- 5,6-Membered CNN palladium pincer complexes of 3-benzyl-8-dimethylamino -3-azabicyclo[3.2.1]octane and 3-benzyl-9-dimethylamino-3-azabicyclo[3.3.1]nonane
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The unsymmetrical CNN pincer ligand precursors 4 and 7b based on the structures of bicyclo[3.2.l]octane and bicyclo[3.3.l]nonane have been synthesized. The corresponding palladium pincer 5,6-membered complexes 5 and 9 were prepared by direct cyclopalladat
- Bulygina, Ludmila A.,Khrushcheva, Natalya S.,Lyssenko, Konstantin A.,Peregudov, Aleksander S.
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- FXR RECEPTOR MODULATOR, PREPARATION METHOD THEREFOR, AND USES THEREOF
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The present disclosure disclosed a modulator of FXR receptor and preparation and use thereof, which relates to the technical filed of medicinal chemistry. The present disclosure provides a modulator of FXR receptor having a structural formula I or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, which can combine with FXR receptor (that is NR1H4) and be acted as a FXR agonist or a partial agonist for preventing and treating the disease mediated by FXR, such as chronic intrahepatic or extrahepatic cholestasis, hepatic fibrosis caused by chronic cholestasis or acute intrahepatic cholestasis, chronic hepatitis B, gallstone, hepatic carcinoma, colon cancer or intestinal inflammatory disease, etc. Specifically, for some chemical compounds, their EC50 for FXR agonist activity reach below 100nM, which show an excellent FXR agonist activity and an excellent prospect to provide a new pharmaceutical selection in clinical treatment for the disease mediated by FXR.
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Paragraph 0072; 0073
(2018/11/27)
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- INDAZOLE- AND PYRROLOPYRIDINE-DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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The present invention relates to a novel indazole- or pyrrolopyridine-derivative, represented by the formula (1) below, that has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same. Formula (1) [wherein each substituent is as defined in claim 1]
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Page/Page column 207; 208
(2013/02/27)
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- Histamine H3 Inverse Agonists and Antagonists and Methods of Use Thereof
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Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
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Page/Page column 64
(2011/04/18)
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- Muscarinic Receptor Antagonists
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Provided are muscarinic receptor antagonists, which can be useful in treating various diseases of the respiratory, urinary or gastrointestinal system mediated through muscarinic receptors. Also provided are processes for preparing compounds described herein, pharmaceutical compositions comprising compounds described herein, and methods for treating diseases mediated through muscarinic receptors.
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Page/Page column 18
(2009/01/23)
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- METHOD FOR PRODUCING PIPERIDIN-4-ONE-DERIVATIVE
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Provided is a method for producing a piperidin-4-one derivative useful as an intermediate for agricultural chemicals or pharmaceutical products. A piperidin-4-one derivative represented by formula (III-a) or formula (III-b) is produced by reacting a cycli
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Page/Page column 11
(2009/06/27)
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- CHEMICAL COMPOUNDS
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The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, m and n are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.
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Page/Page column 79
(2008/06/13)
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- MUSCARINIC RECEPTOR ANTAGONISTS
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This present invention generally relates to muscarinic receptor antagonists of Formula (I), which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the prepration of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.
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Page/Page column 29
(2008/06/13)
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- Azabicyclooctane derivatives useful in the treatment of cardiac arrhythmias
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There is provided compounds of formula (I), wherein R1, R2, R3 and Ra to Rh have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias, a process for the preparation of compounds of formula (I), and intermediate compounds.
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- Aza-tricyclic substance P antagonists
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The synthesis and structure-activity relationships of a series of aza- tricyclic analogs of the quinuclidine substance P (SP) antagonist 1 are described. The SP receptor affinity of these compounds was found to vary according to the size of the new ring fused to the quinuclidine and the mode of fusion. Correlations between receptor affinity and (1) the steric bulk of the newly introduced ring fusion and (2) the dihedral angle between the benzhydryl and benzylamino substituents of these aza-tricyclic compounds were explored.
- Lowe III,Drozda,McLean,Bryce,Crawford,Snider,Longo,Nagahisa,Tsuchiya
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p. 2831 - 2840
(2007/10/02)
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