JP6256771B2 - ヒストンデメチラーゼ阻害剤 - Google Patents
ヒストンデメチラーゼ阻害剤 Download PDFInfo
- Publication number
- JP6256771B2 JP6256771B2 JP2015545854A JP2015545854A JP6256771B2 JP 6256771 B2 JP6256771 B2 JP 6256771B2 JP 2015545854 A JP2015545854 A JP 2015545854A JP 2015545854 A JP2015545854 A JP 2015545854A JP 6256771 B2 JP6256771 B2 JP 6256771B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pyrazol
- formula
- hydrogen
- alkyl
- 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
- BYQBOQLUMFTYSC-UHFFFAOYSA-N COC(CC(Cc(ccc(F)c1)c1F)=O)=O Chemical compound COC(CC(Cc(ccc(F)c1)c1F)=O)=O BYQBOQLUMFTYSC-UHFFFAOYSA-N 0.000 description 1
- UAYJDMXKEJFPHE-UHFFFAOYSA-N Cc1cc(F)c(Cc(cc2O)n[n]2-c2cc(C#N)ccn2)cc1 Chemical compound Cc1cc(F)c(Cc(cc2O)n[n]2-c2cc(C#N)ccn2)cc1 UAYJDMXKEJFPHE-UHFFFAOYSA-N 0.000 description 1
- OUHLSUWZMMWTNI-UHFFFAOYSA-N Cc1cc(F)c(Cc(cc2O)n[n]2-c2nccc(C(O)=O)c2)cc1 Chemical compound Cc1cc(F)c(Cc(cc2O)n[n]2-c2nccc(C(O)=O)c2)cc1 OUHLSUWZMMWTNI-UHFFFAOYSA-N 0.000 description 1
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
- C07D401/04—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
-
- 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
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261734330P | 2012-12-06 | 2012-12-06 | |
| US61/734,330 | 2012-12-06 | ||
| US201361784414P | 2013-03-14 | 2013-03-14 | |
| US61/784,414 | 2013-03-14 | ||
| PCT/US2013/073424 WO2014089364A1 (en) | 2012-12-06 | 2013-12-05 | Histone demethylase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016501882A JP2016501882A (ja) | 2016-01-21 |
| JP2016501882A5 JP2016501882A5 (enExample) | 2016-12-01 |
| JP6256771B2 true JP6256771B2 (ja) | 2018-01-10 |
Family
ID=50884011
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015545854A Expired - Fee Related JP6256771B2 (ja) | 2012-12-06 | 2013-12-05 | ヒストンデメチラーゼ阻害剤 |
Country Status (7)
| Country | Link |
|---|---|
| US (7) | US8987461B2 (enExample) |
| EP (2) | EP2928471B1 (enExample) |
| JP (1) | JP6256771B2 (enExample) |
| CA (1) | CA2894399A1 (enExample) |
| ES (1) | ES2834959T3 (enExample) |
| MX (1) | MX2015007205A (enExample) |
| WO (1) | WO2014089364A1 (enExample) |
Families Citing this family (78)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2654143T3 (es) | 2012-10-02 | 2018-02-12 | Gilead Sciences, Inc. | Inhibidores de desmetilasas de histonas |
| US8987461B2 (en) | 2012-12-06 | 2015-03-24 | Quanticel Pharmaceuticals, Inc. | Histone demethylase inhibitors |
| SG10201707027SA (en) | 2013-02-27 | 2017-09-28 | Epitherapeutics Aps | Inhibitors of histone demethylases |
| JP2017066030A (ja) * | 2014-02-04 | 2017-04-06 | アグロカネショウ株式会社 | 新規なピラゾール誘導体およびこれを有効成分とする農園芸用薬剤 |
| KR102359214B1 (ko) | 2014-04-04 | 2022-02-07 | 델 마 파마슈티컬스 | 폐의 비소세포 암종 및 난소암을 치료하기 위한 디안하이드로갈락티톨 및 이의 유사체 또는 유도체 |
| CN106660982B (zh) * | 2014-06-25 | 2020-09-08 | 赛尔基因昆蒂赛尔研究公司 | 组蛋白脱甲基酶抑制剂 |
| JP6625610B2 (ja) | 2014-07-31 | 2019-12-25 | ビーエーエスエフ ソシエタス・ヨーロピアＢａｓｆ Ｓｅ | ピラゾールの調製方法 |
| BR112017002598B1 (pt) | 2014-08-12 | 2022-03-03 | Syngenta Participations Ag | Derivados heterocíclicos ativos do ponto de vista pesticida com substituintes contendo enxofre |
| JP2017526675A (ja) | 2014-08-27 | 2017-09-14 | ギリアード サイエンシーズ， インコーポレイテッド | ヒストンデメチラーゼを阻害するための化合物および方法 |
| CA2961525A1 (en) * | 2014-09-16 | 2016-03-24 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| US9896436B2 (en) | 2014-09-16 | 2018-02-20 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| CN107592859A (zh) | 2015-05-11 | 2018-01-16 | 巴斯夫欧洲公司 | 制备4‑氨基哒嗪类的方法 |
| JP6900400B2 (ja) | 2016-02-02 | 2021-07-07 | ビーエイエスエフ・ソシエタス・エウロパエアＢａｓｆ Ｓｅ | ピラゾールを調製する接触水素化方法 |
| US20190055212A1 (en) * | 2016-02-16 | 2019-02-21 | Stephen Gwaltney | Histone demethylase inhibitors |
| JP6970680B2 (ja) * | 2016-03-15 | 2021-11-24 | セルジーン クオンティセル リサーチ，インク． | ヒストンデメチラーゼ阻害剤 |
| US10150754B2 (en) | 2016-04-19 | 2018-12-11 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| WO2017198785A1 (en) * | 2016-05-18 | 2017-11-23 | Ieo - Istituto Europeo Di Oncologia S.R.L. | Oxime derivatives useful as inhibitors of histone demethylase kdm4c |
| ES2969239T3 (es) | 2016-05-27 | 2024-05-17 | Gilead Sciences Inc | Combinación de ledipasvir y sofosbuvir para su uso en el tratamiento de infecciones por el virus de la hepatitis B en humanos |
| BR102017010009A2 (pt) | 2016-05-27 | 2017-12-12 | Gilead Sciences, Inc. | Compounds for the treatment of hepatitis b virus infection |
| WO2017207813A1 (en) | 2016-06-03 | 2017-12-07 | Oryzon Genomics, S.A. | Heteroaryl-carboxylic acids as histone demethylase inhibitors |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| WO2018045150A1 (en) | 2016-09-02 | 2018-03-08 | Gilead Sciences, Inc. | 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators |
| SI3507276T1 (sl) | 2016-09-02 | 2022-01-31 | Gilead Sciences, Inc. | Spojine modulatorja toličnih receptorjev |
| KR20230010826A (ko) | 2016-10-14 | 2023-01-19 | 프리시젼 바이오사이언시스 인코포레이티드 | B형 간염 바이러스 게놈 내의 인식 서열에 대해 특이적인 조작된 메가뉴클레아제 |
| TWI714820B (zh) | 2017-01-31 | 2021-01-01 | 美商基利科學股份有限公司 | 替諾福韋艾拉酚胺(tenofovir alafenamide)之晶型 |
| UY37581A (es) | 2017-02-02 | 2018-08-31 | Gilead Sciences Inc | Compuestos para el tratamiento de la infección por virus de la hepatitis b |
| ES2991090T3 (es) | 2017-03-30 | 2024-12-02 | Univ Freiburg Albert Ludwigs | Inhibidores de KDM4 |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| WO2018219478A1 (en) | 2017-06-02 | 2018-12-06 | Oryzon Genomics, S.A. | Heteroaryl-carboxamides as histone demethylase inhibitors |
| US11203610B2 (en) | 2017-12-20 | 2021-12-21 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2′3′ cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| JP7037667B2 (ja) | 2017-12-20 | 2022-03-16 | インスティチュート オブ オーガニック ケミストリー アンド バイオケミストリー エーエスシーアール，ヴイ．ヴイ．アイ． | Ｓｔｉｎｇアダプタータンパク質を活性化するホスホン酸結合を有する３’３’環状ジヌクレオチド |
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| JP7050165B2 (ja) | 2018-02-26 | 2022-04-07 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｂｖ複製阻害剤としての置換ピロリジン化合物 |
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2013
- 2013-12-05 US US14/098,415 patent/US8987461B2/en active Active
- 2013-12-05 WO PCT/US2013/073424 patent/WO2014089364A1/en not_active Ceased
- 2013-12-05 MX MX2015007205A patent/MX2015007205A/es unknown
- 2013-12-05 ES ES13861234T patent/ES2834959T3/es active Active
- 2013-12-05 JP JP2015545854A patent/JP6256771B2/ja not_active Expired - Fee Related
- 2013-12-05 EP EP13861234.6A patent/EP2928471B1/en active Active
- 2013-12-05 CA CA2894399A patent/CA2894399A1/en not_active Abandoned
- 2013-12-05 EP EP20194603.5A patent/EP3763367A1/en not_active Withdrawn
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2015
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| US9604961B2 (en) | 2017-03-28 |
| US9908865B2 (en) | 2018-03-06 |
| US9458129B2 (en) | 2016-10-04 |
| US20160347733A1 (en) | 2016-12-01 |
| US20170158664A1 (en) | 2017-06-08 |
| US20140194469A1 (en) | 2014-07-10 |
| EP2928471A4 (en) | 2016-06-15 |
| MX2015007205A (es) | 2016-03-31 |
| US20160002201A1 (en) | 2016-01-07 |
| ES2834959T3 (es) | 2021-06-21 |
| EP2928471A1 (en) | 2015-10-14 |
| WO2014089364A1 (en) | 2014-06-12 |
| EP2928471B1 (en) | 2020-10-14 |
| US20170275266A1 (en) | 2017-09-28 |
| US8987461B2 (en) | 2015-03-24 |
| EP3763367A1 (en) | 2021-01-13 |
| US9107916B2 (en) | 2015-08-18 |
| JP2016501882A (ja) | 2016-01-21 |
| US10173996B2 (en) | 2019-01-08 |
| US20150164872A1 (en) | 2015-06-18 |
| US9714230B2 (en) | 2017-07-25 |
| US20160068507A1 (en) | 2016-03-10 |
| CA2894399A1 (en) | 2014-06-12 |
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