ECSP19053616A - N-[4-fluoro-5-[[(2s,4s)-2-metil-4-[(5-metil-1,2,4-oxadiazol-3-il)metoxi]-1-piperidil]metil]tiazol-2-il]acetamida como inhibidor de oga - Google Patents

N-[4-fluoro-5-[[(2s,4s)-2-metil-4-[(5-metil-1,2,4-oxadiazol-3-il)metoxi]-1-piperidil]metil]tiazol-2-il]acetamida como inhibidor de oga

Info

Publication number
ECSP19053616A
ECSP19053616A ECSENADI201953616A ECDI201953616A ECSP19053616A EC SP19053616 A ECSP19053616 A EC SP19053616A EC SENADI201953616 A ECSENADI201953616 A EC SENADI201953616A EC DI201953616 A ECDI201953616 A EC DI201953616A EC SP19053616 A ECSP19053616 A EC SP19053616A
Authority
EC
Ecuador
Prior art keywords
methyl
metoxy
oxadiazol
thiazol
piperidyl
Prior art date
Application number
ECSENADI201953616A
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 ECSP19053616A publication Critical patent/ECSP19053616A/es

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

Abstract

La presente invención proporciona un compuesto de Fórmula I o una sal farmacéuticamente aceptable del mismo, y el uso de compuestos de Fórmula I para el tratamiento de enfermedades y trastornos neurodegenerativos, tales como la enfermedad de Alzheimer.
ECSENADI201953616A 2017-01-27 2019-07-26 N-[4-fluoro-5-[[(2s,4s)-2-metil-4-[(5-metil-1,2,4-oxadiazol-3-il)metoxi]-1-piperidil]metil]tiazol-2-il]acetamida como inhibidor de oga ECSP19053616A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201762451137P 2017-01-27 2017-01-27

Publications (1)

Publication Number Publication Date
ECSP19053616A true ECSP19053616A (es) 2019-08-30

Family

ID=61157343

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSENADI201953616A ECSP19053616A (es) 2017-01-27 2019-07-26 N-[4-fluoro-5-[[(2s,4s)-2-metil-4-[(5-metil-1,2,4-oxadiazol-3-il)metoxi]-1-piperidil]metil]tiazol-2-il]acetamida como inhibidor de oga

Country Status (36)

Country Link
US (1) US10081625B2 (es)
EP (1) EP3573983B1 (es)
JP (1) JP6738970B2 (es)
KR (1) KR102275338B1 (es)
CN (1) CN110198940B (es)
AR (1) AR110747A1 (es)
AU (1) AU2018213029B2 (es)
CA (1) CA3049141C (es)
CL (1) CL2019001978A1 (es)
CO (1) CO2019007711A2 (es)
CR (1) CR20190320A (es)
CY (1) CY1124257T1 (es)
DK (1) DK3573983T3 (es)
DO (1) DOP2019000187A (es)
EA (1) EA038368B1 (es)
EC (1) ECSP19053616A (es)
ES (1) ES2871949T3 (es)
HR (1) HRP20211011T1 (es)
HU (1) HUE054990T2 (es)
IL (1) IL267693B (es)
JO (1) JOP20190182B1 (es)
LT (1) LT3573983T (es)
MA (1) MA47368B1 (es)
MD (1) MD3573983T2 (es)
MX (1) MX387166B (es)
MY (1) MY197494A (es)
PE (1) PE20191406A1 (es)
PH (1) PH12019501707A1 (es)
PL (1) PL3573983T3 (es)
PT (1) PT3573983T (es)
RS (1) RS61979B1 (es)
SI (1) SI3573983T1 (es)
TW (1) TWI654978B (es)
UA (1) UA123472C2 (es)
WO (1) WO2018140299A1 (es)
ZA (1) ZA201904171B (es)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
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
AU2017222964B2 (en) 2016-02-25 2020-01-02 Asceneuron S. A. Glycosidase inhibitors
US11612599B2 (en) 2016-02-25 2023-03-28 Asceneuron Sa Glycosidase inhibitors
EP3585783A2 (en) 2016-02-25 2020-01-01 Asceneuron SA Sulfoximine glycosidase inhibitors
EP3419976B1 (en) 2016-02-25 2021-04-07 Asceneuron SA Acid addition salts of piperazine derivatives
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
EP3672959A1 (en) 2017-08-24 2020-07-01 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
CN112543648A (zh) * 2018-07-31 2021-03-23 伊莱利利公司 组合疗法
CN112469476B (zh) * 2018-07-31 2024-07-16 伊莱利利公司 5-甲基-4-氟-噻唑-2-基化合物
US12016852B2 (en) 2018-08-22 2024-06-25 Asceneuron Sa Pyrrolidine glycosidase inhibitors
US11731972B2 (en) 2018-08-22 2023-08-22 Asceneuron Sa Spiro compounds as glycosidase inhibitors
WO2020039028A1 (en) 2018-08-22 2020-02-27 Asceneuron S. A. Tetrahydro-benzoazepine glycosidase inhibitors
EP3841093B1 (en) 2018-08-22 2023-06-21 Asceneuron SA Succinate and fumarate acid addition salts of piperazine derivatives useful as glycosidase inhibitors
IL315564A (en) * 2018-09-19 2024-11-01 Biogen Ma Inc O-glycoprotein-2-acetamido-2-deoxy-3-D-glucopyranosidase inhibitors
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
AR117252A1 (es) 2018-12-05 2021-07-21 Biogen Ma Inc Inhibidores de o-glucoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidasa de morfolinilo, piperazinilo, oxazepanilo y diazepanilo
JP7504898B2 (ja) * 2019-02-04 2024-06-24 バイオジェン・エムエイ・インコーポレイテッド 二環式エーテル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
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
CN114929337A (zh) 2019-12-18 2022-08-19 詹森药业有限公司 Oga抑制剂化合物
JP2023507184A (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
BR112023002013A2 (pt) 2020-08-03 2023-05-02 Biogen Ma Inc Formas cristalinas de um inibidor de o-glicoproteína-2-acetamido-2-desóxi-3-d-glucopiranosidase
CN118139880A (zh) * 2021-10-22 2024-06-04 伊莱利利公司 O-连接的n-乙酰葡糖胺水解酶(oga)抑制剂联合治疗
JP2025506411A (ja) 2022-02-03 2025-03-11 イーライ リリー アンド カンパニー アルツハイマー病の診断及び治療のための局所タウイメージング
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
WO2025184490A1 (en) * 2024-03-01 2025-09-04 Biogen Ma Inc. N-[4-fluor-5-[[(2s, 4 r)-4-[(6-methoxy-4-pyrimidinyl)oxy]- 2-methyl-1-pyrrolidinyl] methyl ]-2-thiazolyl]acetamid for use in the treatment of alzheimer disease
WO2026021588A1 (zh) * 2024-07-26 2026-01-29 浙江同源康医药股份有限公司 Oga抑制剂及其应用

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
MXPA05011223A (es) 2003-04-18 2006-01-26 Lilly Co Eli Compuestos de (piperidiniloxi)fenilo, (piperidiniloxi)piridinilo, (piperidinilsulfanil)fenilo y (piperidinilsulfanil)piridinilo como agonistas 5-htif.
SE0302116D0 (sv) 2003-07-21 2003-07-21 Astrazeneca Ab Novel compounds
EP1976848A2 (en) * 2005-12-21 2008-10-08 Schering Corporation Phenoxypiperidines and analogs thereof useful as histamine h3 antagonists
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
ES2723883T3 (es) * 2013-03-14 2019-09-03 Merck Patent Gmbh Inhibidores de glicosidasa
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
US10913733B2 (en) 2015-12-18 2021-02-09 Alectos Therapeutics Inc. Substituted piperidines thiazolyl acetamides as glycosidase inhibitors and uses thereof
CN110300752A (zh) * 2016-12-16 2019-10-01 詹森药业有限公司 单环oga抑制剂化合物

Also Published As

Publication number Publication date
CL2019001978A1 (es) 2019-12-13
AR110747A1 (es) 2019-05-02
AU2018213029B2 (en) 2020-11-05
CA3049141A1 (en) 2018-08-02
CY1124257T1 (el) 2022-07-22
SI3573983T1 (sl) 2021-08-31
JOP20190182B1 (ar) 2023-03-28
NZ754849A (en) 2021-10-29
PH12019501707A1 (en) 2020-03-16
HUE054990T2 (hu) 2021-10-28
EP3573983A1 (en) 2019-12-04
CN110198940B (zh) 2022-09-23
WO2018140299A1 (en) 2018-08-02
EA201991515A1 (ru) 2020-01-16
KR20190096421A (ko) 2019-08-19
EP3573983B1 (en) 2021-04-21
RS61979B1 (sr) 2021-07-30
MA47368B1 (fr) 2021-07-29
US10081625B2 (en) 2018-09-25
PT3573983T (pt) 2021-06-17
JP6738970B2 (ja) 2020-08-12
TW201836607A (zh) 2018-10-16
MX387166B (es) 2025-03-19
PL3573983T3 (pl) 2021-10-04
US20180215751A1 (en) 2018-08-02
AU2018213029A1 (en) 2019-07-04
KR102275338B1 (ko) 2021-07-12
CA3049141C (en) 2021-02-16
MY197494A (en) 2023-06-19
EA038368B1 (ru) 2021-08-17
MX2019008846A (es) 2019-09-10
DOP2019000187A (es) 2019-08-15
CN110198940A (zh) 2019-09-03
JP2020504142A (ja) 2020-02-06
JOP20190182A1 (ar) 2019-07-25
MD3573983T2 (ro) 2021-10-31
CO2019007711A2 (es) 2019-07-31
TWI654978B (zh) 2019-04-01
ES2871949T3 (es) 2021-11-02
HRP20211011T1 (hr) 2021-09-17
BR112019013535A2 (pt) 2020-01-07
UA123472C2 (uk) 2021-04-07
IL267693A (en) 2019-08-29
CR20190320A (es) 2019-08-27
IL267693B (en) 2021-08-31
ZA201904171B (en) 2022-01-26
LT3573983T (lt) 2021-07-26
DK3573983T3 (da) 2021-06-28
PE20191406A1 (es) 2019-10-04

Similar Documents

Publication Publication Date Title
MX2019008846A (es) N-[4-fluoro-5-[[(2s,4s)-2-metil-4-[(5-metil-1,2,4-oxadiazol-3-il) metoxi]-1-piperidil]metil]tiazol-2-il] acetamida como inhibidor de oga.
AR111693A1 (es) Compuestos de 5-metil-1,3,4-oxadiazol-2-ilo con actividad inhibitoria de oga
PE20151542A1 (es) Compuestos de tetrahidropirrolotiazina
CY1121062T1 (el) Φαρμακευτικες συνθεσεις για την αντιμετωπιση της νοσου alzheimer
DOP2019000010A (es) Compuesto (r)-n-(5-cloro-1-(3,3-difluoro-1-(oxetan-3-il)piperidin-4-il)-1h-pirazol-4-il)-4-etoxi-7h-pirrolo[2,3-d]pirimidin-2-amina o sal farmacéuticamente aceptable del mismo
PE20141824A1 (es) Compuestos terapeuticamente activos y sus metodos de uso
AR103680A1 (es) Inhibidores selectivos de bace1
CO2017001875A2 (es) Terapia de combinación contra el alzheimer usando anticuerpos anti-n3pglu más un inhibidor bace
MX378160B (es) Moduladores del receptor acoplado a la proteina g 40 (gpr40) de pirrolidina para el tratamiento de enfermedades como la diabetes.
EA201791802A1 (ru) СШИТЫЕ ДИГИДРО-4H-ПИРАЗОЛО[5,1-c][1,4]ОКСАЗИНИЛОВЫЕ СОЕДИНЕНИЯ И АНАЛОГИ ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ ЦНС
MY174747A (en) Bace1 inhibitors
JOP20190049A1 (ar) مثبطات دوبامين-b-هيدروكسيلاز
MX2018014298A (es) Nueva forma cristalina de n-[5-(3,5-difluoro-bencilo)-1h-indazol-3 -il]-4-(4-metilo-piperazina-1-il)-2-(tetrahidro-pirano-4-ilamino) -benzamida.
CU24434B1 (es) Compuestos derivados de n-(1,5-dimetil-3-oxo-2,3-dihidro-1h-pirazol-4-il)-4-metil-5-isoxazol-3-carboxamida activos como inhibidores selectivos de smurf-1
CO2018001383A2 (es) Derivados de n-[piridin-4-il]metil]-4-{(1r)-1-[(3s)-3-metil-2,5-dioxopirrolidin-3-il]etil}benzamida como antagonistas del receptor cgrp”
EA201691160A1 (ru) Антагонисты s1p3
EA201692216A1 (ru) Пирролидиновые модуляторы gpr40 для лечения заболеваний, таких как диабет
EA202190359A1 (ru) Способы лечения нейродегенеративных расстройств
CO2019013254A2 (es) Compuestos bicíclicos 5,6-fusionados y composiciones para el tratamiento de enfermedades parasitarias
CL2017002229A1 (es) Inhibidores de bace1.
CO2020001375A2 (es) Derivado de adamantilmetilamina y uso del mismo como producto farmacéutico
FI3878444T3 (fi) (n-(2-((2-bentsyylifenyyli)amino)-2-oksoetyyli)-l-naftamidi) syöpälääkeaineena
EA201792109A1 (ru) Конденсированные с тетрагидрофураном производные аминогидротиазина, пригодные для лечения болезни альцгеймера
MX375329B (es) 2,2,2-trifluoroetil-tiadiazinas.
EA201692485A1 (ru) Новая полиморфная форма n-[2-(6-фтор-1h-индол-3-ил)этил]-3-(2,2,3,3-тетрафторпропокси)бензиламина гидрохлорида для лечения болезни альцгеймера