Patents by Inventor Arwed Cleve
Arwed Cleve 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).
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Publication number: 20150203483Abstract: What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumour disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.Type: ApplicationFiled: August 13, 2013Publication date: July 23, 2015Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Stephan Siegel, Stefan Bäurle, Arwed Cleve, Bernard Haendler, Amaury Ernesto Fernandiez-Montalvan, Ursula Mönning, Sabine Krause, Pascale Lejeune, Norbert Schmees, Matthias Busemann, Simon Holton, Joachim Kuhnke
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Publication number: 20150080382Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: ApplicationFiled: June 24, 2014Publication date: March 19, 2015Inventors: Damian O. Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, Guo Ping Wei, Bin Ye
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Patent number: 8569303Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: GrantFiled: April 30, 2010Date of Patent: October 29, 2013Assignee: Celtaxsys, Inc.Inventors: Damian O Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J Kochanny, Amy Liang, David Light, John Parkinson, David Vogel, Guo Ping Wei, Bin Ye
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Publication number: 20120251551Abstract: The invention relates to substituted (heteroarylmethyl) thiohydantoin compounds of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, and their use for the preparation of medicaments for the treatment and/or prophylaxis of disorders, in particular of prostate cancer.Type: ApplicationFiled: August 28, 2010Publication date: October 4, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Lücking, Arwed Cleve, Bernard Haendler, Hortensia Faus Gimenez, Silke Köhr, Horst Irlbacher
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Publication number: 20120238533Abstract: The invention refers to the use of androgen receptor antagonists for the treatment and/or prevention of fibroids, also known as uterine leiomyoma, leiomyomata. Particularly, the invention refers to the use of an androgen receptor antagonist being any one of the compounds according to the following list: cyproterone acetate, oxendolone, chlormadinone acetate, spironolactone, osaterone acetate, dienogest, flutamide, hydroxyflutamide, nilutamide, bicalutamide, RU 58841, LGD-2226, MDV3100, BMS-641988, BMS-779333, or 4-(3-{[6-(2-hydroxy-2-methylpropoxy)pyridin-3-yl]methyl}-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile (thioxoimidazolidine derivative) for the treatment of fibroids.Type: ApplicationFiled: September 3, 2010Publication date: September 20, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Arwed Cleve, Ulrich Lücking, Stefan Bäurle, Martin Fritsch, Jens Schröder, Bernd-Wolfgang Igl
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Patent number: 8053426Abstract: The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.Type: GrantFiled: November 15, 2007Date of Patent: November 8, 2011Assignee: Bayer Schering Pharma AGInventors: Ulrike Fuhrmann, Anja Schmidt, Arwed Cleve, Orlin Petrov, Gunnar Garke, Stefan Pruehs, Margarete Brudny-Kloeppel, Antje Rottmann, Rainer Hasselmann, Marcus Schultze-Mosgau, Carsten Moeller
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Patent number: 7951790Abstract: The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.Type: GrantFiled: November 15, 2007Date of Patent: May 31, 2011Assignee: Bayer Schering Pharma AGInventors: Ulrike Fuhrmann, Anja Schmidt, Arwed Cleve, Orlin Petrov, Gunnar Garke, Stefan Pruehs, Margarete Brudny-Kloeppel, Antje Rottmann, Rainer Hasselmann, Marcus Schultze-Mosgau, Carsten Moeller
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Patent number: 7910573Abstract: The present invention relates to crystalline forms of 11?-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17?-pregna-4,9-dien-3-one. The invention relates in particular to two crystalline ansolvate/anhydrate forms of this compound, polymorphs I and II. However, the present invention also relates to crystalline solvates, for example methanol and ethanol solvates of 11?-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17?-pregna-4,9-dien-3-one as precursors for preparing these two polymorphs I and II. Processes for preparing polymorph I by displacement crystallization or by trituration are described. Selection of the last solvent before formation of the ansolvate can be based on the differences in the purification behaviour of the individual solvates of 11?-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17?-pregna-4,9-dien-3-one. Polymorph I according to the invention is particularly suitable for the manufacture of medicinal products.Type: GrantFiled: June 1, 2007Date of Patent: March 22, 2011Assignee: Bayer Schering Pharma AGInventors: Wolfgang Beckmann, Gabriele Winter, Edda Kraemer, Thomas Ginko, Evelin Amoulong, Arwed Cleve
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Patent number: 7902178Abstract: The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.Type: GrantFiled: November 15, 2007Date of Patent: March 8, 2011Assignee: Bayer Schering Pharma AGInventors: Ulrike Fuhrmann, Anja Schmidt, Arwed Cleve, Orlin Petrov, Gunnar Garke, Stefan Pruehs, Margarete Brudny-Kloeppel, Antje Rottmann, Rainer Hasselmann, Marcus Schultze-Mosgau, Carsten Moeller
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Publication number: 20100210630Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: ApplicationFiled: April 30, 2010Publication date: August 19, 2010Inventors: Damian Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, David Vogel, Guo Ping Wei, Bin Ye
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Patent number: 7737145Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: GrantFiled: December 22, 2006Date of Patent: June 15, 2010Assignee: Estrellita Pharmaceuticals, LLCInventors: Damian Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, David Vogel, Guo Ping Wei, Bin Ye
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Patent number: 7601748Abstract: This invention relates to anti-androgenic N-[?-[3-[4-cyano-3-(trifluoromethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl]alkyl]-substituted pyrrolidines of general formula I, with a strongly pronounced antiproliferative profile of action; process for the production of the compounds of general formula I, pharmaceutical preparations and the use for the production of pharmaceutical agents.Type: GrantFiled: August 9, 2006Date of Patent: October 13, 2009Assignee: Bayer Schering Pharma AGInventors: Arwed Cleve, Volker Schulze, Dieter Zopf, Jens Hoffmann, Andreas Reichel, Karsten Parczyk
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Publication number: 20080200440Abstract: The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.Type: ApplicationFiled: November 15, 2007Publication date: August 21, 2008Inventors: Ulrike Fuhrmann, Anja Schmidt, Arwed Cleve, Orlin Petrov, Gunnar Garke, Stefan Pruehs, Margarete Brudny-Kloeppel, Antje Rottmann, Rainer Hasselmann, Marcus Schultze-Mosgau, Carsten Moeller
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Publication number: 20080085875Abstract: The present invention relates to crystalline forms of 11?-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17?-pregna-4,9-dien-3-one. The invention relates in particular to two crystalline ansolvate/anhydrate forms of this compound, polymorphs I and II. However, the present invention also relates to crystalline solvates, for example methanol and ethanol solvates of 11?-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17?-pregna-4,9-dien-3-one as precursors for preparing these two polymorphs I and II. Processes for preparing polymorph I by displacement crystallization or by trituration are described. Selection of the last solvent before formation of the ansolvate can be based on the differences in the purification behaviour of the individual solvates of 11?-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17?-pregna-4,9-dien-3-one. Polymorph I according to the invention is particularly suitable for the manufacture of medicinal products.Type: ApplicationFiled: June 1, 2007Publication date: April 10, 2008Inventors: Wolfgang Beckmann, Gabriele Winter, Edda Kraemer, Thomas Ginko, Evelin Amoulong, Arwed Cleve
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Publication number: 20070155727Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4a, R4b, R4c, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, R9 and R10 are described herein, or pharmaceutically acceptable salts, solvates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and which are therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of using and preparing the compounds of the invention are also disclosed.Type: ApplicationFiled: December 22, 2006Publication date: July 5, 2007Applicant: Schering AktiengessellschaftInventors: Ming Chen, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica Kochanny, Amy Liang, David Light, John Parkinson, David Vogel, Guo Wei, Bin Ye, Hong Ye
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Publication number: 20070155726Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: ApplicationFiled: December 22, 2006Publication date: July 5, 2007Applicant: Schering AktiengesellschaftInventors: Damian Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica Kochanny, Amy Liang, David Light, John Parkinson, David Vogel, Guo Wei, Bin Ye
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Publication number: 20070060573Abstract: The present patent application relates to acyltryptophanols of the general formula I, in which Q, X, Y, W, R1, R2, R3, R4, R5, R8 have the meanings stated in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.Type: ApplicationFiled: August 9, 2006Publication date: March 15, 2007Inventors: Lars Wortmann, Arwed Cleve, Bernd Menzenbach, Hans-Peter Muhn, Gernot Langer, Anna Schrey, Ronald Kuehne, Marcu Koppitz, Dirk Kosemund
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Publication number: 20070021481Abstract: This invention relates to anti-androgenic N-[?-[3-[4-cyano-3-(trifluoromethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl]alkyl]-substituted pyrrolidines of general formula I, with a strongly pronounced antiproliferative profile of action; process for the production of the compounds of general formula I, pharmaceutical preparations and the use for the production of pharmaceutical agents.Type: ApplicationFiled: August 9, 2006Publication date: January 25, 2007Inventors: Arwed Cleve, Volker Schulze, Dieter Zopf, Jens Hoffmann, Andreas Reichel, Karsten Parczyk
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Patent number: 7148213Abstract: This invention describes the new 17?-fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with bases. The new compounds have an extraordinary strong antigestagenic action and are suitable for the production of pharmaceutical preparations.Type: GrantFiled: September 24, 2004Date of Patent: December 12, 2006Assignee: Schering AGInventors: Wolfgang Schwede, Arwed Cleve, Ulrich Klar, Gunter Neef, Kristof Chwalisz, Martin Schneider, Ulrike Fuhrmann, Holger Heb-Stumpp
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Patent number: 7138421Abstract: This invention relates to anti-androgenic N-[?-[3-[4-cyano-3-(trifluoromethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl]alkyl]-substituted pyrrolidines of general formula I, with a strongly pronounced antiproliferative profile of action; process for the production of the compounds of general formula I, pharmaceutical preparations and the use for the production of pharmaceutical agents.Type: GrantFiled: May 10, 2004Date of Patent: November 21, 2006Assignee: Schring AktiengesellschaftInventors: Arwed Cleve, Volker Schulze, Dieter Zopf, Jens Hoffmann, Andreas Reichel, Karsten Parczyk