The term "heteroaryl", as used herein, unless otherwise indicated, includes an organic radical derived from an aromatic heterocyclic compound by removal of one hydrogen, such as pyridyl, furyl, pyroy!, thienyl, isothiazoly!, imidazolyl, benzimidazolyl, tetrazolyl, pyrazinyl, pyrimidyl, quinolyl, isoquinoly:, benzofuryl, isobenzofury!, benzothieny!, pyrazolyl, indoiyl, isoindolyl, purinyl, carbazolyl, isoxazolyl, thiazoly!, oxazolyl, benzthiazoly!
The presentinvention also relates to a pharmaceutical composition for (a) the treatment of a condition selected from the group consisting ofarthritis, osteoporosis, cancer, synergy with cytotoxic anticancer agents, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, in combination with standard NSAID'S and analgesics and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic AQUESTIVE EXHIBIT 1004=page 1056 AQUESTIVE EXHIBIT 1004 page 1056
Solid compositions of a similar type may also be employedasfillers in gelatin capsules; preferred materials in this connection also include lactose or milk sugar as well as high molecular weight polyethylene glycols.
intravenous use) a sterile injectable solution of the active ingredient Salutions of a therapeutic compoundof the present invention in either sesame or peanutoil orin aqueous propylene glycol may be employed.
)propionicacid A solution of (2S)-2-hydroxy-3-(4-methoxybenzenesulfonyl)propionic acid benzyl ester (1.0 grams, 2.8 mmole) in methanol (70 mL) wastreated with 10% palladium on activated carbon (100 mg) and hydrogenated at 3 atmospheres pressure for 3 hours in a Parr shaker.