- COMPOUNDS FOR TREATMENT OF CARDIAC ARRHYTHMIAS AND HEART FAILURE
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This disclosure concerns compounds and a method for modulating the activity of calcium ion channels, including Ca2+-induced (or Ca2+-activated) calcium release channels and conformationally coupled calcium release channels such as ryanodine receptors. Some of the compounds have a structure according to formula I, or a stereoisomer, tautomer, hydrate, solvate, prodrug, or pharmaceutically acceptable salt thereof.
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Page/Page column 6; 80
(2019/10/19)
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- N-Arylation of Carbamates through Photosensitized Nickel Catalysis
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A highly efficient method of visible light mediated Ni(II)-catalyzed photoredox N-arylation of Cbz-amines/Boc-amines with aryl electrophiles at room temperature is reported. The methodology provides a common access to a wide variety of N-aromatic and N-heteroaromatic carbamate products that find use in the synthesis of several biologically active molecules and provides a distinct advantage over traditional palladium-catalyzed Buchwald reaction.
- Reddy, Leleti Rajender,Kotturi, Sharadsrikar,Waman, Yogesh,Ravinder Reddy, Vudem,Patel, Chirag,Kobarne, Ajinath,Kuttappan, Sasikumar
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p. 13854 - 13860
(2018/10/31)
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- Synthesis of 3-Aminoimidazo[1,2-a]pyridines from α-Aminopyridinyl Amides
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3-Aminoimidazo[1,2-a]pyridines are rapidly synthesized via a facile and mild cyclodehydration-aromatization reaction starting from readily available amides. The cyclodehydration step is mediated by the activation of N-Boc-protected 2-aminopyridine-containing amides by triflic anhydride (Tf2O) in the presence of 2-methoxypyridine (2-MeO-Py). Subsequently, the addition of K2CO3 in THF ensured a clean deprotection-aromatization sequence to afford the desired heterocycle. A wide variety of functional groups and substitution patterns were tolerated under the optimized procedure, and good to excellent yields were obtained for the fused bicyclic 3-aza-heterocycles. In addition, the reaction was found to be scalable to gram-scale and could be performed with unprotected acyclic amide precursors. We also found that the resulting products were valuable intermediates for both Pd- and Ru-catalyzed C-H arylation reactions, allowing for the elaboration to diversely functionalized building blocks.
- Régnier, Sophie,Bechara, William S.,Charette, André B.
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p. 10348 - 10356
(2016/11/17)
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- DERIVATIVES OF QUINOLINES AND QUINOXALINES AS PROTEIN TYROSINE KINASE INHIBITORS
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The invention relates to compounds of Formula (I), wherein the substituens are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to p
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Page/Page column 122-123
(2009/12/27)
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- IMIDAZOLE DERIVATIVES USED AS TAFIA INHIBITORS
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The invention relates to compounds of formula (I), which are inhibitors of the activated thrombin-activatable fibrinolysis inhibitor. The compounds of formula (I) are suited for producing medicaments for the prevention and treatment of diseases accompanied by thromboses, embolisms, hypercoagulability or fibrotic changes.
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Page/Page column 49
(2010/02/14)
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- ANDROGEN RECEPTOR ANTAGONISTS
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The present invention provides an androgen receptor antagonistic agent and a superior prophylactic or therapeutic agent for hormone-sensitive cancer, which contain a compound of the formula: wherein, R1 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom; R2 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, R3 is a hydrogen atom, a hydrocarbon group which may have substituent (s) , an acyl group or a heterocyclic group which may have substituent(s), R4 is a hydrogen atom, a group binding through a carbon atom, a group binding through a nitrogen atom, a group binding through an oxygen atom or a group binding through a sulfur atom, and R5 is a cyclic group which may have substituent(s); or a salt thereof, or its prodrug.
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