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 |
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| HUE033380T2 (en) | 2012-10-02 | 2017-11-28 | Gilead Sciences Inc | Inhibitors of histone demethylases |
| US9604961B2 (en) | 2012-12-06 | 2017-03-28 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| MX2015011097A (es) | 2013-02-27 | 2016-03-09 | Epitherapeutics Aps | Inhibidores de histona desmetilasas. |
| 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 |
| AR100997A1 (es) * | 2014-06-25 | 2016-11-16 | Quanticel Pharmaceuticals Inc | Derivados de piridina como inhibidores de histona demetilasa |
| TR201909606T4 (tr) | 2014-07-31 | 2019-07-22 | Basf Se | Pi̇razollari hazirlamak i̇çi̇n i̇şlem |
| CN107074846B (zh) | 2014-08-12 | 2020-05-19 | 先正达参股股份有限公司 | 具有含硫取代基的杀有害生物活性杂环衍生物 |
| EA201790154A1 (ru) | 2014-08-27 | 2017-08-31 | Джилид Сайэнс, Инк. | Соединения и способы для ингибирования гистоновых деметилаз |
| US9896436B2 (en) | 2014-09-16 | 2018-02-20 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| CN107073006A (zh) * | 2014-09-16 | 2017-08-18 | 赛尔基因昆蒂赛尔研究公司 | 组蛋白脱甲基酶抑制剂 |
| BR112017023935B1 (pt) | 2015-05-11 | 2020-07-07 | Basf Se | processo para a preparação de um composto |
| DK3411360T3 (da) | 2016-02-02 | 2020-06-08 | Basf Se | Fremgangsmåde til katalytisk hydrogenering til fremstilling af pyrazoler |
| US20190055212A1 (en) * | 2016-02-16 | 2019-02-21 | Stephen Gwaltney | 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 |
| CN118178652A (zh) | 2016-05-27 | 2024-06-14 | 吉利德科学公司 | 使用ns5a、ns5b或ns3抑制剂治疗乙型肝炎病毒感染的方法 |
| 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 |
| MA46093A (fr) | 2016-09-02 | 2021-05-19 | Gilead Sciences Inc | Composés modulateurs du recepteur de type toll |
| US10640499B2 (en) | 2016-09-02 | 2020-05-05 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
| FI3526323T3 (fi) | 2016-10-14 | 2023-06-06 | Prec Biosciences Inc | Hepatiitti B -viruksen genomissa oleville tunnistussekvensseille spesifisiä muokattuja meganukleaaseja |
| TW202510891A (zh) | 2017-01-31 | 2025-03-16 | 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 |
| 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 |
| CA3084569A1 (en) | 2017-12-20 | 2019-06-27 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| KR102492115B1 (ko) | 2017-12-20 | 2023-01-27 | 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. | Sting 어댑터 단백질을 활성화하는 포스포네이트 결합을 가진 2'3' 사이클릭 다이뉴클레오티드 |
| EP4227302A1 (en) | 2018-02-13 | 2023-08-16 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| US10836769B2 (en) | 2018-02-26 | 2020-11-17 | Gilead Sciences, Inc. | Substituted pyrrolizine compounds and uses thereof |
| US10870691B2 (en) | 2018-04-05 | 2020-12-22 | Gilead Sciences, Inc. | Antibodies and fragments thereof that bind hepatitis B virus protein X |
| 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 |
| 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 |
| US11142750B2 (en) | 2018-04-12 | 2021-10-12 | Precision Biosciences, Inc. | Optimized engineered meganucleases having specificity for a recognition sequence in the Hepatitis B virus genome |
| US10899735B2 (en) | 2018-04-19 | 2021-01-26 | 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 |
| UA126421C2 (uk) | 2018-07-13 | 2022-09-28 | Гіліад Сайєнсіз, Інк. | Інгібітори pd-1/pd-l1 |
| 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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| HRP20240541T1 (hr) | 2018-10-31 | 2024-07-05 | Gilead Sciences, Inc. | Supstituirani spojevi 6-azabenzimidazola kao inhibitori hpk1 |
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| WO2020178768A1 (en) | 2019-03-07 | 2020-09-10 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator |
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| EP3935066A1 (en) | 2019-03-07 | 2022-01-12 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 3'3'-cyclic dinucleotides and prodrugs thereof |
| TWI751517B (zh) | 2019-04-17 | 2022-01-01 | 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 |
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| EP4219453A4 (en) * | 2020-09-28 | 2024-10-09 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | PYRAZOLE COMPOUND AND ITS PREPARATION METHOD AND ITS USE |
| 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 |
| WO2022241134A1 (en) | 2021-05-13 | 2022-11-17 | Gilead Sciences, Inc. | COMBINATION OF A TLR8 MODULATING COMPOUND AND ANTI-HBV siRNA THERAPEUTICS |
| AU2022297367B2 (en) | 2021-06-23 | 2025-04-10 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| CN117377671A (zh) | 2021-06-23 | 2024-01-09 | 吉利德科学公司 | 二酰基甘油激酶调节化合物 |
| IL309378A (en) | 2021-06-23 | 2024-02-01 | Gilead Sciences Inc | Diacylglyercol kinase modulating compounds |
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| 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 |
| WO2025240244A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies comprising bulevirtide and lonafarnib for use in the treatment of hepatitis d virus infection |
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| US20170158664A1 (en) | 2017-06-08 |
| US20140194469A1 (en) | 2014-07-10 |
| US10173996B2 (en) | 2019-01-08 |
| EP2928471A1 (en) | 2015-10-14 |
| EP2928471B1 (en) | 2020-10-14 |
| US8987461B2 (en) | 2015-03-24 |
| US20160347733A1 (en) | 2016-12-01 |
| US20170275266A1 (en) | 2017-09-28 |
| JP2016501882A (ja) | 2016-01-21 |
| US9908865B2 (en) | 2018-03-06 |
| ES2834959T3 (es) | 2021-06-21 |
| EP2928471A4 (en) | 2016-06-15 |
| CA2894399A1 (en) | 2014-06-12 |
| US9714230B2 (en) | 2017-07-25 |
| US9604961B2 (en) | 2017-03-28 |
| MX2015007205A (es) | 2016-03-31 |
| US20160002201A1 (en) | 2016-01-07 |
| US9107916B2 (en) | 2015-08-18 |
| US20160068507A1 (en) | 2016-03-10 |
| US20150164872A1 (en) | 2015-06-18 |
| EP3763367A1 (en) | 2021-01-13 |
| US9458129B2 (en) | 2016-10-04 |
| WO2014089364A1 (en) | 2014-06-12 |
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