JP2008521933A5 - - Google Patents
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- Publication number
- JP2008521933A5 JP2008521933A5 JP2007544570A JP2007544570A JP2008521933A5 JP 2008521933 A5 JP2008521933 A5 JP 2008521933A5 JP 2007544570 A JP2007544570 A JP 2007544570A JP 2007544570 A JP2007544570 A JP 2007544570A JP 2008521933 A5 JP2008521933 A5 JP 2008521933A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- solution
- salt
- crystalline
- seed crystal
- 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.)
- Granted
Links
- 229940126062 Compound A Drugs 0.000 description 48
- 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 description 47
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 31
- 239000013078 crystal Substances 0.000 description 29
- 239000000243 solution Substances 0.000 description 27
- 150000003839 salts Chemical class 0.000 description 20
- 238000000034 method Methods 0.000 description 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 14
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 12
- 239000000203 mixture Substances 0.000 description 10
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 8
- 238000010899 nucleation Methods 0.000 description 8
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 8
- 239000002585 base Substances 0.000 description 7
- 238000002425 crystallisation Methods 0.000 description 5
- 230000008025 crystallization Effects 0.000 description 5
- 239000002002 slurry Substances 0.000 description 5
- 239000007864 aqueous solution Substances 0.000 description 4
- 238000001914 filtration Methods 0.000 description 4
- 229910052757 nitrogen Inorganic materials 0.000 description 4
- 239000003960 organic solvent Substances 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 3
- 230000032683 aging Effects 0.000 description 3
- 150000001335 aliphatic alkanes Chemical class 0.000 description 3
- 239000003637 basic solution Substances 0.000 description 3
- 238000004128 high performance liquid chromatography Methods 0.000 description 3
- 229910052700 potassium Inorganic materials 0.000 description 3
- 239000011591 potassium Substances 0.000 description 3
- 239000000725 suspension Substances 0.000 description 3
- 238000005406 washing Methods 0.000 description 3
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 2
- SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 description 2
- 238000003556 assay Methods 0.000 description 2
- 150000004292 cyclic ethers Chemical class 0.000 description 2
- -1 dialkoxyalkanes Chemical class 0.000 description 2
- 150000001983 dialkylethers Chemical class 0.000 description 2
- 238000007865 diluting Methods 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 230000001939 inductive effect Effects 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 150000003511 tertiary amides Chemical class 0.000 description 2
- 125000005270 trialkylamine group Chemical group 0.000 description 2
- GSNUFIFRDBKVIE-UHFFFAOYSA-N DMF Natural products CC1=CC=C(C)O1 GSNUFIFRDBKVIE-UHFFFAOYSA-N 0.000 description 1
- AHVYPIQETPWLSZ-UHFFFAOYSA-N N-methyl-pyrrolidine Natural products CN1CC=CC1 AHVYPIQETPWLSZ-UHFFFAOYSA-N 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000007791 liquid phase Substances 0.000 description 1
- 239000012452 mother liquor Substances 0.000 description 1
- 150000002825 nitriles Chemical class 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000012429 reaction media Substances 0.000 description 1
- 239000012266 salt solution Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 150000003462 sulfoxides Chemical class 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63313204P | 2004-12-03 | 2004-12-03 | |
| US60/633,132 | 2004-12-03 | ||
| PCT/US2005/043781 WO2006060730A2 (en) | 2004-12-03 | 2005-12-02 | Potassium salt of an hiv integrase inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008521933A JP2008521933A (ja) | 2008-06-26 |
| JP2008521933A5 true JP2008521933A5 (cg-RX-API-DMAC7.html) | 2010-12-24 |
| JP4705956B2 JP4705956B2 (ja) | 2011-06-22 |
Family
ID=36171569
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007544570A Expired - Lifetime JP4705956B2 (ja) | 2004-12-03 | 2005-12-02 | Ｈｉｖインテグラーゼ阻害剤のカリウム塩 |
Country Status (35)
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1725528T3 (da) | 2004-03-11 | 2013-09-02 | 4Sc Ag | Sulfonylpyrroler som hdac-inhibitorer |
| CA2588466A1 (en) * | 2004-12-03 | 2006-06-08 | Merck & Co., Inc. | Use of atazanavir for improving the pharmacokinetics of drugs metabolized by ugt1a1 |
| CN101068533B (zh) * | 2004-12-03 | 2011-04-27 | 默沙东公司 | 含有抗成核剂的药物组合物 |
| NZ555120A (en) * | 2004-12-03 | 2009-11-27 | Merck & Co Inc | Pharmaceutical formulation of carboxamide HIV integrase inhibitors containing a release rate controlling composition |
| CN101453986A (zh) * | 2006-03-14 | 2009-06-10 | 默克公司 | 通过微研磨和在微晶种上结晶生产结晶有机微粒组合物的方法和设备及其应用 |
| US20100092427A1 (en) | 2006-07-19 | 2010-04-15 | The University Of Georgia Research Foundation | Pyridinone Diketo Acids: Inhibitors of HIV Replication in Combination Therapy |
| WO2009009531A2 (en) * | 2007-07-09 | 2009-01-15 | Concert Pharmaceuticals Inc. | Pyrimidinecarboxamide derivatives for the treatment of hiv infections |
| EP2231621B1 (en) | 2008-01-08 | 2016-11-02 | Merck Sharp & Dohme Corp. | Process for preparing n-substituted hydroxypyrimidinone carboxamides |
| WO2010140156A2 (en) * | 2009-06-02 | 2010-12-09 | Hetero Research Foundation | Novel polymorphs of raltegravir potassium |
| WO2011024192A2 (en) | 2009-07-27 | 2011-03-03 | Matrix Laboratories Ltd | Novel polymorphs of raltegravir |
| JP6122639B2 (ja) * | 2009-10-26 | 2017-04-26 | メルク・シャープ・エンド・ドーム・コーポレイション | インテグラーゼ阻害剤を含有する固形医薬組成物 |
| DE102009056636A1 (de) | 2009-12-02 | 2011-06-09 | Ratiopharm Gmbh | Raltegravir-Polymorphe |
| US8703801B2 (en) * | 2009-12-07 | 2014-04-22 | University Of Georgia Research Foundation, Inc. | Pyridinone hydroxycyclopentyl carboxamides: HIV integrase inhibitors with therapeutic applications |
| ES2362598B1 (es) * | 2009-12-17 | 2012-06-13 | Consejo Superior De Investigaciones Científicas (Csic) | Uso del raltegravir y derivados para la elaboración de medicamentos destinados al tratamiento de infecciones por herpesvirus. |
| US8987272B2 (en) * | 2010-04-01 | 2015-03-24 | Critical Outcome Technologies Inc. | Compounds and method for treatment of HIV |
| JP5889275B2 (ja) * | 2010-04-01 | 2016-03-22 | テバ ファーマシューティカル インダストリーズ リミティド | ラルテグラビル塩およびその結晶形 |
| WO2011148381A1 (en) * | 2010-05-25 | 2011-12-01 | Hetero Research Foundation | Salts of raltegravir |
| US9107922B2 (en) | 2010-07-16 | 2015-08-18 | Concert Pharmaceuticals, Inc. | Pyrimidinecarboxamide derivatives |
| CN101914067B (zh) * | 2010-08-26 | 2012-07-11 | 陈岱岭 | N-甲基嘧啶酮的合成方法 |
| JO3209B1 (ar) * | 2010-11-05 | 2018-03-08 | H Lundbeck As | طريقة لتصنيع نالتريكسون |
| WO2012103105A1 (en) | 2011-01-24 | 2012-08-02 | Assia Chemical Industries Ltd. | Processes for preparing raltegravir and intermediates in the processes |
| WO2012106534A2 (en) * | 2011-02-02 | 2012-08-09 | The Regents Of The University Of California | Hiv integrase inhibitors |
| US9163009B2 (en) | 2011-04-06 | 2015-10-20 | Lupin Limited | Salts of raltegravir |
| WO2012145446A1 (en) * | 2011-04-22 | 2012-10-26 | Merck Sharp & Dohme Corp. | Taste-masked formulations of raltegravir |
| US9968607B2 (en) | 2011-04-25 | 2018-05-15 | Hetero Research Foundation | Pharmaceutical compositions of raltegravir, methods of preparation and methods of use therof |
| EP2522665A1 (en) | 2011-05-03 | 2012-11-14 | Sandoz Ag | Crystalline sodium salt of an HIV integrase inhibitor |
| ES2450944T3 (es) | 2011-06-01 | 2014-03-25 | Ratiopharm Gmbh | Composición y comprimido que comprenden raltegravir |
| EP2755968A1 (de) | 2011-09-16 | 2014-07-23 | Hexal AG | Neue polymorphe form von raltegravir-kalium |
| CN103130787B (zh) * | 2011-11-24 | 2015-06-10 | 南开大学 | 嘧啶酮酰胺类化合物及其制备方法、抗hiv活性和抗tmv活性 |
| CN103130788B (zh) * | 2011-11-24 | 2015-09-02 | 南开大学 | 嘧啶酰胺类化合物及其制备方法、抗hiv活性和抗tmv活性 |
| WO2013098854A2 (en) * | 2011-12-26 | 2013-07-04 | Emcure Pharmaceuticals Limited | Synthesis of raltegravir |
| US20150328215A1 (en) | 2012-01-25 | 2015-11-19 | Lupin Limited | Stable amorphous raltegravir potassium premix and process for the preparation thereof |
| WO2014064711A2 (en) * | 2012-10-22 | 2014-05-01 | Hetero Research Foundation | Methods of administering raltegravir and raltegravir compositions |
| EP2818470A1 (en) | 2013-06-27 | 2014-12-31 | Basf Se | Cocrystals of raltegravir potassium |
| EP3022209B1 (en) | 2013-07-17 | 2018-03-07 | ratiopharm GmbH | Dolutegravir potassium salt |
| PT3102565T (pt) | 2014-02-03 | 2019-04-01 | Mylan Laboratories Ltd | Processos para a preparação de intermediários de raltegravir |
| CA2942239C (en) | 2014-03-21 | 2020-09-22 | Mylan Laboratories Ltd. | A premix of crystalline raltegravir potassium salt and a process for the preparation thereof |
| US10257840B2 (en) | 2014-10-22 | 2019-04-09 | Telefonaktiebolaget Lm Ericsson (Publ) | Operation of wireless local area network in the presence of periodic interference |
| US10259778B2 (en) | 2014-11-10 | 2019-04-16 | Aurobindo Pharma Ltd | Process for the preparation of raltegravir |
| EP3472134B1 (en) | 2016-06-21 | 2021-10-20 | Pharmathen S.A. | Process for preparing compounds useful as intermediates for the preparation of raltegravir |
| WO2018051239A1 (en) | 2016-09-15 | 2018-03-22 | Lupin Limited | Process for the preparation of pure and stable crystalline raltegravir potassium form 3 |
| CN108610338A (zh) * | 2016-12-12 | 2018-10-02 | 天津国际生物医药联合研究院 | 一种嘧啶酮酰胺类化合物的制备方法 |
| WO2019096773A1 (en) | 2017-11-14 | 2019-05-23 | Cambrex Profarmaco Milano S.R.L. | Process for the preparation of raltegravir |
| US20210290548A1 (en) * | 2018-06-06 | 2021-09-23 | Merck Sharp & Dohme Corp. | Formulations of raltegravir |
| GB201907305D0 (en) * | 2019-05-23 | 2019-07-10 | Douglas Pharmaceuticals Ltd | Treatment of conditions |
| US12465565B2 (en) | 2020-01-23 | 2025-11-11 | Lupin Limited | Pharmaceutical compositions of raltegravir |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH624391A5 (cg-RX-API-DMAC7.html) * | 1976-12-14 | 1981-07-31 | Ciba Geigy Ag | |
| US5717097A (en) | 1991-11-08 | 1998-02-10 | Merck & Co., Inc. | HIV protease inhibitors useful for the treatment of AIDS |
| US5413999A (en) | 1991-11-08 | 1995-05-09 | Merck & Co., Inc. | HIV protease inhibitors useful for the treatment of AIDS |
| IL121789A (en) * | 1996-10-03 | 2001-06-14 | Rohm & Haas | A medicinal product for inhibiting mammalian cell tumors |
| AP2001002169A0 (en) | 1998-12-25 | 2001-06-30 | Shionogi & Co | Aromatic heterocycle compounds having hiv intergrase inhibiting activities |
| IT1318424B1 (it) | 2000-03-24 | 2003-08-25 | Unihart Corp | Composti con attivita' anti-hiv. |
| AU2002211527B2 (en) | 2000-10-12 | 2006-08-24 | Merck Sharp & Dohme Corp. | Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors |
| GB0028483D0 (en) | 2000-11-22 | 2001-01-10 | Hoffmann La Roche | Hydroxyethylamine HIV protease inhibitors |
| CN1700918B (zh) * | 2001-10-26 | 2011-06-08 | P·安杰莱蒂分子生物学研究所 | 关于hiv整合酶的n-取代的羟基嘧啶酮甲酰胺抑制剂 |
| US7354932B2 (en) | 2001-12-21 | 2008-04-08 | Anormed, Inc. | Chemokine receptor binding heterocyclic compounds with enhanced efficacy |
| RU2325387C2 (ru) | 2001-12-21 | 2008-05-27 | Анормед Инк. | Гетероциклические соединения с повышенной эффективностью, связывающиеся с рецептором хемокина |
| KR100665919B1 (ko) | 2002-11-20 | 2007-03-08 | 니뽄 다바코 산교 가부시키가이샤 | 4-옥소퀴놀린 화합물 및 ｈｉｖ 인테그라제 저해제로서의그의 용도 |
| BR0317749A (pt) | 2002-12-27 | 2005-11-22 | Angeletti P Ist Richerche Bio | Composto, composição farmacêutica, e, uso de um composto |
| TW200423930A (en) | 2003-02-18 | 2004-11-16 | Hoffmann La Roche | Non-nucleoside reverse transcriptase inhibitors |
| NZ555120A (en) * | 2004-12-03 | 2009-11-27 | Merck & Co Inc | Pharmaceutical formulation of carboxamide HIV integrase inhibitors containing a release rate controlling composition |
| CA2588466A1 (en) | 2004-12-03 | 2006-06-08 | Merck & Co., Inc. | Use of atazanavir for improving the pharmacokinetics of drugs metabolized by ugt1a1 |
| CN101068533B (zh) | 2004-12-03 | 2011-04-27 | 默沙东公司 | 含有抗成核剂的药物组合物 |
-
2005
- 2005-02-12 UA UAA200707372A patent/UA87884C2/uk unknown
- 2005-11-24 AR ARP050104911A patent/AR052034A1/es not_active Application Discontinuation
- 2005-11-25 MY MYPI20055516A patent/MY144320A/en unknown
- 2005-11-25 TW TW094141625A patent/TWI344463B/zh active
- 2005-12-01 PE PE2005001398A patent/PE20061148A1/es not_active Application Discontinuation
- 2005-12-02 EP EP05852840A patent/EP1819700B1/en not_active Expired - Lifetime
- 2005-12-02 ES ES05852866T patent/ES2370136T3/es not_active Expired - Lifetime
- 2005-12-02 NZ NZ555376A patent/NZ555376A/en unknown
- 2005-12-02 US US11/293,678 patent/US7754731B2/en active Active
- 2005-12-02 WO PCT/US2005/043781 patent/WO2006060730A2/en not_active Ceased
- 2005-12-02 SI SI200531435T patent/SI1819700T1/sl unknown
- 2005-12-02 EP EP05852866A patent/EP1819683B1/en not_active Expired - Lifetime
- 2005-12-02 CA CA2588398A patent/CA2588398C/en not_active Expired - Lifetime
- 2005-12-02 WO PCT/US2005/043728 patent/WO2006060712A2/en not_active Ceased
- 2005-12-02 AT AT05852840T patent/ATE534645T1/de active
- 2005-12-02 MX MX2007006639A patent/MX2007006639A/es active IP Right Grant
- 2005-12-02 ME MEP-2012-21A patent/ME01985B/me unknown
- 2005-12-02 AT AT05852866T patent/ATE518844T1/de active
- 2005-12-02 CN CN2005800416393A patent/CN101068793B/zh not_active Expired - Lifetime
- 2005-12-02 PT PT05852840T patent/PT1819700E/pt unknown
- 2005-12-02 PL PL05852840T patent/PL1819700T3/pl unknown
- 2005-12-02 EA EA200701204A patent/EA012418B1/ru not_active IP Right Cessation
- 2005-12-02 KR KR1020077015278A patent/KR101350420B1/ko not_active Expired - Lifetime
- 2005-12-02 DK DK05852840.7T patent/DK1819700T3/da active
- 2005-12-02 JP JP2007544570A patent/JP4705956B2/ja not_active Expired - Lifetime
- 2005-12-02 BR BRPI0518760A patent/BRPI0518760A8/pt not_active Application Discontinuation
- 2005-12-02 ES ES05852840T patent/ES2375788T3/es not_active Expired - Lifetime
- 2005-12-02 GE GEAP200510157A patent/GEP20105086B/en unknown
- 2005-12-02 KR KR1020137028450A patent/KR20130122031A/ko not_active Withdrawn
- 2005-12-02 AU AU2005311671A patent/AU2005311671B8/en not_active Expired
- 2005-12-02 RS RS20120021A patent/RS52197B/sr unknown
- 2005-12-02 HR HR20120066T patent/HRP20120066T1/hr unknown
-
2007
- 2007-05-22 ZA ZA200704130A patent/ZA200704130B/xx unknown
- 2007-05-23 CR CR9146A patent/CR9146A/es not_active Application Discontinuation
- 2007-05-28 NI NI200700138A patent/NI200700138A/es unknown
- 2007-05-31 IL IL183614A patent/IL183614A/en active IP Right Grant
- 2007-06-01 TN TNP2007000215A patent/TNSN07215A1/fr unknown
- 2007-06-29 MA MA30041A patent/MA29120B1/fr unknown
- 2007-07-02 NO NO20073404A patent/NO338784B1/no unknown
-
2010
- 2010-06-04 US US12/793,801 patent/US8357798B2/en active Active
-
2012
- 2012-02-21 CY CY20121100173T patent/CY1112859T1/el unknown
-
2014
- 2014-04-24 AR ARP140101707A patent/AR101429A2/es not_active Application Discontinuation
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