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)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (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) | US9604961B2 (enExample) |
| EP (2) | EP3763367A1 (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 (76)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2015003959A (es) | 2012-10-02 | 2015-11-16 | Epitherapeutics Aps | Inhibidores de histona demetilasas. |
| EP3763367A1 (en) | 2012-12-06 | 2021-01-13 | Celgene Quanticel Research, Inc. | Pyridine-pyrazole derivatives as histone demethylase inhibitors |
| AU2014222756B2 (en) | 2013-02-27 | 2018-07-26 | Gilead Sciences, Inc. | 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 |
| KR102456088B1 (ko) | 2014-04-04 | 2022-10-19 | 델 마 파마슈티컬스 | 폐의 비소세포 암종 및 난소암을 치료하기 위한 디안하이드로갈락티톨 및 이의 유사체 또는 유도체 |
| HUE053876T2 (hu) | 2014-06-25 | 2021-07-28 | Celgene Quanticel Res Inc | Hiszton demetiláz inhibitorok |
| 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 |
| US10005775B2 (en) | 2014-08-12 | 2018-06-26 | Syngenta Participations, Ag | Pesticidally active heterocyclic derivatives with sulphur containing substituents |
| KR20170040805A (ko) | 2014-08-27 | 2017-04-13 | 길리애드 사이언시즈, 인코포레이티드 | 히스톤 데메틸라제를 억제하기 위한 화합물 및 방법 |
| US9896436B2 (en) | 2014-09-16 | 2018-02-20 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| SG11201702108PA (en) * | 2014-09-16 | 2017-04-27 | Celgene Quanticel Res Inc | Histone demethylase inhibitors |
| US10584102B2 (en) | 2015-05-11 | 2020-03-10 | Basf Se | Process for preparing 4-amino-pyridazines |
| BR112018014357B8 (pt) | 2016-02-02 | 2022-09-06 | Basf Se | Processo para a preparação de um composto de pirazol e composição |
| WO2017143011A1 (en) * | 2016-02-16 | 2017-08-24 | Chrysalis, Inc. | Histone demethylase inhibitors |
| EP3436445B1 (en) * | 2016-03-15 | 2023-09-06 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| 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 |
| BR102017010009A2 (pt) | 2016-05-27 | 2017-12-12 | Gilead Sciences, Inc. | Compounds for the treatment of hepatitis b virus infection |
| KR102202984B1 (ko) | 2016-05-27 | 2021-01-13 | 길리애드 사이언시즈, 인코포레이티드 | Ns5a, ns5b 또는 ns3 억제제를 사용하여 b형 간염 바이러스 감염을 치료하는 방법 |
| 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 |
| US10370342B2 (en) | 2016-09-02 | 2019-08-06 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| US10640499B2 (en) | 2016-09-02 | 2020-05-05 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| CN117402852A (zh) | 2016-10-14 | 2024-01-16 | 精密生物科学公司 | 对乙肝病毒基因组中的识别序列特异性的工程化大范围核酸酶 |
| TWI784370B (zh) | 2017-01-31 | 2022-11-21 | 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 |
| WO2018183370A2 (en) | 2017-03-30 | 2018-10-04 | Albert-Ludwigs-University Freiburg | Kdm4 inhibitors |
| JOP20180040A1 (ar) | 2017-04-20 | 2019-01-30 | Gilead Sciences Inc | مثبطات pd-1/pd-l1 |
| WO2018219478A1 (en) | 2017-06-02 | 2018-12-06 | Oryzon Genomics, S.A. | Heteroaryl-carboxamides as histone demethylase inhibitors |
| AU2018392213B2 (en) | 2017-12-20 | 2021-03-04 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein |
| 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 |
| UA126458C2 (uk) | 2018-02-13 | 2022-10-05 | Гіліад Сайєнсіз, Інк. | Інгібітори pd-1/pd-l1 |
| ES2962605T3 (es) | 2018-02-26 | 2024-03-20 | Gilead Sciences Inc | Compuestos de pirrolizina sustituidos como inhibidores de la replicación del VHB |
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| TW202005654A (zh) | 2018-04-06 | 2020-02-01 | 捷克科學院有機化學與生物化學研究所 | ２，２，─環二核苷酸 |
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| TWI833744B (zh) | 2018-04-06 | 2024-03-01 | 捷克科學院有機化學與生物化學研究所 | 3'3'-環二核苷酸 |
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| WO2020028097A1 (en) | 2018-08-01 | 2020-02-06 | Gilead Sciences, Inc. | Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid |
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| BR112021008255A2 (pt) | 2018-10-31 | 2021-08-03 | Gilead Sciences, Inc. | compostos de 6-azabenzimidazol substituídos como inibidores de hpk1 |
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| US12318403B2 (en) | 2019-03-07 | 2025-06-03 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2′3′-cyclic dinucleotides and prodrugs thereof |
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| CN110128347A (zh) * | 2019-06-17 | 2019-08-16 | 韶远科技（上海)有限公司 | 一种1-甲基-1h-吲唑-6-甲酸的合成方法 |
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| TWI815194B (zh) | 2020-10-22 | 2023-09-11 | 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 |
| TW202310852A (zh) | 2021-05-13 | 2023-03-16 | 美商基利科學股份有限公司 | ＴＬＲ８調節化合物及抗ＨＢＶ ｓｉＲＮＡ療法之組合 |
| EP4359411A1 (en) | 2021-06-23 | 2024-05-01 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| KR20240005901A (ko) | 2021-06-23 | 2024-01-12 | 길리애드 사이언시즈, 인코포레이티드 | 디아실글리세롤 키나제 조절 화합물 |
| CR20230585A (es) | 2021-06-23 | 2024-02-19 | Gilead Sciences Inc | Compuestos Moduladores de Diacilglicerol Quinasa. |
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- 2013-12-05 MX MX2015007205A patent/MX2015007205A/es unknown
- 2013-12-05 JP JP2015545854A patent/JP6256771B2/ja not_active Expired - Fee Related
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- 2013-12-05 CA CA2894399A patent/CA2894399A1/en not_active Abandoned
- 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
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| US9107916B2 (en) | 2015-08-18 |
| US9908865B2 (en) | 2018-03-06 |
| WO2014089364A1 (en) | 2014-06-12 |
| US20140194469A1 (en) | 2014-07-10 |
| US10173996B2 (en) | 2019-01-08 |
| US20170275266A1 (en) | 2017-09-28 |
| US20160068507A1 (en) | 2016-03-10 |
| US9714230B2 (en) | 2017-07-25 |
| US9604961B2 (en) | 2017-03-28 |
| US20170158664A1 (en) | 2017-06-08 |
| MX2015007205A (es) | 2016-03-31 |
| ES2834959T3 (es) | 2021-06-21 |
| EP2928471B1 (en) | 2020-10-14 |
| EP3763367A1 (en) | 2021-01-13 |
| US8987461B2 (en) | 2015-03-24 |
| EP2928471A1 (en) | 2015-10-14 |
| CA2894399A1 (en) | 2014-06-12 |
| US20160347733A1 (en) | 2016-12-01 |
| US9458129B2 (en) | 2016-10-04 |
| US20150164872A1 (en) | 2015-06-18 |
| EP2928471A4 (en) | 2016-06-15 |
| JP2016501882A (ja) | 2016-01-21 |
| US20160002201A1 (en) | 2016-01-07 |
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