Antifungal fusacandins 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
EP0802920 A2 1997-10-29 [EP-802920]EP0802920 B1 2001-10-04 [EP-802920] / 1997-10-292001-10-04
申请号/申请日
1996EP-0903378 / 1996-01-03
发明人
ALDER LISA A;BURRES NEAL S;HOCHLOWSKI JILL E;JACKSON MARIANNA;MCALPINE JAMES B;KLEIN LARRY L;LARTEY PAUL A;YEUNG CLINTON;
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
(EP-802920) Novel antifungal agents having formula (I), wherein R is hydrogen or -C(O)-R1 wherein R1 is alkenyl, C2-C12-alkyl, aryl, arylalkenyl, arylalkyl, aryl-aryl-, arylalkoxy-aryl-, aryloxyl-aryl-, aryl-aryl-aryl- or arylalkoxy-aryl-aryl-, or pharmaceutically acceptable salts, esters or prodrugs thereof, as well as (i) pharmaceutical compositions comprising such compounds, (ii) methods of treatment using such compounds, and (iv) methods and fungal cultures useful in making the same.
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 1996WO-US00225 1996-01-03
主权利要求
(EP-802920)  1. A compound having the formula (see diagramm 1 page 46) 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 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(O)-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(O)-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 C1 -C5 -alkyl, allyloxy, C1 -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(O)-R1  wherein R1  is phenanthrenyl, unsubstituted biphenyl or biphenyl substituted with C1 -C3 -alkyl or C1 -C3 -alkoxy.  8. A compound according to Claim 1 wherein R is selected from the group consisting of: (see diagramm 1 page 47) (see diagramm 2 page 47) (see diagramm 3 page 47) (see diagramm 4 page 47)  (see diagramm 1 page 48) (see diagramm 2 page 48) (see diagramm 3 page 48) and (see diagramm 4 page 48)  9.  A compound according to Claim 1 wherein R is selected from the group consisting of: (see diagramm 5 page 48) (see diagramm 6 page 48)  (see diagramm 1 page 49)  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. Use of a compound according to Claim 1 for manufacturing a medicament for treating a fungal infection in a patient in need of such treatment.  14. Use of a compound according to Claim 2 for manufacturing a medicament for treating a fungal infection in a patient in need of such treatment.  15. Use of a compound according to Claim 3 for manufacturing a medicament for treating a fungal infection in a patient in need of such treatment.  16. A compound according to any of Claims 1-3 for use as a therapeutic agent.  17. A process for preparing a compound according to Claim 1, comprising the steps of   (a) culturing a microorganism having 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 fermentation medium.   18. A process according to Claim 17 wherein the microorganism is Fusarium strain NRRL 21252 or a mutant or derivative thereof.
法律状态
(EP-802920) LEGAL DETAILS FOR EP0802920  Actual or expected expiration date=2016-01-03    Legal state=DEAD    Status=EXPIRED     Event publication date=1996-01-03  Event code=EP/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=EP EP96903378  Application date=1996-01-03  Standardized application number=1996EP-0903378     Event publication date=1997-10-29  Event code=EP/A2  Event type=Examination events  Application published without search report  Publication country=EP  Publication number=EP0802920  Publication stage Code=A2  Publication date=1997-10-29  Standardized publication number=EP-802920     Event publication date=1997-10-29  Event code=EP/AK  Event indicator=Pos  Event type=Designated states  Designated contracting states: Benannte vertragsstaaten AT BE CH DE DK ES FR GB GR IE IT LI LU NL PT SE    Event publication date=1997-10-29  Event code=EP/17P  Event indicator=Pos  Event type=Examination events  Request for examination filed Pruefungsantrag gestellt  Effective date of the event=1997-07-08     Event publication date=1998-12-23  Event code=EP/17Q  Event indicator=Pos  Event type=Examination events  First examination report Erster pruefungsbescheid  Effective date of the event=1998-11-05     Event publication date=2001-10-04  Event code=EP/B1  Event indicator=Pos  Event type=Event indicating In Force  Patent specification  Publication country=EP  Publication number=EP0802920  Publication stage Code=B1  Publication date=2001-10-04  Standardized publication number=EP-802920     Event publication date=2001-10-04  Event code=EP/AK  Event indicator=Pos  Event type=Designated states  Designated contracting states: Benannte vertragsstaaten AT BE CH DE DK ES FR GB GR IE IT LI LU NL PT SE    Event publication date=2002-09-25  Event code=EP/26N  Event indicator=Pos  Event type=No opposition filed  Event type=Event indicating In Force  No opposition filed Kein einspruch eingelegt    Event publication date=2016-01-03  Event code=EP/EEDX  Event indicator=Neg  Event type=Event indicating Not In Force  Patent has expired MEMBER STATE LEGAL DETAILS FOR AT206431  Actual or expected expiration date=2003-01-03    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=AT Corresponding appl: AT96903378  Application date in the designated or member state=1996-01-03   Application number in the designated or member state=1996AT-0903378T Corresponding cc:  Designated or member state=AT Corresponding pat: AT206431  Publication stage code in the designated or member state=T  Publication date in the designated or member state=2001-10-15   Publication number in the designated or member state=ATE206431    Event publication date=2001-10-04  Event code=EP/REF  Event type=Entry into national phase  Corresponds to: Corresponding cc:  Designated or member state=AT     Event publication date=2001-12-11  Event code=EP/PGFP  Event indicator=Pos  Event type=Event indicating In Force 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code=EP/REG  Event code=CH/NV  Event type=Change of name or address  Reference to a national code New agent Neuer vertreter/nouveaux mandataires/nuovi mandatari Corresponding cc:  Designated or member state=CH     Event publication date=2002-03-25  Event code=EP/PGFP  Event indicator=Pos  Event type=Event indicating In Force  Event type=Payment or non-payment notifications  Postgrant: annual fees paid to national office   Annual fees payment date=2002-03-25     Year of payment of annual fees=7  Corresponding cc:  Designated or member state=CH     Event publication date=2003-01-31  Event code=EP/PG25  Event indicator=Neg  Event type=Event indicating Not In Force  Event type=Payment or non-payment notifications  Lapsed in a contracting state announced via postgrant inform. from nat. office to EPO Corresponding cc:  Designated or member state=CH   Effective date of the event=2003-01-31  LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES     Event publication date=2003-09-15  Event code=EP/REG  Event code=CH/PL  Event indicator=Neg  Event type=Event indicating Not In Force  Reference to a national code Patent ceased Loeschung/radiation/radiazion Corresponding cc:  Designated or member state=CH  MEMBER STATE LEGAL DETAILS FOR DE69615657  Actual or expected expiration date=2003-08-01    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=DE Corresponding appl: DE69615657  Application date in the designated or member state=1996-01-03   Application number in the designated or member state=1996DE-6015657 Corresponding cc:  Designated or member state=DE Corresponding pat: DE69615657  Publication stage code in the designated or member state=D1  Publication date in the designated or member state=2001-11-08   Publication number in the designated or member state=DE69615657    Event publication date=2001-11-08  Event code=EP/REF  Event type=Entry into national phase  Corresponds to: Corresponding cc:  Designated or member state=DE     Event publication date=2002-01-31  Event code=EP/PGFP  Event indicator=Pos  Event type=Event indicating In Force  Event type=Payment or non-payment notifications  Postgrant: annual fees paid to national office   Annual fees payment date=2002-01-31     Year of payment of annual fees=7  Corresponding cc:  Designated or member state=DE     Event publication date=2003-08-01  Event code=EP/PG25  Event indicator=Neg  Event type=Event indicating Not In Force  Event type=Payment or non-payment notifications  Lapsed in a contracting state announced via postgrant inform. from nat. office to EPO Corresponding cc:  Designated or member state=DE   Effective date of the event=2003-08-01  LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES  MEMBER STATE LEGAL DETAILS FOR DK802920  Actual or expected expiration date=2003-01-31    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=DK Corresponding appl: DK96903378  Application date in the designated or member state=1996-01-03   Application number in 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In Force  Event type=Payment or non-payment notifications  Lapsed in a contracting state announced via postgrant inform. from nat. office to EPO Corresponding cc:  Designated or member state=DK   Effective date of the event=2003-01-31  LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES     Event publication date=2003-09-08  Event code=EP/REG  Event code=DK/EBP  Event indicator=Neg  Event type=Event indicating Not In Force  Reference to a national code Patent lapsed Ep patentet bortfaldet Corresponding cc:  Designated or member state=DK  MEMBER STATE LEGAL DETAILS FOR ES2164234  Actual or expected expiration date=2003-01-04    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=ES Corresponding appl: ES96903378  Application date in the designated or member state=1996-01-03   Application number in the designated or member state=1996ES-0903378T Corresponding cc:  Designated or member state=ES Corresponding pat: ES2164234  Publication stage code in the designated or 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state=PT   Effective date of the event=2002-01-04  AVAILABILITY OF NATIONAL TRANSLATION     Event publication date=2003-07-31  Event code=EP/PG25  Event indicator=Neg  Event type=Event indicating Not In Force  Event type=Payment or non-payment notifications  Lapsed in a contracting state announced via postgrant inform. from nat. office to EPO Corresponding cc:  Designated or member state=PT   Effective date of the event=2003-07-31  LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES  MEMBER STATE LEGAL DETAILS FOR SE  Actual or expected expiration date=2003-01-04    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=SE     Event publication date=2002-01-07  Event code=EP/PGFP  Event indicator=Pos  Event type=Event indicating In Force  Event type=Payment or non-payment notifications  Postgrant: annual fees paid to national office   Annual fees payment date=2002-01-07     Year of payment of annual fees=7  Corresponding cc:  Designated or member state=SE     Event 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专利类型码
A2B1
国别省市代码
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