BR0304562A - Inibidor de gama-secretase - Google Patents
Inibidor de gama-secretaseInfo
- 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
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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 [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/44—Immunoglobulins [IGs], 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)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Gastroenterology & Hepatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Toxicology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Zoology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Immunology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Medicinal Preparation (AREA)
- Heat Sensitive Colour Forming Recording (AREA)
- Investigating Or Analysing Biological Materials (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.
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 Pending 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)
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 |
JP5379692B2 (ja) | 2006-11-09 | 2013-12-25 | プロビオドルグ エージー | 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての3−ヒドロキシ−1,5−ジヒドロ−ピロール−2−オン誘導体 |
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 |
ZA200905537B (en) | 2007-03-01 | 2010-10-27 | Probiodrug Ag | New use of glutaminyl cyclase inhibitors |
ES2533484T3 (es) | 2007-04-18 | 2015-04-10 | Probiodrug Ag | Derivados de tiourea como inhibidores de la glutaminil ciclasa |
US8501813B2 (en) | 2007-08-09 | 2013-08-06 | Kabushiki Kaisha Yakult Honsha | γ-secretase inhibitor |
EA022007B1 (ru) | 2009-09-11 | 2015-10-30 | Пробиодруг Аг | Гетероциклические производные в качестве ингибиторов глутаминилциклазы |
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 |
KR101790806B1 (ko) | 2010-03-10 | 2017-11-20 | 프로비오드룩 아게 | 글루타미닐 사이클라제(qc, ec 2.3.2.5)의 헤테로사이클릭 억제제 |
EP2560953B1 (en) | 2010-04-21 | 2016-01-06 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
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 |
WO2012123563A1 (en) | 2011-03-16 | 2012-09-20 | Probiodrug Ag | Benz imidazole 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 |
PL3461819T3 (pl) | 2017-09-29 | 2020-11-30 | Probiodrug Ag | Inhibitory cyklazy glutaminylowej |
Family Cites Families (5)
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 |
AU779875B2 (en) * | 2000-01-24 | 2005-02-17 | Merck Sharp & Dohme Limited | Gamma-secretase inhibitors |
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 |
-
2003
- 2003-04-18 AT AT03720938T patent/ATE448242T1/de not_active IP Right Cessation
- 2003-04-18 CN CNB038118963A patent/CN1319987C/zh not_active Expired - Fee Related
- 2003-04-18 BR BR0304562-5A patent/BR0304562A/pt active Pending
- 2003-04-18 JP JP2003587836A patent/JP4404643B2/ja not_active Expired - Fee Related
- 2003-04-18 AU AU2003235283A patent/AU2003235283A1/en not_active Abandoned
- 2003-04-18 KR KR1020047016996A patent/KR101051249B1/ko not_active IP Right Cessation
- 2003-04-18 US US10/511,269 patent/US7585938B2/en not_active Expired - Fee Related
- 2003-04-18 EP EP03720938A patent/EP1498421B1/en not_active Expired - Lifetime
- 2003-04-18 DE DE60329995T patent/DE60329995D1/de not_active Expired - Lifetime
- 2003-04-18 WO PCT/JP2003/005017 patent/WO2003091278A1/ja active Application Filing
- 2003-12-11 NO NO20035535A patent/NO329184B1/no not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
KR101051249B1 (ko) | 2011-07-21 |
NO20035535L (no) | 2004-02-19 |
ATE448242T1 (de) | 2009-11-15 |
EP1498421B1 (en) | 2009-11-11 |
NO20035535D0 (no) | 2003-12-11 |
NO329184B1 (no) | 2010-09-06 |
WO2003091278A1 (fr) | 2003-11-06 |
DE60329995D1 (de) | 2009-12-24 |
CN1319987C (zh) | 2007-06-06 |
AU2003235283A1 (en) | 2003-11-10 |
US7585938B2 (en) | 2009-09-08 |
JP4404643B2 (ja) | 2010-01-27 |
KR20040106370A (ko) | 2004-12-17 |
CN1656115A (zh) | 2005-08-17 |
EP1498421A4 (en) | 2006-05-17 |
US20060205666A1 (en) | 2006-09-14 |
EP1498421A1 (en) | 2005-01-19 |
JPWO2003091278A1 (ja) | 2005-09-02 |
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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] |