JP2008521929A5 - - Google Patents
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- Publication number
- JP2008521929A5 JP2008521929A5 JP2007544548A JP2007544548A JP2008521929A5 JP 2008521929 A5 JP2008521929 A5 JP 2008521929A5 JP 2007544548 A JP2007544548 A JP 2007544548A JP 2007544548 A JP2007544548 A JP 2007544548A JP 2008521929 A5 JP2008521929 A5 JP 2008521929A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- compound
- alkyl
- diluent
- composition according
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 25
- 239000003085 diluting agent Substances 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 229940126062 Compound A Drugs 0.000 claims 15
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 15
- 230000002821 anti-nucleating effect Effects 0.000 claims 13
- 239000000203 mixture Substances 0.000 claims 13
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical group [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 11
- 239000003795 chemical substances by application Substances 0.000 claims 9
- 239000007884 disintegrant Substances 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 7
- 239000000314 lubricant Substances 0.000 claims 7
- 150000003839 salts Chemical group 0.000 claims 7
- 229940079593 drug Drugs 0.000 claims 6
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 6
- 238000000034 method Methods 0.000 claims 5
- 239000003826 tablet Substances 0.000 claims 5
- 235000019739 Dicalciumphosphate Nutrition 0.000 claims 4
- 239000001506 calcium phosphate Substances 0.000 claims 4
- NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 claims 4
- 229940038472 dicalcium phosphate Drugs 0.000 claims 4
- 229910000390 dicalcium phosphate Inorganic materials 0.000 claims 4
- 239000008187 granular material Substances 0.000 claims 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 4
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 4
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 4
- 239000008101 lactose Substances 0.000 claims 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 4
- 239000002667 nucleating agent Substances 0.000 claims 4
- -1 -O-C 1-4 haloalkyl Chemical group 0.000 claims 3
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 3
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 3
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical group [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 3
- 229960001681 croscarmellose sodium Drugs 0.000 claims 3
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 3
- 239000008108 microcrystalline cellulose Substances 0.000 claims 3
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000007787 solid Substances 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 208000030507 AIDS Diseases 0.000 claims 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 2
- 208000031886 HIV Infections Diseases 0.000 claims 2
- 108010002459 HIV Integrase Proteins 0.000 claims 2
- 208000037357 HIV infectious disease Diseases 0.000 claims 2
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims 2
- 239000002585 base Substances 0.000 claims 2
- 239000007891 compressed tablet Substances 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 2
- 229920013821 hydroxy alkyl cellulose Polymers 0.000 claims 2
- 235000019359 magnesium stearate Nutrition 0.000 claims 2
- 238000003801 milling Methods 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 239000002893 slag Substances 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 229920002125 Sokalan® Polymers 0.000 claims 1
- 229910052783 alkali metal Inorganic materials 0.000 claims 1
- 229920013820 alkyl cellulose Polymers 0.000 claims 1
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 229940126534 drug product Drugs 0.000 claims 1
- 238000001035 drying Methods 0.000 claims 1
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000001050 lubricating effect Effects 0.000 claims 1
- DKXULEFCEORBJK-UHFFFAOYSA-N magnesium;octadecanoic acid Chemical compound [Mg].CCCCCCCCCCCCCCCCCC(O)=O DKXULEFCEORBJK-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000004584 polyacrylic acid Substances 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 238000005096 rolling process Methods 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229920003169 water-soluble polymer Polymers 0.000 claims 1
- CZFFBEXEKNGXKS-UHFFFAOYSA-N CC(C)(C(N(C)C1=O)=NC(C(NCc(cc2)ccc2F)=O)=C1O)NC(c1nnc(C)[o]1)=O Chemical compound CC(C)(C(N(C)C1=O)=NC(C(NCc(cc2)ccc2F)=O)=C1O)NC(c1nnc(C)[o]1)=O CZFFBEXEKNGXKS-UHFFFAOYSA-N 0.000 description 3
- 0 *N(*)C(C(N=C(N(*)C1=O)I)=C1O)=O Chemical compound *N(*)C(C(N=C(N(*)C1=O)I)=C1O)=O 0.000 description 2
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63285904P | 2004-12-03 | 2004-12-03 | |
| PCT/US2005/043675 WO2006060681A2 (en) | 2004-12-03 | 2005-12-02 | Pharmaceutical composition containing an anti-nucleating agent |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012116010A Division JP2012184250A (ja) | 2004-12-03 | 2012-05-21 | 抗核形成剤を含有する医薬組成物 |
| JP2012260995A Division JP2013063999A (ja) | 2004-12-03 | 2012-11-29 | 抗核形成剤を含有する医薬組成物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008521929A JP2008521929A (ja) | 2008-06-26 |
| JP2008521929A5 true JP2008521929A5 (https=) | 2009-01-22 |
Family
ID=36565788
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007544548A Pending JP2008521929A (ja) | 2004-12-03 | 2005-12-02 | 抗核形成剤を含有する医薬組成物 |
| JP2012116010A Pending JP2012184250A (ja) | 2004-12-03 | 2012-05-21 | 抗核形成剤を含有する医薬組成物 |
| JP2012260995A Pending JP2013063999A (ja) | 2004-12-03 | 2012-11-29 | 抗核形成剤を含有する医薬組成物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012116010A Pending JP2012184250A (ja) | 2004-12-03 | 2012-05-21 | 抗核形成剤を含有する医薬組成物 |
| JP2012260995A Pending JP2013063999A (ja) | 2004-12-03 | 2012-11-29 | 抗核形成剤を含有する医薬組成物 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8771733B2 (https=) |
| EP (2) | EP1819323B2 (https=) |
| JP (3) | JP2008521929A (https=) |
| CN (1) | CN101068533B (https=) |
| AU (1) | AU2005311714B2 (https=) |
| CA (1) | CA2588465C (https=) |
| ES (1) | ES2727577T5 (https=) |
| TR (1) | TR201907729T4 (https=) |
| WO (1) | WO2006060681A2 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA87884C2 (uk) | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
| EP1819323B2 (en) | 2004-12-03 | 2023-03-22 | Merck Sharp & Dohme Corp. | Pharmaceutical composition containing an anti-nucleating agent |
| EP1904067B2 (en) | 2004-12-03 | 2017-10-11 | Merck Sharp & Dohme Corp. | Pharmaceutical formulation of carboxamide hiv integrase inhibitors containing a release rate controlling composition |
| BRPI0518741A2 (pt) * | 2004-12-03 | 2008-12-02 | Merck & Co Inc | uso de uma combinaÇço de uma droga diretamente metabolizada por ugt1a1 ou um seu sal farmaceuticamente aceitÁvel e atazanavir ou um seu sal farmaceuticamente aceitÁvel, e, combinaÇço farmacÊutica para administraÇço oral a um mamÍfero |
| CN101595133B (zh) * | 2006-10-27 | 2012-11-14 | 比利时胶囊公司 | 羟丙基甲基纤维素硬胶囊及制备方法 |
| CN101197832B (zh) * | 2007-12-13 | 2012-01-25 | 华为技术有限公司 | 一种实现iptv业务的方法、系统、装置 |
| EP2438062B1 (en) * | 2009-06-02 | 2015-07-29 | Hetero Research Foundation | Process for the preparation of amorphous raltegravir potassium |
| US9649311B2 (en) * | 2009-10-26 | 2017-05-16 | Merck Sharp & Dohme Corp. | Solid pharmaceutical compositions containing an integrase inhibitor |
| EP2545048B1 (en) * | 2010-04-01 | 2014-10-08 | Teva Pharmaceutical Industries Ltd. | Raltegravir salts and crystalline forms thereof |
| US9968607B2 (en) | 2011-04-25 | 2018-05-15 | Hetero Research Foundation | Pharmaceutical compositions of raltegravir, methods of preparation and methods of use therof |
| US12472475B2 (en) | 2018-02-02 | 2025-11-18 | The General Hospital Corporation | Methods of supercooling aqueous samples |
| EP4093380A1 (en) | 2020-01-23 | 2022-11-30 | Lupin Limited | Pharmaceutical compositions of raltegravir |
| US20230277587A1 (en) * | 2022-03-03 | 2023-09-07 | Dermacisen, S.A. | Food supplement for oral administration |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4540566A (en) * | 1984-04-02 | 1985-09-10 | Forest Laboratories, Inc. | Prolonged release drug dosage forms based on modified low viscosity grade hydroxypropylmethylcellulose |
| JPH0347124A (ja) * | 1989-04-20 | 1991-02-28 | Fujisawa Pharmaceut Co Ltd | 経口吸収用製剤 |
| CA2019324C (en) * | 1989-07-10 | 1996-08-20 | Robert L. Jerzewski | Fosinopril tablet formulations |
| JP2707023B2 (ja) * | 1992-07-01 | 1998-01-28 | 株式会社大塚製薬工場 | 経口吸収用製剤 |
| AU6329599A (en) † | 1998-09-28 | 2000-04-17 | Glaxo Group Limited | Antiviral combinations comprising (s)-2-ethyl -7-fluoro -3-oxo-3, 4-dihydro -2h-quinoxaline -1-carboxylic acid isopropyl ester |
| PL348596A1 (en) * | 1998-12-25 | 2002-06-03 | Shionogi & Co | Aromatic heterocycle compounds having hiv integrase inhibiting activities |
| GB9922963D0 (en) * | 1999-09-28 | 1999-12-01 | Pfizer Ltd | Polymorphic salt |
| AU783981C (en) * | 2000-05-08 | 2007-05-03 | Janssen Pharmaceutica N.V. | HIV replication inhibitors |
| US7115565B2 (en) † | 2001-01-18 | 2006-10-03 | Pharmacia & Upjohn Company | Chemotherapeutic microemulsion compositions of paclitaxel with improved oral bioavailability |
| ATE355064T1 (de) * | 2001-10-26 | 2006-03-15 | Angeletti P Ist Richerche Bio | Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase |
| IL161337A0 (en) * | 2001-10-26 | 2004-09-27 | Angeletti P Ist Richerche Bio | N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase |
| AU2003220186A1 (en) † | 2002-04-10 | 2003-10-27 | Merck And Co., Inc. | Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant |
| NZ540729A (en) * | 2002-12-27 | 2008-03-28 | Angeletti P Ist Richerche Bio | Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds useful as HIV integrase inhibitors |
| DK1583542T3 (da) † | 2003-01-14 | 2008-09-22 | Gilead Sciences Inc | Sammensætninger og fremgangsmåder til antiviral kombinationsterapi |
| UA87884C2 (uk) * | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
| EP1904067B2 (en) | 2004-12-03 | 2017-10-11 | Merck Sharp & Dohme Corp. | Pharmaceutical formulation of carboxamide hiv integrase inhibitors containing a release rate controlling composition |
| BRPI0518741A2 (pt) | 2004-12-03 | 2008-12-02 | Merck & Co Inc | uso de uma combinaÇço de uma droga diretamente metabolizada por ugt1a1 ou um seu sal farmaceuticamente aceitÁvel e atazanavir ou um seu sal farmaceuticamente aceitÁvel, e, combinaÇço farmacÊutica para administraÇço oral a um mamÍfero |
| EP1819323B2 (en) | 2004-12-03 | 2023-03-22 | Merck Sharp & Dohme Corp. | Pharmaceutical composition containing an anti-nucleating agent |
| US9968607B2 (en) | 2011-04-25 | 2018-05-15 | Hetero Research Foundation | Pharmaceutical compositions of raltegravir, methods of preparation and methods of use therof |
-
2005
- 2005-12-02 EP EP05852790.4A patent/EP1819323B2/en not_active Expired - Lifetime
- 2005-12-02 CA CA2588465A patent/CA2588465C/en not_active Expired - Fee Related
- 2005-12-02 ES ES16198994T patent/ES2727577T5/es not_active Expired - Lifetime
- 2005-12-02 TR TR2019/07729T patent/TR201907729T4/tr unknown
- 2005-12-02 US US11/792,190 patent/US8771733B2/en active Active
- 2005-12-02 WO PCT/US2005/043675 patent/WO2006060681A2/en not_active Ceased
- 2005-12-02 CN CN2005800415795A patent/CN101068533B/zh not_active Expired - Fee Related
- 2005-12-02 AU AU2005311714A patent/AU2005311714B2/en not_active Ceased
- 2005-12-02 JP JP2007544548A patent/JP2008521929A/ja active Pending
- 2005-12-02 EP EP16198994.2A patent/EP3165220B2/en not_active Expired - Lifetime
-
2012
- 2012-05-21 JP JP2012116010A patent/JP2012184250A/ja active Pending
- 2012-11-29 JP JP2012260995A patent/JP2013063999A/ja active Pending
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