CN102985402B - 反苯环丙胺衍生物作为组蛋白去甲基酶lsd1和/或lsd2的抑制剂 - Google Patents

反苯环丙胺衍生物作为组蛋白去甲基酶lsd1和/或lsd2的抑制剂 Download PDF

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CN102985402B
CN102985402B CN201180019945.2A CN201180019945A CN102985402B CN 102985402 B CN102985402 B CN 102985402B CN 201180019945 A CN201180019945 A CN 201180019945A CN 102985402 B CN102985402 B CN 102985402B
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trans
aminocyclopropyl
phenylamino
ylcarbamate
benzyl
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CN102985402A (zh
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S·米努奇
A·麦
A·马泰威
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Ieo-Ccm Foundation
Universita degli Studi di Pavia
Universita degli Studi di Milano
Universita degli Studi di Roma La Sapienza
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Universita degli Studi di Milano
Universita degli Studi di Roma La Sapienza
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CN201180019945.2A 2010-04-20 2011-04-15 反苯环丙胺衍生物作为组蛋白去甲基酶lsd1和/或lsd2的抑制剂 Active CN102985402B (zh)

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US32595210P 2010-04-20 2010-04-20
US61/325,952 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

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CN102985402B true CN102985402B (zh) 2015-04-29

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AU (1) AU2011244478B2 (enExample)
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Families Citing this family (80)

* 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
US8859555B2 (en) 2009-09-25 2014-10-14 Oryzon Genomics S.A. Lysine Specific Demethylase-1 inhibitors and their use
US8946296B2 (en) 2009-10-09 2015-02-03 Oryzon Genomics S.A. Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
US9186337B2 (en) 2010-02-24 2015-11-17 Oryzon Genomics S.A. Lysine demethylase inhibitors for diseases and disorders associated with Hepadnaviridae
WO2011106105A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
RU2599248C2 (ru) 2010-04-19 2016-10-10 Оризон Дженомикс С.А. Лизинспецифические ингибиторы деметилазы-1 и их применение
US9006449B2 (en) 2010-07-29 2015-04-14 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as LSD1 inhibitors
ME03085B (me) 2010-07-29 2019-01-20 Oryzon Genomics Sa Demetilaza inhibitori lsd1 zasnovani na arilciklopropilaminu i njihova medicinska primjena
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
US20140163041A1 (en) 2011-02-08 2014-06-12 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders
EP3981395A1 (en) 2011-02-08 2022-04-13 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative disorders
US20140329833A1 (en) 2011-05-19 2014-11-06 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
UA114406C2 (uk) * 2011-08-09 2017-06-12 Такеда Фармасьютікал Компані Лімітед Похідні циклопропанаміну як інгібітори lsd1
BR112014009238B1 (pt) 2011-10-20 2022-08-09 Oryzon Genomics S.A. Compostos de (hetero)aril ciclopropilamina, seus usos e composições farmacêuticas
BR112014009306B1 (pt) * 2011-10-20 2021-07-20 Oryzon Genomics S.A. Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1
EP2907802B1 (en) 2012-10-12 2019-08-07 Takeda Pharmaceutical Company Limited Cyclopropanamine compound and use thereof
EP2740474A1 (en) * 2012-12-05 2014-06-11 Instituto Europeo di Oncologia S.r.l. Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a
MX383590B (es) 2013-08-06 2025-03-11 Imago Biosciences Inc Inhibidores de kdm1a para el tratamiento de enfermedades.
ME03654B (me) 2014-02-13 2020-07-20 Incyte Corp Ciklopropilamini kao lsd1 inhibitori
TW201613860A (en) 2014-02-13 2016-04-16 Incyte Corp Cyclopropylamines as LSD1 inhibitors
PT3105226T (pt) 2014-02-13 2019-11-06 Incyte Corp Ciclopropilaminas como inibidores de lsd1
WO2015123437A1 (en) 2014-02-13 2015-08-20 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
EP3148974B1 (en) * 2014-05-30 2018-09-26 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
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
CN107074787B (zh) 2014-09-05 2020-10-27 赛尔基因昆蒂赛尔研究公司 赖氨酸特异性脱甲基酶-1的抑制剂
EP2993175A1 (en) 2014-09-05 2016-03-09 IEO - Istituto Europeo di Oncologia Srl Thienopyrroles as histone demethylase inhibitors
WO2016083458A1 (en) * 2014-11-26 2016-06-02 Ieo - Istituto Europeo Di Oncologia S.R.L. Reprogramming-based models of neurodevelopmental disorders and uses thereof
EP3250552B1 (en) * 2015-01-30 2019-03-27 Genentech, Inc. Therapeutic compounds and uses thereof
LT3256218T (lt) 2015-02-12 2025-02-10 Imago Biosciences Inc. Kdm1a inhibitorius ir jo panaudojimas terapijoje
AU2016243939B2 (en) 2015-04-03 2020-09-03 Incyte Holdings Corporation Heterocyclic compounds as LSD1 inhibitors
EP3090998A1 (en) 2015-05-06 2016-11-09 F. Hoffmann-La Roche AG Solid forms
CA2987876A1 (en) 2015-06-12 2016-12-15 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
KR102710120B1 (ko) 2015-08-12 2024-09-27 인사이트 홀딩스 코포레이션 Lsd1 저해제의 염
PL3381896T3 (pl) 2015-11-27 2023-05-08 Taiho Pharmaceutical Co., Ltd. Związek bifenylowy lub jego sól
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
US11013698B2 (en) 2016-03-15 2021-05-25 Oryzon Genomics S.A. Combinations of LSD1 inhibitors for the treatment of hematological malignancies
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
ES3042059T3 (en) 2016-03-16 2025-11-18 Oryzon Genomics Sa Methods to determine kdm1a target engagement and chemoprobes useful therefor
AR109452A1 (es) 2016-04-22 2018-12-12 Incyte Corp Formulación farmacéutica de un inhibidor de lsd1 y método de tratamiento
EP3246330A1 (en) 2016-05-18 2017-11-22 Istituto Europeo di Oncologia S.r.l. Imidazoles as histone demethylase inhibitors
SG11201710199PA (en) 2016-06-10 2018-05-30 Oryzon Genomics Sa Methods of treating multiple sclerosis
CN111194306B (zh) 2016-08-16 2023-05-16 伊美格生物科学公司 用于制备kdm1a抑制剂的方法和过程
US20190256929A1 (en) 2016-11-03 2019-08-22 Oryzon Genomics, S.A. Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents
EP3535420A1 (en) 2016-11-03 2019-09-11 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
WO2018197583A1 (en) 2017-04-26 2018-11-01 Istituto Europeo Di Oncologia Use of a combinational therapy of lsd1 inhibitors with p21 activators in the treatment of cancer
WO2018216795A1 (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を用いた抗腫瘍効果増強剤
MX391414B (es) 2017-05-26 2025-03-21 Taiho Pharmaceutical Co Ltd Compuesto novedoso de bifenilo o sal del mismo.
US12435128B2 (en) 2017-05-31 2025-10-07 Taiho Pharmaceutical Co., Ltd. Method for predicting therapeutic effect of LSD1 inhibitor based on expression of INSM1
SI3661510T1 (sl) 2017-08-03 2025-03-31 Oryzon Genomics, S.A. Postopki zdravljenja vedenjskih sprememb
EP3668877B1 (en) 2017-08-18 2024-05-01 Istituto Europeo di Oncologia 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
WO2019083971A1 (en) * 2017-10-23 2019-05-02 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
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
CN112672994B (zh) * 2018-09-13 2022-09-13 南昌弘益药业有限公司 作为lsd1抑制剂的杂螺环类化合物及其应用
MX2021011254A (es) 2019-03-20 2021-10-01 Oryzon Genomics Sa Metodos de tratamiento del trastorno por deficit de atencion e hiperactividad.
KR20210141933A (ko) 2019-03-20 2021-11-23 오리존 지노믹스 에스.에이. 경계성 인격 장애의 치료 방법
EP3994280A1 (en) 2019-07-05 2022-05-11 Oryzon Genomics, S.A. Biomarkers and methods for personalized treatment of small cell lung cancer using kdm1a inhibitors
PH12022551169A1 (en) 2019-11-13 2024-02-19 Astex Pharmaceuticals Inc METHODS OF TREATING LSD1-RELATED DISEASES and Disorders WITH LSD1 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
AU2021306755B2 (en) * 2020-07-04 2024-05-30 Hitgen Inc. 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
BR112023020554A2 (pt) 2021-04-08 2023-12-05 Oryzon Genomics Sa Combinações de inibidores de lsd1 para o tratamento de cânceres mieloides
JP2025516647A (ja) 2022-05-09 2025-05-30 オリゾン・ゲノミクス・ソシエダッド・アノニマ Lsd1阻害薬を用いる悪性末梢神経鞘腫(mpnst)の治療法
US20250295660A1 (en) 2022-05-09 2025-09-25 Oryzon Genomics, S.A. Methods of treating nf1-mutant tumors using lsd1 inhibitors
AU2023385514A1 (en) 2022-11-24 2025-07-10 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1693062A2 (en) * 2005-02-18 2006-08-23 Universitätsklinikum Freiburg Androgen receptor-dependent gene expression control
CN1918165A (zh) * 2003-12-19 2007-02-21 布里斯托尔-迈尔斯·斯奎布公司 作为大麻素受体调节剂的氮杂双环杂环
WO2010011845A2 (en) * 2008-07-24 2010-01-28 The United States Of America, As Represented By The Secretary, Department Of Health & Human Services Methods of preventing or treating viral infection or reactivation after latency in a host using inhibitors of the lsd1 protein

Family Cites Families (10)

* 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
JP2000507575A (ja) * 1996-03-29 2000-06-20 ジー.ディー.サール アンド カンパニー シクロプロピルアルカノイック酸誘導体
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
US20050014786A1 (en) * 2003-07-11 2005-01-20 Chongqing Sun Tetrahydroquinoline derivatives as cannabinoid receptor modulators
GB0705656D0 (en) * 2007-03-23 2007-05-02 Addex Pharmaceuticals Sa Novel compounds E1
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
JPWO2010143582A1 (ja) 2009-06-11 2012-11-22 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
US8859555B2 (en) 2009-09-25 2014-10-14 Oryzon Genomics S.A. Lysine Specific Demethylase-1 inhibitors and their use

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1918165A (zh) * 2003-12-19 2007-02-21 布里斯托尔-迈尔斯·斯奎布公司 作为大麻素受体调节剂的氮杂双环杂环
EP1693062A2 (en) * 2005-02-18 2006-08-23 Universitätsklinikum Freiburg Androgen receptor-dependent gene expression control
WO2010011845A2 (en) * 2008-07-24 2010-01-28 The United States Of America, As Represented By The Secretary, Department Of Health & Human Services Methods of preventing or treating viral infection or reactivation after latency in a host using inhibitors of the lsd1 protein

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
Comparative Analysis of Small Molecules and Histone Substrate Analogues as LSD1 Lysine Demethylase Inhibitors;Jeffrey C. Culhane等;《J. AM. CHEM. SOC.》;20100211;第132卷(第9期);第3164–3176页 *
Facile synthesis of substituted trans-2-arylcyclopropylamine inhibitors of the human histone demethylase LSD1 and monoamine oxidases A and B;David M. Gooden等;《Bioorg Med Chem Lett》;20080515;第18卷(第10期);第3047–3051页 *
Identification of Cell-Active Lysine Specific Demethylase 1-Selective Inhibitors;Rie Ueda等;《J. AM. CHEM. SOC.》;20091116;第131卷(第48期);第17536-17537页 *
Structural Basis for the Inhibition of the LSD1 Histone Demethylase by the Antidepressant trans-2-Phenylcyclopropylamine;Maojun Yang等;《Biochemistry》;20070317;第46卷(第14期);第8058-8065页 *

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