http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-102165-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_00cf135003c69ae281b696d3bc73e0c9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_116c851e729089df9a427027272fa290 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D493-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-18 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5517 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 |
| filingDate | 2015-10-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6802cfe61f504ae4c9120498dc6536e1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_632f5f0ddd9eff10ca31b9d3b4afaaa8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_193d026e15e6e2fa230b33a291f326be http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_07ff0a2ee3973f01d2bec2820b09bf7e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_144dcdef2fdc413f446b683d9c184564 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_59130cb041096d8dfa9bca2bf07fff00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b245a2b53f3a7b3a0a7ae5a52fdf9645 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6452ff9ae01ad20daca58cadfb4b30c0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_83e17c9cab56aeddea03a15abe1526c9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_57a400df420db85d8627edfdfbd6103a |
| publicationDate | 2017-02-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-102165-A1 |
| titleOfInvention | IMIDAZOL PENTACYCLIC DERIVATIVES FUSED AS MODULATORS OF THE TNFa FUNCTION |
| abstract | A series of fused pentacyclic imidazole derivatives, which are potent modulators of human TNFa activity are consequently beneficial in the treatment and / or prevention of different human diseases, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; eye disorders; and oncological disorders. In particular, 6,7-dihydro-7,14-methanobenzimidazo [1,2-b] [2,5] benzodiazocin-5 (14H) -one derivatives and analogs thereof. Claim 1: A compound characterized in that it is of formula (1) or an N-oxide thereof, or a pharmaceutically acceptable salt thereof, wherein -XQ- represents -O-, -OC (O) -, -C (O) -O-, -OC (CH-CN) -, -S-, -SO-, -SO₂-, -N (Rᵍ) -, -N (Rᶠ) -CO-, -CO-N (Rᶠ) -, -N (Rᶠ) -SO₂-, -SO₂-N (Rᶠ) -, -S (O) (NRᶠ) -, -CH₂-CH₂-, -O-CH₂-, -CH₂-O-, -S-CH₂ -, -SO-CH₂-, -SO₂-CH₂-, CH₂-S-, -CH₂-SO-, -CH₂-SO₂-, -N (Rᵍ) -CH₂-, -CH₂-N (Rᵍ) -, - S (O) (NRᶠ) -CH₂-, -CH₂-S (O) (NRᶠ) -, -N (Rᶠ) -C (S) -, -N = S (O) (CH₃) -, -OC ( = CH₂) - or -S (= N-CN) -, any of whose groups may optionally be substituted with one or more substituents; Z represents methylene; E represents a fused heteroaromatic ring system that can be selected from the groups of formula (2), (3) and (4), where the asterisk (*) represents the binding site of E to the rest of the molecule; R¹ represents hydrogen, halogen, cyano, trifluoromethyl, trifluoromethoxy, -ORᵃ, -SRᵃ, -SORᵃ, -SO₂Rᵃ, -NRᵇRᶜ, -NRᶜCORᵈ, -NRᶜCO₂Rᵈ, -NHCONRᵇRᶜ, -NRᶜSO₂Rᵉ, -CORᵈ, -CO₂RᵈR, -CO₂RᵈR -CONR , or -S (O) (N-Rᵇ) Rᵉ; or C₁₋₆ alkyl, C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, aryl, aryl-C₁₋₆ alkyl, C₃₋₇ heterocycloalkyl, C₃₋₇ heterocycloalkenyl, heteroaryl, heteroaryl-C₁₋₆ alkyl, C₃₋₇ heterocycloalkyl-C₁ ₋₆ alkyl aryl, C₃₋₇ cycloalkyl heteroaryl, C₃₋₇ cycloalkyl-C₁₋₆ alkyl heteroaryl, C₄₋₇ cycloalkenyl heteroaryl, C₄₋₉ bicycloalkyl heteroaryl, C₃₋₇ heterocycloalkyl heteroaryl, C₃₋₇ heterocycloalkyl -C₁₋₆ alkyl heteroaryl, C₃₋₇ heterocycloalkenyl heteroaryl, C₄₋₉ heterobicycloalkyl heteroaryl- or C₄₋₉ spiroheterocycloalkyl heteroaryl, any of whose groups may optionally be substituted with one or more substituents; or R¹ represents C₃₋₇ heterocycloalkenyl aryl, wherein said group may optionally be substituted with one or more substituents; R² represents hydrogen, halogen, cyano, nitro, hydroxy, trifluoromethyl, trifluoromethoxy or -ORᵃ or C₁₋₆ alkyl optionally substituted with one or more substituents; R³ and R⁴ independently represent hydrogen, halogen or trifluoromethyl; or C₁₋₆ alkyl, optionally substituted with one or more substituents; R⁵ and R⁸ independently represent hydrogen, halogen, hydroxy, cyano, trifluoromethyl, difluoromethoxy, trifluoromethoxy, -ORᵃ, or C₁₋₆ alkylsulfonyl; or C₁₋₆ alkyl, optionally substituted with one or more substituents; R⁶ and R⁷ independently represent hydrogen, halogen, trifluoromethyl, C₁₋₆ alkyl or C₁₋₆ alkoxy; R² represents hydrogen or C₁₋₆ alkyl; Rᵃ represents C₁₋₆ alkyl, C₃₋₇ cycloalkyl, C₃₋₇ heterocycloalkyl, aryl, aryl-C₁₋₆ alkyl, heteroaryl or heteroaryl-C₁₋₆ alkyl, any of whose groups may optionally be substituted with one or more substituents; Rᵇ and Rᶜ independently represent hydrogen or trifluoromethyl; or C₁₋₆ alkyl, C₃₋₇ cycloalkyl, C₃₋₇ cycloalkyl-C₁₋₆ alkyl, aryl, aryl-C₁₋₆ alkyl, C₃₋₇ heterocycloalkyl, C₃₋₇ heterocycloalkyl-C₁₋₆ alkyl, heteroaryl or heteroaryl-C₁ ₋₆ alkyl, any of whose groups may optionally be substituted with one or more substituents; or Rᵇ and Rᶜ, when taken together with the nitrogen atom to which both are attached, represent a heterocyclic unit that can be selected from azetidin-1-yl, pyrrolidin-1-yl, oxazolidin-3-yl, isoxazolidin-2 -ilo, thiazolidin-3-yl, isothiazolidin-2-yl, piperidin-1-yl, morpholin-4-yl, thiomorpholin-4-yl, piperazin-1-yl, homopiperidin-1-yl, homomorpholin-4-yl , homopiperazin-1-yl, (imino) (oxo) thiazinan-4-yl, (oxo) thiazinan-4-yl and (dioxo) thiazinan-4-yl, any of whose groups may optionally be substituted with one or more substituents ; Rᵈ represents hydrogen; or C₁₋₆ alkyl, C₃₋₇ cycloalkyl, aryl, C₃₋₇ heterocycloalkyl or heteroaryl, any of whose groups may optionally be substituted with one or more substituents; Rᵉ represents C₁₋₆ alkyl, aryl or heteroaryl, any of whose groups may optionally be substituted with one or more substituents; Rᶠ represents hydrogen; or C₁₋₆ alkyl, C₃₋₇ cycloalkyl, or C₃₋₇ heterocycloalkyl, any of whose groups may optionally be substituted with one or more substituents; and Rᵍ represents hydrogen; or C₁₋₆ alkyl, C₃₋₇ cycloalkyl, C₃₋₇ heterocycloalkyl, -CO-C₁₋₆ alkyl, or -SO₂-C₁₋₆ alkyl, any of whose groups may optionally be substituted with one or more substituents; or Rᵍ represents -CO-C₃₋₇ heterocycloalkyl, -SO₂-C₃₋₇ cycloalkyl, -SO₂-C₃₋₇ heterocycloalkyl, -SO₂-aryl or -SO₂-heteroaryl, any of whose groups may optionally be substituted with one or more substituents ; or Rᵍ represents heteroaryl or C₂₋₆ alkoxycarbonyl, any of whose groups may optionally be substituted with one or more substituents. |
| priorityDate | 2014-10-03-04:00^^<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: 47.