3693-08-1Relevant academic research and scientific papers
PEPTIDOMIMETIC N5-METHYL-N2-(NONANOYL-L-LEUCYL)-L-GLUTAMINATE DERIVATIVES, TRIAZASPIRO[4.14]NONADECANE DERIVATIVES AND SIMILAR COMPOUNDS AS INHIBITORS OF NOROVIRUS AND CORONAVIRUS REPLICATION
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Paragraph 00215; 00446-00447, (2021/09/26)
Peptidomimetic N5-methyl-N2-(nonanoyl-L-leucyl)-L-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds for use in methods of inhibiting the replication of noroviruses and coronaviruses in a biological sample or patient, for use in reducing the amount of noroviruses or coronaviruses in a biological sample or patient, and for use in treating norovirus and coronavirus in a patient, comprising administering to said biological sample or patient a safe and effective amount of a compound represented by formulae I or II, or a pharmaceutically acceptable salt thereof. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. page 99 to page 271; examples 1 to 3; compounds A1 to A104 and Bl to B66; tables A to E).
Identification and characterization of the first fragment hits for SETDB1 Tudor domain
Mader,Mendoza-Sanchez, Rodrigo,Iqbal, Aman,Dong, Aiping,Dobrovetsky,Corless, Victoria B.,Liew, Sean K.,Houliston, Scott R.,De Freitas, Renato Ferreira,Smil,Sena, Carlo C. Dela,Kennedy, Steven,Diaz, Diego B.,Wu, Hong,Dombrovski, Ludmila,Allali-Hassani, Abdellah,Min, Jinrong,Schapira, Matthieu,Vedadi, Masoud,Brown, Peter J.,Santhakumar, Vijayaratnam,Yudin, Andrei K.,Arrowsmith, Cheryl H.
, p. 3866 - 3878 (2019/07/23)
SET domain bifurcated protein 1 (SETDB1) is a human histone-lysine methyltransferase which is amplified in human cancers and was shown to be crucial in the growth of non-small and small cell lung carcinoma. In addition to its catalytic domain, SETDB1 harb
Efficient synthesis of benzene-fused 6/7-membered amides: Via Xphos Pd G2 catalyzed intramolecular C-N bond formation
Xu, Zhou,Li, Ke,Zhai, Rongliang,Liang, Ting,Gui, Xiaodie,Zhang, Rongli
, p. 51972 - 51977 (2017/11/22)
An efficient approach for benzene-fused 6/7-membered amides via intramolecular amidation of aryl chlorides catalyzed by a Buchwald-Hartwig second generation Pd catalyst (Xphos Pd G2) has been successfully developed. This catalyst system allows the primary amides which have only modest nucleophilicity to be coupled successfully even with electron rich aryl chlorides in short reaction time. The intramolecular amidation reaction also has good chemoselectivity and excellent functional group compatibility.
Rh2(II)-Catalyzed Ring Expansion of Cyclobutanol-Substituted Aryl Azides to Access Medium-Sized N-Heterocycles
Mazumdar, Wrickban,Jana, Navendu,Thurman, Bryant T.,Wink, Donald J.,Driver, Tom G.
, p. 5031 - 5034 (2017/05/04)
A new reactivity pattern of Rh2(II)-N-arylnitrenes was discovered that facilitates the synthesis of medium-sized N-heterocycles from ortho-cyclobutanol-substituted aryl azides. The key ring-expansion step of the catalytic cycle is both chemosel
GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO
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Page/Page column 42-43, (2008/12/04)
GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
LXR modulators
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Page/Page column 62, (2010/11/26)
A compound of formula I wherein A, X, q, R1, R2a, R2b, R2c, R3a, and R3b are defined herein.
Substituted pyridoindoles as serotonin agonists and antagonists
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, (2008/06/13)
The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k
Substituted pyridoindoles as serotonin agonists and antagonists
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, (2008/06/13)
The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k
Substituted pyridoindoles as serotonin agonists and antagonists
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, (2008/06/13)
The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k
