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    1,4,5,6-tetrahydropyrimidine derivative as a vitronectin inhibitor
    2.
    发明授权
    1,4,5,6-tetrahydropyrimidine derivative as a vitronectin inhibitor 有权
    1,4,5,6-四氢嘧啶衍生物作为玻连蛋白抑制剂

    公开(公告)号：US06900318B1

    公开(公告)日：2005-05-31

    申请号：US10031121

    申请日：2000-07-08

    申请人： Gerhard Breipohl ,  Anuschirwam Peyman ,  Theodor Wollmann

    发明人： Gerhard Breipohl ,  Anuschirwam Peyman ,  Theodor Wollmann

    IPC分类号： A61K31/505 ,  A61P1/02 ,  A61P3/10 ,  A61P3/14 ,  A61P5/24 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D239/16 ,  C07D239/42

    CPC分类号： C07D239/42 ,  C07D239/16

    摘要： The present invention relates to ethyl (2S)-2-(naphthalene-1-sulfonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionate hemifumarate of formula (I), and to a process for its preparation comprising reacting 4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoic acid or a derivative thereof and ethyl (2S)-3-amino-2-(naphthalene-1-sulfonylamino)propionate. The compound of formula (I) is a valuable pharmaceutical which can be used, for example, in the treatment or prophylaxis of diseases which can be influenced by inhibiting the vitronectin receptor, in particular of bone diseases such as osteoporosis. The invention furthermore relates to chemical intermediates useful for the preparation of the compound of formula (I).

    摘要翻译： 本发明涉及（2S）-2-（萘-1-磺酰基氨基）-3-（4-（2-（1,4,5,6-四氢嘧啶-2-基氨基甲酰基）乙基）苯甲酰氨基）丙酸乙酯半富马酸乙酯 （I）化合物及其制备方法，包括使4-（2-（1,4,5,6-四氢嘧啶-2-基氨基甲酰基）乙基）苯甲酸或其衍生物与（2S）-3- 氨基-2-（萘-1-磺酰基氨基）丙酸酯。 式（I）化合物是一种有价值的药物，其可用于例如治疗或预防可通过抑制玻连蛋白受体，特别是骨疾病例如骨质疏松症而受影响的疾病。 本发明还涉及可用于制备式（I）化合物的化学中间体。

    Diastereomers of 1-(isopropoxycarbonyloxy) ethyl 3-cephem 4-carboxylate
    5.
    发明授权
    Diastereomers of 1-(isopropoxycarbonyloxy) ethyl 3-cephem 4-carboxylate 失效
    1-（异丙氧基羰基氧基）乙基3-头孢烯-4-羧酸酯的非对映异构体

    公开(公告)号：US5550232A

    公开(公告)日：1996-08-27

    申请号：US447229

    申请日：1995-05-22

    申请人： Gerd Fischer ,  Elisabeth Defossa ,  Uwe Gerlach ,  Rolf H orlein ,  Norbert Krass ,  Rudolf Lattrell ,  Ulrich Stache ,  Theodor Wollmann ,  Dieter Isert

    发明人： Gerd Fischer ,  Elisabeth Defossa ,  Uwe Gerlach ,  Rolf H orlein ,  Norbert Krass ,  Rudolf Lattrell ,  Ulrich Stache ,  Theodor Wollmann ,  Dieter Isert

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/06 ,  C07D501/34 ,  C07D501/56 ,  C07D501/14

    CPC分类号： C07D501/00

    摘要： Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(methoxymethyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.2-2 equivalents of a solution of the acid component HY and separating it off by filtration, then precipitating the more readily soluble diastereomer of the formula IV from the filtration solution, it being possible for the acid component HY to be identical or different in the consecutive partial steps and any desired sequence of addition of different acid components HY being possible, and optionally further purifying the obtained salts by crystallization, are described.

    摘要翻译： 1-（异丙氧羰基氧基）乙基（6R，7R）-7- [2-（2-氨基噻唑-4-基）-2-（Z） - （甲氧基亚氨基）乙酰氨基] -3-（甲氧基甲基）-3 式I的化合物 - 头孢烯-4-羧酸酯及其生理学上可接受的盐以及式II化合物的非对映体纯盐，其中HX是单或多元酸，其中X是无机或有机的 生理学上可接受的阴离子，以及制备这些式I或II化合物的方法，其包括首先将式IV的较微溶的非对映体沉淀在1当量的式（I）的非对映体混合物的溶液中， III与0.2-2当量的酸组分HY的溶液并通过过滤分离，然后从过滤溶液中沉淀出更容易溶解的式IV的非对映异构体，酸组分HY可能相同或不同 在一起 描述了部分步骤和任何期望的不同酸组分HY的加入顺序是可能的，并且任选地通过结晶进一步纯化得到的盐。

    Diastereomers of 1-(isopropoxycarbonyloxy)ethyl 3-cephem-4-carboxylate and processes for their preparation
    10.
    发明授权
    Diastereomers of 1-(isopropoxycarbonyloxy)ethyl 3-cephem-4-carboxylate and processes for their preparation 失效
    3-头孢烯-4-羧酸1-（异丙氧基羰基氧基）乙酯的非对映异构体及其制备方法

    公开(公告)号：US5614623A

    公开(公告)日：1997-03-25

    申请号：US447249

    申请日：1995-05-22

    申请人： Gerd Fischer ,  Elisabeth Defo.beta.a ,  Uwe Gerlach ,  Rolf H orlein ,  Norbert Krass ,  Rudolf Lattrell ,  Ulrich Stache ,  Theodor Wollmann ,  Dieter Isert

    发明人： Gerd Fischer ,  Elisabeth Defo.beta.a ,  Uwe Gerlach ,  Rolf H orlein ,  Norbert Krass ,  Rudolf Lattrell ,  Ulrich Stache ,  Theodor Wollmann ,  Dieter Isert

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/06 ,  C07D501/34 ,  C07D501/56 ,  C07D501/22

    CPC分类号： C07D501/00

    摘要： Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R, 7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(methoxymethyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.2-2 equivalents of a solution of the acid component HY and separating it off by filtration, then precipitating the more readily soluble diastereomer of the formula IV from the filtration solution, it being possible for the acid component HY to be identical or different in the consecutive steps.

    摘要翻译： 1-（异丙氧羰基氧基）乙基（6R，7R）-7- [2-（2-氨基噻唑-4-基）-2-（Z） - （甲氧基亚氨基）乙酰氨基] -3-（甲氧基甲基）-3 式I的化合物 - 头孢烯-4-羧酸酯及其生理学上可接受的盐以及式II化合物的非对映体纯盐，其中HX是单或多元酸，其中X是无机或有机的 生理学上可接受的阴离子，以及制备这些式I或II化合物的方法，其包括首先将式IV的较微溶的非对映体沉淀在1当量的式（I）的非对映体混合物的溶液中， III与0.2-2当量的酸组分HY的溶液并通过过滤分离，然后从过滤溶液中沉淀出更容易溶解的式IV的非对映异构体，酸组分HY可能相同或不同 在consecu 有步骤。