公开(公告)号：US3884913A

公开(公告)日：1975-05-20

申请号：US42597973

申请日：1973-12-19

申请人： HOECHST AG

发明人： WINKELMANN ERHARDT ,  RAETHER WOLFGANG

IPC分类号： C07D417/12 ,  C07D295/30 ,  C07D49/36 ,  C09B23/00

CPC分类号： C07D295/30

摘要： 4-(1''-ALKYL-5''-NITROIMIDAZOLYL-2''-METHYLENE-IMINO)-TETRAHYDRO1,4-THIAZINE 1,1-DIOXIDES OF THE FORMULA

IN WHICH R1 is hydrogen, methyl, ethyl, or 2-hydroxy-ethyl and R2 is hydrogen, methyl, ethyl or methoxymethyl, are prepared by reaction of 1-alkyl-5-nitroimidazolyl-2-aldehyde or a functional derivative thereof with 4-amino-tetrahydro-1,4-thiazine 1,1dioxide. The products of the invention are suitable for the treatment of protozoal diseases.

摘要翻译： 其中R1是氢，甲基，乙基或2-甲氧基的4-（1'-烷基-5'-硝基咪唑烷基-2'-甲基 - 亚氨基） - 四氢-1,4-噻唑锌1,1-二氧化物， 羟基 - 乙基和R2是氢，甲基，乙基或甲氧基甲基，是通过1-烷基-5-硝基咪唑基-2-醛或其官能衍生物与4-氨基 - 四氢-1,4-噻嗪1,1 二氧化物。 本发明的产品适用于治疗原生动物疾病。

公开(公告)号：US3903081A

公开(公告)日：1975-09-02

申请号：US42597373

申请日：1973-12-19

申请人： HOECHST AG

发明人： WINKELMANN ERHARDT ,  RAETHER WOLFGANG

IPC分类号： C07D233/91 ,  A23K1/16 ,  A61K31/495 ,  C07D295/30 ,  C07D403/14 ,  C07D49/36 ,  C09B55/00

CPC分类号： C07D295/30 ,  A61K31/495

摘要： 1,4-BIS-(5''-NITROIMIDAZOLYL-2''-METHYLENE-IMINO) PIPERAZINES OF THE FORMULA

IN WHICH R1 is hydrogen, methyl, ethyl or 2-hydroxyethyl and R2 is hydrogen or methyl, are prepared by reaction of 5-nitroimidazolyl-2-aldehydes or the functional derivatives thereof with 1,4-diamino-piperazines. The products of the invention are suitable for the treatment of protozoal diseases.

摘要翻译： 其中R 1为氢，甲基，乙基或2-羟基乙基，R 2为氢或甲基的式（I）化合物的1,4-双 - （5'-硝基咪唑-2-基甲基亚氨基）哌嗪通过5- 硝基 - 咪唑基-2-醛或其功能衍生物与1,4-二氨基 - 哌嗪。 本发明的产品适用于治疗原生动物疾病。

公开(公告)号：US3905985A

公开(公告)日：1975-09-16

申请号：US47699074

申请日：1974-06-06

申请人： HOECHST AG

发明人： WINKELMANN ERHARDT ,  RAETHER WOLFGANG

IPC分类号： C07D401/12 ,  A61K31/44 ,  C07D213/70

CPC分类号： A61K31/44

摘要： New 1-alkyl-2-(pyridyl-sulfinylmethyl)-5-nitro-imidazoles and 1alkyl-2-(pyridyl-sulfonylmethyl)-5-nitro-imidazoles are described according to the formula I

in which R stands for a methyl, ethyl or hydroxyethyl group and Z stands for a -SO- or -SO2- group and the pyridine ring is linked to the sulfinyl or the sulfonyl group in 2, 3 or 4 position as well as a process for their manufacture. The novel compounds have a pronounced activity against protozoae, especially trichomonads and amebae.

摘要翻译： 根据式I描述新的1-烷基-2-（吡啶基 - 亚磺酰基甲基）-5-硝基 - 咪唑和1-烷基-2-（吡啶基 - 磺酰基甲基）-5-硝基 - 咪唑，其中R代表甲基 乙基或羟乙基，Z代表-SO-或-SO2-基团，吡啶环连接于2,3或4位的亚磺酰基或磺酰基，以及其制备方法。

公开(公告)号：US3900482A

公开(公告)日：1975-08-19

申请号：US42608173

申请日：1973-12-19

申请人： HOECHST AG

发明人： WINKELMANN ERHARDT ,  RAETHER WOLFGANG

IPC分类号： C07D401/12 ,  A23K1/16 ,  C07D20060101 ,  C07D31/40

CPC分类号： C07D401/06

摘要： 1-(PYRIDYL-THIOALKYL)-2-ALKYL-5-NITRO-IMIDAZOLES OF THE FORMULA

IN WHICH R1 is hydrogen, methyl or ethyl, -(CH2)n- is an alkyl chain of 2 to 4 carbon atoms which may be branched and to which the pyridyl group is linked in 2-, 3- or 4-position via a sulfur atom, are prepared by reaction of 1-( omega -halogeno-alkyl)-2alkyl-5-nitro-imidazole with mercapto-pyridine in the presence of an acid-binding agent or by reaction of 2-alkyl-5-nitro-imidazole with omega -halogeno-alkyl-thio-pyridine in the presence of an acid-binding agent or with omega -hydroxy-alkyl-thio-pyridine in the presence of a condensation agent or with an aryl-sulfonyloxyalkyl-thio-pyridine. The products of the invention are suitable for the treatment of protozoal diseases.

公开(公告)号：US3639412A

公开(公告)日：1972-02-01

申请号：US3639412D

申请日：1969-05-26

申请人： HOECHST AG

发明人： SCHORR MANFRED ,  MIETH HUBERT ,  RAETHER WOLFGANG

IPC分类号： C07D213/83 ,  C07D31/50

CPC分类号： C07D213/83

摘要： THIOISINICOTINIC ACID AMIDES OF THE FORMULA:

4-((4-(CL-),X-PHENYL)-CH2-CH(-(CH2)N-(Y-1,4-PHENYLENE)-

CL)-CH2-NH-C(=S)-)PYRIDINE

IN WHICH X AND Y ARE HYDROGEN OR CHLORINE AND N STANDS FOR ZERO OR ONE, HAVE BEEN FOUND TO HAVE CHEMOTHERAPEUTIC ACTIVITY AGAINST INFECTIONS CAUSED BY PROTOZOA.

公开(公告)号：US3621013A

公开(公告)日：1971-11-16

申请号：US3621013D

申请日：1969-03-28

申请人： HOECHST AG

发明人： WINKELMANN ERHARDT ,  RAETHER WOLFGANG

IPC分类号： C07D295/195 ,  C07D87/38

CPC分类号： C07D295/195

摘要： Formamidine derivatives of diphenyl-sulfone which are effective medicaments against malaria are prepared by reacting 4,4'' diamino-diphenyl-sulfone of the formula

WITH N-formyl compounds of the formula

IN WHICH -N Z is a pyrrolidino, piperidino or morpholino radical, in the presence of acid halides and, if desired, converting the salts thus obtained into the free bases.

公开(公告)号：US3922344A

公开(公告)日：1975-11-25

申请号：US46013274

申请日：1974-04-11

申请人： HOECHST AG

发明人： RAETHER WOLFGANG ,  DIERY HELMUT ,  CUNTZE ULRICH

IPC分类号： A01N57/12 ,  C07F9/141 ,  C07F9/44 ,  A01N9/36

CPC分类号： C07F9/1411

摘要： Compounds of the formula I

IN WHICH R1 stands for hydrogen or methyl, R2, R3, R4, R5 and R6 which may be identical or different, each stands for hydrogen or alkyl radicals of 1 to 4 carbon atoms, R7 stands for an alkyl or alkenyl radical of 8 to 18 carbon atoms, n is an integer of 2 or 3 and m is zero or an integer from 1 to 4, having an excellent action against pathogenic bacteria and protozoans especially against oocyst of coccidia when they are used in mixture with one or several chlorinated hydrocarbons.

摘要翻译： 式I OR2R4R6的化合物：其中R1代表氢或甲基，R2代表氢，甲基，R2，R2， ，可以相同或不同的R 3，R 4，R 5和R 6各自代表氢或1至4个碳原子的烷基，R7代表8至18个碳原子的烷基或烯基，n是2的整数 或3，m为0或1至4的整数，当与一种或几种氯代烃混合使用时，具有优异的抗病原菌和原生动物的作用，特别是针对球虫的卵囊。

公开(公告)号：US3922277A

公开(公告)日：1975-11-25

申请号：US52391774

申请日：1974-11-14

申请人： HOECHST AG

发明人： WINKELMANN ERHARDT ,  RAETHER WOLFGANG

IPC分类号： C07D401/12

CPC分类号： C07D401/12

摘要： (1-Alkyl-5-nitro-imidazolyl-2-alkyl)-pyridyl-sulfides, sulfoxides and -sulfones of the formula I

in which R1 represents methyl or ethyl, R2 represents a hydrogen atom or methyl, Z represents a sulfide group (-S-), a sulf-oxide group (-SO-) or a sulfone group (-SO2-), which may be linked with the pyridine ring in the 2-, 3- or 4-position, and in which R3 represents a halogen atom, a cyano or nitro group, and process for preparing them. The compounds are active against trichomonas and amebas.

摘要翻译： （1-烷基-5-硝基 - 咪唑基-2-烷基） - 吡啶基 - 硫化物，式Ⅰ化合物，其中R1代表甲基或乙基，R2代表氢原子或甲基，Z代表硫化物基团 （-S-），亚硫氧烷基（-SO-）或砜基（-SO 2 - ），其可以与2-，3-或4-位的吡啶环连接，并且其中R 3 表示卤素原子，氰基或硝基，以及它们的制备方法。 这些化合物对滴虫和安息日是有效的。

公开(公告)号：US3907816A

公开(公告)日：1975-09-23

申请号：US47066674

申请日：1974-05-16

申请人： HOECHST AG

发明人： WINKELMANN ERHARDT ,  RAETHER WOLFGANG

IPC分类号： C07D233/93 ,  E05G7/00 ,  C07D213/70

CPC分类号： C07D233/93

摘要： This invention provides 1-alkyl-2-(pyridylthiomethyl)-5-nitroimidazoles and 1-alkyl-2-(N-oxy-pyridylthiomethyl)-5-nitroimidazoles of the formula

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： 本发明提供式-CH 2 -S-（I）O 2 N的1-烷基-2-（吡啶基硫甲基）-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，吡啶基和N-氧 - 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。