http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-076861-A1
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| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_12b48d4c99a52e300a0cddf45687aa4d http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_710fcb517ce69d1861cc2d091c1c1a44 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-0095 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4545 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-496 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-0019 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-438 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-2059 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 |
| filingDate | 2010-05-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2011-07-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-076861-A1 |
| titleOfInvention | DERIVATIVES OF 1,2,4-TRIAZOLO (4,3-A) PIRIDINE AND ITS USE AS POSITIVE ALOSTERIC MODULATORS OF MGLUR2 RECEIVERS |
| abstract | The present application relates to new triazolo [4,3-a] pyridine derivatives of formula (1). The compounds are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (ômGluR2ö), useful for the treatment or prevention of neurological and psychiatric disorders associated with a dysfunction of glutamate and diseases in which the mGluR2 subtype of metabotropic receptors is involved, also It refers to pharmaceutical compositions comprising said compounds, processes for preparing said compounds and compositions, and the use of said compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved. Claim 1: A compound of formula (1) or a stereochemically isomeric form of said compound wherein n is selected from the group consisting of 0, 1 and 2; m is selected from the group consisting of 0, 1, and 2; R is selected from methyl or trifluoromethyl; R1 is selected from the group consisting of hydrogen; C1-6 alkyl, (C1-3 alkyloxy) - C1-3 alkyl, [(C1-3 alkyloxy) C1-3 alkyl] C1-3 alkyl, C1-3 alkyl substituted with one or more independently selected halo substituents; unsubstituted phenyl; unsubstituted benzyl; Benzyl substituted with 1, 2 or 3 substituents independently selected from the group consisting of halo, C1-3alkyl, C1-3alkyloxy, C1-3alkyloxy C1-3alkyl, C1-3 hydroxyalkyl, cyano, hydroxyl, amino, C (= O) R ', C (= O) O', C (= O) NR'Rö, mono- or di (C1-3 alkyl) amino, morpholinyl, (C3-7 cycloalkyl) C1-3 alkyloxy, trifluoromethyl and trifluoromethoxy , wherein R 'and Rö are independently selected from hydrogen and C1-6 alkyl, (benzyloxy) C1-3 alkyl, unsubstituted C3-7 cycloalkyl; C3-7 cycloalkyl substituted with C1-3alkyl substituted with one or more independently selected halo substituents; (C3-7 cycloalkyl) C1-3 alkyl; [(C3-7 cycloalkyl) C1-3 alkyloxy] C1-3 alkyl; (C3-7 cycloalkyl) C1-3 alkyloxy; 4- (2,3,4,5-tetrahydrobenzo [f] [1,4] oxazepin) methyl; Het1, Het1 C1-3alkyl, Het2 and Het2 C1-3alkyl; R2 is selected from the group consisting of cyano; halo; C1-3 alkyl substituted with one or more independently selected halo substituents; C1-3 alkyloxy substituted with one or more independently selected halo substituents; C1-3 alkyl, C3-7 cycloalkyl and (C3-7 cycloalkyl) C1-3 alkyl; Ring L is a heterocycle containing N selected from the group consisting of (La), (Lb), (Lc), (Ld), (Le), (Lf), (Lg) and (Lh) where R3a is selects from the group consisting of C1-3 alkyl, C1-3 alkyl substituted with one or more independently selected halo substituents; unsubstituted C3-7 cycloalkyl; C3-7 cycloalkyl substituted with 1 or 2 substituents independently selected from C1-3 alkyl, C1-3 alkyl substituted with one or more independently selected halo substituents or hydroxyl; unsubstituted phenyl; phenyl substituted with 1, 2 or 3 substituents independently selected from the group consisting of halo, C1-3alkyl, C1-3 hydroxyalkyl, C1-3alkyl substituted with one or more independently selected halo substituents, cyano, hydroxyl, amino, carboxyl, C1-3 alkyloxy-C1-3alkyl, C1-3alkyloxy, C1-3alkyloxy substituted with one or more independently selected halo substituents, C1-3alkylcarbonyl, mono- and di (C1-3alkyl) amino and morpholinyl; (phenyl) unsubstituted C1-3 alkyl; (phenyl) C1-3alkyl wherein the phenyl and C1-3alkyl part of the substituent can each be independently substituted with 1, 2 or 3 substituents independently selected from the group consisting of halo, C1-3alkyl, C1- hydroxyalkyl 3, C1-3alkyl substituted with one or more independently selected halo substituents, cyano, hydroxyl, amino, carboxyl, C1-3alkyloxyC1-3alkyl, C1-3alkyloxy, C1-3alkyloxy substituted with one or more independently selected halo substituents , C 1-3 alkylcarbonyl, mono- or di (C 1-3 alkyl) amino, morpholinyl and (C 3-7 cycloalkyl) C 1-3 alkyloxy, unsubstituted phenyloxy; phenyloxy substituted with 1, 2 or 3 substituents independently selected from the group consisting of halo, C1-3 alkyl, C1-3 alkyl substituted with one or more independently selected halo substituents, C1-3 alkyloxy, and C1-3 alkyloxy substituted with one or several independently selected halo substituents; unsubstituted phenyloxy (C1-3 alkyl) oxy; (C1-3 phenylalkyl) unsubstituted oxy; phenyl (C1-3 alkyl) oxy wherein the phenyl part of the substituent is substituted with 1, 2 or 3 substituents independently selected from the group consisting of halo, C1-3 alkyl, C1-3 alkyl substituted with one or more halo substituents selected independently, C1-3 alkyloxy, and C1-3 alkyloxy substituted with one or more independently selected halo substituents; unsubstituted C1-3 phenyloxyalkyl; (phenyloxy) C1-3 alkyl substituted with 1 or 2 substituents independently selected from the group consisting of halo, C1-3 alkyl, C1-3 alkyl substituted with one or more independently selected halo substituents, C1-3 alkyloxy, and C1- alkyloxy 3 substituted with one or more independently selected halo substituents; unsubstituted phenylamino; phenylamino substituted with 1 or 2 independently selected halo substituents; (C1-3 phenylalkyl) amino; (phenylamino) (C1-3 alkyl); (C3-7 cycloalkyl) C1-3 alkyl, [phenyl (C3-7 cycloalkyl)] C1-3 alkyl; Het1; Het2; Het2oxi; Het2methyloxy; Het3 and phenyl with two neighboring substituents which, taken together, form a bivalent radical of the formula -N = CH-NH- (a), -CH = CH-NH- (b), or -O-CH2-CH2-NH- (C); R4a is selected from the group consisting of hydrogen; halogen; trifluoromethyl; trifluoromethoxy; hydroxyl; C1-3 alkyl, C1-3 alkyloxy, C1-3 hydroxyalkyl, C1-3 hydroxyl-alkyloxy, C1-3 fluoroalkyl, C1-3 fluoroalkyloxy, cyano; unsubstituted phenyl; and phenyl substituted with 1 or 2 substituents independently selected from the group consisting of halo, C1-3 alkyloxy, C1-3 hydroxyalkyl, trifluoromethyl and trifluoromethoxy; or CR3aR4a forms a radical of formula (d), (e), (f), (g) or (h); wherein each W1d, W1e, W2e and W1f is independently selected from CH and N; each R7d, R7e, R7f, R7g, R8d, R8e, R8f, R8g is independently selected from hydrogen, methyl and fluoro; or each CR7dR8d, CR7eR8e, CR7fR8f, CR7gR8g forms a carbonyl group; each R9d, R9e, R9f and R9g is fluoro; each q1, q2, q3 or q4 is independently selected from 0, 1 and 2; r is 0 or 1; s is 0 or 1; each R3b and R3c is selected from the group consisting of C1-3 alkyl C1-3 alkyl substituted with one or more independently selected halo substituents; unsubstituted phenyl; phenyl substituted with 1, 2 or 3 substituents independently selected from the group consisting of halo, C1-3alkyl, C1-3 hydroxyalkyl, C1-3alkyl substituted with one or more independently selected halo substituents, cyano, hydroxyl, amino, carboxyl, C1-3 alkyloxy C1-3 alkyl, C1-3 alkyloxy, C1-3 alkyloxy substituted with one or more independently selected halo substituents, C1-3alkylcarbonyl, mono- and di (C1-3alkyl) amino, and morpholinyl; (phenyl) unsubstituted C1-3 alkyl; (phenyl) -C1-3alkyl wherein the phenyl and the C1-3alkyl part of the substituent can each be independently substituted with 1, 2 or 3 substituents independently selected from the group consisting of halo, C1-3alkyl, C1-hydroxyalkyl -3, C1-3alkyl substituted with one or more independently selected halo substituents, cyano, hydroxyl, amino, carboxyl, C1-3alkyloxyC1-3alkyl, C1-3alkyloxy, C1-3alkyloxy substituted with one or more selected halo substituents independently, C 1-3 alkylcarbonyl, mono- or di (C 1-3 alkyl) amino, morpholinyl, C 3-7 cycloalkyl, (C 3-7 cycloalkyl) C 1-3 alkyl, and (C 3-7 cycloalkyl) -C 1-3 alkyloxy, (phenyloxy) unsubstituted C1-3 alkyl; (phenyloxy) -C1-3alkyl substituted with 1 or 2 substituents independently selected from the group consisting of halo, C1-3alkyl, C1-3alkyl substituted with one or more independently selected halo substituents, C1-3alkyloxy, and C1 alkyloxy -3 substituted with one or more independently selected halo substituents; (phenylamino) (C1-3 alkyl); phenyl with two neighboring substituents which, taken together, form a bivalent radical of formula (a), (b) or (c) as defined above; Het1, Het2, Het3, unsubstituted C3-7 cycloalkyl; C3-7 cycloalkyl substituted with 1 or 2 substituents independently selected from C1-3 alkyl, C1-3 alkyl substituted with one or more independently selected halo substituents, or hydroxyl; (C3-7 cycloalkyl) C1-3 alkyl and [phenyl- (C3-7 cycloalkyl)] C1-3 alkyl; R3d and R4d are each independently selected from the group consisting of hydrogen and C1-3 alkyl; each R5a, R5b, R5c, R5d, R6a, R6b, R6c and R6d is independently selected from the group consisting of hydrogen and C1-3 alkyl; or each pair R5aR6a, R5bR6b, R5cR6c, R5dR6d are substituents on the same carbon atom and each CR5aR6a, CR5bR6b, CR5cR6c, CR5dR6d together form a (C = O) or a C3-7 cycloalkylidene radical; each R10a, R10b and R10c is selected from H, C1-3 alkyl and C1-3 alkyloxy; wherein, in (Le), when t is 1 or 2, R11 is hydrogen and R12 is selected from a substituent selected from the group consisting of phenyl, phenyloxy and phenylamino, each of which may be optionally substituted with 1 or 2 halo substituents; or when t is 1 or 3, then CR11R12 forms a radical of formula (i) or formula (j) wherein each R13i and R13j is independently selected from methyl and trifluoromethyl; each R14i or R14j is fluoro; each u1 and u2 is independently 0, 1 or 2; v1 is selected from the group of 0, 1 and 2; v2 be selected |
| priorityDate | 2009-05-12-04:00^^<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: 62.