[go: up one dir, main page]

TW201613935A - Tricyclic heterocycles as BET protein inhibitors - Google Patents

Tricyclic heterocycles as BET protein inhibitors

Info

Publication number
TW201613935A
TW201613935A TW104130337A TW104130337A TW201613935A TW 201613935 A TW201613935 A TW 201613935A TW 104130337 A TW104130337 A TW 104130337A TW 104130337 A TW104130337 A TW 104130337A TW 201613935 A TW201613935 A TW 201613935A
Authority
TW
Taiwan
Prior art keywords
tricyclic heterocycles
protein inhibitors
bet protein
inhibitors
tricyclic
Prior art date
Application number
TW104130337A
Other languages
English (en)
Other versions
TWI712603B (zh
Inventor
Andrew P Combs
Richard B Sparks
Original Assignee
Incyte Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of TW201613935A publication Critical patent/TW201613935A/zh
Application granted granted Critical
Publication of TWI712603B publication Critical patent/TWI712603B/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06—Peri-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biotechnology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Otolaryngology (AREA)
  • Obesity (AREA)
  • AIDS & HIV (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
TW104130337A 2014-09-15 2015-09-14 作為ｂｅｔ蛋白抑制劑之三環雜環 TWI712603B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462050500P 2014-09-15 2014-09-15
US62/050,500 2014-09-15

Publications (2)

Publication Number Publication Date
TW201613935A true TW201613935A (en) 2016-04-16
TWI712603B TWI712603B (zh) 2020-12-11

Family

ID=54207768

Family Applications (1)

Application Number Title Priority Date Filing Date
TW104130337A TWI712603B (zh) 2014-09-15 2015-09-14 作為ｂｅｔ蛋白抑制劑之三環雜環

Country Status (6)

Country Link
US (4) US9527864B2 (zh)
EP (1) EP3194406B8 (zh)
JP (1) JP6599979B2 (zh)
ES (1) ES2855225T3 (zh)
TW (1) TWI712603B (zh)
WO (1) WO2016044130A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112679520A (zh) * 2018-08-24 2021-04-20 杭州阿诺生物医药科技有限公司 Sting激动剂及其制备方法

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2903881C (en) 2013-03-15 2021-05-18 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
CA2917319A1 (en) 2013-07-08 2015-01-15 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
FI3674302T3 (fi) 2014-04-23 2023-04-27 Incyte Holdings Corp 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONEJA JA PYRATSOLO[3,4-c]PYRIDIN-7(6H)-ONEJA BET-PROTEIINIEN INHIBIITTOREINA
US9527864B2 (en) * 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
AR106520A1 (es) * 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
DK3472157T3 (da) 2016-06-20 2023-05-01 Incyte Corp Krystallinske faste former af en bet-inhibitor
JP2021530442A (ja) * 2018-06-28 2021-11-11 ジエンス ヘンルイ メデイシンカンパニー リミテッドJiangsu Hengrui Medicine Co., Ltd. 縮合三環系複素環化合物およびその治療上の使用
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (154)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59170313A (ja) 1983-03-14 1984-09-26 Kurimoto Iron Works Ltd スクリ−ンゲ−ト
JPS6085739U (ja) 1983-11-18 1985-06-13 クラリオン株式会社 テ−プレコ−ダにおけるピンチロ−ラ装置
JPH0314566A (ja) 1989-06-09 1991-01-23 Sankyo Co Ltd ベンズイミダゾール誘導体
US5244912A (en) 1991-03-28 1993-09-14 Eli Lilly And Company 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz(cd)indoles and pharmaceutical use thereof
FR2710915B1 (fr) 1993-10-04 1995-11-24 Synthelabo Dérivés de pipéridine, leur préparation et leur utilisation en thérapeutique.
FR2731708B1 (fr) 1995-03-13 1997-04-30 Synthelabo Derives de piperidine, leur procede de preparation et leur application en therapeutique
FR2747678B1 (fr) 1996-04-22 1998-05-22 Synthelabo Composes derives d'imidazobenzoxazine, leurs procedes de preparation et leurs utilisations en therapeutique
US6448258B2 (en) 2000-04-21 2002-09-10 Pharmacia & Upjohn Company Treating fibromyalgia and chronic fatigue syndrome
MXPA03000051A (es) 2000-06-28 2003-08-19 Smithkline Beecham Plc Procedimiento de molido en humedo.
US6919334B2 (en) 2002-09-12 2005-07-19 Wyeth Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine
NZ539952A (en) 2002-11-22 2008-05-30 Japan Tobacco Inc Fused bicyclic nitrogen-containing heterocyclic compounds for treating diabetes, obesity and syndrome X
EP1462103A1 (en) 2003-03-25 2004-09-29 Faust Pharmaceuticals NO donors, combination products and uses as modulators of neurotransmitter release
AU2005214258A1 (en) 2004-02-23 2005-09-01 Dainippon Sumitomo Pharma Co., Ltd. Novel heterocyclic compound
US7897607B2 (en) 2004-04-07 2011-03-01 Takeda Pharmaceutical Company Limited Cyclic compounds
DE102005011058A1 (de) 2005-03-10 2006-09-14 Merck Patent Gmbh Substituierte Tetrahydro-pyrrolo-chinolinderivate
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
JP2009503069A (ja) 2005-08-05 2009-01-29 アストラゼネカ アクチボラグ 三環式ベンゾイミダゾール類、および代謝性グルタミン酸塩受容体のモジュレータとしてのそれらの使用
US8975259B2 (en) 2007-04-27 2015-03-10 University Of Rochester Compositions and methods for inhibiting G protein signaling
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
US8633186B2 (en) 2007-06-08 2014-01-21 Senomyx Inc. Modulation of chemosensory receptors and ligands associated therewith
WO2009020559A2 (en) 2007-08-03 2009-02-12 The J. David Gladstone Institutes Agents that inhibit p-tefb interactions and methods of use thereof
EP2239264A4 (en) 2007-12-28 2012-01-11 Mitsubishi Tanabe Pharma Corp ANTITUMOR AGENT
DE102008052618A1 (de) 2008-10-21 2010-04-22 Henkel Ag & Co. Kgaa Tricyclische Aldehyde und C,H-acide Verbindungen
US8669249B2 (en) 2009-03-27 2014-03-11 Takeda Pharmaceutical Company Limited Poly (ADP-ribose) polymerase (PARP) inhibitors
TW201105681A (en) 2009-06-10 2011-02-16 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
TW201103941A (en) 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
WO2011024987A1 (ja) 2009-08-31 2011-03-03 塩野義製薬株式会社 芳香族縮合へテロ環誘導体およびそれらを含有する医薬組成物
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
WO2011054851A1 (en) 2009-11-05 2011-05-12 Glaxosmithkline Llc Novel process
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EP2722334B1 (en) 2009-11-05 2016-01-13 GlaxoSmithKline LLC Benzodiazepine bromodomain inhibitor
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
DK2496582T3 (en) 2009-11-05 2016-03-21 Glaxosmithkline Llc Benzodiazepine-BROMDOMAeNEINHIBITOR.
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
KR20130069640A (ko) 2010-04-23 2013-06-26 키네타, 인크. 항-바이러스 화합물
WO2011143660A2 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
US9301962B2 (en) 2010-05-14 2016-04-05 Baylor College Of Medicine Male contraceptive compositions and methods of use
CA2799373A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
WO2011143669A2 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc Compositions and methods for treating neoplasia, inflammatory disease and other disorders
EP2585465B1 (en) 2010-06-22 2014-11-12 GlaxoSmithKline LLC Benzotriazolodiazepine compounds inhibitors of bromodomains
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
EP2673269A1 (en) 2011-02-09 2013-12-18 F.Hoffmann-La Roche Ag Heterocyclic compounds as pi3 kinase inhibitors
CA2828212A1 (en) 2011-02-23 2012-08-30 Shiraz Mujtaba Inhibitors of bromodomains as modulators of gene expression
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106743D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
WO2012151512A2 (en) 2011-05-04 2012-11-08 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
US9328117B2 (en) 2011-06-17 2016-05-03 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
CA2840380A1 (en) 2011-06-24 2012-12-27 Dana-Farber Cancer Institute, Inc. Selective inhibitors of histone deacetylase isoform 6 and methods thereof
JP2013010719A (ja) 2011-06-30 2013-01-17 Dainippon Sumitomo Pharma Co Ltd ベンズイミダゾロンおよびオキシインドール誘導体ならびにそれらの医薬用途
EP2736528A4 (en) 2011-07-29 2015-03-18 Philadelphia Children Hospital COMPOSITIONS AND METHODS FOR THE TREATMENT OF HIV
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
HUE036301T2 (hu) 2011-08-31 2018-06-28 Otsuka Pharma Co Ltd Kinolin vegyület
DE102011082013A1 (de) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
US9012642B2 (en) 2011-09-22 2015-04-21 Viiv Healthcare Uk Limited Pyrrolopyridinone compounds and methods for treating HIV
CN103857391B (zh) 2011-09-30 2016-06-08 沈阳蓝桑医药生物技术研发有限公司 含有瑞利格内酯的药物组合物及其应用
AU2012330885B2 (en) 2011-11-01 2016-10-06 Resverlogix Corp. Oral immediate release formulations for substituted quinazolinones
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20150133434A1 (en) 2012-03-28 2015-05-14 The J. David Gladstone Institutes Compositions and Methods for Reactivating Latent Immunodeficiency Virus
US20130281399A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281398A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281397A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281396A1 (en) * 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
JP5989229B2 (ja) 2012-04-20 2016-09-07 アッヴィ・インコーポレイテッド イソインドロン誘導体
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
HK1208681A1 (zh) 2012-06-12 2016-03-11 Abbvie Inc. 吡啶酮和噠嗪酮衍生物
KR20150045423A (ko) 2012-06-25 2015-04-28 온코에틱스 에스에이 티에노트리아졸로디아제핀 화합물을 사용하여 림프종을 치료하는 방법
US9610332B2 (en) 2012-07-18 2017-04-04 Massachusetts Institute Of Technology Compositions and methods for modulating BRD4 bioactivity
ES2628005T3 (es) 2012-08-16 2017-08-01 Bayer Pharma Aktiengesellschaft 2,3-Benzodiazepinas
JP2015524847A (ja) 2012-08-16 2015-08-27 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ 小細胞肺がんを治療するためのベンゾジアゼピン
KR20150100613A (ko) 2012-09-28 2015-09-02 온코에틱스 게엠베하 티에노트리아졸로디아제핀 화합물을 함유하는 약제학적 제제
US9663523B2 (en) 2012-09-28 2017-05-30 Bayer Pharma Aktiengesellschaft BET protein-inhibiting 5-aryltriazoleazepines
US9422290B2 (en) 2012-11-13 2016-08-23 Boehringer Ingelheim International Gmbh Triazolopyridazine
ES2625945T3 (es) 2012-11-14 2017-07-21 Glaxosmithkline Llc Tieno[3,2-c]piridin-4(5H)-onas como inhibidores de bet
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
WO2014095775A1 (de) 2012-12-20 2014-06-26 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydrochinoxalinone
CN105229002A (zh) 2012-12-20 2016-01-06 拜耳医药股份有限公司 抑制bet蛋白的二氢吡啶并吡嗪酮
WO2014096965A2 (en) 2012-12-21 2014-06-26 Rvx Therapeutics Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
EP2961747B1 (en) 2013-02-27 2017-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
EP2970312B1 (en) 2013-03-11 2017-11-15 The Regents of The University of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
JP2016516701A (ja) 2013-03-11 2016-06-09 アッヴィ・インコーポレイテッド 縮合四環系ブロモドメイン阻害剤
AU2014249025A1 (en) 2013-03-11 2015-09-17 Abbvie Inc. Bromodomain inhibitors
SG11201507383WA (en) 2013-03-12 2015-10-29 Abbvie Inc Dihydro-pyrrolopyridinone bromodomain inhibitors
EP2970193B1 (en) 2013-03-12 2018-07-25 AbbVie Inc. Pyrrole amide inhibitors
WO2014139324A1 (en) 2013-03-12 2014-09-18 Abbvie Inc. Tetracyclic bromodomain inhibitors
NZ710765A (en) 2013-03-14 2020-05-29 Glaxosmithkline Ip No 2 Ltd 2,3-disubstituted 1 -acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
AU2014230816B9 (en) 2013-03-14 2016-12-15 Glaxosmithkline Intellectual Property (No.2) Limited Furopyridines as bromodomain inhibitors
WO2014159837A1 (en) 2013-03-14 2014-10-02 Convergene Llc Methods and compositions for inhibition of bromodomain-containing proteins
WO2014159392A1 (en) 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
CA2903881C (en) 2013-03-15 2021-05-18 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
EP2968311A4 (en) 2013-03-15 2016-07-20 Epigenetix Inc OXAZOLO [5,4-C] CHINOLIN-2-ON COMPOUNDS AS BROMODOMENA INHIBITORS
WO2014145051A1 (en) 2013-03-15 2014-09-18 Jiazhong Zhang Heterocyclic compounds and uses thereof
WO2014154762A1 (en) 2013-03-27 2014-10-02 Boehringer Ingelheim International Gmbh Dihydroquinazolinone analogues as brd4 inhibitors
US9102684B2 (en) 2013-03-27 2015-08-11 Boehringer Ingelheim International Gmbh Indolinone analogues
TWI530499B (zh) 2013-03-28 2016-04-21 吉李德科學股份有限公司 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類
US10435364B2 (en) 2013-04-17 2019-10-08 Albert Ludwigs Universität Freiburg Compounds for use as bromodomain inhibitors
MX366623B (es) 2013-04-26 2019-07-16 Beigene Ltd 5-(3,5-dimetilisoxazol-4-il)indolina-2-onas sustituidas.
TWI527811B (zh) * 2013-05-09 2016-04-01 吉李德科學股份有限公司 作爲溴結構域抑制劑的苯並咪唑衍生物
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
JP6373978B2 (ja) 2013-05-27 2018-08-15 ノバルティス アーゲー イミダゾピロリジノン誘導体および疾患の処置におけるその使用
CN105246896B (zh) 2013-05-28 2017-09-08 诺华股份有限公司 吡唑并吡咯烷‑4‑酮衍生物及其在治疗疾病中的用途
CA2912986A1 (en) 2013-05-28 2014-12-04 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease
JP2016521722A (ja) 2013-06-17 2016-07-25 バイエル ファーマ アクチエンゲゼルシャフト 置換フェニル−２，３−ベンゾジアゼピン
ITMI20130991A1 (it) 2013-06-17 2014-12-18 Industrie De Nora Spa Sistema per la misurazione di correnti presenti sugli elettrodi in celle elettrolitiche interconnesse.
CA2915561C (en) 2013-06-21 2020-09-22 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
KR102307566B1 (ko) 2013-06-21 2021-10-05 제니쓰 에피제네틱스 리미티드 신규한 바이사이클릭 브로모도메인 억제제
RU2016102647A (ru) 2013-06-28 2017-08-01 Эббви Инк. Ингибиторы бромодомена
AR096758A1 (es) 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
CA2917319A1 (en) 2013-07-08 2015-01-15 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
PL3022191T3 (pl) 2013-07-16 2017-08-31 Basf Se Chwastobójcze azyny
CA2918910A1 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
KR101672096B1 (ko) 2013-09-30 2016-11-02 주식회사 엘지화학 헤테로환 화합물 및 이를 포함하는 유기 발광 소자
SG11201602996RA (en) 2013-10-18 2016-05-30 Celgene Quanticel Res Inc Bromodomain inhibitors
WO2015081246A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
CN105939996A (zh) 2013-12-09 2016-09-14 艾伯维公司 用作布罗莫结构域抑制剂的二氢吡啶酮和二氢哒嗪酮衍生物
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
WO2015095445A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
MA39172B1 (fr) 2014-01-09 2018-10-31 Orion Corp Dérivés bicycliques hétérocycliques comme inhibiteurs de bromodomaines
WO2015131005A1 (en) 2014-02-28 2015-09-03 The Regents Of The University Of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
JP6538077B2 (ja) 2014-04-23 2019-07-03 ビーエーエスエフ ソシエタス・ヨーロピアＢａｓｆ Ｓｅ 除草剤としてのジアミノトリアジン化合物
FI3674302T3 (fi) 2014-04-23 2023-04-27 Incyte Holdings Corp 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONEJA JA PYRATSOLO[3,4-c]PYRIDIN-7(6H)-ONEJA BET-PROTEIINIEN INHIBIITTOREINA
AR100154A1 (es) 2014-04-23 2016-09-14 Takeda Pharmaceuticals Co Compuesto heterocíclico que contiene nitrógeno
AU2015252844A1 (en) 2014-05-02 2016-11-03 Kay NOEL Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds
AU2015252940A1 (en) 2014-05-02 2016-11-17 Kay NOEL Method of treating resistant non-Hodgkin lymphoma, medulloblastoma, and/or ALK+non-small cell lung cancer using thienotriazolodiazepine compounds
KR20170002610A (ko) 2014-05-08 2017-01-06 온코에틱스 게엠베하 티에노트리아졸로디아제핀 화합물을 사용한 삼중 음성 유방암의 치료 방법
WO2015169953A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating glioma using thienotriazolodiazepine compounds
US10065951B2 (en) 2014-05-30 2018-09-04 Icahn School Of Medicine At Mount Sinai Small molecule transcription modulators of bromodomains
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
CN105029258A (zh) 2014-09-20 2015-11-11 林静 一种多味橄榄的制作方法
MA40943A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
CA2974153A1 (en) 2015-02-03 2016-08-11 Trillium Therapeutics Inc. Fluorinated imidazo[4,5-c]quinoline derivatives as inhibitors of bromodomain containing proteins
WO2016186453A1 (en) 2015-05-20 2016-11-24 Kainos Medicine, Inc. Quinoline derivatives as bromodomain inhibitors
JP6614585B2 (ja) 2015-05-29 2019-12-04 塩野義製薬株式会社 Ｈｉｖ複製阻害作用を有する含窒素３環性誘導体
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
CN105254635A (zh) 2015-10-30 2016-01-20 中国药科大学 一类咪唑并吡嗪类化合物及其药物组合物和用途
US20170127985A1 (en) 2015-11-11 2017-05-11 Medtronic Minimed, Inc. Sensor set
WO2017103670A1 (en) 2015-12-14 2017-06-22 Zenith Epigenetics Lid. 1h-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridinyl heterocyclic bet bromodomain inhibitors
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
CN108770356A (zh) 2016-02-05 2018-11-06 正大天晴药业集团股份有限公司 溴区结构域蛋白抑制剂的三环类化合物及其制备、药物组合物和用途
DK3472157T3 (da) 2016-06-20 2023-05-01 Incyte Corp Krystallinske faste former af en bet-inhibitor
CN108069958A (zh) 2016-11-10 2018-05-25 凯惠科技发展(上海)有限公司 一种含氮杂环类化合物、其制备方法、药物组合物及应用

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112679520A (zh) * 2018-08-24 2021-04-20 杭州阿诺生物医药科技有限公司 Sting激动剂及其制备方法
CN112679520B (zh) * 2018-08-24 2022-03-11 杭州阿诺生物医药科技有限公司 Sting激动剂及其制备方法

Also Published As

Publication number Publication date
JP2017526731A (ja) 2017-09-14
US20180222920A1 (en) 2018-08-09
EP3194406A1 (en) 2017-07-26
US9527864B2 (en) 2016-12-27
US20170158710A1 (en) 2017-06-08
JP6599979B2 (ja) 2019-10-30
WO2016044130A1 (en) 2016-03-24
US10227359B2 (en) 2019-03-12
US20190233435A1 (en) 2019-08-01
US20160075721A1 (en) 2016-03-17
EP3194406B8 (en) 2021-03-31
ES2855225T3 (es) 2021-09-23
US10618910B2 (en) 2020-04-14
US9834565B2 (en) 2017-12-05
TWI712603B (zh) 2020-12-11
EP3194406B1 (en) 2020-12-16

Similar Documents

Publication Publication Date Title
PH12019502318A1 (en) Trycyclic heterocycles as bet protein inhibitors
CY1126052T1 (el) 1η-πυρρολο[2,3-c]πυριδιν-7(6η)-ονες και πυραζολο[3,4-c]πυριδιν-7(6η)- ονες ως αναστολεις των bet πρωτεϊνων
TW201613935A (en) Tricyclic heterocycles as BET protein inhibitors
PH12019502810A1 (en) Bicyclic heterocycles as fgfr inhibitors
PH12016501463B1 (en) Diaryl macrocycles as modulators of protein kinases
NZ731467A (en) Anti-tim3 antibodies and methods of use
HK1245246A1 (zh) 作為溴域抑制劑的取代吡啶酮
HK1245247A1 (zh) 溴結構域的抑制劑
EA201790259A1 (ru) СОСТАВ ТАБЛЕТОК 2-ФТОР-N-МЕТИЛ-4-[7-(ХИНОЛИН-6-ИЛМЕТИЛ)ИМИДАЗО[1,2-b][1,2,4]ТРИАЗИН-2-ИЛ]БЕНЗАМИДА
MX2015012428A (es) Tratamiento contra enfermedades mediadas th2 por inhibicion de bromodominios.
HK40028183A (zh) 抗-b7h3抗體用於治療中樞神經系統癌症的用途