ME03723B - 2-amin0-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridini kао васе1 inhibiтori - Google Patents
2-amin0-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridini kао васе1 inhibiтoriInfo
- Publication number
- ME03723B ME03723B MEP-2018-267A MEP2018267A ME03723B ME 03723 B ME03723 B ME 03723B ME P2018267 A MEP2018267 A ME P2018267A ME 03723 B ME03723 B ME 03723B
- Authority
- ME
- Montenegro
- Prior art keywords
- difluoromethyl
- difluoro
- amino
- tetrahydropyridin
- fluorophenyl
- Prior art date
Links
- 229940125759 BACE1 protease inhibitor Drugs 0.000 title 1
- MSTNBPFTUMAVJC-UHFFFAOYSA-N NC1=NC(C(CC1)(F)F)(C1=CC=CC=C1)C(F)F Chemical compound NC1=NC(C(CC1)(F)F)(C1=CC=CC=C1)C(F)F MSTNBPFTUMAVJC-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 15
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- ZOJVANVWTPGCGF-SFHVURJKSA-N NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(=O)C1=NC=C(C=N1)OC)(F)F Chemical compound NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(=O)C1=NC=C(C=N1)OC)(F)F ZOJVANVWTPGCGF-SFHVURJKSA-N 0.000 claims 1
- OXHGYPKMJMHUJT-IBGZPJMESA-N NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(=O)C1=NC=C(N=C1C)OC)(F)F Chemical compound NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(=O)C1=NC=C(N=C1C)OC)(F)F OXHGYPKMJMHUJT-IBGZPJMESA-N 0.000 claims 1
- BWFWHBMZSDOQJG-KRWDZBQOSA-N NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(=O)C=1N=C(OC=1)C)(F)F Chemical compound NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(=O)C=1N=C(OC=1)C)(F)F BWFWHBMZSDOQJG-KRWDZBQOSA-N 0.000 claims 1
- SCASMRHOWHFBAH-SFHVURJKSA-N NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(C1=NC=C(C=C1)Br)=O)(F)F Chemical compound NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(C1=NC=C(C=C1)Br)=O)(F)F SCASMRHOWHFBAH-SFHVURJKSA-N 0.000 claims 1
- FGBKLHOHAIWKKJ-SFHVURJKSA-N NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(C1=NC=C(C=C1)Cl)=O)(F)F Chemical compound NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(C1=NC=C(C=C1)Cl)=O)(F)F FGBKLHOHAIWKKJ-SFHVURJKSA-N 0.000 claims 1
- PEEPRUHZLOVBDY-COJYBMMNSA-N NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(C1=NC=C(C=C1)OC([2H])([2H])[2H])=O)(F)F Chemical compound NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(C1=NC=C(C=C1)OC([2H])([2H])[2H])=O)(F)F PEEPRUHZLOVBDY-COJYBMMNSA-N 0.000 claims 1
- BMEKAAPGFZBYOC-FQEVSTJZSA-N NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(C1=NC=C(C=C1C)C#N)=O)(F)F Chemical compound NC=1CCC([C@@](N=1)(C(F)F)C=1C=C(C=CC=1F)NC(C1=NC=C(C=C1C)C#N)=O)(F)F BMEKAAPGFZBYOC-FQEVSTJZSA-N 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/12—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 linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Claims (13)
1. Jedinjenje formule I u kojoj je Ar odabran iz grupe koju čine fenil, piridil, pirimidil, pirazinil, imidazolil, pirazolil, tiazolil, oksazolil, izoksazolil, i gde je Ar opciono supstituisani jednim ili više supstituenata odabran od halogena, CN, C1-C6 alkila, C2-C6 alkenila, C2-C6 alkinila, C1-C6 fluoroalkila ili C1-C6 alkoksi; iR1 je vodonik, halogen, C1-C3 fluoroalkil ili C1-C3 alkil;ili njegova farmaceutski prihvatljiva so.
2.Jedinjenje prema zahtevu 1, gde je to jedinjenje formule Ia ili njegova farmaceutski prihvatljiva so.
3.Jedinjenje prema zahtevu 1 ili 2, gde R1 je F ili H.
4.Jedinjenje prema zahtevu 1 ili 2, gde je Ar opciono supstituisan jednim ili više F, Cl, Br, CN, C1-C3 alkila, C1-C3 fluoroalkila ili C1-C3 alkoksi.
5.Jedinjenje prema bilo kom od zahteva 1-4, gde je Ar opciono supstituisani piridil.
6.Jedinjenje prema bilo kom od zahteva 1-4, gde je Ar opciono supstituisani pirimidil.
7.Jedinjenje prema bilo kom od zahteva 1-4, gde je Ar opciono supstituisani pirazinil.
8.Jedinjenje prema bilo kom od zahteva 1-4, gde je Ar opciono supstituisani oksazolil.
9.Jedinjenje prema bilo kom od zahteva 1-4, gde je Ar opciono supstituisani tiazolil.
10.Jedinjenje prema zahtevu 1, gde je to jedinjenje odabrano iz grupe koju čine: (S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-hloropikolinamid,(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-fluoropikolinamid,(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-metoksipirazin-2-karboksamid,(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-2-metiloksazol-4-karboksamid,(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-metoksipikolinamid,(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-(difluorometil)pirazin-2-karboksamid,(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-cijanopikolinamid,(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-4- metiltiazol-2-karboksamid,(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-metoksipirimidin-2-karboksamid,(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-metoksi-3-metilpirazin-2-karboksamid,(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-cijano-3-metilpikolinamid,(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-bromopikolinamid,(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-(metoksi-d3)pikolinamid i(S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-(metoksi-d3)pirazin-2-karboksamid;ili njegova farmaceutski prihvatljiva so.
11.Farmaceutska kombinacija koja obuhvata jedinjenje prema bilo kom od zahteva 1-10 i farmaceutski prihvatljiv nosač.
12.Jedinjenje prema bilo kom od zahteva 1-10 za upotrebu u terapiji.
13.Jedinjenje prema bilo kom od zahteva 1-10 za upotrebu u lečenju bolesti odabrane od Achajmerove bolesti (porodična ili sporadična), prekliničke Achajmerove bolesti, prodromalne Achajmerove bolesti, blagog kognitivnog oštećenja, Daunovog sindroma i cerebralne amiloidne angiopatije.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201400648 | 2014-11-10 | ||
| DKPA201500447 | 2015-08-07 | ||
| PCT/EP2015/076015 WO2016075063A1 (en) | 2014-11-10 | 2015-11-09 | 2-amino-6-(difluoromethyl)- 5,5-difluoro-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors |
| EP15805109.4A EP3218365B1 (en) | 2014-11-10 | 2015-11-09 | 2-amino-6-(difluoromethyl)- 5,5-difluoro-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME03723B true ME03723B (me) | 2021-04-20 |
Family
ID=54783558
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2018-267A ME03723B (me) | 2014-11-10 | 2015-11-09 | 2-amin0-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridini kао васе1 inhibiтori |
Country Status (44)
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MA40941A (fr) | 2014-11-10 | 2017-09-19 | H Lundbeck As | 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 |
| CR20170187A (es) | 2014-11-10 | 2018-02-01 | H Lundbeck As | 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer |
| JO3458B1 (ar) | 2014-11-10 | 2020-07-05 | H Lundbeck As | 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 |
| JO3627B1 (ar) | 2015-04-30 | 2020-08-27 | H Lundbeck As | إيميدازو بيرازينونات على هيئة مثبطات pde1 |
| TW201717948A (zh) | 2015-08-10 | 2017-06-01 | Ｈ 朗德貝克公司 | 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療 |
| CA2993630A1 (en) * | 2015-08-12 | 2017-02-16 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors |
| US10034861B2 (en) | 2016-07-04 | 2018-07-31 | H. Lundbeck A/S | 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors |
| JOP20190081A1 (ar) * | 2016-10-13 | 2019-04-11 | Novartis Ag | مشتق أوكسازين للاستخدام في علاج أو الوقاية من اعتلال وعائي دماغي نشواني |
| WO2018078042A1 (en) | 2016-10-28 | 2018-05-03 | H. Lundbeck A/S | Combination treatments comprising administration of imidazopyrazinones |
| HUE050403T2 (hu) | 2016-10-28 | 2020-12-28 | H Lundbeck As | Imidazopirazinonokkal végzett kombinációs kezelések pszichiátriai és/vagy kognitív betegségek kezelésére |
| TW201829394A (zh) | 2016-12-21 | 2018-08-16 | 丹麥商Ｈ 朗德貝克公司 | 作為ｂａｃｅ１抑制劑之６-胺基-５-氟-５-（氟甲基）-２，３，４，５-四氫吡啶-２-基-苯基-５-（甲氧基-ｄ）-吡-２-甲醯胺及其氟化衍生物 |
| AR113926A1 (es) | 2017-12-14 | 2020-07-01 | H Lundbeck As | Derivados de 1h-pirazolo[4,3-b]piridinas |
| HRP20211784T1 (hr) | 2017-12-14 | 2022-02-18 | H. Lundbeck A/S | Kombinacijski tretmani koji se sastoje od primjene 1h-pirazolo[4,3-b]piridina |
| CN117447475A (zh) | 2017-12-20 | 2024-01-26 | H.隆德贝克有限公司 | 作为PDE1抑制剂的吡唑并[4,3-b]吡啶和咪唑并[1,5-a]嘧啶 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2450167A1 (en) | 2001-06-12 | 2002-12-19 | Elan Pharmaceuticals, Inc. | Macrocycles useful in the treatment of alzheimer's disease |
| GB0124928D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| ES2295553T3 (es) | 2002-02-12 | 2008-04-16 | Smithkline Beecham Corporation | Derivados de nicotinamida utiles como inhibidores de p38. |
| 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 |
| EA021240B1 (ru) * | 2010-06-09 | 2015-05-29 | Янссен Фармацевтика Нв | Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace) |
| JP2014505688A (ja) | 2011-01-12 | 2014-03-06 | ノバルティス アーゲー | オキサジン誘導体および神経障害の処置におけるその使用 |
| CN106117193B (zh) | 2011-01-13 | 2019-09-13 | 诺华股份有限公司 | 新的杂环衍生物及其在神经性疾病治疗中的应用 |
| US8754075B2 (en) | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
| TW201247635A (en) | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
| EA023261B1 (ru) * | 2011-06-07 | 2016-05-31 | Ф.Хоффманн-Ля Рош Аг | Галоген-алкил-1,3-оксазины в качестве ингибиторов bace1 и(или) bace2 |
| UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
| US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| EP2827857A4 (en) | 2012-03-20 | 2016-03-30 | Elan Pharm Inc | SPIROCYCLIC DIHYDRO-THIAZINE AND INHIBITORS OF BACE DIHYDRO-OXAZINE AND COMPOSITIONS AND USES THEREOF |
| WO2014056816A1 (en) | 2012-10-10 | 2014-04-17 | F. Hoffmann-La Roche Ag | COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR |
| JP2016501827A (ja) | 2012-10-24 | 2016-01-21 | 塩野義製薬株式会社 | Ｂａｃｅ１阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
| CA2902212C (en) | 2013-03-01 | 2020-10-13 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| JO3318B1 (ar) | 2013-06-18 | 2019-03-13 | Lilly Co Eli | مثبطات bace |
| AP2016009370A0 (en) | 2014-02-19 | 2016-08-31 | H Lundbeck As | 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease |
| TW201623295A (zh) | 2014-04-11 | 2016-07-01 | 塩野義製藥股份有限公司 | 具有ｂａｃｅ１抑制活性之二氫噻及二氫衍生物 |
| JO3458B1 (ar) | 2014-11-10 | 2020-07-05 | H Lundbeck As | 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 |
| MA40941A (fr) | 2014-11-10 | 2017-09-19 | H Lundbeck As | 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 |
| CR20170187A (es) | 2014-11-10 | 2018-02-01 | H Lundbeck As | 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer |
| TW201717948A (zh) | 2015-08-10 | 2017-06-01 | Ｈ 朗德貝克公司 | 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療 |
| CA2993630A1 (en) | 2015-08-12 | 2017-02-16 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors |
| TW201829394A (zh) | 2016-12-21 | 2018-08-16 | 丹麥商Ｈ 朗德貝克公司 | 作為ｂａｃｅ１抑制劑之６-胺基-５-氟-５-（氟甲基）-２，３，４，５-四氫吡啶-２-基-苯基-５-（甲氧基-ｄ）-吡-２-甲醯胺及其氟化衍生物 |
-
2015
- 2015-10-25 JO JOP/2015/0260A patent/JO3458B1/ar active
- 2015-11-05 US US14/933,301 patent/US9346797B1/en not_active Expired - Fee Related
- 2015-11-09 WO PCT/EP2015/076015 patent/WO2016075063A1/en not_active Ceased
- 2015-11-09 ES ES15805109.4T patent/ES2694860T3/es active Active
- 2015-11-09 TW TW104136839A patent/TWI690318B/zh not_active IP Right Cessation
- 2015-11-09 JP JP2017525010A patent/JP6629320B2/ja not_active Expired - Fee Related
- 2015-11-09 LT LTEP15805109.4T patent/LT3218365T/lt unknown
- 2015-11-09 EP EP18198764.5A patent/EP3461483A1/en not_active Withdrawn
- 2015-11-09 CN CN201580060803.9A patent/CN107074836B/zh not_active Expired - Fee Related
- 2015-11-09 AU AU2015345258A patent/AU2015345258B2/en not_active Expired - Fee Related
- 2015-11-09 RU RU2017116196A patent/RU2017116196A/ru not_active Application Discontinuation
- 2015-11-09 EP EP15805109.4A patent/EP3218365B1/en active Active
- 2015-11-09 ME MEP-2018-267A patent/ME03723B/me unknown
- 2015-11-09 SM SM20180570T patent/SMT201800570T1/it unknown
- 2015-11-09 SG SG11201703547XA patent/SG11201703547XA/en unknown
- 2015-11-09 CA CA2965563A patent/CA2965563A1/en not_active Abandoned
- 2015-11-09 RS RS20181321A patent/RS57946B1/sr unknown
- 2015-11-09 TR TR2018/16427T patent/TR201816427T4/tr unknown
- 2015-11-09 BR BR112017009583A patent/BR112017009583A2/pt not_active Application Discontinuation
- 2015-11-09 CR CR20170186A patent/CR20170186A/es unknown
- 2015-11-09 TN TN2017000144A patent/TN2017000144A1/en unknown
- 2015-11-09 US US15/524,546 patent/US10045974B2/en not_active Expired - Fee Related
- 2015-11-09 EA EA201790818A patent/EA032339B1/ru not_active IP Right Cessation
- 2015-11-09 HR HRP20181698TT patent/HRP20181698T1/hr unknown
- 2015-11-09 MX MX2017006049A patent/MX2017006049A/es unknown
- 2015-11-09 KR KR1020177012442A patent/KR20170081184A/ko not_active Withdrawn
- 2015-11-09 HU HUE15805109A patent/HUE040304T2/hu unknown
- 2015-11-09 SI SI201530464T patent/SI3218365T1/sl unknown
- 2015-11-09 MA MA40955A patent/MA40955B1/fr unknown
- 2015-11-09 UA UAA201704639A patent/UA119576C2/uk unknown
- 2015-11-09 PL PL15805109T patent/PL3218365T3/pl unknown
- 2015-11-09 PE PE2017000825A patent/PE20170946A1/es unknown
- 2015-11-09 GE GEAP201514485A patent/GEP20196949B/en unknown
- 2015-11-09 DK DK15805109.4T patent/DK3218365T3/en active
- 2015-11-09 PT PT15805109T patent/PT3218365T/pt unknown
-
2017
- 2017-04-20 ZA ZA2017/02797A patent/ZA201702797B/en unknown
- 2017-05-03 CO CONC2017/0004465A patent/CO2017004465A2/es unknown
- 2017-05-03 IL IL252089A patent/IL252089B/en not_active IP Right Cessation
- 2017-05-04 CL CL2017001112A patent/CL2017001112A1/es unknown
- 2017-05-05 PH PH12017500841A patent/PH12017500841B1/en unknown
- 2017-05-09 DO DO2017000117A patent/DOP2017000117A/es unknown
- 2017-05-09 SV SV2017005435A patent/SV2017005435A/es unknown
- 2017-05-09 NI NI201700055A patent/NI201700055A/es unknown
- 2017-05-09 EC ECIEPI201728459A patent/ECSP17028459A/es unknown
- 2017-05-10 GT GT201700099A patent/GT201700099A/es unknown
-
2018
- 2018-08-09 US US16/059,715 patent/US10603310B2/en not_active Expired - Fee Related
- 2018-11-13 CY CY20181101200T patent/CY1120846T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ME03723B (me) | 2-amin0-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridini kао васе1 inhibiтori | |
| ZA202500997B (en) | Benzoxazepin oxazolidinone compounds and methods of use | |
| GEP20217248B (en) | 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of dhodh | |
| RU2017120217A (ru) | 2-амино-5,5-дифтор-6-(фторметил)-6-фенил-3,4,5,6-тетрагидпропиридины в качестве ингибиторов bace1 | |
| PH12016501440A1 (en) | Novel heterocyclic compounds | |
| EA202091120A3 (ru) | Производные 2,4-тиазолинидона в лечении расстройств центральной нервной системы | |
| PE20181144A1 (es) | Derivados de heteroarilo como inhibidores de parp | |
| RU2017127135A (ru) | Терапевтическое средство против рака желчных протоков | |
| HRP20210447T1 (hr) | Piridinski spoj | |
| EA201591727A1 (ru) | Соединения биариламида в качестве ингибиторов киназы | |
| NZ630124A (en) | Estrogen receptor modulators and uses thereof | |
| DK3160958T3 (da) | Krystallinske salte af (s)-6-((1-acetylpiperidin-4-yl)amino)-n-(3-(3,4-dihydroisoquinolin-2(1h)-yl)-2-hydroxypropyl)pyrimidin-4-carboxamid | |
| EA201592082A1 (ru) | 3,4-дигидроизохинолин-2(1h)-ильные соединения | |
| UA112317C2 (uk) | Похідні 2-(1,2,3-триазол-2-іл)бензаміду та 3-(1,2,3-триазол-2-іл)піколінаміду як антагоністи рецептора орексину | |
| AR105668A1 (es) | 2-amino-3-fluoro-3-(fluorometil)-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 | |
| HRP20170873T1 (hr) | Monociklički derivat piridina | |
| TW201613890A (en) | Pyridine derivatives as muscarinic M1 receptor positive allosteric modulators | |
| HRP20220683T1 (hr) | Liječenje parkinsonove bolesti | |
| RU2018119102A (ru) | Терапевтическое средство для лечения рака молочной железы | |
| PE20160666A1 (es) | Derivados de etinilo | |
| MX2015013414A (es) | N-(2-ciano heterociclil)pirazolo piridonas como inhibidores de janus quinasa. | |
| NZ598754A (en) | Therapeutic agent for anxiety disorders | |
| MX2016009939A (es) | Derivado de aminopirazolona. | |
| NZ707832A (en) | 2-pyridone compound | |
| MX349697B (es) | Nuevo derivado de fenilpiridina y farmaco que contiene el mismo. |