KR102450671B1 - 리신 특이적 데메틸라제-1의 저해제 - Google Patents
리신 특이적 데메틸라제-1의 저해제 Download PDFInfo
- Publication number
- KR102450671B1 KR102450671B1 KR1020177002953A KR20177002953A KR102450671B1 KR 102450671 B1 KR102450671 B1 KR 102450671B1 KR 1020177002953 A KR1020177002953 A KR 1020177002953A KR 20177002953 A KR20177002953 A KR 20177002953A KR 102450671 B1 KR102450671 B1 KR 102450671B1
- Authority
- KR
- South Korea
- Prior art keywords
- carbonyl
- fluorobenzonitrile
- methyl
- fluoro
- optionally substituted
- 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
Links
Classifications
-
- 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
- C07D401/06—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
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- 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
- C07D401/12—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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462020758P | 2014-07-03 | 2014-07-03 | |
| US62/020,758 | 2014-07-03 | ||
| PCT/US2015/038661 WO2016004105A1 (en) | 2014-07-03 | 2015-06-30 | Inhibitors of lysine specific demethylase-1 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20170027822A KR20170027822A (ko) | 2017-03-10 |
| KR102450671B1 true KR102450671B1 (ko) | 2022-10-04 |
Family
ID=55019933
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020177002953A Expired - Fee Related KR102450671B1 (ko) | 2014-07-03 | 2015-06-30 | 리신 특이적 데메틸라제-1의 저해제 |
Country Status (18)
| Country | Link |
|---|---|
| US (3) | US10414750B2 (enExample) |
| EP (1) | EP3164509B1 (enExample) |
| JP (2) | JP6525422B2 (enExample) |
| KR (1) | KR102450671B1 (enExample) |
| CN (1) | CN106604997B (enExample) |
| AU (1) | AU2015284197B2 (enExample) |
| BR (1) | BR112017000042B1 (enExample) |
| CA (1) | CA2954060A1 (enExample) |
| CL (1) | CL2016003423A1 (enExample) |
| CO (1) | CO2017000363A2 (enExample) |
| EA (1) | EA201790082A1 (enExample) |
| EC (1) | ECSP17006776A (enExample) |
| ES (1) | ES2905280T3 (enExample) |
| IL (1) | IL249876B (enExample) |
| MX (1) | MX391865B (enExample) |
| SG (1) | SG11201700007YA (enExample) |
| WO (1) | WO2016004105A1 (enExample) |
| ZA (1) | ZA201700072B (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA201790082A1 (ru) * | 2014-07-03 | 2017-08-31 | Селджен Квонтисел Рисёрч, Инк. | Ингибиторы лизин-специфической демитилазы-1 |
| WO2016003917A1 (en) * | 2014-07-03 | 2016-01-07 | Quanticel Pharmaceuticals, Inc. | Inhibitors of lysine specific demethylase-1 |
| KR20180011331A (ko) | 2015-06-12 | 2018-01-31 | 오리존 지노믹스 에스.에이. | Lsd1 억제제와 관련된 바이오마커 및 그의 용도 |
| WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| 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 |
| 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 |
| US20190256930A1 (en) | 2016-11-03 | 2019-08-22 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| AU2018309372B2 (en) | 2017-08-03 | 2024-08-15 | Oryzon Genomics, S.A. | Methods of treating behavior alterations |
| AR112900A1 (es) | 2017-09-13 | 2019-12-26 | Hanmi Pharm Ind Co Ltd | Compuesto derivado de pirazol y uso de este |
| HRP20251471T1 (hr) | 2019-03-20 | 2026-01-02 | Oryzon Genomics, S.A. | Postupci liječenja poremećaja hiperaktivnosti s deficitom pažnje korištenjem inhibitora kdm1a kao što je spoj vafidemstat |
| SI3941466T1 (sl) | 2019-03-20 | 2026-04-30 | Oryzon Genomics, S.A. | Vafidemstat za zdravljenje neagresivnih simptomov mejne osebnostne motnje |
| 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 |
| CA3231846A1 (en) | 2021-04-08 | 2022-10-13 | Tamara Maes | Combinations of lsd1 inhibitors for treating myeloid cancers |
| US20250032454A1 (en) * | 2021-10-18 | 2025-01-30 | Imago Biosciences, Inc. | Kdm1a inhibitors for the treatment of disease |
| US20250275969A1 (en) | 2022-05-09 | 2025-09-04 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
| US20250295660A1 (en) | 2022-05-09 | 2025-09-25 | Oryzon Genomics, S.A. | Methods of treating nf1-mutant tumors using lsd1 inhibitors |
| US20260151399A1 (en) | 2022-11-24 | 2026-06-04 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors and menin inhibitors for treating cancer |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040132726A1 (en) | 2002-08-09 | 2004-07-08 | Astrazeneca Ab And Nps Pharmaceuticals, Inc. | New compounds |
| JP4316232B2 (ja) * | 2001-12-28 | 2009-08-19 | 武田薬品工業株式会社 | アンドロゲン受容体拮抗剤 |
| US20140155339A1 (en) | 2012-11-30 | 2014-06-05 | Darlene E. McCord | Hydroxytyrosol and oleuropein compositions for induction of dna damage, cell death and lsd1 inhibition |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5776954A (en) * | 1996-10-30 | 1998-07-07 | Merck & Co., Inc. | Substituted pyridyl pyrroles, compositions containing such compounds and methods of use |
| CA2471754A1 (en) * | 2001-12-28 | 2003-07-17 | Takeda Chemical Industries, Ltd. | Androgen receptor antagonist |
| US7026311B2 (en) * | 2002-01-10 | 2006-04-11 | Abbott Gmbh & Co., Kg | Dibenzodiazepine derivatives, their preparation and use |
| DK2316831T3 (da) * | 2002-11-21 | 2013-06-10 | Novartis Ag | 2-(Morpholin-4-yl)pyrimidiner som phosphotidylinositol (PI)-3-kinaseinhibitorer samt deres anvendelse ved behandling af cancer |
| US7320644B2 (en) * | 2005-02-22 | 2008-01-22 | American Axle & Manufacturing, Inc. | Universal joint with bearing retention device and method |
| UA105005C2 (uk) * | 2008-06-16 | 2014-04-10 | Юніверсіті Оф Теннессі Рісерч Фаундейшн | Сполуки для лікування раку |
| JP2012102018A (ja) * | 2009-03-03 | 2012-05-31 | Astellas Pharma Inc | アミド化合物 |
| US8765820B2 (en) * | 2010-04-20 | 2014-07-01 | Universita Degli Studi Di Roma “La Sapienza” | Tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and/or LSD2 |
| CA2903081A1 (en) | 2013-03-14 | 2014-09-25 | Quanticel Pharmaceuticals, Inc. | Histone demethylase inhibitors |
| EA201790082A1 (ru) * | 2014-07-03 | 2017-08-31 | Селджен Квонтисел Рисёрч, Инк. | Ингибиторы лизин-специфической демитилазы-1 |
-
2015
- 2015-06-30 EA EA201790082A patent/EA201790082A1/ru unknown
- 2015-06-30 ES ES15815609T patent/ES2905280T3/es active Active
- 2015-06-30 CN CN201580047272.XA patent/CN106604997B/zh not_active Expired - Fee Related
- 2015-06-30 BR BR112017000042-3A patent/BR112017000042B1/pt not_active IP Right Cessation
- 2015-06-30 WO PCT/US2015/038661 patent/WO2016004105A1/en not_active Ceased
- 2015-06-30 SG SG11201700007YA patent/SG11201700007YA/en unknown
- 2015-06-30 CA CA2954060A patent/CA2954060A1/en not_active Abandoned
- 2015-06-30 MX MX2017000170A patent/MX391865B/es unknown
- 2015-06-30 KR KR1020177002953A patent/KR102450671B1/ko not_active Expired - Fee Related
- 2015-06-30 EP EP15815609.1A patent/EP3164509B1/en not_active Not-in-force
- 2015-06-30 JP JP2016575769A patent/JP6525422B2/ja not_active Expired - Fee Related
- 2015-06-30 US US15/323,384 patent/US10414750B2/en active Active
- 2015-06-30 AU AU2015284197A patent/AU2015284197B2/en not_active Ceased
-
2016
- 2016-12-30 CL CL2016003423A patent/CL2016003423A1/es unknown
-
2017
- 2017-01-01 IL IL249876A patent/IL249876B/en active IP Right Grant
- 2017-01-04 ZA ZA2017/00072A patent/ZA201700072B/en unknown
- 2017-01-16 CO CONC2017/0000363A patent/CO2017000363A2/es unknown
- 2017-02-01 EC ECIEPI20176776A patent/ECSP17006776A/es unknown
-
2019
- 2019-02-27 US US16/288,085 patent/US10626103B2/en not_active Expired - Fee Related
- 2019-02-28 US US16/289,278 patent/US10626104B2/en not_active Expired - Fee Related
- 2019-04-26 JP JP2019086398A patent/JP6833896B2/ja active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4316232B2 (ja) * | 2001-12-28 | 2009-08-19 | 武田薬品工業株式会社 | アンドロゲン受容体拮抗剤 |
| US20040132726A1 (en) | 2002-08-09 | 2004-07-08 | Astrazeneca Ab And Nps Pharmaceuticals, Inc. | New compounds |
| US20140155339A1 (en) | 2012-11-30 | 2014-06-05 | Darlene E. McCord | Hydroxytyrosol and oleuropein compositions for induction of dna damage, cell death and lsd1 inhibition |
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| JP6768857B2 (ja) | リジン特異的なデメチラーゼ−１の阻害剤 | |
| KR102438302B1 (ko) | 리신 특이적 데메틸라제-1의 억제제 | |
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