898790-15-3Relevant academic research and scientific papers
Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mG
Bollinger, Sean R.,Engers, Darren W.,Panarese, Joseph D.,West, Mary,Engers, Julie L.,Loch, Matthew T.,Rodriguez, Alice L.,Blobaum, Anna L.,Jones, Carrie K.,Thompson Gray, Analisa,Conn, P. Jeffrey,Lindsley, Craig W.,Niswender, Colleen M.,Hopkins, Corey R.
, p. 342 - 358 (2018/10/20)
This work describes the discovery and characterization of novel 6-(1H-pyrazolo[4,3-b]pyridin-3-yl)amino-benzo[d]isothiazole-3-carboxamides as mGlu4 PAMs. This scaffold provides improved metabolic clearance and CYP1A2 profiles compared to previo
INDAZOLE INHIBITORS OF FRUCTOKINASE (KHK) AND METHODS OF USE IN TREATING KHK-MEDIATED DISORDERS OR DISEASES
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, (2018/10/19)
Disclosed herein are novel indazole-based compounds that inhibit fructokinase (aka ketohexokinase) and the downstream metabolic effects mediated by fructose metabolism. Fructokinase inhibitors specifically block the metabolism of both dietary and endogenous fructose metabolism and have a host of potential metabolic benefits. These benefits including blocking sugar craving and sugar induced metabolic syndrome and diabetes, but also blocking fructose metabolism can benefit the rare orphan disease Hereditary Fructose Intolerance, obesity, insulin resistance, metabolic syndrome, fatty liver, hypertension, cardiac injury from ischemia, certain cancers (including hepatocellular and pancreas), acute kidney injury from ischemia, heat stress, rhabdomyolysis or radiocontrast, and chronic diabetic and nondiabetic renal disease.
NOVEL SUBSTITUTED INDOLE AND INDAZOLE COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS
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, (2019/01/10)
The invention relates to novel indole and indazole compounds characterized in that the compound has general formula (I), in which the chemical groupings, substituents, variables and indices are as defined in the description, and to their use as medicament
MODULATORS OF ROR-GAMMA
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Paragraph 00293; 00298; 00299, (2017/06/12)
Provided are novel compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions comprising the novel compounds of Formula I and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
DIFLUOROMETHYLENE COMPOUND
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, (2015/06/16)
The present invention relates to a compound having an URAT1 inhibitory activity, and to an URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition containing the compound. More specifically, the present invention relates to a compound represented by the formula (I): wherein R1 is -Q1-A1 or the like; R2 is a hydrogen atom, a halogen atom, a lower alkyl group or the like; W1, W2, W3 and W4 are each independently a nitrogen atom or a methine group optionally having substituents, or the like; X and Y are each a single bond, an oxygen atom or the like; Z is a hydroxyl group or COOR3 or the like.
RING-FUSED COMPOUND
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Paragraph 0860-0861, (2014/01/07)
The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below. [in the formula, R1 is -Q1-A1 and the like; ---- is a double bond or a single bond; when ---- is a double bond, W1 is a nitrogen atom or a group represented by the general formula: =C(Ra)-, and W2 is a nitrogen atom or a group represented by the general formula: =C(Rb) -; when ---- is a single bond, W1 is a group represented by the general formula: -C(Raa)(Rab)- or a group represented by the general formula: -(C=O) -, and W2 is a group represented by the general formula: C(Rba)(Rbb)-, a group represented by the general formula: - (C=O) - or a group represented by the general formula: -N(Rbc)-; W3, W4 and W5 are each independently a nitrogen atom or a methine group and the like that may have a substituent; X is a single bond, an oxygen atom and the like; Y is a single bond or (CRYiRYi')n; and Z is a hydroxyl group or COOR2 and the like.
