HRP20240162T1 - Kristalna sol epinefrin malonata - Google Patents

Kristalna sol epinefrin malonata Download PDF

Info

Publication number
HRP20240162T1
HRP20240162T1 HRP20240162TT HRP20240162T HRP20240162T1 HR P20240162 T1 HRP20240162 T1 HR P20240162T1 HR P20240162T T HRP20240162T T HR P20240162TT HR P20240162 T HRP20240162 T HR P20240162T HR P20240162 T1 HRP20240162 T1 HR P20240162T1
Authority
HR
Croatia
Prior art keywords
pharmaceutical preparation
epinephrine
preparation according
epinephrine malonate
butanol
Prior art date
Application number
HRP20240162TT
Other languages
English (en)
Inventor
Jean-Pierre Sommadossi
Adel Moussa
Original Assignee
Biothea Pharma, Inc.
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 Biothea Pharma, Inc. filed Critical Biothea Pharma, Inc.
Publication of HRP20240162T1 publication Critical patent/HRP20240162T1/hr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46Compounds 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
    • C07C215/56Compounds 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
    • C07C215/58Compounds 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
    • C07C215/60Compounds 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
    • 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
    • A61K31/137Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/08Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02Dicarboxylic acids
    • C07C55/08Malonic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)

Claims (26)

1. Sol epinefrin malonata u kristalnom obliku.
2. Sol epinefrin malonata prema patentnom zahtjevu 1, naznačena time što kristalni oblik ima spektar rendgenske difrakcije praha koji ima jedan ili više pikova izraženih kao 2 teta na otprilike 12.1843, 13.4653, 14.2595, 14.6991, 15.8664, 17.3570, 17.9004, 19.5883, 20.4659, 21.5801, 22.3908, 22.9301, 23.8776, 24.6585, 25.3418, 26.0105, 26.4829, 25.3418, 26.0105, 26.4829, 27.2385, 27.8939, 29.4741, 33.2425, 34.2629, 34.8439.
3. Farmaceutski pripravak koji sadrži sol epinefrin malonata i farmaceutski prihvatljiv nosač.
4. Farmaceutski pripravak prema patentnom zahtjevu 3, naznačen time što je farmaceutski pripravak pogodan za oralnu, rektalnu, intraželučanu, topikalnu, intrakranijalnu, intranazalnu i parenteralnu primjenu.
5. Farmaceutski pripravak prema patentnom zahtjevu 3, naznačen time što je farmaceutski pripravak pogodan za sublingvalnu ili bukalnu primjenu.
6. Farmaceutski pripravak prema patentnom zahtjevu 5, naznačen time što farmaceutski pripravak sadrži punilo i sredstvo za raspadanje.
7. Farmaceutski pripravak prema patentnom zahtjevu 6, naznačen time što punilo je mikrokristalna celuloza i sredstvo za raspadanje je unakrsno vezani polivinil polipirolidon.
8. Farmaceutski pripravak prema patentnom zahtjevu 7, naznačen time što je punilo prisutno u količini od 20 do 30 težinskih % i sredstvo za raspadanje je prisutno u količini od 5 do 15 težinskih %.
9. Farmaceutski pripravak prema patentnom zahtjevu 8, koji dodatno sadrži lubrikant i klizajuće sredstvo.
10. Farmaceutski pripravak prema patentnom zahtjevu 9, naznačen time što je lubrikant magnezij stearat i klizajuće sredstvo je silicij dioksid.
11. Farmaceutski pripravak prema patentnom zahtjevu 10, koji dodatno sadrži razrjeđivač.
12. Farmaceutski pripravak prema patentnom zahtjevu 11, naznačen time što razrjeđivač je manitol.
13. Farmaceutski pripravak prema patentnom zahtjevu 12, koji dodatno sadrži limunsku kiselinu.
14. Farmaceutski pripravak prema patentnom zahtjevu 5, naznačen time što pripravak sadrži količinu od 0.3 do 10 mg slobodne baze epinefrina.
15. Farmaceutski pripravak prema patentnom zahtjevu 5, naznačen time što se farmaceutski pripravak raspada za manje od ili jednako 30 sekundi.
16. Postupak za proizvodnju soli epinefrin malonata, naznačen time što navedeni postupak sadrži: dodavanje malonske kiseline u otopinu koja sadrži epinefrin i rastvarač; miješanje otopine; i taloženje soli epinefrin malonata iz otopine.
17. Postupak prema patentnom zahtjevu 16, koji dodatno sadrži talog.
18. Postupak prema patentnom zahtjevu 17, koji dodatno sadrži sušenje taloga.
19. Postupak prema patentnom zahtjevu 16, naznačen time što se malonska kiselina dodaje u odnosu od 0.01:1 do 3:1 u odnosu na epinefrin.
20. Postupak prema patentnom zahtjevu 16, naznačen time što je otapalo izabrano iz grupe koja se sastoji od metanola, etanola, n-propanola, izo-propanola, n-butanola, sek-butanola, terc-butanola, n-pentanola, 2-metil-butanola, 3-metil-butanola i heksanola.
21. Postupak prema patentnom zahtjevu 20, naznačen time što otapalo je etanol.
22. Epinefrin malonat za uporabu u liječenju alergijskog stanja.
23. Epinefrin malonat za uporabu prema patentnom zahtjevu 22, naznačen time što se epinefrin malonat primjenjuje oralno, rektalno, intraželučano, topikalno, intrakranijalno, intranazalno ili parenteralno.
24. Epinefrin malonat za uporabu prema patentnom zahtjevu 22, naznačen time što se epinefrin malonat primjenjuje putem bukalne ili sublingvalne tablete.
25. Epinefrin malonat za uporabu prema patentnom zahtjevu 22, naznačen time što je alergijsko stanje izabrano iz grupe koja se sastoji od anafilakse, astme ili bronhijalne astme.
26. Epinefrin malonat za uporabu prema patentnom zahtjevu 25, naznačen time što alergijsko stanje je anafilaksa.
HRP20240162TT 2018-07-30 2019-07-29 Kristalna sol epinefrin malonata HRP20240162T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201862711936P 2018-07-30 2018-07-30
US201862731442P 2018-09-14 2018-09-14
EP19845343.3A EP3829551B1 (en) 2018-07-30 2019-07-29 Crystalline epinephrine malonate salt
PCT/US2019/043856 WO2020028215A1 (en) 2018-07-30 2019-07-29 Crystalline epinephrine malonate salt

Publications (1)

Publication Number Publication Date
HRP20240162T1 true HRP20240162T1 (hr) 2024-04-12

Family

ID=69179001

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20240162TT HRP20240162T1 (hr) 2018-07-30 2019-07-29 Kristalna sol epinefrin malonata

Country Status (17)

Country Link
US (3) US10995059B2 (hr)
EP (1) EP3829551B1 (hr)
JP (1) JP2021532161A (hr)
KR (1) KR20210057022A (hr)
CN (1) CN112739334A (hr)
AU (1) AU2019313324A1 (hr)
BR (1) BR112021001525A2 (hr)
CA (1) CA3123928C (hr)
HR (1) HRP20240162T1 (hr)
IL (1) IL280448A (hr)
MX (1) MX2021001249A (hr)
PL (1) PL3829551T3 (hr)
RS (1) RS65138B1 (hr)
SG (1) SG11202100749UA (hr)
TW (1) TWI819045B (hr)
WO (1) WO2020028215A1 (hr)
ZA (2) ZA202100765B (hr)

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2332075A (en) 1940-05-24 1943-10-19 Wilson & Co Inc Epinephrine derivative and preparation thereof
US2469967A (en) 1946-04-17 1949-05-10 Armour & Co Cyclopentano perhydrophenanthrene compounds
US2602818A (en) * 1949-07-25 1952-07-08 Parke Davis & Co Process for the purification of epinephrine
CN1406126A (zh) * 1998-10-01 2003-03-26 诺瓦提斯公司 新型缓释口服制剂
LT1531794T (lt) * 2002-06-28 2017-08-25 Civitas Therapeutics, Inc. Inhaliuojamas epinefrinas
TW200800142A (en) 2005-09-09 2008-01-01 Univ Manitoba Fast-disintegrating epinephrine tablets for buccal or sublingual administration
FR2891459B1 (fr) 2005-09-30 2007-12-28 Flamel Technologies Sa Microparticules a liberation modifiee d'au moins un principe actif et forme galenique orale en comprenant
WO2009004593A2 (en) * 2007-07-03 2009-01-08 Wockhardt Research Centre Processes for the preparation of epinephrine
WO2015054359A1 (en) * 2013-10-08 2015-04-16 Ebadi Mark A Methods and compositions for symptomatic reflief of the common cold
US10039710B2 (en) 2015-09-18 2018-08-07 Insys Development Company, Inc. Epinephrine spray formulations
BR112018013979A2 (pt) * 2016-01-07 2018-12-11 Viramal Ltd composições em gel para liberação transdérmica para maximizar as concentrações de fármacos no estrato córneo e no soro e métodos de uso dos mesmos

Also Published As

Publication number Publication date
CA3123928A1 (en) 2020-02-06
ZA202201224B (en) 2023-11-29
US20230086578A1 (en) 2023-03-23
US11505521B2 (en) 2022-11-22
CA3123928C (en) 2023-11-14
PL3829551T3 (pl) 2024-04-02
EP3829551A1 (en) 2021-06-09
CN112739334A (zh) 2021-04-30
EP3829551C0 (en) 2024-01-03
ZA202100765B (en) 2022-08-31
KR20210057022A (ko) 2021-05-20
IL280448A (en) 2021-03-25
TW202010491A (zh) 2020-03-16
AU2019313324A1 (en) 2021-02-04
JP2021532161A (ja) 2021-11-25
RS65138B1 (sr) 2024-02-29
US10995059B2 (en) 2021-05-04
EP3829551A4 (en) 2022-04-20
BR112021001525A2 (pt) 2021-04-20
US20200031758A1 (en) 2020-01-30
SG11202100749UA (en) 2021-02-25
US20210214301A1 (en) 2021-07-15
EP3829551B1 (en) 2024-01-03
MX2021001249A (es) 2021-05-27
WO2020028215A1 (en) 2020-02-06
TWI819045B (zh) 2023-10-21

Similar Documents

Publication Publication Date Title
JP2018516883A5 (hr)
JP2018035160A5 (hr)
PE20231301A1 (es) Formulaciones del esteroide c21-n-pirazolilo 19-nor c3,3-disustituido y metodos de uso de este
SI2760821T1 (en) A salt salt of an anti-inflammatory substituted cyclobutenedione compound
JP2015514060A5 (hr)
JP2015518885A5 (hr)
CA2713292A1 (en) Delayed release rasagiline formulation
JP2009513604A5 (hr)
JP2007533687A5 (hr)
DE22154751T1 (de) Tetrahydrobiopterin zur behandlung von zuständen, welche mit erhöhten phenylalanin-spiegeln einhergehen
MXPA03006974A (es) Indanil aminas aciladas y su uso como farmacos.
JP2009541334A5 (hr)
CA2777824A1 (en) Derivatives of purine or deazapurine useful for the treatment of (inter alia) viral infections
JP2009534312A5 (hr)
WO2002066480A3 (en) 2-arylamino-pyrimidines for the treatment of gsk3-related disorders
JP2007532560A5 (hr)
JP2014511374A5 (hr)
JP2019509268A5 (hr)
JP2014198723A5 (hr)
JP2018529742A5 (hr)
JP2010514807A5 (hr)
WO2017021921A1 (en) Process for the preparation of pharmaceutical grade ferric citrate
MX2021003945A (es) Compuestos de indolinona para uso como inhibidores de map4k1.
PH12020551488A1 (en) Novel calcium salt polymorphs as anti-inflammatory, immunomodulatory and anti-proliferatory agents
JP2021073257A5 (hr)