- Synthesis of 1-Amino-2 H-quinolizin-2-one Scaffolds by Tandem Silver Catalysis
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An efficient tandem cycloisomerization-amination reaction catalyzed by silver is described. This rapid and atom-economic reaction delivered 1-amino-2H-quinolizin-2-one scaffolds in high yields under mild conditions. The reaction could be extended to an asymmetric version albeit with moderate enantioselective excess of the products. In addition, the products can be easily reduced into various azabicycles containing 4-pyridones, which are important building blocks in organic synthesis.
- Min, Xiao-Long,Sun, Chao,He, Ying
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- Multi-substituted amine compound and its preparation and use (by machine translation)
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The invention belongs to the field of medical technology, in particular, the present invention provides the following formula I shown multi-substituted amine compound or its isomer or its pharmaceutically acceptable salt, ester, prodrug or hydrate, its pharmaceutical composition, preparation method thereof and its use in the preparation of medicine for treating aids in use. The compound or pharmaceutical composition containing the compound can be used as an inhibitor for inhibiting HIV integrase with LEDGF/p75 between protein - protein interaction and HIV integrase dimerization, then can be used for the treatment of aids. . (by machine translation)
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Paragraph 0748; 0752-0755
(2018/04/27)
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- Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction
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Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R1 is C1 to C3 alkyl substituted with C3 to C6 cycloalkyl, CONR5R6 or a N-linked heterocyclic group; (CH2)nHet or (CH2)nAr; R2 is C1 to C6 alkyl; R3 is C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy; R4 is SO2NR7R8; R5 and R6 are each independently selected from H and C1 to C4 alkyl optionally substituted with C1 to C4 alkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; R7 and R8, together with the nitrogen atom to which they are attached, form a 4-R10-piperazinyl group; R10 is H or C1 to C4 alkyl optionally substituted with OH, C1 to C4 alkoxy or CONH2; H is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of, inter alia, male erectile dysfunction and female sexual dysfunction.
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Page column 54
(2010/02/06)
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- Influence of steric crowding on the electrochemical reduction of substituted tertiary pyridylcarboxamides in aqueous acidic medium
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In order to assess the influence of the steric crowding on the electrochemical reduction of pyridycarboxamides, we have studied a series of tertiary aromatic or alicyclic pyridylcarboxamides. We have shown that increasing steric hindrance at the amide nit
- Largeron, Martine,Auzeil, Nicolas,Bacque, Eric,Fleury, Maurice-Bernard
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p. 495 - 501
(2007/10/03)
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- Potent inhibitors of secretory phospholipase A2: Synthesis and inhibitory activities of indolizine and indene derivatives
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Phospholipase A2 is an enzyme which hydrolyzes the sn-2 position of certain cellular phospholipids. The liberated lysophospholipid and arachidonic acid are precursors in the biosynthesis of various biologically active products. As human nonpancreatic sPLA2 is present in high levels in the blood of patients in several pathological conditions, the potent sPLA2 inhibitors have been suggested to be useful drugs. Here we describe the synthesis, structure-activity relationship, and inhibitory activities of indolizine and indene derivatives. 1-(Carbamoylmethyl)indolizine derivatives and 1-oxamoylindolizine derivatives exhibited very potent inhibitory activity. The former was unstable to air oxidation, but the latter exhibited an improvement both in stability and in potency. Some compounds approached the stoichiometric limit of the chromogenic assay.
- Hagishita, Sanji,Yamada, Masaaki,Shirahase, Kazuhiro,Okada, Toshihiko,Murakami, Yasushi,Ito, Yuji,Matsuura, Takaharu,Wada, Masaaki,Kato, Toshiyuki,Ueno, Masahiko,Chikazawa, Yukiko,Yamada, Katsutoshi,Ono, Takashi,Teshirogi, Isao,Ohtani, Mitsuaki
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p. 3636 - 3658
(2007/10/03)
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- Amino naphthyridine compounds as anti-rhoumatic agents
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This invention relates to compounds of formula I and pharmaceutically acceptable salts thereof STR1 in which R1 represents hydrogen, alkyl, hydroxy, carboxyalkenyl, alkoxycarbonyalkenyl, hydroxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxy, halogenated alkyl, carboxy alkoxycarbonyl or alkanoylamino; R2 represents hydrogen, halo, alkoxy, hydroxy, alkanoyloxy, or phenoxy; R3 represents hydrogen or alkyl; R4 represents hydrogen, halo, alkoxycarbonyl, a benzyloxycarbonyl, alkanoyl, benzoyl, carbamoyl, alkyl, carboxy, hydroxyalkyl or alkylthio; R5 represents hydrogen or alkyl; R6 represents hydrogen, alkyl [optionally substituted by one or more of the following: hydroxy, halo or an amino group of formula --NR12 R13 ], a C3-12 alicyclic hydrocarbon group, phenyl, (cycloalkyl)alkyl or benzyl; R7 represents hydrogen, halo, trifluoromethyl, trifluoromethoxy, alkyl, carboxy, or alkoxy; R8 represents hydrogen, halo, trifluoromethyl, trifluoromethoxy, alkyl or alkoxy; and R9 represents hydrogen or alkyl; which are antirheumatic agents. Compositions containing these compounds and processes to make them are also disclosed.
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- SYNTHESES OF A NATURALLY OCCURRING HYDROXAMIC ACID AND ITS ANALOGUES
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A naturally occurring cyclic hydroxamic acid, isolated from Pseudomonas species, and its analogues were synthesized via six steps starting from 2-hydroxy-3-methoxypyridine.The antimicrobial activity of the synthesized compounds is described.
- Ohta, Akihiro,Takahashi, Nobuhiro,Shirokoma, Yasuko
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p. 875 - 884
(2007/10/02)
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- Fluoroalkoxy substituted benzimidazoles useful as gastric acid secretion inhibitors
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Dialkoxypyridines of formula I STR1 wherein R1 is 1-3C-alkyl which is completely or predominantly substituted by fluorine, or a chlorodifluoromethyl radical and R1' is hydrogen, halo, trifluoromethyl, 1-3C-alkyl, or 1-3C-alkoxy which is optionally completely or predominantly substituted by fluorine, or R1 and R1', together with the oxygen atom to which R1 is bonded, are 1-2C-alkylenedioxy, which is optionally completely or partly substituted by fluorine, or chlorotrifluoroethylenedioxy, R3 is 1-3C-alkoxy, one of R2 and R4 is 1-3C-alkoxy and the other is a hydrogen atom or 1-3C-alkyl and n is 0 or 1, and salts thereof are new compounds with a pronounced protective action on the stomach. Processes for preparing these compounds, medicaments containing them and their use, as well as intermediate compounds and their use for preparing the subject dialkoxypyridines, are disclosed.
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- Heterocyclic ring fused pyrimidine-4 (3H)-ones as anticoccidial agents
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Certain trans-3-[3-(3-hydroxy-2-piperidyl)-2-oxopropyl]thieno[3,2-d]pyrimidin-4(3H)-one and furo[3,2-d]pyrimidin-4(3H)-one derivatives, a method of using same as anticoccidial agents, intermediates therefor, and a process for certain intermediates therefo
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- Picoline derivative useful as gastric acid secretion inhibitors
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Picoline derivatives of the formula I STR1 wherein the substituents have the meanings given in the description, and their salts are new compounds having a pronounced protective action on the stomach.
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- Acid-catalysed Rearrangement of 3-Acyl-6-alkoxy-5,6-dihydro-4H-1,2-oxazines: a Route to 3-Alkoxypyridine 1-Oxides
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6-Alkoxy-5,6-dihydro-4H-1,2-oxazines (2) and (5) have been prepared by the reaction of chloro oximes (1) with enol ethers in the presence of sodium carbonate.The 3-phenyloxazine (2) rearranges to the nitrone (3) in methanolic HCl.In contrast, the 3-acyloxazines (5a-e) are converted into 3-alkoxypyridine 1-oxides (7) in aqueous alcoholic HCl.With HCl in acetic acid the oxazine (5a) is converted into 2-chloromethyl-3-hydroxypuridine hydrochloride (10a); analogous reactions take place with oxazines (5b) and (5d).Possible mechanisms for these reactions are discussed.
- Gilchrist, Thomas L.,Iskander, George M.,Yagoub, Ahmed K.
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p. 2769 - 2774
(2007/10/02)
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