JP7026787B2 - ヒストン脱アセチル化酵素１および／または２（ｈｄａｃ１－２）の選択的阻害剤としての新規なヘテロアリールアミド誘導体 - Google Patents
ヒストン脱アセチル化酵素１および／または２（ｈｄａｃ１－２）の選択的阻害剤としての新規なヘテロアリールアミド誘導体 Download PDFInfo
- Publication number
- JP7026787B2 JP7026787B2 JP2020523052A JP2020523052A JP7026787B2 JP 7026787 B2 JP7026787 B2 JP 7026787B2 JP 2020523052 A JP2020523052 A JP 2020523052A JP 2020523052 A JP2020523052 A JP 2020523052A JP 7026787 B2 JP7026787 B2 JP 7026787B2
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- JP
- Japan
- Prior art keywords
- amino
- group
- fluorophenyl
- disease
- nicotinamide
- 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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Links
- 0 *IC(N=C(C([N+]([O-])=O)=CI)N)=* Chemical compound *IC(N=C(C([N+]([O-])=O)=CI)N)=* 0.000 description 1
- LFRLASKPBYWCLZ-UHFFFAOYSA-N CC1(C=CC(c(nc2NC(c3cnc(C4CC4)cc3)=O)ccc2[N+]([O-])=O)=CC1)F Chemical compound CC1(C=CC(c(nc2NC(c3cnc(C4CC4)cc3)=O)ccc2[N+]([O-])=O)=CC1)F LFRLASKPBYWCLZ-UHFFFAOYSA-N 0.000 description 1
- PYVZAFAYVRKMEG-UHFFFAOYSA-N CN1CCN(CCNc(cc2)ncc2C(Nc(nc(cc2)-c(cc3)ccc3F)c2N)=O)CC1 Chemical compound CN1CCN(CCNc(cc2)ncc2C(Nc(nc(cc2)-c(cc3)ccc3F)c2N)=O)CC1 PYVZAFAYVRKMEG-UHFFFAOYSA-N 0.000 description 1
- JKLQYXBXZQZLJM-UHFFFAOYSA-N CN1CCN(CCNc(nc2)ccc2C(Nc(nc(cc2)-c(cc3)ccc3F)c2[N+]([O-])=O)=O)CC1 Chemical compound CN1CCN(CCNc(nc2)ccc2C(Nc(nc(cc2)-c(cc3)ccc3F)c2[N+]([O-])=O)=O)CC1 JKLQYXBXZQZLJM-UHFFFAOYSA-N 0.000 description 1
- ZZTPXXDOWPKSMC-UHFFFAOYSA-N Nc(cc1)c(NC(c2cnc(NC3CC3)nc2)=O)nc1-c1ccccc1 Chemical compound Nc(cc1)c(NC(c2cnc(NC3CC3)nc2)=O)nc1-c1ccccc1 ZZTPXXDOWPKSMC-UHFFFAOYSA-N 0.000 description 1
- KHEIHESTTQFPKT-UHFFFAOYSA-N Nc1ccc(-c(cc2)ccc2F)nc1NC(c1ccc(C2CC2)nc1)=O Chemical compound Nc1ccc(-c(cc2)ccc2F)nc1NC(c1ccc(C2CC2)nc1)=O KHEIHESTTQFPKT-UHFFFAOYSA-N 0.000 description 1
- GZGZSOYZLZNTMB-UHFFFAOYSA-N Nc1nc(-c(cc2)ccc2F)ccc1[N+]([O-])=O Chemical compound Nc1nc(-c(cc2)ccc2F)ccc1[N+]([O-])=O GZGZSOYZLZNTMB-UHFFFAOYSA-N 0.000 description 1
- AZQLYGCISPLJER-UHFFFAOYSA-N OC(c1cnc(C2CC2)cc1)=O Chemical compound OC(c1cnc(C2CC2)cc1)=O AZQLYGCISPLJER-UHFFFAOYSA-N 0.000 description 1
- DFAZFUMIFHJGKL-UHFFFAOYSA-N [O-][N+](c(cc1)c(NC(c(cn2)ccc2Cl)=O)nc1-c(cc1)ccc1F)=O Chemical compound [O-][N+](c(cc1)c(NC(c(cn2)ccc2Cl)=O)nc1-c(cc1)ccc1F)=O DFAZFUMIFHJGKL-UHFFFAOYSA-N 0.000 description 1
- KDTYRKYOLSDHAZ-UHFFFAOYSA-N [O-][N+](c(cc1)c(NC(c(cn2)cnc2Cl)=O)nc1-c1ccccc1)=O Chemical compound [O-][N+](c(cc1)c(NC(c(cn2)cnc2Cl)=O)nc1-c1ccccc1)=O KDTYRKYOLSDHAZ-UHFFFAOYSA-N 0.000 description 1
- JCTXEGAEDFBDFM-UHFFFAOYSA-N [O-][N+](c(cc1)c(NC(c2c[nH]nc2)=O)nc1-c1ccccc1)=O Chemical compound [O-][N+](c(cc1)c(NC(c2c[nH]nc2)=O)nc1-c1ccccc1)=O JCTXEGAEDFBDFM-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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17382447 | 2017-07-10 | ||
| EP17382447.5 | 2017-07-10 | ||
| PCT/ES2018/070491 WO2019012172A1 (es) | 2017-07-10 | 2018-07-09 | Nuevos derivados heteroaryl amida como inhibidores selectivos de histona deacetilasa 1 y 2 (hdac1/2) |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020527173A JP2020527173A (ja) | 2020-09-03 |
| JP2020527173A5 JP2020527173A5 (https=) | 2021-04-15 |
| JP7026787B2 true JP7026787B2 (ja) | 2022-02-28 |
Family
ID=59315557
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020523052A Active JP7026787B2 (ja) | 2017-07-10 | 2018-07-09 | ヒストン脱アセチル化酵素１および／または２（ｈｄａｃ１－２）の選択的阻害剤としての新規なヘテロアリールアミド誘導体 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US11241428B2 (https=) |
| EP (1) | EP3653620B9 (https=) |
| JP (1) | JP7026787B2 (https=) |
| KR (1) | KR102574135B1 (https=) |
| CN (1) | CN111051300B (https=) |
| AU (1) | AU2018300123B2 (https=) |
| CY (1) | CY1125343T1 (https=) |
| DK (1) | DK3653620T3 (https=) |
| EA (1) | EA039144B1 (https=) |
| ES (1) | ES2911040T3 (https=) |
| HR (1) | HRP20220472T1 (https=) |
| HU (1) | HUE058353T2 (https=) |
| LT (1) | LT3653620T (https=) |
| MX (1) | MX393982B (https=) |
| PL (1) | PL3653620T3 (https=) |
| PT (1) | PT3653620T (https=) |
| RS (1) | RS63156B1 (https=) |
| SI (1) | SI3653620T1 (https=) |
| SM (1) | SMT202200165T1 (https=) |
| WO (1) | WO2019012172A1 (https=) |
| ZA (1) | ZA202000727B (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7736678B2 (ja) | 2019-10-16 | 2025-09-09 | ケモセントリックス，インコーポレイティド | Ｐｄ－ｌ１疾患の処置のためのヘテロアリール－ビフェニルアミド |
| WO2021117759A1 (ja) * | 2019-12-10 | 2021-06-17 | 塩野義製薬株式会社 | 含窒素芳香族複素環式基を有するヒストン脱アセチル化酵素阻害剤 |
| CN114380751B (zh) * | 2020-03-30 | 2025-03-07 | 上海辉启生物医药科技有限公司 | 二氢化茚胺类衍生物、其制备方法和用途 |
| CA3240229A1 (en) | 2021-12-03 | 2023-06-08 | Tango Therapeutics, Inc. | Novel hdac inhibitors and therapeutic use thereof |
| CN114524799B (zh) * | 2022-03-11 | 2023-05-26 | 沈阳药科大学 | 一种hdac抑制剂及其制备方法和用途 |
| EP4306106A1 (en) * | 2022-07-14 | 2024-01-17 | Universidade de Aveiro | Nitro-containing compounds, compositions and uses thereof |
| CN115463215A (zh) * | 2022-07-26 | 2022-12-13 | 苏州大学 | Hdac9及其抑制剂的新用途 |
| CA3263654A1 (en) | 2022-08-05 | 2024-02-08 | Tango Therapeutics, Inc. | HISTONE DEACETYLASE INHIBITOR FOR THE TREATMENT OF CANCER WITH ALTERED STK11 ACTIVITY OR EXPRESSION |
| CN115304513A (zh) * | 2022-08-25 | 2022-11-08 | 湖北科技学院 | 具有抗炎活性的查尔酮类衍生物及其合成方法和应用 |
| CN115368277B (zh) * | 2022-09-15 | 2024-03-29 | 华侨大学 | 一种含异羟肟酸结构的联苯类化合物及其应用 |
| CN116199636A (zh) * | 2023-02-21 | 2023-06-02 | 杭州医学院 | 靶向肿瘤免疫激酶的2,4-二取代嘧啶衍生物、制备方法及其应用 |
Citations (6)
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| JP2009514859A (ja) | 2005-11-03 | 2009-04-09 | メルク エンド カムパニー インコーポレーテッド | 置換ニコチンアミド化合物 |
| JP2009535333A (ja) | 2006-04-26 | 2009-10-01 | メルク エンド カムパニー インコーポレーテッド | 二置換アニリン化合物 |
| JP2010531358A (ja) | 2007-06-27 | 2010-09-24 | メルク・シャープ・エンド・ドーム・コーポレイション | ヒストン脱アセチル化酵素阻害剤としてのピリジル及びピリミジニル誘導体 |
| JP2012529435A (ja) | 2009-06-08 | 2012-11-22 | ギリアード サイエンシーズ， インコーポレイテッド | アルカノイルアミノベンズアミドアニリンｈｄａｃインヒビター化合物 |
| WO2016057779A2 (en) | 2014-10-08 | 2016-04-14 | Acetylon Pharmaceuticals, Inc. | Induction of gata2 by hdac1 and hdac2 inhibitors |
| WO2017004522A1 (en) | 2015-07-02 | 2017-01-05 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibtors |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9603950B1 (en) | 2015-10-25 | 2017-03-28 | Institute Of Nuclear Energy Research | Compounds of imaging agent with HDAC inhibitor for treatment of Alzheimer syndrome and method of synthesis thereof |
-
2018
- 2018-07-09 ES ES18789777T patent/ES2911040T3/es active Active
- 2018-07-09 SI SI201830644T patent/SI3653620T1/sl unknown
- 2018-07-09 JP JP2020523052A patent/JP7026787B2/ja active Active
- 2018-07-09 AU AU2018300123A patent/AU2018300123B2/en active Active
- 2018-07-09 LT LTEPPCT/ES2018/070491T patent/LT3653620T/lt unknown
- 2018-07-09 PL PL18789777T patent/PL3653620T3/pl unknown
- 2018-07-09 RS RS20220320A patent/RS63156B1/sr unknown
- 2018-07-09 MX MX2020000349A patent/MX393982B/es unknown
- 2018-07-09 DK DK18789777.2T patent/DK3653620T3/da active
- 2018-07-09 US US16/629,457 patent/US11241428B2/en active Active
- 2018-07-09 PT PT187897772T patent/PT3653620T/pt unknown
- 2018-07-09 CN CN201880056722.5A patent/CN111051300B/zh active Active
- 2018-07-09 WO PCT/ES2018/070491 patent/WO2019012172A1/es not_active Ceased
- 2018-07-09 HR HRP20220472TT patent/HRP20220472T1/hr unknown
- 2018-07-09 EP EP18789777.2A patent/EP3653620B9/en active Active
- 2018-07-09 KR KR1020207003894A patent/KR102574135B1/ko active Active
- 2018-07-09 EA EA202090259A patent/EA039144B1/ru unknown
- 2018-07-09 HU HUE18789777A patent/HUE058353T2/hu unknown
- 2018-07-09 SM SM20220165T patent/SMT202200165T1/it unknown
-
2020
- 2020-02-04 ZA ZA2020/00727A patent/ZA202000727B/en unknown
-
2022
- 2022-04-15 CY CY20221100286T patent/CY1125343T1/el unknown
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009514859A (ja) | 2005-11-03 | 2009-04-09 | メルク エンド カムパニー インコーポレーテッド | 置換ニコチンアミド化合物 |
| JP2009535333A (ja) | 2006-04-26 | 2009-10-01 | メルク エンド カムパニー インコーポレーテッド | 二置換アニリン化合物 |
| JP2010531358A (ja) | 2007-06-27 | 2010-09-24 | メルク・シャープ・エンド・ドーム・コーポレイション | ヒストン脱アセチル化酵素阻害剤としてのピリジル及びピリミジニル誘導体 |
| JP2012529435A (ja) | 2009-06-08 | 2012-11-22 | ギリアード サイエンシーズ， インコーポレイテッド | アルカノイルアミノベンズアミドアニリンｈｄａｃインヒビター化合物 |
| WO2016057779A2 (en) | 2014-10-08 | 2016-04-14 | Acetylon Pharmaceuticals, Inc. | Induction of gata2 by hdac1 and hdac2 inhibitors |
| WO2017004522A1 (en) | 2015-07-02 | 2017-01-05 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibtors |
Non-Patent Citations (2)
| Title |
|---|
| BRESSI,J.C. et al.，Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides，Bioorganic & Medicinal Chemistry Letters，2010年，Vol.20, No.10，p.3142-3145 |
| METHOT,J.L. et al.，Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2)，Bioorganic & Medicinal Chemistry Letters，2008年，Vol.18, No.3，p.973-978 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3653620B9 (en) | 2022-03-23 |
| JP2020527173A (ja) | 2020-09-03 |
| AU2018300123A1 (en) | 2020-02-13 |
| CY1125343T1 (el) | 2024-12-13 |
| LT3653620T (lt) | 2022-05-10 |
| EP3653620B1 (en) | 2022-02-02 |
| US20200138808A1 (en) | 2020-05-07 |
| ZA202000727B (en) | 2022-07-27 |
| AU2018300123B2 (en) | 2022-03-17 |
| PL3653620T3 (pl) | 2022-06-20 |
| MX2020000349A (es) | 2020-08-17 |
| US11241428B2 (en) | 2022-02-08 |
| KR102574135B1 (ko) | 2023-09-01 |
| CN111051300A (zh) | 2020-04-21 |
| EP3653620A1 (en) | 2020-05-20 |
| WO2019012172A1 (es) | 2019-01-17 |
| ES2911040T3 (es) | 2022-05-17 |
| HRP20220472T1 (hr) | 2022-05-27 |
| HUE058353T2 (hu) | 2022-07-28 |
| SMT202200165T1 (it) | 2022-05-12 |
| DK3653620T3 (da) | 2022-03-28 |
| PT3653620T (pt) | 2022-04-22 |
| KR20200038473A (ko) | 2020-04-13 |
| MX393982B (es) | 2025-03-24 |
| EA202090259A1 (ru) | 2020-05-25 |
| BR112020000564A2 (pt) | 2020-07-21 |
| CN111051300B (zh) | 2022-12-23 |
| CA3069273A1 (en) | 2019-01-17 |
| RS63156B1 (sr) | 2022-05-31 |
| SI3653620T1 (sl) | 2022-05-31 |
| EA039144B1 (ru) | 2021-12-09 |
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