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1. 发明授权

US08394914B2 Functional polyglycolide nanoparticles derived from unimolecular micelles 有权
公开(公告)号：US08394914B2
公开(公告)日：2013-03-12
申请号：US12460655
申请日：2009-07-22
申请人： Gregory L. Baker , Milton R. Smith, III , Erin Vogel
发明人： Gregory L. Baker , Milton R. Smith, III , Erin Vogel
IPC分类号： C08G63/08
CPC分类号： C08G63/08 , A61K9/1075 , A61K9/5153 , A61K47/34 , A61K47/6907 , A61K47/6931 , A61K47/6935 , B82Y5/00 , C08G63/6852
摘要： Poly(glycolide) polymers are disclosed. The polymers generally include a glycolide-based polymer backbone that includes one or more functional groups such as alkynyl groups, hydrophilic organic triazole groups, hydrophobic organic triazole groups (also including amphiphilic organic triazole groups), di-triazole organic crosslinking groups, and triazole-substituted drug derivatives. The alkynyl groups provide reactive sites for further functionalization of the polymer, for example by reaction with azide derivatives. The polymers can further encapsulate a drug for delivery to a patient (i.e., as compared to drug derivatives that are covalently attached to the polymer). The polymers can be in the form of thermodynamically stable unimolecular micelles or crosslinked nanoparticles. The polymer compositions are completely biodegradable and hold great potential for use in biomedical applications.

2. 发明授权

US07923528B2 Degradable 1,4-benzodioxepin-3-hexyl-2,5-dione monomer derived polymer with a high glass transition temperature 有权
标题翻译：具有高玻璃化转变温度的可降解的1,4-苯并二氧杂环庚烯-3-己基-2,5-二酮单体衍生的聚合物
公开(公告)号：US07923528B2
公开(公告)日：2011-04-12
申请号：US11980209
申请日：2007-10-30
申请人： Gregory L. Baker , Feng Jing , Milton R. Smith, III
发明人： Gregory L. Baker , Feng Jing , Milton R. Smith, III
IPC分类号： C08G63/08
CPC分类号： A61L27/18 , C08G63/06 , C08G63/065 , C08L2201/06
摘要： A homopolymer of 1,4-benzodioxepin-3-cyclohexyl-2,5-dione with a Tg of 120° C. Copolymers are also described. The polymers are useful for surgical and other applications where biodegradability is important.
摘要翻译： Tg为120℃的1,4-苯并二氧杂环庚烯-3-环己基-2,5-二酮的均聚物。也描述了共聚物。聚合物可用于生物降解性很重要的手术和其他应用。

3. 发明申请

US20100041902A1 Cyclic alkyl substituted glycolides and polylactides therefrom 失效
标题翻译：环烷基取代的乙交酯和聚交酯
公开(公告)号：US20100041902A1
公开(公告)日：2010-02-18
申请号：US12583635
申请日：2009-08-24
申请人： Gregory L. Baker , Feng Jing , Milton R. Smith, III
发明人： Gregory L. Baker , Feng Jing , Milton R. Smith, III
IPC分类号： C07D319/12
CPC分类号： C07D319/12 , C08G63/06 , C08G63/823 , C08L2203/02
摘要： Cyclic alkyl, particularly cyclohexyl, substituted glycolides and polylactides are described. The polylactides have a high glass transition temperature and improved clarity.
摘要翻译：描述了环状烷基，特别是环己基取代的乙交酯和聚交酯。聚丙交酯具有高玻璃化转变温度和改善的透明度。

4. 发明授权

US06958420B2 Synthesis of aminoarylboronic esters and substituted anilines from arenes via catalytic C-H activation/borylation/amination and uses thereof 有权
标题翻译：通过催化C-H活化/硼化/胺化合成氨基芳基硼酸酯和芳烃的取代苯胺及其用途
公开(公告)号：US06958420B2
公开(公告)日：2005-10-25
申请号：US10623196
申请日：2003-07-18
申请人： Robert E. Maleczka, Jr. , Milton R. Smith, III , Daniel Holmes
发明人： Robert E. Maleczka, Jr. , Milton R. Smith, III , Daniel Holmes
IPC分类号： C07F5/02
CPC分类号： C07F5/025
摘要： A process is described for synthesizing aminoarylboronic esters of the general formula wherein R, R2, and R3 are each an alkyl, aryl, vinyl, alkoxy, carboxylic esters, amides, or halogen; Ar is any variety of phenyl, naphthyl, anthracyl, heteroaryl; and R1 is alkyl, hydrogen, or aryl. The aminoarylboronic esters are produced via the metal-catalyzed coupling of arylboronic esters of the general formula wherein R and R1 are any non-interfering group and X is chloro, bromo, iodo, triflates, or nonaflates to amines (primary and secondary). In particular, a process is described for the synthesis of the aminoarylboronic esters via a step-wise or tandem process in which one catalytic event is a metal-catalyzed borylation and the other catalytic event is a metal-catalyzed amination.
摘要翻译：描述了用于合成通式的氨基芳基硼酸酯的方法，其中R 1，R 2和R 3各自为烷基，芳基，乙烯基，烷氧基，羧酸酯，酰胺，或卤素; Ar是任何各种苯基，萘基，蒽基，杂芳基; 并且R 1是烷基，氢或芳基。氨基芳基硼酸酯通过以下通式的芳基硼酸酯的金属催化偶合而制备：其中R和R 1是任何非干扰基团，X是氯，溴，碘，三氟甲磺酸酯或非卤化物，胺（初级和次级）。特别地，描述了通过逐步或串联方法合成氨基芳基硼酸酯的方法，其中一个催化事件是金属催化的硼化反应，另一个催化事件是金属催化的胺化。

5. 发明授权

US06878830B2 Catalytic boronate ester synthesis from boron reagents and hydrocarbons 有权
公开(公告)号：US06878830B2
公开(公告)日：2005-04-12
申请号：US10194809
申请日：2002-07-12
申请人： Milton R. Smith, III
发明人： Milton R. Smith, III
IPC分类号： B01J31/12 , B01J31/14 , B01J31/18 , B01J31/22 , B01J31/24 , B01J31/28 , C07C1/32 , C07C17/269 , C07F15/00 , C07F17/02 , C08G61/10 , C07D207/00
CPC分类号： C08G61/10 , B01J31/1805 , B01J31/181 , B01J31/22 , B01J31/2295 , B01J31/24 , B01J31/2404 , B01J31/2409 , B01J2231/4211 , B01J2531/822 , B01J2531/824 , B01J2531/827 , C07C1/321 , C07C17/269 , C07C2531/22 , C07F15/0033 , C07F15/004 , C07F15/0073 , C07F15/008 , C07F17/02 , C07C15/00 , C07C22/08 , C07C25/18
摘要： A process for producing a ring-substituted arene borane which comprises reacting a ring-substituted arene with an HB organic compound in the presence of a catalytically effective amount of an iridium or rhodium complex with three or more substituents, excluding hydrogen, bonded to the iridium or rhodium and a phosphorus organic ligand, which is at least in part bonded to the iridium or rhodium, to form the ring-substituted arene borane. Also provided are catalytic compounds for catalyzing the process comprising an iridium or rhodium complex with three or substituents, excluding hydrogen, bonded to the iridium or rhodium and optionally, a phosphorus organic ligand, which is at least in part bonded to the iridium or rhodium.

6. 发明授权

US06828466B2 Process for the synthesis of phenols from arenes 有权
标题翻译：从芳烃合成苯酚的方法
公开(公告)号：US06828466B2
公开(公告)日：2004-12-07
申请号：US10620122
申请日：2003-07-15
申请人： Robert E. Maleczka, Jr. , Milton R. Smith, III , Daniel Holmes , Feng Shi
发明人： Robert E. Maleczka, Jr. , Milton R. Smith, III , Daniel Holmes , Feng Shi
IPC分类号： C07C3700
CPC分类号： C07D213/68 , C07B41/02 , C07C37/50 , C07C41/26 , C07C67/31 , C07C213/00 , C07C69/88 , C07C69/92 , C07C215/76 , C07C39/27 , C07C43/23 , C07C39/28 , C07C39/245 , C07C39/32 , C07C39/07 , C07C39/24 , C07C39/30 , C07C69/84
摘要： A process to synthesize substituted phenols such as those of the general formula RR′R″Ar(OH) wherein R, R′, and R″ are each independently hydrogen or any group which does not interfere in the process for synthesizing the substituted phenol including, but not limited to, halo, alkyl, alkoxy, carboxylic ester, amine, amide; and Ar is any variety of aryl or hetroaryl by means of oxidation of substituted arylboronic esters is described. In particular, a metal-catalyzed C—H activation/borylation reaction is described, which when followed by direct oxidation in a single or separate reaction vessel affords phenols without the need for any intermediate manipulations. More particularly, a process wherein Ir-catalyzed borylation of arenes using pinacolborane (HBPin) followed by oxidation of the intermediate arylboronic ester by OXONE is described.
摘要翻译：合成取代酚的方法，例如通式为R'R''Ar（OH）的取代酚，其中R，R'和R“各自独立地为氢或任何不干扰合成取代基的方法的基团苯酚，包括但不限于卤素，烷基，烷氧基，羧酸酯，胺，酰胺; 并且描述了通过取代的芳基硼酸酯的氧化的任何种类的芳基或杂芳基。特别地，描述了金属催化的C-H活化/硼烷化反应，当在单个或单独的反应容器中直接氧化时，其提供酚，而不需要任何中间操作。更具体地说，描述了使用频哪醇硼烷（HBPin）进行Ir催化的芳烃硼烷化，然后用OXONE氧化中间体芳基硼酸酯的方法。

7. 发明授权

US06469133B2 Process for the preparation of polymers of dimeric cyclic esters 有权
标题翻译：制备二聚环酯聚合物的方法
公开(公告)号：US06469133B2
公开(公告)日：2002-10-22
申请号：US09736991
申请日：2000-12-13
申请人： Gregory L. Baker , Milton R. Smith, III
发明人： Gregory L. Baker , Milton R. Smith, III
IPC分类号： C08G6308
CPC分类号： C08G63/08 , C08G63/823
摘要： The present invention provides a process for the direct synthesis of high melting polymers made from dimeric cyclic esters. In particular, the present invention provides a process for synthesis of polylactic acid (PLA) from racemic materials such as racemic lactide and polymandelide from mandelide. The process further provides racemic metal organic ligand catalysts such as racemic salbinap that catalyzes the polymerization of racemic dimeric cyclic ester monomers to a polylactide stereocomplex. Polymandelide and mixed dimeric cyclic esters are also prepared in the presence of low amounts of water.
摘要翻译：本发明提供直接合成由二聚环酯制成的高熔点聚合物的方法。特别地，本发明提供从外消旋材料如外消旋丙交酯和来自扁桃体的聚扁桃酸酯合成聚乳酸（PLA）的方法。该方法进一步提供外消旋金属有机配位体催化剂，例如外消旋萨拉宾酸，其催化外消旋二聚环状酯单体聚合成聚丙交酯立体络合物。聚山梨糖苷和混合的二聚环状酯也是在少量水存在下制备的。

8. 发明授权

US07709654B2 Process for producing oxazole, imidazole, pyrrazole boryl compounds 有权
标题翻译：制备恶唑，咪唑，吡唑硼烷化合物的方法
公开(公告)号：US07709654B2
公开(公告)日：2010-05-04
申请号：US11900329
申请日：2007-09-11
申请人： Milton R. Smith, III , Robert E. Maleczka, Jr. , Venkata A. Kallepalli , Edith Onyeozili
发明人： Milton R. Smith, III , Robert E. Maleczka, Jr. , Venkata A. Kallepalli , Edith Onyeozili
IPC分类号： C07D263/30 , C07D263/34 , C07D233/54 , C07D233/68 , C07D231/10 , C07D231/16
CPC分类号： C07F5/025
摘要： Process for the preparation of oxazole, imidazole, and pyraxole boryl compounds. The compounds are intermediates to functionalized compounds, both natural and synthetic which are cytotoxic, anticancer and antiviral agents.
摘要翻译：恶唑，咪唑和吡唑氧基硼烷化合物的制备方法。该化合物是天然和合成的功能化化合物的中间体，其为细胞毒性，抗癌和抗病毒剂。

9. 发明授权

US06867302B2 Process for the catalytic synthesis of biaryls and polymers from aryl compounds 有权
标题翻译：从芳基化合物催化合成联芳基和聚合物的方法
公开(公告)号：US06867302B2
公开(公告)日：2005-03-15
申请号：US10194859
申请日：2002-07-12
申请人： Milton R. Smith, III , Robert E. Maleczka
发明人： Milton R. Smith, III , Robert E. Maleczka
IPC分类号： B01J31/12 , B01J31/14 , B01J31/18 , B01J31/22 , B01J31/24 , B01J31/28 , C07C1/32 , C07C17/269 , C07F5/02 , C07F15/00 , C07F17/02 , C08G61/10 , C07D213/14 , C07D213/08
CPC分类号： C08G61/10 , B01J31/1805 , B01J31/22 , B01J31/2295 , B01J31/24 , B01J31/2404 , B01J31/2409 , B01J2231/4211 , B01J2531/822 , B01J2531/824 , B01J2531/827 , B01J2531/842 , C07C1/321 , C07C17/269 , C07C2531/22 , C07F5/025 , C07F15/0033 , C07F15/004 , C07F15/0073 , C07F15/008 , C07F17/02 , C08G2261/312 , C07C15/00 , C07C22/08 , C07C25/18
摘要： A process for producing organic substituted aromatic or heteroaromatic compounds including biaryl and biheteroaryl compounds in a two-step reaction. In the first step, the aromatic or heteroaromatic compound is borylated in a reaction comprising a borane or diborane reagent (any boron reagent where the boron reagent contains a B—H, B—B or B—Si bond) and an iridium or rhodium catalytic complex. In the second step, a metal catalyst catalyzes the formation of the organic substituted aromatic or heteroaromatic compound from the borylated compound and an electrophile such as an aryl or organic halide, triflate (OSO2CF3), or nonaflate (OSO2C4F9). The steps in the process can be performed in a single reaction vessel or in separate reaction vessels. The present invention also provides a process for synthesis of complex polyphenylenes starting from halogenated aromatic compounds.
摘要翻译：一种在两步反应中制备包括联芳基和双杂芳基化合物的有机取代的芳族或杂芳族化合物的方法。在第一步中，在包含硼烷或乙硼烷试剂（硼试剂含有B-H，B-B或B-Si键的任何硼试剂）和铱或铑催化络合物的反应中，芳族或杂芳族化合物被硼酸化。在第二步中，金属催化剂催化从硼化化合物和亲电体如芳基或有机卤化物，三氟甲磺酸酯（OSO 2 CF 3）或非卤化物（OSO 2 C 4 F 9）形成有机取代的芳香族或杂芳族化合物。该方法中的步骤可以在单个反应容器中或在单独的反应容器中进行。本发明还提供从卤代芳族化合物开始合成络合聚苯的方法。

10. 发明申请

US20090325292A1 Functional polyglycolide nanoparticles derived from unimolecular micelles 有权
标题翻译：衍生自单分子胶束的功能聚乙交酯纳米颗粒
公开(公告)号：US20090325292A1
公开(公告)日：2009-12-31
申请号：US12460655
申请日：2009-07-22
申请人： Gregory L. Baker , Milton R. Smith, III , Erin Vogel
发明人： Gregory L. Baker , Milton R. Smith, III , Erin Vogel
IPC分类号： C12N5/06 , C08G63/08 , A61K9/00
CPC分类号： C08G63/08 , A61K9/1075 , A61K9/5153 , A61K47/34 , A61K47/6907 , A61K47/6931 , A61K47/6935 , B82Y5/00 , C08G63/6852
摘要： Poly(glycolide) polymers are disclosed. The polymers generally include a glycolide-based polymer backbone that includes one or more functional groups such as alkynyl groups, hydrophilic organic triazole groups, hydrophobic organic triazole groups (also including amphiphilic organic triazole groups), di-triazole organic crosslinking groups, and triazole-substituted drug derivatives. The alkynyl groups provide reactive sites for further functionalization of the polymer, for example by reaction with azide derivatives. The polymers can further encapsulate a drug for delivery to a patient (i.e., as compared to drug derivatives that are covalently attached to the polymer). The polymers can be in the form of thermodynamically stable unimolecular micelles or crosslinked nanoparticles. The polymer compositions are completely biodegradable and hold great potential for use in biomedical applications.
摘要翻译：公开了聚（乙交酯）聚合物。聚合物通常包括基于乙交酯的聚合物主链，其包括一个或多个官能团，例如炔基，亲水有机三唑基，疏水性有机三唑基团（也包括两亲性有机三唑基团），二 - 三唑有机交联基团和三唑 - 取代的药物衍生物。炔基提供用于聚合物进一步官能化的反应位点，例如通过与叠氮化物衍生物反应。聚合物可以进一步包封用于递送给患者的药物（即，与共价连接到聚合物上的药物衍生物相比）。聚合物可以是热力学稳定的单分子胶束或交联纳米颗粒的形式。聚合物组合物是完全可生物降解的，并且具有用于生物医学应用的巨大潜力。

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