JOP20190182A1 - أسيتاميد n-] 4-فلور-5-]] (4s,2s)-2-ميثيل-4-](5-ميثيل-1،2،4-اوكسادايزول-3-يل)ميثوكسي[-1-بيبيرديل[ميثيل[ ثيازول-2-يل[ كمثبط oga - Google Patents

أسيتاميد n-] 4-فلور-5-]] (4s,2s)-2-ميثيل-4-](5-ميثيل-1،2،4-اوكسادايزول-3-يل)ميثوكسي[-1-بيبيرديل[ميثيل[ ثيازول-2-يل[ كمثبط oga

Info

Publication number
JOP20190182A1
JOP20190182A1 JOP/2019/0182A JOP20190182A JOP20190182A1 JO P20190182 A1 JOP20190182 A1 JO P20190182A1 JO P20190182 A JOP20190182 A JO P20190182A JO P20190182 A1 JOP20190182 A1 JO P20190182A1
Authority
JO
Jordan
Prior art keywords
methyl
oxadiazol
thiazol
piperidyl
acetamide
Prior art date
Application number
JOP/2019/0182A
Other languages
English (en)
Inventor
Peter James Lindsay-Scott
Nicolas Jacques Francois Dreyfus
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of JOP20190182A1 publication Critical patent/JOP20190182A1/ar
Application granted granted Critical
Publication of JOP20190182B1 publication Critical patent/JOP20190182B1/ar

Links

Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/09—Geometrical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

يوفر الاختراع الحالي مركب له الصيغة I: الصيغة I أو ملح مقبول صيدليًا مما سبق، واستخدام مركبات لها الصيغة I لعلاج أمراض تنكسية عصبية واضطرابات، مثل مرض آلزهايمر.
JOP/2019/0182A 2017-01-27 2018-01-19 أسيتاميد n-] 4-فلور-5-]] (4s,2s)-2-ميثيل-4-](5-ميثيل-1،2،4-اوكسادايزول-3-يل)ميثوكسي[-1-بيبيرديل[ميثيل[ ثيازول-2-يل[ كمثبط oga JOP20190182B1 (ar)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762451137P 2017-01-27 2017-01-27
PCT/US2018/014331 WO2018140299A1 (en) 2017-01-27 2018-01-19 N-[4-fluoro-5-[[(2s,4s)-2-methyl-4-[(5-methyl-1,2,4-oxadiazol-3-yl)methoxy]-1-piperidyl]methyl]thiazol-2-yl]acetamide as oga inhibitor

Publications (2)

Publication Number Publication Date
JOP20190182A1 true JOP20190182A1 (ar) 2019-07-25
JOP20190182B1 JOP20190182B1 (ar) 2023-03-28

Family

ID=61157343

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2019/0182A JOP20190182B1 (ar) 2017-01-27 2018-01-19 أسيتاميد n-] 4-فلور-5-]] (4s,2s)-2-ميثيل-4-](5-ميثيل-1،2،4-اوكسادايزول-3-يل)ميثوكسي[-1-بيبيرديل[ميثيل[ ثيازول-2-يل[ كمثبط oga

Country Status (37)

Country Link
US (1) US10081625B2 (ar)
EP (1) EP3573983B1 (ar)
JP (1) JP6738970B2 (ar)
KR (1) KR102275338B1 (ar)
CN (1) CN110198940B (ar)
AR (1) AR110747A1 (ar)
AU (1) AU2018213029B2 (ar)
BR (1) BR112019013535A2 (ar)
CA (1) CA3049141C (ar)
CL (1) CL2019001978A1 (ar)
CO (1) CO2019007711A2 (ar)
CR (1) CR20190320A (ar)
CY (1) CY1124257T1 (ar)
DK (1) DK3573983T3 (ar)
DO (1) DOP2019000187A (ar)
EA (1) EA038368B1 (ar)
EC (1) ECSP19053616A (ar)
ES (1) ES2871949T3 (ar)
HR (1) HRP20211011T1 (ar)
HU (1) HUE054990T2 (ar)
IL (1) IL267693B (ar)
JO (1) JOP20190182B1 (ar)
LT (1) LT3573983T (ar)
MA (1) MA47368B1 (ar)
MD (1) MD3573983T2 (ar)
MX (1) MX2019008846A (ar)
MY (1) MY197494A (ar)
PE (1) PE20191406A1 (ar)
PH (1) PH12019501707A1 (ar)
PL (1) PL3573983T3 (ar)
PT (1) PT3573983T (ar)
RS (1) RS61979B1 (ar)
SI (1) SI3573983T1 (ar)
TW (1) TWI654978B (ar)
UA (1) UA123472C2 (ar)
WO (1) WO2018140299A1 (ar)
ZA (1) ZA201904171B (ar)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201701315VA (en) 2014-08-28 2017-03-30 Asceneuron Sa Glycosidase inhibitors
JP6971999B2 (ja) 2016-02-25 2021-11-24 エースニューロン・ソシエテ・アノニム ピペラジン誘導体の酸付加塩
US11612599B2 (en) 2016-02-25 2023-03-28 Asceneuron Sa Glycosidase inhibitors
MA43680A (fr) 2016-02-25 2018-11-28 Asceneuron Sa Inhibiteurs de glycosidases
US11261183B2 (en) 2016-02-25 2022-03-01 Asceneuron Sa Sulfoximine glycosidase inhibitors
AR111693A1 (es) 2017-05-25 2019-08-07 Lilly Co Eli Compuestos de 5-metil-1,3,4-oxadiazol-2-ilo con actividad inhibitoria de oga
US11213525B2 (en) 2017-08-24 2022-01-04 Asceneuron Sa Linear glycosidase inhibitors
TWI726329B (zh) 2018-06-22 2021-05-01 美商美國禮來大藥廠 2,3-二氫呋喃并[2,3-b]吡啶化合物
JP7016446B2 (ja) * 2018-07-31 2022-02-04 イーライ リリー アンド カンパニー ５－メチル－４－フルオロ－チアゾール－２－イル化合物
JP2021530552A (ja) * 2018-07-31 2021-11-11 イーライ リリー アンド カンパニー 併用療法
WO2020039028A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Tetrahydro-benzoazepine glycosidase inhibitors
WO2020039029A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Spiro compounds as glycosidase inhibitors
UY38376A (es) * 2018-09-19 2020-04-30 Biogen Ma Inc Inhibidores de o-glicoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidasa
TWI716107B (zh) 2018-09-26 2021-01-11 美商美國禮來大藥廠 6-氟-2-甲基苯并[d]噻唑-5-基化合物
WO2020117961A1 (en) 2018-12-05 2020-06-11 Biogen Ma Inc. Morpholinyl, piperazinyl, oxazepanyl and diazepanyl o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
AR117989A1 (es) * 2019-02-04 2021-09-08 Biogen Ma Inc Inhibidores de o-glucoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidasa de éter bicíclico
WO2021094312A1 (en) 2019-11-11 2021-05-20 Janssen Pharmaceutica Nv Pyrrolidine and bicycloheteroaryl containing oga inhibitor compounds
WO2021110656A1 (en) 2019-12-02 2021-06-10 Janssen Pharmaceutica Nv Oga inhibitor compounds
EP4077323A1 (en) 2019-12-18 2022-10-26 Janssen Pharmaceutica NV Oga inhibitor compounds
WO2021123291A1 (en) 2019-12-18 2021-06-24 Janssen Pharmaceutica Nv Oga inhibitor compounds
EP4076654A1 (en) 2019-12-18 2022-10-26 Janssen Pharmaceutica NV Oga inhibitor compounds
TW202220650A (zh) * 2020-07-23 2022-06-01 美商美國禮來大藥廠 5-甲基-1,2,4-噁二唑-3-基化合物之低劑量療法及調配物
MX2023001469A (es) 2020-08-03 2023-06-16 Biogen Ma Inc Formas cristalinas de un inhibidor de la o-glucoproteina-2-acetami do-2-desoxi-3-d-glucopiranosidasa.
CA3235104A1 (en) * 2021-10-22 2023-04-27 Kevin BIGLAN O-glcnacase (oga) inhibitor combination therapy
WO2023150483A1 (en) 2022-02-03 2023-08-10 Eli Lilly And Company Regional tau imaging for diagnosing and treating alzheimer's disease
WO2024083820A1 (en) 2022-10-18 2024-04-25 Institut National de la Santé et de la Recherche Médicale Method and composition for determining the level of o-glcnacylation in horses

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8726763D0 (en) 1987-11-16 1987-12-23 Fujisawa Pharmaceutical Co Thiazole compounds
BRPI0409211A (pt) 2003-04-18 2006-03-28 Lilly Co Eli composto, composição farmacêutica, métodos para ativar receptores 5-ht1f, para inibir extravasão de proteìna neuronial, e para o tratamento ou prevenção de enxaqueca em um mamìfero, e, uso de um composto
SE0302116D0 (sv) 2003-07-21 2003-07-21 Astrazeneca Ab Novel compounds
KR20080087833A (ko) * 2005-12-21 2008-10-01 쉐링 코포레이션 히스타민 ｈ３ 길항제로서 유용한 페녹시피페리딘 및 이의유사체
US20100063032A1 (en) * 2007-03-28 2010-03-11 Debenham John S Substituted pyrido[2,3-d]pyrimidine derivatives as cannabinoid-1 receptor modulators
TWI431004B (zh) * 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
US9120781B2 (en) 2010-05-11 2015-09-01 Simon Fraser University Selective glycosidase inhibitors and uses thereof
HUE043398T2 (hu) 2013-03-14 2019-08-28 Merck Patent Gmbh Glikozidáz inhibítorok
EP3006438A4 (en) * 2013-05-30 2017-01-18 Sumitomo Dainippon Pharma Co., Ltd. Cyclic aminomethyl pyrimidine derivative
SG11201701315VA (en) * 2014-08-28 2017-03-30 Asceneuron Sa Glycosidase inhibitors
EP3389658B1 (en) 2015-12-18 2020-11-25 Merck Sharp & Dohme Corp. Glycosidase inhibitors and uses thereof
EP3555087A1 (en) * 2016-12-16 2019-10-23 Janssen Pharmaceutica NV Monocyclic oga inhibitor compounds

Also Published As

Publication number Publication date
HRP20211011T1 (hr) 2021-09-17
KR20190096421A (ko) 2019-08-19
MA47368B1 (fr) 2021-07-29
EA201991515A1 (ru) 2020-01-16
CN110198940A (zh) 2019-09-03
PL3573983T3 (pl) 2021-10-04
UA123472C2 (uk) 2021-04-07
JP6738970B2 (ja) 2020-08-12
CY1124257T1 (el) 2022-07-22
MD3573983T2 (ro) 2021-10-31
US10081625B2 (en) 2018-09-25
DK3573983T3 (da) 2021-06-28
LT3573983T (lt) 2021-07-26
ZA201904171B (en) 2022-01-26
MY197494A (en) 2023-06-19
CA3049141C (en) 2021-02-16
US20180215751A1 (en) 2018-08-02
CL2019001978A1 (es) 2019-12-13
TW201836607A (zh) 2018-10-16
CA3049141A1 (en) 2018-08-02
EP3573983B1 (en) 2021-04-21
PT3573983T (pt) 2021-06-17
BR112019013535A2 (pt) 2020-01-07
DOP2019000187A (es) 2019-08-15
CR20190320A (es) 2019-08-27
ECSP19053616A (es) 2019-08-30
CN110198940B (zh) 2022-09-23
IL267693B (en) 2021-08-31
PE20191406A1 (es) 2019-10-04
JP2020504142A (ja) 2020-02-06
JOP20190182B1 (ar) 2023-03-28
SI3573983T1 (sl) 2021-08-31
ES2871949T3 (es) 2021-11-02
EP3573983A1 (en) 2019-12-04
MX2019008846A (es) 2019-09-10
WO2018140299A1 (en) 2018-08-02
RS61979B1 (sr) 2021-07-30
NZ754849A (en) 2021-10-29
PH12019501707A1 (en) 2020-03-16
AU2018213029B2 (en) 2020-11-05
CO2019007711A2 (es) 2019-07-31
TWI654978B (zh) 2019-04-01
EA038368B1 (ru) 2021-08-17
AR110747A1 (es) 2019-05-02
IL267693A (en) 2019-08-29
HUE054990T2 (hu) 2021-10-28
KR102275338B1 (ko) 2021-07-12
AU2018213029A1 (en) 2019-07-04

Similar Documents

Publication Publication Date Title
JOP20190182A1 (ar) أسيتاميد n-] 4-فلور-5-]] (4s,2s)-2-ميثيل-4-](5-ميثيل-1،2،4-اوكسادايزول-3-يل)ميثوكسي[-1-بيبيرديل[ميثيل[ ثيازول-2-يل[ كمثبط oga
NZ712207A (en) Tetrahydropyrrolothiazine compounds
EA201790271A1 (ru) Ингибиторы гликозидазы
EA202190681A1 (ru) Амиды диметиламиноазетидина в качестве jak ингибиторов
EA201790305A1 (ru) КОМБИНИРОВАННАЯ ТЕРАПИЯ БОЛЕЗНИ АЛЬЦГЕЙМЕРА С ИСПОЛЬЗОВАНИЕМ КОМБИНАЦИИ МОНОКЛОНАЛЬНЫХ АНТИТЕЛ К N3pGlu АБЕТА И ИНГИБИТОРА BACE
EA202190686A1 (ru) 5-7-членные гетероциклические амиды в качестве ингибиторов jak
PH12019500569A1 (en) Blood-brain barrier-penetrant dopamine-b-hydroxylase inhibitors
BR112018073951A2 (pt) forma cristalina inovadora de n-[5-(3,5-difluoro-benzil)-1h-indazol-3-il]-4-(4-metil-piperazin-1-il)-2-(tetra-hidro-piran-4-ilamino)-benzamida
SA519401322B1 (ar) مركبات أريل كربوكساميد غير متجانسة كمثطبات لكيناز بروتين سيرين/ ثريونين متداخل مع المستقبل 2
PH12020551297A1 (en) Compounds having s1p5 receptor agonistic activity
NZ631388A (en) Phenyl-urea and phenyl-carbamate derivatives as inhibitors of protein aggregation
EA201892687A1 (ru) Кристаллическая форма соединения, подавляющего активность протеинкиназы, и её применение
TN2017000448A1 (en) Tetrahydrofurane-fused aminohydrothiazine derivatives which are useful in the treatment of alzheimer's disease
EA202190359A1 (ru) Способы лечения нейродегенеративных расстройств
EA201891447A1 (ru) Кристаллическая форма 1,3-тиазол-5-илметил-[(2r,5r)-5-{[(2s)-2-[(метил-{[2-(пропан-2-ил)-1,3-тиазол-4-ил]метил}карбамоил)-мино]-4-(морфолин-4-ил)бутаноил-9-амино}-1,6-дифенилгексан-2-ил]карбамата или кобицистата
EA202190452A1 (ru) Ингибиторы cdk8/19
MA40345B1 (fr) Nouvelle forme polymorphe de chlorhydrate de n-[2-(6-fluoro-1h-indol-3-yl)éthyl]-3-(2,2,3,3-tétrafluoropropoxy) benzylamine pour le de traitement de la maladie d'alzheimer
TH1901004570A (th) N-[4-ฟลูออโร-5-[[(2s,4s)-2-เมธิล-4-[(5-เมธิล-1,2,4-ออกซะไดอะซอล-3-อิล)เมธอกซิ]-1-พิเพอริดิล]เมธิล]ไธอะซอล-2-อิล]แอซิแทมีดในการเป็นสารยับยั้งoga
GB201819758D0 (en) Medicine for the treatment of Alzheimer's disease
ZA202006126B (en) Compounds for treating alzheimer's disease
EA202090241A1 (ru) Новые гетероциклические соединения как ингибиторы cdk8/19
TH167631B (th) วิธีการบำบัดโรคอัลไซเมอร์และองค์ประกอบทางเภสัชกรรมของมัน