AR075899A1 - Tripeptidos epoxicetonas cristalinos inhibidores de proteasa - Google Patents
Tripeptidos epoxicetonas cristalinos inhibidores de proteasaInfo
- Publication number
- AR075899A1 AR075899A1 ARP100100894A ARP100100894A AR075899A1 AR 075899 A1 AR075899 A1 AR 075899A1 AR P100100894 A ARP100100894 A AR P100100894A AR P100100894 A ARP100100894 A AR P100100894A AR 075899 A1 AR075899 A1 AR 075899A1
- Authority
- AR
- Argentina
- Prior art keywords
- crystalline
- tripeptides
- epoxyceton
- proteasa
- formula
- Prior art date
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
- 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)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (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)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (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)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Virology (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
Abstract
La presente se refiere a compuestos ceto epoxido de tripéptidos cristalinos, a métodos para su preparacion y a composiciones farmacéuticas relacionadas. El compuesto tripéptido epoxi cetona cristalinos, inhibidores del proteasoma de formula (2). Reivindicacion 1: Un método para preparar un compuesto cristalino de formula (2) que comprende (i) preparar una solucion de un compuesto de formula (2) en un disolvente orgánico; (ii) llevar la solucion a supersaturacion para provocar la formacion de cristales; y (iii) aislar los cristales.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16219609P | 2009-03-20 | 2009-03-20 | |
| US18056109P | 2009-05-22 | 2009-05-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR075899A1 true AR075899A1 (es) | 2011-05-04 |
Family
ID=42738216
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100100894A AR075899A1 (es) | 2009-03-20 | 2010-03-19 | Tripeptidos epoxicetonas cristalinos inhibidores de proteasa |
Country Status (45)
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY145757A (en) | 2005-11-09 | 2012-04-13 | Proteolix Inc | Compounds for enzyme inhibition |
| SI2041158T1 (sl) | 2006-06-19 | 2013-09-30 | Onyx Therapeutics, Inc. | Peptidni epoksiketoni za inhibicijo proteasomov |
| DK2207791T4 (da) | 2007-10-04 | 2019-10-07 | Onyx Therapeutics Inc | Krystallinske peptidepoxyketon-proteasehæmmere og syntese af aminosyreketoepoxider |
| ES2617560T3 (es) * | 2008-10-21 | 2017-06-19 | Onyx Therapeutics, Inc. | Combinación del inhibidor del proteasoma de epoxicetona peptídica carfilzomib con melfalán para su uso en el tratamiento del mieloma múltiple |
| 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 |
| EP3153021B1 (en) | 2009-10-07 | 2018-11-28 | Dow AgroSciences LLC | Synergistic fungicidial mixtures for fungal control in cereals |
| JP5919196B2 (ja) | 2009-11-13 | 2016-05-18 | オニキス セラピューティクス， インク．Ｏｎｙｘ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． | 転移抑制のためのペプチドエポキシケトンの使用 |
| WO2011109355A1 (en) | 2010-03-01 | 2011-09-09 | Onyx Therapeutics, Inc. | Compounds for immunoproteasome inhibition |
| CN102946729B (zh) | 2010-04-07 | 2014-11-05 | 欧尼斯治疗公司 | 结晶肽环氧酮免疫蛋白酶体抑制剂 |
| US9309283B2 (en) | 2012-07-09 | 2016-04-12 | Onyx Therapeutics, Inc. | Prodrugs of peptide epoxy ketone protease inhibitors |
| CN104540959B (zh) * | 2012-08-10 | 2018-11-13 | 味之素株式会社 | γ-谷氨酰缬氨酰甘氨酸晶体的制备方法 |
| UY35091A (es) * | 2012-10-24 | 2014-05-30 | Onyx Therapeutics Inc | Formulaciones de liberacion modificada para oprozomib |
| ES2666144T3 (es) | 2012-12-28 | 2018-05-03 | Dow Agrosciences Llc | Mezclas fungicidas sinérgicas para control fúngico en cereales |
| WO2015100184A1 (en) | 2013-12-26 | 2015-07-02 | Dow Agrosciences Llc | Use of macrocyclic picolinamides as fungicides |
| 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 |
| CN106470982A (zh) | 2014-07-08 | 2017-03-01 | 美国陶氏益农公司 | 作为杀真菌剂的大环吡啶酰胺 |
| WO2016069479A1 (en) | 2014-10-27 | 2016-05-06 | Apicore Us Llc | Methods of making carfilzomib and intermediates thereof |
| CN107427000A (zh) | 2014-12-30 | 2017-12-01 | 美国陶氏益农公司 | 具有杀真菌活性的吡啶酰胺化合物的用途 |
| AU2015374379B2 (en) | 2014-12-30 | 2018-10-04 | Dow Agrosciences Llc | Picolinamides as fungicides |
| CN113173838A (zh) | 2014-12-30 | 2021-07-27 | 美国陶氏益农公司 | 具有杀真菌活性的吡啶酰胺化合物 |
| JP6603720B2 (ja) | 2014-12-30 | 2019-11-06 | ダウ アグロサイエンシィズ エルエルシー | 殺真菌活性を有するピコリンアミド化合物の使用 |
| 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 |
| EP4296257A3 (en) | 2016-06-29 | 2024-03-20 | Kezar Life Sciences | Process of preparing a peptide epoxyketone immunoproteasome inhibitor |
| CA3029032A1 (en) | 2016-06-29 | 2018-01-04 | Henry Johnson | Crystalline salts of peptide epoxyketone immunoproteasome inhibitor |
| US10334852B2 (en) | 2016-08-30 | 2019-07-02 | Dow Agrosciences Llc | Pyrido-1,3-oxazine-2,4-dione compounds with fungicidal activity |
| US10173982B2 (en) | 2016-08-30 | 2019-01-08 | Dow Agrosciences Llc | Picolinamides as fungicides |
| WO2018045006A1 (en) | 2016-08-30 | 2018-03-08 | Dow Agrosciences Llc | Picolinamide n-oxide compounds with fungicidal activity |
| WO2018044991A1 (en) | 2016-08-30 | 2018-03-08 | Dow Agrosciences Llc | Thiopicolinamide compounds with fungicidal activity |
| US20180078532A1 (en) | 2016-09-21 | 2018-03-22 | Amgen Inc. | Immediate release formulations for oprozomib |
| JP2018123119A (ja) | 2016-12-14 | 2018-08-09 | アムジエン・インコーポレーテツド | オプロゾミブのための胃内保持型の徐放性剤形、及びその調製プロセス |
| 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 |
| 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 |
| 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 |
| CA3075714A1 (en) | 2017-09-14 | 2019-03-21 | Glaxosmithkline Intellectual Property Development Limited | Combination treatment for cancer |
| BR102019004480B1 (pt) | 2018-03-08 | 2023-03-28 | Dow Agrosciences Llc | Picolinamidas como fungicidas |
| MX2021004298A (es) | 2018-10-15 | 2021-06-08 | Corteva Agriscience Llc | Metodos de sintesis de oxipicolinamidas. |
Family Cites Families (95)
| 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 |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| AU661270B2 (en) | 1990-03-05 | 1995-07-20 | Cephalon, Inc. | 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 |
| EP0668914B1 (en) * | 1992-06-09 | 2000-08-16 | Chiron Corporation | Crystallization of 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 |
| ES2169880T3 (es) | 1996-10-18 | 2002-07-16 | Vertex Pharma | Inhibidores de proteasas de serina, particularmente de la proteasa ns3 del virus de la hepatitis c. |
| SI0932617T1 (en) | 1996-10-18 | 2002-06-30 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
| US6046177A (en) | 1997-05-05 | 2000-04-04 | Cydex, Inc. | Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations |
| US5874418A (en) | 1997-05-05 | 1999-02-23 | Cydex, Inc. | Sulfoalkyl ether cyclodextrin based solid pharmaceutical formulations and their use |
| JP4439596B2 (ja) | 1997-06-13 | 2010-03-24 | サイデクス ファーマシューティカルズ、 インク． | 長期の貯蔵寿命を有する、極性薬物又は極性プロドラッグを含有する医薬組成物、及びその製造方法 |
| 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 |
| US6838436B1 (en) | 1998-07-10 | 2005-01-04 | 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 |
| US6204257B1 (en) | 1998-08-07 | 2001-03-20 | Universtiy Of Kansas | Water soluble prodrugs of hindered alcohols |
| WO2000023614A1 (en) | 1998-10-20 | 2000-04-27 | Millennium 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 |
| EP1221962A2 (en) | 1999-10-20 | 2002-07-17 | Osteoscreen, Inc. | Inhibitors of proteasomal activity for stimulating bone and hair growth |
| EP1430903A1 (de) | 2000-10-12 | 2004-06-23 | Viromics Gmbh | Verwendung von Proteasome Hemmern zur Behandlung von Virus-Infektionen |
| GB0114185D0 (en) * | 2001-06-12 | 2001-08-01 | Protherics Molecular Design Lt | Compounds |
| EP1355910B1 (en) | 2001-01-25 | 2011-03-09 | The United States of America, represented by the Secretary, Department of Health and Human Services | Formulation of boronic acid compounds |
| DK1392355T3 (da) | 2001-05-21 | 2007-04-30 | Alcon Inc | Anvendelse af proteasominhibitorer tilbehandling af öjentörhedslidelser |
| AU2003219652A1 (en) | 2002-01-08 | 2003-07-30 | Eisai Co. Ltd. | Eponemycin and epoxomicin analogs and uses thereof |
| US20040116329A1 (en) | 2002-01-29 | 2004-06-17 | Epstein Stephen E. | Inhibition of proteasomes to prevent restenosis |
| AU2003220685A1 (en) | 2002-04-09 | 2003-10-27 | Greenville Hospital System | Metastasis modulating activity of highly sulfated oligosaccharides |
| 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 |
| US20030224469A1 (en) | 2002-06-03 | 2003-12-04 | Buchholz Tonia J. | Methods and kits for assays utilizing fluorescence polarization |
| AU2003249682A1 (en) | 2002-06-03 | 2003-12-19 | Als Therapy Development Foundation | Treatment of neurodegenerative diseases using proteasome modulators |
| WO2004010937A2 (en) | 2002-07-26 | 2004-02-05 | Advanced Research & Technology Institute At Indiana University | Method of treating 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 |
| NZ542622A (en) | 2003-04-08 | 2009-01-31 | Novartis Ag | Solid pharmaceutical compositions comprising a S1P receptor agonist and a sugar alcohol |
| CA2528120A1 (en) | 2003-06-10 | 2005-01-20 | The J. David Gladstone Institutes | Methods for treating lentivirus infections |
| US7012063B2 (en) | 2003-06-13 | 2006-03-14 | Children's Medical Center Corporation | Reducing axon degeneration with proteasome inhibitors |
| MX348041B (es) | 2003-12-31 | 2017-05-25 | Cydex Pharmaceuticals Inc | Formulación inhalante que contiene éter sulfoalquilico-ciclodextri na y un corticosteroide. |
| 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 |
| US8198270B2 (en) | 2004-04-15 | 2012-06-12 | Onyx Therapeutics, Inc. | Compounds for proteasome enzyme inhibition |
| PT1745064E (pt) | 2004-04-15 | 2011-03-23 | Proteolix Inc | Compostos para a inibição de uma enzima de proteassoma |
| US7232818B2 (en) | 2004-04-15 | 2007-06-19 | Proteolix, Inc. | Compounds for enzyme inhibition |
| EP1758921A2 (en) | 2004-05-10 | 2007-03-07 | Proteolix, Inc. | Compounds for proteasome enzyme inhibition |
| US20050256324A1 (en) | 2004-05-10 | 2005-11-17 | Proteolix, Inc. | Synthesis of amino acid keto-epoxides |
| CN101044157B (zh) * | 2004-08-06 | 2011-07-13 | 普罗特奥里克斯公司 | 用于抑制蛋白酶体的化合物 |
| EP1805208A2 (en) | 2004-10-20 | 2007-07-11 | Proteolix, Inc. | Labeled compounds for proteasome inhibition |
| PL2261236T3 (pl) | 2004-12-07 | 2015-12-31 | Onyx Therapeutics Inc | Kompozycja do hamowania proteasomu |
| US7468383B2 (en) | 2005-02-11 | 2008-12-23 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| EP1863513A2 (en) | 2005-03-11 | 2007-12-12 | The University of North Carolina at Chapel Hill | Potent and specific immunoproteasome inhibitors |
| 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 | |
| MY145757A (en) | 2005-11-09 | 2012-04-13 | Proteolix 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 (ja) | 2006-04-14 | 2007-11-01 | Eisai R & D Management Co., Ltd. | ベンズイミダゾール化合物 |
| 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 |
| SI2041158T1 (sl) | 2006-06-19 | 2013-09-30 | Onyx Therapeutics, Inc. | Peptidni epoksiketoni za inhibicijo proteasomov |
| WO2008033807A2 (en) | 2006-09-13 | 2008-03-20 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Synergistic combinations of antineoplastic thiol-binding mitochondrial oxidants and antineoplastic proteasome inhibitors for the treatment of cancer |
| US8601054B2 (en) * | 2006-12-07 | 2013-12-03 | International Business Machines Corporation | Project-related communications |
| EP2117556A2 (en) | 2007-01-23 | 2009-11-18 | Gloucester Pharmaceuticals, Inc. | Combination therapy comprising romidepsin and i.a. bortezomib |
| WO2008140782A2 (en) * | 2007-05-10 | 2008-11-20 | Proteolix, Inc. | Compounds for enzyme inhibition |
| US7442830B1 (en) | 2007-08-06 | 2008-10-28 | Millenium Pharmaceuticals, Inc. | Proteasome inhibitors |
| NZ582693A (en) | 2007-08-06 | 2012-01-12 | Millennium Pharm Inc | Boron-containing proteasome inhibitors |
| DK2207791T4 (da) | 2007-10-04 | 2019-10-07 | Onyx Therapeutics Inc | Krystallinske peptidepoxyketon-proteasehæmmere og syntese af aminosyreketoepoxider |
| EP2212334B1 (en) | 2007-10-16 | 2012-08-15 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
| US7838673B2 (en) | 2007-10-16 | 2010-11-23 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
| WO2009067453A1 (en) | 2007-11-19 | 2009-05-28 | Syndax Pharmaceuticals, Inc. | Combinations of hdac inhibitors and proteasome inhibitors |
| SG10201701524XA (en) | 2008-06-17 | 2017-04-27 | 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. |
| ES2617560T3 (es) | 2008-10-21 | 2017-06-19 | Onyx Therapeutics, Inc. | Combinación del inhibidor del proteasoma de epoxicetona peptídica carfilzomib con melfalán para su uso en el tratamiento del mieloma múltiple |
| 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 |
| JP5919196B2 (ja) | 2009-11-13 | 2016-05-18 | オニキス セラピューティクス， インク．Ｏｎｙｘ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． | 転移抑制のためのペプチドエポキシケトンの使用 |
| WO2011109355A1 (en) | 2010-03-01 | 2011-09-09 | Onyx Therapeutics, Inc. | Compounds for immunoproteasome inhibition |
| MX2012011298A (es) | 2010-03-31 | 2012-11-06 | Millennium Pharm Inc | Derivados del acido 1-amino-2-ciclopropiletilboronico. |
| CN102946729B (zh) | 2010-04-07 | 2014-11-05 | 欧尼斯治疗公司 | 结晶肽环氧酮免疫蛋白酶体抑制剂 |
-
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 SA114350283A patent/SA114350283B1/ar unknown
- 2010-03-20 SA SA110310221A patent/SA110310221B1/ar unknown
- 2010-03-22 EA EA201300860A patent/EA024672B1/ru not_active IP Right Cessation
- 2010-03-22 AU AU2010226410A patent/AU2010226410B2/en not_active Ceased
- 2010-03-22 SG SG2014011373A patent/SG2014011373A/en unknown
- 2010-03-22 SG SG2011067204A patent/SG174446A1/en unknown
- 2010-03-22 US US12/728,547 patent/US20100240903A1/en not_active Abandoned
- 2010-03-22 MX MX2013012107A patent/MX343562B/es unknown
- 2010-03-22 RS RS20161122A patent/RS55431B1/sr unknown
- 2010-03-22 MX MX2011009777A patent/MX2011009777A/es active IP Right Grant
- 2010-03-22 GE GEAP201012421A patent/GEP20156392B/en unknown
- 2010-03-22 DK DK10754225.0T patent/DK2408758T3/da active
- 2010-03-22 PT PT141787259T patent/PT2813241T/pt unknown
- 2010-03-22 EA EA201171151A patent/EA020973B1/ru not_active IP Right Cessation
- 2010-03-22 ME MEP-2011-164A patent/ME01277B/me unknown
- 2010-03-22 WO PCT/US2010/028126 patent/WO2010108172A1/en active Application Filing
- 2010-03-22 NZ NZ595847A patent/NZ595847A/en not_active IP Right Cessation
- 2010-03-22 US US13/257,887 patent/US8604215B2/en not_active Expired - Fee Related
- 2010-03-22 AP AP2013007137A patent/AP3513A/xx active
- 2010-03-22 DK DK14178725.9T patent/DK2813241T3/en active
- 2010-03-22 HU HUE14178725A patent/HUE032430T2/en unknown
- 2010-03-22 BR BRPI1009369A patent/BRPI1009369A2/pt not_active Application Discontinuation
- 2010-03-22 NZ NZ61843210A patent/NZ618432A/en not_active IP Right Cessation
- 2010-03-22 ES ES14178725.9T patent/ES2614557T3/es active Active
- 2010-03-22 MA MA34254A patent/MA33197B1/fr unknown
- 2010-03-22 CA CA2755971A patent/CA2755971C/en not_active Expired - Fee Related
- 2010-03-22 LT LTEP14178725.9T patent/LT2813241T/lt unknown
- 2010-03-22 SI SI201031354A patent/SI2813241T1/sl unknown
- 2010-03-22 ES ES10754225.0T patent/ES2527619T3/es active Active
- 2010-03-22 PT PT107542250T patent/PT2408758E/pt unknown
- 2010-03-22 CN CN201080021879.8A patent/CN102428075B/zh not_active Expired - Fee Related
- 2010-03-22 EP EP14178725.9A patent/EP2813241B1/en active Active
- 2010-03-22 SI SI201030833T patent/SI2408758T1/sl unknown
- 2010-03-22 MY MYPI2011004414A patent/MY156522A/en unknown
- 2010-03-22 JP JP2012501028A patent/JP5723357B2/ja active Active
- 2010-03-22 PE PE2011001673A patent/PE20120645A1/es active IP Right Grant
- 2010-03-22 EP EP10754225.0A patent/EP2408758B1/en active Active
- 2010-03-22 KR KR1020117022814A patent/KR101729344B1/ko active IP Right Grant
- 2010-03-22 PL PL14178725T patent/PL2813241T3/pl unknown
- 2010-03-22 RS RS20150015A patent/RS53746B1/en unknown
- 2010-03-22 PL PL10754225T patent/PL2408758T3/pl unknown
-
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 ZA ZA2011/06826A patent/ZA201106826B/en unknown
- 2011-09-19 CR CR20110491A patent/CR20110491A/es unknown
- 2011-09-19 TN TN2011000470A patent/TN2011000470A1/fr unknown
- 2011-09-20 CL CL2011002326A patent/CL2011002326A1/es unknown
- 2011-09-20 US US13/237,655 patent/US8822512B2/en not_active Expired - Fee Related
- 2011-09-20 EC EC2011011341A patent/ECSP11011341A/es unknown
- 2011-09-20 NI NI201100170A patent/NI201100170A/es unknown
- 2011-09-20 HN HN2011002459A patent/HN2011002459A/es unknown
- 2011-09-20 CU CU20110176A patent/CU20110176A7/es unknown
-
2012
- 2012-03-15 HK HK12102641.5A patent/HK1162476A1/xx not_active IP Right Cessation
-
2013
- 2013-09-24 US US14/035,644 patent/US9051353B2/en not_active Expired - Fee Related
-
2015
- 2015-01-08 HR HRP20150014AT patent/HRP20150014T1/hr unknown
- 2015-01-12 SM SM201500009T patent/SMT201500009B/xx unknown
- 2015-03-05 US US14/639,603 patent/US9403868B2/en not_active Expired - Fee Related
- 2015-06-16 HK HK15105658.5A patent/HK1204952A1/xx not_active IP Right Cessation
-
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
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR075899A1 (es) | Tripeptidos epoxicetonas cristalinos inhibidores de proteasa | |
| CO6270366A2 (es) | Inhibidores de epoxi cetona proteasa peptidicos cristalinos y lða sintesis de ceto-epoxidos aminoacidicos | |
| ECSP11011398A (es) | Inhibidores de beta-secretasa | |
| PE20141358A1 (es) | Polimorfos de inhibidores de cinasas | |
| UA108378C2 (uk) | Спосіб одержання плеуромутилінів | |
| CL2012001911A1 (es) | Compuestos derivados de fumarato; composicion farmaceutica que los comprende; y su uso en el tratamiento de una enfermedad inflamatoria o neurodegenerativa. | |
| NZ602872A (en) | Crystalline peptide epoxyketone immunoproteasome inhibitor | |
| CU24354B1 (es) | Procedimiento de obtención de derivados de tetrafluoropropilmorfolina | |
| CU20120137A7 (es) | Hidrato del hidrocloruro de agomelatina y preparación de éste | |
| ES2526902T3 (es) | Procesos de producción de inhibidores de la girasa y topoisomerasa IV | |
| CL2008003095A1 (es) | Procedeimiento de preparacion de dihidrotienopirimidas; uno de los compuestos intermediarios considerados; y el procedimiento de preparacion de dicho compuesto intermediario. | |
| CL2020001244A1 (es) | Inhibidores de inmunoproteasoma. | |
| BR112014019585A8 (pt) | Forma sólida de um composto, composição farmacêutica e cápsula em gel | |
| BR112017018580A2 (pt) | p-toluenossulfonato para inibidor de mek quinase, e forma cristalina do mesmo e método de preparação para tal | |
| CR20110251A (es) | Metodo para la obtencion de un extracto rico en taninos del acido elágico a partir de frutos que contiednen estos compuestos y extracto obtenido usando dicho metodo. | |
| ES2571043T3 (es) | Preparación de dihidropiridinas | |
| ME00929B (me) | NOVI POSTUPAK ZA DOBlJANJE KRISTALNOG OBLIKA V AGOMELATIN A | |
| AR086519A1 (es) | Procedimiento para producir hidrocloruro de epirubicina cristalino e hidrocloruro de epirubicina cristalino producido mediante este procedimiento | |
| BR112017005454A2 (pt) | composto de l-prolina do inibidor 2 do cotransportador de sódio-glicose, e mono-hidrato e cristal do composto de l-prolina | |
| EA201592167A1 (ru) | Способ получения производных пирролидин-2-карбоновой кислоты | |
| AR094240A1 (es) | Proceso para producir cristal de compuesto de pirazol | |
| AR084962A1 (es) | Derivados de flufenoxina utiles para tratar patologias tau o amiloide, tales como alzheimer y composiciones farmaceuticas que los contienen | |
| TH120312A (th) | สารยับยั้งโปรตีเอสชนิดไตรเปปไทด์อีพอกซีคีโตนที่เป็นผลึก | |
| TH120312B (th) | สารยับยั้งโปรตีเอสชนิดไตรเปปไทด์อีพอกซีคีโตนที่เป็นผลึก | |
| CU20100058A7 (es) | Inhibidores de proteasa de péptidos de epoxi cetona cristalinos y la síntesis de aminoácidos ceto-epóxidos |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |