http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-065377-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_8de5520d67b0ce661a2b197ee7f24b57 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 |
| filingDate | 2008-02-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2009-06-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-065377-A1 |
| titleOfInvention | DERIVATIVES OF 4, 5, 6, 7-TETRAHIDRO-PIRAZOLO [3, 4-C] PIRIDINE, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM AND THEIR USE TO TREAT DISEASES MEDIATED BY THE ACTIVITY OF CATEPSINA S. |
| abstract | Carbon-bound tetrahydro-pyrazolo-pyridine compounds are described, which are useful as modulators of cathepsin S. Such compounds can be used in pharmaceutical compositions and for the treatment of medical conditions, disorders, and pathologies mediated by cathepsin S activity, such as psoriasis. , pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis. Claim 1: A compound of Formula (1): wherein: R1 and R2 taken together with the nitrogen atom to which they are attached form a saturated monocyclic heterocycloalkyl group, each group optionally contains an additional member of a heteroatom ring that is O, S, or NRa, and each group is not substituted or is substituted with one, two or substituents Rb; where Ra is H, C1-4 alkyl, -CO C1-4alkyl, -CO (phenyl), or -CO2C1-4alkyl, or a monocyclic cycloalkyl ring, phenyl ring, or monocyclic heteroaryl ring, each ring is unsubstituted or is substituted with OH, C 1-4 alkyl, CF 3, halo, -C 1-4 alkyl, cyano, or -C 1-4 alkyl; and each substituent Rb is independently: i) OH, C1-4 alkyl, -C1-4 alkyl-OH, CF3, NRcRd, halo, -C1-4 alkyl, -C1-4 alkyl, -CO2aC1-4 alkyl, -CO2H , or CONReRf; ii) a monocyclic heterocycloalkyl group unsubstituted or substituted with C1-4alkyl, -COC1-4alkyl, -CO2C1-4alkyl, OH, -C1-4alkyl, NRcRd, or halo; iii) a monocyclic heterocycloalkyl group fused with a phenyl or pyridyl group, the resulting fused cyclic cyclic group is not substituted or substituted with C1-4alkyl, OH, -C1-4alkyl, NRcRd, or halo; or iv) a phenyl group or a monocyclic heteroaryl group, each group is not substituted or substituted with C1-4 alkyl, OH, -C 1-4 alkyl, NRcRd, or halo; or v) two Rb substituents on the same carbon taken together with the carbon to which they are attached form a saturated monocyclic heterocycloalkyl group, unsubstituted or substituted with C1-4alkyl, OH, -C1-4alkyl, NRcRd, or halo: vi) two substituents Rb form a methylene or ethylene bridge; or vii) two Rb substituents on adjacent carbons taken together with the carbons to which they are attached form a saturated monocyclic cycloalkyl group or saturated monocyclic heterocycloalkyl group, each group is not substituted or is substituted with C1-4 alkyl, OH, -C1 alkyl 4, NRcRd, or halo; where Rc is H or C1-4 alkyl; Rd is H, C1-4alkyl, -C1-4alkyl, -COC1-4alkyl-OH, -CO2C1-4alkyl, -CONRxRy, or -SO2C1-4alkyl; where Rx and Ry are each independently H or C1-4 alkyl; and Re and Rf are each independently H or C1-4 alkyl; R 3 is H, OH, C 1-4 alkyl, or -C 1-4 alkyl; R4 is H; C1-4 alkyl; -C1-4alkyl substituted or substituted with OH, F, -OCOC1-4alkyl, or NRtRu; -COCF3 -CO- (monocyclic heteroaryl); -CO (monocyclic heterocycloalkyl attached to C); -CO- (phenyl): -SO2 C1-4alkyl; -SO2CF3; SO2NRtRu; -CONRtRu; -COCO2 C1-4alkyl or -COCONRtRu: where Rty Ru are each independently H, C1-4alkyl, or -C1-4alkyl or Rt and Ru taken together with the nitrogen to which they are attached form a monocyclic heterocycloalkyl ring; R5 is halo or CF3; each R6 is independently H or F; D is -CEC-R7, -CH = CH-R8, - (CH2) 2-3-R8, or - (CH2) 3-5-R9; where R7 is: I) a C1-4 alkyl group unsubstituted or substituted with OH, -C1-4 alkyl, -NRgRh, phenyl, or phenoxy, each phenyl or phenoxy is not substituted or substituted with C1-4 alkyl, OH , -C1-4alkyl, halo, or CF3 where Rg and Rh are each independently H, C1-4alkyl, -C1-4alkyl, -COphenyl, -CO2C1-4alkyl, -SO2C1-4alkyl, or -SO2 -phenyl; or Rg and Rh taken together with the nitrogen to which they are attached form a monocyclic heterocycloalkyl group; or II) a monocyclic cycloalkyl group, phenyl group or monocyclic heteroaryl group, each group is not substituted or is substituted with one or two Rk substituents; where R8 is a phenyl group or a heteroaryl monocyclic group, each group is not substituted or substituted with one or two Rk substituents; where R9 is OH or -NRnRo; where Rn is H or C1-4 alkyl; and Ro is H, C1-4alkyl, monocyclic cycloalkyl, -C1-4alkyl, -COphenyl, -CO2C1-4alkyl, -SO2aC1-4alkyl, -SO2-phenyl, -SO2-benzyl, or -SO2NRpRq, each group phenyl or benzyl is not substituted or substituted with one or two Rk substituents; where Rp and Rq are each independently H or C1-4 alkyl; or Rn and Ro taken together with the nitrogen to which they are attached form a saturated monocyclic heterocycloalkyl ring unsubstituted or substituted with C1-4 alkyl, OH, C1-4alkyl, halo, or CF3; where each Rk substituent in D is independently: a) a C1-4 alkyl group substituted or substituted with OH. -C1-4alkyl, - C1-4alkyl-OH, halo, -CO2C1-4alkyl, CO2H, CN, NRrRs, -N (Rr) CO-phenyl, N (Rr) SO2C1-4alkyl, N (Rr) SO2phenyl , -SO2 C1-4alkyl, phenyl, or phenoxy; b) a substituent of formula (2) wherein each Rv is independently H or C1-4 alkyl, or both Rv substituents together form a carbonyl; Rw is H, C1-4alkyl, -CH2OH, or -CO2C1-4alkyl; A is O or NRaa; where Raa is H or C1-4 alkyl and Z is a phenyl group, benzyl group, cycloalkyl group, heterocycloalkyl group, heteroaryl group, or -CH2- (heteroaryl) group, each group is unsubstituted or is substituted with one or two substituents independently selected from the group consisting of C1-4 alkyl, CF3, halo, OH, -C1-4 alkyl, -OCF3, -OCHF2, NRddRee, -CO2C1-4 alkyl, -C1-4 alkyl, and -SO2C 1-4 alkyl ; where Rdd and Ree are each independently H or C1-4 alkyl; c) two adjacent Rk substituents taken together with the carbons to which they are attached form an anilophenyl, monocyclic heteroaryl ring, monocyclic heterocycloalkyl ring, or fused monocyclic cycloalkyl ring, each fused ring is not substituted or is substituted with: C1-4 alkyl, -C 1-4 alkyl-CF 3 -C 1-4 alkyl-OH, -C 1-4 alkyl-C 1-4 alkyl, CF 3, C 2-4 alkenyl, halo, OH, -C 1-4 alkyl, -C 1-4 alkyl, -COCF 3, -CO2C1-4alkyl, -CO2H, -CONRffRgg or -SO2C1-4alkyl or with a cycloalkyl group, group -CH2- (cycloalkyl), or benzyl group, each group is not substituted or substituted with C1-4alkyl, OH, -C 1-4 alkyl, halo, or CF 3; where Rff and Rgg are each independently H or C1-4 alkyl, or Rff and Rgg taken together with the nitrogen to which they are attached form a monocyclic heterocycloalkyl ring, substituted or substituted with C1-4 alkyl or OH; or d) OH; -C 1-4 alkyl; halo; CF3 -CHO; -CO2 C1-4alkyl CO2H; CN; -NO2 -CONRrRs, NRrRs; -N (Rr) -phenyl; -N (Rr) -benzyl; -N (Rr) -phenethyl; -N (Rr) C1-4alkyl; -N (Rr) CO-phenyl; -N (Rr) SO2C 1-4 alkyl -N (Rr) SO2-phenyl; -SO2C 1-4 alkyl phenoxy; or a heteroaryl group; where each phenyl, benzyl, phenethyl, phenoxy, or heteroaryl group is not substituted or substituted with C1-4 alkyl, OH, -C1-4 alkyl, halo, or CF3 where Rr is H, C1-4 alkyl, C2 alkyl- 4-OH; and Rs is H, C1-4 alkyl, -C1-4 alkyl-CF3, -C1-4 alkyl-CN, -C2-4 alkyl-OH, -C2-4 alkyl-NRbbRcc, -C 1-4 alkyl C1-4 alkyl , -C1-4CO2H alkyl, C3-4 alkenyl, - C1-4alkyl, or CO2C1-4alkyl where Rbb is H or C1-4alkyl and; Rcc is H, C1-4alkyl, -C1-4alkyl, or -CO2C 1-4 alkyl; or Rbb and Rcc taken together with the nitrogen to which they are attached form a monocyclic heterocycloalkyl ring; or Rr and Rs taken together with the nitrogen to which they are attached form a heterocycloalkyl group unsubstituted or substituted with C1-4alkyl, OH, -C1-4alkyl, halo, CF3, or a monocyclic heterocycloalkyl ring unsubstituted or substituted with OH; or a salt acceptable for pharmaceutical, prodrug, or metabolite use. |
| priorityDate | 2007-02-15-04:00^^<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: 54.