AU2018213029B2 - 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 - Google Patents

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 Download PDF

Info

Publication number
AU2018213029B2
AU2018213029B2 AU2018213029A AU2018213029A AU2018213029B2 AU 2018213029 B2 AU2018213029 B2 AU 2018213029B2 AU 2018213029 A AU2018213029 A AU 2018213029A AU 2018213029 A AU2018213029 A AU 2018213029A AU 2018213029 B2 AU2018213029 B2 AU 2018213029B2
Authority
AU
Australia
Prior art keywords
compound
methyl
pharmaceutically acceptable
acceptable salt
disease
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
AU2018213029A
Other languages
English (en)
Other versions
AU2018213029A1 (en
Inventor
Nicolas Jacques Francois Dreyfus
Peter James LINDSAY-SCOTT
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and 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 Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of AU2018213029A1 publication Critical patent/AU2018213029A1/en
Application granted granted Critical
Publication of AU2018213029B2 publication Critical patent/AU2018213029B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2018213029A 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 Active AU2018213029B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762451137P 2017-01-27 2017-01-27
US62/451,137 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
AU2018213029A1 AU2018213029A1 (en) 2019-07-04
AU2018213029B2 true AU2018213029B2 (en) 2020-11-05

Family

ID=61157343

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2018213029A Active AU2018213029B2 (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

Country Status (36)

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

Families Citing this family (29)

* 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
MX2018010192A (es) 2016-02-25 2019-01-31 Asceneuron S A Inhibidores de glucosidasa.
JP2019506430A (ja) 2016-02-25 2019-03-07 エースニューロン・ソシエテ・アノニム グリコシダーゼ阻害剤
US11261183B2 (en) 2016-02-25 2022-03-01 Asceneuron Sa Sulfoximine glycosidase inhibitors
CA3014572C (en) 2016-02-25 2023-10-03 Asceneuron S.A. Acid addition salts of piperazine derivatives
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
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
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
CA3108158C (en) * 2018-07-31 2023-05-16 Eli Lilly And Company 5-methyl-4-fluoro-thiazol-2-yl compounds
US11795165B2 (en) 2018-08-22 2023-10-24 Asceneuron Sa Tetrahydro-benzoazepine glycosidase inhibitors
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
AU2019324522B2 (en) 2018-08-22 2024-11-14 Asceneuron S. A. Succinate and fumarate acid addition salts of piperazine derivatives useful as glycosidase inhibitors
CN113166137B (zh) 2018-09-19 2024-08-16 比奥根Ma公司 O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂
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
EP3891146B1 (en) * 2018-12-05 2023-09-27 Biogen MA Inc. Morpholinyl, piperazinyl, oxazepanyl and diazepanyl derivatives useful as 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
WO2021123294A1 (en) 2019-12-18 2021-06-24 Janssen Pharmaceutica Nv Oga inhibitor compounds
WO2021123297A1 (en) 2019-12-18 2021-06-24 Janssen Pharmaceutica Nv Oga inhibitor compounds
WO2021123291A1 (en) 2019-12-18 2021-06-24 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
CN116917284A (zh) 2020-08-03 2023-10-20 渤健马萨诸塞州股份有限公司 O-糖蛋白-2-乙酰胺基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂的结晶形式
CA3235104A1 (en) * 2021-10-22 2023-04-27 Kevin BIGLAN O-glcnacase (oga) inhibitor combination therapy
EP4472679A1 (en) 2022-02-03 2024-12-11 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
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014159234A1 (en) * 2013-03-14 2014-10-02 Merck Patent Gmbh Glycosidase inhibitors

Family Cites Families (11)

* 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
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
AU2006331882A1 (en) * 2005-12-21 2007-07-05 Schering Corporation Phenoxypiperidines and analogs thereof useful as histamine H3 antagonists
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
US9732065B2 (en) * 2013-05-30 2017-08-15 Sumitomo Dainippon Pharma Co., Ltd. Cyclic aminomethyl pyrimidine derivative
SG11201701315VA (en) 2014-08-28 2017-03-30 Asceneuron Sa Glycosidase inhibitors
US10913733B2 (en) 2015-12-18 2021-02-09 Alectos Therapeutics Inc. Substituted piperidines thiazolyl acetamides as glycosidase inhibitors and uses thereof
WO2018109202A1 (en) * 2016-12-16 2018-06-21 Janssen Pharmaceutica Nv Monocyclic oga inhibitor compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014159234A1 (en) * 2013-03-14 2014-10-02 Merck Patent Gmbh Glycosidase inhibitors

Also Published As

Publication number Publication date
CO2019007711A2 (es) 2019-07-31
UA123472C2 (uk) 2021-04-07
PT3573983T (pt) 2021-06-17
KR102275338B1 (ko) 2021-07-12
WO2018140299A1 (en) 2018-08-02
IL267693A (en) 2019-08-29
KR20190096421A (ko) 2019-08-19
NZ754849A (en) 2021-10-29
PH12019501707A1 (en) 2020-03-16
JOP20190182A1 (ar) 2019-07-25
CY1124257T1 (el) 2022-07-22
MD3573983T2 (ro) 2021-10-31
US20180215751A1 (en) 2018-08-02
DK3573983T3 (da) 2021-06-28
MX2019008846A (es) 2019-09-10
CA3049141C (en) 2021-02-16
JOP20190182B1 (ar) 2023-03-28
CR20190320A (es) 2019-08-27
DOP2019000187A (es) 2019-08-15
HUE054990T2 (hu) 2021-10-28
EP3573983A1 (en) 2019-12-04
JP2020504142A (ja) 2020-02-06
TW201836607A (zh) 2018-10-16
TWI654978B (zh) 2019-04-01
EA201991515A1 (ru) 2020-01-16
ES2871949T3 (es) 2021-11-02
BR112019013535A2 (pt) 2020-01-07
EP3573983B1 (en) 2021-04-21
CN110198940B (zh) 2022-09-23
HRP20211011T1 (hr) 2021-09-17
MX387166B (es) 2025-03-19
CN110198940A (zh) 2019-09-03
IL267693B (en) 2021-08-31
MY197494A (en) 2023-06-19
AU2018213029A1 (en) 2019-07-04
RS61979B1 (sr) 2021-07-30
PL3573983T3 (pl) 2021-10-04
CL2019001978A1 (es) 2019-12-13
PE20191406A1 (es) 2019-10-04
AR110747A1 (es) 2019-05-02
ZA201904171B (en) 2022-01-26
ECSP19053616A (es) 2019-08-30
CA3049141A1 (en) 2018-08-02
US10081625B2 (en) 2018-09-25
SI3573983T1 (sl) 2021-08-31
EA038368B1 (ru) 2021-08-17
MA47368B1 (fr) 2021-07-29
JP6738970B2 (ja) 2020-08-12
LT3573983T (lt) 2021-07-26

Similar Documents

Publication Publication Date Title
AU2018213029B2 (en) 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
EP3630755B1 (en) 5-methyl-1,3,4-oxadiazol-2-yl compounds
NZ754849B2 (en) 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
HK40009770A (en) 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
HK40009770B (en) 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
CA3108158C (en) 5-methyl-4-fluoro-thiazol-2-yl compounds
BR112019013535B1 (pt) N-4-flúor-5-[[(2s,4s)-2-metil-4-[(5-metil1,2,4-oxadiazol-3-il)metóxi]-1-piperidil]metil]tiazol-2- il]acetamida como inibidor da oga, seu uso, composição farmacêutica e processo para preparação da referida composição
CN118184572A (zh) 一类新型HsClpP激动剂的制备及其在抗炎抗肿瘤中的用途

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)