3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives as 5HT.sub.1A ligands
    1.
    发明授权
    3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives as 5HT.sub.1A ligands 失效
    3,5-二氧代 - (2H,4H)-1,2,4-三嗪衍生物作为5HT1A配体

    公开(公告)号:US5591743A

    公开(公告)日:1997-01-07

    申请号:US578522

    申请日:1996-03-26

    CPC分类号: C07D253/075 C07D405/12

    摘要: A 3,5-dioxo-(2H,4H)-1,2,4-triazine compounds of formula I ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, represent hydrogen or C.sub.1 -C.sub.6 alkyl, n is 2 to 6, inclusive,A represents aryl piperazino II ##STR2## the Ar grouping representing phenyl, naphthyl, pyrimidyl, or pyridyl, unsubstituted or substituted by C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, hydroxy, trifluoromethyl, or halogen, or III benzodioxanyl-methyl-amino or pyridodioxanyl-methyl-amino ##STR3## in which R represents hydrogen or C.sub.1 -C.sub.3 alkyl and X represents a nitrogen or carbon atom, therapeutically-acceptable salts and enantiomers thereof, pharmaceutical compositions thereof, and method for treatment of diseases requiring a 5HT.sub.1A receptor agonist therewith.

    摘要翻译: PCT No.PCT / FR94 / 00772 Sec。 371日期:1996年3月26日 102(e)1996年3月26日PCT 1994年6月27日PCT公布。 第WO95 / 01965号公报 日期:1995年1月19日A式Ⅰ的3,5-二氧代 - (2H,4H)-1,2,4-三嗪化合物其中:R1和R2相同或不同,表示氢或C1 C 1-6烷基,n为2至6,包括端值,A表示芳基哌嗪基II代表苯基,萘基,嘧啶基或吡啶基的Ar基团,未取代或被C 1 -C 3烷基,C 1 -C 3烷氧基,羟基, 三氟甲基或卤素,或III苯并二恶烷基 - 甲基 - 氨基或吡啶并二恶烷基 - 甲基 - 氨基,其中R表示氢或C1-C3烷基,X表示氮或碳原子,其治疗上可接受的盐和对映体,药物 其组合物,以及治疗需要5HT1A受体激动剂的疾病的方法。

    Freeze-drying of solid, liquid or paste-like products
    3.
    发明授权
    Freeze-drying of solid, liquid or paste-like products 失效
    固体,液体或糊状产品的冷冻干燥

    公开(公告)号:US4035924A

    公开(公告)日:1977-07-19

    申请号:US608054

    申请日:1975-08-27

    IPC分类号: B65B31/02 F26B5/06 F26B13/30

    CPC分类号: F26B5/06 B65B31/024

    摘要: In the lyophilization of solid, liquid or pasty products the product to be lyophilized is placed in an open secondary container of flexible material which is capable of being subsequently closed and lyophilized in a lyophilization apparatus with the container kept open. On completion of lyophilization the container is closed and the closed container withdrawn from the apparatus. Preferably the container is in the form of a bag, e.g. a heat-sealable plastic bag. A lyophilization apparatus is provided with means for supporting secondary containers accommodating product to be lyophilized, means for keeping the secondary containers open during lyophilization and means for closing the containers on completion of lyophilization.

    摘要翻译: 在固体,液体或糊状产品的冻干中,将要冻干的产品置于柔性材料的开放的二次容器中,其能够随后在容器保持打开的冻干装置中封闭并冻干。 冻结完成后,将容器关闭,从设备中取出密闭的容器。 优选地,容器是袋的形式,例如 一个可热封的塑料袋。 冷冻干燥装置设置有用于支撑容纳要冷冻干燥的产品的二次容器的装置,用于在冻干期间保持次级容器打开的装置以及在冻干完成时关闭容器的装置。

    Derivatives of 1,2-dihydro 2-oxo quinoxalines, their preparation and
their use in therapy
    5.
    发明授权
    Derivatives of 1,2-dihydro 2-oxo quinoxalines, their preparation and their use in therapy 失效
    1,2-二羟基喹喔啉衍生物的制备及其在治疗中的应用

    公开(公告)号:US5198441A

    公开(公告)日:1993-03-30

    申请号:US688536

    申请日:1991-06-17

    CPC分类号: C07D401/06 C07D241/44

    摘要: New derivatives of 1,2-dihydro 2-oxo quinoxalines corresponding to the general formula I: ##STR1## in which: R is a hydrogen or halogen atomR.sub.1 is a hydrogen atom or a straight or branched C.sub.1 -C.sub.4 alkyl radicalR.sub.2 is:a hydrogen atoma C(O)R.sub.4 radical in which R.sub.4 is a straight or branched C.sub.1 -C.sub.4 alkyl groupa C(O)NHR.sub.5 radical in which R.sub.5 is a straight or branched C.sub.1 -C.sub.4 alkyl radical or a phenyl groupA is a C.sub.1 -C.sub.4 alkaline chainR.sub.3 represents:a hydrogen atom, a C.sub.1 -C.sub.4 alkyl radical, a C.sub.3 -C.sub.6 cycloalkyl radical, an alcynyl, nitrile, hydroxyl, carboxamido, pyridyl, phenyl group, or a phenyl group substituted by a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group or a nitro groupan alkenyl radical of the formula: ##STR2## in which R.sub.6, R.sub.7 may, independently of each other, be a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a phenyl group or an alkoxycarbonyl groupa radical of the formula:--OC(O)R.sub.8 in which R.sub.8 represents a C.sub.1 -C.sub.4 alkyl radicala radical of the formula:--OC(O)NHR.sub.9 in which R.sub.9 represents a straight or branched C.sub.1 -C.sub.4 alkyl group, or a phenyl groupmay assume values from 2 to 4.as well as the therapeutically acceptable organic or inorganic salts of these molecules. The compounds are useful in the treatment of respiratory disorders.

    摘要翻译: PCT No.PCT / FR90 / 00752 Sec。 371日期1991年6月17日 102(e)日期1991年6月17日PCT提交1990年10月17日PCT公布。 第WO91 / 05772号公报 日期:1991年5月2日。对应于通式I的1,2-二氢-2-氧代喹喔啉的新衍生物:其中:R为氢或卤素原子,R 1为氢原子或直链或支链C1 -C4烷基R2是:氢原子,C(O)R4基,其中R4是直链或支链C1-C4烷基,C(O)NHR5基,其中R5是直链或支链C1-C4烷基 或苯基A是C1-C4碱基链R3表示:氢原子,C1-C4烷基,C3-C6环烷基,烷酰基,腈,羟基,甲酰氨基,吡啶基,苯基或苯基 被卤素原子取代的基团,C 1 -C 4烷基,C 1 -C 4烷氧基或硝基,下式的链烯基:其中R 6,R 7可以彼此独立地为氢原子 ,C 1 -C 4烷基,苯基或烷氧基羰基,式-OC(O)R 8基团,其中R 8表示C 1 -C 4烷基,式:-OC(O)NHR 9基团在 其中R 9表示直链或支链C 1 -C 4烷基,或苯基可以为2至4的值,以及这些分子的治疗上可接受的有机或无机盐。 该化合物可用于治疗呼吸系统疾病。