JP6584521B2 - 抗がん剤として有用な置換ヌクレオシド誘導体 - Google Patents
抗がん剤として有用な置換ヌクレオシド誘導体 Download PDFInfo
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- JP6584521B2 JP6584521B2 JP2017544584A JP2017544584A JP6584521B2 JP 6584521 B2 JP6584521 B2 JP 6584521B2 JP 2017544584 A JP2017544584 A JP 2017544584A JP 2017544584 A JP2017544584 A JP 2017544584A JP 6584521 B2 JP6584521 B2 JP 6584521B2
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- Prior art keywords
- cancer
- mmol
- etoac
- methyl
- alkyl
- Prior art date
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- 238000012360 testing method Methods 0.000 description 1
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- 229930192474 thiophene Natural products 0.000 description 1
- 230000009974 thixotropic effect Effects 0.000 description 1
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- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/14—Pyrrolo-pyrimidine radicals
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
- C07H19/167—Purine radicals with ribosyl as the saccharide radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/23—Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups C07H19/14 - C07H19/22
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/24—Heterocyclic radicals containing oxygen or sulfur as ring hetero atom
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
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| US201562119932P | 2015-02-24 | 2015-02-24 | |
| US62/119,932 | 2015-02-24 | ||
| US201562213801P | 2015-09-03 | 2015-09-03 | |
| US62/213,801 | 2015-09-03 | ||
| US201662279209P | 2016-01-15 | 2016-01-15 | |
| US62/279,209 | 2016-01-15 | ||
| PCT/IB2016/050803 WO2016135582A1 (en) | 2015-02-24 | 2016-02-15 | Substituted nucleoside derivatives useful as anticancer agents |
Publications (3)
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| JP2018510850A JP2018510850A (ja) | 2018-04-19 |
| JP2018510850A5 JP2018510850A5 (cg-RX-API-DMAC7.html) | 2018-10-04 |
| JP6584521B2 true JP6584521B2 (ja) | 2019-10-02 |
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| JP2017544584A Expired - Fee Related JP6584521B2 (ja) | 2015-02-24 | 2016-02-15 | 抗がん剤として有用な置換ヌクレオシド誘導体 |
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| AR104326A1 (es) | 2015-05-04 | 2017-07-12 | Lilly Co Eli | Compuestos nucleósidos 5-sustituidos |
| TWI791251B (zh) | 2015-08-26 | 2023-02-01 | 比利時商健生藥品公司 | 使用作為ｐｒｍｔ５抑制劑之新穎經６-６雙環芳香環取代之核苷類似物 |
| ES2891320T3 (es) | 2016-03-10 | 2022-01-27 | Janssen Pharmaceutica Nv | Análogos de nucleósidos sustituidos para su uso como inhibidores de PRMT5 |
| KR20180116307A (ko) | 2016-03-10 | 2018-10-24 | 얀센 파마슈티카 엔.브이. | Prmt5 저해제로 사용하기 위한 치환 뉴클레오사이드 유사체 |
| CA3033020A1 (en) | 2016-09-14 | 2018-03-22 | Janssen Pharmaceutica Nv | Fused bicyclic inhibitors of menin-mll interaction |
| MX392051B (es) | 2016-09-14 | 2025-03-21 | Janssen Pharmaceutica Nv | Inhibidores espirobiciclicos de la interaccion de menina-mll |
| US12084462B2 (en) | 2016-09-14 | 2024-09-10 | Janssen Pharmaceutica Nv | Spiro bicyclic inhibitors of menin-MLL interaction |
| WO2018065365A1 (en) | 2016-10-03 | 2018-04-12 | Janssen Pharmaceutica Nv | Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors |
| KR102531344B1 (ko) * | 2016-10-03 | 2023-05-10 | 얀센 파마슈티카 엔.브이. | Prmt5 억제제로서 사용하기 위한 신규의 모노사이클릭 및 바이사이클릭 고리 시스템 치환된 카르바뉴클레오시드 유사체 |
| JP7142010B2 (ja) | 2016-12-15 | 2022-09-26 | ヤンセン ファーマシューティカ エヌ．ベー． | メニン－ｍｌｌ相互作用のアゼパン阻害剤 |
| WO2018152501A1 (en) * | 2017-02-20 | 2018-08-23 | Prelude Therapeutics, Incorporated | Selective inhibitors of protein arginine methyltransferase 5 (prmt5) |
| US11220524B2 (en) * | 2017-02-20 | 2022-01-11 | Prelude Therapeutics Incorporated | Selective inhibitors of protein arginine methyltransferase 5 (PRMT5) |
| JP7225106B2 (ja) | 2017-02-27 | 2023-02-20 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｐｒｍｔ５阻害剤による治療に応答する癌患者の同定におけるバイオマーカーの使用 |
| WO2018160855A1 (en) | 2017-03-01 | 2018-09-07 | Prelude Therapeutics, Incorporated | Selective inhibitors of protein arginine methyltransferase 5 (prmt5) |
| BR112020002736A2 (pt) | 2017-08-09 | 2020-07-28 | Prelude Therapeutics, Incorporated | inibidores seletivos da proteína arginina metiltransferase 5 (prmt5) |
| CA3079545A1 (en) | 2017-10-26 | 2019-05-02 | Prelude Therapeutics, Incorporated | Selective inhibitors of protein arginine methyltransferase 5 (prmt5) |
| JP7352544B2 (ja) | 2017-12-08 | 2023-09-28 | ヤンセン ファーマシューティカ エヌ．ベー． | 新規なスピロ二環式類似体 |
| AU2018385664B2 (en) | 2017-12-13 | 2022-06-02 | Lupin Limited | Substituted bicyclic heterocyclic compounds as PRMT5 inhibitors |
| US11396517B1 (en) | 2017-12-20 | 2022-07-26 | Janssen Pharmaceutica Nv | Exo-aza spiro inhibitors of menin-MLL interaction |
| CA3092357A1 (en) * | 2018-03-14 | 2019-09-19 | Prelude Therapeutics, Incorporated | Selective inhibitors of protein arginine methyltransferase 5 (prmt5) |
| US10711007B2 (en) | 2018-03-14 | 2020-07-14 | Prelude Therapeutics Incorporated | Selective inhibitors of protein arginine methyltransferase 5 (PRMT5) |
| GB201810092D0 (en) | 2018-06-20 | 2018-08-08 | Ctxt Pty Ltd | Compounds |
| US20210309687A1 (en) * | 2018-08-07 | 2021-10-07 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| US20220160713A1 (en) * | 2019-02-13 | 2022-05-26 | Prelude Therapeutics, Incorporated | Selective inhibitor of protein arginine methyltransferase 5 (prmt5) |
| JP7609798B2 (ja) * | 2019-03-25 | 2025-01-07 | カリフォルニア インスティチュート オブ テクノロジー | Ｐｒｍｔ５インヒビター及びその使用 |
| WO2020206299A1 (en) | 2019-04-05 | 2020-10-08 | Prelude Therapeutics, Incorporated | Selective inhibitors of protein arginine methyltransferase 5 |
| TW202112375A (zh) | 2019-06-06 | 2021-04-01 | 比利時商健生藥品公司 | 使用ｐｒｍｔ５抑制劑治療癌症之方法 |
| DK3980417T3 (en) | 2019-06-10 | 2023-12-18 | Lupin Ltd | PRMT5-Inhibitorer |
| PE20220433A1 (es) | 2019-06-12 | 2022-03-29 | Janssen Pharmaceutica Nv | Intermedios espirobiciclicos novedosos |
| RS64931B9 (sr) | 2019-06-18 | 2025-06-30 | Pfizer | Derivati benzizoxazol sulfonamida |
| BR112022004630A2 (pt) * | 2019-09-18 | 2022-05-31 | Prelude Therapeutics Inc | Inibidores seletivos da proteína arginina metiltransferase 5 (prmt5) |
| BR112022007808A2 (pt) | 2019-10-22 | 2022-07-05 | Lupin Ltd | Combinação farmacêutica de inibidores de prmt5 |
| JP7664248B2 (ja) | 2019-12-03 | 2025-04-17 | ルピン・リミテッド | Ｐｒｍｔ５阻害剤としての置換ヌクレオシドアナログ |
| UA129208C2 (uk) | 2019-12-19 | 2025-02-05 | Янссен Фармацевтика Нв | Заміщені спіропохідні з прямим ланцюгом |
| CA3192055A1 (en) | 2020-08-18 | 2022-02-24 | Incyte Corporation | Process and intermediates for preparing a jak1 inhibitor |
| KR20230096973A (ko) | 2020-08-18 | 2023-06-30 | 인사이트 코포레이션 | Jak 저해제를 제조하기 위한 방법 및 중간체 |
| US20240101589A1 (en) * | 2020-10-08 | 2024-03-28 | Strom Therapeutics Limited | Inhibitors of mettl3 |
| CN112679505B (zh) * | 2020-12-25 | 2022-04-22 | 杭州澳赛诺生物科技有限公司 | 一种4-甲基-7H-吡咯并[2,3-d]嘧啶的合成方法 |
| WO2022153161A1 (en) | 2021-01-14 | 2022-07-21 | Pfizer Inc. | Treatment of cancer using a prmt5 inhibitor |
| US12071439B2 (en) | 2021-07-12 | 2024-08-27 | Incyte Corporation | Process and intermediates for preparing a JAK inhibitor |
| WO2023017152A1 (en) * | 2021-08-13 | 2023-02-16 | Albert-Ludwigs-Universität Freiburg | Specific small molecule inhibitors that block kmt9 methyltransferase activity and function |
| WO2024170488A1 (en) | 2023-02-13 | 2024-08-22 | Astrazeneca Ab | Prmt5 inhibitor for use in cancer therapy |
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| US5795977A (en) * | 1989-09-15 | 1998-08-18 | Metabasis Therapeutics, Inc. | Water soluble adenosine kinase inhibitors |
| US5864033A (en) * | 1989-09-15 | 1999-01-26 | Metabasis Therapeutics, Inc. | Adenosine kinase inhibitors |
| US5646128A (en) * | 1989-09-15 | 1997-07-08 | Gensia, Inc. | Methods for treating adenosine kinase related conditions |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| GB9518953D0 (en) | 1995-09-15 | 1995-11-15 | Pfizer Ltd | Pharmaceutical formulations |
| WO2000035298A1 (en) | 1996-11-27 | 2000-06-22 | Wm. Wrigley Jr. Company | Chewing gum containing medicament active agents |
| GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| GB9813554D0 (en) * | 1998-06-23 | 1998-08-19 | Glaxo Group Ltd | Chemical compounds |
| US6831069B2 (en) * | 1999-08-27 | 2004-12-14 | Ribapharm Inc. | Pyrrolo[2,3-d]pyrimidine nucleoside analogs |
| US7022681B2 (en) * | 2002-08-15 | 2006-04-04 | Cv Therapeutics, Inc. | Partial and full agonists of A1 adenosine receptors |
| EP2408306A4 (en) * | 2009-03-20 | 2012-11-07 | Alios Biopharma Inc | SUBSTITUTED NUCLEOSIDE AND NUCLEOTIDE ANALOGUES |
| US20120077814A1 (en) | 2010-09-10 | 2012-03-29 | Zhong Wang | Sulfonamide, sulfamate, and sulfamothioate derivatives |
| EP2731434A4 (en) * | 2011-07-13 | 2014-12-31 | Merck Sharp & Dohme | 5'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHOD FOR THEIR USE FOR THE TREATMENT OF VIRUS DISEASES |
| US8575119B2 (en) * | 2011-09-23 | 2013-11-05 | Enanta Pharmaceuticals, Inc. | 2′-chloroacetylenyl substituted nucleoside derivatives |
| WO2015200680A2 (en) * | 2014-06-25 | 2015-12-30 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| AR104326A1 (es) * | 2015-05-04 | 2017-07-12 | Lilly Co Eli | Compuestos nucleósidos 5-sustituidos |
| JP2018523665A (ja) * | 2015-08-06 | 2018-08-23 | キメリックス インコーポレイテッド | 抗ウイルス剤として有用なピロロピリミジンヌクレオシドおよびその類縁体 |
-
2016
- 2016-02-15 CN CN201680011823.1A patent/CN107278205A/zh active Pending
- 2016-02-15 BR BR112017017396A patent/BR112017017396A2/pt not_active Application Discontinuation
- 2016-02-15 CU CUP2017000105A patent/CU20170105A7/xx unknown
- 2016-02-15 UA UAA201708102A patent/UA118315C2/uk unknown
- 2016-02-15 EA EA201791563A patent/EA031895B1/ru not_active IP Right Cessation
- 2016-02-15 PE PE2017001447A patent/PE20171449A1/es unknown
- 2016-02-15 KR KR1020177026762A patent/KR20170119705A/ko not_active Ceased
- 2016-02-15 WO PCT/IB2016/050803 patent/WO2016135582A1/en not_active Ceased
- 2016-02-15 TN TNP/2017/000357A patent/TN2017000357A1/en unknown
- 2016-02-15 CR CR20170384A patent/CR20170384A/es unknown
- 2016-02-15 MX MX2017010844A patent/MX2017010844A/es unknown
- 2016-02-15 JP JP2017544584A patent/JP6584521B2/ja not_active Expired - Fee Related
- 2016-02-15 EP EP16707209.9A patent/EP3262057B1/en active Active
- 2016-02-15 AU AU2016225133A patent/AU2016225133B2/en not_active Ceased
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- 2016-02-17 US US15/045,679 patent/US10428104B2/en active Active
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- 2016-02-22 UY UY0001036564A patent/UY36564A/es not_active Application Discontinuation
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2017
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- 2017-07-28 NI NI201700095A patent/NI201700095A/es unknown
- 2017-08-08 PH PH12017501413A patent/PH12017501413A1/en unknown
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2018
- 2018-12-11 AU AU2018278842A patent/AU2018278842A1/en not_active Abandoned
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