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183 条记录 (耗时 0.017 秒)

    SUBSTITUTED HETEROCYCLIC COMPOUNDS AS CRAC MODULATORS
    32.
    发明申请
    SUBSTITUTED HETEROCYCLIC COMPOUNDS AS CRAC MODULATORS 有权
    取代的杂环化合物作为CRAC调节剂

    公开(公告)号：US20160145268A1

    公开(公告)日：2016-05-26

    申请号：US14899719

    申请日：2014-06-20

    申请人： LUPIN LIMITED

    发明人： Nageswara Rao IRLAPATI ,  Nilesh Raghunath KHEDKAR ,  Ravindra Babanrao JAPE ,  Rahul Shripad NANDURDIKAR ,  Zubair Abdul Wajid SHAIKH ,  Neelima SINHA ,  Venkata P. PALLE ,  Rajender Kumar KAMBOJ

    IPC分类号： C07D498/04 ,  C07D413/04 ,  C07D265/36 ,  C07D413/14 ,  C07D413/12 ,  C07D263/58 ,  C07D417/04

    CPC分类号： C07D498/04 ,  A61K31/5377 ,  C07D263/58 ,  C07D265/36 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04

    摘要： The invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine for the treatment of diseases, disorders associated with the modulation of calcium release-activated calcium (CRAC) channel. The invention also relates to pharmaceutical compositions containing such compounds in treating diseases disorders associated with calcium release-activated calcium (CRAC) channel modulators. wherein, ring D is Formula (a) or Formula (b): A and B, which may be same or different, are independently CR3 or N; Y is CR3 or N; L is selected from —NR2C(O)—, —C(O)NR2— and —NR2CRaRb—; Ra and Rb are independently hydrogen, halogen or substituted or unsubstituted alkyl; ring E is selected from the Formula (i) to (vii).

    摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中取代基如本文所述，及其在药物中的用途，用于治疗与调节钙释放激活的钙（CRAC）通道相关的疾病，病症 。 本发明还涉及含有这些化合物在治疗与钙释放激活的钙（CRAC）通道调节剂相关的疾病障碍中的药物组合物。 其中环D为式（a）或式（b）：A和B可以相同或不同，独立地为CR 3或N; Y是CR3或N; L选自-NR 2 C（O） - ， - C（O）NR 2 - 和-NR 2 CR a R b - ; R a和R b独立地是氢，卤素或取代或未取代的烷基; 环E选自式（i）至（vii）。

    NOVEL PROCESS AND INTERMEDIATE FOR PREPARATION OF ULIPRISTAL
    33.
    发明申请
    NOVEL PROCESS AND INTERMEDIATE FOR PREPARATION OF ULIPRISTAL 审中-公开
    新兴工艺和制备超临界的中间体

    公开(公告)号：US20150274770A1

    公开(公告)日：2015-10-01

    申请号：US14436179

    申请日：2013-10-01

    申请人： LUPIN LIMITED

    发明人： Purna Chandra Ray ,  Ajinath Tukaram Pathade ,  Suryaprakash Pandurang Patil ,  Yuvraj Atmaram Chavan ,  Girij Pal Singh ,  Dnyaneshwar Tukaram Singare ,  Yogesh Dadaji Pawar

    IPC分类号： C07J41/00

    CPC分类号： C07J41/0083

    摘要： The present invention is related to a novel process for the preparation of ulipristal (I) that comprises reaction of 17-α-ethynyl-17-β-hydroxy-11-β-(4-N,N-dimethylamino phenyl)- 9-norpregna-4,9-diene-3-one (III) with phenyl sulphenyl chloride (IVa) or p-nitro phenyl sulphenyl chloride (Nb) in the presence of organic base and solvent to give sulfoxide (Va) or (Vb) respectively. Sulfoxides (Va) or (Vb) are reacted with alkali metal alkoxide in alcoholic solvent followed by treatment with aqueous acid. The present invention also relates to novel intermediate 11-β-(4-N,N-dimethylaminophenyl)-21(p- nitro-phenyl-sulphinyl)-19-norpregna-4(5), 9(10), 17(20) 20-tetraene, 3-one (Vb).

    摘要翻译： 本发明涉及一种制备乌利司他（I）的新方法，其包括17-α-乙炔基-17-（b-n-羟基-11-和bgr-（4-N，N-二甲基氨基苯基） - （IVa）或对硝基苯基磺酰氯（Nb）在有机碱和溶剂存在下反应，得到亚砜（Ⅴa）或（Ⅴb）的9-异吖丁烷-4,9-二烯-3-酮 ） 分别。 将亚砜（Va）或（Vb）与醇溶剂中的碱金属醇盐反应，然后用含水酸处理。 本发明还涉及新的中间体11-（4-N，N-二甲基氨基苯基）-21（对硝基 - 苯基 - 亚磺酰基）-19-去甲基-4（5），9（10），17（ 20）20-四烯，3-酮（Vb）。

    PROCESS FOR PREPARATION OF RUFINAMIDE
    35.
    发明申请
    PROCESS FOR PREPARATION OF RUFINAMIDE 审中-公开
    制备联吡啶的方法

    公开(公告)号：US20140357871A1

    公开(公告)日：2014-12-04

    申请号：US14369811

    申请日：2013-01-09

    申请人： LUPIN LIMITED

    发明人： Rajinder Singh Siyan ,  Yogesh Subhas Aher ,  Nandu Baban Bhise ,  Girij Pal Singh ,  Sunilkumar Vinubhai Gohel

    IPC分类号： C07D249/04

    CPC分类号： C07D249/04

    摘要： The present invention relates to a novel process for preparation of rufinamide (I) comprising: reacting 2,6-difluorobenzyl azide (II) and propiolic acid (III) in a mixture of alcohol and water to produce 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid (IV), esterifying the acid (IV) to ester (V) and treating ester (V) with ammonia. The invention further relates to process for purification of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid (IV), by crystallization from a mixture of alcohol and water. The present invention also provides process for purification of rufinamide (I) by crystallization from mixture of polar aprotic solvent with water or alcohol.

    摘要翻译： 本发明涉及一种制备呋喃酰胺（I）的新方法，其包括：将2,6-二氟苄基叠氮化物（II）和丙炔酸（III）在醇和水的混合物中反应，得到1-（2,6-二氟苄基 ）-1H-1,2,3-三唑-4-甲酸（IV），将酸（IV）酯化为酯（V）并用氨处理酯（V）。 本发明还涉及通过从醇和水的混合物中结晶来纯化1-（2,6-二氟苄基）-1H-1,2,3-三唑-4-羧酸（Ⅳ）的方法。 本发明还提供了通过极性非质子传递溶剂与水或醇的混合物的结晶来纯化rufinamide（I）的方法。

    Method for preparation of ceftiofur and salts thereof
    37.
    发明申请
    Method for preparation of ceftiofur and salts thereof 失效
    头孢噻呋及其盐的制备方法

    公开(公告)号：US20040132996A1

    公开(公告)日：2004-07-08

    申请号：US10694619

    申请日：2003-10-27

    申请人： LUPIN LIMITED

    发明人： Om Dutt Tyagi ,  Santosh Kumar Richhariya ,  Rajesh Kumar Ramchandra Pawar

    IPC分类号： C07D501/14

    CPC分类号： C07D501/00

    摘要： A process for preparation of ceftiofur sodium of formula (Ib) 1 possessing high stability and having purity of more than 97% and substantially free of impurities, is disclosed. The process comprises:i) reacting cefotaxime or its salts or its esters of formula (VI) 2 nullwherein R3 is hydrogen, an alkali or alkaline earth metal, or an easily hydrolysable ester, with thiofuroic acid, employed in a molar proportion of 1.5 to 3.0 moles per mole of compound (VI), in the presence of acetonitrile as solvent and in the presence of large excess of methanesulfonic acid, employed in molar proportions of 12 to 18 moles per mole of compound (VI), and at a temperature of between null5null C. to 30null C. to give after necessary neutralisation of the alkali or alkaline earth metal or removal of the ester group of the 4-carboxylic acid function, wherever applicable, ceftiofur of formula (Ia), possessing high stability and having purity of more than 97% and substantially free of impurities; 3 ii) converting the ceftiofur of formula (Ia) thus obtained to its salt with an organic amine by treating a solution of ceftiofur in a mixture of water and a water-miscible organic solvent with an organic amine, at a temperature ranging from null10null C. to 10null C.; iii) reacting of the amine salt thus obtained with a sodium metal carrier in a mixture of water and water-miscible organic solvent and in presence of sodium hydrogen sulfite to give ceftiofur sodium of formula (Ib)

    摘要翻译： 公开了制备具有高稳定性和纯度大于97％且基本上不含杂质的式（Ib）头孢噻呋钠的方法。 该方法包括：i）使用摩尔比为1.5至3.0的头孢噻肟或其盐或其通式（VI）的酯，其中R 3为氢，碱金属或碱土金属或易水解的酯与硫代呋喃酸反应 摩尔每摩尔化合物（Ⅵ）在乙腈作为溶剂存在下和在大量过量的甲磺酸存在下，以摩尔比例为12至18摩尔/摩尔化合物（Ⅵ），并且在 在-5℃至30℃下，在必要时中和碱金属或碱土金属或除去适用的具有高稳定性的式（Ia）头孢噻呋酯的4-羧酸官能团的酯基， 纯度大于97％，基本上不含杂质; ii）通过在-10℃的温度范围内用有机胺处理水与水混溶性有机溶剂的混合物中的头孢噻肟溶液，将有机胺衍生的式（Ia）头孢噻吩转化为其盐 ℃至10℃。 iii）将由此获得的胺盐与水和水混溶性有机溶剂的混合物中的钠金属载体反应并在亚硫酸氢钠的存在下反应，得到式（Ib）的头孢噻肟钠，

    MODIFIED DOSING OF VEGF INHIBITORS FOR OPHTHALMIC USE
    40.
    发明申请
    MODIFIED DOSING OF VEGF INHIBITORS FOR OPHTHALMIC USE 有权

    公开(公告)号：US20220306732A1

    公开(公告)日：2022-09-29

    申请号：US17638966

    申请日：2020-09-10

    申请人： Lupin Limited

    发明人： Dhananjay Sadashiv BAKHLE ,  Chirag Anilkumar SHAH ,  Preetam Nivrutti CHAVAN

    IPC分类号： C07K16/22 ,  A61P27/02 ,  A61K9/00

    摘要： The present invention provides a method of treating ocular disorders by administering a suitable amount of VEGF inhibitors in a patient in need thereof, wherein the suitable amount of VEGF inhibitor is determined with respect to the body weight of the patient. Further, present invention also provides a method of treating ocular disorders by administering a personalized dose of a suitable amount of VEGF inhibitors intravitreally, wherein the dose is decided based on the body weight of the said patient at any given point in time.