HRP20140666T1 - Kristalni oblici derivata 2-tiazolil-4-kinolinil-oksi, snažnog hcv-inhibitora - Google Patents
Kristalni oblici derivata 2-tiazolil-4-kinolinil-oksi, snažnog hcv-inhibitora Download PDFInfo
- Publication number
- HRP20140666T1 HRP20140666T1 HRP20140666AT HRP20140666T HRP20140666T1 HR P20140666 T1 HRP20140666 T1 HR P20140666T1 HR P20140666A T HRP20140666A T HR P20140666AT HR P20140666 T HRP20140666 T HR P20140666T HR P20140666 T1 HRP20140666 T1 HR P20140666T1
- Authority
- HR
- Croatia
- Prior art keywords
- sodium salt
- degrees
- compound
- crystalline
- measured
- Prior art date
Links
- -1 2-thiazolyl- 4-quinolinyl-oxy Chemical class 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 230000003389 potentiating effect Effects 0.000 title 1
- 159000000000 sodium salts Chemical class 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 7
- 238000000634 powder X-ray diffraction Methods 0.000 claims 5
- 230000005855 radiation Effects 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 208000005176 Hepatitis C Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000010710 hepatitis C virus infection Diseases 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
Classifications
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- 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
- C07D417/14—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
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (11)
1. Natrijeva sol, naznačena time, da je od spoja sljedeće formule (1):
[image]
2. Natrijeva sol prema zahtjevu 1, naznačena time, da je u kristalnom obliku.
3. Kristalna natrijeva sol prema zahtjevu 2, naznačena time, da ima uzorak difrakcije praha X-zraka koji obuhvaća vršnu vrijednost na 10,1 stupnjeva 2θ (± 0,2 stupnjeva 2θ) kada se mjeri uporabom radijacije CuKα.
4. Kristalna natrijeva sol prema zahtjevu 3, naznačena time, da uzorak difrakcije praha X-zraka nadalje obuhvaća vršne vrijednosti na 13,0 i 18,2 stupnjeva 2θ (± 0,2 stupnjeva 2θ) kada se mjeri uporabom radijacije CuKα.
5. Kristalna natrijeva sol prema zahtjevu 4, naznačena time, da uzorak difrakcije praha X-zraka nadalje obuhvaća vršne vrijednosti na 5,4 i 8,7 stupnjeva 2θ (± 0,2 stupnjeva 2θ) kada se mjeri uporabom radijacije CuKα.
6. Kristalna natrijeva sol prema zahtjevu 2, naznačena time, da ima uzorak difrakcije praha X-zraka koji obuhvaća vršne vrijednosti na 5,4, 6,5, 8,7, 11,9, 13,0, 18,2, 20,2 i 24,7 stupnjeva 2θ (± 0,2 stupnjeva 2θ) kada se mjeri uporabom radijacije CuKα.
7. Kristalna natrijeva sol prema zahtjevu 2, naznačena time, da ima uzorak difrakcije praha X-zraka izmjeren uporabom radijacije CuKα, koji je uglavnom isti kao onaj prikazan na Slici 3.
8. Spoj, naznačen time, da ima sljedeću formulu (1):
[image]
pri čemu najmanje 50% od toga spoja je prisutno u obliku natrijeve soli od spoja prema zahtjevu 1, 2, 3, 4, 5, 6 ili 7.
9. Farmaceutski sastav, naznačen time, da obuhvaća natrijevu sol prema zahtjevu 1, 2, 3, 4, 5, 6 ili 7 kao i farmaceutski prihvatljiv nosač ili razrjeđivač.
10. Farmaceutski sastav prema zahtjevu 9, naznačen time, da je u sastavu prisutno najmanje 50% natrijeve soli spoja formule (1) u obliku kristalnog spoja prema zahtjevu 2, 3, 4, 5, 6 ili 7.
11. Uporaba natrijeve soli od spoja formule (1) prema zahtjevu 1, naznačena time, da je za proizvodnju lijeka za liječenje virusne hepatitis C infekcije kod sisavaca.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9729108P | 2008-09-16 | 2008-09-16 | |
| US15082609P | 2009-03-09 | 2009-03-09 | |
| PCT/US2009/056772 WO2010033444A1 (en) | 2008-09-16 | 2009-09-14 | Crystalline forms of a 2-thiazolyl- 4-quinolinyl-oxy derivative, a potent hcv inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20140666T1 true HRP20140666T1 (hr) | 2014-10-10 |
Family
ID=41268627
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20140666AT HRP20140666T1 (hr) | 2008-09-16 | 2014-07-14 | Kristalni oblici derivata 2-tiazolil-4-kinolinil-oksi, snažnog hcv-inhibitora |
Country Status (34)
| Country | Link |
|---|---|
| US (2) | US8232293B2 (hr) |
| EP (2) | EP2687526A1 (hr) |
| JP (2) | JP5520301B2 (hr) |
| KR (1) | KR101653550B1 (hr) |
| CN (1) | CN102159571B (hr) |
| AR (1) | AR073298A1 (hr) |
| AU (1) | AU2009293494B2 (hr) |
| BR (1) | BRPI0918513A2 (hr) |
| CA (1) | CA2737055C (hr) |
| CL (1) | CL2011000558A1 (hr) |
| CO (1) | CO6351741A2 (hr) |
| CY (1) | CY1115253T1 (hr) |
| DK (1) | DK2331538T3 (hr) |
| EA (1) | EA018603B1 (hr) |
| EC (1) | ECSP11010878A (hr) |
| ES (1) | ES2474992T3 (hr) |
| HK (1) | HK1156624A1 (hr) |
| HR (1) | HRP20140666T1 (hr) |
| IL (1) | IL210345A (hr) |
| MA (1) | MA32633B1 (hr) |
| ME (1) | ME01831B (hr) |
| MX (1) | MX2011002828A (hr) |
| MY (1) | MY153093A (hr) |
| NZ (2) | NZ602163A (hr) |
| PE (2) | PE20130307A1 (hr) |
| PL (1) | PL2331538T3 (hr) |
| PT (1) | PT2331538E (hr) |
| RS (1) | RS53292B (hr) |
| SG (1) | SG189740A1 (hr) |
| SI (1) | SI2331538T1 (hr) |
| TW (1) | TWI471323B (hr) |
| UY (1) | UY32119A (hr) |
| WO (1) | WO2010033444A1 (hr) |
| ZA (1) | ZA201100096B (hr) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY32099A (es) | 2008-09-11 | 2010-04-30 | Enanta Pharm Inc | Inhibidores macrocíclicos de serina proteasas de hepatitis c |
| EP2687526A1 (en) | 2008-09-16 | 2014-01-22 | Boehringer Ingelheim International Gmbh | Crystalline forms of a 2-thiazolyl- 4-quinolinyl-oxy derivative, a potent HCV inhibitor |
| MY152824A (en) | 2008-09-17 | 2014-11-28 | Boehringer Ingelheim Int | Combination of hcv ns3 protease inhibitor with interferon and ribavirin. |
| US9522068B2 (en) * | 2009-03-13 | 2016-12-20 | The University Of Toledo | Minimally invasive collapsible cage |
| WO2010107965A1 (en) * | 2009-03-19 | 2010-09-23 | Boehringer Ingelheim International Gmbh | Process for preparing sulfonyl quinolines |
| EP2427434B1 (en) | 2009-05-05 | 2017-05-31 | Boehringer Ingelheim International GmbH | Process for preparing bromo-substituted quinolines |
| ME01718B (me) | 2009-07-07 | 2014-09-20 | Boehringer Ingelheim Int | Farmaceutska kompozicija za inhibitor proteaze virusnog Hepatitis C |
| EA201200650A1 (ru) | 2009-10-30 | 2012-12-28 | Бёрингер Ингельхайм Интернациональ Гмбх | Курсы комбинированного лечения вируса гепатита с, включающие bi201335, интерферон-альфа и рибавирин |
| US8530497B2 (en) | 2010-03-11 | 2013-09-10 | Boehringer Ingelheim International Gmbh | Crystalline salts of a potent HCV inhibitor |
| MX2013003060A (es) | 2010-09-30 | 2013-05-30 | Boehringer Ingelheim Int | Terapia de combinacion para tratar infeccion por hcv. |
| CA2822556A1 (en) | 2010-12-30 | 2012-07-05 | Enanta Pharmaceuticals, Inc | Macrocyclic hepatitis c serine protease inhibitors |
| CN103380132B (zh) | 2010-12-30 | 2016-08-31 | 益安药业 | 菲啶大环丙型肝炎丝氨酸蛋白酶抑制剂 |
| US10201584B1 (en) | 2011-05-17 | 2019-02-12 | Abbvie Inc. | Compositions and methods for treating HCV |
| AR088463A1 (es) | 2011-10-21 | 2014-06-11 | Abbvie Inc | Metodos para el tratamiento de hcv |
| US8466159B2 (en) | 2011-10-21 | 2013-06-18 | Abbvie Inc. | Methods for treating HCV |
| ES2527544T1 (es) | 2011-10-21 | 2015-01-26 | Abbvie Inc. | Tratamiento mono (PSI-7977) o de combinación con AAD para su uso en el tratamiento del VHC |
| US8492386B2 (en) | 2011-10-21 | 2013-07-23 | Abbvie Inc. | Methods for treating HCV |
| CN104244926A (zh) | 2012-01-12 | 2014-12-24 | 勃林格殷格翰国际有限公司 | 作为强效的hcv 抑制剂的稳定的药物制剂 |
| WO2013137869A1 (en) | 2012-03-14 | 2013-09-19 | Boehringer Ingelheim International Gmbh | Combination therapy for treating hcv infection in an hcv-hiv coinfected patient population |
| WO2013147750A1 (en) | 2012-03-27 | 2013-10-03 | Boehringer Ingelheim International Gmbh | Oral combination therapy for treating hcv infection in specific patient sub-population |
| WO2013147749A1 (en) | 2012-03-27 | 2013-10-03 | Boehringer Ingelheim International Gmbh | Oral combination therapy for treating hcv infection in specific patient subgenotype populations |
| WO2013143581A1 (en) | 2012-03-28 | 2013-10-03 | Boehringer Ingelheim International Gmbh | Combination therapy for treating hcv infection in specific patient subgenotype sub-population |
| UA119315C2 (uk) | 2012-07-03 | 2019-06-10 | Гіліад Фармассет Елелсі | Інгібітори вірусу гепатиту с |
| WO2014138374A1 (en) | 2013-03-08 | 2014-09-12 | Boehringer Ingelheim International Gmbh | Oral combination therapy for treating hcv infection in specific patient sub-population |
| JP6130585B2 (ja) | 2013-03-15 | 2017-05-17 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 無定形状態のｈｃｖ阻害薬の固体経口投薬製剤 |
| SG11201507223TA (en) | 2013-03-15 | 2015-10-29 | Gilead Sciences Inc | Macrocyclic and bicyclic inhibitors of hepatitis c virus |
| WO2015103490A1 (en) | 2014-01-03 | 2015-07-09 | Abbvie, Inc. | Solid antiviral dosage forms |
| WO2017189978A1 (en) | 2016-04-28 | 2017-11-02 | Emory University | Alkyne containing nucleotide and nucleoside therapeutic compositions and uses related thereto |
| WO2022107182A1 (en) * | 2020-11-18 | 2022-05-27 | University Of Petra | A composition of fentanyl and fatty acids, and a method of preparation thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1033128T4 (da) | 1993-09-28 | 2012-03-19 | Scherer Gmbh R P | Blød gelatinekapselfremstilling |
| AR022061A1 (es) | 1998-08-10 | 2002-09-04 | Boehringer Ingelheim Ca Ltd | Peptidos inhibidores de la hepatitis c, una composicion farmaceutica que los contiene, el uso de los mismos para preparar una composicion farmaceutica, el uso de un producto intermedio para la preparacion de estos peptidos y un procedimiento para la preparacion de un peptido analogo de los mismos. |
| US6323180B1 (en) | 1998-08-10 | 2001-11-27 | Boehringer Ingelheim (Canada) Ltd | Hepatitis C inhibitor tri-peptides |
| US6608027B1 (en) | 1999-04-06 | 2003-08-19 | Boehringer Ingelheim (Canada) Ltd | Macrocyclic peptides active against the hepatitis C virus |
| UA74546C2 (en) | 1999-04-06 | 2006-01-16 | Boehringer Ingelheim Ca Ltd | Macrocyclic peptides having activity relative to hepatitis c virus, a pharmaceutical composition and use of the pharmaceutical composition |
| KR20020071931A (ko) * | 2000-01-07 | 2002-09-13 | 트렌스폼 파마수티컬스 인코퍼레이티드 | 다양한 고체-형태들의 고도의 자료 처리 편성, 확인 및분석 |
| UY28240A1 (es) * | 2003-03-27 | 2004-11-08 | Boehringer Ingelheim Pharma | Fases cristalinas de un potente inhibidor de la hcv |
| UY28323A1 (es) * | 2003-05-21 | 2004-12-31 | Boehringer Ingelheim Int | Compuestos inhibidores de la hepatitis c |
| JP5156374B2 (ja) | 2004-05-25 | 2013-03-06 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 非環式ｈｃｖプロテアーゼインヒビターの調製方法 |
| EP2687526A1 (en) * | 2008-09-16 | 2014-01-22 | Boehringer Ingelheim International Gmbh | Crystalline forms of a 2-thiazolyl- 4-quinolinyl-oxy derivative, a potent HCV inhibitor |
| US8530497B2 (en) | 2010-03-11 | 2013-09-10 | Boehringer Ingelheim International Gmbh | Crystalline salts of a potent HCV inhibitor |
-
2009
- 2009-09-14 EP EP13188665.7A patent/EP2687526A1/en not_active Withdrawn
- 2009-09-14 PE PE2012002419A patent/PE20130307A1/es active IP Right Grant
- 2009-09-14 MY MYPI20111140 patent/MY153093A/en unknown
- 2009-09-14 EP EP09792493.0A patent/EP2331538B1/en active Active
- 2009-09-14 RS RS20140230A patent/RS53292B/en unknown
- 2009-09-14 ES ES09792493.0T patent/ES2474992T3/es active Active
- 2009-09-14 JP JP2011527015A patent/JP5520301B2/ja active Active
- 2009-09-14 NZ NZ602163A patent/NZ602163A/xx not_active IP Right Cessation
- 2009-09-14 MX MX2011002828A patent/MX2011002828A/es active IP Right Grant
- 2009-09-14 PL PL09792493T patent/PL2331538T3/pl unknown
- 2009-09-14 AU AU2009293494A patent/AU2009293494B2/en not_active Ceased
- 2009-09-14 ME MEP-2014-43A patent/ME01831B/me unknown
- 2009-09-14 CN CN200980136131.XA patent/CN102159571B/zh not_active Expired - Fee Related
- 2009-09-14 EA EA201100482A patent/EA018603B1/ru not_active IP Right Cessation
- 2009-09-14 KR KR1020117004209A patent/KR101653550B1/ko active IP Right Grant
- 2009-09-14 SI SI200930919T patent/SI2331538T1/sl unknown
- 2009-09-14 SG SG2013024864A patent/SG189740A1/en unknown
- 2009-09-14 WO PCT/US2009/056772 patent/WO2010033444A1/en active Application Filing
- 2009-09-14 DK DK09792493.0T patent/DK2331538T3/da active
- 2009-09-14 BR BRPI0918513A patent/BRPI0918513A2/pt not_active Application Discontinuation
- 2009-09-14 NZ NZ591013A patent/NZ591013A/xx not_active IP Right Cessation
- 2009-09-14 CA CA2737055A patent/CA2737055C/en not_active Expired - Fee Related
- 2009-09-14 PE PE2011000636A patent/PE20110388A1/es not_active Application Discontinuation
- 2009-09-14 PT PT97924930T patent/PT2331538E/pt unknown
- 2009-09-15 TW TW98131069A patent/TWI471323B/zh not_active IP Right Cessation
- 2009-09-15 AR ARP090103540A patent/AR073298A1/es not_active Application Discontinuation
- 2009-09-15 US US12/559,927 patent/US8232293B2/en active Active
- 2009-09-15 UY UY0001032119A patent/UY32119A/es not_active Application Discontinuation
-
2010
- 2010-12-29 IL IL210345A patent/IL210345A/en active IP Right Grant
-
2011
- 2011-01-04 ZA ZA2011/00096A patent/ZA201100096B/en unknown
- 2011-03-09 EC EC2011010878A patent/ECSP11010878A/es unknown
- 2011-03-14 MA MA33699A patent/MA32633B1/fr unknown
- 2011-03-16 CL CL2011000558A patent/CL2011000558A1/es unknown
- 2011-03-16 CO CO11032830A patent/CO6351741A2/es not_active Application Discontinuation
- 2011-10-17 HK HK11111031.5A patent/HK1156624A1/xx not_active IP Right Cessation
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2012
- 2012-07-03 US US13/541,158 patent/US8362035B2/en active Active
-
2013
- 2013-12-09 JP JP2013253812A patent/JP2014062116A/ja not_active Withdrawn
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2014
- 2014-07-11 CY CY20141100526T patent/CY1115253T1/el unknown
- 2014-07-14 HR HRP20140666AT patent/HRP20140666T1/hr unknown
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