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1. 发明申请

US20130029981A1 COMPOUNDS, COMPOSITIONS, AND METHODS FOR CONTROLLING BIOFILMS 有权
标题翻译：化合物，组合物和控制生物体的方法
公开(公告)号：US20130029981A1
公开(公告)日：2013-01-31
申请号：US13526235
申请日：2012-06-18
申请人： Sigrid De Keersmaecker , Dirk De Vos , Denis Ermolatev , Hans Steenackers , Erik Van Der Eycken , Jozef Vanderleyden , Bharat S. Savaliya
发明人： Sigrid De Keersmaecker , Dirk De Vos , Denis Ermolatev , Hans Steenackers , Erik Van Der Eycken , Jozef Vanderleyden , Bharat S. Savaliya
IPC分类号： C07D233/88 , C07D487/04 , C07D405/12 , C07D403/12 , C07D409/14 , C07D413/14 , C07D239/42 , A61K31/4168 , A01N43/50 , A61K31/454 , A61K31/519 , A01N43/90 , A61K31/5377 , A01N43/84 , A61P31/00 , A01P1/00 , A61P31/04 , C07D401/12
CPC分类号： C07D233/88 , C07D405/12 , C07D409/04 , C07D487/04
摘要： The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients. Methods for inhibiting or controlling microbial biofilm formation in a plant, a body part of a human or an animal, or a surface with which a human or an animal may come into contact are also disclosed.
摘要翻译：本发明涉及取代的2-氨基咪唑及其对生物膜形成有活性的咪唑并[1,2-a]嘧啶鎓盐前体。本发明还涉及带有叠氮基烷基取代基的咪唑并[1,2-a]嘧啶鎓盐以及取代的2-氨基咪唑，其中氨基具有通过叠氮基炔代Huisgen环加成反应形成的末端杂环基，例如三唑基由具有叠氮基烷基取代基的咪唑并[1,2-a]嘧啶鎓盐制得。本发明还涉及可用作合成具有叠氮基烷基取代基的所述咪唑并[1,2-a]嘧啶鎓盐的起始原料的一类N-（叠氮基烷基）嘧啶-2-胺。本发明还涉及抗微生物组合物，其包括微生物生物膜形成抑制量的这种取代的2-氨基咪唑或咪唑并[1,2-a]嘧啶鎓盐与赋形剂的组合。还公开了抑制或控制植物，人或动物的身体部位或人或动物可能接触的表面的微生物生物膜形成的方法。

2. 发明授权

US08906915B2 Compounds, compositions, and methods for controlling biofilms 有权
标题翻译：用于控制生物膜的化合物，组合物和方法
公开(公告)号：US08906915B2
公开(公告)日：2014-12-09
申请号：US13526235
申请日：2012-06-18
申请人： Sigrid De Keersmaecker , Dirk De Vos , Denis Ermolatev , Hans Steenackers , Erik Van Der Eycken , Jozef Vanderleyden , Bharat S. Savaliya
发明人： Sigrid De Keersmaecker , Dirk De Vos , Denis Ermolatev , Hans Steenackers , Erik Van Der Eycken , Jozef Vanderleyden , Bharat S. Savaliya
IPC分类号： A61K31/535 , C07D487/04 , C07D405/12 , C07D233/88 , C07D409/04
CPC分类号： C07D233/88 , C07D405/12 , C07D409/04 , C07D487/04
摘要： The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients. Methods for inhibiting or controlling microbial biofilm formation in a plant, a body part of a human or an animal, or a surface with which a human or an animal may come into contact are also disclosed.
摘要翻译：本发明涉及取代的2-氨基咪唑及其对生物膜形成有活性的咪唑并[1,2-a]嘧啶鎓盐前体。本发明还涉及带有叠氮基烷基取代基的咪唑并[1,2-a]嘧啶鎓盐以及取代的2-氨基咪唑，其中氨基具有通过叠氮基炔代Huisgen环加成反应形成的末端杂环基，例如三唑基由具有叠氮基烷基取代基的咪唑并[1,2-a]嘧啶鎓盐制得。本发明还涉及可用作合成具有叠氮基烷基取代基的所述咪唑并[1,2-a]嘧啶鎓盐的起始原料的一类N-（叠氮基烷基）嘧啶-2-胺。本发明还涉及抗微生物组合物，其包括微生物生物膜形成抑制量的这种取代的2-氨基咪唑或咪唑并[1,2-a]嘧啶鎓盐与赋形剂的组合。还公开了抑制或控制植物，人或动物的身体部位或人或动物可能接触的表面的微生物生物膜形成的方法。

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