JP2005525315A5 - - Google Patents
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- Publication number
- JP2005525315A5 JP2005525315A5 JP2003560001A JP2003560001A JP2005525315A5 JP 2005525315 A5 JP2005525315 A5 JP 2005525315A5 JP 2003560001 A JP2003560001 A JP 2003560001A JP 2003560001 A JP2003560001 A JP 2003560001A JP 2005525315 A5 JP2005525315 A5 JP 2005525315A5
- Authority
- JP
- Japan
- Prior art keywords
- moiety
- compound
- aryl
- heteroaryl
- heteroalicyclic
- 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
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 79
- 229910052739 hydrogen Inorganic materials 0.000 claims description 65
- 239000001257 hydrogen Substances 0.000 claims description 65
- 150000002431 hydrogen Chemical group 0.000 claims description 49
- 125000002723 alicyclic group Chemical group 0.000 claims description 38
- 125000001931 aliphatic group Chemical group 0.000 claims description 38
- 125000005418 aryl aryl group Chemical group 0.000 claims description 37
- 229910052736 halogen Inorganic materials 0.000 claims description 10
- 150000002367 halogens Chemical class 0.000 claims description 10
- 125000006239 protecting group Chemical group 0.000 claims description 10
- 229910052760 oxygen Inorganic materials 0.000 claims description 7
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 3
- 125000004122 cyclic group Chemical group 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 126
- 125000003118 aryl group Chemical group 0.000 claims 31
- 125000000217 alkyl group Chemical group 0.000 claims 27
- 239000000651 prodrug Substances 0.000 claims 16
- 229940002612 prodrugs Drugs 0.000 claims 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 15
- QVGXLLKOCUKJST-UHFFFAOYSA-N oxygen atom Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 15
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 13
- -1 OR C Chemical class 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- ZOXJGFHDIHLPTG-UHFFFAOYSA-N boron Chemical compound [B] ZOXJGFHDIHLPTG-UHFFFAOYSA-N 0.000 claims 4
- 229910052796 boron Inorganic materials 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 238000010647 peptide synthesis reaction Methods 0.000 claims 4
- 125000005024 alkenyl aryl group Chemical group 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000002877 alkyl aryl group Chemical group 0.000 claims 3
- 125000005025 alkynylaryl group Chemical group 0.000 claims 3
- 230000001093 anti-cancer Effects 0.000 claims 2
- 230000003110 anti-inflammatory Effects 0.000 claims 2
- 230000001028 anti-proliferant Effects 0.000 claims 2
- 125000005099 aryl alkyl carbonyl group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 239000004593 Epoxy Substances 0.000 claims 1
- 206010017758 Gastric cancer Diseases 0.000 claims 1
- 206010024324 Leukaemias Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010025310 Other lymphomas Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 125000002015 acyclic group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000003275 alpha amino acid group Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000003700 epoxy group Chemical group 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 125000004001 thioalkyl group Chemical group 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 0 *C(C1)*1C(*C*1CC1)C(C(C1)C2C(C3)C13C1CCCC1)C2C1*CCC1 Chemical compound *C(C1)*1C(*C*1CC1)C(C(C1)C2C(C3)C13C1CCCC1)C2C1*CCC1 0.000 description 5
- FOQJHZPURACERJ-UHFFFAOYSA-N CB1OC(C)(C)C(C)(C)O1 Chemical compound CB1OC(C)(C)C(C)(C)O1 FOQJHZPURACERJ-UHFFFAOYSA-N 0.000 description 1
- HQDKMMCQUXZGNG-UHFFFAOYSA-N CNNC1Cc2ccccc2CC1 Chemical compound CNNC1Cc2ccccc2CC1 HQDKMMCQUXZGNG-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34671102P | 2002-01-08 | 2002-01-08 | |
| US37301102P | 2002-04-16 | 2002-04-16 | |
| PCT/US2003/000390 WO2003059898A2 (en) | 2002-01-08 | 2003-01-08 | Eponemycin and epoxomicin analogs and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005525315A JP2005525315A (ja) | 2005-08-25 |
| JP2005525315A5 true JP2005525315A5 (US20100280075A1-20101104-C00054.png) | 2006-02-23 |
| JP4412586B2 JP4412586B2 (ja) | 2010-02-10 |
Family
ID=26994981
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003560001A Expired - Fee Related JP4412586B2 (ja) | 2002-01-08 | 2003-01-08 | 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 |
Country Status (6)
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7223745B2 (en) | 2003-08-14 | 2007-05-29 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| US7576206B2 (en) | 2003-08-14 | 2009-08-18 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| 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 |
| CN102174076A (zh) | 2004-04-15 | 2011-09-07 | 普罗特奥里克斯公司 | 用于抑制蛋白酶体酶的化合物 |
| DK2030981T3 (da) | 2004-05-10 | 2014-10-13 | Onyx Therapeutics Inc | Forbindelser til proteasom-enzymhæmning |
| DK1819353T3 (da) * | 2004-12-07 | 2011-05-16 | Proteolix Inc | Sammensætning til proteasomhæmning |
| US7468383B2 (en) * | 2005-02-11 | 2008-12-23 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| JP5229897B2 (ja) * | 2005-07-05 | 2013-07-03 | タフツ ユニバーシティー／トラスティーズ オブ タフツ カレッジ | 線維芽細胞活性化タンパクα阻害剤 |
| PL1948678T3 (pl) | 2005-11-09 | 2013-09-30 | Onyx Therapeutics Inc | Związki do hamowania enzymów |
| WO2007097980A2 (en) * | 2006-02-16 | 2007-08-30 | Sma Foundation | Ubiquitin/proteasome inhibitors for the treatment of spinal muscular atrophy |
| DK2041158T3 (da) | 2006-06-19 | 2013-06-24 | Onyx Therapeutics Inc | Peptid-epoxidketoner til proteasom inhibering |
| US7642369B2 (en) * | 2006-09-12 | 2010-01-05 | University Of Kentucky Research Foundation | Epoxyketone-based immunoproteasome inhibitors |
| WO2008063513A2 (en) * | 2006-11-13 | 2008-05-29 | Trustees Of Columbia University In The City Of New York | Selective proteasome inhibitors for treating diabetes |
| US7442830B1 (en) * | 2007-08-06 | 2008-10-28 | Millenium Pharmaceuticals, Inc. | Proteasome inhibitors |
| WO2009026579A1 (en) * | 2007-08-23 | 2009-02-26 | Cornell Research Foundation, Inc. | Proteasome inhibitors and their use in treating pathogen infection and cancer |
| KR20150131405A (ko) | 2007-10-04 | 2015-11-24 | 오닉스 세라퓨틱스, 인크. | 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성 |
| CA2704473C (en) * | 2007-11-06 | 2016-10-04 | Edison Pharmaceuticals, Inc. | 4-(p-quinonyl)-2-hydroxybutanamide derivatives for treatment of mitochondrial diseases |
| EP2088205A1 (en) | 2008-02-11 | 2009-08-12 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | PSMB10: A diagnosis marker and therapeutic target of chronic rejection. |
| KR101690571B1 (ko) | 2008-06-17 | 2016-12-28 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 보로네이트 에스테르 화합물 및 이의 제약학적 조성물 |
| CN101638414B (zh) * | 2008-07-30 | 2014-01-08 | 江苏先声药物研究有限公司 | 肽硼酸及其酯类化合物、制备方法及其用途 |
| 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. |
| EP2349313A4 (en) | 2008-10-21 | 2012-08-29 | Onyx Therapeutics Inc | COMBINATION THERAPY WITH EPOXYCLETON PEPTIDES |
| AR075899A1 (es) | 2009-03-20 | 2011-05-04 | Onyx Therapeutics Inc | Tripeptidos epoxicetonas cristalinos inhibidores de proteasa |
| JP2012527474A (ja) | 2009-05-22 | 2012-11-08 | エクセリクシス， インク． | 増殖性疾患に対するベンゾキサゼピンベースのｐｉ３ｋ／ｍｔ０ｒ阻害剤 |
| US8853147B2 (en) | 2009-11-13 | 2014-10-07 | Onyx Therapeutics, Inc. | Use of peptide epoxyketones for metastasis suppression |
| AU2010341530B2 (en) | 2009-12-22 | 2016-03-10 | Cephalon, Inc. | Proteasome inhibitors and processes for their preparation, purification and use |
| MX2012010017A (es) | 2010-03-01 | 2012-10-01 | Onyx Therapeutics Inc | Compuestos de para la inhibicion de inmunoproteasomas. |
| CN102892291A (zh) | 2010-03-31 | 2013-01-23 | 米伦纽姆医药公司 | 1-氨基-2-环丙基乙硼酸衍生物 |
| CN102946729B (zh) | 2010-04-07 | 2014-11-05 | 欧尼斯治疗公司 | 结晶肽环氧酮免疫蛋白酶体抑制剂 |
| US9126997B1 (en) | 2010-09-07 | 2015-09-08 | Northwestern University | Synergistic effect of glucocorticoid receptor agonists in combination with proteosome inhibitors for treating leukemia and myeloma |
| US20140105921A1 (en) | 2012-07-09 | 2014-04-17 | Onyx Therapeutics, Inc. | Prodrugs of Peptide Epoxy Ketone Protease Inhibitors |
| WO2014072985A1 (en) * | 2012-11-06 | 2014-05-15 | Natco Pharma Limited | Novel boronic acid derivatives as anti cancer agents |
| KR102481856B1 (ko) | 2014-05-20 | 2022-12-26 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 일차 암 치료법 후 사용하기 위한 붕소-함유 프로테아좀 저해제 |
| JP6749923B2 (ja) * | 2015-02-02 | 2020-09-02 | ザ リージェンツ オブ ザ ユニバーシティー オブ ミシガン | グルコシルセラミドシンターゼ阻害剤及びそれを使用した治療方法 |
| 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 |
| EP3781561B1 (en) | 2018-04-18 | 2024-03-13 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| US11919912B2 (en) | 2018-05-21 | 2024-03-05 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| 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 (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4912133A (en) | 1988-03-07 | 1990-03-27 | Bristol-Myers Company | BU-3862T antitumor antibiotic |
| US5071957A (en) * | 1989-08-04 | 1991-12-10 | Bristol-Myers Company | Antibiotic BU-4061T |
| US4990448A (en) | 1989-08-04 | 1991-02-05 | Bristol-Myers Company | Bu-4061T |
| JP3107326B2 (ja) | 1992-04-13 | 2000-11-06 | 日本化薬株式会社 | 生理活性物質ｎｋ−０４０００ｐ、ｎｋ−０４０００ｑ、その製造法及びそれを有効成分として含有する除草剤 |
| US5693617A (en) * | 1994-03-15 | 1997-12-02 | Proscript, Inc. | Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein |
| US6083903A (en) | 1994-10-28 | 2000-07-04 | Leukosite, Inc. | Boronic ester and acid compounds, synthesis and uses |
| ATE317850T1 (de) | 2001-05-30 | 2006-03-15 | Novartis Pharma Gmbh | 2-((n-(2-amino-3-(heteroaryl- oder - aryl)propionyl)aminoacyl)amino)- alkylboronsäurederivate |
| WO2003033506A1 (fr) | 2001-10-12 | 2003-04-24 | Kyorin Pharmaceutical Co., Ltd. | Derive d'acide d'aminoborane et medicament inhibiteur de proteasomes le contenant |
-
2003
- 2003-01-08 AU AU2003219652A patent/AU2003219652A1/en not_active Abandoned
- 2003-01-08 EP EP03715921A patent/EP1463719A2/en not_active Withdrawn
- 2003-01-08 US US10/501,120 patent/US7524883B2/en not_active Expired - Fee Related
- 2003-01-08 WO PCT/US2003/000390 patent/WO2003059898A2/en active Application Filing
- 2003-01-08 JP JP2003560001A patent/JP4412586B2/ja not_active Expired - Fee Related
- 2003-05-30 TW TW092114803A patent/TW200412349A/zh unknown
-
2009
- 2009-03-03 US US12/396,849 patent/US20090291998A1/en not_active Abandoned
