KR101739470B1 - 1-아미노-2-시클로부틸에틸보론산의 유도체 - Google Patents
1-아미노-2-시클로부틸에틸보론산의 유도체 Download PDFInfo
- Publication number
- KR101739470B1 KR101739470B1 KR1020117009732A KR20117009732A KR101739470B1 KR 101739470 B1 KR101739470 B1 KR 101739470B1 KR 1020117009732 A KR1020117009732 A KR 1020117009732A KR 20117009732 A KR20117009732 A KR 20117009732A KR 101739470 B1 KR101739470 B1 KR 101739470B1
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- boronic acid
- substituted
- formula
- pharmaceutically acceptable
- 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.)
- Expired - Fee Related
Links
Classifications
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- 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
- A61K31/69—Boron compounds
-
- 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
- C07F5/025—Boronic and borinic acid compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
-
- 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
-
- 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
- C07K5/06—Dipeptides
-
- 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
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Psychology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19461408P | 2008-09-29 | 2008-09-29 | |
| US61/194,614 | 2008-09-29 | ||
| PCT/US2009/005324 WO2010036357A1 (en) | 2008-09-29 | 2009-09-25 | Derivatives of 1-amino-2-cyclobutylethylboronic acid |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20110082534A KR20110082534A (ko) | 2011-07-19 |
| KR101739470B1 true KR101739470B1 (ko) | 2017-05-24 |
Family
ID=41426361
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020117009732A Expired - Fee Related KR101739470B1 (ko) | 2008-09-29 | 2009-09-25 | 1-아미노-2-시클로부틸에틸보론산의 유도체 |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US8664200B2 (https=) |
| EP (1) | EP2346882B1 (https=) |
| JP (3) | JP5736314B2 (https=) |
| KR (1) | KR101739470B1 (https=) |
| CN (2) | CN102203103A (https=) |
| AR (1) | AR075090A1 (https=) |
| AU (1) | AU2009297113B2 (https=) |
| BR (1) | BRPI0919447B8 (https=) |
| CA (1) | CA2739375C (https=) |
| CL (1) | CL2011000653A1 (https=) |
| CO (1) | CO6362015A2 (https=) |
| CR (2) | CR20160475A (https=) |
| DO (1) | DOP2011000086A (https=) |
| EA (1) | EA030539B1 (https=) |
| EC (1) | ECSP11011011A (https=) |
| IL (1) | IL211983A0 (https=) |
| MA (1) | MA32729B1 (https=) |
| MX (1) | MX2011003317A (https=) |
| MY (1) | MY166653A (https=) |
| NZ (2) | NZ606001A (https=) |
| SG (1) | SG194388A1 (https=) |
| TW (2) | TWI598352B (https=) |
| UA (1) | UA105503C2 (https=) |
| WO (1) | WO2010036357A1 (https=) |
| ZA (1) | ZA201203615B (https=) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2453556C2 (ru) | 2005-11-09 | 2012-06-20 | Протеоликс, Инк. | Соединения для ингибирования фермента |
| RU2450016C2 (ru) | 2006-06-19 | 2012-05-10 | Протеоликс, Инк. | Пептидные эпоксикетоны для ингибирования протеасомы |
| KR20170040374A (ko) | 2007-10-04 | 2017-04-12 | 오닉스 세라퓨틱스, 인크. | 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성 |
| CA2727862C (en) | 2008-06-17 | 2016-04-19 | Millennium Pharmaceuticals, Inc. | Boronate ester compounds and pharmaceutical compositions thereof |
| AU2009308516B2 (en) | 2008-10-21 | 2016-08-25 | Onyx Therapeutics, Inc. | Combination therapy with peptide epoxyketones |
| AR075899A1 (es) | 2009-03-20 | 2011-05-04 | Onyx Therapeutics Inc | Tripeptidos epoxicetonas cristalinos inhibidores de proteasa |
| 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 |
| CA2791651C (en) | 2010-03-01 | 2019-08-20 | Onyx Therapeutics, Inc. | Compounds for immunoproteasome inhibition |
| US8513218B2 (en) | 2010-03-31 | 2013-08-20 | Millennium Pharmaceuticals, Inc. | Derivatives of 1-amino-2-cyclopropylethylboronic acid |
| CN104039328B (zh) | 2011-11-11 | 2018-10-09 | 米伦纽姆医药公司 | 对蛋白酶体抑制剂的反应的生物标记 |
| CA2855368A1 (en) | 2011-11-11 | 2013-05-16 | Millennium Pharmaceuticals, Inc. | Biomarkers of response to proteasome inhibitors |
| SG11201403254QA (en) * | 2011-12-22 | 2014-07-30 | Ares Trading Sa | Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors |
| JP6215235B2 (ja) | 2012-01-24 | 2017-10-18 | ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. | 癌の治療方法 |
| JP2015524394A (ja) | 2012-07-09 | 2015-08-24 | 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プロテアーゼ阻害剤のプロドラッグ |
| US9464098B2 (en) * | 2012-12-03 | 2016-10-11 | Hoffmann-La Roche Inc. | Substituted triazole boronic acid compounds |
| MX2016003979A (es) | 2013-10-03 | 2016-06-15 | Millennium Pharm Inc | Metodo para profilaxis o tratamiento de lupus eritematoso sistemico y/o nefritis lupica. |
| ES2748434T3 (es) | 2014-01-10 | 2020-03-16 | Univ Cornell | Dipéptidos como inhibidores de inmunoproteasomas humanos |
| TN2016000492A1 (en) | 2014-05-20 | 2018-04-04 | Millennium Pharm Inc | Boron-containing proteasome inhibitors for use after primary cancer therapy. |
| WO2016022955A1 (en) | 2014-08-07 | 2016-02-11 | Mayo Foundation For Medical Education And Research | Compounds and methods for treating cancer |
| EP3193904B1 (en) | 2014-08-18 | 2025-10-01 | Cornell University | Dipeptidomimetics as inhibitors of human immunoproteasomes |
| RU2017115191A (ru) * | 2014-10-01 | 2018-11-06 | Мерк Патент Гмбх | Производные бороновой кислоты |
| JP6662865B2 (ja) * | 2014-10-01 | 2020-03-11 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | ボロン酸誘導体 |
| BR112017006420A2 (pt) * | 2014-10-01 | 2017-12-19 | Merck Patent Gmbh | derivados de ácido borônico |
| RU2017115193A (ru) * | 2014-10-01 | 2018-11-06 | Мерк Патент Гмбх | Производные бороновой кислоты |
| KR102764027B1 (ko) | 2015-10-15 | 2025-02-07 | 코넬 유니버시티 | 프로테아좀 억제제 및 이의 용도 |
| HUE064412T2 (hu) | 2016-06-21 | 2024-03-28 | Orion Ophthalmology LLC | Heterociklusos prolinamid-származékok |
| 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 |
| EP3589659B1 (en) | 2017-02-28 | 2025-04-09 | Mayo Foundation for Medical Education and Research | Combinations for use in the treatment of cancer |
| EP3694605A4 (en) | 2017-10-11 | 2021-10-27 | Cornell University | PEPTIDOMIMETIC PROTEASOME INHIBITORS |
| US11243207B2 (en) | 2018-03-29 | 2022-02-08 | Mayo Foundation For Medical Education And Research | Assessing and treating cancer |
| JP7598875B2 (ja) | 2019-04-12 | 2024-12-12 | リボサイエンス リミティド ライアビリティ カンパニー | エクトヌクレオチドピロホスファターゼホスホジエステラーゼ1阻害剤としての二環式ヘテロアリール誘導体 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996013266A1 (en) | 1994-10-28 | 1996-05-09 | Proscript, Inc. | Boronic ester and acid compounds, synthesis and uses |
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| NZ203706A (en) | 1982-04-22 | 1986-03-14 | Squibb & Sons Inc | Occlusive multi-layer wound dressing and hydrocolloidal granules for wound treatment |
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| US5250720A (en) | 1987-06-05 | 1993-10-05 | The Dupont Merck Pharmaceutical Company | Intermediates for preparing peptide boronic acid inhibitors of trypsin-like proteases |
| US5187157A (en) | 1987-06-05 | 1993-02-16 | Du Pont Merck Pharmaceutical Company | Peptide boronic acid inhibitors of trypsin-like proteases |
| US5242904A (en) | 1987-06-05 | 1993-09-07 | The Dupont Merck Pharmaceutical Company | Peptide boronic acid inhibitors of trypsin-like proteases |
| EP0315574A3 (de) | 1987-11-05 | 1990-08-22 | Hoechst Aktiengesellschaft | Renin-Inhibitoren |
| US5159060A (en) | 1988-05-27 | 1992-10-27 | Mayo Foundation For Medical Education And Research | Cytotoxic boronic acid peptide analogs |
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| DE3827340A1 (de) * | 1988-08-12 | 1990-02-15 | Hoechst Ag | Verwendung von (alpha)-aminoboronsaeure-derivaten zur prophylaxe und behandlung von viruserkrankungen |
| EP0583536B1 (en) | 1992-08-14 | 1997-03-05 | The Procter & Gamble Company | Liquid detergents containing an alpha-amino boronic acid |
| US5935944A (en) | 1993-09-10 | 1999-08-10 | Neutron Technology Corporation | Formulation for I.V. administration of the boron delivery drug, boronophenylalanine (BPA) |
| US5492900A (en) | 1993-09-10 | 1996-02-20 | Neutron Technology Corporation | Method for enhancing the solubility of the boron delivery drug, boronophenylalanine (BPA) |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996013266A1 (en) | 1994-10-28 | 1996-05-09 | Proscript, Inc. | Boronic ester and acid compounds, synthesis and uses |
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