HRP20230854T1 - Fap-aktivirana terapeutska sredstva i s njima povezane uporabe - Google Patents
Fap-aktivirana terapeutska sredstva i s njima povezane uporabe Download PDFInfo
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- HRP20230854T1 HRP20230854T1 HRP20230854TT HRP20230854T HRP20230854T1 HR P20230854 T1 HRP20230854 T1 HR P20230854T1 HR P20230854T T HRP20230854T T HR P20230854TT HR P20230854 T HRP20230854 T HR P20230854T HR P20230854 T1 HRP20230854 T1 HR P20230854T1
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- alkyl
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- 239000003814 drug Substances 0.000 title claims 5
- 229940124597 therapeutic agent Drugs 0.000 title 1
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 6
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 239000000651 prodrug Substances 0.000 claims 4
- 229940002612 prodrug Drugs 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- -1 cyano, amino Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical group OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 claims 2
- 238000003776 cleavage reaction Methods 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 230000007017 scission Effects 0.000 claims 2
- 210000002536 stromal cell Anatomy 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 2
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- FRJIAZKQGSCKPQ-FSPLSTOPSA-N His-Ala Chemical group OC(=O)[C@H](C)NC(=O)[C@@H](N)CC1=CN=CN1 FRJIAZKQGSCKPQ-FSPLSTOPSA-N 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- ZYJKONDZYOWOHE-UHFFFAOYSA-N [4-amino-3-(hydroxymethyl)phenyl]methanol Chemical compound NC1=CC=C(CO)C=C1CO ZYJKONDZYOWOHE-UHFFFAOYSA-N 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000002950 fibroblast Anatomy 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 108010040030 histidinoalanine Proteins 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/69—Boron compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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- 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
- A61K47/54—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 an organic compound
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- 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
- A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- General Health & Medical Sciences (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Claims (9)
1. Predlijek predstavljen općom formulom
[image]
ili njegova farmaceutski prihvatljiva sol, pri čemu:
R1 predstavlja (C1-C10)alkil, (C1-C10)alkoksi, (C1-C10)alkil-C(O)-(C1-C10)alkil, (C3-C8)cikloalkil, (C3-C8)cikloalkil(C1 -C10)alkil, aril, aril(C1-C10)alkil, heteroaril ili heteroaril(C1-C10)alkil, pri čemu je bilo koji R1 izborno supstituiran s jednim ili više supstituenata neovisno odabranih iz skupine koju čine halo, hidroksi, karboksilat, cijano, amino, nitro i tio (-SH);
R2 predstavlja H ili (C1-C6)alkil;
R3 predstavlja (C1-C6)alkil;
R4 je odsutan ili predstavlja (C1-C6)alkil, -OH, -NH2 ili jedan ili dva halogena;
X predstavlja O ili S;
Cyt’ predstavlja antraciklinski dio; i
L predstavlja vezu ili -N(H)-L predstavlja samospaljivi linker koji se metabolizira nakon cijepanja FAP-a kako bi se oslobodio antraciklinski dio,
pri čemu se prolijek selektivno pretvara u aktivni antraciklin pomoću FAP+ stromalnih stanica.
2. Predlijek predstavljen općom formulom
[image]
ili njegova farmaceutski prihvatljiva sol, gdje:
R1 predstavlja heteroaril, izborno supstituiran s jednim ili više supstituenata neovisno odabranih između
skupina koju čine halo, hidroksi, karboksilat, cijano, amino, nitro i tio (-SH);
R2 predstavlja H ili (C1-C6)alkil;
R3 je metil;
R4 je odsutan;
X je O;
Cyt’ predstavlja antraciklinski dio; i
L predstavlja vezu ili -N(H)-L predstavlja samospaljivi linker koji se metabolizira nakon cijepanja FAP-a u oslobađanju antraciklinskog dijela,
pri čemu se prolijek selektivno pretvara u aktivni antraciklin pomoću FAP+ stromalnih stanica.
3. Predlijek prema bilo kojem od zahtjeva 1 ili 2, naznačen time, da je L samospaljivi linker koji sadrži heterocikl, po izboru gdje je samospaljivi linker odabran iz grupe koju čine His-Ala, p-aminobenziloksikarbonil (PA-BC), i 2,4-bis(hidroksimetil)anilin.
4. Predlijek predstavljen formulom:
[image]
5. Predlijek odabran iz skupine koju čine:
[image]
6. Predlijek prema zahtjevu 5 koji ima sljedeću strukturu:
[image]
7. Farmaceutski pripravak, sadrži predlijek prema bilo kojem od prethodnih zahtjeva, ili njegovu farmaceutski prihvatljivu sol; i farmaceutski prihvatljiv nosač.
8. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 6, ili njegova farmaceutski prihvatljiva sol, koji se koristi u postupku liječenja poremećaja naznačenog porastom fibroblastnog aktivacijskog proteina (FAP).
9. Spoj za upotrebu prema zahtjevu 8, poremećaj naznačen porastom FAP odabranog iz skupine koju čine rak, fibroza i upala.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462011989P | 2014-06-13 | 2014-06-13 | |
| US201462051033P | 2014-09-16 | 2014-09-16 | |
| PCT/US2015/035798 WO2015192123A1 (en) | 2014-06-13 | 2015-06-15 | Fap-activated therapeutic agents, and uses related thereto |
| EP15807049.0A EP3154594B1 (en) | 2014-06-13 | 2015-06-15 | Fap-activated therapeutic agents, and uses related thereto |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20230854T1 true HRP20230854T1 (hr) | 2023-11-10 |
Family
ID=54834485
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20230854TT HRP20230854T1 (hr) | 2014-06-13 | 2015-06-15 | Fap-aktivirana terapeutska sredstva i s njima povezane uporabe |
Country Status (15)
| Country | Link |
|---|---|
| US (5) | US10245248B2 (hr) |
| EP (2) | EP4299134A3 (hr) |
| JP (4) | JP6744826B2 (hr) |
| CN (4) | CN113967258B (hr) |
| CA (1) | CA2952051C (hr) |
| DK (1) | DK3154594T3 (hr) |
| ES (1) | ES2951596T3 (hr) |
| FI (1) | FI3154594T3 (hr) |
| HR (1) | HRP20230854T1 (hr) |
| HU (1) | HUE063194T2 (hr) |
| IL (2) | IL291922A (hr) |
| PL (1) | PL3154594T3 (hr) |
| PT (1) | PT3154594T (hr) |
| SI (1) | SI3154594T1 (hr) |
| WO (1) | WO2015192123A1 (hr) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9737556B2 (en) | 2014-06-13 | 2017-08-22 | Trustees Of Tufts College | FAP-activated therapeutic agents, and uses related thereto |
| HRP20230854T1 (hr) | 2014-06-13 | 2023-11-10 | Bach Biosciences, Llc | Fap-aktivirana terapeutska sredstva i s njima povezane uporabe |
| WO2017189569A1 (en) * | 2016-04-25 | 2017-11-02 | Trustees Of Tufts College | Multimediator dpp4 and fap inhibitors, and uses related thereto |
| EP3532464A4 (en) | 2016-10-28 | 2020-07-08 | Icahn School of Medicine at Mount Sinai | COMPOSITIONS AND METHODS FOR TREATING EZH2-MEDIATED CANCER |
| JP2020514252A (ja) | 2016-12-08 | 2020-05-21 | アイカーン スクール オブ メディスン アット マウント シナイ | Ｃｄｋ４／６媒介性がんを治療するための組成物および方法 |
| ES2972577T3 (es) | 2016-12-14 | 2024-06-13 | Purdue Research Foundation | Formación de imágenes y terapia dirigidas a la proteína de activación de fibroblastos (FAP) |
| EP3391914B1 (en) * | 2017-04-21 | 2021-07-14 | Safe Implant Technology ApS | Gold particles for use in therapy to prevent or reduce capsular contracture |
| WO2019154859A1 (en) * | 2018-02-06 | 2019-08-15 | Universität Heidelberg | Fap inhibitor |
| WO2019173516A1 (en) | 2018-03-06 | 2019-09-12 | Icahn School Of Medicine At Mount Sinai | Serine threonine kinase (akt) degradation / disruption compounds and methods of use |
| CN108864250A (zh) * | 2018-05-29 | 2018-11-23 | 北京大学 | 一种FAPα酶敏感的吉西他滨前体药物及其制备方法和应用 |
| IL311536A (en) * | 2018-06-04 | 2024-05-01 | Tufts College | Binder-drug conjugates activated in the microenvironment and their related uses |
| US12110295B2 (en) | 2018-06-21 | 2024-10-08 | Icahn School Of Medicine At Mount Sinai | WD40 repeat domain protein 5 (WDR5) degradation/disruption compounds and methods of use |
| US11426472B2 (en) | 2018-10-17 | 2022-08-30 | Purdue Research Foundation | Fibroblast activation protein (FAP) targeted imaging and therapy in fibrosis |
| JP2022526979A (ja) * | 2019-04-09 | 2022-05-27 | ダナ－ファーバー キャンサー インスティテュート，インコーポレイテッド | Ａｔｐ競合性ａｋｔ阻害剤ｇｄｃ－００６８とｅ３リガーゼリガンドとの結合によるａｋｔの分解および使用方法 |
| JP2022542560A (ja) * | 2019-07-22 | 2022-10-05 | パーデュー・リサーチ・ファウンデーション | 線維芽細胞を標的とする多価作用物質、および使用方法 |
| WO2021153362A1 (ja) | 2020-01-31 | 2021-08-05 | キヤノン株式会社 | 光電変換装置、光電変換システム、および移動体 |
| CN111233955B (zh) * | 2020-02-28 | 2022-06-10 | 南京缘聚医药科技有限公司 | 一类噻唑酮甲酰胞嘧啶衍生物及其药物用途 |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| US20230331694A1 (en) * | 2020-07-31 | 2023-10-19 | The Johns Hopkins University | Fap-activated compounds for treatment of cancer |
| KR20230141754A (ko) * | 2020-10-30 | 2023-10-10 | 아박타 라이프 사이언시스 리미티드 | Fap-활성화 혈청 반감기 연장된 치료 접합체 |
| CA3201844A1 (en) * | 2020-12-17 | 2022-06-23 | William W. Bachovchin | Fap-activated radiotheranostics, and uses related thereto |
| EP4308110A1 (en) * | 2021-03-16 | 2024-01-24 | Purdue Research Foundation | Compounds targeting fibroblast-activation protein and methods of use thereof |
| CN113018450B (zh) * | 2021-05-24 | 2021-08-06 | 潍坊中医药产业技术研究院 | 一种具有肿瘤细胞和肿瘤相关成纤维细胞双靶向功能的药物载体、制备方法及应用 |
| CN113845563B (zh) * | 2021-09-28 | 2024-02-20 | 遵义医药高等专科学校 | 一种FAPα酶激活式鬼臼毒素衍生物及其制备方法与应用 |
| WO2024008833A1 (en) | 2022-07-05 | 2024-01-11 | Alex Zounek | Prodrug kit for multi-pronged chemotherapy |
| WO2024102956A1 (en) * | 2022-11-09 | 2024-05-16 | Purdue Research Foundation | Keto-amide-based fibroblast activation protein-targeted ligand linked to an imaging or therapeutic agent, compositions and methods of use |
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