- DERIVATIVES OF N-ACYL-N'-PHENYLPIPERAZINE USEFUL (INTER ALIA) FOR THE PROPHYLAXIS OR TREATMENT OF DIABETES
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The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.
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Page/Page column 58
(2012/04/04)
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- FUSED HETEROCYCLIC COMPOUND AND USE THEREOF
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The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like.
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Page/Page column 363
(2008/06/13)
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- COMPOUNDS AND COMPOSITIONS AS PPAR MODULATORS
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The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families.
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Page/Page column 72
(2008/06/13)
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- COMPOUNDS, METHODS AND FORMULATIONS FOR THE ORAL DELIVERY OF A GLUCAGON LIKE PEPTIDE (GLP)-1 COMPOUND OR AN MELANOCORTIN 4 RECEPTOR (MC4) AGONIST PEPTIDE
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The present invention relates to novel compounds, methods, and formulations useful for the oral delivery of a GLP-1 compound or an MC4 agonist peptide.
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Page/Page column 72-73
(2008/06/13)
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- Selective ammonolysis and aminolysis of dimethyl succinate. Synthesis of optically active N-alkylsuccinimides
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Candida antarctica lipase catalyzes the selective monoammonolysis and aminolysis of dimethyl succinate with ammonia and aliphatic amines, respectively, in dioxane as solvent. This enzyme shows a high enantioselectivity when racemic amines are used. Optically active amidoesters are also obtained in the reaction of dimethyl succinate with racemic α-methylalkylamines in hexane as solvent. In this medium, the enzyme catalyzes the formation of N-alkylsuccinimides or optically active N-alkyl-α-methylsuccinimides from dimethyl succinate or α-methylsuccinate and amines.
- Puertas, Susana,Rebolledo, Francisca,Gotor, Vicente
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p. 1495 - 1502
(2007/10/02)
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- Ruthenium-Catalyzed Hydration of Nitriles and Transformation of δ-Ketonitriles to Ene-lactams: Total Synthesis of (-)-Pumiliotoxin C
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Hydration of nitriles with 1-2 equivalents of water can be performed efficiently by using RuH2(PPh3)4 catalyst to give the corresponding amides.Under the similar reaction conditions, δ-ketonitriles can be converted into the corresponding ene-lactams, which are versatile synthetic intermediates.The efficiency of the reaction is demonstrated by the short-step synthesis of (-)-pumiliotoxin C.
- Murahashi, Shun-Ichi,Sasao, Shigehiro,Saito, Eiichiro,Naota, Takeshi
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p. 8805 - 8826
(2007/10/02)
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- Ruthenium-Catalyzed Hydration of Nitriles and Transformation of δ-Keto Nitriles to Ene-Lactams
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Hydration of nitriles and transformation of δ-keto nitriles to ene-lactams can be performed efficiently by using RuH2(PPh3)4 catalyst under mild conditions.The effectiveness of the reaction is illustrated by the short-step synthesis of (-)-pumiliotoxin C.
- Murahashi, Shun-Ichi,Sasao, Shigehiro,Saito, Eiichiro,Naota, Takeshi
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p. 2521 - 2523
(2007/10/02)
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- KINETICS AND MECHANISM OF REVERSIBLE, BASE-CATALYSED RING CLOSURE OF 3-(METHOXYCARBONYL)PROPIONANILIDE AND O-(METHOXYCARBONYLMETHYL)-N-PHENYLCARBAMATE
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The rate constants of reversible, base-catalysed ring closure of 3-(methoxycarbonyl)propionanilide (I) and O-(methoxycarbonylmethyl)-N-phenylcarbamate (II) to 1-phenyl-2,5-pyrrolidinedione (III) and 3-phenyl-2,4-oxazolidinedione (IV), respectively, and the rates of solvolyses of the cyclization products III and IV in water and methanol have been measured.In both cases, an equilibrium is established between the starting ester and the cyclization product in methoxide solutions which is strongly shifted in favour of the starting ester.In the case of ester II in methoxidesolutions, the cyclization is followed by a much slower splitting of the cyclization product to give glycolic acid anilide.The effects of the group X=NH, CH2, O, S in the esters RNHCOXCH2COOCH3 on the rates of the cyclization and solvolysis of the cyclization products is discussed.
- Kavalek, Jaromir,Machacek, Vladimir,Svobodova, Gabriela,Sterba, Vojeslav
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p. 1005 - 1011
(2007/10/02)
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