AU2016319785C1 - Acetamide thienotriazolodiazepines and uses thereof - Google Patents

Acetamide thienotriazolodiazepines and uses thereof Download PDF

Info

Publication number
AU2016319785C1
AU2016319785C1 AU2016319785A AU2016319785A AU2016319785C1 AU 2016319785 C1 AU2016319785 C1 AU 2016319785C1 AU 2016319785 A AU2016319785 A AU 2016319785A AU 2016319785 A AU2016319785 A AU 2016319785A AU 2016319785 C1 AU2016319785 C1 AU 2016319785C1
Authority
AU
Australia
Prior art keywords
optionally substituted
certain embodiments
alkyl
unsubstituted
compound
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.)
Ceased
Application number
AU2016319785A
Other languages
English (en)
Other versions
AU2016319785B2 (en
AU2016319785A8 (en
AU2016319785A1 (en
Inventor
James E. Bradner
Jun Qi
Minoru Tanaka
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Dana Farber Cancer Institute Inc
Original Assignee
Dana Farber Cancer Institute Inc
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 Dana Farber Cancer Institute Inc filed Critical Dana Farber Cancer Institute Inc
Publication of AU2016319785A1 publication Critical patent/AU2016319785A1/en
Publication of AU2016319785A8 publication Critical patent/AU2016319785A8/en
Publication of AU2016319785B2 publication Critical patent/AU2016319785B2/en
Priority to AU2020294169A priority Critical patent/AU2020294169B2/en
Application granted granted Critical
Publication of AU2016319785C1 publication Critical patent/AU2016319785C1/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14Ortho-condensed systems
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • AIDS & HIV (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Biotechnology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2016319785A 2015-09-11 2016-09-09 Acetamide thienotriazolodiazepines and uses thereof Ceased AU2016319785C1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2020294169A AU2020294169B2 (en) 2015-09-11 2020-12-21 Acetamide thienotriazolodiazepines and uses thereof

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562217544P 2015-09-11 2015-09-11
US62/217,544 2015-09-11
PCT/US2016/051017 WO2017044792A1 (en) 2015-09-11 2016-09-09 Acetamide thienotriazoldiazepines and uses thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2020294169A Division AU2020294169B2 (en) 2015-09-11 2020-12-21 Acetamide thienotriazolodiazepines and uses thereof

Publications (4)

Publication Number Publication Date
AU2016319785A1 AU2016319785A1 (en) 2018-03-22
AU2016319785A8 AU2016319785A8 (en) 2019-07-25
AU2016319785B2 AU2016319785B2 (en) 2020-09-24
AU2016319785C1 true AU2016319785C1 (en) 2021-04-01

Family

ID=58240133

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2016319785A Ceased AU2016319785C1 (en) 2015-09-11 2016-09-09 Acetamide thienotriazolodiazepines and uses thereof
AU2020294169A Expired - Fee Related AU2020294169B2 (en) 2015-09-11 2020-12-21 Acetamide thienotriazolodiazepines and uses thereof

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2020294169A Expired - Fee Related AU2020294169B2 (en) 2015-09-11 2020-12-21 Acetamide thienotriazolodiazepines and uses thereof

Country Status (21)

Country Link
US (2) US10881668B2 (cg-RX-API-DMAC7.html)
EP (1) EP3347020A4 (cg-RX-API-DMAC7.html)
JP (1) JP2018526424A (cg-RX-API-DMAC7.html)
KR (1) KR20180051576A (cg-RX-API-DMAC7.html)
CN (1) CN108472299A (cg-RX-API-DMAC7.html)
AU (2) AU2016319785C1 (cg-RX-API-DMAC7.html)
BR (1) BR112018004617A2 (cg-RX-API-DMAC7.html)
CA (1) CA2996977A1 (cg-RX-API-DMAC7.html)
CL (1) CL2018000622A1 (cg-RX-API-DMAC7.html)
CO (1) CO2018002568A2 (cg-RX-API-DMAC7.html)
CR (1) CR20180199A (cg-RX-API-DMAC7.html)
HK (1) HK1256419A1 (cg-RX-API-DMAC7.html)
IL (1) IL257593A (cg-RX-API-DMAC7.html)
MX (1) MX2018003030A (cg-RX-API-DMAC7.html)
PE (1) PE20181086A1 (cg-RX-API-DMAC7.html)
PH (1) PH12018550026A1 (cg-RX-API-DMAC7.html)
RU (1) RU2018112953A (cg-RX-API-DMAC7.html)
SG (1) SG10202007099TA (cg-RX-API-DMAC7.html)
UA (1) UA123946C2 (cg-RX-API-DMAC7.html)
WO (1) WO2017044792A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201801549B (cg-RX-API-DMAC7.html)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10150756B2 (en) 2014-01-31 2018-12-11 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
EP3099693A4 (en) 2014-01-31 2017-08-16 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
JP2017526741A (ja) 2014-08-08 2017-09-14 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
CA2986441A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
HK1256417A1 (zh) 2015-09-11 2019-09-20 达纳-法伯癌症研究所股份有限公司 氰基噻吩並三唑並二氮雜環庚三烯及其用途
BR112018004617A2 (pt) 2015-09-11 2018-09-25 Dana Farber Cancer Inst Inc acetamida tienotriazoldiazepinas e usos das mesmas
SG11201803210YA (en) 2015-11-25 2018-05-30 Dana Farber Cancer Inst Inc Bivalent bromodomain inhibitors and uses thereof
CN107629057B (zh) * 2016-07-19 2020-03-27 上海勋和医药科技有限公司 Bet蛋白抑制剂及其应用
AU2018334788B2 (en) 2017-09-22 2022-11-24 CSPC Zhongqi Pharmaceutical Technology(Shijiazhuang) Co., Ltd. Thienodiazepine derivatives and application thereof
EP3936507A4 (en) * 2019-03-07 2022-11-23 Medshine Discovery Inc. Compounds having both effects of bet bromodomain protein inhibition and pd-l1 gene regulation
WO2021175432A1 (en) 2020-03-04 2021-09-10 Boehringer Ingelheim International Gmbh Method for administration of an anti cancer agent
CN112444582B (zh) * 2021-02-01 2021-06-04 宁波大学 基于液滴萃取的质谱分析方法
CN113816970B (zh) * 2021-09-18 2022-08-09 济宁医学院附属医院 一种选择性铜离子螯合剂、其制备方法及其在肺纤维化中的应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5712274A (en) * 1993-09-16 1998-01-27 Yoshitomi Pharmaceutical Industries, Ltd. Thienotriazolodiazepine compounds and their pharmaceutical use
US20130210813A1 (en) * 2010-05-14 2013-08-15 James Elliott Bradner Male Contraceptive Compositions and Methods of Use
WO2017030814A1 (en) * 2015-08-19 2017-02-23 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins

Family Cites Families (172)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3709898A (en) 1971-02-09 1973-01-09 Upjohn Co Process for the production of triazolobenzodiazepines and intermediates
US3681343A (en) 1971-05-11 1972-08-01 Upjohn Co 6-phenyl-s-triazolo{8 4,3-a{9 {8 1,4{9 {0 benzodiazepines
US3812259A (en) 1971-08-09 1974-05-21 Upjohn Co Animal feed and process
CH622019A5 (en) 1975-10-23 1981-03-13 Upjohn Co Process for the preparation of aminotriazolobenzodiazepines
FR2329668A1 (fr) 1975-10-27 1977-05-27 Upjohn Co Procede de preparation d'aminotriazolobenzodiazepines
EP0087850A1 (en) 1982-01-04 1983-09-07 The Upjohn Company Benzodiazepines for anti-hypertensive use
DE3435973A1 (de) 1984-10-01 1986-04-10 Boehringer Ingelheim KG, 6507 Ingelheim Diazepine enthaltende pharmazeutische zusammensetzungen mit paf-antagonistischer wirkung
JPS62181282A (ja) 1986-01-21 1987-08-08 ベ−リンガ− インゲルハイム コマンデイツト ゲゼルシヤフト チエノ−1,4−ジアゼピン
DE3724164A1 (de) 1986-07-25 1988-01-28 Boehringer Ingelheim Kg Neue 1,4-benzodiazepine, ihre herstellung und verwendung
DE3878833T2 (de) 1987-05-28 1993-06-09 Yoshitomi Pharmaceutical Thieno(triazolo)diazepinverbindungen, und medizinische verwendung derselben.
JPH0676326B2 (ja) 1988-05-24 1994-09-28 吉富製薬株式会社 循環器系疾患治療薬
EP0368175A1 (de) * 1988-11-06 1990-05-16 Boehringer Ingelheim Kg 3S,7S-3-(Morpholinocarbonyl)-5-(2-chlorphenyl)-7,10-dimethyl-3,4-dihydro-2H,7H-cyclopenta[4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin.
EP0387613A1 (de) 1989-03-03 1990-09-19 Boehringer Ingelheim Kg Neue Thienodiazepine
CA2020806A1 (en) 1989-07-12 1991-01-13 Karl-Heinz Weber Thienodiazepine derivatives
DE4010528A1 (de) 1990-04-02 1991-10-17 Boehringer Ingelheim Kg Praeparativ chromatographisches trennverfahren zur herstellung enantiomerenreiner hetrazepine
JP2959591B2 (ja) 1990-05-23 1999-10-06 吉富製薬株式会社 チエノトリアゾロジアゼピン化合物
DE4107521A1 (de) 1991-03-08 1992-09-10 Boehringer Ingelheim Kg Neue acylaminosubstituierte hetrazepine
WO1993007129A1 (fr) 1991-10-11 1993-04-15 Yoshitomi Pharmaceutical Industries, Ltd. Medicament utilise pour traiter l'osteoporose et compose de diazepine
CA2159344A1 (en) 1993-03-30 1994-10-13 Minoru Moriwaki Cell adhesion inhibitor and thienotriazolodiazepine compound
JP3001979U (ja) 1994-03-14 1994-09-06 有限会社マルセ木工 竿掛け具
WO1995032963A1 (en) * 1994-06-01 1995-12-07 Yoshitomi Pharmaceutical Industries, Ltd. Thienylazole compound and thienotriazolodiazepine compound
DK0801651T3 (da) 1995-01-06 2001-10-22 Hoffmann La Roche Hydroxymethyl-imidazodiazepiner og deres estere
BR9610390A (pt) 1995-09-09 1999-07-06 Hoffmann La Roche O uso de uma tienotriazolodiazepina para aumentar os níveis da apoliproteína a-i
US5893397A (en) 1996-01-12 1999-04-13 Bioject Inc. Medication vial/syringe liquid-transfer apparatus
CA2258053A1 (en) 1996-06-12 1997-12-18 Yoshihisa Yamamoto Cytokine production inhibitors, triazepine compounds, and intermediates thereof
US5693641A (en) 1996-08-16 1997-12-02 Berlex Laboratories Inc. Bicyclic pyrimidine derivatives and their use as anti-coagulants
WO1998011111A1 (en) 1996-09-13 1998-03-19 Yoshitomi Pharmaceutical Industries, Ltd. Thienotriazolodiazepine compounds and medicinal uses thereof
US6444664B1 (en) 1997-04-18 2002-09-03 Nederlandse Organisatie Voor Toegepast - Natuurweten Schappelijk Onderzoek (Tno) Method for controlling the plasma level of lipoproteins to treat alzheimeris disease
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
JPH11228576A (ja) 1997-12-10 1999-08-24 Japan Tobacco Inc アポトーシス抑制剤
FR2779652B1 (fr) 1998-06-15 2001-06-08 Sod Conseils Rech Applic Utilisation de diazepines pour la preparation de medicaments destines a traiter les etats pathologiques ou les maladies dans lesquels un des recepteurs de la somatostatine est implique
US7589167B2 (en) 2000-02-22 2009-09-15 J. David Gladstone Institutes ZA loops of bromodomains
CA2412776C (en) 2000-06-16 2011-03-15 Mitsubishi Pharma Corporation Compositions controlling release ph range and/or speed
WO2002002557A2 (en) 2000-06-30 2002-01-10 Neurogen Corporation 2-phenylimidazo[1,2-a]pyridine derivatives: a new class of gaba brain receptor ligands
US20060142257A1 (en) 2001-01-19 2006-06-29 Eberhard Nieschlag Male contraceptive formulation comprising norethisterone
US6979682B2 (en) 2001-02-23 2005-12-27 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Platelet-activating factor antagonist inhibition of angiogenesis and tumor growth induced by basic fibroblast
MXPA04002067A (es) 2001-09-04 2004-06-07 Boehringer Ingelheim Pharma Nuevas dihidropteridinonas, procedimientos para su preparacion y su uso como medicamento.
US6806272B2 (en) 2001-09-04 2004-10-19 Boehringer Ingelheim Pharma Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
US20030216758A1 (en) 2001-12-28 2003-11-20 Angiotech Pharmaceuticals, Inc. Coated surgical patches
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
JP3096299U (ja) 2003-02-20 2003-09-12 宇輪工業股▲ふん▼有限公司 足踏み式健康器
US6861422B2 (en) 2003-02-26 2005-03-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
DK1599478T3 (da) 2003-02-26 2007-09-17 Boehringer Ingelheim Pharma Dihydropteridinoner, fremgangsmåde til fremstilling af disse og anvendelse af disse som lægemiddel
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
WO2005002526A2 (en) 2003-07-01 2005-01-13 President And Fellows Of Harvard College Method and compositions for treatment of viral infections
AU2004272288B2 (en) 2003-09-18 2008-11-13 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
EP1528056A1 (en) 2003-10-29 2005-05-04 Academisch Ziekenhuis bij de Universiteit van Amsterdam Deoxynojirimycin analogues and their uses as glucosylceramidase inhibitors
US7728134B2 (en) 2004-08-14 2010-06-01 Boehringer Ingelheim International Gmbh Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament
US20060035903A1 (en) 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
US7759485B2 (en) 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
US20060074088A1 (en) 2004-08-14 2006-04-06 Boehringer Ingelheim International Gmbh Dihydropteridinones for the treatment of cancer diseases
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
CA2578560A1 (en) 2004-08-27 2006-03-02 Boehringer Ingelheim International Gmbh Dihydropteridinones, method for the production thereof, and use thereof as a medicament
CN1759834B (zh) 2004-09-17 2010-06-23 中国医学科学院医药生物技术研究所 黄连素或其与辛伐他汀联合在制备用于预防或治疗与血脂有关疾病或症状的产品中用途
EP1887008B1 (en) 2005-05-30 2021-04-21 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compound and a medicinal use thereof
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
NZ563454A (en) 2005-06-08 2011-03-31 Rigel Pharmaceuticals Inc 2,4-diaminopyrimidine derivatives for inhibition of the JAK pathway
WO2007014838A1 (en) 2005-08-03 2007-02-08 Boehringer Ingelheim International Gmbh Dihydropteridinones in the treatment of respiratory diseases
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
MX391408B (es) 2005-11-01 2025-03-21 Impact Biomedicines Inc Inhibidores de biaril meta-pirimidina de cinasas.
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
ES2408318T3 (es) 2005-12-23 2013-06-20 Glaxosmithkline Llc Inhibidores de azaindol de las cinasas Aurora
WO2007082806A1 (en) 2006-01-17 2007-07-26 F. Hoffmann-La Roche Ag Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine useful for the treatment of alzheimer’s disease via gaba receptors
WO2007095188A2 (en) 2006-02-14 2007-08-23 Vertex Pharmaceuticals Incorporated Dihydrodiazepines useful as inhibitors of protein kinases
ES2351367T3 (es) 2006-02-14 2011-02-03 Vertex Pharmaceuticals Incorporated Dihidrodiazepinas útiles como inhibidores de proteína quinasas.
US20070218135A1 (en) 2006-03-14 2007-09-20 Glenmark Pharmaceuticals Limited Sustained release matrix pharmaceutical composition
BRPI0711174A2 (pt) 2006-05-03 2011-08-23 Novartis Ag uso de compostos orgánicos
JP2009537500A (ja) 2006-05-19 2009-10-29 アストラゼネカ アクチボラグ 増殖抑制剤としてのジヒドロプテリジン化合物
WO2008009909A1 (en) 2006-07-17 2008-01-24 Astrazeneca Ab Pteridimones as modulators of polo-like kinase
US7981893B2 (en) 2006-10-19 2011-07-19 Signal Pharmaceuticals, Llc Heteroaryl compounds, compositions thereof, and methods of treatment therewith
US8338464B2 (en) 2006-11-30 2012-12-25 Albert Einstein College Of Medicine Of Yeshiva University Small molecule inhibitors of BCL6
JP2008156311A (ja) 2006-12-26 2008-07-10 Institute Of Physical & Chemical Research Brd2ブロモドメイン結合剤
EP2474523B1 (en) 2006-12-26 2020-04-08 Lantheus Medical Imaging, Inc. Ligands for imaging cardiac innervation
KR101157848B1 (ko) 2007-03-22 2012-07-11 다케다 야쿠힌 고교 가부시키가이샤 Plk1 저해제로서 유용한 치환된 피리미도디아제핀
WO2008137081A1 (en) 2007-05-02 2008-11-13 The Trustees Of Columbia University In The City Of New York Substituted ( 5, 6 ) -dihydronaphraalenyl compounds as reversible male contraceptives
KR20080107050A (ko) 2007-06-05 2008-12-10 울산대학교 산학협력단 항-cd137 단일클론 항체를 포함하는 만성이식편대숙주 질환의 예방 또는 치료용 약학적 조성물
AU2008287339A1 (en) 2007-08-15 2009-02-19 Vertex Pharmaceuticals Incorporated 4-(9-(3, 3-difluorocyclopentyl) -5, 7, 7-trimethyl-6-oxo-6, 7, 8, 9-tetrahydro-5H-pyrimido [4, 5-b][1, 4] diazepin-2-ylamino)-3-methoxybenzamide Derivatives as Inhibitors of the Human Protein Kinases PLK1 to PLK4 for the Treatment of Proliferative Diseases
WO2009042711A1 (en) 2007-09-25 2009-04-02 Takeda Pharmaceutical Company Limited Polo-like kinase inhibitors
RU2478100C2 (ru) 2007-09-28 2013-03-27 Сайкласел Лимитед Пиримидиновые производные, используемые в качестве ингибиторов протеинкиназы
US20090291938A1 (en) 2007-11-19 2009-11-26 Takeda Pharmaceutical Company Limited Polo-like kinase inhibitors
US20110028405A1 (en) 2007-12-20 2011-02-03 Richard John Harrison Sulfamides as zap-70 inhibitors
US8476260B2 (en) 2007-12-28 2013-07-02 Mitsubishi Tanabe Pharma Corporation Antitumor agent
AU2009224804B2 (en) 2008-03-10 2013-12-05 Janssen Pharmaceutica Nv 4-aryl-2-anilino-pyrimidines as PLK kinase inhibitors
WO2009112490A1 (en) 2008-03-11 2009-09-17 Cellzome Limited Sulfonamides as zap-70 inhibitors
FR2928923B1 (fr) 2008-03-21 2010-04-23 Sanofi Aventis Derives polysubstitues de 2-heteroaryl-6-phenyl-imidazo °1,2-a!pyridines, leur preparation et leur application en therapeutiques
EP2112152A1 (en) 2008-04-22 2009-10-28 GPC Biotech AG Dihydropteridinones as Plk Inhibitors
EP2303889A1 (en) 2008-06-18 2011-04-06 F. Hoffmann-La Roche AG Halo-substituted pyrimidodiazepines as plkl inhibitors
WO2010015340A1 (en) 2008-08-06 2010-02-11 Bayer Schering Pharma Aktiengesellschaft Daa-pyridine as peripheral benzodiazepine receptor ligand for diagnostic imaging and pharmaceutical treatment
CN102216298B (zh) 2008-09-16 2014-04-16 Csir公司 作为hiv-1逆转录酶抑制剂的咪唑并吡啶和咪唑并嘧啶
CA2741934C (en) 2008-10-30 2016-09-13 Circomed Llc Thienotriazolodiazepine derivatives active on apo a
US9266890B2 (en) 2009-01-06 2016-02-23 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
BRPI1007358A2 (pt) 2009-01-23 2018-03-06 Takeda Pharmaceutical Company Limited inibidores de poli (adp-ribose) polimerase (parp)
CN102020643A (zh) 2009-09-22 2011-04-20 上海恒瑞医药有限公司 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用
JP2013505927A (ja) 2009-09-25 2013-02-21 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼ阻害剤として有用なピリミジン誘導体の調製方法
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
PT2722334E (pt) 2009-11-05 2016-03-11 Glaxosmithkline Llc Inibidor do bromodomínio da benzodiazepina
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919433D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
PL2496582T3 (pl) 2009-11-05 2016-08-31 Glaxosmithkline Llc Benzodiazepinowy inhibitor bromodomeny
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
JP5841548B2 (ja) 2010-02-17 2016-01-13 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 ジヒドロプテリジノン、その製造方法及び使用
MX384074B (es) 2010-05-14 2025-03-12 Dana Farber Cancer Inst Inc Composiciones y métodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos.
JP5913292B2 (ja) 2010-05-14 2016-04-27 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 代謝を調節する組成物および方法
JP5715241B2 (ja) * 2010-05-14 2015-05-07 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 新生物、炎症性疾患、およびその他の障害を治療するための組成物および方法
CN103154246B (zh) * 2010-05-14 2015-11-25 达那-法伯癌症研究所 用于治疗白血病的组合物和方法
JP5844358B2 (ja) 2010-06-22 2016-01-13 グラクソスミスクライン エルエルシー ベンゾトリアゾロジアゼピン化合物を含むブロモドメイン阻害剤
US20120014979A1 (en) 2010-07-16 2012-01-19 Alexander Dent Use of bcl6 inhibitors for treating autoimmune diseases
US9358233B2 (en) 2010-11-29 2016-06-07 Boehringer Ingelheim International Gmbh Method for treating acute myeloid leukemia
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
US9249161B2 (en) * 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
CN103547152A (zh) 2011-02-23 2014-01-29 西奈山伊坎医学院 溴结构域蛋白的抑制剂作为基因表达的调节剂
ES2951688T3 (es) 2011-02-28 2023-10-24 Epizyme Inc Compuestos de heteroarilo biciclico fusionados en 6,5 sustituidos
BR112013022697A2 (pt) 2011-03-07 2019-09-24 Fond Telethon inibidores de fosforilação de tfeb e usos dos mesmos
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
WO2013033270A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same
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
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
CN104203267A (zh) 2012-02-17 2014-12-10 安迅生物制药公司 用于治疗流感和副流感患者的方法、化合物和组合物
US20150133434A1 (en) 2012-03-28 2015-05-14 The J. David Gladstone Institutes Compositions and Methods for Reactivating Latent Immunodeficiency Virus
WO2014023696A1 (en) 2012-08-08 2014-02-13 Novomatic Ag Method of and system for tracking gaming activity
HK1211209A1 (en) 2012-09-28 2016-05-20 Oncoethix Gmbh Pharmaceutical formulation containing thienotriazolodiazepine compounds
US9663523B2 (en) * 2012-09-28 2017-05-30 Bayer Pharma Aktiengesellschaft BET protein-inhibiting 5-aryltriazoleazepines
EP2917203B1 (en) 2012-11-02 2019-04-03 Dana-Farber Cancer Institute, Inc. Method for identifying myc inhibitors
US20160193206A1 (en) 2012-12-20 2016-07-07 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydropyridopyrazinones
US8980879B2 (en) 2013-03-11 2015-03-17 Abbvie Inc. Bromodomain inhibitors
US20140254659A1 (en) 2013-03-11 2014-09-11 Mediatek Inc. Video coding method using at least evaluated visual quality and related video coding apparatus
CN108440528A (zh) 2013-03-12 2018-08-24 艾伯维公司 四环布罗莫结构域抑制剂
US9714946B2 (en) * 2013-03-14 2017-07-25 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
BR112015022604A2 (pt) 2013-03-14 2017-10-24 Genentech Inc usos de um modulador de modificador de cromatina e um antagonista de egfr
CA2918910A1 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
EP3047276B1 (en) 2013-09-19 2023-06-14 Dana-Farber Cancer Institute, Inc. Methods of bh3 profiling
WO2015081280A1 (en) 2013-11-26 2015-06-04 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution
WO2015081284A1 (en) 2013-11-26 2015-06-04 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
AU2014361381A1 (en) 2013-12-10 2016-06-16 Abbvie Inc. Bromodomain inhibitors
EP3099693A4 (en) 2014-01-31 2017-08-16 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
US10150756B2 (en) 2014-01-31 2018-12-11 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
WO2015117083A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
WO2015117055A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
JP2017510561A (ja) * 2014-02-26 2017-04-13 杏林製薬株式会社 ヘテロ環式化合物
EP3110424A1 (en) * 2014-02-28 2017-01-04 Tensha Therapeutics, Inc. Treatment of conditions associated with hyperinsulinaemia
US20180228907A1 (en) * 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
JP2017526741A (ja) 2014-08-08 2017-09-14 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
WO2016022970A1 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
WO2016090219A1 (en) * 2014-12-05 2016-06-09 H. Lee Moffitt Cancer Center And Research Institute, Inc. Bromodomain inhibitor as adjuvant in cancer immunotherapy
JP6815318B2 (ja) 2014-12-23 2021-01-20 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 二官能性分子によって標的化タンパク質分解を誘導する方法
US9694084B2 (en) * 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
MX385750B (es) 2015-03-18 2025-03-18 Arvinas Inc Compuestos y métodos para la degradación mejorada de proteinas específicas.
CA2986441A1 (en) * 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
WO2017007612A1 (en) * 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
CN108350062B (zh) * 2015-08-06 2022-10-14 达纳-法伯癌症研究所股份有限公司 靶向蛋白降解以减弱过继性t细胞疗法相关的不良炎症反应
MX387736B (es) 2015-09-04 2025-03-18 Hoffmann La Roche Derivados de fenoximetilo.
RU2734959C2 (ru) * 2015-09-09 2020-10-26 Джубилант Байосис Лимитед Трициклические конденсированные производные пиридин-2-она и их применение в качестве ингибиторов brd4
JP6868011B2 (ja) 2015-09-11 2021-05-12 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 ピラゾリル置換ヘテロアリール及び医薬としてのその使用
HK1256417A1 (zh) * 2015-09-11 2019-09-20 达纳-法伯癌症研究所股份有限公司 氰基噻吩並三唑並二氮雜環庚三烯及其用途
BR112018004617A2 (pt) 2015-09-11 2018-09-25 Dana Farber Cancer Inst Inc acetamida tienotriazoldiazepinas e usos das mesmas
WO2017091617A1 (en) 2015-11-25 2017-06-01 Gilead Apollo, Llc Triazole acc inhibitors and uses thereof
SG11201803210YA (en) 2015-11-25 2018-05-30 Dana Farber Cancer Inst Inc Bivalent bromodomain inhibitors and uses thereof
PT3380522T (pt) 2015-11-25 2024-02-14 Visterra Inc Moléculas de anticorpos contra april e suas utilizações
HUE053175T2 (hu) 2015-11-25 2021-06-28 Gilead Apollo Llc ACC-gátló észterek és azok alkalmazása
MX2018006285A (es) 2015-11-25 2018-09-07 Gilead Apollo Llc Composiciones fungicidas que contienen derivados de 2,4-dioxido-1,4-dihidrotieno[2,3-d] pirimidina.
KR20180082556A (ko) 2015-11-25 2018-07-18 길리어드 아폴로, 엘엘씨 피라졸 acc 억제제 및 그의 용도
JP7105691B2 (ja) 2015-11-25 2022-07-25 イーフェクター セラピューティクス, インコーポレイテッド Eif4a-阻害化合物およびそれに関連する方法
AU2016362040B2 (en) 2015-12-01 2019-10-10 Nihon Nohyaku Co., Ltd. 3H-pyrrolopyridine compound, N-oxide thereof or salt thereof, agricultural and horticultural insecticide comprising the compound and method for using the same
EP3455219A4 (en) * 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP3455218A4 (en) * 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
WO2017201069A1 (en) * 2016-05-18 2017-11-23 Biotheryx, Inc. Oxoindoline derivatives as protein function modulators
GB201608797D0 (en) 2016-05-19 2016-07-06 Ucb Biopharma Sprl Therapeutic use
WO2018064589A1 (en) * 2016-09-29 2018-04-05 Dana-Farber Cancer Institute, Inc. Targeted protein degradation using a mutant e3 ubiquitin ligase

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5712274A (en) * 1993-09-16 1998-01-27 Yoshitomi Pharmaceutical Industries, Ltd. Thienotriazolodiazepine compounds and their pharmaceutical use
US20130210813A1 (en) * 2010-05-14 2013-08-15 James Elliott Bradner Male Contraceptive Compositions and Methods of Use
WO2017030814A1 (en) * 2015-08-19 2017-02-23 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CAS REG NO. 130066-84-1, STN Entry Date: 26 October 1990 ; 1-Propanone, 3-[6-(2-chlorophenyl)-8,9-dihydro-1-methyl-4H,7H-cyclopenta[4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl]-1-(4-morpholinyl)- *

Also Published As

Publication number Publication date
ZA201801549B (en) 2021-07-28
AU2016319785B2 (en) 2020-09-24
CR20180199A (es) 2018-05-25
AU2016319785A8 (en) 2019-07-25
BR112018004617A2 (pt) 2018-09-25
CN108472299A (zh) 2018-08-31
CO2018002568A2 (es) 2018-07-19
HK1256419A1 (zh) 2019-09-20
UA123946C2 (uk) 2021-06-30
US20210093644A1 (en) 2021-04-01
US10881668B2 (en) 2021-01-05
CL2018000622A1 (es) 2018-08-31
US11406645B2 (en) 2022-08-09
RU2018112953A3 (cg-RX-API-DMAC7.html) 2019-12-26
US20190046541A1 (en) 2019-02-14
IL257593A (en) 2018-04-30
US20210393647A9 (en) 2021-12-23
CA2996977A1 (en) 2017-03-16
AU2020294169B2 (en) 2022-06-16
EP3347020A4 (en) 2019-08-14
AU2016319785A1 (en) 2018-03-22
WO2017044792A1 (en) 2017-03-16
PH12018550026A1 (en) 2018-08-13
KR20180051576A (ko) 2018-05-16
SG10202007099TA (en) 2020-08-28
WO2017044792A8 (en) 2018-04-12
RU2018112953A (ru) 2019-10-14
MX2018003030A (es) 2018-04-11
EP3347020A1 (en) 2018-07-18
AU2020294169A1 (en) 2021-01-28
JP2018526424A (ja) 2018-09-13
PE20181086A1 (es) 2018-07-05

Similar Documents

Publication Publication Date Title
AU2020294169B2 (en) Acetamide thienotriazolodiazepines and uses thereof
AU2016361478B2 (en) Bivalent bromodomain inhibitors and uses thereof
AU2016319116B2 (en) Cyano thienotriazolodiazepines and uses thereof
US10793571B2 (en) Uses of diazepane derivatives
EP3099171A1 (en) Dihydropteridinone derivatives and uses thereof
WO2015117083A1 (en) Diazepane derivatives and uses thereof
EP3099677A1 (en) Diaminopyrimidine benzenesulfone derivatives and uses thereof
EP3177626A1 (en) Diazepane derivatives and uses thereof
WO2016022970A1 (en) Dihydropteridinone derivatives and uses thereof

Legal Events

Date Code Title Description
TH Corrigenda

Free format text: IN VOL 32 , NO 11 , PAGE(S) 1556 UNDER THE HEADING PCT APPLICATIONS THAT HAVE ENTERED THE NATIONAL PHASE - NAME INDEX UNDER THE NAME DANA-FARBER CANCER INSTITUTE, INC., APPLICATION NO. 2016319785, UNDER INID (54) CORRECT THE TITLE TO READ ACETAMIDE THIENOTRIAZOLODIAZEPINES AND USES THEREOF

DA2 Applications for amendment section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 04 NOV 2020

DA2 Applications for amendment section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 21 DEC 2020

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT FILED 04 NOV 2020

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT FILED 21 DEC 2020

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired