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    • 2. 发明授权
    • Use of substitute 2,4-bis (alkylamino) pyrimidines or quinzolines as antimicrobials
    • 使用替代2,4-双(烷基氨基)嘧啶或喹唑啉作为抗微生物剂
    • US07722893B2
    • 2010-05-25
    • US10565545
    • 2004-07-16
    • Sophie Marquais-BienewaldWerner HölzlAndrea PreussAndreas Mehlin
    • Sophie Marquais-BienewaldWerner HölzlAndrea PreussAndreas Mehlin
    • A01N25/00C07D265/30C07D239/22
    • A61Q17/005A01N43/54A61K8/4953A61L2/16A61L2/18A61Q11/00C11D3/28C11D3/48D06M13/355Y10T442/2525
    • The use of 2,4—bis(alkylamino)pyrimidines of formula (1) R1 is C1-C12alkyl or C6-C10laryl; R2 is hydrogen or C1-C12alkyl; or R1 and R2 together form a radical of formula (1a) R′ and R″ are each independently of the other hydrogen, C1-C6alkyl or C1-C6alkoxy, R3 and R5 are each independently of the other hydrogen or C1-C8alkyl; R4 is C1-C20alkyl, unsubstituted phenyl, C6-C10aryl, C6-C10aryl-C1-C6alkyl, hydroxy-C1-C6alkyl, di-C1-C6alkylamino-C 1-C6alkyl, mono-C1-C6alkylamino-C1-C6alkyl, —(CH2)2-(O—(CH2)2)1-4—OH or —(CH2)2—(O—(CH2)2)1-4—NH2; R6 is C1-C20alkyl, C6-C10aryl, C6-C10aryl-C1-C6alkyl, hydroxy-C1-C6alkyl, di-C1C6alkylamino-C1-C6alkyl, mono- C1-C6alkylamino-C1-C 6alkyl, —(CH2)2—(O—(CH2)2)1-4—OH or —(CH2)2—(O—(CH2)2)1-4—NH2; or R3 and R 4 and/or R5 and R6, together form a pyrrolidine, piperidine, hexamethyleneimine or morpholine ring; in the antimicrobial treatment of surfaces.
    • 式(1)R 1的2,4-双(烷基氨基)嘧啶的用途是C 1 -C 12烷基或C 6 -C 10芳基; R2是氢或C1-C12烷基; 或者R 1和R 2一起形成式(1a)的基团,R'和R“各自独立地为氢,C 1 -C 6烷基或C 1 -C 6烷氧基,R 3和R 5各自独立地为氢或C 1 -C 8烷基; R 4是C 1 -C 20烷基,未取代的苯基,C 6 -C 10芳基,C 6 -C 10芳基-C 1 -C 6烷基,羟基-C 1 -C 6烷基,二-C 1 -C 6烷基氨基-C 1 -C 6烷基,单C 1 -C 6烷基氨基-C 1 -C 6烷基, - ( CH2)2-(O-(CH2)2)1-4-OH或 - (CH2)2-(O-(CH2)2)1-4-NH2; R 6是C 1 -C 20烷基,C 6 -C 10芳基,C 6 -C 10芳基-C 1 -C 6烷基,羟基-C 1 -C 6烷基,二-C 1 -C 6烷基氨基-C 1 -C 6烷基,单C 1 -C 6烷基氨基-C 1 -C 6烷基, - (CH 2)2 - ( O-(CH 2)2)1-4-OH或 - (CH 2)2 - (O-(CH 2)2)1-4-NH 2; 或R 3和R 4和/或R 5和R 6一起形成吡咯烷,哌啶,六亚甲基亚胺或吗啉环; 在表面的抗菌处理中。
    • 9. 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
    • 10. 发明授权
    • Process for the preparation of 4,4′-dihalogen-o-hydroxydiphenyl compounds
    • 制备4,4'-二卤代-O-羟基二苯基化合物的方法
    • US06596907B1
    • 2003-07-22
    • US09806668
    • 2001-04-03
    • Armando Di TeodoroWerner HölzlDieter ReinehrRudolf Zink
    • Armando Di TeodoroWerner HölzlDieter ReinehrRudolf Zink
    • C07C4100
    • C07C41/16C07C41/22C07C41/26C07C43/23C07C43/29C07C43/295
    • A description is given of a three-step process for the preparation of 4,4′-dihalogen-o-hydroxydiphenyl compounds of formula (1) which comprises: a) hologenating an alkoxyphenol of formula (6) (=a1), reacting the resulting halogenated phenol compound of formula (5) with p-dihalobenzene of formula (4a) in the presence of copper and/or copper salts to the diphenyl ether compound of formula (2) (=a2) and subsequent ether fission to the diphenyl ether compound of formula (1) (=a3); or b) reacting an alkoxyphenol of formula (6) with the halophenol of formula (4b) to the compound of formula (3) (=b1), then halogenating this compound (=b2) and subsequent ether fission of the resulting compound of formula (2) to the diphenyl ether compound of formula (1) (=b3). The compounds of formula (1) are used for protecting organic materials and objects against microorganisms.
    • 给出了制备式(1)的4​​,4'-二卤代邻羟基二苯基化合物的三步法,其包括:a)使式(6)的烷氧基​​酚(= a1)氢化,使 得到式(5)的卤代酚化合物与式(4a)的对二卤苯在铜和/或铜盐存在下与式(2)(= a2)的二苯基醚化合物反应,随后醚裂解成二苯基醚 式(1)化合物(= a3); 或b)使式(6)的烷氧基​​酚与式(4b)的卤代酚反应到式(3)的化合物(= b1),然后将该化合物(= b2)卤化,随后将所得的式 (2)到式(1)的二苯醚化合物(= b3)。 式(1)化合物用于保护有机材料和物体免受微生物侵害。