HRP20120652T1 - Organski spojevi - Google Patents

Organski spojevi Download PDF

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Publication number
HRP20120652T1
HRP20120652T1 HRP20120652TT HRP20120652T HRP20120652T1 HR P20120652 T1 HRP20120652 T1 HR P20120652T1 HR P20120652T T HRP20120652T T HR P20120652TT HR P20120652 T HRP20120652 T HR P20120652T HR P20120652 T1 HRP20120652 T1 HR P20120652T1
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HR
Croatia
Prior art keywords
staurosporine
benzoyl
crystalline form
solution
compound
Prior art date
Application number
HRP20120652TT
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English (en)
Inventor
Hoehn Pascale
Koch Bernd
Mutz Michael
Original Assignee
Novartis Ag
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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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=35501294&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20120652(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of HRP20120652T1 publication Critical patent/HRP20120652T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Solid-Sorbent Or Filter-Aiding Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Extraction Or Liquid Replacement (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Spoj, naznačen time, da je to kristalni oblik II od N-benzoil-staurosporina, koji ima uzorak difrakcije X-zraka, izra·en u razmacima od 2-teta vrijednosti, koji uključuje pet ili vi®e vr®nih vrijednosti odabrane iz skupine koju čine oko 3,4, 6,0, 7,8, 8,7, 9,2, 9,7, 10,1, 10,4, 11,2, 12,6, 14,1, 15,7, 16,8, 18,2, 18,9, 19,3, 19,6, 20,2 i 24,5 ą 0,2 stupnjeva. Patent sadr·i jo® 16 patentnih zahtjeva.

Claims (17)

1. Spoj, naznačen time, da je to kristalni oblik II od N-benzoil-staurosporina, koji ima uzorak difrakcije x-zraka, izražen u razmacima od 2-teta vrijednosti, koji uključuje pet ili više vršnih vrijednosti odabrane iz skupine koju čine oko 3,4, 6,0, 7,8, 8,7, 9,2, 9,7, 10,1, 10,4, 11,2, 12,6, 14,1, 15,7, 16,8, 18,2, 18,9, 19,3, 19,6, 20,2 i 24,5 ± 0,2 stupnjeva.
2. Spoj prema zahtjevu 1, naznačen time, da ima uglavnom isti uzorak difrakcije X-zraka kao što je prikazano u Slici 1.
3. Spoj prema zahtjevu 1, naznačen time, da ostaje suh na 95% relativne vlažnosti i na 25°C.
4. Spoj prema zahtjevu 1, naznačen time, da ima spektar infracrvene apsorpcije s apsorpcijskim opsegom na oko 789, 773, 743, 704, 1066, 1026, 1458, 1398, 1383, 1602, 1577, 1497, 1627, 1680, 2934 i 3055 cm-1± 2 cm-1.
5. Spoj, naznačen time, da sadrži N-benzoil-staurosporin kao krutinu, pri čemu je najmanje 80 masenih % od spomenute krutine N-benzoil-staurosporina u kristalnom obliku II prema zahtjevu 1.
6. Spoj prema zahtjevu 5, naznačen time, da pri čemu je najmanje 90 masenih % od spomenute krutine N-benzoil-staurosporina u kristalnom obliku II.
7. Spoj prema zahtjevu 5, naznačen time, da pri čemu je najmanje 95 masenih % od spomenute krutine N-benzoil-staurosporina u kristalnom obliku II.
8. Farmaceutski sastav, naznačen time, da sadrži: (a) spoj prema zahtjevu 1; i (b) farmaceutski prihvatljiv nosač ili razrjeđivač.
9. Farmaceutski sastav prema zahtjevu 8, naznačen time, da nadalje sadrži jedno ili više farmaceutski prihvatljivih pomoćnih sredstava.
10. Farmaceutski sastav prema zahtjevu 8, naznačen time, da je u dozirnom obliku pogodnom za oralnu primjenu.
11. Farmaceutski sastav prema zahtjevu 10, naznačen time, da je spomenuti dozirni oblik odabran od tablete, kapsule ili otopine.
12. N-benzoil-staurosporin prema bilo kojem od zahtjeva 1 do 8, naznačen time, da je za uporabu u liječenju tumorskih bolesti.
13. Postupak proizvodnje kristalnog oblika II od N-benzoil-staurosporina prema zahtjevu 1, naznačen time, da obuhvaća: (a) pribavljanje otopine N-benzoil-staurosporina u otapalu; (b) stavljanje u doticaj otopine s drugim otapalom za stvaranje taloga; i (c) izoliranje taloga; pri čemu otapalo je odabrano od sljedećih: benzilni alkohol, DMF, DMSO, octena kiselina ili PEG; pri čemu je drugo otapalo odabrano od sljedećih: etanol, THF ili otopina etanola i vode.
14. Postupak prema zahtjevu 13, naznačen time, da nadalje obuhvaća sušenje izoliranog taloga.
15. Spoj, naznačen time, da je to kristalni oblik II od N-benzoil-staurosporina proizveden postupkom iz zahtjeva 13.
16. Postupak proizvodnje kristalnog oblika II od N-benzoil-staurosporina iz zahtjeva 1, naznačen time, da obuhvaća: (a) reagiranje staurosporina s anhidridom benzoične kiseline za tvorbu otopine; (b) kultiviranje otopine s kristalnim oblikom II od N-benzoil-staurosporina; (c) dodavanje drugog otapala; i (d) izoliranje proizvoda; pri čemu je drugo otapalo odabrano od etanola ili otopine etanola i vode.
17. Spoj, naznačen time, da je to kristalni oblik II od N-benzoil-staurosporina proizveden postupkom iz zahtjeva 16.
HRP20120652TT 2004-11-05 2012-08-10 Organski spojevi HRP20120652T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US62534304P 2004-11-05 2004-11-05
US64213105P 2005-01-07 2005-01-07
PCT/EP2005/011789 WO2006048296A1 (en) 2004-11-05 2005-11-03 Organic compounds

Publications (1)

Publication Number Publication Date
HRP20120652T1 true HRP20120652T1 (hr) 2012-09-30

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ID=35501294

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Application Number Title Priority Date Filing Date
HRP20120652TT HRP20120652T1 (hr) 2004-11-05 2012-08-10 Organski spojevi

Country Status (31)

Country Link
US (2) US8198435B2 (hr)
EP (3) EP2272850B1 (hr)
JP (4) JP5057986B2 (hr)
KR (3) KR101289998B1 (hr)
CN (2) CN102993213A (hr)
AR (1) AR052322A1 (hr)
AU (2) AU2005300693B2 (hr)
BR (1) BRPI0517689A (hr)
CA (1) CA2584911C (hr)
CY (1) CY1113059T1 (hr)
DK (1) DK1812448T3 (hr)
EC (1) ECSP12007431A (hr)
ES (1) ES2388142T3 (hr)
GT (1) GT200500311A (hr)
HK (2) HK1211587A1 (hr)
HR (1) HRP20120652T1 (hr)
IL (3) IL182691A (hr)
JO (1) JO2897B1 (hr)
MA (1) MA29033B1 (hr)
MX (2) MX2007005429A (hr)
MY (2) MY147404A (hr)
NO (2) NO338960B1 (hr)
NZ (3) NZ588025A (hr)
PE (3) PE20130377A1 (hr)
PL (1) PL1812448T3 (hr)
PT (1) PT1812448E (hr)
RU (2) RU2394038C2 (hr)
SI (1) SI1812448T1 (hr)
TN (1) TNSN07165A1 (hr)
TW (4) TWI433852B (hr)
WO (1) WO2006048296A1 (hr)

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CN101516339B (zh) * 2006-08-16 2012-06-13 诺瓦提斯公司 制备高度结晶的治疗化合物的固体分散体的方法
EP2327706A1 (en) * 2009-11-30 2011-06-01 Novartis AG Polymorphous forms III and IV of N-benzoyl-staurosporine
KR20160008267A (ko) 2014-07-14 2016-01-22 주식회사 윈스 네트워크 기반 영상감시체계에서의 사용자 행위 분석 시스템
EP3592749A1 (en) * 2017-03-06 2020-01-15 Teva Pharmaceutical Works Ltd. Solid state forms of midostaurin
WO2019215759A1 (en) * 2018-05-09 2019-11-14 Alaparthi Lakshmi Prasad An improved process for preparation of midostaurin
IT201900004729A1 (it) 2019-03-29 2020-09-29 Procos Spa Processo per la preparazione di midostaurina ad elevato grado di purezza
WO2020261293A1 (en) * 2019-06-24 2020-12-30 Dr. Reddy's Laboratories Limited Process for preparation of midostaurin
IT201900014346A1 (it) * 2019-08-08 2021-02-08 Procos Spa Processo per la preparazione di midostaurina amorfa con un basso contenuto di solvente organico residuo
IT202000004291A1 (it) 2020-03-02 2021-09-02 Indena Spa Processo per la purificazione di alcaloidi indolo carbazolici
CN111393454A (zh) * 2020-05-07 2020-07-10 奥锐特药业(天津)有限公司 米哚妥林的新晶型及其制备方法
CN115124551B (zh) * 2021-03-24 2024-04-30 奥锐特药业(天津)有限公司 一种高纯度米哚妥林的制备方法
WO2023205504A1 (en) * 2022-04-22 2023-10-26 Rutgers, The State University Of New Jersey Formulations and methods for treating epidermolysis bullosa simplex and related conditions

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Also Published As

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RU2467012C2 (ru) 2012-11-20
RU2007120695A (ru) 2008-12-10
KR101265850B1 (ko) 2013-05-20
AU2005300693A1 (en) 2006-05-11
CN102627658A (zh) 2012-08-08
IL207702A (en) 2016-09-29
IL182691A0 (en) 2007-09-20
TWI433852B (zh) 2014-04-11
JP2012149099A (ja) 2012-08-09
MX346525B (es) 2017-03-23
EP2272850B1 (en) 2017-05-10
BRPI0517689A (pt) 2008-10-14
PE20130377A1 (es) 2013-04-03
MY147404A (en) 2012-11-30
JP5701246B2 (ja) 2015-04-15
TW200628474A (en) 2006-08-16
RU2394038C2 (ru) 2010-07-10
US8710216B2 (en) 2014-04-29
KR20120101600A (ko) 2012-09-13
PE20090433A1 (es) 2009-05-05
AU2009245817A1 (en) 2009-12-24
TNSN07165A1 (en) 2008-11-21
TWI530500B (zh) 2016-04-21
IL217571A (en) 2017-07-31
NO20072290L (no) 2007-05-30
JP2015063569A (ja) 2015-04-09
RU2009137788A (ru) 2011-04-20
CY1113059T1 (el) 2016-04-13
PL1812448T3 (pl) 2012-10-31
EP2272850A3 (en) 2011-09-21
TW201446773A (zh) 2014-12-16
KR20120101601A (ko) 2012-09-13
CA2584911C (en) 2017-10-24
TW201247680A (en) 2012-12-01
JP5057986B2 (ja) 2012-10-24
TWI530501B (zh) 2016-04-21
SI1812448T1 (sl) 2012-09-28
EP2272850A2 (en) 2011-01-12
PT1812448E (pt) 2012-08-24
AU2005300693B2 (en) 2010-08-19
NZ599033A (en) 2012-09-28
US20120322789A1 (en) 2012-12-20
ECSP12007431A (es) 2012-06-29
KR20070083979A (ko) 2007-08-24
MA29033B1 (fr) 2007-11-01
IL207702A0 (en) 2010-12-30
US20090137552A1 (en) 2009-05-28
TWI455941B (zh) 2014-10-11
CA2584911A1 (en) 2006-05-11
US8198435B2 (en) 2012-06-12
JP2008518995A (ja) 2008-06-05
KR101289998B1 (ko) 2013-07-30
WO2006048296A1 (en) 2006-05-11
GT200500311A (es) 2006-05-22
HK1108881A1 (en) 2008-05-23
JP2017061578A (ja) 2017-03-30
ES2388142T3 (es) 2012-10-09
CN102993213A (zh) 2013-03-27
AU2009245817B2 (en) 2013-02-21
EP2955186A1 (en) 2015-12-16
JO2897B1 (en) 2015-09-15
EP1812448B1 (en) 2012-05-23
NO340404B1 (no) 2017-04-18
KR101333851B1 (ko) 2013-11-27
NO20161152A1 (no) 2007-05-30
NZ554653A (en) 2010-10-29
NZ588025A (en) 2012-04-27
MY154878A (en) 2015-08-14
PE20060947A1 (es) 2006-10-30
AR052322A1 (es) 2007-03-14
TW201247681A (en) 2012-12-01
HK1211587A1 (en) 2016-05-27
NO338960B1 (no) 2016-11-07
IL182691A (en) 2013-02-28
DK1812448T3 (da) 2012-08-27
EP1812448A1 (en) 2007-08-01
MX2007005429A (es) 2007-05-18

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