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
-
- 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
-
- 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
-
- 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)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Physical Education & Sports Medicine (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Communicable Diseases (AREA)
- Analytical Chemistry (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Transplantation (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Tropical Medicine & Parasitology (AREA)
- Virology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (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 |
|---|---|---|---|---|
| US8716322B2 (en) | 2005-11-09 | 2014-05-06 | Onyx Therapeutics, Inc. | Compounds for enzyme inhibition |
| NZ597545A (en) | 2006-06-19 | 2013-07-26 | Proteolix Inc | Peptide epoxyketones for proteasome inhibition |
| JP5734656B2 (ja) | 2007-10-04 | 2015-06-17 | オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. | ペプチドエポキシケトンプロテアーゼ阻害剤結晶及びアミノ酸ケトエポキシドの調製 |
| EA024364B1 (ru) | 2008-10-21 | 2016-09-30 | Оникс Терапьютикс, Инк. | Способ лечения множественной миеломы |
| TWI504598B (zh) | 2009-03-20 | 2015-10-21 | Onyx Therapeutics Inc | 結晶性三肽環氧酮蛋白酶抑制劑 |
| PL3153021T3 (pl) | 2009-10-07 | 2019-05-31 | Dow Agrosciences Llc | Synergistyczne mieszaniny grzybobójcze do zwalczania grzybów w zbożach |
| WO2011060179A1 (fr) | 2009-11-13 | 2011-05-19 | Onyx Therapeutics, Inc | Utilisation de peptides epoxycetones pour la suppression de la metastase |
| CA2791651C (fr) | 2010-03-01 | 2019-08-20 | Onyx Therapeutics, Inc. | Composes pour inhibition de l'immunoproteasome |
| EP2555621A4 (fr) | 2010-04-07 | 2014-07-02 | Onyx Therapeutics Inc | Inhibiteur d'immunoprotéasome de peptide époxycétone cristallin |
| WO2014011695A2 (fr) | 2012-07-09 | 2014-01-16 | Onyx Therapeutics, Inc. | Promédicaments d'inhibiteurs d'époxy cétone protéase peptidique |
| EP2883960B1 (fr) * | 2012-08-10 | 2020-05-13 | Ajinomoto Co., Inc. | PROCÉDÉ DE PRODUCTION D'UN CRISTAL DE gamma-GLUTAMYL-VALYL-GLYCINE |
| UY35091A (es) * | 2012-10-24 | 2014-05-30 | Onyx Therapeutics Inc | Formulaciones de liberacion modificada para oprozomib |
| EP2938191B1 (fr) | 2012-12-28 | 2018-01-31 | Dow AgroSciences LLC | Mélanges fongicides synergiques destinés au contrôle d'infection fongique dans les céréales |
| 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 |
| US20160115198A1 (en) | 2014-10-27 | 2016-04-28 | Apicore Us Llc | Methods of making carfilzomib and intermediates thereof |
| KR20170100549A (ko) | 2014-12-30 | 2017-09-04 | 다우 아그로사이언시즈 엘엘씨 | 살진균 활성을 갖는 피콜린아미드 화합물 |
| US10173971B2 (en) | 2014-12-30 | 2019-01-08 | Dow Agrosciences Llc | Picolinamides with fungicidal activity |
| CN107426999B (zh) | 2014-12-30 | 2023-01-20 | 美国陶氏益农公司 | 具有杀真菌活性的吡啶酰胺化合物 |
| UA121561C2 (uk) | 2014-12-30 | 2020-06-25 | Дау Аґросаєнсиз Елелсі | Застосування сполук аміду як фунгіцидів |
| AU2015374379B2 (en) | 2014-12-30 | 2018-10-04 | Dow Agrosciences Llc | Picolinamides as fungicides |
| 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 |
| HRP20230533T1 (hr) | 2016-06-29 | 2023-08-04 | Kezar Life Sciences | Kristalne soli inhibitora imunoproteazoma za peptid epoksiketon |
| AU2017290147B2 (en) | 2016-06-29 | 2021-09-09 | Kezar Life Sciences | Process of preparing a peptide epoxyketone immunoproteasome inhibitor, and precursors thereof |
| WO2018045010A1 (fr) | 2016-08-30 | 2018-03-08 | Dow Agrosciences Llc | Composés de pyrido -1,3-oxazine -2,4-dione à activité fongicide |
| WO2018044996A1 (fr) | 2016-08-30 | 2018-03-08 | Dow Agrosciences Llc | Picolinamides utilisés en tant que fongicides |
| WO2018045006A1 (fr) | 2016-08-30 | 2018-03-08 | Dow Agrosciences Llc | Composés de n-oxyde de picolinamide à activité fongicide |
| US10231452B2 (en) | 2016-08-30 | 2019-03-19 | Dow Agrosciences Llc | Thiopicolinamide compounds with fungicidal activity |
| 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 |
| 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 |
| EP3618626A4 (fr) | 2017-05-02 | 2020-12-02 | Dow Agrosciences LLC | Utilisation d'un composé picolinamide acyclique en tant que fongicide pour lutter contre des maladies fongiques sur des gazons |
| 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 |
| CN111108125A (zh) | 2017-09-14 | 2020-05-05 | 葛兰素史密斯克莱知识产权发展有限公司 | 用于癌症的组合治疗 |
| BR102019004480B1 (pt) | 2018-03-08 | 2023-03-28 | Dow Agrosciences Llc | Picolinamidas como fungicidas |
| WO2020081382A1 (fr) | 2018-10-15 | 2020-04-23 | Dow Agrosciences Llc | Procédés de synthèse d'oxypicolinamides |
| CN114554848A (zh) | 2019-10-18 | 2022-05-27 | 科迪华农业科技有限责任公司 | 用于合成吡啶酰胺的方法 |
| 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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008140782A2 (fr) * | 2007-05-10 | 2008-11-20 | Proteolix, Inc. | Composés d'inhibition enzymatique |
Family Cites Families (94)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4733665C2 (en) | 1985-11-07 | 2002-01-29 | Expandable Grafts Partnership | Expandable intraluminal graft and method and apparatus for implanting an expandable intraluminal graft |
| US5135919A (en) | 1988-01-19 | 1992-08-04 | Children's Medical Center Corporation | Method and a pharmaceutical composition for the inhibition of angiogenesis |
| US5441944A (en) | 1989-04-23 | 1995-08-15 | The Trustees Of The University Of Pennsylvania | Substituted cyclodextrin sulfates and their uses as growth modulating agents |
| US4990448A (en) | 1989-08-04 | 1991-02-05 | Bristol-Myers Company | Bu-4061T |
| US5071957A (en) | 1989-08-04 | 1991-12-10 | Bristol-Myers Company | Antibiotic BU-4061T |
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| HUT62312A (en) | 1990-03-05 | 1993-04-28 | Cephalon Inc | Process for producing chymotrypsin-like proteases and their inhibitors |
| US5561134A (en) * | 1990-09-25 | 1996-10-01 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties |
| US5340736A (en) | 1991-05-13 | 1994-08-23 | The President & Fellows Of Harvard College | ATP-dependent protease and use of inhibitors for same in the treatment of cachexia and muscle wasting |
| WO1993025687A1 (fr) * | 1992-06-09 | 1993-12-23 | Chiron Corporation | Cristallisation du m-csf |
| GB9300048D0 (en) | 1993-01-04 | 1993-03-03 | Wellcome Found | Endothelin converting enzyme inhibitors |
| TW380137B (en) | 1994-03-04 | 2000-01-21 | Merck & Co Inc | Process for making an epoxide |
| US5693617A (en) | 1994-03-15 | 1997-12-02 | Proscript, Inc. | Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein |
| US6660268B1 (en) | 1994-03-18 | 2003-12-09 | The President And Fellows Of Harvard College | Proteasome regulation of NF-KB activity |
| US6506876B1 (en) | 1994-10-11 | 2003-01-14 | G.D. Searle & Co. | LTA4 hydrolase inhibitor pharmaceutical compositions and methods of use |
| US6083903A (en) | 1994-10-28 | 2000-07-04 | Leukosite, Inc. | Boronic ester and acid compounds, synthesis and uses |
| DE19505263A1 (de) | 1995-02-16 | 1996-08-22 | Consortium Elektrochem Ind | Verfahren zur Reinigung von wasserlöslichen Cyclodextrinderivaten |
| US6335358B1 (en) | 1995-04-12 | 2002-01-01 | President And Fellows Of Harvard College | Lactacystin analogs |
| US6150415A (en) | 1996-08-13 | 2000-11-21 | The Regents Of The University Of California | Epoxide hydrolase complexes and methods therewith |
| AU4499697A (en) | 1996-09-13 | 1998-04-02 | New York University | Method for treating parasitic diseases with proteasome inhibitors |
| CZ298749B6 (cs) | 1996-10-18 | 2008-01-16 | Vertex Pharmaceuticals Incorporated | Inhibitory serinových proteáz a farmaceutické prostředky s jejich obsahem |
| EP1136498A1 (fr) | 1996-10-18 | 2001-09-26 | Vertex Pharmaceuticals Incorporated | Inhibiteurs de sérines protéases, notamment de NS3 protéase du virus de l'hépatite c |
| US5874418A (en) | 1997-05-05 | 1999-02-23 | Cydex, Inc. | Sulfoalkyl ether cyclodextrin based solid pharmaceutical formulations and their use |
| US6046177A (en) | 1997-05-05 | 2000-04-04 | Cydex, Inc. | Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations |
| US6133248A (en) | 1997-06-13 | 2000-10-17 | Cydex, Inc. | Polar drug of prodrug compositions with extended shelf-life storage and a method of making thereof |
| US6133308A (en) | 1997-08-15 | 2000-10-17 | Millennium Pharmaceuticals, Inc. | Synthesis of clasto-lactacystin beta-lactone and analogs thereof |
| US6100282A (en) * | 1998-01-02 | 2000-08-08 | Hoffman-La Roche Inc. | Thiazole derivatives |
| US6075150A (en) | 1998-01-26 | 2000-06-13 | Cv Therapeutics, Inc. | α-ketoamide inhibitors of 20S proteasome |
| US6099851A (en) | 1998-06-02 | 2000-08-08 | Weisman; Kenneth M. | Therapeutic uses of leuprolide acetate |
| US6902721B1 (en) | 1998-07-10 | 2005-06-07 | Osteoscreen, Inc. | Inhibitors of proteasomal activity for stimulating bone growth |
| US6462019B1 (en) | 1998-07-10 | 2002-10-08 | Osteoscreen, Inc. | Inhibitors of proteasomal activity and production for stimulating bone growth |
| US6838436B1 (en) | 1998-07-10 | 2005-01-04 | Osteoscreen Inc. | Inhibitors of proteasomal activity for stimulating bone growth |
| US6204257B1 (en) | 1998-08-07 | 2001-03-20 | Universtiy Of Kansas | Water soluble prodrugs of hindered alcohols |
| NZ511197A (en) | 1998-10-20 | 2003-08-29 | Millenium Pharmaceuticals Inc | Method for monitoring proteasome inhibitor drug action |
| US6492333B1 (en) | 1999-04-09 | 2002-12-10 | Osteoscreen, Inc. | Treatment of myeloma bone disease with proteasomal and NF-κB activity inhibitors |
| US6831099B1 (en) | 1999-05-12 | 2004-12-14 | Yale University | Enzyme inhibition |
| US6114365A (en) * | 1999-08-12 | 2000-09-05 | Pharmacia & Upjohn S.P.A. | Arylmethyl-carbonylamino-thiazole derivatives, process for their preparation, and their use as antitumor agents |
| JP2003528039A (ja) | 1999-10-20 | 2003-09-24 | オステオスクリーン,インコーポレイテッド | 骨および毛成長を刺激するためのプロテアソーム活性のインヒビター |
| EP2301565A1 (fr) | 2000-10-12 | 2011-03-30 | ViroLogik GmbH | Inhibiteurs du proteasome pour le traitement des infections virales |
| GB0114185D0 (en) * | 2001-06-12 | 2001-08-01 | Protherics Molecular Design Lt | Compounds |
| DK3078667T3 (en) | 2001-01-25 | 2019-01-07 | The United States Of America Represented By The Sec Dep Of Health And Human Services | Formulation of boric acid compounds |
| ES2278049T3 (es) | 2001-05-21 | 2007-08-01 | Alcon, Inc. | Uso de inhibidores de proteasoma para tratar trastornos de ojo seco. |
| EP1463719A2 (fr) | 2002-01-08 | 2004-10-06 | Eisai Co., Ltd | Analogues d'eponemycine et d'epoxomicine et leurs utilisations |
| US20040116329A1 (en) | 2002-01-29 | 2004-06-17 | Epstein Stephen E. | Inhibition of proteasomes to prevent restenosis |
| WO2003086283A2 (fr) | 2002-04-09 | 2003-10-23 | Greenville Hospital System | Activite de modulation de metastase d'oligosaccharides hautement sulfates |
| US7968569B2 (en) | 2002-05-17 | 2011-06-28 | Celgene Corporation | Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione |
| US7902185B2 (en) | 2002-06-03 | 2011-03-08 | Als Therapy Development Foundation, Inc. | Treatment of neurodegenerative diseases using proteasome modulators |
| US20030224469A1 (en) | 2002-06-03 | 2003-12-04 | Buchholz Tonia J. | Methods and kits for assays utilizing fluorescence polarization |
| WO2004010937A2 (fr) | 2002-07-26 | 2004-02-05 | Advanced Research & Technology Institute At Indiana University | Methode de traitement du cancer |
| US7189740B2 (en) | 2002-10-15 | 2007-03-13 | Celgene Corporation | Methods of using 3-(4-amino-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myelodysplastic syndromes |
| TW200418791A (en) | 2003-01-23 | 2004-10-01 | Bristol Myers Squibb Co | Pharmaceutical compositions for inhibiting proteasome |
| BRPI0409250B8 (pt) | 2003-04-08 | 2022-01-18 | Mitsubishi Pharma Corp | Composições farmacêuticas sólidas compreendendo um agonista receptor de s1p e um álcool do açúcar |
| JP4653103B2 (ja) | 2003-06-10 | 2011-03-16 | ザ ジェイ.ディヴィッド グラッドストン インスティテューツ | レンチウイルス感染症を治療するための方法 |
| US7012063B2 (en) | 2003-06-13 | 2006-03-14 | Children's Medical Center Corporation | Reducing axon degeneration with proteasome inhibitors |
| CA2552641A1 (fr) | 2003-12-31 | 2005-07-21 | Cydex, Inc. | Formulation pour inhalation contenant du sulfoalkyle ether cyclodextrine et un corticosteroide, a base d'une suspension en doses unitaires |
| GB0400804D0 (en) | 2004-01-14 | 2004-02-18 | Innoscience Technology Bv | Pharmaceutical compositions |
| US20050228031A1 (en) * | 2004-04-13 | 2005-10-13 | Bilodeau Mark T | Tyrosine kinase inhibitors |
| US8129346B2 (en) | 2004-04-15 | 2012-03-06 | Onyx Therapeutics, Inc. | Compounds for enzyme inhibition |
| US8198270B2 (en) | 2004-04-15 | 2012-06-12 | Onyx Therapeutics, Inc. | Compounds for proteasome enzyme inhibition |
| US7232818B2 (en) | 2004-04-15 | 2007-06-19 | Proteolix, Inc. | Compounds for enzyme inhibition |
| WO2005111009A2 (fr) | 2004-05-10 | 2005-11-24 | Proteolix, Inc. | Synthese de ceto-epoxydes d'acides amines |
| ES2510840T3 (es) | 2004-05-10 | 2014-10-21 | Onyx Therapeutics, Inc. | Compuestos para la inhibición enzimática del proteosoma |
| ES2359004T3 (es) * | 2004-08-06 | 2011-05-17 | Onyx Therapeutics, Inc. | Compuestos para inhibición enzimática de proteasoma. |
| EP2100899A3 (fr) | 2004-10-20 | 2009-09-30 | Proteolix, Inc. | Composés pour inhibition d'enzyme |
| WO2006063154A1 (fr) | 2004-12-07 | 2006-06-15 | Proteolix, Inc. | Composition destinee a inhiber le proteasome |
| US7468383B2 (en) | 2005-02-11 | 2008-12-23 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| EP1863513A2 (fr) * | 2005-03-11 | 2007-12-12 | The University of North Carolina at Chapel Hill | Inhibiteurs puissants et spécifiques d'immunoprotéasomes |
| US7998938B2 (en) | 2005-04-15 | 2011-08-16 | Geron Corporation | Cancer treatment by combined inhibition of proteasome and telomerase activities |
| GT200600350A (es) | 2005-08-09 | 2007-03-28 | Formulaciones líquidas | |
| US8716322B2 (en) | 2005-11-09 | 2014-05-06 | Onyx Therapeutics, Inc. | Compounds for enzyme inhibition |
| AR057227A1 (es) | 2005-12-09 | 2007-11-21 | Centocor Inc | Metodo para usar antagonistas de il6 con inhibidores del proteasoma |
| US20070207950A1 (en) | 2005-12-21 | 2007-09-06 | Duke University | Methods and compositions for regulating HDAC6 activity |
| WO2007122686A1 (fr) | 2006-04-14 | 2007-11-01 | Eisai R & D Management Co., Ltd. | Composes benzimidazole |
| DE102006026464A1 (de) | 2006-06-01 | 2007-12-06 | Virologik Gmbh Innovationszentrum Medizintechnik Und Pharma | Pharmazeutische Zusammensetzung zur Behandlung von Virusinfektionen und / oder Tumorerkrankungen durch Inhibition der Proteinfaltung und des Proteinabbaus |
| NZ597545A (en) | 2006-06-19 | 2013-07-26 | Proteolix Inc | Peptide epoxyketones for proteasome inhibition |
| WO2008033807A2 (fr) | 2006-09-13 | 2008-03-20 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Combinaisons synergiques d'oxydants mitochondriaux antinéoplasiques se liant au thiol et d'inhibiteurs du protéasome antinéoplasiques pour le traitement du cancer |
| US8601054B2 (en) * | 2006-12-07 | 2013-12-03 | International Business Machines Corporation | Project-related communications |
| AU2008209555A1 (en) | 2007-01-23 | 2008-07-31 | Gloucester Pharmaceuticals, Inc. | Combination therapy comprising romidepsin and I.A. bortezomib |
| US7442830B1 (en) | 2007-08-06 | 2008-10-28 | Millenium Pharmaceuticals, Inc. | Proteasome inhibitors |
| MY161991A (en) | 2007-08-06 | 2017-05-31 | Millennium Pharm Inc | Proteasome inhibitors |
| JP5734656B2 (ja) | 2007-10-04 | 2015-06-17 | オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. | ペプチドエポキシケトンプロテアーゼ阻害剤結晶及びアミノ酸ケトエポキシドの調製 |
| JP5600595B2 (ja) | 2007-10-16 | 2014-10-01 | ミレニアム ファーマシューティカルズ, インコーポレイテッド | プロテアソーム阻害剤 |
| US7838673B2 (en) | 2007-10-16 | 2010-11-23 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
| WO2009067453A1 (fr) | 2007-11-19 | 2009-05-28 | Syndax Pharmaceuticals, Inc. | Combinaisons d'inhibiteurs de la hdac et d'inhibiteurs de protéasomes |
| DK2730581T3 (en) | 2008-06-17 | 2016-08-15 | Millennium Pharm Inc | Boronate Ester Compounds and Pharmaceutical Compositions thereof. |
| AR075090A1 (es) | 2008-09-29 | 2011-03-09 | Millennium Pharm Inc | Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden. |
| EA024364B1 (ru) | 2008-10-21 | 2016-09-30 | Оникс Терапьютикс, Инк. | Способ лечения множественной миеломы |
| TWI504598B (zh) | 2009-03-20 | 2015-10-21 | Onyx Therapeutics Inc | 結晶性三肽環氧酮蛋白酶抑制劑 |
| CN101928329B (zh) | 2009-06-19 | 2013-07-17 | 北京大学 | 三肽硼酸(酯)类化合物、其制备方法和应用 |
| WO2011060179A1 (fr) | 2009-11-13 | 2011-05-19 | Onyx Therapeutics, Inc | Utilisation de peptides epoxycetones pour la suppression de la metastase |
| CA2791651C (fr) | 2010-03-01 | 2019-08-20 | Onyx Therapeutics, Inc. | Composes pour inhibition de l'immunoproteasome |
| AU2011235227B2 (en) | 2010-03-31 | 2016-09-08 | Millennium Pharmaceuticals, Inc. | Derivatives of 1-amino-2-cyclopropylethylboronic acid |
| EP2555621A4 (fr) | 2010-04-07 | 2014-07-02 | Onyx Therapeutics Inc | Inhibiteur d'immunoprotéasome de peptide époxycétone cristallin |
-
2010
- 2010-03-19 TW TW099108136A patent/TWI504598B/zh not_active IP Right Cessation
- 2010-03-19 AR ARP100100894A patent/AR075899A1/es unknown
- 2010-03-20 SA SA110310221A patent/SA110310221B1/ar unknown
- 2010-03-20 SA SA114350283A patent/SA114350283B1/ar unknown
- 2010-03-22 GE GEAP201012421A patent/GEP20156392B/en unknown
- 2010-03-22 KR KR1020117022814A patent/KR101729344B1/ko not_active Expired - Fee Related
- 2010-03-22 PL PL14178725T patent/PL2813241T3/pl unknown
- 2010-03-22 MA MA34254A patent/MA33197B1/fr unknown
- 2010-03-22 PL PL10754225T patent/PL2408758T3/pl unknown
- 2010-03-22 PT PT141787259T patent/PT2813241T/pt unknown
- 2010-03-22 MY MYPI2011004414A patent/MY156522A/en unknown
- 2010-03-22 EA EA201300860A patent/EA024672B1/ru not_active IP Right Cessation
- 2010-03-22 JP JP2012501028A patent/JP5723357B2/ja active Active
- 2010-03-22 ES ES10754225.0T patent/ES2527619T3/es active Active
- 2010-03-22 CA CA2755971A patent/CA2755971C/fr not_active Expired - Fee Related
- 2010-03-22 DK DK10754225.0T patent/DK2408758T3/da active
- 2010-03-22 NZ NZ61843210A patent/NZ618432A/en not_active IP Right Cessation
- 2010-03-22 RS RS20161122A patent/RS55431B1/sr unknown
- 2010-03-22 EA EA201171151A patent/EA020973B1/ru not_active IP Right Cessation
- 2010-03-22 US US12/728,547 patent/US20100240903A1/en not_active Abandoned
- 2010-03-22 PT PT107542250T patent/PT2408758E/pt unknown
- 2010-03-22 AU AU2010226410A patent/AU2010226410B2/en not_active Ceased
- 2010-03-22 ME MEP-2011-164A patent/ME01277B/me unknown
- 2010-03-22 MX MX2011009777A patent/MX2011009777A/es active IP Right Grant
- 2010-03-22 MX MX2013012107A patent/MX343562B/es unknown
- 2010-03-22 SM SM20170068T patent/SMT201700068T1/it unknown
- 2010-03-22 LT LTEP14178725.9T patent/LT2813241T/lt unknown
- 2010-03-22 AP AP2013007137A patent/AP3513A/xx active
- 2010-03-22 BR BRPI1009369A patent/BRPI1009369A2/pt not_active Application Discontinuation
- 2010-03-22 PE PE2011001673A patent/PE20120645A1/es active IP Right Grant
- 2010-03-22 WO PCT/US2010/028126 patent/WO2010108172A1/fr not_active Ceased
- 2010-03-22 HU HUE14178725A patent/HUE032430T2/en unknown
- 2010-03-22 SI SI201031354A patent/SI2813241T1/sl unknown
- 2010-03-22 HR HRP20150014AT patent/HRP20150014T1/hr unknown
- 2010-03-22 NZ NZ595847A patent/NZ595847A/en not_active IP Right Cessation
- 2010-03-22 DK DK14178725.9T patent/DK2813241T3/en active
- 2010-03-22 SI SI201030833T patent/SI2408758T1/sl unknown
- 2010-03-22 ES ES14178725.9T patent/ES2614557T3/es active Active
- 2010-03-22 EP EP10754225.0A patent/EP2408758B1/fr active Active
- 2010-03-22 SG SG2014011373A patent/SG2014011373A/en unknown
- 2010-03-22 EP EP14178725.9A patent/EP2813241B1/fr active Active
- 2010-03-22 US US13/257,887 patent/US8604215B2/en not_active Expired - Fee Related
- 2010-03-22 RS RS20150015A patent/RS53746B1/sr unknown
- 2010-03-22 SG SG2011067204A patent/SG174446A1/en unknown
- 2010-03-22 CN CN201080021879.8A patent/CN102428075B/zh not_active Expired - Fee Related
-
2011
- 2011-09-15 IL IL215174A patent/IL215174A/en not_active IP Right Cessation
- 2011-09-16 CO CO11120506A patent/CO6430433A2/es not_active Application Discontinuation
- 2011-09-16 DO DO2011000286A patent/DOP2011000286A/es unknown
- 2011-09-19 TN TN2011000470A patent/TN2011000470A1/fr unknown
- 2011-09-19 CR CR20110491A patent/CR20110491A/es unknown
- 2011-09-19 ZA ZA2011/06826A patent/ZA201106826B/en unknown
- 2011-09-20 CL CL2011002326A patent/CL2011002326A1/es unknown
- 2011-09-20 EC EC2011011341A patent/ECSP11011341A/es unknown
- 2011-09-20 US US13/237,655 patent/US8822512B2/en not_active Expired - Fee Related
- 2011-09-20 NI NI201100170A patent/NI201100170A/es unknown
- 2011-09-20 CU CU20110176A patent/CU20110176A7/es unknown
- 2011-09-20 HN HN2011002459A patent/HN2011002459A/es unknown
-
2013
- 2013-09-24 US US14/035,644 patent/US9051353B2/en not_active Expired - Fee Related
-
2015
- 2015-01-12 SM SM201500009T patent/SMT201500009B/xx unknown
- 2015-03-05 US US14/639,603 patent/US9403868B2/en not_active Expired - Fee Related
-
2016
- 2016-03-11 ZA ZA2016/01686A patent/ZA201601686B/en unknown
- 2016-12-06 HR HRP20161654TT patent/HRP20161654T1/hr unknown
- 2016-12-16 CY CY20161101307T patent/CY1118359T1/el unknown
-
2017
- 2017-01-30 SM SM201700068T patent/SMT201700068B/it unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008140782A2 (fr) * | 2007-05-10 | 2008-11-20 | Proteolix, Inc. | Composés d'inhibition enzymatique |
Non-Patent Citations (1)
| Title |
|---|
| GROLL M. et al. "Crystal Structure of Epoxomicin:20S Proteasome Reveals a Molecular Basis for Selectivity of alpha',beta'-Epoxyketone Proteasome Inhibitors", J. Am. Chem. Soc., 2000, 122, 1237-1238. See whole document; figures 1&2 * |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AP3513A (en) | Crystalline tripeptide epoxy ketone protease inhibitors | |
| ZA201202631B (en) | Hcv protease inhibitors | |
| ZA201008988B (en) | Hcv protease inhibitors | |
| ZA201107636B (en) | Protease inhibitors | |
| IL222330A0 (en) | Crystalline peptide epoxyketone immunoproteasome inhibitor | |
| EP2509956A4 (fr) | Inhibiteurs des cystéine protéases | |
| EP2313426A4 (fr) | Nouveaux inhibiteurs de protéases | |
| ZA201102179B (en) | Protease inhibitors | |
| ZA201200811B (en) | Cathepsin c inhibitors | |
| AP2912A (en) | Crystalline tripeptide epoxy protease inhibitors | |
| GB0817425D0 (en) | Protease inhibitors | |
| SG2014011258A (en) | Hcv protease inhibitors | |
| AU2009902963A0 (en) | Novel protease inhibitors | |
| HK1175945A (en) | Crystalline peptide epoxyketone immunoproteasome inhibitor | |
| TWM379488U (en) | Improved screwdriver stem | |
| GB0915927D0 (en) | Novel inhibitors | |
| GB0902661D0 (en) | Inhibitors | |
| GB0903650D0 (en) | Glyoalase inhibitors |