JOP20190182B1 - 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 ogaInfo
- Publication number
- JOP20190182B1 JOP20190182B1 JOP/2019/0182A JOP20190182A JOP20190182B1 JO P20190182 B1 JOP20190182 B1 JO P20190182B1 JO P20190182 A JOP20190182 A JO P20190182A JO P20190182 B1 JOP20190182 B1 JO P20190182B1
- Authority
- JO
- Jordan
- Prior art keywords
- methyl
- oxadiazol
- thiazol
- piperidyl
- acetamide
- Prior art date
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
- 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
- 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
- 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.
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 JOP20190182A1 (ar) | 2019-07-25 |
JOP20190182B1 true 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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
BR112017003658B1 (pt) | 2014-08-28 | 2022-12-06 | Asceneuron Sa | Composto, mistura, método para inibição de uma glicosidase, e, composição farmacêutica |
MA43677A (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 |
CN109071526B (zh) | 2016-02-25 | 2023-02-28 | 阿森纽荣股份公司 | 哌嗪衍生物的酸加成盐 |
AU2017222964B2 (en) | 2016-02-25 | 2020-01-02 | Asceneuron S. A. | Glycosidase inhibitors |
TWI669302B (zh) | 2017-05-25 | 2019-08-21 | 美商美國禮來大藥廠 | 5-甲基-1,3,4-<img align="absmiddle" height="18px" width="27px" file="d10999.TIF" alt="其他非圖式 ed10999.png" img-content="tif" orientation="portrait" inline="yes" giffile="ed10999.png"></img>二唑-2-基化合物 |
WO2019037860A1 (en) | 2017-08-24 | 2019-02-28 | Asceneuron S.A. | LINEAR INHIBITORS OF GLYCOSIDASE |
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 |
WO2020028115A1 (en) * | 2018-07-31 | 2020-02-06 | Eli Lilly And Company | 5-methyl-4-fluoro-thiazol-2-yl compounds |
EP3829634A1 (en) | 2018-07-31 | 2021-06-09 | Eli Lilly and Company | Combination therapy |
US11731972B2 (en) | 2018-08-22 | 2023-08-22 | Asceneuron Sa | Spiro compounds as glycosidase inhibitors |
US11795165B2 (en) | 2018-08-22 | 2023-10-24 | Asceneuron Sa | Tetrahydro-benzoazepine glycosidase inhibitors |
BR112021004739A2 (pt) | 2018-09-19 | 2021-06-01 | Biogen Ma Inc. | inibidores de o-glicoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidase |
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 |
JP2022510430A (ja) | 2018-12-05 | 2022-01-26 | バイオジェン・エムエイ・インコーポレイテッド | モルホリニル、ピペラジニル、オキサゼパニル及びジアゼパニルo-糖タンパク質-2-アセトアミド-2-デオキシ-3-d-グルコピラノシダーゼ阻害剤 |
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 |
IL293931A (en) | 2019-12-18 | 2022-08-01 | Janssen Pharmaceutica Nv | oga inhibitor compounds |
CA3160367A1 (en) | 2019-12-18 | 2021-06-24 | Jose Manuel Bartolome-Nebreda | Oga inhibitor compounds |
WO2021123291A1 (en) | 2019-12-18 | 2021-06-24 | Janssen Pharmaceutica Nv | Oga inhibitor compounds |
AR123031A1 (es) | 2020-07-23 | 2022-10-26 | Lilly Co Eli | Régimen de dosis baja y formulación de un compuesto 5-metil-1,2,4-oxadiazol-3-ilo |
US20230286972A1 (en) | 2020-08-03 | 2023-09-14 | Biogen Ma Inc. | Crystaline forms of an 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 |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
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GB8726763D0 (en) | 1987-11-16 | 1987-12-23 | Fujisawa Pharmaceutical Co | Thiazole compounds |
ES2388547T3 (es) | 2003-04-18 | 2012-10-16 | Eli Lilly And Company | Compuestos de (piperidiniloxi)fenilo, (piperidiniloxi)piridinilo, (piperidinilsulfanil)fenilo y (piperidinilsulfanil)piridinilo como agonistas de 5-HT 1F |
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 |
WO2008121257A1 (en) * | 2007-03-28 | 2008-10-09 | Merck & Co., Inc. | 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 |
AU2014241065B2 (en) * | 2013-03-14 | 2017-08-31 | Merck Patent Gmbh | Glycosidase inhibitors |
US9732065B2 (en) * | 2013-05-30 | 2017-08-15 | Sumitomo Dainippon Pharma Co., Ltd. | Cyclic aminomethyl pyrimidine derivative |
BR112017003658B1 (pt) * | 2014-08-28 | 2022-12-06 | Asceneuron Sa | Composto, mistura, método para inibição de uma glicosidase, e, composição farmacêutica |
WO2017106254A1 (en) | 2015-12-18 | 2017-06-22 | Merck Sharp & Dohme Corp. | Glycosidase inhibitors and uses thereof |
US20200079766A1 (en) * | 2016-12-16 | 2020-03-12 | Janssen Pharmaceutica Nv | Monocyclic oga inhibitor compounds |
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2018
- 2018-01-12 AR ARP180100080A patent/AR110747A1/es unknown
- 2018-01-12 TW TW107101135A patent/TWI654978B/zh active
- 2018-01-19 PT PT187031547T patent/PT3573983T/pt unknown
- 2018-01-19 BR BR112019013535-9A patent/BR112019013535A2/pt active Search and Examination
- 2018-01-19 EP EP18703154.7A patent/EP3573983B1/en active Active
- 2018-01-19 AU AU2018213029A patent/AU2018213029B2/en active Active
- 2018-01-19 ES ES18703154T patent/ES2871949T3/es active Active
- 2018-01-19 DK DK18703154.7T patent/DK3573983T3/da active
- 2018-01-19 EA EA201991515A patent/EA038368B1/ru unknown
- 2018-01-19 CR CR20190320A patent/CR20190320A/es unknown
- 2018-01-19 MD MDE20191326T patent/MD3573983T2/ro unknown
- 2018-01-19 CN CN201880008537.9A patent/CN110198940B/zh active Active
- 2018-01-19 PE PE2019001459A patent/PE20191406A1/es unknown
- 2018-01-19 MA MA47368A patent/MA47368B1/fr unknown
- 2018-01-19 US US15/874,947 patent/US10081625B2/en active Active
- 2018-01-19 RS RS20210757A patent/RS61979B1/sr unknown
- 2018-01-19 KR KR1020197021750A patent/KR102275338B1/ko active IP Right Grant
- 2018-01-19 SI SI201830274T patent/SI3573983T1/sl unknown
- 2018-01-19 CA CA3049141A patent/CA3049141C/en active Active
- 2018-01-19 MX MX2019008846A patent/MX2019008846A/es unknown
- 2018-01-19 HU HUE18703154A patent/HUE054990T2/hu unknown
- 2018-01-19 JP JP2019537118A patent/JP6738970B2/ja active Active
- 2018-01-19 LT LTEP18703154.7T patent/LT3573983T/lt unknown
- 2018-01-19 UA UAA201907115A patent/UA123472C2/uk unknown
- 2018-01-19 MY MYPI2019004268A patent/MY197494A/en unknown
- 2018-01-19 JO JOP/2019/0182A patent/JOP20190182B1/ar active
- 2018-01-19 WO PCT/US2018/014331 patent/WO2018140299A1/en active Application Filing
- 2018-01-19 PL PL18703154T patent/PL3573983T3/pl unknown
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2019
- 2019-06-26 ZA ZA2019/04171A patent/ZA201904171B/en unknown
- 2019-06-27 IL IL267693A patent/IL267693B/en unknown
- 2019-07-12 CL CL2019001978A patent/CL2019001978A1/es unknown
- 2019-07-18 DO DO2019000187A patent/DOP2019000187A/es unknown
- 2019-07-18 CO CONC2019/0007711A patent/CO2019007711A2/es unknown
- 2019-07-25 PH PH12019501707A patent/PH12019501707A1/en unknown
- 2019-07-26 EC ECSENADI201953616A patent/ECSP19053616A/es unknown
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2021
- 2021-06-10 CY CY20211100516T patent/CY1124257T1/el unknown
- 2021-06-28 HR HRP20211011TT patent/HRP20211011T1/hr unknown
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