GEP20105086B - Potassium salt of an hiv integrase inhibitor - Google Patents
Potassium salt of an hiv integrase inhibitorInfo
- Publication number
- GEP20105086B GEP20105086B GEAP200510157A GEAP2005010157A GEP20105086B GE P20105086 B GEP20105086 B GE P20105086B GE AP200510157 A GEAP200510157 A GE AP200510157A GE AP2005010157 A GEAP2005010157 A GE AP2005010157A GE P20105086 B GEP20105086 B GE P20105086B
- Authority
- GE
- Georgia
- Prior art keywords
- potassium salt
- hiv integrase
- integrase inhibitor
- radiation
- copper
- Prior art date
Links
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 title abstract 2
- 229940099797 HIV integrase inhibitor Drugs 0.000 title 1
- 239000003084 hiv integrase inhibitor Substances 0.000 title 1
- 229940126062 Compound A Drugs 0.000 abstract 1
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 abstract 1
- 108010002459 HIV Integrase Proteins 0.000 abstract 1
- 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 abstract 1
- 229910052802 copper Inorganic materials 0.000 abstract 1
- 239000010949 copper Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
- 230000005855 radiation Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
- C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/557—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D313/00—Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
- C07D313/02—Seven-membered rings
- C07D313/06—Seven-membered rings condensed with carbocyclic rings or ring systems
- C07D313/10—Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
- C07D313/12—[b,e]-condensed
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Virology (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63313204P | 2004-12-03 | 2004-12-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| GEP20105086B true GEP20105086B (en) | 2010-10-11 |
Family
ID=36171569
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GEAP200510157A GEP20105086B (en) | 2004-12-03 | 2005-12-02 | Potassium salt of an hiv integrase inhibitor |
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 |
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| 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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