JP6256772B2 - 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
- JP6256772B2 JP6256772B2 JP2015549728A JP2015549728A JP6256772B2 JP 6256772 B2 JP6256772 B2 JP 6256772B2 JP 2015549728 A JP2015549728 A JP 2015549728A JP 2015549728 A JP2015549728 A JP 2015549728A JP 6256772 B2 JP6256772 B2 JP 6256772B2
- Authority
- JP
- Japan
- Prior art keywords
- preparation
- compound
- fluoro
- nmr
- mhz
- 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
- MDHZNBDRDJQKNA-UHFFFAOYSA-N CC(C)(C)OC(N1CC(CC[n](c(c2c3)ccc3F)nc2I)CCC1)=O Chemical compound CC(C)(C)OC(N1CC(CC[n](c(c2c3)ccc3F)nc2I)CCC1)=O MDHZNBDRDJQKNA-UHFFFAOYSA-N 0.000 description 1
- VWIMPFAZHUNPKK-UHFFFAOYSA-N CCC[n](c1c2CCC=C1F)nc2Nc(cncc1)c1C(O)=O Chemical compound CCC[n](c1c2CCC=C1F)nc2Nc(cncc1)c1C(O)=O VWIMPFAZHUNPKK-UHFFFAOYSA-N 0.000 description 1
- JITWKGJFUDNUKH-UHFFFAOYSA-N CN1CCC(CC[n](c(cc2)c3cc2F)nc3Nc(cncc2)c2C(O)=O)CC1 Chemical compound CN1CCC(CC[n](c(cc2)c3cc2F)nc3Nc(cncc2)c2C(O)=O)CC1 JITWKGJFUDNUKH-UHFFFAOYSA-N 0.000 description 1
- QWHULRZVRSTPNH-UHFFFAOYSA-N CNCCCCC[n](c(cc1)c2cc1F)nc2Nc(cncc1)c1C(O)=O Chemical compound CNCCCCC[n](c(cc1)c2cc1F)nc2Nc(cncc1)c1C(O)=O QWHULRZVRSTPNH-UHFFFAOYSA-N 0.000 description 1
- NMKOEUOMKQUPGP-UHFFFAOYSA-N Fc(cc1)cc2c1[n](CC1OCCC1)nc2I Chemical compound Fc(cc1)cc2c1[n](CC1OCCC1)nc2I NMKOEUOMKQUPGP-UHFFFAOYSA-N 0.000 description 1
- GRCMLULLNYVGSI-UHFFFAOYSA-N Fc(ccc1n[n]2CC3OCCC3)cc1c2I Chemical compound Fc(ccc1n[n]2CC3OCCC3)cc1c2I GRCMLULLNYVGSI-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
- C07D401/12—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
-
- 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
- C07D401/14—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
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261739521P | 2012-12-19 | 2012-12-19 | |
| US61/739,521 | 2012-12-19 | ||
| US201361792930P | 2013-03-15 | 2013-03-15 | |
| US61/792,930 | 2013-03-15 | ||
| PCT/US2013/076666 WO2014100463A1 (en) | 2012-12-19 | 2013-12-19 | Histone demethylase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016503799A JP2016503799A (ja) | 2016-02-08 |
| JP2016503799A5 JP2016503799A5 (enExample) | 2016-12-01 |
| JP6256772B2 true JP6256772B2 (ja) | 2018-01-10 |
Family
ID=50931614
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015549728A Expired - Fee Related JP6256772B2 (ja) | 2012-12-19 | 2013-12-19 | ヒストンデメチラーゼ阻害剤 |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US9617242B2 (enExample) |
| EP (1) | EP2934145B1 (enExample) |
| JP (1) | JP6256772B2 (enExample) |
| AU (1) | AU2013361255B2 (enExample) |
| CA (1) | CA2895355A1 (enExample) |
| CY (1) | CY1119901T1 (enExample) |
| DK (1) | DK2934145T3 (enExample) |
| ES (1) | ES2658597T3 (enExample) |
| HR (1) | HRP20180067T1 (enExample) |
| HU (1) | HUE037312T2 (enExample) |
| LT (1) | LT2934145T (enExample) |
| PL (1) | PL2934145T3 (enExample) |
| PT (1) | PT2934145T (enExample) |
| RS (1) | RS56821B1 (enExample) |
| SI (1) | SI2934145T1 (enExample) |
| SM (1) | SMT201800070T1 (enExample) |
| WO (1) | WO2014100463A1 (enExample) |
Families Citing this family (69)
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| CN113679717A (zh) | 2012-08-22 | 2021-11-23 | 康奈尔大学 | 用于抑制肌成束蛋白的方法 |
| CN104981458B (zh) | 2012-10-02 | 2017-07-21 | 吉利德科学公司 | 组蛋白去甲基化酶抑制剂 |
| HUE037312T2 (hu) | 2012-12-19 | 2018-08-28 | Celgene Quanticel Res Inc | Hiszton demetiláz inhibitorok |
| KR20150100814A (ko) | 2012-12-21 | 2015-09-02 | 콴티셀 파마슈티컬스, 인크. | 히스톤 데메틸라제 억제제 |
| SG10201707027SA (en) | 2013-02-27 | 2017-09-28 | Epitherapeutics Aps | Inhibitors of histone demethylases |
| EP2968282B1 (en) | 2013-03-12 | 2018-05-09 | Celgene Quanticel Research, Inc. | Histone dementhylase inhibitors |
| EP2970307B1 (en) | 2013-03-13 | 2020-03-11 | Genentech, Inc. | Pyrazolo compounds and uses thereof |
| CA2940144C (en) | 2014-02-20 | 2023-06-13 | Cornell University | Substituted indazol-3-yl derivatives and pharmaceutical compositions thereof useful as inhibitor of fascin |
| NZ728120A (en) | 2014-06-25 | 2023-06-30 | Celgene Quanticel Res Inc | Histone demethylase inhibitors |
| KR20170040805A (ko) | 2014-08-27 | 2017-04-13 | 길리애드 사이언시즈, 인코포레이티드 | 히스톤 데메틸라제를 억제하기 위한 화합물 및 방법 |
| US10030017B2 (en) | 2014-09-17 | 2018-07-24 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| KR20170048591A (ko) | 2014-09-17 | 2017-05-08 | 셀젠 콴티셀 리서치, 인크. | 히스톤 데메틸라제 억제제 |
| ES2751464T3 (es) | 2014-09-17 | 2020-03-31 | Celgene Quanticel Res Inc | Inhibidores de histona desmetilasa |
| CN108698997A (zh) | 2015-12-28 | 2018-10-23 | 赛尔基因昆蒂赛尔研究公司 | 组蛋白脱甲基酶抑制剂 |
| CN105601555B (zh) * | 2016-03-14 | 2018-07-31 | 苏州大学 | 一种制备硝基吲哚衍生物的方法 |
| JP6970681B2 (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 |
| 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 |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| ES2826748T3 (es) | 2016-09-02 | 2021-05-19 | Gilead Sciences Inc | Derivados de 4,6-diamino-pirido[3,2-d]pirimidina como moduladores de receptores de tipo Toll |
| KR102268448B1 (ko) | 2016-09-02 | 2021-06-22 | 길리애드 사이언시즈, 인코포레이티드 | 톨 유사 수용체 조정제 화합물 |
| MA46535A (fr) | 2016-10-14 | 2019-08-21 | Prec Biosciences Inc | Méganucléases modifiées spécifiques de séquences de reconnaissance dans le génome du virus de l'hépatite b |
| EP3535242B1 (en) * | 2016-10-20 | 2024-01-24 | B.G. Negev Technologies and Applications Ltd., at Ben-Gurion University | Dna primase and gyrase inhibitors |
| TWI868958B (zh) | 2017-01-31 | 2025-01-01 | 美商基利科學股份有限公司 | 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型 |
| JOP20180008A1 (ar) | 2017-02-02 | 2019-01-30 | Gilead Sciences Inc | مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b |
| WO2018149986A1 (en) * | 2017-02-16 | 2018-08-23 | Oryzon Genomics, S.A. | 2-(bicyclo-heteroaryl)-isonicotinic derivatives as histone demethylase inhibitors |
| JP7442439B2 (ja) | 2017-03-30 | 2024-03-04 | アルベルト－ルートヴィヒ－ユニバーシティー フライブルク | Ｋｄｍ４阻害剤 |
| JOP20180040A1 (ar) | 2017-04-20 | 2019-01-30 | Gilead Sciences Inc | مثبطات pd-1/pd-l1 |
| CN111511754B (zh) | 2017-12-20 | 2023-09-12 | 捷克共和国有机化学与生物化学研究所 | 活化sting转接蛋白的具有膦酸酯键的2’3’环状二核苷酸 |
| EP3728283B1 (en) | 2017-12-20 | 2023-11-22 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
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| KR102526964B1 (ko) | 2018-02-26 | 2023-04-28 | 길리애드 사이언시즈, 인코포레이티드 | Hbv 복제 억제제로서의 치환된 피롤리진 화합물 |
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| KR102658602B1 (ko) | 2018-10-31 | 2024-04-19 | 길리애드 사이언시즈, 인코포레이티드 | Hpk1 억제 활성을 갖는 치환된 6-아자벤즈이미다졸 화합물 |
| FI3873903T3 (fi) | 2018-10-31 | 2024-03-26 | Gilead Sciences Inc | Substituoituja 6-azabentsiimidatsoliyhdisteitä HPK1-inhibiittoreina |
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| DK4069729T3 (da) | 2019-12-06 | 2025-04-07 | Prec Biosciences Inc | Optimerede, modificerede meganukleaser med specificitet for en genkendelsessekvens i hepatitis b-virusgenomet |
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| JP7712352B2 (ja) | 2020-08-07 | 2025-07-23 | ギリアード サイエンシーズ， インコーポレイテッド | ホスホンアミドヌクレオチド類似体のプロドラッグ及びその薬学的使用 |
| TW202406932A (zh) | 2020-10-22 | 2024-02-16 | 美商基利科學股份有限公司 | 介白素2-Fc融合蛋白及使用方法 |
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| AU2022299051B2 (en) | 2021-06-23 | 2025-03-13 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
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| WO2025240242A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
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| AU2009320683B2 (en) * | 2008-11-28 | 2012-07-19 | Kowa Company, Ltd. | Pyridine-3-carboxyamide derivative |
| JP5864546B2 (ja) * | 2010-05-07 | 2016-02-17 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ | インダゾール |
| EP3323820B1 (en) * | 2011-02-28 | 2023-05-10 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| HUE037312T2 (hu) | 2012-12-19 | 2018-08-28 | Celgene Quanticel Res Inc | Hiszton demetiláz inhibitorok |
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2013
- 2013-12-19 HU HUE13866465A patent/HUE037312T2/hu unknown
- 2013-12-19 US US14/653,818 patent/US9617242B2/en active Active
- 2013-12-19 PT PT138664651T patent/PT2934145T/pt unknown
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- 2013-12-19 SI SI201330913T patent/SI2934145T1/en unknown
- 2013-12-19 WO PCT/US2013/076666 patent/WO2014100463A1/en not_active Ceased
- 2013-12-19 ES ES13866465.1T patent/ES2658597T3/es active Active
- 2013-12-19 PL PL13866465T patent/PL2934145T3/pl unknown
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- 2013-12-19 EP EP13866465.1A patent/EP2934145B1/en active Active
- 2013-12-19 US US14/134,989 patent/US8969343B2/en active Active
- 2013-12-19 DK DK13866465.1T patent/DK2934145T3/en active
- 2013-12-19 JP JP2015549728A patent/JP6256772B2/ja not_active Expired - Fee Related
- 2013-12-19 HR HRP20180067TT patent/HRP20180067T1/hr unknown
- 2013-12-19 AU AU2013361255A patent/AU2013361255B2/en not_active Ceased
- 2013-12-19 CA CA2895355A patent/CA2895355A1/en not_active Abandoned
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2017
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Also Published As
| Publication number | Publication date |
|---|---|
| CA2895355A1 (en) | 2014-06-26 |
| DK2934145T3 (en) | 2018-02-05 |
| PL2934145T3 (pl) | 2018-04-30 |
| WO2014100463A1 (en) | 2014-06-26 |
| US10040779B2 (en) | 2018-08-07 |
| LT2934145T (lt) | 2018-02-26 |
| US20180305336A1 (en) | 2018-10-25 |
| AU2013361255A1 (en) | 2015-07-09 |
| EP2934145B1 (en) | 2017-11-15 |
| CY1119901T1 (el) | 2018-06-27 |
| US20160060247A1 (en) | 2016-03-03 |
| HUE037312T2 (hu) | 2018-08-28 |
| US20140171432A1 (en) | 2014-06-19 |
| US10336727B2 (en) | 2019-07-02 |
| PT2934145T (pt) | 2018-02-13 |
| SMT201800070T1 (it) | 2018-03-08 |
| JP2016503799A (ja) | 2016-02-08 |
| SI2934145T1 (en) | 2018-03-30 |
| ES2658597T3 (es) | 2018-03-12 |
| RS56821B1 (sr) | 2018-04-30 |
| US9617242B2 (en) | 2017-04-11 |
| EP2934145A1 (en) | 2015-10-28 |
| AU2013361255B2 (en) | 2017-01-05 |
| US20170174656A1 (en) | 2017-06-22 |
| HRP20180067T1 (hr) | 2018-02-23 |
| US8969343B2 (en) | 2015-03-03 |
| EP2934145A4 (en) | 2016-06-29 |
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