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71. 发明授权

US06664268B1 Crystal modification B of 8-cyano-1-cyclopropyl-7-(1S,6S-2, 8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid 有权
标题翻译： 8-氰基-1-环丙基-7-（1S，6S-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
公开(公告)号：US06664268B1
公开(公告)日：2003-12-16
申请号：US09856670
申请日：2001-05-23
申请人： Thomas Himmler , Werner Hallenbach , Hubert Rast
发明人： Thomas Himmler , Werner Hallenbach , Hubert Rast
IPC分类号： A61K314709
CPC分类号： C07D471/04
摘要： The present invention relates to a defined crystal modification of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (I), to processes for its preparation and to its use in pharmaceutical preparations. The crystal modification can be distinguished from other crystal modifications of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (I) by its characteristic X-ray powder diffractogram and its differential thermodiagram (see description).
摘要翻译：本发明涉及8-氰基-1-环丙基-7-（1S，6S-2,8-二氮杂双环[4.3.0]壬烷-8-基）-6-氟-1,4- 式（I）的二氢-4-氧代-3-喹啉羧酸，其制备方法及其在药物制剂中的应用。晶体修饰可以区别于8-氰基-1-环丙基-7 - （1S，6S-2,8-二氮杂双环[4.3.0]壬烷-8-基）-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸其特征 X射线粉末衍射图及其差示热图（见说明）。

72. 发明授权

US06436955B1 Crystal modification A of 8-cyano-1-cyclopropyl-7-(is,6s-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid 有权
标题翻译： 8-氰基-1-环丙基-7-（is，6s-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
公开(公告)号：US06436955B1
公开(公告)日：2002-08-20
申请号：US09856669
申请日：2001-05-23
申请人： Thomas Himmler , Werner Hallenbach , Hubert Rast
发明人： Thomas Himmler , Werner Hallenbach , Hubert Rast
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： The present invention relates to a defined crystal modification of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0] nonan-8-yl)-6-fluoro-1, 4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (I), to processes for its preparation and to its use in pharmaceutical preparations. The crystal modification can be distinguished from other crystal modifications of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl )-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (I) by its characteristic X-ray powder diffractogram and its differential thermodiagram (see description).
摘要翻译：本发明涉及8-氰基-1-环丙基-7-（1S，6S-2,8-二氮杂双环[4.3.0]壬烷-8-基）-6-氟-1,4- 式（I）的二氢-4-氧代-3-喹啉羧酸，其制备方法及其在药物制剂中的应用。晶体修饰可以区别于8-氰基-1-环丙基-7 - （1S，6S-2,8-二氮杂双环[4.3.0]壬烷-8-基）-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸其特征 X射线粉末衍射图及其差示热图（见说明）。

73. 发明授权

US06432948B1 USE OF 7-(2-OXA-5,8-DIAZABICYLCO[4.3.0]NON-8-YL)-QUINOLONE CARBOXYLIC ACID AND NAPHTHYRIDON CARBOXYLIC ACID DERIVATIVES FOR THE TREATMENT OF HELIOBACTER PYLORI INFECTIONS AND ASSOCIATED GASTRODUODENAL DISEASES 有权
标题翻译： 7-（2-OXA-5,8-二氮杂双环[4.3.0]壬-8-基） - 喹啉酮羧酸和萘硫酮羧酸衍生物用于治疗幽门螺杆菌感染和相关胃肠道疾病的用途
公开(公告)号：US06432948B1
公开(公告)日：2002-08-13
申请号：US09436316
申请日：1999-11-08
申请人： Michael Matzke , Uwe Petersen , Thomas Jaetsch , Stephan Bartel , Thomas Schénke , Thomas Himmler , Bernd Baasner , Hans-Otto Werling , Klaus Schaller , Harald Labischinski
发明人： Michael Matzke , Uwe Petersen , Thomas Jaetsch , Stephan Bartel , Thomas Schénke , Thomas Himmler , Bernd Baasner , Hans-Otto Werling , Klaus Schaller , Harald Labischinski
IPC分类号： A61K315365
CPC分类号： C07D498/04 , A61K31/5383 , A61K31/5395 , C07D519/00
摘要： The invention relates to the use of quinolone- and naphthyridonecarboxylic acid derivatives, which are substituted in the 7-position by a 2-oxa-5,8-diazabicyclo[4.3.0]-non-8-yl) radical, and their pharmaceutically utilizable hydrates and/or salts for the therapy of Helicobacter pylori infections and the gastroduodenal disorders associated therewith.
摘要翻译：本发明涉及使用2-氧杂-5,8-二氮杂双环[4.3.0] - 壬-8-基）基团在7-位取代的喹诺酮和萘啶酮羧酸衍生物及其药学上可接受的盐用于治疗幽门螺杆菌感染的可利用的水合物和/或盐和与之相关的胃十二指肠疾病。

74. 发明授权

US06288081B1 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 失效
标题翻译： 7-（1-氨基甲基-2-氧杂-7-氮杂 - 双环[3.3.0]辛-7-基） - 喹诺酮羧酸和萘啶酮羧酸衍生物用于治疗幽门螺杆菌感染和与之相关的胃十二指肠疾病
公开(公告)号：US06288081B1
公开(公告)日：2001-09-11
申请号：US09319848
申请日：1999-08-06
申请人： Uwe Petersen , Michael Matzke , Thomas Jaetsch , Thomas Schenke , Thomas Himmler , Stephan Bartel , Bernd Baasner , Hans-Otto Werling , Klaus Schaller , Harald Labischinski , Rainer Endermann
发明人： Uwe Petersen , Michael Matzke , Thomas Jaetsch , Thomas Schenke , Thomas Himmler , Stephan Bartel , Bernd Baasner , Hans-Otto Werling , Klaus Schaller , Harald Labischinski , Rainer Endermann
IPC分类号： A61K314709
CPC分类号： C07D491/04 , A61K31/4375 , A61K31/4709 , A61K31/4745 , A61K31/5383 , A61K31/5395 , C07F9/6561
摘要： The invention relates to the use of quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in position 7 by a 1-aminomethyl-2-oxa-7-azabicyclo[3.3.0]oct-7-yl radical, and of their salts for the therapy of Helicobacter pylori infections and associated gastroduodenal disorders.
摘要翻译：本发明涉及在位置7被1-氨基甲基-2-氧杂-7-氮杂双环[3.3.0]辛-7-基取代的喹诺酮和萘啶酮羧酸衍生物及其盐用于治疗幽门螺杆菌感染和相关的胃十二指肠疾病。

75. 发明授权

US06278013B1 Optionally substituted 8-cyano-1-cyclopropyl-7-(2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids and their derivatives 有权
标题翻译：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-喹啉羧酸及其衍生品
公开(公告)号：US06278013B1
公开(公告)日：2001-08-21
申请号：US09718062
申请日：2000-11-21
申请人： Stefan Bartel , Thomas Jaetsch , Thomas Himmler , Hans-Georg Rast , Werner Hallenbach , Ernst Heinen , Franz Pirro , Martin Scheer , Michael Stegemann , Hans-Peter Stupp , Heinz-Georg Wetzstein
发明人： Stefan Bartel , Thomas Jaetsch , Thomas Himmler , Hans-Georg Rast , Werner Hallenbach , Ernst Heinen , Franz Pirro , Martin Scheer , Michael Stegemann , Hans-Peter Stupp , Heinz-Georg Wetzstein
IPC分类号： C07C25550
CPC分类号： C07D471/04 , A01N43/90
摘要： Intermediates useful in the preparation of 8-cyano-1-cyclopropyl-7-(2,8-diazabicyclo[4.3.0]nonan-8-yl-6-fluorol,4-dihydro-4-oxo-3-quinolinecarboxylic acids of the following structures are claimed.
摘要翻译：可用于制备8-氰基-1-环丙基-7-（2,8-二氮杂双环[4.3.0]壬烷-8-基-6-氟，4-二氢-4-氧代-3-喹啉羧酸的中间体要求下列结构。

76. 发明授权

US06255335B1 Substituted 2-oxo-alkanoic acid-[2-(indol-3-yl)-ethyl] amides 失效
标题翻译：取代的2-氧代 - 链烷酸 - [2-（吲哚-3-基） - 乙基]酰胺
公开(公告)号：US06255335B1
公开(公告)日：2001-07-03
申请号：US09673155
申请日：2000-10-11
申请人： Thomas Himmler , Franz Pirro
发明人： Thomas Himmler , Franz Pirro
IPC分类号： A61K31404
CPC分类号： C07D209/14
摘要： The invention relates to novel N-[2-(indol-3-yl)ethyl]-2-oxo-alkanarnides of the general formula (I) in which R1 represents optionally branched C1-C8-alkyl or C4-C8-cycloalkyl, R2 independently of R3 represents hydrogen, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-thioalkyl, phenyl or halogen, R3 represents hydrogen, C1 -C4-alkyl or halogen and R4 represents optionally branched C1-C6-alkyl, C4-C6-cycloalkyl, phenyl which is optionally mono- to trisubstituted by C1-C3-alkyl, C1-C3-alkoxy, C1-C3-thioalkyl, halogen, nitro or amino or benzyl which is optionally mono- to trisubstituted by C1-C3-alkyl, C1-C3-alkoxy, C1-C3-thioalkyl, halogen, nitro or amino, to processes for their preparation and to their use in antibacterial compositions.
摘要翻译：本发明涉及通式（I）的新的N- [2-（吲哚-3-基）乙基] -2-氧代 - 烷酰胺，其中R 1表示任选支链的C 1 -C 8 - 烷基或C 4 -C 8 - 环烷基，R 2 独立的R 3表示氢，C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 硫代烷基，苯基或卤素，R 3表示氢，C 1 -C 4烷基或卤素，R 4表示任选支链的C 1 -C 6 - C 1-6 - 环烷基，任选被C 1 -C 3烷基，C 1 -C 3 - 烷氧基，C 1 -C 3 - 硫代烷基，卤素，硝基或氨基或苄基单取代，三取代的苯基，其任选被C1-C3单取代，三取代 - 烷基，C 1 -C 3 - 烷氧基，C 1 -C 3 - 硫代烷基，卤素，硝基或氨基，用于其制备及其在抗菌组合物中的应用。

77. 发明授权

US5744478A Thiazolo �3,2-a! quinoline and thiazolo �3,2-a! naphthyridine derivatives 失效
标题翻译：噻唑并[3,2-a]喹啉和噻唑并[3,2-a]萘啶衍生物
公开(公告)号：US5744478A
公开(公告)日：1998-04-28
申请号：US793795
申请日：1997-02-21
申请人： Thomas Jaetsch , Werner Hallenbach , Thomas Himmler , Klaus-Dieter Bremm , Rainer Endermann , Franz Pirro , Michael Stegemann , Heinz-Georg Wetzstein
发明人： Thomas Jaetsch , Werner Hallenbach , Thomas Himmler , Klaus-Dieter Bremm , Rainer Endermann , Franz Pirro , Michael Stegemann , Heinz-Georg Wetzstein
IPC分类号： C07D513/04 , A61K31/435 , A61K31/535 , A61P31/04 , C07D513/14 , C07D513/16 , C07D519/00
CPC分类号： C07D513/14
摘要： The present invention relates to new thiazolo�3,2-a!quinoline and thiazolo�3,2-a!naphthyridine derivatives of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, Z and X have the meaning indicated in the description, processes for their preparation and their use in antibacterial compositions.
摘要翻译： PCT No.PCT / EP95 / 03315 Sec。 371日期1997年2月21日 102（e）日期1997年2月21日PCT提交1995年8月21日PCT公布。出版物WO96 / 06848 日期：1996年3月7日本发明涉及在描述中描述的通式（I）的新的噻唑并[3,2-a]喹啉和噻唑并[3,2-a]萘啶衍生物，其制备方法以及它们在抗菌组合物中的应用。

78. 发明授权

US5462955A Azolylmethyl-fluorocyclopropyl derivatives 失效
标题翻译：唑基甲基 - 氟代环丙基衍生物
公开(公告)号：US5462955A
公开(公告)日：1995-10-31
申请号：US197016
申请日：1994-02-15
申请人： Jurgen Scherkenbeck , Thomas Himmler , Stefan Bohm , Hermann Hagemann , Klaus Stroech , Stefan Dutzmann , Heinz-Wilhelm Dehne , Gerd Hanssler
发明人： Jurgen Scherkenbeck , Thomas Himmler , Stefan Bohm , Hermann Hagemann , Klaus Stroech , Stefan Dutzmann , Heinz-Wilhelm Dehne , Gerd Hanssler
IPC分类号： A01N43/653 , C07D249/08 , C07D301/02 , C07D303/08 , C07D303/18 , C07D303/20 , C07D521/00
CPC分类号： C07D249/08 , A01N43/653 , C07D231/12 , C07D233/56
摘要： New azolylmethyl-fluorocyclopropyl derivatives of the formula ##STR1## in which R represents ##STR2## and addition products thereof which acids or metal salts are very effective for combating fungi.New oxiranes of the formula ##STR3## in which R has the abovementioned meaning, are valuable intermediates for the preparation of compounds of the formula (I).
摘要翻译：式（Ⅰ）的新的吡唑基甲基 - 氟代环丙基衍生物，其中R代表

79. 发明授权

US5216180A Microbicidal hydroxyethyl-cyclopropyl-azolyl derivatives 失效
标题翻译：杀微生物羟乙基 - 环丙基 - 唑基衍生物
公开(公告)号：US5216180A
公开(公告)日：1993-06-01
申请号：US786481
申请日：1991-11-01
申请人： Jurgen Scherkenbeck , Monika Frie , Klaus Stroech , Thomas Himmler , Georg-W. Ludwig , Wilhelm Brandes , Stefan Dutzmann
发明人： Jurgen Scherkenbeck , Monika Frie , Klaus Stroech , Thomas Himmler , Georg-W. Ludwig , Wilhelm Brandes , Stefan Dutzmann
IPC分类号： A01N43/50 , A01N43/653 , C07C33/44 , C07C33/50 , C07C45/74 , C07C49/577 , C07D303/22 , C07D307/46 , C07D333/16 , C07D407/06 , C07D407/14 , C07D409/06 , C07D409/14 , C07D521/00
CPC分类号： C07D303/22 , A01N43/50 , A01N43/653 , C07C33/44 , C07C33/50 , C07C45/74 , C07C49/577 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/46 , C07D333/16 , C07D407/06 , C07D407/14 , C07D409/06 , C07D409/14
摘要： A herbicidal hydroxyethyl-cyclopropyl-azolyl derivative of the formula ##STR1## in which R.sup.1 represents halogen, phenyl or the grouping --Z-R.sup.3, whereinZ represents oxygen, sulphur, SO or SO.sub.2 andR.sup.3 represents alkyl, phenyl or benzyl,R.sup.2 represents alkenyl, optionally substituted furyl, optionally substituted thienyl or the radical of the formula ##STR2## wherein R.sup.4 represents difluoromethoxy, 1,1,2,2-tetrafluoroethoxy, 1,1,2-trifluoro-2-chloro-ethoxy, cyano, formyl, alkoximinoalkyl, carbalkoxy, dialkoxyalkyl, phenoxyalkyl which is optionally substituted in the phenyl moiety by halogen, or benzyloxy which is optionally substituted in the phenyl moiety by halogen andR.sup.5 represents hydrogen or halogen, orR.sup.4 and R.sup.5 are linked in the ortho-position and together represent --O--CH.sub.2 --O--, orR.sup.2 represents the radical of the formula ##STR3## in which R.sup.6 represents difluoromethoxy, 1,1,2,2-tetrafluoroethoxy or 1,1,2-trifluoro-2-chloro-ethoxy, orR.sup.2 also represents phenyl which is optionally substituted by halogen and/or phenyl if Y represents the grouping ##STR4## X represents nitrogen or a CH group and Y represents the groupings --CH.sub.2 -CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C-- or ##STR5## or an acid or metal salt addition product thereof.
摘要翻译：式（I）的除草羟乙基 - 环丙基 - 唑基衍生物，其中R 1表示卤素，苯基或基团-Z-R 3，其中Z表示氧，硫，SO或SO 2，R 3表示烷基，苯基或苄基，R 2表示烯基，任选取代的呋喃基，任选取代的噻吩基或式的基团其中R 4表示二氟甲氧基，1,1,2,2-四氟乙氧基，1,1,2-三氟-2-氯乙氧基，氰基，甲酰基，肟基烷基，烷氧基，二烷氧基烷基，在苯基部分被卤素任意取代的苯氧基烷基，或在苯基部分被卤素任意取代的苄氧基，R5代表氢或卤素，或R4和R5连接在邻位并且一起表示-O-CH 2 -O-，或R 2表示式“IMAGE”的基团，其中R 6表示二氟甲氧基，1,1,2,2-四氟乙氧基或1,1,2-三氟-2- 氯乙氧基，或R2也表示任选取代的苯基如果Y表示分组，则由卤素和/或苯基发生。X表示氮或CH基，Y表示分组-CH 2 -CH 2 - ， - CH = CH - ， - C 3BOND C或或酸或金属盐加成产物。

80. 发明授权

US5216006A Fungicidal azolyl-propanol derivatives 失效
标题翻译：杀真菌剂 - 丙酰胺衍生物
公开(公告)号：US5216006A
公开(公告)日：1993-06-01
申请号：US709540
申请日：1991-06-03
申请人： Je,uml/u/ rgen Scherkenbeck , Thomas Himmler , Klaus Stroech , Stefan Dutzmann , Gerd Hanssler , Heinz-Wilhelm Dehne
发明人： Je,uml/u/ rgen Scherkenbeck , Thomas Himmler , Klaus Stroech , Stefan Dutzmann , Gerd Hanssler , Heinz-Wilhelm Dehne
IPC分类号： A01N43/50 , A01N43/653 , C07D233/60 , C07D249/08 , C07D301/02 , C07D303/08 , C07D303/12 , C07D303/22 , C07D405/06 , C07D407/04 , C07D521/00
CPC分类号： C07D249/08 , A01N43/653 , C07D231/12 , C07D233/56 , C07D303/08
摘要： Fungicidal azolyl-propanols of the formula ##STR1## in which R represents halogenoalkyl, halogenoalkenyl, a 2-phenoxy-isopropyl radical, ##STR2## Y represents nitrogen or a CH group, Z represents halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, cyano, phenoxy, halo-phenoxy, or optionally substituted aryl,m represents the number 0, 1, 2, or 3, and addition products thereof with acids and metal salts.
摘要翻译：其中R表示卤代烷基，卤代烯基，2-苯氧基 - 异丙基，Y或Y表示式（I）的杀真菌唑基 - 丙醇代表氮或CH基，Z表示卤素，烷基，卤代烷基，烷氧基，卤代烷氧基，氰基，苯氧基，卤代苯氧基或任选取代的芳基，m表示数0,1,2或3，以及其与酸和金属盐的加成产物。

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