http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-050786-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cf32b60391b469c41e86c353437f5751 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-47 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 |
| filingDate | 2005-08-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2006-11-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-050786-A1 |
| titleOfInvention | COMPOUNDS AND USEFUL COMPOSITIONS AS INHIBITORS OF CATEPSINA-S |
| abstract | This refers to the use of a 2-cyano-pyrimidine compound of the formula (1), wherein: R1, R2, R3 and X are as defined in the specification and in the claims, in free form or in salt form, and where possible, in tautomeric form, as an inhibitor of the activity of cathepsin S. Claim 1: A 2-cyano-pyrimidine of the formula (1), R1 denotes a radical of the formula (2) , wherein A, E, and G, independently of each other, represent O, S, or CH2, with the proviso that at least one of A and E represents CH2; T is O, S, or a link, if G is CH2, and T is a link if G is O or S; Ra, Rb, and Rc, independently of each other, represent hydrogen or C1-4 alkyl; s is 0, 1 or 2, t is 1, 2, 3, or 4, and p is 0, 1, or 2; R2 denotes halogen, C1-4 alkyl, unsubstituted or substituted aryl, 5- or 6-membered heterocyclyl -C (O) NR4R5, -NHC (O) R4, or CH2NHC (O) R4, wherein: R4 represents: a) alkyl C1-7 which is unsubstituted or substituted by halogen; amino, which is mono- or di-substituted by C3-5 cycloalkyl or C1-6 alkyl, which in each case are unsubstituted or mono-, di-, or tri-substituted by halogen; unsubstituted or substituted C4-8 aliphatic heterocyclyl, comprising at least one nitrogen atom; unsubstituted or substituted aryl; unsubstituted or substituted heteroaryl; spiro [4.5] unsubstituted or substituted decane, which comprises one or two heteroatoms selected from oxygen, nitrogen, and sulfur; unsubstituted or substituted C3-6 cycloalkyl; or 1-aza-C5-8 cycloalkyl; b) unsubstituted or substituted N-C1-4-piperidinyl or N-cycloalkylC4-6-piperidinyl; c) substituted or substituted aryl; d) unsubstituted or substituted C3-6 cycloalkyl; or e) unsubstituted or substituted 5 or 6 membered heteroaryl containing a nitrogen atom; and R5 represents hydrogen or C1-4 alkyl; or R4 and R5, together with the nitrogen with which they are attached, represent unsubstituted or substituted C4-8 aliphatic heterocyclyl, comprising at least one nitrogen atom; or R2 denotes -N (R9) SO2R10; R9 represents hydrogen or C1-4 alkyl; and R10 represents C1-4 alkyl, which is unsubstituted or substituted by aryl; or R9 and R10 together form a radical - (CRR ') m-, where m is an integer from and including 2 and to and including 5, and R and R' both represent, independently of each other, hydrogen or C1- alkyl 4; R3 denotes hydrogen, halogen, phenyl, pyridyl, which is unsubstituted or mono-, di-, or tri-substituted by halogen, Y-R6, or NR7R8, wherein: Y represents O, CH2, S, SO, SO2, or NRN, wherein RN denotes hydrogen or C1-4 alkyl which is unsubstituted or substituted by C1-4 alkoxy; R6 represents C1-6 alkyl, phenyl, 5- or 6-membered nitrogen containing heteroyl- (CO2) q-, wherein q is an integer from 0 to 4, or 5 or 6 membered aliphatic heterocyclyl- (CH2) n- , wherein n is an integer from 0 to 4 and the heterocyclyl fraction comprises at least one ring nitrogen atom, whose radicals in each case may be unsubstituted or substituted; R7 and R8, together with the nitrogen to which they are attached, represent unsubstituted or substituted 5 or 6-membered aliphatic heterocyclyl, wherein the heterocyclyl fraction comprises at least one nitrogen atom; X denotes O, HN, C1-4-N alkyl, S, SO, SO2, O (CH2) gNH, where g is 1 or 2, (CH2) h, where h is 1 or 2, or aryl that is unsubstituted or mono-, di-, or tri-substituted by halogen, C1-4 alkyl, or C1-4 alkoxy; or a tautomer and / or salt of this 2-cyano-pyrimidine. |
| priorityDate | 2004-08-17-04:00^^<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: 64.