http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-068889-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/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D493-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 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/C07D471-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D231-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
| filingDate | 2008-10-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2009-12-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-068889-A1 |
| titleOfInvention | COMPOUNDS TO INHIBIT THE ACTIVITY OF KSP KINESINA |
| abstract | The present further relates to compositions (including compositions acceptable for pharmaceutical use) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for use in inhibiting the activity of the kinesin KSP, and to treat cell proliferative diseases or disorders associated with the activity of the KSP kinesin. Claim 1: A compound having the general structure shown in formula (1), or a salt, solvate, ester, prodrug, or isomer acceptable for pharmaceutical use thereof; where R1, R2, R3, p, R27, R28, E, ring A, and ring B are independently selected from each other and where p is 0, 1, 2, 3 or 4; Ring A (which includes E and the unsaturation shown) is a 4- to 8-membered heterocycloalkenyl or cycloalkenyl ring; E is selected from the group consisting of -O-, -S-, -S (O) -, -S (O) 2-, -C (R4) (R5) -, -N (R6) -, -N ( C (Y) R7) -, -N (C (Y) OR8) -, -N (C (Y) N (R9) (R10)) -, -C (O) N (R11) -, -N ( R11) -C (O) -, -S (O) 2-N (R11) -, -N (R11) -S (O) 2-, -C (O) -O-, -OC (O, - ON (R6) -, -N (R6) -O-, -N (R6) -N (R12) -, -N = N-, -C (R7) = N-, -C (O) -C ( R7) = N-, -C (O) -N = N-, -OC (Y) -N (R11) -, -N (R11) -C (Y) -O-, -N (R11) -C (Y) -N (R12) -, -C (Y) -N (R11) -O-, -C (Y) N (R11) -N (R12) -, -ON (R11) -C (Y) -, and -N (R12) -N (R11) -C (Y) -, where each Y is independently selected from the group consisting of (= O), (= S), (= N (R13)), (= N (CN)), (= N (OR14)), (= N (R15) (R16)), and (= C (R17) (R18)); Ring B is an aromatic or heteroaromatic ring, or a ring partially unsaturated alicyclic, or a partially unsaturated heterocyclic ring, wherein said ring is unsubstituted or optionally substituted independently with one or more substituents, which may be the same or different, each substituent is independently selected from the halogen integrated group, -CN, - NO2, alkyl , heteroalkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, aryl, heteroaryl, aryl-alkyl-, heteroaryl-alkyl-, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, azido, -OR19, -OC (O) OR20, -NR21, -NR21, -NR21 -NR23SO2R24, -NR23C (O) OR20, -NR23C (O) R24, -SO2NR25R26, -C (O) R24, -C (O) OR20, -SR19, -S (O) R19, -SO2R19, -OC ( O) R24, -C (O) NR25R26, -NR23C (N-CN) NR25R26 and -NR23C (O) NR25R26; R1 is selected from the group consisting of aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl, where each said aryl, each said heteroaryl, each said cycloalkyl, each said cycloalkenyl, each said heterocycloalkyl, and each said heterocycloalkenyl is unsubstituted or optionally independently substituted with one or more substituents, which may be the same or different, each substituent is independently selected from the group consisting of halogen, -CN, -NO2, alkyl, heteroalkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, aryl, heteroaryl , aryl-alkyl-, heteroaryl-alkyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, azido, -OR19, -OC (O) OR20, -NR21R22, -NR23SO2R24, -NR23C (O) OR20, -NR23C (O) R24, -SO2NR25R26, C (O) R24, -C (O) OR20, -SR19, -S (O) R19, -SO2R19, -OC (O) R24, -C (O) NR25R26, -NR23C (N-CN) NR25R26 and -NR23C (O) NR25R26; R2 is selected from the group consisting of -C (Z) R7, -C (Z) NR9R10, -C (Z) OR8, -SO2NR9R10, alkyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl, where each Z is independently selected from the group consisting of (= O), (= S), (= N (R13)), (= N (CN)), (= N (OR14), (= N (R15) (R16) ), and (= C (R17) (R18)), and where each said alkyl, each said heteroalkyl, each said aryl, each said heteroaryl, each said cycloalkyl, each said cycloalkenyl, each said heterocycloalkyl, and each said heterocycloalkenyl is not substituted or optionally substituted independently with one or more substituents, which may be the same or different, each substituent is independently selected from the group consisting of oxo (with the proviso that said aryl and said heteroaryl are not substituted with oxo), halogen, -CN , -NO2, alkyl, heteroalkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, aryl, heteroaryl, aryl -alkyl, heteroaryl-alkyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, azido, -OR19, -OC (O) OR20, -NR21R22, -NR23SO2R24, -NR23C (O) OR20, -NR23C (O) R24, -SO2NR2526 -C (O) R24, -C (O) OR20, -SR19, -S (O) R19, -SO2R19, -OC (O) R24, -C (O) NR25R26, -NR23C (N-CN) NR25R26 and -NR23C (O) NR25R26; R27 (when not bound with R28) is independently selected from the group consisting of H, alkyl, heteroalkyl, alkenyl, heteroalkenyl, alkynyl, heteroalkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, halogen, -CN, -NO2, -OR19, -OC (O) OR20, -NR21R22, -NR23SO2R24, -NR23C (O) OR20, -NR23C (O) R24, -SO2NR25R26, -C (O) R24, -C (O) OR20, -SR19, -S (O) R19, -SO2R19, -OC (O) R24, -C (O) NR25R26, -NR23C (N-CN) NR25R26 and -NR23C (O) NR25R26, where each said alkyl, each heteroalkyl, each said alkenyl, each said heteroalkenyl, each said alkynyl, each said heteroalkynyl, each said aryl, each said heteroaryl, each said cycloalkyl, each said cycloalkenyl, each said heterocycloalkyl, and each said heterocycloalkenyl is unsubstituted or optionally substituted independently with one or more substituents, which may be the same or different, each substituent is independently selected from the group of or xo, halogen, -CN, -NO2, alkyl, heteroalkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, azido, -OR19, -OC (O) OR20, -NR21 , -NR23SO2R24, -NR23C (O) OR20, -NR23C (O) R24, -SO2NR25R26, -C (O) R24, -C (O) OR20, -SR19, -S (O) R19, -SO2R19, -OC (O) R24, -C (O) NR25R26, -NR23C (N-CN) NR25R26 and -NR23C (O) NR25R26; R28 (when not bound with R27) is independently selected from the group consisting of H, alkyl, heteroalkyl, alkenyl, heteroalkenyl, alkynyl, heteroalkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, halogen, -CN, -NO2, -OR19, -OC (O) OR20, -NR21R22, -NR23SO2R24, -NR23C (O) OR20, -NR23C (O) R24, -SO2NR25R26, -C (O) R24, -C (O) OR20, -SR19, -S (O) R19, -SO2R19, -OC (O) R24, -C (O) NR25R26, -NR23C (N-CN) NR25R26 and -NR23C (O) NR25R26, where each said alkyl, each heteroalkyl, each said alkenyl, each said heteroalkenyl, each said alkynyl, each said heteroalkynyl, each said aryl, each said heteroaryl, each said cycloalkyl, each said cycloalkenyl, each said heterocycloalkyl, and each said heterocycloalkenyl is unsubstituted or optionally substituted independently with one or more substituents, which may be the same or different, each substituent is independently selected from the group of or xo, halogen, -CN, -NO2, alkyl, heteroalkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, azido, -OR19, -OC (O) OR20, -NR21 , -NR23SO2R24, -NR23C (O) OR20, -NR23C (O) R24, -SO2NR25R26, -C (O) R24, -C (O) OR20, -SR19, -S (O) R19, -SO2R19, -OC (O) R24, -C (O) NR25R26, -NR23C (N-CN) NR25R26 and -NR23C (O) NR25R26; or alternatively, R27 and R28, together with the carbon atom to which they are attached, form a cycloalkyl, cycloalkenyl, heterocycloalkyl ring containing one to three heteroatoms selected from the group consisting of N, O, and S, or a heterocycloalkenyl ring which they contain one to three heteroatoms selected from the group consisting of N, O, and S, wherein said heterocycloalkyl ring and said heterocycloalkenyl ring are each unsubstituted or optionally substituted independently with one or more substituents, which may be the same or different , each substituent is independently selected from the group of oxo, halogen, -CN, -NO2, alkyl, heteroalkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, aryl, heteroaryl, aryl-alkyl, heteroaryl-alkyl-, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, azido, -OR19, -OC (O) OR20, -NR21R22, -NR23SO2R24, -NR23C (O) OR20, -NR23C (O) R24, -SO2NR25R26, -C (O) R2 4, -C (O) OR20, -SR19, -S (O) R19, -SO2R19, -OC (O) R24, -C (O) NR25R26, -NR23C (N-CN) NR25R26 and -NR23C (O) NR25R26; each R3 (when present) is independently selected from the group consisting of alkyl, heteroalkyl, alkenyl, heteroalkenyl, alkynyl, heteroalkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, halogen, -CN, -NO2, -OR19, - OC (O) OR20, -NR21R22, -NR23SO2R24, -NR23C (O) OR20, -NR23C (O) R24, -SO2NR25R26, -C (O) R24, -C (S) R24, -C (O) OR20, -SR19, -S (O) R19, -SO2R19, -OC (O) R24, -C (O) NR25R26, -NR23C (N-CN) NR25R26, -NR23C (O) NR25R26, and -NR23-C (NH ) -N (R26) 2, wherein each said alkyl, each said heteroalkyl, each said alkenyl, each said heteroalkenyl, each said alkynyl, each said heteroalkynyl, each said aryl, each said heteroaryl, each said cycloalkyl, each said cycloalkenyl, each said heterocycloalkyl, and each said heterocycloalkenyl is unsubstituted or optional and independently substituted with one or more substituents, which may be the same or different, each substituent is independently selected The group consisting of oxo, halogen, -CN, -NO2, alkyl, heteroalkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, azido, -OR19, -OC (O ) OR20, -NR21R22, -NR23SO2R24, -NR23C (O) OR20, -NR23C (O) R24, -SO2NR25R26, -C (O) R24, -C (O) OR20, -SR19, -S (O) R19, -SO2R19, -OC (O) R24, -C (O) NR25R26, -NR23C (N-CN) NR25R26 and -NR23C (O) NR25R26, or, alternatively, when p is 2, 3 or 4, either R3 groups attached to the same carbon atom of the ring are taken j |
| priorityDate | 2007-11-09-04:00^^<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: 27.