HK1147490A1 - Condensed aminodihydrothiazine derivative - Google Patents

Condensed aminodihydrothiazine derivative

Info

Publication number
HK1147490A1
HK1147490A1 HK11101641.8A HK11101641A HK1147490A1 HK 1147490 A1 HK1147490 A1 HK 1147490A1 HK 11101641 A HK11101641 A HK 11101641A HK 1147490 A1 HK1147490 A1 HK 1147490A1
Authority
HK
Hong Kong
Prior art keywords
hydrogen atom
independently
ring
inhibitory effect
aryl group
Prior art date
Application number
HK11101641.8A
Other languages
English (en)
Inventor
Yuichi Suzuki
Takafumi Motoki
Toshihiko Kaneko
Mamoru Takaishi
Tasuku Ishida
Paschalis Dimopoulos
Kunitoshi Takeda
Yoichi Kita
Noboru Yamamoto
Afzal Khan
Original Assignee
Eisai R&D Man Co Ltd
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=HK1147490(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Eisai R&D Man Co Ltd filed Critical Eisai R&D Man Co Ltd
Publication of HK1147490A1 publication Critical patent/HK1147490A1/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D279/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/041,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/081,3-Thiazines; Hydrogenated 1,3-thiazines condensed with carbocyclic rings or ring systems
    • 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
    • A61K31/54Heterocyclic 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
    • A61K31/542Heterocyclic 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
    • 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
    • A61P25/28Drugs 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-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)
HK11101641.8A 2008-01-18 2011-02-18 Condensed aminodihydrothiazine derivative HK1147490A1 (en)

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
HK1147490A1 true HK1147490A1 (en) 2011-08-12

Family

ID=40885398

Family Applications (2)

Application Number Title Priority Date Filing Date
HK11101641.8A HK1147490A1 (en) 2008-01-18 2011-02-18 Condensed aminodihydrothiazine derivative
HK11101751.4A HK1147743A1 (zh) 2008-01-18 2011-02-23 稠合氨基二氫噻嗪衍生物

Family Applications After (1)

Application Number Title Priority Date Filing Date
HK11101751.4A HK1147743A1 (zh) 2008-01-18 2011-02-23 稠合氨基二氫噻嗪衍生物

Country Status (27)

Country Link
US (4) US20100317850A1 (zh)
EP (1) EP2233474B1 (zh)
JP (1) JP4520533B2 (zh)
KR (1) KR101564634B1 (zh)
CN (1) CN101910143B (zh)
AU (1) AU2009205072C1 (zh)
BR (1) BRPI0906962B8 (zh)
CA (1) CA2711655C (zh)
CY (1) CY1117014T1 (zh)
DK (1) DK2233474T3 (zh)
ES (1) ES2548774T3 (zh)
HK (2) HK1147490A1 (zh)
HR (1) HRP20151030T1 (zh)
HU (1) HUE026064T2 (zh)
IL (1) IL206952A (zh)
MY (1) MY160690A (zh)
NZ (1) NZ586796A (zh)
PE (1) PE20091438A1 (zh)
PL (1) PL2233474T3 (zh)
PT (1) PT2233474E (zh)
RS (1) RS54311B1 (zh)
RU (1) RU2476431C2 (zh)
SI (1) SI2233474T1 (zh)
TW (1) TWI423970B (zh)
UA (1) UA101352C2 (zh)
WO (1) WO2009091016A1 (zh)
ZA (1) ZA201004799B (zh)

Families Citing this family (136)

* 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
KR20080029965A (ko) 2005-06-14 2008-04-03 쉐링 코포레이션 아스파르틸 프로테아제 억제제
KR20080028881A (ko) 2005-06-14 2008-04-02 쉐링 코포레이션 헤테로사이클릭 아스파르틸 프로테아제 억제제, 이의제조방법 및 용도
CN103936690B (zh) 2005-10-25 2016-06-08 盐野义制药株式会社 氨基二氢噻嗪衍生物
AR061264A1 (es) 2006-06-12 2008-08-13 Schering Corp Inhibidores de aspartil-proteasas derivados de pirimidina, composiciones farmaceuticas que los contienen y usos para tratar enfermedades cognitivas o neurodegenerativas, y como inhibidores del virus vih.
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
KR20100017255A (ko) 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
PL2233474T3 (pl) 2008-01-18 2015-12-31 Eisai R&D Man Co Ltd Skondensowana pochodna aminodihydrotiazyny
MX2010011563A (es) 2008-04-22 2010-11-12 Schering Corp Compuestos 2-imino-3-metil pirrolo pirimidinona fenil-sustituidos como inhibidores de enzima de escision de proteina precursora amiloide sitio beta-1, composiciones y su uso.
NZ589590A (en) 2008-06-13 2012-05-25 Shionogi & Co Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
WO2010013794A1 (en) 2008-07-28 2010-02-04 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
ES2459195T3 (es) * 2008-09-11 2014-05-08 Amgen Inc. Compuestos de anillo espiro-tetracíclico como moduladores de beta-secretasa y métodos de uso
RU2503681C2 (ru) * 2008-09-30 2014-01-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Новое конденсированное производное аминодигидротиазина
AR073406A1 (es) 2008-09-30 2010-11-03 Eisai R&D Man Co Ltd Aminodihidrotiazinas fusionadas con tetrahidropiranos,inhibidoras de bace1 y de la produccion de abeta amiloide, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de enfermedades neurodegenerativas,tales como alzheimer.
US8703785B2 (en) 2008-10-22 2014-04-22 Shionogi & Co., Ltd. 2-aminopyrimidin-4-one and 2-aminopyridine derivatives both having BACE1-inhibiting activity
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
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace 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
US8569310B2 (en) 2009-10-08 2013-10-29 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use
EP2500344A4 (en) 2009-11-13 2013-05-01 Shionogi & Co AMINOTHIAZIN OR AMINOOXAZINE DERIVATIVES WITH AN AMINO TERMINATION
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
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
AU2010328975B2 (en) 2009-12-11 2015-01-22 Shionogi & Co. Ltd. Oxazine derivative
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
PE20121640A1 (es) 2009-12-31 2012-12-17 Novartis Ag Derivados de pirazina como inhibidores de bace
JP5584352B2 (ja) 2010-03-15 2014-09-03 アムジエン・インコーポレーテツド β−セクレターゼ調節剤としてのアミノ−ジヒドロオキサジン系およびアミノ−ジヒドロチアジン系スピロ化合物ならびにそれらの医学的用途
EP2547685A1 (en) 2010-03-15 2013-01-23 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
SG178311A1 (en) 2010-07-13 2012-03-29 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
EP2601197B1 (en) 2010-08-05 2014-06-25 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
WO2012057247A1 (ja) 2010-10-29 2012-05-03 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
AU2011321427A1 (en) 2010-10-29 2013-05-02 Shionogi & Co., Ltd. Naphthyridine 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
MX2013008111A (es) 2011-01-12 2013-10-30 Novartis Ag Derivados de oxazina y su uso en el tratamiento de transtornos neurologicos.
JP5715710B2 (ja) 2011-01-13 2015-05-13 ノバルティス アーゲー 新規複素環誘導体および神経障害の処置におけるそれらの使用
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
US8426584B2 (en) 2011-01-21 2013-04-23 Eisai R&D Management Co., Ltd. Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
WO2012109165A1 (en) 2011-02-07 2012-08-16 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
WO2012112462A1 (en) 2011-02-15 2012-08-23 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
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
WO2012138590A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. Pyrrolidine-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
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
CA2844988A1 (en) 2011-08-22 2013-02-28 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono- and dioxides as bace inhibitors, compositions, and their use
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
AU2013211646B2 (en) 2012-01-26 2017-09-14 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
CA2871264A1 (en) * 2012-04-27 2013-10-31 Eisai R&D Management Co., Ltd. Method for producing 5-(difluoromethyl)pyrazine-2-carboxilic acid and production intermediate thereof
WO2013164730A1 (en) 2012-05-04 2013-11-07 Pfizer Inc. Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2.
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
WO2014045162A1 (en) 2012-09-20 2014-03-27 Pfizer Inc. ALKYL-SUBSTITUTED HEXAHYDROPYRANO[3,4-d] [1,3]THIAZIN-2-ANIME COMPOUNDS
US9540359B2 (en) 2012-10-24 2017-01-10 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity
US9328124B2 (en) 2012-10-26 2016-05-03 Eli Lilly And Company 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
EP2931731A1 (en) 2012-12-11 2015-10-21 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
JP2016507551A (ja) * 2013-02-13 2016-03-10 ファイザー・インク ヘテロアリール置換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
US9233981B1 (en) 2013-02-15 2016-01-12 Pfizer Inc. Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
TW201446758A (zh) 2013-03-01 2014-12-16 Amgen Inc 作爲β-分泌酶抑制劑的全氟化5,6-二氫-4H-1,3-□-2-胺化合物及其用途
KR20150124985A (ko) 2013-03-08 2015-11-06 암젠 인크 베타-세크레타제 억제제로서 퍼플루오르화된 사이클로프로필 융합된 1,3-옥사진-2-아민 화합물 및 그의 사용 방법
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
MY174747A (en) 2013-04-11 2020-05-13 Hoffmann La Roche Bace1 inhibitors
TWI639607B (zh) * 2013-06-18 2018-11-01 美國禮來大藥廠 Bace抑制劑
US9096615B2 (en) 2013-07-30 2015-08-04 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof
TWI684452B (zh) * 2014-03-14 2020-02-11 美國禮來大藥廠 胺基噻嗪化合物
MD20160105A2 (ro) 2014-04-10 2017-03-31 Pfizer Inc. 2-Amino-6-metil-4,4a,5,6-tetrahidropirano[3,4-d][1,3]tiazin-8a(8H)-il-1,3-tiazol-4-il amide
CN106795147B (zh) 2014-08-08 2020-09-22 美国安进公司 作为β-分泌酶抑制剂的环丙基稠合噻嗪-2-胺化合物和使用方法
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
AU2015329027B2 (en) * 2014-10-10 2020-04-30 Eisai R&D Management Co., Ltd. Pharmaceutical composition of fused aminodihydrothiazine derivative
TWI574969B (zh) * 2015-01-30 2017-03-21 美國禮來大藥廠 甲苯磺酸鹽
AR103680A1 (es) * 2015-02-23 2017-05-24 Lilly Co Eli Inhibidores selectivos de bace1
US9938266B2 (en) 2015-03-19 2018-04-10 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
US10246429B2 (en) 2015-08-06 2019-04-02 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
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
AU2016325665A1 (en) 2015-09-24 2018-03-08 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
JP2018534251A (ja) 2015-09-24 2018-11-22 ファイザー・インク Bace阻害剤として有用なn−[2−(3−アミノ−2,5−ジメチル−1,1−ジオキシド−5,6−ジヒドロ−2h−1,2,4−チアジアジン−5−イル)−1,3−チアゾール−4−イル]アミド
MA52119A (fr) 2015-10-19 2018-08-29 Ncyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
EP3875459B1 (en) 2015-10-30 2023-12-13 Neurocrine Biosciences, Inc. Valbenazine dihydrochloride salts and polymorphs thereof
SG11201804152RA (en) 2015-11-19 2018-06-28 Incyte Corp Heterocyclic compounds as immunomodulators
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
TW201726623A (zh) * 2015-12-17 2017-08-01 英塞特公司 作為免疫調節劑之雜環化合物
EP4292650A3 (en) 2015-12-22 2024-02-28 Incyte Corporation Heterocyclic compounds as immunomodulators
US10160757B2 (en) 2015-12-23 2018-12-25 Neuroscrine Biosciences, Inc. Synthetic methods for preparation of (S)-(2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl 2-amino-3-methylbutanoate di(4-methylbenzenesulfonate)
TW201740954A (zh) * 2016-03-16 2017-12-01 美國禮來大藥廠 組合療法
AR108396A1 (es) 2016-05-06 2018-08-15 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
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
CN109641052A (zh) * 2016-08-18 2019-04-16 伊莱利利公司 BACE-1抑制剂和抗-N3pGlu Aβ抗体的组合疗法
US20180057486A1 (en) 2016-08-29 2018-03-01 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
US20200299411A9 (en) * 2016-10-27 2020-09-24 Eisai R&D Management Co., Ltd. Composition and method for treating alzheimer's disease
EP3555085B1 (en) 2016-12-15 2020-12-02 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
MX2019007104A (es) 2016-12-15 2019-11-05 Amgen Inc Derivados de dioxido de 1,4-tiazina y dioxido de 1,2,4-tiadiazina como inhibidores de beta-secretasa y metodos de uso.
MA54100A (fr) 2016-12-15 2021-10-20 Amgen Inc Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
CA3047285A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
CA3047286A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
US10308644B2 (en) 2016-12-22 2019-06-04 Incyte Corporation Heterocyclic compounds as immunomodulators
US20180179201A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
PL3558990T3 (pl) 2016-12-22 2022-12-19 Incyte Corporation Pochodne tetrahydroimidazo[4,5-c]pirydyny jako induktory internalizacji pd-l1
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
EA201991780A1 (ru) 2017-01-27 2021-10-26 Нейрокрин Байосайенсиз, Инк. Способы введения некоторых vmat2-ингибиторов
IL273300B2 (en) 2017-09-21 2024-06-01 Neurocrine Biosciences Inc High dose valbenazine formulation and related preparations, methods and kits
JP2021502959A (ja) 2017-10-10 2021-02-04 ニューロクライン バイオサイエンシーズ,インコーポレイテッド 特定のvmat2インヒビターを投与するための方法
US10993941B2 (en) 2017-10-10 2021-05-04 Neurocrine Biosciences, Inc. Methods for the administration of certain VMAT2 inhibitors
WO2019191707A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Heterocyclic compounds as immunomodulators
DK3790877T3 (da) 2018-05-11 2023-04-24 Incyte Corp Tetrahydro-imidazo[4,5-c]pyridinderivater som pd-l1-immunmodulatorer
EP3826674A2 (en) 2018-07-24 2021-06-02 Eisai R&D Management Co., Ltd. Methods of treatment and prevention of alzheimer's disease
JP2021528481A (ja) 2018-08-15 2021-10-21 ニューロクライン バイオサイエンシーズ,インコーポレイテッド 特定のvmat2阻害剤を投与するための方法
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
US11753406B2 (en) 2019-08-09 2023-09-12 Incyte Corporation Salts of a PD-1/PD-L1 inhibitor
US10940141B1 (en) 2019-08-23 2021-03-09 Neurocrine Biosciences, Inc. Methods for the administration of certain VMAT2 inhibitors
KR20220075382A (ko) 2019-09-30 2022-06-08 인사이트 코포레이션 면역조절제로서의 피리도[3,2-d]피리미딘 화합물
BR112022009031A2 (pt) 2019-11-11 2022-10-11 Incyte Corp Sais e formas cristalinas de um inibidor de pd-1/pd-l1
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
AU2021373044A1 (en) 2020-11-06 2023-06-08 Incyte Corporation Process for making a pd-1/pd-l1 inhibitor and salts and crystalline forms thereof
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

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3227713A (en) * 1966-01-04 Azine derivatives
US3235551A (en) 1966-02-15 Novel derivatives of
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
KR20020097484A (ko) * 2000-05-19 2002-12-31 다케다 야쿠힌 고교 가부시키가이샤 β-씨크리타아제 억제제
US6562783B2 (en) 2001-05-30 2003-05-13 Neurologic, Inc. Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors
NZ560368A (en) 2002-05-03 2008-11-28 Israel Inst Biolog Res Methods and compostions for treatment of central and peripheral nervous system disorders and novel compounds useful therefor
WO2004014843A1 (ja) 2002-08-09 2004-02-19 Takeda Chemical Industries, Ltd. 置換アミノ化合物およびその用途
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
ATE443043T1 (de) 2002-11-12 2009-10-15 Merck & Co Inc Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer
PT1699455E (pt) 2003-12-15 2013-08-27 Merck Sharp & Dohme Inibidores de protease de aspartilo heterocíclicos
AU2005230878A1 (en) 2004-03-30 2005-10-20 Merck & Co., Inc. 2-aminothiazole compounds useful as aspartyl protease inhibitors
CN101084198A (zh) 2004-10-15 2007-12-05 阿斯利康(瑞典)有限公司 取代的氨基-嘧啶酮及其用途
CN101084199A (zh) 2004-10-15 2007-12-05 阿斯利康(瑞典)有限公司 取代的氨基化合物及其用途
US8338614B2 (en) * 2005-01-19 2012-12-25 Merck, Sharp & Dohme Corp. Tertiary carbinamines having substituted heterocycles which are active as β-secretase inhibitors for the treatment of alzheimer's disease
ATE550338T1 (de) 2005-07-18 2012-04-15 Merck Sharp & Dohme Spiropiperidininhibitoren von beta-secretase zur behandlung von alzheimer-krankheit
JP2007049532A (ja) * 2005-08-11 2007-02-22 Seiko Epson Corp ハンドスキャナ、ハンドスキャナの制御方法及びその制御プログラム
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
CN103936690B (zh) 2005-10-25 2016-06-08 盐野义制药株式会社 氨基二氢噻嗪衍生物
WO2007097767A2 (en) 2006-02-21 2007-08-30 United States Postal Service Systems and methods for creating on-demand routes for powered industrial vehicles
KR20100017255A (ko) * 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
EP2151435A4 (en) * 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
PL2233474T3 (pl) * 2008-01-18 2015-12-31 Eisai R&D Man Co Ltd Skondensowana pochodna aminodihydrotiazyny
TWI431004B (zh) * 2008-05-02 2014-03-21 Lilly Co Eli Bace抑制劑
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
WO2010013794A1 (en) 2008-07-28 2010-02-04 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
AR073406A1 (es) * 2008-09-30 2010-11-03 Eisai R&D Man Co Ltd Aminodihidrotiazinas fusionadas con tetrahidropiranos,inhibidoras de bace1 y de la produccion de abeta amiloide, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de enfermedades neurodegenerativas,tales como alzheimer.
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
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
US8426584B2 (en) 2011-01-21 2013-04-23 Eisai R&D Management Co., Ltd. Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
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

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