BR0210721A - Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição - Google Patents

Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição

Info

Publication number
BR0210721A
BR0210721A BR0210721-0A BR0210721A BR0210721A BR 0210721 A BR0210721 A BR 0210721A BR 0210721 A BR0210721 A BR 0210721A BR 0210721 A BR0210721 A BR 0210721A
Authority
BR
Brazil
Prior art keywords
patient
compound
disease
treating
salt
Prior art date
Application number
BR0210721-0A
Other languages
English (en)
Inventor
Varghese John
Roy Hom
John Tucker
Original Assignee
Elan Pharm Inc
Upjohn Co
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 Pharm Inc, Upjohn Co filed Critical Elan Pharm Inc
Publication of BR0210721A publication Critical patent/BR0210721A/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/84Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/90Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/28Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/12Oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/36Sulfur atom
    • C07D473/38Sulfur atom attached in position 6

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

"COMPOSTO, SAL OU éSTER FARMACEUTICAMENTE ACEITáVEL, MéTODO PARA FABRICAR UM COMPOSTO, E, MéTODO PARA TRATAR UM PACIENTE QUE TEM, OU PARA EVITAR QUE O PACIENTE ADQUIRA UMA DOENçA OU CONDIçãO". A invenção refere-se a compostos de álcool substituídos da fórmula (I), em que X, R~ 1~, R~ 2~, R~ 3~, R~ N~, R~ 20~ e R~ C~ são definidos neste. Os compostos são úteis no tratamento ou prevenção do mal de Alzheimer e mais especificamente a compostos que são capazes de inibir beta-secretase, uma enzima que cliva proteína precursora de amilóide para produzir peptídeo amilóide beta (A-beta), um componente principal das placas de amilóide encontrados nos cérebros dos sofredores de Alzheimer.
BR0210721-0A 2001-06-27 2002-06-27 Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição BR0210721A (pt)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US30121001P 2001-06-27 2001-06-27
US32339601P 2001-09-18 2001-09-18
US33273601P 2001-11-19 2001-11-19
PCT/US2002/020754 WO2003002122A1 (en) 2001-06-27 2002-06-27 Beta-hydroxyamine derivatives useful in treatment of alzheimer's disease

Publications (1)

Publication Number Publication Date
BR0210721A true BR0210721A (pt) 2004-07-20

Family

ID=27404798

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0210721-0A BR0210721A (pt) 2001-06-27 2002-06-27 Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição

Country Status (7)

Country Link
US (2) US6982264B2 (pt)
EP (1) EP1401452A1 (pt)
JP (1) JP2005500319A (pt)
BR (1) BR0210721A (pt)
CA (1) CA2452039A1 (pt)
MX (1) MXPA04000140A (pt)
WO (1) WO2003002122A1 (pt)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7521481B2 (en) 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
JP2007528400A (ja) 2004-03-09 2007-10-11 エラン ファーマシューティカルズ,インコーポレイテッド 置換ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬
WO2007047305A1 (en) 2005-10-12 2007-04-26 Elan Pharmaceuticals, Inc. Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors
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
WO2007061670A1 (en) 2005-11-21 2007-05-31 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
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
JP5930573B2 (ja) 2007-03-01 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤の新規使用
EP2142514B1 (en) 2007-04-18 2014-12-24 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
WO2008137954A2 (en) * 2007-05-07 2008-11-13 Environmental Packaging Technologies Limited Universal shipping container
CL2008001500A1 (es) 2007-05-25 2008-12-26 Amgen Inc Compuestos derivados de hidroxietil amina sustituidas, moduladores de betasecretasa; proceso de preparacion de dichos c ompuestos; composicion farmaceutica que los comprende; y su uso para tratar un trastorno neurologico, tal como alzheimer, sindrome de down, demencia degenerativa, entre otros.
WO2008147544A1 (en) 2007-05-25 2008-12-04 Amgen Inc. Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
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
EP2227471A1 (en) 2007-12-11 2010-09-15 Schering Corporation Gamma secretase modulators
CA2731171C (en) 2008-07-28 2016-10-18 Blanchette Rockefeller Neurosciences Institute Pkc-activating compounds for the treatment of neurodegenerative diseases
MY148558A (en) * 2008-09-11 2013-04-30 Amgen Inc Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use
JP5934645B2 (ja) 2009-09-11 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体
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
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)
EP2547685A1 (en) 2010-03-15 2013-01-23 Amgen Inc. Spiro-tetracyclic ring compounds as beta - secretase modulators
US8497264B2 (en) 2010-03-15 2013-07-30 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
US9346827B2 (en) 2011-02-07 2016-05-24 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
WO2013044092A1 (en) 2011-09-21 2013-03-28 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
WO2014078314A1 (en) 2012-11-15 2014-05-22 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US20140249377A1 (en) * 2013-03-01 2014-09-04 Eugen Tarnow Well defined system and method for monitoring neurological disease onset and progress and onset of the effects of neuropharmacological drugs using the recency-primacy shift and overall free recall differences
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa

Family Cites Families (183)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3547119A (en) 1967-12-08 1970-12-15 Baxter Laboratories Inc Catheter assembly
US3739778A (en) 1971-08-12 1973-06-19 Bard Inc C R Catheter introduction system
US3996923A (en) 1973-03-23 1976-12-14 Guerra Luis A Blood taking device
US4106491A (en) 1975-07-24 1978-08-15 Guerra Luis A Device for prolonged intravascular infusion
JPS5753564Y2 (pt) 1977-06-01 1982-11-19
US4126133A (en) 1977-07-13 1978-11-21 Boris Schwartz Intracorporeal catheter improvement
CH624011A5 (pt) 1977-08-05 1981-07-15 Battelle Memorial Institute
FR2416008A1 (fr) 1978-02-02 1979-08-31 Oreal Lyophilisats de liposomes
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4394448A (en) 1978-02-24 1983-07-19 Szoka Jr Francis C Method of inserting DNA into living cells
DE2845643C2 (de) 1978-10-20 1982-04-08 Max Dr. 8520 Erlangen Hubmann Katheteranschlußkopf mit mindestens einem Kanal in einem Grundkörper
US4258940A (en) 1979-03-01 1981-03-31 Bio-Dynamics, Inc. Sealing connector for liquid and gas systems
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
US4311137A (en) 1980-04-30 1982-01-19 Sherwood Medical Industries Inc. Infusion device
US5142056A (en) 1989-05-23 1992-08-25 Abbott Laboratories Retroviral protease inhibiting compounds
US4430081A (en) 1981-01-06 1984-02-07 Cook, Inc. Hemostasis sheath
US4418944A (en) 1981-02-11 1983-12-06 Haines Stephen W Fluid coupling
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
US4713339A (en) 1983-01-19 1987-12-15 Genentech, Inc. Polycistronic expression vector construction
AU2353384A (en) 1983-01-19 1984-07-26 Genentech Inc. Amplification in eukaryotic host cells
US5281206A (en) 1983-01-24 1994-01-25 Icu Medical, Inc. Needle connector with rotatable collar
US4531937A (en) 1983-01-24 1985-07-30 Pacesetter Systems, Inc. Introducer catheter apparatus and method of use
US5330450A (en) 1983-01-24 1994-07-19 Icu Medical, Inc. Medical connector
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
US4636491A (en) 1984-03-27 1987-01-13 Merck & Co., Inc. Renin inhibitory peptides having improved solubility
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
FR2578746B1 (fr) 1985-03-12 1991-12-20 Sifc Dispositif de maintien en conditions aseptiques d'un site de connexion, d'injection ou de prelevement a usage medical
US4645495A (en) 1985-06-26 1987-02-24 Vaillancourt Vincent L Vascular access implant needle patch
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
US4755173A (en) 1986-02-25 1988-07-05 Pacesetter Infusion, Ltd. Soft cannula subcutaneous injection set
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
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
BE1002213A5 (fr) 1987-04-23 1990-10-16 Sandoz Sa Nouveaux derives peptidiques, leur preparation et leur utilisation comme medicaments.
JPH02504143A (ja) 1987-06-29 1990-11-29 ジ・アップジョン・カンパニー リンゴ酸誘導体含有レニン抑制ペプチド
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
JPH02504509A (ja) 1987-08-07 1990-12-20 ジ・アップジョン・カンパニー 非ペプチド結合を有するレニン抑制ペプチド
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
KR0154872B1 (ko) 1987-12-21 1998-10-15 로버트 에이. 아미테이지 발아하는 식물종자의 아크로박테리움 매개된 형질전환
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
ES2096590T3 (es) 1989-06-29 1997-03-16 Medarex Inc Reactivos biespecificos para la terapia del sida.
US5019054A (en) 1989-11-06 1991-05-28 Mectra Labs, Inc. Medical device valving mechanism
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
US5098394A (en) 1990-05-31 1992-03-24 Luther Ronald B Biased shut off valve assembly for needle and catheter
ES2217250T3 (es) 1990-06-15 2004-11-01 Scios Inc. Mamifero transgenico, no humano que muestra la patologia de formacion amiloides de la enfermedad de alzheimer.
US5912410A (en) 1990-06-15 1999-06-15 Scios Inc. Transgenic non-human mice displaying the amyloid-forming pathology of alzheimer's disease
JPH05508855A (ja) 1990-07-06 1993-12-09 スミスクライン・ビーチャム・コーポレイション レトロウイルスプロテアーゼ阻害剤
US5176662A (en) 1990-08-23 1993-01-05 Minimed Technologies, Ltd. Subcutaneous injection set with improved cannula mounting arrangement
US5482947A (en) 1990-11-19 1996-01-09 Talley; John J. 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
ES2236682T5 (es) 1991-01-21 2011-03-31 Elan Pharmaceuticals, Inc. Ensayo y modelo para la enfermedad de alzheimer.
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
JPH06506463A (ja) 1991-04-04 1994-07-21 ジ・アップジョン・カンパニー Hivおよび他のレトロウイルスの治療に有用な化合物
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
AU671093B2 (en) 1992-01-07 1996-08-15 Elan Pharmaceuticals, Inc. Transgenic animal models for alzheimer's disease
EP0628035A4 (en) 1992-02-26 1995-03-29 Smithkline Beecham Corp RETROVIRAL PROTEASE INHIBITORS.
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
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
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
ES2123065T3 (es) 1992-08-25 1999-01-01 Searle & Co Hidroxietilamino-sulfonamidas utiles como inhibidores de proteasas retroviricas.
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
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.
EP0604182B1 (en) 1992-12-22 2000-10-11 Eli Lilly And Company Inhibitors of HIV protease useful for the treatment of Aids
US5484926A (en) 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US5545143A (en) 1993-01-21 1996-08-13 T. S. I. Medical Device for subcutaneous medication delivery
US5461067A (en) 1993-02-25 1995-10-24 Abbott Laboratories Retroviral protease inhibiting compounds
US5257980A (en) 1993-04-05 1993-11-02 Minimed Technologies, Ltd. Subcutaneous injection set with crimp-free soft cannula
US5300045A (en) 1993-04-14 1994-04-05 Plassche Jr Walter M Interventional needle having an automatically capping stylet
NZ264143A (en) 1993-08-09 1996-11-26 Lilly Co Eli Use of an aspartyl protease inhibitor to inhibit beta-amyloid peptide production
EP0715618B1 (en) 1993-08-24 1998-12-16 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
US5427145A (en) 1993-10-07 1995-06-27 Abbott Laboratories Connector with integral valve
CA2132277C (en) 1993-10-22 2005-05-10 Giorgio Cirelli Injection device
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
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
DK0708085T3 (da) 1994-10-19 2002-11-11 Novartis Ag Antivirale ethere af aspartatproteasesubstrat-isostere
US6001813A (en) 1994-11-21 1999-12-14 Cortech Inc. Val-pro containing α-keto oxadiazoles as serine protease inhibitors
DE4442352C1 (de) 1994-11-29 1995-12-21 Braun Melsungen Ag Ventilvorrichtung
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
US5863902A (en) 1995-01-06 1999-01-26 Sibia Neurosciences, Inc. Methods of treating neurodegenerative disorders using 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
CA2210889C (en) 1995-01-20 2007-08-28 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
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
US5565483A (en) 1995-06-07 1996-10-15 Bristol-Myers Squibb Company 3-substituted oxindole derivatives as potassium channel modulators
IE77523B1 (en) 1995-09-11 1997-12-17 Elan Med Tech Medicament delivery device
ZA9610374B (en) 1995-12-11 1997-06-23 Elan Med Tech Cartridge-based drug delivery device
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
US5922770A (en) 1996-07-22 1999-07-13 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
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
EP0958293B1 (en) 1997-02-04 2005-01-19 The Regents Of The University Of California Nanomolar, non-peptide inhibitors of cathepsin d
US5851197A (en) 1997-02-05 1998-12-22 Minimed Inc. Injector for a subcutaneous infusion set
US6093172A (en) 1997-02-05 2000-07-25 Minimed Inc. Injector for a subcutaneous insertion set
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
WO1998038167A1 (en) 1997-02-26 1998-09-03 Pfizer Inc. 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
US6186982B1 (en) 1998-05-05 2001-02-13 Elan Corporation, Plc Subcutaneous drug delivery device with improved filling system
IL132630A0 (en) 1997-05-08 2001-03-19 Smithkline Beecham Corp Protease inhibitors
US5968011A (en) 1997-06-20 1999-10-19 Maersk Medical A/S Subcutaneous injection set
US5962506A (en) 1997-07-07 1999-10-05 Pharmacopeia, Inc. Glycol and hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases
US6213973B1 (en) 1998-01-12 2001-04-10 C. R. Bard, Inc. Vascular access port with elongated septum
DE69943314D1 (de) 1998-02-12 2011-05-12 Kapil N Bhalla Sphingolipid-derivate und verfahren zu deren verwendung
US6095997A (en) 1998-03-04 2000-08-01 Corvascular, Inc. Intraluminal shunt and methods of use
US6056718A (en) 1998-03-04 2000-05-02 Minimed Inc. Medication infusion set
US5980506A (en) 1998-03-20 1999-11-09 Mathiasen; Orla Subcutaneous infusion device
DE19817461A1 (de) 1998-04-20 1999-10-21 Basf Ag Neue substituierte Benzamide, deren Herstellung und Anwendung
USD404482S (en) 1998-05-01 1999-01-19 Elan Medical Technologies Limited Drug delivery device
DE19821723C2 (de) 1998-05-14 2000-07-06 Disetronic Licensing Ag Katheterkopf für subkutane Verabreichung eines Wirkstoffs
PT1086076E (pt) 1998-06-19 2005-05-31 Vertex Pharma Inibidores de sulfonamida de aspartil protease
US6355021B1 (en) 1998-07-14 2002-03-12 Maersk Medical A/S Medical puncturing device
PL205294B1 (pl) 1998-09-24 2010-03-31 Upjohn Co Izolowany lub oczyszczony polipeptyd, oczyszczony lub izolowany polinukleotyd, wektor, wektor ekspresyjny, komórka gospodarza, sposób wytwarzania polipeptydu, sposoby identyfikowania czynnika obniżającego, modulującego lub hamującego aktywność, zastosowanie takiego czynnika, izolowany kwas nukleinowy, obejmujący go wektor i ich zastosowanie, sposoby zmniejszania komórkowego wytwarzania beta amyloidu i zastosowanie antysensownego reagenta
GB2364059B (en) 1999-02-10 2004-01-14 Elan Pharm Inc Beta-Secretase enzyme compositions and methods
JP2002539260A (ja) 1999-03-24 2002-11-19 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 アスパルチルプロテアーゼインヒビターを使用して神経変性障害を処置する方法
JP2002541801A (ja) 1999-04-09 2002-12-10 ヒューマン ジノーム サイエンシーズ, インコーポレイテッド 48個のヒト分泌タンパク質
US6419699B1 (en) 1999-04-14 2002-07-16 Mcghan Medical Corporation Universal implant fill connector
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
CA2374610A1 (en) 1999-06-28 2001-01-04 Jordan J. N. Tang Catalytically active recombinant memapsin and methods of use thereof
WO2001010387A2 (en) 1999-08-09 2001-02-15 Vanderbilt University Antiviral therapy use of p-glycoprotein modulators
CA2377221A1 (en) 1999-09-13 2001-03-22 Bristol-Myers Squibb Pharma Company Hydroxyalkanoyl aminolactams and related structures as inhibitors of a.beta. protein production
WO2001023533A2 (en) 1999-09-23 2001-04-05 Pharmacia & Upjohn Company Alzheimer's disease secretase, app substrates therefor, and uses therefor
GB9924957D0 (en) 1999-10-21 1999-12-22 Smithkline Beecham Plc Novel treatment
CA2395240A1 (en) 2000-01-13 2001-07-19 Genset S.A. Biallelic markers derived from genomic regions carrying genes involved in central nervous system disorders
DE60124080T2 (de) 2000-03-23 2007-03-01 Elan Pharmaceuticals, Inc., San Francisco Verbindungen und verfahren zur behandlung der alzheimerschen krankheit
JP2004502664A (ja) 2000-06-30 2004-01-29 イーラン ファーマスーティカルズ、インコーポレイテッド アルツハイマー病処置用化合物
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
US20030096864A1 (en) 2000-06-30 2003-05-22 Fang Lawrence Y. Compounds to treat alzheimer's disease
WO2002070037A2 (en) 2001-03-04 2002-09-12 Sterling Medivations, Inc. Infusion hub assembly and fluid line disconnect system
AU2002359376B2 (en) 2001-11-08 2008-01-10 Elan Pharmaceuticals, Inc. N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives

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