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31. 发明授权

US06750205B2 Motilide compounds 有权
标题翻译：化合物
公开(公告)号：US06750205B2
公开(公告)日：2004-06-15
申请号：US10409429
申请日：2003-04-07
申请人： Gary Ashley , Mark Burlingame , Christopher Carreras , Daniel Santi
发明人： Gary Ashley , Mark Burlingame , Christopher Carreras , Daniel Santi
IPC分类号： A61K3170
CPC分类号： C07H17/08
摘要： The present invention provides novel macrolide compounds of the formulas wherein: R is hydroxyl or methoxy; R1 is selected from the group consisting of hydrogen, hydroxyl, halide, NH2, OR9, where R9 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or heteroaryl and R10 and R11 are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or aryl; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, alkylaryl, alkenylaryl alkynylaryl or R2 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：本发明提供下式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，其中R 9是C 1 -C 10 烷基，C 2 -C 10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，烷基芳基，烯基芳基炔基芳基或R 2和R 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，并且它们连接的碳形成环状碳酸酯; 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 5一起形成的碳原子和它们所连接的碳原子形成环状碳酸酯; 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，酰氨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，链烯基芳基，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; x是单键或双键。

32. 发明授权

US06280999B1 Sorangium polyketide synthases and encoding DNA therefor 失效
标题翻译：山梨聚酮化合物合成酶并编码DNA
公开(公告)号：US06280999B1
公开(公告)日：2001-08-28
申请号：US09144085
申请日：1998-08-31
申请人： Claes Gustafsson , Mary C. Betlach , Gary Ashley , Bryan Julien , Rainer Ziermann
发明人： Claes Gustafsson , Mary C. Betlach , Gary Ashley , Bryan Julien , Rainer Ziermann
IPC分类号： C12N120
CPC分类号： C12N9/1029 , C12N9/0006 , C12N15/52
摘要： Novel Sorangium polyketide synthases, and domains thereof, and polynucleotides encoding therefor. Additionally, chimeric polyketide synthases that include domains, or subsets of domains, patterned on said novel polyketide synthases. Methods to prepare polyketide combinatorial libraries are described, as are recombinant host cells in which polyketides are produced.
摘要翻译：新型Sorangium polyketide synthase及其结构域，以及编码它们的多核苷酸。另外，嵌合聚酮化合物合酶包括在所述新型聚酮化合物合成酶上图案化的结构域或结构域。描述了制备聚酮化合物组合文库的方法，以及其中产生聚酮化合物的重组宿主细胞。

33. 发明申请

US20060148052A1 Production of polyketides in bacteria and yeast 审中-公开
公开(公告)号：US20060148052A1
公开(公告)日：2006-07-06
申请号：US11260661
申请日：2005-10-27
申请人： Philip Barr , Daniel Santi , Gary Ashley , Rainer Ziermann
发明人： Philip Barr , Daniel Santi , Gary Ashley , Rainer Ziermann
IPC分类号： C12P7/26 , C12N1/21
CPC分类号： C12N9/1288 , A01K2217/05 , C07K2319/00 , C12N9/00 , C12N9/1025 , C12N15/52 , C12N15/70 , C12N15/76 , C12N15/81 , C12P7/26 , C12P7/42 , C12P17/162 , C12P19/62
摘要： Hybrid and novel polyketide synthases and polyketides are produced by use of a multiple vector system. The combinatorial possibilities offered by placing the various catalytic activities of PKS systems on separate vectors permits the construction of improved libraries of PKS and polyketides. In addition, polyketides can be produced in hosts that ordinarily do not produce polyketides by supplying, along with an expression system for the desired PKS, an expression system for holo ACP synthase.

34. 发明申请

US20060019371A1 Macrolide analogs 审中-公开
公开(公告)号：US20060019371A1
公开(公告)日：2006-01-26
申请号：US11036315
申请日：2005-01-14
申请人： Chaitan Khosla , Gary Ashley , Camilla Kao , Robert McDaniel
发明人： Chaitan Khosla , Gary Ashley , Camilla Kao , Robert McDaniel
IPC分类号： A61K31/7048 , C07H17/08 , C12N1/20
CPC分类号： C07D309/36 , C07D311/92 , C07D313/00 , C07D323/00 , C07D407/06 , C07H17/08 , C12N9/93 , C12N15/52 , C12P7/26 , C12P17/06 , C12P17/08 , C12P17/162 , 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.

35. 发明授权

US06710189B2 Method to produce novel polyketides 失效
标题翻译：生产新型聚酮化合物的方法
公开(公告)号：US06710189B2
公开(公告)日：2004-03-23
申请号：US10187333
申请日：2002-06-28
申请人： Chaitan Khosla , Rembert Pieper , Guanglin Luo , David E. Cane , Camilla Kao , Gary Ashley
发明人： Chaitan Khosla , Rembert Pieper , Guanglin Luo , David E. Cane , Camilla Kao , Gary Ashley
IPC分类号： C07D31316
CPC分类号： C07H17/08 , C12N15/52 , C12P17/06 , C12P17/08
摘要： A polyketide, or an antibiotic which is obtainable from the polyketide by a method comprising treating the polyketide with a culture medium conditioned by Saccharopolyspora erythraea, selected from the group consisting of:
摘要翻译：聚酮化合物或抗生素，其可以通过包括用由糖酵母调节的培养基处理所述聚酮化合物的方法获得，所述培养基选自由以下组成的组：

36. 发明授权

US06670389B2 Laulimalide derivatives 有权
公开(公告)号：US06670389B2
公开(公告)日：2003-12-30
申请号：US10071839
申请日：2002-02-08
申请人： Gary Ashley , Brian Metcalf
发明人： Gary Ashley , Brian Metcalf
IPC分类号： C07D41706
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.

37. 发明授权

US06562795B2 Motilide compounds 有权
标题翻译：化合物
公开(公告)号：US06562795B2
公开(公告)日：2003-05-13
申请号：US09788314
申请日：2001-02-15
申请人： Gary Ashley , Mark Burlingame , Christopher Carreras , Daniel Santi
发明人： Gary Ashley , Mark Burlingame , Christopher Carreras , Daniel Santi
IPC分类号： A61K3170
CPC分类号： C07H17/08
摘要： The present invention provides novel macrolide compounds of the formulas wherein: R is hydroxyl or methoxy; R1 is selected from the group consisting of hydrogen, hydroxyl, halide, NH2, OR9, where R9 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or heteroaryl and R10 and R11 are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or aryl; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, alkylaryl, alkenylaryl, alkynylaryl or R2 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：本发明提供下式的新型大环内酯化合物，其中R为羟基或甲氧基; R 1选自氢，羟基，卤素，NH 2，OR 9，其中R 9为C 1 -C 10烷基，C 2 -C 10烯基， C10炔基，芳基或杂芳基，R10和R11各自独立地为氢，C1-C10烷基，C2-C10烯基，C2-C10炔基或芳基; R2和R3各自独立地选自氢，C1-C10 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和R 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原子形成环状碳酸酯; 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和它们所连接的碳一起形成环状碳酸酯; 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，链烯基芳基，芳基芳基，酰氨基烷基芳基，酰胺基烯基芳基或酰氨基炔基芳基; R8是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胺基炔基芳基; x是单键或双键。

38. 发明授权

US06489314B1 Epothilone derivatives and methods for making and using the same 有权
标题翻译：埃坡霉素衍生物及其制备和使用方法
公开(公告)号：US06489314B1
公开(公告)日：2002-12-03
申请号：US09825856
申请日：2001-04-03
申请人： Gary Ashley , Brian Metcalf
发明人： Gary Ashley , Brian Metcalf
IPC分类号： A61K3133
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： The present invention relates to 16-membered macrocyclic compounds. In one aspect of the present invention, compounds of the formula are provided wherein: R1, R2, R3, and R5 are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or alkylaryl; R4 is hydrogen, halogen, C1-C10 alkyl, C1-C10 hydroxyalkyl, C1-C10 haloalkyl, aryl, —C(═O)R6, —C(═O)OR6, —NR6R7 where R6 and R7 are each independently hydrogen, C1-C10 aliphatic, aryl or alkylaryl; W is O, NR8 where R8 is hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or alkylaryl; X is O, CH2 or a carbon-carbon double bond; Y is absent or a C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl; and Ar is aryl; provided that 10,11-dehydroepothilone C is excluded.
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，提供下列化合物，其中：R1，R2，R3和R5各自独立地为氢，C1-C10烷基，C2-C10烯基，C2-C10炔基，芳基或烷基芳基; R4为氢卤素，C 1 -C 10烷基，C 1 -C 10羟基烷基，C 1 -C 10卤代烷基，芳基，-C（= O）R 6，-C（= O）OR 6，-NR 6 R 7，其中R 6和R 7各自独立地为氢，脂族，芳基或烷基芳基; W是O，NR8，其中R8是氢，C1-C10烷基，C2-C10烯基，C2-C10炔基，芳基或烷基芳基; X是O，CH2或碳 - 碳双键; Y是不存在或C 1 -C 10烷基，C 2 -C 10烯基或C 2 -C 10炔基; 且Ar为芳基; 条件是排除了10,11-脱氢抗坏血酸酮C.

39. 发明授权

US06395710B1 Macrolide antiinfective agents 有权
标题翻译：大环内酯类抗感染药
公开(公告)号：US06395710B1
公开(公告)日：2002-05-28
申请号：US09550045
申请日：2000-04-14
申请人： Daniel T. W. Chu , Gary Ashley
发明人： Daniel T. W. Chu , Gary Ashley
IPC分类号： A61K3170
CPC分类号： C07H17/08 , Y02P20/55
摘要： Compounds of the formula wherein Ra is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20); or ORa is replaced by H; Rb is H or halogen; Rc is H or a protecting group; Rd is methyl, unsubstituted alkyl (3-10C); substituted alkyl (1-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); substituted or unsubstituted arylalkenyl (5-20C); substituted or unsubstituted arylalkynyl (5-20C); substituted or unsubstituted amidoarylalkyl (5-20C); substituted or unsubstituted amidoarylalkenyl (5-20C); or substituted or unsubstituted amidoarylalkynyl (5-20C); Re is H or a protecting group; L is methylene or carbonyl; T is —O—, —N(R)—, —N(OR)—, —N(NHCOR)—, —N(N═CHR)—, or —N(NHR)— wherein R is H or Ra as defined above, with the proviso that when L is methylene, T is —O—; one of Z and Y is H and the other is OH, protected OH, or amino, mono- or dialkylamino, protected amino, or an amino heterocycle or Z and Y together are ═O, ═NOH or a derivatized oxime; including any pharmaceutically acceptable salts thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof, are antimicrobial agents.
摘要翻译：化学式R a的化合物是H; 取代或未取代的烷基（1-10C）; 取代或未取代的烯基（2-10C）; 取代或未取代的炔基（2-10C）; 取代或未取代的芳基（4-14C）; 取代或未取代的芳烷基（5-20）; 或ORa被H代替; Rb是H或卤素; Rc是H或保护基; Rd是甲基，未取代的烷基（3-10C）; 取代的烷基（1-10C）; 取代或未取代的炔基（2-10C）; 取代或未取代的芳基（4-14C）; 取代或未取代的芳基烷基（5-20℃）; 取代或未取代的芳基烯基（5-20℃）; 取代或未取代的芳基炔基（5-20℃）; 取代或未取代的酰氨基芳基烷基（5-20℃）; 取代或未取代的酰氨基芳基烯基（5-20℃）; 或取代或未取代的酰氨基芳基炔基（5-20℃）; Re是H或保护基; L是亚甲基或羰基; T是-O-，-N（R） - ， - N（OR） - ， - N（NHCOR） - ，-N（N = CHR） - 或-N（NHR） - ，其中R是如上定义的H或Ra，条件是当L是亚甲基时，T是-O-; Z和Y之一是H 另一个是OH，保护的OH或氨基，单或二烷基氨基，保护的氨基或氨基杂环，或Z和Y一起为= O，= NOH或衍生的肟;包括其任何药学上可接受的盐和任何立体异构形式，其立体异构形式的混合物是抗微生物剂。

40. 发明授权

US06391594B1 Modified modular PKS with retained scaffold 失效
标题翻译：具有保留支架的改进的模块化PKS
公开(公告)号：US06391594B1
公开(公告)日：2002-05-21
申请号：US08846247
申请日：1997-04-30
申请人： Chaitan Khosla , Gary Ashley , Hong Fu , Camilla M. Kao , Robert McDaniel
发明人： Chaitan Khosla , Gary Ashley , Hong Fu , Camilla M. Kao , Robert McDaniel
IPC分类号： C12N1564
CPC分类号： C12N9/93 , C07D309/36 , C07D311/92 , C07D323/00 , C07D407/06 , C07H17/08 , C12N15/52 , C12P7/26 , C12P17/06 , C12P17/08 , C12P17/162 , 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.
摘要翻译：聚酮化合物的组合文库可以通过适当操作宿主模块化聚酮化合物合成酶基因簇（例如编码红霉素的PKS的簇）来获得。组合文库可用作药物活性化合物的来源。

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