CA2754890C - Bicyclic heterocycles - Google Patents

Bicyclic heterocycles Download PDF

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Publication number
CA2754890C
CA2754890C CA2754890A CA2754890A CA2754890C CA 2754890 C CA2754890 C CA 2754890C CA 2754890 A CA2754890 A CA 2754890A CA 2754890 A CA2754890 A CA 2754890A CA 2754890 C CA2754890 C CA 2754890C
Authority
CA
Canada
Prior art keywords
amino
thiazolo
piperazin
pyrimidin
pyrimidine
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.)
Expired - Fee Related
Application number
CA2754890A
Other languages
English (en)
French (fr)
Other versions
CA2754890A1 (en
Inventor
Piet Herdewijn
Steven De Jonghe
Ling-Jie Gao
Mi-Yeon Jang
Bart Vanderhoydonck
Mark Jozef Albert Waer
Yuan Lin
Jean Ferdinand Herman
Thierry Andre Michel Louat
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.)
Katholieke Universiteit Leuven
Original Assignee
Katholieke Universiteit Leuven
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
Priority claimed from GB0904353A external-priority patent/GB0904353D0/en
Priority claimed from GB0904373A external-priority patent/GB0904373D0/en
Priority claimed from GB0911022A external-priority patent/GB0911022D0/en
Application filed by Katholieke Universiteit Leuven filed Critical Katholieke Universiteit Leuven
Priority to CA2987743A priority Critical patent/CA2987743A1/en
Publication of CA2754890A1 publication Critical patent/CA2754890A1/en
Application granted granted Critical
Publication of CA2754890C publication Critical patent/CA2754890C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • 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
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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 two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2754890A 2009-03-13 2010-03-15 Bicyclic heterocycles Expired - Fee Related CA2754890C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA2987743A CA2987743A1 (en) 2009-03-13 2010-03-15 Purine derivatives and their use as immunosuppressive agents

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GB0904353A GB0904353D0 (en) 2009-03-13 2009-03-13 Novel thiazolopyrimidines
GB0904353.0 2009-03-13
GB0904373.8 2009-03-13
GB0904373A GB0904373D0 (en) 2009-03-13 2009-03-13 Novel thienopyrimidines
GB0911022.2 2009-06-26
GB0911022A GB0911022D0 (en) 2009-06-26 2009-06-26 Novel purines
PCT/EP2010/053318 WO2010103130A2 (en) 2009-03-13 2010-03-15 Novel bicyclic heterocycles

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CA2987743A Division CA2987743A1 (en) 2009-03-13 2010-03-15 Purine derivatives and their use as immunosuppressive agents

Publications (2)

Publication Number Publication Date
CA2754890A1 CA2754890A1 (en) 2010-09-16
CA2754890C true CA2754890C (en) 2018-01-16

Family

ID=42181129

Family Applications (2)

Application Number Title Priority Date Filing Date
CA2754890A Expired - Fee Related CA2754890C (en) 2009-03-13 2010-03-15 Bicyclic heterocycles
CA2987743A Abandoned CA2987743A1 (en) 2009-03-13 2010-03-15 Purine derivatives and their use as immunosuppressive agents

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA2987743A Abandoned CA2987743A1 (en) 2009-03-13 2010-03-15 Purine derivatives and their use as immunosuppressive agents

Country Status (6)

Country Link
US (2) US8901132B2 (https=)
EP (2) EP2405973B1 (https=)
JP (2) JP5647998B2 (https=)
CA (2) CA2754890C (https=)
ES (2) ES2665277T3 (https=)
WO (1) WO2010103130A2 (https=)

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Also Published As

Publication number Publication date
CA2987743A1 (en) 2010-09-16
ES2543216T3 (es) 2015-08-17
JP2015028088A (ja) 2015-02-12
JP6021880B2 (ja) 2016-11-09
EP2405973B1 (en) 2015-04-22
CA2754890A1 (en) 2010-09-16
JP5647998B2 (ja) 2015-01-07
WO2010103130A3 (en) 2010-12-23
WO2010103130A2 (en) 2010-09-16
JP2012520269A (ja) 2012-09-06
ES2665277T3 (es) 2018-04-25
EP2923734A1 (en) 2015-09-30
US20120046278A1 (en) 2012-02-23
US8901132B2 (en) 2014-12-02
US20150038494A1 (en) 2015-02-05
US9221822B2 (en) 2015-12-29
EP2923734B1 (en) 2018-01-10
EP2405973A2 (en) 2012-01-18

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