Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/485
C07D-489/02
A61K-009/00
A61K-009/02
A61K-009/10
A61K-009/14
A61K-009/20
A61K-009/48
A61K-031/472
A61K-041/00
A61K-045/06
A61K-047/26
A61K-047/36
A61K-047/38
C07D-221/28
출원번호
US-0316443
(2014-06-26)
등록번호
US-9527858
(2016-12-27)
발명자
/ 주소
Cantrell, Gary L.
Rajagopalan, Raghavan
Karwa, Amolkumar
Dorshow, Richard B.
출원인 / 주소
Mallinckrodt LLC
인용정보
피인용 횟수 :
0인용 특허 :
46
초록▼
The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class o
The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class of opioid compounds and structurally related opioid derivatives exhibiting anti-VEGF activity for use in therapeutic procedures, including phototherapy. Opioid compounds and structurally related opioid derivatives of the invention may be administered alone or in combination with administration of a phototherapy agent and/or other therapeutic agent.
대표청구항▼
1. A method for treating cancer, the method comprising: administering to a patient in need of treatment an effective amount of a purified (+) enantiomer compound substantially free of a corresponding (−) enantiomer, the (+) enantiomer compound having the formula (FX1): wherein:ring A is X is —OH, —O
1. A method for treating cancer, the method comprising: administering to a patient in need of treatment an effective amount of a purified (+) enantiomer compound substantially free of a corresponding (−) enantiomer, the (+) enantiomer compound having the formula (FX1): wherein:ring A is X is —OH, —OCH3, or C2-C8 alkoxy;Y is —H or —OH;W is —(CR10R11)—, —(C═O)—, —(C═S)—, —(C═CR12R13)—, or —(CR14NR15R16)—;each of R1 and R2 is independently —H, —CH3, —(O−), C1-C10 alkyl, C3-C10 cycloalkyl, C2-C10 alkenyl, C1-C10 haloalkyl, C5-C10 aryl, C5-C10 heteroaryl, C5-C10 alkylaryl, C5-C10 alkylheteroaryl, C5-C10 carbonylalkenylaryl, or C5-C10 carbonylalkenylheteroaryl;each of R3—R5, R9—R16 and R50—R54 is independently —H, —OH, —OCH3, C1-C8 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl, C2-C8 alkoxy, C5-C10 aryl, C5-C10 heteroaryl, C5-C10 alkylaryl, C5-C10 alkylheteroaryl, halo, nitrile, C1-C8 haloalkyl, C1-C10 hydroxyalkyl, or C5-C10 carbonylalkenylheteroaryl; andn is 1, and the nitrogen to which R2 is attached has a positive charge and optionally is associated with an anion. 2. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX11): wherein: A−z is independently an anion;z is independently 1, 2 or 3; andm is independently 0 or 1, wherein when m is 0, A−z is not present. 3. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX15): 4. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX17): 5. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX20): 6. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX22): 7. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX24): 8. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX26): 9. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX28): 10. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX29): 11. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX31) 12. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX33): 13. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX35): 14. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX37): 15. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX40): 16. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX42): 17. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX44): 18. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX46): 19. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX48): 20. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX49). 21. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX51): 22. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX53): 23. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX55): 24. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX57): 25. The method of claim 1 wherein said (+) enantiomer compound has the formula (FX59): 26. The method of claim 1 wherein said (+) enantiomer compound has the formula: 27. The method for treating cancer of claim 1, further comprising administering to said patient a mixture of two or more purified (+) enantiomer compounds each independently having a formula (FX1). 28. The method of claim 1, comprising a method for treating pancreatic cancer. 29. The method of claim 1, comprising a method of suppressing tumor growth or tumor metastasis. 30. The method of claim 1, further comprising administering to said patient one or more chemotherapeutic agents. 31. The method of claim 1, further comprising administering to said patient one or more VEGF inhibitors. 32. The method of claim 1, further comprising administering to said patient 5-fluorouracil, floxuridine, furtulon, capecitabine, gemcitabine, taxol, doxorubicin, cisplatin, thalidomide, paclitaxel, docetaxel or bevacizumab. 33. A method for treating cancer, the method comprising: administering to a patient in need of treatment an effective amount of a purified (+) enantiomer compound substantially free of a corresponding (−) enantiomer, the (+) enantiomer compound having the formula (FX13): wherein: each of R1 and R2 is independently —H, —CH3, —(O−), C1-C10 alkyl, C3-C10 cycloalkyl, C2-C10 alkenyl, C1-C10 haloalkyl, C5-C10 aryl, C5-C10 heteroaryl, C5-C10 alkylaryl, C5-C10 alkylheteroaryl, C5-C10 carbonylalkenylaryl, or C5-C10 carbonylalkenylheteroaryl; andn is 1, and the nitrogen to which R2 is attached has a positive charge and optionally is associated with an anion. 34. The method of claim 33, wherein said (+) enantiomer compound has the formula (FX72): 35. The method of claim 33, wherein said (+) enantiomer compound has the formula (FX74): 36. The method of claim 33, wherein said (+) enantiomer compound has the formula (FX80): 37. The method of claim 33, wherein said (+) enantiomer compound has the formula (FX82): 38. The method of claim 33, wherein said (+) enantiomer compound has the formula (FX84): 39. The method of claim 33, wherein said (+) enantiomer compound has the formula (FX87): 40. The method of claim 33, wherein said (+) enantiomer compound has the formula (FX100): 41. The method for treating cancer of claim 33 further comprising administering to said patient a mixture of two or more purified (+) enantiomer compounds each independently having a formula (FX13). 42. The method of claim 33, comprising a method for treating pancreatic cancer. 43. The method of claim 33, comprising a method of suppressing tumor growth or tumor metastasis. 44. The method of claim 33, further comprising administering to said patient one or more chemotherapeutic agents. 45. The method of claim 33, further comprising administering to said patient one or more VEGF inhibitors. 46. The method of claim 33, further comprising administering to said patient 5-fluorouracil, floxuridine, furtulon, capecitabine, gemcitabine, taxol, doxorubicin, cisplatin, thalidomide, paclitaxel, docetaxel or bevacizumab. 47. A method for treating cancer, the method comprising: administering to a patient in need of treatment an effective amount of a purified (+) enantiomer compound substantially free of a corresponding (−) enantiomer, the (+) enantiomer compound having the formula (FX15): wherein: each of R1 and R2 is independently —H, —CH3, —(O−), C1-C10 alkyl, C3-C10 cycloalkyl, C2-C10 alkenyl, C1-C10 haloalkyl, C5-C10 aryl, C5-C10 heteroaryl, C5-C10 alkylaryl, C5-C10 alkylheteroaryl, C5-C10 carbonylalkenylaryl, or C5-C10 carbonylalkenylheteroaryl; andn is 1, and the nitrogen to which R2 is attached has a positive charge and optionally is associated with an anion. 48. The method of claim 47, wherein said (+) enantiomer compound has the formula (FX92): 49. The method of claim 47, wherein said (+) enantiomer compound has the formula (FX95): 50. The method of claim 47, wherein said (+) enantiomer compound has the formula (FX106): 51. The method for treating cancer of claim 47, further comprising administering to said patient a mixture of two or more purified (+) enantiomer compounds each independently having a formula (FX15). 52. The method of claim 47, comprising a method for treating pancreatic cancer. 53. The method of claim 47, comprising a method of suppressing tumor growth or tumor metastasis. 54. The method of claim 47, further comprising administering to said patient one or more chemotherapeutic agents. 55. The method of claim 47, further comprising administering to said patient one or more VEGF inhibitors. 56. The method of claim 47, further comprising administering to said patient 5-fluorouracil, floxuridine, furtulon, capecitabine, gemcitabine, taxol, doxorubicin, cisplatin, thalidomide, paclitaxel, docetaxel or bevacizumab.
Cantrell, Gary L.; Rajagopalan, Raghavan; Berberich, David W.; Karwa, Amolkumar; Dorshow, Richard B., Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers.
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