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1. 发明授权

US07015228B2 4-amino-2-(2-pyridyl)pyrimidines as microbicidal active substances 失效
公开(公告)号：US07015228B2
公开(公告)日：2006-03-21
申请号：US10124198
申请日：2002-04-17
申请人： Wolfgang Haap , Werner Hölzl , Karin Petzold
发明人： Wolfgang Haap , Werner Hölzl , Karin Petzold
IPC分类号： A61K31/506 , A61P31/00 , A61P31/04 , C07D239/42
CPC分类号： C07D401/04 , A61K31/506
摘要： 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.

2. 发明授权

US06743940B2 4-aminobut-2-ynecarboxylic acid derivatives 失效
标题翻译： 4-氨基丁-2-炔酸衍生物
公开(公告)号：US06743940B2
公开(公告)日：2004-06-01
申请号：US10016542
申请日：2001-12-13
申请人： Werner Hölzl , Wolfgang Haap , Jürgen Koppold , Dietmar Ochs , Karin Petzold , Marcel Schnyder
发明人： Werner Hölzl , Wolfgang Haap , Jürgen Koppold , Dietmar Ochs , Karin Petzold , Marcel Schnyder
IPC分类号： C07C22900
CPC分类号： C07C229/30
摘要： There are described 4-aminobut-2-ynecarboxylic acid derivatives of formula wherein R1 and R2 are each independently of the other hydrogen, C1-C20alkyl; C3-C12cycloalkyl; unsubstituted or C1-C5alkyl-, C3-C12cycloalkyl-, C1-C5alkoxy-, C3-C12cycloalkoxy-, halo-, oxo-, carboxy-, carboxy-C1-C7alkyl ester-, carboxy-C3-C12cycloalkyl ester-, cyano-, trifluoromethyl-, pentafluoroethyl-, amino-, N,N-mono- or di-C1-C20alkylamino- or nitro-substituted phenyl, phenyl-C1-C5alkyl, naphthyl and naphthyl-C1-C5alkyl; and R3 is C1-C20alkyl; C3-C12cycloalkyl. The compounds exhibit a pronounced activity against gram-positive and gram-negative bacteria, and also against yeasts and moulds.
摘要翻译：描述了通式为R 1的4-氨基丁-2-炔酸衍生物，R 2各自独立地为氢，C 1 -C 20烷基; C 3 -C 12环烷基; 未取代的或C 1 -C 5烷基 - ，C 3 -C 12环烷基 - ，C 1 -C 5烷氧基 - ，C 3 -C 12环烷氧基 - ，卤代 - ，氧代 - ，羧基 - ，羧基-C 1 -C 7烷基酯 - ，羧基-C 3 -C 12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，苯基-C 1 -C 5烷基，萘基和萘基-C 1 -C 5烷基; 和R 3是C 1 -C 20烷基; C3-C12环烷基。化合物对革兰氏阳性和革兰氏阴性细菌以及酵母和霉菌都表现出明显的活性。

3. 发明授权

US06967215B2 Tetrahydrocarbazoles, a process for the preparation of those compounds, and the use thereof 失效
标题翻译：四氢咔唑，这些化合物的制备方法及其用途
公开(公告)号：US06967215B2
公开(公告)日：2005-11-22
申请号：US10380573
申请日：2001-09-11
申请人： Wolfgang Haap , Andreas Mehlin , Karin Petzold , Dietmar Ochs , Werner Hölzl
发明人： Wolfgang Haap , Andreas Mehlin , Karin Petzold , Dietmar Ochs , Werner Hölzl
IPC分类号： A61K8/49 , A61K8/69 , A61K31/407 , A61K31/437 , A61L2/16 , A61Q11/00 , A61Q15/00 , A61Q17/00 , C07D209/86 , C07D209/88 , C07D471/04 , C07D471/14 , C07D471/22 , C07D487/04 , C11D3/00 , C11D3/28 , C11D3/48 , D21H21/36 , D21H25/18 , A61K31/403 , A61K7/40 , C07D487/02
CPC分类号： A61Q17/005 , A61K8/492 , A61K8/4933 , A61K8/494 , A61K8/69 , A61L2/16 , A61Q11/00 , A61Q15/00 , C07D471/14 , C07D487/04 , C11D3/28 , C11D3/48 , D21H21/36 , D21H25/18
摘要： Tetrahydrocarbazoles of formula where Q is —SO2—; —O—; or —(CO)—; X is —(CH)—; or —N—; m is from 1 to 3; t is 0 or 1 and the remaining substituents are as defined herein, are useful as antimicrobial active ingredients.
摘要翻译：其中Q为-SO 2 - 的式的四氢咔唑; -O-; 或 - （CO） - ; X为 - （CH） - ; 或-N-; m为1〜3; t为0或1，其余取代基如本文所定义，可用作抗微生物活性成分。

4. 发明授权

US06846492B2 Use of phenylethylamine derivatives for the antimicrobial treatment of surfaces 失效
标题翻译：苯乙胺衍生物用于表面抗微生物处理
公开(公告)号：US06846492B2
公开(公告)日：2005-01-25
申请号：US10204520
申请日：2001-02-13
申请人： Wolfgang Haap , Werner Hölzl , Dietmar Ochs , Karin Petzold , Marcel Schnyder
发明人： Wolfgang Haap , Werner Hölzl , Dietmar Ochs , Karin Petzold , Marcel Schnyder
IPC分类号： A01N33/10 , A01N37/38 , A01N39/00 , A01N39/02 , A01N39/04 , C07C217/60 , C07C255/54 , A01N25/00 , A61K7/075 , A61K7/50 , C11D7/00 , D06L1/00
CPC分类号： C07C255/54 , A01N33/10 , A01N37/38 , A01N39/00 , A01N39/02 , A01N39/04 , C07C217/60 , C07C2601/08
摘要： 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.
摘要翻译：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

5. 发明授权

US06620854B2 Surface-active preparations 有权
标题翻译：表面活性剂
公开(公告)号：US06620854B2
公开(公告)日：2003-09-16
申请号：US09885346
申请日：2001-06-19
申请人： Marcel Schnyder , François Brugger , Fernand Hoffstetter , Karin Mühlbauer , Karin Petzold , Radojka Vukomanovic
发明人： Marcel Schnyder , François Brugger , Fernand Hoffstetter , Karin Mühlbauer , Karin Petzold , Radojka Vukomanovic
IPC分类号： A01N3114
CPC分类号： C11D3/48 , C11D3/2034 , C11D3/2068 , C11D3/3418
摘要： There are described surface-active soap compositions containing (a) from 0.01 to 2% by weight of an antimicrobial active ingredient from the class of diphenyl ethers, (b) from 0.1 to 30% by weight of a hydrotropic agent, (c) from 6.0 to 50% by weight of one or more synthetic detergents or soaps or a combination of such substances, (d) from 0 to 70% by weight of a monohydric or dihydric alcohol, and (e) tap water or deionised water ad 100%. The composition is used for disinfecting and cleaning human skin and hands and hard objects, and in washing and cleaning formulations for textile fibre materials.
摘要翻译：描述了表面活性皂组合物，其包含（a）0.01至2重量％的来自二苯醚类的抗微生物活性成分，（b）0.1至30重量％的水溶助推剂，（c） 6.0至50重量％的一种或多种合成洗涤剂或肥皂或这些物质的组合，（d）0至70重量％的一元醇或二元醇，和（e）自来水或去离子水至100重量％该组合物用于消毒和清洁人体皮肤，手和硬物，以及纺织纤维材料的清洗和清洁配方。

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