SG11201601230RA - Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses - Google Patents

Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses

Info

Publication number
SG11201601230RA
SG11201601230RA SG11201601230RA SG11201601230RA SG11201601230RA SG 11201601230R A SG11201601230R A SG 11201601230RA SG 11201601230R A SG11201601230R A SG 11201601230RA SG 11201601230R A SG11201601230R A SG 11201601230RA SG 11201601230R A SG11201601230R A SG 11201601230RA
Authority
SG
Singapore
Prior art keywords
synthesis
methods
pharmaceutical compositions
therapeutic uses
macrolide
Prior art date
Application number
SG11201601230RA
Other languages
English (en)
Inventor
Thomas Nittoli
Nareshkumar F Jain
Thomas Patrick Markotan
Original Assignee
Regeneron Pharma
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 Regeneron Pharma filed Critical Regeneron Pharma
Publication of SG11201601230RA publication Critical patent/SG11201601230RA/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/537Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5365Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68033Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6807Drugs 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
    • A61K47/6809Antibiotics, e.g. antitumor antibiotics anthracyclins, adriamycin, doxorubicin or daunomycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6851Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • Cell Biology (AREA)
  • Molecular Biology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (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)
SG11201601230RA 2013-08-26 2014-08-26 Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses SG11201601230RA (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361869954P 2013-08-26 2013-08-26
US201461934313P 2014-01-31 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 (1)

Publication Number Publication Date
SG11201601230RA true SG11201601230RA (en) 2016-03-30

Family

ID=51542449

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201601230RA SG11201601230RA (en) 2013-08-26 2014-08-26 Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses

Country Status (17)

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

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6847388B2 (ja) 2013-03-15 2021-03-31 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 生物活性分子、そのコンジュゲート、及び治療用途
BR112016004023A2 (pt) 2013-08-26 2022-11-16 Regeneron Pharma Composição, métodos para preparar uma composição e para tratar uma doença, e, composto
BR112017020149A8 (pt) * 2015-03-27 2023-05-02 Regeneron Pharma Derivados de maitansinoide, conjugados dos mesmos e métodos de uso
IL296285A (en) 2015-07-06 2022-11-01 Regeneron Pharma Multispecific antigen-binding molecules and uses thereof
BR112018014759B1 (pt) 2016-01-25 2024-02-27 Regeneron Pharmaceuticals, Inc Compostos derivados de maitasinoide e seus conjugados, composição compreendendo os mesmos, seus métodos de fabricação e uso
EP3448891A1 (en) 2016-04-28 2019-03-06 Regeneron Pharmaceuticals, Inc. Methods of making multispecific antigen-binding molecules
JP7066690B2 (ja) 2016-09-23 2022-05-13 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 抗muc16(ムチン16)抗体
MY199468A (en) 2016-09-23 2023-10-31 Regeneron Pharma Anti-steap2 antibodies, antibody-drug conjugates, and bispecific antigen-binding molecules that bind steap2 and cd3, and uses thereof
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
DK3635009T3 (da) 2017-06-07 2026-03-30 Regeneron Pharma Sammensætninger og fremgangsmåder til internalisering af enzymer
MX2020004691A (es) 2017-11-07 2020-08-20 Regeneron Pharma Enlazadores hidrofilicos para conjugados anticuerpo-farmaco.
KR102871690B1 (ko) 2018-04-30 2025-10-16 리제너론 파마슈티칼스 인코포레이티드 Her2 및/또는 aplp2에 결합하는 항체 및 이중특이적 항원-결합 분자 및 접합체 그리고 이들의 용도
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
EP3843749A4 (en) * 2018-08-31 2022-07-27 Osteoanalgesia, LLC DIASTEREOMERS CONJUGATE COMPOSITIONS AND METHODS OF MAKING AND USE THEREOF
CA3128519A1 (en) 2019-02-21 2020-08-27 Regeneron Pharmaceuticals, Inc. Methods of treating ocular cancer using anti-met antibodies and bispecific antigen binding molecules that bind met
AU2020349462A1 (en) 2019-09-16 2022-03-03 Regeneron Pharmaceuticals, Inc. Radiolabeled MET binding proteins for immuno-PET imaging
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
KR20220148200A (ko) 2020-02-28 2022-11-04 리제너론 파마슈티칼스 인코포레이티드 Her2에 결합하는 이중특이적 항원 결합 분자 및 이의 사용 방법
CN115968304A (zh) 2020-04-16 2023-04-14 瑞泽恩制药公司 狄尔斯-阿尔德缀合方法
CN116390771A (zh) 2020-07-13 2023-07-04 瑞泽恩制药公司 与蛋白中的谷氨酰胺残基缀合的喜树碱类似物及其用途
CA3190569A1 (en) 2020-10-22 2022-04-28 Christopher Daly Anti-fgfr2 antibodies and methods of use thereof
US20220143194A1 (en) 2020-11-10 2022-05-12 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

Family Cites Families (69)

* 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
US5208020A (en) 1989-10-25 1993-05-04 Immunogen Inc. Cytotoxic agents comprising maytansinoids and their therapeutic use
CA2026147C (en) 1989-10-25 2006-02-07 Ravi J. Chari 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
KR20130065723A (ko) 2003-06-27 2013-06-19 암젠 프레몬트 인코포레이티드 상피 성장 인자 수용체의 결실 돌연변이체 지향 항체 및 그 용도
GB0316294D0 (en) 2003-07-11 2003-08-13 Polytherics Ltd Conjugated biological molecules and their preparation
AR048098A1 (es) 2004-03-15 2006-03-29 Wyeth Corp Conjugados de caliqueamicina
NZ579482A (en) 2004-06-01 2011-02-25 Genentech Inc Antibody drug conjugates and methods
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
US8603483B2 (en) 2004-12-09 2013-12-10 Janssen Biotech, Inc. Anti-integrin immunoconjugates, methods and uses
US7750116B1 (en) 2006-02-18 2010-07-06 Seattle Genetics, Inc. Antibody drug conjugate metabolites
BRPI0717638A2 (pt) 2006-10-27 2013-11-12 Genentech Inc Anticorpors e imunoconjugados e usos para os mesmos
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
CL2008001334A1 (es) 2007-05-08 2008-09-22 Genentech Inc Anticuerpo anti-muc16 disenado con cisteina; conjugado que lo comprende; metodo de produccion; formulacion farmaceutica que lo comprende; y su uso para tratar el cancer.
EP2167963B1 (en) 2007-05-23 2019-04-17 Ventana Medical Systems, Inc. Polymeric carriers for immunohistochemistry and in situ hybridization
DK2644194T3 (en) * 2008-03-18 2017-07-03 Genentech Inc Combinations of an anti-HER2 antibody-drug conjugate and docetaxel
SG189817A1 (en) 2008-04-30 2013-05-31 Immunogen Inc Potent conjugates and hydrophilic linkers
AU2009275358C1 (en) 2008-07-21 2015-09-24 Polytherics Limited Novel reagents and method for conjugating biological molecules
EP2403538B1 (en) 2009-03-04 2017-10-04 Polytherics Limited Conjugated proteins and peptides
AU2010283632B2 (en) 2009-08-10 2016-08-25 Ucl Business Plc Reversible covalent linkage of functional molecules
TW201117814A (en) 2009-10-02 2011-06-01 Sanofi Aventis New maytansinoids and the use of said maytansinoids to prepare conjugates with an antibody
UY32914A (es) 2009-10-02 2011-04-29 Sanofi Aventis Anticuerpos que se usan específicamente al receptor epha2
CN102596922A (zh) * 2009-10-06 2012-07-18 免疫基因公司 有效的缀合物和亲水性连接体
US8501692B2 (en) 2009-12-14 2013-08-06 The Regents Of The University Of Michigan Compositions and methods for altering cocaine esterase activity
SI2528625T1 (sl) 2010-04-15 2013-11-29 Spirogen Sarl Pirolobenzodiazepini in njihovi konjugati
US20130244905A1 (en) 2010-07-06 2013-09-19 Ed Grabczyk Reporter for RNA Polymerase II Termination
SMT201700023T1 (it) 2010-08-02 2017-03-08 Regeneron Pharma Topi che producono proteine leganti vl
RS53519B1 (sr) 2010-09-01 2015-02-27 Bayer Intellectual Property Gmbh N-(tetrazol-5-il)- i n-(triazol-5-il)aril amidi karboksilne kiseline i njihova upotreba kao herbicida
EA201390575A1 (ru) 2010-10-29 2014-01-30 Иммьюноджен, Инк. Неантагонистические egfr-связывающие молекулы и их иммуноконъюгаты
AU2011323316B2 (en) 2010-11-03 2016-02-25 Immunogen, Inc. Cytotoxic agents comprising new ansamitocin derivatives
CA2836338C (en) 2011-05-16 2022-05-03 Koninklijke Philips N.V. Tetrazine derivatives used in bio-orthogonal drug activation
CN110078789A (zh) 2011-05-27 2019-08-02 Ambrx 公司 含有非天然氨基酸连接的海兔毒素衍生物的组合物、涉及该海兔毒素衍生物的方法及其用途
US8815226B2 (en) 2011-06-10 2014-08-26 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
JP6209159B2 (ja) 2011-06-21 2017-10-04 イミュノジェン・インコーポレーテッド ペプチドリンカーを有する新規メイタンシノイド誘導体およびその結合体
EP2751111B1 (en) 2011-10-14 2017-04-26 MedImmune Limited Asymmetrical bis-(5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one) derivatives for the treatment of proliferative or autoimmune diseases
BR112014009070B1 (pt) 2011-10-14 2021-11-23 Medimmune Limited Método de síntese e intermediários úteis na preparação de pirrolobenzo-diazepinas
CA2850373C (en) 2011-10-14 2019-07-16 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
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
RU2014124984A (ru) 2011-12-05 2016-01-27 Идженика Биотерапьютикс, Инк. Конъюгаты антитело-лекарственное средство и родственные соединения, композиции и способы
GB201210770D0 (en) 2012-06-18 2012-08-01 Polytherics Ltd Novel conjugation reagents
EP2861261A2 (en) 2012-06-19 2015-04-22 Polytherics Limited Process for preparation of antibody conjugates and antibody conjugates
CN105142672B (zh) 2012-10-23 2019-04-05 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
NO2789793T3 (https=) 2012-10-24 2018-01-27
CA2891280C (en) 2012-11-24 2018-03-20 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
CN104688740A (zh) 2012-12-21 2015-06-10 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
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
JP6847388B2 (ja) 2013-03-15 2021-03-31 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 生物活性分子、そのコンジュゲート、及び治療用途
CN103254311B (zh) * 2013-05-09 2015-05-13 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
WO2014194030A2 (en) 2013-05-31 2014-12-04 Immunogen, Inc. Conjugates comprising cell-binding agents and cytotoxic agents
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
SG11201509982UA (https=) 2013-06-06 2016-04-28 Igenica Biotherapeutics Inc
US10781259B2 (en) 2013-06-06 2020-09-22 Magenta Therapeutics, Inc. Modified antibodies 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
BR112016004023A2 (pt) 2013-08-26 2022-11-16 Regeneron Pharma Composição, métodos para preparar uma composição e para tratar uma doença, e, composto
CN115504924A (zh) 2013-11-27 2022-12-23 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
US9562059B2 (en) 2013-12-02 2017-02-07 Hong Kong Baptist University Anticancer maytansinoids with two fused macrocyclic rings
US9951141B2 (en) 2014-06-02 2018-04-24 Regeneron Pharmaceuticals, Inc. Antibody-drug conjugates, their preparation and their therapeutic use
BR112017020149A8 (pt) 2015-03-27 2023-05-02 Regeneron Pharma Derivados de maitansinoide, conjugados dos mesmos e métodos de uso
BR112018014759B1 (pt) 2016-01-25 2024-02-27 Regeneron Pharmaceuticals, Inc Compostos derivados de maitasinoide e seus conjugados, composição compreendendo os mesmos, seus métodos de fabricação e uso

Also Published As

Publication number Publication date
US20160354482A1 (en) 2016-12-08
CN105530942A (zh) 2016-04-27
MX373528B (es) 2020-04-21
EA201600191A1 (ru) 2016-07-29
KR102252925B1 (ko) 2021-05-18
ZA201601534B (en) 2023-11-29
AU2014311361B2 (en) 2018-11-29
HK1220115A1 (en) 2017-04-28
CA2921412C (en) 2024-05-28
EP3038624B1 (en) 2024-09-25
EP3038624A1 (en) 2016-07-06
CN105530942B (zh) 2019-10-11
JP6608823B2 (ja) 2019-11-20
IL244203A0 (en) 2016-04-21
PH12016500380A1 (en) 2016-05-16
WO2015031396A1 (en) 2015-03-05
CL2016000408A1 (es) 2017-02-24
NZ716768A (en) 2021-10-29
EA201600191A8 (ru) 2018-04-30
US20190151323A1 (en) 2019-05-23
US20230321109A1 (en) 2023-10-12
CA2921412A1 (en) 2015-03-05
IL244203B (en) 2018-12-31
AU2014311361A1 (en) 2016-03-03
ES2989322T3 (es) 2024-11-26
JP2016528304A (ja) 2016-09-15
NZ756518A (en) 2021-10-29
EA038192B1 (ru) 2021-07-21
MX2016002149A (es) 2016-10-28
KR20160045146A (ko) 2016-04-26
US11596635B2 (en) 2023-03-07
BR112016004023A2 (pt) 2022-11-16

Similar Documents

Publication Publication Date Title
IL244203A0 (en) Pharmaceutical compositions containing diastereomers of macrolides, methods for their synthesis and therapeutic uses
IL285390A (en) Arylquinazolines, their preparation and pharmaceutical preparations containing them
EP2981611A4 (en) ANTIBIOTICUM PROTOCOLS AND PHARMACEUTICAL FORMULATIONS AND TREATMENT METHODS THEREWITH
IL286759A (en) Therapeutic methods and preparations
IL240876B (en) History of aminopurine, their preparation and pharmaceutical preparations containing them
IL240290B (en) History of pyridazinone-amide and pharmaceutical preparations containing them
LT2986304T (lt) Farmacinė kompozicija, gydymo būdai ir jų panaudojimas
SG11201507358VA (en) Pharmaceutical composition of s-ketamine hydrochloride
SG10201802104QA (en) Pharmaceutical composition of s-ketamine hydrochloride
IL242347B (en) Macrocyclic compounds, their preparation and pharmaceutical compositions containing them
SG11201508167PA (en) Therapeutic compositions and uses thereof
HUE056143T2 (hu) Pimobendán javított gyógyászati készítményei
SG11201601047SA (en) Derivatives of uncialamycin, methods of synthesis and their use as antitumor agents
ZA201505318B (en) 2-substituted-6-biarylmethylamino-9-cyclopentyl-9h-purine derivatives, use thereof as medicaments, and pharmaceutical compositions
PT2859896T (pt) Composições farmacêuticas para o tratamento de distúrbios musculares
ZA201802033B (en) Heteroaryl compounds and their use as therapeutic drugs
IL243733A0 (en) Cyclopentane history, their preparation and medicines containing them
IL239054A0 (en) History of azaquinazoline carboxamide, their preparation and pharmaceutical preparations containing them
IL246406A0 (en) History of imidazopyrazinone, their preparation and pharmaceutical preparations containing them
IL243227B (en) History of diaminocyclopentane carboxamide, their preparation and pharmaceutical preparations containing them
IL246298A0 (en) History of piperidine, their preparation and pharmaceutical preparations containing them
SG11201602826VA (en) Icotinib-containing topical skin pharmaceutical compositions and uses thereof
IL239873A0 (en) The history of piperidinylcarbazole, their preparation and pharmaceutical preparations containing them
ZA201501597B (en) Macrolide derivatives,preparation thereof and therapeutic use thereof
GB201319255D0 (en) Therapeutic compositions and methods