KR102677015B1 - Bet 억제제로서의 헤테로시클릭 화합물 - Google Patents
Bet 억제제로서의 헤테로시클릭 화합물 Download PDFInfo
- Publication number
- KR102677015B1 KR102677015B1 KR1020227003392A KR20227003392A KR102677015B1 KR 102677015 B1 KR102677015 B1 KR 102677015B1 KR 1020227003392 A KR1020227003392 A KR 1020227003392A KR 20227003392 A KR20227003392 A KR 20227003392A KR 102677015 B1 KR102677015 B1 KR 102677015B1
- Authority
- KR
- South Korea
- Prior art keywords
- formula
- iiia
- iia
- pharmaceutically acceptable
- compound
- 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.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962870020P | 2019-07-02 | 2019-07-02 | |
| US62/870,020 | 2019-07-02 | ||
| US202063017547P | 2020-04-29 | 2020-04-29 | |
| US63/017,547 | 2020-04-29 | ||
| PCT/US2020/040566 WO2021003310A1 (en) | 2019-07-02 | 2020-07-01 | Heterocyclic compounds as bet inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20220028072A KR20220028072A (ko) | 2022-03-08 |
| KR102677015B1 true KR102677015B1 (ko) | 2024-06-19 |
Family
ID=74065335
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020227003392A Active KR102677015B1 (ko) | 2019-07-02 | 2020-07-01 | Bet 억제제로서의 헤테로시클릭 화합물 |
Country Status (11)
| Country | Link |
|---|---|
| US (3) | US11584756B2 (https=) |
| EP (1) | EP3997070A4 (https=) |
| JP (1) | JP7465945B2 (https=) |
| KR (1) | KR102677015B1 (https=) |
| CN (1) | CN114286818B (https=) |
| AU (1) | AU2020299592A1 (https=) |
| CA (1) | CA3145827A1 (https=) |
| CL (1) | CL2021003513A1 (https=) |
| IL (1) | IL289439B2 (https=) |
| MX (1) | MX2022000050A (https=) |
| WO (1) | WO2021003310A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3828183A4 (en) * | 2018-07-25 | 2022-03-09 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | SULFOXIMINE COMPOUND AS BROMO-DOMAIN INHIBITOR AND PHARMACEUTICAL COMPOSITION AND MEDICAL USE THEREOF |
| US11192900B2 (en) | 2018-10-30 | 2021-12-07 | Nuvation Bio Inc. | Substituted 1,6-dihydropyridinones and 1,2-dihydroisoquinolinones as bet inhibitors |
| GB201905721D0 (en) | 2019-04-24 | 2019-06-05 | Univ Dundee | Compounds |
| KR102677015B1 (ko) * | 2019-07-02 | 2024-06-19 | 누베이션 바이오 인크. | Bet 억제제로서의 헤테로시클릭 화합물 |
| WO2021222466A1 (en) * | 2020-04-29 | 2021-11-04 | Nuvation Bio Inc. | Heterocyclic compounds as bet inhibitors |
| CA3224302A1 (en) | 2021-06-29 | 2023-01-05 | Tay Therapeutics Limited | Pyrrolopyridone derivatives useful in the treatment of cancer |
| CN116135858B (zh) * | 2021-11-16 | 2025-04-01 | 中国科学院广州生物医药与健康研究院 | 一种呋喃并吡啶酮类化合物及其应用 |
| JP2025502064A (ja) * | 2022-01-06 | 2025-01-24 | デザイン セラピューティクス，インク． | フリードライヒ運動失調症を治療するための化合物及び方法 |
| CN114907335A (zh) * | 2022-02-25 | 2022-08-16 | 陕西维世诺新材料有限公司 | 2-（苯并噻吩-2-基）苯并[d]惡唑衍生物、制备方法及应用 |
| CN115028646B (zh) * | 2022-05-31 | 2023-06-30 | 山东第一医科大学(山东省医学科学院) | 一种含氮杂环类化合物、制备方法及在抗肿瘤制剂中的应用 |
| WO2024138023A1 (en) * | 2022-12-22 | 2024-06-27 | Nuvation Bio Inc. | Combination treatment of cancers with a bet inhibitor |
| AU2024329991A1 (en) * | 2023-08-25 | 2026-03-05 | Nuvation Bio Inc. | Crystalline forms of a bet inhibitor |
| WO2025251167A1 (zh) * | 2024-06-03 | 2025-12-11 | 中国科学院广州生物医药与健康研究院 | 一类溴结构域抑制活性的化合物及其用途 |
Family Cites Families (49)
| Publication number | Priority date | Publication date | Assignee | Title |
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| IL118631A (en) | 1995-06-27 | 2002-05-23 | Tanabe Seiyaku Co | History of pyridazinone and processes for their preparation |
| WO2004022540A2 (en) * | 2002-09-06 | 2004-03-18 | Fujisawa Pharmaceutical Co., Ltd. | Pyridazinone and pyridone derivatives as adenosine antagonists |
| US7378423B2 (en) | 2004-06-11 | 2008-05-27 | Japan Tobacco Inc. | Pyrimidine compound and medical use thereof |
| EA015127B1 (ru) * | 2006-06-08 | 2011-06-30 | Эли Лилли Энд Компани | Антагонисты мсн-рецепторов |
| WO2009054952A2 (en) | 2007-10-22 | 2009-04-30 | Angion Biomedica Corp. | Small molecule inhibitors of parp activity |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| ES2625945T3 (es) | 2012-11-14 | 2017-07-21 | Glaxosmithkline Llc | Tieno[3,2-c]piridin-4(5H)-onas como inhibidores de bet |
| US9266891B2 (en) | 2012-11-16 | 2016-02-23 | Boehringer Ingelheim International Gmbh | Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors |
| EP2961747B1 (en) | 2013-02-27 | 2017-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| EP2970312B1 (en) | 2013-03-11 | 2017-11-15 | The Regents of The University of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| US9050346B2 (en) | 2013-03-11 | 2015-06-09 | Abbvie Inc. | Bromodomain inhibitors |
| UY35395A (es) | 2013-03-12 | 2014-10-31 | Abbvie Inc | Inhibidores de bromodominios tetracíclicos |
| HUE043568T2 (hu) | 2013-03-14 | 2019-08-28 | Glaxosmithkline Ip No 2 Ltd | 2,3-diszubsztituált 1-acil-4-amino-1,2,3,4-tetrahidrokinolin származékok és bromodomén inhibitorokkénti felhasználásuk |
| US9670221B2 (en) | 2013-03-14 | 2017-06-06 | Glaxosmithkline Intellectual Property (No. 2) Limited | Furopyridines as bromodomain inhibitors |
| SI3010503T1 (sl) | 2013-06-21 | 2020-07-31 | Zenith Epigenetics Ltd. | Novi biciklični inhibitorji bromodomene |
| WO2014206150A1 (en) | 2013-06-28 | 2014-12-31 | Abbvie Inc. | Bromodomain inhibitors |
| SG10201804471PA (en) * | 2013-10-18 | 2018-07-30 | Celgene Quanticel Research Inc | Bromodomain inhibitors |
| RU2720237C2 (ru) | 2013-11-18 | 2020-04-28 | Форма Терапеутикс, Инк. | Композиции, содержащие бензопиперазин, в качестве ингибиторов бромодоменов вет |
| CN110627770A (zh) | 2013-11-18 | 2019-12-31 | 福马疗法公司 | 作为bet溴域抑制剂的四氢喹啉组成物 |
| WO2015099107A1 (ja) | 2013-12-26 | 2015-07-02 | 塩野義製薬株式会社 | 含窒素６員環誘導体およびそれらを含有する医薬組成物 |
| HUE041546T2 (hu) | 2014-01-09 | 2019-05-28 | Orion Corp | Biciklusos heterociklusos származékvegyületek mint bromo doméninhibitorok |
| WO2015131005A1 (en) | 2014-02-28 | 2015-09-03 | The Regents Of The University Of Michigan | 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors |
| PL3134403T3 (pl) | 2014-04-23 | 2020-07-13 | Incyte Corporation | 1H-pirolo[2,3-c]pirydyn-7(6H)-ony i pirazolo[3,4-c]pirydyn-7(6H)-ony jako inhibitory białek BET |
| BR112017004580A2 (pt) | 2014-09-12 | 2018-01-23 | GlaxoSmithKline Intellectual Property | composto, composição farmacêutica, produto de combinação, uso de um composto ou sal farmaceuticamente aceitável, e, método de tratamento. |
| WO2016092375A1 (en) | 2014-12-11 | 2016-06-16 | Zenith Epigenetics Corp. | Substituted heterocycles as bromodomain inhibitors |
| EP3262045A1 (en) | 2015-02-27 | 2018-01-03 | The Regents of The University of Michigan | 9h-pyrimido [4,5-b]indoles as bet bromodomain inhibitors |
| AR104259A1 (es) | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| JP2018527293A (ja) | 2015-06-16 | 2018-09-20 | オリオン コーポレーション | ブロモドメイン阻害剤としてのスピロ［シクロブタン−１，３’−インドリン］−２’−オン誘導体 |
| ES2913048T3 (es) | 2015-09-21 | 2022-05-31 | Opna Immuno Oncology Sa | Compuestos heterocíclicos y usos de estos |
| CA2998545A1 (en) | 2015-09-22 | 2017-03-30 | Glaxosmithkline Intellectual Property (No.2) Limited | Pyridinone dicarboxamide for use as bromodomain inhibitors |
| EP3374350B1 (en) | 2015-11-09 | 2022-01-05 | Forge Therapeutics, Inc. | Hydroxypyridinone and hydroxypyrimidinone based compounds for treating bacterial infections |
| WO2017103670A1 (en) | 2015-12-14 | 2017-06-22 | Zenith Epigenetics Lid. | 1h-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridinyl heterocyclic bet bromodomain inhibitors |
| PT3442972T (pt) | 2016-04-15 | 2020-05-29 | Abbvie Inc | Inibidores de bromodomínio |
| EP3445750A4 (en) | 2016-04-18 | 2019-11-27 | Celgene Quanticel Research, Inc. | THERAPEUTIC COMPOUNDS |
| WO2017197056A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Bromodomain targeting degronimers for target protein degradation |
| WO2017223452A1 (en) | 2016-06-23 | 2017-12-28 | Dana-Farber Cancer Institute, Inc. | Degradation of bromodomain-containing protein 9 (brd9) by conjugation of brd9 inhibitors with e3 ligase ligand and methods of use |
| CN108069958A (zh) | 2016-11-10 | 2018-05-25 | 凯惠科技发展(上海)有限公司 | 一种含氮杂环类化合物、其制备方法、药物组合物及应用 |
| CN110167939B (zh) * | 2017-01-11 | 2021-12-31 | 江苏豪森药业集团有限公司 | 吡咯并[2,3-c]吡啶类衍生物、其制备方法及其在医药上的应用 |
| JP7840635B2 (ja) | 2017-12-20 | 2026-04-06 | 貝達薬業股▲ふん▼有限公司 | ブロモドメインタンパク質阻害剤である化合物、および組成物 |
| US11427593B2 (en) | 2018-01-16 | 2022-08-30 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Bromodomain inhibitor compound and use thereof |
| CN110041253B (zh) | 2018-01-17 | 2022-03-29 | 上海翰森生物医药科技有限公司 | 吡啶类n-氧化衍生物及其制备方法和应用 |
| EP3828183A4 (en) * | 2018-07-25 | 2022-03-09 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | SULFOXIMINE COMPOUND AS BROMO-DOMAIN INHIBITOR AND PHARMACEUTICAL COMPOSITION AND MEDICAL USE THEREOF |
| CN110964012B (zh) | 2018-09-29 | 2021-08-13 | 上海凌达生物医药有限公司 | 一类稠杂环联芳基苄醇类化合物、制备方法和用途 |
| US11192900B2 (en) | 2018-10-30 | 2021-12-07 | Nuvation Bio Inc. | Substituted 1,6-dihydropyridinones and 1,2-dihydroisoquinolinones as bet inhibitors |
| US20230065463A1 (en) | 2019-01-29 | 2023-03-02 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| WO2020187123A1 (zh) | 2019-03-17 | 2020-09-24 | 上海凌达生物医药有限公司 | 一类吡咯酰胺并吡啶酮类化合物、制备方法和用途 |
| WO2020253711A1 (zh) | 2019-06-17 | 2020-12-24 | 中国科学院上海药物研究所 | 一种吡咯并吡啶酮类化合物、其制备方法、其组合物和用途 |
| KR102677015B1 (ko) * | 2019-07-02 | 2024-06-19 | 누베이션 바이오 인크. | Bet 억제제로서의 헤테로시클릭 화합물 |
| WO2021222466A1 (en) | 2020-04-29 | 2021-11-04 | Nuvation Bio Inc. | Heterocyclic compounds as bet inhibitors |
-
2020
- 2020-07-01 KR KR1020227003392A patent/KR102677015B1/ko active Active
- 2020-07-01 MX MX2022000050A patent/MX2022000050A/es unknown
- 2020-07-01 JP JP2022500105A patent/JP7465945B2/ja active Active
- 2020-07-01 US US16/918,997 patent/US11584756B2/en active Active
- 2020-07-01 WO PCT/US2020/040566 patent/WO2021003310A1/en not_active Ceased
- 2020-07-01 CA CA3145827A patent/CA3145827A1/en active Pending
- 2020-07-01 IL IL289439A patent/IL289439B2/en unknown
- 2020-07-01 EP EP20834516.5A patent/EP3997070A4/en active Pending
- 2020-07-01 AU AU2020299592A patent/AU2020299592A1/en active Pending
- 2020-07-01 CN CN202080060057.4A patent/CN114286818B/zh active Active
-
2021
- 2021-12-27 CL CL2021003513A patent/CL2021003513A1/es unknown
-
2023
- 2023-01-09 US US18/152,049 patent/US20230339964A1/en not_active Abandoned
-
2024
- 2024-10-14 US US18/915,226 patent/US20250276978A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021003310A1 (en) | 2021-01-07 |
| CN114286818A (zh) | 2022-04-05 |
| EP3997070A4 (en) | 2023-07-26 |
| JP7465945B2 (ja) | 2024-04-11 |
| KR20220028072A (ko) | 2022-03-08 |
| JP2022538917A (ja) | 2022-09-06 |
| CA3145827A1 (en) | 2021-01-07 |
| IL289439B2 (en) | 2026-04-01 |
| CN114286818B (zh) | 2024-09-20 |
| AU2020299592A1 (en) | 2022-02-17 |
| IL289439B1 (en) | 2025-12-01 |
| IL289439A (en) | 2022-02-01 |
| MX2022000050A (es) | 2022-05-24 |
| US20230339964A1 (en) | 2023-10-26 |
| US11584756B2 (en) | 2023-02-21 |
| BR112021026668A2 (pt) | 2022-02-15 |
| US20250276978A1 (en) | 2025-09-04 |
| EP3997070A1 (en) | 2022-05-18 |
| US20210002293A1 (en) | 2021-01-07 |
| CL2021003513A1 (es) | 2022-10-28 |
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