KR102666390B1 - 고체 형태 - Google Patents

고체 형태 Download PDF

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Publication number
KR102666390B1
KR102666390B1 KR1020177035160A KR20177035160A KR102666390B1 KR 102666390 B1 KR102666390 B1 KR 102666390B1 KR 1020177035160 A KR1020177035160 A KR 1020177035160A KR 20177035160 A KR20177035160 A KR 20177035160A KR 102666390 B1 KR102666390 B1 KR 102666390B1
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delete delete
xrpd
solid form
certain embodiments
cancer
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Korean (ko)
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KR20180022660A (ko
Inventor
랄프 디오돈
우르스 슈비터
르네 트루사르디
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오리존 지노믹스 에스.에이.
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00Compounds containing amino groups bound to a carbon skeleton
    • C07C211/33Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/39Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton
    • C07C211/40Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing only non-condensed rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/62Preparation of compounds containing amino groups bound to a carbon skeleton by cleaving carbon-to-nitrogen, sulfur-to-nitrogen, or phosphorus-to-nitrogen bonds, e.g. hydrolysis of amides, N-dealkylation of amines or quaternary ammonium compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/68Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
    • C07C209/78Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton from carbonyl compounds, e.g. from formaldehyde, and amines having amino groups bound to carbon atoms of six-membered aromatic rings, with formation of methylene-diarylamines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/82Purification; Separation; Stabilisation; Use of additives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/82Purification; Separation; Stabilisation; Use of additives
    • C07C209/84Purification
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020177035160A 2015-05-06 2016-05-02 고체 형태 Active KR102666390B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP15166641.9 2015-05-06
EP15166641.9A EP3090998A1 (en) 2015-05-06 2015-05-06 Solid forms
PCT/EP2016/059726 WO2016177656A1 (en) 2015-05-06 2016-05-02 Solid forms

Publications (2)

Publication Number Publication Date
KR20180022660A KR20180022660A (ko) 2018-03-06
KR102666390B1 true KR102666390B1 (ko) 2024-05-21

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Country Status (15)

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US (1) US10221125B2 (enExample)
EP (2) EP3090998A1 (enExample)
JP (2) JP7005007B2 (enExample)
KR (1) KR102666390B1 (enExample)
CN (1) CN107735394B (enExample)
AR (1) AR104505A1 (enExample)
AU (1) AU2016259054B2 (enExample)
BR (1) BR112017023740B1 (enExample)
CA (1) CA2984203C (enExample)
ES (1) ES2969970T3 (enExample)
HU (1) HUE065558T2 (enExample)
IL (1) IL255194B (enExample)
MX (1) MX378732B (enExample)
PL (1) PL3292100T3 (enExample)
WO (1) WO2016177656A1 (enExample)

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AU2012324803B9 (en) 2011-10-20 2017-08-24 Oryzon Genomics, S.A. (hetero)aryl cyclopropylamine compounds as LSD1 inhibitors
EP3090998A1 (en) 2015-05-06 2016-11-09 F. Hoffmann-La Roche AG Solid forms
EP3307267B1 (en) 2016-06-10 2019-04-10 Oryzon Genomics, S.A. Multiple sclerosis treatment
CN120661674A (zh) 2016-03-15 2025-09-19 奥莱松基因组股份有限公司 用于治疗实体瘤的lsd1抑制剂的组合
MX2018011100A (es) 2016-03-15 2019-01-10 Oryzon Genomics Sa Combinaciones de inhibidores de desmetilasa-1 especifica de lisina (lsd1) para el tratamiento de malignidades hematologicas.
US11034991B2 (en) 2016-03-16 2021-06-15 Oryzon Genomics S.A. Methods to determine KDM1A target engagement and chemoprobes useful therefor
CA3071804A1 (en) 2017-08-03 2019-02-07 Oryzon Genomics, S.A. Use of a kdm1a inhibitor in the treatment of behavior alterations
US20210228490A1 (en) * 2018-05-04 2021-07-29 Oryzon Genomics, S.A. Stable pharmaceutical formulation
CN113631164A (zh) 2019-03-20 2021-11-09 奥莱松基因组股份有限公司 使用kdm1a抑制剂如化合物伐菲德司他治疗注意缺陷多动症的方法
HRP20260110T1 (hr) 2019-03-20 2026-03-13 Oryzon Genomics, S.A. Vafidemstat za liječenje neagresivnih simptoma graničnog poremećaja osobnosti
KR20210142614A (ko) * 2019-03-25 2021-11-25 오리존 지노믹스 에스.에이. 암 치료를 위한 이아다뎀스타트 조합물
JP2022546908A (ja) 2019-07-05 2022-11-10 オリゾン・ゲノミクス・ソシエダッド・アノニマ Kdm1a阻害剤を使用した小細胞肺がんの個別化された処置のためのバイオマーカーおよび方法
MX2023011779A (es) 2021-04-08 2023-11-22 Oryzon Genomics Sa Combinaciones de inhibidores de lsd1 para el tratamiento de canceres mieloides.
CN119497613A (zh) 2022-05-09 2025-02-21 奥莱松基因组股份有限公司 使用lsd1抑制剂治疗nf1-突变肿瘤的方法
US20250275969A1 (en) 2022-05-09 2025-09-04 Oryzon Genomics, S.A. Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors
CN120529900A (zh) 2022-11-24 2025-08-22 奥莱松基因组股份有限公司 用于治疗癌症的LSD1抑制剂和Menin抑制剂的组合

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ATE476970T1 (de) 2005-02-18 2010-08-15 Universitaetsklinikum Freiburg Kontrolle der androgen rezeptor-abhängigen gen expression durch hemmung der aminoxidase aktivität der lysin spezifischen demethylase (lsd1)
CN101410367A (zh) 2005-08-10 2009-04-15 约翰·霍普金斯大学 多胺用在抗寄生虫与抗癌治疗学以及作为赖氨酸-特异性脱甲基酶抑制剂
WO2008127734A2 (en) 2007-04-13 2008-10-23 The Johns Hopkins University Lysine-specific demethylase inhibitors
EP2317992A2 (en) 2008-07-24 2011-05-11 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Preventing or treating viral infection using an inhibitor of the lsd1 protein, a mao inhibitor or an inhibitor of lsd1 and a mao inhibitor
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Also Published As

Publication number Publication date
KR20180022660A (ko) 2018-03-06
HUE065558T2 (hu) 2024-06-28
EP3292100C0 (en) 2023-11-15
JP2021119136A (ja) 2021-08-12
WO2016177656A1 (en) 2016-11-10
CA2984203C (en) 2024-07-02
IL255194A0 (en) 2017-12-31
EP3292100B1 (en) 2023-11-15
AU2016259054A1 (en) 2017-11-16
PL3292100T3 (pl) 2024-04-22
CN107735394B (zh) 2021-11-02
MX2017014035A (es) 2018-03-01
MX378732B (es) 2025-03-11
BR112017023740A2 (pt) 2018-07-17
AU2016259054B2 (en) 2020-08-13
US20180086692A1 (en) 2018-03-29
JP7005007B2 (ja) 2022-02-04
ES2969970T3 (es) 2024-05-23
BR112017023740B1 (pt) 2023-11-07
IL255194B (en) 2021-03-25
EP3090998A1 (en) 2016-11-09
AR104505A1 (es) 2017-07-26
EP3292100A1 (en) 2018-03-14
HK1252089A1 (en) 2019-05-17
JP2018516883A (ja) 2018-06-28
HK1245235A1 (zh) 2018-08-24
CN107735394A (zh) 2018-02-23
CA2984203A1 (en) 2016-11-10
US10221125B2 (en) 2019-03-05

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