AR056862A1 - 1,2-etilendiaminas sustituidas, medicamentos que contienen a estos compuestos, su uso y procedimiento para su preparacion - Google Patents

1,2-etilendiaminas sustituidas, medicamentos que contienen a estos compuestos, su uso y procedimiento para su preparacion

Info

Publication number
AR056862A1
AR056862A1 ARP060101206A ARP060101206A AR056862A1 AR 056862 A1 AR056862 A1 AR 056862A1 AR P060101206 A ARP060101206 A AR P060101206A AR P060101206 A ARP060101206 A AR P060101206A AR 056862 A1 AR056862 A1 AR 056862A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkynyl
aryl
cycloalkyl
heterocyclyl
Prior art date
Application number
ARP060101206A
Other languages
English (en)
Inventor
Cornelia Dorner-Ciossek
Niklas Heine
Stefan Peters
Sandra Handschuh
Marcus Kostka
Christian Eickmeier
Technical Services Heineken
Klaus Klinder
Klaus Fuchs
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR056862A1 publication Critical patent/AR056862A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0821Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Son objeto de la presente 1,2-etilendiaminas sustituidas de la formula general (1), en donde los radicales R1 a R15, A, B, L, i, así como X1-X4 están definidos como eh la memoria descriptiva y las reivindicaciones, y su uso para el tratamiento de la enfermedad de Alzheimer (EA) y enfermedades similares. Reivindicacion 1: Compuestos de la formula general (1), en la que A significa arilo- o heteroarilo-, en donde el grupo A junto a los radicales L puede estar eventualmente sustituido con uno o varios átomos de fluor; L, en cada caso independientemente uno de otro, significa hidrogeno, fluor, cloro, bromo, yodo, hidroxi-, carboxi-, formilo-, ciano-, nitro-, F3C-, HF2C-, FH2C-, alquilo C1-6-, alquenilo C2-6-, alquinilo C2-6-, alquil C1-6-S- , alquil C1-6-S-alquilo C1-3-, cicloalquilo C3-7-, cicloalquenilo C3-7-, cicloalquil C3-7-alquilo C1-6-, cicloalquil C3-7-alquenilo C2-6-, cicloalquil C3-7-alquinilo C2-6-, cicloalquenil C3-7-alquilo C1-6-, cicloalquenil C3-7-alquenilo C2-6-, cicloalquenil C3-7-alquinilo C2-6-, arilo-, aril-alquilo C1-6-, aril-alquenilo C2-6-, aril-alquinilo C2-6-, heterociclilo-, heterociclil-alquilo C1-6-, heterociclil-alquenilo C2-6-, heterociclilalquinilo C2-6-, heteroarilo-, heteroaril-alquilo C1-6- , heteroarilalquenilo C2-6-, heteroaril-alquinilo C2-6-, R15-O-, R15-O-alquilo C1-3-, (R14)2N-, (R14)2N-CO-, R14-CO-(R14)N-, (R14)2N-CO-(R14)N-, R14-SO2-(R14)N-, (R14)2N-SO2- o R14-SO2-, en donde los grupos arriba mencionados pueden estar sustituidos, eventualmente de forma independiente uno de otro, con uno o varios radicales seleccionados del grupo consistente en fluor, cloro, bromo, yodo, hidroxi-, oxo-, carboxi-, formilo-, ciano-, nitro-, F3C-, HF2C-, FH2C- hidroxi-alquilo C1-6-, alquilo C1-3-, alcoxi C1-6-, (R14)2N-, (R14)2N-alquilo C1-3-, (R14)2N-CO- y HOSO2-; i significa 0, 1, 2 o 3; B significa un puente de alquileno C1-4, en donde en el caso de un puente de alquileno C3-4 el grupo -CH2 del puente de alquileno C3-4, el cual está unido al grupo A, puede estar reemplazado por -O-, y en donde el puente de alquileno C1-4 puede estar sustituido eventualmente con uno o varios radicales seleccionados del grupo fluor, cloro, bromo, yodo, hidroxi-, oxo-, carboxi-, ciano-, nitro-, F3C-, HF2C-, FH2C-, alquilo C1-4-, alquil C1-6-S-alquilo C1-3-, cicloalquilo C3-7, -cicloalquil C3-7-alquilo C1-3-, heterociclilo-, heterociclil-alquilo C1-3-, arilo-, aril-alquilo C1-3-, heteroarilo-, heteroaril-alquilo C1-3-, R15-O-, (R14)2N-SO2-, (R14)2N-; (R14)2N-alquilo C1-3-, (R14)2N-CO-, R14-SO2-, R14-CO-(R14)N-, R14-SO2(R14)N-, (R14)2N-SO2-, R14-CO- y en donde dos radicales alquilo C1-4, unidos al mismo átomo de carbono del puente de alquileno C1-4, pueden estar unidos entre sí con formacion de un grupo cicloalquilo C3-7, y en donde los radicales arriba mencionados y el grupo cicloalquilo C3-7 configurado a partir de los radicales alquilo C1-4, eventualmente de forma independiente uno de otro, pueden estar sustituidos con uno o varios radicales seleccionados del grupo consistente en fluor, cloro, bromo, yodo, hidroxi-, oxo-, carboxi-, formilo-, ciano-, nitro-, F3C-, HF2C-, FH2C-alquilo C1-3-, alcoxi C1-3-, R15-O-alquilo C1-3-, R14-CO(R14)N-, R14- SO2(R14)N-, (R14)2N-, (R14)2N-alquilo C1-3-, (R14)2N-CO-, (R14)2N-SO2- y HOSO2-; R1 significa hidrogeno, alquilo C1-6-, alquenilo C2-6-, alquinilo C2-6-, cicloalquilo C3-7-, cicloalquil C3-7-alquilo C1-6-, cicloalquil C3-7-alquenilo C2-6-, cicloalquil C3-7-alquinilo C2-6-, cicloalquenilo C3-7-, cicloalquenil C3-7-alquilo C1-6-, cicloalquenil C3-7-alquenilo C2-6-, cicloalquenil C3-7-alquinilo C2-6-, arilo-, aril-alquilo C1-6-, aril-alquenilo C2-6-, arilalquinilo C2-6-, heterociclilo-, heterociclil-alquilo C1-6-, heterociclil alquenilo C2-6-, heterociclil-alquinilo C2-6-, heteroarilo-, heteroarilalquilo C1-6-, heteroaril-alquenilo C2-6- o heteroaril-alquinilo C2-6-, en donde los radicales arriba mencionados pueden estar sustituidos, eventualmente de forma independiente uno de otro, con uno o varios radicales seleccionados del grupo consistente en fluor, cloro, bromo, yodo, hidroxi-, oxo-, carboxi-, formilo-, ciano-, nitro-, F3C-, HF2C-, FH2C-, alquilo C1-3-, alcoxi C1-3-, hidroxi-alquilo C1-6-, (R14)2N-, (R14)2N-alquilo C1-3-, (R14)2N-CO-(R14)2N-SO2-, R14-CO-(R14)N-, y HOSO2-; X1 significa nitrogeno o C(R10); X2, X3, X4, en cada caso independientemente uno de otro, significan nitrogeno o C(R11), con la condicion de que 0, 1, 2 o 3 de los grupos X1, X2, X3 y X4 puedan ser nitrogeno; R2 significa alquilo C1-6-, alquenilo C2-6-, alquinilo C2-6-, R15-O-alquilo C1-3-, alquil C1-6-S-alquilo C1-3-, cicloalquilo C3-7-, cicloalquil C3-7-alquinilo C2-6-, cicloalquenilo C3-7-, cicloalquenil C3-7-alquilo C1-6-, cicloalquenil C3-7-alquenilo C2-6-, cicloalquenil C3-7-alquinilo C2-6-, heterociclilo-, cicloalquil C3-7-alquilo C1-3-, heterociclil-alquilo C1-3-, cicloalquil C3-7-alquenilo C2-3-, heterociclil-alquenilo C2-3-, heterociclil-alquinilo C2-3-, arilo-, heteroarilo-, aril-alquilo C1-3-, heteroarilalquilo C1-3-, aril-alquenilo C2-3-, aril-alquinilo C2-3-, heteroarilalquenilo C2-3- o heteroaril-alquinilo C2-3-, en donde los radicales arriba mencionados, eventualmente de forma independiente uno de otro, pueden estar sustituidos con uno o varios radicales seleccionados del grupo consistente en fluor, cloro, bromo, yodo, F3C-, HF2C-, FH2C- hidroxi-, oxo-, carboxi-, formilo-, ciano- , nitro-, (R14)2N-, (R14)2N-alquilo C1-3, HOSO2-, alquilo C1-3, alquil C1-6-S-alquilo C1-3, (R14)2N-SO2-, R14-CO(R14)N-, R14-SO2(R14)N-, (R14)2N-CO-, R15-O- y R15-O-alquilo C1-3-; R3, R4, en cada caso independientemente uno de otro, significan hidrogeno, alquilo C1-4-, fluor, F3C-, HF2C- o FH2C-; R5, R7, en cada caso independientemente uno de otro, significa hidrogeno, alquilo C1-6-, alquenilo C2-6-, alquinilo C2-6-, cicloalquilo C3-7-, heterociclilo-, cicloalquil C3-7-alquilo C1-3-, cicloalquil C3-7-alquinilo C2-6-, heterociclil-alquilo C1-3-, cicloalquil C3-7-alquenilo C2-4-, heterociclilalquenilo C2-4-, heterociclil-alquinilo C2-4-, cicloalquenilo C3-7-, cicloalquenil C3-7-alquilo C1-6-, cicloalquenil C3-7-alquenilo C2-6-, cicloalquenil C3-7-alquinilo C2-6-, arilo-, heteroarilo-, aril-alquilo heteroaril-alquilo C1-3-, aril-alquenilo C2-3-, heteroaril-alquenilo C2-3-, aril-alquinilo C2-3- o heteroaril-alquinilo C2-3-, en donde los radicales arriba mencionados, eventualmente de forma independiente uno de otro, pueden estar sustituidos con uno o varios radicales seleccionados del grupo consistente en fluor, cloro, bromo, yodo, hidroxi-, oxo-, carboxi-, formilo-, ciano, nitro-, alquilo C1-3-, R15-O-, alquil C1-3-S-, arilo-, heteroarilo-, heteroaril-alquilo C1-3-, aril-alquilo C1-6-, R14-CO-(R14)N-, R14-SO2-(R14)N-, (R14)2N-SO2-, (R14)2N-, (R14)2N-alquilo C1-3, (R14)2N-CO- y HOSO2-; R6, R9 significan, en cada caso independientemente uno de otro, hidrogeno, alquilo C1-6-, alcoxi C1-6-alquilo C1-3-, cicloalquilo C3-7-, cicloalquil C3-7-alquilo C1-3-, alquenilo C2-6-, heterociclil-alquilo C1-3-, heteroarilo-, heteroaril-alquilo C1-3, o alquinilo C2-6-, en donde los radicales arriba mencionados pueden estar sustituidos, eventualmente de forma independiente uno de otro, con uno o varios radicales seleccionados del grupo consistente en fluor, cloro, bromo, yodo, ciano-, alquilo C1-3-, alcoxi C1-6-; R8 significa hidrogeno, alquilo C1-6-, alquenilo C2-6-, alquinilo C2-6-, cicloalquilo C3-7-, cicloalquil C3-7-alquilo C1-3-, cicloalquil C3-7-alquenilo C2-4-, cicloalquil C3-7-alquinilo C2-4-, cicloalquenilo C3-7-, cicloalquenil C-3-7-alquilo C1-6, cicloalquenil C3-7-alquenilo C2-6, cicloalquenil C3-7-alquinilo-C2-6-, heterociclilo-, heterociclil-alquilo C1-3-, heterociclil-alquenilo C2-4-, heterociclil-alquinilo C2-4-, arilo-, aril-alquilo C1-3-, aril-alquenilo C2-4, - aril-alquinilo C2-4-, heteroarilo-, heteroaril-alquilo C1- 3-, heteroarilalquenilo C2-4- o heteroaril-alquinilo C2-4-, en donde los radicales arriba mencionados, eventualmente de forma independiente uno de otro, pueden estar sustituidos con uno o varios radicales seleccionados del grupo consistente en fluor, cloro, bromo, yodo, hidroxi-, oxo-, carboxi-, formilo-, ciano-, nitro-, alquilo C1-3-, heterociclilo-, heterociclil-alquilo C1-3-, R15-O-, R15-O-alquilo C1-3-, R15-S-, R15-S-alquilo C1-3-, arilo-, heteroarilo-, heteroarilalquilo C1-3-, aril- alquilo C1-6-, (R14)2N-, (R14)2N-alquilo C1-3-, (R14)2N-CO-, (R14)2N-CO-N(R14)-, (R14)2N-SO2- y HOSO2-; R10 significa hidrogeno, fluor, cloro, bromo, yodo, ciano-, alquilo C1-6-, alquenilo C2-6-, alquinilo C2-6-, cicloalquilo C3-7-, cicloalquil C3-7- alquilo C1-6-, cicloalquil C3-7-alquinilo C2-6-, heterociclilo-, heterociclil-alquilo C1-6-, heterociclil-alquenilo C2-6-, heterociclil-alquinilo C2-6-, cicloalquil C3-7-alquenilo C2-6-, heterociclil-alquenilo C2-4-, cicloalquenilo C3-7-, cicloalquenil C3-7-alquilo C1-6-, cicloalquenil C3-7-alquenilo C2-6, cicloalquenil C3-7-alquinilo C2-6-, arilo:, aril-alquilo C1-6-, heteroarilo-, heteroaril-alquilo C1-6-, aril-alquenilo C2-6-, heteroaril-alquenilo C2-6-, aril-alquinilo C2-6- o heteroaril-alquinilo C2-6-, R15-O-, R15-O-alquilo C1-3-, R12-SO2-(R13)N- o R12-CO-(R13)N-, en donde los grupos arriba mencionados pueden estar sustituidos, eventualmente de forma independiente uno de otro, con uno o varios radicales seleccionados del grupo consistente en fluor, cloro, bromo, yodo, hidroxi-, oxo-, carboxi-, formilo-, ciano-, nitro-, alquilo C1-6-, alquenilo C2-6, alquinilo C2-6, alquil C1-6-S-, alquil C1-6-S-alquilo C1-3-, cicloalquilo C3-7-, cicloalquil C3-7-alquilo C1-6-, arilo-, aril-alquilo C1-6-, heterociclilo-, heterociclil-alquilo C1-6-, heteroarilo-, heteroaril-alquilo C1-6-, R15-O-, R15-O-CO-, R15-CO-, R15-O-CO-(R14)N-, (R14)2N-CO-O-, R15-O-alquilo C1-3-, (R14)2N-, (R14)2N-CO-, R14-CO-(R14)N-, (R14)2N-CO- (R14)N-, (R14)2N-SO2-, (R14)2N-SO2-(R14)N-, R14SO2, F3C-, HF2C-, FH2C, F3C-O-, HF2CO-, FH2C-O y R14-SO2-(R14)N-; R11, en cada independientemente uno de otro, signifi
ARP060101206A 2005-03-30 2006-03-29 1,2-etilendiaminas sustituidas, medicamentos que contienen a estos compuestos, su uso y procedimiento para su preparacion AR056862A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP05006939 2005-03-30

Publications (1)

Publication Number Publication Date
AR056862A1 true AR056862A1 (es) 2007-10-31

Family

ID=36545049

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060101206A AR056862A1 (es) 2005-03-30 2006-03-29 1,2-etilendiaminas sustituidas, medicamentos que contienen a estos compuestos, su uso y procedimiento para su preparacion

Country Status (7)

Country Link
US (3) US7713961B2 (es)
EP (1) EP1866034A1 (es)
JP (1) JP2008534541A (es)
AR (1) AR056862A1 (es)
CA (1) CA2603404A1 (es)
TW (1) TW200716152A (es)
WO (1) WO2006103038A1 (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2603404A1 (en) * 2005-03-30 2006-10-05 Boehringer Ingelheim International Gmbh Substituted 1,2-ethylendiamines, medicaments comprising said compound; their use and their method of manufacture
CA2617294A1 (en) * 2005-08-03 2007-02-08 Boehringer Ingelheim International Gmbh Substituted ethane-1,2-diamines for the treatment of alzheimer's disease ii
WO2007017510A2 (de) * 2005-08-11 2007-02-15 Boehringer Ingelheim International Gmbh Isophthalsäurediamide zur behandlung der alzheimer erkrankung
CA2618019A1 (en) * 2005-08-11 2007-02-15 Boehringer Ingelheim International Gmbh Compounds for the treatment of alzheimer's disease
CA2618481A1 (en) * 2005-08-11 2007-02-15 Boehringer Ingelheim International Gmbh Compounds for treating alzheimer's disease
CA2618013A1 (en) * 2005-08-11 2007-02-15 Boehringer Ingelheim International Gmbh Beta-secretase inhibitors for use in the treatment of alzheimer's disease
EP2349308A4 (en) 2008-10-10 2012-09-12 Purdue Research Foundation COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
WO2010059953A1 (en) 2008-11-20 2010-05-27 Purdue Research Foundation Quinazoline inhibitors of bace 1 and methods of using
US8859590B2 (en) 2008-12-05 2014-10-14 Purdue Research Foundation Inhibitors of BACE1 and methods for treating Alzheimer's disease
WO2011044057A1 (en) * 2009-10-05 2011-04-14 Comentis, Inc. Sulfonamido pyrrolidine compounds which inhibit beta-secretase activity and methods of use thereof
US20140066488A1 (en) * 2012-08-30 2014-03-06 Purdue Research Foundation Inhibitors of Memapsin 2 Cleavage for the Treatment of Alzheimer's Disease

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ184194A3 (en) 1993-08-09 1995-03-15 Lilly Co Eli Aspartylprotease inhibitor and method of identifying thereof
US7087399B1 (en) 1999-05-13 2006-08-08 Scios, Inc. β-secretase and modulation of β-secretase activity
US6545127B1 (en) 1999-06-28 2003-04-08 Oklahoma Medical Research Foundation Catalytically active recombinant memapsin and methods of use thereof
US20050130941A1 (en) * 2001-06-08 2005-06-16 Heinrich Schostarez Methods of treating alzheimer's disease
EP1453516A2 (de) 2001-10-17 2004-09-08 Boehringer Ingelheim Pharma GmbH & Co.KG 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren
WO2003057721A2 (en) * 2002-01-04 2003-07-17 Elan Pharmaceuticals, Inc. Substituted amino carboxamides for the treatment of alzheimer's disease
JP2006501282A (ja) * 2002-09-27 2006-01-12 イーラン ファーマスーティカルズ、インコーポレイテッド アルツハイマー病治療のための化合物
EP1562897B1 (en) * 2002-11-12 2009-09-16 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer s disease
US20050090449A1 (en) 2003-05-13 2005-04-28 Boehringer Ingelheim International Gmbh Novel statine derivatives for the treatment of Alzheimer's disease
EP1641748B1 (en) * 2003-06-30 2013-08-28 Merck Sharp & Dohme Corp. N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer s disease
WO2005110422A2 (en) 2004-05-19 2005-11-24 Boehringer Ingelheim International Gmbh Treatment of diseases associated with altered level of amyloid beta peptides
WO2005113582A1 (en) 2004-05-22 2005-12-01 Boehringer Ingelheim International Gmbh Substituted ethane-1,2-diamines for the treatment of alzheimer's disease
WO2006050862A1 (en) 2004-11-10 2006-05-18 Boehringer Ingelheim International Gmbh Statine derivatives for the treatment of alzheimer's disease
WO2006050861A2 (en) 2004-11-10 2006-05-18 Boehringer Ingelheim International Gmbh Statine derivatives for the treatment of alzheimer's disease
CA2603404A1 (en) * 2005-03-30 2006-10-05 Boehringer Ingelheim International Gmbh Substituted 1,2-ethylendiamines, medicaments comprising said compound; their use and their method of manufacture
CA2617294A1 (en) 2005-08-03 2007-02-08 Boehringer Ingelheim International Gmbh Substituted ethane-1,2-diamines for the treatment of alzheimer's disease ii
CA2618019A1 (en) 2005-08-11 2007-02-15 Boehringer Ingelheim International Gmbh Compounds for the treatment of alzheimer's disease

Also Published As

Publication number Publication date
US20060223759A1 (en) 2006-10-05
WO2006103038A1 (en) 2006-10-05
EP1866034A1 (en) 2007-12-19
JP2008534541A (ja) 2008-08-28
CA2603404A1 (en) 2006-10-05
US7713961B2 (en) 2010-05-11
US20090325940A1 (en) 2009-12-31
US20100204160A1 (en) 2010-08-12
TW200716152A (en) 2007-05-01

Similar Documents

Publication Publication Date Title
AR056862A1 (es) 1,2-etilendiaminas sustituidas, medicamentos que contienen a estos compuestos, su uso y procedimiento para su preparacion
UY33961A (es) Compuestos de bis(fuoroalquil)-1,4-benziodiazepinona
EA200700909A1 (ru) Азаиндолкарбоксамиды
CO6290658A2 (es) Derivados de azetidina y ciclobutano como inhibidores de jack
HN2012000889A (es) Derivados de la cromenona con actividad anti-tumoral
AR056560A1 (es) Pirrolopiridinonas como moduladores cb1
ECSP10010209A (es) Agonistas novedosos de los receptores de glucocorticoides
EA201171098A1 (ru) 8-замещенные хинолины и родственные аналоги в качестве модуляторов сиртуина
AR063015A1 (es) Derivados de quinazolinona 5-sustituida y composiciones que los comprenden y metodos para utilizarlos en el tratamiento del cancer
PA8604201A1 (es) Derivados de 2-amino-piridina utiles para el tratamiento de enfermedades
SV2006002098A (es) Compuestos de morfolina sustituida para el tratamiento de trastornos del sistema nervioso central ref. pc32250a
BRPI0515546A (pt) compostos para inflamação e usos imune-relacionados
AR051326A1 (es) Pirazolobenzodiazepinas disustituidas
AR077413A1 (es) Derivados piridin-4-ilo
CO6321241A2 (es) Derivados de 1,3,4- tiadiazol espiro condensados para la inhibicion de la actividad de quinesina (ksp)
UY28150A1 (es) Agentes terapeuticos
CY1111733T1 (el) Παραγωγα 2-(1η-ινδολυλοσουλφανυλ)-βενζυλαμινης ως ssri
PA8627001A1 (es) Compuestos para el tratamiento de enfermedades
AR090712A1 (es) Agentes para tratar trastornos que implican la modulacion de receptores de rianodina
SE0502254L (sv) Nya disubstituerade fenyl-piperidiner som modulatorer för dopaminneurotransmission
PA8779101A1 (es) "compuestos tricíclicos como inhibidores de metaloproteinasas matriciales"
AR078142A1 (es) Compuestos inhibidores heteroarilicos biciclicos de pde4, las composiciones farmaceuticas que los contienen y el uso de los mismos para la preparacion de medicamentos.
EA201000362A1 (ru) Производные 1,3-дигидроизоиндола
CR8636A (es) Compuestos utiles para el tratamiento de enfermedades
SE0401465D0 (sv) New substituted piperdines as modulators of dopamine neurotransmission

Legal Events

Date Code Title Description
FA Abandonment or withdrawal