189884-30-8Relevant articles and documents
Synthesis and α-adrenergic activity of 2- and 6-methyl-substituted (3,4-dihydroxyphenyl)-3-piperidinols
Macchia, B.,Macchia, M.,Martinelli, A.,Martinotti, E.,Orlandini, E.,et al.
, p. 231 - 240 (1997)
Previous drug-receptor interaction mechanism studies at the molecular level of adrenergic drugs made it possible to construct two three-dimensional molecular models, A and B, using conformationally restrained cyclic analogues of natural catecholamines, including 3-(3,4-dihydroxyphenyl)-3-piperidinol (3-DPP, 3); these models offer useful information about the steric requirements for the direct activation of α1- and α2-adrenergic receptors, respectively.In order to gain further knowledge about the steric requirements of these receptors, we also synthesized 3-(3,4-dihydroxyphenyl)-c-2-methyl-r-3-piperidinol (2-MDPP, 8) and the 3-(3,4-dihydroxyphenyl)-c- and -t-6-methyl-r-3-piperidinols (6-MDPPs 9 and 10); these differ from the 3-DPP 3 used for the construction of the molecular models exclusively in the presence of a methyl in the 2 or 6 position of the heterocyclic ring.The configuration and conformation of the MDPPs 8-10 were assigned by 1H-NMR and IR studies, and confirmed by conformational analysis performed by means of theoretical calculations.The α1- and α2-adrenergic properties were evaluated in vitro both by radioligand binding assays and by functional tests on isolated preparations.The results obtained made it possible to obtain a more refined steric definition of the A and B models. - Keywords: 3-piperidinol derivative; adrenergic α-stimulating activity; conformational analysis; molecular model.
IDH1 mutant micromolecule inhibitor, and preparation method and application thereof
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Paragraph 0242-0243; 0245, (2019/07/16)
The invention discloses an IDH1 mutant micromolecule inhibitor, and a preparation method and application thereof. The structure of the inhibitor is as shown in a formula I, and the definition of the substituent groups is as described in the specification
KRAS G12C INHIBITORS
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Paragraph 0640, (2019/05/24)
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
KRAS G12C INHIBITORS
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Paragraph 0362, (2017/12/18)
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
P2X7 MODULATORS
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Paragraph 0493, (2014/09/30)
The present invention is directed to a compound of Formula (I) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
PYRIMIDINONE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 206, (2008/12/08)
The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of G protein-coupled receptor 119 ("GPR119") in a patient.