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1.发明公开COMBINATORIAL POLYKETIDE LIBRARIES PRODUCED USING A MODULAR PKS GENE CLUSTER AS SCAFFOLD 失效使用模块化PKS基因簇作为分支构建组合型多肽库
公开(公告)号：EP0979286A2
公开(公告)日：2000-02-16
申请号：EP98918891.7
申请日：1998-04-30
发明人： KHOSLA, Chaitan , ASHLEY, Gary , FU, Hong , KAO, Camilla, M. , MCDANIEL, Robert
IPC分类号： C12N15/52 , C12N15/76 , C12N9/00 , C12N1/21 , C12P17/06 , C07D309/00 , C07D313/04 , C07D493/10 , C07D313/00 , C07H17/04
CPC分类号： C07H17/08 , C07D323/00 , C12N15/52 , C40B40/00
摘要： Combinatorial libraries of polyketides can be obtained by suitable manipulation of a host modular polyketide synthase gene cluster such as that which encodes the PKS for erythromycin. The combinatorial library is useful as a source of pharmaceutically active compounds. In addition, novel polyketides and antibiotics are prepared using this method.
摘要翻译： 聚酮化合物组合文库可通过适当操作宿主模块化聚酮化合物合酶基因簇，如编码红霉素PKS的基因簇获得。 组合文库可用作药物活性化合物的来源。 另外，使用这种方法制备新颖的聚酮化合物和抗生素。
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公开(公告)号：EP1255763A2
公开(公告)日：2002-11-13
申请号：EP01910921.4
申请日：2001-02-15
CPC分类号： C07H17/08
摘要： The present invention provides novel macrolide compounds of the formulas (I, II, III or IV) wherein: R is hydroxyl or methoxy; R1 is selected from the group consisting of hydrogen, hydroxyl, halide, NH¿2, OR?9, (a, b, c, and d) where R9 is C1-C10 alkenyl, C2-C10 alkynyl, aryl or heteroaryl and R?10 and R11¿ are each independently hydrogen, C¿1?-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or aryl; R?2 and R3¿ are each independently selected from the group consisting of hydrogen, C¿1?-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, alkylaryl, alkenylaryl, alkynylaryl or R?2 and R3¿ together form a cycloalkyl or a cycloaryl moiety; R4 is hydrogen or methyl; R5 is hydrogen, hydroxyl, oxo, or together with R6 and the carbons to which they are attached form a cyclic carbonate; R6 is hydrogen, hydroxyl, OR12 where R12 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or together with R5 and the carbons to which they are attached form a cyclic carbonate; R7 is methyl, C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl; R8 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl; and, x is a single or a double bond.
摘要翻译： 本发明提供了式（I，II，III或IV）的新的大环内酯化合物，其中：R是羟基或甲氧基; （a，b，c和d），其中R 9为C 1 -C 10烯基，C 2 -C 10炔基，芳基或杂芳基，R 1选自氢，羟基，卤素，NH 2，OR 9 R 10和R 11各自独立地为氢，C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基或芳基; R 2和R 3各自独立地选自氢，C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，芳基，烷基芳基，烯基芳基，炔基芳基或R 2 2和R 3' 形成环烷基或环芳基部分; R4是氢或甲基; R5是氢，羟基，氧代或与R6和它们所连接的碳一起形成环状碳酸酯; R6为氢，羟基，OR12，其中R12为C1-C10烷基，C2-C10烯基，C2-C10炔基或与R5和它们所连接的碳一起形成环状碳酸酯; R7为甲基，C3-C10烷基，C2-C10烯基，C2-C10炔基，烷基芳基，烯基芳基，炔基芳基，酰氨基烷基芳基，酰氨基烷芳基或酰氨基烷芳基; R8为C1-C10烷基，C2-C10烯基，C2-C10炔基，烷基芳基，烯基芳基，炔基芳基，酰氨基烷基芳基，酰氨基烯基芳基或酰氨基炔基芳基; 并且，x是单键或双键。
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公开(公告)号：EP1320611A2
公开(公告)日：2003-06-25
申请号：EP01973782.4
申请日：2001-04-26
发明人： ARSLANIAN, Robert, L. , ASHLEY, Gary , FRYKMAN, Scott , JULIEN, Bryan , KATZ, Leonard , KHOSLA, Chaitan , LAU, Janice , LICARI, Peter, J. , REGENTIN, Rika , SANTI, Daniel , TANG, Li
IPC分类号： C12N15/52 , C12N15/74 , C12N9/00 , C12N1/21 , C12P17/16 , C12P17/18 , C07D313/00 , C07D413/06 , C07D417/06 , C07D493/04 , C07D493/06
CPC分类号： C12P17/181 , C07D313/00 , C07D405/06 , C07D407/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D491/04 , C07D493/04 , C12N1/20 , C12N9/00 , C12N15/52 , C12N15/74 , C12P17/16 , C12R1/01
摘要： Recombinant Myxococcus host cells can be used to produce polyketides, including epothilone and epothilone analogs that can be purified from the fermentation broth and crystallized.
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4.发明授权COMBINATORIAL POLYKETIDE LIBRARIES PRODUCED USING A MODULAR PKS GENE CLUSTER AS SCAFFOLD 失效使用模块化PKS基因簇作为分支构建组合型多肽库
公开(公告)号：EP0979286B1
公开(公告)日：2014-01-29
申请号：EP98918891.7
申请日：1998-04-30
发明人： KHOSLA, Chaitan , ASHLEY, Gary , FU, Hong , KAO, Camilla, M. , MCDANIEL, Robert
IPC分类号： C12N15/52 , C12N15/76 , C12N9/00 , C12N1/21 , C12P17/06 , C07D309/00 , C07D313/04 , C07D493/10 , C07D313/00 , C07H17/04
CPC分类号： C07H17/08 , C07D323/00 , C12N15/52 , C40B40/00
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公开(公告)号：EP2121957A1
公开(公告)日：2009-11-25
申请号：EP08724771.4
申请日：2008-01-23
CPC分类号： C12P17/10 , C07D225/06
摘要： Macrolactams are made by feeding aromatic amino acids as replacement starter units to a mutant strain of the geldanamycin-producing microorganism Streptomyces hygroscopicus var. geldanus NRRL 3602, wherein the gene cluster encoding enzymes for the biosynthesis of the natural starter unit 3-amino-5-hydroxybenzoic acid has been deleted.
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公开(公告)号：EP1358186A1
公开(公告)日：2003-11-05
申请号：EP02703356.2
申请日：2002-02-08
发明人： ASHLEY, Gary , METCALF, Brian
IPC分类号： C07D417/06 , C07D493/18 , C07D493/08 , A61K31/335
CPC分类号： C07D493/08
摘要： Laulimalide compounds, intermediates thereto and methods for their preparation and methods for their use in the treatment of diseases characterized by cellular hyperproliferation. Formula (I).
摘要翻译： 劳拉米尔化合物，其中间体及其制备方法和它们用于治疗以细胞过度增殖为特征的疾病的方法。 公式（I）。
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公开(公告)号：EP1303615A2
公开(公告)日：2003-04-23
申请号：EP01957264.3
申请日：2001-07-25
发明人： SANTI, Daniel , METCALF, Brian , ASHLEY, Gary
CPC分类号： C12N9/0071 , C12P17/08 , C12P17/167 , C12P17/181
摘要： Desoxyepothilone compounds are produced by fermentation of an epothilone microorganism in the presence of a P450 enzyme inhibitor.
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公开(公告)号：EP1471923A1
公开(公告)日：2004-11-03
申请号：EP03713257.8
申请日：2003-01-17
发明人： ASHLEY, Gary , SHAW, Simon James , LI, Yandong
CPC分类号： C07H17/08 , Y02P20/582
摘要： Various macrolide compounds such as those having the following formulas are provided where the variables have the values provided herein.
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公开(公告)号：EP1345953A2
公开(公告)日：2003-09-24
申请号：EP01981580.2
申请日：2001-10-12
发明人： HLASTA, Dennis , HENNINGER, Todd, C. , GRANT, Eugene, B. , KHOSLA, Chaitin , CHU, Daniel, T., W. , ASHLEY, Gary
IPC分类号： C07H17/08 , A61K31/7048 , A61P31/04
摘要： The present invention includes compounds of the formula wherein: X is hydrogen or halide; R2 is hydrogen, acyl, or a hydroxy protecting group; R6 is hydrogen, hydroxyl, or -ORa wherein Ra is a substituted or unsubstituted moiety selected from the group consisting of C¿1?-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; R?13¿ is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C¿3?-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and, R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are useful for the treatment of bacterial and protozoal infections.
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10.发明公开A MULTI-PLASMID METHOD FOR PREPARING LARGE LIBRARIES OF POLYKETIDES AND NON-RIBOSOMAL PEPTIDES 有权多质粒用于生产大型图书馆和聚酮化非核糖体肽
公开(公告)号：EP1171583A2
公开(公告)日：2002-01-16
申请号：EP00922192.0
申请日：2000-04-12
发明人： SANTI, Daniel, V. , XUE, Qun , ASHLEY, Gary
摘要： A multiple-plasmid system for heterologous expression of polyketides facilitates combinatorial biosynthesis. The method can be extended to any modular polyketide synthase (PKS) or non-ribosomal peptide synthase (NRPS) and has the potential to produce thousands of novel natural products, including ones derived from further modification of the PKS or NRPS products by tailoring enzymes.
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