HRP20211907T1 - Pirazol – oksazolidinon spoj za anti – hepatitis b virus - Google Patents
Pirazol – oksazolidinon spoj za anti – hepatitis b virus Download PDFInfo
- Publication number
- HRP20211907T1 HRP20211907T1 HRP20211907TT HRP20211907T HRP20211907T1 HR P20211907 T1 HRP20211907 T1 HR P20211907T1 HR P20211907T T HRP20211907T T HR P20211907TT HR P20211907 T HRP20211907 T HR P20211907T HR P20211907 T1 HRP20211907 T1 HR P20211907T1
- Authority
- HR
- Croatia
- Prior art keywords
- image
- enantiomer
- pharmaceutically acceptable
- tautomer
- acceptable salt
- Prior art date
Links
- -1 Pyrazole-oxazolidinone compound Chemical class 0.000 title 1
- 241000700605 Viruses Species 0.000 title 1
- 208000006454 hepatitis Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000002541 furyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 2
- 229910052805 deuterium Inorganic materials 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 241000700721 Hepatitis B virus Species 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000002672 hepatitis B Diseases 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/41—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
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P31/20—Antivirals for DNA viruses
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Biotechnology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (11)
1. Spoj s formulom I, ili farmaceutski prihvatljiva sol ili enantiomer ili tautomer iste:
[image]
pri čemu,
svaki od R1, R2 i R3 je nezavisno odabran od vodika, halogena, C1 – C3 alkila, amino i hidroksila;
[image]
je odabran od:
[image]
R6 je odabran od deuterija, halogena, amino i hidroksila;
n je 0, 1 ili 2;
Q je aril ili heteroaril opcionalno supstituiran s jednim ili više halogena, arilna skupina je fenil, i heteroaril je odabran od furila, pirolila, tienila i piridila;
enantiomer je racemat ili R izomer.
2. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol ili enantiomer ili tautomer istoga, pri čemu je kiralni ugljik u R konfiguraciji i struktura je vidljiva u formuli I – R:
[image]
3. Spoj iz patentnog zahtjeva 1 ili 2, ili farmaceutski prihvatljiva sol ili enantiomer ili tautomer istoga, pri čemu
je svaki od Ri, R2 i R3 samostalno vodik ili halogen;
[image]
odabran od
[image]
R6 je deuterij ili halogen;
Q je aril ili heteroaril opcionalno supstituiran s jednim ili više halogena, navedeni aril je fenil, i navedeni heteroaril je odabran od furila, pirolila i tienila.
4. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, ili farmaceutski prihvatljiva sol ili enantiomer ili tautomer istoga, pri čemu je Q p-fluorofenil, ili tienil ili furil;
[image]
odabran od:
[image]
5. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, ili farmaceutski prihvatljiva sol ili enantiomer ili tautomer istoga, pri čemu je sljedeći dio u formuli I i formuli I – R:
[image]
odabran od:
[image]
[image]
6. Spoj prema bilo kojem od patentnih zahtjeva 1 – 5, ili farmaceutski prihvatljiva sol ili enantiomer ili tautomer istoga, pri čemu je sljedeći dio u formuli I i formuli I – R:
[image]
odabran od:
[image]
7. Spoj prema bilo kojem od patentnih zahtjeva 1 – 5, ili farmaceutski prihvatljiva sol ili enantiomer ili tautomer istoga, pri čemu je sljedeći dio u formuli I i formuli I – R:
[image]
je
[image]
8. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, ili farmaceutski prihvatljiva sol ili enantiomer ili tautomer istoga, pri čemu je spoj odabran od:
[image]
[image]
[image]
[image]
9. Farmaceutski sastav koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1 – 8 ili farmaceutski prihvatljivu sol ili enantiomer ili tautomer istog, i farmaceutski prihvatljiv nosač.
10. Spoj prema bilo kojem od patentnih zahtjeva 1 – 8 ili farmaceutski prihvatljiva sol ili enantiomer ili tautomer istog ili farmaceutskog sastava iz patentnog zahtjeva 9 za korištenje u proizvodnji lijeka za inhibiciju hepatitis B virusa.
11. Spoj ili farmaceutski sastav za korištenje prema patentnom zahtjevu 10, pri čemu se lijek koristi u liječenju virusne infekcije hepatitisom B kod sisavaca.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610210422 | 2016-04-06 | ||
| EP17778663.9A EP3441389B1 (en) | 2016-04-06 | 2017-04-06 | Pyrazole-oxazolidinone compound for anti-hepatitis b virus |
| PCT/CN2017/079552 WO2017173999A1 (zh) | 2016-04-06 | 2017-04-06 | 抗乙肝病毒的吡唑-噁唑烷酮类化合物 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20211907T1 true HRP20211907T1 (hr) | 2022-03-18 |
Family
ID=60000897
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20211907TT HRP20211907T1 (hr) | 2016-04-06 | 2017-04-06 | Pirazol – oksazolidinon spoj za anti – hepatitis b virus |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10519145B2 (hr) |
| EP (1) | EP3441389B1 (hr) |
| JP (1) | JP6581745B2 (hr) |
| KR (1) | KR102083818B1 (hr) |
| CN (1) | CN109311865B (hr) |
| CY (1) | CY1124671T1 (hr) |
| DK (1) | DK3441389T3 (hr) |
| ES (1) | ES2893208T3 (hr) |
| HR (1) | HRP20211907T1 (hr) |
| LT (1) | LT3441389T (hr) |
| PL (1) | PL3441389T3 (hr) |
| PT (1) | PT3441389T (hr) |
| RS (1) | RS62597B1 (hr) |
| SI (1) | SI3441389T1 (hr) |
| WO (1) | WO2017173999A1 (hr) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3138384A1 (en) | 2019-04-30 | 2020-11-05 | Aicuris Gmbh & Co. Kg | Novel phenyl and pyridyl ureas active against the hepatitis b virus (hbv) |
| CU20210088A7 (es) | 2019-04-30 | 2022-06-06 | Aicuris Gmbh & Co Kg | Compuestos derivados sustituidos de indol-2-carboxamidas activas contra el virus de la hepatitis b (vhb) |
| EP3962913A1 (en) | 2019-04-30 | 2022-03-09 | AiCuris GmbH & Co. KG | Novel indolizine-2-carboxamides active against the hepatitis b virus (hbv) |
| SG11202111493WA (en) | 2019-04-30 | 2021-11-29 | Aicuris Gmbh & Co Kg | Novel oxalyl piperazines active against the hepatitis b virus (hbv) |
| CN112574188B (zh) * | 2019-09-29 | 2022-05-06 | 苏州爱科百发生物医药技术有限公司 | 一种吡唑类化合物及其应用 |
| CN114685473A (zh) * | 2020-12-25 | 2022-07-01 | 杭州百新生物医药科技有限公司 | 5-烷基-2-吡唑-恶唑烷-4-酮类衍生物及其用途 |
| CN115677681A (zh) * | 2021-07-23 | 2023-02-03 | 上海挚盟医药科技有限公司 | 一种乙肝病毒核衣壳抑制剂的制备方法 |
| CN115677680A (zh) * | 2021-07-23 | 2023-02-03 | 上海挚盟医药科技有限公司 | 式i化合物的晶型及其制备和应用 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006033995A2 (en) * | 2004-09-16 | 2006-03-30 | Valeant Research And Development | Thiazolidin-4-ones having anti-hepatitis b activity |
| WO2007014023A1 (en) * | 2005-07-21 | 2007-02-01 | Valeant Research & Development | Thiazolidinones, oxazolidinones, and pyrrolidinones for hbv |
-
2017
- 2017-04-06 WO PCT/CN2017/079552 patent/WO2017173999A1/zh active Application Filing
- 2017-04-06 HR HRP20211907TT patent/HRP20211907T1/hr unknown
- 2017-04-06 US US16/091,320 patent/US10519145B2/en active Active
- 2017-04-06 LT LTEPPCT/CN2017/079552T patent/LT3441389T/lt unknown
- 2017-04-06 EP EP17778663.9A patent/EP3441389B1/en active Active
- 2017-04-06 CN CN201780035186.6A patent/CN109311865B/zh active Active
- 2017-04-06 ES ES17778663T patent/ES2893208T3/es active Active
- 2017-04-06 KR KR1020187031104A patent/KR102083818B1/ko active IP Right Grant
- 2017-04-06 PT PT177786639T patent/PT3441389T/pt unknown
- 2017-04-06 RS RS20211423A patent/RS62597B1/sr unknown
- 2017-04-06 DK DK17778663.9T patent/DK3441389T3/da active
- 2017-04-06 JP JP2019503613A patent/JP6581745B2/ja active Active
- 2017-04-06 PL PL17778663T patent/PL3441389T3/pl unknown
- 2017-04-06 SI SI201730993T patent/SI3441389T1/sl unknown
-
2021
- 2021-10-19 CY CY20211100903T patent/CY1124671T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US10519145B2 (en) | 2019-12-31 |
| WO2017173999A1 (zh) | 2017-10-12 |
| EP3441389A1 (en) | 2019-02-13 |
| KR20180128953A (ko) | 2018-12-04 |
| SI3441389T1 (sl) | 2022-01-31 |
| PL3441389T3 (pl) | 2022-01-24 |
| ES2893208T3 (es) | 2022-02-08 |
| CN109311865B (zh) | 2021-08-31 |
| US20190152963A1 (en) | 2019-05-23 |
| PT3441389T (pt) | 2021-11-11 |
| JP2019513830A (ja) | 2019-05-30 |
| KR102083818B1 (ko) | 2020-03-03 |
| JP6581745B2 (ja) | 2019-09-25 |
| DK3441389T3 (da) | 2021-11-08 |
| RS62597B1 (sr) | 2021-12-31 |
| CN109311865A (zh) | 2019-02-05 |
| CY1124671T1 (el) | 2022-07-22 |
| EP3441389B1 (en) | 2021-09-08 |
| LT3441389T (lt) | 2021-10-11 |
| EP3441389A4 (en) | 2019-09-04 |
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