JP6701077B2 - 標的化薬物結合体と使用するためのメチレンカルバメートリンカー - Google Patents

標的化薬物結合体と使用するためのメチレンカルバメートリンカー Download PDF

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Publication number: JP6701077B2
Authority: JP; Japan
Prior art keywords: unit; drug; formula; ligand; self
Prior art date: 2013-12-19
Legal status (The legal status 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 status listed.): Expired - Fee Related

Application number

JP2016536776A

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English (en)

Japanese (ja)

Other versions

JP2017500299A (ja

JP2017500299A5 (2

Inventor

ロバートコラコウスキー，

スコットジェフリー，

パトリックバーク，

Original Assignee

シアトルジェネティックス，インコーポレイテッド

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.)

2013-12-19

Filing date

2014-12-19

Publication date

2020-05-27

2014-12-19 Application filed by シアトルジェネティックス，インコーポレイテッド, シアトルジェネティックス，インコーポレイテッド filed Critical シアトルジェネティックス，インコーポレイテッド

2017-01-05 Publication of JP2017500299A publication Critical patent/JP2017500299A/ja

2018-02-01 Publication of JP2017500299A5 publication Critical patent/JP2017500299A5/ja

2020-05-27 Application granted granted Critical

2020-05-27 Publication of JP6701077B2 publication Critical patent/JP6701077B2/ja

Status Expired - Fee Related legal-status Critical Current

2034-12-19 Anticipated expiration legal-status Critical

Links

0 C**N(C1)C(C)CN1C1[C@](C)CCC1 Chemical compound C**N(C1)C(C)CN1C1[C@](C)CCC1 0.000 description 7
UCPISOURSRJCPU-UHFFFAOYSA-N CC(C)(CC(C)(C)NC)C(C)=O Chemical compound CC(C)(CC(C)(C)NC)C(C)=O UCPISOURSRJCPU-UHFFFAOYSA-N 0.000 description 1
GQFMWKZGYUUBOJ-MSZQBOFLSA-N CC(CC(N1[C@@H](CN)C(C)=O)=O)C1=O Chemical compound CC(CC(N1[C@@H](CN)C(C)=O)=O)C1=O GQFMWKZGYUUBOJ-MSZQBOFLSA-N 0.000 description 1
UXUWCCFSZDUUBO-MSZQBOFLSA-N CC(CC(O)=O)C(N[C@@H](CN)C(C)=O)=O Chemical compound CC(CC(O)=O)C(N[C@@H](CN)C(C)=O)=O UXUWCCFSZDUUBO-MSZQBOFLSA-N 0.000 description 1
GDFXLEZMBVTRFB-UHFFFAOYSA-N NCc(c1ccccc11)c[n]1I Chemical compound NCc(c1ccccc11)c[n]1I GDFXLEZMBVTRFB-UHFFFAOYSA-N 0.000 description 1

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
- A61K47/68—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
- 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
- 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
- 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
- A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
- 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
- A61K47/6835—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6851—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
- 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
- A61K47/6835—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6851—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
- A61K47/6863—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from stomach or intestines cancer cell
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

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Health & Medical Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Chemical & Material Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Immunology (AREA)
Epidemiology (AREA)
Cell Biology (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
Oncology (AREA)
Transplantation (AREA)
Medicinal Preparation (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

JP2016536776A 2013-12-19 2014-12-19 標的化薬物結合体と使用するためのメチレンカルバメートリンカー Expired - Fee Related JP6701077B2 (ja)

Applications Claiming Priority (5)

Application Number	Priority Date	Filing Date	Title
US201361918539P	2013-12-19	2013-12-19
US61/918,539		2013-12-19
TW103144705A TWI727919B (zh)	2013-12-19	2014-12-19	與標的-藥物結合物併用之亞甲基胺基甲酸酯連接物
TW103144705		2014-12-19
PCT/US2014/071593 WO2015095755A1 (en)	2013-12-19	2014-12-19	Methylene carbamate linkers for use with targeted-drug conjugates

Related Child Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2019041218A Division JP6784790B2 (ja)	2013-12-19	2019-03-07	標的化薬物結合体と使用するためのメチレンカルバメートリンカー

Publications (3)

Publication Number	Publication Date
JP2017500299A JP2017500299A (ja)	2017-01-05
JP2017500299A5 JP2017500299A5 (2)	2018-02-01
JP6701077B2 true JP6701077B2 (ja)	2020-05-27

Family

ID=60450371

Family Applications (4)

Application Number	Title	Priority Date	Filing Date
JP2016536776A Expired - Fee Related JP6701077B2 (ja)	2013-12-19	2014-12-19	標的化薬物結合体と使用するためのメチレンカルバメートリンカー
JP2019041218A Active JP6784790B2 (ja)	2013-12-19	2019-03-07	標的化薬物結合体と使用するためのメチレンカルバメートリンカー
JP2020109383A Active JP7229202B2 (ja)	2013-12-19	2020-06-25	標的化薬物結合体と使用するためのメチレンカルバメートリンカー
JP2023020516A Withdrawn JP2023055973A (ja)	2013-12-19	2023-02-14	標的化薬物結合体と使用するためのメチレンカルバメートリンカー

Family Applications After (3)

Application Number	Title	Priority Date	Filing Date
JP2019041218A Active JP6784790B2 (ja)	2013-12-19	2019-03-07	標的化薬物結合体と使用するためのメチレンカルバメートリンカー
JP2020109383A Active JP7229202B2 (ja)	2013-12-19	2020-06-25	標的化薬物結合体と使用するためのメチレンカルバメートリンカー
JP2023020516A Withdrawn JP2023055973A (ja)	2013-12-19	2023-02-14	標的化薬物結合体と使用するためのメチレンカルバメートリンカー

Country Status (13)

Country	Link
US (2)	US11116847B2 (2)
JP (4)	JP6701077B2 (2)
KR (3)	KR102442906B1 (2)
CN (3)	CN105813653B (2)
AU (3)	AU2014369019B2 (2)
CA (1)	CA2932647C (2)
IL (5)	IL290330B2 (2)
MX (2)	MX385651B (2)
NZ (1)	NZ721877A (2)
SG (1)	SG11201610465PA (2)
TW (1)	TWI727919B (2)
WO (1)	WO2015095755A1 (2)
ZA (2)	ZA201604564B (2)

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CN105813653B (zh)	2020-06-26
IL246015A0 (en)	2016-07-31
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CN111569086B (zh)	2024-06-21
KR20220127364A (ko)	2022-09-19
JP2019081813A (ja)	2019-05-30
MX2021010192A (es)	2021-09-21
CN105813653A (zh)	2016-07-27
TW201532616A (zh)	2015-09-01
AU2020281140A1 (en)	2021-01-07
CN111558049B (zh)	2024-06-21
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IL290330B2 (en)	2023-09-01
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WO2015095755A1 (en)	2015-06-25
CN111558049A (zh)	2020-08-21
US20160303254A1 (en)	2016-10-20
SG11201610465PA (en)	2017-01-27
KR20160098303A (ko)	2016-08-18
CA2932647C (en)	2022-06-14
AU2022283652B2 (en)	2024-10-03
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