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AR056865A1 - Heterociclos nitrogenados y su uso como inhibidores de proteasas, composiciones farmaceuticas - Google Patents

Heterociclos nitrogenados y su uso como inhibidores de proteasas, composiciones farmaceuticas

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Publication number
AR056865A1
AR056865A1 ARP060102462A ARP060102462A AR056865A1 AR 056865 A1 AR056865 A1 AR 056865A1 AR P060102462 A ARP060102462 A AR P060102462A AR P060102462 A ARP060102462 A AR P060102462A AR 056865 A1 AR056865 A1 AR 056865A1
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AR
Argentina
Prior art keywords
ring
cycloalkenyl
cycloalkyl
heterocyclyl
group
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ARP060102462A
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English (en)
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Schering Corp
Pharmacopeia Drug Discovery
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Publication of AR056865A1 publication Critical patent/AR056865A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P31/10—Antimycotics
    • 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
    • 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
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • 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

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

Abstract

Composiciones farmacéuticas que comprenden los compuestos de la formula (1) y el método para inhibir aspartil proteasas y, en particular, los métodos para tratar enfermedades cardiovasculares, enfermedades cognitivas y neuroedegenerativas. Reivindicacion 1: Un compuesto que presenta la formula estructural (1), o un estereoisomero, tautomero o sal o solvato del mismo aceptable para uso farmacéutico, donde Q es un enlace o -N(R5)-; T es un enlace, -O-, -C(O)-; -S-, -N(R5)-, -S(O)-, -S(O)2- o -C(R6'R7')-; U es un enlace o -C(R6)(R7)-; Y es C o N; Z es C o N; el anillo A, que incluye las variables Y y Z, es un anillo cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilo, arilo y heteroarilo de tres a nueve miembros que tiene 0 a 7, con preferencia 0 a 4, heteroátomos seleccionados independientemente del grupo que consiste en O, S, N y -N(R)-, donde el anillo A está no sustituido o sustituido con 1 a 5 residuos R1 seleccionados independientemente y/u oxo cuando el anillo A es cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo; donde R se selecciona independientemente del grupo que consiste en hidrogeno alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, arilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, heteroarilalquilo, arilcicloalquilo, -OR15, -C(O)R8, -C(O)OR9, -S(O)R10, -S(O)2R10, -C(O)N(R11)(R12), -S(O)N(R11)(R12) y -S(O)2N(R11)(R12); R1 se selecciona independientemente del grupo que consiste en H, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halo, -CN, -OR15, -C(O)R15, -C(O)OR15, - C(O)N(R15)(R16), -S(O)0-2R15, -S(O)N(R15)(R16), -S(O)1-2-N(15)(R16), S(O)2N(R15)(R16), -C(=NOR15)R16, -P(O)(OR15)(OR16), -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; y opcionalmente, iii) cuando el anillo A está disustituido con dos grupos en el mismo átomo de carbono, los dos grupos R1 junto con el átomo de carbono del anillo forman un anillo cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo de 3 a 7 miembros que tiene 0 a 4, con preferencia 0 a 2, heteroátomos seleccionados independientemente del grupo que consiste en O, N, S o -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos o iv) cuando el anillo A está disustituido con: a) dos grupos R1; o b) un grupo R y un grupo R1, los dos grupos o el grupo R y el grupo R1 junto con los átomos del anillo A al cual están unidos forman un anillo cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilo, arilo o heteroarilo de 3 a 7 miembros que tiene 0 a 4, con preferencia 0 a 2 heteroátomos seleccionados independientemente del grupo que consiste en O, N, S o -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos R14; R2 se selecciona independientemente del grupo que consiste en 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, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilarilo, heterocicloalquenilarilo, -OR15, -CN, -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(R8)2; R3, R4, R6 y R7 se seleccionan independientemente del grupo que consiste en 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, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilarilo, heterocicloalquenilarilo, halo, -CH2-O-Si(R9)(R10)(R19), -SH, -CN, -OR9, -C(O)R5, -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; y opcionalmente, (i) R3 y R4, junto con el átomo al cual están unidos forman un anillo cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilo, arilo o heteroarilo de 3 a 8 miembros que tiene 0 a 3 heteroátomos seleccionados independientemente del grupo que consiste en O, N, S y -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos R14 y/u oxo, cuando dicho anillo es un anillo cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo; (ii) R6 y R7, junto con el carbono al cual están unidos forman un anillo cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilo, arilo o heteroarilo de 3 a 8 miembros que tiene 0 a 3 heteroátomos seleccionados independientemente del grupo que consiste en O, N, S o -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos R14 y/u oxo, cuando dicho anillo es un anillo cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo; (iii) cuando U es - C(R6)(R7)-, R3 y R6 junto con los átomos de carbono a los cuales están unidos forman un anillo de cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilo, arilo o heteroarilo de 3 a 7 miembros que tiene 0 a 4, con preferencia 0 a 2 heteroátomos seleccionados independientemente del grupo que consiste en O, N, S o -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos R14 y/u oxo cuando dicho anillo es un anillo cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo; (iv) cuando T es -C(R6')(R7'), R3 y R6' junto con los átomos de carbono a los cuales están unidos forman un anillo cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilarilo o heteroarilo de 3 a 7 miembros que tiene 0 a 4, con preferencia 0 a 2 heteroátomos seleccionados independientemente del grupo que consiste en O, N, S o -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos R14 y/u oxo cuando dicho anillo es un anillo cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo; (v) cuando T es -N(R5)-, R3 y R5 junto con los átomos a los cuales están unidos forman un anillo heterociclilo, heterociclenilo, heteroarilo de 3 a 7 miembros que tiene 1 a 4, con preferencia 1 a 2, heteroátomos seleccionados independientemente del grupo que consiste en O, N, S o -N(R)-, el cual está opcionalmente sustituido con 1 a 5 grupos R14 y/o con oxo cuando dicho anillo es un anillo heterociclilo o un anillo heterociclenilo; o (vi) a) R3 y R4, junto con el carbono al cual están unidos, o b) R6 y R7 junto con el carbono al cual están unidos, forman uno de los grupos multicíclicos (2), donde: M es independientemente -(CH2)-, -S-, -N(R19)-, -O-, -S(O)-, -S(O)2- o -C(O)-; q es 0, 1 o 2; A y B son independientemente arilo, heteroarilo, cicloalquilo, cicloalquenilo o heterociclilo; E es arilo o heteroarilo; y F es cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo, con la condicion de que no haya ningun átomo de oxigeno y/o azufre adyacente presente en el sistema anular y además con la condicion de que ambos (a) R3 y R4; y (b) R6 y R7 no se puedan combinar para formar dichos grupos multicíclicos (2), al mismo tiempo; R5 se selecciona del grupo que consiste en 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, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilarilo, heterocicloalquenilarilo, - CH2-O-Si(R9)(R10)(R19), -CN, -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; R6' y R7' se seleccionan independientemente del grupo que consiste en 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, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquil-heteroarilo, cicloalquenilarilo, heterocicloalquenilarilo, -halo, -CH2-O-Si(9)(R10)(R19), -SH, -CN, -OR9, -C(O)R8, -C(O)OR9, -C(O)N(R11)(P12), -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; u opcionalmente R6' y R7' jun
ARP060102462A 2005-06-14 2006-06-12 Heterociclos nitrogenados y su uso como inhibidores de proteasas, composiciones farmaceuticas AR056865A1 (es)

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Publication number Priority date Publication date Assignee Title
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
AU2006259572A1 (en) 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
WO2006138192A1 (en) * 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
ES2537898T3 (es) 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
KR20090015967A (ko) 2006-06-12 2009-02-12 쉐링 코포레이션 헤테로사이클릭 아스파르틸 프로테아제 억제제
TW200815349A (en) * 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
CA2672293A1 (en) 2006-12-12 2008-06-19 Schering Corporation Aspartyl protease inhibitors
EP2061771A1 (en) * 2006-12-12 2009-05-27 Schering Corporation Aspartyl protease inhibitors containing a tricyclic ring system
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
KR20100017255A (ko) 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
TW200902499A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
WO2009005470A1 (en) * 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
WO2009005471A1 (en) * 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
EP2200990A1 (en) 2007-09-06 2010-06-30 Schering Corporation Gamma secretase modulators
CN101910178A (zh) 2007-11-05 2010-12-08 先灵公司 γ分泌酶调节剂
JP2011506461A (ja) 2007-12-11 2011-03-03 シェーリング コーポレイション γ−セクレターゼモジュレーター
ES2475206T3 (es) 2008-02-01 2014-07-10 Takeda Pharmaceutical Company Limited Derivados de oxima como inhibidores de HSP90
EP2305672B1 (en) 2008-06-13 2019-03-27 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY
MY148558A (en) 2008-09-11 2013-04-30 Amgen Inc Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use
CN102186841A (zh) 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
RU2011123862A (ru) 2008-11-13 2012-12-20 Шеринг Корпорейшн Модуляторы гамма-секретазы
US20100125081A1 (en) * 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 574
WO2010056195A1 (en) * 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
TW201020244A (en) * 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
EP2379563B1 (en) 2008-12-22 2014-07-16 Merck Sharp & Dohme Corp. Gamma secretase modulators
AR074702A1 (es) * 2008-12-22 2011-02-02 Schering Corp Moduladores de gamma secretasa y composiciones farmaceuticas que los contienen
US20120232108A1 (en) 2009-06-16 2012-09-13 Xianhai Huang Gamma secretase modulators
EP2443119A1 (en) 2009-06-16 2012-04-25 Schering Corporation Gamma secretase modulators
EP2443121A2 (en) 2009-06-16 2012-04-25 Schering Corporation Gamma secretase modulators
EP2281824A1 (en) 2009-08-07 2011-02-09 Noscira, S.A. Furan-imidazolone derivatives, for the treatment of cognitive, neurodegenerative or neuronal diseases or disorders
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
EP2485920B1 (en) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2011044184A1 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
JP5584352B2 (ja) 2010-03-15 2014-09-03 アムジエン・インコーポレーテツド β−セクレターゼ調節剤としてのアミノ−ジヒドロオキサジン系およびアミノ−ジヒドロチアジン系スピロ化合物ならびにそれらの医学的用途
WO2011115938A1 (en) 2010-03-15 2011-09-22 Amgen Inc. Spiro-tetracyclic ring compounds as beta - secretase modulators
CN102933564B (zh) 2010-06-09 2015-07-22 詹森药业有限公司 用作β-分泌酶(BACE)抑制剂的5,6-二氢-2H-[1,4]噁嗪-3-基-胺衍生物
EP2601197B1 (en) 2010-08-05 2014-06-25 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
MX2013003246A (es) * 2010-09-22 2013-05-22 Janssen Pharmaceutica Nv Derivados de 4, 7-dihidro-pirazolo [1, 5-a] pirazin-6-ilamina utiles como inhibidores de beta-secretasa (bace).
JP5766198B2 (ja) * 2010-10-29 2015-08-19 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
CN103261199A (zh) 2010-10-29 2013-08-21 盐野义制药株式会社 萘啶衍生物
JP2013542973A (ja) 2010-11-22 2013-11-28 ノスシラ、ソシエダッド、アノニマ 神経変性疾患または神経変性状態を治療するためのビピリジンスルホンアミド誘導体
WO2012071279A1 (en) 2010-11-23 2012-05-31 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
WO2012085038A1 (en) 2010-12-22 2012-06-28 Janssen Pharmaceutica Nv 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
US9346827B2 (en) 2011-02-07 2016-05-24 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use
WO2012112462A1 (en) 2011-02-15 2012-08-23 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
PL2681219T3 (pl) 2011-03-01 2016-03-31 Janssen Pharmaceutica Nv Pochodne 6,7-dihydropirazolo[1,5-a]pirazyn-4-yloaminowe jako inhibitory beta-sekretazy (BACE)
JP5853035B2 (ja) 2011-03-09 2016-02-09 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ β−セクレターゼ（ＢＡＣＥ）の阻害剤として有用な３，４−ジヒドロ−ピロロ［１，２−ａ］ピラジン−１−イルアミン誘導体
WO2012138734A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2012138590A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2012147763A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤
EP2747769B1 (en) 2011-08-22 2017-08-02 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
WO2013044092A1 (en) 2011-09-21 2013-03-28 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
EP3607946B1 (en) 2012-03-19 2023-02-22 Buck Institute for Research on Aging App specific bace inhibitors (asbis) and uses thereof
WO2014062549A1 (en) 2012-10-17 2014-04-24 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2908824B1 (en) 2012-10-17 2018-05-02 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
WO2014078314A1 (en) 2012-11-15 2014-05-22 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US10202355B2 (en) 2013-02-12 2019-02-12 Buck Institute For Research On Aging Hydantoins that modulate bace-mediated app processing
US9663475B2 (en) 2013-02-25 2017-05-30 Merck Patent Gmbh 2 amino-3,4-dihydrcquinazoline derivatives and the use thereof as cathepsin D inhibitors
CN105324383B (zh) 2013-06-12 2017-10-31 詹森药业有限公司 作为β‑分泌酶(BACE)抑制剂的4‑氨基‑6‑苯基‑6,7‑二氢[1,2,3]三唑并[1,5‑A]吡嗪衍生物
ES2627633T3 (es) 2013-06-12 2017-07-28 Janssen Pharmaceutica N.V. Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]piracin-3(2H)-ona como inhibidores de beta-secretasa (BACE)
ES2697684T3 (es) 2013-06-12 2019-01-25 Janssen Pharmaceutica Nv Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE)
KR20170095881A (ko) 2014-12-18 2017-08-23 얀센 파마슈티카 엔.브이. 베타―세크레타제의 ２,３,４,５―테트라히드로피리딘―６―아민 및 ３,４―디히드로―２ｈ―피롤―５―아민 화합물 억제제
RU2642246C2 (ru) * 2014-12-30 2018-01-24 Федеральное государственное бюджетное научное учреждение "Институт экспериментальной медицины" (ФГБНУ "ИЭМ") Применение пробиотического штамма микроорганизма enterococcus faecium l-3 для лечения нейродегенеративных заболеваний
US20200069691A1 (en) * 2016-12-22 2020-03-05 Merck Sharp & Dohme Corp. Heterocyclic compounds as hiv protease inhibitors
WO2019023247A1 (en) 2017-07-25 2019-01-31 Immutics, Inc. TREATMENT OF CANCER BY BLOCKING THE INTERACTION OF TIM-3 AND ITS LIGAND
JOP20180094A1 (ar) 2017-10-18 2019-04-18 Hk Inno N Corp مركب حلقي غير متجانس كمثبط بروتين كيناز
CN110563631B (zh) * 2018-06-05 2023-05-23 爱斯特（成都）生物制药股份有限公司 一种抑制ido的化合物及其应用
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
CN116063505B (zh) 2019-01-30 2024-05-03 真和制药有限公司 抗gal3抗体及其用途
EP4157338A4 (en) 2020-05-26 2024-11-13 TrueBinding, Inc. METHOD FOR TREATING INFLAMMATORY DISEASES BY GALECTIN-3 BLOCKING

Family Cites Families (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1077204A (en) 1912-11-20 1913-10-28 John Bonner Semple Tracer for projectiles.
US3632814A (en) * 1968-11-25 1972-01-04 Velsicol Chemical Corp Phosphoramidate esters
JPS5013951B1 (es) * 1969-05-23 1975-05-23
DE2430354A1 (de) * 1974-06-25 1976-01-15 Basf Ag Neue substituierte 1-amino-isoindole, verfahren zu deren herstellung sowie diese enthaltende pharmazeutische zubereitungen
DE2757982C2 (de) * 1977-12-24 1980-02-21 Basf Ag, 6700 Ludwigshafen Verbindungen der Isoindolinreihe und Verfahren zur Herstellung von in den anwendungstechnischen Eigenschaften verbesserten Pigmenten
WO1983002920A1 (fr) * 1982-02-27 1983-09-01 Kabashima, Kazuo Procede de coloration et materiau de formation de couleur
IL92011A0 (en) * 1988-10-19 1990-07-12 Abbott Lab Heterocyclic peptide renin inhibitors
AU2436792A (en) 1991-08-16 1993-03-16 Merck & Co., Inc. Quinazoline derivatives as inhibitors of hiv reverse transcriptase
DE4419849A1 (de) * 1994-06-07 1995-12-14 Hoechst Ag Isoindolinpigmente
US5629322A (en) 1994-11-15 1997-05-13 Merck & Co., Inc. Cyclic amidine analogs as inhibitors of nitric oxide synthase
JP3666922B2 (ja) * 1995-02-21 2005-06-29 山本化成株式会社 カルボン酸塩、その製造方法および該塩化合物を用いる感熱記録材料
US5889006A (en) 1995-02-23 1999-03-30 Schering Corporation Muscarinic antagonists
IL117149A0 (en) 1995-02-23 1996-06-18 Schering Corp Muscarinic antagonists
DE19516804A1 (de) * 1995-05-08 1996-11-14 Hoechst Ag Isoindolinpigmente auf Basis von Aminochinoxalindionen
US5935958A (en) 1996-07-01 1999-08-10 Schering Corporation Muscarinic antagonists
US5952349A (en) 1996-07-10 1999-09-14 Schering Corporation Muscarinic antagonists for treating memory loss
US5977138A (en) 1996-08-15 1999-11-02 Schering Corporation Ether muscarinic antagonists
AU9298098A (en) * 1997-09-03 1999-03-22 Guilford Pharmaceuticals Inc. Amino-substituted compounds, methods, and compositions for inhibiting parp activity
AU2012199A (en) * 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
US6066636A (en) 1998-06-30 2000-05-23 Schering Corporation Muscarinic antagonists
PL364045A1 (en) * 1999-09-13 2004-12-13 Boehringer Ingelheim Pharmaceuticals, Inc. Novel spiroheterocyclic compounds useful as reversible inhibitors of cysteine proteases
US6420364B1 (en) * 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
US6294554B1 (en) 1999-09-22 2001-09-25 Schering Corporation Muscarinic antagonists
PE20020276A1 (es) 2000-06-30 2002-04-06 Elan Pharm Inc COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER
CA2431952C (en) 2000-12-22 2010-03-09 Schering Corporation Muscarinic antagonists
AU2002306734A1 (en) 2001-03-15 2002-10-03 The Johns Hopkins University Inhibitors of plasmepsins
WO2003014075A2 (en) * 2001-08-03 2003-02-20 Schering Corporation Novel gamma secretase inhibitors
EP1434766B1 (en) 2001-10-10 2006-08-02 Schering Corporation Piperidine compounds as muscarinic antagonists
MY149978A (en) 2003-12-15 2013-11-15 Merck Sharp & Dohme Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
EP1756087B1 (en) * 2004-06-16 2009-10-07 Wyeth Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase
JP2008503460A (ja) * 2004-06-16 2008-02-07 ワイス β−セクレターゼのインヒビターとしてのジフェニルイミダゾピリミジンおよびイミダゾールアミン
US8436006B2 (en) 2004-08-06 2013-05-07 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
ATE482936T1 (de) 2004-08-06 2010-10-15 Janssen Pharmaceutica Nv Als b-sekretase (bace)-hemmer nützliche 2-amino- chinazolinderivate
EP1776350B1 (en) 2004-08-06 2013-01-23 Janssen Pharmaceutica NV NOVEL 2-AMINO-QUINAZOLINE DERIVATIVES USEFUL AS INHIBITORS OF ß-SECRETASE ( BACE )
US8114887B2 (en) 2004-10-13 2012-02-14 Merck, Sharp & Dohme Corp. Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
WO2006044492A2 (en) 2004-10-14 2006-04-27 Ingenious Targeting Laboratory, Inc. Methods for generating rat embryo-derived cell lines and genetic modification of rat genome
EP1802587A4 (en) 2004-10-15 2010-02-17 Astrazeneca Ab SUBSTITUTED AMINO BINDINGS AND THEIR APPLICATIONS
US20090062282A1 (en) * 2004-10-15 2009-03-05 Astrazeneca Ab Substituted Amino-Pyrimidones and Uses Thereof
MX2007008555A (es) 2005-01-14 2007-11-21 Wyeth Corp Amino-imidazolonas para la inhibicion de (-secretasa.
US7812013B2 (en) * 2005-06-14 2010-10-12 Schering Corporation Macrocyclic heterocyclic aspartyl protease inhibitors
AU2006259572A1 (en) * 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
US8110682B2 (en) * 2005-06-14 2012-02-07 Schering Corporation Preparation and use of compounds as aspartyl protease inhibitors
TW200738683A (en) * 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
JP2009500329A (ja) * 2005-06-30 2009-01-08 ワイス アミノ−５−（６員）ヘテロアリールイミダゾロン化合物およびβ−セレクターゼ調節のためのその使用
TW200730523A (en) * 2005-07-29 2007-08-16 Wyeth Corp Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation
CN101273018A (zh) * 2005-09-26 2008-09-24 惠氏公司 用于β分泌酶（BACE）抑制剂的氨基-5-[4-(二氟甲氧基)苯基]-5-苯基咪唑酮化合物
ES2537898T3 (es) 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
PT1966198E (pt) * 2005-10-25 2011-05-13 Janssen Pharmaceutica Nv Derivados de 2-amino-3,4-di-hidro-pirido[3,4-d]pirimidina ?teis como inibidores de beta-secretase (bace)
DE602006016314D1 (de) 2005-10-27 2010-09-30 Schering Corp Heterozyklische aspartyl-proteasehemmer
WO2007053506A1 (en) * 2005-10-31 2007-05-10 Schering Corporation Aspartyl protease inhibitors
TW200804290A (en) 2005-11-15 2008-01-16 Astrazeneca Ab Compounds and uses thereof
AR058381A1 (es) * 2005-12-19 2008-01-30 Astrazeneca Ab Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica
WO2007092854A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
WO2007092846A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-3,4-DIHYDRO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
WO2007092839A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. Macrocycle derivatives useful as inhibitors of beta-secretase (bace)
WO2007100536A1 (en) * 2006-02-24 2007-09-07 Wyeth DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE
EP2004630A4 (en) 2006-04-05 2010-05-19 Astrazeneca Ab 2-AMINOPYRIMIDIN-4-ONES AND THEIR USE FOR THE TREATMENT OR PREVENTION OF PATHOLOGIES RELATED TO PROTEIN A
KR20090015967A (ko) * 2006-06-12 2009-02-12 쉐링 코포레이션 헤테로사이클릭 아스파르틸 프로테아제 억제제
TW200808796A (en) * 2006-06-14 2008-02-16 Astrazeneca Ab New compounds III
US20080051420A1 (en) * 2006-06-14 2008-02-28 Astrazeneca Ab New Compounds 317
TW200815447A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds IV
TW200815443A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds I
TW200815449A (en) * 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds II
TW200815349A (en) * 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
TW200817406A (en) 2006-08-17 2008-04-16 Wyeth Corp Imidazole amines as inhibitors of β-secretase
WO2008063114A1 (en) 2006-11-20 2008-05-29 Astrazeneca Ab Amino- imidazolones and their use as medicament for treating cognitive impairment alzheimer disease, neurodegeneration and dementia
EP2061771A1 (en) 2006-12-12 2009-05-27 Schering Corporation Aspartyl protease inhibitors containing a tricyclic ring system
CA2672293A1 (en) 2006-12-12 2008-06-19 Schering Corporation Aspartyl protease inhibitors
TW200831484A (en) * 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
KR20100017255A (ko) 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
TW200902503A (en) * 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
TW200902499A (en) * 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
WO2009005471A1 (en) 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
WO2009005470A1 (en) 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
JP5450407B2 (ja) 2007-07-06 2014-03-26 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 置換アミノ−キナゾリノン、前記化合物を含む薬物、それらの使用及び製造方法
SI2233474T1 (sl) 2008-01-18 2015-11-30 Eisai R&D Management Co., Ltd. Kondenziran derivat aminodihidrotiazina
WO2009092566A1 (en) 2008-01-22 2009-07-30 Boehringer Ingelheim International Gmbh Substituted amino-benzimidazoles, medicaments comprising said compound, their use and their method of manufacture
CA2713998A1 (en) 2008-01-28 2009-08-06 Janssen Pharmaceutica N.V. 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of.beta.-secretase (bace)
BRPI0907061A2 (pt) 2008-01-29 2015-07-07 Janssen Pharmaceutica Nv Derivados de 2-aminoquinolina úteis como inibidores de beta-secretase (base)
CN101952260B (zh) * 2008-02-18 2013-02-13 弗·哈夫曼-拉罗切有限公司 4,5-二氢-*唑-2-基胺衍生物
CA2714058A1 (en) 2008-02-28 2009-09-03 Ivory D. Hills 2-aminoimidazole beta-secretase inhibitors for the treatment of alzheimer's disease
US8450331B2 (en) 2008-04-22 2013-05-28 Merck Sharp & Dohme Corp. Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
EP2305672B1 (en) 2008-06-13 2019-03-27 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY
WO2010013302A1 (ja) 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体
WO2010013794A1 (en) 2008-07-28 2010-02-04 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
ES2539859T3 (es) 2008-09-30 2015-07-06 Eisai R&D Management Co., Ltd. Nuevo derivado de aminodihidrotiazina condensado
CN102186841A (zh) 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
WO2010056195A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
US20100125081A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 574
EP2376083A4 (en) 2008-11-20 2012-06-20 Purdue Research Foundation QUINAZOLIN-BASED BACE-1 INHIBITORS AND METHODS OF USE

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TW200716643A (en) 2007-05-01
JP4896972B2 (ja) 2012-03-14
WO2006138265A2 (en) 2006-12-28
JP5454956B2 (ja) 2014-03-26
EP1896032A2 (en) 2008-03-12
EP2345411A1 (en) 2011-07-20
ES2436795T3 (es) 2014-01-07
NO20080186L (no) 2008-03-14
AU2006259573A1 (en) 2006-12-28
EP2345411B1 (en) 2013-10-02
CA2610828A1 (en) 2006-12-28
CN101394852A (zh) 2009-03-25
US9382242B2 (en) 2016-07-05
US8722708B2 (en) 2014-05-13
WO2006138265A3 (en) 2007-03-01
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ZA200710385B (en) 2008-11-26
US20080176868A1 (en) 2008-07-24
ECSP078004A (es) 2008-01-23
US20140206715A1 (en) 2014-07-24
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BRPI0612545A2 (pt) 2010-11-23
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