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Last Updated: December 23, 2024

Claims for Patent: 9,796,741


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Summary for Patent: 9,796,741
Title:Aryl, heteroaryl, and heterocyclic compounds for treatment of complement mediated disorders
Abstract:Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein Ror Ron the A group is an aryl, heteroaryl or heterocycle (R) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
Inventor(s):Gadhachanda Venkat Rao, Wang Qiuping, Pais Godwin, Hashimoto Akihiro, Chen Dawei, Wang Xiangzhu, Agarwal Atul, Deshpande Milind, Wiles Jason Allan, Phadke Avinash S.
Assignee:Achillion Pharmaceuticals, Inc.
Application Number:US14631625
Patent Claims: 2. A method for the treatment of a disorder mediated by complement factor D claim 1 , comprising administering an effective amount to a host in need thereof of a compound of or a pharmaceutically acceptable salt thereof claim 1 , optionally in a pharmaceutically acceptable carrier.3. The method of claim 2 , wherein the host is a human.4. The method of claim 2 , wherein the disorder is age-related macular degeneration (AMD).5. The method of claim 2 , wherein the disorder is retinal degeneration.6. The method of claim 2 , wherein the disorder is an ophthalmic disease.7. The method of claim 2 , wherein the disorder is paroxysymal nocturnal hemoglobinuria (PNH).8. The method of claim 2 , wherein the disorder is multiple sclerosis.9. The method of claim 2 , wherein the disorder is arthritis.10. The method of claim 2 , wherein the disorder is rheumatoid arthritis.11. The method of claim 2 , wherein the disorder is a respiratory disease or a cardiovascular disease.22. The compound of claim 1 , wherein B is —(C-Calkyl)(aryl) or —(C-Calkyl)(heteroaryl) each of which B is unsubstituted or substituted with one or more substituents independently chosen from Rand R claim 1 , and 0 or 1 substituents chosen from Rand R.23. The compound of claim 22 , wherein B is —(CH)(aryl) substituted with two substituents independently chosen from Rand R.24. The compound of claim 23 , wherein Ris halogen.25. The compound of claim 24 , wherein there are two Rsubstituents and one is chlorine and the other is fluorine.26. The compound of claim 22 , wherein B is aryl or heteroaryl each of which B is unsubstituted or substituted with one or more substituents independently chosen from Rand R.27. The compound of claim 26 , wherein B is aryl.28. The compound of claim 26 , wherein B is heteroaryl.29. The compound of claim 28 , wherein heteroaryl is 2-pyridine.30. The compound of claim 29 , wherein 2-pyridine is substituted with one substituent independently chosen from R.31. The compound of claim 30 , wherein Ris halogen.39. The method of claim 2 , wherein the disorder is MPGN II.41. The method of claim 40 , wherein the host is a human.42. The method of claim 40 , wherein the disorder is age-related macular degeneration (AMD).43. The method of claim 40 , wherein the disorder is retinal degeneration.44. The method of claim 40 , wherein the disorder is an ophthalmic disease.45. The method of claim 40 , wherein the disorder is paroxysymal nocturnal hemoglobinuria (PNH).46. The method of claim 40 , wherein the disorder is multiple sclerosis.47. The method of claim 40 , wherein the disorder is arthritis.48. The method of claim 40 , wherein the disorder is rheumatoid arthritis.49. The method of claim 40 , wherein the disorder is a respiratory disease or a cardiovascular disease.50. The method of claim 40 , wherein the disorder is MPGN II.

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