JP2004529118A - インテグリンリガンドを有する酵素活性化細胞分裂停止接合体 - Google Patents
インテグリンリガンドを有する酵素活性化細胞分裂停止接合体 Download PDFInfo
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- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical compound C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 description 1
- 125000000612 phthaloyl group Chemical group C(C=1C(C(=O)*)=CC=CC1)(=O)* 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920002223 polystyrene Polymers 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- CAEWJEXPFKNBQL-UHFFFAOYSA-N prop-2-enyl carbonochloridate Chemical compound ClC(=O)OCC=C CAEWJEXPFKNBQL-UHFFFAOYSA-N 0.000 description 1
- 125000004368 propenyl group Chemical group C(=CC)* 0.000 description 1
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 description 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000006308 propyl amino group Chemical group 0.000 description 1
- 125000004673 propylcarbonyl group Chemical group 0.000 description 1
- 125000004742 propyloxycarbonyl group Chemical group 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 150000003242 quaternary ammonium salts Chemical class 0.000 description 1
- WYROLENTHWJFLR-ACLDMZEESA-N queuine Chemical compound C1=2C(=O)NC(N)=NC=2NC=C1CN[C@H]1C=C[C@H](O)[C@@H]1O WYROLENTHWJFLR-ACLDMZEESA-N 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
- 239000000376 reactant Substances 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- BOLDJAUMGUJJKM-LSDHHAIUSA-N renifolin D Natural products CC(=C)[C@@H]1Cc2c(O)c(O)ccc2[C@H]1CC(=O)c3ccc(O)cc3O BOLDJAUMGUJJKM-LSDHHAIUSA-N 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 238000007142 ring opening reaction Methods 0.000 description 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
- 229960001860 salicylate Drugs 0.000 description 1
- DUIOPKIIICUYRZ-UHFFFAOYSA-N semicarbazide Chemical compound NNC(N)=O DUIOPKIIICUYRZ-UHFFFAOYSA-N 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- QDRKDTQENPPHOJ-UHFFFAOYSA-N sodium ethoxide Chemical compound [Na+].CC[O-] QDRKDTQENPPHOJ-UHFFFAOYSA-N 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 238000000527 sonication Methods 0.000 description 1
- 210000000130 stem cell Anatomy 0.000 description 1
- 201000011549 stomach cancer Diseases 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 238000000967 suction filtration Methods 0.000 description 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 description 1
- 229940124530 sulfonamide Drugs 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- 150000003461 sulfonyl halides Chemical class 0.000 description 1
- 230000006103 sulfonylation Effects 0.000 description 1
- 238000005694 sulfonylation reaction Methods 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- MTEOSPVWMLTGFN-UHFFFAOYSA-N tert-butyl 2,5-dioxo-1,3-oxazolidine-3-carboxylate Chemical compound CC(C)(C)OC(=O)N1CC(=O)OC1=O MTEOSPVWMLTGFN-UHFFFAOYSA-N 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 150000003527 tetrahydropyrans Chemical group 0.000 description 1
- RAOIDOHSFRTOEL-UHFFFAOYSA-N tetrahydrothiophene Chemical group C1CCSC1 RAOIDOHSFRTOEL-UHFFFAOYSA-N 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 150000003585 thioureas Chemical class 0.000 description 1
- 229910052718 tin Inorganic materials 0.000 description 1
- 229960001479 tosylchloramide sodium Drugs 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- 102000035160 transmembrane proteins Human genes 0.000 description 1
- 108091005703 transmembrane proteins Proteins 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- DBGVGMSCBYYSLD-UHFFFAOYSA-N tributylstannane Chemical compound CCCC[SnH](CCCC)CCCC DBGVGMSCBYYSLD-UHFFFAOYSA-N 0.000 description 1
- 210000000689 upper leg Anatomy 0.000 description 1
- 150000003672 ureas Chemical class 0.000 description 1
- 125000002114 valyl group Chemical group 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 125000005023 xylyl group Chemical group 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
- A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01105350A EP1238678A1 (en) | 2001-03-08 | 2001-03-08 | Enzyme-activated cytostatic conjugates with integrin ligands |
| PCT/EP2002/002501 WO2002072151A1 (en) | 2001-03-08 | 2002-03-07 | Enzyme-activated cytostatic conjugates with integrin ligands |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004529118A true JP2004529118A (ja) | 2004-09-24 |
| JP2004529118A5 JP2004529118A5 (https=) | 2005-12-22 |
Family
ID=8176682
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002571109A Pending JP2004529118A (ja) | 2001-03-08 | 2002-03-07 | インテグリンリガンドを有する酵素活性化細胞分裂停止接合体 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US7304037B2 (https=) |
| EP (2) | EP1238678A1 (https=) |
| JP (1) | JP2004529118A (https=) |
| CA (1) | CA2439897A1 (https=) |
| WO (1) | WO2002072151A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2022506299A (ja) * | 2018-11-05 | 2022-01-17 | バイエル ファーマ アクチェンゲゼルシャフト | インテグリンリガンドを有する新規な細胞増殖抑制コンジュゲート |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102453036B (zh) * | 2010-10-27 | 2015-12-02 | 李红玉 | 一种喜树碱类化合物及其制备方法和在农药中的用途 |
| US9737556B2 (en) | 2014-06-13 | 2017-08-22 | Trustees Of Tufts College | FAP-activated therapeutic agents, and uses related thereto |
| CN106573073B (zh) | 2014-06-13 | 2021-09-28 | 塔夫茨大学信托人 | Fap激活的治疗剂以及其相关用途 |
| CN109575051B (zh) * | 2019-01-23 | 2021-07-27 | 遵义医科大学 | 一种天然药物成分修饰衍生物及其抗肿瘤应用 |
| US20230293716A1 (en) | 2020-05-08 | 2023-09-21 | Bolt Biotherapeutics, Inc. | Elastase-substrate, peptide linker immunoconjugates, and uses thereof |
| WO2023057813A1 (en) | 2021-10-04 | 2023-04-13 | Vincerx Pharma Gmbh | Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorders |
| WO2023057814A1 (en) | 2021-10-04 | 2023-04-13 | Vincerx Pharma Gmbh | Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorders |
| WO2023057812A1 (en) | 2021-10-04 | 2023-04-13 | Vincerx Pharma Gmbh | Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorder |
| JP2025537882A (ja) | 2022-11-17 | 2025-11-20 | ハンス-ゲオルク レルケン | 腫瘍微小環境において切断可能な小分子-薬物コンジュゲート |
| GB202407865D0 (en) | 2024-06-03 | 2024-07-17 | Elasmogen Ltd | Self immolative compounds |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3611194A1 (de) | 1986-04-04 | 1987-10-08 | Bayer Ag | Cancerostatisches mittel |
| GB8705477D0 (en) | 1987-03-09 | 1987-04-15 | Carlton Med Prod | Drug delivery systems |
| US4975278A (en) | 1988-02-26 | 1990-12-04 | Bristol-Myers Company | Antibody-enzyme conjugates in combination with prodrugs for the delivery of cytotoxic agents to tumor cells |
| US4980343A (en) | 1988-10-27 | 1990-12-25 | Bayer Aktiengesellschaft | Aminooxodihydroisoindoloquinazoline carcinostatic agents |
| CA2076982A1 (en) | 1990-12-27 | 1992-06-28 | Akira Okura | Pyridonecarboxylic acid derivatives |
| US5561116A (en) * | 1991-04-11 | 1996-10-01 | Kabushiki Kaisha Hayashibara Seibutsu Kagaku Kenkyujo | Solid product containing propolis components, and preparation and uses thereof |
| FR2676058B1 (fr) | 1991-04-30 | 1994-02-25 | Hoechst Lab | Prodrogues glycosylees, leur procede de preparation et leur utilisation dans le traitement des cancers. |
| DE4120646A1 (de) | 1991-06-22 | 1992-12-24 | Bayer Ag | 7-isoindolinyl-chinolon- und naphthyridoncarbonsaeure-derivate |
| DE4229903A1 (de) | 1992-09-08 | 1994-03-10 | Bayer Ag | Neue Acetale von Ketophosphamid und Alkylglycosiden |
| DE4236237A1 (de) | 1992-10-27 | 1994-04-28 | Behringwerke Ag | Prodrugs, ihre Herstellung und Verwendung als Arzneimittel |
| US5646159A (en) | 1994-07-20 | 1997-07-08 | Research Triangle Institute | Water-soluble esters of camptothecin compounds |
| DE19512484A1 (de) | 1995-04-04 | 1996-10-17 | Bayer Ag | Kohlenhydratmodifizierte Cytostatika |
| CA2265484C (en) * | 1996-09-10 | 2008-12-02 | The Burnham Institute | Tumor homing molecules, conjugates derived therefrom, and methods of using same |
| ID23424A (id) | 1997-05-14 | 2000-04-20 | Bayer Ag | Glikokonjugat dari 20(s)-kamptotesin |
| JP2002510709A (ja) * | 1998-04-08 | 2002-04-09 | ジー・ディー・サール・アンド・カンパニー | 二重Avb3及び転移関連受容体リガンド |
| US6291503B1 (en) | 1999-01-15 | 2001-09-18 | Bayer Aktiengesellschaft | β-phenylalanine derivatives as integrin antagonists |
| CA2370245A1 (en) * | 1999-05-14 | 2000-11-23 | Boehringer Ingelheim Pharmaceuticals, Inc. | Enzyme-activated anti-tumor prodrug compounds |
| ATE438413T1 (de) * | 1999-09-08 | 2009-08-15 | Markus Albers | Integrin-vermittelte arzneimittel-zielrichtung |
-
2001
- 2001-03-08 EP EP01105350A patent/EP1238678A1/en not_active Withdrawn
-
2002
- 2002-03-07 EP EP20020702402 patent/EP1372732A1/en not_active Withdrawn
- 2002-03-07 WO PCT/EP2002/002501 patent/WO2002072151A1/en not_active Ceased
- 2002-03-07 JP JP2002571109A patent/JP2004529118A/ja active Pending
- 2002-03-07 CA CA002439897A patent/CA2439897A1/en not_active Abandoned
- 2002-03-08 US US10/096,120 patent/US7304037B2/en not_active Expired - Fee Related
-
2007
- 2007-12-04 US US11/999,445 patent/US20080108576A1/en not_active Abandoned
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2022506299A (ja) * | 2018-11-05 | 2022-01-17 | バイエル ファーマ アクチェンゲゼルシャフト | インテグリンリガンドを有する新規な細胞増殖抑制コンジュゲート |
| JP7509768B2 (ja) | 2018-11-05 | 2024-07-02 | バイエル ファーマ アクチェンゲゼルシャフト | インテグリンリガンドを有する新規な細胞増殖抑制コンジュゲート |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1238678A1 (en) | 2002-09-11 |
| WO2002072151A1 (en) | 2002-09-19 |
| US20080108576A1 (en) | 2008-05-08 |
| EP1372732A1 (en) | 2004-01-02 |
| CA2439897A1 (en) | 2002-09-19 |
| US7304037B2 (en) | 2007-12-04 |
| US20020193311A1 (en) | 2002-12-19 |
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