917910-75-9Relevant academic research and scientific papers
Amine compound inhibiting SSAO/VAP-1 and application thereof in medicine
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Paragraph 0906; 0907; 0908; 0909, (2019/02/04)
The invention relates to an amine compound for inhibiting semicarbazide-sensitive amine oxidase (SSAO) and/or vascular adhesion protein 1 (VAP-1) and medicinal application thereof, and further relatesto a pharmaceutical composition containing the compound
OCTAHYDROPYRIDO[1,2-ALPHA]PYRAZINES AS MAGL INHIBITORS
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Page/Page column 84, (2019/07/20)
The invention provides new heterocyclic compounds having the general formula (le), wherein R1, R1a and R7 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods
NITROGEN-CONTAINING AROMATIC HETEROCYCLYL COMPOUND
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Page/Page column 56, (2011/04/25)
The present invention provides a compound having excellent regulating action on blood lipid level. The present invention provides a compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, etc., wherein A represents a 5-membered nitrogen-containing aromatic heterocyclyl group; R1 represents COOH or the like; each R2 represents an alkyl or the like; each R3 represents an optionally substituted phenyl, an optionally substituted phenylalkyl, or the like; m represents 0, 1, 2, or 3; n represents 0 or 1; each of R4, R5, R6, and R7 represents H, an alkyl, or the like; and B represents an optionally substituted naphthyl, an optionally substituted aromatic heterocyclyl, or a group represented by the following formula (II) wherein each of B1 and B2 represents an optionally substituted phenyl or an optionally substituted aromatic heterocyclyl.
The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties
Imbriglio, Jason E.,Dirocco, Daniel,Bodner, Rena,Raghavan, Subharekha,Chen, Weichun,Marley, Daria,Esser, Craig,Holt, Tom G.,Wolff, Michael S.,Taggart, Andrew K.P.,Waters, M. Gerard,Tata, James R.,Colletti, Steven L.
supporting information; scheme or table, p. 2721 - 2724 (2011/06/20)
Amino-anthranilic acid derivatives have been identified as a new class of low serum shifted, high affinity full agonists of the human orphan G-protein-coupled receptor GPR109a with improved ADME properties.
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): A potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate
Shen, Hong C.,Ding, Fa-Xiang,Raghavan, Subharekha,Deng, Qiaolin,Luell, Silvi,Forrest, Michael J.,Carballo-Jane, Ester,Wilsie, Larissa C.,Krsmanovic, Mihajlo L.,Taggart, Andrew K.,Wu, Kenneth K.,Wu, Tsuei-Ju,Cheng, Kang,Ren, Nina,Cai, Tian-Quan,Chen, Qing,Wang, Junying,Wolff, Michael S.,Tong, Xinchun,Holt, Tom G.,Waters, M.Gerard,Hammond, Milton L.,Tata, James R.,Colletti, Steven L.
supporting information; experimental part, p. 2666 - 2670 (2010/08/22)
Biaryl cyclohexene carboxylic acids were discovered as full and potent niacin receptor (GPR 109A) agonists. Compound 1e (MK-6892) displayed excellent receptor activity, good PK across species, remarkably clean off-target profiles, good ancillary pharmacology, and superior therapeutic window over niacin regarding the FFA reduction versus vasodilation in rats and dogs.
Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment
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Page/Page column 53, (2009/04/24)
The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.
NIACIN RECEPTOR AGONISTS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Page/Page column 24; 30, (2008/12/05)
The present invention encompasses compounds of Formula (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also
NIACIN RECEPTOR AGONISTS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Page/Page column 31; 55, (2008/06/13)
The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.
NIACIN RECEPTOR AGONISTS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Page/Page column 25; 36, (2008/06/13)
The present invention encompasses compounds of Formula (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dysliptdemias and the like. Pharmaceutical compositions and methods of use are also
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor
Shen, Hong C.,Ding, Fa-Xiang,Luell, Silvi,Forrest, Michael J.,Carballo-Jane, Ester,Wu, Kenneth K.,Wu, Tsuei-Ju,Cheng, Kang,Wilsie, Larissa C.,Krsmanovic, Mihajlo L.,Taggart, Andrew K.,Ren, Ning,Cai, Tian-Quan,Deng, Qiaolin,Chen, Qing,Wang, Junying,Wolff, Michael S.,Tong, Xinchun,Holt, Tom G.,Waters, M. Gerard,Hammond, Milton L.,Tata, James R.,Colletti, Steven L.
, p. 6303 - 6306 (2008/04/12)
Biaryl anthranilides are reported as potent and selective full agonists for the high affinity niacin receptor GPR109A. The SAR presented outlines approaches to reduce serum shift and both CYPCYP2C8 and CYP2C9 liabilities, while improving PK and maintainin
