UA101352C2 - Конденсоване похідне амінодигідротіазину - Google Patents

Конденсоване похідне амінодигідротіазину

Info

Publication number
UA101352C2
UA101352C2 UAA201010101A UAA201010101A UA101352C2 UA 101352 C2 UA101352 C2 UA 101352C2 UA A201010101 A UAA201010101 A UA A201010101A UA A201010101 A UAA201010101 A UA A201010101A UA 101352 C2 UA101352 C2 UA 101352C2
Authority
UA
Ukraine
Prior art keywords
heading
hydrogen atom
normal
pharmaceutically acceptable
acceptable salt
Prior art date
Application number
UAA201010101A
Other languages
English (en)
Russian (ru)
Inventor
Юічі Судзукі
Такафумі Мотокі
Тошіхіко Канеко
Мамору Такаіші
Тасуку Ішіда
Кунітоші Такеда
Йоічі Кіта
Нобору ЯМАМОТО
Афзал КХАН
Пасчаліс Дімопоулос
Original Assignee
Ейсей Р Енд Д Менеджмент Ко., Лтд.
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=40885398&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=UA101352(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ейсей Р Енд Д Менеджмент Ко., Лтд. filed Critical Ейсей Р Енд Д Менеджмент Ко., Лтд.
Publication of UA101352C2 publication Critical patent/UA101352C2/uk

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/08—1,3-Thiazines; Hydrogenated 1,3-thiazines condensed with carbocyclic rings or ring systems
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07D417/12—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 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Compositions Of Macromolecular Compounds (AREA)

Abstract

Представлений винахід стосується сполуки загальної формули (І): EMBED MDLDrawOLE.MDLDrawObject.1 (I) або її фармацевтично прийнятної солі, або її сольвату, які демонструють інгібуючу активність щодо вироблення Αβ або інгібуючу активність щодо ВАСЕ1 та можуть застосовуватись як профілактичні або терапевтичні агенти при нейродегенеративних захворюваннях, спричинених Αβ, типовим представником яких є слабоумство альцгеймерівського типу.
UAA201010101A 2008-01-18 2009-01-16 Конденсоване похідне амінодигідротіазину UA101352C2 (uk)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US2193908P 2008-01-18 2008-01-18
JP2008008680 2008-01-18
US8502408P 2008-07-31 2008-07-31
JP2008197204 2008-07-31
PCT/JP2009/050511 WO2009091016A1 (ja) 2008-01-18 2009-01-16 縮合アミノジヒドロチアジン誘導体

Publications (1)

Publication Number Publication Date
UA101352C2 true UA101352C2 (uk) 2013-03-25

Family

ID=40885398

Family Applications (1)

Application Number Title Priority Date Filing Date
UAA201010101A UA101352C2 (uk) 2008-01-18 2009-01-16 Конденсоване похідне амінодигідротіазину

Country Status (26)

Country Link
US (4) US8158620B2 (uk)
EP (1) EP2233474B1 (uk)
JP (1) JP4520533B2 (uk)
KR (1) KR101564634B1 (uk)
CN (1) CN101910143B (uk)
AU (1) AU2009205072C1 (uk)
BR (1) BRPI0906962B8 (uk)
CA (1) CA2711655C (uk)
CY (1) CY1117014T1 (uk)
DK (1) DK2233474T3 (uk)
ES (1) ES2548774T3 (uk)
HR (1) HRP20151030T1 (uk)
HU (1) HUE026064T2 (uk)
IL (1) IL206952A (uk)
MY (1) MY160690A (uk)
NZ (1) NZ586796A (uk)
PE (1) PE20091438A1 (uk)
PL (1) PL2233474T3 (uk)
PT (1) PT2233474E (uk)
RS (1) RS54311B1 (uk)
RU (1) RU2476431C2 (uk)
SI (1) SI2233474T1 (uk)
TW (1) TWI423970B (uk)
UA (1) UA101352C2 (uk)
WO (1) WO2009091016A1 (uk)
ZA (1) ZA201004799B (uk)

Families Citing this family (137)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
CA2610828A1 (en) 2005-06-14 2006-12-28 Schering Corporation Heterocyclic aspartyl protease inhibitors, preparation and use thereof
CN101228163A (zh) 2005-06-14 2008-07-23 先灵公司 天冬氨酰蛋白酶抑制剂
EP2612854B1 (en) 2005-10-25 2015-04-29 Shionogi&Co., Ltd. Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
EP2032542A2 (en) 2006-06-12 2009-03-11 Schering Corporation Heterocyclic aspartyl protease inhibitors
WO2008133273A1 (ja) 2007-04-24 2008-11-06 Shionogi & Co., Ltd. アルツハイマー症治療用医薬組成物
TW200902526A (en) 2007-04-24 2009-01-16 Shionogi & Amp Co Ltd Aminodihydrothiazin derivative substituted with a cyclic group
ES2548774T3 (es) * 2008-01-18 2015-10-20 Eisai R&D Management Co., Ltd. Derivado de aminodihidrotiazina condensado
CL2009000954A1 (es) 2008-04-22 2010-12-31 Schering Corp Compuestos derivados de 2-imino-3-metil pirrolo pirimidinona,inhibidores de bace-1; composicion farmaceutica; y su uso para tratar, prevenir y/o retardar el inicio de una patologia de beta-amiloide seleccionada de enfermedad de alzheimer, enfermedad de parkinson, perdida de la memoria, sindrome de down, entre otras.
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
CN102105475B (zh) * 2008-07-28 2014-04-09 卫材R&D管理有限公司 螺氨基二氢噻嗪衍生物
CA2736130C (en) * 2008-09-11 2014-01-14 Amgen Inc. Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use
AU2009300836B2 (en) * 2008-09-30 2014-02-27 Eisai R&D Management Co., Ltd. Novel fused aminodihydrothiazine derivative
RU2503681C2 (ru) * 2008-09-30 2014-01-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Новое конденсированное производное аминодигидротиазина
JPWO2010047372A1 (ja) 2008-10-22 2012-03-22 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２−アミノピリミジン−４−オンおよび２−アミノピリジン誘導体
AR077277A1 (es) * 2009-07-09 2011-08-17 Lilly Co Eli Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer
GB0912777D0 (en) * 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydropyrimidone derivatives
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
AR077328A1 (es) 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
WO2011044184A1 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
WO2011058763A1 (ja) 2009-11-13 2011-05-19 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
US8870950B2 (en) 2009-12-08 2014-10-28 Mitral Tech Ltd. Rotation-based anchoring of an implant
EP2514747A4 (en) 2009-12-09 2013-05-08 Shionogi & Co SUBSTITUTED AMINOTHIAZINE DERIVATIVE
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
JPWO2011071109A1 (ja) * 2009-12-11 2013-04-22 塩野義製薬株式会社 アミノ基を有する縮合ヘテロ環化合物
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
UA110467C2 (uk) 2009-12-11 2016-01-12 Шионогі Енд Ко., Лтд. Похідні оксазину
CN102712621B (zh) 2009-12-31 2015-03-11 诺华股份有限公司 吡嗪衍生物及其在治疗神经学障碍中的用途
AU2011227501B9 (en) 2010-03-15 2013-08-22 Amgen Inc. Amino -dihydrooxazine and amino - dihydrothiazine spiro compounds as Beta - secretase modulators and their medical use
WO2011115938A1 (en) 2010-03-15 2011-09-22 Amgen Inc. Spiro-tetracyclic ring compounds as beta - secretase modulators
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
DK2483255T3 (da) 2010-07-13 2014-01-20 Novartis Ag Oxazinderivater samt deres anvendelse ved behandling af neurologiske lidelser
WO2012019056A1 (en) 2010-08-05 2012-02-09 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
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
WO2012071279A1 (en) 2010-11-23 2012-05-31 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
EA201391029A1 (ru) 2011-01-12 2014-01-30 Новартис Аг Производные оксазина и их применение при лечении неврологических нарушений
CA2824220C (en) 2011-01-13 2020-09-01 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
GB201101140D0 (en) * 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
BR112013016241A2 (pt) * 2011-01-21 2016-07-12 Eisai R&D Man Co Ltd composto, e, método para fabricar um composto
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
US9346827B2 (en) 2011-02-07 2016-05-24 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use
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
EP2675810A1 (en) 2011-02-15 2013-12-25 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
US8815841B2 (en) 2011-02-18 2014-08-26 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
US9145426B2 (en) 2011-04-07 2015-09-29 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
WO2012138734A1 (en) 2011-04-07 2012-10-11 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
WO2012147763A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤
KR20140054295A (ko) 2011-08-22 2014-05-08 머크 샤프 앤드 돔 코포레이션 Bace 억제제로서의 2-스피로-치환된 이미노티아진 및 그의 모노- 및 디옥시드, 조성물 및 그의 용도
JP6043355B2 (ja) 2011-08-31 2016-12-14 ファイザー・インク ヘキサヒドロピラノ［３，４−ｄ］［１，３］チアジン−２−アミン化合物
US9296759B2 (en) 2011-09-21 2016-03-29 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
EP2807155B1 (en) 2012-01-26 2017-04-12 F. Hoffmann-La Roche AG Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
JO3143B1 (ar) * 2012-04-03 2017-09-20 Lilly Co Eli مركبات تتراهيدرو بيرولو ثيازين
EP2841423B1 (en) * 2012-04-27 2016-11-30 Eisai R&D Management Co., Ltd. Method for producing 5-(difluoromethyl)pyrazine-2-carboxilic acid and production intermediate thereof
ES2585262T3 (es) 2012-05-04 2016-10-04 Pfizer Inc Compuestos heterocíclicos de hexahidropiran[3,4-d][1,3]tiazin-2-amina sustituidos como inhibidores de PPA, BACE1 y BACE2
WO2014015125A1 (en) * 2012-07-19 2014-01-23 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivative salts and uses thereof
GB201212871D0 (en) * 2012-07-20 2012-09-05 Eisai Ltd Novel compounds
CA2882389A1 (en) 2012-09-20 2014-03-27 Pfizer Inc. Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
HUE031764T2 (en) 2012-10-26 2017-07-28 Lilly Co Eli Tetrahydropyrrolothiazine derivatives as BACE inhibitors
WO2014078314A1 (en) 2012-11-15 2014-05-22 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
WO2014091352A1 (en) * 2012-12-11 2014-06-19 Pfizer Inc. Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1
CA2893333C (en) * 2012-12-19 2017-10-24 Pfizer Inc. Carbocyclic-and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
WO2014120658A1 (en) 2013-01-29 2014-08-07 Amgen Inc. Fused multicyclic 3-amino-5,6-dihydro-2h-1,4-thiazine derivatives and their use as beta-secretase inhibitors
WO2014125394A1 (en) 2013-02-13 2014-08-21 Pfizer Inc. HETEROARYL-SUBSTITUTED HEXAHYDROPYRANO [3,4-d][1,3] THIAZIN-2-AMINE COMPOUNDS
US9233981B1 (en) * 2013-02-15 2016-01-12 Pfizer Inc. Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
CA2902212C (en) 2013-03-01 2020-10-13 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
AU2014225604B2 (en) 2013-03-08 2018-05-17 Amgen Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
TWI593692B (zh) * 2013-03-12 2017-08-01 美國禮來大藥廠 四氫吡咯并噻嗪化合物
PE20151748A1 (es) 2013-04-11 2015-12-02 Hoffmann La Roche Inhibidores de bace1
TWI639607B (zh) * 2013-06-18 2018-11-01 美國禮來大藥廠 Ｂａｃｅ抑制劑
WO2015017407A1 (en) 2013-07-30 2015-02-05 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta- secretase
TWI684452B (zh) 2014-03-14 2020-02-11 美國禮來大藥廠 胺基噻嗪化合物
CR20160455A (es) 2014-04-10 2016-12-16 Pfizer 2-AMINO-6-METIL-4,4a,5,6-TETRAHIDROPIRANO[3,4-d][1,3]TIAZIN-8a(8H)-IL-1,3-TIAZOL-4-ILA
AU2015301028B2 (en) 2014-08-08 2019-09-26 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
TWI570127B (zh) * 2014-09-15 2017-02-11 美國禮來大藥廠 結晶型N-[3-[(4aR,7aS)-2-胺基-6-(5-氟嘧啶-2-基)-4,4a,5,7-四氫吡咯并[3,4-d][1,3]噻嗪-7a-基]-4-氟-苯基]-5-甲氧基-吡嗪-2-甲醯胺、其用途及醫藥組合物
TWI599358B (zh) * 2014-09-16 2017-09-21 美國禮來大藥廠 組合療法
KR102524217B1 (ko) * 2014-10-10 2023-04-21 에자이 알앤드디 매니지먼트 가부시키가이샤 축합 아미노디하이드로티아진 유도체의 의약 조성물
AR103406A1 (es) * 2015-01-30 2017-05-10 Lilly Co Eli Sal de tosilato
AR103680A1 (es) * 2015-02-23 2017-05-24 Lilly Co Eli Inhibidores selectivos de bace1
EP3271356B1 (en) * 2015-03-19 2019-10-16 Eli Lilly and Company Selective bace1 inhibitors
AR104241A1 (es) 2015-04-29 2017-07-05 Lilly Co Eli Derivados de tetrahidrofuro tiazina como inhibidores de bace1 selectivos
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
WO2017051276A1 (en) 2015-09-24 2017-03-30 Pfizer Inc. N-[2-(2-amino-6,6-disubstituted-4, 4a, 5, 6-tetrahydropyrano [3,4-d][1,3] thiazin-8a (8h)-yl) -1, 3-thiazol-4-yl] amides
EP3353174A1 (en) 2015-09-24 2018-08-01 Pfizer Inc N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2h-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl]amides useful as bace inhibitors
JP2018531924A (ja) 2015-09-24 2018-11-01 ファイザー・インク テトラヒドロピラノ［３，４−ｄ］［１，３］オキサジン誘導体、およびｂａｃｅ阻害剤としてのその使用
ES2928164T3 (es) 2015-10-19 2022-11-15 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
IL284874B2 (en) 2015-10-30 2023-10-01 Neurocrine Biosciences Inc Valbenazine salts and polymorphs thereof
MD3377488T2 (ro) 2015-11-19 2023-02-28 Incyte Corp Compuși heterociclici ca imunomodulatori
WO2017095759A1 (en) * 2015-12-04 2017-06-08 Merck Sharp & Dohme Corp. C5-c6-carbocyclic fused iminothiadiazine dioxides as bace inhibitors, compositions, and their use
MA44075A (fr) 2015-12-17 2021-05-19 Incyte Corp Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1
MY199705A (en) 2015-12-22 2023-11-20 Incyte Corp Heterocyclic compounds as immunomodulators
LT3394057T (lt) 2015-12-23 2022-06-27 Neurocrine Biosciences, Inc. Sintezės būdas, skirtas pagaminti (s)-(2r,3r,11br)-3-izobutil-9,10-dimetoksi-2,3,4,6,7,11b-heksahidro-1h-pirido[2,1-a]izochinolin-2-ilo 2-amino-3-metilbutanoato di(4-metilbenzensulfonatą)
TW201740954A (zh) * 2016-03-16 2017-12-01 美國禮來大藥廠 組合療法
WO2017192961A1 (en) 2016-05-06 2017-11-09 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2017205464A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
KR102685249B1 (ko) 2016-06-20 2024-07-17 인사이트 코포레이션 면역조절제로서의 복소환식 화합물
MA45669A (fr) 2016-07-14 2019-05-22 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
JP2019530647A (ja) * 2016-08-18 2019-10-24 イーライ リリー アンド カンパニー Ｂａｃｅ−１阻害剤と抗ｎ３ｐｇｌｕ ａベータ抗体の併用療法
WO2018044783A1 (en) 2016-08-29 2018-03-08 Incyte Corporation Heterocyclic compounds as immunomodulators
TWI669119B (zh) 2016-10-21 2019-08-21 美國禮來大藥廠 組合療法
CA3042020A1 (en) * 2016-10-27 2018-05-03 Eisai R&D Management Co., Ltd. Composition comprising an anti-abeta protofibril antibody and a beta-secretase bace1 inhibitor for the treatment of alzheimer's disease
CA3047285A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
MX387729B (es) 2016-12-15 2025-03-18 Amgen Inc Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso.
AU2017378316B2 (en) 2016-12-15 2021-04-01 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
MA54100A (fr) 2016-12-15 2021-10-20 Amgen Inc Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
US10947223B2 (en) 2016-12-15 2021-03-16 Amgen Inc. Substituted oxazines as beta-secretase inhibitors
CA3047991A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
EP3558989B1 (en) 2016-12-22 2021-04-14 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
PE20191532A1 (es) 2016-12-22 2019-10-23 Incyte Corp Compuestos heterociclicos como inmunomoduladores
WO2018119224A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Tetrahydro imidazo[4,5-c]pyridine derivatives as pd-l1 internalization inducers
EP3558973B1 (en) 2016-12-22 2021-09-15 Incyte Corporation Pyridine derivatives as immunomodulators
CN107892697B (zh) * 2016-12-26 2020-11-03 郑州泰基鸿诺医药股份有限公司 一种[1,3]噻嗪-2-胺类化合物及应用，药物组合物
KR20230169457A (ko) 2017-01-27 2023-12-15 뉴로크린 바이오사이언시즈 인코퍼레이티드 특정 vmat2 억제제의 투여 방법
RS66714B1 (sr) 2017-09-21 2025-05-30 Neurocrine Biosciences Inc Formulacija visoke doze valbenazina i sastavi, postupci i kompleti povezani sa njim
KR20250070134A (ko) 2017-10-10 2025-05-20 뉴로크린 바이오사이언시즈 인코퍼레이티드 특정 vmat2 억제제의 투여 방법
MX2020003421A (es) 2017-10-10 2020-07-20 Neurocrine Biosciences Inc Metodos para la administracion de ciertos inhibidores del transportador vesicular de monoamina 2 (vmat2).
RS64055B1 (sr) 2018-03-30 2023-04-28 Incyte Corp Heterociklična jedinjenja kao imunomodulatori
MD3790877T2 (ro) 2018-05-11 2023-08-31 Incyte Corp Derivați de tetrahidro-imidazo[4,5-c]piridină în calitate de imunomodulatori PD-L1
CA3107370A1 (en) 2018-07-24 2020-01-30 Eisai R&D Management Co., Ltd. Methods of treatment and prevention of alzheimer's disease
MA53239A (fr) 2018-08-15 2022-05-04 Neurocrine Biosciences Inc Procédés d'administration de certains inhibiteurs de vmat2
CN109748878A (zh) * 2019-01-21 2019-05-14 江苏中旗科技股份有限公司 一种甲磺草胺关键中间体苯连三唑啉酮衍生物的制备方法
JP7665593B2 (ja) 2019-08-09 2025-04-21 インサイト・コーポレイション Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩
US10940141B1 (en) 2019-08-23 2021-03-09 Neurocrine Biosciences, Inc. Methods for the administration of certain VMAT2 inhibitors
AR120109A1 (es) 2019-09-30 2022-02-02 Incyte Corp Compuestos de pirido[3,2-d]pirimidina como inmunomoduladores
PE20230407A1 (es) 2019-11-11 2023-03-07 Incyte Corp Sales y formas cristalinas de un inhibidor de pd-1/pd-l1
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
WO2022099075A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Crystalline form of a pd-1/pd-l1 inhibitor
TW202233616A (zh) 2020-11-06 2022-09-01 美商英塞特公司 用於製備ｐｄ－１／ｐｄ－ｌ１抑制劑以及其鹽及結晶形式之方法

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3235551A (en) 1966-02-15 Novel derivatives of
US3227713A (en) 1966-01-04 Azine derivatives
SU770029A1 (ru) * 1979-05-11 1986-12-15 Научно-исследовательский институт фармакологии Производные 2-аминометил-4,4-диметил-4 @ -1,3-бензтиазина в свободном виде или в виде кислотно-аддитивной соли,обладающие антидепрессивной активностью
AU4149696A (en) * 1994-11-15 1996-06-06 Merck & Co., Inc. Substituted heterocycles as inhibitors of nitric oxide synthase
JPH0967355A (ja) 1995-08-31 1997-03-11 Tokyo Tanabe Co Ltd チアジン誘導体、チアゾール誘導体及びそれらの製造方法
EP1283039A4 (en) 2000-05-19 2007-05-30 Takeda Pharmaceutical INHIBITORS OF -SECRETASE
US6562783B2 (en) 2001-05-30 2003-05-13 Neurologic, Inc. Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors
US7439251B2 (en) 2002-05-03 2008-10-21 Israel Institute For Biological Research Methods and compositions for treatment of central and peripheral nervous system disorders and novel compounds useful therefor
AU2003254844A1 (en) 2002-08-09 2004-02-25 Takeda Chemical Industries, Ltd. Substituted amino compounds and use thereof
JP2004149429A (ja) 2002-10-29 2004-05-27 Takeda Chem Ind Ltd インドール化合物およびその用途
EP1562897B1 (en) 2002-11-12 2009-09-16 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer s disease
EP2335701B1 (en) 2003-12-15 2012-07-11 Schering Corporation Heterocyclic aspartyl protease inhibitors
CA2561267A1 (en) 2004-03-30 2005-10-20 Merck & Co., Inc. 2-aminothiazole compounds useful as aspartyl protease inhibitors
JP2008516946A (ja) 2004-10-15 2008-05-22 アストラゼネカ・アクチエボラーグ 置換されたアミノ−ピリミドンおよびそれらの使用
US20090221579A1 (en) 2004-10-15 2009-09-03 Jeffrey Scott Albert Substituted Amino-Compounds and Uses Thereof
AU2006206654A1 (en) 2005-01-19 2006-07-27 Merck & Co., Inc. Tertiary carbinamines having substituted heterocycles, which are active as inhibitors of beta-secretase, for the treatment of Alzheimer's disease
US8211904B2 (en) * 2005-07-18 2012-07-03 Merck, Sharp & Dohme Corp. Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
US7233721B2 (en) 2005-09-30 2007-06-19 Corning Incorporated Low loss spectrally periodic all-fiber filters
US7303440B2 (en) 2005-10-03 2007-12-04 Stull Michael F Universal battery charger/power source adapter
EP2612854B1 (en) 2005-10-25 2015-04-29 Shionogi&Co., Ltd. Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
US7613617B2 (en) 2006-02-21 2009-11-03 United States Postal Service Systems and methods for managing powered industrial vehicles
WO2008133273A1 (ja) * 2007-04-24 2008-11-06 Shionogi & Co., Ltd. アルツハイマー症治療用医薬組成物
TW200902526A (en) * 2007-04-24 2009-01-16 Shionogi & Amp Co Ltd Aminodihydrothiazin derivative substituted with a cyclic group
ES2548774T3 (es) 2008-01-18 2015-10-20 Eisai R&D Management Co., Ltd. Derivado de aminodihidrotiazina condensado
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
CN102105475B (zh) 2008-07-28 2014-04-09 卫材R&D管理有限公司 螺氨基二氢噻嗪衍生物
WO2010013302A1 (ja) 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体
AU2009300836B2 (en) 2008-09-30 2014-02-27 Eisai R&D Management Co., Ltd. Novel fused aminodihydrothiazine derivative
AR077277A1 (es) 2009-07-09 2011-08-17 Lilly Co Eli Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
GB0912777D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydropyrimidone derivatives
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
BR112013016241A2 (pt) 2011-01-21 2016-07-12 Eisai R&D Man Co Ltd composto, e, método para fabricar um composto
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
JO3143B1 (ar) 2012-04-03 2017-09-20 Lilly Co Eli مركبات تتراهيدرو بيرولو ثيازين

Also Published As

Publication number Publication date
CN101910143B (zh) 2013-08-21
BRPI0906962B8 (pt) 2021-05-25
EP2233474B1 (en) 2015-08-05
CA2711655A1 (en) 2009-07-23
HK1147490A1 (en) 2011-08-12
US20090209755A1 (en) 2009-08-20
HK1147743A1 (en) 2011-08-19
AU2009205072A1 (en) 2009-07-23
US20130203741A1 (en) 2013-08-08
KR101564634B1 (ko) 2015-10-30
PL2233474T3 (pl) 2015-12-31
BRPI0906962A2 (pt) 2015-07-14
AU2009205072B2 (en) 2013-01-24
DK2233474T3 (en) 2015-10-19
EP2233474A1 (en) 2010-09-29
KR20100103702A (ko) 2010-09-27
HUE026064T2 (en) 2016-05-30
NZ586796A (en) 2011-10-28
PE20091438A1 (es) 2009-09-26
RS54311B1 (sr) 2016-02-29
TWI423970B (zh) 2014-01-21
PT2233474E (pt) 2015-10-26
US8158620B2 (en) 2012-04-17
SI2233474T1 (sl) 2015-11-30
JPWO2009091016A1 (ja) 2011-05-26
TW200936581A (en) 2009-09-01
JP4520533B2 (ja) 2010-08-04
ZA201004799B (en) 2011-10-26
EP2233474A4 (en) 2011-11-02
IL206952A (en) 2014-09-30
CN101910143A (zh) 2010-12-08
BRPI0906962B1 (pt) 2020-07-14
US20100317850A1 (en) 2010-12-16
RU2010134403A (ru) 2012-02-27
HRP20151030T1 (hr) 2015-11-06
US8946210B2 (en) 2015-02-03
CY1117014T1 (el) 2017-04-05
IL206952A0 (en) 2010-12-30
US8946211B2 (en) 2015-02-03
CA2711655C (en) 2013-03-05
WO2009091016A1 (ja) 2009-07-23
MY160690A (en) 2017-03-15
RU2476431C2 (ru) 2013-02-27
ES2548774T3 (es) 2015-10-20
AU2009205072C1 (en) 2016-10-13
US20120094984A1 (en) 2012-04-19

Similar Documents

Publication Publication Date Title
MY160690A (en) Condensed aminodihydrothiazine derivative
IN2012DN00688A (uk)
AU2009258496A8 (en) Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
TW200728307A (en) Novel spirochromanone derivatives
TN2014000042A1 (en) Cyclopropaneamine compound
TW200734311A (en) New compounds
AU2002950217A0 (en) 8- Hydroxy Quinoline Derivatives
MY166866A (en) Heterocyclic derivative and pharmaceutical drug
NZ598242A (en) Triazolopyridine compound, and action thereof as prolyl hydroxylase inhibitor and erythropoietin production inducer
UA92083C2 (uk) Азабіциклічні алканові похідні, заміщені конденсованим біциклогетероциклом
MX347706B (es) Derivados de triazol y su uso para trastornos neurologicos.
TW200833675A (en) Nicotinamide derivatives
HUP0303164A2 (hu) Kinazolinok mint MMP-13 gátlók, eljárás az előállításukra, intermedierjeik és a vegyületeket tartalmazó gyógyszerkészítmények
IL198979A (en) Enzyme inhibitors diacylglycerol o-acetyltransferase type 1
MX2012002528A (es) Agente terapeutico para trastornos del estado de animo.
TW200640900A (en) 1-(2h)-isoquinolone derivative
MX2009009238A (es) Nuevos inhibidores de fosfodiesterasa.
WO2011159124A3 (ko) Ｉｎｔｅｒｌｅｕｋｉｎ-６ 억제 작용을 갖는 신규한 벤즈옥사졸 유도체, 이의 제조 방법 및 이를 포함하는 약학적 조성물
MX2009010302A (es) Derivados de indol que tienen actividad inhibidora de cpla2 y aplicaciones y metodos de produccion.
IN2014MN01756A (uk)
TW200640913A (en) 5-Substituted quinoline and isoquinoline derivatives, a process for their production and their use as anti-inflammatory agents
MX2009004884A (es) Derivados 8-piperidinil-2-piridinil-pirimido [1,2-a] pirimidin-6-ona y 8-piperidinil-2-pirimidinil-pirimido [1,2-a] pirimidin-6-ona sustuidos.
TW200621739A (en) Asymmetric synthesis of substituted dihydrobenzofurans
TW200619212A (en) Morpholine derivatives
PL1758852T3 (pl) Podstawione związki cyklopentenu