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) | 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 (75)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150203453A1 (en) | 2012-10-02 | 2015-07-23 | Epitherapeutics Aps | Inhibitors of histone demethylases |
| EP3763367A1 (en) | 2012-12-06 | 2021-01-13 | Celgene Quanticel Research, Inc. | Pyridine-pyrazole derivatives as histone demethylase inhibitors |
| JP6514117B2 (ja) | 2013-02-27 | 2019-05-15 | エピセラピューティクス アーペーエス | ヒストン脱メチル化酵素の阻害剤 |
| 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 |
| AU2015240465B2 (en) | 2014-04-04 | 2020-02-27 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer |
| SG11201610813TA (en) * | 2014-06-25 | 2017-01-27 | Quanticel Pharmaceuticals Inc | Histone demethylase inhibitors |
| DK3174858T3 (da) | 2014-07-31 | 2019-07-15 | Basf Se | Fremgangsmåde til fremstilling af pyrazoler |
| JP6689821B2 (ja) | 2014-08-12 | 2020-04-28 | シンジェンタ パーティシペーションズ アーゲー | 硫黄含有置換基を有する殺有害生物的に活性な複素環式誘導体 |
| CA2957947A1 (en) | 2014-08-27 | 2016-03-03 | Gilead Sciences, Inc. | Compounds and methods for inhibiting histone demethylases |
| MX2017003464A (es) * | 2014-09-16 | 2017-07-13 | Celgene Quanticel Res Inc | Inhibidores de histona desmetilasa. |
| US9896436B2 (en) | 2014-09-16 | 2018-02-20 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| MX390421B (es) | 2015-05-11 | 2025-03-20 | Basf Se | Proceso para preparar 4-amino-piridazinas. |
| 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 |
| WO2017143011A1 (en) * | 2016-02-16 | 2017-08-24 | Chrysalis, Inc. | Histone demethylase inhibitors |
| WO2017161033A1 (en) * | 2016-03-15 | 2017-09-21 | 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 |
| MX2018014377A (es) | 2016-05-27 | 2019-03-14 | Gilead Sciences Inc | Metodos para tratar infecciones por virus de hepatitis b usando inhibidores de proteina no estructural 5a (ns5a), proteina no estructural 5b (ns5b) o proteina no estructural 3 (ns3). |
| 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 |
| PT3507276T (pt) | 2016-09-02 | 2022-01-11 | Gilead Sciences Inc | Compostos moduladores do recetor de tipo toll |
| 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 |
| 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 |
| 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 |
| JOP20180008A1 (ar) | 2017-02-02 | 2019-01-30 | Gilead Sciences Inc | مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b |
| 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 |
| WO2019123339A1 (en) | 2017-12-20 | 2019-06-27 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| SI3752501T1 (sl) | 2018-02-13 | 2023-08-31 | Gilead Sciences, Inc. | Inhibitorji pd-1/pd-l1 |
| 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 |
| EP3774883A1 (en) | 2018-04-05 | 2021-02-17 | Gilead Sciences, Inc. | Antibodies and fragments thereof that bind hepatitis b virus protein x |
| 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 |
| TWI818007B (zh) | 2018-04-06 | 2023-10-11 | 捷克科學院有機化學與生物化學研究所 | 2'3'-環二核苷酸 |
| 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 |
| TW201945388A (zh) | 2018-04-12 | 2019-12-01 | 美商精密生物科學公司 | 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶 |
| CA3093130C (en) | 2018-04-19 | 2023-10-17 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| TW202014193A (zh) | 2018-05-03 | 2020-04-16 | 捷克科學院有機化學與生物化學研究所 | 包含碳環核苷酸之2’3’－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 |
| JP7158577B2 (ja) | 2018-10-24 | 2022-10-21 | ギリアード サイエンシーズ， インコーポレイテッド | Ｐｄ－１／ｐｄ－ｌ１阻害剤 |
| CA3117556A1 (en) | 2018-10-31 | 2020-05-07 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds as hpk1 inhibitors |
| TWI721624B (zh) | 2018-10-31 | 2021-03-11 | 美商基利科學股份有限公司 | 經取代之6-氮雜苯并咪唑化合物 |
| WO2020178770A1 (en) | 2019-03-07 | 2020-09-10 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotides and prodrugs thereof |
| JP7350871B2 (ja) | 2019-03-07 | 2023-09-26 | 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． | ２’３’－環状ジヌクレオチドおよびそのプロドラッグ |
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| TW202210480A (zh) | 2019-04-17 | 2022-03-16 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
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| JP7237311B2 (ja) * | 2019-06-06 | 2023-03-13 | 京都府公立大学法人 | 化合物、医薬組成物、ｋｄｍ５ｃ阻害剤及び抗うつ剤 |
| 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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| BR112023002164A2 (pt) | 2020-08-07 | 2023-03-14 | Gilead Sciences Inc | Profármacos de análogos de nucleotídeos de fosfonamida e seu uso farmacêutico |
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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 |
| TW202348237A (zh) | 2021-05-13 | 2023-12-16 | 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 |
| CA3222277A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| EP4359389A1 (en) | 2021-06-23 | 2024-05-01 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| JP7686091B2 (ja) | 2021-06-23 | 2025-05-30 | ギリアード サイエンシーズ， インコーポレイテッド | ジアシルグリセロールキナーゼ調節化合物 |
| AU2022298639C1 (en) | 2021-06-23 | 2025-07-17 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| WO2024100791A1 (ja) * | 2022-11-09 | 2024-05-16 | 株式会社日本ファインケム | １－アルキル－５－ヒドロキシピラゾールの製造方法 |
| US20250345389A1 (en) | 2024-05-13 | 2025-11-13 | Gilead Sciences, Inc. | Combination therapies |
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| CA2894399A1 (en) | 2014-06-12 |
| US9714230B2 (en) | 2017-07-25 |
| EP2928471B1 (en) | 2020-10-14 |
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| MX2015007205A (es) | 2016-03-31 |
| WO2014089364A1 (en) | 2014-06-12 |
| EP3763367A1 (en) | 2021-01-13 |
| US20160002201A1 (en) | 2016-01-07 |
| EP2928471A4 (en) | 2016-06-15 |
| US20170158664A1 (en) | 2017-06-08 |
| US9107916B2 (en) | 2015-08-18 |
| US20140194469A1 (en) | 2014-07-10 |
| US9908865B2 (en) | 2018-03-06 |
| US20170275266A1 (en) | 2017-09-28 |
| EP2928471A1 (en) | 2015-10-14 |
| US10173996B2 (en) | 2019-01-08 |
| US9458129B2 (en) | 2016-10-04 |
| US20160068507A1 (en) | 2016-03-10 |
| US20150164872A1 (en) | 2015-06-18 |
| JP2016501882A (ja) | 2016-01-21 |
| US9604961B2 (en) | 2017-03-28 |
| US20160347733A1 (en) | 2016-12-01 |
| US8987461B2 (en) | 2015-03-24 |
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