CO4940496A1 - HIV PROTEASE INHIBITORS - Google Patents

HIV PROTEASE INHIBITORS

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Publication number
CO4940496A1
CO4940496A1 CO98014251A CO98014251A CO4940496A1 CO 4940496 A1 CO4940496 A1 CO 4940496A1 CO 98014251 A CO98014251 A CO 98014251A CO 98014251 A CO98014251 A CO 98014251A CO 4940496 A1 CO4940496 A1 CO 4940496A1
Authority
CO
Colombia
Prior art keywords
alkyl
group
cycloalkyl
aryl
acyl
Prior art date
Application number
CO98014251A
Other languages
Spanish (es)
Inventor
Albizati Kim
Siegfried Reich
Michael D Varney
E Zhang Kanyin
Kobayashi Takuo
Original Assignee
Agouron Pharma
Japan Tobacco Inc
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 Agouron Pharma, Japan Tobacco Inc filed Critical Agouron Pharma
Publication of CO4940496A1 publication Critical patent/CO4940496A1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D207/14Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/56Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no 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
    • C07D307/22Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no 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
    • C07D309/14Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/30Hetero atoms other than halogen
    • C07D333/36Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D335/00Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/02Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto de la fórmula (9): donde: R y R´ se seleccionan independientemente de H, un grupo de alquil-OR1 sustituido por mercapto, tioéter, nitro (NO2 ), amino, ariloxi, halógeno, hidroxilo, alcoxilo, acilo, arilo, cicloalquilo, heterociclos saturados y parcialmente saturados, o no sustituido, un grupo cicloalquilo sustituido con un grupo alquilo de (C1 -C6 ) o un grupo alquil-OH de (C1 -C6 ), un grupo heterociclo sustituido con un grupo alquilo de (C1 -C6 ) o un grupo alquil-OH de (C1 -C6 ), un grupo alquil-NR2 R3 o un grupo alquil- S(X)(Y)R4 , dondeR1 es H, un grupo alquilo sustituido por mercapto, tioéter, nitro (NO2 ), amino, ariloxi, halógeno, hidroxilo, alcoxilo, acilo, arilo, cicloalquilo, heterociclos saturados y parcialmente saturados, o no sustituido o un grupo acilo; R2 y R3 se seleccionan cada uno independientemente de H, grupos alquilos, cicloalquilos, heterociclos y arilos sustituidos o no sustituidos y grupos acilos y sulfonilos;donde los sustituyentes de los grupos alquilo y arilos son mercapto, tioéster, nitro (NO2 ), amino, ariloxi, halógeno, hidroxilo, alcoxilo, acilo, arilo, cicloalquilo, heterociclos saturados y parcialmente saturados. y los sustituyentes de los grupos cicloalquilos y heterociclos son mercapto, tioéster, nitro, amino, ariloxi, halógeno, hidroxilo, alcoxilo, acilo, arilo, cicloalquilo, heterociclos saturados y parcialmente saturados y alquilo, R4 es H, un grupo alquilo, cicloalquilo, heterociclo o arilo sustituido o no sustituido; donde los sustituyentes del grupo alquilo y arilo son mercapto, tioéter, nitro (NO2 ) amino, ariloxilo, halógeno, hiroxilo, alcoxilo, acilo, arilo, cicloalquilo, heterociclos saturados y parcialmente saturados. Y los sustituyentes del grupo cicloalquilo y heterociclo son mercapto, tioéter, nitro, amino, ariloxi, halógeno, hidroxilo, alcoxilo, acilo, arilo, cicloalquilo, heterociclos, saturados y parcialmente saturados y alquilo.X es Y se seleccionan cada uno independientemente de = O y nada; o una prodroga, sal o solvato farmacéuticamente aceptable de los mismos.A compound of formula (9): where: R and R 'are independently selected from H, a group of alkyl-OR1 substituted by mercapto, thioether, nitro (NO2), amino, aryloxy, halogen, hydroxyl, alkoxy, acyl, aryl, cycloalkyl, saturated and partially saturated, or unsubstituted heterocycles, a cycloalkyl group substituted with an alkyl group of (C1-C6) or an alkyl-OH group of (C1-C6), a heterocycle group substituted with an alkyl group of (C1-C6) or an alkyl-OH group of (C1-C6), an alkyl-NR2 group R3 or an alkyl-S (X) (Y) R4 group, where R1 is H, an alkyl group substituted by mercapto, thioether , nitro (NO2), amino, aryloxy, halogen, hydroxyl, alkoxy, acyl, aryl, cycloalkyl, saturated and partially saturated, or unsubstituted heterocycles or an acyl group; R2 and R3 are each independently selected from H, substituted or unsubstituted alkyl, cycloalkyl, heterocycles and aryl groups and acyl and sulfonyl groups; where the substituents on the alkyl and aryl groups are mercapto, thioester, nitro (NO2), amino, aryloxy, halogen, hydroxyl, alkoxy, acyl, aryl, cycloalkyl, saturated and partially saturated heterocycles. and the substituents for the cycloalkyl groups and heterocycles are mercapto, thioester, nitro, amino, aryloxy, halogen, hydroxyl, alkoxy, acyl, aryl, cycloalkyl, saturated and partially saturated heterocycles and alkyl, R4 is H, an alkyl, cycloalkyl group, heterocycle or substituted or unsubstituted aryl; where the substituents of the alkyl and aryl group are mercapto, thioether, nitro (NO2) amino, aryloxy, halogen, hiroxy, alkoxy, acyl, aryl, cycloalkyl, saturated and partially saturated heterocycles. And the substituents of the cycloalkyl and heterocycle group are mercapto, thioether, nitro, amino, aryloxy, halogen, hydroxyl, alkoxy, acyl, aryl, cycloalkyl, heterocycles, saturated and partially saturated and alkyl.X is Y are each independently selected from = O and nothing; or a pharmaceutically acceptable prodrug, salt or solvate thereof.

CO98014251A 1997-03-13 1998-03-13 HIV PROTEASE INHIBITORS CO4940496A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US81595197A 1997-03-13 1997-03-13

Publications (1)

Publication Number Publication Date
CO4940496A1 true CO4940496A1 (en) 2000-07-24

Family

ID=25219265

Family Applications (1)

Application Number Title Priority Date Filing Date
CO98014251A CO4940496A1 (en) 1997-03-13 1998-03-13 HIV PROTEASE INHIBITORS

Country Status (35)

Country Link
EP (1) EP0970055A2 (en)
JP (1) JP2001516350A (en)
KR (1) KR100511089B1 (en)
CN (1) CN1179948C (en)
AP (1) AP1358A (en)
AR (1) AR012556A1 (en)
AU (1) AU743078B2 (en)
BG (1) BG63540B1 (en)
BR (1) BR9808867A (en)
CA (1) CA2284163A1 (en)
CO (1) CO4940496A1 (en)
CZ (1) CZ296647B6 (en)
EA (1) EA002378B1 (en)
EE (1) EE04114B1 (en)
GE (1) GEP20022764B (en)
HR (1) HRP980112A2 (en)
HU (1) HUP0001380A3 (en)
IL (2) IL131870A0 (en)
IS (1) IS5176A (en)
MX (1) MXPA99008395A (en)
MY (1) MY117535A (en)
NO (1) NO315555B1 (en)
NZ (1) NZ337706A (en)
OA (1) OA11196A (en)
PA (1) PA8448801A1 (en)
PE (1) PE58799A1 (en)
PL (1) PL192786B1 (en)
SA (1) SA98181116B1 (en)
SK (1) SK283636B6 (en)
SV (1) SV1998000038A (en)
TR (1) TR199902508T2 (en)
TW (1) TW200517112A (en)
UA (1) UA57772C2 (en)
WO (1) WO1998040357A2 (en)
ZA (1) ZA982047B (en)

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5484926A (en) * 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors

Also Published As

Publication number Publication date
HUP0001380A2 (en) 2000-09-28
IS5176A (en) 1999-09-10
IL131870A0 (en) 2001-03-19
KR20000076236A (en) 2000-12-26
EE9900416A (en) 2000-04-17
SV1998000038A (en) 1999-02-15
CA2284163A1 (en) 1998-09-17
CZ296647B6 (en) 2006-05-17
EA002378B1 (en) 2002-04-25
AU743078B2 (en) 2002-01-17
HUP0001380A3 (en) 2001-12-28
BG103727A (en) 2000-04-28
CZ319199A3 (en) 2000-06-14
KR100511089B1 (en) 2005-08-31
SA98181116B1 (en) 2006-10-04
EA199900823A1 (en) 2000-04-24
EP0970055A2 (en) 2000-01-12
PL192786B1 (en) 2006-12-29
JP2001516350A (en) 2001-09-25
NO994415L (en) 1999-11-10
MY117535A (en) 2004-07-31
NZ337706A (en) 2001-04-27
NO315555B1 (en) 2003-09-22
NO994415D0 (en) 1999-09-10
SK283636B6 (en) 2003-11-04
TW200517112A (en) 2005-06-01
UA57772C2 (en) 2003-07-15
BR9808867A (en) 2000-07-11
WO1998040357A2 (en) 1998-09-17
AP1358A (en) 2004-12-03
EE04114B1 (en) 2003-08-15
AR012556A1 (en) 2000-11-08
PL335672A1 (en) 2000-05-08
AP9901648A0 (en) 1999-09-30
AU6457598A (en) 1998-09-29
PE58799A1 (en) 1999-07-12
CN1253548A (en) 2000-05-17
IL131870A (en) 2006-04-10
BG63540B1 (en) 2002-04-30
HRP980112A2 (en) 1998-12-31
WO1998040357A3 (en) 1998-11-26
SK122299A3 (en) 2000-05-16
OA11196A (en) 2003-05-21
TR199902508T2 (en) 2000-02-21
ZA982047B (en) 1998-09-28
MXPA99008395A (en) 2003-08-12
CN1179948C (en) 2004-12-15
PA8448801A1 (en) 2000-05-24
GEP20022764B (en) 2002-08-26

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