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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (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)

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CA2628074C (en) 2005-10-25 2014-01-14 Shionogi & Co., Ltd. Aminodihydrothiazine derivative
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
JP5383484B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 環式基で置換されたアミノジヒドロチアジン誘導体
KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
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
EP2485920B1 (en) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. 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
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2485590B1 (en) 2009-10-08 2015-01-07 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.
JP5816630B2 (ja) 2010-10-29 2015-11-18 塩野義製薬株式会社 ナフチリジン誘導体
EP2634188A4 (en) 2010-10-29 2014-05-07 Shionogi & Co FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE
EP2694489B1 (en) 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2694521B1 (en) 2011-04-07 2015-11-25 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US8883779B2 (en) 2011-04-26 2014-11-11 Shinogi & Co., Ltd. Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them
CN103874496A (zh) 2011-08-22 2014-06-18 默沙东公司 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途
EP2854797A4 (en) 2012-05-30 2016-01-13 Comentis Inc chroman
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
WO2014134341A1 (en) 2013-03-01 2014-09-04 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
MX374512B (es) 2013-03-08 2025-03-06 Amgen Inc Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y métodos 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
EP3271355B1 (en) 2015-03-20 2020-07-29 H. Hoffnabb-La Roche Ag Bace1 inhibitors

Family Cites Families (18)

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MXPA04010952A (es) 2002-05-09 2005-01-25 Pharmacia Corp Compuestos de pirazolilo sustituidos para el tratamiento de la inflamacion.
SV2006002232A (es) * 2004-09-21 2006-05-25 Lilly Co Eli Inhibidores bace ref. x-16940
JP2009502786A (ja) * 2005-07-18 2009-01-29 メルク エンド カムパニー インコーポレーテッド アルツハイマー病を治療するためのスピロピペリジンβ−セクレターゼ阻害剤
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Also Published As

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

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