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

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

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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)

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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)
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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)
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PE (1) PE20191406A1 (ar)
PH (1) PH12019501707A1 (ar)
PL (1) PL3573983T3 (ar)
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UA (1) UA123472C2 (ar)
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WO2016030443A1 (en) 2014-08-28 2016-03-03 Asceneuron Sa Glycosidase inhibitors
KR20180132629A (ko) 2016-02-25 2018-12-12 아셰뉴론 에스아 글리코시다제 저해제
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
ES2879351T3 (es) 2016-02-25 2021-11-22 Asceneuron Sa Sales de derivados de piperazina obtenidas por adición de ácidos
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
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CA3107788A1 (en) * 2018-07-31 2020-02-06 Eli Lilly And Company Combination of anti-tau antibody and oga inhibitor for treatment of diseases characterized by aberrant tau aggregation
US11795165B2 (en) 2018-08-22 2023-10-24 Asceneuron Sa Tetrahydro-benzoazepine glycosidase inhibitors
WO2020039029A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Spiro compounds as glycosidase inhibitors
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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
TW202039482A (zh) 2018-12-05 2020-11-01 美商百健Ｍａ公司 嗎啉基、哌嗪基、氧氮雜環庚烷基及二氮雜環庚烷基o-醣蛋白-2-乙醯胺基-2-去氧-3-d-葡萄哌喃醣苷酶抑制劑
WO2020163193A1 (en) * 2019-02-04 2020-08-13 Biogen Ma Inc. Bicyclic ether o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
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
WO2021123291A1 (en) 2019-12-18 2021-06-24 Janssen Pharmaceutica Nv Oga inhibitor compounds
AU2020409728A1 (en) 2019-12-18 2022-08-11 Janssen Pharmaceutica Nv OGA inhibitor compounds
JP2023507180A (ja) 2019-12-18 2023-02-21 ヤンセン ファーマシューティカ エヌ．ベー． Ｏｇａ阻害剤化合物
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
IL300365A (en) 2020-08-03 2023-04-01 Biogen Ma Inc Crystal forms of O-glycoprotein-2-acetamido-2-deoxy-3-D-glucopyranosidase inhibitor
WO2023070064A1 (en) * 2021-10-22 2023-04-27 Eli Lilly And Company 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

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DK2970272T3 (en) * 2013-03-14 2019-04-23 Merck Patent Gmbh glycosidase
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WO2016030443A1 (en) * 2014-08-28 2016-03-03 Asceneuron Sa Glycosidase inhibitors
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CA3045957A1 (en) * 2016-12-16 2018-06-21 Janssen Pharmaceutica Nv Monocyclic oga inhibitor compounds

Also Published As

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

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