- NOVEL DUAL ACTION RECEPTORS ANTAGONISTS (DARA) AT THE AT1 AND ETA RECEPTORS
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The present invention relates to new compounds of the formula [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, and R31 are as specified herein. The invention also relates to a method for preparation thereof, as well as combinations of the new compounds with previously known agents. The invention also relates to the use of the above-mentioned compounds and combinations for the preparation of a medicament for treating hypertension of different kinds, alleviating organ damage of different kinds, treating or preventing diabetic nephropathy, treating endothelin and angiotensin mediated disorders, and treating prostate cancer.
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Page/Page column 41
(2010/11/28)
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- 2-(Ethoxycarbonylmethyl)-1H-naphtho[1,8-de]-1,2,3-triazine anion: A new glycine enolate equivalent
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The titled triazine can be alkylated with LDA and a variety of alkyl halides: Subsequent reduction with aluminium amalgam cleaves the naphthotriazine moiety to afford substituted α amino acids in excellent overall yields; the sequence defines a novel methodology that can be applied under non-acidic and largely non-aqueous conditions. (C) 2000 Elsevier Science Ltd.
- Anilkumar,Chandrasekhar,Sridhar
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p. 6665 - 6668
(2007/10/03)
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- Therapeutic agents
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Compounds of formula I STR1 and pharmaceutically acceptable salts thereof in which m is an integer from 1 to 3; n is an integer from 2 to 6; R1 is phenyl optionally substituted by one or more substituents selected from halo, hydroxy, alkoxy, alkanoyl, alkyl, halogenated alkyl, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, nitro, optionally substituted amino, optionally substituted sulphamoyl, optionally substituted carbamoyl or phenyl, or R1 is naphthyl; R2 is H, alkyl or phenyl; R3 is H, alkyl, alkenyl or alkoxyalkyl; R4 is H or hydroxy; and R5 is H or together with R4 represents a bond; have utility in the treatment of obesity and affective disorders such as depression and anxiety.
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- A simple method for the synthesis of cyclic α-amino acids
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The benzylidene derivative of glycine ethyl ester was alkylated with various electrophiles to synthesize cyclic α-amino acids bearing aromatic and aliphatic side chains.
- Kotha,Kuki
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p. 1565 - 1568
(2007/10/02)
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- Peptide derivatives and processes for their preparation
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Peptide ester and amide derivatives of the general formula I: STR1 in which X is H or an acyl, A and B are structurally defined amino acid residues, n is an integer of from 1 to 3, R1 is H or a lower alkyl and either R2 or C is a def
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- A FACILE PROCEDURE FOR THE PREPARATION OF ALICYCLIC α-AMINO ACIDS
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A convenient method for the preparation of alicyclic α-amino acids is described which utilizes ethyl isocyanoacetate and the appropriate dibromo-substituted aliphatic alkylating agent.
- Kalvin, Douglas,Ramalingam, Kondareddiar,Woodward, Ronald
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p. 267 - 272
(2007/10/02)
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- Cyclit-Reaktionen, II. Darstellung von Bausteinen zur Synthese carbocyclischer Furanose-Analoga
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The four isomeric hydroxycyclopentenmethanols 6a to 9a can easily be made by allylhydroxylation of the epoxides 2 and 4 with phenyl selenide.In a second way the pair 8a and 9a has been synthesized from 11 via 15.As the preparation of 20 demonstrates, the functionalisation of 6a to 9a to carbocyclic furanoses is possible.The dicarboxylic diethyl esters 23 and 33 can be converted into models for carbocyclic ketofuranoses.
- Paulsen, Hans,Maass, Uwe
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p. 346 - 358
(2007/10/02)
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- Synthesis of 1,1-Diphenylaminoalcohols
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The synthesis of 2-amino-2-methyl-1,1-diphenyl-1-propanol (2a) and some of its aryl- and N-substituted derivatives from amino acid esters and Grignard compounds is described.The limits of this synthesis are reported, and so are other methods for the synthesis of amino alcohols.
- Bertram, Juergen
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