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    Derivatives of thioformamide
    23.
    发明公开
    Derivatives of thioformamide 失效
    Thioformamidderivate。

    公开(公告)号：EP0321274A1

    公开(公告)日：1989-06-21

    申请号：EP88311927.3

    申请日：1988-12-16

    申请人： RHONE POULENC RORER LIMITED

    发明人： Cook, David Charles ,  Hart, Terance William ,  McLay, Iain McFarlane ,  Palfreyman, Malcolm Norman ,  Walsh, Roger John Aitchison

    IPC分类号： C07D213/59 ,  C07D213/61 ,  C07D215/14 ,  C07D217/16 ,  C07D239/26 ,  C07D401/12 ,  C07D213/50 ,  C07D213/53 ,  C07D215/12 ,  A61K31/44 ,  A61K31/47

    CPC分类号： C07D213/53 ,  C07D213/56 ,  C07D213/61 ,  C07D215/12 ,  C07D215/14 ,  C07D217/14 ,  C07D239/26

    摘要： Therapeutically useful thioformamide derivatives of the formula:
    wherein R represents alkyl, Het represents pyrid-3-yl, isoquinolin-4-yl, tetrahydroquinolin-3-yl, quinolin-3-yl, pyridazin-4-yl, pyrimid-5-yl, thiazol-5-yl, thieno[2,3-b]­pyridin-5-yl, pyrazin-2-yl, indol-3-yl and thieno[3,2-b]­pyridin-6-yl, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C=NOR¹, >C=NN(R¹)₂ or >C=NN(R¹)CON(R¹)₂ in which R¹ represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl, or two R¹ substituents on the same nitrogen atom may together form an optionally substituted alkylene radical chain and salts thereof, processes for their preparation and compositions containing them are described.

    摘要翻译： 治疗上有用的下式的硫代甲酰胺衍生物：其中R代表烷基，Het代表吡啶-3-基，异喹啉-4-基，四氢喹啉-3-基，喹啉-3-基，哒嗪-4-基，嘧啶-4-基， 噻吩并[2,3-b]吡啶-5-基，吡嗪-2-基，吲哚-3-基和噻吩并[3,2-b]吡啶-6-基， Y代表乙烯，亚甲基或价键，X代表羰基，羟基亚甲基，C = NOR 1，C = NN（R 1）2或C = NN（R 1）CON 1）其中R 1表示氢或任选取代的烷基，苄基，苯乙基，1-萘基甲基，2-萘基甲基或吡啶-3-基甲基或同一氮原子上的两个R 1取代基可以一起 形成任选取代的亚烷基自由基链及其盐，其制备方法和含有它们的组合物。

    INHALER
    25.
    发明授权
    INHALER 失效
    气雾

    公开(公告)号：EP0533747B1

    公开(公告)日：1998-01-28

    申请号：EP91910833.2

    申请日：1991-06-14

    申请人： RHONE-POULENC RORER LIMITED

    发明人： CALVERT, John, Richard ,  COOK, Robert, Stanley ,  HOBBS, Michael, Anthony ,  LEIGHTON, Ann-Marie ,  SIMPKIN, Gordon, Thomas ,  TRUNLEY, Roy ,  WEST, Anthony, Douglas

    IPC分类号： A61M15/00

    CPC分类号： A61M15/00 ,  A61M11/003 ,  A61M15/0028 ,  A61M15/0033 ,  A61M2202/064 ,  A61M2205/0233 ,  A61M2206/16

    摘要： An inhaler for inhaling pulverulent medicament from within a capsule comprises a chamber (24) within which the capsule is positioned with its longitudinal axis in the median plane of the chamber and thus generally parallel to the front (29) and rear walls (30) of the chamber, where the spacing between said front and rear walls is just greater than the diameter of the capsule and the diameter of the chamber is larger than the capsule's length. The device includes pins (21) serving as opening means to pierce the ends of the capsule while it is seated in a recess (25). Air inlets (26), chamber (24) and mouthpiece (27) are in such a spatial relation as to create a swirling or vortexing movement of the airflow which allows good capsule's emptying and powders to be finely dispersed. Chamber and mouthpiece inner walls can be of antistatic material.

    摘要翻译： 用于从胶囊内吸入粉末状药物的吸入器包括腔室24，在该腔室内胶囊可自由旋转，同时其纵向轴线位于腔室的中间平面中，因此大致平行于腔室的前后壁29和30 由于所述前壁和后壁之间的间隔小于胶囊的轴向长度，而是大于胶囊的直径。 该装置包括用作打开装置的销21，其在其位于凹部25中时刺穿胶囊的端部，于是引脚21的缩回允许胶囊在吸入空气通过期间被夹带在腔室24中的旋转气流中 空气入口26并通过吸口喷嘴27排出。

    Powder inhaler
    26.
    发明公开
    Powder inhaler 失效
    Pulverinhalator

    公开(公告)号：EP0804935A3

    公开(公告)日：1998-01-07

    申请号：EP97110943.4

    申请日：1991-06-14

    申请人： RHONE-POULENC RORER LIMITED

    发明人： Calvert, John Richard ,  Cook, Robert Stanley ,  Hobbs, Michael Anthony ,  Leighton, Ann-Marie ,  Simpkin, Gordon Thomas ,  Trunley, Roy ,  West, Anthony Douglas

    IPC分类号： A61M15/00

    CPC分类号： A61M15/00 ,  A61M11/003 ,  A61M15/0028 ,  A61M15/0033 ,  A61M2202/064 ,  A61M2205/0233 ,  A61M2206/16

    摘要： An inhaler for inhaling pulverulent medicament from within a capsule comprises a chamber 24 within which the capsule is free to rotate while having its longitudinal axis in the median plane of the chamber and thus generally parallel to the front and rear walls 29 and 30 of the chamber, by virtue of the fact that the spacing between said front and rear walls is less than the axial length of the capsule but just greater than the diameter of the capsule. The device includes pins 21 serving as opening means to pierce the ends of the capsule while it is seated in a recess 25, whereupon the retraction of the pins 21 allows the capsule to be entrained into swirling airflow in the chamber 24 during inhalation of air through air inlets 26 and out through a mouthpiece nozzle 27.

    摘要翻译： 用于从胶囊内吸入粉末状药物的吸入器包括腔室24，在该腔室内胶囊可自由旋转，同时其纵向轴线位于腔室的中间平面中，因此大致平行于腔室的前后壁29和30 由于所述前壁和后壁之间的间隔小于胶囊的轴向长度，而是大于胶囊的直径。 该装置包括用作打开装置的销21，其在其位于凹部25中时刺穿胶囊的端部，于是引脚21的缩回允许胶囊在吸入空气通过期间被夹带在腔室24中的旋转气流中 空气入口26并通过吸口喷嘴27排出。

    PROCESS FOR THE PREPARATION OF STEROID DERIVATIVES
    27.
    发明公开
    PROCESS FOR THE PREPARATION OF STEROID DERIVATIVES 失效
    用于生产的甾类衍生物

    公开(公告)号：EP0793670A1

    公开(公告)日：1997-09-10

    申请号：EP95936008.0

    申请日：1995-11-02

    申请人： RHONE-POULENC RORER LIMITED

    发明人： PARKINSON, Nigel, Christofer ,  VAN SICKLE, Andrew, Paul

    IPC分类号： C07J71

    CPC分类号： C07J71/0031

    摘要： A process is described for the preparation of a compound of formula (I) or a stereoisomeric compound thereof, in which the 1,2-position is saturated or is a double bond; X?1 and X2¿ are each independently hydrogen or halogen; R1 is hydrogen or acyl; R2 is hydroxyl, acyloxy or oxo; and R3 is alkyl, by reacting a compound of formula (II) with an aldehyde R3CHO in either phosphoric acid or about 60 % to about 75 % w/w sulphuric acid. Compounds of formula (I) are either pharmacologically active steroids or are intermediates in the synthesis of pharmacologically active steroids.

    NEW STEROIDS
    28.
    发明授权
    NEW STEROIDS 失效
    新类固醇

    公开(公告)号：EP0675897B1

    公开(公告)日：1997-06-18

    申请号：EP94903944.0

    申请日：1993-12-24

    申请人： RHONE-POULENC RORER LIMITED

    发明人： ASHTON, Michael, John Rhone-Poulenc Rorer Ltd. ,  KARLSSON, Sven, Jan-Anders ,  VACHER, Bernard, Yvon, Jack ,  WITHNALL, Michael, Thomas

    IPC分类号： C07J71/00 ,  A61K31/56

    CPC分类号： C07J71/0031 ,  C07J3/005 ,  C07J5/0092

    摘要： Steroids of formula (I) where -^_-^_-^_-^_ is independently at each of the 1,2-, 4,5- and 6,7-positions, a single or double bond; R1 is a straight- or branched-chain C1-4 alkyl or C2-4 alkenyl; R2 is hydrogen or methyl; R3 is C1-7 alkyl, phenyl, substituted phenyl, heteroaryl, substituted heteroaryl or -CH2R where R is halo, hydroxy, C1-5 alkoxy or C1-10 alkanoyloxy; R4 is hydrogen, halo, hydroxy, keto or C1-3 alkoxy when -^_-^_-^_-^_ at the 6,7-position forms a single bond, or hydrogen, halo or C1-3 alkoxy when -^_-^_-^_-^_ at the 6,7-position forms a double bond; R5 is hydrogen or halo; R6 is hydrogen when -^_-^_-^_-^_ at the 1,2-position forms a single bond or hydrogen or chloro when -^_-^_-^_-^_ at the 1,2-position forms a double bond; and n is 0-2; and racemic mixtures and diastereoisomers thereof, processes for their preparation, pharmaceutical compositions containing them, and methods for their use, especially as antiinflammatories.

    ABUSE RESISTANT TABLETS
    29.
    发明公开
    ABUSE RESISTANT TABLETS 失效
    防止滥用保护片剂

    公开(公告)号：EP0742711A1

    公开(公告)日：1996-11-20

    申请号：EP95906418.0

    申请日：1995-01-24

    申请人： RHONE-POULENC RORER LIMITED

    发明人： BASTIN, Richard, James ,  LITHGOW, Bruce, Hamilton

    IPC分类号： A61K9

    CPC分类号： A61K9/2086

    摘要： This invention relates to an abuse resistant tablet containing two or more layers comprising one or more drugs and one or more gelling agents wherein the drug(s) and gelling agent(s) are contained in separate layers of the tablet. The multilayer tablet is particularly suitable for the administration of drugs prone to abuse by unauthorised parenteral administration such as analgesics, hypnotics and anxiolytics.