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1. 发明公开

US20230265049A1 Lipidoids for Nucleic Acid Transfection and Use Thereof 审中-公开
公开(公告)号：US20230265049A1
公开(公告)日：2023-08-24
申请号：US18015254
申请日：2021-07-23
申请人： Ustav Organicke Chemie a Biochemie AV CR, v.v.i.
发明人： Petr CIGLER , Klara GRANTZ SASKOVA , Vaclav VANEK , Zuzana KRUZIKOVA , Frantisek SEDLAK
IPC分类号： C07C233/62 , A61K48/00 , A61K9/51 , C12N15/11 , A61P43/00
CPC分类号： C07C233/62 , A61K48/0033 , A61K9/5123 , C12N15/11 , A61P43/00 , C12N2320/30
摘要： The subject of the present invention is a lipidoid of general formula (I), wherein X, Y, Z and R are as defined in the claims. This lipidoid is useful as a transfection agent. The invention further describes transfection agents, transfection particles containing this lipidoid, and their use.

2. 发明申请

US20220259119A1 COMPOUNDS FOR CHROMATOGRAPHIC SEPARATION OF RARE EARTH ELEMENTS AND S-, P-, D-METALS, METHOD OF SEPARATION, AND USE THEREOF 有权
公开(公告)号：US20220259119A1
公开(公告)日：2022-08-18
申请号：US17616340
申请日：2020-05-28
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I
发明人： Miloslav Polasek
IPC分类号： C07B59/00 , C07D401/06 , C07F9/6524 , C07D401/14 , B01D15/42
摘要： The present invention relates to compounds of general formula (I), wherein —X is selected from a group consisting of H; C1 to C6, alkyl; halogen (F, Cl, Br or I); Y is selected from a group consisting of nitrogen; N-oxide; Z1, Z2, Zm, wherein m is 1 or 2, are independently selected from the group consisting of —CH2—CH2— and —CH2—CH2—CH24 A, Am, wherein m is 1 or 2, are independently selected from H; —CH2COOH; —CH2C(O)NH2; —CH2P(O)(OH)2, and n is 1 or 2; R1, R2, R3 are independently H; C1 to C6, alkyl; C1 to C6 alkyloxy; C6 to C10 aryloxy; benzyloxy; C1 to C6 alkylthio; C6, to C10 arylthio; F; Cl; Br; I; OH; SH; NH2; C1 to C6, alkylamino; di(C1 to C6, alkyl)amino; C1 to C6 acylamino; di(C1 to C6 acyl) amino; C6 to C10 arylamino; di(C6 to C10 aryl)amino; CN; OH; nitro; COORn, C(O)NHRn, C(O)N(Rn)2, wherein Rn is independently H or C1 to C10 alkyl or C6, to C10 aryl; and/or neighboring two of R1, R2, R3 together with neighboring two carbon atoms of the aromatic cycle form a six-membered ring, optionally substituted with one or more substituents independently selected from the group consisting of OH, SH, CF3, F, Cl, Br, I, C1 to C6, alkyl, C1to C6, alkyloxy, C1 to C6 alkylthio, NH2, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, NO2, COOH, COORn, C(O)NHRn, C(O)N(Rn)2, wherein Rn is WO 2020/244686 A1 independently H or C1 to C10 alkyl or C6 to C10 aryl; with the proviso that when n is 2 and all of Z1, Z2, Zm are —CH2—CH2—, then A is not —CH2COOH; for chromatographic separation of rare earth elements and/or s-, p- and d-block metals, as well as to the method of the separation of rare earth elements.

3. 发明申请

US20220177514A1 A METHOD FOR FUNCTIONALIZATION OF AN AROMATIC AMINO ACID OR A NUCLEOBASE 有权
公开(公告)号：US20220177514A1
公开(公告)日：2022-06-09
申请号：US17603400
申请日：2020-05-05
申请人： CF PLUS CHEMICALS S.R.O. , USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I. , MIKROBIOLOGICKY USTAV AV CR, V.V.I.
发明人： Vaclav MATOUSEK , Petr BEIER , Petr NOVAK
IPC分类号： C07K1/107 , C07D209/16 , C07C217/60 , C07C69/02 , C07C247/04 , C07C309/58 , C07C43/225 , C07C227/16 , C07D233/64 , C07H1/00 , C07B39/00
摘要： A method for functionalization of an aromatic amino acid or a nucleobase with a fluoroalkyl-containing moiety RF, wherein the aromatic amino acid is reacted in the presence of at least one reductant with at least one hypervalent iodine fluoroalkyl reagent carrying the floroalkyl-containing moiety RF is disclosed. Novel hypervalent iodine fluoroalkyl reagents is also disclosed.

4. 发明授权

US10759826B2 15β-substituted estrone derivatives as selective inhibitors of 17β-hydroxysteroid-dehydrogenases, method of preparation and use thereof 有权
公开(公告)号：US10759826B2
公开(公告)日：2020-09-01
申请号：US16305829
申请日：2017-06-07
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I. , USTAV MOLEKULARNI GENETIKY AKADEMIE VED CR, V.V.I. , UNIVERZITA PALACKEHO V OLOMOUCI , HELMHOLTZ ZENTRUM MUNCHEN
发明人： Martin Kotora , Eva Prchalova , Jerzy Adamski , Gabriele Moeller , Ondrej Stepanek , Petr Bartunek , David Sedlak , Marian Hajduch , Petr Dzubak
IPC分类号： A61K31/566 , C07J1/00
摘要： 15β-substituted derivatives of estrone of general formula I wherein R1, R2, R3, R4, R5 are independently selected from the group consisting of: C1-C4 alkyl, C1-C4 alkoxy, C1-C4 halogenalkyl, halogen, COOR6 wherein R6 is C1-C4 alkyl; H, OH; optionally, R3, R4 and R5 are each formed by a hydrogen atom, while R1 and R2 together form an aryl group, preferably naphthyl, in which the aromatic ring in position C-15 can be mono-, di-, tri-, tetra- and penta-substituted with substituents R1-R5. Compounds of the invention may be used for diagnosis and possibly also for the treatment of estrogen-dependent diseases.

5. 发明申请

US20200016240A1 LIPIDATED PEPTIDES AS NEUROPROTECTIVE AGENTS 审中-公开
公开(公告)号：US20200016240A1
公开(公告)日：2020-01-16
申请号：US16550654
申请日：2019-08-26
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.
发明人： Lenka Maletinska , Blanka Zelezna , Miroslava Blechova , Andrea Spolcova , Barbora Mikulaskova , Jaroslav Kunes , Stepan Strnad
IPC分类号： A61K38/22 , A61P25/28
摘要： Lipidated neuropeptides PrRP31, PrRP20, containing C14 to C16 fatty acid, and their analogs, wherein a sequence of IRPVGRF-NH2 at the C-terminus is variable in the site of isoleucine, valine and phenylalanine; said fatty acid is bound in position 1 or 11 for PrRP31 or its analog and in position 1 or 7 for PrRP20 or its analog; the bond comprises an amide bond between an amino acid having at least one free NH2 group and a carboxylic group of the fatty acid and alternatively includes also a binding through arm X2, which is a hydrophilic linker selected from a group comprising β-alanine, γ-aminobutyric acid or γ-glutamic acid; for use in the treatment and prevention of diseases, which are Alzheimer's disease (AD), Parkinson's disease (PD), cognitive impairment no dementia (CIND), brain trauma, and neurodegenerative changes and disorders.

6. 发明申请

US20190144487A1 SUBSTITUTED THIENOPYRROLOPYRIMIDINE RIBONUCLEOSIDES FOR THERAPEUTIC USE 审中-公开
公开(公告)号：US20190144487A1
公开(公告)日：2019-05-16
申请号：US16098068
申请日：2016-06-29
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I. , UNIVERZITA PALACKEHO V OLOMOUCI
发明人： MICHAL HOCEK , Michal TICHY , Marian HAJDUCH , Petr DZUBAK
IPC分类号： C07H19/24 , A61P35/00
CPC分类号： C07H19/24 , A61P35/00
摘要： A group of substituted thienopyrrolopyrimidine ribonucleosides of general formula I, in which R shows strong cytostatic and cytotoxic activities preferably against cancer cell lines of broad spectrum of diseases including tumors of various histogenetic origin.

7. 发明申请

US20180011085A1 MACROMOLECULAR CONJUGATES FOR ISOLATION, IMMOBILIZATION AND VISUALIZATION OF PROTEINS 审中-公开
公开(公告)号：US20180011085A1
公开(公告)日：2018-01-11
申请号：US15542792
申请日：2016-01-13
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I. , USTAV MAKROMOLEKULARNI CHEMIE AV CR, V.V.I. , UNIVERZITA KARLOVA
发明人： Pavel Sacha , Jan KONVALINKA , Jiri SCHIMER , Tomas KNEDLIK , Vladimir SUBR , Karel ULBRICH , Jiri STROHALM
IPC分类号： G01N33/532 , C08F8/30 , G01N33/533 , G01N33/58
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.

8. 发明申请

US20210015856A1 NANODIAMONDS AS ARTIFICIAL PROTEINS FOR REGULATION OF A CELL SIGNALLING SYSTEM 有权
公开(公告)号：US20210015856A1
公开(公告)日：2021-01-21
申请号：US16981578
申请日：2019-03-26
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I. , MASARYKOVA UNIVERZITA , FAKULTNI NEMOCNICE U SV. ANNY V BRNE
发明人： Petr CIGLER , Lukas BALEK , Jan HAVLIK , Pavel KREJCI , Lukas TRANTIREK , Silvie TRANTIRKOVA
IPC分类号： A61K33/44 , A61K9/14 , A61K45/06 , C07K14/50
摘要： Nanodiamonds having a positive ξ-potential of at least 1 mV for use in sequestration of at least one FGF family member in organisms in vivo and in vitro. It has been found that nanodiamonds with a positive ξ-potential show an extremely strong and selective binding to FGF family members, thus leading to their usability in the treatment of diseases related to aberrant FGF-FGFR signalling and/or interaction.

9. 发明申请

US20200291139A1 CYCLODEXTRI N-BASED TRANSPORTER OF NUCLEOSIDE TRIPHOSPHATE TRANSPORTER ACROSS THE CELL MEMBRANE, ITS PREPARATION AND USE 审中-公开
公开(公告)号：US20200291139A1
公开(公告)日：2020-09-17
申请号：US16084024
申请日：2017-03-15
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.
发明人： Tomas KRAUS , Zbigniew ZAWADA
IPC分类号： C08B37/16 , G01N33/483
摘要： Compounds of general formulae 6 and 13 where X is —NH—C(NH2)═N+H2 or —N+H3, Y is a linear oligomer of arginine units terminated with an aminodimethylenamide unit (—Arg)n—NH—(CH2)2—NH2, where n=6-10, or arginine-aminocaproic units (—Arg—Aca)n—NH2, where n=6 to 10, A—═CF3COO— or Cl— and m=1-2. Preparation and use of compounds of general formula 6 and 13 as carriers of nucleoside triphosphates across the cell membranes for the purpose of incorporation of modified nucleoside triphosphates into cellular DNA or RNA. Use of compounds of general formula 6 and 13 as carriers of nucleoside triphosphates across the cell membrane for determining the virostatic activities of modified nucleoside triphosphates. Use of compounds of general formula 6 and 13 as carriers of modified nucleoside triphosphates across the cell membrane for determining cell proliferation and S phase of the cell cycle.

10. 发明授权

US10751390B2 Lipidated peptides as neuroprotective agents 有权
公开(公告)号：US10751390B2
公开(公告)日：2020-08-25
申请号：US16550654
申请日：2019-08-26
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.
发明人： Lenka Maletinska , Blanka Zelezna , Miroslava Blechova , Andrea Spolcova , Barbora Mikulaskova , Jaroslav Kunes , Stepan Strnad
IPC分类号： A61K38/22 , A61P25/28
摘要： Lipidated neuropeptides PrRP31, PrRP20, containing C14 to C16 fatty acid, and their analogs, wherein a sequence of IRPVGRF-NH2 at the C-terminus is variable in the site of isoleucine, valine and phenylalanine; said fatty acid is bound in position 1 or 11 for PrRP31 or its analog and in position 1 or 7 for PrRP20 or its analog; the bond comprises an amide bond between an amino acid having at least one free NH2 group and a carboxylic group of the fatty acid and alternatively includes also a binding through arm X2, which is a hydrophilic linker selected from a group comprising β-alanine, γ-aminobutyric acid or γ-glutamic acid; for use in the treatment and prevention of diseases, which are Alzheimer's disease (AD), Parkinson's disease (PD), cognitive impairment no dementia (CIND), brain trauma, and neurodegenerative changes and disorders.

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