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 PDF

Info

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
trifluoro
dimethyl
carboxamide
Prior art date
Application number
EA201691447A
Other languages
English (en)
Russian (ru)
Other versions
EA201691447A1 (ru
Inventor
Карстен Джухл
Мауро Мариго
Лена Тагмозе
Томас Дженсен
Original Assignee
Х. Лундбекк А/С
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Х. Лундбекк А/С filed Critical Х. Лундбекк А/С
Publication of EA201691447A1 publication Critical patent/EA201691447A1/ru
Publication of EA031132B1 publication Critical patent/EA031132B1/ru

Links

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)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
EA201691447A 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 EA031132B1 (ru)

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 (1) GEP20186892B (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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106029639B (zh) 2014-02-19 2019-01-08 H.隆德贝克有限公司 治疗阿尔茨海默病的bace1抑制剂的2-氨基-3，5，5-三氟-3，4，5，6-四氢吡啶
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
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
US10011596B2 (en) * 2015-08-12 2018-07-03 H. Lundbeck A/S 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors
WO2017044807A2 (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
CA3041595A1 (en) 2016-10-28 2018-05-03 H. Lundbeck A/S Combination treatments comprising administration of imidazopyrazinones
WO2018078038A1 (en) 2016-10-28 2018-05-03 H. Lundbeck A/S Combination treatments comprising imidazopyrazinones for the treatment of psychiatric and/or cognitive disorders
WO2018114910A1 (en) 2016-12-21 2018-06-28 H. Lundbeck A/S 6-amino-5-fluoro-5-(fluoromethyl)-2,3,4,5-tetrahydropyridin-2-yl-phenyl-5-(methoxy-d3)-pyrazine-2-carboxamides and fluorinated derivatives thereof as bace1 inhibitors
UY37918A (es) 2017-10-05 2019-04-30 Fulcrum Therapeutics Inc Inhibidores de la quinasa p38 que reducen la expresión de dux4 y de los genes corriente abajo para el tratamiento de fshd
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
KR20200099154A (ko) 2017-12-14 2020-08-21 하. 룬드벡 아크티에셀스카브 1H-피라졸로[4,3-b]피리딘의 투여를 포함하는 조합 치료제
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
WO2019121840A1 (en) 2017-12-20 2019-06-27 H. Lundbeck A/S Pyrazolo[3,4-b]pyridines and imidazo[1,5-b]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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7067507B2 (en) * 2001-06-12 2006-06-27 Pharmacia & Upjohn Company Macrocycles useful in the treatment of Alzheimer's disease
TWI431004B (zh) * 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
EP2580200B1 (en) * 2010-06-09 2016-09-14 Janssen Pharmaceutica, N.V. 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
CN103261199A (zh) * 2010-10-29 2013-08-21 盐野义制药株式会社 萘啶衍生物
CA2824097A1 (en) * 2011-01-12 2012-07-19 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
MA34898B1 (fr) * 2011-01-13 2014-02-01 Novartis Ag Nouveaux dérivés hétérocycliques et leur utilisation dans le traitement de troubles neurologiques
US8754075B2 (en) * 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
WO2012147763A1 (ja) * 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤
WO2012168164A1 (en) * 2011-06-07 2012-12-13 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
WO2013142613A1 (en) 2012-03-20 2013-09-26 Elan Pharmaceuticals, Inc. Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, 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
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
AU2014223334C1 (en) 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
CN106029639B (zh) 2014-02-19 2019-01-08 H.隆德贝克有限公司 治疗阿尔茨海默病的bace1抑制剂的2-氨基-3，5，5-三氟-3，4，5，6-四氢吡啶
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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 *

Also Published As

Publication number Publication date
EA201691447A1 (ru) 2016-12-30
DOP2016000194A (es) 2016-09-30
KR20160115936A (ko) 2016-10-06
TW201609700A (zh) 2016-03-16
CL2016002072A1 (es) 2017-01-20
EP3107897A1 (en) 2016-12-28
UA117695C2 (uk) 2018-09-10
AR099489A1 (es) 2016-07-27
MA39225A1 (fr) 2017-04-28
GEP20186892B (en) 2018-09-10
US9353084B2 (en) 2016-05-31
CN106029639A (zh) 2016-10-12
AU2015220873A1 (en) 2016-08-11
RU2016133626A (ru) 2018-03-20
AP2016009370A0 (en) 2016-08-31
MX2016010777A (es) 2016-10-26
PE20161225A1 (es) 2016-12-04
CR20160352A (es) 2016-10-20
CA2940028A1 (en) 2015-08-27
RU2016133626A3 (enExample) 2018-09-25
ECSP16072941A (es) 2017-02-24
JP6483146B2 (ja) 2019-03-13
US20150232449A1 (en) 2015-08-20
CN106029639B (zh) 2019-01-08
SG11201606812WA (en) 2016-09-29
US20170066741A1 (en) 2017-03-09
IL246875A0 (en) 2016-08-31
PH12016501600A1 (en) 2017-02-06
JP2017506237A (ja) 2017-03-02
WO2015124576A1 (en) 2015-08-27

Similar Documents

Publication Publication Date Title
EA031132B1 (ru) 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера
EP3218362B1 (en) 2-amino-3,5-difluoro-3,6-dimethyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors for treating alzheimer's disease
JP6629320B2 (ja) Ｂａｃｅ１阻害剤としての２−アミノ−６−（ジフルオロメチル）−５，５−ジフルオロ−６−フェニル−３，４，５，６−テトラヒドロピリジン
US10058540B2 (en) 2-amino-5,5-difluoro-6-(fluoromethyl)-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors
AU2016305275A1 (en) 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors
US10004738B2 (en) Combination treatment comprising administration of 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahydropyridines
JP2018527338A (ja) ＢＡＣＥ１阻害剤としての２−アミノ−７ａ−フェニル−３，４，４ａ，５，７，７ａ−ヘキサヒドロフロ［３，４−ｂ］ピリジン
OA17882A (en) 2-Amino-3, 5, 5-Trifluoro-3, 4, 5, 6Tetrahydropyridines as Bace1 inhibitors for treatment of Alzheimer's disease.
OA18264A (en) 2-amino-3,5-difluoro-3,6-dimethyl-6-phenyl3,4,5,6-tetrahydropyridines as bacel inhibitors for treating Alzheimer's disease.
HK1242320B (en) 2-amino-3,5-difluoro-3,6-dimethyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors for treating alzheimer’s disease
HK1242320A1 (en) 2-amino-3,5-difluoro-3,6-dimethyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors for treating alzheimer’s disease

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU