[go: up one dir, main page]

ES2248356T3 - Compuestos para tratar la enfermedad de alzheimer. - Google Patents

Compuestos para tratar la enfermedad de alzheimer.

Info

Publication number
ES2248356T3
ES2248356T3 ES01950719T ES01950719T ES2248356T3 ES 2248356 T3 ES2248356 T3 ES 2248356T3 ES 01950719 T ES01950719 T ES 01950719T ES 01950719 T ES01950719 T ES 01950719T ES 2248356 T3 ES2248356 T3 ES 2248356T3
Authority
ES
Spain
Prior art keywords
disease
compounds
treat alzheimer
alzheimer
treat
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
ES01950719T
Other languages
English (en)
Inventor
Lawrence Y. Fang
Roy Hom
Varghese John
Michel Maillard
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
Original Assignee
Elan Pharmaceuticals 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
Publication date
Application filed by Elan Pharmaceuticals LLC filed Critical Elan Pharmaceuticals LLC
Application granted granted Critical
Publication of ES2248356T3 publication Critical patent/ES2248356T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/22—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
    • C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/84—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C239/00—Compounds containing nitrogen-to-halogen bonds; Hydroxylamino compounds or ethers or esters thereof
    • C07C239/08—Hydroxylamino compounds or their ethers or esters
    • C07C239/20—Hydroxylamino compounds or their ethers or esters having oxygen atoms of hydroxylamino groups etherified
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C243/00—Compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
    • C07C243/10—Hydrazines
    • C07C243/22—Hydrazines having nitrogen atoms of hydrazine groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C243/00—Compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
    • C07C243/24—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids
    • C07C243/26—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C243/28—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of a saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/18—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by doubly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
    • C07C275/20—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C275/24—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C311/05—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
    • C07C311/13—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen 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
    • C07D211/36—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 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/04—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/36—Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
    • 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
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/52—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D333/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (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)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epoxy Compounds (AREA)

Abstract

Una amina sustituida de **fórmula**, en la que R1 es -CH2-fenilo, en el que el fenilo está opcionalmente sustituido con uno, dos, tres o cuatro de los siguientes sustituyentes sobre el anillo fenílico: (A) 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, -CN, -CF3, alcoxi C1-C3, y -NR1-aR1-b, en el que R1-a y R1-b son -H o alquilo C1-C6, (B) alquenilo C2-C6 con uno o dos dobles enlaces, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste en -F, -Cl, -OH, -SH, -CN, -CF3, alcoxi C1-C3, y -NR1- aR1-b, en el que R1-a y R1-b son -H o alquilo C1-C6, (C) alquinilo C2-C6 con uno o dos triples enlaces, opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste en -F, -Cl, -OH, -SH, -CN, -CF3, alcoxi C1-C3, y NR1- aR1-b, en el que R1-a y R1-b son -H o alquilo C1-C6; o sus sales farmacéuticamente aceptables.
ES01950719T 2000-06-30 2001-06-29 Compuestos para tratar la enfermedad de alzheimer. Expired - Lifetime ES2248356T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US21532300P 2000-06-30 2000-06-30
US215323P 2000-06-30

Publications (1)

Publication Number Publication Date
ES2248356T3 true ES2248356T3 (es) 2006-03-16

Family

ID=22802522

Family Applications (2)

Application Number Title Priority Date Filing Date
ES01952352T Expired - Lifetime ES2252257T3 (es) 2000-06-30 2001-06-29 Compuestos para tratar la enfermedad de alzheimer.
ES01950719T Expired - Lifetime ES2248356T3 (es) 2000-06-30 2001-06-29 Compuestos para tratar la enfermedad de alzheimer.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES01952352T Expired - Lifetime ES2252257T3 (es) 2000-06-30 2001-06-29 Compuestos para tratar la enfermedad de alzheimer.

Country Status (15)

Country Link
US (2) US7034182B2 (es)
EP (2) EP1299349B1 (es)
JP (2) JP2004502665A (es)
KR (1) KR20030058959A (es)
CN (1) CN1217920C (es)
AT (2) ATE302751T1 (es)
AU (3) AU2001273113A1 (es)
BR (1) BR0111980A (es)
CA (2) CA2410680A1 (es)
DE (2) DE60112942T2 (es)
ES (2) ES2252257T3 (es)
MX (1) MXPA02012560A (es)
NZ (1) NZ523005A (es)
WO (3) WO2002002505A2 (es)
ZA (2) ZA200209991B (es)

Families Citing this family (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2252257T3 (es) 2000-06-30 2006-05-16 Elan Pharmaceuticals, Inc. Compuestos para tratar la enfermedad de alzheimer.
US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
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
AU2001281250A1 (en) * 2000-08-11 2002-02-25 The Brigham And Women's Hospital, Inc. (hydroxyethyl)ureas as inhibitors of alzheimer's beta-amyloid production
AR035960A1 (es) 2001-04-23 2004-07-28 Elan Pharm Inc Epoxidos sustituidos y procesos para prepararlos
BR0209985A (pt) * 2001-05-22 2004-06-29 Elan Pharm Inc Composto e método para o tratamento de um paciente
CA2448834A1 (en) 2001-06-01 2002-12-12 Elan Pharmaceuticals, Inc. Hydroxy alkyl amine derivatives as beta-secretase inhibitors and their use for the treatment of alzheimer's disease and similar diseases
CA2452039A1 (en) 2001-06-27 2003-01-09 Elan Pharmaceuticals, Inc. Beta-hydroxyamine derivatives useful in treatment of alzheimer's disease
MXPA04001980A (es) * 2001-08-28 2005-02-17 Pharmacia & Up John Company Metodos de tratamiento de la enfermedad de alzheimer usando derivados de quinaldoil.amina de hidrocarburos substituidos con oxo e hidroxi.
AR039555A1 (es) 2001-11-08 2005-02-23 Upjohn Co Derivados n,n'-sustituidos de 1,3-diamino-2-hidroxipropano
ATE359995T1 (de) * 2001-11-19 2007-05-15 Elan Pharm Inc Amin-1,2- und -1,3-diolverbindungen und deren verwendung zur behandlung von alzheimer-krankheit
US20050159460A1 (en) * 2001-12-04 2005-07-21 Elan Pharmaceuticals Peptide isosteres containing a heterocycle useful in the treatment of alzheimer's disease
CA2469622A1 (en) * 2001-12-06 2003-06-19 Elan Pharmaceuticals, Inc. Substituted hydroxyethylamines
JP4354180B2 (ja) * 2001-12-26 2009-10-28 武田薬品工業株式会社 軽度認知障害治療剤
US7115652B2 (en) 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
EP1515944A1 (en) 2002-06-17 2005-03-23 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
US7459476B2 (en) 2002-06-27 2008-12-02 Elan Pharmaceuticals, Inc. Methods for treating Alzheimer's disease using hydroxyethylene compounds containing a heterocyclic amide bond isostere
US7557137B2 (en) * 2002-08-05 2009-07-07 Bristol-Myers Squibb Company Gamma-lactams as beta-secretase inhibitors
US20060160079A1 (en) * 2002-08-07 2006-07-20 Lane Roger M Methods for the treatment of dementia based on apo e genotype
WO2004014843A1 (ja) * 2002-08-09 2004-02-19 Takeda Chemical Industries, Ltd. 置換アミノ化合物およびその用途
BR0314071A (pt) * 2002-09-06 2005-07-05 Pharmacia & Upjohn Co Llc Derivados de pró-droga de 1,3-diamino-2-hidroxipropano
UY27967A1 (es) * 2002-09-10 2004-05-31 Pfizer Acetil 2-hindroxi-1,3-diaminoalcanos
CA2498269A1 (en) * 2002-09-10 2004-03-25 Pharmacia & Upjohn Company Llc Substituted aminoethers for the treatment of alzheimer's disease
ATE443043T1 (de) 2002-11-12 2009-10-15 Merck & Co Inc Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer
BR0316629A (pt) * 2002-11-27 2005-10-11 Elan Pharm Inc Uréias e carbamatos substituìdos
GB0228410D0 (en) 2002-12-05 2003-01-08 Glaxo Group Ltd Novel Compounds
US7521481B2 (en) 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
GB0305918D0 (en) * 2003-03-14 2003-04-23 Glaxo Group Ltd Novel compounds
PE20050420A1 (es) * 2003-04-21 2005-06-13 Elan Pharm Inc Fenacilo 2-hidroxi-3-diaminoalcanos
TW200512195A (en) * 2003-04-21 2005-04-01 Elan Pharm Inc Benzamide 2-hydroxy-3-diaminoalkanes
GB0309221D0 (en) * 2003-04-23 2003-06-04 Glaxo Group Ltd Novel compounds
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
TW200524910A (en) * 2003-08-08 2005-08-01 Schering Corp Cyclic amine BACE-1 inhibitors having a heterocyclic substituent
TW200519084A (en) 2003-08-08 2005-06-16 Schering Corp Cyclic amine bace-1 inhibitors having a benzamide substituent
GB0328900D0 (en) * 2003-12-12 2004-01-14 Glaxo Group Ltd Novel compounds
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
FR2866647B1 (fr) * 2004-02-20 2006-10-27 Servier Lab Nouveaux derives azabicycliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US7544717B2 (en) * 2004-03-25 2009-06-09 Elan Pharmaceuticals, Inc. 2-amino- and 2-thio- substituted 1,3-diaminopropanes
AR049726A1 (es) 2004-07-22 2006-08-30 Schering Corp Amidas sustituidas inhibidoras de beta secretasa
US7652003B2 (en) 2004-07-28 2010-01-26 Schering-Plough Corporation Macrocyclic β-secretase inhibitors
US7361789B1 (en) 2004-07-28 2008-04-22 Amgen Inc. Dihydronaphthalene compounds, compositions, uses thereof, and methods for synthesis
EP1797052A1 (en) * 2004-09-17 2007-06-20 Comentis, Inc. Bicyclic compounds which inhibit beta-secretase activity and methods of use thereof
JP2008513433A (ja) * 2004-09-21 2008-05-01 ファイザー・プロダクツ・インク 中枢神経系の症状の治療において有用なｎ−エチルヒドロキシエチルアミン
WO2006032999A1 (en) 2004-09-21 2006-03-30 Pfizer Products Inc. N-methyl hydroxyethylamine useful in treating cns conditions
US7745470B2 (en) 2005-03-10 2010-06-29 Bristol-Myers Squibb Company Isophthalates as beta-secretase inhibitors
GB0506562D0 (en) * 2005-03-31 2005-05-04 Glaxo Group Ltd Novel compounds
AU2006235344B2 (en) * 2005-04-08 2012-07-26 Comentis, Inc. Compounds which inhibit beta-secretase activity and methods of use thereof
CA2618653A1 (en) 2005-08-12 2007-02-22 Takeda Pharmaceutical Company Limited Brain/neuronal cell-protecting agent and therapeutic agent for sleep disorder
EP1971598A1 (en) 2005-11-21 2008-09-24 Amgen Inc. Beta-secretase modulators and methods of use
US7745484B2 (en) 2005-11-21 2010-06-29 Amgen Inc. Beta-secretase modulators and methods of use
US7872009B2 (en) 2005-11-21 2011-01-18 Amgen Inc. Beta-Secretase modulators and methods of use
US7838676B2 (en) 2005-11-21 2010-11-23 Amgen Inc. Beta-secretase modulators and methods of use
PE20080145A1 (es) * 2006-03-21 2008-02-11 Janssen Pharmaceutica Nv Tetrahidro-pirimidoazepinas como moduladores de trpv1
WO2007110727A2 (en) * 2006-03-27 2007-10-04 Pfizer Products Inc. Amide stabilized hydroxyethylamines
GB0607952D0 (en) * 2006-04-21 2006-05-31 Minster Res Ltd Novel treatment
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
EP2089383B1 (en) 2006-11-09 2015-09-16 Probiodrug AG 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
US9126987B2 (en) 2006-11-30 2015-09-08 Probiodrug Ag Inhibitors of glutaminyl cyclase
MX2009006228A (es) 2006-12-12 2009-06-22 Schering Corp Inhibidores de aspartil proteasa.
CA2676715A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
EP2481408A3 (en) 2007-03-01 2013-01-09 Probiodrug AG New use of glutaminyl cyclase inhibitors
WO2008128985A1 (en) 2007-04-18 2008-10-30 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
US8163909B2 (en) 2007-05-25 2012-04-24 Amgen Inc. Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
JP5440984B2 (ja) 2007-05-25 2014-03-12 アムジエン・インコーポレーテツド β−セクレターゼ修飾剤としての置換ヒドロキシエチルアミン化合物および使用方法
US20100286145A1 (en) * 2007-07-26 2010-11-11 Comentis, Inc. Isophthalamide derivatives inhibiting beta-secretase activity
EP2205596A1 (en) 2007-09-24 2010-07-14 Comentis, Inc. (3-hydroxy-4-amino-butan-2-yl) -3- (2-thiazol-2-yl-pyrrolidine-1-carbonyl) benzamide derivatives and related compounds as beta-secretase inhibitors for treating
SE531873C2 (sv) * 2007-11-12 2009-09-01 Lifeassays Ab Anordning för biokemisk bearbetning och analys av provvätska
US7803809B2 (en) 2008-11-12 2010-09-28 Amgen Inc. Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use
TW200942549A (en) 2007-12-17 2009-10-16 Janssen Pharmaceutica Nv Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of TRPV1
WO2009128057A2 (en) 2008-04-18 2009-10-22 UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN et al Psycho-pharmaceuticals
AU2009242127B2 (en) * 2008-04-29 2014-03-27 Pharnext New therapeutic approaches for treating Alzheimer disease and related disorders through a modulation of cell stress response
CA2731171C (en) 2008-07-28 2016-10-18 Blanchette Rockefeller Neurosciences Institute Pkc-activating compounds for the treatment of neurodegenerative diseases
KR20110073511A (ko) * 2008-09-11 2011-06-29 암젠 인크 베타세크레타제 조절제로서의 스피로-테트라사이클릭 고리 화합물 및 사용 방법
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
RU2011150521A (ru) * 2009-05-13 2013-06-20 ПРОТЕИН ДЕЛИВЕРИ СОЛЮШНЗ, ЭлЭлСи Фармацевтическая система для трансмембранной доставки
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
CA2772488C (en) 2009-09-11 2018-04-17 Probiodrug Ag Heterocyclic derivatives as inhibitors of glutaminyl cyclase
WO2011063233A1 (en) 2009-11-23 2011-05-26 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
EP2504330A1 (en) 2009-11-23 2012-10-03 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
CA2788363A1 (en) 2010-01-19 2011-07-28 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
JP2013518882A (ja) * 2010-02-05 2013-05-23 ファイザー・インク ＪＡＫ阻害剤としてのピロロ［２，３−ｄ］ピリミジン尿素化合物
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
NZ602312A (en) 2010-03-10 2014-02-28 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
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
CA2791281A1 (en) 2010-03-15 2011-09-22 Amgen Inc. Spiro-tetracyclic ring compounds as beta-secretase modulators
JP5945532B2 (ja) 2010-04-21 2016-07-05 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体
WO2012069428A1 (en) 2010-11-22 2012-05-31 Noscira, S.A. Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions
EP2673279A1 (en) 2011-02-07 2013-12-18 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
EP2758406A1 (en) 2011-09-21 2014-07-30 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9302992B2 (en) * 2013-04-02 2016-04-05 Annji Pharmaceutical Co., Ltd. Multifunctional quinoline derivatives as anti-neurodegenerative agents
CN106748892B (zh) * 2017-01-18 2018-09-18 四川大学 靶向自噬激动剂及其在神经退行性疾病治疗药物中的应用
IL273428B2 (en) 2017-09-22 2023-09-01 Jubilant Epipad LLC Heterocyclic compounds as pad inhibitors
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa
CN111225915B (zh) 2017-10-18 2023-03-07 朱比兰特埃皮帕德有限公司 作为pad抑制剂的咪唑并吡啶化合物
BR112020008851A2 (pt) 2017-11-06 2020-10-20 Jubilant Prodel LLC composto da fórmula i, processo de preparação de compostos da fórmula i, composição farmacêutica, método para o tratamento e/ou prevenção de várias doenças, uso, método para o tratamento de câncer, método de tratamento de câncer e método para o tratamento e/ou prevenção de câncer e doenças infecciosas
JP7368369B2 (ja) 2017-11-24 2023-10-24 ジュビラント・エピスクライブ・エルエルシー Ｐｒｍｔ５阻害剤としてのヘテロ環式化合物
JP7279063B6 (ja) 2018-03-13 2024-02-15 ジュビラント プローデル エルエルシー Ｐｄ１／ｐｄ－ｌ１相互作用／活性化の阻害剤としての二環式化合物

Family Cites Families (155)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5753564Y2 (es) 1977-06-01 1982-11-19
CH624011A5 (es) 1977-08-05 1981-07-15 Battelle Memorial Institute
FR2416008A1 (fr) 1978-02-02 1979-08-31 Oreal Lyophilisats de liposomes
US4394448A (en) 1978-02-24 1983-07-19 Szoka Jr Francis C Method of inserting DNA into living cells
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4399216A (en) 1980-02-25 1983-08-16 The Trustees Of Columbia University Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
ZA811368B (en) 1980-03-24 1982-04-28 Genentech Inc Bacterial polypedtide expression employing tryptophan promoter-operator
US5142056A (en) 1989-05-23 1992-08-25 Abbott Laboratories Retroviral protease inhibiting compounds
NZ201705A (en) 1981-08-31 1986-03-14 Genentech Inc Recombinant dna method for production of hepatitis b surface antigen in yeast
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US4870009A (en) 1982-11-22 1989-09-26 The Salk Institute For Biological Studies Method of obtaining gene product through the generation of transgenic animals
US4668770A (en) 1982-12-27 1987-05-26 Merck & Co., Inc. Renin inhibitory tripeptides
AU2353384A (en) 1983-01-19 1984-07-26 Genentech Inc. Amplification in eukaryotic host cells
US4713339A (en) 1983-01-19 1987-12-15 Genentech, Inc. Polycistronic expression vector construction
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
US4474778A (en) * 1983-11-09 1984-10-02 E. R. Squibb & Sons, Inc. Lactam containing compounds, their pharmaceutical compositions and method of use
US4512988A (en) * 1984-03-01 1985-04-23 E. R. Squibb & Sons, Inc. Acylamino oxo or hydroxy substituted alkylamino thiazines and thiazepines
US4636491A (en) 1984-03-27 1987-01-13 Merck & Co., Inc. Renin inhibitory peptides having improved solubility
US4736866A (en) 1984-06-22 1988-04-12 President And Fellows Of Harvard College Transgenic non-human mammals
JPH0662529B2 (ja) 1984-07-13 1994-08-17 三共株式会社 アミノ酸誘導体
US4880781A (en) 1984-08-06 1989-11-14 The Upjohn Company Renin inhibitory peptides containing an N-alkyl-histidine moiety
JPS6150912A (ja) 1984-08-16 1986-03-13 Shionogi & Co Ltd リポソ−ム製剤の製造法
US4814270A (en) 1984-09-13 1989-03-21 Becton Dickinson And Company Production of loaded vesicles
US4749792A (en) 1984-09-26 1988-06-07 E. R. Squibb & Sons, Inc. Diamino ketones and alcohols as analgesic agents
US4616088A (en) 1984-10-29 1986-10-07 E. R. Squibb & Sons, Inc. Amino acid ester and amide renin inhibitor
US4665193A (en) 1984-12-14 1987-05-12 E. R. Squibb & Sons, Inc. Amino acid ester renin inhibitors
US4897355A (en) 1985-01-07 1990-01-30 Syntex (U.S.A.) Inc. N[ω,(ω-1)-dialkyloxy]- and N-[ω,(ω-1)-dialkenyloxy]-alk-1-yl-N,N,N-tetrasubstituted ammonium lipids and uses therefor
US4753788A (en) 1985-01-31 1988-06-28 Vestar Research Inc. Method for preparing small vesicles using microemulsification
CA1290097C (en) 1985-07-24 1991-10-01 Merck & Co., Inc. Peptide enzyme inhibitors
US4729985A (en) 1985-08-09 1988-03-08 Pfizer Inc. Renin inhibitors containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues
US5175281A (en) 1985-09-12 1992-12-29 The Upjohn Company Pharmaceutically active pyrimidinylpiperazinylsterioids
US4676980A (en) 1985-09-23 1987-06-30 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Target specific cross-linked heteroantibodies
JPS63501364A (ja) 1985-11-15 1988-05-26 ジ・アップジョン・カンパニ− Ｓ−アリ−ル−ｄ−またはｌ−またはｄｌ−システイニル、３−（アリ−ルチオ）乳酸または３−（アリ−ルチオ）アルキル基を含有する新規レニン阻害ポリペプチド同族体
WO1987004349A1 (en) 1986-01-16 1987-07-30 Joseph Dellaria Peptide analogs
WO1987005330A1 (en) 1986-03-07 1987-09-11 Michel Louis Eugene Bergh Method for enhancing glycoprotein stability
DE3610593A1 (de) 1986-03-29 1987-10-01 Hoechst Ag Substituierte 4-amino-3-hydroxybuttersaeure-derivate verfahren zu deren herstellung, diese enthaltende mittel und ihre verwendung
US4851387A (en) 1986-10-14 1989-07-25 Banyu Pharmaceutical Co., Ltd. 5-substituted amino-4-hydroxy-pentanoic acid derivatives and their use
US4935405A (en) * 1986-10-31 1990-06-19 Pfizer Inc. Nor-statine and nor-cyclostatine polypeptides
ES2062988T3 (es) 1986-12-19 1995-01-01 Sankyo Co Nuevos oligopeptidos inhibidores de la renina, su preparacion y su uso.
US5250565A (en) 1987-02-10 1993-10-05 Abbott Laboratories Indole-,benzofuran-,and benzothiophene-containing lipoxygenase-inhibiting compounds
DE3721855A1 (de) 1987-03-12 1988-09-22 Merck Patent Gmbh Aminosaeurederivate
FR2614533A1 (fr) 1987-04-23 1988-11-04 Sandoz Sa Nouveaux derives peptidiques, leur preparation et leur utilisation comme medicaments
EP0366669A1 (en) 1987-06-29 1990-05-09 The Upjohn Company Malic acid derivative containing renin inhibiting peptides
US5010182A (en) 1987-07-28 1991-04-23 Chiron Corporation DNA constructs containing a Kluyveromyces alpha factor leader sequence for directing secretion of heterologous polypeptides
AU2123288A (en) 1987-08-07 1989-03-09 Upjohn Company, The Renin inhibiting peptides with nonpeptide linkages
GB8724885D0 (en) 1987-10-23 1987-11-25 Binns M M Fowlpox virus promotors
GB8728561D0 (en) 1987-12-07 1988-01-13 Glaxo Group Ltd Chemical compounds
EP0371068B1 (de) 1987-12-16 1991-06-19 Dallmer GmbH & Co. Ablaufarmatur für einen fliesenfussboden
JPH04501201A (ja) 1987-12-21 1992-03-05 ジ・アップジョン・カンパニー 発芽植物種子類のアグロバクテリウム媒介形質転換
IL89900A0 (en) 1988-04-12 1989-12-15 Merck & Co Inc Hiv protease inhibitors useful for the treatment of aids and pharmaceutical compositions containing them
AU4005289A (en) 1988-08-25 1990-03-01 Smithkline Beecham Corporation Recombinant saccharomyces
DE3841520A1 (de) 1988-12-09 1990-06-13 Hoechst Ag Enzymhemmende harnstoffderivate von dipeptiden, verfahren zu ihrer herstellung, diese enthaltende mittel und ihre verwendung
FR2646437B1 (fr) 1989-04-28 1991-08-30 Transgene Sa Nouvelles sequences d'adn, leur application en tant que sequence codant pour un peptide signal pour la secretion de proteines matures par des levures recombinantes, cassettes d'expression, levures transformees et procede de preparation de proteines correspondant
DE69029036T2 (de) 1989-06-29 1997-05-22 Medarex Inc Bispezifische reagenzien für die aids-therapie
GB8927915D0 (en) 1989-12-11 1990-02-14 Hoffmann La Roche Novel alcohols
DE3941235A1 (de) 1989-12-14 1991-06-20 Bayer Ag Neue peptide, ihre herstellung und ihre verwendung in arzneimitteln
DE4001236A1 (de) 1990-01-18 1991-07-25 Bayer Ag Neue peptide, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel, insbesondere als arzneimittel gegen retroviren
DE4003575A1 (de) 1990-02-07 1991-08-08 Bayer Ag Retroisostere dipeptide, verfahren zur herstellung und ihre verwendung als renininhibitoren in arzneimitteln
GB9004483D0 (en) 1990-02-28 1990-04-25 Erba Carlo Spa New aryl-and heteroarylethenylene derivatives and process for their preparation
US5912410A (en) 1990-06-15 1999-06-15 Scios Inc. Transgenic non-human mice displaying the amyloid-forming pathology of alzheimer's disease
AU646877B2 (en) 1990-06-15 1994-03-10 Scios Nova Inc. Transgenic non-human mammal displaying the amyloid-forming pathology of alzheimer's disease
CA2086414A1 (en) 1990-07-06 1992-01-07 Geoffrey B. Dreyer Retroviral protease inhibitors
US5708004A (en) 1990-11-19 1998-01-13 Monsanto Company Retroviral protease inhibitors
US5648511A (en) 1990-11-19 1997-07-15 G.D. Searle & Co. Method for making intermediates useful in the synthesis of retroviral protease inhibitors
US5482947A (en) 1990-11-19 1996-01-09 Talley; John J. Retroviral protease inhibitors
JP3510244B2 (ja) 1991-01-21 2004-03-22 エラン ファーマシューティカルス，インコーポレイテッド アルツハイマー病に関するテストおよびモデル
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
US5206161A (en) 1991-02-01 1993-04-27 Genentech, Inc. Human plasma carboxypeptidase B
AU1748792A (en) 1991-04-04 1992-11-02 Upjohn Company, The Phosphorus containing compounds as inhibitors of retroviruses
EP0586505A1 (en) 1991-05-14 1994-03-16 Repligen Corporation Heteroconjugate antibodies for treatment of hiv infection
US5753652A (en) 1991-07-03 1998-05-19 Novartis Corporation Antiretroviral hydrazine derivatives
DE59207226D1 (de) * 1991-07-03 1996-10-31 Ciba Geigy Ag Pharmakologisch wirksame Hydrazinderivate und Verfahren zu deren Herstellung
IE922316A1 (en) 1991-07-17 1993-01-27 Smithkline Beecham Corp Retroviral protease inhibitors
US5516784A (en) 1991-08-13 1996-05-14 Schering Corporation Anti-HIV (AIDS) agents
WO1993008829A1 (en) 1991-11-04 1993-05-13 The Regents Of The University Of California Compositions that mediate killing of hiv-infected cells
ATE243746T1 (de) 1992-01-07 2003-07-15 Elan Pharm Inc Transgene tiermodelle fur alzheimer-krankheit
WO1993017003A1 (en) 1992-02-26 1993-09-02 Smithkline Beecham Corporation Retroviral protease inhibitors
ATE253050T1 (de) 1992-03-11 2003-11-15 Narhex Ltd Aminderivate von oxo- und hydroxy- substituierten kohlenwasserstoffen
DE69300043T2 (de) 1992-03-13 1995-05-24 Bio Mega Boehringer Ingelheim Substituierte Pipecoline-Säurederivate als HIV-Protease-Hemmer.
US5502187A (en) 1992-04-03 1996-03-26 The Upjohn Company Pharmaceutically active bicyclic-heterocyclic amines
US5441870A (en) 1992-04-15 1995-08-15 Athena Neurosciences, Inc. Methods for monitoring cellular processing of β-amyloid precursor protein
US5604102A (en) 1992-04-15 1997-02-18 Athena Neurosciences, Inc. Methods of screening for β-amyloid peptide production inhibitors
US5376542A (en) 1992-04-27 1994-12-27 Georgetown University Method for producing immortalized cell lines using human papilluma virus genes
US5766846A (en) 1992-07-10 1998-06-16 Athena Neurosciences Methods of screening for compounds which inhibit soluble β-amyloid peptide production
ES2123065T3 (es) 1992-08-25 1999-01-01 Searle & Co Hidroxietilamino-sulfonamidas utiles como inhibidores de proteasas retroviricas.
RU2146668C1 (ru) 1992-08-25 2000-03-20 Джи Ди Сирл энд Компани Сульфонилалканоиламино-гидроксиэтиламино-сульфонамидное соединение, фармацевтические композиции и способы лечения и ингибирования ретровирусных протеаз
US5760076A (en) 1992-08-25 1998-06-02 G.D Searle & Co. Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US5830897A (en) 1992-08-27 1998-11-03 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US5578606A (en) 1992-10-30 1996-11-26 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
US5484926A (en) 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
MX9308025A (es) 1992-12-22 1994-08-31 Lilly Co Eli Compuestos inhibidores de la proteasa del virus dela inmunodeficiencia humana, procedimiento para supreparacion y formulacion farmaceutica que los contiene.
ES2150933T3 (es) 1992-12-22 2000-12-16 Lilly Co Eli Inhibidores de la proteasa vih utiles para el tratamiento del sida.
US5461067A (en) 1993-02-25 1995-10-24 Abbott Laboratories Retroviral protease inhibiting compounds
IL110525A0 (en) * 1993-08-09 1994-11-11 Lilly Co Eli Identification and use of protease inhibitors
EP0715618B1 (en) 1993-08-24 1998-12-16 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
JPH09507746A (ja) 1993-10-27 1997-08-12 アテナ ニューロサイエンシズ，インコーポレイティド Ｓｗｅｄｉｓｈ変異を有するＡＰＰ対立遺伝子を含有するトランスジェニック動物
JPH07126286A (ja) 1993-11-05 1995-05-16 Yamanouchi Pharmaceut Co Ltd 新規なペプチド誘導体
US5733882A (en) 1994-01-17 1998-03-31 Smithkline Beecham Corporation Retroviral protease inhibitors
US5877399A (en) 1994-01-27 1999-03-02 Johns Hopkins University Transgenic mice expressing APP-Swedish mutation develop progressive neurologic disease
US5625031A (en) 1994-02-08 1997-04-29 Bristol-Myers Squibb Company Peptide inhibitors of the p33cdk2 and p34cdc2 cell cycle regulatory kinases and human papillomavirus E7 oncoprotein
US5475138A (en) 1994-07-07 1995-12-12 Pharm-Eco Laboratories Incorporated Method preparing amino acid-derived diaminopropanols
ES2180600T3 (es) 1994-10-19 2003-02-16 Novartis Ag Eteres de isosteros substrato de aspartato proteasa antivirales.
US6001813A (en) 1994-11-21 1999-12-14 Cortech Inc. Val-pro containing α-keto oxadiazoles as serine protease inhibitors
AUPM982594A0 (en) * 1994-12-02 1995-01-05 University Of Queensland, The HIV protease inhibitors
US5481011A (en) 1994-12-13 1996-01-02 Bristol-Myers Squibb Company Process for preparing N-protected amino acid α-halomethyl ketones and alcohols from N-protected amino acid esters
US6017887A (en) 1995-01-06 2000-01-25 Sibia Neurosciences, Inc. Peptide, peptide analog and amino acid analog protease inhibitors
US5804560A (en) 1995-01-06 1998-09-08 Sibia Neurosciences, Inc. Peptide and peptide analog protease inhibitors
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
US6143747A (en) 1995-01-20 2000-11-07 G. D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
ID18218A (id) 1995-01-27 1998-03-19 Novo Nordisk As Senyawa dengan sifat-sifat pelepas hormon pertumbuhan
US5545640A (en) 1995-04-04 1996-08-13 Bio-Mega/Boehringer Ingeleheim Research Inc. Protease inhibiting succinic acid derivatives
TW493991B (en) 1995-05-08 2002-07-11 Novartis Ag Pharmaceutical composition for oral administration of active agent having low water solubility and process for preparation of the same
US5565483A (en) 1995-06-07 1996-10-15 Bristol-Myers Squibb Company 3-substituted oxindole derivatives as potassium channel modulators
JPH11507538A (ja) 1995-06-07 1999-07-06 アテナ ニューロサイエンシズ インコーポレイティド β−セクレターゼ、β−セクレターゼに対する抗体、及びβ−セクレターゼ阻害を検出するためのアッセイ
US5744346A (en) 1995-06-07 1998-04-28 Athena Neurosciences, Inc. β-secretase
EP0876336B1 (en) 1995-11-21 2002-06-05 Novartis AG Azahexane derivatives as substrate isosters of retroviral asparate proteases
US5886046A (en) 1996-01-19 1999-03-23 The Trustees Of The University Of Pennsylvania Dicarbonyl-containing compounds
US5849691A (en) 1996-02-20 1998-12-15 The United States Of America As Represented By The Department Of Health And Human Services Peptidomimetic inhibitors of cathepsin D and plasmepsins I and II
US5849911A (en) 1996-04-22 1998-12-15 Novartis Finance Corporation Antivirally active heterocyclic azahexane derivatives
JP2000509717A (ja) 1996-05-07 2000-08-02 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド オキシランメタンアミン誘導体の調製方法
WO1998003473A1 (en) 1996-07-22 1998-01-29 Novo Nordisk A/S Compounds with growth hormone releasing properties
US5914333A (en) 1996-07-31 1999-06-22 Novo Nordisk A/S Treatment of psychotic disorders
US5703129A (en) 1996-09-30 1997-12-30 Bristol-Myers Squibb Company 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of β-amyloid protein production
WO1998022597A2 (en) 1996-11-20 1998-05-28 Oklahoma Medical Research Foundation Cloning and characterization of napsin, an aspartic protease
US6191166B1 (en) 1997-11-21 2001-02-20 Elan Pharmaceuticals, Inc. Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
US6153652A (en) 1996-11-22 2000-11-28 Elan Pharmaceuticals, Inc. N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6127556A (en) 1996-12-31 2000-10-03 G. D. Searle & Co. Epoxide formation by continuous in-situ synthesis process
JP2001510474A (ja) * 1997-02-04 2001-07-31 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア カテプシンｄのナノモルの非ペプチド阻害剤
US6045829A (en) 1997-02-13 2000-04-04 Elan Pharma International Limited Nanocrystalline formulations of human immunodeficiency virus (HIV) protease inhibitors using cellulosic surface stabilizers
PL335484A1 (en) 1997-02-26 2000-04-25 Pfizer Derivatives of heteroarylhexamide, their production and application as selective inhibitors of mip-1a being assimilated by its ccr1 receptor
US6221670B1 (en) 1997-03-21 2001-04-24 Scios Inc. Methods to identify β-amyloid reducing agents
WO1998050342A1 (en) 1997-05-08 1998-11-12 Smithkline Beecham Corporation Protease inhibitors
US5962506A (en) 1997-07-07 1999-10-05 Pharmacopeia, Inc. Glycol and hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases
US6087383A (en) 1998-01-20 2000-07-11 Bristol-Myers Squibb Company Bisulfate salt of HIV protease inhibitor
CA2320117A1 (en) 1998-02-12 1999-08-19 Emory University Sphingolipid derivatives and their methods of use
DE19817461A1 (de) 1998-04-20 1999-10-21 Basf Ag Neue substituierte Benzamide, deren Herstellung und Anwendung
BR9912169A (pt) * 1998-06-19 2001-04-10 Vertex Pharma Inibidores de sulfonamida de protease de aspartil
KR20070013361A (ko) 1998-09-24 2007-01-30 파마시아 앤드 업존 캄파니 엘엘씨 알츠하이머병 세크레타제
NZ534876A (en) 1999-02-10 2006-02-24 Elan Pharm Inc Human beta-secretase enzyme, inhibitors and their compositions and uses
CA2367112A1 (en) 1999-03-24 2000-09-28 The Regents Of The University Of California Methods for treating neurodegenerative disorders using aspartyl protease inhibitors
AU4072200A (en) 1999-04-09 2000-11-14 Human Genome Sciences, Inc. 48 human secreted proteins
US7087399B1 (en) 1999-05-13 2006-08-08 Scios, Inc. β-secretase and modulation of β-secretase activity
EP1192177A1 (en) 1999-06-15 2002-04-03 Elan Pharmaceuticals, Inc. Statine-derived tetrapeptide inhibitors of beta-secretase
CN1379819A (zh) 1999-06-28 2002-11-13 俄克拉荷马州医学研究基金会 具有催化活性的重组memapsin蛋白酶及其应用方法
CA2378984A1 (en) 1999-08-09 2001-02-15 Richard B. Kim Antiviral therapy use of p-glycoprotein modulators
MXPA02001813A (es) 1999-09-13 2004-03-19 Bristol Myers Squibb Pharma Co Hidroxialcanoilaminolactamas y estructuras relacionas como inhibidores de la produccion de la proteina abeta.
PE20010693A1 (es) 1999-09-23 2001-06-24 Upjohn Co Metodo para la determinacion de actividad alfa-secretasa sobre la app
GB9924957D0 (en) 1999-10-21 1999-12-22 Smithkline Beecham Plc Novel treatment
WO2001051659A2 (en) 2000-01-13 2001-07-19 Genset Biallelic markers derived from genomic regions carrying genes involved in central nervous system disorders
ES2252257T3 (es) 2000-06-30 2006-05-16 Elan Pharmaceuticals, Inc. Compuestos para tratar la enfermedad de alzheimer.
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
BR0209985A (pt) 2001-05-22 2004-06-29 Elan Pharm Inc Composto e método para o tratamento de um paciente
CA2448834A1 (en) 2001-06-01 2002-12-12 Elan Pharmaceuticals, Inc. Hydroxy alkyl amine derivatives as beta-secretase inhibitors and their use for the treatment of alzheimer's disease and similar diseases
AR039555A1 (es) 2001-11-08 2005-02-23 Upjohn Co Derivados n,n'-sustituidos de 1,3-diamino-2-hidroxipropano

Also Published As

Publication number Publication date
NZ523005A (en) 2004-11-26
EP1299349A2 (en) 2003-04-09
CN1443155A (zh) 2003-09-17
JP2004502664A (ja) 2004-01-29
ES2252257T3 (es) 2006-05-16
WO2002002505A2 (en) 2002-01-10
WO2002002506A8 (en) 2003-11-20
AU2001273113A1 (en) 2002-01-14
MXPA02012560A (es) 2003-05-14
EP1299352A2 (en) 2003-04-09
WO2002002518A2 (en) 2002-01-10
AU2001271686A1 (en) 2002-01-14
ATE314343T1 (de) 2006-01-15
DE60112942D1 (de) 2005-09-29
US7432389B2 (en) 2008-10-07
WO2002002505A3 (en) 2002-08-01
ATE302751T1 (de) 2005-09-15
ZA200209991B (en) 2004-05-03
HK1055721A1 (en) 2004-01-21
AU2001273094A1 (en) 2002-01-14
DE60112942T2 (de) 2006-06-22
US7034182B2 (en) 2006-04-25
US20020016320A1 (en) 2002-02-07
US20060211860A1 (en) 2006-09-21
KR20030058959A (ko) 2003-07-07
WO2002002506A3 (en) 2002-08-29
ZA200300327B (en) 2004-03-25
JP2004502665A (ja) 2004-01-29
WO2002002505A8 (en) 2003-11-20
CA2410972A1 (en) 2002-01-10
EP1299349B1 (en) 2005-08-24
EP1299352B1 (en) 2005-12-28
BR0111980A (pt) 2003-05-06
CA2410680A1 (en) 2002-01-10
DE60116313T2 (de) 2006-08-31
WO2002002506A2 (en) 2002-01-10
CN1217920C (zh) 2005-09-07
DE60116313D1 (de) 2006-02-02
WO2002002518A3 (en) 2002-08-08

Similar Documents

Publication Publication Date Title
ES2248356T3 (es) Compuestos para tratar la enfermedad de alzheimer.
UY26813A1 (es) Compuestos para tratar enfermedad de alzheimer
WO2002002520A8 (en) Compounds to treat alzheimer's disease
AU2001252958A1 (en) Compounds and methods to treat alzheimer's disease
GB0005251D0 (en) Therapeutic compounds
ATE346039T1 (de) Sulfonamido-substituierte verbrückte bicycloalkylderivative
EA200300293A1 (ru) Противовоспалительные конденсированные пирролокарбазолы
TNSN04165A1 (en) Substituted hydroxyethylamines
BR9909844A (pt) Processo para sintetizar um composto, e, composto.
BR0111913A (pt) Análogos de gabapentina para distúrbios do sono
DK1109817T3 (da) Phosphohalogenhydriner, deres fremstilling og anvendelse
BR0205812A (pt) Benzimidazois úteis no tratamento da disfunção sexual
BR9808923A (pt) Composto, e, processo para fazer o mesmo
SE9904674D0 (sv) Novel compounds
TR200402070T4 (tr) Siklobüten-dion türevleri ve bunların damar sertliği tedavisinde kullanımı
EA200000242A1 (ru) Применение фанхинона для лечения болезни альцгеймера
CY1107039T1 (el) Αναστολεις τριπεπτιδυλ πεπτιδασης
TR200103561T2 (tr) Rodanin türevleri ve amiloidlerin önlenmesi ve görüntülenmesinde kullanımları
PT1347960E (pt) Processo para a preparacao de (+)-trans-4-p-fluorofenil-3-hidroximetil-1-metilpiperidina
EA200300061A1 (ru) Комбинированная противоопухолевая терапия, включающая применение производных замещенного акрилоилдистамицина и алкилирующих агентов
EA200201234A1 (ru) Производные сульфонамида
BRPI0409586A (pt) ácidos hidroxámicos úteis no tratamento de distúrbios hiperproliferativos
EP1586556A3 (en) Compounds to treat Alzheimer's disease
ES2097688A1 (es) Hexahidroazepinonas y tetrahidrobenzazepinonas sustituidas.