HRP20210957T1 - Spojevi inhibitori autotaksina - Google Patents

Spojevi inhibitori autotaksina Download PDF

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Publication number
HRP20210957T1
HRP20210957T1 HRP20210957TT HRP20210957T HRP20210957T1 HR P20210957 T1 HRP20210957 T1 HR P20210957T1 HR P20210957T T HRP20210957T T HR P20210957TT HR P20210957 T HRP20210957 T HR P20210957T HR P20210957 T1 HRP20210957 T1 HR P20210957T1
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Croatia
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substituted
indol
thio
pharmaceutically acceptable
solvate
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HRP20210957TT
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John Howard Hutchinson
David Lonergan
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Sabre Therapeutics Llc
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Publication of HRP20210957T1 publication Critical patent/HRP20210957T1/hr

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    • 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
    • C07D401/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Nutrition Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (14)

1. Spoj, naznačen time, da ima Formulu (III), ili njegova farmaceutski prihvatljiva sol, ili solvat: [image] u kojoj R1 je -Cl, -Br, ili -CN; R2 je Cl; R3 je H, F ili Cl; W je CH, CF ili N; RA jest H; L1 je odsutan, C1-C6 alkilen, ili C3-C6 cikloalkilen; Q je -CO2H, ili -CO2(C1-C6 alkil); Prsten B je furanil, pirolil, oksazolil, tiazolil, imidazolil, pirazolil, triazolil, tetrazolil, izoksazolil, izotiazolil, oksadiazolil, tiadiazolil, piridinil, pirimidinil, pirazinil, piridazinil, ili triazinil; svaki RB je neovisno H, halogen, -CN, -NO2, -OH, OR9, -SR9, -S(=O)R9, -S(=O)2R9, -S(=O)2N(R10)2, C1-C6 alkil, C1-C6 fluoroalkil, C1-C6 deuteroalkil, C1-C6 heteroalkil, supstituirani ili nesupstituirani C3-C10 cikloalkil, supstituirani ili nesupstituirani C2-C10 heterocikloalkil, supstituirani ili nesupstituirani fenil, C1-C4 alkilen-(supstituirani ili nesupstituirani fenil), supstituirani ili nesupstituirani monociklički heteroaril, C1-C4 alkilen-(supstituirani ili nesupstituirani monociklički heteroaril), supstituirani ili nesupstituirani biciklički heteroaril, ili C1-C4 alkilen-(supstituirani ili nesupstituirani biciklički heteroaril); n je 0, 1 ili 2; R9 je C1-C6 alkil, C1-C6 fluoroalkil, C1-C6 deuteroalkil, C3-C6 cikloalkil, supstituirani ili nesupstituirani fenil, supstituirani ili nesupstituirani monociklički heteroaril, supstituirani ili nesupstituirani biciklički heteroaril; svaki R10 je neovisno H, C1-C6 alkil, C1-C6 fluoroalkil, C1-C6 deuteroalkil, C3-C6 cikloalkil, supstituirani ili nesupstituirani fenil, ili supstituirani ili nesupstituirani monociklički heteroaril; ili se dvije skupine R10 koje su vezane na isti N atom, uzimaju zajedno s N atomom na kojega su vezane, kako bi tvorile supstituiranu ili nesupstituiranu heterocikličku strukturu; pri čemu su supstituirane skupine supstituirane s jednom ili više skupina pojedinačno i neovisno odabranih od halogena, -CN, NH2, -OH, -NH(CH3), -N(CH3)2, -CH3, -CH2CH3, -CF3, -OCH3 i -OCF3; i pritom se izraz „alkil“ kao sam ili u izrazu „heteroalkil“, također odnosi na vrstu alkilne skupine u kojoj se nalazi najmanje jedna dvostruka veza ugljik-ugljik.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, ili solvat, naznačeni time, da: L1 je odsutan, -CH2-, -CH(CH3)-, -C(CH3)2-, ili ciklopropil-1,1-diil.
3. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj ima sljedeću strukturu: [image] u kojoj RA jest H; RB je H, C1-C6 alkil, C1-C6 fluoroalkil, ili C1-C6 deuteroalkil, R1 je -Cl, -Br, ili -CN; R2 jest Cl; i R3 je H, F ili Cl; ili njegova farmaceutski prihvatljiva sol, ili solvat.
4. Spoj prema patentnom zahtjevu 3, naznačen time, da spoj ima sljedeću strukturu: [image] ili njegova farmaceutski prihvatljiva sol, ili solvat.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, ili njegova farmaceutski prihvatljiva sol, ili solvat, naznačeni time, da: RB jest C1-C6 alkil.
6. Spoj prema bilo kojem od patentnih zahtjeva 3 do 5, ili njegova farmaceutski prihvatljiva sol, ili solvat, naznačeni time, da: L1 je odsutan, -CH2-, -CH(CH3)-, -C(CH3)2-, ili ciklopropil-1,1-diil.
7. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5, ili njegova farmaceutski prihvatljiva sol, ili solvat, naznačeni time, da: L1 je odsutan.
8. Spoj prema patentnom zahtjevu 1, naznačen time, da je spoj: 3-((2,6-dikloro-1-(1-propil-1H-pirazol-4-il)-1H-indol-3-il)tio)benzojeva kiselina; 3-((6-kloro-2-cijano-1-(1-propil-1H-pirazol-4-il)-1H-indol-3-il)tio)benzojeva kiselina; 3-((2,6-dikloro-7-fluoro-1-(1-propil-1H-pirazol-4-il)-1H-indol-3-il)tio)benzojeva kiselina; 3-((2-bromo-6-kloro-1-(1-propil-1H-pirazol-4-il)-1H-indol-3-il)tio)benzojeva kiselina; 3-((2,6-dikloro-7-fluoro-1-(1-propil-1H-pirazol-4-il)-1H-indol-3-il)tio)-2-fluorobenzojeva kiselina; 3-((2,6-dikloro-7-fluoro-1-(1-metil-1H-pirazol-4-il)-1H-indol-3-il)tio)-2-fluorobenzojeva kiselina; 3-((2,6-dikloro-1-(1-etil-1H-pirazol-4-il)-7-fluoro-1H-indol-3-il)tio)-2-fluorobenzojeva kiselina; 3-((2,6-dikloro-7-fluoro-1-(1-piridin-3-il)-1H-indol-3-il)tio)-2-fluorobenzojeva kiselina; 3-((2-bromo-6-kloro-7-fluoro-1-(piridin-3-il)-1H-indol-3-il)tio)-2-fluorobenzojeva kiselina; ili njegova farmaceutski prihvatljiva sol, ili solvat.
9. Spoj prema patentnom zahtjevu 1, naznačen time, da je spoj: 3-((2,6-dikloro-7-fluoro-1-(1-propil-1H-pirazol-4-il)-1H-indol-3-il)tio)-1-fluorobenzojeva kiselina; 3-((2,6-dikloro-7-fluoro-1-(1-metil-1H-pirazol-4-il)-1H-indol-3-il)tio)-2-fluorobenzojeva kiselina; 3-((2,6-dikloro-1-(1-etil-1H-pirazol-4-il)-7-fluoro-1H-indol-3-il)tio)-2-fluorobenzojeva kiselina; ili njegova farmaceutski prihvatljiva sol, ili solvat.
10. Spoj prema patentnom zahtjevu 1, naznačen time, da je spoj: 3-((2,6-dikloro-7-fluoro-1-(1-metil-1H-pirazol-4-il)-1H-indol-3-il)tio)-2-fluorobenzojeva kiselina; ili njegova farmaceutski prihvatljiva sol, ili solvat.
11. Spoj prema patentnom zahtjevu 1, naznačen time, da je spoj: 3-((2,6-dikloro-1-(1-etil-1H-pirazol-4-il)-7-fluoro-1H-indol-3-il)tio)-2-fluorobenzojeva kiselina; ili njegova farmaceutski prihvatljiva sol, ili solvat.
12. Farmaceutski pripravak, naznačen time, da sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 11 ili njegovu farmaceutski prihvatljivu sol, ili solvat, i najmanje jedno farmaceutski prihvatljivo pomoćno sredstvo.
13. Farmaceutski pripravak prema patentnom zahtjevu 12, naznačen time, da se farmaceutski pripravak nalazi u obliku tablete, pilule, kapsule, tekućine, suspenzije, gela, disperzije, otopine, emulzije, masti, ili losiona.
14. Spoj prema bilo kojem od patentnih zahtjeva 1 do 11, ili njegova farmaceutski prihvatljiva sol, ili solvat, naznačeni time, da su za uporabu u postupku liječenja sisavaca putem terapije, ili za uporabu u postupku liječenja fibroze ili raka kod sisavca.
HRP20210957TT 2013-11-22 2021-06-15 Spojevi inhibitori autotaksina HRP20210957T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361907965P 2013-11-22 2013-11-22
US201462038121P 2014-08-15 2014-08-15
PCT/US2014/066706 WO2015077503A1 (en) 2013-11-22 2014-11-20 Autotaxin inhibitor compounds
EP14864293.7A EP3071561B1 (en) 2013-11-22 2014-11-20 Autotaxin inhibitor compounds

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HRP20210957T1 true HRP20210957T1 (hr) 2021-09-17

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US (6) US9334261B2 (hr)
EP (2) EP3878848A1 (hr)
JP (1) JP6501367B2 (hr)
KR (2) KR102515248B1 (hr)
CN (2) CN110372671B (hr)
AU (2) AU2014352888B2 (hr)
BR (1) BR112016010220B1 (hr)
CA (1) CA2930737C (hr)
CL (1) CL2016001231A1 (hr)
CR (2) CR20190394A (hr)
CY (1) CY1124407T1 (hr)
DK (1) DK3071561T3 (hr)
EA (1) EA030068B1 (hr)
ES (1) ES2875899T3 (hr)
HK (1) HK1226075A1 (hr)
HR (1) HRP20210957T1 (hr)
HU (1) HUE055213T2 (hr)
IL (2) IL245383B (hr)
LT (1) LT3071561T (hr)
MX (2) MX2016006623A (hr)
MY (1) MY182095A (hr)
NI (1) NI201600071A (hr)
NZ (1) NZ720478A (hr)
PE (1) PE20160654A1 (hr)
PH (1) PH12016500862B1 (hr)
PL (1) PL3071561T3 (hr)
PT (1) PT3071561T (hr)
RS (1) RS62027B1 (hr)
SI (1) SI3071561T1 (hr)
WO (1) WO2015077503A1 (hr)
ZA (2) ZA201603083B (hr)

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