http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2627703-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_2e639c6bc8757f0eed17bf02fa72892c |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 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/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4985 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 |
| filingDate | 2011-01-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2017-07-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ab06f1ca0745b17604b430fc8e0a6ed8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bb50e89578b73120eb3adfe3df0a9722 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_95725e81a6a322fbfd697ca3c4e0ce31 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_58f6e48fbdce302670d67f524c512d6f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ed83ba0c33a1ff021f88ed6ad0183e51 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_00441974c68c42cfc1155e4e4a6fb085 |
| publicationDate | 2017-07-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2627703-T3 |
| titleOfInvention | PI3 kinase inhibitors |
| abstract | A compound of formula I, ** Formula ** wherein: A1 represents N or C (R1); A4 represents N or C (R1a); A4a represents N or C (R1b); where at least one of A4 and A4a does not represent N; A5 represents N or C (R2); wherein when A4, A4a and A5 respectively represent C (R1a), C (R1b) and C (R2), then A1 does not represent N; each B1, B1a, B2, B2a, B3, B3a, B4 and B4a independently represent hydrogen or a substituent selected from halogen, -C (> = Y) -R10a, -C (> = Y) -OR10a, -C ( > = Y) N (R10a) R11a, -S (O) 2N (R10a) R11a, C1-12 alkyl, heterocycloalkyl (the last two groups of which are optionally substituted with one or more substituents selected from> = O and E1), aryl and / or heteroaryl (the last two groups of which are optionally substituted with one or more substituents selected from E2); or any pair of B1, B1a, B2, B2a, B3, B3a, B4 and B4a substituents that are attached to the same carbon atom (i.e., B1 and B1a; B2 and B2a; B3 and B3a and / or B4 and B4a) they can form between them a group> = O; or, any pair of B1, B1a, B2, B2a, B3, B3a, B4, and B4a substituents can join together to form another 3- to 12-membered ring, optionally containing (in addition to the morpholine ring atom (s)) one or more heteroatoms, whose ring optionally contains one or more double bonds, and whose ring is optionally substituted by one or more substituents selected from halogen,> = O and C1-3 alkyl optionally substituted by one or more fluorine atoms ; R1 and R2 independently represent hydrogen or a substituent selected from halogen, -CN, -OR10b, -N (R10b) R11b, -C (O) N (R10b) R11b, C1-12 alkyl (eg, C1- 6) and heterocycloalkyl, the last two groups of which are optionally substituted with one or more substituents selected from E3 and> = O; R1b (when present) represents: (i) C1-12 alkyl optionally substituted with one or more substituents selected from Q1a; (ii) heterocycloalkyl (linked through a carbon atom) optionally substituted with one or more substituents selected from> = O and Q1b; or (iii) a fragment of formula IA; R1a (when present) represents: (i) hydrogen; (ii) Q1; (iii) C1-12 alkyl optionally substituted with one or more substituents selected from> = O,> = S,> = N (R10a) and Q2; or (iv) a fragment of formula IA; ** Formula ** the fragment of formula IA represents: ** Formula ** wherein: m represents 1, 2, 3, 4, 5 or 6; each R15 represents hydrogen, halogen or C1-6 alkyl optionally substituted with one or more substituents selected from E4; or the two R15 groups may be attached to each other to form (along with the necessary carbon atom to which these R15 groups are necessarily attached) a 3- to 6-membered (spirocyclic) ring, the ring optionally containing one or more doubles bonds and optionally contains an additional heteroatom selected from nitrogen, sulfur, and oxygen, and the ring of which is optionally substituted with one or more substituents selected from E5; Ra and Rb are bonded together, together with the necessary nitrogen atom to which they are necessarily bonded, to form a first 3- to 7-membered cyclic group, optionally containing an additional heteroatom selected from nitrogen, sulfur, and oxygen, and whose ring: (a) is fused with a second ring which is a 3-7 membered saturated heterocycloalkyl group containing from one to four heteroatoms selected from oxygen, sulfur, and nitrogen, a 3-12 membered saturated carbocyclic ring, or a ring 5- to 12-membered heterocyclic or carbocyclic unsaturated (wherein heteroatoms are preferably selected from sulfur and, above all, nitrogen and oxygen); (b) comprises a connecting group - (C (Rx) 2) p- and / or - (C (Rx) 2) rO- (C (Rx) 2) s- (where p is 1 or 2; r is 0 or 1; s is 0 or 1; and each Rx independently represents hydrogen or C1-6 alkyl), which joins together any pair of 3- to 7-membered non-adjacent first ring atoms (i.e., forming a bridging structure ); or (c) comprises a second ring that is either a 3- to 12-membered saturated carbocyclic ring or a 3- to 7-membered saturated heterocycloalkyl group containing from one to four heteroatoms selected from oxygen and nitrogen and whose second ring is linked with the first ring through a single carbon atom common to both rings (i.e., forming a spiro-cycle), all said cyclic groups, defined by the union of Ra and Rb, are optionally substituted with one or more substituents selected from > = O,> = NOR10a and E6; R3 represents aryl or heteroaryl (both of which are optionally substituted with one or more substituents selected from E7); each independent Q1a, Q1b, Q1 and Q2 represents, on each occasion when used herein: halogen, -CN, -NO2, -N (R10a) R11a, -OR10a, -C (> = Y) -R10a, - C (> = Y) -OR10a, -C (> = Y) N (R10a) R11a, -C (> = Y) N (R10a) -OR11c, -OC (> = Y) -R10a, -OC (> = Y) -OR10a, -OC (> = Y) N (R10a) R11a, -OS (O) 2OR10a, -OP (> = Y) (OR10a) (OR11a), -OP (OR10a) (OR11a), - N (R12a) C (> = Y) R11a, -N (R12a) C (> = Y) OR11a, -N (R12a) C (> = Y) N (R10a) R11a, -NR12aS (O) 2R10a, - NR12aS (O) 2N (R10a) R11a, -S (O) 2N (R10a) R11a, -SC (> = Y) R10a, -S (O) 2R10a, -SR10a, -S (O) R10a, C1-alkyl 12, heterocycloalkyl (whose last two groups are optionally substituted with one or more substituents selected from> = O,> = S,> = N (R10a) and E8), aryl or heteroaryl (whose last two groups are optionally substituted with one or plus selected substituents from E9); each R11c independently represents C1-12 alkyl, heterocycloalkyl (whose last two groups are optionally substituted with one or more substituents selected from> = O,> = S,> = N (R20) and E10), aryl or heteroaryl (whose last two groups are optionally substituted with one or more substituents selected from E11); each R10a, R11a, R10b, R11b and R12a independently represent, on each occasion used herein, hydrogen, C1-12 alkyl, heterocycloalkyl (the last two groups of which are optionally substituted with one or more substituents selected from> = O ,> = S,> = N (R20) and E10), aryl or heteroaryl (the last two groups of which are optionally substituted with one or more substituents selected from E11); or any relevant pair of R10a and R11a or R10b and R11b 45 substituents may be linked together to form a 4- to 20-membered ring, optionally containing one or more heteroatoms, optionally containing one or more instants, and whose ring is optionally substituted with one or more substituents selected from> = O,> = S,> = N (R20) and E12; each E1, E2, E3, E4, E5, E6, E7, E8, E9, E10, E11 and E12 independently represents, on each occasion when used herein: (i) Q4; (ii) C1-12 alkyl optionally substituted with one or more substituents selected from> = O and Q5; or any pair of E1, E2, E3, E4, E5, E6, E7, E8, E9, E10, E11 or E12 groups can be linked together to form a 3- to 12-membered ring, optionally containing one or more unsaturations , and whose ring is optionally substituted with one or more substituents selected from> = O and J1; each Q4 and Q5 independently represent, each time when used herein: halogen, -CN, -NO2, -N (R20) R21, -OR20, -C (> = Y) -R20, -C (> = Y) -OR20, -C (> = Y) N (R20) R21, -C (> = Y) N (R20) -O-R21a, -OC (> = Y) -R20, -OC (> = Y ) - OR20, -OC (> = Y) N (R20) R21, -OS (O) 2OR20, -OP (> = Y) (OR20) (OR21), -OP (OR20) (OR21), -N ( R22) C (> = Y) R21, -N (R22) C (> = Y) OR21, -N (R22) C (> = Y) N (R20) R21, -NR22S (O) 2R20, -NR22S ( O) 2N (R20) R21, -S (O) 2N (R20) R21, -SC (> = Y) R20, -S (O) 2R20, -SR20, -S (O) R20, C1-6 alkyl, heterocycloalkyl (whose last two groups are optionally substituted with one or more substituents selected from> = O and J2), aryl or heteroaryl (whose last two groups are optionally substituted with one or more substituents selected from J3); each Y independently represents, each time it is used in this document,> = O,> = S,> = NR23 or> = N-CN; each R21 represents C1-6 alkyl, heterocycloalkyl (whose last two groups are optionally substituted with one or more substituents selected from J4 and> = O), aryl or heteroaryl (whose last two groups are optionally substituted with one or more substituents selected from J5 ); each R20, R21, R22 and R23 independently represent, on each occasion used herein, hydrogen, C1-6 alkyl, heterocycloalkyl (the last two groups of which are optionally substituted with one or more substituents selected from J4 and> = O ), aryl or heteroaryl (the last two groups of which are optionally substituted with one or more substituents selected from J5); or any suitable pair of R20, R21 and R22 may be linked together to form a 4- to 20-membered ring, optionally containing one or more heteroatoms, optionally containing one or more unsaturations, and whose ring is optionally substituted with one or plus selected substituents of J6 and> = O; each independent J1, J2, J3, J4, J5, and J6 represents, each time it is used in this document: (i) Q7; (ii) C1-6alkyl or heterocycloalkyl, both of which are optionally substituted with one or more substituents selected from> = O and Q8; each independent Q7 and Q8 represents, each time it is used in this document: halogen, -CN, -N (R50) R51, -OR50, -C (> = Ya) -R50, -C (> = Ya) -OR50, -C (> = Ya) N (R50) R51, -N (R52) C (> = Ya) R51, -NR52S (O) 2R50, -S (O) 2N (R50) R51, -N ( R52) -C (> = Ya) -N (R50) R51, -S (O) 2R50, -SR50, -S (O) R5, C1-6 alkyl (optionally substituted with one or more fluorine atoms), heterocycloalkyl , aryl or heteroaryl (the last three groups of which are optionally substituted with one or more substituents selected from halogen, -OR60 and -N (R61) R62); each Ya independently represents, each time it is used in this document,> = O,> = S,> = NR53 or> = N-CN; each R50, R51, R52 and R53 independently represents, on each occasion used herein, hydrogen or C1-6alkyl optionally substituted with one or more substituents selected from fluorine, -OR60 and -N (R61) R62 ; or any suitable pair of R50, R51 and R52 may be linked together to form a 3- to 8-membered ring, optionally containing one or more heteroatoms, optionally containing one or more unsaturations, and whose ring is optionally substituted with one or plus selected substituents of> = O and C1-3 alkyl; each R60, R61 and R62 independently represent hydrogen or C1-6 alkyl optionally substituted with one or more fluorine atoms, or a pharmaceutically acceptable ester, amide, solvate or salt thereof. |
| priorityDate | 2010-01-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 821.