19620-33-8Relevant academic research and scientific papers
Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors
Anandam, Aravind,Balog, Aaron,Borzilleri, Robert,Cherney, Emily C.,D'arienzo, Celia J.,Delpy, Diane,Dhar, Gopal,Discenza, Lorell N.,Fereshteh, Mark,Foster, Kimberly A.,Grubb, Mary F.,Gullo-Brown, Johnni,Guo, Weiwei,Gupta, Anuradha,Hong, Zhenqiu,Huang, Audris,Huang, Christine,Hunt, John T.,Johnston, Kathy A.,Kempson, James,Kopcho, Lisa,Li, Xin,Lin, Tai-An,Mahankali, Sandeep,Maley, Derrick,Mariappan, T. Thanga,Mathur, Arvind,Murali, Venkata,Nimje, Roshan Y.,Padmanabhan, Shweta,Pattasseri, Shabeerali,Rajanna, Prabhakar,Rampulla, Richard,Ranasinghe, Asoka,Seitz, Steven,Shan, Weifang,Stefanski, Kevin,Traeger, Sarah C.,Vite, Gregory,Williams, David,Yang, Zheng,Zhang, Liping,Zhu, Xiao
, p. 1143 - 1150 (2021/07/19)
IDO1 inhibitors have shown promise as immunotherapies for the treatment of a variety of cancers, including metastatic melanoma and renal cell carcinoma. We recently reported the identification of several novel heme-displacing IDO1 inhibitors, including the clinical molecules linrodostat (BMS-986205) and BMS-986242. Both molecules contain quinolines that, while being present in successful medicines, are known to be potentially susceptible to oxidative metabolism. Efforts to swap this quinoline with an alternative aromatic system led to the discovery of 2,3-disubstituted pyridines as suitable replacements. Further optimization, which included lowering ClogP in combination with strategic fluorine incorporation, led to the discovery of compound 29, a potent, selective IDO1 inhibitor with robust pharmacodynamic activity in a mouse xenograft model.
RADIOLIGANDS FOR IMAGING THE IDO1 ENZYME
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Page/Page column 16; 17, (2018/02/14)
The present invention relates to radiolabeled IDO1 inhibitors or pharmaceutically acceptable salts thereof which are useful for the quantitative imaging of IDO enzymes in mammals.
IMMUNOREGULATORY AGENTS
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Paragraph 0400; 0427, (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, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
IMMUNOREGULATORY AGENTS
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Paragraph 0428, (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, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
IMMUNOREGULATORY AGENTS
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Paragraph 0584, (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,
NOVEL TETRAHYDROISOQUINOLINE DERIVATIVE
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Page/Page column 99; 100, (2010/12/29)
The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent DGAT inhibitory effect and feeding suppressant effect. The present invention provides a compound represented by the general formula (I), or pharmacologically acceptable salt thereof: [wherein, R1 represents a phenylaminocarbonyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group A, a benzoxazol-2-yl group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group A, or the like; R2 independently represents a C1-C6 alkyl group; R3 represents a group represented by the formula -C(=O)-O-R4 or the like; R4 represents a hydrogen atom, a C1-C6 alkyl group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group B, or the like; X represents an oxygen atom, a methylene group, or a group represented by the formula -NH-, or the like; L represents a single bond, a methylene group, or the like;...... represents a single bond or a double bond; m represents 1 or 2; n represents an integer of 0 to 5; Substituent Group A represents a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a C1-C6 alkoxy group, or the like; and Substituent Group B represents a C3-C6 cycloalkyl group, a phenyl group, a carboxyl group, or the like].
Total synthesis of (±)-β-chamigrene and (±)-laurencenone C via Ireland ester Claisen rearrangement and an intramolecular type II carbonyl ene reaction sequence
Srikrishna,Babu, R. Ramesh
, p. 10501 - 10506 (2008/12/23)
A combination of Ireland ester Claisen rearrangement and intramolecular type II carbonyl ene reactions were exploited for the total synthesis of chamigrenes containing a quaternary carbon atom next to the spirocentre in spiro[5.5]undecane.
Total syntheses of (±)-α-acorenol, β-acorenol, α-epi-acorenol and β-epi-acorenol via an Ireland ester Claisen rearrangement and RCM reaction sequence
Srikrishna,Babu, R. Ramesh
, p. 6916 - 6919 (2008/02/13)
Total syntheses of (±)-α- and β-acorenols and (±)-α- and β-epi-acorenols, spiro[4.5]decane sesquiterpenes, isolated from the western Australian sandalwood oil, have been accomplished employing a combination of Ireland ester Claisen rearrangement and RCM r
An Asymmetric Intramolecular Alkylation to form a Bicyclohexanone Derivative
Hamon, David P. G.,Shirley, Nail J.
, p. 425 - 426 (2007/10/02)
The epoxy ketol (-)-2-hydroxymethyl-1-oxaspirooctan-6-one (7b) isomerises with base to 1-(1,2-dihydroxy-1-methylethyl)bicyclohexan-4-one (5b) with high diastereoselectivity.
