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ES2284970T3 - Compuestos amina 1,2- y 1,3-diol y su utilizacion para el tratamiento de alzheimer. - Google Patents

Compuestos amina 1,2- y 1,3-diol y su utilizacion para el tratamiento de alzheimer. Download PDF

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Publication number
ES2284970T3
ES2284970T3 ES02797133T ES02797133T ES2284970T3 ES 2284970 T3 ES2284970 T3 ES 2284970T3 ES 02797133 T ES02797133 T ES 02797133T ES 02797133 T ES02797133 T ES 02797133T ES 2284970 T3 ES2284970 T3 ES 2284970T3
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ES
Spain
Prior art keywords
sub
treatment
alzheimer
useful
compounds
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES02797133T
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English (en)
Inventor
Arthur Glenn Romero
Heinrich Schostarez
Christina M Roels
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Elan Pharmaceuticals LLC
Pharmacia and Upjohn Co LLC
Original Assignee
Elan Pharmaceuticals LLC
Pharmacia and Upjohn Co LLC
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
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Application filed by Elan Pharmaceuticals LLC, Pharmacia and Upjohn Co LLC filed Critical Elan Pharmaceuticals LLC
Application granted granted Critical
Publication of ES2284970T3 publication Critical patent/ES2284970T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/67—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/68—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/73—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/77—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/78—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/12—Oxygen or sulfur atoms
    • 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
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/10—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/04—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D309/06—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/10—Oxygen atoms
    • C07D309/12—Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/16—Radicals substituted by singly bound hetero atoms other than halogen by oxygen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Furan Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrane Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

Compuesto de fórmula I (Ver fórmula) o una sal farmacéuticamente aceptable del mismo, en el que RN es RN - 1-XN- en el que XN es -CO-, en el que RN - 1 es RN - arilo, en el que RN - arilo es fenilo; opcionalmente sustituido con uno, dos o tres de los siguientes sustituyentes que pueden ser el mismo o diferentes y son: (1) alquilo C1-C6, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste en alquilo C1-C3, -F, -Cl, -Br, -I, -OH, -SH, -C N, -CF3, alcoxi C1-C3, y -NR1 - aR1 - b, en el que R1 - a y R1 - b en cada caso son independientemente H o alquilo C1-C6, (2) -OH, (3) -NO2, (4) -F, -Cl, -Br, -I, (5) -CO2H, (6) -C=N, (7) -(CH2)0 - 4-CO-NRN - 2RN - 3, en el que RN - 2 y RN - 3 son el mismo o diferente y se seleccionan del grupo que consiste en: (a) -H, (b) -alquilo C1-C8 opcionalmente sustituido con un sustituyente seleccionado del grupo que consiste en: (i) -OH, y (ii) -NH2, (c) - alquilo C1-C6 opcionalmente sustituido con 1, 2 ó 3 grupos que sonindependientemente -F, -Cl, -Br o -I, (d) - cicloalquilo C3-C7, (e) -(alquilo C1-C2)-Cicloalquilo C3-C7, (f) -(alquilo C1-C6)-O-(alquilo C1-C3), (g) - alquenilo C2-C6 con 1 ó 2 dobles enlaces, (h) - alquinilo C2-C6 con 1 ó 2 triples enlaces, (i) - cadena alquílica C1-C6 con un doble enlace y un triple enlace, (j) -R1 - arilo, en el que R1 - arilo en cada caso es independientemente fenilo, naftilo, indanilo, indenilo, dihidronaftilo, o tetralinilo, cada uno de los cuales está opcionalmente sustituido con 1, 2, 3 ó 4 grupos.
ES02797133T 2001-11-19 2002-11-19 Compuestos amina 1,2- y 1,3-diol y su utilizacion para el tratamiento de alzheimer. Expired - Lifetime ES2284970T3 (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US33308101P 2001-11-19 2001-11-19
US333081P 2001-11-19
US33400001P 2001-11-28 2001-11-28
US334000P 2001-11-28
US36275202P 2002-03-08 2002-03-08
US362752P 2002-03-08

Publications (1)

Publication Number Publication Date
ES2284970T3 true ES2284970T3 (es) 2007-11-16

Family

ID=27406892

Family Applications (1)

Application Number Title Priority Date Filing Date
ES02797133T Expired - Lifetime ES2284970T3 (es) 2001-11-19 2002-11-19 Compuestos amina 1,2- y 1,3-diol y su utilizacion para el tratamiento de alzheimer.

Country Status (11)

Country Link
US (1) US7388118B2 (es)
EP (1) EP1453792B1 (es)
JP (1) JP2005536448A (es)
AT (1) ATE359995T1 (es)
AU (1) AU2002362008A1 (es)
BR (1) BR0214293A (es)
CA (1) CA2467798A1 (es)
DE (1) DE60219680T2 (es)
ES (1) ES2284970T3 (es)
MX (1) MXPA04004771A (es)
WO (1) WO2003043975A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7291620B2 (en) 2003-06-30 2007-11-06 Merck + Co., Inc. N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
ITPD20040151A1 (it) * 2004-06-15 2004-09-15 Univ Degli Studi Trieste Inibitori peptidomimetici di proteasi retrovirali e loro uso come antivirali
WO2010107384A1 (en) * 2009-03-19 2010-09-23 Medivir Ab Aspartyl protease inhibitors
AU2015362790A1 (en) 2014-12-16 2017-07-20 Axovant Sciences Gmbh Geminal substituted quinuclidine amide compounds as agonists of alpha-7 nicotinic acetylcholine receptors
AU2016274694A1 (en) 2015-06-10 2018-01-18 Axovant Sciences Gmbh Aminobenzisoxazole compounds as agonists of A7-nicotinic acetylcholine receptors
WO2017027600A1 (en) 2015-08-12 2017-02-16 Forum Pharmaceuticals, Inc. GEMINAL SUBSTITUTED AMINOBENZISOXAZOLE COMPOUNDS AS AGONISTS OF α7-NICOTINIC ACETYLCHOLINE RECEPTORS

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4864017A (en) * 1986-09-05 1989-09-05 The Upjohn Company Novel renin inhibiting peptides having a dihyroxyethylene isostere transition state insert
ES2275675T3 (es) * 2000-03-23 2007-06-16 Elan Pharmaceuticals, Inc. Compuestos y metodos para tratar la enfermedad de alzheimer.
BR0111980A (pt) * 2000-06-30 2003-05-06 Elan Pharm Inc Amina substituìda, composto protegido, métodos para tratar um paciente que tenha ou para prevenir que um paciente contraia uma doença ou condição, para inibir a atividade da beta-secretase, para inibir a clivagem da proteìna precursora de amilóide (app), para inibir a produção do peptìdeo beta amilóide (a beta) em uma célula, para inibir a produção de placa beta0amilóide em um animal, e para tratar ou prevenir uma doença compreendendo depósitos de beta-amilóide no cérebro, composição método para produzir um complexo de beta-secretase, conjunto, e, uso de amina substituìda
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
US6846813B2 (en) * 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
AU2002315131A1 (en) * 2001-06-13 2002-12-23 Elan Pharmaceuticals, Inc. Aminediols as agents for the treatment of alzheimer's disease

Also Published As

Publication number Publication date
ATE359995T1 (de) 2007-05-15
CA2467798A1 (en) 2003-05-30
EP1453792A1 (en) 2004-09-08
DE60219680D1 (de) 2007-05-31
MXPA04004771A (es) 2004-07-30
AU2002362008A1 (en) 2003-06-10
DE60219680T2 (de) 2007-12-27
EP1453792B1 (en) 2007-04-18
BR0214293A (pt) 2005-04-19
US20040039064A1 (en) 2004-02-26
US7388118B2 (en) 2008-06-17
JP2005536448A (ja) 2005-12-02
WO2003043975A1 (en) 2003-05-30

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