AU2001273094A1 - Compounds to treat alzheimer's disease - Google Patents

Compounds to treat alzheimer's disease

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Publication number
AU2001273094A1
AU2001273094A1 AU2001273094A AU7309401A AU2001273094A1 AU 2001273094 A1 AU2001273094 A1 AU 2001273094A1 AU 2001273094 A AU2001273094 A AU 2001273094A AU 7309401 A AU7309401 A AU 7309401A AU 2001273094 A1 AU2001273094 A1 AU 2001273094A1
Authority
AU
Australia
Prior art keywords
disease
compounds
treat alzheimer
alzheimer
treat
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
AU2001273094A
Inventor
James P. Beck
Andrea Gailunas
Roy Hom
Barbara Jagodzinska
Varghese John
Michel Maillaird
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pharmacia and Upjohn Co
Elan Pharmaceuticals LLC
Original Assignee
Pharmacia and Upjohn Co
Elan Pharmaceuticals LLC
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 Pharmacia and Upjohn Co, Elan Pharmaceuticals LLC, Upjohn Co filed Critical Pharmacia and Upjohn Co
Publication of AU2001273094A1 publication Critical patent/AU2001273094A1/en
Abandoned legal-status Critical Current

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    • C07D295/04Heterocyclic 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
    • C07D295/12Heterocyclic 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
    • C07D295/125Heterocyclic 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
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Abstract

The present invention is substituted amine s of formula (XV) useful in treating Alzheimer's ease and other similar disease.
AU2001273094A 2000-06-30 2001-06-29 Compounds to treat alzheimer's disease Abandoned AU2001273094A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US21532300P 2000-06-30 2000-06-30
US60/215,323 2000-06-30
PCT/US2001/020856 WO2002002518A2 (en) 2000-06-30 2001-06-29 Compounds to treat alzheimer's disease

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AU2001273094A1 true AU2001273094A1 (en) 2002-01-14

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AU2001271686A Abandoned AU2001271686A1 (en) 2000-06-30 2001-06-29 Compounds to treat alzheimer's disease
AU2001273113A Abandoned AU2001273113A1 (en) 2000-06-30 2001-06-29 Compounds to treat alzheimer's disease
AU2001273094A Abandoned AU2001273094A1 (en) 2000-06-30 2001-06-29 Compounds to treat alzheimer's disease

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AU2001271686A Abandoned AU2001271686A1 (en) 2000-06-30 2001-06-29 Compounds to treat alzheimer's disease
AU2001273113A Abandoned AU2001273113A1 (en) 2000-06-30 2001-06-29 Compounds to treat alzheimer's disease

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US (2) US7034182B2 (en)
EP (2) EP1299349B1 (en)
JP (2) JP2004502665A (en)
KR (1) KR20030058959A (en)
CN (1) CN1217920C (en)
AT (2) ATE314343T1 (en)
AU (3) AU2001271686A1 (en)
BR (1) BR0111980A (en)
CA (2) CA2410680A1 (en)
DE (2) DE60112942T2 (en)
ES (2) ES2248356T3 (en)
HK (1) HK1055721A1 (en)
MX (1) MXPA02012560A (en)
NZ (1) NZ523005A (en)
WO (3) WO2002002505A2 (en)
ZA (2) ZA200209991B (en)

Families Citing this family (99)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20020276A1 (en) 2000-06-30 2002-04-06 Elan Pharm Inc SUBSTITUTE AMINE COMPOUNDS AS ß-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER
US6846813B2 (en) * 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
US6696488B2 (en) 2000-08-11 2004-02-24 The Brigham And Women's Hospital, Inc. (Hydroxyethyl)ureas as inhibitors of alzheimer's β-amyloid production
AR035960A1 (en) 2001-04-23 2004-07-28 Elan Pharm Inc REPLACED EPOXIDS AND PROCESSES TO PREPARE THEM
EP1392645A2 (en) * 2001-05-22 2004-03-03 Elan Pharmaceuticals, Inc. Aza hydroxylated ethyl amine compounds
WO2002098849A2 (en) 2001-06-01 2002-12-12 Elan Pharmaceuticals, Inc. Hydroxy alkyl amine derivatives as beta-secretase inhibitors and their use for the treatment of alzheimer’s disease and similar diseases
JP2005506979A (en) * 2001-08-28 2005-03-10 ファルマシア アンド アップジョン カンパニー リミティド ライアビリティー カンパニー Method of treating Alzheimer's disease using quinaldyl-amine derivatives of oxo-substituted and hydroxy-substituted hydrocarbons
AP2004003049A0 (en) 2001-11-08 2004-06-30 Elan Pharm Inc N,N' -substituted-1,3-diamino -2-hydroxypropane derivatives.
CA2467798A1 (en) * 2001-11-19 2003-05-30 Pharmacia & Upjohn Company Amine 1,2- and 1,3-diol compounds and their use for treatment of alzheimer's disease
CA2469130A1 (en) * 2001-12-04 2003-06-12 Elan Pharmaceuticals, Inc. Peptide isosteres containing a heterocycle useful in the treatment of alzheimer's disease
BR0214736A (en) 2001-12-06 2004-11-23 Elan Pharm Inc Compound and its pharmaceutically acceptable salts, pharmaceutical composition and method of treating humans or animals suffering from diseases or conditions
JP4354180B2 (en) * 2001-12-26 2009-10-28 武田薬品工業株式会社 Mild cognitive impairment treatment
US7115652B2 (en) 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
AU2003276047A1 (en) 2002-06-17 2003-12-31 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
US7459476B2 (en) 2002-06-27 2008-12-02 Elan Pharmaceuticals, Inc. Methods for treating Alzheimer's disease using hydroxyethylene compounds containing a heterocyclic amide bond isostere
US7557137B2 (en) * 2002-08-05 2009-07-07 Bristol-Myers Squibb Company Gamma-lactams as beta-secretase inhibitors
CA2494585A1 (en) * 2002-08-07 2004-02-19 Novartis Ag Methods for the treatment of dementia based on apo e genotype
AU2003254844A1 (en) * 2002-08-09 2004-02-25 Takeda Chemical Industries, Ltd. Substituted amino compounds and use thereof
US7294642B2 (en) * 2002-09-06 2007-11-13 Elan Pharmaceuticals, Inc. 1,3-Diamino-2-hydroxypropane pro-drug derivatives
JP2005538177A (en) * 2002-09-10 2005-12-15 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 Substituted amino ether compounds for the treatment of Alzheimer's disease
UY27967A1 (en) * 2002-09-10 2004-05-31 Pfizer 2-HINDROXI-1,3-DIAMINOALCANE OIL
DE60329316D1 (en) 2002-11-12 2009-10-29 Merck & Co Inc PHENYL ACARBOXAMIDE AS A BETA SEKRETASE INHIBITOR FOR THE TREATMENT OF ALZHEIMER
US7351738B2 (en) * 2002-11-27 2008-04-01 Elan Pharmaceuticals, Inc. Substituted ureas and carbamates
GB0228410D0 (en) * 2002-12-05 2003-01-08 Glaxo Group Ltd Novel Compounds
US7521481B2 (en) 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
GB0305918D0 (en) * 2003-03-14 2003-04-23 Glaxo Group Ltd Novel compounds
CL2004000849A1 (en) * 2003-04-21 2005-01-28 Elan Pharmaceuticals Inc Pharm COMPOUNDS DERIVED FROM BENZAMIDAS-2-HIDROXI-3-DIAMINOALCANS, USEFUL FOR THE TREATMENT OR PREVENTION OF ALZHEIMER, DOWN SYNDROME, HEREDITARY CEREBRAL HEMORRAGY, DEGENERATIVE DEMENCIES AND OTHERS.
CL2004000848A1 (en) * 2003-04-21 2005-01-28 Elan Pharmaceuticals Inc Pharm COMPOUNDS DERIVED FROM FENACIL-2-HIDROXI-3-DIAMINOALCANS, INHIBITORS OF THE ENZYME BETASECRETASA, USEFUL TO PREPARE A MEDICINAL PRODUCT TO TREAT ALZHEIMER, DOWN SYNDROME, HEREDITAR CEREBRAL HERIDAL AND OEREDOS
GB0309221D0 (en) * 2003-04-23 2003-06-04 Glaxo Group Ltd Novel compounds
CN100430377C (en) * 2003-06-30 2008-11-05 麦克公司 N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
MXPA06001558A (en) 2003-08-08 2006-05-15 Schering Corp Cyclic amine base-1 inhibitors having a heterocyclic substituent.
US7662816B2 (en) 2003-08-08 2010-02-16 Schering Corporation Cyclic amine BACE-1 inhibitors having a benzamide substituent
GB0328900D0 (en) * 2003-12-12 2004-01-14 Glaxo Group Ltd Novel compounds
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
FR2866647B1 (en) * 2004-02-20 2006-10-27 Servier Lab NOVEL AZABICYCLIC DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
MXPA06010899A (en) * 2004-03-25 2006-12-15 Elan Pharm Inc 2-amino- and 2-thio-substituted 1,3-diaminopropanes.
WO2006014762A1 (en) * 2004-07-22 2006-02-09 Schering Corporation Substituted amide beta secretase inhibitors
US7361789B1 (en) 2004-07-28 2008-04-22 Amgen Inc. Dihydronaphthalene compounds, compositions, uses thereof, and methods for synthesis
ES2306200T3 (en) 2004-07-28 2008-11-01 Schering Corporation BETA-SECRETASA MACROCICLIC INHIBITORS.
EP1797052A1 (en) * 2004-09-17 2007-06-20 Comentis, Inc. Bicyclic compounds which inhibit beta-secretase activity and methods of use thereof
US20070213368A1 (en) * 2004-09-21 2007-09-13 Kleinman Edward F N-ethyl hydroxyethylamine useful in treating cns conditions
CA2581023A1 (en) 2004-09-21 2006-03-30 Pfizer Products Inc. N-methyl hydroxyethylamine useful in treating cns conditions
US7745470B2 (en) 2005-03-10 2010-06-29 Bristol-Myers Squibb Company Isophthalates as beta-secretase inhibitors
GB0506562D0 (en) * 2005-03-31 2005-05-04 Glaxo Group Ltd Novel compounds
JP2008535863A (en) * 2005-04-08 2008-09-04 コメンティス,インコーポレーテッド Compounds that inhibit β-secretase activity and methods of use thereof
WO2007020888A1 (en) 2005-08-12 2007-02-22 Takeda Pharmaceutical Company Limited Brain/neuronal cell-protecting agent, and therapeutic agent for sleep disorder
US7745484B2 (en) 2005-11-21 2010-06-29 Amgen Inc. Beta-secretase modulators and methods of use
US7872009B2 (en) 2005-11-21 2011-01-18 Amgen Inc. Beta-Secretase modulators and methods of use
US7838676B2 (en) 2005-11-21 2010-11-23 Amgen Inc. Beta-secretase modulators and methods of use
CA2629402C (en) 2005-11-21 2011-07-26 Amgen Inc. Beta-secretase modulators and methods of use
PE20080145A1 (en) * 2006-03-21 2008-02-11 Janssen Pharmaceutica Nv TETRAHYDRO-PYRIMIDOAZEPINE AS MODULATORS OF TRPV1
WO2007110727A2 (en) * 2006-03-27 2007-10-04 Pfizer Products Inc. Amide stabilized hydroxyethylamines
GB0607952D0 (en) * 2006-04-21 2006-05-31 Minster Res Ltd Novel treatment
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
SI2091948T1 (en) 2006-11-30 2012-07-31 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
US8093254B2 (en) 2006-12-12 2012-01-10 Schering Corporation Aspartyl protease inhibitors
EP2121633A2 (en) 2007-02-12 2009-11-25 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
EP2481408A3 (en) 2007-03-01 2013-01-09 Probiodrug AG New use of glutaminyl cyclase inhibitors
DK2142514T3 (en) 2007-04-18 2015-03-23 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
EP2167471B1 (en) 2007-05-25 2013-10-16 Amgen Inc. Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
CL2008001500A1 (en) 2007-05-25 2008-12-26 Amgen Inc Compounds derived from substituted hydroxyethyl amine, betasecretase modulators; process of preparation of said c omposites; pharmaceutical composition that includes them; and its use to treat a neurological disorder, such as Alzheimer's, down syndrome, degenerative dementia, among others.
CA2697166A1 (en) * 2007-07-26 2009-01-29 Comentis, Inc. Isophthalamide derivatives inhibiting betasecretase activity
KR20100059919A (en) 2007-09-24 2010-06-04 코멘티스, 인코포레이티드 (3-hydroxy-4-amino-butan-2-yl)-3-(2-thiazol-2-yl-pyrrolidine-1-carbonyl) benzamide derivatives and related compounds as beta-secretase inhibitors for treating
SE531873C2 (en) * 2007-11-12 2009-09-01 Lifeassays Ab Device for biochemical processing and analysis of sample liquid
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
PE20091102A1 (en) 2007-12-17 2009-07-25 Janssen Pharmaceutica Nv IMIDAZOLO-, OXAZOLO-, AND THIAZOLOPYRIMIDINE MODULATORS OF TRPV1
WO2009128057A2 (en) 2008-04-18 2009-10-22 UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN et al Psycho-pharmaceuticals
CN102065897B (en) * 2008-04-29 2013-11-13 法奈科斯公司 New therapeutic approaches for treating alzheimer disease and related disorders through a modulation of cell stress response
EP3586839A1 (en) 2008-07-28 2020-01-01 Blanchette Rockefeller Neurosciences, Institute Pkc-activating compounds for the treatment of neurodegenerative diseases
US8426447B2 (en) * 2008-09-11 2013-04-23 Amgen Inc. Spiro-tricyclic ring compounds as beta-secretase modulators and methods of use
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
BRPI1010639A2 (en) * 2009-05-13 2016-03-15 Protein Delivery Solutions Llc pharmaceutical system for transmembrane distribution
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
AU2010294214B2 (en) 2009-09-11 2015-05-07 Vivoryon Therapeutics N.V. Heterocylcic derivatives as inhibitors of glutaminyl cyclase
EP2504330A1 (en) 2009-11-23 2012-10-03 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
US9296698B2 (en) 2009-11-23 2016-03-29 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
CA2788363A1 (en) 2010-01-19 2011-07-28 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
JP2013518882A (en) * 2010-02-05 2013-05-23 ファイザー・インク Pyrrolo [2,3-d] pyrimidine urea compounds as JAK inhibitors
JP6026284B2 (en) 2010-03-03 2016-11-16 プロビオドルグ エージー Inhibitors of glutaminyl cyclase
AU2011226074B2 (en) 2010-03-10 2015-01-22 Vivoryon Therapeutics N.V. Heterocyclic inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5)
JP5584352B2 (en) 2010-03-15 2014-09-03 アムジエン・インコーポレーテツド Amino-dihydrooxazine and amino-dihydrothiazine spiro compounds as β-secretase modulators and their medical use
US8883782B2 (en) 2010-03-15 2014-11-11 Amgen Inc. Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
WO2012069428A1 (en) 2010-11-22 2012-05-31 Noscira, S.A. Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions
EP2673279A1 (en) 2011-02-07 2013-12-18 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
JP6050264B2 (en) 2011-03-16 2016-12-21 プロビオドルグ エージー 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
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9302992B2 (en) * 2013-04-02 2016-04-05 Annji Pharmaceutical Co., Ltd. Multifunctional quinoline derivatives as anti-neurodegenerative agents
CN106748892B (en) * 2017-01-18 2018-09-18 四川大学 Target autophagy agonist and its application in neurodegenerative disease therapeutic agent
US11833156B2 (en) 2017-09-22 2023-12-05 Jubilant Epipad LLC Heterocyclic compounds as pad inhibitors
PL3461819T3 (en) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitors of glutaminyl cyclase
FI3697785T3 (en) 2017-10-18 2023-04-03 Jubilant Epipad LLC Imidazo-pyridine compounds as pad inhibitors
EP3707135A1 (en) 2017-11-06 2020-09-16 Jubilant Prodel LLC Pyrimidine derivatives as inhibitors of pd1/pd-l1 activation
JP7368369B2 (en) 2017-11-24 2023-10-24 ジュビラント・エピスクライブ・エルエルシー Heterocyclic compounds as PRMT5 inhibitors
JP7279063B6 (en) 2018-03-13 2024-02-15 ジュビラント プローデル エルエルシー Bicyclic compounds as inhibitors of PD1/PD-L1 interaction/activation

Family Cites Families (104)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5753564Y2 (en) 1977-06-01 1982-11-19
CH624011A5 (en) 1977-08-05 1981-07-15 Battelle Memorial Institute
FR2416008A1 (en) 1978-02-02 1979-08-31 Oreal LIPOSOME LYOPHILISATES
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
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
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
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
US4736866B1 (en) 1984-06-22 1988-04-12 Transgenic non-human mammals
JPH0662529B2 (en) 1984-07-13 1994-08-17 三共株式会社 Amino acid derivative
US4880781A (en) 1984-08-06 1989-11-14 The Upjohn Company Renin inhibitory peptides containing an N-alkyl-histidine moiety
JPS6150912A (en) 1984-08-16 1986-03-13 Shionogi & Co Ltd Production of liposome preparation
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
DE3610593A1 (en) 1986-03-29 1987-10-01 Hoechst Ag SUBSTITUTED 4-AMINO-3-HYDROXYBUTTERIC ACID DERIVATIVES METHOD FOR THE PRODUCTION THEREOF, THE CONTAINERS THEREOF AND THEIR USE
US4935405A (en) * 1986-10-31 1990-06-19 Pfizer Inc. Nor-statine and nor-cyclostatine polypeptides
US5250565A (en) 1987-02-10 1993-10-05 Abbott Laboratories Indole-,benzofuran-,and benzothiophene-containing lipoxygenase-inhibiting compounds
DE3721855A1 (en) 1987-03-12 1988-09-22 Merck Patent Gmbh AMINO ACID DERIVATIVES
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
GB8927915D0 (en) * 1989-12-11 1990-02-14 Hoffmann La Roche Novel alcohols
DE3941235A1 (en) 1989-12-14 1991-06-20 Bayer Ag NEW PEPTIDES, THEIR PREPARATION AND THEIR USE IN MEDICINAL PRODUCTS
DE4003575A1 (en) 1990-02-07 1991-08-08 Bayer Ag RETROISOSTERIC DIPEPTIDES, METHOD FOR THE PREPARATION AND THEIR USE AS RENININHIBITORS IN MEDICAMENTS
GB9004483D0 (en) 1990-02-28 1990-04-25 Erba Carlo Spa New aryl-and heteroarylethenylene derivatives and process for their preparation
WO1991019810A1 (en) 1990-06-15 1991-12-26 California Biotechnology Inc. Transgenic non-human mammal displaying the amyloid-forming pathology of alzheimer's disease
US5912410A (en) 1990-06-15 1999-06-15 Scios Inc. Transgenic non-human mice displaying the amyloid-forming pathology of alzheimer's disease
US5648511A (en) 1990-11-19 1997-07-15 G.D. Searle & Co. Method for making intermediates useful in the synthesis of retroviral protease inhibitors
US5510378A (en) 1990-11-19 1996-04-23 G.D. Searle & Co. Retroviral protease inhibitors
US5482947A (en) 1990-11-19 1996-01-09 Talley; John J. Retroviral protease inhibitors
JP3510244B2 (en) 1991-01-21 2004-03-22 エラン ファーマシューティカルス,インコーポレイテッド Tests and models 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
US5753652A (en) 1991-07-03 1998-05-19 Novartis Corporation Antiretroviral hydrazine derivatives
ES2093237T3 (en) * 1991-07-03 1996-12-16 Ciba Geigy Ag DERIVATIVES OF HYDRAZINE PHARMACOLOGICALLY ACTIVE AND PROCEDURE FOR THEIR OBTAINING.
US5516784A (en) 1991-08-13 1996-05-14 Schering Corporation Anti-HIV (AIDS) agents
WO1993014200A1 (en) 1992-01-07 1993-07-22 Tsi Corporation Transgenic animal models for alzheimer's disease
DE69333270T2 (en) 1992-03-11 2004-08-05 Narhex Ltd. AMINE DERIVATIVES OF OXO AND HYDROXY SUBSTITUTED CARBON HYDROGEN
ES2066623T3 (en) 1992-03-13 1995-03-01 Bio Mega Boehringer Ingelheim SUBSTITUTED DERIVATIVES OF PIPECOLINIC ACID AS HIV-PROTEASE INHIBITORS.
US5502187A (en) 1992-04-03 1996-03-26 The Upjohn Company Pharmaceutically active bicyclic-heterocyclic amines
US5441870A (en) 1992-04-15 1995-08-15 Athena Neurosciences, Inc. Methods for monitoring cellular processing of β-amyloid precursor protein
US5604102A (en) 1992-04-15 1997-02-18 Athena Neurosciences, Inc. Methods of screening for β-amyloid peptide production inhibitors
US5376542A (en) 1992-04-27 1994-12-27 Georgetown University Method for producing immortalized cell lines using human papilluma virus genes
US5766846A (en) 1992-07-10 1998-06-16 Athena Neurosciences Methods of screening for compounds which inhibit soluble β-amyloid peptide production
US5760076A (en) 1992-08-25 1998-06-02 G.D Searle & Co. Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
DK0656887T3 (en) 1992-08-25 1999-07-05 Searle & Co Hydroxyethylaminosulfonamides for use as inhibitors of retroviral proteases
CA2140928C (en) 1992-08-25 2008-01-29 Michael L. Vazquez Sulfonylalkanoylamino 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
DE69329544T2 (en) 1992-12-22 2001-05-31 Lilly Co Eli HIV protease inhibiting compounds
US5484926A (en) 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US5461067A (en) 1993-02-25 1995-10-24 Abbott Laboratories Retroviral protease inhibiting compounds
NZ264143A (en) * 1993-08-09 1996-11-26 Lilly Co Eli Use of an aspartyl protease inhibitor to inhibit beta-amyloid peptide production
CA2174429C (en) 1993-10-27 2011-08-30 Lisa C. Mcconlogue Transgenic animals harboring app allele having swedish mutation
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
EP0708085B1 (en) 1994-10-19 2002-07-17 Novartis AG Antiviral ethers of aspartate protease substrate isosteres
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
US6017887A (en) 1995-01-06 2000-01-25 Sibia Neurosciences, Inc. Peptide, peptide analog and amino acid analog protease inhibitors
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
ID18218A (en) 1995-01-27 1998-03-19 Novo Nordisk As COMPOUND WITH GROWTH HORMONE EXTENSION
US5545640A (en) 1995-04-04 1996-08-13 Bio-Mega/Boehringer Ingeleheim Research Inc. Protease inhibiting succinic acid derivatives
JPH11507538A (en) 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-secretase, antibodies to β-secretase, and assays for detecting β-secretase inhibition
US5744346A (en) 1995-06-07 1998-04-28 Athena Neurosciences, Inc. β-secretase
US5565483A (en) 1995-06-07 1996-10-15 Bristol-Myers Squibb Company 3-substituted oxindole derivatives as potassium channel modulators
ATE218538T1 (en) 1995-11-21 2002-06-15 Novartis Erfind Verwalt Gmbh AZAHEXANE DERIVATIVES AS SUBSTRATISOSTERS OF RETROVIRAL ASPARTATE PROTEASES
US5886046A (en) 1996-01-19 1999-03-23 The Trustees Of The University Of Pennsylvania Dicarbonyl-containing compounds
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
EP0923539B1 (en) 1996-07-22 2002-06-05 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
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
AU749281B2 (en) * 1997-02-04 2002-06-20 Regents Of The University Of California, The 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
US6221670B1 (en) 1997-03-21 2001-04-24 Scios Inc. Methods to identify β-amyloid reducing agents
US5962506A (en) 1997-07-07 1999-10-05 Pharmacopeia, Inc. Glycol and hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases
EP1086076B1 (en) * 1998-06-19 2004-12-22 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease
US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
PE20020276A1 (en) 2000-06-30 2002-04-06 Elan Pharm Inc SUBSTITUTE AMINE COMPOUNDS AS ß-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER
EP1392645A2 (en) 2001-05-22 2004-03-03 Elan Pharmaceuticals, Inc. Aza hydroxylated ethyl amine compounds
WO2002098849A2 (en) 2001-06-01 2002-12-12 Elan Pharmaceuticals, Inc. Hydroxy alkyl amine derivatives as beta-secretase inhibitors and their use for the treatment of alzheimer’s disease and similar diseases
AP2004003049A0 (en) 2001-11-08 2004-06-30 Elan Pharm Inc N,N' -substituted-1,3-diamino -2-hydroxypropane derivatives.

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