87306-82-9Relevant academic research and scientific papers
THERAPEUTIC COMPOUNDS
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, (2018/08/30)
The invention provides compounds of formula Ia′, Ib′, Ic′, and Id′: and pharmaceutically acceptable salts thereof, wherein the variables A, R6, R7, R8, R9, Rx, L, X, Y, and Z have the meaning as described herein. The compounds are useful for reducing endoplasmic reticulum stress and for producing analgesia in an animal.
Optimisation of imidazole compounds as selective TAAR1 agonists: Discovery of RO5073012
Galley, Guido,Stalder, Henri,Goergler, Annick,Hoener, Marius C.,Norcross, Roger D.
, p. 5244 - 5248 (2012/09/07)
A series of imidazole compounds has been identified which affords potent and selective partial and full agonists of the TAAR1 receptor. Starting from 2-benzyl-imidazoline screening hits, a series of structurally related 2-benzyl- and 4-benzyl-imidazoles was investigated first, but it proved highly challenging to obtain compounds having sufficient selectivity against the adrenergic alpha 2 receptor. This issue could be successfully addressed by modification of the linker region and SAR exploration led to the discovery of highly selective isopropyl-substituted 4-aminomethyl-imidazole compounds. The work culminated in the identification of the selective TAAR1 partial agonist RO5073012 (4-chlorophenyl)-(1H-imidazol-4-ylmethyl)-isopropyl-amine, 24), which has a good pharmacokinetic profile after oral administration in rodents. RO5073012 has been found to be active in a behavioural rat model which is considered indicative for schizophrenia.
Method for the treatment of CNS disorders with substituted 2-imidazoles or imidazole derivatives
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Page/Page column 14, (2010/11/28)
The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.
PYRROLOY2,3-c¨PYRIDINE COMPOUND, PROCESS FOR PRODUCING THE SAME, AND USE
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Page/Page column 45, (2010/11/27)
Provision of a compound having a superior proton pump action, which shows an antiulcer activity and the like after conversion to an in vivo proton pump inhibitor, a production method thereof and use thereof. A pyrrolo[2,3-c]pyridine compound represented by the formula: wherein each symbol is as defined in the specification.
PALLADIUM-MEDIATED 2,6-DIALKYLATION OF N-BENZILIDINE IMINES: PREPARATION OF 2,6-DIALKYLBENZALDEHYDES
McCallum, J. Stuart,Gasdaska, John R.,Liebeskind, Lanny S.
, p. 4085 - 4088 (2007/10/02)
Treatment of di-μ-trifluoroacetatobisdipalladium with two equivalents of primary alkyl iodides and subsequent hydrolysis provides an efficient route to 2,6-disubstituted benzaldehydes.
Fused Indoles. Synthesis of β-Carbolines and Azerinoindoles from 3-(2-Alkylindol-3-yl)-2-azidoacrylates
Moody, Christopher J.,Ward, John G.
, p. 2895 - 2901 (2007/10/02)
Decomposition of the azidoacrylates (6) derived from 2-substituted indole-3-carbaldehydes gives pharmacologically important β-carbolines , azepinoindoles (13), or enamines (14) depending on the conditions.The formation of azepinoindoles, shown to proceed by cyclisation of the initially formed enamines, represents a new reaction of vinyl azides which is particularly favoured in the indole series.
Reductive Cleavage of Aryl Oxazolines to Benzaldehydes and Substituted Toluenes
Meyers, A. I.,Himmelsbach, Richard J.,Reuman, Michael
, p. 4053 - 4058 (2007/10/02)
Aryl oxazolines have been converted to their corresponding benzaldehydes and toluenes by several routes by passing through the intermediate amino alcohols.The transformations proceeded under mild conditions and were shown to be generally applicable to a variety of substitutions on the aromatic nucleus.
