SG11201506924YA - Tricyclic heterocycles as bet protein inhibitors - Google Patents

Tricyclic heterocycles as bet protein inhibitors

Info

Publication number
SG11201506924YA
SG11201506924YA SG11201506924YA SG11201506924YA SG11201506924YA SG 11201506924Y A SG11201506924Y A SG 11201506924YA SG 11201506924Y A SG11201506924Y A SG 11201506924YA SG 11201506924Y A SG11201506924Y A SG 11201506924YA SG 11201506924Y A SG11201506924Y A SG 11201506924YA
Authority
SG
Singapore
Prior art keywords
protein inhibitors
bet protein
tricyclic heterocycles
tricyclic
heterocycles
Prior art date
Application number
SG11201506924YA
Inventor
Andrew P Combs
Richard B Sparks
Thomas P Maduskuie Jr
James D Rodgers
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 SG11201506924YA publication Critical patent/SG11201506924YA/en

Links

Classifications

    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/06—Peri-condensed systems
    • 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
    • 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
    • C07D498/12—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 three hetero rings
    • C07D498/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
SG11201506924YA 2013-03-15 2014-03-14 Tricyclic heterocycles as bet protein inhibitors SG11201506924YA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361794812P 2013-03-15 2013-03-15
PCT/US2014/027872 WO2014143768A1 (en) 2013-03-15 2014-03-14 Tricyclic heterocycles as bet protein inhibitors

Publications (1)

Publication Number Publication Date
SG11201506924YA true SG11201506924YA (en) 2015-09-29

Family

ID=50639971

Family Applications (2)

Application Number Title Priority Date Filing Date
SG11201506924YA SG11201506924YA (en) 2013-03-15 2014-03-14 Tricyclic heterocycles as bet protein inhibitors
SG10201707487VA SG10201707487VA (en) 2013-03-15 2014-03-14 Tricyclic heterocycles as bet protein inhibitors

Family Applications After (1)

Application Number Title Priority Date Filing Date
SG10201707487VA SG10201707487VA (en) 2013-03-15 2014-03-14 Tricyclic heterocycles as bet protein inhibitors

Country Status (25)

Country Link
US (6) US9227985B2 (en)
EP (2) EP2970282B1 (en)
JP (3) JP6243003B2 (en)
KR (2) KR102216288B1 (en)
CN (2) CN109593096B (en)
AR (1) AR095326A1 (en)
AU (1) AU2014228175B2 (en)
BR (1) BR112015022942B1 (en)
CA (1) CA2903881C (en)
CL (1) CL2015002734A1 (en)
CR (1) CR20150513A (en)
EA (2) EA038494B1 (en)
EC (1) ECSP15043772A (en)
ES (2) ES2755827T3 (en)
HK (1) HK1218650A1 (en)
IL (2) IL241158B (en)
MX (2) MX366703B (en)
NZ (1) NZ712453A (en)
PE (1) PE20151990A1 (en)
PH (2) PH12015502157A1 (en)
SG (2) SG11201506924YA (en)
TW (2) TWI667238B (en)
UA (1) UA119848C2 (en)
WO (1) WO2014143768A1 (en)
ZA (2) ZA201507255B (en)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
CA2895905A1 (en) 2012-12-21 2014-06-26 Zenith Epigenetics Corp. Novel heterocyclic compounds as bromodomain inhibitors
WO2014110574A1 (en) 2013-01-14 2014-07-17 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
ES2790419T3 (en) 2013-01-15 2020-10-27 Incyte Holdings Corp Thiazolecarboxamide and pyridinecarboxamide compounds useful as PIM kinase inhibitors
SG11201506924YA (en) * 2013-03-15 2015-09-29 Incyte Corp Tricyclic heterocycles as bet protein inhibitors
BR112015031073B1 (en) 2013-06-21 2022-11-29 Zenith Epigenetics Ltd BICYCLIC BROMODIMANIUM INHIBITORS AND PHARMACEUTICAL COMPOSITION CONTAINING SAID COMPOUNDS
US9662311B2 (en) 2013-06-21 2017-05-30 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
WO2015015318A2 (en) 2013-07-31 2015-02-05 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
US9556197B2 (en) 2013-08-23 2017-01-31 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as pim kinase 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
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
ES2942723T3 (en) 2014-04-23 2023-06-06 Incyte Holdings Corp 1H-pyrrolo[2,3-C]pyridin-7(6H)-ones and pyrazolo[3,4-C]pyridin-7(6H)-ones as inhibitors of BET proteins
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
WO2016044130A1 (en) * 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
AU2015333689A1 (en) 2014-10-14 2017-05-25 The Regents Of The University Of California Use of CDK9 and BRD4 inhibitors to inhibit inflammation
WO2016087942A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridines as bromodomain inhibitors
CA2966298A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
WO2016092375A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Corp. Substituted heterocycles as bromodomain inhibitors
WO2016097863A1 (en) 2014-12-17 2016-06-23 Zenith Epigenetics Corp. Inhibitors of bromodomains
CN111662226B (en) * 2015-01-28 2022-03-18 中国科学院广州生物医药与健康研究院 2-oxo-1, 2-dihydrobenzo [ cd ] indole compound
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
US9540347B2 (en) 2015-05-29 2017-01-10 Incyte Corporation Pyridineamine compounds useful as Pim kinase inhibitors
US10065970B2 (en) 2015-09-08 2018-09-04 Genentech, Inc. Tricyclic PI3K inhibitor compounds and methods of use
TWI734699B (en) 2015-09-09 2021-08-01 美商英塞特公司 Salts of a pim kinase inhibitor
US9920032B2 (en) 2015-10-02 2018-03-20 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
WO2017133681A1 (en) * 2016-02-05 2017-08-10 正大天晴药业集团股份有限公司 Tricyclic compound for bromodomain-containing protein inhibitor and preparation, pharmaceutical composition, and application thereof
US10517877B2 (en) 2016-03-30 2019-12-31 Wisconsin Alumni Research Foundation Compounds and methods for modulating frataxin expression
CN114369091A (en) 2016-06-20 2022-04-19 因赛特公司 Crystalline solid forms of BET inhibitors
US11759533B2 (en) 2017-03-29 2023-09-19 Wisconsin Alumni Research Foundation Methods and compositions for modulating gene expression
TW201924683A (en) 2017-12-08 2019-07-01 美商英塞特公司 Low dose combination therapy for treatment of myeloproliferative neoplasms
US20220257600A1 (en) * 2018-06-20 2022-08-18 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with a jak or other kinase inhibitor
CN111386275B (en) * 2018-08-24 2023-03-10 杭州阿诺生物医药科技有限公司 High activity STING protein agonists
CN110879294A (en) * 2018-09-05 2020-03-13 成都市第三人民医院 Use of protein marker in product for diagnosing irritable bowel syndrome and kit for diagnosing irritable bowel syndrome
CN113195473B (en) * 2018-12-14 2022-11-22 江苏恒瑞医药股份有限公司 Tricyclic compound as STING agonist and preparation method and medical application thereof
CN111349094B (en) * 2020-04-23 2021-02-02 杭州师范大学 6H-imidazo [4,5,1-ij ] quinolone and synthesis method and application thereof
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US20240140963A1 (en) * 2021-02-03 2024-05-02 Tuojie Biotech (Shanghai) Co., Ltd. Fused tricyclic cyclin-dependent kinase inhibitor, and preparation method therefor and pharmaceutical use thereof
CA3228524A1 (en) * 2021-08-10 2023-02-16 Bryan William STROUSE Momelotinib combination therapy
CN113975278B (en) * 2021-10-29 2023-04-07 中国科学院昆明动物研究所 Application of bromocriptine in preparation of product for treating African swine fever

Family Cites Families (161)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59170313A (en) 1983-03-14 1984-09-26 Kurimoto Iron Works Ltd Screen gate
JPS6085739U (en) 1983-11-18 1985-06-13 クラリオン株式会社 Pinch roller device in tape recorder
JPH0314566A (en) * 1989-06-09 1991-01-23 Sankyo Co Ltd Benzimidazole derivative
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 (en) 1993-10-04 1995-11-24 Synthelabo Piperidine derivatives, their preparation and their therapeutic use.
GB9410469D0 (en) * 1994-05-25 1994-07-13 Erba Farmitalia Imidazolylalkyl derivatives of imidazo (5,1-c) (1,4) benzoxazin-1-one and process for their preparation
FR2731708B1 (en) * 1995-03-13 1997-04-30 Synthelabo PIPERIDINE DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR THERAPEUTIC APPLICATION
FR2747678B1 (en) 1996-04-22 1998-05-22 Synthelabo COMPOUNDS DERIVED FROM IMIDAZOBENZOXAZINE, PROCESSES FOR THEIR PREPARATION AND THERAPEUTIC USES
US6287693B1 (en) 1998-02-25 2001-09-11 John Claude Savoir Stable shaped particles of crystalline organic compounds
DK1274430T3 (en) 2000-04-21 2006-02-13 Pharmacia & Upjohn Co Llc Cabergoline for the treatment of fibromyalgia and chronic fatigue syndrome
NZ522783A (en) 2000-06-28 2004-07-30 Smithkline Beecham P Wet milling process for pharmaceuticals with agitator or chamber having nylon with internal lubricant
SK1582003A3 (en) * 2000-08-08 2003-08-05 Sanofi Synthelabo Benzimidazole derivatives, preparation and therapeutic use thereof
FR2816619B1 (en) 2000-11-15 2003-01-31 Sanofi Synthelabo BENZIMIDAZOLE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
US6919334B2 (en) * 2002-09-12 2005-07-19 Wyeth Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine
WO2004047755A2 (en) 2002-11-22 2004-06-10 Japan Tobacco Inc. Fused bicyclic nitrogen-containing heterocycles
EP1462103A1 (en) 2003-03-25 2004-09-29 Faust Pharmaceuticals NO donors, combination products and uses as modulators of neurotransmitter release
EP1719761A4 (en) 2004-02-23 2007-10-10 Dainippon Sumitomo Pharma Co Novel heterocyclic compound
US7713954B2 (en) 2004-09-30 2010-05-11 Roche Palo Alto Llc Compositions and methods for treating cognitive disorders
DE102005011058A1 (en) * 2005-03-10 2006-09-14 Merck Patent Gmbh Substituted tetrahydro-pyrrolo-quinoline derivatives
AU2006279034A1 (en) * 2005-08-05 2007-02-15 Astrazeneca Ab Tricyclic benzimidazoles and their use as metabotropic glutamate receptor modulators
US8975259B2 (en) 2007-04-27 2015-03-10 University Of Rochester Compositions and methods for inhibiting G protein signaling
US8633186B2 (en) 2007-06-08 2014-01-21 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
US9603848B2 (en) 2007-06-08 2017-03-28 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
JP5478262B2 (en) 2007-12-28 2014-04-23 田辺三菱製薬株式会社 Anticancer drug
DE102008052618A1 (en) 2008-10-21 2010-04-22 Henkel Ag & Co. Kgaa Tricyclic aldehydes and C, H-acidic compounds
JP5730281B2 (en) 2009-03-27 2015-06-10 武田薬品工業株式会社 Poly (ADP-ribose) polymerase (PARP) inhibitor
TW201103941A (en) * 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
TW201105681A (en) * 2009-06-10 2011-02-16 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
JP5524343B2 (en) 2009-11-05 2014-06-18 グラクソスミスクライン エルエルシー Benzodiazepine bromodomain inhibitor
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EP2955524A3 (en) 2009-11-05 2016-03-23 GlaxoSmithKline LLC Novel process
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EA023441B1 (en) 2009-11-05 2016-06-30 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Benzodiazepine bromodomain inhibitor
MX2012012353A (en) 2010-04-23 2013-02-07 Kineta Inc Anti-viral compounds.
CN103119160B (en) 2010-05-14 2016-06-01 达那-法伯癌症研究所 For regulating compositions and the method for metabolism
BR122014024883A2 (en) 2010-05-14 2019-08-20 Dana-Farber Cancer Institute, Inc. COMPOUNDS IN NEOPLASIA TREATMENT
CN105582014B (en) 2010-05-14 2019-06-14 达那-法伯癌症研究所 For treating the composition and method of leukaemia
CN103180318B (en) 2010-05-14 2017-05-10 达那-法伯癌症研究所 male contraceptive compositions and methods of use
JP5844358B2 (en) 2010-06-22 2016-01-13 グラクソスミスクライン エルエルシー Bromodomain inhibitors containing benzotriazolodiazepine compounds
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
AR084070A1 (en) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc BROMODOMINIUM INHIBITORS AND USES OF THE SAME
EP2673269A1 (en) 2011-02-09 2013-12-18 F.Hoffmann-La Roche Ag Heterocyclic compounds as pi3 kinase inhibitors
EP2677865A4 (en) 2011-02-23 2015-04-22 Icahn School Med Mount Sinai Inhibitors of bromodomains as modulators of gene expression
US9090628B2 (en) * 2011-03-21 2015-07-28 Genentech, Inc. Benzoxazepin compounds selective for PI3K P110 delta and methods of use
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
EP2705039B1 (en) 2011-05-04 2017-07-26 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
WO2012178208A2 (en) 2011-06-24 2012-12-27 The Trustees Of The Stevens Institute Of Technology Selective inhibitors of histone deacetylase isoform 6 and methods thereof
JP2013010719A (en) 2011-06-30 2013-01-17 Dainippon Sumitomo Pharma Co Ltd Benzimidazolone and oxindole derivative, and pharmaceutical application of them
JP2014524409A (en) 2011-07-29 2014-09-22 ザ・チルドレンズ・ホスピタル・オブ・フィラデルフィア 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
WO2013033270A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution, 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
CA2845459C (en) 2011-08-31 2019-08-27 Otsuka Pharmaceutical Co., Ltd. Quinolone compound and antimicrobial use thereof
DE102011082013A1 (en) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-thieno [3,2-f] [1,2,4] triazolo [4,3-a] [1,4] diazepines
EP2757887B1 (en) 2011-09-22 2017-04-26 VIIV Healthcare UK Limited Pyrrolopyridinone compounds and methods for treating hiv
WO2013044511A1 (en) 2011-09-30 2013-04-04 沈阳蓝桑医药生物技术研发有限公司 Pharmaceutical composition containing riligustilide and use thereof
EP2771340B1 (en) 2011-10-25 2016-04-13 Sanofi 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
DK2773354T3 (en) 2011-11-01 2019-08-05 Resverlogix Corp ORAL FORMS WITH IMMEDIATE RELEASE FOR SUBSTITUTED QUINAZOLINONS
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
EP2830629A4 (en) 2012-03-28 2016-01-20 Icahn School Of Medicine Mount Sinai 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
US20130281396A1 (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
CA2870931A1 (en) 2012-04-20 2013-10-24 Abbvie Inc. Isoindolone derivatives
US9624244B2 (en) 2012-06-06 2017-04-18 Constellation Pharmaceuticals, Inc. Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof
TWI602820B (en) 2012-06-06 2017-10-21 星宿藥物公司 Bromodomain inhibitors and uses thereof
CA2874953A1 (en) 2012-06-12 2013-12-19 Abbvie Inc. Pyridinone and pyridazinone derivatives
JP6265979B2 (en) 2012-06-25 2018-01-24 オンコエシックス ゲーエムベーハー Method of treating lymphoma using thienotriazolodiazepine compounds
US9610332B2 (en) 2012-07-18 2017-04-04 Massachusetts Institute Of Technology Compositions and methods for modulating BRD4 bioactivity
KR20150041787A (en) 2012-08-16 2015-04-17 바이엘 파마 악티엔게젤샤프트 2,3-benzodiazepines
WO2014028547A1 (en) 2012-08-16 2014-02-20 Glaxosmithkline Llc Benzodiazepines for treating small cell lung cancer
JP2015531365A (en) 2012-09-28 2015-11-02 オンコエシックス エスエー Pharmaceutical formulations containing thienotriazolodiazepine compounds
WO2014048945A1 (en) 2012-09-28 2014-04-03 Bayer Pharma Aktiengesellschaft Bet protein-inhibiting 5-aryl triazole azepines
SI2917181T1 (en) 2012-11-09 2020-01-31 Mmv Medicines For Malaria Venture Heteroaryl derivatives and uses thereof
US9422290B2 (en) 2012-11-13 2016-08-23 Boehringer Ingelheim International Gmbh Triazolopyridazine
ES2625945T3 (en) 2012-11-14 2017-07-21 Glaxosmithkline Llc Thieno [3,2-c] pyridin-4 (5H) -ones as bet inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
EP2935261A1 (en) 2012-12-20 2015-10-28 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydroquinoxalinones
JP2016504990A (en) 2012-12-20 2016-02-18 バイエル ファーマ アクチエンゲゼルシャフト BET protein inhibitory dihydropyridopyrazinone
CA2895905A1 (en) 2012-12-21 2014-06-26 Zenith Epigenetics Corp. 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
CA2903463A1 (en) 2013-03-11 2014-10-09 The Regents Of The University Of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
AU2014249034A1 (en) 2013-03-11 2015-09-24 Abbvie Inc. Fused tetracyclic bromodomain inhibitors
MX2015012005A (en) 2013-03-11 2016-04-04 Abbvie Inc Bromodomain inhibitors.
TW201443051A (en) 2013-03-12 2014-11-16 Abbvie Inc Dihydro-pyrrolopyridinone inhibitors
US10035800B2 (en) 2013-03-12 2018-07-31 Abbvie Inc. Substituted 1,4,10-triazadibenzo[cd,f]azulenes, substituted 1,4,5,10-tetraazadibenzo[cd,f]azulenes and substituted 1,4,5,7,10-pentaazadibenzo[cd,f]azulenes as bromodomain inhibitors
AU2014248647A1 (en) 2013-03-12 2015-10-01 Abbvie Inc. Pyrrole amide inhibitors
KR101780784B1 (en) 2013-03-14 2017-09-21 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 2,3-disubstituted 1-acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
ES2654362T3 (en) 2013-03-14 2018-02-13 Glaxosmithkline Intellectual Property (No. 2) Limited Furopyridines as bromodomain inhibitors
US9695179B2 (en) 2013-03-14 2017-07-04 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
SG11201506924YA (en) 2013-03-15 2015-09-29 Incyte Corp Tricyclic heterocycles as bet protein inhibitors
JP2016519660A (en) 2013-03-15 2016-07-07 エピジェネティクス・インコーポレイテッド Oxazolo [5,4-c] quinolin-2-one compounds as bromodomain inhibitors
DK2970265T3 (en) 2013-03-15 2018-10-01 Plexxikon Inc HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
JP6370368B2 (en) 2013-03-27 2018-08-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Indolinone analogs as BRD4 inhibitors
WO2014154762A1 (en) 2013-03-27 2014-10-02 Boehringer Ingelheim International Gmbh Dihydroquinazolinone analogues as brd4 inhibitors
TWI530499B (en) 2013-03-28 2016-04-21 吉李德科學股份有限公司 Benzimidazolone derivatives as bromodomain inhibitors
WO2014170350A1 (en) 2013-04-17 2014-10-23 Albert Ludwigs Universität Freiburg Compounds for use as bromodomain inhibitors
WO2014173241A1 (en) 2013-04-26 2014-10-30 Beigene, Ltd. Substituted5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
TWI527811B (en) 2013-05-09 2016-04-01 吉李德科學股份有限公司 Benzimidazole derivatives as bromodomain inhibitors
JP6373978B2 (en) 2013-05-27 2018-08-15 ノバルティス アーゲー Imidazopyrrolidinone derivatives and their use in the treatment of diseases
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
JP6403761B2 (en) 2013-05-28 2018-10-10 ノバルティス アーゲー Pyrazolo-pyrrolidin-4-one derivatives and their use in the treatment of diseases
PT3004108T (en) 2013-05-28 2018-01-24 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease
ITMI20130991A1 (en) 2013-06-17 2014-12-18 Industrie De Nora Spa CURRENT MEASUREMENT SYSTEM PRESENT IN ELECTRODES IN INTERCONNECTED ELECTROLYTIC CELLS.
JP2016521722A (en) 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 Substituted phenyl-2,3-benzodiazepine
BR112015031073B1 (en) 2013-06-21 2022-11-29 Zenith Epigenetics Ltd BICYCLIC BROMODIMANIUM INHIBITORS AND PHARMACEUTICAL COMPOSITION CONTAINING SAID COMPOUNDS
US9662311B2 (en) 2013-06-21 2017-05-30 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
AR096758A1 (en) 2013-06-28 2016-02-03 Abbvie Inc BROMODOMINIUM CRYSTAL INHIBITORS
JP2016525503A (en) 2013-06-28 2016-08-25 アッヴィ・インコーポレイテッド Bromodomain inhibitor
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
MX363518B (en) 2013-07-16 2019-03-26 Basf Se Herbicidal azines.
WO2015013635A2 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
KR101672096B1 (en) 2013-09-30 2016-11-02 주식회사 엘지화학 Heterocyclic compound and organic light emitting device comprising the same
LT3057586T (en) 2013-10-18 2020-03-10 Celgene Quanticel Research, Inc. Bromodomain 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
US20150148372A1 (en) 2013-11-26 2015-05-28 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015089075A1 (en) 2013-12-09 2015-06-18 Abbvie Inc. Dihydropyridinone and dihydropyridazinone derivatives useful as bromodomain inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
EP3083559B1 (en) 2013-12-20 2021-03-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
SI3092227T1 (en) 2014-01-09 2018-10-30 Orion Corporation Bicyclic heterocyclic derivatives as bromodomain inhibitors
CA2940554A1 (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
CR20160545A (en) 2014-04-23 2017-03-31 Basf Se DIAMINOTRIAZINE COMPOUNDS AS HERBICIDES
ES2942723T3 (en) 2014-04-23 2023-06-06 Incyte Holdings Corp 1H-pyrrolo[2,3-C]pyridin-7(6H)-ones and pyrazolo[3,4-C]pyridin-7(6H)-ones as inhibitors of BET proteins
TN2016000455A1 (en) 2014-04-23 2018-04-04 Takeda Pharmaceuticals Co Isoindoline-1-one derivatives as cholinergic muscarinic m1 receptor positive alloesteric modulator activity for the treatment of alzheimers disease.
CN106687117A (en) 2014-05-02 2017-05-17 翁科埃斯克斯有限公司 Method of treating resistant non-hodgkin lymphoma, medulloblastoma, and/or ALK+ non-small cell lung cancer using thienotriazolodiazepine compounds
MX2016014301A (en) 2014-05-02 2017-04-27 Oncoethix Gmbh Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds.
WO2015169953A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating glioma using thienotriazolodiazepine compounds
CA2947970A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating triple-negative breast cancer using thienotriazolodiazepine compounds
EP3148543B1 (en) 2014-05-30 2020-04-08 Icahn School of Medicine at Mount Sinai Small molecule transcription modulators of bromodomains
CA2952830C (en) 2014-06-20 2022-11-01 Constellation Pharmaceuticals, Inc. Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
WO2016044130A1 (en) 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
TWI744218B (en) 2014-10-24 2021-11-01 美商必治妥美雅史谷比公司 Indole carboxamide compounds
MA40943A (en) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc SUBSTITUTED PYRROLOPYRIDINES USED AS BROMODOMA INHIBITORS
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
US10494380B2 (en) 2015-05-29 2019-12-03 Shionogi & Co., Ltd. Nitrogen-containing tricyclic derivatives having HIV replication inhibitory activity
CN105039258B (en) 2015-07-03 2018-04-17 北京大学 Method and composition by non-neuronal cell reprogramming for neuron cell
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN105254635A (en) 2015-10-30 2016-01-20 中国药科大学 Imidazo pyrazine compound, medicine composition of imidazo pyrazine compound and purpose of imidazo pyrazine compound
US20170127985A1 (en) 2015-11-11 2017-05-11 Medtronic Minimed, Inc. Sensor set
US20190263799A1 (en) 2015-12-14 2019-08-29 Zenith Epigenetics Ltd. 1h-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridinyl heterocyclic bet bromodomain inhibitors
US10519151B2 (en) 2016-01-28 2019-12-31 Neomed Institute Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals
WO2017133681A1 (en) 2016-02-05 2017-08-10 正大天晴药业集团股份有限公司 Tricyclic compound for bromodomain-containing protein inhibitor and preparation, pharmaceutical composition, and application thereof
CN114369091A (en) 2016-06-20 2022-04-19 因赛特公司 Crystalline solid forms of BET inhibitors
CN108069958A (en) 2016-11-10 2018-05-25 凯惠科技发展(上海)有限公司 A kind of nitrogen-containing hetero cyclics, its preparation method, pharmaceutical composition and application

Also Published As

Publication number Publication date
EA035469B1 (en) 2020-06-22
US20140275030A1 (en) 2014-09-18
US9624241B2 (en) 2017-04-18
JP6243003B2 (en) 2017-12-06
US11498926B2 (en) 2022-11-15
US20200131195A1 (en) 2020-04-30
JP6529546B2 (en) 2019-06-12
PH12019502318A1 (en) 2020-12-07
EP2970282A1 (en) 2016-01-20
UA119848C2 (en) 2019-08-27
CL2015002734A1 (en) 2016-03-28
JP6712344B2 (en) 2020-06-17
US20210188872A1 (en) 2021-06-24
US9227985B2 (en) 2016-01-05
MX2015013149A (en) 2016-01-08
ES2755827T3 (en) 2020-04-23
BR112015022942B1 (en) 2022-02-22
ZA202001242B (en) 2021-08-25
TWI667238B (en) 2019-08-01
EP3581576B1 (en) 2022-01-26
AU2014228175B2 (en) 2018-05-31
KR102216288B1 (en) 2021-02-18
IL267609A (en) 2019-08-29
KR20150136497A (en) 2015-12-07
MX2019008521A (en) 2019-10-30
BR112015022942A2 (en) 2017-07-18
EP3581576A1 (en) 2019-12-18
PH12015502157A1 (en) 2016-01-25
EP2970282B1 (en) 2019-08-21
KR20210021090A (en) 2021-02-24
AR095326A1 (en) 2015-10-07
MX366703B (en) 2019-07-22
CA2903881C (en) 2021-05-18
IL241158A0 (en) 2015-11-30
SG10201707487VA (en) 2017-10-30
TWI719464B (en) 2021-02-21
CN109593096B (en) 2022-01-14
CN105164131B (en) 2018-12-28
JP2018008958A (en) 2018-01-18
CA2903881A1 (en) 2014-09-18
EA038494B1 (en) 2021-09-07
TW201512198A (en) 2015-04-01
IL241158B (en) 2019-07-31
AU2014228175A1 (en) 2015-10-08
US10464947B2 (en) 2019-11-05
EA201992712A3 (en) 2020-05-31
IL267609B (en) 2020-07-30
NZ712453A (en) 2020-06-26
US9938294B2 (en) 2018-04-10
ZA201507255B (en) 2023-03-29
JP2019142973A (en) 2019-08-29
HK1218650A1 (en) 2017-03-03
CN105164131A (en) 2015-12-16
JP2016513716A (en) 2016-05-16
US20160046650A1 (en) 2016-02-18
US20180346481A1 (en) 2018-12-06
TW201930303A (en) 2019-08-01
KR102355670B1 (en) 2022-02-08
US20170210754A1 (en) 2017-07-27
EA201591785A1 (en) 2015-12-30
US10919912B2 (en) 2021-02-16
WO2014143768A1 (en) 2014-09-18
EA201992712A2 (en) 2020-03-31
PE20151990A1 (en) 2016-01-13
ES2909778T3 (en) 2022-05-10
CN109593096A (en) 2019-04-09
ECSP15043772A (en) 2017-08-31
CR20150513A (en) 2016-01-04

Similar Documents

Publication Publication Date Title
ZA202001242B (en) Tricyclic heterocycles as bet protein inhibitors
HK1223617A1 (en) Tricyclic heterocycles as bet protein inhibitors bet
ZA201800854B (en) Novel bicyclic bromodomain inhibitors
IL256946B (en) Bromodomain inhibitors
HK1224296A1 (en) Bromodomain inhibitors
HK1218547A1 (en) Novel quinazolinones as bromodomain inhibitors
IL241123A0 (en) Dihydro-pyrrolopyridinone bromodomain inhibitors
IL239827A0 (en) Methoblic triphosphatase inhibitors
GB201314578D0 (en) Bicyclic inhibitors