http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-087628-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_1c89ce4d9ac03f9acd8ddede1162f94d |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-47 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 |
| filingDate | 2012-08-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2014-04-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-087628-A1 |
| titleOfInvention | PYRIMIDINE PDE10 INHIBITORS |
| abstract | This refers to pyrimidine compounds that are useful as therapeutic agents for the treatment of disorders of the central nervous system associated with phosphodiesterase 10 (PDE10). This also refers to the use of said compounds to treat neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatum hypofunction or basal ganglia dysfunction. Claim 1: A compound of the formula (1) wherein: A is selected from the group consisting of: (i) pyridyl, (ii) quinolinyl, (iii) naphthyridinyl, (iv) thiazolyl, (v) pyridazinyl, (vi) oxazolyl, and (vii) pyrazolyl, (viii) dihydropyrrolopyrazolyl, (ix) dihydrocyclopentapyridinyl, (x) imidazopyridazinyl and (xi) pyrazolopyrimidinyl; B is selected from the group consisting of: (i) thiazolyl, (ii) pyrazolyl, (iii) thiadiazolyl, (iv) isoxazolyl, (v) isothiazolyl, (vi) pyridyl and (vii) pyrimidinyl; R¹ᵃ, R¹ᵇ and R¹ᶜ are independently selected from the group consisting of: (i) hydrogen, (ii) halogen, (iii) hydroxyl, (iv) - (C = O) ₘ-Oₙ-C₁₋₆ alkyl, in the that m is 0 or 1, n is 0 or 1 (in which if m is 0 on is 0, a bond is present) and in which the alkyl is unsubstituted or substituted with one or more substituents selected from R¹³, ( v) - (C = O) ₘ-Oₙ-C₃₋₆ cycloalkyl, where the cycloalkyl is unsubstituted or substituted with one or more substituents selected from R¹³, (vi) - (C = O) ₘ-Cque alkenyl, where the alkenyl is unsubstituted or substituted with one or more substituents selected from R¹³, (vii) - (C = O) ₘ-Cin alkynyl, where the alkynyl is unsubstituted or substituted with one or more substituents selected from R¹³, (viii) - (C = O) ₘ-Oₙ-phenyl or - (C = O) ₘ-Oₙ-naphthyl, where phenyl or naphthyl are unsubstituted or substituted with one or more substituents selected from R¹ ³, (ix) - (C = O) ₘ-Oₙ-heteroaryl, where the heteroaryl is unsubstituted or substituted with one or more substituents selected from R¹³, (x) - (C = O) ₘ-NR¹⁰R¹¹, (xi) -S (O) ₂-NR¹⁰R¹¹, (xii) -S (O) q-R¹², where q is 0, 1 or 2 and where R¹² is selected from the definitions of R¹⁰ and R¹¹, (xiii) -CO₂H, (xiv ) -CN and (xv) -NO₂; R²ᵃ, R²ᵇ and R²ᶜ are independently selected from the group consisting of: (i) hydrogen, (ii) halogen, (iii) hydroxyl, (iv) - (C = O) ₘ-Oₙ-C alquilo alkyl, where the alkyl is unsubstituted or substituted with one or more substituents selected from R¹³, (v) - (C = O) ₘ-Oₙ-C₃₋₆ cycloalkyl, where the cycloalkyl is unsubstituted or substituted with one or more substituents selected from R¹³, (vi) - (C = O) ₘ-Cque alkenyl, where the alkenyl is unsubstituted or substituted with one or more substituents selected from R¹³, (vii) - (C = O) ₘ-Cin alkynyl, where the alkynyl is unsubstituted or substituted with one or more substituents selected from R¹³, (viii) - (C = O) ₙ-Oₙ-phenyl or - (C = O) ₘ-Oₙ-naphthyl, where the phenyl or naphthyl are unsubstituted or substituted with one or more substituents selected from R¹³, (ix) - (C = O) ₘ-Oₙ-heterocyclyl, where the heterocyclyl is unsubstituted or substituted with one or more substituents selected from R¹³, (x) - (C = O) ₘ-NR¹⁰R¹¹, (xi) -S (O) ₂-NR¹⁰R¹¹, (xii) -S (O) q-R¹², (xiii) -CO₂H , (xiv) -CN and (xv) -NO₂; R³ is selected from the group consisting of: (i) CH₃, (ii) CF₃, (iii) CH₂F, (iv) CH₂CH₃, (v) cyclopropyl, (vi) cyano, (vii) hydrogen, (viii) NH₂, (ix) C (O) OR⁵, (x) -O-C₁₋₆ alkyl, (xi) - (CO) NH₂, (xii) C₁₋₆OH alkyl, (xiii) C (O) C₁₋₆ alkyl, and (xiv) halogen; R⁴ is selected from the group consisting of: (i) hydrogen, (ii) halo, (iii) -C₁₋₆ alkyl, and (iv) cyano; R⁵ is selected from the group consisting of: (i) hydrogen and (ii) C₁₋₆ alkyl; R⁶ is selected from the group consisting of: (i) hydrogen, (ii) C₁₋₆ alkyl, and (iii) O-C₁₋₆ alkyl; R¹⁰ and R¹¹ are independently selected from the group consisting of: (a) hydrogen, (b) C₁₋₆ alkyl, which is unsubstituted or substituted with R¹⁴, (c) C₃₋₆ alkenyl, which is unsubstituted or substituted with R¹⁴, (d) C₃₋₆ alkynyl, which is unsubstituted or substituted with R¹⁴, (e) C₃₋₆ cycloalkyl, which is unsubstituted or substituted with R¹⁴, (f) C₁₋₆ alkoxy, which is unsubstituted or substituted with R¹⁴, (g) phenyl, which is unsubstituted or substituted with R¹⁴, and (h) heteroaryl, which is unsubstituted or substituted with R¹⁴; R¹³ is selected from the group consisting of: (i) halogen, (ii) hydroxyl, (iii) - (C = O) ₙ-Oₙ-C₁₋₆ alkyl, where the alkyl is unsubstituted or substituted with one or more substituents selected from R¹⁴, (iv) -Oₙ-perfluoroalkyl C₁₋₃, (v) - (C = O) ₙ-Oₙ-cycloalkyl C₃₋₆, where the cycloalkyl is unsubstituted or substituted with one or more substituents selected from R¹⁴ , (vi) - (C = O) ₘ-Cque alkenyl, where the alkenyl is unsubstituted or substituted with one or more substituents selected from R¹⁴, (vii) - (C = O) ₘ-Cin alkynyl, where the alkynyl is unsubstituted or substituted with one or more substituents selected from R¹⁴, (viii) - (C = O) ₙ-Oₙ-phenyl or - (C = O) ₘ-Oₙ-naphthyl, where the phenyl or naphthyl are unsubstituted or substituted with one or more substituents selected from R¹⁴, (ix) - (C = O) ₘ-Oₙ-heteroaryl, where the heteroaryl is unsubstituted or substituted with one or more of its stitudents selected from R¹⁴, (x) - (C = O) ₘ-NR¹⁰R¹¹, (xi) -S (O) ₂-NR¹⁰R¹¹, (xii) -S (O) q-R¹², (xiii) -CO₂H, (xiv ) -CN and (xv) -NO₂; R¹⁴ is selected from the group consisting of: (i) hydroxyl, (ii) halogen, (iii) C₁₋₆ alkyl, (iv) -C₃₋₆ cycloalkyl, (v) -O-C₁₋₆ alkyl, (vi ) -O (C = O) -C₁₋₆ alkyl, (vii) -NH-C₁₋₆ alkyl, (viii) phenyl, (ix) heteroaryl, (x) -CO₂H and (xi) -CN; or a pharmaceutically acceptable salt thereof. |
| priorityDate | 2011-08-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 42.