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1. 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。

2. 再颁专利

USRE39836E1 Macrolide antinfective agents 有权
标题翻译：大环内酯类抗感染药
公开(公告)号：USRE39836E1
公开(公告)日：2007-09-11
申请号：US11182038
申请日：2005-07-13
申请人： Daniel Chu , Gary Ashley
发明人： Daniel Chu , Gary Ashley
IPC分类号： A61K31/70 , C07H17/08
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：下式的化合物其中R a a为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OR被替换为H; R b是H或卤素; R c是H或保护基; R d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℃）; R e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）如上所定义，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一起是-O，-NOH或衍生化的肟; 包括其任何药学上可接受的盐和其立体异构体形式及其立体异构形式的混合物均为抗微生物剂。

3. 发明授权

US06794366B2 Macrolide antiinfective agents 有权
标题翻译：大环内酯类抗感染药
公开(公告)号：US06794366B2
公开(公告)日：2004-09-21
申请号：US10124988
申请日：2002-04-17
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 or the 10,11-anhydro forms therefor, wherein Ra is H or OH; 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 alkenyl (2-10C) or 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 or is mono- or disubstituted amino carbonyl; Rf is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (1-10C); substituted or unsubstituted alkynyl (1-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); or —ORf may be replaced by —H; one of Z and Y is H and the other is OH or protected OH, or is amino, mono- or dialkyl-amino, protected amino, or an aminoheterocycle 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：式的化合物或其形成的10,11-脱氢，其中R a是H或OH; Rb是H或卤素; R c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）; 取代或未取代的烯基（2-10C）或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为H或保护基团或为单或二取代氨基羰基; Rf为H; 取代或未取代的烷基（1-10C）; 取代或未取代的烯基（1-10C）; 取代或未取代的炔基（1-10C）; 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-OR f可以被-H取代; Z和Y之一是H，另一个是OH或保护的OH，或者是氨基，单或二烷基氨基，保护的氨基或氨基杂环，或者Z和Y一起是= O ，= NOH或衍生化的肟，包括其任何药学上可接受的盐和任何立体异构形式及其立体异构形式的混合物，均为抗微生物剂。

4. 发明授权

US08754190B2 Controlled release from macromolecular conjugates 有权
标题翻译：从大分子缀合物的控制释放
公开(公告)号：US08754190B2
公开(公告)日：2014-06-17
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： A61K38/06 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07D487/00 , C07D491/00 , C07D513/00 , C07D239/02 , C07C247/00 , C07J41/00
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。

5. 发明申请

US20130123487A1 CONTROLLED RELEASE FROM SOLID SUPPORTS 有权
标题翻译：控制从固体支持的释放
公开(公告)号：US20130123487A1
公开(公告)日：2013-05-16
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
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。

6. 发明授权

US07070964B2 Epothilone compounds and methods for making the same 有权
标题翻译：埃坡霉素化合物及其制备方法
公开(公告)号：US07070964B2
公开(公告)日：2006-07-04
申请号：US10295342
申请日：2002-11-14
申请人： Li Tang , Brian Metcalf , Leonard Katz , Gary Ashley
发明人： Li Tang , Brian Metcalf , Leonard Katz , Gary Ashley
IPC分类号： C12P17/00
CPC分类号： C07D417/06 , C07D493/04 , C07D493/08 , C12P17/167 , C12P17/181
摘要： The present invention provides bioconversion methods for making epothilone analogs. These analogs differ from the starting material by the addition of one or more hydroxyl groups or by the addition of an epoxide. These compounds, in turn, can be further modified by chemical synthesis.
摘要翻译：本发明提供用于制备埃坡霉素类似物的生物转化方法。这些类似物通过加入一个或多个羟基或通过加入环氧化物与原料不同。这些化合物又可以通过化学合成进一步改性。

7. 发明授权

US07049100B2 Multi-plasmid method for preparing large libraries of polyketides and non-ribosomal peptides 有权
公开(公告)号：US07049100B2
公开(公告)日：2006-05-23
申请号：US10104417
申请日：2002-03-22
申请人： Daniel V. Santi , Qun Xue , Gary Ashley
发明人： Daniel V. Santi , Qun Xue , Gary Ashley
IPC分类号： C12P19/62 , C12N9/00
CPC分类号： C07H17/08 , A01K2217/05 , C07K2319/00 , C12N9/00 , C12N9/1025 , C12N9/1288 , C12N15/52 , C12N15/70 , C12N15/76 , C12N15/81 , C12P7/26 , C12P7/42 , 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.

8. 发明授权

US07022825B2 Polyketides and antibiotics 有权
标题翻译：聚酮化合物和抗生素
公开(公告)号：US07022825B2
公开(公告)日：2006-04-04
申请号：US10215964
申请日：2002-08-08
申请人： Gary Ashley , Isaac C. Chan-Kai , Mark A. Burlingame
发明人： Gary Ashley , Isaac C. Chan-Kai , Mark A. Burlingame
IPC分类号： C07H17/08 , A16K31/7048 , C12P19/62
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 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。

9. 发明授权

US06590083B1 Ketolide antibacterials 有权
标题翻译：酮内酯抗菌剂
公开(公告)号：US06590083B1
公开(公告)日：2003-07-08
申请号：US09691540
申请日：2000-10-18
申请人： Dennis Hlasta , Todd C. Henninger , Eugene B. Grant , Chaitin Khosla , Daniel T. W. Chu , Gary Ashley
发明人： Dennis Hlasta , Todd C. Henninger , Eugene B. Grant , Chaitin Khosla , Daniel T. W. Chu , Gary Ashley
IPC分类号： C07H1708
CPC分类号： C07H17/08 , Y02P20/55
摘要： The present invention includes compounds of the formula wherein: X is hydrogen or halide; R2 is hydrogen, acyl, or a hydroxy protecting group; R6 is hydrogen, hydroxyl, or —ORa wherein Ra is a substituted or unsubstituted moiety selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; R13 is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; and, R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are useful for the treatment of bacterial and protozoal infections.
摘要翻译：本发明包括糠醛的化合物：X是氢或卤化物; R 2是氢，酰基或羟基保护基; R 6是氢，羟基或-OR a，其中R a是选自以下的取代或未取代的部分： C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，芳基，杂环基，芳基（C 1 -C 10）烷基，芳基（C 2 -C 10）烯基，芳基（C 2 -C 10）炔基，杂环（C 1 -C 10），杂环基（C 2 -C 10）烯基和杂环基（C 2 -C 10）炔基; R 13是氢或取代或未取代的部分，其中该部分选自甲基; C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，芳基，杂环基，芳基（C 1 -C 10）烷基，芳基（C 2 -C 10），杂环基（C 2 -C 10）烯基和杂环基（C 2 -C 10）炔基; C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，芳基，杂环基，芳基（C 1 -C 10）烷基，芳基（C 1 -C 10） C 2 -C 10）烯基，芳基（C 2 -C 10）炔基，杂环基（C 1 -C 10）烷基，杂环（C 2 -C 10）烯基和杂环（C 2 -C 10）炔基;及其药学上可接受的盐，酯和前药形式。这些化合物具有抗感染活性，可用于治疗细菌和原生动物感染。

10. 发明授权

US06492562B1 Racemic thioesters for production of polyketides 失效
标题翻译：用于生产聚酮化合物的外消旋硫酯
公开(公告)号：US06492562B1
公开(公告)日：2002-12-10
申请号：US09492733
申请日：2000-01-27
申请人： Gary Ashley , Isaac C. Chan-Kai , Mark A. Burlingame
发明人： Gary Ashley , Isaac C. Chan-Kai , Mark A. Burlingame
IPC分类号： C07C1100
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 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。

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