AP2016009370A0 - 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease - Google Patents

2-amino-3,5,5-trifluoro-3,4,5,6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease

Info

Publication number
AP2016009370A0
AP2016009370A0 AP2016009370A AP2016009370A AP2016009370A0 AP 2016009370 A0 AP2016009370 A0 AP 2016009370A0 AP 2016009370 A AP2016009370 A AP 2016009370A AP 2016009370 A AP2016009370 A AP 2016009370A AP 2016009370 A0 AP2016009370 A0 AP 2016009370A0
Authority
AP
ARIPO
Prior art keywords
tetrahydropyridines
trifluoro
alzheimer
disease
amino
Prior art date
Application number
AP2016009370A
Other languages
English (en)
Inventor
Karsten Juhl
Mauro Marigo
Lena Tagmose
Thomas Jensen
Original Assignee
H Lundbeck As
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 H Lundbeck As filed Critical H Lundbeck As
Publication of AP2016009370A0 publication Critical patent/AP2016009370A0/en

Links

Classifications

    • 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
    • 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
    • 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)
AP2016009370A 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 AP2016009370A0 (en)

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 (1)

Publication Number Publication Date
AP2016009370A0 true AP2016009370A0 (en) 2016-08-31

Family

ID=59009438

Family Applications (1)

Application Number Title Priority Date Filing Date
AP2016009370A AP2016009370A0 (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

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) 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 (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170066741A1 (en) 2014-02-19 2017-03-09 H. Lundbeck A/S 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
RU2018104868A (ru) * 2015-08-12 2019-09-13 Х. Лундбекк А/С 2-амино-3-фтор-3-(фторметил)-6-метил-6-фенил-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1
EP3347486A4 (en) 2015-09-09 2019-06-19 The Trustees of Columbia University in the City of New York REDUCTION OF ER-MAM-LOCALIZED APP-C99 AND METHOD FOR THE TREATMENT OF ALZHEIMER 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
LT3532064T (lt) 2016-10-28 2020-09-25 H. Lundbeck A/S Kompleksiniai gydymai, apimantys imidazopirazonus, skirti psichiatrinių ir (arba) kognityvinių sutrikimų gydymui
RU2019108717A (ru) 2016-10-28 2020-11-30 Х. Лундбекк А/С Комбинированные средства для лечения, предусматривающего введение имидазопиразинонов
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
ES2927715T3 (es) 2017-10-05 2022-11-10 Fulcrum Therapeutics Inc Inhibidores de la quinasa p38 reducen la expresión de dux4 y de los genes que le siguen para el tratamiento de la FSHD
RU2020118913A (ru) 2017-12-14 2022-01-14 Х. Лундбекк А/С (H. Lundbeck A/S) Виды комбинированного лечения, предусматривающего введение 1h-пиразолo[4,3-b]пиридинов
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
US11535611B2 (en) 2017-12-20 2022-12-27 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

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1395257A1 (en) * 2001-06-12 2004-03-10 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
CN100369898C (zh) * 2002-02-12 2008-02-20 史密丝克莱恩比彻姆公司 用作p38抑制剂的烟酰胺衍生物
TWI431004B (zh) * 2008-05-02 2014-03-21 Lilly Co Eli Bace抑制劑
AR081587A1 (es) 2010-06-09 2012-10-03 Janssen Pharmaceutica Nv DERIVADOS DE 5,6-DIHIDRO-2H-[1,4]OXAZIN-3-IL-AMINA UTILES COMO INHIBIDORES DE LA b-SECRETASA (BACE)
CA2816285A1 (en) * 2010-10-29 2012-05-03 Shionogi & Co., Ltd. Naphthyridine derivative
CN103429589A (zh) * 2011-01-12 2013-12-04 诺瓦提斯公司 噁嗪衍生物及其在治疗神经障碍中的用途
KR101569260B1 (ko) * 2011-01-13 2015-11-13 노파르티스 아게 신규 헤테로시클릭 유도체 및 신경계 장애의 치료에서의 그의 용도
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
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
US9493485B2 (en) 2012-03-20 2016-11-15 Imago 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
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
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
US20170066741A1 (en) 2014-02-19 2017-03-09 H. Lundbeck A/S 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

Also Published As

Publication number Publication date
JP6483146B2 (ja) 2019-03-13
CA2940028A1 (en) 2015-08-27
CN106029639B (zh) 2019-01-08
PH12016501600A1 (en) 2017-02-06
EA031132B1 (ru) 2018-11-30
EA201691447A1 (ru) 2016-12-30
CR20160352A (es) 2016-10-20
JP2017506237A (ja) 2017-03-02
ECSP16072941A (es) 2017-02-24
AU2015220873A1 (en) 2016-08-11
GEAP201814248A (en) 2018-04-10
EP3107897A1 (en) 2016-12-28
MX2016010777A (es) 2016-10-26
US20150232449A1 (en) 2015-08-20
GEP20186892B (en) 2018-09-10
RU2016133626A (ru) 2018-03-20
AR099489A1 (es) 2016-07-27
RU2016133626A3 (enExample) 2018-09-25
SG11201606812WA (en) 2016-09-29
US20170066741A1 (en) 2017-03-09
TW201609700A (zh) 2016-03-16
KR20160115936A (ko) 2016-10-06
CL2016002072A1 (es) 2017-01-20
PE20161225A1 (es) 2016-12-04
DOP2016000194A (es) 2016-09-30
US9353084B2 (en) 2016-05-31
IL246875A0 (en) 2016-08-31
CN106029639A (zh) 2016-10-12
MA39225A1 (fr) 2017-04-28
WO2015124576A1 (en) 2015-08-27
UA117695C2 (uk) 2018-09-10

Similar Documents

Publication Publication Date Title
IL246875A0 (en) 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahydropyridines as bace1 inhibitors for the treatment of Alzheimer's disease
ZA201702799B (en) 2-amino-3,5-difluoro-3,6-dimethyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors for treating alzheimer's disease
IL264049A (en) Compounds, preparations and methods for treating the disease
IL264156A (en) Compounds, preparations and methods for treating the disease
IL247085A0 (en) Methods for treating Alzheimer's disease
IL252433B (en) Methods for treating Alzheimer's disease
IL248732A0 (en) Compounds for the treatment of ophthalmological diseases and disorders
LT3224269T (lt) Kompozicijos ir būdai, skirti cns sutrikimams gydyti
ZA201605341B (en) Methods of treating alzheimer's disease
ZA201702797B (en) 2-amino-6-(difluoromethyl)- 5,5-difluoro-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors
SMT202100082T1 (it) Composti eteroarilici per il trattamento di malattie oftalmiche
EP3169405A4 (en) Methods, compounds, and compositions for the treatment of musculoskeletal diseases
IL257072A (en) Combination treatment comprising administration of 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahydropyridines
HUE070257T2 (hu) Vegyületek a lipofuscinhoz kapcsolódó betegségek kezelésére
IL252543B (en) Compounds for the treatment of degenerative retinal tissues
IL248428A0 (en) Use of 3,1-propanedisulfonic acid or pharmaceutically acceptable saline to treat sarcoidosis
EP3244897A4 (en) Methods for treating alzheimer's disease
LT3119752T (lt) 3,4-diamino-6-chlorpirazin-2-karboksamido junginiai, skirti enac sąlygotų ligų gydymui
SG11201703330YA (en) Iminosugars useful for the treatment of viral diseases
HK1227027A1 (en) 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer’s disease
GB201511453D0 (en) Treatment of alzheimer's disease