ATE482233T1 - Inhibitoren des memapsin 2 und ihre verwendung - Google Patents

Inhibitoren des memapsin 2 und ihre verwendung

Info

Publication number
ATE482233T1
ATE482233T1 AT00943236T AT00943236T ATE482233T1 AT E482233 T1 ATE482233 T1 AT E482233T1 AT 00943236 T AT00943236 T AT 00943236T AT 00943236 T AT00943236 T AT 00943236T AT E482233 T1 ATE482233 T1 AT E482233T1
Authority
AT
Austria
Prior art keywords
memapsin
substrate
ala
bond
leu
Prior art date
Application number
AT00943236T
Other languages
German (de)
English (en)
Inventor
Jordan Tang
Lin Hong
Arun Ghosh
Xinli Lin
Gerald Koelsch
Original Assignee
Oklahoma Med Res Found
Univ Illinois
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 Oklahoma Med Res Found, Univ Illinois filed Critical Oklahoma Med Res Found
Application granted granted Critical
Publication of ATE482233T1 publication Critical patent/ATE482233T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1021—Tetrapeptides with the first amino acid being acidic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/113—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides without change of the primary structure
    • C07K1/1136—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides without change of the primary structure by reversible modification of the secondary, tertiary or quarternary structure, e.g. using denaturating or stabilising agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6478—Aspartic endopeptidases (3.4.23)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2299/00—Coordinates from 3D structures of peptides, e.g. proteins or enzymes
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A90/00—Technologies having an indirect contribution to adaptation to climate change
    • Y02A90/10—Information and communication technologies [ICT] supporting adaptation to climate change, e.g. for weather forecasting or climate simulation

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biotechnology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Analytical Chemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AT00943236T 1999-06-28 2000-06-27 Inhibitoren des memapsin 2 und ihre verwendung ATE482233T1 (de)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US14136399P 1999-06-28 1999-06-28
US16806099P 1999-11-30 1999-11-30
US17783600P 2000-01-25 2000-01-25
US17836800P 2000-01-27 2000-01-27
US21029200P 2000-06-08 2000-06-08
PCT/US2000/017742 WO2001000665A2 (en) 1999-06-28 2000-06-27 Inhibitors of memapsin 2 and use thereof

Publications (1)

Publication Number Publication Date
ATE482233T1 true ATE482233T1 (de) 2010-10-15

Family

ID=27538142

Family Applications (1)

Application Number Title Priority Date Filing Date
AT00943236T ATE482233T1 (de) 1999-06-28 2000-06-27 Inhibitoren des memapsin 2 und ihre verwendung

Country Status (9)

Country Link
US (7) US6545127B1 (https=)
EP (2) EP1196609A2 (https=)
JP (2) JP4484410B2 (https=)
CN (1) CN1379819A (https=)
AT (1) ATE482233T1 (https=)
AU (2) AU5773500A (https=)
CA (2) CA2374346C (https=)
DE (1) DE60045005D1 (https=)
WO (2) WO2001000663A2 (https=)

Families Citing this family (114)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9701684D0 (en) 1997-01-28 1997-03-19 Smithkline Beecham Plc Novel compounds
US20040234976A1 (en) * 1998-09-24 2004-11-25 Gurney Mark E. Alzheimer's disease secretase, app substrates therefor, and uses therefor
CN1300320C (zh) * 1998-09-24 2007-02-14 法玛西雅厄普约翰美国公司 阿尔茨海默氏疾病分泌酶
US6844148B1 (en) 1998-09-24 2005-01-18 Pharmacia & Upjohn Company Alzheimer's disease secretase, APP substrates therefor, and uses therefor
US6699671B1 (en) 1998-09-24 2004-03-02 Pharmacia & Upjohn Company Alzheimer's disease secretase, APP substrates therefor, and uses therefor
US7456007B1 (en) 1998-12-31 2008-11-25 Elan Pharmaceuticals, Inc. β-secretase enzyme compositions and methods
US7115410B1 (en) 1999-02-10 2006-10-03 Elan Pharmaceuticals, Inc. β-secretase enzyme compositions and methods
CN1390232A (zh) 1999-02-10 2003-01-08 艾兰制药公司 人β分泌酶、抑制剂、其组合物和用途
EP1196609A2 (en) * 1999-06-28 2002-04-17 Oklahoma Medical Research Foundation Catalytically active recombinant memapsin and methods of use thereof
US20090162883A1 (en) * 1999-09-23 2009-06-25 Pharmacia & Upjohn Company Alzheimer's Disease Secretase, APP Substrates Thereof, and Uses Thereof
GB9924957D0 (en) * 1999-10-21 1999-12-22 Smithkline Beecham Plc Novel treatment
GB9925136D0 (en) * 1999-10-22 1999-12-22 Smithkline Beecham Plc Novel treatment
US7514408B1 (en) 1999-12-02 2009-04-07 Elan Pharmaceuticals, Inc. β-secretase enzyme compositions and methods
CA2397543A1 (en) * 2000-01-24 2001-07-26 Timothy Harrison Gamma-secretase inhibitors
US6583268B2 (en) 2000-01-25 2003-06-24 Oklahoma Medical Research Foundation Universal procedure for refolding recombinant proteins
DE60124080T2 (de) 2000-03-23 2007-03-01 Elan Pharmaceuticals, Inc., San Francisco Verbindungen und verfahren zur behandlung der alzheimerschen krankheit
EP1666452A2 (en) 2000-06-30 2006-06-07 Elan Pharmaceuticals, Inc. 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
EP1299352B1 (en) 2000-06-30 2005-12-28 Elan Pharmaceuticals, Inc. Compounds to treat alzheimer's disease
US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
US7205120B2 (en) * 2000-07-19 2007-04-17 Pharmacia & Upjohn Company Substrates and assays for β-secretase activity
US7630838B2 (en) * 2000-09-22 2009-12-08 American Home Products Corporation Method for identifying agents that interact with beta-site APP cleaving enzyme (BACE)
US7601528B1 (en) 2000-12-23 2009-10-13 Elan Pharmaceuticals, Inc. Crystallization and structure determination of glycosylated human beta secretase, an enzyme implicated in alzheimer's disease
US7217556B1 (en) 2000-12-23 2007-05-15 Pfizer Inc Crystallization and structure determination of glycosylated human beta secretase, an enzyme implicated in Alzheimer's disease
US7806980B2 (en) 2000-12-23 2010-10-05 Elan Pharmaceuticals, Inc. Method for crystallizing human beta secretase in complex with an inhibitor
US20040121947A1 (en) * 2000-12-28 2004-06-24 Oklahoma Medical Research Foundation Compounds which inhibit beta-secretase activity and methods of use thereof
EP1233021A3 (en) * 2001-02-20 2002-11-20 Pfizer Products Inc. An inhibitor of Beta amyloid cleavage enzyme
WO2002068623A2 (en) * 2001-02-23 2002-09-06 Dsm Ip Assets B.V. Genes encoding proteolytic enzymes from aspargilli
US7384773B1 (en) 2001-05-10 2008-06-10 Pfizer Inc Crystal of HIV protease-cleaved human beta secretase and method for crystallization thereof
US7524668B1 (en) 2001-05-10 2009-04-28 Elan Pharmaceuticals, Inc. Crystal of human beta secretase having monoclinic space group symmetry C2 and methods for crystallization thereof
US7196163B2 (en) 2001-05-22 2007-03-27 Merk & Co., Inc. Assays using amyloid precursor proteins with modified β-secretase cleavage sites to monitor β-secretase activity
EP1390497A2 (en) 2001-05-25 2004-02-25 Genset Human cdnas and proteins and uses thereof
CA2450557A1 (en) * 2001-06-11 2002-12-19 Michel Maillard Substituted aminoalcohols useful in treatment of alzheimer's disease
EP1401452A1 (en) 2001-06-27 2004-03-31 Elan Pharmaceuticals, Inc. Beta-hydroxyamine derivatives useful in the treatment of alzheimer's disease
EP1409660A2 (en) * 2001-07-26 2004-04-21 Astex Technology Limited Crystal structure of beta-site app cleaving enzyme (bace) and use thereof
US7186539B1 (en) * 2001-08-31 2007-03-06 Pharmacia & Upjohn Company Method for refolding enzymes
CA2464736A1 (en) * 2001-10-23 2003-05-15 Oklahoma Medical Research Foundation Beta-secretase inhibitors and methods of use
US20060234944A1 (en) * 2001-10-23 2006-10-19 Oklahoma Medical Reseach Foundation Beta-secretase inhibitors and methods of use
WO2003040393A2 (en) * 2001-11-06 2003-05-15 Decode Genetics Ehf. Nucleic acids encoding proteases
CH698246B1 (de) * 2001-12-20 2009-06-30 Hoffmann La Roche Test zur Identifizierung von Inhibitoren von Beta-Sekretasen.
AU2003213252A1 (en) 2002-02-21 2003-09-09 Pharmacia And Upjohn Company Modified bace
KR101011657B1 (ko) 2002-03-01 2011-01-28 다케다 야쿠힌 고교 가부시키가이샤 항우울제
US7442537B1 (en) 2002-05-10 2008-10-28 Elan Pharmaceuticals, Inc. Crystals of unliganded beta secretase and/or beta secretase-like proteins and the use thereof
AU2003230392A1 (en) 2002-05-17 2003-12-12 Merck And Co., Inc. Beta-secretase inhibitors
US7166454B1 (en) 2002-05-24 2007-01-23 Schering Corporation Codon-optimized β-secretase and methods of refolding and processing
US6746303B2 (en) 2002-05-31 2004-06-08 Mattel, Inc. Flexible toy figure with wire armature
WO2004011641A2 (en) * 2002-07-26 2004-02-05 Astex Technology Limited Crystal structure of beta-site app-cleaving enzyme (bace) mutants and uses thereof
US20050074456A1 (en) * 2002-12-04 2005-04-07 Marcus Ballinger Constructs for homogenously processed preparations of beta site APP-cleaving enzyme
US7371853B2 (en) 2003-01-07 2008-05-13 Merck & Co., Inc. Macrocyclic β-secretase inhibitors for the treatment of Alzheimer's disease
EP1473362A1 (en) 2003-05-02 2004-11-03 Elan Pharmaceuticals, Inc. Glycosylation variants of BACE
CN100430377C (zh) 2003-06-30 2008-11-05 麦克公司 用于治疗阿尔茨海默病的N-烷基苯基甲酰胺β分泌酶抑制剂
CN1909897A (zh) 2003-07-01 2007-02-07 默克公司 用于治疗阿尔茨海默病的苯基羧化物β－分泌酶抑制剂
AU2004277981B2 (en) 2003-10-03 2009-10-01 Merck & Co., Inc. Benzylether and benzylamino beta-secretase inhibitors for the treatment of Alzheimer's disease
FR2860796B1 (fr) * 2003-10-14 2006-02-10 Centre Nat Rech Scient Procede de dissociation de la molecule d'hemoglobine extracellulaire d'arenicola marina, chaines proteiques constituant ladite molecule et sequences nucleotidiques codant pour lesdites chaines proteiques
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US20060019368A1 (en) * 2004-07-20 2006-01-26 Marcus Ballinger Constructs for homogenously processed preparations of beta site APP-cleaving enzyme
US7906625B2 (en) * 2005-01-24 2011-03-15 Amgen Inc. Humanized anti-amyloid antibody
ES2400287T3 (es) * 2005-03-14 2013-04-08 High Point Pharmaceuticals, Llc Derivados de benzazol, composiciones y procedimientos de uso como inhibidores de beta-secretasa
CA2603404A1 (en) 2005-03-30 2006-10-05 Boehringer Ingelheim International Gmbh Substituted 1,2-ethylendiamines, medicaments comprising said compound; their use and their method of manufacture
AU2006279896A1 (en) * 2005-08-10 2007-02-22 Oklahoma Medical Research Foundation Truncated memapsin 2 for use for treating Alzheimer's disease
WO2007020888A1 (ja) 2005-08-12 2007-02-22 Takeda Pharmaceutical Company Limited 脳・神経細胞保護剤および睡眠障害治療薬
US7816387B2 (en) 2005-09-05 2010-10-19 Dainippon Sumitomo Pharma Co., Ltd. β secretase inhibitor
WO2007081534A2 (en) * 2005-12-22 2007-07-19 Pfizer Products Inc Method of producing catalytically active bace2 enzymes
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
EP2168947A4 (en) 2007-06-22 2010-07-28 Yoshiaki Kiso NOVEL COMPOUND HAVING SECRETASE INHIBITING ACTIVITY
CA2687750C (en) 2007-07-06 2016-10-18 Boehringer Ingelheim International Gmbh Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture
KR20100059919A (ko) * 2007-09-24 2010-06-04 코멘티스, 인코포레이티드 치료를 위한 베타-세크레타제 억제제로서 (3-히드록시-4-아미노-부탄-2일)-3-(2-티아졸-2-일-피롤리딘-1-카르보닐) 벤즈아미드 유도체 및 관련 화합물
WO2009085200A2 (en) 2007-12-21 2009-07-09 Amgen Inc. Anti-amyloid antibodies and uses thereof
WO2009155609A1 (en) 2008-06-20 2009-12-23 Oklahoma Medical Research Foundation IMMUNOGENIC MEMAPSIN 2 β-SECRETASE PEPTIDES AND METHODS OF USE
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
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
US8956859B1 (en) 2010-08-13 2015-02-17 Aviex Technologies Llc Compositions and methods for determining successful immunization by one or more vaccines
MX346500B (es) 2010-11-10 2017-03-22 Genentech Inc * Metodos y composiciones para inmunoterapia para enfermedad neural.
EP2643299B1 (en) 2010-11-22 2016-06-22 Noscira, S.A. Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions
PL2763979T3 (pl) 2011-10-07 2019-06-28 Takeda Pharmaceutical Company Limited Związki 1-arylokarbonyl-4-oksy-piperydynowe użyteczne do leczenia chorób neurodegeneracyjnych
JP2015518048A (ja) 2012-05-30 2015-06-25 コメンティス， インコーポレイテッド クロマン化合物
US9296746B2 (en) 2012-10-16 2016-03-29 Takeda Pharmaceutical Company Limited Heterocyclic compound
PE20151162A1 (es) 2012-12-11 2015-08-28 Takeda Pharmaceutical Compuestos heterociclicos inhibidores del colesterol 24-hidroxilasa (ch24h)
JP6272832B2 (ja) 2013-04-04 2018-01-31 武田薬品工業株式会社 複素環化合物
EP2982670B1 (en) 2013-04-04 2018-11-07 Takeda Pharmaceutical Company Limited Heterocyclic compound
EP3152198B1 (en) 2014-06-09 2019-02-27 Takeda Pharmaceutical Company Limited Radiolabeled compounds
EP3221361B1 (en) 2014-11-19 2021-04-21 Genentech, Inc. Anti-transferrin receptor / anti-bace1 multispecific antibodies and methods of use
WO2016081639A1 (en) 2014-11-19 2016-05-26 Genentech, Inc. Antibodies against bace1 and use thereof for neural disease immunotherapy
WO2017040808A1 (en) * 2015-09-03 2017-03-09 Contact Effect, Inc. Management of tenant locations in multi-tenant environments
LT3984994T (lt) 2016-02-04 2024-10-10 Takeda Pharmaceutical Company Limited Pakeistas piperidino junginys kaip 2 tipo oreksino agonistas narkolepsijai gydyti
US9919021B2 (en) * 2016-04-15 2018-03-20 Ibet—Instituto De Biologia Experimental E Tecnológica Brain permeant peptidomimetic beta-secretase 1 inhibitors for the treatment or prophylaxis of neurological disorders or conditions
US11059780B2 (en) 2017-03-08 2021-07-13 Takeda Pharmaceutical Company Limited Substituted pyrrolidine compound and use thereof
JP7012703B2 (ja) 2017-03-08 2022-02-14 武田薬品工業株式会社 置換ピロリジン化合物およびその用途
EP3660003B1 (en) 2017-07-28 2024-01-24 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2019027003A1 (ja) 2017-08-03 2019-02-07 武田薬品工業株式会社 複素環化合物およびその用途
US10428023B2 (en) 2017-08-03 2019-10-01 Takeda Pharmaceutical Company Limited Heterocyclic compound and use thereof
US10807987B2 (en) 2018-03-28 2020-10-20 Takeda Pharmaceutical Company Limited Heterocyclic compound and use thereof
CN108588040B (zh) * 2018-06-08 2021-06-15 中国医学科学院病原生物学研究所 重组MtMetRS、其晶体及它们在制备抗结核药物中的应用
JP7339250B2 (ja) 2018-06-29 2023-09-05 武田薬品工業株式会社 複素環化合物およびその用途
WO2020004537A1 (ja) 2018-06-29 2020-01-02 武田薬品工業株式会社 複素環化合物およびその用途
EP3896060B1 (en) 2018-12-12 2023-08-16 Takeda Pharmaceutical Company Limited Heterocyclic compound
US12071434B2 (en) 2018-12-12 2024-08-27 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2020153414A1 (ja) 2019-01-24 2020-07-30 武田薬品工業株式会社 複素環化合物及びその用途
JP7253640B2 (ja) 2019-01-31 2023-04-06 武田薬品工業株式会社 複素環化合物およびその用途
KR20220062361A (ko) 2019-09-13 2022-05-16 다케다 야쿠힌 고교 가부시키가이샤 과도한 졸림의 치료를 위한 오렉신 2 수용체 효능제의 용도
AU2020346456A1 (en) 2019-09-13 2022-04-14 Takeda Pharmaceutical Company Limited TAK-925 for use in treating narcolepsy
JP2021080177A (ja) 2019-11-14 2021-05-27 武田薬品工業株式会社 複素環化合物及びその用途
US12448377B2 (en) 2019-11-27 2025-10-21 Takeda Pharmaceutical Company Limited Heterocyclic compound
JP2021183586A (ja) 2020-05-22 2021-12-02 武田薬品工業株式会社 複素環化合物
JP2021183587A (ja) 2020-05-22 2021-12-02 武田薬品工業株式会社 複素環化合物
US20230313196A1 (en) * 2020-07-23 2023-10-05 John Mansell Compositions and methods for treating pain and anxiety disorders
TW202302100A (zh) 2021-03-12 2023-01-16 日商武田藥品工業股份有限公司 食慾激素２受體促效劑於治療食慾激素介導之疾病或病症之用途
JPWO2023090268A1 (https=) 2021-11-17 2023-05-25
WO2023199091A1 (en) 2022-04-12 2023-10-19 Takeda Pharmaceutical Company Limited Heterocyclic compound
TW202428580A (zh) 2022-10-31 2024-07-16 日商武田藥品工業股份有限公司 雜環化合物
AR131202A1 (es) 2022-11-30 2025-02-26 Takeda Pharmaceuticals Co Compuesto heterocíclico y uso del mismo
PE20252742A1 (es) 2023-03-16 2025-12-05 Takeda Pharmaceuticals Co Compuestos heterociclicos macrociclicos y sus usos
WO2025229494A1 (en) 2024-04-29 2025-11-06 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2025229495A1 (en) 2024-04-29 2025-11-06 Takeda Pharmaceutical Company Limited Heterocyclic compound

Family Cites Families (104)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US72050A (en) * 1867-12-10 Improvement in horse hiy-foeks
US81634A (en) * 1868-09-01 Improved kailway-switch
US159991A (en) * 1875-02-16 Improvement in shoe-tips
US55459A (en) * 1866-06-12 Improvement in artificial legs
US111365A (en) * 1871-01-31 Improvement in combined rocking sofas and bedsteads
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4235877A (en) 1979-06-27 1980-11-25 Merck & Co., Inc. Liposome particle containing viral or bacterial antigenic subunit
US4391904A (en) 1979-12-26 1983-07-05 Syva Company Test strip kits in immunoassays and compositions therein
US4501728A (en) 1983-01-06 1985-02-26 Technology Unlimited, Inc. Masking of liposomes from RES recognition
US5019369A (en) 1984-10-22 1991-05-28 Vestar, Inc. Method of targeting tumors in humans
US4945050A (en) 1984-11-13 1990-07-31 Cornell Research Foundation, Inc. Method for transporting substances into living cells and tissues and apparatus therefor
US5036006A (en) 1984-11-13 1991-07-30 Cornell Research Foundation, Inc. Method for transporting substances into living cells and tissues and apparatus therefor
US4797368A (en) 1985-03-15 1989-01-10 The United States Of America As Represented By The Department Of Health And Human Services Adeno-associated virus as eukaryotic expression vector
US5139941A (en) 1985-10-31 1992-08-18 University Of Florida Research Foundation, Inc. AAV transduction vectors
US4946778A (en) 1987-09-21 1990-08-07 Genex Corporation Single polypeptide chain binding molecules
US4837028A (en) 1986-12-24 1989-06-06 Liposome Technology, Inc. Liposomes with enhanced circulation time
US5219740A (en) 1987-02-13 1993-06-15 Fred Hutchinson Cancer Research Center Retroviral gene transfer into diploid fibroblasts for gene therapy
US5132405A (en) 1987-05-21 1992-07-21 Creative Biomolecules, Inc. Biosynthetic antibody binding sites
US4985544A (en) 1987-08-04 1991-01-15 Kyowa Hakko Kogyo Co., Ltd. Process for renaturing fish growth hormone
DE10399032I1 (de) 1987-08-28 2004-01-29 Health Research Inc Rekombinante Viren.
US5591624A (en) 1988-03-21 1997-01-07 Chiron Viagene, Inc. Retroviral packaging cell lines
US4923967A (en) * 1988-09-26 1990-05-08 Eli Lilly And Company Purification and refolding of recombinant proteins
GB8823869D0 (en) 1988-10-12 1988-11-16 Medical Res Council Production of antibodies
US5703055A (en) 1989-03-21 1997-12-30 Wisconsin Alumni Research Foundation Generation of antibodies through lipid mediated DNA delivery
JP4041535B2 (ja) 1989-08-18 2008-01-30 オックスフォード バイオメディカ（ユーケー）リミテッド 標的細胞にベクター構造体を運搬する組換レトロウィルス
US5221607A (en) 1989-09-18 1993-06-22 Scios Nova Inc. Assays and reagents for amyloid deposition
US5286634A (en) 1989-09-28 1994-02-15 Stadler Joan K Synergistic method for host cell transformation
ATE157012T1 (de) 1989-11-03 1997-09-15 Univ Vanderbilt Verfahren zur in vivo-verabreichung von funktionsfähigen fremden genen
FR2658432B1 (fr) 1990-02-22 1994-07-01 Medgenix Group Sa Microspheres pour la liberation controlee des substances hydrosolubles et procede de preparation.
US5279833A (en) 1990-04-04 1994-01-18 Yale University Liposomal transfection of nucleic acids into animal cells
US5235043A (en) * 1990-04-06 1993-08-10 Synergen, Inc. Production of biologically active, recombinant members of the ngf/bdnf family of neurotrophic proteins
US5204253A (en) 1990-05-29 1993-04-20 E. I. Du Pont De Nemours And Company Method and apparatus for introducing biological substances into living cells
US5308854A (en) 1990-06-18 1994-05-03 Merck & Co., Inc. Inhibitors of HIV reverse transcriptase
US5252463A (en) 1990-06-22 1993-10-12 The Du Pont Merck Pharmaceutical Company Clipsin, a chymotrypsin-like protease and method of using same
WO1992001070A1 (en) 1990-07-09 1992-01-23 The United States Of America, As Represented By The Secretary, U.S. Department Of Commerce High efficiency packaging of mutant adeno-associated virus using amber suppressions
MY109299A (en) 1990-08-15 1996-12-31 Virogenetics Corp Recombinant pox virus encoding flaviviral structural proteins
US5200339A (en) 1990-08-17 1993-04-06 Abraham Carmela R Proteases causing abnormal degradation of amyloid β-protein precursor
US5545806A (en) 1990-08-29 1996-08-13 Genpharm International, Inc. Ransgenic non-human animals for producing heterologous antibodies
US5633425A (en) 1990-08-29 1997-05-27 Genpharm International, Inc. Transgenic non-human animals capable of producing heterologous antibodies
ATE300615T1 (de) 1990-08-29 2005-08-15 Genpharm Int Transgene mäuse fähig zur produktion heterologer antikörper
US5625126A (en) 1990-08-29 1997-04-29 Genpharm International, Inc. Transgenic non-human animals for producing heterologous antibodies
US5661016A (en) 1990-08-29 1997-08-26 Genpharm International Inc. Transgenic non-human animals capable of producing heterologous antibodies of various isotypes
US5187074A (en) 1990-10-11 1993-02-16 Merck & Co., Inc. Method of hydroxylation with ATCC 55086
US5192668A (en) 1990-10-11 1993-03-09 Merck & Co., Inc. Synthesis of protease inhibitor
US5173414A (en) 1990-10-30 1992-12-22 Applied Immune Sciences, Inc. Production of recombinant adeno-associated virus vectors
JP3534749B2 (ja) 1991-08-20 2004-06-07 アメリカ合衆国 アデノウイルスが介在する胃腸管への遺伝子の輸送
WO1993008184A1 (en) 1991-10-23 1993-04-29 Merck & Co., Inc. Hiv protease inhibitors
US5413999A (en) 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
IL105793A0 (en) 1992-05-28 1993-09-22 Lilly Co Eli Protease and related dna compounds
US5587308A (en) 1992-06-02 1996-12-24 The United States Of America As Represented By The Department Of Health & Human Services Modified adeno-associated virus vector capable of expression from a novel promoter
EP0646178A1 (en) 1992-06-04 1995-04-05 The Regents Of The University Of California expression cassette with regularoty regions functional in the mammmlian host
US5665720A (en) 1992-08-07 1997-09-09 Merck & Co., Inc. Benzoxazinones as inhibitors of HIV reverse transcriptase
CN1127527A (zh) 1993-05-17 1996-07-24 加利福尼亚大学董事会 人免疫缺陷型病毒感染和艾滋病的核酶基因治疗方法
US5679647A (en) 1993-08-26 1997-10-21 The Regents Of The University Of California Methods and devices for immunizing a host against tumor-associated antigens through administration of naked polynucleotides which encode tumor-associated antigenic peptides
US5804566A (en) 1993-08-26 1998-09-08 The Regents Of The University Of California Methods and devices for immunizing a host through administration of naked polynucleotides with encode allergenic peptides
US6015686A (en) 1993-09-15 2000-01-18 Chiron Viagene, Inc. Eukaryotic layered vector initiation systems
AU7973994A (en) 1993-10-13 1995-05-04 Merck & Co., Inc. Combination therapy for hiv infection
US5739118A (en) 1994-04-01 1998-04-14 Apollon, Inc. Compositions and methods for delivery of genetic material
US5476874A (en) 1994-06-22 1995-12-19 Merck & Co., Inc. New HIV protease inhibitors
US5736524A (en) 1994-11-14 1998-04-07 Merck & Co.,. Inc. Polynucleotide tuberculosis vaccine
US5986054A (en) 1995-04-28 1999-11-16 The Hospital For Sick Children, Hsc Research And Development Limited Partnership Genetic sequences and proteins related to alzheimer's disease
US5922687A (en) 1995-05-04 1999-07-13 Board Of Trustees Of The Leland Stanford Junior University Intracellular delivery of nucleic acids using pressure
US5744346A (en) 1995-06-07 1998-04-28 Athena Neurosciences, Inc. β-secretase
US6329163B1 (en) 1995-06-07 2001-12-11 Elan Pharmaceuticals, Inc. Assays for detecting β-secretase inhibition
US6221645B1 (en) 1995-06-07 2001-04-24 Elan Pharmaceuticals, Inc. β-secretase antibody
US5942400A (en) 1995-06-07 1999-08-24 Elan Pharmaceuticals, Inc. Assays for detecting β-secretase
US5978740A (en) 1995-08-09 1999-11-02 Vertex Pharmaceuticals Incorporated Molecules comprising a calcineurin-like binding pocket and encoded data storage medium capable of graphically displaying them
AU732508B2 (en) 1996-01-26 2001-04-26 Governing Council Of The University Of Toronto, The Nucleic acids and proteins related to Alzheimer's disease, and uses therefor
US5846978A (en) 1996-05-02 1998-12-08 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
EP0812916A3 (en) 1996-06-14 1998-12-09 Smithkline Beecham Corporation Cathepsin k gene
DE19641180A1 (de) 1996-09-24 1998-03-26 Schering Ag Verfahren zur Darstellung von APP-Sekretase Modulation und deren Verwendung als Mittel zur Behandlung der Alzheimer'schen Erkrankung
WO1998015828A1 (en) 1996-10-07 1998-04-16 Scios Inc. Method to identify direct inhibitors of the beta-amyloid forming enzyme gamma-secretase
WO1998021589A1 (en) 1996-11-15 1998-05-22 The Trustees Of The University Of Pennsylvania Screening for modulators of amyloid processing
US6207710B1 (en) * 1996-11-22 2001-03-27 Elan Pharmaceuticals, Inc. Compounds for inhibiting β-amyloid peptide release and/or its synthesis
AU1684097A (en) 1996-12-11 1998-07-03 Athena Neurosciences, Inc. Beta-secretase isolated from human 293 cells
GB9701684D0 (en) * 1997-01-28 1997-03-19 Smithkline Beecham Plc Novel compounds
US6077682A (en) 1998-03-19 2000-06-20 University Of Medicine And Dentistry Of New Jersey Methods of identifying inhibitors of sensor histidine kinases through rational drug design
AU3054899A (en) 1998-03-31 1999-10-25 Chugai Seiyaku Kabushiki Kaisha Cell line not expressing beta-secretase activity
EP1084240A1 (fr) 1998-06-05 2001-03-21 Aventis Pharma S.A. Polypeptides possedant une activite de type beta-secretase
US20040234976A1 (en) 1998-09-24 2004-11-25 Gurney Mark E. Alzheimer's disease secretase, app substrates therefor, and uses therefor
US6844148B1 (en) 1998-09-24 2005-01-18 Pharmacia & Upjohn Company Alzheimer's disease secretase, APP substrates therefor, and uses therefor
CN1300320C (zh) * 1998-09-24 2007-02-14 法玛西雅厄普约翰美国公司 阿尔茨海默氏疾病分泌酶
US6699671B1 (en) 1998-09-24 2004-03-02 Pharmacia & Upjohn Company Alzheimer's disease secretase, APP substrates therefor, and uses therefor
US6245884B1 (en) * 1998-10-16 2001-06-12 Vivian Y. H. Hook Secretases related to alzheimer's dementia
US6313268B1 (en) 1998-10-16 2001-11-06 Vivian Y. H. Hook Secretases related to Alzheimer's dementia
US7115410B1 (en) 1999-02-10 2006-10-03 Elan Pharmaceuticals, Inc. β-secretase enzyme compositions and methods
CN1390232A (zh) 1999-02-10 2003-01-08 艾兰制药公司 人β分泌酶、抑制剂、其组合物和用途
WO2000058479A1 (en) 1999-03-26 2000-10-05 Amgen Inc. Beta secretase genes and polypeptides
EP1192177A1 (en) 1999-06-15 2002-04-03 Elan Pharmaceuticals, Inc. Statine-derived tetrapeptide inhibitors of beta-secretase
EP1196609A2 (en) 1999-06-28 2002-04-17 Oklahoma Medical Research Foundation Catalytically active recombinant memapsin and methods of use thereof
EP1496124A1 (en) 1999-06-28 2005-01-12 Oklahoma Medical Research Foundation Catalytically active recombinant memapsin and methods of use thereof
PT1224297E (pt) 1999-09-23 2009-08-17 Pharmacia & Upjohn Co Llc Secretase da doença de alzheimer, seus substratos app e suas utilizações
US6361975B1 (en) * 1999-11-16 2002-03-26 Smithkline Beecham Corporation Mouse aspartic secretase-2(mASP-2)
US6291223B1 (en) * 1999-11-23 2001-09-18 Smithkline Beecham Corporation Mouse aspartic secretase-1 (mASP1)
US6583268B2 (en) * 2000-01-25 2003-06-24 Oklahoma Medical Research Foundation Universal procedure for refolding recombinant proteins
DE60124080T2 (de) 2000-03-23 2007-03-01 Elan Pharmaceuticals, Inc., San Francisco Verbindungen und verfahren zur behandlung der alzheimerschen krankheit
US6713276B2 (en) * 2000-06-28 2004-03-30 Scios, Inc. Modulation of Aβ levels by β-secretase BACE2
ATE388402T1 (de) 2000-07-19 2008-03-15 Genisphere Inc Verfahren zur erkennung und zum assay von nukleinsäuresequenzen
AU2001281250A1 (en) 2000-08-11 2002-02-25 The Brigham And Women's Hospital, Inc. (hydroxyethyl)ureas as inhibitors of alzheimer's beta-amyloid production
US7630838B2 (en) * 2000-09-22 2009-12-08 American Home Products Corporation Method for identifying agents that interact with beta-site APP cleaving enzyme (BACE)
AU2002243391A1 (en) 2000-10-27 2002-06-24 The Johns Hopkins University School Of Medicine Beta-secretase transgenic organisms, anti-beta-secretase antibodies, and methods of use thereof
US20040121947A1 (en) 2000-12-28 2004-06-24 Oklahoma Medical Research Foundation Compounds which inhibit beta-secretase activity and methods of use thereof
AU2002239727C1 (en) 2000-12-28 2005-12-22 Oklahoma Medical Research Foundation Inhibitors of memapsin 2 and use thereof
AU2006279896A1 (en) * 2005-08-10 2007-02-22 Oklahoma Medical Research Foundation Truncated memapsin 2 for use for treating Alzheimer's disease

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