, -C0-4-O-C3-8 heterocyclyl, -C0-4-O-C6-10 -alkyl, -C0-4-O-C5-10 -alkylene alkyl, -C0 alkylene -4-Q-C0-4-N alkyl (R9R9 '), -C0-4-N alkylene (R10) -Q-C1-4 alkyl, -C0-4-N alkylene (R10) -Q-C3 cycloalkyl- 8, -C0-4-N alkylene (R10) -Q-C3-8 heterocyclyl, -C0-4-N alkylene (R10) -Q-ari C5-10, -C0-4-N alkylene (R10) -Q-C5-10 heteroaryl, -C0-4-QN alkylene (R11R11 '), -C0-4-N alkylene (R12) -QN (R13R13' ), -C0-4-R14 alkylene, -C0-4-Q-C 1-6 alkyl, -C0-4-Q-C3-8 -alkyl alkyl, -C0-4-Q-C3-8 heterocyclyl, - C0-4-Q-C5-10 alkylene, C0-4-Q-C5-1o-alkylene, C0-4-OQN (R15R15 ') alkylene and C0-4-N (R16) -QO- alkylene (R17), in which Q is selected from -C (O) - and -SO2-, in which R12 and R16 are independently selected from -H, -C1-6 alkyl and -C3-6 cycloalkyl, in which R9, R9 'R10, R11, R11', R13, R13 ', R15 and R15' are independently selected from -H, -C1-6 alkyl and -C3-6 cycloalkyl, or where R9 and R9 ', R11 and R11 ', R13 and R13', R15 and R15 'together form a -C2-6 alkylene group, in which R14 and R17 are independently selected from -H, -C1-6 alkyl, -C5-10 aryl, -C5 heteroaryl -10, -C3-8cycloalkyl and -C3-8 heterocyclyl, wherein said -C3-8 heterocyclyl optionally comprises nitrogen and / or -SO2- in the ring, and in which R14 and R17 are optionally substituted with one or more groups selected from -OH, -OCH3, -CF3, -OCF3, -CN, -halogen, -C 1-4 alkyl, = O and -SO2- C1-4 alkyl, or in which R4 and / or R5 are independently a group of the structure -L2-R18, in which L2 is selected from -NH- and -N (C1-4 alkyl) -, in which R18 is selected from -C5-10 aryl, -C5-10 heteroaryl, -C3-8 cycloalkyl and -C3-8 heterocyclyl, wherein R18 is optionally substituted with one or more groups selected from halogen, -CF3, -OCF3, -CN, -OH, -O-C1-4 alkyl, -C1-6 alkyl, -NH-C (O) -C1-6 alkyl, -N (C1-4 alkyl) -C (O) -C1-alkyl 6, -C (O) -C 1-6 alkyl, -S (O) 2-C 1-6 alkyl, -NH-S (O) 2-C 1-6 alkyl, -N (C 1-4 alkyl) -S ( O) 2-C1-6 alkyl and -C (O) -O-C1-6 alkyl, and in which R4, R5 and R18 are optionally further substituted with C3-8 spirocycloalkyl or C3-8 spiro-heterocyclyl such that together with R4, R5 and / or R18 a spirocycle is formed, wherein said C3-8 spiro-heterocyclyl optionally comprises one or more groups selected from nitrogen, -C (O) -, -SO2- and -N (SO2-C1-4 alkyl) - in the ring, or in which R4, R5 and R18 are optionally further substituted bivalently with one or more groups forming spirocyclic or anelated rings selected from -C 1-6 alkylene, C 2-6 alkenylene and C 4-6 alkenylene, where one or two carbon centers may optionally be replaced by one or two heteroatoms selected from N, O and S and which may be optionally substituted with one or more groups in one ring atom or in two neighboring atoms in the ring selected from -OH, -NH2, -C1-3 alkyl, O-C1-6 alkyl, -CN , -CF3, -OCF3 and halogen; wherein R6 is selected from -H, -C1-4alkyl, -OH, -O-C1-4alkyl, -halogen, -CN, -CF3 and -OCF3: where A is selected from a single bond, = CH-, -CH2-, -O-, -S- and -NH-; in which n is 1, 2 or 3; wherein Z is C or N, as well as in the form of its acid addition salts with pharmacologically acceptable acids. |
| priorityDate | 2008-12-19-04:00^^<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: 61.