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    • 1. 发明申请
    • NASAL SPRAY DEVICE
    • NASAL喷雾装置
    • WO2012048867A1
    • 2012-04-19
    • PCT/EP2011/005118
    • 2011-10-12
    • IVAX PHARMACEUTICALS IRELANDTEVA BRANDED PHARMACEUTICAL PRODUCTS R&D, INC.WALSH, DeclanZENG, XIan-MingLY, JadeMORALES, ArmandoIVAX RESEARCH, LLC
    • WALSH, DeclanZENG, XIan-MingLY, JadeMORALES, Armando
    • A61M15/00A61M15/08B05B1/00
    • A61M15/009A61K9/0043A61K31/57A61M15/08B65D83/54
    • This invention relates to a nasal spray device (1) for the delivery of a pharmaceutical formulation to the nasal cavity in metered doses. The device comprises: a pressurised aerosol canister (3) including a vial (4) containing a pharmaceutical formulation comprising an active ingredient, a propellant and, optionally, a co- solvent, the aerosol canister further including a metering valve (6) having a valve stem (8); and an actuator (2) for the aerosol canister, the actuator including a stem block (11) having a receptacle into which the valve stem of metering valve of the aerosol canister is received and axially located and being displaceable relative to the vial of the aerosol canister to actuate the metering valve of the aerosol canister, a sump (15) extending below the receptacle, the stem block further defining a discharge orifice (19) for the pharmaceutical formulation and a transfer channel (13) through which a dispensed dose of the pharmaceutical formulation is able to pass from the sump to the discharge orifice. The actuator further comprises a delivery outlet (12) for the aerosol plume, the discharge orifice being arranged to direct the aerosol plume through the delivery outlet, and wherein the device is adapted to produce an aerosol plume for a dispensed dose having a spray force value no greater than 40 mN measured at a distance of 30 mm from the discharge orifice. Use of the term formulation encompasses both solution and suspension formulations.
    • 本发明涉及一种用于以计量剂量将药物制剂递送至鼻腔的鼻喷雾装置(1)。 该装置包括:加压气溶胶罐(3),其包括含有包含活性成分,推进剂和任选的助溶剂的药物制剂的小瓶(4),所述气溶胶罐还包括计量阀(6),其具有 阀杆(8); 和用于气溶胶罐的致动器(2),所述致动器包括具有容器的杆块(11),所述气溶胶罐的计量阀的阀杆被容纳在所述容器中并且被轴向定位并且相对于所述气溶胶小瓶可移位 致动所述气溶胶罐的计量阀,在所述容器下方延伸的贮槽(15),所述阀杆块还限定用于所述药物制剂的排出孔(19)和输送通道(13),所述分配剂量 药物制剂能够从贮槽通过排放口。 所述致动器还包括用于所述气溶胶羽流的输送出口(12),所述排放孔布置成引导所述气溶胶羽流通过所述输送出口,并且其中所述装置适于产生具有喷雾力值的分配剂量的气溶胶羽流 在距离排放口30mm的距离处测量不大于40mN。 术语制剂的使用包括溶液和悬浮液制剂。
    • 2. 发明申请
    • PROCESSES FOR PREPARATION OF TAXANES AND INTERMEDIATES THEREOF
    • 制备TAXANES及其中间体的方法
    • WO2009137084A2
    • 2009-11-12
    • PCT/US2009/002851
    • 2009-05-06
    • IVAX RESEARCH, LLCTEVA PHARMACEUTICALS USA, INC.CVAK, LadislavVALIK, MartinHOLAS, TomasMALECEK, Jiri
    • CVAK, LadislavVALIK, MartinHOLAS, TomasMALECEK, Jiri
    • C07D305/14
    • C07D305/14Y02P20/55
    • A paclitaxel intermediate of formula 1 : wherein R 1 is acetyl, R 2 is tert-butyloxycarbonyl (BOC), R 3 and R 4 are phenyl and R 5 is 1- ethoxyethyl, is provided. Also provided are processes for preparing taxane intermediates of formula 1 comprising reacting a compound of formula 2 with a compound of formula 3 wherein, R 1 , R 2 and R 5 are independently a hydroxyl protecting group; R 3 is phenyl, substituted phenyl, a straight or branched alkyl containing 1 to 12 carbon atoms, alkenyl containing 2 to 12 carbon atoms, cycloalkyl containing 4 to 15 carbon atoms, cycloalkenyl or an R 6 -O- group in which R 6 is: phenyl, substituted phenyl group, a C 1 -C 8 straight or branched alkyl, a C 2 -C 8 straight or branched alkenyl group, a C 3 -C 8 straight or branched alkynyl, a C 3 -C 7 cycloalkyl, C 4 -C 7 cycloalkenyl, a C 7 -C 11 bicycloalkyl substituent, or a saturated or unsaturated nitrogen; and R 4 is phenyl or a substituted phenyl group.
    • 式1的紫杉醇中间体:其中R1是乙酰基,R2是叔丁氧基羰基(BOC),R3和R4是苯基,R5是1-乙氧基乙基。 还提供了制备式1的紫杉烷中间体的方法,包括使式2的化合物与式3的化合物反应,其中R 1,R 2和R 5独立地是羟基保护基; R3是苯基,取代苯基,含有1至12个碳原子的直链或支链烷基,含有2至12个碳原子的烯
      基,含有4至15个碳原子的环烷基,环烯基或R6-O-基,其中R6是:苯基, 取代的苯基,C1-C8直链或支链烷基,C2-C8直链或支链烯基,C3-C8直链或支链炔基,C3-C7环烷基,C4-C7环烯基,C7-C11双环烷基取代基, 或饱和或不饱和氮; 并且R 4是苯基或取代的苯基。