HUP0500164A2 - Heterociklussal szubsztituált benzolszulfonamidok mint HIV proteáz inhibitorok és az ezeket tartalmazó gyógyszerkészítmények - Google Patents

Heterociklussal szubsztituált benzolszulfonamidok mint HIV proteáz inhibitorok és az ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0500164A2
HUP0500164A2 HU0500164A HUP0500164A HUP0500164A2 HU P0500164 A2 HUP0500164 A2 HU P0500164A2 HU 0500164 A HU0500164 A HU 0500164A HU P0500164 A HUP0500164 A HU P0500164A HU P0500164 A2 HUP0500164 A2 HU P0500164A2
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HU
Hungary
Prior art keywords
compounds
protease inhibitors
hiv protease
optionally
substituted
Prior art date
Application number
HU0500164A
Other languages
English (en)
Inventor
Sandrine Marie Helene Vendeville
Wim Gaston Verschueren
Abdellah Tahri
Samuel Leo Christiaan Moors
Montserrat Erra Solá
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Tibotec Pharmaceuticals Ltd.
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Publication date
Application filed by Tibotec Pharmaceuticals Ltd. filed Critical Tibotec Pharmaceuticals Ltd.
Publication of HUP0500164A2 publication Critical patent/HUP0500164A2/hu
Publication of HUP0500164A3 publication Critical patent/HUP0500164A3/hu

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic 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
    • C07D277/32Heterocyclic 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
    • C07D277/38Nitrogen atoms
    • C07D277/42Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • 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
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16Sulfonamides 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
    • C07C311/18Sulfonamides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/64Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/66Heterocyclic 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
    • C07D233/88Nitrogen atoms, e.g. allantoin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30Heterocyclic 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
    • C07D263/32Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic 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
    • C07D277/32Heterocyclic 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
    • C07D277/38Nitrogen atoms
    • C07D277/40Unsubstituted amino or imino radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic 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
    • C07D277/32Heterocyclic 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
    • C07D277/38Nitrogen atoms
    • C07D277/44Acylated amino or imino radicals
    • C07D277/46Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • 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
    • C07D417/04Heterocyclic 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
    • 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
    • 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
    • C07D417/14Heterocyclic 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
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    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/04Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12Ortho- 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
    • C07C2603/18Fluorenes; Hydrogenated fluorenes

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (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

A jelen találmány tárgya széles spektrumú, heterociklusos,szubsztituált benzol szulfonamid HIV proteáz inhibitorok. A találmány)az (I) általános képletű vegyületekre, N-oxidjaira, sóira,sztereoizomer formáira, racém elegyeire, prodrugjaira, észtereire ésmetabolitjaira vonatkozik, ahol H-aril jelentése aromás monociklusos,biciklusos vagy triciklusos, 3-14 gyűrűtagot tartalmazó heterociklus,amely egy vagy több heteroatom-gyűrűtagként nitrogén-, oxigén- vagykénatomot tartalmaz, és amely adott esetben szubsztituálva lehet (i)egy vagy több szénatomon 1-6 szénatomos alkilcsoporttal,halogénatommal, hidroxil-, adott esetben mono- vagy diszubsztituáltamino-, nitro-, ciano-, halogén-(1-6 szénatomos alkil)-, karboxil-, 3-7 szénatomos cikloalkil-, adott esetben mono- vagy di-szubsztituáltaminokarbonil-, metil-tio-, metil-szulfonil-, aril-, -(R7a)n-M-R7b,Het1 vagy Het2 csoporttal; ahol az adott esetben jelenlevőszubsztituensek bármelyik aminocsoporton egymástól függetlenüllehetnek R5 vagy -A-R6 csoport; és (ii) egy nitrogénatomon, ha jelenvan, hidroxil- vagy -A-R6 csoporttal, R1, R2, R3, R4, R5, R6, R7, R7b,A, L, M, Het1, Het2 jelentései és n értéke a leírásban megadottak. Atalálmány kiterjed a vegyületek széles spektrumu HIV proteázinhibitorként történő alkalmazására gyógyszerkészítményekelőállítására, valamint a vegyületeket tartalmazógyógyszerkészítményekre és diagnosztikai kitekre. Kiterjed a találmánytovábbá a vegyületek más anti-retrovirális szerrel történőkombinálására, és referenciavegyületként vagy reagensként történőalkalmazásukra kísérletekben. Ó
HU0500164A 2001-12-21 2002-12-20 Heterocyclic substituted benzenesulfonamides as hiv protease inhibitors and pharmaceutical compositions containing them HUP0500164A3 (en)

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 (2)

Publication Number Publication Date
HUP0500164A2 true HUP0500164A2 (hu) 2005-05-30
HUP0500164A3 HUP0500164A3 (en) 2009-03-30

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ID=8181520

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HU0500164A HUP0500164A3 (en) 2001-12-21 2002-12-20 Heterocyclic substituted benzenesulfonamides as hiv protease inhibitors and pharmaceutical compositions containing them

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

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100364531C (zh) * 2002-12-18 2008-01-30 西托维亚公司 3,5-二取代-[1,2,4]-二唑及类似物和其用途
JP2007507469A (ja) * 2003-09-30 2007-03-29 テイボテク・フアーマシユーチカルズ・リミテツド Hcv阻害性スルホンアミド
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
WO2008004100A2 (en) 2006-07-05 2008-01-10 Pfizer Products Inc. Therapeutic compounds
KR101483834B1 (ko) 2009-12-23 2015-01-16 카트호리이케 유니버시타이트 로이펜 항바이러스 화합물
EP2611295B1 (en) 2010-09-02 2017-07-19 Purdue Research Foundation Fused tricyclic ether carbamates and their use
WO2012066442A1 (en) 2010-11-15 2012-05-24 Pfizer Limited Inhibitors of hiv replication
KR20140003438A (ko) 2010-11-15 2014-01-09 카톨리에케 유니버시테이트 루벤 항바이러스성 축합 헤테로사이클릭 화합물
JPWO2016039403A1 (ja) * 2014-09-11 2017-06-29 塩野義製薬株式会社 持続性hivプロテアーゼ阻害剤

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JP4578101B2 (ja) 2010-11-10
CN1620292A (zh) 2005-05-25
IL162574A0 (en) 2005-11-20
BR0215260A (pt) 2004-12-07
IL162574A (en) 2014-09-30
CA2470964A1 (en) 2003-07-03
EA009556B1 (ru) 2008-02-28
AP2004003083A0 (en) 2004-09-30
NZ533665A (en) 2005-10-28
AU2002361235B2 (en) 2008-07-24
HUP0500164A3 (en) 2009-03-30
PL216539B1 (pl) 2014-04-30
HK1070001A1 (en) 2005-06-10
US7763641B2 (en) 2010-07-27
AP1922A (en) 2008-11-21
MXPA04006201A (es) 2004-12-06
EP1463502B1 (en) 2011-07-13
ZA200405784B (en) 2005-11-30
WO2003053435A1 (en) 2003-07-03
HRP20040662B1 (hr) 2013-12-06
ATE516029T1 (de) 2011-07-15
KR100942743B1 (ko) 2010-02-16
CA2470964C (en) 2013-07-02
HRP20040662A2 (en) 2005-08-31
NO328122B1 (no) 2009-12-14
EA200400828A1 (ru) 2005-02-24
EP1463502A1 (en) 2004-10-06
AU2002361235A1 (en) 2003-07-09
TW200410673A (en) 2004-07-01
AR037976A1 (es) 2004-12-22
PL370801A1 (en) 2005-05-30
US20050222215A1 (en) 2005-10-06
TWI336621B (en) 2011-02-01
KR20040077863A (ko) 2004-09-07
NO20043114L (no) 2004-09-20
JP2005513102A (ja) 2005-05-12
MY138657A (en) 2009-07-31
CN100448444C (zh) 2009-01-07

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