PH12012501719A1 - Compounds for immunoproteasome inhibition - Google Patents
Compounds for immunoproteasome inhibitionInfo
- Publication number
- PH12012501719A1 PH12012501719A1 PH1/2012/501719A PH12012501719A PH12012501719A1 PH 12012501719 A1 PH12012501719 A1 PH 12012501719A1 PH 12012501719 A PH12012501719 A PH 12012501719A PH 12012501719 A1 PH12012501719 A1 PH 12012501719A1
- Authority
- PH
- Philippines
- Prior art keywords
- compounds
- relates
- immunoproteasome
- administering
- compound
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 230000005764 inhibitory process Effects 0.000 title 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000004245 Proteasome Endopeptidase Complex Human genes 0.000 abstract 1
- 108090000708 Proteasome Endopeptidase Complex Proteins 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—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
- A61P35/00—Antineoplastic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D209/20—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
- C07D295/104—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
- C07D303/02—Compounds containing oxirane rings
- C07D303/36—Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/04—Esters of boric acids
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30936610P | 2010-03-01 | 2010-03-01 | |
| PCT/US2011/026629 WO2011109355A1 (en) | 2010-03-01 | 2011-03-01 | Compounds for immunoproteasome inhibition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PH12012501719A1 true PH12012501719A1 (en) | 2012-11-12 |
Family
ID=43983939
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PH1/2012/501719A PH12012501719A1 (en) | 2010-03-01 | 2011-03-01 | Compounds for immunoproteasome inhibition |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US9359398B2 (enExample) |
| EP (1) | EP2542238B1 (enExample) |
| JP (1) | JP6042724B2 (enExample) |
| KR (1) | KR20130075723A (enExample) |
| CN (1) | CN102892417A (enExample) |
| AU (1) | AU2011223795B2 (enExample) |
| BR (1) | BR112012022060A2 (enExample) |
| CA (1) | CA2791651C (enExample) |
| CL (1) | CL2012002404A1 (enExample) |
| CO (1) | CO6612265A2 (enExample) |
| CR (1) | CR20120451A (enExample) |
| CU (1) | CU20120125A7 (enExample) |
| DO (1) | DOP2012000238A (enExample) |
| EA (1) | EA201290844A1 (enExample) |
| EC (1) | ECSP12012140A (enExample) |
| MA (1) | MA34133B1 (enExample) |
| MX (1) | MX2012010017A (enExample) |
| PH (1) | PH12012501719A1 (enExample) |
| SG (1) | SG183843A1 (enExample) |
| WO (1) | WO2011109355A1 (enExample) |
| ZA (1) | ZA201206479B (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101434522B1 (ko) | 2005-11-09 | 2014-08-26 | 오닉스 세라퓨틱스, 인크. | 효소 저해를 위한 화합물 |
| RU2450016C2 (ru) | 2006-06-19 | 2012-05-10 | Протеоликс, Инк. | Пептидные эпоксикетоны для ингибирования протеасомы |
| SI2207791T2 (sl) | 2007-10-04 | 2019-09-30 | Onyx Therapeutics, Inc. | Kristalinični peptidepoksiketonski proteazni inhibitorji in sinteza aminokislinskih ketoepoksidov |
| EP2796134B1 (en) | 2008-10-21 | 2016-12-07 | Onyx Therapeutics, Inc. | Combination of the peptide epoxyketone proteasome inhibitor carfilzomib with melphalan for use in the treatment of multiple myeloma |
| AR075899A1 (es) | 2009-03-20 | 2011-05-04 | Onyx Therapeutics Inc | Tripeptidos epoxicetonas cristalinos inhibidores de proteasa |
| EP2498793B1 (en) | 2009-11-13 | 2019-07-10 | Onyx Therapeutics, Inc. | Oprozomib for use in metastasis suppression |
| AU2011223795B2 (en) * | 2010-03-01 | 2015-11-05 | Onyx Therapeutics, Inc. | Compounds for immunoproteasome inhibition |
| KR20130094185A (ko) | 2010-04-07 | 2013-08-23 | 오닉스 세라퓨틱스, 인크. | 결정성 펩티드 에폭시케톤 면역프로테아좀 저해제 |
| US20140105921A1 (en) | 2012-07-09 | 2014-04-17 | Onyx Therapeutics, Inc. | Prodrugs of Peptide Epoxy Ketone Protease Inhibitors |
| CN104822689B (zh) * | 2012-12-03 | 2016-11-02 | 弗·哈夫曼-拉罗切有限公司 | 取代的三唑硼酸化合物 |
| EP2970225B1 (en) * | 2013-03-14 | 2018-08-15 | Onyx Therapeutics, Inc. | Dipeptide and tripeptide epoxy ketone protease inhibitors |
| EP2961765A4 (en) * | 2013-03-15 | 2016-11-09 | Adaerata Ltd Partnership | SMALL MOLECULAR PCSK9 MODULATORS AND METHOD OF USE THEREOF |
| ES2748434T3 (es) | 2014-01-10 | 2020-03-16 | Univ Cornell | Dipéptidos como inhibidores de inmunoproteasomas humanos |
| CN103804469B (zh) * | 2014-02-17 | 2016-04-06 | 苏州明锐医药科技有限公司 | 卡非佐米中间体的制备方法 |
| CN107073069B (zh) | 2014-08-18 | 2022-03-08 | 康奈尔大学 | 作为人免疫蛋白酶体的抑制剂的二肽模拟物 |
| BR112017006349A2 (pt) * | 2014-10-01 | 2017-12-12 | Merck Patent Gmbh | derivados de ácido borônico |
| CN106588965A (zh) * | 2015-10-15 | 2017-04-26 | 北京大学 | 脲拟肽硼酸化合物及其药物组合物、制备方法和用途 |
| CN114306297A (zh) | 2015-10-15 | 2022-04-12 | 康奈尔大学 | 蛋白酶体抑制剂及其用途 |
| WO2017222914A1 (en) | 2016-06-21 | 2017-12-28 | Inception 4, Inc. | Carbocyclic prolinamide derivatives |
| EP3472149B1 (en) | 2016-06-21 | 2023-08-30 | Orion Ophthalmology LLC | Heterocyclic prolinamide derivatives |
| WO2019075252A1 (en) | 2017-10-11 | 2019-04-18 | Cornell University | PEPTIDOMIMETIC INHIBITORS OF PROTEASOME |
| AU2018367515B2 (en) * | 2017-11-16 | 2023-04-27 | Principia Biopharma Inc. | Immunoproteasome inhibitors |
| CN120884714A (zh) * | 2017-11-16 | 2025-11-04 | 美国安进公司 | 聚乙二醇化卡非佐米化合物的稳定的组合物 |
| LV15544A (lv) * | 2019-07-01 | 2021-01-20 | Latvijas Organiskās Sintēzes Institūts | Jauni borskābi saturoši peptidomimētiķi kā malārijas serīna proteāzes inhibitori |
Family Cites Families (91)
| 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 |
| DE3827340A1 (de) * | 1988-08-12 | 1990-02-15 | Hoechst Ag | Verwendung von (alpha)-aminoboronsaeure-derivaten zur prophylaxe und behandlung von viruserkrankungen |
| JPH0291023U (enExample) | 1989-01-05 | 1990-07-19 | ||
| 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 |
| US5071957A (en) | 1989-08-04 | 1991-12-10 | Bristol-Myers Company | Antibiotic BU-4061T |
| US4990448A (en) | 1989-08-04 | 1991-02-05 | Bristol-Myers Company | 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 |
| JPH05506777A (ja) | 1990-03-05 | 1993-10-07 | セファロン、インコーポレーテッド | キモトリプシン様プロテアーゼ及びそれらの阻害剤 |
| 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 |
| 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 |
| EP1136498A1 (en) | 1996-10-18 | 2001-09-26 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hepatitis c virus NS3 protease |
| DE69709671T2 (de) | 1996-10-18 | 2002-08-22 | Vertex Pharmaceuticals Inc., Cambridge | Inhibitoren von serinproteasen, insbesondere von ns3-protease des hepatitis-c-virus |
| 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 |
| 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 |
| 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 |
| BR9914648A (pt) | 1998-10-20 | 2001-11-27 | Millennium Pharm Inc | Processo para monitorar ação medicamentosa deinibidor de proteasoma |
| 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 |
| CA2385958A1 (en) | 1999-10-20 | 2001-04-26 | Osteoscreen, Inc. | Inhibitors of proteasomal activity for stimulating bone and hair growth |
| ES2272558T3 (es) | 2000-10-12 | 2007-05-01 | Viromics Gmbh | Inhibidores del proteasoma para el tratamiento de infecciones causadas por virus de la hepatitis. |
| ES2571219T3 (es) | 2001-01-25 | 2024-09-23 | The United States Of America Represented By The Sec Dep Of Health And Human Services | Formulación de compuestos de ácido borónico |
| EP1392355B1 (en) | 2001-05-21 | 2007-02-14 | Alcon, Inc. | Use of proteasome inhibitors to treat dry eye disorders |
| JP4416501B2 (ja) * | 2001-05-30 | 2010-02-17 | ノバルティス アクチエンゲゼルシャフト | ２−｛［ｎ−（２−アミノ−３−（ヘテロアリールまたはアリール）プロピオニル）−アミノアシル］−アミノ｝−アルキルボロン酸誘導体 |
| EP1463719A2 (en) | 2002-01-08 | 2004-10-06 | 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 |
| EP1496916A2 (en) | 2002-04-09 | 2005-01-19 | 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 |
| AU2003256847A1 (en) | 2002-07-26 | 2004-02-16 | Advanced Research And 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 |
| EP2008650A3 (en) | 2003-04-08 | 2011-04-27 | Novartis AG | Solid oral composition comprising a S 1 P receptor agonist and a sugar alcohol |
| US8338180B2 (en) | 2003-06-10 | 2012-12-25 | 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 |
| RU2390330C2 (ru) | 2003-12-31 | 2010-05-27 | Сайдекс, Инк. | Ингаляционная препаративная форма, содержащая простой сульфоалкиловый эфир гамма-циклодекстрина и кортикостероид |
| GB0400804D0 (en) | 2004-01-14 | 2004-02-18 | Innoscience Technology Bv | Pharmaceutical compositions |
| 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 |
| US8129346B2 (en) | 2004-04-15 | 2012-03-06 | Onyx Therapeutics, Inc. | Compounds for enzyme inhibition |
| PT2030981E (pt) | 2004-05-10 | 2014-10-14 | Onyx Therapeutics Inc | Compostos para inibição da enzima proteassoma |
| AU2005243140A1 (en) | 2004-05-10 | 2005-11-24 | Proteolix, Inc. | Synthesis of amino acid keto-epoxides |
| CA2584515A1 (en) | 2004-10-20 | 2006-04-27 | Proteolix, Inc. | Labeled compounds for proteasome inhibition |
| CN102847136A (zh) | 2004-12-07 | 2013-01-02 | 普罗特奥里克斯公司 | 抑制蛋白酶体的组合物 |
| US7468383B2 (en) * | 2005-02-11 | 2008-12-23 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| US7589066B2 (en) * | 2005-03-11 | 2009-09-15 | The University Of North Carolina At Chapel Hill | Potent and specific immunoproteasome inhibitors |
| EP1876893B1 (en) | 2005-04-15 | 2012-04-11 | Geron Corporation | Cancer treatment by combined inhibition of proteasome and telomerase activities |
| GT200600350A (es) | 2005-08-09 | 2007-03-28 | Formulaciones líquidas | |
| KR101434522B1 (ko) | 2005-11-09 | 2014-08-26 | 오닉스 세라퓨틱스, 인크. | 효소 저해를 위한 화합물 |
| 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 |
| RU2450016C2 (ru) | 2006-06-19 | 2012-05-10 | Протеоликс, Инк. | Пептидные эпоксикетоны для ингибирования протеасомы |
| 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 |
| US20090105200A1 (en) | 2007-01-23 | 2009-04-23 | Mitchell Keegan | Combination therapy |
| 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 |
| KR20150010802A (ko) | 2007-08-06 | 2015-01-28 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 프로테아좀 억제제 |
| SI2207791T2 (sl) | 2007-10-04 | 2019-09-30 | Onyx Therapeutics, Inc. | Kristalinični peptidepoksiketonski proteazni inhibitorji in sinteza aminokislinskih ketoepoksidov |
| 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 (en) | 2007-11-19 | 2009-05-28 | Syndax Pharmaceuticals, Inc. | Combinations of hdac inhibitors and proteasome inhibitors |
| US20090325903A1 (en) | 2008-06-17 | 2009-12-31 | Millennium Pharmaceuticals, 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. |
| EP2796134B1 (en) | 2008-10-21 | 2016-12-07 | Onyx Therapeutics, Inc. | Combination of the peptide epoxyketone proteasome inhibitor carfilzomib with melphalan for use in the treatment of multiple myeloma |
| AR075899A1 (es) | 2009-03-20 | 2011-05-04 | Onyx Therapeutics Inc | Tripeptidos epoxicetonas cristalinos inhibidores de proteasa |
| 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 |
| EP2498793B1 (en) | 2009-11-13 | 2019-07-10 | Onyx Therapeutics, Inc. | Oprozomib for use in metastasis suppression |
| AU2011223795B2 (en) * | 2010-03-01 | 2015-11-05 | Onyx Therapeutics, Inc. | Compounds for immunoproteasome inhibition |
| US8513218B2 (en) | 2010-03-31 | 2013-08-20 | Millennium Pharmaceuticals, Inc. | Derivatives of 1-amino-2-cyclopropylethylboronic acid |
| KR20130094185A (ko) | 2010-04-07 | 2013-08-23 | 오닉스 세라퓨틱스, 인크. | 결정성 펩티드 에폭시케톤 면역프로테아좀 저해제 |
| FR2962092B1 (fr) * | 2010-06-30 | 2013-06-28 | Valeo Systemes Dessuyage | Adaptateur d'essuie-glace a contacts electriques |
-
2011
- 2011-03-01 AU AU2011223795A patent/AU2011223795B2/en active Active
- 2011-03-01 PH PH1/2012/501719A patent/PH12012501719A1/en unknown
- 2011-03-01 BR BR112012022060A patent/BR112012022060A2/pt not_active IP Right Cessation
- 2011-03-01 CN CN201180022010XA patent/CN102892417A/zh active Pending
- 2011-03-01 MX MX2012010017A patent/MX2012010017A/es active IP Right Grant
- 2011-03-01 EA EA201290844A patent/EA201290844A1/ru unknown
- 2011-03-01 US US13/580,112 patent/US9359398B2/en active Active
- 2011-03-01 CA CA2791651A patent/CA2791651C/en active Active
- 2011-03-01 MA MA35248A patent/MA34133B1/fr unknown
- 2011-03-01 EP EP11715320.5A patent/EP2542238B1/en active Active
- 2011-03-01 JP JP2012556160A patent/JP6042724B2/ja active Active
- 2011-03-01 WO PCT/US2011/026629 patent/WO2011109355A1/en not_active Ceased
- 2011-03-01 SG SG2012064531A patent/SG183843A1/en unknown
- 2011-03-01 KR KR1020127025901A patent/KR20130075723A/ko not_active Withdrawn
-
2012
- 2012-08-28 ZA ZA2012/06479A patent/ZA201206479B/en unknown
- 2012-08-29 DO DO2012000238A patent/DOP2012000238A/es unknown
- 2012-08-30 CU CU2012000125A patent/CU20120125A7/es unknown
- 2012-08-30 CR CR20120451A patent/CR20120451A/es unknown
- 2012-08-31 CL CL2012002404A patent/CL2012002404A1/es unknown
- 2012-09-04 EC ECSP12012140 patent/ECSP12012140A/es unknown
- 2012-09-28 CO CO12170402A patent/CO6612265A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CA2791651C (en) | 2019-08-20 |
| BR112012022060A2 (pt) | 2018-05-08 |
| CN102892417A (zh) | 2013-01-23 |
| CO6612265A2 (es) | 2013-02-01 |
| EP2542238A1 (en) | 2013-01-09 |
| EA201290844A1 (ru) | 2013-03-29 |
| US20130072422A1 (en) | 2013-03-21 |
| KR20130075723A (ko) | 2013-07-05 |
| JP6042724B2 (ja) | 2016-12-14 |
| ZA201206479B (en) | 2015-08-26 |
| CR20120451A (es) | 2012-10-16 |
| CL2012002404A1 (es) | 2012-12-21 |
| CA2791651A1 (en) | 2011-09-09 |
| MX2012010017A (es) | 2012-10-01 |
| SG183843A1 (en) | 2012-10-30 |
| MA34133B1 (fr) | 2013-04-03 |
| WO2011109355A1 (en) | 2011-09-09 |
| US9359398B2 (en) | 2016-06-07 |
| ECSP12012140A (es) | 2012-10-30 |
| JP2013521295A (ja) | 2013-06-10 |
| AU2011223795B2 (en) | 2015-11-05 |
| CU20120125A7 (es) | 2012-11-15 |
| AU2011223795A1 (en) | 2012-09-20 |
| EP2542238B1 (en) | 2015-08-12 |
| DOP2012000238A (es) | 2013-01-15 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PH12012501719A1 (en) | Compounds for immunoproteasome inhibition | |
| MY147832A (en) | Compounds for enzyme inhibition | |
| IN2014CN02887A (enExample) | ||
| EA201300860A1 (ru) | Кристаллические трипептидные ингибиторы эпоксикетон-протеазы | |
| PH12013501871A1 (en) | Cyclopropylamines as lsd1 inhibitors | |
| PH12013500543A1 (en) | Breast cancer therapeutics | |
| MD4659B1 (ro) | Polimorf al inhibitorilor SYK | |
| PH12014500215B1 (en) | Notch pathway signaling inhibitor compound | |
| ZA201406124B (en) | Inhibition of glycine cleavage system for treatment of cancer | |
| IL221404A (en) | Inhibits thiogenethone-based autophagy based on cancer therapy | |
| PH12015500867A1 (en) | Treatment of prostate cancer with tor kinase inhibitors | |
| MX343968B (es) | Inhibidor de proteasoma delanzomib para uso en el tratamiento de lupus. | |
| GB201012845D0 (en) | Inhibition of dicer function for treatment of cancer | |
| WO2012037553A9 (en) | Use of pkc-iota inhibitors for the treatment of breast cancer | |
| IL231448A0 (en) | Phosphatidylinositol 3-kinase inhibitors for cancer treatment | |
| UA110609C2 (uk) | Сполуки для інгібування ферменту протеасоми | |
| TN2013000515A1 (en) | Notch pathway signaling inhibitor compound | |
| EA201491695A1 (ru) | Лечение рака ингибиторами tor-киназы |