BR112015022391A8 - inibidores de domínio bromo tetracíclico - Google Patents
inibidores de domínio bromo tetracíclico Download PDFInfo
- Publication number
- BR112015022391A8 BR112015022391A8 BR112015022391A BR112015022391A BR112015022391A8 BR 112015022391 A8 BR112015022391 A8 BR 112015022391A8 BR 112015022391 A BR112015022391 A BR 112015022391A BR 112015022391 A BR112015022391 A BR 112015022391A BR 112015022391 A8 BR112015022391 A8 BR 112015022391A8
- Authority
- BR
- Brazil
- Prior art keywords
- tetracyclic
- domain inhibitors
- bromine domain
- formula
- bromine
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/16—Peri-condensed 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
- C07D471/22—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 systems contains four or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/16—Masculine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- 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
- C07D471/12—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 three hetero rings
- C07D471/16—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
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)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Virology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Tropical Medicine & Parasitology (AREA)
- Oncology (AREA)
- AIDS & HIV (AREA)
- Endocrinology (AREA)
- Molecular Biology (AREA)
- Reproductive Health (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Hydrogenated Pyridines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
resumo inibidores de domínio bromo tetracíclico a presente invenção provê compostos da formula (i): (i) em que r1, r2, r6, y1, y2, y3, a1, a2, a3, e a4 apresentam qualquer um dos valores definidos no relatório descritivo e sais farmaceuticamente aceitáveis dos mesmos, que são úteis como agentes no tratamento de doenças e condições, inclu-indo doenças inflamatórias, câncer e aids. também são providas composições farmacêuticas compreendendo um ou mais compostos da fórmula (i).
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361777797P | 2013-03-12 | 2013-03-12 | |
| US61/777,797 | 2013-03-12 | ||
| US201461928779P | 2014-01-17 | 2014-01-17 | |
| US61/928,779 | 2014-01-17 | ||
| PCT/CN2014/000258 WO2014139324A1 (en) | 2013-03-12 | 2014-03-12 | Tetracyclic bromodomain inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BR112015022391A2 BR112015022391A2 (pt) | 2017-07-18 |
| BR112015022391A8 true BR112015022391A8 (pt) | 2019-11-26 |
| BR112015022391B1 BR112015022391B1 (pt) | 2021-12-21 |
Family
ID=51535867
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112015022391-5A BR112015022391B1 (pt) | 2013-03-12 | 2014-03-12 | Compostos inibidores do domínio bromo tetracíclico, composição farmacêutica que compreende os referidos compostos e usos terapêuticos dos mesmos |
Country Status (22)
| Country | Link |
|---|---|
| US (5) | US10035800B2 (pt) |
| EP (2) | EP2970330B1 (pt) |
| JP (2) | JP6419735B2 (pt) |
| KR (1) | KR102224992B1 (pt) |
| CN (2) | CN105026403B (pt) |
| AR (1) | AR095266A1 (pt) |
| AU (2) | AU2014231563A1 (pt) |
| BR (1) | BR112015022391B1 (pt) |
| CA (1) | CA2903910C (pt) |
| CR (1) | CR20150474A (pt) |
| DO (1) | DOP2015000216A (pt) |
| HK (1) | HK1217102A1 (pt) |
| IL (1) | IL241010B (pt) |
| MX (1) | MX363913B (pt) |
| PE (1) | PE20151788A1 (pt) |
| PH (1) | PH12015502004A1 (pt) |
| RU (1) | RU2015143192A (pt) |
| SG (1) | SG11201507402WA (pt) |
| TW (1) | TWI635087B (pt) |
| UY (1) | UY35395A (pt) |
| WO (1) | WO2014139324A1 (pt) |
| ZA (1) | ZA201506477B (pt) |
Families Citing this family (57)
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| AU2013276617B9 (en) | 2012-06-13 | 2018-03-29 | F. Hoffmann-La Roche Ag | New diazaspirocycloalkane and azaspirocycloalkane |
| RS59512B1 (sr) | 2012-09-25 | 2019-12-31 | Hoffmann La Roche | Derivati heksahidropirolo[3,4−c]pirola i srodna jedinjenja kao inhibitori autotaksina (atx) i kao inhibitori proizvodnje lizofosfatidne kiseline (lpa) za lečenje npr. bubrežnih bolesti |
| SG11201507402WA (en) * | 2013-03-12 | 2015-10-29 | Abbvie Inc | Tetracyclic bromodomain inhibitors |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| AU2014228175B2 (en) | 2013-03-15 | 2018-05-31 | Incyte Holdings Corporation | Tricyclic heterocycles as BET protein inhibitors |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| CN105611835A (zh) | 2013-07-25 | 2016-05-25 | 达纳-法伯癌症研究所股份有限公司 | 转录因子抑制剂及其用途 |
| PT3074400T (pt) | 2013-11-26 | 2018-01-22 | Hoffmann La Roche | Novo octahidro-ciclobuta [1,2-c;3,4-c']dipirrol-2-il |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | 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 |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| WO2015117053A1 (en) | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Diaminopyrimidine benzenesulfone derivatives and uses thereof |
| WO2015117087A1 (en) | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| EP3590939A1 (en) | 2014-03-26 | 2020-01-08 | F. Hoffmann-La Roche AG | Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| WO2015144609A1 (en) | 2014-03-26 | 2015-10-01 | F. Hoffmann-La Roche Ag | Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| MX2016013851A (es) | 2014-04-23 | 2017-07-14 | Incyte Corp | 1h-pirrolo[2,3-c]piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h) -onas como inhibidores de proteinas de bromodominio y extra terminal (bet). |
| JP2017526741A (ja) | 2014-08-08 | 2017-09-14 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | ジアゼパン誘導体およびその使用 |
| CA2955077A1 (en) | 2014-08-08 | 2016-02-11 | Dana-Farber Cancer Institute, Inc. | Dihydropteridinone derivatives and uses thereof |
| ES2855225T3 (es) | 2014-09-15 | 2021-09-23 | Incyte Corp | Heterociclos tricíclicos para su uso como inhibidores de proteínas BET |
| JP6639497B2 (ja) | 2014-11-10 | 2020-02-05 | ジェネンテック， インコーポレイテッド | ブロモドメインインヒビターおよびその使用 |
| MA40943A (fr) | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| MA40940A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| WO2016123391A1 (en) | 2015-01-29 | 2016-08-04 | Genentech, Inc. | Therapeutic compounds and uses thereof |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| ES2911886T3 (es) | 2015-03-30 | 2022-05-23 | Jubilant Biosys Ltd | Derivados condensados tricíclicos de 1-(ciclo)alquilpiridin-2-ona útiles para el tratamiento del cáncer |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| AU2016316717B2 (en) | 2015-09-04 | 2021-02-18 | F. Hoffmann-La Roche Ag | Phenoxymethyl derivatives |
| PT3347356T (pt) | 2015-09-09 | 2021-06-28 | Jubilant Biosys Ltd | Derivados tricíclicos de piridinaa-2-ona fundidos e a sua utilização como inibidores brd4 |
| SG10202007099TA (en) | 2015-09-11 | 2020-08-28 | Dana Farber Cancer Inst Inc | Acetamide thienotriazoldiazepines and uses thereof |
| EP3347021A4 (en) | 2015-09-11 | 2019-07-24 | Dana-Farber Cancer Institute, Inc. | CYANO-THIENOTRIAZOLOAZEPINES AND THEIR USES |
| KR20180054635A (ko) | 2015-09-24 | 2018-05-24 | 에프. 호프만-라 로슈 아게 | 오토탁신(atx) 억제제로서 이환형 화합물 |
| CN107922415B (zh) | 2015-09-24 | 2022-04-15 | 豪夫迈·罗氏有限公司 | 新的作为双重atx/ca抑制剂的二环化合物 |
| MX2018002217A (es) | 2015-09-24 | 2018-03-23 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores de autotaxina (atx). |
| JP6845230B2 (ja) | 2015-09-24 | 2021-03-17 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | デュアルａｔｘ／ｃａ阻害剤としての新規な二環式化合物 |
| US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| JP7385356B2 (ja) | 2015-11-25 | 2023-11-22 | ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド | 二価ブロモドメインインヒビターおよびそれらの使用 |
| PE20190472A1 (es) | 2016-04-15 | 2019-04-04 | Abbvie Inc | Inhibidores de bromodominios |
| BR112018076486A2 (pt) | 2016-06-20 | 2019-04-09 | Incyte Corporation | formas sólidas cristalinas de um inibidor de bet |
| CN108069976A (zh) | 2016-11-10 | 2018-05-25 | 山东罗欣药业集团股份有限公司 | 一种含氮大环类化合物、其制备方法、药物组合物及应用 |
| WO2018130174A1 (zh) * | 2017-01-11 | 2018-07-19 | 江苏豪森药业集团有限公司 | 吡咯并[2,3-c]吡啶类衍生物、其制备方法及其在医药上的应用 |
| BR112019019017A2 (pt) | 2017-03-16 | 2020-04-14 | Hoffmann La Roche | compostos heterocíclicos de utilidade como inibidores duplos de atx/ca |
| CN110382484B (zh) | 2017-03-16 | 2022-12-06 | 豪夫迈·罗氏有限公司 | 新的作为atx抑制剂的二环化合物 |
| EP3609896A4 (en) * | 2017-04-14 | 2020-11-04 | AbbVie Inc. | BROMODOMAIN INHIBITORS |
| CN110305123B (zh) * | 2018-03-27 | 2021-12-10 | 海创药业股份有限公司 | 一种含有金刚烷的化合物及其在治疗癌症中的用途 |
| CN110865130B (zh) * | 2018-08-27 | 2023-08-22 | 北京海晶生物医药科技有限公司 | 一种盐酸奥洛他定及其有关物质的检测方法 |
| CA3115110A1 (en) | 2018-10-24 | 2020-04-30 | F. Hoffmann-La Roche Ag | Conjugated chemical inducers of degradation and methods of use |
| CA3116931A1 (en) | 2018-10-30 | 2020-05-07 | Nuvation Bio Inc. | Heterocyclic compounds as bet inhibitors |
| CN109394768B (zh) * | 2018-12-10 | 2019-08-23 | 牡丹江医学院 | 一种治疗湿疹的药物及其制备方法 |
| CN111377934B (zh) * | 2018-12-29 | 2023-01-24 | 中国科学院上海药物研究所 | 一类杂环化合物，其制备及用途 |
| EP3967690A4 (en) * | 2019-03-17 | 2023-04-12 | Shanghai Ringene BioPharma Co., Ltd. | PYRROLE AMIDOPYRIDONE COMPOUND, METHOD FOR PREPARING IT AND ITS USE |
| AU2020299592A1 (en) | 2019-07-02 | 2022-02-17 | Nuvation Bio Inc. | Heterocyclic compounds as BET inhibitors |
| WO2021121276A1 (zh) * | 2019-12-17 | 2021-06-24 | 江苏恒瑞医药股份有限公司 | 稠合四环类衍生物、其制备方法及其在医药上的应用 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| AR124681A1 (es) | 2021-01-20 | 2023-04-26 | Abbvie Inc | Conjugados anticuerpo-fármaco anti-egfr |
| CA3214399A1 (en) * | 2021-04-09 | 2022-10-13 | Frank Perabo | Treatment of cancer with kdm4 inhibitors |
| EP4363417A1 (en) * | 2021-06-29 | 2024-05-08 | Tay Therapeutics Limited | Pyrrolopyridone derivatives useful in the treatment of cancer |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5159305B2 (ja) | 2005-05-30 | 2013-03-06 | 田辺三菱製薬株式会社 | チエノトリアゾロジアゼピン化合物及びその医薬としての用途 |
| MX2009004771A (es) * | 2006-11-01 | 2009-06-17 | Vertex Pharma | Compuestos heteroaril triciclicos utiles como inhibidores de janus cinasa. |
| GB0919426D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| JP5702396B2 (ja) * | 2009-11-05 | 2015-04-15 | グラクソスミスクライン エルエルシー | ベンゾジアゼピンブロモドメイン阻害剤 |
| US9085582B2 (en) * | 2010-06-22 | 2015-07-21 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| AR084070A1 (es) * | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| WO2012151512A2 (en) * | 2011-05-04 | 2012-11-08 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| SG11201507402WA (en) * | 2013-03-12 | 2015-10-29 | Abbvie Inc | Tetracyclic bromodomain inhibitors |
-
2014
- 2014-03-12 SG SG11201507402WA patent/SG11201507402WA/en unknown
- 2014-03-12 CA CA2903910A patent/CA2903910C/en active Active
- 2014-03-12 AU AU2014231563A patent/AU2014231563A1/en not_active Abandoned
- 2014-03-12 AR ARP140100878 patent/AR095266A1/es unknown
- 2014-03-12 KR KR1020157028346A patent/KR102224992B1/ko active IP Right Grant
- 2014-03-12 UY UY0001035395A patent/UY35395A/es not_active Application Discontinuation
- 2014-03-12 TW TW103108954A patent/TWI635087B/zh active
- 2014-03-12 BR BR112015022391-5A patent/BR112015022391B1/pt active IP Right Grant
- 2014-03-12 US US14/774,866 patent/US10035800B2/en active Active
- 2014-03-12 CN CN201480015201.7A patent/CN105026403B/zh active Active
- 2014-03-12 EP EP14762617.0A patent/EP2970330B1/en active Active
- 2014-03-12 PE PE2015001915A patent/PE20151788A1/es not_active Application Discontinuation
- 2014-03-12 RU RU2015143192A patent/RU2015143192A/ru not_active Application Discontinuation
- 2014-03-12 EP EP19156935.9A patent/EP3539962A1/en not_active Withdrawn
- 2014-03-12 CN CN201810419623.0A patent/CN108440528A/zh active Pending
- 2014-03-12 MX MX2015012006A patent/MX363913B/es active IP Right Grant
- 2014-03-12 JP JP2015561913A patent/JP6419735B2/ja active Active
- 2014-03-12 WO PCT/CN2014/000258 patent/WO2014139324A1/en active Application Filing
-
2015
- 2015-09-01 IL IL241010A patent/IL241010B/en active IP Right Grant
- 2015-09-03 ZA ZA2015/06477A patent/ZA201506477B/en unknown
- 2015-09-04 DO DO2015000216A patent/DOP2015000216A/es unknown
- 2015-09-08 PH PH12015502004A patent/PH12015502004A1/en unknown
- 2015-09-11 CR CR20150474A patent/CR20150474A/es unknown
-
2016
- 2016-05-04 HK HK16105095.5A patent/HK1217102A1/zh unknown
-
2018
- 2018-05-31 AU AU2018203833A patent/AU2018203833A1/en not_active Abandoned
- 2018-06-26 US US16/018,357 patent/US20180298003A1/en not_active Abandoned
- 2018-10-09 JP JP2018190645A patent/JP2019014748A/ja active Pending
-
2019
- 2019-01-22 US US16/254,124 patent/US20190389861A1/en not_active Abandoned
-
2020
- 2020-03-23 US US16/827,026 patent/US20200291027A1/en not_active Abandoned
- 2020-11-16 US US17/099,133 patent/US20210070756A1/en not_active Abandoned
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