BRPI0509879A - compostos para inibição enzimática - Google Patents
compostos para inibição enzimáticaInfo
- Publication number
- BRPI0509879A BRPI0509879A BRPI0509879-3A BRPI0509879A BRPI0509879A BR PI0509879 A BRPI0509879 A BR PI0509879A BR PI0509879 A BRPI0509879 A BR PI0509879A BR PI0509879 A BRPI0509879 A BR PI0509879A
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- peptide
- based compounds
- activity
- inhibition
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 7
- 230000005764 inhibitory process Effects 0.000 title abstract 2
- 102000004190 Enzymes Human genes 0.000 title 1
- 108090000790 Enzymes Proteins 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 4
- 230000000694 effects Effects 0.000 abstract 3
- NOWKCMXCCJGMRR-UHFFFAOYSA-N Aziridine Chemical compound C1CN1 NOWKCMXCCJGMRR-UHFFFAOYSA-N 0.000 abstract 1
- 108090000604 Hydrolases Proteins 0.000 abstract 1
- 102000004157 Hydrolases Human genes 0.000 abstract 1
- 102000004245 Proteasome Endopeptidase Complex Human genes 0.000 abstract 1
- 108090000708 Proteasome Endopeptidase Complex Proteins 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 230000037012 chymotrypsin-like activity Effects 0.000 abstract 1
- 230000002255 enzymatic effect Effects 0.000 abstract 1
- 150000002118 epoxides Chemical class 0.000 abstract 1
- 238000007306 functionalization reaction Methods 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000035407 negative regulation of cell proliferation Effects 0.000 abstract 1
- 230000000269 nucleophilic effect Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
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
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- 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
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- 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
- C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Tropical Medicine & Parasitology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Physical Education & Sports Medicine (AREA)
- AIDS & HIV (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
COMPOSTOS PARA INIBIçãO ENZIMáTICA Compostos baseados em peptídeos incluindo anéis de três membros contendo heteroátomo, inibindo seletivamente atividades específicas das hidrolases (Ntn) nucleofílicas N-terminais. As atividades daqueles Ntn com múltiplas atividades pode ser diferencialmente inibida pelos compostos descritos. Por exemplo, a atividade semelhante à quimiotripsina do proteassoma 20S pode ser seletivamente inibida com os compostos da invenção. Os compostos baseados em peptídeos incluem pelo menos três unidades pepídicas, um epóxido ou aziridina, e a funcionalização do N-terminal. Dentre outras utilidades terapêuticas, se espera que os compostos baseados em peptídeos apresentem propriedades antiinflamatórias e inibição da proliferação celular.
Applications Claiming Priority (8)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US56234004P | 2004-04-15 | 2004-04-15 | |
US56909604P | 2004-05-07 | 2004-05-07 | |
US59940104P | 2004-08-06 | 2004-08-06 | |
US61015904P | 2004-09-14 | 2004-09-14 | |
US61000204P | 2004-09-14 | 2004-09-14 | |
US61000104P | 2004-09-14 | 2004-09-14 | |
US62057304P | 2004-10-20 | 2004-10-20 | |
PCT/US2005/012740 WO2005105827A2 (en) | 2004-04-15 | 2005-04-14 | Compounds for proteasome enzyme inhibition |
Publications (1)
Publication Number | Publication Date |
---|---|
BRPI0509879A true BRPI0509879A (pt) | 2007-10-16 |
Family
ID=34965899
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BRPI0509879-3A BRPI0509879A (pt) | 2004-04-15 | 2005-04-14 | compostos para inibição enzimática |
Country Status (18)
Country | Link |
---|---|
US (9) | US8129346B2 (pt) |
EP (1) | EP1745064B1 (pt) |
JP (3) | JP5616569B2 (pt) |
CN (2) | CN102174076A (pt) |
AT (1) | ATE494298T1 (pt) |
AU (1) | AU2005238445B2 (pt) |
BE (1) | BE2016C014I2 (pt) |
BR (1) | BRPI0509879A (pt) |
CA (1) | CA2562411A1 (pt) |
CY (1) | CY1117244T1 (pt) |
DE (1) | DE602005025750D1 (pt) |
DK (1) | DK1745064T3 (pt) |
HK (1) | HK1097860A1 (pt) |
IL (3) | IL178400A (pt) |
PL (1) | PL1745064T3 (pt) |
PT (1) | PT1745064E (pt) |
SG (2) | SG152239A1 (pt) |
WO (1) | WO2005105827A2 (pt) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9340820B2 (en) | 2009-08-26 | 2016-05-17 | Queen's University Of Belfast | Compounds and methods for protease detection |
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US7232818B2 (en) * | 2004-04-15 | 2007-06-19 | Proteolix, Inc. | Compounds for enzyme inhibition |
AU2012203602B2 (en) * | 2004-04-15 | 2015-08-27 | Onyx Therapeutics, Inc. | Compounds for proteasome enzyme inhibition |
US8198270B2 (en) | 2004-04-15 | 2012-06-12 | Onyx Therapeutics, Inc. | Compounds for proteasome enzyme inhibition |
CN102174076A (zh) | 2004-04-15 | 2011-09-07 | 普罗特奥里克斯公司 | 用于抑制蛋白酶体酶的化合物 |
DK2030981T3 (da) | 2004-05-10 | 2014-10-13 | Onyx Therapeutics Inc | Forbindelser til proteasom-enzymhæmning |
DK1819353T3 (da) | 2004-12-07 | 2011-05-16 | Proteolix Inc | Sammensætning til proteasomhæmning |
PL1948678T3 (pl) | 2005-11-09 | 2013-09-30 | Onyx Therapeutics Inc | Związki do hamowania enzymów |
DK2041158T3 (da) | 2006-06-19 | 2013-06-24 | Onyx Therapeutics Inc | Peptid-epoxidketoner til proteasom inhibering |
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CN106946981B (zh) * | 2017-03-08 | 2020-08-21 | 南京陵瑞医药科技有限公司 | 一种四肽环氧丙烷衍生物及其制备方法和用途 |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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US9340820B2 (en) | 2009-08-26 | 2016-05-17 | Queen's University Of Belfast | Compounds and methods for protease detection |
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