- TRIAZOLOPYRIDIN-3-ONES OR THEIR SALTS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
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The present technology provides triazolopyridin-3-ones or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The triazolopyridin-3-ones or their pharmaceutically acceptable salts exhibit inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
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- SUBSTITUTED OXOPYRIDINE DERIVATIVES
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The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular vascular disorders, preferably thrombotic
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Page/Page column 160
(2020/07/14)
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- TRIAZOLONES DERIVATIVES FOR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
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The present invention relates to a compound having the general formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, codrug, cocrystal, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
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Page/Page column 32; 33
(2017/04/18)
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- Pyrido[1,2-a]pyrimidone analogs as PI3K inhibitors
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The present invention discloses a class of pyrido[1,2-a]pyrimidone analogs as PI3K inhibitors, and particularly relates to a compound represented by a formula (I) or a pharmaceutically acceptable salt thereof. The formula (I) is defined in the specification.
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Paragraph 0355; 0360; 0361; 0362
(2016/10/08)
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- PYRIDO[1,2-a]PYRIMIDONE DERIVATIVES AS A mTOR/PI3K SUPPRESSOR
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The invention discloses pyrido[1,2-a]pyrimidone derivatives as a mTOR/PI3K suppressor; and in particular, this invention relates to a compound having the formula (I) structure or its pharmaceutically acceptable salts.
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Paragraph 0122; 0123
(2016/10/08)
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- TRIAZOLOPYRIDINE COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS
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The invention relates to a compound of Formula I or IA and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:
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Paragraph 0098; 0099
(2016/05/02)
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- Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine
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Previously we disclosed the discovery of potent Late INa current inhibitor 2 (GS-458967, IC50 of 333 nM) that has a good separation of late versus peak Nav1.5 current, but did not have a favorable CNS safety window due to high brain penetration (3-fold higher partitioning into brain vs plasma) coupled with potent inhibition of brain sodium channel isoforms (Nav1.1, 1.2, 1.3). We increased the polar surface area from 50 to 84 ?2 by adding a carbonyl to the core and an oxadiazole ring resulting in 3 GS-462808 that had lower brain penetration and serendipitously lower activity at the brain isoforms. Compound 3 has an improved CNS window (>20 rat and dog) relative to 2, and improved anti-ischemic potency relative to ranolazine. The development of 3 was not pursued due to liver lesions in 7 day rat toxicology studies.
- Koltun, Dmitry O.,Parkhill, Eric Q.,Elzein, Elfatih,Kobayashi, Tetsuya,Jiang, Robert H.,Li, Xiaofen,Perry, Thao D.,Avila, Belem,Wang, Wei-Qun,Hirakawa, Ryoko,Smith-Maxwell, Catherine,Wu, Lin,Dhalla, Arvinder K.,Rajamani, Sridharan,Mollova, Nevena,Stafford, Brian,Tang, Jennifer,Belardinelli, Luiz,Zablocki, Jeff A.
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supporting information
p. 3207 - 3211
(2016/06/13)
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- SUBSTITUTED FUSED HETEROCYCLES AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS
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The present invention relates to substituted fused heterocyclic compounds. The substituted fused heterocyclic compounds are GPR1 19 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of substituted fused heterocyclic compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
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Page/Page column 57
(2015/11/17)
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- TRIAZOLOPYRIDINONE PDE10 INHIBITORS
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The present invention is directed to triazolopyridinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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Page/Page column 37
(2013/06/05)
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- Fused Heterocyclic Compounds as Ion Channel Modulators
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The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
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Page/Page column 53
(2012/01/15)
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- BICYCLIC TRIAZOLONE DERIVATIVES AND HERBICIDES CONTAINING THE SAME
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The present invention provides a bicyclic triazolone derivative represented by the formula:J-Ar [wherein, J is and Ar is ], which has excellent selective weeding activity and weed killer containing the said bicyclic triazolone derivative.
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