411238-92-1Relevant academic research and scientific papers
A Rh(III)-Catalyzed Formal [4+1] Approach to Pyrrolidines from Unactivated Terminal Alkenes and Nitrene Sources
Lee, Sumin,Lei, Honghui,Rovis, Tomislav
, p. 12536 - 12540 (2019/08/26)
We have developed a formal [4+1] approach to pyrrolidines from readily available unactivated terminal alkenes as 4-carbon partners. The reaction provides a rapid construction of various pyrrolidine containing structures, especially for the diastereoselect
Polycyclic compound and its pharmaceutical composition and application
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, (2018/03/26)
The invention discloses a polycyclic compound and its preparation method, pharmaceutical composition and application. The polycyclic compound (I) and its isomer, prodrug, stable isotope derivative ora pharmaceutically acceptable salt have the structure shown in the description. The polycyclic compound has good IDO1 inhibitory effects and can be used for effectively treating, alleviating and/or preventing various related diseases such as tumors and infectious diseases caused by immunosuppression.
IMMUNOREGULATORY AGENTS
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, (2016/06/01)
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,
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.
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.
Synthesis and biological evaluation of aminobenzimidazole derivatives with a phenylcyclohexyl acetic acid group as anti-obesity and anti-diabetic agents
Kwak, Hyun Jung,Pyun, Yu Mi,Kim, Ji Young,Pagire, Haushabhau S.,Kim, Ki Young,Kim, Kwang Rok,Rhee, Sang Dal,Jung, Won Hoon,Song, Jin Sook,Bae, Myung Ae,Lee, Duck Hyung,Ahn, Jin Hee
, p. 4713 - 4718 (2013/08/23)
A series of benzimidazole derivatives with a phenylcyclohexyl acetic acid group as DGAT-1 inhibitors was developed. Among the benzimidazole series, compound 5k showed submicromolar in vitro activity toward human and mouse DGAT-1, good selectivity toward D
MONOACYLGLYCEROL LIPASE INHIBITORS FOR MODULATION OF CANNABINOID ACTIVITY
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Page/Page column 126, (2009/05/28)
Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.
