HRP20240173T1 - Fluorofenil beta-hidroksietilamini i njihova upotreba u liječenju hiperglikemije - Google Patents

Fluorofenil beta-hidroksietilamini i njihova upotreba u liječenju hiperglikemije Download PDF

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Publication number
HRP20240173T1
HRP20240173T1 HRP20240173TT HRP20240173T HRP20240173T1 HR P20240173 T1 HRP20240173 T1 HR P20240173T1 HR P20240173T T HRP20240173T T HR P20240173TT HR P20240173 T HRP20240173 T HR P20240173T HR P20240173 T1 HRP20240173 T1 HR P20240173T1
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Croatia
Prior art keywords
fluorophenyl
ethan
hyperglycemia
pharmaceutically acceptable
pentan
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HRP20240173TT
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English (en)
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Benjamin Pelcman
Tore Bengtsson
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Atrogi Ab
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Publication of HRP20240173T1 publication Critical patent/HRP20240173T1/hr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/22—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
    • C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
    • C07C215/30—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/68—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings and hydroxy groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/22—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
    • C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
    • C07C215/34—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton and at least one hydroxy group bound to another carbon atom of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/42—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having amino groups or hydroxy groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C215/56—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups
    • C07C215/58—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups with hydroxy groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
    • C07C215/60—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups with hydroxy groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain the chain having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/42—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/43—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/04—Systems containing only non-condensed rings with a four-membered ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (6)

1. Farmaceutski sastav koji sadrži spoj formule IC [image] ili njegovu farmaceutski prihvatljivu sol, i opcionalno jedan ili više farmaceutski prihvatljivih adjuvanasa, razblaživača i/ili nosača, gdje: Y1, Y4 i Y5 svaki predstavljaju H; jedan od Y2 i Y3 predstavlja F i drugi predstavlja H; R1 predstavlja C4-5 alkil; i R2 i R3 oba predstavljaju H, pri čemu alkil grupe mogu biti pravog lanca ili, kada je dovoljan broj atoma ugljika, biti razgranatog lanca, i/ili ciklične ili djelomično ciklične, i kada se spoj nalazi u enantiomernom višku (e.e.) od najmanje 90%.
2. Sastav prema zahtjevu 1, gdje je spoj formule IC odabran iz grupe koja obuhvaća: (R)-2-(butilamino)-1-(4-fluorofenil)etan-1-ol; (R)-2-(butilamino)-1-(3-fluorofenil)etan-1-ol; (R)-2-(terc-butilamino)-1-(3-fluorofenil)etan-1-ol; (R)-1-(4-fluorofenil)-2-(((R)-pentan-2-il)amino)etan-1-ol; (R)-1-(4-fluorofenil)-2-(((S)-pentan-2-il)amino)etan-1-ol; (R)-1-(3-fluorofenil)-2-(((R)-pentan-2-il)amino)etan-1-ol; i (R)-1-(3-fluorofenil)-2-(((S)-pentan-2-il)amino)etan-1-ol, i njihove farmaceutski prihvatljive sol.
3. Farmaceutski sastav kao što je definirano u zahtjevu 1 ili zahtjevu 2 za upotrebu u liječenju hiperglikemije ili poremećaja koji karakterizira hiperglikemija.
4. Sastav za upotrebu prema zahtjevu 3, gdje je: tretman za dijabetes tipa 2, koji po potrebi karakterizira pacijent koji pokazuje tešku inzulinsku otpornost (TIR); ili hiperglikemiju ili poremećaj koji karakterizira hiperglikemija je, ili se karakterizira, pacijentom koji pokazuje tešku inzulinsku otpornost, opcionalno pri čemu se poremećaj bira iz grupe koju čine Rabson-Mendenholov sindrom, Donohueov sindrom (leprehaunizam), tip A i tip B sindromi insulinske otpornosti, sindromi HAIR-AN (hiperandrogenizam, inzulinska otpornost i akantoza (lat. acanthosis nigricans)), pseudoakromegalija i lipodistrofija.
5. Komplet iz djelova koji se sastoji od: (a) farmaceutskog sastava kao što je definirano u patentnom zahtjevu 1 ili patentnom zahtjevu 2, i (b) jednog ili više terapijskog agensa koji je koristan u liječenju hiperglikemije ili poremećaja koji karakterizira hiperglikemija, po potrebi u smjesi sa jednim ili više farmaceutski-prihvatljivih adjuvanasa, razblaživača ili nosača, gdje je svaka od komponenti (a) i (b) osigurana u obliku koji je pogodan za davanje u kombinaciji sa drugom.
6. Spoj formule IC, ili njegova farmaceutski prihvatljiva sol, kao što je definirano u zahtjevu 1 ili zahtjevu 2 za upotrebu u medicini.
HRP20240173TT 2017-09-13 2018-09-13 Fluorofenil beta-hidroksietilamini i njihova upotreba u liječenju hiperglikemije HRP20240173T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1714734.9A GB201714734D0 (en) 2017-09-13 2017-09-13 New compounds and uses
PCT/GB2018/052594 WO2019053426A1 (en) 2017-09-13 2018-09-13 FLUOROPHENYL BETA-HYDROXYETHYLAMINES AND THEIR USE IN THE TREATMENT OF HYPERGLYCEMIA
EP18773825.7A EP3681857B1 (en) 2017-09-13 2018-09-13 Fluorophenyl beta-hydroxyethylamines and their use in the treatment of hyperglycaemia

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HRP20240173T1 true HRP20240173T1 (hr) 2024-04-12

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HRP20240173TT HRP20240173T1 (hr) 2017-09-13 2018-09-13 Fluorofenil beta-hidroksietilamini i njihova upotreba u liječenju hiperglikemije

Country Status (20)

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US (2) US11648216B2 (hr)
EP (2) EP4249054A3 (hr)
JP (2) JP7441784B2 (hr)
KR (1) KR20200051777A (hr)
CN (1) CN111148731A (hr)
AU (2) AU2018332146B2 (hr)
CA (1) CA3075706A1 (hr)
DK (1) DK3681857T3 (hr)
ES (1) ES2966644T3 (hr)
FI (1) FI3681857T3 (hr)
GB (1) GB201714734D0 (hr)
HR (1) HRP20240173T1 (hr)
IL (2) IL296282A (hr)
LT (1) LT3681857T (hr)
MX (2) MX2020002823A (hr)
PL (1) PL3681857T3 (hr)
PT (1) PT3681857T (hr)
RS (1) RS65231B1 (hr)
SI (1) SI3681857T1 (hr)
WO (1) WO2019053426A1 (hr)

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GB201714736D0 (en) 2017-09-13 2017-10-25 Atrogi Ab New compounds and uses
GB201714740D0 (en) 2017-09-13 2017-10-25 Atrogi Ab New compounds and uses
GB201714745D0 (en) 2017-09-13 2017-10-25 Atrogi Ab New compounds and uses
CN111333513B (zh) * 2020-04-17 2021-08-27 江苏恒沛药物科技有限公司 一种2,4-二氟-3-硝基苯甲酸的制备方法
GB202205895D0 (en) * 2022-04-22 2022-06-08 Atrogi Ab New medical uses
CN115010624B (zh) * 2022-07-27 2023-12-22 阿尔塔(天津)标准物质研究院有限公司 一种氘标记西布特罗的制备方法

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