BR112012022060A2 - composto para a inibição de imunoproteassoma - Google Patents
composto para a inibição de imunoproteassomaInfo
- Publication number
- BR112012022060A2 BR112012022060A2 BR112012022060A BR112012022060A BR112012022060A2 BR 112012022060 A2 BR112012022060 A2 BR 112012022060A2 BR 112012022060 A BR112012022060 A BR 112012022060A BR 112012022060 A BR112012022060 A BR 112012022060A BR 112012022060 A2 BR112012022060 A2 BR 112012022060A2
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- immunoproteasome
- inhibition
- relates
- treatment
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 230000005764 inhibitory process Effects 0.000 title abstract 2
- 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
- 208000026278 immune system disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
Classifications
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- 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
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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
- 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
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- 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
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- 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
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- 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)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (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)
Abstract
composto para a inibição de imunoproteassoma. um aspecto da invenção refere-se aos inibidores que inibem preferencialmente atividade de imunoproteassoma sobre atividade de proteassoma constitutivo. em determinadas concretizações, a invenção refere-se ao tratamento de enfermidades imuno relacionadas, que compreende administrar um composto da invenção. em determinadas concretizações, a invenção refere-se ao tratamento de câncer, que compreende administrar um composto da invenção.
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 |
---|---|
BR112012022060A2 true BR112012022060A2 (pt) | 2018-05-08 |
Family
ID=43983939
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112012022060A BR112012022060A2 (pt) | 2010-03-01 | 2011-03-01 | composto para a inibição de imunoproteassoma |
Country Status (20)
Country | Link |
---|---|
US (1) | US9359398B2 (pt) |
EP (1) | EP2542238B1 (pt) |
JP (1) | JP6042724B2 (pt) |
KR (1) | KR20130075723A (pt) |
CN (1) | CN102892417A (pt) |
AU (1) | AU2011223795B2 (pt) |
BR (1) | BR112012022060A2 (pt) |
CA (1) | CA2791651C (pt) |
CL (1) | CL2012002404A1 (pt) |
CO (1) | CO6612265A2 (pt) |
CR (1) | CR20120451A (pt) |
CU (1) | CU20120125A7 (pt) |
DO (1) | DOP2012000238A (pt) |
EA (1) | EA201290844A1 (pt) |
EC (1) | ECSP12012140A (pt) |
MA (1) | MA34133B1 (pt) |
MX (1) | MX2012010017A (pt) |
SG (1) | SG183843A1 (pt) |
WO (1) | WO2011109355A1 (pt) |
ZA (1) | ZA201206479B (pt) |
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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 |
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 |
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US20160031935A1 (en) * | 2013-03-15 | 2016-02-04 | Adaerata, Limited Partnership | Small molecule modulators of pcsk9 and methods 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 |
US11202817B2 (en) | 2014-08-18 | 2021-12-21 | Cornell University | Dipeptidomimetics as inhibitors of human immunoproteasomes |
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 |
EP4006012A1 (en) | 2015-10-15 | 2022-06-01 | Cornell University | Proteasome inhibitors and uses thereof |
US10526315B2 (en) | 2016-06-21 | 2020-01-07 | Orion Ophthalmology LLC | Carbocyclic prolinamide derivatives |
BR112018076614A2 (pt) | 2016-06-21 | 2019-04-02 | Orion Ophthalmology LLC | derivados heterocíclicos de prolinamida |
EP3694605A4 (en) | 2017-10-11 | 2021-10-27 | Cornell University | PEPTIDOMIMETIC PROTEASOME INHIBITORS |
EP3710063A1 (en) * | 2017-11-16 | 2020-09-23 | Amgen Inc. | Stable compositions of pegylated carfilzomib compounds |
EP3710458A1 (en) * | 2017-11-16 | 2020-09-23 | 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 |
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EP2542238B1 (en) | 2015-08-12 |
CA2791651C (en) | 2019-08-20 |
CO6612265A2 (es) | 2013-02-01 |
CA2791651A1 (en) | 2011-09-09 |
US9359398B2 (en) | 2016-06-07 |
ECSP12012140A (es) | 2012-10-30 |
SG183843A1 (en) | 2012-10-30 |
MX2012010017A (es) | 2012-10-01 |
JP2013521295A (ja) | 2013-06-10 |
CR20120451A (es) | 2012-10-16 |
KR20130075723A (ko) | 2013-07-05 |
AU2011223795B2 (en) | 2015-11-05 |
EA201290844A1 (ru) | 2013-03-29 |
WO2011109355A1 (en) | 2011-09-09 |
AU2011223795A1 (en) | 2012-09-20 |
MA34133B1 (fr) | 2013-04-03 |
DOP2012000238A (es) | 2013-01-15 |
EP2542238A1 (en) | 2013-01-09 |
CN102892417A (zh) | 2013-01-23 |
ZA201206479B (en) | 2015-08-26 |
CU20120125A7 (es) | 2012-11-15 |
US20130072422A1 (en) | 2013-03-21 |
CL2012002404A1 (es) | 2012-12-21 |
JP6042724B2 (ja) | 2016-12-14 |
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