JP2010523477A5 - - Google Patents
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- Publication number
- JP2010523477A5 JP2010523477A5 JP2009554735A JP2009554735A JP2010523477A5 JP 2010523477 A5 JP2010523477 A5 JP 2010523477A5 JP 2009554735 A JP2009554735 A JP 2009554735A JP 2009554735 A JP2009554735 A JP 2009554735A JP 2010523477 A5 JP2010523477 A5 JP 2010523477A5
- Authority
- JP
- Japan
- Prior art keywords
- carbonyl
- amino acid
- aryl
- side chain
- arylamino
- 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.)
- Abandoned
Links
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 36
- -1 5-tetrazolyl Chemical group 0.000 claims 15
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 125000001691 aryl alkyl amino group Chemical group 0.000 claims 12
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 12
- 125000001769 aryl amino group Chemical group 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000004104 aryloxy group Chemical group 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 11
- 125000003282 alkyl amino group Chemical group 0.000 claims 10
- 239000003112 inhibitor Substances 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 9
- 150000001413 amino acids Chemical class 0.000 claims 9
- 125000003710 aryl alkyl group Chemical group 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000002252 acyl group Chemical group 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 8
- 150000008574 D-amino acids Chemical group 0.000 claims 6
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 6
- 125000004414 alkyl thio group Chemical group 0.000 claims 6
- 125000004659 aryl alkyl thio group Chemical group 0.000 claims 6
- 125000005110 aryl thio group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- DYMRYCZRMAHYKE-UHFFFAOYSA-N n-diazonitramide Chemical compound [O-][N+](=O)N=[N+]=[N-] DYMRYCZRMAHYKE-UHFFFAOYSA-N 0.000 claims 6
- 125000006239 protecting group Chemical group 0.000 claims 6
- 125000004469 siloxy group Chemical group [SiH3]O* 0.000 claims 6
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 6
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 150000008575 L-amino acids Chemical group 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 241000283690 Bos taurus Species 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 241000282472 Canis lupus familiaris Species 0.000 claims 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 241000283086 Equidae Species 0.000 claims 1
- 241000282326 Felis catus Species 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000008999 Giant Cell Carcinoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 241001494479 Pecora Species 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 241000283984 Rodentia Species 0.000 claims 1
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 1
- 241000282887 Suidae Species 0.000 claims 1
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims 1
- 206010006007 bone sarcoma Diseases 0.000 claims 1
- 125000001589 carboacyl group Chemical group 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 230000000762 glandular Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 201000000014 lung giant cell carcinoma Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 CCCCN([C@](C)*)C(C(C)(*)NN)=* Chemical compound CCCCN([C@](C)*)C(C(C)(*)NN)=* 0.000 description 3
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US89578707P | 2007-03-20 | 2007-03-20 | |
| PCT/US2008/057636 WO2008116054A1 (en) | 2007-03-20 | 2008-03-20 | Inhibitors of fibroblast activation protein, and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010523477A JP2010523477A (ja) | 2010-07-15 |
| JP2010523477A5 true JP2010523477A5 (enExample) | 2011-05-12 |
Family
ID=39766448
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009554735A Abandoned JP2010523477A (ja) | 2007-03-20 | 2008-03-20 | 線維芽細胞活性化タンパク質の阻害剤、およびそれを使用する方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20100105753A1 (enExample) |
| EP (1) | EP2139337A4 (enExample) |
| JP (1) | JP2010523477A (enExample) |
| AU (1) | AU2008228863A1 (enExample) |
| CA (1) | CA2681351A1 (enExample) |
| WO (1) | WO2008116054A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120053222A1 (en) * | 2009-01-23 | 2012-03-01 | Mark Gorrell | Novel Metabolic Disease Therapy |
| WO2012082672A2 (en) * | 2010-12-14 | 2012-06-21 | Merck Sharp & Dohme Corp. | Process and intermediates for preparing macrolactams |
| JP6207509B2 (ja) * | 2011-08-30 | 2017-10-04 | トラスティーズ オブ タフツ カレッジ | 固形腫瘍を治療するためのｆａｐ活性化プロテアソーム阻害剤 |
| AU2012340887A1 (en) | 2011-11-22 | 2014-07-03 | Trustees Of Tufts College | Small molecule enhancer for dendritic cell cancer vaccines |
| US20200237936A1 (en) | 2016-12-14 | 2020-07-30 | Purdue Research Foundation | Fibroblast activation protein (fap)-targeted imaging and therapy |
| EP3763726A1 (en) | 2019-07-08 | 2021-01-13 | 3B Pharmaceuticals GmbH | Compounds comprising a fibroblast activation protein ligand and use thereof |
| KR20220032078A (ko) | 2019-07-08 | 2022-03-15 | 쓰리비 파마슈티컬스 게엠베하 | 섬유모세포 활성화 단백질 리간드를 포함하는 화합물 및 그의 용도 |
| EP3997103B9 (en) | 2019-07-08 | 2025-02-26 | 3B Pharmaceuticals GmbH | Compounds comprising a fibroblast activation protein ligand and use thereof |
| EP4147053B1 (en) | 2020-05-07 | 2026-01-28 | Institut Curie | Antxr1 as a biomarker of immunosuppressive fibroblast populations and its use for predicting response to immunotherapy |
| EP4050018A1 (en) | 2021-01-07 | 2022-08-31 | 3B Pharmaceuticals GmbH | Compounds comprising a fibroblast activation protein ligand and use thereof |
| JP2024503637A (ja) | 2021-01-07 | 2024-01-26 | ３ベー ファーマシューティカルズ ゲーエムベーハー | 線維芽細胞活性化タンパク質リガンドを含む化合物およびその使用 |
| CN114316136B (zh) * | 2022-01-13 | 2023-01-31 | 西华师范大学 | 一种氢键增强型水合物抑制剂及其制备方法 |
| KR20250057810A (ko) * | 2022-08-25 | 2025-04-29 | 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 | 섬유아세포 활성화 단백질 알파-절단가능 프로-펩티드 및 사용 방법 |
| AU2024334645A1 (en) | 2023-08-31 | 2026-02-26 | Stichting Radboud Universitair Medisch Centrum | Endometriosis tracer |
| US20250186630A1 (en) | 2023-12-12 | 2025-06-12 | Viewpoint Molecular Targeting, Inc. | Fibroblast activation protein targeting peptides |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1520582A3 (en) * | 1998-02-02 | 2009-07-01 | Trustees Of Tufts College | Use of dipeptidylpetidase inhibitors to regulate glucose metabolism |
| US6890904B1 (en) * | 1999-05-25 | 2005-05-10 | Point Therapeutics, Inc. | Anti-tumor agents |
| US7041696B2 (en) * | 2002-06-17 | 2006-05-09 | The Procter & Gamble Company | Interleukin-1β converting enzyme inhibitors |
| KR20150003157A (ko) * | 2005-12-19 | 2015-01-08 | 트러스티즈 오브 터프츠 칼리지 | 소프트 단백질분해효소 억제자 및 이의 프로-소프트 폼 |
-
2008
- 2008-03-20 EP EP08732547A patent/EP2139337A4/en not_active Withdrawn
- 2008-03-20 US US12/532,274 patent/US20100105753A1/en not_active Abandoned
- 2008-03-20 AU AU2008228863A patent/AU2008228863A1/en not_active Abandoned
- 2008-03-20 JP JP2009554735A patent/JP2010523477A/ja not_active Abandoned
- 2008-03-20 CA CA002681351A patent/CA2681351A1/en not_active Abandoned
- 2008-03-20 WO PCT/US2008/057636 patent/WO2008116054A1/en not_active Ceased
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