Eckol derivatives, methods of synthesis and uses thereof
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
C07D-319/24
C07D-493/04
출원번호
US-0808790
(2017-11-09)
등록번호
US-10106521
(2018-10-23)
발명자
/ 주소
Shin, Hyeon-Cheol
Hwang, Hyejeong
Park, Kwang Yong
Kim, Seong Ho
Lee, Haengwoo
출원인 / 주소
Phloronol, Inc.
대리인 / 주소
Young Basile Hanlon & MacFarlane, P.C.
인용정보
피인용 횟수 :
0인용 특허 :
69
초록▼
Provided herein are eckol derivatives, methods of synthesis thereof and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, Alzheimer's disease, microbial infections,
Provided herein are eckol derivatives, methods of synthesis thereof and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, Alzheimer's disease, microbial infections, obesity, diabetes, cancer or inflammation using the compounds and pharmaceutical compositions disclosed herein.
대표청구항▼
1. A compound of structural Formula (IV): wherein R1 is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, R10C(O)— or R11OC(O)—; R7 is a
1. A compound of structural Formula (IV): wherein R1 is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, R10C(O)— or R11OC(O)—; R7 is alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, R70C(O)— or R71OC(O)—; and R10, R11, R70 and R71 are independently alkyl or aryl. 2. The compound of claim 1, wherein R10, R11, R70 and R71 are independently methyl or phenyl. 3. The compound of claim 1, wherein R1 is hydrogen, —CF3, —CH2Ph, —C(O)CH3, —C(O)Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH and R7 is —CH3, —CF3, —CH2Ph, —C(O)CH3, —C(O)Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 4. The compound of claim 1, wherein R1 is hydrogen and R7 is —CH3, —CF3, —CH2Ph, —C(O)OCH3, —C(O)CH3, —C(O)Ph, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 5. The compound of claim 1, wherein R1 is hydrogen and R7 is —CH3, —CF3, —CH2Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 6. The compound of claim 1, wherein R1 is hydrogen, —CF3, —CH2Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH and R7 is —CH3, —CF3, —CH2Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 7. A method of treating or preventing Alzheimer's disease in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a compound of claim 1. 8. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable vehicle. 9. A compound of structural Formula (VI): wherein R1 is alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, R10C(O)— or R11OC(O)—; and R10 and R11 are independently alkyl or aryl. 10. The compound of claim 9, wherein R10 and R11 are independently methyl or phenyl. 11. The compound of claim 9, wherein R1 is —CH3, —CF3, —CH2Ph, —C(O)CH3, —C(O)Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 12. The compound of claim 9, wherein R1 is —CH3, —CF3, —CH2Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 13. A method of treating or preventing Alzheimer's disease in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a compound of claim 9. 14. A pharmaceutical composition comprising a compound of claim 9 and a pharmaceutically acceptable vehicle. 15. A compound of structural Formula (VII): wherein R1 is (C2-C20) alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, R10C(O)— or R11OC(O)—; and R10 and R11 are independently alkyl or aryl. 16. The compound of claim 15, wherein R10 and R11 are independently methyl or phenyl. 17. The compound of claim 15, wherein R1 is —CH3, —CF3, —CH2Ph, —C(O)CH3, —C(O)Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 18. The compound of claim 15, wherein R1 is —CH3, —CF3, —CH2Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 19. A method of treating or preventing Alzheimer's disease in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a compound of claim 15. 20. A pharmaceutical composition comprising a compound of claim 15 and a pharmaceutically acceptable vehicle. 21. A compound of structural Formula (XI): wherein R1 is alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, R10C(O)— or R11OC(O)—, R90 is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, R100C(O), R101OC(O); and R10, R11, R100 and R101 are independently alkyl or aryl. 22. The compound of claim 21, wherein R10, R11, R100 and R101 are independently methyl or phenyl. 23. The compound of claim 21, wherein R1 is —CH2C(O)(CH2)5OH, —CH2C(O)(CH2)5SH, —CH2C(O)CH2CO2CH3 and R90 is hydrogen. 24. The compound of claim 21, wherein R1 is —CH3, —CF3, —CH2Ph, —C(O)CH3, —C(O)Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH and R90 is hydrogen, —CH3, —CF3, —CH2Ph, —C(O)CH3, —C(O)Ph, —C(O)OCH3, —C(O)OPh, —CH2O CH3 or —CH2C≡CH. 25. The compound of claim 21, wherein R1 is —CH3, —CF3, —CH2Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH and R90 is hydrogen, —CH3, —CF3, —CH2Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 26. A method of treating or preventing Alzheimer's disease in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a compound of claim 21. 27. A pharmaceutical composition comprising a compound of claim 21 and a pharmaceutically acceptable vehicle. 28. A compound of structural Formula (XI): wherein R1 is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, R10C(O)— or R11OC(O)—, R90 is alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, R100C(O), R101OC(O); and R10, R11, R100 and R101 are independently alkyl or aryl. 29. The compound of claim 28, wherein R10 and R11 are independently methyl or phenyl. 30. The compound of claim 28, wherein R1 is hydrogen, —CH3, —CF3, —CH2Ph, —C(O)CH3, —C(O)Ph, —C(O)OCH3, —C(O)OPh, —CH2O CH3 or —CH2C≡CH and R9 is —CH3, —CF3, —CH2Ph, —C(O)CH3, —C(O)Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 31. The compound of claim 28, wherein R1 is hydrogen, —CH3, —CF3, —CH2Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH and R9 is —CH3, —CF3, —CH2Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 32. A method of treating or preventing Alzheimer's disease in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a compound of claim 28. 33. A pharmaceutical composition comprising a compound of claim 28 and a pharmaceutically acceptable vehicle. 34. A compound of structural Formula (VIII): wherein R1 is alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, R10C(O)— or R11OC(O)—; and R10 and R11 are independently alkyl or aryl. 35. The compound of claim 34, wherein R10 and R11 are independently methyl or phenyl. 36. The compound of claim 34, wherein R1 is —CH3, —CF3, —CH2Ph, —C(O)CH3, —C(O)Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 37. The compound of claim 34, wherein R1 is —CH3, —CF3, —CH2Ph, —C(O)OCH3, —C(O)OPh, —CH2OCH3 or —CH2C≡CH. 38. A method of treating or preventing Alzheimer's disease in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a compound of claim 34. 39. A pharmaceutical composition comprising a compound of claim 34 and a pharmaceutically acceptable vehicle.
Yuzhakov Vadim Vladimirovich ; Sherman Faiz Feisal ; Owens Grover David ; Gartstein Vladimir, Apparatus and method for using an intracutaneous microneedle array.
Oh, Jong Eun; Lee, Keon Hyoung; Park, Tae Gwan; Nam, Yoon Sung, Controlled drug delivery system using the conjugation of drug to biodegradable polyester.
Oshlack Benjamin (New York NY) Chasin Mark (Manalapan NJ) Pedi ; Jr. Frank (Yorktown Heights NY), Controlled release formulations coated with aqueous dispersions of acrylic polymers.
Marshall Lucia G. I. (St. Charles MO) Patel Kanaiyalal R. (St. Louis MO) Roufa Dikla G. (St. Louis MO), Controlled release formulations of trophic factors in ganglioside-lipsome vehicle.
Yatvin Milton B. ; Stowell Michael H. B. ; Gallicchio Vincent S. ; Meredith Michael J., Covalent microparticle-drug conjugates for biological targeting.
Mohr Judy M. (Menlo Park CA) Baker Richard W. (Palo Alto CA) Nakaji Lisa A. (San Jose CA), Liquid reservoir transdermal patch for the administration of ketorolac.
Calanchi Massimo,ITX ; Zema Marco,ITX ; Brunetti Gabriele,ITX ; Giorgetti Enzo,ITX, Method for targeted and controlled release of drugs in the intestinal tract and more particularly in the colon.
Santus Giancarlo (Milan ITX) Bilato Ettore (Padua ITX) Lazzarini Gabriele (Pero ITX), Pharmaceutical composition for the controlled release of moguisteine in a liquid suspension.
Le Grazie Cristina (Milan ITX), Pharmaceutical compositions containing 5-methyltetrahydrofolic acid, 5-formyltetrahydrofolic acid and their pharmaceutic.
Venkateshwaran Srinivasan ; Fikstad David ; Ebert Charles D., Pressure sensitive adhesive matrix patches for transdermal delivery of salts of pharmaceutical agents.
Eppstein Deborah A. (Los Altos CA) Fraser-Smith Elizabeth B. (Los Altos CA) Matthews Thomas R. (Los Gatos CA), Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides.
Saikawa, Akira; Igari, Yasutaka; Hata, Yoshio; Yamamoto, Kazumichi, Sustained release compositions, process for producing the same and utilization thereof.
Bodmer David (Klingnau CHX) Fong Jones W. (Parsippany NJ) Kissel Thomas (Staufen DEX) Maulding Hawkins V. (Mendham NJ) Nagele Oskar (Sissach CHX) Pearson Jane E. (Ogendensburg NJ), Sustained release formulations of water soluble peptides.
Unger Evan C. ; Fritz Thomas A. ; Matsunaga Terry ; Ramaswami VaradaRajan ; Yellowhair David ; Wu Guanli, Targeted gas and gaseous precursor-filled liposomes.
Friend David R. ; Ng Steve ; Sarabia Rafael E. ; Weber Thomas P. ; Geoffroy Jean-Marie, Taste-masked microcapsule compositions and methods of manufacture.
Norris James ; Clawson Gary ; Westwater Caroline ; Schofield David ; Schmidt Michael ; Hoel Brian ; Dolan Joseph ; Pan Wei-Hua, Tissue-specific and pathogen-specific toxic agents and ribozymes.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.