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    Diastereomers of 1-(isopropoxycarbonyloxy) ethyl 3-cephem 4-carboxylate
    3.
    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
    4.
    发明授权
    Diastereomers of 1-(isopropoxycarbonyloxy)ethyl 3-cephem-4-carboxylate 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

    公开(公告)号：US5461043A

    公开(公告)日：1995-10-24

    申请号：US940367

    申请日：1992-09-03

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

    发明人： Gerd Fischer ,  Elisabeth Defossa ,  Uwe Gerlach ,  Rolf Horlein ,  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 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
    6.
    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。

    Corticosteroid 17-alkyl carbonate 21-[0]-carboxylic and carbonic esters, and pharmaceuticals containing these compounds
    8.
    发明授权
    Corticosteroid 17-alkyl carbonate 21-[0]-carboxylic and carbonic esters, and pharmaceuticals containing these compounds 失效
    皮质类固醇17-烷基碳酸酯21- [0] - 羧酸和碳酸酯，以及含有这些化合物的药物

    公开(公告)号：US5608093A

    公开(公告)日：1997-03-04

    申请号：US294804

    申请日：1994-08-25

    申请人： Ulrich Stache ,  Hans-Georg Alpermann ,  Walter D urckheimer ,  Manfred Bohn

    发明人： Ulrich Stache ,  Hans-Georg Alpermann ,  Walter D urckheimer ,  Manfred Bohn

    IPC分类号： A61K31/57 ,  A61P17/00 ,  A61P29/00 ,  C07J5/00 ,  C07J17/00 ,  C07J31/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00 ,  A61K31/56

    CPC分类号： C07J5/0053 ,  C07J17/00 ,  C07J31/006 ,  C07J33/002 ,  C07J41/005 ,  C07J43/003 ,  C07J5/0076

    摘要： Corticoid 17-alkyl carbonate 21-carboxylic and carbonic esters of the formula I ##STR1## are described in which A is CHOH and CHCl, CH.sub.2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH.sub.3 ; R(1) is aryl or hetaryl; n and m are zero or 1; R(2) is alkyl or --(CH.sub.2).sub.2 --OCH.sub.3 ; R(3) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(5) is OH, with an activated carboxylic acid of the formula III,R(6)--CO--(O).sub.n --(X)--R(1) III.The compounds I have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects, which ratio is often markedly superior to that of analogous corticoid 17-alkyl carbonate 21-esters which do not carry any aryl or heteraryl group in the 21-ester radical.

    摘要翻译： 其中A是CHOH和CHCl，CH2，C = O或9（11）双键，其中描述了式I的皮质激素17-烷基碳酸酯21-羧酸和碳酸酯。 Y为H，F或Cl; Z是H，F或CH 3; R（1）是芳基或杂芳基; n和m为零或1; R（2）是烷基或 - （CH 2）2 -OCH 3; R（3）为H或甲基。 R（6）-CO-（O）n-（X）的活化羧酸与式（Ⅶ）化合物反应，其中R（5）为OH， -R（1）III。 化合物I具有非常强的局部和局部抗炎作用，并表现出非常好的局部与全身抗炎作用的比例，该比例通常明显优于不携带任何芳基或类似物的类似皮质类固醇17-烷基碳酸酯21-酯的比例 21位芳基中的杂芳基。

    Corticoid-17-alkyl-carbonates substituted in the 17-position, process for their preparation and pharmaceuticals containing them
    10.
    发明授权
    Corticoid-17-alkyl-carbonates substituted in the 17-position, process for their preparation and pharmaceuticals containing them 失效
    在17位取代的皮质类固醇-17-烷基 - 碳酸酯，其制备方法和含有它们的药物

    公开(公告)号：US5362721A

    公开(公告)日：1994-11-08

    申请号：US015041

    申请日：1993-02-08

    申请人： Ulrich Stache ,  Walter Durckheimer ,  Hans G. Alpermann ,  Walter Petri

    发明人： Ulrich Stache ,  Walter Durckheimer ,  Hans G. Alpermann ,  Walter Petri

    IPC分类号： A61K31/57 ,  A61P29/00 ,  A61P37/08 ,  C07J5/00 ,  C07J7/00 ,  C07J21/00 ,  C07J31/00 ,  C07J9/00

    CPC分类号： C07J7/0085 ,  C07J21/00 ,  C07J31/006 ,  C07J5/0053 ,  C07J5/0076

    摘要： The disclosed invention includes corticoid-17-alkylcarbonates substituted in the 17-position, a process for their preparation and pharmaceuticals containing them. These corticoid-17-alkylcarbonates have the following formula I ##STR1## where A is CHOH in any desired steric arrangement, C.dbd.O or CH.sub.2 ; Y is H, F, or Cl; Z is H, F or CH.sub.3 ; R(1) is O-acyl, carbonylalkyl, alkylsulfonate or arylsulfonate;R(2) is branched alkyl or (CH.sub.2).sub.2-4 --OCH.sub.3 andR(3) is H or methyl. They have excellent local and topical antiinflammatory action. They are distinguished by a particularly good ratio of local to systemic antiinflammatory activity and in some cases also show stronger local antiinflammatory activities than their isomeric corticoid-17-alkylcarbonates having a linear alkyl group in the 17-alkylcarbonate moiety.

    摘要翻译： 所公开的发明包括在17位取代的皮质类固醇-17-烷基碳酸酯，其制备方法和含有它们的药物。 这些皮质激素-17-烷基碳酸酯具有以下分子式I，其中A是任何所需空间排列中的CHOH，C = O或CH 2; Y是H，F或Cl; Z是H，F或CH 3; R（1）是O-酰基，羰基烷基，烷基磺酸酯或芳基磺酸酯; R（2）是支链烷基或（CH2）2-4-OCH3，R（3）是H或甲基。 他们具有优异的局部和局部抗炎作用。 它们的区别在于局部与系统性抗炎活性的比例特别好，并且在某些情况下也显示出比其在17-烷基碳酸酯部分具有直链烷基的异构的类皮质激素-17-烷基碳酸酯更强的局部抗炎活性。