CY1119405T1 - Ενωση για την αναστολη ενζυμων - Google Patents
Ενωση για την αναστολη ενζυμωνInfo
- Publication number
- CY1119405T1 CY1119405T1 CY20171100781T CY171100781T CY1119405T1 CY 1119405 T1 CY1119405 T1 CY 1119405T1 CY 20171100781 T CY20171100781 T CY 20171100781T CY 171100781 T CY171100781 T CY 171100781T CY 1119405 T1 CY1119405 T1 CY 1119405T1
- Authority
- CY
- Cyprus
- Prior art keywords
- peptide
- based compounds
- union
- enzymes
- suspension
- Prior art date
Links
Classifications
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/69—Boron compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/06—Tripeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/55—Protease inhibitors
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
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- 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
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- 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
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- 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]
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
- C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
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- 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
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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- 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
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
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- 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
- 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
- C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
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- 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
- C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
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- 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
-
- 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
- C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
-
- 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
- C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
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- 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)
- Biophysics (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Οι ενώσεις που βασίζονται σε πεπτίδια οι οποίες περιλαμβάνουν τριμελείς δακτυλίους που περιέχουν ετεροάτομα αναστέλλουν αποτελεσματικά και επιλεκτικά συγκεκριμένες δράσεις πυρηνόφιλων υδρολασών με τελικό άκρο Ν (Ntn) οι οποίες σχετίζονται με το πρωτεάσωμα. Οι ενώσεις που βασίζονται σε πεπτίδια περιλαμβάνουν ένα εποξείδιο ή αζιριδίνη, και λειτουργικοποίηση στο τελικό άκρο Ν. Ανάμεσα σε άλλες θεραπευτικές χρήσεις, οι ενώσεις που βασίζονται σε πεπτίδια αναμένεται να παρουσιάζουν αντι-φλεγμονώδεις ιδιότητες και αναστολή του κυτταρικού πολλαπλασιασμού. Η χορήγηση από το στόμα αυτών των αναστολέων πρωτεασώματος που βασίζονται σε πεπτίδια είναι δυνατή εξαιτίας των προφίλ βιοδιαθεσιμότητάς τους.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US73611805P | 2005-11-09 | 2005-11-09 | |
US84258206P | 2006-09-05 | 2006-09-05 | |
EP06837164.0A EP1948678B1 (en) | 2005-11-09 | 2006-11-09 | Compounds for enzyme inhibition |
Publications (1)
Publication Number | Publication Date |
---|---|
CY1119405T1 true CY1119405T1 (el) | 2018-03-07 |
Family
ID=37671954
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CY20171100781T CY1119405T1 (el) | 2005-11-09 | 2017-07-21 | Ενωση για την αναστολη ενζυμων |
Country Status (29)
Country | Link |
---|---|
US (8) | US8716322B2 (el) |
EP (2) | EP2623113B1 (el) |
JP (3) | JP5436860B2 (el) |
KR (3) | KR101434522B1 (el) |
CN (2) | CN105237621A (el) |
AU (1) | AU2006311584B2 (el) |
BR (1) | BRPI0618468A2 (el) |
CA (1) | CA2629084C (el) |
CY (1) | CY1119405T1 (el) |
DK (2) | DK2623113T3 (el) |
EC (1) | ECSP088460A (el) |
ES (2) | ES2628620T3 (el) |
GT (1) | GT200800063A (el) |
HK (2) | HK1121172A1 (el) |
HN (1) | HN2008000738A (el) |
HU (1) | HUE034863T2 (el) |
IL (2) | IL191344A (el) |
LT (1) | LT2623113T (el) |
MX (1) | MX2008006090A (el) |
MY (2) | MY145757A (el) |
NZ (2) | NZ595196A (el) |
PH (1) | PH12013501656A1 (el) |
PL (2) | PL2623113T3 (el) |
PT (2) | PT2623113T (el) |
RU (2) | RU2453556C2 (el) |
SI (1) | SI2623113T1 (el) |
SV (1) | SV2009002903A (el) |
WO (1) | WO2007056464A1 (el) |
ZA (1) | ZA200804455B (el) |
Families Citing this family (36)
Publication number | Priority date | Publication date | Assignee | Title |
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US8198270B2 (en) * | 2004-04-15 | 2012-06-12 | Onyx Therapeutics, Inc. | Compounds for proteasome enzyme inhibition |
EP1745064B1 (en) | 2004-04-15 | 2011-01-05 | Proteolix, Inc. | Compounds for proteasome enzyme inhibition |
CA2565407A1 (en) * | 2004-05-10 | 2005-11-24 | Proteolix, Inc. | Compounds for enzyme inhibition |
PT2623113T (pt) | 2005-11-09 | 2017-07-14 | Onyx Therapeutics Inc | Compostos para inibição de enzimas |
SI2041158T1 (sl) * | 2006-06-19 | 2013-09-30 | Onyx Therapeutics, Inc. | Peptidni epoksiketoni za inhibicijo proteasomov |
WO2008140782A2 (en) * | 2007-05-10 | 2008-11-20 | Proteolix, Inc. | Compounds for enzyme inhibition |
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BRPI0919668A2 (pt) | 2008-10-21 | 2018-05-29 | Onyx Therapeutics, Inc. | terapia de combinação com epóxi-cetonas de peptídeo |
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MX2012011604A (es) | 2010-04-07 | 2013-02-27 | Onyx Therapeutics Inc | Inhibidor de inmunoproteasoma de péptido epoxicetona cristalino. |
WO2013112601A1 (en) | 2012-01-24 | 2013-08-01 | Millennium Pharmaceuticals, Inc. | Methods of treatment of cancer |
SG194417A1 (en) * | 2012-05-08 | 2013-12-30 | Onyx Therapeutics Inc | Cylodextrin complexation methods for formulating peptide proteasome inhibitors |
WO2014011695A2 (en) | 2012-07-09 | 2014-01-16 | Onyx Therapeutics, Inc. | Prodrugs of peptide epoxy ketone protease inhibitors |
EP2885314A4 (en) * | 2012-08-14 | 2016-02-10 | Fluorinov Pharma Inc | FLUORINATED EPOXYCETONE COMPOUNDS AND USES THEREOF AS PROTEASE INHIBITORS |
UY35091A (es) * | 2012-10-24 | 2014-05-30 | Onyx Therapeutics Inc | Formulaciones de liberacion modificada para oprozomib |
AR095426A1 (es) | 2013-03-14 | 2015-10-14 | Onyx Therapeutics Inc | Inhibidores tripeptídicos de la epoxicetona proteasa |
AU2014240122B2 (en) * | 2013-03-14 | 2019-02-14 | Onyx Therapeutics, Inc. | Dipeptide and tripeptide epoxy ketone protease inhibitors |
US20160166632A1 (en) | 2013-07-19 | 2016-06-16 | Onyx Therapeutics, Inc. | Peptide epoxyketone proteasome inhibitors in combination with pim kinase inhibitors for treatment of cancers |
CN104945470B (zh) | 2014-03-30 | 2020-08-11 | 浙江大学 | 杂环构建的三肽环氧酮类化合物及制备和应用 |
PT3166933T (pt) | 2014-07-14 | 2018-12-06 | Centrax Int Inc | Compostos de epoxicetona para inibição de enzimas |
EP3177292B1 (en) | 2014-08-07 | 2020-11-25 | Mayo Foundation for Medical Education and Research | Compounds and methods for treating cancer |
WO2016069479A1 (en) | 2014-10-27 | 2016-05-06 | Apicore Us Llc | Methods of making carfilzomib and intermediates thereof |
US9980976B2 (en) * | 2015-02-17 | 2018-05-29 | Northwestern University | Use of REDD1 inhibitors to dissociate therapeutic and adverse atrophogenic effects of glucocorticoid receptor agonists |
US11306107B2 (en) | 2016-02-25 | 2022-04-19 | Amgen Inc. | Compounds that inhibit MCL-1 protein |
SG11201811507YA (en) | 2016-06-29 | 2019-01-30 | Kezar Life Sciences | Crystalline salts of peptide epoxyketone immunoproteasome inhibitor |
KR102524751B1 (ko) | 2016-06-29 | 2023-04-21 | 케자르 라이프 사이언스 | 펩티드 에폭시케톤 면역프로테아제 저해제 및 그 전구체의 제조 방법 |
KR101720736B1 (ko) | 2016-12-15 | 2017-03-28 | 이숙자 | 스플린트용 커버 조립체 |
CA3054572A1 (en) | 2017-02-28 | 2018-09-07 | Mayo Foundation For Medical Education And Research | Compounds and methods for treating cancer |
WO2019053611A1 (en) | 2017-09-14 | 2019-03-21 | Glaxosmithkline Intellectual Property Development Limited | POLY THERAPY FOR THE TREATMENT OF CANCER |
US10537585B2 (en) | 2017-12-18 | 2020-01-21 | Dexcel Pharma Technologies Ltd. | Compositions comprising dexamethasone |
US11243207B2 (en) | 2018-03-29 | 2022-02-08 | Mayo Foundation For Medical Education And Research | Assessing and treating cancer |
CN110092813B (zh) * | 2019-06-05 | 2021-05-11 | 南京师范大学 | 一种三肽环氧丙烷衍生物及其制备方法和用途 |
WO2021221445A1 (ko) * | 2020-04-27 | 2021-11-04 | 주식회사 오토텍바이오 | Ubr 박스 도메인 리간드로의 화합물 |
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