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110 条记录 (耗时 0.039 秒)

    Process for preparing organic compounds
    71.
    发明授权
    Process for preparing organic compounds 失效
    制备有机化合物的方法

    公开(公告)号：US07723550B2

    公开(公告)日：2010-05-25

    申请号：US12224418

    申请日：2007-11-08

    申请人： Peter Herold ,  Robert Mah ,  Stefan Stutz ,  Aleksandar Stojanovic ,  Isabelle Lyothier ,  Dirk Behnke

    发明人： Peter Herold ,  Robert Mah ,  Stefan Stutz ,  Aleksandar Stojanovic ,  Isabelle Lyothier ,  Dirk Behnke

    IPC分类号： C07C29/36 ,  C07C29/44 ,  C07C41/18 ,  C07C41/30 ,  C07C43/23

    CPC分类号： C07C41/20 ,  C07B2200/07 ,  C07C41/22 ,  C07C41/30 ,  C07C231/12 ,  C07C235/34 ,  C07C43/23 ,  C07C43/225

    摘要： Process for preparing a compound of the formula (I) in which R1 and R2 are each independently H, C1-C8-alkyl, halogen, polyhalo-C1-C8-alkoxy, polyhalo-C1-C8-alkyl, C1-C8-alkoxy, C1-C8-alkoxy-C1-C8-alkyl, or C1-C8-alkoxy-C1-C8-alkoxy, where R1 and R2 are not both H, and R3 is C1-C8-alkyl, which is characterized in that a) a compound of the formula (II) in which R1 and R2 are each as defined above and X is Br, I, triflate, toyslate or mesylate is reacted with prop-2-yn-1-ol to give the compound of the formula (III), b) the compound of the formula (III) is reacted with an alkyl-metal compound in which “alkyl” is as defined above for R3 to give a compound of the formula (I).

    摘要翻译： 制备式（I）化合物的方法，其中R 1和R 2各自独立地为H，C 1 -C 8 - 烷基，卤素，多卤代-C 1 -C 8 - 烷氧基，多卤代-C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基 ，C 1 -C 8 - 烷氧基-C 1 -C 8 - 烷基或C 1 -C 8 - 烷氧基-C 1 -C 8 - 烷氧基，其中R 1和R 2不都是H，且R 3是C 1 -C 8 - 烷基，其特征在于 ）其中R 1和R 2各自如上定义并且X是Br，I，三氟甲磺酸酯，玩具或甲磺酸酯的式（II）化合物与丙-2-炔-1-醇反应，得到式 （III）中，b）式（III）化合物与烷基金属化合物反应，其中“烷基”如上述R3所定义，得到式（I）化合物。

    Process for Preparing organic compounds
    73.
    发明申请
    Process for Preparing organic compounds 失效
    制备有机化合物的方法

    公开(公告)号：US20090105503A1

    公开(公告)日：2009-04-23

    申请号：US12224418

    申请日：2007-11-08

    申请人： Peter Herold ,  Robert Mah ,  Stefan Stutz ,  Aleksandar Stojanovic ,  Isabelle Lyothier ,  Dirk Behnke

    发明人： Peter Herold ,  Robert Mah ,  Stefan Stutz ,  Aleksandar Stojanovic ,  Isabelle Lyothier ,  Dirk Behnke

    IPC分类号： C07C231/12 ,  C07C41/08 ,  C07C43/23

    CPC分类号： C07C41/20 ,  C07B2200/07 ,  C07C41/22 ,  C07C41/30 ,  C07C231/12 ,  C07C235/34 ,  C07C43/23 ,  C07C43/225

    摘要： Process for preparing a compound of the formula (I) in which R1 and R2 are each independently H, C1-C8-alkyl, halogen, polyhalo-C1-C8-alkoxy, polyhalo-C1-C8-alkyl, C1-C8-alkoxy, C1-C8-alkoxy-C1-C8-alkyl, or C1-C8-alkoxy-C1-C8-alkoxy, where R1 and R2 are not both H, and R3 is C1-C8-alkyl, which is characterized in that a) a compound of the formula (II) in which R1 and R2 are each as defined above and X is Br, I, triflate, toyslate or mesylate is reacted with prop-2-yn-1-ol to give the compound of the formula (III), b) the compound of the formula (III) is reacted with an alkyl-metal compound in which “alkyl” is as defined above for R3 to give a compound of the formula (I).

    摘要翻译： 制备式（I）化合物的方法，其中R 1和R 2各自独立地为H，C 1 -C 8 - 烷基，卤素，多卤代-C 1 -C 8 - 烷氧基，多卤代-C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基 ，C 1 -C 8 - 烷氧基-C 1 -C 8 - 烷基或C 1 -C 8 - 烷氧基-C 1 -C 8 - 烷氧基，其中R 1和R 2不都是H，且R 3是C 1 -C 8 - 烷基，其特征在于 ）其中R 1和R 2各自如上定义并且X是Br，I，三氟甲磺酸酯，玩具或甲磺酸酯的式（II）化合物与丙-2-炔-1-醇反应，得到式 （III）中，b）式（III）化合物与烷基金属化合物反应，其中“烷基”如上述R3所定义，得到式（I）化合物。

    Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa
    74.
    发明授权
    Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa 有权
    胰蛋白酶样丝氨酸蛋白酶抑制剂，它们的制备和用作凝血因子IIa和Xa的选择性抑制剂

    公开(公告)号：US08497245B2

    公开(公告)日：2013-07-30

    申请号：US13332900

    申请日：2011-12-21

    申请人： Peter Herold ,  Stjepan Jelakovic ,  Mohammed Daghish ,  Claudia Reichelt ,  Alexander Schulze ,  Andrea Schweinitz ,  Friedrich-Alexander Ludwig ,  Adel Rafai Far ,  Ting Kang

    发明人： Peter Herold ,  Stjepan Jelakovic ,  Mohammed Daghish ,  Claudia Reichelt ,  Alexander Schulze ,  Andrea Schweinitz ,  Friedrich-Alexander Ludwig ,  Adel Rafai Far ,  Ting Kang

    IPC分类号： A61K38/05

    CPC分类号： C07K5/06121 ,  A61K38/00 ,  C07K5/06104 ,  C07K5/06113 ,  C07K5/06191

    摘要： The invention provides methods of making and using compounds of the formula: or a pharmaceutically acceptable salt thereof; wherein n is an integer between 1 and 2 inclusively; m is an integer between 0 and 2 inclusively; X is selected from the group consisting of CH or N; R1 is selected from the group consisting of —CH2NH2, and R2 is selected from the group consisting of —H, —OH, —NH2 and acetyl; R3 is selected from the group consisting of —H, benzyloxycarbonyl and benzylsulfonyl; and R4 is selected from the group consisting of —OH, wherein p is an integer between 0 and 2 inclusively, Y is selected from the group consisting of —O—, —S—, —S(═O)—, —SO2—, methylene, —CH(OH)—, —CH(NH2)—, —CH(CH2—OH)—, —CH(CH2—NH2)— or —N(R6)—, R5 is selected from the group consisting of —H or a simple (C1-C3) alkyl and R6 is selected from the group consisting of —H, a simple (C1-C3) alkyl or a simple (C1-C3) acyl. These compounds are useful as anticoagulant agents as a result of their selective dual inhibition of thrombin and prothrombinase.

    摘要翻译： 本发明提供制备和使用下式的化合物或其药学上可接受的盐的方法： 其中n是1和2之间的整数; m是0和2之间的整数; X选自CH或N; R1选自-CH2NH2，R2选自-H，-OH，-NH2和乙酰基; R3选自-H，苄氧基羰基和苄基磺酰基; 并且R 4选自-OH，其中p是包括0和2的整数，Y选自-O - ， - S - ， - S（= O） - ， - SO 2 - ，亚甲基，-CH（OH） - ， - CH（NH 2） - ， - CH（CH 2 -OH） - ， - CH（CH 2 -NH 2） - 或-N（R 6） - ，R 5选自 -H或简单（C 1 -C 3）烷基，R 6选自-H，简单（C 1 -C 3）烷基或简单（C 1 -C 3）酰基）。 由于它们选择性双重抑制凝血酶和凝血酶原酶，这些化合物可用作抗凝血剂。