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

Info

Publication number
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
Authority
CN
China
Prior art keywords
trans
aminocyclopropyl
phenylamino
ylcarbamate
benzyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201180019945.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN102985402A (zh
Inventor
S·米努奇
A·麦
A·马泰威
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ieo-Ccm Foundation
Universita degli Studi di Pavia
Universita degli Studi di Milano
Universita degli Studi di Roma La Sapienza
Original Assignee
Universita degli Studi di Pavia
Universita degli Studi di Milano
Universita degli Studi di Roma La Sapienza
FONDAZIONE IEO
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Universita degli Studi di Pavia, Universita degli Studi di Milano, Universita degli Studi di Roma La Sapienza, FONDAZIONE IEO filed Critical Universita degli Studi di Pavia
Publication of CN102985402A publication Critical patent/CN102985402A/zh
Application granted granted Critical
Publication of CN102985402B publication Critical patent/CN102985402B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/42—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/44—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a carbon atom of an unsaturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/77—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/80—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00—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
    • 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
    • C07C259/06—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 having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • 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
    • C07C271/28—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 to a carbon atom of a non-condensed six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
    • C07C275/20—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C275/24—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
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

Publications (2)

Publication Number Publication Date
CN102985402A CN102985402A (zh) 2013-03-20
CN102985402B true CN102985402B (zh) 2015-04-29

Family

ID=43929076

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180019945.2A Active CN102985402B (zh) 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

Country Status (12)

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

Families Citing this family (81)

* 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
WO2010084160A1 (en) 2009-01-21 2010-07-29 Oryzon Genomics S.A. Phenylcyclopropylamine derivatives and their medical use
RU2602814C2 (ru) 2009-09-25 2016-11-20 Оризон Дженомикс С.А. Лизинспецифические ингибиторы деметилазы-1 и их применение
US8946296B2 (en) 2009-10-09 2015-02-03 Oryzon Genomics S.A. Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
WO2011106573A2 (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
RS55348B1 (sr) 2010-04-19 2017-03-31 Oryzon Gnomics S A Inhibitori lizin specifične demetilaze-1 i njihova upotreba
WO2012013728A1 (en) 2010-07-29 2012-02-02 Oryzon Genomics S.A. Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use
EP2598480B1 (en) 2010-07-29 2019-04-24 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
US20140163041A1 (en) 2011-02-08 2014-06-12 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders
WO2012107498A1 (en) 2011-02-08 2012-08-16 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative 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
KR20140052018A (ko) 2011-08-09 2014-05-02 다케다 야쿠힌 고교 가부시키가이샤 시클로프로판아민 화합물
MX356344B (es) * 2011-10-20 2018-05-23 Oryzon Genomics Sa Compuestos de (hetero)arilciclopropilamina como inhibidores de lsd1.
RU2668952C2 (ru) 2011-10-20 2018-10-05 Оризон Дженомикс, С.А. (гетеро)арилциклопропиламины в качестве ингибиторов lsd1
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
ES2734209T3 (es) 2013-08-06 2019-12-04 Imago Biosciences Inc Inhibidores de KDM1A para el tratamiento de enfermedades
MX373103B (es) 2014-02-13 2020-04-17 Incyte Holdings Corp Ciclopropilaminas como inhibidores de desmetilasa específica de lisina 1 (lsd1).
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
SI3105218T1 (sl) 2014-02-13 2019-11-29 Incyte Corp Ciklopropilamini kot inhibitorji LSD1
AR099994A1 (es) 2014-04-11 2016-08-31 Takeda Pharmaceuticals Co Compuesto de ciclopropanamina y sus usos
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
US10414750B2 (en) 2014-07-03 2019-09-17 Celgene Quanticel Research, Inc. Inhibitors of lysine specific demethylase-1
WO2016007727A1 (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
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
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
EP2993175A1 (en) 2014-09-05 2016-03-09 IEO - Istituto Europeo di Oncologia Srl Thienopyrroles as histone demethylase inhibitors
EA201790376A1 (ru) 2014-09-05 2017-08-31 Селджен Квонтисел Рисёрч, Инк. Ингибиторы лизин-специфической деметилазы-1
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
WO2016123387A1 (en) * 2015-01-30 2016-08-04 Genentech, Inc. Therapeutic compounds and uses thereof
PL3256218T3 (pl) 2015-02-12 2025-03-31 Imago Biosciences Inc. Inhibitor kdm1a i jego zastosowanie w terapii
EP3277689B1 (en) 2015-04-03 2019-09-04 Incyte 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
LT3334709T (lt) 2015-08-12 2025-03-10 Incyte Holdings Corporation Lsd1 inhibitoriaus druskos
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
ES3057783T3 (en) 2016-03-15 2026-03-04 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases
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
JP6999574B2 (ja) 2016-04-22 2022-01-18 インサイト・コーポレイション Ｌｓｄ１阻害剤の製剤
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
WO2018083189A1 (en) 2016-11-03 2018-05-11 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
CN110740991B (zh) 2017-05-26 2023-07-04 大鹏药品工业株式会社 新型联苯化合物或其盐
JP6738962B2 (ja) * 2017-05-26 2020-08-12 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
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
MX2020001323A (es) 2017-08-03 2020-03-20 Oryzon Genomics Sa Metodos para tratar alteraciones del comportamiento.
ES2986559T3 (es) 2017-08-18 2024-11-11 St Europeo Di Oncologia S R L Derivados de indol como inhibidores de la histona desmetilasa
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
BR112021001066A2 (pt) 2018-05-11 2021-04-20 Imago Biosciences, Inc. composto, método de tratamento de uma doença mediada por kdm1a, método de tratamento de uma doença mediada por globina, composição farmacêutica; método de inibição de kdm1a, método para obter um efeito em um paciente, e método para inibir pelo menos uma função de kdm1a
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
ES3053813T3 (en) 2019-03-20 2026-01-26 Oryzon Genomics Sa Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat
SG11202109159VA (en) 2019-03-20 2021-10-28 Oryzon Genomics Sa Methods of treating borderline personality disorder
CN114341366A (zh) 2019-07-05 2022-04-12 奥莱松基因组股份有限公司 用于使用kdm1a抑制剂个体化治疗小细胞肺癌的生物标志物和方法
MX2022005812A (es) 2019-11-13 2022-08-16 Taiho Pharmaceutical Co Ltd Metodos de tratamiento de enfermedades y trastornos relacionados con desmetilasa 1 especifica de lisina con inhibidores de desmetilasa 1 especifica de lisina.
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
ES3060380T3 (en) * 2020-07-04 2026-03-26 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
JP2024513260A (ja) 2021-04-08 2024-03-22 オリゾン ジェノミックス ソシエダッド アノニマ 骨髄癌処置のためのｌｓｄ１阻害剤の組み合わせ
CN119546292A (zh) 2022-05-09 2025-02-28 奥莱松基因组股份有限公司 使用lsd1抑制剂治疗恶性周围神经鞘瘤(mpnst)的方法
JP2025516648A (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ｎｆ１変異腫瘍の治療法
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
WO2025212569A1 (en) 2024-04-05 2025-10-09 Park City Bio, LLC Selective serotonin receptor modultors and methods of making and using the same

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
AU2323897A (en) * 1996-03-29 1997-10-22 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
US7276608B2 (en) * 2003-07-11 2007-10-02 Bristol-Myers Squibb Company 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
WO2010084160A1 (en) * 2009-01-21 2010-07-29 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
RU2602814C2 (ru) * 2009-09-25 2016-11-20 Оризон Дженомикс С.А. Лизинспецифические ингибиторы деметилазы-1 и их применение

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 *

Also Published As

Publication number Publication date
PL2560949T3 (pl) 2017-01-31
US8765820B2 (en) 2014-07-01
BR112012027062B1 (pt) 2021-04-20
US20130035377A1 (en) 2013-02-07
CA2797011C (en) 2018-10-02
BR112012027062B8 (pt) 2021-05-25
EA022459B1 (ru) 2016-01-29
JP2013525318A (ja) 2013-06-20
WO2011131576A1 (en) 2011-10-27
ZA201207856B (en) 2013-06-29
EP2560949A1 (en) 2013-02-27
AU2011244478A1 (en) 2012-11-01
JP5934184B2 (ja) 2016-06-15
BR112012027062A2 (pt) 2017-03-14
ES2564352T3 (es) 2016-03-22
EA201291073A1 (ru) 2013-10-30
AU2011244478B2 (en) 2014-07-17
CA2797011A1 (en) 2011-10-27
CN102985402A (zh) 2013-03-20
EP2560949B1 (en) 2015-12-02

Similar Documents

Publication Publication Date Title
CN102985402B (zh) 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
JP5670338B2 (ja) ミトコンドリアの膜透過性遷移の阻害剤として有用なアクリルアミド誘導体
US20250074904A1 (en) Nsd2-targeted checmical degraderts and compositions and methods of use thereof
JP6867998B2 (ja) ガンを処置するのに使用するための置換疎水性ベンゼンスルホンアミドチアゾール化合物
JP5868994B2 (ja) Ｋａｔｉｉ阻害剤
MX2008008529A (es) Inhibidores de amida hidrolasa de acido graso.
CN108409608B (zh) 芳香氮芥类组蛋白去乙酰化酶抑制剂及其制备方法和应用
CN102241673B (zh) 丙烯酰胺类化合物及其医药用途
CN106187898A (zh) 氨基甲酸酯衍生物及其合成方法和用途
JPWO1995009160A1 (ja) ベンゾラクタム誘導体
HUP0001023A2 (hu) 2-(Szubsztituált benzoil)-1-cikloalkánkarbonsav-származékok
CN105481736A (zh) 一种含有苯甘氨酸的肉桂酰胺类组蛋白去乙酰化酶抑制剂及其制备方法和应用
US6797730B2 (en) Peptide deformylase inhibitors
US9255071B2 (en) Compounds having antibacterial activity, process for their preparation and pharmaceutical compositions comprising them
US12162820B2 (en) Peripheral alkyl and alkenyl chains extended benzene derivatives and pharmaceutical composition including the same
HUP0001797A2 (hu) Új nitro-metil-keton-származékok, eljárás előállításukra és ilyen vegyületeket tartalmazó gyógyászati készítmények
WO2011140681A1 (zh) 丙烯酰胺类化合物及其抑制细胞凋亡的用途
HK1088317B (en) 1,2,4-triaminobenzene derivatives useful for treating disorders of the central nervous system

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
C56 Change in the name or address of the patentee
CP01 Change in the name or title of a patent holder

Address after: Rome Italy

Patentee after: Universita Degli Studi Di Roma "La Sapienza"

Patentee after: IEO-CCM Foundation

Patentee after: Universita Degli Studi Di Pavia

Patentee after: Universita Degli Studi Di Milano

Address before: Rome Italy

Patentee before: Universita Degli Studi Di Roma "La Sapienza"

Patentee before: Fondazione IEO

Patentee before: Universita Degli Studi Di Pavia

Patentee before: Universita Degli Studi Di Milano