http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-068639-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/C07D403-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 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/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D295-192 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/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-58 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/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 |
| filingDate | 2008-09-30^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ed46f90cfa6f27c1e720ff4f4c517fef http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2e6de93399b16fca8512d7b71b40edec http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5da5dea38a5b59e4f438b848a75314c5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f5b0da28895765dd2b438ffb3dbd6cd1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_027b02953f27c8fe8bf305ffa3b10a8d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_aee0e0ef6e0905e6b0ad53f19d41ac52 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5df9d7e996793a85d4a746fdaa693d97 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8fc1b58f4f9603395c75ae2c2c2b0c2e |
| publicationDate | 2009-11-25^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-068639-A1 |
| titleOfInvention | BIARILO DERIVATIVES |
| abstract | The compound, a pharmaceutical composition and the use of the compound to prepare medicaments are claimed. Claim 1: Compounds of formula (1) wherein R 1 is halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 haloalkyl, heteroalkyl, C 1-6 alkylsulfanyl, C 1-6 alkylsulfinyl, C 1-6 alkylsulfonyl, C 3 cycloalkyl -7, C3-7 cycloalkylC1-6alkyl; R2 is hydrogen, C1-6 alkyl, C1-6 haloalkyl, trimethylsilanyl-C1-6 alkyl, heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 hydroxy-alkenyl, C3-6 hydroxy-alkynyl, C1- alkoxy 6 C3-6alkenyl, C1-6 alkoxyC3-6 alkynyl, trimethylsilynylC2-6 alkynyl, hydroxy, C1-6 alkoxy, optionally substituted C1-6 haloalkoxy, heteroalkoxy, C3-7 cycloalkyl optionally substituted C3-7alkyl , halogen, cyano, optionally substituted phenyl, optionally substituted heteroaryl, optionally substituted heterocyclyl or optionally substituted phenylmethoxy C1-6 alkoxy, provided that the optionally substituted phenyl does not possess a nitro as. substituent; R3 is, when attached to a ring carbon atom, independently hydrogen, C1-6 alkyl, C1-6 haloalkyl, heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 hydroxy-alkenyl, C3 hydroxy-alkynyl -6, C1-6 alkoxyC3-6 alkenyl, C1-6 alkoxyC3-6 alkynyl, hydroxy, C1-6 alkoxy, C1-6 haloalkoxy, heteroalkoxy, halogen, cyano, optionally substituted phenyl, optionally substituted C3-7 cycloalkyl, C3 cycloalkyl -7 optionally substituted C1-6 alkyl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-6 phenylalkyl, optionally substituted C1-6 heteroarylalkyl, optionally substituted C1-6 heterocyclylalkyl, nitro, carboxy, formyl, acyl, C1-6 alkoxycarbonyl , carbamoyl, aminocarbonyl substituted by mono- or di- C1-6 alkyl, thioalkyl C1-6, alkylsulfinyl C1-6 or alkylsulfonyl C1-6 or amino optionally substituted by one or two substituents independently, selected from the group consisting of C1-6 alkyl, heteroalkyl, optionally substituted C3-7 cycloalkyl and optionally substituted heterocyclyl; when attached to a ring nitrogen atom, independently hydrogen, C1-6 alkyl, C1-6 haloalkyl, heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 hydroxy-alkenyl, C3-6 hydroxy-alkynyl, C1-6 alkoxyC3-6 alkenyl, C1-6 alkoxyC3-6 alkynyl, optionally substituted C3-7 cycloalkyl or optionally substituted C3-7 cycloalkyl, optionally substituted heterocyclyl, or optionally substituted heterocyclyl C1-6 alkyl; m is 0, 1, 2, 3 or 4; the cyclic part A in the formula (1) is heterocyclyl, which is a non-aromatic mono-cyclic radical of four. to eight atoms in the ring, in which one or two atoms in the ring are nitrogen atoms, the rest of the atoms in the ring being carbon atoms; one of X1, X2 and X3 is C-R4, the others are independently N or C-R5; R4 is phenyl or heteroaryl, which is an aromatic monocyclic radical of six ring atoms, in which one or two atoms in the ring are nitrogen atoms, the remaining atoms in the ring being carbon atoms, and said phenyl and said heteroaryl are substituted by one, two or three substituents independently selected from the group consisting of C1-8 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkyloxy, halogen and cyano; R5 is hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl or halogen; provided that the cyclic part A contains at least one nitrogen atom, which is not directly linked to the carbonyl group or to a heteroatom; and that the cyclic part A does not contain a nitrogen atom, which is directly attached to a heteroatom; and provided that the cyclic part A is not optionally substituted 2- (pyrrolidin-1-yl-C 1-6 alkyl) -pyrrolidine-1-yl; or pharmaceutically acceptable prodrugs or salts thereof, in which, unless otherwise indicated, the term "heterocyclyl" denotes non-aromatic monocyclic radicals of four to seven atoms in the ring, in which one to three atoms in the ring they are heteroatoms independently selected from N, O and S (O) n (in which n is an integer between 0 and 2), the remaining atoms in the ring being atoms of C; the term "heteroaryl" indicates an aromatic mono-cyclic radical of 5 or 6 ring atoms, with one to three ring heteroatoms independently selected from N, O, and S, with the remaining atoms in the ring being atoms of C ; the term "optionally substituted C3-7cycloalkyl" indicates a C3-7 cycloalkyl optionally substituted by one to three substituents independently selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 hydroxy-alkenyl, C3-6 hydroxy-alkynyl, C1-6 alkoxyC3-6 alkenyl, C1-6 alkoxyC3-6 alkoxy, hydroxy, C1-6 alkoxy, C1-6 haloalkoxy, heteroalkoxy, C3-7 cycloalkyl, cycloalkyl C3-7 C1-6 alkyl, halogen, cyano, nitro, amino, amino substituted by mono- or di- C1-6 alkyl, carboxy, formyl, acyl, C1-6 alkoxycarbonyl, carbamoyl, aminocarbonyl substituted by mono- or di- C 1-6 alkyl, C 1-6 thioalkyl, C 1-6 alkylsulfinyl, C 1-6 alkylsulfonyl and acylamino; the term "optionally substituted phenyl" indicates a phenyl optionally substituted by one to three substituents independently selected from the group consisting of C 1-6 alkyl, C 1-6 haloalkyl, heteroalkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 hydroxy-alkenyl , hydroxyC3-6 alkynyl, C1-6 alkoxyC3-6 alkenyl, C1-6 alkoxyC3-6 alkynyl, hydroxy, C1-6 alkoxy, C1-6 haloalkoxy, heteroalkoxy, C3-7 cycloalkyl, C3-7 cycloalkylC1-7 alkyl 6, halogen, cyano, nitro, amino, amino substituted by mono- or di- C1-6 alkyl, carboxy, formyl, acyl, C1-6 alkoxycarbonyl, carbamoyl, aminocarbonyl substituted by mono- or di- C1-6 alkyl, C1-6 thioalkyl, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl and acylamino; the term "optionally substituted heterocyclyl" indicates a heterocyclyl optionally substituted by one to three substituents independently selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, hydroxyC3-6 alkenyl , hydroxyC3-6 alkynyl, C1-6 alkoxyC3-6 alkenyl, C1-6 alkoxyC3-6 alkynyl, hydroxy, C1-6 alkoxy, C1-6 haloalkoxy, heteroalkoxy, C3-7 cycloalkyl, C3-7 cycloalkylC1-7 alkyl 6, halogen, cyano, nitro, amino, amino substituted by mono- or di- C1-6 alkyl, carboxy, formyl, acyl, C1-6 alkoxycarbonyl, carbamoyl, aminocarbonyl substituted by mono- or di- C1-6 alkyl, thioalkyl C1-6, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl and acylamino; the term "optionally substituted heteroaryl" indicates a heteroaryl optionally substituted by one to three substituents independently selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 hydroxy-alkenyl , hydroxyC3-6 alkynyl, C1-6 alkoxyC3-6 alkenyl, C1-6 alkoxyC3-6 alkynyl, hydroxy, C1-6 alkoxy, C1-6 haloalkoxy, heteroalkoxy, C3-7 cycloalkyl, C3-7 cycloalkylC1-7 alkyl 6, halogen, cyano, nitro, amino, amino substituted by mono- or di- C1-6 alkyl, carboxy, formyl, acyl, C1-6 alkoxycarbonyl, carbamoyl, aminocarbonyl substituted by mono- or di- C1-6 alkyl, thioalkyl C1-6, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl and acylamino; the term "heteroalkyl" denotes C1-6 alkyl substituted by one or more substituents independently selected from the group consisting of nitro, hydroxy, cyano, C1-6 alkoxy, formyl, acyl, carboxyl, C1-6 thioalkyl, C1-6 alkylsulfinyl, C1-alkylsulfonyl -6, carbamoyl, amino and amino substituted by mono- or di- C 1-6 alkyl; the term "heteroalkoxy" denotes C1-6 alkoxy substituted by one or more substituents independently selected from the group consisting of nitro, hydroxy, cyano, C1-6 alkoxy, formyl, acyl, carboxyl, C1-6 thioalkyl, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, carbamoyl, amino and amino substituted by mono- or di- C1-6 alkyl; the term "acyl" indicates R-C (O) -, wherein R is C 1-6 alkyl, C 1-6 haloalkyl, C 3-7 cycloalkyl or C 3-7 cycloalkyl; the term "optionally substituted pyrrolidin-1-yl" indicates a pyrrolidin-1-yl optionally substituted by one to three substituents independently selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, heteroalkyl, C2-6 alkenyl, C2- alkynyl 6, hydroxyC3-6 alkenyl, hydroxyC3-6 alkynyl, C1-6 alkoxyC3-6 alkoxy, C1-6 alkoxyC3-6 alkoxy, hydroxy, C1-6 alkoxy, C1-6 haloalkoxy, heteroalkoxy, C3-7 cycloalkyl , C3-7 cycloalkyl C1-6 alkyl, halogen, cyano, nitro, amino, amino substituted by mono- or di- C1-6 alkyl, carboxy, formyl, acyl, C1-6 alkoxycarbonyl, carbamoyl, aminocarbonyl substituted by mono- or di- C 1-6 alkyl, C 1-6 thioalkyl, C 1-6 alkylsulfinyl, C 1-6 alkylsulfonyl and acylamino. |
| priorityDate | 2007-10-01^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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