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ECSP13013048A - Spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas como inhibidores - Google Patents

Spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas como inhibidores

Info

Publication number
ECSP13013048A
ECSP13013048A ECSP13013048A ECSP13013048A EC SP13013048 A ECSP13013048 A EC SP13013048A EC SP13013048 A ECSP13013048 A EC SP13013048A EC SP13013048 A ECSP13013048 A EC SP13013048A
Authority
EC
Ecuador
Prior art keywords
spiro
oxacepins
oxacines
inhibitors
present
Prior art date
Application number
Other languages
English (en)
Inventor
Robert Narquizian
Emmanuel Pinard
Wolfgang Wostl
Original Assignee
Hoffmann La Roche
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46177417&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ECSP13013048(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of ECSP13013048A publication Critical patent/ECSP13013048A/es

Links

Classifications

    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/537—Heterocyclic 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 spiro-condensed or forming part of bridged ring systems
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/18—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 2
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invención proporciona spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas de fórmula I:que presentan actividad inhibidora de BACE1 y/o de BACE2, su preparación, composiciones farmacéuticas que las contienen y su utilización como sustancias terapéuticamente activas. Los compuestos activos de la presente invención resultan útiles en el tratamiento terapéutico y/o profiláctico de, por ejemplo, la enfermedad de Alzheimer y de la diabetes de tipo 2.
ECSP13013048 2011-05-27 2013-11-25 Spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas como inhibidores ECSP13013048A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11167835 2011-05-27

Publications (1)

Publication Number Publication Date
ECSP13013048A true ECSP13013048A (es) 2014-01-31

Family

ID=46177417

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP13013048 ECSP13013048A (es) 2011-05-27 2013-11-25 Spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas como inhibidores

Country Status (23)

Country Link
US (1) US9079919B2 (es)
EP (1) EP2714697B1 (es)
JP (1) JP2014515382A (es)
KR (1) KR20140048137A (es)
CN (1) CN103596961B (es)
AU (1) AU2012264875B2 (es)
BR (1) BR112013030281A2 (es)
CA (1) CA2833813A1 (es)
CL (1) CL2013003372A1 (es)
CO (1) CO6801773A2 (es)
CR (1) CR20130580A (es)
EA (1) EA024286B1 (es)
EC (1) ECSP13013048A (es)
ES (1) ES2600636T3 (es)
IL (1) IL229334A (es)
MA (1) MA35191B1 (es)
MX (1) MX2013013910A (es)
PE (1) PE20141205A1 (es)
PH (1) PH12013502262A1 (es)
SG (1) SG194835A1 (es)
UA (1) UA111847C2 (es)
WO (1) WO2012163790A1 (es)
ZA (1) ZA201308395B (es)

Families Citing this family (25)

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EP1942105B8 (en) 2005-10-25 2014-08-13 Shionogi&Co., Ltd. Aminodihydrothiazine derivative
JP5383483B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 アルツハイマー症治療用医薬組成物
RU2476430C2 (ru) 2007-04-24 2013-02-27 Сионоги Энд Ко., Лтд. Производные аминодигидротиазина, замещенные циклической группой
US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
CN102186841A (zh) 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
EP2485591B1 (en) 2009-10-08 2016-03-23 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US8557826B2 (en) 2009-10-08 2013-10-15 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use
MX2012006491A (es) 2009-12-11 2012-07-03 Shionogi & Co Derivados de oxazina.
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
CN103261199A (zh) 2010-10-29 2013-08-21 盐野义制药株式会社 萘啶衍生物
US9145426B2 (en) 2011-04-07 2015-09-29 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
US9221839B2 (en) 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
JP2014524472A (ja) 2011-08-22 2014-09-22 メルク・シャープ・アンド・ドーム・コーポレーション Ｂａｃｅ阻害剤としての２−スピロ置換イミノチアジンならびにそのモノオキシドおよびジオキシド、組成物、ならびにそれらの使用
MX2014014066A (es) 2012-05-30 2015-03-19 Comentis Inc Compuestos de cromano.
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
WO2014099788A1 (en) 2012-12-21 2014-06-26 Merck Sharp & Dohme Corp. C5-spiro iminothiadiazine dioxides as bace inhibitors
US9296734B2 (en) 2013-03-01 2016-03-29 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
PE20151794A1 (es) 2013-03-08 2015-12-03 Amgen Inc Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y metodos de uso
WO2015038446A1 (en) 2013-09-13 2015-03-19 Merck Sharp & Dohme Corp. C5-spiro iminothiazine dioxides as bace inhibitors, compositions, and their use
CN106795147B (zh) 2014-08-08 2020-09-22 美国安进公司 作为β-分泌酶抑制剂的环丙基稠合噻嗪-2-胺化合物和使用方法
WO2016055858A1 (en) * 2014-10-07 2016-04-14 Astrazeneca Ab Compounds and their use as bace inhibitors
CA2979113A1 (en) 2015-03-20 2016-09-29 F. Hoffmann-La Roche Ag Bace1 inhibitors

Family Cites Families (18)

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Publication number Priority date Publication date Assignee Title
EP1501805A1 (en) 2002-05-09 2005-02-02 Pharmacia Corporation Substituted pyrazolyl compounds for the treatment of inflammation
TW200624426A (en) * 2004-09-21 2006-07-16 Lilly Co Eli BACE inhibitors
ATE550338T1 (de) * 2005-07-18 2012-04-15 Merck Sharp & Dohme Spiropiperidininhibitoren von beta-secretase zur behandlung von alzheimer-krankheit
EP1942105B8 (en) * 2005-10-25 2014-08-13 Shionogi&Co., Ltd. Aminodihydrothiazine derivative
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UA103272C2 (uk) * 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2
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Also Published As

Publication number Publication date
KR20140048137A (ko) 2014-04-23
WO2012163790A1 (en) 2012-12-06
JP2014515382A (ja) 2014-06-30
ES2600636T3 (es) 2017-02-10
MA35191B1 (fr) 2014-06-02
IL229334A (en) 2017-02-28
IL229334A0 (en) 2014-01-30
EA201391752A1 (ru) 2014-04-30
CA2833813A1 (en) 2012-12-06
AU2012264875B2 (en) 2017-04-27
EA024286B1 (ru) 2016-09-30
UA111847C2 (uk) 2016-06-24
MX2013013910A (es) 2014-01-24
CO6801773A2 (es) 2013-11-29
US9079919B2 (en) 2015-07-14
PH12013502262A1 (en) 2016-01-22
CL2013003372A1 (es) 2014-07-25
CR20130580A (es) 2013-12-09
US20120302549A1 (en) 2012-11-29
ZA201308395B (en) 2014-07-30
EP2714697A1 (en) 2014-04-09
NZ616817A (en) 2015-12-24
AU2012264875A1 (en) 2013-10-31
PE20141205A1 (es) 2014-09-22
CN103596961A (zh) 2014-02-19
SG194835A1 (en) 2013-12-30
BR112013030281A2 (pt) 2016-11-29
CN103596961B (zh) 2016-09-28
EP2714697B1 (en) 2016-08-31

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