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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：US20080199940A1
公开(公告)日：2008-08-21
申请号：US11511586
申请日：2006-08-28
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：US07312339B2
公开(公告)日：2007-12-25
申请号：US10865767
申请日：2004-06-14
IPC分类号： C07D207/444 , C07D209/48
CPC分类号： C12R1/60 , C07D263/32 , C07D413/12 , C12P17/14
摘要： Polyene oxazoles of the following formula wherein R3 is selected from H and methyl, are disclosed. Such compounds, and pharmaceutically acceptable salts thereof, may be used in the inhibition of tumor cell growth. The polyene oxazoles and their pharmaceutically acceptable salts may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers for use in the inhibition of tumor cells. The polyene oxazoles may be obtained from strains of Streptomyces sparsogenes, such as strain 022 having deposit number IDAC 270504-04.
摘要翻译： 公开了下式的多烯恶唑，其中R 3选自H和甲基。 这些化合物及其药学上可接受的盐可用于抑制肿瘤细胞生长。 多烯恶唑及其药学上可接受的盐可以配制成具有用于抑制肿瘤细胞的药学上可接受的载体的药物组合物。 多烯恶唑可以从天竺葵链霉菌菌株获得，例如具有保藏号IDAC 270504-04的菌株022。
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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：US07375088B2
公开(公告)日：2008-05-20
申请号：US10760493
申请日：2004-01-21
CPC分类号： C07H15/203 , C07C215/24 , C07C225/14 , C07C235/28 , C07C237/16 , C07C279/22 , C07C305/14 , C07C2601/10 , C07C2601/14 , C07H15/10 , C07H15/18 , C07H15/26 , C12P7/42 , C12P11/00 , C12P13/001 , C12P13/02 , C12P19/44 , C12R1/465 , Y10S435/886
摘要： This invention relates to a new class of polyene polyketides, their pharmaceutically acceptable salts and derivatives, and to methods for obtaining the compounds. One method of obtaining these compounds is by cultivation of novel strains of Streptomyces aizunensis; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to the novel strains of Streptomyces aizunensis used to produce these compounds, to the use of these compounds and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of fungal cell growth and cancer cell growth. The invention also relates to pharmaceutical compositions comprising these novel polyketides or a pharmaceutically acceptable salts or derivatives thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of these novel polyketides.
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6.发明授权Cyclic hexadepsipeptides, processes for their production and their use as pharmaceuticals 失效环十六肽，其制备方法及其作为药物的用途公开(公告)号：US08076287B2
公开(公告)日：2011-12-13
申请号：US12294213
申请日：2007-03-28
IPC分类号： A61K38/12
CPC分类号： C07K7/06 , A61K38/00 , C12P17/188 , C12P21/02 , C12R1/465
摘要： The present invention provides cyclic hexadepsipeptides and their pharmaceutically acceptable salts, solvates and prodrugs, and methods for obtaining the compounds, by fermentation, optionally followed by post-biosynthesis chemical modification. The present invention further provides uses of cyclic hexadepsipeptides, and their pharmaceutically acceptable salts, solvates and prodrugs as pharmaceuticals, in particular to their use as antibacterial, antifungal or antineoplastic agents, and to pharmaceutical compositions comprising a cyclic hexadepsipeptide, or a pharmaceutically acceptable salt, solvate or prodrug thereof, together with a carrier.
摘要翻译： 本发明提供环状十六肽及其药学上可接受的盐，溶剂合物和前药，以及通过发酵，任选地随后进行生物合成化学修饰来获得化合物的方法。 本发明进一步提供了环状十六肽及其药学上可接受的盐，溶剂合物和前药作为药物，特别是其作为抗细菌剂，抗真菌剂或抗肿瘤剂的用途的用途，以及包含环十六肽或其药学上可接受的盐， 溶剂化物或前药，以及载体。
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7.发明申请CYCLIC HEXADEPSIPEPTIDES, PROCESSES FOR THEIR PRODUCTION AND THEIR USE AS PHARMACEUTICALS 失效周期性十六烷基硫酸酯，其生产工艺及其作为药物的使用公开(公告)号：US20090215789A1
公开(公告)日：2009-08-27
申请号：US12294213
申请日：2007-03-28
IPC分类号： A61K31/501 , C07D401/14 , C12N1/20 , C12P17/16 , A61P31/04 , A61P35/00
CPC分类号： C07K7/06 , A61K38/00 , C12P17/188 , C12P21/02 , C12R1/465
摘要： The present invention provides cyclic hexadepsipeptides and their pharmaceutically acceptable salts, solvates and prodrugs, and methods for obtaining the compounds, by fermentation, optionally followed by post-biosynthesis chemical modification. The present invention further provides uses of cyclic hexadepsipeptides, and their pharmaceutically acceptable salts, solvates and prodrugs as pharmaceuticals, in particular to their use as antibacterial, antifungal or antineoplastic agents, and to pharmaceutical compositions comprising a cyclic hexadepsipeptide, or a pharmaceutically acceptable salt, solvate or prodrug thereof, together with a carrier.
摘要翻译： 本发明提供环状十六肽及其药学上可接受的盐，溶剂合物和前药，以及通过发酵，任选地随后进行生物合成化学修饰来获得化合物的方法。 本发明进一步提供了环状十六肽及其药学上可接受的盐，溶剂合物和前药作为药物，特别是其作为抗细菌剂，抗真菌剂或抗肿瘤剂的用途的用途，以及包含环十六肽或其药学上可接受的盐， 溶剂化物或前药，以及载体。
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公开(公告)号：US07300921B2
公开(公告)日：2007-11-27
申请号：US10937379
申请日：2004-09-10
IPC分类号： A61K31/70 , C07H15/00 , C07D237/00 , C12P19/60
CPC分类号： C07C279/14 , C07C2601/10 , C07D309/10 , C07H5/04 , C07H5/06 , C12N15/52 , C12P7/42 , C12P13/001 , C12P13/02 , C12P17/06 , C12P17/16 , C12P19/44 , C12R1/01 , Y10S435/821
摘要： Novel polyene polyketides, their pharmaceutically acceptable salts, prodrugs and derivatives have been found to have antibiotic activity. One method for obtaining the compounds is by cultivation of Amycolatopsis orientalis ATCC™ 43491 or a mutant or variant such as the strain IDAC-220604-1. Another method for obtaining the compounds is post-biosynthesis chemical modification of the compounds obtained by cultivation. Novel polynucleotide sequences and encoded proteins for the biosynthesis of the polyene polyketides are also presented.
摘要翻译： 已经发现新型多烯聚酮化合物，其药学上可接受的盐，前药和衍生物具有抗生素活性。 获得化合物的一种方法是通过种植侧寄生菌ATCC 43491或突变体或变体例如菌株IDAC-220604-1。 获得化合物的另一种方法是通过培养获得的化合物的后生物合成化学修饰。 还提出了用于多烯聚酮化合物的生物合成的新型多核苷酸序列和编码的蛋白质。
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9.发明授权Polyene polyketides, processes for their production and their use as a pharmaceutical 失效聚烯烃聚合物，其生产方法及其作为药物的用途公开(公告)号：US07416868B2
公开(公告)日：2008-08-26
申请号：US10760494
申请日：2004-01-21
IPC分类号： C12N9/00
CPC分类号： C07H15/203 , C07C215/24 , C07C225/14 , C07C235/28 , C07C237/16 , C07C279/22 , C07C305/14 , C07C2601/10 , C07C2601/14 , C07H15/10 , C07H15/18 , C07H15/26 , C12P7/42 , C12P11/00 , C12P13/001 , C12P13/02 , C12P19/44 , C12R1/465 , Y10S435/886
摘要： This invention relates to a new class of polyene polyketides, their pharmaceutically acceptable salts and derivatives, and to methods for obtaining the compounds. One method of obtaining these compounds is by cultivation of novel strains of Streptomyces aizunensis; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to the novel strains of Streptomyces aizunensis used to produce these compounds, to the use of these compounds and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of fungal cell growth and cancer cell growth. The invention also relates to pharmaceutical compositions comprising these novel polyketides or a pharmaceutically acceptable salts or derivatives thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of these novel polyketides.
摘要翻译： 本发明涉及新类型的多烯聚酮化合物，其药学上可接受的盐和衍生物，以及获得化合物的方法。 获得这些化合物的一种方法是通过培养新的链霉菌链霉菌菌株; 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。 本发明还涉及用于制备这些化合物的新型链霉菌Streptomyces aizunensis菌株，使用这些化合物及其药学上可接受的盐和衍生物作为药物，特别是其作为真菌细胞生长抑制剂和癌细胞生长的用途。 本发明还涉及包含这些新型聚酮化合物或其药学上可接受的盐或衍生物的药物组合物。 最后，本发明涉及参与这些新型聚酮化合物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：US20100016170A1
公开(公告)日：2010-01-21
申请号：US11803406
申请日：2007-05-14
IPC分类号： C40B20/04
CPC分类号： C07K14/36 , C07K14/365 , C12N15/52 , C12P19/62
摘要： A method for identifying gene cluster is disclosed. The method may be used for identifying gene clusters involved in the biosynthesis of natural products. A small insert library of DNA fragments of genomic DNA and a large insert library of DNA fragments of genomic DNA are prepared. Fragments in the small insert library are sequenced and compared by homology comparison under computer control to a database containing genes, gene fragments or proteins known to be involved in the biosynthesis of microbial natural products. Fragments having similar structure to genes, gene fragments or proteins known to be involved in the biosynthesis of naturally occurring metabolites are used as probes to screen the large insert library of genomic DNA to detect gene clusters involved in the biosynthesis of microbial natural products.
摘要翻译： 公开了鉴定基因簇的方法。 该方法可用于鉴定涉及天然产物生物合成的基因簇。 制备基因组DNA的DNA片段的小插入文库和基因组DNA的DNA片段的大插入文库。 对小插入片段中的片段进行测序，并通过计算机控制下的同源性比较与包含已知参与微生物天然产物生物合成的基因，基因片段或蛋白质的数据库进行比较。 具有与基因相似结构的片段，已知参与天然存在的代谢物的生物合成的基因片段或蛋白质被用作筛选基因组DNA的大插入文库以探测参与微生物天然产物生物合成的基因簇的片段。
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