| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 1 | 利用小单孢菌将密实菌素羟基化为普伐他汀 | CN200410049355.6 | 2000-06-29 | CN1590555A | 2005-03-09 | A·杰克尔; G·阿姆布鲁斯; E·伊尔克伊; I·霍瓦斯; A·孔亚; I·M·斯扎博; Z·纳吉; G·霍瓦斯; J·默泽斯; I·巴塔; G·索莫格伊; J·萨拉特; S·伯罗斯 |
| 本发明涉及一种通过浸没培养在有氧条件下能够对式(II)化合物进行6β－羟基化的菌株并分离和纯化在生物转化过程中形成的式(I)化合物，由通式(II)的化合物制备式(I)化合物的新微生物方法，其中R代表碱金属或铵离子。所述方法包括以下步骤：在25－32℃下在一种含有可利用的碳源和氮源以及无机盐的营养培养基上培养小单孢菌属菌株，该菌株能够对通式(II)化合物进行6β－羟基化，其中R如上所定义，然后将需要被转化的底物添加到生长的培养物中，然后对底物进行羟基化直至完成生物转化，然后从培养液中分离式(I)化合物，如果需要，纯化该化合物。 | ||||||
| 2 | 具有抗肿瘤活性的大环内酯类 | CN98809559.9 | 1998-08-04 | CN1276791A | 2000-12-13 | L·M·卡内多; F·埃斯普列戈; R·I·费尔南德斯-奇梅诺; J·L·费尔南德斯-普恩特斯; J·佩雷兹-巴兹; F·罗梅罗 |
| 通过培养在保藏号CECT－3333下获得的菌株小单孢菌属菌种ES25—008,可以得到具有结构(Ⅰ)的在此称为IB－96212的化合物,并且可以将其水解得到具有结构(Ⅱ)的IB－96212B。为L－玫瑰糖的糖取代基本身能够衍生化或者该糖能够被替代,无论何种情况均可得到在所述糖位置上具有非L－玫瑰糖基团的IB－96212另外的衍生物。 | ||||||
| 3 | 通过发酵生产法尼基化二苯并二氮杂酮的方法 | CN200780022216.6 | 2007-04-16 | CN101495616A | 2009-07-29 | M·皮拉伊; F·耶博亚 |
| 本发明提供了用于制备包含大量法尼基化二苯并二氮杂酮的浓缩物的可计量方法，所述方法包括使能够产生法尼基化二苯并二氮杂酮的微生物菌株发酵，发酵完成后收获发酵液并且提取发酵液以获得提取物，然后处理提取物以形成浓缩物。所由此生成的浓缩物可用于生产药物化合物的下游方法中。提供了能够以高产率产生法尼基化二苯并二氮杂酮的小单孢菌属以及用于培养微生物的培养基，和用于产生浓缩物的法尼基化二苯并二氮杂酮的发酵条件。 | ||||||
| 4 | 二苯并二氮杂酮类似物，它们的生产方法和它们作为药物的用途 | CN200580040322.8 | 2005-09-26 | CN101065365A | 2007-10-31 | J·B·麦卡尔平; A·H·班斯科塔 |
| 本发明涉及式(I)所示的生物学活性二苯并二氮杂酮类似物，其中R1为直链C1－10烷基，和其中法呢基部分可以具有一个、两个或者三个氢化或者氢化烷氧基化的双键，或者其药学上可接受的盐或者前药，还涉及包含这些化合物的药物组合物、它们的生产方法和它们在制备用于治疗瘤形成症状的药物中的用途。 | ||||||
| 5 | LL-E33288抗肿瘤抗生素的N-酰基衍生物的制备方法 | CN90102100.8 | 1990-04-14 | CN1027267C | 1995-01-04 | 梅·蒂-明·李 |
| 本发明涉及LL-E33288抗肿瘤抗生素的N-酰基衍生物的制备方法，即将抗生素与合适的取代酸酐，酰氯、乙酸和甲酸的混合酸酐或丁二烯酸的单甲酸的酸酐进行酰基反应；或者再进一步用硼氢化钠还原，得到相应的二氢化物。 | ||||||
| 6 | 具有抗肿瘤活性的大环内酯类及其制备方法和用途 | CN98809559.9 | 1998-08-04 | CN1109687C | 2003-05-28 | L·M·卡内多; F·埃斯普列戈; R·I·费尔南德斯-奇梅诺; J·L·费尔南德斯-普恩特斯; J·佩雷兹-巴兹; F·罗梅罗 |
| 通过培养在保藏号CECT-3333下获得的菌株小单孢菌属菌种ES25-008，可以得到具有结构(I)的在此称为IB-96212的化合物，并且可以将其水解得到具有结构(II)的IB-96212B。为L-玫瑰糖的糖取代基本身能够衍生化或者该糖能够被替代，无论何种情况均可得到在所述糖位置上具有非L-玫瑰糖基团的IB-96212另外的衍生物。 | ||||||
| 7 | 利用小单孢菌将密实菌素羟基化为普伐他汀 | CN00811127.8 | 2000-06-29 | CN1399686A | 2003-02-26 | A·杰克尔; G·阿姆布鲁斯; E·伊尔克伊; I·霍瓦斯; A·孔亚; I·M·斯扎博; Z·纳吉; G·霍瓦斯; J·默泽斯; I·巴塔; G·索莫格伊; J·萨拉特; S·伯罗斯 |
| 本发明涉及一种通过浸没培养在有氧条件下能够对式(II)化合物进行6β－羟基化的菌株并分离和纯化在生物转化过程中形成的式(I)化合物，由通式(II)的化合物制备式(I)化合物的新微生物方法，其中R代表碱金属或铵离子。所述方法包括以下步骤：在25－32℃下在一种含有可利用的碳源和氮源以及无机盐的营养培养基上培养小单孢菌属菌株，该菌株能够对通式(II)化合物进行6β－羟基化，其中R如上所定义，然后将需要被转化的底物添加到生长的培养物中，然后对底物进行羟基化直至完成生物转化，然后从培养液中分离式(I)化合物，如果需要，纯化该化合物。 | ||||||
| 8 | LL-E33288抗肿瘤抗生素的N-酰基衍生物 | CN90102100.8 | 1990-04-14 | CN1048390A | 1991-01-09 | 梅·蒂一明·李 |
| 本发明涉及通称为E33288复合物的抗肿瘤和抗生素系列的N-酰基和二氢-N-酰基衍生物。 | ||||||
| 9 | 항종양 활성을 갖는 마크로리드 화합물 | KR1020007001301 | 1998-08-04 | KR1020010022705A | 2001-03-26 | 카네도,리브라다마리아; 로메로,프란시스코; 에스플리에고,페르난도; 페르난데즈-쁘엔트,조스루이스; 페르난데즈-치메노,로사이사벨; 페레즈-바즈,줄리아 |
| 본발명화합물 IB-96212은기탁번호 CECT-3333의마이크로모노스포라 sp. ES25-008 균주를배양하여수득되며, 가수분해되어 IB-96212B 화합물이된다. L-로디노스당 치환체는그 자체가변형될수 있고, 치환될수도있으며, 상기한두 경우에있어서당의위치에 L-로디노스이외의다른작용기가있는 IB-96212의유도체가생성된다. | ||||||
| 10 | 마크롤라이드 항생물질과 그의 제법 및 이들을 함유하는 약학 조성물 | KR1019800004295 | 1980-11-08 | KR1019830004333A | 1983-07-09 | 위이츠제이앨런 |
| 내용없음 | ||||||
| 11 | 항종양 항생물질인 LL-E33288의 N-아실 유도체와 그의 제조 방법 및 그의 사용 | KR1019900005138 | 1990-04-13 | KR100149493B1 | 1998-08-17 | 메이디인-밍리이 |
| 내용없음 | ||||||
| 12 | 마크로라이드 항생물질의 제조방법 | KR1019850009715 | 1985-12-23 | KR1019920009519B1 | 1992-10-17 | 이마이하루미쭈; 스즈끼겐-이찌; 미야자끼시게루; 가도따시게노부 |
| 내용 없음. | ||||||
| 13 | 글루타리마이드계 항생물질 스트렙티미돈을 이용한 식물병방제용 살균제 | KR1020000004873 | 2000-02-01 | KR1020010077219A | 2001-08-17 | 황병국; 김범석; 문석식 |
| PURPOSE: Provided is a sterilizer for preventing botanical diseases which includes streptimidone of glutarimide class antibiotic as effective component so that it shows prevention effect against botanical diseases as actinomicetes-led natural materials. CONSTITUTION: The sterilizer for preventing botanical diseases by streptimidone shown in a formula(1) as glutarimide class antibiotic shows prevention effect against the botanical diseases such as Botrytis cinerea, Cladosporium cucumerinum, Didymella bryoniae, Magnaporthe grisea and Phytophthora capsici. The streptimidone of glutarimide class antibiotic is prepared from Micromonospora coerulea Ao58 strain. | ||||||
| 14 | 신규한 항균제 및 제암제인 LL-E33288 복합체의 슈도아글리콘 및 그의 디히드로 유도체와 이들의 제조 및 정제방법 | KR1019880000867 | 1988-01-29 | KR1019970001533B1 | 1997-02-11 | 메이딘밍리이; 마이클그린스타인; 데이빗드폴레이비더; 아미디오앨릭잰더환티니 |
| 15 | BU-3420T 항종양 항생제 | KR1019890007988 | 1989-06-09 | KR1019910005631B1 | 1991-08-01 | 히로아끼오꾸마; 마사다까고니시; 기요시마쓰모또; 도시까즈오끼; 유따까호시노 |
| 내용 없음. | ||||||
| 16 | Use as production methods and agents of farnesyl benzodiazepinone | JP2006500437 | 2004-01-21 | JP2006515874A | 2006-06-08 | エマヌエル ザゾプロス; ブライアン オー バックマン; マームード ピレー; クリス エム ファーネット; ジェイムス ビー ムカルピン |
| 【化１】
【化２】 本発明は、ＥＣＯ−０４６０１と名付けられた新規のファルネシル化ジベンゾジアゼピノン、その薬学的に許容される塩及び誘導体、並びにかかる化合物を得る方法に関する。 ＥＣＯ−０４６０１化合物を得る方法には、新規のMicromonospora sp.株、すなわち０４６−ＥＣＯ１１の培養による方法や、形質転換した宿主生物における生合成経路遺伝子の発現を伴う方法がある。 本発明は更にMicromonospora sp.０４６−ＥＣＯ１１株に関し、ＥＣＯ−０４６０１並びにその薬学的に許容される塩及び誘導体の医薬組成物としての使用、特に、癌細胞の増殖、細菌細胞の増殖、哺乳類リポキシゲナーゼの阻害剤としての使用、及びＥＣＯ−０４６０１若しくはその薬学的に許容される塩又は誘導体を含む医薬組成物に関する。 最後に、本発明は、新規のポリヌクレオチド配列及びそれによってコードされるタンパク質に関し、これらのポリヌクレオチド配列やタンパク質はＥＣＯ−０４６０１の生合成に関与する。 |
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| 17 | Analogue of ll-e33288 antibiotic substance | JP14992597 | 1997-05-26 | JPH1057093A | 1998-03-03 | LEE MAY D-M; MICHAEL GREENSTEIN; DAVID PAUL RABEDA; AMEDEO ALEXANDER FANTINI |
| PROBLEM TO BE SOLVED: To obtain a novel compound which is useful as an antibacterial and an antitumor agent and comprises a dihydro derivative of analogues of LL-E33288 antibiotic substance, for example, antibiotic substance BBM-1675, FR-900405, PD-114759 or the like. SOLUTION: This novel substance is dihydro-BBM-1675, dihydro-FR-900405, -900406, dihydro-PD-114759, -115024, dihydro-CL-1577A, 1577B, -1577D, -1577E, or CL-1724. These substances are obtained by adding an alkyl iodide to a solution of one of antibiotics; BBM-1675, FR-900405, -900406, PD-114759, -115024, CL-1577A, -1577B, -1577D, -1577E, or CL-1724, cooling the solution to the ice-bath temperature. Then, a solution of sodium borohydride in ethanol is added to the solution followed by decomposing the formed borate complex with acetic acid. Then, the reaction mixture is dissolved in ethyl acetate, hexane is added to cause precipitation and the mixture is further purified by chromatography. | ||||||
| 18 | Production of dienonemacrolide | JP32425996 | 1996-12-04 | JPH09163982A | 1997-06-24 | KURAUDEIO DEII DENOYA; EDOMANDO DABURIYUU HAFUNAA; HAMITSUSHIYU EI AI MATSUKAASAA |
| PROBLEM TO BE SOLVED: To obtain an antibiotic useful as an antimicrobial agent, etc., by mutating a microorganism capable of producing a wild type epoxymacrolide, inactivating epoxydase activity to afford the microorganism capable of producing an olefin macrolide and culturing the microorganism. SOLUTION: A wild type epoxymacrolide-producing microorganism (e.g. Micromonospora rosaria ATCC 55708) is cultured in a medium containing ethyl methanesulfonate(EMS) as a mutagenic agent so as to induce mutation and inactivate epoxydase activity to afford a mutant microorganism (Micromonospora rosaria ATCC55709) capable of producing an olefin macrolide (e.g. dienonemacrolide) and the mutant microorganism is fermented in an aqueous nutrient medium containing a carbon source and a nitrogen source capable of assimilating the mircoorganism to provide repromicin which is an olefin macrolide antibiotic represented by the formula. COPYRIGHT: (C)1997,JPO | ||||||
| 19 | Antitumor antibiotic | JP32179794 | 1994-11-18 | JPH07233193A | 1995-09-05 | TOOMASU TEI DABURA; JIEEMUSU EI MATOSON; KIN SHINGU RAMU; DONARUDO AARU GASUTABUSON; GUREISU EI HESURAA; RONARUDO ERU BERII |
| PURPOSE: To obtain a novel antitumor antibiotic which is obtained by culturing a Micromonospora C39500 strain or a mutant strain capable of producing an antitumor antibiotic in a culture medium, and is effective against the P388 leukemia and the Ma dison 109 lung cancer model in mice. CONSTITUTION: A novel antitumor antibiotic represented by the formula (wherein R 1 is 2-methylpropanoyl, and R 2 2-methylpropanoyl, propanoyl or acetyl; or R 1 is 3-methylbutanoyl, and R 2 is 2-methylpropanoyl; or R 1 is propanoyl and R 2 is acetyl or propanoyl), having an excellent activity against the P388 leukemia and the Madison 109 lung cancer model in mice is produced. The antibiotic is obtained by the fermentation culture of a Micromonospora C39500 strain (ATCC55011) or a mutant strain capable of producing an antitumor antibiotic in an aqueous nutritious culture medium containing assimilable sources of carbon and nitrogen in a submerged aerobic condition, isolating the produced antibiotic from the culture medium, and refining the same. COPYRIGHT: (C)1995,JPO | ||||||
| 20 | Dynemicin c antitumor antibiotic | JP34934691 | 1991-11-05 | JPH04368388A | 1992-12-21 | SAITO KYOICHIRO; MIYAGI TAKEO; YAMAMOTO HARUAKI; ODA NAOMI |
| PURPOSE: To obtain a novel compd. having excellent antibacterial activity, antifungal activity and antitumor activity. CONSTITUTION: A compd. of the formula. For example, Dynemicin C. The compd. of the formula is obtd. by culturing, for example, Micromonospora chermina F1085 (ATCC-55077) or its variant in an aq. nutrient medium contg. an assimilable carbon source or nitrogen source under an intra-liquid aerobic condition preferably at about 28°C for 3 to 4 days and executing isolation and refining with chromatography, etc. A medicinal compsn. is obtd. by combining a carrier and diluent with the effective amt. of the compd. of the formula. COPYRIGHT: (C)1992,JPO | ||||||
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