JP2013515082A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013515082A5 JP2013515082A5 JP2012546173A JP2012546173A JP2013515082A5 JP 2013515082 A5 JP2013515082 A5 JP 2013515082A5 JP 2012546173 A JP2012546173 A JP 2012546173A JP 2012546173 A JP2012546173 A JP 2012546173A JP 2013515082 A5 JP2013515082 A5 JP 2013515082A5
- Authority
- JP
- Japan
- Prior art keywords
- pat
- international publication
- european
- opposition
- patent application
- 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.)
- Granted
Links
- 239000003112 inhibitor Substances 0.000 description 7
- 102000035195 Peptidases Human genes 0.000 description 6
- 108091005804 Peptidases Proteins 0.000 description 6
- 230000005764 inhibitory process Effects 0.000 description 5
- 239000004365 Protease Substances 0.000 description 4
- 229940079156 Proteasome inhibitor Drugs 0.000 description 4
- GXJABQQUPOEUTA-RDJZCZTQSA-N bortezomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)B(O)O)NC(=O)C=1N=CC=NC=1)C1=CC=CC=C1 GXJABQQUPOEUTA-RDJZCZTQSA-N 0.000 description 4
- 210000004027 cell Anatomy 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 239000003207 proteasome inhibitor Substances 0.000 description 4
- 108090000623 proteins and genes Proteins 0.000 description 4
- 102000004169 proteins and genes Human genes 0.000 description 4
- 206010028980 Neoplasm Diseases 0.000 description 3
- 108090000708 Proteasome Endopeptidase Complex Proteins 0.000 description 3
- 102000004245 Proteasome Endopeptidase Complex Human genes 0.000 description 3
- 108010026552 Proteome Proteins 0.000 description 3
- 229960001467 bortezomib Drugs 0.000 description 3
- 201000011510 cancer Diseases 0.000 description 3
- 238000012512 characterization method Methods 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- -1 pinanediol boronic acid ester derivative of bortezomib Chemical class 0.000 description 3
- 108090000765 processed proteins & peptides Proteins 0.000 description 3
- 235000019419 proteases Nutrition 0.000 description 3
- 238000011160 research Methods 0.000 description 3
- 238000003786 synthesis reaction Methods 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 2
- 230000015556 catabolic process Effects 0.000 description 2
- 230000022131 cell cycle Effects 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000006731 degradation reaction Methods 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 238000011275 oncology therapy Methods 0.000 description 2
- 230000003389 potentiating effect Effects 0.000 description 2
- 239000002243 precursor Substances 0.000 description 2
- 235000019833 protease Nutrition 0.000 description 2
- 230000017854 proteolysis Effects 0.000 description 2
- 230000002797 proteolythic effect Effects 0.000 description 2
- 229940124718 AIDS vaccine Drugs 0.000 description 1
- 108010022579 ATP dependent 26S protease Proteins 0.000 description 1
- 102000007566 ATP-Dependent Proteases Human genes 0.000 description 1
- 108010071550 ATP-Dependent Proteases Proteins 0.000 description 1
- 101100161935 Caenorhabditis elegans act-4 gene Proteins 0.000 description 1
- 101710155556 Calcium-dependent protease Proteins 0.000 description 1
- 241001432959 Chernes Species 0.000 description 1
- 108090000317 Chymotrypsin Proteins 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 208000031886 HIV Infections Diseases 0.000 description 1
- 241000238631 Hexapoda Species 0.000 description 1
- DAQAKHDKYAWHCG-UHFFFAOYSA-N Lactacystin Natural products CC(=O)NC(C(O)=O)CSC(=O)C1(C(O)C(C)C)NC(=O)C(C)C1O DAQAKHDKYAWHCG-UHFFFAOYSA-N 0.000 description 1
- 108010028275 Leukocyte Elastase Proteins 0.000 description 1
- 102000016799 Leukocyte elastase Human genes 0.000 description 1
- 102000043136 MAP kinase family Human genes 0.000 description 1
- 108091054455 MAP kinase family Proteins 0.000 description 1
- 102000043129 MHC class I family Human genes 0.000 description 1
- 108091054437 MHC class I family Proteins 0.000 description 1
- 206010029260 Neuroblastoma Diseases 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- 108010067372 Pancreatic elastase Proteins 0.000 description 1
- 102000016387 Pancreatic elastase Human genes 0.000 description 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 1
- 108010018242 Transcription Factor AP-1 Proteins 0.000 description 1
- 102100023132 Transcription factor Jun Human genes 0.000 description 1
- 238000001042 affinity chromatography Methods 0.000 description 1
- 150000001414 amino alcohols Chemical class 0.000 description 1
- 210000004102 animal cell Anatomy 0.000 description 1
- 230000030741 antigen processing and presentation Effects 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 125000003180 beta-lactone group Chemical group 0.000 description 1
- 230000003115 biocidal effect Effects 0.000 description 1
- 238000006795 borylation reaction Methods 0.000 description 1
- 229960005520 bryostatin Drugs 0.000 description 1
- MJQUEDHRCUIRLF-TVIXENOKSA-N bryostatin 1 Chemical compound C([C@@H]1CC(/[C@@H]([C@@](C(C)(C)/C=C/2)(O)O1)OC(=O)/C=C/C=C/CCC)=C\C(=O)OC)[C@H]([C@@H](C)O)OC(=O)C[C@H](O)C[C@@H](O1)C[C@H](OC(C)=O)C(C)(C)[C@]1(O)C[C@@H]1C\C(=C\C(=O)OC)C[C@H]\2O1 MJQUEDHRCUIRLF-TVIXENOKSA-N 0.000 description 1
- MUIWQCKLQMOUAT-AKUNNTHJSA-N bryostatin 20 Natural products COC(=O)C=C1C[C@@]2(C)C[C@]3(O)O[C@](C)(C[C@@H](O)CC(=O)O[C@](C)(C[C@@]4(C)O[C@](O)(CC5=CC(=O)O[C@]45C)C(C)(C)C=C[C@@](C)(C1)O2)[C@@H](C)O)C[C@H](OC(=O)C(C)(C)C)C3(C)C MUIWQCKLQMOUAT-AKUNNTHJSA-N 0.000 description 1
- 230000003197 catalytic effect Effects 0.000 description 1
- 230000003034 chemosensitisation Effects 0.000 description 1
- 238000004587 chromatography analysis Methods 0.000 description 1
- 229960002376 chymotrypsin Drugs 0.000 description 1
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 1
- 229940125808 covalent inhibitor Drugs 0.000 description 1
- 230000000593 degrading effect Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 150000002009 diols Chemical class 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 239000006260 foam Substances 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 230000014509 gene expression Effects 0.000 description 1
- 230000035876 healing Effects 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 238000002955 isolation Methods 0.000 description 1
- MBOMYENWWXQSNW-AWEZNQCLSA-N ixazomib citrate Chemical compound N([C@@H](CC(C)C)B1OC(CC(O)=O)(CC(O)=O)C(=O)O1)C(=O)CNC(=O)C1=CC(Cl)=CC=C1Cl MBOMYENWWXQSNW-AWEZNQCLSA-N 0.000 description 1
- DAQAKHDKYAWHCG-RWTHQLGUSA-N lactacystin Chemical compound CC(=O)N[C@H](C(O)=O)CSC(=O)[C@]1([C@@H](O)C(C)C)NC(=O)[C@H](C)[C@@H]1O DAQAKHDKYAWHCG-RWTHQLGUSA-N 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 1
- 210000004962 mammalian cell Anatomy 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 239000003016 pheromone Substances 0.000 description 1
- 230000001817 pituitary effect Effects 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 125000006239 protecting group Chemical group 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000003642 reactive oxygen metabolite Substances 0.000 description 1
- 239000013037 reversible inhibitor Substances 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 229940099039 velcade Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28895709P | 2009-12-22 | 2009-12-22 | |
| US61/288,957 | 2009-12-22 | ||
| PCT/US2010/061695 WO2011087822A1 (en) | 2009-12-22 | 2010-12-22 | Proteasome inhibitors and processes for their preparation, purification and use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013515082A JP2013515082A (ja) | 2013-05-02 |
| JP2013515082A5 true JP2013515082A5 (https=) | 2014-02-13 |
| JP5783659B2 JP5783659B2 (ja) | 2015-09-24 |
Family
ID=43530797
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012546173A Expired - Fee Related JP5783659B2 (ja) | 2009-12-22 | 2010-12-22 | プロテアソーム阻害剤およびその調製、精製および使用のための方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US8541590B2 (https=) |
| EP (1) | EP2516449A1 (https=) |
| JP (1) | JP5783659B2 (https=) |
| CN (1) | CN102725300B (https=) |
| AU (1) | AU2010341530B2 (https=) |
| CA (1) | CA2785300A1 (https=) |
| IL (1) | IL220190A0 (https=) |
| MX (1) | MX2012007341A (https=) |
| NZ (1) | NZ600786A (https=) |
| WO (1) | WO2011087822A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20150067175A (ko) | 2012-09-11 | 2015-06-17 | 시플라 리미티드 | 보르테조밉을 제조하기 위한 방법 |
| CN103897027A (zh) * | 2012-12-29 | 2014-07-02 | 曹亚英 | 关键中间体晶型，制备方法及其在硼替佐米合成中的运用 |
| CN103897026A (zh) * | 2012-12-29 | 2014-07-02 | 朱继东 | 硼替佐米关键中间体的晶型，制备方法及其运用 |
| IN2013MU01431A (https=) | 2013-04-16 | 2015-06-26 | Cipla Ltd | |
| CZ2015233A3 (cs) | 2015-04-03 | 2016-10-12 | Zentiva, K.S. | Způsob přípravy Ixazomib citrátu |
| CZ2015253A3 (cs) | 2015-04-15 | 2016-10-26 | Zentiva, K.S. | Nové formy Ixazomib citrátu |
| US10144761B2 (en) | 2015-06-19 | 2018-12-04 | Hanlin Scientific Inc. | Chiral specific boron-containing compounds and their use in treating cancer or amyloidosis |
| CZ2016204A3 (cs) | 2016-04-08 | 2017-11-01 | Zentiva, K.S. | Formulace Ixazomib citrátu formy 3 |
| EP3583110A1 (en) | 2017-02-17 | 2019-12-25 | Fresenius Kabi Oncology Ltd | An improved process for the preparation of boronic acid esters |
| JP7086987B2 (ja) * | 2017-03-21 | 2022-06-20 | ザ スクリプス リサーチ インスティテュート | 銅およびニッケル触媒による脱炭酸ホウ素化反応 |
| CN110540547A (zh) * | 2018-05-28 | 2019-12-06 | 秦艳茹 | 一种肽硼酸酯类化合物的合成与用途 |
Family Cites Families (63)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3301354A1 (de) | 1983-01-18 | 1984-07-19 | Matth. Hohner Ag, 7218 Trossingen | Elektronisches musikinstrument |
| US4537773A (en) | 1983-12-05 | 1985-08-27 | E. I. Du Pont De Nemours And Company | α-Aminoboronic acid derivatives |
| US4499082A (en) | 1983-12-05 | 1985-02-12 | E. I. Du Pont De Nemours And Company | α-Aminoboronic acid peptides |
| US5242904A (en) | 1987-06-05 | 1993-09-07 | The Dupont Merck Pharmaceutical Company | Peptide boronic acid inhibitors of trypsin-like proteases |
| 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 |
| EP0315574A3 (de) | 1987-11-05 | 1990-08-22 | Hoechst Aktiengesellschaft | Renin-Inhibitoren |
| AU3418389A (en) | 1988-03-28 | 1989-10-16 | Regents Of The University Of California, The | Nerve growth factor peptides |
| US5023236A (en) | 1988-04-07 | 1991-06-11 | Corvas, Inc. | Factor VII/VIIA active site inhibitors |
| US5106948A (en) | 1988-05-27 | 1992-04-21 | Mao Foundation For Medical Education And Research | Cytotoxic boronic acid peptide analogs |
| US5159060A (en) | 1988-05-27 | 1992-10-27 | Mayo Foundation For Medical Education And Research | Cytotoxic boronic acid peptide analogs |
| US4963655A (en) | 1988-05-27 | 1990-10-16 | Mayo Foundation For Medical Education And Research | Boron analogs of amino acid/peptide protease inhibitors |
| DE3827340A1 (de) | 1988-08-12 | 1990-02-15 | Hoechst Ag | Verwendung von (alpha)-aminoboronsaeure-derivaten zur prophylaxe und behandlung von viruserkrankungen |
| AU661270B2 (en) | 1990-03-05 | 1995-07-20 | Cephalon, Inc. | Chymotrypsin-like proteases and their inhibitors |
| EP0583536B1 (en) | 1992-08-14 | 1997-03-05 | The Procter & Gamble Company | Liquid detergents containing an alpha-amino boronic acid |
| EP0684829A4 (en) | 1993-02-10 | 1997-05-21 | Harvard College | THE ROLE OF ATP-UBIQUITIN-DEPENDENT PROTEOLYSIS IN MHC-1 DEPENDENT ANTIGENT PRESENTATION AND RELATED INHIBITORS. |
| IL109319A0 (en) | 1993-04-27 | 1994-07-31 | Du Pont Merck Pharma | Amidino and guanidino substituted boronic acid compounds |
| US5658885A (en) | 1993-04-27 | 1997-08-19 | The Dupont Merck Pharmaceutical Company | Amidino and guanidino substituted boronic acid inhibitors of trypsin-like enzymes |
| US5672582A (en) | 1993-04-30 | 1997-09-30 | Merck & Co., Inc. | Thrombin inhibitors |
| DE69431718T2 (de) | 1993-04-30 | 2003-07-10 | Merck & Co., Inc. | Thrombin-inhibitoren |
| FR2707085B1 (fr) | 1993-06-30 | 1995-08-18 | Adir | Nouveaux dérivés d'alpha amino acides, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent. |
| JPH09505281A (ja) | 1993-10-01 | 1997-05-27 | メレルファーマスーティカルズ インコーポレイテッド | β−アミロイド蛋白質製造の阻害剤類 |
| 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 |
| GB9401483D0 (en) | 1994-01-26 | 1994-03-23 | Sandoz Ltd | Organic compounds |
| 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 |
| US6083903A (en) | 1994-10-28 | 2000-07-04 | Leukosite, Inc. | Boronic ester and acid compounds, synthesis and uses |
| US5550262A (en) | 1994-11-14 | 1996-08-27 | Cephalon, Inc. | Multicatalytic protease inhibitors |
| US5614649A (en) | 1994-11-14 | 1997-03-25 | Cephalon, Inc. | Multicatalytic protease inhibitors |
| US5834487A (en) | 1996-09-24 | 1998-11-10 | Cv Therapeutics | Inhibition of 26S and 20S proteasome by indanones |
| AP1019A (en) | 1996-10-18 | 2001-10-16 | Vertex Pharma | Inhibitors of serinre proteases, particularly hepatitis C virus NS3 protease. |
| GB9623908D0 (en) | 1996-11-18 | 1997-01-08 | Hoffmann La Roche | Amino acid derivatives |
| US6096778A (en) | 1997-10-07 | 2000-08-01 | Cephalon, Inc. | α-ketoamide multicatalytic protease inhibitors |
| CN1282242A (zh) | 1997-12-16 | 2001-01-31 | 赛福伦公司 | 多相催化蛋白酶抑制剂用作抗肿瘤剂 |
| US6075150A (en) | 1998-01-26 | 2000-06-13 | Cv Therapeutics, Inc. | α-ketoamide inhibitors of 20S proteasome |
| GB9806815D0 (en) | 1998-03-30 | 1998-05-27 | Hoffmann La Roche | Amino acid derivatives |
| US6462019B1 (en) | 1998-07-10 | 2002-10-08 | Osteoscreen, Inc. | Inhibitors of proteasomal activity and production for stimulating bone growth |
| EP0995757A3 (en) | 1998-08-26 | 2002-05-22 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Bivalent inhibitors of the proteasome |
| BR9914648A (pt) | 1998-10-20 | 2001-11-27 | Millennium Pharm Inc | Processo para monitorar ação medicamentosa deinibidor de proteasoma |
| EP1053750A1 (en) | 1999-04-22 | 2000-11-22 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Use of proteasome-inhibitor for the induction of programmed cell death (apoptosis) |
| BR0010134A (pt) | 1999-04-27 | 2002-01-15 | Novartis Ag | Uso de derivados de ácido 2,4-diamino-3-hidroxicarboxìlico como inibidores de proteassoma |
| SE9901573D0 (sv) | 1999-05-03 | 1999-05-03 | Astra Ab | New compounds |
| WO2001002424A2 (en) | 1999-07-07 | 2001-01-11 | Du Pont Pharmaceuticals Company | Peptide boronic acid inhibitors of hepatitis c virus protease |
| US7122627B2 (en) | 1999-07-26 | 2006-10-17 | Bristol-Myers Squibb Company | Lactam inhibitors of Hepatitis C virus NS3 protease |
| WO2001020995A1 (en) | 1999-09-23 | 2001-03-29 | Washington University | Compounds directed against pilus biogenesis and activity in pathogenic bacteria; methods and compositions for synthesis thereof |
| EP1477180A1 (en) | 1999-10-20 | 2004-11-17 | Osteoscreen, Inc. | Inhibitors of proteasomal activity for stimulating bone and hair growth |
| SK742003A3 (en) | 2000-07-21 | 2003-06-03 | Schering Corp | Novel peptides as NS3-serine protease inhibitors of hepatitis C virus |
| ATE338564T1 (de) | 2000-10-12 | 2006-09-15 | Viromics Gmbh | Proteasome inhibitoren zur behandlung von hepatitis-virus infektionen |
| JP4162491B2 (ja) | 2001-01-25 | 2008-10-08 | アメリカ合衆国 | ボロン酸化合物製剤 |
| KR20040002905A (ko) | 2001-04-09 | 2004-01-07 | 알란 크리스챤 쇼우 | 세포내 세균으로부터 단백질을 동정하는 방법 |
| US7214769B2 (en) | 2001-05-23 | 2007-05-08 | The Curators Of The University Of Missouri | Method for inverse solid phase synthesis of peptides |
| DE60209227T2 (de) | 2001-05-30 | 2006-08-17 | Novartis Ag | 2-((n-(2-amino-3-(heteroaryl- oder -aryl)propionyl)aminoacyl)amino)-alkylboronsäurederivate |
| AU2002324734A1 (en) | 2001-08-16 | 2003-03-03 | Levente Fabry-Asztalos | Borinic acid protease inhibitors |
| JPWO2003033507A1 (ja) | 2001-10-12 | 2005-02-03 | 杏林製薬株式会社 | ベンジルマロン酸誘導体およびそれを含有するプロテアソーム阻害薬 |
| JP4412586B2 (ja) | 2002-01-08 | 2010-02-10 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | エポネマイシンおよびエポキソマイシン類似物およびそれらの用途 |
| US7576206B2 (en) | 2003-08-14 | 2009-08-18 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| UA88771C2 (ru) * | 2003-08-14 | 2009-11-25 | Сефалон, Инк. | Ингибиторы протеасомы и способ их применения (варианты) |
| US7223745B2 (en) | 2003-08-14 | 2007-05-29 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| HRP20212002T1 (hr) | 2004-03-30 | 2022-04-01 | Millennium Pharmaceuticals, Inc. | Sinteza estera i spojeva borove kiseline |
| US7468383B2 (en) | 2005-02-11 | 2008-12-23 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| AU2007357338B2 (en) | 2007-08-06 | 2014-03-20 | Takeda Pharmaceutical Company Limited | Proteasome inhibitors |
| US7442830B1 (en) | 2007-08-06 | 2008-10-28 | Millenium Pharmaceuticals, Inc. | Proteasome inhibitors |
| EP2238973A1 (en) * | 2009-04-07 | 2010-10-13 | Cephalon France | Lyophilized preparations of proteasome inhibitors |
-
2010
- 2010-12-22 AU AU2010341530A patent/AU2010341530B2/en not_active Ceased
- 2010-12-22 CN CN201080058991.9A patent/CN102725300B/zh not_active Expired - Fee Related
- 2010-12-22 WO PCT/US2010/061695 patent/WO2011087822A1/en not_active Ceased
- 2010-12-22 EP EP10798930A patent/EP2516449A1/en not_active Withdrawn
- 2010-12-22 JP JP2012546173A patent/JP5783659B2/ja not_active Expired - Fee Related
- 2010-12-22 NZ NZ600786A patent/NZ600786A/en not_active IP Right Cessation
- 2010-12-22 MX MX2012007341A patent/MX2012007341A/es active IP Right Grant
- 2010-12-22 CA CA2785300A patent/CA2785300A1/en not_active Abandoned
-
2012
- 2012-06-05 IL IL220190A patent/IL220190A0/en not_active IP Right Cessation
- 2012-06-20 US US13/528,147 patent/US8541590B2/en not_active Expired - Fee Related
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013515082A5 (https=) | ||
| Kisselev et al. | The caspase-like sites of proteasomes, their substrate specificity, new inhibitors and substrates, and allosteric interactions with the trypsin-like sites | |
| Kisselev et al. | Proteasome inhibitors: an expanding army attacking a unique target | |
| Touchet et al. | Aminoboronic acids and esters: from synthetic challenges to the discovery of unique classes of enzyme inhibitors | |
| AU2004264422B2 (en) | Proteasome inhibitors and methods of using the same | |
| Stein et al. | Kinetic characterization of the chymotryptic activity of the 20S proteasome | |
| Groll et al. | Crystal structure of the 20 S proteasome: TMC-95A complex: a non-covalent proteasome inhibitor | |
| Milo Jr et al. | Chemical and biological evaluation of dipeptidyl boronic acid proteasome inhibitors for use in prodrugs and pro-soft drugs targeting solid tumors | |
| Walker et al. | Strategies for the inhibition of serine proteases | |
| Mirabella et al. | Specific cell-permeable inhibitor of proteasome trypsin-like sites selectively sensitizes myeloma cells to bortezomib and carfilzomib | |
| Gardner et al. | Characterization of peptidyl boronic acid inhibitors of mammalian 20 S and 26 S proteasomes and their inhibition of proteasomes in cultured cells | |
| Dorsey et al. | Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer | |
| Demuth | Recent developments in inhibiting cysteine and serine proteases | |
| Borissenko et al. | 20S proteasome and its inhibitors: crystallographic knowledge for drug development | |
| JP2007502302A5 (https=) | ||
| Adams et al. | Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids | |
| Akopian et al. | Cleavage specificity of Mycobacterium tuberculosis ClpP1P2 protease and identification of novel peptide substrates and boronate inhibitors with anti-bacterial activity | |
| Kisselev et al. | Proteasome active sites allosterically regulate each other, suggesting a cyclical bite-chew mechanism for protein breakdown | |
| LeBeau et al. | Potent and selective peptidyl boronic acid inhibitors of the serine protease prostate-specific antigen | |
| Klein et al. | Structure-based optimization and discovery of M3258, a specific inhibitor of the immunoproteasome subunit LMP7 (β5i) | |
| JP5783659B2 (ja) | プロテアソーム阻害剤およびその調製、精製および使用のための方法 | |
| JP2007502304A5 (https=) | ||
| Li et al. | Synthesis and evaluation of novel α-amino cyclic boronates as inhibitors of HCV NS3 protease | |
| Rydzewski et al. | Optimization of subsite binding to the β5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1, 3, 4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors | |
| Gaczynska et al. | Small-molecule inhibitors of proteasome activity |