52802-20-7Relevant academic research and scientific papers
Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kδ
Pujala, Brahmam,Agarwal, Anil K.,Middya, Sandip,Banerjee, Monali,Surya, Arjun,Nayak, Anjan K.,Gupta, Ashu,Khare, Sweta,Guguloth, Rambabu,Randive, Nitin A.,Shinde, Bharat U.,Thakur, Anamika,Patel, Dhananjay I.,Raja, Mohd.,Green, Michael J.,Alfaro, Jennifer,Avila, Patricio,Pérez de Arce, Felipe,Almirez, Ramona G.,Kanno, Stacy,Bernales, Sebastián,Hung, David T.,Chakravarty, Sarvajit,McCullagh, Emma,Quinn, Kevin P.,Rai, Roopa,Pham, Son M.
supporting information, p. 1161 - 1166 (2016/12/16)
The aberrant activation of B-cells has been implicated in several types of cancers and hematological disorders. BTK and PI3Kδ are kinases responsible for B-cell signal transduction, and inhibitors of these enzymes have demonstrated clinical benefit in certain types of lymphoma. Simultaneous inhibition of these pathways could result in more robust responses or overcome resistance as observed in single agent use. We report a series of novel compounds that have low nanomolar potency against both BTK and PI3Kδ as well as acceptable PK properties that could be useful in the development of treatments against B-cell related diseases.
HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Paragraph 0209; 0244, (2015/05/05)
The present application discloses compounds that are inhibitors of Btk, compounds that are inhibitors of ΡΒΚδ, and compounds that are dual inhibitors of both Btk and PI3Kδ. Also described are methods for synthesizing such inhibitors and methods for using such inhibitors for the treatment of diseases wherein inhibition of Btk and PI3Kδ provides a therapeutic benefit to a patient having the disease.
Synthesis and evaluation of dimeric 1,2,3,4-Tetrahydro-naphthalenylamine and Indan-1-ylamine derivatives with mast cell-stabilising and anti-allergic activity
Barlow, James W.,Walsh, John J.
experimental part, p. 25 - 37 (2010/03/04)
In a continuation of our studies into 4-Amino-3,4-dihydro-2H-naphthalen-1-ones as novel modulators of allergic and inflammatory phenomena, we have extended our work to include dimeric analogues. Of these derivatives, the most promising activity was seen with tertiary amine 58a, which exhibited potent mast cell-stabilising activity in vitro against a variety of stimuli and also in vivo against passive cutaneous anaphylaxis.
Herbicidal bicyclic compounds
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, (2008/06/13)
This invention relates to certain bicyclic derivatives which are indane and tetralin compounds and which have herbicidal properties, to processes for their preparation, to herbicidal compositions containing them and to a method of using them as herbicides
