HRP20210724T1 - Supstituirani derivati indolina kao inhibitori replikacije denga virusa - Google Patents
Supstituirani derivati indolina kao inhibitori replikacije denga virusa Download PDFInfo
- Publication number
- HRP20210724T1 HRP20210724T1 HRP20210724TT HRP20210724T HRP20210724T1 HR P20210724 T1 HRP20210724 T1 HR P20210724T1 HR P20210724T T HRP20210724T T HR P20210724TT HR P20210724 T HRP20210724 T HR P20210724T HR P20210724 T1 HRP20210724 T1 HR P20210724T1
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- HR
- Croatia
- Prior art keywords
- hydrogen
- chlorine
- carbon
- compound
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- Prior art date
Links
- 206010012310 Dengue fever Diseases 0.000 title claims 4
- 208000025729 dengue disease Diseases 0.000 title claims 4
- 208000001490 Dengue Diseases 0.000 title 1
- 229940123627 Viral replication inhibitor Drugs 0.000 title 1
- 125000003387 indolinyl group Chemical class N1(CCC2=CC=CC=C12)* 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 33
- 239000001257 hydrogen Substances 0.000 claims 33
- 150000002431 hydrogen Chemical group 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 11
- 239000000460 chlorine Substances 0.000 claims 10
- 229910052801 chlorine Inorganic materials 0.000 claims 10
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 9
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 6
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000001309 chloro group Chemical group Cl* 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 1
- 241000700605 Viruses Species 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 229910052805 deuterium Inorganic materials 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- -1 pentafluorosulfanyl Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000005034 trifluormethylthio group Chemical group FC(S*)(F)F 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- 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
- A61K31/40—Heterocyclic 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
- A61K31/403—Heterocyclic 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
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/40—Heterocyclic 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
- A61K31/407—Heterocyclic 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 other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; 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
- C07D209/32—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; 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
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- 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
-
- 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
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- Y—GENERAL 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Claims (11)
1. Spoj s formulom (I), uključujući bilo koji njegov stereokemijski izomerni oblik,
[image]
naznačen time što
A je
[image]
pri čemu
R1 je klor, R2 je vodik, R3 je vodik, A je (a-1), R4 je pentafluorsulfanil, R5 je vodik, Z je ugljik, i R6 je vodik; ili
R1 je klor, R2 je vodik, R3 je vodik, A je (a-1), R4 je trifluormetil, R5 je vodik, Z je ugljik, i R6 je metil; ili
R1 je klor, R2 je vodik, R3 je vodik, A je (a-1), R4 je trifluormetil, R5 je fluor, Z je ugljik, i R6 je vodik; ili
R1 je klor, R2 je vodik, R3 je vodik, A je (a-1), R4 je trifluormetoksi, R5 je vodik, Z je ugljik, i R6 je metil; ili
R1 je klor, R2 je vodik, R3 je vodik, A je (a-1), R4 je trifluormetoksi, R5 je fluor, Z je ugljik, i R6 je vodik; ili
R1 je fluor, R2 je metoksi, R3 je vodik, A je (a-1), R4 je trifluormetoksi, R5 je vodik, Z je ugljik, i R6 je vodik; ili
R1 je klor, R2 je vodik, R3 je deuterij, A je (a-1), R4 je trifluormetoksi, R5 je vodik, Z je ugljik, i R6 je vodik; ili
R1 je klor, R2 je -OCH2CH2OH, R3 je vodik, A je (a-1), R4 je trifluormetoksi, R5 je vodik, Z je ugljik, i R6 je vodik; ili
R1 je klor, R2 je vodik, R3 je vodik, A je (a-1), R4 je trifluormetil, R5 je metoksi, Z je dušik, i R6 je odsutan; ili
R1 je klor, R2 je vodik, R3 je vodik, A je (a-2), i R4 je trifluormetil; ili
R1 je klor, R2 je vodik, R3 je vodik, A je (a-1), R4 je trifluormetiltio, R5 je vodik, Z je ugljik, i R6 je vodik;
ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf.
2. Spoj prema patentnom zahtjevu 1 naznačen time što A je (a-1).
3. Spoj prema patentnom zahtjevu 1 naznačen time što A je (a-2).
4. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3 naznačen time što navedeni spoj ima (+) specifičnu rotaciju.
5. Spoj prema patentnom zahtjevu 1 naznačen time što se navedeni spoj bira od:
[image]
[image]
[image]
[image]
6. Farmaceutski pripravak naznačen time što sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 5 zajedno s jednom ili više farmaceutski prihvatljivih pomoćnih tvari, razrjeđivača ili nosača.
7. Farmaceutski pripravak prema patentnom zahtjevu 6 naznačen time što sadrži drugi ili daljnji aktivni sastojak.
8. Farmaceutski pripravak prema patentnom zahtjevu 7 naznačen time što je drugi ili daljnji aktivni sastojak antivirusno sredstvo.
9. Spoj s formulom (I) prema bilo kojem od patentnih zahtjeva 1 do 5 naznačen time što je za uporabu kao lijek.
10. Spoj s formulom (I) prema bilo kojem od patentnih zahtjeva 1 do 5 se koristi u liječenju virusne infekcije Denga groznicom i za prevenciju ili liječenje bolesti povezane s virusnom infekcijom Denga groznicom.
11. Spoj s formulom (I) za uporabu u skladu s patentnim zahtjevom 10 naznačen time što je virusna infekcija Denga groznicom infekcija virusima soja DENV-1, DENV-2, DENV-3 ili DENV-4.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP17172247 | 2017-05-22 | ||
PCT/EP2018/063029 WO2018215316A1 (en) | 2017-05-22 | 2018-05-18 | Substituted indoline derivatives as dengue viral replication inhibitors |
EP18729051.5A EP3630724B1 (en) | 2017-05-22 | 2018-05-18 | Substituted indoline derivatives as dengue viral replication inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20210724T1 true HRP20210724T1 (hr) | 2021-10-15 |
Family
ID=58745159
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20210724TT HRP20210724T1 (hr) | 2017-05-22 | 2021-05-10 | Supstituirani derivati indolina kao inhibitori replikacije denga virusa |
Country Status (29)
Country | Link |
---|---|
US (2) | US11053196B2 (hr) |
EP (1) | EP3630724B1 (hr) |
JP (1) | JP7179773B2 (hr) |
KR (1) | KR102625991B1 (hr) |
CN (1) | CN110753682B (hr) |
AR (1) | AR111820A1 (hr) |
AU (1) | AU2018274101C1 (hr) |
BR (1) | BR112019024311A2 (hr) |
CA (1) | CA3061026C (hr) |
CL (1) | CL2019003309A1 (hr) |
CO (1) | CO2019013042A2 (hr) |
CR (1) | CR20190531A (hr) |
DK (1) | DK3630724T3 (hr) |
EA (1) | EA039702B1 (hr) |
EC (1) | ECSP19083621A (hr) |
ES (1) | ES2884157T3 (hr) |
HR (1) | HRP20210724T1 (hr) |
HU (1) | HUE054379T2 (hr) |
IL (1) | IL270727B2 (hr) |
LT (1) | LT3630724T (hr) |
MX (1) | MX2019013878A (hr) |
PE (1) | PE20200342A1 (hr) |
PH (1) | PH12019502577A1 (hr) |
SI (1) | SI3630724T1 (hr) |
TW (1) | TWI771420B (hr) |
UA (1) | UA125970C2 (hr) |
UY (1) | UY37741A (hr) |
WO (1) | WO2018215316A1 (hr) |
ZA (1) | ZA201907713B (hr) |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
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GB201116559D0 (en) | 2011-09-26 | 2011-11-09 | Univ Leuven Kath | Novel viral replication inhibitors |
JOP20160086B1 (ar) | 2015-05-08 | 2021-08-17 | 2 Katholieke Univ Leuven Ku Leuven Research And Development | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
JO3633B1 (ar) | 2015-09-16 | 2020-08-27 | Katholieke Univ Leuven Ku Leuven Research & Development | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
JOP20160198B1 (ar) | 2015-09-16 | 2022-03-14 | Janssen Pharmaceuticals Inc | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
WO2017167953A1 (en) | 2016-03-31 | 2017-10-05 | Janssen Pharmaceuticals, Inc. | Substituted indoline derivatives as dengue viral replication inhibitors |
MX2018011784A (es) | 2016-03-31 | 2019-02-13 | Janssen Pharmaceuticals Inc | Derivados de indol sustituidos como inhibidores de la replicacion virica del dengue. |
BR112018068956A2 (pt) | 2016-04-01 | 2019-01-22 | Janssen Pharmaceuticals Inc | derivados do composto indol substituídos como inibidores da replicação viral da dengue |
JOP20170069B1 (ar) | 2016-04-01 | 2021-08-17 | 1 Janssen Pharmaceuticals Inc | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
JOP20180025B1 (ar) | 2017-03-31 | 2021-08-17 | Janssen Pharmaceuticals Inc | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
JOP20180026A1 (ar) | 2017-03-31 | 2019-01-30 | Univ Leuven Kath | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
ES2929667T3 (es) | 2017-05-22 | 2022-11-30 | Janssen Pharmaceuticals Inc | Derivados de indolina sustituidos como inhibidores de la replicación vírica de dengue |
MA52976A (fr) * | 2018-06-19 | 2021-04-28 | Novartis Ag | Dérivés de tétrahydrothiénopyridine n-substitués et leurs utilisations |
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WO2023278564A1 (en) | 2021-07-02 | 2023-01-05 | Mirati Therapeutics, Inc. | Aminopyridine-based mta-cooperative prmt5 inhibitors |
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