http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2905673-T3
Outgoing Links
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| filingDate | 2016-10-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2022-04-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_94b9825699bfc616d2924bceb0a6a112 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_485876fa17b9b79d2891511a6aa1758b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_031ebb2943255bc6cbb8629da2b6d2c5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_571d790e60f8c52da323e4d6997ae3f4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1721f5f4b60c6612fbb532559ac376a1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4a7b1a39cd425158f02fee5de785fb99 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2f717ecfcceabeafdf6fa6b16b3ea374 |
| publicationDate | 2022-04-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2905673-T3 |
| titleOfInvention | Quinoxaline and pyridopyrazine derivatives as PI3KBETA inhibitors |
| abstract | A compound of Formula (I) **(See formula)** a tautomer or a stereoisomeric form thereof, wherein Y represents CR3 or N; L represents -CH(C1-4 alkyl)-CH2-, -CH2-CH(C1-4 alkyl)-, -CH(C1-4 alkyl)-CH(C1-4 alkyl)-, -CHR1a-X-, or -X-CHR1c-; X represents O, S, or NR1b; R1a represents hydrogen, C1-4alkyl, or C1-4alkyl substituted with an -OH; R1c represents hydrogen or C1-4alkyl; R1b represents hydrogen, C1-4alkyl, -CH2-C(=O)-NR6aR6b, or C1-4alkyl substituted with a substituent selected from the group consisting of hydroxyl, -OC1-4alkyl, and -NR6cR6d; or R1b is taken together with R1a or R1c to form -(CH2)3-; or R1b is taken together with R1c to form -(CH2)2- or -(CH2)4-; R2 represents **(See formula)** each of R6a and R6b is independently selected from the group consisting of hydrogen and C1-4alkyl; R6c and R6d are each independently selected from the group consisting of hydrogen, C1-4alkyl, and C1-4alkyl substituted with a substituent selected from the group consisting of hydroxyl, -NH2, -NH(C1-4alkyl), and -N(C1-4alkyl)2; R3 represents R7, -(C=O)H, -(C=O)-C1-4alkyl, -(C=O)-NR5aR5b, -(C=O)-OR5c, -C(=O)-Het1 , -C(=O)-NH-Het2, -C(=O)- NH-C1-4alkyl-Het1, -C(=O)-N(C1-4alkyl)-C1-4alkyl-Het1, -C(=O)-N(C1-4 alkyl)-Het2, C1-4 alkyl, -CH=N-OH, -CH(OH)- CH2-NR5dR5e, -CH(OH)-CH2-Het1, - CH(OH)-C1-4alkyl, -C(OH)(C1-4alkyl)2, halo, or R3 represents C1-4alkyl substituted with a substituent selected from the group consisting of hydroxyl, fluorine, -NR5fR5g, Het1 , -O-(C=O)- CH(NH2)-C1-4 alkyl, -O-(C=O)-CH(NH2)-C1-4 alkyl-Ar,**(See formula)** , -O-C1-4alkyl-OH, and -O-C1-4alkyl-NH2; R5a and R5b are each independently selected from the group consisting of hydrogen, C1-4 alkyl, -O-C1-4 alkyl, -S(=O)2-NH2, -S(=O)2-C1-alkyl- 4, -S(=O)2-C3-6 cycloalkyl, C1-4 alkyl substituted with one or more halo atoms, and C1-4 alkyl substituted with a substituent selected from the group consisting of hydroxyl, -O-C1 alkyl -4, -S(=O)2- C1-4 alkyl, -O-C1-4 alkyl-NH2, -O-C1-4 alkyl-NH(C1-4 alkyl), -O-C1-4 alkyl- N(C1-4alkyl)2, -(C=O)-O-C1-4alkyl, -(C=O)-OH, -(C=O)-C1-4alkyl, -NH2, -NH( C1-4alkyl) and -N(C1-4alkyl)2; R5c represents hydrogen or C1-4alkyl; R5d and R5e are each independently selected from the group consisting of hydrogen and C1-4alkyl; R5f and R5g are each independently selected from the group consisting of hydrogen, C1-4 alkyl, C1-4 alkyl substituted with one or more halo atoms, and C1-4 alkyl substituted with a substituent selected from the group consisting of hydroxyl , -OC1-4alkyl, -S(=O)2-C1-4alkyl, -NH2, -NH(C1-4alkyl), and -N(C1-4alkyl)2; each of R4a, R4b, and R4c is independently selected from the group consisting of hydrogen, cyano, C1-4 alkyl, halo, -C(=O)H, -NR6eR6f, -OC1-4 alkyl, and C1-4 alkyl. 4 substituted with one or more substituents each independently selected from the group consisting of hydroxyl, halo, and -NR6gR6h; R6e and R6f are each independently selected from the group consisting of hydrogen, C1-4alkyl, and C1-4alkyl substituted with a substituent selected from the group consisting of -NH2, -NH(C1-4alkyl), and hydroxyl ; R6g and R6h are each independently selected from the group consisting of hydrogen, C1-4alkyl, and C1-4alkyl substituted with a substituent selected from the group consisting of -NH2, -NH(C1-4alkyl), and hydroxyl ; Het1 represents a 4-, 5-, 6- or 7-membered monocyclic saturated or partially saturated heterocyclyl containing at least one heteroatom each independently selected from O, S, S(=O)p and N; or Het1 represents a bicyclic 8-, 9- or 10-membered saturated or partially saturated heterocyclyl containing at least one heteroatom each independently selected from O, S, S(=O)p and N; each optionally substituted with one or two substituents each independently selected from the group consisting of halo, -NR9aR9b, C1-4alkyl, -(C=O)-OR5h, -S(=O)2-C1-6alkyl, -C1-4alkyl-S(=O)2-C1-6alkyl, hydroxyl, -OC1-4alkyl, cyano, C1-4alkyl substituted with one or more halo atoms, and C1-4alkyl substituted with a substituent selected from the group consisting of hydroxyl, -NH2, -NH(C1-4alkyl), and -N(C1-4alkyl)2; or two substituents on the same carbon atom of said heterocyclyl are taken together to form together with the common carbon atom to which they are attached Ring A; each of R9a and R9b is independently selected from the group consisting of hydrogen, C1-4alkyl, and C1-4alkyl substituted with one or more halo atoms; Het2 represents **(See formula)** n1 represents 1 or 2; n2 represents 1 or 2; R8 represents hydrogen, C1-4alkyl, or C1-4alkyl substituted with one or more halo atoms; R5h represents hydrogen or C1-4alkyl; Ring A represents cyclobutyl, cyclopentyl, cyclohexyl, or a saturated 4-, 5-, or 6-membered heterocyclyl containing at least one heteroatom each independently selected from O, S, S(=O)p, and N; said saturated 4-, 5-, or 6-membered cyclobutyl, cyclopentyl, cyclohexyl, or heterocyclyl is optionally substituted with one or two C1-4 alkyl substituents, with one C1-4 alkyl and one hydroxy substituent, or with one hydroxy substituent; p represents 1 or 2; Ar represents phenyl optionally substituted with a hydroxyl; R7 represents ; or an N-oxide, a pharmaceutically acceptable addition salt or a solvate thereof. |
| priorityDate | 2015-10-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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