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    Processes for preparing clarithromycin and clarithromycin intermediate, essentially oxime-free clarithromycin, and pharmaceutical composition comprising the same
    1.
    发明授权
    Processes for preparing clarithromycin and clarithromycin intermediate, essentially oxime-free clarithromycin, and pharmaceutical composition comprising the same 失效
    用于制备克拉霉素和克拉霉素中间体，基本上不含肟的克拉霉素的方法和包含其的药物组合物

    公开(公告)号：US06617436B2

    公开(公告)日：2003-09-09

    申请号：US09736447

    申请日：2000-12-15

    申请人： Iiya Avrutov ,  Igor Lifshitz ,  Elizabeth Lewiner

    发明人： Iiya Avrutov ,  Igor Lifshitz ,  Elizabeth Lewiner

    IPC分类号： C07H100

    CPC分类号： C07H17/08 ,  C07F7/1892

    摘要： The present invention relates to processes for preparing protected silylated clarithromycin oxime, preferably 6-O-methyl-2′, 4″-bis(trimethylsilyl)-erythromycin A 9-O-(2-methoxyprop-2-yl)oxime (“S-MOP oxime”), and for converting protected silylated clarithromycin oxime, preferably S-MOP oxime, to clarithromycin. Processes for preparing protected silylated clarithromycin oxime according to the present invention, include reacting a silyl oxime derivative with methylating agent in the presence of at least one solvent and a base, where the solvent comprises methyl tertbutyl ether. Processes for converting protected silylated clarithromycin oxime to clarithromycin according to the present invention, include reacting protected silylated clarithromycin oxime with ethanol and water at an ethanol to water ratio of about 1:1, in the presence of an acid and a deoximating agent and cooling the reaction mixture prior to adding sodium hydroxide, where the process takes place without any additional water addition. Further processes for converting protected silylated clarithromycin oxime to clarithromycin, include heating a mixture of protected silylated clarithromycin oxime, acid, and deoximating agent in an ethanol/water solvent to reflux for more than 4 hours, with a two-fold addition of deoximating agent to produce essentially oxime-free clarithromycin.

    摘要翻译： 本发明涉及制备受保护的甲硅烷基化克拉霉素肟，优选6-O-甲基-2'，4“ - 双（三甲基甲硅烷基） - 红霉素A 9-O-（2-甲氧基丙-2-基）肟（” S-MOP肟“），并将保护的甲硅烷基化克拉霉素肟（优选S-MOP肟）转化为克拉霉素。 根据本发明的制备受保护的甲硅烷基化克拉霉素肟的方法包括使甲硅烷基肟衍生物与甲基化剂在至少一种溶剂和碱的存在下反应，其中溶剂包括甲基叔丁基醚。 将受保护的甲硅烷基化克拉霉素肟转化为克拉霉素的方法包括在酸和脱肟剂的存在下，将保护的甲硅烷基化克拉霉素肟与乙醇和水以约1:1的乙醇与水反应并冷却 在加入氢氧化钠之前的反应混合物，其中该方法进行而没有任何额外的水添加。 将受保护的甲硅烷基化克拉霉素肟转化为克拉霉素的其它方法包括在乙醇/水溶剂中将受保护的甲硅烷基化克拉霉素肟，酸和脱肟剂的混合物加热回流4小时以上，加入二肟剂至 产生基本上无肟的克拉霉素。

    Processes for preparing clarithromycin and clarithromycin intermediate, essentially oxime-free clarithromycin, and pharmaceutical composition comprising the same
    2.
    发明申请
    Processes for preparing clarithromycin and clarithromycin intermediate, essentially oxime-free clarithromycin, and pharmaceutical composition comprising the same 审中-公开

    公开(公告)号：US20060205683A1

    公开(公告)日：2006-09-14

    申请号：US11432983

    申请日：2006-05-11

    申请人： Ilya Avrutov ,  Igor Lifshitz ,  Elizabeth Lewiner

    发明人： Ilya Avrutov ,  Igor Lifshitz ,  Elizabeth Lewiner

    IPC分类号： A61K31/7048 ,  C07H17/08

    CPC分类号： C07H17/08 ,  C07F7/1892

    摘要： The present invention relates to processes for preparing protected silylated clarithromycin oxime, preferably 6-O-methyl-2′, 4″-bis(trimethylsilyl)-erythromycin A 9-O-(2-methoxyprop-2-yl)oxime (“S-MOP oxime”), and for converting protected silylated clarithromycin oxime, preferably S-MOP oxime, to clarithromycin. Processes for preparing protected silylated clarithromycin oxime according to the present invention, include reacting a silyl oxime derivative with methylating agent in the presence of at least one solvent and a base, where the solvent comprises methyl tertbutyl ether. Processes for converting protected silylated clarithromycin oxime to clarithromycin according to the present invention, include reacting protected silylated clarithromycin oxime with ethanol and water at an ethanol to water ratio of about 1:1, in the presence of an acid and a deoximating agent and cooling the reaction mixture prior to adding sodium hydroxide, where the process takes place without any additional water addition. Further processes for converting protected silylated clarithromycin oxime to clarithromycin, include heating a mixture of protected silylated clarithromycin oxime, acid, and deoximating agent in an ethanol/water solvent to reflux for more than 4 hours, with a two-fold addition of deoximating agent to produce essentially oxime-free clarithromycin.

    Processes for preparing clarithromycin and clarithromycin intermediate, essentially oxime-free clarithromycin, and pharmaceutical composition comprising the same
    3.
    发明授权
    Processes for preparing clarithromycin and clarithromycin intermediate, essentially oxime-free clarithromycin, and pharmaceutical composition comprising the same 失效

    公开(公告)号：US07101858B2

    公开(公告)日：2006-09-05

    申请号：US10435141

    申请日：2003-05-09

    申请人： Ilya Avrutov ,  Igor Lifshitz ,  Elizabeth Lewiner

    发明人： Ilya Avrutov ,  Igor Lifshitz ,  Elizabeth Lewiner

    IPC分类号： A61K31/70 ,  C07H17/08

    CPC分类号： C07H17/08 ,  C07F7/1892

    摘要： The present invention relates to processes for preparing protected silylated clarithromycin oxime, preferably 6-O-methyl-2′,4″-bis(trimethylsilyl)-erythromycin A 9-O-(2-methoxyprop-2-yl)oxime (“S-MOP oxime”), and for converting protected silylated clarithromycin oxime, preferably S-MOP oxime, to clarithromycin. Processes for preparing protected silylated clarithromycin oxime according to the present invention, include reacting a silyl oxime derivative with methylating agent in the presence of at least one solvent and a base, where the solvent comprises methyl tertbutyl ether. Processes for converting protected silylated clarithromycin oxime to clarithromycin according to the present invention, include reacting protected silylated clarithromycin oxime with ethanol and water at an ethanol to water ratio of about 1:1, in the presence of an acid and a deoximating agent and cooling the reaction mixture prior to adding sodium hydroxide, where the process takes place without any additional water addition. Further processes for converting protected silylated clarithromycin oxime to clarithromycin, include heating a mixture of protected silylated clarithromycin oxime, acid, and deoximating agent in an ethanol/water solvent to reflux for more than 4 hours, with a two-fold addition of deoximating agent to produce essentially oxime-free clarithromycin.

    Risedronate sodium having a very low content of iron
    4.
    发明授权
    Risedronate sodium having a very low content of iron 失效
    利塞膦酸钠具有非常低的铁含量

    公开(公告)号：US07358360B2

    公开(公告)日：2008-04-15

    申请号：US10759919

    申请日：2004-01-16

    申请人： Revital Lifshitz-Liron ,  Ramiy Lidor-Hadas ,  Nissm Sasson ,  Igor Lifshitz

    发明人： Revital Lifshitz-Liron ,  Ramiy Lidor-Hadas ,  Nissm Sasson ,  Igor Lifshitz

    IPC分类号： C07F9/28

    CPC分类号： C07F9/59

    摘要： The present invention relates to a method of making risedronate sodium substantially free of iron including the steps of refluxing, especially with mechanical agitation, a combination of risedronic acid, a sodium base, especially sodium hydroxide, and an iron-reducing amount of EDTA in a liquid that is water, a lower alkanol, or, especially, a mixture of a lower alkanol and water; and isolating risedronate sodium substantially free of iron from the combination.

    摘要翻译： 本发明涉及一种制备基本上不含铁的利塞膦酸钠的方法，包括以下步骤：特别是机械搅拌下，将利塞膦酸，钠碱，特别是氢氧化钠和减铁量的EDTA的组合在 液体是水，低级链烷醇，或特别是低级链烷醇和水的混合物; 并从该组合中分离出基本上不含铁的利塞膦酸钠。

    Process for preparing pure crystalline lorazepam
    7.
    发明授权
    Process for preparing pure crystalline lorazepam 失效
    制备纯结晶劳拉西泮的方法

    公开(公告)号：US06350870B2

    公开(公告)日：2002-02-26

    申请号：US09799318

    申请日：2001-03-05

    申请人： Igor Lifshitz

    发明人： Igor Lifshitz

    IPC分类号： C07D24324

    CPC分类号： C07D243/24

    摘要： The present invention provides a process for preparing crystalline lorazepam substantially free of bound solvent from a lorazepam alcohol solvate or hydrate by suspending the lorazepam solvate in an organic medium selected from ethyl acetate, cyclohexane, dichloromethane, toluene and mixtures thereof. This process is useful in producing the anti-anxiety and sedative agent lorazepam in increased yields. A process for converting lorazepam lower alcohol solvates to lorazepam hydrate is also disclosed.

    摘要翻译： 本发明提供了一种通过将劳拉西泮溶剂化物悬浮在选自乙酸乙酯，环己烷，二氯甲烷，甲苯及其混合物的有机介质中来制备基本上不含结合的溶剂的劳拉西泮醇溶剂化物或水合物的结晶性劳拉西泮的方法。 该方法可用于产生抗焦虑和镇静剂劳拉西泮的产量增加。 还公开了将劳拉西泮低级醇溶剂化物转化为水合氯雷他平的方法。

    Food press form
    8.
    发明授权
    Food press form 失效
    食品新闻形式

    公开(公告)号：US4362497A

    公开(公告)日：1982-12-07

    申请号：US293513

    申请日：1981-08-14

    申请人： Igor Lifshitz

    发明人： Igor Lifshitz

    IPC分类号： A21C11/00 ,  A21C11/10 ,  B29C1/00

    CPC分类号： A21C11/106 ,  A21C11/00

    摘要： Food products are processed prior to consumption in a press form having multiple, separate, pre-selected planar food product molds, each having tapered walls, providing easy food product removal. The food products can have pastry dough exteriors and can be filled with selected food fillings held in position and shaped by dough crust exteriors. Multiple press form food product molds have regular planar shapes disposed multiple in a tray. One face of each product mold has a cutting-edge knife disposed thereon, conforming to the mold interior shape. The cutting-edge knife can be disposed at either mold wall taper terminus. A cooperatively shaped, one-piece negative pusher plug mold, sized to intercept each one of the multiple food product molds disposed in the tray, is used to cooperatively push each food product out of the molds in the tray simultaneously. Additional, easily insertable and removable partitions of single and double cross-wise edge-knife units can be disposed in the molds, further dividing the food products.

    摘要翻译： 食品在消费之前被加工成具有多个分开的，预选的平面食品模具的压榨形式，每个模具具有锥形壁，从而提供容易的食品移除。 食品可以有糕点面团外观，并且可以填充保持在适当位置的选定的食物馅料，并通过面外皮成型。 多重冲压成​​型食品模具在托盘中具有多个布置的规则的平面形状。 每个产品模具的一个面具有设置在其上的切割刀，符合模具内部形状。 前刀可以设置在任何一个模具壁锥形终点。 用于协调地设置成拦截设置在托盘中的多个食品模具中的每一个的协同成形的单件式负推塞模具用于将每个食品同时推出托盘中的模具。 另外，可以在模具中设置单个和两个交叉边缘刀单元的容易插入和移除的隔板，进一步分割食品。

    Crystalline forms of carvedilol and processes for their preparation
    9.
    发明申请
    Crystalline forms of carvedilol and processes for their preparation 审中-公开
    卡维地洛的结晶形式及其制备方法

    公开(公告)号：US20070043099A1

    公开(公告)日：2007-02-22

    申请号：US11450699

    申请日：2006-06-09

    申请人： Igor Lifshitz ,  Shlomit Wizel

    发明人： Igor Lifshitz ,  Shlomit Wizel

    IPC分类号： A61K31/403 ,  C07D209/82

    CPC分类号： C07D209/88

    摘要： This invention relates to a novel crystalline form of carvedilol, to processes for its preparation, to compositions containing it and to its use in medicine. This invention further relates to a novel process for preparing crystalline carvedilol Form II.

    摘要翻译： 本发明涉及一种新颖的卡维地洛结晶形式，其制备方法，含有它的组合物及其在药物中的用途。 本发明还涉及制备结晶卡维地洛II型的新方法。