SG11201703492RA - Diheteroaryl histone deacetylase inhibitors and their use in therapy - Google Patents

Diheteroaryl histone deacetylase inhibitors and their use in therapy

Info

Publication number
SG11201703492RA
SG11201703492RA SG11201703492RA SG11201703492RA SG11201703492RA SG 11201703492R A SG11201703492R A SG 11201703492RA SG 11201703492R A SG11201703492R A SG 11201703492RA SG 11201703492R A SG11201703492R A SG 11201703492RA SG 11201703492R A SG11201703492R A SG 11201703492RA
Authority
SG
Singapore
Prior art keywords
diheteroaryl
therapy
histone deacetylase
deacetylase inhibitors
inhibitors
Prior art date
Application number
SG11201703492RA
Other languages
English (en)
Inventor
Stephen Joseph Shuttleworth
Alexander Richard Liam Cecil
Somhairle Maccormick
William John Nodes
Cyrille Davy Tomassi
Franck Alexandre Silva
Original Assignee
Karus Therapeutics 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 Karus Therapeutics Ltd filed Critical Karus Therapeutics Ltd
Publication of SG11201703492RA publication Critical patent/SG11201703492RA/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/4985—Pyrazines or piperazines 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
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
SG11201703492RA 2014-10-29 2015-10-29 Diheteroaryl histone deacetylase inhibitors and their use in therapy SG11201703492RA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1419228.0A GB201419228D0 (en) 2014-10-29 2014-10-29 Compounds
PCT/GB2015/053260 WO2016067040A1 (en) 2014-10-29 2015-10-29 Diheteroaryl histone deacetylase inhibitors and their use in therapy

Publications (1)

Publication Number Publication Date
SG11201703492RA true SG11201703492RA (en) 2017-05-30

Family

ID=52103566

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201703492RA SG11201703492RA (en) 2014-10-29 2015-10-29 Diheteroaryl histone deacetylase inhibitors and their use in therapy

Country Status (13)

Country Link
US (1) US10407435B2 (enExample)
EP (1) EP3212625A1 (enExample)
JP (1) JP2017532357A (enExample)
KR (1) KR20170081194A (enExample)
CN (1) CN107001340A (enExample)
AU (1) AU2015340305B2 (enExample)
BR (1) BR112017008794A2 (enExample)
CA (1) CA2966072A1 (enExample)
GB (1) GB201419228D0 (enExample)
IL (1) IL251860A0 (enExample)
MX (1) MX2017005422A (enExample)
SG (1) SG11201703492RA (enExample)
WO (1) WO2016067040A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2015DN03235A (enExample) * 2012-11-07 2015-10-02 Karus Therapeutics Ltd
PT2994465T (pt) 2013-05-10 2018-10-25 Karus Therapeutics Ltd Novos inibidores de histona desacetilase
GB201419228D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201419264D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
US20180141897A1 (en) 2014-12-08 2018-05-24 The Research Foundation For The State University Of New York Anti-fungals targeting the synthesis of fungal shingolipids
WO2018232298A1 (en) 2017-06-16 2018-12-20 The Research Foundation For The State University Of New York Anti-fungals compounds targeting the synthesis of fungal sphingolipids
BR112021026334A2 (pt) 2019-06-27 2022-05-10 Medstar Health Macrófagos ativados por hdac6, composições, e usos dos mesmos
US11850233B2 (en) 2019-10-28 2023-12-26 Matibur Rahaman Zamadar Reduced adaptive microbial resistance treatment for flesh eating disease (necrotizing fasciitis)
CN112237994B (zh) * 2020-09-21 2022-09-13 昆明冶金研究院有限公司 一种多金属硫化矿硫化锌抑制剂及其制备方法与应用

Family Cites Families (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4017500A (en) 1973-07-16 1977-04-12 Schering Corporation Certain 8-amino-1,7-naphthyridines
DE2908324A1 (de) * 1979-03-03 1980-09-18 Hoechst Ag Triazolsubstituierte hydratopasaeurederivate, verfahren zu ihrer herstellung und ihre verwendung als pflanzenschutzmittel
US4792562A (en) 1985-12-04 1988-12-20 Hoechst-Roussel Pharmaceuticals, Inc. N-(pyrrol-1-yl)pyridinamines having memory enhancing activity
JPH0532662A (ja) * 1990-11-09 1993-02-09 Nissan Chem Ind Ltd 置換ピラゾール誘導体および農園芸用殺菌剤
US5214038A (en) 1991-04-15 1993-05-25 Hoechst-Roussel Pharmaceuticals Inc. 1-(pyrido[3,4-b]-1,4-oxazinyl-4-yl)-1H-indoles and intermediates for the preparation thereof
DE4120107A1 (de) * 1991-06-14 1992-12-17 Schering Ag Bicyclisch substituierte vinylimidazole, -triazole und -tetrazole
TW343965B (en) * 1994-03-30 1998-11-01 Hoffmann La Roche Novel mono- and bicyclic DNA gyrase inhibitors
JP2000511883A (ja) 1996-04-19 2000-09-12 ノボ ノルディスク アクティーゼルスカブ ホスホチロシン認識ユニットを有する分子のモジュレーター
EP0887348A1 (en) 1997-06-25 1998-12-30 Boehringer Mannheim Italia S.p.A. Bis-Indole derivatives having antimetastatic activity, a process for their preparation and pharmaceutical compositions containing them
JP3712529B2 (ja) 1998-04-24 2005-11-02 大鵬薬品工業株式会社 ３，３−ジピリジルアクリル酸アミド誘導体又はその薬学的に許容される塩
JP5278983B2 (ja) 1999-11-17 2013-09-04 塩野義製薬株式会社 アミド化合物の新規用途
GB9929988D0 (en) 1999-12-17 2000-02-09 Celltech Therapeutics Ltd Chemical compounds
US6608053B2 (en) 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
WO2001083456A1 (en) 2000-04-27 2001-11-08 Yamanouchi Pharmaceutical Co., Ltd. Condensed heteroaryl derivatives
JP2004502686A (ja) 2000-06-30 2004-01-29 スージェン・インコーポレーテッド ４−ヘテロアリール−３−ヘテロアリーリデニル−２−インドリノンおよび蛋白質キナーゼ阻害剤としてのその使用
JP2002255964A (ja) 2000-10-24 2002-09-11 Sankyo Co Ltd イミダゾピリジン誘導体
WO2002034748A1 (fr) 2000-10-24 2002-05-02 Sankyo Company, Limited Derives d'imidazopyridine
US6905669B2 (en) 2001-04-24 2005-06-14 Supergen, Inc. Compositions and methods for reestablishing gene transcription through inhibition of DNA methylation and histone deacetylase
US7429593B2 (en) 2001-09-14 2008-09-30 Shionogi & Co., Ltd. Utilities of amide compounds
ES2347544T3 (es) 2002-03-13 2010-11-02 Janssen Pharmaceutica Nv Inhibidores de histona-desacetilasas.
JP2003313126A (ja) 2002-04-23 2003-11-06 Sankyo Co Ltd イミダゾピリジン誘導体を有効成分とする医薬
JP2004002826A (ja) 2002-04-24 2004-01-08 Sankyo Co Ltd 高分子イミダゾピリジン誘導体
JP4235726B2 (ja) 2002-11-19 2009-03-11 国立大学法人 奈良先端科学技術大学院大学 大きな二光子吸収特性を示すアセチレン結合により連結されたビス（イミダゾリルポルフィリン金属錯体）を構成単位とするポルフィリン連鎖体及びその製造方法
AU2003900608A0 (en) 2003-02-11 2003-02-27 Fujisawa Pharmaceutical Co., Ltd. Hdac inhibitor
WO2005082887A1 (ja) 2004-02-26 2005-09-09 Aska Pharmaceutical Co., Ltd. ピリミジン誘導体
JP4698671B2 (ja) 2004-06-01 2011-06-08 エフ．ホフマン−ラ ロシュ アーゲー モノアミン再取り込み阻害剤としての３−アミノ−１−アリールプロピルインドール
CA2581489A1 (en) 2004-10-06 2006-04-13 Recepticon Aps Use of compounds for the prevention of drug-induced cell toxicity
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
EP1851219A1 (en) 2005-02-14 2007-11-07 Miikana Therapeutics, Inc. Fused heterocyclic compounds useful as inhibitors of histone deacetylase
CN101495116A (zh) 2005-03-22 2009-07-29 哈佛大学校长及研究员协会 蛋白降解病症的治疗
EP1881983B1 (en) 2005-05-20 2012-01-11 Vertex Pharmaceuticals, Inc. Pyrrolopyridines useful as inhibitors of protein kinase
TW200716545A (en) 2005-06-10 2007-05-01 Sigma Tau Ind Farmaceuti Indole derivatives having anti-tumor activity
AU2006306542B2 (en) 2005-10-21 2012-04-19 Merck Sharp & Dohme Corp. Potassium channel inhibitors
CA2635899A1 (en) 2006-01-19 2007-07-26 Osi Pharmaceuticals, Inc. Fused heterobicyclic kinase inhibitors
WO2007085540A1 (en) 2006-01-27 2007-08-02 Glaxo Group Limited 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives
MX2008013582A (es) 2006-04-26 2009-01-19 Hoffmann La Roche Derivados de pirimidina como inhibidores de fosfatidilinositol-3-c inasa.
KR101402474B1 (ko) 2006-04-26 2014-06-19 제넨테크, 인크. 포스포이노시티드 3-키나제 억제제 화합물 및 이를 포함하는 약학적 조성물
EP2050734A1 (en) 2006-07-13 2009-04-22 Kyowa Hakko Kirin Co., Ltd. Pentadienamide derivative
WO2008033746A2 (en) 2006-09-11 2008-03-20 Curis, Inc. Tyrosine kinase inhibitors containing a zinc binding moiety
CN103275067B (zh) 2006-10-28 2015-09-02 梅特希尔基因公司 组蛋白脱乙酰酶抑制剂
CA2670223A1 (en) 2006-11-22 2008-05-29 Karus Therapeutics Limited Depsipeptides and their therapeutic use
CN101663276A (zh) 2007-01-31 2010-03-03 沃泰克斯药物股份有限公司 用作激酶抑制剂的2-氨基吡啶衍生物
AU2008210455A1 (en) 2007-01-31 2008-08-07 Vertex Pharmaceuticals Incorporated 2-aminopyridine derivatives useful as kinase inhibitors
TWI539947B (zh) * 2007-04-09 2016-07-01 米希爾金尼公司 組蛋白去乙醯基酶之抑制劑
WO2008139987A1 (ja) 2007-04-26 2008-11-20 Japan Science And Technology Agency Ｇタンパク質共役型レセプタ－作動剤
WO2008137270A1 (en) 2007-05-04 2008-11-13 H. Lundbeck A/S Methods of diagnosing and monitoring of npy y5 based disorders
WO2008150827A1 (en) 2007-05-29 2008-12-11 Smithkline Beecham Corporation Naphthyridine, derivatives as p13 kinase inhibitors
GB0710528D0 (en) 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
WO2009063240A1 (en) 2007-11-16 2009-05-22 Arrow Therapeutics Limited 2,4-diaminopyrimidine derivatives useful as inhibitors of aurora kinase
WO2009137462A2 (en) 2008-05-05 2009-11-12 Envivo Pharmaceuticals, Inc. Methods for treating cognitive disorders using inhibitors of histone deacetylase
CA2732087A1 (en) 2008-08-05 2010-02-11 Boehringer Ingelheim International Gmbh Substituted naphthyridines and their use as medicaments
AU2009299894A1 (en) 2008-10-03 2010-04-08 Merck Serono S.A. 4 -morpholino-pyrido [3, 2 -d] pyrimidines active on Pi3k
GB2465405A (en) 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
MX2011007864A (es) 2009-01-28 2011-09-30 Karus Therapeutics Ltd Isosteros para realzar la transcripcion y su uso en terapia.
CN102498115B (zh) 2009-08-20 2016-12-07 卡鲁斯治疗有限公司 作为磷酸肌醇3-激酶抑制剂的三环杂环化合物
GB201007347D0 (en) 2010-04-30 2010-06-16 Karus Therapeutics Ltd Compounds
AU2011311531B2 (en) 2010-10-08 2014-11-20 Life Sciences Research Partners Vzw HDAC inhibitors to treat Charcot-Marie-Tooth disease
MX2013006858A (es) 2010-12-16 2013-07-29 Hoffmann La Roche Compuesto triciclicos inhibidores de la pi3k y metodos de uso.
WO2012106343A2 (en) 2011-02-01 2012-08-09 The Board Of Trustees Of The University Of Illinois Hdac inhibitors and therapeutic methods using the same
EP2508510A1 (en) 2011-04-06 2012-10-10 Ikerchem, S.L. Hydroxyphenyl pyrrole compounds containing an hydroxamic acid as hdac inhibitors and medicinal applications thereof
EP2734500A4 (en) 2011-07-20 2015-04-08 Gen Hospital Corp SELECTIVE HISTONDEACETYLASE-6 INHIBITORS FOR THE TREATMENT OF BONE DISORDERS
AU2012319188B2 (en) 2011-10-03 2016-11-24 Sloan-Kettering Institute For Cancer Research Novel molecules that selectively inhibit histone deacetylase 6 relative to histone deacetylase 1
JP6240078B2 (ja) 2011-10-04 2017-11-29 バルーク エス．ブルームバーグ インスティテュート 肝細胞癌を含む癌の阻害剤、および肝炎ウイルス複製の阻害剤としての置換アミノチアゾール
DK2790705T3 (en) 2011-12-15 2018-03-12 Novartis Ag Use of inhibitors of the activity or function of PI3K
KR101415742B1 (ko) 2011-12-21 2014-07-04 영남대학교 산학협력단 6―아미노피리딘―3―올 유도체 또는 이의 약제학적 허용가능한 염 및 이를 유효성분으로 함유하는 혈관신생으로 인한 질환의 예방 또는 치료용 약학조성물
GB201204125D0 (en) 2012-03-08 2012-04-25 Karus Therapeutics Ltd Compounds
WO2014032019A2 (en) 2012-08-23 2014-02-27 Georgetown University Compounds and methods of use thereof for treating tumors
IN2015DN03235A (enExample) 2012-11-07 2015-10-02 Karus Therapeutics Ltd
US9737521B2 (en) 2012-11-08 2017-08-22 Rhizen Pharmaceuticals Sa Pharmaceutical compositions containing a PDE4 inhibitor and a PI3 delta or dual PI3 delta-gamma kinase inhibitor
US9169214B2 (en) 2012-12-21 2015-10-27 The Board Of Trustees Of The Leland Stanford Junior University Compounds and compositions that bind and stabilize transthyretin and their use for inhibiting transthyretin amyloidosis and protein-protein interactions
WO2014139145A1 (en) 2013-03-15 2014-09-18 Hutchison Medipharma Limited Novel pyrimidine and pyridine compounds and usage thereof
WO2014153280A1 (en) 2013-03-22 2014-09-25 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
PT2994465T (pt) 2013-05-10 2018-10-25 Karus Therapeutics Ltd Novos inibidores de histona desacetilase
GB201402431D0 (en) 2014-02-12 2014-03-26 Karus Therapeutics Ltd Compounds
EP3187497A4 (en) 2014-08-26 2018-02-07 Takeda Pharmaceutical Company Limited Heterocyclic compound
GB201419264D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201419228D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201609786D0 (en) 2016-06-03 2016-07-20 Karus Therapeutics Ltd Compounds and method of use
US11066396B2 (en) 2016-06-23 2021-07-20 Merck Sharp & Dohme Corp. 3-aryl- heteroaryl substituted 5-trifluoromethyl oxadiazoles as histonedeacetylase 6 (HDAC6) inhibitors
WO2017222952A1 (en) 2016-06-23 2017-12-28 Merck Sharp & Dohme Corp. 3- heteroaryl substituted 5-trifluoromethyl oxadiazoles as histone deacetylase 6 (hdac6) inhibitors
WO2017222950A1 (en) 2016-06-23 2017-12-28 Merck Sharp & Dohme Corp. 3-heterocyclyl substituted 5-trifluoromethyl oxadiazoles as histone deacetylase 6 (hdac6) inhibitors

Also Published As

Publication number Publication date
AU2015340305B2 (en) 2018-12-06
MX2017005422A (es) 2017-08-24
BR112017008794A2 (pt) 2017-12-26
US10407435B2 (en) 2019-09-10
CN107001340A (zh) 2017-08-01
IL251860A0 (en) 2017-06-29
GB201419228D0 (en) 2014-12-10
CA2966072A1 (en) 2016-05-06
JP2017532357A (ja) 2017-11-02
WO2016067040A1 (en) 2016-05-06
KR20170081194A (ko) 2017-07-11
US20170313712A1 (en) 2017-11-02
AU2015340305A1 (en) 2017-05-18
EP3212625A1 (en) 2017-09-06

Similar Documents

Publication Publication Date Title
IL251618A0 (en) Combined treatment including ox40 binding agonists and tigit inhibitors
IL249476A0 (en) Combined treatment with glutaminase inhibitors
IL251860A0 (en) Dithyroaryl histone deacetylase inhibitors and their use in therapy
IL251051A0 (en) mk2 inhibitors and their uses
DK3256218T3 (da) Kdm1a-hæmmer og anvendelse deraf i terapi
GB201901338D0 (en) Histone deacetylase inhibitors for use in immunotherapy
PL3240777T3 (pl) Inhibitory arginazy oraz ich zastosowania terapeutyczne
IL245926A0 (en) Combinations of histone deacetylase inhibitors and immunomodulatory drugs
IL263360A (en) Combinations comprising histone deacetylase inhibitors
IL251861A0 (en) Polyheteroaryl histone deacetylase inhibitors and their use in therapy
IL249339A0 (en) Histone deacetylase inhibitors and compositions and methods of using them
HUE063848T2 (hu) LSD1 gátlók és gyógyászati alkalmazásaik
IL267238A (en) The paranase inhibitors and their use
IL255530A (en) Efflux-pump inhibitors and therapeutic uses thereof
IL251077B (en) Integrin inhibitors and their use
IL256438B (en) Histone deacetylase inhibitors
GB201406172D0 (en) Therapy and pharmaceutical composition
IL251078B (en) Integrin inhibitors and their use
IL267243A (en) The paranase inhibitors and their use
ZA201803212B (en) Gelatinase inhibitors and use thereof
HK1240920A1 (en) Diheteroaryl histone deacetylase inhibitors and their use in therapy
IL247872A0 (en) stat5 inhibitors and their uses
TH1501007058A (th) อนุพันธ์ไพราโซโลไพร์โรลิดีน และการใช้งานของพวกมันในการบำบัดโรค
GB201409978D0 (en) Novel compounds and their use in therapy
GB201404335D0 (en) Selective glycosidase inhibitors and uses thereof