Transnasal anticonvulsive compositions and modulated process
    11.
    发明授权
    Transnasal anticonvulsive compositions and modulated process 失效
    经鼻抗惊厥组合物和调节过程

    公开(公告)号:US06627211B1

    公开(公告)日:2003-09-30

    申请号:US09624305

    申请日:2000-07-24

    IPC分类号: A61F1300

    摘要: A method of vehicle modulated administration of an anticonvulsive agent to the nasal mucous membranes of humans and animals is disclosed. The vehicle system is an aqueous pharmaceutical carrier comprising an aliphatic alcohol, a glycol and a biological surfactant such as a bile salt or a lecithin. The pharmaceutical composition provides a means to control and promote the rate and extent of transmucosal permeation and absorption of the medicaments via a single and multiple administration. Nasal administration of the pharmaceutical preparation produces a high plasma concentration of the anticonvulsant nearly as fast as intravenous administration. Such compositions are particularly suitable for a prompt and timely medication of patients in the acute and/or emergency treatment of status epilepticus and other fever-induced seizures.

    摘要翻译: 公开了一种向人和动物的鼻粘膜施用抗惊厥药的车辆调节方法。 载体系统是包含脂族醇,二醇和生物表面活性剂如胆汁盐或卵磷脂的水性药物载体。 药物组合物通过单次和多次施用提供控制和促进药物经粘膜渗透和吸收的速率和程度的手段。 药物制剂的鼻内给药几乎与静脉内施用一样快地产生抗惊厥药的高血浆浓度。 这种组合物特别适用于急性和/或紧急治疗癫痫持续状态和其他发热引起的发作的患者的及时和及时的药物。

    Substituted carboxylic acid derivatives for the treatment of diabetes and lipid disorders, their preparation and use
    14.
    发明授权
    Substituted carboxylic acid derivatives for the treatment of diabetes and lipid disorders, their preparation and use 失效
    用于治疗糖尿病和脂质疾病的取代的羧酸衍生物,其制备和用途

    公开(公告)号:US07456293B2

    公开(公告)日:2008-11-25

    申请号:US11391031

    申请日:2006-03-28

    IPC分类号: A61K31/4184 C07D235/04

    CPC分类号: C07D235/10

    摘要: The present invention is concerned with racemic or enantiomerically enriched substituted carboxylic acids and derivatives thereof represented by Formula 1; or pharmaceutically acceptable salts thereof. The present invention also includes pharmaceutical compositions comprising an effective amount of a compound of Formula 1 in admixture with a pharmaceutically acceptable carrier or excipient. The compositions may include additional therapeutic agents for combination therapy. The present invention provides a new class of pharmaceutically active compounds, which are useful in the treatment and control of diabetes and its related metabolic diseases.

    摘要翻译: 本发明涉及由式1表示的外消旋或对映体富集的取代羧酸及其衍生物; 或其药学上可接受的盐。 本发明还包括药物组合物,其包含与药学上可接受的载体或赋形剂混合的有效量的式1化合物。 组合物可以包括用于组合治疗的其它治疗剂。 本发明提供了一类新的药物活性化合物,其可用于治疗和控制糖尿病及其相关代谢疾病。

    Transnasal microemulsions containing diazepam
    15.
    发明申请
    Transnasal microemulsions containing diazepam 审中-公开
    经鼻微乳液含地西泮

    公开(公告)号:US20050002987A1

    公开(公告)日:2005-01-06

    申请号:US10869195

    申请日:2004-06-16

    摘要: Diazepam is administered intranasally in the form of specific microemulsions having advantageous properties. The microemulsions are comprised of about equal quantities of a fatty acid and water with the remainder being a hydrophilic surfactant, a polar solvent and an alcohol in a weight ratio such that alcohol is present in a greater quantity by weight than either of the other two. Nasal administration of the subject microemulsions produces a high plasma concentration of diazepam nearly as fast as intravenous administration. The present microemulsions are particularly suitable for a prompt and timely treatment of patients in the acute and/or emergency treatment of status epilepticus and other fever-induced seizures.

    摘要翻译: 地西泮以具有有利性质的特定微乳液的形式鼻内施用。 微乳液由约等量的脂肪酸和水组成,其余部分是亲水性表面活性剂,极性溶剂和醇,其重量比使得醇以比其它两种重量更大的量存在。 目标微乳液的鼻腔给药产生几乎与静脉内给药相当快的地西泮的高血浆浓度。 目前的微乳液特别适用于急性和/或紧急治疗癫痫持续状态和其他发热引起的癫痫发作的患者及时及时的治疗。

    Carbamate compounds for use in preventing or treating bipolar disorder
    16.
    发明授权
    Carbamate compounds for use in preventing or treating bipolar disorder 有权
    用于预防或治疗双相情感障碍的氨基甲酸酯化合物

    公开(公告)号:US06562867B2

    公开(公告)日:2003-05-13

    申请号:US10081766

    申请日:2002-02-21

    IPC分类号: A61K3127

    CPC分类号: A61K31/27

    摘要: This invention is directed to a method for preventing or treating bipolar disorder comprising administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I): wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1 and R2 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

    摘要翻译: 本发明涉及一种预防或治疗双相情感障碍的方法,包括向有需要的受试者施用治疗有效量的式(I)化合物:其中苯基在X被一至五个选自下列的卤素原子取代: 由氟,氯,溴和碘组成; 并且R 1和R 2独立地选自氢和C 1 -C 4烷基; 其中C 1 -C 4烷基任选被苯基取代(其中苯基任选被独立地选自卤素,C 1 -C 4烷基,C 1 -C 4烷氧基,氨基,硝基和氰基的取代基取代)。

    Tetrahydroisoquinolinealkanol derivatives and pharmaceutical
compositions containing same
    17.
    发明授权
    Tetrahydroisoquinolinealkanol derivatives and pharmaceutical compositions containing same 失效
    四氢异喹啉烷醇衍生物和含有它们的药物组合物

    公开(公告)号:US5955471A

    公开(公告)日:1999-09-21

    申请号:US995645

    申请日:1998-01-13

    申请人: Yong Moon Choi

    发明人: Yong Moon Choi

    摘要: The present invention provides novel 1,2,3,4-tetrahydroisoquinoline carbamate and thiocarbamate derivatives represented by Formula I ##STR1## wherein: X.sub.1 and X.sub.2 are the same or different from each other and independently represent a a member selected from the group consisting of hydrogen, alkyl, alkoxy, thioalkoxy, halogen, hydroxy, nitro and trifluorocarbon;Y is a member selected from the group consisting of oxygen and sulfur;R.sub.1 is a member selected from the group consisting of hydrogen, alkyl, arylalkyl, and CONHR' where R' is selected from the group consisting of hydrogen, alkyl, arylalkyl and aryl;R.sub.2 and R.sub.3 are the same or different from each other and independently represent a member selected from the group consisting of hydrogen, alkyl, arylalkyl, and cycloalkyl, or R.sub.2 and R.sub.3 may form a 5 to 7-membered ring together with the nitrogen atom to which they are bonded;R.sub.4 is a member selected from the group consisting of hydrogen or lower alkyl; andnontoxic pharmacologically acceptable salts thereof.Compounds are useful in the treatment of central nervous system disorders, including depression.

    摘要翻译: 本发明提供由式I表示的新的1,2,3,4-四氢异喹啉氨基甲酸酯和硫代氨基甲酸酯衍生物,其中:X 1和X 2彼此相同或不同,并且独立地表示选自氢,烷基, 烷氧基,硫代烷氧基,卤素,羟基,硝基和三氟碳; Y是选自氧和硫的成员; R1是选自氢,烷基,芳烷基和CONHR'的成员,其中R'选自氢,烷基,芳烷基和芳基; R2和R3彼此相同或不同,并且独立地表示选自氢,烷基,芳基烷基和环烷基的成员,或者R2和R3可以与氮原子一起形成5至7元环至 他们联系在一起 R4是选自氢或低级烷基的成员; 和无毒的药理学上可接受的盐。 化合物可用于治疗中枢神经系统疾病,包括抑郁症。