- NOVEL HETEROCYCLIC COMPOUNDS AND USE THEREOF IN MEDICINE AND IN COSMETICS
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The invention relates to novel heterocyclic compounds of general formula (I), as well as their pharmaceutically acceptable salts, and their enantiomers. The invention also relates to the use thereof as a medicinal product, preferably in the prevention and/or treatment of inflammatory diseases with a neurogenic component or use thereof as a cosmetic. The compounds of the present invention act as antagonists of the CGRP-R receptor.
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- Discovery of Novel KRAS-PDEδ Inhibitors by Fragment-Based Drug Design
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Targeting KRAS-PDEδ protein-protein interactions with small molecules represents a promising opportunity for developing novel antitumor agents. However, current KRAS-PDEδ inhibitors are limited by poor cellular antitumor potency and the druggability of the target remains to be validated by new inhibitors. To tackle these challenges, herein, novel, highly potent KRAS-PDEδ inhibitors were identified by fragment-based drug design, providing promising lead compounds or chemical probes for investigating the biological functions and druggability of KRAS-PDEδ interaction.
- Chen, Long,Zhuang, Chunlin,Lu, Junjie,Jiang, Yan,Sheng, Chunquan
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supporting information
p. 2604 - 2610
(2018/03/26)
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- Dihydro quinazolinone derivative, as well as preparation method and application thereof
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The invention relates to the technical field of medicines, in particular to a new dihydro quinazolinone derivative with the following chemical structure general formula and pharmaceutically acceptablesalts thereof, (the formula is shown in the description.), A pharmacological experiment shows that the derivative or the salt provided by the invention has higher inhibitory activity on KRAS-PDE delta protein interaction, and has higher anti-tumor activity in vitro. The invention also provides a preparation method of the derivative and the pharmaceutically acceptable salts thereof, and application to preparatioin of a KRAS-PDE delta inhibitor and an anti-tumor drug.
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Paragraph 0171; 0172
(2018/07/30)
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- DIPHENYLBUTYPIPERIDINE AUTOPHAGY INDUCERS
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Autophagy inducing compounds, methods of their preparation and use, and kits containg said compounds are disclosed herein.
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Page/Page column 8; 87-90
(2011/12/02)
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- Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: Effects of fused heterocycles on antiviral activity and pharmacokinetic properties
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A series of 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists containing a variety of fused heterocycles at the 4-position of the piperidine side chain has been discovered, which are orally bioavailable with potent anti-HIV activity.
- Kim, Dooseop,Wang, Liping,Hale, Jeffrey J.,Lynch, Christopher L.,Budhu, Richard J.,MacCoss, Malcolm,Mills, Sander G.,Malkowitz, Lorraine,Gould, Sandra L.,Demartino, Julie A.,Springer, Martin S.,Hazuda, Daria,Miller, Michael,Kessler, Joseph,Hrin, Renee C.,Carver, Gwen,Carella, Anthony,Henry, Karen,Lineberger, Janet,Schleif, William A.,Emini, Emilio A.
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p. 2129 - 2134
(2007/10/03)
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- Modified aminoacids, pharmaceuticals containing these compounds and method for their production
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The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4and R11are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
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Example A10a)
(2008/06/13)
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- Modified amino acids, pharmaceuticals containing these compounds and method for their production
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The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
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- Pyrrolidine modulators of chemokine receptor activity
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The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R14and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
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