MD4592B1 - Derivaţi de benzimidazol ca inhibitori ai bromodomeniului - Google Patents
Derivaţi de benzimidazol ca inhibitori ai bromodomeniului Download PDFInfo
- Publication number
- MD4592B1 MD4592B1 MDA20150121A MD20150121A MD4592B1 MD 4592 B1 MD4592 B1 MD 4592B1 MD A20150121 A MDA20150121 A MD A20150121A MD 20150121 A MD20150121 A MD 20150121A MD 4592 B1 MD4592 B1 MD 4592B1
- Authority
- MD
- Moldova
- Prior art keywords
- benzimidazole derivatives
- compounds
- bromodomain inhibitors
- bromodomain
- inhibitors
- Prior art date
Links
- 102000001805 Bromodomains Human genes 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 108050009021 Bromodomains Proteins 0.000 title 1
- 229940058303 antinematodal benzimidazole derivative Drugs 0.000 title 1
- 125000003785 benzimidazolyl group Chemical class N1=C(NC2=C1C=CC=C2)* 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 abstract 2
- 101710126815 Bromodomain-containing protein 4 Proteins 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 108091005575 Bromodomain-containing proteins Proteins 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Invenţia se referă la compuşi chimici care pot acţiona ca inhibitori sau care altfel pot modula activitatea proteinei conţinând bromodomeniu, inclusiv a proteinei conţinând bromodomeniul 4 (BRD4), precum şi la compoziţii şi formulări care conţin astfel de compuşi şi la utilizarea unor astfel de compuşi. Compuşii sunt prezentaţi de formula (I)(I)în care R1a, R1b, R2a, R2b, R3, R4a, R4b şi R5 sunt descrişi în prezentul document.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361821612P | 2013-05-09 | 2013-05-09 | |
| US201361826912P | 2013-05-23 | 2013-05-23 | |
| US201361860229P | 2013-07-30 | 2013-07-30 | |
| US201461951347P | 2014-03-11 | 2014-03-11 | |
| PCT/US2014/037344 WO2014182929A1 (en) | 2013-05-09 | 2014-05-08 | Benzimidazole derivatives as bromodomain inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MD20150121A2 MD20150121A2 (ro) | 2016-05-31 |
| MD4592B1 true MD4592B1 (ro) | 2018-09-30 |
Family
ID=50897952
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MDA20150121A MD4592B1 (ro) | 2013-05-09 | 2014-05-08 | Derivaţi de benzimidazol ca inhibitori ai bromodomeniului |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US20160075695A1 (ro) |
| EP (1) | EP2994469B1 (ro) |
| JP (1) | JP6049942B2 (ro) |
| KR (1) | KR101761049B1 (ro) |
| CN (1) | CN105324379B (ro) |
| AP (1) | AP2015008869A0 (ro) |
| AR (1) | AR096246A1 (ro) |
| AU (1) | AU2014262622B2 (ro) |
| BR (1) | BR112015028017A2 (ro) |
| CA (1) | CA2911408C (ro) |
| CL (1) | CL2015003280A1 (ro) |
| CR (1) | CR20150639A (ro) |
| EA (1) | EA029091B1 (ro) |
| ES (1) | ES2710120T3 (ro) |
| MD (1) | MD4592B1 (ro) |
| MX (1) | MX2015015478A (ro) |
| NZ (1) | NZ713718A (ro) |
| PE (1) | PE20160029A1 (ro) |
| PH (1) | PH12015502534A1 (ro) |
| PT (1) | PT2994469T (ro) |
| SG (1) | SG11201509220XA (ro) |
| TW (1) | TWI527811B (ro) |
| UA (1) | UA112618C2 (ro) |
| UY (1) | UY35559A (ro) |
| WO (1) | WO2014182929A1 (ro) |
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| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| CA2895905A1 (en) | 2012-12-21 | 2014-06-26 | Zenith Epigenetics Corp. | Novel heterocyclic compounds as bromodomain inhibitors |
| MX366703B (es) | 2013-03-15 | 2019-07-22 | Incyte Holdings Corp | Heterociclos tricíclicos como inhibidores de la proteína bet. |
| WO2015004533A2 (en) * | 2013-06-21 | 2015-01-15 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| PL3010503T3 (pl) | 2013-06-21 | 2020-08-24 | Zenith Epigenetics Ltd. | Nowe bicykliczne inhibitory bromodomen |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| EP3027604B1 (en) | 2013-07-31 | 2019-02-20 | Zenith Epigenetics Ltd. | Novel quinazolinones as bromodomain inhibitors |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| KR102702503B1 (ko) | 2014-04-23 | 2024-09-05 | 인사이트 홀딩스 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
| EP3177604A1 (en) * | 2014-08-05 | 2017-06-14 | Bristol-Myers Squibb Company | Heterocyclic kinase inhibitors |
| WO2016044130A1 (en) | 2014-09-15 | 2016-03-24 | Incyte Corporation | Tricyclic heterocycles for use as bet protein inhibitors |
| EP3227280B1 (en) | 2014-12-01 | 2019-04-24 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| CN107207474B (zh) | 2014-12-11 | 2021-05-07 | 恒翼生物医药科技(上海)有限公司 | 被取代的杂环作为溴结构域抑制剂 |
| WO2016097870A1 (en) * | 2014-12-17 | 2016-06-23 | Zenith Epigenetics Corp. | Substituted bicyclic compounds as bromodomain inhibitors |
| US10231953B2 (en) * | 2014-12-17 | 2019-03-19 | Zenith Epigenetics Ltd. | Inhibitors of bromodomains |
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| EP3298005B1 (en) | 2015-05-21 | 2024-01-24 | The Regents of The University of California | Anti-cancer compounds |
| CN108137585B (zh) * | 2015-09-21 | 2021-10-22 | 普莱希科公司 | 杂环化合物及其应用 |
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| US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
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| GB201617630D0 (en) | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
| GB201617627D0 (en) * | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
| JP7171557B2 (ja) | 2016-10-27 | 2022-11-15 | セルジーン クオンティセル リサーチ，インク． | ブロモドメインおよびエクストラ末端タンパク質阻害剤を含む組合せ医薬 |
| WO2018085069A1 (en) * | 2016-11-03 | 2018-05-11 | Gilead Sciences, Inc. | Combination of a bcl-2 inhibitor and a bromodomain inhibitor for treating cancer |
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| US20180153867A1 (en) * | 2016-12-06 | 2018-06-07 | Gilead Sciences, Inc. | Treatment of prostate cancer by concomitant administration of a bromodomain inhibitor and a second agent |
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2014
- 2014-05-07 TW TW103116235A patent/TWI527811B/zh active
- 2014-05-08 AP AP2015008869A patent/AP2015008869A0/xx unknown
- 2014-05-08 AU AU2014262622A patent/AU2014262622B2/en active Active
- 2014-05-08 MX MX2015015478A patent/MX2015015478A/es unknown
- 2014-05-08 PT PT14729182T patent/PT2994469T/pt unknown
- 2014-05-08 PE PE2015002375A patent/PE20160029A1/es not_active Application Discontinuation
- 2014-05-08 CN CN201480035623.0A patent/CN105324379B/zh active Active
- 2014-05-08 ES ES14729182T patent/ES2710120T3/es active Active
- 2014-05-08 EP EP14729182.7A patent/EP2994469B1/en active Active
- 2014-05-08 SG SG11201509220XA patent/SG11201509220XA/en unknown
- 2014-05-08 JP JP2016513078A patent/JP6049942B2/ja active Active
- 2014-05-08 NZ NZ713718A patent/NZ713718A/en not_active IP Right Cessation
- 2014-05-08 CA CA2911408A patent/CA2911408C/en active Active
- 2014-05-08 BR BR112015028017A patent/BR112015028017A2/pt not_active Application Discontinuation
- 2014-05-08 KR KR1020157034918A patent/KR101761049B1/ko active Active
- 2014-05-08 MD MDA20150121A patent/MD4592B1/ro not_active IP Right Cessation
- 2014-05-08 WO PCT/US2014/037344 patent/WO2014182929A1/en not_active Ceased
- 2014-05-08 US US14/787,374 patent/US20160075695A1/en not_active Abandoned
- 2014-05-08 EA EA201591965A patent/EA029091B1/ru not_active IP Right Cessation
- 2014-05-08 US US14/273,147 patent/US9458145B2/en active Active
- 2014-05-09 AR ARP140101893A patent/AR096246A1/es unknown
- 2014-05-09 UY UY0001035559A patent/UY35559A/es not_active Application Discontinuation
- 2014-08-05 UA UAA201510960A patent/UA112618C2/uk unknown
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2015
- 2015-11-05 PH PH12015502534A patent/PH12015502534A1/en unknown
- 2015-11-09 CL CL2015003280A patent/CL2015003280A1/es unknown
- 2015-12-04 CR CR20150639A patent/CR20150639A/es unknown
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2016
- 2016-08-17 US US15/239,422 patent/US10017501B2/en active Active
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2018
- 2018-06-06 US US16/001,832 patent/US20180282316A1/en not_active Abandoned
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| KA4A | Patent for invention lapsed due to non-payment of fees (with right of restoration) |