- Amide compound and derivative thereof, preparation method, pharmaceutical composition and application thereof
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The invention discloses an amide compound and derivative thereof, a preparation method, a pharmaceutical composition and application thereof. The structure of the amide compound is shown as a formula (I). The derivatives of theamide compound relate to a stereoisomer, a tautomer, a metabolite, a metabolic precursor, a prodrug, a solvate, a salt of the solvate, a crystal, a pharmaceutically acceptable salt or a mixture of the above of theamide compound. The amide compound and the derivative thereof have an efficient inhibition effect on indoleamine 2, 3-dioxygenase 1, and can be used for preparing medicines for treating indoleamine 2, 3-dioxygenase 1 mediated immunosuppression related diseases, the prepared medicine can exert the medicine effect at the molecular level and is wide in application, and the synthesis method of the compound is simple, convenient and easy to operate.
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Paragraph 0304-0307
(2021/07/09)
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- CHEMOSELECTIVE METHYLENE HYDROXYLATION IN AROMATIC MOLECULES
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A chemoselective and reactive Mn(CF3-PDP) catalyst system that enables for the first time the strategic advantages of late-stage aliphatic C—H hydroxylation to be leveraged in aromatic compounds. This discovery will benefit small molecule therapeutics by enabling the rapid diversification of aromatic drugs and natural products and identification of their metabolites.
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Paragraph 0129; 0176; 0183-0184
(2020/03/28)
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- INHIBITOR OF INDOLEAMINE-2,3-DIOXYGENASE (IDO)
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The present disclosure provides compounds of Formula (I). The compounds described herein may be useful in treating a disease associated with IDO, for example, cancer or an infectious disease (e.g., viral or bacterial infectious diseases). Also, provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
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Paragraph 00201-00202
(2017/09/05)
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- Synthesis and pharmacological evaluation of 1-Alkyl-N-[(1R)-1-(4- fluorophenyl)-2-methylpropyl]piperidine-4-carboxamide derivatives as novel antihypertensive agents
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We synthesized and evaluated inhibitory activity against T-type Ca 2+ channels for a series of 1-alkyl-N- [(1R)-1-(4-fluorophenyl)-2- methylpropyl]piperidine-4-carboxamide derivatives. Structure-activity relationship studies have revealed that the isopropyl substituent at the benzylic position plays an important role in exerting potent inhibitory activity, and the absolute configuration of the benzylic position was found to be opposite that of mibefradil, which was first launched as a new class of T-type Ca2+ channel blocker. Oral administration of N- [(1R)-1-(4-fluorophenyl)-2-methylpropyl]-1-[2-(3-methoxyphenyl)ethyl] piperidine-4-carboxamide (17f) lowered blood pressure in spontaneously hypertensive rats without inducing reflex tachycardia, an adverse effect often caused by traditional L-type Ca2+ channel blockers.
- Watanuki, Susumu,Matsuura, Keisuke,Tomura, Yuichi,Okada, Minoru,Okazaki, Toshio,Ohta, Mitsuaki,Tsukamoto, Shin-Ichi
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experimental part
p. 1376 - 1385
(2012/01/05)
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- Synthesis and pharmacological evaluation of 1-alkyl-N-[2-ethyl-2-(4- fluorophenyl)butyl]piperidine-4-carboxamide derivatives as novel antihypertensive agents
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We synthesized and evaluated inhibitory activity against T-type Ca 2+ channels for a series of 1-alkyl-N-[2-ethyl-2-(4-fluorophenyl) butyl]piperidine-4-carboxamide derivatives. Structure-activity relationship studies have revealed that dialkyl substituents at the benzylic position play an important role in increasing inhibitory activity. Oral administration of N-[2-ethyl-2-(4-fluorophenyl)butyl]-1-(2-phenylethyl)piperidine-4-carboxamide (20d) lowered blood pressure in spontaneously hypertensive rats without inducing reflex tachycardia, which is often caused by traditional L-type Ca2+ channel blockers.
- Watanuki, Susumu,Matsuura, Keisuke,Tomura, Yuichi,Okada, Minoru,Okazaki, Toshio,Ohta, Mitsuaki,Tsukamoto, Shin-Ichi
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experimental part
p. 5628 - 5638
(2011/10/12)
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