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)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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)
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) |
Families Citing this family (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PL1948678T3 (pl) | 2005-11-09 | 2013-09-30 | Onyx Therapeutics Inc | Związki do hamowania enzymów |
SI2041158T1 (sl) | 2006-06-19 | 2013-09-30 | Onyx Therapeutics, Inc. | Peptidni epoksiketoni za inhibicijo proteasomov |
US8367617B2 (en) | 2007-10-04 | 2013-02-05 | Onyx Therapeutics, Inc. | Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides |
JP5675629B2 (ja) | 2008-10-21 | 2015-02-25 | オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. | ペプチドエポキシケトンを用いた併用療法 |
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 |
MX2012010017A (es) * | 2010-03-01 | 2012-10-01 | Onyx Therapeutics Inc | Compuestos de para la inhibicion de inmunoproteasomas. |
MX2012011604A (es) | 2010-04-07 | 2013-02-27 | Onyx Therapeutics Inc | Inhibidor de inmunoproteasoma de péptido epoxicetona cristalino. |
US9309283B2 (en) | 2012-07-09 | 2016-04-12 | Onyx Therapeutics, Inc. | Prodrugs of peptide epoxy ketone protease inhibitors |
KR101782235B1 (ko) * | 2012-12-03 | 2017-09-26 | 에프. 호프만-라 로슈 아게 | 치환된 트라이아졸 붕소산 화합물 |
UY35455A (es) * | 2013-03-14 | 2014-09-30 | Onyx Therapeutics Inc | Inhibidores tripeptidicos de la epoxicetona proteasa |
CA2905237A1 (en) * | 2013-03-15 | 2014-09-18 | Adaerata, Limited Partnership | Small molecule modulators of pcsk9 and methods of use thereof |
US9988421B2 (en) | 2014-01-10 | 2018-06-05 | 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 |
CN114796207A (zh) | 2014-08-18 | 2022-07-29 | 康奈尔大学 | 作为人免疫蛋白酶体的抑制剂的二肽模拟物 |
WO2016050356A1 (en) * | 2014-10-01 | 2016-04-07 | Merck Patent Gmbh | Boronic acid derivatives |
KR20180064427A (ko) | 2015-10-15 | 2018-06-14 | 코넬 유니버시티 | 프로테아좀 억제제 및 이의 용도 |
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 |
EP4257191A3 (en) | 2016-06-21 | 2023-11-22 | Orion Ophthalmology LLC | Heterocyclic prolinamide derivatives |
EP3694605A4 (en) | 2017-10-11 | 2021-10-27 | Cornell University | PEPTIDOMIMETIC PROTEASOME INHIBITORS |
CN111344018A (zh) * | 2017-11-16 | 2020-06-26 | 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 |
AU2018367515B2 (en) * | 2017-11-16 | 2023-04-27 | 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 (pt) | 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 |
US4990448A (en) | 1989-08-04 | 1991-02-05 | Bristol-Myers Company | Bu-4061T |
US5071957A (en) | 1989-08-04 | 1991-12-10 | Bristol-Myers Company | Antibiotic BU-4061T |
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 |
CA2077665A1 (en) | 1990-03-05 | 1991-09-06 | Robert Siman | 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 |
WO1998010779A1 (en) | 1996-09-13 | 1998-03-19 | New York University | Method for treating parasitic diseases with proteasome inhibitors |
UA79749C2 (en) | 1996-10-18 | 2007-07-25 | Vertex Pharma | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
EP1136498A1 (en) | 1996-10-18 | 2001-09-26 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hepatitis c virus NS3 protease |
US5874418A (en) | 1997-05-05 | 1999-02-23 | Cydex, Inc. | Sulfoalkyl ether cyclodextrin based solid pharmaceutical formulations and their use |
US6046177A (en) | 1997-05-05 | 2000-04-04 | Cydex, Inc. | Sulfoalkyl ether cyclodextrin based controlled release solid pharmaceutical formulations |
PT986403E (pt) | 1997-06-13 | 2004-04-30 | Cydex Inc | Composicao com um tempo de vida de armazenagem prolongado compreendendo a ciclodextrina e drogas ou prodrogas que se decompoem em compostos insoluveis em agua |
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 |
WO2000023614A1 (en) | 1998-10-20 | 2000-04-27 | Millennium Pharmaceuticals, Inc. | Method for monitoring proteasome inhibitor drug action |
US6492333B1 (en) | 1999-04-09 | 2002-12-10 | Osteoscreen, Inc. | Treatment of myeloma bone disease with proteasomal and NF-κB activity inhibitors |
US6831099B1 (en) | 1999-05-12 | 2004-12-14 | Yale University | Enzyme inhibition |
AU784304B2 (en) | 1999-10-20 | 2006-03-09 | Osteoscreen, Inc. | Inhibitors of proteasomal activity for stimulating bone growth |
ATE338564T1 (de) | 2000-10-12 | 2006-09-15 | Viromics Gmbh | Proteasome inhibitoren zur behandlung von hepatitis-virus infektionen |
DK1355910T3 (da) | 2001-01-25 | 2011-06-27 | Us Of America Represented By The Secretary Dept Of Health And Human Services | Formulering af borsyreforbindelser |
DE60218153T2 (de) | 2001-05-21 | 2007-06-28 | Alcon Inc. | Verwendung von proteasom-inhibitoren zur behandlung des trockenen auges |
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 |
AU2003220685A1 (en) | 2002-04-09 | 2003-10-27 | Greenville Hospital System | Metastasis modulating activity of highly sulfated oligosaccharides |
US7968569B2 (en) | 2002-05-17 | 2011-06-28 | Celgene Corporation | Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione |
US20030224469A1 (en) | 2002-06-03 | 2003-12-04 | Buchholz Tonia J. | Methods and kits for assays utilizing fluorescence polarization |
US7902185B2 (en) | 2002-06-03 | 2011-03-08 | Als Therapy Development Foundation, Inc. | 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 |
DE122011100047I1 (de) | 2003-04-08 | 2011-12-15 | Mitsubishi Tanabe Pharma Corp | Feste pharmazeutische darreichungsformen mit einemS1P rezeptoragonisten und einem zuckeralkohol. |
JP4653103B2 (ja) | 2003-06-10 | 2011-03-16 | ザ ジェイ.ディヴィッド グラッドストン インスティテューツ | レンチウイルス感染症を治療するための方法 |
US7012063B2 (en) | 2003-06-13 | 2006-03-14 | Children's Medical Center Corporation | Reducing axon degeneration with proteasome inhibitors |
MX348041B (es) | 2003-12-31 | 2017-05-25 | Cydex Pharmaceuticals Inc | Formulación inhalante que contiene éter sulfoalquilico-ciclodextri na y un corticosteroide. |
GB0400804D0 (en) | 2004-01-14 | 2004-02-18 | Innoscience Technology Bv | Pharmaceutical compositions |
WO2005105827A2 (en) | 2004-04-15 | 2005-11-10 | Proteolix, Inc. | Compounds for proteasome 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 |
US8088741B2 (en) | 2004-05-10 | 2012-01-03 | Onyx Therapeutics, Inc. | Compounds for enzyme inhibition |
WO2005111009A2 (en) | 2004-05-10 | 2005-11-24 | Proteolix, Inc. | Synthesis of amino acid keto-epoxides |
WO2006045066A2 (en) | 2004-10-20 | 2006-04-27 | Proteolix, Inc. | Labeled compounds for proteasome inhibition |
HUE027850T2 (en) | 2004-12-07 | 2016-11-28 | Onyx Therapeutics Inc | Preparation for proteasome inhibition |
US7468383B2 (en) * | 2005-02-11 | 2008-12-23 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
EP1863513A2 (en) * | 2005-03-11 | 2007-12-12 | The University of North Carolina at Chapel Hill | Potent and specific immunoproteasome inhibitors |
US7998938B2 (en) | 2005-04-15 | 2011-08-16 | Geron Corporation | Cancer treatment by combined inhibition of proteasome and telomerase activities |
GT200600350A (es) | 2005-08-09 | 2007-03-28 | Formulaciones líquidas | |
PL1948678T3 (pl) | 2005-11-09 | 2013-09-30 | Onyx Therapeutics Inc | Związki do hamowania enzymów |
AR057227A1 (es) | 2005-12-09 | 2007-11-21 | Centocor Inc | Metodo para usar antagonistas de il6 con inhibidores del proteasoma |
US20070207950A1 (en) | 2005-12-21 | 2007-09-06 | Duke University | Methods and compositions for regulating HDAC6 activity |
WO2007122686A1 (ja) | 2006-04-14 | 2007-11-01 | Eisai R & D Management Co., Ltd. | ベンズイミダゾール化合物 |
DE102006026464A1 (de) | 2006-06-01 | 2007-12-06 | Virologik Gmbh Innovationszentrum Medizintechnik Und Pharma | Pharmazeutische Zusammensetzung zur Behandlung von Virusinfektionen und / oder Tumorerkrankungen durch Inhibition der Proteinfaltung und des Proteinabbaus |
SI2041158T1 (sl) | 2006-06-19 | 2013-09-30 | Onyx Therapeutics, Inc. | Peptidni epoksiketoni za inhibicijo proteasomov |
WO2008033807A2 (en) | 2006-09-13 | 2008-03-20 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Synergistic combinations of antineoplastic thiol-binding mitochondrial oxidants and antineoplastic proteasome inhibitors for the treatment of cancer |
WO2008091620A2 (en) | 2007-01-23 | 2008-07-31 | Gloucester Pharmaceuticals, Inc. | Combination therapy comprising romidepsin and i.a. bortezomib |
WO2008140782A2 (en) | 2007-05-10 | 2008-11-20 | Proteolix, Inc. | Compounds for enzyme inhibition |
SG10201508712QA (en) | 2007-08-06 | 2015-11-27 | Millenium Pharmaceuticals Inc | Proteasome inhibitors |
US7442830B1 (en) | 2007-08-06 | 2008-10-28 | Millenium Pharmaceuticals, Inc. | Proteasome inhibitors |
US8367617B2 (en) | 2007-10-04 | 2013-02-05 | Onyx Therapeutics, Inc. | Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides |
US7838673B2 (en) | 2007-10-16 | 2010-11-23 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
EP2212334B1 (en) | 2007-10-16 | 2012-08-15 | 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 |
EP2733147A1 (en) | 2008-06-17 | 2014-05-21 | 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. |
JP5675629B2 (ja) | 2008-10-21 | 2015-02-25 | オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. | ペプチドエポキシケトンを用いた併用療法 |
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 |
MX2012010017A (es) * | 2010-03-01 | 2012-10-01 | Onyx Therapeutics Inc | Compuestos de para la inhibicion de inmunoproteasomas. |
KR20130036228A (ko) | 2010-03-31 | 2013-04-11 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 1-아미노-2-사이클로프로필에틸보론산의 유도체 |
MX2012011604A (es) | 2010-04-07 | 2013-02-27 | Onyx Therapeutics Inc | Inhibidor de inmunoproteasoma de péptido epoxicetona cristalino. |
FR2962092B1 (fr) * | 2010-06-30 | 2013-06-28 | Valeo Systemes Dessuyage | Adaptateur d'essuie-glace a contacts electriques |
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EA201290844A1 (ru) | 2013-03-29 |
CL2012002404A1 (es) | 2012-12-21 |
WO2011109355A1 (en) | 2011-09-09 |
AU2011223795A1 (en) | 2012-09-20 |
CA2791651C (en) | 2019-08-20 |
CR20120451A (es) | 2012-10-16 |
US9359398B2 (en) | 2016-06-07 |
ECSP12012140A (es) | 2012-10-30 |
CN102892417A (zh) | 2013-01-23 |
KR20130075723A (ko) | 2013-07-05 |
JP6042724B2 (ja) | 2016-12-14 |
US20130072422A1 (en) | 2013-03-21 |
MA34133B1 (fr) | 2013-04-03 |
SG183843A1 (en) | 2012-10-30 |
EP2542238B1 (en) | 2015-08-12 |
CA2791651A1 (en) | 2011-09-09 |
AU2011223795B2 (en) | 2015-11-05 |
CU20120125A7 (es) | 2012-11-15 |
ZA201206479B (en) | 2015-08-26 |
EP2542238A1 (en) | 2013-01-09 |
MX2012010017A (es) | 2012-10-01 |
JP2013521295A (ja) | 2013-06-10 |
CO6612265A2 (es) | 2013-02-01 |
DOP2012000238A (es) | 2013-01-15 |
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