EA035026B1 - Производные 2,3,4,5-тетрагидропиридин-6-амина - Google Patents

Производные 2,3,4,5-тетрагидропиридин-6-амина Download PDF

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Publication number
EA035026B1
EA035026B1 EA201890769A EA201890769A EA035026B1 EA 035026 B1 EA035026 B1 EA 035026B1 EA 201890769 A EA201890769 A EA 201890769A EA 201890769 A EA201890769 A EA 201890769A EA 035026 B1 EA035026 B1 EA 035026B1
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EA
Eurasian Patent Office
Prior art keywords
compound
dementia
mmol
added
alkyl
Prior art date
Application number
EA201890769A
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English (en)
Russian (ru)
Other versions
EA201890769A1 (ru
Inventor
Фредерик Ян Рита Ромбаутс
Хенрикус Якобус Мария Гейсен
Свен Францискус Анна Ван Брандт
Андрес Авелино Трабанко-Суарес
Original Assignee
Янссен Фармацевтика Н.В.
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.)
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Application filed by Янссен Фармацевтика Н.В. filed Critical Янссен Фармацевтика Н.В.
Publication of EA201890769A1 publication Critical patent/EA201890769A1/ru
Publication of EA035026B1 publication Critical patent/EA035026B1/ru

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    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84Nitriles
    • C07D213/85Nitriles in position 3

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
EA201890769A 2015-09-23 2016-09-23 Производные 2,3,4,5-тетрагидропиридин-6-амина EA035026B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP15186394 2015-09-23
EP16172005 2016-05-30
PCT/EP2016/072710 WO2017050978A1 (en) 2015-09-23 2016-09-23 2,3,4,5-tetrahydropyridin-6-amine derivatives

Publications (2)

Publication Number Publication Date
EA201890769A1 EA201890769A1 (ru) 2018-09-28
EA035026B1 true EA035026B1 (ru) 2020-04-20

Family

ID=56985626

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201890769A EA035026B1 (ru) 2015-09-23 2016-09-23 Производные 2,3,4,5-тетрагидропиридин-6-амина

Country Status (14)

Country Link
US (1) US20180334447A1 (https=)
EP (1) EP3353163B1 (https=)
JP (1) JP2018527387A (https=)
KR (1) KR20180053357A (https=)
CN (1) CN108026069A (https=)
AU (1) AU2016328589A1 (https=)
BR (1) BR112018005591A2 (https=)
CA (1) CA2995161A1 (https=)
EA (1) EA035026B1 (https=)
HK (1) HK1254800A1 (https=)
IL (1) IL258217A (https=)
MX (1) MX2018003565A (https=)
TW (1) TW201726651A (https=)
WO (1) WO2017050978A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019208509A1 (en) * 2018-04-23 2019-10-31 Shionogi & Co., Ltd. Bicyclic heterocycle derivatives having selective bace1 inhibitory activity
TW202014191A (zh) 2018-04-27 2020-04-16 日商鹽野義製藥股份有限公司 具有選擇性bace1抑制活性的四氫哌喃并衍生物
CN114380736B (zh) * 2020-10-21 2023-10-03 复旦大学 一种2,3,4,5-四氢吡啶类化合物的合成方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011009943A1 (en) * 2009-07-24 2011-01-27 Novartis Ag Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders
WO2014059185A1 (en) * 2012-10-12 2014-04-17 Amgen Inc. Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
WO2015124576A1 (en) * 2014-02-19 2015-08-27 H. Lundbeck A/S 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120258961A1 (en) * 2009-12-24 2012-10-11 Shionogi & Co., Ltd. 4-amino-1,3-thiazine or oxazine derivative
US8673894B2 (en) 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds
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
JP5766198B2 (ja) 2010-10-29 2015-08-19 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
US8815841B2 (en) 2011-02-18 2014-08-26 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
US8785436B2 (en) 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
CA2902212C (en) 2013-03-01 2020-10-13 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011009943A1 (en) * 2009-07-24 2011-01-27 Novartis Ag Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders
WO2014059185A1 (en) * 2012-10-12 2014-04-17 Amgen Inc. Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
WO2015124576A1 (en) * 2014-02-19 2015-08-27 H. Lundbeck A/S 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease

Also Published As

Publication number Publication date
EP3353163A1 (en) 2018-08-01
TW201726651A (zh) 2017-08-01
WO2017050978A1 (en) 2017-03-30
EP3353163B1 (en) 2020-02-05
BR112018005591A2 (pt) 2018-10-09
HK1254800A1 (zh) 2019-07-26
CA2995161A1 (en) 2017-03-30
AU2016328589A1 (en) 2018-03-01
US20180334447A1 (en) 2018-11-22
JP2018527387A (ja) 2018-09-20
EA201890769A1 (ru) 2018-09-28
MX2018003565A (es) 2018-06-18
CN108026069A (zh) 2018-05-11
IL258217A (en) 2018-05-31
KR20180053357A (ko) 2018-05-21

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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