http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-053710-A1
Outgoing Links
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|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_5f1a30682c7f24ace5f2b16c6be633b6 |
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| filingDate | 2006-04-10^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9a9aa7a6bf971c3c610d436e5e30a92d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_51547a446d5dab797f99713edb65a38f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_93f1e2651efa477955d58c41f4af90f1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0f44c6bbbb289979de3cf66b45ed2e12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_144cb1bf2265347e26d7d6a7a2dddcd1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_205b1cba70ea514adc01bb1a2b31a899 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b8bc048767a20715b9e9261abceb1ec3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7ca360c76618224603b9c93abdfb5103 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3fc4c3789558266bf53ee8a01799ee6d |
| publicationDate | 2007-05-16^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-053710-A1 |
| titleOfInvention | SPIROHETEROCICLIC COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS |
| abstract | These are useful for the treatment and / or prevention of diseases or conditions mediated by sodium channels, such as pain. Pharmaceutical compositions comprising the compounds and methods for preparing and using the compounds. Claim 1: A compound of formula (1), wherein: p is between 1 and 4; j and k are each independently 0, 1, 2 or 3; Q is - C (R1a) H-, -C (O) -, -O-, -S-, -N (R5) -, -CF2-, -C (O) O-, -C (O) N (R5) - or -N (R5) C (O) -; R1a is hydrogen or -OR5; formula (2) is a fused heteroaryl ring or a fused heterocyclyl ring; R1 is hydrogen, alkyl, alkenyl, alkynyl, halalkyl, aryl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, -R8-OR5, -R8-CN, -R9- P (O) (OR5) 2, or -R9-O- R9-OR5; or R1 is aralkyl substituted with -C (O) N (R6) R7 where: R6 is hydrogen, alkyl, aryl or aralkyl; and R7 is hydrogen, alkyl, haloalkyl, -R9-CN, -R9-OR5, -R9-N (R4) R5, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; or R6 and R7, together with the nitrogen to which they are attached, form a heterocyclyl or heteroaryl; and where each aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl and heteroaryl group for R6 and R7 may be optionally substituted with one or more substituents selected from the group consisting of alkyl, cycloalkyl, aryl, aralkyl, halo, haloalkyl , -R8-CN, -R8-OR5, heterocyclyl and heteroaryl; or R1 is aralkyl optionally substituted with -R8-OR5, -C (O) OR5, halo, haloalkyl, alkyl, nitro, cyano, aryl (optionally substituted with cyano), aralkyl (optionally substituted with one or more alkyl groups), heterocyclyl or heteroaryl; or R1 is -R9-N (R10) R11, -R9-N (R12) C (O) R11 or -R9-N (R10) C (O) N (R10) R11 where: each R10 is hydrogen, alkyl, aryl or aralkyl; each R11 is hydrogen, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl, -R9-OC (O) R5, -R9-C (O) OR5, -R9-C (O) N (R4) R5, -R9-C (O) R5, -R9-OR5, or -R9-CN; R12 is hydrogen, alkyl, aryl, aralkyl or -C (O) R5; and wherein each aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl and heteroarylalkyl group for R10 and R11 may be optionally substituted with one or more substituents selected from the group consisting of alkyl, cycloalkyl, aryl, aralkyl, halo, haloalkyl , nitro, -R8-CN, -R8-OR5, -R8-C (O) R5, heterocyclyl and heteroaryl; or R1 is heterocyclylalkyl or heteroarylalkyl where the heterocyclylalkyl or heteroaryl group is optionally substituted with one or more substituents selected from the group consisting of alkyl, halo, haloalkyl, -R8-OR5, -R8-C (O) OR5, aryl and aralkyl ; each R2 is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, alkoxy, halo, haloalkyl, haloalkenyl, haloalkoxy, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroaryl-heteroaryl-heteroaryl-heteroaryl R8-CN, -R8-NO2, -R8-OR5, -R8-N (R4) R5, -N = C (R4) R5, -S (O) mR4, - R8-C (O) R4; -C (S) R4, -C (R4) 2C (O) R5, -R8-C (O) OR4, -C (S) OR4, -R8-C (O) N (R4) R5, -C ( S) N (R4) R5, -N (R5) C (O) R4, -N (R5) C (S) R4, -N (R5) C (O) OR4, -N (R5) C (S) OR4, -N (R5) C (O) N (R4) R5, - N (R5) C (S) N (R4) R5, -N (R5) S (O) nR4, -N (R5) S ( O) nN (R4) R5, -R8-S (O) nN (R4) R5, - N (R5) C (= NR5) N (R4) R5, and -N (R5) C (= N-CN) N (R4) R5, where each m is independently 0, 1, or 2 and each n is independently 1 or 2; and wherein each of the cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl and heteroarylalkyl groups for each R2 may be optionally substituted with one or more substituents selected from the group consisting of alkyl, alkenyl, alkynyl, alkoxy , halo, haloalkyl, haloalkenyl, haloalkoxy, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl, -R8-CN, -R8-NO2, -R8-OR5, -R8-N (R8-N) , -S (O) mR4, -R8-C (O) R4; -R8-C (O) OR4, -R8- C (O) N (R4) R5, -N (R5) C (O) R4, and -N (R5) S (O) nR4, where each m is in independently 0, 1 or 2 and each n is independently 1 or 2; or two adjacent R2 groups, together with the fused heteroaryl ring or the fused heterocyclyl ring to which they are directly attached, can form a fused ring selected from cycloalkyl, aryl, heterocyclyl and heteroaryl, and the remaining R2 groups, if present, are as has been described; R3a, R3b, R3c and R3d are independently selected from each other from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, alkoxy, halo, haloalkyl, haloalkenyl, haloalkoxy, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl, -R8-CN, -R8-NO2, -R8-OR5, -R8-N (R4) R5, -N = C (R4) R5, -S (O) mR4, -R8-C (O) R4; -C (S) R4, -C (R4) 2C (O) R5, -R8-C (O) OR4, -C (S) OR4, -R8-C (O) N (R4) R5, -C ( S) N (R4) R5, -N (R5) C (O) R4, -N (R5) C (S) R4, -N (R5) C (O) OR4, -N (R5) C (S) OR4, -N (R5) C (O) N (R4) R5, - N (R5) C (S) N (R4) R5, -N (R5) S (O) nR4, -N (R5) S ( O) nN (R4) R5, -R8-S (O) nN (R4) R5, -N (R5) C (= NR5) N (R4) R5, and -N (R5) C (N = C (R4 ) R5) N (R4) R5, where each m is independently 0, 1 or 2 and each n is independently 1 or 2; or R3a and R3b, or R3b and R3c, or R3c and R3d, together with the carbon atoms of the ring to which they are directly attached, can form a fused ring selected from cycloalkyl, heterocyclyl, aryl or heteroaryl, and R3a groups, R3b, R3c or R3d remaining are as defined; each R4 and R5 is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocyclyl, and heteroaryl; or when R4 and R5 are both attached to the same nitrogen atom, then; R4 and R5, together with the nitrogen atom to which they are attached, can form a heterocyclyl or heteroaryl; and each R8 is a direct bond or a linear or branched alkylene chain, a linear or branched alkenylene chain or a linear or branched alkynylene chain; and each R9 is a linear or branched alkylene chain, a linear or branched alkenylene chain or a linear or branched alkynylene chain; as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or solvates, prodrugs or salts acceptable for pharmaceutical use thereof. |
| priorityDate | 2005-04-11^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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