HRP20150941T1 - Derivati aminodihidrotiazina kao inhibitori bace u lijeäśenju alzheimerove bolesti - Google Patents
Derivati aminodihidrotiazina kao inhibitori bace u lijeäśenju alzheimerove bolesti Download PDFInfo
- Publication number
- HRP20150941T1 HRP20150941T1 HRP20150941TT HRP20150941T HRP20150941T1 HR P20150941 T1 HRP20150941 T1 HR P20150941T1 HR P20150941T T HRP20150941T T HR P20150941TT HR P20150941 T HRP20150941 T HR P20150941T HR P20150941 T1 HRP20150941 T1 HR P20150941T1
- Authority
- HR
- Croatia
- Prior art keywords
- fluorine
- pharmaceutically acceptable
- compound according
- hydrogen
- acceptable salt
- Prior art date
Links
- 208000024827 Alzheimer disease Diseases 0.000 title claims 2
- VNTNANCAPVJRJP-UHFFFAOYSA-N 3,4-dihydrothiazin-2-amine Chemical class NN1CCC=CS1 VNTNANCAPVJRJP-UHFFFAOYSA-N 0.000 title 1
- 101150058765 BACE1 gene Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 12
- 229910052731 fluorine Chemical group 0.000 claims 10
- 239000011737 fluorine Chemical group 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 239000000460 chlorine Substances 0.000 claims 5
- 229910052801 chlorine Inorganic materials 0.000 claims 5
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 2
- MJQMRGWYPNIERM-HNNXBMFYSA-N (4s)-4-(2,4-difluoro-5-pyrimidin-5-ylphenyl)-4-methyl-5,6-dihydro-1,3-thiazin-2-amine Chemical compound C=1C(C=2C=NC=NC=2)=C(F)C=C(F)C=1[C@]1(C)CCSC(N)=N1 MJQMRGWYPNIERM-HNNXBMFYSA-N 0.000 claims 1
- MJQMRGWYPNIERM-UHFFFAOYSA-N 4-(2,4-difluoro-5-pyrimidin-5-ylphenyl)-4-methyl-5,6-dihydro-1,3-thiazin-2-amine Chemical compound C=1C(C=2C=NC=NC=2)=C(F)C=C(F)C=1C1(C)CCSC(N)=N1 MJQMRGWYPNIERM-UHFFFAOYSA-N 0.000 claims 1
- -1 aminothiazine nitrogen Chemical compound 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
- C07D279/06—1,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
Claims (10)
1. Spoj Formule I:
[image]
,
naznačen time što:
n je 0, 1 ili 2;
R1 je pirimidinil, pirazinil izborno supstituiran s klorom ili fluorom, ili piridinil izborno supstituiran s jednim ili dva supstituenta, od kojih se svakog neovisno bira između klora, fluora i C1-C3 alkoksi;
R2 se u svakom slučaju neovisno bira između klora ili fluora;
R3 je vodik ili C1-C4 alkil izborno supstituiran s hidroksi; i
R4 je vodik ili C1-C3 alkil;
ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je R1 pirimidinil, piridinil izborno supstituiran s jednim ili dva supstituenta, od kojih se svaki neovisno bira između klora, fluora ili metoksi, ili pirazinil izborno supstituiran s fluorom; R2 je klor ili fluor; R3 je vodik, metil, metil supstituiran s hidroksi, ili iso-propil supstituiran s hidroksi; R4 je vodik; a n je 0, 1 ili 2; ili njegova farmaceutski prihvatljiva sol.
3. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 2, naznačen time što je R1 pirimidinil, piridinil izborno supstituiran s fluorom, ili pirazinil izborno supstituiran s fluorom; R2 je fluor; R3 je vodik ili metil; R4 je vodik; a n je 1 ili 2; ili njegova farmaceutski prihvatljiva sol.
4. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što je R1 pirimidinil, R2 je fluor, R3 je vodik, R4 je vodik, a n je 2, ili njegova farmaceutski prihvatljiva sol.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što je konfiguracija kiralnog centra u susjedstvu aminotiazinskog dušika (S), ili njegova farmaceutski prihvatljiva sol.
6. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj 4-(2,4-difluor-5-(pirimidin-5-il)fenil)-4-metil-5,6-dihidro-4H-1,3-tiazin-2-amin:
[image]
;
ili njegova farmaceutski prihvatljiva sol.
7. Spoj u skladu s patentnim zahtjevom 6, naznačen time što je spoj (S)-4-(2,4-difluor-5-(pirimidin-5-il)fenil)-4-metil-5,6-dihidro-4H-1,3-tiazin-2-amin:
[image]
;
ili njegova farmaceutski prihvatljiva sol.
8. Farmaceutska formulacija, naznačena time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 7, ili njegovu farmaceutski prihvatljivu sol, u kombinaciji s farmaceutski prihvatljivom podlogom, razrjeđivačem ili pomoćnom tvari.
9. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time što je namijenjen upotrebi u terapiji.
10. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time što je namijenjen upotrebi u liječenju Alzheimerove bolesti.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4988108P | 2008-05-02 | 2008-05-02 | |
| PCT/US2009/040589 WO2009134617A1 (en) | 2008-05-02 | 2009-04-15 | Aminodihydrothiazine derivatives as bace inhibitors for the treatment of alzheimer's disease |
| EP09739419.1A EP2297120B1 (en) | 2008-05-02 | 2009-04-15 | Aminodihydrothiazine derivatives as bace inhibitors for the treatment of alzheimer's disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20150941T1 true HRP20150941T1 (hr) | 2015-10-09 |
Family
ID=40839645
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20150941TT HRP20150941T1 (hr) | 2008-05-02 | 2015-09-07 | Derivati aminodihidrotiazina kao inhibitori bace u lijeäśenju alzheimerove bolesti |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US7648983B2 (hr) |
| EP (1) | EP2297120B1 (hr) |
| JP (3) | JP5658139B2 (hr) |
| KR (1) | KR101253835B1 (hr) |
| CN (1) | CN102015667B (hr) |
| AR (1) | AR071187A1 (hr) |
| AU (1) | AU2009241515B2 (hr) |
| CA (1) | CA2723207C (hr) |
| CL (1) | CL2009000860A1 (hr) |
| CO (1) | CO6311079A2 (hr) |
| CR (1) | CR11776A (hr) |
| DK (1) | DK2297120T3 (hr) |
| DO (1) | DOP2010000328A (hr) |
| EA (1) | EA016955B1 (hr) |
| EC (1) | ECSP10010582A (hr) |
| ES (1) | ES2549087T3 (hr) |
| HR (1) | HRP20150941T1 (hr) |
| HU (1) | HUE025520T2 (hr) |
| IL (1) | IL208350A (hr) |
| MA (1) | MA32351B1 (hr) |
| MX (1) | MX2010011972A (hr) |
| NZ (1) | NZ588300A (hr) |
| PE (1) | PE20091816A1 (hr) |
| PL (1) | PL2297120T3 (hr) |
| PT (1) | PT2297120E (hr) |
| RS (1) | RS54260B1 (hr) |
| SI (1) | SI2297120T1 (hr) |
| SV (1) | SV2010003718A (hr) |
| TW (1) | TWI431004B (hr) |
| UA (1) | UA102251C2 (hr) |
| WO (1) | WO2009134617A1 (hr) |
| ZA (1) | ZA201006868B (hr) |
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