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    PROCESS FOR PREPARING 1 -HYDROXY-2 -SUBSTITUTED CYCLOHEXYL AZETIDIN-2-ONE COMPOUNDS
    2.
    发明授权
    PROCESS FOR PREPARING 1 -HYDROXY-2 -SUBSTITUTED CYCLOHEXYL AZETIDIN-2-ONE COMPOUNDS 有权
    用于生产1-羟基-2-取代CYCLOHEXYLAZETIDIN-2-ONE COMPOUNDS

    公开(公告)号：EP1940853B1

    公开(公告)日：2009-11-04

    申请号：EP06792145.2

    申请日：2006-09-19

    申请人： LEK Pharmaceuticals d.d.

    发明人： SELIC, Lovro ,  VILFAN, Gregor ,  URLEB, Uros

    IPC分类号： C07F7/18

    CPC分类号： C07F7/1892 ,  Y02P20/55

    摘要： A novel process for the preparation of 1'-hydroxy-2'-substituted cyclohexyl azetidin-2- one compound of formula 2, which is important intermediate in the synthesis of trinems, is described by epoxide ring opening of (3S,4R)-3-[(1R)-1-(tert- butyldimethylsilyloxy)ethyl]-4-[(1'R,2'S,3'R)-1',2'-epoxycyclohexan-3'-yl]azetidin-2-one of formula 1 with the nucleophile compound of formula RYH, where nucleophile may act as solvent itself if the nucleophile is in the liquid form, in a suitable solvent and in the presence of a suitable catalyst from the group of salt of trifluoromethane sulfonic acid, preferably ytterbium (III) trifluoromethanesulfonate, stannous (II) trifluoromethanesulfonate or dysprosium (III) trifluoromethanesulfonate, under a) ultrasonic irradiation or b) under microwave irradiation of the reaction mixture following by isolation and purification of the desired compound. A variant of the novel process describes ring epoxide opening of the starting compound of formula 1 with the compound of formula NH 4 X in a suitable solvent under a) microwave irradiation or b) without microwave irradiation to obtain the desired compound of formula 2. Instead of compound of formula 1 a compound of formula 6 may be used as starting compound where any other suitable hydroxy protecting group known in the art may be used in the formula of the starting compound.

    Use of inhibitor of beta-lactamases and its combination with beta-lactam antibiotics
    3.
    发明公开
    Use of inhibitor of beta-lactamases and its combination with beta-lactam antibiotics 审中-公开
    Verwendung eines Hemmers von Beta-Lactamasen und dessen Kombination mit Beta-Lactam-Antibiotika

    公开(公告)号：EP2085084A1

    公开(公告)日：2009-08-05

    申请号：EP08150776.6

    申请日：2008-01-29

    申请人： LEK Pharmaceuticals d.d.

    发明人： Prezelj, Andrej ,  Urleb, Uros ,  Vilfan, Gregr

    IPC分类号： A61K31/397 ,  A61P31/04 ,  C07D477/00

    CPC分类号： C07D477/00 ,  A61K31/397

    摘要： The present invention relates to A pharmaceutical composition with broad-spectrum of activity against class A, class C and D enzymes comprising an antibiotic and a pharmaceutically effective amount of a compound of formula (I)

    compounds of formula (I), the use of a therapeutically effective amount of one or more compounds of formula (I) as a broad-spectrum beta-lactamase inhibitor and the use of such a pharmaceutical composition for the treatment of an infection in humans or animals caused by bacteria.

    摘要翻译： 本发明涉及一种对A类，C类和D类具有广谱活性的药物组合物，其包含抗生素和药学上有效量的式（I）化合物的式（I）化合物，使用 治疗有效量的一种或多种式（I）化合物作为广谱β-内酰胺酶抑制剂，以及这种药物组合物用于治疗由细菌引起的人或动物感染的用途。

    Synthesis of statins
    4.
    发明公开
    Synthesis of statins 审中-公开
    Statinsynthese

    公开(公告)号：EP2017267A1

    公开(公告)日：2009-01-21

    申请号：EP07112529.8

    申请日：2007-07-16

    申请人： LEK Pharmaceuticals d.d.

    发明人： Kopitar, gregor ,  Mrak, Peter ,  Oslaj, Matej

    IPC分类号： C07D239/42 ,  C07D309/10 ,  C07C217/46

    CPC分类号： C07D239/42 ,  C07D309/10 ,  C12P17/06

    摘要： The process for synthesis of statins is presented where the intermediate intermediate (4 R ,6 S )-6-(dialkoxymethyl)tetrahydro-2 H -pyran-2,4-diol which already possesses the desired stereochemistry corresponding to final statin is prepared by an aldolaze.

    摘要翻译： 提出了合成他汀类药物的方法，其中已经具有对应于最终他汀的所需立体化学的中间体中间体（4R，6S）-6-（二烷氧基甲基）四氢-2H-吡喃-2,4-二醇通过 一个aldolaze

    Novel polymorphic forms of N-piperidino-5-(4-chlorophenyl)-1-(2, 4-dichlorphenyl)-4-methyl-3-pyrazolecarboxamide
    6.
    发明公开
    Novel polymorphic forms of N-piperidino-5-(4-chlorophenyl)-1-(2, 4-dichlorphenyl)-4-methyl-3-pyrazolecarboxamide 审中-公开
    （4-氯苯基）-1-（2,4-二氯苯基）-4-甲基-3-吡唑甲酰胺的多聚甲醛

    公开(公告)号：EP1953144A1

    公开(公告)日：2008-08-06

    申请号：EP07101421.1

    申请日：2007-01-30

    申请人： SANDOZ AG

    发明人： Ludescher, Johannes ,  Griesser, Ulrich J. ,  Langes, Christoph ,  Fucke, Katherina ,  Wieser, Josef

    IPC分类号： C07D231/14 ,  A61K31/415 ,  A61P3/00

    CPC分类号： C07D231/14

    摘要： The present invention relates to novel polymorphic forms of N-piperidino-5-(4-chlorophenyl)-1-(2, 4-dichlorphenyl)-4-methyl-3-pyrazolecarboxamide and to novel methods for their preparation. More particularly the invention relates to the preparation of a monohydrate of N-piperidino-5-(4-chlorophenyl)-1-(2, 4-dichlorphenyl)-4-methyl-3-pyrazolecarboxaniide rimonabant and to a novel anhydrous form of N-piperidino-5-(4-chlorophenyl)-1-(2, 4-dichlorphenyl)-4-methyl-3-pyrazolecarboxamide, and to pharmaceutical compositions thereof.

    摘要翻译： 本发明涉及N-哌啶子基-5-（4-氯苯基）-1-（2,4-二氯苯基）-4-甲基-3-吡唑甲酰胺的新型多晶型物及其制备方法。 更具体地，本发明涉及制备N-哌啶子基-5-（4-氯苯基）-1-（2,4-二氯苯基）-4-甲基-3-吡唑并咪唑利纳邦的一水合物，并且制备新的无水形式的N - 哌啶-5-基（4-氯苯基）-1-（2,4-二氯苯基）-4-甲基-3-吡唑酰胺，及其药物组合物。

    Process for the preparation of recombinant polypeptides
    9.
    发明公开
    Process for the preparation of recombinant polypeptides 有权
    生产重组多肽的方法

    公开(公告)号：EP2302068A1

    公开(公告)日：2011-03-30

    申请号：EP10009128.9

    申请日：2004-08-19

    申请人： Sandoz AG

    发明人： Stempfer, Günter ,  Palma, Norbert

    IPC分类号： C12P21/02

    CPC分类号： C12P21/02

    摘要： The present invention relates to the preparation of a recombinant polypeptide, which polypeptide upon expression has been secreted into the periplasm of a transformed host cell. In particular, this invention relates to a process to enhance the extraction yield of said recombinant polypeptide from the periplasm before further downstream processing.

    Active pharmaceutical ingredient on solid support, amorphous and with improved solubility
    10.
    发明公开
    Active pharmaceutical ingredient on solid support, amorphous and with improved solubility 审中-公开
    在固体载体上的活性药物成分，具有改善的溶解性和无定形

    公开(公告)号：EP2072042A1

    公开(公告)日：2009-06-24

    申请号：EP07150359.3

    申请日：2007-12-21

    申请人： Lek Pharmaceuticals D.D.

    发明人： Grahek, Rok ,  Resman, Aleksander ,  Batarda, Andrej ,  Crnugelj, Martin

    IPC分类号： A61K9/18 ,  A61K31/122 ,  A61K31/397

    CPC分类号： A61K31/122 ,  A61K9/143 ,  A61K31/397

    摘要： The present invention discloses a combination preparation comprising an active pharmaceutical ingredient (API) and a pharmaceutically acceptable solid support,
    wherein said solid support is in a water-insoluble particulate form and comprises a material selected from silicic acid, aluminum hydroxide and titanium hydroxide, wherein said API is a compound having both, at least one hydrophobic structural moiety causing the API to have low solubility in water or in an aqueous solution, and multiple hydrophilic groups arranged to form multiple intermolecular interactions to said solid support involving polar or ionic or hydrogen bonding, wherein the hydrophilic groups of the API are independently equal or different and comprise at least one of the group consisting of OH- and halogen-groups;
    wherein said API is bound to said solid support by adsorption, and wherein a major proportion of said API is in the amorphous state.
    The present invention also discloses a pharmaceutical preparation comprising such a combination preparation as well as a method for producing such a combination preparation.

    摘要翻译： 本发明光盘松散的组合制剂，其包含活性药物成分（API）和药学可接受的固体载体的，worin所述固体支持物是在水不溶性颗粒形式，并且包括选自硅酸，氢氧化铝和氢氧化钛，worin中选择的材料 所述API是具有两者的化合物，至少一个疏水结构部分使API在水中具有或在wässrige溶液的溶解度低，并且布置以形成多个分子间相互作用于所述固体支持涉及极性或离子键或氢键的多个亲水性基团 ，worin API的亲水基团是unabhängig相等或不同的，包括选自由OH-和卤素 - 基团中的至少一者; worin所述API通过吸附作用结合于所述固体载体，以及worin说API的主要部分处于非晶状态。 因此，本发明盘松动的药物制剂，其包含寻求的组合制剂以及用于制造寻求组合制剂的方法。