AP3513A - Crystalline tripeptide epoxy ketone protease inhibitors - Google Patents
Crystalline tripeptide epoxy ketone protease inhibitorsInfo
- Publication number
- AP3513A AP3513A AP2013007137A AP2013007137A AP3513A AP 3513 A AP3513 A AP 3513A AP 2013007137 A AP2013007137 A AP 2013007137A AP 2013007137 A AP2013007137 A AP 2013007137A AP 3513 A AP3513 A AP 3513A
- Authority
- AP
- ARIPO
- Prior art keywords
- protease inhibitors
- epoxy ketone
- ketone protease
- tripeptide epoxy
- crystalline tripeptide
- Prior art date
Links
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 title 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
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
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- A61P31/04—Antibacterial agents
-
- 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
- A61P33/00—Antiparasitic agents
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- A61P37/08—Antiallergic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07K1/02—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution
- C07K1/026—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution by fragment condensation in solution
-
- 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
-
- 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
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- 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
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Communicable Diseases (AREA)
- Analytical Chemistry (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Virology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Tropical Medicine & Parasitology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16219609P | 2009-03-20 | 2009-03-20 | |
| US18056109P | 2009-05-22 | 2009-05-22 | |
| PCT/US2010/028126 WO2010108172A1 (fr) | 2009-03-20 | 2010-03-22 | Inhibiteurs de tripeptide époxy cétone protéases cristallines |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AP2013007137A0 AP2013007137A0 (en) | 2013-09-30 |
| AP3513A true AP3513A (en) | 2016-01-05 |
Family
ID=42738216
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AP2013007137A AP3513A (en) | 2009-03-20 | 2010-03-22 | Crystalline tripeptide epoxy ketone protease inhibitors |
Country Status (44)
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5436860B2 (ja) * | 2005-11-09 | 2014-03-05 | オニキス セラピューティクス, インク. | 酵素阻害のための化合物 |
| NZ573759A (en) | 2006-06-19 | 2012-03-30 | Proteolix Inc | Peptide epoxyketones for proteasome inhibition |
| EA018973B1 (ru) | 2007-10-04 | 2013-12-30 | Оникс Терапьютикс, Инк. | Кристаллические пептидные кето-эпоксидные ингибиторы протеаз и синтез кето-эпоксидов аминокислот |
| BRPI0919668A2 (pt) | 2008-10-21 | 2018-05-29 | Onyx Therapeutics, Inc. | terapia de combinação com epóxi-cetonas de peptídeo |
| AR075899A1 (es) | 2009-03-20 | 2011-05-04 | Onyx Therapeutics Inc | Tripeptidos epoxicetonas cristalinos inhibidores de proteasa |
| HUE042624T2 (hu) | 2009-10-07 | 2019-07-29 | Dow Agrosciences Llc | Szinergetikus fungicid keverékek gombák kontrollálására gabonafélékben |
| EP2498793B1 (fr) | 2009-11-13 | 2019-07-10 | Onyx Therapeutics, Inc. | Oprozomib pour l'utilsation dans la suppression des metastases |
| PH12012501719A1 (en) | 2010-03-01 | 2012-11-12 | Onyx Therapeutics Inc | Compounds for immunoproteasome inhibition |
| US8697646B2 (en) | 2010-04-07 | 2014-04-15 | Onyx Therapeutics, Inc. | Crystalline peptide epoxyketone immunoproteasome inhibitor |
| US9309283B2 (en) | 2012-07-09 | 2016-04-12 | Onyx Therapeutics, Inc. | Prodrugs of peptide epoxy ketone protease inhibitors |
| MY169137A (en) * | 2012-08-10 | 2019-02-18 | Ajinomoto Kk | Method for producing ?-gamma-glutamyl-valyl-glycine crystal |
| UY35091A (es) * | 2012-10-24 | 2014-05-30 | Onyx Therapeutics Inc | Formulaciones de liberacion modificada para oprozomib |
| LT2938191T (lt) | 2012-12-28 | 2018-05-10 | Dow Agrosciences Llc | Sinergistiniai fungicidiniai mišiniai, skirti grybelių kontrolei javuose |
| WO2015100184A1 (fr) | 2013-12-26 | 2015-07-02 | Dow Agrosciences Llc | Utilisation de picolinamides macrocycliques en tant que fongicides |
| 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 |
| CN104974221B (zh) * | 2014-04-03 | 2020-10-23 | 中国医学科学院药物研究所 | 二肽及三肽类蛋白酶体抑制剂及其制法和药物用途 |
| EP3166936A4 (fr) | 2014-07-08 | 2017-11-22 | Dow AgroSciences LLC | Picolinamides macrocycliques à utiliser en tant que fongicides |
| WO2016069479A1 (fr) | 2014-10-27 | 2016-05-06 | Apicore Us Llc | Procédés de préparation de carfilzomib et d'intermédiaires de celui-ci |
| US20170290333A1 (en) | 2014-12-30 | 2017-10-12 | Dow Agrosciences Llc | Picolinamide compounds with fungicidal activity |
| EP3240412A4 (fr) | 2014-12-30 | 2018-04-25 | Dow Agrosciences LLC | Utilisation de composés de picolinamide présentant une activité fongicide |
| CA2972408A1 (fr) | 2014-12-30 | 2016-07-07 | Dow Agrosciences Llc | Utilisation de composes de picolinamide presentant une activite fongicide |
| NZ732812A (en) | 2014-12-30 | 2019-01-25 | Dow Agrosciences Llc | Use of picolinamides and other compounds as fungicides |
| AU2015374375B2 (en) * | 2014-12-30 | 2019-03-21 | Dow Agrosciences Llc | Picolinamides with fungicidal activity |
| CN105949279A (zh) * | 2016-04-27 | 2016-09-21 | 浙江大学 | 蛋白酶体抑制剂Oprozomib及其类似物的制备方法 |
| FI3478670T3 (fi) | 2016-06-29 | 2023-05-04 | Kezar Life Sciences | Peptidi-epoksiketoni-immunoproteasomi-estäjän kiteiset suolat |
| IL263771B2 (en) | 2016-06-29 | 2023-09-01 | Kezar Life Sciences | Preparation process of immunoproteasome epoxytone peptide inhibitor and its precursors |
| US10334852B2 (en) | 2016-08-30 | 2019-07-02 | Dow Agrosciences Llc | Pyrido-1,3-oxazine-2,4-dione compounds with fungicidal activity |
| WO2018045003A1 (fr) | 2016-08-30 | 2018-03-08 | Dow Agrosciences Llc | Composés de n-oxdes de picolinamide à activité fongicide |
| WO2018044987A1 (fr) | 2016-08-30 | 2018-03-08 | Dow Agrosciences Llc | Composés de thiopicolinamide à activité fongicide |
| US10214490B2 (en) | 2016-08-30 | 2019-02-26 | Dow Agrosciences Llc | Picolinamides as fungicides |
| US20180078532A1 (en) | 2016-09-21 | 2018-03-22 | Amgen Inc. | Immediate release formulations for oprozomib |
| US20180161279A1 (en) | 2016-12-14 | 2018-06-14 | Amgen Inc. | Gastro-retentive modified release dosage forms for oprozomib and process to make thereof |
| BR102018000183B1 (pt) | 2017-01-05 | 2023-04-25 | Dow Agrosciences Llc | Picolinamidas, composição para controle de um patógeno fúngico, e método para controle e prevenção de um ataque por fungos em uma planta |
| TWI774761B (zh) | 2017-05-02 | 2022-08-21 | 美商科迪華農業科技有限責任公司 | 用於穀物中的真菌防治之協同性混合物 |
| CN110996665B (zh) | 2017-05-02 | 2021-10-26 | 陶氏益农公司 | 无环吡啶酰胺化合物作为针对草坪草上的真菌病害的杀真菌剂的用途 |
| TW201842851A (zh) | 2017-05-02 | 2018-12-16 | 美商陶氏農業科學公司 | 用於穀類中的真菌防治之協同性混合物 |
| JP2020533382A (ja) | 2017-09-14 | 2020-11-19 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited | 癌の組合せ治療 |
| BR102019004480B1 (pt) | 2018-03-08 | 2023-03-28 | Dow Agrosciences Llc | Picolinamidas como fungicidas |
| US11639334B2 (en) | 2018-10-15 | 2023-05-02 | Corteva Agriscience Llc | Methods for synthesis of oxypicolinamides |
| EP4044811A4 (fr) | 2019-10-18 | 2023-09-27 | Corteva Agriscience LLC | Procédé de synthèse de picolinamides |
| TWI869142B (zh) * | 2022-12-27 | 2025-01-01 | 大陸商上海美悦生物科技發展有限公司 | 三肽環氧酮化合物、藥物組合物及其製備方法和用途 |
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| WO2008140782A2 (fr) * | 2007-05-10 | 2008-11-20 | Proteolix, Inc. | Composés d'inhibition enzymatique |
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