AU2017330443B2 - Chromobox protein inhibitors and uses thereof - Google Patents

Chromobox protein inhibitors and uses thereof Download PDF

Info

Publication number
AU2017330443B2
AU2017330443B2 AU2017330443A AU2017330443A AU2017330443B2 AU 2017330443 B2 AU2017330443 B2 AU 2017330443B2 AU 2017330443 A AU2017330443 A AU 2017330443A AU 2017330443 A AU2017330443 A AU 2017330443A AU 2017330443 B2 AU2017330443 B2 AU 2017330443B2
Authority
AU
Australia
Prior art keywords
acv
compound
compounds
cancer
cbx
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.)
Active
Application number
AU2017330443A
Other languages
English (en)
Other versions
AU2017330443A1 (en
Inventor
James E. Bradner
Alexander FEDERATION
Zoe JACOBSON
Jun Qi
Anthony VARCA
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 AU2017330443A1 publication Critical patent/AU2017330443A1/en
Application granted granted Critical
Publication of AU2017330443B2 publication Critical patent/AU2017330443B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/46—Iso-indoles; Hydrogenated iso-indoles with an oxygen atom in position 1
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/48—Acylated amino or imino radicals by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof, e.g. carbonylguanidines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
    • C07D277/38—Nitrogen atoms
    • C07D277/50—Nitrogen atoms bound to hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
    • C07D277/54—Nitrogen and either oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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 in position 2
    • C07D277/82—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/12—1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/18—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Indole Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2017330443A 2016-09-26 2017-09-25 Chromobox protein inhibitors and uses thereof Active AU2017330443B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662399857P 2016-09-26 2016-09-26
US62/399,857 2016-09-26
PCT/US2017/053229 WO2018058029A1 (en) 2016-09-26 2017-09-25 Chromobox protein inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
AU2017330443A1 AU2017330443A1 (en) 2019-03-21
AU2017330443B2 true AU2017330443B2 (en) 2023-08-24

Family

ID=61690673

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017330443A Active AU2017330443B2 (en) 2016-09-26 2017-09-25 Chromobox protein inhibitors and uses thereof

Country Status (6)

Country Link
US (2) US12129248B2 (OSRAM)
EP (1) EP3515449B1 (OSRAM)
JP (2) JP7203018B2 (OSRAM)
AU (1) AU2017330443B2 (OSRAM)
CA (1) CA3034652A1 (OSRAM)
WO (1) WO2018058029A1 (OSRAM)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019147706A1 (en) * 2018-01-23 2019-08-01 National Jewish Health Methods of treating steroid resistant diseases or conditions
US20220144812A1 (en) * 2019-03-28 2022-05-12 Epizyme, Inc. Quinoline derivatives and their use for the treatment of cancer
CN113336759B (zh) * 2020-12-25 2022-12-06 中国药科大学 溴结构域蛋白4小分子抑制剂、其制备方法及应用
EP4608514A1 (en) * 2022-10-24 2025-09-03 CeMM - Forschungszentrum für Molekulare Medizin GmbH Tasl mimicking molecules and applications thereof
WO2024108227A1 (en) * 2022-11-18 2024-05-23 The Regents Of The University Of Colorado, A Body Corporate Cbx2 inhibitory compounds for treating high grade serous ovarian cancer
CN116354959B (zh) * 2023-03-10 2024-04-19 石河子大学 一种N-N桥连噻唑单元的β-咔啉衍生物及其制备方法、应用
CN116554123A (zh) * 2023-04-27 2023-08-08 山东大学 六种噻唑酰腙类化合物在抗肿瘤药物中的应用

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998057931A2 (en) * 1997-06-19 1998-12-23 Sepracor Inc. Quinoline-indole antimicrobial agents, uses and compositions related thereto
WO2008154207A1 (en) * 2007-06-08 2008-12-18 The Burnham Institute For Medical Research Methods and compounds for regulating apoptosis
WO2010151799A2 (en) * 2009-06-26 2010-12-29 University Of Massachusetts Compounds for modulating rna binding proteins and uses therefor
EP2325181A1 (en) * 2008-07-10 2011-05-25 Pharma Ip General Incorporated Association Stat3 inhibitor containing quinolinecarboxamide derivative as active ingredient
WO2012122370A2 (en) * 2011-03-08 2012-09-13 Eutropics Pharmaceuticals, Inc. Compositions and methods useful for treating diseases
WO2016077632A2 (en) * 2014-11-13 2016-05-19 Buck Institute For Research On Aging Inhibition of proline catabolism for the treatment of cancer and other therapeutic applications

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4172896A (en) 1978-06-05 1979-10-30 Dainippon Pharmaceutical Co., Ltd. Methane-sulfonamide derivatives, the preparation thereof and composition comprising the same
US5645988A (en) 1991-05-08 1997-07-08 The United States Of America As Represented By The Department Of Health And Human Services Methods of identifying drugs with selective effects against cancer cells
GB9217295D0 (en) 1992-08-14 1992-09-30 Wellcome Found Controlled released tablets
US5541231A (en) 1993-07-30 1996-07-30 Glaxo Wellcome Inc. Stabilized Pharmaceutical
GB9315856D0 (en) 1993-07-30 1993-09-15 Wellcome Found Stabilized pharmaceutical
US5358970A (en) 1993-08-12 1994-10-25 Burroughs Wellcome Co. Pharmaceutical composition containing bupropion hydrochloride and a stabilizer
CN100408100C (zh) 1997-07-29 2008-08-06 阿尔康实验室公司 含半乳甘露聚糖聚合物和硼酸盐的眼用组合物
JP2002501892A (ja) 1998-01-29 2002-01-22 セプラコア インコーポレーテッド 光学的に純粋な（−）−ビュープロピオンの薬学的使用
US8889112B2 (en) 1999-09-16 2014-11-18 Ocularis Pharma, Llc Ophthalmic formulations including selective alpha 1 antagonists
US6933289B2 (en) 2003-07-01 2005-08-23 Allergan, Inc. Inhibition of irritating side effects associated with use of a topical ophthalmic medication
US8512717B2 (en) 2003-08-07 2013-08-20 Allergan, Inc. Compositions for delivery of therapeutics into the eyes and methods for making and using same
US20050059744A1 (en) 2003-09-12 2005-03-17 Allergan, Inc. Methods and compositions for the treatment of pain and other alpha 2 adrenergic-mediated conditions
WO2006044826A2 (en) 2004-10-20 2006-04-27 Compass Pharmaceuticals Llc Thiophens and their use as anti-tumor agents
AU2006218405A1 (en) * 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Acridine and quinoline derivatives as sirtuin modulators
US20070099970A1 (en) 2005-08-19 2007-05-03 Mackerell Alexander Immunomodulatory compounds that target and inhibit the pY'binding site of tyrosene kinase p56 LCK SH2 domain
CA2631082C (en) 2005-11-23 2015-02-03 Board Of Regents Of The University Of Texas System Oncogenic ras-specific cytotoxic compound and methods of use thereof
DK2078197T3 (en) * 2006-11-01 2016-05-23 Ventana Med Syst Inc Haptenes, hapten conjugates, compositions thereof and processes for their preparation and use
WO2008090327A1 (en) 2007-01-22 2008-07-31 Betagenon Ab New combination for use in the treatment of cancer
US8183236B2 (en) 2007-04-12 2012-05-22 University Of Southern California Compounds with HIV-1 integrase inhibitory activity and use thereof as anti-HIV/AIDS therapeutics
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2009089277A2 (en) 2008-01-08 2009-07-16 The Trustees Of The University Of Pennsylvania Rel inhibitors and methods of use thereof
WO2010039538A2 (en) 2008-09-23 2010-04-08 Georgetown University Flavivirus inhibitors and methods for their use
CA2787784A1 (en) 2010-01-29 2011-08-04 Dana-Farber Cancer Institute, Inc. Small molecules for the modulation of mcl-1 and methods of modulating cell death, cell division, cell differentiation and methods of treating disorders
EP2635280A4 (en) 2010-11-05 2014-05-28 Univ Minnesota CYTOSINDEAMINASE MODULATORS TO IMPROVE DNA TRANSFECTION
WO2013059944A1 (en) 2011-10-28 2013-05-02 British Columbia Cancer Agency Branch Epigenetic regulators and uses thereof
KR102438072B1 (ko) 2012-01-12 2022-08-31 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
US9261497B2 (en) 2012-10-16 2016-02-16 New York University Method of treating cancer with modulators of SCFSkp2
US9562002B2 (en) 2013-01-15 2017-02-07 Board Of Regents, The University Of Texas System STAT3 inhibitor
CN105102442B (zh) 2013-03-18 2018-11-09 基因科学医药公司 作为抗癌药的喹啉衍生物
CN105473580A (zh) 2013-07-10 2016-04-06 葛兰素史密斯克莱知识产权（第2号）有限公司 Zeste同源物增强子2抑制剂
WO2016004035A1 (en) 2014-07-01 2016-01-07 Icahn School Of Medicine At Mount Sinai 2-aryl-4-quinolinecarboxamide derivatives for treating thyroid diseases

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998057931A2 (en) * 1997-06-19 1998-12-23 Sepracor Inc. Quinoline-indole antimicrobial agents, uses and compositions related thereto
WO2008154207A1 (en) * 2007-06-08 2008-12-18 The Burnham Institute For Medical Research Methods and compounds for regulating apoptosis
EP2325181A1 (en) * 2008-07-10 2011-05-25 Pharma Ip General Incorporated Association Stat3 inhibitor containing quinolinecarboxamide derivative as active ingredient
WO2010151799A2 (en) * 2009-06-26 2010-12-29 University Of Massachusetts Compounds for modulating rna binding proteins and uses therefor
WO2012122370A2 (en) * 2011-03-08 2012-09-13 Eutropics Pharmaceuticals, Inc. Compositions and methods useful for treating diseases
WO2016077632A2 (en) * 2014-11-13 2016-05-19 Buck Institute For Research On Aging Inhibition of proline catabolism for the treatment of cancer and other therapeutic applications

Non-Patent Citations (10)

* Cited by examiner, † Cited by third party
Title
Abd El-Aal, H. A. K. et al., ‘Efficient synthesis, characterization and biological evaluation of some new atophan carbohydrazide derivatives’, Journal of Chemical and Pharmaceutical Research. 2014, vol.6, pages 90-99 *
Belen’kaya, R. S. et al., ‘Synthesis of nitrogenous derivatives of 2-phenyl- and 1-(2,2'-dithienyl-5-yl)cinchoninic acid’, Khimiko-Farmatsevticheskii Zhurnal. 1974, vol.8, pages 19-23 *
CAS Registry Number 1061510-34-6; STN Entry Date 15 October 2008; 2-(3-Pyridinyl)-N-[4-(1-pyrrolidinyl)phenyl]-4-quinolinecarboxamide *
CAS Registry Number 1378176-70-5; STN Entry Date 14 June 2012; N-[1-(1H-Imidazol-2-yl)ethyl]-2-(4-methylphenyl)-4-quinolinecarboxamide *
CAS Registry Number 1624164-86-8; STN Entry Date 22 September 2014; 2-(2-Furanyl)-N-[3-(4-methyl-1-piperazinyl)propyl]-4-quinolinecarboxamide *
CAS Registry Number 1625513-10-1; STN Entry Date 24 September 2014; N-[4-[3-(Dimethylamino)propoxy]phenyl]-2-(3-pyridinyl)-4-quinolinecarboxamide *
CAS Registry Number 730948-00-2; STN Entry Date 23 August 2004; 2-(2-Furanyl)-N-[3-(4-morpholinyl)propyl]-4-quinolinecarboxamide *
Dahal, U. P. et al., ‘Small Molecule Quantification by Liquid Chromatography-Mass Spectrometry for Metabolites of Drugs and Drug Candidates’, DRUG METABOLISM AND DISPOSITION. 2011, vol.39, pages 2355-2360 *
KENJI MATSUNO ET AL: "Identification of a New Series of STAT3 Inhibitors by Virtual Screening", ACS MEDICINAL CHEMISTRY LETTERS, AMERICAN CHEMICAL SOCIETY, US, vol. 1, no. 8, January 2010 (2010-01-01), pages 371 - 375 *
MICHAEL PODVINEC ET AL: "Novel Inhibitors of Dengue Virus Methyltransferase: Discovery by in Vitro-Driven Virtual Screening on a Desktop Computer Grid", JOURNAL OF MEDICINAL CHEMISTRY, vol. 53, no. 4, 25 February 2010 (2010-02-25) *

Also Published As

Publication number Publication date
EP3515449B1 (en) 2023-07-12
EP4275759A3 (en) 2024-01-17
WO2018058029A1 (en) 2018-03-29
CA3034652A1 (en) 2018-03-29
JP2022174272A (ja) 2022-11-22
EP3515449A4 (en) 2020-08-05
EP4275759A2 (en) 2023-11-15
EP3515449A1 (en) 2019-07-31
JP2019534865A (ja) 2019-12-05
US20200024267A1 (en) 2020-01-23
AU2017330443A1 (en) 2019-03-21
US12129248B2 (en) 2024-10-29
US20250034126A1 (en) 2025-01-30
JP7203018B2 (ja) 2023-01-12

Similar Documents

Publication Publication Date Title
AU2017330443B2 (en) Chromobox protein inhibitors and uses thereof
AU2018346331B2 (en) Small molecule inhibition of transcription factor SALL4 and uses thereof
AU2011280297B2 (en) Cyclic N,N'-diarylthioureas and N,N'-diarylureas as androgen receptor antagonists, anti-cancer agent, method for producing and using same
EP3570843A1 (en) Fused heterocyclic compounds as selective bmp inhibitors
US11382908B2 (en) Compositions and methods for treating inflammatory bowel disease
CA3083228A1 (en) Small molecule degraders that recruit dcaft15
WO2019178383A1 (en) Inhibition of bmp signaling, compounds, compositions and uses thereof
WO2023129513A2 (en) Bicyclic heteroaromatic inhibitors of nicotinamide n-methyltransferase, and compositions and uses thereof
US12479852B2 (en) Compounds, compositions, and methods for protein degradation
EP4275759B1 (en) Quinoline derivatives as chromobox (cbx) protein inhibitors for treating cancer
AU2016226036A1 (en) Salicylate inhibitors of MELK and methods of use
AU2017355566A1 (en) Inhibitors of mtor-deptor interactions and methods of use thereof
CN111108083A (zh) 氨基亚甲基环己烷1,3-二酮化合物的用途
Class et al. Patent application title: INHIBITORS OF MTOR-DEPTOR INTERACTIONS AND METHODS OF USE THEREOF
WO2023225311A1 (en) 1,4,5-trisubstituted-1,2,3-triazoles and uses thereof
EA049776B1 (ru) Композиции и способы для лечения мышечных дистрофий

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)