http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-068048-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a7f82940e47ba7a1188f8e2ffca55e0f |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4365 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-517 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-337 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 |
| filingDate | 2008-07-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2009-11-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-068048-A1 |
| titleOfInvention | COMBINATION OF ANTIMITOTIC AGENT AND INHIBITOR OF AURORA QUINASA AS ANTICANCERIGENO TREATMENT |
| abstract | Claim 1: A pharmaceutical composition for treating or improving cancer, comprising in combination (a) at least one antifungal agent selected from the group consisting of a taxane, paclitaxel, docetaxel, a Cenp-E inhibitor, abraxane, epothilone, monastrol, an inhibitor of KSP, ispinesib and a compound of the formulas (A) - (D) shown in points a) - d) below: a) A compound represented by the structural formula (A) or one of its salts , pharmaceutically acceptable solvates or esters, wherein the Y ring is a 5 or 6 membered aryl or a fused 5 or 6 membered heteroaryl as indicated in formula (A), wherein in said aryl and heteroaryl each carbon of the Replaceable ring is independently substituted with R2 and each nitrogen in the replaceable ring is independently substituted with R6; W is N or C (R12); X is N or N-oxide; Z is S, S (= O) or S (= O) 2; R1 is H, alkyl, alkoxy, hydroxy, halo, -CN, -S (O) m-alkyl, -C (O) NR9R10, - (CR9R10) 1-6OH or -NR4 (CR9R10) 1-2OR9; each R2 is independently selected from the group consisting of H, halo, alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, - (CR10R11) 0-6-OR7, -C (O ) R4, -C (S) R4, -C (O) OR7, -C (S) OR7, -OC (O) R7, -OC (S) R7, -C (O) NR4R5, -C (S) NR4R5, -C (O) NR4OR7, -C (S) NR4OR7, -C (O) NR7NR4R5, -C (S) NR7NR4R5, -C (S) NR4OR7, -C (O) SR7, -NR4R5, -NR4C ( O) R5, -NR4C (S) R5, -NR4C (O) OR7, -NR4C (S) OR7, -OC (O) NR4R5, -OC (S) NR4R5, -NR4C (O) NR4R5, -NR4C (S ) NR4R5, -NR4C (O) NR4OR7, -NR4C (S) NR4OR7, - (CR10R11) 0-6SR7, -SO2R7, -S (O) 1-2NR4R5, -N (R7) SO2R7, -S (O) 1 -2NR5OR7, -CN, -OCF3, -SCF3, -C (= NR7) NR4, -C (O) NR7 (CH2) 1-10NR4R5, -C (O) NR7 (CH2) 1-10OR7, -C (S ) NR7 (CH2) 1-10NR4R5, -C (S) NR7 (CH2) 1-10OR7, haloalkyl and alkylsilyl, wherein each of said alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, aralkyl, heteroaryl or heteroarylalkyl is optionally substituted, independently, with 1-5 R9 residues; each R3 is independently selected from the group consisting of H, halo, alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, - (CR10R11) 0-6-OR7, -C (O ) R4, -C (S) R4, -C (O) OR7, -C (S) OR7, -OC (O) R7, -OC (S) R7, -C (O) NR4R5, -C (S) NR4R5, -C (O) NR4OR7, -C (S) NR4OR7, -C (O) NR7NR4R5, -C (S) NR7NR4R5, -C (S) NR4OR7, -C (O) SR7, -NR4R5, -NR4C ( O) R5, -NR4C (S) R5, -NR4C (O) OR7, -NR4C (S) OR7, -OC (O) NR4R5, -OC (S) NR4R5, -NR4C (O) NR4R5, -NR4C (S ) NR4R5, -NR4C (O) NR4OR7, -NR4C (S) NR4OR7, - (CR10R11) 0-6SR7, SO2R7, -S (O) 1-2NR4R5, -N (R7) SO2R7, -S (O) 1- 2NR5OR7, -CN, -OCF3, -SCF3, -C (= NR7) NR4R5, -C (O) NR7 (CH2) 1-10NR4R5, -C (O) NR7 (CH2) 1-10OR7, -C (S) NR7 (CH2) 1-10NR4R5, -C (S) NR7 (CH2) 1-10OR7, haloalkyl and alkylsilyl, wherein each of said alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, aralkyl, heteroaryl or heteroaralkyl is optionally independently replaced with 1-5 R9 residues; each R4 and R5 is independently selected from the group consisting of H, alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, -OR7, -C (O) R7 and -C (O ) OR7, wherein each of said alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, aralkyl, heteroaryl or heteroaralkyl is optionally substituted with 1-4 R8 moieties; or R4 and R5, when attached to the same nitrogen atom, are optionally taken together with the nitrogen atom to which they are attached to form a 3-6 membered heterocyclic ring having 0-2 additional heteroatoms selected from N, O or S; each R6 is independently selected from the group consisting of H, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroaralkyl, - (CH2) 1-6CF3, -C (O) R7, - C (O) OR7 and -SO2R7; each R7 is independently selected from the group consisting of H, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl and heteroaralkyl, wherein each member of R7 except H is optionally substituted with 1-4 residues R8; each R8 is independently selected from the group consisting of halo, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, -NO2, -OR10, - (C1-6 alkyl) -OR10, -CN, -NR10R11, -C (O) R10, -C (O) OR10, -C (O) NR10R11, -CF3, -OCF3, -CF2CF3, -C (= NOH) R10, -N (R10) C (O) R11, -C ( = NR10) NR10R11 and -NR10C (O) OR11, wherein each of said alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl is optionally substituted, independently, with 1-3 moieties selected from the group consisting of halo, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, -NO2, -OR10, - (C1-6 alkyl) -OR10, -CN, -NR10R11, -C (O) OR10, -C (O) NR10R11, -CF3, -OCF3, -NR10C (O) OR11 and -NR10 (O) R40; or two R8 groups, when attached to the same carbon atom, are optionally taken together with the carbon atom to which they are attached to form a C = O group or a C = S group; each R9 is independently selected from the group consisting of H, alkyl, alkoxy, OH, CN, halo, - (CR10R11) 0-4NR4R5, haloalkyl, hydroxyalkyl, alkoxyalkyl, -C (O) NR4R5, -C ( O) OR7, -OC (O) NR4R5, -NR4C (O) R5 and -NR4C (O) NR4R5; each R10 is, independently, H or alkyl; or R9 and R10, when attached to the same nitrogen atom, are optionally taken together with the nitrogen atom to which they are attached to form a 3-6 membered heterocyclic ring having 0-2 additional heteroatoms selected from N, O or S; each R11 is, independently, H or alkyl; or R10 and R11 when attached to the same nitrogen atom, are optionally taken together with the nitrogen atom to which they are attached to form a 3-6 membered heterocyclic ring having 0-2 additional heteroatoms selected from N, O or S ; each R12 is independently selected from the group consisting of H, halo, alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, - (CR10R11) 0-6-OR7, -C (O ) R4, -C (S) R4, -C (O) OR7, -C (S) OR7, -OC (O) R7, -OC (S) R7, -C (O) NR4R5, -C (S) NR4R5, -C (O) NR4OR7, -C (S) NR4OR7, -C (O) NR7NR4R5, -C (S) NR7NR4R5, -C (S) NR4OR7, -C (O) SR7, -NR4R5, -NR4C ( O) R5, -NR4C (S) R5, NR4C (O) OR7, -NR4C (S) OR7, -OC (O) NR4R5, -OC (S) NR4R5, -NR4C (O) NR4R5, -NR4C (S) NR4R5, -NR4C (O) NR4OR7, -NR4C (S) NR4OR7, - (CR10R11) 0-6SR7, SO2R7, -S (O) 1-2NR4R5, -N (R7) SO2R7, -S (O) 1-2NR5OR7 , -CN, -OCF3, -SCF3, -C (NR7) NR4, -C (O) NR7 (CH2) 1-10NR4R5, -C (O) NR7 (CH2) 1-10OR7, -C (S) NR7 ( CH2) 1-10NR4R5, -C (S) NR7 (CH2) 1-10OR7, haloalkyl and alkylsilyl, wherein each of said alkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, aryl, aralkyl, heteroaryl or heteroarylalkyl is optionally substituted, independently, with 1-5 R9 residues; and R40 is selected from the group consisting of cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein each of said cycloalkyl, heterocyclyl, aryl and heteroaryl is optionally substituted, independently, with 1-3 moieties selected, independently, from the group consisting of -CN, -OH, halo, alkyl, haloalkyl, alkoxy and -NR10R11; b) A compound represented by structural formula (B) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the Y ring is a 5- to 7-membered ring selected from the group consisting of cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclyl fused as indicated in formula (B), wherein in each of said 5 to 7 member rings, each carbon of the replaceable ring is independently substituted with 1-2 R2 moieties and each heteroatom of the replaceable ring it is substituted, independently, with R6; W is N or C (R12); X is N or N-oxide; Z is S, S (= O) or S (= O) 2; R1 is H, alkyl, alkoxy, hydroxy, halo, -CN, -S (O) m-alkyl, -C (O) NR9R10, - (CR9R10) 1-6OH or -NR4 (CR9R10) 1-2OR9; where m is 0 to 2; each R2 is independently selected from the group consisting of H, halo, alkyl, cycloalkyl, alkylsilyl, cycloalkenyl, heterocyclyl, heterocyclynyl, aryl, heteroaryl, - (CR10R11) 0-6-OR7, -C (O) R4 , -C (S) R4, -C (O) OR7, -C (S) ORT, -OC (O) R7, -OC (S) R7, -C (O) NR4R5, -C (S) NR4R5, -C (O) NR4OR7, -C (S) NR4OR7, -C (O) NR7NR4R5, -C (S) NR7NR4R5, -C (S) NR4OR7, -C (O) SR7, -NR4R5, -NR4C (O) R5, -NR4C (S) R5, -NR4C (O) OR7, -NR4C (S) OR7, -OC (O) NR4R5, -OC (S) NR4R5, -NR4C (O) NR4R5, -NR4C (S) NR4R5 , -NR4C (O) NR4OR7, -NR4C (S) NR4OR7, - (CR10R11) 0-6SR7, SO2R7, -S (O) 1-2NR4R5, -N (R7) SO2R7, -S (O) 1-2NR5OR7, -CN, -OCF3, -SCF3, -C (= NR7) NR4, -C (O) NR7 (CH2) 1-10NR4R5, -C (O) NR7 (CH2) 1-10OR7, -C (S) NR7 ( CH2) 1-10NR4R5 and -C (S) NR7 (CH2) 1-10OR7, wherein each of said alkyl, cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclynyl, aryl and heteroaryl is optionally substituted, independently, with 1-5 R9 residues; or two R2 groups on the same carbon atom are optionally taken together with the carbon atom to which they are attached to form a C = O group, a C = S group or an ethylenedioxy group; R3 is independently selected from the group consisting of H, halo, alkyl, cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclynyl, aryl, heteroaryl, - (CR10R11) 0-6-OR7, -C (O) R4, -C (S) R4, -C (O) OR7, -C (S) OR7, -OC (O) R7, -OC (S) R7, -C (O) NR4R5, -C (S) NR4R, -C ( O) NR4OR7, -C (S) NR4OR7, -C (O) NR7NR4R5 -C (S) NR7NR4R5, -C (S) NR4OR7, -C (O) SR7, -NR4R5, -NR4C (O) R5, -NR4C (S) R5, -NR4C (O) OR7, -NR4C (S) OR7, -OC (O) NR4R5, -OC (S) NR4R5, -NR4C (O) NR4R5, -NR4C (S) NR4R5, -NR4C ( O) NR4OR7, -NR4C (S) NR4OR7, - (CR10R11) 0-6SR7, SO2R7, -S (O) 1-2NR4R5, -N (R7) SO2R7, -S (O) 1-2NR5OR7, -CN, - C (= NR7) NR4R5, -C (O) N (R7) - (CR40R41) 1-5-C (= NR7) NR4R5, -C (O) N (R7) (CR40R41) 1-5-NR4R5-C (O) N (R7) (CR40R41) 1-5-C (O) -NR4R5, -C (O) N (R7) (CR40R41) 1-5-OR7, -C (S) NR7 (CH2) 1- 5NR4R5 and -C (S) NR7 (CH2) 1-5OR7, wherein each of said alkyl, cycloalkyl, cycloalkenyl, heter |
| priorityDate | 2007-07-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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