http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2906107-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c7ba8052a2cec6dcd5293713a6839cd8 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02A50-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4015 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4015 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-522 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4985 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-444 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-444 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-522 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4709 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4985 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4015 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-404 |
| filingDate | 2017-09-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2022-04-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b7113c2f692a252dbfc3600461d772d6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_78956cef9f1b0dc928e6ebac9a34650e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_693a72ced42f2d4aa462cb12eb8c68f8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4804ca5bf11e62b6a769c58b4441d579 |
| publicationDate | 2022-04-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2906107-T3 |
| titleOfInvention | novel uses |
| abstract | A PDE1 inhibitor for use in the treatment or prophylaxis of neuroinflammation and/or diseases or disorders associated with neuroinflammation and/or microglial function comprising administering a PDE1 inhibitor to a patient in need thereof, wherein the PDE1 inhibitor is : A. a compound of Formula V: **(See formula)** wherein (I) R1 is H or C1-4 alkyl (eg, methyl); (ii) R4 is H or C1-4 alkyl and R2 and R3 are independently H or C1-4 alkyl (eg, R2 and R3 are both methyl, or R2 is H and R3 is isopropyl), aryl, heteroaryl, (optionally hetero)arylalkoxy or (optionally hetero)arylalkyl; or R2 is H and R3 and R4 together form a di-, tri-, or tetramethylene bridge (pref. where R3 and R4 together have the cis configuration, e.g., where the carbons bearing R3 and R4 have the configurations R and S, respectively); (iii) R5 is a substituted heteroarylalkyl, e.g. e.g., substituted haloalkyl or R5 is attached to one of the nitrogens on the pyrazolo portion of Formula V and is a moiety of Formula A: **(See formula)** where X, Y and Z are, independently, N or C, and R8, R9, R11, and R12 are independently H or halogen (eg, Cl or F), and R10 is halogen, alkyl, cycloalkyl, haloalkyl (eg, trifluoromethyl), aryl (eg, phenyl), heteroaryl (eg, pyridyl (eg, pyrid-2-yl) or thiadiazolyl (eg, 1,2,3-thiadiazol-4-yl)), diazolyl, triazolyl, tetrazolyl , arylcarbonyl (eg, benzoyl), alkylsulfonyl (eg, methylsulfonyl), heteroarylcarbonyl, or alkoxycarbonyl; provided that when X, Y, or Z is nitrogen, R8, R9, or R10, respectively, is not present; and (iv) R6 is H, alkyl, aryl, heteroaryl, arylalkyl (eg, benzyl), arylamino (eg, phenylamino), heteroarylamino, N,N-dialkylamino, N,N-diarylamino, or N- aryl-N-(arylalkyl)amino (eg, N-phenyl-N-(1,1'-biphen-4-ylmethyl)amino); and (v) n=0 or 1; (vi) when n=1, A is -C(R13R14)- where R13 and R14 are independently H or C1-4alkyl, aryl, heteroaryl, (optionally hetero)arylalkoxy or (optionally hetero)arylalkyl; in free, salt or enantiomers, diastereoisomers and racemates; B. a compound of Formula VII: **(See formula)** (i) X is C1-6 alkylene (eg, methylene, ethylene, or prop-2-yn-1-ylene); (ii) Y is a single bond, alkynylene (eg -C≡C-), arylene (eg phenylene), or heteroarylene (eg pyridylene); (iii) Z is H, aryl (eg phenyl), heteroaryl (eg pyridyl, eg pyrid-2-yl), halo (eg F, Br, Cl ), halo C1-6 alkyl (eg, trifluoromethyl), -C(O)-R1, -N(R2)(D3), or C3-7 cycloalkyl optionally containing at least one atom selected from a group consisting of consists of N or O (eg, cyclopentyl, cyclohexyl, tetrahydro-2H-pyran-4-yl, or morpholinyl); (iv) R1 is C1-6 alkyl, halo C1-6 alkyl, -OH, or -OC1-6 alkyl (eg, -OCH3); (v) R2 and R3 are independently H or C1-6 alkyl; (vi) R4 and R5 are independently H, C1-6 alkyl or aryl (eg phenyl) optionally substituted with one or more halo (eg fluorophenyl, eg 4-fluorophenyl), hydroxy (eg, hydroxyphenyl, eg, 4-hydroxyphenyl or 2-hydroxyphenyl) or C1-6 alkoxy; (vii) wherein X, Y and Z are independently and optionally substituted with one or more halo (eg F, Cl or Br), C1-6 alkyl (eg methyl), halo C1- 6 (eg, trifluoromethyl), p. g., Z is heteroaryl, e.g. g., pyridyl substituted with one or more halo (eg, 6-fluoropyrid-2-yl, 5-fluoropyrid-2-yl, 6-fluoropyrid-2-yl, 3-fluoropyrid-2-yl, 4-fluoropyrid-2 -yl, 4,6-dichloropyrid-2-yl), halo C1-6 alkyl (eg, 5-trifluoromethylpyrid-2-yl), or C1-6 alkyl (eg, 5-methylpyrid-2- yl), or Z is aryl, e.g. eg, phenyl, substituted with one or more halo (eg, 4-fluorophenyl), in pharmaceutically acceptable free salt form; or C. a compound of Formula XII: **(See formula)** wherein (i) R1 is H or C1-4 alkyl (eg, methyl or ethyl); (ii) R2 and R3 are independently H or C1-6 alkyl (eg, methyl or ethyl); (iii) R4 is H or C1-4 alkyl (eg, methyl or ethyl); (iv) R5 is aryl (eg phenyl) optionally substituted with one or more groups independently selected from -C(=O)-C1-6alkyl (eg -C(=O)-CH3) and C1-6 hydroxyalkyl (eg, 1-hydroxyethyl); (v) R6 and R7 are independently H or aryl (eg phenyl) optionally substituted with one or more groups independently selected from C1-6 alkyl (eg methyl or ethyl) and halogen (eg C1-6 alkyl). , F or Cl), e.g. eg, unsubstituted phenyl or phenyl substituted with one or more halogens (eg, F) or phenyl substituted with one or more C1-6 alkyl and one or more halogens or phenyl substituted with one C1-6 alkyl and one halogen , p. eg, 4-fluorophenyl or 3,4-difluorophenyl or 4-fluoro-3-methylphenyl; and (vi) n is 1, 2, 3 or 4, in free or salt form. |
| priorityDate | 2016-09-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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