AR033360A1 - CRYSTAL FORMS OF (2S, 3S, 5S) -2- (2,6-DIMETHYLPHENOXIACETILE) AMIN-3-HIDROXI-5- (2- (1-TETRAHYDROPIRIMID-2-ONIL) -3-METHYLBUTANOIL) AMIN-1,6 -DIFENILHEXANO (LOPINAVIR) - Google Patents

CRYSTAL FORMS OF (2S, 3S, 5S) -2- (2,6-DIMETHYLPHENOXIACETILE) AMIN-3-HIDROXI-5- (2- (1-TETRAHYDROPIRIMID-2-ONIL) -3-METHYLBUTANOIL) AMIN-1,6 -DIFENILHEXANO (LOPINAVIR)

Info

Publication number
AR033360A1
AR033360A1 ARP010101522A ARP010101522A AR033360A1 AR 033360 A1 AR033360 A1 AR 033360A1 AR P010101522 A ARP010101522 A AR P010101522A AR P010101522 A ARP010101522 A AR P010101522A AR 033360 A1 AR033360 A1 AR 033360A1
Authority
AR
Argentina
Prior art keywords
amin
lopinavir
tetrahydropirimid
methylbutanoil
dimethylphenoxiacetile
Prior art date
Application number
ARP010101522A
Other languages
Spanish (es)
Inventor
Rodger F Henry
David Lechuga-Ballesteros
Yuping Niu
William Porter
Daniel A Dickman
S Chemburkar
James J Fort
Original Assignee
Abbott Lab
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27065762&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR033360(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US09/793,536 external-priority patent/US6608198B2/en
Application filed by Abbott Lab filed Critical Abbott Lab
Publication of AR033360A1 publication Critical patent/AR033360A1/en

Links

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
    • C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
    • C07D239/10—Oxygen or sulfur atoms
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Formas cristalinas del compuesto (2S, 3S, 5S)-2-(2,6-dimetilfenoxiacetil) amin-3-hidroxi-5-(2-(1-tetrahidropirimid-2-onil)-3-metilbutanoíl)amin-1,6-difenoxihexano(lopinavir). Se describen las formas cristalinas hidratadas solvatadas, las formas cristalinas y las formas cristalinas no solvatadas de lopinavir así como las formas sustancialmente puras de todas las formas anteriormente mencionadas. El lopinavir es de utilidad en la inhibicion de la proteasa del VIH y la inhibicion de una infeccion por VIH.Crystalline forms of the compound (2S, 3S, 5S) -2- (2,6-dimethylphenoxyacetyl) amin-3-hydroxy-5- (2- (1-tetrahydropyrimid-2-onyl) -3-methylbutanoyl) amin-1, 6-diphenoxyhexane (lopinavir). Solvated hydrated crystalline forms, crystalline forms and non-solvated crystalline forms of lopinavir are described as well as substantially pure forms of all the aforementioned forms. Lopinavir is useful in inhibiting HIV protease and inhibiting HIV infection.

ARP010101522A 2000-03-30 2001-03-29 CRYSTAL FORMS OF (2S, 3S, 5S) -2- (2,6-DIMETHYLPHENOXIACETILE) AMIN-3-HIDROXI-5- (2- (1-TETRAHYDROPIRIMID-2-ONIL) -3-METHYLBUTANOIL) AMIN-1,6 -DIFENILHEXANO (LOPINAVIR) AR033360A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US53825700A 2000-03-30 2000-03-30
US09/793,536 US6608198B2 (en) 2000-03-30 2001-02-27 Crystalline pharmaceutical

Publications (1)

Publication Number Publication Date
AR033360A1 true AR033360A1 (en) 2003-12-17

Family

ID=27065762

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP010101522A AR033360A1 (en) 2000-03-30 2001-03-29 CRYSTAL FORMS OF (2S, 3S, 5S) -2- (2,6-DIMETHYLPHENOXIACETILE) AMIN-3-HIDROXI-5- (2- (1-TETRAHYDROPIRIMID-2-ONIL) -3-METHYLBUTANOIL) AMIN-1,6 -DIFENILHEXANO (LOPINAVIR)
ARP050102702A AR049560A2 (en) 2000-03-30 2005-06-29 CRYSTAL FORMS OF (2S, 3S, 5S) -2- (2,6-DIMETHYLPHENOXIACETILE) AMIN 3-HYDROXY-5- (2- (1-TETRAHYDROPIRIMID-2-ONIL) -3-METHYLBUTANOL) AMIN-1,6- DIFENILHEXANO (LOPINAVIR)

Family Applications After (1)

Application Number Title Priority Date Filing Date
ARP050102702A AR049560A2 (en) 2000-03-30 2005-06-29 CRYSTAL FORMS OF (2S, 3S, 5S) -2- (2,6-DIMETHYLPHENOXIACETILE) AMIN 3-HYDROXY-5- (2- (1-TETRAHYDROPIRIMID-2-ONIL) -3-METHYLBUTANOL) AMIN-1,6- DIFENILHEXANO (LOPINAVIR)

Country Status (22)

Country Link
EP (1) EP1268442A2 (en)
JP (1) JP2003529592A (en)
KR (1) KR100773258B1 (en)
CN (2) CN1330639C (en)
AR (2) AR033360A1 (en)
AU (3) AU2001250920B2 (en)
BG (1) BG107165A (en)
BR (1) BR0109433A (en)
CA (1) CA2403635A1 (en)
CZ (1) CZ20023529A3 (en)
HU (1) HUP0302675A3 (en)
IL (1) IL151551A0 (en)
MX (1) MXPA02009559A (en)
MY (1) MY128296A (en)
NO (1) NO325005B1 (en)
NZ (1) NZ521183A (en)
PE (1) PE20011232A1 (en)
PL (1) PL359727A1 (en)
SA (2) SA06270303B1 (en)
SK (1) SK14832002A3 (en)
TW (1) TWI284640B (en)
WO (1) WO2001074787A2 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6608198B2 (en) 2000-03-30 2003-08-19 Abbott Laboratories Crystalline pharmaceutical
US8025899B2 (en) 2003-08-28 2011-09-27 Abbott Laboratories Solid pharmaceutical dosage form
WO2010089753A2 (en) * 2009-02-06 2010-08-12 Hetero Research Foundation Novel polymorphs of lopinavir
WO2011025849A1 (en) * 2009-08-27 2011-03-03 Merck Sharp & Dohme Corp. Processes for preparing protease inhibitors of hepatitis c virus
CN112830899A (en) * 2021-01-18 2021-05-25 合肥华方医药科技有限公司 Novel lopinavir crystal form and preparation method thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5914332A (en) * 1995-12-13 1999-06-22 Abbott Laboratories Retroviral protease inhibiting compounds
WO1998057648A1 (en) * 1997-06-16 1998-12-23 Vertex Pharmaceuticals Incorporated Methods of increasing the bioavailability of stable crystal polymorphs of a compound

Also Published As

Publication number Publication date
JP2003529592A (en) 2003-10-07
SA06270303B1 (en) 2009-08-02
TWI284640B (en) 2007-08-01
HUP0302675A2 (en) 2003-12-29
KR100773258B1 (en) 2007-11-05
KR20030011807A (en) 2003-02-11
WO2001074787A2 (en) 2001-10-11
NO20024679D0 (en) 2002-09-30
AU5092001A (en) 2001-10-15
NZ521183A (en) 2004-03-26
AU2001250920B2 (en) 2006-06-29
CN101066952A (en) 2007-11-07
PL359727A1 (en) 2004-09-06
WO2001074787A3 (en) 2002-02-07
NO325005B1 (en) 2008-01-14
AU2006222711A1 (en) 2006-10-19
BR0109433A (en) 2004-08-10
AR049560A2 (en) 2006-08-16
SK14832002A3 (en) 2003-02-04
PE20011232A1 (en) 2001-12-08
MY128296A (en) 2007-01-31
CN1330639C (en) 2007-08-08
HUP0302675A3 (en) 2004-03-29
CA2403635A1 (en) 2001-10-11
IL151551A0 (en) 2003-04-10
EP1268442A2 (en) 2003-01-02
MXPA02009559A (en) 2003-05-21
SA01220270B1 (en) 2006-11-14
NO20024679L (en) 2002-09-30
CN1422259A (en) 2003-06-04
BG107165A (en) 2003-07-31
CZ20023529A3 (en) 2003-02-12

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