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AR076259A2 - Derivados de 3,5-dietil-1h-pirazol-4-il-oxi nitrilos, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de infecciones por hiv - Google Patents

Derivados de 3,5-dietil-1h-pirazol-4-il-oxi nitrilos, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de infecciones por hiv

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Publication number
AR076259A2
AR076259A2 ARP100100890A ARP100100890A AR076259A2 AR 076259 A2 AR076259 A2 AR 076259A2 AR P100100890 A ARP100100890 A AR P100100890A AR P100100890 A ARP100100890 A AR P100100890A AR 076259 A2 AR076259 A2 AR 076259A2
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
heteroatom
optionally substituted
conr5r5
Prior art date
Application number
ARP100100890A
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English (en)
Original Assignee
Pfizer
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
Priority claimed from GB0108999A external-priority patent/GB0108999D0/en
Priority claimed from GB0127426A external-priority patent/GB0127426D0/en
Application filed by Pfizer filed Critical Pfizer
Publication of AR076259A2 publication Critical patent/AR076259A2/es

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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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/02Immunomodulators
    • 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
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    • 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
    • C07D231/14Heterocyclic 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 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
    • C07D231/18One oxygen or sulfur atom
    • 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
    • C07D231/14Heterocyclic 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 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
    • C07D231/18One oxygen or sulfur atom
    • C07D231/20One oxygen atom attached in position 3 or 5
    • 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
    • C07D233/56Heterocyclic 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 only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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

Abstract

Reivindicacion 1: Un compuesto caracterizado por la formula (1) o una sal farmacéuticamente aceptable del mismo, donde: R1 es H, alquilo C1-6, cicloalquilo C3-7 o -OR7, dicho alquilo C1-6 y cicloalquilo C3-7, pueden estar opcionalmente sustituidos por halo, -CN, -OR10, S(O)xR10, -CO2R10, -CONR5R10, -OCONR5R10, -NR5CO2R10, -NR10R11, -NR5COR10, -SO2NR5R10, -NR5CONR5R10, -NR5SO2R10 o R10; R2 es H, alquilo C1-6, alquenilo C3-6 o R9, dicho alquilo C1-6 están opcionalmente sustituido por halo, -OR5, -OR12, -CN, -CO2R7, -OCONR5R5, -CONR5R5, -C(=NR5)NR5OR5, -CONR5NR5R5, -NR6R6, -NR5R12, -NR5COR5, -NR5COR8, -NR5COR12, -NR5CO2R5, -NR5CONR5R5, -SO2NR5R5, -NR5SO2R5, R8 o R9; R3 es H o alquilo C1-6, dicho alquilo C1-6 está opcionalmente sustituido por halo, -CN, -OR5, -CO2R5, -CONR5R5, -OCONR5R5, -NR5CO2R5, -NR6R6, -NR5COR5, -SO2NR5R5, -NR5CONR5R5, -NR5SO2R5, R8 o R9; R4 es fenilo sustituido por R8, halo, -CN, alquilo C1-6, C1-6 haloalquilo C1-6, cicloalquilo C3-7 o alcoxi C1-6; cada R5 esta cada uno independientemente H, alquilo C1-6 o cicloalquilo C3-7 o, cuando dos grupos R5 están unidos al mismo átomo de nitrogeno, aquellos dos grupos tomados juntos con el átomo de nitrogeno al cual están unidos representan azetidinilo, pirrolidinilo, piperidinilo, homopiperidinilo, piperazinilo, homopiperazinilo o morfolinilo, dicho azetidinilo, pirrolidinilo, piperidinilo, homopiperidinilo, piperazinilo, homopiperazinilo y morfolinilo están opcionalmente sustituidos por C1-6 alquilo C1-6 o cicloalquilo C3-7; cada R6 es independientemente tanto H, alquilo C1-6 o cicloalquilo C3-7; R7 es alquilo C1-6 o cicloalquilo C3-7; R8 es un grupo heterocíclico aromático, de cinco o seis miembros que contiene (i) de 1 a 4 heteroátomo(s) de nitrogeno o (ii) 1 o 2 heteroátomo(s) de nitrogeno y 1 un heteroátomo de oxígeno o 1 heteroátomo de azufre o (iii) 1 o 2 heteroátomo(s) de oxigeno o azufre, dicho grupo heterocíclico esta opcionalmente sustituido por halo, oxo, -CN, -COR5, -CONR5R5, -SO2NR5R5, -NR5SO2R5, -OR5, -NR5R5, -(alquileno C1-6)-NR5R5, alquilo C1-6, fluoro alquilo C1-6 o cicloalquilo C3-7; R9 es un grupo heterocíclico saturado o parcialmente insaturado de cuatro a siete miembros, que contiene (i) 1 o 2 heteroátomo(s) de nitrogeno o (ii) 1 heteroátomo(s) de nitrogeno y 1 heteroátomo de oxígeno o 1 heteroátomo de azufre o (iii) 1 heteroátomo(s) de oxígeno o un heteroátomo(s) azufre, dicho grupo heterocíclico estando opcionalmente sustituido por oxo, alquilo C1-6 cicloalquilo C3-7, -SO2R5, -CONR5R5, -COOR5, -CO-(alquileno)-OR5 o -COR5 y opcionalmente sustituido sobre un átomo de carbono que no es adyacente a un heteroátomo por halo, -OR5, -NR5R5, -NR5COR5, -NR5COOR5, -NR5CONR5R5, -NR5SO2R5 o -CN; R10 es H, R8, R9, R13, alquilo C1-6, cicloalquilo C3-7 o -(alquilo C1-6)-(cicloalquilo C3-7), dicho alquilo C1-6 y cicloalquilo C3-7 estando opcionalmente sustituidos por -OR5, -OR13, R8, R9, R13 o -COR13; R11 es H, alquilo C1-6 o cicloalquilo C3-7, dicho alquilo C1-6 y cicloalquilo C3-7 estando opcionalmente sustituido por -OR5, -NR5R5, -NR5COR5, -CONR5R5, R8 o R9; R12 es alquilo C1-6 sustituido por R8, R9, -OR5, -CONR5R5, -NR5COR5 o -NR5R5; R13 es fenilo opcionalmente sustituido por halo, -CN, -COR5, -CONR5R5, -SO2NR5R5, -NR5SO2R5, -OR5, -NR5R5, -(alquileno C1-6)-NR5R5, alquilo C1-6, haloalquilo C1-6 o cicloalquilo C3-7; y x es 0, 1 o 2.
ARP100100890A 2001-04-10 2010-03-19 Derivados de 3,5-dietil-1h-pirazol-4-il-oxi nitrilos, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de infecciones por hiv AR076259A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0108999A GB0108999D0 (en) 2001-04-10 2001-04-10 Pyrazole derivatives
GB0127426A GB0127426D0 (en) 2001-11-15 2001-11-15 Pyrazole derivatives

Publications (1)

Publication Number Publication Date
AR076259A2 true AR076259A2 (es) 2011-06-01

Family

ID=26245955

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP020101281A AR037319A1 (es) 2001-04-10 2002-04-08 Compuestos derivados de pirazol, procedimientos para la preparacion, intermediarios, composiciones farmaceuticas, procedimiento de tratamiento
ARP100100890A AR076259A2 (es) 2001-04-10 2010-03-19 Derivados de 3,5-dietil-1h-pirazol-4-il-oxi nitrilos, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de infecciones por hiv

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ARP020101281A AR037319A1 (es) 2001-04-10 2002-04-08 Compuestos derivados de pirazol, procedimientos para la preparacion, intermediarios, composiciones farmaceuticas, procedimiento de tratamiento

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US (4) US7109228B2 (es)
EP (2) EP1377556B1 (es)
JP (1) JP3806090B2 (es)
KR (1) KR100569324B1 (es)
CN (1) CN100408564C (es)
AR (2) AR037319A1 (es)
AT (2) ATE358669T1 (es)
AU (1) AU2002242926B2 (es)
BG (1) BG66349B1 (es)
BR (1) BRPI0208811B8 (es)
CA (1) CA2443449C (es)
CR (1) CR7069A (es)
CY (2) CY1107626T1 (es)
CZ (1) CZ305099B6 (es)
DE (1) DE60219292T2 (es)
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ES (2) ES2283532T3 (es)
GE (1) GEP20053619B (es)
HR (1) HRP20030783B1 (es)
HU (1) HU229025B1 (es)
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NO (1) NO326518B1 (es)
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PE (1) PE20021056A1 (es)
PL (3) PL216985B1 (es)
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SI (2) SI1762567T1 (es)
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