Patents Assigned to Ustav Organicke Chemie A Biochemie AV CR, V.V.I.
  • Publication number: 20200330484
    Abstract: The present invention provides steroidal compounds for the treatment of mental and neurological disorders by targeted rectification of defects caused by a mutation occurring in the membrane region of a human N-methyl-D-aspartate receptor subunit by potentiation of the effects of the said receptor.
    Type: Application
    Filed: November 26, 2018
    Publication date: October 22, 2020
    Applicants: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., FYZIOLOGICKY USTAV AV CR, V. V. I.
    Inventors: Eva KUDOVA, Ladislav VYKLICKY
  • Publication number: 20200291139
    Abstract: 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.
    Type: Application
    Filed: March 15, 2017
    Publication date: September 17, 2020
    Applicant: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.
    Inventors: Tomas KRAUS, Zbigniew ZAWADA
  • Patent number: 10759826
    Abstract: 15?-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.
    Type: Grant
    Filed: June 7, 2017
    Date of Patent: September 1, 2020
    Assignees: 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
    Inventors: Martin Kotora, Eva Prchalova, Jerzy Adamski, Gabriele Moeller, Ondrej Stepanek, Petr Bartunek, David Sedlak, Marian Hajduch, Petr Dzubak
  • Patent number: 10751390
    Abstract: 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 ?-alanine, ?-aminobutyric acid or ?-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.
    Type: Grant
    Filed: August 26, 2019
    Date of Patent: August 25, 2020
    Assignee: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.
    Inventors: Lenka Maletinska, Blanka Zelezna, Miroslava Blechova, Andrea Spolcova, Barbora Mikulaskova, Jaroslav Kunes, Stepan Strnad
  • Patent number: 10730905
    Abstract: Substituted heteropentadieno-pyrrolopyrimidine ribonucleosides of general formula I, where R is selected from the group comprising furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl or chloro, and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers.
    Type: Grant
    Filed: July 31, 2017
    Date of Patent: August 4, 2020
    Assignees: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., UNIVERZITA PALACKEHO V OLOMOUCI
    Inventors: Michal Hocek, Anna Tokarenko, Sabina Smolen, Marian Hajduch, Petr Dzubak
  • Publication number: 20200199080
    Abstract: The invention describes the pyrimidine-based compounds of the general formula I. Described compounds lower the production of the prostaglandin E2. In concentrations lowering production of this factor by 50%, these compounds have no negative effect on the cell viability and they are not cytotoxic. Furthermore, the method of production of the compounds of the general formula I is provided. A pharmaceutical composition comprising the polysubstituted pyrimidines according to the invention and the use of these compounds for the treatment of the inflammatory diseases are also provided.
    Type: Application
    Filed: May 23, 2018
    Publication date: June 25, 2020
    Applicants: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., USTAV EXPERIMENTALNI MEDICINY AV CR, V.V.I.
    Inventors: VIKTOR KOLMAN, Filip KALCIC, Zlatko JANEBA, Zdenek ZIDEK
  • Publication number: 20200095278
    Abstract: Compounds useful for the treatment of malaria, cancer, Parkinson's disease, diabetes, and bacterial infection.
    Type: Application
    Filed: June 12, 2018
    Publication date: March 26, 2020
    Applicant: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.
    Inventors: Kvido STRISOVSKY, Pavel MAJER, Stanco STANCEV, Anezka TICHA
  • Patent number: 10590091
    Abstract: Process for the preparation of azidoperfluoroalkanes and azidopolyfluoroalkanes of general formula RF—N3, where RF is chosen from a group containing CnF2n+1, CnFxH2n+1?x, CnFxX2n+1?x or R1CF2CF2, where n is an integer in the range of 1 to 10, x is an integer in the range of 2 to 20, X is Cl, Br, or I, R1 is C1-10 alkyl, ArO, ArS, imidazolyl, benzimidazolyl, or pyrazolyl and Ar is phenyl or substituted phenyl, by the reaction of electrophilic azidation reagent of general formula R2—N3, where R2 is n-C4F9SO2, ArSO2, Br, I, with synthetic equivalent of polyfluoroalkylated carbanion of general formula [RF]?.
    Type: Grant
    Filed: November 30, 2017
    Date of Patent: March 17, 2020
    Assignees: Ustav Organicke Chemie A Biochemie AV CR , v.v.i., CF Plus Chemicals s.r.o.
    Inventors: Petr Beier, Vaclav Matousek, Zsofia E. Blastik, Svatava Voltrova
  • Publication number: 20190330258
    Abstract: 15?-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.
    Type: Application
    Filed: June 7, 2017
    Publication date: October 31, 2019
    Applicants: 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
    Inventors: Martin KOTORA, Eva PRCHALOVA, Jerzy ADAMSKI, Gabriele MOELLER, Ondrej STEPANEK, Petr BARTUNEK, David SEDLAK, Marian HAJDUCH, Petr DZUBAK
  • Patent number: 10414788
    Abstract: 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.
    Type: Grant
    Filed: June 29, 2016
    Date of Patent: September 17, 2019
    Assignees: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., UNIVERZITA PALACKEHO V OLOMOUCI
    Inventors: Michal Hocek, Michal Tichy, Marian Hajduch, Petr Dzubak
  • Publication number: 20190240456
    Abstract: A catheter that has a catheter tube everting inside-out during the process of catheterization. The catheter tube has a plurality of longitudinal protrusions extending from the first end of the catheter tube through at least a portion of the catheter tube, and forming an angle of 0 degrees to 45 degrees with respect to the longitudinal axis of the catheter tube and facing radially inwards, and provides for dilating a circumference of the catheter tube upon everting the catheter tube inside-out from the first end of the catheter tube.
    Type: Application
    Filed: August 30, 2017
    Publication date: August 8, 2019
    Applicants: RIOCATH MEDICAL DEVICES A.S., USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.
    Inventors: VIT POKORNY, Miroslav SVOBODA
  • Publication number: 20190161452
    Abstract: Process for the preparation of azidoperfluoroalkanes and azidopolyfluoroalkanes of general formula RF—N3, where RF is chosen from a group containing CnF2n+1, CnFxH2n+1?x, CnFxX2n+1?x or R1CF2CF2, where n is an integer in the range of 1 to 10, x is an integer in the range of 2 to 20, X is Cl, Br, or I, R1 is C1-10 alkyl, ArO, ArS, imidazolyl, benzimidazolyl, or pyrazolyl and Ar is phenyl or substituted phenyl, by the reaction of electrophilic azidation reagent of general formula R2—N3, where R2 is n-C4F9SO2, ArSO2, Br, I, with synthetic equivalent of polyfluoroalkylated carbanion of general formula [RF]?.
    Type: Application
    Filed: November 30, 2017
    Publication date: May 30, 2019
    Applicants: Ustav organicke chemie a biochemie AV CR, v.v.i., CF Plus Chemicals s.r.o.
    Inventors: Petr BEIER, Vaclav MATOUSEK, Zsofia E. BLASTIK, Svatava VOLTROVA
  • Patent number: 10302632
    Abstract: A macromolecular water-soluble conjugates based on synthetic copolymers to which at least one affinity tag, at least one imaging probe and at least one targeting ligand are bound via covalent bonds. The macromolecular conjugate may be used in identification, visualization, quantification or isolation of proteins and/or cells.
    Type: Grant
    Filed: September 12, 2018
    Date of Patent: May 28, 2019
    Assignees: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., USTAV MAKROMOLEKULARNI CHEMIE AV CR, V.V.I., UNIVERZITA KARLOVA V PRAZE, PRIRODOVEDECKA FAKULTA
    Inventors: Pavel Sacha, Jan Konvalinka, Jiri Schimer, Tomas Knedlik, Vaclav Navratil, Jan Tykvart, Frantisek Sedlak, Pavel Majer, Petr Cigler, Vladimir Subr, Karel Ulbrich, Jiri Strohalm
  • Publication number: 20190144487
    Abstract: 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.
    Type: Application
    Filed: June 29, 2016
    Publication date: May 16, 2019
    Applicants: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., UNIVERZITA PALACKEHO V OLOMOUCI
    Inventors: MICHAL HOCEK, Michal TICHY, Marian HAJDUCH, Petr DZUBAK
  • Publication number: 20190144486
    Abstract: Substituted heteropentadieno-pyrrolopyrimidine ribonucleosides of general formula I, where R is selected from the group comprising furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl or chloro, and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers.
    Type: Application
    Filed: July 31, 2017
    Publication date: May 16, 2019
    Applicants: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., UNIVERZITA PALACKEHO V OLOMOUCI
    Inventors: Michal HOCEK, Anna TOKARENKO, Sabina SMOLEN, Marian HAJDUCH, Petr DZUBAK
  • Publication number: 20190033300
    Abstract: A macromolecular water-soluble conjugates based on synthetic copolymers to which at least one affinity tag, at least one imaging probe and at least one targeting ligand are bound via covalent bonds. The macromolecular conjugate may be used in identification, visualization, quantification or isolation of proteins and/or cells.
    Type: Application
    Filed: September 12, 2018
    Publication date: January 31, 2019
    Applicants: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., USTAV MAKROMOLEKULARNI CHEMIE AV CR, V.V.I., UNIVERZITA KARLOVA V PRAZE, PRIRODOVEDECKA FAKULTA
    Inventors: PAVEL SACHA, JAN KONVALINKA, JIRI SCHIMER, TOMAS KNEDLIK, VACLAV NAVRATIL, JAN TYKVART, FRANTISEK SEDLAK, PAVEL MAJER, PETR CIGLER, VLADIMIR SUBR, KAREL ULBRICH, JIRI STROHALM
  • Patent number: 10160785
    Abstract: Synthetic analogs of general formula (I-A), (I-A) a-Ile-b-c-d-e-f-Lys-Lys-g-h-i-j-Ile-k-Lys-NH2 where a is Gly, Lys or ?-Ala; b is Met, Leu, Nle, Ile, Trp, Val or Phe; c is Ser, Lys, Arg or Orn; d is Ser, Lys, Arg or Orn; e is Leu, Nle, Ile, Trp, Val or Phe; f is Met, Leu, Nle, Ile, Trp, Val or Phe; g is Leu, Nle, Ile or Trp; h is Lys, Arg, Orn or Ala; i is Lys, Arg, Orn or Ala; j is Ile, Leu, Nle or His; k is Lys, Arg, Orn or Ala; where amino acids in all positions may be in D-configuration, and their use for the treatment of topical infections caused by pathogenic bacteria or yeasts.
    Type: Grant
    Filed: April 8, 2016
    Date of Patent: December 25, 2018
    Assignees: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., FYZIOLOGICKY USTAV AV CR, V.V.I.
    Inventors: Vaclav Cerovsky, Ondrej Nesuta, Vlasta Dudkova, Hana Sychrova, Marie Kodedova
  • Patent number: 10114014
    Abstract: 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.
    Type: Grant
    Filed: January 13, 2016
    Date of Patent: October 30, 2018
    Assignees: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., USTAV MAKROMOLEKULARNI CHEMIE AV CR, V.V.I., UNIVERZITA KARLOVA
    Inventors: Pavel Sacha, Jan Konvalinka, Jiri Schimer, Tomas Knedlik, Vladimir Subr, Karel Ulbrich, Jiri Strohalm
  • Patent number: 10017535
    Abstract: Amphiphilic compounds with tetradecahydrophenanthrene skeleton and their enantiomers, exhibiting neuroprotective effects, their use in methods of treatment of neuropsychiatric disorders associated with an imbalance in glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post-traumatic stress disorder and diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addiction, multiple sclerosis, epilepsy, glioma, and a pharmaceutical composition containing compound.
    Type: Grant
    Filed: August 25, 2015
    Date of Patent: July 10, 2018
    Assignees: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., FYZIOLOGICKY USTAV AV CR, V.V.I.
    Inventors: Eva Kudova, Hana Chodounska, Vojtech Kapras, Ladislav Vyklicky, Karel Vales, Ullrich Jahn
  • Patent number: 9932339
    Abstract: Helquat derivatives of general formula I, in which substituents R1 and R2 are independently selected from a group comprising H and C1 to C4 alkyl, up to three of S1,2, S1?,2?, S3,4 and S3?,4? are present, each of S1,2, S1?,2?, S3,4 and S3?,4? independently represents a linker consisting of a bivalent hydrocarbon chain having 3-6 carbon atoms, preferably hydrocarbon chain having 4 carbon atoms, and one to four atoms selected from the carbon atoms with the descriptor 2, 4, 2?, and 4? are substituted with a substituent R3 of general formula II, wherein R4 is substituted or unsubstituted heteroaryl, T1 and T2 are independent linkers that bridge atoms N5 with C8 and N5? with C8?, wherein T1 and T2 independently represent a bivalent hydrocarbon chain having 2-5 carbon atoms, preferably 2 or 3 carbon atoms; and anions (X1)? and (X2)? independently represent anions of pharmaceutically acceptable salts.
    Type: Grant
    Filed: May 26, 2015
    Date of Patent: April 3, 2018
    Assignees: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., VYSOKA SKOLA CHEMICKO-TECHNOLOGICKA V PRAZE
    Inventors: Filip Teply, Miroslav Hajek, Erika Kuzmova, Jaroslav Kozak, Veronika Komarkova, Pavla Hubalkova, Paul Eduardo Reyes-Gutierrez, Michael Jirasek, Manoj R. Sonawane, Vishwas D. Joshi, Lukas Severa, Jana Novotna