公开(公告)号：CA2591554A1

公开(公告)日：2006-08-03

申请号：CA2591554

申请日：2005-12-15

Applicant: BAXTER INT ,  BAXTER HEALTHCARE SA

Inventor： HAI TON THAT ,  KIPP JAMES E ,  MELNICK BENNETT P

IPC: C08G65/326 ,  C08G65/334 ,  C08L71/02

公开(公告)号：AU2005326168A1

公开(公告)日：2006-08-03

申请号：AU2005326168

申请日：2005-12-15

Applicant: BAXTER HEALTHCARE SA ,  BAXTER INT

Inventor： HAI TON THAT ,  MELNICK BENNETT P ,  KIPP JAMES E

IPC: C08G65/326 ,  C08G65/334 ,  C08L71/02

公开(公告)号：AU2005304952A1

公开(公告)日：2006-05-18

申请号：AU2005304952

申请日：2005-11-03

Applicant: BAXTER INT ,  BAXTER HEALTHCARE SA

Inventor： KIPP JAMES E ,  ROESSLER BERTHOLD ,  DOTY MARK ,  PAPADOPOULOS PAVLOS

IPC: A61K31/404 ,  A61K9/00 ,  A61P35/00

Abstract: The present invention is directed to novel pharmaceutical compositions comprising nano- and micro-particulate formulations of poorly water soluble tubulin inhibitors of the indole chemical class, preferably N-substituted indol-3-glyoxyamides, and more preferably N-(Pyridin-4-yl)-[1-(4-chlorobenzyl)-indol-3-yl]glyoxylic acid amide (D-24851), also known as “Indibulin,” and methods of making and using such compositions for the treatment of anti-tumor agent resistant cancers and other diseases.

公开(公告)号：JP2012097120A

公开(公告)日：2012-05-24

申请号：JP2012030443

申请日：2012-02-15

Applicant: Baxter Healthcare Sa ,  Baxter Internatl Inc ,  バクスター・インターナショナル・インコーポレイテッドBaxter International Incorp0Rated ,  バクスター・ヘルスケヤー・ソシエテ・アノニムBaxter Healthcare S.A.

Inventor： PAPADOPOULOS PAVLOS ,  GERHARD RAAB ,  DOTY MARK ,  KIPP JAMES E ,  ROESSLER BERTHOLD

IPC: A61K31/4439 ,  A61K9/14 ,  A61K9/51 ,  A61K31/405 ,  A61K47/02 ,  A61K47/10 ,  A61K47/28 ,  A61K47/34 ,  A61P11/02 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P35/04 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D209/18 ,  C07D401/12

CPC classification number: C07D401/12 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/10 ,  A61K9/14 ,  A61K9/145 ,  A61K9/146 ,  A61K9/5123 ,  A61K9/5146 ,  A61K31/404 ,  A61K31/4439 ,  Y10T428/2982

Abstract: PROBLEM TO BE SOLVED: To provide nanoparticulate compositions of tubulin inhibitor compounds.SOLUTION: The present invention is directed to novel pharmaceutical compositions comprising nano- and micro-particulate formulations of poorly water soluble tubulin inhibitors of the indole chemical class, preferably N-substituted indol-3-glyoxyamides, and more preferably N-(Pyridin-4-yl)-[1-(4-chlorobenzyl)-indol-3-yl]glyoxylic acid amide (D-24851), also known as "Indibulin", and methods of making and using such compositions for the treatment of anti-tumor agent resistant cancers and other diseases.

Abstract translation: 待解决的问题：提供微管蛋白抑制剂化合物的纳米颗粒组合物。 解决方案：本发明涉及新的药物组合物，其包含吲哚化学类的水溶性差的微管蛋白抑制剂的纳米和微粒子制剂，优选N-取代的吲哚-3-乙酰氧基酰胺，更优选N-（ 吡啶-4-基） - [1-（4-氯苄基） - 吲哚-3-基]乙醛酸酰胺（D-24851），也称为“靛红”，以及制备和使用这些组合物用于治疗 抗肿瘤药物抗癌药物等疾病。 版权所有（C）2012，JPO＆INPIT

公开(公告)号：WO02055059A3

公开(公告)日：2002-09-06

申请号：PCT/US0149737

申请日：2001-12-20

Applicant: BAXTER INT

Inventor： KIPP JAMES E ,  WONG JOSEPH CHUNG TAK ,  DOTY MARK J ,  REBBECK CHRISTINE L ,  BRYNJELSEN SEAN ,  WERLING JANE ,  SRIRAM RAJARAM

IPC: C07D407/14 ,  A61K9/10 ,  A61K9/14 ,  A61K9/16 ,  A61K31/495 ,  A61K31/496 ,  A61K47/12 ,  A61K47/14 ,  A61K47/18 ,  A61K47/20 ,  A61K47/24 ,  A61K47/28 ,  A61K47/34 ,  A61K47/36 ,  A61K47/38 ,  A61K47/42 ,  A61P31/10 ,  A61K9/20 ,  A61K9/51

CPC classification number: A61K31/495 ,  A61K9/10 ,  A61K9/14 ,  A61K9/145 ,  A61K9/146 ,  A61K9/1688 ,  A61K31/496

Abstract: The present invention provides a method for preparing a suspension of a pharmaceutically-active compound, the solubility of which is greater in a water-miscible first organic solvent than in a second solvent which is aqueous. The process includes the steps of : (i) dissolving a first quantity of the pharmaceutically-active compound in the water-miscible first organic solvent to form a first solution ; (ii) mixing the first solution with the second solvent to precipitate the pharmaceutically-active compound ; and (iii) seeding the first solution or the second solvent or the presuspension.

Abstract translation: 本发明提供了制备药物活性化合物的悬浮液的方法，所述药物活性化合物在水混溶性第一有机溶剂中的溶解度大于含水第二溶剂中的溶解度。 该方法包括以下步骤：（i）将第一数量的药学活性化合物溶解在可与水混溶的第一有机溶剂中以形成第一溶液; （ii）将第一溶液与第二溶剂混合以沉淀药物活性化合物; 和（iii）接种第一溶液或第二溶剂或预悬浮液。

公开(公告)号：WO2004084860A3

公开(公告)日：2005-03-24

申请号：PCT/US2004009242

申请日：2004-03-24

Applicant: BAXTER INT

Inventor： KIPP JAMES E ,  WONG JOSEPH CHUNG TAK ,  WISLER MONTE ,  GARCIA RHONDA

IPC: A61K9/10 ,  A61K9/14

CPC classification number: A61K9/145 ,  A61K9/10 ,  Y10S516/924 ,  Y10S516/925 ,  Y10S977/84

Abstract: Methods and apparatuses for comminuting and stabilizing small particles are provided. In one embodiment, an apparatus moves an organic compound dissolved in a solvent to form a suspension of particles in a first fluid stream and moves the suspension in a second fluid stream, wherein the second fluid stream is oriented and positioned with respect to the first stream to cause shearing between the streams and mixing of at least some of the particles in the first and second streams.

Abstract translation: 提供粉碎和稳定小颗粒的方法和装置。 在一个实施方案中，装置移动溶解在溶剂中的有机化合物以形成第一流体物流中的颗粒悬浮液并将悬浮液移动到第二流体流中，其中第二流体流相对于第一流定向和定位 以引起流之间的剪切和第一和第二流中的至少一些颗粒的混合。

公开(公告)号：WO03026611A3

公开(公告)日：2003-07-03

申请号：PCT/US0230447

申请日：2002-09-25

Applicant: BAXTER INT

Inventor： BRYNJELSEN SEAN ,  STERNBERG SHMUEL ,  DUNHAM ANDREW J ,  DOTY MARK J ,  KIPP JAMES E ,  JAYSWAL NAILESH ,  NARAYANAN KRISHNASWAMY

IPC: A61K9/14 ,  A61K9/19 ,  A61K9/51 ,  A61K31/496 ,  A61K45/00 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/18 ,  A61K47/20 ,  A61K47/24 ,  A61K47/28 ,  A61K47/32 ,  A61K47/34 ,  A61K47/36 ,  A61K47/38 ,  A61K47/42 ,  B01J13/04

CPC classification number: A61K9/14 ,  A61K9/145 ,  A61K9/5169 ,  A61K9/5192 ,  B01J13/04

Abstract: The present invention relates to a process for preparing submicron sized nanoparticles of a poorly water soluble compound by sonicating to evaporate a portion of the organic phase or by lyophilizing a dispersion or microdispersion of a multiphase system having an organic phase and an aqueous phase, the organic phase havingthe poorly water soluble organic compound therein. The method is preferably used to prepare nanoparticles of a poorly water soluble, pharmaceutically active compound suitable for in vivo delivery, particularly by parenteral routes.

Abstract translation: 本发明涉及通过超声处理以蒸发一部分有机相或通过冻干具有有机相和水相的多相体系的分散体或微分散体来制备难溶于水的化合物的亚微米尺寸的纳米颗粒的方法，所述有机相和水相的有机相 相中其水溶性差的有机化合物。 该方法优选用于制备适于体内递送的水溶性差的药学活性化合物的纳米颗粒，特别是通过肠胃外途径。

公开(公告)号：WO2004054500A3

公开(公告)日：2004-08-26

申请号：PCT/US0324353

申请日：2003-08-04

Applicant: BAXTER INT

Inventor： WERLING JANE ,  KIPP JAMES E ,  SRIRAM RAJARAM ,  DOTY MARK J ,  REBBECK CHRISTINE L ,  WONG JOSEPH CHUNG TAK

IPC: A61K9/00 ,  A61K31/495 ,  A61K9/127 ,  A61K9/14

CPC classification number: A61K9/14 ,  A61K9/0019 ,  A61K9/10 ,  A61K31/495

Abstract: The present invention provides a method of preparing particles with polymorph and size control of a pharmaceutical compound, the method including the steps of: (1) providing pharmaceutical compound in a first phase; (2) seeding the compound; (3) causing a phase change in the pharmaceutical compound to a second phase of a desired polymorphic form; and (4) wherein the mean particle size of the particles is less than 7µm. The present invention further provides a polymorphic form of itraconazole.

Abstract translation: 本发明提供一种制备具有药物化合物的多晶型物和粒度控制的颗粒的方法，所述方法包括以下步骤：（1）在第一相中提供药物化合物; （2）接种化合物; （3）引起药物化合物相变为所需多晶型物的第二相; 和（4）其中颗粒的平均粒度小于7μm。 本发明还提供了伊曲康唑的多晶型物。

公开(公告)号：WO02078605A3

公开(公告)日：2003-02-06

申请号：PCT/US0210094

申请日：2002-03-28

Applicant: BAXTER INT

Inventor： DOTY MARK J ,  REBBECK CHRISTINE L ,  KIPP JAMES E ,  RAGHAVAN NEERVALUR V

IPC: C07D307/80 ,  A61K9/00 ,  A61K9/08 ,  A61K31/343 ,  A61K47/02 ,  A61K47/10 ,  A61K47/18 ,  A61K47/26 ,  A61K47/34 ,  A61K47/36 ,  A61P9/06

CPC classification number: A61K9/0019 ,  A61K31/343 ,  A61K47/26

Abstract: A premix parenteral solution for intravenous administration having amiodarone, as an active ingredient, solubilized in a solution of water for injection and about 0.4 - 12 mg/ml of a non-ionic surfactant to a concentration range of from 0.2 to 6 mg/ml is disclosed. The solution optionally may include an osmotic agent. No dilution of the solution is required before administering to a patient and the sterile packaged solution has an initial pH within the range of from about 2.9 to about 3.2, preferably about 3.1. Additionally, a method for producing an amiodarone solution suitable for intravenous administration is further disclosed.

Abstract translation: 用于静脉内给药的预混合肠胃外溶液，其具有溶解于注射用水和约0.4-12mg / ml非离子表面活性剂的胺碘酮作为活性成分，浓度范围为0.2至6mg / ml， 披露。 溶液任选地可以包括渗透剂。 在给予患者之前不需要稀释溶液，无菌包装溶液的初始pH范围为约2.9至约3.2，优选约3.1。 此外，还公开了适用于静脉内给药的胺碘酮溶液的制备方法。

公开(公告)号：WO0174395A3

公开(公告)日：2002-02-07

申请号：PCT/US0110598

申请日：2001-03-30

Applicant: BAXTER INT

Inventor： KIPP JAMES E ,  DOTY MARK J ,  REBBECK CHRISTINE L ,  EILERT JAN Y

IPC: A61K9/08 ,  A61K9/00 ,  A61K31/34 ,  A61K31/343 ,  A61K47/04 ,  A61K47/10 ,  A61K47/12 ,  A61K47/18 ,  A61K47/20 ,  A61K47/26 ,  A61P9/06

CPC classification number: A61K9/0019 ,  A61K31/34 ,  A61K47/12

Abstract: The present invention provides an amiodarone parenteral solution suitable for intravenous administration without the necessity of dilution. The parenteral solution has an amiodarone concentration from 0.2 to 10 mg/ml and a buffer solution selected from the group consisting of lactate buffer, methanesulfonate buffer, or combinations thereof, the solution having a pH within the range from approximately 2.5 - 4.5.

Abstract translation: 本发明提供了一种适于静脉内给药而不需要稀释的胺碘酮肠胃外溶液。 肠胃外溶液具有0.2至10mg / ml的胺碘酮浓度和选自乳酸盐缓冲液，甲磺酸盐缓冲液或其组合的缓冲溶液，该溶液的pH值在约2.5-4.5的范围内。