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公开(公告)号：US20220024940A1
公开(公告)日：2022-01-27
申请号：US17496939
申请日：2021-10-08
Applicant: MERCK & CIE
Inventor： Rudolf MOSER , Viola GROEHN , Thomas EGGER , Thomas AMMANN
IPC: C07D487/14 , C07D475/04
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.
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公开(公告)号：US20200283443A1
公开(公告)日：2020-09-10
申请号：US16796164
申请日：2020-02-20
Applicant: MERCK & CIE
Inventor： Rudolf MOSER , Viola GROEHN , Thomas EGGER , Thomas AMMANN
IPC: C07D475/12 , A61K31/519 , A61K9/08 , A61K9/19 , A61K9/00 , C07D475/04
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.
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公开(公告)号：US20150315189A1
公开(公告)日：2015-11-05
申请号：US14797640
申请日：2015-07-13
Applicant: MERCK & CIE
Inventor： Simon Mensah AMETAMEY , Rudolf MOSER , Tobias Ludwig ROSS , Phoebe LAM , Viola GROEHN
IPC: C07D475/04 , C07B59/00
CPC classification number: C07D475/04 , A61K51/0459 , A61K51/0497 , C07B59/002
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.
Abstract translation: 本发明涉及一种合成18 F-叶酸放射性药物的新方法，其中氟-18通过与氟化氟[18 F]直接放射性标记以及18F-叶酸连接在叶酸（或叶酸）或其衍生物上 通过这种合成方法获得的放射性药物及其在诊断和监测癌症治疗和治疗炎性和自身免疫疾病中的用途。
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公开(公告)号：US20220143027A1
公开(公告)日：2022-05-12
申请号：US17583994
申请日：2022-01-25
Applicant: MERCK & CIE
Inventor： Rudolf MOSER , Viola GROEHN , Thomas EGGER , Thomas AMMANN
IPC: A61K31/519 , A61K9/00 , A61K9/19 , A61K31/282 , A61K31/4745 , A61K39/395
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.
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公开(公告)号：US20180134711A1
公开(公告)日：2018-05-17
申请号：US15869499
申请日：2018-01-12
Applicant: MERCK & CIE
Inventor： Rudolf MOSER , Viola GROEHN , Thomas EGGER , Thomas AMMANN
IPC: C07D475/12 , A61K31/519 , A61K9/19 , A61K9/08
CPC classification number: C07D475/12 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K31/519 , C07B2200/13 , C07D475/04 , A61K2300/00
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.
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Patent Agency Ranking
公开(公告)号：US20170233394A1
公开(公告)日：2017-08-17
申请号：US15435787
申请日：2017-02-17
Applicant: MERCK & CIE
Inventor： Rudolf MOSER , Viola GROEHN , Thomas EGGER , Thomas AMMANN
IPC: C07D475/12 , A61K9/08 , A61K31/519 , A61K9/19
CPC classification number: C07D475/12 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K31/519 , C07B2200/13 , C07D475/04 , A61K2300/00
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.
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公开(公告)号：US20240400574A1
公开(公告)日：2024-12-05
申请号：US18799606
申请日：2024-08-09
Applicant: MERCK & CIE
Inventor： Rudolf MOSER , Viola GROEHN , Thomas EGGER , Thomas AMMANN
IPC: C07D487/14 , C07D475/04
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.
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公开(公告)号：US20180072734A1
公开(公告)日：2018-03-15
申请号：US15711316
申请日：2017-09-21
Applicant: MERCK & CIE
Inventor： Roger SCHIBLI , Rudolf MOSER , Cristina Magdalena MULLER , Simon Mensah AMETAMEY , Tobias Ludwig ROSS , Viola GROEHN
IPC: C07D475/04
CPC classification number: C07D475/04
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.
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9.发明申请公开(公告)号：US20170128599A1
公开(公告)日：2017-05-11
申请号：US15358787
申请日：2016-11-22
Applicant: MERCK & CIE
Inventor： Rudolf MOSER , Roger SCHIBLI , Cristina Magdalena MULLER , Viola GROEHN , Urs MICHEL , Christoph SPARR , Thomas Leighton MINDT
CPC classification number: A61K51/0459 , A61K51/0402 , A61K51/0497 , C07B59/002 , C07B2200/05 , C07D475/04 , C07F13/00 , G01N23/2204 , G01N33/5005 , G01N33/82 , G01N2333/705
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.
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10.发明申请公开(公告)号：US20160185787A1
公开(公告)日：2016-06-30
申请号：US14912328
申请日：2014-08-14
Applicant: MERCK & CIE
Inventor： Rudolf MOSER , Viola GROEHN , Thomas EGGER , Thomas AMMANN
IPC: C07D487/14
CPC classification number: C07D487/14 , C07D475/04
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.
Abstract translation: 本发明涉及5,10-亚甲基 - （6R） - 四氢叶酸的半硫酸盐，优选基本上为结晶形式，以及其药物组合物及其在治疗，优选化学疗法中的用途。
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