Patents Assigned to Merck & Cie
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Publication number: 20220143027Abstract: 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: ApplicationFiled: January 25, 2022Publication date: May 12, 2022Applicant: MERCK & CIEInventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
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Patent number: 11306094Abstract: 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: GrantFiled: February 20, 2020Date of Patent: April 19, 2022Assignee: MERCK & CIEInventors: Rudolf Moser, Viola Groehn, Thomas Egger, Thomas Ammann
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Publication number: 20220024940Abstract: 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: October 8, 2021Publication date: January 27, 2022Applicant: MERCK & CIEInventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
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Patent number: 10973936Abstract: 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: GrantFiled: May 1, 2019Date of Patent: April 13, 2021Assignee: MERCK & CIEInventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Cindy Ramona Fischer, Viola Groehn
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Patent number: 10961246Abstract: 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: GrantFiled: September 21, 2017Date of Patent: March 30, 2021Assignee: MERCK & CIEInventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Tobias Ludwig Ross, Viola Groehn
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Publication number: 20200283443Abstract: 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: ApplicationFiled: February 20, 2020Publication date: September 10, 2020Applicant: MERCK & CIEInventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
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Patent number: 10570134Abstract: 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: GrantFiled: May 17, 2019Date of Patent: February 25, 2020Assignee: MERCK & CIEInventors: Rudolf Moser, Viola Groehn, Thomas Egger, Thomas Ammann
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Patent number: 10463666Abstract: 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: GrantFiled: December 10, 2015Date of Patent: November 5, 2019Assignees: MERCK & CIE, Bayer Intellectual Property GmbHInventors: Kai Strothmann, Gavin Welch Wasserfall-Smith, Klaus Pietrzik, Kristina King, Rudolf Moser
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Publication number: 20190270745Abstract: 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: ApplicationFiled: May 17, 2019Publication date: September 5, 2019Applicant: MERCK & CIEInventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
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Publication number: 20190255200Abstract: 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: May 1, 2019Publication date: August 22, 2019Applicant: MERCK & CIEInventors: Roger SCHIBLI, Rudolf MOSER, Christina Magdalena MULLER, Simon Mensah AMETAMEY, Cindy Ramona FISCHER, Viola GROEHN
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Patent number: 10377756Abstract: 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: GrantFiled: July 13, 2015Date of Patent: August 13, 2019Assignee: MERCK & CIEInventors: Simon Mensah Ametamey, Rudolf Moser, Tobias Ludwig Ross, Phoebe Lam, Viola Groehn
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Patent number: 10336758Abstract: 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: GrantFiled: January 12, 2018Date of Patent: July 2, 2019Assignee: MERCK & CIEInventors: Rudolf Moser, Viola Groehn, Thomas Egger, Thomas Ammann
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Patent number: 10322195Abstract: 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: GrantFiled: August 21, 2012Date of Patent: June 18, 2019Assignee: Merck & CIEInventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Cindy Ramona Fischer, Viola Groehn
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Publication number: 20190106431Abstract: 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: December 6, 2018Publication date: April 11, 2019Applicant: MERCK & CIEInventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
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Patent number: 10059710Abstract: 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: GrantFiled: February 17, 2017Date of Patent: August 28, 2018Assignee: MERCK & CIEInventors: Rudolf Moser, Viola Groehn, Thomas Egger, Thomas Ammann
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Publication number: 20180134711Abstract: 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: ApplicationFiled: January 12, 2018Publication date: May 17, 2018Applicant: MERCK & CIEInventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
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Publication number: 20180072734Abstract: 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: September 21, 2017Publication date: March 15, 2018Applicant: MERCK & CIEInventors: Roger SCHIBLI, Rudolf MOSER, Cristina Magdalena MULLER, Simon Mensah AMETAMEY, Tobias Ludwig ROSS, Viola GROEHN
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Patent number: 9771368Abstract: 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: February 12, 2016Date of Patent: September 26, 2017Assignee: MERCK & CIEInventors: Simon Mensah Ametamey, Rudolf Moser, Tobias Ludwig Ross, Viola Groehn
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Publication number: 20170233394Abstract: 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: ApplicationFiled: February 17, 2017Publication date: August 17, 2017Applicant: MERCK & CIEInventors: Rudolf MOSER, Viola GROEHN, Thomas EGGER, Thomas AMMANN
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Publication number: 20170128599Abstract: 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: ApplicationFiled: November 22, 2016Publication date: May 11, 2017Applicant: MERCK & CIEInventors: Rudolf MOSER, Roger SCHIBLI, Cristina Magdalena MULLER, Viola GROEHN, Urs MICHEL, Christoph SPARR, Thomas Leighton MINDT