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    • 2. 发明授权
    • Use of phenylethylamine derivatives for the antimicrobial treatment of surfaces
    • 苯乙胺衍生物用于表面抗微生物处理
    • US06846492B2
    • 2005-01-25
    • US10204520
    • 2001-02-13
    • Wolfgang HaapWerner HölzlDietmar OchsKarin PetzoldMarcel Schnyder
    • Wolfgang HaapWerner HölzlDietmar OchsKarin PetzoldMarcel Schnyder
    • A01N33/10A01N37/38A01N39/00A01N39/02A01N39/04C07C217/60C07C255/54A01N25/00A61K7/075A61K7/50C11D7/00D06L1/00
    • C07C255/54A01N33/10A01N37/38A01N39/00A01N39/02A01N39/04C07C217/60C07C2601/08
    • The use of compounds of formula (1) is described, in which compounds R1, R2 and R3 are each independently of the others hydrogen; C1-C20alkyl; C3-C7cycloalkyl; C2-C20alkenyl; C4-C7cycloalkenyl; C2-C20alkynyl, C4-C7cycloalkynyl; or unsubstituted or C1-C5alkyl-, C3-C7cylcoalkyl-, C1-C5alkoxyl-, C3-C7cycloakoxy-, halo-, oxo-, carboxy-, carboxy-C1-C7alkyl ester-, carboxy-C3-C7cylcloalkyl ester-, cyano-, trifluoromethyl-, pentafluoroethyl-, amino-, N,N-mono- or di-C1-C20alkylamino- or nitro-substituted phenyl-C1-C5alkyl, naphthyl-C1-C5alkyl, phenylcarbonyl-C1-C5alkyl, naphthylcarbonyl-C1-C5alkyl, pyrrolylalkyl, furanylalkyl, thiophenylalkyl, pyrazolylalkyl, imidazolylalkyl, oxazolylalkyl, thiazolylalkyl, isoxazolylalkyl, isothiazolylalkyl, 1,2,3-triazolylalkyl, 1,2,4-triazolylalkyl, 1,2,3-oxadiazolylalkyl, 1,3,4-oxadiazolylalkyl, 1,2,3-thiadiazolylalkyl, 1,3,4-thiadiazolylalkyl, indolylalkyl, pyridylalkyl, pyridazinylalkyl, pyrimidinylalkyl, pyridazinylalkyl, quinolinylalkyl, isoquinolinylalkyl, pyrrolyl, furanyl, thiophenyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,3-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,3-thiadiazolyl, 1,3,4-thiadiazolyl, indolyl, pyridyl, pyridazinyl, pyrimidinyl, pyridazinyl, quinolinyl or isoquinolinyl; R4, R5, R6 and R7 are each independently of the others hydrogen; C1-C20alkyl; C3-C7 cycloalky; C2-C20alkenyl; C4-C7 cycloalkenyl; C2-C20alkynyl; or C4-C7 cycloalkynyl; and m and n are each independently of the other 0 or 1, for antimicrobial treatment of surfaces. The compounds exhibit a pronounced activity against pathogenic gram-positive and gram-negative bacteria, and also against yeasts and moulds. They are accordingly suitable for the antimicrobial treatment, especially preservation and disinfection, of surfaces.
    • 描述了式(1)化合物的用途,其中化合物R1,R2和R3各自独立地为氢; C1-C20烷基; C 3 -C 7环烷基; C2-C20烯基; C4-C7环烯基; C 2 -C 20炔基,C 4 -C 7环炔基; 或未取代的或C 1 -C 5烷基 - ,C 3 -C 7烷基烷基 - ,C 1 -C 5烷氧基 - ,C 3 -C 7环烷氧基 - ,卤代 - ,氧代 - ,羧基 - ,羧基-C 1 -C 7烷基酯 - ,羧基-C 3 -C 7环烷基酯 - 氰基 - 三氟甲基 - ,五氟乙基 - ,氨基 - ,N,N-单或二-C 1 -C 20烷基氨基或硝基取代的苯基-C 1 -C 5烷基,萘基-C 1 -C 5烷基,苯基羰基-C 1 -C 5烷基,萘基羰基-C 1 -C 5烷基 ,吡咯基烷基,呋喃基烷基,噻吩基烷基,吡唑基烷基,咪唑基烷基,恶唑基烷基,噻唑基烷基,异恶唑基烷基,异噻唑基烷基,1,2,3-三唑基烷基,1,2,4-三唑基烷基,1,2,3-恶二唑基烷基,1,3,4-恶二唑基烷基 1,2,3-噻二唑基烷基,1,3,4-噻二唑基烷基,吲哚基烷基,吡啶基烷基,哒嗪基烷基,嘧啶基烷基,哒嗪基烷基,喹啉基烷基,异喹啉基烷基,吡咯基,呋喃基,噻吩基,吡唑基,咪唑基,恶唑基,噻唑基,异恶唑基,异噻唑基, ,2,3-三唑基,1,2,4-三唑基,1,2,3-恶二唑基,1,3,4-恶二唑基,1,2,3-噻二唑基,1,3,4-噻二唑基,吲哚基, 吡啶基,哒嗪基,嘧啶基,哒嗪基,喹啉基或异喹啉基; R4,R5,R6和R7各自独立地为氢; C1-C20烷基; C3-C7环烷基; C2-C20烯基; C4-C7环烯基; C2-C20炔基; 或C 4 -C 7环炔基; m和n各自独立地为0或1,用于表面的抗微生物处理。 该化合物显示出对病原性革兰氏阳性的显着活性
    • 4. 发明授权
    • 4-amino-2-(2-pyridyl)pyrimidines as microbicidal active substances
    • US07015228B2
    • 2006-03-21
    • US10124198
    • 2002-04-17
    • Wolfgang HaapWerner HölzlKarin Petzold
    • Wolfgang HaapWerner HölzlKarin Petzold
    • A61K31/506A61P31/00A61P31/04C07D239/42
    • C07D401/04A61K31/506
    • Compounds of formula wherein R1 and R2 are each independently of the other hydrogen; unsubstituted or mono- or poly-halo-substituted C1–C20alkyl, C1–C20alkoxy, C2–C20alkenyl, C2–C20alkynyl, C3–C18cycloalkyl, C3–C7cycloalkyl-C1–C20alkyl; hydroxy; C1–C6alkoxy-C1–C20alkyl; carboxy; C1–C6alkyloxycarbonyl; cyano; mono- or di-C1–C20alkylamino; C1–C6alkylamino-C1–C20alkyl; halogen; phenyl; unsubstituted or C1–C5alkyl-, halo- or hydroxy-substituted phenyl-C1–C20alkyl, phenoxy or phenyl-C1–C20alkoxy; or R1 and R2 form a polymethylene chain of formula —(CH2)m— wherein m=2–12; R3 is unsubstituted C7–C20alkyl; or amino-, hydroxy-, carboxy- or C1–C6alkyloxycarbonyl-substituted C2–C20alkyl; C8–C18cycloalkyl; C8–C20alkenyl; C8–C20alkynyl; C3–C7cycloalkyl-C8–C20alkyl; C1–C4alkoxy-C8–C20alkyl; R7R8N—C7–C20alkyl; phenyl; phenyl-C1–C4alkyl; or phenyl-C1–C4alkoxy; R4 is hydrogen; unsubstituted or C1–C5alkyl-, halo- or hydroxy-substituted C1–C20alkyl, C2–C20alkenyl, C2–C20alkynyl, C3–C20cycloalkyl, C3–C7cycloalkyl-C1–C20alkyl, C1–C20alkoxy-C1–C6alkyl or R7R8N—C1–C20alkyl, phenyl, phenyl-C1–C20alkyl or phenoxy-C1–C20alkyl; R5 and R6 are each independently of the other hydrogen; C1–C20alkyl; C2–C20alkenyl; C2–C20-alkynyl; C3–C18cycloalkyl; C3–C7cycloalkyl-C1–C20alkyl; hydroxy; C2–C20alkoxy; C1–C6alkoxy-C1–C20alkyl; carboxy; C1–C6alkyloxycarbonyl; cyano; nitro; C1–C20alkylamino; C1–C20alkylaminoalkyl; C1–C20haloalkyl; C1–C20haloalkoxy; halogen; unsubstituted or C1–C5alkyl-, halo- or hydroxy-substituted phenyl, phenoxy or phenyl-C1–C20alkyl or phenyl-C1–C20alkoxy; or R5 and R6 together form a polymethylene chain of formula —(CH2)m— wherein m=2–12; and R7 and R8 are each independently of the other hydrogen; C1–C20alkyl; C3–C20alkenyl; C3–C20alkynyl; C3–C7cycloalkyl; C3–C20cycloalkyl-C1–C4alkyl; phenyl; or phenyl-C1–C4alkyl are suitable for the antimicrobial treatment of surfaces.