公开(公告)号：EP2510511A1

公开(公告)日：2012-10-17

申请号：EP10809131.5

申请日：2010-12-06

申请人： Ustav Organicke Chemie a Biochemie Akademie Ved Ceske Republiky, V.V.I. ,  Zentiva, K.S.

发明人： BÁRTA, Jaroslav ,  MUDRA, Petr ,  PESEK, Václav ,  PONCAR, Pavel ,  DOHNAL, Jirí ,  JAMPÍLEK, Josef ,  KRÁL. Vladimír ,  POKORNY, Vít ,  REZÁCOVÁ, Anna

IPC分类号： G09B23/30 ,  G09B23/32 ,  B01F11/00

CPC分类号： G09B23/30 ,  B01F11/0065 ,  G09B23/32

摘要： A digestive tract simulator, comprising hydraulically interconnected at least two elastic bags (12) kept at the constant temperature and a controllable heating source, wherein a heating source is represented by a heated temperating plate (2) over whose working surface intended for placing of elastic bags (12) two levers (7) are arranged in an axial distance, swinging around a common axis; to these levers (7) a deflected wing (3) placed in parallel with the temperating plate (2) and having working arms opened in a wide angle in direction from the temperating plate (2) is mounted on the lever's side near to the temperating plate (2); at least one of levers (7) is connected to a pendulum engine (4) having an adjustable motion so that elastic bags (12) are in operating state situated between the working surface of the temperating plate (2) and the deflected wing (3); each of bags (12) is equipped by an air cock (127) and an input and output pipe channel (126) for working medium, connecting bags (12) together via tubing coupled through a peristaltic pump (5).

公开(公告)号：EP2598509A1

公开(公告)日：2013-06-05

申请号：EP11781995.3

申请日：2011-07-27

申请人： Ustav Organicke Chemie a Biochemie Akademie Ved Ceske Republiky, V.V.I.

发明人： JANSA, Petr ,  HOLY, Antonín ,  CESNEK, Michal

IPC分类号： C07F9/40

CPC分类号： C07F9/4006

摘要： The invention deals with the method of the synthesis of dialkyl haloalkylphosphonates and dialkyl haloalkyloxyalkylphosphonates via a microwave-heated Michaelis-Arbuzov reaction of trialkylphosphites with dihaloalkanes or bis(haloalkyl)ethers in a closed vessel, during which the reaction mixture, containing a dihaloalkane or bis(haloalkyl)ether and a trialkylphosphite, is heated with microwave radiation with the standard frequency (2.45 GHz) to reach a reaction temperature which is specific for each individual halogen. In the subsequent reaction of the first dihaloalkane or bis(haloalkyl)ether halogen atom with trialkyl phosphite, the desired dialkyl haloalkylphosphonate or dialkyl haloalkyloxyalkylphosphonate is formed, but the reaction of its halogen atom with the so-far present trialkylphosphite, leading to the creation of the relevant bisphosphonate, no longer takes place. In the case of an inhomogeneous reaction mixture, also the desired product in the amount of 0.1-5 molar % is added to the reaction mixture for its homogenization, which homogenizes it and thus precludes its uncontrollable overheating. The entire process of synthesis is more effective, faster, less expensive and more environmentally friendly than the methods described so far in the literature. The possibility of performing the described procedure also in a continuous-flow microwave reactor allows industrial production with minimal demands on an optimization of the reaction conditions for larger quantities, eliminates some security risks, dramatically reduces the spatial demands in production and reduces the need for the usage of large-tonnage industrial reactors.

摘要翻译： 本发明涉及通过在密闭容器中通过三烷基亚磷酸酯与二卤代烷烃或双（卤代烷基）醚的微波加热的迈克尔斯 - 阿布佐夫反应合成卤代烷基膦酸二烷基酯和二烷基卤代烷氧基烷基膦酸酯的方法，其中含有二卤代烷或二 （卤代烷基）醚和三烷基亚磷酸酯，以标准频率（2.45GHz）的微波辐射加热，达到对于各个卤素特异的反应温度。 在第一个二卤代烷烃或双（卤代烷基）醚卤素原子与亚磷酸三烷基酯的反应中，形成了所需的卤代烷基膦酸二烷基酯或卤代烷基氧基烷基膦酸二烷基酯，但其卤素原子与目前为止存在的亚磷酸三烷基酯反应，导致产生 相关的二膦酸盐，不再发生。 在不均匀的反应混合物的情况下，将均匀化均匀化的反应混合物中所需的0.1-5摩尔％的量也加入其中，从而排除其不可控制的过热。 整个合成过程比文献中迄今描述的方法更有效，更快，更便宜，更环保。 在连续流微波反应器中执行所描述的过程的可能性允许工业生产对较大量的反应条件的优化的需求最小化，消除一些安全风险，大大降低了生产中的空间需求，并且减少了对 大吨位工业反应堆的使用。

公开(公告)号：EP2265631B1

公开(公告)日：2012-04-25

申请号：EP09716413.1

申请日：2009-03-03

申请人： Ustav Organicke Chemie a Biochemie Akademie Ved Ceske Republiky, V.V.I.

发明人： CEROVSKY, Václav ,  SLANINOVÁ, Jirina ,  HOVORKA, Oldrich ,  CVACKA, Josef ,  VOBURKA, Zdenek ,  FUCÍK, Vladimír ,  BEDNÁROVÁ, Lucie ,  VOTRUBA, Ivan ,  BOROVICKOVÁ, Lenka ,  TURÁNEK, Jaroslav

IPC分类号： C07K7/08 ,  A61K38/10

CPC分类号： C07K14/43572 ,  A61K38/00 ,  C07K7/08

摘要： This invention involves four novel peptides of the formulas I, II, III a IV isolated from natural sources and their synthetic analogs of general formula V and VI, where
R
1 represents acyl, alkyl or unprotected amino group,
R
2 represents amid, substituted amid, unprotected carboxylic group or ester,
Xaa represents, independently from each other, proteinogenic amino acid, D-amino acid, non-standard amino acid or amino acid with the side chain modification,
n means position of the amino acid replacement and
m means the number of the replacements in the peptide chain, and their applications as antimicrobial, antiviral, antifungal, antiparasitic and anticancer compounds. Therefore, they are practical for the production of medication for the treatment of microbial, parasitic and fungal diseases and for the cancer treatment. Formulas for summary: H-Gly-Phe-Leu-Ser-Ile-Leu-Lys-Lys-Val-Leu-Pro-Lys-Val-Met-Ala-His-Met-Lys-NH
2 (I) H-VaI-Asn-Trp-Lys-Lys-VaI-Leu-GIy-Lys-IIe-IIe-Lys-VaI-AIa-Lys-NH
2 (II) H-VaI-Asn-Trp-Lys-Lys-IIe-Leu-GIy-Lys-IIe-IIe-Lys-VaI-AIa-Lys-NH
2 (III) H-Val-Asn-Trp-Lys-Lys-Ile-Leu-Gly-Lys-Ile-Ile-Lys-Val-Val-Lys-NH
2 (IV) R
1 -[Xaa
n ]
m -Gly-Phe-Leu-Ser-Ile-Leu-Lys-Lys-Val-Leu-Pro-Lys-Val-Met-Ala-His-Met-Lys-R
2 (V) R
1 -[Xaa
n ]
m -Val-Asn-Trp-Lys-Lys-Ile-Leu-Gly-Lys-Ile-Ile-Lys-Val-Val-Lys-R
2 (VI)

公开(公告)号：EP2265631A2

公开(公告)日：2010-12-29

申请号：EP09716413.1

申请日：2009-03-03

申请人： Ustav Organicke Chemie a Biochemie Akademie Ved Ceske Republiky, V.V.I.

发明人： CEROVSKY, Václav ,  SLANINOVÁ, Jirina ,  HOVORKA, Oldrich ,  CVACKA, Josef ,  VOBURKA, Zdenek ,  FUCÍK, Vladimír ,  BEDNÁROVÁ, Lucie ,  VOTRUBA, Ivan ,  BOROVICKOVÁ, Lenka ,  TURÁNEK, Jaroslav

IPC分类号： C07K7/08 ,  A61K38/10

CPC分类号： C07K14/43572 ,  A61K38/00 ,  C07K7/08

摘要： This invention involves four novel peptides of the formulas I, II, III a IV isolated from natural sources and their synthetic analogs of general formula V and VI, where
R
1 represents acyl, alkyl or unprotected amino group,
R
2 represents amid, substituted amid, unprotected carboxylic group or ester,
Xaa represents, independently from each other, proteinogenic amino acid, D-amino acid, non-standard amino acid or amino acid with the side chain modification,
n means position of the amino acid replacement and
m means the number of the replacements in the peptide chain, and their applications as antimicrobial, antiviral, antifungal, antiparasitic and anticancer compounds. Therefore, they are practical for the production of medication for the treatment of microbial, parasitic and fungal diseases and for the cancer treatment. Formulas for summary: H-Gly-Phe-Leu-Ser-Ile-Leu-Lys-Lys-Val-Leu-Pro-Lys-Val-Met-Ala-His-Met-Lys-NH
2 (I) H-VaI-Asn-Trp-Lys-Lys-VaI-Leu-GIy-Lys-IIe-IIe-Lys-VaI-AIa-Lys-NH
2 (II) H-VaI-Asn-Trp-Lys-Lys-IIe-Leu-GIy-Lys-IIe-IIe-Lys-VaI-AIa-Lys-NH
2 (III) H-Val-Asn-Trp-Lys-Lys-Ile-Leu-Gly-Lys-Ile-Ile-Lys-Val-Val-Lys-NH
2 (IV) R
1 -[Xaa
n ]
m -Gly-Phe-Leu-Ser-Ile-Leu-Lys-Lys-Val-Leu-Pro-Lys-Val-Met-Ala-His-Met-Lys-R
2 (V) R
1 -[Xaa
n ]
m -Val-Asn-Trp-Lys-Lys-Ile-Leu-Gly-Lys-Ile-Ile-Lys-Val-Val-Lys-R
2 (VI)

公开(公告)号：EP3245513A2

公开(公告)日：2017-11-22

申请号：EP16706121.7

申请日：2016-01-13

申请人： Ustav Organicke Chemie a Biochemie Akademie Ved Ceske Republiky, V.V.I. ,  Ustav Makromolekularni Chemie AV CR, v.v.i. ,  Univerzita Karlova v Praze, Prírodovedecká fakulta

发明人： SACHA, Pavel ,  KONVALINKA, Jan ,  SCHIMER, Jiri ,  KNEDLIK, Tomas ,  SUBR, Vladimir ,  ULBRICH, Karel ,  STROHALM, Jiri

IPC分类号： G01N33/531 ,  G01N33/532 ,  G01N33/533 ,  G01N33/534 ,  C08F20/58 ,  C08F220/58

CPC分类号： G01N33/532 ,  C08F8/30 ,  G01N33/531 ,  G01N33/533 ,  G01N33/534 ,  G01N33/58 ,  G01N33/582

摘要： Synthetic macromolecular conjugate for selective interaction with proteins has a synthetic copolymer, and at least one binding group and at least one further group selected from an affinity tag and an imaging probe, and at least one binding group and at least one further group being bound via covalent bond to the synthetic copolymer. The macromolecular conjugate is suitable in particular for identification, visualization, quantification or isolation of proteins and/or cells.

公开(公告)号：EP3245513B1

公开(公告)日：2019-07-10

申请号：EP16706121.7

申请日：2016-01-13

申请人： Ustav Organicke Chemie a Biochemie Akademie Ved Ceske Republiky, V.V.I. ,  Ustav Makromolekularni Chemie AV CR, v.v.i. ,  Univerzita Karlova v Praze, Prírodovedecká fakulta

发明人： SACHA, Pavel ,  KONVALINKA, Jan ,  SCHIMER, Jiri ,  KNEDLIK, Tomas ,  SUBR, Vladimir ,  ULBRICH, Karel ,  STROHALM, Jiri

IPC分类号： G01N33/531 ,  G01N33/532 ,  G01N33/533 ,  G01N33/534 ,  C08F8/30

公开(公告)号：EP2283025B1

公开(公告)日：2011-12-07

申请号：EP09721251.8

申请日：2009-03-19

申请人： Ustav Organicke Chemie a Biochemie Akademie Ved Ceske Republiky, V.V.I.

发明人： SLAVIKOVA, Barbora ,  KASAL, Alexander ,  KOHOUT, Ladislav ,  BUDESINSKY, Milos ,  SWACZYNOVA, Jana

IPC分类号： C07J1/00 ,  A01N45/00

CPC分类号： C07J1/007 ,  A01N45/00 ,  Y02P20/55

摘要： 5-Fluoro-3α,17β-dihydroxy-5α-androstan-6-one IV and the method of its production are described. The synthesis consists of partial hydrolyses of 5-fluoro-6-oxo-5α-androstan-3β,17β-diyl diacetate with mild alkaline agent to 5-fluoro-3β-hydroxy-6-oxo-5α-androstan-17β-yl acetate that on solvolytic change of hydroxyl configuration in position 3 affords 5-fluoro-3α-hydroxy-6-oxo-5α-androstan-17β-yl acetate, which on deprotection afforded desired 5-fluoro-3α,17β-dihydroxy-5α-androstan-6-one IV. The invention relates also to the use of 5-fluoro-3α,17β-dihydroxy-5α-androstaii-6-one IV for influencing of plant growth, especially for increasing of plant yield and also for removal of plant stresses.