JP5840763B2 - 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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JP5840763B2
JP5840763B2 JP2014505610A JP2014505610A JP5840763B2 JP 5840763 B2 JP5840763 B2 JP 5840763B2 JP 2014505610 A JP2014505610 A JP 2014505610A JP 2014505610 A JP2014505610 A JP 2014505610A JP 5840763 B2 JP5840763 B2 JP 5840763B2
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compound
methyl
acetyl
amino
mmol
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Japanese (ja)
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JP2014511891A (ja
JP2014511891A5 (https=
Inventor
アマン，ドミニク
ドゥモント，エマニュエル，ユベール
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
ジェイ ワトソン，ロバート
ジェイ ワトソン，ロバート
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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
    • 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

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  • 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)
JP2014505610A 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 Expired - Fee Related JP5840763B2 (ja)

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 (3)

Publication Number Publication Date
JP2014511891A JP2014511891A (ja) 2014-05-19
JP2014511891A5 JP2014511891A5 (https=) 2015-04-30
JP5840763B2 true JP5840763B2 (ja) 2016-01-06

Family

ID=44147335

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2014505610A Expired - Fee Related JP5840763B2 (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 (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)

* Cited by examiner, † Cited by third party
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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

Family Cites Families (12)

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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
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
WO2011054851A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Novel process
GB0919434D0 (en) * 2009-11-05 2009-12-23 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
WO2013033268A2 (en) * 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same

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
CN103619820B (zh) 2015-08-19
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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