- PIPERIDINYLALKYLAMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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The present invention relates to piperidinylalkylamide derivatives having dual pharmacological activity towards both the sigma (σ) receptor and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising
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Page/Page column 114-115
(2017/11/10)
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- INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
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The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase (e.g., CDK7), and therefore induce cellular apoptosis and/or inhibit transcription in the subject.
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Paragraph 421; 422
(2016/12/26)
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- Two-step synthesis of substituted 3-aminoindazoles from 2-bromobenzonitriles
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A general two-step synthesis of substituted 3-aminoindazoles from 2-bromobenzonitriles involving a palladium-catalyzed arylation of benzophenone hydrazone followed by an acidic deprotection/cyclization sequence is described. This procedure offers a general and efficient alternative to the typical S NAr reaction of hydrazine with o-fluorobenzonitriles.
- Lefebvre, Valerie,Cailly, Thomas,Fabis, Frederic,Rault, Sylvain
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supporting information; experimental part
p. 2730 - 2732
(2010/07/08)
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