Patents by Inventor Gerhard Breipohl
Gerhard Breipohl 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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Patent number: 8268560Abstract: The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.Type: GrantFiled: January 24, 2011Date of Patent: September 18, 2012Assignee: Sanofi-Aventis Deutschland GmbHInventors: Eugen Uhlmann, Gerhard Breipohl, David W. Will
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Publication number: 20110117569Abstract: The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.Type: ApplicationFiled: January 24, 2011Publication date: May 19, 2011Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Eugen UHLMANN, Gerhard BREIPOHL, David W. WILL
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Patent number: 7897346Abstract: The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.Type: GrantFiled: May 29, 2009Date of Patent: March 1, 2011Assignee: Sanofi-Aventis Deutschland GmbHInventors: Eugen Uhlmann, Gerhard Breipohl, David William Will
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Publication number: 20100022016Abstract: The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.Type: ApplicationFiled: May 29, 2009Publication date: January 28, 2010Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Eugen UHLMANN, Gerhard Breipohl, David W. Will
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Patent number: 7550582Abstract: The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.Type: GrantFiled: September 14, 2007Date of Patent: June 23, 2009Assignee: sanofi-aventis Deutschland GmbHInventors: Eugen Uhlmann, Gerhard Breipohl, David William Will
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Patent number: 7485421Abstract: Polyamide-oligonucleotide derivatives of the formula F[(DNA-Li)q(PNA-Li)r(DNA-Li)s(PNA)t]xF? wherein q, r, s, t are, independently of one another, zero or 1, where the total of two or more adjacent q, r, s and t?2; x is 1 to 20; DNA is a nucleic acid such as DNA or RNA or a known derivative thereof; Li is a covalent linkage between DNA and PNA, where the covalent linkage comprises a bond or an organic radical with at least one atom from the series consisting of C, N, O or S; PNA is a polyamide structure which contains at least one nucleotide base which is different from thymine; and F and F? are end groups and/or are linked together by a covalent bond, and the physiologically tolerated salts thereof, a process for their preparation and their use as pharmaceutical, as gene probe and as primer, are described.Type: GrantFiled: September 10, 2004Date of Patent: February 3, 2009Assignee: Hoechst GmbHInventors: Eugen Uhlmann, Gerhard Breipohl
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Publication number: 20080070258Abstract: The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.Type: ApplicationFiled: September 14, 2007Publication date: March 20, 2008Applicant: AVENTIS PHARMA DEUTSCHLAND GMBHInventors: Eugen UHLMANN, Gerhard Breipohl, David Will
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Patent number: 7241882Abstract: The present invention relates to PNA derivatives which carry, at the N terminus of the PNA backbone, a phosphoryl radical. The phosphoryl radical can be, for example, a phosphate radical, or a substituted phosphoryl radical, with substituted phosphoryl derivatives carrying, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the abovementioned PNA derivatives and to their use as pharmaceuticals and diagnostic agents.Type: GrantFiled: June 9, 2004Date of Patent: July 10, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Eugen Uhlmann, Gerhard Breipohl, David William Will
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Patent number: 7084250Abstract: The present invention relates to a process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides of the formula I, in which the anions X are physiologically acceptable anions, and their analogs, which are effective inhibitors of the blood coagulation factor Xa and which can be used, for example, for preventing thromboses. The process according to the invention comprises the coupling of 2-[2-acetylamino-3-(4-amidinophenyl)propionylamino]-2-cyclohexylacetic acid, which is obtained from 2-[2-acetylamino-3-(4-cyanophenyl)acryloylamino]-2-cyclohexylacetic acid by asymmetric hydrogenation and conversion of the cyano group into the amidine, or a salt thereof, with a 3-(2-amino-2-carbamoylethyl)-1-methylpyridinium salt or a salt thereof. The invention furthermore provides starting materials and intermediates for this process, processes for their preparation and acetyl-(S)-4-amidiniophenylalanyl-(S)-cyclohexylglycyl-(S)-(1-methyl-3-pyridinio)alaninamide as ditosylate salt.Type: GrantFiled: June 17, 2004Date of Patent: August 1, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Gerhard Breipohl, Wolfgang Holla, Heiner Jendralla, Gerhard Beck
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Patent number: 6919441Abstract: The invention provides polyamide-oligonucleotide derivatives of the formula: F[(DNA-Li)q(PNA-Li)r(DNA-Li)s(PNA)t]xF?. In the formula, q, r, s, and t are, independently of one another, zero or 1, where the total of two or more adjacent q, r, s, and t is greater than or equal to 2; and x is 1 to 20. In the formula, DNA is a nucleic acid such as DNA or RNA or a known derivative thereof. Li is a covalent linkage between DNA and PNA, where the covalent linkage comprises a bond or an organic radical with at least one atom from the series consisting of C, N, O, or S. PNA is a polyamide structure which contains at least one nucleotide base that is different from thymine. F and F? are end groups and/or are linked together by a covalent bond. The invention also provides physiologically tolerated salts of the above formula. The invention further provides a process for preparation of the polyamide-oligonucleotide derivatives of the invention as well as their use as pharmaceuticals, as gene probes, and as primers.Type: GrantFiled: February 27, 2001Date of Patent: July 19, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Eugen Uhlmann, Gerhard Breipohl
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Patent number: 6905820Abstract: The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.Type: GrantFiled: April 17, 2001Date of Patent: June 14, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Eugen Uhlmann, Gerhard Breipohl, David William Will
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Patent number: 6900318Abstract: The present invention relates to ethyl (2S)-2-(naphthalene-1-sulfonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionate hemifumarate of formula (I), and to a process for its preparation comprising reacting 4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoic acid or a derivative thereof and ethyl (2S)-3-amino-2-(naphthalene-1-sulfonylamino)propionate. The compound of formula (I) is a valuable pharmaceutical which can be used, for example, in the treatment or prophylaxis of diseases which can be influenced by inhibiting the vitronectin receptor, in particular of bone diseases such as osteoporosis. The invention furthermore relates to chemical intermediates useful for the preparation of the compound of formula (I).Type: GrantFiled: July 8, 2000Date of Patent: May 31, 2005Assignee: Aventis Pharma Deutscland GmbHInventors: Gerhard Breipohl, Anuschirwam Peyman, Theodor Wollmann
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Publication number: 20050026817Abstract: Polyamide-oligonucleotide derivatives of the formula F[(DNA-Li)q(PNA-Li)r(DNA-Li)s(PNA)t]xF? wherein q, r, s, t are, independently of one another, zero or 1, where the total of two or more adjacent q, r, s and t?2; x is 1 to 20; DNA is a nucleic acid such as DNA or RNA or a known derivative thereof; Li is a covalent linkage between DNA and PNA, where the covalent linkage comprises a bond or an organic radical with at least one atom from the series consisting of C, N, O or S; PNA is a polyamide structure which contains at least one nucleotide base which is different from thymine; and F and F? are end groups and/or are linked together by a covalent bond, and the physiologically tolerated salts thereof, a process for their preparation and their use as pharmaceutical, as gene probe and as primer, are described.Type: ApplicationFiled: September 10, 2004Publication date: February 3, 2005Applicant: Aventis Pharma Deutschland GmbHInventors: Eugen Uhlmann, Gerhard Breipohl
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Publication number: 20050009073Abstract: The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.Type: ApplicationFiled: June 2, 2004Publication date: January 13, 2005Applicant: Aventis Pharma Deutschland GmbHInventors: Eugen Uhlmann, Gerhard Breipohl, David Will
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Publication number: 20040265885Abstract: The present invention relates to PNA derivatives which carry, at the N terminus of the PNA backbone, a phosphoryl radical. The phosphoryl radical can be, for example, a phosphate radical, or a substituted phosphoryl radical, with substituted phosphoryl derivatives carrying, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the abovementioned PNA derivatives and to their use as pharmaceuticals and diagnostic agents.Type: ApplicationFiled: June 9, 2004Publication date: December 30, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: Eugen Uhlmann, Gerhard Breipohl, David William Will
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Publication number: 20040225109Abstract: The present invention relates to a process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides of the formula I, 1Type: ApplicationFiled: June 17, 2004Publication date: November 11, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: Gerhard Breipohl, Wolfgang Holla, Heiner Jendralla, Gerhard Beck
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Patent number: 6777544Abstract: The present invention relates to PNA derivatives which carry, at the N terminus of the PNA backbone, a phosphoryl radical. The phosphoryl radical can be, for example, a phosphate radical, or a substituted phosphoryl radical, with substituted phosphoryl derivatives carrying, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the abovementioned PNA derivatives and to their use as pharmaceuticals and diagnostic agents.Type: GrantFiled: April 17, 2001Date of Patent: August 17, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Eugen Uhlmann, Gerhard Breipohl, David William Will
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Patent number: 6723727Abstract: The present invention relates to compounds of the formulae I and Ia in which X, Y, W, Wa, G and Ga have the meanings given in the patent claims, and their physiologically tolerable salts and their prodrugs, their preparation, their use, in particular as pharmaceutical active compounds, and pharmaceutical preparations comprising them. The compounds of the formula I are vitronectin receptor antagonists and can be employed, for example, as inhibitors of bone resorption and for the treatment of osteoporosis.Type: GrantFiled: June 15, 2000Date of Patent: April 20, 2004Assignees: Hoechst Aktiengesellschaft, GenentechInventors: Anuschirwan Peyman, Jochen Knolle, Volkmar Wehner, Gerhard Breipohl, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek
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Publication number: 20030203359Abstract: Polyamide-oligonucleotide derivatives of the formulaType: ApplicationFiled: February 27, 2001Publication date: October 30, 2003Applicant: Hoechst Marion Roussel Deutschland GmbHInventors: Eugen Uhlmann, Gerhard Breipohl
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Publication number: 20030022172Abstract: The present invention relates to PNA derivatives which carry, at the N terminus of the PNA backbone, a phosphoryl radical. The phosphoryl radical can be, for example, a phosphate radical, or a substituted phosphoryl radical, with substituted phosphoryl derivatives carrying, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the abovementioned PNA derivatives and to their use as pharmaceuticals and diagnostic agents.Type: ApplicationFiled: April 17, 2001Publication date: January 30, 2003Inventors: Eugen Uhlmann, Gerhard Breipohl, David William Will