FI3154594T3 - Fap-aktivoituja terapeuttisia aineita ja niihin liittyviä käyttöjä - Google Patents
Fap-aktivoituja terapeuttisia aineita ja niihin liittyviä käyttöjä Download PDFInfo
- Publication number
- FI3154594T3 FI3154594T3 FIEP15807049.0T FI15807049T FI3154594T3 FI 3154594 T3 FI3154594 T3 FI 3154594T3 FI 15807049 T FI15807049 T FI 15807049T FI 3154594 T3 FI3154594 T3 FI 3154594T3
- Authority
- FI
- Finland
- Prior art keywords
- alkyl
- prodrug
- fap
- pharmaceutically acceptable
- group
- Prior art date
Links
- 239000003814 drug Substances 0.000 title 1
- 229940124597 therapeutic agent Drugs 0.000 title 1
- 239000000651 prodrug Substances 0.000 claims 9
- 229940002612 prodrug Drugs 0.000 claims 9
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 3
- -1 cyano, amino Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical compound 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
- 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
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder 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
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 108010040030 histidinoalanine Proteins 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000008194 pharmaceutical composition 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- 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)
Applications Claiming Priority (3)
| 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| FI3154594T3 true FI3154594T3 (fi) | 2023-08-07 |
Family
ID=54834485
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FIEP15807049.0T FI3154594T3 (fi) | 2014-06-13 | 2015-06-15 | Fap-aktivoituja terapeuttisia aineita ja niihin liittyviä käyttöjä |
Country Status (15)
| Country | Link |
|---|---|
| US (6) | US10245248B2 (enExample) |
| EP (2) | EP3154594B1 (enExample) |
| JP (4) | JP6744826B2 (enExample) |
| CN (4) | CN113786495A (enExample) |
| CA (1) | CA2952051C (enExample) |
| DK (1) | DK3154594T3 (enExample) |
| ES (1) | ES2951596T3 (enExample) |
| FI (1) | FI3154594T3 (enExample) |
| HR (1) | HRP20230854T1 (enExample) |
| HU (1) | HUE063194T2 (enExample) |
| IL (2) | IL249370B (enExample) |
| PL (1) | PL3154594T3 (enExample) |
| PT (1) | PT3154594T (enExample) |
| SI (1) | SI3154594T1 (enExample) |
| WO (1) | WO2015192123A1 (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113786495A (zh) * | 2014-06-13 | 2021-12-14 | 塔夫茨大学信托人 | Fap激活的治疗剂以及其相关用途 |
| US9737556B2 (en) | 2014-06-13 | 2017-08-22 | Trustees Of Tufts College | FAP-activated therapeutic agents, and uses related thereto |
| WO2017189569A1 (en) * | 2016-04-25 | 2017-11-02 | Trustees Of Tufts College | Multimediator dpp4 and fap inhibitors, and uses related thereto |
| MX2019004950A (es) | 2016-10-28 | 2019-09-26 | Icahn School Med Mount Sinai | Composiciones y metodos para tratar el cancer mediado por el potenciador del homologo zeste 2. |
| CA3045037A1 (en) | 2016-12-08 | 2018-06-14 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating cdk4/6-mediated cancer |
| 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 |
| ES2894106T3 (es) * | 2017-04-21 | 2022-02-11 | Safe Implant Tech Aps | Partículas de oro para su uso en la terapia para prevenir o reducir la contractura capsular |
| GB201710973D0 (en) | 2017-07-07 | 2017-08-23 | Avacta Life Sciences Ltd | Scaffold proteins |
| WO2019154859A1 (en) * | 2018-02-06 | 2019-08-15 | Universität Heidelberg | Fap inhibitor |
| JP2021515013A (ja) * | 2018-03-06 | 2021-06-17 | 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 | セリンスレオニンキナーゼ（ａｋｔ）分解／破壊化合物および使用方法 |
| 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 |
| WO2019236567A2 (en) * | 2018-06-04 | 2019-12-12 | Trustees Of Tufts College | Tumor microenvironment-activated drug-binder conjugated, and uses related thereto |
| WO2019246570A1 (en) | 2018-06-21 | 2019-12-26 | Icahn School Of Medicine At Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| AU2019360944B2 (en) * | 2018-10-17 | 2022-09-29 | Purdue Research Foundation | Fibroblast activation protein (FAP) targeted imaging and therapy in fibrosis |
| WO2020210337A1 (en) * | 2019-04-09 | 2020-10-15 | Dana-Farber Cancer Institute, Inc. | Degradation of akt by conjugation of atp-competitive akt inhibitor gdc-0068 with e3 ligase ligands and methods of use |
| CN118908962A (zh) | 2019-05-06 | 2024-11-08 | 西奈山伊坎医学院 | 作为hpk1的降解剂的异双功能化合物 |
| WO2021016392A1 (en) * | 2019-07-22 | 2021-01-28 | Purdue Research Foundation | Multivalent fibroblast-targeted agents and methods of use |
| JP7638664B2 (ja) | 2020-01-31 | 2025-03-04 | 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 |
| WO2022026729A1 (en) * | 2020-07-31 | 2022-02-03 | The Johns Hopkins University | Fap-activated compounds for treatment of cancer |
| KR20230141755A (ko) * | 2020-10-30 | 2023-10-10 | 아박타 라이프 사이언시스 리미티드 | 효소 활성화 혈청 반감기 연장된 치료 접합체 |
| WO2022094262A1 (en) * | 2020-10-30 | 2022-05-05 | Avacta Life Sciences Limited | Fap-activated serum extended half-life therapeutic conjugates |
| CN116981479A (zh) * | 2020-12-17 | 2023-10-31 | 塔夫茨大学信托人 | Fap激活的放射治疗诊断法以及与之相关的用途 |
| US20240238458A1 (en) * | 2021-03-16 | 2024-07-18 | 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 |
| CN120077031A (zh) | 2022-07-05 | 2025-05-30 | 亚历克斯·祖内克 | 用于多管齐下化疗的前药试剂盒 |
| EP4615521A1 (en) * | 2022-11-09 | 2025-09-17 | Purdue Research Foundation | Keto-amide-based fibroblast activation protein-targeted ligand linked to an imaging or therapeutic agent, compositions and methods of use |
| WO2025159301A1 (ko) * | 2024-01-24 | 2025-07-31 | 서울대학교산학협력단 | 섬유아세포 활성화 단백질에 의해 활성화되는 프로드러그 화합물 |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3719667A (en) | 1970-08-24 | 1973-03-06 | Lilly Co Eli | Epimerization of 6-acylamido and 6-imido penicillin sulfoxide esters |
| US3840556A (en) | 1971-05-28 | 1974-10-08 | Lilly Co Eli | Penicillin conversion by halogen electrophiles and anti-bacterials derived thereby |
| NO812612L (no) | 1980-08-06 | 1982-02-08 | Ferring Pharma Ltd | Enzym-inhibitorer. |
| US5433955A (en) | 1989-01-23 | 1995-07-18 | Akzo N.V. | Site specific in vivo activation of therapeutic drugs |
| AU643141B2 (en) | 1991-03-15 | 1993-11-04 | Amgen, Inc. | Pulmonary administration of granulocyte colony stimulating factor |
| GB9309663D0 (en) | 1993-05-11 | 1993-06-23 | Erba Carlo Spa | Biologically active compounds |
| US5451569A (en) | 1994-04-19 | 1995-09-19 | Hong Kong University Of Science And Technology R & D Corporation Limited | Pulmonary drug delivery system |
| US5767242A (en) | 1994-04-20 | 1998-06-16 | Boehringer Ingelheim Int'l Gmbh | Isolated dimeric fibroblast activation protein alpha, and uses thereof |
| TR200103406T2 (tr) | 1998-03-19 | 2002-06-21 | Vertex Pharmaceuticals Incorporated | Kaspaz inhibitörleri. |
| US6613879B1 (en) * | 1999-05-14 | 2003-09-02 | Boehringer Ingelheim Pharma Kg | FAP-activated anti-tumour compounds |
| EP1294404A2 (en) * | 2000-06-14 | 2003-03-26 | Corixa Corporation | Prodrug compounds with an oligopeptide having an isoleucine residue |
| US20030232742A1 (en) * | 2000-11-10 | 2003-12-18 | Stefan Peters | FAP-activated anti-tumor compounds |
| US20030055052A1 (en) | 2000-11-10 | 2003-03-20 | Stefan Peters | FAP-activated anti-tumor compounds |
| GB0027552D0 (en) * | 2000-11-10 | 2000-12-27 | Boehringer Ingelheim Pharma | Anti-tumor compounds |
| US20020155565A1 (en) | 2000-11-10 | 2002-10-24 | Pilar Garin-Chesa | FAP-activated anti-tumor compounds |
| EP1238678A1 (en) | 2001-03-08 | 2002-09-11 | Bayer Aktiengesellschaft | Enzyme-activated cytostatic conjugates with integrin ligands |
| JP4541693B2 (ja) | 2001-06-11 | 2010-09-08 | メダレックス，インコーポレイティド | Ｃｄ１０活性化プロドラッグ化合物 |
| EP1333033A1 (en) | 2002-01-30 | 2003-08-06 | Boehringer Ingelheim Pharma GmbH & Co.KG | FAP-activated anti-tumor compounds |
| AU2003233238A1 (en) | 2002-05-10 | 2003-11-11 | Boehringer Ingelheim Pharma Gmbh And Co Kg | Fap-activated anti-tumor prodrugs |
| US20040033957A1 (en) | 2002-05-10 | 2004-02-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | FAP-activated anti-tumor prodrugs |
| JP5064037B2 (ja) | 2004-02-23 | 2012-10-31 | ジェネンテック， インコーポレイテッド | 複素環式自壊的リンカーおよび結合体 |
| EP1812082B1 (en) * | 2004-10-21 | 2013-08-14 | IGF Oncology, LLC | Toxins and radionuclides coupled to IGF-1 receptor ligands for the treatment of cancer |
| US20100047170A1 (en) | 2006-01-05 | 2010-02-25 | Denmeade Samuel R | Peptide Prodrugs |
| WO2008011157A2 (en) | 2006-07-20 | 2008-01-24 | The General Hospital Corporation | Methods, compositions, and kits for the selective activation of protoxins through combinatorial targeting |
| WO2008116053A2 (en) | 2007-03-20 | 2008-09-25 | Trustees Of Tufts College | Fap-activated chemotherapeutic compounds, and methods of use thereof |
| CN108383893A (zh) | 2011-08-30 | 2018-08-10 | 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 |
| EP2827871A1 (de) | 2012-03-21 | 2015-01-28 | Bayer Intellectual Property GmbH | Verwendung von (rs)-s-cyclopropyl-s-(4-{[4-{[(1r, 2r)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluormethyl)pyrimidin-2-yl]amino}phenyl)sulfoximid zur behandlung spezifischer tumore |
| EP2908838A4 (en) | 2012-10-16 | 2016-12-21 | Inspyr Therapeutics Inc | INJECTABLE CANCER COMPOSITIONS |
| CA2890288A1 (en) | 2012-11-16 | 2014-05-22 | Merck Patent Gmbh | Novel heterocyclic derivatives as modulators of kinase activity |
| AU2013369261B2 (en) * | 2012-12-28 | 2018-08-09 | Cobiores Nv | Minimally toxic prodrugs |
| US9737556B2 (en) | 2014-06-13 | 2017-08-22 | Trustees Of Tufts College | FAP-activated therapeutic agents, and uses related thereto |
| CN113786495A (zh) | 2014-06-13 | 2021-12-14 | 塔夫茨大学信托人 | Fap激活的治疗剂以及其相关用途 |
| JP2017529853A (ja) | 2014-09-25 | 2017-10-12 | アムジエン・インコーポレーテツド | プロテアーゼにより活性化可能な二重特異性タンパク質 |
| WO2017173347A1 (en) | 2016-04-01 | 2017-10-05 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Par2 mimetic peptides and uses thereof |
| WO2017189569A1 (en) | 2016-04-25 | 2017-11-02 | Trustees Of Tufts College | Multimediator dpp4 and fap inhibitors, and uses related thereto |
-
2015
- 2015-06-15 CN CN202111061513.XA patent/CN113786495A/zh active Pending
- 2015-06-15 HU HUE15807049A patent/HUE063194T2/hu unknown
- 2015-06-15 HR HRP20230854TT patent/HRP20230854T1/hr unknown
- 2015-06-15 CN CN202111061534.1A patent/CN113967258B/zh active Active
- 2015-06-15 FI FIEP15807049.0T patent/FI3154594T3/fi active
- 2015-06-15 PL PL15807049.0T patent/PL3154594T3/pl unknown
- 2015-06-15 ES ES15807049T patent/ES2951596T3/es active Active
- 2015-06-15 WO PCT/US2015/035798 patent/WO2015192123A1/en not_active Ceased
- 2015-06-15 US US15/318,627 patent/US10245248B2/en active Active
- 2015-06-15 EP EP15807049.0A patent/EP3154594B1/en active Active
- 2015-06-15 CN CN202111061659.4A patent/CN113956325A/zh active Pending
- 2015-06-15 EP EP23185698.0A patent/EP4299134A3/en active Pending
- 2015-06-15 JP JP2016572687A patent/JP6744826B2/ja not_active Expired - Fee Related
- 2015-06-15 PT PT158070490T patent/PT3154594T/pt unknown
- 2015-06-15 CN CN201580043350.9A patent/CN106573073B/zh active Active
- 2015-06-15 DK DK15807049.0T patent/DK3154594T3/da active
- 2015-06-15 SI SI201531956T patent/SI3154594T1/sl unknown
- 2015-06-15 IL IL249370A patent/IL249370B/en unknown
- 2015-06-15 CA CA2952051A patent/CA2952051C/en active Active
- 2015-06-15 IL IL291922A patent/IL291922A/en unknown
-
2019
- 2019-02-13 US US16/274,387 patent/US11033525B2/en active Active
-
2020
- 2020-07-31 JP JP2020130483A patent/JP7093912B2/ja active Active
-
2021
- 2021-04-01 US US17/220,635 patent/US12121505B2/en active Active
- 2021-04-01 US US17/220,675 patent/US12023316B2/en active Active
- 2021-05-26 US US17/330,848 patent/US12053450B2/en active Active
-
2022
- 2022-05-27 JP JP2022086532A patent/JP7530111B2/ja active Active
-
2024
- 2024-07-19 JP JP2024115840A patent/JP2024150608A/ja active Pending
- 2024-09-09 US US18/828,942 patent/US20250108031A1/en active Pending
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| FI3154594T3 (fi) | Fap-aktivoituja terapeuttisia aineita ja niihin liittyviä käyttöjä | |
| ES2543007T3 (es) | Micropartículas que comprenden sales de dicetopiperazina para la administración de fármacos | |
| CL2018003577A1 (es) | Piridina substituida como inhibidor de dnmt1. | |
| CL2018003290A1 (es) | Amidas heterocíclicas útiles como moduladores de proteínas (divisional de solicitud cl 2850-2018). | |
| CL2009000394A1 (es) | Compuestos derivados de n-(1h-indazol-5-il)pirrolidin-3-carboxamida sustituida, inhibidores de erk; composicion farmaceutica; y su uso en el tratamiento del cancer. | |
| CL2009000882A1 (es) | Un compuesto n-(4-cloro-3-(piridin-2-il)fenil)-4-(2-hidroxi-2-metilpropilsulfonil)-2-metilbenzamida, inhibidor de la via de señalización hedgehog; composición farmacéutica que comprende a dicho compuesto; y su uso para tratar el cancer. | |
| CU20100200A7 (es) | Una composición farmacéutica que comprende n-(3,4-difluoro-2-4-iodofenilamino)-6-metoxifenil)-l-(2,3-dihidroxipropil)ciclopropano-l-sulfonamida, útil para el tratamiento y prevención del cáncer y de enfermedades inflamatorias | |
| SMT201300096B (it) | Inibitori di prolil idrossilasi | |
| PL410258A1 (pl) | Weterynaryjne doustne kompozycje przeciwpasożytnicze obejmujące działające systemowo substancje czynne, sposoby i zastosowania je obejmujące | |
| ES2422557T3 (es) | Compuestos y composiciones como moduladores de la ruta Hedgehog | |
| PH12015502628A1 (en) | Pyrazolopyrrolidine derivatives and their use in the treatment of disease | |
| AR107864A1 (es) | ÁCIDO 7a,11b-DIHIDROXI-6a-ETIL-5b-COLAN-24-OICO Y COMPOSICIONES FARMACÉUTICAS | |
| EA201001368A1 (ru) | Гетероциклические производные мочевины и способы их применения-211 | |
| AR067495A1 (es) | Composiciones farmaceuticas y procedimientode tratamientos de trastornos de ojo seco | |
| MX2015016344A (es) | Derivados de imidazo-pirrolidinona y su uso en el tratamiento de enfermedades. | |
| AR088195A1 (es) | Composiciones farmaceuticas de n-metil-2-[3-(e)-2-piridin-2-il-vinil)-1h-indazol-6-ilsulfanil]-benzamida | |
| EA201300342A1 (ru) | Производные изоксазола и их применение в качестве потенциирующих средств для метаботропных глутаматных рецепторов | |
| ECSP10010052A (es) | Formulaciones galenicas de alisquireno y valsartan | |
| EA201692542A1 (ru) | Индановые и индолиновые производные и их применение в качестве активаторов растворимой гуанилатциклазы | |
| MX2011008910A (es) | Derivados de azol sustituidos, composicion farmaceutica que comprende los derivados, y uso de los derivados para tratar enfermeda de parkinson. | |
| CY1119328T1 (el) | Αναστολεας ανοχης σε αναλγητικα | |
| AR096045A1 (es) | Composición farmacéutica y formulación para prevenir o tratar el síndrome de ojo seco | |
| CU20190029A7 (es) | Compuestos de aza-indazol útiles en lesiones de tendones y/o ligamentos | |
| EA201001859A1 (ru) | Гетероциклические производные мочевины и способы их применеия | |
| HRP20221356T1 (hr) | Nova alkilirajuća sredstva |