BR112013017757A2 - derivado de oxazina cristalino e seu uso como inibidor de bace - Google Patents

derivado de oxazina cristalino e seu uso como inibidor de bace

Info

Publication number
BR112013017757A2
BR112013017757A2 BR112013017757A BR112013017757A BR112013017757A2 BR 112013017757 A2 BR112013017757 A2 BR 112013017757A2 BR 112013017757 A BR112013017757 A BR 112013017757A BR 112013017757 A BR112013017757 A BR 112013017757A BR 112013017757 A2 BR112013017757 A2 BR 112013017757A2
Authority
BR
Brazil
Prior art keywords
crystalline
bace inhibitor
oxazine derivative
crystalline form
oxazine
Prior art date
Application number
BR112013017757A
Other languages
English (en)
Inventor
Rita Ramos
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of BR112013017757A2 publication Critical patent/BR112013017757A2/pt

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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

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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

derivado de oxazina cristalino e seu uso como inibidor de bace a presente invenção refere-se a [3-((3r, 6r)-5-amino-3, 6-dimetil-6-trifluormetil-3, 6-di-hidro-2h-[1, 4]oxazin-3-il)-4-fluor-fenil]-amida do ácido 5-ciano-3-metil-piridino-2-carboxílico em forma cristalina, à sua preparação, seu uso médico e a medicamentos compreendendo o dito composto em forma cristalina para uso no tratamento de doença de alzheimer.
BR112013017757A 2011-01-12 2012-01-11 derivado de oxazina cristalino e seu uso como inibidor de bace BR112013017757A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161432058P 2011-01-12 2011-01-12
US201161435088P 2011-01-21 2011-01-21
PCT/EP2012/050367 WO2012095451A1 (en) 2011-01-12 2012-01-11 Crystalline oxazine derivative and its use as bace inhibitor

Publications (1)

Publication Number Publication Date
BR112013017757A2 true BR112013017757A2 (pt) 2016-10-11

Family

ID=45833304

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112013017757A BR112013017757A2 (pt) 2011-01-12 2012-01-11 derivado de oxazina cristalino e seu uso como inibidor de bace

Country Status (15)

Country Link
US (1) US8524897B2 (pt)
EP (1) EP2663560A1 (pt)
JP (1) JP2014502625A (pt)
KR (1) KR20140051823A (pt)
CN (1) CN103429588A (pt)
AR (1) AR084832A1 (pt)
AU (1) AU2012206633A1 (pt)
BR (1) BR112013017757A2 (pt)
CA (1) CA2824207A1 (pt)
CY (1) CY1114757T1 (pt)
EA (1) EA201391026A1 (pt)
MX (1) MX2013008112A (pt)
TW (1) TW201309685A (pt)
UY (1) UY33864A (pt)
WO (1) WO2012095451A1 (pt)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
AR077328A1 (es) 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
EP2485591B1 (en) 2009-10-08 2016-03-23 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
EP2663561B1 (en) 2011-01-13 2016-03-16 Novartis AG Novel heterocyclic derivatives and their use in the treatment of neurological disorders
WO2014065434A1 (en) 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
JP2019524825A (ja) 2016-08-26 2019-09-05 イーライ リリー アンド カンパニー 選択的ｂａｃｅ１阻害剤として有用な１，４−オキサジン

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TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
TW200505902A (en) 2003-03-20 2005-02-16 Schering Corp Cannabinoid receptor ligands
US20070149547A1 (en) 2004-02-12 2007-06-28 Celine Bonnefous Bipyridyl amides as modulators of metabotropic glutamate receptor-5
TW200624426A (en) * 2004-09-21 2006-07-16 Lilly Co Eli BACE inhibitors
US7888374B2 (en) 2005-01-28 2011-02-15 Abbott Laboratories Inhibitors of c-jun N-terminal kinases
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US8822497B2 (en) 2007-03-01 2014-09-02 Novartis Ag PIM kinase inhibitors and methods of their use
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
KR20100017255A (ko) 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
GB0713686D0 (en) 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
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US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
WO2010007756A1 (ja) 2008-07-14 2010-01-21 塩野義製薬株式会社 Ｔｔｋ阻害作用を有するピリジン誘導体
EP2360155A4 (en) 2008-10-22 2012-06-20 Shionogi & Co 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT
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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
JPWO2011058763A1 (ja) 2009-11-13 2013-03-28 塩野義製薬株式会社 アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体
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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
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
JPWO2011077726A1 (ja) 2009-12-24 2013-05-02 塩野義製薬株式会社 ４−アミノ−１，３−チアジンまたはオキサジン誘導体
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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
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JP2013531644A (ja) 2010-06-09 2013-08-08 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 βセクレターゼ（ＢＡＣＥ）の阻害剤として有用な５−アミノ−３，６−ジヒドロ−１Ｈ−ピラジン−２−オン誘導体
SG178311A1 (en) * 2010-07-13 2012-03-29 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders

Also Published As

Publication number Publication date
KR20140051823A (ko) 2014-05-02
TW201309685A (zh) 2013-03-01
MX2013008112A (es) 2013-10-01
JP2014502625A (ja) 2014-02-03
AU2012206633A1 (en) 2013-08-01
UY33864A (es) 2012-08-31
US8524897B2 (en) 2013-09-03
CA2824207A1 (en) 2012-07-19
WO2012095451A1 (en) 2012-07-19
CY1114757T1 (el) 2016-12-14
EP2663560A1 (en) 2013-11-20
AR084832A1 (es) 2013-06-26
CN103429588A (zh) 2013-12-04
EA201391026A1 (ru) 2013-12-30
US20120178745A1 (en) 2012-07-12

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Legal Events

Date Code Title Description
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]
B350 Update of information on the portal [chapter 15.35 patent gazette]