CA2588398C - Potassium salt of an hiv integrase inhibitor - Google Patents

Potassium salt of an hiv integrase inhibitor Download PDF

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Publication number
CA2588398C
CA2588398C CA2588398A CA2588398A CA2588398C CA 2588398 C CA2588398 C CA 2588398C CA 2588398 A CA2588398 A CA 2588398A CA 2588398 A CA2588398 A CA 2588398A CA 2588398 C CA2588398 C CA 2588398C
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CA
Canada
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 - Lifetime
Application number
CA2588398A
Other languages
English (en)
French (fr)
Other versions
CA2588398A1 (en
Inventor
Kevin M. Belyk
Henry G. Morrison
Amar J. Mahajan
Daniel J. Kumke
Hsien-Hsin Tung
Lawrence Wai
Vanessa Pruzinsky
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 UK Ltd
MSD Italia SRL
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme Ltd
Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
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.)
Filing date
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=CA2588398(C) "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 Ltd, Istituto di Ricerche di Biologia Molecolare P Angeletti SpA, Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme Ltd
Publication of CA2588398A1 publication Critical patent/CA2588398A1/en
Application granted granted Critical
Publication of CA2588398C publication Critical patent/CA2588398C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • 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
    • 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
    • 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)
CA2588398A 2004-12-03 2005-12-02 Potassium salt of an hiv integrase inhibitor Expired - Lifetime CA2588398C (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 (2)

Publication Number Publication Date
CA2588398A1 CA2588398A1 (en) 2006-06-08
CA2588398C true CA2588398C (en) 2011-07-12

Family

ID=36171569

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2588398A Expired - Lifetime CA2588398C (en) 2004-12-03 2005-12-02 Potassium salt of an hiv integrase inhibitor

Country Status (35)

Country Link
US (2) US7754731B2 (OSRAM)
EP (2) EP1819683B1 (OSRAM)
JP (1) JP4705956B2 (OSRAM)
KR (2) KR101350420B1 (OSRAM)
CN (1) CN101068793B (OSRAM)
AR (2) AR052034A1 (OSRAM)
AT (2) ATE534645T1 (OSRAM)
AU (1) AU2005311671B8 (OSRAM)
BR (1) BRPI0518760A8 (OSRAM)
CA (1) CA2588398C (OSRAM)
CR (1) CR9146A (OSRAM)
CY (1) CY1112859T1 (OSRAM)
DK (1) DK1819700T3 (OSRAM)
EA (1) EA012418B1 (OSRAM)
ES (2) ES2375788T3 (OSRAM)
GE (1) GEP20105086B (OSRAM)
HR (1) HRP20120066T1 (OSRAM)
IL (1) IL183614A (OSRAM)
MA (1) MA29120B1 (OSRAM)
ME (1) ME01985B (OSRAM)
MX (1) MX2007006639A (OSRAM)
MY (1) MY144320A (OSRAM)
NI (1) NI200700138A (OSRAM)
NO (1) NO338784B1 (OSRAM)
NZ (1) NZ555376A (OSRAM)
PE (1) PE20061148A1 (OSRAM)
PL (1) PL1819700T3 (OSRAM)
PT (1) PT1819700E (OSRAM)
RS (1) RS52197B (OSRAM)
SI (1) SI1819700T1 (OSRAM)
TN (1) TNSN07215A1 (OSRAM)
TW (1) TWI344463B (OSRAM)
UA (1) UA87884C2 (OSRAM)
WO (2) WO2006060712A2 (OSRAM)
ZA (1) ZA200704130B (OSRAM)

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US20070259894A1 (en) * 2004-12-03 2007-11-08 Kelem Kassahun Use of Atazanavir for Improving the Pharmacokinetics of Drugs Metabolized by Ugt1a1
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
AU2007275805A1 (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
CN103254138A (zh) * 2008-01-08 2013-08-21 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
WO2011024192A2 (en) 2009-07-27 2011-03-03 Matrix Laboratories Ltd Novel polymorphs of raltegravir
HUE057248T2 (hu) * 2009-10-26 2022-04-28 Merck Sharp & Dohme Integráz inhibitort tartalmazó szilárd gyógyszerészeti kompozíciók
DE102009056636A1 (de) 2009-12-02 2011-06-09 Ratiopharm Gmbh Raltegravir-Polymorphe
EA201270651A1 (ru) * 2009-12-07 2013-01-30 Юниверсити Оф Джорджия Рисерч Фаундейшн, Инк. Карбоксамиды пиридинон гидроксициклопентила: ингибиторы вич интегразы и области терапевтического применения
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.
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EP2575465A4 (en) * 2010-05-25 2013-11-20 Hetero Research Foundation Raltegravir SALTS
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
AU2012241050B2 (en) 2011-04-06 2016-05-19 Lupin Limited Novel salts of raltegravir
EP2699094A4 (en) * 2011-04-22 2014-12-17 Merck Sharp & Dohme TASTE-MASKED FORMULATIONS BY 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
EP2529741B1 (en) 2011-06-01 2014-02-12 Ratiopharm GmbH Composition and Tablet Comprising 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
WO2013098854A2 (en) * 2011-12-26 2013-07-04 Emcure Pharmaceuticals Limited Synthesis of raltegravir
JP2015504913A (ja) 2012-01-25 2015-02-16 ルピン・リミテッドＬｕｐｉｎ Ｌｉｍｉｔｅｄ 安定な非晶質のラルテグラビルカリウムプレミックス、及び、その調製方法
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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
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
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US10752618B2 (en) 2016-09-15 2020-08-25 Lupin Limited Process for the preparation of pure and stable crystalline Raltegravir potassium form 3
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US20070259894A1 (en) 2004-12-03 2007-11-08 Kelem Kassahun Use of Atazanavir for Improving the Pharmacokinetics of Drugs Metabolized by Ugt1a1

Also Published As

Publication number Publication date
BRPI0518760A8 (pt) 2017-12-12
ATE518844T1 (de) 2011-08-15
HRP20120066T1 (hr) 2012-03-31
MY144320A (en) 2011-08-29
CN101068793A (zh) 2007-11-07
NO20073404L (no) 2007-07-02
EA200701204A1 (ru) 2007-12-28
NO338784B1 (no) 2016-10-17
HK1115011A1 (en) 2008-11-14
IL183614A (en) 2012-03-29
KR20130122031A (ko) 2013-11-06
PL1819700T3 (pl) 2012-04-30
EP1819700B1 (en) 2011-11-23
MX2007006639A (es) 2007-06-19
GEP20105086B (en) 2010-10-11
TNSN07215A1 (en) 2008-11-21
JP2008521933A (ja) 2008-06-26
CN101068793B (zh) 2011-05-25
WO2006060712A3 (en) 2006-09-21
KR20070089990A (ko) 2007-09-04
TWI344463B (en) 2011-07-01
ZA200704130B (en) 2008-08-27
AR052034A1 (es) 2007-02-28
TW200631944A (en) 2006-09-16
PE20061148A1 (es) 2006-11-09
JP4705956B2 (ja) 2011-06-22
CA2588398A1 (en) 2006-06-08
RS52197B (sr) 2012-10-31
US20060122205A1 (en) 2006-06-08
ES2370136T3 (es) 2011-12-13
MA29120B1 (fr) 2007-12-03
IL183614A0 (en) 2007-09-20
UA87884C2 (uk) 2009-08-25
US8357798B2 (en) 2013-01-22
NI200700138A (es) 2008-05-13
PT1819700E (pt) 2012-02-01
AR101429A2 (es) 2016-12-21
AU2005311671B2 (en) 2011-01-27
WO2006060730A2 (en) 2006-06-08
ES2375788T3 (es) 2012-03-06
DK1819700T3 (da) 2012-03-19
EP1819683B1 (en) 2011-08-03
CR9146A (es) 2007-10-04
EP1819683A2 (en) 2007-08-22
NZ555376A (en) 2009-11-27
SI1819700T1 (sl) 2012-07-31
AU2005311671B8 (en) 2011-02-10
AU2005311671A1 (en) 2006-06-08
WO2006060730A3 (en) 2006-08-17
EA012418B1 (ru) 2009-10-30
BRPI0518760A2 (pt) 2008-12-09
US20100249410A1 (en) 2010-09-30
US7754731B2 (en) 2010-07-13
WO2006060712A9 (en) 2006-07-27
WO2006060712A2 (en) 2006-06-08
ME01985B (me) 2012-10-31
KR101350420B1 (ko) 2014-02-17
EP1819700A2 (en) 2007-08-22
ATE534645T1 (de) 2011-12-15
CY1112859T1 (el) 2016-04-13

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