SG11201704520PA - 2-amino-5,5-difluoro-6-(fluoromethyl)-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors - Google Patents

2-amino-5,5-difluoro-6-(fluoromethyl)-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors

Info

Publication number
SG11201704520PA
SG11201704520PA SG11201704520PA SG11201704520PA SG11201704520PA SG 11201704520P A SG11201704520P A SG 11201704520PA SG 11201704520P A SG11201704520P A SG 11201704520PA SG 11201704520P A SG11201704520P A SG 11201704520PA SG 11201704520P A SG11201704520P A SG 11201704520PA
Authority
SG
Singapore
Prior art keywords
tetrahydropyridines
fluoromethyl
difluoro
phenyl
amino
Prior art date
Application number
SG11201704520PA
Inventor
Karsten Juhl
Lena Tagmose
Mauro Marigo
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 SG11201704520PA publication Critical patent/SG11201704520PA/en

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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
    • 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
    • A61K31/435—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
    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
SG11201704520PA 2014-11-10 2015-11-09 2-amino-5,5-difluoro-6-(fluoromethyl)-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors SG11201704520PA (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA201400647 2014-11-10
DKPA201500446 2015-08-07
PCT/EP2015/076017 WO2016075064A1 (en) 2014-11-10 2015-11-09 2-amino-5,5-difluoro-6-(fluoromethyl)-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors

Publications (1)

Publication Number Publication Date
SG11201704520PA true SG11201704520PA (en) 2017-07-28

Family

ID=59078291

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201704520PA SG11201704520PA (en) 2014-11-10 2015-11-09 2-amino-5,5-difluoro-6-(fluoromethyl)-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors

Country Status (16)

Country Link
US (1) US10058540B2 (en)
EP (1) EP3218364A1 (en)
JP (1) JP2017533251A (en)
KR (1) KR20170090433A (en)
CN (1) CN107074810A (en)
AU (1) AU2015345259A1 (en)
CA (1) CA2969486A1 (en)
CO (1) CO2017005588A2 (en)
CR (1) CR20170247A (en)
EA (1) EA201791030A1 (en)
EC (1) ECSP17035415A (en)
MA (1) MA40941A (en)
PH (1) PH12017501043A1 (en)
RU (1) RU2017120217A (en)
SG (1) SG11201704520PA (en)
WO (1) WO2016075064A1 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA40941A (en) 2014-11-10 2017-09-19 H Lundbeck As 2-AMINO-5,5-DIFLUORO-6- (FLUOROMETHYL) -6-PHENYL-3,4,5,6-TETRAHYDROPYRIDINES AS BACE1 INHIBITORS
CR20170187A (en) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors for the treatment of Alzheimer's disease
JO3458B1 (en) 2014-11-10 2020-07-05 H Lundbeck As 2-Amino-6-(difluoromethyl)- 5,5-difluoro-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors
JO3627B1 (en) 2015-04-30 2020-08-27 H Lundbeck As Imidazopyrazinones as PDE1 inhibitors
TW201717948A (en) 2015-08-10 2017-06-01 Ｈ 朗德貝克公司 Combination treatment comprising administration of 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahydropyridines
BR112017007472A2 (en) 2015-08-12 2018-01-23 H Lundbeck As 2-AMINO-3-FLUORO-3- (FLUORO METHIL) -6-METHYL-6-PHENYL 3,4,5,6-TETRA-HYDROPYRIDINES AS BACE INHIBITORS1
US10034861B2 (en) 2016-07-04 2018-07-31 H. Lundbeck A/S 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors
MX2019004859A (en) 2016-10-28 2019-06-20 H Lundbeck As Combination treatments comprising administration of imidazopyrazinones.
CA3041607A1 (en) 2016-10-28 2018-05-03 H. Lundbeck A/S Combination treatments comprising imidazopyrazinones for the treatment of psychiatric and/or cognitive disorders
WO2019115566A1 (en) 2017-12-14 2019-06-20 H. Lundbeck A/S Combination treatments comprising administration of 1h-pyrazolo[4,3-b]pyridines
AR113926A1 (en) 2017-12-14 2020-07-01 H Lundbeck As DERIVATIVES OF 1H-PYRAZOLE [4,3-B] PYRIDINES
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

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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
PT1474395E (en) 2002-02-12 2008-01-02 Smithkline Beecham Corp Nicotinamide derivates useful as p38 inhibitors
AR077277A1 (en) 2009-07-09 2011-08-17 Lilly Co Eli BICYCLE COMPOUNDS (1,3) TIAZIN-2-AMINA PHARMACEUTICAL FORMULATION THAT INCLUDES IT AND ITS USE FOR THE MANUFACTURE OF A USEFUL MEDICINAL PRODUCT FOR THE TREATMENT OF ALZHEIMER'S DISEASE
NZ603427A (en) * 2010-06-09 2013-08-30 Janssen Pharmaceutica Nv 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
BR112013017779A2 (en) 2011-01-12 2016-10-11 Novartis Ag oxazine derivatives and their use in the treatment of neurological disorders
HUE029226T2 (en) 2011-01-13 2017-02-28 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
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 (en) * 2011-06-07 2016-05-31 Ф.Хоффманн-Ля Рош Аг Halogen-alkyl-1,3 oxazines as bace1 and/or bace2 inhibitors
UY34278A (en) 2011-08-25 2013-04-05 Novartis Ag NEW NOXEDINE DERIVATIVES OF OXAZINE AND ITS USE IN THE TREATMENT OF DISEASES
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
JP2016501827A (en) 2012-10-24 2016-01-21 塩野義製薬株式会社 Dihydrooxazine or oxazepine derivative having BACE1 inhibitory action
TW201446758A (en) 2013-03-01 2014-12-16 Amgen Inc Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
JO3318B1 (en) 2013-06-18 2019-03-13 Lilly Co Eli Bace inhibitors
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TW201623295A (en) 2014-04-11 2016-07-01 塩野義製藥股份有限公司 Dihydrothiazine and dihydrooxazine derivatives having BACE1 inhibitory activity
CR20170187A (en) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors for the treatment of Alzheimer's disease
MA40941A (en) 2014-11-10 2017-09-19 H Lundbeck As 2-AMINO-5,5-DIFLUORO-6- (FLUOROMETHYL) -6-PHENYL-3,4,5,6-TETRAHYDROPYRIDINES AS BACE1 INHIBITORS
JO3458B1 (en) 2014-11-10 2020-07-05 H Lundbeck As 2-Amino-6-(difluoromethyl)- 5,5-difluoro-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors
TW201717948A (en) 2015-08-10 2017-06-01 Ｈ 朗德貝克公司 Combination treatment comprising administration of 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahydropyridines
BR112017007472A2 (en) 2015-08-12 2018-01-23 H Lundbeck As 2-AMINO-3-FLUORO-3- (FLUORO METHIL) -6-METHYL-6-PHENYL 3,4,5,6-TETRA-HYDROPYRIDINES AS BACE INHIBITORS1

Also Published As

Publication number Publication date
CN107074810A (en) 2017-08-18
ECSP17035415A (en) 2017-08-31
EA201791030A1 (en) 2017-11-30
US10058540B2 (en) 2018-08-28
MA40941A (en) 2017-09-19
CO2017005588A2 (en) 2017-10-20
KR20170090433A (en) 2017-08-07
EP3218364A1 (en) 2017-09-20
US20170340618A1 (en) 2017-11-30
PH12017501043A1 (en) 2017-11-27
CA2969486A1 (en) 2016-05-19
AU2015345259A1 (en) 2017-06-29
WO2016075064A1 (en) 2016-05-19
RU2017120217A (en) 2018-12-13
CR20170247A (en) 2017-08-18
JP2017533251A (en) 2017-11-09

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