MXPA04008929A - Benzimidazol sulfonamidas sustituidas como inhibidores de amplio espectro de la proteasa del vih. - Google Patents

Benzimidazol sulfonamidas sustituidas como inhibidores de amplio espectro de la proteasa del vih.

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Publication number
MXPA04008929A
MXPA04008929A MXPA04008929A MXPA04008929A MXPA04008929A MX PA04008929 A MXPA04008929 A MX PA04008929A MX PA04008929 A MXPA04008929 A MX PA04008929A MX PA04008929 A MXPA04008929 A MX PA04008929A MX PA04008929 A MXPA04008929 A MX PA04008929A
Authority
MX
Mexico
Prior art keywords
4alkyl
6alkyl
amino
het2
aryl
Prior art date
Application number
MXPA04008929A
Other languages
English (en)
Inventor
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 MXPA04008929A publication Critical patent/MXPA04008929A/es

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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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (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)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

La presente invencion se refiere a compuestos que tienen la formula:(ver formula)los N-oxidos, sales, formas estereoisomericas, mezclas racemicas, profarmacos, esteres y metabolitos de los mismos, en la cual formula: R1 y R8 son, cada uno de ellos e independientemente entre si, H, alquilo de (C1-C6) opcionalmente sustituido, alquenilo de (C2-C6), cicloalquilo de (C3-C7), arilo Het1, Het2; R1 tambien puede ser radical de la formula (R11aR11b)NC(R10aR10b)R9; t vale 0, 1 o 2; R2 es H o alquilo de (C1-C6); L es -C(=O)-, -O-C(=O)-, -NR8- C(=O)-, -O-alcanodiilo(C1-C6)-C(=O)-, NR8-alcanodiilo(C1-C6)-C-(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2-; R3 es alquilo de (C1-C6), arilo, cicloalquilo de (C3-C7), cicloalquilo(C3-C7)alquilo(C1-C4), o arilo de (C1-C4); R4 es H, alquilo(C1-C4)OC(=O), carboxilo, amino C(=O), mono- o di(alquilo(C1-C4)) amino C(=o), cicloalquilo de (C3-C7), alquenilo de (C2-C6), alquinilo de (C2-C6) o alquilo de (C1-C6) opcionalmente sustituido; A es alcanodiilo de (C1-C6), -C(=O)-, -C(=S)-, -S(=O)2, alcanodiilo(C1-C6)-C(=O)-, alcanodiilo(C1-C6)-C(=S)- o alcanodiilo(C1-C6)-S(=O)2, R5 es H, OH, alquilo de (C1-C6), Het1alquilo(C1-C6), Het2alquilo(C1-C6), amino alquilo de (C1-C6) opcionalmente sustituido; R6 alquilo(C1-C6)O, Het1, Het1O, Het2, Het2O, arilo, arilo, alquilo(C1-C6)oxicarbonilamino o amino; y en el caso en que -A- no es alcanodiilo de (C1-C6), entonces R6 puede tambien se alquilo de (C1-C6), Het1alquilo(C1-C4), Het1Oalquilo(C1-C4), Het2alquilo(C1-C4), Het2Oalquilo(C1-C4), arilalquilo de (C1-C4), arilOalquilo de (C1-C4), o amino alquilo de (C1-C4); pudiendo cada uno de los grupos amino en la definicion de R6 estar sustituido; R5 y -A-R5 tomados conjuntamente con el atomo de nitrogeno al cual estan fijados pueden tambien formar Het1 o Het2, R12 es H, -NH2, -NR5R6, alquilo de (C1-C4) o alquilo-W-R14, estando dicho alquilo opcionalmente sustituido con halogeno, hidroxi, arilo, heteroarilo, Het1, Het2 o amino, estando dicho amino opcionalmente mono- o di sustituido con alquilo de (C1-C4), y R13 es H, alquilo de (C1-C6) opcionalmente sustituido por arilo, Ht1, Het2, hidroxi, halogeno, amino, pudiendo el grupo amino esta opcionalmente mono- o di-sustituido por alquilo de (C1-C4).
MXPA04008929A 2002-03-12 2003-03-12 Benzimidazol sulfonamidas sustituidas como inhibidores de amplio espectro de la proteasa del vih. MXPA04008929A (es)

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
MXPA04008929A true MXPA04008929A (es) 2004-11-26

Family

ID=27798870

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA04008929A MXPA04008929A (es) 2002-03-12 2003-03-12 Benzimidazol sulfonamidas sustituidas como inhibidores de amplio espectro de la proteasa del vih.

Country Status (26)

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

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101090102B1 (ko) * 2003-09-30 2011-12-07 티보텍 파마슈티컬즈 벤조옥사졸 설폰아미드 화합물 및 그의 중간체를 제조하는방법
MXPA06012909A (es) * 2004-05-07 2007-09-06 Sequoia Pharmaceuticals Inc Inhibidores de proteasa retroviral repelente de resistencia.
ES2331257T3 (es) 2005-02-25 2009-12-28 Tibotec Pharmaceuticals Sintesis de precursores de inhibidores de proteasas.
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
KR20120136411A (ko) 2012-12-18
EA011946B1 (ru) 2009-06-30
JP2005519952A (ja) 2005-07-07
KR20040093119A (ko) 2004-11-04
TW200400945A (en) 2004-01-16
TWI329639B (en) 2010-09-01
CA2479012A1 (en) 2003-09-18
WO2003076413A1 (en) 2003-09-18
JP4557552B2 (ja) 2010-10-06
AU2003219159B2 (en) 2009-09-03
EP1485358B1 (en) 2011-02-02
PL374152A1 (en) 2005-10-03
AP2111A (en) 2010-03-03
CN101935303B (zh) 2014-03-12
SI1485358T1 (sl) 2011-05-31
DE60335939D1 (de) 2011-03-17
PL213645B1 (pl) 2013-04-30
MY142238A (en) 2010-11-15
NO20035023D0 (no) 2003-11-12
US20090203743A1 (en) 2009-08-13
BR0303373A (pt) 2004-03-23
IL163960A0 (en) 2005-12-18
HRP20040936A2 (en) 2005-10-31
NZ535439A (en) 2009-09-25
AU2003219159A1 (en) 2003-09-22
US8143421B2 (en) 2012-03-27
CN1653053A (zh) 2005-08-10
KR20100102742A (ko) 2010-09-24
CA2479012C (en) 2011-11-01
EA200401188A1 (ru) 2005-04-28
HK1072053A1 (en) 2005-08-12
US20050171175A1 (en) 2005-08-04
EP1485358A1 (en) 2004-12-15
ATE497494T1 (de) 2011-02-15
CN101935303A (zh) 2011-01-05
DK1485358T3 (da) 2011-05-09
NO326702B1 (no) 2009-02-02
KR101302421B1 (ko) 2013-09-02
AR038928A1 (es) 2005-02-02
AP2004003151A0 (en) 2004-12-31
HRP20040936B1 (en) 2012-09-30
ZA200407242B (en) 2005-12-28

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