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1. 发明申请

WO0192255A3 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：WO0192255A3
公开(公告)日：2002-02-28
申请号：PCT/US0115763
申请日：2001-05-15
申请人： KOSAN BIOSCIENCES INC , SANTI DANIEL , FARDIS MARIA , ASHLEY GARY
发明人： SANTI DANIEL , FARDIS MARIA , ASHLEY GARY
IPC分类号： C07D417/06 , C07D417/14 , C07D491/04 , C07D493/04 , A61K31/335 , A61P35/00
CPC分类号： C07D417/06 , C07D417/14 , C07D491/04 , C07D493/04
摘要： The present invention relates to 16-membered macrocyclic compounds. In one aspect of the present invention, compounds of the formula (I), are provided wherein: R , R , R , and R are each independently hydrogen, methyl or ethyl; R is hydrogen, hydroxyl, oxo, or NRR' where R and R' are independently hydrogen, C1-C10 aliphatic, aryl or alkylaryl; R is hydrogen, oxo, or C1-C10 aliphatic, or optionally R and R together form a carbon-carbon double bond; R is hydrogen, hydroxyl, oxo, C1-C10 aliphatic, C1-C10 alkylester, or halide; R is hydrogen or C1-C10 aliphatic that is optionally substituted C1-C5 aliphatic, C1-C5 alkoxy, aryl, or a functional group selected from the group consisting of acetal, alcohol, aldehyde, amide, amine, carbamate, carboalkoxy, carbonate, carbodiimide, carboxylic acid, dioxolane and halogen, or optionally, R and R together form a 1,3-dioxane that is optionally substituted at the 2-position; R and R are both hydrogen or together form a carbon-carbon double bond or an epoxide; Ar is aryl; and, W is O or NR where R is hydrogen, C1-C10 aliphatic, aryl or alkylaryl provided that at least one of R , R , and R is not hydrogen. These compounds are cytotoxic agents and can be used to treat cancer and non-cancer disorders characterized by cellular hyperproliferation.
摘要翻译：本发明涉及16元大环化合物。在本发明的一个方面，提供式（I）化合物，其中：R 1，R 2，R 3和R 10各自独立地为氢，甲基或乙基; R 4是氢，羟基，氧代或NRR'，其中R和R'独立地是氢，C 1 -C 10脂族，芳基或烷基芳基; R 5是氢，氧代或C 1 -C 10脂族基，或任选地R 4和R 5一起形成碳 - 碳双键; R 6是氢，羟基，氧代，C 1 -C 10脂族，C 1 -C 10烷基酯或卤化物; R 7是氢或C 1 -C 10脂族基，其是任选取代的C 1 -C 5脂族，C 1 -C 5烷氧基，芳基或选自缩醛，醇，醛，酰胺，胺，氨基甲酸酯，烷氧羰基的官能团，碳酸酯，碳二亚胺，羧酸，二氧戊环和卤素，或任选地，R 6和R 7一起形成任选在2-位取代的1,3-二恶烷; R 8和R 9均为氢或一起形成碳 - 碳双键或环氧化物; Ar为芳基; 并且W是O或NR 11，其中R 11是氢，C 1 -C 10脂族，芳基或烷基芳基，条件是R 4，R 5和R 6中的至少一个不是氢。这些化合物是细胞毒性剂，可用于治疗以细胞过度增殖为特征的癌症和非癌症疾病。

2. 发明申请

WO0212534A3 BIO-INTERMEDIATES FOR USE IN THE CHEMICAL SYNTHESIS OF POLYKETIDES 审中-公开
标题翻译：用于化学合成聚合物的生物中间体
公开(公告)号：WO0212534A3
公开(公告)日：2002-09-06
申请号：PCT/US0125112
申请日：2001-08-09
申请人： KOSAN BIOSCIENCES INC
发明人： SANTI DANIEL V , ASHLEY GARY , MYLES DAVID C
IPC分类号： C12N15/09 , A61K31/366 , A61K31/427 , A61P35/00 , C07C271/16 , C07C275/24 , C07D211/76 , C07D309/30 , C07D309/32 , C07D313/00 , C07D319/06 , C07D413/06 , C07D417/06 , C12P7/26 , C12P11/00 , C12P13/02 , C12P17/06 , C12P17/08 , C12P17/12 , C12P17/16 , C12P17/18 , G06F19/00
CPC分类号： C07D413/06 , C07D309/30 , C07D309/32 , C07D319/06 , C07D417/06 , C12P7/26 , C12P11/00 , C12P13/02 , C12P17/06 , C12P17/08 , C12P17/12 , C12P17/16 , C12P17/181
摘要： The present invention relates to compounds made by a subset of modules from one or more polyketide synthase ("PKS") genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates ("bio-intermediates") generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specifity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greatly simplified.
摘要翻译：本发明涉及由一种或多种聚酮化合物合酶（“PKS”）基因的模块子集构成的化合物，其用作新型分子的化学合成中的原料，特别是天然存在的聚酮化合物或其衍生物。生物衍生的中间体（“生物中间体”）通常代表由于一种或多种立体中心而使用传统化学方法合成的特别困难的化合物。在本发明的一个方面，提供埃坡霉素合成中的中间体，其进入Danishefsky及其同事的合成方案。在本发明的另一方面，提供了合成麦芽糖醇的中间体，其进入史密斯及其同事的合成方案。通过利用生物过程的固有立体化学特性，大大简化了关键中间体的合成以及化合物如埃坡霉素和discodermolide的总体合成。

3. 发明申请

WO0063361A3 A MULTI-PLASMID METHOD FOR PREPARING LARGE LIBRARIES OF POLYKETIDES AND NON-RIBOSOMAL PEPTIDES 审中-公开
标题翻译：用于制备大量多核苷酸和非结构蛋白质图谱的多级PLASMID方法
公开(公告)号：WO0063361A3
公开(公告)日：2001-07-12
申请号：PCT/US0010021
申请日：2000-04-12
申请人： KOSAN BIOSCIENCES INC
发明人： SANTI DANIEL V , XUE QUN , ASHLEY GARY
IPC分类号： C12N15/09 , A61K31/7048 , A61P3/06 , A61P31/04 , A61P37/06 , C07B61/00 , C07H17/08 , C12N15/52 , C12P17/08 , C12P19/62 , C12P21/02 , C12N15/10 , A61K31/70 , A61P31/00 , C07D309/00 , C07D313/04 , C07D493/10 , C07H17/04 , C12N9/10 , C12N15/63 , C12N15/90 , C12R1/465
CPC分类号： C07H17/08 , C12N15/52 , C12P17/08 , C12P19/62 , C40B40/00
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.
摘要翻译：用于异源表达聚酮化合物的多质粒系统促进组合生物合成。该方法可以扩展到任何模块化聚酮化合物合酶（PKS）或非核糖体肽合成酶（NRPS），并且具有产生数千种新型天然产物的潜力，包括衍生自通过定制酶进一步修饰PKS或NRPS产物的新天然产物。

4. 发明申请

WO0232916A3 SIXTEEN-MEMBERED MACROLIDE COMPOUNDS 审中-公开
标题翻译：第六届会议化妆品化学品
公开(公告)号：WO0232916A3
公开(公告)日：2003-01-16
申请号：PCT/US0130725
申请日：2001-09-24
申请人： KOSAN BIOSCIENCES INC , KATZ LEONARD , ASHLEY GARY , BURLINGAME MARK A , DONG STEVEN D , FU HONG , LI YONG , MYLES DAVID C
发明人： KATZ LEONARD , ASHLEY GARY , BURLINGAME MARK A , DONG STEVEN D , FU HONG , LI YONG , MYLES DAVID C
IPC分类号： A61P31/00 , C07D313/00 , C07H17/08 , A61K31/70 , C07C327/30
CPC分类号： C07H17/08 , C07D313/00
摘要： The present invention provides novel sixteen-membered macrolide compounds that are useful as anti-infective agents or as intermediates thereto. The present invention also provides methods for the preparation of these compounds, and methods and formulations for their use. In one aspect of the present invention, sixteen-membered macrolide possessing a side chain Z are provided where Z is aliphatic, aryl, alkylaryl, halide, =NOR , =NNHR , or -W-R where W is O, S, NC(=O)R , NC(=O)OR , NC(=O)NHR or NR where R and R are each independently hydrogen, aliphatic, aryl or alkylaryl. In another aspect of the present invention, bicyclic compounds are provided where one of the cyclic-components is a sixteen-membered macrolide and the other is a cyclic moiety whose cyclic structure is formed by between 3 and 10 atoms. In another aspect of the present invention, sixteen-membered macrolide compounds that bind to the domain II region of the 23S RNA are provided.
摘要翻译：本发明提供可用作抗感染剂或作为其中间体的新颖的十六元大环内酯化合物。本发明还提供了制备这些化合物的方法及其用途的方法和制剂。在本发明的一个方面，提供了具有侧链Z的十六元大环内酯，其中Z是脂族，芳基，烷基芳基，卤化物，= NOR 3，= NNHR 3或-WR 3，其中W 是O，S，NC（= O）R 4，NC（= O）OR 4，NC（= O）NHR 4或NR 4，其中R 3和R 4是各自独立地为氢，脂族，芳基或烷基芳基。在本发明的另一方面，提供了双环化合物，其中环状组分之一是十六元大环内酯，另一个是其环状结构由3至10个原子形成的环状部分。在本发明的另一方面，提供了结合23S RNA的结构域II的十六元大环内酯化合物。

5. 发明申请

WO0183800A8 PRODUCTION OF POLYKETIDES 审中-公开
标题翻译：生产多晶硅
公开(公告)号：WO0183800A8
公开(公告)日：2003-01-03
申请号：PCT/US0113793
申请日：2001-04-26
申请人： KOSAN BIOSCIENCES INC , ARSLANIAN ROBERT L , ASHLEY GARY , FRYKMAN SCOTT , JULIEN BRYAN , KATZ LEONARD , KHOSLA CHAITAN , LAU JANICE , LICARI PETER J , REGENTIN RIKA , SANTI DANIEL , TANG LI
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： C07D313/00 , C07D405/06 , C07D413/06 , C07D417/06 , C07D491/04 , C12N1/20 , C12N1/21 , C12N9/00 , C12N15/52 , C12N15/74 , C12P17/16 , C12P17/18 , C12R1/01 , C12P17/00
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.
摘要翻译：可以使用重组的粘液球菌宿主细胞来产生聚酮化合物，包括可从发酵液中纯化并结晶的埃坡霉素和埃坡霉素类似物。

6. 发明申请

WO9961599A3 RECOMBINANT NARBONOLIDE POLYKETIDE SYNTHASE 审中-公开
标题翻译：重组NARBONOLIDE POLYKETIDE SYNTHASE
公开(公告)号：WO9961599A3
公开(公告)日：2000-01-27
申请号：PCT/US9911814
申请日：1999-05-27
申请人： KOSAN BIOSCIENCES INC
发明人： ASHLEY GARY , BETLACH MELANIE C , BETLACH MARY , MCDANIEL ROBERT , TANG LI
IPC分类号： C12N15/09 , C07D313/00 , C07D405/12 , C07D493/22 , C07D498/18 , C07H17/08 , C07K19/00 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/00 , C12N9/14 , C12N15/65 , C12N15/52 , C12N15/76
CPC分类号： C12N15/65 , C12N9/14
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。

7. 发明申请

WO0183800A9 HETEROLOGOUS PRODUCTION OF POLYKETIDES 审中-公开
标题翻译：异源生产聚酮化合物
公开(公告)号：WO0183800A9
公开(公告)日：2003-09-12
申请号：PCT/US0113793
申请日：2001-04-26
申请人： KOSAN BIOSCIENCES INC , ARSLANIAN ROBERT L , ASHLEY GARY , FRYKMAN SCOTT , JULIEN BRYAN , KATZ LEONARD , KHOSLA CHAITAN , LAU JANICE , LICARI PETER J , REGENTIN RIKA , SANTI DANIEL , TANG LI
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： C07D313/00 , C07D405/06 , C07D413/06 , C07D417/06 , C07D491/04 , C12N1/20 , C12N1/21 , C12N9/00 , C12N15/52 , C12N15/74 , C12P17/16 , C12P17/18 , C12R1/01 , 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.
摘要翻译：重组粘球菌属宿主细胞可用于生产聚酮化合物，包括可从发酵液中纯化并结晶的埃坡霉素和埃坡霉素类似物。

8. 发明申请

WO0183800A3 HETEROLOGOUS PRODUCTION OF POLYKETIDES 审中-公开
标题翻译：聚合物的异质生产
公开(公告)号：WO0183800A3
公开(公告)日：2003-04-10
申请号：PCT/US0113793
申请日：2001-04-26
申请人： KOSAN BIOSCIENCES INC , ARSLANIAN ROBERT L , ASHLEY GARY , FRYKMAN SCOTT , JULIEN BRYAN , KATZ LEONARD , KHOSLA CHAITAN , LAU JANICE , LICARI PETER J , REGENTIN RIKA , SANTI DANIEL , TANG LI
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： C07D313/00 , C07D405/06 , C07D413/06 , C07D417/06 , C07D491/04 , C12N1/20 , C12N1/21 , C12N9/00 , C12N15/52 , C12N15/74 , C12P17/16 , C12P17/18 , C12R1/01 , 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.
摘要翻译：重组粘球菌宿主细胞可用于产生聚酮化合物，包括可从发酵液中纯化并结晶的埃坡霉素和埃坡霉素类似物。

9. 发明申请

WO02051855A2 MOTILIDE COMPOUNDS 审中-公开
标题翻译： MOTILIDE化合物
公开(公告)号：WO02051855A2
公开(公告)日：2002-07-04
申请号：PCT/US0143963
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： C07H17/00 , A61K31/7052 , A61P1/00 , A61P1/04 , A61P1/06 , A61P1/08 , A61P1/10 , A61P1/14 , A61P1/16 , A61P17/00 , A61P43/00 , C07H17/08
CPC分类号： C07H17/08
摘要： The present invention provides novel macrolide compounds of the formulas for the treatment of gastrointestinal motility disorders.
摘要翻译：本发明提供了用于治疗胃肠运动障碍的新的大环内酯化合物。

10. 发明申请

WO0208440A2 FERMENTATION PROCESS FOR EPOTHILONES 审中-公开
标题翻译： EPOTHILONES的发酵工艺
公开(公告)号：WO0208440A2
公开(公告)日：2002-01-31
申请号：PCT/US0123549
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： C12N15/09 , C12N1/21 , C12N9/02 , C12N15/53 , C12P17/08 , C12P17/16 , C12P17/18 , C12R1/01 , C12P17/00
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.
摘要翻译：脱氧皮质醇化合物通过在P450酶抑制剂存在下发酵埃坡霉素微生物而产生。

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