Antifungal fusacandins, process for their preparation, pharmaceutical compositions containing them and uses thereof 机翻标题: 暂无翻译,请尝试点击翻译按钮。

源语言标题
(IL-116646) פוסאקאנדינים נגד פיטריות, תהליך להכנתם, תרכיבי רוקחות המכילים אותם ושימושים בהם
公开号/公开日
IL116646 A 1996-05-14 [IL-116646]IL116646 B 2001-08-26 [IL-116646] / 1996-05-142001-08-26
申请号/申请日
1996IL-0116646 / 1996-01-01
发明人
;
申请人
ABBOTT LABORATORIES;
主分类号
IPC分类号
A01N-043/16A61K-031/70A61K-031/7042A61K-031/7048A61P-031/04A61P-031/10C07H-015/10C07H-017/04C12P-017/06C12R-001/645
摘要
(IL-116646) A compound of the formula 1969 ז' באלול התשס" א - August 26, 2001 wherein R is hydrogen or -C(O)-R1 wherein R1 is alkenyl, C2-C12-alkyl, aryl, arylalkenyl, arylalkyl, aryl-aryl-, arylalkoxy-aryl,-, aryloxy-aryl, arylalkyl-aryl-, aryl-aryl-aryl- or arylalkoxy-aryl-aryl-, with the proviso that when aryl is naphthyl, alkoxy substituents on naphthyl must have fewer than 8 carbon atoms; or a pharmaceutically acceptable acid, ester or prodrug thereof.
机翻摘要
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地址
代理人
代理机构
;
优先权号
1995US-08370934 1995-01-10 1995US-08548803 1995-12-21
主权利要求
(IL-116646) 1. A compound having the formula OH HO OH wherein R is hydrogen or -C(0)-Ri wherein R1 is alkenyl, C2 -C12 -alkyl, aryl, arylalkenyl, arylalkyl, aryl -aryl-, arylalkoxy-aryl-, aryloxy-aryl, arylalkyl-aryl-, aryl -aryl -aryl- or arylalkoxy-aryl-aryl-, with the proviso that when aryl is naphthyl, alkoxy substutuents on naphthyl must have fewer than 8 carbon atoms; or a pharmaceutically acceptable acid, ester or prodrug thereof. 2. A compound according to Claim 1 wherein R is -C(0)-R1 wherein R1 is alkenyl, aryl, arylalkyl, aryl -phenyl-, arylalkoxy-phenyl-, aryloxy-phenyl, aryl -aryl -phenyl- or arylalkoxy-aryl-phenyl-. 3. A compound according to Claim 1 wherein R is -C(0)-R1 where R1 is C2 - C12 - alkenyl groups containing up to three double bonds, C2 -C12 -alkyl, phenyl, naphthyl, anthracenyl, phenanthrenyl, biphenylenyl, styryl, benzyl, naphthylmethyl, biphenyl, naphthyl-phenyl-, phenyl-naphthyl-, benzyloxy-phenyl-, benzyloxy-naphthyl-, phenoxy-phenyl-, biphenyl -phenyl-, or benzyloxy-biphenyl wherein phenyl or aryl groups are unsubstituted or substituted with one or two groups selected from Ci-05-alkyl, allyloxy, Ci- C8-alkoxy, methylenedioxy, and hydroxy. 4. A compound according to Claim 3 wherein R1 is alkenyl containing from four to twelve carbon atoms and two or three double bonds. 5. A compound according to Claim 3 wherein R1 is alkenyl containing from eight to ten carbon atoms and two or three double bonds. 6. A compound according to Claim 5 wherein R1 is trans, cis-1,3-nonadienyl, trans, cis, trans-1,3,6-nonatrienyl, or trans, trans-1,2-nonadienyl. 7. A compound according to Claim 1 wherein R is -C(0)-Ri wherein R1 is phenanthrenyl, unsubstituted biphenyl or biphenyl substituted with Ci-C3-alkyl or C1-C3- alkoxy. 8. A compound according to Claim 1 wherein R is selected from the group consisting of : CH3 CH 3 Et CH 3 0 and 9. A compound according to Claim 1 wherein R is selected from the group consisting of: Et and 10. A pharmaceutical composition comprising a compound according to Claim 1 in combination with a pharmaceutically acceptable carrier. 11. A pharmaceutical composition comprising a compound according to Claim 2 in combination with a pharmaceutically acceptable carrier. 12. A pharmaceutical composition comprising a compound according to Claim 3 in combination with a pharmaceutically acceptable carrier. 13. A method of treating a fungal infection in a non -human animal in need of such treatment, comprising administering to the non -human animal a therapeutically effective amount of a compound according to claim 1. 14. A method of treating a fungal infection in a non -human animal in need of such treatment, comprising administering to the non -human animal a therapeutically effective amount of a compound according to claim 2. 15. A method of treating a fungal infection in a non -human animal in need of such treatment, comprising administering to the non -human animal a therapeutically effective amount of a compound according to claim 3. 16. A process for preparing a compound according to Claim 1, comprising the steps of (a) culturing a microorganism. having substantially all the characteristics of Fusarium species AB 1900A-1314 under suitable conditions in a fermentation medium containing assimilable sources of carbon and nitrogen; (b) allowing the compound to accumulate in the fermentation medium; and (c) isolating the compound from the fernientation medium. 17. A process according to Claim 16 wherein the microorganism is Fusarium strain NRRL 21252 or a mutant or derivative thereof. 18. Use of a compound according to claim 1 in the preparation of a medicament for the treatment of a fungal infection, substantially as described in the specification. 19. Use of a compound according to claim 2 in the preparation of a medicament for the treatment of a fungal infection, substantially as described in the specification. 20. Use of a compound according to claim 3 in the preparation of a medicament for the treatment of a fungal infection, substantially as described in the specification. 21. A compound according to claim 1 for use as a medicament for the treatment of a fungal infection. 22. A compound according to claim 2 for use as a medicament for the treatment of a fungal infection. 23. A compound according to claim 3 for use as a medicament for the treatment of a fungal infection. 24. The compound according to any one of claims 1-9 and 21-23, substantially as herein described with reference to the examples and the drawings. 25. The pharmaceutical composition according to any one of claims 10-12, substantially as herein described with reference to the examples and the drawings. 26. The method according to any one of claims 13-15, substantially as herein described and with reference to the examples and the drawings. 27. The process according to claim 16 or 17, substantially as herein described with reference to the examples and the drawings. Dr. Shiomo Coh Law 124 Ib Tel Tel. 0'x'5 g: \e2001\8878\23\ insl.doc 04/02/01 fir/op2*
法律状态
(IL-116646) LEGAL DETAILS FOR IL116646  Actual or expected expiration date=2006-09-05    Legal state=DEAD    Status=LAPSED     Event publication date=1996-01-01  Event code=IL/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=IL IL11664696  Application date=1996-01-01  Standardized application number=1996IL-0116646     Event publication date=1996-05-14  Event code=IL/A  Event type=Examination events  Application of patent for invention  Publication country=IL  Publication number=IL116646  Publication stage Code=A  Publication date=1996-05-14  Standardized publication number=IL-116646     Event publication date=2001-08-26  Event code=IL/B  Event indicator=Pos  Event type=Event indicating In Force  Granted patent  Publication country=IL  Publication number=IL116646  Publication stage Code=B  Publication date=2001-08-26  Standardized publication number=IL-116646     Event publication date=2002-05-23  Event code=IL/KB  Event indicator=Pos  Event type=Event indicating In Force  Event type=Restitution or restoration  Patents renewed    Event publication date=2006-09-05  Event code=IL/MM9K  Event indicator=Neg  Event type=Event indicating Not In Force  Patent not in force due to non-payment of renewal fees
专利类型码
AB
国别省市代码
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