Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies

Journal of Medicinal Chemistry

Volumn 60, Issue 23, 2017, Pages 9769-9789

  Bezençon, Olivier ^a   Heidmann, Bibia ^a   Siegrist, Romain ^a   Stamm, Simon ^a   Richard, Sylvia ^a   Pozzi, Davide ^a   Corminboeuf, Olivier ^a   Roch, Catherine ^a   Kessler, Melanie ^a   Ertel, Eric A ^a   Reymond, Isabelle ^a   Pfeifer, Thomas ^a   De Kanter, Ruben ^a   Toeroek Schafroth, Michael ^a   Moccia, Luca G ^a   Mawet, Jacques ^a   Moon, Richard ^a   Rey, Markus ^a   Capeleto, Bruno ^a   Fournier, Elvire ^a  

^a IDORSIA PHARMACEUTICALS LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

2 [4 [1 (TRIFLUOROMETHYL)CYCLOPROPYL]PHENYL]ACETIC ACID; 6 [(3 AMINO 1H PYRAZOL 1 YL)METHYL]NICOTINONITRILE; ACT 709478; ANTICONVULSIVE AGENT; BENZIMIDAZOLE; BENZOIC ACID; CALCIUM CHANNEL BLOCKING AGENT; CALCIUM CHANNEL T TYPE; CARBOXYLIC ACID; METHYL GROUP; N [1 [(5 CYANOPYRIDIN 2 YL)METHYL] 1H PYRAZOL 3 YL] 2 [4 [1 (TRIFLUOROMETHYL)CYCLOPROPYL] PHENYL]ACETAMIDE; PHENYLACETIC ACID; PYRAZOLE DERIVATIVE; TERT BUTYL 2 [4 [1 (TRIFLUOROMETHYL)CYCLOPROPYL]PHENYL]ACETATE; TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG; 2-PHENYLACETAMIDE; BENZENEACETAMIDE DERIVATIVE;

ABSENCE LIKE SEIZURE; AEROBIC METABOLISM; ALKYLATION; ALLOMETRY; AMES TEST; ANIMAL TISSUE; ARTICLE; AUDIOGENIC SEIZURE; BENZYLATION; CLONIC SEIZURE; CYCLIZATION; CYCLOADDITION; DESS MARTIN OXIDATION; DRUG CLEARANCE; DRUG HALF LIFE; DRUG PENETRATION; DRUG POTENCY; DRUG SOLUBILITY; DRUG STABILITY; DRUG SYNTHESIS; ELECTROENCEPHALOGRAPHY; ENANTIOMER; GENERALIZED EPILEPSY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; HUMAN TISSUE; HYDROBORATION; HYDROGEN BOND; HYDROLYSIS; IC50; IN VITRO STUDY; IN VIVO STUDY; INTRINSIC CLEARANCE; LIQUID CHROMATOGRAPHY-MASS SPECTROMETRY; LIVER CELL; LIVER MICROSOME; METABOLIC ACTIVATION; METABOLIC STABILITY; MUTAGENICITY; NONHUMAN; NUCLEOPHILICITY; PHYSICAL CHEMISTRY; PROTON NUCLEAR MAGNETIC RESONANCE; RAT; REVERTANT; SALMONELLA ENTERICA SEROVAR TYPHIMURIUM; STRUCTURE ACTIVITY RELATION; ANIMAL; BRAIN; CHEMISTRY; DOG; DRUG DEVELOPMENT; DRUG EFFECTS; GUINEA PIG; MACACA FASCICULARIS; METABOLISM; WISTAR RAT;

ANIMALS; BENZENEACETAMIDES; BRAIN; CALCIUM CHANNEL BLOCKERS; CALCIUM CHANNELS, T-TYPE; DOGS; DRUG DISCOVERY; EPILEPSY, GENERALIZED; GUINEA PIGS; HUMANS; MACACA FASCICULARIS; PYRAZOLES; RATS, WISTAR; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 85038380630     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.7b01236     Document Type: Article

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