Discovery of 9-Cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial
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چکیده
منابع مشابه
Pharmacology of Basimglurant (RO4917523, RG7090), a Unique Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator in Clinical Development for Depression s
Major depressive disorder (MDD) is a serious public health burden and a leading cause of disability. Its pharmacotherapy is currently limited tomodulators of monoamine neurotransmitters and secondgeneration antipsychotics. Recently, glutamatergic approaches for the treatment of MDD have increasingly received attention, and preclinical research suggests that metabotropic glutamate receptor 5 (mG...
متن کاملSELECTIVE CYCLIZATION OF 2-PROPARGYLTHIO-6-METHYL-PYRIMIDIN- 4(1 H)-ONE TO THIAZOLO [3,2-a] PYRIMIDIN 7-ONE
Selective transformation of 2-propargylthio-6-methyl-pyrimidin-4(1H)On e (2) to 3,5-dimethyl-7H-thiazolo [3,2-a] pyrimidin-7-one (3) is performed under the conditionof base catalysis . For elucidation of structure, palladium catalyzed cyclization reaction of (2) was carried out and the structures of the products were assigned (5) and (6). These compounds underwent isomerization to (3) and (4...
متن کامل(S)-5-Hexyl-1-[(S)-2-hydroxy-1-phenylethyl]-4-methoxy-1H-pyrrol-2(5H)-one
The title compound, C(19)H(27)NO(3), was obtained by the reaction of (3S,7aR)-7a-hexyl-7-meth-oxy-3-phenyl-2,3-dihydro-pyrrolo[2,1-b]oxazol-5(7aH)-one and triethyl-silane using titanium(IV) chloride as catalyst. In the mol-ecule, the phenyl and dihydro-pyrrolone rings form a dihedral angle of 83.8 (1)°. O-H⋯O hydrogen-bonding inter-actions lead to the formation of a chain parallel to the a axis.
متن کاملPharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression.
Major depressive disorder (MDD) is a serious public health burden and a leading cause of disability. Its pharmacotherapy is currently limited to modulators of monoamine neurotransmitters and second-generation antipsychotics. Recently, glutamatergic approaches for the treatment of MDD have increasingly received attention, and preclinical research suggests that metabotropic glutamate receptor 5 (...
متن کاملSYNTHESIS OF OXAZOLO [3, 2-b] 1, 2, 4- TRIAZINES A NOVEL HETEROCYCLIC SYSTEM
The synthesis of 6- methyl- 2- phenyl- 7H- oxazolo [3,2-b] 1,2,4-Triazine- 7-one (6, R=Ph) and its 2-P- bromophenyl analogue to the two members of a new heterocyclic system is described
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2020
ISSN: 0022-2623,1520-4804
DOI: 10.1021/acs.jmedchem.0c00272