公开(公告)号：US20100323020A1

公开(公告)日：2010-12-23

申请号：US12817640

申请日：2010-06-17

申请人： Rajeev Gokhale ,  Kennan C. Marsh ,  Yi Shi

发明人： Rajeev Gokhale ,  Kennan C. Marsh ,  Yi Shi

IPC分类号： A61K31/5377 ,  A61K9/14 ,  A61P35/04 ,  A61P35/00 ,  A61P7/00

CPC分类号： A61K9/10 ,  A61K9/0095 ,  A61K31/5377 ,  A61K47/02 ,  A61K47/10

摘要： A liquid pharmaceutical composition comprises an aqueous medium having suspended therein a solid particulate Bc1-2 family protein inhibitory compound such as ABT-263, having a D90 particle size not greater than about 3 μm; wherein the aqueous medium further comprises at least one pharmaceutically acceptable surfactant and at least one pharmaceutically acceptable basifying agent such as sodium bicarbonate in amounts that are effective together to inhibit particle size increase. The composition is suitable for oral or parenteral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bc1-2 family proteins, for example cancer.

摘要翻译： 液体药物组合物包含其中悬浮有固体颗粒Bc1-2家族蛋白质抑制化合物如ABT-263的水性介质，其D90粒度不大于约3μm; 其中所述水性介质还包含至少一种药学上可接受的表面活性剂和至少一种药学上可接受的碱化剂如碳酸氢钠，其量可以一起有效抑制粒度增加。 该组合物适合于需要其的受试者口服或肠胃外给药，用于治疗以一种或多种抗凋亡Bc1-2家族蛋白（例如癌症）过表达为特征的疾病。

公开(公告)号：US06911214B2

公开(公告)日：2005-06-28

申请号：US09946085

申请日：2001-09-04

申请人： Laman Alani ,  Donald P. Gauwitz ,  Dilip Kaul ,  John M. Lipari ,  Soumojeet Ghosh ,  Kennan C. Marsh ,  Richard H. Whelan ,  Vanik D. Petrossian

发明人： Laman Alani ,  Donald P. Gauwitz ,  Dilip Kaul ,  John M. Lipari ,  Soumojeet Ghosh ,  Kennan C. Marsh ,  Richard H. Whelan ,  Vanik D. Petrossian

IPC分类号： A61K9/00 ,  A61K47/00 ,  A61K9/20 ,  A61K9/48 ,  A61K9/68

CPC分类号： A61K47/46 ,  A61K9/0095 ,  A61K47/02 ,  A61K47/12

摘要： A flavoring system for a liquid pharmaceutical composition and pharmaceutical compositions containing such flavoring systems are disclosed. Flavoring systems of the invention include at least one sweetening agent, at least two flavored ingredients, and at least one flavor modifier selected from the group consisting of citric acid, sodium citrate, sodium chloride, and mixtures thereof. At least two of the flavored ingredients are selected from the group consisting of a vanilla flavored ingredient, a peppermint flavored ingredient, a menthol flavored ingredient, a cotton candy flavored ingredient, and mixtures thereof. The one or more sweetening agents comprise glycerin, monoammonium glycyrrhizinate, saccharin sodium, acesulfame potassium, high fructose corn syrup, and/or mixtures thereof. Pharmaceutical compositions of the invention include a flavoring system of the invention, a solvent system, and at least one pharmaceutically active agent, such as lopinavir or derivatives thereof, ritonavir or derivatives thereof, or mixtures thereof. Methods for making such liquid pharmaceutical compositions are also disclosed.

公开(公告)号：US06193954B1

公开(公告)日：2001-02-27

申请号：US08822631

申请日：1997-03-21

申请人： Akwete L. Adjei ,  Jack Zheng ,  Pramod K. Gupta ,  Kennan C. Marsh ,  Vivian Wu ,  Dennis Y. Lee

发明人： Akwete L. Adjei ,  Jack Zheng ,  Pramod K. Gupta ,  Kennan C. Marsh ,  Vivian Wu ,  Dennis Y. Lee

IPC分类号： A61L904

CPC分类号： A61K9/008 ,  A61K31/473

摘要： The present invention relates to methods and formulations for administering a dopamine agonist to the airways of a patient. The preferred dopamine agonist is selected from (5aR-trans)-4,5,6,7,11b-hexahydro-2-propylbenzo[f]thieno[2,3-c]quinoline- 9,10) -diol, diacetate (ester) hydrochloride. The delivery method relates to certain aerosol formulations and liquid formulations which are administered into the airways to provide effective delivery of the dopamine agonists to the receptor.

摘要翻译： 本发明涉及向患者的气道施用多巴胺激动剂的方法和制剂。 优选的多巴胺激动剂选自（5aR-反式）-4,5,6,7,11b-六氢-2-丙基苯并[f]噻吩并[2,3-c]喹啉-9,10） - 二醇，二乙酸酯 酯）盐酸盐。 递送方法涉及给气道中的某些气雾剂和液体制剂，以提供多巴胺激动剂向受体的有效递送。

公开(公告)号：US5610193A

公开(公告)日：1997-03-11

申请号：US650261

申请日：1996-05-22

申请人： Laman A. Al-Razzak ,  Kennan C. Marsh ,  Richard A. Pyter

发明人： Laman A. Al-Razzak ,  Kennan C. Marsh ,  Richard A. Pyter

IPC分类号： C07D277/28 ,  A61K9/14 ,  A61K9/18 ,  A61K9/48 ,  A61K31/425 ,  A61K31/426 ,  A61K45/00 ,  A61P43/00 ,  A61K31/16 ,  A61K31/695

CPC分类号： A61K9/4841 ,  A61K31/425 ,  A61K9/143 ,  A61K9/485 ,  Y10S514/962

摘要： A solid pharmaceutical composition is disclosed which comprises a pharmaceutically acceptable adsorbent or a mixture of pharmaceutically acceptable adsorbents to which is adsorbed a mixture of (1) a pharmaceutically acceptable organic solvent or a mixture of pharmaceutically acceptable organic solvents, (2) an HIV protease inhibiting compound and (3) one or more pharmaceutically acceptable acids. The solid composition can optionally be encapsulated in a hard gelatin capsule.

摘要翻译： 公开了一种固体药物组合物，其包含药学上可接受的吸附剂或药学上可接受的吸附剂的混合物，其吸附了（1）药学上可接受的有机溶剂或药学上可接受的有机溶剂的混合物的混合物，（2）HIV蛋白酶抑制 化合物和（3）一种或多种药学上可接受的酸。 固体组合物可任选地包封在硬明胶胶囊中。

公开(公告)号：US5876749A

公开(公告)日：1999-03-02

申请号：US435918

申请日：1995-05-04

申请人： Laman A. Al-Razzak ,  Kennan C. Marsh ,  Dilip Kaul ,  Lourdes P. Manning

发明人： Laman A. Al-Razzak ,  Kennan C. Marsh ,  Dilip Kaul ,  Lourdes P. Manning

IPC分类号： C07D277/28 ,  A61K9/48 ,  A61K31/00 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/551 ,  A61K31/635 ,  A61P31/12 ,  A61P37/04 ,  A61P43/00

CPC分类号： A61K31/635 ,  A61K31/00 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/551 ,  A61K9/4858

摘要： A pharmaceutical composition is disclosed which comprises a solution of an HIV protease inhibiting compound in a pharmaceutically acceptable organic solvent comprising a pharmaceutically acceptable alcohol. The composition can optionally comprise a pharmaceutically acceptable acid or a combination of pharmaceutically acceptable acids. The solution can optionally be encapsulated in hard gelatin capsules or soft elastic gelatin capsules. The solution can optionally be granulated with a pharmaceutically acceptable granulating agent.

公开(公告)号：US5725878A

公开(公告)日：1998-03-10

申请号：US435009

申请日：1995-05-04

申请人： Laman A. Al-Razzak ,  Kennan C. Marsh ,  Dilip Kaul ,  Lourdes P. Manning

发明人： Laman A. Al-Razzak ,  Kennan C. Marsh ,  Dilip Kaul ,  Lourdes P. Manning

IPC分类号： C07D277/28 ,  A61K9/48 ,  A61K31/00 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/551 ,  A61K31/635 ,  A61P31/12 ,  A61P37/04 ,  A61P43/00

CPC分类号： A61K31/635 ,  A61K31/00 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/551 ,  A61K9/4858

摘要： A pharmaceutical composition is disclosed which comprises a solution of an HIV protease inhibiting compound in a pharmaceutically acceptable organic solvent comprising a pharmaceutically acceptable alcohol. The composition can optionally comprise a pharmaceutically acceptable acid or a combination of pharmaceutically acceptable acids. The solution can optionally be encapsulated in hard gelatin capsules or soft elastic gelatin capsules. The solution can optionally be granulated with a pharmaceutically acceptable granulating agent.

摘要翻译： 公开了一种药物组合物，其包含HIV蛋白酶抑制化合物在包含药学上可接受的醇的药学上可接受的有机溶剂中的溶液。 组合物可任选地包含药学上可接受的酸或药学上可接受的酸的组合。 该溶液可任选地包封在硬明胶胶囊或软弹性明胶胶囊中。 该溶液可以任选地用药学上可接受的制粒剂造粒。

公开(公告)号：US20090105267A1

公开(公告)日：2009-04-23

申请号：US12208604

申请日：2008-09-11

申请人： Marlon D. Cowart ,  Kennan C. Marsh ,  Huaqing Liu ,  Jae Y. Lee ,  Maria G. Beconi ,  Jill M. Wetter ,  Lawrence A. Black ,  Thomas C. Custer

发明人： Marlon D. Cowart ,  Kennan C. Marsh ,  Huaqing Liu ,  Jae Y. Lee ,  Maria G. Beconi ,  Jill M. Wetter ,  Lawrence A. Black ,  Thomas C. Custer

IPC分类号： A61K31/501 ,  C07D487/04 ,  A61P25/28

CPC分类号： C07D487/04

摘要： The invention relates to octahydro-pyrrolo[3,4-b]pyrrole N-oxides as prodrugs of CNS-active compounds, compositions comprising such compounds, methods for making the compounds, salts, and polymorphs, and methods of treating conditions and disorders using such compounds and compositions. Octahydro-pyrrolo[3,4-b]pyrrole N-oxides of formula (I) are prodrugs of histamine-3 antagonists, and are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole N-oxide compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

摘要翻译： 本发明涉及作为CNS活性化合物前药的八氢吡咯并[3,4-b]吡咯N-氧化物，包含这些化合物的组合物，制备化合物，盐和多晶型物的方法，以及使用 这些化合物和组合物。 式（I）的八氢 - 吡咯并[3,4-b]吡咯N-氧化物是组胺-3拮抗剂的前药，可用于治疗组胺-3受体配体预防或改善的病症或病症。 八氢吡咯并[3,4-b]吡咯N-氧化物化合物，使用这些化合物的方法，制备它们的组合物，以及这些化合物的制备方法。

公开(公告)号：US5559158A

公开(公告)日：1996-09-24

申请号：US297004

申请日：1994-08-31

申请人： Laman A. Al-Razzak ,  Kennan C. Marsh ,  Richard A. Pyter

发明人： Laman A. Al-Razzak ,  Kennan C. Marsh ,  Richard A. Pyter

IPC分类号： C07D277/28 ,  A61K9/14 ,  A61K9/18 ,  A61K9/48 ,  A61K31/425 ,  A61K31/426 ,  A61K45/00 ,  A61P43/00 ,  A61K31/16 ,  A61K31/42 ,  A61K31/695

CPC分类号： A61K9/4841 ,  A61K31/425 ,  A61K9/143 ,  A61K9/485 ,  Y10S514/962

摘要： A solid pharmaceutical composition is disclosed which comprises a pharmaceutically acceptable adsorbent or a mixture of pharmaceutically acceptable adsorbents to which is adsorbed a mixture of (1) a pharmaceutically acceptable organic solvent or a mixture of pharmaceutically acceptable organic solvents, (2) an HIV protease inhibiting compound and (3) one or more pharmaceutically acceptable acids. The solid composition can optionally be encapsulated in a hard gelatin capsule.

摘要翻译： 公开了一种固体药物组合物，其包含药学上可接受的吸附剂或药学上可接受的吸附剂的混合物，其吸附了（1）药学上可接受的有机溶剂或药学上可接受的有机溶剂的混合物的混合物，（2）HIV蛋白酶抑制 化合物和（3）一种或多种药学上可接受的酸。 固体组合物可任选地包封在硬明胶胶囊中。

公开(公告)号：US08901157B2

公开(公告)日：2014-12-02

申请号：US12958899

申请日：2010-12-02

申请人： Dale J. Kempf ,  Kennan C. Marsh

发明人： Dale J. Kempf ,  Kennan C. Marsh

IPC分类号： A61K31/407 ,  A61K31/4965 ,  A61K31/497 ,  A61K38/21 ,  A61K31/403 ,  A61K31/7056

CPC分类号： A61K38/212 ,  A61K31/407 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/7056 ,  A61K2300/00

摘要： The present invention discloses compositions and a method of improving the pharmacokinetics of pharmaceutical agents (or pharmaceutically acceptable salts, esters, and prodrugs thereof) which are metabolized by cytochrome P450 monoxygenase comprising coadministering ritonavir or a pharmaceutically acceptable salt, ester, and prodrug thereof.

摘要翻译： 本发明公开了通过包含联合利托那韦或其药学上可接受的盐，酯和前药的细胞色素P450单加氧酶代谢的药物（或其药学上可接受的盐，酯和前体药物）的药代动力学的组合物和方法。

公开(公告)号：US20120277190A1

公开(公告)日：2012-11-01

申请号：US13544130

申请日：2012-07-09

申请人： Arthur R. Gomtsyan ,  Erol K. Bayburt ,  John R. Koenig ,  Kennan C. Marsh ,  Robert G. Schmidt, JR. ,  Chih-Hung Lee ,  Weili Wang ,  Jerome F. Daanen ,  Brian S. Brown

发明人： Arthur R. Gomtsyan ,  Erol K. Bayburt ,  John R. Koenig ,  Kennan C. Marsh ,  Robert G. Schmidt, JR. ,  Chih-Hung Lee ,  Weili Wang ,  Jerome F. Daanen ,  Brian S. Brown

IPC分类号： A61K31/5377 ,  C07D231/56 ,  A61K31/416 ,  A61P13/10 ,  A61K31/454 ,  C07F9/09 ,  A61K31/675 ,  A61P25/00 ,  C07D413/06 ,  C07D401/12

CPC分类号： C07D405/12 ,  C07D231/56 ,  C07D403/12 ,  C07F9/65038

摘要： Compounds of formula (I) wherein A, R1, R2, and R3 are defined in the specification, and which are useful as therapeutic compounds particularly for treating disorders or conditions associated with inflammation, pain, bladder overactivity, urinary incontinence, and other disorders caused by or exacerbated by TRPV1.

摘要翻译： 其中A，R 1，R 2和R 3在本说明书中定义并且可用作特别用于治疗与炎症，疼痛，膀胱过度活动，尿失禁和其他疾病相关的疾病或病症的治疗化合物的式（I）化合物 由TRPV1引起或加剧。