Patent EA-004882-B1 (EA)
Title: Sodium-hydrogen-exchanger type 1 inhibitor (nhe-1)
Inventor: CHEN WEICHAO GEORGE
IPC: A61P9/00
Filed: 2001-02-28
Abstract: 1. A compound having the Formula I a prodrug thereof or a pharmaceutically acceptable salt of said compound or of said prodrug with the proviso that [5-cyclopropyl-1-(quinolin-5-yl)-1H-pyrazole-4-carbonyl]guanidine is not included. 2. [5-Cyclopropyl-1-(2-quinolon-5-yl)-1H-pyrazole-4-carbonyl]guanidine, or a pharmaceutically acceptable salt thereof. 3. A method of reducing tissue damage resulting from ischemia or hypoxia comprising administering to a mammal in need of such treatment a therapeutical effective amount of a compound of claim 1, a prodrug thereof or a pharmaceutical acceptable salt of said compound or of said prodrug. 4. A method as recited in claim 3 wherein the tissue is cardiac, brain, liver, kidney, lung, gut, skeletal muscle, spleen, pancreas, nerve, spinal cord, retina tissue, the vasculature, or intestinal tissue. 5. A method as recited in claim 3 wherein the amount of the compound of claim 1, a prodrug thereof or a pharmaceutical acceptable salt of said compound or of said prodrug is about 0.01 mg/kg/day to about 50 mg/kg/day. 6. A method as recited in claim 5 wherein the mammal is a female or male human. 7. A method as recited in claim 6 wherein said tissue is heart tissue. 8. A method as recited in claim 6 wherein said tissue is brain tissue. 9. A method as recited in claim 6 wherein said tissue is liver tissue. 10. A method as recited in claim 6 wherein said tissue is kidney tissue. 11. A method as recited in claim 6 wherein said tissue is lung tissue. 12. A method as recited in claim 6 wherein said tissue is gut tissue. 13. A method as recited in claim 6 wherein said tissue is skeletal muscle tissue. 14. A method as recited in claim 6 wherein said tissue is spleen tissue. 15. A method as recited in claim 6 wherein said tissue is pancreas tissue. 16. A method as recited in claim 6 wherein said tissue is retina tissue. 17. A method as recited in claim 6 wherein the compound is administered prophylactically. 18. A method as recited in claim 6 wherein the compound is administered prior to surgery. 19. A method as recited in claim 6 wherein the compound is administered prior to cardiac surgery. 20. A method as recited in claim 6 wherein the compound is administered during surgery. 21. A method as recited in claim 6 wherein the compound is administered during cardiac surgery. 22. A method as recited in claim 6 wherein the compound is administered within twenty-four hours after surgery. 23. A method as recited in claim 6 wherein the compound is administered within twenty four hours after cardiac surgery. 24. A method as recited in claim 6 wherein the tissue damage resulting from ischemia is ischemic damage and is incurred during organ transplantation. 25. A method as recited in claim 6 wherein the compound is administered to prevent perioperative myocardial ischemic injury. 26. A pharmaceutical composition which comprises an amount of the compound of claim 1, a prodrug thereof or a pharmaceutical acceptable salt of said compound or of said prodrug and a pharmaceutical acceptable carrier, vehicle or diluent. 27. A pharmaceutical composition for the reduction of tissue damage resulting from ischemia or hypoxia which comprises a therapeutical effective amount of the compound of claim 1, a prodrug thereof or a pharmaceutical acceptable salt of said compound or of said prodrug and a pharmaceutical acceptable carrier, vehicle or diluent. 28. A method as recited in claim 6 wherein the compound is administered prior to, during and after surgery. 29. A method as recited in claim 6 wherein the compound is administered prior to, during and after cardiac surgery. 30. A method of producing [5-cyclopropyl-1-(2-quinolon-5-yl)-1H-pyrazole-4-carbonyl]guanidine by administering [5-cyclopropyl-1-(quinolin-5-yl)-1H-pyrazole-4-carbonyl]guanidine to a human.