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1. 发明授权

US6114351A N-oxides as antibacterial agents 失效
标题翻译： N-氧化物作为抗菌剂
公开(公告)号：US6114351A
公开(公告)日：2000-09-05
申请号：US952762
申请日：1997-11-19
申请人： Hubert Rast , Martin Scheer , Werner Hallenbach
发明人： Hubert Rast , Martin Scheer , Werner Hallenbach
IPC分类号： A23K20/195 , A61K31/47 , A61K31/535 , A61P31/04 , C07D215/56 , C07D215/58 , C07D471/08 , C07D471/14 , C07D487/08 , C07D498/06 , C07D519/00 , A01N43/42 , C07D215/16
CPC分类号： C07D215/56 , C07D471/08 , C07D487/08
摘要： The present invention relates to new antibacterial compositions, in particular orally administrable compositions, based on N-oxides of saturated nitrogen-containing heterocycles which are substituted by quinolonecarboxylic acids or naphthyridonecarboxylic acids, and to new active compounds and their preparation.
摘要翻译： PCT No.PCT / EP96 / 02171 Sec。 371日期：1997年11月19日 102（e）日期1997年11月19日PCT提交1996年5月20日PCT公布。 WO96 / 38417 PCT出版物日本1996年12月5日本发明涉及基于被喹诺酮羧酸或萘啶酮羧酸取代的饱和含氮杂环的N-氧化物的新型抗菌组合物，特别是可口服给药的组合物，以及新的活性化合物及其制备方法。

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

US4845262A Novel arylethanolamines for promoting livestock production 失效
标题翻译：用于促进畜牧生产的新型芳基乙醇胺
公开(公告)号：US4845262A
公开(公告)日：1989-07-04
申请号：US89691
申请日：1987-08-25
申请人： Hans Lindel , Werner Hallenbach , Friedrich Berschauer , Anno de Jong , Martin Scheer
发明人： Hans Lindel , Werner Hallenbach , Friedrich Berschauer , Anno de Jong , Martin Scheer
IPC分类号： A23K1/16 , A61K31/135 , A61K31/275 , A61P3/00 , C07C67/00 , C07C255/58 , C07C255/59 , C07C313/00 , C07C315/04 , C07C317/48 , C07C317/50
CPC分类号： C07C255/00 , A23K20/111
摘要： The growth of livestock is promoted by the novel arylethanolamines of the formula ##STR1## in which R.sup.1 represents cyano,R.sup.2 represents amino, alkylamino or acylamino,R.sup.3 represents hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, hydroxymethyl, nitro or methylsulphonylmethyl,R.sup.4 represents hydrogen, alkyl or acyl,R.sup.5 represents hydrogen or alkyl,R.sup.6 represents alkyl,n represents 1, 2 or 3,R.sup.7 represents the radicals --COR.sup.9, --O-alkylene-COR.sup.9, -alkylene-R.sup.10 or --O-alkylene-R.sup.10,R.sup.8 represents hydrogen, alkyl or halogen,R.sup.9 represents hydroxyl, alkoxy or the radical --NR.sup.11 R.sup.12,R.sup.10 represents hydroxyl, alkoxy or the radical NR.sup.11 R.sup.12,R.sup.11 represents hydrogen or alkyl, andR.sup.12 represents hydrogen or alkyl,and the physiologically acceptable salts thereof.
摘要翻译：通过式（I）的新型芳基乙醇胺促进家畜的生长，其中R1代表氰基，R2代表氨基，烷基氨基或酰氨基，R3代表氢，卤素，烷基，卤代烷基，烷氧基，卤代烷氧基，羟基甲基，硝基或甲基磺酰基甲基，R 4表示氢，烷基或酰基，R 5表示氢或烷基，R 6表示烷基，n表示1,2或3，R 7表示基团-COR 9，-O-亚烷基-CON 9， - 亚烷基-R 10或-O - 亚烷基-R 10，R 8表示氢，烷基或卤素，R 9表示羟基，烷氧基或基团-NR 11 R 12，R 10表示羟基，烷氧基或基团NR 11 R 12，R 11表示氢或烷基，R 12表示氢或烷基，其可接受的盐。

4. 发明授权

US4760063A Thienooxazinones, processes for their preparation, and their use as growth promoters 失效
标题翻译：噻吩并恶嗪酮，其制备方法及其作为生长促进剂的用途
公开(公告)号：US4760063A
公开(公告)日：1988-07-26
申请号：US929921
申请日：1986-11-12
申请人： Werner Hallenbach , Hans Lindel , Friedrich Berschauer , Martin Scheer , Anno de Jong
发明人： Werner Hallenbach , Hans Lindel , Friedrich Berschauer , Martin Scheer , Anno de Jong
IPC分类号： A23K1/16 , A61K31/535 , A61P15/00 , A61P15/14 , C07D333/38 , C07D333/42 , C07D333/68 , C07D333/78 , C07D498/04 , A61K31/38 , C07D265/04
CPC分类号： C07D333/38 , C07D333/68 , C07D333/78
摘要： Novel thienooxazines of the formula ##STR1## in which R.sup.1 and R.sup.2, together with the adjacent C atoms, represent an optionally substituted thiophene ring,R.sup.3 represents hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl or aryl, andR.sup.4 represents optionally substituted alkyl, cycloalkyl, alkenyl or aryl, orR.sup.3 and R.sup.4, together with the adjacent nitrogen atom, form a saturated heterocyclic structure which may optionally contain further hetero atoms,promote the yield of animals, e.g. rate of growth, ratio of meat to fat, etc. They are made from new intermediates of the formulas ##STR2## in which R.sup.5 and R.sup.6 may be hydrogen or various organic radicals, or together form a ring.
摘要翻译：式中，R1和R2与相邻的C原子一起代表任选取代的噻吩环，R3代表氢，任选取代的烷基，环烷基，烯基或芳基，R4代表任意取代的烷基，环烷基，烯基或芳基，或者R 3和R 4与相邻的氮原子一起形成饱和的杂环结构，其可以任选地含有另外的杂原子，促进动物的产量，例如生长速度，肉类与脂肪的比例等。它们是由新型的中间体，其中R5和R6可以是氢或各种有机基团，或者一起形成一个环。

5. 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。

6. 发明授权

US4863939A Heteroarylethylamine as production promoters in livestock 失效
标题翻译：杂环三乙胺作为家畜生产促进剂
公开(公告)号：US4863939A
公开(公告)日：1989-09-05
申请号：US80284
申请日：1987-07-30
申请人： Hans Lindel , Werner Hallenbach , Friedrich Berschauer , Anno de Jong , Martin Scheer
发明人： Hans Lindel , Werner Hallenbach , Friedrich Berschauer , Anno de Jong , Martin Scheer
IPC分类号： C07D213/84 , A23K20/132 , A61K31/44 , A61K31/4402 , A61K31/4412 , A61K31/4418 , A61P15/00 , C07D213/36 , C07D213/38 , C07D213/61 , C07D213/70 , C07D213/72 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/81
CPC分类号： C07D213/73 , A23K20/132 , C07D213/38 , C07D213/61
摘要： The growth of livestock is promoted by the new compounds of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, halogen, halogenoalkyl, hydroxyl, cyano, alkoxycarbonyl, aminocarbonyl, mono- and dialkylaminocarbonyl, alkoxy, halogenoalkoxy, halogenoalkylthio or NHSO.sub.2 -alkyl,R.sup.2 represents hydrogen, hydroxyl, alkoxy or the --NR.sup.11 R.sup.12 radical,R.sup.3 represents the radicals mentioned in the case of R.sup.1R.sup.4 represents hydroxyl, acyloxy or alkoxy,R.sup.5 represents hydrogen or alkyl,R.sup.6 represents hydrogen or alkyl,R.sup.7 represents hydrogen or alkyl,R.sup.8 represents hydrogen or alkyl,X represents C.sub.1 -C.sub.10 -alkylene or a direct bond,Y represents oxygen or a direct bond,R.sup.9 represents hydrogen, C.sub.1 -C.sub.10 -alkyl which is optionally substituted by hydroxyl, alkoxy, acyloxy or the --NR.sup.13 R.sup.14 radical, or represents the COR.sup.15 radical or the O--Z--R.sup.16 radical,Z represents C.sub.1 -C.sub.10 -alkylene, C.sub.1 -C.sub.10 -alkenylene or C.sub.1 -C.sub.10 -alkinylene,R.sup.10 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl or the COR.sup.15 radical,R.sup.11 represents hydrogen or alkyl,R.sup.12 represents hydrogen, alkyl, halogenoalkyl or acyl,R.sup.13 represents hydrogen, optionally substituted alkyl or optionally substituted aryl,R.sup.14 represents the radicals mentioned in the case of R.sup.13,R.sup.15 represents hydroxyl, alkoxy or the NR.sup.13 R.sup.14 radical, andR.sup.16 represents hydroxyl, alkoxy, acyloxy, the NR.sup.13 R.sup.14 radical or the COR.sup.15 radical,and the physiologically acceptable salts and N-oxides thereof. Several new intermediates are also disclosed.
摘要翻译：新型化合物“IMAGE”促进了家畜的生长，其中R1代表氢，烷基，卤素，卤代烷基，羟基，氰基，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，卤代烷硫基或NHSO2-烷基，R 2表示氢，羟基，烷氧基或-NR 11 R 12基团，R 3表示在R 4表示羟基，酰氧基或烷氧基的情况下提及的基团，R 5表示氢或烷基，R 6表示氢或烷基，R 7表示氢或烷基， R8表示氢或烷基，X表示C1-C10-亚烷基或直接键，Y表示氧或直接键，R9表示氢，任选被羟基，烷氧基，酰氧基或-NR13R14基团取代的C1-C10-烷基，或表示COR15基团或OZ-R16基团，Z表示C1-C10-亚烷基，C1-C10亚烯基或C1-C10亚烯基，R10表示氢，卤素，烷基，烷氧基，羟基或COR15基，R11 代理人 R12表示氢，烷基，卤代烷基或酰基，R13表示氢，任选取代的烷基或任选取代的芳基，R 14表示在R 13的情况下提及的基团，R 15表示羟基，烷氧基或NR 13 R 14基，R 16 表示羟基，烷氧基，酰氧基，NR 13 R 14基或COR 15基，及其生理上可接受的盐和N-氧化物。还披露了几个新的中间体。

7. 发明授权

US5808076A Orally administrable formulations of quinolone- or naphthyridonecarboxylic acids 失效
标题翻译：口服给药的喹诺酮或萘啶酮羧酸的制剂
公开(公告)号：US5808076A
公开(公告)日：1998-09-15
申请号：US761687
申请日：1996-12-06
申请人： Oliver Vetter , Reinhold Lohr , Matthias Kuhn , Hubert Rast , Martin Scheer , Ernst Heinen , Francisco Cabrera
发明人： Oliver Vetter , Reinhold Lohr , Matthias Kuhn , Hubert Rast , Martin Scheer , Ernst Heinen , Francisco Cabrera
IPC分类号： A61K31/47 , A61K31/19 , A61K31/194 , A61K31/4375 , A61K31/495 , A61K31/496 , A61P33/00 , C07D215/16
CPC分类号： A61K31/496
摘要： The present invention relates to the preparation of orally administrable formulations of quinolone- or naphthyridonecarboxylic acids by mixing quinolone- or naphthyridonecarboxylic acids as such or in the form of their water-soluble salts or derivatives, preferably in the form of their aqueous salt solutions, with embonic acid as such or in the form of its water-soluble salts or derivatives, preferably in the form of its aqueous salt solutions, in the presence of an excipient, optionally in the presence of auxiliaries, when using dry mixtures in the presence of water, and optionally converting the mixture obtained into further ready-to-use forms.
摘要翻译：本发明涉及通过将喹诺酮或萘啶酮羧酸本身混合或以其水溶性盐或衍生物的形式，优选以其盐水溶液的形式，通过混合喹诺酮或萘啶酮羧酸的口服给药制剂，或者以其水溶性盐或衍生物的形式，优选以其盐水溶液的形式，在赋形剂存在下，任选地在助剂的存在下，当在水存在下使用干混合物时，，并且任选地将所获得的混合物转化成另外的即用形式。

8. 发明授权

US5152986A Preparation and use of ion exchange resins loaded with quinolonecarboxylic acid derivatives 失效
标题翻译：离子交换树脂与喹啉羧酸衍生物的制备和使用
公开(公告)号：US5152986A
公开(公告)日：1992-10-06
申请号：US426123
申请日：1989-10-24
申请人： Peter M. Lange , Alfred Mitschker , Arundev H. Naik , Hubert Rast , Martin Scheer , Herbert Voege
发明人： Peter M. Lange , Alfred Mitschker , Arundev H. Naik , Hubert Rast , Martin Scheer , Herbert Voege
IPC分类号： C08J5/20 , A23K1/00 , A23K1/16 , A61K9/00 , A61K9/18 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/535 , A61K47/30 , A61K47/48 , B01J39/18 , B01J41/12
CPC分类号： A61K47/48184 , A61K31/44 , A61K31/47 , A61K31/535
摘要： Known antibacterial quinolonecarboxylic acid derivatives such as ciprofloxacin are administered to animals in their food in the form of weak cation exchangers loaded therewith. The taste is much improved and the animals accept the material more readily.
摘要翻译：将已知的抗菌喹诺酮羧酸衍生物如环丙沙星以其负载的弱阳离子交换剂的形式施用于其食物中的动物。味道大大改善，动物更容易接受材料。

9. 发明授权

US4678797A Biologically active agents containing substituted isoxazolidines 失效
标题翻译：含有取代异恶唑烷的生物活性剂
公开(公告)号：US4678797A
公开(公告)日：1987-07-07
申请号：US733449
申请日：1985-05-10
申请人： Axel Ingendoh , Friedrich Berschauer , Benedikt Becker , Wilhelm Stendel , Bernhard Homeyer , Martin Scheer , Anno de Jong , Gerd Hanssler , Paul Reinecke
发明人： Axel Ingendoh , Friedrich Berschauer , Benedikt Becker , Wilhelm Stendel , Bernhard Homeyer , Martin Scheer , Anno de Jong , Gerd Hanssler , Paul Reinecke
IPC分类号： A01N43/80 , A23K1/16 , A61K31/42 , A61K31/44 , A61P3/00 , A61P33/00 , C07C67/00 , C07C209/00 , C07C211/52 , C07C239/00 , C07C239/08 , C07D261/02 , C07D317/00 , C07D413/04
CPC分类号： C07D261/02 , A01N43/80 , A23K20/137 , C07D413/04
摘要： Substituted isoxazolidines of the formula ##STR1## in which R.sup.1 represents optionally substituted alkyl, cycloalkyl, aralkyl, aryl or heteroaryl or radicals of the formula --COR.sup.4,R.sup.4 represents optionally substituted alkyl, aryl, alkoxy, alkylthio, aroxy, arylthio, amino, alkylamino, dialkylamino, arylamino, arylalkylamino, diarylamino or cycloalkylamino, or optionally substituted heterocyclic radicals which are bonded via nitrogen,R.sup.2 represents hydrogen or the radicals mentioned for R.sup.1, it being possible for R.sup.1 and R.sup.2 to be identical or different, andR.sup.3 represents optionally substituted alkyl, cycloalkyl, alkenyl, alkinyl or aryl, or saturated heterocyclic radicals, which are optionally substituted,and acid salts thereof, are pesticidally active and increase animals' utilization of feed. Intermediates therefor are also new.
摘要翻译：取代的式“IMAGE”的异恶唑烷，其中R 1表示任选取代的烷基，环烷基，芳烷基，芳基或杂芳基或式-COR 4的基团，R 4表示任选取代的烷基，芳基，烷氧基，烷硫基，芳氧基，芳硫基，氨基，，二烷基氨基，芳基氨基，芳基烷基氨基，二芳基氨基或环烷基氨基，或通过氮键合的任选取代的杂环基，R 2表示氢或R1所述的基团，R 1和R 2可以相同或不同，并且R 3表示任选取代烷基，环烷基，烯基，炔基或芳基，或任选被取代的饱和杂环基，及其酸式盐是杀虫活性的并增加动物饲料的利用。中间体也是新的。

10. 发明授权

US4261988A Chromanone derivatives 失效
标题翻译：色酮衍生物
公开(公告)号：US4261988A
公开(公告)日：1981-04-14
申请号：US20119
申请日：1979-03-13
申请人： Arno Widdig , Hans-Joachim Kabbe , Martin Scheer , Rudiger Sitt
发明人： Arno Widdig , Hans-Joachim Kabbe , Martin Scheer , Rudiger Sitt
IPC分类号： A61K31/35 , A61K31/352 , A61P19/06 , C07D311/22 , C07D311/24 , C07D311/32 , C07D311/92 , C07D311/96 , C07D405/04 , C07D491/10 , C07D491/107
CPC分类号： C07D491/10 , C07D311/22 , C07D311/24 , C07D311/32 , C07D311/92 , C07D311/96
摘要： Compounds useful in the treatment of cholesterolaemia are of the general formula ##STR1## or salts thereof in which R.sup.1 and R.sup.2 independently denote radicals including hydrogen, alkyl, aryl and heterocyclic radical or together complete a carbocyclic or heterocylic ring, R.sup.3 denotes a radical ##STR2## in which R.sup.9, R.sup.10 and R.sup.11 include hydrogen, cyano, nitro, alkyl and aryl or, in pairs, complete carbocyclic rings, X denotes cyano, nitro or substituted carbonyl, sulphonyl or phosphonyl group, R.sup.4 is hydrogen or a radical defined for R.sup.1 or R.sup.3, and R.sup.5, R.sup.6, R.sup.7 and R.sup.8 include hydrogen, nitro, cyano, carboxyl, alkyl and aryl or, in pairs, complete carbocyclic rings, with the proviso that R.sup.1 and R.sup.9 are not both phenyl if X denotes CO--C.sub.6 H.sub.6. The compounds exhibit considerably higher hypocholesterolaemic activity than the known clofibrate and in addition exhibit a pronounced nutritive effect, e.g., in a medicated fodder or premix.
摘要翻译：用于治疗胆固醇血症的化合物具有通式（I）或其盐，其中R 1和R 2独立地表示包括氢，烷基，芳基和杂环基团的基团，或者一起完成碳环或杂环，R3表示其中R9，R10和R11包括氢，氰基，硝基，烷基和芳基，或成对地成为完全碳环，X表示氰基，硝基或取代的羰基，磺酰基或膦酰基，R4是氢或基团对于R 1或R 3而言，R 5，R 6，R 7和R 8包括氢，硝基，氰基，羧基，烷基和芳基，或成对地成为完全碳环，条件是如果X表示CO，则R 1和R 9不是苯基 -C6H6。化合物显示比已知的氯贝特明显更高的降血胆固醇血症活性，并且还显示出明显的营养作用，例如在药物饲料或预混物中。

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