- 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 72
(2017/07/06)
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- HETEROARYL SUBSTITUTED PYRAZOLE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
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This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.
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Page/Page column 75
(2009/01/20)
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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 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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- Activation of Exocyclic α-Positions of Azole N-Oxides by O-Silylation
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Exocyclic α-positions at immonium ring carbon atoms of pyrazole and 1,2,3-triazole 1-oxides are selectively attacked in a one-pot sequence comprising silylation with iodotrimethylsilane, deprotonation with 1,2,2,6,6-pentamethylpiperidine and allylic substitution of the trimethylsilyloxy group with the iodide ions liberated by the silylation.In this way 3- and 5-iodomethylpyrazoles as well as 4-iodomethyl-1,2,3-triazoles are obtained in good yields.These may be useful for the preparation of heteroarylmethyl derivatives since the iodine atom can be displaced by even weak nucleophiles such as acetate ions.The side chain iodination is complementary to O-alkylation of the N-oxides followed by nucleophilic attack which preferentially takes place at ring carbon atoms.
- Begtrup, Mikael,Vedso, Per
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p. 2555 - 2564
(2007/10/02)
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