[go: up one dir, main page]

CL2012001464A1 - Compuestos derivados de (2-amino-5,5-difluor-5,6-dihidro-4h-[1,3]oxazin-4-il)-fenilamida, inhibidores bace1 y/o bace2; composicion farmaceutica; procedimiento de preparacion; y uso en el tratamiento terapeutico y/o profilactico de enfermedades tales como alzheimer y diabetes. - Google Patents

Compuestos derivados de (2-amino-5,5-difluor-5,6-dihidro-4h-[1,3]oxazin-4-il)-fenilamida, inhibidores bace1 y/o bace2; composicion farmaceutica; procedimiento de preparacion; y uso en el tratamiento terapeutico y/o profilactico de enfermedades tales como alzheimer y diabetes.

Info

Publication number
CL2012001464A1
CL2012001464A1 CL2012001464A CL2012001464A CL2012001464A1 CL 2012001464 A1 CL2012001464 A1 CL 2012001464A1 CL 2012001464 A CL2012001464 A CL 2012001464A CL 2012001464 A CL2012001464 A CL 2012001464A CL 2012001464 A1 CL2012001464 A1 CL 2012001464A1
Authority
CL
Chile
Prior art keywords
difluor
bace1
phenylamide
oxazin
alzheimer
Prior art date
Application number
CL2012001464A
Other languages
English (en)
Inventor
David Guba Wolfgang Hilpert Hans Mauser Harald Mayweg Alexander V Narquizian Robert Pinard Em Banner
Original Assignee
F Hoffmann La Roche Ag Siena Biotech S P A
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=43585547&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CL2012001464(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by F Hoffmann La Roche Ag Siena Biotech S P A filed Critical F Hoffmann La Roche Ag Siena Biotech S P A
Publication of CL2012001464A1 publication Critical patent/CL2012001464A1/es

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
    • C07D265/041,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/061,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
    • C07D265/081,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • 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
    • 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
    • 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)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CL2012001464A 2009-12-11 2012-06-05 Compuestos derivados de (2-amino-5,5-difluor-5,6-dihidro-4h-[1,3]oxazin-4-il)-fenilamida, inhibidores bace1 y/o bace2; composicion farmaceutica; procedimiento de preparacion; y uso en el tratamiento terapeutico y/o profilactico de enfermedades tales como alzheimer y diabetes. CL2012001464A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09178983 2009-12-11

Publications (1)

Publication Number Publication Date
CL2012001464A1 true CL2012001464A1 (es) 2014-03-07

Family

ID=43585547

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2012001464A CL2012001464A1 (es) 2009-12-11 2012-06-05 Compuestos derivados de (2-amino-5,5-difluor-5,6-dihidro-4h-[1,3]oxazin-4-il)-fenilamida, inhibidores bace1 y/o bace2; composicion farmaceutica; procedimiento de preparacion; y uso en el tratamiento terapeutico y/o profilactico de enfermedades tales como alzheimer y diabetes.

Country Status (26)

Country Link
US (1) US8389513B2 (es)
EP (1) EP2509965A1 (es)
JP (1) JP5584778B2 (es)
KR (1) KR101506773B1 (es)
CN (1) CN102712609A (es)
AR (1) AR079327A1 (es)
AU (1) AU2010330031B2 (es)
BR (1) BR112012013175A2 (es)
CA (1) CA2776727C (es)
CL (1) CL2012001464A1 (es)
CO (1) CO6541656A2 (es)
CR (1) CR20120262A (es)
EC (1) ECSP12011961A (es)
IL (1) IL219107A (es)
IN (1) IN2012DN03043A (es)
MA (1) MA34779B1 (es)
MX (1) MX2012006493A (es)
MY (1) MY169962A (es)
NZ (1) NZ599008A (es)
PE (1) PE20121500A1 (es)
PH (1) PH12012500619A1 (es)
RU (1) RU2515221C2 (es)
SG (1) SG181610A1 (es)
TW (1) TWI487704B (es)
UA (1) UA103272C2 (es)
WO (1) WO2011069934A1 (es)

Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101346357B (zh) 2005-10-25 2014-04-02 盐野义制药株式会社 氨基二氢噻嗪衍生物
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
EP2689780A1 (en) 2007-04-24 2014-01-29 Shionogi & Co., Ltd. Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group
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
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
EP2485591B1 (en) 2009-10-08 2016-03-23 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
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
KR20120104570A (ko) 2009-12-11 2012-09-21 시오노기세야쿠 가부시키가이샤 옥사진 유도체
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
CN103261199A (zh) 2010-10-29 2013-08-21 盐野义制药株式会社 萘啶衍生物
EP2634188A4 (en) 2010-10-29 2014-05-07 Shionogi & Co FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE
EP2643325A1 (en) 2010-11-23 2013-10-02 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
BR112013015430A2 (pt) 2010-12-22 2016-09-20 Janssen Pharmaceutica Nv derivados de 5,6-diidro-imidazo[1,2-a]pirazin-8-ilamina úteis como inibidores de beta-secretase (bace)
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
DK2663561T3 (en) 2011-01-13 2016-06-06 Novartis Ag New heterocyclic derivatives and their use in treating neurological disorders
TWI547482B (zh) 2011-01-25 2016-09-01 陶氏農業科學公司 增加可回收之3-氯-4,5,6-三氟-2-氰吡啶之量的改良方法
US8404680B2 (en) 2011-02-08 2013-03-26 Hoffmann-La Roche Inc. N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors
US8815841B2 (en) * 2011-02-18 2014-08-26 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
PH12013501805A1 (en) 2011-03-09 2013-11-18 Janssen Pharmaceutica Nv 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
US9145426B2 (en) 2011-04-07 2015-09-29 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
US8754075B2 (en) * 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
RU2013150349A (ru) 2011-04-13 2015-05-20 Мерк Шарп И Доум Корп. 5-замещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов васе, содержащие их композиции и их применение
CN103608345A (zh) * 2011-04-26 2014-02-26 盐野义制药株式会社 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂
US8785436B2 (en) * 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
US9079919B2 (en) * 2011-05-27 2015-07-14 Hoffmann-La Roche Inc. Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors
AU2012266544A1 (en) * 2011-06-07 2013-11-21 F. Hoffmann-La Roche Ag Halogen-alkyl-1,3 oxazines as BACE1 and/or BACE2 inhibitors
MX2013014007A (es) * 2011-06-07 2014-03-12 Hoffmann La Roche [1,3] oxazinas.
US9181236B2 (en) 2011-08-22 2015-11-10 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
UY34278A (es) * 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
US20130073953A1 (en) * 2011-09-21 2013-03-21 Timothy Onyenobi News headline screenshot viewing system
UA111749C2 (uk) * 2011-12-05 2016-06-10 Янссен Фармацевтика Нв Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну
PE20142376A1 (es) * 2012-01-26 2015-01-17 Hoffmann La Roche Fluormetil-5,6-dihidro-4h-[1,3]oxazinas
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
JP2015514073A (ja) 2012-03-20 2015-05-18 エラン ファーマシューティカルズ, リミテッド・ライアビリティ・カンパニー スピロ環式ジヒドロ−チアジンおよびジヒドロ−オキサジンbace阻害剤、ならびにその組成物および使用
CA2872179A1 (en) 2012-05-24 2013-11-28 F. Hoffmann-La Roche Ag 5-amino[1,4]thiazines as bace 1 inhibitors
KR20150023450A (ko) * 2012-06-26 2015-03-05 에프. 호프만-라 로슈 아게 Bace1 억제제로서의 다이플루오로-헥사하이드로-사이클로펜타옥사진일 및 다이플루오로-헥사하이드로-벤조옥사진일
WO2014056816A1 (en) 2012-10-10 2014-04-17 F. Hoffmann-La Roche Ag COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR
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
WO2014065434A1 (en) * 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
US9309263B2 (en) 2013-01-29 2016-04-12 Amgen Inc. Fused multi-cyclic sulfone compounds as inhibitors of beta-secretase and methods of use thereof
JP6389830B2 (ja) * 2013-03-01 2018-09-12 アムジエン・インコーポレーテツド ベータ−セクレターゼ阻害剤としてのパーフルオロ化5,6−ジヒドロ−4h−1,3−オキサジン−2−アミン化合物および使用方法
JP6374889B2 (ja) 2013-03-08 2018-08-15 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過フッ素化シクロプロピル縮合1,3−オキサジン−2−アミン化合物、及び使用方法
AU2014253275B2 (en) 2013-04-11 2018-10-18 F. Hoffmann-La Roche Ag BACE1 inhibitors
MX2015014728A (es) * 2013-04-26 2016-03-07 Hoffmann La Roche Sintesis de inhibidores de beta secretasa (bace).
US9751886B2 (en) 2013-06-12 2017-09-05 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)
WO2014198851A1 (en) 2013-06-12 2014-12-18 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)
JO3318B1 (ar) 2013-06-18 2019-03-13 Lilly Co Eli مثبطات bace
WO2015017407A1 (en) 2013-07-30 2015-02-05 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta- secretase
TW201623295A (zh) 2014-04-11 2016-07-01 塩野義製藥股份有限公司 具有bace1抑制活性之二氫噻及二氫衍生物
US9550762B2 (en) 2014-08-08 2017-01-24 Amgen, Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
ES2768823T3 (es) 2014-12-18 2020-06-23 Janssen Pharmaceutica Nv Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa
CN107406440B (zh) 2015-03-20 2021-05-07 豪夫迈·罗氏有限公司 Bace1抑制剂
WO2017024180A1 (en) 2015-08-06 2017-02-09 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
WO2017061534A1 (en) 2015-10-08 2017-04-13 Shionogi & Co., Ltd. Dihydrothiazine derivatives
MX388697B (es) 2016-12-15 2025-03-20 Amgen Inc Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso.
MX386618B (es) 2016-12-15 2025-03-19 Amgen Inc Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso.
MA54101A (fr) 2016-12-15 2021-10-27 Amgen Inc Dérivés de thiazine et d'oxazine bicycliques en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
EP3555086B1 (en) 2016-12-15 2021-09-01 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
MA52722A (fr) 2016-12-15 2021-04-14 Amgen Inc Dérivés d'oxazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
CA3098430A1 (en) 2018-04-27 2019-10-31 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective bace1 inhibitory activity
CN110747276B (zh) * 2019-11-22 2020-06-30 山东大学齐鲁医院 Bace2作为胶质瘤预后/诊断/治疗标志物的应用

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1156798T3 (da) * 1999-02-09 2003-11-03 Univ Virginia Felbamat-afledte forbindelser
AU2003273310A1 (en) * 2002-09-10 2004-04-30 Pharmacia And Upjohn Substituted aminoethers for the treatment of alzheimer's disease
ATE443043T1 (de) * 2002-11-12 2009-10-15 Merck & Co Inc Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer
RU2336270C2 (ru) * 2003-06-30 2008-10-20 Дайити Фармасьютикал Ко., Лтд. Гетероциклические метилсульфоновые производные
JP2008513426A (ja) 2004-09-20 2008-05-01 バイオリポックス エービー 炎症の治療に有用なピラゾール化合物
EP1802587A4 (en) * 2004-10-15 2010-02-17 Astrazeneca Ab SUBSTITUTED AMINO BINDINGS AND THEIR APPLICATIONS
CN101346357B (zh) 2005-10-25 2014-04-02 盐野义制药株式会社 氨基二氢噻嗪衍生物
SA08290245B1 (ar) 2007-04-23 2012-02-12 استرازينيكا ايه بي مشتقات كربو كساميد جديدة من -n (8-اريل رباعي هيدرو نفثالين غير متجانس- 2- يل) أو -n (5-اريل كرومان غير متجانس -3-يل) لعلاج الألم
EP2689780A1 (en) 2007-04-24 2014-01-29 Shionogi & Co., Ltd. Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group
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
BRPI0906962B8 (pt) 2008-01-18 2021-05-25 Eisai R&D Man Co Ltd composto de aminodiidrotiazina fundido
KR101259240B1 (ko) 2008-02-18 2013-04-29 시에나 바이오테크 에스.피.에이. 4,5-다이하이드로-옥사졸-2-일 아민 유도체
GB0912778D0 (en) * 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
US20120245155A1 (en) * 2009-12-11 2012-09-27 Shionogi & Co., Ltd. Fused heterocyclic compound having amino group

Also Published As

Publication number Publication date
US8389513B2 (en) 2013-03-05
CA2776727A1 (en) 2011-06-16
AU2010330031A1 (en) 2012-06-07
ECSP12011961A (es) 2012-07-31
SG181610A1 (en) 2012-07-30
RU2515221C2 (ru) 2014-05-10
JP2013513563A (ja) 2013-04-22
BR112012013175A2 (pt) 2019-09-24
PE20121500A1 (es) 2012-11-05
CR20120262A (es) 2012-07-27
NZ599008A (en) 2013-08-30
IL219107A0 (en) 2012-06-28
AR079327A1 (es) 2012-01-18
MA34779B1 (fr) 2014-01-02
KR101506773B1 (ko) 2015-03-27
JP5584778B2 (ja) 2014-09-03
IN2012DN03043A (es) 2015-07-31
CO6541656A2 (es) 2012-10-16
KR20120104598A (ko) 2012-09-21
PH12012500619A1 (en) 2012-10-22
EP2509965A1 (en) 2012-10-17
MX2012006493A (es) 2012-07-03
CN102712609A (zh) 2012-10-03
CA2776727C (en) 2016-05-31
UA103272C2 (uk) 2013-09-25
AU2010330031B2 (en) 2013-06-20
TW201124408A (en) 2011-07-16
IL219107A (en) 2015-10-29
TWI487704B (zh) 2015-06-11
US20110144097A1 (en) 2011-06-16
WO2011069934A1 (en) 2011-06-16
MY169962A (en) 2019-06-19
RU2012126989A (ru) 2014-01-20

Similar Documents

Publication Publication Date Title
CL2012001464A1 (es) Compuestos derivados de (2-amino-5,5-difluor-5,6-dihidro-4h-[1,3]oxazin-4-il)-fenilamida, inhibidores bace1 y/o bace2; composicion farmaceutica; procedimiento de preparacion; y uso en el tratamiento terapeutico y/o profilactico de enfermedades tales como alzheimer y diabetes.
PH12013502090A1 (en) 1,3 oxazines as bace1 and/or bace2 inhibitors
IN2012DN00766A (es)
MX2013014007A (es) [1,3] oxazinas.
PH12013502316A1 (en) Halogen-alkyl-1,3 oxazines as bace1 and/or bace2 inhibitors
PH12013502156A1 (en) 1,3-oxazines as bace1 and/or bace2 inhibitors
CL2007002708A1 (es) Compuestos derivados de pirrolo[2,3-b]piridina; procedimiento de preparacion; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, caquexia, trastornos inflamatorios, entre otros.
WO2012104263A3 (en) 1,4 oxazines as bace1 and/or bace2 inhibitors
MX2013007558A (es) 1,4-oxazinas como inhibidores de los genes enzima de segmentacion de la proteina precursora del sitio 1 y/o 2 (bace1 y/o bace2).
CL2008000307A1 (es) Compuestos derivados de cromen-2-ona sustituido; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como ateroesclerosis, asma, rinitis alergica y epoc.
PH12013502262A1 (en) Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as bace1 and/or bace2 inhibitors
CL2007003765A1 (es) Compuestos derivados de 2-oxo-4-hidroxi-benzotiazol; procesode preparacion; composicion farmaceutica; combinacion farmaceutica; y uso en el tratamiento de enfermedades tales como epoc, bronquitis, asma y bronquiectasias.
CL2007002513A1 (es) Compuestos derivados de isoindolina sustituidos, compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento y prevencion de enfermedades tales como cancer, dolor, degeneracion macular, entre otras.
CL2007003879A1 (es) Compuestos derivados de aril-carboxamida; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como alzheimer, epilepsia y parkinson.
CL2008000690A1 (es) Compuestos derivados del acido indol-3-propionico; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como hiperlipidemia, hipertension; entre otras.
CL2008000434A1 (es) Compuestos derivados de 2-amino-oxazolinas; proceso de obtencion; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como depresion, ansiedad, estres, trastorno bipolar, entre otros.
CL2008001994A1 (es) Compuestos derivados de pirazin-2-ona; combinacion farmaceutica; y uso en el tratamiento de enfermedades tales como diabetes, aterosclerosis, hipertension, entre otras.
CL2008001025A1 (es) Compuestos derivados de pirimido[5,4-d]pirimidina-2,4,6,8-tetraona; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como trastorno metabolico, dislipidemia y cancer.
MX2013008478A (es) 1, 4 riazepinas/sulfonas como inhibidores de beta secretasa 1 (base1) y/o beta secretasa 2 (bace2).
PH12014501334A1 (en) Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
CL2007002207A1 (es) Compuestos derivados de sulfonilaminas; composicion farmaceutica; y uso de los compuestos en el tratamiento del glaucoma.
CL2008000875A1 (es) Compuestos derivados de imidazolidin-2-ona; proceso de obtencion; composicion farmaceutica; y uso en el tratamiento y/o profilaxis de enfermedades tales como dislipidemia, diabetes, enfermedades inflamatorias, entre otras.
MX2013014194A (es) 1,3-tiazepinas fusionadas a ciclopropilo como inhibidores de beta-secretasa 1 (bace) y/o beta-secretasa 2 (bace 2).
CL2011000119A1 (es) Compuestos derivados de triazolo[4,3-a]piridina; procedimiento de preparacion; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer.
CL2014003325A1 (es) Compuestos derivados de difluoro-hexahidro-ciclopentaoxacinilos y difluoro-hexahidro-benzooxacinilos, inhibidores de bace 1; composicion farmaceutica; y su uso en el tratamiento de enfermedades con niveles elevados de beta-amiloide, tal como la enfermedad de alzheimer