http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-097199-A1
Outgoing Links
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|---|---|
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| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-52 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D473-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D261-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-50 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D231-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-00 |
| filingDate | 2014-08-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_37350f62fe16bb7b0d5132030ebf49c5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_247f718ac636a9412856abd4df673441 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1f53a440b1e6883eb6c621d67ef2c23f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7614ff3b7a4da4077c2728ab00b22049 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9e4b2edbee91cea10ad9f820baae6dcd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4d5ad1d093414771a20c413b6e00fdd5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cd474acb1ac2addbfe3e7764e6d9f015 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c573a9f34194a9fe4971fd5dffec87b1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_02acd59c7a39115616aa8014e2a35199 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5c2610fae0f5390612f432f96c29967f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e7bbb60e984c736a39dec4544dc7d680 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_543e09b4d92626a9ddf93e558c30c390 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8885aad60e3c7e72b10477d58e94182e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a3cc0f91878003f0899daf7a465a2e3e |
| publicationDate | 2016-02-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-097199-A1 |
| titleOfInvention | RORC2 INHIBITORS AND THEIR METHODS OF USE |
| abstract | Compounds, pharmaceutical compositions, methods for inhibiting the activity of RORg and / or reducing the amount of IL-17 in a subject, and methods for treating various medical disorders using these compounds and pharmaceutical compositions. Useful compounds to treat inflammatory and immune disorders. Claim 1: A compound characterized by formulas (1), (2), (3), (4), (5), (6) or (7), or a pharmaceutically acceptable salt, a metabolite pharmaceutically active, a pharmaceutically acceptable prodrug or a pharmaceutically acceptable solvate thereof, wherein, Y is hydrogen, halo, cyano, C₁₋₃alkyl, C₁₋₃hydroxyalkyl, C₁₋₅alkenyl, C₁₋ ₃haloalkyl, C₁₋₃hydroxyhaloalkyl, C₃₋₆cycloalkyl, C₁₋₃alkoxy or C₁₋₃haloalkoxy; R¹ is hydrogen, C₁₋₆alkyl, C₁₋₆hydroxyalkyl or C₁₋₆haloalkyl; X is a compound selected from the group of formulas (8); R² is C₁₋₆alkyl, C₃₋₈cycloalkyl, C₃₋₈heterocycloalkyl, aryl or heteroaryl, optionally substituted with 1, 2, 3, 4 or 5 substituents independently selected, for each case, from the group consisting of halo, cyano, C₁₋₄alkyl , C₁₋₄haloalkyl, C₁₋₄cianoalkyl, hydroxyl, -OR, C₁₋₄hydroxyalkyl, C₁₋₄hydroxyalkoxy, C₁₋₄hydroxyalkoxyC₁₋₄alkyl, C₁₋₄alkoxy, C₁₋₄alkoxyC₁₋₄alkyl, C₁₋₄alkoxyC₁₋₄alkoxy, C₁₋₄alkoxyC₁₋₄alkoxyC₁₋ ₄alkyl, C₁₋₄haloalkoxy, -NR₂, (R₂N) C₁₋₄alkyl-, C₁₋₄alkylthio, C₁₋₄haloalkylthio, -C (= O) R, -C (= O) OR, -OC (= O) R, - C (= O) NR₂, -N (R) C (= O) R, -CH₂C (= O) R, -CH₂C (= O) OR, -CH₂OC (= O) R, -CH₂C (= O) NR₂ , -CH₂N (R) C (= O) R, -S (= O) ₂R, -S (= O) ₂NR₂, -N (R) S (= O) ₂R, -A and -CH₂A; R is independently selected, for each case, from the group consisting of hydrogen, C₁₋₄alkyl, C₁₋₄haloalkyl, C₁₋₄cianoalkyl, C₁₋₄hydroxyalkyl, C₃₋₈cycloalkyl or C₃₋₈heterocycloalkyl; or where a nitrogen is substituted with two R groups, which can be taken together with the nitrogen atom to which they are attached to form a saturated 4, 5, 6 or 7-membered C-heterocycloalkyl which, when formed, can be optionally substitute with 1, 2 or 3 substituents independently selected from the group consisting of C₁₋₄alkyl, halo, hydroxyl, C₁₋₄hydroxyalkyl, C₁₋₄cianoalkyl, C₁₋₄haloalkyl y = O; A is independently selected, for each case, from the group consisting of C₃₋₈cycloalkyl, C₃₋₈heterocycloalkyl, aryl and heteroaryl, optionally substituted with 1, 2, 3, 4 or 5 substituents independently selected, for each case, from the group consisting in halo, cyano, C₁₋₄alkyl, C₁₋₄haloalkyl, C₁₋₄cianoalkyl, hydroxyl, C₁₋₄hydroxyalkyl, C₁₋₄alkoxy, C₁₋₄alkoxyC₁₋₄alkyl, C₁₋₄haloalkoxy, -NR₂, (R₂N) C₁₋₄alquil-, C₁₋ Qualkylthio, C₁₋₄haloalkylthio, -C (= O) R, -C (= O) OR, -OC (= O) R, -C (= O) NR₂, -N (R) C (= O) R, -CH₂C (= O) R, -CH₂C (= O) OR, -CH₂OC (= O) R, -CH₂C (= O) NR₂, -CH₂N (R) C (= O) R, -S (= O) ₂R, -S (= O) ₂NR₂ and -N (R) S (= O) ₂R; W is a moiety selected from the group of formulas (9), optionally substituted with 1, 2, 3, 4 or 5 substituents independently selected, for each case, from the group consisting of halo, C₁₋₆alkyl, C₁₋₆hydroxyalkyl and C₁₋ Lohaloalkyl; R³ is C₁₋₆alkyl, C₃₋₈cycloalkyl, C₃₋₈heterocycloalkyl, aryl, heteroaryl, -C (= O) R⁴, -C (= O) OR⁴, -C (= O) N (R⁵) ₂ or -S (= O) ₂R⁴, optionally substituted with 1, 2, 3, 4 or 5 substituents independently selected, for each case, from the group consisting of halo, cyano, C₁₋₄alkyl, C₁₋₄haloalkyl, C₁₋₄cianoalkyl, hydroxyl, C₁₋₄hydroxyalkyl , C₁₋₄alkoxy, C₁₋₄alkoxyC₁₋₄alkyl, C₁₋₄haloalkoxy, -NR₂, (R₂N) C₁₋₄alkyl-, C₁₋₄alkylthio, C₁₋₄haloalkylthio, -C (= O) R, -C (= O) OR, -OC (= O) R, -C (= O) NR₂, -N (R) C (= O) R, -CH₂C (= O) R, -CH₂C (= O) OR, -CH₂OC (= O) R, -CH₂C (= O) NR₂, -CH₂N (R) C (= O) R, -S (= O) ₂R, -S (= O) ₂NR₂, -N (R) S (= O) ₂R, -A and -CH₂A; R⁴ is hydrogen, C₁₋₆alkyl, C₃₋₈cycloalkyl, C₃₋₈heterocycloalkyl, C₃₋₈cycloalkylC₁₋₆alkyl, C₃₋₈heterocycloalkylC₁₋₆alkyl, aryl or heteroaryl, optionally substituted with 1, 2, 3, 4 or 5 independently selected substituents, for each case, of the group consisting of halo, cyano, C₁₋₄alkyl, C₁₋₄haloalkyl, C₁₋₄cianoalkyl, hydroxyl, C₁₋₄hydroxyalkyl, C₁₋₄alkoxy, C₁₋₆alkoxyC₁₋₆alkyl, C₁₋₆haloalkoxy, -NR₂, (R₂N) C₁ Qualkyl, C₁₋₆alkylthio, C₁₋₆haloalkylthio, -C (= O) R, -C (= O) OR, -OC (= O) R, -C (= O) NR₂, -N (R) C ( = O) R, -CH₂C (= O) R, -CH₂C (= O) OR, -CH₂OC (= O) R, -CH₂C (= O) NR₂, -CH₂N (R) C (= O) R, - S (= O) ₂R, -S (= O) ₂NR₂, -N (R) S (= O) ₂R, -AY -CH₂A; and R⁵ is independently selected, for each case, from the group consisting of hydrogen, C₁₋₆alkyl, C₃₋₈cycloalkyl, C₃₋₈heterocycloalkyl, C₃₋₈cycloalkylC₁₋₆alkyl, C₃₋₈heterocycloalkylC₁₋₆alkyl, aryl and heteroaryl, optionally substituted with 1, 2, 3, 4 or 5 substituents, independently selected, for each case, from the group consisting of halo, cyano, C₁₋₄alkyl, C₁₋₄haloalkyl, C₁₋₄cianoalkyl, hydroxyl, C₁₋₄hydroxyalkyl, C₁₋₄alkoxy, C₁₋₄alkoxyC₁ Qualkyl, C₁₋₄haloalkoxy, -NR₂, (R₂N) C₁₋₄alkyl-, C₁₋₄alkylthio, C₁₋₄haloalkylthio, -C (= O) R, -C (= O) OR, -OC (= O) R, -C (= O) NR₂, -N (R) C (= O) R, -CH₂C (= O) R, -CH₂C (= O) OR, -CH₂OC (= O) R, -CH₂C (= O) NR₂, -CH₂N (R) C (= O) R, -S (= O) ₂R, -S (= O) ₂NR₂, -N (R) S (= O) ₂R, -A and -CH₂A; or wherein a nitrogen is substituted with two R⁵ groups that can be taken together with the nitrogen atom to which they are attached to form a saturated 4, 5, 6 or 7-membered heterocycloalkyl which, when formed, can optionally be substituted with 1, 2 or 3 substituents independently selected from the group consisting of C₁₋₄alkyl, halo, hydroxyl, C₁₋₄hydroxyalkyl, C₁₋₄haloalkyl y = O. |
| priorityDate | 2013-08-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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