36983-35-4Relevant academic research and scientific papers
7H-PYRROLO[2,3-D]PYRIMIDINE-4-AMINE DERIVATIVE
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Paragraph 0304, (2021/12/31)
The present invention provides a novel compound inhibiting EGFR or a salt of the compound. According to one embodiment of the present invention, provided is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.
ATF6 INHIBITORS AND USES THEREOF
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Paragraph 0290; 0287; 0304; 0302; 0336; 0334; 0342; 0340, (2019/10/29)
Compounds as inhibitors of Activating Transcription Factor 6 (ATF6) are provided. The compounds may find use as therapeutic agents for the treatment of diseases or disorders mediated by ATF6 and may find particular use in the treatment of viral infections, neurodegenerative diseases, vascular diseases, or cancer.
Regio-specific synthesis of new 1-(tert-butyl)-1H-pyrazolecarboxamide derivatives
Ruatta, Santiago Matías,Murguía, Marcelo César,Ramírez de Arellano, Carmen,Fustero, Santos
supporting information, p. 2441 - 2444 (2017/06/05)
Regio-specific and non-regiospecific condensation reactions on 1,3-dicarbonyl compounds rendered 1,3,5-trisubstituted pyrazoles. Herein, the control of regio-specificity was a significant improvement in pyrazole research. A high yield acylation of poorly
Diphenylpyrazoles as replication protein A inhibitors
Waterson, Alex G.,Kennedy, J. Phillip,Patrone, James D.,Pelz, Nicholas F.,Feldkamp, Michael D.,Frank, Andreas O.,Vangamudi, Bhavatarini,Souza-Fagundes, Elaine M.,Rossanese, Olivia W.,Chazin, Walter J.,Fesik, Stephen W.
supporting information, p. 140 - 145 (2015/03/04)
Replication Protein A is the primary eukaryotic ssDNA binding protein that has a central role in initiating the cellular response to DNA damage. RPA recruits multiple proteins to sites of DNA damage via the N-terminal domain of the 70 kDa subunit (RPA70N). Here we describe the optimization of a diphenylpyrazole carboxylic acid series of inhibitors of these RPA-protein interactions. We evaluated substituents on the aromatic rings as well as the type and geometry of the linkers used to combine fragments, ultimately leading to submicromolar inhibitors of RPA70N protein-protein interactions.
Synthesis of fluorinated and nonfluorinated tebufenpyrad analogues for the study of anti-angiogenesis MOA
Roman, Raquel,Navarro, Antonio,Wodka, Dariusz,Alvim-Gaston, Maria,Husain, Saba,Franklin, Natalie,Simon-Fuentes, Antonio,Fustero, Santos
, p. 1027 - 1036 (2014/10/15)
In this contribution we report the synthesis of fluorinated and nonfluorinated tebufenpyrad analogues to explore potential druglike properties through the phenotypic screening as part of the Lilly Open Innovation Drug Discovery (OIDD) program.
Synthesis and insecticidal activities of novel anthranilic diamides containing modified N-pyridylpyrazoles
Feng, Qi,Liu, Zhi-Li,Xiong, Li-Xia,Wang, Ming-Zhong,Li, Yong-Qiang,Li, Zheng-Ming
experimental part, p. 12327 - 12336 (2011/09/14)
In order to look for novel insecticides targeting the ryanodine receptor, four new series of anthranilic diamides containing modified N-pyridylpyrazoles were designed and synthesized. All of the compounds were characterized and confirmed by 1H NMR, 13C NMR, and HRMS. The single crystal structure of 10c was determined by X-ray diffraction. Their insecticidal activities against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella) indicated that most of the compounds showed moderate to high activities at the tested concentration, while compound 19 showed comparable higher activity at the concentration of 0.125 mg/L. The preliminary structure-activity relationship (SAR) was discussed.
Novel 6-N-arylcarboxamidopyrazolo[4,3-d]pyrimidin-7-one derivatives as potential anti-cancer agents
Devegowda, Vani N.,Kim, Jung Hyun,Han, Ki-Cheol,Yang, Eun Gyeong,Choo, Hyunah,Pae, Ae Nim,Nam, Ghilsoo,Choi, Kyung Il
scheme or table, p. 1630 - 1633 (2010/06/19)
A novel series of 3,5,6-trisubstituted pyrazolo[4,3-d]pyrimidin-7-one derivatives, especially 6-N-arylcarboxamidopyrazolo[4,3-d]pyrimidin-7-ones were synthesized and evaluated for their in vitro anticancer activities against various human cancer cell line
NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS
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Page/Page column 104, (2009/10/01)
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
PHARMACEUTICAL COMPOSITION FOR PREVENTINTION AND TREATMENT OF RESTENOSIS COMPRISING ISOXAZOLE DERIVATIVES
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Page/Page column 17-18, (2009/03/07)
There is provided a pharmaceutical composition for prevention and treatment of restenosis comprising isoxazole derivatives. The pharmaceutical composition includes a therapeutic effective amount of isoxazole derivatives represented by Formula 1 or pharmaceutically available salts thereof. The pharmaceutical composition may be useful to prevent and treat vascular restenosis since the pharmaceutical composition shows an anti-restenosis activity and accelerates the re-endothelization.
ISOXAZOLE DERIVATIVES AND USE THEREOF
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Page/Page column 12, (2009/05/28)
Disclosed herein are isoxazole derivatives and uses thereof. Serving as agonists of Wnt, the isoxazole derivatives activate Wnt/beta-catenin signaling and thus can be used in the treatment and prevention of diseases related to the signal transduction. Also, pharmaceutically acceptable salts of the isoxazole derivatives are disclosed
