- Discovery of phenylpyrrolidine derivatives as a novel class of retinol binding protein 4 (RBP4) reducers
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Retinol-binding protein 4 (RBP4) is a potential drug target for metabolic and ophthalmologic diseases. A high-throughput screening of our compound library has identified a small-molecule RBP4 reducer 7a, as a hit compound. Aiming to provide a suitable too
- Akao, Yuichiro,Cho, Nobuo,Furuyama, Naoki,Goto, Akihiko,Kamaura, Masahiro,Kasai, Shizuo,Mizukami, Atsushi,Nakamura, Natsuko,Nakamura, Shinji
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supporting information
(2021/12/30)
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- Tetrahydrochromenoimidazoles as potassium-competitive acid blockers (P-CABs): Structure-activity relationship of their antisecretory properties and their affinity toward the hERG channel
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Potassium-competitive acid blockers (P-CABs) constitute a new therapeutic option for the treatment of acid-related diseases that are widespread and constitute a significant economical burden. Enantiomerically pure tetrahydrochromenoimidazoles were prepared using the readily available candidate 4 (BYK 405879) as starting material or the Noyori asymmetric reduction of ketones as key reaction. A comprehensive SAR regarding the influence of the 5-carboxamide and the 8-aryl residue on in vitro activity, acid-suppression in the Ghosh Schild rat, and affinity toward the hERG channel was established. In addition, efficacy and duration of the antisecretory action was examined for the most promising target compounds by 24 h pH-metry in the fistula dog and a significantly different SAR was observed as compared to the Ghosh Schild rat. Several tetrahydrochromenoimidazoles were identified that possessed a comparable profile as the candidate 4.
- Palmer, Andreas M.,Chiesa, Vittoria,Schmid, Anja,Münch, Gabriela,Grobbel, Burkhard,Zimmermann, Peter J.,Brehm, Christof,Buhr, Wilm,Simon, Wolfgang-Alexander,Kromer, Wolfgang,Postius, Stefan,Volz, Jürgen,Hess, Dietmar
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supporting information; experimental part
p. 3645 - 3674
(2010/07/05)
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- Azetidine based transition state analogue inhibitors of N-ribosyl hydrolases and phosphorylases
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N-Ribosyl phosphorylases and hydrolases catalyze nucleophilic displacement reactions by migration of the cationic ribooxacarbenium carbon from the fixed purine to phosphate and water nucleophiles, respectively. As the lysis reaction progresses along the r
- Evans, Gary B.,Furneaux, Richard H.,Greatrex, Ben,Murkin, Andrew S.,Schramm, Vern L.,Tyler, Peter C.
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p. 948 - 956
(2008/09/19)
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- ENANTIOPURE PHARMACOLOGICALLY ACTIVE TRICYCLIC BENZIMIDAZOLES
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The invention provides compounds of the formula (1) in which the substituents and symbols are as de fined in the description. The compounds inhibit the secretion of gastric acid.
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Page/Page column 78-79
(2008/12/08)
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- Indolobenzazepine HCV NS5B inhibitors
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The invention encompasses compounds and salts of Formulas I, II, III, and IV as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 278
(2008/06/13)
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- CB1 MODULATOR COMPOUNDS
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Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith.
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Page/Page column 162-163
(2008/06/13)
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- Triazine derivative and medicine
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The invention relates to a medicinal composition comprising a triazine derivative of the following general formula ?I! STR1 or a solvate thereof, or a salt thereof, as an active ingredient. In the above formula, R1 and R2 may be the
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