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21. 发明授权

US5670364A A83543 compounds and process for production thereof 失效
标题翻译： A83543化合物及其制备方法
公开(公告)号：US5670364A
公开(公告)日：1997-09-23
申请号：US474026
申请日：1995-06-07
申请人： Jon S. Mynderse , James A. Mabe , Jan R. Turner , Mary L. B. Huber , Mary C. Broughton , Walter M. Nakatsukasa , Lawrence Creemer , Herbert A. Kirst , James W. Martin
发明人： Jon S. Mynderse , James A. Mabe , Jan R. Turner , Mary L. B. Huber , Mary C. Broughton , Walter M. Nakatsukasa , Lawrence Creemer , Herbert A. Kirst , James W. Martin
IPC分类号： A01N43/22 , C07H15/20 , C07H17/08 , C12P19/62 , C12N1/20 , A61K31/71 , C07H17/04
CPC分类号： C07H17/08 , A01N43/22 , C12P19/62 , C12R1/01 , Y10S424/08 , Y10S424/10 , Y10S435/822
摘要： New A83543 components, including fermentation products A83543K, A835430, A83543P, A83543U, A83543V, A83543W and A83543Y and N-demethyl derivatives, and salts thereof, are useful for the control of insects and mites. The pseudoaglycones of the new A83543 components are useful for the preparation of A83543 components. Methods are provided for making the new A83543 components by culturing of Saccharopolyspora spinosa NRRL 18395, NRRL 18537, NRRL 18538, or NRRL 18539, or NRRL 18743 or NRRL 18719 or NRRL 18823 in suitable culture medium. Insecticidal and ectoparasiticidal compositions containing new A83543 components are also provided.
摘要翻译：包括发酵产物A83543K，A835430，A83543P，A83543U，A83543V，A83543W和A83543Y和N-甲基衍生物及其盐的新A83543组分可用于防治昆虫和螨虫。新的A83543组分的假脂肪酸可用于制备A83543组分。提供了通过在合适的培养基中培养多孢子虫NRRL 18395，NRRL 18537，NRRL 18538或NRRL 18539或NRRL 18743或NRRL 18719或NRRL 18823来制备新的A83543成分的方法。还提供了含有新A83543组分的杀虫剂和灭寄生组合物。

22. 发明授权

US5229362A Antibiotic A10255 complex and factors, and process and production therefor 失效
标题翻译：抗生素A10255复合物及其因素及其制备及生产
公开(公告)号：US5229362A
公开(公告)日：1993-07-20
申请号：US732347
申请日：1991-07-17
申请人： Herbert A. Kirst , Karl H. Michel
发明人： Herbert A. Kirst , Karl H. Michel
IPC分类号： C12P1/06 , C12P21/04
CPC分类号： C12P1/06 , Y10S435/822
摘要： Newly-discovered antibiotic A10255 factors B, C, E, F, G, H, and J are produced by submerged aerobic fermentation of Streptomyces gardneri NRRL 15537 and NRRL 18260 or an A10255-producing variant or mutant thereof. The antibiotics are active against a wide variety of pathogenic bacteria, and also enhance feed-utilization efficiency in chickens, weanling pigs, cattle and sheep. The antibiotics can also be used to detect the thiostrepton-resistance gene in Streptomyces species.
摘要翻译：新发现的抗生素A10255因子B，C，E，F，G，H和J通过Streptomyces gardneri NRRL 15537和NRRL 18260或其产生A10255的变体或突变体的浸没需氧发酵产生。抗生素对各种致病菌具有活性，也可以提高鸡，断奶仔猪，牛，羊的饲料利用效率。抗生素也可用于检测链霉菌属中的硫链丝菌素抗性基因。

23. 发明授权

US5202242A A83543 compounds and processes for production thereof 失效
标题翻译： A83543化合物及其制备方法
公开(公告)号：US5202242A
公开(公告)日：1993-04-13
申请号：US790287
申请日：1991-11-08
申请人： Jon S. Mynderse , James W. Martin , Jan R. Turner , Lawrence C. Creemer , Herbert A. Kirst , Mary C. Broughton , Mary L. B. Huber
发明人： Jon S. Mynderse , James W. Martin , Jan R. Turner , Lawrence C. Creemer , Herbert A. Kirst , Mary C. Broughton , Mary L. B. Huber
IPC分类号： A01N43/22 , C07D313/00 , C07H17/08 , C12N1/20 , C12P1/06 , C12P19/62
CPC分类号： C07H17/08 , A01N43/22 , C07D313/00 , C12N1/20 , C12P1/06 , C12P19/62 , Y10S435/822
摘要： New fermentation products A83543L, A83543M, and A83543N, N-demethyl derivatives thereof, and salts thereof, are useful for the control of insects. A83543PsaL1 is useful for the preparation of A83543 components. Methods for making A83543J, A83543L, A83543M, and A83543N by culture of Saccharopolyspora spinosa NRRL 18719 or NRRL 18720 are provided. Insecticidal and ectoparasiticidal compositions containing A83543L, A83543M, A83543N, and N-demethyl derivatives thereof are also provided.
摘要翻译：新发酵产品A83543L，A83543M和A83543N，其N-去甲基衍生物及其盐可用于防治昆虫。 A83543PsaL1可用于制备A83543组分。提供了通过培养酿酒孢子菌NRRL 18719或NRRL 18720制备A83543J，A83543L，A83543M和A83543N的方法。还提供了含有A83543L，A83543M，A83543N和N-去甲基衍生物的杀虫剂和灭寄生组合物。

24. 发明授权

US4920103A Modifications of mycinose and 3-O-demethylmycinose in tylosin-type macrolides 失效
标题翻译：泰乐菌素大环内酯中的霉菌素和3-O-脱甲基霉素的修饰
公开(公告)号：US4920103A
公开(公告)日：1990-04-24
申请号：US912891
申请日：1986-09-29
申请人： Herbert A. Kirst , James P. Leeds
发明人： Herbert A. Kirst , James P. Leeds
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08
摘要： New 4'"-O-modified-20-modified tylosin and 4"-O-modified-20-modified-desmycosin and 4'-deoxydesmycosin derivatives of formula 1 have significant oral antibacterial activity. Compositions containing and methods of using these compounds are also provided.
摘要翻译：式1的新的4'''O-修饰的泰乐菌素和4“-O-修饰的20-修饰的脱沙霉素和4'-脱氧霉菌素衍生物具有显着的口服抗菌活性。还提供了组合物和使用这些化合物的方法。

25. 发明授权

US4396613A 23-Ester derivatives of DMT and method of using same 失效
标题翻译： DMT的23-酯衍生物及其使用方法
公开(公告)号：US4396613A
公开(公告)日：1983-08-02
申请号：US330294
申请日：1981-12-14
申请人： Herbert A. Kirst
发明人： Herbert A. Kirst
IPC分类号： C07H17/08 , A61K31/71
CPC分类号： C07H17/08
摘要： 23-Ester derivatives of demycinosyltylosin (DMT) of the formula: ##STR1## wherein R is selected from hydrogen, optionally substituted C.sub.1 -C.sub.5 -alkanoyl or optionally substituted benzoyl, phenylacetyl, or phenylpropionyl; and R.sup.1 is an acyl group selected from: ##STR2## p is 0 or 1; m and n are integers from 0 to 4; R.sup.2 is hydrogen, halo, C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, phenyl, C.sub.5 -C.sub.8 -cycloalkenyl, naphthyl, indenyl, tetralinyl, decalinyl, adamantyl, cinnoxacinyl, a monocyclic heterocyclic ring system comprising 3 to 8 atoms or a bicyclic heterocyclic ring system comprising 6 to 11 atoms, provided that at least 1 atom of the ring system is carbon and at least 1 atom of the ring system is a heteroatom selected from O, N, and S; and wherein R.sup.2 and the connecting alkyl groups --(CH.sub.2).sub.m -- and --(CH.sub.2).sub.n -- are optionally substituted by one or two halo, methyl, ethyl, methoxy, amino, N-protected-amino, methylamino, dimethylamino, nitro, acetoxy, acetamido, azido, carbomethoxy, carboxamido, cyano, or hydroxyl groups, provided that, if the substituent is other than halo or alkyl, there can be no more than one substituent on any connecting --CH.sub.2 -- group; X is O, S, --NH--, --N(CH.sub.3)--, --C.tbd.C--, --CH.dbd.CH--, --C(CH.sub.3).dbd.CH--, --CH.dbd.C(CH.sub.3)-- or --C(CH.sub.3).dbd.C(CH.sub.3)--; R.sup.3 and R.sup.4 are C.sub.1 -C.sub.5 -alkyl or optionally substituted phenyl or benzyl; and salts thereof are useful antibiotics or intermediates to antibiotics.
摘要翻译：式（1）所示的霉菌霉素（DMT）的23-酯衍生物：其中R选自氢，任选取代的C 1 -C 5 - 烷酰基或任选取代的苯甲酰基，苯乙酰基或苯基丙酰基; 并且R 1是选自以下的酰基：p = 0或1; m和n是0至4的整数; R2是氢，卤素，C1-C4-烷基，C3-C8-环烷基，苯基，C5-C8-环烯基，萘基，茚基，四氢萘基，十氢萘基，金刚烷基，噌啉酰基，包含3-8个原子的单环杂环体系或包含6至11个原子的双环杂环体系，条件是至少1个环系是碳原子，至少1个环系是选自O，N和S的杂原子; 并且其中R 2和连接的烷基 - （CH 2）m - 和 - （CH 2）n任选被一个或两个卤素，甲基，乙基，甲氧基，氨基，N-保护的 - 氨基，甲基氨基，二甲基氨基，硝基，乙酰氧基，乙酰氨基，叠氮基，甲酯基，甲酰胺基，氰基或羟基，条件是如果取代基不是卤素或烷基，则在任何连接的-CH 2 - 基上可以不多于一个取代基; X是O，S，-NH-，-N（CH 3） - ， - C 3BOND C - ， - CH = CH-，-C（CH 3）= CH-，-CH = C（CH 3） CH3）= C（CH3） - ; R3和R4是C1-C5-烷基或任选取代的苯基或苄基; 其盐是有用的抗生素或抗生素的中间体。

26. 发明授权

US4357325A Methods of controlling Pasteurella infections 失效
标题翻译：控制巴氏杆菌感染的方法
公开(公告)号：US4357325A
公开(公告)日：1982-11-02
申请号：US255576
申请日：1981-04-20
申请人： Earl E. Ose , Herbert A. Kirst
发明人： Earl E. Ose , Herbert A. Kirst
IPC分类号： A61K20060101 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08 , C12P19/62 , A61K31/71 , C07H17/04
CPC分类号： C07H17/08 , C12P19/62 , C12R1/54
摘要： Methods of controlling Pasteurella infections are provided which comprise administering to an infected or susceptible warm-blooded aninal an effective amount of a composition comprising (1) a suitable pharmaceutical vehicle and (2) a compound selected from the group consisting of desmycosin, lactenocin, cirramycin A.sub.1, 23-deoxy-5-0-mycaminosyltylonolide, antibiotic M-4365 G.sub.2, 9-dihydrodesmycosin, 9-dihydrolactenocin, 20-dihydrodesmycosin, 20-dihydrolactenocin, rosaramicin, and the pharmaceutically acceptable acid addition salts of these compounds.
摘要翻译：提供了控制巴斯德氏菌感染的方法，其包括向感染的或易感染的温血的阴道施用有效量的组合物，所述组合物包含（1）合适的药物载体和（2）选自脱霉霉素，乳内酯，西拉霉素 A1，23-脱氧-5-0-碳霉糖基太乐内酯，抗生素M-4365G2，9-二氢去甲肌氨酸，9-二氢化己内酰素，20-二氢二十二碳烯酸，20-二氢化己内酰素，rosaramicin，以及这些化合物的药学上可接受的酸加成盐。

27. 发明授权

US4341770A Method of controlling ureaplasma infections 失效
标题翻译：控制脲酶体感染的方法
公开(公告)号：US4341770A
公开(公告)日：1982-07-27
申请号：US255575
申请日：1981-04-20
申请人： Earl E. Ose , Herbert A. Kirst
发明人： Earl E. Ose , Herbert A. Kirst
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P33/02 , C07H17/08 , C12P19/62 , A61K31/71
CPC分类号： C07H17/08 , C12P19/62 , C12R1/54
摘要： Method of controlling Ureaplasma infections which comprises administering to an infected or susceptible warm-blooded animal an effective amount of 5-0-mycaminosyl tylonolide or a pharmaceutically acceptable acid addition salt thereof.
摘要翻译：控制解索拉霉菌感染的方法，其包括向受感染的或易感染的温血动物施用有效量的5-0-碳霉糖基太乐内酯或其药学上可接受的酸加成盐。

28. 发明授权

US4304856A Process for producing 20-dihydro-20-deoxy-23-demycinosyltylosin 失效
标题翻译：制备20-二氢-20-脱氧-23-脱霉霉素的方法
公开(公告)号：US4304856A
公开(公告)日：1981-12-08
申请号：US205539
申请日：1980-11-10
申请人： Richard H. Baltz , Herbert A. Kirst , Gene M. Wild , Eugene T. Seno
发明人： Richard H. Baltz , Herbert A. Kirst , Gene M. Wild , Eugene T. Seno
IPC分类号： C12P13/00 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08 , C12N1/20 , C12P19/62 , C12R1/465 , C12R1/54
CPC分类号： C07H17/08 , C12P19/62 , C12R1/54 , Y10S435/896
摘要： 20-Dihydro-20-deoxy-23-demycinosyltylosin (DH-DO-DMT), 20-dihydro-20-deoxy-5-O-mycaminosyltylonolide (DH-DO-OMT), specified acyl ester derivatives, and their acid addition salts are useful intermediates and antibacterial agents. Methods of preparing DH-DO-DMT and DH-DO-OMT by fermentation of Streptomyces fradiae and the microorganism S. fradiae ATCC 31733 are included.
摘要翻译：（DH-DO-DMT），20-二氢-20-脱氧-5-O-碳霉糖基三奈醇（DH-DO-OMT），特定酰基酯衍生物及其酸加成盐是有用的中间体和抗菌剂。包括通过发酵Streptomyces fradiae和微生物S.fradiae ATCC 31733制备DH-DO-DMT和DH-DO-OMT的方法。

29. 发明授权

US5106961A Erythromycin ring-contracted derivatives 失效
标题翻译：红霉素环收缩衍生物
公开(公告)号：US5106961A
公开(公告)日：1992-04-21
申请号：US307556
申请日：1989-02-07
申请人： Herbert A. Kirst , Julie A. Wind
发明人： Herbert A. Kirst , Julie A. Wind
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08
摘要： Novel 12-membered lactone and 11-membered lactone derivatives of erythromycin, having antimicrobial activity against certain Gram-positive pathogens such as Steptococcus pyogenes and Gram-negative cocci such as Haemophilus influenzae, and useful as intermediates to other macrolide derivatives, are disclosed.
摘要翻译：公开了具有抗某些革兰氏阳性病原体如化脓性致瘟病菌和革兰氏阴性球菌如流感嗜血杆菌的抗微生物活性的红霉素的新型12-元内酯和11-元内酯衍生物，并且可用作其它大环内酯衍生物的中间体。

30. 发明授权

US4487923A Method of preparing 23-monoesters of OMT and DMT 失效
标题翻译：制备OMT和DMT的23-单酯的方法
公开(公告)号：US4487923A
公开(公告)日：1984-12-11
申请号：US475271
申请日：1983-03-14
申请人： Herbert A. Kirst , John E. Toth
发明人： Herbert A. Kirst , John E. Toth
IPC分类号： C07H17/08 , C07H1/00
CPC分类号： C07H17/08
摘要： An improved method of preparing 23-monoester derivatives of 5-O-mycaminosyl tylonolide (OMT) and demycinosyltylosin (DMT) is provided. This method comprises esterifying the antibiotic with an acylating agent in the presence of an external base, such as pyridine or 2,4,6-collidine, until acylation of the 23-hydroxyl group is substantially complete, and separating the 23-monoester derivative. 23-Monoester derivatives of OMT and DMT are useful antibiotics and/or intermediates to antibiotics.
摘要翻译：提供了一种改进的制备5-O-碳霉糖基太乐内酯（OMT）和脱霉素基毒素（DMT）的23-单酯衍生物的方法。该方法包括在外部碱如吡啶或2,4,6-可力丁的存在下用酰化剂酯化抗生素，直到23-羟基的酰化基本上完成，并分离出23-单酯衍生物。 OMT和DMT的23-单酯衍生物是有用的抗生素和/或抗生素的中间体。

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