MD4531C1 - Derivaţi ai benzimidazolonei în calitate de inhibitori ai bromodomeniului - Google Patents
Derivaţi ai benzimidazolonei în calitate de inhibitori ai bromodomeniuluiInfo
- Publication number
- MD4531C1 MD4531C1 MDA20150104A MD20150104A MD4531C1 MD 4531 C1 MD4531 C1 MD 4531C1 MD A20150104 A MDA20150104 A MD A20150104A MD 20150104 A MD20150104 A MD 20150104A MD 4531 C1 MD4531 C1 MD 4531C1
- Authority
- MD
- Moldova
- Prior art keywords
- bromodomain inhibitors
- compounds
- benzimidazolone derivatives
- bromodomain
- inhibitors
- 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
- C07D413/14—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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (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
Invenţia se referă la compuşi chimici care pot acţiona ca inhibitori sau care în alt mod pot modula activitatea unei proteine conţinând un domeniu bromic, inclusiv a proteinei conţinând domeniul bromic 4 (BRD4), la compoziţii şi formulări ce conţin astfel de compuşi, precum şi la utilizarea unor astfel de compuşi. Compuşii sunt prezentaţi de formula (I)(I),în care semnificaţiile R1a, R1b, R2a, R2b, R3 şi X sunt dezvăluite în descriere şi revendicări.Revendicări: 17
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361805995P | 2013-03-28 | 2013-03-28 | |
US201361860230P | 2013-07-30 | 2013-07-30 | |
PCT/US2014/032031 WO2014160873A1 (en) | 2013-03-28 | 2014-03-27 | Benzimidazolone derivatives as bromodomain inhibitors |
Publications (3)
Publication Number | Publication Date |
---|---|
MD20150104A2 MD20150104A2 (ro) | 2016-02-29 |
MD4531B1 MD4531B1 (ro) | 2017-11-30 |
MD4531C1 true MD4531C1 (ro) | 2018-06-30 |
Family
ID=50897885
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MDA20150104A MD4531C1 (ro) | 2013-03-28 | 2014-03-27 | Derivaţi ai benzimidazolonei în calitate de inhibitori ai bromodomeniului |
Country Status (35)
Country | Link |
---|---|
US (2) | US9255089B2 (ro) |
EP (1) | EP2978759B1 (ro) |
JP (1) | JP6339175B2 (ro) |
KR (1) | KR101847698B1 (ro) |
CN (1) | CN105102453B (ro) |
AP (1) | AP2015008741A0 (ro) |
AU (1) | AU2014241152B2 (ro) |
BR (1) | BR112015024078A2 (ro) |
CA (1) | CA2907502C (ro) |
CL (1) | CL2015002871A1 (ro) |
CR (1) | CR20150515A (ro) |
CY (1) | CY1119165T1 (ro) |
DK (1) | DK2978759T3 (ro) |
EA (1) | EA029497B1 (ro) |
ES (1) | ES2626397T3 (ro) |
HK (1) | HK1220692A1 (ro) |
HR (1) | HRP20170750T1 (ro) |
HU (1) | HUE034772T2 (ro) |
IL (1) | IL241186A0 (ro) |
LT (1) | LT2978759T (ro) |
MD (1) | MD4531C1 (ro) |
MX (1) | MX2015013798A (ro) |
MY (1) | MY176634A (ro) |
NZ (1) | NZ711586A (ro) |
PE (1) | PE20151982A1 (ro) |
PH (1) | PH12015502246A1 (ro) |
PL (1) | PL2978759T3 (ro) |
PT (1) | PT2978759T (ro) |
RS (1) | RS56050B1 (ro) |
SG (1) | SG11201507926RA (ro) |
SI (1) | SI2978759T1 (ro) |
TW (1) | TWI530499B (ro) |
UY (1) | UY35516A (ro) |
WO (1) | WO2014160873A1 (ro) |
ZA (1) | ZA201506356B (ro) |
Families Citing this family (36)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8053440B2 (en) | 2007-02-01 | 2011-11-08 | Resverlogix Corporation | Compounds for the prevention and treatment of cardiovascular diseases |
BRPI1009315B8 (pt) | 2009-03-18 | 2021-05-25 | Resverlogix Corp | composto anti-flamatórios e suas composições farmacêuticas |
PL2773354T3 (pl) | 2011-11-01 | 2019-12-31 | Resverlogix Corp. | Doustna formulacja o natychmiastowym uwalnianiu dla podstawowych chinazolinów |
US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
CA2895905A1 (en) | 2012-12-21 | 2014-06-26 | Zenith Epigenetics Corp. | Novel heterocyclic compounds as bromodomain inhibitors |
UA119848C2 (uk) | 2013-03-15 | 2019-08-27 | Інсайт Холдинґс Корпорейшн | Трициклічні гетероцикли як інгібітори білків бет |
US9636328B2 (en) * | 2013-06-21 | 2017-05-02 | Zenith Epigenetics Ltd. | Substituted bicyclic compounds as bromodomain inhibitors |
BR112015031073B1 (pt) * | 2013-06-21 | 2022-11-29 | Zenith Epigenetics Ltd | Compostos inibidores bicíclicos de bromodomínio e composição farmacêutica contendo os referidos compostos |
US9290514B2 (en) | 2013-07-08 | 2016-03-22 | Incyte Holdings Corporation | Tricyclic heterocycles as BET protein inhibitors |
KR20160038008A (ko) | 2013-07-31 | 2016-04-06 | 제니쓰 에피제네틱스 코포레이션 | 브로모도메인 억제제로서 신규 퀴나졸리논 |
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 |
US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
EA039678B1 (ru) | 2014-04-23 | 2022-02-24 | Инсайт Корпорейшн | 1H-ПИРРОЛО[2,3-c]ПИРИДИН-7(6H)-ОНЫ И ПИРАЗОЛО[3,4-c]ПИРИДИН-7(6H)-ОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕЛКОВ BET |
TWI712603B (zh) | 2014-09-15 | 2020-12-11 | 美商英塞特公司 | 作為bet蛋白抑制劑之三環雜環 |
CA3000633C (en) | 2014-10-14 | 2023-10-03 | The Regents Of The University Of California | Use of cdk9 and brd4 inhibitors to inhibit inflammation |
US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
US10179125B2 (en) | 2014-12-01 | 2019-01-15 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
WO2016092375A1 (en) | 2014-12-11 | 2016-06-16 | Zenith Epigenetics Corp. | Substituted heterocycles as bromodomain inhibitors |
US10231953B2 (en) | 2014-12-17 | 2019-03-19 | Zenith Epigenetics Ltd. | Inhibitors of bromodomains |
US10111885B2 (en) | 2015-03-13 | 2018-10-30 | Resverlogix Corp. | Compositions and therapeutic methods for the treatment of complement-associated diseases |
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 |
US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
WO2017114843A1 (en) | 2015-12-29 | 2017-07-06 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Xanthine derivative inhibitors of bet proteins |
PT3472157T (pt) | 2016-06-20 | 2023-05-30 | Incyte Corp | Formas sólidas cristalinas de um inibidor bet |
WO2018097976A1 (en) * | 2016-11-22 | 2018-05-31 | Gilead Sciences, Inc. | Synthesis of a compound that modulates the activity of bromodomain-containing proteins |
US11180510B2 (en) | 2017-11-06 | 2021-11-23 | Centre National De La Recherche Scientifique | Xanthine derivatives and uses thereof as inhibitors of bromodomains of BET proteins |
AU2018391833A1 (en) | 2017-12-20 | 2020-07-30 | Betta Pharmaceuticals Co., Ltd | Compound functioning as bromodomain protein inhibitor, and composition |
CN113365699B (zh) * | 2019-02-02 | 2024-06-14 | 石药集团中奇制药技术(石家庄)有限公司 | 靶向泛素化降解brd4蛋白化合物及其制备方法和应用 |
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 |
US20220378923A1 (en) | 2019-09-30 | 2022-12-01 | Kyowa Kirin Co., Ltd. | Bet degrader |
US20230183215A1 (en) * | 2020-05-21 | 2023-06-15 | Stemsynergy Therapeutics, Inc. | Notch Inhibitors and Uses Thereof |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
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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 |
US6162804A (en) | 1997-09-26 | 2000-12-19 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
EP1620413A2 (en) | 2003-04-30 | 2006-02-01 | Cytokinetics, Inc. | Compounds, compositions, and methods |
GB0420719D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
AU2008287421A1 (en) | 2007-08-10 | 2009-02-19 | Glaxosmithkline Llc | Nitrogen containing bicyclic chemical entities for treating viral infections |
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 |
WO2012116440A1 (en) | 2011-03-03 | 2012-09-07 | Zalicus Pharmaceuticals Ltd. | Benzimidazole inhibitors of the sodium channel |
GB201114103D0 (en) * | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
BR112015031073B1 (pt) * | 2013-06-21 | 2022-11-29 | Zenith Epigenetics Ltd | Compostos inibidores bicíclicos de bromodomínio e composição farmacêutica contendo os referidos compostos |
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2014
- 2014-03-26 TW TW103111238A patent/TWI530499B/zh not_active IP Right Cessation
- 2014-03-27 PE PE2015002057A patent/PE20151982A1/es not_active Application Discontinuation
- 2014-03-27 MD MDA20150104A patent/MD4531C1/ro not_active IP Right Cessation
- 2014-03-27 PT PT147291140T patent/PT2978759T/pt unknown
- 2014-03-27 LT LTEP14729114.0T patent/LT2978759T/lt unknown
- 2014-03-27 CA CA2907502A patent/CA2907502C/en not_active Expired - Fee Related
- 2014-03-27 SG SG11201507926RA patent/SG11201507926RA/en unknown
- 2014-03-27 KR KR1020157030708A patent/KR101847698B1/ko active IP Right Grant
- 2014-03-27 PL PL14729114T patent/PL2978759T3/pl unknown
- 2014-03-27 EP EP14729114.0A patent/EP2978759B1/en active Active
- 2014-03-27 CN CN201480018645.6A patent/CN105102453B/zh active Active
- 2014-03-27 EA EA201591455A patent/EA029497B1/ru not_active IP Right Cessation
- 2014-03-27 DK DK14729114.0T patent/DK2978759T3/da active
- 2014-03-27 NZ NZ711586A patent/NZ711586A/en not_active IP Right Cessation
- 2014-03-27 BR BR112015024078A patent/BR112015024078A2/pt not_active Application Discontinuation
- 2014-03-27 US US14/227,736 patent/US9255089B2/en active Active
- 2014-03-27 JP JP2016505567A patent/JP6339175B2/ja not_active Expired - Fee Related
- 2014-03-27 MY MYPI2015002440A patent/MY176634A/en unknown
- 2014-03-27 ES ES14729114.0T patent/ES2626397T3/es active Active
- 2014-03-27 WO PCT/US2014/032031 patent/WO2014160873A1/en active Application Filing
- 2014-03-27 AP AP2015008741A patent/AP2015008741A0/xx unknown
- 2014-03-27 MX MX2015013798A patent/MX2015013798A/es unknown
- 2014-03-27 SI SI201430191A patent/SI2978759T1/sl unknown
- 2014-03-27 RS RS20170569A patent/RS56050B1/sr unknown
- 2014-03-27 HU HUE14729114A patent/HUE034772T2/en unknown
- 2014-03-27 AU AU2014241152A patent/AU2014241152B2/en not_active Ceased
- 2014-03-27 US US14/774,019 patent/US20160031868A1/en not_active Abandoned
- 2014-03-28 UY UY0001035516A patent/UY35516A/es not_active Application Discontinuation
-
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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2016
- 2016-07-25 HK HK16108876.4A patent/HK1220692A1/zh unknown
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2017
- 2017-05-19 HR HRP20170750TT patent/HRP20170750T1/hr unknown
- 2017-06-13 CY CY20171100624T patent/CY1119165T1/el unknown
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG4A | Patent for invention issued | ||
KA4A | Patent for invention lapsed due to non-payment of fees (with right of restoration) | ||
MM4A | Patent for invention definitely lapsed due to non-payment of fees |