JP2009500423A5 - - Google Patents
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- Publication number
- JP2009500423A5 JP2009500423A5 JP2008520373A JP2008520373A JP2009500423A5 JP 2009500423 A5 JP2009500423 A5 JP 2009500423A5 JP 2008520373 A JP2008520373 A JP 2008520373A JP 2008520373 A JP2008520373 A JP 2008520373A JP 2009500423 A5 JP2009500423 A5 JP 2009500423A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- group
- alkyl
- compound according
- aralkyl
- 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
- 150000001875 compounds Chemical class 0.000 claims 54
- 125000000217 alkyl group Chemical group 0.000 claims 19
- 125000002252 acyl group Chemical group 0.000 claims 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims 8
- -1 2-phenylethylcarbonyl Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 4
- 229910052796 boron Inorganic materials 0.000 claims 4
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 4
- 125000004452 carbocyclyl group Chemical group 0.000 claims 4
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000004001 thioalkyl group Chemical group 0.000 claims 3
- ZOXJGFHDIHLPTG-UHFFFAOYSA-N Boron Chemical group [B] ZOXJGFHDIHLPTG-UHFFFAOYSA-N 0.000 claims 2
- 201000009030 Carcinoma Diseases 0.000 claims 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 2
- 125000000612 phthaloyl group Chemical group C(C=1C(C(=O)*)=CC=CC1)(=O)* 0.000 claims 2
- YQTCQNIPQMJNTI-UHFFFAOYSA-N 2,2-dimethylpropan-1-one Chemical group CC(C)(C)[C]=O YQTCQNIPQMJNTI-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000032383 Soft tissue cancer Diseases 0.000 claims 1
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 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
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 1
- 125000005412 pyrazyl group Chemical group 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US69677205P | 2005-07-05 | 2005-07-05 | |
| US60/696,772 | 2005-07-05 | ||
| PCT/US2006/026258 WO2007005991A1 (en) | 2005-07-05 | 2006-07-05 | Inhibitors of fibroblast activation protein alpha |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012033777A Division JP2012140439A (ja) | 2005-07-05 | 2012-02-20 | 線維芽細胞活性化タンパクα阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009500423A JP2009500423A (ja) | 2009-01-08 |
| JP2009500423A5 true JP2009500423A5 (enExample) | 2010-08-26 |
| JP5229897B2 JP5229897B2 (ja) | 2013-07-03 |
Family
ID=37604810
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008520373A Expired - Fee Related JP5229897B2 (ja) | 2005-07-05 | 2006-07-05 | 線維芽細胞活性化タンパクα阻害剤 |
| JP2012033777A Pending JP2012140439A (ja) | 2005-07-05 | 2012-02-20 | 線維芽細胞活性化タンパクα阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012033777A Pending JP2012140439A (ja) | 2005-07-05 | 2012-02-20 | 線維芽細胞活性化タンパクα阻害剤 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US7998997B2 (enExample) |
| EP (1) | EP1898899A4 (enExample) |
| JP (2) | JP5229897B2 (enExample) |
| KR (1) | KR20080030079A (enExample) |
| CN (1) | CN101247799B (enExample) |
| AU (1) | AU2006264305B2 (enExample) |
| BR (1) | BRPI0612607A2 (enExample) |
| CA (1) | CA2613795A1 (enExample) |
| IL (2) | IL188327A0 (enExample) |
| MX (1) | MX2008000318A (enExample) |
| NO (1) | NO20080626L (enExample) |
| WO (1) | WO2007005991A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006125227A2 (en) * | 2005-05-19 | 2006-11-23 | Genentech, Inc. | Fibroblast activation protein inhibitor compounds and methods |
| EP1760076A1 (en) * | 2005-09-02 | 2007-03-07 | Ferring B.V. | FAP Inhibitors |
| EP2527347A1 (en) | 2007-08-06 | 2012-11-28 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
| US7442830B1 (en) | 2007-08-06 | 2008-10-28 | Millenium Pharmaceuticals, Inc. | Proteasome inhibitors |
| US7838673B2 (en) | 2007-10-16 | 2010-11-23 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
| EP2212334B1 (en) * | 2007-10-16 | 2012-08-15 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
| SG194349A1 (en) | 2008-06-17 | 2013-11-29 | Millennium Pharm Inc | Boronate ester compounds and pharmaceutical compositions thereof |
| 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. |
| SG184222A1 (en) | 2010-03-31 | 2012-10-30 | Millennium Pharm Inc | Derivatives of 1-amino-2-cyclopropylethylboronic acid |
| CN103945856A (zh) * | 2011-08-30 | 2014-07-23 | 塔夫茨大学信托人 | 用于治疗实体瘤的fap-活化的蛋白酶体抑制剂 |
| CN104039952A (zh) * | 2011-11-22 | 2014-09-10 | 塔夫茨大学信托人 | 用于树突状细胞癌症疫苗的小分子增强剂 |
| WO2014022636A1 (en) * | 2012-08-02 | 2014-02-06 | Trustees Of Tufts College | Broad spectrum inhibitors of the post proline cleaving enzymes for treatment of hepatitis c virus infections |
| SG10202003693RA (en) | 2014-05-20 | 2020-05-28 | Millennium Pharm Inc | Boron-containing proteasome inhibitors for use after primary cancer therapy |
| CZ2014527A3 (cs) | 2014-08-05 | 2016-02-17 | Ústav Organické Chemie A Biochemie Akademie Věd Čr, V.V.I. | Způsob detekce aktivní formy analytů ve vzorku a stanovení schopnosti dalších látek vázat se do aktivních míst těchto analytů |
| MA41505A (fr) | 2015-02-11 | 2017-12-19 | Millennium Pharm Inc | Nouvelle forme cristalline d'un inhibiteur de protéasome |
| WO2016171446A1 (ko) * | 2015-04-20 | 2016-10-27 | 동아에스티 주식회사 | 펩타이드 붕소산 화합물을 함유하는 안정화 약학 제제 |
| 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 |
| JP6223508B2 (ja) * | 2016-06-27 | 2017-11-01 | 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． | プロテアソーム阻害剤 |
| CN110291401B (zh) | 2016-12-14 | 2023-04-11 | 普渡研究基金会 | 成纤维细胞活化蛋白(fap)-靶向成像和治疗 |
| EP3565560B1 (en) | 2017-01-09 | 2024-05-29 | OnkosXcel Therapeutics, LLC | Predictive and diagnostic methods for prostate cancer |
| CN108929340B (zh) * | 2017-05-22 | 2019-12-13 | 北京大学 | 脯氨酸硼酸类化合物及其制备方法和用途 |
| WO2019154859A1 (en) * | 2018-02-06 | 2019-08-15 | Universität Heidelberg | Fap inhibitor |
| CN115697413B (zh) * | 2020-03-24 | 2025-08-01 | 塔夫茨大学信托人 | 靶向fap的放射性药物和显像剂以及与之相关的用途 |
| JP2024511054A (ja) * | 2021-03-24 | 2024-03-12 | トラスティーズ オブ タフツ カレッジ | ボロン酸化合物、組成物および方法 |
| CN118955616B (zh) * | 2024-05-01 | 2025-09-02 | 杭州景嘉航生物医药科技有限公司 | 一种靶向结合成纤维细胞活化蛋白化合物及应用 |
| CN119390720B (zh) * | 2024-12-31 | 2025-04-01 | 杭州景嘉航生物医药科技有限公司 | 一种靶向结合成纤维细胞活化蛋白的双环[1.1.1]戊烷类化合物及其应用 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US497A (en) * | 1837-12-01 | Improvement in the machine for preparing ice for shipping and storing | ||
| US4935493A (en) * | 1987-10-06 | 1990-06-19 | E. I. Du Pont De Nemours And Company | Protease inhibitors |
| US4963655A (en) * | 1988-05-27 | 1990-10-16 | Mayo Foundation For Medical Education And Research | Boron analogs of amino acid/peptide protease 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 |
| EP1463719A2 (en) * | 2002-01-08 | 2004-10-06 | Eisai Co., Ltd | Eponemycin and epoxomicin analogs and uses thereof |
| WO2003092605A2 (en) * | 2002-04-30 | 2003-11-13 | Trustees Of Tufts College | Protease inhibitors |
| US20050084490A1 (en) * | 2002-07-09 | 2005-04-21 | Point Therapeutics, Inc. | Boroproline compound combination therapy |
| AU2003297612A1 (en) * | 2002-12-02 | 2004-06-23 | Gilead Sciences, Inc. | 2-substituted-3-propenamide derivatives and methods of using the same |
| US7576206B2 (en) * | 2003-08-14 | 2009-08-18 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| DK1689757T3 (en) * | 2003-11-12 | 2014-12-08 | Sino Med Internat Alliance Inc | HETEROCYCLIC DRY ACID COMPOUNDS |
| WO2006125227A2 (en) * | 2005-05-19 | 2006-11-23 | Genentech, Inc. | Fibroblast activation protein inhibitor compounds and methods |
-
2006
- 2006-07-05 EP EP06786415A patent/EP1898899A4/en not_active Withdrawn
- 2006-07-05 AU AU2006264305A patent/AU2006264305B2/en not_active Ceased
- 2006-07-05 JP JP2008520373A patent/JP5229897B2/ja not_active Expired - Fee Related
- 2006-07-05 BR BRPI0612607-3A patent/BRPI0612607A2/pt not_active Application Discontinuation
- 2006-07-05 MX MX2008000318A patent/MX2008000318A/es active IP Right Grant
- 2006-07-05 KR KR1020087002781A patent/KR20080030079A/ko not_active Ceased
- 2006-07-05 US US11/994,707 patent/US7998997B2/en not_active Expired - Fee Related
- 2006-07-05 WO PCT/US2006/026258 patent/WO2007005991A1/en not_active Ceased
- 2006-07-05 CN CN2006800307719A patent/CN101247799B/zh not_active Expired - Fee Related
- 2006-07-05 CA CA002613795A patent/CA2613795A1/en not_active Abandoned
-
2007
- 2007-12-20 IL IL188327A patent/IL188327A0/en unknown
-
2008
- 2008-02-04 NO NO20080626A patent/NO20080626L/no not_active Application Discontinuation
-
2011
- 2011-07-06 US US13/177,268 patent/US20120077779A1/en not_active Abandoned
-
2012
- 2012-01-17 IL IL217579A patent/IL217579A/en not_active IP Right Cessation
- 2012-02-20 JP JP2012033777A patent/JP2012140439A/ja active Pending