Design, synthesis and evaluation of novel potent angiotensin II receptor 1 antagonists
A series of new angiotensin II (Ang II) receptor 1 antagonists were designed, synthesized and evaluated. All compounds showed nanomolar affinities for the angiotensin II type 1 receptor in radioligand binding assays and could reduce blood pressure signifi
A process for the preparation of Irbesartan or a pharmaceutically acceptable salt thereof comprising the step of coupling the 1-pentanamidocyclapentanecarboxamide of formula (V) with 4'-substituted methyl biphenyl-2-carbonitrile or 1-(4'-substituted methyl biphenyl-2-yl)-1H-tetrazole wherein tetrazole can be protected or unprotected to obtain the N-[(2'-cyanobiphenyl-4-yl)methyl]-1-pentanamidocyclopentanecarboxamide or N-[1-({[2'-(1H-tetrazol-1-yl)biphenyl-4-yl]methylamino)methyl)cydopentyl]pentanamide wherein tetrazole can be protected or unprotected that is further processed to Irbesartan or a pharmaceutical acceptable salt thereof.
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Page/Page column 10; 12
(2010/06/20)
SYNTHESIS OF 2-BUTYL-3-(2'-(1-TRITYL-1H-TETRAZOL-5-YL)BIPHENYL-4-YL)-1,3-DIAZASPIROL[4,4]-NON-ENE-4-ONE
Provided is a novel method of making 2-butyl-3-[[2'(1-trityl-1H-tetrazol-5-yl)biphen-4-yl]methyl]1,3-diazaspiro[4,4]non-1-ene-4-one, which can be converted to irbesartan. Also provided are methods of making irbesartan.
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Page 18
(2010/02/08)
Preparation of acylated α-amino carboxylic acid amides
A method of preparing acylated α-amino carboxylic acid amides directly from amino nitriles in high yield and purity. The method involves acylating the amino nitrile with an acyl halide under Schotten-Baumann conditions, and hydrolyzing the resulting nitrile to the amide. The resulting acylated amino carboxylic acid amide precipitates and can be isolated by filtration in high purity.
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(2008/06/13)
Method of treating or preventing cardiac arrhythmia employing an N-substituted heterocyclic derivative
The invention relates to the use of an N-substituted heterocyclic derivative and its pharmaceutically acceptable salts for the treatment or prevention of cardiac arrhythmia. These derivatives have the structure STR1
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(2008/06/13)
N-SUBSTITUTED HETEROCYCLIC DERIVATIVES, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT
The invention relates to N-substituted heterocyclic derivatives and its salts. These derivatives have the formula (I) in which the substituents are as defined in the specification. Application: Angiotensin II antagonists
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(2008/06/13)
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