CN110461860A - 卡奇霉素衍生物及其抗体药物缀合物 - Google Patents

卡奇霉素衍生物及其抗体药物缀合物 Download PDF

Info

Publication number
CN110461860A
CN110461860A CN201880020707.5A CN201880020707A CN110461860A CN 110461860 A CN110461860 A CN 110461860A CN 201880020707 A CN201880020707 A CN 201880020707A CN 110461860 A CN110461860 A CN 110461860A
Authority
CN
China
Prior art keywords
alkyl
optionally substituted
absent
formula
con
Prior art date
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.)
Pending
Application number
CN201880020707.5A
Other languages
English (en)
Chinese (zh)
Inventor
O.K.艾哈迈德
S.P.布朗
K.J.迪里科
R.杜欣
G.F.菲尔岑
S.普滕维蒂尔
P.斯特罗普
C.苏布拉曼亚姆
L.N.塔米
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Inc
Original Assignee
Pfizer Inc
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 Pfizer Inc filed Critical Pfizer Inc
Publication of CN110461860A publication Critical patent/CN110461860A/zh
Pending legal-status Critical Current

Links

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
    • A61K47/62—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/22—Cyclohexane rings, substituted by nitrogen atoms
    • 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
    • A61K47/6867—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 a cell of a blood cancer
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
    • 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
    • A61K47/6807—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug or compound being a sugar, nucleoside, nucleotide, nucleic acid, e.g. RNA antisense
    • 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
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Cell Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Saccharide Compounds (AREA)
  • Peptides Or Proteins (AREA)
CN201880020707.5A 2017-01-24 2018-01-10 卡奇霉素衍生物及其抗体药物缀合物 Pending CN110461860A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762449839P 2017-01-24 2017-01-24
US62/449839 2017-01-24
PCT/IB2018/050153 WO2018138591A1 (en) 2017-01-24 2018-01-10 Calicheamicin derivatives and antibody drug conjugates thereof

Publications (1)

Publication Number Publication Date
CN110461860A true CN110461860A (zh) 2019-11-15

Family

ID=61168135

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880020707.5A Pending CN110461860A (zh) 2017-01-24 2018-01-10 卡奇霉素衍生物及其抗体药物缀合物

Country Status (14)

Country Link
US (2) US11993625B2 (cg-RX-API-DMAC10.html)
EP (1) EP3573995A1 (cg-RX-API-DMAC10.html)
JP (1) JP7078405B2 (cg-RX-API-DMAC10.html)
KR (1) KR20190111086A (cg-RX-API-DMAC10.html)
CN (1) CN110461860A (cg-RX-API-DMAC10.html)
AU (1) AU2018211561B2 (cg-RX-API-DMAC10.html)
BR (1) BR112019015069A2 (cg-RX-API-DMAC10.html)
CA (1) CA3051038C (cg-RX-API-DMAC10.html)
IL (1) IL268245A (cg-RX-API-DMAC10.html)
MX (1) MX2019008773A (cg-RX-API-DMAC10.html)
RU (1) RU2732568C1 (cg-RX-API-DMAC10.html)
SG (1) SG11201906414VA (cg-RX-API-DMAC10.html)
TW (1) TWI687221B (cg-RX-API-DMAC10.html)
WO (1) WO2018138591A1 (cg-RX-API-DMAC10.html)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3824906A1 (en) 2016-12-21 2021-05-26 Amgen Inc. Anti-tnf alpha antibody formulations
EP3573995A1 (en) * 2017-01-24 2019-12-04 Pfizer Inc. Calicheamicin derivatives and antibody drug conjugates thereof
EP3720504A1 (en) * 2017-12-06 2020-10-14 Synaffix B.V. Enediyne conjugates
EP3976112A1 (en) * 2019-06-03 2022-04-06 Synaffix B.V. Acetal-based cleavable linkers
GB2585102B (en) 2019-10-09 2021-06-30 Audio Inventions Ltd System for identification of a note played by a musical instrument
WO2025151608A1 (en) * 2024-01-10 2025-07-17 Systimmune, Inc. Connecting units for ligand-drug conjugates and methods of making and using thereof
WO2026050757A2 (en) * 2024-08-30 2026-03-05 ALX Oncology Inc. Calicheamicin derivatives and antibody-drug conjugates thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0313873A1 (en) * 1987-10-30 1989-05-03 American Cyanamid Company Targeted forms of methyltrithio antitumor agents
EP0689845A2 (en) * 1994-06-03 1996-01-03 American Cyanamid Company Conjugates of methyltrithio antitumor agents and intermediates for their synthesis
US5606040A (en) * 1987-10-30 1997-02-25 American Cyanamid Company Antitumor and antibacterial substituted disulfide derivatives prepared from compounds possessing a methyl-trithio group

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2036891B (en) 1978-12-05 1983-05-05 Windsor Smith C Change speed gear
GB8308235D0 (en) 1983-03-25 1983-05-05 Celltech Ltd Polypeptides
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
JPS6147500A (ja) 1984-08-15 1986-03-07 Res Dev Corp Of Japan キメラモノクロ−ナル抗体及びその製造法
EP0173494A3 (en) 1984-08-27 1987-11-25 The Board Of Trustees Of The Leland Stanford Junior University Chimeric receptors by dna splicing and expression
GB8422238D0 (en) 1984-09-03 1984-10-10 Neuberger M S Chimeric proteins
US4970198A (en) 1985-10-17 1990-11-13 American Cyanamid Company Antitumor antibiotics (LL-E33288 complex)
JPS61134325A (ja) 1984-12-04 1986-06-21 Teijin Ltd ハイブリツド抗体遺伝子の発現方法
DE3689123T2 (de) 1985-11-01 1994-03-03 Xoma Corp Modulare einheit von antikörpergenen, daraus hergestellte antikörper und verwendung.
US5225539A (en) 1986-03-27 1993-07-06 Medical Research Council Recombinant altered antibodies and methods of making altered antibodies
US5053394A (en) 1988-09-21 1991-10-01 American Cyanamid Company Targeted forms of methyltrithio antitumor agents
US5530101A (en) 1988-12-28 1996-06-25 Protein Design Labs, Inc. Humanized immunoglobulins
DE3920358A1 (de) 1989-06-22 1991-01-17 Behringwerke Ag Bispezifische und oligospezifische, mono- und oligovalente antikoerperkonstrukte, ihre herstellung und verwendung
US5633425A (en) 1990-08-29 1997-05-27 Genpharm International, Inc. Transgenic non-human animals capable of producing heterologous antibodies
ES2246502T3 (es) 1990-08-29 2006-02-16 Genpharm International, Inc. Animales no humanos transgenicos capaces de producir anticuerpos heterologos.
US5661016A (en) 1990-08-29 1997-08-26 Genpharm International Inc. Transgenic non-human animals capable of producing heterologous antibodies of various isotypes
US5545806A (en) 1990-08-29 1996-08-13 Genpharm International, Inc. Ransgenic non-human animals for producing heterologous antibodies
US5625126A (en) 1990-08-29 1997-04-29 Genpharm International, Inc. Transgenic non-human animals for producing heterologous antibodies
DE69233528T2 (de) 1991-11-25 2006-03-16 Enzon, Inc. Verfahren zur Herstellung von multivalenten antigenbindenden Proteinen
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
CA2249195A1 (en) 1996-03-18 1997-09-25 Board Of Regents, The University Of Texas System Immunoglobin-like domains with increased half lives
WO2000035298A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Chewing gum containing medicament active agents
WO2005009882A1 (en) * 2003-06-27 2005-02-03 Otis Elevator Company Absolute positioning system for elevators using dual encoders
HUE035853T2 (en) 2005-07-18 2018-05-28 Seattle Genetics Inc Beta-glucuronide-linker-drug conjugates
EP1886696A1 (en) * 2006-08-03 2008-02-13 Endotis Pharma Conjugates of antithrombin binding oligosaccharide derivatives and therapeutic proteins
EP3279215B1 (en) 2009-11-24 2020-02-12 MedImmune Limited Targeted binding agents against b7-h1
JP6055404B2 (ja) * 2010-06-15 2016-12-27 ゲンマブ エー／エス 組織因子に対するヒト抗体薬物結合体
SG186451A1 (en) 2010-07-12 2013-01-30 Covx Technologies Ireland Ltd Multifunctional antibody conjugates
CA2813411C (en) 2010-11-05 2016-08-02 Rinat Neuroscience Corporation Engineered polypeptide conjugates and methods for making thereof using transglutaminase
SG11201401699WA (en) 2011-11-11 2014-09-26 Rinat Neuroscience Corp Antibodies specific for trop-2 and their uses
BR112014012819B1 (pt) 2011-11-28 2022-08-16 Merck Patent Gmbh Anticorpo anti-pd-l1 ou fragmento de ligação ao antígeno do mesmo e composição
EP3539982B1 (en) 2011-12-23 2025-02-19 Pfizer Inc. Engineered antibody constant regions for site-specific conjugation and methods and uses therefor
MX340090B (es) 2012-11-05 2016-06-23 Pfizer Analogos de spliceostatina.
US9453508B2 (en) 2013-02-25 2016-09-27 Asmo Co., Ltd. Electric oil pump and hydraulic pressure supply device
KR101614151B1 (ko) 2014-07-01 2016-04-22 한국화학연구원 흡입 독성 시험용 폐 모델 장치
HUE049325T2 (hu) 2014-08-28 2020-09-28 Pfizer Stabilitás modulátor linker antitest-hatóanyag konjugátumokhoz történõ alkalmazásra
JP6852065B2 (ja) 2015-10-20 2021-03-31 ジェネンテック， インコーポレイテッド カリケアマイシン−抗体−薬物コンジュゲート及び使用方法
WO2017172907A1 (en) 2016-03-29 2017-10-05 Sorrento Therapeutics, Inc. Calicheamicin antibody drug conjugates linking an amidoacetyl group to a sugar moiety on calicheamicin
WO2018069851A2 (en) 2016-10-11 2018-04-19 Sorrento Therapeutics, Inc. C-met antibody drug conjugate
EP3573995A1 (en) * 2017-01-24 2019-12-04 Pfizer Inc. Calicheamicin derivatives and antibody drug conjugates thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0313873A1 (en) * 1987-10-30 1989-05-03 American Cyanamid Company Targeted forms of methyltrithio antitumor agents
US5606040A (en) * 1987-10-30 1997-02-25 American Cyanamid Company Antitumor and antibacterial substituted disulfide derivatives prepared from compounds possessing a methyl-trithio group
EP0689845A2 (en) * 1994-06-03 1996-01-03 American Cyanamid Company Conjugates of methyltrithio antitumor agents and intermediates for their synthesis

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
CHARLES E. MELANÇON III，ET AL.: "Glyco-Stripping and Glyco-Swapping", 《ACS CHEMICAL BIOLOGY》 *
IRWIN HOLLANDER，ET AL.: "Selection of Reaction Additives Used in the Preparation of Monomeric Antibody-Calicheamicin Conjugates", 《BIOCONJUGATE CHEM.》 *
LOIS M. HINMAN，ET AL.: "Preparation and Characterization of Monoclonal Antibody Conjugates of the Calicheamicins: A Novel and Potent Family of Antitumor Antibiotics", 《CANCER RESEARCH》 *

Also Published As

Publication number Publication date
JP2018123122A (ja) 2018-08-09
RU2732568C1 (ru) 2020-09-21
TW201838632A (zh) 2018-11-01
BR112019015069A2 (pt) 2020-03-03
IL268245A (en) 2019-09-26
KR20190111086A (ko) 2019-10-01
WO2018138591A1 (en) 2018-08-02
US11993625B2 (en) 2024-05-28
AU2018211561A1 (en) 2019-07-18
US20240409573A1 (en) 2024-12-12
MX2019008773A (es) 2019-09-18
US20190345186A1 (en) 2019-11-14
CA3051038C (en) 2022-07-26
JP7078405B2 (ja) 2022-05-31
SG11201906414VA (en) 2019-08-27
TWI687221B (zh) 2020-03-11
EP3573995A1 (en) 2019-12-04
AU2018211561B2 (en) 2020-04-30
CA3051038A1 (en) 2018-08-02

Similar Documents

Publication Publication Date Title
US20240409573A1 (en) Calicheamicin derivatives and antibody drug conjugates thereof
JP6751165B2 (ja) 抗ｂ７−ｈ３抗体及び抗体薬物コンジュゲート
TWI654998B (zh) 雙官能性胞毒劑
CN109562170B (zh) 抗cd98抗体及抗体药物偶联物
CN116059201A (zh) 抗egfr抗体药物偶联物
CN106661123A (zh) 抗‑cd22抗体‑药物缀合物及其使用方法
IL303048A (en) Bcl-xl inhibitor antibody-drug conjugates and methods of use thereof
WO2015195904A1 (en) Her2 antibody-drug conjugates
TW202404645A (zh) Met bcl-xl抑制劑抗體-藥物結合物及其使用方法
HK40017839A (en) Calicheamicin derivatives and antibody drug conjugates thereof
CN107660208B (zh) 包含cti药效团的双功能细胞毒性剂
TW202540186A (zh) 抗ｃｄ７抗體藥物結合物及其使用方法
NZ788873A (en) Anti-B7-H3 antibodies and antibody drug conjugates
BR112018075626B1 (pt) Conjugado fármaco-anticorpo anti-b7-h3 humano
HK1245252B (en) Bifunctional cytotoxic agents containing the cti pharmacophore
HK1233252B (en) Bifunctional cytotoxic agents

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40017839

Country of ref document: HK

WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20191115

WD01 Invention patent application deemed withdrawn after publication
REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 40017839

Country of ref document: HK