JP2004502665A - アルツハイマー病を治療する化合物 - Google Patents

アルツハイマー病を治療する化合物 Download PDF

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JP2004502665A
JP2004502665A JP2002507763A JP2002507763A JP2004502665A JP 2004502665 A JP2004502665 A JP 2004502665A JP 2002507763 A JP2002507763 A JP 2002507763A JP 2002507763 A JP2002507763 A JP 2002507763A JP 2004502665 A JP2004502665 A JP 2004502665A
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ファング、ローレンス、ワイ
ジョン、ヴァーゲーズ
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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
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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    • C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
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    • C07C233/78—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
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    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/84—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C243/28—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of a saturated carbon skeleton
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    • C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
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    • C07C271/18—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by doubly-bound oxygen atoms
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    • C07C275/24—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
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    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
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    • C07C311/05—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
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    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
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    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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JP2002507763A 2000-06-30 2001-06-29 アルツハイマー病を治療する化合物 Pending JP2004502665A (ja)

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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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JP2002507763A Pending JP2004502665A (ja) 2000-06-30 2001-06-29 アルツハイマー病を治療する化合物
JP2002507762A Abandoned JP2004502664A (ja) 2000-06-30 2001-06-29 アルツハイマー病処置用化合物

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US (2) US7034182B2 (enExample)
EP (2) EP1299349B1 (enExample)
JP (2) JP2004502665A (enExample)
KR (1) KR20030058959A (enExample)
CN (1) CN1217920C (enExample)
AT (2) ATE302751T1 (enExample)
AU (3) AU2001273094A1 (enExample)
BR (1) BR0111980A (enExample)
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009534367A (ja) * 2006-04-21 2009-09-24 ミンスター・リサーチ・リミテッド 前駆症状症候群の治療にｍ１／ｍ４ムスカリン性アゴニスト（サブコメリン）を用いる単独及び組合せ療法

Families Citing this family (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2004502665A (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 アルツハイマー病を治療する化合物
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 (es) * 2001-04-23 2004-07-28 Elan Pharm Inc Epoxidos sustituidos y procesos para prepararlos
US6960664B2 (en) 2001-05-22 2005-11-01 Pharmacia & Upjohn Company 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
WO2003002122A1 (en) 2001-06-27 2003-01-09 Elan Pharmaceuticals, Inc. Beta-hydroxyamine derivatives useful in treatment of alzheimer's disease
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
RS50504A (sr) * 2001-11-08 2007-04-10 Elan Pharmaceuticals Inc., Derivati n,n'-supstituisanog-1,3- diamino-2-hidroksipropana
JP2005536448A (ja) * 2001-11-19 2005-12-02 ファルマシア アンド アップジョン カンパニー アミン１，２−及び１，３−ジオール化合物、及びアルツハイマー病を治療するためのその使用
AU2002357232A1 (en) * 2001-12-04 2003-06-17 Elan Pharmaceuticals, Inc. Peptide isosteres containing a heterocycle useful in the treatment of alzheimer's disease
MXPA04005428A (es) 2001-12-06 2004-12-06 Elan Pharm Inc Hidroxietilaminas substituidas.
JP4354180B2 (ja) * 2001-12-26 2009-10-28 武田薬品工業株式会社 軽度認知障害治療剤
US7115652B2 (en) 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
AU2003276047A1 (en) 2002-06-17 2003-12-31 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
US20060160079A1 (en) * 2002-08-07 2006-07-20 Lane Roger M 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
NZ538625A (en) * 2002-09-06 2008-05-30 Pharmacia & Upjohn Co Llc 1,3-Diamino-2-hydroxypropane prodrug derivatives
UY27967A1 (es) * 2002-09-10 2004-05-31 Pfizer Acetil 2-hindroxi-1,3-diaminoalcanos
WO2004024675A1 (en) * 2002-09-10 2004-03-25 Pharmacia & Upjohn Company Llc Substituted aminoethers for the treatment of alzheimer's disease
EP1562897B1 (en) 2002-11-12 2009-09-16 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer s disease
JP2006508166A (ja) * 2002-11-27 2006-03-09 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 置換尿素及びカルバメート
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
MXPA05011150A (es) * 2003-04-21 2005-12-14 Elan Pharm Inc 2-hidroxi-3-diaminoalcanos de benzamida.
CA2522805A1 (en) * 2003-04-21 2004-11-04 Elan Pharmaceuticals, Inc. Phenacyl 2-hydroxy-3-diaminoalkanes
GB0309221D0 (en) * 2003-04-23 2003-06-04 Glaxo Group Ltd Novel compounds
JP2007516207A (ja) * 2003-06-30 2007-06-21 メルク　エンド　カムパニー　インコーポレーテッド アルツハイマー病の治療のためのＮ−アルキルフェニルカルボキサミドβ−セクレターゼ阻害剤
EP1660443B1 (en) 2003-08-08 2009-03-04 Schering Corporation Cyclic amine bace-1 inhibitors having a benzamide substituent
MXPA06001558A (es) * 2003-08-08 2006-05-15 Schering Corp Inhibidores de amina ciclica bace-1 que poseen un sustituyente heterociclico.
GB0328900D0 (en) * 2003-12-12 2004-01-14 Glaxo Group Ltd Novel compounds
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
FR2866647B1 (fr) * 2004-02-20 2006-10-27 Servier Lab Nouveaux derives azabicycliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
MXPA06010899A (es) * 2004-03-25 2006-12-15 Elan Pharm Inc 1,3-diaminopropanos substituidos con 2-amino y 2-tio.
ATE491693T1 (de) 2004-07-22 2011-01-15 Schering Corp Substituierte amide als inhibitoren der beta- sekretase
US7361789B1 (en) 2004-07-28 2008-04-22 Amgen Inc. Dihydronaphthalene compounds, compositions, uses thereof, and methods for synthesis
WO2006014944A1 (en) 2004-07-28 2006-02-09 Schering Corporation Macrocyclic beta-secretase inhibitors
WO2006034277A1 (en) * 2004-09-17 2006-03-30 Comentis, Inc. Bicyclic compounds which inhibit beta-secretase activity and methods of use thereof
JP2008513432A (ja) 2004-09-21 2008-05-01 ファイザー・プロダクツ・インク Ｃｎｓ状態の治療に有用なｎ−メチルヒドロキシエチルアミン
WO2006033000A2 (en) * 2004-09-21 2006-03-30 Pfizer Products Inc. N-ethyl hydroxyethylamine useful in treating cns conditions
WO2006099352A1 (en) 2005-03-10 2006-09-21 Bristol-Myers Squibb Company Novel isophthalates as beta-secretase inhibitors
GB0506562D0 (en) * 2005-03-31 2005-05-04 Glaxo Group Ltd Novel compounds
NZ562314A (en) * 2005-04-08 2010-02-26 Comentis Inc Compounds which inhibit beta-secretase activity and methods of use thereof
EP1923388A4 (en) 2005-08-12 2011-03-09 Takeda Pharmaceutical BRAIN / NEURONAL CELL PROTECTIVE AGENT AND THERAPEUTIC AGENT FOR SLEEP DISORDERS
US7745484B2 (en) 2005-11-21 2010-06-29 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
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
US7872009B2 (en) 2005-11-21 2011-01-18 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
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
JP5523107B2 (ja) 2006-11-30 2014-06-18 プロビオドルグ エージー グルタミニルシクラーゼの新規阻害剤
JP2010512389A (ja) 2006-12-12 2010-04-22 シェーリング コーポレイション アスパルチルプロテアーゼ阻害剤
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
WO2008128985A1 (en) 2007-04-18 2008-10-30 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
WO2008147547A1 (en) 2007-05-25 2008-12-04 Amgen Inc. Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
JP5440984B2 (ja) 2007-05-25 2014-03-12 アムジエン・インコーポレーテツド β−セクレターゼ修飾剤としての置換ヒドロキシエチルアミン化合物および使用方法
KR20100051668A (ko) * 2007-07-26 2010-05-17 코멘티스, 인코포레이티드 베타-세크레타제 활성을 억제하는 이소프탈아미드 유도체
CA2699787A1 (en) 2007-09-24 2009-04-02 Comentis, Inc. (3-hydroxy-4-amino-butan-2-yl)-3-(2-thiazol-2-yl-pyrrolidine-1-carbonyl) benzamide derivatives and related compounds as beta-secretase inhibitors for treating
SE531873C2 (sv) * 2007-11-12 2009-09-01 Lifeassays Ab Anordning för biokemisk bearbetning och analys av provvätska
US7803809B2 (en) 2008-11-12 2010-09-28 Amgen Inc. Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use
WO2009078999A1 (en) 2007-12-17 2009-06-25 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
BRPI0911518A2 (pt) * 2008-04-29 2017-06-13 Pharnext novas aproximações terapêuticas para o tratamento da doença de alzheimer e doenças relacionadas através de uma modulação de resposta ao estresse de célula
EP3586839A1 (en) 2008-07-28 2020-01-01 Blanchette Rockefeller Neurosciences, Institute Pkc-activating compounds for the treatment of neurodegenerative diseases
CA2736130C (en) * 2008-09-11 2014-01-14 Amgen Inc. Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
WO2010132605A1 (en) * 2009-05-13 2010-11-18 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
MX2012002993A (es) 2009-09-11 2012-04-19 Probiodrug Ag Derivados heterociclicos como inhibidores de ciclasa glutaminilo.
WO2011063272A1 (en) 2009-11-23 2011-05-26 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
US8735384B2 (en) 2010-01-19 2014-05-27 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
EP2531508A1 (en) * 2010-02-05 2012-12-12 Pfizer Inc. Pyrrolo [ 2, 3 - d]pyrimidine urea compounds as jak inhibitors
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
US8269019B2 (en) 2010-03-10 2012-09-18 Probiodrug Ag Inhibitors
AU2011227501B9 (en) 2010-03-15 2013-08-22 Amgen Inc. Amino -dihydrooxazine and amino - dihydrothiazine spiro compounds as Beta - secretase modulators and their medical use
WO2011115938A1 (en) 2010-03-15 2011-09-22 Amgen Inc. Spiro-tetracyclic ring compounds as beta - secretase modulators
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
JP2013542973A (ja) 2010-11-22 2013-11-28 ノスシラ、ソシエダッド、アノニマ 神経変性疾患または神経変性状態を治療するためのビピリジンスルホンアミド誘導体
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
ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
US9296759B2 (en) 2011-09-21 2016-03-29 Amgen Inc. Amino-oxazine 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
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
SG11202002032SA (en) 2017-09-22 2020-04-29 Jubilant Epipad LLC Heterocyclic compounds as pad inhibitors
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
CA3076476A1 (en) 2017-10-18 2019-04-25 Jubilant Epipad LLC Imidazo-pyridine compounds as pad inhibitors
BR112020008851A2 (pt) 2017-11-06 2020-10-20 Jubilant Prodel LLC composto da fórmula i, processo de preparação de compostos da fórmula i, composição farmacêutica, método para o tratamento e/ou prevenção de várias doenças, uso, método para o tratamento de câncer, método de tratamento de câncer e método para o tratamento e/ou prevenção de câncer e doenças infecciosas
PL3704120T3 (pl) 2017-11-24 2024-09-16 Jubilant Episcribe Llc Związki heterocykliczne jako inhibitory prmt5
SG11202008950PA (en) 2018-03-13 2020-10-29 Jubilant Prodel LLC Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH05201945A (ja) * 1991-07-03 1993-08-10 Ciba Geigy Ag 医薬的に活性なヒドラジン誘導体およびその製造方法
JPH07165606A (ja) * 1993-08-09 1995-06-27 Eli Lilly & Co プロテアーゼインヒビターの同定および用途
JPH08507061A (ja) * 1993-02-25 1996-07-30 アボツト・ラボラトリーズ レトロウィルスプロテアーゼ抑制性化合物
JPH11514996A (ja) * 1995-11-21 1999-12-21 ノバルティス アクチエンゲゼルシャフト レトロウイルスアスパラギン酸プロテアーゼの置換同配体としてのアザヘキサン誘導体
WO1999065870A2 (en) * 1998-06-19 1999-12-23 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease
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

Family Cites Families (149)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5753564Y2 (enExample) 1977-06-01 1982-11-19
CH624011A5 (enExample) 1977-08-05 1981-07-15 Battelle Memorial Institute
FR2416008A1 (fr) 1978-02-02 1979-08-31 Oreal Lyophilisats de liposomes
US4394448A (en) 1978-02-24 1983-07-19 Szoka Jr Francis C Method of inserting DNA into living cells
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4399216A (en) 1980-02-25 1983-08-16 The Trustees Of Columbia University Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
ZA811368B (en) 1980-03-24 1982-04-28 Genentech Inc Bacterial polypedtide expression employing tryptophan promoter-operator
US5142056A (en) 1989-05-23 1992-08-25 Abbott Laboratories Retroviral protease inhibiting compounds
NZ201705A (en) 1981-08-31 1986-03-14 Genentech Inc Recombinant dna method for production of hepatitis b surface antigen in yeast
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US4870009A (en) 1982-11-22 1989-09-26 The Salk Institute For Biological Studies Method of obtaining gene product through the generation of transgenic animals
US4668770A (en) 1982-12-27 1987-05-26 Merck & Co., Inc. Renin inhibitory tripeptides
AU2353384A (en) 1983-01-19 1984-07-26 Genentech Inc. Amplification in eukaryotic host cells
US4713339A (en) 1983-01-19 1987-12-15 Genentech, Inc. Polycistronic expression vector construction
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
US4474778A (en) * 1983-11-09 1984-10-02 E. R. Squibb & Sons, Inc. Lactam containing compounds, their pharmaceutical compositions and method of use
US4512988A (en) * 1984-03-01 1985-04-23 E. R. Squibb & Sons, Inc. Acylamino oxo or hydroxy substituted alkylamino thiazines and thiazepines
US4636491A (en) 1984-03-27 1987-01-13 Merck & Co., Inc. Renin inhibitory peptides having improved solubility
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
EP0245361A1 (en) 1985-11-15 1987-11-19 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
JPS63503380A (ja) 1986-01-16 1988-12-08 アボット・ラボラトリーズ ペプチド類似体
WO1987005330A1 (en) 1986-03-07 1987-09-11 Michel Louis Eugene Bergh Method for enhancing glycoprotein stability
DE3610593A1 (de) 1986-03-29 1987-10-01 Hoechst Ag Substituierte 4-amino-3-hydroxybuttersaeure-derivate verfahren zu deren herstellung, diese enthaltende mittel und ihre verwendung
US4851387A (en) 1986-10-14 1989-07-25 Banyu Pharmaceutical Co., Ltd. 5-substituted amino-4-hydroxy-pentanoic acid derivatives and their use
US4935405A (en) * 1986-10-31 1990-06-19 Pfizer Inc. Nor-statine and nor-cyclostatine polypeptides
ES2062988T3 (es) 1986-12-19 1995-01-01 Sankyo Co Nuevos oligopeptidos inhibidores de la renina, su preparacion y su uso.
US5250565A (en) 1987-02-10 1993-10-05 Abbott Laboratories Indole-,benzofuran-,and benzothiophene-containing lipoxygenase-inhibiting compounds
DE3721855A1 (de) 1987-03-12 1988-09-22 Merck Patent Gmbh Aminosaeurederivate
FR2614533A1 (fr) 1987-04-23 1988-11-04 Sandoz Sa Nouveaux derives peptidiques, leur preparation et leur utilisation comme medicaments
EP0366669A1 (en) 1987-06-29 1990-05-09 The Upjohn Company Malic acid derivative containing renin inhibiting peptides
US5010182A (en) 1987-07-28 1991-04-23 Chiron Corporation DNA constructs containing a Kluyveromyces alpha factor leader sequence for directing secretion of heterologous polypeptides
EP0364493A1 (en) 1987-08-07 1990-04-25 The Upjohn Company Renin inhibiting peptides with nonpeptide linkages
GB8724885D0 (en) 1987-10-23 1987-11-25 Binns M M Fowlpox virus promotors
GB8728561D0 (en) 1987-12-07 1988-01-13 Glaxo Group Ltd Chemical compounds
EP0371068B1 (de) 1987-12-16 1991-06-19 Dallmer GmbH & Co. Ablaufarmatur für einen fliesenfussboden
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
EP0479909B1 (en) 1989-06-29 1996-10-30 Medarex, Inc. Bispecific reagents for aids therapy
GB8927915D0 (en) * 1989-12-11 1990-02-14 Hoffmann La Roche Novel alcohols
DE3941235A1 (de) 1989-12-14 1991-06-20 Bayer Ag Neue peptide, ihre herstellung und ihre verwendung in arzneimitteln
DE4001236A1 (de) 1990-01-18 1991-07-25 Bayer Ag Neue peptide, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel, insbesondere als arzneimittel gegen retroviren
DE4003575A1 (de) 1990-02-07 1991-08-08 Bayer Ag Retroisostere dipeptide, verfahren zur herstellung und ihre verwendung als renininhibitoren in arzneimitteln
GB9004483D0 (en) 1990-02-28 1990-04-25 Erba Carlo Spa New aryl-and heteroarylethenylene derivatives and process for their preparation
US5912410A (en) 1990-06-15 1999-06-15 Scios Inc. Transgenic non-human mice displaying the amyloid-forming pathology of alzheimer's disease
WO1991019810A1 (en) 1990-06-15 1991-12-26 California Biotechnology Inc. Transgenic non-human mammal 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
US5602175A (en) 1990-11-19 1997-02-11 G.D. Searle & Co. Retroviral protease inhibitors
US5648511A (en) 1990-11-19 1997-07-15 G.D. Searle & Co. Method for making intermediates useful in the synthesis of retroviral protease inhibitors
US5482947A (en) 1990-11-19 1996-01-09 Talley; John J. Retroviral protease inhibitors
CA2372251A1 (en) 1991-01-21 1992-08-06 Michael John Mullan Test and model for alzheimer's disease
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
US5206161A (en) 1991-02-01 1993-04-27 Genentech, Inc. Human plasma carboxypeptidase B
EP0578745A1 (en) 1991-04-04 1994-01-19 The Upjohn Company Phosphorus containing compounds as inhibitors of retroviruses
WO1992020373A1 (en) 1991-05-14 1992-11-26 Repligen Corporation Heteroconjugate antibodies for treatment of hiv infection
US5753652A (en) 1991-07-03 1998-05-19 Novartis Corporation Antiretroviral hydrazine derivatives
IE922316A1 (en) 1991-07-17 1993-01-27 Smithkline Beecham Corp Retroviral protease inhibitors
US5516784A (en) 1991-08-13 1996-05-14 Schering Corporation Anti-HIV (AIDS) agents
WO1993008829A1 (en) 1991-11-04 1993-05-13 The Regents Of The University Of California Compositions that mediate killing of hiv-infected cells
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
AU3735793A (en) 1992-02-26 1993-09-13 Smithkline Beecham Corporation Retroviral protease inhibitors
DE69333270T2 (de) 1992-03-11 2004-08-05 Narhex Ltd. Aminderivate von oxo- und hydroxy- substituierten kohlenwasserstoffen
ES2066623T3 (es) 1992-03-13 1995-03-01 Bio Mega Boehringer Ingelheim Derivados sustituidos del acido pipecolinico como inhibidores de la vih-proteasa.
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
US5521219A (en) 1992-08-25 1996-05-28 G. D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US5760076A (en) 1992-08-25 1998-06-02 G.D Searle & Co. Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
JP3657002B2 (ja) 1992-08-25 2005-06-08 ジー．ディー．サール アンド カンパニー レトロウイルスプロテアーゼ阻害剤として有用なα−およびβ−アミノ酸ヒドロキシエチルアミノスルホンアミド
US5830897A (en) 1992-08-27 1998-11-03 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US5578606A (en) 1992-10-30 1996-11-26 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
US5484926A (en) 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
MX9308025A (es) 1992-12-22 1994-08-31 Lilly Co Eli Compuestos inhibidores de la proteasa del virus dela inmunodeficiencia humana, procedimiento para supreparacion y formulacion farmaceutica que los contiene.
ES2150933T3 (es) 1992-12-22 2000-12-16 Lilly Co Eli Inhibidores de la proteasa vih utiles para el tratamiento del sida.
AU7669794A (en) 1993-08-24 1995-03-21 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
JPH09507746A (ja) 1993-10-27 1997-08-12 アテナ ニューロサイエンシズ，インコーポレイティド Ｓｗｅｄｉｓｈ変異を有するＡＰＰ対立遺伝子を含有するトランスジェニック動物
JPH07126286A (ja) 1993-11-05 1995-05-16 Yamanouchi Pharmaceut Co Ltd 新規なペプチド誘導体
US5733882A (en) 1994-01-17 1998-03-31 Smithkline Beecham Corporation Retroviral protease inhibitors
US5877399A (en) 1994-01-27 1999-03-02 Johns Hopkins University Transgenic mice expressing APP-Swedish mutation develop progressive neurologic disease
US5625031A (en) 1994-02-08 1997-04-29 Bristol-Myers Squibb Company Peptide inhibitors of the p33cdk2 and p34cdc2 cell cycle regulatory kinases and human papillomavirus E7 oncoprotein
US5475138A (en) 1994-07-07 1995-12-12 Pharm-Eco Laboratories Incorporated Method preparing amino acid-derived diaminopropanols
PT708085E (pt) 1994-10-19 2002-11-29 Novartis Ag Eteres antivirais de isosteros de substrato de aspartato protease
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
WO1996022287A1 (en) 1995-01-20 1996-07-25 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
CZ238197A3 (en) 1995-01-27 1997-12-17 Novo Nordisk As Growth hormone formation stimulating compounds
US5545640A (en) 1995-04-04 1996-08-13 Bio-Mega/Boehringer Ingeleheim Research Inc. Protease inhibiting succinic acid derivatives
TW493991B (en) 1995-05-08 2002-07-11 Novartis Ag Pharmaceutical composition for oral administration of active agent having low water solubility and process for preparation of the same
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
US5565483A (en) 1995-06-07 1996-10-15 Bristol-Myers Squibb Company 3-substituted oxindole derivatives as potassium channel modulators
US5886046A (en) 1996-01-19 1999-03-23 The Trustees Of The University Of Pennsylvania Dicarbonyl-containing compounds
US5849691A (en) 1996-02-20 1998-12-15 The United States Of America As Represented By The Department Of Health And Human Services Peptidomimetic inhibitors of cathepsin D and plasmepsins I and II
US5849911A (en) 1996-04-22 1998-12-15 Novartis Finance Corporation Antivirally active heterocyclic azahexane derivatives
US5847169A (en) 1996-05-07 1998-12-08 Boehringer Ingelheim Pharmaceuticals, Inc. Process for preparing oxiranemethanamine derivatives
DE69734215T2 (de) 1996-07-22 2006-06-29 Novo Nordisk A/S Verbindungen mit Wachstumshormon-freisetzenden Eigenschaften
US5914333A (en) 1996-07-31 1999-06-22 Novo Nordisk A/S Treatment of psychotic disorders
US5703129A (en) 1996-09-30 1997-12-30 Bristol-Myers Squibb Company 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of β-amyloid protein production
US6225103B1 (en) 1996-11-20 2001-05-01 Oklahoma Medical Research Foundation Cloning and characterization of napsin
US6153652A (en) 1996-11-22 2000-11-28 Elan Pharmaceuticals, Inc. N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US6191166B1 (en) 1997-11-21 2001-02-20 Elan Pharmaceuticals, Inc. Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
US6127556A (en) 1996-12-31 2000-10-03 G. D. Searle & Co. Epoxide formation by continuous in-situ synthesis process
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
CN1248968A (zh) 1997-02-26 2000-03-29 辉瑞大药厂 杂芳基－己酸酰胺衍生物、其制备方法及其作为MIP－1α与其CCRI受体结合的选择性抑制剂的用途
US6221670B1 (en) 1997-03-21 2001-04-24 Scios Inc. Methods to identify β-amyloid reducing agents
AU734302B2 (en) 1997-05-08 2001-06-07 Smithkline Beecham Corporation Protease inhibitors
US5962506A (en) 1997-07-07 1999-10-05 Pharmacopeia, Inc. Glycol and hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases
US6087383A (en) 1998-01-20 2000-07-11 Bristol-Myers Squibb Company Bisulfate salt of HIV protease inhibitor
CA2320117A1 (en) 1998-02-12 1999-08-19 Emory University Sphingolipid derivatives and their methods of use
DE19817461A1 (de) 1998-04-20 1999-10-21 Basf Ag Neue substituierte Benzamide, deren Herstellung und Anwendung
KR20070013361A (ko) 1998-09-24 2007-01-30 파마시아 앤드 업존 캄파니 엘엘씨 알츠하이머병 세크레타제
JP4653318B2 (ja) 1999-02-10 2011-03-16 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 βセクレターゼ酵素組成物および方法
WO2000061748A1 (en) 1999-04-09 2000-10-19 Human Genome Sciences, Inc. 48 human secreted proteins
AU3771700A (en) 1999-03-24 2000-10-09 Regents Of The University Of California, The Methods for treating neurodegenerative disorders using aspartyl protease inhibitors
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
CA2374346C (en) 1999-06-28 2010-06-22 Jordan J. N. Tang Inhibitors of memapsin 2 and use thereof
WO2001010387A2 (en) 1999-08-09 2001-02-15 Vanderbilt University Antiviral therapy use of p-glycoprotein modulators
IL147774A0 (en) 1999-09-13 2002-08-14 Du Pont Pharm Co Hydroxyalkanoyl aminolactams and related structures as inhibitors of as protein production
ATE431419T1 (de) 1999-09-23 2009-05-15 Pharmacia & Upjohn Co Llc Alzheimer krankheit sekretase, app (amyloid vorlaüfer-protein) substrate dafür und verwendungen
GB9924957D0 (en) 1999-10-21 1999-12-22 Smithkline Beecham Plc Novel treatment
AU2699901A (en) 2000-01-13 2001-07-24 Serono Genetics Institute S.A. Biallelic markers derived from genomic regions carrying genes involved in central nervous system disorders
JP2004502665A (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 アルツハイマー病を治療する化合物
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
US6960664B2 (en) 2001-05-22 2005-11-01 Pharmacia & Upjohn Company 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
RS50504A (sr) 2001-11-08 2007-04-10 Elan Pharmaceuticals Inc., Derivati n,n'-supstituisanog-1,3- diamino-2-hidroksipropana

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH05201945A (ja) * 1991-07-03 1993-08-10 Ciba Geigy Ag 医薬的に活性なヒドラジン誘導体およびその製造方法
JPH08507061A (ja) * 1993-02-25 1996-07-30 アボツト・ラボラトリーズ レトロウィルスプロテアーゼ抑制性化合物
JPH07165606A (ja) * 1993-08-09 1995-06-27 Eli Lilly & Co プロテアーゼインヒビターの同定および用途
JPH11514996A (ja) * 1995-11-21 1999-12-21 ノバルティス アクチエンゲゼルシャフト レトロウイルスアスパラギン酸プロテアーゼの置換同配体としてのアザヘキサン誘導体
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
WO1999065870A2 (en) * 1998-06-19 1999-12-23 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009534367A (ja) * 2006-04-21 2009-09-24 ミンスター・リサーチ・リミテッド 前駆症状症候群の治療にｍ１／ｍ４ムスカリン性アゴニスト（サブコメリン）を用いる単独及び組合せ療法

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