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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sub
treatment
alzheimer
useful
compounds
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Expired - Lifetime
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ES02797133T
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Inventor
Arthur Glenn Romero
Heinrich Schostarez
Christina M Roels
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Elan Pharmaceuticals LLC
Pharmacia and Upjohn Co LLC
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Elan Pharmaceuticals LLC
Pharmacia and Upjohn Co LLC
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/64Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/67Carboxylic 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
    • C07C233/68Carboxylic 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
    • C07C233/73Carboxylic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/64Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/77Carboxylic 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
    • C07C233/78Carboxylic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/08Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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
    • C07D207/12Oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/10Heterocyclic 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
    • C07D211/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04Heterocyclic 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
    • C07D307/10Heterocyclic 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
    • C07D307/12Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic 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
    • C07D309/04Heterocyclic 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
    • C07D309/06Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic 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
    • C07D309/08Heterocyclic 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
    • C07D309/10Oxygen atoms
    • C07D309/12Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic 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
    • C07D333/06Heterocyclic 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
    • C07D333/14Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/16Radicals substituted by singly bound hetero atoms other than halogen by oxygen atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (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
CN100430377C (zh) * 2003-06-30 2008-11-05 麦克公司 用于治疗阿尔茨海默病的N-烷基苯基甲酰胺β分泌酶抑制剂
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
JP6612874B2 (ja) 2014-12-16 2019-11-27 アクソファント サイエンシーズ ゲーエムベーハー α7−ニコチン性アセチルコリン受容体のアゴニストとしてのジェミナル置換キヌクリジンアミド化合物
CA2988968A1 (en) 2015-06-10 2016-12-15 Forum Pharmaceuticals, Inc. Aminobenzisoxazole compounds as agonists of a7-nicotinic acetylcholine receptors
EP3334740A4 (en) 2015-08-12 2019-02-06 Axovant Sciences GmbH GEMINAL SUBSTITUTED AMINOBENZISOXAZOLE COMPOUNDS AS AGONISTS OF ALPHA 7-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
ATE343562T1 (de) * 2000-03-23 2006-11-15 Elan Pharm Inc Verbindungen und verfahren zur behandlung der alzheimerschen krankheit
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
DE60112942T2 (de) * 2000-06-30 2006-06-22 Elan Pharmaceuticals, Inc., South San Francisco Verbindungen zur behandlung der alzheimerischen krankheit
US6846813B2 (en) * 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
CA2450205A1 (en) * 2001-06-13 2002-12-19 Elan Pharmaceuticals, Inc. Aminediols for the treatment of alzheimer's disease

Also Published As

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

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