- PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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The present invention relates to pyrazolopyrimidine derivatives having dual pharmacological activity towards both the α2δ subunit of the voltage-gated calcium channel and the sigma-1 (σ1) receptor, to processes of preparation of such compounds,
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Page/Page column 171
(2021/12/08)
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- [1,2,4]-TRIAZOLO [1,5-A]-PYRIMIDINYL DERIVATIVES SUBSTITUTED WITH PIPERIDINE, MORPHOLINE OR PIPERAZINE AS OGA INHIBITORS
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The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations.
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Page/Page column 48
(2018/09/19)
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- [1,2,4]TRIAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AS PDE2 INHIBITORS
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The present invention relates to novel [1,2,4]triazolo[1,5-a]pyrimidin-yl derivatives as inhibitors of phosphodiesterase 2 (PDE2). The invention is also directed to pharmaceutical compositions comprising the compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, such as neurological and psychiatric disorders.
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Page/Page column 41; 58; 59
(2018/05/24)
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- NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
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Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridge
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Page/Page column 80
(2012/05/19)
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- PIPERIDINE AMIDES AS MODULATORS OF THE GHRELIN RECEPTOR
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Compounds of formula (I) or pharmaceutically acceptable salts thereof, are useful for the treatment of diabetes and obesity.
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- SUBSTITUTED ARYL SULFONE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
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A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more ot
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Page/Page column 62
(2010/04/27)
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- Synthesis and pharmacological evaluation of aminopyrimidine series of 5-HT1A partial agonists
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Aminopyrimidine 2 (4-(1-(2-(1H-indol-3-yl)ethyl)piperidin-3-yl)-N-cyclopropylpyrimidin-2-amine) emerged from a high throughput screen as a novel 5-HT1A agonist. This compound showed moderate potency for 5-HT1A in binding and functional assays, as well as moderate metabolic stability. Implementation of a strategy for improving metabolic stability by lowering the lipophilicity (c Log D) led to identification of methyl ether 31 (4-(1-(2-(1H-indol-3-yl)ethyl)piperidin-3-yl)-N-(2-methoxyethyl)pyrimidin-2-amine) as a substantially improved compound within the series.
- Dounay, Amy B.,Barta, Nancy S.,Bikker, Jack A.,Borosky, Susan A.,Campbell, Brian M.,Crawford, Terry,Denny, Lynne,Evans, Lori M.,Gray, David L.,Lee, Pil,Lenoir, Edward A.,Xu, Wenjian
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scheme or table
p. 1159 - 1163
(2009/08/07)
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- Microwave-assisted synthesis of novel (5-nitropyridin-2-yl)alkyl and (5-nitropyridin-3-yl)alkyl carbamates
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A straightforward approach to novel (5-nitropyridin-2-yl)alkyl and (5-nitropyridin-3-yl)alkyl carbamate building blocks is presented in this study. Their construction is achieved by condensation of N-carbamate a- and β-amino carbonyl derivatives with l-methyl-3,5-dinitro-2-pyridone 1 under microwave irradiation. Judiciously chosen modifications in the nature of the parent carbonyl starting material has influenced the regiochemical outcome of the reaction and allowed an efficient access to novel nitrogen-containing scaffolds. Compounds sharing morphological similarities have been gathered in three libraries differing from each other in a single structural parameter.
- Henry, Christophe,Haupt, Andreas,Turner, Sean C.
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supporting information; experimental part
p. 1932 - 1938
(2009/08/07)
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- Pyrrolopyrimidines useful as inhibitors of protein kinase
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The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, c
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Page/Page column 27
(2008/06/13)
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