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1. 发明授权

US08003687B2 Esters of compounds in the leptomycin family 有权
标题翻译：雷伯霉素家族中化合物的酯类
公开(公告)号：US08003687B2
公开(公告)日：2011-08-23
申请号：US11991879
申请日：2006-09-11
申请人： Steven D. Dong , Daniel V. Santi
发明人： Steven D. Dong , Daniel V. Santi
IPC分类号： A01N43/16 , A61K31/35 , C07D309/38
CPC分类号： C07D309/32 , C07D405/12
摘要： Esters of compounds in the leptomycin family, having a structure according to formula I where R, R10, R11, R12, R13, and R14 are as defined herein, exhibit anti-tumor properties.
摘要翻译：具有根据式I的结构的灵霉素家族中的化合物的酯，其中R，R10，R11，R12，R13和R14如本文所定义，表现出抗肿瘤性质。

2. 发明授权

US07655808B2 Leptomycin compounds 有权
标题翻译：洛泊霉素化合物
公开(公告)号：US07655808B2
公开(公告)日：2010-02-02
申请号：US12241218
申请日：2008-09-30
申请人： Steven D. Dong , Daniel V. Santi , David C. Myles , Brian Hearn
发明人： Steven D. Dong , Daniel V. Santi , David C. Myles , Brian Hearn
IPC分类号： C07D413/00 , C07D309/30
CPC分类号： C07D407/12 , C07D309/32 , C07D405/12 , C07D409/12 , C07D487/04
摘要： Leptomycin-type compounds according to formula I wherein R0, R1, R2, R10, R11, R12, R13, R14, and m are as defined herein, exhibit anti-tumor activity.
摘要翻译：其中R 0，R 1，R 2，R 10，R 11，R 12，R 13，R 14和m如本文所定义的根据式I的曲霉霉素化合物显示抗肿瘤活性。

3. 发明申请

US20100222382A1 Esters of Compounds in the Leptomycin Family 有权
标题翻译：氯霉素家族中化合物的酯类
公开(公告)号：US20100222382A1
公开(公告)日：2010-09-02
申请号：US11991879
申请日：2006-09-11
申请人： Steven D Dong , Daniel V. Santi
发明人： Steven D Dong , Daniel V. Santi
IPC分类号： A61K31/366 , C07D309/38 , C07D405/12 , A61P35/00 , A61P35/02 , A61K31/4709
CPC分类号： C07D309/32 , C07D405/12
摘要： Esters of compounds in the leptomycin family, having a structure according to formula I where R, R10, R11, R12, R13, and R14 are as defined herein, exhibit anti-tumor properties.
摘要翻译：具有根据式I的结构的灵霉素家族中的化合物的酯，其中R，R10，R11，R12，R13和R14如本文所定义，表现出抗肿瘤性质。

4. 发明申请

US20130123461A1 CONTROLLED DRUG RELEASE FROM DENDRIMERS 有权
标题翻译：控制药物从DENDRIMERS发布
公开(公告)号：US20130123461A1
公开(公告)日：2013-05-16
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： A61K47/48
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。

5. 发明授权

US07214708B2 Synthetic discodermolide analogs 有权
标题翻译：合成discodermolide类似物
公开(公告)号：US07214708B2
公开(公告)日：2007-05-08
申请号：US11261686
申请日：2005-10-28
申请人： Kurt F. Sundermann , Simon James Shaw , Daniel V. Santi
发明人： Kurt F. Sundermann , Simon James Shaw , Daniel V. Santi
IPC分类号： A01N43/16 , A61K31/35 , C07D309/00 , C07D407/00 , C07D309/30
CPC分类号： C07D309/30 , C07D307/33
摘要： Synthetic discodermolide analogs having utility as antiproliferative agents, having a structure represented by formula A where RA through RE and XA are as defined herein.
摘要翻译：具有用作抗增殖剂的合成的discodermolide类似物，其具有由式A表示的结构，其中R A至R E和X A A的定义如本文所定义。

6. 发明授权

US06258566B1 Production of polyketides in bacteria and yeast 有权
标题翻译：在细菌和酵母中生产聚酮化合物
公开(公告)号：US06258566B1
公开(公告)日：2001-07-10
申请号：US09422073
申请日：1999-10-21
申请人： Philip J. Barr , Daniel V. Santi , Gary W. Ashley , Rainer Ziermann
发明人： Philip J. Barr , Daniel V. Santi , Gary W. Ashley , Rainer Ziermann
IPC分类号： C12P1962
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 (PKSs) 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 acyl carrier protein (ACP) synthase.
摘要翻译：通过使用多重载体系统产生杂合和新型聚酮化合物合酶（PKS）和聚酮化合物。通过将PKS系统的各种催化活性放置在单独的载体上提供的组合可能性允许构建改进的PKS和聚酮化合物库。此外，聚酮化合物可以在通常不通过供应所需的PKS的表达系统，全酰酰基载体蛋白（ACP）合酶的表达系统）的情况下产生聚酮化合物的宿主中生产。

7. 发明授权

US6075121A Modified peptide and peptide libraries with protease resistance, derivatives thereof and methods of producing and screening such 失效
标题翻译：具有蛋白酶抗性的修饰肽和肽文库，其衍生物以及生产和筛选方法
公开(公告)号：US6075121A
公开(公告)日：2000-06-13
申请号：US438436
申请日：1995-05-10
申请人： Reyna J. Simon , Paul A. Bartlett , Daniel V. Santi
发明人： Reyna J. Simon , Paul A. Bartlett , Daniel V. Santi
IPC分类号： A61K38/00 , A61K47/48 , B01J19/00 , C07H21/00 , C07K1/04 , C07K5/02 , C07K7/02 , C07K14/00 , C40B40/10 , C40B60/14
CPC分类号： C07H21/00 , A61K47/48238 , B01J19/0046 , C07K1/045 , C07K1/047 , C07K14/001 , C07K5/0207 , C07K7/02 , A61K38/00 , B01J2219/00283 , B01J2219/00286 , B01J2219/00308 , B01J2219/00416 , B01J2219/00418 , B01J2219/00423 , B01J2219/00466 , B01J2219/00493 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/00691 , B01J2219/00725 , C07B2200/11 , C40B40/10 , C40B60/14
摘要： Peptoids are provided which are polymers comprised of monomer units wherein the monomer units include at least some substitute amino acids and may include conventional amino acids. The peptoids can be synthesized in large numbers so as to provide libraries of peptoids which can be screened in order to isolate peptoids of desired biological activity. Although the peptoids may include amino acids, they preferably include only substituted amino acids and are designed in a manner so as to have a particular biological activity. Certain peptoids are designed to mimic as closely as possible the activity of known proteins. Other peptoids are designed so as to have greater or lesser activity than known proteins and may be designed so as to block known receptor sites and/or elicit a desired immunogenic response and thereby act as vaccines. In that the peptoids are comprised of substitute amino acids they can be designed to have structures which natural proteins cannot conform to. A range of different amino acid substitutes are disclosed, as are their methods of synthesis and methods of using such amino acid substitutes in the synthesis of peptoids and peptoid libraries. Methods of screening the libraries in order to obtain desired peptoids of a particular biological activity are also disclosed. The peptoids are preferably linked to a pharmaceutically active drug forming a conjugate with increased binding affinity to a particular biological receptor site.
摘要翻译：提供了由单体单元组成的聚合物，其中单体单元包括至少一些替代氨基酸并且可以包括常规氨基酸。可以大量合成拟肽，以便提供可以筛选的拟肽文库，以分离所需生物活性的拟肽。虽然拟肽可以包括氨基酸，但它们优选仅包括取代的氨基酸，并且以具有特定生物活性的方式设计。某些拟肽被设计为尽可能模拟已知蛋白质的活性。其他拟肽被设计为具有比已知蛋白质更大或更小的活性，并且可以被设计成阻断已知的受体位点和/或引发所需的免疫原性应答并由此作为疫苗。因为拟肽由替代氨基酸组成，它们可被设计成具有天然蛋白质不能符合的结构。公开了一系列不同的氨基酸替代物，以及它们的合成方法以及在合成拟肽和拟肽文库中使用这种氨基酸替代物的方法。还公开了为了获得特定生物活性所需的拟肽而筛选文库的方法。拟肽优选与形成具有对特定生物受体位点的增加的结合亲和力的缀合物的药学活性药物连接。

8. 发明授权

US5840841A Method and apparatus for biopolymer synthesis 失效
标题翻译：用于生物聚合物合成的方法和装置
公开(公告)号：US5840841A
公开(公告)日：1998-11-24
申请号：US853066
申请日：1997-05-08
申请人： Ronald N. Zuckermann , Verena D. Heubner , Daniel V. Santi , Michael A. Siani
发明人： Ronald N. Zuckermann , Verena D. Heubner , Daniel V. Santi , Michael A. Siani
IPC分类号： B01J19/00 , C07H21/00 , C07K1/04 , C07K7/08 , C07K14/575 , C07K16/00 , C40B40/06 , C40B40/10 , C40B60/14 , C07K1/02 , C07H21/04 , C07K1/06
CPC分类号： C07H21/00 , B01J19/0046 , C07K1/045 , C07K1/047 , B01J2219/00283 , B01J2219/00286 , B01J2219/00308 , B01J2219/00416 , B01J2219/00418 , B01J2219/00423 , B01J2219/00466 , B01J2219/00493 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/00691 , B01J2219/00722 , B01J2219/00725 , C40B40/06 , C40B40/10 , C40B60/14
摘要： Method and apparatus for synthesizing biopolymers, such as polypeptides and polynucleotides. The apparatus includes plural reaction vessels in which subunit coupling to biopolymers in a particle suspension is carried out. The vessels are connected to common valving structure for use in mixing the suspension and removing suspension liquid. In one embodiment, a robotic arm in the apparatus is operable to transfer reaction solution to the reaction vessels, and to transfer particle suspensions from the reaction vessels to a mixing vessel and back to the reaction vessels. The method can be used to produce preferably equi-molar amounts of different-sequence biopolymers, such as polypeptides and polynucleotides.
摘要翻译：用于合成生物聚合物的方法和装置，例如多肽和多核苷酸。该装置包括多个反应容器，其中进行与颗粒悬浮液中的生物聚合物偶合的亚基。容器连接到公共阀结构，用于混合悬浮液并除去悬浮液。在一个实施例中，设备中的机器人手臂可操作以将反应溶液转移到反应容器中，并将颗粒悬浮液从反应容器转移到混合容器并返回到反应容器中。该方法可用于产生优选等摩尔量的不同序列生物聚合物，例如多肽和多核苷酸。

9. 发明授权

US5438119A Method of obtaining a peptide with desired target property 失效
标题翻译：获得具有所需靶特性的肽的方法
公开(公告)号：US5438119A
公开(公告)日：1995-08-01
申请号：US981759
申请日：1992-11-25
申请人： William J. Rutter , Daniel V. Santi
发明人： William J. Rutter , Daniel V. Santi
IPC分类号： A61K38/02 , C07K1/04 , C07K1/14 , C07K1/36 , C07K5/00 , C07K7/00 , G01N33/68 , A61K38/00 , C07K17/00
CPC分类号： C07K1/047 , C07K1/36 , G01N33/68
摘要： A method to obtain selected individual peptides or families thereof which have a target property and optionally to determine the amino acid sequence of a selected peptide or peptides to permit synthesis in practical quantities is disclosed. In general outline, the method of the invention comprises synthesizing a mixture of randomly or deliberately generated peptides using standard synthesis techniques, but adjusting the individual concentrations of the components of a mixture of sequentially added amino acids according to the coupling constants for each amino acid/amino acid coupling. The subgroup of peptides having the target property can then be selected, and either each peptide isolated and sequenced, or analysis performed on the mixture to permit its composition to be reproduced. Also included in the invention is an efficient method to determine the relevant coupling constants.
摘要翻译：公开了获得具有目标特性并任选地确定所选择的肽或肽的氨基酸序列以允许实际合成的所选单独肽或其家族的方法。总的来说，本发明的方法包括使用标准合成技术合成随机或故意产生的肽的混合物，但是根据每个氨基酸/偶联物的偶联常数调节相继添加的氨基酸的混合物的组分的个体浓度，氨基酸偶联。然后可以选择具有靶特性的肽亚组，并且分离和测序每个肽，或对混合物进行分析以允许其复制其组成。本发明还包括确定相关耦合常数的有效方法。

10. 发明授权

US5266684A Peptide mixtures 失效
标题翻译：肽混合物
公开(公告)号：US5266684A
公开(公告)日：1993-11-30
申请号：US525899
申请日：1990-05-18
申请人： William J. Rutter , Daniel V. Santi
发明人： William J. Rutter , Daniel V. Santi
IPC分类号： A61K38/02 , C07K1/04 , C07K1/14 , C07K1/36 , C07K5/00 , C07K7/00 , G01N33/68 , C07K1/08
CPC分类号： C07K1/047 , C07K1/36 , G01N33/68
摘要： A method to obtain selected individual peptides or families thereof which have a target property and optionally to determine the amino acid sequence of a selected peptide or peptides to permit synthesis in practical quantities is disclosed. In general outline, the method of the invention comprises synthesizing a mixture of randomly or deliberately generated peptides using standard synthesis techniques, but adjusting the individual concentrations of the components of a mixture of sequentially added amino acids according to the coupling constants for each amino acid/amino acid coupling. The subgroup of peptides having the target property can then be selected, and either each peptide isolated and sequenced, or analysis performed on the mixture to permit its composition to be reproduced. Also included in the invention is an efficient method to determine the relevant coupling constants.
摘要翻译：公开了获得具有目标特性并任选地确定所选择的肽或肽的氨基酸序列以允许实际合成的所选单独肽或其家族的方法。总的来说，本发明的方法包括使用标准合成技术合成随机或故意产生的肽的混合物，但是根据每个氨基酸/偶联物的偶联常数调节相继添加的氨基酸的混合物的组分的个体浓度，氨基酸偶联。然后可以选择具有靶特性的肽亚组，并且分离和测序每个肽，或对混合物进行分析以允许其复制其组成。本发明还包括确定相关耦合常数的有效方法。

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