http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2529545-T3
Outgoing Links
Predicate | Object |
---|---|
assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f2d3599fb8f8f479dba95ca9bb504884 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4353 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D221-12 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-473 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D221-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
filingDate | 2009-03-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2015-02-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_25052811a40d6b7a6b195b8de3cf746e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_58f8734e3bfcfe863c6884d05d091a4e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ac338f51f0f5349757af6345d4d825f9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b73724436321e6ab815deed69a92cfe2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_031ebb2943255bc6cbb8629da2b6d2c5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ca295cbf7dfd579aff0184e3d6882b35 |
publicationDate | 2015-02-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | ES-2529545-T3 |
titleOfInvention | Tetrahydrofenantridinones and tetrahydrocyclopentaquinolinones as inhibitors of tubulin and PARP polymerization |
abstract | Compound of formula (I), ** Formula ** including a stereochemically isomeric form thereof; wherein Y is CH2 or CH2-CH2; R1 is aryl or Het; in which aryl is phenyl or naphthalenyl; in which Het is thienyl, pyrrolyl, pyrrolinyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, tetrazolyl, thiadiazolyl, furanyl, piperidinyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrimidinyl, triazinyl, triazinyl, aryrazinyl, pyrimidinyl, triazinyl, aryrazinyl, pyrimidininyl, pyrimidinyl, pyrimidininyl, Pyrimidinyl, Inrazin, Pyrimidininyl, Pyrazinyl, Inrazin, Pyrimidinyl, Inrazin, Pyrimidinyl, Inrazinyl, Inrazine, Pyrimidinyl, Inrazine, Pyrimidinyl, Inrazin, Pyrimidinyl, Inrazin, Pyrimidinyl, Inrazinyl, Inrazinyl, Inrazine , indolyl, indolinyl, benzothienyl, indazolyl, benzoxazolyl, benzimidazolyl, benzofuranyl, benzothiazolyl, benzotriazolyl, chromanyl, purinyl, quinolinyl, cinolinyl, phthalazinyl, quinazolinyl, quinoxazolinyl, naphthyridinyl; two carbon atoms in aryl or Het may be bridged (ie, form a bi or tricyclic moiety) with a bivalent radical selected from -O-CH2-CH2-O- (a-1), -CH2-O- CH2-O- (a-2), -O-CH2-CH2-CH2- (a-3), -O-CH2-CH2-NR8- (a-4), -O-CR8 2-O- (a -5), -O-CH2-CH2- (a-6), -CH2-N-CH2-CH2- (a-7), - (CH2) 3- (a-8), or - (CH2) 4 - (a-9); each aryl, Het, bridge-linked aryl or bridge-linked Het may be substituted with one, two, three, four or five substituents each independently selected from halo, cyano, nitro, hydroxycarbonyl, C1-6 alkyl, C2-6 alkenyl , C2-6 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkylamino, methylethylamino, C3-6 aminocycloalkyl, C1-6 haloalkyl, C1-6 trihaloalkyl, C1-6-carbonyl, C2-6-carbonyl alkyloxy, C2- alkenyl 6-carbonyl, oxime, C1-6-oxime alkyl, amidoxime, -CC-CH2O-CH3, -CC-CH2N (CH3) 2, -CC-Si (CH3) 3, C1-6 hydroxyalkyl, C2-6 hydroxyalkenyl, C2-6 hydroxyalkynyl, C1-6 cyanoalkyl, C2-6 cyanoalkenyl, C1-6 aminocarbonylalkyl, C1-6 alkylsulfonyl C1-6 alkyl, C1-6 alkylsulfonyl C1-6 alkylsulfonyl, C2-6 alkylsulfonyl, -PO (O-C1-6 alkyl) 2, -B (OH) 2, -S-CH3, SF5, C1-6 alkylsulfonyl, -NR8R9, -C 1-6 alkyl-NR8R9, -OR8, C1-6 alkyl OR8, -CONR8R9, piperidinylalkyl C1-6, piperazinylalkyl C1-6, alkyl C1-6-piperazinylalkyl C1-6, morpholi C1-6 n-alkyl, piperidinyl, piperazinyl, C1-6 alkyl-piperazinyl, morpholinyl, phenyl, thienyl, pyrazolyl, pyrrolyl, pyrrolidinyl, pyridinyl, pyrimidinyl, oxadiazolyl, imidazolyl, imidazolylalkyl-C2-6alkyl-C1-6 imidazol cyanopyridinyl, phenylC 1-6 alkyl, phenylC2-6 alkyl, morpholinylC1-6 alkyl, C1-6 alkyloxyphenyl, trihaloalkylC 1-6 phenyl, methylpyrazolyl, halopyrimidinyl or dimethylaminopyrrolidinyl; or R1 is a radical of formula ** Formula ** in which X1 is CH2, NH or N-CH3; wherein X2 is CH2, C> = O, O, NH or N-CH3; wherein R 10 is phenyl, pyridinyl, pyridazinyl or pyrimidinyl, in which each phenyl, pyridinyl, pyridazinyl or pyrimidinyl can be substituted with one or two substituents each independently selected from halo, hydroxyl, cyano, C 1-6 alkyl, amino, C1-6 polyhaloalkyl or C1-6 alkyloxy; or R1 is a radical of formula ** Formula ** in which X3 is CH or N; R2 is methyl, ethyl, propyl or C3-6 cycloalkyl; each R3 and R4 is independently selected from hydrogen, methyl, ethyl, propyl, hydroxy, trifluoromethyl, methyl oxyl; or R3 and R4 are taken together with the carbon atom to which they are attached to form a cyclopropyl ring or a radical of formula C (> = O); each R5 and R6 is independently selected from hydrogen, halo, C1-6 alkyloxy, cyano, C1-6 alkyl, -OCH2CH2NR8R9, -CH2OCH2CH2NR8R9, -OCH2CH2CH2NR8R9; R7 is hydrogen, methyl or fluorine; each R8 and R9 is independently selected from hydrogen, halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, carbonyl, C1-6 alkylsulfonyl-C1-6 alkyl, C1-6 alkyloxy-C1-6 alkyl, hydroxyalkyl C1-6, dihydroxyalkyl C1-6, cyanoalkyl C1-6, trihaloalkyl C1-6, phenylalkyl C1-6, di (C1-6 alkyl) aminoalkyl C1-6, alkylsulfonyl C1-6, morpholinyl alkyl C1-6, morpholinylcarbonyl, piperazinylalkyl C1 -6, C1-6 alkyl-piperazinylalkyl C1-6 alkyl, piperidinylalkyl C1-6, thiomorpholinyl alkyl C1-6, cycloalkyl C3-6-methyl, pyridinyl, pyrimidinyl, phenyl, halophenyl, oxanylalkyl C1-6, alkylsulfonyl C1-6-alkyl -6 or C1-6 alkylcarbonylaminoC 1-6 alkyl; an N-oxide form thereof, pharmaceutically acceptable addition salts thereof and solvates thereof. |
priorityDate | 2008-03-27-04:00^^<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: 1096.