- SMALL MOLECULE ACTIVATORS OF NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NAMPT) AND USES THEREOF
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Provided herein are small molecule activators of Nicotinamide Phosphoribosyltransferase (NAMPT), compositions comprising the compounds, and methods of using the compounds and compositions.
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Paragraph 00738
(2018/08/03)
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- TRICYCLIC COMPOUND AND MEDICAL USE THEREOF
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The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom, a halogen atom, a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or mercapto optionally having a substituent, Xa to Xe are each a carbon atom or a nitrogen atom, m is 0 to 2, and ring A to ring C are each a ring optionally having substituent(s), or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.
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Page/Page column 45
(2009/09/28)
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- AZABENZOFURAN SUBSTITUTED THIOUREAS; INHIBITORS OF VIRAL REPLICATION
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The present invention provides compounds of Formula: (1), wherein the variables Ar, A1, A2, A3, A4, R5, R6, R7, V, W, X, and Y are defined herein. Certain compounds of Formula (1
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- Furopyridines. XXI [1]. Synthesis of Cyano Derivatives of Furo-[2,3-b]-,-[2,3-c]- And -[3,2-c]pyridine and Their Conversion to Derivatives Having Another Carbon-substituent
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Cyanation of furo[2,3-b]-, -[2,3-c]- and -[3,2-c]pyridine N-oxides 1a, 1b and 1c by the Reissert-Henze method, reaction with benzoyl chloride and trimethylsilyl cyanide in dichloromethane and the reaction with trimethylsilyl cyanide and triethylamine in acetonitrile afforded 6-cyanofuro[2,3-b]- 2a, 7-cyanofuro[2,3-c]- 2b and 4-cyanofuro[3,2-c]pyridine 2c in moderate to excellent yield. The cyano group in 2a, 2b and 2c was converted to carboxamides 3a, 3b and 3c, ethyl imidates 5a, 5b and 5c and ethyl carboxylates 6a, 6b and 6c. Reaction of the N-oxides with trimethylsily bromide in acetonitrile gave the deoxygenated furopyridine 7a and 7d, bifuropyridyl 8b and 8c, and the N-oxide 9 of 8c.
- Shiotani, Shunsaku,Taniguchi, Katsunori
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p. 493 - 499
(2007/10/03)
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- Furopyridines. XII. Reaction of 3-Bromo, 2-Phenylthio and 2-Phenylthio-3-bromo Derivatives of Furo-, Furo-, Furo- and Furopyridine with Several Alkyllithiums
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This paper describes reactions of 3-bromo- 1a-d, 2-phenylthio- 5a-d and 2-phenylthio-3-bromofuropyridines 6a-d with n-butyl-, t-butyl- and methyllithium and lithioacetonitrile.Lithiation of compounds 1a-d with n-butyl- or methyllithium gave the parent furopyridines 2a-d and o-ethynylpyridinols 3a-d.Reaction of compounds 5a-d with methyllithium afforded o-(phenylthioethynyl)pyridinols 7a-d, which were also yielded by reaction of compounds 6a-d with t-butyl- or methyllithium.The phenylthio group in compounds 7a-d were substituted with t-butyl group by the reaction with excess t-butyllithium.In contrast, 2-phenylthio group in compounds 5a-d and 6a-d was substituted with cyanomethyl group by reaction with lithioacetonitrile to give compounds 11a-d and 10b,c respectively.
- Shiotani, Shunsaku,Morita, Hiroyuki
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p. 413 - 422
(2007/10/02)
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- Thieno and furopyridinium-substituted cephalosporins
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Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetylamino group and in the 3-position with a thienopyridinium methyl group or a furopyridinium methyl group are broad spectrum antibiotics highly effective in combating bacterial infections of gram-negative and gram-positive microorganisms. The cephalosporins are best prepared by reacting a silylated 7-[2-(heterocyclic)-2-oximinoacetylamino-3-iodomethyl-3-cephem-4-carboxylic acid with the thienopyridine or the furopyridine. Pharmaceutical formulations comprising a compound of the invention and a method for treating bacterial infections comprising their use are also provided.
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- Oxazole and oxadiazole cephalosporins
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Broad spectrum cephalosporin antibiotics represented by the betaine structure of the formula STR1 wherein R is a 5-membered amino-substituted heterocyclic containing oxygen and nitrogen; R' is e.g., hydrogen or C1 -C4 alkyl; and bicyclicpyridinium is a thienopyridinium or a furopyridinium group; are prepared by reacting a silylated 3-iodomethyl cephalosporin with a thienopyridine, e.g., thieno[2,3-b]pyridine or a furopyridine. The compounds are potent antibacterials against gram-positive and gram-negative organisms. Pharmaceutical compositions and a method for treating bacterial infections are also provided.
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