153888-45-0Relevant articles and documents
6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS
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Paragraph 0446; 0447, (2021/11/13)
The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
Compound with BRD4 inhibitory activity, preparation method and application thereof
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Paragraph 0185-0189, (2021/04/10)
The invention discloses a compound with BRD4 inhibitory activity, a preparation method and application thereof. The structure of the compound with the BRD4 inhibitory activity is shown as a formula I, and definitions of substituent groups are shown in the specification and claims. The compound provided by the invention has very high bromodomain protein inhibition activity, especially BRD4 targeted inhibition activity, and can be used for treating or/and preventing related diseases mediated by bromodomain protein.
Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition
Fearon, Daren,Westwood, Isaac M.,van Montfort, Rob L.M.,Bayliss, Richard,Jones, Keith,Bavetsias, Vassilios
supporting information, p. 3021 - 3029 (2018/05/25)
Screening a 3-aminopyridin-2-one based fragment library against a 26-kinase panel representative of the human kinome identified 3-amino-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2(1H)-one (2) and 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one (3) as ligand efficient inhibitors of the mitotic kinase Monopolar Spindle 1 (MPS1) and the Aurora kinase family. These kinases are well recognised as attractive targets for therapeutic intervention for treating cancer. Elucidation of the binding mode of these fragments and their analogues has been carried out by X-ray crystallography. Structural studies have identified key interactions with a conserved lysine residue and have highlighted potential regions of MPS1 which could be targeted to improve activity and selectivity.
New Pyridinones and Isoquinolinones as Inhibitors of the Bromodomain BRD9
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Paragraph 0443-0444, (2018/03/25)
The present invention encompasses compounds of general formula (I) wherein the groups R1 to R9, X1 and X2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, e.g. cancer, pharmaceutical preparations containing such compounds and their uses as a medicament.
Development of a scalable synthesis of a Bruton's tyrosine kinase inhibitor via C-N and C-C bond couplings as an end game strategy
Hong, Jun Bae,Davidson, James P.,Jin, Qingwu,Lee, Gary R.,Matchett, Michael,O'Brien, Erin,Welch, Michael,Bingenheimer, Bill,Sarma, Keshab
, p. 228 - 238 (2014/05/20)
A scalable and convergent synthesis of a BTK (Bruton's tyrosine kinase) inhibitor has been developed. Synthetic routes to key intermediates were explored for the scale-up campaign, especially the process for 6-dimethylaminodihydroisoquinolinone, which was prepared via a regioselective cyclization of an isocyanate, mediated by AlCl3. Improved routes to key building blocks were demonstrated by expedient multikilogram productions. The target compound was assembled through a Pd-catalyzed amidation reaction followed by a Suzuki-Miyaura cross-coupling reaction.
PYRIDINONES/PYRAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF
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Page/Page column 110, (2012/03/26)
Pyridone and pyrazinone compounds of Formula (I) including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF
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Page/Page column 39-40, (2009/04/24)
Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are de
Calcitonin gene-related peptide (CGRP) receptor antagonists: Investigations of a pyridinone template
Nguyen, Diem N.,Paone, Daniel V.,Shaw, Anthony W.,Burgey, Christopher S.,Mosser, Scott D.,Johnston, Victor,Salvatore, Christopher A.,Leonard, Yvonne M.,Miller-Stein, Cynthia M.,Kane, Stefanie A.,Koblan, Kenneth S.,Vacca, Joseph P.,Graham, Samuel L.,Williams, Theresa M.
, p. 755 - 758 (2008/09/16)
In our effort to find potent, orally bioavailable CGRP receptor antagonists for the treatment of migraine, a novel series based on a pyridinone template was investigated. After optimizing the privileged structure and the placement of the attached phenyl r
CGRP RECEPTOR ANTAGONISTS
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Page/Page column 69, (2010/11/23)
Compounds of Formula (I), (where variables R1, A, B, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.