DK2401272T3 - Amorf salt af en makrocyklisk inhibitor af hcv - Google Patents
Amorf salt af en makrocyklisk inhibitor af hcv Download PDFInfo
- Publication number
- DK2401272T3 DK2401272T3 DK10706539.3T DK10706539T DK2401272T3 DK 2401272 T3 DK2401272 T3 DK 2401272T3 DK 10706539 T DK10706539 T DK 10706539T DK 2401272 T3 DK2401272 T3 DK 2401272T3
- Authority
- DK
- Denmark
- Prior art keywords
- compound
- hcv
- formula
- amorphous
- sodium salt
- Prior art date
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- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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Claims (14)
1. Natriumsalt af forbindelsen med formel I:
(0 i fast amorf form.
2. Fremgangsmåde til fremstilling af saltet ifølge krav 1, der omfatter: (a) fremstilling af en blanding af forbindelsen med formel I i et ikke-vandigt opløsningsmiddel og en vandig natriumhydroxid; og (b) sprøjtetørring af blandingen fra (a) i et sprøj tetørringsapparat.
3. Fremgangsmåde ifølge krav 2, hvor trin a) omfatter blanding af en natriumhydroxidopløsning i vand med opløsningsmidlet og efterfølgende tilsætning af forbindelsen med formel I.
4. Fremgangsmåde ifølge krav 3, hvor i trin a) forbindelsen med formel I får mulighed for at danne en opløsning.
5. Fremgangsmåde ifølge et hvilket som helst af kravene 2 til 4, hvor opløsningsmidlet er et halogeneret carbonhydrid.
6. Fremgangsmåde ifølge krav 2, hvor opløsningsmidlet er dichlormethan, og den vandige natriumhydroxid er fra ca. 7,5 N til ca. 12,5 N natriumhydroxidopløsning i vand.
7. Farmaceutisk sammensætning, der omfatter natriumsaltet af forbindelsen med formel I i amorf form ifølge krav 1 og et farmaceutisk acceptabelt bæremateriale.
8. Forbindelse ifølge krav 1 til anvendelse som en medicin.
9. Forbindelse ifølge krav 1 til anvendelse som en HCV- inhibitor.
10. Anvendelse af forbindelsen ifølge krav 1 til fremstilling af et medikament til behandling af HCV.
11. Kombination, der omfatter: (a) forbindelsen ifølge krav 1; og (b) en anden antiviral forbindelse som et kombineret præparat til samtidig, separat eller sekventiel anvendelse.
12. Kombination ifølge krav 11, hvor den antivirale forbindelse er en anti-HCV-forbindelse.
13. Kombination ifølge krav 12, hvor anti-HCV-forbindelsen er en inhibitor af HCV-polymerase, en inhibitor af HCV-protease, en inhibitor af andre mål i HCV-livscyklen, et immunmodulatorisk middel eller en kombination deraf.
14. Kombination, der omfatter: (a) forbindelsen ifølge krav 1; og (b) ritonavir som et kombineret præparat til samtidig, separat eller sekventiel anvendelse.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09153964 | 2009-02-27 | ||
| PCT/EP2010/001197 WO2010097229A2 (en) | 2009-02-27 | 2010-02-26 | Amorphous salt of a macrocyclic inhibitor of hcv |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2401272T3 true DK2401272T3 (da) | 2017-02-27 |
Family
ID=40756982
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK10706539.3T DK2401272T3 (da) | 2009-02-27 | 2010-02-26 | Amorf salt af en makrocyklisk inhibitor af hcv |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US9321758B2 (da) |
| EP (2) | EP3150596A1 (da) |
| JP (2) | JP5711672B2 (da) |
| KR (2) | KR101868412B1 (da) |
| CN (2) | CN104478868A (da) |
| AU (1) | AU2010219160B2 (da) |
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| CA (2) | CA2898529C (da) |
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| ES (1) | ES2616603T3 (da) |
| HK (1) | HK1208464A1 (da) |
| HR (1) | HRP20170214T1 (da) |
| HU (1) | HUE031738T2 (da) |
| IL (2) | IL214398A0 (da) |
| LT (1) | LT2401272T (da) |
| MX (1) | MX340792B (da) |
| NZ (1) | NZ594403A (da) |
| PL (1) | PL2401272T3 (da) |
| PT (1) | PT2401272T (da) |
| RU (1) | RU2536868C2 (da) |
| SG (2) | SG173772A1 (da) |
| SI (1) | SI2401272T1 (da) |
| SM (2) | SMT201700121T1 (da) |
| WO (1) | WO2010097229A2 (da) |
| ZA (1) | ZA201106303B (da) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI454476B (zh) | 2008-07-08 | 2014-10-01 | Tibotec Pharm Ltd | 用作ｃ型肝炎病毒抑制劑之巨環吲哚衍生物 |
| SMT201700121T1 (it) * | 2009-02-27 | 2017-03-08 | Janssen Pharmaceuticals Inc | Sale amorfo di un inibitore macrociclico di hcv |
| US9034832B2 (en) * | 2011-12-29 | 2015-05-19 | Abbvie Inc. | Solid compositions |
| EP2797586A1 (en) * | 2011-12-29 | 2014-11-05 | AbbVie Inc. | Solid compositions comprising an hcv inhibitor |
| EP2890378A2 (en) * | 2012-08-31 | 2015-07-08 | Janssen Pharmaceuticals, Inc. | Combination of a macrocyclic protease inhibitor of hcv, a non-nucleoside hcv inhibitor and ritonavir |
| UA118256C2 (uk) | 2013-01-31 | 2018-12-26 | Гіліад Фармассет Елелсі | Комбінований склад двох противірусних сполук |
| CN105228593B (zh) * | 2013-03-15 | 2018-08-28 | 勃林格殷格翰国际有限公司 | 呈无定形状态的hcv抑制剂的固体口服剂型 |
| NZ716840A (en) | 2013-08-27 | 2017-06-30 | Gilead Pharmasset Llc | Combination formulation of two antiviral compounds |
| CN104995189B (zh) * | 2014-01-21 | 2017-03-29 | 杭州普晒医药科技有限公司 | 丙型肝炎药物的晶型及其制备方法、其药物组合物和用途 |
| WO2015180253A1 (zh) * | 2014-05-29 | 2015-12-03 | 杭州普晒医药科技有限公司 | 丙型肝炎药物的晶型及其制备方法、其药物组合物和用途 |
| WO2016054240A1 (en) * | 2014-09-30 | 2016-04-07 | Sean Dalziel | Fixed dose combinations for the treatment of viral diseases |
| CZ2015220A3 (cs) * | 2015-03-27 | 2016-10-05 | Zentiva, K.S. | Amorfní sůl makrocyklického inhibitoru viru hepatitidy C |
| WO2016177625A1 (en) | 2015-05-04 | 2016-11-10 | Sandoz Ag | Amorphous simeprevir potassium |
| WO2017017604A1 (en) | 2015-07-27 | 2017-02-02 | Lupin Limited | Substantially pure amorphous simeprevir sodium salt and the process for preparation thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060083784A1 (en) * | 2002-08-07 | 2006-04-20 | Smithkline Beecham Corporation | Amorphous pharmaceutical compositions |
| CN1889970B (zh) * | 2003-10-14 | 2012-06-13 | F·霍夫曼-罗须公司 | 作为hcv复制抑制剂的巨环羧酸和酰基磺酰胺 |
| SI1713823T1 (sl) | 2004-01-30 | 2010-04-30 | Medivir Ab | Inhibitorji HCV NS-3 serin proteaze |
| AU2005214469A1 (en) * | 2004-02-24 | 2005-09-01 | Siegfried Generics International Ag | Pharmacologically acceptable salts of clopidogrel |
| JP4950026B2 (ja) | 2004-03-30 | 2012-06-13 | インターミューン・インコーポレーテッド | ウイルス複製阻害剤としての大環状化合物 |
| UA91677C2 (ru) * | 2004-03-30 | 2010-08-25 | Интермюн, Инк. | Макроциклические соединения как ингибиторы вирусной репликации |
| WO2006054317A1 (en) * | 2004-11-19 | 2006-05-26 | Matrix Laboratories Ltd | Process for the preparation of novel amorphous montelukast sodium |
| PE20070343A1 (es) | 2005-07-29 | 2007-05-12 | Medivir Ab | Inhibidores macrociclicos del virus de la hepatitis c |
| PE20070211A1 (es) * | 2005-07-29 | 2007-05-12 | Medivir Ab | Compuestos macrociclicos como inhibidores del virus de hepatitis c |
| JP2008115173A (ja) * | 2006-10-13 | 2008-05-22 | Eisai R & D Management Co Ltd | スルフィニルベンズイミダゾール化合物の塩およびそれらの結晶ならびに非晶質体 |
| US8399434B2 (en) | 2006-11-08 | 2013-03-19 | Duke University | Method of activation of oxazaphosphorines |
| US8143402B2 (en) * | 2007-02-01 | 2012-03-27 | Tibotec Pharmaceuticals Ltd. | Polymorphic forms of a macrocyclic inhibitor of HCV |
| ATE467630T1 (de) * | 2007-02-01 | 2010-05-15 | Tibotec Pharm Ltd | Verfahren und zwischenprodukte zur herstellung eines makrozyklischen proteasehemmers von hcv |
| MX2010002300A (es) * | 2007-08-29 | 2010-03-18 | Pfizer Prod Inc | Polimorfos de sal sodica del acido (3-(((4-terc-butil-bencil)-(pir idin-3-sulfonil)-amino)-metil)-fenoxi)-acetico o un hidrato de los mismos y procedimientos para fabricar los mismos. |
| SMT201700121T1 (it) * | 2009-02-27 | 2017-03-08 | Janssen Pharmaceuticals Inc | Sale amorfo di un inibitore macrociclico di hcv |
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- 2010-02-26 LT LTEP10706539.3T patent/LT2401272T/lt unknown
- 2010-02-26 HR HRP20170214TT patent/HRP20170214T1/hr unknown
- 2010-02-26 DK DK10706539.3T patent/DK2401272T3/da active
- 2010-02-26 KR KR1020177005726A patent/KR101868412B1/ko not_active Expired - Fee Related
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- 2010-02-26 CA CA2898529A patent/CA2898529C/en not_active Expired - Fee Related
- 2010-02-26 EP EP16195560.4A patent/EP3150596A1/en not_active Withdrawn
- 2010-02-26 BR BRPI1008918A patent/BRPI1008918A2/pt not_active Application Discontinuation
- 2010-02-26 SG SG2014008981A patent/SG2014008981A/en unknown
- 2010-02-26 CN CN201410616884.3A patent/CN104478868A/zh active Pending
- 2010-02-26 CA CA2753667A patent/CA2753667C/en not_active Expired - Fee Related
- 2010-02-26 NZ NZ594403A patent/NZ594403A/xx not_active IP Right Cessation
- 2010-02-26 WO PCT/EP2010/001197 patent/WO2010097229A2/en active Application Filing
- 2010-02-26 EP EP10706539.3A patent/EP2401272B1/en active Active
- 2010-02-26 JP JP2011551440A patent/JP5711672B2/ja not_active Expired - Fee Related
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- 2010-02-26 MX MX2011008999A patent/MX340792B/es active IP Right Grant
- 2010-02-26 PL PL10706539T patent/PL2401272T3/pl unknown
- 2010-02-26 ES ES10706539.3T patent/ES2616603T3/es active Active
- 2010-02-26 US US13/202,166 patent/US9321758B2/en not_active Expired - Fee Related
- 2010-02-26 PT PT107065393T patent/PT2401272T/pt unknown
- 2010-02-26 AU AU2010219160A patent/AU2010219160B2/en not_active Ceased
- 2010-02-26 RU RU2011139325/04A patent/RU2536868C2/ru not_active IP Right Cessation
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2011
- 2011-08-02 IL IL214398A patent/IL214398A0/en unknown
- 2011-08-26 ZA ZA2011/06303A patent/ZA201106303B/en unknown
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- 2015-03-06 JP JP2015044264A patent/JP6214584B2/ja not_active Expired - Fee Related
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2016
- 2016-03-08 US US15/063,821 patent/US20160251345A1/en not_active Abandoned
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- 2017-02-22 SM SM201700121T patent/SMT201700121B/it unknown
- 2017-02-22 CY CY20171100246T patent/CY1119121T1/el unknown
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