- Multicomponent Pharmaceutical Adducts of α-Eprosartan: Physicochemical Properties and Pharmacokinetic Study
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Pharmaceutical adducts of α-eprosartan (EPR) with nicotinamide (NIC) and p-hydroxy benzoic acid (PHB) were prepared by a liquid assisted grinding technique. Prior to conducting this study, the single crystal structure of EPR was determined. This study was designed to improve the pH-dependent solubility and dissolution rate of EPR and hence its oral absorption across the gastrointestinal tract. Initially, differential scanning calorimetry and powder X-ray diffractometry were used as a screening tool for rapid cocrystal or eutectic mixture screening. The eutectic mixture of EPR with PHB in a 1:3 stoichiometry ratio shows a better solubility and dissolution rate in all aqueous buffers as compared to EPR/NIC cocrystals and pure EPR. The EPR/NIC cocrystal in a 1:1 stoichiometry ratio shows a better dissolution rate initially as compared to pure EPR but does revert back to EPR within the first 30 min in pH 1.2 and 6.8. Absorption and desorption profile of EPR adducts are reversible, suggesting no solid state transformation under experimental conditions. A significant increase in oral bioavailability in overnight fasted Sprague-Dawley rats is achieved with the EPR/NIC cocrystal (2.4-fold) and EPR/PHB eutectics (6.1-fold), even when the cocrystal transformation is suspected based on in vitro studies.
- Khare, Sawani G.,Jena, Sunil K.,Sangamwar, Abhay T.,Khullar, Sadhika,Mandal, Sanjay K.
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p. 1589 - 1599
(2017/04/11)
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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 EPROSARTAN INTERMEDIATE
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The present invention provides an improved process for preparation of (E)-α-[[2-butyl-1-[[4-(methoxycarbonyl)phenyl]methyl]-1H-imidazole-5-yl]methylene]-2-thiophene propanoic acid ethyl ester in high purity and in high yield. Thus, for example, 4-[[2-buty
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Page/Page column 3
(2011/04/14)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF PURE EPROSARTANAND ITS PHARMACEUTICAL ACCEPTABLE SALTS
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The present invention relates to an improved process for preparation of pure Eprosartan and its pharmaceutical acceptable salts comprising the steps of: a) treating the Eprosartan with hydrochloric acid; b) suspending the resulted Eprosartan hydrochloride
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Page/Page column 7
(2011/05/11)
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- PHARMACEUTICAL FORMULATION CONTAINING ANGIOTENSIN-II RECEPTOR BLOCKER
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The present invention provides a pharmaceutical formulation containing an angiotensin-II receptor blocker and a release-control material as a pharmacologically active ingredient and a pharmaceutical formulation comprising an immediate-release compartment and an extended-release compartment. The immediate-release compartment contains an agent as a pharmacologically active ingredient for preventing and inhibiting hepatitis and the extended-release compartment has an angiotensin-II receptor blocker as a pharmacologically active ingredient. The formulation of the present invention maximizes the effectiveness on pharmacologically and clinically lowering blood pressure and preventing complications when taking the formulation, helps to avoid interaction with a drug which is metabolized by the same enzyme in the liver, and prevents and inhibits the incidence of drug-induced hepatitis which is caused by drug administration for a long time.
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- AN IMPROVED PROCESS FOR THE PREPARATION OF EPROSARTAN
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The present invention provides an improved process for the preparation of Eprosartan or its pharmaceutically acceptable salt comprising the steps of: condensing compound of formula (a) with compound of formula (b) in presence of a catalyst, in a solvent to get a compound of formula (c), and hydrolyzing the compound of formula (c) to get Eprosartan and optionally converting Eprosartan to its pharmaceutically acceptable salt. The present invention also relates to process for the preparation of compound of formula (c) by condensing compound of formula (a) with compound of formula (b) in presence of dehydrating agent.
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Page/Page column 6-7
(2010/04/06)
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- IMPROVED PROCESS FOR MANUFACTURING ANHYDROUS (E)-3-[2-BUTYL-1- {(4-CARBOXYPHENYL) METHYL}-1H-IMIDAZOLE-5-YL]-(THIOPHEN-2- YLMETHYL)PROP-2-ENOIC ACID METHANE SULFONATE
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The present invention relates to a simple efficient and cost effective process for commercial manufacture of (E)-3-[2-Butyl-1-{(4-carboxyphenyl) methyl}-1H-imidazole-5-yl]- 2-(thiophen-2-ylmethyl)prop-2-enoic acid and its conversion to substantially pure
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Page/Page column 7; 11-12
(2009/08/14)
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- EPROSARTAN MESYLATE CRYSTALLINE PARTICLES AND A PROCESS FOR PREPARING PURE EPROSARTAN
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The present invention relates to eprosartan mesylate particles having relatively larger surface area, to the methods for the manufacture of said crystalline particles, and to pharmaceutical compositions comprising said crystalline particles. The present i
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Page/Page column 10-11
(2009/03/07)
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- IMPROVED PROCESS FOR EPROSARTAN INTERMEDIATE
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The present invention provides an improved process for preparation of (E)-α-[[2-butyl-1-[[4-(methoxycarbonyl)phenyl]methyl]-1 H-imidazole-5-yl] methylene]-2-thiophene propanoic acid ethyl ester in high purity and in high yield. Thus, for example, 4-[[2-bu
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- Synthesis and biological evaluation of [carboxyl-11C]eprosartan
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Essential hypertension occurs in approximately 25% of the adult population and one cause of hypertension is primary aldosteronism. Targeting the angiotensin II AT1 receptor using PET and an appropriate tracer may offer a diagnostic method for a
- Aberg, Ola,Lindhe, Oerjan,Hall, Hakan,Hellman, Per,Kihlberg, Tor,Langstroem, Bengt
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experimental part
p. 295 - 303
(2010/08/06)
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- IMPROVED PROCESS FOR EPROSARTAN
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The present invention provides an improved and commercially viable process for preparation of eprosartan and its pharmaceutically acceptable acid addition salts thereof in high purity and in high yield. Thus, for example, methyl 4-[[2-butyl-5-formyl-1 H-i
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Page/Page column 8-9
(2008/12/06)
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- Medicament
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The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for improving cognitive function.
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- Medicament
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The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the prevention of atheroma progression and the regression of atheroma.
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- Medicament
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The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for primary and secondary prevention of infarction.
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- Medicament
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The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the treatment of haemorrhagic stroke.
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- Medicament
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The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the treatment of angina.
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- Medicament
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The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the treatment of macular degeneration.
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- Medicament
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The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the treatment of diabetic nephropathy.
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- Medicaments
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The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the treatment of chronic inflammatory disease states.
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- ANGIOTENSIN II RECEPTOR BLOCKING COMPOSITIONS
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This invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier, an angiotensin II receptor antagonist and a second agent selected from a diuretic, a calcium channel blocker, a β-adrenoceptor blocker, a renin inhibit
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- Medicament
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The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the primary and secondary prevention of infarction.
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- 2-butyl-4-iodoimidazole-5-carboxaldehyde: A versatile intermediate for the synthesis of highly functionalized imidazoles
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The facile preparation of 2-butyl-4-iodoimidazole-5-carboxaldehyde 1 is described. The versatility of this intermediate in the synthesis of highly functionalized imidazoles is demonstrated with the synthesis of two potent and selective angiotensin II rece
- Wittenberger,Tasker,Sorensen,Donner
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p. 3231 - 3248
(2007/10/02)
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- Potent Nonpeptide Angiotensin II Receptor Antagonists. 2. (1-Carboxybenzyl)imidazole-5-acrylic Acids
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The further evolution of the imidazole-5-acrylic acid series of nonpeptide angiotensin II receptor antagonists is detailed (for Part 1, see: J.Med.Chem. 1992, 35, 3858).Modifications of the N-benzyl ring substitution were undertaken in an effort to mimic the Tyr4 residue of angiotensin II.Introduction of a p-carboxylic acid on the N-benzyl ring resulted in the discovery of compounds with nanomolar affinity for the receptor and good oral activity.SAR studies of these potent antagonists revealed that the thienyl ring, the (E)-acrylic acid, and the imidazole ring in addition to the two acid groups were important for high potency.Also, overlay comparisons of the parent diacid with both angiotensin II and a representative biphenylyltetrazole nonpeptide angiotensin II receptor antagonist are presented.The parent diacid analog, SKF 108566 or (E)-3--2-propenoic acid, is currently in clinical development for the treatment of hypertension.
- Keenan, Richard M.,Weinstock, Joseph,Finkelstein, Joseph A.,Franz, Robert G.,Gaitanopoulos, Dimitri E.,et al.
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p. 1880 - 1892
(2007/10/02)
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- Imidazolyl-alkenoic acids useful as angiotensin II receptor antagonists
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Angiotensin II receptor antagonists having the formula: STR1 which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma, pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals.
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