JP5788890B2 - テトラヒドロキノリン誘導体及びその薬学的使用 - Google Patents

テトラヒドロキノリン誘導体及びその薬学的使用 Download PDF

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Publication number
JP5788890B2
JP5788890B2 JP2012537377A JP2012537377A JP5788890B2 JP 5788890 B2 JP5788890 B2 JP 5788890B2 JP 2012537377 A JP2012537377 A JP 2012537377A JP 2012537377 A JP2012537377 A JP 2012537377A JP 5788890 B2 JP5788890 B2 JP 5788890B2
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methyl
tetrahydro
acetyl
quinolinyl
methylethyl
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Japanese (ja)
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JP2013510120A5 (enExample
JP2013510120A (ja
Inventor
デモント，エマニュエル，ヒューバート
ガートン，ニール，スチュアート
ゴスミニ，ロマン，リュック，マリー
ヘイホウ，トーマス，ジョージ，クリストファー
シール，ジョナサン
ウィルソン，デヴィッド，マシュー
ウッドロー，マイケル，デヴィッド
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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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
JP2012537377A 2009-11-05 2010-11-03 テトラヒドロキノリン誘導体及びその薬学的使用 Expired - Fee Related JP5788890B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0919431.7 2009-11-02
GBGB0919431.7A GB0919431D0 (en) 2009-11-05 2009-11-05 Novel compounds
PCT/EP2010/066693 WO2011054841A1 (en) 2009-11-05 2010-11-03 Tetrahydroquinoline derivatives and their pharmaceutical use

Publications (3)

Publication Number Publication Date
JP2013510120A JP2013510120A (ja) 2013-03-21
JP2013510120A5 JP2013510120A5 (enExample) 2013-11-07
JP5788890B2 true JP5788890B2 (ja) 2015-10-07

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JP2012537377A Expired - Fee Related JP5788890B2 (ja) 2009-11-05 2010-11-03 テトラヒドロキノリン誘導体及びその薬学的使用

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Country Link
US (1) US8697725B2 (enExample)
EP (1) EP2496557B1 (enExample)
JP (1) JP5788890B2 (enExample)
ES (1) ES2449470T3 (enExample)
GB (1) GB0919431D0 (enExample)
WO (1) WO2011054841A1 (enExample)

Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2496580B1 (en) 2009-11-05 2013-12-11 GlaxoSmithKline LLC Benzodiazepine bromodomain inhibitor
SI2496582T1 (sl) 2009-11-05 2016-04-29 Glaxosmithkline Llc Corporation Service Company Benzodiazepinski inhibitor bromodomene
MX384074B (es) 2010-05-14 2025-03-12 Dana Farber Cancer Inst Inc Composiciones y métodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos.
MX373121B (es) 2010-05-14 2020-04-30 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
US9301962B2 (en) 2010-05-14 2016-04-05 Baylor College Of Medicine Male contraceptive compositions and methods of use
ES2526671T3 (es) 2010-06-22 2015-01-14 Glaxosmithkline Llc Compuestos de benzotriazoldiazepina inhibidores de bromodominios
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
GB201106750D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106743D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) * 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
US9328117B2 (en) 2011-06-17 2016-05-03 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033269A1 (en) * 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
US9624244B2 (en) 2012-06-06 2017-04-18 Constellation Pharmaceuticals, Inc. Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
US9271978B2 (en) 2012-12-21 2016-03-01 Zenith Epigenetics Corp. Heterocyclic compounds as bromodomain inhibitors
AU2014223990A1 (en) * 2013-02-28 2015-09-10 Washington University Methods of treatment of human cytomegalovirus infection and diseases with 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
US9714946B2 (en) 2013-03-14 2017-07-25 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
US9227985B2 (en) 2013-03-15 2016-01-05 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
WO2014173241A1 (en) 2013-04-26 2014-10-30 Beigene, Ltd. Substituted5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
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
WO2015013635A2 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
AU2014298051B2 (en) 2013-07-31 2018-11-15 Zenith Epigenetics Ltd. Novel quinazolinones as bromodomain inhibitors
EP3066101B1 (en) 2013-11-08 2020-07-29 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (bet) protein 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
US9994581B2 (en) 2013-12-10 2018-06-12 Abbvie Inc. Bromodomain inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
JP2017504650A (ja) 2014-01-31 2017-02-09 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド ジアゼパン誘導体およびその使用
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
EP3099677A4 (en) 2014-01-31 2017-07-26 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
KR20160130778A (ko) 2014-02-28 2016-11-14 텐샤 세러퓨틱스 인코포레이티드 고인슐린혈증과 관련된 질환의 치료
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
PL3157928T3 (pl) 2014-06-20 2019-07-31 Constellation Pharmaceuticals, Inc. Krystaliczne postacie 2-((4S)-6-(4-chlorofenylo)-1-metylo-4H-benzo[ c]izoksazolo-[4,5-e]azepin-4-ylo)acetamidu
MX2017001757A (es) 2014-08-08 2017-05-30 Dana Farber Cancer Inst Inc Derivados de dihidropteridinona y sus usos.
EP3177626A4 (en) 2014-08-08 2017-12-27 Dana Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
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
WO2016087942A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridines as bromodomain inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones 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
WO2016198691A1 (en) 2015-06-11 2016-12-15 Basilea Pharmaceutica Ag Efflux-pump inhibitors and therapeutic uses thereof
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. COMBINATION THERAPY OF TRANSCRIPTION INHIBITORS AND CHINESE INHIBITORS
WO2016203335A1 (en) 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
BR112017028178A2 (en) 2015-06-26 2018-08-28 Tensha Therapeutics, Inc. nut midline carcinoma treatment
PE20181287A1 (es) 2015-09-11 2018-08-07 Dana Farber Cancer Inst Inc Ciano tienotriazolpirazinas y usos de las mismas
UA123946C2 (uk) 2015-09-11 2021-06-30 Дана-Фарбер Кенсер Інстітьют, Інк. Ацетамідтієнотриазолодіазепіни й шляхи їх застосування
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CA3003288A1 (en) 2015-11-25 2017-06-01 Dana-Farber Cancer Institute, Inc. Bivalent bromodomain inhibitors and uses thereof
WO2017205536A2 (en) * 2016-05-24 2017-11-30 Genentech, Inc. Therapeutic compounds and uses thereof
KR102643344B1 (ko) 2016-06-20 2024-03-07 인사이트 코포레이션 Bet 저해제의 결정질 고체 형태
WO2018111805A1 (en) 2016-12-13 2018-06-21 St. Jude Children's Research Hospital Tetrahydroquinoline-based bromodomain inhibitors
WO2021175432A1 (en) 2020-03-04 2021-09-10 Boehringer Ingelheim International Gmbh Method for administration of an anti cancer agent
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN114751836B (zh) * 2021-02-23 2024-05-31 四川青木制药有限公司 3-(4-甲基-1h-咪唑-1-基)-5-(三氟甲基)苯胺合成方法及其中间体
JP2025514712A (ja) 2022-04-19 2025-05-09 ヌエヴォリューション・アクティーゼルスカブ ブロモドメインに対して活性な化合物

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU570439B2 (en) 1983-03-28 1988-03-17 Compression Labs, Inc. A combined intraframe and interframe transform coding system
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
US6140342A (en) * 1998-09-17 2000-10-31 Pfizer Inc. Oxy substituted 4-carboxyamino-2-methyl-1,2,3,4-tetrahydroquinolines
CN1901958B (zh) 2003-11-03 2011-03-09 葛兰素集团有限公司 流体分配装置
CA2561564A1 (en) 2004-04-07 2005-10-27 Millennium Pharmaceuticals, Inc. Pgd2 receptor antagonists for the treatment of inflammatory diseases
JP4531027B2 (ja) * 2005-09-29 2010-08-25 田辺三菱製薬株式会社 医薬組成物
JP2008156311A (ja) 2006-12-26 2008-07-10 Institute Of Physical & Chemical Research Ｂｒｄ２ブロモドメイン結合剤
US8476260B2 (en) * 2007-12-28 2013-07-02 Mitsubishi Tanabe Pharma Corporation Antitumor agent
GB0919434D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds

Also Published As

Publication number Publication date
GB0919431D0 (en) 2009-12-23
US20120208798A1 (en) 2012-08-16
ES2449470T3 (es) 2014-03-19
WO2011054841A1 (en) 2011-05-12
JP2013510120A (ja) 2013-03-21
EP2496557B1 (en) 2013-12-18
EP2496557A1 (en) 2012-09-12
US8697725B2 (en) 2014-04-15

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