197569-11-2Relevant academic research and scientific papers
SUBSTITUTED 1H-IMIDAZO[1, 2-B]PYRAZOLE-3-CARBOXAMIDE AS BRUTON TYROSINE KINASE INHIBITORS
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Page/Page column 27-28, (2022/01/24)
This invention relates to a series of compounds 1H-imidazo [1, 2-b] pyrazole-3-carboxamide substituted represented by formula I used as kinase inhibitors, in particular BTK inhibitors (Bruton tyrosine kinase), and the methods of manufacture and use thereof for the treatment of an autoimmune disease, inflammatory disease, cancer and potentially allergies.
Structure-activity relationship investigation for imidazopyrazole-3-carboxamide derivatives as novel selective inhibitors of Bruton's tyrosine kinase
Ding, Qingjie,He, Xing,Jiang, Yuqin,Li, Wei,Ma, Chunhua,Wang, Yue,Wu, Xiaofang,Xu, Guiqing,Yang, Shouning,Zhang, Dandan,Zhang, Shuting,Zhao, Jie
supporting information, (2021/08/13)
BTK (Bruton's tyrosine kinase) inhibitors are the most promising drugs for the treatment of hematological tumors. A high selectivity of BTK inhibitors ensures reduced side effects from off-targeting. Accordingly, here, based on Zanubrutinib, we designed a
Triazolopyridine and imidazopyridine compounds as well as preparation method and medical application thereof
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Paragraph 0293-0297, (2020/07/13)
The invention relates to triazolopyridine and imidazopyridine compounds as well as a preparation method and medical application thereof. Particularly, the invention relates to a compound as shown in ageneral formula (I), a preparation method thereof and a
QUINOLINE AND QUINAZOLINE COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 00205; 00213; 00361-00362, (2020/10/09)
Compounds and methods for their preparation and use as therapeutic or prophylactic agents, fo example for treatment of cancer, bacterial or viral diseases by targeting Ectonucleotide Pyrophosphatase/Phosphodiesterase- 1 (ENPP1).
Structure-activity relationship study of tryptophan-based butyrylcholinesterase inhibitors
Brazzolotto, Xavier,Gobec, Stanislav,Gro?elj, Uro?,Knez, Damijan,Malikowska-Racia, Natalia,Meden, An?e,Nachon, Florian,Sa?at, Kinga,Svete, Jurij
, (2020/09/15)
A series of tryptophan-based selective nanomolar butyrylcholinesterase (BChE) inhibitors was designed and synthesized. Compounds were optimized in terms of potency, selectivity, and synthetic accessibility. The crystal structure of the inhibitor 18 in complex with BChE revealed the molecular basis for its low nanomolar inhibition (IC50 = 2.8 nM). The favourable in vitro results enabled a first-in-animal in vivo efficacy and safety trial, which demonstrated a positive impact on fear-motivated and spatial long-term memory retrieval without any concomitant adverse motor effects. Altogether, this research culminated in a handful of new lead compounds with promising potential for symptomatic treatment of patients with Alzheimer's disease.
Cyano-substituted cyclic hydrazine derivatives and application thereof
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Paragraph 0221-0227, (2019/12/02)
The invention provides cyano-substituted cyclic hydrazine derivatives. The cyano-substituted cyclic hydrazine derivatives are characterized in that the cyano-substituted cyclic hydrazine derivatives are compounds as shown in the following structural formula shown in the specification or stereoisomers, geometrical isomers, tautomers, racemates, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof; the compounds are useful for the prevention, treatment, treatment or amelioration of autoimmune diseases or proliferative diseases in patients, and/or for the inhibition or modulation of protein kinase activity.
ECTONUCLEOTIDE PYROPHOSPHATASE-PHOSPHODIESTERASE 1 (ENPP-1) INHIBITORS AND USES THEREOF
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Paragraph 0437, (2019/03/17)
Disclosed herein are methods and compounds of augmenting and enhancing the production of type I IFNs in vivo. In some embodiments, the compounds disclosed herein are ENPP-1 inhibitors, pharmaceutical compositions, and methods for the treatment of cancer or a viral infection.
Synthesis and biological evaluation of novel quinazoline-4-piperidinesulfamide derivatives as inhibitors of NPP1
Forcellini, Elsa,Boutin, Sophie,Lefebvre, Carole-Anne,Shayhidin, Elnur Elyar,Boulanger, Marie-Chloé,Rhéaume, Gabrielle,Barbeau, Xavier,Lagüe, Patrick,Mathieu, Patrick,Paquin, Jean-Fran?ois
, p. 130 - 149 (2018/02/14)
The ecto-nucleotide pyrophosphatase/phosphodiesterase-1 (NPP1) was recently shown to promote mineralization of the aortic valve, hence, its inhibition represents a significant target. A quinazoline-4-piperidine sulfamide compound (QPS1) has been described as a specific and non-competitive inhibitor of NPP1. We report herein the synthesis and in vitro inhibition studies of novel quinazoline-4-piperidine sulfamide analogues using QPS1 as the lead compound. Of the 26 derivatives prepared, four compounds were found to have Ki 105 nM against human NPP1.
Synthesis of novel substituted pyrimidine derivatives bearing a sulfamide group and their in vitro cancer growth inhibition activity
Lefebvre, Carole-Anne,Forcellini, Elsa,Boutin, Sophie,C?té, Marie-France,C.-Gaudreault, René,Mathieu, Patrick,Lagüe, Patrick,Paquin, Jean-Fran?ois
supporting information, p. 299 - 302 (2016/12/27)
The synthesis of two series of novel substituted pyrimidine derivatives bearing a sulfamide group have been described and their in vitro cancer growth inhibition activities have been evaluated against three human tumour cell lines (HT-29, M21, and MCF7). In general, growth inhibition activity has been enhanced by the introduction of a bulky substituent on the aromatic ring with the best compound having GI50??6?μM for all the human tumour cell lines. The MCF7 selective compounds were evaluated on four additional human invasive breast ductal carcinoma cell lines (MDA-MB-231, MDA-MB-468, SKBR3, and T47D) and were selective against T47D cell line in all cases except one, suggesting a potential antiestrogen activity.
Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes
Storer, R. Ian,Pike, Andy,Swain, Nigel A.,Alexandrou, Aristos J.,Bechle, Bruce M.,Blakemore, David C.,Brown, Alan D.,Castle, Neil A.,Corbett, Matthew S.,Flanagan, Neil J.,Fengas, David,Johnson, M. Scott,Jones, Lyn H.,Marron, Brian E.,Payne, C. Elizabeth,Printzenhoff, David,Rawson, David J.,Rose, Colin R.,Ryckmans, Thomas,Sun, Jianmin,Theile, Jonathan W.,Torella, Rubben,Tseng, Elaine,Warmus, Joseph S.
supporting information, p. 4805 - 4811 (2017/10/17)
The discovery and selection of a highly potent and selective NaV1.7 inhibitor PF-06456384, designed specifically for intravenous infusion, is disclosed. Extensive in vitro pharmacology and ADME profiling followed by in vivo preclinical PK and efficacy model data are discussed. A proposed protein–ligand binding mode for this compound is also provided to rationalise the high levels of potency and selectivity over inhibition of related sodium channels. To further support the proposed binding mode, potent conjugates are described which illustrate the potential for development of chemical probes to enable further target evaluation.
