- GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
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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.
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Paragraph 001235; 001237; 001255; 001256
(2021/01/22)
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- GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
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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.
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Paragraph 001277; 001278; 001280; 001297; 001298; 001299
(2019/07/17)
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- Discovery of 6-(Fluoro-18F)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine ([18F]-MK-6240): A Positron Emission Tomography (PET) Imaging Agent for Quantification of Neurofibrillary Tangles (NFTs)
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Neurofibrillary tangles (NFTs) made up of aggregated tau protein have been identified as the pathologic hallmark of several neurodegenerative diseases including Alzheimer's disease. In vivo detection of NFTs using PET imaging represents a unique opportuni
- Walji, Abbas M.,Hostetler, Eric D.,Selnick, Harold,Zeng, Zhizhen,Miller, Patricia,Bennacef, Idriss,Salinas, Cristian,Connolly, Brett,Gantert, Liza,Holahan, Marie,O'Malley, Stacey,Purcell, Mona,Riffel, Kerry,Li, Jing,Balsells, Jaume,Obrien, Julie A.,Melquist, Stacey,Soriano, Aileen,Zhang, Xiaoping,Ogawa, Aimie,Xu, Serena,Joshi, Elizabeth,Della Rocca, Joseph,Hess, Fred J.,Schachter, Joel,Hesk, David,Schenk, David,Struyk, Arie,Babaoglu, Kerim,Lohith, Talakad G.,Wang, Yaode,Yang, Kun,Fu, Jianmin,Evelhoch, Jeffrey L.,Coleman, Paul J.
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p. 4778 - 4789
(2016/06/13)
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- PYRROLO[2,3-C]PYRIDINES AS IMAGING AGENTS FOR NEUROFIBRILARY TANGLES
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Pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts are disclosed, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha- synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, the compounds are used as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. Futher, the compounds are useful for measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.
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- CYCLOALKYLAMINE SUBSTITUTED ISOQUINOLINE DERIVATIVES
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The invention relates to 6-substituted isoquinoline derivatives of the Formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
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Page/Page column 110
(2008/12/06)
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- ISOQUINOLINE DERIVATIVES AS INHIBITORS OF RHO-KINASE
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The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I); useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
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Page/Page column 110-111
(2008/06/13)
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