http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2886587-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_73e0d5808f34f512649e277bd216a344 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-53 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4985 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D495-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4985 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D495-04 |
| filingDate | 2017-04-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2021-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1b60b30cfbd83bb763cbeb9bb3bdb8ca http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dbd5b6befa473eeefb6dc2ae2254466b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0ff4cadae9f07f8e8eaddb5c063d8269 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f27e142e15fc1c490636eff80be3554c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b877cb2ac93debecf76abfc164b22bce http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_29cc510d87c0dd3c5c5eedce4e0a6a46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b4b6ac811c1605c03d02f9133e94b386 |
| publicationDate | 2021-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2886587-T3 |
| titleOfInvention | Heterocyclic compounds as RET kinase inhibitors |
| abstract | A compound, or a pharmaceutically acceptable salt, hydrate or solvate thereof, having the structural formula shown below: **(See Formula)** where: HET is selected from one of the following: **(See formula)** where **(See formula)** denotes the junction point; R1 is selected from hydrogen, (1-4C)haloalkyl, (1-4C)haloalkoxy, and a group of the formula: -L-Y-Q where: L is absent or is (1-5C)alkylene optionally substituted with one or more selected substituents (1-2C)alkyl or oxo; Y is absent or is O, S, SO, SO2, N(Ra), C(O), C(O)O, OC(O), C(O)N(Ra), N(Ra)C(O ), N(Ra)C(O)N(Rb), N(Ra)C(O)O, OC(O)N(Ra), S(O)2N(Ra) or N(Ra)SO2, in where Ra and Rb are each independently selected from hydrogen or (1-4C)alkyl; and Q is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, aryl, (3-10C)cycloalkyl, (3-10C)cycloalkenyl, heteroaryl, or heterocyclyl; wherein Q is optionally substituted with one or more substituent groups independently selected from (1-4C)alkyl, halo, (1-4C)haloalkyl, (1-4C)haloalkoxy, amino, (1-4C)aminoalkyl, cyano, hydroxy , carboxy, carbamoyl, sulfamoyl, mercapto, ureido, NRcRd, ORc, C(O)Rc, C(O)ORc, OC(O)Rc, C(O)N(Rd)Rc, N(Rd)C(O )Rc, S(O)yRc where y is 0, 1 or 2, SO2N(Rd)Rc, N(Rd)SO2Rc, Si(Rd)(Rc)Re and (CH2)zNRcRd where z is 1, 2 or 3 ; wherein Rc, Rd and Re are each independently selected from hydrogen, (1-6C)alkyl and (3-6C)cycloalkyl; or Rc and Rd may be attached such that, together with the nitrogen atom to which they are attached, they form a 4-7 membered heterocyclic ring which is optionally substituted with one or more substituents selected from (1-4C)alkyl, halo, (1-4C)haloalkyl, (1-4C)haloalkoxy, (1-4C)alkoxy, (1-4C)alkylamino, amino, cyano and hydroxyl; or Q is optionally substituted by a group of the formula: -L1-LQ1-Z1 wherein: L1 is absent or is (1-3C)alkylene optionally substituted with one or more substituents selected from (1-2C)alkyl or oxo; LQ1 is absent or selected from S, SO, SO2, N(Rf), C(O), C(O)O, OC(O), C(O)N(Rf), N(Rf)C(O ), N(Rg)C(O)N(Rf), N(Rf)C(O)O, OC(O)N(Rf), S(O)2N(Rf), and N(Rf)SO2, in where Rf and Rg are each independently selected from hydrogen and (1-2C)alkyl; and Z1 is hydrogen, (1-6C)alkyl, aryl, (1-2C)arylalkyl, (3-8C)cycloalkyl, (3-8C)cycloalkenyl, heteroaryl, or heterocyclyl; wherein Z1 is optionally substituted with one or more substituents selected from (1-4C)alkyl, halo, (1-4C)haloalkyl, (1-4C)haloalkoxy, (1-4C)alkoxy, (1-4C)alkylamino, amino , cyano, hydroxy, carboxy, carbamoyl, sulfamoyl, mercapto, ureido, aryl, heteroaryl, heterocyclyl, (3-6C)cycloalkyl, NRhRi, ORh, C(O)Rh, C(O)ORh, OC(O)Rh, C(O)N(Ri)Rh, N(Ri)C(O)Rh, S(O)yaRh where ya is 0, 1 or 2, SO2N(Ri)Rh, N(Ri)SO2Rh and (CH2)zaNRiRh where za is 1, 2 or 3; wherein Rh and Ri are each independently selected from hydrogen, (1-4C)alkyl and (3-6C)cycloalkyl; R1a and R1b are each selected from hydrogen, (1-4C)alkyl, halo, (1-4C)haloalkyl, (1-4C)haloalkoxy, (1-4C)alkoxy, (1-4C)alkylamino, amino, cyano , hydroxy, carboxy, carbamoyl, sulfamoyl, and mercapto; W is selected from O, S and NRj, where Rj is selected from H and (1-2C)alkyl; X1 and X2 are each independently selected from N and CRk; wherein Rk is selected from hydrogen, halo, (1-4C)alkyl, (1-4C)alkoxy, amino, (1-4C)alkylamino, (1-4C)dialkylamino, cyano, (2C)alkynyl, C(O )Rk1, C(O)ORk1, OC(O)Rk1, C(O)N(Rk2)Rc, N(Rk2)C(O)Rk1, S(O)ybRk1 where yb is 0, 1 or 2, SO2N (Rk2)Rk1, N(Rk2)SO2Rk1 and (CH2)zbNRk1Rk2 where zb is 1, 2 or 3; wherein said (1-4C)alkyl is optionally substituted with one or more substituents selected from amino, hydroxy, (1-2C)alkoxy and halo; and Rk1 and Rk2 are each independently selected from hydrogen and (1-4C)alkyl; X3 is selected from N and CRm; wherein Rm is selected from hydrogen, halo, (1-4C)alkyl, (1-4C)alkoxy, amino, (1-4C)alkylamino, (1-4C)dialkylamino, cyano, (2C)alkynyl, C(O )Rm1, C(O)ORm1, OC(O)Rm1, C(O)N(Rm2)Rm1, N(Rm2)C(O)Rm1, S(O)ycRm1 where yc is 0, 1 or 2, SO2N (Rm2)Rm1, N(Rm2)SO2Rm1 and (CH2)zcNRm1Rm2 where zc is 1, 2 or 3; wherein said (1-4C)alkyl is optionally substituted with one or more substituents selected from amino, hydroxy, (1-2C)alkoxy and halo; and Rm1 and Rm2 are each independently selected from hydrogen and (1-4C)alkyl; Ro is selected from halo, (1-4C)alkyl, (1-4C)alkoxy, amino, (1-4C)alkylamino, (1-4C)dialkylamino, cyano, (2C)alkynyl, C(O)Ro1, C (O)ORo1, OC(O)Ro1, C(O)N(Ro2)Ro1, N(Ro2)C(O)Ro1, S(O)ydRo1 where yd is 0, 1 or 2, SO2N(Ro2)Ro1 , N(Ro2)SO2Ro1 and (CH2)zdNRo1Ro2 where zd is 1, 2 or 3; wherein said (1-4C)alkyl is optionally substituted with one or more substituents selected from amino, hydroxy, (1-2C)alkoxy and halo; and Ro1 and Ro2 are each independently selected from hydrogen and (1-4C)alkyl; R2 is selected from hydrogen, (1-4C)alkyl and a group of the formula: -L2-Y2-Q2 wherein: L2 is absent or is (1-3C)alkylene optionally substituted with one or more substituents selected from ( 1-2C) or oxo; Y2 is absent or is C(O), C(O)O or C(O)N(Rp), where Rp is selected from hydrogen and (1-4C)alkyl; and Q2 is hydrogen, (1-6C)alkyl, aryl, (3-8C)cycloalkyl, (3-8C)cycloalkenyl, heteroaryl, or heterocyclyl; wherein Q2 is optionally substituted with one or more substituent groups independently selected from (1-4C)alkyl, halo, (1-4C)haloalkyl, (1-4C)haloalkoxy, amino, cyano, hydroxy, carboxy, carbamoyl, sulfamoyl, NRqRr and ORq, wherein Rq and Rr are each independently selected from hydrogen, (1-4C)alkyl, and (3-6C)cycloalkyl; R3 is selected from a group of the formula: -Y3-Q3 where: Y3 is C(O), C(O)N(Ry), C(O)N(Ry)O, N(Ry)(O)C , C(O)O, OC(O), N(Ry)C(O)N(Ry1), SO2N(Ry), N(Ry)SO2, oxazolyl, triazolyl, oxadiazolyl, thiazolyl, imidazolyl, thiadiazolyl, pyridinyl, pyrazolyl, pyrrolyl, or tetrazolyl, wherein Ry and Ry1 are independently selected from hydrogen and (1-2C)alkyl; and Q3 is hydrogen, (1-6C)alkyl, aryl, (1-2C)arylalkyl, (3-8C)cycloalkyl, (3-8C)cycloalkenyl, heteroaryl, or heterocyclyl; wherein Q3 is optionally substituted with one or more substituent groups independently selected from (1-4C)alkyl, halo, (1-4C)haloalkyl, (1-4C)haloalkoxy, amino, cyano, hydroxy, carboxy, carbamoyl, sulfamoyl, NRzRaa and ORz, where Rz and Raa are each independently selected from hydrogen, (1-4C)alkyl and (3-6C)cycloalkyl; or Q3 is optionally substituted with a group of the formula: -L4-LQ4-Z4 wherein: L4 is absent or is (1-3C)alkylene optionally substituted with one or more substituents selected from (1-2C)alkyl or oxo; LQ4 is absent or selected from O, S, SO, SO2, N(Rab), C(O), C(O)O, OC(O), C(O)N(Rab), N(Rab)C (O), N(Rac)C(O)N(Rab), N(Rab)C(O)O, OC(O)N(Rab), S(O)2N(Rab), and N(Rab)SO2 , wherein Rab and Rac are each independently selected from hydrogen and (1-2C)alkyl; and Z4 is hydrogen, (1-6C)alkyl, aryl, (1-2C)arylalkyl, (3-8C)cycloalkyl, (3-8C)cycloalkenyl, heteroaryl, or heterocyclyl; wherein Z4 is optionally substituted with one or more substituents selected from (1-4C)alkyl, halo, (1-4C)haloalkyl, (1-4C)haloalkoxy, (1-4C)alkoxy, (1-4C)alkylamino, amino, cyano, hydroxy, carboxy, carbamoyl, sulfamoyl, mercapto, ureido, aryl, heteroaryl, heterocyclyl, (3-6C)cycloalkyl, NRadRae, ORad, C(O)Rad, C(O)ORad, OC(O)Rad , C(O)N(Rae)Rad, N(Rae)C(O)Rad, S(O)yeRad where ye is 0, 1, or 2, SO2N(Rae)Rad, N(Rae)SO2Rad, and (CH2) zeNRadRae where ze is 1, 2 or 3; wherein Rad and Rae are each independently selected from hydrogen, (1-4C)alkyl and (3-6C)cycloalkyl; o Q3 and Ry are bonded such that, together with the nitrogen atom to which they are bonded, they form a 4-7 membered heterocyclic ring that is optionally substituted with one or more substituents selected from (1-4C)alkyl, halo , (1-4C)haloalkyl, (1-4C)haloalkoxy, (1-4C)alkoxy, (1-4C)alkylamino, amino, cyano and hydroxyl; provided that only one or two of X1, X2 or X3 can be N. |
| priorityDate | 2016-04-15-04:00^^<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: 1140.