JP6042724B2 - イムノプロテアソーム阻害のための化合物 - Google Patents
イムノプロテアソーム阻害のための化合物 Download PDFInfo
- Publication number
- JP6042724B2 JP6042724B2 JP2012556160A JP2012556160A JP6042724B2 JP 6042724 B2 JP6042724 B2 JP 6042724B2 JP 2012556160 A JP2012556160 A JP 2012556160A JP 2012556160 A JP2012556160 A JP 2012556160A JP 6042724 B2 JP6042724 B2 JP 6042724B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound according
- compound
- aralkyl
- hydrogen
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
-
- 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
- A61K31/40—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
-
- 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
- A61K31/535—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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Child & Adolescent Psychology (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (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 (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30936610P | 2010-03-01 | 2010-03-01 | |
| US61/309,366 | 2010-03-01 | ||
| PCT/US2011/026629 WO2011109355A1 (en) | 2010-03-01 | 2011-03-01 | Compounds for immunoproteasome inhibition |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013521295A JP2013521295A (ja) | 2013-06-10 |
| JP2013521295A5 JP2013521295A5 (https=) | 2014-04-17 |
| JP6042724B2 true JP6042724B2 (ja) | 2016-12-14 |
Family
ID=43983939
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012556160A Active JP6042724B2 (ja) | 2010-03-01 | 2011-03-01 | イムノプロテアソーム阻害のための化合物 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US9359398B2 (https=) |
| EP (1) | EP2542238B1 (https=) |
| JP (1) | JP6042724B2 (https=) |
| KR (1) | KR20130075723A (https=) |
| CN (1) | CN102892417A (https=) |
| AU (1) | AU2011223795B2 (https=) |
| BR (1) | BR112012022060A2 (https=) |
| CA (1) | CA2791651C (https=) |
| CL (1) | CL2012002404A1 (https=) |
| CO (1) | CO6612265A2 (https=) |
| CR (1) | CR20120451A (https=) |
| CU (1) | CU20120125A7 (https=) |
| DO (1) | DOP2012000238A (https=) |
| EA (1) | EA201290844A1 (https=) |
| EC (1) | ECSP12012140A (https=) |
| MA (1) | MA34133B1 (https=) |
| MX (1) | MX2012010017A (https=) |
| PH (1) | PH12012501719A1 (https=) |
| SG (1) | SG183843A1 (https=) |
| WO (1) | WO2011109355A1 (https=) |
| ZA (1) | ZA201206479B (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY171061A (en) * | 2005-11-09 | 2019-09-24 | Onyx Therapeutics Inc | Compounds for enzyme inhibition |
| CA2657213C (en) | 2006-06-19 | 2017-01-03 | Proteolix, Inc. | Peptide epoxyketones for proteasome inhibition |
| KR20170125413A (ko) | 2007-10-04 | 2017-11-14 | 오닉스 세라퓨틱스, 인크. | 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성 |
| EP3090737A1 (en) | 2008-10-21 | 2016-11-09 | Onyx Therapeutics, Inc. | Combination therapy with peptide epoxyketones |
| 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 |
| US8853147B2 (en) | 2009-11-13 | 2014-10-07 | Onyx Therapeutics, Inc. | Use of peptide epoxyketones for metastasis suppression |
| EP2542238B1 (en) | 2010-03-01 | 2015-08-12 | Onyx Therapeutics, Inc. | Compounds for immunoproteasome inhibition |
| NZ602872A (en) | 2010-04-07 | 2014-05-30 | Onyx Therapeutics Inc | Crystalline peptide epoxyketone immunoproteasome inhibitor |
| US20140105921A1 (en) | 2012-07-09 | 2014-04-17 | Onyx Therapeutics, Inc. | Prodrugs of Peptide Epoxy Ketone Protease Inhibitors |
| MX2015006715A (es) * | 2012-12-03 | 2015-08-14 | Hoffmann La Roche | Compuestos de acido triazolboronico sustituido. |
| EA030957B1 (ru) * | 2013-03-14 | 2018-10-31 | Оникс Терапьютикс, Инк. | Дипептидные и трипептидные эпоксикетонные ингибиторы протеазы |
| EP2961765A4 (en) * | 2013-03-15 | 2016-11-09 | Adaerata Ltd Partnership | SMALL MOLECULAR PCSK9 MODULATORS AND METHOD OF USE THEREOF |
| EP3092244B1 (en) | 2014-01-10 | 2019-08-14 | Cornell University | Dipeptides as inhibitors of human immunoproteasomes |
| 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 |
| EP3201208B1 (en) * | 2014-10-01 | 2021-03-24 | Merck Patent GmbH | Boronic acid derivatives |
| WO2017066763A1 (en) | 2015-10-15 | 2017-04-20 | Cornell University | Proteasome inhibitors and uses thereof |
| 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 |
| US10526315B2 (en) | 2016-06-21 | 2020-01-07 | Orion Ophthalmology LLC | Carbocyclic prolinamide derivatives |
| PL3472149T3 (pl) | 2016-06-21 | 2024-02-12 | Orion Ophthalmology LLC | Heterocykliczne pochodne prolinamidu |
| US11203613B2 (en) | 2017-10-11 | 2021-12-21 | Cornell University | Peptidomimetic proteasome inhibitors |
| AU2018370019C1 (en) * | 2017-11-16 | 2025-01-30 | Amgen Inc. | Stable compositions of pegylated carfilzomib compounds |
| EP3710458B1 (en) * | 2017-11-16 | 2026-03-25 | Principia Biopharma Inc. | Immunoproteasome inhibitors |
| 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 (https=) | 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 |
| 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 |
| 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 |
| SI0932617T1 (en) | 1996-10-18 | 2002-06-30 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
| KR100509388B1 (ko) | 1996-10-18 | 2005-08-23 | 버텍스 파마슈티칼스 인코포레이티드 | 세린 프로테아제, 특히 간염 ｃ 바이러스 ｎｓ３ 프로테아제의 저해제 |
| 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 |
| 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 |
| KR20010080267A (ko) | 1998-10-20 | 2001-08-22 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 프로테아솜 억제제 약물 작용을 모니터링하는 방법 |
| 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 |
| BR0209883A (pt) | 2001-05-21 | 2004-06-08 | Alcon Inc | Uso de inibidores da proteasoma para o tratamento de distúrbios do olho seco |
| WO2002096933A1 (en) * | 2001-05-30 | 2002-12-05 | Novartis Ag | 2-{[n-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl]-amino}-alkylboronic acid derivatives |
| 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 |
| CA2481306A1 (en) | 2002-04-09 | 2003-10-23 | 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 |
| WO2003101481A1 (en) | 2002-06-03 | 2003-12-11 | 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 |
| PE20130200A1 (es) | 2003-04-08 | 2013-03-09 | Novartis Ag | Composicion farmaceutica que contiene un agonista del receptor s1p y un alcohol de azucar |
| ATE506456T1 (de) | 2003-06-10 | 2011-05-15 | David Gladstone Inst | Verfahren zur behandlung von lentivirusinfektionen |
| US7012063B2 (en) | 2003-06-13 | 2006-03-14 | Children's Medical Center Corporation | Reducing axon degeneration with proteasome inhibitors |
| AU2004311478A1 (en) | 2003-12-31 | 2005-07-21 | Cydex Pharmaceuticals, Inc. | Inhalant formulation containing sulfoalkyl ether cyclodextrin and corticosteroid |
| GB0400804D0 (en) | 2004-01-14 | 2004-02-18 | Innoscience Technology Bv | Pharmaceutical compositions |
| 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 |
| AU2005243140A1 (en) | 2004-05-10 | 2005-11-24 | Proteolix, Inc. | Synthesis of amino acid keto-epoxides |
| EP2030981B1 (en) | 2004-05-10 | 2014-07-09 | Onyx Therapeutics, Inc. | Compounds for proteasome enzyme inhibition |
| US20060088471A1 (en) | 2004-10-20 | 2006-04-27 | Proteolix, Inc. | Compounds for enzyme inhibition |
| PT2260835E (pt) | 2004-12-07 | 2013-05-28 | Onyx Therapeutics Inc | Composição para inibição do proteassoma |
| 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 |
| WO2006113470A2 (en) | 2005-04-15 | 2006-10-26 | Geron Corporation | Cancer treatment by combined inhibition of proteasome and telomerase activities |
| GT200600350A (es) | 2005-08-09 | 2007-03-28 | Formulaciones líquidas | |
| MY171061A (en) | 2005-11-09 | 2019-09-24 | 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 (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 |
| CA2657213C (en) | 2006-06-19 | 2017-01-03 | Proteolix, Inc. | Peptide epoxyketones for proteasome inhibition |
| 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 |
| JP2010516767A (ja) | 2007-01-23 | 2010-05-20 | グラスター ファーマシューティカルズ， インコーポレイテッド | ロミデプシンおよびｉ．ａ．ボルテゾミブを含む併用療法 |
| 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 |
| PL2178888T3 (pl) | 2007-08-06 | 2012-11-30 | Millennium Pharm Inc | Inhibitory proteasomów |
| KR20170125413A (ko) | 2007-10-04 | 2017-11-14 | 오닉스 세라퓨틱스, 인크. | 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성 |
| US7838673B2 (en) | 2007-10-16 | 2010-11-23 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
| WO2009051581A1 (en) | 2007-10-16 | 2009-04-23 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
| US20090131367A1 (en) | 2007-11-19 | 2009-05-21 | The Regents Of The University Of Colorado | Combinations of HDAC Inhibitors and Proteasome Inhibitors |
| EP2730579A1 (en) | 2008-06-17 | 2014-05-14 | 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. |
| EP3090737A1 (en) | 2008-10-21 | 2016-11-09 | Onyx Therapeutics, Inc. | Combination therapy with peptide epoxyketones |
| 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 |
| US8853147B2 (en) | 2009-11-13 | 2014-10-07 | Onyx Therapeutics, Inc. | Use of peptide epoxyketones for metastasis suppression |
| EP2542238B1 (en) | 2010-03-01 | 2015-08-12 | 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. |
| NZ602872A (en) | 2010-04-07 | 2014-05-30 | Onyx Therapeutics Inc | Crystalline peptide epoxyketone immunoproteasome inhibitor |
| FR2962092B1 (fr) * | 2010-06-30 | 2013-06-28 | Valeo Systemes Dessuyage | Adaptateur d'essuie-glace a contacts electriques |
-
2011
- 2011-03-01 EP EP11715320.5A patent/EP2542238B1/en active Active
- 2011-03-01 KR KR1020127025901A patent/KR20130075723A/ko not_active Withdrawn
- 2011-03-01 BR BR112012022060A patent/BR112012022060A2/pt not_active IP Right Cessation
- 2011-03-01 AU AU2011223795A patent/AU2011223795B2/en active Active
- 2011-03-01 MA MA35248A patent/MA34133B1/fr unknown
- 2011-03-01 SG SG2012064531A patent/SG183843A1/en unknown
- 2011-03-01 MX MX2012010017A patent/MX2012010017A/es active IP Right Grant
- 2011-03-01 WO PCT/US2011/026629 patent/WO2011109355A1/en not_active Ceased
- 2011-03-01 CN CN201180022010XA patent/CN102892417A/zh active Pending
- 2011-03-01 PH PH1/2012/501719A patent/PH12012501719A1/en unknown
- 2011-03-01 EA EA201290844A patent/EA201290844A1/ru unknown
- 2011-03-01 JP JP2012556160A patent/JP6042724B2/ja active Active
- 2011-03-01 CA CA2791651A patent/CA2791651C/en active Active
- 2011-03-01 US US13/580,112 patent/US9359398B2/en active Active
-
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 |
|---|---|
| CA2791651A1 (en) | 2011-09-09 |
| CA2791651C (en) | 2019-08-20 |
| KR20130075723A (ko) | 2013-07-05 |
| JP2013521295A (ja) | 2013-06-10 |
| WO2011109355A1 (en) | 2011-09-09 |
| PH12012501719A1 (en) | 2012-11-12 |
| CO6612265A2 (es) | 2013-02-01 |
| EP2542238B1 (en) | 2015-08-12 |
| SG183843A1 (en) | 2012-10-30 |
| AU2011223795A1 (en) | 2012-09-20 |
| MX2012010017A (es) | 2012-10-01 |
| CU20120125A7 (es) | 2012-11-15 |
| ECSP12012140A (es) | 2012-10-30 |
| US20130072422A1 (en) | 2013-03-21 |
| CL2012002404A1 (es) | 2012-12-21 |
| MA34133B1 (fr) | 2013-04-03 |
| AU2011223795B2 (en) | 2015-11-05 |
| EA201290844A1 (ru) | 2013-03-29 |
| DOP2012000238A (es) | 2013-01-15 |
| US9359398B2 (en) | 2016-06-07 |
| CN102892417A (zh) | 2013-01-23 |
| EP2542238A1 (en) | 2013-01-09 |
| ZA201206479B (en) | 2015-08-26 |
| BR112012022060A2 (pt) | 2018-05-08 |
| CR20120451A (es) | 2012-10-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6042724B2 (ja) | イムノプロテアソーム阻害のための化合物 | |
| JP5226679B2 (ja) | 酵素阻害のための化合物 | |
| CN101405294B (zh) | 用于酶抑制的化合物 | |
| CN102946729B (zh) | 结晶肽环氧酮免疫蛋白酶体抑制剂 | |
| ES2510840T3 (es) | Compuestos para la inhibición enzimática del proteosoma | |
| IL181127A (en) | Compounds for proteasome enzyme inhibition | |
| KR20070086924A (ko) | 프로테아좀 저해를 위한 조성물 | |
| ES2359004T3 (es) | Compuestos para inhibición enzimática de proteasoma. | |
| US20060193844A1 (en) | Methods for enzyme inhibition | |
| AU2013203467A1 (en) | Compounds for immunoproteasome inhibition | |
| AU2013203525A1 (en) | Crystalline peptide epoxyketone immunoproteasome inhibitor |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20140226 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20140226 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20150313 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20150407 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20150702 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20150731 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20151007 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20160405 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20160705 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20160905 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20161018 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20161110 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6042724 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |