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1. 发明申请

US20060142343A1 Pyrrolines 失效
标题翻译：吡咯啉
公开(公告)号：US20060142343A1
公开(公告)日：2006-06-29
申请号：US10528259
申请日：2003-09-08
申请人： Johannes Jansen , Udo Kraatz , Hubertus Stakemeier , Thomas Seitz , Fritz Maurer , Martin Fusslein , Bernd Alig , Christian Funke , Werner Hallenbach , Jorg Konze , Udo Beckmann , Ulrich Gorgens
发明人： Johannes Jansen , Udo Kraatz , Hubertus Stakemeier , Thomas Seitz , Fritz Maurer , Martin Fusslein , Bernd Alig , Christian Funke , Werner Hallenbach , Jorg Konze , Udo Beckmann , Ulrich Gorgens
IPC分类号： A01N43/40 , C07D403/14
CPC分类号： C07D403/10 , C07D409/10 , C07D413/10
摘要： The invention relates to novel Δ1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R8, R9 and Q are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling pests.
摘要翻译：本发明涉及其中R 1，R 2，R 3，R 3，R 3，R 3，R 3， R 4，S 4，A 1，A 2，R 5，R 6， R 7，R 8，R 9和R 9如本公开所定义，与制备这些化合物的方法和用于控制害虫。

2. 发明授权

US06323213B1 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 有权
标题翻译：可取代的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-喹啉羧酸酸及其衍生物
公开(公告)号：US06323213B1
公开(公告)日：2001-11-27
申请号：US09125191
申请日：1998-08-13
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： A61K31407
CPC分类号： C07D471/04 , A01N43/90
摘要： The present invention relates to novel optionally substituted 8-cyano-1-cyclo-propyl-7-(2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids and their derivatives, of the general formula (I) in which R1 represents hydrogen, C1-C4-alkyl which is optionally substituted by hydroxyl, methoxy, amino, methylamino or dimethylamino, or (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl, R2 represents hydrogen, benzyl, C1-C3-alkyl, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl, radicals having the structures —CH═CH—COOR3, —CH2CH2COOR3, —CH2CH2CN, —CH2CH2COCH3 or —CH2COCH3, in which R3 represents methyl or ethyl, or a radical of the general structure R4—(NH—CHR5—CO)n—, in which R4 represents hydrogen, C1-C3-alkyl or the radical —COO-tert-butyl, R5 represents hydrogen, C1-C4-alkyl, hydroxyalkyl, aminoalkyl, thioalkyl, carboxyalkyl or benzyl and n is 1 or 2, and Y is oxygen or sulfur, the process for their preparation and their use in antibacterial compositions.
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- 甲氧基，氨基，甲基氨基或二甲基氨基取代的C 1 -C 4 - 烷基，或（5-甲基-2-羟基喹啉羧酸）或其衍生物，其中R 1表示氢，氧代-1,3-二氧杂环戊烯-4-基）甲基，R 2表示氢，苄基，C 1 -C 3 - 烷基，（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基）甲基，结构-CH = CH-COOR 3，-CH 2 CH 2 COOR 3，-CH 2 CH 2 CN，-CH 2 CH 2 COCH 3或-CH 2 COCH 3，其中R 3表示甲基或乙基，或通式结构R4-（NH-CHR5-CO）n - 的基团，其中R4 代表氢，C 1 -C 3 - 烷基或-COO-叔丁基，R 5表示氢，C 1 -C 4 - 烷基，羟基烷基，氨基烷基，硫代烷基，羧基烷基或苄基，n是1或2，Y是氧或硫，其制备方法及其在抗菌组合物中的应用。

3. 发明授权

US5854241A Pyrido�3,2,1-I,J!�3,1!benzoxazine derivatives 失效
标题翻译：吡啶并[3,2,1-I，J] [3,1]苯并恶嗪衍生物
公开(公告)号：US5854241A
公开(公告)日：1998-12-29
申请号：US765212
申请日：1997-01-03
申请人： Werner Hallenbach , Thomas Himmler , Thomas Jaetsch , Burkhard Mielke , Klaus Dieter Bremm , Rainer Endermann , Franz Pirro , Michael Stegemann , Heinz-Georg Wetzstein
发明人： Werner Hallenbach , Thomas Himmler , Thomas Jaetsch , Burkhard Mielke , Klaus Dieter Bremm , Rainer Endermann , Franz Pirro , Michael Stegemann , Heinz-Georg Wetzstein
IPC分类号： A61K31/535 , C07C17/16 , C07D498/06 , C07D519/00 , C07D221/00 , C07D265/00
CPC分类号： C07D498/06 , C07C17/16 , C07D519/00
摘要： Disclosed are pyrido�3,2,1-i,j!�3,1!benzoxazine compounds of the formula (I): ##STR1## wherein z represents a radical having the formula: ##STR2## wherein B represents --CH.sub.2 --, --O-- or a direct bond; and the other variables in formula (I) and Z are as described herein. The compounds have antibacterial properties and also disclosed are antibacterial compositions containing them and methods of using them to prevent or combat bacterial infections. Methods for preparing the compounds are also disclosed.
摘要翻译： PCT No.PCT / EP95 / 02510 Sec。 371日期1997年1月3日 102（e）日期1997年1月3日PCT Filed June 28，1995 PCT Pub。出版物WO96 / 01829 日期1996年1月25日公开是式（I）的吡啶并[3,2,1-i，j] [3,1]苯并恶嗪化合物：其中z表示具有下式的基团： O-或直接结合; 式（I）和Z中的其它变量如本文所述。该化合物具有抗菌特性，并且还公开了含有它们的抗菌组合物和使用它们来预防或抵抗细菌感染的方法。还公开了制备化合物的方法。

4. 发明授权

US5374605A Isoxazolecarboxylic acid derivatives 失效
标题翻译：异恶唑羧酸衍生物
公开(公告)号：US5374605A
公开(公告)日：1994-12-20
申请号：US2307
申请日：1993-01-08
申请人： Werner Hallenbach , Hans-Joachim Santel , Klaus Lurssen , Robert R. Schmidt
发明人： Werner Hallenbach , Hans-Joachim Santel , Klaus Lurssen , Robert R. Schmidt
IPC分类号： A01N43/80 , C07D261/18 , C07D413/12 , C07D261/08 , C07D261/10
CPC分类号： C07D413/10 , A01N43/80 , C07D261/18
摘要： The invention relates to isoxazolecarboxylic acid derivatives of the general formula (I) ##STR1## in which A represents alkanediyl,Q represents oxygen, sulphur, imino (NH) or alkylimino (N-alkyl),R.sup.1 represents an in each case optionally substituted radical from the series comprising alkyl, cycloalkyl or phenyl,R.sup.2 represents hydrogen, halogen or optionally substituted alkyl, andR.sup.3 represents in each case optionally substituted cyclohexyl or phenyl,with the exception of the compounds: N-benzyl-5-cyclopropyl-isoxazole-3-carboxamide N-(2-phenyl-ethyl)-5-methyl-isoxazole-3-carboxamide and N-benzyl-5-methyl-isoxazole-3-carboxamide, a process for their preparation, and their use as herbicides.
摘要翻译：本发明涉及通式（I）的化合物（I）的异恶唑羧酸衍生物，其中A代表烷二基，Q代表氧，硫，亚氨基（NH）或烷基亚氨基（N-烷基），R1代表每种情况任选取代的烷基，环烷基或苯基系列的取代基，R 2表示氢，卤素或任选取代的烷基，R 3表示在任何情况下均为任选取代的环己基或苯基，但化合物除外：N-苄基-5-环丙基 - 异恶唑-3-甲酰胺N-（2-苯基 - 乙基）-5-甲基 - 异恶唑-3-甲酰胺和N-苄基-5-甲基 - 异恶唑-3-甲酰胺，其制备方法及其作为除草剂的用途。

5. 发明授权

US5028617A Heteroarylethanol-pyridylalkylamines for controlling animal growth 失效
标题翻译：用于控制动物生长的杂芳基乙醇 - 吡啶基烷基胺
公开(公告)号：US5028617A
公开(公告)日：1991-07-02
申请号：US467593
申请日：1990-01-19
申请人： Hans Lindel , Werner Hallenbach , Friedrich Berschauer , Heinrich A. Greife , Gernot Klotz
发明人： Hans Lindel , Werner Hallenbach , Friedrich Berschauer , Heinrich A. Greife , Gernot Klotz
IPC分类号： A23K1/16 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P3/04 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/73 , C07D213/80
CPC分类号： C07D213/64 , C07D213/38 , C07D213/61 , C07D213/65 , C07D213/73 , C07D213/80
摘要： A compound for promoting livestock production and for controlling obesity in humans and animals, of the formula ##STR1## in which A represents .dbd.CH-- or .dbd.N--,R.sup.0 represents hydrogen or methyl,R.sup.1 and R.sup.3 each independently represents hydrogen, hydroxyl, halogen, cyano, alkyl, halogenoalkyl, hydroxyalkyl, alkoxycarbonyl, aminocarbonyl, mono- and dialkylaminocarbonyl, alkoxy, halogenoalkoxy, halogenoalkylthio, NHSO.sub.2 -alkyl,R.sup.2 represents hydrogen, hydroxyl, alkoxy or the radical --NR.sup.5 R.sup.6,R.sup.4 represents hydrogen, C.sub.1 -C.sub.10 -alkyl which is optionally substituted by hydroxyl, halogen, alkoxy, acyloxy or the radical --NH.sup.7 R.sup.8, or represents the radical COR.sup.9 or the radical --O--Z--R.sup.10,Z represents C.sub.1 -C.sub.10 -alkylene, -alkenylene or alkynylene,R.sup.5 represents hydrogen or alkyl,R.sup.6 represents hydrogen, alkyl, halogenoalkyl or acyl, or R.sup.5 and R.sup.6 together with the adjoining N atom form a saturated or unsaturated heterocyclic 4-, 5- or 6-membered ring,R.sup.7 and R.sup.8 each independently represents hydrogen, optionally substituted alkyl, optionally substituted aryl,R.sup.9 represents hydroxyl, alkoxy or the radical --NR.sup.7 R.sup.8,R.sup.10 represents hydroxyl, alkoxy, acyloxy, optionally substituted aryloxy or aralkyloxy,with the substituent R.sup.4 and the alkylamino group in the pyridyl ring of the formula I being in the p position with respect to one another, or a physiologically tolerated salt thereof, or, if A represents nitrogen, optionally the N-oxide thereof.
摘要翻译：一种用于促进家畜生产和控制人和动物肥胖的化合物，其中A表示= CH-或= N-，R0表示氢或甲基，R1和R3各自独立地表示氢，羟基，卤素，氰基，烷基，卤代烷基，羟基烷基，烷氧基羰基，氨基羰基，一烷基氨基羰基和二烷基氨基羰基，烷氧基，卤代烷氧基，卤代烷硫基，NHSO2-烷基，R2代表氢，羟基，烷氧基或基-NR5R6，R4代表氢，C1- 任选被羟基，卤素，烷氧基，酰氧基或基团-NH 7 R 8取代的C 10 - 烷基，或表示基团COR 9或基团-OZ-R 10，Z表示C 1 -C 10 - 亚烷基， - 亚烯基或亚炔基，R 5表示氢或烷基，R 6表示氢，烷基，卤代烷基或酰基，或R 5和R 6与相邻的N原子一起形成饱和或不饱和的4-，5-或6-元环，R 7和R 8各自独立地表示氢，取代的烷基，任选取代的芳基，R 9表示羟基，烷氧基或基团-NR 7 R 8，R 10表示羟基，烷氧基，酰氧基，任选取代的芳氧基或芳烷氧基，式I的吡啶环中的取代基R4和烷基氨基在相对于彼此的p位置或其生理上耐受的盐，或者如果A表示氮，则任选地其N-氧化物。

6. 发明授权

US4895950A 5-halogeno-6-amino-nicotinic acid halides 失效
标题翻译： 5-卤代-6-氨基烟酰卤
公开(公告)号：US4895950A
公开(公告)日：1990-01-23
申请号：US216047
申请日：1988-07-07
申请人： Hans Lindel , Werner Hallenbach
发明人： Hans Lindel , Werner Hallenbach
IPC分类号： C07D213/75 , C07D213/73 , C07D213/74 , C07D213/78 , C07D401/04
CPC分类号： C07D213/73 , C07D213/78
摘要： Novel 5-halogeno-6-amino-nicotinic acid halides of the formula ##STR1## in which R represents hydrogen or alkyl,R.sup.1 represents hydrogen, alkyl or acyl orR and R.sup.1, together with the nitrogen atom to which they are bonded, represent an optionally substituted heterocyclic radical,R.sup.2 represents halogen andHal represents halogen,are prepared by halogenating the corresponding nicotinic acids. The Co Hal moiety is converted to CH.sub.3 by reaction withR.sup.3 OMgCR.sup.4 (COOR.sup.3).sub.2 (IV)in whichR.sup.3 represents C.sub.1-3 alkyl andR.sup.4 represents hydrogen or C.sub.1 -C.sub.2 -alkyl,and then hydrolyzing and decarboxylating the product.
摘要翻译：式（I）的新的5-卤代-6-氨基烟碱酰卤，其中R表示氢或烷基，R 1表示氢，烷基或酰基或R和R 1与它们所在的氮原子一起表示任选取代的杂环基，R2表示卤素，Hal表示卤素，通过卤化相应的烟酸制备。通过与R 3表示C 1-3烷基和R 4表示氢或C 1 -C 2 - 烷基的R 3 OMgCR 4（COOR 3）2（Ⅳ）反应将Co Hal部分转化成CH3，然后水解和脱羧产物。

7. 发明授权

US4740520A Use of thienylurea derivatives as selective fungicides 失效
标题翻译：使用噻吩脲衍生物作为选择性杀真菌剂
公开(公告)号：US4740520A
公开(公告)日：1988-04-26
申请号：US931293
申请日：1986-11-14
申请人： Werner Hallenbach , Hans Lindel , Wilhelm Brandes
发明人： Werner Hallenbach , Hans Lindel , Wilhelm Brandes
IPC分类号： A01N47/36 , C07D333/38 , A01N43/06
CPC分类号： A01N47/36 , C07D333/38
摘要： A method of combating fungi which comprises applying to such fungi or to a fungus habitat a fungicidally effective amount of a thienylurea derivative of the formula ##STR1## in which X is oxygen or sulphur,R is C.sub.1 -C.sub.4 -alkoxy,R.sup.1 is C.sub.3 -C.sub.4 -alkyl, andR.sup.2 and R.sup.3 each independently is C.sub.1 -C.sub.4 -alkyl and one of them may also be hydrogen.
摘要翻译：一种防治真菌的方法，其包括将杀真菌有效量的式（I）的噻吩基脲衍生物（其中X为氧或硫），R为C1-C4-烷氧基，R1为C3- C 4 - 烷基，R 2和R 3各自独立地为C 1 -C 4 - 烷基，并且它们之一也可以是氢。

8. 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）。

9. 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）。

10. 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。

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