1160502-41-9Relevant academic research and scientific papers
UREA, AMIDE, AND SUBSTITUTED HETEROARYL COMPOUNDS FOR CBL-B INHIBITION
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Paragraph 0408, (2021/02/05)
Compounds of formulae (I) and (II), compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells invivo, in vitro, or ex vivo.
Discovery of selective, orally bioavailable pyrazolopyridine inhibitors of protein kinase cθ (pkcθ) that ameliorate symptoms of experimental autoimmune encephalomyelitis
Collier, Philip N.,Twin, Heather C.,Knegtel, Ronald M. A.,Boyall, Dean,Brenchley, Guy,Davis, Christopher J.,Keily, Shazia,Mak, Chau,Miller, Andrew,Pierard, Fran?oise,Settimo, Luca,Bolton, Clare M.,Chiu, Peter,Curnock, Adam,Doyle, Elisabeth,Tanner, Adam J.,Jimenez, Juan-Miguel
supporting information, p. 1134 - 1139 (2019/08/27)
PKCθ plays an important role in T cell biology and is a validated target for a number of disease states. A series of potent and selective PKCθ inhibitors were designed and synthesized starting from a HTS hit compound. Cell activity, while initially a challenge to achieve, was built into the series by transforming the nitrile unit of the scaffold into a primary amine, the latter predicted to form a new hydrogen bond to Asp508 near the entrance of the ATP binding site of PKCθ. Significant improvements in physiochemical parameters were observed on introduction of an oxetane group proximal to a primary amine leading to compound 22, which demonstrated a reduction of symptoms in a mouse model of multiple sclerosis.
INHIBITORS OF CBL-B AND METHODS OF USE THEREOF
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Paragraph 1538, (2019/08/12)
Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.
Efficient one-pot synthesis of dihydroquinolinones in water at room temperature
Linsenmeier, Anna M.,Braje, Wilfried M.
, p. 6913 - 6919 (2015/08/24)
A mild and robust one-pot protocol for the Rh-catalyzed 1,4-addition of 2-aminoboronic acid to α,β-unsaturated esters for the efficient synthesis of dihydroquinolinones has been developed. Furthermore the addition of a variety of substituted boronic acids to diverse α,β-unsaturated esters has been investigated. The reactions proceed in water containing catalytic amounts of the commercially available designer surfactant TPGS-750-M (via the formation of nanomicelles). This mild and easy to perform process proceeds at room temperature and tolerates a wide range of functionalities.
[1H- PYRAZOLO [3, 4-B] PYRIDINE-4-YL] -PHENYLE OR -PYRIDIN-2-YLE DERIVATIVES AS PROTEIN KINASE C-THETA
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Page/Page column 164-165, (2009/07/17)
The present invention relates to compounds of formula (I) and (IA) useful as inhibitors of protein kinase (1a). The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. (a) : in particular protein kinase C theta, wherein A and A' are independently -N- or -C(R+) -. Ring B is five- or six-membered saturated carbocyclic or heterocyclic R1, R2, R3, R4, R5, R6, R7, x and y are as described herein.
