http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-083842-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_1f67dd95fb433cb3458c52756dbd5b4c |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5386 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-541 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 |
| classificationIPCInventive | 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/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 |
| filingDate | 2011-11-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9f8bad01f47dc846b64a67470c6a98b2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6e80995f7e2bfc49d2f8b82d14053573 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2d0deb57942c7f1f25289bd4e4967c6a |
| publicationDate | 2013-03-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-083842-A1 |
| titleOfInvention | DERIVATIVES OF 2,3-DIHYDROIMIDAZO [1,2-C] QUINAZOLINE SUBSTITUTED WITH AMINOALCOHOLES THAT ARE USEFUL TO TREAT HYPERPROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS |
| abstract | Pharmaceutical compositions containing said compounds. Use of said compounds or of said compositions in the inhibition of phosphotidylinositol-3-kinase (PI3K) and in the treatment of diseases associated with phosphotidylinositol-3-kinase (PI3K), particularly in the treatment of hyperproliferative and / or related disorders with angiogenesis, alone or in combination with other active ingredients. Claim 1: A compound of general formula (1) wherein: R1 represents - (CH2) n- (CHR4) - (CH2) mN (R5) (R5 ') ; R2 represents a heteroaryl of structure of formula (2) optionally substituted with 1, 2 or 3 R6 groups, wherein: * represents the point of attachment of said heteroaryl with the rest of the compound of general formula (1), X represents N or C-R6, X 'represents O, S, NH, N-R6, N or C-R6, with the proviso that when X and X' are both C-R6, then a C-R6 is CH; R3 is methyl; R4 is hydroxy; R5 and R5 'are the same or different and are, independently of each other, a hydrogen atom, or a C1-6 alkyl, C3-6 cycloalkyl-C1-6 alkyl, or C1-6 alkoxy-C1-6 alkyl, or R5 and R5 ', taken together with the nitrogen atom to which they are attached, represent a 3- to 7-membered nitrogen-containing heterocyclic ring that optionally contains at least one additional heteroatom selected from oxygen, nitrogen or sulfur and which may be optionally substituted with 1 or more R6 'groups; the instances of R6 may be the same or different and are independently a hydrogen atom, a halogen atom, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkyl C1-6, aryl, aryl-C1-6 alkyl, heteroaryl, heteroaryl-C1-6 alkyl, heterocyclic ring of 3-8 members, heterocyclyl-C1-6 alkyl of 3-8 members, -C 1-6 alkyl- OR7, -C1-6-SR7 alkyl, -C1-6-N-alkyl (R7) (R7 '), -C1-6-C alkyl (= O) R7, -CN, -C (= O) OR7, - C (= O) N (R7) (R7 '), -OR7, -SR7, -N (R7) (R7'), or -NR7C (= O) R7 each of which may be optionally substituted with 1 or more R8 groups; the instances of R6 ’can be the same or different and are independently C1-6 alkyl, C3-6 cycloalkyl-C1-6 alkyl, or C1-6-OR7 alkyl; the instances of R7 and R7 'may be the same or different and are independently a hydrogen atom, or a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkyl C 1-6, C 3-6 cycloalkenyl, aryl, C 1-6 alkyl aryl, heteroaryl, 3- and 8-membered heterocyclic ring, C 1-6 heterocyclyl-C 3-6 alkyl, or C 1-6 heteroaryl-alkyl; the instances of R8 are independently a halogen atom, or nitro, hydroxy, cyano, formyl, acetyl, amino, C1-6 alkyl, C1-6 alkoxy, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl , C3-6 cycloalkyl-C 1-6 alkyl, C 1-6 cycloalkenyl, aryl, aryl-C 1-6 alkyl, heteroaryl, 3- and 8-membered heterocyclic ring, heterocyclyl-C 1-6 alkyl, or heteroaryl-C 1-6 alkyl ; n is the integer 1 and m is the integer 1; with the proviso that when: said R5 and R5 ', taken together with the nitrogen atom to which they are attached, represent the remainder of formula (3) where * represents the point of attachment with the rest of the structure of the general formula (1), then said R2 heteroaryl of structure of formula (2) is not a residue of formula (4) wherein * represents the point of attachment with the rest of the structure of general formula (1); or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate or a salt thereof, in particular a physiologically acceptable salt, or a mixture thereof. Claim 17: A compound of the general formula (5) wherein R1 and R3 are as defined for the general formula (1) in any of claims 1 to 9. |
| priorityDate | 2010-11-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 45.