SI9620040B - Postopek in kristalne oblike 2-metil-tieno-benzodiazepina - Google Patents

Postopek in kristalne oblike 2-metil-tieno-benzodiazepina Download PDF

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Publication number
SI9620040B
SI9620040B SI9620040A SI9620040A SI9620040B SI 9620040 B SI9620040 B SI 9620040B SI 9620040 A SI9620040 A SI 9620040A SI 9620040 A SI9620040 A SI 9620040A SI 9620040 B SI9620040 B SI 9620040B
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SI
Slovenia
Prior art keywords
olanzapine
ray powder
polymorph
diffraction pattern
pharmaceutical formulation
Prior art date
Application number
SI9620040A
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English (en)
Other versions
SI9620040A (sl
Inventor
Charles Arthur Bunnell
Barry Arnold Hendriksen
Samuel Dean Larsen
Original Assignee
Eli Lilly And Company
Lilly Industries Limited
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Application filed by Eli Lilly And Company, Lilly Industries Limited filed Critical Eli Lilly And Company
Publication of SI9620040A publication Critical patent/SI9620040A/sl
Publication of SI9620040B publication Critical patent/SI9620040B/sl

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicinal Preparation (AREA)

Claims (9)

1 PATENTNI ZAHTEVKI 1. Olanzapin polimorf oblike II s tipičnim rentgenskim praškovnim difrakcijskim vzorcem, kot je prikazan z naslednjimi medravninskimi 5 razdaljami: d (A) 10.2689 8.577 7.4721 7.125 6.1459 6.071 5.4849 5.2181 5.1251 4.9874 4.7665 4.7158 4.4787 4.3307 4.2294 4.141 3.9873 3.7206 3.5645 3.5366 3.3828 2 3.2516 3.134 3.0848 s 3.0638 3.0111 2.8739 2.8102 2.7217 ίο 2.6432 2.6007 ki je substancionalno čist.
2. Oblika II po zahtevku 1, ki vsebuje manj kot okoli 5% oblike I, ki ima is sledeč substancionalno tipični rentgenski praškovni difrakcijski vzorec, pridobljen z uporabo Siemens D5000 rentgenskega praškovnega difraktometra, kjer d predstavlja medravninsko razdaljo: d(A) 20 9.9463 8.5579 8.2445 6.8862 6.3787 25 6.2439 5.5895 5.3055 4.9815 3 4.8333 4.7255 4.6286 4.533 4.4624 4.2915 4.2346 4.0855 3.8254 3.7489 3.6983 3.5817 3.5064 3.3392 3.2806 3.2138 3.1118 3.0507 2.948 2.8172 2.7589 2.6597 2.6336 2.5956
3. Oblika II po zahtevku 2, ki vsebuje manj kot okoli 2% vsebine oblike I.
4. Oblika II po kateremkoli zahtevku od 1 do 3, ki je prosta solvatov. 4
5. Oblika II po zahtevku od 1 do 4 , ki je anhidrid (anhydrous).
6. Farmacevtska formulacija vsebujoča aktivno obliko II, po kateremkoli od zahtevkov od 1 do 5, skupaj z enim ali večimi farmacevtsko s sprejemljivimi nosilci, ekscipienti ali diluenti.
7. Farmacevtska formulacija po zahtevku 6, ki je tableta.
8. Postopek priprave oblike II, po kateremkoli zahtevku od 1 do 5, ki io obsega raztapljanje tehničnega olanzapina v etilacetatu pod anhidridnimi pogoji in kristalizacijo oblike II iz nastale raztopine.
9. Oblika II olanzapin polimorfa po kateremkoli zahtevku od 1 do 5, za uporabo pri zdravljenju bolezenskih stanj iz skupine, sestavljene iz is psihoz, shizofrenij, motenj shizofrene oblike, anksioznih stanj, gastrointestinalne motenj in akutnih manij. 20
SI9620040A 1995-03-24 1996-03-22 Postopek in kristalne oblike 2-metil-tieno-benzodiazepina SI9620040B (sl)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US40956695A 1995-03-24 1995-03-24
PCT/US1996/003917 WO1996030375A1 (en) 1995-03-24 1996-03-22 Process and crystal forms of 2-methyl-thieno-benzodiazepine

Publications (2)

Publication Number Publication Date
SI9620040A SI9620040A (sl) 1998-06-30
SI9620040B true SI9620040B (sl) 2002-02-28

Family

ID=23621056

Family Applications (4)

Application Number Title Priority Date Filing Date
SI9620040A SI9620040B (sl) 1995-03-24 1996-03-22 Postopek in kristalne oblike 2-metil-tieno-benzodiazepina
SI9630743T SI1445259T1 (sl) 1995-03-24 1996-03-22 Uporaba kristalnih oblik 2-metil-tienobenzodiazepina
SI9630345T SI0733635T1 (sl) 1995-03-24 1996-03-22 Kristalna oblika tieno(2,3-b)(1,5) benzodiazepinskega derivata in postopek za njegovo pripravo
SI9630636T SI1095941T1 (sl) 1995-03-24 1996-03-22 Postopek in kristalne oblike 2-metil-tieno-benzodiazepina

Family Applications After (3)

Application Number Title Priority Date Filing Date
SI9630743T SI1445259T1 (sl) 1995-03-24 1996-03-22 Uporaba kristalnih oblik 2-metil-tienobenzodiazepina
SI9630345T SI0733635T1 (sl) 1995-03-24 1996-03-22 Kristalna oblika tieno(2,3-b)(1,5) benzodiazepinskega derivata in postopek za njegovo pripravo
SI9630636T SI1095941T1 (sl) 1995-03-24 1996-03-22 Postopek in kristalne oblike 2-metil-tieno-benzodiazepina

Country Status (49)

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US (1) US5736541A (sl)
EP (3) EP1445259B1 (sl)
JP (1) JPH11502535A (sl)
KR (1) KR100399688B1 (sl)
CN (1) CN1065536C (sl)
AP (1) AP828A (sl)
AR (2) AR002719A1 (sl)
AT (4) AT406771B (sl)
AU (1) AU706471B2 (sl)
BG (1) BG62619B1 (sl)
BR (1) BR9607790A (sl)
CA (1) CA2214005C (sl)
CH (1) CH690579A5 (sl)
CO (1) CO4650278A1 (sl)
CZ (1) CZ292688B6 (sl)
DE (4) DE69636313T2 (sl)
DK (4) DK0733635T3 (sl)
EA (1) EA000149B1 (sl)
EE (1) EE03489B1 (sl)
EG (1) EG23659A (sl)
ES (3) ES2208220T3 (sl)
FI (1) FI973750A (sl)
GB (1) GB2313835B (sl)
HK (1) HK1013988A1 (sl)
HU (1) HU224989B1 (sl)
IL (1) IL117610A (sl)
IS (1) IS1896B (sl)
LT (1) LT4349B (sl)
LU (1) LU90096B1 (sl)
LV (1) LV12018B (sl)
MY (1) MY114701A (sl)
NO (1) NO314663B1 (sl)
NZ (1) NZ306110A (sl)
OA (1) OA10510A (sl)
PA (1) PA8353701A1 (sl)
PE (1) PE44897A1 (sl)
PL (1) PL183723B1 (sl)
PT (3) PT1095941E (sl)
RO (1) RO118872B1 (sl)
SE (1) SE9703205D0 (sl)
SI (4) SI9620040B (sl)
SK (1) SK284143B6 (sl)
SV (1) SV1996000031A (sl)
TR (1) TR199701017T1 (sl)
TW (2) TW442488B (sl)
UA (1) UA44765C2 (sl)
WO (1) WO1996030375A1 (sl)
YU (1) YU49478B (sl)
ZA (2) ZA962342B (sl)

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HK1013988A1 (en) 1999-09-17
NO974365D0 (no) 1997-09-22
WO1996030375A1 (en) 1996-10-03
EP1445259B1 (en) 2006-06-28
AP9701065A0 (en) 1997-10-31
AR010448A1 (es) 2000-06-28
YU49478B (sh) 2006-05-25
CN1179160A (zh) 1998-04-15
EA000149B1 (ru) 1998-10-29
DE69636313T2 (de) 2007-05-31
CA2214005C (en) 2001-07-03
ES2208220T3 (es) 2004-06-16
CO4650278A1 (es) 1998-09-03
LV12018B (en) 1998-09-20
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LT4349B (lt) 1998-05-25
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