ES2615238T3 - Derivados de tetrahidroquinolinas como inhibidores de bromodominio - Google Patents

Derivados de tetrahidroquinolinas como inhibidores de bromodominio Download PDF

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Publication number
ES2615238T3
ES2615238T3 ES12718620.3T ES12718620T ES2615238T3 ES 2615238 T3 ES2615238 T3 ES 2615238T3 ES 12718620 T ES12718620 T ES 12718620T ES 2615238 T3 ES2615238 T3 ES 2615238T3
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Spain
Prior art keywords
mmol
methyl
acetyl
amino
tetrahydroquinolin
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
ES12718620.3T
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English (en)
Spanish (es)
Inventor
Dominique AMANS
Emmanuel Hubert Demont
Darren Jason Mitchell
Jonathan Thomas Seal
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GlaxoSmithKline LLC
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GlaxoSmithKline LLC
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • C07D215/44Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
ES12718620.3T 2011-04-21 2012-04-19 Derivados de tetrahidroquinolinas como inhibidores de bromodominio Active ES2615238T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB201106750 2011-04-21
GBGB1106750.1A GB201106750D0 (en) 2011-04-21 2011-04-21 Novel compounds
PCT/EP2012/057113 WO2012143415A1 (en) 2011-04-21 2012-04-19 Tetrahydroquinoline derivatives useful as bromodomain inhibitors

Publications (1)

Publication Number Publication Date
ES2615238T3 true ES2615238T3 (es) 2017-06-06

Family

ID=44147342

Family Applications (1)

Application Number Title Priority Date Filing Date
ES12718620.3T Active ES2615238T3 (es) 2011-04-21 2012-04-19 Derivados de tetrahidroquinolinas como inhibidores de bromodominio

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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GB201106743D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
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
MX2015012005A (es) 2013-03-11 2016-04-04 Abbvie Inc Inhibidores de bromodominio.
WO2014164780A1 (en) 2013-03-11 2014-10-09 Abbvie Inc. Fused tetracyclic bromodomain inhibitors
PE20151596A1 (es) 2013-03-14 2015-11-24 Glaxosmithkline Intellectual Property N 2 Ltd Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina 2,3-disustituidos y su uso como inhibidores del bromodominio
CA2903881C (en) 2013-03-15 2021-05-18 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
SG11201510409QA (en) 2013-06-21 2016-01-28 Zenith Epigenetics Corp Novel bicyclic bromodomain inhibitors
CA2915622C (en) 2013-06-21 2020-08-18 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
US9855271B2 (en) 2013-07-31 2018-01-02 Zenith Epigenetics Ltd. Quinazolinones as bromodomain inhibitors
CN106029076B (zh) 2013-11-18 2019-06-07 福马疗法公司 作为bet溴域抑制剂的苯并哌嗪组合物
ES2860695T3 (es) * 2013-11-18 2021-10-05 Forma Therapeutics Inc Composiciones de tetrahidroquinolina como inhibidores de bromodominio BET
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles 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
LT3092227T (lt) * 2014-01-09 2018-08-10 Orion Corporation Bicikliniai heterocikliniai dariniai kaip bromodomeno inhibitoriai
DK3674302T3 (da) 2014-04-23 2023-04-03 Incyte Holdings Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-oner og pyrazolo[3,4-c]pyridin-7(6h)-oner som inhibitorer af bet-proteiner
CN106573915B (zh) * 2014-08-01 2020-12-25 纽韦卢森公司 针对布罗莫结构域有活性的化合物
PT3191476T (pt) 2014-09-12 2019-01-17 Glaxosmithkline Ip No 2 Ltd Derivados de tetra-hidroquinolina como inibidores de bromodomínio
EP3194406B8 (en) 2014-09-15 2021-03-31 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
EP3227281A4 (en) 2014-12-01 2018-05-30 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
HK1245248B (en) 2014-12-11 2020-05-15 恒翼生物医药(上海)股份有限公司 Substituted heterocycles as bromodomain inhibitors
HK1245247A1 (zh) 2014-12-17 2018-08-24 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
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
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
CA3220957A1 (en) 2016-06-20 2017-12-28 Incyte Corporation Crystalline solid forms of a bet inhibitor
EP3490552B1 (en) 2016-07-26 2022-11-23 University of Southern California Selective bromodomain inhibition of fungal bdf1
US11028051B2 (en) 2016-12-13 2021-06-08 St. Jude Children's Research Hospital Tetrahydroquinoline-based bromodomain inhibitors
US11629152B2 (en) * 2018-03-30 2023-04-18 Kyowa Kirin Co., Ltd. Compound with anticancer activity
KR20250107972A (ko) 2018-05-04 2025-07-14 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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GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
PL1699512T3 (pl) 2003-11-03 2012-11-30 Glaxo Group Ltd Urządzenie do dozowania płynów
JP2008156311A (ja) 2006-12-26 2008-07-10 Institute Of Physical & Chemical Research Brd2ブロモドメイン結合剤
CA2710740C (en) 2007-12-28 2016-07-19 Shinji Miyoshi Thienotriazolodiazepine compound as antitumor agent
WO2010018874A1 (en) * 2008-08-12 2010-02-18 Takeda Pharmaceutical Company Limited Amide compound
US20100113514A1 (en) * 2008-10-30 2010-05-06 Gilead Palo Alto, Inc. Fused heterocyclic compounds as ion channel modulators
WO2010111626A2 (en) * 2009-03-27 2010-09-30 Takeda Pharmaceutical Company Limited Poly (adp-ribose) polymerase (parp) inhibitors
GB0919431D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
ES2539964T3 (es) * 2009-11-05 2015-07-07 Glaxosmithkline Llc Procedimiento novedoso
GB0919432D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919434D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds

Also Published As

Publication number Publication date
EP2699551A1 (en) 2014-02-26
US8993554B2 (en) 2015-03-31
US20140031336A1 (en) 2014-01-30
JP5905075B2 (ja) 2016-04-20
GB201106750D0 (en) 2011-06-01
JP2014511892A (ja) 2014-05-19
WO2012143415A1 (en) 2012-10-26
EP3168213B1 (en) 2018-08-01
EP3168213A1 (en) 2017-05-17
EP2699551B1 (en) 2016-11-16

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