134419-59-3Relevant academic research and scientific papers
Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis
Klug, Dana M.,Mavrogiannaki, Eftychia M.,Forbes, Katherine C.,Silva, Lisseth,Diaz-Gonzalez, Rosario,Pérez-Moreno, Guiomar,Ceballos-Pérez, Gloria,Garcia-Hernández, Raquel,Bosch-Navarrete, Cristina,Cordón-Obras, Carlos,Gómez-Li?án, Claudia,Saura, Andreu,Momper, Jeremiah D.,Martinez-Martinez, Maria Santos,Manzano, Pilar,Syed, Ali,El-Sakkary, Nelly,Caffrey, Conor R.,Gamarro, Francisco,Ruiz-Perez, Luis Miguel,Gonzalez Pacanowska, Dolores,Ferrins, Lori,Navarro, Miguel,Pollastri, Michael P.
supporting information, p. 9404 - 9430 (2021/07/25)
Neglected tropical diseases such as human African trypanosomiasis (HAT) are prevalent primarily in tropical climates and among populations living in poverty. Historically, the lack of economic incentive to develop new treatments for these diseases has meant that existing therapeutics have serious shortcomings in terms of safety, efficacy, and administration, and better therapeutics are needed. We now report a series of 3,5-disubstituted-7-azaindoles identified as growth inhibitors of Trypanosoma brucei, the parasite that causes HAT, through a high-throughput screen. We describe the hit-to-lead optimization of this series and the development and preclinical investigation of 29d, a potent antitrypanosomal compound with promising pharmacokinetic (PK) parameters. This compound was ultimately not progressed beyond in vivo PK studies due to its inability to penetrate the blood-brain barrier (BBB), critical for stage 2 HAT treatments.
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis
Bello, Davide,Braillard, Stéphanie,Caljon, Guy,Carvalho, Sandra,Corpas-Lopez, Victoriano,Freund, Yvonne,Gilbert, Ian H.,Glossop, Paul A.,Jacobs, Robert T.,Lukac, Iva,Maes, Louis,Mowbray, Charles E.,Nare, Bakela,Pandi, Bharathi,Patterson, Stephen,Speake, Jason,Van Den Kerkhof, Magali,Wall, Richard J.,Whitlock, Gavin A.,Wyllie, Susan,Yardley, Vanessa,Zuccotto, Fabio
supporting information, p. 16159 - 16176 (2021/11/16)
Visceral leishmaniasis (VL) is a parasitic disease endemic across multiple regions of the world and is fatal if untreated. Current therapies are unsuitable, and there is an urgent need for safe, short-course, and low-cost oral treatments to combat this ne
AZAINDOLE DERIVATIVE AND USE THEREOF AS FGFR AND C-MET INHIBITOR
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Paragraph 0125; 0130, (2021/05/29)
A series of pyrazolopymidine derivatives, and use thereof in the preparation of a medicament for treating disease associated with FGFR and c-Met. The pyrazolopymidine derivative is a compound represented by formula (I), a tautomer, or a pharmaceutically acceptable salt thereof.
6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS
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Paragraph 0269; 0270, (2021/11/13)
The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
PYRROLO(PYRAZOLO)PYRIMIDINE DERIVATIVE AS LRRK2 INHIBITOR
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, (2020/11/23)
The present invention relates to a pyrrolo(pyrazolo)pyrimidine derivative having efficacy as an LRRK2 inhibitor, a preparation method therefor, and a pharmaceutical composition for preventing or treating degenerative brain diseases, containing the same.
Optimizing Pyrazolopyrimidine Inhibitors of Calcium Dependent Protein Kinase 1 for Treatment of Acute and Chronic Toxoplasmosis
Janetka, James W.,Hopper, Allen T.,Yang, Ziping,Barks, Jennifer,Dhason, Mary Savari,Wang, Qiuling,Sibley, L. David
supporting information, p. 6144 - 6163 (2020/07/10)
Calcium dependent protein kinase 1 (CDPK1) is an essential Ser/Thr kinase that controls invasion and egress by the protozoan parasite Toxoplasma gondii. The Gly gatekeeper of CDPK1 makes it exquisitely sensitive to inhibition by small molecule 1H-pyrazolo
PYRROLOTRIAZINE DERIVATIVES FOR TREATING KIT- AND PDGFRA-MEDIATED DISEASES
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Paragraph 00236-00237, (2020/10/21)
The present disclosure provides compounds of Formula I, pharmaceutical salts thereof, and/or solvates of any of the foregoing which are useful for treating diseases and conditions related to mutant KIT and PDGFRa and present an advantageously non-brain pe
Quinoline Derivatives and Their Use as ALK and ALK L1196M Inhibitors
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Paragraph 0243-0244; 0280-0281; 0287, (2019/05/04)
The present invention relates to quinoline derivatives and a use thereof as inhibitors of ALK and mutated ALK. A pharmaceutical composition containing quinoline derivatives of chemical formula 1 or each of pharmaceutically acceptable salt thereof, has an effect of preventing or treating diseases associated with ALK and ALK L1196M, in other words, proliferative diseases caused by abnormal cell growth and function or behavior thereof.COPYRIGHT KIPO 2019
TAM KINASE INHIBITORS
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Paragraph 0165, (2019/02/02)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat diseases, such as cancer.
Novel heterocyclic derivative capable of being used as SHP2 inhibitor
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Paragraph 0329, (2019/08/30)
The invention relates to a novel heterocyclic derivative capable of being used as an SHP2 inhibitor, specifically relates to a compound shown by a formula I or pharmaceutically acceptable salts thereof, further relates to a use of the compound shown by the formula I or the pharmaceutically acceptable salts thereof and a pharmaceutical composition thereof in drug preparation, and particularly relates to a use in preparation of drugs for treatment, inhibition or prevention of diseases or discomforts mediated by SHP2 activity.
