- TETRAHYDRO- AND DIHYDROQUINAZOLINONES
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The present invention relates to the use of tetrahydro- and dihydroquinazolinones of formula (I) as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases, their
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Page/Page column 62; 63; 73
(2010/11/23)
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- Access to variously substituted 5,6,7,8-tetrahydro-3H-quinazolin-4-ones via Diels-Alder adducts of phenyl vinyl sulfone to cyclobutene-annelated pyrimidinones
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Under basic conditions (Et3N, dioxane), the aromatic amidines 4 and also S-methylisothiourea 4g cleanly undergo Michael addition to methyl 2-chloro-2-cyclopropylideneacetate (5), followed by intramolecular nucleophilic substitution, cyclopropyl
- Dalai, Suryakanta,Belov, Vladimir N.,Nizamov, Shamil,Rauch, Karsten,Finsinger, Dirk,De Meijere, Armin
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p. 2753 - 2765
(2007/10/03)
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- PYRIMIDINE CARBOXYLIC ACID DERIVATIVES AND USE THEREOF
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The invention relates to pyrimidine carboxylic acid derivatives of formula (I), to methods for the production thereof, to their use for treating and/or preventing diseases, and their use for producing medicaments for treating and/or preventing diseases, p
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Page/Page column 34
(2010/11/23)
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- Triazole derivatives
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The present invention relates to triazole and imidazole derivatives of formula I and to their pharmaceutically acceptable acid addition salts. These compounds are NMDA receptor subtype blockers and are useful for the treatment of diseases related to the NMDA receptor.
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- Preparation of Triazolopyrimidines as Potential Antiasthma Agents
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With the use of the human basophil histamine release assay, 5-aryl-2-aminotriazolopyrimidines were found to be active as mediator release inhibitors.These compounds were prepared by reacting arylamidines with sodium ethyl formylacetate or with ethyl propiolate to give pyrimidinones.Treatment with phosphorus oxychloride gave a chloropyrimidine, which was converted to a hydrazinopyrimidine with hydrazine.Cyclization, using cyanogen bromide, gave the triazolopyrimidines, after a Dimroth rearrangement.Following a structure-activity evaluation, the5--2-amino (8-10), 5-(3-bromophenyl)-2-amino (8-13), 5--2-amino (8-11), and 5-(4-pyridinyl)-2-amino (6-7) compounds were found to have the best activity.They were chosen for further pharmacological and toxicological study.
- Medwid, Jeffrey B.,Paul, Rolf,Baker, Jannie S.,Brockman, John A.,Du, Mila T.,et al.
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p. 1230 - 1241
(2007/10/02)
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