CA2963203A1 - Boronic acid derivatives - Google Patents
Boronic acid derivatives Download PDFInfo
- Publication number
- CA2963203A1 CA2963203A1 CA2963203A CA2963203A CA2963203A1 CA 2963203 A1 CA2963203 A1 CA 2963203A1 CA 2963203 A CA2963203 A CA 2963203A CA 2963203 A CA2963203 A CA 2963203A CA 2963203 A1 CA2963203 A1 CA 2963203A1
- Authority
- CA
- Canada
- Prior art keywords
- amino
- ethyl
- boronic acid
- prop
- acetyl
- 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.)
- Pending
Links
Classifications
-
- 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
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- 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
- 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
- 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
- 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
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- 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
- C07F5/025—Boronic and borinic acid compounds
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14003389.5 | 2014-10-01 | ||
| EP14003389 | 2014-10-01 | ||
| PCT/EP2015/001973 WO2016050358A1 (en) | 2014-10-01 | 2015-10-01 | Boronic acid derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2963203A1 true CA2963203A1 (en) | 2016-04-07 |
Family
ID=51751859
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2963203A Pending CA2963203A1 (en) | 2014-10-01 | 2015-10-01 | Boronic acid derivatives |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US10669289B2 (enExample) |
| EP (1) | EP3201206B1 (enExample) |
| JP (1) | JP6662865B2 (enExample) |
| KR (1) | KR102457840B1 (enExample) |
| CN (1) | CN107001391B (enExample) |
| AU (1) | AU2015327345B9 (enExample) |
| BR (1) | BR112017006622A2 (enExample) |
| CA (1) | CA2963203A1 (enExample) |
| CL (1) | CL2017000792A1 (enExample) |
| DK (1) | DK3201206T3 (enExample) |
| ES (1) | ES2761774T3 (enExample) |
| IL (1) | IL251302B (enExample) |
| MX (1) | MX372823B (enExample) |
| MY (1) | MY186911A (enExample) |
| NZ (1) | NZ730981A (enExample) |
| PH (1) | PH12017500293A1 (enExample) |
| RU (1) | RU2717558C2 (enExample) |
| SG (1) | SG11201702628XA (enExample) |
| UA (1) | UA122672C2 (enExample) |
| WO (1) | WO2016050358A1 (enExample) |
| ZA (1) | ZA201703007B (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| EP3201208B1 (en) | 2014-10-01 | 2021-03-24 | Merck Patent GmbH | Boronic acid derivatives |
| US10294246B2 (en) | 2014-10-01 | 2019-05-21 | Merck Patent Gmbh | Substituted boronic acids and boronate esters as immunoproteasome inhibitors |
| EP3201205B1 (en) | 2014-10-01 | 2020-05-13 | Merck Patent GmbH | Boronic acid derivatives |
| PT3571208T (pt) | 2017-01-18 | 2021-04-13 | Principia Biopharma Inc | Inibidores do imunoproteassoma |
| US11274109B2 (en) | 2017-08-24 | 2022-03-15 | Merck Patent Gmbh | Boronic acid derivatives |
| WO2019042301A1 (zh) * | 2017-08-29 | 2019-03-07 | 浙江海正药业股份有限公司 | (E)-α,β-不饱和酰胺化合物及其制备方法和用途 |
| EP3694528A4 (en) * | 2017-10-13 | 2021-07-28 | The Regents of the University of California | MTORC1 MODULATORS |
| EP3710458B1 (en) * | 2017-11-16 | 2026-03-25 | Principia Biopharma Inc. | Immunoproteasome inhibitors |
| ES2928787T3 (es) * | 2017-11-16 | 2022-11-22 | Principia Biopharma Inc | Inhibidores del inmunoproteasoma |
| IL280376B2 (en) | 2018-07-26 | 2024-08-01 | Merck Patent Gmbh | Boronic acid derivatives, their preparation and pharmaceutical compositions containing them |
| CN113135944A (zh) * | 2020-01-19 | 2021-07-20 | 首药控股(北京)有限公司 | 硼酸衍生物 |
| CN113135943A (zh) * | 2020-01-19 | 2021-07-20 | 首药控股(北京)有限公司 | 硼酸衍生物 |
| EP4377324A1 (en) | 2021-07-29 | 2024-06-05 | Merck Patent GmbH | Novel crystalline forms of [(1r)-2-(1-benzofuran-3-yl)-1-{[(1s,2r,4r)-7- oxabicyclo[2.2.1]heptan-2-yl]formamido}ethyl]boronic acid, adducts thereof, and processes to obtain |
| US20240425529A1 (en) * | 2021-10-14 | 2024-12-26 | Shouyao Holdings (beijing) Co., Ltd. | Boric acid derivative |
| WO2023232830A1 (en) | 2022-06-02 | 2023-12-07 | Merck Patent Gmbh | Boronic acid adducts |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5658885A (en) * | 1993-04-27 | 1997-08-19 | The Dupont Merck Pharmaceutical Company | Amidino and guanidino substituted boronic acid inhibitors of trypsin-like enzymes |
| IL111175A0 (en) | 1993-10-07 | 1994-12-29 | Du Pont Merck Pharma | Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them |
| US5462964A (en) * | 1993-10-20 | 1995-10-31 | The Du Pont Merck Pharmaceutical Company | Dipeptide boronic acid inhibitors of trypsin-like enzymes |
| AU5920400A (en) * | 1999-07-07 | 2001-01-22 | Du Pont Pharmaceuticals Company | Cell-based assay systems for examining hcv ns3 protease activity |
| BR0314450A (pt) * | 2002-09-09 | 2005-07-26 | Trigen Ltd | Sais de ácido borÈnico com adição de uma base farmaceuticamente aceitável, formulação farmacêutica, e uso dos referidos sais para preparar uma formulação farmacêutica |
| UA88771C2 (ru) * | 2003-08-14 | 2009-11-25 | Сефалон, Инк. | Ингибиторы протеасомы и способ их применения (варианты) |
| US7576206B2 (en) * | 2003-08-14 | 2009-08-18 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| 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. |
| SG10201503168VA (en) | 2010-04-22 | 2015-06-29 | Mars Inc | Inhibitors of arginase and their therapeutic applications |
| SG11201403254QA (en) | 2011-12-22 | 2014-07-30 | Ares Trading Sa | Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors |
| SG10201908467RA (en) | 2014-01-31 | 2019-10-30 | Bristol Myers Squibb Co | Macrocycles with hetrocyclic p2' groups as factor xia inhibitors |
| MX2017004298A (es) | 2014-10-01 | 2017-07-19 | Janssen Pharmaceuticals Inc | Indoles mono o disustituidos como inhibidores de la replicacion del virus del denge. |
| US10294246B2 (en) | 2014-10-01 | 2019-05-21 | Merck Patent Gmbh | Substituted boronic acids and boronate esters as immunoproteasome inhibitors |
| EP3201208B1 (en) | 2014-10-01 | 2021-03-24 | Merck Patent GmbH | Boronic acid derivatives |
| ME03360B (me) | 2014-10-01 | 2019-10-20 | Janssen Pharmaceuticals Inc | Mono- ili di-supsтituisani derivaтi indola као inhibiтori replikacije virusa denge |
| EP3201205B1 (en) | 2014-10-01 | 2020-05-13 | Merck Patent GmbH | Boronic acid derivatives |
| NO2721243T3 (enExample) | 2014-10-01 | 2018-10-20 |
-
2015
- 2015-10-01 CN CN201580053501.9A patent/CN107001391B/zh active Active
- 2015-10-01 EP EP15778613.8A patent/EP3201206B1/en active Active
- 2015-10-01 KR KR1020177011562A patent/KR102457840B1/ko active Active
- 2015-10-01 AU AU2015327345A patent/AU2015327345B9/en active Active
- 2015-10-01 CA CA2963203A patent/CA2963203A1/en active Pending
- 2015-10-01 NZ NZ730981A patent/NZ730981A/en unknown
- 2015-10-01 MY MYPI2017701058A patent/MY186911A/en unknown
- 2015-10-01 MX MX2017003999A patent/MX372823B/es active IP Right Grant
- 2015-10-01 WO PCT/EP2015/001973 patent/WO2016050358A1/en not_active Ceased
- 2015-10-01 BR BR112017006622-0A patent/BR112017006622A2/pt not_active Application Discontinuation
- 2015-10-01 US US15/516,427 patent/US10669289B2/en active Active
- 2015-10-01 DK DK15778613.8T patent/DK3201206T3/da active
- 2015-10-01 UA UAA201704168A patent/UA122672C2/uk unknown
- 2015-10-01 RU RU2017115192A patent/RU2717558C2/ru active
- 2015-10-01 ES ES15778613T patent/ES2761774T3/es active Active
- 2015-10-01 JP JP2017518070A patent/JP6662865B2/ja active Active
- 2015-10-01 SG SG11201702628XA patent/SG11201702628XA/en unknown
-
2017
- 2017-02-16 PH PH12017500293A patent/PH12017500293A1/en unknown
- 2017-03-21 IL IL251302A patent/IL251302B/en active IP Right Grant
- 2017-03-31 CL CL2017000792A patent/CL2017000792A1/es unknown
- 2017-04-28 ZA ZA2017/03007A patent/ZA201703007B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL251302A0 (en) | 2017-05-29 |
| BR112017006622A2 (pt) | 2018-07-03 |
| DK3201206T3 (da) | 2019-12-16 |
| MY186911A (en) | 2021-08-26 |
| JP2017531646A (ja) | 2017-10-26 |
| AU2015327345B9 (en) | 2020-06-18 |
| KR20170067802A (ko) | 2017-06-16 |
| NZ730981A (en) | 2024-01-26 |
| AU2015327345B2 (en) | 2019-12-05 |
| ES2761774T3 (es) | 2020-05-21 |
| KR102457840B1 (ko) | 2022-10-21 |
| RU2017115192A3 (enExample) | 2019-03-26 |
| AU2015327345A1 (en) | 2017-05-18 |
| WO2016050358A1 (en) | 2016-04-07 |
| EP3201206A1 (en) | 2017-08-09 |
| JP6662865B2 (ja) | 2020-03-11 |
| IL251302B (en) | 2020-03-31 |
| RU2017115192A (ru) | 2018-11-06 |
| US20180179232A1 (en) | 2018-06-28 |
| ZA201703007B (en) | 2022-05-25 |
| US10669289B2 (en) | 2020-06-02 |
| RU2717558C2 (ru) | 2020-03-24 |
| MX2017003999A (es) | 2018-02-09 |
| UA122672C2 (uk) | 2020-12-28 |
| CN107001391A (zh) | 2017-08-01 |
| MX372823B (es) | 2020-07-03 |
| PH12017500293A1 (en) | 2017-06-28 |
| SG11201702628XA (en) | 2017-04-27 |
| CN107001391B (zh) | 2020-11-27 |
| EP3201206B1 (en) | 2019-09-18 |
| CL2017000792A1 (es) | 2017-11-10 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2015327345B9 (en) | Boronic acid derivatives | |
| AU2015327411B2 (en) | Boronic acid derivatives | |
| AU2015327346B2 (en) | Boronic acid derivatives | |
| EP3201208B1 (en) | Boronic acid derivatives | |
| EP2793900A1 (en) | Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20200928 |
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| U00 | Fee paid |
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