- Preparation of 2-Substituted 4-Chloro-5-Formylimidazole and 5-Formylimidazole
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The invention relates to a preparation process for 2-substituted 5-formylimidazoles, wherein the intermediate high-pressurized synthesis of an 2-substituted 4-hydroxymethylimidazole as known in the art is conveniently avoided, and wherein much higher yields are obtained. Instead, it is proposed to prepare such 2-substituted 5-formylimidazoles via a one-pot synthesis involving 2-substituted 4-chloro-5-formylimidazole, thereby employing an additional hydrodehalogenation step. Moreover, it is found that the yield and purity of 2-substituted 4-chloro-5-formylimidazole itself can be significantly improved using a triflate catalyst in the preparation process.
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Page/Page column 3
(2008/12/08)
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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 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 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 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 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 left ventricular hypertrophy regression.
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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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- Substituted imidazolyl-alkylthio-alkanoic acids
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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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- A New Regioselective Synthesis of 1,2,5-Trisubstituted 1H-Imidazoles and Its Application to the Development of Eprosartan
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A new method is presented for the preparation of 1,2-disubstitued-1H-imidazole-5-carboxaldehydes by the reaction of N-monosubstituted amidines with 2-halo-3-alkoxy-2-propenals. The reaction is highly regioselective with ratios of 1,2,5:1,2,4-imidazolecarboxaldehydes ranging from 85:15 to 100: 0. This methodology could be extended with similar results to the synthesis of imidazole-5-nitriles by the reaction of 2-bromo-3-methoxy-2-propenenitrile with N-monosubstituted amidines.
- Shilcrat, Susan C.,Mokhallalati, Mohamed K.,Fortunak, Joseph M. D.,Pridgen, Lendon N.
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p. 8449 - 8454
(2007/10/03)
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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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- N-SUBSTITUTED IMIDAZOLE AND BENZIMIDAZOLE DERIVATIVES USEFUL AS ANGIOTENSON II ANTAGONISTS
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Compounds are disclosed having the formula STR1 These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
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- N-(heteroaryl) imidazolyl-alkenoic acids having angiotension II receptor antagonist activity
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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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- Substituted histidines having angiotension II receptor antagonist activity
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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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- 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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- Substituted [1H-imidazol-5-ylialkanoic acids having angiotension II receptor antagonist activity
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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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- SUBSTITUTED IMIDAZOLES HAVING ANGIOTENSIN II RECEPTOR BLOCKING ACTIVITY
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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
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- Process for production of 2-substituted-4-hydromethylimidazole compounds
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The invention provides a process for producing a 2-substituted-4-hydroxymethylimidazole easily and in good yield by means of simple equipment. This process comprises reacting hydroxymethylglyoxal, a monoaldehyde and ammonia in a sequence such that said monoaldehyde and ammonia are first reacted with each other and hydroxymethylglyoxal is then introduced into the reaction system for further reaction.
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- BENZOXAZOLE AND RELATED HETEROCYCLIC SUBSTITUTED IMIDAZOLE AND BENZIMIDAZOLE DERIVATIVES
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Novel compounds are disclosed having the formula STR1 wherein X, Y, R 1, R 2, R 3, R 4, and R 5 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
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- Imidazole and benzimidazole derivatives
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Novel angiotensin-II receptor antagonists are disclosed having the general formula STR1 wherein R 1, R 2, R 3, R 4, R 5, W and X are as defined herein.
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- Substituted 5-(alkyl)carboxamide imidazoles
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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
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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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- Substituted 5-((tetrazolyl)alkenyl)imidazoles and pharmaceutical methods of use thereof
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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
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- PREPARATION OF A MODEL SYSTEM FOR A CONSTRAINED ANGIOTENSIN II RECEPTOR ANTAGONIST
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An imidazooxazin-8-one system, designed to be a fused ring analog of a potent angiotensin II receptor antagonist, was prepared.
- Boschelli, Diane H.,Connor, David T.
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p. 121 - 124
(2007/10/02)
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- A practical synthesis of 2-butyl-4(5)-chloro-5(4)-hydroxymethyl-1H-imidazole
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A practical process for the synthesis of 2-butyl-4-hydroxymethyl imidazole (4) followed by chlorination to provide chloroimidazole 1 in an overall 71% yield has been developed.
- Shi,Frey,Tschaen,Verhoeven
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p. 2623 - 2630
(2007/10/02)
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