JP5905075B2 - ブロモドメイン阻害剤として有用なテトラヒドロキノリン誘導体 - Google Patents

ブロモドメイン阻害剤として有用なテトラヒドロキノリン誘導体 Download PDF

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JP5905075B2
JP5905075B2 JP2014505612A JP2014505612A JP5905075B2 JP 5905075 B2 JP5905075 B2 JP 5905075B2 JP 2014505612 A JP2014505612 A JP 2014505612A JP 2014505612 A JP2014505612 A JP 2014505612A JP 5905075 B2 JP5905075 B2 JP 5905075B2
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methyl
amino
acetyl
tetrahydroquinolin
mmol
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JP2014511892A5 (https=
JP2014511892A (ja
Inventor
アマン，ドミニク
ユベール ドゥモント，エマニュエル
ユベール ドゥモント，エマニュエル
ジェイソン ミッチェル，ダレン
ジェイソン ミッチェル，ダレン
トーマス シール，ジョナサン
トーマス シール，ジョナサン
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グラクソスミスクライン エルエルシー
グラクソスミスクライン エルエルシー
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    • 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
    • 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
    • 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
    • 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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2014505612A 2011-04-21 2012-04-19 ブロモドメイン阻害剤として有用なテトラヒドロキノリン誘導体 Active JP5905075B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1106750.1A GB201106750D0 (en) 2011-04-21 2011-04-21 Novel compounds
GB1106750.1 2011-04-21
PCT/EP2012/057113 WO2012143415A1 (en) 2011-04-21 2012-04-19 Tetrahydroquinoline derivatives useful as bromodomain inhibitors

Publications (3)

Publication Number Publication Date
JP2014511892A JP2014511892A (ja) 2014-05-19
JP2014511892A5 JP2014511892A5 (https=) 2015-04-30
JP5905075B2 true JP5905075B2 (ja) 2016-04-20

Family

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JP2014505612A Active JP5905075B2 (ja) 2011-04-21 2012-04-19 ブロモドメイン阻害剤として有用なテトラヒドロキノリン誘導体

Country Status (6)

Country Link
US (1) US8993554B2 (https=)
EP (2) EP2699551B1 (https=)
JP (1) JP5905075B2 (https=)
ES (1) ES2615238T3 (https=)
GB (1) GB201106750D0 (https=)
WO (1) WO2012143415A1 (https=)

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US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
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US9050346B2 (en) 2013-03-11 2015-06-09 Abbvie Inc. Bromodomain inhibitors
MX2015012158A (es) 2013-03-11 2015-12-01 Abbvie Inc Inhibidores de bomodominio tetraciclicos fusionados.
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
RU2720237C2 (ru) * 2013-11-18 2020-04-28 Форма Терапеутикс, Инк. Композиции, содержащие бензопиперазин, в качестве ингибиторов бромодоменов вет
CN110627770A (zh) * 2013-11-18 2019-12-31 福马疗法公司 作为bet溴域抑制剂的四氢喹啉组成物
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
US9142676B2 (en) 2013-12-30 2015-09-22 Taiwan Semiconductor Manufacturing Company, Ltd. Semiconductor liner of semiconductor device
HUE041546T2 (hu) 2014-01-09 2019-05-28 Orion Corp Biciklusos heterociklusos származékvegyületek mint bromo doméninhibitorok
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
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones 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
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Also Published As

Publication number Publication date
EP3168213B1 (en) 2018-08-01
EP2699551A1 (en) 2014-02-26
ES2615238T3 (es) 2017-06-06
US8993554B2 (en) 2015-03-31
EP3168213A1 (en) 2017-05-17
WO2012143415A1 (en) 2012-10-26
US20140031336A1 (en) 2014-01-30
GB201106750D0 (en) 2011-06-01
JP2014511892A (ja) 2014-05-19
EP2699551B1 (en) 2016-11-16

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