EA201490491A1 - Производные 2-амино-4-(пиридин-2-ил)-5,6-дигидро-4h-1,3-оксазинов и их использование в качестве ингибиторов bace-1 и/или bace-2 - Google Patents

Производные 2-амино-4-(пиридин-2-ил)-5,6-дигидро-4h-1,3-оксазинов и их использование в качестве ингибиторов bace-1 и/или bace-2

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Publication number
EA201490491A1
EA201490491A1 EA201490491A EA201490491A EA201490491A1 EA 201490491 A1 EA201490491 A1 EA 201490491A1 EA 201490491 A EA201490491 A EA 201490491A EA 201490491 A EA201490491 A EA 201490491A EA 201490491 A1 EA201490491 A1 EA 201490491A1
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Eurasian Patent Office
Prior art keywords
bace
derivatives
oxazines
pyridin
dihydro
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EA201490491A
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English (en)
Other versions
EA024580B1 (ru
Inventor
Райнер Мартин Люенд
Райнер Махауэр
Хайнрих Рюэгер
Сим Якоб Венстра
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Новартис Аг
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Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201490491A1 publication Critical patent/EA201490491A1/ru
Publication of EA024580B1 publication Critical patent/EA024580B1/ru

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    • 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
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Настоящее изобретение относится к новым производным оксазина формулы (I) и к их фармацевтически приемлемым солям, в которых все переменные определены в описании, к их фармацевтическим композициям, к их комбинациям и к их использованию в качестве лекарственных средств, особенно для лечения болезни Альцгеймера или диабета за счет ингибирования ВАСЕ-1 или ВАСЕ-2.
EA201490491A 2011-08-25 2012-08-23 Производные 2-амино-4-(пиридин-2-ил)-5,6-дигидро-4h-1,3-оксазинов и их использование в качестве ингибиторов bace-1 и/или bace-2 EA024580B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161527172P 2011-08-25 2011-08-25
US201261665395P 2012-06-28 2012-06-28
PCT/IB2012/054269 WO2013027188A1 (en) 2011-08-25 2012-08-23 2 -amino-4 - (pyridin- 2 -yl) - 5, 6 -dihydro-4h- 1, 3 -oxazine derivatives and their use as bace-1 and/or bace - 2 inhibitors

Publications (2)

Publication Number Publication Date
EA201490491A1 true EA201490491A1 (ru) 2014-06-30
EA024580B1 EA024580B1 (ru) 2016-09-30

Family

ID=47018309

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201490491A EA024580B1 (ru) 2011-08-25 2012-08-23 Производные 2-амино-4-(пиридин-2-ил)-5,6-дигидро-4h-1,3-оксазинов и их использование в качестве ингибиторов bace-1 и/или bace-2

Country Status (28)

Country Link
US (2) US9163011B2 (ru)
EP (2) EP3023423B1 (ru)
JP (1) JP5816369B2 (ru)
KR (1) KR101601571B1 (ru)
CN (1) CN103906748B (ru)
AP (1) AP2014007507A0 (ru)
AR (1) AR087668A1 (ru)
AU (1) AU2012298177B2 (ru)
BR (1) BR112014004131A2 (ru)
CA (1) CA2845093A1 (ru)
CL (1) CL2014000458A1 (ru)
CO (1) CO6890097A2 (ru)
CR (1) CR20140084A (ru)
EA (1) EA024580B1 (ru)
ES (2) ES2638832T3 (ru)
GT (1) GT201400031A (ru)
HK (1) HK1195903A1 (ru)
IL (1) IL230975A0 (ru)
MA (1) MA35356B1 (ru)
MX (1) MX339303B (ru)
PE (1) PE20141540A1 (ru)
PL (1) PL2748162T3 (ru)
SG (1) SG2014012108A (ru)
TN (1) TN2014000062A1 (ru)
TW (1) TW201313706A (ru)
UY (1) UY34278A (ru)
WO (1) WO2013027188A1 (ru)
ZA (1) ZA201401139B (ru)

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MX2019007104A (es) 2016-12-15 2019-11-05 Amgen Inc Derivados de dioxido de 1,4-tiazina y dioxido de 1,2,4-tiadiazina como inhibidores de beta-secretasa y metodos de uso.
JP7149272B2 (ja) 2016-12-15 2022-10-06 アムジエン・インコーポレーテツド β-セクレターゼ阻害剤としてのチアジン誘導体および使用方法
JP7159161B2 (ja) 2016-12-15 2022-10-24 アムジエン・インコーポレーテツド β-セクレターゼ阻害剤としてのシクロプロピル縮合チアジン誘導体および使用方法
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Publication number Publication date
CL2014000458A1 (es) 2014-09-05
CO6890097A2 (es) 2014-03-10
CN103906748A (zh) 2014-07-02
AU2012298177B2 (en) 2015-10-29
US20130172331A1 (en) 2013-07-04
BR112014004131A2 (pt) 2017-06-13
TN2014000062A1 (en) 2015-07-01
AU2012298177A1 (en) 2014-03-06
JP2014524463A (ja) 2014-09-22
NZ621093A (en) 2015-05-29
MA35356B1 (fr) 2014-08-01
JP5816369B2 (ja) 2015-11-18
TW201313706A (zh) 2013-04-01
CR20140084A (es) 2014-05-02
EA024580B1 (ru) 2016-09-30
CA2845093A1 (en) 2013-02-28
AR087668A1 (es) 2014-04-09
PE20141540A1 (es) 2014-10-31
SG2014012108A (en) 2014-05-29
ES2638832T3 (es) 2017-10-24
PL2748162T3 (pl) 2016-06-30
EP2748162A1 (en) 2014-07-02
US9163011B2 (en) 2015-10-20
US20150150877A1 (en) 2015-06-04
IL230975A0 (en) 2014-03-31
ZA201401139B (en) 2014-12-23
ES2565229T3 (es) 2016-04-01
EP3023423A1 (en) 2016-05-25
AP2014007507A0 (en) 2014-03-31
WO2013027188A1 (en) 2013-02-28
CN103906748B (zh) 2017-06-16
MX339303B (es) 2016-05-19
EP3023423B1 (en) 2017-05-31
KR20140054313A (ko) 2014-05-08
KR101601571B1 (ko) 2016-03-08
GT201400031A (es) 2015-02-19
HK1195903A1 (en) 2014-11-28
UY34278A (es) 2013-04-05
MX2014002230A (es) 2014-04-25
EP2748162B1 (en) 2015-12-16

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