公开(公告)号：US5556850A

公开(公告)日：1996-09-17

申请号：US447635

申请日：1995-05-23

Applicant: Elisabeth Defossa ,  Gerd Fischer ,  Joachim-Heiner Jendralla ,  Rudolf Lattrell ,  Theodor Wollmann ,  Dieter Isert

Inventor： Elisabeth Defossa ,  Gerd Fischer ,  Joachim-Heiner Jendralla ,  Rudolf Lattrell ,  Theodor Wollmann ,  Dieter Isert

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07B57/00 ,  C07D417/12 ,  C07D501/00 ,  C07D501/12 ,  C07D501/18 ,  C07D501/32 ,  C07D501/34

CPC classification number: C07D501/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5409918A

公开(公告)日：1995-04-25

申请号：US931505

申请日：1992-08-21

Applicant: Friedhelm Adam ,  Walter Durckheimer ,  Burkhard Mencke ,  Dieter Isert

Inventor： Friedhelm Adam ,  Walter Durckheimer ,  Burkhard Mencke ,  Dieter Isert

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/34 ,  C07D501/56 ,  C07D501/32

CPC classification number: C07D501/00

Abstract: Crystalline cephem acid addition salts of the general formula II ##STR1## pharmaceutical preparations effective against bacterial infections which contain such cephem derivatives, processes for the preparation of the cephem derivatives and the pharmaceutical preparations, and the use of the cephem derivatives for combating bacterial infections.

Abstract translation: 具有通式II的结晶头孢酸加成盐对于含有此类头孢烯衍生物的细菌感染药物制剂，制备头孢烯衍生物和药物制剂的方法，以及使用头孢烯 防治细菌感染的衍生物。

公开(公告)号：US5091382A

公开(公告)日：1992-02-25

申请号：US552058

申请日：1990-07-13

Applicant: Friedhelm Adam ,  Walter Durckheimer ,  Karl-Heinz Scheunemann ,  Dieter Isert ,  Gerhard Seibert

Inventor： Friedhelm Adam ,  Walter Durckheimer ,  Karl-Heinz Scheunemann ,  Dieter Isert ,  Gerhard Seibert

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D277/36 ,  C07D277/56 ,  C07D501/00 ,  C07D501/36

CPC classification number: C07D277/56 ,  C07D277/36 ,  C07D501/00

Abstract: Cephalosporin derivatives of the general formula ##STR1## pharmaceutical preparations active against bacterial infections which contain such cephalosporin derivatives, processes for the preparation of the cephalosporin derivatives, use of the cephalosporin derivatives for the preparation of a pharmaceutical for combating bacterial infections, and starting products for the preparation of cephalosporin derivatives.

Abstract translation: 具有通式的头孢菌素衍生物，其含有这种头孢菌素衍生物的细菌感染活性的药物制剂，头孢菌素衍生物的制备方法，头孢菌素衍生物用于制备抗菌细菌感染药物，以及起始产品 头孢菌素衍生物的制备。

公开(公告)号：US5994307A

公开(公告)日：1999-11-30

申请号：US203388

申请日：1998-12-02

Applicant: Laszlo Vertesy ,  Martin Knauf ,  Joachim Wink ,  Dieter Isert ,  Wilhelm Stahl ,  Gunther Riess ,  Jozsef Aszodi ,  Dominique Le Beller

Inventor： Laszlo Vertesy ,  Martin Knauf ,  Joachim Wink ,  Dieter Isert ,  Wilhelm Stahl ,  Gunther Riess ,  Jozsef Aszodi ,  Dominique Le Beller

IPC: C12P1/06 ,  A61K38/00 ,  A61P31/00 ,  C07K7/08 ,  C12N1/20 ,  C12P21/02 ,  C12R1/465 ,  C12R1/645 ,  A61K38/02 ,  C07K5/00 ,  C07K7/00

CPC classification number: C07K7/08 ,  C12R1/465 ,  A61K38/00

Abstract: This invention relates to the antibiotic feglymycin, as well as processes for its preparation and use. Feglymycin is represented by the structural formula (SEQ. ID. NO. 1) ##STR1##

Abstract translation: 本发明涉及抗生素feglymycin，以及其制备和应用的方法。 铁氰霉素由结构式（SEQ ID NO：1）表示，

公开(公告)号：US5306717A

公开(公告)日：1994-04-26

申请号：US924598

申请日：1992-07-24

Applicant: Friedhelm Adam ,  Walter Durckheimer ,  Gerd Fischer ,  Burkhard Mencke ,  Gerhard Seibert ,  Dieter Isert ,  Norbert Klesel

Inventor： Friedhelm Adam ,  Walter Durckheimer ,  Gerd Fischer ,  Burkhard Mencke ,  Gerhard Seibert ,  Dieter Isert ,  Norbert Klesel

IPC: A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/22 ,  C07D501/34 ,  C07D501/46

CPC classification number: C07D501/34

Abstract: Cephalosporin derivatives of the general formula ##STR1## pharmaceutical preparations which are active against bacterial infections and contain such cephem derivatives, processes for the preparation of the cephem derivatives and the pharmaceutical preparations and the use of the cephem derivatives for combating bacterial infections.

Abstract translation: 具有抗细菌感染和含有此类头孢烯衍生物的通式为“IMAGE”+ TR 的药物制剂的头孢菌素衍生物，头孢烯衍生物和药物制剂的制备方法以及头孢烯衍生物用于对抗细菌 感染。

公开(公告)号：US5891851A

公开(公告)日：1999-04-06

申请号：US988552

申请日：1997-12-11

Applicant: Laszlo Vertesy ,  Martin Knauf ,  Joachim Wink ,  Dieter Isert ,  Wilhelm Stahl ,  Gunther Riess ,  Jozsef Aszodi ,  Dominique Le Beller

Inventor： Laszlo Vertesy ,  Martin Knauf ,  Joachim Wink ,  Dieter Isert ,  Wilhelm Stahl ,  Gunther Riess ,  Jozsef Aszodi ,  Dominique Le Beller

IPC: C12P1/06 ,  A61K38/00 ,  A61P31/00 ,  C07K7/08 ,  C12N1/20 ,  C12P21/02 ,  C12R1/465 ,  C12R1/645 ,  A61K38/02 ,  C07K5/00 ,  C07K7/00

CPC classification number: C07K7/08 ,  C12R1/465 ,  A61K38/00

Abstract: This invention relates to the antibiotic feglymycin, as well as processes for its preparation and use. Feglymycin is represented by the structural formula (SEQ ID NO:1): ##STR1##

Abstract translation: 本发明涉及抗生素feglymycin，以及其制备和应用的方法。 Feglymycin由结构式（SEQ ID NO：1）表示： + TR

公开(公告)号：US5100887A

公开(公告)日：1992-03-31

申请号：US555807

申请日：1990-07-23

Applicant: Friedhelm Adam ,  Jurgen Blumbach ,  Walter Durckheimer ,  Gerd Fischer ,  Burghard Mencke ,  Dieter Isert ,  Gerhard Seibert

Inventor： Friedhelm Adam ,  Jurgen Blumbach ,  Walter Durckheimer ,  Gerd Fischer ,  Burghard Mencke ,  Dieter Isert ,  Gerhard Seibert

IPC: A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/32 ,  C07D501/34

CPC classification number: C07D501/34 ,  C07D501/00

Abstract: Cephemcarboxylic acid esters of the general formula ##STR1## pharmaceutical preparations which are active against bacterial infections, which contain such cephem derivatives, a process for the preparation of the cephem derivatives and the pharmaceutical preparations, and also the use of the cephem derivatives for combating bacterial infections.

Abstract translation: 具有抗细菌感染活性的含有此类头孢烯衍生物的通式 + TR 药物制剂的头孢霉羧酸酯，制备头孢烯衍生物和药物制剂的方法，以及使用 头孢烯衍生物用于对抗细菌感染。

公开(公告)号：US5550232A

公开(公告)日：1996-08-27

申请号：US447229

申请日：1995-05-22

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

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

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

CPC classification number: C07D501/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5629288A

公开(公告)日：1997-05-13

申请号：US411931

申请日：1995-03-28

Applicant: Rudolf Lattrell ,  Theodor Wollmann ,  Holger Wallmeier ,  Peter Hammann ,  Dieter Isert

Inventor： Rudolf Lattrell ,  Theodor Wollmann ,  Holger Wallmeier ,  Peter Hammann ,  Dieter Isert

IPC: A61K38/00 ,  A61K38/08 ,  A61K38/12 ,  A61P31/00 ,  A61P31/04 ,  C07K7/06 ,  C07K7/56 ,  C07K7/60 ,  C07K14/195 ,  C07K14/41

CPC classification number: C07K7/56 ,  A61K38/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5614623A

公开(公告)日：1997-03-25

申请号：US447249

申请日：1995-05-22

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

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

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

CPC classification number: C07D501/00

Abstract: 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.

Abstract translation: 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。