PH12019550230A1 - Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation - Google Patents
Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparationInfo
- Publication number
- PH12019550230A1 PH12019550230A1 PH12019550230A PH12019550230A PH12019550230A1 PH 12019550230 A1 PH12019550230 A1 PH 12019550230A1 PH 12019550230 A PH12019550230 A PH 12019550230A PH 12019550230 A PH12019550230 A PH 12019550230A PH 12019550230 A1 PH12019550230 A1 PH 12019550230A1
- Authority
- PH
- Philippines
- Prior art keywords
- conjugates
- therapy
- useful
- preparation
- cryptophycin
- Prior art date
Links
- 229930188224 Cryptophycin Natural products 0.000 title abstract 3
- 108010006226 cryptophycin Proteins 0.000 title abstract 3
- PSNOPSMXOBPNNV-VVCTWANISA-N cryptophycin 1 Chemical compound C1=C(Cl)C(OC)=CC=C1C[C@@H]1C(=O)NC[C@@H](C)C(=O)O[C@@H](CC(C)C)C(=O)O[C@H]([C@H](C)[C@@H]2[C@H](O2)C=2C=CC=CC=2)C/C=C/C(=O)N1 PSNOPSMXOBPNNV-VVCTWANISA-N 0.000 title abstract 3
- PSNOPSMXOBPNNV-UHFFFAOYSA-N cryptophycin-327 Natural products C1=C(Cl)C(OC)=CC=C1CC1C(=O)NCC(C)C(=O)OC(CC(C)C)C(=O)OC(C(C)C2C(O2)C=2C=CC=CC=2)CC=CC(=O)N1 PSNOPSMXOBPNNV-UHFFFAOYSA-N 0.000 title abstract 3
- 238000002560 therapeutic procedure Methods 0.000 title 1
- 125000003636 chemical group Chemical group 0.000 abstract 2
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229920001184 polypeptide Polymers 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/15—Depsipeptides; Derivatives thereof
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
-
- 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
- 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
- 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
- A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
- A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
- A61K47/6817—Toxins
- A61K47/6829—Bacterial toxins, e.g. diphteria toxins or Pseudomonas exotoxin A
-
- 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
- A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K11/00—Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
- C07K5/06052—Val-amino acid
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Toxicology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Gastroenterology & Hepatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17305531 | 2017-05-10 | ||
| PCT/EP2018/061989 WO2018206635A1 (en) | 2017-05-10 | 2018-05-09 | Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PH12019550230A1 true PH12019550230A1 (en) | 2020-07-06 |
Family
ID=58873750
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PH12019550230A PH12019550230A1 (en) | 2017-05-10 | 2019-11-05 | Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation |
Country Status (21)
| Country | Link |
|---|---|
| US (5) | US20180369401A1 (https=) |
| EP (1) | EP3621658A1 (https=) |
| JP (2) | JP2020519610A (https=) |
| KR (1) | KR102722886B1 (https=) |
| CN (1) | CN110831633A (https=) |
| AR (1) | AR111781A1 (https=) |
| AU (2) | AU2018265333C1 (https=) |
| BR (1) | BR112019023336A2 (https=) |
| CA (1) | CA3062977A1 (https=) |
| CO (1) | CO2019012108A2 (https=) |
| EA (1) | EA201992667A1 (https=) |
| EC (1) | ECSP19078277A (https=) |
| IL (1) | IL270507B2 (https=) |
| MA (1) | MA50764A (https=) |
| MX (1) | MX2019013421A (https=) |
| MY (1) | MY204075A (https=) |
| PH (1) | PH12019550230A1 (https=) |
| TN (1) | TN2019000303A1 (https=) |
| TW (1) | TWI778059B (https=) |
| UY (1) | UY37728A (https=) |
| WO (1) | WO2018206635A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110366428B (zh) | 2016-12-30 | 2024-05-17 | Vaxcyte公司 | 具有非天然氨基酸的多肽-抗原缀合物 |
| US11951165B2 (en) | 2016-12-30 | 2024-04-09 | Vaxcyte, Inc. | Conjugated vaccine carrier proteins |
| TN2019000303A1 (en) | 2017-05-10 | 2021-05-07 | Sanofi Sa | Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation |
| CN111154133B (zh) * | 2020-01-03 | 2022-07-12 | 万华化学集团股份有限公司 | 一种环氧树脂发泡剂，环氧树脂组合物及环氧发泡材料的制备方法和用途 |
| CN114053426B (zh) * | 2020-07-30 | 2024-06-18 | 成都科岭源医药技术有限公司 | 一种双药链接组装单元及双药靶向接头-药物偶联物 |
| CN115105607B (zh) * | 2021-03-22 | 2024-12-20 | 成都科岭源医药技术有限公司 | 一种用于adc的双药-接头的制备方法及其用途 |
| KR20240150807A (ko) | 2022-02-22 | 2024-10-16 | 아라리스 바이오테크 아게 | 2개 이상의 페이로드를 포함하는 펩티드 링커 |
| CN115212315A (zh) * | 2022-08-03 | 2022-10-21 | 联宁（苏州）生物制药有限公司 | 一种抗体偶联药物中间体及含有其的抗体偶联药物 |
| WO2025082990A1 (en) | 2023-10-15 | 2025-04-24 | Araris Biotech Ag | Antibody-drug conjugates using two different types of topoisomerase i inhibitors |
| WO2026013234A1 (en) | 2024-07-10 | 2026-01-15 | Araris Biotech Ag | Triple-payload antibody-drug conjugates (adcs) |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4040907A (en) * | 1974-06-20 | 1977-08-09 | Syva Company | Iodothyronine enzyme conjugates |
| JPH09510436A (ja) | 1993-12-21 | 1997-10-21 | ユニバーシティー オブ ハワイ | 新規なクリプトフィシン類 |
| AU722492B2 (en) * | 1996-08-30 | 2000-08-03 | University Of Hawaii | Pharmaceutical compounds |
| US20020128185A1 (en) | 1998-02-25 | 2002-09-12 | Chuan Shih | Pharmaceutical compounds |
| US7230101B1 (en) | 2002-08-28 | 2007-06-12 | Gpc Biotech, Inc. | Synthesis of methotrexate-containing heterodimeric molecules |
| US20050175619A1 (en) | 2004-02-05 | 2005-08-11 | Robert Duffy | Methods of producing antibody conjugates |
| US8212083B2 (en) | 2006-04-27 | 2012-07-03 | Intezyne Technologies, Inc. | Heterobifunctional poly(ethylene glycol) containing acid-labile amino protecting groups and uses thereof |
| MX2009000709A (es) | 2006-07-18 | 2009-02-04 | Sanofi Aventis | Anticuerpo antagonista contra epha2 para el tratamiento de cancer. |
| CN101784565B (zh) * | 2007-06-25 | 2014-12-10 | 恩多塞特公司 | 含有亲水性间隔区接头的共轭物 |
| FR2947269B1 (fr) * | 2009-06-29 | 2013-01-18 | Sanofi Aventis | Nouveaux composes anticancereux |
| EP2451213B1 (en) | 2009-06-30 | 2017-03-01 | Alcatel Lucent | Roaming method for mobile terminal in wireless local area network, related access controller and access point device |
| UY32914A (es) | 2009-10-02 | 2011-04-29 | Sanofi Aventis | Anticuerpos que se usan específicamente al receptor epha2 |
| NZ758049A (en) | 2013-10-15 | 2024-03-22 | Seagen Inc | Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics |
| AU2014337317A1 (en) * | 2013-10-15 | 2016-09-15 | Sorrento Therapeutics Inc. | Drug-conjugates with a targeting molecule and two different drugs |
| EP3068443B1 (en) * | 2013-11-12 | 2019-04-10 | Centre for Probe Development and Commercialization | Residualizing linkers and uses thereof |
| WO2016065142A2 (en) | 2014-10-22 | 2016-04-28 | The Johns Hopkins University | New scaffolds and multifunctional intermediates for imaging psma and cancer therapy |
| CN113209306A (zh) * | 2014-12-09 | 2021-08-06 | 艾伯维公司 | 具有细胞渗透性的bcl-xl抑制剂的抗体药物缀合物 |
| KR20170139110A (ko) * | 2015-04-21 | 2017-12-18 | 애브비 스템센트알엑스 엘엘씨 | 칼리케아마이신 구성체 및 사용 방법 |
| TWI714661B (zh) | 2015-11-05 | 2021-01-01 | 法商賽諾菲公司 | 新穎念珠藻素化合物及接合物、其製備與其治療用途 |
| CN108066772B (zh) * | 2016-11-14 | 2021-07-13 | 中国科学院上海药物研究所 | 靶向tacstd2的抗体与药物偶联体(adc)分子 |
| TN2019000303A1 (en) | 2017-05-10 | 2021-05-07 | Sanofi Sa | Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation |
-
2018
- 2018-05-09 TN TNP/2019/000303A patent/TN2019000303A1/en unknown
- 2018-05-09 KR KR1020197035740A patent/KR102722886B1/ko active Active
- 2018-05-09 BR BR112019023336-9A patent/BR112019023336A2/pt unknown
- 2018-05-09 AU AU2018265333A patent/AU2018265333C1/en active Active
- 2018-05-09 EP EP18722557.8A patent/EP3621658A1/en active Pending
- 2018-05-09 AR ARP180101213A patent/AR111781A1/es not_active Application Discontinuation
- 2018-05-09 WO PCT/EP2018/061989 patent/WO2018206635A1/en not_active Ceased
- 2018-05-09 EA EA201992667A patent/EA201992667A1/ru unknown
- 2018-05-09 CN CN201880044816.0A patent/CN110831633A/zh active Pending
- 2018-05-09 JP JP2019561911A patent/JP2020519610A/ja active Pending
- 2018-05-09 CA CA3062977A patent/CA3062977A1/en active Pending
- 2018-05-09 MA MA050764A patent/MA50764A/fr unknown
- 2018-05-09 MY MYPI2019006354A patent/MY204075A/en unknown
- 2018-05-09 UY UY0001037728A patent/UY37728A/es not_active Application Discontinuation
- 2018-05-09 MX MX2019013421A patent/MX2019013421A/es unknown
- 2018-05-09 US US15/975,423 patent/US20180369401A1/en not_active Abandoned
- 2018-05-09 TW TW107115718A patent/TWI778059B/zh active
- 2018-05-09 US US16/612,090 patent/US20200093934A1/en active Pending
-
2019
- 2019-10-29 CO CONC2019/0012108A patent/CO2019012108A2/es unknown
- 2019-10-31 EC ECSENADI201978277A patent/ECSP19078277A/es unknown
- 2019-11-04 US US16/673,367 patent/US11007275B2/en active Active
- 2019-11-05 PH PH12019550230A patent/PH12019550230A1/en unknown
- 2019-11-07 IL IL270507A patent/IL270507B2/en unknown
-
2021
- 2021-03-23 US US17/210,072 patent/US11998611B2/en active Active
-
2022
- 2022-06-30 AU AU2022204711A patent/AU2022204711C1/en active Active
-
2023
- 2023-04-06 JP JP2023061810A patent/JP2023085475A/ja active Pending
-
2024
- 2024-04-10 US US18/631,600 patent/US20250205348A1/en active Pending
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