PE20160029A1 - Derivados de benzimidazol como inhibidores de bromodominio - Google Patents
Derivados de benzimidazol como inhibidores de bromodominioInfo
- Publication number
- PE20160029A1 PE20160029A1 PE2015002375A PE2015002375A PE20160029A1 PE 20160029 A1 PE20160029 A1 PE 20160029A1 PE 2015002375 A PE2015002375 A PE 2015002375A PE 2015002375 A PE2015002375 A PE 2015002375A PE 20160029 A1 PE20160029 A1 PE 20160029A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- inhibitors
- bromodominium
- benzimidazole derivatives
- dimethylisozaxol
- Prior art date
Links
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
La presente invencion se relaciona con compuestos quimicos que pueden actuar como inhibidores, o modular de alguna otra forma, la actividad de una proteina que contiene bromodominio, incluyendo de una proteina 4 que contiene bromodominio (BRD4) y con composiciones y formulaciones que contienen dichos compuestos, asi como metodos para realizar dichos compuestos. Los compuestos incluyen compuestos de Formula (I), en donde: R1a y R1b son alquilo C1-6, etc. R2a y R2b son H o halo, R3 es -C(O) ORA, etc. R4a y R4b es hidrogeno, etc. R5 es -C(O) ORA, etc. Ra es H, alquilo C1-10, etc. Compuestos preferidos son: N-Ciclopentil-2-(ciclopropilmetilamino)-6-(3,5-dimetilisozaxol-4-il)-1H-benzo[d] imidazol-4-sulfonamida; N- Ciclopentil-6-(3,5- dimetilisozaxol-4-il)-2-(3-metoxipropilamino)-1H-benzo[d] imidazol-4-sulfonamida
Applications Claiming Priority (4)
| 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20160029A1 true PE20160029A1 (es) | 2016-02-14 |
Family
ID=50897952
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015002375A PE20160029A1 (es) | 2013-05-09 | 2014-05-08 | Derivados de benzimidazol como inhibidores de bromodominio |
Country Status (26)
| Country | Link |
|---|---|
| US (4) | US20160075695A1 (es) |
| EP (1) | EP2994469B1 (es) |
| JP (1) | JP6049942B2 (es) |
| KR (1) | KR101761049B1 (es) |
| CN (1) | CN105324379B (es) |
| AP (1) | AP2015008869A0 (es) |
| AR (1) | AR096246A1 (es) |
| AU (1) | AU2014262622B2 (es) |
| BR (1) | BR112015028017A2 (es) |
| CA (1) | CA2911408C (es) |
| CL (1) | CL2015003280A1 (es) |
| CR (1) | CR20150639A (es) |
| EA (1) | EA029091B1 (es) |
| ES (1) | ES2710120T3 (es) |
| HK (2) | HK1219278A1 (es) |
| MD (1) | MD4592B1 (es) |
| MX (1) | MX2015015478A (es) |
| NZ (1) | NZ713718A (es) |
| PE (1) | PE20160029A1 (es) |
| PH (1) | PH12015502534A1 (es) |
| PT (1) | PT2994469T (es) |
| SG (1) | SG11201509220XA (es) |
| TW (1) | TWI527811B (es) |
| UA (1) | UA112618C2 (es) |
| UY (1) | UY35559A (es) |
| WO (1) | WO2014182929A1 (es) |
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| JP2016507496A (ja) | 2012-12-21 | 2016-03-10 | ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． | ブロモドメイン阻害剤としての新規複素環式化合物 |
| EP2970282B1 (en) | 2013-03-15 | 2019-08-21 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| CN105407888B (zh) | 2013-06-21 | 2019-05-21 | 齐尼思表观遗传学有限公司 | 新双环溴结构域抑制剂 |
| EP3010918B1 (en) * | 2013-06-21 | 2018-08-15 | Zenith Epigenetics Ltd. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| AR096837A1 (es) | 2013-07-08 | 2016-02-03 | Incyte Corp | Heterociclos tricíclicos como inhibidores de proteínas bet |
| US9855271B2 (en) | 2013-07-31 | 2018-01-02 | Zenith Epigenetics Ltd. | Quinazolinones as bromodomain inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| TWI735002B (zh) | 2014-04-23 | 2021-08-01 | 美商英塞特公司 | 作為BET蛋白抑制劑之1H-吡咯并[2,3-c]吡啶-7(6H)-酮及吡唑并[3,4-c]吡啶-7(6H)-酮 |
| EP3177604A1 (en) * | 2014-08-05 | 2017-06-14 | Bristol-Myers Squibb Company | Heterocyclic kinase inhibitors |
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| CA2966298A1 (en) | 2014-12-01 | 2016-06-09 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| US10179125B2 (en) | 2014-12-01 | 2019-01-15 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| US10292968B2 (en) | 2014-12-11 | 2019-05-21 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
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| WO2016097870A1 (en) * | 2014-12-17 | 2016-06-23 | Zenith Epigenetics Corp. | Substituted bicyclic compounds as bromodomain inhibitors |
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-
2014
- 2014-05-07 TW TW103116235A patent/TWI527811B/zh active
- 2014-05-08 WO PCT/US2014/037344 patent/WO2014182929A1/en active Application Filing
- 2014-05-08 AP AP2015008869A patent/AP2015008869A0/xx unknown
- 2014-05-08 MX MX2015015478A patent/MX2015015478A/es unknown
- 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 KR KR1020157034918A patent/KR101761049B1/ko active IP Right Grant
- 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 PT PT14729182T patent/PT2994469T/pt unknown
- 2014-05-08 BR BR112015028017A patent/BR112015028017A2/pt not_active Application Discontinuation
- 2014-05-08 JP JP2016513078A patent/JP6049942B2/ja active Active
- 2014-05-08 US US14/273,147 patent/US9458145B2/en active Active
- 2014-05-08 PE PE2015002375A patent/PE20160029A1/es not_active Application Discontinuation
- 2014-05-08 EP EP14729182.7A patent/EP2994469B1/en active Active
- 2014-05-08 ES ES14729182T patent/ES2710120T3/es active Active
- 2014-05-08 AU AU2014262622A patent/AU2014262622B2/en active Active
- 2014-05-08 MD MDA20150121A patent/MD4592B1/ro not_active IP Right Cessation
- 2014-05-08 CN CN201480035623.0A patent/CN105324379B/zh active Active
- 2014-05-08 SG SG11201509220XA patent/SG11201509220XA/en unknown
- 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
- 2016-06-24 HK HK16107380.5A patent/HK1219278A1/zh not_active IP Right Cessation
- 2016-08-17 US US15/239,422 patent/US10017501B2/en active Active
- 2016-09-05 HK HK16110539.9A patent/HK1222646A1/zh unknown
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2018
- 2018-06-06 US US16/001,832 patent/US20180282316A1/en not_active Abandoned
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