DK2297120T3 - Aminodihydrothiazinderivater som bace-inhibitorer til behandling af Alzheimers sygdom - Google Patents
Aminodihydrothiazinderivater som bace-inhibitorer til behandling af Alzheimers sygdom Download PDFInfo
- Publication number
- DK2297120T3 DK2297120T3 DK09739419.1T DK09739419T DK2297120T3 DK 2297120 T3 DK2297120 T3 DK 2297120T3 DK 09739419 T DK09739419 T DK 09739419T DK 2297120 T3 DK2297120 T3 DK 2297120T3
- Authority
- DK
- Denmark
- Prior art keywords
- methyl
- compound
- dihydro
- equiv
- mmoles
- Prior art date
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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
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- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (10)
1. Forbindelse med formel I:
i hvor: n er 0, 1 eller 2; R1 er pyrimidinyl, pyrazinyl, eventuelt substitueret med chlor eller fluor, eller pyridinyl, eventuelt substitueret med en eller to substituenter, som hver især uafhængigt er udvalgt fra chlor, fluor og CrC3 alkoxy; R2 i hvert tilfælde uafhængigt er udvalgt fra chlor eller fluor; R3 er hydrogen eller CrC4 alkyl, eventuelt substitueret med hydroxy; og R4 er hydrogen eller CrC3 alkyl; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse ifølge krav 1, hvor R1 er pyrimidinyl, pyridinyl, eventuelt substitueret en eller to gange i hvert tilfælde uafhængigt udvalgt fra chlor, fluor eller methoxy eller pyrazinyl, eventuelt substitueret med fluor; R2 er chlor eller fluor; R3 er hydrogen, methyl, methyl, som er substitueret med hydroxy, eller /so-propyl, som er substitueret med hydroxy; R4 er hydrogen; og n er 0, 1 eller 2; eller et farmaceutisk acceptabelt salt deraf.
3. Forbindelse ifølge et af kravene 1 til 2, hvor R1 er pyrimidinyl, pyridinyl, eventuelt substitueret med fluor, eller pyrazinyl, eventuelt substitueret med fluor; R2 er fluor; R3 er hydrogen eller methyl; R4 er hydrogen; og n er 1 eller 2; eller et farmaceutisk acceptabelt salt deraf.
4. Forbindelse ifølge et af kravene 1 til 3, hvor R1 er pyrimidinyl, R2 er fluor, R3 er hydrogen, R4 er hydrogen, og n er 2, eller et farmaceutisk acceptabelt salt deraf.
5. Forbindelse ifølge et af kravene 1 til 4, hvor konfigurationen af det chirale center tilstødende til nitrogenet af aminothiazinet er (S), eller et farmaceutisk acceptabelt salt deraf.
6. Forbindelse ifølge krav 1, hvor forbindelsen er 4-(2,4-difluor-5-(pyrimidin-5-yl)phenyl)-4-methyl-5,6-dihydro-4/-/-1,3-thiazin-2-amin:
eller et farmaceutisk acceptabelt salt deraf.
7. Forbindelse ifølge krav 6, hvor forbindelsen er (S)-4-(2,4-difluor-5-(pyrimidin-5-yl)phenyl)-4-methyl-5,6-dihydro-4/-/-1,3-thiazin-2-amin:
eller et farmaceutisk acceptabelt salt deraf.
8. Farmaceutisk formulering omfattende en forbindelse ifølge et af kravene 1 til 7 eller et farmaceutisk acceptabelt salt deraf i kombination med en farmaceutisk acceptabel bærer, et fortyndingsmiddel eller excipiens.
9. Forbindelse ifølge et af kravene 1 til 7 til anvendelse inden for terapi.
10. Forbindelse ifølge et af kravene 1 til 7 til anvendelse ved behandling af Alzheimers sygdom.
Applications Claiming Priority (2)
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 |
Publications (1)
Publication Number | Publication Date |
---|---|
DK2297120T3 true DK2297120T3 (da) | 2015-10-12 |
Family
ID=40839645
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK09739419.1T DK2297120T3 (da) | 2008-05-02 | 2009-04-15 | Aminodihydrothiazinderivater som bace-inhibitorer til behandling af Alzheimers sygdom |
Country Status (32)
Country | Link |
---|---|
US (1) | US7648983B2 (da) |
EP (1) | EP2297120B1 (da) |
JP (3) | JP5658139B2 (da) |
KR (1) | KR101253835B1 (da) |
CN (1) | CN102015667B (da) |
AR (1) | AR071187A1 (da) |
AU (1) | AU2009241515B2 (da) |
CA (1) | CA2723207C (da) |
CL (1) | CL2009000860A1 (da) |
CO (1) | CO6311079A2 (da) |
CR (1) | CR11776A (da) |
DK (1) | DK2297120T3 (da) |
DO (1) | DOP2010000328A (da) |
EA (1) | EA016955B1 (da) |
EC (1) | ECSP10010582A (da) |
ES (1) | ES2549087T3 (da) |
HR (1) | HRP20150941T1 (da) |
HU (1) | HUE025520T2 (da) |
IL (1) | IL208350A (da) |
MA (1) | MA32351B1 (da) |
MX (1) | MX2010011972A (da) |
NZ (1) | NZ588300A (da) |
PE (1) | PE20091816A1 (da) |
PL (1) | PL2297120T3 (da) |
PT (1) | PT2297120E (da) |
RS (1) | RS54260B1 (da) |
SI (1) | SI2297120T1 (da) |
SV (1) | SV2010003718A (da) |
TW (1) | TWI431004B (da) |
UA (1) | UA102251C2 (da) |
WO (1) | WO2009134617A1 (da) |
ZA (1) | ZA201006868B (da) |
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WO1996014842A1 (en) | 1994-11-15 | 1996-05-23 | Merck & Co., Inc. | Substituted heterocycles as inhibitors of nitric oxide synthase |
JPH08333258A (ja) | 1994-12-14 | 1996-12-17 | Japan Tobacco Inc | チアジン又はチアゼピン誘導体及びそれら化合物を含有してなる一酸化窒素合成酵素阻害剤 |
GB0324498D0 (en) * | 2003-07-21 | 2003-11-26 | Aventis Pharma Inc | Heterocyclic compounds as P2X7 ion channel blockers |
US7592348B2 (en) * | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
WO2006041404A1 (en) * | 2004-10-15 | 2006-04-20 | Astrazeneca Ab | Substituted amino-compounds and uses thereof |
WO2006041405A1 (en) * | 2004-10-15 | 2006-04-20 | Astrazeneca Ab | Substituted amino-pyrimidones and uses thereof |
EP2612854B1 (en) * | 2005-10-25 | 2015-04-29 | Shionogi&Co., Ltd. | Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors |
JP2009532464A (ja) * | 2006-04-05 | 2009-09-10 | アストラゼネカ・アクチエボラーグ | 2−アミノピリミジン−4−オン及びAβ−関連の病理を治療又は予防するためのその使用 |
CN101687827B (zh) | 2007-04-24 | 2014-04-23 | 盐野义制药株式会社 | 环状基团取代的氨基二氢噻嗪衍生物 |
JP5383483B2 (ja) * | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | アルツハイマー症治療用医薬組成物 |
TWI431004B (zh) * | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
KR101324426B1 (ko) * | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
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