PE20151982A1 - Derivados de bencimidazolona como inhibidores del bromodominio - Google Patents
Derivados de bencimidazolona como inhibidores del bromodominioInfo
- Publication number
- PE20151982A1 PE20151982A1 PE2015002057A PE2015002057A PE20151982A1 PE 20151982 A1 PE20151982 A1 PE 20151982A1 PE 2015002057 A PE2015002057 A PE 2015002057A PE 2015002057 A PE2015002057 A PE 2015002057A PE 20151982 A1 PE20151982 A1 PE 20151982A1
- Authority
- PE
- Peru
- Prior art keywords
- derivatives
- bromodominium
- benzhimidazolone
- inhibitors
- compounds
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 102000001805 Bromodomains Human genes 0.000 abstract 3
- 108050009021 Bromodomains Proteins 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000000203 mixture Substances 0.000 abstract 2
- 102000004169 proteins and genes Human genes 0.000 abstract 2
- 108090000623 proteins and genes Proteins 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 150000008641 benzimidazolones Chemical class 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 235000020824 obesity Nutrition 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
- C07D413/14—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se refiere al desarrollo de derivados de bencimidazolona de formula (I), donde R1a, R1b, R2a, R2b, R3, y X son aqui descritos. Estos compuestos son moduladores de la actividad de una proteina que contiene bromodominio, incluyendo la proteina 4 que contiene bromodominio (BRD4), por lo que son utiles en el tratamiento de cancer, diabetes, obesidad, entre otros. Tambien, se incluye las composiciones y formulaciones que contienen tales compuestos, y metodos de uso y fabricacion de tales compuestos
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361805995P | 2013-03-28 | 2013-03-28 | |
| US201361860230P | 2013-07-30 | 2013-07-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20151982A1 true PE20151982A1 (es) | 2016-01-28 |
Family
ID=50897885
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015002057A PE20151982A1 (es) | 2013-03-28 | 2014-03-27 | Derivados de bencimidazolona como inhibidores del bromodominio |
Country Status (35)
| Country | Link |
|---|---|
| US (2) | US9255089B2 (es) |
| EP (1) | EP2978759B1 (es) |
| JP (1) | JP6339175B2 (es) |
| KR (1) | KR101847698B1 (es) |
| CN (1) | CN105102453B (es) |
| AP (1) | AP2015008741A0 (es) |
| AU (1) | AU2014241152B2 (es) |
| BR (1) | BR112015024078A2 (es) |
| CA (1) | CA2907502C (es) |
| CL (1) | CL2015002871A1 (es) |
| CR (1) | CR20150515A (es) |
| CY (1) | CY1119165T1 (es) |
| DK (1) | DK2978759T3 (es) |
| EA (1) | EA029497B1 (es) |
| ES (1) | ES2626397T3 (es) |
| HR (1) | HRP20170750T1 (es) |
| HU (1) | HUE034772T2 (es) |
| IL (1) | IL241186A0 (es) |
| LT (1) | LT2978759T (es) |
| MD (1) | MD4531C1 (es) |
| MX (1) | MX2015013798A (es) |
| MY (1) | MY176634A (es) |
| NZ (1) | NZ711586A (es) |
| PE (1) | PE20151982A1 (es) |
| PH (1) | PH12015502246A1 (es) |
| PL (1) | PL2978759T3 (es) |
| PT (1) | PT2978759T (es) |
| RS (1) | RS56050B1 (es) |
| SG (1) | SG11201507926RA (es) |
| SI (1) | SI2978759T1 (es) |
| SM (1) | SMT201700249T1 (es) |
| TW (1) | TWI530499B (es) |
| UY (1) | UY35516A (es) |
| WO (1) | WO2014160873A1 (es) |
| ZA (1) | ZA201506356B (es) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2118074E (pt) | 2007-02-01 | 2014-03-20 | Resverlogix Corp | Compostos para a prevenção e tratamento de doenças cardiovasculares |
| NZ617779A (en) | 2009-03-18 | 2015-08-28 | Resverlogix Corp | Novel anti-inflammatory agents |
| PT2773354T (pt) | 2011-11-01 | 2019-07-17 | Resverlogix Corp | Formulações orais de libertação imediata para quinazolinonas substituídas |
| 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 |
| 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 |
| EA035469B1 (ru) | 2013-03-15 | 2020-06-22 | Инсайт Холдингс Корпорейшн | Трициклические гетероциклы как ингибиторы белков бэт |
| KR102307566B1 (ko) | 2013-06-21 | 2021-10-05 | 제니쓰 에피제네틱스 리미티드 | 신규한 바이사이클릭 브로모도메인 억제제 |
| CN105473581B (zh) * | 2013-06-21 | 2019-04-23 | 齐尼思表观遗传学有限公司 | 作为溴结构域抑制剂的新取代的双环化合物 |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| CA2919948C (en) | 2013-07-31 | 2020-07-21 | Zenith Epigenetics Corp. | Novel quinazolinones as bromodomain inhibitors |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein 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 |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| SMT202000133T1 (it) | 2014-04-23 | 2020-05-08 | Incyte Corp | 1h-pirrolo[2,3-c]piridin-7(6h)-oni e pirazolo[3,4-c]piridin-7(6h)-oni come inibitori di proteine bet |
| JP6599979B2 (ja) | 2014-09-15 | 2019-10-30 | インサイト・コーポレイション | Ｂｅｔタンパク質阻害剤として用いるための三環式複素環化合物 |
| CN107108512B (zh) * | 2014-10-10 | 2021-05-04 | 基因泰克公司 | 治疗性化合物及其用途 |
| US10300073B2 (en) | 2014-10-14 | 2019-05-28 | The Regents Of The University Of California | Use of CDK9 and BRD4 inhibitors to inhibit inflammation |
| US10179125B2 (en) | 2014-12-01 | 2019-01-15 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| HK1245246A1 (zh) | 2014-12-01 | 2018-08-24 | 恒翼生物医药科技(上海)有限公司 | 作为溴域抑制剂的取代吡啶酮 |
| WO2016092375A1 (en) | 2014-12-11 | 2016-06-16 | Zenith Epigenetics Corp. | Substituted heterocycles as bromodomain inhibitors |
| CN107406438B (zh) | 2014-12-17 | 2021-05-14 | 恒翼生物医药科技(上海)有限公司 | 溴结构域的抑制剂 |
| CN114984016A (zh) | 2015-03-13 | 2022-09-02 | 雷斯韦洛吉克斯公司 | 用于治疗补体相关疾病之组合物及治疗方法 |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| GB201504689D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| WO2016203335A1 (en) | 2015-06-18 | 2016-12-22 | Pfizer Inc. | Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors |
| WO2017075377A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| EP3397640B1 (en) | 2015-12-29 | 2021-08-04 | INSERM - Institut National de la Santé et de la Recherche Médicale | Xanthine derivative inhibitors of bet proteins |
| CN109715625B (zh) | 2016-06-20 | 2022-04-19 | 因赛特公司 | Bet抑制剂的结晶固体形式 |
| US20180179191A1 (en) * | 2016-11-22 | 2018-06-28 | Gilead Sciences, Inc. | Synthesis of a compound that modulates the activity of bromodomain-containing proteins |
| CA3081753A1 (en) | 2017-11-06 | 2019-05-09 | Centre National De La Recherche Scientifique | Xanthine derivatives and uses thereof as inhibitors of bromodomains of bet proteins |
| TWI713952B (zh) | 2017-12-20 | 2020-12-21 | 大陸商貝達藥業股份有限公司 | 作為溴結構域蛋白質抑制劑的化合物和組合物 |
| JP7394140B2 (ja) * | 2019-02-02 | 2023-12-07 | シーエスピーシー ゾンチー ファーマシューティカル テクノロジー（シージアチュアン）カンパニー，リミテッド | 標的ユビキチン化分解ｂｒｄ４タンパク質化合物、その調製方法および応用 |
| CN109912584B (zh) * | 2019-03-22 | 2021-08-13 | 中国药科大学 | 一种具有抗肿瘤活性的brd4蛋白抑制剂及其制备方法和应用 |
| CN114502534A (zh) | 2019-09-30 | 2022-05-13 | 协和麒麟株式会社 | Bet降解剂 |
| BR112022023559A2 (pt) * | 2020-05-21 | 2023-01-24 | Stemsynergy Therapeutics Inc | Inibidores de notch e seus usos |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CA3251059A1 (en) | 2022-05-02 | 2023-11-09 | The Board Of Trustees Of The Leland Stanford Junior University | Compositions, systems and methods for modulating a target gene |
| CN117821344B (zh) * | 2024-03-06 | 2024-07-26 | 江苏古道农业科技有限公司 | 一种草甘膦降解菌及其应用 |
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| US3845770A (en) * | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US4326525A (en) | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| US5364620A (en) * | 1983-12-22 | 1994-11-15 | Elan Corporation, Plc | Controlled absorption diltiazem formulation for once daily administration |
| US5023252A (en) * | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US4992445A (en) * | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| US5001139A (en) * | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4902514A (en) * | 1988-07-21 | 1990-02-20 | Alza Corporation | Dosage form for administering nilvadipine for treating cardiovascular symptoms |
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| GB0420719D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| CN101842098A (zh) | 2007-08-10 | 2010-09-22 | 基因实验室技术有限公司 | 用于治疗病毒感染的含氮的二环化学实体 |
| US20100204265A1 (en) | 2009-02-09 | 2010-08-12 | Genelabs Technologies, Inc. | Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| CA2828456C (en) | 2011-03-03 | 2021-05-04 | Zalicus Pharmaceuticals Ltd. | N-benzl-amino-carboxamide inhibitors of the sodium channel |
| GB201114103D0 (en) * | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| KR102307566B1 (ko) * | 2013-06-21 | 2021-10-05 | 제니쓰 에피제네틱스 리미티드 | 신규한 바이사이클릭 브로모도메인 억제제 |
-
2014
- 2014-03-26 TW TW103111238A patent/TWI530499B/zh not_active IP Right Cessation
- 2014-03-27 US US14/227,736 patent/US9255089B2/en active Active
- 2014-03-27 NZ NZ711586A patent/NZ711586A/en not_active IP Right Cessation
- 2014-03-27 EA EA201591455A patent/EA029497B1/ru not_active IP Right Cessation
- 2014-03-27 CA CA2907502A patent/CA2907502C/en not_active Expired - Fee Related
- 2014-03-27 MX MX2015013798A patent/MX2015013798A/es unknown
- 2014-03-27 DK DK14729114.0T patent/DK2978759T3/da active
- 2014-03-27 MD MDA20150104A patent/MD4531C1/ro not_active IP Right Cessation
- 2014-03-27 AP AP2015008741A patent/AP2015008741A0/xx unknown
- 2014-03-27 PL PL14729114T patent/PL2978759T3/pl unknown
- 2014-03-27 KR KR1020157030708A patent/KR101847698B1/ko not_active Expired - Fee Related
- 2014-03-27 SG SG11201507926RA patent/SG11201507926RA/en unknown
- 2014-03-27 PE PE2015002057A patent/PE20151982A1/es not_active Application Discontinuation
- 2014-03-27 CN CN201480018645.6A patent/CN105102453B/zh active Active
- 2014-03-27 LT LTEP14729114.0T patent/LT2978759T/lt unknown
- 2014-03-27 HU HUE14729114A patent/HUE034772T2/en unknown
- 2014-03-27 WO PCT/US2014/032031 patent/WO2014160873A1/en not_active Ceased
- 2014-03-27 SI SI201430191A patent/SI2978759T1/sl unknown
- 2014-03-27 HR HRP20170750TT patent/HRP20170750T1/hr unknown
- 2014-03-27 JP JP2016505567A patent/JP6339175B2/ja not_active Expired - Fee Related
- 2014-03-27 ES ES14729114.0T patent/ES2626397T3/es active Active
- 2014-03-27 PT PT147291140T patent/PT2978759T/pt unknown
- 2014-03-27 BR BR112015024078A patent/BR112015024078A2/pt not_active Application Discontinuation
- 2014-03-27 US US14/774,019 patent/US20160031868A1/en not_active Abandoned
- 2014-03-27 RS RS20170569A patent/RS56050B1/sr unknown
- 2014-03-27 AU AU2014241152A patent/AU2014241152B2/en not_active Ceased
- 2014-03-27 MY MYPI2015002440A patent/MY176634A/en unknown
- 2014-03-27 SM SM20170249T patent/SMT201700249T1/it unknown
- 2014-03-27 EP EP14729114.0A patent/EP2978759B1/en active Active
- 2014-03-28 UY UY0001035516A patent/UY35516A/es not_active Application Discontinuation
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2015
- 2015-08-31 ZA ZA2015/06356A patent/ZA201506356B/en unknown
- 2015-09-06 IL IL241186A patent/IL241186A0/en unknown
- 2015-09-24 PH PH12015502246A patent/PH12015502246A1/en unknown
- 2015-09-25 CL CL2015002871A patent/CL2015002871A1/es unknown
- 2015-10-02 CR CR20150515A patent/CR20150515A/es unknown
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2017
- 2017-06-13 CY CY20171100624T patent/CY1119165T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |