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HRP20171961T1 - Kemijski spojevi - Google Patents

Kemijski spojevi Download PDF

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Publication number
HRP20171961T1
HRP20171961T1 HRP20171961TT HRP20171961T HRP20171961T1 HR P20171961 T1 HRP20171961 T1 HR P20171961T1 HR P20171961T T HRP20171961T T HR P20171961TT HR P20171961 T HRP20171961 T HR P20171961T HR P20171961 T1 HRP20171961 T1 HR P20171961T1
Authority
HR
Croatia
Prior art keywords
fluoro
pyrido
phenyl
indol
methylpropyl
Prior art date
Application number
HRP20171961TT
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English (en)
Inventor
Nadim AKHTAR
Robert Hugh Bradbury
David Buttar
Gordon Stuart Currie
Christopher De Savi
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 HRP20171961T1 publication Critical patent/HRP20171961T1/hr

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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

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  • 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. Spoj s formulom (I) [image] naznačen time da: R1 i R2 su svaki neovisno H ili F; R3 je H ili metil; i bilo koji od: a) R4 je H i R5 je F; ili b) R4 je F i R5 je H; ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da spoj je spoj s formulom (IA). [image]
3. Spoj prema zahtjevu 1 ili zahtjevu 2, ili farmaceutski prihvatljiva sol naznačen time da R3 je vodik.
4. Spoj prema bilo kojem od prethodnih zahtjeva, ili njegova farmaceutski prihvatljiva sol naznačen time da R4 je vodik i R5 je fluoro.
5. Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol naznačen time da je spoj odabran od: (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-enske kiseline.
6. Spoj prema zahtjevu 5, naznačen time da 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)akrilne kiseline, koji spoj ima slijedeću strukturu: [image] ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema zahtjevu 6 naznačen time da 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)akrilne kiseline.
8. Spoj prema zahtjevu 6 naznačen time da je maleatna sol (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. Spoj prema zahtjevu 7 u kristalnom obliku, naznačen time da ima uzorak difrakcije X-zraka na prahu (XRPD) s barem dva specifična maksimuma 2-theta = 8.4° i 10.9° pri čemu navedene vrijednosti mogu biti plus ili minus 0.2° 2-theta.
10. Spoj prema bilo kojem od prethodnih zahtjeva, ili njegova farmaceutski prihvatljiva sol naznačen time da je uporabu kao lijek.
11. Spoj prema bilo kojem od zahtjeva 1 do 9, ili njegova farmaceutski prihvatljiva sol naznačen time da je uporabu za sprječavanje ili liječenje raka kod toplokrvne životinje kao što je čovjek.
12. Spoj za uporabu za sprječavanje ili liječenje raka, prema zahtjevu 11, naznačen time da 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 njegova farmaceutski prihvatljiva sol.
13. Spoj za uporabu za liječenje raka, ili njegova farmaceutski prihvatljiva sol, prema zahtjevu 11 ili zahtjevu 12, naznačen time da rak je rak dojke ili ginekološki karcinom.
14. Farmaceutski pripravak naznačen time da sadrži spoj s Formulom (I) ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od zahtjeva 1 do 9, te farmaceutski prihvatljivo sredstvo za otapanje ili nosač.
15. Farmaceutski pripravak prema zahtjevu 14 naznačen time da 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)akrilne kiseline ili njegova farmaceutski prihvatljiva sol, u kombinaciji s barem jednim farmaceutski prihvatljivim sredstvom za otapanje ili nosačem, pri čemu pripravak sadrži manje od 5% m/m (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. Farmaceutski pripravak prema zahtjevu 15, naznačen time da pripravak dodatno sadrži antioksidans i proizvoljno dodatno sadrži sredstvo za keliranje metala.
HRP20171961TT 2013-05-28 2017-12-18 Kemijski spojevi HRP20171961T1 (hr)

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
EP14727036.7A EP3004090B1 (en) 2013-05-28 2014-05-27 Chemical compounds
PCT/GB2014/051607 WO2014191726A1 (en) 2013-05-28 2014-05-27 Chemical compounds

Publications (1)

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HRP20171961T1 true HRP20171961T1 (hr) 2018-02-09

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HRP20171961TT HRP20171961T1 (hr) 2013-05-28 2017-12-18 Kemijski spojevi

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US (4) US9155727B2 (hr)
EP (2) EP3360875A1 (hr)
JP (1) JP6286031B2 (hr)
KR (1) KR20160013198A (hr)
CN (1) CN105229004B (hr)
AP (1) AP2015008858A0 (hr)
AU (1) AU2014272856B2 (hr)
BR (1) BR112015029455A8 (hr)
CA (1) CA2911859A1 (hr)
CL (1) CL2015003491A1 (hr)
CR (1) CR20150629A (hr)
CY (1) CY1120474T1 (hr)
DK (1) DK3004090T3 (hr)
DO (1) DOP2015000274A (hr)
ES (1) ES2654161T3 (hr)
HK (1) HK1222859A1 (hr)
HR (1) HRP20171961T1 (hr)
HU (1) HUE035738T2 (hr)
IL (1) IL242559B (hr)
LT (1) LT3004090T (hr)
ME (1) ME02892B (hr)
MX (1) MX361538B (hr)
NI (1) NI201500167A (hr)
PE (1) PE20160874A1 (hr)
PH (1) PH12015502615B1 (hr)
PL (1) PL3004090T3 (hr)
PT (1) PT3004090T (hr)
RS (1) RS56678B1 (hr)
RU (1) RU2664109C2 (hr)
SG (1) SG11201509393VA (hr)
SI (1) SI3004090T1 (hr)
TN (1) TN2015000516A1 (hr)
TW (1) TWI653235B (hr)
UY (1) UY35590A (hr)
WO (1) WO2014191726A1 (hr)

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