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1. 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

2. 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。

3. 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。

4. 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。

5. 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。

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

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

8. 发明授权

US06632838B1 Use of bissulfonamides for producing medicines for the treatment of hyperlipidemia 有权
标题翻译：使用双磺酰胺生产用于治疗高脂血症的药物
公开(公告)号：US06632838B1
公开(公告)日：2003-10-14
申请号：US09653253
申请日：2000-08-31
申请人： Reinhard Kirsch , Hans-Ludwig Schaefer , Eugen Falk , Norbert Krass
发明人： Reinhard Kirsch , Hans-Ludwig Schaefer , Eugen Falk , Norbert Krass
IPC分类号： A61K3118
CPC分类号： A61K31/635 , A61K31/18 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/5377
摘要： The use of bissulfonamides for producing medicines for the treatment of hyperlipidemia. The invention relates to the use of bissulfonamides and their salts for producing medicines for the treatment of hyperlipidemia. The use of compounds of formula I in which the radicals have the stated meanings, and of their salts for producing a medicine for the treatment of hyperlipidemia is described.
摘要翻译：使用双磺酰胺生产用于治疗高脂血症的药物。本发明涉及双磺酰胺及其盐用于制备用于治疗高脂血症的药物的用途。使用式Iin化合物，其中描述了具有所述含义的自由基及其用于制备治疗高脂血症药物的盐。

9. 发明授权

US5939424A Compounds for treating disorders of lipid metabolism and their preparation 失效
标题翻译：用于治疗脂质代谢紊乱及其制备的化合物
公开(公告)号：US5939424A
公开(公告)日：1999-08-17
申请号：US868991
申请日：1997-06-04
申请人： Hans Georg Boger , Axel Hoffmann , Gerhard Jahne , Norbert Krass , Hans-Ludwig Schafer
发明人： Hans Georg Boger , Axel Hoffmann , Gerhard Jahne , Norbert Krass , Hans-Ludwig Schafer
IPC分类号： A61K31/505 , A61P3/06 , C07D403/04
CPC分类号： C07D403/04
摘要： The invention relates to 4-Amino-2-ureidopyrimidine-5-carboxamides of the formula I ##STR1## in which R.sup.1 is H or (C.sub.1 -C.sub.8)-alkyl, where one or more H can be replaced by F; R.sup.2 is selected from the group consisting of F, Cl, Br, H, -O-(C.sub.1 -C.sub.8)-alkyl, and -S-(C.sub.1 -C.sub.8)-alkyl, where the alkyl groups have one or more H replaced by F; R.sup.3 is -O-(C.sub.1 -C.sub.8)-alkyl or -S-(C.sub.1 -C.sub.8)-alkyl, where the alkyl groups have one or more H replaced by F; or R.sup.2 and R.sup.3 together form -O-(C.sub.1 -C.sub.5)-alkylene-O-, where the alkylene portion has one or more H replaced by F; and their physiologically tolerable salts. The invention further provides processes for preparing the compounds of formula I. The compounds are suitable for the treatment of disorders of lipid metabolism.
摘要翻译：本发明涉及式I的4-氨基-2-脲基嘧啶-5-甲酰胺，其中R 1为H或（C 1 -C 8） - 烷基，其中一个或多个H可被F取代; R 2选自F，Cl，Br，H，-O-（C 1 -C 8） - 烷基和-S-（C 1 -C 8） - 烷基，其中烷基具有一个或多个H被 F; R 3是-O-（C 1 -C 8） - 烷基或-S-（C 1 -C 8） - 烷基，其中烷基具有一个或多个H被F取代; 或R 2和R 3一起形成-O-（C 1 -C 5） - 亚烷基-O-，其中亚烷基部分具有一个或多个H被F取代; 及其生理上可耐受的盐。本发明还提供了制备式I化合物的方法。该化合物适用于治疗脂质代谢紊乱。

10. 发明授权

US5773447A Compounds for treating disorders of lipid metabolism and their preparation 失效
标题翻译：用于治疗脂质代谢紊乱及其制备的化合物
公开(公告)号：US5773447A
公开(公告)日：1998-06-30
申请号：US874255
申请日：1997-06-13
申请人： Gerhard Rackur , Hans Georg Boger , Norbert Krass , Axel Hoffmann , Michael Leineweber
发明人： Gerhard Rackur , Hans Georg Boger , Norbert Krass , Axel Hoffmann , Michael Leineweber
IPC分类号： A61K31/505 , A61P3/06 , C07D403/04 , C07D403/14 , C07D239/02
CPC分类号： C07D403/04 , C07D403/14
摘要： The present invention relates to tertiary 4-amino-2-ureidopyrimidine-5-carboxamides of formula I: ##STR1## in which R.sup.1 is (C.sub.1 -C.sub.8)-alkyl wherein one or more H are replaced by F; R.sup.2 is selected from the group consisting of F, Cl, Br, H, --O--(C.sub.1 -C.sub.8)-alkyl and (C.sub.1 -C.sub.8)-alkyl, wherein one or more of the H of the alkyls can be replaced by F; R.sup.3 is selected from the group consisting of F, Cl, Br, H, --O--(C.sub.1 -C.sub.4)-alkyl and (C.sub.1 -C.sub.4)-alkyl, wherein one or more of the H of the alkyl can be replaced by F; R.sup.4 is CF.sub.3 or OCF.sub.3 ; and their physiologically tolerable salts. Process for preparing the compounds of formula I are also described. The compounds are suitable for the treatment of disorders of lipid metabolism.
摘要翻译：本发明涉及式I的叔-4-氨基-2-脲基嘧啶-5-甲酰胺：一个或多个H被F取代; R 2选自F，Cl，Br，H，-O-（C 1 -C 8） - 烷基和（C 1 -C 8） - 烷基，其中烷基的H中的一个或多个可以被F ; R 3选自F，Cl，Br，H，-O-（C 1 -C 4） - 烷基和（C 1 -C 4） - 烷基，其中烷基的H中的一个或多个可以被F ; R4是CF3或OCF3; 及其生理上可耐受的盐。还描述了制备式I化合物的方法。该化合物适用于治疗脂质代谢紊乱。

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