公开(公告)号：US08906915B2

公开(公告)日：2014-12-09

申请号：US13526235

申请日：2012-06-18

Applicant: Sigrid De Keersmaecker ,  Dirk De Vos ,  Denis Ermolatev ,  Hans Steenackers ,  Erik Van Der Eycken ,  Jozef Vanderleyden ,  Bharat S. Savaliya

Inventor： Sigrid De Keersmaecker ,  Dirk De Vos ,  Denis Ermolatev ,  Hans Steenackers ,  Erik Van Der Eycken ,  Jozef Vanderleyden ,  Bharat S. Savaliya

IPC: A61K31/535 ,  C07D487/04 ,  C07D405/12 ,  C07D233/88 ,  C07D409/04

CPC classification number: C07D233/88 ,  C07D405/12 ,  C07D409/04 ,  C07D487/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20130150626A1

公开(公告)日：2013-06-13

申请号：US13704406

申请日：2011-06-14

Applicant: Pascal Mertens ,  Dirk De Vos ,  Bart Steenackers

Inventor： Pascal Mertens ,  Dirk De Vos ,  Bart Steenackers

IPC: C07C45/66

CPC classification number: C07C45/66 ,  C07C51/36 ,  C12C3/12 ,  C07C59/90

Abstract: The invention relates to a process for the production of hexahydro-iso-alpha-acids starting from iso-alpha-acids (or tetrahydro-iso-alpha-acids) in which iso-alpha-acids (or tetrahydro-iso-alpha-acids) are mixed with a heterogeneous ruthenium containing catalyst, that catalyzes the hydrogenation from iso-alpha-acids or tetrahydro-iso-alpha-acids to hexahydro-iso-alpha-acids, either in solvent-free conditions, or in the presence of a solvent phase (e.g. carbon dioxide, water, ethanol or another organ-ic solvent, or mixtures thereof), and in the absence or presence of other hop compounds (such as beta-acids). The resulting mix-ture is then subjected to a temperature at which the iso-alpha-acid (or tetrahydro-iso-alpha-acid) containing reaction medium is sufficiently low in viscosity to allow easy mixing with the heterogeneous ruthenium containing catalyst and held under a hydrogen containing atmosphere (either pure hydrogen gas or mixed with an inert gas) for a reaction tune sufficient to effect high conver-sion of the iso-alpha-acid (or tetrahydro-iso-alpha-acid) reactant into the hexahydro-iso-alpha-acid product. The molar ratio of iso-alpha-acid or tetrahydro-iso-alpha-acid to ruthenium varies between 1:1 and 2000:1. After the hydrogenation process, the hetero-geneous ruthenium containing catalyst can be separated from the hexahydro-iso-alpha-acid product phase by centrifugation, filtra-tion, decantation or other liquid-solid separation techniques. The hydrogenation process can be performed batch-wise or alterna-tively in continuous mode.

Abstract translation: 本发明涉及从异-α-酸（或四氢异α-酸）开始制备六氢异-5-酸的方法，其中异-α-酸（或四氢异α-酸） ）与含异丁烯的含钌催化剂混合，催化剂在无溶剂条件下或在无水条件下催化从异-α-酸或四氢异-α-酸氢化成六氢异-α-酸 溶剂相（如二氧化碳，水，乙醇或其他有机溶剂或其混合物），以及其它啤酒花化合物（如β-酸）不存在或不存在时。 然后将所得混合物经受含有异-α酸（或四氢异α-酸）的反应介质的粘度足够低的温度，以容易地与含异丁烯的含钌催化剂混合并保持在 用于反应曲线的氢气气氛（纯氢气或惰性气体混合）足以使异α酸（或四氢异α-酸）反应物高效转化为六氢异构体 -α-酸产物。 异-α-酸或四氢异-α-酸与钌的摩尔比在1:1至2000:1之间变化。 在氢化过程之后，通过离心，过滤，倾析或其它液固分离技术，可以将异质含钌的催化剂与六氢 - 异α-酸产物相分离。 氢化过程可以分批进行或以连续模式交替进行。

公开(公告)号：US20120259148A1

公开(公告)日：2012-10-11

申请号：US13438408

申请日：2012-04-03

Applicant: Bilge Yilmaz ,  Ulrich Müller ,  Faruk Özkirim ,  Dirk de Vos ,  Feng-Shou Xiao ,  Takashi Tatsumi ,  Xinhe Bao ,  Weiping Zhang ,  Hermann Gies ,  Hiroyuki Imai ,  Bart Tijsebaert

Inventor： Bilge Yilmaz ,  Ulrich Müller ,  Faruk Özkirim ,  Dirk de Vos ,  Feng-Shou Xiao ,  Takashi Tatsumi ,  Xinhe Bao ,  Weiping Zhang ,  Hermann Gies ,  Hiroyuki Imai ,  Bart Tijsebaert

IPC: C07C2/66

CPC classification number: C07C2/66 ,  C07C2529/70 ,  C07C15/073 ,  C07C15/02

Abstract: The present invention relates to a process for the alkylation of an organic compound comprising: (a) providing a catalyst comprising one or more zeolitic materials having a BEA framework structure, wherein the BEA framework structure comprises YO2 and optionally comprises X2O3, wherein Y is a tetravalent element, and X is a trivalent element, (b) contacting the catalyst with one or more alkylatable organic compounds in the presence of one or more alkylating agents in one or more reactors for obtaining one or more alkylated organic compounds, wherein the one or more zeolitic materials is obtainable from a synthetic process which does not employ an organotemplate as structure directing agent.

Abstract translation: 本发明涉及一种有机化合物的烷基化方法，包括：（a）提供包含一种或多种具有BEA骨架结构的沸石材料的催化剂，其中所述BEA骨架结构包含YO 2并且任选地包含X 2 O 3，其中Y是 四价元素，X是三价元素，（b）在一个或多个烷基化剂存在下，在一个或多个烷基化剂存在下使催化剂与一种或多种可烷基化的有机化合物接触，以获得一种或多种烷基化有机化合物，其中所述一种或多种烷基化有机化合物， 更多的沸石材料可以从不使用有机模板作为结构导向剂的合成方法获得。

公开(公告)号：US20110319251A1

公开(公告)日：2011-12-29

申请号：US13254046

申请日：2010-03-03

Applicant: Bilge Yilmaz ,  Ulrich Müller ,  Feng-Shou Xiao ,  Hermann Gies ,  Xinhe Bao ,  Dirk De Vos ,  Takashi Tatsumi ,  Weiping Zhang

Inventor： Bilge Yilmaz ,  Ulrich Müller ,  Feng-Shou Xiao ,  Hermann Gies ,  Xinhe Bao ,  Dirk De Vos ,  Takashi Tatsumi ,  Weiping Zhang

IPC: B01J29/00 ,  C04B35/622 ,  C01B35/00 ,  C01B33/20 ,  C01B33/26

CPC classification number: C01B37/005 ,  C01B37/02 ,  C04B35/16 ,  C04B2235/3217 ,  C04B2235/3232 ,  C04B2235/3239 ,  C04B2235/3244 ,  C04B2235/3251 ,  C04B2235/3272 ,  C04B2235/3286 ,  C04B2235/3287 ,  C04B2235/3293 ,  C04B2235/3409 ,  C04B2235/3427 ,  C04B2235/441 ,  C04B2235/5409 ,  C04B2235/602 ,  C04B2235/6021

Abstract: The present invention relates to a process for the preparation of an isomorphously substituted RUB-36 silicate comprising (1) providing a mixture containing silica, preferably amorphous silica, and/or at least one silica precursor, water, at least one suitable structure directing agent, (2) heating the mixture obtained according to (1) under hydrothermal conditions to give a suspension containing an RUB-36 silicate, (3) separating the RUB-36 silicate, wherein (a) either the mixture according to (1) contains at least one element suitable for isomorphous substitution and/or (b) the separated RUB-36 silicate according to (3) is subjected to isomorphous substitution.

Abstract translation: 本发明涉及一种制备同晶取代的RUB-36硅酸盐的方法，其包括（1）提供含有二氧化硅，优选无定形二氧化硅和/或至少一种二氧化硅前体，水，至少一种合适的结构导向剂 ，（2）在水热条件下加热根据（1）获得的混合物，得到含有RUB-36硅酸盐的悬浮液，（3）分离RUB-36硅酸盐，其中（a）根据（1）的混合物含有 适于同晶取代的至少一种元素和/或（b）根据（3）的分离的RUB-36硅酸盐进行同晶取代。

公开(公告)号：US20100191000A1

公开(公告)日：2010-07-29

申请号：US12665509

申请日：2008-06-18

Applicant: Johann-Peter Melder ,  Martin Ernst ,  Till Gerlach ,  Ekkehard Schwab ,  Csaba Varszegi ,  Bert Sels ,  Dirk de Vos

Inventor： Johann-Peter Melder ,  Martin Ernst ,  Till Gerlach ,  Ekkehard Schwab ,  Csaba Varszegi ,  Bert Sels ,  Dirk de Vos

IPC: C07D203/08 ,  C25B3/02

CPC classification number: C07D203/08 ,  C07D203/02

Abstract: Process for preparing an N-unsubstituted or N-substituted aziridine of the formula which comprises reacting an olefin of the formula I where R1 to R5 are each, independently of one another, hydrogen, a linear or branched alkyl radical having from 1 to 16 carbon atoms, a hydroxyalkyl radical having from 1 to 4 carbon atoms, a cycloalkyl radical having from 5 to 7 carbon atoms, a benzyl or phenyl radical which in each case may be substituted in the o, m or p position of the phenyl radical by methoxy, hydroxy, chlorine or alkyl radicals having from 1 to 4 carbon atoms and the radical R1 or R2 together with the radical R3 or R4 may be closed to form a 5- to 12-membered ring or the radicals R1 and R2 may be closed to form a 5- to 12-membered ring, with ammonia or a primary amine of the formula R5NH2 in the presence of iodine or bromine.

Abstract translation: 制备下式的N-未取代的或N-取代的氮丙啶的方法，其包括使式I的烯烃（其中R 1至R 5）彼此独立地彼此独立地为氢，具有1至16个碳原子的直链或支链烷基 原子，具有1至4个碳原子的羟基烷基，具有5至7个碳原子的环烷基，苄基或苯基，其在每种情况下可以在苯基的o，m或p位置被甲氧基取代 ，羟基，氯或具有1至4个碳原子的烷基和基团R 1或R 2与基团R 3或R 4一起可以封闭以形成5至12元环，或者基团R 1和R 2可以被封闭 在碘或溴的存在下与氨或式R 5 NH 2的伯胺形成5-至12元环。

公开(公告)号：US5079349A

公开(公告)日：1992-01-07

申请号：US473537

申请日：1990-02-01

Applicant: Johan W. Scheeren ,  Joannes F. M. De Bie ,  Dirk De Vos

Inventor： Johan W. Scheeren ,  Joannes F. M. De Bie ,  Dirk De Vos

IPC: C07F7/08

CPC classification number: C07F7/0818

Abstract: The invention relates to novel compounds of the formulae ##STR1## wherein S is H, alkyl or alkoxy and R is a good leaving group, and to the preparation of these compounds in a stereospecific manner to obtain a configuration wherein OH at C-3 and OR at C-1 are in the cis-position, which compounds can be used for the synthesis of daunomycinone and derivatives thereof.Daunomycinone can be used for the preparation of daunomycin and adriamycin.

公开(公告)号：US09909088B2

公开(公告)日：2018-03-06

申请号：US13876915

申请日：2011-09-29

Applicant: Dirk De Vos ,  Pascal Mertens

Inventor： Dirk De Vos ,  Pascal Mertens

IPC: C12C3/12

CPC classification number: C12C3/12

Abstract: The invention relates to a process for the production of iso-alpha-acids starting from alpha-acids in which an alpha-acid containing hop extract is mixed with a carbon-containing chemical compound with one or more functional groups containing a (basic) nitrogen atom with a lone pair (or mixtures thereof), either in solvent-free conditions or in the presence of solvents and preferably under an oxygen-free atmosphere. The resulting mixture is subjected to a temperature of at least 278 K for a time sufficient to effect the intended conversion of the alpha-acid reactant into the iso-alpha-acid product. The present invention further relates to iso-alpha-acid compositions obtained by said improved isomerisation process and to the use of said iso-alpha-acid compositions as bittering formulation and/or as source to obtain reduced or hydrogenated iso-alpha-acid compositions.

公开(公告)号：US20130209653A1

公开(公告)日：2013-08-15

申请号：US13876915

申请日：2011-09-29

Applicant: Dirk De Vos ,  Pascal Mertens

Inventor： Dirk De Vos ,  Pascal Mertens

IPC: C12C3/12

CPC classification number: C12C3/12

Abstract: The invention relates to a process for the production of iso-alpha-acids starting from alpha-acids in which an alpha-acid containing hop extract is mixed with a carbon-containing chemical compound with one or more functional groups containing a (basic) nitrogen atom with a lone pair (or mixtures thereof), either in solvent-free conditions or in the presence of solvents and preferably under an oxygen-free atmosphere. The resulting mixture is subjected to a temperature of at least 278 K for a time sufficient to effect the intended conversion of the alpha-acid reactant into the iso-alpha-acid product. The present invention further relates to iso-alpha-acid compositions obtained by said improved isomerisation process and to the use of said iso-alpha-acid compositions as bittering formulation and/or as source to obtain reduced or hydrogenated iso-alpha-acid compositions.

Abstract translation: 本发明涉及从α-酸开始生产异α酸的方法，其中将含有α-酸的啤酒花提取物与含碳化合物与含有（碱）氮的一个或多个官能团混合 原子与一对（或其混合物），无溶剂条件下或在溶剂存在下，优选在无氧气氛下进行。 将所得混合物经受至少278K的温度足以实现将α-酸反应物预期转化成异α酸产物的时间。 本发明还涉及通过所述改进的异构化方法获得的异-α酸组合物和所述异-α-酸组合物作为苦味制剂和/或作为来源以获得还原或氢化异-α酸组合物的用途。

公开(公告)号：US20130029981A1

公开(公告)日：2013-01-31

申请号：US13526235

申请日：2012-06-18

Applicant: Sigrid De Keersmaecker ,  Dirk De Vos ,  Denis Ermolatev ,  Hans Steenackers ,  Erik Van Der Eycken ,  Jozef Vanderleyden ,  Bharat S. Savaliya

Inventor： Sigrid De Keersmaecker ,  Dirk De Vos ,  Denis Ermolatev ,  Hans Steenackers ,  Erik Van Der Eycken ,  Jozef Vanderleyden ,  Bharat S. Savaliya

IPC: 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 classification number: C07D233/88 ,  C07D405/12 ,  C07D409/04 ,  C07D487/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20120016045A1

公开(公告)日：2012-01-19

申请号：US13254022

申请日：2010-03-03

Applicant: Bilge Yilmaz ,  Ulrich Müller ,  Meike Pfaff ,  Hermann Gies ,  Feng-Shou Xiao ,  Takashi Tatsumi ,  Dirk de Vos ,  Xinhe Bao ,  Weiping Zhang

Inventor： Bilge Yilmaz ,  Ulrich Müller ,  Meike Pfaff ,  Hermann Gies ,  Feng-Shou Xiao ,  Takashi Tatsumi ,  Dirk de Vos ,  Xinhe Bao ,  Weiping Zhang

IPC: C08J9/00 ,  C01B33/20

CPC classification number: C01B33/20 ,  B01J20/10 ,  B01J20/30 ,  B01J21/16 ,  B01J29/049 ,  C01B33/38 ,  C01B37/00 ,  C01B37/02 ,  C01B39/02 ,  C01B39/04

Abstract: The present invention relates to a process for the preparation of a layered silicate containing at least silicon and oxygen, comprising (1) providing a mixture containing silica and/or at least one silica precursor, water, at least one tetraalkylammonium compound selected from the group consisting of diethyldimethylammonium compound, a triethylmethylammonium compound, and a mixture of a diethyldimethylammonium and a triethylmethylammonium compound, and at least one base, and optionally at least one suitable seeding material; and (2) heating of the mixture obtained according to (1) under autogenous pressure (hydrothermal conditions) to a temperature in the range of from to 120 to 160° C. for a period in the range of from 5 to 10 days to give a suspension containing the layered silicate.

Abstract translation: 本发明涉及一种制备至少含硅和氧的层状硅酸盐的方法，其包括（1）提供含有二氧化硅和/或至少一种二氧化硅前体的混合物，水，至少一种选自以下的四烷基铵化合物 由二乙基二甲基铵化合物，三乙基甲基铵化合物和二乙基二甲基铵和三乙基甲基铵化合物的混合物组成，以及至少一种碱和任选的至少一种合适的接种材料; 和（2）根据（1）获得的混合物在自生压力（水热条件）下加热至120至160℃的温度范围为5至10天，得到 含有层状硅酸盐的悬浮液。