JP6692350B2 - リジン特異的なデメチラーゼ−１の阻害剤 - Google Patents

リジン特異的なデメチラーゼ−１の阻害剤 Download PDF

Info

Publication number
JP6692350B2
JP6692350B2 JP2017512320A JP2017512320A JP6692350B2 JP 6692350 B2 JP6692350 B2 JP 6692350B2 JP 2017512320 A JP2017512320 A JP 2017512320A JP 2017512320 A JP2017512320 A JP 2017512320A JP 6692350 B2 JP6692350 B2 JP 6692350B2
Authority
JP
Japan
Prior art keywords
pharmaceutically acceptable
compound
acceptable salt
pyrazin
formula
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.)
Expired - Fee Related
Application number
JP2017512320A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017527561A (ja
JP2017527561A5 (enExample
Inventor
チェン，ヤング，ケイ．
カノウニ，トウフィケ
スタッフォード，ジェフリー，アラン
ヴィール，ジェイムス，マービン
Original Assignee
セルジーン クオンティセル リサーチ，インク．
セルジーン クオンティセル リサーチ，インク．
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 セルジーン クオンティセル リサーチ，インク．, セルジーン クオンティセル リサーチ，インク． filed Critical セルジーン クオンティセル リサーチ，インク．
Publication of JP2017527561A publication Critical patent/JP2017527561A/ja
Publication of JP2017527561A5 publication Critical patent/JP2017527561A5/ja
Priority to JP2020072573A priority Critical patent/JP6983273B2/ja
Application granted granted Critical
Publication of JP6692350B2 publication Critical patent/JP6692350B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • 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
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • 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
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07D401/12—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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2017512320A 2014-09-05 2015-09-03 リジン特異的なデメチラーゼ−１の阻害剤 Expired - Fee Related JP6692350B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2020072573A JP6983273B2 (ja) 2014-09-05 2020-04-14 リジン特異的なデメチラーゼ−１の阻害剤

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462046842P 2014-09-05 2014-09-05
US62/046,842 2014-09-05
PCT/US2015/048429 WO2016037005A1 (en) 2014-09-05 2015-09-03 Inhibitors of lysine specific demethylase-1

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2020072573A Division JP6983273B2 (ja) 2014-09-05 2020-04-14 リジン特異的なデメチラーゼ−１の阻害剤

Publications (3)

Publication Number Publication Date
JP2017527561A JP2017527561A (ja) 2017-09-21
JP2017527561A5 JP2017527561A5 (enExample) 2018-10-18
JP6692350B2 true JP6692350B2 (ja) 2020-05-13

Family

ID=55440376

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2017512320A Expired - Fee Related JP6692350B2 (ja) 2014-09-05 2015-09-03 リジン特異的なデメチラーゼ−１の阻害剤
JP2020072573A Expired - Fee Related JP6983273B2 (ja) 2014-09-05 2020-04-14 リジン特異的なデメチラーゼ−１の阻害剤

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2020072573A Expired - Fee Related JP6983273B2 (ja) 2014-09-05 2020-04-14 リジン特異的なデメチラーゼ−１の阻害剤

Country Status (17)

Country Link
US (3) US9822119B2 (enExample)
EP (1) EP3189038B1 (enExample)
JP (2) JP6692350B2 (enExample)
KR (1) KR102476459B1 (enExample)
CN (2) CN112125901A (enExample)
AU (2) AU2015311805B2 (enExample)
BR (1) BR112017004334A2 (enExample)
CA (1) CA2960188A1 (enExample)
CL (1) CL2017000521A1 (enExample)
CO (1) CO2017002191A2 (enExample)
EA (1) EA201790376A1 (enExample)
EC (1) ECSP17013466A (enExample)
ES (1) ES2935114T3 (enExample)
IL (1) IL250876B (enExample)
MX (1) MX381597B (enExample)
SG (2) SG10202008486SA (enExample)
WO (1) WO2016037005A1 (enExample)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112125901A (zh) * 2014-09-05 2020-12-25 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
MX2017015922A (es) 2015-06-12 2018-12-11 Oryzon Genomics Sa Biomarcadores asociados con inhibidores de lsd1 y usos de los mismos.
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
US10059668B2 (en) 2015-11-05 2018-08-28 Mirati Therapeutics, Inc. LSD1 inhibitors
KR102204748B1 (ko) 2015-11-27 2021-01-19 다이호야쿠힌고교 가부시키가이샤 신규 비페닐 화합물 또는 그의 염
SG11201805645QA (en) 2015-12-29 2018-07-30 Mirati Therapeutics Inc Lsd1 inhibitors
EP3429571B1 (en) 2016-03-15 2025-10-08 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases
JP2019512546A (ja) 2016-03-16 2019-05-16 オリゾン・ゲノミクス・ソシエダッド・アノニマ Ｋｄｍ１ａ標的会合を決定するための方法、およびそれに有用な化学プローブ
US10150754B2 (en) 2016-04-19 2018-12-11 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
CN105924397B (zh) * 2016-04-29 2017-11-24 河南省农业科学院植物保护研究所 一种1,5‑二芳基‑3‑甲酸酯吡唑类化合物、制备方法及用途
KR20210141778A (ko) * 2016-06-07 2021-11-23 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
CN116478131A (zh) * 2016-07-12 2023-07-25 锐新医药公司 作为变构shp2抑制剂的2,5-双取代型及2,5,6-三取代型3-甲基吡嗪
EP3535420A1 (en) 2016-11-03 2019-09-11 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
KR102361918B1 (ko) * 2017-05-26 2022-02-14 다이호야쿠힌고교 가부시키가이샤 신규 비페닐 화합물 또는 그의 염
EP3632443B1 (en) * 2017-05-26 2023-06-07 Taiho Pharmaceutical Co., Ltd. Anti-tumor effect potentiator using a biphenyl compound
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
BR112020000827A2 (pt) 2017-08-03 2020-07-21 Oryzon Genomics, S.A. métodos de tratamento de alterações de comportamento
US20210393623A1 (en) 2018-09-26 2021-12-23 Jacobio Pharmaceuticals Co., Ltd. Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors
PH12021552251A1 (en) 2019-03-20 2022-07-25 Oryzon Genomics Sa Methods of treating borderline personality disorder
JP7535797B2 (ja) 2019-03-20 2024-08-19 オリソン ヘノミクス，ソシエダ アノニマ 化合物バフィデムスタット（ｖａｆｉｄｅｍｓｔａｔ）などｋｄｍ１ａ阻害剤を使用した注意欠陥多動性障害の処置方法
EP3986404A1 (en) 2019-06-20 2022-04-27 Celgene Quanticel Research, Inc. Azacitidine in combination with venetoclax, gilteritinib, midostaurin or other compounds for treating leukemia or myelodysplastic syndrome
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
CA3157404A1 (en) 2019-11-13 2021-05-20 Taiho Pharmaceutical Co., Ltd. Novel salt of terphenyl compound
TWI834127B (zh) * 2021-03-11 2024-03-01 大陸商南京明德新藥研發有限公司 噻吩類化合物及其應用
CN117062813A (zh) * 2021-03-24 2023-11-14 四川汇宇制药股份有限公司 一种多环化合物及其应用
BR112023020554A2 (pt) 2021-04-08 2023-12-05 Oryzon Genomics Sa Combinações de inibidores de lsd1 para o tratamento de cânceres mieloides
US20250032454A1 (en) * 2021-10-18 2025-01-30 Imago Biosciences, Inc. Kdm1a inhibitors for the treatment of disease
CN118206499A (zh) * 2021-11-29 2024-06-18 郑州大学 一种2,3,5-三取代吡嗪类化合物及其制备方法和应用
US20250163016A1 (en) * 2022-01-25 2025-05-22 Chengdu Easton Biopharmaceuticals Co., Ltd. Pyridine derivative, preparation method therefor and use thereof
CN116836167B (zh) * 2022-03-25 2025-09-09 腾讯科技（深圳）有限公司 咪唑并[1,2-a]吡嗪或吡唑并[1,5-a]嘧啶衍生物及其用途
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
CN119497613A (zh) 2022-05-09 2025-02-21 奥莱松基因组股份有限公司 使用lsd1抑制剂治疗nf1-突变肿瘤的方法
EP4622635A1 (en) 2022-11-24 2025-10-01 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer
WO2024208187A1 (zh) * 2023-04-03 2024-10-10 上海复星医药（集团）股份有限公司 氮杂芳基化合物及其作为lsd1抑制剂的用途

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6432975B1 (en) 1998-12-11 2002-08-13 Targacept, Inc. Pharmaceutical compositions and methods for use
JP2005500294A (ja) * 2001-06-19 2005-01-06 ブリストル−マイヤーズ　スクイブ　カンパニー ホスホジエステラーゼ７に対するピリミジン阻害剤
EP2316831B1 (en) 2002-11-21 2013-03-06 Novartis AG 2-(morpholin-4-yl)pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer
CA2506568A1 (en) * 2002-11-22 2004-06-10 Merck & Co., Inc. 2-[(4-benzyl)-1-piperidinyl)methyl]benzimidazole-5-ol derivatives as nr2b receptor antagonists
EP1694670A1 (en) * 2003-12-16 2006-08-30 GPC Biotech AG Pyrazine derivatives as effective compounds against infectious diseases
CA2560346A1 (en) * 2004-04-13 2005-10-27 Icagen, Inc. Polycyclic pyridines as potassium ion channel modulators
US20070078135A1 (en) * 2005-04-18 2007-04-05 Neurogen Corporation Substituted heteroaryl CB1 antagonists
FR2896800B1 (fr) * 2006-01-30 2008-04-11 Servier Lab Nouveaux composes pyridinylaminoalkylene-et pyridinyloxyalkylene-cyclopropanamines polysubstitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
AR072845A1 (es) * 2008-07-29 2010-09-22 Boehringer Ingelheim Int 5-alquil-pirimidinas y su uso en el tratamiento de enfermedades mediadas por la actividad de quinasas.
EP2258865A1 (en) 2009-06-05 2010-12-08 Universitätsklinikum Freiburg Lysine-specific demethylase 1 (LSD1) is a biomarker for breast cancer
RU2012132682A (ru) * 2009-12-31 2014-02-10 Пирамал Энтерпрайзис Лимитед Ингибиторы диацилглицерин ацилтрансферазы
EP2560949B1 (en) 2010-04-20 2015-12-02 Università degli Studi di Roma "La Sapienza" Tranylcypromine derivatives as inhibitors of histone demethylase lsd1 and/or lsd2
EP2598480B1 (en) * 2010-07-29 2019-04-24 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as lsd1 inhibitors
KR101351919B1 (ko) 2012-05-23 2014-01-24 현대모비스 주식회사 차선 유지 보조 시스템 및 방법
EP2925307B1 (en) 2012-11-30 2020-10-28 McCord, Darlene E. Hydroxytyrosol and oleuropein compositions for induction of dna damage, cell death and lsd1 inhibition
AR098203A1 (es) 2013-11-13 2016-05-18 Dow Global Technologies Llc Reactivo de ensayo de formaldehído
DK3080100T3 (da) * 2013-12-11 2023-02-06 Celgene Quanticel Res Inc Hæmmere af lysinspecifik demethylase-1
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
CN112125901A (zh) * 2014-09-05 2020-12-25 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

Also Published As

Publication number Publication date
CN112125901A (zh) 2020-12-25
US20180028508A1 (en) 2018-02-01
CA2960188A1 (en) 2016-03-10
MX2017002824A (es) 2017-05-30
EP3189038A4 (en) 2018-02-28
JP2017527561A (ja) 2017-09-21
US10543198B2 (en) 2020-01-28
BR112017004334A2 (pt) 2018-08-07
WO2016037005A1 (en) 2016-03-10
CN107074787B (zh) 2020-10-27
CL2017000521A1 (es) 2017-11-03
KR20170045342A (ko) 2017-04-26
KR102476459B1 (ko) 2022-12-09
CO2017002191A2 (es) 2017-05-19
JP2020125321A (ja) 2020-08-20
MX381597B (es) 2025-03-12
US20200108052A1 (en) 2020-04-09
US9822119B2 (en) 2017-11-21
ECSP17013466A (es) 2017-05-31
AU2020204287A1 (en) 2020-07-16
ES2935114T3 (es) 2023-03-01
EP3189038B1 (en) 2022-11-23
US20160108046A1 (en) 2016-04-21
AU2015311805A1 (en) 2017-03-23
EA201790376A1 (ru) 2017-08-31
IL250876B (en) 2021-09-30
IL250876A0 (en) 2017-04-30
AU2015311805B2 (en) 2020-04-02
JP6983273B2 (ja) 2021-12-17
SG11201701683XA (en) 2017-04-27
SG10202008486SA (en) 2020-09-29
EP3189038A1 (en) 2017-07-12
US10864202B2 (en) 2020-12-15
CN107074787A (zh) 2017-08-18

Similar Documents

Publication Publication Date Title
JP6983273B2 (ja) リジン特異的なデメチラーゼ−１の阻害剤
US10385051B2 (en) Inhibitors of lysine specific demethylase-1
AU2019261771B2 (en) Inhibitors of lysine specific demethylase-1
CN106659914B (zh) 赖氨酸特异性脱甲基酶-1的抑制剂
JP2017525668A (ja) リジン特異的なデメチラーゼ−１の阻害剤
EP4161657A1 (en) Inhibitors of fibroblast growth factor receptor kinases
HK1230202B (en) Inhibitors of lysine specific demethylase-1
HK1230202A1 (en) Inhibitors of lysine specific demethylase-1

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180831

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20180831

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20190509

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20190522

RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7422

Effective date: 20190808

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20190809

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20190820

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20191021

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20200316

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20200414

R150 Certificate of patent or registration of utility model

Ref document number: 6692350

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees