ME02892B - Hemijska jedinjenja - Google Patents

Hemijska jedinjenja

Info

Publication number
ME02892B
ME02892B MEP-2017-292A MEP2017292A ME02892B ME 02892 B ME02892 B ME 02892B ME P2017292 A MEP2017292 A ME P2017292A ME 02892 B ME02892 B ME 02892B
Authority
ME
Montenegro
Prior art keywords
fluoro
pyrido
indol
phenyl
methylpropyl
Prior art date
Application number
MEP-2017-292A
Other languages
German (de)
English (en)
French (fr)
Inventor
Nadim Akhtar
Robert Hugh Bradbury
David Buttar
Gordon Stuart Currie
Savi Christopher De
Craig Samuel Donald
Richard Albert Norman
Matthew Osborne
Alfred Arthur Rabow
Heather Marie Redfearn
Helen Elizabeth Williams
Neda Yavari
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of ME02892B publication Critical patent/ME02892B/me

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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/145—Maleic acid
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (16)

1. Jedinjenje, naznačeno time, što ima Formulu (I) u kojoj: R1 i R2 su svaki nezavisno H ili F; R3 je H ili metil; i ili: a)R4 je H, a R5 je F; ili b)R4 je F, a R5 je H; ili neka njegova farmaceutski-prihvatljiva so.
2. Jedinjenje kao šta se zahteva u zahtevu 1, ili neka njegova farmaceutski-prihvatljiva so, naznačeno time, što ima formulu (IA).
3. Jedinjenje kao šta se zahteva u zahtevu 1 ili u zahtevu 2, ili neka njegova farmaceutski-prihvatljiva so, naznačeno time, što R3 je vodonik.
4. Jedinjenje kao šta se zahteva u bilo kojem od prethodnih zahteva, ili neka njegova farmaceutski-prihvatljiva so, naznačeno time, što R4 je vodonik, a R5 je fluoro.
5. Jedinjenje kao šta se zahteva u zahtevu 1 ili neka njegova farmaceutski-prihvatljiva so, naznačeno time, što je izabrano iz: (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(3,5-difluoro-4-((1R,3R)-2-((S)-3-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(4-((1R,3R)-2-((S)-3-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(3,5-difluoro-4-(2-((S)-3-fluoro-2-metilpropil)-3,3-dimetil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(3,5-difluoro-4-(2-(2-fluoro-2-metilpropil)-3,3-dimetil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(4-(2-((S)-3-fluoro-2-metilpropil)-3,3-dimetil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(4-(2-(2-fluoro-2-metilpropil)-3,3-dimetil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(3-fluoro-4-(2-((S)-3-fluoro-2-metilpropil)-3,3-dimetil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; i (E)-3-[4-[(1R,3R)-1-deuterio-2-(2-fluoro-2-metil-propil)-3-metil-4,9-dihidro-3H-pirido[3,4-b]indol-1-il]-3,5-difluoro-fenil]prop-2-enoične kiseline.
6. Jedinjenje kao šta se zahteva u zahtevu 5, naznačeno time, što je (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilna kiselina, pri čemu pomenuto jedinjenje ima sledeću strukturu: ili neka njegova farmaceutski-prihvatljiva so.
7. Jedinjenje kao šta se zahteva u zahtevu 6, naznačeno time, što je (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilna kiselina.
8. Jedinjenje kao šta se zahteva u zahtevu 6, naznačeno time, što je maleatna so (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline.
9. Jedinjenje kao šta se zahteva u zahtevu 7 u kristalnoj formi, naznačeno time, što ima obrazac difrakcije X-zraka na prahu (XRPD) sa najmanje dva specifična šiljka kod 2-teta = 8.4° i 10.9° pri čemu pomenute vrednosti mogu da variraju plus ili minus 0.2° 2-teta.
10. Jedinjenje kao šta se zahteva u bilo kojem od prethodnih zahteva ili neka njegova farmaceutski-prihvatljiva so, naznačeno time, što se upotrebljava kao medikament.
11. Jedinjenje kao šta se zahteva u bilo kojem od zahteva od 1 do 9 ili neka njegova farmaceutski-prihvatljiva so, naznačeno time, što se upotrebljava u prevenciji ili tretmanu raka kod toplo-krvnih životinja poput čoveka.
12. Jedinjenje za upotrebu u prevenciji ili tretmanu raka, kao šta se zahteva u zahtevu 11, naznačeno time, što je (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilna kiselina, ili neka njena farmaceutski-prihvatljiva so.
13. Jedinjenje za upotrebu u tretmanu raka, ili neka njegova farmaceutski-prihvatljiva so, kao šta se zahteva u zahtevu 11 ili zahtevu 12, naznačeno time, što pomenuti rak je rak dojke ili ginekološki rak.
14. Farmaceutska kompozicija, naznačena time, što sadrži jedinjenje sa Formulom (I) ili neku njegovu farmaceutski-prihvatljivu so, kao šta se zahteva u bilo kojem od zahteva od 1 do 9, i neki farmaceutski-prihvatljivi razređivač ili nosilac.
15. Farmaceutska kompozicija u skladu sa zahtevom 14 koja sadrži (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilnu kiselinu ili neku njezinu farmaceutski-prihvatljivu so, zajedno sa barem jednim farmaceutski-prihvatljivim razređivačem ili nosiocem, naznačena time, što pomenuta kompozicija sadrži manje od 5% w/w (R,E)-3-(3,5-difluoro-4-(2-(2-fluoro-2-metilpropil)-3-metil-4,9-dihidro-3H-pirido[3,4-b]indol-2-ium-1-il)fenil)akrilata.
16. Farmaceutska kompozicija u skladu sa zahtevom 15, naznačena time, što pomenuta kompozicija dodatno sadrži neki anti-oksidans i opciono dodatno sadrži neki metalo-helatni agens.
MEP-2017-292A 2013-05-28 2014-05-27 Hemijska jedinjenja ME02892B (me)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361827951P 2013-05-28 2013-05-28
US201361915685P 2013-12-13 2013-12-13
PCT/GB2014/051607 WO2014191726A1 (en) 2013-05-28 2014-05-27 Chemical compounds
EP14727036.7A EP3004090B1 (en) 2013-05-28 2014-05-27 Chemical compounds

Publications (1)

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ME02892B true ME02892B (me) 2018-04-20

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US (4) US9155727B2 (me)
EP (2) EP3360875A1 (me)
JP (1) JP6286031B2 (me)
KR (1) KR20160013198A (me)
CN (1) CN105229004B (me)
AP (1) AP2015008858A0 (me)
AU (1) AU2014272856B2 (me)
BR (1) BR112015029455A8 (me)
CA (1) CA2911859A1 (me)
CL (1) CL2015003491A1 (me)
CR (1) CR20150629A (me)
CY (1) CY1120474T1 (me)
DK (1) DK3004090T3 (me)
DO (1) DOP2015000274A (me)
ES (1) ES2654161T3 (me)
HR (1) HRP20171961T1 (me)
HU (1) HUE035738T2 (me)
IL (1) IL242559B (me)
LT (1) LT3004090T (me)
ME (1) ME02892B (me)
MX (1) MX361538B (me)
NI (1) NI201500167A (me)
PE (1) PE20160874A1 (me)
PH (1) PH12015502615B1 (me)
PL (1) PL3004090T3 (me)
PT (1) PT3004090T (me)
RS (1) RS56678B1 (me)
RU (1) RU2664109C2 (me)
SG (1) SG11201509393VA (me)
SI (1) SI3004090T1 (me)
SM (1) SMT201700589T1 (me)
TN (1) TN2015000516A1 (me)
TW (1) TWI653235B (me)
UY (1) UY35590A (me)
WO (1) WO2014191726A1 (me)

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