Abstract: Novel fluorinated diamino-heptene and-heptyne derivatives are inhibitors of ornithine decarboxylase enzyme involved in polyamine formation and have the following general Formula I: ##STR1## wherein: Y represents CH.sub.2 .dbd.CH-- or CH.tbd.C--; andp represents 1 or 2.
Abstract: Substances isolated after cultivation of a microorganism belonging to the genus Aspergillus in a culture medium comprise compounds which have structures: ##STR1## Together with salts and esters of the carboxylic acid, these compounds form a class of highly active hypocholesteremic and hypolipemic medicaments.
Type:
Grant
Filed:
May 28, 1981
Date of Patent:
December 13, 1983
Assignee:
Merck & Co., Inc.
Inventors:
George Albers-Schonberg, Henry Joshua, Maria B. Lopez
Abstract: Described is a process for preparing the compound having the structure: ##STR1## comprising the steps of reacting 1-acetyl-3,3-dimethylcyclohexane with a dialkyl carbonate; thereby forming a ketoester having the structure: ##STR2## wherein R represents C.sub.1 -C.sub.3 lower alkyl; reacting the said ketoester with an allyl halide to form a substituted ketoester having the structure: ##STR3## saponifying the substituted ketoester with base forming a substituted keto carboxylic ester salt; and hydrolyzing the said keto carboxylic acid salt with acid to form the corresponding acid; and then heating and decarboxylating the resulting keto carboxylic acid to form the desired compound.
Abstract: N-Acetyl-para-aminophenyl N'-acetylaminothioalkanoates I are new analgesic compounds with greatly reduced hepatotoxic effects, when taken in overdose, relative to N-acetyl-para-aminophenyl. They are prepared by reacting an N-acetylaminothioalkanoic acid IV with a reactive organic chloride V to form a mixed anhydride II and then reacting the latter with N-acetyl-para-aminophenol. The mixed anhydrides II are new and useful intermediates. Alternatively the derivatives I may be prepared by reacting the acid IV with bis-(4-nitrophenyl) sulfite to form a para-nitrophenyl N-acetylaminothioalkanoic acid ester VIII, reducing the latter to a para-aminophenyl N-acetylaminothioalkanoate VII, and acetylating this product. The esters VII and VIII are new and useful intermediates. Both reactions may pass through S-blocked intermediates, which are also new. Pharmaceutical compositions containing the derivatives I are disclosed, and also analgesic methods using them.
Type:
Grant
Filed:
March 22, 1982
Date of Patent:
September 20, 1983
Assignee:
Sterling Drug Inc.
Inventors:
George Margetts, Roderic S. Andrews, Jean Legros
Abstract: Process for the preparation of peptides including higher polypeptides utilizing indenylmethoxycarbonyl blocking groups and products produced thereby.
Abstract: Compounds represented by the formula ##STR1## wherein R and R.sup.1 are independently hydrogen or lower alkyl; R.sup.2 is lower alkenyl, lower alkynyl or --CH.sub.2 X wherein X is halogen, hydroxyl, lower alkoxy, lower alkylthio or a furanyl ring; and Z is hydroxyl, lower alkoxy or --NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl possess fungicidal activity. Moreover, some of the compounds of this invention also possess herbicidal activity.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, methanesulfonyl, or acetyl,R.sub.2 and R.sub.3 jointly mean oxo, oximino, or separately two hydrogen atoms, orR.sub.2 is hydrogen and R.sub.3 is hydroxy or amino, and when R.sub.3 is amino, the physiologically acceptable acid salts thereofpossess valuable pharmacological properties.
Type:
Grant
Filed:
January 27, 1982
Date of Patent:
March 1, 1983
Assignee:
Schering Aktiengesellschaft
Inventors:
Eberhard Schroeder, deceased, Clemens Rufer