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41. 发明授权

US4782056A 2-phenylhexahydro-1,2,4-triazine-3-,5-diones 失效
标题翻译： 2-苯基六氢-1,2,4-三嗪-3-，5-二酮
公开(公告)号：US4782056A
公开(公告)日：1988-11-01
申请号：US903752
申请日：1986-09-05
申请人： Manfred Rosner , Wolfgang Raether
发明人： Manfred Rosner , Wolfgang Raether
IPC分类号： A23K1/16 , A61K31/53 , A61P31/00 , A61P33/02 , C07D253/06 , C07D253/075
CPC分类号： C07D253/06
摘要： Compounds of the formula I ##STR1## with n=1-3, R=H, Hal, CF.sub.3, alkyl, cycloalkyl, alkyloxy, alkylthio, alkylsulfinyl, alkylsulfonyl, benzylsulfinyl, benzylsulfonyl, nitro, cyano, amino, alkylamino, dialkylamino, piperidino, morpholino, pyrrolidinyl, 4-methyl-1-piperazinyl, acylamino or substituted phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, benzoyl, benzoylamino or anilino, with R.sup.2 =H, alkyl, cycloalkyl, optionally substituted benzyl, alkanoyl or benzoyl and R.sup.3 =H, alkyl, cycloalkyl or optionally substituted benzyl, at least R.sup.2 or R.sup.3 not being H, are obtained by alkylation or acylation of a compound II ##STR2## in which R.sup.1 is as defined above, with compounds R.sup.3 X (X=leaving group) or R.sup.2 Y (Y=leaving group), R.sup.2 and R.sup.3 being defined as indicated.Compounds I are coccidiostatics.
摘要翻译：式I的化合物其中n = 1-3，R = H，Hal，CF 3，烷基，环烷基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，苄基亚磺酰基，苄基磺酰基，硝基，氰基，氨基，烷基氨基，二烷基氨基，哌啶子基，吗啉代，吡咯烷基，4-甲基-1-哌嗪基，酰基氨基或取代的苯氧基，苯硫基，苯基亚磺酰基，苯基磺酰基，苯甲酰基，苯甲酰氨基或苯胺基，其中R2 = H，烷基，环烷基，任选取代的苄基，烷酰基或苯甲酰基， R3 = H，烷基，环烷基或任选取代的苄基，至少R2或R3不为H，通过化合物II（II）（其中R 1如上定义）与化合物R3X（X =离去基团）或R2Y（Y =离去基团），R2和R3如所指定。化合物I是球虫病。

42. 发明授权

US4640917A 2-phenyl-hexahydro-1,2,4-triazine-3,5-diones 失效
标题翻译： 2-苯基 - 六氢-1,2,4-三嗪-3,5-二酮
公开(公告)号：US4640917A
公开(公告)日：1987-02-03
申请号：US709798
申请日：1985-03-08
申请人： Manfred Rosner , Wolfgang Raether
发明人： Manfred Rosner , Wolfgang Raether
IPC分类号： C07D249/12 , A23K1/16 , A61K31/41 , A61K31/53 , A61P33/02 , C07D253/06 , C07D253/075 , A61K31/535 , A61K31/54
CPC分类号： C07D253/075
摘要： Substituted 2-phenyl-hexahydro-1,2,4-triazine-3,5-diones of the formula ##STR1## in which n is one, two or three and the individual substituents R are independently of one another (a) hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, alkyl having 1 to 6 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, alkoxy, alkylthio, alkylsulfinyl or alkylsulfonyl each having 1 to 6 carbon atoms in the alkyl moiety, nitro, cyano, amino, alkylamino or dialkylamino each having 1 to 12 carbon atoms in the alkyl moiety, piperidino, morpholino, thiomorpholino, 1-pyrrolidinyl, 4-methyl-1-piperazinyl or acylamino having 1 to 6 carbon atoms in the acyl moiety, or (b) a phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, benzoyl, benzoylamino or aniline radical which is in each case R.sub.(a) -substituted, and the alkali metal salts, alkaline earth metal salts or ammonium salts thereof, a process for their preparation, their use, veterinary drugs and a process for controlling protozoal diseases.
摘要翻译：式（I）的取代的2-苯基 - 六氢-1,2,4-三嗪-3,5-二酮其中n为1,2或3，各个取代基R彼此独立地为）氢，氟，氯，溴，碘，三氟甲基，具有1至6个碳原子的烷基，具有3至6个碳原子的环烷基，烷基部分中具有1至6个碳原子的烷氧基，烷硫基，烷基亚磺酰基或烷基磺酰基，硝基，氰基，氨基，烷基氨基或二烷基氨基，其在烷基部分中具有1至12个碳原子，哌啶子基，吗啉代，硫代吗啉代，1-吡咯烷基，4-甲基-1-哌嗪基或酰基部分具有1至6个碳原子的酰基氨基，或（b）在各种情况下R（a）被取代的苯氧基，苯硫基，苯基亚磺酰基，苯磺酰基，苯甲酰基，苯甲酰基氨基或苯胺基，及其碱金属盐，碱土金属盐或铵盐，其制备方法，它们的使用，兽药和控制原生动物疾病的过程 es。

43. 发明授权

US4593027A 3-aryl-7-chloro-3,4-dihydroacridine-1,9(2H,10H)-dione 1-oximes and 1-hydrazone derivatives, their salts, a process for their preparation, agents containing them and their use 失效
标题翻译： 3-芳基-7-氯-3,4-二氢吖啶-1,9（2H，10H） - 二酮1-肟和1-腙衍生物，其盐，其制备方法，含有它们的试剂及其用途
公开(公告)号：US4593027A
公开(公告)日：1986-06-03
申请号：US540647
申请日：1983-10-11
申请人： Erhardt Winklemann , Walter Durckheimer , Wolfgang Raether
发明人： Erhardt Winklemann , Walter Durckheimer , Wolfgang Raether
IPC分类号： C07D219/06 , C07D219/08 , A61K31/495 , A61K31/435 , C07D295/04 , C07D471/00
CPC分类号： C07D219/06 , C07D219/08
摘要： 3-Aryl-7-chloro-3,4-dihydroacridine-1,9(2H,10H)-dione 1-oximes and 1-hydrazone derivatives of the formula I ##STR1## and their physiologically tolerated acid addition and ammonium salts are described, as is a process for their preparation. The new compounds are chemotherapeutic agents and are active against protozoa, especially malaria plasmodia.
摘要翻译： 3-芳基-7-氯-3,4-二氢吖啶-1,9（2H，10H） - 二酮1-肟和式I的1-腙衍生物（I）及其生理上耐受的酸加成和铵描述了盐，以及它们的制备方法。新化合物是化学治疗剂，对抗原生动物，特别是疟疾疟原虫是有活性的。

44. 发明授权

US4042705A 1-Methyl-2-(phenyl-oxymethyl)-5-nitro-imidazoles and process for their manufacture 失效
标题翻译： 1-甲基-2-（苯基 - 氧甲基）-5-硝基 - 咪唑及其制备方法
公开(公告)号：US4042705A
公开(公告)日：1977-08-16
申请号：US704100
申请日：1976-07-09
申请人： Erhardt Winkelmann , Wolfgang Raether
发明人： Erhardt Winkelmann , Wolfgang Raether
IPC分类号： A61K31/415 , A61P31/04 , C07D233/94
CPC分类号： C07D233/94
摘要： 1-Methyl-2-(phenyl-oxymethyl)-5-nitro-imidazoles and a process for preparing them are disclosed. The compounds of the invention are suitable for the treatment of protozoal diseases caused in humans and animals and of bacteria and fungi.
摘要翻译：公开了1-甲基-2-（苯基 - 氧甲基）-5-硝基 - 咪唑及其制备方法。本发明的化合物适用于治疗在人和动物以及细菌和真菌中引起的原生动物疾病。

45. 发明授权

US3991191A Antiprotozoal (1-alkyl-5-nitro-imidazolyl-2-alkyl)-pyrimidines 失效
标题翻译：抗原生动物（1-烷基-5-硝基 - 咪唑-2-基） - 嘧啶
公开(公告)号：US3991191A
公开(公告)日：1976-11-09
申请号：US543165
申请日：1975-01-22
申请人： Erhardt Winkelmann , Akhileswer Sinharay , Wolfgang Raether
发明人： Erhardt Winkelmann , Akhileswer Sinharay , Wolfgang Raether
IPC分类号： C07D403/12 , A01N43/48 , A61K31/505 , C07D239/28
CPC分类号： A01N43/48
摘要： New (1-alkyl-5-nitro-imidazolyl-2-alkyl)-heteroaryl compounds are disclosed as well as a process for their manufacture.The new compounds are effective against pathogens, such as bacteria and protozoa, as well as against fungi.
摘要翻译：公开了新的（1-烷基-5-硝基 - 咪唑-2-基） - 杂芳基化合物及其制备方法。

46. 发明授权

US3984560A Composition for and method of treating disease caused by protozon 失效
标题翻译：治疗由原始细胞引起的疾病的组合物和方法
公开(公告)号：US3984560A
公开(公告)日：1976-10-05
申请号：US610407
申请日：1975-09-04
申请人： Erhardt Winkelmann , Wolfgang Raether
发明人： Erhardt Winkelmann , Wolfgang Raether
IPC分类号： C07D233/93 , A61K31/44
CPC分类号： C07D233/93
摘要： This invention provides 1-alkyl-2-(pyridylthiomethyl)-5-nitro-imidazoles and 1-alkyl-2-(N-oxy-pyridylthiomethyl)-5-nitro-imidazoles of the formula ##SPC1##In which R is methyl, ethyl or hydroxyethyl and the pyridyl and N-oxy-pyridyl group is linked in 2-, 3- or 4-position to the sulfur atom, as well as process for the manufacture of these compounds.The novel compounds are suitable for the treatment of protozoal diseases in mammals.
摘要翻译：本发明提供下式的1-烷基-2-（吡啶基硫基甲基）-5-硝基 - 咪唑和1-烷基-2-（N-氧 - 吡啶基硫甲基）-5-硝基 - 咪唑，其中R是甲基，乙基或羟乙基并且吡啶基和N-氧代吡啶基在2-，3-或4-位与硫原子连接，以及制备这些化合物的方法。

47. 发明授权

US3984426A (1-Alkyl-5-nitro-imidazolyl-2-alkyl)-heteroaryl compounds 失效
标题翻译：（1-烷基-5-硝基 - 咪唑-2-基） - 杂芳基化合物
公开(公告)号：US3984426A
公开(公告)日：1976-10-05
申请号：US527705
申请日：1974-11-27
申请人： Erhardt Winkelmann , Wolfgang Raether
发明人： Erhardt Winkelmann , Wolfgang Raether
IPC分类号： C07D413/12 , C07D417/12 , C07D413/00 , C07D417/00
CPC分类号： C07D417/12
摘要： (1-ALKYL-5-NITRO-IMIDAZOLYL-2-ALKYL)-HETEROARYL COMPOUNDS AND A PROCESS FOR THEIR MANUFACTURE ARE DESCRIBED. The new compounds are well compatible and are effective against bacteria and protozoa as well as against fungi. They are especially active against trichomonads and amebae.
摘要翻译：（1-烷基-5-硝基咪唑烷-2-基） - 乙酸酯化合物及其制备方法。新化合物很好地相容，对细菌和原生动物以及对真菌有效。他们对毛滴虫和阿米巴特别活跃。

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