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filingDate 2020-07-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fcdd1f1b419b833bf05999d8f6dc08a2
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publicationDate 2021-12-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-119322-A1
titleOfInvention COMPOUNDS DERIVED FROM 1H-PYRIDO[1,2-A]PYRAZINE AS MAGL INHIBITORS
abstract Pyrido-pyrazine derivatives such as monoacylglycerol lipase (MAGL) inhibitors, pharmaceutical compositions comprising them and their use for the treatment or prophylaxis of neuroinflammation, neurodegenerative diseases, pain, cancer and mental disorders. Claim 1: Compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein: R¹ is selected from the group consisting of: (i) C₆₋₁₄ aryl optionally substituted with 1 to 2 substituents independently selected from the group consisting of at C₁₋₆ alkoxy, halogen and a group of formula (2), (ii) 5 to 6 membered heteroaryl optionally substituted with 1 to 2 substituents independently selected from the group consisting of halogen, hydroxy, C₁₋₆ alkoxy, -B (OH)₂, 5-6 membered heteroaryl, C₁₋₆ alkyl, and amino, and (iii) 5-14 membered heterocyclyl optionally substituted with 1 to 3 substituents independently selected from the group consisting of halogen, C₁₋₆ alkyl and oxo, R² is selected from the group consisting of: (i) C₁₋₆ alkyl optionally substituted with 1 to 3 substituents independently selected from halogen, (ii) C₃₋₁₄ cycloalkyl, (iii) C₆₋₁₄ aryl optionally substituted with 1 to 2 substituents selected s independently of halogen, (iv) 5 to 14 membered heteroaryl optionally substituted with 1 to 3 substituents independently selected from halogen, C₁₋₆ alkyl, C₁₋₆ haloalkyl and oxo, and (v) optionally substituted 5 to 14 membered heteroaryloxy with 1 to 3 substituents independently selected from halogen, C₁₋₆ alkyl, C₁₋₆ haloalkyl and oxo, and (vi) 5 to 14 membered heterocyclyl optionally substituted with 1 to 3 substituents independently selected from halogen, C₁₋₆ alkyl, haloalkyl C₁₋₆ and oxo, R³ is selected from the group consisting of hydrogen, halogen, C₁₋₆ alkoxy, C₃₋₁₄ cycloalkyloxy, and hydroxy, R⁴ is selected from the group consisting of hydrogen, halogen, C₁₋₆ alkyl, hydroxy-alkyl C₁₋₆, C₁₋₆-alkoxy-carbonyl, C₁₋₆-alkoxy-carbonyl-NH-, hydroxy, amino, carboxy, C₁₋₆-alkyl-C(O)-NH-, C₂₋₆-alkenyl-C(O)-NH -, carboxy-NH-, oxo, C₃₋₁₄-cycloalkyl, and hydroxy-C₃₋₁₄-cycloalkyl, L is selected from the group consisting of a co bond valent and -CH=CH-, A is selected from the group consisting of C₆₋₁₄ aryl, 5 to 14 membered heteroaryl, and 5 to 14 membered heterocyclyl, and n is 1, 2, 3, or 4.
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Total number of triples: 54.