90433-20-8Relevant academic research and scientific papers
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.
PRMT5 INHIBITORS
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Page/Page column 44; 48; 58, (2019/05/30)
The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
MODULATORS OF ROR-GAMMA
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Paragraph 00212; 00213; 00214, (2017/06/12)
Provided are novel compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions comprising the novel compounds of Formula I and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
A: Meta -selective-C-H alkenylation of phenol-derivatives employing a traceless organosilicon template
Mi, Rui-Jie,Sun, Jing,Kühn, Fritz E.,Zhou, Ming-Dong,Xu, Zhaoqing
supporting information, p. 13209 - 13212 (2017/12/26)
A traceless organosilicon template-directed meta-selective-C-H alkenylation of phenols was realized with good yields and high selectivities. The template was readily removable through F--promoted O-Si cleavage under extremely mild conditions or recyclable through a p-TSA catalyzed process. The product was successfully applied in the preparation of a series of meta-alkenylated aromatic compounds.
ISOPROPYL TRIAZOLO PYRIDINE COMPOUNDS
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Paragraph 0069-0071, (2016/12/01)
The present invention provides a compound of the Formula (I) below: Wherein R1 is selected from the group consisting of H, CH3, CN, CH2CN, C(CH3)2CN, and F; R2 is selected from the group consisting of H, O(C1-C3alkyl)R5, CH2CN, and CN; R3 is selected from the group consisting of H, OCH3, CN, C(CH3)2CN, and CH2CN; R4 is selected from the group consisting of H and CH3; R5 is selected from the group consisting of H, CN, C(CH3)2CN, OCH3, S(O)2CH3, and C(CH3)2OH; provided that at least one selected from the group consisting of R1, R2, R3 and R4 is H; or a pharmaceutically acceptable salt thereof, methods of treating diabetes using the compound and a process for preparing the compound.
ISOPROPYL TRIAZOLO PYRIDINE COMPOUNDS
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Page/Page column 18; 19, (2015/07/23)
The present invention provides a compound of the Formula (I) below: Wherein R1 is selected from the group consisting of H, CH3, CN, CH2CN, C(CH3)2CN, and F; R2 is selected from the group consisting of H, O(C1-C3alkyl)R5, CH2CN, and CN; R3 is selected from the group consisting of H, OCH3, CN, C(CH3)2CN, and CH2CN; R4 is selected from the group consisting of H and CH3; R5 is selected from the group consisting of H, CN, C(CH3)2CN, OCH3, S(O)2CH3, and C(CH3)2OH; provided that at least one selected from the group consisting of R1, R2, R3 and R4 is H; or a pharmaceutically acceptable salt thereof, methods of treating diabetes using the compound and a process for preparing the compound.
COMPOUNDS AND METHODS for the inhibition of HDAC
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Paragraph 0130-0131; 0972-0973, (2015/11/24)
Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.
LXR MODULATORS
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Page/Page column 64, (2014/10/04)
The present invention provides compounds of Formula I and Formula II: or pharmaceutically acceptable salts or solvates thereof, as modulators of liver X receptors (LXRs), and compositions comprising any of such novel compounds and methods of use thereof. These compounds are useful as medicaments for treatment and/or prophylaxis for diseases or conditions related to activity of LXRs.
LXR MODULATORS
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Page/Page column 74-75, (2014/09/29)
The present invention provides compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as modulators of liver X receptors (LXR), compositions comprising any of such novel compounds, methods of using these compounds or compositions as medicaments for prevention or treatment of diseases or disorders related to liver X receptor (LXR), as well as methods of preparing these LXR modulators and using them in the manufacture of medicaments.
Meta-selective C-H functionalization using a nitrile-based directing group and cleavable Si-tether
Lee, Sunggi,Lee, Hyelee,Tan, Kian L.
supporting information, p. 18778 - 18781 (2014/01/06)
A nitrile-based template that enables meta-selective C-H bond functionalization was developed. The template is applicable to a range of substituted arenes and tolerates a variety of functional groups. The directing group uses a silicon atom for attachment
