Patents Assigned to Merck & Cie
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Publication number: 20160185787Abstract: The present invention is directed towards the hemisulfate salt of 5,10-methylene-(6R)-tetrahydrofolic acid, preferably in substantially crystalline form, as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.Type: ApplicationFiled: August 14, 2014Publication date: June 30, 2016Applicant: MERCK & CIEInventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
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Publication number: 20160159802Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein the fluorine-18 is covalently linked to the aminobenzoyl moiety, which connects the condensed pyrimidine heterocycle to the amino acid portion within folate structures, as well as their precursors and their non-radioactive references, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.Type: ApplicationFiled: February 12, 2016Publication date: June 9, 2016Applicant: MERCK & CIEInventors: Simon Mensah AMETAMEY, Rudolf MOSER, Tobais Ludwig ROSS, Viola GROEHN
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Patent number: 9315506Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein the fluorine-18 is covalently linked to the aminobenzoyl moiety, which connects the condensed pyrimidine heterocycle to the amino acid portion within folate structures, as well as their precursors and their non-radioactive references, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.Type: GrantFiled: April 11, 2008Date of Patent: April 19, 2016Assignee: MERCK & CIEInventors: Simon Mensah Ametamey, Rudolf Moser, Tobias Ludwig Ross, Viola Groehn
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Publication number: 20160095860Abstract: The present invention relates to a pharmaceutical composition which comprises progestogens, preferably drospirenone, estrogens, preferably ethinylestradiol and 5-methyl-(6S)-tetrahydrofolate, can be employed as oral contraceptive and moreover prevents disorders caused by folate deficiency in the consumers, in particular cardiovascular disorders and, after conception of the embryo, congenital malformations caused by folate deficiency such as, for example, neural tube defects, ventricular valve defects, urogenital defects, and cleft lip, jaw and palate, without masking the symptoms of vitamin B12 deficiency, and at the same time even in the case of homozygous or heterozygous polymorphism of methylenetetrahydrofolate reductase facilitates unimpaired utilizability of the folate component 5-methyl-(6S)-tetrahydrofolate by the body and thus its biological activity for preventing the abovementioned congenital malformations caused by folate deficiency.Type: ApplicationFiled: December 10, 2015Publication date: April 7, 2016Applicants: MERCK & CIE, Bayer Intellectual Property GmbHInventors: Kai STROTHMANN, Gavin Welch SMITH, Klaus PIETRZIK, Kristina KING, Rudolf MOSER
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Patent number: 9295739Abstract: The present invention is directed towards new trifunctional folate-conjugates comprising a folate, an albumin binder and a radionuclide-based therapeutic or diagnostic moiety as well as pharmaceutical compositions thereof, their method of production and their use in diagnostic and therapeutic medical applications, such as diagnostic nuclear imaging and radionuclide therapy.Type: GrantFiled: August 10, 2012Date of Patent: March 29, 2016Assignee: MERCK & CIEInventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Harriet Struthers, Viola Groehn, Simon Mensah Ametamey, Cindy Ramona Fischer
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Patent number: 9265746Abstract: Method for selective targeting of one or more effector moiety such as diagnostic or a therapeutic agent to a cell or population of cells expressing a folate-receptor comprising simultaneous or sequential administration of an antifolate with a folate- or pteroate-conjugate comprising said one or more effector moiety.Type: GrantFiled: May 31, 2006Date of Patent: February 23, 2016Assignee: MERCK & CIEInventors: Rudolf Moser, Viola Groehn, Roger Schibli, Cristina Magdalena Mueller
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Publication number: 20160030573Abstract: This invention relates to stable pharmaceutical compositions of 5,10-methylene-(6R)-, -(6S)-, or -(6R,S)-tetrahydrofolate (MTHF), by adjusting a basic pH and the simultaneous use of citrate. Stabilisation is effected even in the absence of a reducing agent. The present invention is particularly suitable for producing lyophlisation solutions and lyophilisates or dry powders and dry mixtures, since the stable MTHF solutions can be used in high concentrations for filling corresponding vessels such as vials, ampoules, etc. The lyophilisates have a surprisingly long shelf life and are surprisingly stable. They can be reconstituted without problems by adding wateror aqueous solutions, and the final clear injection solutions again exhibit excellent stability properties. Moreover, the present invention even makes it possible to prepare difficulty soluble calcium 15 or acidic salts of MTHF in high concentrations and as physiologically compatible isotonic solutions.Type: ApplicationFiled: October 15, 2015Publication date: February 4, 2016Applicant: MERCK & CIEInventors: Rudolf MOSER, Thomas AMMANN
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Patent number: 9180128Abstract: This invention relates to stable pharmaceutical compositions of 5,10-methylene-(6R)-, -(65)- or -(6R,S)-tetrahydrofolate (MTHF), by adjusting to a basic pH and the simultaneous use of citrate. Stabilisation is effected even in the absence of a reducing agent. The present invention is particularly suitable for producing lyophilisation solutions and lyophilisates or dry powders and dry mixtures, since the stable MTHF solutions can be used in high concentrations for filling corresponding vessels such as vials, ampoules, etc. The lyophilisates have a surprisingly long shelf life and are surprisingly stable. They can be reconstituted without problems by adding water or aqueous solutions, and the final clear injection solutions again exhibit excellent stability properties. Moreover, the present invention even makes it possible to prepare difficultly soluble calcium 15 or acidic salts of MTHF in high concentrations and as physiologically compatible isotonic solutions.Type: GrantFiled: June 28, 2004Date of Patent: November 10, 2015Assignee: MERCK & CIEInventors: Rudolf Moser, Thomas Ammann
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Publication number: 20150315189Abstract: The present invention is directed towards a new method of synthesis of 18F-folate radiopharmaceuticals, wherein fluorine-18 is attached to a pteroate (or folate) or derivative thereof, through direct radiolabeling with 18[F]fluoride, as well as 18F-folate radiopharmaceuticals obtained by such method of synthesis and their use in diagnosis and monitoring of cancer therapy and therapy of inflammatory and autoimmune diseases.Type: ApplicationFiled: July 13, 2015Publication date: November 5, 2015Applicant: MERCK & CIEInventors: Simon Mensah AMETAMEY, Rudolf MOSER, Tobias Ludwig ROSS, Phoebe LAM, Viola GROEHN
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Publication number: 20150125390Abstract: The present invention is directed towards new 18F-folate/antifolate analogue radiopharmaceuticals, wherein the phenyl group within folate structures has been replaced by an 18F-heterocycle, their precursors, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.Type: ApplicationFiled: May 8, 2013Publication date: May 7, 2015Applicant: MERCK & CIEInventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Mueller, Simon Mensah Ametamey, Thomas Betzel, Viola Groehn
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Publication number: 20140234216Abstract: The present invention is directed towards new trifunctional folate-conjugates comprising a folate, an albumin binder and a radionuclide-based therapeutic or diagnostic moiety as well as pharmaceutical compositions thereof, their method of production and their use in diagnostic and therapeutic medical applications, such as diagnostic nuclear imaging and radionuclide therapy.Type: ApplicationFiled: August 10, 2012Publication date: August 21, 2014Applicant: MERCK & CIEInventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Harriet Struthers, Viola Groehn, Simon Mensah Ametamey, Cindy Ramona Fischer
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Publication number: 20140193337Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein the 18F isotope is linked via a prosthetic group, more specifically via a prosthetic group having a saccharide group, such as a cyclic mono- or oligosaccharide, preferably based on a pyranoside or furanoside, which is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.Type: ApplicationFiled: August 21, 2012Publication date: July 10, 2014Applicant: MERCK & CIEInventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Cindy Ramona Fischer, Viola Groehn
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Patent number: 8318745Abstract: Crystal forms of (6R)-L-erythro-tetrahydrobiopterin dihydrochloride, hydrates and solvates and processes for their preparation are provided. These crystal forms are either intermediates for the preparation of stable polymorphic form B or are suitable for solid formulations.Type: GrantFiled: December 3, 2009Date of Patent: November 27, 2012Assignee: Merck & CIEInventors: Rudolf Moser, Viola Groehn, Thomas Egger, Fritz Blatter
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Publication number: 20110286921Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein fluorine-18 is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of therapy of cancer and inflammatory and autoimmune diseases.Type: ApplicationFiled: October 12, 2009Publication date: November 24, 2011Applicant: MERCK & CIEInventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Tobias Ludwig Ross, Viola Groehn
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Patent number: 7816525Abstract: Process for the preparation of tetrahydropterin and tetrahydropterin derivatives by hydrogenating pterin and pterin derivatives with hydrogen in the presence of a hydrogenating catalyst, in which the hydrogenation is carried out in a polar reaction medium and metal complexes that are soluble in the reaction medium are employed as the hydrogenation catalysts. The process is suited to the hydrogenation, particularly asymmetric hydrogenation, of folic acid, folic acid salts, folic acid esters, folic acid ester salts or dihydroforms thereof, with the proviso that in the event of using folic acid, carboxylic acid salts thereof or dihydroforms thereof the reaction medium is aqueous, and in the event of using folic acid esters, folic acid ester salts or dihydroforms thereof the reaction medium is an alcohol. The process opens up straightforward access to achiral and chiral pterin derivatives.Type: GrantFiled: July 12, 2000Date of Patent: October 19, 2010Assignee: Merck & CieInventors: Hans Rudolf Muller, Rudolf Moser, Viola Groehn, Benoit Pugin