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1. 发明申请

WO1996001829A1 PYRIDO[3,2,1-i,j][3,1]BENZOXAZINE DERIVATIVES 审中-公开
标题翻译：吡啶并[3,2,1-I，J] [3,1]苯并恶嗪
公开(公告)号：WO1996001829A1
公开(公告)日：1996-01-25
申请号：PCT/EP1995002510
申请日：1995-06-28
申请人： BAYER AKTIENGESELLSCHAFT , HALLENBACH, Werner , HIMMLER, Thomas , JAETSCH, Thomas , MIELKE, Burkhard , BREMM, Klaus, Dieter , ENDERMANN, Rainer , PIRRO, Franz , STEGEMANN, Michael , WETZSTEIN, Heinz-Georg
发明人： BAYER AKTIENGESELLSCHAFT
IPC分类号： C07D498/06
CPC分类号： C07D498/06 , C07C17/16 , C07D519/00 , C07C21/19
摘要： The present invention relates to novel pyrido[3,2,1-i,j][3,1]benzoxazine derivatives of the formula (I) in which R is hydrogen or C1-C4 alkyl possibly substituted by hydroxy or halogen; R is hydrogen or methyl independently of R ; R is hydrogen or C1-C4 alkyl; R is hydrogen or methyl; R is hydrogen, alkyl with 1 to 4 carbon atoms, possibly substituted by hydroxy, methoxy, amino, methyl amino or dimethyl amino or (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl; X is hydrogen or halogen; Z is radicals of the structures ((a), (b), (c)) in which R is hydrogen, hydroxy, -NR R , hydroxy methyl or -CH2-NR R , carboxyl, methoxy carbonyl or ethoxy carbonyl, where R is hydrogen, possibly hydroxy-substituted C1-C3 alkyl, alkoxy carbonyl with 1 to 4 C atoms in the alkoxy part or C1-C3-acyl, and R is hydrogen or methyl; R is hydrogen, straight or branched chained C1-C3 alkyl or cyclopropyl; R is hydrogen or methyl; R is hydrogen or methyl; R is hydrogen, methyl or radicals of the structures -CH=CH-CO2R , -CH2-CH2-CO2R , -CH2-CO-CH3, -CH2-CH2-CN; R is methyl or ethyl; and B is -CH2-, O or a direct bond, their production and use for the therapy or the prevention of bacterial infections.
摘要翻译：本发明涉及新的吡啶并[3,2,1-I，J] [3,1]式（I），其中R <1>代表氢或任选经羟基或卤素取代的C1-C4烷基的苯并恶嗪衍生物，R <2>是，独立于R <1>表示氢或甲基，R <3>是氢或C1-C4烷基，R <3“>是氢或甲基，R <4>是氢，任选被羟基，甲氧基，氨基，甲氨基或二甲氨基，具有1至4个碳原子或（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基） - 甲基烷基取代的，X <1>是氢或卤素 ; Z表示的结构（（a）中，（B），（C）），其中R <7>是氢，羟基，-NR <10> - [R <11>，羟甲基或-CH 2 NR <10>的R基团 <11>，羧基，甲氧羰基或乙氧羰基，其中R <10>代表氢，任选地羟基取代的C1-C3烷基，具有在烷氧基部分或C1-C3酰基1至4个碳原子的烷氧基羰基，并且R < 11>是氢或甲基，R <8>为氢，直链或支链的C1-C3烷基或环丙基; [R <9>是氢或甲基，R <6>是氢或甲基，R <5>是氢，甲基或结构的基团-CH = CH-CO 2 R <5“>，-CH2-CH2-CO 2 R < 5 '>，-CH2-CO-CH3，-CH2-CH2-CN，R <5'>是甲基或乙基; B表示-CH 2 - ，O或直键，其制备方法及其用于细菌感染的治疗或预防的用途。

2. 发明申请

WO1996006848A1 NEW THIAZOLO[3,2-a]QUINOLINE AND THIAZOLO[3,2-a]NAPHTHYRIDINE DERIVATIVES 审中-公开
标题翻译： NEW噻唑并[3,2-a]喹啉和-NAPHTHYRIDINDERIVATE
公开(公告)号：WO1996006848A1
公开(公告)日：1996-03-07
申请号：PCT/EP1995003315
申请日：1995-08-21
申请人： BAYER AKTIENGESELLSCHAFT , JÄTSCH, Thomas , HALLENBACH, Werner , HIMMLER, Thomas , BREMM, Klaus-Dieter , ENDERMANN, Rainer , PIRRO, Franz , STEGEMANN, Michael , WETZSTEIN, Heinz-Georg
发明人： BAYER AKTIENGESELLSCHAFT
IPC分类号： C07D513/04
CPC分类号： C07D513/14
摘要： New thiazolo[3,2-a]quinoline and thiazolo-[3,2-a]naphthyridine derivatives have the general formula (I), in which R , R , Z and X have the meanings given in the description. Also disclosed are a process for preparing the same and their use in bactericide agents.
摘要翻译：本发明涉及新的噻唑并[3,2-a]喹啉和噻唑并[3,2-α〕通式（I）的萘啶衍生物，其中R <1>，R <2>，Z和X在的意义的说明，如上所述，它们的制备方法和它们在抗菌剂的用途。

3. 发明申请

WO1998000421A1 QUINOLONE CARBOXYLIC ACIDS SUBSTITUTED BY 7-(3-VINYL-1,4-PIPERAZINE-1-YL) 审中-公开
标题翻译： 7-（3-乙烯基-1,4-哌嗪-1-基） - 取代的喹诺酮羧酸
公开(公告)号：WO1998000421A1
公开(公告)日：1998-01-08
申请号：PCT/EP1997003116
申请日：1997-06-16
申请人： BAYER AKTIENGESELLSCHAFT , HIMMLER, Thomas , JAETSCH, Thomas , HALLENBACH, Werner , RAST, Hans-Georg , WETZSTEIN, Heinz-Georg , HEINEN, Ernst , PIRRO, Franz , SCHEER, Martin , STEGEMANN, Michael , STUPP, Hans-Peter
发明人： BAYER AKTIENGESELLSCHAFT
IPC分类号： C07D401/04
CPC分类号： C07D215/56
摘要： The invention concerns new quinolone carbonic acids substituted by 7-(3-vinyl-1,4-piperazine-1-yl) of general formula (I) in which R stands for hydrogen or alkyl optionally substituted by hydroxy, methoxy, amino, methylamino or dimethylamino with 1 to 4 carbon atoms or (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl; R stands for hydrogen or fluorine when at the same time R is a different hydrogen or fluorine, or stands for amino, methyl or vinyl; R stands for hydrogen, benzyl, alkyl with 1 to 3 carbon atoms, groups of -CH=CH-COOR , -CH2CH2-COOR , -CH2CH2CN, -CH2CH2COCH3, -CH2COCH3, in which R stands for methyl or ethyl or stands for a group of the general structure R -(NH-CHR -CO)n- in which R stands for hydrogen, alkyl with 1 to 3 carbon atoms or stands for the -COO-tertiary butyl group, R stands for hydrogen, alkyl with 1 to 4 carbon atoms, hydroxyalkyl with 1 or 2 carbon atoms, CH2-phenyl, aminoalkyl or thioalkyl with 1 or 2 carbon atoms and n = 1 or 2; and R stands for hydrogen or flourine when R stands for amino, methyl or vinyl or stands for chlorine, methoxy, difluoromethoxy, CN or ethinyl. The invention also concerns a method for their use and their use in antibacterial substances.
摘要翻译：本发明涉及新颖的7-（3-乙烯基-1,4-哌嗪-1-基）通式（I）中R <1>是氢，任选被羟基，甲氧基，氨基，甲氨基或取代的取代的喹诺酮羧酸二甲基氨基 - 取代的碳原子数为1〜4的烷基或（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基）甲基; [R <2>代表氢或氟时，R是在同一时间<4>不为氢或氟，或表示氨基，甲基或乙烯基; [R <3>是具有1〜3个碳原子，结构的基团为氢，苄基，烷基-CH = CH-COOR <5> -CH2CH2-COOR <5>，-CH2CH2CN，-CH2CH2COCH3，-CH2COCH3，其中R < 5>代表甲基或乙基，或基团为式R <6> - （NH-CHR <7> -CO）N，其中R <6>于氢，具有1至3个碳原子的烷基，或自由基-COO - 叔丁基，R <7>是具有1至4个碳原子，具有1或2个碳原子，CH 2 - 苯基，氨基烷基羟烷基或硫代烷基具有1或2个碳原子和n = 1或2个氢，烷基是; 且R <4>代表氢或氟，当R <2>代表氨基，甲基或乙烯基，或为氯，甲氧基，二氟甲氧基，CN或乙炔基，使用它们并且它们的使用在抗菌剂的方法。

4. 发明申请

WO1997031001A1 POSSIBLY SUBSTITUTED 8-CYANO-1-CYCLOPROPYL-7-(2,8-DIAZABICYCLO-[4.3.0]-NONAN-8-YL)-6-FLUORO-1,4-DIHYDRO-4-OXO-3-QUINOLIN CARBOXYLIC ACIDS AND THEIR DERIVATIVES 审中-公开
标题翻译：任选取代的8-氰基-1-环丙基-7-（2,8-二氮杂双环[4.3.0]壬烷-8-基）-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸和及其衍生物
公开(公告)号：WO1997031001A1
公开(公告)日：1997-08-28
申请号：PCT/EP1997000637
申请日：1997-02-12
申请人： BAYER AKTIENGESELLSCHAFT , BARTEL, Stefan , JAETSCH, Thomas , HIMMLER, Thomas , RAST, Hans-Georg , HALLENBACH, Werner , HEINEN, Ernst , PIRRO, Franz , SCHEER, Martin , STEGEMANN, Michael , STUPP, Hans-Peter , WETZSTEIN, Heinz-Georg
发明人： BAYER AKTIENGESELLSCHAFT
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A01N43/90
摘要： The present invention relates to novel possibly substituted 8-cyano-1-cyclopropyl-7-(2,8-diazabicyclo-(4.3.0)-onan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolin carboxylic acids and their derivatives of the general formula (I) in which R is hydrogen, C1-C4 alkyl possibly substituted by hydroxy, methoxy, amino, methylamino or dimethylamino or (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl, R is hydrogen, benzyl, C1-C3 alkyl, (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl, radicals of the structures -CH=CH-COOR , -CH2CH2COOR , -CH2CH2CN, -CH2CH2COCH3, -CH2COCH3, where R is methyl or ethyl, or a radical of the general structure R -(NH-CHR -CO)n-, in which R is hydrogen, C1-C3 alkyl or the radical -COO-tert.-butyl, R is hydrogen, C1-C4 alkyl, hydroxyalkyl, aminoalkyl, thioalkyl, carboxyalkyl or benzyl and n = 1 or 2, and Y is oxygen or sulplur. The invention further concerns the process for their production and their use in anti-bacterial agents.
摘要翻译：本发明涉及新的任选取代的8-氰基-1-环丙基-7-（2,8-二氮杂双环[4.3.0]壬烷-8-基）-6-氟-1,4-二氢-4-氧代-3- -chinolincarbonsäuren和它们在通式（I）中R <1>表示氢的衍生物，任选地被羟基，甲氧基，氨基，甲基氨基或二甲基氨基，C1-C4烷基或（5-甲基-2-氧代-1-基， 3-二氧杂环戊烯-4-基）甲基，R <2>是氢，苄基，C1-C3烷基，（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基）甲基，基团结构的-CH = CH-COOR <3>，-CH2CH2COOR <3>，-CH2CH2CN，-CH2CH2COCH3，-CH2COCH3，其中R <3>代表甲基或乙基，或基团的式R <4>的 - （NH-CHR <5>-CO）N，<4>其中R是氢，C1-C3烷基或基团-COO - 叔丁基，R <5>是氢，C1-C4 烷基，羟烷基，氨基烷基，硫代烷基，羧基烷基或苄基，n是1或2，Y表示氧或硫，它们的制备和它们的VERWEIJ过程本发明中的抗菌剂。

5. 发明申请

WO1998026768A2 USE OF 7-(1-AMINOMETHYL-2-OXA-7-AZA-BICYCLO[3.3.0]OCT-7-YL)-QUINOLONE CARBOXYLIC ACID AND NAPHTHYRIDONE CARBOXYLIC ACID DERIVATIVES FOR TREATING HELICOBACTER PYLORI INFECTIONS AND THE GASTRODUODENAL DISEASES ASSOCIATED THEREWITH 审中-公开
标题翻译： 7-（1-氨基甲基-2-氧杂-7-氮杂双环[3.3.0]辛-7-基）-CHINOLONCARBONSÄURE--NAPHTHYRIDONCARBONSÄURE及其衍生物幽门螺杆菌感染的治疗利用和与其相关联的胃十二指肠疾病
公开(公告)号：WO1998026768A2
公开(公告)日：1998-06-25
申请号：PCT/EP1997006751
申请日：1997-12-03
申请人： BAYER AKTIENGESELLSCHAFT , PETERSEN, Uwe , MATZKE, Michael , JAETSCH, Thomas , SCHENKE, Thomas , HIMMLER, Thomas , BARTEL, Stephan , BAASNER, Bernd , WERLING, Hans-Otto , SCHALLER, Klaus , LABISCHINSKI, Harald , ENDERMANN, Rainer
发明人： BAYER AKTIENGESELLSCHAFT
IPC分类号： A61K31/00
CPC分类号： C07D491/04 , A61K31/4375 , A61K31/4709 , A61K31/4745 , A61K31/5383 , A61K31/5395 , C07F9/6561
摘要： The invention concerns the use of quinolone and naphthyridone carboxylic acid derivatives which are substituted in position 7 by a 1-aminomethyl-2-oxa-7-azabicyclo[3.3.0]oct-7-yl group and their salts for treating Helicobacter pylori infections and the gastroduodenal diseases associated therewith.
摘要翻译：本发明涉及使用喹诺酮和naphthyridonecarboxylic酸衍生物的其在7位上由1氨基甲基-2-氧杂-7-氮杂 - 双环取代的[3.3.0]辛-7-基团，以及它们的盐幽门螺杆菌感染和与其相关联的胃十二指肠疾病的治疗。

6. 发明申请

WO1998026779A1 THE USE OF 7-(2-OXA-5,8-DIAZABICYCLO[4.3.0]NON-8-YL)-QUINOLONE CARBOXYLIC ACID AND NAPHTHYRIDON CARBOXYLIC ACID DERIVATIVES FOR THE TREATMENT OF HELICOBACTER PYLORI INFECTIONS AND ASSOCIATED GASTRODUODENAL DISEASES 审中-公开
标题翻译：使用7-（2-氧杂-5,8-二氮杂双环[4.3.0]壬-8-基）-CHINOLONCARBONSÄURE-AND-NAPHTHYRIDONCARBONSÄURE衍生物对幽门螺杆菌感染的与其相关联的治疗和胃十二指肠疾病
公开(公告)号：WO1998026779A1
公开(公告)日：1998-06-25
申请号：PCT/EP1997006781
申请日：1997-12-04
申请人： BAYER AKTIENGESELLSCHAFT , MATZKE, Michael , PETERSEN, Uwe , JAETSCH, Thomas , BARTEL, Stephan , SCHENKE, Thomas , HIMMLER, Thomas , BAASNER, Bernd , WERLING, Hans-Otto , SCHALLER, Klaus , LABISCHINSKI, Harald
发明人： BAYER AKTIENGESELLSCHAFT
IPC分类号： A61K31/47
CPC分类号： C07D498/04 , A61K31/5383 , A61K31/5395 , C07D519/00
摘要： The invention relates to the use of quinolone and naphthyridon carboxylic acid derivatives, which are substituted by a 2-oxa-5,8-diazabicyclo[4.3.0]-non-8-yl-radical in position seven, as well as to their pharmaceutically applicable hydrates and/or salts in the treatment of Helicobacter pylori infections and associated gastroduodenal diseases.
摘要翻译：本发明涉及使用喹诺酮和naphthyridonecarboxylic酸衍生物的其在7位上被2-氧杂-5,8-二氮杂双环[4.3.0] - 壬-8-基团，以及其可药用的水合物取代和/或盐幽门螺杆菌感染和与其相关联的胃十二指肠疾病的治疗。

7. 发明申请

WO1997015354A1 METHODS FOR DECOMPOSING QUINOLONES AND NAPHTHYRIDONES 审中-公开
标题翻译：方法去除喹诺酮类和NAPHTHYRIDONEN的
公开(公告)号：WO1997015354A1
公开(公告)日：1997-05-01
申请号：PCT/EP1996004421
申请日：1996-10-11
申请人： BAYER AKTIENGESELLSCHAFT , WETZSTEIN, Heinz-Georg , RAST, Hans-Georg , KARL, Wolfgang , MARTENS, Rainer , ZADRAZIL, Frantisek
发明人： BAYER AKTIENGESELLSCHAFT
IPC分类号： A62D03/00
CPC分类号： C02F3/34 , A62D3/02 , A62D2101/22 , A62D2101/28 , B09C1/10
摘要： The invention concerns two methods of treating quinolones and naphthyridones having an antimicrobial, in particular antibacterial, action, as well as derivatives of such compounds with wood-rotting fungi, optionally in the presence of water and/or inert solid or liquid substrates and other auxiliaries.
摘要翻译：本发明涉及两种方法的抗微生物治疗，特别是抗菌，喹诺酮作用和naphthyridonecarboxylic羧酸及其衍生物与木材腐菌体，如果合适的话在水的存在下和/或惰性固体或液体的底物和其它助剂。

8. 发明申请

WO1996031532A1 SUGAR-MODIFIED CYTOSTATICS 审中-公开
标题翻译：碳水化合物修饰的细胞抑制剂
公开(公告)号：WO1996031532A1
公开(公告)日：1996-10-10
申请号：PCT/EP1996001279
申请日：1996-03-22
申请人： BAYER AKTIENGESELLSCHAFT , LERCHEN, Hans-Georg , VON DEM BRUCH, Karsten , PETERSEN, Uwe , BAUMGARTEN, Jörg , PIEL, Norbert , ANTONICEK, Horst-Peter , WEICHEL, Walter , SPERZEL, Michael , BREMM, Klaus, Dieter
发明人： BAYER AKTIENGESELLSCHAFT
IPC分类号： C07K09/00
CPC分类号： C07D401/04 , A61K31/02 , C07D487/04 , C07H15/203 , C07K9/001 , Y02P20/55
摘要： The invention relates to cytostatics which are made tumour-specific by modification with sugar. Suitable spacers ensure serum-stability and intracellular effect at the same time.
摘要翻译：本发明涉及细胞生长抑制剂其是肿瘤特异性的，通过用糖修饰。合适的间隔保证血清稳定性，并在同一细胞内的作用。

9. 发明申请

WO1995006654A1 GLYCOSYL AMIDES OF 2-AMINOACYLAMINO-2-DEOXY SUGARS 审中-公开
标题翻译：糖基的2-氨酰基氨基-2-脱氧糖
公开(公告)号：WO1995006654A1
公开(公告)日：1995-03-09
申请号：PCT/EP1994002736
申请日：1994-08-17
申请人： BAYER AKTIENGESELLSCHAFT , LOCKHOFF, Oswald , MIELKE, Burkhard , BRUNNER, Helmut , SCHALLER, Klaus
发明人： BAYER AKTIENGESELLSCHAFT
IPC分类号： C07H15/12
CPC分类号： C07H15/12 , A61K38/00 , C07K9/005 , Y10S514/885
摘要： The present invention relates to (2-aminoacylamino-2-deoxy glycosyl) amides substituted on the nitrogen atom of the amino-acid of general formula (I) in which the substituents have the meaning given in the specification, process for producing them and their use in medicaments.
摘要翻译：本发明涉及在氨基酸取代（2-氨酰基氨基-2-脱氧糖基）的通式（I）的 - 酰胺的氮原子，其中各取代基具有本说明书给出的含义，它们的制备方法和其医药用途。

10. 发明申请

WO1995006655A1 (GLYCOSIL AMIDE) URONIC ACID DERIVATIVES 审中-公开
标题翻译：（Glycosylamide）-URONSÄURE衍生物
公开(公告)号：WO1995006655A1
公开(公告)日：1995-03-09
申请号：PCT/EP1994002737
申请日：1994-08-17
申请人： BAYER AKTIENGESELLSCHAFT , LOCKHOFF, Oswald , MIELKE, Burkhard , BRUNNER, Helmut
发明人： BAYER AKTIENGESELLSCHAFT
IPC分类号： C07H15/12
CPC分类号： C07H15/12 , A61K38/00 , C07K9/005
摘要： The present invention relates to (glycosil amide) uronic acid derivatives of general formula (I) in which the substituents have the meaning given in the specification, process for producing them and their use in medicaments.
摘要翻译：现在，本发明涉及通式（I），其中各取代基具有本说明书给出的含义的（glycosylamide）-uronsäure衍生物，它们的制备方法，以及它们在药物的用途。

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