188577-70-0Relevant academic research and scientific papers
Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-RafV600E inhibitors
Li, Xiaokai,Shen, Jiayi,Tan, Li,Zhang, Zhang,Gao, Donglin,Luo, Jinfeng,Cheng, Huimin,Zhou, Xiaoping,Ma, Jie,Ding, Ke,Lu, Xiaoyun
, p. 2760 - 2763 (2016)
B-RafV600E was an effective target for the treatment of human cancers. Based on a pan-Raf inhibitor TAK-632, a series of N-(4-aminopyridin-2-yl)amide derivatives were designed as novel B-RafV600E inhibitors. Detailed structure-activi
IMPROVED METHODS, KITS, COMPOSITIONS AND DOSING REGIMENS FOR THE USE OF HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2
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Page/Page column 132-133, (2021/05/07)
The present application provides improved compositions, methods, kits and dosing regimens for the use of heterocyclic compounds and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, or stereoisomers thereof. These compositions, methods, kit
HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Paragraph 000294, (2020/02/06)
The present invention discloses compounds useful in treatment of conditions associated with excessive activity of transforming growth factor beta (TGF-β), particularly type 1 or activin-like kinase 5 (ALK 5). Specifically the present invention discloses compound of formula (I) which exhibit inhibitory activity against ALK 5. Method of treating conditions associated with excessive activity (ALK 5) with such compound is disclosed. Uses thereof, pharmaceutical composition, and kits are also disclosed.
Palladium-Catalyzed Site-Selective Amidation of Dichloroazines
Young, Ian S.,Glass, Anna-Lena,Cravillion, Theresa,Han, Chong,Zhang, Haiming,Gosselin, Francis
supporting information, p. 3902 - 3906 (2018/07/25)
A highly site-selective amidation reaction of substituted 2,4-dichloroazines is reported. Palladium acetate/1,1′-bis(diphenylphosphino)ferrocene (dppf) was identified as the optimal catalyst system, producing >99:1 C-2/C-4 selectivity for most examples. The generality of this transformation was demonstrated through a survey of a diverse amide/substituted 2,4-dichloroazine scope, leading to the preparation of the desired C-2 amidated products in good to excellent yields.
HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATMENT OF CANCER
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Paragraph 0554-0555, (2017/01/02)
The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a
NOVEL HETEROCYCLIC DERIVATIVES AND THEIR USES
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Paragraph 0865-0867, (2014/10/29)
The present invention relates to novel heterocyclic compounds useful in preparing drugs for treatment of diseases associated with various functions of the histamine 4 receptor. Especially, the said drugs are useful for treatment of inflammatory diseases, allergy, pain, nasal polyps, rhinitis, chronic sinusitis, nasal congestion, nasal itch, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis, eczema, pruritus, itchy skin, urticaria, idiopathic chronic urticaria, scleroderma, conjunctivitis, keratoconjunctivitis, ocular inflammation, dry eye, cardiac dysfunction, arrhythmia, atherosclerosis, multiple sclerosis, inflammatory bowel disease (including colitis, Crohn's disease, ulcerative colitis), inflammatory pain, neuropathic pain, osteoarthritic pain, autoimmune thyroid disease, immune-mediated (also known as type I) diabetes, lupus, post-operative adhesions, vestibular disorders and cancer.
NOVEL IMIDAZOPYRIDINE DERIVATIVES AS A TYROSINE KINASE INHIBITOR
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Page/Page column 13; 14, (2013/07/19)
Provided is a novel imidazopyridine derivative having irreversible tyrosine kinase inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of inflammatory diseases, autoimmune diseases, p
NAPHTHYRIDININONES AS AURORA KINASE INHIBITORS
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Page/Page column 55-56, (2010/04/03)
Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative di
3 -AZABICYCLO [4.1.0] HEPTANES USED AS OREXIN ANTAGONISTS
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Page/Page column 65-66, (2010/11/05)
This invention relates to 3-azabicyclo[4.1.0] heptane derivatives (I) and their use as orexin receptor antagonists.
PYRAZIN-2-YL-PYRIDIN-2-YL-AMINE AND PYRAZIN-2-YL-PYRIMIDIN-4-YL-AMINE COMPOUNDS AND THEIR USE
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Page/Page column 218-219, (2009/05/29)
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin- 2 - yl -pyridin- 2 -yl -amine and pyrazine - 2 - yl -pyrimidin- 4 - yl -amine compounds of formula (I), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1 ) kinase function The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1. that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or Il inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionisiπq radiation. wherein: -X= is independently -CRA5= or -N=; and the rest of the substituents are as specified in the claims.
