http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-077147-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_05a203d85ee01909eaf728dc16f0f6cb |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4738 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D215-60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 |
| filingDate | 2010-06-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_667a0094c281397850d13df5c7c6b081 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_67552b7b38aea238f899d93ce62fa988 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_577f83ad917e67c16a619c57bca7919f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4257e5afd80c7840b721a90f4ec9c2df http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_70fbd63e0644b860f7be052e54a44061 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b8a1cdb0617c91c89a18b42a4652a9ab http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8a00c01afbf5c916504c3742df450bc8 |
| publicationDate | 2011-08-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-077147-A1 |
| titleOfInvention | BICYCLE AND TRICICLIC COMPOUNDS AS KAT II INHIBITORS |
| abstract | Compounds of formula (1) and their pharmaceutically acceptable salts, as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and / or neurological disorders in mammals, including the human claim 1: A compound of formula (1) characterized because A, X, Y, and Z are defined as follows: (i) A is N or CR1, X is N or CR2, Y is N or CR3, and Z is N or CR4, with the proviso that no more than two of A, X, Y, and Z are N; (ii) A and X together form a 5 or 6-membered aromatic, heteroaromatic ring containing N, or heterocycloalkyl containing O, condensed with the ring containing A and X, Y is N or CR3, and Z is N or CR4 , wherein the 5 or 6-membered aromatic, heteroaromatic ring containing N, or heterocycloalkyl containing O is substituted with R1 and R2; (iii) X and Y together form a 5 or 6-membered aromatic, heteroaromatic ring containing N, or heterocycloalkyl containing O, condensed with the ring containing X and Y, A is N or CR1, and Z is N or CR4 , wherein the 5 or 6-membered aromatic, heteroaromatic ring containing N, or heterocycloalkyl containing O is substituted with R2 and R3; or (iv) Y and Z together form a 5- or 6-membered aromatic, heteroaromatic ring containing N, or heterocycloalkyl containing O, condensed with the ring containing Y and Z, A is N or CR1, and X is N or CR2, wherein the 5 or 6-membered aromatic, heteroaromatic ring containing N, or heterocycloalkyl containing O is substituted with R3 and R4; R1 is H, halogen, alkyl, alkoxy or cyclopropyl; R2, R3, and R4 are independently H, halogen, alkyl, aryl, aralkyl, heteroaryl, alkoxy, cycloalkyloxy, alkoxyaryl, aryloxy, aralkyloxy, heterocycloalkyloxy, heteroaryloxy, cycloalkyl, alkylaryloxy, alkylheterocycloalkyl, alkylheteroaryloxy, CN8, hetero8, NR8, hetero8, NR8, hetero8, NR7, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR7, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR7, hetero8, NR8, hetero8, NR7, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8, NR8, hetero8 C (= O) NR7R8, SO2NR7R8, SO2R7a, NR7SO2R7a, and NR7C (= O) R7a, wherein each of said alkyl, aryl, aralkyl, heteroaryl, alkoxy, cycloalkyloxy, alkoxyaryl, aryloxy, aralkyloxy, heterocycloalkyloxy, heterocycloalkyloxy, cycloalkyl, alkylaryloxy, alkylheterocycloalkyl, alkylheteroaryloxy, and heterocycloalkyl may be substituted with one or more substituents selected from hydroxy, amino, halogen, alkyl, haloalkyl, CN, alkoxy, haloalkoxy, alkylamino, and aminoalkyl; R5 is H, C (= O) R9, C (= O) OR9, C (= O) NR9aR9b, or (CH2) R10; R6a and R6b are independently H, methyl, halomethyl, fluorine, or methoxy; each R7 and R8 is independently H, alkyl, haloalkyl, aryl, or heteroaryl; each R7a is independently alkyl, haloalkyl, aryl, or heteroaryl; R9 is alkyl, aryl, heteroaryl, or cycloalkyl, wherein each of said alkyl, aryl, heteroaryl, and cycloalkyl may be substituted with one or more substituents selected from hydroxy, amino, halogen, alkoxy, and aminoalkyl; each R9a and R9b is independently H, alkyl, aryl, heteroaryl, or cycloalkyl, wherein each of said alkyl, aryl, heteroaryl, and cycloalkyl may be substituted with one or more substituents selected from hydroxy, amino, halogen, alkoxy, and aminoalkyl, or when R5 is C (= O) NR9aR9b, R9a and R9b, together with the nitrogen atom to which they are attached, form a heterocyclic ring containing 5 or 6 membered N; R10 is of structure (2) where R11 is H, alkyl, aryl, heteroaryl, or cycloalkyl, wherein each of said alkyl, aryl, heteroaryl, and cycloalkyl may be substituted with one or more substituents selected from hydroxy, amino, halogen, alkoxy, and aminoalkyl; and its pharmaceutically acceptable salts; with the proviso that the compound of formula (1) is not (3S) -3-amino-7- bromo-1-hydroxy-3,4-dihydroquinolin-2 (1H) -one; (3R) -3-amino-7-bromo-1-hydroxy-3,4-dihydroquinolin-2 (1H) -one; rac-3-amino-7-bromo-1-hydroxy-3,4-dihydroquinolin-2 (1H) -one; rac-3-amino-8-chloro-1-hydroxy-3,4-dihydroquinolin-2 (1H) -one; rac-3-amino-7-chloro-1-hydroxy-3,4-dihydroquinolin-2 (1H) -one; rac-3-amino-7-fluoro-1-hydroxy-3,4-dihydroquinolin-2 (1H) -one; rac-3-amino-6-chloro-1-hydroxy-3,4-dihydroquinolin-2 (1H) -one; rac-3-amino-5-chloro-1-hydroxy-3,4-dihydroquinolin-2 (1H) -one; rac-3-amino-6-bromo-1-hydroxy-3,4-dihydroquinolin-2 (1H) -one; rac-3-amino-6-fluoro-1-hydroxy-3,4-dihydroquinolin-2 (1H) -one; rac-3-amino-1-hydroxy-4-methyl-3,4-dihydroquinolin-2 (1H) -one; (3S) -3-amino-1-hydroxy-3,4-dihydroquinolin-2 (1H) -one; or (3R) -3-amino-1-hydroxy-3,4-dihydroquinolin-2 (1H) -one. |
| priorityDate | 2009-06-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 80.