PE20161225A1 - 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer - Google Patents

2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer

Info

Publication number
PE20161225A1
PE20161225A1 PE2016001299A PE2016001299A PE20161225A1 PE 20161225 A1 PE20161225 A1 PE 20161225A1 PE 2016001299 A PE2016001299 A PE 2016001299A PE 2016001299 A PE2016001299 A PE 2016001299A PE 20161225 A1 PE20161225 A1 PE 20161225A1
Authority
PE
Peru
Prior art keywords
trifluoro
amino
alzheimer
treatment
tetrahydropyridines
Prior art date
Application number
PE2016001299A
Other languages
English (en)
Spanish (es)
Inventor
Thomas Jensen
Lena Tagmose
Mauro Marigo
Karsten Juhl
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 PE20161225A1 publication Critical patent/PE20161225A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic 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
    • C07D211/72Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D227/00Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00
    • C07D227/02Heterocyclic 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
    • C07D227/06Heterocyclic 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
    • C07D227/10Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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)
PE2016001299A 2014-02-19 2015-02-17 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer PE20161225A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA201400086 2014-02-19
DKPA201400349 2014-07-01

Publications (1)

Publication Number Publication Date
PE20161225A1 true PE20161225A1 (es) 2016-12-04

Family

ID=59009438

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016001299A PE20161225A1 (es) 2014-02-19 2015-02-17 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer

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)

* Cited by examiner, † Cited by third party
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

Family Cites Families (19)

* Cited by examiner, † Cited by third party
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
GB0124928D0 (en) * 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
JP4472349B2 (ja) * 2002-02-12 2010-06-02 スミスクライン ビーチャム コーポレーション p38阻害薬として有用なニコチンアミド誘導体
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

Also Published As

Publication number Publication date
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
EA031132B1 (ru) 2018-11-30
GEP20186892B (en) 2018-09-10
JP6483146B2 (ja) 2019-03-13
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

Similar Documents

Publication Publication Date Title
PE20161225A1 (es) 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer
PE20170947A1 (es) 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1
EA201890594A1 (ru) Арильные, гетероарильные и гетероциклические соединения для лечения заболеваний
PE20181289A1 (es) 3-azabiciclo[3.1.0]hexanos sustituidos como inhibidores de cetohexoquinasa
PE20180024A1 (es) Triazolopirazinonas como inhibidores de pde1
PE20151542A1 (es) Compuestos de tetrahidropirrolotiazina
PE20181015A1 (es) 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
PE20180508A1 (es) Amidas heterociclicas como inhibidores de quinasa
PE20160843A1 (es) Pirrolidinonas herbicidas
PE20190711A1 (es) N-(fenils ulfonil) benzamidas y compuestos relacionados como inhibidores de bcl-2
EA201691428A1 (ru) Бициклические гетероциклические производные в качестве ингибиторов irak4
PE20170695A1 (es) Compuestos de indol carboxamida utiles como inhibidores de cinasas
PE20181074A1 (es) Compuestos heteroaromaticos como inhibidores de btk
MX379474B (es) Nuevos compuestos de 5-amino-6h-tiazolo[4,5-d]pirimidin-2,7-diona 3-sustituidos para el tratamiento y profilaxis de infecciones virales
JO3581B1 (ar) مركبات ميثيل-بيبيريدين جديدة مفيدة لتثبيط إنزيم سينثاز -1 بروستاجلاندين e2 ميكروسومي
MX374296B (es) Compuestos de pirazina novedosos para el tratamiento de enfermedades infecciosas
MX376106B (es) Nuevas piridazonas y triazinonas para el tratamiento y la profilaxis de infección por virus de hepatitis b.
PE20180021A1 (es) Derivados de sobetiroma
PE20170664A1 (es) Agonistas del receptor de apelina(apj) y usos de los mismos
PE20170946A1 (es) 2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
PY1218709A (es) Inhibidores sustituidos de acetil-coa carboxilasa
EA201691997A1 (ru) Производные 2,4-тиазолинидона в лечении расстройств центральной нервной системы
PE20170186A1 (es) Nuevos compuestos
AR089781A1 (es) Fluorometil-5,6-dihidro-4h-[1,3]oxazinas
PE20180355A1 (es) Desacetoxitubulisina h y analogos de esta

Legal Events

Date Code Title Description
FA Abandonment or withdrawal