1260160-79-9Relevant academic research and scientific papers
Direct C-H Alkenylation of Functionalized Pyrazoles
Han, Su Jin,Kim, Hyun Tae,Joo, Jung Min
, p. 689 - 698 (2016)
We have developed inter- and intramolecular C-H alkenylation reactions of pyrazoles. The catalyst, derived from Pd(OAc)2 and pyridine, enabled the oxidative alkenylation of pyrazoles containing a variety of functional groups at the C4 position.
Alkynyl pyrimidine or alkynyl pyridine compound as well as composition and application thereof
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Paragraph 0109-0111, (2020/08/18)
The invention relates to alkynyl pyrimidine or alkynyl pyridine compounds represented by a formula (I) or pharmaceutically acceptable salts, isomers, solvates, crystals or prodrugs thereof. The invention also discloses a pharmaceutical composition contain
COMPOUNDS, COMPOSITIONS AND METHODS OF USE
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Page/Page column 287-288, (2020/07/06)
Herein, compounds, compositions and methods for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmological diseases, and viral infections are described.
Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling
Zak, Mark,Hanan, Emily J.,Lupardus, Patrick,Brown, David G.,Robinson, Colin,Siu, Michael,Lyssikatos, Joseph P.,Romero, F. Anthony,Zhao, Guiling,Kellar, Terry,Mendonca, Rohan,Ray, Nicholas C.,Goodacre, Simon C.,Crackett, Peter H.,McLean, Neville,Hurley, Christopher A.,Yuen, Po-wai,Cheng, Yun-Xing,Liu, Xiongcai,Liimatta, Marya,Kohli, Pawan Bir,Nonomiya, Jim,Salmon, Gary,Buckley, Gerry,Lloyd, Julia,Gibbons, Paul,Ghilardi, Nico,Kenny, Jane R.,Johnson, Adam
supporting information, p. 1522 - 1531 (2019/04/25)
Disruption of interleukin-13 (IL-13) signaling with large molecule antibody therapies has shown promise in diseases of allergic inflammation. Given that IL-13 recruits several members of the Janus Kinase family (JAK1, JAK2, and TYK2) to its receptor complex, JAK inhibition may offer an alternate small molecule approach to disrupting IL-13 signaling. Herein we demonstrate that JAK1 is likely the isoform most important to IL-13 signaling. Structure-based design was then used to improve the JAK1 potency of a series of previously reported JAK2 inhibitors. The ability to impede IL-13 signaling was thereby significantly improved, with the best compounds exhibiting single digit nM IC50’s in cell-based assays dependent upon IL-13 signaling. Appropriate substitution was further found to influence inhibition of a key off-target, LRRK2. Finally, the most potent compounds were found to be metabolically labile, which makes them ideal scaffolds for further development as topical agents for IL-13 mediated diseases of the lungs and skin (for example asthma and atopic dermatitis, respectively).
For the treatment of tumor macrocyclic derivatives (by machine translation)
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Paragraph 0111-0112; 0184-0185, (2017/07/20)
The invention discloses a method for modulating protein kinase activity, and is used for the treatment or prevention of protein kinase related disorders. Specifically, the invention relates to a method for the treatment of tumor of the macrocyclic derivatives, which belongs to the regulating Anaplastic lymphoma kinase (ALK) active compound, and provides the preparation method of the compound, and the compound used for the treatment or prevention of diseases associated with the ALK pharmaceutical use. (by machine translation)
BICYCLIC LACTAMS AND METHODS OF USE THEREOF
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Page/Page column 147-148, (2017/01/23)
The invention provides novel compounds having the general formula I: (I) wherein R1, X, Z1, L, n, the A ring, the B ring, and the C ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.
FACTOR XIa INHIBITORS
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Page/Page column 200, (2017/05/21)
The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein.
MACROCYCLES WITH HETROCYCLIC P2' GROUPS AS FACTOR XIA INHIBITORS
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Page/Page column 176; 177; 308; 309, (2015/09/23)
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of
MACROCYCLIC FACTOR XIA INHIBITORS CONDENSED WITH HETEROCYCLES
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Page/Page column 82; 83; 93; 94, (2015/09/23)
The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
5-CHLORO-2-DIFLUOROMETHOXYPHENYL PYRAZOLOPYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF
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Paragraph 0482, (2015/12/05)
Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.
