http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-072747-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D285-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D243-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D241-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-551 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-06 |
| filingDate | 2009-07-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5df9d7e996793a85d4a746fdaa693d97 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2e6de93399b16fca8512d7b71b40edec http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_aee0e0ef6e0905e6b0ad53f19d41ac52 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_027b02953f27c8fe8bf305ffa3b10a8d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5da5dea38a5b59e4f438b848a75314c5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7ac7eacba374807feab484feb085af25 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e1f8a369915641529fb573156f80434c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8fc1b58f4f9603395c75ae2c2c2b0c2e |
| publicationDate | 2010-09-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-072747-A1 |
| titleOfInvention | DERIVATIVES OF OXO-PIPERAZINA AND OXO-DIAZEPAN, METHODS FOR THEIR PREPARATION AND ITS USE FOR THE TREATMENT OF DISEASES MEDIATED BY THE ANTAGONISM OF THE RECEIVERS CCR2, CCR3 OR CCR5. |
| abstract | These compounds are antagonists of the CCR2 receptor, CCR5 receptor and / or CCR3 receptor and can be used as a medication for the treatment of asthma, rheumatoid arthritis and stroke among other diseases. Claim 1: Compounds of the formula (1) wherein A is aryl, heteroaryl, arylmethyl or heteroarylmethyl, the aryl of said aryl and arylmethyl and the heteroaryl of said heteroaryl and heteroarylmethyl are optionally substituted one to three times by substituents chosen with independence between the group consisting of halogen, aryl, heteroaryl, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 alkoxy and C 1-6 haloalkoxy, or said aryl and heteroaryl are optionally substituted by C 1-6 alkylenedioxy; X is -N (R1) (R2); R1 and R2 are independently hydrogen, C1-6 alkyl, C3-6 alkenyl, C3-6 alkynyl, C2-6 hydroxyalkyl, (C1-6 alkoxy) -C2-6 alkyl, C3-7 cycloalkyl, (C3-7 cycloalkyl ) -C1-6 alkyl, C7-10 bicycloalkyl, C1-3 phenylalkyl, C1-3 heteroaryl-alkyl, heterocyclyl, or C1-6 heterocyclyl alkyl in which the cycloalkyl of said C3-7 cycloalkyl and (C3-7 cycloalkyl) - C1-3 alkyl, the phenyl of said C1-3 phenylalkyl, the heteroaryl of said heteroaryl-C1-3 alkyl and the heterocyclyl of said heterocyclyl and C1-6 heterocyclyl alkyl are optionally substituted one to three times by substituents independently selected from the group formed by Rd; or R1 and R2 together with the nitrogen atom to which they are attached form a heterocyclyl optionally substituted one to three times by substituents independently selected from the group consisting of and one of the carbon atoms of said heterocyclyl ring formed by R1 and R2 it has been optionally replaced by a carbonyl group; and / or one of the carbon atoms of the heterocyclyl ring formed by R1 and R2 may be a carbon atom of another ring that is C3-7 cycloalkyl or heterocyclyl, one or two carbon atoms of said other ring have been optionally replaced by a carbonyl group and said other ring is optionally substituted by C1-6 alkyl; R 3 and R 4 are independently hydrogen, hydroxy, C 1-6 alkyl, C 1-6 alkoxy, C 3-7 cycloalkyl, (C 3-7 cycloalkyl) -C 1-6 alkyl, (C 1-6 alkoxy) -carbonyl, carboxyl, carbamoyl, mono- or disubstituted carbamoyl by C1-6 alkyl, (C1-6 alkoxy) -carbonyloxy, aminocarbonyloxy mono- or di-substituted by C1-6 alkyl, (C1-20 alkyl) -carbonyloxy-C1-6 alkyl, (C1- alkoxy 20) -carbonyloxy-C1-6 alkyl, aryl-carbonyloxy-C1-6 alkyl, aminocarbonyloxy-C1-6 alkyl mono- or disubstituted by C1-6 alkyl, aminocarbonyloxy-C1-6 alkyl substituted by aryl, hydroxy C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, halogen or C1-6 haloalkyl, said aryl are optionally substituted one to three times by substituents independently selected from the group consisting of halogen, C1-6 alkyl, C1-6 haloalkyl, alkoxy C1-6 and C1-6 haloalkoxy; or R3 and R4, together with the carbon atom to which they are attached form C3-7 cycloalkyl or heterocyclyl optionally substituted one to three times by substituents independently selected from the group consisting of C1-4 alkyl, C1-4 haloalkyl and halogen ; Y1 is C (O) or S (O) 2; Y2 is O or S; Y3 is NH or O; p is the number 0 or 1; R5 and R6 are independently hydrogen, C1-6 alkyl or C3-7 cycloalkyl, said C1-6 alkyl and C3-7 cycloalkyl are optionally substituted one to three times by substituents independently selected from the group consisting of amino, hydroxy, carboxyl, carbamoyl, carbamoyl mono- or disubstituted by C1-6 alkyl and (C1-6 alkoxy) -carbonyl; or R5 and R6 together with the carbon atom to which they are attached form a C3-7 cycloalkyl or heterocyclyl; R7, R8, R9 and R10 are independently hydrogen, C1-6 alkyl, C3-7 cycloalkyl or aryl, said C1-6 alkyl is optionally substituted one to three times by substituents independently selected from the group consisting of hydroxy, alkoxy C1-6, carboxyl, carbamoyl, carbamoyl mono- or disubstituted by C1-6 alkyl and (C1-6 alkoxy) -carbonyl, aryl and heteroaryl, said aryl and heteroaryl are optionally substituted one to three times by substituents independently selected from the group consisting of halogen, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy and C1-6 haloalkoxy; Rd is hydroxy, cyano, NRaRb, halogen, C1-6 alkyl, C1-6 haloalkyl, C1-6 hydroxyalkyl, C1-6 alkoxy, (C1-6 alkoxy) -C1-6 alkyl, C3-7 cycloalkyl, (C1 alkoxy -6) -carbonyl, acyl, -c (o) NRaRb, -NRa-C (O) -Rb, -NRa-C (O) ORb, NRa-C (O) -NRb, NRa-so2-Rb, NRa -so2-NRbRc, -OC (O) NRaRb, -oc (o) oRa, C1-6 alkylsulfonyl, C1-6 alkylsulfinyl, C1-6 alkylthio, phenyl, phenyl-C1-3alkyl, heteroaryl, C1-3 heteroarylalkyl and heterocyclyl, and the phenyl of said phenyl and phenyl-C1-3alkyl, the heteroaryl of said heteroaryl and heteroaryl-C1-3alkyl, and the heterocyclyl are optionally substituted one to three times by substituents independently selected from the group consisting of hydroxy, cyano, NRaRb, halogen, C1-6 alkyl, C1-6 haloalkyl, C1-6 hydroxyalkyl, (C1-6 alkoxy) -carbonyl, acyl, -c (o) nRaRb, NRa-c (o) -Rb, -NRa-C (O) -ORb, NRa-C (O) -NRb, -NRa-so2-Rb, -NRa-so2-NRbRc, -OC (O) NRaRb, -OC (O) ORa, C1-alkylsulfonyl 6, C1-6 alkylsulfinyl and C1-6 alkylthio and one or two car atoms heterocyclyl ring bond has been optionally replaced by a carbonyl group; Ra, Rb and Rc are independently hydrogen or C1-6 alkyl; n is an integer from 0 to 3; m is an integer from 0 to 3; m + n is an integer from 1 to 5; or the pharmaceutically acceptable prodrugs or salts thereof; wherein, unless otherwise indicated, the term "aryl" means phenyl or naphthyl; the term "heterocyclyl" means mono- or bicyclic non-aromatic moieties, from four to nine ring atoms, from one to three of said ring atoms are heteroatoms chosen from N, O and S (O) n (said n is an integer from 0 to 2), the other atoms of the ring are C; the term "heteroaryl, alone or in combination with other groups, means an aromatic monocyclic or bicyclic moiety of 5 to 10 atoms in the ring, having one to three heteroatoms in the ring, which are independently selected from N, O and S, the other atoms in the ring are C; the term 'acyl' means RC (O) -, in which R is C 1-6 alkyl, C 1-6 haloalkyl, C 3-7 cycloalkyl, or C 3-7 cycloalkyl-C 1-6 alkyl 6. |
| priorityDate | 2008-07-16-04:00^^<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: 50.