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    IMPROVED METHOD FOR PREPARING CRYSTALLINE SODIUM RISEDRONATE
    1.
    发明申请
    IMPROVED METHOD FOR PREPARING CRYSTALLINE SODIUM RISEDRONATE 审中-公开
    制备晶体钠阳离子的改进方法

    公开(公告)号：WO2007042048A2

    公开(公告)日：2007-04-19

    申请号：PCT/DK2006050054

    申请日：2006-10-05

    申请人： SANDOZ AS ,  PREIKSCHAT HERBERT FRITZ ,  FISCHER ERIK ,  BECK FREDERICK ,  BENNEKOU JACOB

    发明人： PREIKSCHAT HERBERT FRITZ ,  FISCHER ERIK ,  BECK FREDERICK ,  BENNEKOU JACOB

    IPC分类号： C07F9/58 ,  A61K31/675

    CPC分类号： C07F9/582

    摘要： A new procedure for preparing crystalline sodium risedronate is disclosed, which procedure takes place under conditions where the availability of water is strictly limited. New sodium risedronate forms prepared according to the new procedure are also disclosed. The new sodium risedronate forms are useful for the preparation of pharmaceutical compositions for the treatment of diseases of bone and calcium metabolism.

    摘要翻译： 公开了制备结晶的利塞膦酸钠的新方法，该方法在严格限制水的可用性的条件下进行。 还公开了根据新方法制备的新的利塞膦酸钠形式。 新的利塞膦酸钠形式可用于制备用于治疗骨和钙代谢疾病的药物组合物。

    NEW RISEDRONATE SALTS
    4.
    发明申请
    NEW RISEDRONATE SALTS 审中-公开
    新升级销售

    公开(公告)号：WO2005066190A1

    公开(公告)日：2005-07-21

    申请号：PCT/DK2004/000923

    申请日：2004-12-29

    申请人： HEXAL A/S ,  PREIKSCHAT, Herbert, Fritz ,  FISCHER, Erik ,  TRANEKJER, Michael ,  NIELSEN, Lotte, Basse

    发明人： PREIKSCHAT, Herbert, Fritz ,  FISCHER, Erik ,  TRANEKJER, Michael ,  NIELSEN, Lotte, Basse

    IPC分类号： C07F9/58

    CPC分类号： C07F9/584 ,  A61K31/4406 ,  C07C215/08 ,  C07D295/027 ,  C07D295/088 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/414

    摘要： New risedronate salts selected among disodium risedronate, monopotassium risedronate, dipotassium risedronate, monoammonium risedronate, diammonium risedronate, hemipiperazine risedronate, ethanolamine risedronate and morpholinoethanolamine risedronate and hydrates thereof are disclosed. The new salts have a very low tendency to incorporate additional water into their crystals, which make these salts stable during storage in ambient air. Further pharmaceutical compositions comprising the new risedronate salts and hydrates thereof are disclosed.

    摘要翻译： 新的利塞膦酸盐选自利塞膦酸二钠，利塞膦酸单钾，利塞膦酸二钾，利塞膦酸二铵，利塞膦酸二铵，利塞膦酸二哌嗪，利塞膦酸二乙醇胺和利塞膦酸吗啉代乙醇胺及其水合物。 新的盐具有将额外的水掺入其晶体的非常低的趋势，这使得这些盐在环境空气中储存期间稳定。 公开了包含新的利塞膦酸盐及其水合物的其它药物组合物。

    SUBSTITUTED 3-PHENYL-1,2,3,4-OXATRIAZOLE-5-IMINES USEFUL FOR THE TREATMENT OF ASTHMA AND THROMBOSIS
    5.
    发明申请
    SUBSTITUTED 3-PHENYL-1,2,3,4-OXATRIAZOLE-5-IMINES USEFUL FOR THE TREATMENT OF ASTHMA AND THROMBOSIS 审中-公开
    用于治疗哮喘和血栓形成的替代的3-苯基-1,2,3,4-氧杂噻唑-5-胺

    公开(公告)号：WO1996011191A1

    公开(公告)日：1996-04-18

    申请号：PCT/DK1994000375

    申请日：1994-10-07

    申请人： A/S GEA FARMACEUTISK FABRIK ,  KARUP, Gunnar, Leo ,  PREIKSCHAT, Herbert, Fritz ,  PEDERSEN, Soren Bols ,  CORELL, Tim, Niss ,  WILHELMSEN, Ellen, Sloth

    发明人： A/S GEA FARMACEUTISK FABRIK

    IPC分类号： C07D273/00

    CPC分类号： C07D273/00

    摘要： 3- and 5-substituted 1,2,3,4-oxatriazole-5-imine compounds of general formula (I), wherein R is the same or different groups and represents alkyl or alkoxy groups having 1 to 3 carbon atoms, halogen, trifluoromethyl, nitro, cyano, phenyl or alkylsulphonyl groups; n is 1 to 3; X is -C(O)NH-; -SO2-; -C(O)- or a direct bond; Y means -S-Z; -SO-Z; -S (Z)2, A ; N (Z)3, A ; -C(Z) = CZ2; -C C-Z or a group (a), wherein b = c = N or C-Z; d = N-Z, O or S, and A is any pharmaceutically acceptable anion; and Z is the same or different groups and represents H, cyano, nitro, trifluoromethyl, -CH = CH2, -C CH, straight or branched C1-C6-alkyl, C3-C7-cycloalkyl, phenyl or optionally substituted phenyl; may be used for the preparation of a medicament for the treatment of asthma, a medicament for the treatment of blood clots (thrombosis), a medicament being effective against impotence and a medicament being effective against pre-eclampsia.

    摘要翻译： 具有通式（I）的3-和5-取代的1,2,3,4-氧杂三唑-5-亚胺化合物，其中R 1是相同或不同的基团，并且代表具有1至3个碳原子的烷基或烷氧基 卤素，三氟甲基，硝基，氰基，苯基或烷基磺酰基; n为1〜3; X是-C（O）NH-; -SO2-; -C（O） - 或直接键; Y表示-S-Z; -SO-Z; -S +（Z）2，A < N +（Z）3，A < -C（Z）= CZ2; -C C-Z或基团（a），其中b = c = N或C-Z; d = N-Z，O或S，A - 为任何药学上可接受的阴离子; Z是相同或不同的基团，代表H，氰基，硝基，三氟甲基，-CH = CH 2，-CCH，直链或支链C 1 -C 6烷基，C 3 -C 7 - 环烷基，苯基或任选取代的苯基; 可用于制备用于治疗哮喘的药物，用于治疗血块（血栓形成）的药物，有效抵抗阳a的药物和有效抵抗先兆子痫的药物。

    3- AND 5-SUBSTITUTED 1,2,3,4-OXATRIAZOLE-5-IMINE COMPOUNDS, A PROCESS FOR THE PREPARATION THEREOF, A PHARMACEUTICAL PREPARATION CONTAINING SAID COMPOUNDS AND THE USE OF SAID COMPOUNDS FOR THE PREPARATION OF MEDICAMENTS
    6.
    发明申请
    3- AND 5-SUBSTITUTED 1,2,3,4-OXATRIAZOLE-5-IMINE COMPOUNDS, A PROCESS FOR THE PREPARATION THEREOF, A PHARMACEUTICAL PREPARATION CONTAINING SAID COMPOUNDS AND THE USE OF SAID COMPOUNDS FOR THE PREPARATION OF MEDICAMENTS 审中-公开
    3-和5-取代的1,2,3,4-氧杂噻唑-5-酮化合物，其制备方法，含有化合物的药物制剂和用于制备药物的合成化合物的用途

    公开(公告)号：WO1994003442A1

    公开(公告)日：1994-02-17

    申请号：PCT/DK1993000234

    申请日：1993-07-08

    申请人： A/S GEA FARMACEUTISK FABRIK ,  KARUP, Gunnar, Leo ,  PREIKSCHAT, Herbert, Fritz ,  PEDERSEN, Soren, Bols ,  CORELL, Tim, Niss ,  ALHEDE, Borge, Ingvar, Frisch

    发明人： A/S GEA FARMACEUTISK FABRIK

    IPC分类号： C07D273/00

    CPC分类号： C07D273/00 ,  C07D413/12

    摘要： 3- and 5-substituted 1,2,3,4-oxatriazole-5-imine compounds of general formula (I) wherein R is the same or different groups and represents alkyl or alkoxy groups having 1 to 3 carbon atoms, halogen, trifluoromethyl, nitro, cyano, phenyl or alkylsulphonyl groups, n is 1 to 3, X is -SO2 or -C(O)NH-, Y is -(CHR )m-, wherein m = 1 to 4, and R means -CH2-aryl, alkyl, hydrogen or a direct bond, and Q means 10-camphoryl, --C(O)O-alkyl, aryl, -SO2-alkyl or -SO2-aryl, are prepared by ring closing a 1-arylthiosemicarbazide derivative of general formula (II) wherein R and n have the same meaning as in formula (I), by treatment with alkyl nitrite having 1 to 6 carbon atoms or alkali metal nitrite under acidic conditions at 0 to 10 DEG C, whereafter the resulting salts is converted into the corresponding free compound, which is subsequently reacted with a compound of the type C1SO2-Y-Q or O=C=N-Y-Q, wherein Y and Q have the same meaning as in formula (I).

    摘要翻译： 具有通式（I）的3-和5-取代的1,2,3,4-氧杂三唑-5-亚胺化合物，其中R 1是相同或不同的基团，并且表示具有1至3个碳原子的烷基或烷氧基， 卤素，三氟甲基，硝基，氰基，苯基或烷基磺酰基，n为1至3，X为-SO 2或-C（O）NH-，Y为 - （CHR 2）m - ，其中m = ，R 2表示-CH 2 - 芳基，烷基，氢或直接键，Q表示10-樟脑基，-C（O）O-烷基，芳基，-SO 2 - 烷基或-SO 2 - 芳基 通过在酸性下通过用具有1至6个碳原子的亚硝酸烷基酯或碱金属亚硝酸盐处理而闭合其中R 1和n具有与式（I）中相同含义的通式（II）的1-芳基硫代氨基脲衍生物 条件为0至10℃，然后将所得盐转化为相应的游离化合物，随后与C1SO2-YQ或O = C = NYQ的化合物反应，其中Y和Q的定义与 式（I）。

    REAGENT AND USE THEREOF FOR THE PRODUCTION OF BISPHOSPHONATES
    7.
    发明申请
    REAGENT AND USE THEREOF FOR THE PRODUCTION OF BISPHOSPHONATES 审中-公开
    用于生产二磷酸酯的试剂和用途

    公开(公告)号：WO2008058722A1

    公开(公告)日：2008-05-22

    申请号：PCT/EP2007/009841

    申请日：2007-11-14

    申请人： SANDOZ A/S ,  LERSTRUP, Knud ,  PREIKSCHAT, Herbert, Fritz ,  FISCHER, Erik

    发明人： LERSTRUP, Knud ,  PREIKSCHAT, Herbert, Fritz ,  FISCHER, Erik

    IPC分类号： C07F9/38 ,  C07F9/58 ,  C07F9/6506 ,  C08K5/52

    CPC分类号： C07F9/3873 ,  C07F9/582 ,  C07F9/65061 ,  C08K5/5205

    摘要： A new liquid reagent is disclosed in form of an ionic liquid containing phosphorous acid and a tertiary amine. The reagent can be used as a replacement of phosphorous acid, where the new reagent as a liquid reagent can be handled using usual equipment for handling liquids and the dosing of the reagent can therefore be controlled more precisely in industrial plants compared to phosphorous acid, which is a solid at ambient temperature. The new liquid reagent is particular suitable for the synthesis of bisphosphonates.

    摘要翻译： 以含有亚磷酸和叔胺的离子液体的形式公开了新的液体试剂。 该试剂可用作亚磷酸的替代物，其中作为液体试剂的新试剂可以使用通常的处理液体的设备进行处理，因此与亚磷酸相比，可以在工业装置中更准确地控制试剂的投加量， 在环境温度下是固体。 新的液体试剂特别适用于双膦酸盐的合成。