AR030558A1 - COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA, - Google Patents

COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA,

Info

Publication number
AR030558A1
AR030558A1 ARP010101794A ARP010101794A AR030558A1 AR 030558 A1 AR030558 A1 AR 030558A1 AR P010101794 A ARP010101794 A AR P010101794A AR P010101794 A ARP010101794 A AR P010101794A AR 030558 A1 AR030558 A1 AR 030558A1
Authority
AR
Argentina
Prior art keywords
conhch
alkyl
cycloalkyl
aryl
carbamate
Prior art date
Application number
ARP010101794A
Other languages
English (en)
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of AR030558A1 publication Critical patent/AR030558A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Un compuesto macrocíclico, incluyendo los enantiomeros, estereoisomeros rotámeros y tautomeros de dicho compuesto , así como las sales o solvatos farmacéuticamente aceptables de dicho compuesto, que tiene la estructura general expuesta en la formula (1) en la cual E, X e Y pueden estar independientemente presentes o ausentes y, en caso de estar presentes, son independientemente seleccionados entre las porciones: alquilo, arilo, alquilarilo, heteroarilo, arilheteroarilo, alquilheteroarilo, cicloalquilo, éter alquílico, éter alquilarílico, éter arílico, alquilamino, arilamino, alquilarilamino, alquilsulfuro, alquilarilsulfuro, arilsulfuro, alquilsulfona, alquilarilsulfona, arilsulfona, alquilalquilsulfoxido, alquilarilsulfoxido, alquilamida, arilamida, alquilsufonamida, alquilarilsulfonamida, arilsulfonamida, alquilurea, alquilarilurea, arilurea, carbamato de alquilo, carbamato de alquilarilo, carbamato de arilo, alquilhidrazida, alquilarilhidrazida, alquilhidroxamida, alquilarilhidroxamida, alquilsufonilo, arilsulfonilo, heteroalquilsulfonilo, hetroarilsulfonilo, alquilcarbonilo, arilcarbonilo, heteroarilalquilcarbonilo, heteroarilcarbonilo, alcoxicarbonilo, ariloxicarbonilo, hetoroariloxicarbonilo, alquilaminocarbonilo, arilaminocarbonilo, heteroarilaminocarbonilo, o una combinacion de las mismas; con la condicion de que optativamente E, X, e Y pueden estar sustituidas además con porciones seleccionadas entre el grupo que consiste en aromáticos, alquilo, alquilarilo, heteroalquilo, arilheteroarilo, alquilheteroarilo, cicloalquilo, éter alquílico, éter alquilarílico, alquilsulfuro, alquilarilsulfuro, alquilsulfona, alquilarilsulfona, alquilamida, alquilarilamida, alquilsulfonamida, alquilaminas, alquilarilsulfonamida, alquilurea, alquilarilurea, carbamato de alquilo, carbamato de alquilarilo, halogeno, hidroxilamino, carbazato de alquilo, carbazato de arilo; R1=COR5 o B(OR)2, donde R5=H, OH, OR8NR9R10, CF3, C2F5, C3F7, CF2R6, R6, COR7 donde R7 = H, OH, OR8, CHR9R10, donde R6, R8, R9 y R10 son independientemente seleccionados entre el grupo que consiste en H, alquilo, arilo, heteroalquilo, heteroarilo, cicloalquilo, cicloalquilo, arilalquilo, heteroarilalquilo, CH(R1')COOR11, CH(R1')CONR12R13, CH(R1')CONHCH(R2')COOR11, CH(R1')CONHCH(R2')CONR12R13, CH(R1')CONHCH(R2')CONHCH(R3')COOR11, CH(R1')CONHCH(R2')CONHCH(R3')CONR12R13, CH(R1')CONHCH(R2')CONHCH(R3')CONHCH(R4')COOR11, CH(R1')CONHCH(R2')CONHCH(R3')CONHCH(R4')CONR12R13, CH(R1')CONHCH(R2')CONHCH(R3')CONHCH(R4')CONHCH(R5')COOR11, CH(R1')CONHCH(R2')CONHCH(R3')CONHCHR4')CONHCH(R5')CONR12R13 donde R1', R2', R3', R4,', R5', R11, R12, R13 son independientemente seleccionados entre el grupo que consiste en H, alquilo, arilo, heteroalquilo, heteroarilo, cicloalquilo, alquilarilo, alquilheteroarilo, arilalquilo, y heteroaralquilo; Z es seleccionado entre O, N o CH; W puede estar presente o ausente y, en caso de estar presente W es seleccionado entre C=O, C=S, SO2 o C=NR; Q es (NR)p, O, S, CH2, CHR, CRR' o un enlace doble hacia V; A es O, CH2, (CHR)p, (CHR-CHR')p, (CRR')p, NR, S, SO2, C=O o un enlace; G es (CH2)p, (CHR)p, (CRR')p, NR, O, S, SO2, S(O)2NH, C=O o un enlace doble hacia E o V; V es CH, CR o N; p es un numero de 0 a 6 y R, R', R2, R3, y R4 son independientemente seleccionados entre el grupo que consiste en H, alquilo, C1-10, alquenilo C2-10, cicloalquilo C3-8, heterocicloalquilo C3-8, arilo, alcoxi, ariloxi, alquiltio, ariltio, amino, amido, éster, ácido carboxílico, carbamato, urea, cetona, aldehído, ciano, nitro, heteroarilo, alquilarilo, alquilheteroarilo, (cicloalquil)alquilo y (heterocicloalquil)alquilo, donde dicho cicloalquilo se compone de tres a ocho átomos de carbono y de cero a seis átomos de oxígeno, nitrogeno, azufre o fosforo y dicho alquilo es de uno a seis átomos de carbono; donde dichas porciones alquilo, heteroarilo, alquenilo, heteroalquenilo, arilo, heteroarilo cicloalquilo y heterocicloalquilo pueden estar optativamente sustituidas, y donde dicho término "sustituido" se refiere a una sustitucion optativa y adecuada con una o más opciones seleccionadas entre el grupo que consiste en alquilo, alquenilo, alquinilo, arilo, aralquilo, cicloalquilo, heterocíclico, halogeno, hidroxi, tio, alcoxi, ariloxi, alquiltio, ariltio, amino, amido, éster, ácido carboxílico, carbamato, urea, cetona, aldehído, ciano, nitro, sulfonamida, sulfoxido, sulfona, sulfonilurea, hidrazida e hidraxamato y tiourea; así como métodos para la preparacion de dichos compuestos. En otra realizacion, también se describen composiciones farmacéuticas que comprenden dichos macrocíclicos así como su uso para la cloracion de un medicamento en el tratamiento de trastornos asociados con la proteasa de VHC, inhibidores de la reina proteasa NS-3 del virus de la hepatitis C.
ARP010101794A 2000-04-19 2001-04-17 COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA, AR030558A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US19820400P 2000-04-19 2000-04-19

Publications (1)

Publication Number Publication Date
AR030558A1 true AR030558A1 (es) 2003-08-27

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010101794A AR030558A1 (es) 2000-04-19 2001-04-17 COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA,

Country Status (22)

Country Link
US (1) US6914122B2 (es)
EP (1) EP1274724A2 (es)
JP (1) JP4748912B2 (es)
KR (1) KR20020097220A (es)
CN (3) CN101580536A (es)
AR (1) AR030558A1 (es)
AU (1) AU2001253621A1 (es)
BR (1) BR0110104A (es)
CA (1) CA2406532A1 (es)
CZ (1) CZ20023473A3 (es)
HK (1) HK1048479A1 (es)
HU (1) HUP0302957A2 (es)
IL (1) IL151935A0 (es)
MX (1) MXPA02010375A (es)
NO (1) NO20025030L (es)
NZ (1) NZ521456A (es)
PE (1) PE20011288A1 (es)
PL (1) PL358591A1 (es)
RU (1) RU2002131163A (es)
SK (1) SK14952002A3 (es)
WO (1) WO2001081325A2 (es)
ZA (1) ZA200208014B (es)

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