http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2773138-T3
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| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f2d3599fb8f8f479dba95ca9bb504884 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
| filingDate | 2014-04-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2020-07-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_967285a2a937cbf64e494070af735d21 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f3f4f0606d87a317286fef21f60c1d5e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7565878751ea4217ef9f7be5a62dfcaf http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_daf3873219280555392d997d3fb88637 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_673c13bc89232ebffc42950b667d13b9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c21388da8f63e6998868b1f6d4182cd8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b80e04bcd5a71bd43d37c4fcc1d02021 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1fdeeb240ed8848416fb2c03075ae35b |
| publicationDate | 2020-07-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2773138-T3 |
| titleOfInvention | 3- (2-Aminopyrimidin-4-yl) -5- (3-hydroxypropinyl) -1H-pyrrolo [2,3-c] pyridine derivatives as NIK inhibitors for cancer treatment |
| abstract | A compound of formula (I): ** (See formula) ** or a tautomer or a stereoisomeric form thereof, where R1 is selected from the group consisting of hydrogen; C1-6alkyl; C1-6alkyl substituted with one or more fluoro substituents; and C1-6alkyl substituted with a substituent selected from the group consisting of -NR1aR1b, -OH and -OC1-4alkyl; R2 is selected from the group consisting of hydrogen; C1-6alkyl; C1-6alkyl substituted with one or more fluoro substituents; C1-6alkyl substituted with a substituent selected from the group consisting of -NR2aR2b, -OH, -OC1-4alkyl, C3-6cycloalkyl, Het1, Het2, and phenyl; -C (= O) -NR2cR2d; C3-6cycloalkyl; Het1; Het2; and phenyl; wherein the phenyl groups are optionally substituted with one or two substituents independently selected from the group consisting of halogen, cyano, C1-4alkyl, C1-4alkoxy, C1-4alkyl substituted with one or more fluoro substituents, and C1-4alkyloxy substituted with one or more fluoro substituents; R1a, R1b, R2a, R2b, R2c and R2d are independently selected from each other from hydrogen and C1-4alkyl; Het1 is a heterocyclyl selected from the group consisting of piperidinyl, piperazinyl, tetrahydropyranyl, pyrrolidinyl, tetrahydrofuranyl, azetidinyl, and oxetanyl, each of which may be optionally substituted with a C1-4alkyl; Het2 is a heteroaryl selected from the group consisting of thienyl, thiazolyl, pyrrolyl, oxazolyl, pyrazolyl, imidazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyrimidinyl, pyridazinyl, and pyrazinyl, each of which may be optionally substituted with one or two substituents selected as independent of halogen, cyano, C1-4alkyl, C1-4alkoxy, C1-4alkyl substituted with one or more fluoro substituents, and C1-4alkyloxy substituted with one or more fluoro substituents; or R1 and R2 together with the carbon atom to which they are attached form a C3-6cycloalkyl or a Het3 group; where Het3 is a heterocyclyl selected from the group consisting of piperidinyl, tetrahydropyranyl, pyrrolidinyl, tetrahydrofuranyl, azetidinyl and oxetanyl, each of which may be optionally substituted with a C1-4alkyl; or Het3 is 2-oxo-3-pyrrolidinyl optionally substituted with a C1-4alkyl; R3 is selected from the group consisting of hydrogen; halo; C3-6cycloalkyl; C1-4alkyl; C1-4alkyl substituted with one or more fluoro substituents; and C1-4alkyloxy substituted with one or more fluoro substituents; R4 is selected from the group consisting of hydrogen; halogen; C1-4alkyl; C1-4alkyl substituted with one or more fluoro substituents; and cyano; R5 is selected from the group consisting of hydrogen; C1-6alkyl; C1-6alkyl substituted with one or more fluoro substituents; cyano; C1-6alkyl substituted with a substituent selected from the group consisting of -NR5aR5b, -OH, -OC1-4alkyl, C3-6cycloalkyl, and Het4; C3-6cycloalkyl; and -C (= O) -NR5cR5d; where R5a and R5b are independently selected from the group consisting of hydrogen and C1-4alkyl; and R5c and R5d are independently selected from the group consisting of hydrogen; C1-6alkyl optionally substituted with Het5; and C2-6alkyl substituted with a substituent selected from -NR5xR5y, -OH and -OC1-4alkyl; Het4 is a heterocyclyl selected from the group consisting of piperidinyl, morpholinyl, piperazinyl, tetrahydropyranyl, pyrrolidinyl, tetrahydrofuranyl, azetidinyl, and oxetanyl, each of which may be optionally substituted with a C1-4alkyl; Het5 is a heterocyclyl selected from the group consisting of piperidinyl, morpholinyl, piperazinyl, tetrahydropyranyl, pyrrolidinyl, tetrahydrofuranyl, azetidinyl, and oxetanyl, each of which may be optionally substituted with a C1-4alkyl; R5x and R5y are independently selected from the group consisting of hydrogen and C1-4alkyl; or R5c and R5d together with the nitrogen atom to which they are attached form a Het6 group; where Het6 is a heterocyclyl selected from the group consisting of piperidinyl, pyrrolidinyl, azetidinyl, piperazinyl, and morpholinyl, each of which may be optionally substituted with a substituent selected from C1-4alkyl; -OC1-4alkyl; and C1-4alkyl substituted with an -OH; R6 is selected from the group consisting of hydrogen; halogen; cyano; C1-6alkyl; C1-6alkyl substituted with one or more fluoro substituents; C1-6alkyl substituted with an -OH; C1-6alkyl substituted with an NH2; -C1-6alkyloxyC1-4alkyl; -C 1-6 alkyl-C (= O) -NR6aR6b; -OC1-6alkyl; -OC1-6alkyl substituted with one or more fluoro substituents; -OC1-6alkyl substituted with a Het7 substituent; -OC2-6alkyl substituted with a substituent selected from the group consisting of -NR6cR6d, -OH, and -OC1-4alkyl; and -C (= O) -NR6aR6b; where R6a, R6c and R6d are independently selected from among hydrogen and C1-4alkyl; and R6b is selected from hydrogen, C1-4alkyl, C2-4alkyloxyC1-4alkyl and C2-4alkylNR6xR6y; or R6a and R6b, together with the nitrogen atom to which they are attached form a heterocyclyl selected from the group consisting of piperidinyl, piperazinyl, morpholinyl, pyrrolidinyl, and azetidinyl, each of which may be optionally substituted with a C1-4alkyl; R6x is hydrogen or C1-4alkyl and R6y is C1-4alkyl; and Het7 is a heterocyclyl selected from the group consisting of piperidinyl, piperazinyl, morpholinyl, tetrahydropyranyl, pyrrolidinyl, tetrahydrofuranyl, azetidinyl, and oxetanyl, each of which may be optionally substituted with a C1-4alkyl; R7 is selected from the group consisting of hydrogen, C1-4alkyl, cyano, -OC1-4alkyl, -NHC1-4alkyl, -NH-C (= O) -C1-4alkyl and -C (= O) -NR7aR7b; where R7a and R7b are independently selected from one another from hydrogen and C1-4alkyl; R8 is selected from the group consisting of hydrogen; -C (= O) -NR8gR8h; Het8; C1-6alkyl optionally substituted with Het9; -C (= O) -Het12; C3-6cycloalkyl optionally substituted with a -OC1-4alkyl; C1-6alkyl substituted with one cyano; -CH2-C (= O) NR8aR8b; and C2-6alkyl substituted with one or more substituents independently selected from the group consisting of (i) fluoro, (ii) -NR8aR8b, (iii) -NR8cC (= O) R8d, (iv) -NR8cC (= O) NR8aR8b , (v) -NR8cC (= O) OR8e, (vi) -NR8cS (= O) 2NR8aR8b, (vii) -NR8cS (= O) 2R8d, (viii) -OR8f, (ix) -OC (= O) NR8aR8b , (x) -C (= O) NR8aR8b, (xi) -SR8e, (xii) -S (O) 2R8d, and (xiii) -S (O) 2NR8aR8b; where R8a, R8b, R8c and R8f are independently selected from the group consisting of hydrogen; C1-6alkyl, which may be optionally substituted with a substituent selected from Het10 and Het11; C3-6cycloalkyl; and C2-6alkyl substituted with a substituent selected from -NR8xR8y, -OH, and -OC1-4alkyl; R8d is selected from the group consisting of C1-6alkyl, which may be optionally substituted with a substituent selected from -NR8xR8y, -OH, -OC1-4alkyl, Het10 and Het11; and C3-6cycloalkyl; R8e is selected from the group consisting of C1-6alkyl, which may be optionally substituted with a substituent selected from Het10 and Het11; C3-6cycloalkyl; and C2-6alkyl substituted with a substituent selected from -NR8xR8y, -OH, and -OC1-4alkyl; where R8x and R8y are independently selected from hydrogen and C1-4alkyl; R8g and R8h are independently selected from the group consisting of hydrogen, C1-4alkyl and C2-4alkyl substituted with an -OC1-4alkyl; and Het8 is a heterocyclyl, attached through any available carbon atom, selected from the group consisting of piperidinyl, tetrahydropyranyl, pyrrolidinyl, tetrahydrofuranyl, azetidinyl, and oxetanyl, each of which may be optionally substituted with a substituent selected from halo, - C (= O) -C1-4alkyl, C1-4alkyl, C3-6cycloalkyl, C1-4alkyl substituted with a C3-6cycloalkyl, C1-4alkyl substituted with one or more fluoro substituents, and C1-4alkyl substituted with a -OC1-4alkyl ; Het9 is a heterocyclyl selected from the group consisting of morpholinyl, piperidinyl, piperazinyl, tetrahydropyranyl, pyrrolidinyl, tetrahydrofuranyl, azetidinyl, and oxetanyl, each of which may be optionally substituted with a substituent selected from halo, C1-4alkyl, C1-4alkyl substituted with one or more fluoro substituents, and -OC1-4alkyl; or Het9 is a heteroaryl selected from the group consisting of oxazolyl, pyrrolyl, pyrazolyl, imidazolyl, pyridinyl, pyrimidinyl, pyridazinyl and pyrazinyl, each of which may be optionally substituted with a C1-4alkyl; or Het9 is selected from the group consisting of ** (See formula) ** Het10 is a heterocyclyl selected from the group consisting of piperazinyl, morpholinyl, piperidinyl, tetrahydropyranyl, pyrrolidinyl, tetrahydrofuranyl, azetidinyl, and oxetanyl, each of which may be optionally substituted with a C1-4alkyl; Het11 is selected from the group consisting of ** (See formula) ** Het12 is a heterocyclyl selected from the group consisting of 1-piperidinyl, 1-piperazinyl, 1-pyrrolidinyl, and 1-azetidinyl, each of which may be optionally substituted with a substituent selected from C1-4alkyl and -OC1-4alkyl; R9 is hydrogen; or a pharmaceutically acceptable salt or a solvate thereof. |
| priorityDate | 2013-04-24-04:00^^<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: 785.