CA3125998A1 - Traceless linkers and protein-conjugates thereof - Google Patents

Traceless linkers and protein-conjugates thereof Download PDF

Info

Publication number
CA3125998A1
CA3125998A1 CA3125998A CA3125998A CA3125998A1 CA 3125998 A1 CA3125998 A1 CA 3125998A1 CA 3125998 A CA3125998 A CA 3125998A CA 3125998 A CA3125998 A CA 3125998A CA 3125998 A1 CA3125998 A1 CA 3125998A1
Authority
CA
Canada
Prior art keywords
hydrogen
alkylene
compound
alkyl
membered heterocyclyl
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
CA3125998A
Other languages
English (en)
French (fr)
Inventor
Amy Han
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.)
Regeneron Pharmaceuticals Inc
Original Assignee
Regeneron Pharmaceuticals 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
Priority claimed from US16/243,020 external-priority patent/US20190209702A1/en
Application filed by Regeneron Pharmaceuticals Inc filed Critical Regeneron Pharmaceuticals Inc
Publication of CA3125998A1 publication Critical patent/CA3125998A1/en
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/0026—Oxygen-containing hetero ring cyclic ketals
    • C07J71/0031—Oxygen-containing hetero ring cyclic ketals at positions 16, 17
    • 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
    • A61K47/61—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 the organic macromolecular compound being a polysaccharide or a derivative 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
    • A61K47/50—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
    • 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
    • A61K47/6849—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 receptor, a cell surface antigen or a cell surface determinant
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0088—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing unsubstituted amino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0046—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa
    • C07J5/0061—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa substituted in position 16
    • C07J5/0069—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group
    • C07J5/0076—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group by an alkyl group
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
    • C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/0006—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid
    • C08B37/0009—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid alpha-D-Glucans, e.g. polydextrose, alternan, glycogen; (alpha-1,4)(alpha-1,6)-D-Glucans; (alpha-1,3)(alpha-1,4)-D-Glucans, e.g. isolichenan or nigeran; (alpha-1,4)-D-Glucans; (alpha-1,3)-D-Glucans, e.g. pseudonigeran; Derivatives thereof
    • C08B37/0012—Cyclodextrin [CD], e.g. cycle with 6 units (alpha), with 7 units (beta) and with 8 units (gamma), large-ring cyclodextrin or cycloamylose with 9 units or more; Derivatives thereof

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Cell Biology (AREA)
  • Polymers & Plastics (AREA)
  • Materials Engineering (AREA)
  • Molecular Biology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CA3125998A 2019-01-08 2020-01-08 Traceless linkers and protein-conjugates thereof Pending CA3125998A1 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US16/243,020 US20190209702A1 (en) 2018-01-08 2019-01-08 Steroids and antibody-conjugates thereof
PCT/US2019/012786 WO2019136487A2 (en) 2018-01-08 2019-01-08 Steroids and antibody-conjugates thereof
US16/243,020 2019-01-08
USPCT/US2019/012786 2019-01-08
US201962872229P 2019-07-09 2019-07-09
US62/872,229 2019-07-09
US201962937721P 2019-11-19 2019-11-19
US62/937,721 2019-11-19
PCT/US2020/012798 WO2020146541A2 (en) 2019-01-08 2020-01-08 Traceless linkers and protein-conjugates thereof

Publications (1)

Publication Number Publication Date
CA3125998A1 true CA3125998A1 (en) 2020-07-16

Family

ID=71521936

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3125998A Pending CA3125998A1 (en) 2019-01-08 2020-01-08 Traceless linkers and protein-conjugates thereof

Country Status (14)

Country Link
EP (1) EP3908323A2 (es)
JP (1) JP2022517767A (es)
KR (1) KR20210114008A (es)
CN (1) CN113905767A (es)
AU (1) AU2020205662A1 (es)
BR (1) BR112021013464A2 (es)
CA (1) CA3125998A1 (es)
CL (1) CL2021001790A1 (es)
CO (1) CO2021010315A2 (es)
IL (1) IL284673A (es)
MA (2) MA59295A1 (es)
MX (1) MX2021008114A (es)
SG (1) SG11202107212QA (es)
WO (1) WO2020146541A2 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7330101B2 (ja) 2016-11-08 2023-08-21 レゲネロン ファーマシューティカルス，インコーポレーテッド ステロイド及びそのタンパク質コンジュゲート
CN110944718A (zh) 2017-05-18 2020-03-31 里珍纳龙药品有限公司 环糊精蛋白质药物偶联物
BR112020022400A2 (pt) 2018-05-09 2021-02-02 Regeneron Pharmaceuticals, Inc. anticorpos anti-msr1 e métodos de uso dos mesmos
US11806405B1 (en) 2021-07-19 2023-11-07 Zeno Management, Inc. Immunoconjugates and methods
WO2023079362A1 (en) * 2021-11-03 2023-05-11 Ripple Therapeutics Corporation Processable compositions and use for the same
US20230287138A1 (en) 2022-01-12 2023-09-14 Regneron Pharmaceuticals, Inc. Protein-drug conjugates comprising camptothecin analogs and methods of use thereof
TW202340252A (zh) * 2022-01-29 2023-10-16 大陸商上海盛迪醫藥有限公司 糖皮質激素的藥物偶聯物

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5208020A (en) 1989-10-25 1993-05-04 Immunogen Inc. Cytotoxic agents comprising maytansinoids and their therapeutic use
US5714586A (en) 1995-06-07 1998-02-03 American Cyanamid Company Methods for the preparation of monomeric calicheamicin derivative/carrier conjugates
US20070258987A1 (en) 2000-11-28 2007-11-08 Seattle Genetics, Inc. Recombinant Anti-Cd30 Antibodies and Uses Thereof
TW200539855A (en) 2004-03-15 2005-12-16 Wyeth Corp Calicheamicin conjugates
BRPI0510883B8 (pt) 2004-06-01 2021-05-25 Genentech Inc composto conjugado de droga e anticorpo, composição farmacêutica, método de fabricação de composto conjugado de droga e anticorpo e usos de uma formulação, de um conjugado de droga e anticorpo e um agente quimioterapêutico e de uma combinação
JP2008521828A (ja) 2004-11-29 2008-06-26 シアトル ジェネティックス， インコーポレイテッド 操作された抗体およびイムノコンジュゲート
US7750116B1 (en) 2006-02-18 2010-07-06 Seattle Genetics, Inc. Antibody drug conjugate metabolites
WO2008122039A2 (en) 2007-04-02 2008-10-09 The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Selenocysteine mediated hybrid antibody molecules
EP2167963B1 (en) 2007-05-23 2019-04-17 Ventana Medical Systems, Inc. Polymeric carriers for immunohistochemistry and in situ hybridization
BRPI0911442A2 (pt) 2008-04-30 2019-03-12 Immunogen, Inc. conjugados potentes e ligantes hidrofílicos
KR101000067B1 (ko) 2008-12-30 2010-12-10 엘지전자 주식회사 고효율 태양전지용 레이저 소성장치 및 고효율 태양전지 제조방법
US20130028917A1 (en) 2010-04-15 2013-01-31 Spirogen Developments Sàrl Pyrrolobenzodiazepines and conjugates thereof
WO2012005982A2 (en) 2010-07-06 2012-01-12 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Reporter for rna polymerase ii termination
EP2714685B1 (en) 2011-05-27 2016-10-19 Ambrx, Inc. Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
US8815226B2 (en) 2011-06-10 2014-08-26 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
WO2013053872A1 (en) 2011-10-14 2013-04-18 Spirogen Sàrl Synthesis method and intermediates useful in the preparation of pyrrolobenzodiazepines
WO2013055990A1 (en) 2011-10-14 2013-04-18 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
KR101891859B1 (ko) 2011-10-14 2018-08-24 메디뮨 리미티드 피롤로벤조디아제핀
CN103997893B (zh) 2011-10-14 2019-04-12 西雅图基因公司 吡咯并苯并二氮杂卓和靶向结合物
WO2013068874A1 (en) 2011-11-11 2013-05-16 Pfizer Inc. Antibody-drug conjugates
CN110201186A (zh) 2012-10-23 2019-09-06 西纳福克斯股份有限公司 经修饰的抗体、抗体-缀合物及其制备方法
KR20160042871A (ko) * 2013-06-21 2016-04-20 이나뜨 파르마, 에스.아. 폴리펩티드의 효소적 콘쥬게이션
TWI641620B (zh) 2013-08-21 2018-11-21 再生元醫藥公司 抗－ｐｒｌｒ抗體及其用途
SG11201608309PA (en) * 2014-04-10 2016-11-29 Daiichi Sankyo Co Ltd Anti-her3 antibody-drug conjugate
CA3025377A1 (en) * 2016-06-02 2017-12-07 Abbvie Inc. Glucocorticoid receptor agonist and immunoconjugates thereof
CA3037732A1 (en) 2016-09-23 2018-03-29 Regeneron Pharmaceuticals, Inc. Anti-steap2 antibodies, antibody-drug conjugates, and bispecific antigen-binding molecules that bind steap2 and cd3, and uses thereof
EA201900562A1 (ru) * 2017-05-18 2020-05-12 Регенерон Фармасьютикалз, Инк. Бис-октагидрофенантрена карбоксамиды и их белковые конъюгаты
CN110944718A (zh) * 2017-05-18 2020-03-31 里珍纳龙药品有限公司 环糊精蛋白质药物偶联物
WO2019034176A1 (zh) * 2017-08-18 2019-02-21 四川百利药业有限责任公司 一种喜树碱-抗体偶联物
WO2019034177A1 (zh) * 2017-08-18 2019-02-21 四川百利药业有限责任公司 具有两种不同药物的抗体药物偶联物
CA3086926A1 (en) * 2018-01-08 2019-07-11 Regeneron Pharmaceuticals, Inc. Steroids and antibody-conjugates thereof
CN112135542B (zh) 2018-05-08 2022-08-16 耐克创新有限合伙公司 与聚烯烃板的结合以及由其形成的鞋类物品
BR112020022400A2 (pt) 2018-05-09 2021-02-02 Regeneron Pharmaceuticals, Inc. anticorpos anti-msr1 e métodos de uso dos mesmos

Also Published As

Publication number Publication date
CO2021010315A2 (es) 2021-08-19
WO2020146541A3 (en) 2020-08-13
EP3908323A2 (en) 2021-11-17
MX2021008114A (es) 2021-08-05
MA59295A1 (fr) 2023-07-31
BR112021013464A2 (pt) 2021-09-21
KR20210114008A (ko) 2021-09-17
WO2020146541A2 (en) 2020-07-16
AU2020205662A1 (en) 2021-07-22
IL284673A (en) 2021-08-31
MA53772B1 (fr) 2023-08-31
SG11202107212QA (en) 2021-07-29
CN113905767A (zh) 2022-01-07
JP2022517767A (ja) 2022-03-10
MA53772A1 (fr) 2022-10-31
CL2021001790A1 (es) 2022-07-01

Similar Documents

Publication Publication Date Title
US20240101594A1 (en) Steroids and protein-conjugates thereof
CA3125998A1 (en) Traceless linkers and protein-conjugates thereof
US20190209702A1 (en) Steroids and antibody-conjugates thereof
TW202404648A (zh) 抗體－吡咯并苯二氮呯衍生物複合體
CA3098453A1 (en) Anti-msr1 antibodies and methods of use thereof
CA3063871A1 (en) Cyclodextrin protein drug conjugates
CA2970565A1 (en) Antibody-drug conjugates (adcs) of ksp inhibitors with aglycosylated anti-tweakr antibodies
CA3063872A1 (en) Bis-octahydrophenanthrene carboxamides and protein conjugates thereof
KR20210106467A (ko) 튜불리신 및 단백질-튜불리신 접합체
US20230119539A1 (en) Traceless linkers and protein-conjugates thereof
CA3185601A1 (en) Tubulysins and protein-tubulysin conjugates
EA045111B1 (ru) Стероиды и их антитело-конъюгаты
EA045579B1 (ru) Стероиды и их конъюгаты с белками
NZ793831A (en) Steroids and protein-conjugates thereof

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20220926

EEER Examination request

Effective date: 20220926

EEER Examination request

Effective date: 20220926

EEER Examination request

Effective date: 20220926

EEER Examination request

Effective date: 20220926

EEER Examination request

Effective date: 20220926