Abstract: A malic acid or oxalacetic acid derivative is represented by the following formula (1): wherein ring Z is an alicyclic carbon ring; each of Ra and Rb is independently a hydrogen atom, a metal atom, or an organic group; and Y is a hydroxyl group or an oxygen atom, where ring Z is a bridged carbon ring or a monocyclic carbon ring having eight or more members when Y is an oxygen atom. The alicyclic carbon ring includes, for example, cyclooctane ring and adamantane ring. This compound is a novel malic acid derivative having an alicyclic group bonded to a carbon atom at the 3-position, or a novel oxalacetic acid derivative having a specific alicyclic group bonded to a carbon atom at the 3-position.

Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula I The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.

Abstract: The invention relates to processes for the preparation of 4a,5,9,10,11,12-hexahydro-6H-benzofuro(3a,3,2-ef)(2)benzazepine, or derivatives thereof. Furthermore, the invention also relates to the compounds formed during the preparation of 4a,5,9,10,11,12-hexahydro-6H-benzofuro(3a,3,2-ef)(2)benzazepine.

Abstract: Cysteine protease inhibitors which deactivate the protease by covalently bonding to the cysteine protease and releasing the enolate of a 1,3-dicarbonyl (or its enolic form). The cysteine protease inhibitors of the present invention accordingly comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a .beta.-dicarbonyl enol ether leaving group.

Abstract: .alpha.-Arylacrylates substituted by a heterocyclic radical and of the general formula I ##STR1## where R.sup.1 is alkoxy or alkylthio, R.sup.2 is alkyl, Het is quinolyl, which is unsubstituted or substituted, A is oxygen and n is 1, and their plant-tolerated acid addition salts and metal complexes, and the N-oxides of the heterocyclic compounds, and fungicides containing these compounds.