HRP20210847T1 - Supstituirani derivati indola kao inhibitori replikacije denga virusa - Google Patents

Supstituirani derivati indola kao inhibitori replikacije denga virusa Download PDF

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Publication number
HRP20210847T1
HRP20210847T1 HRP20210847TT HRP20210847T HRP20210847T1 HR P20210847 T1 HRP20210847 T1 HR P20210847T1 HR P20210847T T HRP20210847T T HR P20210847TT HR P20210847 T HRP20210847 T HR P20210847T HR P20210847 T1 HRP20210847 T1 HR P20210847T1
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HR
Croatia
Prior art keywords
compound
image
pharmaceutically acceptable
solvate
polymorph
Prior art date
Application number
HRP20210847TT
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English (en)
Inventor
Dorothée Alice Marie-Eve Bardiot
Jean-François BONFANTI
Bart Rudolf Romanie Kesteleyn
Arnaud Didier M Marchand
Pierre Jean-Marie Bernard Raboisson
Original Assignee
Janssen Pharmaceuticals, Inc.
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.)
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Application filed by Janssen Pharmaceuticals, Inc., Katholieke Universiteit Leuven filed Critical Janssen Pharmaceuticals, Inc.
Publication of HRP20210847T1 publication Critical patent/HRP20210847T1/hr

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    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32Oxygen atoms
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Claims (15)

1. Spoj s formulom (Ia) ili (Ib) [image] stereoizomerni oblik, ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf; navedeni spoj je odabran iz skupine pri čemu: R1 je CF3 ili OCF3, R2 je H ili OCH3 ili F, R3 je H; i kada R2 je H tada R3 može također biti CH3.
2. Spoj ili njegov stereoizomerni oblik, ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf prema patentnom zahtjevu 1 naznačen time što navedeni spoj je odabran iz skupine koju čine: [image] [image] [image] [image] [image] [image] [image] [image]
3. Farmaceutski pripravak naznačen time što sadrži spoj s formulom (Ia) ili (Ib) ili stereoizomerni oblik, ili njihova farmaceutski prihvatljiva sol, solvat ili polimorf prema patentnom zahtjevu 1 ili 2 zajedno s jednom ili više farmaceutski prihvatljivih pomoćnih tvari, razrjeđivača ili nosača.
4. Spoj s formulom (Ia) ili (Ib) ili stereoizomerni oblik, ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf prema patentnom zahtjevu 1 ili farmaceutski pripravak prema patentnom zahtjevu 3 naznačen time što se koristi kao lijek.
5. Spoj s formulom (Ia) ili (Ib) ili stereoizomerni oblik, ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf prema patentnom zahtjevu 1 ili farmaceutski pripravak prema patentnom zahtjevu 3 naznačen time što se koristi u liječenju denga groznice.
6. Spoj s formulom (Ia) ili (Ib) ili stereoizomerni oblik, ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf prema patentnom zahtjevu 1 naznačen time što je za uporabu u inhibiciji replikacije denga virusa u biološkom uzorku ili pacijentu.
7. Spoj za uporabu prema patentnom zahtjevu 6 naznačen time što se nadalje obuhvaća istodobnu primjenu dodatnog terapijskog sredstva.
8. Spoj za uporabu prema patentnom zahtjevu 7 naznačen time što je navedeno dodatno terapijsko sredstvo odabrano od antivirusnog sredstva ili cjepiva protiv denga groznice, ili oboje.
9. Spoj prema patentnom zahtjevu 1 naznačen time što se spoj bira između [image] [image] [image] [image] [image] [image] [image] [image] ili njihove farmaceutski prihvatljive soli, solvata ili polimorfa.
10. Farmaceutski pripravak naznačen time što sadrži spoj prema patentnom zahtjevu 9, ili njegovu farmaceutski prihvatljivu sol, solvat ili polimorf zajedno s jednom ili više farmaceutski prihvatljivih pomoćnih tvari, razrjeđivača ili nosača.
11. Spoj prema patentnom zahtjevu 9, ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf ili farmaceutski pripravak prema patentnom zahtjevu 10 naznačen time što se koristi kao lijek.
12. Spoj prema patentnom zahtjevu 9, ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf ili farmaceutski pripravak prema patentnom zahtjevu 10 naznačen time što je za uporabu u liječenju denga groznice.
13. Spoj kao što je predstavljen bilo kojom strukturnom formulom iz patentnog zahtjeva 9, ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf naznačen time što je za uporabu u inhibiciji replikacije denga virusa u biološkom uzorku ili pacijentu.
14. Spoj za uporabu prema patentnom zahtjevu 13 naznačen time što se nadalje obuhvaća istodobnu primjenu dodatnog terapijskog sredstva.
15. Spoj za uporabu prema patentnom zahtjevu 14 naznačen time što je navedeno dodatno terapijsko sredstvo odabrano od antivirusnog sredstva ili cjepiva protiv denga groznice, ili oboje.
HRP20210847TT 2016-03-31 2021-05-27 Supstituirani derivati indola kao inhibitori replikacije denga virusa HRP20210847T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16163312 2016-03-31
PCT/EP2017/057660 WO2017167950A1 (en) 2016-03-31 2017-03-31 Substituted indole derivatives as dengue viral replication inhibitors
EP17714750.1A EP3436435B1 (en) 2016-03-31 2017-03-31 Substituted indole derivatives as dengue viral replication inhibitors

Publications (1)

Publication Number Publication Date
HRP20210847T1 true HRP20210847T1 (hr) 2021-07-23

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HRP20210847TT HRP20210847T1 (hr) 2016-03-31 2021-05-27 Supstituirani derivati indola kao inhibitori replikacije denga virusa

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US (1) US10646469B2 (hr)
EP (1) EP3436435B1 (hr)
JP (1) JP6888021B2 (hr)
KR (1) KR102359743B1 (hr)
CN (1) CN108884033B (hr)
AU (1) AU2017242893A1 (hr)
BR (1) BR112018068676A2 (hr)
CA (1) CA3013405A1 (hr)
CL (1) CL2018002729A1 (hr)
CO (1) CO2018009559A2 (hr)
CR (1) CR20180495A (hr)
DK (1) DK3436435T3 (hr)
EA (1) EA201892214A1 (hr)
EC (1) ECSP18073245A (hr)
ES (1) ES2882488T3 (hr)
HK (1) HK1258142A1 (hr)
HR (1) HRP20210847T1 (hr)
HU (1) HUE054936T2 (hr)
IL (1) IL261944A (hr)
LT (1) LT3436435T (hr)
MX (1) MX2018011784A (hr)
PH (1) PH12018502015A1 (hr)
SG (1) SG11201808138YA (hr)
SI (1) SI3436435T1 (hr)
WO (1) WO2017167950A1 (hr)
ZA (1) ZA201806473B (hr)

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Publication number Publication date
EP3436435A1 (en) 2019-02-06
US20190274999A1 (en) 2019-09-12
CO2018009559A2 (es) 2018-09-20
SI3436435T1 (sl) 2021-08-31
ECSP18073245A (es) 2018-10-31
DK3436435T3 (da) 2021-08-09
KR102359743B1 (ko) 2022-02-07
EA201892214A1 (ru) 2019-03-29
JP6888021B2 (ja) 2021-06-16
CA3013405A1 (en) 2017-10-05
PH12018502015A1 (en) 2019-07-15
HK1258142A1 (zh) 2019-11-08
LT3436435T (lt) 2021-08-25
IL261944A (en) 2018-10-31
ES2882488T3 (es) 2021-12-02
HUE054936T2 (hu) 2021-10-28
MX2018011784A (es) 2019-02-13
WO2017167950A1 (en) 2017-10-05
CN108884033B (zh) 2021-03-09
CL2018002729A1 (es) 2018-11-23
SG11201808138YA (en) 2018-10-30
CN108884033A (zh) 2018-11-23
US10646469B2 (en) 2020-05-12
KR20180130498A (ko) 2018-12-07
AU2017242893A1 (en) 2018-08-09
BR112018068676A2 (pt) 2019-01-15
JP2019510024A (ja) 2019-04-11
EP3436435B1 (en) 2021-05-12
CR20180495A (es) 2018-12-06
ZA201806473B (en) 2020-05-27

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