CR20130550A - Ciclopropilaminas como inhibidores de desmetilasa 1 específica de lisina - Google Patents

Ciclopropilaminas como inhibidores de desmetilasa 1 específica de lisina

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Publication number
CR20130550A
CR20130550A CR20130550A CR20130550A CR20130550A CR 20130550 A CR20130550 A CR 20130550A CR 20130550 A CR20130550 A CR 20130550A CR 20130550 A CR20130550 A CR 20130550A CR 20130550 A CR20130550 A CR 20130550A
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CR
Costa Rica
Prior art keywords
demethylase
specific
cyclopropilamins
lisina
inhibitors
Prior art date
Application number
CR20130550A
Other languages
English (en)
Inventor
Neil W Johnson
Jiri Kasparec
William Henry Miller
Meagan B Rouse
Dominic Suarez
Xinrong Tian
Original Assignee
Glaxosmithkline Ip No 2 Ltd
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Filing date
Publication date
Application filed by Glaxosmithkline Ip No 2 Ltd filed Critical Glaxosmithkline Ip No 2 Ltd
Publication of CR20130550A publication Critical patent/CR20130550A/es

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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • 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
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/33—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/34—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton
    • C07C211/35—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing only non-condensed rings
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/33—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/34—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton
    • C07C211/36—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing at least two amino groups bound to the carbon skeleton
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    • 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
    • C07C271/24—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 ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96—Sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/04—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with only hydrogen atoms, halogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02—Boron compounds
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    • C07—ORGANIC CHEMISTRY
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    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/59—Hydrogenated pyridine rings
    • 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

Abstract

Esta invención se relaciona al uso de derivados de ciclopropilamina para la modulación, en particular lal inhibición de la actividad de desmetilasa 1 específica de Lisina (LSD1); convenientemente, la presente invención se relaciona al uso de ciclopropilaminas en el tratamiento de cáncer.
CR20130550A 2011-03-25 2013-10-25 Ciclopropilaminas como inhibidores de desmetilasa 1 específica de lisina CR20130550A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161467524P 2011-03-25 2011-03-25
US201161514140P 2011-08-02 2011-08-02
US201261594012P 2012-02-02 2012-02-02

Publications (1)

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CR20130550A true CR20130550A (es) 2014-03-24

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CR20130550A CR20130550A (es) 2011-03-25 2013-10-25 Ciclopropilaminas como inhibidores de desmetilasa 1 específica de lisina

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US (4) US8853408B2 (es)
EP (1) EP2688568B1 (es)
JP (1) JP5813855B2 (es)
KR (1) KR101884493B1 (es)
CN (1) CN103857393B (es)
AU (1) AU2012236868B2 (es)
BR (1) BR112013024502B1 (es)
CA (1) CA2831143C (es)
CL (1) CL2013002737A1 (es)
CO (1) CO6771447A2 (es)
CR (1) CR20130550A (es)
DO (1) DOP2013000211A (es)
EA (1) EA023143B1 (es)
ES (1) ES2742805T3 (es)
IL (1) IL228248A (es)
MA (1) MA35096B1 (es)
MX (1) MX347913B (es)
MY (1) MY165620A (es)
PE (1) PE20141322A1 (es)
SG (1) SG193241A1 (es)
WO (1) WO2012135113A2 (es)
ZA (1) ZA201306580B (es)

Families Citing this family (103)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010084160A1 (en) 2009-01-21 2010-07-29 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
EP2486002B1 (en) 2009-10-09 2019-03-27 Oryzon Genomics, S.A. Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use
WO2011106574A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
WO2011106106A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae
CA2796726C (en) 2010-04-19 2021-02-16 Oryzon Genomics S.A. Lysine specific demethylase-1 inhibitors and their use
RS57331B1 (sr) 2010-07-29 2018-08-31 Oryzon Genomics Sa Inhibitori demetilaze za lsd1 zasnovani na arilciklopropilaminu i njihova medicinska upotreba
US9006449B2 (en) 2010-07-29 2015-04-14 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as LSD1 inhibitors
WO2012045883A1 (en) 2010-10-08 2012-04-12 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
AP2014007488A0 (en) * 2011-08-09 2014-03-31 Takeda Pharmaceutical Cyclopropaneamine compound
CN104203914B (zh) 2011-10-20 2017-07-11 奥瑞泽恩基因组学股份有限公司 作为lsd1抑制剂的(杂)芳基环丙胺化合物
US9469597B2 (en) 2011-10-20 2016-10-18 Oryzon Genomics S.A. (Hetero)aryl cyclopropylamine compounds as LSD1 inhibitors
MD20150043A2 (ro) 2012-10-02 2015-08-31 Epitherapeutics Aps Inhibitori ai histon-demetilazelor
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
EP3170811A1 (en) 2013-02-27 2017-05-24 Gilead Sciences, Inc. Ethyl pyridine-4-carboxylate compound as inhibitor of histone demethylases
EP3003301B1 (en) * 2013-05-30 2021-02-24 Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Vegas Novel suicidal lsd1 inhibitors targeting sox2-expressing cancer cells
KR101595183B1 (ko) * 2013-07-25 2016-02-17 동아에스티 주식회사 벤즈아미드 유도체의 제조방법, 그의 제조에 사용되는 새로운 중간체 및 상기 중간체의 제조방법
AU2014306149B2 (en) * 2013-08-06 2019-09-19 Imago Biosciences Inc. KDM1A inhibitors for the treatment of disease
US9527835B2 (en) * 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
HUE045725T2 (hu) * 2014-02-13 2020-01-28 Incyte Corp Ciklopropilaminok mint LSD1 inhibitorok
EP3392244A1 (en) 2014-02-13 2018-10-24 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
AU2015217073B2 (en) * 2014-02-13 2019-08-22 Incyte Holdings Corporation Cyclopropylamines as LSD1 inhibitors
CN104042616B (zh) * 2014-02-20 2016-08-24 复旦大学附属眼耳鼻喉科医院 赖氨酸特异性去甲基化酶1抑制剂的应用
UY36071A (es) 2014-04-11 2015-11-30 Takeda Pharmaceutical Compuesto de ciclopropanamina y sus usos
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
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
CN107074807A (zh) 2014-08-27 2017-08-18 吉利德科学公司 用于抑制组蛋白脱甲基酶的组合物和方法
WO2016055935A1 (en) * 2014-10-06 2016-04-14 Glaxosmithkline Intellectual Property (No.2) Limited Combination of lysine-specific demethylase 1 inhibitor and thrombopoietin agonist
EA039196B1 (ru) * 2014-10-08 2021-12-16 Инсайт Корпорейшн Циклопропиламины в качестве ингибиторов lsd1
WO2016123387A1 (en) * 2015-01-30 2016-08-04 Genentech, Inc. Therapeutic compounds and uses thereof
KR102626978B1 (ko) 2015-02-12 2024-01-18 이마고 바이오사이언시즈 인코포레이티드 질환 치료를 위한 kdm1a 저해제
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
US10526287B2 (en) 2015-04-23 2020-01-07 Constellation Pharmaceuticals, Inc. LSD1 inhibitors and uses thereof
EP3090998A1 (en) 2015-05-06 2016-11-09 F. Hoffmann-La Roche AG Solid forms
EP3307909A1 (en) 2015-06-12 2018-04-18 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
MY189367A (en) * 2015-08-12 2022-02-08 Incyte Corp Salts of an lsd1 inhibitor
JP2018526371A (ja) 2015-08-27 2018-09-13 ジェネンテック， インコーポレイテッド 治療化合物及びその使用方法
US10059668B2 (en) * 2015-11-05 2018-08-28 Mirati Therapeutics, Inc. LSD1 inhibitors
MA43304A (fr) 2015-11-25 2018-10-03 Genentech Inc Benzamides substitués utiles en tant que bloqueurs de canaux sodiques
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
KR20180117602A (ko) 2015-12-29 2018-10-29 미라티 테라퓨틱스, 인크. Lsd1 억제제
WO2017114497A1 (en) 2015-12-30 2017-07-06 Novartis Ag Immune effector cell therapies with enhanced efficacy
EA201892075A1 (ru) 2016-03-15 2019-04-30 Оризон Дженомикс, С.А. Комбинации ингибиторов lsd1 для применения для лечения солидных опухолей
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.
CN107200706A (zh) * 2016-03-16 2017-09-26 中国科学院上海药物研究所 一类氟取代的环丙胺类化合物及其制备方法、药物组合物和用途
EP3430015A1 (en) 2016-03-16 2019-01-23 Oryzon Genomics, S.A. Methods to determine kdm1a target engagement and chemoprobes useful therefor
EP3854782A1 (en) 2016-03-30 2021-07-28 Genentech, Inc. Substituted benzamides and methods of use thereof
EP3445339B1 (en) 2016-04-22 2023-08-23 Incyte Corporation Formulations of an lsd1 inhibitor
CN107459476B (zh) * 2016-06-03 2022-06-24 中国科学院上海药物研究所 反吲哚啉环丙胺类化合物及其制备方法、药物组合物和用途
SI3307267T1 (sl) 2016-06-10 2019-08-30 Oryzon Genomics, S.A. Zdravljenje multiple skleroze
WO2018020366A1 (en) 2016-07-26 2018-02-01 Glaxosmithkline Intellectual Property (No.2) Limited Crystalline (r)-mandelate salt of (1r,2s)-2-phenylcyclopropylamine
SG10201610038SA (en) * 2016-07-29 2017-12-28 Apple Inc Systems and methods for management of asymmetrical multi-tapped battery packs
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
SG11201903348UA (en) 2016-10-17 2019-05-30 Genentech Inc Therapeutic compounds and methods of use thereof
WO2018083189A1 (en) 2016-11-03 2018-05-11 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
WO2018083138A1 (en) 2016-11-03 2018-05-11 Oryzon Genomics, S.A. Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents
WO2018106984A1 (en) 2016-12-09 2018-06-14 Constellation Pharmaceuticals, Inc. Markers for personalized cancer treatment with lsd1 inhibitors
CA3056527A1 (en) 2017-01-24 2018-08-02 Medshine Discovery Inc. Lsd1 inhibitor and preparation method and application thereof
WO2018175707A1 (en) 2017-03-24 2018-09-27 Genentech, Inc. 4-piperidin-n-(pyrimidin-4-yl)chroman-7-sulfonamide derivatives as sodium channel 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
JP6843979B2 (ja) 2017-05-26 2021-03-17 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
DK3632443T3 (da) 2017-05-26 2023-09-11 Taiho Pharmaceutical Co Ltd Potentiator af antitumorvirkning ved hjælp af en biphenylforbindelse
MA50518A (fr) 2017-05-31 2020-09-09 Taiho Pharmaceutical Co Ltd Méthode de prédiction de l'effet thérapeutique d'un inhibiteur de lsd1 en fonction de l'expression d'insm1
KR20180134675A (ko) * 2017-06-09 2018-12-19 한미약품 주식회사 시클로프로필아민 유도체 화합물 및 이의 용도
JP2020152641A (ja) * 2017-07-07 2020-09-24 国立研究開発法人理化学研究所 リジン特異的脱メチル化酵素１阻害活性を有する新規化合物、その製造方法及びその用途
CN110996949A (zh) 2017-08-03 2020-04-10 奥瑞泽恩基因组学股份有限公司 用于治疗行为改变的方法
AR112900A1 (es) 2017-09-13 2019-12-26 Hanmi Pharm Ind Co Ltd Compuesto derivado de pirazol y uso de este
WO2019068326A1 (en) 2017-10-05 2019-04-11 Université D'aix-Marseille INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES
KR20190040783A (ko) 2017-10-11 2019-04-19 한미약품 주식회사 라이신 특이적 데메틸라제-1 억제제로서의 피라졸 유도체
KR20190040763A (ko) 2017-10-11 2019-04-19 한미약품 주식회사 피라졸로피리딘 유도체 화합물 및 이의 용도
US11685782B2 (en) 2017-10-23 2023-06-27 Children's Medical Center Corporation Methods of treating cancer using LSD1 inhibitors in combination with immunotherapy
WO2019109095A1 (en) * 2017-12-01 2019-06-06 Beth Israel Deaconess Medical Center, Inc. Arsenic trioxide and retinoic acid compounds for treatment of idh2-associated disorders
CN108107199B (zh) * 2017-12-21 2019-02-12 广州市进德生物科技有限公司 一种酶化学发光法测定尿酸的检测试剂盒
US11028075B2 (en) 2018-02-26 2021-06-08 Genentech, Inc. Therapeutic compounds and methods of use thereof
US10947251B2 (en) 2018-03-30 2021-03-16 Genentech, Inc. Therapeutic compounds and methods of use thereof
KR20210008064A (ko) 2018-05-11 2021-01-20 이마고 바이오사이언시즈 인코포레이티드 질환의 치료를 위한 kdm1a 저해제
WO2020015745A1 (zh) * 2018-07-20 2020-01-23 南京明德新药研发有限公司 一种lsd1抑制剂的盐及其晶型
US10968200B2 (en) 2018-08-31 2021-04-06 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
US11649245B2 (en) 2018-09-13 2023-05-16 Helioeast Pharmaceutical Co., Ltd. Cyclopropylamine compound as LSD1 inhibitor and use thereof
EP3890715A4 (en) * 2018-12-04 2023-03-29 The Board Of Regents Of The University Of Texas System THERAPEUTIC AGENTS TARGETING ADENOMATOCOLIC POLYPOSIS (APC) MUTANT FOR THE TREATMENT OF CANCER
JPWO2020138398A1 (ja) * 2018-12-28 2021-11-04 国立研究開発法人理化学研究所 リジン特異的脱メチル化酵素１を阻害する新規化合物、その製造方法及びその用途
WO2020159285A1 (ko) 2019-02-01 2020-08-06 한미약품 주식회사 이미다조피리딘 유도체 화합물 및 이의 용도
AU2020216034A1 (en) 2019-02-01 2021-08-19 Hanmi Pharm. Co., Ltd. Imidazopyridine derivative compounds and use of same
CA3130638A1 (en) 2019-03-20 2020-09-24 Oryzon Genomics, S.A. Methods of treating borderline personality disorder
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
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
WO2021058024A1 (zh) * 2019-09-29 2021-04-01 南京明德新药研发有限公司 Lsd1抑制剂
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
CN115485282A (zh) * 2021-02-09 2022-12-16 南昌弘益药业有限公司 一种氧氮杂螺环化合物、其盐型及其晶型
EP4319732A1 (en) 2021-04-08 2024-02-14 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors for treating myeloid cancers
CN116888122A (zh) * 2021-06-22 2023-10-13 南昌弘益药业有限公司 含氮氧杂螺环类化合物及其应用
CN113512031B (zh) * 2021-07-01 2024-01-30 都创(上海)医药开发有限公司 一种lsd1酶抑制剂tak-418中间体化合物制备方法
GB202115017D0 (en) 2021-10-20 2021-12-01 Univ London Queen Mary Sequential treatments and biomarkers to reverse resistance to kinase inhibitors
WO2023067058A1 (en) 2021-10-20 2023-04-27 Queen Mary University Of London Sequential treatments and biomarkers to reverse resistance to kinase inhibitors
WO2023217784A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating nf1-mutant tumors using lsd1 inhibitors
WO2023217758A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9802206D0 (sv) * 1998-06-22 1998-06-22 Astra Pharma Inc Novel compounds
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
US8859555B2 (en) 2009-09-25 2014-10-14 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
CA2796726C (en) 2010-04-19 2021-02-16 Oryzon Genomics S.A. Lysine specific demethylase-1 inhibitors and their use
RS57331B1 (sr) 2010-07-29 2018-08-31 Oryzon Genomics Sa Inhibitori demetilaze za lsd1 zasnovani na arilciklopropilaminu i njihova medicinska upotreba
US9006449B2 (en) 2010-07-29 2015-04-14 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as LSD1 inhibitors
US20140163041A1 (en) 2011-02-08 2014-06-12 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders
EP2712315B1 (en) 2011-02-08 2021-11-24 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative disorders
CN104203914B (zh) * 2011-10-20 2017-07-11 奥瑞泽恩基因组学股份有限公司 作为lsd1抑制剂的(杂)芳基环丙胺化合物

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