JP4705956B2 - Hivインテグラーゼ阻害剤のカリウム塩 - Google Patents

Hivインテグラーゼ阻害剤のカリウム塩 Download PDF

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Publication number
JP4705956B2
JP4705956B2 JP2007544570A JP2007544570A JP4705956B2 JP 4705956 B2 JP4705956 B2 JP 4705956B2 JP 2007544570 A JP2007544570 A JP 2007544570A JP 2007544570 A JP2007544570 A JP 2007544570A JP 4705956 B2 JP4705956 B2 JP 4705956B2
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Japan
Prior art keywords
compound
solution
potassium
solvent
mixture
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Expired - Lifetime
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JP2007544570A
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English (en)
Japanese (ja)
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JP2008521933A (ja
JP2008521933A5 (https=
Inventor
ベリク,ケビン・エム
モリソン,ヘンリー・ジー
ジヨーンズ,フイリツプ
スンマ,ビンセンツオ
クーパー,ブイ・ブレツト
マハジヤン,アマール・ジエイ
クムケ,ダニエル・ジエイ
トン,シエン−シン
ワイ,ローレンス
プルジンスキー,バネツサ
パイ,フイリツプ
アンジユロー,レミ
マンチエーニヨ,ダニー
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Merck and Co Inc
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Merck and Co Inc
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Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of JP2008521933A publication Critical patent/JP2008521933A/ja
Publication of JP2008521933A5 publication Critical patent/JP2008521933A5/ja
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545Two 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
    • C07D239/557Two 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D313/00Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
    • C07D313/02Seven-membered rings
    • C07D313/06Seven-membered rings condensed with carbocyclic rings or ring systems
    • C07D313/10Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
    • C07D313/12[b,e]-condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (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)
JP2007544570A 2004-12-03 2005-12-02 Hivインテグラーゼ阻害剤のカリウム塩 Expired - Lifetime JP4705956B2 (ja)

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 JP2008521933A5 (https=) 2010-12-24
JP4705956B2 true 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)

Country Link
US (2) US7754731B2 (https=)
EP (2) EP1819700B1 (https=)
JP (1) JP4705956B2 (https=)
KR (2) KR20130122031A (https=)
CN (1) CN101068793B (https=)
AR (2) AR052034A1 (https=)
AT (2) ATE518844T1 (https=)
AU (1) AU2005311671B8 (https=)
BR (1) BRPI0518760A8 (https=)
CA (1) CA2588398C (https=)
CR (1) CR9146A (https=)
CY (1) CY1112859T1 (https=)
DK (1) DK1819700T3 (https=)
EA (1) EA012418B1 (https=)
ES (2) ES2375788T3 (https=)
GE (1) GEP20105086B (https=)
HR (1) HRP20120066T1 (https=)
IL (1) IL183614A (https=)
MA (1) MA29120B1 (https=)
ME (1) ME01985B (https=)
MX (1) MX2007006639A (https=)
MY (1) MY144320A (https=)
NI (1) NI200700138A (https=)
NO (1) NO338784B1 (https=)
NZ (1) NZ555376A (https=)
PE (1) PE20061148A1 (https=)
PL (1) PL1819700T3 (https=)
PT (1) PT1819700E (https=)
RS (1) RS52197B (https=)
SI (1) SI1819700T1 (https=)
TN (1) TNSN07215A1 (https=)
TW (1) TWI344463B (https=)
UA (1) UA87884C2 (https=)
WO (2) WO2006060730A2 (https=)
ZA (1) ZA200704130B (https=)

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EP1819323B2 (en) * 2004-12-03 2023-03-22 Merck Sharp & Dohme Corp. Pharmaceutical composition containing an anti-nucleating agent
MX2007006635A (es) * 2004-12-03 2007-06-19 Merck & Co Inc Formulacion farmaceutica de inhibidores dela carboxamida vih integrasa que contienen una composicion que controla la velocidad de liberacion.
WO2007106768A2 (en) * 2006-03-14 2007-09-20 Merck & Co., Inc. Processes and apparatuses for the production of crystalline organic microparticle compositions by micro-milling and crystallization on micro-seed and their use
EP2046328A4 (en) 2006-07-19 2009-10-28 Univ Georgia Res Found PYRIDINONE DIKETOIC 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
CN101918372B (zh) * 2008-01-08 2014-03-26 默沙东公司 用于制备n-取代的羟基嘧啶酮羧酰胺类化合物的方法
US8742105B2 (en) 2009-06-02 2014-06-03 Hetero Research Foundation Polymorphs of raltegravir potassium
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WO2013037731A1 (de) 2011-09-16 2013-03-21 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
ES2825029T3 (es) 2011-12-26 2021-05-14 Emcure Pharmaceuticals Ltd Síntesis de raltegravir
WO2013111100A1 (en) 2012-01-25 2013-08-01 Lupin Limited Stable amorphous raltegravir potassium premix and process for the preparation thereof
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US10391178B2 (en) * 2014-03-21 2019-08-27 Mylan Laboratories Limited Premix of crystalline raltegravir potassium salt and a process for the preparation thereof
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Also Published As

Publication number Publication date
MX2007006639A (es) 2007-06-19
AR052034A1 (es) 2007-02-28
EA200701204A1 (ru) 2007-12-28
EA012418B1 (ru) 2009-10-30
AR101429A2 (es) 2016-12-21
EP1819683A2 (en) 2007-08-22
RS52197B (sr) 2012-10-31
EP1819683B1 (en) 2011-08-03
WO2006060730A3 (en) 2006-08-17
ES2370136T3 (es) 2011-12-13
ES2375788T3 (es) 2012-03-06
CY1112859T1 (el) 2016-04-13
ATE534645T1 (de) 2011-12-15
EP1819700A2 (en) 2007-08-22
IL183614A0 (en) 2007-09-20
US8357798B2 (en) 2013-01-22
HRP20120066T1 (hr) 2012-03-31
CA2588398C (en) 2011-07-12
KR20070089990A (ko) 2007-09-04
JP2008521933A (ja) 2008-06-26
US7754731B2 (en) 2010-07-13
ZA200704130B (en) 2008-08-27
GEP20105086B (en) 2010-10-11
TNSN07215A1 (en) 2008-11-21
EP1819700B1 (en) 2011-11-23
US20060122205A1 (en) 2006-06-08
PL1819700T3 (pl) 2012-04-30
TWI344463B (en) 2011-07-01
CN101068793B (zh) 2011-05-25
WO2006060712A3 (en) 2006-09-21
WO2006060712A2 (en) 2006-06-08
IL183614A (en) 2012-03-29
ATE518844T1 (de) 2011-08-15
KR20130122031A (ko) 2013-11-06
BRPI0518760A8 (pt) 2017-12-12
ME01985B (me) 2012-10-31
US20100249410A1 (en) 2010-09-30
UA87884C2 (uk) 2009-08-25
NO338784B1 (no) 2016-10-17
NO20073404L (no) 2007-07-02
SI1819700T1 (sl) 2012-07-31
NZ555376A (en) 2009-11-27
MA29120B1 (fr) 2007-12-03
WO2006060730A2 (en) 2006-06-08
NI200700138A (es) 2008-05-13
PT1819700E (pt) 2012-02-01
TW200631944A (en) 2006-09-16
DK1819700T3 (da) 2012-03-19
HK1115011A1 (en) 2008-11-14
AU2005311671A1 (en) 2006-06-08
CN101068793A (zh) 2007-11-07
BRPI0518760A2 (pt) 2008-12-09
CR9146A (es) 2007-10-04
CA2588398A1 (en) 2006-06-08
MY144320A (en) 2011-08-29
AU2005311671B2 (en) 2011-01-27
KR101350420B1 (ko) 2014-02-17
PE20061148A1 (es) 2006-11-09
WO2006060712A9 (en) 2006-07-27
AU2005311671B8 (en) 2011-02-10

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