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11. 发明授权

US08946405B2 Controlled release from solid supports 有权
标题翻译：从固体支持物控制释放
公开(公告)号：US08946405B2
公开(公告)日：2015-02-03
申请号：US13696300
申请日：2011-05-05
申请人： Gary Ashley , Daniel V. Santi
发明人： Gary Ashley , Daniel V. Santi
IPC分类号： A61K47/48 , A61K49/00 , A61L15/44 , A61L27/54 , A61L29/16 , A61L31/16
CPC分类号： A61K47/48215 , A61K47/58 , A61K47/60 , A61K47/6435 , A61K47/6903 , A61K47/6953 , A61K47/6957 , A61K49/0043 , A61K49/0054 , A61L15/44 , A61L27/54 , A61L29/16 , A61L31/16 , A61L2300/252 , A61L2300/258
摘要： The invention relates to solid supports useful in medical applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the solid support through a linkage that releases the drug or a prodrug through controlled beta elimination.
摘要翻译：本发明涉及用于医疗应用中的固体支持物，其提供药物如肽，核酸和小分子的受控释放。这些药物通过通过控制β消除释放药物或前药的连接共价偶联到固体支持物上。

12. 发明申请

US20050233431A1 Recombinant narbonolide polyketide synthase 审中-公开
标题翻译：重组纳博内酯聚酮化合物合成酶
公开(公告)号：US20050233431A1
公开(公告)日：2005-10-20
申请号：US10846335
申请日：2004-05-14
申请人： Gary Ashley , Melanie Betlach , Mary Betlach , Robert McDaniel , Li Tang
发明人： Gary Ashley , Melanie Betlach , Mary Betlach , Robert McDaniel , Li Tang
IPC分类号： C07B61/00 , C07D323/00 , C07H17/08 , C12N1/21 , C12N9/14 , C12N15/52 , C12N15/65 , C12P17/08 , C12P19/62 , C12N9/16 , C07H21/04 , C12N15/74
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。

13. 发明授权

US06927057B2 Macrolide analogs 失效
标题翻译：大环内酯类似物
公开(公告)号：US06927057B2
公开(公告)日：2005-08-09
申请号：US09859854
申请日：2001-05-16
申请人： Chaitan Khosla , Gary Ashley , Camilla M. Kao , Robert McDaniel
发明人： Chaitan Khosla , Gary Ashley , Camilla M. Kao , Robert McDaniel
IPC分类号： C07B61/00 , C07D309/36 , C07D311/92 , C07D323/00 , C07D407/06 , C07H17/08 , C12N9/00 , C12N15/52 , C12P7/26 , C12P17/06 , C12P17/16 , C12P1/00
CPC分类号： C07D407/06 , C07D309/36 , C07D311/92 , C07D323/00 , C07H17/08 , C12N9/93 , C12N15/52 , C12P7/26 , C12P17/06 , 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.
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。此外，使用该方法制备新的聚酮化合物和抗生素。

14. 发明申请

US20050038086A1 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：US20050038086A1
公开(公告)日：2005-02-17
申请号：US10845467
申请日：2004-05-12
申请人： Gary Ashley , Robert Arslanian , John Carney , Brian Metcalf , Li Tang
发明人： Gary Ashley , Robert Arslanian , John Carney , Brian Metcalf , Li Tang
IPC分类号： C07D313/00 , C07D405/06 , C07D413/06 , C07D417/06 , C07D491/04 , C12N1/20 , C12N9/00 , C12N15/52 , C12N15/74 , C12P17/16 , C12P17/18 , C07D417/02 , A61K31/427
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 R1, R2, R3, R4, R5, 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。

15. 发明申请

US20050032176A1 Modular polyketide synthases with altered activity 审中-公开
标题翻译：具有改变活性的模块化聚酮化合物合酶
公开(公告)号：US20050032176A1
公开(公告)日：2005-02-10
申请号：US10850308
申请日：2004-05-19
申请人： Chaitan Khosla , Gary Ashley , Hong Fu , Camilla Kao , Robert McDaniel
发明人： Chaitan Khosla , Gary Ashley , Hong Fu , Camilla Kao , Robert McDaniel
IPC分类号： C12N15/09 , C07B61/00 , C07D309/36 , C07D309/38 , C07D311/02 , C07D311/86 , C07D311/92 , C07D323/00 , C07D407/06 , C07H17/08 , C12N1/15 , C12N1/21 , C12N9/00 , C12N15/52 , C12P7/26 , C12P17/06 , C12P17/08 , C12P17/16 , C12R1/465 , C12P19/60 , C07H21/04 , C12N9/10 , C12N15/74 , C12Q1/68
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： The substrate specificity of modular polyketide synthases is altered by mutating or replacing acyltransferase regions thereof.
摘要翻译：模块化聚酮化合物合成酶的底物特异性通过突变或替换其酰基转移酶区而改变。

16. 发明授权

US06593302B2 Macrolide antiinfective agents 有权
标题翻译：大环内酯类抗感染药
公开(公告)号：US06593302B2
公开(公告)日：2003-07-15
申请号：US10075466
申请日：2002-02-13
申请人： Daniel Chu , Gary Ashley
发明人： Daniel 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 (5-20C); 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）; 取代或未取代的芳基烷基（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。

17. 发明授权

US06503741B1 Polyketide synthase genes from Streptomyces venezuelae 失效
标题翻译：来自维他命C链球菌的聚酮化合物合成酶基因
公开(公告)号：US06503741B1
公开(公告)日：2003-01-07
申请号：US09141908
申请日：1998-08-28
申请人： Gary Ashley , Melanie C. Betlach , Mary Betlach , Robert McDaniel , Li Tang
发明人： Gary Ashley , Melanie C. Betlach , Mary Betlach , Robert McDaniel , Li Tang
IPC分类号： C12N900
CPC分类号： C12N9/14 , C12N15/65
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 picromycin. The combinatorial library is useful as a source of pharmaceutically active compounds. In addition, novel polyketides and antibiotics are prepared using this method.
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的聚酮化合物合酶基因簇（例如编码picromycin的PKS的簇）来获得。组合文库可用作药物活性化合物的来源。此外，使用该方法制备新的聚酮化合物和抗生素。

18. 发明授权

US08703907B2 Controlled drug release from dendrimers 有权
标题翻译：受控药物从树枝状大分子释放
公开(公告)号：US08703907B2
公开(公告)日：2014-04-22
申请号：US13696301
申请日：2011-05-05
申请人： Gary Ashley , Daniel V. Santi
发明人： Gary Ashley , Daniel V. Santi
IPC分类号： A61K38/26 , A61K38/28 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , A61K38/00 , A61K38/04
CPC分类号： A61K47/48315 , A61K38/2242 , A61K38/26 , A61K38/50 , A61K47/60 , A61K47/641 , A61K47/645 , C08G83/003 , C08G83/004
摘要： The invention relates to compositions that comprise dendrimers useful in medical and veterinary applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the dendrimer through a linkage that releases the drug or a prodrug through controlled beta elimination.
摘要翻译：本发明涉及包含用于医学和兽医学应用中的树枝状大分子的组合物，其提供药物（例如肽，核酸和小分子）的受控释放。这些药物通过通过对照β消除释放药物或前药的连接共价偶联到树状聚合物上。

19. 发明申请

US20130116407A1 CONTROLLED RELEASE FROM MACROMOLECULAR CONJUGATES 有权
标题翻译：从大分子结合物的控制释放
公开(公告)号：US20130116407A1
公开(公告)日：2013-05-09
申请号：US13696299
申请日：2011-05-05
申请人： Gary Ashley , Daniel V. Santi
发明人： Gary Ashley , Daniel V. Santi
IPC分类号： A61K47/48
CPC分类号： A61K47/48215 , A61K9/0019 , A61K9/08 , A61K47/54 , A61K47/60 , C07D487/04 , C07D491/22
摘要： The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates.
摘要翻译：本发明涉及大分子载体的缀合物和包含通过速率控制的β-消除释放药物或前药的接头的药物，以及制备和使用缀合物的方法。

20. 发明授权

US06984515B2 Macrolide analogs 失效
标题翻译：大环内酯类似物
公开(公告)号：US06984515B2
公开(公告)日：2006-01-10
申请号：US09852416
申请日：2001-05-09
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： C12Q1/00 , C12P1/00
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： A polyketide or glycosylated polyketide which has the formula: wherein R* is methyl or ethyl; each of R1-R6 is methyl; X1 is OH or H; and/or X2 is=O, OH or H; X3 is OH or H; X4 is OH or H; a pi bond is present at positions 10-11, 8-9, 4-5 and/or 2-3; and wherein at least one of the following characteristics is present: X1 is H; X2 is OH or H; X3 is H; X4 is H; or a pi bond is present at positions 10-11, 8-9, 4-5 and/or 2-3.
摘要翻译：具有下式的聚酮化合物或糖基化聚酮化合物：其中R *是甲基或乙基; R 1〜R 6中的每一个为甲基; X 1是OH或H; 和/或X 2是= O，OH或H; X 3是OH或H; X 4是OH或H; 位置10-11,8-9,4-5和/或2-3存在π键; 并且其中存在以下特征中的至少一个：X 1是H; X 2是OH或H; X 3是H; X 4是H; 或者π键存在于位置10-11,8-9,4-5和/或2-3处。

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