CN106687453A8 - 作为溴结构域抑制剂的四氢喹啉衍生物 - Google Patents
作为溴结构域抑制剂的四氢喹啉衍生物 Download PDFInfo
- Publication number
- CN106687453A8 CN106687453A8 CN201580048713.8A CN201580048713A CN106687453A8 CN 106687453 A8 CN106687453 A8 CN 106687453A8 CN 201580048713 A CN201580048713 A CN 201580048713A CN 106687453 A8 CN106687453 A8 CN 106687453A8
- Authority
- CN
- China
- Prior art keywords
- domain inhibitor
- bromine domain
- tetrahydroquinoline derivative
- bromine
- inhibitor
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 title abstract 2
- 229910052794 bromium Inorganic materials 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000000147 tetrahydroquinolinyl group Chemical class N1(CCCC2=CC=CC=C12)* 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
- A61P31/04—Antibacterial agents
-
- 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
- A61P31/10—Antimycotics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Virology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Quinoline Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
本发明涉及特定新型化合物、含有此类化合物的药物组合物及其作为溴结构域抑制剂在疗法中的用途。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462049449P | 2014-09-12 | 2014-09-12 | |
| US62/049,449 | 2014-09-12 | ||
| PCT/EP2015/070665 WO2016038120A1 (en) | 2014-09-12 | 2015-09-09 | Tetrahydroquinoline derivatives as bromodomain inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| CN106687453A CN106687453A (zh) | 2017-05-17 |
| CN106687453A8 true CN106687453A8 (zh) | 2017-06-30 |
| CN106687453B CN106687453B (zh) | 2019-07-19 |
Family
ID=54065889
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580048713.8A Expired - Fee Related CN106687453B (zh) | 2014-09-12 | 2015-09-09 | 作为溴结构域抑制剂的四氢喹啉衍生物 |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US10059699B2 (zh) |
| EP (1) | EP3191476B1 (zh) |
| JP (1) | JP6531167B2 (zh) |
| KR (1) | KR20170054421A (zh) |
| CN (1) | CN106687453B (zh) |
| AR (1) | AR101806A1 (zh) |
| AU (1) | AU2015314184B2 (zh) |
| BR (1) | BR112017004580A2 (zh) |
| CA (1) | CA2958159A1 (zh) |
| CL (1) | CL2017000587A1 (zh) |
| CO (1) | CO2017001601A2 (zh) |
| CR (1) | CR20170090A (zh) |
| CY (1) | CY1121369T1 (zh) |
| DK (1) | DK3191476T3 (zh) |
| DO (1) | DOP2017000058A (zh) |
| EA (1) | EA031679B9 (zh) |
| ES (1) | ES2705623T3 (zh) |
| HR (1) | HRP20182064T1 (zh) |
| HU (1) | HUE041694T2 (zh) |
| IL (1) | IL250397A0 (zh) |
| LT (1) | LT3191476T (zh) |
| MA (1) | MA40366A (zh) |
| MX (1) | MX2017003219A (zh) |
| PE (1) | PE20170675A1 (zh) |
| PH (1) | PH12017500348B1 (zh) |
| PL (1) | PL3191476T3 (zh) |
| PT (1) | PT3191476T (zh) |
| RS (1) | RS58135B1 (zh) |
| SG (1) | SG11201701043UA (zh) |
| SI (1) | SI3191476T1 (zh) |
| TR (1) | TR201820050T4 (zh) |
| TW (1) | TWI686389B (zh) |
| UY (1) | UY36292A (zh) |
| WO (1) | WO2016038120A1 (zh) |
| ZA (1) | ZA201700883B (zh) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20151727A1 (es) | 2013-03-14 | 2015-12-17 | Boehringer Ingelheim Int | Acido 2-aza-biciclo[2.2.1]heptano-3-carboxilico (bencil-ciano-metil)-amidas sustituidas inhibidores de catepsina c |
| EP3191487B1 (en) | 2014-09-12 | 2019-08-07 | Boehringer Ingelheim International GmbH | Spirocyclic inhibitors of cathepsin c |
| WO2018111805A1 (en) | 2016-12-13 | 2018-06-21 | St. Jude Children's Research Hospital | Tetrahydroquinoline-based bromodomain inhibitors |
| AU2019372121A1 (en) | 2018-10-30 | 2021-05-27 | Nuvation Bio Inc. | Heterocyclic compounds as BET inhibitors |
| KR102677015B1 (ko) | 2019-07-02 | 2024-06-19 | 누베이션 바이오 인크. | Bet 억제제로서의 헤테로시클릭 화합물 |
| EP4095128A1 (en) | 2021-05-25 | 2022-11-30 | Centre national de la recherche scientifique | Tetrahydroquinoline (thq) coumpounds |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2415764A4 (en) * | 2009-03-31 | 2012-08-08 | Kowa Co | PROPHYLACTIC AND / OR THERAPEUTIC AGENT AGAINST ANEMIA WITH A TETRAHYDROCHINOLINE COMPOUND AS AN ACTIVE SUBSTANCE |
| GB0919431D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919434D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB201106743D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201106750D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201107325D0 (en) | 2011-05-04 | 2011-06-15 | Glaxosmithkline Llc | Novel compounds |
| NZ710765A (en) * | 2013-03-14 | 2020-05-29 | Glaxosmithkline Ip No 2 Ltd | 2,3-disubstituted 1 -acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors |
-
2015
- 2015-09-09 EP EP15760461.2A patent/EP3191476B1/en active Active
- 2015-09-09 PL PL15760461T patent/PL3191476T3/pl unknown
- 2015-09-09 SI SI201530529T patent/SI3191476T1/sl unknown
- 2015-09-09 KR KR1020177008675A patent/KR20170054421A/ko unknown
- 2015-09-09 JP JP2017513723A patent/JP6531167B2/ja not_active Expired - Fee Related
- 2015-09-09 WO PCT/EP2015/070665 patent/WO2016038120A1/en active Application Filing
- 2015-09-09 AU AU2015314184A patent/AU2015314184B2/en not_active Ceased
- 2015-09-09 EA EA201790484A patent/EA031679B9/ru not_active IP Right Cessation
- 2015-09-09 ES ES15760461T patent/ES2705623T3/es active Active
- 2015-09-09 CN CN201580048713.8A patent/CN106687453B/zh not_active Expired - Fee Related
- 2015-09-09 CA CA2958159A patent/CA2958159A1/en not_active Abandoned
- 2015-09-09 US US15/509,894 patent/US10059699B2/en active Active
- 2015-09-09 RS RS20190001A patent/RS58135B1/sr unknown
- 2015-09-09 HU HUE15760461A patent/HUE041694T2/hu unknown
- 2015-09-09 LT LTEP15760461.2T patent/LT3191476T/lt unknown
- 2015-09-09 TR TR2018/20050T patent/TR201820050T4/tr unknown
- 2015-09-09 PE PE2017000388A patent/PE20170675A1/es unknown
- 2015-09-09 BR BR112017004580-0A patent/BR112017004580A2/pt not_active Application Discontinuation
- 2015-09-09 MX MX2017003219A patent/MX2017003219A/es active IP Right Grant
- 2015-09-09 PT PT15760461T patent/PT3191476T/pt unknown
- 2015-09-09 SG SG11201701043UA patent/SG11201701043UA/en unknown
- 2015-09-09 CR CR20170090A patent/CR20170090A/es unknown
- 2015-09-09 MA MA040366A patent/MA40366A/fr unknown
- 2015-09-09 DK DK15760461.2T patent/DK3191476T3/en active
- 2015-09-10 TW TW104129977A patent/TWI686389B/zh not_active IP Right Cessation
- 2015-09-10 AR ARP150102888A patent/AR101806A1/es unknown
- 2015-09-10 UY UY0001036292A patent/UY36292A/es not_active Application Discontinuation
-
2017
- 2017-02-01 IL IL250397A patent/IL250397A0/en unknown
- 2017-02-03 ZA ZA2017/00883A patent/ZA201700883B/en unknown
- 2017-02-17 CO CONC2017/0001601A patent/CO2017001601A2/es unknown
- 2017-02-27 PH PH12017500348A patent/PH12017500348B1/en unknown
- 2017-03-07 DO DO2017000058A patent/DOP2017000058A/es unknown
- 2017-03-09 CL CL2017000587A patent/CL2017000587A1/es unknown
-
2018
- 2018-12-06 HR HRP20182064TT patent/HRP20182064T1/hr unknown
-
2019
- 2019-01-15 CY CY20191100049T patent/CY1121369T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| CI01 | Publication of corrected invention patent application | ||
| CI01 | Publication of corrected invention patent application |
Correction item: Priority Correct: 62/049,449 2014.09.12 US Number: 20 Volume: 33 |
|
| CI02 | Correction of invention patent application | ||
| CI02 | Correction of invention patent application |
Correction item: Priority Correct: 62/049,449 2014.09.12 US Number: 20 Page: The title page Volume: 33 |
|
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20190719 |