EA202191244A1 - Новые цитостатические конъюгаты с лигандами интегрина - Google Patents

Новые цитостатические конъюгаты с лигандами интегрина

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Publication number
EA202191244A1
EA202191244A1 EA202191244A EA202191244A EA202191244A1 EA 202191244 A1 EA202191244 A1 EA 202191244A1 EA 202191244 A EA202191244 A EA 202191244A EA 202191244 A EA202191244 A EA 202191244A EA 202191244 A1 EA202191244 A1 EA 202191244A1
Authority
EA
Eurasian Patent Office
Prior art keywords
conjugates
integrin ligands
new cytostatic
new
cytostatic
Prior art date
Application number
EA202191244A
Other languages
English (en)
Inventor
Ханс-Георг Лерхен
Беатрикс Стелте-Людвиг
Шарлотте Кристине КОПИТЦ
Original Assignee
Байер Фарма Акциенгезельшафт
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Байер Фарма Акциенгезельшафт filed Critical Байер Фарма Акциенгезельшафт
Publication of EA202191244A1 publication Critical patent/EA202191244A1/ru

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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
    • A61K47/65—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
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K47/545—Heterocyclic compounds
    • 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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings

Abstract

Настоящее изобретение относится к новым фармацевтическим соединениям, состоящим из антагониста v3 интегрина, связывающего звена, состоящего из L-Val-L-Pro-L-Asp, расщепляемого эластазой, полиэтиленгликолевого (PEG) спейсера и цитотоксического элемента, к способам их получения, к их применению для лечения, предупреждения или контроля заболеваний и состояний, в том числе гиперпролиферативных нарушений, таких как рак, у людей и других млекопитающих.
EA202191244A 2018-11-05 2019-10-30 Новые цитостатические конъюгаты с лигандами интегрина EA202191244A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP18204423 2018-11-05
PCT/EP2019/079601 WO2020094471A1 (en) 2018-11-05 2019-10-30 Cytostatic conjugates with integrin ligands

Publications (1)

Publication Number Publication Date
EA202191244A1 true EA202191244A1 (ru) 2021-10-11

Family

ID=64453279

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202191244A EA202191244A1 (ru) 2018-11-05 2019-10-30 Новые цитостатические конъюгаты с лигандами интегрина

Country Status (16)

Country Link
US (1) US20210386864A1 (ru)
EP (1) EP3876993A1 (ru)
JP (1) JP2022506299A (ru)
KR (1) KR20210100607A (ru)
CN (1) CN113260382A (ru)
AR (1) AR116999A1 (ru)
AU (1) AU2019376293A1 (ru)
BR (1) BR112021008232A2 (ru)
CA (1) CA3118041A1 (ru)
CL (1) CL2021001142A1 (ru)
EA (1) EA202191244A1 (ru)
IL (1) IL282748A (ru)
MX (1) MX2021005134A (ru)
SG (1) SG11202104491SA (ru)
TW (1) TW202039005A (ru)
WO (1) WO2020094471A1 (ru)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20180020225A (ko) 2015-06-23 2018-02-27 바이엘 파마 악티엔게젤샤프트 Ksp 억제제의 표적화된 접합체
JP7022707B2 (ja) 2016-06-15 2022-02-18 バイエル・ファルマ・アクティエンゲゼルシャフト Ｋｓｐ阻害剤および抗ｃｄ１２３抗体を含む特異的抗体－薬物－コンジュゲート（ａｄｃ）
WO2018114578A1 (de) 2016-12-21 2018-06-28 Bayer Pharma Aktiengesellschaft Binder-wirkstoff-konjugate (adcs) mit enzymatisch spaltbaren gruppen
CA3047522A1 (en) 2016-12-21 2018-06-28 Bayer Pharma Aktiengesellschaft Specific antibody drug conjugates (adcs) having ksp inhibitors
WO2023057814A1 (en) 2021-10-04 2023-04-13 Vincerx Pharma Gmbh Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorders
WO2023057813A1 (en) 2021-10-04 2023-04-13 Vincerx Pharma Gmbh Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorders
WO2023057812A1 (en) 2021-10-04 2023-04-13 Vincerx Pharma Gmbh Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorder

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8705477D0 (en) 1987-03-09 1987-04-15 Carlton Med Prod Drug delivery systems
US4975278A (en) 1988-02-26 1990-12-04 Bristol-Myers Company Antibody-enzyme conjugates in combination with prodrugs for the delivery of cytotoxic agents to tumor cells
US4943579A (en) 1987-10-06 1990-07-24 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Water soluble prodrugs of camptothecin
FR2676058B1 (fr) 1991-04-30 1994-02-25 Hoechst Lab Prodrogues glycosylees, leur procede de preparation et leur utilisation dans le traitement des cancers.
DE4229903A1 (de) 1992-09-08 1994-03-10 Bayer Ag Neue Acetale von Ketophosphamid und Alkylglycosiden
DE4236237A1 (de) 1992-10-27 1994-04-28 Behringwerke Ag Prodrugs, ihre Herstellung und Verwendung als Arzneimittel
US5646159A (en) 1994-07-20 1997-07-08 Research Triangle Institute Water-soluble esters of camptothecin compounds
DE69734887T2 (de) 1996-09-10 2006-08-24 The Burnham Institute, La Jolla Tumor findende moleküle, davon abstammende konjugate und verfahren zu deren verwendung
JP2002544242A (ja) 1999-05-14 2002-12-24 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 酵素活性化抗腫瘍プロドラッグ化合物
EP1238678A1 (en) 2001-03-08 2002-09-11 Bayer Aktiengesellschaft Enzyme-activated cytostatic conjugates with integrin ligands
TW201004647A (en) * 2008-05-20 2010-02-01 Sigma Tau Ind Farmaceuti Novel dual targeting antitumoural conjugates

Also Published As

Publication number Publication date
AR116999A1 (es) 2021-06-30
CA3118041A1 (en) 2020-05-14
EP3876993A1 (en) 2021-09-15
KR20210100607A (ko) 2021-08-17
BR112021008232A2 (pt) 2021-08-03
TW202039005A (zh) 2020-11-01
JP2022506299A (ja) 2022-01-17
MX2021005134A (es) 2021-07-07
WO2020094471A1 (en) 2020-05-14
IL282748A (en) 2021-06-30
SG11202104491SA (en) 2021-05-28
CL2021001142A1 (es) 2021-11-12
US20210386864A1 (en) 2021-12-16
AU2019376293A1 (en) 2021-06-03
CN113260382A (zh) 2021-08-13

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