1236357-60-0Relevant articles and documents
PROCESSES FOR PREPARING TRIAZOLE GLYCOLATE OXIDASE INHIBITORS
-
, (2021/07/17)
The present disclosure provides processes for preparing 1,2,3-triazole-4-carboxylic acid related compounds of formulae (I) and (II) via a Suzuki coupling reaction. The Suzuki coupling reaction is achieved by coupling a compound of formula (IV), a boron-containing derivative of 1,2,3-triazole-4-carboxylate, with a cycloalkyl phenyl halide or sulfonate of formula (V).
GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
-
Paragraph 001437; 001438, (2021/01/22)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with a defect in glyoxylate metabolism, for example a disease or disorder associated with the enzyme glycolate oxidase (GO) or alterations in oxalate metabolism. Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.
GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
-
Paragraph 001479; 001480; 001481, (2019/07/17)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme glycolate oxidase (GO). Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies
Bezen?on, Olivier,Heidmann, Bibia,Siegrist, Romain,Stamm, Simon,Richard, Sylvia,Pozzi, Davide,Corminboeuf, Olivier,Roch, Catherine,Kessler, Melanie,Ertel, Eric A.,Reymond, Isabelle,Pfeifer, Thomas,De Kanter, Ruben,Toeroek-Schafroth, Michael,Moccia, Luca G.,Mawet, Jacques,Moon, Richard,Rey, Markus,Capeleto, Bruno,Fournier, Elvire
, p. 9769 - 9789 (2017/12/26)
We report here the discovery and pharmacological characterization of N-(1-benzyl-1H-pyrazol-3-yl)-2-phenylacetamide derivatives as potent, selective, brain-penetrating T-type calcium channel blockers. Optimization focused mainly on solubility, brain penetration, and the search for an aminopyrazole metabolite that would be negative in an Ames test. This resulted in the preparation and complete characterization of compound 66b (ACT-709478), which has been selected as a clinical candidate.
OXAZOLIDINONE HYDROXAMIC ACID COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
-
, (2015/05/19)
This invention pertains generally to treating bacterial infections using organic compounds of Formula I. In certain aspects, the invention pertains to treating infections caused by Gram-negative bacteria. (I) wherein X, Y, R1, R2, R3, R4 and R5 and defined herein.
4-AMINO-5-OXO-7, 8-DIHYDROPYRIMIDO [5,4-F] [1,4] OXAZEPIN-6 (5H) -YL) PHENYL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
-
Page/Page column 44-45, (2010/08/09)
The invention provides compounds of Formula (I), wherein R1, R2a, R2b, R3, m and A are as defined herein, as well as compositions thereof and methods for treating a disease, condition or disorder that is modulated by the inhibition of the diacylglycerol O-acyltransferase 1 (DGAT-1) enzyme by administering the compounds of the present invention and/or compositions thereof.
4-AMINO-7,8-DIHYDROPYRIDO[4,3-d]PYRIMIDIN-5(6H)-ONE DERIVATIVES
-
Page/Page column 15, (2010/08/08)
The invention provides compounds of the general Formula (I) where R1, R2, and A are defined herein, as well as the preparation, compositions and uses thereof.