ME02867B - Nova jedinjenja - Google Patents

Nova jedinjenja

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Publication number
ME02867B
ME02867B MEP-2017-188A MEP2017188A ME02867B ME 02867 B ME02867 B ME 02867B ME P2017188 A MEP2017188 A ME P2017188A ME 02867 B ME02867 B ME 02867B
Authority
ME
Montenegro
Prior art keywords
pirolo
amin
butil
pirimidin
pentil
Prior art date
Application number
MEP-2017-188A
Other languages
German (de)
English (en)
French (fr)
Inventor
Diane Mary Coe
Stephen Allan Smith
Original Assignee
Glaxosmithkline Llc
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 Glaxosmithkline Llc filed Critical Glaxosmithkline Llc
Publication of ME02867B publication Critical patent/ME02867B/me

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/39Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/08Antiallergic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/555Medicinal preparations containing antigens or antibodies characterised by a specific combination antigen/adjuvant
    • A61K2039/55511Organic adjuvants

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (22)

1.Jedinjenje formule (I) ili njegova so gde R1 je n-C4-6alkil ili C1-2alkoksiC1-2alkil-; R2 je vodonik ili metil; svaki R3 je hidroksi, halo ili n-C1-3alkil; m je celi broj koji ima vrednost od 2 do 4; n je ceo broj koji ima vrednost od 0 do 3; p je ceo broj koji ima vrednost od 0 do 2.
2.Jedinjenje prema zahtevu 1, ili njegova so, gde je R1 n-butil.
3.Jedinjenje prema zahtevu 1, ili njegova so, gde je R1 etoksimetil.
4.Jedinjenje prema zahtevu 1, ili njegova so, gde je R1 2-metoksietil.
5.Jedinjenje prema bilo kom zahtevu 1-4, ili njegova so, gde je R2 vodonik.
6.Jedinjenje prema bilo kom zahtevu 1-4, ili njegova so, gde je R2 je metil.
7.Jedinjenje prema bilo kom zahtevu 1-6, ili njegova so, gde je n ceo broj koji ima vrednost 1 ili 2.
8.Jedinjenje prema bilo kom zahtevu 1-7, ili njegova so, gde je p 0.
9.Jedinjenje prema bilo kom zahtevu 1-7, ili njegova so, gde je R3 hidroksi ili halo.
10.Jedinjenje prema bilo kom zahtevu 1-7, ili njegova so, gde je p 1 i R3 je hidroksi ili fluoro.
11.Jedinjenje prema bilo kom od zahteva 1-7, ili njegova so, gde je p 2 i R3 je fluoro.
12.Jedinjenje prema zahtevu 1, ili njegova so, izabrano iz grupe koju čine: 2-Butil-7-(6-(piperidin-1-il)heksil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-7-(5-(piperidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-7-(4-(piperidin-1-il)butil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-(Etoksietil)-7-(6-(piperidin-1-il)heksil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-(2-Metoksietil)-7-(6-(piperidin-1-il)heksil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-6-metil-7-(6-(piperidin-1-il)heksil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-6-metil-7-(5-(piperidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-6-metil-7-(4-(piperidin-1-il)butil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-7-(5-(pirolidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-7-(6-(pirolidin-1-il)heksil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Pentil-7-(6-(piperidin-1-il)heksil)-5H-pirolo[3,2-d]pirimidin-4-amin; 7-(5-(Azepan-1-il)pentil)-2-butil-5H-pirolo[3,2-d]pirimidin-4-amin; 7-(4-(Azepan-1-il)butil)-2-butil-6-metil-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-6-metil-7-(6-(pirolidin-1-il)heksil)-5H-pirolo[3,2-d]pirimidin-4-amin; 7-(6-(Azetidin-1-il)heksil)-2-butil-6-metil-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-6-metil-7-(5-(pirolidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin; 7-(5-(Azetidin-1-il)pentil)-2-butil-5H-pirolo[3,2-d]pirimidin-4-amin; 7-(5-(Azetidin-1-il)pentil)-2-butil-6-metil-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-6-metil-7-(4-(pirolidin-1-il)butil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-7-(5-(4,4-difluoropiperidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-7-(5-(4-fluoropiperidin-l-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin; 7-(5-(4-Fluoropiperidin-1-il)pentil)-2-(2-metoksietil)-5H-pirolo[3,2-d]pirimidin-4-amin; 1-(5-(4-Amino-2-butil-5H-pirolo[3,2-d]pirimidin-7-il)pentil)piperidin-4-ol; (R)-2-Butil-7-(5-(3-fluoropirolidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin; (S)-2-Butil-7-(5-(3-fluoropirolidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin; (R)-7-(5-(3-Fluoropirolidin-1-il)pentil)-2-(2-metoksietil)-5H-pirolo[3,2-d]pirimidin-4-amin; (S)-7-(5-(3-Fluoropirolidin-1-il)pentil)-2-(2-metoksietil)-5H-pirolo[3,2-d]pirimidin-4-amin; (S)-1-(5-(4-Amino-2-butil-5H-pirolo[3,2-d]pirimidin-7-il)pentil)pirolidin-3-ol; 1-(5-(4-Amino-2-butil-5H-pirolo[3,2-d]pirimidin-7-il)pentil)azetidin-3-ol; 7-(6-(Azepan-1-il)heksil)-2-(2-metoksietil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-7-(6-(4-fluoropiperidin-1-il)heksil)-5H-pirolo[3,2-d]pirimidin-4-amin; (R)-2-Butil-7-(6-(3-fluoropirolidin-1-il)heksil)-5H-pirolo[3,2-d]pirimidin-4-amin; (S)-2-Butil-7-(6-(3-fluoropirolidin-1-il)heksil)-5H-pirolo[3,2-d]pirimidin-4-amin; (S)-2-Butil-7-(5-(2-metilpirolidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin; (R)-2-Butil-7-(5-(2-metilpirolidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-7-(5-(3-metilazetidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-7-(5-(3-fluoroazetidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-6-metil-7-(6-(pirolidin-1-il)heksil)-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-7-(5-(4-fluoropiperidin-1-il)pentil)-6-metil-5H-pirolo[3,2-d]pirimidin-4-amin; (S)-2-Butil-7-(5-(3-fluoropirolidin-1-il)pentil)-6-metil-5H-pirolo[3,2-d]pirimidin-4-amin; (R)-2-Butil-7-(5-(3-fluoropirolidin-1-il)pentil)-6-metil-5H-pirolo[3,2-d]pirimidin-4-amin; 2-Butil-7-(5-(3-fluoroazetidin-1-il)pentil)-6-metil-5H-pirolo[3,2-d]pirimidin-4-amin; i 2-(2-Metoksietil)-7-(5-(pirolidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin.
13.Jedinjenje prema zahtevu 1, koje je 2-butil-7-(5-(pirolidin-1-il)pentil)-5H-pirolo[3,2-d]pirimidin-4-amin ili njegova so.
14.Jedinjenje prema bilo kom od zahteva 1-13, koje je u obliku farmaceutske prihvatljive soli.
15.Jedinjenje prema bilo kom od zahteva 1-13, koje je u obliku slobodne baze.
16.Farmaceutska kompozicija koja sadrži jedinjenje koje je definisano prema bilo kom od zahteva 1-13, ili njegova farmaceutski prihvatljiva so, i jedan ili više farmaceutski prihvatljivih ekscipijenata.
17.Kompozicija vakcine koja sadrži jedinjenje definisano prema bilo kom od zahteva 1-13, ili njegovu farmaceutski prihvatljivu so i antigen ili antigenu kompoziciju.
18.Jedinjenje definisano prema bilo kom od zahteva 1-13, ili njegova farmaceutski prihvatljiva so za upotrebu u terapiji.
19.Jedinjenje koje je definisano prema bilo kom od zahteva 1-13, ili njegova farmaceutski prihvatljiva so, za upotrebu u lečenju alergijskog odgovora i drugih inflamatornih stanja, infektivnih bolesti i kancera.
20.Jedinjenje koje je definisano prema bilo kom od zahteva 1-13, ili njegova farmaceutski prihvatljiva so, za upotrebu u lečenju alergijskog rinitisa.
21.Jedinjenje koje je definisano prema bilo kom od zahteva 1-13, ili njegova farmaceutski prihvatljiva so, za upotrebu u lečenju astme.
22. Upotreba jedinjenja definisanog prema bilo kom od zahteva 1-13, ili njegove farmaceutski prihvatljive soli, u proizvodnji leka za lečenje alergijskih bolesti i drugih inflamatornih stanja, infektivnih bolesti i kancera.
MEP-2017-188A 2012-11-20 2013-11-18 Nova jedinjenja ME02867B (me)

Applications Claiming Priority (4)

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US201261728390P 2012-11-20 2012-11-20
US201361774087P 2013-03-07 2013-03-07
EP13857477.7A EP2922549B1 (en) 2012-11-20 2013-11-18 Novel compounds
PCT/US2013/070472 WO2014081645A1 (en) 2012-11-20 2013-11-18 Novel compounds

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US (3) US9540383B2 (me)
EP (1) EP2922549B1 (me)
JP (1) JP6228223B2 (me)
KR (1) KR20150085055A (me)
CN (1) CN104780922B (me)
AU (1) AU2013348218B2 (me)
BR (1) BR112015011400A8 (me)
CA (1) CA2892218A1 (me)
CL (1) CL2015001342A1 (me)
CR (1) CR20150268A (me)
CY (1) CY1119557T1 (me)
DK (1) DK2922549T3 (me)
DO (1) DOP2015000121A (me)
EA (1) EA028480B1 (me)
ES (1) ES2639789T3 (me)
HR (1) HRP20171150T1 (me)
HU (1) HUE13857477T2 (me)
IL (1) IL238800B (me)
LT (1) LT2922549T (me)
ME (1) ME02867B (me)
MX (1) MX358025B (me)
NZ (1) NZ707319A (me)
PE (1) PE20151086A1 (me)
PH (1) PH12015501100B1 (me)
PL (1) PL2922549T3 (me)
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RS (1) RS56233B1 (me)
SG (1) SG11201503282RA (me)
SI (1) SI2922549T1 (me)
SM (1) SMT201700378T1 (me)
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