AU2005311671B8 - Potassium salt of an HIV integrase inhibitor - Google Patents

Potassium salt of an HIV integrase inhibitor Download PDF

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Publication number
AU2005311671B8
AU2005311671B8 AU2005311671A AU2005311671A AU2005311671B8 AU 2005311671 B8 AU2005311671 B8 AU 2005311671B8 AU 2005311671 A AU2005311671 A AU 2005311671A AU 2005311671 A AU2005311671 A AU 2005311671A AU 2005311671 B8 AU2005311671 B8 AU 2005311671B8
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AU
Australia
Prior art keywords
compound
solution
amount
range
solvent
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.)
Expired
Application number
AU2005311671A
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English (en)
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AU2005311671A1 (en
AU2005311671B2 (en
Inventor
Kevin M. Belyk
Daniel J. Kumke
Amar J. Mahajan
Henry G. Morrison
Vanessa Pruzinsky
Hsien-Hsin Tung
Lawrence Wai
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
Priority date (The priority date 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 date listed.)
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36171569&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU2005311671(B8) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Publication of AU2005311671A1 publication Critical patent/AU2005311671A1/en
Assigned to MERCK SHARP & DOHME LIMITED, ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A., MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME LIMITED Alteration of Name(s) of Applicant(s) under S113 Assignors: ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A., MERCK & CO., INC., MERCK SHARP & DOHME LIMITED
Publication of AU2005311671B2 publication Critical patent/AU2005311671B2/en
Application granted granted Critical
Publication of AU2005311671B8 publication Critical patent/AU2005311671B8/en
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK SHARP & DOHME CORP.
Assigned to MERCK SHARP & DOHME LLC reassignment MERCK SHARP & DOHME LLC Request to Amend Deed and Register Assignors: MERCK SHARP & DOHME CORP.
Anticipated expiration legal-status Critical
Expired legal-status Critical Current

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Classifications

    • 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)
  • 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)
AU2005311671A 2004-12-03 2005-12-02 Potassium salt of an HIV integrase inhibitor Expired AU2005311671B8 (en)

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
AU2005311671A1 AU2005311671A1 (en) 2006-06-08
AU2005311671B2 AU2005311671B2 (en) 2011-01-27
AU2005311671B8 true AU2005311671B8 (en) 2011-02-10

Family

ID=36171569

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2005311671A Expired AU2005311671B8 (en) 2004-12-03 2005-12-02 Potassium salt of an HIV integrase inhibitor

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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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
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WO2012009446A1 (en) 2010-07-16 2012-01-19 Concert Pharmaceuticals Inc. Novel 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
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WO2012106534A2 (en) * 2011-02-02 2012-08-09 The Regents Of The University Of California Hiv integrase inhibitors
WO2012137142A1 (en) 2011-04-06 2012-10-11 Lupin Limited Novel salts of raltegravir
CA2833006A1 (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
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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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
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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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WO2016075605A1 (en) 2014-11-10 2016-05-19 Aurobindo Pharma Ltd An improved process for the preparation of raltegravir
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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
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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
JP4705956B2 (ja) 2011-06-22

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Free format text: IN VOL 25, NO 4, PAGE(S) 457 UNDER THE HEADING APPLICATIONS ACCEPTED - NAME INDEX UNDER THE NAME MERCK SHARP & DOHME CORP., APPLICATION NO. 2005311671, UNDER INID (72) REMOVE CO-INVENTOR JONES, PHILIP

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Owner name: MERCK SHARP & DOHME LLC

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