- Novel Compounds
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The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C- terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c, R1d, R1e, R1f, R1g, R2, X, L and A are as defined herein.
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Page/Page column 71; 72
(2017/07/06)
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- TRICYCLIC FUSED INDOLE DERIVATIVES AND THEIR USE AS AURORA KINASE INHIBITORS
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Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them an
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Page/Page column 19-20
(2010/11/25)
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- Monocyclic heterocycles as kinase inhibitors
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The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.
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Page/Page column 94
(2008/06/13)
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- Pyrazolecarboxamide human neuropeptide Y5 receptor ligands with in vivo antifeedant activity
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1-Aryl-3-carboxamido-5-alkylpyrazoles were prepared based on a hit found in high-throughput screening of our corporate compound library in an assay measuring affinity for the human neuropeptide Y5 receptor. 1-(3-Trifluoromethylphenyl)-3-[N-(5-quinolinyl)carboxamido]-5-methylpyrazole (31) bound to the human neuropeptide Y5 receptor with a 80 nM IC50and was shown to inhibit cumulative food consumption 43.2% 2-6 h after ip dosing in a fasting-induced feeding model in rats.
- Kordik, Cheryl P.,Luo, Chi,Zanoni, Brian C.,Lovenberg, Timothy W.,Wilson, Sandy J.,Vaidya, Anil H.,Crooke, Jeffrey J.,Rosenthal, Daniel I.,Reitz, Allen B.
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p. 2287 - 2290
(2007/10/03)
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- Orientation de la reaction d'alkylation des pyrazoles dans des conditions neutres et en catalyse par transfert de phase
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The N-butylation and N-benzylation of nine pyrazoles bearing different substituents in positions 3 and 5 have been studied in neutral and basic medium (phase transfer catalysis).The orientation of the reaction depends strongly on the method used when the
- Tarrago, Georges,Ramdani, Abdelkrim,Elguero, Jose,Espada, Modesta
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p. 137 - 142
(2007/10/02)
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