BR0215260A - Inibidores de hiv protease de sulfonamida contendo fenila substituìda heterocìclica de amplo espectro - Google Patents

Inibidores de hiv protease de sulfonamida contendo fenila substituìda heterocìclica de amplo espectro

Info

Publication number
BR0215260A
BR0215260A BR0215260-6A BR0215260A BR0215260A BR 0215260 A BR0215260 A BR 0215260A BR 0215260 A BR0215260 A BR 0215260A BR 0215260 A BR0215260 A BR 0215260A
Authority
BR
Brazil
Prior art keywords
protease inhibitors
broad spectrum
hiv protease
het
hydroxy
Prior art date
Application number
BR0215260-6A
Other languages
English (en)
Inventor
Sandrine Marie Hele Vendeville
Wim Gaston Verschueren
Abdellah Tahri
Samuel Leo Christiaan Moors
Montserrat Erra Sola
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 BR0215260A publication Critical patent/BR0215260A/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
    • C07D233/88—Nitrogen atoms, e.g. allantoin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/40—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D417/14—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 three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18—Fluorenes; Hydrogenated fluorenes

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

"INIBIDORES DE HIV PROTEASE DE SULFONAMIDA CONTENDO FENILA SUBSTITUìDA HETEROCìCLICA DE AMPLO ESPECTRO". A presente invenção refere-se a compostos tendo a fórmula (I), N-óxidos, sais, formas estereoisoméricas, misturas racêmicas, pró-drogas, ésteres e seus metabólitos, em que Harila é heterociclo monocíclico, bicíclico ou tricíclico aromático tendo de 3 a 14 membros de anel que contém um ou mais membros de anel heteroátomo selecionados de nitrogênio, oxigênio e enxofre e que podem opcionalmente estar substituídos sobre (i) um ou mais átomos de carbono por C~ 1-6~ alquila, halogênio, hidróxi, amino opcionalmente mono-ou dissubstituído, nitro, ciano, haloC~ 1-6~,-6 alquila, carboxila, C~ 3-7~ cicloalquila, aminocarbonila opcionalmente mono-ou dissubstituída, metiltio, metilsulfonila, arila, -(R~ 7 a~)n-M-~ 7b~, Het^ 1^ e Het^ 2^; pelo que os substituintes opcionais sobre qualquer função de amino são independentemente selecionados de R~ 5~ e -A-R~ 6~; e sobre (II) um átomo de nitrogênio se presente por hidróxi ou -A-R~ 6~. Este ulteriormente refere-se ao seu uso como inibidores de protease HIV de amplo espectro, a processos para a sua preparação bem como a composições farmacêuticas e a kits compreendendo as mesmas. Ela também refere-se a suas combinações com um outro agente anti-retroviral, e ao seu uso em ensaios como compostos de referência ou como reagentes.
BR0215260-6A 2001-12-21 2002-12-20 Inibidores de hiv protease de sulfonamida contendo fenila substituìda heterocìclica de amplo espectro BR0215260A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01205115 2001-12-21
PCT/EP2002/014839 WO2003053435A1 (en) 2001-12-21 2002-12-20 Broadspectrum heterocyclic substituted phenyl containing sulfonamide hiv protease inhibitors

Publications (1)

Publication Number Publication Date
BR0215260A true BR0215260A (pt) 2004-12-07

Family

ID=8181520

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0215260-6A BR0215260A (pt) 2001-12-21 2002-12-20 Inibidores de hiv protease de sulfonamida contendo fenila substituìda heterocìclica de amplo espectro

Country Status (24)

Country Link
US (1) US7763641B2 (pt)
EP (1) EP1463502B1 (pt)
JP (1) JP4578101B2 (pt)
KR (1) KR100942743B1 (pt)
CN (1) CN100448444C (pt)
AP (1) AP1922A (pt)
AR (1) AR037976A1 (pt)
AT (1) ATE516029T1 (pt)
AU (1) AU2002361235B2 (pt)
BR (1) BR0215260A (pt)
CA (1) CA2470964C (pt)
EA (1) EA009556B1 (pt)
HK (1) HK1070001A1 (pt)
HR (1) HRP20040662B1 (pt)
HU (1) HUP0500164A3 (pt)
IL (2) IL162574A0 (pt)
MX (1) MXPA04006201A (pt)
MY (1) MY138657A (pt)
NO (1) NO328122B1 (pt)
NZ (1) NZ533665A (pt)
PL (1) PL216539B1 (pt)
TW (1) TWI336621B (pt)
WO (1) WO2003053435A1 (pt)
ZA (1) ZA200405784B (pt)

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CA2509224A1 (en) * 2002-12-18 2004-07-15 Cytovia, Inc. 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
WO2005030194A1 (en) * 2003-09-30 2005-04-07 Tibotec Pharmaceuticals Ltd. Hcv inhibitiing sulfonamides
WO2005110428A2 (en) * 2004-05-07 2005-11-24 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
BRPI0607827B8 (pt) 2005-02-25 2021-05-25 Janssen R & D Ireland composto precursor de inibidor de protease, processo para a produção do referido composto e seu uso
WO2008004100A2 (en) 2006-07-05 2008-01-10 Pfizer Products Inc. Therapeutic compounds
WO2011076765A1 (en) 2009-12-23 2011-06-30 Katholieke Universiteit Leuven Novel antiviral compounds
WO2012031237A1 (en) * 2010-09-02 2012-03-08 Purdue Research Foundation Fused tricyclic ether carbamates and their use
MX343274B (es) 2010-11-15 2016-10-31 Viiv Healthcare Uk Ltd Inhibidores de la replicacion del vih.
WO2012065963A2 (en) 2010-11-15 2012-05-24 Katholieke Universiteit Leuven Novel antiviral compounds
EP3192794A4 (en) * 2014-09-11 2018-06-27 Shionogi & Co., Ltd. Sustained hiv protease inhibitor

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Also Published As

Publication number Publication date
PL216539B1 (pl) 2014-04-30
US20050222215A1 (en) 2005-10-06
PL370801A1 (en) 2005-05-30
ATE516029T1 (de) 2011-07-15
HRP20040662A2 (en) 2005-08-31
AP1922A (en) 2008-11-21
NO328122B1 (no) 2009-12-14
KR20040077863A (ko) 2004-09-07
WO2003053435A1 (en) 2003-07-03
EP1463502B1 (en) 2011-07-13
HUP0500164A3 (en) 2009-03-30
AP2004003083A0 (en) 2004-09-30
IL162574A (en) 2014-09-30
EA200400828A1 (ru) 2005-02-24
KR100942743B1 (ko) 2010-02-16
CA2470964A1 (en) 2003-07-03
CA2470964C (en) 2013-07-02
TWI336621B (en) 2011-02-01
CN100448444C (zh) 2009-01-07
NZ533665A (en) 2005-10-28
HRP20040662B1 (hr) 2013-12-06
MXPA04006201A (es) 2004-12-06
AR037976A1 (es) 2004-12-22
MY138657A (en) 2009-07-31
US7763641B2 (en) 2010-07-27
HUP0500164A2 (hu) 2005-05-30
HK1070001A1 (en) 2005-06-10
IL162574A0 (en) 2005-11-20
EP1463502A1 (en) 2004-10-06
JP2005513102A (ja) 2005-05-12
AU2002361235A1 (en) 2003-07-09
JP4578101B2 (ja) 2010-11-10
AU2002361235B2 (en) 2008-07-24
NO20043114L (no) 2004-09-20
ZA200405784B (en) 2005-11-30
TW200410673A (en) 2004-07-01
EA009556B1 (ru) 2008-02-28
CN1620292A (zh) 2005-05-25

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