SI22888B - Polimorfi donepezil hidroklorida in postopek izdelave - Google Patents

Polimorfi donepezil hidroklorida in postopek izdelave Download PDF

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Publication number
SI22888B
SI22888B SI9720102A SI9720102A SI22888B SI 22888 B SI22888 B SI 22888B SI 9720102 A SI9720102 A SI 9720102A SI 9720102 A SI9720102 A SI 9720102A SI 22888 B SI22888 B SI 22888B
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SI
Slovenia
Prior art keywords
polymorph
donepezil hydrochloride
donepezil
manufacture
hydrochloride
Prior art date
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SI9720102A
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English (en)
Other versions
SI22888A (sl
Inventor
Akio Imai
Hideaki Watanabe
Takashi Kajima
Yasushi Ishihama
Akiyo Ohtsuka
Tomohide Tanaka
Jukio Narabu
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Eisai Co Ltd
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Application filed by Eisai Co Ltd filed Critical Eisai Co Ltd
Priority claimed from PCT/JP1997/001932 external-priority patent/WO1997046527A1/en
Publication of SI22888A publication Critical patent/SI22888A/sl
Publication of SI22888B publication Critical patent/SI22888B/sl

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Investigating Or Analysing Materials By Optical Means (AREA)

Abstract

Donepezil hidroklorid namreč benzil dimetoksi indanon il metilpiperidin hidroklorid je na voljo v obliki polimorfov ki so pri farmacevtski uporabi odporni proti toploti in vlagi Možno jih je industrijsko proizvajati Opredeljeniso z vrhovi vzorcev pri X žarkovni praškasi difrakciji ter z absorpcijskimi vrhovi pri infrardečem absorpcijskem spektru v kalijevem bromidu

Claims (14)

  1. Eisai Co., Ltd. Polimorfi donepezil hidroklorida in postopek izdelave PATENTNI ZAHTEVKI 1. Donepezil hidroklorid, namreč l-benzil-4-[(5,6-dimetoksi-l-indanon)-2-il]metilpiperidin hidroklorid, v obliki polimorfa (IV), pri čemer je polimorf opredeljen z vrhovi ob spodaj navedenih difrakcijskih stopnjah in spodaj navedeni intenziteti vzorcev praškaste X-žarkovne difrakcije, izraženi z I/I0, kot tudi spodaj navedenih absorpcijskih vrhov pri infrardečih absorpcijskih spektrih v kalijevem bromidu, izraženih v recipročnih centrimetrih, pri čemer velja polimorfi (IV) vrhovi pri praškastih X-žarkovnih difrakcijskih vzorcih so Difrakciiski koti (2Θ.°)_Intenziteta (I/L) 6,24 9,66 11,0412,12 12,54 12,76 13,98 14,42 14,88 15 12 22 24 67 61 27 15 11 2 16,34 12 17,46 100 18,12 25 18,60 32 19,06 15 19,98 74 20,24 41 20,62 34 21,30 48 21,80 63 22,58 78 23,04 46 24,00 32 24,54 49 25,14 90 25,36 99 26,06 34 28,10 41 28,58 39 29,30 31 29.44 28. Valovna števila (cm1) infrardečih absorpcijskih spektrov v kalijevem bromidu so: 401, 431, 459, 467, 490, 506, 518, 561, 586, 606, 631, 651, 709, 758, 766, 857, 944, 1009, 1041, 1106, 1119, 1132, 1213, 1225, 1265, 1304, 1318, 1429, 1458, 1470, 1500, 1589, 1605, 1630, 1647, 1683, 2562, 2577, 2608, 2634, 2689, 2717, 2836, 2924, 2949, 2989, 3007, 3032, 3061, 3322, 3376, 3422 cm '. 3
  2. 2. Postopek izdelave polimorfa (IV) donepezil hidroklorida po zahtevku 1, obsegajoč korak navlaženja v nadaljevanju definiranega polimorfa (II): (2) Polimorfi (II) Vrhovi v vzorcu praškaste X-žarkovne di frakcij e so: Intenziteta (I/Ll 8 100 13 40 38 38 35 17 20 17 19 19 47 24 19 33 22 25 27 18 14 Difrakciiski koti (2Θ.°) 7.40 9,88 12,36 15,54 16,10 16,22 16,48 17,30 18,04 18,44 18.84 19,34 19.84 21,16 22.40 23,18 24,02 24,92 25,72 26.40 27.22_ 4 Valovna števila (cm1) infrardečih absorpcijskih spektrov v kalijevem bromidu so: 699, 748, 762, 845, 947, 1009, 1035, 1067, 1103, 1118, 1129, 1174, 1193, 1206, 1222, 1247, 1267, 1317, 1365, 1422, 1436, 1456, 1465, 1502, 1592, 1607, 1688, 2412, 2489, 2627, 2846, 2868, 2913, 2928, 3435 cm1.
  3. 3. Postopek izdelave polimorfa (IV) donepezil hidroklorida po zahtevku 1, obsegajoč korak raztapljanja donepezila v vodi z dodajanjem tetrahidrofurana ali brez dodajanja le-tega ter z dodajanjem klorovodikove kisline ali vodikovega klorida raztopini.
  4. 4. Postopek izdelave polimorfa (IV) donepezil hidroklorida po zahtevku 1, obsegajoč korak raztapljanja donepezila v klorovodikovi kislini ter dodajanja tetrahidrofurana raztopini.
  5. 5. Postopek izdelave polimorfa (IV) donepezil hidroklorida po zahtevku 1, obsegajoč korak korak raztapljanja donepezila v toluenu ter dodajanja klorovodikove kisline raztopini.
  6. 6. Postopek izdelave polimorfa (IV) donepezil hidroklorida po zahtevku 1, obsegajoč korak raztapljanja donepezila v n-heksanu ter dodajanja klorovodikove kisline raztopini.
  7. 7. Postopek izdelave polimorfa (IV) donepezil hidroklorida po zahtevku 1, obsegajoč korak kristalizacije donepezila v mešanici metanola in klorovodikove kisline. 5
  8. 8. Postopek izdelave polimorfa (IV) donepezil hidroklorida po zahtevku 1, obsegajoč korak korak kristalizacije donepezila iz vode.
  9. 9. Postopek izdelave polimorfa (IV) donepezil hidroklorida po zahtevku 1, obsegajoč korak navlaženja amorfne oblike donepezil hidroklorida.
  10. 10. Postopek izdelave polimorfa (IV) donepezil hidroklorida po zahtevku 1, obsegajoč korak navlaženja polimorfa (II) donepezil hidroklorida
  11. 11. Uporaba farmakološko učinkovite količine donepezil hidroklorida v obliki polimorfa po zahtevku 1 za pripravo zdravila za zdravljenje bolezni, povezanih z acetilholinasterazno aktivnostjo.
  12. 12. Uporaba po zahtevku 11, pri čemer bolezen predstavlja senilna demenca.
  13. 13. Uporaba po zahtevku 11, pri čemer bolezen predstavlja senilna demenca Alzheimerjeve vrste.
  14. 14. Terapevtski sestavek, obsegajoč farmakološko učinkovito količino donepezil hidroklorida v obliki polimorfa po zahtevku 1 in farmakološko sprejemljiv nosilec.
SI9720102A 1996-06-07 1997-06-06 Polimorfi donepezil hidroklorida in postopek izdelave SI22888B (sl)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP14629396 1996-06-07
PCT/JP1996/003881 WO1997046526A1 (en) 1996-06-07 1996-12-27 Stable polymorphs of donepezil (1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine) hydrochloride and process for production
US08/774,802 US6140321A (en) 1996-06-07 1996-12-30 Polymorphs of donepezil hydrochloride and process for production
PCT/JP1997/001932 WO1997046527A1 (en) 1996-06-07 1997-06-06 Polymorphs of donepezil hydrochloride and process for production

Publications (2)

Publication Number Publication Date
SI22888A SI22888A (sl) 2010-04-30
SI22888B true SI22888B (sl) 2010-06-30

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Country Status (17)

Country Link
US (1) US6140321A (sl)
JP (2) JP2005015486A (sl)
KR (1) KR100545851B1 (sl)
CN (1) CN1312129C (sl)
AT (1) ATE445603T1 (sl)
AU (1) AU1153097A (sl)
CA (1) CA2516108C (sl)
DE (1) DE69739622D1 (sl)
DK (1) DK1211243T3 (sl)
ES (1) ES2330997T3 (sl)
HK (1) HK1080078A1 (sl)
HU (1) HUP0900417A3 (sl)
PT (1) PT1211243E (sl)
SI (1) SI22888B (sl)
UA (1) UA60307C2 (sl)
WO (1) WO1997046526A1 (sl)
ZA (1) ZA975064B (sl)

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