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86 条记录 (耗时 0.044 秒)

    Novel benzothiazinone derivatives, processes for their preparation, medicaments containing them and their use
    52.
    发明授权
    Novel benzothiazinone derivatives, processes for their preparation, medicaments containing them and their use 失效
    新的苯并噻嗪酮衍生物，其制备方法，含有它们的药物及其用途

    公开(公告)号：US4831028A

    公开(公告)日：1989-05-16

    申请号：US42867

    申请日：1987-04-24

    申请人： Ulrich Lerch ,  Rainer Henning

    发明人： Ulrich Lerch ,  Rainer Henning

    IPC分类号： A61K31/54 ,  A61K31/5415 ,  A61P3/00 ,  A61P3/14 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D279/16

    CPC分类号： C07D279/16

    摘要： Benzothiazinone derivatives I ##STR1## with R.sup.1 and R.sup.4 being H, alkyl, alkoxy, Hal, CF.sub.3, NO.sub.2, OH, acetamido or amino,R.sup.2 being H, (cyclo)alk(en)yl, cycloalkylakyl, phenyl or phenylalkyl,A being (CH.sub.2).sub.m O(CH.sub.2).sub.n, (CH.sub.2).sub.p --CH(OH)--CH.sub.2).sub.q, (CH.sub.2).sub.p --CH(OCH.sub.3)--(CH.sub.2).sub.q, or (CH.sub.2).sub.r OCH.sub.2 --CO-- and (CH.sub.2).sub.s --CO--,R.sup.5 being NR(6)R(7) or certain cyclic amines, show a calcium-antagonistic action.They are obtained, inter alia, from II ##STR2## by reaction with III ##STR3## A and B are same or different and are lower alkylene having 1 to 6 carbon atoms; and n is 3 to 4.

    摘要翻译： 苯并噻嗪酮衍生物I（I）其中R 1和R 4是H，烷基，烷氧基，卤素，CF 3，NO 2，OH，乙酰氨基或氨基，R 2是H，（环）烷（烯）基，环烷基，苯基或苯基 ，（CH2）mO（CH2）n，（CH2）p-CH（OH）-CH2）q，（CH2）p-CH（OCH3） - （CH2）q或（CH2）rOCH2-CO-和 （CH2）s-CO-，R5是NR（6）R（7）或某些环胺，表现出钙拮抗作用。 它们是通过与III'相互作用而获得的，II'与III'相同或不同，并且是低级亚烷基 具有1至6个碳原子; n为3〜4。

    Process for the enantioselective synthesis of 2(R)-benzylsuccinic acid monoamide derivatives
    53.
    发明授权
    Process for the enantioselective synthesis of 2(R)-benzylsuccinic acid monoamide derivatives 失效
    2（R） - 苄基琥珀酸单酰胺衍生物的对映选择性合成方法

    公开(公告)号：US5321139A

    公开(公告)日：1994-06-14

    申请号：US22887

    申请日：1993-02-16

    申请人： Ulrich Lerch ,  Heiner Jendralla ,  Bernhard Seuring ,  Rainer Henning

    发明人： Ulrich Lerch ,  Heiner Jendralla ,  Bernhard Seuring ,  Rainer Henning

    IPC分类号： B01J31/24 ,  C07B61/00 ,  C07C231/02 ,  C07C231/18 ,  C07C233/14 ,  C07C233/22 ,  C07C233/40 ,  C07D211/44 ,  C07D211/58 ,  C07D241/04 ,  C07F9/572 ,  C07F15/00 ,  C07D211/06

    CPC分类号： C07F15/0013 ,  C07C231/18 ,  C07D211/58 ,  C07F15/008 ,  C07F9/5726

    摘要： Two processes are described for the preparation of the optically pure compounds of formula 1: ##STR1## in which R.sup.1 and R.sup.2 are e.g. alkyl, R.sup.3 and R.sup.4 are e.g. hydrogen and R.sup.5 is e.g. hydrogen. Both processes include, as key steps, the enantioselective hydrogenation of a C.dbd.C double bond and the regioselective formation of a dicarboxylic acid monoamide derivative. In one process a phenylitaconic acid derivative is asymmetrically hydrogenated to give an optically active (R)-benzylsuccinic acid which is then converted to a diester, said diester being converted to the monoamide compound of formula 1. In the second process, a phenylitaconic acid derivative is converted to its anhydride, and the anhydride is then converted to a monoamide which is then asymmetrically hydrogenated to give the compound of formula 1.

    摘要翻译： 描述了制备光学纯的式1化合物的两种方法：其中R 1和R 2是例如： 烷基，R 3和R 4是例如。 氢和R 5是例如。 氢。 作为关键步骤，两种方法都包括C = C双键的对映选择性氢化和二羧酸单酰胺衍生物的区域选择性形成。 在一个过程中，苯基衣康酸衍生物被不对称氢化，得到光学活性（R） - 苄基琥珀酸，然后将其转化为二酯，所述二酯转化成式1的单酰胺化合物。在第二种方法中，苯基衣康酸衍生物 转化成其酐，然后将酸酐转化为单酰胺，然后将其不对称氢化，得到式1的化合物。

    Pharmaceutical composition for treating haemorrhagic shock and its consecutive symptoms
    55.
    发明授权
    Pharmaceutical composition for treating haemorrhagic shock and its consecutive symptoms 失效
    用于治疗出血性休克及其连续症状的药物组合物

    公开(公告)号：US07897574B2

    公开(公告)日：2011-03-01

    申请号：US12158670

    申请日：2006-11-10

    申请人： Peter Petzelbauer ,  Rainer Henning

    发明人： Peter Petzelbauer ,  Rainer Henning

    IPC分类号： A61K38/36

    CPC分类号： A61K38/16 ,  Y02A50/411

    摘要： The invention is concerned with the use of a peptide comprising the N-terminal sequence Gly-His-Arg-Pro-Leu-Asp-Lys-Lys-Arg-Glu-Glu-Ala-Pro-Ser-Leu-Arg-Pro-Ala- Pro-Pro-Pro-Ile-Ser-Gly-Gly-Gly-Tyr-Arg (SEQ ID NO: 1) or any allelic variant or derivative of said peptide possessing the biological property of matching the inducible VE-cadherin binding motif on the Bβ-chain (i.e. Bβ15-42) of human fibrin for the preparation of a pharmaceutical preparation for the treatment of shock, more specifically of hemorrhagic shock.

    摘要翻译： 本发明涉及使用包含N-末端序列Gly-His-Arg-Pro-Leu-Asp-Lys-Lys-Arg-Glu-Glu-Ala-Pro-Ser-Leu-Arg-Pro- （SEQ ID NO：1）或具有与诱导型VE-钙粘蛋白结合基序匹配的生物学特性的所述肽的任何等位基因变体或衍生物（Pro-Pro-Pro-Pro-Ile-Ser-Gly-Gly-Gly-Tyr-Arg 在人类纤维蛋白的B＆bgr-chain（即B＆Bgr; 15-42）上制备用于治疗休克的药物制剂，更具体地说是出血性休克。

    (En) Pharmaceutical Composition for Treating Haemorrhagic Shock and its Consecutive Symptoms
    57.
    发明申请
    (En) Pharmaceutical Composition for Treating Haemorrhagic Shock and its Consecutive Symptoms 失效
    （En）用于治疗出血性休克及其连续症状的药物组合物

    公开(公告)号：US20090005310A1

    公开(公告)日：2009-01-01

    申请号：US12158670

    申请日：2006-11-10

    申请人： Peter Petzelbauer ,  Rainer Henning

    发明人： Peter Petzelbauer ,  Rainer Henning

    IPC分类号： A61K38/17 ,  A61P7/04 ,  C12Q1/02

    CPC分类号： A61K38/16 ,  Y02A50/411

    摘要： The invention is concerned with the use of a peptide comprising the N-terminal sequence Gly-His-Arg-Pro-Leu-Asp-Lys-Lys-Arg-Glu-Glu-Ala- Pro-Ser-Leu-Arg-Pro-Ala-Pro-Pro-Pro-Ile-Ser-Gly- Gly-Gly-Tyr-Arg or any allelic variant or derivative of said peptide possessing the biological property of matching the inducible VE-cadherin binding motif on the Bβ-chain (i.e. Bβ15-42) of human fibrin for the preparation of a pharmaceutical preparation for the treatment of shock, more specifically of hemorrhagic shock.

    摘要翻译： 本发明涉及使用包含N-末端序列的肽

    Pro-Ser-Leu-Arg-Pro-Ala-Pro -Pro-Pro-Ile-Ser-Gly - Gly-Gly-Tyr-Arg 或具有与Bbeta链上的诱导型VE-钙粘蛋白结合基序匹配的生物学特性的所述肽的任何等位基因变体或衍生物（即Bbeta15 -42），用于制备用于治疗休克的药物制剂，更具体地说是出血性休克。