CN103619820B - 可用作溴区结构域抑制剂的四氢喹啉衍生物 - Google Patents
可用作溴区结构域抑制剂的四氢喹啉衍生物 Download PDFInfo
- Publication number
- CN103619820B CN103619820B CN201280029939.XA CN201280029939A CN103619820B CN 103619820 B CN103619820 B CN 103619820B CN 201280029939 A CN201280029939 A CN 201280029939A CN 103619820 B CN103619820 B CN 103619820B
- Authority
- CN
- China
- Prior art keywords
- compound
- methyl
- amino
- mmol
- acid
- 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.)
- Expired - Fee Related
Links
- JNUOPXDFUISVND-SVQMELKDSA-N C[C@@H](CC(c1c2)Nc(cc3)ccc3Cl)N(C=O)c1ccc2-c(cc1)ccc1C(OCCCN(C)C)=O Chemical compound C[C@@H](CC(c1c2)Nc(cc3)ccc3Cl)N(C=O)c1ccc2-c(cc1)ccc1C(OCCCN(C)C)=O JNUOPXDFUISVND-SVQMELKDSA-N 0.000 description 1
- MTEKEUSLCRUVNZ-QKKBWIMNSA-N C[C@@H](C[C@@H](c1c2)Nc(cc3)ncc3C#N)N(C(C)=O)c1ccc2-c(cc1)ncc1C(O)=O Chemical compound C[C@@H](C[C@@H](c1c2)Nc(cc3)ncc3C#N)N(C(C)=O)c1ccc2-c(cc1)ncc1C(O)=O MTEKEUSLCRUVNZ-QKKBWIMNSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
- C07D215/44—Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
-
- 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
- A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
-
- 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
- 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
- A61P37/02—Immunomodulators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
-
- 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
- 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
- C07D401/14—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 three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1106743.6 | 2011-04-21 | ||
| GB201106743A GB201106743D0 (en) | 2011-04-21 | 2011-04-21 | Novel compounds |
| PCT/EP2012/057111 WO2012143413A1 (en) | 2011-04-21 | 2012-04-19 | Tetrahydroquinoline derivatives useful as bromodomain inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103619820A CN103619820A (zh) | 2014-03-05 |
| CN103619820B true CN103619820B (zh) | 2015-08-19 |
Family
ID=44147335
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280029939.XA Expired - Fee Related CN103619820B (zh) | 2011-04-21 | 2012-04-19 | 可用作溴区结构域抑制剂的四氢喹啉衍生物 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US9029395B2 (https=) |
| EP (1) | EP2699550B1 (https=) |
| JP (1) | JP5840763B2 (https=) |
| KR (1) | KR101896599B1 (https=) |
| CN (1) | CN103619820B (https=) |
| AU (1) | AU2012244759B2 (https=) |
| BR (1) | BR112013026834A2 (https=) |
| CA (1) | CA2832763C (https=) |
| EA (1) | EA022341B1 (https=) |
| ES (1) | ES2544302T3 (https=) |
| GB (1) | GB201106743D0 (https=) |
| IL (1) | IL228707A (https=) |
| MX (1) | MX338515B (https=) |
| SG (1) | SG194469A1 (https=) |
| WO (1) | WO2012143413A1 (https=) |
| ZA (1) | ZA201307645B (https=) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201107325D0 (en) | 2011-05-04 | 2011-06-15 | Glaxosmithkline Llc | Novel compounds |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives 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 |
| HUE043568T2 (hu) | 2013-03-14 | 2019-08-28 | Glaxosmithkline Ip No 2 Ltd | 2,3-diszubsztituált 1-acil-4-amino-1,2,3,4-tetrahidrokinolin származékok és bromodomén inhibitorokkénti felhasználásuk |
| SG11201506924YA (en) | 2013-03-15 | 2015-09-29 | Incyte Corp | Tricyclic heterocycles as bet protein inhibitors |
| JP6461118B2 (ja) | 2013-06-21 | 2019-01-30 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての新規の置換された二環式化合物 |
| SI3010503T1 (sl) | 2013-06-21 | 2020-07-31 | Zenith Epigenetics Ltd. | Novi biciklični inhibitorji bromodomene |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| JP6542212B2 (ja) | 2013-07-31 | 2019-07-10 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての新規キナゾリノン |
| 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 |
| EP3105232B1 (en) | 2014-02-10 | 2019-08-28 | Concert Pharmaceuticals Inc. | Substituted triazolobenzodiazepines |
| PL3134403T3 (pl) | 2014-04-23 | 2020-07-13 | Incyte Corporation | 1H-pirolo[2,3-c]pirydyn-7(6H)-ony i pirazolo[3,4-c]pirydyn-7(6H)-ony jako inhibitory białek BET |
| JP6759514B2 (ja) | 2014-08-01 | 2020-09-23 | ヌエヴォリューション・アクティーゼルスカブＮｕｅｖｏｌｕｔｉｏｎ Ａ／Ｓ | ブロモドメインに対して活性な化合物 |
| BR112017004580A2 (pt) | 2014-09-12 | 2018-01-23 | GlaxoSmithKline Intellectual Property | composto, composição farmacêutica, produto de combinação, uso de um composto ou sal farmaceuticamente aceitável, e, método de tratamento. |
| 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 |
| CA2960090A1 (en) * | 2014-10-02 | 2016-04-07 | Glaxosmithkline Intellectual Property (No.2) Limited | Compound |
| 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 |
| CA2966450A1 (en) | 2014-12-17 | 2016-06-23 | Olesya KHARENKO | Inhibitors of bromodomains |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| 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 |
| CA3028689A1 (en) | 2016-06-20 | 2017-12-28 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| US10918647B2 (en) | 2016-07-26 | 2021-02-16 | University Of Southern California | Selective bromodomain inhibition of fungal Bdf1 |
| WO2018111805A1 (en) | 2016-12-13 | 2018-06-21 | St. Jude Children's Research Hospital | Tetrahydroquinoline-based bromodomain inhibitors |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011054851A1 (en) * | 2009-11-05 | 2011-05-12 | Glaxosmithkline Llc | Novel process |
| WO2011054848A1 (en) * | 2009-11-05 | 2011-05-12 | Glaxosmithkline Llc | Thetrahydroquinolines derivatives as bromodomain inhibitors |
| WO2011054841A1 (en) * | 2009-11-05 | 2011-05-12 | Glaxosmithkline Llc | Tetrahydroquinoline derivatives and their pharmaceutical use |
| WO2011054843A1 (en) * | 2009-11-05 | 2011-05-12 | Glaxosmithkline Llc | Bromodomain inhibitors for treating autoimmune and inflammatory diseases |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| CN1901958B (zh) | 2003-11-03 | 2011-03-09 | 葛兰素集团有限公司 | 流体分配装置 |
| JP2008156311A (ja) | 2006-12-26 | 2008-07-10 | Institute Of Physical & Chemical Research | Ｂｒｄ２ブロモドメイン結合剤 |
| KR101600634B1 (ko) | 2007-12-28 | 2016-03-07 | 미쓰비시 타나베 파마 코퍼레이션 | 항암제 |
| WO2010113498A1 (ja) * | 2009-03-31 | 2010-10-07 | 興和株式会社 | テトラヒドロキノリン化合物を有効成分とする貧血の予防及び／又は治療剤 |
| GB201106750D0 (en) * | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201107325D0 (en) * | 2011-05-04 | 2011-06-15 | Glaxosmithkline Llc | Novel compounds |
| WO2013033268A2 (en) * | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bivalent bromodomain ligands, and methods of using same |
-
2011
- 2011-04-21 GB GB201106743A patent/GB201106743D0/en not_active Ceased
-
2012
- 2012-04-19 SG SG2013076146A patent/SG194469A1/en unknown
- 2012-04-19 CA CA2832763A patent/CA2832763C/en not_active Expired - Fee Related
- 2012-04-19 JP JP2014505610A patent/JP5840763B2/ja not_active Expired - Fee Related
- 2012-04-19 EA EA201391285A patent/EA022341B1/ru not_active IP Right Cessation
- 2012-04-19 KR KR1020137030972A patent/KR101896599B1/ko not_active Expired - Fee Related
- 2012-04-19 AU AU2012244759A patent/AU2012244759B2/en not_active Ceased
- 2012-04-19 BR BR112013026834A patent/BR112013026834A2/pt not_active Application Discontinuation
- 2012-04-19 ES ES12716378.0T patent/ES2544302T3/es active Active
- 2012-04-19 US US14/111,580 patent/US9029395B2/en not_active Expired - Fee Related
- 2012-04-19 WO PCT/EP2012/057111 patent/WO2012143413A1/en not_active Ceased
- 2012-04-19 CN CN201280029939.XA patent/CN103619820B/zh not_active Expired - Fee Related
- 2012-04-19 EP EP12716378.0A patent/EP2699550B1/en active Active
- 2012-04-19 MX MX2013012190A patent/MX338515B/es active IP Right Grant
-
2013
- 2013-10-03 IL IL228707A patent/IL228707A/en active IP Right Grant
- 2013-10-14 ZA ZA2013/07645A patent/ZA201307645B/en unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011054851A1 (en) * | 2009-11-05 | 2011-05-12 | Glaxosmithkline Llc | Novel process |
| WO2011054848A1 (en) * | 2009-11-05 | 2011-05-12 | Glaxosmithkline Llc | Thetrahydroquinolines derivatives as bromodomain inhibitors |
| WO2011054841A1 (en) * | 2009-11-05 | 2011-05-12 | Glaxosmithkline Llc | Tetrahydroquinoline derivatives and their pharmaceutical use |
| WO2011054843A1 (en) * | 2009-11-05 | 2011-05-12 | Glaxosmithkline Llc | Bromodomain inhibitors for treating autoimmune and inflammatory diseases |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2832763A1 (en) | 2012-10-26 |
| KR20140025484A (ko) | 2014-03-04 |
| EA022341B1 (ru) | 2015-12-30 |
| EP2699550B1 (en) | 2015-06-10 |
| SG194469A1 (en) | 2013-12-30 |
| AU2012244759A1 (en) | 2013-10-31 |
| CN103619820A (zh) | 2014-03-05 |
| GB201106743D0 (en) | 2011-06-01 |
| JP5840763B2 (ja) | 2016-01-06 |
| US9029395B2 (en) | 2015-05-12 |
| EA201391285A1 (ru) | 2014-04-30 |
| IL228707A0 (en) | 2013-12-31 |
| BR112013026834A2 (pt) | 2016-12-27 |
| US20140039006A1 (en) | 2014-02-06 |
| EP2699550A1 (en) | 2014-02-26 |
| JP2014511891A (ja) | 2014-05-19 |
| IL228707A (en) | 2016-09-29 |
| MX2013012190A (es) | 2014-01-31 |
| ES2544302T3 (es) | 2015-08-28 |
| CA2832763C (en) | 2019-09-24 |
| WO2012143413A1 (en) | 2012-10-26 |
| AU2012244759B2 (en) | 2016-03-03 |
| ZA201307645B (en) | 2015-04-29 |
| MX338515B (es) | 2016-04-20 |
| KR101896599B1 (ko) | 2018-09-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| 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: 20150819 Termination date: 20210419 |