Patents Assigned to Merck & Cie
  • Publication number: 20160095860
    Abstract: 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: Application
    Filed: December 10, 2015
    Publication date: April 7, 2016
    Applicants: MERCK & CIE, Bayer Intellectual Property GmbH
    Inventors: Kai STROTHMANN, Gavin Welch SMITH, Klaus PIETRZIK, Kristina KING, Rudolf MOSER
  • Patent number: 9295739
    Abstract: 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: Grant
    Filed: August 10, 2012
    Date of Patent: March 29, 2016
    Assignee: MERCK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Harriet Struthers, Viola Groehn, Simon Mensah Ametamey, Cindy Ramona Fischer
  • Patent number: 9265746
    Abstract: 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: Grant
    Filed: May 31, 2006
    Date of Patent: February 23, 2016
    Assignee: MERCK & CIE
    Inventors: Rudolf Moser, Viola Groehn, Roger Schibli, Cristina Magdalena Mueller
  • Publication number: 20160030573
    Abstract: 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: Application
    Filed: October 15, 2015
    Publication date: February 4, 2016
    Applicant: MERCK & CIE
    Inventors: Rudolf MOSER, Thomas AMMANN
  • Patent number: 9180128
    Abstract: 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: Grant
    Filed: June 28, 2004
    Date of Patent: November 10, 2015
    Assignee: MERCK & CIE
    Inventors: Rudolf Moser, Thomas Ammann
  • Publication number: 20150315189
    Abstract: 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: Application
    Filed: July 13, 2015
    Publication date: November 5, 2015
    Applicant: MERCK & CIE
    Inventors: Simon Mensah AMETAMEY, Rudolf MOSER, Tobias Ludwig ROSS, Phoebe LAM, Viola GROEHN
  • Publication number: 20150125390
    Abstract: 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: Application
    Filed: May 8, 2013
    Publication date: May 7, 2015
    Applicant: MERCK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Mueller, Simon Mensah Ametamey, Thomas Betzel, Viola Groehn
  • Publication number: 20140234216
    Abstract: 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: Application
    Filed: August 10, 2012
    Publication date: August 21, 2014
    Applicant: MERCK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Harriet Struthers, Viola Groehn, Simon Mensah Ametamey, Cindy Ramona Fischer
  • Publication number: 20140193337
    Abstract: 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: Application
    Filed: August 21, 2012
    Publication date: July 10, 2014
    Applicant: MERCK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Cindy Ramona Fischer, Viola Groehn
  • Patent number: 8318745
    Abstract: 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: Grant
    Filed: December 3, 2009
    Date of Patent: November 27, 2012
    Assignee: Merck & CIE
    Inventors: Rudolf Moser, Viola Groehn, Thomas Egger, Fritz Blatter
  • Publication number: 20110286921
    Abstract: 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: Application
    Filed: October 12, 2009
    Publication date: November 24, 2011
    Applicant: MERCK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Tobias Ludwig Ross, Viola Groehn
  • Patent number: 7816525
    Abstract: 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: Grant
    Filed: July 12, 2000
    Date of Patent: October 19, 2010
    Assignee: Merck & Cie
    Inventors: Hans Rudolf Muller, Rudolf Moser, Viola Groehn, Benoit Pugin