Patents by Inventor István Borza

István Borza has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 11026946
    Abstract: The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention al so relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention al so provides a method for manufacture of medicaments useful in the treatment of such disorders.
    Type: Grant
    Filed: March 12, 2018
    Date of Patent: June 8, 2021
    Assignee: RICHTER GEDEON NYRT.
    Inventors: István Borza, Viktor Román, János Éles, Zsuzsa Hadady
  • Patent number: 10960007
    Abstract: The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention also relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention also provides a method for manufacture of medicaments useful in the treatment of such disorders.
    Type: Grant
    Filed: March 12, 2018
    Date of Patent: March 30, 2021
    Assignee: RICHTER GEDEON NYRT.
    Inventors: István Borza, Viktor Román, János Éles, Zsuzsa Hadady, József Huszár
  • Publication number: 20200129515
    Abstract: The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention al so relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention al so provides a method for manufacture of medicaments useful in the treatment of such disorders.
    Type: Application
    Filed: March 12, 2018
    Publication date: April 30, 2020
    Inventors: István BORZA, Viktor ROMÁN, János ÉLES, Zsuzsa HADADY
  • Publication number: 20200061068
    Abstract: The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention also relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention also provides a method for manufacture of medicaments useful in the treatment of such disorders.
    Type: Application
    Filed: March 12, 2018
    Publication date: February 27, 2020
    Inventors: István BORZA, Viktor ROMAN, János ÉLES, Zsuzsa HADADY, József HUSZÁR
  • Publication number: 20130217702
    Abstract: The present invention relates to the indole derivatives of formula (I), wherein R1-R6 and X are defined in the claims and optical antipodes or racemates and/or salts thereof which are selective antagonists of bradykinin B1 to process for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: November 4, 2011
    Publication date: August 22, 2013
    Inventors: Gyula Beke, Gyula Attila Bényei, István Borza, Éva Bozó, Sándor Farkas, Katalin Hornok, Andrea Papp, István Vágó, Mónika Vastag
  • Patent number: 8008326
    Abstract: The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica.
    Type: Grant
    Filed: July 21, 2005
    Date of Patent: August 30, 2011
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Istvan Borza, Csilla Horvath, Sandor Farkas, Istvan Gyertyan, Jozsef Nagy, Sandor Kolok, Kornel Galgoczy, Katalin Saghy
  • Publication number: 20090170901
    Abstract: The new benzoyl urea derivatives of formula (I) wherein the meaning of X and Y independently are hydrogen atom, hydroxy, benzyloxy, amino, nitro, C1-C4 alkylsulfonamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkoxy, aroyl-carbamoyl optionally substituted with halogen atom or C1-C4 alkyl or C1-C4 alkoxycarbonyl group, or the neighboring X and Y groups optionally form together with one or more identical or different additional hetero atom and —CH? and/or —CH2— groups an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably morpholine, pyrrole, pyrrolidine, oxo- or thioxo-pyrrolidine, pyrazole, pyrazolidine, imidazole, imidazolidine, oxo- or thioxo-imidazole or imidazolidine, 1,4-oxazine, oxazole, oxazolidine, triazole, oxo- or thioxo-oxazolidine, or 3-oxo-1,4-oxazine ring, V and Z independently are hydrogen or halogen atom, cyano, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl, hydroxy o
    Type: Application
    Filed: July 21, 2005
    Publication date: July 2, 2009
    Inventors: Istvan Borza, Gizella Bartané Szalai, Eva Bozo, Csilla Acsné Kiss, Csilla Horvath, Sandor Farkas, Jozsef Nagy, Sandor Kolok
  • Publication number: 20090048303
    Abstract: The present invention relates therefore first to new indole-2-carboxamidine derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl group, Y, V and Z independently are hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, trifluoromethyl, trifluoromethoxy, C1-C4 alkyl, C1-C4 alkoxy group, or the neighboring V and Z groups in given case together with one or more identical or different additional hetero atom and —CH? and/or —CH2— groups can form an optionally substituted 4-7 membered homo- or heterocyclic ring, preferably benzene, dioxolane ring, A, B and C independently are substituted carbon atom or one of them is nitrogen atom, and the salts thereof.
    Type: Application
    Filed: July 21, 2005
    Publication date: February 19, 2009
    Inventors: Istvan Borza, Csilla Horvath, Sandor Farkas, Jozsef Nagy, Sandor Kolok
  • Publication number: 20090012118
    Abstract: The new kynurenic acid amide derivatives of formula (I): and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor.
    Type: Application
    Filed: July 21, 2005
    Publication date: January 8, 2009
    Inventors: István Borza, Csilla Horvath, Sandor Farkas, Jozsef Nagy, Sandor Kolok
  • Publication number: 20080312222
    Abstract: The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica.
    Type: Application
    Filed: July 21, 2005
    Publication date: December 18, 2008
    Inventors: Istvan Borza, Csilla Horvath, Sandor Farkas, Istvan Gyertyan, Jozsef Nagy, Sandor Kolok, Kornel Galgoczy, Katalin Saghy
  • Publication number: 20080300276
    Abstract: The invention relates to new heterocyclic carboxylic acid amide derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, arylsulfonamido groups, is —CH? group or —N? atom, Z is one or more hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, cyano, trifluromethyl, trifluoromethoxy group and to the salts thereof, which are antagonists of NMDA receptor or are intermediates for preparing thereof.
    Type: Application
    Filed: July 21, 2005
    Publication date: December 4, 2008
    Inventors: Istvan Borza, Csilla Horvath, Sandor Farkas, Istvan Gyertyan, Jozsef Nagy, Sandor Kolok, Kornel Galgoczy, Katalin Saghy
  • Patent number: 7435744
    Abstract: The present invention relates to a compound of formula (I): wherein: V and U are hydrogen, halogen, C1-C4 alkylamino, or together form a group that contains one or more heteroatoms, and that taken together with one or more: (a) hydrogen atoms; (b) carbon atoms; (c) —CH? groups; (d) —CH2— groups; or (e) additional heteroatoms of the same or different type; or any combination thereof, form a 4-7 membered homocyclic or heterocyclic ring, wherein the homocyclic or heterocyclic ring may combine with the phenyl group to form a bicyclic ring, and wherein the homocyclic or heterocyclic ring or the bicyclic ring may contain one or more oxo, thioxo, amino, mercapto, trifluoromethyl, C1-C4 alkyl, ?S or —SH groups; W: is —CO—, —CH2— or —CH2—(C1-C4 alkyl)-; X: is —CO—; Y: is —O—, C1-C4 alkylene, C1-C4 alkynylene, cycloalkylene, aminocarbonyl, —NH—, —N(C1-C4 alkyl)-, -C1-C4 alkylene-N(C1-C4 alkyl)-, —CH2O—, —CH(OH)— or —OCH2—; Z: is hydrogen, halogen, nitro, amino, C1-C4 alkyl, C1-C4 alkoxy, cyano, trifluorometh
    Type: Grant
    Filed: January 21, 2004
    Date of Patent: October 14, 2008
    Assignee: Gedeon Richter Vegyeszeti Gyar RT
    Inventors: Gyorgy Domány, Csilla Horváth, Gizella Bartáné Szalai, József Nagy, Sándor Kolok, Éva Kovácsné Bozó, István Borza, István Vágó, Attila Bielik, Györgyi Ignáczné Szendrei, György Keserü, Sándor Farkas
  • Patent number: 7378431
    Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a nitrogen atom, or pharmaceutically acceptable salts thereof formed with acids or bases.
    Type: Grant
    Filed: December 29, 2004
    Date of Patent: May 27, 2008
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csilla Horvath, Sandor Farkas, György Domany, Istvan Borza, Gizella Bartane Szalai, Jozsef Nagy, Sandor Kolok
  • Patent number: 7375116
    Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) where two of the neighboring R1, R2, R3 and R4 groups form an imidazole ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
    Type: Grant
    Filed: December 29, 2004
    Date of Patent: May 20, 2008
    Assignee: Richter Gedeon Vegyeszeti Gyar RT.
    Inventors: Csilla Horvath, Sandor Farkas, György Domany, Istvan Borza, Gizella Bartane Szalai, Jozsef Nagy, Sandor Kolok
  • Patent number: 7365083
    Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein two of the neighboring R1, R2, R3 and R4 groups form an oxo-oxazolidine ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
    Type: Grant
    Filed: December 28, 2004
    Date of Patent: April 29, 2008
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csilla Horvath, Sandor Farkas, György Domany, Istvan Borza, Gizella Bartane Szalai, Jozsef Nagy, Sandor Kolok
  • Patent number: 7361670
    Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
    Type: Grant
    Filed: December 28, 2004
    Date of Patent: April 22, 2008
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csilla Horvath, Sandor Farkas, György Domany, Istvan Borza, Gizella Bartane Szalai, Jozsef Nagy, Sandor Kolok
  • Publication number: 20050159451
    Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) where two of the neighboring R1, R2, R3 and R4 groups form an imidazole ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
    Type: Application
    Filed: December 29, 2004
    Publication date: July 21, 2005
    Inventors: Csilla Horvath, Sandor Farkas, Gyorgy Domany, Istvan Borza, Gizella Szalai, Jozsef Nagy, Sandor Kolok
  • Patent number: 6919355
    Abstract: New Formula (I) compounds are disclosed having NR2B selective NMDA receptor antagonist activity: wherein one of the neighboring R1, R2, R3 and R4 groups is OH or NH2 and the others are each hydrogen , or two of the neighboring R1, R2 R3 and R4 groups in given case together with one or more identical or different additional hetero atom and —CH? and/or —CH2— groups forms a 5-6 membered homo- or heterocyclic ring, preferably pyrrole, pyrazole, imidazole, oxazole, oxo-oxazolidine, or 3-oxo-1,4-oxazine ring, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by hydroxy group, and/or in given case phenyl or phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), anilino, phenyl-(C1-C4 alkylamino), [phenyl-(C1-C4 alkyl)]-amino, benzoyl, hydroxy-diphenylmethyl, C1-C4 alkoxycarbonyl-phenoxymethyl or benzhydrylidene group, optionally substitut
    Type: Grant
    Filed: April 11, 2003
    Date of Patent: July 19, 2005
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csilla Horvath, Sandor Farkas, György Domany, Istvan Borza, Gizella Bartane Szalai, Jozsef Nagy, Sandor Kolok
  • Publication number: 20050113359
    Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
    Type: Application
    Filed: December 28, 2004
    Publication date: May 26, 2005
    Inventors: Csilla Horvath, Sandor Farkas, Gyorgy Domany, Istvan Borza, Gizella Bartane Szalai, Jozsef Nagy, Sandor Kolok
  • Publication number: 20050113360
    Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein two of the neighboring R1, R2, R3 and R4 groups form an oxo-oxazolidine ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.
    Type: Application
    Filed: December 28, 2004
    Publication date: May 26, 2005
    Inventors: Csilla Horvath, Sandor Farkas, Gyorgy Domany, Istvan Borza, Gizella Bartane Szalai, Jozsef Nagy, Sandor Kolok