DK1485358T3 - Substitueret benzimidazol-sulfonamid som bred-sprektrum HIV-protease-inhibitorer - Google Patents

Substitueret benzimidazol-sulfonamid som bred-sprektrum HIV-protease-inhibitorer

Info

Publication number
DK1485358T3
DK1485358T3 DK03714954.9T DK03714954T DK1485358T3 DK 1485358 T3 DK1485358 T3 DK 1485358T3 DK 03714954 T DK03714954 T DK 03714954T DK 1485358 T3 DK1485358 T3 DK 1485358T3
Authority
DK
Denmark
Prior art keywords
broad
protease inhibitors
hiv protease
substituted benzimidazole
spectrum hiv
Prior art date
Application number
DK03714954.9T
Other languages
English (en)
Inventor
Bernhard Joanna Bernard Vergouwen
Dominique Louis Nestor Ghislain Surleraux
Piet Tom Bert Paul Wigerinck
Marieke Christiane Johanna Voets
Kock Herman Augustinus De
Sandrine Marie Helene Vendeville
Original Assignee
Tibotec Pharm Ltd
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
Application filed by Tibotec Pharm Ltd filed Critical Tibotec Pharm Ltd
Application granted granted Critical
Publication of DK1485358T3 publication Critical patent/DK1485358T3/da

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08Radicals containing only hydrogen and carbon atoms
    • 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
    • A61K31/4151,2-Diazoles
    • 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
    • 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
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/30Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/30Nitrogen atoms not forming part of a nitro radical
    • C07D235/32Benzimidazole-2-carbamic acids, unsubstituted or substituted; Esters thereof; Thio-analogues thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
DK03714954.9T 2002-03-12 2003-03-12 Substitueret benzimidazol-sulfonamid som bred-sprektrum HIV-protease-inhibitorer DK1485358T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02075999 2002-03-12
PCT/EP2003/050057 WO2003076413A1 (en) 2002-03-12 2003-03-12 Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors

Publications (1)

Publication Number Publication Date
DK1485358T3 true DK1485358T3 (da) 2011-05-09

Family

ID=27798870

Family Applications (1)

Application Number Title Priority Date Filing Date
DK03714954.9T DK1485358T3 (da) 2002-03-12 2003-03-12 Substitueret benzimidazol-sulfonamid som bred-sprektrum HIV-protease-inhibitorer

Country Status (25)

Country Link
US (2) US20050171175A1 (da)
EP (1) EP1485358B1 (da)
JP (1) JP4557552B2 (da)
KR (3) KR20040093119A (da)
CN (2) CN1653053A (da)
AP (1) AP2111A (da)
AR (1) AR038928A1 (da)
AT (1) ATE497494T1 (da)
AU (1) AU2003219159B2 (da)
BR (1) BR0303373A (da)
CA (1) CA2479012C (da)
DE (1) DE60335939D1 (da)
DK (1) DK1485358T3 (da)
EA (1) EA011946B1 (da)
HR (1) HRP20040936B1 (da)
IL (1) IL163960A0 (da)
MX (1) MXPA04008929A (da)
MY (1) MY142238A (da)
NO (1) NO326702B1 (da)
NZ (1) NZ535439A (da)
PL (1) PL213645B1 (da)
SI (1) SI1485358T1 (da)
TW (1) TWI329639B (da)
WO (1) WO2003076413A1 (da)
ZA (1) ZA200407242B (da)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL1670773T3 (pl) * 2003-09-30 2007-06-29 Tibotec Pharm Ltd Sposób wytwarzania sulfonamidów benzoksazolu i ich związków pośrednich
MXPA06012909A (es) * 2004-05-07 2007-09-06 Sequoia Pharmaceuticals Inc Inhibidores de proteasa retroviral repelente de resistencia.
AU2006217922B2 (en) 2005-02-25 2012-04-05 Janssen Sciences Ireland Uc Protease inhibitor precursor synthesis
UA103013C2 (uk) * 2007-12-06 2013-09-10 Тиботек Фармасьютикелз Амідні сполуки як активатори противірусних препаратів
WO2011061590A1 (en) 2009-11-17 2011-05-26 Hetero Research Foundation Novel carboxamide derivatives as hiv inhibitors
WO2013011485A1 (en) * 2011-07-20 2013-01-24 Ranbaxy Laboratories Limited Process for the preparation of sulfonamides useful as retroviral protease inhibitors

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
JP3657002B2 (ja) * 1992-08-25 2005-06-08 ジー.ディー.サール アンド カンパニー レトロウイルスプロテアーゼ阻害剤として有用なα−およびβ−アミノ酸ヒドロキシエチルアミノスルホンアミド
PH30929A (en) 1992-09-03 1997-12-23 Janssen Pharmaceutica Nv Beads having a core coated with an antifungal and a polymer.
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
AU7669794A (en) 1993-08-24 1995-03-21 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
SK283569B6 (sk) 1993-10-01 2003-09-11 Astra Aktiebolag Spôsob spracovania jemne deleného práškového liečiva, zariadenie na vykonávanie tohto spôsobu a aglomeráty vyrobené týmto spôsobom
WO1996022287A1 (en) * 1995-01-20 1996-07-25 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
US5756533A (en) * 1995-03-10 1998-05-26 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6140505A (en) * 1995-03-10 2000-10-31 G. D. Searle & Co. Synthesis of benzo fused heterocyclic sulfonyl chlorides
US5776971A (en) * 1995-03-10 1998-07-07 G.D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6150556A (en) * 1995-03-10 2000-11-21 G. D. Dearle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US5705500A (en) * 1995-03-10 1998-01-06 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
AU717598B2 (en) * 1995-03-10 2000-03-30 G.D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
JP2000515488A (ja) 1995-11-15 2000-11-21 ジー.ディー.サール アンド カンパニー 置換スルホニルアルカノイルアミノヒドロキシエチルアミノスルホンアミド レトロウイルスプロテアーゼ阻害剤
DK0904060T3 (da) 1996-05-20 2004-04-13 Janssen Pharmaceutica Nv Antifungale præparater med forbedret biotilgængelighed
WO1998042318A1 (en) 1997-03-26 1998-10-01 Janssen Pharmaceutica N.V. Pellets having a core coated with an antifungal and a polymer
CA2297070A1 (en) * 1997-08-01 1999-02-11 Morphosys Ag Novel method and phage for the identification of nucleic acid sequences encoding members of a multimeric (poly)peptide complex
WO1999033795A1 (en) 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
BR9814484A (pt) 1997-12-24 2000-10-10 Vertex Pharma "pró-drogas de inibidores de aspartil protease"
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
WO1999033792A2 (en) 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
NZ508855A (en) * 1998-06-19 2003-10-31 Vertex Pharma Sulfonamide inhibitors of HIV aspartyl protease
WO1999067254A2 (en) * 1998-06-23 1999-12-29 The United States Of America Represented By The Secretary, Department Of Health And Human Services Multi-drug resistant retroviral protease inhibitors and use thereof
AR031520A1 (es) * 1999-06-11 2003-09-24 Vertex Pharma Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion

Also Published As

Publication number Publication date
ATE497494T1 (de) 2011-02-15
PL374152A1 (en) 2005-10-03
KR20040093119A (ko) 2004-11-04
AU2003219159B2 (en) 2009-09-03
EP1485358A1 (en) 2004-12-15
NO326702B1 (no) 2009-02-02
AR038928A1 (es) 2005-02-02
US8143421B2 (en) 2012-03-27
TWI329639B (en) 2010-09-01
EP1485358B1 (en) 2011-02-02
KR20100102742A (ko) 2010-09-24
JP4557552B2 (ja) 2010-10-06
CA2479012A1 (en) 2003-09-18
TW200400945A (en) 2004-01-16
NO20035023D0 (no) 2003-11-12
HRP20040936A2 (en) 2005-10-31
KR101302421B1 (ko) 2013-09-02
BR0303373A (pt) 2004-03-23
SI1485358T1 (sl) 2011-05-31
AP2111A (en) 2010-03-03
IL163960A0 (en) 2005-12-18
US20090203743A1 (en) 2009-08-13
CN101935303A (zh) 2011-01-05
EA200401188A1 (ru) 2005-04-28
AU2003219159A1 (en) 2003-09-22
EA011946B1 (ru) 2009-06-30
DE60335939D1 (de) 2011-03-17
US20050171175A1 (en) 2005-08-04
NZ535439A (en) 2009-09-25
KR20120136411A (ko) 2012-12-18
PL213645B1 (pl) 2013-04-30
JP2005519952A (ja) 2005-07-07
AP2004003151A0 (en) 2004-12-31
WO2003076413A1 (en) 2003-09-18
ZA200407242B (en) 2005-12-28
HRP20040936B1 (hr) 2012-09-30
MY142238A (en) 2010-11-15
MXPA04008929A (es) 2004-11-26
CA2479012C (en) 2011-11-01
CN1653053A (zh) 2005-08-10
CN101935303B (zh) 2014-03-12
HK1072053A1 (en) 2005-08-12

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