BR0111980A - Amina substituìda, composto protegido, métodos para tratar um paciente que tenha ou para prevenir que um paciente contraia uma doença ou condição, para inibir a atividade da beta-secretase, para inibir a clivagem da proteìna precursora de amilóide (app), para inibir a produção do peptìdeo beta amilóide (a beta) em uma célula, para inibir a produção de placa beta0amilóide em um animal, e para tratar ou prevenir uma doença compreendendo depósitos de beta-amilóide no cérebro, composição método para produzir um complexo de beta-secretase, conjunto, e, uso de amina substituìda - Google Patents

Amina substituìda, composto protegido, métodos para tratar um paciente que tenha ou para prevenir que um paciente contraia uma doença ou condição, para inibir a atividade da beta-secretase, para inibir a clivagem da proteìna precursora de amilóide (app), para inibir a produção do peptìdeo beta amilóide (a beta) em uma célula, para inibir a produção de placa beta0amilóide em um animal, e para tratar ou prevenir uma doença compreendendo depósitos de beta-amilóide no cérebro, composição método para produzir um complexo de beta-secretase, conjunto, e, uso de amina substituìda

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Publication number
BR0111980A
BR0111980A BR0111980-0A BR0111980A BR0111980A BR 0111980 A BR0111980 A BR 0111980A BR 0111980 A BR0111980 A BR 0111980A BR 0111980 A BR0111980 A BR 0111980A
Authority
BR
Brazil
Prior art keywords
beta
inhibiting
disease
patient
substituted amine
Prior art date
Application number
BR0111980-0A
Other languages
English (en)
Inventor
Lawrence Y Fang
Varghese John
Original Assignee
Elan Pharm Inc
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 filed Critical Elan Pharm Inc
Publication of BR0111980A publication Critical patent/BR0111980A/pt

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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
    • C07D295/13Heterocyclic 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
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Abstract

"AMINA SUBSTITUìDA, COMPOSTO PROTEGIDO, MéTODOS PARA TRATAR UM PACIENTE QUE TENHA OU PARA PREVENIR QUE UM PACIENTE CONTRAIA UMA DOENçA OU CONDIçãO, PARA INIBIR A ATIVIDADE DA BETA-SECRETASE, PARA INIBIR A CLIVAGEM DA PROTEìNA PRECURSORA DE AMELóIDE (APP), PARA INIBIR A PRODUçãO DO PEPTìDEO BETA AMILóIDE (A BETA) EM UMA CéLULA, PARA INIBIR A PRODUçãO DE PLACA BETA-AMILóIDE EM UM ANIMAL E PARA TRATAR OU PREVENIR UMA DOENçA COMPREENDENDO DEPóSITOS DE BETA-AMILóIDE NO CéREBRO, COMPOSIçãO, MéTODO PARA PRODUZIR UM COMPLEXO DE BETA-SECRETASE, CONJUNTO, E, USO DE UMA AMINA SUBSTITUìDA". A presente invenção são aminas substituídas da fórmula (XV): úteis no tratamento da doença de Alzheimer e de outras doenças similares.
BR0111980-0A 2000-06-30 2001-06-29 Amina substituìda, composto protegido, métodos para tratar um paciente que tenha ou para prevenir que um paciente contraia uma doença ou condição, para inibir a atividade da beta-secretase, para inibir a clivagem da proteìna precursora de amilóide (app), para inibir a produção do peptìdeo beta amilóide (a beta) em uma célula, para inibir a produção de placa beta0amilóide em um animal, e para tratar ou prevenir uma doença compreendendo depósitos de beta-amilóide no cérebro, composição método para produzir um complexo de beta-secretase, conjunto, e, uso de amina substituìda BR0111980A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US21532300P 2000-06-30 2000-06-30
PCT/US2001/020930 WO2002002506A2 (en) 2000-06-30 2001-06-29 Compounds to treat alzheimer's disease

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Families Citing this family (99)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2002014264A2 (en) * 2000-08-11 2002-02-21 The Brigham And Women's Hospital, Inc. (hydroxyethyl)ureas as inhibitors of alzheimer's beta-amyloid production
AR035960A1 (es) * 2001-04-23 2004-07-28 Elan Pharm Inc Epoxidos sustituidos y procesos para prepararlos
CA2448084A1 (en) * 2001-05-22 2002-11-28 Elan Pharmaceuticals, Inc. Aza hydroxylated ethyl amine compounds
MXPA03011046A (es) 2001-06-01 2004-06-25 Elan Pharm Inc Hidroxialquilaminas.
BR0212242A (pt) * 2001-08-28 2004-07-20 Upjohn Co Métodos para tratar ou previnir mal de alzheimer e uma doença, tratar mal de alzheimer e um indivìduo que tem ou para evitar que um paciente adquira uma doença ou condição, para inibir a atividade de beta-secretase, a clivagem de um isotipo de proteìna de precursor de amilóide e a produção de peptìdeo beta amilóide em uma célula e de placa beta-amilóide em um animal, para produzir um complexo beta-secretase, composição e uso de um composto
OA12846A (en) * 2001-11-08 2006-09-15 Elan Pharm Inc N,N'-substituted-1,3-diamino-2-hydroxypropane derivatives.
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
WO2003047576A1 (en) * 2001-12-04 2003-06-12 Elan Pharmaceuticals, Inc. Peptide isosteres containing a heterocycle useful in the treatment of alzheimer's disease
WO2003050073A1 (en) * 2001-12-06 2003-06-19 Elan Pharmaceuticals, Inc. Substituted hydroxyethylamines
EP1459764A4 (en) * 2001-12-26 2006-08-16 Takeda Pharmaceutical REMEDIES AGAINST LIGHT COGNITIVE DISORDERS
US7115652B2 (en) 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
EP1515944A1 (en) 2002-06-17 2005-03-23 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
AU2003247758A1 (en) * 2002-06-27 2004-01-19 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
DE60328198D1 (de) * 2002-08-07 2009-08-13 Novartis Ag Verfahren zur Vorhersage des Behandlungserfolgs mit Rivastigmine basierend auf einer Bestimmung des ApoE Genotyps eines Demenzkranken
AU2003254844A1 (en) * 2002-08-09 2004-02-25 Takeda Chemical Industries, Ltd. Substituted amino compounds and use thereof
CN1732161A (zh) * 2002-09-06 2006-02-08 艾伦药物公司 1,3-二氨基-2-羟基丙烷前体药物衍生物
UY27967A1 (es) * 2002-09-10 2004-05-31 Pfizer Acetil 2-hindroxi-1,3-diaminoalcanos
BR0314180A (pt) * 2002-09-10 2005-08-09 Pharmacia & Upjohn Co Llc Aminoéteres substituìdos para o tratamento da doença de alzheimer
US7109217B2 (en) 2002-11-12 2006-09-19 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
EP1565428A1 (en) * 2002-11-27 2005-08-24 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
UY28279A1 (es) * 2003-04-21 2004-11-30 Pharmacia & Amp Fenacilo 2 -hidroxi - 3 - diaminoalcanos
UY28280A1 (es) * 2003-04-21 2004-11-30 Pharmacia & Amp 2- hidroxi - 3- diaminoalcanos de benzamida
GB0309221D0 (en) * 2003-04-23 2003-06-04 Glaxo Group Ltd Novel compounds
CA2529994A1 (en) 2003-06-30 2005-01-20 Merck & Co., Inc. N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
AR045218A1 (es) 2003-08-08 2005-10-19 Schering Corp Aminas ciclicas inhibidoras de bace-1 que poseen una benzamida sustituyente; composiciones farmaceuticas que las contienen y su uso en la fabricacion de medicamentos para tratar enfermedades cognitivas o neurodegenerativas.
JP4472700B2 (ja) 2003-08-08 2010-06-02 シェーリング コーポレイション 複素環置換基を有する環状アミンbase−1阻害剤
GB0328900D0 (en) * 2003-12-12 2004-01-14 Glaxo Group Ltd Novel compounds
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
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
FR2866647B1 (fr) * 2004-02-20 2006-10-27 Servier Lab Nouveaux derives azabicycliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2005095326A2 (en) * 2004-03-25 2005-10-13 Elan Pharmaceuticals, Inc. 2-amino- and 2-thio-substituted 1,3-diaminopropanes
ES2355733T3 (es) 2004-07-22 2011-03-30 Schering Corporation Inhibidores de amida beta-secretasa sustituidos.
US7361789B1 (en) 2004-07-28 2008-04-22 Amgen Inc. Dihydronaphthalene compounds, compositions, uses thereof, and methods for synthesis
JP2008508289A (ja) 2004-07-28 2008-03-21 シェーリング コーポレイション 大環状βセクレターゼ阻害剤
CA2580238A1 (en) * 2004-09-17 2006-03-30 Comentis, Inc. Bicyclic compounds which inhibit beta-secretase activity and methods of use thereof
BRPI0515383A (pt) * 2004-09-21 2008-07-22 Pfizer Prod Inc n-etil hidroxietilamina útil no tratamento de condições do snc
WO2006032999A1 (en) 2004-09-21 2006-03-30 Pfizer Products Inc. N-methyl hydroxyethylamine useful in treating cns conditions
US7745470B2 (en) 2005-03-10 2010-06-29 Bristol-Myers Squibb Company Isophthalates as beta-secretase inhibitors
GB0506562D0 (en) * 2005-03-31 2005-05-04 Glaxo Group Ltd Novel compounds
BRPI0607019A2 (pt) * 2005-04-08 2009-07-28 Univ Illinois compostos que inibem a atividade de beta -secretase e métodos de uso dos mesmos
US7812025B2 (en) 2005-08-12 2010-10-12 Takeda Pharmaceutical Company Limited Brain/neuronal cell-protecting agent and therapeutic agent for sleep disorder
US7838676B2 (en) 2005-11-21 2010-11-23 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
JP5274258B2 (ja) 2005-11-21 2013-08-28 アムジエン・インコーポレーテツド β−セクレターゼ調節物質及び使用方法
US7745484B2 (en) 2005-11-21 2010-06-29 Amgen Inc. Beta-secretase modulators and methods of use
PE20080145A1 (es) * 2006-03-21 2008-02-11 Janssen Pharmaceutica Nv Tetrahidro-pirimidoazepinas como moduladores de trpv1
WO2007110727A2 (en) * 2006-03-27 2007-10-04 Pfizer Products Inc. Amide stabilized hydroxyethylamines
GB0607952D0 (en) * 2006-04-21 2006-05-31 Minster Res Ltd Novel treatment
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
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
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
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
EP2865670B1 (en) 2007-04-18 2017-01-11 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
CA2687608C (en) 2007-05-25 2013-07-02 Amgen Inc. Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
US8163909B2 (en) 2007-05-25 2012-04-24 Amgen Inc. Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
MX2010000956A (es) * 2007-07-26 2010-03-01 Comentis Inc Derivados de isoftalamida que inhiben actividad de beta-secretasa.
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
SE531873C2 (sv) * 2007-11-12 2009-09-01 Lifeassays Ab Anordning för biokemisk bearbetning och analys av provvätska
US7803809B2 (en) 2008-11-12 2010-09-28 Amgen Inc. Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use
EP2224929B1 (en) 2007-12-17 2016-05-04 Janssen Pharmaceutica, N.V. Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of trpv1
US8461389B2 (en) 2008-04-18 2013-06-11 University College Dublin, National University Of Ireland, Dublin Psycho-pharmaceuticals
DK2282779T3 (da) * 2008-04-29 2013-05-27 Pharnext Nye terapeutiske fremgangsmåder til behandling af alzheimer sygdom og beslægtede lidelser gennem en modulation af cellestress-respons
ES2683021T3 (es) 2008-07-28 2018-09-24 Blanchette Rockefeller Neurosciences Institute Compuestos activadores de la PKC para el tratamiento de enfermedades neurodegenerativas
AU2009291602B2 (en) * 2008-09-11 2013-02-14 Amgen Inc. Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
SG176000A1 (en) * 2009-05-13 2011-12-29 Protein Delivery Solutions Llc Pharmaceutical system for trans-membrane delivery
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
EP2475428B1 (en) 2009-09-11 2015-07-01 Probiodrug AG 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
EP2504315A1 (en) 2009-11-23 2012-10-03 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
WO2011090911A1 (en) 2010-01-19 2011-07-28 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
CN102822177A (zh) * 2010-02-05 2012-12-12 美国辉瑞有限公司 吡咯并[2,3-d]嘧啶脲化合物
ES2586231T3 (es) 2010-03-03 2016-10-13 Probiodrug Ag Inhibidores de glutaminil ciclasa
CN102791704B (zh) 2010-03-10 2015-11-25 前体生物药物股份公司 谷氨酰胺酰环化酶(qc, ec 2.3.2.5)的杂环抑制剂
WO2011115928A1 (en) 2010-03-15 2011-09-22 Amgen Inc. Amino -dihydrooxazine and amino - dihydrothiazine spiro compounds as beta - 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
US9284296B2 (en) 2010-11-22 2016-03-15 Aubergine Pharmaceuticals Llc Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions
WO2012109165A1 (en) 2011-02-07 2012-08-16 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
US8530670B2 (en) 2011-03-16 2013-09-10 Probiodrug Ag Inhibitors
US9296759B2 (en) 2011-09-21 2016-03-29 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9302992B2 (en) * 2013-04-02 2016-04-05 Annji Pharmaceutical Co., Ltd. Multifunctional quinoline derivatives as anti-neurodegenerative agents
CN106748892B (zh) * 2017-01-18 2018-09-18 四川大学 靶向自噬激动剂及其在神经退行性疾病治疗药物中的应用
CN111108105B (zh) 2017-09-22 2023-03-31 朱比兰特埃皮帕德有限公司 作为pad抑制剂的杂环化合物
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
WO2019077631A1 (en) 2017-10-18 2019-04-25 Jubilant Biosys Limited IMIDAZO-PYRIDINE COMPOUNDS FOR USE AS PAD INHIBITORS
KR20200085836A (ko) 2017-11-06 2020-07-15 주빌런트 프로델 엘엘씨 Pd1/pd-l1 활성화 억제제로서의 피리미딘 유도체
BR112020010322A2 (pt) 2017-11-24 2020-11-17 Jubilant Episcribe Llc composto da fórmula i; composto da fórmula ia; composto da fórmula ib; processo de preparação de compostos da fórmula i; composição farmacêutica; método para o tratamento e/ou prevenção de várias doenças; uso dos compostos; método para o tratamento de câncer; e método para o tratamento e/ou prevenção de uma afecção mediada por prmt5 ou um distúrbio proliferativo ou câncer
WO2019175897A1 (en) 2018-03-13 2019-09-19 Jubilant Biosys Limited 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 (pt) 1977-06-01 1982-11-19
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
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 (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
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
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 (de) 1987-03-12 1988-09-22 Merck Patent Gmbh Aminosaeurederivate
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 (de) 1989-12-14 1991-06-20 Bayer Ag Neue peptide, ihre herstellung und ihre verwendung in arzneimitteln
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
EP0647268B1 (en) 1990-06-15 2004-03-03 Scios 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
US5482947A (en) 1990-11-19 1996-01-09 Talley; John J. Retroviral protease inhibitors
US5708004A (en) 1990-11-19 1998-01-13 Monsanto Company 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
US5753652A (en) 1991-07-03 1998-05-19 Novartis Corporation Antiretroviral hydrazine derivatives
DE59207226D1 (de) * 1991-07-03 1996-10-31 Ciba Geigy Ag Pharmakologisch wirksame Hydrazinderivate und Verfahren zu deren Herstellung
US5516784A (en) 1991-08-13 1996-05-14 Schering Corporation Anti-HIV (AIDS) agents
JPH07506720A (ja) 1992-01-07 1995-07-27 アテナ ニューロサイエンシーズ, インコーポレイテッド アルツハイマー病のトランスジェニック動物モデル
ATE253050T1 (de) * 1992-03-11 2003-11-15 Narhex Ltd Aminderivate von oxo- und hydroxy- substituierten kohlenwasserstoffen
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
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
DE69321845T2 (de) 1992-08-25 1999-04-29 Searle & Co Hydroxyethylaminosulfonamide verwendbar als inhibitoren retroviraler proteasen
ES2112430T3 (es) 1992-08-25 1998-04-01 Searle & Co Sulfonilalcanoilamino 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
ES2150933T3 (es) 1992-12-22 2000-12-16 Lilly Co Eli Inhibidores de la proteasa vih utiles para el tratamiento del sida.
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
IL110525A0 (en) * 1993-08-09 1994-11-11 Lilly Co Eli Identification and use of protease inhibitors
EP0730643B1 (en) 1993-10-27 2001-01-10 Elan Pharmaceuticals, Inc. 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
ATE220661T1 (de) 1994-10-19 2002-08-15 Novartis Erfind Verwalt Gmbh Antivirale ether von aspartat-protease-substrat- isosteren
US6001813A (en) 1994-11-21 1999-12-14 Cortech Inc. Val-pro containing α-keto oxadiazoles as serine protease inhibitors
AUPM982594A0 (en) * 1994-12-02 1995-01-05 University Of Queensland, The HIV protease inhibitors
US5481011A (en) 1994-12-13 1996-01-02 Bristol-Myers Squibb Company Process for preparing N-protected amino acid α-halomethyl ketones and alcohols from N-protected amino acid esters
US6017887A (en) 1995-01-06 2000-01-25 Sibia Neurosciences, Inc. Peptide, peptide analog and amino acid analog protease inhibitors
US5804560A (en) 1995-01-06 1998-09-08 Sibia Neurosciences, Inc. Peptide and peptide analog protease inhibitors
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
EP0805816B1 (en) 1995-01-27 2004-07-28 Novo Nordisk A/S 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
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
AU6383396A (en) 1995-06-07 1996-12-30 Athena Neurosciences, Inc. Beta-secretase, antibodies to beta-secretase, and assays for detecting beta-secretase inhibition
ATE218538T1 (de) * 1995-11-21 2002-06-15 Novartis Erfind Verwalt Gmbh Azahexan-derivate als substratisostere von retroviralen aspartat-proteasen
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
JP2000509717A (ja) 1996-05-07 2000-08-02 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド オキシランメタンアミン誘導体の調製方法
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
JP2001510474A (ja) * 1997-02-04 2001-07-31 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア カテプシンdのナノモルの非ペプチド阻害剤
US6045829A (en) 1997-02-13 2000-04-04 Elan Pharma International Limited Nanocrystalline formulations of human immunodeficiency virus (HIV) protease inhibitors using cellulosic surface stabilizers
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
DK1086076T3 (da) * 1998-06-19 2005-03-29 Vertex Pharma Sulfonamidinhibitorer af aspartylprotease
PE20020276A1 (es) * 2000-06-30 2002-04-06 Elan Pharm Inc COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER
US6846813B2 (en) * 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
CA2448084A1 (en) * 2001-05-22 2002-11-28 Elan Pharmaceuticals, Inc. Aza hydroxylated ethyl amine compounds
MXPA03011046A (es) 2001-06-01 2004-06-25 Elan Pharm Inc Hidroxialquilaminas.
OA12846A (en) * 2001-11-08 2006-09-15 Elan Pharm Inc N,N'-substituted-1,3-diamino-2-hydroxypropane derivatives.

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ATE314343T1 (de) 2006-01-15
WO2002002505A3 (en) 2002-08-01
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