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1. 发明申请

WO2006127252A1 MOTILIDE COMPOUNDS 审中-公开
标题翻译：胶体化合物
公开(公告)号：WO2006127252A1
公开(公告)日：2006-11-30
申请号：PCT/US2006/017672
申请日：2006-05-08
申请人： KOSAN BIOSCIENCES INCORPORATED , LIU, Yaoquan , CARRERAS, Christopher , MYLES, David, C. , LI, Yong , SHAW, Simon, James , FU, Hong , CHEN, Yue , ZHENG, Hao , LI, Yandong , BURLINGAME, Mark, A.
发明人： LIU, Yaoquan , CARRERAS, Christopher , MYLES, David, C. , LI, Yong , SHAW, Simon, James , FU, Hong , CHEN, Yue , ZHENG, Hao , LI, Yandong , BURLINGAME, Mark, A.
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： C07H17/08
摘要： Compounds having a structure according to formula (I) where R A , R B , R C , R D , R E , and R F are as defined herein, are useful as prokinetic agents.
摘要翻译：具有式（I）结构的化合物其中R A，R B，R C，R D，D， R E和R F如本文所定义，可用作促动力剂。

2. 发明申请

WO2004101508A3 SYNTHETIC TECHNIQUES AND INTERMEDIATES FOR POLYHYDROXY DIENYL LACTONES AND MIMICS THEREOF 审中-公开
标题翻译：聚羟基二烯丙基内酯及其模拟物的合成工艺及中间体
公开(公告)号：WO2004101508A3
公开(公告)日：2005-03-03
申请号：PCT/US2004010272
申请日：2004-04-02
申请人： UNIV PENNSYLVANIA , MYLES DAVID C , BURLINGAME MARK , SHAW SIMON JAMES , SUNDERMANN KURT F , FREEZE BRIAN SCOTT , MARTIN IGNACIO BROUARD , HIROSE TOMOYASU , SMITH AMOS B
发明人： MYLES DAVID C , BURLINGAME MARK , SHAW SIMON JAMES , SUNDERMANN KURT F , FREEZE BRIAN SCOTT , MARTIN IGNACIO BROUARD , HIROSE TOMOYASU , SMITH AMOS B
IPC分类号： C07D20060101 , C07D309/10 , C07D309/30 , C07D309/32 , C07F9/28
CPC分类号： C07D309/30 , C07F9/5428 , C07F9/5442
摘要： Synthetic methods and intermediates useful in the preparation of lactone containing compounds such as discodermolide and compounds which mimic the chemical or biological activity of discodermolide are provided.
摘要翻译：提供了用于制备含内酯化合物如discodermolide的合成方法和中间体以及模拟discodermolide化学或生物活性的化合物。

3. 发明申请

WO2004101508A2 SYNTHETIC TECHNIQUES AND INTERMEDIATES FOR POLYHYDROXY DIENYL LACTONES AND MIMICS THEREOF 审中-公开
标题翻译：合成技术及其中间体的聚羟基二烯基酯及其衍生物
公开(公告)号：WO2004101508A2
公开(公告)日：2004-11-25
申请号：PCT/US2004/010272
申请日：2004-04-02
申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA , MYLES, David, C. , BURLINGAME, Mark , SHAW, Simon, James , SUNDERMANN, Kurt, F. , FREEZE, Brian, Scott , MARTÌN, Ignació, Brouard , HIROSE, Tomoyasu , SMITH, Amos, B.
发明人： MYLES, David, C. , BURLINGAME, Mark , SHAW, Simon, James , SUNDERMANN, Kurt, F. , FREEZE, Brian, Scott , MARTÌN, Ignació, Brouard , HIROSE, Tomoyasu , SMITH, Amos, B.
IPC分类号： C07D
CPC分类号： C07D309/30 , C07F9/5428 , C07F9/5442
摘要： Synthetic methods and intermediates useful in the preparation of lactone containing compounds such as discodermolide and compounds which mimic the chemical or biological activity of discodermolide are provided.
摘要翻译：提供了可用于制备含内酯化合物如discodermolide的合成方法和中间体以及模仿discodermolide的化学或生物活性的化合物。

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

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

WO0044717A2 SYNTHESIS OF OLIGOKETIDES 审中-公开
标题翻译：合成寡糖
公开(公告)号：WO0044717A2
公开(公告)日：2000-08-03
申请号：PCT/US0002397
申请日：2000-01-27
申请人： KOSAN BIOSCIENCES INC , ASHLEY GARY , CHAN KAI ISAAC CHU WAH , BURLINGAME MARK ALMA
发明人： ASHLEY GARY , CHAN-KAI ISAAC CHU-WAH , BURLINGAME MARK ALMA
IPC分类号： C12P17/08 , C07B53/00 , C07C327/30 , C07D209/48 , C07D213/55 , C07D239/38 , C07D277/20 , C07D277/30 , C07D307/16 , C12N1/20 , C40B40/02 , C40B40/04 , C40B50/00 , C40B50/06 , C07C327/00
CPC分类号： C07C327/30
摘要： Facile methods for preparing diketide and triketide thioesters are disclosed. The resulting thioesters may be used as intermediates in the synthesis of desired polyketides, and may contain functional groups which ultimately reside in side chains on the resulting polyketide and thus can be used further to manipulate the polyketide so as to form derivatives. The polyketides produced may also be tailored by glycosylation, hydroxylation and the like. New polyketides and their derivatives and tailored forms are thereby produced.
摘要翻译：公开了制备二酮化合物和三酮化物硫酯的简便方法。所得硫酯可用作合成所需聚酮化合物的中间体，并且可以含有最终存在于所得聚酮化合物上的侧链中的官能团，因此可以进一步用于操作聚酮化合物以形成衍生物。产生的聚酮化合物也可以通过糖基化，羟基化等来定制。由此生产新的聚酮化合物及其衍生物和定制的形式。

7. 发明申请

WO2007070536A3 7-QUINOLYL KETOLIDE ANTIBACTERIAL AGENTS 审中-公开
标题翻译： 7-QUINOLYL KETOLIDE抗菌剂
公开(公告)号：WO2007070536A3
公开(公告)日：2008-04-03
申请号：PCT/US2006047439
申请日：2006-12-12
申请人： KOSAN BIOSCIENCES INC , SHAW SIMON JAMES , ASHLEY GARY W , BURLINGAME MARK A
发明人： SHAW SIMON JAMES , ASHLEY GARY W , BURLINGAME MARK A
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： C07D405/14
摘要： 15-fluoroketolides of the formula (I): having improved activity and safety, compositions comprising them, and methods for their preparation and use in the treatment of bacterial infections.
摘要翻译：式（I）的15-氟代内酯：具有改善的活性和安全性，包含它们的组合物及其制备和用于治疗细菌感染的方法。

8. 发明申请

WO2007070536A2 7-QUINOLYL KETOLIDE ANTIBACTERIAL AGENTS 审中-公开
标题翻译： 7-喹诺酮类抗生素代谢物
公开(公告)号：WO2007070536A2
公开(公告)日：2007-06-21
申请号：PCT/US2006/047439
申请日：2006-12-12
申请人： KOSAN BIOSCIENCES INCORPORATED , SHAW, Simon, James , ASHLEY, Gary, W. , BURLINGAME, Mark, A.
发明人： SHAW, Simon, James , ASHLEY, Gary, W. , BURLINGAME, Mark, A.
IPC分类号： A61K31/7052
CPC分类号： C07D405/14
摘要： 15-fluoroketolides of the formula (I): having improved activity and safety, compositions comprising them, and methods for their preparation and use in the treatment of bacterial infections.
摘要翻译：式（I）的15-氟代内酯：具有改善的活性和安全性，包含它们的组合物及其制备和用于治疗细菌感染的方法。

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