[go: up one dir, main page]
More Web Proxy on the site http://driver.im/

BR112015016315A2 - fluoro-[1,3]oxazinas como inibidores de bace1 - Google Patents

fluoro-[1,3]oxazinas como inibidores de bace1

Info

Publication number
BR112015016315A2
BR112015016315A2 BR112015016315A BR112015016315A BR112015016315A2 BR 112015016315 A2 BR112015016315 A2 BR 112015016315A2 BR 112015016315 A BR112015016315 A BR 112015016315A BR 112015016315 A BR112015016315 A BR 112015016315A BR 112015016315 A2 BR112015016315 A2 BR 112015016315A2
Authority
BR
Brazil
Prior art keywords
oxazine
fluoro
bace1 inhibitors
bace1
present
Prior art date
Application number
BR112015016315A
Other languages
English (en)
Inventor
Kuglstatter Andreas
Limberg Anja
Pinard Emmanuel
Hilpert Hans
Woltering Thomas
Obst Sander Ulrike
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 BR112015016315A2 publication Critical patent/BR112015016315A2/pt

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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • A61P9/10—Drugs 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
    • 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
    • C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
    • C07D265/08—1,3-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
    • 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
    • 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
    • C07D413/10—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 carbon chain containing aromatic rings
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (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)
  • Epidemiology (AREA)

Abstract

resumo patente de invenção: "fluoro-[1,3]oxazinas como inibidores de bace1". a presente invenção refere-se a um composto de fórmula i i, tendo atividade inibitória de bace1, sua fabricação, composições farmacêuticas contendo os mesmos e seu uso como substâncias terapeuticamente ativas. os compostos ativos da presente invenção são úteis no tratamento terapêutico e/ou profilático de, por exemplo, doença de alzheimer.
BR112015016315A 2013-01-22 2014-01-15 fluoro-[1,3]oxazinas como inibidores de bace1 BR112015016315A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13152213 2013-01-22
PCT/EP2014/050645 WO2014114532A1 (en) 2013-01-22 2014-01-15 Fluoro-[1,3]oxazines as bace1 inhibitors

Publications (1)

Publication Number Publication Date
BR112015016315A2 true BR112015016315A2 (pt) 2017-07-11

Family

ID=47559345

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015016315A BR112015016315A2 (pt) 2013-01-22 2014-01-15 fluoro-[1,3]oxazinas como inibidores de bace1

Country Status (11)

Country Link
US (1) US20150376172A1 (pt)
EP (1) EP2948446A1 (pt)
JP (1) JP2016505055A (pt)
KR (1) KR20150109429A (pt)
CN (1) CN104968660A (pt)
BR (1) BR112015016315A2 (pt)
CA (1) CA2896185A1 (pt)
HK (1) HK1210609A1 (pt)
MX (1) MX2015008957A (pt)
RU (1) RU2015132181A (pt)
WO (1) WO2014114532A1 (pt)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2010013256A (es) 2008-06-13 2010-12-21 Shionogi & Co Derivado heterociclico que contiene azufre que tiene actividad inhibitoria de beta-secretasa.
ES2590038T5 (es) 2009-12-11 2021-10-19 Shionogi & Co Derivado de oxazina
WO2014065434A1 (en) 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
MX366855B (es) 2013-03-01 2019-07-26 Amgen Inc Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso.
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
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
CA2957544C (en) 2014-08-08 2023-01-24 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
US10047081B2 (en) 2015-03-20 2018-08-14 Hoffman-La Roche Inc. BACE1 inhibitors
CN107683283B (zh) * 2015-08-12 2021-05-18 豪夫迈·罗氏有限公司 Bace1抑制剂
WO2017061534A1 (en) 2015-10-08 2017-04-13 Shionogi & Co., Ltd. Dihydrothiazine derivatives
WO2017070089A1 (en) 2015-10-19 2017-04-27 Incyte Corporation Heterocyclic compounds as immunomodulators
PT3377488T (pt) 2015-11-19 2022-11-21 Incyte Corp Compostos heterocíclicos como imunomoduladores
US20170174671A1 (en) * 2015-12-17 2017-06-22 Incyte Corporation Heterocyclic compounds as immunomodulators
MX2018007774A (es) 2015-12-22 2018-11-09 Incyte Corp Compuestos heterociclicos como inmunomoduladores.
WO2017148878A1 (en) * 2016-03-01 2017-09-08 F. Hoffmann-La Roche Ag Bace 1 inhibitors
AR108396A1 (es) 2016-05-06 2018-08-15 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
US20170342060A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
PT3472167T (pt) 2016-06-20 2022-11-11 Incyte Corp Compostos heterocíclicos como imunomoduladores
WO2018013789A1 (en) 2016-07-14 2018-01-18 Incyte Corporation Heterocyclic compounds as immunomodulators
MA46045A (fr) 2016-08-29 2021-04-28 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
CA3047287A1 (en) * 2016-12-15 2018-06-21 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
PE20200005A1 (es) 2016-12-22 2020-01-06 Incyte Corp Derivados de tetrahidro imidazo[4,5-c]piridina como inductores de internalizacion pd-l1
WO2018119236A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
ES2899402T3 (es) 2016-12-22 2022-03-11 Incyte Corp Derivados de piridina como inmunomoduladores
GEP20227428B (en) 2016-12-22 2022-10-25 Incyte Corp Heterocyclic compounds as immunomodulators
US11825838B2 (en) 2017-03-31 2023-11-28 Bayer Cropscience Aktiengesellschaft Tricyclic carboxamides for controlling arthropods
CA3095758A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Heterocyclic compounds as immunomodulators
US11629154B2 (en) 2018-04-27 2023-04-18 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity
JP7328995B2 (ja) 2018-05-11 2023-08-17 インサイト・コーポレイション Ｐｄ－ｌ１免疫調節剤としてのテトラヒドロ－イミダゾ［４，５－ｃ］ピリジン誘導体
WO2021030162A1 (en) 2019-08-09 2021-02-18 Incyte Corporation Salts of a pd-1/pd-l1 inhibitor
CA3155852A1 (en) 2019-09-30 2021-04-08 Incyte Corporation PYRIDO[3,2-D]PYRIMIDINE COMPOUNDS AS IMMUNOMODULATORS
EP4058461A1 (en) 2019-11-11 2022-09-21 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
CN111892550B (zh) * 2020-08-25 2022-07-19 苏州大学 4-苯基-6h-1,3-噁嗪-6-酮衍生物及其制备和应用
TW202233615A (zh) 2020-11-06 2022-09-01 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式
IL302590A (en) 2020-11-06 2023-07-01 Incyte Corp Process for preparing PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8785436B2 (en) * 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
KR20140041590A (ko) * 2011-06-07 2014-04-04 에프. 호프만-라 로슈 아게 [1,3]옥사진
EA023261B1 (ru) * 2011-06-07 2016-05-31 Ф.Хоффманн-Ля Рош Аг Галоген-алкил-1,3-оксазины в качестве ингибиторов bace1 и(или) bace2
BR112014015630B1 (pt) * 2012-01-26 2022-05-17 Siena Biotech S.P.A. Fluorometil-5,6-di-hidro-4h-[1,3]oxazinas, seus usos, e composição farmacêutica

Also Published As

Publication number Publication date
CA2896185A1 (en) 2014-07-31
HK1210609A1 (en) 2016-04-29
WO2014114532A1 (en) 2014-07-31
EP2948446A1 (en) 2015-12-02
JP2016505055A (ja) 2016-02-18
CN104968660A (zh) 2015-10-07
KR20150109429A (ko) 2015-10-01
US20150376172A1 (en) 2015-12-31
MX2015008957A (es) 2015-09-29
RU2015132181A (ru) 2017-03-02

Similar Documents

Publication Publication Date Title
BR112015016315A2 (pt) fluoro-[1,3]oxazinas como inibidores de bace1
BR112013031098A2 (pt) halogeno-alquil-1,3 oxazinas como inibidores de bace1 e/ou bace2
BR112014015630A2 (pt) fluorometil-5,6-di-hidro-4h-[1,3]oxazinas
EA201391752A1 (ru) Спиро-[1,3]-оксазины и спиро-[1,4]-оксазепины в качестве ингибиторов bace1 и/или bace2
EA201391670A1 (ru) 1,3-оксазины в качестве ингибиторов bace1 и/или bace2
BR112015019412A2 (pt) inibidores de bace1
BR112013031510A2 (pt) [1,3]oxazinas
BR112013019955A2 (pt) n-[3-(5-amino-3,3a,7,7a-tetra-hidro-1h-2,4-dioxa-6-aza-inden-7-il)-fenil]-amidas como inibidores de bace1 e/ou de bace2
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).
BR112013021798A2 (pt) 1,4 tiazepinaas/sulfonas como inibidores de bace1 e/ou bace2
EA201391468A1 (ru) 1,3-оксазины в качестве ингибиторов bace1 и/или bace2
BR112014006763A2 (pt) n-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexa-hidro-ciclopenta[e][1,3]oxazin-4-il)-fenil)-amidas como inibidores de bace1
MX2013007957A (es) 1,4-oxazinas como inhibidores de los genes de enzima de segmentacion de la proteina precursora amiloide del sitio beta 1 y/o (bace1 y/o bace2).
BR112014028813A2 (pt) 5-amino[1,4]tiazinas como inibidores bace1
MX2013014194A (es) 1,3-tiazepinas fusionadas a ciclopropilo como inhibidores de beta-secretasa 1 (bace) y/o beta-secretasa 2 (bace 2).
EA201590066A1 (ru) Дифторгексагидроциклопентаоксазинилы и дифторгексагидробензоксазинилы в качестве ингибиторов бета-секретазы 1
BR112017015474A2 (pt) inibidores de bace1
BR112016007430A2 (pt) 5-aril-1-imino-1-oxo-[1,2,4]tiadiazinas
BR112016026814A8 (pt) 2,2,2-trifluoroetil-tiadiazinas, intermediário, seu uso e seu processo de preparação, e composição farmacêutica

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]