EA031132B1 - 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера - Google Patents
2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера Download PDFInfo
- Publication number
- EA031132B1 EA031132B1 EA201691447A EA201691447A EA031132B1 EA 031132 B1 EA031132 B1 EA 031132B1 EA 201691447 A EA201691447 A EA 201691447A EA 201691447 A EA201691447 A EA 201691447A EA 031132 B1 EA031132 B1 EA 031132B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- amino
- fluorophenyl
- dimethyl
- trifluoro
- carboxamide
- Prior art date
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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
-
- 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
-
- 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
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D227/00—Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00
- C07D227/02—Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D227/06—Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D227/10—Nitrogen atoms not forming part of a nitro radical
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201400086 | 2014-02-19 | ||
| DKPA201400349 | 2014-07-01 | ||
| PCT/EP2015/053327 WO2015124576A1 (en) | 2014-02-19 | 2015-02-17 | 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201691447A1 EA201691447A1 (ru) | 2016-12-30 |
| EA031132B1 true EA031132B1 (ru) | 2018-11-30 |
Family
ID=59009438
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201691447A EA031132B1 (ru) | 2014-02-19 | 2015-02-17 | 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US20170066741A1 (enExample) |
| EP (1) | EP3107897A1 (enExample) |
| JP (1) | JP6483146B2 (enExample) |
| KR (1) | KR20160115936A (enExample) |
| CN (1) | CN106029639B (enExample) |
| AP (1) | AP2016009370A0 (enExample) |
| AR (1) | AR099489A1 (enExample) |
| AU (1) | AU2015220873A1 (enExample) |
| CA (1) | CA2940028A1 (enExample) |
| CL (1) | CL2016002072A1 (enExample) |
| CR (1) | CR20160352A (enExample) |
| DO (1) | DOP2016000194A (enExample) |
| EA (1) | EA031132B1 (enExample) |
| EC (1) | ECSP16072941A (enExample) |
| GE (2) | GEAP201814248A (enExample) |
| IL (1) | IL246875A0 (enExample) |
| MA (1) | MA39225A1 (enExample) |
| MX (1) | MX2016010777A (enExample) |
| PE (1) | PE20161225A1 (enExample) |
| PH (1) | PH12016501600A1 (enExample) |
| RU (1) | RU2016133626A (enExample) |
| SG (1) | SG11201606812WA (enExample) |
| TW (1) | TW201609700A (enExample) |
| UA (1) | UA117695C2 (enExample) |
| WO (1) | WO2015124576A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GEAP201814248A (en) | 2014-02-19 | 2018-04-10 | H Lundbeck As | 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease |
| 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 |
| 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 |
| 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 |
| 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 |
| JP2018531889A (ja) * | 2015-08-12 | 2018-11-01 | ハー・ルンドベック・アクチエゼルスカベット | Ｂａｃｅ１阻害剤としての２−アミノ−３−フルオロ−３−（フルオロメチル）−６−メチル−６−フェニル−３，４，５，６−テトラヒドロピリジン |
| CA2997947A1 (en) * | 2015-09-09 | 2017-03-16 | The Trustees Of Columbia University In The City Of New York | Reduction of er-mam-localized app-c99 and methods of treating alzheimer's disease |
| TW201726651A (zh) * | 2015-09-23 | 2017-08-01 | 健生藥品公司 | ２，３，４，５－四氫吡啶－６－胺衍生物 |
| US10034861B2 (en) | 2016-07-04 | 2018-07-31 | H. Lundbeck A/S | 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors |
| EP3532064B1 (en) | 2016-10-28 | 2020-07-29 | H. Lundbeck A/S | Combination treatments comprising imidazopyrazinones for the treatment of psychiatric and/or cognitive disorders |
| KR20190077349A (ko) | 2016-10-28 | 2019-07-03 | 하. 룬드벡 아크티에셀스카브 | 이미다조피라지논의 투여를 포함하는 병용 치료 |
| BR112018017058A2 (pt) | 2016-12-21 | 2019-07-02 | H Lundbeck As | 6-amino-5-fluoro-5-(fluorometil)-2,3,4,5-tetra-hidropiridin-2-il-fenil-5-(metóxi-d3)-pirazina-2-carboxamidas e derivados fluorados do mesmo como inibidores de bace1 |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| JP2021501130A (ja) | 2017-10-05 | 2021-01-14 | フルクラム セラピューティクス，インコーポレイテッド | ＤＵＸ４の発現を低減するためのｐ３８阻害剤の使用 |
| RS62551B1 (sr) | 2017-12-14 | 2021-12-31 | H Lundbeck As | Kombinovane terapije koje obuhvataju primenu 1h-pirazolo[4,3-b]piridina |
| AR113926A1 (es) | 2017-12-14 | 2020-07-01 | H Lundbeck As | Derivados de 1h-pirazolo[4,3-b]piridinas |
| EP3728250A1 (en) | 2017-12-20 | 2020-10-28 | H. Lundbeck A/S | PYRAZOLO[3,4-beta]PYRIDINES AND IMIDAZO[1,5-beta]PYRIDAZINES AS PDE1 INHIBITORS |
| KR102507861B1 (ko) | 2018-04-19 | 2023-03-09 | 삼성에스디에스 주식회사 | 부채널 공격에 안전한 연산 장치 및 방법 |
| KR102510077B1 (ko) | 2018-04-24 | 2023-03-14 | 삼성에스디에스 주식회사 | 부채널 공격에 안전한 연산 장치 및 방법 |
| US12042492B2 (en) | 2020-10-09 | 2024-07-23 | Texas Tech University System | BACE1 inhibitory ligand molecules against amyloid beta-induced synaptic and mitochondrial toxicities |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003032970A1 (en) * | 2001-10-17 | 2003-04-24 | Glaxo Group Limited | 5'-carbamoyl-2'-methyl-1,1'-biphenyl-4-carboxamide derivatives and their use as p38 kinase inhibitors |
| WO2003068747A1 (en) * | 2002-02-12 | 2003-08-21 | Smithkline Beecham Corporation | Nicotinamide derivates useful as p38 inhibitors |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR0210391A (pt) * | 2001-06-12 | 2004-06-15 | Elan Pharm Inc | Composto, métodos de tratar um paciente que tenha ou de prevenir um paciente de contrair uma doença ou condição e de preparar um composto, e, uso de um composto |
| TWI431004B (zh) * | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Ｂａｃｅ抑制劑 |
| KR101730937B1 (ko) * | 2010-06-09 | 2017-04-27 | 얀센 파마슈티카 엔.브이. | 베타-세크레타아제(ｂａｃｅ) 저해제로 유용한 5,6-디하이드로-2ｈ-[1,4]옥사진-3-일-아민 유도체 |
| CN103261199A (zh) * | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
| KR20140051822A (ko) | 2011-01-12 | 2014-05-02 | 노파르티스 아게 | 옥사진 유도체 및 신경계 장애의 치료에서의 그의 용도 |
| DK2663561T3 (en) * | 2011-01-13 | 2016-06-06 | Novartis Ag | New heterocyclic derivatives and their use in treating neurological disorders |
| US8754075B2 (en) * | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
| CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
| AU2012266544A1 (en) * | 2011-06-07 | 2013-11-21 | F. Hoffmann-La Roche Ag | Halogen-alkyl-1,3 oxazines as BACE1 and/or BACE2 inhibitors |
| 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 |
| JP2015514073A (ja) | 2012-03-20 | 2015-05-18 | エラン ファーマシューティカルズ， リミテッド・ライアビリティ・カンパニー | スピロ環式ジヒドロ−チアジンおよびジヒドロ−オキサジンｂａｃｅ阻害剤、ならびにその組成物および使用 |
| WO2014056816A1 (en) | 2012-10-10 | 2014-04-17 | F. Hoffmann-La Roche Ag | COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR |
| WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
| JP6389830B2 (ja) | 2013-03-01 | 2018-09-12 | アムジエン・インコーポレーテツド | ベータ−セクレターゼ阻害剤としてのパーフルオロ化５，６−ジヒドロ−４ｈ−１，３−オキサジン−２−アミン化合物および使用方法 |
| GEAP201814248A (en) | 2014-02-19 | 2018-04-10 | 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 |
-
2015
- 2015-02-17 GE GEAP201814248A patent/GEAP201814248A/en unknown
- 2015-02-17 KR KR1020167021930A patent/KR20160115936A/ko not_active Withdrawn
- 2015-02-17 AP AP2016009370A patent/AP2016009370A0/en unknown
- 2015-02-17 MX MX2016010777A patent/MX2016010777A/es unknown
- 2015-02-17 RU RU2016133626A patent/RU2016133626A/ru not_active Application Discontinuation
- 2015-02-17 GE GEAP201514248A patent/GEP20186892B/en unknown
- 2015-02-17 JP JP2016551851A patent/JP6483146B2/ja not_active Expired - Fee Related
- 2015-02-17 MA MA39225A patent/MA39225A1/fr unknown
- 2015-02-17 US US15/119,639 patent/US20170066741A1/en not_active Abandoned
- 2015-02-17 EP EP15707304.0A patent/EP3107897A1/en not_active Withdrawn
- 2015-02-17 UA UAA201608414A patent/UA117695C2/uk unknown
- 2015-02-17 TW TW104105281A patent/TW201609700A/zh unknown
- 2015-02-17 PE PE2016001299A patent/PE20161225A1/es not_active Application Discontinuation
- 2015-02-17 AU AU2015220873A patent/AU2015220873A1/en not_active Abandoned
- 2015-02-17 CN CN201580009034.XA patent/CN106029639B/zh not_active Expired - Fee Related
- 2015-02-17 CR CR20160352A patent/CR20160352A/es unknown
- 2015-02-17 EA EA201691447A patent/EA031132B1/ru not_active IP Right Cessation
- 2015-02-17 WO PCT/EP2015/053327 patent/WO2015124576A1/en not_active Ceased
- 2015-02-17 SG SG11201606812WA patent/SG11201606812WA/en unknown
- 2015-02-17 CA CA2940028A patent/CA2940028A1/en not_active Abandoned
- 2015-02-18 AR ARP150100475A patent/AR099489A1/es unknown
- 2015-02-19 US US14/625,658 patent/US9353084B2/en not_active Expired - Fee Related
-
2016
- 2016-07-21 IL IL246875A patent/IL246875A0/en unknown
- 2016-07-28 DO DO2016000194A patent/DOP2016000194A/es unknown
- 2016-08-11 PH PH12016501600A patent/PH12016501600A1/en unknown
- 2016-08-17 CL CL2016002072A patent/CL2016002072A1/es unknown
- 2016-09-09 EC ECIEPI201672941A patent/ECSP16072941A/es unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003032970A1 (en) * | 2001-10-17 | 2003-04-24 | Glaxo Group Limited | 5'-carbamoyl-2'-methyl-1,1'-biphenyl-4-carboxamide derivatives and their use as p38 kinase inhibitors |
| WO2003068747A1 (en) * | 2002-02-12 | 2003-08-21 | Smithkline Beecham Corporation | Nicotinamide derivates useful as p38 inhibitors |
Non-Patent Citations (7)
| Title |
|---|
| GARY PROBST, YING-ZI XU: "Small-molecule BACE1 inhibitors: a patent literature review (2006 – 2011)", EXPERT OPINION ON THERAPEUTIC PATENTS, vol. 22, no. 5, 1 May 2012 (2012-05-01), pages 511 - 540, XP055175034, ISSN: 13543776, DOI: 10.1517/13543776.2012.681302 * |
| Hans Hilpert ET AL.: "S1 Supporting Information [beta]-Secretase (BACE1) Inhibitors with High In Vivo Efficacy Suitable for Clinical Evaluation in Alzheimer's Disease", 16 May 2013 (2013-05-16), pages 66-70, XP055102028, Retrieved from the Internet: URL:http://pubs.acs.org/doi/suppl/10.1021/jm400225m/suppl_file/jm400225m_si_001.pdf [retrieved on 2014-02-13], compounds 14b, 14b-14v, 66-113 * |
| HANS HILPERT, WOLFGANG GUBA, THOMAS J. WOLTERING, WOLFGANG WOSTL, EMMANUEL PINARD, HARALD MAUSER, ALEXANDER V. MAYWEG, MARK ROGERS: "β-Secretase (BACE1) Inhibitors with High in Vivo Efficacy Suitable for Clinical Evaluation in Alzheimer’s Disease", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 56, no. 10, 23 May 2013 (2013-05-23), pages 3980 - 3995, XP055113495, ISSN: 00222623, DOI: 10.1021/jm400225m * |
| MALAMAS, M.S. ; BARNES, K. ; HUI, Y. ; JOHNSON, M. ; LOVERING, F. ; CONDON, J. ; FOBARE, W. ; SOLVIBILE, W. ; TURNER, J. ; HU, Y. : "Novel pyrrolyl 2-aminopyridines as potent and selective human sz-secretase (BACE1) inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, vol. 20, no. 7, 1 April 2010 (2010-04-01), AMSTERDAM, NL, pages 2068 - 2073, XP026971013, ISSN: 0960-894X * |
| SO-YOUNG JEON, KIHWAN BAE, YEON-HEE SEONG, KYUNG-SIK SONG: "Green tea catechins as a BACE1 (β-Secretase) inhibitor", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, vol. 13, no. 22, 1 November 2003 (2003-11-01), pages 3905 - 3908, XP055049387, ISSN: 0960894X, DOI: 10.1016/j.bmcl.2003.09.018 * |
| WOLTERING THOMAS J.; WOSTL WOLFGANG; HILPERT HANS; ROGERS-EVANS MARK; PINARD EMMANUEL; MAYWEG ALEXANDER; G�BEL MARTIN; BANNER DAVI: "BACE1 inhibitors: A head group scan on a series of amides", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, vol. 23, no. 14, 18 May 2013 (2013-05-18), AMSTERDAM, NL, pages 4239 - 4243, XP028573309, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2013.05.003 * |
| YOSHIO HAMADA, YOSHIAKI KISO: "Recent progress in the drug discovery of non-peptidic BACE1 inhibitors", EXPERT OPINION ON DRUG DISCOVERY, INFORMA HEALTHCARE, LONDON, GB, vol. 4, no. 4, 1 January 2009 (2009-01-01), London, GB, pages 391 - 416, XP009147269, ISSN: 1746-0441 * |
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| IL246875A0 (en) | 2016-08-31 |
| RU2016133626A (ru) | 2018-03-20 |
| GEAP201814248A (en) | 2018-04-10 |
| WO2015124576A1 (en) | 2015-08-27 |
| AR099489A1 (es) | 2016-07-27 |
| EP3107897A1 (en) | 2016-12-28 |
| TW201609700A (zh) | 2016-03-16 |
| MX2016010777A (es) | 2016-10-26 |
| KR20160115936A (ko) | 2016-10-06 |
| CA2940028A1 (en) | 2015-08-27 |
| PH12016501600A1 (en) | 2017-02-06 |
| JP2017506237A (ja) | 2017-03-02 |
| EA201691447A1 (ru) | 2016-12-30 |
| US20150232449A1 (en) | 2015-08-20 |
| SG11201606812WA (en) | 2016-09-29 |
| CL2016002072A1 (es) | 2017-01-20 |
| DOP2016000194A (es) | 2016-09-30 |
| UA117695C2 (uk) | 2018-09-10 |
| AP2016009370A0 (en) | 2016-08-31 |
| CN106029639B (zh) | 2019-01-08 |
| AU2015220873A1 (en) | 2016-08-11 |
| GEP20186892B (en) | 2018-09-10 |
| JP6483146B2 (ja) | 2019-03-13 |
| PE20161225A1 (es) | 2016-12-04 |
| MA39225A1 (fr) | 2017-04-28 |
| RU2016133626A3 (enExample) | 2018-09-25 |
| US20170066741A1 (en) | 2017-03-09 |
| CR20160352A (es) | 2016-10-20 |
| US9353084B2 (en) | 2016-05-31 |
| ECSP16072941A (es) | 2017-02-24 |
| CN106029639A (zh) | 2016-10-12 |
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