MX2016013035A - Derivados de dihidrotiazina y dihidrooxazina que tienen actividad inhibidora de enzima de escision de proteina precursora amiloide 1 en sitio beta (bace1). - Google Patents

Derivados de dihidrotiazina y dihidrooxazina que tienen actividad inhibidora de enzima de escision de proteina precursora amiloide 1 en sitio beta (bace1).

Info

Publication number
MX2016013035A
MX2016013035A MX2016013035A MX2016013035A MX2016013035A MX 2016013035 A MX2016013035 A MX 2016013035A MX 2016013035 A MX2016013035 A MX 2016013035A MX 2016013035 A MX2016013035 A MX 2016013035A MX 2016013035 A MX2016013035 A MX 2016013035A
Authority
MX
Mexico
Prior art keywords
dihydrothiazine
dihydrooxazine
derivatives
substituted
inhibitory activity
Prior art date
Application number
MX2016013035A
Other languages
English (en)
Inventor
Fuchino Kouki
Ichi Kusakabe Ken-
Tadano Genta
Komano Kazuo
Nakahara Kenji
Original Assignee
Shionogi & Co
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 Shionogi & Co filed Critical Shionogi & Co
Publication of MX2016013035A publication Critical patent/MX2016013035A/es

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • 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
    • 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
    • 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
    • C07D413/14Heterocyclic 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
    • 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
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-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)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La presente invención proporciona un compuesto que tiene un efecto de inhibir la producción de amiloide ß, especialmente un efecto de inhibir BACE1, y que es útil como un agente terapéutico o profiláctico para enfermedades inducidas por la producción, secreción y/o deposición de proteínas amiloides ß. Un compuesto de la fórmula (I) (ver Fórmula) en la que X es -S- o -O-, R3a es alquilo, haloalquilo, es alquilo, haloalquilo o similares, R2a es H, halógeno, alquiloxi, haloalquiloxi o similares, R2b es H o similares, R3b es H o alquilo, el anillo A y el anillo B es cada uno independientemente un carbociclo aromático sustituido o no sustituido, un heterociclo aromático sustituido o no sustituido o similares, y es alquilo sustituido o no sustituido o similares, o una sal farmacéuticamente sal aceptable del mismo.
MX2016013035A 2014-04-11 2015-04-10 Derivados de dihidrotiazina y dihidrooxazina que tienen actividad inhibidora de enzima de escision de proteina precursora amiloide 1 en sitio beta (bace1). MX2016013035A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2014081524 2014-04-11
PCT/JP2015/062314 WO2015156421A1 (en) 2014-04-11 2015-04-10 Dihydrothiazine and dihydrooxazine derivatives having bace1 inhibitory activity

Publications (1)

Publication Number Publication Date
MX2016013035A true MX2016013035A (es) 2017-01-09

Family

ID=53284477

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016013035A MX2016013035A (es) 2014-04-11 2015-04-10 Derivados de dihidrotiazina y dihidrooxazina que tienen actividad inhibidora de enzima de escision de proteina precursora amiloide 1 en sitio beta (bace1).

Country Status (15)

Country Link
US (1) US20170073337A1 (es)
EP (1) EP3129370A1 (es)
JP (1) JP2017510587A (es)
KR (1) KR20160141849A (es)
CN (1) CN106414431A (es)
AR (1) AR100049A1 (es)
AU (1) AU2015244702A1 (es)
CA (1) CA2945272A1 (es)
EA (1) EA201692048A1 (es)
IL (1) IL248228A0 (es)
MX (1) MX2016013035A (es)
PH (1) PH12016501891A1 (es)
SG (1) SG11201607999VA (es)
TW (1) TW201623295A (es)
WO (1) WO2015156421A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
CA2903215C (en) 2013-03-08 2021-07-20 Amgen Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
US20170066741A1 (en) 2014-02-19 2017-03-09 H. Lundbeck A/S 2-Amino-3,5,5-Trifluoro-3,4,5,6-Tetrahydropyridines as BACE1 Inhibitors for Treatment of Alzheimer's Disease
US9550762B2 (en) 2014-08-08 2017-01-24 Amgen, Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
EP3271356B1 (en) 2015-03-19 2019-10-16 Eli Lilly and Company Selective bace1 inhibitors
TW201717948A (zh) 2015-08-10 2017-06-01 H 朗德貝克公司 包括給予2-胺基-3,5,5-三氟-3,4,5,6-四氫吡啶的聯合治療
PE20181015A1 (es) 2015-08-12 2018-06-26 H Lundbeck As 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
WO2017061534A1 (en) 2015-10-08 2017-04-13 Shionogi & Co., Ltd. Dihydrothiazine derivatives
JP6616525B2 (ja) * 2016-03-01 2019-12-04 エフ.ホフマン−ラ ロシュ アーゲー Bace1阻害剤
AU2019258575A1 (en) 2018-04-27 2020-10-29 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity
JP7127808B2 (ja) * 2018-05-29 2022-08-30 国立大学法人山口大学 フルオロアルキル基を含有するイミン類の製造方法

Family Cites Families (38)

* 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
WO2006138217A1 (en) 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
EP1942105B8 (en) * 2005-10-25 2014-08-13 Shionogi&Co., Ltd. Aminodihydrothiazine derivative
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
KR20100017255A (ko) 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
EP2360155A4 (en) 2008-10-22 2012-06-20 Shionogi & Co 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT
JPWO2010113848A1 (ja) 2009-03-31 2012-10-11 塩野義製薬株式会社 Bace1阻害作用を有するイソチオウレア誘導体またはイソウレア誘導体
JPWO2011058763A1 (ja) 2009-11-13 2013-03-28 塩野義製薬株式会社 アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体
JP5554346B2 (ja) 2009-12-09 2014-07-23 塩野義製薬株式会社 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物
WO2011070781A1 (ja) 2009-12-09 2011-06-16 塩野義製薬株式会社 置換アミノチアジン誘導体
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
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
WO2011071109A1 (ja) 2009-12-11 2011-06-16 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
JPWO2011077726A1 (ja) 2009-12-24 2013-05-02 塩野義製薬株式会社 4−アミノ−1,3−チアジンまたはオキサジン誘導体
CA2816285A1 (en) 2010-10-29 2012-05-03 Shionogi & Co., Ltd. Naphthyridine derivative
JP5766198B2 (ja) 2010-10-29 2015-08-19 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
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
US8754075B2 (en) 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
JPWO2012147762A1 (ja) 2011-04-26 2014-07-28 塩野義製薬株式会社 ピリジン誘導体およびそれを含有するbace1阻害剤
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
JP2012250933A (ja) 2011-06-03 2012-12-20 Shionogi & Co Ltd オキサジン誘導体を含有するアルツハイマー症治療用または予防用医薬組成物
KR20140041590A (ko) 2011-06-07 2014-04-04 에프. 호프만-라 로슈 아게 [1,3]옥사진
WO2012168164A1 (en) * 2011-06-07 2012-12-13 F. Hoffmann-La Roche Ag Halogen-alkyl-1,3 oxazines as bace1 and/or bace2 inhibitors
UY34278A (es) 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
US8476264B2 (en) 2011-09-21 2013-07-02 Hoffmann-La Roche Inc. N-(3-(2-amino-6,6-difluoro-4,4A,5,6,7,7A-hexahydro-cyclopenta[E][1,3]oxazin-4-yl)-phenylamides as BACE1 inhibitors
CN104066727B (zh) 2012-01-26 2019-04-26 霍夫曼-拉罗奇有限公司 氟甲基-5,6-二氢-4h-[1,3]噁嗪类
CN104470915B (zh) 2012-06-26 2019-07-26 霍夫曼-拉罗奇有限公司 作为bace1抑制剂的二氟-六氢-环戊二烯并噁嗪基类和二氟-六氢-苯并噁嗪基类
WO2014010748A1 (en) 2012-07-10 2014-01-16 Shionogi & Co., Ltd. Cyclopropane derivative having bace1 inhibiting activity
JP2014101354A (ja) 2012-10-24 2014-06-05 Shionogi & Co Ltd Bace1阻害作用を有するオキサジン誘導体
WO2014065434A1 (en) * 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
JP2014101353A (ja) 2012-10-26 2014-06-05 Shionogi & Co Ltd オキサジン誘導体を含有するアルツハイマー症治療用または予防用医薬組成物
WO2014098831A1 (en) 2012-12-19 2014-06-26 Bristol-Myers Squibb Company 4,6-diarylaminothiazines as bace1 inhibitors and their use for the reduction of beta-amyloid production
CN104968660A (zh) 2013-01-22 2015-10-07 霍夫曼-拉罗奇有限公司 作为bace1抑制剂的氟-[1,3]噁嗪类化合物
EP2961749B1 (en) 2013-03-01 2019-10-09 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
MA38556A1 (fr) 2013-04-11 2017-09-29 Hoffmann La Roche Inhibiteurs de bace1

Also Published As

Publication number Publication date
KR20160141849A (ko) 2016-12-09
CA2945272A1 (en) 2015-10-15
EP3129370A1 (en) 2017-02-15
CN106414431A (zh) 2017-02-15
JP2017510587A (ja) 2017-04-13
PH12016501891A1 (en) 2016-12-19
IL248228A0 (en) 2016-11-30
EA201692048A1 (ru) 2017-04-28
SG11201607999VA (en) 2016-10-28
WO2015156421A1 (en) 2015-10-15
TW201623295A (zh) 2016-07-01
AR100049A1 (es) 2016-09-07
AU2015244702A1 (en) 2016-10-06
US20170073337A1 (en) 2017-03-16

Similar Documents

Publication Publication Date Title
PH12016501891A1 (en) Dihydrothiazine and dihydrooxazine derivatives having bace1 inhibitory activity
MX2022011029A (es) Compuestos de arilo, heteroarilo y heterociclicos para el tratamiento de trastornos medicos.
MX2017008417A (es) Procedimientos para preparar inhibidores de cinasa 1 reguladora de señal de apoptosis (ask1).
SA518400547B1 (ar) مشتقات بيرازولو بيريميدين كمثبط كيناز
MY153621A (en) Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
PH12017502171A1 (en) PYRIDO[3,4-d]PYRIMIDINE DERIVATIVE AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
MX2023001876A (es) Derivados de rapamicina.
MX2016017147A (es) Compuestos de indazole substituidos como inhibidores de irak4.
TW201613872A (en) IRAK4 inhibiting agents
MX2015012822A (es) 3-pirimidin-4-il-oxazolidin-2-onas- como inhibidores del idh mutante.
PH12021550388A1 (en) Process for preparing jak inhibitors and intermediates thereof
PH12017550004A1 (en) Heterocyclic derivatives and use thereof
PH12017501160A1 (en) 5-[(piperazin-1-yl)-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as adamts inhibitors for the treatment of osteoarthritis
MX2015015168A (es) Derivados heterociclicos y sus usos.
PH12017502260A1 (en) Tricyclic compounds and their use as phosphodiesterase inhibitors
MX2015011180A (es) Derivados de aril sulfamida y sulfamato como moduladores del receptor huerfano relacionado con el receptor del retinoide (porc).
PH12016501461A1 (en) 5-biphenyl-4-heteroarylcarbonylamino-pentanoic acid derivatives as neprilysin inhibitors
PH12016501941B1 (en) Use of heterocyclic compounds for controlling nematodes
PH12016501846A1 (en) Tricyclic compound and jack inhibitor
PH12019501171A1 (en) Pyrido [3, 4-d] pyrimidine derivative and pharmaceutically acceptable salt thereof
MX2019001228A (es) Metodo de produccion del compuesto de pirazol-amida.
MX2018011592A (es) Compuesto que tiene actividad inhibitoria de idh mutante, metodo de preparacion y usos del mismo.
TN2013000074A1 (en) Fused triazoles for the treatment or prophylaxis of mild cognitive impairment