BR112013016360A2 - 1,4 oxazinas como inibidores de bace1 e/ou bace2 - Google Patents

1,4 oxazinas como inibidores de bace1 e/ou bace2

Info

Publication number
BR112013016360A2
BR112013016360A2 BR112013016360A BR112013016360A BR112013016360A2 BR 112013016360 A2 BR112013016360 A2 BR 112013016360A2 BR 112013016360 A BR112013016360 A BR 112013016360A BR 112013016360 A BR112013016360 A BR 112013016360A BR 112013016360 A2 BR112013016360 A2 BR 112013016360A2
Authority
BR
Brazil
Prior art keywords
bace2
bace1
oxazines
inhibitors
Prior art date
Application number
BR112013016360A
Other languages
English (en)
Portuguese (pt)
Inventor
V Mayweg Alexander
Gabellieri Emanuele
Power Eoin
Hilpert Hans
Mauser Harald
Travagli Massimiliano
Andreini Matteo
Narquizian Robert
Woltering Thomas
Guba Wolfgang
Wostl Wolfgang
Original Assignee
Hoffmann La Roche
Siena Biotech Spa
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 Hoffmann La Roche, Siena Biotech Spa filed Critical Hoffmann La Roche
Publication of BR112013016360A2 publication Critical patent/BR112013016360A2/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
BR112013016360A 2011-01-18 2012-01-16 1,4 oxazinas como inibidores de bace1 e/ou bace2 BR112013016360A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11151294 2011-01-18
PCT/EP2012/050537 WO2012098064A1 (en) 2011-01-18 2012-01-16 1,4 oxazines as bace1 and/or bace2 inhibitors

Publications (1)

Publication Number Publication Date
BR112013016360A2 true BR112013016360A2 (pt) 2018-06-26

Family

ID=45491607

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112013016360A BR112013016360A2 (pt) 2011-01-18 2012-01-16 1,4 oxazinas como inibidores de bace1 e/ou bace2

Country Status (10)

Country Link
US (1) US9242943B2 (https=)
EP (1) EP2665713A1 (https=)
JP (1) JP2014502982A (https=)
KR (1) KR20140014133A (https=)
CN (1) CN103328454A (https=)
BR (1) BR112013016360A2 (https=)
CA (1) CA2819158A1 (https=)
MX (1) MX2013007558A (https=)
RU (1) RU2013135678A (https=)
WO (1) WO2012098064A1 (https=)

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RU2416603C9 (ru) 2005-10-25 2012-06-20 Сионоги Энд Ко., Лтд. Производные аминодигидротиазина
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
EP2147914B1 (en) 2007-04-24 2014-06-04 Shionogi&Co., Ltd. Aminodihydrothiazine derivatives substituted with cyclic groups
WO2009151098A1 (ja) 2008-06-13 2009-12-17 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
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
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
EP2485590B1 (en) 2009-10-08 2015-01-07 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2485920B1 (en) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
TWI488852B (zh) 2009-12-11 2015-06-21 Shionogi & Co 衍生物
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
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
SG191097A1 (en) 2010-12-22 2013-08-30 Janssen Pharmaceutica Nv 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
JP5853033B2 (ja) 2011-03-01 2016-02-09 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap β−セクレターゼ(BACE)の阻害剤として有用な6,7−ジヒドロ−ピラゾロ[1,5−a]ピラジン−4−イルアミン誘導体
EP2683721B1 (en) 2011-03-09 2015-01-28 Janssen Pharmaceutica N.V. 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
EP2694521B1 (en) 2011-04-07 2015-11-25 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
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
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
RU2014111055A (ru) 2011-08-22 2015-09-27 Мерк Шарп И Доум Корп. 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение
CA2851445A1 (en) * 2011-10-13 2013-04-18 Novartis Ag Novel oxazine derivatives and their use in the treatment of disease
ES2582473T3 (es) * 2011-12-06 2016-09-13 Janssen Pharmaceutica, N.V. Derivados de 5-(3-aminofenil)-5-alquil-5,6-dihidro-2H-[1,4]oxazin-3-amina para el tratamiento de trastornos en que está implicada la beta-secretasa
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
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
CA2912156C (en) 2013-06-12 2021-07-20 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)
KR102243134B1 (ko) 2013-06-12 2021-04-22 얀센 파마슈티카 엔.브이. 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진 유도체
WO2014198854A1 (en) 2013-06-12 2014-12-18 Janssen Pharmaceutica Nv 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)
MX2017008083A (es) 2014-12-18 2017-10-31 Janssen Pharmaceutica Nv Compuestos 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2h-pirrol-5-amina inhibidores de beta-secretasa.
CR20170426A (es) 2015-03-20 2017-10-23 Hoffmann La Roche Inhibidores de bace 1

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WO2009024615A1 (en) * 2007-08-23 2009-02-26 Novartis Ag Aminobenzyl-substituted cyclic sulfones useful as bace inhibitors
WO2009151098A1 (ja) 2008-06-13 2009-12-17 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
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US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
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
US8748418B2 (en) * 2011-03-18 2014-06-10 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

Also Published As

Publication number Publication date
US9242943B2 (en) 2016-01-26
US20120184540A1 (en) 2012-07-19
JP2014502982A (ja) 2014-02-06
CA2819158A1 (en) 2012-07-26
EP2665713A1 (en) 2013-11-27
CN103328454A (zh) 2013-09-25
RU2013135678A (ru) 2015-02-27
WO2012098064A1 (en) 2012-07-26
KR20140014133A (ko) 2014-02-05
MX2013007558A (es) 2013-08-21

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B08F Application fees: application dismissed [chapter 8.6 patent gazette]
B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2478 DE 03-07-2018 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.

B350 Update of information on the portal [chapter 15.35 patent gazette]