http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-094232-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_dcce39a20bef16c3f04497659caba40f |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-20 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P5-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-551 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D513-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-00 |
| filingDate | 2013-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_54108cafaf74b5bc8f829e2f050372de http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_839dd69017a541155a7a1a34eb225f28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fe4693efd65ba5b9101bbbc0137c67cb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c53882b9cf928e38081c254419d88e4b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_672914a788806d480261f1719da4b515 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9f10472627410528e44872b376b7db36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_06ca651e110bdb6e16ad73354e2759d3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d0d8a243f72b61a54bd1de11fb86f1e7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b8c5538d9bac9f417945cadb7f675cb4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_957e50ca9bd7ea1f188ac374985070d5 |
| publicationDate | 2015-07-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-094232-A1 |
| titleOfInvention | HETEROCICLIC MODULATORS OF NUCLEAR HORMONE RECEPTORS |
| abstract | The compounds herein are useful for the treatment of immunological and oncological conditions. Claim 1: A compound characterized in that it is represented by formula (1), or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein: ring 1 is heterocyclic or heteroaromatic; X is N, N (R⁴), C (R⁴), C (R⁴) (R⁴), S or O; Y is N, N (R⁴), C (R⁴), S, O or C (= O); Z is N (R⁴), C (R⁴) C (R⁴) or C (R⁴); A is, N (R³), C (R³) (R³) or C (= O); G and J are independently S, S (O), S (O) ₂, O, C (R¹) (R²), N (R³) or C (= O) with the proviso that at least one of G and J is C (R¹) (R²) or C (= O); E is N (R⁴), S, S (O), S (O) ₂, O, C (R¹) (R²), or C (= O); L is N (R⁵), C (R⁵) (R⁵) or C (R⁵) (R⁵); or L is C (R⁵) or C (R⁵) and J is C (R¹) or N; M and Q are independently N, C or CH; with the proviso that X, Y, and Z are not both heteroatoms at the same time; no more than three of A, E, G, J, L, M and Q are heteroatoms; M and Q are not both N; adjacent atoms do not form S-S, S-O, O-O or -C (= O) -C (= O) bonds; at least one of X, Y and Z is C (R⁴) or C (= O); when Q is N, X is not S or O; when J is S, O, S (O) or N (R³), L is not N (R⁵); R¹ and R², in each instance, is independently -H, CF₃, CN, -C (= O) NH₂, OH, optionally substituted C₁₋₆ alkyl, optionally substituted C₃₋₆ cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocycle; or R¹ and R², together with the carbon to which they are attached, form an optionally substituted C₃₋₆ carbocyclic ring spiro to ring 2 or an optionally substituted heterocyclic ring spiro to ring 2; R³ is independently -H, CF₃, CN, OH, -NRᵃRᵇ, optionally substituted C₁₋₆ alkyl, optionally substituted C₂₋₆ alkenyl, optionally substituted C₂₋₆ alkynyl, optionally substituted aryl, optionally substituted C₃₋₆ cycloalkyl, heteroaryl optionally substituted, optionally substituted heterocycle, or optionally substituted benzyl; R³ is independently -H, optionally substituted C₁₋₆ alkyl, optionally substituted C₂₋₆ alkenyl, optionally substituted C₂₋₆ alkynyl, optionally substituted aryl, optionally substituted C₃₋₆ cycloalkyl, optionally substituted heteroaryl, optionally substituted heterocycle, or benzyl optionally substituted; R⁴ is independently H, -CF₃, -CN, -OH, -NRᵃRᵇ, optionally substituted C₁₋₆ alkyl, optionally substituted C₂₋₆ alkenyl, optionally substituted C₂₋₆ alkynyl, optionally substituted C₁₋₆ alkoxy, optionally substituted aryl , optionally substituted C₃₋₆ cycloalkyl, optionally substituted heteroaryl, or optionally substituted heterocycle; R⁴ is independently -H, optionally substituted C₁₋₈ alkyl, optionally substituted C₂₋₆ alkenyl, optionally substituted C₂₋₆ alkynyl, optionally substituted C₃₋₆ cycloalkyl, optionally substituted heterocycle, optionally substituted aryl, or optionally substituted heteroaryl; with the proviso that R⁴ is not optionally substituted bencisoxazolyl, optionally substituted isobenzazolyl, optionally substituted quinazolinyl, optionally substituted isoquinolinyl or optionally substituted phthalazinyl; R⁵ is independently -H, OH, F, CF₃, CN, optionally substituted C₁₋₆ alkyl, optionally substituted C₂₋₆ alkenyl, optionally substituted C₂₋₆ alkynyl, optionally substituted C₃₋₆ cycloalkyl, - (CH₂) ₙ- optionally substituted aryl, - (CH₂) ₙ-optionally substituted heterocycle, or - (CH₂) ₙ-optionally substituted heteroaryl; or both R⁵, together with the carbon to which they are attached, form a spirocyclic carbocyclic ring; R⁵ is -R⁵ᵃ-R⁵ᵇ-R⁵ᶜ where R⁵ᵃ binds to the ring and R⁵ᵃ is optionally substituted phenyl or optionally substituted heteroaryl; R⁵ᵇ is a union or -C (= O) N (H) where -C (= O) joins R⁵ᵃ; and R⁵ᶜ is optionally substituted isoxazolyl, optionally substituted oxazolyl, optionally substituted phenyl, optionally substituted pyrazolyl, optionally substituted pyridazinyl, optionally substituted pyridinyl, optionally substituted pyrimidinyl, optionally substituted pyrimidinyl [2,3-b], tetrazolyl, 1,3,5 optionally substituted thiadiazolyl, or 1,2,4-triazolyl; Rᵃ and Rᵇ are independently H and optionally substituted C₁₋₆ alkyl; and n, in each instance, is independently 0, 1, 2 or 3; with the proviso that when the compound is of formula (2) then R⁵ is not unsubstituted phenyl or phenyl substituted with COOH, Cl, F, OH, NO₂ or two OCH₃; with the proviso that when M and Q are both CH or M and Q are both C and ring 1 contains two nitrogen atoms, ring 2 is not a residue of formula (3) or (4); with the proviso that no more than one of X, Y and Z is substituted with phenyl; and with the proviso that the compound is not of formula (5) or (6) where R¹ and R² are independently H or CH₃; R⁴ is H, optionally substituted C₁₋₈ alkyl, -CH₂C (O) OCH₂CH₃, optionally substituted C₃₋₈ cycloalkyl, optionally substituted benzyl, optionally substituted pyridinyl, optionally substituted pyrimidinyl, the remainder of formula (7) or the remainder of formula ( 8). |
| priorityDate | 2012-12-21-04:00^^<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: 43.