56515-89-0Relevant academic research and scientific papers
OXIME COMPOUNDS AS AGONISTS OF THE MUSCARINIC M1 AND/OR M4 RECEPTOR
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Page/Page column 38, (2017/05/20)
This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic Μ1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula (I) where p; q; X1; X2; Y; R1; R2; R3; R4; R5 and R6 are as defined herein.
SUBSTITUTED AZEPINE- AND DIAZEPINE-SULFONAMIDES USEFUL TO INHIBIT 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE-1
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Page/Page column 56-57, (2009/04/25)
In its many embodiments, the present invention relates to a novel class of substituted azepine- and diazepine-sulfonamide compounds useful to inhibit 11BETA-hydroxysteroid dehydrogenase type-1, pharmaceutical compositions containing the compounds, and met
The discovery of azepane sulfonamides as potent 11β-HSD1 inhibitors
Neelamkavil, Santhosh F.,Boyle, Craig D.,Chackalamannil, Samuel,Greenlee, William J.,Zhang, Lili,Terracina, Giuseppe
scheme or table, p. 4563 - 4565 (2010/04/05)
Discovery of a series of azepine sulfonamides as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is described. SAR studies at the 4-position of the azepane ring have resulted in the discovery of a very potent compound 30 which has
PYRIMIDINONE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 190-191, (2008/12/08)
The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of G protein-coupled receptor 119 ("GPR119") in a patient.
Design, Synthesis, and Evaluation of Metabolism-Based Analogues of Haloperidol Incapable of Forming MPP+-like Species
Lyles-Eggleston,Altundas,Xia,Sikazwe,Fan,Yang,Li,Zhang,Zhu,Schmidt,Vanase-Frawley,Shrihkande,Villalobos,Borne,Ablordeppey
, p. 497 - 508 (2007/10/03)
The long-term, irreversible, Parkinsonism-like side effects of haloperidol have been speculated to involve several mechanisms. More recently, it has been speculated that the metabolic transformation to MPP+-like species may contribute to the Parkinsonism-like side effects. Because BCPP+ and its reduced analogue have been shown to possess the potential to destroy dopamine receptors in the nigrostriatum, we have designed new analogues of haloperidol lacking the structural features necessary to form neurotoxic quaternary species but retaining their dopamine-binding capacity. The most potent agent at the D2 receptor, the homopiperidine analogue 11, was found to be equipotent to haloperidol. It was also of interest to identify analogues with DA binding profiles similar to that of clozapine at the dopamine receptor subtypes. Evaluation of the proposed agents shows that the ratio of D2 to D4 (2) binding of clozapine was mimicked by 7 [Ki(D2) = 33, Ki(D3) = 200, Ki(D4) = 11 nM; Ki(D2)/Ki(D4) = 3] and 9 [Ki(D2) = 44, Ki(D3) = 170, Ki(D4) = 24 nM; Ki(D2)/Ki(D4) = 2]. A preliminary in-vivo testing of compound 7 shows that its behavioral profile is similar to that of clozapine. This profile suggests that there is a need for further evaluation of these two synthetic agents and their enantiomers for efficacy and lack of catalepsy in animal models.
4-Anilidopiperidine Analgesics. 3. 1-Substituted 4-(Propananilido)perhydroazepines as Ring-Expanded Analogues
Finney, Z. Gail,Riley, Thomas N.
, p. 895 - 899 (2007/10/02)
A study of ring-expanded analogues of the 4-(propananilido)piperidine analgesics has been undertaken in order to evaluate the influence of this structural modification on both analgesic activity and physical-dependence capacity.Thus, a series of 1-substit
