公开(公告)号：WO2008042389A1

公开(公告)日：2008-04-10

申请号：PCT/US2007/021184

申请日：2007-10-02

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  BYCROFT, Matthew ,  CANTRILL, Alexander, A. ,  KEENE, Philip, A.

Inventor： BYCROFT, Matthew ,  CANTRILL, Alexander, A. ,  KEENE, Philip, A.

IPC: C12P7/40 ,  C12P7/62 ,  C12P41/00

CPC classification number: C12P7/40 ,  C12P7/62 ,  C12P41/005

Abstract: A process for the preparation of a 3-amino-3-arylpropionic acid ester that is enriched in the ( S )-enantiomer to at least 80% ee, or the preparation of 3-amino-3-arylpropionic acid that is enriched in the ( R )-enantiomer to at least 80% enantiomeric excess (ee), is disclosed. The process comprises enantioselectively hydrolyzing an enantiomeric mixture of 3- amino-3-arylpropionic acid esters, and recovering the optically active ester ( S )-(I) which is not hydrolyzed. Use of an ester hydrolase obtained from Aspergillus in the process is also disclosed.

Abstract translation: 制备富含（S） - 对映异构体至少80％ee的3-氨基-3-芳基丙酸酯的方法，或其中富含3-氨基-3-芳基丙酸的方法 （R） - 对映体至至少80％对映异构体过量（ee）。 该方法包括对映体选择性水解3-氨基-3-芳基丙酸酯的对映异构体混合物，并回收未水解的光学活性酯（S） - （I）。 还公开了在该方法中从曲霉得到的酯水解酶的用途。

公开(公告)号：WO2004013618A1

公开(公告)日：2004-02-12

申请号：PCT/US2003/021883

申请日：2003-07-14

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  TUCKER, Christopher, J.

Inventor： TUCKER, Christopher, J.

IPC: G01N21/51

CPC classification number: G01N33/15 ,  G01N15/0205 ,  G01N21/51 ,  G01N2013/006 ,  G01N2015/0693

Abstract: A method for determining the percent of a solid material dissolved into a liquid medium is disclosed. The method comprises the steps of combining the solid material and the liquid medium; determining the initial solid concentration (i); determining the dynamic solid concentration (d) using a light scattering technique; and calculating the percent dissolved material according to the formula: [(i - d)/i] x 100 . Methods for determining dissolution rate and particle size using turbidity measurements are also disclosed.

Abstract translation: 公开了一种确定溶解在液体介质中的固体材料的百分比的方法。 该方法包括将固体材料与液体介质结合的步骤; 确定初始固体浓度（i）; 使用光散射技术确定动态固体浓度（d）; 并根据以下公式计算溶解的百分比：[（i-d）/ i]×100。 还公开了使用浊度测量来确定溶解速率和粒径的方法。

公开(公告)号：WO2005049096A2

公开(公告)日：2005-06-02

申请号：PCT/US2004/037769

申请日：2004-11-12

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  ATHEY, Phillip, S. ,  KIEFER, Garry, E. ,  SIMON, Jaime ,  FRANK, R. Keith ,  ADAIR, Christopher ,  GULYAS, Gyongyi

Inventor： ATHEY, Phillip, S. ,  KIEFER, Garry, E. ,  SIMON, Jaime ,  FRANK, R. Keith ,  ADAIR, Christopher ,  GULYAS, Gyongyi

IPC: A61K51/06

CPC classification number: A61K51/065 ,  A61K49/085 ,  A61K49/126 ,  A61K49/14 ,  A61K51/0497 ,  A61K51/088

Abstract: The present invention is a pharmaceutical composition that exhibits enhanced IP blood retention, the composition comprising: a biotargeting molecule; and a chelating agent conjugated to the biotargeting molecule; wherein the composition exhibits a half-life in the bloodstream of from 15 minutes to 24 hours. The present invention is also directed to the use of functionalized chelants to modify the pharmacokinetics of radiopharmaceuticals. Compared with non-functionalized chelants, chelants functionalized with bulky and/or lipophilic groups can slow down the renal clearance and enhance the blood retention of metals complexed therewith. This enhanced blood retention leads to increased uptake of metal in target tissue.

Abstract translation: 本发明是一种具有增强的IP血液保留性的药物组合物，该组合物包含：生物靶向分子; 和与生物靶向分子缀合的螯合剂; 其中所述组合物在血液中的半衰期为15分钟至24小时。 本发明还涉及功能化螯合剂用于改变放射性药物的药代动力学的用途。 与非官能化螯合剂相比，用大体积和/或亲脂基团官能化的螯合剂可以减慢肾清除率并增强与其结合的金属的血液保持性。 这种增强的血液保留导致靶组织中金属的摄取增加。

公开(公告)号：WO2002098559A2

公开(公告)日：2002-12-12

申请号：PCT/US2002/006992

申请日：2002-03-06

Applicant: UNION CARBIDE CHEMICALS & PLASTICS TECHNOLOGY COR PORATION ,  ANNIS, Loana ,  WASSERMAN, Eric, P.

Inventor： ANNIS, Loana ,  WASSERMAN, Eric, P.

IPC: B01J31/00

CPC classification number: C08G65/24 ,  B01J31/143 ,  B01J31/2226 ,  B01J31/226 ,  B01J2531/31 ,  C07F5/066 ,  C08G65/12 ,  C08L2205/05

Abstract: An organoaluminum reaction product of A.) a ligand of the formula I, wherein R 1 represents an alkyl, aryl, arylalkyl, or alkylaryl group, a C 3-24 silyl group, or hydrogen, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 12 , and R 13 are the same or different and represent an alkyl, aryl, arylalkyl, or alkylaryl group, a C 3-24 silyl group, halide, or hydrogen, with the proviso that at least one of the groups R 4 and R 13 represents hydrogen, R 8 represents an alkoxy, alkyl, aryl, arylalkyl, or alkylaryl group, a C 3-24 silyl group, halide, hydroxyl radical, or hydrogen, E represents O, S, Se, or Te, and n is an integer from 1 to 4, and B.) an aluminum compound of formula A1R 9 R 10 R 11 , wherein R 9 and R 10 are the same or different and represent C 1-20 alkyl, aryl, arylalkyl, or alkylaryl group, or hydrogen, and R 11 is a C 1-20 alkyl, aryl, arylalkyl, alkylaryl or alkoxy group, hydrogen, or halogen is useful as a polymerization catalyst, particularly for the homopolymerization or copolymerization of an alkylene oxide.

Abstract translation: A）的有机铝反应产物，其中R1表示烷基，芳基，芳烷基或烷基芳基，C3-24甲硅烷基或氢，R2，R3，R4，R5，R6，R7 R 12和R 13相同或不同，表示烷基，芳基，芳基烷基或烷基芳基，C 3-4-24甲硅烷基，卤化物或氢，条件是基团R 4和R 13中的至少一个表示氢 ，R8代表烷氧基，烷基，芳基，芳基烷基或烷基芳基，C3-24甲硅烷基，卤化物，羟基或氢，E表示O，S，Se或Te，n表示1〜 4和B.）式A1R9R10R11的铝化合物，其中R 9和R 10相同或不同并且表示C 1-20烷基，芳基，芳基烷基或烷基芳基或氢，R 11是C 1-20烷基，芳基 ，芳基烷基，烷基芳基或烷氧基，氢或卤素可用作聚合催化剂，特别是用于烯化氧的均聚或共聚。

公开(公告)号：WO2006026502A1

公开(公告)日：2006-03-09

申请号：PCT/US2005/030543

申请日：2005-08-26

Applicant: THE DOW CHEMICAL COMPANY ,  BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM ,  HITT, James, E. ,  ROGERS, True, L. ,  GILLESPIE, Ian, B. ,  SCHERZER, Brian, D. ,  GARCIA, Paula, C. ,  BECK, Nicholas, S. ,  TUCKER, Christopher, J. ,  YOUNG, Timothy, J. ,  HAYES, David, A. ,  WILLIAMS, Robert, O., III ,  JOHNSTON, Keith, P. ,  MCCONVILLE, Jason, T. ,  PETERS, Jay, I. ,  TALBERT, Robert ,  BURGESS, David

Inventor： HITT, James, E. ,  ROGERS, True, L. ,  GILLESPIE, Ian, B. ,  SCHERZER, Brian, D. ,  GARCIA, Paula, C. ,  BECK, Nicholas, S. ,  TUCKER, Christopher, J. ,  YOUNG, Timothy, J. ,  HAYES, David, A. ,  WILLIAMS, Robert, O., III ,  JOHNSTON, Keith, P. ,  MCCONVILLE, Jason, T. ,  PETERS, Jay, I. ,  TALBERT, Robert ,  BURGESS, David

IPC: A61K9/12 ,  A61K31/496

CPC classification number: A61K31/496 ,  A61K9/0073 ,  A61K9/008 ,  A61K9/19

Abstract: Inhalable compositions are described. The inhalable compositions comprise one or more respirable aggregates, the respirable aggregates comprising one or more poorly water soluble active agents, wherein at least one of the active agents reaches a maximum lung concentration (C max ) of at least about 0.25 μg/gram of lung tissue and remains at such concentration for a period of at least one hour after being delivered to the lung. Methods for making such compositions and methods for using such compositions are also disclosed.

Abstract translation: 描述了可吸入组合物。 可吸入组合物包含一种或多种可呼吸聚集体，可呼吸聚集体包含一种或多种难溶于水的活性剂，其中至少一种活性剂达到最大肺浓度（C

公开(公告)号：WO2003032951A1

公开(公告)日：2003-04-24

申请号：PCT/US2002/027444

申请日：2002-08-27

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  HITT, James, E. ,  TUCKER, Christopher, J. ,  EVANS, Jonathan, C. ,  CURTIS, Cathy, A. ,  SVENSON, Sonke

Inventor： HITT, James, E. ,  TUCKER, Christopher, J. ,  EVANS, Jonathan, C. ,  CURTIS, Cathy, A. ,  SVENSON, Sonke

IPC: A61K9/14

CPC classification number: A61K9/5146 ,  A61K9/1635 ,  A61K9/1688 ,  B01D9/005 ,  B82Y5/00

Abstract: A process for preparing crystalline particles of a drug substance is disclosed, said process comprising recirculating an anti-solvent through a mixing zone, dissolving the drug substance in a solvent to form a solution, adding the solution to the mixing zone to form a article slurry in the anti-solvent, and recirculating at least a portion of the particle slurry back through the mixing zone. Particles produced from the process are also disclosed. The present invention has the ability to be operated in a continuous fashion, resulting in a more efficient process and a more uniform product. The present invention has the additional advantage of having the ability to operate at a relatively low solvent ratio, thereby increasing the drug to excipient ratio.

Abstract translation: 公开了一种制备药物结晶颗粒的方法，所述方法包括通过混合区使反溶剂再循环，将药物溶解在溶剂中以形成溶液，将溶液加入混合区以形成制品浆料 在反溶剂中，并且将至少一部分颗粒浆料再循环通过混合区。 还公开了从该方法生产的颗粒。 本发明具有以连续方式操作的能力，从而产生更有效的工艺和更均匀的产品。 本发明具有能够以相对低的溶剂比操作的能力的另外的优点，从而将药物增加到赋形剂比例。

公开(公告)号：WO2002047659A3

公开(公告)日：2002-06-20

申请号：PCT/US2001/051337

申请日：2001-10-22

Applicant: BOARD OF REGENTS UNIVERSITY OF TEXAS SYSTEM

Inventor： JOHNSTON, Keith, P. ,  WILLIAMS, Robert, O. ,  YOUNG, Timothy, J. ,  CHEN, Xiaoxia

IPC: A61K9/14

Abstract: A method for preparing poorly water soluble drug particles is disclosed. The method comprises dissolving a drug in at least one organic solvent to form a drug/organic mixture, spraying the drug/organic mixture into an aqueous solution and concurrently evaporating the organic solvent in the presence of the aqueous solution to form an aqueous dispersion of the drug particles. The resulting drug particles are in the nanometer to micrometer size range and show enhanced dissolution rates and reduced crystallinity when compared to the unprocessed drug.

公开(公告)号：WO2008036370A2

公开(公告)日：2008-03-27

申请号：PCT/US2007/020399

申请日：2007-09-20

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  KAR, Kishore, K. ,  PIRAS, Luciano ,  MONAGHEDDU, Marzio ,  GNAGNETTI, Andrea

Inventor： KAR, Kishore, K. ,  PIRAS, Luciano ,  MONAGHEDDU, Marzio ,  GNAGNETTI, Andrea

CPC classification number: B01F5/221 ,  B01F7/00466 ,  B01F7/00641 ,  B01J10/002 ,  B01J19/0066 ,  B01J19/1806 ,  B01J2219/00105 ,  B01J2219/0013

Abstract: A liquid-gas phase reactor system including a slinger located in an upper section (headspace region) of a reaction vessel. The slinger comprises an upper horizontal surface including a plurality of vertically raised vanes extending radially outward along a curved path which effectively distribute liquid about the reactor vessel. A method for conducting an oxidation reaction using a liquid-gas phase reactor system is also disclosed. The disclosed reactor system and method have a broad range of applications but are particularly suited for the production of terephthalic acid.

Abstract translation: 液 - 气相反应器系统，其包括位于反应容器的上部（顶空区域）中的抛油环。 抛油环包括上部水平表面，所述上部水平表面包括沿着弯曲路径径向向外延伸的多个垂直升高的叶片，所述弯曲路径有效地将液体分布在反应堆容器周围。 还公开了使用液 - 气相反应器系统进行氧化反应的方法。 所公开的反应器系统和方法具有广泛的应用范围，但特别适用于生产对苯二甲酸。

公开(公告)号：WO2007016377A2

公开(公告)日：2007-02-08

申请号：PCT/US2006/029494

申请日：2006-07-27

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  STRICKLAND, Alan, D. ,  SIMON, Jaime

Inventor： STRICKLAND, Alan, D. ,  SIMON, Jaime

CPC classification number: A61K47/12 ,  A61K33/00 ,  A61K33/14 ,  A61K45/06 ,  A61K47/32

Abstract: Dialysis solutions comprising aqueous solutions including physiologically acceptable salts and a polyelectrolyte osmotic agent are disclosed. The subject solutions provide an improved osmotic gradient resulting in reduced dialysis times and/or reduced volumes of required dialysis solution. Moreover, the subject osmotic agents do not significantly migrate into the patient's blood over the time period of dialysis nor are the subject osmotic agents as susceptible to forming detrimental degradation products during gamma sterilization. The subject osmotic agents are much less susceptible to microbial contamination than currently available osmotic agents used in dialysis. The use of free radical scavengers is also described along with the use of a filter to reduce the introduction of bacteria into the peritoneal cavity.

Abstract translation: 公开了包含包含生理上可接受的盐和聚电解质渗透剂的水溶液的透析溶液。 本发明溶液提供改善的渗透梯度，导致透析时间减少和/或减少所需透析溶液的体积。 此外，在渗透期间，本发明的渗透剂不会显着迁移到患者的血液中，而且在伽马灭菌期间，受试者渗透剂也易于形成有害的降解产物。 本发明的渗透剂比目前在透析中使用的渗透剂更不易受微生物污染。 还描述了使用自由基清除剂以及使用过滤器以减少将细菌引入腹膜腔中。

公开(公告)号：WO2007014084A1

公开(公告)日：2007-02-01

申请号：PCT/US2006/028513

申请日：2006-07-21

Applicant: DOW GLOBAL TECHNOLOGIES INC. ,  CRANLEY, Paul ,  WARREN, Malcolm, J., II. ,  SUN, Larry ,  PRESSLER, Michelle ,  WHITE, Douglas, P. ,  LAKROUT, Hamed ,  DANOWSKI, Kristine

Inventor： CRANLEY, Paul ,  WARREN, Malcolm, J., II. ,  SUN, Larry ,  PRESSLER, Michelle ,  WHITE, Douglas, P. ,  LAKROUT, Hamed ,  DANOWSKI, Kristine

IPC: A61K9/20 ,  A61K9/48 ,  A61B5/06

CPC classification number: A61B7/008 ,  A61B5/42 ,  A61B5/4839 ,  A61B5/6831 ,  A61B5/7405 ,  A61B8/12 ,  A61K9/0009

Abstract: A tablet, pill or capsule containing a material which produces sound waves when the tablet, pill or capsule is exposed to the gastrointestinal system. A two step method for oral drug compliance monitoring. The first step is to ingest a tablet, pill or capsule containing a material which produces sound waves when the tablet, pill or capsule is exposed to the gastrointestinal system of a person. The second step is to detect the sound waves produced when the tablet, pill or capsule is exposed to the gastrointestinal system to confirm that the person has ingested the tablet, pill or capsule.

Abstract translation: 包含当片剂，药丸或胶囊暴露于胃肠系统时产生声波的材料的片剂，药丸或胶囊。 口服药物依从性监测的两步法。 第一步是摄取含有当片剂，药丸或胶囊暴露于人的胃肠系统时产生声波的材料的片剂，药丸或胶囊。 第二步是检测当片剂，药片或胶囊暴露于胃肠系统时产生的声波，以确认该人已经摄取了片剂，丸剂或胶囊。