PROTEIN KINASE C INHIBITOR

• Main Authors: ENGEL, GARY, L, FAUL, MARGARET, M, JIROUSEK, MICHAEL, R, RICHADSON, LORI, A, WINNEROSKI, LEONARD, L., JR, FARID, NAGY, A
• Format: Patent
• Language: English; Russian
• Published: 28.08.2000
• Edition: 7
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

1. A salt of the Formula: and solvates thereof. 2. A salt of claim 1 of the Formula: and solvates thereof. 3. A salt of claims 1 or 2 which is substantially crystalline. 4. A salt of claim 3, which is (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16,21-dimetheno-1H,13H-dibenzo[E,K]pyrrolo[3,4-H][1,4,13]-oxadiazacyclohex adecine-1,3(2H)-dione methanesulfonate monohydrate 5. A salt of any one of claims 1 through 4, said salt having less than about 5 % total related substances. 6. A method of treating microvascular diabetic complications, which comprises administering a mammal in need thereof, a pharmaceutically effective amount of a compound of any one of claims 1 through 5. 7. A method of claim 6, wherein the pharmaceutically effective amount is 0.05 mg/kg/day to 0.25 ing/kg/day. 8. A pharmaceutical formulation comprising a salt of any one of claims 1 through 5 together with one or more pharmaceuticaily acceptable diluents, excipients or carriers. 9. A pharmaceutical formulation of claim 8, wherein the formulation comprises about 1 to about 20 mg of the salt. 10. A salt as claimed in any one of claims 1 through 5 for use a pharmaceutical. 11. A process for preparing a salt as claimed in any one of claims 1 through 5, which comprises reacting a compound of the formula: with mefchanesulfonic acid in a non-reactive organic solvent. 12. The process of claim 11, wherein the solvent is acetone-water. 13. The process of claim 12, wherein the solvent is about 5:1 to about 10:1 acetone to water by volume. 14. The process of claim 14, wherein the solvent is about 9:1 acetone to water by volume. 15. A compound whenever prepared by a process according to any one of claims 11 through 14.