公开(公告)号：WO2007124224A3

公开(公告)日：2008-04-17

申请号：PCT/US2007064679

申请日：2007-03-22

Applicant: BAXTER INT ,  BAXTER HEALTHCARE SA ,  RABINOW BARRETT E ,  GENDELMAN HOWARD E ,  KIPP JAMES E

Inventor： RABINOW BARRETT E ,  GENDELMAN HOWARD E ,  KIPP JAMES E

IPC: A61K9/10 ,  A61K9/00 ,  A61K9/51 ,  A61K47/48 ,  A61P31/18

CPC classification number: A61K9/0085 ,  A61K9/10 ,  A61K9/5123 ,  A61K9/5146 ,  A61K47/6901

Abstract: The present invention is concerned with delivering a pharmaceutical composition to a tissue target of a mammalian subject for treating brain diseases or disorders. The process includes the steps of: (i) providing a dispersion of the pharmaceutical composition as particles having an average particle size of from about 150 nm to about 100 microns, and (ii) administering the dispersion to the mammalian subject for delivery to the tissue target of a portion of the pharmaceutical composition by cells capable of reaching the tissue target. The dispersion of the pharmaceutical composition as particles, for example, can be phagocytised or adsorbed by the cells prior or subsequent to administration into the mammalian subject. The dispersion of the pharmaceutical composition can be administered to the central nervous system or the vascular system. After administration, the loaded cells transport the pharmaceutical composition as particles into the tissue target.

Abstract translation: 本发明涉及将药物组合物递送至哺乳动物受试者的组织靶以治疗脑部疾病或病症。 该方法包括以下步骤：（i）提供药物组合物的分散体作为平均粒度为约150nm至约100微米的颗粒，和（ii）向哺乳动物受试者施用分散体以递送至组织 通过能够到达组织靶的细胞的一部分药物组合物的靶标。 例如，作为颗粒的药物组合物的分散体可以在给予哺乳动物受试者之前或之后被细胞吞噬或吸附。 药物组合物的分散体可以施用于中枢神经系统或血管系统。 给药后，负载的细胞将药物组合物作为颗粒输送到组织靶中。

公开(公告)号：WO2007059515A3

公开(公告)日：2007-11-01

申请号：PCT/US2006060939

申请日：2006-11-15

Applicant: BAXTER INT ,  BAXTER HEALTHCARE SA ,  KIPP JAMES E ,  WERLING JANE ,  GUPTA PRAMOD ,  BURESH RITA

Inventor： KIPP JAMES E ,  WERLING JANE ,  GUPTA PRAMOD ,  BURESH RITA

IPC: A61K9/14 ,  A61K9/10 ,  A61K9/19 ,  A61K31/38 ,  A61P1/00 ,  A61P9/10 ,  A61P11/06 ,  A61P17/06 ,  A61P17/10 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08

CPC classification number: A61K9/10 ,  A61K9/0043 ,  A61K9/0048 ,  A61K9/19 ,  A61K9/5146 ,  A61K31/38 ,  A61K31/381

Abstract: Pharmaceutical compositions comprising particles of lipoxygenase inhibitor compounds having an effective average size of from about 10 nm to about 50 microns are provided. More particularly, pharmaceutical compositions of particle of a 5 -lipoxygenase inhibitor compound having an effective average size of from about 50 nm to about 5 microns are provided. The pharmaceutical compositions are in the form of aqueous suspensions with the particle of the 5-lipoxygenase-inhibitor compound present in concentrations of from about 5 to about 200 mg/ml. In addition, methods for making such pharmaceutical compositions are provided. In particular, microprecipitation and direct homogenization in the presence of at least one surfactant are disclosed for making the pharmaceutical compositions.

Abstract translation: 提供了包含有效平均尺寸为约10nm至约50微米的脂氧合酶抑制剂化合物颗粒的药物组合物。 更特别地，提供了具有约50nm至约5微米的有效平均尺寸的5-脂氧合酶抑制剂化合物颗粒的药物组合物。 药物组合物呈含水悬浮液的形式，其中5-脂氧合酶抑制剂化合物颗粒以约5至约200mg / ml的浓度存在。 另外，提供了制备这种药物组合物的方法。 具体而言，公开了用于制备药物组合物的微量沉淀和在至少一种表面活性剂存在下的直接均质化。

公开(公告)号：WO2007059507A2

公开(公告)日：2007-05-24

申请号：PCT/US2006060914

申请日：2006-11-15

Applicant: BAXTER INT ,  BAXTER HEALTHCARE SA ,  KIPP JAMES E ,  GUPTA PRAMOD

Inventor： KIPP JAMES E ,  GUPTA PRAMOD

IPC: A61K47/48

CPC classification number: B82Y5/00 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0031 ,  A61K9/0034 ,  A61K9/0043 ,  A61K9/0073 ,  A61K9/19 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/724 ,  A61K47/40 ,  A61K47/6951 ,  A61K2300/00

Abstract: The present invention is directed to formulations of inclusion complexes of lipoxygenase inhibitors and cyclodextrins having a therapeutically effective concentration of the lipoxygenase inhibitor, methods of making the same and methods of treating disease states using the same. Forming cyclodextrin complexes permits the enhancement of the aqueous solubility of lipoxygenase inhibitors which allows higher concentrations of the lipoxygenase in solution. Aqueous formulations of lipoxygenase inhibitors-cyclodextrin complexes are suitable for parenteral or oral administration for treating and/or preventing inflammatory disease states. The aqueous formulations can be lyophilized to prolong storage stability, assist in oral administration and/or provide for convenient and economical packaging.

Abstract translation: 本发明涉及脂氧合酶抑制剂和具有治疗有效浓度的脂氧合酶抑制剂的环糊精的包合物的制剂，其制备方法以及使用其的治疗疾病状态的方法。 形成环糊精复合物允许提高脂氧合酶抑制剂的水溶性，其允许溶液中更高浓度的脂氧合酶。 脂氧合酶抑制剂 - 环糊精复合物的水性制剂适用于肠胃外或口服给药以治疗和/或预防炎性疾病状态。 水性制剂可以冻干以延长储存稳定性，有助于口服给药和/或提供方便和经济的包装。

公开(公告)号：WO2006081000A3

公开(公告)日：2006-09-28

申请号：PCT/US2005045321

申请日：2005-12-15

Applicant: BAXTER INT ,  BAXTER HEALTHCARE SA ,  KIPP JAMES E ,  HAI TON THAT ,  MELNICK BENNETT P

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

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

CPC classification number: C08G65/334 ,  A61K8/90 ,  A61K9/146 ,  A61K47/34 ,  A61Q19/00 ,  C08G65/326 ,  C08L71/02

Abstract: The present invention is directed to novel compounds, methods of manufacture and methods of use. The present invention is also directed to solid drug/active agent particles having one or more of the compounds of the present invention associated with the surface thereof. The compounds of the present invention are comprised of a non-polar polyether covalently linked to an anionic sulfonate group. The compounds have an amphipathic quality and preferably, are surface active. Such compounds are preferably useful as surface-active agents to coat and stabilize dispersions of particles in a continuous liquid medium. These surface-active agents may be applied in the stabilization of suspensions, emulsions, or liposome formulations intended for pharmaceutical, medical, cosmetic, or agricultural use. The particles that can be prepared by a variety of methods and will preferably comprise a pharmaceutical agent. Pharmaceutical compositions of the present invention can be used to treat amyriad of conditions and can be administered by many routes, including intravenous, intramuscular, subcutaneous, intrathecal, subdural, intracameral, intracerebral, intralesional, topical, oral, buccal, rectal, pulmonary, and nasal.

Abstract translation: 本发明涉及新化合物，制备方法和使用方法。 本发明还涉及具有一种或多种与其表面相关的本发明化合物的固体药物/活性剂颗粒。 本发明的化合物由与阴离子磺酸盐基团共价连接的非极性聚醚组成。 该化合物具有两性质量，优选表面活性。 这些化合物优选用作表面活性剂以涂覆和稳定颗粒在连续液体介质中的分散体。 这些表面活性剂可以用于稳定用于制药，医疗，化妆品或农业用途的悬浮液，乳剂或脂质体制剂。 可以通过多种方法制备并且优选包含药剂的颗粒。 本发明的药物组合物可用于治疗异常的病症，并且可以通过许多途径施用，包括静脉内，肌肉内，皮下，鞘内，硬膜下，阴道内，脑内，肠内，局部，口服，口腔，直肠，肺和 鼻。

公开(公告)号：WO2005077337A3

公开(公告)日：2006-03-23

申请号：PCT/US2005002471

申请日：2005-01-26

Applicant: BAXTER INT ,  KIPP JAMES E ,  DOTY MARK ,  REBBECK CHRISTINE L

Inventor： KIPP JAMES E ,  DOTY MARK ,  REBBECK CHRISTINE L

IPC: A61K9/113 ,  A61K9/107 ,  A61K9/127 ,  A61K31/557 ,  A61K38/17 ,  A61K48/00

CPC classification number: A61K9/1075 ,  A61K9/113 ,  A61K31/557

Abstract: The present invention relates to a dispersion of an active agent, which includes a multiphase system of an organic phase and an aqueous phase. The agent, preferably poorly water soluble, possesses surface active properties and itself serves as a dispersantor a stabilizer for the dispersion. The dispersion is suitable for pharmaceutical, veterinary, cosmetic, and agricultural applications, and is suitable for in vivo delivery, particularly by parenteral routes.

Abstract translation: 本发明涉及活性剂的分散体，其包括有机相和水相的多相体系。 优选水溶性差的试剂具有表面活性，并且其本身用作分散剂或分散体的稳定剂。 该分散体适用于药物，兽医，化妆品和农业应用，并且适合于体内递送，特别是通过肠胃外途径。

公开(公告)号：WO0033064A9

公开(公告)日：2001-03-29

申请号：PCT/US9928567

申请日：1999-12-02

Applicant: BAXTER INT

Inventor： KIPP JAMES E ,  WEHRMANN GLENN JR ,  HAMMOND RICHARD B ,  REBBECK CHRISTINE L

IPC: G01N27/30 ,  G01N27/416

CPC classification number: G01N27/301

Abstract: The present invention provides a reference electrode solution containing ammonium salts and phosphonium salts for the potentiometric measurement of pH and method of using the same. The use of the ammonium salts and the phosphonium salts to replace potassium chloride or sodium chloride as reference electrolytes in a standard reference electrode minimizes the formation of precipitates in sample solutions containing cation-sensitive compounds. Disruption of ion flow through the reference electrode is eliminated, and accurate pH measurements may be obtained in solutions that contain compounds having a strong affinity for hard cations.

Abstract translation: 本发明提供了含有铵盐和鏻盐的参比电极溶液，用于电位测量pH值和使用该方法。 在标准参考电极中使用铵盐和鏻盐代替氯化钾或氯化钠作为参考电解质，使含有阳离子敏感化合物的样品溶液中沉淀物的形成最小化。 消除通过参比电极的离子流的破坏，并且可以在含有对硬阳离子具有强亲和力的化合物的溶液中获得精确的pH测量。

公开(公告)号：ES2424255T3

公开(公告)日：2013-09-30

申请号：ES05851355

申请日：2005-11-03

Applicant: BAXTER INT ,  BAXTER HEALTHCARE SA

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

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

Abstract: Composición farmacéutica en partículas que incluye partículas con un tamaño medio efectivo de entreaproximadamente 15 nm y aproximadamente 50 micrómetros de al menos un inhibidor de la tubulina defórmula (1): donde X es R3 es arilo o heteroarilo; R3' es hidrógeno; R4, R5, R6 y R7 son independientemente hidrógeno, halógeno o alquilo; R1 es arilalquilo; y R2 es hidrógeno, alquilo, acilo, arilo, alcoxicarbonilo, ariloxicarbonilo, heteroariloxicarbonilo, cicloalcoxicarbonilo,heterocicloalcoxicarbonilo, alqueniloxicarbonilo, cicloalqueniloxicarbonilo y heterocicloalqueniloxi-carbonilo; yal menos un agente tensioactivo seleccionado de entre el grupo consistente en agentes tensioactivos noiónicos, agentes tensioactivos aniónicos, agentes tensioactivos catiónicos, agentes tensioactivos derivadosbiológicamente, agentes tensioactivos zwitteriónicos y aminoácidos.

公开(公告)号：BRPI0414970A2

公开(公告)日：2012-12-11

申请号：BRPI0414970

申请日：2004-06-15

Applicant: BAXTER INT

Inventor： RABINOW BARRETT E ,  GENDELMAN HOWARD E ,  KIPP JAMES E

IPC: A61K9/00 ,  A61K9/51 ,  A61K47/48

Abstract: The present invention is concerned with delivering a pharmaceutical composition to the brain of a mammalian subject for treating brain diseases or disorders. The process includes the steps of: (i) providing a dispersion of the pharmaceutical composition as particles having an average particle size of from about 150 nm to about 100 microns, and (ii) administering the dispersion to the mammalian subject for delivery to the brain of a portion of the pharmaceutical composition by cells capable of reaching the brain. The dispersion of the pharmaceutical composition as particles, for example, can be phagocytized or adsorbed by the cells prior or subsequent to administration into the mammalian subject. The dispersion of the pharmaceutical composition can be administered to the central nervous system or the vascular system. After administration, the loaded cells transport the pharmaceutical composition as particles into the brain.

公开(公告)号：CA2431705C

公开(公告)日：2010-10-05

申请号：CA2431705

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: A61K9/20 ,  C07D407/14 ,  A61K9/10 ,  A61K9/14 ,  A61K9/16 ,  A61K9/51 ,  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

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.

公开(公告)号：DK1435909T3

公开(公告)日：2010-03-15

申请号：DK02773797

申请日：2002-10-18

Applicant: BAXTER INT

Inventor： KONKEL JAMIE TERESA ,  KIPP JAMES E ,  DOTY MARK J ,  REBBECK CHRISTINE L ,  BRYNJELSEN SEAN

IPC: A61K9/10 ,  A61K8/02 ,  A61K8/04 ,  A61K8/06 ,  A61K8/34 ,  A61K8/35 ,  A61K8/36 ,  A61K8/365 ,  A61K8/37 ,  A61K8/39 ,  A61K8/40 ,  A61K8/41 ,  A61K8/44 ,  A61K8/46 ,  A61K8/60 ,  A61K8/64 ,  A61K8/73 ,  A61K8/86 ,  A61K8/89 ,  A61K8/891 ,  A61K9/107 ,  A61K9/14 ,  A61K31/12 ,  A61K31/4985 ,  A61K31/58 ,  A61K47/02 ,  A61K47/06 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/16 ,  A61K47/18 ,  A61K47/20 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61K47/36 ,  A61K47/38 ,  A61K47/42 ,  A61K47/44 ,  A61K47/46 ,  A61Q19/00