EA201691404A1 - Бициклические гетероциклические производные в качестве ингибиторов бромодомена - Google Patents
Бициклические гетероциклические производные в качестве ингибиторов бромодоменаInfo
- Publication number
- EA201691404A1 EA201691404A1 EA201691404A EA201691404A EA201691404A1 EA 201691404 A1 EA201691404 A1 EA 201691404A1 EA 201691404 A EA201691404 A EA 201691404A EA 201691404 A EA201691404 A EA 201691404A EA 201691404 A1 EA201691404 A1 EA 201691404A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- bicyclic heterocyclic
- heterocyclic derivatives
- pharmaceutically acceptable
- inhibitors
- formula
- 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
- C07D413/02—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
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/536—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
-
- 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
- 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
- C07D401/14—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
-
- 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
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Abstract
В настоящем изобретении предложены бициклические гетероциклические производные формулы (I), которые могут быть терапевтически полезны, особенно в качестве ингибиторов бромодоменагде R, R, R, R, L, L, Cy, Cy, X, n и пунктирная линия имеют значения, указанные в описании, и их фармацевтически приемлемые соли или фармацевтически приемлемые стереоизомеры можно применять для лечения или профилактики заболеваний или нарушений, в частности, их можно использовать для лечения заболеваний или нарушений, связанных с ингибиторами бромодомена. В настоящем изобретении также раскрыто получение указанных соединений и фармацевтических композиций, включающих по меньшей мере одно из бициклических гетероциклических производных формулы (I), вместе с его фармацевтически приемлемым носителем, разбавителем или эксципиентом.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN125CH2014 | 2014-01-09 | ||
| PCT/IB2015/050090 WO2015104653A1 (en) | 2014-01-09 | 2015-01-06 | Bicyclic heterocyclic derivatives as bromodomain inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201691404A1 true EA201691404A1 (ru) | 2016-10-31 |
| EA029224B1 EA029224B1 (ru) | 2018-02-28 |
Family
ID=52462967
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201691404A EA029224B1 (ru) | 2014-01-09 | 2015-01-06 | Бициклические гетероциклические производные в качестве ингибиторов бромодомена |
Country Status (30)
| Country | Link |
|---|---|
| US (2) | US10077259B2 (ru) |
| EP (1) | EP3092227B1 (ru) |
| JP (1) | JP6480944B2 (ru) |
| KR (1) | KR102394518B1 (ru) |
| CN (1) | CN106061966B (ru) |
| AU (1) | AU2015205339B2 (ru) |
| BR (1) | BR112016015311B1 (ru) |
| CA (1) | CA2934788C (ru) |
| CL (1) | CL2016001737A1 (ru) |
| CY (1) | CY1122046T1 (ru) |
| DK (1) | DK3092227T3 (ru) |
| EA (1) | EA029224B1 (ru) |
| ES (1) | ES2687497T3 (ru) |
| HR (1) | HRP20181650T1 (ru) |
| HU (1) | HUE041546T2 (ru) |
| IL (1) | IL246140B (ru) |
| LT (1) | LT3092227T (ru) |
| MA (1) | MA39172B1 (ru) |
| MX (1) | MX2016009052A (ru) |
| MY (1) | MY190835A (ru) |
| PE (1) | PE20161021A1 (ru) |
| PH (1) | PH12016501355A1 (ru) |
| PL (1) | PL3092227T3 (ru) |
| PT (1) | PT3092227T (ru) |
| RS (1) | RS57586B1 (ru) |
| SA (1) | SA516371448B1 (ru) |
| SG (1) | SG11201604916YA (ru) |
| SI (1) | SI3092227T1 (ru) |
| UA (1) | UA117165C2 (ru) |
| WO (1) | WO2015104653A1 (ru) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| BR112015022942B1 (pt) | 2013-03-15 | 2022-02-22 | Incyte Holdings Corporation | Compostos heterocíciclos tricíclicos, método para inibir proteína bet in vitro e composição farmacêutica compreendendo os referidos compostos |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| NZ763740A (en) | 2014-04-23 | 2023-06-30 | Incyte Holdings Corp | 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins |
| 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 |
| US20180312496A1 (en) * | 2015-07-02 | 2018-11-01 | Orion Corporation | Bicyclic heterocycle derivatives as bromodomain inhibitors |
| WO2017024408A1 (en) | 2015-08-11 | 2017-02-16 | Neomed Institute | Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals |
| WO2017024406A1 (en) | 2015-08-11 | 2017-02-16 | Neomed Institute | N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals |
| WO2017024412A1 (en) | 2015-08-12 | 2017-02-16 | Neomed Institute | Substituted benzimidazoles, their preparation and their use as pharmaceuticals |
| WO2017066876A1 (en) | 2015-10-21 | 2017-04-27 | Neomed Institute | Substituted imidazopyridines, their preparation and their use as pharmaceuticals |
| WO2017075377A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| CN105198871A (zh) * | 2015-11-06 | 2015-12-30 | 中国药科大学 | 一类喹喔啉酮类化合物及其制备方法和用途 |
| WO2017127930A1 (en) | 2016-01-28 | 2017-08-03 | Neomed Institute | Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals |
| JP2019513804A (ja) * | 2016-04-18 | 2019-05-30 | セルジーン クオンティセル リサーチ，インク． | 治療用化合物 |
| DE102017005089A1 (de) | 2016-05-30 | 2017-11-30 | Bayer Pharma Aktiengesellschaft | Substitulerte 3,4-Dihydrochinoxalin-2(1H)-one |
| FI3472157T3 (fi) | 2016-06-20 | 2023-06-01 | Incyte Corp | Bet-inhibiittorin kiteisiä kiinteitä muotoja |
| JP2020503312A (ja) | 2016-12-22 | 2020-01-30 | バイエル・クロップサイエンス・アクチェンゲゼルシャフト | 置換１，２，４−チアジアゾリルピロロンおよび１，２，４−チアジアゾリルヒダントイン、ならびにその塩、ならびにその除草剤としての使用 |
| CN110392680A (zh) | 2016-12-22 | 2019-10-29 | 拜耳作物科学股份公司 | 取代的唑基吡咯酮和唑基乙内酰脲及其盐及其作为除草活性物质的用途 |
| WO2018161876A1 (zh) * | 2017-03-08 | 2018-09-13 | 中国科学院上海药物研究所 | 二氢喹喔啉类溴结构域识别蛋白抑制剂及制备方法和用途 |
| JP2020516672A (ja) | 2017-04-18 | 2020-06-11 | セルジーン クオンティセル リサーチ，インク． | 治療用化合物 |
| CN110092782B (zh) * | 2018-01-30 | 2022-10-21 | 中国科学院广州生物医药与健康研究院 | 一种苯并六元氮杂环化合物及其制备方法和应用 |
| CN110960528A (zh) * | 2018-09-30 | 2020-04-07 | 四川大学 | Ar和bet双重抑制剂及其用途 |
| EP3873474A4 (en) | 2018-10-30 | 2022-07-13 | Nuvation Bio Inc. | HETEROCYCLIC COMPOUNDS AS BET Inhibitors |
| WO2020208307A1 (en) | 2019-04-11 | 2020-10-15 | Orion Corporation | Crystalline form of a bet-inhibitor and manufacture thereof |
| MX2022000050A (es) | 2019-07-02 | 2022-05-24 | Nuvation Bio Inc | Compuestos heterocíclicos como inhibidores de bromodominio extraterminal (bet). |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| KR102600176B1 (ko) * | 2021-10-18 | 2023-11-10 | 주식회사 사피엔스바이오 | 신규한 화합물 및 이를 포함하는 약학적 조성물 |
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| GB0919434D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
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| GB201106750D0 (en) * | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201107325D0 (en) | 2011-05-04 | 2011-06-15 | Glaxosmithkline Llc | Novel compounds |
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| US9321750B2 (en) * | 2012-04-20 | 2016-04-26 | Innov17 Llc | ROR modulators and their uses |
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| MX367420B (es) * | 2013-03-14 | 2019-08-21 | Convergene Llc | Metodos y composiciones para inhibicion de proteinas que contienen bromodominio. |
| EP2978758B1 (en) * | 2013-03-27 | 2017-02-08 | Boehringer Ingelheim International GmbH | Dihydroquinazolinone analogues as brd4 inhibitors |
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2015
- 2015-01-06 HU HUE15703314A patent/HUE041546T2/hu unknown
- 2015-01-06 SI SI201530357T patent/SI3092227T1/sl unknown
- 2015-01-06 BR BR112016015311-1A patent/BR112016015311B1/pt not_active IP Right Cessation
- 2015-01-06 UA UAA201608674A patent/UA117165C2/uk unknown
- 2015-01-06 PL PL15703314T patent/PL3092227T3/pl unknown
- 2015-01-06 CN CN201580004048.2A patent/CN106061966B/zh active Active
- 2015-01-06 SG SG11201604916YA patent/SG11201604916YA/en unknown
- 2015-01-06 DK DK15703314.3T patent/DK3092227T3/en active
- 2015-01-06 MX MX2016009052A patent/MX2016009052A/es unknown
- 2015-01-06 US US15/110,361 patent/US10077259B2/en active Active
- 2015-01-06 KR KR1020167021643A patent/KR102394518B1/ko active IP Right Grant
- 2015-01-06 MA MA39172A patent/MA39172B1/fr unknown
- 2015-01-06 RS RS20180847A patent/RS57586B1/sr unknown
- 2015-01-06 AU AU2015205339A patent/AU2015205339B2/en active Active
- 2015-01-06 LT LTEP15703314.3T patent/LT3092227T/lt unknown
- 2015-01-06 WO PCT/IB2015/050090 patent/WO2015104653A1/en active Application Filing
- 2015-01-06 EA EA201691404A patent/EA029224B1/ru not_active IP Right Cessation
- 2015-01-06 CA CA2934788A patent/CA2934788C/en active Active
- 2015-01-06 PT PT15703314T patent/PT3092227T/pt unknown
- 2015-01-06 MY MYPI2016001265A patent/MY190835A/en unknown
- 2015-01-06 JP JP2016545312A patent/JP6480944B2/ja active Active
- 2015-01-06 EP EP15703314.3A patent/EP3092227B1/en active Active
- 2015-01-06 ES ES15703314.3T patent/ES2687497T3/es active Active
- 2015-01-06 PE PE2016001002A patent/PE20161021A1/es active IP Right Grant
-
2016
- 2016-06-09 IL IL246140A patent/IL246140B/en active IP Right Grant
- 2016-07-03 SA SA516371448A patent/SA516371448B1/ar unknown
- 2016-07-07 CL CL2016001737A patent/CL2016001737A1/es unknown
- 2016-07-08 PH PH12016501355A patent/PH12016501355A1/en unknown
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2018
- 2018-08-01 US US16/051,913 patent/US10590118B2/en active Active
- 2018-09-18 CY CY20181100961T patent/CY1122046T1/el unknown
- 2018-10-11 HR HRP20181650TT patent/HRP20181650T1/hr unknown
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