701232-68-0Relevant academic research and scientific papers
IMMUNOREGULATORY AGENTS
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, (2016/01/27)
Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
NOVEL BETA-ALANINE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS ACTIVE INGREDIENT
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Paragraph 0062-0064, (2015/03/16)
The present invention relates to a beta-alanine derivative, pharmaceutically acceptable salts thereof, and a pharmaceutical composition including the same as an active ingredient. The novel beta-alanine derivative and pharmaceutically acceptable salts the
Development of novel benzomorpholine class of diacylglycerol acyltransferase i inhibitors
Zhou, Gang,Zorn, Nicolas,Ting, Pauline,Aslanian, Robert,Lin, Mingxiang,Cook, John,Lachowicz, Jean,Lin, Albert,Smith, Michelle,Hwa, Joyce,Van Heek, Margaret,Walker, Scott
, p. 544 - 549 (2014/06/09)
Diacylglycerol acyltransferase 1 (DGAT1) presents itself as a potential therapeutic target for obesity and diabetes for its important role in triglyceride biosynthesis. Herein we report the rational design of a novel class of DGAT1 inhibitors featuring a
Discovery of 6-phenylpyrimido[4,5- B ][1,4]oxazines as potent and selective Acyl CoA: Diacylglycerol acyltransferase 1 (DGAT1) inhibitors with in vivo efficacy in rodents
Fox, Brian M.,Sugimoto, Kazuyuki,Iio, Kiyosei,Yoshida, Atsuhito,Zhang, Jian,Li, Kexue,Hao, Xiaolin,Labelle, Marc,Smith, Marie-Louise,Rubenstein, Steven M.,Ye, Guosen,McMinn, Dustin,Jackson, Simon,Choi, Rebekah,Shan, Bei,Ma, Ji,Miao, Shichang,Matsui, Takuya,Ogawa, Nobuya,Suzuki, Masahiro,Kobayashi, Akio,Ozeki, Hidekazu,Okuma, Chihiro,Ishii, Yukihito,Tomimoto, Daisuke,Furakawa, Noboru,Tanaka, Masahiro,Matsushita, Mutsuyoshi,Takahashi, Mitsuru,Inaba, Takashi,Sagawa, Shoichi,Kayser, Frank
, p. 3464 - 3483 (2014/05/20)
The discovery and optimization of a series of acyl CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitors based on a pyrimido[4,5-b][1,4]oxazine scaffold is described. The SAR of a moderately potent HTS hit was investigated resulting in the discovery of phenylcyclohexylacetic acid 1, which displayed good DGAT1 inhibitory activity, selectivity, and PK properties. During preclinical toxicity studies a metabolite of 1 was observed that was responsible for elevating the levels of liver enzymes ALT and AST. Subsequently, analogues were synthesized to preclude the formation of the toxic metabolite. This effort resulted in the discovery of spiroindane 42, which displayed significantly improved DGAT1 inhibition compared to 1. Spiroindane 42 was well tolerated in rodents in vivo, demonstrated efficacy in an oral triglyceride uptake study in mice, and had an acceptable safety profile in preclinical toxicity studies.
Proton exchange reactions in isotope chemistry (II) synthesis of stable isotope-labeled LCQ908
Jian, Zhigang,Ray, Tapan,Wu, Amy,Jones, Lawrence,Forseth, Ry
, p. 670 - 673 (2015/02/02)
The proton exchange reaction was applied to the preparation of stable isotope-labeled LCQ908. For this synthesis, a suitable intermediate with protons alpha to a carbonyl group was first subjected to the H-D exchange reaction; subsequent coupling of a car
4-AMINO-5-OXO-7,8-DIHYDROPYRIMIDO[5, 4 -F] [1, 4] OXAZEPINE COMPOUNDS AS DGAT1 INHIBITORS
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, (2013/05/23)
Described herein are compounds of formula (I). The compounds of formula (I) act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
LACTAM DERIVATIVES AS DGAT-1 INHIBITORS
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, (2012/09/22)
Described herein are compounds of formula I The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
COMPOSITIONS AND METHODS FOR MODULATING LPA RECEPTORS
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, (2012/10/18)
The present invention relates to compounds of Formula (1), or pharmaceutically acceptable salts thereof and their pharmaceutical compositions, wherein variables are as defined herein, which are useful as modulators of the activity of lysophosphatidic acid (LPA).
DIACYLETHYLENEDIAMINE COMPOUND
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Page/Page column 14, (2012/03/10)
[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition
BENZIMIDAZOLES AND THEIR USE FOR THE TREATEMNT OF DIABETES
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, (2008/06/13)
Compounds of formula (I), or salts thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, (A chemical formula should be inserted here - please see paper copy enclosed herewith) (I) wherein: Rsup
