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1. 发明授权

US5055572A Cephalosporin derivatives 失效
标题翻译： CEPHALOSPORIN衍生物
公开(公告)号：US5055572A
公开(公告)日：1991-10-08
申请号：US179199
申请日：1988-04-08
申请人： Andre Furlenmeier , Erwin Gotschi , Paul Hebeisen , Werner Hofheinz , Helmut Link
发明人： Andre Furlenmeier , Erwin Gotschi , Paul Hebeisen , Werner Hofheinz , Helmut Link
IPC分类号： C07D519/06 , A61K31/545 , A61P31/04 , C07D501/36 , C07D501/46 , C07D519/00
CPC分类号： C07D501/36 , C07D519/00 , Y02P20/55
摘要： Acyl derivatives of the formula ##STR1## in which R is an acyl group, excluding those acyl groups of the formula ##STR2## in which A is a group of the formulae --NHCO--, --NHCONHCO--, --NHCOCH.dbd.CH--, ##STR3## wherein R.sup.6 is hydrogen or lower alkyl; R.sup.1 and R.sup.2 are hydrogen or a protecting group, X is hydrogen, halogen, lower alkoxy, nitro or --OR.sup.2, n is 1 or 2, R.sup.4 and R.sup.5 are hydrogen or together represent an additional bond and Z is a direct bond or carbonyl (where R.sup.4 and R.sup.5 both represent hydrogen) or a group of the formula --O--B-- (where R.sup.4 and R.sup.5 together represent an additional bond) in which B is a straight-chain, branched or cyclic lower alkylene;and wherein R.sup.3 is a substituted bicyclic group of the formulae ##STR4## wherein R.sup.7 and R.sup.8 are independently hydrogen, lower alkyl or trifluoromethyl or, in formulae (a), (b), (e) and (f) together represent alkylene with 3 or 4 carbon atoms, and R', R" and R"' are independently hydrogen, lower alkyl or lower cycloalkyl; wherein compounds of formula I in which R.sup.4 and R.sup.5 together represent an additional bond are present in the syn-isomeric form or as a mixture with the anti-isomeric form in which the syn-isomeric form predominates,as well as readily hydrolyzable esters and salts of these compounds and hydrates of the compounds of formula I or of their esters and salts.These compounds are useful as antibiotics.
摘要翻译：除了那些其中A是式-NHCO-，-NHCONHCO-，-NHCOCH = CH-的基团的式“IMAGE”的酰基之外，其中R是酰基的式Ⅰ的酰基衍生物，其中R6是氢或低级烷基; R1和R2是氢或保护基，X是氢，卤素，低级烷氧基，硝基或-OR2，n是1或2，R4和R5是氢或一起代表另外的键，Z是直接键或羰基（其中R4和R5都表示氢）或式-BB-（其中R4和R5一起代表附加键）的基团，其中B是直链，支链或环状低级亚烷基; 并且其中R 3是下式的取代的双环基团：其中R 7和R 8独立地是氢，低级烷基或三氟甲基，或者在式（a），（b）中，），（e）和（f）共同表示具有3或4个碳原子的亚烷基，R'，R“和R”'独立地是氢，低级烷基或低级环烷基; 其中R 4和R 5一起代表另外的键的式Ⅰ化合物以顺式异构形式存在，或作为其中顺式异构体形式占优势的抗异构体形式的混合物以及容易水解的酯和盐的这些化合物和式I化合物的水合物或它们的酯和盐。这些化合物可用作抗生素。

2. 发明授权

US5438052A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5438052A
公开(公告)日：1995-08-01
申请号：US979519
申请日：1992-11-20
申请人： Peter Angehrn , Andre Furlenmeier , Paul Hebeisen , Werner Hofheinz , Helmut Link
发明人： Peter Angehrn , Andre Furlenmeier , Paul Hebeisen , Werner Hofheinz , Helmut Link
IPC分类号： A61K31/545 , A61K20060101 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/00 , C07D501/18 , C07D501/20 , C07D501/34 , C07D501/36 , C07D519/06
CPC分类号： C07D501/00
摘要： Cephalosporin derivatives have the formula ##STR1## wherein Z.sup.1, Z.sup.2, X, Y, P, Q, m, n and p are as defined in the following text. Also described are the readily hydrolyzable esters and pharmaceutically compatible salts of these compounds, and hydrates of compounds of formula I, their esters and salts. Processes are provided for manufacture and pharmaceutical preparations which contain these compounds. Intermediates from the manufacture of these compounds are described, as is the use of the compounds in the control of illnesses and for the manufacture of the aforementioned preparations.
摘要翻译：头孢菌素衍生物具有下式的定义：其中Z1，Z2，X，Y，P，Q，m，n和p如下文所定义。还描述了这些化合物的易水解的酯和药学上相容的盐，以及式I化合物及其酯和盐的水合物。提供了含有这些化合物的制造方法和药物制剂。描述了这些化合物的制造中的中间体，以及化合物在控制疾病和制备上述制剂中的用途。

3. 发明授权

US5486466A Process for the preparation of DNA gyrase inhibitors 失效
标题翻译： DNA促旋酶抑制剂的制备方法
公开(公告)号：US5486466A
公开(公告)日：1996-01-23
申请号：US339442
申请日：1994-11-14
申请人： Mikio Arisawa , Erwin Gotschi , Paul Hebeisen , Tsutomu Kamiyama , Helmut Link , Raffaello Masciadri , Hisao Shimada , Junko Watanabe
发明人： Mikio Arisawa , Erwin Gotschi , Paul Hebeisen , Tsutomu Kamiyama , Helmut Link , Raffaello Masciadri , Hisao Shimada , Junko Watanabe
IPC分类号： A61K31/395 , A61K31/42 , A61K31/425 , A61K38/00 , A61P31/04 , C07C317/24 , C07C317/28 , C07C317/46 , C07C317/48 , C07C323/56 , C07C323/58 , C07C323/64 , C07D291/08 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D419/04 , C07D419/12 , C07K5/02 , C07K5/078 , C07K5/097 , C07K5/103 , C07K7/06 , C12P13/04 , C12N1/20
CPC分类号： C07D419/04 , C07D291/08 , C07K5/0202 , C07K5/06139 , C07K5/0821 , C07K5/1008 , C07K7/06 , A61K38/00 , Y10S435/886
摘要： Bicyclic derivatives of the general formula ##STR1## wherein X.sup.1 is --S-- or --SO--;X.sup.2 is --CO-- or --CS--;R.sup.1 is hydrogen, halogen or lower alkyl optionally substituted by halogen or lower alkoxy;R.sup.2 and R.sup.3 are each independently hydrogen, lower alkyl, halogen, amino, lower alkylamino, di-lower alkylamino, acylamino, lower alkexy, lower alkoxymethoxy or a group OR.sup.4 ;R.sup.4 is hydrogen or an easily hydrolyzable group;R.sup.5 is hydrogen, optionally esterified carboxy or amidated (thio)carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted acyl or heterocyclyl;R.sup.6 and R.sup.7a are each independently hydrogen or lower alkyl;R.sup.7b is hydrogen, optionally substituted hydroxy, --NR--A or --N.dbd.B, in which R is hydrogen or lower alkyl, A is hydrogen, optionally substituted alkyl, lower cycloalkyl, iminoyl, (thio)acyl, esterified carboxy or amidated (thio)carboxy and B is lower alkylidene;R.sup.7a and R.sup.7b together represent oxo, lower alkoxycarbonylmethylidene or optionally substituted hydroxyimino; andR.sup.8 is hydrogen, optionally substituted alkyl, optionally esterified carboxy or amidated (thio)carboxy; provided that no more than two of R.sup.1 -R.sup.3 are nitrogen-containing groups; no more than two of R.sup.1 -R.sup.3 are oxygen containing groups and no more than two of R.sup.1 -R.sup.3 are either nitrogen containing or oxygen containing groups;and pharmaceutically acceptable salts of the compounds of formula I carrying an acidic and/or basic substituent.The products are antimicrobially active.
摘要翻译：通式为其中X 1为-S-或-SO-的通式为其的双环衍生物; X2是-CO-或-CS-; R 1为氢，卤素或任选被卤素或低级烷氧基取代的低级烷基; R2和R3各自独立地为氢，低级烷基，卤素，氨基，低级烷基氨基，二低级烷基氨基，酰氨基，低级烷基，低级烷氧基甲氧基或基团OR4; R4是氢或易水解基团; R 5为氢，任选酯化的羧基或酰胺基（硫代）羧基，任选取代的烷基，任选取代的烯基，任选取代的酰基或杂环基; R6和R7a各自独立地为氢或低级烷基; R7b是氢，任选取代的羟基，-NR-A或-N = B，其中R是氢或低级烷基，A是氢，任选取代的烷基，低级环烷基，亚氨酰基，（硫代）酰基，酯化的羧基或酰胺基（硫代）羧基，B是低级亚烷基; R7a和R7b一起代表氧代，低级烷氧基羰基亚甲基或任选取代的羟基亚氨基; 和R 8是氢，任选取代的烷基，任选酯化的羧基或酰胺基（硫代）羧基; 条件是R1-R3中不超过两个为含氮基团; R1-R3中不超过两个为含氧基团，R1-R3中不超过两个为含氮基团或含氧基团; 和具有酸性和/或碱性取代基的式I化合物的药学上可接受的盐。该产品具有抗微生物活性。

4. 发明授权

US5665746A Mono- and bicyclic DNA gyrase inhibitors 失效
标题翻译：单环和双环DNA促旋酶抑制剂
公开(公告)号：US5665746A
公开(公告)日：1997-09-09
申请号：US540678
申请日：1995-10-11
申请人： Jurgen Geiwiz , Erwin Gotschi , Paul Hebeisen , Helmut Link , Thomas Lubbers
发明人： Jurgen Geiwiz , Erwin Gotschi , Paul Hebeisen , Helmut Link , Thomas Lubbers
IPC分类号： A61K31/395 , A61K31/40 , A61K31/41 , A61K31/4245 , A61K31/425 , A61K31/44 , A61K31/535 , A61K31/5377 , A61P31/04 , C07D271/06 , C07D291/08 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D419/04 , C07D419/12 , C07D521/00 , C07F7/18
CPC分类号： C07D271/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D291/08 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D419/04 , C07D419/12 , C07F7/1856
摘要： The present invention relates to a compound of the formula ##STR1## wherein X.sup.1, R.sup.1, R.sup.2, OP, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.0 are as described herein, and their pharmaceutically acceptable salts thereof carrying an acidic andr basic substituent.The compound of formula I as well as their pharmaceutically acceptable salts inhibit DNA gyrase activity in bacteria and possess antibiotic, especially antibacterial activity against microorganisms and can be used in the control or prevention of infectious diseases.
摘要翻译：本发明涉及下式的化合物，其中X1，R1，R2，OP，R3，R4，R5，R6和R0如本文所述，及其药学上可接受的盐携带酸性和/或碱性取代基。式I化合物及其药学上可接受的盐抑制细菌中的DNA促旋酶活性，并且具有抗生素，特别是对微生物的抗菌活性，并且可用于控制或预防感染性疾病。

5. 发明授权

US5294609A DNA gyrase inhibitors and pharmaceutical preparations therefor 失效
标题翻译： DNA促旋酶抑制剂及其药物制剂
公开(公告)号：US5294609A
公开(公告)日：1994-03-15
申请号：US952537
申请日：1992-12-09
申请人： Mikio Arisawa , Erwin Gotschi , Paul Hebeisen , Tsutomu Kamiyama , Helmut Link , Raffaello Masciadri , Hisao Shimada , Junko Watanabe
发明人： Mikio Arisawa , Erwin Gotschi , Paul Hebeisen , Tsutomu Kamiyama , Helmut Link , Raffaello Masciadri , Hisao Shimada , Junko Watanabe
IPC分类号： A61K31/395 , A61K31/42 , A61K31/425 , A61K38/00 , A61P31/04 , C07C317/24 , C07C317/28 , C07C317/46 , C07C317/48 , C07C323/56 , C07C323/58 , C07C323/64 , C07D291/08 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D419/04 , C07D419/12 , C07K5/02 , C07K5/078 , C07K5/097 , C07K5/103 , C07K7/06
CPC分类号： C07D419/04 , C07D291/08 , C07K5/0202 , C07K5/06139 , C07K5/0821 , C07K5/1008 , C07K7/06 , A61K38/00 , Y10S435/886
摘要： Bicyclic derivatives of the formula ##STR1## wherein X.sup.1, X.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7a, R.sup.7b, and R.sup.8 are as defined in the specification. These compounds are antimicrobially active.
摘要翻译： PCT No.PCT / EP92 / 00809 Sec。 371日期：1992年12月9日 102（e）日期1992年12月9日PCT提交1992年4月9日PCT公布。公开号WO92 / 18490 日期：1992年10月29日。式（*化学结构*）I的双环衍生物其中X1，X2，R1，R2，R3，R4，R5，R6，R7a，R7b和R8如本说明书中所定义。这些化合物是抗微生物活性的。

6. 发明授权

US5399741A DNA gyrase inhibitors, process for their manufacture and pharmaceutical preparations containing same 失效
标题翻译： DNA促旋酶抑制剂，其制备方法和含有它们的药物制剂
公开(公告)号：US5399741A
公开(公告)日：1995-03-21
申请号：US177483
申请日：1994-01-06
申请人： Mikio Arisawa , Erwin Gotschi , Paulfaello Hebeisen , Tsutomu Kamiyama , Helmut Link , Raffaello Masciadri , Hisao Shimada , Junko Watanabe
发明人： Mikio Arisawa , Erwin Gotschi , Paulfaello Hebeisen , Tsutomu Kamiyama , Helmut Link , Raffaello Masciadri , Hisao Shimada , Junko Watanabe
IPC分类号： A61K31/395 , A61K31/42 , A61K31/425 , A61K38/00 , A61P31/04 , C07C317/24 , C07C317/28 , C07C317/46 , C07C317/48 , C07C323/56 , C07C323/58 , C07C323/64 , C07D291/08 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D419/04 , C07D419/12 , C07K5/02 , C07K5/078 , C07K5/097 , C07K5/103 , C07K7/06 , C07F7/04
CPC分类号： C07D419/04 , C07D291/08 , C07K5/0202 , C07K5/06139 , C07K5/0821 , C07K5/1008 , C07K7/06 , A61K38/00 , Y10S435/886
摘要： Compounds of the formula ##STR1## in which P is hydroxy and T is the group -X.sup.2 -CR.sup.7a R.sup.7b -CHR.sup.8 -OH or T is hydrogen and P is the group O-CHR.sup.8 -CR.sup.7a R.sup.7b -X.sup.2 -OH and, wherein X.sup.1, X.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7a, R.sup.7b, and R.sup.8 are as defined in the specification,or a reactive derivative thereof. These compounds are useful in the preparation of DNA gyrase inhibitors.
摘要翻译：其中P是羟基并且T是基团-X2-CR7aR7b-CHR8-OH或T的式Ⅱ化合物是氢，P是O-CHR8-CR7aR7b-X2-OH基团，其中X1，X2 ，R1，R2，R3，R4，R5，R6，R7a，R7b和R8如说明书中所定义，或其活性衍生物。这些化合物可用于制备DNA促旋转录酶抑制剂。

7. 发明授权

US5594135A Tricyclic DNA gyrase inhibitors 失效
标题翻译：三环DNA促旋酶抑制剂
公开(公告)号：US5594135A
公开(公告)日：1997-01-14
申请号：US541077
申请日：1995-10-11
申请人： J urgen Geiwiz , Erwin G otschi , Paul Hebeisen , Helmut Link , Thomas L ubbers
发明人： J urgen Geiwiz , Erwin G otschi , Paul Hebeisen , Helmut Link , Thomas L ubbers
IPC分类号： A61K31/395 , A61K31/40 , A61K31/41 , A61K31/4245 , A61K31/425 , A61K31/44 , A61K31/535 , A61K31/5377 , A61P31/04 , C07D271/06 , C07D291/08 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D419/04 , C07D419/12 , C07D521/00 , C07F7/18 , C07D515/08 , C07D515/18
CPC分类号： C07D271/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D291/08 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D419/04 , C07D419/12 , C07F7/1856
摘要： The present invention relates to a compound of the formula ##STR1## wherein X.sup.1, R.sup.1, R.sup.2, OP, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.0 are as described herein, and their pharmaceutically acceptable salts thereof carrying an acidic and/or basic substituent.The compound of formula I as well as their pharmaceutically acceptable salts inhibit DNA gyrase activity in bacteria and possess antibiotic, especially antibacterial activity against microorganisms and can be used in the control or prevention of infectious diseases.
摘要翻译：本发明涉及下式的化合物，其中X1，R1，R2，OP，R3，R4，R5，R6和R0如本文所述，及其药学上可接受的盐携带酸性和/或碱性取代基。式I化合物及其药学上可接受的盐抑制细菌中的DNA促旋酶活性，并且具有抗生素，特别是对微生物的抗菌活性，并且可用于控制或预防感染性疾病。

8. 发明授权

US5589473A Mono- and bicyclic DNA gyrase inhibitors 失效
标题翻译：单环和双环DNA促旋酶抑制剂
公开(公告)号：US5589473A
公开(公告)日：1996-12-31
申请号：US407730
申请日：1995-03-20
申请人： J urgen Geiwiz , Erwin G otschi , Paul Hebeisen , Helmut Link , Thomas L ubbers
发明人： J urgen Geiwiz , Erwin G otschi , Paul Hebeisen , Helmut Link , Thomas L ubbers
IPC分类号： A61K31/395 , A61K31/40 , A61K31/41 , A61K31/4245 , A61K31/425 , A61K31/44 , A61K31/535 , A61K31/5377 , A61P31/04 , C07D271/06 , C07D291/08 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D419/04 , C07D419/12 , C07D521/00 , C07F7/18
CPC分类号： C07D271/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D291/08 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D419/04 , C07D419/12 , C07F7/1856
摘要： The present invention relates to a compound of the formula ##STR1## wherein X.sup.1, R.sup.1, R.sup.2, OP, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.0 are as described herein, and their pharmaceutically acceptable salts thereof carrying an acidic and/or basic substituent.The compound of formula I as well as their pharmaceutically acceptable salts inhibit DNA gyrase activity in bacteria and possess antibiotic, especially antibacterial activity against microorganisms and can be used in the control or prevention of infectious diseases.
摘要翻译：本发明涉及下式的化合物，其中X1，R1，R2，OP，R3，R4，R5，R6和R0如本文所述，及其药学上可接受的盐携带酸性和/或碱性取代基。式I化合物及其药学上可接受的盐抑制细菌中的DNA促旋酶活性，并且具有抗生素，特别是对微生物的抗菌活性，并且可用于控制或预防感染性疾病。

9. 发明授权

US4831151A Antimicrobial imidazolium derivatives 失效
标题翻译：抗菌咪唑衍生物
公开(公告)号：US4831151A
公开(公告)日：1989-05-16
申请号：US853831
申请日：1986-04-21
申请人： Helmut Link , Marc Montavon , Eva M. Karpitschka , Wilhelm Klotzer , Renate Mussner
发明人： Helmut Link , Marc Montavon , Eva M. Karpitschka , Wilhelm Klotzer , Renate Mussner
IPC分类号： C07D233/54 , C07D233/56 , C07D521/00
CPC分类号： C07D233/54 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Compounds of the formula ##STR1## wherein the various substituents are defined hereinbelow and the pharmaceutically acceptable acid addition salts thereof, possess pharmacological properties. In particular, they possess antibacterial, antimycotic, protozoacidal and/or anthelmintic properties.
摘要翻译：下文定义的各种取代基及其药学上可接受的酸加成盐的式IMA化合物具有药理学性质。特别地，它们具有抗菌，抗真菌，原生动物和/或驱虫性质。

10. 发明授权

US4407814A Imidazolidine derivatives 失效
标题翻译：咪唑烷衍生物
公开(公告)号：US4407814A
公开(公告)日：1983-10-04
申请号：US330364
申请日：1981-12-14
申请人： Karl Bernauer , Helmut Link , Harro Stohler
发明人： Karl Bernauer , Helmut Link , Harro Stohler
IPC分类号： A61K31/415 , A61K31/4166 , A61P5/00 , A61P33/10 , C07D233/66 , C07D233/72 , C07D233/74 , C07D233/88
CPC分类号： C07D233/88 , C07D233/72
摘要： Imidazolidine derivatives of the formula ##STR1## wherein X is oxygen or imino and R is one of the groups ##STR2## their preparation, use as antiandrogenically or schistosomicidally active agents, and corresponding pharmaceutical preparations, are described.
摘要翻译：描述了其中X是氧或亚氨基并且R是其中之一的组合物，其用作抗雄激素或血吸虫病活性剂以及相应的药物制剂的式Ⅰ的咪唑烷衍生物。

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