Other

Proscript, Inc.

Osteoarthritis Sciences, Inc.

Alan R Jacobson

Jozef Oleksyszyn

Douglas G Gabler

Amino acid amides of 5-amino-1,3,4-thiadiazole-2-thione are disclosed. These compounds inhibit matrix metalloproteinase enzymes and cartilage degradation. Methods of treating diseases caused by over-activity of matrix metalloproteinases, such as osteoarthritis and rheumatoid arthritis, are also disclosed.

Amino acid amides of 1,3,4-thiadiazoles as matrix metalloproteinase

The present invention relates to a bile acid derivative, which comprises a bile acid derivatized at the carboxyl group with a hydroxamic acid or hydroxamate ester. The carboxyl group in the bile acid compound can also be derivatized with an amino acid or oligopeptide, whose C-terminus is derivatized with a hydroxamic acid or a hydroxamate ester. The present invention also relates to a method of use of a bile acid or a bile acid derivative to inhibit a metalloproteinase enzyme, comprising contacting a metalloproteinase with an effective amount of a bile acid or bile acid derivative. In another embodiment, the present invention further relates to a method of use of a bile acid or bile acid derivative to therapeutically treat a disease, which is ameliorated by inhibiting a metalloproteinase enzyme. In this method, a therapeutically effective amount of a bile acid, a bile acid derivative or physiologically acceptable salts thereof, is administered to a human or other mammal.

Bile acid inhibitors of metalloproteinase enzymes

A buoyant material/cable assembly is formed by placing elongated segments of a syntactic foam material around an underwater cable or the like to form a structure suitable for deep water applications. Banding in the form of oppositely directed spirals extend about the assembly and about its length to secure the segments together, to the cable, and against relative movement with respect to the cable. The bandings are fastened together at selected intervals along their length. Another form of the assembly consists of individual units of buoyant material formed of combined segments, secured together by bands. The units are spaced along the length of the cable. Another form consists of individual flotation units, or buoys, secured by flexible links to the cable. Oppositely directed spiral bandings extend along the length of the cable to secure the flexible links against movement with respect to the cable and with respect to each other. A floating platform is provided with cable tensioning, storage and feeding equipment; banding equipment; fastening equipment; buoyant material storage and supply reels and cable storage and supply reels in order to facilitate the construction of a buoyant material/cable assembly and simultaneous laying of the cable in deep water applications. While cable is continuously fed from storage and into the water the flotation material is applied along its length and secured to the cable. The amount of flotation material applied is varied to accommodate the laying conditions and seafloor conditions.

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Somerville, MA, United States of America

Alan R Jacobson