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公开(公告)号：WO2022223664A1
公开(公告)日：2022-10-27
申请号：PCT/EP2022/060494
申请日：2022-04-21
Applicant: CHARITÉ - UNIVERSITÄTSMEDIZIN BERLIN , MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN IN DER HELMHOLTZ-GEMEINSCHAFT , FORSCHUNGSVERBUND BERLIN E.V.
Inventor： STEIN, Ulrike , KOBELT, Dennis , WALTHER, Wolfgang , NAZARÉ, Marc , SPECKER, Edgar , YAN, Shixian
IPC: A61K31/5025 , A61P35/00 , A61P35/04
Abstract: The invention relates to MACC1 inhibitors for use as a medicament in the treatment of cancer. The general formula 1 provided by the invention shows beneficial effects in inhibiting the formation of metastasis, cell proliferation and cancer progression. The invention further relates to the MACC1 inhibitors of the invention for the treatment of a subject with elevated MACC1 levels and wherein said treatment inhibits MACC1 expression in said subject. The invention further relates to the MACC1 inhibitors of the invention in the treatment of subjects with a solid cancer at early stages of cancer progression such as stage I or II for colorectal or pancreatic cancer or metastatic cancer, and/or for the prevention of developing metastases.
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公开(公告)号：WO2022043465A1
公开(公告)日：2022-03-03
申请号：PCT/EP2021/073663
申请日：2021-08-26
Applicant: MAX DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN IN DER HELMHOLTZ-GEMEINSCHAFT , CHARITÉ - UNIVERSITÄTSMEDIZIN BERLIN , FORSCHUNGSVERBUND BERLIN E.V.
Inventor： KETTENMANN, Helmut , WOLF, Susanne , JORDAN, Philipp , KLEISSLE, Sabrina , NEUENSCHWANDER, Martin , SPECKER, Edgar , NAZARE, Marc
Abstract: The invention relates to compounds useful as inhibitors of NO production, especially inhibitors of the inducible NO synthase iNOS expressed by microglia and macrophages. The invention also relates to pharmaceutical compositions comprising these compounds and to therapeutic uses of these compounds, especially in the prophylaxis or treatment of conditions characterized by excess NO production, such as ischemic stroke and retinopathies.
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公开(公告)号：WO2017186793A1
公开(公告)日：2017-11-02
申请号：PCT/EP2017/059930
申请日：2017-04-26
Applicant: FORSCHUNGSVERBUND BERLIN E.V.
Inventor： KRAUSE, Gerd , HOYER, Inna , SPECKER, Edgar , FURKERT, Jens , MARCINKOWSKI, Patrick , VON KRIES, Jens-Peter , NEUENSCHWANDER, Martin , NAZARE, Marc
IPC: A61K31/429 , A61K31/495 , A61P5/14 , A61P35/00
Abstract: The invention relates to chemical compounds that are useful in the treatment of a subject afflicted by a thyroid disease, in particular to compounds that exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists and their use in the treatment of hyperthyroidism, Graves' disease, Graves' Ophthalmopathy and thyroid cancer.
Abstract translation: 本发明涉及用于治疗患有甲状腺疾病的受试者的化合物，特别是涉及表现出作为促甲状腺激素受体（TSHR）拮抗剂的活性的化合物及其在 甲状腺功能亢进症，格雷夫斯病，格雷夫斯眼病和甲状腺癌的治疗。
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4.发明申请XANTHINE DERIVATIVES, THEIR USE AS A MEDICAMENT, AND PHARMACEUTICAL PREPARATIONS COMPRISING THE SAME 审中-公开黄嘌呤衍生物，它们作为药物的用途以及包含它们的药物制剂
公开(公告)号：WO2018019917A1
公开(公告)日：2018-02-01
申请号：PCT/EP2017/068950
申请日：2017-07-27
Inventor： BADER, Michael , SPECKER, Edgar , MATTHES, Susann , SCHÜTZ, Anja , MALLOW, Keven , GROHMANN, Maik , NAZARÉ, Marc
IPC: C07D519/00
Abstract: The invention relates to a xanthine derivative defined by chemical formula I or a salt thereof, its use as a medicament, especially for use in the treatment of serotonin-related diseases or disorders, and a pharmaceutical preparation comprising the xanthine derivative. The novel xanthine compounds are capable of inhibiting tryptophan hydroxylases (TPH) involved in the biosynthesis of serotonin and are effective in influencing the serotonin level in the body.
Abstract translation: 本发明涉及由化学式I定义的黄嘌呤衍生物或其盐，其作为药物的用途，特别是用于治疗血清素相关疾病或病症的用途，以及药物制剂，其包含 黄嘌呤衍生物。 新的黄嘌呤化合物能够抑制参与5-羟色胺生物合成的色氨酸羟化酶（TPH），并能有效地影响体内5-羟色胺水平。
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5.发明申请XANTHINE DERIVATIVES, THEIR USE AS A MEDICAMENT, AND PHARMACEUTICAL PREPARATIONS COMPRISING THE SAME 审中-公开XANTHINE衍生物，它们作为药物使用，以及包含其的药物制剂
公开(公告)号：WO2016135199A1
公开(公告)日：2016-09-01
申请号：PCT/EP2016/053872
申请日：2016-02-24
Inventor： BADER, Michael , SPECKER, Edgar , MATTHES, Susann , SCHÜTZ, Anja , MALLOW, Keven , GROHMANN, Maik , NAZARÉ, Marc
IPC: C07D487/04 , C07D519/00 , A61K31/522 , A61P3/04 , A61P11/06 , A61P19/10 , A61P25/18 , A61P25/24 , A61P29/00 , A61P35/00
CPC classification number: C07D473/06 , C07D487/04 , C07D519/00
Abstract: The invention relates to a xanthine derivative defined by chemical formula I or a salt thereof, its use as a medicament, especially for use in the treatment of serotonin-related diseases or disorders, and a pharmaceutical preparation comprising the xanthine derivative. The novel xanthine compounds are capable of inhibiting tryptophan hydroxylases (TPH) involved in the biosynthesis of serotonin and are effective in influencing the serotonin level in the body.
Abstract translation: 本发明涉及由化学式I或其盐定义的黄嘌呤衍生物，其用作药物，特别是用于治疗5-羟色胺相关疾病或病症的用途，以及包含黄嘌呤衍生物的药物制剂。 新颖的黄嘌呤化合物能够抑制参与血清素生物合成的色氨酸羟化酶（TPH），有效影响体内血清素水平。
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Patent Agency Ranking6.发明授权
公开(公告)号：EP3262044B1
公开(公告)日：2019-02-06
申请号：EP16707062.2
申请日：2016-02-24
Inventor： BADER, Michael , SPECKER, Edgar , MATTHES, Susann , SCHÜTZ, Anja , MALLOW, Keven , GROHMANN, Maik , NAZARÉ, Marc
IPC: C07D487/04 , C07D519/00 , A61K31/522 , A61P3/04 , A61P11/06 , A61P19/10 , A61P25/18 , A61P25/24 , A61P29/00 , A61P35/00
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7.发明授权
公开(公告)号：EP3490996B1
公开(公告)日：2020-08-26
申请号：EP17754278.4
申请日：2017-07-27
Inventor： BADER, Michael , SPECKER, Edgar , MATTHES, Susann , SCHÜTZ, Anja , MALLOW, Keven , GROHMANN, Maik , NAZARÉ, Marc
IPC: C07D519/00
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8.发明公开
公开(公告)号：EP3490996A1
公开(公告)日：2019-06-05
申请号：EP17754278.4
申请日：2017-07-27
Inventor： BADER, Michael , SPECKER, Edgar , MATTHES, Susann , SCHÜTZ, Anja , MALLOW, Keven , GROHMANN, Maik , NAZARÉ, Marc
IPC: C07D519/00
Abstract: The invention relates to a xanthine derivative defined by chemical formula I or a salt thereof, its use as a medicament, especially for use in the treatment of serotonin-related diseases or disorders, and a pharmaceutical preparation comprising the xanthine derivative. The novel xanthine compounds are capable of inhibiting tryptophan hydroxylases (TPH) involved in the biosynthesis of serotonin and are effective in influencing the serotonin level in the body.
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公开(公告)号：EP3448381A1
公开(公告)日：2019-03-06
申请号：EP17720091.2
申请日：2017-04-26
Applicant: Forschungsverbund Berlin E.V.
Inventor： KRAUSE, Gerd , HOYER, Inna , SPECKER, Edgar , FURKERT, Jens , MARCINKOWSKI, Patrick , VON KRIES, Jens-Peter , NEUENSCHWANDER, Martin , NAZARE, Marc
IPC: A61K31/429 , A61K31/495 , A61P5/14 , A61P35/00
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10.发明公开XANTHINE DERIVATIVES, THEIR USE AS A MEDICAMENT, AND PHARMACEUTICAL PREPARATIONS COMPRISING THE SAME 审中-公开黄嘌呤衍生物，它们作为药物的用途以及包含它们的药物制剂
公开(公告)号：EP3262044A1
公开(公告)日：2018-01-03
申请号：EP16707062.2
申请日：2016-02-24
Inventor： BADER, Michael , SPECKER, Edgar , MATTHES, Susann , SCHÜTZ, Anja , MALLOW, Keven , GROHMANN, Maik , NAZARÉ, Marc
IPC: C07D487/04 , C07D519/00 , A61K31/522 , A61P3/04 , A61P11/06 , A61P19/10 , A61P25/18 , A61P25/24 , A61P29/00 , A61P35/00
CPC classification number: C07D473/06 , C07D487/04 , C07D519/00
Abstract: The invention relates to a xanthine derivative defined by chemical formula I or a salt thereof, its use as a medicament, especially for use in the treatment of serotonin-related diseases or disorders, and a pharmaceutical preparation comprising the xanthine derivative. The novel xanthine compounds are capable of inhibiting tryptophan hydroxylases (TPH) involved in the biosynthesis of serotonin and are effective in influencing the serotonin level in the body.
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