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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (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 (xx)
EP (1) EP1485358B1 (xx)
JP (1) JP4557552B2 (xx)
KR (3) KR20120136411A (xx)
CN (2) CN101935303B (xx)
AP (1) AP2111A (xx)
AR (1) AR038928A1 (xx)
AT (1) ATE497494T1 (xx)
AU (1) AU2003219159B2 (xx)
BR (1) BR0303373A (xx)
CA (1) CA2479012C (xx)
DE (1) DE60335939D1 (xx)
DK (1) DK1485358T3 (xx)
EA (1) EA011946B1 (xx)
HK (1) HK1072053A1 (xx)
HR (1) HRP20040936B1 (xx)
IL (1) IL163960A0 (xx)
MX (1) MXPA04008929A (xx)
MY (1) MY142238A (xx)
NO (1) NO326702B1 (xx)
NZ (1) NZ535439A (xx)
PL (1) PL213645B1 (xx)
SI (1) SI1485358T1 (xx)
TW (1) TWI329639B (xx)
WO (1) WO2003076413A1 (xx)
ZA (1) ZA200407242B (xx)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1860107B (zh) * 2003-09-30 2013-08-21 泰博特克药品有限公司 苯并*唑磺酰胺化合物的制备方法及其中间体
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
WO2006089942A1 (en) 2005-02-25 2006-08-31 Tibotec Pharmaceuticals Ltd. 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

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
WO1996028418A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Sulfonylalkanoylamino 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
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)

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Publication number Priority date Publication date Assignee Title
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
US5843946A (en) * 1992-08-25 1998-12-01 G.D. Searle & Co. α-and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
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
ES2127938T3 (es) 1993-08-24 1999-05-01 Searle & Co Hidroxietilamino sulfonamidas utiles como inhibidores de proteasas retroviricas.
PT721331E (pt) 1993-10-01 2002-05-31 Astrazeneca Ab Processo i
US5776971A (en) * 1995-03-10 1998-07-07 G.D. Searle & Co. Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
AU7722296A (en) 1995-11-15 1997-06-05 G.D. Searle & Co. Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
CA2240161C (en) 1996-05-20 2005-05-24 Janssen Pharmaceutica N.V. Antifungal compositions with improved bioavailability
ID21477A (id) 1997-03-26 1999-06-17 Janssen Pharmaceutica Nv Pelet-pelet yang mempunyai inti yang dilapisi dengan suatu anti jamur dan suatu polimer
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
WO1999033792A2 (en) 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
AU2012199A (en) 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
EP1042280A2 (en) 1997-12-24 2000-10-11 Vertex Pharmaceuticals Incorporated Prodrugs of 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
WO1996028418A1 (en) * 1995-03-10 1996-09-19 G.D. Searle & Co. Sulfonylalkanoylamino 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
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
PL374152A1 (en) 2005-10-03
AU2003219159A1 (en) 2003-09-22
ATE497494T1 (de) 2011-02-15
DK1485358T3 (da) 2011-05-09
NO326702B1 (no) 2009-02-02
WO2003076413A1 (en) 2003-09-18
AP2111A (en) 2010-03-03
NO20035023D0 (no) 2003-11-12
KR20120136411A (ko) 2012-12-18
JP2005519952A (ja) 2005-07-07
HK1072053A1 (en) 2005-08-12
EA200401188A1 (ru) 2005-04-28
IL163960A0 (en) 2005-12-18
BR0303373A (pt) 2004-03-23
AU2003219159B2 (en) 2009-09-03
KR20040093119A (ko) 2004-11-04
EP1485358A1 (en) 2004-12-15
CA2479012C (en) 2011-11-01
KR101302421B1 (ko) 2013-09-02
DE60335939D1 (de) 2011-03-17
CN1653053A (zh) 2005-08-10
EA011946B1 (ru) 2009-06-30
CN101935303A (zh) 2011-01-05
TW200400945A (en) 2004-01-16
US8143421B2 (en) 2012-03-27
MXPA04008929A (es) 2004-11-26
US20090203743A1 (en) 2009-08-13
AP2004003151A0 (en) 2004-12-31
SI1485358T1 (sl) 2011-05-31
CN101935303B (zh) 2014-03-12
AR038928A1 (es) 2005-02-02
US20050171175A1 (en) 2005-08-04
KR20100102742A (ko) 2010-09-24
PL213645B1 (pl) 2013-04-30
NZ535439A (en) 2009-09-25
JP4557552B2 (ja) 2010-10-06
MY142238A (en) 2010-11-15
TWI329639B (en) 2010-09-01
ZA200407242B (en) 2005-12-28
EP1485358B1 (en) 2011-02-02
HRP20040936A2 (en) 2005-10-31
CA2479012A1 (en) 2003-09-18

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