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公开(公告)号:KR810000071B1
公开(公告)日:1981-02-12
申请号:KR770000946
申请日:1977-04-20
Applicant: HOECHST AG
Inventor: RAETHER W , WINKELMANN E
IPC: A61K31/415 , C07D233/94
Abstract: Title compds. (I; A = O, S; R1 = methyl or ethyl; R2 = H, methyl or halogen), useful as protozoacides, were prepd. by the reaction of II(X= halogen, acyloxy, arylsulfonyloxy) and III(Y= H, alkali metal or ammonium). Thus, 14.0 g 4-methyl-mercaptophenol and 19.0 g 1-ethyl-2-chloro-methyl-5-nitroimidazole were stirred at 25≦̸C in DMF soln. in the presence of K2CO3 to give 17.0 g 1-ethyl-2-(4-methyl-thiophenyloxy-methyl)-5-nitroimidazole.
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公开(公告)号:KR800001476B1
公开(公告)日:1980-12-17
申请号:KR760000122
申请日:1976-01-16
Applicant: HOECHST AG
Inventor: WINKELMANN E , RAETHER W
IPC: A61K31/40 , C07D233/95
Abstract: Title compds. (I, A = S or -SO-; R = C1-3 alkyl), useful as protozoaides, were prepd. by reacting nitro-imidazole(II; X = halogen, acyloxy, acryloxysulfonyloxy) and phenol(III; Y = H, alkaline metal ion or ammonium) or by alkylating nitroimidazole(IV) or by oxidizing I(A = S) to I(A = -SO-). Thus, 4-methylmercapto-phenol of 1-1:1-methyl-2-(4-methylthiophenyl-oxyethyl)-5-nitro-imidazole dissolved in DMF, powdered K2CO3 and 1-methyl-2-chloromethyl-5-nitro-imidazole were mixed under 35≦̸C to give 1-methyl-2-(4-methylthiophenyl-oxymethyl)-nitro-imdazole(m.p. 116≦̸C).
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公开(公告)号:KR800001147B1
公开(公告)日:1980-10-14
申请号:KR770000423
申请日:1977-02-24
Applicant: HOECHST AG
Inventor: WINKELMANN E
IPC: C07D207/333
Abstract: Title imidazoles (I, R1 = methyl, R2 = methylsulfonyl, ethylsulfonyl, R3 = H, methyl, halogen) are prepd. by oxidation of 1-methyl-2-(penoxymethyl)-5-nitroimidazoles (II, A = sulfur atom, sulfoxide group(-s) at 40o-60oC in solvent. Thus, 27.9g l-methyl-2-(4-methylthio-phenoxy-methyl)-5-nitroimidazole) was dissolved in 250ml acetic anhydride and heated with 30% hydroperoxide 24.3g at 60oC for 1hr. to give 29g 1-methyl-2-(4-methylsulfonyl-phenoxymethyl)-5-nitroimidazole.
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公开(公告)号:KR800001264B1
公开(公告)日:1980-10-26
申请号:KR800001554
申请日:1980-04-15
Applicant: HOECHST AG
Inventor: WINKELMANN E , RAETHER W
IPC: C07D233/66
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公开(公告)号:KR800001248B1
公开(公告)日:1980-10-25
申请号:KR750001508
申请日:1975-07-09
Applicant: HOECHST AG
Inventor: RAETHER W , WINKELMANN E
IPC: C07D233/66
Abstract: 1-Alky1-2-(phenoxymethy1)-5-nitroimidazoles (I; R1 = methy1, ethy1; R2 = trifluoromethy1, trichloromethy1, nitro, cyano, methylsulfony1, ethylsulfony1; R3 = H, F, Cl, Br, I, trifluoromethy1, trichloromethy1, cyano, nitro; X = halogen, acyloxy, arylsulfonyloxy), useful as protozoacides(no data), were prepd. by reaction of alky1-2-halogenomethy1-5-nitroimidazole(II) with phenol derivs.(III).
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公开(公告)号:NZ205906A
公开(公告)日:1986-06-11
申请号:NZ20590683
申请日:1983-10-10
Applicant: HOECHST AG
Inventor: WINKELMANN E , DURCKHEIMER W , RAETHER W
IPC: A61K31/435 , C07D219/06 , C07D219/08 , C07D219/00 , C07D401/00 , C07D241/00 , A61K31/495
Abstract: 3-Aryl-7-chloro-3,4-dihydroacridine-1,9(2H,10H)-dione 1-oximes and 1-hydrazone derivatives of the formula I (I) 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.
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公开(公告)号:DK519581A
公开(公告)日:1982-05-25
申请号:DK519581
申请日:1981-11-23
Applicant: HOECHST AG
Inventor: WINKELMANN E , RAETHER W , ROLLY H
IPC: C07C46/00 , C07C50/24 , C07C50/34 , C07D211/14 , C07D211/26 , C07D295/116 , C07C
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8.
公开(公告)号:PH12370A
公开(公告)日:1979-01-29
申请号:PH18793
申请日:1976-08-16
Applicant: HOECHST AG
Inventor: RAETHER W , WINKELMANN E
IPC: C07D233/94 , A61K31/415 , C07D233/54
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公开(公告)号:ZA764098B
公开(公告)日:1977-09-28
申请号:ZA764098
申请日:1976-07-09
Applicant: HOECHST AG
Inventor: WINKELMANN E , RAETHER W
IPC: C07D233/94 , C07D , A61K
Abstract: New 1-methyl-2-phenoxymethyl-5-nitro-imidazoles of formula (I): (where A is S or SO; R is 1-3C alkyl). Cpds. (I) are antiprotozoal agents esp. useful for treating trichomoniasis and amoebiasis. They also have antibacterial and antifungal activity. A typical cpd. is (I; A=S, R=Me). In an example, this is prepd. by reacting 4-methylthiophenol with 1-methyl-2-chloromethyl-5-nitro-imidazole.
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公开(公告)号:ZA7604098B
公开(公告)日:1977-09-28
申请号:ZA7604098
申请日:1976-07-09
Applicant: HOECHST AG
Inventor: WINKELMANN E , RAETHER W
IPC: C07D233/94 , C07D , A61K
CPC classification number: C07D233/94 , Y02A50/486
Abstract: New 1-methyl-2-phenoxymethyl-5-nitro-imidazoles of formula (I): (where A is S or SO; R is 1-3C alkyl). Cpds. (I) are antiprotozoal agents esp. useful for treating trichomoniasis and amoebiasis. They also have antibacterial and antifungal activity. A typical cpd. is (I; A=S, R=Me). In an example, this is prepd. by reacting 4-methylthiophenol with 1-methyl-2-chloromethyl-5-nitro-imidazole.
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