5090-33-5Relevant academic research and scientific papers
TETRAHYDROISOQUINOLINE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
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, (2017/11/06)
Described herein are tetrahydroisoquinoline compounds with estrogen receptor modulation activity or function having the Formula I structure: I and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
Dynamic kinetic resolution of 2-phenylpropanal derivatives to yield β-chiral primary amines via bioamination
Fuchs, Christine S.,Hollauf, Manuel,Meissner, Maximilian,Simon, Robert C.,Besset, Tatiana,Reek, Joost N. H.,Riethorst, Waander,Zepeck, Ferdinand,Kroutil, Wolfgang
, p. 2257 - 2265 (2014/07/21)
The amination of racemic α-chiral aldehydes, 2-phenylpropanal derivatives, was investigated employing ω-transaminases. By medium and substrate engineering the optical purity of the resulting β-chiral chiral amine could be enhanced to reach optical purities up to 99% ee. Using enantiocomplementary ω-transaminases allowed us to access the (R)- as well as the (S)-enantiomer in most cases. It is important to note that the stereopreference of the ω-transaminases found for α-chiral aldehydes did not correlate with the stereopreference previously observed for the amination of methyl ketones. In one case the stereopreference switched even upon exchanging a methyl substituent to a methoxy group.
MODULATORS OF THE HISTAMINE H3 RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
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Page/Page column 90-91, (2009/10/18)
Amide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as excessive daytime sleepiness, narcolepsy, shift-work sleep disorder, drowsiness as a side effect from a medication, maintenance of vigilance to aid in the completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease, pain and the like.
Tetrahydroisoquinoline LXR modulators
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Page/Page column 56, (2010/11/26)
A compound of formula I wherein X, R1, R2a, R3a, R3b, R4a, R4b, R4c and R5 are defined herein.
Synthesis of 6-Hydroxy-1,4-dimethylisoquinoline and of Ethyl 7-Hydroxy-6-methoxy-1-methylisoquinoline-3-carboxylate
Martinez, Silvio J.,Larsen, Lesley,Street, Janathan D.,Joule, John A.
, p. 1705 - 1710 (2007/10/02)
The syntheses of 6-methoxy- and 6-hydroxy-1,4-dimethylisoquinoline and of ethyl 7-hydroxy-6-methoxy-1-methylisoquinoline-3-carboxylate, key intermediates required for a synthetic approach to the antitumour antibiotic CC-1065, are described.
