DK3041827T3 - 1,2,4-oxadiazolderivater som immunmodulatorer - Google Patents
1,2,4-oxadiazolderivater som immunmodulatorer Download PDFInfo
- Publication number
- DK3041827T3 DK3041827T3 DK14790320.7T DK14790320T DK3041827T3 DK 3041827 T3 DK3041827 T3 DK 3041827T3 DK 14790320 T DK14790320 T DK 14790320T DK 3041827 T3 DK3041827 T3 DK 3041827T3
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- Denmark
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- following structure
- amino acid
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- C—CHEMISTRY; METALLURGY
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- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- 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
- A61K31/4245—Oxadiazoles
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- 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
- A61K31/433—Thidiazoles
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- A61P37/02—Immunomodulators
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
- C07D273/08—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and more than one oxygen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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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
Claims (48)
1. Forbindelse med formel (I)
hvor, Q er S eller O; Ri repræsenterer en sidekæde af en aminosyrerest udvalgt fra Ser og Thr, eventuelt substitueret med alkyl eller acyl; R2 er hydrogen eller -CO-Aaa; Aaa er en aminosyrerest udvalgt fra Thr og Ser; hvor en C-terminus deraf er en fri terminus, er amideret eller er esterificeret; R3 repræsenterer en sidekæde af en aminosyrerest udvalgt fra Asn, Asp, Gin og Glu; -----er en eventuel binding; R4 og R5 uafhængigt er hydrogen eller fraværende; R6 er hydrogen, alkyl eller acyl; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse ifølge krav 1, hvor Q er O.
3. Forbindelse ifølge krav 1, hvor Re er H.
4. Forbindelse ifølge krav 1, hvor Re er -C(0)CH3, -C(0)CH2CH3, -C(0)(CH2)2CH3, -C(0)(CH2)3CH3, -C(0)(CH2)4CH3 eller -C(0)(CH2)5CH3.
5. Forbindelse ifølge krav 1, hvor R2 er -CO-Aaa.
6. Forbindelse ifølge krav 1, hvor forbindelsen med formlen (I) er en forbindelse med formlen (IA):
eller et farmaceutisk acceptabelt salt deraf; hvor, Ri repræsenterer en sidekæde af en aminosyrerest udvalgt fra Ser og Thr, eventuelt substitueret med alkyl eller acyl; R3 repræsenterer en sidekæde af en aminosyrerest udvalgt fra Asn, Asp, Gin og Glu; og Aaa er en aminosyrerest udvalgt fra Thr og Ser; hvor C-terminus deraf er en fri terminus, er amideret eller er esterificeret.
7. Forbindelse ifølge krav 1, hvor Aaa er en aminosyrerest udvalgt fra Thr og Ser; hvor C-terminus er en fri terminus.
8. Forbindelse ifølge krav 1, hvor forbindelsen med formlen (I) er en forbindelse med formlen (IB):
eller et farmaceutisk acceptabelt salt deraf; hvor, Ri repræsenterer en sidekæde af en aminosyrerest udvalgt fra Ser og Thr, eventuelt substitueret med alkyl eller acyl; og R3 repræsenterer en sidekæde af en aminosyrerest udvalgt fra Asn, Asp, Gin og Glu.
9. Forbindelse ifølge krav 1, hvor: Ri repræsenterer en sidekæde af en aminosyrerest udvalgt fra Ser og Thr.
10. Forbindelse ifølge krav 1, hvor Ri er substitueret med Ci-5-alkyl.
11. Forbindelse ifølge krav 1, hvor R3 repræsenterer en sidekæde af en aminosyrerest udvalgt fra Asn og Glu.
12. Forbindelse ifølge krav 1, hvor: Ri repræsenterer en sidekæde af en aminosyrerest udvalgt fra Ser og Thr; R2 er -CO-Aaa; Aaa er en aminosyrerest udvalgt fra Thr og Ser; hvor C-terminus er en fri terminus; R3 repræsenterer en sidekæde af en aminosyrerest udvalgt fra Asn og Glu.
13. Forbindelse ifølge krav 1, hvor Ri repræsenterer en sidekæde af en aminosyrerest Ser.
14. Forbindelse ifølge krav 1, hvor Ri repræsenterer en sidekæde af en aminosyrerest Thr.
15. Forbindelse ifølge krav 1, hvor Aaa er Ser.
16. Forbindelse ifølge krav 1, hvor Aaa er Thr.
17. Forbindelse ifølge krav 1, hvor R3 repræsenterer en sidekæde af en aminosyrerest Asn.
18. Forbindelse ifølge krav 1, hvor R3 repræsenterer en sidekæde af en aminosyrerest Asp.
19. Forbindelse ifølge krav 1, hvor R3 repræsenterer en sidekæde af en aminosyrerest Gin.
20. Forbindelse ifølge krav 1, hvor R3 repræsenterer en sidekæde af en aminosyrerest Glu.
21. Forbindelse ifølge krav 1, hvor R2 er H.
22. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
23. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
24. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
25. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
26. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
27. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
28. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
29. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
30. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
31. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
32. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
33. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
34. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
35. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
36. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
37. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
38. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
39. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
40. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
41. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
42. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
43. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
44. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
45. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
46. Forbindelse ifølge krav 1, der har følgende struktur:
eller et farmaceutisk acceptabelt salt deraf.
47. Farmaceutisk sammensætning, der omfatter en farmaceutisk acceptabel bærer eller excipiens og mindst én forbindelse ifølge et hvilket som helst af kravene 1-46 eller et farmaceutisk acceptabelt salt deraf.
48. Farmaceutisk sammensætning ifølge krav 47, der endvidere omfatter mindst ét middel af et anticancermiddel, et kemoterapimiddel og en antiproliferativ forbindelse.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN4011CH2013 | 2013-09-06 | ||
PCT/IB2014/064279 WO2015033299A1 (en) | 2013-09-06 | 2014-09-05 | 1,2,4-oxadiazole derivatives as immunomodulators |
Publications (1)
Publication Number | Publication Date |
---|---|
DK3041827T3 true DK3041827T3 (da) | 2018-07-16 |
Family
ID=51830558
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK14790320.7T DK3041827T3 (da) | 2013-09-06 | 2014-09-05 | 1,2,4-oxadiazolderivater som immunmodulatorer |
DK18162983.3T DK3363790T3 (da) | 2013-09-06 | 2014-09-05 | 1,2,4-oxadiazolderivater som immunmodulatorer |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
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DK18162983.3T DK3363790T3 (da) | 2013-09-06 | 2014-09-05 | 1,2,4-oxadiazolderivater som immunmodulatorer |
Country Status (28)
Country | Link |
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US (8) | US9233940B2 (da) |
EP (2) | EP3041827B1 (da) |
JP (1) | JP6521977B2 (da) |
KR (1) | KR102362277B1 (da) |
CN (2) | CN108164474B (da) |
AU (4) | AU2014316682B2 (da) |
BR (1) | BR112016004889B1 (da) |
CA (1) | CA2922607C (da) |
CU (1) | CU24362B1 (da) |
CY (2) | CY1120899T1 (da) |
DK (2) | DK3041827T3 (da) |
EA (1) | EA030155B1 (da) |
ES (2) | ES2788848T3 (da) |
HR (2) | HRP20181052T1 (da) |
HU (2) | HUE048874T2 (da) |
IL (3) | IL244314A (da) |
LT (2) | LT3363790T (da) |
MX (1) | MX365218B (da) |
MY (1) | MY186438A (da) |
PH (1) | PH12016500406A1 (da) |
PL (2) | PL3363790T3 (da) |
PT (2) | PT3363790T (da) |
RS (2) | RS60317B1 (da) |
SG (1) | SG11201601682RA (da) |
SI (2) | SI3041827T1 (da) |
TR (1) | TR201809838T4 (da) |
WO (1) | WO2015033299A1 (da) |
ZA (1) | ZA201602193B (da) |
Families Citing this family (183)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PT2928474T (pt) | 2012-12-07 | 2019-01-30 | Chemocentryx Inc | Diazol lactamas |
US11265444B2 (en) | 2013-08-23 | 2022-03-01 | Preemadonna Inc. | Apparatus for applying coating to nails |
US9687059B2 (en) | 2013-08-23 | 2017-06-27 | Preemadonna Inc. | Nail decorating apparatus |
AU2014316682B2 (en) | 2013-09-06 | 2018-11-22 | Aurigene Discovery Technologies Limited | 1,2,4-oxadiazole derivatives as immunomodulators |
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