http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-061761-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f2d3599fb8f8f479dba95ca9bb504884 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 |
| filingDate | 2007-06-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2008-09-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-061761-A1 |
| titleOfInvention | TRPV1 THIAZOLOPIRIMIDINE MODULATORS |
| abstract | Certain thiazolopyrimidine compounds are described, which are useful as modulators of TRPV1. Such compounds can be used in pharmaceutical compositions and methods for the treatment of pathological conditions, disorders and conditions mediated by TRPV1, such as pain, arthritis, pruritus, asthma cough or inflammatory bowel disease. Claim 1: A chemical entity selected from (a) compounds of Formula (1): wherein: R1 is -H; -NRaRb; a -C1-6 alkyl, -C1-6 alkyl, -S-C1-6 alkyl or -SO2-C1-6 alkyl unsubstituted or substituted with a substituent -OH, -C1-4alkyl, -NReRf or halo; or a monocyclic cycloalkyl or phenyl group unsubstituted or substituted with a substituent -C 1-6 alkyl, -OH, -C 1-4 alkyl, -NReRf or halo; where Ra and Rb are each independently -H; -C1-6 alkyl; a -C2-3alkyl group substituted with a substituent -OH, -C1-4alkyl, -NRcRd or halo; or a saturated monocyclic cycloalkyl group, -C1-alkyl (saturated monocyclic cycloalkyl), saturated monocyclic heterocycloalkyl, -C1-alkyl (saturated monocyclic heterocycloalkyl), phenyl or benzyl unsubstituted or substituted with one, two or three moieties independently selected from the group consisting of substituents -C 1-6 alkyl, -OH, -C 1-4 alkyl, -NRpRq and halo; or Ra and Rb, taken together with the binding nitrogen in -NRaRb, form a saturated monocyclic heterocycloalkyl group unsubstituted or substituted with one, two or three moieties independently selected from the group consisting of substituents -C1-6 alkyl, -OH, - C1-4alkyl, -NRpRq, halo, -CO2H and benzyl; where Rc and rd are each independently -H or -C1-6 alkyl; or Rc and Rd, taken together with the binding nitrogen in -NRcRd, form a saturated monocyclic heterocycloalkyl; where Rp and Rq are each independently -H or -C1-6 alkyl; or Rp and Rq, taken together with the binding nitrogen in -NRpRq, form a saturated monocyclic heterocycloalkyl; where Re and rf are each independently -H or -C1-6 alkyl; or Re and Rf, taken together with their binding nitrogen in -NReRf, form a saturated monocyclic heterocycloalkyl; R2 is -H or -C 1-6 alkyl; R3 is a monocyclic cycloalkyl, phenyl, benzyl, phenethyl, indanyl, five-membered monocyclic heteroaryl, six-membered monocyclic heteroaryl or -C1-alkyl (monocyclic heteroaryl) unsubstituted or substituted with one, two or three rg substituents; where each Rg substituent is -C1-6 alkyl, -OH, -C1-6 alkyl, phenoxy, -CN, -NO2, -N (Rh) Ri, -C (O) N (Rh) Ri, -N (Rh) C (O) Ri, -N (Rh) SO2C1-6 alkyl, -C (O) C1-6 alkyl, -S (O) 0-2-C1-6 alkyl, -SO2CF3, -SO2N (Rh) Ri, -SCF3, halo , -CF3, -OCF3, -CO2H, -CO2C1-6 alkyl, -C (Rj) 2-OH; or two adjacent Rg substituents taken together form -C1-2O-, -C2-6O- or -C2-6N (Rh) - alkyl; where Rh and Ri are each independently -H or -C1-6 alkyl; where each Rj is independently -H or C1-6 alkyl; R4 is -H or -C 1-6 alkyl; and R5 is a five-membered phenyl, monocyclic heteroaryl or six-membered monocyclic heteroaryl group unsubstituted or substituted with one, two or three Rk substituents; where each Rk substituent is independently -C1-6 alkyl, -OH, -C1-6 alkyl, phenyl, phenoxy, -CN, -NO2, -N (Rl) Rm, -C (O) N (Rl) Rm, -N ( Rl) C (O) Rm, -N (Rl) SO2C1-6 alkyl, -N (Rl) SO2CF3, -C (O) C1-6 alkyl, -S (O) 0-2-C1-6 alkyl, -SO2CF3, - SO2N (Rl) Rm, -SCF3, halo, -CF3, -OCF3, -CO2H or -CO2C1-6 alkyl; or two adjacent Rk substituents taken together form -C1-2O-alkyl; where Rl and Rm are each independently -H or -C1-6 alkyl; and (b) pharmaceutically acceptable salts of the compounds of Formula 1, pharmaceutically acceptable prodrugs of the compounds of Formula 1 and pharmaceutically active metabolites of the compounds of Formula 1. |
| priorityDate | 2006-06-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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