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1. 发明授权

US5410042A Process for the cleavage of cephalosporin prodrug esters to 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid 失效
标题翻译：将头孢菌素前药酯切割成7-氨基-3-甲氧基甲基头孢-3-烯-4-羧酸的方法
公开(公告)号：US5410042A
公开(公告)日：1995-04-25
申请号：US063574
申请日：1993-05-19
申请人： Norbert Krass , Elisabeth Defossa , Gerd Fischer , Uwe Gerlach , Rolf Hoerlein , Rudolf Lattrell , Adolf H. Linkies , Wolfgang Martin , Ulrich Stache , Theodor Wollmann
发明人： Norbert Krass , Elisabeth Defossa , Gerd Fischer , Uwe Gerlach , Rolf Hoerlein , Rudolf Lattrell , Adolf H. Linkies , Wolfgang Martin , Ulrich Stache , Theodor Wollmann
IPC分类号： C07D501/00 , C07D501/04 , C07D501/18
CPC分类号： C07D501/00
摘要： The present invention relates to a process for the preparation of 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid (I) from 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid esters (II) or their salts by ester cleavage.The process comprises treating the compound II with formic acid, trifluoroacetic acid, methanesulfonic acid or trifluoromethanesulfonic acid or a mixture of two of these acids in each case.
摘要翻译：本发明涉及从7-氨基-3-甲氧基甲基头孢-3-烯-4-羧酸酯（II）制备7-氨基-3-甲氧基甲基头孢-3-烯-4-羧酸（I）的方法）或它们的盐通过酯裂解。该方法包括在各种情况下用甲酸，三氟乙酸，甲磺酸或三氟甲磺酸或这些酸的两种混合物处理化合物II。

2. 发明授权

US5637721A Process for the preparation of cephem prodrug esters 失效
标题翻译：头孢烯前药酯的制备方法
公开(公告)号：US5637721A
公开(公告)日：1997-06-10
申请号：US470422
申请日：1995-06-06
申请人： Elisabeth Defossa , Gerd Fischer , Uwe Gerlach , Rolf Horlein , Norbert Krass , Rudolf Lattrell , Ulrich Stache , Theodor Wollmann
发明人： Elisabeth Defossa , Gerd Fischer , Uwe Gerlach , Rolf Horlein , Norbert Krass , Rudolf Lattrell , Ulrich Stache , Theodor Wollmann
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D277/40 , C07D417/12 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/34
CPC分类号： C07D277/587 , C07D417/12 , C07D501/00 , Y02P20/55
摘要： The invention relates to a process which comprises a compound of the formula II ##STR1##
摘要翻译：本发明涉及包含式II化合物的方法

3. 发明授权

US5550232A Diastereomers of 1-(isopropoxycarbonyloxy) ethyl 3-cephem 4-carboxylate 失效
标题翻译： 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。

4. 发明授权

US5589594A Process for the preparation of cephem prodrug esters 失效
标题翻译：头孢烯前药酯的制备方法
公开(公告)号：US5589594A
公开(公告)日：1996-12-31
申请号：US176501
申请日：1993-12-30
申请人： Elisabeth Defossa , Gerd Fischer , Uwe Gerlach , Rolf Horlein , Norbert Krass , Rudolf Lattrell , Ulrich Stache , Theodor Wollmann
发明人： Elisabeth Defossa , Gerd Fischer , Uwe Gerlach , Rolf Horlein , Norbert Krass , Rudolf Lattrell , Ulrich Stache , Theodor Wollmann
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D277/40 , C07D417/12 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/34 , C07D501/02
CPC分类号： C07D277/587 , C07D417/12 , C07D501/00 , Y02P20/55
摘要： The invention relates to a process for the preparation of cephem prodrug esters of the formula: ##STR1## in which R.sup.1 is C.sub.1 -C.sub.5 -alkanoyloxy-C.sub.1 -C.sub.3 -alkyl or C.sub.1 -C.sub.5 -alkoxycarbonyloxy-C.sub.1 -C.sub.3 -alkyl and X is an inorganic or organic anion, and in which the hydroxyimino group is present in the syn-form.
摘要翻译：本发明涉及一种制备下式的头孢烯前药酯的方法：其中R 1是C 1 -C 5 - 烷酰氧基-C 1 -C 3 - 烷基或C 1 -C 5 - 烷氧羰基氧基-C 1 -C 3烷基和X 是无机或有机阴离子，其中羟基亚氨基以合成形式存在。

5. 发明授权

US5461043A Diastereomers of 1-(isopropoxycarbonyloxy)ethyl 3-cephem-4-carboxylate 失效
标题翻译： 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。

6. 发明授权

US5614623A Diastereomers of 1-(isopropoxycarbonyloxy)ethyl 3-cephem-4-carboxylate and processes for their preparation 失效
标题翻译： 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。

7. 发明授权

US5556850A Crystalline acid addition salts of diastereomerically pure 1-(2,2-dimethyl-propionyloxy)-ethyl-3-cephem-4-carboxylate 失效
标题翻译：非对映体纯的1-（2,2-二甲基 - 丙酰氧基） - 乙基-3-头孢烯-4-羧酸的结晶酸加成盐
公开(公告)号：US5556850A
公开(公告)日：1996-09-17
申请号：US447635
申请日：1995-05-23
申请人： Elisabeth Defossa , Gerd Fischer , Joachim-Heiner Jendralla , Rudolf Lattrell , Theodor Wollmann , Dieter Isert
发明人： Elisabeth Defossa , Gerd Fischer , Joachim-Heiner Jendralla , Rudolf Lattrell , Theodor Wollmann , Dieter Isert
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07B57/00 , C07D417/12 , C07D501/00 , C07D501/12 , C07D501/18 , C07D501/32 , C07D501/34
CPC分类号： C07D501/00
摘要： The invention relates to crystalline acid addition salt of the two diastereomers of the 1-(2,2-dimethylpropionyloxy)ethyl 3-cephem-4-carboxylate of the general formula II ##STR1## in which X is the anion of a physiologically acceptable, mono- or polybasic, inorganic or organic acid and the group .dbd.N--OH is in the syn-position, pharmaceutical formulations which are active against bacterial infections and contain such cephem derivatives, processes for the preparation of the cephem derivatives and the use of the cephem derivatives for combating bacterial infections.
摘要翻译：本发明涉及通式II II的1-（2,2-二甲基丙酰氧基）乙基3-头孢烯-4-羧酸酯的两种非对映异构体的结晶酸加成盐，其中X是生理上可接受的单 - 或多碱性，无机或有机酸，并且组= N-OH处于顺式位置，对细菌感染有活性并含有此类头孢烯衍生物的药物制剂，用于制备头孢烯衍生物的方法和使用用于对抗细菌感染的头孢烯衍生物。

8. 发明授权

US5594133A Crystalline acid addition salts of diastereomerically pure 1-(2,2-dimethylpropinonyloxy)-ethyl-3-cephem-4-carboxylate 失效
标题翻译：非对映体纯的1-（2,2-二甲基丙酰氧基） - 乙基-3-头孢烯-4-羧酸的结晶酸加成盐
公开(公告)号：US5594133A
公开(公告)日：1997-01-14
申请号：US447045
申请日：1995-05-22
申请人： Elisabeth Defossa , Gerd Fischer , Joachim-Heiner Jendralla , Rudolf Lattrell , Theodor Wollmann , Dieter Isert
发明人： Elisabeth Defossa , Gerd Fischer , Joachim-Heiner Jendralla , Rudolf Lattrell , Theodor Wollmann , Dieter Isert
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07B57/00 , C07D417/12 , C07D501/00 , C07D501/12 , C07D501/18 , C07D501/32 , C07D501/34 , C07D501/56 , C07D501/54
CPC分类号： C07D501/00
摘要： Crystalline acid addition salts of diastereomerically pure 1-(2,2-dimethylpropionyloxy)ethyl 3-cephem-4-carboxylateThe invention relates to crystalline acid addition salt of the two diastereomers of the 1-(2,2-dimethylpropionyloxy)ethyl 3-cephem-4-carboxylate of the general formula II ##STR1## in which X is the anion of a physiologically acceptable, mono- or polybasic, inorganic or organic acid and the group =N--OH is in the syn-position, pharmaceutical formulations which are active against bacterial infections and contain such cephem derivatives, processes for the preparation of the cephem derivatives and the use of the cephem derivatives for combating bacterial infections.
摘要翻译：非对映异构纯的3-头孢烯-4-羧酸1-（2,2-二甲基丙酰氧基）乙酯的结晶酸加成盐本发明涉及3-（2,2-二甲基丙酰氧基）乙基3-头孢烯-4-羧酸酯的两种非对映异构体的结晶酸加成盐，头孢烯-4-羧酸酯，其中X是生理上可接受的，单或多碱性，无机或有机酸的阴离子，并且基团= N-OH在同一位置，药物制剂其对细菌感染有活性并含有此类头孢烯衍生物，头孢烯衍生物的制备方法和头孢烯衍生物用于抗菌感染的用途。

9. 发明授权

US5405844A Tetracyclic antibiotics and processes for their preparation 失效
标题翻译：四环抗生素及其制备方法
公开(公告)号：US5405844A
公开(公告)日：1995-04-11
申请号：US889350
申请日：1992-05-28
申请人： Uwe Gerlach , Rolf Horlein , Norbert Krass , Rudolf Lattrell , Theo Wollmann , Michael Limbert , Astrid Markus
发明人： Uwe Gerlach , Rolf Horlein , Norbert Krass , Rudolf Lattrell , Theo Wollmann , Michael Limbert , Astrid Markus
IPC分类号： A61K31/40 , A61K31/397 , A61K31/435 , A61P31/04 , C07D471/14 , C07D477/00 , C07D491/14 , C07D491/147 , C07D495/04 , C07D495/14
CPC分类号： C07D477/00 , C07D471/14 , C07D491/14 , C07D495/14
摘要： Tetracyclic antibiotics and processes for their preparation .beta.-Lactam antibiotics of the formula I, and their pharmaceutically tolerable salts ##STR1## where X is (CH.sub.2).sub.0-2, CR(a)R(b), O, SO.sub.0-2 or NR(c),R1, R2 and R3 are a multiplicity of substituents, are outstanding antibiotics with remarkably good antibacterial activity both against gram-positive and against gram-negative microorganisms. They have a high stability to renal dehydropeptidase.They are obtained by cyclization of the compounds II ##STR2## or III ##STR3##
摘要翻译：四环抗生素及其制备方法式I的β-内酰胺抗生素及其药学上可耐受的盐，其中X为（CH 2）0-2，CR（a）R（b），O，SOO 2或 NR（c），R1，R2和R3是多个取代基，是抗革兰氏阳性和革兰氏阴性微生物具有非常好的抗菌活性的杰出抗生素。它们对肾脱水肽酶具有高稳定性。它们通过化合物II II或III III的环化获得

10. 发明授权

US5629288A Lipopeptide derivatives, a process for their preparation and their use 失效
标题翻译：脂肽衍生物，其制备方法及其用途
公开(公告)号：US5629288A
公开(公告)日：1997-05-13
申请号：US411931
申请日：1995-03-28
申请人： Rudolf Lattrell , Theodor Wollmann , Holger Wallmeier , Peter Hammann , Dieter Isert
发明人： Rudolf Lattrell , Theodor Wollmann , Holger Wallmeier , Peter Hammann , Dieter Isert
IPC分类号： A61K38/00 , A61K38/08 , A61K38/12 , A61P31/00 , A61P31/04 , C07K7/06 , C07K7/56 , C07K7/60 , C07K14/195 , C07K14/41
CPC分类号： C07K7/56 , A61K38/00
摘要： Lipopeptide derivatives of the formula I ##STR1## with R.sup.1 equal to OH or NH.sub.2 and R.sup.2 a C.sub.8 -C.sub.22 -acyl radical, pharmaceutical products which are effective for bacterial infections and contain such lipopeptide derivatives, process for preparing the lipopeptide derivatives and the pharmaceutical products, and the use of the lipopeptide derivatives for controlling bacterial infections are described.
摘要翻译：式I的脂肽衍生物，其中R1等于OH或NH2，R2为C8-C22-酰基，对细菌感染有效并含有这种脂肽衍生物的药物产品，制备脂肽衍生物的方法和药物描述了用于控制细菌感染的脂肽衍生物的用途。

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