Patents Assigned to Merck & Cie
  • Patent number: 10973936
    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: Grant
    Filed: May 1, 2019
    Date of Patent: April 13, 2021
    Assignee: MERCK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Cindy Ramona Fischer, Viola Groehn
  • Patent number: 10961246
    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: Grant
    Filed: September 21, 2017
    Date of Patent: March 30, 2021
    Assignee: MERCK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Tobias Ludwig Ross, Viola Groehn
  • Publication number: 20200283443
    Abstract: The invention is directed towards stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid and its hemisulfate salt as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.
    Type: Application
    Filed: February 20, 2020
    Publication date: September 10, 2020
    Applicant: MERCK & CIE
    Inventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
  • Patent number: 10570134
    Abstract: The invention is directed towards stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid and its hemisulfate salt as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.
    Type: Grant
    Filed: May 17, 2019
    Date of Patent: February 25, 2020
    Assignee: MERCK & CIE
    Inventors: Rudolf Moser, Viola Groehn, Thomas Egger, Thomas Ammann
  • Patent number: 10463666
    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: Grant
    Filed: December 10, 2015
    Date of Patent: November 5, 2019
    Assignees: MERCK & CIE, Bayer Intellectual Property GmbH
    Inventors: Kai Strothmann, Gavin Welch Wasserfall-Smith, Klaus Pietrzik, Kristina King, Rudolf Moser
  • Publication number: 20190270745
    Abstract: The invention is directed towards stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid and its hemisulfate salt as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.
    Type: Application
    Filed: May 17, 2019
    Publication date: September 5, 2019
    Applicant: MERCK & CIE
    Inventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
  • Publication number: 20190255200
    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: May 1, 2019
    Publication date: August 22, 2019
    Applicant: MERCK & CIE
    Inventors: Roger SCHIBLI, Rudolf MOSER, Christina Magdalena MULLER, Simon Mensah AMETAMEY, Cindy Ramona FISCHER, Viola GROEHN
  • Patent number: 10377756
    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: Grant
    Filed: July 13, 2015
    Date of Patent: August 13, 2019
    Assignee: MERCK & CIE
    Inventors: Simon Mensah Ametamey, Rudolf Moser, Tobias Ludwig Ross, Phoebe Lam, Viola Groehn
  • Patent number: 10336758
    Abstract: The invention is directed towards stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid and its hemisulfate salt as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: July 2, 2019
    Assignee: MERCK & CIE
    Inventors: Rudolf Moser, Viola Groehn, Thomas Egger, Thomas Ammann
  • Patent number: 10322195
    Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein the 18F isotope F 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: Grant
    Filed: August 21, 2012
    Date of Patent: June 18, 2019
    Assignee: Merck & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Cindy Ramona Fischer, Viola Groehn
  • Publication number: 20190106431
    Abstract: 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: Application
    Filed: December 6, 2018
    Publication date: April 11, 2019
    Applicant: MERCK & CIE
    Inventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
  • Patent number: 10059710
    Abstract: The invention is directed towards stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid and its hemisulfate salt as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: August 28, 2018
    Assignee: MERCK & CIE
    Inventors: Rudolf Moser, Viola Groehn, Thomas Egger, Thomas Ammann
  • Publication number: 20180134711
    Abstract: The invention is directed towards stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid and its hemisulfate salt as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.
    Type: Application
    Filed: January 12, 2018
    Publication date: May 17, 2018
    Applicant: MERCK & CIE
    Inventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
  • Publication number: 20180072734
    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: September 21, 2017
    Publication date: March 15, 2018
    Applicant: MERCK & CIE
    Inventors: Roger SCHIBLI, Rudolf MOSER, Cristina Magdalena MULLER, Simon Mensah AMETAMEY, Tobias Ludwig ROSS, Viola GROEHN
  • Patent number: 9771368
    Abstract: 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: Grant
    Filed: February 12, 2016
    Date of Patent: September 26, 2017
    Assignee: MERCK & CIE
    Inventors: Simon Mensah Ametamey, Rudolf Moser, Tobias Ludwig Ross, Viola Groehn
  • Publication number: 20170233394
    Abstract: The invention is directed towards stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid and its hemisulfate salt as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.
    Type: Application
    Filed: February 17, 2017
    Publication date: August 17, 2017
    Applicant: MERCK & CIE
    Inventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
  • Publication number: 20170128599
    Abstract: The present invention is directed towards novel folate-conjugates of formula I wherein F is a folate or derivative thereof, Z1, Z2, Z3 are independently of each other C or N, S1 to S4 are independently of each other a single bond or a spacer, Ra, Ra?, and Rb are donor groups and/or another group F, Rc is optionally another group F and n is 1 or 2. The invention further contemplates the corresponding metal-chelate complexes as well as pharmaceutical compositions thereof, and their uses in diagnostic imaging and radiotherapy.
    Type: Application
    Filed: November 22, 2016
    Publication date: May 11, 2017
    Applicant: MERCK & CIE
    Inventors: Rudolf MOSER, Roger SCHIBLI, Cristina Magdalena MULLER, Viola GROEHN, Urs MICHEL, Christoph SPARR, Thomas Leighton MINDT
  • Publication number: 20160185787
    Abstract: 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: Application
    Filed: August 14, 2014
    Publication date: June 30, 2016
    Applicant: MERCK & CIE
    Inventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
  • Publication number: 20160159802
    Abstract: 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: Application
    Filed: February 12, 2016
    Publication date: June 9, 2016
    Applicant: MERCK & CIE
    Inventors: Simon Mensah AMETAMEY, Rudolf MOSER, Tobais Ludwig ROSS, Viola GROEHN
  • Patent number: 9315506
    Abstract: 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: Grant
    Filed: April 11, 2008
    Date of Patent: April 19, 2016
    Assignee: MERCK & CIE
    Inventors: Simon Mensah Ametamey, Rudolf Moser, Tobias Ludwig Ross, Viola Groehn