19689-86-2Relevant articles and documents
ALLOSTERIC ACTIVATORS OF THE ALPHA1A -ADRENERGIC RECEPTOR
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Page/Page column 34; 46-47, (2020/11/04)
The present invention relates to compounds that are activators of the Alpha1A-Adrenergic Receptor (α1A-AR) and methods of using such compounds: for treating neurological conditions, for cardio-protection, and for treating other condi
Highly Enantioselective Synthesis of Indazoles with a C3-Quaternary Chiral Center Using CuH Catalysis
Ye, Yuxuan,Kevlishvili, Ilia,Feng, Sheng,Liu, Peng,Buchwald, Stephen L.
supporting information, p. 10550 - 10556 (2020/07/27)
C3-substituted 1H-indazoles are useful and important substructures in many pharmaceuticals. Methods for direct C3-functionalization of indazoles are relatively rare, compared to reactions developed for the more nucleophilic N1 and N2 positions. Herein, we report a highly C3-selective allylation reaction of 1H-N-(benzoyloxy)indazoles using CuH catalysis. A variety of C3-allyl 1H-indazoles with quaternary stereocenters were efficiently prepared with high levels of enantioselectivity. Density functional theory (DFT) calculations were performed to explain the reactivity differences between indazole and indole electrophiles, the latter of which was used in our previously reported method. The calculations suggest that the indazole allylation reaction proceeds through an enantioselectivity-determining six-membered Zimmerman-Traxler-type transition state, rather than an oxidative addition/reductive elimination sequence, as we proposed in the case of indole alkylation. The enantioselectivity of the reaction is governed by both ligand-substrate steric interactions and steric repulsions involving the pseudoaxial substituent in the six-membered allylation transition state.
NOVEL FUNGICIDAL CARBAMATE COMPOUNDS
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Page/Page column 54, (2018/08/20)
An object of the present invention is to provide a carbamate compound or a salt thereof that controls diseases. The present invention provides a carbamate compound represented by Formula (1), or a salt thereof, wherein R1, R3 and R6 are identical or different and each represents hydrogen, or the like; R2 represents hydrogen, halogen, or C1-6 alkyl; R4 and R5 are identical or different and each represents hydrogen, or the like; R7 represents hydrogen, or the like; R8 represents hydrogen, or C1-6 alkyl; X and Χ1 independently represent oxygen, or sulfur; Y represents oxygen, or sulfur; Z represents oxygen/ or sulfur; l is an integer of 0 to 2; m is an integer of 0 to 3; n is an integer of 0 to 4; and when l, m or n is more than one, the l, m or n may be the same or different.
Photoactivatable BODIPYs Designed to Monitor the Dynamics of Supramolecular Nanocarriers
Zhang, Yang,Swaminathan, Subramani,Tang, Sicheng,Garcia-Amorós, Jaume,Boulina, Marcia,Captain, Burjor,Baker, James D.,Raymo, Francìisco M.
, p. 4709 - 4719 (2015/04/27)
Self-assembling nanoparticles of amphiphilic polymers can transport hydrophobic molecules across hydrophilic media and, as a result, can be valuable delivery vehicles for a diversity of biomedical applications. Strategies to monitor their dynamics noninva
2-OXO-2- (2-PHENYL-5,6,7,8-TETRAHYDRO-INDOLIZIN-3-YL) -ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ANTIFUNGAL AGENTS
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Page/Page column 23, (2011/02/15)
The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof: wherein: R1, R2, R3, R4, R5, R6, R7, R8, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
PYRROLE ANTIFUNGAL AGENTS
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Page/Page column 133, (2009/12/05)
The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof; wherein: R1, R2, R3, R4, R5, R6, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors
Rzasa, Robert M.,Kaller, Matthew R.,Liu, Gang,Magal, Ella,Nguyen, Thomas T.,Osslund, Timothy D.,Powers, David,Santora, Vincent J.,Viswanadhan, Vellarkad N.,Wang, Hui-Ling,Xiong, Xiaoling,Zhong, Wenge,Norman, Mark H.
, p. 6574 - 6595 (2008/03/27)
Cyclin-dependent kinase 5 (CDK5) is a serine/threonine kinase that plays a critical role in the early development of the nervous system. Deregulation of CDK5 is believed to contribute to the abnormal phosphorylation of various cellular substrates associated with neurodegenerative disorders such as Alzheimer's disease, amyotrophic lateral sclerosis, and ischemic stroke. Acyclic urea 3 was identified as a potent CDK5 inhibitor and co-crystallographic data of urea 3/CDK2 enzyme were used to design a novel series of 3,4-dihydroquinazolin-2(1H)-ones as CDK5 inhibitors. In this investigation we present our synthetic studies toward this series of compounds and discuss their biological relevance as CDK5 inhibitors.
Non-nucleoside reverse transcriptase inhibitors
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Page 11, (2010/02/07)
Compounds represented by formula I: wherein R1 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, and haloalkyl; R2 is H or (C1-4)alkyl; R3 is H or (C1-4)alkyl; R4 is (C1-4)alkyl, (C1-4)alkyl(C3-7)cycloalkyl, or (C3-7)cycloalkyl; and Q is a fused phenyl-5 or 6-membered saturated heterocycle having one to two heteroatoms selected from O and N, said Q being optionally substituted with hydroxy, or (C1-4)alkyl which in turn maybe optionally substituted with pyridinyl-N-oxide or C(O)OR wherein R is H or (C1-4)alkyl; or a salt thereof. The compounds have inhibitory activity against Wild Type, and single and double mutants strains, of HIV.
Oxime O-ether compounds and fungicides for agricultural and horticultural use
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, (2008/06/13)
The present invention relates to novel oxime O-ether compounds represented by a general formula [I]; wherein R1represents C1-6alkyl, C3-6cycloalkyl, C1-6alkoxy, etc., m represents an integer of 1 to 4, R2/
2-oxo-1,3,4-trihydroquinazolinyl derivatives and methods of use
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Page 26, (2010/02/05)
Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.