HRP20240255T1 - Ketamin pamoat i njegova uporaba - Google Patents

Ketamin pamoat i njegova uporaba Download PDF

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Publication number
HRP20240255T1
HRP20240255T1 HRP20240255TT HRP20240255T HRP20240255T1 HR P20240255 T1 HRP20240255 T1 HR P20240255T1 HR P20240255T T HRP20240255T T HR P20240255TT HR P20240255 T HRP20240255 T HR P20240255T HR P20240255 T1 HRP20240255 T1 HR P20240255T1
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HR
Croatia
Prior art keywords
ketamine
pamoate salt
pharmaceutical preparation
xrpd pattern
pamoate
Prior art date
Application number
HRP20240255TT
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English (en)
Inventor
Tong-Ho Lin
Yung-Shun WEN
Chia-Hsien Chen
Wei-Ju Chang
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Alar Pharmaceuticals 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.)
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Publication date
Application filed by Alar Pharmaceuticals Inc. filed Critical Alar Pharmaceuticals Inc.
Publication of HRP20240255T1 publication Critical patent/HRP20240255T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C225/00Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/20Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00Compounds containing amino groups bound to a carbon skeleton
    • C07C211/33Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/34Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton
    • C07C211/35Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing only non-condensed rings
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/01Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
    • C07C65/105Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
    • C07C65/11Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic with carboxyl groups on a condensed ring system containing two rings
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/16Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • C07C69/94Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring of polycyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of six-membered aromatic rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (12)

1. Pamoatna sol ketamina naznačena time što ima stehiometriju od 2:1 ketamina prema pamoatu.
2. Pamoatna sol ketamina u skladu sa patentnim zahtjevom 1, naznačena time što je: pamoatna sol R, S-ketamina predstavljena pomoću formule (I) u nastavku: [image] pamoatna sol S-ketamina predstavljena pomoću formule (II) u nastavku: [image] ili pamoatna sol R-ketamina predstavljena pomoću formule (III) u nastavku: [image]
3. Pamoatna sol ketamina u skladu sa patentnim zahtjevom 1, naznačena time što je amorfna.
4. Pamoatna sol ketamina u skladu sa patentnim zahtjevom 1, naznačena time što je kristalna i ima obrazac difrakcije rendgenskih zraka na prahu (XRPD) koji sadrži jednu ili više 2θ vrijednosti ± 0.2 2θ koje su odabrane od 6.0, 10.7, 11.6, 12.0, 13.0, 14.7, 15.0, 19.6, 22.2, 25.2 i 30.3.
5. Pamoatna sol ketamina u skladu sa patentnim zahtjevom 2, naznačena time što je pamoatna sol R, S-ketamina kristalna i ima XRPD obrazac koji je predstavljen pomoću najmanje jednog od sljedećih: (i) XRPD obrazac koji sadrži jednu ili više 2θ vrijednosti ± 0.2 2θ koje su odabrane od 6.0, 8.6, 10.7, 11.6, 12.0, 13.0, 14.7, 15.0, 15.3, 17.9, 18.6, 19.6, 20.0, 21.1, 21.6, 22.2, 23.3, 24.4, 25.2, 25.9, 26.9, 28.6, 29.7, 30.3, 32.4, 34.0 i 36.6; i (ii) XRPD obrazac koji je pokazan na SL. 2A.
6. Pamoatna sol ketamina u skladu sa patentnim zahtjevom 2, naznačena time što je pamoatna sol S-ketamina kristalna i ima specifičnu rotaciju [image] 6. i XRPD obrazac koji je predstavljen pomoću najmanje jednog od sljedećih: (i) XRPD obrazac koji sadrži jednu ili više 2θ vrijednosti ± 0.2 2θ koje su odabrane od 6.0, 10.8, 11.7, 12.0, 12.6, 13.1, 14.6, 15.1, 18.2, 19.2, 19.7, 20.1, 22.0, 22.8, 23.3, 23.7, 24.1, 24.7, 25.2, 27.3, 30.1, 31.6, 45.4, 56.4 i 75.2; i (ii) XRPD obrazac koji je pokazan na SL. 2B.
7. Pamoatna sol ketamina u skladu sa patentnim zahtjevom 2, naznačena time što je pamoatna sol R-ketamina kristalna i ima specifičnu rotaciju [image] 7. i XRPD obrazac koji je predstavljen pomoću najmanje jednog od sljedećih: (i) XRPD obrazac koji sadrži jednu ili više 2θ vrijednosti ± 0.2 2θ koje su odabrane od 6.0, 10.8, 11.7, 12.0, 12.6, 13.1, 14.6, 15.0, 18.2, 19.3, 19.7, 20.6, 22.0, 22.9, 23.6, 24.1, 24.7, 25.2, 25.9, 27.3, 30.1, 31.6, 45.4, 56.4 i 75.2; i (ii) XRPD obrazac koji je pokazan na SL. 2C.
8. Pamoatna sol ketamina u skladu sa bilo kojim od patentnih zahtjeva 1 do 7, naznačena time što ima čistoću veću od 95%.
9. Farmaceutski pripravak za uporabu u liječenju bolesti centralnog nervnog sistema (CNS), koji sadrži primjenu subjektu kojem je to potrebno efikasne količine farmaceutskog pripravka, naznačeno time što farmaceutski pripravak sadrži pamoatnu sol ketamina u skladu sa bilo kojim od patentnih zahtjeva 1 do 8 i njen farmaceutski prihvatljiv ekscipijens.
10. Farmaceutski pripravak za uporabu u skladu sa patentnim zahtjevom 9, naznačen time što je bolest CNS odabrana iz grupe koja se sastoji od velikog depresivnog poremećaja (MDD), MDD sa neposrednim rizikom od suicidalnih ideja, depresije rezistentne na terapiju (TRD), bipolarnog poremećaja, opsesivno-kompulzivnog poremećaja, posttraumatskog stresnog poremećaja (PTSD), poremećaja iz spektra autizma, tinitusa, refraktorne kronične migrene, astme, anksioznosti, poremećaja uporabe supstanci, poremećaja uporabe alkohola, poremećaja u ishrani, refraktornog status epilepticus, ishemije mozga, Alzheimerove bolesti, Parkinsonove bolesti, moždanog udara, traumatske povrede mozga, multiple skleroze, i bola.
11. Farmaceutski pripravak za uporabu u anesteziranju subjekta kojem je to potrebno, koji sadrži primjenu subjektu efikasne količine farmaceutskog pripravka, naznačen time što farmaceutski pripravak sadrži pamoatnu sol ketamina u skladu sa bilo kojim od patentnih zahtjeva 1 do 8 i njen farmaceutski prihvatljiv ekscipijens.
12. Farmaceutski pripravak za uporabu u skladu sa bilo kojim od patentnih zahtjeva 9 do 11, naznačen time što liječenje bolesti CNS ili anestezija počinje unutar 24 sata i traje najmanje 10 dana poslije primjene farmaceutskog pripravka.
HRP20240255TT 2019-01-11 2020-01-10 Ketamin pamoat i njegova uporaba HRP20240255T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962791058P 2019-01-11 2019-01-11
US201962871763P 2019-07-09 2019-07-09
PCT/CN2020/071404 WO2020143762A1 (en) 2019-01-11 2020-01-10 Ketamine pamoate and use thereof
EP20739053.5A EP3908570B1 (en) 2019-01-11 2020-01-10 Ketamine pamoate and use thereof

Publications (1)

Publication Number Publication Date
HRP20240255T1 true HRP20240255T1 (hr) 2024-05-24

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US (1) US11981617B2 (hr)
EP (1) EP3908570B1 (hr)
JP (1) JP7451538B2 (hr)
KR (1) KR20210116517A (hr)
CN (1) CN113423686B (hr)
AU (1) AU2020206826B2 (hr)
BR (1) BR112021013340A2 (hr)
CA (1) CA3118954A1 (hr)
CL (1) CL2021001803A1 (hr)
CO (1) CO2021006884A2 (hr)
DK (1) DK3908570T3 (hr)
ES (1) ES2974259T3 (hr)
FI (1) FI3908570T3 (hr)
HR (1) HRP20240255T1 (hr)
LT (1) LT3908570T (hr)
MX (1) MX2021006029A (hr)
PE (1) PE20211550A1 (hr)
PH (1) PH12021551157A1 (hr)
PT (1) PT3908570T (hr)
RS (1) RS65271B1 (hr)
SG (1) SG11202104792SA (hr)
SI (1) SI3908570T1 (hr)
TW (1) TWI827783B (hr)
WO (1) WO2020143762A1 (hr)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3753557A4 (en) 2018-02-15 2021-12-01 National University Corporation Chiba University PREVENTIVE OR THERAPEUTIC AGENT AND PHARMACEUTICAL COMPOSITION FOR INFLAMMATORY DISEASES OR BONE DISEASES
CN118121577A (zh) 2018-05-04 2024-06-04 感知神经科学公司 治疗物质滥用的方法
EP4076410A4 (en) * 2019-12-20 2024-02-07 Alar Pharmaceuticals Inc. LONG-ACTING INJECTABLE FORMULATIONS OF KETAMINE PAMOATE SALTS
US20210322669A1 (en) * 2020-04-16 2021-10-21 Invictus Health, Inc. Method for treatment of traumatic brain injuries
CN112263572A (zh) * 2020-11-17 2021-01-26 厦门大学附属翔安医院 右旋氯胺酮在制备治疗脱髓鞘疾病药物中的应用

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US20020048610A1 (en) 2000-01-07 2002-04-25 Cima Michael J. High-throughput formation, identification, and analysis of diverse solid-forms
US20080293695A1 (en) * 2007-05-22 2008-11-27 David William Bristol Salts of physiologically active and psychoactive alkaloids and amines simultaneously exhibiting bioavailability and abuse resistance
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JO2857B1 (en) 2008-06-16 2015-03-15 سانوفي أفينتس Vinyl pipers with modified activity of tumor-resistant TNF
JO3227B1 (ar) 2011-09-08 2018-03-08 Otsuka Pharma Co Ltd مشتقات بنزو ثيوفين بها استبدال ببرازين كعوامل مضادة للذهان
JP2014196292A (ja) 2013-03-07 2014-10-16 大塚製薬株式会社 医薬
CN106562952B (zh) * 2015-10-09 2020-06-09 江阴安博生物医药有限公司 氯胺酮在治疗重性抑郁障碍中的应用
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CA3048485C (en) 2016-12-26 2022-07-19 Cellix Bio Private Limited Compositions and methods for the treatment of chronic pain
AU2019206950B2 (en) * 2018-01-10 2021-07-01 XWPharma Ltd. Prodrugs of ketamine, compositions and uses thereof

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Publication number Publication date
RS65271B1 (sr) 2024-03-29
DK3908570T3 (da) 2024-02-26
CN113423686A (zh) 2021-09-21
LT3908570T (lt) 2024-03-12
BR112021013340A2 (pt) 2021-09-14
JP7451538B2 (ja) 2024-03-18
SI3908570T1 (sl) 2024-04-30
EP3908570A1 (en) 2021-11-17
ES2974259T3 (es) 2024-06-26
JP2022518003A (ja) 2022-03-11
PE20211550A1 (es) 2021-08-16
TW202042796A (zh) 2020-12-01
WO2020143762A1 (en) 2020-07-16
EP3908570B1 (en) 2023-12-13
SG11202104792SA (en) 2021-06-29
US20220119338A1 (en) 2022-04-21
AU2020206826B2 (en) 2024-05-02
PT3908570T (pt) 2024-03-15
PH12021551157A1 (en) 2021-11-03
CL2021001803A1 (es) 2021-12-24
MX2021006029A (es) 2021-09-23
CA3118954A1 (en) 2020-07-16
TWI827783B (zh) 2024-01-01
US11981617B2 (en) 2024-05-14
KR20210116517A (ko) 2021-09-27
AU2020206826A1 (en) 2021-06-03
FI3908570T3 (fi) 2024-02-13
CO2021006884A2 (es) 2021-06-10
EP3908570A4 (en) 2022-10-19
CN113423686B (zh) 2023-08-22

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