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    N-[5-(Aminosulfony1)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate
    81.
    发明授权
    N-[5-(Aminosulfony1)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate 有权
    N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基]乙酰胺甲磺酸盐一水合物

    公开(公告)号：US09340535B2

    公开(公告)日：2016-05-17

    申请号：US14347287

    申请日：2012-09-26

    申请人： AiCuris GmbH & Co. KG

    发明人： Wilfried Schwab ,  Alexander Birkmann ,  Kurt Vogtli ,  Dieter Haag ,  Andreas Lender ,  Alfons Grunenberg ,  Birgit Keil ,  Joachim Rehse

    IPC分类号： C07D417/12

    CPC分类号： C07D417/12

    摘要： The present invention relates to an improved and shortened synthesis of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide and the mesylate monohydrate salt thereof by using boronic acid derivatives or borolane reagents while avoiding toxic organic tin compounds and to the mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions.

    摘要翻译： 本发明涉及N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基 ]乙酰胺及其甲磺酸酯一水合物盐，同时避免有毒的有机锡化合物和N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑烷酮的甲磺酸酯一水合物盐， 2-基] -N-甲基-2- [4-（2-吡啶基）苯基]乙酰胺，证明了药物组合物的长期稳定性和释放动力学。

    CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARMACEUTICAL FORMULATIONS
    82.
    发明申请
    CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARMACEUTICAL FORMULATIONS 有权
    N- [5-（氨基甲酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基]乙酰胺单甲酸酯单磺酸盐具有特定颗粒尺寸 分配范围和用于制药配方的特定面积范围

    公开(公告)号：US20160008341A1

    公开(公告)日：2016-01-14

    申请号：US14840690

    申请日：2015-08-31

    申请人： AICURIS GMBH & CO. KG

    发明人： Wilfried SCHWAB ,  Alexander BIRKMANN ,  Kerstin PAULUS ,  Kurt VOGTLI ,  Dieter HAAG ,  Stephan MAAS ,  Kristian RUEPP

    IPC分类号： A61K31/4439 ,  A61K45/06 ,  A61K9/16

    CPC分类号： A61K31/4439 ,  A61K9/145 ,  A61K9/16 ,  A61K31/10 ,  A61K45/06 ,  C07D417/12 ,  Y10T428/2982

    摘要： The present invention relates to the crystalline mono mesylate monohydrate salt of N-[5-(amino sulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide in a definite particle size range, particle size distribution and a specific surface area range, which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions, as well as to pharmaceutical compositions containing said crystalline N-[5-(amino sulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mono mesylate monohydrate having the afore-mentioned particle size range, particle size distribution and specific surface area range. Moreover, the present invention relates to the pharmacokinetic and pharmacodynamic in vivo profiles of the resultant free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]-acetamide after administration of the afore-mentioned crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]-acetamide mono mesylate monohydrate salt to a subject in need thereof.

    摘要翻译： 本发明涉及N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基） ）苯基]乙酰胺，具有明确的粒度范围，粒度分布和比表面积范围，其已经证明了药物组合物的长期稳定性和释放动力学增加，以及含有所述N- [5-（ 氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基]乙酰胺单甲磺酸酯一水合物，具有上述粒径范围，粒径 分布和比表面积范围。 此外，本发明涉及得到的N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2-吡咯烷酮的游离碱的体内药代动力学和药效学特征， [4-（2-吡啶基）苯基] - 乙酰胺在给予上述N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基] - 乙酰胺单甲磺酸盐一水合物盐。

    Crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mono mesylate monohydrate having a specific particle size distribution range and a specific surface area range for use in pharmaceutical formulations
    83.
    发明授权
    Crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mono mesylate monohydrate having a specific particle size distribution range and a specific surface area range for use in pharmaceutical formulations 有权
    具有特定粒度的结晶N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基]乙酰胺单甲磺酸酯一水合物 分布范围和用于药物制剂的比表面积范围

    公开(公告)号：US09119786B2

    公开(公告)日：2015-09-01

    申请号：US14069850

    申请日：2013-11-01

    申请人： AICURIS GMBH & CO. KG

    发明人： Wilfried Schwab ,  Alexander Birkmann ,  Kerstin Paulus ,  Kurt Vogtli ,  Dieter Haag ,  Stephan Maas ,  Kristian Ruepp

    IPC分类号： A61K45/06 ,  A61K31/10 ,  A61K9/14 ,  A61K31/4439 ,  C07D417/12

    CPC分类号： A61K31/4439 ,  A61K9/145 ,  A61K9/16 ,  A61K31/10 ,  A61K45/06 ,  C07D417/12 ,  Y10T428/2982

    摘要： The present invention relates to the crystalline mono mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide in a definite particle size range, particle size distribution and a specific surface area range, which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions, as well as to pharmaceutical compositions containing said crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mono mesylate monohydrate having the afore-mentioned particle size range, particle size distribution and specific surface area range. Moreover, the present invention relates to the pharmacokinetic and pharmacodynamic in vivo profiles of the resultant free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]-acetamide after administration of the afore-mentioned crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]-acetamide mono mesylate monohydrate salt to a subject in need thereof.

    摘要翻译： 本发明涉及N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基） 苯基]乙酰胺，其具有确定的粒度范围，粒度分布和比表面积范围，其已经证明了药物组合物的长期稳定性和释放动力学的增加，以及含有所述N- [5-（氨基磺酰基） ）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基]乙酰胺单甲磺酸酯一水合物，具有上述粒度范围，粒度分布和 比表面积范围。 此外，本发明涉及得到的N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2-吡咯烷酮的游离碱的体内药代动力学和药效学特征， [4-（2-吡啶基）苯基] - 乙酰胺在给予上述N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基] - 乙酰胺单甲磺酸盐一水合物盐。

    PHARMACEUTICAL COMPOSITION CONTAINING AN ANTIVIRALLY ACTIVE DIHYDROQUINAZOLINE DERIVATIVE
    84.
    发明申请
    PHARMACEUTICAL COMPOSITION CONTAINING AN ANTIVIRALLY ACTIVE DIHYDROQUINAZOLINE DERIVATIVE 审中-公开
    含有杀真菌活性二氢吲哚啉衍生物的药物组合物

    公开(公告)号：US20150133461A1

    公开(公告)日：2015-05-14

    申请号：US14381290

    申请日：2013-02-28

    申请人： AICURIS GMBH & CO. KG

    发明人： Kerstin Paulus ,  Wilfried Schwab ,  Dominique Grunder ,  Peter Van Hoogevest

    IPC分类号： A61K47/40 ,  A61K47/26 ,  A61K47/18 ,  A61K47/02 ,  A61K31/517 ,  A61K9/00

    摘要： The invention relates to pharmaceutical compositions, particularly for intravenous administration, containing {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid in combination with at least one of the cyclodextrin excipients, lysine and arginine; the method for its production; and its use in methods of treatment of and/or as a prophylactic for illnesses, particularly its use as an antiviral, preferably against cytomegaloviruses.

    摘要翻译： 本发明涉及含有{8-氟-2- [4-（3-甲氧基苯基）哌嗪-1-基] -3- [2-甲氧基-5-（三氟甲基）苯基] - 3,4-二氢喹唑啉-4-基}乙酸与至少一种环糊精赋形剂，赖氨酸和精氨酸组合; 其生产方法; 及其在治疗和/或预防疾病的方法中的用途，特别是其用作抗病毒剂，优选抗巨细胞病毒的方法。

    N-[5-(Aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate
    87.
    发明申请
    N-[5-(Aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate 有权
    N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基]乙酰胺甲磺酸盐一水合物

    公开(公告)号：US20140221433A1

    公开(公告)日：2014-08-07

    申请号：US14347287

    申请日：2012-09-26

    申请人： AiCuris GmbH & Co. KG

    发明人： Wilfried Schwab ,  Alexander Birkmann ,  Kurt Vogtli ,  Dieter Haag ,  Andreas Lender ,  Alfons Grunenberg ,  Birgit Keil ,  Joachim Reshe

    IPC分类号： C07D417/12

    CPC分类号： C07D417/12

    摘要： The present invention relates to an improved and shortened synthesis of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide and the mesylate monohydrate salt thereof by using boronic acid derivatives or borolane reagents while avoiding toxic organic tin compounds and to the mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions.

    摘要翻译： 本发明涉及N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基 ]乙酰胺及其甲磺酸酯一水合物盐，同时避免有毒的有机锡化合物和N- [5-（氨基磺酰基）-4-甲基-1,3-噻唑烷酮的甲磺酸酯一水合物盐， 2-基] -N-甲基-2- [4-（2-吡啶基）苯基]乙酰胺，证明了药物组合物的长期稳定性和释放动力学。