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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JP
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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JP2008521933A5 (enExample
JP2008521933A (ja
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
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Publication of JP2008521933A5 publication Critical patent/JP2008521933A5/ja
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    • 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
    • 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (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 (enExample) 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 (enExample)
EP (2) EP1819700B1 (enExample)
JP (1) JP4705956B2 (enExample)
KR (2) KR20130122031A (enExample)
CN (1) CN101068793B (enExample)
AR (2) AR052034A1 (enExample)
AT (2) ATE534645T1 (enExample)
AU (1) AU2005311671B8 (enExample)
BR (1) BRPI0518760A8 (enExample)
CA (1) CA2588398C (enExample)
CR (1) CR9146A (enExample)
CY (1) CY1112859T1 (enExample)
DK (1) DK1819700T3 (enExample)
EA (1) EA012418B1 (enExample)
ES (2) ES2375788T3 (enExample)
GE (1) GEP20105086B (enExample)
HR (1) HRP20120066T1 (enExample)
IL (1) IL183614A (enExample)
MA (1) MA29120B1 (enExample)
ME (1) ME01985B (enExample)
MX (1) MX2007006639A (enExample)
MY (1) MY144320A (enExample)
NI (1) NI200700138A (enExample)
NO (1) NO338784B1 (enExample)
NZ (1) NZ555376A (enExample)
PE (1) PE20061148A1 (enExample)
PL (1) PL1819700T3 (enExample)
PT (1) PT1819700E (enExample)
RS (1) RS52197B (enExample)
SI (1) SI1819700T1 (enExample)
TN (1) TNSN07215A1 (enExample)
TW (1) TWI344463B (enExample)
UA (1) UA87884C2 (enExample)
WO (2) WO2006060730A2 (enExample)
ZA (1) ZA200704130B (enExample)

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EP3165220B2 (en) † 2004-12-03 2024-11-13 Merck Sharp & Dohme LLC Pharmaceutical composition containing an anti-nucleating agent
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
CA2642504A1 (en) * 2006-03-14 2007-09-20 Brian K. Johnson Processes and apparatuses for the production of crystalline organic microparticle compositions by micro-milling and crystallization on micro-seed and their use
CA2657034A1 (en) 2006-07-19 2008-01-24 University Of Georgia Research Foundation, Inc. Pyridinone diketo acids: inhibitors of hiv replication in combination therapy
US7687509B2 (en) 2007-07-09 2010-03-30 Concert Pharmaceuticals Inc. Pyrimidinecarboxamide derivatives
EP2231621B1 (en) * 2008-01-08 2016-11-02 Merck Sharp & Dohme Corp. Process for preparing n-substituted hydroxypyrimidinone carboxamides
US8742105B2 (en) 2009-06-02 2014-06-03 Hetero Research Foundation Polymorphs of raltegravir potassium
WO2011024192A2 (en) 2009-07-27 2011-03-03 Matrix Laboratories Ltd Novel polymorphs of raltegravir
AU2010313571B2 (en) 2009-10-26 2014-07-31 Merck Sharp & Dohme Llc Solid pharmaceutical compositions containing an integrase inhibitor
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CN101914067B (zh) * 2010-08-26 2012-07-11 陈岱岭 N-甲基嘧啶酮的合成方法
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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
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RU2382648C2 (ru) 2004-12-03 2010-02-27 Мерк Энд Ко., Инк. Фармацевтический состав карбоксамидных ингибиторов интегразы вич, содержащий композицию с контролируемой скоростью высвобождения
EP3165220B2 (en) 2004-12-03 2024-11-13 Merck Sharp & Dohme LLC Pharmaceutical composition containing an anti-nucleating agent

Also Published As

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

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