BR0304562A - Inibidor de gama-secretase - Google Patents

Inibidor de gama-secretase

Info

Publication number
BR0304562A
BR0304562A BR0304562-5A BR0304562A BR0304562A BR 0304562 A BR0304562 A BR 0304562A BR 0304562 A BR0304562 A BR 0304562A BR 0304562 A BR0304562 A BR 0304562A
Authority
BR
Brazil
Prior art keywords
val
group
leu
alkyl
ile
Prior art date
Application number
BR0304562-5A
Other languages
English (en)
Inventor
Hiroshi Mori
Original Assignee
Hiroshi Mori
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 Hiroshi Mori filed Critical Hiroshi Mori
Publication of BR0304562A publication Critical patent/BR0304562A/pt

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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • 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
    • 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
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/4711—Alzheimer's disease; Amyloid plaque core protein
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/81—Protease inhibitors
    • C07K14/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
    • C07K14/811—Serine protease (E.C. 3.4.21) inhibitors
    • C07K14/8114—Kunitz type inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/44—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material not provided for elsewhere, e.g. haptens, metals, DNA, RNA, amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Toxicology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Zoology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Heat Sensitive Colour Forming Recording (AREA)

Abstract

"INIBIDOR DE GAMA-SECRETASE". é destinado, como compostos inibindo a atividade <sym>-secretase, compostos tendo uma seq³ência de aminoácido que compreende pelo menos 3 aminoácidos consecutivos incluindo Val-Val-lle-Ala-Thr-Val-lle-Val-lleThr-Leu-Val-Met-Leu-Lys-Lys-Lys, tem grupo(s) hidroxietileno como um substituto para a ligação de peptídeo entre a Leu e um aminoácido imediatamente antes e/ou depois da mesma, tendo um grupo alcoxicarbonila com base em grupo C1-10 alquila opcionalmente substituído por fenila ou naftila no terminal N, tendo sido esterificado por alquila ou amidado por alquila no terminal C por um grupo C1-10 alquila opcionalmente substituído por fenila ou naftila, e opcionalmente substituído em grupo hidroxila da 10^ a^ Thr por um grupo hidrofóbico de C1-4 ou um grupo Z ou seu sal.
BR0304562-5A 2002-04-24 2003-04-18 Inibidor de gama-secretase BR0304562A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2002121983 2002-04-24
PCT/JP2003/005017 WO2003091278A1 (fr) 2002-04-24 2003-04-18 Inhibiteurs de gamma secretase

Publications (1)

Publication Number Publication Date
BR0304562A true BR0304562A (pt) 2004-07-20

Family

ID=29267426

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0304562-5A BR0304562A (pt) 2002-04-24 2003-04-18 Inibidor de gama-secretase

Country Status (11)

Country Link
US (1) US7585938B2 (pt)
EP (1) EP1498421B1 (pt)
JP (1) JP4404643B2 (pt)
KR (1) KR101051249B1 (pt)
CN (1) CN1319987C (pt)
AT (1) ATE448242T1 (pt)
AU (1) AU2003235283A1 (pt)
BR (1) BR0304562A (pt)
DE (1) DE60329995D1 (pt)
NO (1) NO329184B1 (pt)
WO (1) WO2003091278A1 (pt)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7521481B2 (en) 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
WO2008055924A1 (en) * 2006-11-07 2008-05-15 Vib Vzw Diagnosis and treatment of t-cell acute lymphoblastic leukemia
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
JP5930573B2 (ja) 2007-03-01 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤の新規使用
EP2142514B1 (en) 2007-04-18 2014-12-24 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
CN101970458B (zh) * 2007-08-09 2013-08-28 株式会社益力多本社 新型γ分泌酶抑制剂
JP5934645B2 (ja) 2009-09-11 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体
WO2012144972A2 (en) * 2010-01-19 2012-10-26 The General Hospital Corporation Methods to inhibit neurodegeneration
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
NZ602312A (en) 2010-03-10 2014-02-28 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
CN102344485A (zh) * 2010-08-05 2012-02-08 中国人民解放军军事医学科学院毒物药物研究所 用于治疗阿尔茨海默病的肽类β分泌酶抑制剂及其用途
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
WO2016059220A1 (en) 2014-10-16 2016-04-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Tcr-activating agents for use in the treatment of t-all
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0236734A3 (de) 1986-02-07 1988-05-11 Ciba-Geigy Ag Durch schwefelhaltigen Gruppen substituierte 5-Amino-4-hydroxyvalerylderivate
JP2003520266A (ja) * 2000-01-24 2003-07-02 メルク シャープ エンド ドーム リミテッド γ−セクレターゼ阻害薬
US6753410B2 (en) 2000-03-02 2004-06-22 Merck & Co., Inc. Investigational compounds
ATE339496T1 (de) * 2000-05-11 2006-10-15 Scios Inc Modulation von gamma-secretase aktivität
US20030022251A1 (en) * 2001-07-04 2003-01-30 Boehringer Ingelheim Pharma Kg Gamma-secretase in vitro screening assay

Also Published As

Publication number Publication date
JP4404643B2 (ja) 2010-01-27
CN1319987C (zh) 2007-06-06
NO20035535L (no) 2004-02-19
JPWO2003091278A1 (ja) 2005-09-02
EP1498421A1 (en) 2005-01-19
KR101051249B1 (ko) 2011-07-21
US20060205666A1 (en) 2006-09-14
EP1498421B1 (en) 2009-11-11
KR20040106370A (ko) 2004-12-17
DE60329995D1 (de) 2009-12-24
ATE448242T1 (de) 2009-11-15
NO329184B1 (no) 2010-09-06
NO20035535D0 (no) 2003-12-11
EP1498421A4 (en) 2006-05-17
US7585938B2 (en) 2009-09-08
WO2003091278A1 (fr) 2003-11-06
AU2003235283A1 (en) 2003-11-10
CN1656115A (zh) 2005-08-17

Similar Documents

Publication Publication Date Title
BR0304562A (pt) Inibidor de gama-secretase
HK22296A (en) Arginine salt and amide inhibitors of no synthase and cyclooxygenase
PE107299A1 (es) Composiciones farmaceuticas que comprenden un analogo de gaba y un antiinflamatorio no esteroideo
AP2001002217A0 (en) Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids.
DK1599216T3 (da) Fremgangsmåde til forebyggelse af mitokondriel permeabilitets-transition
DE69732571D1 (de) Beta-sulfonyl-hydroxamsäuren als matrix-metalloproteinaseinhibitoren
BR0307060A (pt) ésteres hidroxamato do ácido n-(fenil 4-substituìdo)-antranìlico
IS7482A (is) Fjölhringa efnasambönd sem sterk alfa2-adrenóviðtakamótlyf
EP1502949A4 (en) ANTIMICROBIAL POLYPEPTIDE AND USE THEREOF
BR0307071A (pt) ésteres hidroxamato do ácido n-(fenil 4-substituìdo)-antranìlico
WO2001072263A3 (de) Verwendung von ectoin oder ectoin-derivaten zum schutz der stressprotein in der haut
CY1107990T1 (el) Τριπεπτιδια και παραγωγα τριπεπτιδιων για τη θepαπεια νευροεκφυλιστικων ασθενειων
PT1226160E (pt) Novos peptidos antiarritmicos
DE59900730D1 (de) Korrosionsinhibitoren enthaltender Injektionszement
BR0311642A (pt) Formulação de divalproex de sódio de liberação aumentada
DK0624586T3 (da) Substituerede pyrroler
BR0208999A (pt) Processo para a preparação de ácido de cefpodoxima
HRP20080330T3 (en) Antitumoral compounds based on kahalalide f
AU8294401A (en) A process for the preparation of alpha&#39; chloroketones
DK0832101T3 (da) Urethan-formidlede, GST-specifikke molekylfrigörelsessystemer
AU2003275889A1 (en) Phosphinic acid analogs of glutamate
ATE170873T1 (de) Bombesin-analogen
EP0331756A4 (en) Agents for prophylaxis and treatment of thrombopenia
AU5270696A (en) Novel heterocyclic compounds
YU19194A (sh) Supstituisani piroli

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B11E Dismissal acc. art. 34 of ipl - requirements for examination incomplete
B11T Dismissal of application maintained [chapter 11.20 patent gazette]