ZA201206479B - Compounds for immunoproteasome inhibition - Google Patents
Compounds for immunoproteasome inhibitionInfo
- Publication number
- ZA201206479B ZA201206479B ZA2012/06479A ZA201206479A ZA201206479B ZA 201206479 B ZA201206479 B ZA 201206479B ZA 2012/06479 A ZA2012/06479 A ZA 2012/06479A ZA 201206479 A ZA201206479 A ZA 201206479A ZA 201206479 B ZA201206479 B ZA 201206479B
- Authority
- ZA
- South Africa
- Prior art keywords
- compounds
- immunoproteasome
- inhibition
- immunoproteasome inhibition
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
-
- 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
-
- 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)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (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)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (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 |
|---|---|
| ZA201206479B true ZA201206479B (en) | 2015-08-26 |
Family
ID=43983939
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA2012/06479A ZA201206479B (en) | 2010-03-01 | 2012-08-28 | 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) |
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| US7687456B2 (en) | 2005-11-09 | 2010-03-30 | Proteolix, Inc. | Compounds for enzyme inhibition |
| EP2484688B1 (en) | 2006-06-19 | 2016-06-08 | Onyx Therapeutics, Inc. | Peptide epoxyketones for proteasome inhibition |
| MX2010003732A (es) | 2007-10-04 | 2010-08-09 | Onyx Therapeutics Inc | Inhibidores de peptido cetona epoxi de proteasa cristalina y la sintesis de ceto-epoxidos de aminoacido. |
| PE20120059A1 (es) * | 2008-10-21 | 2012-02-27 | Onyx Therapeutics Inc | Combinaciones farmaceuticas con epoxicetonas peptidicas |
| 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 |
| US9359398B2 (en) * | 2010-03-01 | 2016-06-07 | Onyx Therapeutics, Inc. | Compounds for immunoproteasome inhibition |
| WO2011136905A2 (en) | 2010-04-07 | 2011-11-03 | Onyx Therapeutics, Inc. | Crystalline peptide epoxyketone immunoproteasome inhibitor |
| US9309283B2 (en) | 2012-07-09 | 2016-04-12 | Onyx Therapeutics, Inc. | Prodrugs of peptide epoxy ketone protease inhibitors |
| JP6018319B2 (ja) * | 2012-12-03 | 2016-11-02 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 置換トリアゾールボロン酸化合物 |
| SG11201507106PA (en) * | 2013-03-14 | 2015-10-29 | Onyx Therapeutics Inc | Dipeptide and tripeptide epoxy ketone protease inhibitors |
| BR112015023761A2 (pt) * | 2013-03-15 | 2017-07-18 | Adaerata Lp | moduladores de molécula pequena de pcsk9 e seus métodos e usos |
| 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 |
| EP3193904B1 (en) | 2014-08-18 | 2025-10-01 | Cornell University | Dipeptidomimetics as inhibitors of human immunoproteasomes |
| CA2963198A1 (en) * | 2014-10-01 | 2016-04-07 | Merck Patent Gmbh | Boronic acid derivatives |
| 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 |
| JP6970085B2 (ja) | 2015-10-15 | 2021-11-24 | コーネル・ユニバーシティーCornell University | プロテアソーム阻害剤およびその用途 |
| MX392422B (es) | 2016-06-21 | 2025-03-24 | Orion Ophthalmology LLC | Derivados de prolinamida heterociclica |
| JP7164521B2 (ja) | 2016-06-21 | 2022-11-01 | オリオン・オフサルモロジー・エルエルシー | 炭素環式プロリンアミド誘導体 |
| US11203613B2 (en) | 2017-10-11 | 2021-12-21 | Cornell University | Peptidomimetic proteasome 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 |
| EA202090900A1 (ru) * | 2017-11-16 | 2020-10-02 | Принсипиа Биофарма Инк. | Ингибиторы иммунопротеасом |
| LV15544A (lv) * | 2019-07-01 | 2021-01-20 | Latvijas Organiskās Sintēzes Institūts | Jauni borskābi saturoši peptidomimētiķi kā malārijas serīna proteāzes inhibitori |
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-
2011
- 2011-03-01 US US13/580,112 patent/US9359398B2/en active Active
- 2011-03-01 KR KR1020127025901A patent/KR20130075723A/ko not_active Withdrawn
- 2011-03-01 MX MX2012010017A patent/MX2012010017A/es active IP Right Grant
- 2011-03-01 AU AU2011223795A patent/AU2011223795B2/en active Active
- 2011-03-01 PH PH1/2012/501719A patent/PH12012501719A1/en unknown
- 2011-03-01 EP EP11715320.5A patent/EP2542238B1/en active Active
- 2011-03-01 SG SG2012064531A patent/SG183843A1/en unknown
- 2011-03-01 WO PCT/US2011/026629 patent/WO2011109355A1/en not_active Ceased
- 2011-03-01 JP JP2012556160A patent/JP6042724B2/ja active Active
- 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 MA MA35248A patent/MA34133B1/fr unknown
- 2011-03-01 EA EA201290844A patent/EA201290844A1/ru unknown
- 2011-03-01 CA CA2791651A patent/CA2791651C/en active Active
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2012
- 2012-08-28 ZA ZA2012/06479A patent/ZA201206479B/en unknown
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- 2012-08-30 CU CU2012000125A patent/CU20120125A7/es unknown
- 2012-08-30 CR CR20120451A patent/CR20120451A/es unknown
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Also Published As
| Publication number | Publication date |
|---|---|
| PH12012501719A1 (en) | 2012-11-12 |
| US20130072422A1 (en) | 2013-03-21 |
| EP2542238A1 (en) | 2013-01-09 |
| JP2013521295A (ja) | 2013-06-10 |
| CL2012002404A1 (es) | 2012-12-21 |
| SG183843A1 (en) | 2012-10-30 |
| CR20120451A (es) | 2012-10-16 |
| KR20130075723A (ko) | 2013-07-05 |
| AU2011223795A1 (en) | 2012-09-20 |
| MA34133B1 (fr) | 2013-04-03 |
| MX2012010017A (es) | 2012-10-01 |
| CU20120125A7 (es) | 2012-11-15 |
| CN102892417A (zh) | 2013-01-23 |
| ECSP12012140A (es) | 2012-10-30 |
| WO2011109355A1 (en) | 2011-09-09 |
| US9359398B2 (en) | 2016-06-07 |
| CA2791651C (en) | 2019-08-20 |
| BR112012022060A2 (pt) | 2018-05-08 |
| DOP2012000238A (es) | 2013-01-15 |
| AU2011223795B2 (en) | 2015-11-05 |
| JP6042724B2 (ja) | 2016-12-14 |
| CO6612265A2 (es) | 2013-02-01 |
| EP2542238B1 (en) | 2015-08-12 |
| CA2791651A1 (en) | 2011-09-09 |
| EA201290844A1 (ru) | 2013-03-29 |
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