AU2014298051B2 - Novel quinazolinones as bromodomain inhibitors - Google Patents

Novel quinazolinones as bromodomain inhibitors Download PDF

Info

Publication number
AU2014298051B2
AU2014298051B2 AU2014298051A AU2014298051A AU2014298051B2 AU 2014298051 B2 AU2014298051 B2 AU 2014298051B2 AU 2014298051 A AU2014298051 A AU 2014298051A AU 2014298051 A AU2014298051 A AU 2014298051A AU 2014298051 B2 AU2014298051 B2 AU 2014298051B2
Authority
AU
Australia
Prior art keywords
amino
cancer
mmol
dimethoxy
pyridin
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
AU2014298051A
Other languages
English (en)
Other versions
AU2014298051A1 (en
Inventor
Vladimir Khlebnikov
John Frederick Quinn
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.)
Zenith Epigenetics Ltd
Original Assignee
Zenith Epigenetics Ltd
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 Zenith Epigenetics Ltd filed Critical Zenith Epigenetics Ltd
Publication of AU2014298051A1 publication Critical patent/AU2014298051A1/en
Assigned to ZENITH EPIGENETICS LTD. reassignment ZENITH EPIGENETICS LTD. Request for Assignment Assignors: ZENITH EPIGENETICS CORP.
Application granted granted Critical
Publication of AU2014298051B2 publication Critical patent/AU2014298051B2/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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/04Artificial tears; Irrigation solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • 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
    • A61P31/04Antibacterial agents
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • C07D239/91Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
AU2014298051A 2013-07-31 2014-07-30 Novel quinazolinones as bromodomain inhibitors Ceased AU2014298051B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361860403P 2013-07-31 2013-07-31
US61/860,403 2013-07-31
PCT/IB2014/002510 WO2015015318A2 (en) 2013-07-31 2014-07-30 Novel quinazolinones as bromodomain inhibitors

Publications (2)

Publication Number Publication Date
AU2014298051A1 AU2014298051A1 (en) 2016-01-28
AU2014298051B2 true AU2014298051B2 (en) 2018-11-15

Family

ID=52432501

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2014298051A Ceased AU2014298051B2 (en) 2013-07-31 2014-07-30 Novel quinazolinones as bromodomain inhibitors

Country Status (10)

Country Link
US (2) US9855271B2 (enExample)
EP (1) EP3027604B1 (enExample)
JP (1) JP6542212B2 (enExample)
KR (1) KR20160038008A (enExample)
CN (1) CN105593224B (enExample)
AU (1) AU2014298051B2 (enExample)
CA (1) CA2919948C (enExample)
EA (1) EA201690087A1 (enExample)
IL (1) IL243479B (enExample)
WO (1) WO2015015318A2 (enExample)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
MX2015007921A (es) 2012-12-21 2016-03-03 Zenith Epigenetics Corp Compuestos heterociclicos novedosos como inhibidores de bromodominio.
EP2968360B1 (en) 2013-03-14 2021-01-20 ConverGene LLC Quinolinone derivatives for the inhibition of bromodomain-containing proteins
CN105407888B (zh) 2013-06-21 2019-05-21 齐尼思表观遗传学有限公司 新双环溴结构域抑制剂
WO2015004534A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
JP6542212B2 (ja) 2013-07-31 2019-07-10 ゼニス・エピジェネティクス・リミテッドZenith Epigenetics Ltd. ブロモドメイン阻害剤としての新規キナゾリノン
EP3125896A2 (en) * 2014-04-04 2017-02-08 Constellation Pharmaceuticals, Inc. EXPRESSION LEVELS OF BCL-xL, BCL2, BCL-w, AND BAD AND CANCER THERAPIES
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
CA2966298A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
CA2966303A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
WO2016092375A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Corp. Substituted heterocycles as bromodomain inhibitors
CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
JP7269731B2 (ja) 2015-03-18 2023-05-09 アルビナス・オペレーションズ・インコーポレイテッド 標的タンパク質の分解向上のための化合物および方法
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
CN112535685A (zh) * 2015-05-08 2021-03-23 四川大学华西第二医院 多聚adp核糖聚合酶抑制剂治疗乙肝病毒相关疾病的新用途
US20180164317A1 (en) * 2015-05-28 2018-06-14 Bayer Pharma Aktiengesellschaft Method for stratification of melanoma patients by determination of oxygen consumption, ppargc1a, ppargc1b and mitf levels
WO2017015027A1 (en) * 2015-07-20 2017-01-26 Mayo Foundation For Medical Education And Research Methods and materials for treating cancer
EP3331905B1 (en) 2015-08-06 2022-10-05 Dana-Farber Cancer Institute, Inc. Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
EA033679B1 (ru) 2015-09-02 2019-11-15 Glaxosmithkline Ip No 2 Ltd Пиридинондикарбоксамиды для применения в качестве ингибиторов бромодомена
JP6795588B2 (ja) 2015-09-22 2020-12-02 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited ブロモドメイン阻害薬としての使用のためのピリジノンジカルボキサミド
ES2831322T3 (es) 2015-10-05 2021-06-08 Glaxosmithkline Ip No 2 Ltd Compuestos de 2-oxo-1,2-dihidropiridin-3,5-dicarboxamida como inhibidores de bromodominios
EP4050005B1 (en) 2015-11-25 2024-12-25 Convergene Llc Bicyclic bet bromodomain inhibitors and uses thereof
CA3019342A1 (en) 2016-03-30 2017-10-05 Wisconsin Alumni Research Foundation Methods and compositions for modulating frataxin expression
AU2017245641A1 (en) 2016-04-07 2018-09-13 Glaxosmithkline Intellectual Property (No.2) Limited Pyridyl derivatives as bromodomain inhibitors
WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
EP4483875A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
CN109153646B (zh) * 2016-05-24 2022-08-02 葛兰素史克知识产权第二有限公司 作为溴结构域抑制剂的吡啶二甲酰胺衍生物
IL312367A (en) 2017-01-31 2024-06-01 Arvinas Operations Inc Cereblon ligands and bifunctional compounds comprising the same
US11311609B2 (en) 2017-02-08 2022-04-26 Dana-Farber Cancer Institute, Inc. Regulating chimeric antigen receptors
GB201703282D0 (en) 2017-03-01 2017-04-12 Glaxosmithkline Intellectual Property (No 2) Ltd Compounds
JOP20190192A1 (ar) 2017-03-01 2019-08-08 Glaxosmithkline Ip No 2 Ltd مشتقات بيرازول بوصفها مثبطات برومودومين
EP3596117A4 (en) 2017-03-17 2021-01-13 The Johns Hopkins University TARGETED EPIGENETIC THERAPY AGAINST THE DISTAL EXPRESSION REGULATORY ELEMENT OF TGFB2
US11759533B2 (en) 2017-03-29 2023-09-19 Wisconsin Alumni Research Foundation Methods and compositions for modulating gene expression
WO2018237026A1 (en) 2017-06-20 2018-12-27 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
EP3743066A4 (en) 2018-01-26 2021-09-08 Yale University IMIDE-BASED PROTEOLYSIS MODULATORS AND RELATED METHODS OF USE
KR20210003804A (ko) 2018-04-13 2021-01-12 아비나스 오퍼레이션스, 인코포레이티드 세레브론 리간드 및 이를 포함하는 2작용성 화합물
CN108715834B (zh) * 2018-06-01 2021-09-14 天晴干细胞股份有限公司 一种富含cd41+、cd81+微囊的血小板裂解液制备方法
US20220089609A1 (en) 2018-07-26 2022-03-24 Domain Therapeutics Substituted quinazolinone derivatives and their use as positive allosteric modulators of mglur4
CN109350616B (zh) * 2018-12-18 2020-04-21 南华大学 I-brd9或其衍生物在制备抗癫痫药物中的应用
WO2020132561A1 (en) 2018-12-20 2020-06-25 C4 Therapeutics, Inc. Targeted protein degradation
EP3958867B1 (en) * 2019-04-24 2024-06-26 Convergene Llc Small molecule bromodomain inhibitors and uses thereof
WO2021107656A2 (ko) * 2019-11-26 2021-06-03 주식회사 베노바이오 신규한 퀘르세틴 리독스 유도체 및 bet 억제제로서의 용도
KR102420263B1 (ko) * 2019-11-26 2022-07-13 주식회사 베노바이오 신규한 퀴나졸린 리독스 유도체 및 bet 억제제로서의 용도
CN111012786B (zh) * 2019-12-16 2021-05-25 中山大学 一种激活炎症小体的小分子化合物及其应用
CN118638043A (zh) 2019-12-19 2024-09-13 阿尔维纳斯运营股份有限公司 用于雄激素受体的靶向降解的化合物和方法
CN113754593B (zh) * 2020-06-01 2024-03-19 上海中医药大学 一种brd4蛋白抑制剂及其应用
JP2023539931A (ja) * 2020-09-09 2023-09-20 オーリジーン オンコロジー リミテッド Cbp/ep300ブロモドメイン阻害剤としての複素環式化合物
CN112546049A (zh) * 2020-12-22 2021-03-26 中山大学中山眼科中心 一种小分子药物(+)-jq1在治疗地图样萎缩型年龄相关性黄斑变性药物中的应用
CN113754594B (zh) * 2021-09-16 2025-01-21 中国药科大学 喹唑啉酮类化合物或其可药用的盐、异构体及其制备方法、药物组合物和用途
KR20240045472A (ko) * 2022-09-30 2024-04-08 주식회사 베노바이오 퀴나졸린염 화합물을 포함하는 관절염 치료용 조성물 및 이의 제조 방법
WO2025049555A1 (en) 2023-08-31 2025-03-06 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013064900A1 (en) * 2011-11-01 2013-05-10 Resverlogix Corp. Oral immediate release formulations for substituted quinazolinones

Family Cites Families (176)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3508258A1 (de) 1985-03-08 1986-09-18 Bayer Ag, 5090 Leverkusen Ss-lactamantibiotika, verfahren zur herstellung und ihre verwendung als und in arzneimitteln
FR2643903A1 (fr) 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
DE4023369A1 (de) 1990-07-23 1992-01-30 Thomae Gmbh Dr K Benzimidazole, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
RU1836357C (ru) 1990-07-23 1993-08-23 Др.Карл Томэ ГмбХ Производные бензимидазола, их изомеры, смеси изомеров, гидраты или их физиологически переносимые соли, обладающие антагонистическими в отношении ангиотензина свойствами
DE4225756A1 (de) 1992-01-22 1994-03-10 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE4224752A1 (de) 1992-04-11 1994-02-03 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
SI9210098B (sl) 1991-02-06 2000-06-30 Dr. Karl Thomae Benzimidazoli, zdravila, ki te spojine vsebujejo, in postopek za njihovo pripravo
US5614519A (en) 1991-02-06 1997-03-25 Karl Thomae Gmbh (1-(2,3 or 4-N-morpholinoalkyl)-imidazol-4-yl)-benizimidazol-1-yl-methyl]-biphenyls useful as angiotensin-II antagonists
US5125961A (en) 1991-08-12 1992-06-30 Monsanto Company Substituted pyridine compounds
DE4219534A1 (de) 1992-02-19 1993-12-16 Thomae Gmbh Dr K Substituierte Biphenylylderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE4408497A1 (de) 1994-03-14 1995-09-21 Thomae Gmbh Dr K Benzimidazole, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
WO1996004274A1 (en) 1994-08-02 1996-02-15 Merck Sharp & Dohme Limited Azetidine, pyrrolidine and piperidine derivatives
JP3342874B2 (ja) 1995-04-21 2002-11-11 ニューロサーチ、アクティーゼルスカブ ベンズイミダゾール化合物、およびgabaaレセプター複合体モジュレーターとしてのその使用
JP2000072675A (ja) 1998-08-26 2000-03-07 Tanabe Seiyaku Co Ltd 医薬組成物
CA2349616A1 (en) 1998-12-04 2000-06-15 Neurosearch A/S New benzimidazolone-, benzoxazolone-, or benzothiazolone derivatives as ion channel modulating agents
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
US6664252B2 (en) 1999-12-02 2003-12-16 Osi Pharmaceuticals, Inc. 4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof
GB0002100D0 (en) 2000-01-28 2000-03-22 Novartis Ag Organic compounds
WO2001057019A1 (en) 2000-02-01 2001-08-09 Cor Therapeutics, Inc. INDALONE AND BENZIMIDAZOLONE INHIBITORS OF FACTOR Xa
US20120028912A1 (en) 2000-02-22 2012-02-02 J.David Gladstone Institute Methods of modulating bromodomains
IL155510A0 (en) 2000-10-27 2003-11-23 Dow Agrosciences Llc Substituted 4,5-dihydro-1,2,4-triazin-6-ones, 1,2,4-triazin-6-ones, and their use as fungicides and insecticides
CA2430577A1 (en) 2000-12-01 2002-07-25 Osi Pharmaceuticals, Inc. Compounds specific to adenosine a1, a2a, and a3 receptor and uses thereof
JP3616628B2 (ja) 2001-03-01 2005-02-02 塩野義製薬株式会社 Hivインテグラーゼ阻害活性を有する含窒素芳香族複素環化合物
WO2002072576A1 (en) 2001-03-09 2002-09-19 Pfizer Products Inc. Benzimidazole anti-inflammatory compounds
DE60221368T2 (de) 2001-03-15 2008-04-17 Janssen Pharmaceutica N.V. Hiv hemmende pyrazinon-derivate
JP4329003B2 (ja) 2001-03-23 2009-09-09 バイエル コーポレイション Rhoキナーゼ阻害剤
US7081454B2 (en) 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
RU2003131693A (ru) 2001-03-28 2005-05-10 Бристол-Маерс Сквибб Компани (Us) Новые ингибиторы тирозин киназ
US20050176858A1 (en) 2002-02-15 2005-08-11 Bridgestone Corporation Rubber composition and pneumatic tire made therefrom
TWI276631B (en) 2002-09-12 2007-03-21 Avanir Pharmaceuticals Phenyl-aza-benzimidazole compounds for modulating IgE and inhibiting cellular proliferation
WO2004043913A2 (en) 2002-11-08 2004-05-27 Trimeris, Inc. Hetero-substituted benzimidazole compounds and antiviral uses thereof
AR043063A1 (es) 2002-12-13 2005-07-13 Altana Pharma Ag Bencimidazoles 6-sustituidos y su uso como inhibidores de secreciones gastricas
AR042956A1 (es) 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
CL2004000409A1 (es) 2003-03-03 2005-01-07 Vertex Pharma Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu
EP1620413A2 (en) 2003-04-30 2006-02-01 Cytokinetics, Inc. Compounds, compositions, and methods
AU2003902860A0 (en) 2003-06-06 2003-06-26 Daicel Chemical Industries, Ltd Benzimidazole compounds
AU2004263190A1 (en) 2003-08-08 2005-02-17 Avanir Pharmaceuticals Selective pharmacologic inhibition of protein trafficking and related methods of treating human diseases
CL2004002050A1 (es) 2003-08-13 2005-06-03 Pharmacia Corp Sa Organizada B Compuestos derivados de piridinonas sustituidas; su uso en el tratamiento de afecciones causadas o exacerbadas por actividad p38 map kinasa y/o tnf no regulada, tales como inflamaciones, tumores, sida y otros.
WO2005080380A1 (en) 2004-02-03 2005-09-01 Eli Lilly And Company Kinase inhibitors
WO2005075432A1 (ja) 2004-02-06 2005-08-18 Chugai Seiyaku Kabushiki Kaisha 1−(2h)−イソキノロン誘導体およびその抗ガン剤としての使用
JP4627315B2 (ja) 2004-03-23 2011-02-09 エフ.ホフマン−ラ ロシュ アーゲー 非ヌクレオシド逆転写酵素阻害剤としてのベンジルピリダジノン誘導体
US20080015196A1 (en) 2004-04-16 2008-01-17 Neurogen Corporation Imidazopyrazines, Imidazopyridines, and Imidazopyrimidines as Crf1 Receptor Ligands
JP4991527B2 (ja) 2004-06-01 2012-08-01 ユニバーシティ オブ バージニア パテント ファンデーション 二つの部分からなる低分子量の癌および血管新生の抑制剤
WO2005121132A1 (ja) 2004-06-11 2005-12-22 Shionogi & Co., Ltd. 抗hcv作用を有する縮合ヘテロ環化合物
EP1786777A1 (en) 2004-08-26 2007-05-23 Pfizer, Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006038734A1 (en) 2004-10-08 2006-04-13 Astellas Pharma Inc. Pyridazinone derivatives cytokines inhibitors
US7846915B2 (en) 2004-10-20 2010-12-07 Resverlogix Corporation Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases
EP1848718B1 (en) 2005-02-04 2012-08-01 Millennium Pharmaceuticals, Inc. Inhibitors of e1 activating enzymes
US7893267B2 (en) 2005-03-14 2011-02-22 High Point Pharmaceuticals, Llc Benzazole derivatives, compositions, and methods of use as β-secretase inhibitors
EP1881966A2 (en) 2005-05-03 2008-01-30 Dow AgroSciences LLC Substituted 4,5-dihydro-1,2,4-triazin-6-ones, 1,2,4-trianzin-6-ones, and their use as fungicides
NZ566180A (en) 2005-07-29 2011-04-29 Resverlogix Corp Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices
RU2008112691A (ru) 2005-10-03 2009-10-10 Оно Фармасьютикал Ко., Лтд. (Jp) Азотсодержащее гетероциклическое соединение и его фармацевтическое применение
US20070197532A1 (en) 2005-11-18 2007-08-23 Cao Sheldon X Glucokinase activators
AU2006319247B2 (en) 2005-12-01 2010-03-11 F. Hoffmann-La Roche Ag Heteroaryl substituted piperidine derivatives as L-CPT1 inhibitors
MX2008010611A (es) 2006-02-17 2008-11-12 Pfizer Ltd Derivados de 3-desazapurina como moduladores de receptores similares a toll.
CN101384593A (zh) 2006-02-17 2009-03-11 辉瑞有限公司 用作tlr7调节剂的3-脱氮嘌呤衍生物
EA200870404A1 (ru) 2006-04-03 2009-04-28 Глэксо Груп Лимитед Производные азабицикло[3.1.0.]гексила в качестве модуляторов рецепторов допамина d3
CA2700988A1 (en) 2006-09-27 2008-05-08 Surface Logix, Inc. Rho kinase inhibitors
MX2009006312A (es) 2006-12-14 2009-08-07 Astellas Pharma Inc Compuestos de acido policiclico utiles como antagonistas crth2 y agentes antialergicos.
SG144809A1 (en) 2007-01-11 2008-08-28 Millipore U K Ltd Benzimidazole compounds and their use as chromatographic ligands
MX2009008099A (es) 2007-02-01 2009-12-14 Resverlogix Corp Compuestos para la prevencion y tratamiento de enfermedades cardiovasculares.
WO2008153701A1 (en) 2007-05-24 2008-12-18 Schering Corporation Compounds for inhibiting ksp kinesin activity
CN101687815A (zh) 2007-06-26 2010-03-31 塞诺菲-安万特股份有限公司 苯并咪唑和氮杂苯并咪唑的区域选择性铜催化合成
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
DE102007038957A1 (de) 2007-08-17 2009-02-19 Merck Patent Gmbh 6-Thioxo-pyridazinderivate
GB0719235D0 (en) 2007-10-02 2007-11-14 Glaxo Group Ltd Novel compounds
WO2009054790A1 (en) 2007-10-26 2009-04-30 Astrazeneca Ab Amide linked heteroaromatic derivatives as modulators of mglur5
CA2708262A1 (en) 2007-12-07 2009-06-18 Elan Pharmaceuticals, Inc. Methods and compositions for treating liquid tumors
US8084466B2 (en) 2007-12-18 2011-12-27 Janssen Pharmaceutica Nv Bicyclic heteroaryl-substituted imidazoles as modulators of the histamine H4 receptor
KR101600634B1 (ko) 2007-12-28 2016-03-07 미쓰비시 타나베 파마 코퍼레이션 항암제
TW200942537A (en) 2008-02-01 2009-10-16 Irm Llc Compounds and compositions as kinase inhibitors
WO2009158258A1 (en) 2008-06-25 2009-12-30 E. I. Du Pont De Nemours And Company Herbicidal dihydro oxo six-membered azinyl isoxazolines
US9540322B2 (en) 2008-08-18 2017-01-10 Yale University MIF modulators
US9643922B2 (en) 2008-08-18 2017-05-09 Yale University MIF modulators
EA201170349A1 (ru) 2008-08-18 2011-08-30 Йейл Юниверсити Модуляторы mif
US8877772B2 (en) 2008-11-25 2014-11-04 University Of Rochester Substituted pyrrolo[2,3-B]pyridines as MLK inhibitors
PL2370413T3 (pl) 2008-12-08 2016-01-29 Arena Pharm Inc Modulatory receptora prostacykliny (PGI2) użyteczne w leczeniu zaburzeń z nimi związanych
EP2196465A1 (en) 2008-12-15 2010-06-16 Almirall, S.A. (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors
DE102008062826A1 (de) 2008-12-23 2010-07-01 Merck Patent Gmbh Pyridazinonderivate
US8389550B2 (en) 2009-02-25 2013-03-05 Hoffmann-La Roche Inc. Isoxazoles / O-pyridines with ethyl and ethenyl linker
EP2406236A4 (en) 2009-03-09 2013-07-24 Surface Logix Inc INHIBITORS OF RHO KINASE
NZ595747A (en) * 2009-03-18 2015-06-26 Resverlogix Corp Novel quinazolinones and related compounds for use as anti-inflammatory agents
EP2408449A4 (en) 2009-03-18 2012-08-08 Univ Leland Stanford Junior METHOD AND COMPOSITIONS FOR TREATING FLAVIVIRIDAE VIRUS INFECTIONS
EP2421533B1 (en) 2009-04-22 2018-10-17 Resverlogix Corp. Novel anti-inflammatory agents
JP5466292B2 (ja) 2009-05-05 2014-04-09 エフ.ホフマン−ラ ロシュ アーゲー イソオキサゾール−ピリジン誘導体
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
ES2652304T3 (es) 2009-11-05 2018-02-01 Glaxosmithkline Llc Compuesto de benzodiacepina novedoso
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
US9102677B2 (en) 2009-11-05 2015-08-11 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
WO2011062437A2 (ko) 2009-11-20 2011-05-26 에스케이케미칼주식회사 고나도트로핀 방출 호르몬 수용체 길항제, 이의 제조방법 및 이를 함유하는 약제학적 조성물
WO2011097607A1 (en) 2010-02-08 2011-08-11 Southern Research Institute Anti-viral treatment and assay to screen for anti-viral agent
KR101165996B1 (ko) 2010-04-23 2012-07-18 주식회사 녹십자 프탈라지논 유도체, 이의 제조방법 및 이를 함유하는 약학적 조성물
EP2902030B1 (en) 2010-05-14 2016-09-14 Dana-Farber Cancer Institute, Inc. Thienotriazolodiazepine compounds for treating neoplasia
WO2011156626A1 (en) 2010-06-09 2011-12-15 Rutgers, The State University Of New Jersey Antimicrobial agents
WO2011159926A1 (en) 2010-06-16 2011-12-22 Rutgers, The State University Of New Jersey Antimicrobial agents
WO2012003576A1 (en) 2010-07-06 2012-01-12 Université de Montréal Imidazopyridine, imidazopyrimidine and imidazopyrazine derivatives as melanocortin-4 receptor modulators
WO2012009258A2 (en) 2010-07-13 2012-01-19 Edward Roberts Peptidomimetic galanin receptor modulators
EP2603079B1 (en) 2010-08-12 2018-09-19 Merck Sharp & Dohme Corp. Positive allosteric modulators of mglur2
WO2012040499A2 (en) 2010-09-22 2012-03-29 Surface Logix, Inc. Metabolic inhibitors
KR101242572B1 (ko) 2010-10-12 2013-03-19 한국화학연구원 5-환 헤테로 아릴로 치환된 프탈라지논 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 약학적 조성물
GB201018147D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Method of treatment
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
CN102731409A (zh) 2011-04-08 2012-10-17 中国科学院上海药物研究所 一类哒嗪酮类化合物,其药物组合物、制备方法及用途
GB201106743D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
WO2012174487A2 (en) 2011-06-17 2012-12-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
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
JP6141863B2 (ja) 2011-12-01 2017-06-07 ケモセントリックス,インコーポレイティド Ccr(4)アンタゴニストとしての置換ベンズイミダゾール及びベンゾピラゾール
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20130281397A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281399A1 (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
US20130281398A1 (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
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
TR201807207T4 (tr) 2012-06-11 2018-06-21 Ucb Biopharma Sprl Tnf-alfa modüle edici benzimidazol bileşikleri.
EP2888256A4 (en) 2012-08-24 2016-02-17 Univ Texas HETEROCYCLIC HIF ACTIVITY MODULATORS FOR THE TREATMENT OF DISEASES
BR112015004858A2 (pt) 2012-09-05 2017-07-04 Bayer Cropscience Ag uso de 2-amidobenzimidazóis, 2-amidobenzoxazóis e 2-amidobenzotiazóis substituídos ou sais dos mesmos como substâncias ativas contra estresse abiótico em plantas
US20150246888A1 (en) 2012-09-11 2015-09-03 Michael Johnson Enoyl reductase inhibitors with antibacterial activity
ES2625945T3 (es) 2012-11-14 2017-07-21 Glaxosmithkline Llc Tieno[3,2-c]piridin-4(5H)-onas como inhibidores de bet
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
EP2935261A1 (de) 2012-12-20 2015-10-28 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydrochinoxalinone
MX2015007921A (es) 2012-12-21 2016-03-03 Zenith Epigenetics Corp Compuestos heterociclicos novedosos como inhibidores de bromodominio.
WO2014128111A1 (de) 2013-02-22 2014-08-28 Bayer Pharma Aktiengesellschaft 4-substituierte pyrrolo- und pyrazolo-diazepine
WO2014128070A1 (de) 2013-02-22 2014-08-28 Bayer Pharma Aktiengesellschaft Pyrrolo- und pyrazolo-triazolodiazepine als bet-proteininhibitoren zur behandlung von hyper-proliferativen erkrankungen
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
EP2961747B1 (en) 2013-02-27 2017-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
EP2970285B1 (en) 2013-03-11 2019-04-17 AbbVie Inc. Fused tetracyclic bromodomain inhibitors
JP2016512524A (ja) 2013-03-11 2016-04-28 アッヴィ・インコーポレイテッド ブロモドメイン阻害剤
CN105377851B (zh) 2013-03-11 2018-07-20 密执安州立大学董事会 Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法
HK1218909A1 (zh) 2013-03-12 2017-03-17 Abbvie Inc. 二氢-吡咯并吡啶酮布罗莫结构域抑制剂
CN105164113B (zh) 2013-03-12 2018-03-02 艾伯维公司 吡咯酰胺抑制剂
WO2014140077A1 (en) 2013-03-14 2014-09-18 Glaxosmithkline Intellectual Property (No.2) Limited Furopyridines as bromodomain inhibitors
ES2704048T3 (es) 2013-03-14 2019-03-14 Glaxosmithkline Ip No 2 Ltd Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina-2,3-disustituida y su uso como inhibidores de bromodominio
EP2968360B1 (en) 2013-03-14 2021-01-20 ConverGene LLC Quinolinone derivatives for the inhibition of bromodomain-containing proteins
MX366703B (es) 2013-03-15 2019-07-22 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de la proteína bet.
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
NZ630875A (en) 2013-03-15 2017-12-22 Plexxikon Inc Heterocyclic compounds and uses thereof
US20160039842A1 (en) 2013-03-15 2016-02-11 Epigenetix, Inc. Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors
EP2978758B1 (en) 2013-03-27 2017-02-08 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
EP2792355A1 (en) 2013-04-17 2014-10-22 Albert-Ludwigs-Universität Freiburg Compounds for use as bromodomain inhibitors
WO2014170350A1 (en) 2013-04-17 2014-10-23 Albert Ludwigs Universität Freiburg Compounds for use as bromodomain inhibitors
CA2901083A1 (en) 2013-04-26 2014-10-30 Beigene, Ltd. Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
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
EP3004109A1 (en) 2013-05-27 2016-04-13 Novartis AG Imidazopyrrolidinone derivatives and their use in the treatment of disease
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
CA2915419A1 (en) 2013-06-17 2014-12-24 Bayer Pharma Aktiengesellschaft Substituted phenyl-2,3-benzodiazepines
WO2015004534A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
CN105407888B (zh) 2013-06-21 2019-05-21 齐尼思表观遗传学有限公司 新双环溴结构域抑制剂
AR096758A1 (es) 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
JP2016525135A (ja) 2013-07-23 2016-08-22 バイエル ファーマ アクチエンゲゼルシャフト BETタンパク質およびポロ様キナーゼの二重阻害薬としての置換されたジヒドロピリド[3,4−b]ピラジノン類
CA2918910A1 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
JP6542212B2 (ja) 2013-07-31 2019-07-10 ゼニス・エピジェネティクス・リミテッドZenith Epigenetics Ltd. ブロモドメイン阻害剤としての新規キナゾリノン
US20150051208A1 (en) 2013-08-14 2015-02-19 Boehringer Ingelheim International Gmbh Pyridinones
BR112016011024B1 (pt) 2013-11-18 2020-09-01 Forma Therapeutics, Inc Composto, composição farmacêutica, e, usos dos mesmos
WO2015074081A1 (en) 2013-11-18 2015-05-21 Bair Kenneth W Benzopiperazine compositions as bet bromodomain inhibitors
GB201321739D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
US9458156B2 (en) 2014-12-23 2016-10-04 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
CA2966298A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
CA2966303A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
WO2016092375A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Corp. Substituted heterocycles as bromodomain inhibitors
WO2016097870A1 (en) 2014-12-17 2016-06-23 Zenith Epigenetics Corp. Substituted bicyclic compounds as bromodomain inhibitors
CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013064900A1 (en) * 2011-11-01 2013-05-10 Resverlogix Corp. Oral immediate release formulations for substituted quinazolinones

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
PAKRASHI S. C., "4-Quinazolinones. II. Self-condensation of anthranilamide", JOURNAL OF ORGANIC CHEMISTRY, (1971-03-01), vol. 36, no. 5, pages 642 - 645 *
VOITENKO ET AL., DOPOVIDI NATSIONAL'NOI AKADEMII NAUK UKRAINI, (2005), vol. 8, pages 132 - 138 *

Also Published As

Publication number Publication date
US9855271B2 (en) 2018-01-02
CA2919948C (en) 2020-07-21
US10500209B2 (en) 2019-12-10
KR20160038008A (ko) 2016-04-06
IL243479B (en) 2019-06-30
WO2015015318A4 (en) 2015-09-03
HK1218547A1 (en) 2017-02-24
EP3027604A2 (en) 2016-06-08
JP6542212B2 (ja) 2019-07-10
US20160193218A1 (en) 2016-07-07
CA2919948A1 (en) 2015-02-05
CN105593224B (zh) 2021-05-25
AU2014298051A1 (en) 2016-01-28
CN105593224A (zh) 2016-05-18
JP2016527263A (ja) 2016-09-08
US20180092924A1 (en) 2018-04-05
EA201690087A1 (ru) 2016-08-31
EP3027604A4 (en) 2016-12-14
EP3027604B1 (en) 2019-02-20
IL243479A0 (en) 2016-02-29
WO2015015318A2 (en) 2015-02-05
WO2015015318A3 (en) 2015-07-16

Similar Documents

Publication Publication Date Title
AU2014298051B2 (en) Novel quinazolinones as bromodomain inhibitors
US11026926B2 (en) Substituted bicyclic compounds as bromodomain inhibitors
US10231953B2 (en) Inhibitors of bromodomains
US9278940B2 (en) Cyclic amines as bromodomain inhibitors
EP3230277B1 (en) Substituted heterocycles as bromodomain inhibitors
EP3227280B1 (en) Substituted pyridines as bromodomain inhibitors
WO2016097870A1 (en) Substituted bicyclic compounds as bromodomain inhibitors
HK1245248A1 (en) Substituted heterocycles as bromodomain inhibitors
WO2016087936A1 (en) Substituted pyridinones as bromodomain inhibitors
HK1246273A1 (en) Substituted pyridines as bromodomain inhibitors
HK1218547B (en) Novel quinazolinones as bromodomain inhibitors

Legal Events

Date Code Title Description
PC1 Assignment before grant (sect. 113)

Owner name: ZENITH EPIGENETICS LTD.

Free format text: FORMER APPLICANT(S): ZENITH EPIGENETICS CORP.

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