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AR053902A1 - Inhibidores de aspartil proteasa heterociclicos macrociclicos - Google Patents

Inhibidores de aspartil proteasa heterociclicos macrociclicos

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Publication number
AR053902A1
AR053902A1 ARP060102460A ARP060102460A AR053902A1 AR 053902 A1 AR053902 A1 AR 053902A1 AR P060102460 A ARP060102460 A AR P060102460A AR P060102460 A ARP060102460 A AR P060102460A AR 053902 A1 AR053902 A1 AR 053902A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
heteroarylalkyl
cycloalkylalkyl
heterocycloalkyl
Prior art date
Application number
ARP060102460A
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English (en)
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Schering Corp
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Publication of AR053902A1 publication Critical patent/AR053902A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • A61P33/00—Antiparasitic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Reivindicacion 1: Un compuesto que tiene la formula estructural (1), o una sal, solvato o éster farmacéuticamente aceptable del mismo, en donde: W es un enlace, -C(=S)(C(R3)(R4))a, -(C(R3)(R4))aC(=S)-, S(O)1-2(C(R3)(R4))a-, -(C(R3)(R4))aS(O)1-2, - C(=O)(C(R3)(R4))a-, -(C(R3)(R4))aC(=O)-, -O(C(R3)(R4))a-, -(C(R3)(R4))aO-, -(C(R3(R4))a-, -N(R5)(C(R3)(R4))a-, -(C(R3)(R4))aN(R5)- o -C(=N(R5))(C(R3)(R4))a-, -(C(R3)(R4))aC(=N(R5))-; en donde a es 0-2; U es un enlace, -S(O)1-2-, -C(=O)-, -O-, - P(O)(OR6)-, -(C(R3)(R4))b-, -N(R5)- o -C(=N(R5))-; en donde b es 0-2; siempre que cuando W sea -S(O)-, -S(O)2-, -O-, o -N(R5)-, U no sea -S(O)-, -S(O)2-, -O-, o -N(R5)-; R1 y R5 están independientemente seleccionados a partir del grupo consistente en H, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, arilciclalquilo, -OR19, -CN, -C(O)R20, -C(O)OR19, -S(O)1-2R21, -C(O)N(R22)(R23), -S(O)1-2N(R22)(R23), -NO2, -N=C(R22)(R23) y -N(R22)(R23); o R5 es un grupo de formulas (2) a (5), en donde R26 numera 0 a 5 sustituyentes, m es 0 a 6 y n es 1 a 5; R2, R3, R4, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 y R18 están independientemente seleccionados a partir del grupo consistente en H, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquialquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, arilcicloalquilo, halo, -CF3, -SH, -OR19, -CN, -C(O)R20, -C(O)OR19, -S(O)0-2R21, -S(O)1-2N(R22)(R23), -C(O)N(R22)(R23), -N(R22)C(O)R20, -N(R22)C(O)N(R22)(R23), -N(R22)C(O)OR19, -N(R22)S(O)1-2R21, -NO2, -N=C(R22)(R23) y -N(R22)(R23); en donde c, d, e, f, g y h son 0- 4; X, Y y Z están independientemente seleccionados a partir del grupo consistente en -O-, -N(R5)- , -C(O)-, -S(O)0-2-, -C(O)N(R22)-, -N(R22)C(O)-, -S(O)1-2N(R22)-, -N(R22)S(O)1-2- o un enlace; L(s) y M(t) están independientemente seleccionados a partir del grupo consiste en cicloalquileno, heterocicloalquileno, alquenileno, alquinileno, arileno, heteroarileno, o un enlace; en donde los átomos del anillo e L y M están opcionalmente sustituidos con 1 a 5 grupos R24 independientemente seleccionados a partir del grupo consistente en H, alquilo alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, arilcicloalquilo, halo, -CF3, -SH, - OR19, -CN, -C(O)R20, -C(O)OR19, -S(O)0-2R21, -S(O)1-2N(R22)(R23), -C (O)N(R22)(R23), -N(R22)C(O)R20, -N(R22)C(O)N(R22)(R23), -N(R22)C(O)OR19, -N(R22)S(O)1-2R21, -NO2, -N=C(R22)(R23) y -N(R22)(R23); en donde s es 1 o 2 y t es 1 o 2; R19 es H, alquilo, alquenilo, alquinilo, arilo, cicloalquilo, cicloalquilalquilo, heteroarilo, arilalquilo, heteroarilalquilo, heterocicloalquilo o heterocicloalquilalquilo; R20 es H, alquilo, alquenilo, alquinilo, arilo, cicloalquilo, cicloalquilalquilo, heteroarilo, arilalquilo, heteroarilalquilo, heterocicloalquilo, heterocicloalquilalquilo o -N(R23)(R24); R21 es alquilo, alquenilo, alquinilo, arilo, cicloalquilo, cicloalquilalquilo, heteroarilo, arilalquilo, heteroarilalquilo, heterocicloalquilo o heterocicloalquilalquilo; R22 y R23 son H, alquilo, alquenilo, alquinilo, arilo, cicloalquilo, cicloalquilalquilo, heteroarilo, arilalquilo, heteroarilalquilo, heterocicloalquilo o heterocicloalquilalquilo; siempre que i) cuando U es un enlace, -O- o -N(R5)-, entonces R2 no está seleccionado a partir del grupo consistente en halo, -SH, -OR19, -S(O)0-2R21, -S(O)1-2N(R22)(R23), -N(R22)C(O)R20, -N(R22)C(O)N(R22)(R23), -N(R22)C(O)OR19, -N(R22)S(O)1-2R21, -NO2, -N=C(R22)(R23) y -N(R22)(R23); ii) cuando W es -O(C(R3)(R4))a- o -N(R5)(C(R3)(R4))a- y a es O, entonces R2 no está seleccionado a partir del grupo consistente en halo, -SH, -OR19, -S(O)0-2R21, -S(O)1-2N(R22)(R23), -N(R22)C(O)R20, -N(R22)C(O)N(R22)(R23), -N(R22)C(O)OR19, -N(R22)S(O)1- 2R21, -NO2, -N=C(R22)(R23) y -N(R22)(R23); iii) cuando W es -O(C(R3)(R4))a- o -N(R5)(C(R3)(R4))a- y a es 1 o 2, entonces R3 y R4 sobre el átomo de carbono adyacente al heteroátomo de W, no están seleccionados a partir del grupo consistente en halo, - SH, -OR19, -S(O)0-2R21, -S(O)1-2N(R22)(R23), -N(R22)C(O)R20, -N(R22)C(O)N(R22)(R23), -N(R22)C(O)OR19, -N(R22)S(O)1-2R21, -NO2, -N=C(R22)(R23) y -N(R22)(R23); iv) cuando U es un enlace, -O- o -N(R5)- y c es 0, entonces Z no es -O-, -N(R5)-, -S(O)0-2- , -N(R22)C(O)-, -S(O)1-2N(R22)- o -N(R22)S(O)1-2-; v) cuando W es -O(C(R3)(R4))a- o -N(R5)(C(R3)(R4))a- y a y c son 0, entonces Z no es -O-, -N(R5)-, -S(O)0-2-, -N(R22)C(O)-, -S(O)1-2N(R22)- o -N(R22)S(O)1-2-; vi) cuando Z es -O- o -N(R5)-, entonces R7, R8, R9 y R10 sobre el átomo de carbono adyacente a Z no están seleccionados a partir del grupo consistente en halo, -SH, -OR19, -S(O)0-2R21, -S(O)1-2N(R22)(R23), -N(R22)C(O)R20, -N(R22)C(O)N(R22)(R23), -N(R22)C(O)OR19, -N(R22)S(O)1-2R21, -NO2, - N=C(R22)(R23) y -N(R22)(R23); (vii) cuando Y es -O- o -N(R5)-, entonces R11, R12, R13 y R14 sobre el átomo de carbono adyacente a Y no están seleccionados a partir del grupo consistente en halo, -SH, -OR19, -S(O)0-2R21, -S(O)1-2N(R22)(R23), - N(R22)C(O)R20, -N(R22)C(O)N(R22)(R23), -N(R22)C(O)OR19, -N(R22)S(O)1-2R21, -NO2, -N=C(R22)(R23) y -N(R22)(R23); viii) cuando X es -O- o -N(R5)-, entonces R15, R16, R17, y R18 sobre el átomo de carbono adyacente a X no están seleccionados a partir del grupo consistente en halo, -SH, -OR19, -S(O)0-2R21, -S(O)1-2N(R22)(R23), -N(R22)C(O)R20, -N(R22)C(O)N(R22)(R23), -N(R22)C(O)OR19, -N(R22)S(O)1-2R21, -NO2, -N=C(R22)(R23) y -N(R22)(R23); ix) cuando d y e son ambos cero y M es un enlace, entonces Z o Y no pueden ser ambos -O-; x) cuando f y g son ambos cero y L es un enlace, entonces Y o X no pueden ser ambos -O-; xi) cuando h es 1, entonces X no es -O- o -N(R5)-; xii) X, L, M, Y, Z y los átomos de carbono de -(C(R17)(R18))h-, - (C(R15)(R16))g-, -(C(R13)(R14))r, -(C(R11)(R12))e-, -(C(R9)(R10))d- y -(C(R7)(R8))c-, conjuntamente con W, el carbono de -C(R2)- y el átomo de nitrogeno al cual W está unido forman un anillo de al menos 5 átomos; xiii) cuando W es un enlace, entonces el anillo formado por X, L, M, Y, Z y los átomos de carbono de -(C(R17)(R18)h, -(C(R15)(R16))g-, -(C(R13)(R14))f-, -(C(R11)(R12))e-, -(C(R9)(R10))d-, -(C(R7)(R8))c-, W, el carbono de -C(R2)- y el átomo de nitrogeno unido a W, posee un tamano de anillo superior a 9 átomos; y en donde cada uno de los grupos alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, arilcicloalquilo en las definiciones precedentes está independientemente no sustituido o sustituido con 1 a 5 residuos R26 independientemente seleccionados a partir del grupo consistente en alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, arilcicloalquilo, halo, haloalquilo, haloalcoxi, -CN, -CF3, -SH, -OR19, -CN, -CH(R22)R23), -C(O)R20, -C(O)OR19, - C(=NOR19)R22, -P(O)(OR19)(OR19), -S(O)0-2R21, -S(O)1-2N(R22)(R23), -C(O)N(R22)(R23), -N(R22)C(O)R20, -alquil-N(R22)C(O)R20, -N(R22)C(O)N(R22)(R23), -alquil-N(R22)C(O)N(R22)(R23), -CH2-R22, -N(R22)C(O)OR19, -N(R22)S(O)1-2R21, -N(R22)S(O)1-2, N(R22)(R23), -N3, -NO2, -N=C(R22)(R23), =NOR19-N(R22)(R23) y -alquil-N(R22)(R23); en donde cada uno del alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, arilcicloalquilo, halo, haloalquilo y haloalcoxi en el grupo R26 precedente está independientemente no sustituido o sustituido con 1 a 5 residuos R27 independientemente seleccionados a partir del grupo consistente en alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, arilcicloalquilo, halo, haloalquilo, haloalcoxi, -CN, - CF3, -SH, -OR19, -CN, -CH(R22)(R23), -C(O)R20, -C(O)OR19, -C(=NOR19)R22, -P(O)(OR19)(OR19), -S(O)0-2R21, -S(O)1-2N(R22)(R23), -C(O)N(R22)(R23), -N(R22)C(O)R20, -alquil-N(R22)C(O)R20, -N(R22)C(O)N(R22)(R23) , -alquil-N(R22)C(O)N(R22)(R23), -CH2-R22, - N(R22)C(O)OR19, -N(R22)S(O)1-2R21, -N(R22)S(O)1-2N(R22)(R23), -N3, -NO2, -N=C(R22)(R23), =NOR19-N(R22)(R23) y-alquil-N(R22)(R23).
ARP060102460A 2005-06-14 2006-06-12 Inhibidores de aspartil proteasa heterociclicos macrociclicos AR053902A1 (es)

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US (2) US7812013B2 (es)
EP (1) EP1902057B1 (es)
JP (1) JP2008543841A (es)
CN (1) CN101193892A (es)
AR (1) AR053902A1 (es)
CA (1) CA2609562A1 (es)
MX (1) MX2007016185A (es)
PE (1) PE20070078A1 (es)
TW (1) TW200716645A (es)
WO (1) WO2006138195A1 (es)

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