http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2645973-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cf32b60391b469c41e86c353437f5751 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4184 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-454 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4545 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-553 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-551 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-65583 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D411-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-14 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 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 |
| filingDate | 2013-06-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2017-12-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f72c8da2514dfc703057a46646517008 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c6eb0f69b91b13765ebdbfb9b18d7115 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_da9f52106beca78a12805d8db974d7ba http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5bf748e923951840aa228f2dee76b7a7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dd7553cb4a845745d7c64d1fea820374 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4bbb28718a921c9c8ddd42deac1da19b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a49f9c64e0a4fac2aa749e0fe2334536 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_04245dd2f881f4558dd769f4c0a9d2b0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4c6d3ee3737a83493625f4355ef7dc1c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f09b510d20f5c321fdaa6509176ddfa5 |
| publicationDate | 2017-12-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2645973-T3 |
| titleOfInvention | Compounds and compositions to modulate EGFR activity |
| abstract | A compound of the formula (I) or a tautomer thereof, ** Formula ** wherein Ring A is a 6-10 membered monocyclic or bicyclic aryl; a 5-10 membered heteroaryl comprising 1-4 heteroatoms selected from N, O and S, or a 4-12 membered monocyclic or bicyclic heterocyclyl comprising 1-4 heteroatoms selected from N, O and S, and optionally substituted with oxo; Ring B is phenyl; a 5-6 membered heteroaryl comprising 1- 3 heteroatoms selected from N, O and S, or a 5-6 membered heterocyclyl comprising 1- 2 heteroatoms selected from N, O and S, and optionally substituted by oxo; E is NH or CH2; R1, and R1 'are independently hydrogen; halo; cyano; C1-6 alkyl; C1-6 haloalkyl, 5-6 membered heteroaryl comprising 1-4 heteroatoms selected from N, O and S; phenyl, 5-6 membered heterocyclyl comprising 1- 2 heteroatoms selected from N, O, S and P, and optionally substituted by oxo; -X1-C (O) OR3; - X1-O-C (O) R3; -X1-C (O) R3; -X1-C (O) NR4R5; -X1-C (O) NR4-X3-C (O) OR3; -X1-C (O) NR4-X3-S (O) 0-2R6; -X1-NR4R5; -X1NR4- X2-C (O) R3; -X1-NR4-X2-C (O) OR3; -X1-NR4-X2-C (O) NR4R5; -X1-NR4-X3-S (O) 0-2R6; -X1-NR4S (O) 2R6; -X1-OS (O) 2R6; -X1- OR3; -X1-O-X4-OR3; -X1-O-X4-S (O) 0-2R6; -X1-O-X4-NR4R5; -X1-S (O) 0-2R6; -X1-S (O) 0-2-X3-NR4R5; -X1-C (O) NR4-X3- P (O) R6aR6b; -X1-NR4-X1-P (O) R6aR6b; -X1-O-X1-P (O) R6aR6b; -X1-P (O) R6a-X1-NR4R5; -X1-P (O) R6aR6b or -X1-S (O) 2NR4R5; wherein each phenyl, heteroaryl, or heterocyclyl in R 1 is substituted or unsubstituted by 1- 3 groups selected from OH, halo, C 1-6 alkyl, C 1-6 haloalkyl and C 1-6 haloalkoxy; R2 is selected from hydrogen; halo; cyano; C1-6 alkyl; C1-6haloalkyl; 5-6 membered heteroaryl comprising 1-4 heteroatoms selected from N, O and S; phenyl, 5-6 membered heterocyclyl comprising 1-2 heteroatoms selected from N, O, S and P, and optionally substituted by oxo; - X1-C (O) OR3; -X1-O-C (O) R3; -X1- C (O) R3; -X1-C (O) NR4R5; -X1-C (O) NR4-X3-C (O) OR3; -X1-C (O) NR4-X3-S (O) 0-2R6; -X1-NR4R5; -X1NR4-X2-C (O) R3; -X1- NR4-X2-C (O) OR3; -X1-NR4-X2-C (O) NR4R5; -X1-NR4-X3-S (O) 0-2R6; -X1-NR4S (O) 2R6; -X1-OS (O) 2R6; -X1-OR3; -X1-O-X4- OR3; -X1-O-X4-S (O) 0-2R6; -X1-O-X4-NR4R5; -X1-S (O) 0-2R6; -X1-S (O) 0-2-X3-NR4R5; -X1-C (O) NR4-X3-P (O) R6aR6b; -X1- NR4-X1-P (O) R6aR6b; -X1-O-X1-P (O) R6aR6b; -X1-P (O) R6a-X1-NR4R5; -X1-P (O) R6aR6b; -X1-S (O) 2NR4R5 and ((4- acetylpiperazin-1-yl) methyl); wherein each phenyl heteroaryl, or heterocyclyl R2 is substituted or unsubstituted by 1- 3 groups selected from OH, halo, C1-6 alkyl, C1-6 haloalkyl and C1-6 haloalkoxy; R3, R4 and R5 are independently hydrogen, C1-6alkyl or C1-6haloalkyl, or in which R4 and R5 together with N in NR4R5 can form a 4-7 membered ring containing 1- 2 heteroatoms selected from N, O, S and P, and optionally substituted with 1- 4 R7 groups; R6 is C1-6 alkyl or C1-6 haloalkyl; R6a and R6b are independently hydroxyl, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, 6- or 10-membered monocyclic or bicyclic aryl; a 5-10 membered heteroaryl comprising 1-4 heteroatoms selected from N, O and S, or a 4-12 membered monocyclic or bicyclic heterocyclyl comprising 1-4 heteroatoms selected from N, O and S, and optionally substituted with oxo; Z is ** Formula ** where Y is O or NR19; R8 is ** Formula ** R9 and R10 are independently hydrogen, halo, C1-6 alkyl, C1-6 haloalkyl, OH, cyano, C1-6 alkoxy, C1-6 haloalkoxy; R11a, R11b, R11c, R11d, R11e, R11f, R11g, R11h, R11i, R11j, R11k and R11l are independently hydrogen, C1-6 alkyl or C1-6 haloalkyl; R12 and R13 are independently hydrogen, halo, cyano, C1-6 alkyl or C1-6 haloalkyl; R14 and R15 are independently hydrogen, C1-6 alkyl, -L1- R23, - (CRaRb) 2- 3-Rc or -L2-Rd; or R14 and R15 together with N in NR4R5 can form a 4-7 membered ring containing 1- 2 heteroatoms selected from N, O, S and P, and optionally substituted with 1- 4 R18 groups; R16 and R17 are independently hydrogen or C1-6 alkyl; or R16 and R17 together with the carbon to which they are attached can form a C3-6 cycloalkyl; X1 and X2 are independently a bond or C1-6 alkyl; X3 is C1-6 alkyl; X4 is C2-6 alkyl; R19 is hydrogen, C1-6 alkyl, COR20, COOR20, CONR20R21 or S (O) 2R20; R20 is C1-6 alkyl or C1-6 haloalkyl or cycloalkyl; R21 is hydrogen or C1-6 alkyl; or R20 and R21 together with N in NR20R21 can form a 4-7 membered ring containing 1- 2 heteroatoms selected from N, O, S, P and optionally substituted by 1- 4 R22 groups; R7, R18 and R22 are independently oxo, halo, hydroxyl, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy or C1-6 haloalkoxy; R23 is independently C3-7cycloalkyl, or a 4-10 membered heterocyclyl comprising 1-3 heteroatoms selected from N, O and S, and is optionally substituted with oxo, and R23 is substituted or unsubstituted by C1-6alkyl, C1- 6haloalkyl, - L3- Re or L4- Rf; Rc and Re are independently halo, cyano, hydroxyl, - OR24, - NRR25, - NR- CO2R24, - NR- SO2- R26, - NR- COR26, - NR- C (O) - NRR25, -OC (O) - NRR25, or C1-6 alkyl substituted by halo, C1-6 alkoxy, hydroxyl or cyano; Rd and Rf are independently - SO2NRR25, - CONRR25, - C (O) OR24, - SO2R26 or C (O) R26; R24 is C1-6 alkyl, C1- 6haloalkyl, -L2- R23a or - (CRaRb) 2- 3- N (RaRb) 2; R25 is hydrogen, C1-6 alkyl, C1- 6haloalkyl, -L2- R23b or - (CR2) 2- 3- N (RaRb) 2; R26 is C1-6 alkyl, C1- 6haloalkyl, -L2- R23c or - (CRaRb) 1- 3- N (RaRb) 2; R23a, R23b and R23c are independently selected from R23; R, Ra and Rb are independently hydrogen or C1-6 alkyl; L1, L2, L3 and L4 are independently a bond or - (CRaRb) 1- 3; and n and m are independently 1-3; and p and q are 1-4; or a pharmaceutically acceptable salt thereof. |
| priorityDate | 2012-06-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 1422.