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1. 发明申请

WO2002097062A3 RECOMBINANT NARBONOLIDE POLYKETIDE SYNTHASE 审中-公开
公开(公告)号：WO2002097062A3
公开(公告)日：2002-12-05
申请号：PCT/US2002/005642
申请日：2002-02-22
申请人： KOSAN BIOSCIENCES, INC. , ASHLEY, Gary , BETLACH, Melanie, C. , BETLACH, Mary , MCDANIEL, Robert , TANG, Li
发明人： ASHLEY, Gary , BETLACH, Melanie, C. , BETLACH, Mary , MCDANIEL, Robert , TANG, Li
IPC分类号： C12N1/20
摘要： Recombinant DNA compounds that encode all or a portion of the narbonolide polyketide synthase are used to express recombinant polyketide synthase genes in host cells for the production of narbonolide, narbonolide derivatives, and polyketides that are useful as antibiotics and as intermediates in the synthesis of compounds with pharmaceutical value.

2. 发明申请

WO2002097062A2 RECOMBINANT NARBONOLIDE POLYKETIDE SYNTHASE 审中-公开
标题翻译：重组NARBONOLIDE POLYKETIDE SYNTHASE
公开(公告)号：WO2002097062A2
公开(公告)日：2002-12-05
申请号：PCT/US2002/005642
申请日：2002-02-22
申请人： KOSAN BIOSCIENCES, INC. , ASHLEY, Gary , BETLACH, Melanie, C. , BETLACH, Mary , MCDANIEL, Robert , TANG, Li
发明人： ASHLEY, Gary , BETLACH, Melanie, C. , BETLACH, Mary , MCDANIEL, Robert , TANG, Li
IPC分类号： C12N
CPC分类号： C07D323/00 , C07H17/08 , C12N9/14 , C12N15/52 , C12N15/65 , C12P17/08 , C12P19/62 , C40B40/00
摘要： Recombinant DNA compounds that encode all or a portion of the narbonolide polyketide synthase are used to express recombinant polyketide synthase genes in host cells for the production of narbonolide, narbonolide derivatives, and polyketides that are useful as antibiotics and as intermediates in the synthesis of compounds with pharmaceutical value.
摘要翻译：用于编码全部或部分纳博内酯聚酮化合物合成酶的重组DNA化合物用于在宿主细胞中表达重组聚酮化合物合成酶基因，用于生产可用作抗生素的纳博内酯，纳博内酯衍生物和聚酮化合物，并且作为合成具有药品价值。

3. 发明申请

WO2002064589A1 LAULIMALIDE DERIVATIVES 审中-公开
标题翻译： LAULIMALIDE衍生物
公开(公告)号：WO2002064589A1
公开(公告)日：2002-08-22
申请号：PCT/US2002/003706
申请日：2002-02-08
申请人： KOSAN BIOSCIENCES, INC.
发明人： ASHLEY, Gary , METCALF, Brian
IPC分类号： C07D417/06
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：酸性化合物，其中间体及其制备方法及其用于治疗以细胞过度增殖为特征的疾病的方法。式（I）。

4. 发明申请

WO2002051855A3 MOTILIDE COMPOUNDS 审中-公开
公开(公告)号：WO2002051855A3
公开(公告)日：2002-07-04
申请号：PCT/US2001/043963
申请日：2001-11-21
申请人： KOSAN BIOSCIENCES, INC.
发明人： SANTI, Daniel , TIAN, Zong-Qiang , METCALF, Brian , ASHLEY, Gary
IPC分类号： C07H17/08
摘要： The present invention provides novel macrolide compounds of the formulas for the treatment of gastrointestinal motility disorders.

5. 发明申请

WO2003061671A1 AMIDO MACROLIDES 审中-公开
公开(公告)号：WO2003061671A1
公开(公告)日：2003-07-31
申请号：PCT/US2003/001398
申请日：2003-01-17
申请人： KOSAN BIOSCIENCES, INC.
发明人： ASHLEY, Gary , SHAW, Simon James , LI, Yandong
IPC分类号： A61K31/70
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.
摘要翻译：提供了各种大环内酯化合物，例如具有下式的那些化合物，其中变量具有本文提供的值。

6. 发明申请

WO2002080846A3 EPOTHILONE DERIVATIVES AND METHODS FOR MAKING AND USING THE SAME 审中-公开
公开(公告)号：WO2002080846A3
公开(公告)日：2002-10-17
申请号：PCT/US2002/010468
申请日：2002-04-02
申请人： KOSAN BIOSCIENCES, INC.
发明人： ASHLEY, Gary , ARSLANIAN, Robert, L. , CARNEY, John , METCALF, Brian , TANG, Li
IPC分类号： A61K31/33
摘要： This invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , W, X, Y, and Ar are as defined herein. Compounds of formula (I) are useful in the treatment of diseases or conditions characterized by cellular hyperproliferation. This invention also relates to means for the preparation of compounds of Formula (I); formulations containing compounds of formula (I); and methods for the use of said compounds and formulations in the treatment of a disease or condition characterized by cellular hyperproliferation, including cancer.

7. 发明申请

WO2002080846A2 EPOTHILONE DERIVATIVES AND METHODS FOR MAKING AND USING THE SAME 审中-公开
标题翻译： EPOTHILONE衍生物及其制备和使用方法
公开(公告)号：WO2002080846A2
公开(公告)日：2002-10-17
申请号：PCT/US2002/010468
申请日：2002-04-02
申请人： KOSAN BIOSCIENCES, INC.
发明人： ASHLEY, Gary , ARSLANIAN, Robert, L. , CARNEY, John , METCALF, Brian , TANG, Li
IPC分类号： A61K
CPC分类号： C07D405/06 , C07D313/00 , C07D413/06 , C07D417/06 , C07D491/04 , C12N1/20 , C12N9/00 , C12N15/52 , C12N15/74 , C12P17/16 , C12P17/181 , C12R1/01
摘要： This invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , W, X, Y, and Ar are as defined herein. Compounds of formula (I) are useful in the treatment of diseases or conditions characterized by cellular hyperproliferation. This invention also relates to means for the preparation of compounds of Formula (I); formulations containing compounds of formula (I); and methods for the use of said compounds and formulations in the treatment of a disease or condition characterized by cellular hyperproliferation, including cancer.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐和溶剂化物，其中R 1，R 2，R 3，R 4，R 5，W，X，Y ，Ar如本文所定义。式（I）化合物可用于治疗以细胞过度增殖为特征的疾病或病症。本发明还涉及制备式（I）化合物的方法; 含有式（I）化合物的制剂; 以及在治疗以细胞过度增殖为特征的疾病或病症（包括癌症）中使用所述化合物和制剂的方法。

8. 发明申请

WO2002008440A3 FERMENTATION PROCESS FOR EPOTHILONES 审中-公开
公开(公告)号：WO2002008440A3
公开(公告)日：2002-01-31
申请号：PCT/US2001/023549
申请日：2001-07-25
申请人： KOSAN BIOSCIENCES, INC.
发明人： SANTI, Daniel , METCALF, Brian , ASHLEY, Gary
IPC分类号： C12N15/53
摘要： Desoxyepothilone compounds are produced by fermentation of an epothilone microorganism in the presence of a P450 enzyme inhibitor.

9. 发明公开

EP1255763A2 MOTILIDE COMPOUNDS 审中-公开
标题翻译： MOTILIDE化合物
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
申请人： Kosan Biosciences, Inc.
发明人： ASHLEY, Gary , BURLINGAME, Mark , CARRERAS, Christopher , SANTI, Daniel
IPC分类号： C07H17/08 , A61K31/70
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。

10. 发明公开

EP2121957A1 MACROLACTAMS BY ENGINEERED BIOSYNTHESIS 审中-公开
标题翻译：按工业生物合成WON macrolactams
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
申请人： Kosan Biosciences, Inc.
发明人： ASHLEY, Gary , MENZELLA, Hugo, G. , WEE, Janice, Lau , CARNEY, John, R.
IPC分类号： C12P19/62 , A01N43/04 , A61K31/70
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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