HRP20121028T1 - Kristalni oblici febuksostata - Google Patents

Kristalni oblici febuksostata Download PDF

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Publication number
HRP20121028T1
HRP20121028T1 HRP20121028AT HRP20121028T HRP20121028T1 HR P20121028 T1 HRP20121028 T1 HR P20121028T1 HR P20121028A T HRP20121028A T HR P20121028AT HR P20121028 T HRP20121028 T HR P20121028T HR P20121028 T1 HRP20121028 T1 HR P20121028T1
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HR
Croatia
Prior art keywords
febuxostat
crystalline form
designated
signals
ppm
Prior art date
Application number
HRP20121028AT
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English (en)
Inventor
Maytal Piran
Leonid Metsger
Original Assignee
Teva Pharmaceutical Industries Ltd.
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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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42352168&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20121028(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Teva Pharmaceutical Industries Ltd. filed Critical Teva Pharmaceutical Industries Ltd.
Publication of HRP20121028T1 publication Critical patent/HRP20121028T1/hr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Claims (14)

1. Kristalni oblik febuksostata, označen kao Oblik F10, naznačen time što su za njega karakteristični podaci koji se biraju između: (a) uzorka difrakcije rendgenskih zraka na prahu, sa signalima na 6,7°, 7,7°, 12,8°, 13,3° i 20,0° ± 0,2° 2θ; (b) 13C-NMR spektra čvrstog stanja, sa signalima na 112,7, 125,7, 132,4 i 168,3 ± 0,2 ppm; (c) 13C-NMR spektra čvrstog stanja s razlikama u kemijskim pomacima između signala koji pokazuje najmanji kemijski pomak i drugog u rasponu kemijskih pomaka od 100 do 180 ppm od 11,7, 24,7, 31,4 i 67,3 ± 0,1 ppm; i njihove kombinacije.
2. Kristalni oblik febuksostata, označen kao Oblik F10, u skladu s patentnim zahtjevom 1, naznačen time što je za njega karakterističan uzorak difrakcije rendgenskih zraka na prahu, sa signalima na 6,7°, 7,7°, 12,8°, 13,3° i 20,0° ± 0,2° 2θ.
3. Kristalni oblik febuksostata označen kao Oblik F10, u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je za njega dodatno karakteristična difrakcija rendgenskih zraka na prahu sa signalima na 3,3°, 16,3°, 16,9°, 24,5° i 25,8° ± 0,2° 2θ.
4. Kristalni oblik febuksostata, označen kao Oblik F10, u skladu s patentnim zahtjevom 1, naznačen time što je za njega karakterističan uzorak difrakcije rendgenskih zraka na prahu koji je uglavnom onakav kako je opisano na Slici 8.
5. Kristalni oblik febuksostata, označen kao Oblik F10, u skladu s patentnim zahtjevom 1, naznačen time što je za njega karakterističan 13C-NMR spektar čvrstog stanja koji je uglavnom onakav kako je opisano na Slikama 9 ili 10.
6. Kristalni oblik febuksostata, označen kao Oblik F2, naznačen time što su za njega karakteristični podaci koji se biraju između: (a) uzorka XRD na prahu sa signalima na 3,0°, 5,9°, 8,8°, 11,8° i 12,5° ± 0,2° 2θ; (b) 13C-NMR spektra čvrstog stanja, sa signalima na 112,3, 163,9, 168,8 ± 0,2 ppm; (c) 13C-NMR spektra čvrstog stanja s razlikama u kemijskim pomacima između signala koji pokazuje najmanji kemijski pomak i drugog u rasponu kemijskih pomaka od 100 do 180 ppm od 11,5, 63,1 i 68,0 ± 0,1 ppm; i njihove kombinacije.
7. Kristalni oblik febuksostata, označen kao Oblik F2, u skladu s patentnim zahtjevom 6, naznačen time što je za njega dodatno karakteristična dodatna difrakcija rendgenskih zraka na prahu sa signalima na: 13,1 °, 14,7°, 17,5°, 24,4° i 25,2° ± 0,2° 2θ.
8. Kristalni oblik febuksostata, označen kao Oblik F2, u skladu s patentnim zahtjevom 6, naznačen time što je za njega karakterističan uzorak difrakcije rendgenskih zraka na prahu koji je uglavnom onakav kako je opisano na Slikama 4 ili 5.
9. Kristalni oblik febuksostata, označen kao Oblik F2, u skladu s patentnim zahtjevom 6, naznačen time što je za njega karakterističan 13C-NMR spektar čvrstog stanja koji je uglavnom onakav kako je opisano na Slikama 6 ili 7.
10. Farmaceutski pripravak naznačen time što sadrži kristalni oblik febuksostata u skladu s bilo kojim od prethodnih patentnih zahtjeva, kao i najmanje jednu farmaceutski prihvatljivu pomoćnu tvar.
11. Kristalni oblik febuksostata u skladu s bilo kojim od patentnih zahtjeva 1-9, naznačen time što je namijenjen upotrebi u obliku farmaceutske formulacije.
12. Postupak priprave farmaceutske formulacije, naznačen time što se sastoji u kombiniranju kristalnog oblika febuksostata u skladu s bilo kojim od patentnih zahtjeva 1-9, s najmanje jednom farmaceutski prihvatljivom pomoćnom tvari.
13. Kristalni oblik u skladu s bilo kojim od patentnih zahtjeva 1-9, naznačen time što je namijenjen upotrebi u liječenju hiperuricemije kod pacijenata s gihtom.
14. Farmaceutski pripravak u skladu s patentnim zahtjevom 10, naznačen time što je namijenjen upotrebi u liječenju pacijenta s gihtom.
HRP20121028AT 2009-06-10 2012-12-13 Kristalni oblici febuksostata HRP20121028T1 (hr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US18577509P 2009-06-10 2009-06-10
US22258309P 2009-07-02 2009-07-02
US23355209P 2009-08-13 2009-08-13
US23548109P 2009-08-20 2009-08-20
PCT/US2010/038143 WO2010144685A1 (en) 2009-06-10 2010-06-10 Crystalline forms of febuxostat

Publications (1)

Publication Number Publication Date
HRP20121028T1 true HRP20121028T1 (hr) 2013-01-31

Family

ID=42352168

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20121028AT HRP20121028T1 (hr) 2009-06-10 2012-12-13 Kristalni oblici febuksostata

Country Status (13)

Country Link
US (3) US8415481B2 (hr)
EP (2) EP2532654A1 (hr)
JP (1) JP5215505B2 (hr)
KR (2) KR101310002B1 (hr)
CN (1) CN102803240A (hr)
CA (1) CA2764600A1 (hr)
DE (1) DE202010017868U1 (hr)
ES (1) ES2395381T3 (hr)
HR (1) HRP20121028T1 (hr)
IL (1) IL216648A0 (hr)
PL (1) PL2398784T3 (hr)
PT (1) PT2398784E (hr)
WO (1) WO2010144685A1 (hr)

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EP2718272A2 (en) * 2011-06-06 2014-04-16 Hetero Research Foundation Process for febuxostat
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EP3002006A1 (en) 2014-10-01 2016-04-06 Bluepharma - Industria Farmacêutica, S.A. Pharmaceutical composition capable for the incorporation Febuxostat in the crystalline modifications F10, II, G and A
CZ27857U1 (cs) 2014-12-12 2015-02-23 Zentiva, K.S. Formulace obsahující tuhý roztok febuxostatu
JP7164926B2 (ja) * 2015-04-22 2022-11-02 日本ケミファ株式会社 ２－［３－シアノ－４－（２－メチルプロポキシ）フェニル］－４－メチルチアゾール－５－カルボン酸の結晶、その製造方法、及びそれらの利用
KR20180013563A (ko) * 2016-07-29 2018-02-07 한미정밀화학주식회사 고순도 결정형 페북소스타트의 개선된 제조 방법
CN106511288A (zh) * 2016-12-20 2017-03-22 天津泰普制药有限公司 一种非布司他片剂的制备方法
JP7096957B2 (ja) * 2020-07-13 2022-07-06 日本碍子株式会社 精製方法
WO2022013919A1 (ja) * 2020-07-13 2022-01-20 日本碍子株式会社 精製方法

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Also Published As

Publication number Publication date
JP2012529537A (ja) 2012-11-22
IL216648A0 (en) 2012-03-01
KR101310002B1 (ko) 2013-09-25
EP2532654A1 (en) 2012-12-12
ES2395381T3 (es) 2013-02-12
US8415481B2 (en) 2013-04-09
WO2010144685A1 (en) 2010-12-16
PT2398784E (pt) 2012-12-27
CN102803240A (zh) 2012-11-28
US8609856B2 (en) 2013-12-17
US8742129B2 (en) 2014-06-03
KR20120140267A (ko) 2012-12-28
US20130178504A1 (en) 2013-07-11
JP5215505B2 (ja) 2013-06-19
US20100317702A1 (en) 2010-12-16
DE202010017868U1 (de) 2012-11-28
EP2398784A1 (en) 2011-12-28
CA2764600A1 (en) 2010-12-16
KR20120034077A (ko) 2012-04-09
US20130245077A1 (en) 2013-09-19
PL2398784T3 (pl) 2013-07-31
EP2398784B1 (en) 2012-10-17

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