公开(公告)号：US20040254171A1

公开(公告)日：2004-12-16

申请号：US10846978

申请日：2004-05-14

Applicant: Dynogen, Inc.

Inventor： Steven B. Landau ,  Cheryl L. Miller ,  Karl B. Thor

IPC: A61K031/551 ,  A61K031/519

CPC classification number: A61K31/135 ,  A61K31/519 ,  A61K31/535 ,  A61K31/551 ,  A61K41/00 ,  A61K45/06 ,  A61K2300/00

Abstract: The invention relates to a method of treating nausea, vomiting, retching or any combination thereof in a subject in need of treatment. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of treating nausea, vomiting, retching or any combination thereof in a subject in need thereof, comprising coadministering to said subject a first amount of a 5-HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount. In addition, the method of the invention comprises administering a NARI alone.

公开(公告)号：US20040248884A1

公开(公告)日：2004-12-09

申请号：US10770382

申请日：2004-02-02

Applicant: AVENTIS PHARMA S.A.

Inventor： Marcel Patek ,  Anil Nair ,  Augustin Hittinger ,  Conception Nemecek ,  Daniel Bond ,  Greg Harlow ,  Herve Bouchard ,  Jacques Mauger ,  Jean-Luc Malleron ,  Mark Palermo ,  Fahad Al-Obeidi ,  Thomas Faitg ,  Hartmut Strobel ,  Sven Ruf ,  Kurt Ritter ,  Youssef El-Ahmad ,  Dominique Lesuisse

IPC: A61K031/551 ,  A61K031/513 ,  C07D49/02 ,  C07D45/02

CPC classification number: C07D401/06 ,  C07D401/14

Abstract: The present invention relates to a cyclic urea compound of formula I: 1 as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.

Abstract translation: 本发明涉及式I的环脲化合物：如本文所定义。 本发明还涉及其制备方法，包含其的药物组合物及其药物用途，作为蛋白激酶上的抑制剂。 因此，通过抑制蛋白激酶（例如实体瘤）的活性来预防或治疗能够调节的生理障碍是有用的。

公开(公告)号：US20040248825A1

公开(公告)日：2004-12-09

申请号：US10809127

申请日：2004-03-25

Applicant: St. Jude Children's Research Hospital

Inventor： Jonathan A. McCullers

IPC: A61K031/7056 ,  A61K031/551

CPC classification number: A61K45/06 ,  A61K31/00 ,  A61K31/196 ,  A61K31/215 ,  A61K31/551 ,  A61K31/60 ,  A61K31/7012 ,  A61K31/7056 ,  A61K2300/00

Abstract: The invention provides a novel use for neuraminidase inhibitors in chemoprophylactic and treatment methods for the prevention, attenuation and treatment of bacterial infections that may occur in association with, or as a sequelae of, viral influenza. The prophylactic methods of the invention are particularly suitable for the prevention of secondary bacterial infections, such as, but not limited to infections of the lower respiratory tract (e.g., pneumonia), middle ear infections (e.g., otitis media) and bacterial sinusitis. The treatment methods are suitable for use in protocols designed to attenuate or treat bacterial infections that occur concurrent with, or as a sequelae of the flu.

Abstract translation: 本发明提供了用于预防，减弱和治疗可能与病毒流感相关联或作为后遗症发生的细菌感染的化学预防和治疗方法中的神经氨酸酶抑制剂的新用途。 本发明的预防方法特别适用于预防继发性细菌感染，例如但不限于下呼吸道感染（例如肺炎），中耳感染（例如中耳炎）和细菌性鼻窦炎。 治疗方法适用于设计用于减弱或治疗与流感并发或作为后遗症发生的细菌感染的方案。

公开(公告)号：US20040235855A1

公开(公告)日：2004-11-25

申请号：US10815017

申请日：2004-03-31

Inventor： Bharat Lagu ,  Meng Pan ,  Kenneth Rupert ,  Michael Wachter

IPC: A61K031/496 ,  A61K031/495 ,  A61K031/551

CPC classification number: C07D295/192 ,  C07D295/155

Abstract: This invention is directed to heterocyclyl-substituted anilino phospholipase C inhibitor compounds useful in treating or ameliorating an inflammatory disorders and/or restenosis of the general formula (I): 1 and enantiomers, diastereomers and pharmaceutically acceptable salts thereof. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions affected by phospholipase modulation.

公开(公告)号：US20040208921A1

公开(公告)日：2004-10-21

申请号：US10757775

申请日：2004-01-14

Inventor： Rodney J. Y. Ho ,  Che-Chung Tsai

IPC: A61K009/127 ,  A61K031/551

CPC classification number: A61K9/127 ,  A61K47/6911

Abstract: Various embodiments of the present invention are directed to lipid-pharmaceutical compositions and related methods for producing a lipid-drug complex under conditions near the neutral pH range. Optimal pH range is provided for the efficient incorporation of various lipid-drug complexes. A lipid-drug complex, such as a liposome, readily encapsulates drugs having low aqueous solubility within a neutral pH range. In some embodiments, the lipid-drug complex comprises a lipid bilayer and a lipid-soluble drug having a range of molar ratio values of lipid-to-drug from about 3:1 to about 100:1 or higher for relatively toxic drugs. Lipid-drug complexes can also be formed within a range of molar ratios from about 3:1 to about 10:1, and a range of molar ratios from about 5:1 to about 7:1. In various embodiments, biomolecules, such as nucleic acids and proteins, that can have pharmacological activities may also be incorporated within lipid vesicles. The methods for targeting lymphoid tissue involve subcutaneous administration of lipid-drug complexes and lipid-biomolecule complexes, and not by systemic administration.

Abstract translation: 本发明的各种实施方案涉及脂质 - 药物组合物和在接近中性pH范围的条件下生产脂质 - 药物复合物的相关方法。 提供了最佳的pH范围，用于有效地掺入各种脂质 - 药物复合物。 脂质体复合物，例如脂质体，容易地将具有低水溶性的药物包封在中性pH范围内。 在一些实施方案中，脂质 - 药物复合物包含脂质双层和脂质可溶性药物，对于相对毒性的药物，脂质与药物的摩尔比值范围为约3:1至约100:1或更高。 脂质 - 药物复合物也可以在约3:1至约10:1的摩尔比范围和约5:1至约7:1的摩尔比范围内形成。 在各种实施方案中，可以具有药理活性的生物分子，例如核酸和蛋白质也可以并入脂质囊泡中。 用于靶向淋巴组织的方法包括皮下施用脂质 - 药物复合物和脂质 - 生物分子复合物，而不是全身给药。

公开(公告)号：US20040180877A1

公开(公告)日：2004-09-16

申请号：US10482363

申请日：2003-12-30

Inventor： Dan Peters ,  Gunnar M Olsen ,  Elsebert Ostergaard Nielsen ,  Philip K ahring ,  Tino Dyhring Jorgensen

IPC: A61K031/551 ,  A61K031/519 ,  A61K031/496

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D333/66 ,  C07D409/04 ,  C07D417/04 ,  C07D451/02 ,  C07D451/14 ,  C07D453/02 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08

Abstract: The present invention relates to novel compounds that are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

Abstract translation: 本发明涉及在烟碱乙酰胆碱受体和单胺受体和转运蛋白的调节剂中被发现是胆碱能配体的新化合物。 由于其药理学特征，本发明的化合物可用于治疗与中枢神经系统（CNS），周围神经系统（PNS），疾病或病症相关的胆碱能系统相关的疾病或障碍 平滑肌肉收缩，内分泌疾病或病症，与神经变性相关的疾病或病症，与由化学物质的滥用终止引起的炎症，疼痛和戒断症状相关的疾病或病症。

公开(公告)号：US20040157831A1

公开(公告)日：2004-08-12

申请号：US10770894

申请日：2004-02-03

Applicant: Pharmacia & Upjohn Company

Inventor： William W. McWhorter JR.

IPC: A61K031/551 ,  C07D498/04 ,  C07D491/04 ,  A61K031/542 ,  A61K031/538

CPC classification number: C07D498/16 ,  C07D513/16

Abstract: The present invention provides compounds of Formula (I): 1 wherein R1, R2, R3, R4, R5, R6, R7, and R8 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands, and are useful for treating diseases whereas modulation of 5-HT activity is desired.

Abstract translation: 本发明提供式（I）化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 7， 8>具有说明书中定义的任何值，以及包含该化合物的药物组合物。 本发明还提供治疗方法以及可用于制备式（I）化合物的方法和中间体。 该化合物是5-HT配体，并且可用于治疗疾病，而期望5-HT活性的调节。

公开(公告)号：US20040147510A1

公开(公告)日：2004-07-29

申请号：US10757981

申请日：2004-01-13

Applicant: Dynogen Pharmaceuticals, Inc.

Inventor： Steven B. Landau ,  Cheryl L. Miller ,  Karl B. Thor

IPC: A61K031/551 ,  A61K031/519

CPC classification number: A61K31/135 ,  A61K31/519 ,  A61K31/535 ,  A61K31/551 ,  A61K41/00 ,  A61K45/06 ,  A61K2300/00

Abstract: The invention relates to a method of treating nausea, vomiting, retching or any combination thereof in a subject in need of treatment. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of treating nausea, vomiting, retching or any combination thereof in a subject in need thereof, comprising coadministering to said subject a first amount of a 5-HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount. In addition, the method of the invention comprises administering a NARI alone.

Abstract translation: 本发明涉及在需要治疗的受试者中治疗恶心，呕吐，呕吐或其任何组合的方法。 该方法包括向需要治疗的受试者施用治疗有效量的具有5-HT 3受体拮抗剂活性的化合物和NorAdrenaline再摄取抑制剂（NARI）活性。 本发明还涉及在有需要的受试者中治疗恶心，呕吐，呕吐或其任何组合的方法，包括向所述受试者加入第一量的5-HT 3拮抗剂和第二量的NARI，其中第一 并且第二量一起包含治疗有效量或者以治疗有效量存在。 此外，本发明的方法包括单独施用NARI。

公开(公告)号：US20040142926A1

公开(公告)日：2004-07-22

申请号：US10659537

申请日：2003-09-10

Inventor： Deborah Ann Evrard ,  Dahui Zhou ,  Gary Paul Stack ,  Aranapakam Madumbai Venkatesan ,  Amedeo A. Failli ,  Susan Christman Croce

IPC: A61K031/551 ,  A61K031/496 ,  C07D47/14

CPC classification number: C07D491/04 ,  Y02P20/582

Abstract: Compounds of the formula I: 1 are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

Abstract translation: 式I化合物可用于治疗抑郁症（包括但不限于重度抑郁症，儿童抑郁症和抑郁症），焦虑症，恐慌症，创伤后应激障碍，经前期焦虑症（也称为月经前） 综合征），注意缺陷障碍（伴有和不伴有多动症），强迫症，社会焦虑症，广泛性焦虑症，肥胖症，进食障碍如神经性厌食症和神经性贪食症，血管舒缩性潮红，可卡因和酒精成瘾，性功能障碍及相关 疾病

公开(公告)号：US20040127422A1

公开(公告)日：2004-07-01

申请号：US10351608

申请日：2003-01-24

Inventor： Roland Buelow ,  Suhasini Iyer ,  Satya Dandekar

IPC: A61K038/08 ,  A61K031/7072 ,  A61K031/551

CPC classification number: A61K38/08 ,  A61K38/19 ,  A61K2300/00

Abstract: The present invention relates to pharmaceutical preparations and methods for treating individuals infected with the human immunodeficiency virus (HIV). The pharmaceutical preparations comprise an immunomodulating agent and a anti-retroviral compound. The pharmaceutical preparations are used to treat HIV infected patients, particularly for gastrointestinal complications arising from viral infection. In addition, the pharmaceutical preparations of the present invention have the effect of raising the levels of CD4null single positive and CD4null and CD8null double positive T cells, thus promoting restoration and normalization of the immune system following HIV infection.

Abstract translation: 本发明涉及用于治疗感染人类免疫缺陷病毒（HIV）的个体的药物制剂和方法。 药物制剂包含免疫调节剂和抗逆转录病毒化合物。 药物制剂用于治疗HIV感染的患者，特别是用于病毒感染引起的胃肠道并发症。 此外，本发明的药物制剂具有提高CD4 +单阳性和CD4 +和CD8 +双重阳性T细胞的水平的作用，从而促进HIV后的免疫系统的恢复和正常化 感染。