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    Crystalline citalopram diol intermediate alkali
    3.
    发明申请
    Crystalline citalopram diol intermediate alkali 有权
    结晶西酞普兰二醇中间体碱

    公开(公告)号：US20070117992A1

    公开(公告)日：2007-05-24

    申请号：US10583360

    申请日：2004-12-06

    申请人： Runan Mei ,  Dianwu Guo ,  Shulong Wang

    发明人： Runan Mei ,  Dianwu Guo ,  Shulong Wang

    IPC分类号： C07D307/81

    CPC分类号： C07D307/87 ,  C07C255/53

    摘要： The present invention relates to the diol intermediate of citalopram useful for treatment of depression, that is to say, the crystal of free alkali of 3-hydroxylmethyl-4-[1-(4-fluorophenyl)-1-hydroxyl-4-(dimethylamino)] butylbenzonitrile and the method of crystallization thereof. The present invention has disclosed the method to prepare pure citalopram and its purified salts through crystallization of the described alkali;the optical resolution method of citalopram diol intermediate, the method to prepare S-citalopram and its purified salts by crystals mentioned above. The present invention has also disclosed the method to prepare citalopram and its purified salts, S-citalopram and its purified salts, as well as pharmaceutical formulation thereof obtained. Using methods of the present invention, the quality and yield of the product can be signally improved, and the production cost of the medicinal material can be decreased.

    摘要翻译： 本发明涉及可用于治疗抑郁症的西酞普兰的二醇中间体，也就是3-羟甲基-4- [1-（4-氟苯基）-1-羟基-4-（二甲基氨基 ）]丁基苄腈及其结晶方法。 本发明公开了通过所述碱的结晶制备纯西酞普兰及其纯化盐的方法，西酞普兰二醇中间体的光学拆分方法，上述晶体制备S-西酞普兰及其纯化盐的方法。 本发明还公开了制备西酞普兰及其纯化盐S-西酞普兰及其纯化盐的方法及其药物制剂。 采用本发明的方法，可以显着提高产品的质量和产量，降低药材的生产成本。

    Quinazoline derivative, composition having the derivative, and use of the derivative in preparing medicament
    4.
    发明授权
    Quinazoline derivative, composition having the derivative, and use of the derivative in preparing medicament 有权
    喹唑啉衍生物，具有该衍生物的组合物，以及该衍生物在制备药物中的用途

    公开(公告)号：US09499530B2

    公开(公告)日：2016-11-22

    申请号：US14234326

    申请日：2012-07-21

    申请人： Shulong Wang ,  Jian Cai ,  Qiufu Ge ,  Dianwu Guo ,  Lan Yang ,  Binnan Huang ,  Zhenhua Liu ,  Zhonghua Peng ,  Ximing Shen ,  Feiyu Feng

    发明人： Shulong Wang ,  Jian Cai ,  Qiufu Ge ,  Dianwu Guo ,  Lan Yang ,  Binnan Huang ,  Zhenhua Liu ,  Zhonghua Peng ,  Ximing Shen ,  Feiyu Feng

    IPC分类号： C07D417/04 ,  C07D405/14 ,  C07D405/04 ,  C07D403/14

    CPC分类号： C07D417/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14

    摘要： A class of quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof with novel structures is provided; meanwhile, a pharmaceutical composition comprising a pharmaceutically effective amount of said quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof, and pharmaceutically acceptable excipients or additives is also provided. By modifying and transforming the quinazoline and screening of the transformed compounds on the activity of tyrosine kinase inhibition, most of the compounds have been found to possess inhibitory activity against one or several of EGFR, VEGFR-2, c-erbB-2, c-erbB-4, c-met, tie-2, PDGFR, c-src, lck, Zap70 and fyn kinases. The present invention has the advantages of reasonable design, broad source of and easy access to the raw materials, simple and easy operation of the preparation methods, mild reaction conditions, high yield of the products and being beneficial for industrial-scale production.

    摘要翻译： 提供了一类具有新颖结构的喹唑啉衍生物或其药学上可接受的盐或溶剂合物; 同时，还提供了包含药学上有效量的所述喹唑啉衍生物或其药学上可接受的盐或溶剂合物以及药学上可接受的赋形剂或添加剂的药物组合物。 通过修饰和转化喹唑啉和筛选转化的化合物对酪氨酸激酶抑制的活性，已经发现大多数化合物具有对EGFR，VEGFR-2，c-erbB-2，c- erbB-4，c-met，tie-2，PDGFR，c-src，lck，Zap70和fyn激酶。 本发明设计合理，原料来源广泛，易于获得原料，操作简便，制备方法简单，反应条件温和，产品收率高，有利于工业规模生产。

    Crystalline citalopram diol intermediate alkali
    5.
    发明授权
    Crystalline citalopram diol intermediate alkali 有权
    结晶西酞普兰二醇中间体碱

    公开(公告)号：US07435838B2

    公开(公告)日：2008-10-14

    申请号：US10583360

    申请日：2004-12-06

    申请人： Runan Mei ,  Dianwu Guo ,  Shulong Wang

    发明人： Runan Mei ,  Dianwu Guo ,  Shulong Wang

    IPC分类号： C07D307/78 ,  C07D307/87 ,  C07D307/93

    CPC分类号： C07D307/87 ,  C07C255/53

    摘要： The present invention relates to the diol intermediate of citalopram useful for treatment of depression, which is the crystal of free base of 3-hydroxylmethyl-4-[1-(4-fluorophenyl)-1-hydroxyl-4-(dimethylamino)]butylbenzonitrile and the method of crystallization thereof. The present invention has disclosed the method to prepare pure citalopram and its purified salts through crystallization of the described base; the optical resolution method of citalopram diol intermediate, the method to prepare S-citalopram and its purified salts by crystals mentioned above. The present invention has also disclosed the method to prepare citalopram and its purified salts, S-citalopram and its purified salts, as well as pharmaceutical formulation thereof obtained. Using methods of the present invention, the quality and yield of the product can be significantly improved, and the production cost of the medicinal material can be reduced.

    摘要翻译： 本发明涉及可用于治疗抑郁症的西酞普兰的二醇中间体，其是3-羟甲基-4- [1-（4-氟苯基）-1-羟基-4-（二甲基氨基）]丁基苄腈的游离碱的晶体 及其结晶方法。 本发明公开了通过所述碱的结晶制备纯西酞普兰及其纯化盐的方法; 西酞普兰二元醇中间体的光学拆分方法，上述晶体制备S-西酞普兰及其纯化盐的方法。 本发明还公开了制备西酞普兰及其纯化盐S-西酞普兰及其纯化盐的方法及其药物制剂。 采用本发明的方法可以显着提高产品的质量和产量，降低药材的生产成本。

    Curcumol derivatives, the compositions containing the said derivatives, and the use of the same in the manufacture of medicaments
    6.
    发明申请
    Curcumol derivatives, the compositions containing the said derivatives, and the use of the same in the manufacture of medicaments 失效
    姜黄衍生物，含有所述衍生物的组合物及其在制备药物中的用途

    公开(公告)号：US20070191360A1

    公开(公告)日：2007-08-16

    申请号：US11568770

    申请日：2005-05-26

    申请人： Shulong Wang ,  Dianwu Guo ,  Zhaoke Meng

    发明人： Shulong Wang ,  Dianwu Guo ,  Zhaoke Meng

    IPC分类号： A61K31/5377 ,  A61K31/506 ,  A61K31/496 ,  A61K31/452 ,  A61K31/353

    CPC分类号： C07D493/10 ,  C07D493/08 ,  C07D493/20

    摘要： The present invention provides curcumol derivatives of the following formula (I) or pharmaceutical acceptable salts thereof: wherein, Y is selected from the group consisting of ═CHR2, —CH2R2, ═O,  —OH or —OR1;R1 is selected from H, R, RCO or HO3S; and R is selected from the group consisting of H; saturated or unsaturated linear C1-10 hydrocarbon group and the like; R2 is selected from the group consisting of F; Cl; Br; I; H; —OH; —OR; —HSO3 and the like; with the proviso that both R1 and R2 are not H. The present invention also provides anti-tumor or antiviral pharmaceutical compositions comprising said derivatives or pharmaceutical acceptable salts thereof. The present invention further provides the use of said derivatives or pharmeceutical acceptable salts thereof in the preparation of a medicament for prophylaxis and/or treatment tumor or an antiviral medicament.

    摘要翻译： 本发明提供下式（I）的姜黄素衍生物或其药学上可接受的盐：其中Y选自-CHR 2，-CH 2， R 2，-O，-OH或-OR 1; R 1选自H，R，RCO或HO 3 并且R选自H; 饱和或不饱和直链C 1-10烃基等; R 2选自F; Cl; Br; 一世; H; -哦; -要么; -HSO 3等; 条件是R 1和R 2两者都不是H.本发明还提供了包含所述衍生物或其药学上可接受的盐的抗肿瘤或抗病毒药物组合物。 本发明还提供了所述衍生物或其药学上可接受的盐在制备用于预防和/或治疗肿瘤或抗病毒药物的药物中的用途。

    QUINAZOLINE DERIVATIVE, COMPOSITION HAVING THE DERIVATIVE, AND USE OF THE DERIVATIVE IN PREPARING MEDICAMENT
    8.
    发明申请
    QUINAZOLINE DERIVATIVE, COMPOSITION HAVING THE DERIVATIVE, AND USE OF THE DERIVATIVE IN PREPARING MEDICAMENT 有权
    喹啉衍生物，具有衍生物的组合物，以及衍生物在制备药物中的用途

    公开(公告)号：US20150080392A1

    公开(公告)日：2015-03-19

    申请号：US14234326

    申请日：2012-07-21

    申请人： Shulong Wang ,  Jian Cai ,  Qiufu Ge ,  Dianwu Guo ,  Lan Yang ,  Binnan Huang ,  Zhenhua Liu ,  Zhonghua Peng ,  Ximing Shen ,  Feiyu Feng

    发明人： Shulong Wang ,  Jian Cai ,  Qiufu Ge ,  Dianwu Guo ,  Lan Yang ,  Binnan Huang ,  Zhenhua Liu ,  Zhonghua Peng ,  Ximing Shen ,  Feiyu Feng

    IPC分类号： C07D417/04 ,  C07D403/14 ,  C07D405/04

    CPC分类号： C07D417/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14

    摘要： A class of quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof with novel structures is provided; meanwhile, a pharmaceutical composition comprising a pharmaceutically effective amount of said quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof, and pharmaceutically acceptable excipients or additives is also provided. By modifying and transforming the quinazoline and screening of the transformed compounds on the activity of tyrosine kinase inhibition, most of the compounds have been found to possess inhibitory activity against one or several of EGFR, VEGFR-2, c-erbB-2, c-erbB-4, c-met, tie-2, PDGFR, c-src, lck, Zap70 and fyn kinases. The present invention has the advantages of reasonable design, broad source of and easy access to the raw materials, simple and easy operation of the preparation methods, mild reaction conditions, high yield of the products and being beneficial for industrial-scale production.

    摘要翻译： 提供了一类具有新颖结构的喹唑啉衍生物或其药学上可接受的盐或溶剂合物; 同时，还提供了包含药学上有效量的所述喹唑啉衍生物或其药学上可接受的盐或溶剂合物以及药学上可接受的赋形剂或添加剂的药物组合物。 通过修饰和转化喹唑啉和筛选转化的化合物对酪氨酸激酶抑制的活性，已经发现大多数化合物具有对EGFR，VEGFR-2，c-erbB-2，c- erbB-4，c-met，tie-2，PDGFR，c-src，lck，Zap70和fyn激酶。 本发明设计合理，原料来源广泛，易于获得原料，操作简便，制备方法简单，反应条件温和，产品收率高，有利于工业规模生产。

    Curcumol derivatives, the compositions containing the said derivatives, and the use of the same in the manufacture of medicaments
    10.
    发明授权
    Curcumol derivatives, the compositions containing the said derivatives, and the use of the same in the manufacture of medicaments 失效
    姜黄衍生物，含有所述衍生物的组合物及其在制备药物中的用途

    公开(公告)号：US07700584B2

    公开(公告)日：2010-04-20

    申请号：US11568770

    申请日：2005-05-26

    申请人： Shulong Wang ,  Dianwu Guo ,  Zhaoke Meng

    发明人： Shulong Wang ,  Dianwu Guo ,  Zhaoke Meng

    IPC分类号： A61K43/00 ,  A61K43/16 ,  C07D311/94 ,  C07D265/30 ,  C07D401/00

    CPC分类号： C07D493/10 ,  C07D493/08 ,  C07D493/20

    摘要： The present invention provides curcumol derivatives of the following formula (I) or pharmaceutical acceptable salts thereof: wherein, Y is selected from the group consisting of ═CHR2, —CH2R2, ═O,  —OH or —OR1;R1 is selected from H, R, RCO or HO3S; and R is selected from the group consisting of H; saturated or unsaturated linear C1-10 hydrocarbon group and the like; R2 is selected from the group consisting of F; Cl; Br; I; H; —OH; —OR; —HSO3 and the like; with the proviso that both R1 and R2 are not H. The present invention also provides anti-tumor or antiviral pharmaceutical compositions comprising said derivatives or pharmaceutical acceptable salts thereof. The present invention further provides the use of said derivatives or pharmaceutical acceptable salts thereof in the preparation of a medicament for prophylaxis and/or treatment tumor or an antiviral medicament.

    摘要翻译： 本发明提供下式（I）的姜黄素衍生物或其药学上可接受的盐：其中Y选自：CHR 2，-CH 2 R 2，= O，-OH或-OR 1; R 1选自H， R，RCO或HO3S; 并且R选自H; 饱和或不饱和直链C 1-10烃基等; R2选自F; Cl; Br; 一世; H; -哦; -要么; -HSO 3等; 条件是R1和R2都不为H.本发明还提供包含所述衍生物或其药学上可接受的盐的抗肿瘤或抗病毒药物组合物。 本发明还提供了所述衍生物或其药学上可接受的盐在制备用于预防和/或治疗肿瘤或抗病毒药物的药物中的用途。