Abstract: The present invention relates to the use of 3?-hydroxychlormadinone acetate (17?-acetoxychloropregna-4,6-dien-3?-ol-20-one) and/or 3?-hydroxychlormadinone acetate (17?-acetoxychloropregna-4,6-dien-3?-ol-20-one) for producing a medicament for treating skin, preferably human skin by means of topical application, and to a pharmaceutical or cosmetic composition containing 3?-hydroxychlormadinone acetate and/or 3?-hydroxychlormadinone acetate.
Abstract: The invention relates to a process for the preparation of 17-hydroxy-6?,7?;15?,16?-bismethylene-17?-pregn-4-ene-3-one-21-carboxylic acid ?-lactone of formula (I) as well as to key-intermediates for this process.
Type:
Grant
Filed:
October 11, 2005
Date of Patent:
May 28, 2013
Assignee:
Richter Gedeon Nyrt.
Inventors:
György Gálik, Judit Horváth, Béla Sörös, Sándor Mahö, Zoltán Tuba, Gábor Balogh
Abstract: The present invention relates to a novel selective synthesis of 9?-hydroxy-steroid derivatives of the general formula (I) (I)—wherein the meaning of -A-A?- is —CH2—CH2— or —CH?CH— group—by the bioconversion of compounds of the general formula (II) (II) wherein the meaning of -A-A?- is —CH2—CH2— or —CH?CH— group—by using Nocardia farcinica bacterium strain, deposition number of which is NCAIM (P)—B 001342, as hydroxylating microorganism in the bioconversion.
Type:
Grant
Filed:
June 30, 2008
Date of Patent:
February 5, 2013
Assignee:
Richter Gedeon Nyrt.
Inventors:
Katalin Olasz, Anikó Tegdes, Valéria Gancsos, Gábor Hantos, Kálmán Könczöl, Gabor Balogh, Sándor Erdélyi
Abstract: The present invention relates to the use of at least one gestagen selected from the group consisting of chlormadinone acetate, 3?-hydroxy-6-chloro-17?-acetoxy-4,6-pregnadien-20-one (3?-hydroxy-chlormadinone acetate) and 3?-hydroxy-6-chloro-17?-acetoxy-4,6-pregnadien-20-one (3?-hydroxy-chlormadinone acetate) as gestagen component and optionally at least one oestrogen selected from the group consisting of ethinyl oestradiol, oestrone, oestriol as oestrogen component and oestradiol to produce a medicament for the treatment and/or prevention of melasma and optionally for simultaneous hormonal contraception or optionally for simultaneous hormone replacement for women.
Abstract: The invention relates to an industrial process for the preparation of 17-hydroxy-6?,7?;15?,16?-bismethylene-3-oxo-17?-pregn-4-ene-21-carboxylic acid ?-lactone of formula (I), and to the key-intermediates for this process.
Type:
Grant
Filed:
October 11, 2005
Date of Patent:
November 13, 2012
Assignee:
Richter Gedeon Nyrt.
Inventors:
Béla Sörös, Judit Horváth, György Gálik, József Bódi, Zoltán Tuba, Sándor Mahó, Gábor Balogh, Antal Aranyi
Abstract: Provided herein are Thieno[2,3-b]pyridine compounds with mGluR activity. Also provided herein are processes and intermediates for the preparation of the Thieno[2,3-b]pyridine compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in treatment, therapy, and/or prevention of conditions which require modulation of mGluR1 and mGluR5 receptors.
Type:
Grant
Filed:
June 24, 2009
Date of Patent:
September 11, 2012
Assignee:
Richter Gedeon Nyrt.
Inventors:
Istvan Gyertyan, Katalin Nogradi, Ottilia Elekes, Monika Vastag, Amrita Agnes Bobok, Katalin Saghy
Abstract: A pharmaceutical composition is disclosed containing amorphous rosuvastatin calcium and at least one of the following stabilizing agents: magnesium hydroxide, calcium acetate, calcium gluconate, calcium glycerophosphate, or aluminum hydroxide, together with at least one pharmaceutically acceptable excipient.
Abstract: The present invention relates to a process for the synthesis of the 17-acetoxy-11?-[4-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione of formula (I): from 3,3-[1,2-etandiyl-bis(oxy)]-oestr-5(10),9(11)-dien-17-one of formula (II):
Type:
Grant
Filed:
June 19, 2008
Date of Patent:
May 22, 2012
Assignee:
Richter Gedeon Nyrt.
Inventors:
József Bódi, György Visky, János Széles, Sándor Mahó, Csaba Sánta, János Csörgei, Zoltán Tuba, László Terdy, Csaba Molnár, Antal Aranyi, Zoltán Horváth, Gábor Balogh
Abstract: A process for the production of 1-(4-3(R)-[3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) according to the following reaction scheme: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI) where the substances of the general Formulas II, IV, VI, VIII, IX, X and XI are new, Formula III is a non-isolated intermediate, R1, R2 and R3 are represented by the compounds of Formulas Va-Vd, (Va), (Vb), (Vc), (Vd) and R4 is a silyl, e.g., tert-butyl-dimethyl-silyl, tert-butyl-diphenyl-silyl group.
Type:
Grant
Filed:
December 18, 2006
Date of Patent:
May 15, 2012
Assignee:
Richter Gedeon Nyrt.
Inventors:
József Bódi, János Éles, Katalin Szöke, Krisztina Vukics, Tamás Gáti, Krisztina Temesvári, Dorottya Kiss-Bartos
Abstract: A new industrial process for the synthesis of solvate-free 17?-acetoxy-11?-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB-2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process.
Type:
Grant
Filed:
May 18, 2007
Date of Patent:
February 7, 2012
Assignee:
Richter Gedeon Nyrt.
Inventors:
Lajosné Dancsi, György Visky, Zoltán Tuba, János Csörgei, Csaba Molnár, Endréné Magyari
Abstract: The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I) and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes and intermediates for their preparation, to pharmaceutical compositions containing these compounds and to their use in treatment and/or prevention of conditions which require modulation of mGluR1 and mGluR5 receptors.
Abstract: The present invention relates to methods of treating diabetic neuropathic pain comprising administering piperidine derivatives, such as 2-[4-(4-fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazol-6-yl)acetamide, and pharmaceutically acceptable salts thereof. Methods of treating post-herpetic neuralgia, chronic lower back pain, osteoarthritis and acute inflammatory pain are described.
Abstract: The invention relates to a process for the preparation of a phenolic hydroxy-substituted compound of the general formula (I) by desalkylation of an alkyl aryl ether of the general formula (II) by treatment with a thiourea/aluminum chloride reagent pair, in said general formulae R1 stands for straight chain or branched C1-6 alkyl group; R2, R3 , R4 , R5, and R6 have the same or different meanings and stand for hydrogen or halogen atom, hydroxy, carboxy, nitro, oxo, C1-6 alkylcarbonyl, straight chain or branched alkyl or -alkoxy, or aryl group, or R2 and R3 together stand for a 5-7 membered ring or fused ring system; said 5-7 membered ring may be a partially saturated ring optionally substituted with an oxo group or can be an unsaturated ring; or said fused ring system may constitute with the first ring a steroid, preferably an estratriene derivative optionally substituted with an oxo or C1-6 alkylcarbonyloxy group in the 17 position.
Type:
Grant
Filed:
December 7, 2005
Date of Patent:
July 5, 2011
Assignee:
Richter Gedeon Nyrt.
Inventors:
András Vass, József Dudás, László Borbély, Ferenc Haász, Péter Jekkel
Abstract: The present invention relates to novel monohydrochloride, dihydrochloride, monohydrobromide, maleate and methanesulphonate salts of trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and/or their hydrates and/or solvates. Moreover, the invention relates to the process for preparing the salts and their hydrates and/or solvates, to their use in the treatment and/or prevention of conditions which require modulation of dopamine receptor and to pharmaceutical compositions containing them.
Type:
Grant
Filed:
May 9, 2008
Date of Patent:
May 17, 2011
Assignee:
Richter Gedeon Nyrt.
Inventors:
Laszlo Czibula, Ferenc Sebok, Istvan Greiner, Gyorgy Domany, Eva Againe Csongor
Abstract: The present invention relates to new dopamine D3 and D2 ligands of formula (I): wherein R1, R2 and Q are as described herein, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes for preparing the same, to compositions containing the same and to their use in the treatment and/or prevention of conditions which requires modulation of dopamine receptors.
Type:
Grant
Filed:
December 3, 2008
Date of Patent:
January 25, 2011
Assignee:
Richter Gedeon Nyrt.
Inventors:
Gizella Bartane Szalai, Eva Againe Csongor, Gyorgy Domany, Istvan Gyertyan, Bela Kiss, Judit Laszy, Katalin Saghy, Eva Schmidt, Sandor Farkas, Zsolt Komlodi
Abstract: The invention relates to drospirenone containing film-coated tablet with improved resistance against the environmental influences, especially against atmospheric humidity. The invention further relates to a method for the preparation film-coated tablet cores whereby applying the active agent to the core may be accomplished with increased safety.
Type:
Application
Filed:
September 2, 2008
Publication date:
January 6, 2011
Applicant:
RICHTER GEDEON NYRT.
Inventors:
Attila Bodis, Istvan Greiner, Jonathan Mihaly Nagy Kasza
Abstract: Provided herein are Thieno[2,3-b]pyridine compounds with mGluR activity. Also provided herein are processes and intermediates for the preparation of the Thieno[2,3-b]pyridine compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in treatment, therapy, and/or prevention of conditions which require modulation of mGluR1 and mGluR5 receptors.
Type:
Application
Filed:
June 24, 2009
Publication date:
December 31, 2009
Applicant:
RICHTER GEDEON NYRT.
Inventors:
Istvan Gyertyan, Katalin Nogradi, Ottilia Elekes, Monika Vastag, Amrita Agnes Bobok, Katalin Saghy
Abstract: The present invention relates to a new industrial process for the synthesis of solvate-free 17?-acetoxy-11?-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB-2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process.
Abstract: The present invention relates to novel monohydrochloride, dihydrochloride, monohydrobromide, maleate and methanesulphonate salts of trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and/or their hydrates and/or solvates. Moreover, the invention relates to the process for preparing the salts and their hydrates and/or solvates, to their use in the treatment and/or prevention of conditions which require modulation of dopamine receptor and to pharmaceutical compositions containing them.
Type:
Application
Filed:
May 9, 2008
Publication date:
January 22, 2009
Applicant:
RICHTER GEDEON NYRT.
Inventors:
Laszlo Czibula, Ferenc Sebok, Istvan Greiner, Gyorgy Domany