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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

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。

3. 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。

4. 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。

5. 发明申请

WO0160833A3 MOTILIDE COMPOUNDS 审中-公开
标题翻译：胶体化合物
公开(公告)号：WO0160833A3
公开(公告)日：2002-01-24
申请号：PCT/US0105218
申请日：2001-02-15
申请人： KOSAN BIOSCIENCES INC , ASHLEY GARY , BURLINGAME MARK , CARRERAS CHRISTOPHER , SANTI DANIEL
发明人： ASHLEY GARY , BURLINGAME MARK , CARRERAS CHRISTOPHER , SANTI DANIEL
IPC分类号： A61K31/7048 , A61P1/00 , A61P1/04 , A61P1/10 , A61P1/14 , A61P1/16 , A61P17/00 , 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; R is selected from the group consisting of hydrogen, hydroxyl, halide, NH2, OR , (a, b, c, and d) where R is C1-C10 alkenyl, C2-C10 alkynyl, aryl or heteroaryl and R and R are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or aryl; R and R are each independently selected from the group consisting of hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, alkylaryl, alkenylaryl, alkynylaryl or R and R together form a cycloalkyl or a cycloaryl moiety; R is hydrogen or methyl; R is hydrogen, hydroxyl, oxo, or together with R and the carbons to which they are attached form a cyclic carbonate; R is hydrogen, hydroxyl, OR where R 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; R 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：本发明提供式（I，II，III或IV）的新型大环内酯化合物，其中：R是羟基或甲氧基; R 1选自氢，羟基，卤素，NH 2，OR 9，（a，b，c和d）其中R 9是C 1 -C 10链烯基，C 2 -C 10炔基，芳基或杂芳基，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，烷芳基，烯基芳基，炔基芳基或R 2， 3>一起形成环烷基或环芳基部分; R 4是氢或甲基; R 5是氢，羟基，氧代或与R 6一起，并且与它们相连的碳形成环状碳酸酯; R 6是氢，羟基，OR 12，其中R 12是C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，或与R 5一起，并且与它们相连的碳形成环状碳酸酯 ; R 7是甲基，C 3 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，烷基芳基，烯基芳基，炔基芳基，酰氨基烷基芳基，酰胺基烯基芳基或酰胺基炔基芳基; R 8是C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10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胺基炔基芳基; x是单键或双键。

6. 发明申请

WO2005103279A3 SYNTHETIC GENES 审中-公开
标题翻译：合成基因
公开(公告)号：WO2005103279A3
公开(公告)日：2009-04-23
申请号：PCT/US2005011452
申请日：2005-04-05
申请人： KOSAN BIOSCIENCES INC , SANTI DANIEL , KODUMAL SARAH J , REID RALPH C , PATEL KEDAR G
发明人： SANTI DANIEL , KODUMAL SARAH J , REID RALPH C , PATEL KEDAR G
IPC分类号： C12Q1/70 , C07H21/02 , C07H21/04 , C07K1/00 , C12N1/21 , C12N9/10 , C12N15/00 , C12N15/10 , C12N15/52 , C12N15/64 , C12N15/66 , C12N15/74 , C12P21/06
CPC分类号： C12N15/1031 , C12N15/1058 , C12N15/52 , C12N15/64 , C12N15/66
摘要： The invention provides strategies, methods, vectors, reagents, and systems for production of synthetic genes, production of libraries of such genes, and manipulation and characterization of the genes and corresponding encoded polypeptides. In one aspect, the synthetic genes can encode polyketide synthase polypeptides and facilitate production of therapeutically or commercially important polyketide compounds.
摘要翻译：本发明提供用于生产合成基因的策略，方法，载体，试剂和系统，这些基因的文库的生产，以及基因和相应的编码多肽的操作和表征。在一个方面，合成基因可以编码聚酮化合物合成酶多肽并促进治疗或商业上重要的聚酮化合物的产生。

7. 发明申请

WO0020601A3 POLYKETIDE SYNTHASE ENZYMES AND RECOMBINANT DNA CONSTRUCTS THEREFOR 审中-公开
公开(公告)号：WO0020601A3
公开(公告)日：2000-10-26
申请号：PCT/US9922886
申请日：1999-10-01
申请人： KOSAN BIOSCIENCES INC , REEVES CHRISTOPHER , CHU DANIEL , KHOSLA CHAITAN , SANTI DANIEL , WU KAI
发明人： REEVES CHRISTOPHER , CHU DANIEL , KHOSLA CHAITAN , SANTI DANIEL , WU KAI
IPC分类号： C12N15/09 , A61K31/436 , A61P25/00 , A61P37/06 , C07D498/18 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/00 , C12N9/10 , C12N9/12 , C12N15/52 , C12P17/18 , C12P19/32 , C12P19/62 , C12N15/54 , C12N15/62
CPC分类号： C07D498/18 , C07K2319/00 , C12N9/1029 , C12N9/1205 , C12N15/52 , C12P17/188 , C12P19/32
摘要： Host cells comprising recombinant vectors encoding the FK-520 polyketide synthase and FK-520 modification enzymes can be used to produce the FK-520 polyketide. Recombinant DNA constructs comprising one or more FK-520 polyketide synthase domains, modules, open reading frames, and variants thereof can be used to produce recombinant polyketide synthases and a variety of different polyketides with application as pharmaceutical and veterinary products.

8. 发明申请

WO0020601A9 POLYKETIDE SYNTHASE ENZYMES AND RECOMBINANT DNA CONSTRUCTS THEREFOR 审中-公开
标题翻译： POLYKTIDE SYNTHASE酶及其重组DNA构建体
公开(公告)号：WO0020601A9
公开(公告)日：2000-08-31
申请号：PCT/US9922886
申请日：1999-10-01
申请人： KOSAN BIOSCIENCES INC , REEVES CHRISTOPHER , CHU DANIEL , KHOSLA CHAITAN , SANTI DANIEL , WU KAI
发明人： REEVES CHRISTOPHER , CHU DANIEL , KHOSLA CHAITAN , SANTI DANIEL , WU KAI
IPC分类号： C12N15/09 , A61K31/436 , A61P25/00 , A61P37/06 , C07D498/18 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/00 , C12N9/10 , C12N9/12 , C12N15/52 , C12P17/18 , C12P19/32 , C12P19/62 , C12N15/54 , C12N15/62
CPC分类号： C07D498/18 , C07K2319/00 , C12N9/1029 , C12N9/1205 , C12N15/52 , C12P17/188 , C12P19/32
摘要： Host cells comprising recombinant vectors encoding the FK-520 polyketide synthase and FK-520 modification enzymes can be used to produce the FK-520 polyketide. Recombinant DNA constructs comprising one or more FK-520 polyketide synthase domains, modules, open reading frames, and variants thereof can be used to produce recombinant polyketide synthases and a variety of different polyketides with application as pharmaceutical and veterinary products.
摘要翻译：包含编码FK-520聚酮化合物合酶和FK-520修饰酶的重组载体的宿主细胞可用于生产FK-520聚酮化合物。包含一个或多个FK-520聚酮化合物合酶结构域，模块，开放阅读框及其变体的重组DNA构建体可用于生产重组聚酮化合物合酶和各种不同的聚酮化合物作为药物和兽药产品。

9. 发明申请

WO0131035A3 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：WO0131035A3
公开(公告)日：2001-11-22
申请号：PCT/US0029775
申请日：2000-10-27
申请人： KOSAN BIOSCIENCES INC
发明人： SANTI DANIEL , PECK LARRY , DAYEM LINDA , KEALEY JAMES
IPC分类号： C12N1/19 , C12N1/21 , C12N5/10 , C12N9/90 , C12N15/61 , C12P11/00 , C12P19/62
CPC分类号： C12N9/90 , C12P11/00 , C12P19/62
摘要： Recombinant host cells that comprise recombinant DNA expression vectors that drive expression of a product and a precursor for biosynthesis of that product can be used to produce useful products such as polyketides in host cells that do not naturally produce the product or produce the product or precursor at low levels due to the absence of the precursor or the presence of the precursor in rate limiting amounts.
摘要翻译：包含驱动产物表达的重组DNA表达载体和用于生物合成该产物的前体的重组宿主细胞可以用于在宿主细胞中产生有用的产物，例如聚酮化合物，所述产物不天然产生产物或产生产物或前体由于不存在前体或在速率限制量下存在前体，所以水平低。

10. 发明申请

WO2004019879A8 MOTILIDE COMPOUNDS 审中-公开
标题翻译：胶体化合物
公开(公告)号：WO2004019879A8
公开(公告)日：2004-07-29
申请号：PCT/US0326991
申请日：2003-08-26
申请人： KOSAN BIOSCIENCES INC
发明人： SANTI DANIEL , METCALF BRIAN , CARRERAS CHRISTOPHER , LIU YAOQUAN , MCDANIEL ROBERT , RODRIGUEZ EDUARDO J
IPC分类号： A61K31/35 , A61K31/7048 , A61P1/00 , C07D313/00 , C07H17/08 , C12N1/21 , C12N15/52 , C12P19/62 , A61K31/335
CPC分类号： C07H17/08 , C12N15/52 , C12P19/62
摘要： Motilide compounds having the formula (I), wherein R , R , R , and R are as defined herein, and methods for their preparation and use in the treatment of diseases or conditions characterized by impaired gastric motility.
摘要翻译：具有式（I）的其中R 1，R 2，R 3和R 4的术语化合物如本文所定义，以及其制备和用于治疗特征的疾病或病症的方法由胃运动受损。

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