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公开(公告)号：US07101872B2
公开(公告)日：2006-09-05
申请号：US10762107
申请日：2004-01-21
IPC分类号： C07D243/10 , A61K31/55
CPC分类号： C12N9/93 , A61K38/00 , C07D243/38 , C07D405/06 , C07D405/14 , C12N9/0004 , C12N9/10 , C12N9/12 , C12N9/14 , C12N9/88 , C12N9/90 , C12N15/52 , C12P17/10 , C12R1/29 , Y02A50/473
摘要： This invention relates to a novel farnesylated dibenzodiazepinone, named ECO-04601, its pharmaceutically acceptable salts and derivatives, and to methods for obtaining such compounds. One method of obtaining the ECO-04601 compound is by cultivation of a novel strain of Micromonospora sp., 046-ECO11; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to Micromonospora sp. strain 046-ECO11, to the use of ECO-04601 and its pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of cancer cell growth, bacterial cell growth, mammalian lipoxygenase, and to pharmaceutical compositions comprising ECO-04601 or a pharmaceutically acceptable salt or derivative thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of ECO-04601.
摘要翻译： 本发明涉及名为ECO-04601的新型法呢基化二苯并二氮杂酮，其药学上可接受的盐和衍生物，以及获得这些化合物的方法。 获得ECO-04601化合物的一种方法是通过培养一种新型的小单孢菌属菌株046-ECO11; 另一种方法涉及在转化的宿主细胞中表达生物合成途径基因。 本发明还涉及小单孢菌属 应用046-ECO11，使用ECO-04601及其药学上可接受的盐和衍生物作为药物，特别是其作为癌细胞生长抑制剂，细菌细胞生长，哺乳动物脂氧合酶的用途，以及包含ECO-04601或 其药学上可接受的盐或衍生物。 最后，本发明涉及参与ECO-04601的生物合成的新型多核苷酸序列及其编码的蛋白质。
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公开(公告)号：US6004787A
公开(公告)日：1999-12-21
申请号：US439009
申请日：1995-05-11
申请人： Leonard Katz , Stefano Donadio , James B. McAlpine
发明人： Leonard Katz , Stefano Donadio , James B. McAlpine
摘要： A method to produce novel polyketide structures by designing and introducing specified changes in the DNA governing the synthesis of the polyketide is disclosed. The biosynthesis of specific polyketide analogs is accomplished by genetic manipulation of a polyketide-producing microorganism by isolating a polyketide biosynthetic gene-containing DNA sequence, identifying enzymatic activities associated within the DNA sequence, introducing one or more specified changes into the DNA sequence which codes for one of the enzymatic activities which results in an altered DNA sequence, introducing the altered DNA sequence into the polyketide-producing microorganism to replace the original sequence, growing a culture of the altered microorganism under conditions suitable for the formation of the specific polyketide analog, and isolating the specific polyketide analog from the culture. The method is most useful when the segment of the chromosome modified is involved in an enzymatic activity associated with polyketide biosynthesis, particularly for manipulating polyketide synthase genes from Saccarharopolyspora or Streptomyces.
摘要翻译： 公开了一种通过设计和引入控制聚酮化合物合成的DNA的特定变化产生新型聚酮化合物结构的方法。 特定聚酮化合物类似物的生物合成是通过分离含聚酮化合物生物合成基因的DNA序列，鉴定DNA序列内相关的酶活性，将一个或多个特定变化导入DNA序列的遗传操作来实现的， 导致改变的DNA序列的酶活性之一，将改变的DNA序列引入聚酮化合物生产微生物中以替代原始序列，在适于形成特定聚酮化合物类似物的条件下培养改变的微生物的培养物;以及 从培养物中分离特定的聚酮化合物类似物。 当染色体修饰的片段参与与聚酮化合物生物合成相关的酶活性，特别是用于操作来自蛔虫多孢菌或链霉菌的聚酮化合物合酶基因时，该方法是最有用的。
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公开(公告)号：US5585251A
公开(公告)日：1996-12-17
申请号：US370934
申请日：1995-01-10
摘要： Novel antifungal agents having the formula: ##STR1## wherein R is hydrogen or a radical of the formula ##STR2## and pharmaceutically acceptable 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.
摘要翻译： 具有下式的新颖的抗真菌剂：其中R是氢或下式的基团及其药学上可接受的前药，以及（i）包含这些化合物的药物组合物，（ii）使用这些化合物的治疗方法 ，和（iv）有用的方法和真菌培养物。
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公开(公告)号：US5530020A
公开(公告)日：1996-06-25
申请号：US317978
申请日：1994-10-04
IPC分类号： A61K31/335 , A61K31/337 , A61K31/558 , A61P3/06 , A61P35/00 , C07D20060101 , C07D305/14 , C07D493/06
CPC分类号： C07D493/06 , C07D305/14
摘要： Compounds having the formula ##STR1## wherein --OR.sup.1 comprises the C-13 side-chain of taxol and R.sup.3 comprises hydrogen, as well as a method for the preparation thereof.
摘要翻译： 具有式“IMAGE”的化合物，其中-OR1包含紫杉醇的C-13侧链，R 3包含氢，以及其制备方法。
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公开(公告)号：US4418193A
公开(公告)日：1983-11-29
申请号：US366800
申请日：1982-04-09
IPC分类号： C07H15/224 , C07H15/22
CPC分类号： C07H15/224 , Y02P20/55
摘要： An improved method of producing 2-epi-fortimicin A directly from fortimicin A by protecting the amine functions of fortimicin A, converting the N-protected fortimicin A to an intermediate of the formula: ##STR1## wherein L is a leaving group and Z is an amine-protecting group, reacting the intermediate (I) with a loweralkyl metal halide in N,N-dimethylformamide to form N-protected-2-epi-fortimicin A, and then hydrogenating the N-protected-2-epi-fortimicin A to obtain 2-epi-fortimicin A.
摘要翻译： 通过保护苦丁霉素A的胺官能团，将N-保护的fortimicin A转化为下式的中间体，其中L是离去基团，其中L是离去基团 并且Z是胺保护基团，使中间体（I）与N，N-二甲基甲酰胺中的低级烷基金属卤化物反应，形成N-保护的2-表 - 敌霉素A，然后将N-保护的2-表面 - 有益霉素A获得2-epi-fortimicin A.
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公开(公告)号：US4189569A
公开(公告)日：1980-02-19
申请号：US922134
申请日：1978-07-05
IPC分类号： C07H15/236 , C12P19/48 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234 , C12P19/485
摘要： Described are novel derivatives of seldomycin factor 5 (XK-88-5) and particularly 3'-Epi-seldomycin factor 5, which exhibit improved activity against gram-positive and gram-negative bacteria resistant to aminoglycoside antibiotics, and a method of preparing them.
摘要翻译： 描述了对青霉素因子5（XK-88-5）特别是3-Epi-seldomycin因子5的新型衍生物，其对抗氨基糖苷类抗生素的革兰氏阳性和革兰氏阴性菌具有改善的活性，以及制备它们的方法 。
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7.发明授权Dibenzodiazepinone analogues, processes for their production and their use as pharmaceuticals 失效二苯并二氮杂酮类似物，其制备方法及其作为药物的用途公开(公告)号：US07655646B2
公开(公告)日：2010-02-02
申请号：US11962855
申请日：2007-12-21
IPC分类号： C07D243/10 , A61K31/55
CPC分类号： C07D243/38 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/14
摘要： The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions.
摘要翻译： 本发明涉及由式I表示的生物活性二苯并二氮杂酮类似物，其制备方法，包含它们的药物组合物和治疗肿瘤病症的方法。
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公开(公告)号：US20090069396A1
公开(公告)日：2009-03-12
申请号：US11934125
申请日：2007-11-02
IPC分类号： A61K31/422 , C07D263/02 , A61P35/00
CPC分类号： C12R1/60 , C07D263/32 , C07D413/12 , C12P17/14
摘要： This invention relates to novel biologically active polyene oxazoles, their pharmaceutically acceptable salts and derivatives, and to methods of obtaining them. One method for obtaining the compounds is by cultivation of Streptomyces sparsogenes NRRL 2940 or a mutant or variant thereof.
摘要翻译： 本发明涉及新的生物活性多烯恶唑，其药学上可接受的盐和衍生物，以及获得它们的方法。 用于获得化合物的一种方法是通过培养链霉菌NRRL 2940或其突变体或变体。
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公开(公告)号：US06307070B1
公开(公告)日：2001-10-23
申请号：US09122257
申请日：1998-07-24
申请人： Wai-Lam Alex Chu , Flemming R. Jensen , Thomas B. Jensen , James B. McAlpine , Birgitte Søkilde , Alexandra M. SantAna-Sørensen , Sunil Ratnayake , Jack B. Jiang , Catharine Noble , Angela M. Stafford
发明人： Wai-Lam Alex Chu , Flemming R. Jensen , Thomas B. Jensen , James B. McAlpine , Birgitte Søkilde , Alexandra M. SantAna-Sørensen , Sunil Ratnayake , Jack B. Jiang , Catharine Noble , Angela M. Stafford
IPC分类号： C07D30783
CPC分类号： C07D307/82 , A61K31/343 , C07D307/83
摘要： A method for treating a fungal infection is disclosed. The method includes administering to a patient a pharmaceutical composition containing a compound of formula (IA): where each R is independently H, OH, Br, Cl, I, amino, thiol, nitro, C1-4 alkoxy, C1-4 alkenyloxy, C2-6 alkoxyalkyleneoxy, C1-4 alkylthio, C3-18 alkyl, or C3-18 alkenyl; or two adjacent R's, taken together, are a C2-18 bivalent moiety containing at least one oxgen atom, substituted or disubstituted with A or B or both, A being H, OH, Br, Cl, I, amino, or thiol, and B being H, C1-10 alkyl, C2-18 alkenyl, or C6-18 aryl; provided at least two Rs are not H; X is C4-10 alkyl, C4-20 alkenyl, or a C4-20 single, C6-20 bridged, or C6-20 fused ring moiety containing cycloalkyl, cycloalkenyl, aryl, heterocycle, or heteroaryl, where X is substituted with H, OH, Cl, Br, I, amino, cyano, nitro, alkyl, alkoxy, alkenyl, or alkenyloxy; provided that if X is a heteroaryl or heterocyclic moiety where two Rs are each OH and meta to each other, then the remaining R is H and ortho to each of the two hydroxyls, and Y and Z are each O and a ring atom of X is linked directly to the sp2 carbon atom adjacent to X, then substituted with H, OH, Cl, Br, I, amino, cyano, alkyl, alkoxy, alkenyl, or alkenyloxy; and each of Y and Z is independently selected from O, S, and NH; or a pharmaceutically acceptable salt or ester thereof.
摘要翻译： 公开了一种治疗真菌感染的方法。 该方法包括向患者施用含有式（IA）化合物的药物组合物：其中每个R独立地为H，OH，Br，Cl，I，氨基，硫醇，硝基，C 1-4烷氧基，C 1-4链烯氧基， C 2-6烷氧基亚烷基氧基，C 1-4烷硫基，C 3-8烷基或C 3-8烯基; 或两个相邻的R一起是含有至少一个被A或B或两者取代或二取代的氧原子的C2-18二价部分，A是H，OH，Br，Cl，I，氨基或硫醇，以及 B是H，C 1-10烷基，C 2-8烯基或C 6-18芳基; 提供至少两个R不是H; X是C 4-10烷基，C 4-20链烯基，或含有环烷基，环烯基，芳基，杂环或碳原子的C 4-20单-C6-20桥环或C6-20稠环部分 杂芳基，其中X被H，OH，Cl，Br，I，氨基，氰基，硝基，烷基，烷氧基，烯基或烯氧基取代; 条件是如果X是杂芳基或杂环部分，其中两个R 5各自为OH并且彼此相互间隔，则剩余的R是H和两个羟基中的每一个的邻位，Y和Z各自为O，X为环原子 直接与X相邻的sp2碳原子连接，然后用H，OH，Cl，Br，I，氨基，氰基，烷基，烷氧基，烯基或烯氧基取代; Y和Z各自独立地选自O，S和NH; 或其药学上可接受的盐或酯。
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公开(公告)号：US5589485A
公开(公告)日：1996-12-31
申请号：US429405
申请日：1995-04-26
申请人： Jill E. Hochlowski , Marianna Jackson , Sunil K. Kadam , James P. Karwowski , James B. McAlpine
发明人： Jill E. Hochlowski , Marianna Jackson , Sunil K. Kadam , James P. Karwowski , James B. McAlpine
IPC分类号： C07D211/88 , C07D211/40 , A61K31/44 , A61K31/445 , C07D211/76
CPC分类号： C07D211/88
摘要： Novel antifungal and antitumor agents having the formula ##STR1## as well as pharmaceutically acceptable salts, esters, amides and pro-drugs thereof, wherein R is selected from the group consisting of ##STR2## Also disclosed are pharmaceutical compositions comprising such compounds, and methods of treatment and processes of manufacture relating thereto.
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