摘要:
Novel unnatural dipeptoids useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. The compounds are agents useful for preventing the response to withdrawal from chronic treatment or use of nicotine, diazepam, alcohol, cocaine, caffeine, and opioids. The compounds are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare diagnostic compositions.
摘要:
This invention provides a method for treating or preventing inflammation or atherosclerosis in mammals comprising administering an effective amount of a 15-LO inhibitor of Formula I: ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, nitro, halo, CN, OR.sup.6, NR.sup.6 R.sup.7, --CO.sub.2 R.sup.6, CONR.sup.6 R.sup.7, CH.sub.2 OR.sup.6, or CH.sub.2 NR.sup.6 R.sup.7, and R.sup.2 and R.sup.3, and R.sup.4 and R.sup.5, when attached to adjacent ring atoms, can be --(CH.sub.2).sub.3 or 4 --;in which R.sup.6 and R.sup.7 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl, and when taken together with the nitrogen to which they are attached, R.sup.6 and R.sup.7 can complete a cyclic ring having from 3 to 7 carbon atoms; ##STR2## in which R.sup.8, R.sup.8', R.sup.9, and R.sup.9' independently are hydrogen or C.sub.1 -C.sub.6 alkyl, n is 0, 1, or 2, and Z.sup..crclbar. is an anion, and pharmaceutically acceptable salts thereof.
摘要:
The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.
摘要:
The present invention relates to novel coumarin derivatives and related compounds which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The coumarin derivatives are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized coumarins and of related structures.
摘要:
The present invention relates to novel substituted tricyclic pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The tricyclic pyrone derivatives are useful in the development of therapies for the treatment of vital infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized tricyclic pyrones and of related structures.