PE20050360A1 - PROTEASOME INHIBITORS - Google Patents
PROTEASOME INHIBITORSInfo
- Publication number
- PE20050360A1 PE20050360A1 PE2004000784A PE2004000784A PE20050360A1 PE 20050360 A1 PE20050360 A1 PE 20050360A1 PE 2004000784 A PE2004000784 A PE 2004000784A PE 2004000784 A PE2004000784 A PE 2004000784A PE 20050360 A1 PE20050360 A1 PE 20050360A1
- Authority
- PE
- Peru
- Prior art keywords
- amino
- alkyl
- methylbutyl
- methyl
- benzodioxaborol
- Prior art date
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
REFERIDA A UN COMPUESTO DE FORMULA I DONDE R1 ES ALQUILO C1-C8, ALQUENILO C2-C8, ALQUINILO C3-C7, ENTRE OTROS; R2 ES H, -(CH2)aCH2NHC(=NR4)NH-Y, -(CH2)cCH2N(R4)CONH2, ENTRE OTROS; a Y c SON CADA UNO 0-6; R4 ES H O ALQUILO C1-C10; Y ES H, -CN, -NO2, ENTRE OTROS; X ES RAC(=O)-, RANHC(=O)-, RA, ENTRE OTROS; RA ES ALQUILO C1-C20, ALQUENILO C2-C20, ALQUINILO C2-C20, ENTRE OTROS; Q ES UN ESTER BORONICO CICLICO, -B(OH)2, -B(OR14)2, ENTRE OTROS; R14 ES H, ALQUILO C1-C4, CICLOALQUILO, ARILO, ENTRE OTROS. TAMBIEN REFERIDA A UN PROCESO PARA PREPARAR ESTOS COMPUESTOS CUYOS PREFERIDOS SON: ACIDO BORONICO, [(1R)-1-[[(2S)-5-[[IMINO(NITROAMINO)METIL]AMINO]-2-[(2,2-DIMETILHEXANOIL)AMINO]-1-OXOPENTIL]AMINO]-3-METILBUTIL]; DECANAMIDA, N-[1-[[[(1R)-1-[(3aS,4S,6S,7aR)-HEXAHIDRO-3a,5,5-TRIMETIL-4,6-METANO-1,3,2-BENZODIOXABOROL-2-IL]-3-METILBUTIL]AMINO]CARBONIL]METIL] Y NAFTALENO-2-CARBOXAMIDA, N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-HEXAHIDRO-3a,5,5-TRIMETIL-4,6-METANO-1,3,2-BENZODIOXABOROL-2-IL]-3-METILBUTIL]AMINO]CARBONIL]-4-[[IMINO(NITROAMINO)METIL]AMINO]BUTIL]; ENTRE OTROS. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE CANCER Y OTROS DESORDENES ASOCIADOS A LA ACTIVIDAD DEL PROTEASOMAREFERRING TO A COMPOUND OF FORMULA I WHERE R1 IS C1-C8 ALKYL, C2-C8 ALKENYL, C3-C7 ALKYNYL, AMONG OTHERS; R2 IS H, - (CH2) aCH2NHC (= NR4) NH-Y, - (CH2) cCH2N (R4) CONH2, AMONG OTHERS; a AND c ARE EACH 0-6; R4 IS H O C1-C10 ALKYL; Y IS H, -CN, -NO2, AMONG OTHERS; X IS RAC (= O) -, RANHC (= O) -, RA, AMONG OTHERS; RA IS C1-C20 ALKYL, C2-C20 ALKYL, C2-C20 ALKYL, AMONG OTHERS; Q IS A CYCLIC BORONIC ESTER, -B (OH) 2, -B (OR14) 2, AMONG OTHERS; R14 IS H, C1-C4 ALKYL, CYCLOALKYL, ARYL, AMONG OTHERS. ALSO REFERRED TO A PROCESS TO PREPARE THESE COMPOUNDS WHOSE PREFERRED ARE: BORONIC ACID, [(1R) -1 - [[(2S) -5 - [[IMINO (NITROAMINE) METHYL] AMINO] -2 - [(2,2- DIMETHYLHEXANOYL) AMINO] -1-OXOPENTIL] AMINO] -3-METHYLBUTYL]; DECANAMIDE, N- [1 - [[[(1R) -1 - [(3aS, 4S, 6S, 7aR) -HEXAHYDRO-3a, 5,5-TRIMETHYL-4,6-METHANE-1,3,2-BENZODIOXABOROL -2-IL] -3-METHYLBUTYL] AMINO] CARBONYL] METHYL] AND NAPHTHALENE-2-CARBOXAMIDE, N - [(1S) -1 - [[[(1R) -1 - [(3aS, 4S, 6S, 7aR ) -HEXAHYDRO-3a, 5,5-TRIMETHYL-4,6-METHANE-1,3,2-BENZODIOXABOROL-2-IL] -3-METHYLBUTYL] AMINO] CARBONYL] -4 - [[IMINO (NITROAMINE) METHYL] AMINO] BUTYL]; AMONG OTHERS. SUCH COMPOUNDS ARE USEFUL IN THE TREATMENT OF CANCER AND OTHER DISORDERS ASSOCIATED WITH THE ACTIVITY OF THE PROTEASOMA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US49576403P | 2003-08-14 | 2003-08-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20050360A1 true PE20050360A1 (en) | 2005-06-10 |
Family
ID=37426112
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2004000784A PE20050360A1 (en) | 2003-08-14 | 2004-08-13 | PROTEASOME INHIBITORS |
Country Status (7)
| Country | Link |
|---|---|
| CN (1) | CN1867572B (en) |
| AR (2) | AR045381A1 (en) |
| MY (1) | MY162518A (en) |
| PE (1) | PE20050360A1 (en) |
| TW (1) | TWI345465B (en) |
| UA (1) | UA88771C2 (en) |
| ZA (1) | ZA200601293B (en) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20140042932A (en) * | 2007-08-06 | 2014-04-07 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Proteasome inhibitors |
| CN102961387B (en) * | 2007-08-06 | 2016-04-27 | 米伦纽姆医药公司 | Proteasome inhibitor |
| CN105837608B (en) * | 2007-08-06 | 2018-06-08 | 米伦纽姆医药公司 | Proteasome inhibitor and combinations thereof and purposes |
| CN103497232A (en) * | 2008-06-17 | 2014-01-08 | 米伦纽姆医药公司 | Boronate ester compounds and pharmaceutical compositions thereof |
| CN101638414B (en) * | 2008-07-30 | 2014-01-08 | 江苏先声药物研究有限公司 | Peptidyl boronic acid, ester compound thereof, preparation method of peptidyl boronic acid and ester compound thereof, and use of peptidyl boronic acid and ester compound thereof |
| AR075090A1 (en) * | 2008-09-29 | 2011-03-09 | Millennium Pharm Inc | ACID DERIVATIVES 1-AMINO-2-CYCLLOBUTILETILBORONICO PROTEOSOMA INHIBITORS, USEFUL AS ANTI-BANKER AGENTS, AND PHARMACEUTICAL COMPOSITIONS THAT UNDERSTAND THEM. |
| CN101747354B (en) * | 2008-12-04 | 2014-08-13 | 江苏先声药物研究有限公司 | Dipeptide boronic acids consisting of beta amino acids, ester compounds and preparation methods and uses thereof |
| EP2516449A1 (en) * | 2009-12-22 | 2012-10-31 | Cephalon, Inc. | Proteasome inhibitors and processes for their preparation, purification and use |
| MX2012011298A (en) * | 2010-03-31 | 2012-11-06 | Millennium Pharm Inc | Derivatives of 1-amino-2-cyclopropylethylboronic acid. |
| US10669289B2 (en) * | 2014-10-01 | 2020-06-02 | Merck Patent Gmbh | Boronic acid derivatives |
| CN106588965A (en) * | 2015-10-15 | 2017-04-26 | 北京大学 | Urea peptidomimetic boric acid compound as well as pharmaceutical composition, preparation method and application thereof |
| CN107400142B (en) * | 2016-05-19 | 2019-11-19 | 成都奥璟生物科技有限公司 | A kind of boric acid and boric acid ester compound and its application |
| WO2018136401A1 (en) * | 2017-01-18 | 2018-07-26 | Principia Biopharma Inc. | Immunoproteasome inhibitors |
| CN108440583B (en) * | 2017-01-23 | 2020-12-04 | 成都奥璟生物科技有限公司 | Boric acid derivative and its medicinal composition |
| CN114437119B (en) * | 2020-10-30 | 2024-08-09 | 苏州开拓药业股份有限公司 | C-Myc protein inhibitor and preparation method and application thereof |
-
2004
- 2004-08-13 TW TW93124291A patent/TWI345465B/en not_active IP Right Cessation
- 2004-08-13 PE PE2004000784A patent/PE20050360A1/en active IP Right Grant
- 2004-08-13 MY MYPI20043299A patent/MY162518A/en unknown
- 2004-08-13 CN CN2004800301520A patent/CN1867572B/en not_active Expired - Lifetime
- 2004-08-13 UA UAA200602694A patent/UA88771C2/en unknown
- 2004-08-17 AR ARP040102935 patent/AR045381A1/en not_active Application Discontinuation
-
2006
- 2006-02-13 ZA ZA200601293A patent/ZA200601293B/en unknown
-
2014
- 2014-03-11 AR ARP140100859A patent/AR095249A2/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CN1867572A (en) | 2006-11-22 |
| CN1867572B (en) | 2012-03-28 |
| MY162518A (en) | 2017-06-15 |
| TWI345465B (en) | 2011-07-21 |
| AR045381A1 (en) | 2005-10-26 |
| AR095249A2 (en) | 2015-09-30 |
| UA88771C2 (en) | 2009-11-25 |
| ZA200601293B (en) | 2009-09-30 |
| TW200529810A (en) | 2005-09-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |