http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-096902-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_d9af4d89807e0db8298692dffeabf875 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K2300-00 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D251-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D251-48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-53 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-10 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-53 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-04 |
| filingDate | 2014-07-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_52b61478bfad17785095557a62288838 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b5ffe593d6d93df05b3817e502ee8be4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2dd2624213d15dc12909ab924d170bca http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c57d77956197093163f1071d18b6d013 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f0154a2672a10d10bf38a9db4574eaeb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d4750a43b21b2bc965371b3876c15dee |
| publicationDate | 2016-02-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-096902-A1 |
| titleOfInvention | DERIVATIVES OF TRIAZINE AND PYRIMIDINE AS INHIBITORS OF IDH1 AND / OR IDH2 MUTANTS AND THEIR USE IN THE TREATMENT OF CANCER |
| abstract | Compounds useful for the treatment of cancer and their use in the treatment of cancer are provided. Claim 1: A compound having the formula (1), or a pharmaceutically acceptable salt or hydrate thereof, wherein: ring A is an optionally substituted 5-6 membered monocyclic aryl or monocyclic heteroaryl; X is N, CH or C-halo; R¹, R³, R⁴ and R⁶ are each independently selected from hydrogen, C₁₋₄ alkyl, C₁₋₄ haloalkyl, -O-C₁₋₄ alkyl and CN, wherein each of said alkyl moieties of R¹, R³, R⁴ and R⁶ is each independently substituted optionally by -OH, -NH₂, -CN, -O-C₁₋₄ alkyl, -NH (C₁₋₄ alkyl) or -N (C₁₋₄ alkyl) ₂; each R² and R⁵ is independently selected from: - (C₁₋₆ alkyl), - (C₁₋₆ alkyl) -C (O) -NH₂, - (C₁₋₆ alkyl) -CO₂H, - (Cque alkenyl or alkynyl ), - (C₁₋₆ alkylene) -N (R⁶) - (C₁₋₆ alkylene) -O- (C₁₋₆ alkyl), - (C₁₋₆ alkylene) -N (R⁶) - (C₀₋₆ alkylene) -Q, - (C₁₋₆ alkylene) -N (R⁶) (R⁶), - (C₁₋₆ alkylene) -N (R⁶) -S (O) ₁₋₂- (C₁₋₆ alkyl), - (alkylene C₁₋₆) -N (R⁶) -S (O) ₁₋₂- (C₀₋₆ alkyl) -Q, - (C₁₋₆ alkylene) -S (O) ₁₋₂-N (R⁶) (R⁶) , - (C₁₋₄ alkylene) -S (O) ₁₋₂-N (R⁶) - (C₁₋₆ alkylene) -Q, -C (O) N (R⁶) - (C₁₋₆ alkylene) -C ( O) - (C₀₋₆ alkylene) -O- (C₁₋₆ alkyl), -C (O) N (R⁶) - (C₁₋₆ alkylene) -C (O) - (C₀₋₆ alkylene) -O- (C₀₋₆ alkylene) -Q, - (C₁₋₆ alkylene) -OC (O) - (C₁₋₆ alkyl), - (C₁₋₆ alkylene) -OC (O) - (C₀₋₆ alkyl) -Q , - (C₁₋₆ alkylene) -O- (C₁₋₆ alkyl), - (C₁₋₆ alkylene) -O- (C₁₋₆ alkylene) -Q, - (C₀₋₆ alkylene) -C (O) - (C₀₋₆ alkylene) -O- (C₁₋₆ alkyl), - (C₀₋₆ alkylene) -C (O) - (C₀₋₆ alkylene ) -O- (C₁₋₆ alkylene) -Q, - (C₁₋₆ alkylene) -OC (O) - (C₁₋₆ alkyl), - (C₁₋₆ alkylene) -OC (O) - (C₀₋ alkylene ₆) -Q, - (C₀₋₆ alkylene) -C (O) N (R⁶) - (C₁₋₆ alkyl), - (C₀₋₆ alkylene) -C (O) N (R⁶) - (C₀₋ alkylene ₆) -Q, - (C₁₋₆ alkylene) -N (R⁶) C (O) - (C₁₋₆ alkyl), - (C₁₋₆ alkylene) -N (R⁶) C (O) - (C₀₋ alkylene ₆) -Q, - (C₀₋₆ alkylene) -S (O) ₀₋₂- (C₁₋₆ alkyl), - (C₀₋₆ alkylene) -S (O) ₀₋₂- (C₀₋₆ alkylene) -Q, - (C₁₋₆ alkylene) -N (R⁶) -C (O) -N (R⁶) - (C₁₋₆ alkyl), - (C₀₋₆ alkylene) -Q, - (C₀₋₆ alkylene) -C (O) - (C₁₋₆ alkyl), - (C₀₋₆ alkylene) -C (O) - (C₀₋₆ alkylene) -Q, where: any alkyl or alkylene moiety present in R² and R⁵ is optionally substituted by one or more -OH, -O (C₁₋₄ alkyl), -CO₂H or halo; any terminal methyl moiety present in R² and R⁵ is optionally replaced by -CH₂OH, CF₃, -CH₂F, -CH₂Cl, C (O) CH₃, C (O) CF₃, CN or CO₂H; R⁷ and R⁸ are each independently selected from hydrogen and C₁₋₆ alkyl; and Q is selected from aryl, heteroaryl, carbocyclyl and heterocyclyl, any of which is optionally substituted; wherein R¹ and R³ are optionally taken together with the carbon atom to which they are attached to form C (= O); or R⁴ and R⁶ are optionally taken together with the carbon atom to which they are attached to form C (= O); or R¹ and R² are optionally taken together to form an optionally substituted carbocyclyl or optionally substituted heterocyclyl; or R⁴ and R⁵ are optionally taken together to form an optionally substituted carbocyclyl, optionally substituted heterocyclyl, an optionally substituted aryl or an optionally substituted heteroaryl; wherein: (i) when X is N and A is optionally substituted phenyl, then (a) neither N (R⁷) C (R⁴) (R⁵) (R⁶) nor N (R⁸) C (R¹) (R²) (R³ ) is NHCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, 4 - [[2- (2- (2-aminoethoxy) ethoxy] ethyl] amino] and (b) N (R⁷) C (R⁴) (R⁵) (R⁶) and N (R⁸) C (R¹ ) (R²) (R³) are not both NHEt, NH (n-propyl), NH (n-butyl), NH (n-docecyl), NH - [(4-methoxyphenyl) methyl], NHCH₂CH₂CHO, NHCH₂CH₂OCH₃, NHCH₂CH₂OH, NHCH₂CH (OH) CH₃, NHCH₂CH₂OC (O) phenyl, NHCH₂CH₂CH₂OH, NHCH₂CH₂CH₂N (CH₃) phenyl, NHCH₂C (O) OCH₃, NHCH₂C (O) OCH₂CH₃, NHCH₂-phenyl, NHCH (CH₃) CH₂CH₃ or NHCH₂CH₂OC (II) ) when X is CH or C-Cl and A is phenyl optionally substituted by F, Cl or SO₂CH₃, then neither N (R⁷) C (R⁴) (R⁵) (R⁶) nor N (R⁸) C (R¹) (R²) (R³) is N (CH₃) CH₂C (O) NH-i-propyl, NHCH (CH₃) (CH₂) ₃N (CH₂CH₃) ₂, NHCH₂CH₂OH, NHCH₂CH₂OCH₃, NHCH₂CH₂OSO₃H, NHCH₂CH₂CH₂OCH₂CH₂O-phenyl, NHCH₂CH₂CH₂OH₂CH NHCH₂OH , NHCH₂CH (OH) CH₃, N (CH₂CH₃) ₂, NH-i-propyl, NHCH₂CH₂NHC (O) OCH₃, NHCH₂CH₂NHC (O) CH₃, NHCH₂CH₂NH₂ or NHCH₂-phenyl; (iii) when X is CH and A is optionally substituted pyridyl , then neither N (R⁷) C (R⁴) (R⁵) (R⁶) nor N (R⁸) C (R¹) (R²) (R³) is NHCH₂-phenyl, NHCH₂- (2,4-difluorophenyl), N (CH₃ ) CH₂CH₂C (O) OH, NHCH₂CH₂C (O) OH, NHCH₂CH₂C (O) OCH₂CH₃, NHCH₂CH₂C (O) Ot-butyl, NHCH₂CH₂C (O) NH₂, NHCH₂CH₂-phenyl, NHCH₂CH₂OH, NHCH₂CH₂NH₂, NHCH₂CH₂N (CH₃CH₂N) (iv) when X is CH and A is optionally substituted 1-imidazolyl, optionally substituted 1-pyrazolyl, then neither N (R⁷) C (R⁴) (R⁵) (R⁶) nor N (R⁸) C (R¹) (R²) (R³) is NH (CH₂) ₇CH₃, NHCH₂- (o-chloro-phenyl) or NHCH₂CH₂OH; (v) when X is N and A is an optionally substituted pyridyl, then (A) or N (R⁷) C (R⁴) (R⁵) (R⁶) or N (R⁸) C (R¹) (R²) (R³) is NHC (O) - [2-chloro-4- (methylsulfonyl)], N (CH₃) ₂, NHCH₂CH₂OCH₂CH₂SO₂CH₂CH₂Cl or NHCH₂CH₂SO₂CH₂CH₂Cl, (B) N (R⁷) C (R⁴) (R⁵) (R⁶) and N (R⁸) C (R¹) (R²) (R³) are not both NHC (O) C (CH₃) ₃, NHC (O) CH = CH₂, NHC (O) C (CH₃) = CH₂, NHCH₂CH₂OH, NH-cyclohexyl, NHCH₂-phenyl , NHC (O) phenyl, NHC (O) (CH₂) ₅NH₂, NHC (O) OCH₃, NHC (O) CH₃ and NHC (O) NH-phenyl optionally substituted and (C) when N (R⁷) C (R⁴) (R⁵) (R⁶) is NHC (CH₃) ₃, then N (R⁸) C (R¹) (R²) (R³) is not NHCH₂-phenyl or NH-CH₂CH₃; (vi) when X is N and A is an optionally substituted heteroaryl, then N (R⁷) C (R⁴) (R⁵) (R⁶) and N (R⁸) C (R¹) (R²) (R³) are not both N ( CH₂CH₃) ₂, NHCH₂CH₂-i-propyl, NHCH₂CH (CH₃) ₂ and NHC (O) CH₃, (vii) when X is CH and A is unsubstituted 2-pyridinyl, then the ring formed by R⁴ and R⁵ is not 5-methyl -1H- pyrazol-3-yl, (viii) when A is optionally substituted 1-pyrazolyl, then neither N (R⁷) C (R⁴) (R⁵) (R⁶) nor N (R⁸) C (R¹) (R²) ( R³) is N (CH₃) ₂, NHCH₃, NHAc, NH-isopropyl, NHCH₂CH₃, NHCH₂CH₂SO₃H or N (CH₂CH₃) ₂, (ix) when X is N and A is optionally substituted phenyl, thienyl or pyridinyl, then neither N (R⁷ ) C (R⁴) (R⁵) (R⁶) or N (R⁸) C (R¹) (R²) (R³) is NH-cyclohexyl-C (O) NHCH₂R, where R is phenyl or pyridinyl which is substituted by one or more than OCF₃, OCH₃, chlorine or CF₃, (x) when X is N, A is an optionally substituted phenyl and R⁴ and R⁵ form an optionally substituted phenyl, then N (R⁸) C (R¹) (R²) (R ³) is not NHCH₂ (4-fluorophenyl), NHCH₂CO₂H, NHCH₂C (O) Cl, NHCH (CO₂H) (CH₂SCH₂ phenyl) or NHCH₂C (O) NHC (O) NHR or NHCH₂C (O) NHC (S) NHR, where R is optionally substituted phenyl or naphthyl, (xi) when X is N, A is an oxadiazole substituted by an optionally substituted pyridinyl, then R⁴ and R⁵ do not form an optionally substituted phenyl, (xii) when A is 1-pyre |
| priorityDate | 2013-07-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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