HUP0400438A2 - Széles spektrumú 2-amino-benzoxazol-6-szulfonamidok, alkalmazásuk HIV proteáz inhibitorként és az ezeket tartalmazó gyógyszerkészítmények - Google Patents

Széles spektrumú 2-amino-benzoxazol-6-szulfonamidok, alkalmazásuk HIV proteáz inhibitorként és az ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0400438A2
HUP0400438A2 HU0400438A HUP0400438A HUP0400438A2 HU P0400438 A2 HUP0400438 A2 HU P0400438A2 HU 0400438 A HU0400438 A HU 0400438A HU P0400438 A HUP0400438 A HU P0400438A HU P0400438 A2 HUP0400438 A2 HU P0400438A2
Authority
HU
Hungary
Prior art keywords
alkyl
cycloalkyl
hydrogen atom
compounds
aryl
Prior art date
Application number
HU0400438A
Other languages
English (en)
Inventor
Marie-Pierre T.M.M.G. Bethune
Herman Augustinus Kock
Dominique Louis Nestor Ghislain Surleraux
Abdellah Tahri
Sandrine Marie Helene Vendeville
Wim Gaston Verschueren
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 HUP0400438A2 publication Critical patent/HUP0400438A2/hu
Publication of HUP0400438A3 publication Critical patent/HUP0400438A3/hu

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    • 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
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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
    • 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
    • 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
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Virology (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

A jelen találmány tárgyát az (I) általános képletű vegyületek és N-oxidjaik, sóik, sztereoizomer formáik, racém keverékeik, előanyagaik,észtereik és metabolitjaik képezik, ahol R1 és R8 jelentése egymástólfüggetlenül hidrogénatom, adott esetben helyettesített 1-6 szénatomosalkil-, 2-6 szénatomos alkenil-, 3-7 szénatomos cikloalkil-, aril-,Hetl-, Het2-csoport; R1 jelentése lehet (R11aR=11b) NC (R10aR10b) CR9-csoport is; t jelentése 0, 1 vagy 2; R2 jelentése hidrogénatom vagy 1-6 szénatomos alkil-csoport; L jelentése -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -0-1-6 szénatomos alkándiil-C(=O)-, -NR8-1-6 szénatomosalkándiil C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2- csoport; R3jelentése 1-6 szénatomos a1ki1-, aril-, 3-7 szénatomos cikloalkil-, 3-7 szénatomos cikloalkil-l-4 szénatomos alkil- vagy aril-l-4 szénatomosalkilcsoport; R9 jelentése hidrogénatom, 1-9 szénatomosalkiloxikarbonil-, karboxi-, aminokarbonil-, mono- vagy di(1-4szénatomos alkil)aminokarbonil-, 3-7 szénatomos cikloalkil-, 2-6szénatomos alkenil-, 2-6 szénatomos alkinil- vagy adott esetbenhelyettesített 1-6 szénatomos alkilcsoport; R5 és R6 jelentésehidrogénatom vagy 1-6 szénatomos alkilcsoport. A találmány tárgyatovábbá a találmány szerinti vegyületek alkalmazása széles spektrumúHIV-proteáz inhibitorokként, eljárások előállításukra, valamint avegyületeket tartalmazó gyógyszerkészítmények és diagnosztikaikészletek (kitek). A találmány tárgya továbbá a találmány szerintivegyületek kombinálása más antiretrovirális szerrel és összehasonlítóvegyületekként vagy reagensekként való alkalmazása vizsgálatokban. Ó
HU0400438A 2001-05-11 2002-05-10 Broadspectrum 2-amino-benzoxazole-6-sulfonamides, their use as hiv protease inhibitor and pharmaceutical compositions containing them HUP0400438A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01201732 2001-05-11
PCT/EP2002/005212 WO2002092595A1 (en) 2001-05-11 2002-05-10 Broadspectrum 2-amino-benzoxazole sulfonamide hiv protease inhibitors

Publications (2)

Publication Number Publication Date
HUP0400438A2 true HUP0400438A2 (hu) 2004-08-30
HUP0400438A3 HUP0400438A3 (en) 2007-08-28

Family

ID=8180286

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0400438A HUP0400438A3 (en) 2001-05-11 2002-05-10 Broadspectrum 2-amino-benzoxazole-6-sulfonamides, their use as hiv protease inhibitor and pharmaceutical compositions containing them

Country Status (32)

Country Link
US (2) US7622490B2 (hu)
EP (1) EP1387842B1 (hu)
JP (1) JP4467889B2 (hu)
KR (1) KR100878853B1 (hu)
CN (1) CN100549007C (hu)
AP (1) AP1652A (hu)
AR (1) AR035970A1 (hu)
AT (1) ATE429431T1 (hu)
AU (1) AU2002310818B2 (hu)
BG (1) BG66350B1 (hu)
BR (1) BR0209594A (hu)
CA (1) CA2444895C (hu)
CY (1) CY1109247T1 (hu)
CZ (1) CZ304524B6 (hu)
DE (1) DE60232067D1 (hu)
DK (1) DK1387842T3 (hu)
EA (1) EA009590B1 (hu)
EE (1) EE05307B1 (hu)
ES (1) ES2325809T3 (hu)
HK (1) HK1062912A1 (hu)
HR (1) HRP20031026B1 (hu)
HU (1) HUP0400438A3 (hu)
IL (1) IL158093A0 (hu)
MX (1) MXPA03010258A (hu)
NO (1) NO326883B1 (hu)
NZ (1) NZ529250A (hu)
OA (1) OA13134A (hu)
PL (1) PL209029B1 (hu)
PT (1) PT1387842E (hu)
SK (1) SK287952B6 (hu)
WO (1) WO2002092595A1 (hu)
ZA (1) ZA200307799B (hu)

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DE10026698A1 (de) 2000-05-30 2001-12-06 Basf Ag Selbstemulgierende Wirkstoffformulierung und Verwendung dieser Formulierung
US7109230B2 (en) 2002-01-07 2006-09-19 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
US7157489B2 (en) 2002-03-12 2007-01-02 The Board Of Trustees Of The University Of Illinois HIV protease inhibitors
US8025899B2 (en) 2003-08-28 2011-09-27 Abbott Laboratories Solid pharmaceutical dosage form
SI1670773T1 (sl) * 2003-09-30 2007-06-30 Tibotec Pharm Ltd Postopki za pripravo benzoksazol sulfonamidnih spojin in njihovih intermediatov
US20050131042A1 (en) * 2003-12-11 2005-06-16 Flentge Charles A. HIV protease inhibiting compounds
US8193227B2 (en) 2003-12-11 2012-06-05 Abbott Laboratories HIV protease inhibiting compounds
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DE602004021640D1 (de) 2003-12-23 2009-07-30 Tibotec Pharm Ltd Verfahren zur herstellung von (1s,2r)-3-ää(4-aminophenyl)sulfonylü(isobutyl)aminoü-1-benzyl-2-hydroxypropylcarbamidsäure-(3r,3as,6ar)-hexahydrofuroä2,3-büfuran-3-ylester
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
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AR053845A1 (es) * 2005-04-15 2007-05-23 Tibotec Pharm Ltd 5-tiazolilmetil[(1s,2r)-3-[[(2-amino-6-benzoxazolil)sulfonil)](2-metilpropil)amino]-2-hidroxi-1-(fenilmetil)propil]carbamato como mejorador de farmacos metabolizados por el citocromo p450
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Also Published As

Publication number Publication date
HUP0400438A3 (en) 2007-08-28
NO326883B1 (no) 2009-03-09
ATE429431T1 (de) 2009-05-15
ZA200307799B (en) 2005-03-30
MXPA03010258A (es) 2005-03-07
DE60232067D1 (de) 2009-06-04
HRP20031026A2 (en) 2005-10-31
SK287952B6 (sk) 2012-06-04
HK1062912A1 (en) 2004-12-03
CZ304524B6 (cs) 2014-06-18
NZ529250A (en) 2005-05-27
DK1387842T3 (da) 2009-08-10
EE05307B1 (et) 2010-06-15
IL158093A0 (en) 2004-03-28
EA009590B1 (ru) 2008-02-28
KR100878853B1 (ko) 2009-01-15
AP1652A (en) 2006-08-11
EE200300547A (et) 2004-02-16
CY1109247T1 (el) 2014-07-02
PL366780A1 (en) 2005-02-07
WO2002092595A1 (en) 2002-11-21
CA2444895C (en) 2011-02-15
US20040106661A1 (en) 2004-06-03
JP2004534757A (ja) 2004-11-18
US7863306B2 (en) 2011-01-04
CZ20033290A3 (cs) 2004-05-12
BG108309A (bg) 2004-12-30
NO20034988D0 (no) 2003-11-10
CN100549007C (zh) 2009-10-14
EP1387842B1 (en) 2009-04-22
US7622490B2 (en) 2009-11-24
BR0209594A (pt) 2004-03-30
CA2444895A1 (en) 2002-11-21
HRP20031026B1 (en) 2012-07-31
BG66350B1 (bg) 2013-08-30
CN1507446A (zh) 2004-06-23
OA13134A (en) 2006-12-13
AU2002310818B2 (en) 2007-12-13
PL209029B1 (pl) 2011-07-29
ES2325809T3 (es) 2009-09-18
PT1387842E (pt) 2009-07-20
AP2003002904A0 (en) 2003-12-31
JP4467889B2 (ja) 2010-05-26
KR20040022417A (ko) 2004-03-12
SK14902003A3 (sk) 2004-07-07
EA200301234A1 (ru) 2004-04-29
EP1387842A1 (en) 2004-02-11
US20100029632A1 (en) 2010-02-04
AR035970A1 (es) 2004-07-28

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