177760-52-0Relevant academic research and scientific papers
NOVEL COMPOUNDS FOR INHIBITION OF JANUS KINASE 1
-
Page/Page column 172-173, (2020/12/11)
An object of the invention is to provide compounds as selective JAK1 inhibitor, a process for preparation of the inhibitors, a composition containing the compounds and utility of the compounds.
Asymmetric synthesis and biological evaluation of imidazole- and oxazole-containing synthetic lipoxin A4 mimetics (sLXms)
de Gaetano, Monica,Butler, Eibhlín,Gahan, Kevin,Zanetti, Andrea,Marai, Mariam,Chen, Jianmin,Cacace, Antonino,Hams, Emily,Maingot, Catherine,McLoughlin, Alisha,Brennan, Eoin,Leroy, Xavier,Loscher, Christine E.,Fallon, Padraic,Perretti, Mauro,Godson, Catherine,Guiry, Patrick J.
, p. 80 - 108 (2018/11/21)
Lipoxins (LXs) are endogenously generated eicosanoids with potent bio-actions consistent with attenuation of inflammation. The costly synthesis and metabolic instability of LXs may limit their therapeutic potential. Here we report the synthesis and charac
ANTIBACTERIAL THERAPEUTICS AND PROPHYLACTICS
-
Paragraph 00382, (2017/02/24)
The present disclosure relates generally to novel molecules, compositions, and formulations for treatment of bacterial infections in general and more specifically to bacterial infections with antibiotic resistant pathogens.
HETEROCYCLIC COMPOUND
-
Paragraph 0601, (2015/01/18)
The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
Tuning and predicting biological affinity: Aryl nitriles as cysteine protease inhibitors
Ehmke, Veronika,Quinsaat, Jose Enrico Q.,Rivera-Fuentes, Pablo,Heindl, Cornelia,Freymond, Céline,Rottmann, Matthias,Brun, Reto,Schirmeister, Tanja,Diederich, Fran?ois
supporting information; experimental part, p. 5764 - 5768 (2012/08/28)
A series of aryl nitrile-based ligands were prepared to investigate the effect of their electrophilicity on the affinity against the cysteine proteases rhodesain and human cathepsin L. Density functional theory calculations provided relative reactivities of the nitriles, enabling prediction of their biological affinity and cytotoxicity and a clear structure-activity relationship.
TRICYCLIC SPIROCYCLE DERIVATIVES AND METHODS OF USE
-
Page/Page column 40, (2011/07/29)
The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or aired fasting glucose.
Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): Structure-activity relationships leading to the identification of 6-((5 S,9 R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7- triazaspiro[4.4]nonan-7-yl)nico
Watterson, Scott H.,Xiao, Zili,Dodd, Dharmpal S.,Tortolani, David R.,Vaccaro, Wayne,Potin, Dominique,Launay, Michele,Stetsko, Dawn K.,Skala, Stacey,Davis, Patric M.,Lee, Deborah,Yang, Xiaoxia,McIntyre, Kim W.,Balimane, Praveen,Patel, Karishma,Yang, Zheng,Marathe, Punit,Kadiyala, Pathanjali,Tebben, Andrew J.,Sheriff, Steven,Chang, Chiehying Y.,Ziemba, Theresa,Zhang, Huiping,Chen, Bang-Chi,Delmonte, Albert J.,Aranibar, Nelly,McKinnon, Murray,Barrish, Joel C.,Suchard, Suzanne J.,Murali Dhar
experimental part, p. 3814 - 3830 (2010/07/05)
Leukocyte function-associated antigen-1 (LFA-1), also known as CD11a/CD18 or αLβ2, belongs to the β2 integrin subfamily and is constitutively expressed on all leukocytes. The major ligands of LFA-1 include three intercellu
METHODS FOR THE PREPARATION OF AZOLE COMPOUNDS
-
Page/Page column 9-10, (2010/02/17)
The present invention is directed to processes, compositions and methods associated with the preparation of azole derivatives of formula I:
Total synthesis of enigmazole a from cinachyrella enigmatica. Bidirectional bond constructions with an ambident 2,4-disubstituted oxazole synthon
Skepper, Colin K.,Quach, Tim,Molinski, Tadeusz F.
body text, p. 10286 - 10292 (2010/09/06)
The first total synthesis of the cytotoxic marine macrolide enigmazole A has been completed in 22 steps (longest linear sequence). The sensitive, densely functionalized 2,4-disubstituted oxazole fragment was constructed using an efficient Negishi-type cou
AMINOALKYLAZOLE DERIVATIVES AS HISTAMINE-3 ANTAGONISTS
-
Page/Page column 33-34, (2009/02/11)
The present invention provides a compound of formula I: and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
