Methods for treating PDEIV-mediated diseases or conditions
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- VANDA PHARMACEUTICALS INC
- Filing Date
- 2026-02-25
- Publication Date
- 2026-06-23
Smart Images
Figure 2026102632000031 
Figure 2026102632000032 
Figure 2026102632000033
Abstract
Claims
1. A method for treating a patient having a phosphodiesterase IV (PDEIV)-mediated disease or condition, comprising: a compound of formula (I) in an amount effective to treat the disease or condition: 【Chemistry 1】 A method comprising administering a pharmaceutically acceptable salt thereof.
2. The method according to claim 1, wherein the phosphodiesterase IV (PDEIV)-mediated disease or condition is an inflammatory disease or condition.
3. The method according to claim 1 or claim 2, wherein the PDEIV-mediated disease or condition is an inflammatory skin disease.
4. The method according to any one of the preceding claims, wherein the PDEIV-mediated disease or condition is psoriasis, psoriasis vulgaris, atopic dermatitis, contact dermatitis, seborrheic dermatitis, congestive dermatitis, maculoplasty, Behçet's syndrome, lupus, alopecia, frontal fibrous alopecia, vitiligo, acne, lichen planus, uveitis, nodular prurigo, or discoid lupus erythematosus.
5. The method according to any one of claims 1 to 4, wherein the PDEIV-mediated disease or condition is psoriasis.
6. The method according to any one of claims 1 to 4, wherein the PDEIV-mediated disease or condition is atopic dermatitis.
7. The method according to any one of claims 1 to 4, wherein the PDEIV-mediated disease or condition is contact dermatitis.
8. The method according to claim 1, wherein the PDEIV-mediated disease or condition is psoriatic arthritis, psoriasis vulgaris, atopic dermatitis, or COPD.
9. The method according to claim 1, wherein the phosphodiesterase IV (PDEIV)-mediated disease or condition is an immune disorder.
10. The method according to claim 1, wherein the PDEIV-mediated disease or condition is a chronic inflammatory disorder, asthma, rheumatoid arthritis, or Behçet's syndrome.
11. The method according to claim 1, wherein the phosphodiesterase IV (PDEIV)-mediated disease or condition is a cytokine-mediated disease.
12. The method according to claim 1, wherein the phosphodiesterase IV (PDEIV)-mediated disease or condition is a neutrophil-mediated disease.
13. The method according to claim 1, wherein the phosphodiesterase IV (PDEIV)-mediated disease or condition is a neurodegenerative disorder.
14. The method according to any one of the claims, wherein the patient is a human being.
15. The method according to any one of the claims, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered as a pharmaceutical composition comprising the compound of formula (I) or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.
16. The method according to any one of the claims, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered topically, orally, orally, as a suppository, intravenously, parenterally, intraperitoneally, intramuscularly, intrafocally, subarachnoidally, intranasally, or subcutaneously.
17. The method according to any one of the claims, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered topically.
18. The method according to any one of claims 1 to 17, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered orally.
19. A method for inhibiting the release of inflammatory cytokines from mammalian inflammatory cells, wherein the mammalian inflammatory cells are subjected to an amount of a compound of formula (I) effective in inhibiting the release of inflammatory cytokines from the mammalian inflammatory cells: 【Chemistry 2】 A method comprising contacting the substance with a pharmaceutically acceptable salt thereof.
20. The method according to claim 19, wherein the inflammatory cytokine is an interleukin (IL) comprising tumor necrosis factor alpha (TNFα), IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-7, IL-8, IL-9, IL-10, IL-11, or IL-12, or an interferon comprising alpha-interferon, beta-interferon, or gamma-interferon.
21. A method for inhibiting PDEIV activity in mammalian inflammatory cells, wherein the mammalian inflammatory cells are subjected to an amount of a compound of formula (I) effective in inhibiting the PDEIV activity in the mammalian inflammatory cells: 【Transformation 3】 A method comprising contacting the substance with a pharmaceutically acceptable salt thereof.
22. A method for treating a patient having allergic conjunctivitis, comprising: a compound of formula (I) in an amount effective for treating the allergic conjunctivitis: 【Chemistry 4】 A method comprising administering a pharmaceutically acceptable salt thereof.
23. The method according to claim 22, wherein the amount of the compound of formula (I) or a pharmaceutically acceptable salt thereof that is effective in treating the allergic conjunctivitis is an amount effective in reducing the signs or symptoms of allergic conjunctivitis.
24. The method according to claim 23, wherein the signs or symptoms of allergic conjunctivitis are itchy eyes, redness of the conjunctiva, redness of the ciliary body, redness of the episclera, conjunctival edema, swelling of the eyelids, lacrimation, runny nose, itching of the nose, itching of the ear or palate, or congestion of the nose.
25. Compound of formula (I): 【Transformation 5】 A compound of formula (I) or a pharmaceutically acceptable salt thereof for use in treating a patient having a phosphodiesterase IV (PDEIV)-mediated disease or condition, wherein the use comprises administering to the patient an amount of the compound effective in treating the disease or condition.
26. The compound for use according to claim 25, wherein the phosphodiesterase IV (PDEIV)-mediated disease or condition is an inflammatory disease or condition.
27. The compound for use according to claim 25 or claim 26, wherein the PDEIV-mediated disease or condition is an inflammatory skin disease.
28. The compound for use according to claim 25 or claim 26, wherein the PDEIV-mediated disease or condition is psoriasis, psoriasis vulgaris, atopic dermatitis, contact dermatitis, seborrheic dermatitis, congestive dermatitis, macular scleroderma, Behçet's syndrome, lupus, alopecia, frontal fibrous alopecia, vitiligo, acne, lichen planus, uveitis, nodular prurigo, or discoid lupus erythematosus.
29. The compound for use according to claim 28, wherein the PDEIV-mediated disease or condition is psoriasis.
30. The compound for use according to claim 28, wherein the PDEIV-mediated disease or condition is atopic dermatitis.
31. The compound for use according to claim 28, wherein the PDEIV-mediated disease or condition is contact dermatitis.
32. The compound for use according to claim 25, wherein the PDEIV-mediated disease or condition is psoriatic arthritis, psoriasis vulgaris, atopic dermatitis, or COPD.
33. The compound for use according to claim 25, wherein the phosphodiesterase IV (PDEIV)-mediated disease or condition is an immunodeficiency.
34. The compound for use according to claim 25, wherein the PDEIV-mediated disease or condition is a chronic inflammatory disorder, asthma, rheumatoid arthritis, or Behçet's syndrome.
35. The compound for use according to claim 25, wherein the phosphodiesterase IV (PDEIV)-mediated disease or condition is a cytokine-mediated disease.
36. The compound for use according to claim 25, wherein the phosphodiesterase IV (PDEIV)-mediated disease or condition is a neutrophil-mediated disease.
37. The compound for use according to claim 25, wherein the phosphodiesterase IV (PDEIV)-mediated disease or condition is a neurodegenerative disorder.
38. The compound according to claim 25, wherein the patient is a human.
39. The compound for use according to claim 25, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered as a pharmaceutical composition comprising the compound of formula (I) or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.
40. The compound for use according to claim 25, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered topically, orally, orally, as a suppository, intravenously, parenterally, intraperitoneally, intramuscularly, intrafocally, subarachnoidally, intranasally, or subcutaneously.
41. The compound for use according to claim 25, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered topically.
42. The compound for use according to claim 25, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered orally.
43. A compound of formula (I) for use in inhibiting the release of inflammatory cytokines from mammalian inflammatory cells, 【Transformation 6】 or a pharmaceutically acceptable salt thereof, the compound for use, wherein the use comprises contacting the mammalian inflammatory cells with an amount of the compound effective in inhibiting the release of the inflammatory cytokines from the mammalian inflammatory cells.
44. The compound for use according to claim 43, wherein the inflammatory cytokine is an interleukin (IL) comprising tumor necrosis factor alpha (TNFα), IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-7, IL-8, IL-9, IL-10, IL-11, or IL-12, or an interferon comprising alpha-interferon, beta-interferon, or gamma-interferon.
45. A compound of formula (I) for use in inhibiting the release of inflammatory cytokines from mammalian inflammatory cells, 【Transformation 7】 or a pharmaceutically acceptable salt thereof, wherein the use comprises contacting the inflammatory cells of the mammal with an amount of the compound effective in inhibiting the PDEIV activity in the inflammatory cells of the mammal.
46. A compound of formula (I) for use in treating patients with allergic conjunctivitis; 【Transformation 8】 or a pharmaceutically acceptable salt thereof, the compound for use, wherein the use comprises administering to the patient an amount of the compound effective in treating the allergic conjunctivitis.
47. The compound for use according to claim 46, wherein the amount of the compound of formula (I) or a pharmaceutically acceptable salt thereof that is effective in treating the allergic conjunctivitis is an amount effective in reducing the signs or symptoms of allergic conjunctivitis.
48. The compound for use according to claim 47, wherein the signs or symptoms of allergic conjunctivitis are itchy eyes, redness of the conjunctiva, redness of the ciliary body, redness of the episclera, conjunctival edema, swelling of the eyelids, lacrimation, runny nose, itching of the nose, itching of the ear or palate, or nasal congestion.