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 (enExample
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)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline 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 (enExample) 2015-04-30
JP5905075B2 true JP5905075B2 (ja) 2016-04-20

Family

ID=44147342

Family Applications (1)

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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 (enExample)
EP (2) EP3168213B1 (enExample)
JP (1) JP5905075B2 (enExample)
ES (1) ES2615238T3 (enExample)
GB (1) GB201106750D0 (enExample)
WO (1) WO2012143415A1 (enExample)

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WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
US9271978B2 (en) 2012-12-21 2016-03-01 Zenith Epigenetics Corp. Heterocyclic compounds as bromodomain inhibitors
JP2016512524A (ja) 2013-03-11 2016-04-28 アッヴィ・インコーポレイテッド ブロモドメイン阻害剤
EP2970285B1 (en) 2013-03-11 2019-04-17 AbbVie Inc. Fused tetracyclic bromodomain inhibitors
ES2704048T3 (es) 2013-03-14 2019-03-14 Glaxosmithkline Ip No 2 Ltd Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina-2,3-disustituida y su uso como inhibidores de bromodominio
US9227985B2 (en) 2013-03-15 2016-01-05 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
SG11201510409QA (en) 2013-06-21 2016-01-28 Zenith Epigenetics Corp Novel bicyclic bromodomain inhibitors
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
AU2014298051B2 (en) 2013-07-31 2018-11-15 Zenith Epigenetics Ltd. Novel quinazolinones as bromodomain inhibitors
PT3071203T (pt) * 2013-11-18 2021-03-11 Forma Therapeutics Inc Composições de tetra-hidroquinolina como inibidores de bromodomínio bet
WO2015074081A1 (en) 2013-11-18 2015-05-21 Bair Kenneth W Benzopiperazine compositions as bet bromodomain inhibitors
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
US9309246B2 (en) 2013-12-19 2016-04-12 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
JP6480944B2 (ja) * 2014-01-09 2019-03-13 オリオン コーポレーション ブロモドメイン阻害剤としての二環式複素環誘導体
MY180775A (en) 2014-04-23 2020-12-09 Incyte Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
ES2896400T3 (es) * 2014-08-01 2022-02-24 Nuevolution As Compuestos activos frente a bromdominios
TR201820050T4 (tr) 2014-09-12 2019-01-21 Glaxosmithkline Ip No 2 Ltd Bromodomain inhibitörleri olarak tetrahidrokinolin türevleri.
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
WO2016087942A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridines as bromodomain inhibitors
CN107207474B (zh) 2014-12-11 2021-05-07 恒翼生物医药科技(上海)有限公司 被取代的杂环作为溴结构域抑制剂
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
KR102643344B1 (ko) 2016-06-20 2024-03-07 인사이트 코포레이션 Bet 저해제의 결정질 고체 형태
WO2018022802A1 (en) 2016-07-26 2018-02-01 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
TWI825085B (zh) * 2018-03-30 2023-12-11 日商協和麒麟股份有限公司 具有抗癌活性之化合物
WO2019213570A1 (en) 2018-05-04 2019-11-07 Remedy Plan, Inc. Cancer treatments targeting cancer stem cells
KR20220110744A (ko) 2019-11-06 2022-08-09 레미디 플랜, 인크. 암 줄기 세포를 표적화하는 암 치료
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
UY39276A (es) 2020-06-19 2022-01-31 Bayer Ag Uso de compuestos de 1,3,4–oxadiazol–2–ilpirimidina para controlar microorganismos fitopatógenos, métodos de uso y composiciones.
WO2022129190A1 (en) 2020-12-18 2022-06-23 Bayer Aktiengesellschaft (hetero)aryl substituted 1,2,4-oxadiazoles as fungicides

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Also Published As

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

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