http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2565983-T3
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_1c89ce4d9ac03f9acd8ddede1162f94d |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D515-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D285-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D515-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 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/A61P17-06 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-433 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D515-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D515-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D285-14 |
filingDate | 2008-10-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2016-04-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0f39b94d2ec376bdaa535186b5e6a373 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4799cb05e14ca0c4cf893182e0025fe0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f7477ab100740cad26f1d62510bf2659 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cffe1e6e237f3e7c2a39a74bd5c98615 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_42302a5741f4f91e2dff3eb5eb71b654 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f9981d90cb73cc1a78965af8ec0ec29b |
publicationDate | 2016-04-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | ES-2565983-T3 |
titleOfInvention | 1,3,4-thiadiazole spiro-condensed derivatives to inhibit the kinesin activity of KSP |
abstract | A compound having the general structure shown in Formula (I), or a pharmaceutically acceptable salt or solvate, ester or pharmaceutically acceptable stereoisomer or geometric isomer thereof: ** Formula ** in which X, R1, R2, R3 , p, E, ring A and ring B are independently selected from each other, and in which: p is 0, 1, 2, 3 or 4; X is selected from the group consisting of S, S (O) and S (O) 2; Ring A (including E and the unsaturation shown) is a 4-8 membered cycloalkenyl or heterocycloalkenyl 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 partially unsaturated alicyclic ring, 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 being substituent 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; R1 is selected from the group consisting of aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl and heterocycloalkenyl, wherein each of said aryl, each of said heteroaryl, each of said cycloalkyl, each of said cycloalkenyl, each of said heterocycloalkyl and each of said heterocycloalkenyl are unsubstituted or optionally substituted independently with one or more substituents, which may be the same or different, each substituent independently being 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, -NR23R22, -NR23R2, -NR23R2, -NR23R2, -NR23R2, -NR23R2, -NR23R2 -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 and -C (Z) OR8, in which 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)); 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, -NR21SO2R24, -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 of said alkyl, each of said heteroalkyl, each of said alkenyl, each of said heteroalkenyl, each of said alkynyl, each of said heteroalkynyl, each of said aryl, each of said heteroaryl, each of said cycloalkyl, each of said cycloalkenyl, each of said heterocycloalkyl, and each of said heterocycloalkenyl are unsubstituted or optionally substituted independently with one or more substitutes ituents, which may be the same or different, each substituent independently being selected from the group 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 (NCN) NR25R26 and -NR23C (O) NR25R26, or, alternatively, when p is 2, 3 or 4, any two R3 groups linked to the same carbon atom of the ring are taken together with the carbon atom to which they are attached to form a spirocycloalkyl ring, a spirocycloalkenyl ring or a spiroheterocycloalkyl ring containing from one to three heteroatoms in the ring independently selected from the group consisting of -NH-, -NR6-, -S-, -S (O) -, -S (O) 2- and -O-, or a spirohete ring rocycloalkenyl containing one to three ring heteroatoms independently selected from the group consisting of -NH-, -NR6-, -S-, -S (O) -, -S (O) 2- and -O-, or, alternatively, R2 and R3, together with the atom to which they are attached, are taken together with the carbon atom to which they are attached to form a cycloalkyl ring, a cycloalkenyl ring, a heterocycloalkyl ring containing one to three heteroatoms in the ring independently selected from the group consisting of -NH-, -NR6-, -S-, -S (O) -, -S (O) 2- and -O-, or a heterocycloalkenyl ring containing one to three heteroatoms in the ring independently selected from the group consisting of -NH-, -NR6-, -S-, -S (O) -, -S (O) 2- and -O-; each R4 (when not bound with R5) 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, |
priorityDate | 2007-10-19-04:00^^<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: 61.