1219020-59-3Relevant articles and documents
Efficient synthesis of cyclopropylhydrazine salts
Shibue, Taku,Fukuda, Yasumichi
, p. 4102 - 4104 (2014)
An efficient procedure for the synthesis of cyclopropylhydrazine in the form of its salts is reported. The copper salt-catalyzed addition of cyclopropylboronic acid to the azo group of di-tert-butyl azodicarboxylate and subsequent deprotection gave the cy
Homologation of the Fischer Indolization: A Quinoline Synthesis via Homo-Diaza-Cope Rearrangement
De, Chandra Kanta,Gerosa, Gabriela Guillermina,List, Benjamin,Maji, Rajat,Schwengers, Sebastian Armin
, p. 20485 - 20488 (2020)
We disclose a new Br?nsted acid promoted quinoline synthesis, proceeding via homo-diaza-Cope rearrangement of N-aryl-N′-cyclopropyl hydrazines. Our strategy can be considered a homologation of Fischer's classical indole synthesis and delivers 6-membered N-heterocycles, including previously inaccessible pyridine derivatives. This approach can also be used as a pyridannulation methodology toward constructing polycyclic polyheteroaromatics. A computational analysis has been employed to probe plausible activation modes and to interrogate the role of the catalyst.
BI-ARYL DIHYDROOROTATE DEHYDROGENASE INHIBITORS
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Page/Page column 200; 355-356, (2021/04/17)
Disclosed are compounds, compositions and methods for treating diseases, disorders, or medical conditions that are affected by the modulation of DHODH. Such compounds are represented by Formula I as follows: Formula I wherein R1, R2, R3, and Q are defined herein.
CDPK1 INHIBITORS, COMPOSITIONS, AND METHODS RELATED THERETO
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Paragraph 0204-0206, (2021/11/13)
The invention relates to inhibitors of calcium-dependent protein kinase 1 (CDPK1) and pharmaceutical preparations thereof. The invention further relates to methods of treatment of parasitic infections, such as T. gondii, P. falciparum, C. hominis, or C. parvum infections, using the novel inhibitors of the invention.
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
Decarboxylative hydrazination of unactivated carboxylic acids by cerium photocatalysis
Yatham, Veera Reddy,Bellotti, Peter,K?nig, Burkhard
supporting information, p. 3489 - 3492 (2019/03/26)
We report the cerium photocatalyzed radical decarboxylative hydrazination of carboxylic acids with di-tert-butylazodicarboxylate (DBAD). The operationally simple protocol provides rapid access to synthetically useful hydrazine derivatives and overcomes current scope limitations in the photoredox-catalyzed decarboxylation of carboxylic acids.
CDPK1 INHIBITORS, COMPOSITIONS, AND METHODS RELATED THERETO
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Page/Page column 42-43, (2019/03/05)
The invention relates to inhibitors of calcium-dependent protein kinase 1 (CDPK1 and pharmaceutical preparations thereof. The invention further relates to methods of treatment of parasitic infections, such as T. gondii, P. falciparum, C. hominis, or C. parvum infections, using the novel inhibitors of the invention.
CDPK1 INHIBITORS, COMPOSITIONS AND METHODS RELATED THERETO
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Page/Page column 28; 35, (2018/10/19)
The invention relates to inhibitors of calcium-dependent protein kinase 1 (CDPKl) and pharmaceutical preparations thereof. The invention further relates to methods of treatment of parasitic infections, such as T. gondii, T. cruzi, P. falciparum, T. brucei, or L. major infections, using the novel inhibitors of the invention.
1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-ones as PDE1 Inhibitors
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Paragraph 0206; 0207, (2017/10/30)
The present invention provides 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-ones of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
SPIROCYCLIC COMPOUNDS
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Paragraph 0320, (2017/07/31)
Disclosed herein are spirocyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.