KR102252925B1 - 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도 - Google Patents

마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도 Download PDF

Info

Publication number
KR102252925B1
KR102252925B1 KR1020167008038A KR20167008038A KR102252925B1 KR 102252925 B1 KR102252925 B1 KR 102252925B1 KR 1020167008038 A KR1020167008038 A KR 1020167008038A KR 20167008038 A KR20167008038 A KR 20167008038A KR 102252925 B1 KR102252925 B1 KR 102252925B1
Authority
KR
South Korea
Prior art keywords
formula
compound
diastereomer
iib
chiral carbon
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.)
Active
Application number
KR1020167008038A
Other languages
English (en)
Korean (ko)
Other versions
KR20160045146A (ko
Inventor
토마스 니톨리
나레시쿠마르 에프. 자인
토마스 패트릭 마르코탄
Original Assignee
리제너론 파마슈티칼스 인코포레이티드
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 리제너론 파마슈티칼스 인코포레이티드 filed Critical 리제너론 파마슈티칼스 인코포레이티드
Publication of KR20160045146A publication Critical patent/KR20160045146A/ko
Application granted granted Critical
Publication of KR102252925B1 publication Critical patent/KR102252925B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • A61K47/68033—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
    • 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
    • A61K47/6809—Antibiotics, e.g. antitumor antibiotics anthracyclins, adriamycin, doxorubicin or daunomycin
    • 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
    • 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
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Cell Biology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
KR1020167008038A 2013-08-26 2014-08-26 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도 Active KR102252925B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361869954P 2013-08-26 2013-08-26
US61/869,954 2013-08-26
US201461934313P 2014-01-31 2014-01-31
US61/934,313 2014-01-31
PCT/US2014/052757 WO2015031396A1 (en) 2013-08-26 2014-08-26 Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses

Publications (2)

Publication Number Publication Date
KR20160045146A KR20160045146A (ko) 2016-04-26
KR102252925B1 true KR102252925B1 (ko) 2021-05-18

Family

ID=51542449

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020167008038A Active KR102252925B1 (ko) 2013-08-26 2014-08-26 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도

Country Status (17)

Country Link
US (3) US20160354482A1 (OSRAM)
EP (1) EP3038624B1 (OSRAM)
JP (1) JP6608823B2 (OSRAM)
KR (1) KR102252925B1 (OSRAM)
CN (1) CN105530942B (OSRAM)
AU (1) AU2014311361B2 (OSRAM)
BR (1) BR112016004023A2 (OSRAM)
CA (1) CA2921412C (OSRAM)
CL (1) CL2016000408A1 (OSRAM)
EA (1) EA038192B1 (OSRAM)
ES (1) ES2989322T3 (OSRAM)
IL (1) IL244203B (OSRAM)
MX (1) MX373528B (OSRAM)
PH (1) PH12016500380A1 (OSRAM)
SG (1) SG11201601230RA (OSRAM)
WO (1) WO2015031396A1 (OSRAM)
ZA (1) ZA201601534B (OSRAM)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3964237B1 (en) 2013-03-15 2026-02-18 Regeneron Pharmaceuticals, Inc. Biologically active molecules, conjugates thereof, and therapeutic uses
KR102252925B1 (ko) 2013-08-26 2021-05-18 리제너론 파마슈티칼스 인코포레이티드 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도
KR20240142591A (ko) 2015-03-27 2024-09-30 리제너론 파아마슈티컬스, 인크. 메이탄시노이드 유도체, 이의 컨주게이트, 및 사용 방법
MY189159A (en) 2015-07-06 2022-01-29 Regeneron Pharma Multispecific antigen-binding molecules and uses thereof
MY198605A (en) 2016-01-25 2023-09-08 Regeneron Pharma Maytansinoid derivatives conjugates thereof, and methods of use
WO2017190079A1 (en) 2016-04-28 2017-11-02 Regeneron Pharmaceuticals, Inc. Methods of making multispecific antigen-binding molecules
US10738130B2 (en) 2016-09-23 2020-08-11 Regeneron Pharmaceuticals, Inc. Bispecific antigen-binding molecules that bind MUC16 and CD3, and compositions thereof
MA46417A (fr) 2016-09-23 2019-07-31 Regeneron Pharma Anticorps anti-steap2, conjugués anticorps-médicament, et molécules bispécifiques de liaison à l'antigène qui se lient à steap2 et cd3, et leurs utilisations
TWI782930B (zh) * 2016-11-16 2022-11-11 美商再生元醫藥公司 抗met抗體,結合met之雙特異性抗原結合分子及其使用方法
EP3548514A1 (en) 2016-11-29 2019-10-09 Regeneron Pharmaceuticals, Inc. Methods of treating prlr positive breast cancer
KR20200007905A (ko) 2017-05-18 2020-01-22 리제너론 파마슈티칼스 인코포레이티드 사이클로덱스트린 단백질 약물 접합체
ES3065816T3 (en) 2017-06-07 2026-05-08 Regeneron Pharma Compositions and methods for internalizing enzymes
IL313068A (en) 2017-11-07 2024-07-01 Regeneron Pharma Hydrophilic linkers for antibody drug conjugates
CN112074538B (zh) 2018-04-30 2024-10-18 瑞泽恩制药公司 结合her2和/或aplp2的抗体和双特异性抗原结合分子、其缀合物和用途
BR112020023145A2 (pt) 2018-05-17 2021-02-02 Regeneron Pharmaceuticals, Inc. anticorpo anti-cd63 ou fragmento de ligação ao antígeno do mesmo, molécula de ligação ao antígeno biespecífica, proteína terapêutica de múltiplos domínios, polinucleotídeo composição farmacêutica, e, composto
CA3111147A1 (en) * 2018-08-31 2020-03-05 Osteoanalgesia Llc Diastereomeric conjugate compositions and methods of making and using same
MX2021010114A (es) 2019-02-21 2021-12-10 Regeneron Pharma Métodos para tratar el cáncer ocular mediante el uso de anticuerpos anti-met y moléculas de unión a antígeno bispecíficas que se unen a met.
JP7750828B2 (ja) 2019-09-16 2025-10-07 リジェネロン・ファーマシューティカルズ・インコーポレイテッド 免疫pet撮像のための放射標識されたmet結合タンパク質
US11814428B2 (en) 2019-09-19 2023-11-14 Regeneron Pharmaceuticals, Inc. Anti-PTCRA antibody-drug conjugates and uses thereof
EP4058024A1 (en) 2019-11-15 2022-09-21 Seagen Inc. Methods of treating her2 positive breast cancer with tucatinib in combination with an anti-her2 antibody-drug conjugate
IL295312A (en) 2020-02-28 2022-10-01 Regeneron Pharma Bispecific antigen binding molecules that bind her2, and methods of use thereof
JP2023521885A (ja) 2020-04-16 2023-05-25 リジェネロン・ファーマシューティカルズ・インコーポレイテッド ディールス-アルダーコンジュゲーション方法
US12605459B2 (en) 2020-07-13 2026-04-21 Regeneron Pharmaceuticals, Inc. Protein-drug conjugates comprising camptothecin analogs and methods of use thereof
CA3190569A1 (en) 2020-10-22 2022-04-28 Christopher Daly Anti-fgfr2 antibodies and methods of use thereof
AU2021377185A1 (en) 2020-11-10 2023-06-08 Regeneron Pharmaceuticals, Inc. Selenium antibody conjugates
CN115215780B (zh) * 2022-04-22 2023-08-08 上海格苓凯生物科技有限公司 一种利用n,n-二琥珀酰亚胺基碳酸酯制备异双功能交联剂smcc的方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010126551A1 (en) 2009-04-30 2010-11-04 Immunogen, Inc. Potent conjugates and hydrophilic linkers
CN103254311A (zh) 2013-05-09 2013-08-21 齐鲁制药有限公司 一种制备抗体-美登素类生物碱药物偶联物的方法

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4307016A (en) 1978-03-24 1981-12-22 Takeda Chemical Industries, Ltd. Demethyl maytansinoids
JPS5566585A (en) 1978-11-14 1980-05-20 Takeda Chem Ind Ltd Novel maytansinoid compound and its preparation
CA2026147C (en) 1989-10-25 2006-02-07 Ravi J. Chari Cytotoxic agents comprising maytansinoids and their therapeutic use
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
US6596541B2 (en) 2000-10-31 2003-07-22 Regeneron Pharmaceuticals, Inc. Methods of modifying eukaryotic cells
US20070258987A1 (en) 2000-11-28 2007-11-08 Seattle Genetics, Inc. Recombinant Anti-Cd30 Antibodies and Uses Thereof
EP1258255A1 (en) 2001-05-18 2002-11-20 Boehringer Ingelheim International GmbH Conjugates of an antibody to CD44 and a maytansinoid
US20090068178A1 (en) * 2002-05-08 2009-03-12 Genentech, Inc. Compositions and Methods for the Treatment of Tumor of Hematopoietic Origin
US8088387B2 (en) 2003-10-10 2012-01-03 Immunogen Inc. Method of targeting specific cell populations using cell-binding agent maytansinoid conjugates linked via a non-cleavable linker, said conjugates, and methods of making said conjugates
US7276497B2 (en) 2003-05-20 2007-10-02 Immunogen Inc. Cytotoxic agents comprising new maytansinoids
US7736644B2 (en) 2003-06-27 2010-06-15 Amgen Fremont Inc. Antibodies directed to the deletion mutants of epidermal growth factor receptor and uses thereof
GB0316294D0 (en) 2003-07-11 2003-08-13 Polytherics Ltd Conjugated biological molecules and their preparation
TW200539855A (en) 2004-03-15 2005-12-16 Wyeth Corp Calicheamicin conjugates
MXPA06014065A (es) 2004-06-01 2007-01-31 Genentech Inc Conjugados de droga-anticuerpo y metodos.
AU2005316844A1 (en) 2004-11-29 2006-06-22 Seattle Genetics, Inc. Engineered antibodies and immunoconjugates
PL1819359T3 (pl) 2004-12-09 2015-08-31 Janssen Biotech Inc Immunokoniugaty skierowane przeciw integrynie, metody ich wytwarzania oraz ich zastosowanie
US7750116B1 (en) 2006-02-18 2010-07-06 Seattle Genetics, Inc. Antibody drug conjugate metabolites
AU2007308792B2 (en) 2006-10-27 2013-01-24 Genentech, Inc. Antibodies and immunoconjugates and uses therefor
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
TW200902554A (en) 2007-05-08 2009-01-16 Genentech Inc Cysteine engineered anti-MUC16 antibodies and antibody drug conjugates
ES2731432T3 (es) 2007-05-23 2019-11-15 Ventana Med Syst Inc Transportadores poliméricos para inmunohistoquímica e hibridación in situ
NZ587706A (en) * 2008-03-18 2012-12-21 Genentech Inc Combinations of an anti-her2 antibody-drug conjugate and chemotherapeutic agents, and methods of use
RU2487877C2 (ru) 2008-04-30 2013-07-20 Иммьюноджен, Инк. Высокоэффективные конъюгаты и гидрофильные сшивающие агенты (линкеры)
WO2010010324A1 (en) 2008-07-21 2010-01-28 Polytherics Limited Novel reagents and method for conjugating biological molecules
US9005598B2 (en) 2009-03-04 2015-04-14 Polytherics Limited Conjugated proteins and peptides
WO2011018613A1 (en) 2009-08-10 2011-02-17 Ucl Business Plc Functionalisation of solid substrates
UY32913A (es) 2009-10-02 2011-04-29 Sanofi Aventis Nuevos maitansinoides y el uso de dichos maitansinoides para preparar conjugados con un anticuero
UY32914A (es) 2009-10-02 2011-04-29 Sanofi Aventis Anticuerpos que se usan específicamente al receptor epha2
US8501692B2 (en) 2009-12-14 2013-08-06 The Regents Of The University Of Michigan Compositions and methods for altering cocaine esterase activity
WO2011130598A1 (en) 2010-04-15 2011-10-20 Spirogen Limited 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
KR102306967B1 (ko) 2010-08-02 2021-10-01 리제너론 파아마슈티컬스, 인크. Vl 도메인을 포함하는 결합 단백질을 생성하는 마우스
WO2012028579A1 (de) 2010-09-01 2012-03-08 Bayer Cropscience Ag N-(tetrazol-5-yl)- und n-(triazol-5-yl)arylcarbonsäureamide und ihre verwendung als herbizide
CN103328505B (zh) 2010-10-29 2015-12-02 伊缪诺金公司 非拮抗性egfr结合分子及其免疫偶联物
JP2013542958A (ja) 2010-11-03 2013-11-28 イミュノジェン・インコーポレーテッド アンサマイトシン誘導体を含む細胞傷害性剤
EP2709666B1 (en) 2011-05-16 2021-07-14 Koninklijke Philips N.V. Bio-orthogonal drug activation
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
MX350954B (es) 2011-06-21 2017-09-26 Immunogen Inc Derivados de maitansinoides novedosos con enlazador de peptido y conjugados de estos.
MX358757B (es) 2011-10-14 2018-09-03 Seattle Genetics Inc Pirrolobenzodiazepinas y conjugados dirigidos.
SG11201401021TA (en) 2011-10-14 2014-08-28 Spirogen Sarl Pyrrolobenzodiazepines
US9526798B2 (en) 2011-10-14 2016-12-27 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
US9102704B2 (en) 2011-10-14 2015-08-11 Spirogen Sarl Synthesis method and intermediates useful in the preparation of pyrrolobenzodiazepines
WO2013068874A1 (en) 2011-11-11 2013-05-16 Pfizer Inc. Antibody-drug conjugates
AU2012348017A1 (en) 2011-12-05 2014-07-03 Igenica Biotherapeutics, Inc. Antibody-drug conjugates and related compounds, compositions, and methods
GB201210770D0 (en) 2012-06-18 2012-08-01 Polytherics Ltd Novel conjugation reagents
SG11201407600UA (en) 2012-06-19 2014-12-30 Polytherics Ltd Novel process for preparation of antibody conjugates and novel antibody conjugates
ES2659270T5 (en) 2012-10-23 2026-02-11 Synaffix Bv Modified antibody, antibody-conjugate and process for the preparation thereof
NO2789793T3 (OSRAM) 2012-10-24 2018-01-27
AU2012395148B2 (en) 2012-11-24 2016-10-27 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules
TW201425336A (zh) * 2012-12-07 2014-07-01 Amgen Inc Bcma抗原結合蛋白質
CN103254213B (zh) 2012-12-21 2015-02-25 百奥泰生物科技(广州)有限公司 类美登素酯的制备方法及用于所述方法的组合物
CN104650113A (zh) 2012-12-21 2015-05-27 百奥泰生物科技(广州)有限公司 类美登素衍生物及其制备方法和用途
EP3964237B1 (en) 2013-03-15 2026-02-18 Regeneron Pharmaceuticals, Inc. Biologically active molecules, conjugates thereof, and therapeutic uses
WO2014194030A2 (en) 2013-05-31 2014-12-04 Immunogen, Inc. Conjugates comprising cell-binding agents and cytotoxic agents
WO2014197866A1 (en) 2013-06-06 2014-12-11 Igenica Biotherapeutics, Inc. Modified antibodies and related compounds, compositions, and methods of use
SG10201708143QA (en) 2013-06-06 2017-11-29 Pf Medicament Anti-c10orf54 antibodies and uses thereof
WO2014197854A1 (en) 2013-06-06 2014-12-11 Igenica Biotherapeutics, Inc. Novel linkers for antibody-drug conjugates and related compounds, compositions, and methods of use
US20140363454A1 (en) 2013-06-06 2014-12-11 Igenica Biotherapeutics, Inc. Antibody-Drug Conjugates, Compositions and Methods of Use
US9545451B2 (en) 2013-08-21 2017-01-17 Regeneron Pharmaceuticals, Inc. Anti-PRLR antibodies and methods for killing PRLR-expressing cells
KR102252925B1 (ko) 2013-08-26 2021-05-18 리제너론 파마슈티칼스 인코포레이티드 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도
CN105744935B (zh) 2013-11-27 2022-09-30 雷德伍德生物科技股份有限公司 肼基-吡咯并化合物及用于生成缀合物的方法
CN105793268B (zh) 2013-12-02 2019-03-15 香港浸会大学 具有两个稠合大环的抗癌性美登木素类化合物
WO2015187596A2 (en) 2014-06-02 2015-12-10 Regeneron Pharmaceuticals, Inc. Biologically active molecule conjugates, reagents and methods of manufacture, and therapeutic uses
KR20240142591A (ko) 2015-03-27 2024-09-30 리제너론 파아마슈티컬스, 인크. 메이탄시노이드 유도체, 이의 컨주게이트, 및 사용 방법
MY198605A (en) 2016-01-25 2023-09-08 Regeneron Pharma Maytansinoid derivatives conjugates thereof, and methods of use

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010126551A1 (en) 2009-04-30 2010-11-04 Immunogen, Inc. Potent conjugates and hydrophilic linkers
CN103254311A (zh) 2013-05-09 2013-08-21 齐鲁制药有限公司 一种制备抗体-美登素类生物碱药物偶联物的方法

Also Published As

Publication number Publication date
CA2921412C (en) 2024-05-28
US11596635B2 (en) 2023-03-07
EP3038624B1 (en) 2024-09-25
WO2015031396A1 (en) 2015-03-05
SG11201601230RA (en) 2016-03-30
JP6608823B2 (ja) 2019-11-20
US20160354482A1 (en) 2016-12-08
EP3038624A1 (en) 2016-07-06
HK1220115A1 (en) 2017-04-28
EA201600191A1 (ru) 2016-07-29
MX2016002149A (es) 2016-10-28
NZ716768A (en) 2021-10-29
BR112016004023A2 (pt) 2022-11-16
CL2016000408A1 (es) 2017-02-24
AU2014311361A1 (en) 2016-03-03
AU2014311361B2 (en) 2018-11-29
EA038192B1 (ru) 2021-07-21
IL244203A0 (en) 2016-04-21
ES2989322T3 (es) 2024-11-26
MX373528B (es) 2020-04-21
EA201600191A8 (ru) 2018-04-30
US20230321109A1 (en) 2023-10-12
JP2016528304A (ja) 2016-09-15
KR20160045146A (ko) 2016-04-26
IL244203B (en) 2018-12-31
CN105530942B (zh) 2019-10-11
PH12016500380A1 (en) 2016-05-16
NZ756518A (en) 2021-10-29
CN105530942A (zh) 2016-04-27
CA2921412A1 (en) 2015-03-05
US20190151323A1 (en) 2019-05-23
ZA201601534B (en) 2023-11-29

Similar Documents

Publication Publication Date Title
US20230321109A1 (en) Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses
JP7728821B2 (ja) 抗体-薬物コンジュゲートの改良製造方法
EP4162954A1 (en) Camptothecin drug having high-stability hydrophilic connecting unit and conjugate thereof
AU2017211120B2 (en) Maytansinoid derivatives, conjugates thereof, and methods of use
KR20200083605A (ko) 프로그램가능한 중합체성 약물
TWI662968B (zh) 配體-細胞毒性藥物偶聯物、其製備方法及其應用
KR20200067132A (ko) 프로그램가능한 중합체성 약물
TW202342419A (zh) 抗體-藥物結合物之新穎製造方法
KR20200064059A (ko) 프로그램가능한 수지상 약물
NZ756914A (en) Printing-fluid cartridge, set of printing-fluid cartridges, and system including the printing-fluid cartridge and printing-fluid consuming apparatus
NZ757070B2 (en) Printing-fluid cartridge, set of printing-fluid cartridges, and system including the printing-fluid cartridge and printing-fluid consuming apparatus
HK1220115B (en) Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses
NZ756518B2 (en) Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses
NZ756914B2 (en) Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses
NZ716768B2 (en) Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses
JP7667870B2 (ja) Dna毒性二量体及びその複合体
NZ757070A (en) Fire extinguisher with internal mixing and gas cartridge
RU2851263C2 (ru) Конъюгат антитело-лекарственное средство и его применение
TW202615104A (zh) 曲妥珠單抗—藥物綴合物
JP2025533577A (ja) 抗cd33抗体及び抗cd33抗体-薬物複合体ならびにその使用
HK40083545A (en) Camptothecin drug having high-stability hydrophilic connecting unit and conjugate thereof
IL307317A (en) Dna toxic dimer compound and conjugate thereof

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20160325

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20190822

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20200717

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20210216

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20210511

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20210512

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
PR1001 Payment of annual fee

Payment date: 20240424

Start annual number: 4

End annual number: 4