TWI776886B - Sestrin-gator2交互作用之調節劑及其用途 - Google Patents

Sestrin-gator2交互作用之調節劑及其用途 Download PDF

Info

Publication number
TWI776886B
TWI776886B TW107114086A TW107114086A TWI776886B TW I776886 B TWI776886 B TW I776886B TW 107114086 A TW107114086 A TW 107114086A TW 107114086 A TW107114086 A TW 107114086A TW I776886 B TWI776886 B TW I776886B
Authority
TW
Taiwan
Prior art keywords
mmol
acid
solution
mixture
give
Prior art date
Application number
TW107114086A
Other languages
English (en)
Chinese (zh)
Other versions
TW201841629A (zh
Inventor
艾登 薩亞
喬治 維拉蘇克
Original Assignee
美商奈維特製藥公司
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 美商奈維特製藥公司 filed Critical 美商奈維特製藥公司
Publication of TW201841629A publication Critical patent/TW201841629A/zh
Application granted granted Critical
Publication of TWI776886B publication Critical patent/TWI776886B/zh

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/133Amines having hydroxy groups, e.g. sphingosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/136Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/145Amines having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/18Sulfonamides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/192Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/221Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/223Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of alpha-aminoacids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/275Nitriles; Isonitriles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4015Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41521,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/417Imidazole-alkylamines, e.g. histamine, phentolamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/4211,3-Oxazoles, e.g. pemoline, trimethadione
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245Oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4453Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/69Boron compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/695Silicon compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Steroid Compounds (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)
  • Optical Modulation, Optical Deflection, Nonlinear Optics, Optical Demodulation, Optical Logic Elements (AREA)
  • Control Of Indicators Other Than Cathode Ray Tubes (AREA)
TW107114086A 2017-04-26 2018-04-25 Sestrin-gator2交互作用之調節劑及其用途 TWI776886B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762490280P 2017-04-26 2017-04-26
US62/490,280 2017-04-26

Publications (2)

Publication Number Publication Date
TW201841629A TW201841629A (zh) 2018-12-01
TWI776886B true TWI776886B (zh) 2022-09-11

Family

ID=63920059

Family Applications (1)

Application Number Title Priority Date Filing Date
TW107114086A TWI776886B (zh) 2017-04-26 2018-04-25 Sestrin-gator2交互作用之調節劑及其用途

Country Status (10)

Country Link
US (4) US10912750B2 (https=)
EP (2) EP4556069A3 (https=)
JP (1) JP7179015B2 (https=)
CN (2) CN110809467B (https=)
AU (2) AU2018258355B2 (https=)
CA (1) CA3061611A1 (https=)
ES (1) ES3040534T3 (https=)
PL (1) PL3615019T3 (https=)
TW (1) TWI776886B (https=)
WO (1) WO2018200625A1 (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE061437T2 (hu) 2015-10-23 2023-06-28 Navitor Pharm Inc A Sestrin-GATOR2 kölcsönhatás modulátorai és ezek alkalmazásai
US10912750B2 (en) 2017-04-26 2021-02-09 Navitor Pharmaceuticals, Inc. Modulators of Sestrin-GATOR2 interaction and uses thereof
CN113164414A (zh) 2018-10-24 2021-07-23 纳维托制药有限公司 多晶型化合物和其用途
KR102659859B1 (ko) 2018-10-30 2024-04-25 길리애드 사이언시즈, 인코포레이티드 알파4β7 인테그린의 억제를 위한 화합물
AU2019373242B2 (en) 2018-10-30 2023-07-13 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin
EP4541422A3 (en) 2018-10-30 2025-06-25 Gilead Sciences, Inc. Quinoline derivatives as alpha4beta7 integrin inhibitors
CN112969700B (zh) 2018-10-30 2024-08-20 吉利德科学公司 作为α4β7整合素抑制剂的咪唑并吡啶衍生物
CN111689993B (zh) * 2019-03-11 2023-04-14 凯特立斯(深圳)科技有限公司 一种新的含硼类佐米药物关键中间体手性α-氨基硼酸酯的制备方法
KR102908219B1 (ko) 2019-08-14 2026-01-08 길리애드 사이언시즈, 인코포레이티드 알파 4 베타 7 인테그린의 저해용 화합물
CA3156436A1 (en) * 2019-11-01 2021-05-06 Steven LEVENTER Methods of treatment using an mtorc1 modulator
CN113876784B (zh) * 2021-09-27 2023-07-21 潍坊博创国际生物医药研究院 硼代亮氨酸类化合物的新用途
CN115927459A (zh) * 2022-07-19 2023-04-07 华南农业大学 猪ctns基因在促进动物骨骼肌生长中的应用
EP4612120A1 (en) * 2022-11-01 2025-09-10 Navitor Pharmaceuticals, Inc. Modulators of mtorc1 activity and uses thereof
CN120993707B (zh) * 2025-08-18 2026-02-10 衡水海宏环保设备制造有限公司 一种滤饼成型动态压控智能调控方法

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4110368A (en) 1972-07-24 1978-08-29 American Cyanamid Company Hydro substituted prostanoic acids and esters
US4346110A (en) * 1981-06-01 1982-08-24 Merrell Toraude Et Compagnie Method for treating depression
JPS61149964A (ja) 1984-12-25 1986-07-08 Canon Inc 電子写真感光体
US4670196A (en) 1985-09-05 1987-06-02 Norton Company Tower packing element
ES2029799T3 (es) 1986-01-24 1992-10-01 Toray Industries, Inc. Derivados de 2,5,6,7 tetranor-4,8-inter-m-fenilen pg12.
GB8827885D0 (en) 1988-11-30 1989-01-05 Wellcome Found Novel heterocyclic pesticidal compounds
US5639600A (en) 1994-08-05 1997-06-17 The Regents Of The University Of California Diagnosis and treatment of cell proliferative disease having clonal macrophage involvement
DE19623142A1 (de) 1996-06-10 1997-12-11 Huels Chemische Werke Ag Enantiomerenangereicherte, durch einen tertiären Kohlenwasserstoffrest substituierte Malonsäuremonoester sowie deren Herstellung
TR199900399T2 (xx) * 1996-08-28 1999-06-21 The Procter & Gamble Company Matris metaloproteaz inhibit�rleri olarak fosfinik asit amidleri.
US7087648B1 (en) 1997-10-27 2006-08-08 The Regents Of The University Of California Methods for modulating macrophage proliferation using polyamine analogs
US6458781B1 (en) 1998-04-27 2002-10-01 David Thomas Connor Substituted diarylalkyl amides as calcium channel antagonists
KR20010033872A (ko) 1998-11-04 2001-04-25 간디 지오프레이 에이치. 올레핀의 중합을 위한 성분 및 촉매
US6329546B1 (en) 1999-01-12 2001-12-11 Laboratory Of Molecular Biophotonics Caged amino acids
US20030203900A1 (en) 1999-05-18 2003-10-30 Martin Quibell Cysteine protease inhibitors
ES2317839T3 (es) 1999-06-10 2009-05-01 Warner-Lambert Company Llc Acidos 3-propil gamma-aminobutiricos monosustituidos.
AU2002236527A1 (en) * 2000-11-30 2002-06-11 The Health Research Institute Nutrient supplements and methods for treating autism and for preventing the onset of autism
JP5076257B2 (ja) 2001-02-01 2012-11-21 旭硝子株式会社 撥水性組成物、表面処理された基材、その製造方法および輸送機器用物品
EP1389617B1 (en) 2001-04-27 2007-01-03 Zenyaku Kogyo Kabushiki Kaisha Heterocyclic compound and antitumor agent containing the same as active ingredient
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
WO2004019973A1 (en) 2002-08-14 2004-03-11 Atugen Ag Use of protein kinase n beta
US6787664B2 (en) 2002-09-17 2004-09-07 Warner-Lambert Company Llc Process for preparing single enantiomers of 5,5,5,5′,5′,5′-hexafluoroleucine and protected analogs
AU2002953255A0 (en) * 2002-12-11 2003-01-02 Cytopia Research Pty Ltd Protein kinase inhibitors
KR20070087266A (ko) 2003-04-03 2007-08-28 세마포르 파머슈티컬즈, 아이엔씨. 피아이-3 키나아제 억제제 프로드러그
CN1832939B (zh) 2003-05-30 2010-04-28 杰明X医药品加拿大公司 用于治疗癌症或病毒病的三杂环化合物、组合物和方法
US7173015B2 (en) 2003-07-03 2007-02-06 The Trustees Of The University Of Pennsylvania Inhibition of Syk kinase expression
SI2612862T1 (sl) 2004-05-13 2017-04-26 Icos Corporation Kinazolini kot inhibitorji humane fosfatidilinozitol 3-kinaze delta
US20070212428A1 (en) * 2004-06-04 2007-09-13 Mood Management Sciences, Inc. Methods and compositions for treating mood disorder
DE102004053407A1 (de) 2004-11-05 2006-05-11 Bayer Healthcare Ag Acylierte Nonadepsipeptide II
DE602006010979D1 (de) 2005-01-19 2010-01-21 Rigel Pharmaceuticals Inc Prodrugs aus 2,4-pyrimidindiamin-verbindungen und ihre verwendungen
CA2598491A1 (en) 2005-02-18 2006-11-09 Innodia Inc. Diastereoisomers of 4-hydroxyisoleucine and uses thereof
EP1888550B1 (en) 2005-05-12 2014-06-25 AbbVie Bahamas Ltd. Apoptosis promoters
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
US7402325B2 (en) 2005-07-28 2008-07-22 Phoenix Biotechnology, Inc. Supercritical carbon dioxide extract of pharmacologically active components from Nerium oleander
BRPI0617162B8 (pt) 2005-10-07 2021-05-25 Exelixis Inc compostos inibidores de fosfatidilinositol 3-quinase composições farmacêuticas que os contem e métodos de uso dos mesmos
CN103626742B (zh) 2005-11-01 2017-04-26 塔格根公司 激酶的联-芳基间-嘧啶抑制剂
EP2455382B1 (en) 2005-12-13 2016-10-26 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
MX2008013578A (es) 2006-04-26 2009-03-23 Hoffmann La Roche Derivados de tieno [3,2-d]pirimidina utiles como inhibidores de fosfatidilinositol 3-cinasa(p13k).
JP2010501566A (ja) 2006-08-21 2010-01-21 プレクサ ファーマシューティカルズ, インコーポレイテッド 中枢神経系障害の治療において使用するための多伝達物質トランスポータ阻害剤
BRPI0622054B8 (pt) 2006-09-22 2021-05-25 Oxford Amherst Llc composto e composição farmacêutica
KR101336510B1 (ko) 2006-09-25 2013-12-03 욱크하르트 리미티드 치환된 피페리디노페닐 옥사졸리디논
TWI397418B (zh) * 2006-10-10 2013-06-01 Otsuka Pharma Co Ltd 抗憂鬱劑
WO2008051406A2 (en) 2006-10-20 2008-05-02 Merck & Co., Inc. Substituted imidazoles as bombesin receptor subtype-3 modulators
HRP20151386T1 (hr) 2007-03-12 2016-02-26 Ym Biosciences Australia Pty Ltd Fenil aminopirimidinski spojevi i njihova primjena
WO2008118802A1 (en) 2007-03-23 2008-10-02 Regents Of The University Of Minnesota Therapeutic compounds
TW200902019A (en) 2007-04-26 2009-01-16 Ono Pharmaceutical Co Dicyclic heterocyclic compound
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
US8431608B2 (en) 2007-08-17 2013-04-30 Icagen Inc. Heterocycles as potassium channel modulators
US8445686B2 (en) 2007-08-27 2013-05-21 Abbvie Inc. 4-(4-pyridinyl)-benzamides and their use as rock activity modulators
US8158616B2 (en) 2008-03-11 2012-04-17 Incyte Corporation Azetidine and cyclobutane derivatives as JAK inhibitors
US8613951B2 (en) 2008-06-16 2013-12-24 Bind Therapeutics, Inc. Therapeutic polymeric nanoparticles with mTor inhibitors and methods of making and using same
CN102256966B (zh) * 2008-10-17 2016-02-10 白头生物医学研究所 可溶性mTOR复合物和其调节剂
WO2010146172A2 (en) 2009-06-19 2010-12-23 Lek Pharmaceuticals D.D. NEW SYNTHETIC ROUTE FOR THE PREPARATION OF α-AMINO BORONIC ACID DERIVATIVES VIA SUBSTITUTED ALK-1-YNES
US20120219596A1 (en) * 2009-07-30 2012-08-30 Wendelin Stark Injectable formulation for treatment and protection of patients having an inflammatory reaction or an ischemia-reperfusion event
NZ600857A (en) 2010-01-29 2014-06-27 Boehringer Ingelheim Int Substituted naphthyridines and their use as syk kinase inhibitors
WO2012002577A1 (ja) 2010-06-30 2012-01-05 富士フイルム株式会社 新規なニコチンアミド誘導体またはその塩
CN102464701B (zh) 2010-11-08 2015-10-21 上海医药工业研究院 一类新型化合物、其制备方法及用途
WO2012076063A1 (en) 2010-12-10 2012-06-14 Rottapharm S.P.A. Pyridine amide derivatives as ep4 receptor antagonists
WO2012113847A1 (en) 2011-02-25 2012-08-30 Lonza Ltd Branched linker for protein drug conjugates
US9321727B2 (en) 2011-06-10 2016-04-26 Hoffmann-La Roche Inc. Pyridine derivatives as agonists of the CB2 receptor
WO2013052393A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
EP2589383A1 (en) * 2011-11-06 2013-05-08 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Berlin FKBP subtype-specific rapamycin analogue for use in treatment of diseases
WO2013142229A1 (en) 2012-03-19 2013-09-26 President And Fellows Of Harvard College Designing novel peptides for inducing fibronectin matrix assembly
PL2880014T3 (pl) 2012-08-06 2017-10-31 Pitney Pharmaceuticals Pty Ltd Związki do leczenia chorób związanych ze szlakiem mTOR
WO2014127052A1 (en) 2013-02-13 2014-08-21 Zondlo Neal Perfluoro-tert-butyl hydroxyproline
US9650376B2 (en) 2013-03-15 2017-05-16 Knopp Biosciences Llc Imidazo(4,5-B) pyridin-2-yl amides as KV7 channel activators
US20160129030A1 (en) 2013-06-14 2016-05-12 The Brigham And Women's Hospital, Inc. Treatment of mtor hyperactive related diseases and disorders
US10168338B2 (en) * 2014-09-12 2019-01-01 Whitehead Institute For Biomedical Research Methods of identifying modulators of sestrin-gator-2 interaction for modulating mTORC1 activity
HUE061437T2 (hu) 2015-10-23 2023-06-28 Navitor Pharm Inc A Sestrin-GATOR2 kölcsönhatás modulátorai és ezek alkalmazásai
US20180327364A1 (en) 2015-11-13 2018-11-15 Brandeis University Mtor inhibitors and methods of use thereof
NZ748599A (en) 2016-04-21 2022-08-26 Baylor College Medicine Compositions and methods for the treatment of lysosomal storage disorders and disorders characterized by lysosomal dysfunction
US10912750B2 (en) 2017-04-26 2021-02-09 Navitor Pharmaceuticals, Inc. Modulators of Sestrin-GATOR2 interaction and uses thereof
CA3090258A1 (en) 2018-02-08 2019-08-15 Ovid Therapeutics Inc. Use of (1s,3s)-3-amino-4-(difluoromethylidene) cyclopentane-1-carboxylic acid and (s)-3-amino-4-(difluoromethylidene) cyclopentane-1-carboxylic acid and (s)-3-amino-4-(difluoromethylenyl) cyclopent-1-ene-1-carboxylic acid in the treatment of tinnitus and acute sensorineural hearing loss
CN113164414A (zh) 2018-10-24 2021-07-23 纳维托制药有限公司 多晶型化合物和其用途
US10926803B2 (en) 2019-07-17 2021-02-23 GM Global Technology Operations LLC Four rail front crush structure with load dissemination into eight element support structure
CA3156436A1 (en) 2019-11-01 2021-05-06 Steven LEVENTER Methods of treatment using an mtorc1 modulator
JP6689441B1 (ja) 2019-11-01 2020-04-28 エヌ・ティ・ティ・コミュニケーションズ株式会社 電子マネー管理システムおよび電子マネー管理方法

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
期刊 Ignácio, Zuleide M., et al."New perspectives on the involvement of mTOR in depression as well as in the action of antidepressant drugs."British journal of clinical pharmacology 82 .5 2016 1280-1290 *
期刊 Nagamori, Shushi, et al. "Structure–activity relations of leucine derivatives reveal critical moieties for cellular uptake and activation of mTORC1-mediated signaling." Amino Acids 48 .4 2016 1045-1058; *

Also Published As

Publication number Publication date
US20240091184A1 (en) 2024-03-21
CN116370448A (zh) 2023-07-04
CN110809467A (zh) 2020-02-18
AU2018258355B2 (en) 2024-05-30
US10912750B2 (en) 2021-02-09
US11679090B2 (en) 2023-06-20
US12427130B2 (en) 2025-09-30
US20210228523A1 (en) 2021-07-29
WO2018200625A1 (en) 2018-11-01
ES3040534T3 (en) 2025-11-03
EP3615019B1 (en) 2025-06-04
US20180333381A1 (en) 2018-11-22
CN116370448B (zh) 2026-01-13
CA3061611A1 (en) 2018-11-01
CN110809467B (zh) 2023-03-10
JP2020517707A (ja) 2020-06-18
AU2018258355A1 (en) 2019-11-14
EP4556069A2 (en) 2025-05-21
JP7179015B2 (ja) 2022-11-28
EP4556069A3 (en) 2025-08-13
PL3615019T3 (pl) 2026-01-19
TW201841629A (zh) 2018-12-01
AU2024216489A1 (en) 2024-09-19
EP3615019A4 (en) 2021-01-27
US20260034084A1 (en) 2026-02-05
EP3615019A1 (en) 2020-03-04

Similar Documents

Publication Publication Date Title
TWI776886B (zh) Sestrin-gator2交互作用之調節劑及其用途
KR101692275B1 (ko) 2차 구조 안정화된 nmda 수용체 조절제 및 그의 용도
JP6800968B2 (ja) セストリン−gator2相互作用のモジュレーターおよびその使用
KR20150110784A (ko) 스피로-락탐 nmda 수용체 조절인자 및 그의 용도
US10294230B2 (en) 3,3-difluoropiperidine carbamate heterocyclic compounds as NR2B NMDA receptor antagonists
KR20150110586A (ko) 스피로-락탐 nmda 수용체 조절인자 및 그의 용도
CA2906194A1 (en) Benzimidazole derivatives and uses thereof
WO2018053373A1 (en) Uses of satl-inducible kinase (sik) inhibitors for treating osteoporosis
WO2018215557A1 (fr) Composés inhibiteurs des canaux ioniques pour le traitement du cancer
US20230037225A1 (en) SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINES AS APELIN RECEPTOR AGONISTS
JP7102354B2 (ja) 4-(5-(4,7-ジメチルベンゾフラン-2-イル)-1,2,4-オキサジアゾール-3-イル)安息香酸の結晶形態及びそれらの調製方法
CN112218878A (zh) Ntcp抑制剂
JP2026067907A (ja) 神経変性疾患及びミトコンドリア病の治療用の組成物ならびにその使用方法
EA039229B1 (ru) Модуляторы взаимодействия сестрина-gator2 и их применение

Legal Events

Date Code Title Description
GD4A Issue of patent certificate for granted invention patent