- Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-RafV600E inhibitors
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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
- Li, Xiaokai,Shen, Jiayi,Tan, Li,Zhang, Zhang,Gao, Donglin,Luo, Jinfeng,Cheng, Huimin,Zhou, Xiaoping,Ma, Jie,Ding, Ke,Lu, Xiaoyun
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Read Online
- IMPROVED METHODS, KITS, COMPOSITIONS AND DOSING REGIMENS FOR THE USE OF HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2
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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
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Page/Page column 132-133
(2021/05/07)
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- HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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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.
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Paragraph 000294
(2020/02/06)
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- Palladium-Catalyzed Site-Selective Amidation of Dichloroazines
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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.
- Young, Ian S.,Glass, Anna-Lena,Cravillion, Theresa,Han, Chong,Zhang, Haiming,Gosselin, Francis
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supporting information
p. 3902 - 3906
(2018/07/25)
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- HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATMENT OF CANCER
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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
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Paragraph 0554-0555
(2017/01/02)
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- NOVEL HETEROCYCLIC DERIVATIVES AND THEIR USES
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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.
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Paragraph 0865-0867
(2014/10/29)
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- NOVEL IMIDAZOPYRIDINE DERIVATIVES AS A TYROSINE KINASE INHIBITOR
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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
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Page/Page column 13; 14
(2013/07/19)
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- NAPHTHYRIDININONES AS AURORA KINASE INHIBITORS
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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
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Page/Page column 55-56
(2010/04/03)
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- 3 -AZABICYCLO [4.1.0] HEPTANES USED AS OREXIN ANTAGONISTS
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This invention relates to 3-azabicyclo[4.1.0] heptane derivatives (I) and their use as orexin receptor antagonists.
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Page/Page column 65-66
(2010/11/05)
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- PYRAZIN-2-YL-PYRIDIN-2-YL-AMINE AND PYRAZIN-2-YL-PYRIMIDIN-4-YL-AMINE COMPOUNDS AND THEIR USE
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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.
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Page/Page column 218-219
(2009/05/29)
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- Enzyme Inhibitors
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Compounds of formula (I), are aurora kinase inhibitors: wherein X is —N—, —CH2—N—, —CH2—CH—, or —CH—; R1 is a radical of formula (IA) wherein Z is —CH2—, —NH—, -0-, —S(O)— —S—, —S(O)2 or a divalent monocyclic carbocyclic or heterocyclic radical having 3-7 ring atoms; Alk is an optionally substituted divalent C1-C6 alkylene radical; A is hydrogen or an optionally substituted monocyclic carbocyclic or heterocyclic ring having 5-7 ring atoms; r, s and t are independently 0 or 1, provided that when A is hydrogen then at least one of r and s is 1; R2 is halogen, —CN, —CF3, —OCH3, or cyclopropyl; and R3 is a radical of formula (IB) wherein Q is hydrogen or an optionally substituted phenyl or monocyclic heterocyclic ring with 5 or 6 ring atoms; Z[!It!]1> is —S—, —S(O)—, —S(O)2—, —O—, —SO2NH—, —NHSO2—, NHC(═O)NH, —NH(C═S)NH—, Or —N(R4)—wherein R4 is hydrogen, C1-C3 alkyl, cycloalkyl, or benzyl; and Alk[!It!]1> and Alk[!It!]2> are, independently, optionally substituted divalent C1-C3 alkylene radicals; and m, n and p are independently 0 or 1. Data supplied from the esp@cenet datatbase—Worldwide d77
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Page/Page column 6
(2009/10/06)
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- Imidazo[1,2-a]pyridine C-nucleosides as antiviral agents
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This invention pertains to nucleoside analogs that have antiviral activity and improved metabolic stability, compositions comprising them, and methods of antiviral treatment employing them. More particularly, this invention pertains to imidazo[1,2-a]pyridine C-nucleosides, as exemplified by compounds such as imidazo[l,2-a]pyridine C5-nucleosides and imidazo[1,2-a]pyridine C3-nucleosides, and may be represented by formula (I), wherein exactly one of Q3and Q5is a sugar-like moiety; exactly one of Q3and Q5is —H; and Q2, Q6, Q7and Q8are independently imidazo[1,2-a]pyridine substituents, such as —H, —F, —Cl, —Br and —I.
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- An improved large scale synthesis of 2-amino-4-chloropyridine and its use for the convenient preparation of various polychlorinated 2-aminopyridines
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An efficient large scale synthesis of 2-amino-4-chloropyridine (3) has been achieved through a modification of existing literature procedures. Compound 3 was used to prepare the previously unreported 2-amino-4,5-dichloropyridine (4). The known 2-amino-3,4-dichloropyridine (5) and 2-amino-3,4,5-trichloropyridine (6) were pepared from 3 by new routes and in higher yields than previously reported.
- Gudmundsson, Kristjan S.,Hinkley, Jack M.,Brieger, Michael S.,Drach, John C.,Townsend, Leroy B.
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p. 861 - 870
(2007/10/03)
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