PE20220935A1 - Quelantes macrociclicos y metodos de uso de estos - Google Patents
Quelantes macrociclicos y metodos de uso de estosInfo
- Publication number
- PE20220935A1 PE20220935A1 PE2021001868A PE2021001868A PE20220935A1 PE 20220935 A1 PE20220935 A1 PE 20220935A1 PE 2021001868 A PE2021001868 A PE 2021001868A PE 2021001868 A PE2021001868 A PE 2021001868A PE 20220935 A1 PE20220935 A1 PE 20220935A1
- Authority
- PE
- Peru
- Prior art keywords
- ring
- alkyl
- hydrogen
- independently
- chelator
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/025—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus inorganic Tc complexes or compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
- A61K51/0482—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group chelates from cyclic ligands, e.g. DOTA
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
- A61K51/10—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
- A61K51/1027—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody against receptors, cell-surface antigens or cell-surface determinants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
- A61K51/10—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
- A61K51/1093—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody conjugates with carriers being antibodies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Optics & Photonics (AREA)
- Epidemiology (AREA)
- Physics & Mathematics (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invencion se refiere a un compuesto quelante de formula (I), donde: cada uno del anillo A y el anillo B es independientemente un arilo de 6-10 miembros o un heteroarilo de 5-10 miembros, en donde cada uno del anillo A y el anillo B se sustituye opcionalmente con uno o mas sustituyentes seleccionados independientemente del grupo que consiste en halo, alquilo, entre otros; Z1 y Z2 son independientemente -(C(R12)2)m- o -(CH2)n-C(R12)(X)-(CH2)n-, donde X es -L1-R11, n es 0 a 5, m es 1 a 5, L1 esta ausente o es un enlazador, R11 es una entidad nucleofilica o una entidad electrofilica, R12 es hidrogeno, alquilo, cicloalquilo, entre otros; R14 a R17 son independientemente hidrogeno, alquilo, entre otros, o alternativamente R14 y R15 y/o R16 y R17 se toman juntos con los atomos de carbono a los cuales se acoplan para formar un anillo cicloalquilo de 5 o 6 miembros opcionalmente sustituido con X, siempre que el quelante comprenda al menos un X, y cuando X esta presente en el anillo A o anillo B, L1 es un enlazador o al menos uno de R12 y R14-R17 no es hidrogeno. Tambien se refiere a un complejo de radiometal de formula (I-m) que comprende un quelante unido a un ion de radiometal emisor alfa a traves de un enlace coordinado, donde M es un ion de radiometal, preferentemente un ion emisor alfa de actinio-225 (225Ac) y a un inmunoconjugado, donde el anticuerpo o fragmento de union al antigeno de este se une especificamente a un antigeno tumoral, el cual puede ser pertuzumab, cetuximab, panitumumab, entre otros. Tambien se refiere a una composicion farmaceutica y a un metodo de produccion. Los radioinmunoconjugados producidos mediante conjugacion del quelante de la invencion con un ligando dirigido son utiles en el tratamiento de una enfermedad o trastorno neoplasico, tal como el cancer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962846044P | 2019-05-10 | 2019-05-10 | |
| PCT/IB2020/054381 WO2020229974A1 (en) | 2019-05-10 | 2020-05-08 | Macrocyclic chelators and methods of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20220935A1 true PE20220935A1 (es) | 2022-05-31 |
Family
ID=70804855
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021001868A PE20220935A1 (es) | 2019-05-10 | 2020-05-08 | Quelantes macrociclicos y metodos de uso de estos |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US11576986B2 (es) |
| EP (1) | EP3966211A1 (es) |
| JP (2) | JP7734078B2 (es) |
| KR (1) | KR20220006613A (es) |
| CN (1) | CN114127059B (es) |
| AU (1) | AU2020273654A1 (es) |
| BR (1) | BR112021022237A2 (es) |
| CA (1) | CA3139806A1 (es) |
| CL (1) | CL2021002960A1 (es) |
| CO (1) | CO2021015713A2 (es) |
| CR (1) | CR20210556A (es) |
| DO (1) | DOP2021000233A (es) |
| EA (1) | EA202193076A1 (es) |
| EC (1) | ECSP21089217A (es) |
| IL (1) | IL287909A (es) |
| MA (1) | MA55885A (es) |
| MX (1) | MX2021013667A (es) |
| PE (1) | PE20220935A1 (es) |
| PH (1) | PH12021552791A1 (es) |
| SG (1) | SG11202112100PA (es) |
| UA (1) | UA129220C2 (es) |
| WO (1) | WO2020229974A1 (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3474903B1 (en) | 2016-06-23 | 2025-01-22 | Cornell University | Double targeted constructs to affect tumor kill |
| US10806806B2 (en) | 2016-06-23 | 2020-10-20 | Cornell University | Trifunctional constructs with tunable pharmacokinetics useful in imaging and anti-tumor therapies |
| EP3883610A4 (en) | 2018-11-20 | 2022-11-02 | Cornell University | MACROCYCLIC COMPLEXES OF RADIONUCLIDES AND THEIR USE IN CANCER RADIATION THERAPY |
| EA202193076A1 (ru) | 2019-05-10 | 2022-02-16 | Янссен Байотек, Инк. | Макроциклические хелаторы и способы их применения |
| HUE064465T2 (hu) | 2019-05-10 | 2024-04-28 | Deciphera Pharmaceuticals Llc | Heteroarilaminopirimidin amid autophagia inhibitorok és azok felhasználási eljárásai |
| SMT202300469T1 (it) | 2019-05-10 | 2024-01-10 | Deciphera Pharmaceuticals Llc | Inibitori dell'autofagia a base di fenilamminopirimidinammidi, e metodi di loro utilizzo |
| AU2020297422B2 (en) | 2019-06-17 | 2024-03-21 | Deciphera Pharmaceuticals, Llc | Aminopyrimidine amide autophagy inhibitors and methods of use thereof |
| WO2021250240A1 (en) * | 2020-06-12 | 2021-12-16 | Orano | Diaza-18-crown-6 derivative useful for chelating radium, conjugate and radium chelate comprising the same, and uses thereof |
| MX2023005462A (es) * | 2020-11-10 | 2023-05-22 | Janssen Biotech Inc | Compuestos macrociclicos y metodos para usarlos. |
| CA3205707A1 (en) | 2021-01-27 | 2022-08-04 | Fei Shen | Immunoconjugates comprising kallikrein related peptidase 2 antigen binding domains and their uses |
| EP4317152A4 (en) * | 2021-03-26 | 2025-03-26 | Nihon Medi-Physics Co., Ltd. | COMPOUND, METHOD FOR PRODUCING AND METHOD FOR STORING A COMPOUND, METHOD FOR PRODUCING A TARGETING AGENT AND COMPOSITION |
| WO2022211051A1 (ja) * | 2021-03-31 | 2022-10-06 | 日本メジフィジックス株式会社 | 抗egfr抗体の放射性複合体、及び、放射性医薬 |
| MX2023014069A (es) | 2021-05-27 | 2024-03-15 | Janssen Biotech Inc | Composiciones y métodos para el tratamiento del cáncer de próstata. |
| EP4380633A2 (en) * | 2021-08-02 | 2024-06-12 | Rayzebio, Inc. | Stabilized compositions of radionuclides and uses thereof |
| JP2024125438A (ja) * | 2021-08-03 | 2024-09-19 | 住友化学株式会社 | 放射性金属錯体及びその製造方法、並びに放射性金属捕捉剤 |
| AU2022333321A1 (en) | 2021-08-27 | 2024-04-11 | Janssen Biotech, Inc. | Anti-psma antibodies and uses thereof |
| JP2024532372A (ja) * | 2021-08-27 | 2024-09-05 | ヤンセン バイオテツク,インコーポレーテツド | 抗psma放射性コンジュゲート及びその使用 |
| US20250009917A1 (en) * | 2021-09-29 | 2025-01-09 | The University Of Melbourne | Macrocycle containing compounds and radiolabelled complexes thereof, as ligands in targeted radiotherapy applications |
| EP4429718A1 (en) * | 2021-11-09 | 2024-09-18 | Janssen Biotech, Inc. | Macrocyclic compounds and diagnostic uses thereof |
| EP4430040A1 (en) * | 2021-11-09 | 2024-09-18 | Janssen Biotech, Inc. | Macrocyclic compounds and methods of making the same |
| WO2023144723A1 (en) | 2022-01-26 | 2023-08-03 | Janssen Biotech, Inc. | Immunoconjugates comprising kallikrein related peptidase 2 antigen binding domains and their uses |
| JP2023135733A (ja) * | 2022-03-16 | 2023-09-29 | Jfeエンジニアリング株式会社 | ジルコニウム錯体およびその合成方法 |
| CN114656422B (zh) * | 2022-04-22 | 2023-05-23 | 重庆理工大学 | 一种新型氮杂冠醚化合物及其阳离子脂质体、制备方法与应用 |
| CN114874214B (zh) * | 2022-05-31 | 2023-03-21 | 南京航空航天大学 | 可偶联巯基的双功能大环螯合剂衍生物及其制备方法 |
| CN114949259B (zh) * | 2022-07-11 | 2023-09-19 | 重庆理工大学 | 一种氮杂冠醚结构的基因递送载体及其制备方法和应用 |
| WO2025072791A2 (en) | 2023-09-29 | 2025-04-03 | Aktis Oncology, Inc. | Miniproteins, conjugates & uses thereof |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1341373C (en) * | 1988-06-24 | 2002-07-02 | Roberta C. Cheng | Macrocyclic bifunctional chelants, complexes thereof and their antibody conjugates |
| AU4450100A (en) | 1999-03-23 | 2000-10-23 | United States Of America, Represented By The Secretary, Department Of Health And Human Services, The | 225Ac-heha and related compounds, methods of synthesis and methods of use |
| EP2595967B1 (en) | 2010-07-23 | 2016-03-23 | University Of Delaware | Tetrazine-trans-cyclooctene ligation for the rapid construction of radionuclide labeled probes |
| US10556024B2 (en) | 2013-11-13 | 2020-02-11 | Whitehead Institute For Biomedical Research | 18F labeling of proteins using sortases |
| CN105980404B (zh) | 2013-11-19 | 2021-01-12 | 弗雷达克斯有限责任公司 | 人源化抗激肽释放酶-2抗体 |
| PT3334744T (pt) | 2015-08-11 | 2020-07-28 | Galera Labs Llc | Complexos de anel penta-aza macrocíclico que possuem biodisponibilidade oral |
| EP4218833A1 (en) | 2015-10-01 | 2023-08-02 | Whitehead Institute for Biomedical Research | Labeling of antibodies |
| FR3045606B1 (fr) | 2015-12-18 | 2019-04-05 | Ecole Normale Superieure De Lyon | Complexes de lanthanide pour la cristallisation de macromolecules biologiques et la determination de leur structure cristallographique |
| TWI742074B (zh) | 2016-04-22 | 2021-10-11 | 瑞典商阿斯特捷利康公司 | Mcl-1抑制劑及其使用方法 |
| MX392700B (es) | 2016-08-10 | 2025-03-11 | Cancer Targeted Tech Llc | Inhibidores de antígeno de la membrana específico para la próstata (psma) quelados. |
| JP2018068834A (ja) * | 2016-11-01 | 2018-05-10 | オリンパス株式会社 | 走査型内視鏡および走査型内視鏡の製造方法 |
| AU2018243682B2 (en) | 2017-03-30 | 2023-11-09 | Cornell University | Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer |
| AU2018249559B2 (en) * | 2017-04-05 | 2025-04-17 | Cornell University | Trifunctional constructs with tunable pharmacokinetics useful in imaging and anti-tumor therapies |
| WO2019090242A1 (en) | 2017-11-04 | 2019-05-09 | Advanced Proteome Therapeutics Inc. | Composition and method for modifying polypeptides |
| JP2021506842A (ja) | 2017-12-18 | 2021-02-22 | ヤンセン バイオテツク,インコーポレーテツド | ポリペプチドの放射性標識 |
| PE20211916A1 (es) | 2018-05-24 | 2021-09-28 | Janssen Biotech Inc | Agentes aglutinantes del psma y usos de estos |
| EP3883610A4 (en) | 2018-11-20 | 2022-11-02 | Cornell University | MACROCYCLIC COMPLEXES OF RADIONUCLIDES AND THEIR USE IN CANCER RADIATION THERAPY |
| CN120393061A (zh) | 2018-12-03 | 2025-08-01 | 融合制药公司 | 放射性免疫缀合物与dna损伤和修复抑制剂组合疗法 |
| MX2021013657A (es) | 2019-05-10 | 2022-02-21 | Takeda Pharmaceuticals Co | Conjugados de anticuerpo y farmaco. |
| EA202193076A1 (ru) | 2019-05-10 | 2022-02-16 | Янссен Байотек, Инк. | Макроциклические хелаторы и способы их применения |
| MX2023005462A (es) | 2020-11-10 | 2023-05-22 | Janssen Biotech Inc | Compuestos macrociclicos y metodos para usarlos. |
| CA3205707A1 (en) | 2021-01-27 | 2022-08-04 | Fei Shen | Immunoconjugates comprising kallikrein related peptidase 2 antigen binding domains and their uses |
| EP4429718A1 (en) | 2021-11-09 | 2024-09-18 | Janssen Biotech, Inc. | Macrocyclic compounds and diagnostic uses thereof |
| EP4430040A1 (en) | 2021-11-09 | 2024-09-18 | Janssen Biotech, Inc. | Macrocyclic compounds and methods of making the same |
-
2020
- 2020-05-08 EA EA202193076A patent/EA202193076A1/ru unknown
- 2020-05-08 UA UAA202107060A patent/UA129220C2/uk unknown
- 2020-05-08 MA MA055885A patent/MA55885A/fr unknown
- 2020-05-08 EP EP20727846.6A patent/EP3966211A1/en active Pending
- 2020-05-08 JP JP2021566438A patent/JP7734078B2/ja active Active
- 2020-05-08 AU AU2020273654A patent/AU2020273654A1/en active Pending
- 2020-05-08 SG SG11202112100PA patent/SG11202112100PA/en unknown
- 2020-05-08 BR BR112021022237A patent/BR112021022237A2/pt unknown
- 2020-05-08 CN CN202080050202.0A patent/CN114127059B/zh active Active
- 2020-05-08 MX MX2021013667A patent/MX2021013667A/es unknown
- 2020-05-08 CA CA3139806A patent/CA3139806A1/en active Pending
- 2020-05-08 PE PE2021001868A patent/PE20220935A1/es unknown
- 2020-05-08 PH PH1/2021/552791A patent/PH12021552791A1/en unknown
- 2020-05-08 CR CR20210556A patent/CR20210556A/es unknown
- 2020-05-08 US US16/869,771 patent/US11576986B2/en active Active
- 2020-05-08 KR KR1020217040423A patent/KR20220006613A/ko active Pending
- 2020-05-08 WO PCT/IB2020/054381 patent/WO2020229974A1/en not_active Ceased
-
2021
- 2021-11-08 IL IL287909A patent/IL287909A/en unknown
- 2021-11-09 CL CL2021002960A patent/CL2021002960A1/es unknown
- 2021-11-10 DO DO2021000233A patent/DOP2021000233A/es unknown
- 2021-11-23 CO CONC2021/0015713A patent/CO2021015713A2/es unknown
- 2021-12-09 EC ECSENADI202189217A patent/ECSP21089217A/es unknown
-
2022
- 2022-06-30 US US17/810,316 patent/US12453785B2/en active Active
-
2025
- 2025-08-25 JP JP2025139342A patent/JP2025176045A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JP2025176045A (ja) | 2025-12-03 |
| MA55885A (fr) | 2022-03-16 |
| EP3966211A1 (en) | 2022-03-16 |
| IL287909A (en) | 2022-01-01 |
| CN114127059B (zh) | 2024-09-24 |
| JP2022532157A (ja) | 2022-07-13 |
| SG11202112100PA (en) | 2021-11-29 |
| CA3139806A1 (en) | 2020-11-19 |
| US11576986B2 (en) | 2023-02-14 |
| WO2020229974A1 (en) | 2020-11-19 |
| CO2021015713A2 (es) | 2021-11-30 |
| CR20210556A (es) | 2021-12-17 |
| AU2020273654A1 (en) | 2021-11-25 |
| ECSP21089217A (es) | 2022-01-31 |
| US12453785B2 (en) | 2025-10-28 |
| MX2021013667A (es) | 2022-01-31 |
| DOP2021000233A (es) | 2022-07-31 |
| US20200353105A1 (en) | 2020-11-12 |
| CN114127059A (zh) | 2022-03-01 |
| EA202193076A1 (ru) | 2022-02-16 |
| BR112021022237A2 (pt) | 2022-03-29 |
| UA129220C2 (uk) | 2025-02-12 |
| JP7734078B2 (ja) | 2025-09-04 |
| PH12021552791A1 (en) | 2022-09-05 |
| KR20220006613A (ko) | 2022-01-17 |
| US20230110178A1 (en) | 2023-04-13 |
| CL2021002960A1 (es) | 2022-06-24 |
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