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    • 51. 发明申请
    • Urea compounds as inhibitors for vla-4
    • 尿素化合物作为vla-4的抑制剂
    • US20030087956A1
    • 2003-05-08
    • US10149932
    • 2002-06-14
    • Craig JohnstoneMichael Stewart Large
    • A61K031/36A61K031/277A61K031/195A61K031/24A61K031/165
    • C07D295/088C07C275/42C07C317/18C07C323/12C07C2601/08C07D211/22C07D211/54
    • 1 A compound of formula (I) where D is a VLA-4 specificity determinant which does not impart significant IIB/IIIa activity; R41 is a group of the formula (V): U - (CH2)d - V - T wherein U is selected from oxygen, sulphur, a direct bond or nullCH2Onull, V is selected from nitrogen, oxygen, sulphur, S(O), S(O)2 or a direct bond, d is zero or a number from 1 to 4, and T is selected from a range of variables defined in the application; and other variables are defined in the application, or a pharmaceutically acceptable salt or in vivo hydrolysable derivative thereof. The compounds are useful in the treatment of disease mediated by the interaction between VCAM-1 and/or fibronectin and the integrin receptor null4null1. Pharmaceutical compositions and methods of use or treatment are also described and claimed.
    • 式(I)的化合物,其中D是不赋予显着IIB / IIIa活性的VLA-4特异性决定簇; R41是式(Ⅴ)的基团:U-(CH2)d-V-T其中U选自氧,硫,直接键或-CH 2 O-,V选自氮,氧,硫,S( O),S(O)2或直接键合,d为0或1至4的数,T选自本申请中定义的变量范围; 和其它变量在本申请中定义,或其药学上可接受的盐或体内可水解的衍生物。 该化合物可用于治疗由VCAM-1和/或纤连蛋白与整联蛋白受体α4β1相互作用介导的疾病。 也描述和要求保护药物组合物和使用或治疗方法
    • 53. 发明申请
    • Delivery of anti-migraine compounds through an inhalation route
    • 通过吸入途径输送抗偏头痛化合物
    • US20030021754A1
    • 2003-01-30
    • US10152640
    • 2002-05-20
    • Joshua D. RabinowitzAlejandro C. Zaffaroni
    • A61K009/14A61K031/554A61K031/553A61K031/24
    • A61K9/007A61K9/0073A61K9/12A61K31/00A61K31/137A61K31/138A61K31/165A61K31/19A61K31/192A61K31/195A61K31/216A61K31/27A61K31/404A61K31/405A61K31/407A61K31/4196A61K31/421A61K31/422A61K31/423A61K31/437A61K31/473A61K31/485A61K31/49A61K31/495A61K31/496A61K31/4985A61K31/501A61K31/519A61K31/53A61K31/551A61K31/5517A61K47/54A61M11/042A61M15/06A61M2205/8206F24V30/00Y10S514/923Y10S514/958
    • The present invention relates to the delivery of anti-migraine compounds through an inhalation route. Specifically, it relates to aerosols containing lidocaine, verapamil, diltiazem, isometheptene, or lisuride that are used in inhalation therapy. In a composition aspect of the present invention, the aerosol comprises particles comprising at least 5 percent by weight of lidocaine, verapamil, diltiazem, isometheptene, or lisuride. In a method aspect of the present invention, one of lidocaine, verapamil, diltiazem, isometheptene, or lisuride is delivered to a mammal through an inhalation route. The method comprises: a) heating a composition, wherein the composition comprises at least 5 percent by weight of lidocaine, verapamil, diltiazem, isometheptene, or lisuride, to form a vapor; and, b) allowing the vapor to cool, thereby forming a condensation aerosol comprising particles, which is inhaled by the mammal. In a kit aspect of the present invention, a kit for delivering lidocaine, verapamil, diltiazem, isometheptene, or lisuride through an inhalation route to a mammal is provided which comprises: a) a composition comprising at least 5 percent by weight of lidocaine, verapamil, diltiazem, isometheptene, or lisuride; and, b) a device that forms a lidocaine, verapamil, diltiazem, isometheptene, or lisuride containing aerosol from the composition, for inhalation by the mammal.
    • 本发明涉及通过吸入途径递送抗偏头痛化合物。 具体地说,它涉及在吸入治疗中使用的含有利多卡因,维拉帕米,地尔硫卓,异月精或伊瑞沙德的气溶胶。 在本发明的组合物方面,所述气雾剂包含包含至少5重量%的利多卡因,维拉帕米,地尔硫卓,异月桂烯或碘化尿素的颗粒。 在本发明的方法方面,通过吸入途径将利多卡因,维拉帕米,地尔硫卓,异月精或伊瑞沙肽中的一种递送至哺乳动物。 所述方法包括:a)加热组合物,其中所述组合物包含至少5重量%的利多卡因,维拉帕米,地尔硫卓,异月桂烯或碘化尿,以形成蒸气; 和b)允许蒸气冷却,由此形成包含由哺乳动物吸入的颗粒的冷凝气雾剂。 在本发明的试剂盒方面,提供了一种用于通过吸入途径将哺乳动物输送利多卡因,维拉帕米,地尔硫卓,异月桂烯或伊瑞沙丁的试剂盒,其包括:a)包含至少5重量%的利多卡因,维拉帕米 ,地尔硫卓,异月桂烯或碘化;; 和b)一种从哺乳动物吸入形成利多卡因,维拉帕米,地尔硫卓,异月桂烯或含有来自该组合物的气溶胶的装置。