知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

17 条记录 (耗时 0.03 秒)

    Nitrogen containing heterobicycles as factor Xa inhibitors
    1.
    发明授权
    Nitrogen containing heterobicycles as factor Xa inhibitors 有权
    含氮杂双环作为因子Xa抑制剂

    公开(公告)号：US06716841B2

    公开(公告)日：2004-04-06

    申请号：US10205792

    申请日：2002-07-26

    申请人： Irina C. Jacobson ,  Mimi L. Quan

    发明人： Irina C. Jacobson ,  Mimi L. Quan

    IPC分类号： A61K31423

    CPC分类号： C07D403/06 ,  C07D413/14

    摘要： This invention relates generally to nitrogen containing heterobicycles of formulas A and B: which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.

    摘要翻译： 本发明一般涉及式A和B的含氮杂双环：其是胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa，含有它们的药物组合物，以及使用其作为抗凝血剂治疗和预防血栓栓塞的方法 疾病

    Indane derivatives
    3.
    发明授权
    Indane derivatives 有权
    茚满衍生物

    公开(公告)号：US06762199B2

    公开(公告)日：2004-07-13

    申请号：US10229592

    申请日：2002-08-28

    申请人： Garry Fenton ,  Clive McCarthy ,  Robert Edward MacKenzie ,  Andrew David Morley

    发明人： Garry Fenton ,  Clive McCarthy ,  Robert Edward MacKenzie ,  Andrew David Morley

    IPC分类号： A61K31423

    CPC分类号： C07D263/58 ,  C07D235/30

    摘要： The invention is directed to physiologically active compounds of general formula (I): wherein: R1 represents aryl, heteroaryl or a group R3—L2—Ar1—L3—; R2 represents hydrogen or lower alkyl; R3 represents aryl or heteroaryl; and Ar1 represents an optionally substituted saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring system containing at least one heteroatom selected from O, S or N; Y is carboxy or an acid bioisostere; and their corresponding N-oxides or prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their corresponding N-oxides or prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).

    摘要翻译： 本发明涉及通式（I）的生理活性化合物：其中：R 1表示芳基，杂芳基或基团R 3 -L 2 -Ar 1 -L 3 - ; R R 2表示氢或低级烷基; R 3表示芳基或杂芳基; 并且Ar 1表示任选取代的饱和，部分饱和或完全不饱和的8至10元双环体系，其含有至少一个选自O，S或N的杂原子; Y是羧基或酸式生物电子等排体;及其相应的N-氧化物或 这些化合物具有有价值的药物性质，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1）的相互作用的能力， 。

    Methods for treating neuropathic pain using heteroarylmethanesulfonamides
    4.
    发明授权
    Methods for treating neuropathic pain using heteroarylmethanesulfonamides 失效
    使用杂芳基甲烷磺酰胺治疗神经性疼痛的方法

    公开(公告)号：US06489350B1

    公开(公告)日：2002-12-03

    申请号：US09663107

    申请日：2000-09-15

    申请人： Mark J. Benedyk

    发明人： Mark J. Benedyk

    IPC分类号： A61K31423

    CPC分类号： A61K31/423

    摘要： A method of treating neuropathic pain and its progression is disclosed comprising administering to a subject a compound of formula wherein R is hydrogen or a halogen atom, R2 and R3 are the same or different and are each hydrogen or a straight or branched alkyl having 1 to 3 carbon atoms, and one of X and Y is a carbon atom and another is a nitrogen atoms, provided that the methanesulfonamide group is bonded to the carbon atom of either X and Y, exemplified by zonisamide.

    摘要翻译： 公开了一种治疗神经性疼痛及其进展的方法，其包括向受试者施用糠醛的化合物，R为氢或卤素原子，R 2和R 3相同或不同，为氢或具有1至3个碳原子的直链或支链烷基 碳原子，X和Y中的一个是碳原子，另一个是氮原子，条件是甲磺酰胺基团与X和Y的碳原子结合，例如唑尼沙胺。

    Heteroatom substituted benzoyl derivatives that enhance synaptic responses mediated by AMPA receptors
    5.
    发明授权
    Heteroatom substituted benzoyl derivatives that enhance synaptic responses mediated by AMPA receptors 失效
    杂原子取代的苯甲酰基衍生物，其增强AMPA受体介导的突触反应

    公开(公告)号：US06274600B1

    公开(公告)日：2001-08-14

    申请号：US09286167

    申请日：1999-04-05

    申请人： Gary S. Lynch ,  Gary A. Rogers

    发明人： Gary S. Lynch ,  Gary A. Rogers

    IPC分类号： A61K31423

    CPC分类号： C07D235/06 ,  C07D235/08 ,  C07D241/42 ,  C07D263/56 ,  C07D317/60 ,  C07D319/18 ,  C07D319/20 ,  C07D405/06

    摘要： Compounds are useful for enhancing synaptic responses mediated by AMPA receptors are disclosed, as are methods for the preparation thereof and methods for their use for treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors and for improving memory encoding.

    摘要翻译： 公开了用于增强由AMPA受体介导的突触反应的化合物，以及其制备方法及其用于治疗由于兴奋性突触的数目的缺陷而受神经功能受损或智力功能受损的受试者的方法 AMPA受体。 本发明化合物还可用于治疗非受损受试者，以提高依赖于使用AMPA受体的脑网络和改善记忆编码的感觉运动和认知任务中的表现。

    Isoindole derivatives
    6.
    发明授权
    Isoindole derivatives 失效
    异吲哚衍生物

    公开(公告)号：US06777410B2

    公开(公告)日：2004-08-17

    申请号：US10408220

    申请日：2003-04-08

    申请人： Toshio Nagase ,  Tomoharu Iino ,  Yoshiyuki Sato ,  Teruyuki Nishimura ,  Jun-ichi Eiki

    发明人： Toshio Nagase ,  Tomoharu Iino ,  Yoshiyuki Sato ,  Teruyuki Nishimura ,  Jun-ichi Eiki

    IPC分类号： A61K31423

    CPC分类号： C07D498/04

    摘要： This invention relates to compounds represented by the general formula [I] wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及由通式[I]表示的化合物，其中R表示叠氮基等，R 1和R 2相同或不同，表示氢原子等，R 3， 和R 4相同或不同，表示氢原子等，X 1表示氧原子等，X 2表示氧原子等，Y表示氧原子等，Z表示缩合 芳基等，或其药学上可接受的盐，其制备方法和用于治疗糖尿病的药物，用于糖尿病慢性并发症的预防剂或抗肥胖药物，其含有作为有效成分的化合物或药学上可接受的盐 其可接受的盐。

    Anilide compounds, including use thereof in ACAT inhibitition
    8.
    发明授权
    Anilide compounds, including use thereof in ACAT inhibitition 失效
    酰苯胺化合物，包括其在ACAT抑制中的用途

    公开(公告)号：US06204278B1

    公开(公告)日：2001-03-20

    申请号：US08858244

    申请日：1997-05-19

    申请人： Kimiyuki Shibuya ,  Katsumi Kawamine ,  Yukihiro Sato ,  Toshiyuki Edano ,  Souhei Tanabe ,  Masami Shiratsuchi

    发明人： Kimiyuki Shibuya ,  Katsumi Kawamine ,  Yukihiro Sato ,  Toshiyuki Edano ,  Souhei Tanabe ,  Masami Shiratsuchi

    IPC分类号： A61K31423

    CPC分类号： C07D263/58 ,  C07D235/28 ,  C07D277/70

    摘要： The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: where Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NH6—; R6 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.

    摘要翻译： 本发明提供了新的酰苯胺化合物和包含它们的药物组合物。本发明涉及下式的化合物：其中Ar是任选取代的芳基; R 4和R 5相同或不同，并且各自是氢原子，低级烷基 ，或低级烷氧基; 并且R 4和R 5可以一起形成其中一个或多个亚甲基部分可以任选地被氧和/或硫原子取代的低级亚烷基; X是-NH-或氧或硫原子; Y是-NH-，氧 或硫原子，或亚砜或砜基; Z为单键或-NH6-; R6表示氢原子或低级亚烷基; 和n为0至15的整数;以及它们的盐和溶剂化物。本发明的化合物可用作药物组合物，特别是作为酰基辅酶A胆固醇酰基转移酶（ACAT）抑制剂。