A strain of streptomyces avermitilis glycosylates avermectin compounds 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
WO9318779 A1 1993-09-30 [WO9318779] / 1993-09-30
申请号/申请日
1993WO-US02366 / 1993-03-16
发明人
ARISON BYRON H;MACNEIL TANYA;SCHULMAN MARVIN D;MACNEIL DOUGLAS J;
申请人
MERCK SHARP & DOHME;
主分类号
IPC分类号
A01N-043/90A61K-031/70A61K-031/7028A61K-031/7048A61P-033/00C07H-015/26C07H-019/01C12N-001/20C12P-019/58C12P-019/62C12R-001/465
摘要
(WO9318779) Avermectin compounds are glycosylated at the 4',13- Or 14a-positions by adding the avermectin compounds to the fermentation medium of a novel strain of Streptomyces avermitilis.  The 4'-hydroxy, 13-hydroxy and 14a-hydroxy methyl groups of the avermectin compound are glycosylated with a glycosyl moiety, specifically an oleandrose group.  The new strain offers the added advantage of not producing any C5-O-methylation products.  The compounds are potent anthelmintic and antiparasite agents, and compositions for such uses are also disclosed.  U.S patent 3950360 to Aoki e &cir& _t &cir& _ a &cir& _1 &cir& _, discloses milbemycin compounds and European patent application 242052 to Rudd e &cir& _t &cir& _ a &cir& _1 &cir& _ discloses nemedectin compounds with a 25-hydroxy group and a 25-unsaturated alkyl group.
机翻摘要
暂无翻译结果,您可以尝试点击头部的翻译按钮。
地址
代理人
代理机构
;
优先权号
1992US-07855310 1992-03-23 1992US-07855311 1992-03-23
主权利要求
(WO9318779) WHAT IS CLAIMED IS: 1. A biologically pure culture of Streptomyces avermitilis which is an avermectin non-producer which does not methylate at the position C5-hydroxy and which glycosylates at the 41-, 13- or 14a- positions or both the 14a and one of the 4* and 13- positions, of avermectin aglycones, milbemycins or nemadectins or 14a hydroxy derivatives thereof. 2. The culture of Claim'1 which is lacking the DNA which includes the gene for C5-0-methylation and for synthesis of, the avermectin aglycone structure. 3. A biologically pure culture of the microorganism Streptomyces avermitilis MA 6941 or a mutant thereof, which is capable of preparing compounds having the formula.  30 wherein: R^ is present only when the broken line represents a single bond at the 22,23-position and is hydrogen, hydroxy, or hydroximino; R2is alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms or cycloalkyl of 3 to 8 carbon atoms; R3 is hydroxy, methoxy, oxo or acetoxy; and R^ is hydrogen β-hydroxy or n where n is 0 or 1; m is 1 o-r 2; Rg is hydroxy, amino, alkyl of 1 to 8 carbon atoms dialkyl of 1 to 8 carbon atoms or (alkyl of 1 to 8 carbon atoms) (alkanoyl of 1 to 8 carbon atoms)amino; and R5 is hydrogen or hydroxy. and wherein the fermentation of the microorganism is carried out in an aqueous medium of assimilable sources of carbon, nitrogen and inorganic salts and a compound having the formula:  wherein R^, R2, R3, R4and R5are as defined above. 4. A fermentation medium containing assimilable sources of carbon, nitrogen and inorganic salts and a culture of Streptomyces avermitilis MA 6941. 5. A process for the preparation of compounds having the formula:  30 wherein: R^ is present only when the broken line represents a single bond at the 22,23-position and is hydrogen, hydroxy, or hydroximino; R is alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms or cycloalkyl of 3 to 8 carbon atoms; 3 is hydroxy, methoxy, oxo or acetoxy; and R4is hydrogen β-hydroxy or n where n is 0 or 1; m is 1 or 2; R6is hydroxy, amino, alkyl of 1 to 8 carbon atoms dialkyl of 1 to 8 carbon atoms or (alkyl of 1 to 8 carbon atoms) (alkanoyl of 1 to 8 carbon atoms)amino; and R5 is hydrogen or hydroxy. and wherein the fermentation of the microorganism is carried out in an aqueous medium of assimilable sources of carbon, nitrogen and inorganic salts and a compound having the formula:  wherein Rl5R2, R3, R and R5are as defined above, 6. A compound having the formula: where the broken line at the 22,23-position indicates a single or a double bond at the 22,23-position; R^ is present only when the broken line represents a 22,23-position single bond and is hydrogen or hydroxy; R2is alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms or cycloalkyl of 3 to 8 carbon atoms; R3 is hydroxy or methoxy; and R4is hydrogen or β-hydroxy. 7. A composition useful for the treatment of parasitic diseases of animals or parasitic infections of plants or plant crops which comprises an inert carrier and an effective amount of a compound of Claim 8. 8. A method for the treatment of parasitic diseases of animals which comprises administering to an animal an effective amount of a compound of Claim 8. - 9. A method for the treatment of parasitic infections of plants or plant crops which comprises administering to such plants, to the soil in which such plants grow or to the crops of such plants, an effective amount of a compound of Claim 8.
法律状态
(WO9318779) LEGAL DETAILS FOR WO9318779  Actual or expected expiration date=1995-09-23    Legal state=DEAD    Status=LAPSED     Event publication date=1993-03-16  Event code=WO/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=WO WOUS9302366  Application date=1993-03-16  Standardized application number=1993WO-US02366     Event publication date=1993-09-30  Event code=WO/A1  Event type=Examination events  Published application with search report  Publication country=WO  Publication number=WO9318779  Publication stage Code=A1  Publication date=1993-09-30  Standardized publication number=WO9318779     Event publication date=1993-09-30  Event code=WO/AL  Event indicator=Pos  Event type=Designated states  Designated countries for regional patents AT BE CH DE DK ES FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN ML MR SN TD TG    Event publication date=1993-09-30  Event code=WO/AK  Event indicator=Pos  Event type=Designated states  Designated states AU BB BG BR CA CZ FI HU JP KR LK MG MN MW NO NZ PL RO RU SD SK UA    Event publication date=1993-12-09  Event code=WO/DFPE  Event type=Examination events  Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)    Event publication date=1995-09-23  Event code=WO/EETL  Event type=Event indicating Not In Force  PCT Application validity period expired. LEGAL DETAILS FOR DESIGNATED STATE CA  Actual or expected expiration date=1995-11-23    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=CA     Event publication date=1995-11-23  Event code=WO/NENP  Event type=Event indicating Not In Force  Non-entry into the national phase in: Corresponding cc:  Designated or member state=CA  LEGAL DETAILS FOR DESIGNATED STATE DK0637244  Actual or expected expiration date=2003-03-31    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=DK Corresponding appl: DK93907514  Application date in the designated or member state=1993-03-16   Application number in the designated or member state=1993DK-0907514 Corresponding cc:  Designated or member state=DK Corresponding pat: DK0637244  Publication stage code in the designated or member state=T3  Publication date in the designated or member state=2001-01-29   Publication number in the designated or member state=DK-637244T    Event publication date=2001-01-29  Event code=DK/STCHG  Patent Status changed by the national office Corresponding cc:  Designated or member state=DK  LEGAL DETAILS FOR DESIGNATED STATE EP0637244  Actual or expected expiration date=2013-03-16    Legal state=DEAD    Status=EXPIRED   Corresponding cc:  Designated or member state=EP Corresponding appl: EP93907514  Application date in the designated or member state=1993-03-16   Application number in the designated or member state=1993EP-0907514 Corresponding cc:  Designated or member state=EP Corresponding pat: EP0637244  Publication stage code in the designated or member state=A1  Publication date in the designated or member state=1995-02-08   Publication number in the designated or member state=EP-637244    Event publication date=1994-09-02  Event code=WO/WWE  Event indicator=Pos  Event type=Entry into national phase  Wipo information: entry into national phase Corresponding cc:  Designated or member state=EP     Event publication date=1995-02-08  Event code=WO/WWP  Event indicator=Pos  Event type=Examination events  Wipo information: published in national office Corresponding cc:  Designated or member state=EP     Event publication date=2001-01-03  Event code=WO/WWG  Event indicator=Pos  Event type=Event indicating In Force  Wipo information: grant in national office Corresponding cc:  Designated or member state=EP     Event publication date=2002-01-02  Event code=EP/STCHG  Patent Status changed by the national office Corresponding cc:  Designated or member state=EP  LEGAL DETAILS FOR DESIGNATED STATE GR3035187  Actual or expected expiration date=2003-10-02    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=GR Corresponding appl: GR20000402816  Application date in the designated or member state=2001-01-04   Application number in the designated or member state=2000GR-0402816 Corresponding cc:  Designated or member state=GR Corresponding pat: GR3035187  Publication stage code in the designated or member state=T3  Publication date in the designated or member state=2001-04-30   Publication number in the designated or member state=GR3035187    Event publication date=2003-10-02  Event code=GR/STCHG  Patent Status changed by the national office Corresponding cc:  Designated or member state=GR  LEGAL DETAILS FOR DESIGNATED STATE JPH07505280  Actual or expected expiration date=2004-12-21    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=JP Corresponding appl: JP51666293  Application date in the designated or member state=1993-03-16   Application number in the designated or member state=1993JP-0516662 Corresponding cc:  Designated or member state=JP Corresponding pat: JPH07505280  Publication stage code in the designated or member state=A  Publication date in the designated or member state=1995-06-15   Publication number in the designated or member state=JP07505280    Event publication date=2004-12-21  Event code=JP/STCHG  Patent Status changed by the national office Corresponding cc:  Designated or member state=JP
专利类型码
A1
国别省市代码
若您需要申请原文,请登录。

最新评论

暂无评论。

登录后可以发表评论

意见反馈
返回顶部