SG194469A1 - Tetrahydroquinoline derivatives useful as bromodomain inhibitors - Google Patents
Tetrahydroquinoline derivatives useful as bromodomain inhibitors Download PDFInfo
- Publication number
- SG194469A1 SG194469A1 SG2013076146A SG2013076146A SG194469A1 SG 194469 A1 SG194469 A1 SG 194469A1 SG 2013076146 A SG2013076146 A SG 2013076146A SG 2013076146 A SG2013076146 A SG 2013076146A SG 194469 A1 SG194469 A1 SG 194469A1
- Authority
- SG
- Singapore
- Prior art keywords
- derivatives useful
- tetrahydroquinoline derivatives
- bromodomain inhibitors
- tetrahydroquinoline
- bromodomain
- Prior art date
Links
- 125000000147 tetrahydroquinolinyl group Chemical class N1(CCCC2=CC=CC=C12)* 0.000 title abstract 2
- 102000001805 Bromodomains Human genes 0.000 title 1
- 108050009021 Bromodomains Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 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 (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 (1)
| Publication Number | Publication Date |
|---|---|
| SG194469A1 true SG194469A1 (en) | 2013-12-30 |
Family
ID=44147335
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG2013076146A SG194469A1 (en) | 2011-04-21 | 2012-04-19 | Tetrahydroquinoline derivatives useful as bromodomain inhibitors |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US9029395B2 (enExample) |
| EP (1) | EP2699550B1 (enExample) |
| JP (1) | JP5840763B2 (enExample) |
| KR (1) | KR101896599B1 (enExample) |
| CN (1) | CN103619820B (enExample) |
| AU (1) | AU2012244759B2 (enExample) |
| BR (1) | BR112013026834A2 (enExample) |
| CA (1) | CA2832763C (enExample) |
| EA (1) | EA022341B1 (enExample) |
| ES (1) | ES2544302T3 (enExample) |
| GB (1) | GB201106743D0 (enExample) |
| IL (1) | IL228707A (enExample) |
| MX (1) | MX338515B (enExample) |
| SG (1) | SG194469A1 (enExample) |
| WO (1) | WO2012143413A1 (enExample) |
| ZA (1) | ZA201307645B (enExample) |
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 |
| CN105189461B (zh) * | 2013-03-14 | 2018-05-15 | 葛兰素史克知识产权第二有限公司 | 2,3-二取代的1-酰基-4-氨基-1,2,3,4-四氢喹啉衍生物和它们作为溴结构域抑制剂的用途 |
| 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 |
| WO2015120393A1 (en) | 2014-02-10 | 2015-08-13 | Concert Pharmaceuticals, Inc. | Substituted triazolobenzodiazepines |
| 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 |
| SG10201900631TA (en) | 2014-08-01 | 2019-02-27 | Nuevolution As | Compounds active towards bromodomains |
| WO2016038120A1 (en) | 2014-09-12 | 2016-03-17 | Glaxosmithkline Intellectual Property (No.2) Limited | Tetrahydroquinoline derivatives as bromodomain inhibitors |
| 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 |
| KR20170055549A (ko) * | 2014-10-02 | 2017-05-19 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | 화합물 |
| 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 |
| 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 |
| 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 |
| 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 |
| CN109715625B (zh) | 2016-06-20 | 2022-04-19 | 因赛特公司 | Bet抑制剂的结晶固体形式 |
| EP3490552B1 (en) | 2016-07-26 | 2022-11-23 | University of Southern California | Selective bromodomain inhibition of fungal bdf1 |
| US11028051B2 (en) * | 2016-12-13 | 2021-06-08 | 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 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| BRPI0416128B8 (pt) | 2003-11-03 | 2021-06-22 | Glaxo Group Ltd | dispositivo de dispensação de fluido |
| JP2008156311A (ja) | 2006-12-26 | 2008-07-10 | Institute Of Physical & Chemical Research | Ｂｒｄ２ブロモドメイン結合剤 |
| CN101910182B (zh) | 2007-12-28 | 2013-07-17 | 田边三菱制药株式会社 | 抗癌剂 |
| 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 |
| GB0919431D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| WO2011054851A1 (en) * | 2009-11-05 | 2011-05-12 | Glaxosmithkline Llc | Novel process |
| GB0919434D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| 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 JP JP2014505610A patent/JP5840763B2/ja not_active Expired - Fee Related
- 2012-04-19 WO PCT/EP2012/057111 patent/WO2012143413A1/en not_active Ceased
- 2012-04-19 KR KR1020137030972A patent/KR101896599B1/ko not_active Expired - Fee Related
- 2012-04-19 ES ES12716378.0T patent/ES2544302T3/es active Active
- 2012-04-19 CN CN201280029939.XA patent/CN103619820B/zh not_active Expired - Fee Related
- 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 EP EP12716378.0A patent/EP2699550B1/en active Active
- 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 US US14/111,580 patent/US9029395B2/en not_active Expired - Fee Related
- 2012-04-19 MX MX2013012190A patent/MX338515B/es active IP Right Grant
- 2012-04-19 EA EA201391285A patent/EA022341B1/ru not_active IP Right Cessation
-
2013
- 2013-10-03 IL IL228707A patent/IL228707A/en active IP Right Grant
- 2013-10-14 ZA ZA2013/07645A patent/ZA201307645B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP5840763B2 (ja) | 2016-01-06 |
| WO2012143413A1 (en) | 2012-10-26 |
| IL228707A (en) | 2016-09-29 |
| US9029395B2 (en) | 2015-05-12 |
| US20140039006A1 (en) | 2014-02-06 |
| AU2012244759B2 (en) | 2016-03-03 |
| KR20140025484A (ko) | 2014-03-04 |
| CA2832763C (en) | 2019-09-24 |
| JP2014511891A (ja) | 2014-05-19 |
| ZA201307645B (en) | 2015-04-29 |
| IL228707A0 (en) | 2013-12-31 |
| MX338515B (es) | 2016-04-20 |
| ES2544302T3 (es) | 2015-08-28 |
| EA022341B1 (ru) | 2015-12-30 |
| KR101896599B1 (ko) | 2018-09-07 |
| AU2012244759A1 (en) | 2013-10-31 |
| EP2699550B1 (en) | 2015-06-10 |
| EA201391285A1 (ru) | 2014-04-30 |
| EP2699550A1 (en) | 2014-02-26 |
| MX2013012190A (es) | 2014-01-31 |
| BR112013026834A2 (pt) | 2016-12-27 |
| CN103619820A (zh) | 2014-03-05 |
| GB201106743D0 (en) | 2011-06-01 |
| CN103619820B (zh) | 2015-08-19 |
| CA2832763A1 (en) | 2012-10-26 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| MX338515B (es) | Derivados de tetrahidroquinolina utiles como inhibidores de bromodominio. | |
| GB201106750D0 (en) | Novel compounds | |
| IN2014CN00568A (enExample) | ||
| EP2721033A4 (en) | COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE AS IDH1 MUTANT INHIBITORS FOR THE TREATMENT OF CANCER | |
| IN2014DN10386A (enExample) | ||
| IN2014MN02598A (enExample) | ||
| MX2015007921A (es) | Compuestos heterociclicos novedosos como inhibidores de bromodominio. | |
| GEP201706688B (en) | Cdk8/cdk19 selective inhibitors and their use in anti- metastatic and chemopreventative methods for cancer | |
| IN2014DN10670A (enExample) | ||
| PH12015501998A1 (en) | Heterocyclic compounds and their uses | |
| MY177344A (en) | Compounds and their methods of use | |
| EA201400771A1 (ru) | Новые производные азетидина, фармацевтические композиции и их применение | |
| IL232113A (en) | Boron-containing compounds, pharmaceuticals containing them and their use in inhibiting arginase | |
| IL234884A0 (en) | Inhibitors of kynurenine-3-monooxygenase pharmaceutical compositions, and methods of their use | |
| IN2014MN02049A (enExample) | ||
| PH12015501609A1 (en) | Phenicol antibacterials | |
| IL230705A0 (en) | Certain inhibitors of kynurenine-3-monooxygenase pharmaceutical compositions, and methods of their use | |
| EA032271B9 (ru) | Вещества, фармацевтическая композиция и методы применения при лечении воспалительных заболеваний | |
| MX2015012416A (es) | Compuestos heterociclicos y sus usos. | |
| MX2016004741A (es) | Composicion farmaceutica que comprende un antagonista de trpa1 y un agente analgesico. | |
| MX2015011614A (es) | Derivados de pirrolidina, composiciones farmaceuticas que los contienen, y su uso en terapia. | |
| PH12017500348A1 (en) | Tetrahydroquinoline derivatives as bromodomain inhibitors | |
| MX2016003522A (es) | Derivados de quinazolinas y su uso como inhibidores de la adn metiltransferasa. | |
| ZA201306905B (en) | Novel octahydrothienoquinonline derivative,pharmaceutical composition comprising derivative, and use of these | |
| EA201400444A1 (ru) | Производные 2-оксопиперидинила |