- SUBSTITUTED ARYL COMPOUND AND PREPARATION METHOD THEREFOR AND USE THEREOF
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The present application relates to a substituted aryl compound or a pharmaceutically acceptable salt, a stereoisomer, a polymorph, a solvate, a N-oxide, an isotope-labeled compound, a metabolite or a prodrug thereof, and a preparation method therefor and use thereof, also relates to a pharmaceutical composition containing the compound and a therapeutic use thereof. The compound or a pharmaceutical composition thereof can inhibit the activity of adenosine A2a receptor, and can be used for treating or preventing a disease related to adenosine A2a receptor, especially for treating a tumor.
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Paragraph 0204; 0206
(2021/11/04)
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- CYCLIC AMINE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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A compound exerts a strong analgesic effect against pain, in particular, neuropathic pain and/or fibromyalgia syndrome. The cyclic amine derivative is represented by formula, a prodrug thereof or a pharmacologically acceptable salt thereof: wherein A represents a group represented by Formula (IIa), (IIb) or (IIc): wherein R3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, R4 represents a hydrogen atom or an alkylcarbonyl group having 2 to 6 carbon atoms or an alkyl group having 1 to 6 carbon atoms and optionally substituted with an alkylcarbonylamino group having 2 to 6 carbon atoms and n represents 1 or 2, in which when R3 and R4 each independently represent an alkyl group having 1 to 6 carbon atoms, R1 represents an alkyl group having 1 to 6 carbon atoms and substituted with a hydroxyl group, an amino group or a carboxyl group.
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- Cyclic amine derivative and pharmaceutical use thereof
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The purpose of the present invention is to provide a compound that exerts a strong analgesic action against on pain, in particular, against neuropathic pain and/or fibromyalgia syndrome. The present invention provides a cyclic amine derivative represented by chemical formula, a prodrug thereof or a pharmaceutically acceptable salt thereof.
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Paragraph 0317
(2016/10/09)
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- Design and synthesis of a hybrid series of potent and selective agonists of α7 nicotinic acetylcholine receptor
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α7 nicotinic acetylcholine receptor agonists are promising therapeutic candidates for the treatment of cognitive impairment. As a follow up of our internal medicinal chemistry program we investigated a novel series of α7 nAChR agonists. Starting from molecular docking studies on two series of molecules recently developed in our laboratories, an alternative scaffold was designed attempting to combine the optimal features of these previously identified urea and pyrazole compounds. Based on our previous SAR knowledge and on predicted drug-like properties, a small library was synthesized in parallel manner, affording compounds with excellent α7 nAChR activity, selectivity and preliminary ADME profile.
- Nencini, Arianna,Castaldo, Cristiana,Comery, Thomas A.,Dunlop, John,Genesio, Eva,Ghiron, Chiara,Haydar, Simon,Maccari, Laura,Micco, Iolanda,Turlizzi, Elisa,Zanaletti, Riccardo,Zhang, Jean
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p. 401 - 418
(2014/04/17)
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- Improved, selective, human intestinal carboxylesterase inhibitors designed to modulate 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (irinotecan; CPT-11) toxicity
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CPT-11 is an antitumor prodrug that is hydrolyzed by carboxylesterases (CE) to yield SN-38, a potent topoisomerase I poison. However, the dose limiting toxicity delays diarrhea that is thought to arise, in part, from activation of the prodrug by a human i
- Hicks, Latorya D.,Hyatt, Janice L.,Stoddard, Shana,Tsurkan, Lyudmila,Edwards, Carol C.,Wadkins, Randy M.,Potter, Philip M.
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scheme or table
p. 3742 - 3752
(2010/04/05)
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- Benzothiazole derivatives with activity as adenosine receptor ligands
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The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.
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