133077-42-6Relevant articles and documents
Design, synthesis and biological evaluation of pyridyl substituted benzoxazepinones as potent and selective inhibitors of aldosterone synthase
Zhu, Haichao,Liu, Meihua,Li, Haiyan,Guan, Ting,Zhang, Qi,Chen, Yang,Liu, Yingxiang,Hartmann, Rolf R.,Yin, Lina,Hu, Qingzhong
supporting information, p. 2327 - 2332 (2021/04/12)
Exorbitant aldosterone is closely associated with various severe diseases, including congestive heart failure and chronic kidney disease. As aldosterone synthase is the pivotal enzyme in aldosterone biosynthesis, its inhibition constitutes a promising tre
Facile access to chiral 4-substituted chromanes through Rh-catalyzed asymmetric hydrogenation
Tao, Lin,Zhao, Qingyang,Zhang, Xumu,Dong, Xiu-Qin
supporting information, p. 1859 - 1862 (2020/01/21)
Rh/ZhaoPhos-catalyzed asymmetric hydrogenation of a series of (E)-2-(chroman-4-ylidene)acetates was successfully developed to prepare various chiral 4-substituted chromanes with high yields and excellent enantioselectivities (up to 99percent yield, 98percent ee). Moreover, the gram-scale hydrogenation could be performed well in the presence of 0.02 molpercent catalyst loading (TON = 5000), the hydrogenation product was easily converted to access other important compounds, which demonstrated the synthetic utility of this asymmetric catalytic methodology.
Steroid synthase inhibitors and therapeutic application thereof
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Paragraph 0066-0068, (2020/12/31)
The invention discloses a steroid synthase inhibitor and treatment application thereof, and belongs to the field of medicines. The compound capable of being used as the medicine has the effect of inhibiting steroid synthase, is high in inhibition rate and
Exploiting the Chromone Scaffold for the Development of Inhibitors of Corticosteroid Biosynthesis
Gobbi, Silvia,Hu, Qingzhong,Zimmer, Christina,Engel, Matthias,Belluti, Federica,Rampa, Angela,Hartmann, Rolf W.,Bisi, Alessandra
, p. 2468 - 2477 (2016/04/10)
The inhibition of corticosteroid biosynthesis could be considered as an emerging strategy to reduce their abnormally high levels, and in this framework CYP11B1 and CYP11B2 represent the most promising targets. In continuing our studies on flavonoid-like scaffolds as privileged structures in medicinal chemistry, in this paper we describe a small library of pyridyl- and imidazolylmethylchromones as potential inhibitors of these enzymes. Testing results proved that position 3 of the chromone scaffold is the most favorable for the introduction of the heme-coordinating heterocycles and, among them, the 4-imidazolyl moiety is the most convenient for the interaction with the heme iron of the selected cytochromes. A low nanomolar inhibitor of CYP11B1 (5c) was obtained, endowed with reasonable selectivity toward CYP11B2 and able to better discriminate with respect to CYP17 and CYP19.
Synthesis, enantiomeric separation and docking studies of spiropiperidine analogues as ligands of the nociceptin/orphanin FQ receptor
Battisti, Umberto M.,Corrado, Sandra,Sorbi, Claudia,Cornia, Andrea,Tait, Annalisa,Malfacini, Davide,Cerlesi, Maria Camilla,Calò, Girolamo,Brasili, Livio
supporting information, p. 973 - 983 (2014/07/08)
A series of triazospirodecanone derivatives were synthesized as potential NOP ligands. 8-(Chroman-4-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (4) and its 5-fluoro analogue (18) proved to be active as agonists with EC50 values in the submicromolar range. Single enantiomers of compound 4 were separated and tested as NOP agonists; the eutomer R-(+)-4 showed a pEC 50 of 7.34. Finally docking studies were performed on the NOP receptor to identify the most significant stereospecific interactions.
PHARMACEUTICALLY ACTIVE 6-N-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES
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Page/Page column 62, (2009/01/24)
The invention provides compounds of the formula (0), in which the substituents and symbols are as defined in the description. The compounds inhibit the secretion of gastric acid.
CHROMAN DERIVATIVES AND THEIR USE AS 5-HT RECEPTOR LIGANDS
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Page/Page column 30, (2008/06/13)
Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1, R2, R3 and R4 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula (I).
CHROMAN DERIVATIVES AND USES THEREOF IN THE TREATMENT OF CNS DISORDERS
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Page/Page column 24, (2008/06/13)
Compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1, R2, R3 and R4 are as defined herein. Also provided are methods for preparing, compositions comprising, and met
BICYCLIC SUBSTITUTED INDOLE-DERIVATIVE STEROID HORMONE NUCLEAR RECEPTOR MODULATORS
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Page/Page column 55, (2010/02/14)
The present invention provides a compound of the formula: Formula (I); or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient, and methods for treating physiological disorders, particularly congestive heart disease, hypertension, and atherosclerosis, comprising administering to a patient in thereof an effective amount of a compound of Formula I. X-16125
Quinoxaline compounds
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Page/Page column 30, (2008/06/13)
Certain amidophenyl-sulfonylamino-quinoxaline compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
