CN101068793B - Hiv整合酶抑制剂的钾盐 - Google Patents

Hiv整合酶抑制剂的钾盐 Download PDF

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Publication number
CN101068793B
CN101068793B CN2005800416393A CN200580041639A CN101068793B CN 101068793 B CN101068793 B CN 101068793B CN 2005800416393 A CN2005800416393 A CN 2005800416393A CN 200580041639 A CN200580041639 A CN 200580041639A CN 101068793 B CN101068793 B CN 101068793B
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China
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compound
solution
potassium salt
temperature
salt
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Expired - Lifetime
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CN2005800416393A
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Chinese (zh)
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CN101068793A (zh
Inventor
K·M·贝利克
H·G·莫里森
P·琼斯
V·萨马
V·B·库珀
A·J·马哈延
D·J·库姆克
H·-H·唐
L·魏
V·普鲁津斯基
P·佩
R·安热洛
D·曼切诺
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Msd Uk Ltd
MSD Italia SRL
Merck Sharp and Dohme BV
Original Assignee
Merck Sharp and Dohme Ltd
Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
Schering Corp
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Application filed by Merck Sharp and Dohme Ltd, Istituto di Ricerche di Biologia Molecolare P Angeletti SpA, Schering Corp filed Critical Merck Sharp and Dohme Ltd
Publication of CN101068793A publication Critical patent/CN101068793A/zh
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    • 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
    • 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
    • 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
    • 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

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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)
  • 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)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN2005800416393A 2004-12-03 2005-12-02 Hiv整合酶抑制剂的钾盐 Expired - Lifetime CN101068793B (zh)

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 (2)

Publication Number Publication Date
CN101068793A CN101068793A (zh) 2007-11-07
CN101068793B true CN101068793B (zh) 2011-05-25

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CN2005800416393A Expired - Lifetime CN101068793B (zh) 2004-12-03 2005-12-02 Hiv整合酶抑制剂的钾盐

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US (2) US7754731B2 (https=)
EP (2) EP1819683B1 (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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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
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
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US7687509B2 (en) * 2007-07-09 2010-03-30 Concert Pharmaceuticals Inc. Pyrimidinecarboxamide derivatives
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US9649311B2 (en) 2009-10-26 2017-05-16 Merck Sharp & Dohme Corp. Solid pharmaceutical compositions containing an integrase inhibitor
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AU2012245524A1 (en) * 2011-04-22 2013-10-24 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
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WO2013037731A1 (de) 2011-09-16 2013-03-21 Hexal Ag Neue polymorphe form von raltegravir-kalium
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
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
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KR20130122031A (ko) 2013-11-06
HK1115011A1 (en) 2008-11-14
NZ555376A (en) 2009-11-27
PL1819700T3 (pl) 2012-04-30
MA29120B1 (fr) 2007-12-03
US8357798B2 (en) 2013-01-22
EP1819700A2 (en) 2007-08-22
PE20061148A1 (es) 2006-11-09
CA2588398A1 (en) 2006-06-08
IL183614A (en) 2012-03-29
ZA200704130B (en) 2008-08-27
CA2588398C (en) 2011-07-12
ATE518844T1 (de) 2011-08-15
KR20070089990A (ko) 2007-09-04
WO2006060712A2 (en) 2006-06-08
JP2008521933A (ja) 2008-06-26
SI1819700T1 (sl) 2012-07-31
WO2006060730A2 (en) 2006-06-08
ATE534645T1 (de) 2011-12-15
WO2006060712A3 (en) 2006-09-21
CR9146A (es) 2007-10-04
WO2006060730A3 (en) 2006-08-17
US20100249410A1 (en) 2010-09-30
ES2370136T3 (es) 2011-12-13
AU2005311671B2 (en) 2011-01-27
NI200700138A (es) 2008-05-13
PT1819700E (pt) 2012-02-01
DK1819700T3 (da) 2012-03-19
EP1819683B1 (en) 2011-08-03
BRPI0518760A8 (pt) 2017-12-12
TWI344463B (en) 2011-07-01
IL183614A0 (en) 2007-09-20
EP1819700B1 (en) 2011-11-23
RS52197B (sr) 2012-10-31
ES2375788T3 (es) 2012-03-06
AU2005311671B8 (en) 2011-02-10
AU2005311671A1 (en) 2006-06-08
TW200631944A (en) 2006-09-16
HRP20120066T1 (hr) 2012-03-31
KR101350420B1 (ko) 2014-02-17
US7754731B2 (en) 2010-07-13
US20060122205A1 (en) 2006-06-08
EA200701204A1 (ru) 2007-12-28
AR052034A1 (es) 2007-02-28
CN101068793A (zh) 2007-11-07
BRPI0518760A2 (pt) 2008-12-09
MX2007006639A (es) 2007-06-19
MY144320A (en) 2011-08-29
NO20073404L (no) 2007-07-02
AR101429A2 (es) 2016-12-21
CY1112859T1 (el) 2016-04-13
JP4705956B2 (ja) 2011-06-22
EA012418B1 (ru) 2009-10-30
GEP20105086B (en) 2010-10-11
TNSN07215A1 (en) 2008-11-21
ME01985B (me) 2012-10-31
NO338784B1 (no) 2016-10-17
EP1819683A2 (en) 2007-08-22
WO2006060712A9 (en) 2006-07-27
UA87884C2 (uk) 2009-08-25

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