960298-00-4Relevant articles and documents
GPR40 AGONISTS
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Paragraph 00264-00265; 00289-00290, (2021/09/04)
This disclosure is directed, at least in part, to GPR40 agonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the GPR40 agonists are gut-restricted compounds. In some embodiments, the GPR40 agonists are full agonists or partial agonists. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.
Concise Entries to 4-Halo-2-pyridones and 3-Bromo-4-halo-2-pyridones
Honraedt, Aurélien,Gallagher, Timothy
supporting information, p. 67 - 69 (2015/12/26)
Methods for the synthesis of both simple 4-halo-2-pyridones and more functionalized 3,4-di- and (3,4,5-tri)-halo-2-pyridones are described that are based on a combination of Sandmeyer and regioselective (copper-mediated) halogenation, with a 2-chloro or a 2-benzyloxy moiety serving as a masked 2-pyridone.
Mild and Regioselective N-Alkylation of 2-Pyridones in Water
Hao, Xin,Xu, Zhongmiao,Lu, Hongfu,Dai, Xuedong,Yang, Ting,Lin, Xichen,Ren, Feng
supporting information, p. 3382 - 3385 (2015/07/28)
A mild and regioselective N-alkylation reaction of 2-pyridones in water has been developed. Tween 20 (2% w/w) was added to create a micellar system for improved solubility of starting materials, which leads to enhanced reaction rates. The protocol demonstrated a wide substrate scope with good isolated yields (40-94%) for all of the 24 examples evaluated. High regioselectivity favoring N-alkylation over O-alkylation was observed for benzyl halides (>5:1), primary alkyl halides (>6:1), and bulky and less reactive secondary alkyl halides (>2.4:1).
THIENO[3,2-C]PYRIDIN-4(5H)-ONES AS BET INHIBITORS
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Page/Page column 129, (2014/06/11)
Thienopyridone compounds of formula (I) or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicated.
New compounds, pharmaceutical compositions and uses thereof
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Page/Page column 44, (2012/09/05)
The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
5H-PYRROLO[3,4-£>]PYRAZIN-7-AMINE DERIVATIVES INHIBITORS OF BETA-SECRETASE
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Page/Page column 37, (2011/02/24)
The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β- amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
ANTIVIRAL COMPOUNDS
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Page/Page column 467, (2010/12/17)
The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
3,4 - SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS
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Page/Page column 28-29, (2010/06/22)
The present invention relates to 3,4-substituted piperidinyl - based renin inhibitor compounds bearing at 4-position oxopyridine or lsoquinolone and having the formula (I): wherein., S is Formula (IIa) or Formula (IIb). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.
RENIN INHIBITORS
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Page/Page column 43; 59-60, (2009/07/17)
The present invention relates to piperidinyl-based renin inhibitor compounds having the formula containing amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.