EE200200716A - Ühendid Alzheimeri tõve käitluseks - Google Patents

Ühendid Alzheimeri tõve käitluseks

Info

Publication number
EE200200716A
EE200200716A EEP200200716A EEP200200716A EE200200716A EE 200200716 A EE200200716 A EE 200200716A EE P200200716 A EEP200200716 A EE P200200716A EE P200200716 A EEP200200716 A EE P200200716A EE 200200716 A EE200200716 A EE 200200716A
Authority
EE
Estonia
Prior art keywords
alzheimer
disease
compounds
treatment
Prior art date
Application number
EEP200200716A
Other languages
English (en)
Inventor
Maillard Michel
Hom Roy
Gailunas Andrea
Jagodzinska Barbara
Y. Fang Lawrence
John Varghese
N. Freskos John
R. Pulley Shon
P. Beck James
E. Tenbrink Ruth
Original Assignee
Elan Pharmaceuticals, Inc.
Pharmacia & Upjohn Company
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, Inc., Pharmacia & Upjohn Company filed Critical Elan Pharmaceuticals, Inc.
Publication of EE200200716A publication Critical patent/EE200200716A/et

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • 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
    • C07D295/22—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 hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—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
    • 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
    • C07C311/08—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
    • 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
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (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)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Furan Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Indole Compounds (AREA)
EEP200200716A 2000-06-30 2001-06-29 Ühendid Alzheimeri tõve käitluseks EE200200716A (et)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US21532300P 2000-06-30 2000-06-30
US25273600P 2000-11-22 2000-11-22
US25595600P 2000-12-15 2000-12-15
US26849701P 2001-02-13 2001-02-13
US27977901P 2001-03-29 2001-03-29
US29558901P 2001-06-04 2001-06-04
PCT/US2001/021012 WO2002002512A2 (en) 2000-06-30 2001-06-29 Compounds to treat alzheimer's disease

Publications (1)

Publication Number Publication Date
EE200200716A true EE200200716A (et) 2004-08-16

Family

ID=27559082

Family Applications (1)

Application Number Title Priority Date Filing Date
EEP200200716A EE200200716A (et) 2000-06-30 2001-06-29 Ühendid Alzheimeri tõve käitluseks

Country Status (22)

Country Link
US (1) US7214715B2 (et)
EP (1) EP1353898A2 (et)
JP (1) JP2004502669A (et)
KR (1) KR20030058960A (et)
CN (1) CN100366605C (et)
AR (1) AR031852A1 (et)
AU (1) AU2001273137A1 (et)
BR (1) BR0112000A (et)
CA (1) CA2410651A1 (et)
CZ (1) CZ20024194A3 (et)
EA (1) EA007337B1 (et)
EE (1) EE200200716A (et)
HU (1) HUP0303037A3 (et)
IL (1) IL153214A0 (et)
MX (1) MXPA02012608A (et)
NO (1) NO20026199L (et)
NZ (3) NZ538542A (et)
PE (1) PE20020276A1 (et)
PL (1) PL359864A1 (et)
SK (1) SK18442002A3 (et)
UY (1) UY26813A1 (et)
WO (1) WO2002002512A2 (et)

Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2410680A1 (en) * 2000-06-30 2002-01-10 Elan Pharmaceuticals, Inc. Compounds to treat alzheimer's disease
WO2002008189A1 (en) * 2000-07-24 2002-01-31 The University Of Queensland Compounds and inhibitors of phospholipases
AR035960A1 (es) 2001-04-23 2004-07-28 Elan Pharm Inc Epoxidos sustituidos y procesos para prepararlos
CA2452039A1 (en) 2001-06-27 2003-01-09 Elan Pharmaceuticals, Inc. Beta-hydroxyamine derivatives useful in treatment of alzheimer's disease
US20070213407A1 (en) * 2001-06-29 2007-09-13 Elan Pharmaceuticals And Pharmacia & Upjohn Company Llc Compounds to treat Alzheimer's disease
AU2002320490B2 (en) * 2001-07-11 2008-10-02 Elan Pharmaceuticals, Inc. N-(3-amino-2-hydroxy-propyl) substituted alkylamide compounds
JP2005535559A (ja) * 2001-10-29 2005-11-24 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー アルツハイマー病を治療するためのヒドロキシ置換アミド
AR039555A1 (es) * 2001-11-08 2005-02-23 Upjohn Co Derivados n,n'-sustituidos de 1,3-diamino-2-hidroxipropano
EP1453792B1 (en) * 2001-11-19 2007-04-18 Elan Pharmaceuticals, Inc. Amine 1,2- and 1,3-diol compounds and their use for treatment of alzheimer's disease
WO2003050073A1 (en) * 2001-12-06 2003-06-19 Elan Pharmaceuticals, Inc. Substituted hydroxyethylamines
JP2005533811A (ja) 2002-06-20 2005-11-10 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー ５−（１，３−オキサゾル−２−イル）安息香酸誘導体の調製方法
AU2003254844A1 (en) * 2002-08-09 2004-02-25 Takeda Chemical Industries, Ltd. Substituted amino compounds and use thereof
RU2357962C2 (ru) * 2002-09-06 2009-06-10 Элан Фармасьютикалз, Инк. Пролекарственные производные 1,3-диамино-2-гидроксипропана
UY27967A1 (es) * 2002-09-10 2004-05-31 Pfizer Acetil 2-hindroxi-1,3-diaminoalcanos
AU2003273310A1 (en) * 2002-09-10 2004-04-30 Pharmacia And Upjohn Substituted aminoethers for the treatment of alzheimer's disease
US7763646B2 (en) 2002-09-27 2010-07-27 Elan Pharmaceuticals, Inc. Compounds for the treatment of alzheimer's disease
TW200509968A (en) * 2002-11-01 2005-03-16 Elan Pharm Inc Prevention and treatment of synucleinopathic disease
US9034337B2 (en) * 2003-10-31 2015-05-19 Prothena Biosciences Limited Treatment and delay of outset of synucleinopathic and amyloidogenic disease
DE60329316D1 (de) * 2002-11-12 2009-10-29 Merck & Co Inc Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer
PE20040762A1 (es) * 2002-11-27 2004-11-06 Elan Pharm Inc Ureas substituidas y carbamatos utiles para el tratamiento de la enfermedad de alzheimer
ATE401307T1 (de) * 2002-11-28 2008-08-15 Suven Life Sciences Ltd N-arylsulfonyl-2-substituierte indole mit affinität zum serotonin rezeptor, verfahren zu deren herstellung und diese enthaltende pharmazeutische zusammensetzungen
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
TW200512195A (en) * 2003-04-21 2005-04-01 Elan Pharm Inc Benzamide 2-hydroxy-3-diaminoalkanes
CL2004000848A1 (es) * 2003-04-21 2005-01-28 Elan Pharmaceuticals Inc Pharm Compuestos derivados de fenacil-2-hidroxi-3-diaminoalcanos, inhibidores de la enzima betasecretasa, utiles para preparar un medicamento para tratar alzheimer, sindrome de down, hemorragia cerebral hereditaria con amiloidosis de tipo holandes, y otras
CA2534950A1 (en) 2003-08-08 2005-02-24 Schering Corporation Cyclic amine bace-1 inhibitors having a benzamide substituent
CN1863770B (zh) 2003-08-08 2011-05-25 先灵公司 具有杂环取代基的环胺base-1抑制剂
KR100793095B1 (ko) * 2003-10-01 2008-01-10 주식회사 프로메디텍 Ｂａｃｅ 저해효능을 가진 신규한 술폰 아미드 유도체
WO2005032471A2 (en) 2003-10-03 2005-04-14 Merck & Co., Inc. Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease
US20050255488A1 (en) * 2003-10-15 2005-11-17 Genaissance Pharmaceuticals NTRK1 genetic markers associated with age of onset of Alzheimer's Disease
WO2005047860A2 (en) 2003-11-08 2005-05-26 Elan Pharmaceuticals, Inc. Antibodies to alpha-synuclein
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
JP2007517781A (ja) * 2003-12-19 2007-07-05 メルク　エンド　カムパニー　インコーポレーテッド アルツハイマー病治療用のフェニルアミドおよびピリジルアミド系β−セクレターゼ阻害薬
EP1734961A2 (en) * 2004-03-09 2006-12-27 Elan Pharmaceuticals, Inc. Methods of treatment of amyloidosis using bi-cyclic aspartyl protease inhibitors
US20050239790A1 (en) * 2004-03-09 2005-10-27 Varghese John Substituted hydroxyethylamine aspartyl protease inhibitors
CA2558034A1 (en) 2004-03-09 2005-09-22 Elan Pharmaceuticals, Inc. Substituted hydroxyethylamine aspartyl protease inhibitors
CA2572775A1 (en) * 2004-07-09 2006-01-26 Elan Pharmaceuticals, Inc. Oxime derivative hydroxyethylamine aspartyl-protease inhibitors
EP1773756A2 (en) * 2004-07-09 2007-04-18 Elan Pharmaceuticals, Inc. Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors
JP2008507538A (ja) 2004-07-22 2008-03-13 シェーリング　コーポレイション 置換アミドβセクレターゼインヒビター
CA2575340A1 (en) 2004-07-28 2006-02-09 Schering Corporation Macrocyclic beta-secretase inhibitors
US7361789B1 (en) 2004-07-28 2008-04-22 Amgen Inc. Dihydronaphthalene compounds, compositions, uses thereof, and methods for synthesis
JP2008513495A (ja) * 2004-09-17 2008-05-01 コメンティス，インコーポレーテッド ベータ−セクレターゼ活性を阻害する二環式化合物およびその使用方法
WO2006043710A1 (ja) * 2004-10-19 2006-04-27 Reverse Proteomics Research Institute Co., Ltd. 創薬標的タンパク質及び標的遺伝子、並びにスクリーニング方法
WO2006099352A1 (en) 2005-03-10 2006-09-21 Bristol-Myers Squibb Company Novel isophthalates as beta-secretase inhibitors
US20060223849A1 (en) * 2005-03-14 2006-10-05 Mjalli Adnan M Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors
MX2007012341A (es) 2005-04-08 2008-02-12 Comentis Inc Compuestos que inhiben actividad beta-secretasa y metodos de uso de los mismos.
CN101198583A (zh) * 2005-04-08 2008-06-11 科门蒂斯公司 抑制β-分泌酶(SECRETASE)活性的化合物及其使用方法
US8722708B2 (en) 2005-06-14 2014-05-13 Merck Sharp & Dohme Inc. Substituted isoindolines as aspartyl protease inhibitors
ES2426345T3 (es) * 2005-07-20 2013-10-22 Eli Lilly And Company Compuesto unidos en posición 1-amino
US7476764B2 (en) * 2005-08-04 2009-01-13 Bristol-Myers Squibb Company Phenylcarboxyamides as beta-secretase inhibitors
EP1923388A4 (en) 2005-08-12 2011-03-09 Takeda Pharmaceutical BRAIN / NEURONAL CELL PROTECTIVE AGENT AND THERAPEUTIC AGENT FOR SLEEP DISORDERS
WO2007047305A1 (en) 2005-10-12 2007-04-26 Elan Pharmaceuticals, Inc. Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors
WO2007110727A2 (en) * 2006-03-27 2007-10-04 Pfizer Products Inc. Amide stabilized hydroxyethylamines
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
EP2066884B1 (fr) * 2006-09-22 2011-08-24 Renault Trucks Circuit de refroidissement d'un moteur thermique de vehicule automobile
EP2094645A1 (en) * 2006-11-23 2009-09-02 Novartis AG 2-hydroxy-1,3-diaminopropane derivatives
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
CN101348456B (zh) * 2007-07-17 2011-05-11 中国科学院上海药物研究所 苄基哌啶类化合物及其制备方法和用途
EP2178837A2 (en) * 2007-07-26 2010-04-28 Comentis, Inc. Isophthalamide derivatives inhibiting beta-secretase activity
CN101868457B (zh) 2007-09-24 2013-02-13 科门蒂斯公司 作为β-分泌酶抑制剂用于治疗的(3-羟基-4-氨基-丁-2-基)-3-(2-噻唑-2-基-吡咯烷-1-羰基)苯甲酰胺衍生物和相关化合物
WO2009129532A1 (en) * 2008-04-18 2009-10-22 University Of Connecticut Compounds for lysosomal modulation and methods of use
WO2009128057A2 (en) 2008-04-18 2009-10-22 UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN et al Psycho-pharmaceuticals
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
WO2010107384A1 (en) * 2009-03-19 2010-09-23 Medivir Ab Aspartyl protease inhibitors
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
US9284296B2 (en) 2010-11-22 2016-03-15 Aubergine Pharmaceuticals Llc Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions
CN102558157B (zh) * 2010-12-20 2014-04-30 中国科学院上海药物研究所 羟乙基三唑类化合物或氨乙基三唑类化合物及其制备方法和用途
CN103275070A (zh) * 2013-05-10 2013-09-04 郑彪 调节单核细胞增殖的四环化合物及其应用
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
CN111201030B (zh) 2017-07-25 2024-11-01 真和制药有限公司 通过阻断tim-3和其配体的相互作用治疗癌症
CN108530319A (zh) * 2018-05-17 2018-09-14 辽宁凯莱英医药化学有限公司 肟类化合物及腈类化合物连续合成的方法
KR20210124308A (ko) 2019-01-30 2021-10-14 트루바인딩 아이엔씨. 항-gal3 항체 및 이의 용도
MX2022014786A (es) 2020-05-26 2023-01-16 Truebinding Inc Metodos para tratar enfermedades inflamatorias mediante el bloqueo de galectina-3.

Family Cites Families (155)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1599907A (en) 1977-04-26 1981-10-07 Glaxo Lab Ltd Isoindolines
JPS5753564Y2 (et) 1977-06-01 1982-11-19
CH624011A5 (et) 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
US4604402A (en) * 1984-03-30 1986-08-05 E. R. Squibb & Sons, Inc. Hydroxy substituted ureido amino and imino acids
US4736866B1 (en) 1984-06-22 1988-04-12 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
WO1987002986A1 (en) 1985-11-15 1987-05-21 The Upjohn Company Novel renin inhibiting polypeptide analogs containing s-aryl-d- or l- or dl-cysteinyl, 3-(arylthio)lactic acid or 3-(arylthio)alkyl moieties
EP0258289A4 (en) 1986-01-16 1991-01-02 Joseph Dellaria Peptide analogs
JPS63502716A (ja) 1986-03-07 1988-10-13 マサチューセッツ・インステチュート・オブ・テクノロジー 糖タンパク安定性の強化方法
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
EP0264106B1 (en) 1986-10-14 1994-03-16 Banyu Pharmaceutical Co., Ltd. 5-Substituted amino-4-hydroxy-pentanoic acid derivatives and their use
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
WO1989000161A1 (en) 1987-06-29 1989-01-12 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
EP0364493A1 (en) 1987-08-07 1990-04-25 The Upjohn Company 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
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
EP0739904A1 (en) 1989-06-29 1996-10-30 Medarex, Inc. Bispecific reagents for aids therapy
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
JPH06507782A (ja) 1990-06-15 1994-09-08 サイオス　ノバ　インコーポレイテッド アルツハイマー病のアミロイド形成開症状を示すヒト以外の組換え哺乳動物
US5912410A (en) 1990-06-15 1999-06-15 Scios Inc. Transgenic non-human mice displaying the amyloid-forming pathology of alzheimer's disease
WO1992000750A1 (en) 1990-07-06 1992-01-23 Smithkline Beecham Corporation Retroviral protease inhibitors
CA2096528C (en) * 1990-11-19 2005-12-06 Kathryn Lea Reed Retroviral protease inhibitors
US5510487A (en) 1990-11-19 1996-04-23 G.D. Searle & Co. 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
AU652997B2 (en) 1991-01-21 1994-09-15 Elan Pharmaceuticals, Inc. Test and model for alzheimer's disease
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
EP0578745A1 (en) 1991-04-04 1994-01-19 The Upjohn Company Phosphorus containing compounds as inhibitors of retroviruses
WO1992020373A1 (en) 1991-05-14 1992-11-26 Repligen Corporation Heteroconjugate antibodies for treatment of hiv infection
US5753652A (en) 1991-07-03 1998-05-19 Novartis Corporation Antiretroviral hydrazine derivatives
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
DE69233109T2 (de) 1992-01-07 2004-05-19 Elan Pharmaceuticals, Inc., San Francisco Transgene tiermodelle fur alzheimer-krankheit
EP0628035A4 (en) 1992-02-26 1995-03-29 Smithkline Beecham Corp RETROVIRAL PROTEASE INHIBITORS.
ATE116640T1 (de) 1992-03-13 1995-01-15 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
US5604102A (en) 1992-04-15 1997-02-18 Athena Neurosciences, Inc. Methods of screening for β-amyloid peptide production inhibitors
US5441870A (en) 1992-04-15 1995-08-15 Athena Neurosciences, Inc. Methods for monitoring cellular processing of β-amyloid precursor protein
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
US5559256A (en) * 1992-07-20 1996-09-24 E. R. Squibb & Sons, Inc. Aminediol protease inhibitors
US5760076A (en) 1992-08-25 1998-06-02 G.D Searle & Co. Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
ATE161828T1 (de) 1992-08-25 1998-01-15 Searle & Co Sulfonylalkanoylaminohydroxyethylaminosulfonami e verwendbar als retrovirale protease-inhibitoren
DE122007000045I2 (de) 1992-08-25 2011-07-21 Gd Searle Llc Gd Searle Llc Darunavir oder pharmazeutisch vertragliche Salze, Hydroxyethylaminosulfonamide verwendbar als InhibiEster oder Prodrugs davon. toren retroviraler Proteasen.
US5830897A (en) 1992-08-27 1998-11-03 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
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.
DE69329544T2 (de) 1992-12-22 2001-05-31 Eli Lilly And Co., Indianapolis HIV Protease hemmende Verbindungen
US5461067A (en) 1993-02-25 1995-10-24 Abbott Laboratories Retroviral protease inhibiting compounds
CZ184194A3 (en) * 1993-08-09 1995-03-15 Lilly Co Eli Aspartylprotease inhibitor and method of identifying thereof
ES2127938T3 (es) 1993-08-24 1999-05-01 Searle & Co Hidroxietilamino sulfonamidas utiles como inhibidores de proteasas retroviricas.
AU702293B2 (en) 1993-10-27 1999-02-18 Athena Neurosciences, Inc. Transgenic animals harboring APP allele having Swedish mutation
JPH07126286A (ja) 1993-11-05 1995-05-16 Yamanouchi Pharmaceut Co Ltd 新規なペプチド誘導体
WO1995018971A1 (en) * 1994-01-11 1995-07-13 Affymax Technologies N.V. Methods for the solid phase synthesis of glycoconjugates
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
DE69527405T2 (de) 1994-10-19 2003-03-13 Novartis Ag, Basel Antivirale Ether von Aspartat-Protease-Substrat-Isosteren
US5492910A (en) * 1994-11-17 1996-02-20 Bristol-Myers Squibb Co. Retrocarbamate protease inhibitors
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
US5804560A (en) 1995-01-06 1998-09-08 Sibia Neurosciences, Inc. Peptide and peptide analog protease inhibitors
US5863902A (en) 1995-01-06 1999-01-26 Sibia Neurosciences, Inc. Methods of treating neurodegenerative disorders using protease inhibitors
DE69637380T2 (de) 1995-01-20 2009-09-17 G.D. Searle Llc, Chicago Bis-sulfonamid-hydroxyethylamino-derivate als inhibitoren retroviraler proteasen
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
MY113488A (en) 1995-01-27 2002-03-30 Novo Nordisk As Compounds with growth hormone releasing properties
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
US5744346A (en) 1995-06-07 1998-04-28 Athena Neurosciences, Inc. β-secretase
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
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
CA2251066A1 (en) 1996-05-07 1997-11-13 Boehringer Ingelheim Pharmaceuticals, Inc. Process for preparing oxiranemethanamine derivatives
EP1184370B1 (en) 1996-07-22 2005-09-14 Novo Nordisk A/S Compounds with growth hormone releasing properties
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
DE69738653T2 (de) 1996-11-20 2009-06-04 Oklahoma Medical Research Foundation, Oklahoma Klonierung und charakterisierung von napsin, einer aspartat-protease
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
US6191166B1 (en) 1997-11-21 2001-02-20 Elan Pharmaceuticals, Inc. Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
US6127556A (en) 1996-12-31 2000-10-03 G. D. Searle & Co. Epoxide formation by continuous in-situ synthesis process
WO1998033795A1 (en) * 1997-02-04 1998-08-06 The Regents Of The University Of California Nanomolar, non-peptide inhibitors of cathepsin d
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
SK112899A3 (en) 1997-02-26 2001-05-10 Pfizer Heteroaryl-hexanoic acid amide derivatives, their preparation and their use as selective inhibitors of mip-1-alpha binding to its ccr1 receptor
US6221670B1 (en) 1997-03-21 2001-04-24 Scios Inc. Methods to identify β-amyloid reducing agents
EP0983228A4 (en) * 1997-05-08 2002-08-07 Smithkline Beecham Corp PROTEASE INHIBITORS
US5962506A (en) 1997-07-07 1999-10-05 Pharmacopeia, Inc. Glycol and hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases
EP1053243B1 (en) 1998-02-12 2011-03-30 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
AU5002399A (en) 1998-07-17 2000-02-07 National Broach And Machine Company Full form roll finishing technique
ES2318902T3 (es) 1998-09-24 2009-05-01 PHARMACIA & UPJOHN COMPANY LLC Secretasa en la enfermedad del alzheimer.
WO2000047618A2 (en) 1999-02-10 2000-08-17 Elan Pharmaceuticals, Inc. HUMAN β-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
EP1171591A1 (en) 1999-04-09 2002-01-16 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
JP2003502342A (ja) 1999-06-15 2003-01-21 エラン ファーマスーティカルズ インコーポレイテッド ベータ−セクレターゼのスタチン誘導テトラペプチド阻害剤
EP1194449B1 (en) 1999-06-28 2010-09-22 Oklahoma Medical Research Foundation Inhibitors of memapsin 2 and use thereof
AU7757400A (en) 1999-08-09 2001-03-05 Vanderbilt University Antiviral therapy use of p-glycoprotein modulators
AU783914B2 (en) 1999-09-13 2005-12-22 Bristol-Myers Squibb Pharma Company Hydroxyalkanoyl aminolactams and related structures as inhibitors of a beta protein production
DK1224297T3 (da) 1999-09-23 2009-09-07 Pharmacia & Upjohn Co Llc Alzheimers sygdom -sekretase, APP-substrater derfor og anvendelser deraf
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
AU2001252958A1 (en) * 2000-03-23 2001-10-03 Elan Pharmaceuticals, Inc. Compounds and methods to treat alzheimer's disease
US20030096864A1 (en) 2000-06-30 2003-05-22 Fang Lawrence Y. Compounds to treat alzheimer's disease
US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
CA2410680A1 (en) 2000-06-30 2002-01-10 Elan Pharmaceuticals, Inc. Compounds to treat alzheimer's disease

Also Published As

Publication number Publication date
EP1353898A2 (en) 2003-10-22
AU2001273137A1 (en) 2002-01-14
HUP0303037A2 (hu) 2004-03-01
CA2410651A1 (en) 2002-01-10
HUP0303037A3 (en) 2006-02-28
CZ20024194A3 (cs) 2004-01-14
NZ547529A (en) 2008-04-30
US7214715B2 (en) 2007-05-08
SK18442002A3 (sk) 2004-07-07
BR0112000A (pt) 2003-06-03
NO20026199D0 (no) 2002-12-23
PE20020276A1 (es) 2002-04-06
CN1447789A (zh) 2003-10-08
KR20030058960A (ko) 2003-07-07
UY26813A1 (es) 2002-01-31
MXPA02012608A (es) 2003-05-14
WO2002002512A3 (en) 2003-08-21
PL359864A1 (en) 2004-09-06
NZ538542A (en) 2006-09-29
HU0303037D0 (en) 2003-11-28
AR031852A1 (es) 2003-10-08
JP2004502669A (ja) 2004-01-29
WO2002002512A2 (en) 2002-01-10
EA007337B1 (ru) 2006-08-25
IL153214A0 (en) 2003-07-06
US20020128255A1 (en) 2002-09-12
CN100366605C (zh) 2008-02-06
EA200201247A1 (ru) 2003-10-30
NZ522899A (en) 2005-06-24
NO20026199L (no) 2003-02-21

Similar Documents

Publication Publication Date Title
NO20026199D0 (no) Forbindelser for behandling av Alzheimers sykdom
CY2018020I2 (el) Θεραπεια της νοσου ρομρε
IL160884A0 (en) Azabicyclic-substituted fused-heteroaryl compounds for the treatment of disease
AU2001273132A1 (en) Compounds to treat alzheimer's disease
DK1392287T3 (da) Anvendelse af substituerede azetidinonderivater i behandlingen af Alzheimers sygdom
IL224393B (en) Compositions for treatment of huntington's disease
PL367311A1 (en) Quinuclidines-substituted-multi-cyclic-heteroaryls for the treatment of disease
IL150742A0 (en) Pyridopyrimidinone derivatives for the treatment of neurodegenerative disease
MA27126A1 (fr) 3'PROMEDICAMENTS DE 2'-DESOXY- β-L-NUCLEOSIDES
AU2001233299A1 (en) Methods for treating alzheimer's disease
NO20031443L (no) Forbindelser nyttige for behandling av inflammatoriske sykdommer
ITVR20010019A0 (it) "contrafforte per calzature"
AU2003206413A8 (en) Substituted amino carboxamides for the treatment of alzheimer's disease
EE200300216A (et) Radiofarmatseutilised ained Alzheimeri tõve diagnoosimiseks
AU2002315131A1 (en) Aminediols as agents for the treatment of alzheimer's disease
NO20001869D0 (no) Fremgangsmõte for behandling av Alzheimerssykdom
ITMI20010985A0 (it) Farmaci per il morbo di alzheimer
NO20010953D0 (no) En fremgangsmÕte for behandling av stafylokokkal sykdom
NO20033804D0 (no) Karbamatforbindelser for behandling av smerte
FR2818979B1 (fr) Procede de preparation d'imidaclopride
IS5951A (is) 5HT1 mótlyf fyrir meðferð gegn þunglyndi
AU2003303141A8 (en) Hydroxypropyl amides for the treatment of alzheimer's disease
AU2003273310A1 (en) Substituted aminoethers for the treatment of alzheimer's disease
EP1181550A4 (en) METHODS OF IDENTIFYING COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
NO20030717L (no) Forbindelser for behandling av avhengighetsforstyrrelser

Legal Events

Date Code Title Description
HB1A Correction of owner name or address