AR054617A1 - Derivados de pirrol[3, 4 - d]pirimidina como inhibidores de aspartil proteasas y composiciones farmacéuticas que los comprenden - Google Patents

Derivados de pirrol[3, 4 - d]pirimidina como inhibidores de aspartil proteasas y composiciones farmacéuticas que los comprenden

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Publication number
AR054617A1
AR054617A1 ARP060102461A ARP060102461A AR054617A1 AR 054617 A1 AR054617 A1 AR 054617A1 AR P060102461 A ARP060102461 A AR P060102461A AR P060102461 A ARP060102461 A AR P060102461A AR 054617 A1 AR054617 A1 AR 054617A1
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Argentina
Prior art keywords
cycloalkyl
arylheterocycloalkylalkyl
heteroarylheterocycloalkylalkyl
heteroarylcycloalkylalkyl
heterocycloalkenylaryl
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ARP060102461A
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English (en)
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Schering Corp
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Publication of AR054617A1 publication Critical patent/AR054617A1/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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • 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
    • A61P35/00—Antineoplastic 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Además se revela la actividad inhibitoria de la aspartil proteasa.Composiciones farmacéuticas que los contienen. También se revelanel uso de estos para tratar enfermedades cognitivas o neurodegenerativas en combinacion con un inhibidor de colinesterasa o un agonista m1 o antagonista m2 muscarínico. Reivindicacion 1: Un compuesto que tiene la formula estructural (1) o su estereoisomero, tautomero o sal aceptable para uso farmacéutico, donde j es 0 o 1; k es 0 o 1, siempre que cuando k es 1, U no puede ser -N-; W es un enlace, -C(=S)-, -S(O)-, -S(O)2-, -C(=O)-, -O-, -C(R6)(R7)-, -N(R5)-, -C(R6)(R7)C(=O)-, o -C(=N(R5))-; U es -N- o -C(R6)-; R es 1-5 grupos R21; R1, R2 y R5 se seleccionan independientemente grupo integrado por H, alquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilcicloalquilalquilo, heteroarilcicloalquilalquilo, arilheterocicloalquilalquilo, heteroarilheterocicloalquilalquilo, cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, alquenilo, arilalquenilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, alquinilo, arilalquinilo, arilo, cicloalquilarilo, heterocicloalquilarilo, cicloalquenilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilheteroarilo, heterocicloalquenilheteroarilo, -OR15, -CN, -C(=NR11)R8, -C(O)R8, -C(O)OR9, -S(O)R10, -S(O)2R10, -C(O)N(R11)(R12), -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -NO2, -N=C(R8)2 y -N(R11)(R12), siempre que R1 y R5 no sean ambos seleccionados de -NO2, - N=C(R8)2 y -N(R11)(R12), R3, R6 y R7 se seleccionan independientemente del grupo integrado por H, alquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilcicloalquilalquilo, heteroarilcicloalquilalquilo, arilheterocicloalquilalquilo, heteroarilheterocicloalquilalquilo, cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, alquenilo, arilalquenilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, alquinilo, arilalquinilo, arilo, cicloalquilarilo, heterocicloalquilarilo, cicloalquenilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilheteroarilo, heterocicloalquenilheteroarilo, halo, -CH2-O-Si(R9)(R10)(R19), -SH, -CN, -OR9, -C(O)R8, -C(O)OR9, -C(O)N(R11)(R12), -SR19, -S(O)N(R11)(R12), - S(O)2N(R11)(R12), -N(R11)(R12), -N(R11)C(O)R8, -N(R11)S(O)R10, -N(R11)S(O)2R10-, -N(R11)C(O)N(R12)(R13), -N(R11)C(O)OR9 y -C(=NOH)R8; R4 y R7a se seleccionan independientemente del grupo integrado por un enlace, alquileno, arilalquileno, heteroarilalquileno, cicloalquilalquileno, heterocicloalquilalquileno, arilcicloalquilalquileno, heteroarilcicloalquilalquileno, arilheterocicloalquilalquileno, heteroarilheterocicloalquilalquileno, cicloalquileno, arilcicloalquileno, heteroarilcicloalquileno, heterocicloalquileno, arilheterocicloalquileno, heteroarilheterocicloalquileno, alquenileno, arilalquenileno, cicloalquenileno, arilcicloalquenileno, heteroarilcicloalquenileno, heterocicloalquenileno, arilheterocicloalquenileno, heteroarilheterocicloalquenileno, alquinileno, arilalquinileno, arileno, cicloalquilarileno, heterocicloalquilarileno, cicloalquenilarileno, cicloalquenilarileno, heterocicloalquenilarileno, heteroarileno, cicloalquilheteroarileno, heterocicloalquilheteroarileno, cicloalquenilheteroarileno y heterocicloalquenilheteroarileno, siempre que ambos R4 y R7no sean un enlace; R4 y R7a juntos pueden ser una cadena de carbonos C1 a C8, donde, opcionalmente, uno, dos o tres carbonos del anillo pueden ser reemplazados por -O-, -C(O)-, -C(S)-, -S-,-S(O), -S(O)2- o -N(R5)-, y R4 y R7a junto con los átomos de C a los cuales están unidos, forman un anillo de 3 a 8 miembros, opcionalmente sustituido con R; con las siguientes salvedades: que cuando al menos uno de los C es reemplazado por -O-, -C(O)-, -C(S)-, -S-, -S(O)-, -S(O)2- o -N(R5)-; entonces el numero de C en la porcion R4 y R7a de la cadena que se une con U es b, donde b es 0 a 5, y el numero de C que están en la porcion de R4 y R7a de la cadena que se une con el C de -C(R3)- es c, donde c es 0 a 5; que cuando j es 0 o 1, al menos uno de los átomos en el anillo debe estar reemplazado por -O-, -C(O)-, -C(S)-, -S-, -S(O)-, -S(O)2- o -N(R5)- ; que cuando j es 0 o 1 y solo un C en el anillo está reemplazado con -O-, -C(O)-, -C(S)-, -S-, -S(O)-, -S(O)2- o -N(R5)-, R4 y R7a no pueden formar un cicloalquiléter; R8 se selecciona independientemente del grupo integrado por H, alquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilcicloalquilalquilo, heteroarilcicloalquilalquilo, arilheterocicloalquilalquilo, heteroarilheterocicloalquilalquilo, cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, alquenilo, arilalquenilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, alquinilo, arilalquinilo, arilo, cicloalquilarilo, heterocicloalquilarilo, cicloalquenilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilheteroarilo, heterocicloalquenilheteroarilo, -OR15, -N(R15)(R16), -N(R15)C(O)R16, -N(R15)S(O)R16, -N(R15)S(O)2R16, N(R15)S(O)2N(R16)(R17), -N(R15)S(O)N(R16)(R17), -N(R15)C(O)N(R16)(R17), y -N(R15)C(O)OR16; R9 se selecciona independientemente del grupo integrado por H, alquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilcicloalquilalquilo, heteroarilcicloalquilalquilo, arilheterocicloalquilalquilo, heteroarilheterocicloalquilalquilo, cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, alquenilo, arilalquenilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, alquinilo, arilalquinilo, arilo, cicloalquilarilo, heterocicloalquilarilo, cicloalquenilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilheteroarilo, y heterocicloalquenilheteroarilo; R10 se selecciona independientemente del grupo integrado por H, alquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilcicloalquilalquilo, heteroarilcicloalquilalquilo, arilheterocicloalquilalquilo, heteroarilheterocicloalquilalquilo, cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, alquenilo, arilalquenilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, alquinilo, arilalquinilo, arilo, cicloalquilarilo, heterocicloalquilarilo, cicloalquenilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilheteroarilo, heterocicloalquenilheteroarilo, y -N(R15)(R16); R11, R12 y R13 se seleccionan independientemente del grupo integrado por H, alquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilcicloalquilalquilo, heteroarilcicloalquilalquilo, arilheterocicloalquilalquilo, heteroarilheterocicloalquilalquilo, cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, alquenilo, arilalquenilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, alquinilo, arilalquinilo, arilo, cicloalquilarilo, heterocicloalquilarilo, cicloalquenilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilheteroarilo, heterocicloalquenilheteroarilo, - C(O)R8, -C(O)OR9, -S(O)R10, -S(O)2R10, -C(O)N(R11)(R12), -S(O)N(R11)(R12), -S(O)2N(R11)(R12), y -CN; R15, R16 y R17 se seleccionan independientemente del grupo integrado por H, alquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilcicloalquilalquilo, heteroarilcicloalquilalquilo, arilheterocicloalquilalquilo, heteroarilheterocicloalquilalquilo, cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, alquenilo, arilalquenilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, alquinilo, arilalquinilo, arilo, cicloalquilarilo, heterocicloalquilarilo, cicloalquenilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilheteroarilo, heterocicloalquenilheteroarilo, R18-alquilo, R18-arilalquilo, R18-heteroarilalquilo, R18-cicloalquilalquilo, R18-heterocicloalquilalquilo, R18-arilcicloalquilalquilo, R18-heteroarilcicloalquilalquilo, R18-arilheterocicloalquilalquilo, R18-heteroarilheterocicloalquilalquilo, R18-cicloalquilo, R18arilcicloalquilo, R18- heteroarilcicloalquilo, R18-heterocicloalquilo, R18-arilheterocicloalquilo, R18-heteroarilheterocicloalquilo, R18-alquenilo, R18-arilalquenilo, R18-cicloalquenilo, R18-arilcicloalquenilo, R18-heteroarilcicloalquenilo, R18-heterocicloalquenilo, R18- arilheterocicloalquenilo, R18-heteroarilheterocicloalquenilo, R18-alquinilo, R18-arilalquinilo, R18-arilo, R18-cicloalquilarilo, R18-heterocicloalquilarilo, R18-cicloalquenilarilo, R18-heterocicloalquenilarilo, R18-heteroarilo, R18- cicloalquilheteroarilo, R18-heterocicloalquilheteroarilo, R18-cicloalquenilheteroarilo y R18-hete
ARP060102461A 2005-06-14 2006-06-12 Derivados de pirrol[3, 4 - d]pirimidina como inhibidores de aspartil proteasas y composiciones farmacéuticas que los comprenden AR054617A1 (es)

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US (1) US7868000B2 (es)
EP (1) EP1896478B1 (es)
JP (2) JP2008543849A (es)
KR (1) KR20080029965A (es)
CN (1) CN101228163A (es)
AR (1) AR054617A1 (es)
AU (1) AU2006259572A1 (es)
BR (1) BRPI0612072A2 (es)
CA (1) CA2609582A1 (es)
EC (1) ECSP078003A (es)
IL (1) IL187814A0 (es)
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