- On the Michael Type Addition of Dipeptides to 4-Oxo-4-phenyl-2-butenoic Acid Derivatives
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The title reaction afforded the adducts 3 in variable selectivity, but the isomers of (S,S,S)-configuration were easily isolated; the reversibility of the reaction permits the recovery of the starting materials from the mother liquor.High selectivity has been observed in one case only. - Keywords: Michael type addition; 4-Oxo-4-phenyl-2-butenoic acids; (S)-Alanyl-(S)-proline; (S)-Lysyl-(S)-proline
- Fischer, Janos,Fodor, Tamas,Dobay, Laszlo
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- A process for preparing high-purity lisinopril
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The invention provides a method for synthesizing high purity lisinopril, using L - proline weakly alkaline compound ammonium salt to replace the L - proline in the strong alkali compound salt (such as tetramethyl ammonium hydroxide, sodium hydroxide), (II) with the lisinopril hydride in the DCC and N - hydroxy succinimide (NHS) in the presence of a condensation, hydrolysis to obtain the lisinopril. The preparation method from the source control the specific impurity N6 - (3 - Carboxyl propionyl) lisinopril (I) generating, so that the obtained lisinopril and its dihydrate pharmaceutical standards, is suitable for industrial production.
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Paragraph 0045-0074
(2019/05/15)
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- COMPOSITIONS AND METHODS FOR DIAGNOSING AND TREATING SALT SENSITIVITY OF BLOOD PRESSURE
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To characterize the urinary exosome miRNome, microarrays were used to identify the miRNA spectrum present within urinary exosomes from ten individuals that were previously classified for their salt sensitivity status. The present application discloses distinct patterns of selected exosomal miRNA expression that were different between salt-sensitive (SS), salt-resistant (SR), and inverse salt-sensitive (ISS) individuals. These miRNAs can be useful as biomarkers either individually or as panels comprising multiple miRNAs. The present invention provides compositions and methods for identifying, diagnosing, monitoring, and treating subjects with salt sensitivity of blood pressure. The applications discloses panels of miRNAs useful for comparing profiles, and in some cases one or more of the miRNAs in a panel can be used. The miRNAs useful for distinguishing SS and SR or ISS and SR subjects. One or more of the 45 miRNAs can be used. Some of the miRNAs have not been previously reported to be circulating. See those miRNAs with asterisks in FIG. 1 and below. The present invention encompasses the use of one or more of these markers for identifying and diagnosing SR, SS, and ISS subjects.
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- Process for separating the diastereomers of RSS-snd SSS-N- a [1-carboxy -3-Phenylpropyl] lysylproline
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A process for separating the diastereomers of RSS— and SSS—N-α[1-carboxy-3-phenylpropyl]lysylproline is described. Previous chromatographic processes for separating the diastereomers of this peptide active substance, such as for example adsorption chromatography, exhibited disadvantages with regard to the solvents used and throughput. These disadvantages do not occur if basic ion exchangers are used in the chromatographic separation of the diastereomers. In particular, purely aqueous solutions may be used as the eluent.
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Page/Page column 2
(2011/04/19)
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- USE OF SUBSTITUTED 2 PHENYLBENZIMIDAZOLES AS MEDICAMENTS
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The present invention relates to the use of a substituted 2-phenylbenzimidazole of formula I wherein R1, R2, R3, R 4, R5 and m have the meanings given in the claims, for the preparation of a medicament for the treatment or prevention of diseases involving glucagon receptors, as well as new compounds of formula I wherein R1 is a group of formula
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- A Stereoselective Synthesis of N--L-alanine Derivatives by Means of Reductive Amination
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A stereoselective synthesis of N--L-alanine, a portion of the molecule of angiotensin converting-enzyme(ACE) inhibitors, by reductive amination utilizing catecholborane and further applications of the reaction to the synthesis of ACE inhibitors are described.
- Iwasaki, Genji,Kimura, Rieko,Numao, Naganori,Kondo, Kiyoshi
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p. 1691 - 1694
(2007/10/02)
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- Synthesis of N2-[(S)-1-carboxy-3-phenylpropyl]-L-lysyl-L-proline (lisinopril).
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The synthesis and some of the spectral properties of N2-[(S)-1-carboxy-3-phenylpropyl]-L-lysyl-L-proline (lisinopril, MK-521) are described. This compound inhibits angiotensin-converting enzyme with an IC50 of 1.2 X 10(-9) M.
- Wu,Douglas,Ondeyka,Payne,Ikeler,Joshua,Patchett
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p. 352 - 354
(2007/10/02)
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- ANTIHYPERTENSIVE COMPOSITION
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A pharmaceutical composition is disclosed which comprises the combination of interphenylene 9-thia-11-oxo-12-aza prostanoic acid derivatives and carboxyalkyl dipeptide derivatives.
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