348640-07-3Relevant academic research and scientific papers
General methods for the synthesis and late-stage diversification of 2,4-substituted 7-azaindoles
Varnes, Jeffrey G.,McGuire, Thomas,Meadows, Rebecca E.,Barlaam, Bernard,Clark, Jemma,Cook, Calum R.,Davison, Gemma,Dishington, Allan,De Savi, Chris,Donald, Craig,Grebe, Tyler,Hande, Sudhir,Hawkins, Janet,Hird, Alexander W.,Holmes, Jane,Lister, Andrew,Lucas, Simon,Moore, Jane,Moore, Esther,Patel, Anil,Pike, Kurt G.,Roberts, Bryan,Stark, Andrew,Stead, Darren,Thakur, Kumar,Turner, Paul,Vasbinder, Melissa,Yang, Bin
, p. 4718 - 4722 (2016)
As part of a medicinal chemistry program, we adapted known synthetic methods for the late-stage diversification of 2,4-substituted 7-azaindoles. The strengths and weaknesses of these strategies are discussed. In the course of this work, three optimized co
Pyrimidine derivative, and preparation method and application thereof
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Paragraph 0108-0111, (2021/06/12)
The invention discloses a compound represented by general formula (I) capable of being used as an ATR protein kinase inhibitor, and an isomer or pharmaceutically acceptable salt thereof. The compound, and the isomer or the pharmaceutically acceptable salt thereof can be used for preparing medicines for treating and/or preventing hyperproliferative diseases.
CDK9 Kinase inhibitors
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Paragraph 0234-0236; 0240, (2021/11/21)
The present application relates to CDK9 kinase inhibitors which provide a compound of formula (I) or a stereoisomer thereof. A solvate, a metabolite, a pharmaceutically acceptable salt or prodrug, and a pharmaceutical composition comprising the same. Also provided are the use of compounds and pharmaceutical compositions in the manufacture of a medicament for the treatment of cancer.
Development of Potent PfCLK3 Inhibitors Based on TCMDC-135051 as a New Class of Antimalarials
Mahindra, Amit,Janha, Omar,Mapesa, Kopano,Sanchez-Azqueta, Ana,Alam, Mahmood M.,Amambua-Ngwa, Alfred,Nwakanma, Davis C.,Tobin, Andrew B.,Jamieson, Andrew G.
supporting information, p. 9300 - 9315 (2020/10/19)
The protein kinase PfCLK3 plays a critical role in the regulation of malarial parasite RNA splicing and is essential for the survival of blood stage Plasmodium falciparum. We recently validated PfCLK3 as a drug target in malaria that offers prophylactic,
Synthesis of Differentially Protected Azatryptophan Analogs via Pd2(dba)3/XPhos Catalyzed Negishi Coupling of N-Ts Azaindole Halides with Zinc Derivative from Fmoc-Protected tert-Butyl (R)-2-Amino-3-iodopropanoate
Nimje, Roshan Y.,Vytla, Devaiah,Kuppusamy, Prakasam,Velayuthaperumal, Rajeswari,Jarugu, Lokesh Babu,Reddy, China Anki,Chikkananjaiah, Nanjundaswamy Kanikahalli,Rampulla, Richard A.,Cavallaro, Cullen L.,Li, Jianqing,Mathur, Arvind,Gupta, Anuradha,Roy, Amrita
, p. 11519 - 11530 (2020/10/12)
Unnatural amino acids play an important role in peptide based drug discovery. Herein, we report a class of differentially protected azatryptophan derivatives synthesized from N-tosyl-3-haloazaindoles 1 and Fmoc-protected tert-butyl iodoalanine 2 via a Neg
TYROSINE AMIDE DERIVATIVES AS RHO- KINASE INHIBITORS
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Page/Page column 70, (2020/02/14)
The invention relates to compounds of formula I inhibiting Rho Kinase that are bicyclic dihydropyrimidine-carboxamide derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
ATR INHIBITOR AND APPLICATION THEREOF
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Paragraph 0105; 0106, (2020/12/29)
Disclosed are a compound as an ATR inhibitor and an application in preparing a drug as an ATR inhibitor. In particular, disclosed is a compound represented by formula (I) or an isomer or pharmaceutically acceptable salt thereof.
TYROSINE ANALOGUES DERIVATIVES AS RHO- KINASE INHIBITORS
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Page/Page column 70, (2019/04/09)
The invention relates to compounds of formula (I) inhibiting Rho Kinase that are tyrosine analogues derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
Development and Scale-up of a Route to ATR Inhibitor AZD6738
Goundry, William R. F.,Dai, Kuangchu,Gonzalez, Miguel,Legg, Daniel,O'Kearney-Mcmullan, Anne,Morrison, James,Stark, Andrew,Siedlecki, Paul,Tomlin, Paula,Yang, Jianbo
, p. 1333 - 1342 (2019/08/12)
AZD6738 is currently being tested in multiple phase I/II trials for the treatment of cancer. Its structure, comprising a pyrimidine core decorated with a chiral morpholine, a cyclopropyl sulfoximine, and an azaindole, make it a challenging molecule to syn
DIHYDROISOQUINOLINE-2(1H)-CARBOXAMIDE AND RELATED COMPOUNDS AND THEIR USE IN TREATING MEDICAL CONDITIONS
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Paragraph 000551, (2019/11/04)
The invention provides dihydroisoquinoline-2(1H)-carboxamide and related compounds, pharmaceutical compositions, and their use in the treatment of medical conditions, such as cancer, and in inhibiting HPK1 activity.
