EA201291073A1 - Производные транилципромина в качестве ингибиторов гистон деметилаз lsd1 и/или lsd2 - Google Patents

Производные транилципромина в качестве ингибиторов гистон деметилаз lsd1 и/или lsd2

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Publication number
EA201291073A1
EA201291073A1 EA201291073A EA201291073A EA201291073A1 EA 201291073 A1 EA201291073 A1 EA 201291073A1 EA 201291073 A EA201291073 A EA 201291073A EA 201291073 A EA201291073 A EA 201291073A EA 201291073 A1 EA201291073 A1 EA 201291073A1
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Prior art keywords
inhibitors
lsd2
lsd1
derivatives
hyston
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EA201291073A
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English (en)
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EA022459B1 (ru
Inventor
Саверио Минуччи
Антонелло Май
Андреа Маттеви
Original Assignee
Университа Дельи Студи Ди Рома "Ла Сапиенца"
Фондацьоне Иэо
Университа Дельи Студи Ди Павия
Университа Дельи Студи Ди Милано
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Publication of EA201291073A1 publication Critical patent/EA201291073A1/ru
Publication of EA022459B1 publication Critical patent/EA022459B1/ru

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    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07C259/04—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
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    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

В изобретении описаны производные транилципромина, используемые в качестве терапевтических агентов, в частности для профилактики и/или лечения заболеваний и состояний, связанных с активностью гистон деметилаз LSD1 и LSD2, например заболеваний, характеризующихся нарушением регуляции транскрипции генов, дифференцировки и пролиферации клеток, таких как опухоли и вирусные инфекции. Эти соединения соответствуют структурной формуле (I), где А и Rопределены в описании изобретения. Кроме того, изобретение относится к препаратам этих соединений, а также к содержащим их композициям и к их терапевтическому применению.
EA201291073A 2010-04-20 2011-04-15 Производные транилципромина в качестве ингибиторов гистон деметилаз lsd1 и/или lsd2 EA022459B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US32595210P 2010-04-20 2010-04-20
PCT/EP2011/055990 WO2011131576A1 (en) 2010-04-20 2011-04-15 Tranylcypromine derivatives as inhibitors of histone demethylase lsd1 and/or lsd2

Publications (2)

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EA201291073A1 true EA201291073A1 (ru) 2013-10-30
EA022459B1 EA022459B1 (ru) 2016-01-29

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Country Status (12)

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US (1) US8765820B2 (ru)
EP (1) EP2560949B1 (ru)
JP (1) JP5934184B2 (ru)
CN (1) CN102985402B (ru)
AU (1) AU2011244478B2 (ru)
BR (1) BR112012027062B8 (ru)
CA (1) CA2797011C (ru)
EA (1) EA022459B1 (ru)
ES (1) ES2564352T3 (ru)
PL (1) PL2560949T3 (ru)
WO (1) WO2011131576A1 (ru)
ZA (1) ZA201207856B (ru)

Families Citing this family (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2361242B1 (en) 2008-10-17 2018-08-01 Oryzon Genomics, S.A. Oxidase inhibitors and their use
US8993808B2 (en) 2009-01-21 2015-03-31 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
WO2011035941A1 (en) 2009-09-25 2011-03-31 Oryzon Genomics S.A. Lysine specific demethylase-1 inhibitors and their use
EP2486002B1 (en) 2009-10-09 2019-03-27 Oryzon Genomics, S.A. Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use
WO2011106106A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae
WO2011106574A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
CA2796726C (en) 2010-04-19 2021-02-16 Oryzon Genomics S.A. Lysine specific demethylase-1 inhibitors and their use
SI2598482T1 (sl) 2010-07-29 2018-09-28 Oryzon Genomics, S.A. Inhibitorji demetilaze lsd1 na osnovi arilciklopropilamina in njihova medicinska uporaba
WO2012013727A1 (en) 2010-07-29 2012-02-02 Oryzon Genomics S.A. Cyclopropylamine derivatives useful as lsd1 inhibitors
US9061966B2 (en) * 2010-10-08 2015-06-23 Oryzon Genomics S.A. Cyclopropylamine inhibitors of oxidases
WO2012072713A2 (en) 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae
EP2712315B1 (en) 2011-02-08 2021-11-24 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative disorders
WO2012107499A1 (en) 2011-02-08 2012-08-16 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders
EP2741741A2 (en) 2011-05-19 2014-06-18 Oryzon Genomics, S.A. Lysine demethylase inhibitors for inflammatory diseases or conditions
US20140296255A1 (en) 2011-05-19 2014-10-02 Oryzong Genomics, S.A. Lysine demethylase inhibitors for thrombosis and cardiovascular diseases
MX2014001568A (es) * 2011-08-09 2014-03-31 Takeda Pharmaceutical Compuesto de ciclopropanoamina.
MY187638A (en) 2011-10-20 2021-10-06 Oryzon Genomics Sa (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
EP2768805B1 (en) * 2011-10-20 2020-03-25 Oryzon Genomics, S.A. (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
CN105051005B (zh) 2012-10-12 2017-06-13 武田药品工业株式会社 环丙胺化合物及其用途
EP2740474A1 (en) 2012-12-05 2014-06-11 Instituto Europeo di Oncologia S.r.l. Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a
JP6521967B2 (ja) 2013-08-06 2019-05-29 イマーゴ バイオサイエンシーズ インコーポレイテッド 疾患の治療のためのｋｄｍ１ａ阻害剤
MX2016010395A (es) 2014-02-13 2017-02-28 Incyte Corp Ciclopropilamina como inhibidor de la desmetilasa 1 especifica de lisinas (lsd1).
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
TW201613860A (en) 2014-02-13 2016-04-16 Incyte Corp Cyclopropylamines as LSD1 inhibitors
EP3626714A1 (en) 2014-02-13 2020-03-25 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
BR112016023382B1 (pt) 2014-04-11 2023-01-10 Takeda Pharmaceutical Company Limited Composto, medicamento, e, uso de um composto
US10233165B2 (en) 2014-05-30 2019-03-19 Istituto Europeo Di Oncologia S.R.L. Cyclopropylamine compounds as histone demethylase inhibitors
EP2949648A1 (en) 2014-05-30 2015-12-02 IEO - Istituto Europeo di Oncologia Srl Cyclopropylamine derivatives as histone demethylase inhibitors
ES2905280T3 (es) 2014-07-03 2022-04-07 Celgene Quanticel Res Inc Inhibidores de la desmetilasa 1 específica de lisina
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
AU2015311805B2 (en) 2014-09-05 2020-04-02 Celgene Quanticel Research, Inc. Inhibitors of lysine specific demethylase-1
EP2993175A1 (en) 2014-09-05 2016-03-09 IEO - Istituto Europeo di Oncologia Srl Thienopyrroles as histone demethylase inhibitors
ES2973286T3 (es) * 2014-11-26 2024-06-19 St Europeo Di Oncologia S R L Modelos de trastornos del desarrollo neurológico basados en la reprogramación y usos de los mismos
CN107438593B (zh) * 2015-01-30 2020-10-30 基因泰克公司 治疗化合物及其用途
CA2976350C (en) 2015-02-12 2023-09-19 Hugh Young Rienhoff, Jr. Kdm1a inhibitors for the treatment of disease
TWI714567B (zh) 2015-04-03 2021-01-01 美商英塞特公司 作為lsd1抑制劑之雜環化合物
EP3090998A1 (en) 2015-05-06 2016-11-09 F. Hoffmann-La Roche AG Solid forms
CN107849611A (zh) 2015-06-12 2018-03-27 奥瑞泽恩基因组学股份有限公司 与lsd1抑制剂相关的生物标志物及其用途
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
UA126277C2 (uk) 2015-08-12 2022-09-14 Інсайт Корпорейшн Солі інгібітору lsd1
SG11201804121RA (en) 2015-11-27 2018-06-28 Taiho Pharmaceutical Co Ltd Novel biphenyl compound or salt thereof
WO2017097865A1 (en) * 2015-12-07 2017-06-15 Istituto Europeo Di Oncologia Combination of caloric restriction (cr) or igf1/insulin receptor inhibitor with lsd1 inhibitor
WO2017157825A1 (en) 2016-03-15 2017-09-21 F. Hoffmann-La Roche Ag Combinations of lsd1 inhibitors for use in the treatment of solid tumors
CN109462980B (zh) 2016-03-15 2022-02-08 奥莱松基因组股份有限公司 用于治疗血液恶性肿瘤的lsd1抑制剂的组合
WO2017158136A1 (en) 2016-03-16 2017-09-21 Oryzon Genomics, S.A. Methods to determine kdm1a target engagement and chemoprobes useful therefor
EP3445339B1 (en) 2016-04-22 2023-08-23 Incyte Corporation Formulations of an lsd1 inhibitor
EP3246330A1 (en) 2016-05-18 2017-11-22 Istituto Europeo di Oncologia S.r.l. Imidazoles as histone demethylase inhibitors
RS58951B1 (sr) 2016-06-10 2019-08-30 Oryzon Genomics Sa Lečenje multiple skleroze
WO2018035259A1 (en) 2016-08-16 2018-02-22 Imago Biosciences, Inc. Methods and processes for the preparation of kdm1a inhibitors
WO2018083138A1 (en) 2016-11-03 2018-05-11 Oryzon Genomics, S.A. Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents
US20190256930A1 (en) 2016-11-03 2019-08-22 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
US11918580B2 (en) 2017-04-26 2024-03-05 Istituto Europeo Di Oncologia S.R.L. Use of a combinational therapy of LSD1 inhibitors with P21 activators in the treatment of cancer
WO2018216800A1 (ja) 2017-05-26 2018-11-29 大鵬薬品工業株式会社 新規なビフェニル化合物又はその塩
PT3632443T (pt) * 2017-05-26 2023-08-31 Taiho Pharmaceutical Co Ltd Potenciador de efeito antitumoral que utiliza um composto de bifenilo
KR20240122847A (ko) 2017-08-03 2024-08-13 오리존 지노믹스 에스.에이. 행동 변경 치료 방법
AU2018316542B2 (en) 2017-08-18 2023-02-16 Istituto Europeo Di Oncologia (Ieo) S.R.L. Indole derivatives as histone demethylase inhibitors
WO2019068326A1 (en) 2017-10-05 2019-04-11 Université D'aix-Marseille INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES
US11685782B2 (en) 2017-10-23 2023-06-27 Children's Medical Center Corporation Methods of treating cancer using LSD1 inhibitors in combination with immunotherapy
CA3103392A1 (en) 2018-05-11 2019-11-14 Imago Biosciences, Inc. Kdm1a inhibitors for the treatment of disease
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
WO2020052647A1 (zh) * 2018-09-13 2020-03-19 南京明德新药研发有限公司 作为lsd1抑制剂的杂螺环类化合物及其应用
CA3130638A1 (en) 2019-03-20 2020-09-24 Oryzon Genomics, S.A. Methods of treating borderline personality disorder
US20220151999A1 (en) 2019-03-20 2022-05-19 Oryzon Genomics, S.A. Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat
WO2021004610A1 (en) 2019-07-05 2021-01-14 Oryzon Genomics, S.A. Biomarkers and methods for personalized treatment of small cell lung cancer using kdm1a inhibitors
IT202000007873A1 (it) 2020-04-14 2021-10-14 St Europeo Di Oncologia S R L Molecole per uso nel trattamento delle infezioni virali
CN111454252B (zh) * 2020-05-13 2021-06-11 郑州大学 含芳环/芳杂环-三氮唑-亚甲基-tcp衍生物及其制备方法和应用
CA3184924A1 (en) * 2020-07-04 2022-01-13 Jin Li Immunomodulator
KR20220027555A (ko) 2020-08-27 2022-03-08 재단법인대구경북과학기술원 트라닐시프로민을 유효성분으로 포함하는 신경염증성 질환의 예방 또는 치료용 약학적 조성물
EP3964204A1 (en) 2020-09-08 2022-03-09 Université d'Aix-Marseille Lsd1 inhibitors for use in the treatment and prevention of fibrosis of tissues
WO2022058405A2 (en) 2020-09-16 2022-03-24 Ifom - Istituto Firc Di Oncologia Molecolare Histone deacetylase inhibitors and uses thereof
CN113750095B (zh) * 2021-03-10 2023-07-04 中国医学科学院医药生物技术研究所 含有环丙基骨架的化合物在制备治疗和/或预防冠状病毒感染药物中的应用
CA3231846A1 (en) 2021-04-08 2022-10-13 Tamara Maes Combinations of lsd1 inhibitors for treating myeloid cancers
WO2023217758A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors
WO2023217784A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating nf1-mutant tumors using lsd1 inhibitors
WO2024110649A1 (en) 2022-11-24 2024-05-30 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9311282D0 (en) * 1993-06-01 1993-07-21 Rhone Poulenc Rorer Ltd New compositions of matter
WO1997036858A1 (en) * 1996-03-29 1997-10-09 G.D. Searle & Co. Cyclopropyl alkanoic acid derivatives
US20020052370A1 (en) * 2000-07-06 2002-05-02 Barber Christopher Gordon Cyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase
WO2005007614A1 (en) * 2003-07-03 2005-01-27 The Government Of The United States Of America As Represented By The Secretary, Department Of Health And Human Services 6011 Monoamine oxidase inhibitors
WO2005007628A1 (en) * 2003-07-11 2005-01-27 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives as cannabinoid receptor modulators
TW200530246A (en) * 2003-12-19 2005-09-16 Bristol Myers Squibb Co Azabicyclic heterocycles as cannabinoid receptor modulators
EP1693062A3 (en) 2005-02-18 2007-12-12 Universitätsklinikum Freiburg Androgen receptor-dependent gene expression control
GB0705656D0 (en) * 2007-03-23 2007-05-02 Addex Pharmaceuticals Sa Novel compounds E1
US8916596B2 (en) 2008-07-24 2014-12-23 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
EP2361242B1 (en) * 2008-10-17 2018-08-01 Oryzon Genomics, S.A. Oxidase inhibitors and their use
US8993808B2 (en) 2009-01-21 2015-03-31 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
WO2010143582A1 (ja) * 2009-06-11 2010-12-16 公立大学法人名古屋市立大学 フェニルシクロプロピルアミン誘導体及びlsd1阻害剤
WO2011035941A1 (en) 2009-09-25 2011-03-31 Oryzon Genomics S.A. Lysine specific demethylase-1 inhibitors and their use

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