BR0303373A - Inibidores de hiv protease de sulfonamidas benzimidazol- substituìdas de espectro amplo - Google Patents

Inibidores de hiv protease de sulfonamidas benzimidazol- substituìdas de espectro amplo

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Publication number
BR0303373A
BR0303373A BR0303373-2A BR0303373A BR0303373A BR 0303373 A BR0303373 A BR 0303373A BR 0303373 A BR0303373 A BR 0303373A BR 0303373 A BR0303373 A BR 0303373A
Authority
BR
Brazil
Prior art keywords
alkyl
het
alkanediyl
amino
optionally substituted
Prior art date
Application number
BR0303373-2A
Other languages
English (en)
Inventor
Dominique Louis Nest Surleraux
Piet Tom Bert Paul Wigerinck
Marieke Christiane Johan Voets
Sandrine Marie Hele Vendeville
Herman Augustinus De Kock
Bernhard Joanna Bern Vergouwen
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
Publication of BR0303373A publication Critical patent/BR0303373A/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • 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
    • A61K31/415—1,2-Diazoles
    • 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
    • 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
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; 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
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; 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
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C07D235/32—Benzimidazole-2-carbamic acids, unsubstituted or substituted; Esters thereof; Thio-analogues thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems

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  • 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)

Abstract

"INIBIDORES DE HIV PROTEASE DE SULFONAMIDAS BENZIMIDAZOL-SUBSTITUìDAS DE ESPECTRO AMPLO". A presente invenção refere-se aos compostos tendo a fórmula (I), em que N-óxidos, sais, formas estereoisoméricas, misturas racêmicas, pró-drogas, ésteres e metabólitos destes, em que R~ 1~ e R~ 8~ cada um é H, C~ 1-6~alquila opcionalmente substituída, C~ 2-6~alquenila, C~ 3-7~cicloalquila, arila, Het^ 1^, Het^ 2^; R~ 1~ também pode ser um radical da fórmula (R~ 11a~R~ 11b~)NC(R~ 10a~R~ 10b~)CR~ 9~-; t é 0, 1 ou 2; R~ 2~ é H OU C~ 1-6~alquila; L é -C(=O)-, -O-C(=O)-, -NR~ 8~-C(=O)-, -O-C~ 1-6~alcanodiil-C(=O)-, -NR~ 8~-C~ 1-6~alcanodiil-C(=O)-, -S(=O)~ 2~-, -O-S(=0)~ 2~-, -NR~ 8~-S(=O)~ 2~; R~ 3~ é C~ 1-6~alquila, arila, C~ 3-7~cicloalquila, C~ 3-7~cicloalquilC~ 1-4~alquila ou arilC~ 1-4~alquila; R~ 4~ é H, C~ 1-4~alquilOC(=O), carboxila, aminoC(=O), mono ou di(C~ 1-4~alquil)aminoC(=O), C~ 3-7~cicloalquila, C~ 2-6~alquenila, C~ 2-6~alquinila ou C~ 1-6~ alquila opcionalmente substituída; A é C~ 1-6~alcanodiila, -C(=O)-, -C(=S)-, -S(=O)~ 2~-, C~ 1-6~alcanodiil-C(=O)-, C~ 1-6~alcanodiil-C(=S)- ou C~ 1-6~alcanodiil-S(=O)~ 2~-; R~ 5~ é H, OH, C~ 1-6~alquila, Het^ 1^C~ 1-6~alquila, Het^ 2^C~ 1-6~alquila, amino-C~ 1-6~ alquila opcionalmente substituída; R~ 6~ é C~ 1-6~alquilO, Het^ 1^, Het^ 1^O, Het^ 2^, Het^ 2^O, arila, arilO, C~ 1-6~alquiloxicarbonilamino ou amino; e no caso de -A- ser diferente de C~ 1-6~alcanodiila, então R~ 6~ também pode ser C~ 1-6~alquila, Het^ 1^C~ 1-4~ alquila, Het^ 1^OC~ 1-4~alquila, Het~ 2~C~ 1-4~alquila, Het^ 2^OC~ 1-4~alquila, arilC~ 1-4~alquila, arilOC~ 1-4~ alquila ou aminoC~ 1-4~alquila; onde cada um dos grupos amino na definição de R~ 6~ pode ser opcionalmente substituído; R~ 5~ e -A-R~ 6~ considerados juntos com o átomo de nitrogênio ao qual eles estão ligados podem também formar Het^ 1^ ou Het^ 2^; R^ 12^ é H, -NH~ 2~, -NR~ 5~AR~ 6~, -C~ 1-6~alquila ou alquil-W-R~ 14~, em que a dita alquila é opcionalmente substituída por halogênio, hidróxi, arila, heteroarila, Het^ 1^, Het^ 2^, ou amino em que o dito amino é opcionalmente mono ou dissubstituído por C~ 1-4~alquila e R~ 13~ é H, C~ 1-6~-alquila opcionalmente substituída por arila, Het^ 1^, Het^ 2^, hidróxi, halogênio, amino onde o grupo amino pode ser opcionalmente mono ou dissubstituído por C~ 1-4~alquila.
BR0303373-2A 2002-03-12 2003-03-12 Inibidores de hiv protease de sulfonamidas benzimidazol- substituìdas de espectro amplo BR0303373A (pt)

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
BR0303373A true BR0303373A (pt) 2004-03-23

Family

ID=27798870

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0303373-2A BR0303373A (pt) 2002-03-12 2003-03-12 Inibidores de hiv protease de sulfonamidas benzimidazol- substituìdas de espectro amplo

Country Status (26)

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

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE602004004674T2 (de) * 2003-09-30 2007-11-22 Tibotec Pharmaceuticals Ltd. Verfahren zur herstellung von benzoxazolsulfonamidverbindungen und zwischenprodukten davon
EP2422780A1 (en) * 2004-05-07 2012-02-29 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
CA2595295C (en) 2005-02-25 2014-07-08 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

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Also Published As

Publication number Publication date
DK1485358T3 (da) 2011-05-09
NO326702B1 (no) 2009-02-02
AU2003219159B2 (en) 2009-09-03
US20090203743A1 (en) 2009-08-13
DE60335939D1 (de) 2011-03-17
JP2005519952A (ja) 2005-07-07
IL163960A0 (en) 2005-12-18
KR101302421B1 (ko) 2013-09-02
SI1485358T1 (sl) 2011-05-31
NZ535439A (en) 2009-09-25
WO2003076413A1 (en) 2003-09-18
PL213645B1 (pl) 2013-04-30
HK1072053A1 (en) 2005-08-12
EA200401188A1 (ru) 2005-04-28
ZA200407242B (en) 2005-12-28
TW200400945A (en) 2004-01-16
ATE497494T1 (de) 2011-02-15
AP2111A (en) 2010-03-03
CN101935303B (zh) 2014-03-12
HRP20040936A2 (en) 2005-10-31
MY142238A (en) 2010-11-15
US20050171175A1 (en) 2005-08-04
AR038928A1 (es) 2005-02-02
KR20100102742A (ko) 2010-09-24
AU2003219159A1 (en) 2003-09-22
HRP20040936B1 (en) 2012-09-30
KR20120136411A (ko) 2012-12-18
EP1485358A1 (en) 2004-12-15
AP2004003151A0 (en) 2004-12-31
TWI329639B (en) 2010-09-01
US8143421B2 (en) 2012-03-27
CN1653053A (zh) 2005-08-10
CA2479012C (en) 2011-11-01
EP1485358B1 (en) 2011-02-02
EA011946B1 (ru) 2009-06-30
NO20035023D0 (no) 2003-11-12
CN101935303A (zh) 2011-01-05
JP4557552B2 (ja) 2010-10-06
CA2479012A1 (en) 2003-09-18
PL374152A1 (en) 2005-10-03
MXPA04008929A (es) 2004-11-26
KR20040093119A (ko) 2004-11-04

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