HRP20160674T1 - Tetrahidropirolotiazinski spojevi - Google Patents
Tetrahidropirolotiazinski spojevi Download PDFInfo
- Publication number
- HRP20160674T1 HRP20160674T1 HRP20160674TT HRP20160674T HRP20160674T1 HR P20160674 T1 HRP20160674 T1 HR P20160674T1 HR P20160674T T HRP20160674T T HR P20160674TT HR P20160674 T HRP20160674 T HR P20160674T HR P20160674 T1 HRP20160674 T1 HR P20160674T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- image
- salt
- pharmaceutically acceptable
- salt according
- Prior art date
Links
- NDYYBQHNPPJCSU-UHFFFAOYSA-N 2,3,4,4a-tetrahydropyrrolo[2,3-e]thiazine Chemical class S1NCCC2N=CC=C21 NDYYBQHNPPJCSU-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 12
- JTNSTOMSFFQQFP-SDBXPKJASA-N (4ar,7ar)-6-(5-fluoropyrimidin-2-yl)-7a-(1,2-thiazol-5-yl)-4,4a,5,7-tetrahydropyrrolo[3,4-d][1,3]thiazin-2-amine Chemical compound C([C@@]1(N=C(SC[C@@H]1C1)N)C=2SN=CC=2)N1C1=NC=C(F)C=N1 JTNSTOMSFFQQFP-SDBXPKJASA-N 0.000 claims 2
- RETXRSPROBYJQT-VFZGTOFNSA-N 5-[(4ar,7ar)-2-amino-6-(5-fluoropyrimidin-2-yl)-4,4a,5,7-tetrahydropyrrolo[3,4-d][1,3]thiazin-7a-yl]thiophene-2-carbonitrile Chemical compound C([C@@]1(N=C(SC[C@@H]1C1)N)C=2SC(=CC=2)C#N)N1C1=NC=C(F)C=N1 RETXRSPROBYJQT-VFZGTOFNSA-N 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 239000002585 base Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Claims (15)
1. Spoj formule:
[image]
,
naznačen time što se A bira iz skupine koju čine:
[image]
R1 je H ili F;
R2 je H, -CH2OH, C1-C3 alkil,
[image]
R3 je H, F ili CN;
R4 je H, F ili CN; i
R5 je H, -CH3 ili -OCH3;
ili njegova farmaceutski prihvatljiva sol.
2. Spoj ili sol u skladu s patentnim zahtjevom 1, naznačen time što se A bira iz skupine koju čine:
[image]
3. Spoj ili sol u skladu s bilo patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što se A bira iz skupine koju čine:
[image]
4. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što je A:
[image]
.
5. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što je R1 F.
6. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što je R2 H.
7. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 6, naznačen time što je R2
[image]
.
8. Spoj ili sol u skladu s patentnim zahtjevom 1, naznačen time što je (4aR,7aR)-6-(5-fluorpirimidin-2-il)-7a-izotiazol-5-il-4,4a,5,7-tetrahidropirolo[3,4-d][1,3]tiazin-2-amin:
[image]
.
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (4aR,7aR)-6-(5-fluorpirimidin-2-il)-7a-izotiazol-5-il-4,4a,5,7-tetrahidropirolo[3,4-d][1,3]tiazin-2-amin:
[image]
.
10. Spoj ili sol u skladu s patentnim zahtjevom 1, naznačen time što je 5-[(4aR,7aR)-2-amino-6-(5-fluorpirimidin-2-il)-4a,5,6,7-tetrahidropirolo[3,4-d][1,3]tiazin-7a(4H)-il]tiofen-2-karbonitril:
[image]
.
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je 5-[(4aR,7aR)-2-amino-6-(5-fluorpirimidin-2-il)-4a,5,6,7-tetrahidropirolo[3,4-d][1,3]tiazin-7a(4H)-il]tiofen-2-karbonitril HCl:
[image]
.
12. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s bilo kojim od patentnih zahtjeva 1-11, naznačen time što je namijenjen upotrebi u terapiji.
13. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s bilo kojim od patentnih zahtjeva 1-11, naznačen time što je namijenjen upotrebi u liječenju Alzheimerove bolesti.
14. Farmaceutski pripravak, naznačen time što sadrži spoj, ili njegovu farmaceutski prihvatljivu sol, u skladu s bilo kojim od patentnih zahtjeva 1-11, u kombinaciji s jednim ili više farmaceutski prihvatljivih podloga, razrjeđivača ili pomoćnih tvari.
15. Farmaceutski pripravak u skladu s patentnim zahtjevom 16, naznačen time što dodatno sadrži jedno ili više drugih terapijskih sredstava.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261619460P | 2012-04-03 | 2012-04-03 | |
| US201261700960P | 2012-09-14 | 2012-09-14 | |
| US201361758798P | 2013-01-31 | 2013-01-31 | |
| PCT/US2013/033959 WO2013151832A1 (en) | 2012-04-03 | 2013-03-27 | Tetrahydropyrrolothiazine compounds |
| EP13715556.0A EP2836495B1 (en) | 2012-04-03 | 2013-03-27 | Tetrahydropyrrolothiazine compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20160674T1 true HRP20160674T1 (hr) | 2016-07-15 |
Family
ID=48083661
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20160674TT HRP20160674T1 (hr) | 2012-04-03 | 2016-06-14 | Tetrahidropirolotiazinski spojevi |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US8629270B2 (hr) |
| EP (1) | EP2836495B1 (hr) |
| JP (1) | JP6067099B2 (hr) |
| CN (1) | CN104185635B (hr) |
| AR (1) | AR090474A1 (hr) |
| CA (1) | CA2866201C (hr) |
| CY (1) | CY1117688T1 (hr) |
| DK (1) | DK2836495T3 (hr) |
| ES (1) | ES2584827T3 (hr) |
| HR (1) | HRP20160674T1 (hr) |
| HU (1) | HUE030097T2 (hr) |
| JO (1) | JO3143B1 (hr) |
| ME (1) | ME02404B (hr) |
| PL (1) | PL2836495T3 (hr) |
| PT (1) | PT2836495T (hr) |
| RS (1) | RS54899B1 (hr) |
| SI (1) | SI2836495T1 (hr) |
| TW (1) | TWI572610B (hr) |
| WO (1) | WO2013151832A1 (hr) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8158620B2 (en) | 2008-01-18 | 2012-04-17 | Eisai R&D Management Co., Ltd. | Fused aminodihydrothiazine derivatives |
| WO2014066132A1 (en) * | 2012-10-26 | 2014-05-01 | Eli Lilly And Company | Bace inhibitors |
| TWI593692B (zh) * | 2013-03-12 | 2017-08-01 | 美國禮來大藥廠 | 四氫吡咯并噻嗪化合物 |
| TWI684452B (zh) * | 2014-03-14 | 2020-02-11 | 美國禮來大藥廠 | 胺基噻嗪化合物 |
| TWI570127B (zh) | 2014-09-15 | 2017-02-11 | 美國禮來大藥廠 | 結晶型N-[3-[(4aR,7aS)-2-胺基-6-(5-氟嘧啶-2-基)-4,4a,5,7-四氫吡咯并[3,4-d][1,3]噻嗪-7a-基]-4-氟-苯基]-5-甲氧基-吡嗪-2-甲醯胺、其用途及醫藥組合物 |
| JP2019524788A (ja) * | 2016-08-11 | 2019-09-05 | イーライ リリー アンド カンパニー | アミノチアジンおよびｂａｃｅ１阻害剤としてのそれらの使用 |
| TWI726329B (zh) | 2018-06-22 | 2021-05-01 | 美商美國禮來大藥廠 | 2,3-二氫呋喃并[2,3-b]吡啶化合物 |
| CN111184725B (zh) * | 2020-02-27 | 2020-12-01 | 慈溪市人民医院医疗健康集团(慈溪市人民医院) | 一种防治脑梗塞的药物制剂及其制备方法 |
| CN111675659B (zh) * | 2020-06-16 | 2022-03-11 | 阿里生物新材料（常州）有限公司 | 一种（5-氟嘧啶-4-基）甲醇的合成方法 |
| CN112263583B (zh) * | 2020-11-23 | 2021-10-22 | 诸城市精神卫生中心 | 一种治疗帕金森疾病的药物及其制备方法 |
| CN113666878A (zh) * | 2021-08-27 | 2021-11-19 | 宁夏常晟药业有限公司 | 一种5-溴-2-氯嘧啶-4-羧酸甲酯的合成方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1896478B1 (en) * | 2005-06-14 | 2014-05-21 | Merck Sharp & Dohme Corp. | Aspartyl protease inhibitors |
| WO2008133273A1 (ja) * | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| US8158620B2 (en) * | 2008-01-18 | 2012-04-17 | Eisai R&D Management Co., Ltd. | Fused aminodihydrothiazine derivatives |
| JP2011518224A (ja) | 2008-04-22 | 2011-06-23 | シェーリング コーポレイション | Ｂａｃｅ−１阻害剤としてのチオフェニル置換２−イミノ−３−メチルピロロピリミジノン化合物、組成物、およびそれらの使用 |
| ES2539859T3 (es) | 2008-09-30 | 2015-07-06 | Eisai R&D Management Co., Ltd. | Nuevo derivado de aminodihidrotiazina condensado |
| AR077277A1 (es) | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
| GB0912778D0 (en) * | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| US7964594B1 (en) * | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
| EP2511269A4 (en) | 2009-12-11 | 2013-04-24 | Shionogi & Co | FUSED HETEROCYCLIC COMPOUND HAVING AN AMINO GROUP |
| AR086539A1 (es) | 2011-05-24 | 2014-01-08 | Bristol Myers Squibb Co | COMPUESTOS PARA LA REDUCCION DE LA PRODUCCION DE b-AMILOIDE |
| JP6043355B2 (ja) | 2011-08-31 | 2016-12-14 | ファイザー・インク | ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物 |
-
2013
- 2013-03-21 JO JOP/2013/0080A patent/JO3143B1/ar active
- 2013-03-22 AR ARP130100947A patent/AR090474A1/es unknown
- 2013-03-22 TW TW102110358A patent/TWI572610B/zh not_active IP Right Cessation
- 2013-03-27 SI SI201330189A patent/SI2836495T1/sl unknown
- 2013-03-27 CA CA2866201A patent/CA2866201C/en not_active Expired - Fee Related
- 2013-03-27 WO PCT/US2013/033959 patent/WO2013151832A1/en active Application Filing
- 2013-03-27 RS RS20160505A patent/RS54899B1/sr unknown
- 2013-03-27 US US13/851,116 patent/US8629270B2/en not_active Expired - Fee Related
- 2013-03-27 JP JP2015504623A patent/JP6067099B2/ja not_active Expired - Fee Related
- 2013-03-27 EP EP13715556.0A patent/EP2836495B1/en active Active
- 2013-03-27 HU HUE13715556A patent/HUE030097T2/en unknown
- 2013-03-27 CN CN201380017730.6A patent/CN104185635B/zh not_active Expired - Fee Related
- 2013-03-27 PT PT137155560T patent/PT2836495T/pt unknown
- 2013-03-27 DK DK13715556.0T patent/DK2836495T3/en active
- 2013-03-27 ES ES13715556.0T patent/ES2584827T3/es active Active
- 2013-03-27 ME MEP-2016-117A patent/ME02404B/me unknown
- 2013-03-27 PL PL13715556.0T patent/PL2836495T3/pl unknown
- 2013-12-04 US US14/096,443 patent/US8772282B2/en not_active Expired - Fee Related
-
2014
- 2014-05-22 US US14/284,452 patent/US8889856B2/en not_active Expired - Fee Related
-
2016
- 2016-06-14 HR HRP20160674TT patent/HRP20160674T1/hr unknown
- 2016-06-24 CY CY20161100566T patent/CY1117688T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP2836495B1 (en) | 2016-05-18 |
| JO3143B1 (ar) | 2017-09-20 |
| JP2015512445A (ja) | 2015-04-27 |
| EP2836495A1 (en) | 2015-02-18 |
| ME02404B (me) | 2016-09-20 |
| ES2584827T3 (es) | 2016-09-29 |
| AR090474A1 (es) | 2014-11-12 |
| CN104185635B (zh) | 2016-03-09 |
| CY1117688T1 (el) | 2017-05-17 |
| CA2866201C (en) | 2016-09-20 |
| SI2836495T1 (sl) | 2016-06-30 |
| US20140094454A1 (en) | 2014-04-03 |
| RS54899B1 (sr) | 2016-10-31 |
| US20140256933A1 (en) | 2014-09-11 |
| JP6067099B2 (ja) | 2017-01-25 |
| PT2836495T (pt) | 2016-07-18 |
| CN104185635A (zh) | 2014-12-03 |
| TWI572610B (zh) | 2017-03-01 |
| CA2866201A1 (en) | 2013-10-10 |
| US8629270B2 (en) | 2014-01-14 |
| US8772282B2 (en) | 2014-07-08 |
| TW201400491A (zh) | 2014-01-01 |
| DK2836495T3 (en) | 2016-08-15 |
| HUE030097T2 (en) | 2017-04-28 |
| US8889856B2 (en) | 2014-11-18 |
| WO2013151832A1 (en) | 2013-10-10 |
| PL2836495T3 (pl) | 2016-11-30 |
| US20130261111A1 (en) | 2013-10-03 |
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