HRP20040936B1 - Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors - Google Patents

Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors

Info

Publication number
HRP20040936B1
HRP20040936B1 HRP20040936AA HRP20040936A HRP20040936B1 HR P20040936 B1 HRP20040936 B1 HR P20040936B1 HR P20040936A A HRP20040936A A HR P20040936AA HR P20040936 A HRP20040936 A HR P20040936A HR P20040936 B1 HRP20040936 B1 HR P20040936B1
Authority
HR
Croatia
Prior art keywords
4alkyl
protease inhibitors
hiv protease
amino
substituted benzimidazole
Prior art date
Application number
HRP20040936AA
Other languages
English (en)
Croatian (hr)
Inventor
Louis Nestor Ghislai Surleraux Dominique
Tom Bert Paul Wigerinck Piet
Christiane Johanna Voets Marieke
Marie Helene Vendeville Sandrine
Augustinus De Kock Herman
Joanna Bernard Vergouwen Bernhard
Original Assignee
Tibotec Pharmaceuticals 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 Pharmaceuticals Ltd. filed Critical Tibotec Pharmaceuticals Ltd.
Publication of HRP20040936A2 publication Critical patent/HRP20040936A2/xx
Publication of HRP20040936B1 publication Critical patent/HRP20040936B1/xx

Links

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)
HRP20040936AA 2002-03-12 2004-10-07 Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors HRP20040936B1 (en)

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 (2)

Publication Number Publication Date
HRP20040936A2 HRP20040936A2 (en) 2005-10-31
HRP20040936B1 true HRP20040936B1 (en) 2012-09-30

Family

ID=27798870

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20040936AA HRP20040936B1 (en) 2002-03-12 2004-10-07 Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors

Country Status (26)

Country Link
US (2) US20050171175A1 (no)
EP (1) EP1485358B1 (no)
JP (1) JP4557552B2 (no)
KR (3) KR20120136411A (no)
CN (2) CN101935303B (no)
AP (1) AP2111A (no)
AR (1) AR038928A1 (no)
AT (1) ATE497494T1 (no)
AU (1) AU2003219159B2 (no)
BR (1) BR0303373A (no)
CA (1) CA2479012C (no)
DE (1) DE60335939D1 (no)
DK (1) DK1485358T3 (no)
EA (1) EA011946B1 (no)
HK (1) HK1072053A1 (no)
HR (1) HRP20040936B1 (no)
IL (1) IL163960A0 (no)
MX (1) MXPA04008929A (no)
MY (1) MY142238A (no)
NO (1) NO326702B1 (no)
NZ (1) NZ535439A (no)
PL (1) PL213645B1 (no)
SI (1) SI1485358T1 (no)
TW (1) TWI329639B (no)
WO (1) WO2003076413A1 (no)
ZA (1) ZA200407242B (no)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI1670773T1 (sl) * 2003-09-30 2007-06-30 Tibotec Pharm Ltd Postopki za pripravo benzoksazol sulfonamidnih spojin in njihovih intermediatov
JP5073480B2 (ja) * 2004-05-07 2012-11-14 セコイア、ファーマシューティカルズ、インコーポレイテッド 耐性防止レトロウイルスプロテアーゼ阻害薬
DE602006008751D1 (de) 2005-02-25 2009-10-08 Tibotec Pharm Ltd Synthese von proteaseinhibitorvorstufen
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

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996022287A1 (en) * 1995-01-20 1996-07-25 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
WO1996028464A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
WO1996028463A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
WO1996028465A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
WO1996028418A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
WO1999059989A1 (en) * 1998-05-19 1999-11-25 G.D. Searle & Co. Process for the preparation of a benzo fused heterocyclo sulfonyl halide intermediate
WO1999065870A2 (en) * 1998-06-19 1999-12-23 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of 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
WO2000076961A1 (en) * 1999-06-11 2000-12-21 Vertex Pharmaceuticals Incorporated Inhibitors of aspartyl protease

Family Cites Families (15)

* 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
ATE218541T1 (de) * 1992-08-25 2002-06-15 Searle & Co Hydroxyethylaminosulfonamide verwendbar als inhibitoren retroviraler proteasen
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
DK0715618T3 (da) 1993-08-24 1999-08-23 Searle & Co Hydroxyethylaminosulfonamider til anvendelse som inhibitorer af retrovirale proteaser
CN1110300C (zh) 1993-10-01 2003-06-04 阿斯特拉公司 工艺技术ⅰ
US5776971A (en) * 1995-03-10 1998-07-07 G.D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US5753660A (en) 1995-11-15 1998-05-19 G. D. Searle & Co. Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
KR19990044257A (ko) 1996-05-20 1999-06-25 디르크 반테 생체이용율이 개선된 항진균성 조성물
SI0969821T1 (en) 1997-03-26 2003-10-31 Janssen Pharmaceutica N.V. Pellets having a core coated with an antifungal and a polymer
EP1005569A2 (en) * 1997-08-01 2000-06-07 MorphoSys AG Novel method and phage for the identification of nucleic acid sequences encoding members of a multimeric (poly)peptide complex
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
CA2316218A1 (en) 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
AU2012199A (en) 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
WO1999033792A2 (en) 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996022287A1 (en) * 1995-01-20 1996-07-25 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
WO1996028464A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
WO1996028463A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
WO1996028465A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
WO1996028418A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
WO1999059989A1 (en) * 1998-05-19 1999-11-25 G.D. Searle & Co. Process for the preparation of a benzo fused heterocyclo sulfonyl halide intermediate
WO1999065870A2 (en) * 1998-06-19 1999-12-23 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of 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
WO2000076961A1 (en) * 1999-06-11 2000-12-21 Vertex Pharmaceuticals Incorporated Inhibitors of aspartyl protease

Also Published As

Publication number Publication date
NO326702B1 (no) 2009-02-02
NZ535439A (en) 2009-09-25
KR101302421B1 (ko) 2013-09-02
PL374152A1 (en) 2005-10-03
DK1485358T3 (da) 2011-05-09
CN101935303A (zh) 2011-01-05
KR20100102742A (ko) 2010-09-24
KR20040093119A (ko) 2004-11-04
HRP20040936A2 (en) 2005-10-31
AR038928A1 (es) 2005-02-02
ZA200407242B (en) 2005-12-28
CA2479012A1 (en) 2003-09-18
KR20120136411A (ko) 2012-12-18
PL213645B1 (pl) 2013-04-30
IL163960A0 (en) 2005-12-18
EA011946B1 (ru) 2009-06-30
NO20035023D0 (no) 2003-11-12
SI1485358T1 (sl) 2011-05-31
MY142238A (en) 2010-11-15
CA2479012C (en) 2011-11-01
US20090203743A1 (en) 2009-08-13
TW200400945A (en) 2004-01-16
DE60335939D1 (de) 2011-03-17
US8143421B2 (en) 2012-03-27
BR0303373A (pt) 2004-03-23
AU2003219159A1 (en) 2003-09-22
CN1653053A (zh) 2005-08-10
MXPA04008929A (es) 2004-11-26
EP1485358B1 (en) 2011-02-02
AP2004003151A0 (en) 2004-12-31
HK1072053A1 (en) 2005-08-12
JP4557552B2 (ja) 2010-10-06
JP2005519952A (ja) 2005-07-07
AU2003219159B2 (en) 2009-09-03
TWI329639B (en) 2010-09-01
WO2003076413A1 (en) 2003-09-18
CN101935303B (zh) 2014-03-12
AP2111A (en) 2010-03-03
EA200401188A1 (ru) 2005-04-28
US20050171175A1 (en) 2005-08-04
EP1485358A1 (en) 2004-12-15
ATE497494T1 (de) 2011-02-15

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