EA201792101A1 - Биологически расщепляемые тетрапептидные связывающие агенты - Google Patents

Биологически расщепляемые тетрапептидные связывающие агенты

Info

Publication number
EA201792101A1
EA201792101A1 EA201792101A EA201792101A EA201792101A1 EA 201792101 A1 EA201792101 A1 EA 201792101A1 EA 201792101 A EA201792101 A EA 201792101A EA 201792101 A EA201792101 A EA 201792101A EA 201792101 A1 EA201792101 A1 EA 201792101A1
Authority
EA
Eurasian Patent Office
Prior art keywords
tetrapeptid
fissible
biologically
binding agents
compound
Prior art date
Application number
EA201792101A
Other languages
English (en)
Other versions
EA036949B1 (ru
Inventor
Джеффри С. Карлсон
Андрей В. Блохин
Original Assignee
Эрроухэд Фармасьютикалз, Инк.
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 Эрроухэд Фармасьютикалз, Инк. filed Critical Эрроухэд Фармасьютикалз, Инк.
Publication of EA201792101A1 publication Critical patent/EA201792101A1/ru
Publication of EA036949B1 publication Critical patent/EA036949B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1008—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • 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
    • A61K47/54—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 compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • 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
    • A61K47/54—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 compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/101—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Immunology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Описаны тетрапептидные линкеры для обратимого присоединения первого соединения к аминосодержащему второму соединению. Также описаны соединения, содержащие тетрапептидные линкеры, и способы применения тетрапептидных линкеров.
EA201792101A 2015-05-29 2016-05-27 Биологически расщепляемые тетрапептидные связывающие агенты EA036949B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562168244P 2015-05-29 2015-05-29
US201562235833P 2015-10-01 2015-10-01
PCT/US2016/034517 WO2016196243A1 (en) 2015-05-29 2016-05-27 Biologically cleavable tetrapeptide linking agents

Publications (2)

Publication Number Publication Date
EA201792101A1 true EA201792101A1 (ru) 2018-06-29
EA036949B1 EA036949B1 (ru) 2021-01-19

Family

ID=57398322

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201792101A EA036949B1 (ru) 2015-05-29 2016-05-27 Биологически расщепляемые тетрапептидные связывающие агенты

Country Status (15)

Country Link
US (2) US10005815B2 (ru)
EP (1) EP3302516B1 (ru)
JP (1) JP6966427B2 (ru)
KR (1) KR102633963B1 (ru)
CN (1) CN107614002B (ru)
AU (1) AU2016270597B2 (ru)
BR (1) BR112017025719A2 (ru)
CA (1) CA2984499A1 (ru)
EA (1) EA036949B1 (ru)
IL (1) IL255999A (ru)
MX (1) MX2017014638A (ru)
SG (1) SG11201708602XA (ru)
TW (1) TWI732761B (ru)
WO (1) WO2016196243A1 (ru)
ZA (1) ZA201707149B (ru)

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
AUPP616498A0 (en) * 1998-09-25 1998-10-15 University Of Queensland, The Synthesis of cyclic peptides
GB9903087D0 (en) * 1999-02-12 1999-03-31 Glaxo Group Ltd Process
US8137695B2 (en) 2006-08-18 2012-03-20 Arrowhead Madison Inc. Polyconjugates for in vivo delivery of polynucleotides
WO2002015700A1 (en) 2000-08-24 2002-02-28 Coulter Pharmaceutical, Inc. Prodrugs activated by plasmin and their use in cancer chemotherapy
GB0310593D0 (en) * 2003-05-08 2003-06-11 Leuven K U Res & Dev Peptidic prodrugs
CA2559955C (en) 2004-03-15 2016-02-16 City Of Hope Methods and compositions for the specific inhibition of gene expression by double-stranded rna
WO2009117531A1 (en) * 2008-03-18 2009-09-24 Seattle Genetics, Inc. Auristatin drug linker conjugates
US20100227920A1 (en) 2008-09-29 2010-09-09 The Regents Of The University Of California Aldehyde dehydrogenase inhibitors as novel depigmenting agents
US20100249214A1 (en) 2009-02-11 2010-09-30 Dicerna Pharmaceuticals Multiplex dicer substrate rna interference molecules having joining sequences
JP5855463B2 (ja) 2008-12-18 2016-02-09 ダイセルナ ファーマシューティカルズ， インコーポレイテッドＤｉｃｅｒｎａ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． 遺伝子発現の特異的阻害のための拡張ｄｉｃｅｒ基質薬剤および方法
EP2382993A1 (en) * 2010-04-19 2011-11-02 KTB Tumorforschungsgesellschaft mbH Combination of drugs with protein-binding prodrugs
CA3131967A1 (en) 2010-12-29 2012-07-05 F. Hoffman-La Roche Ag Small molecule conjugates for intracellular delivery of nucleic acids
EP3045468B1 (en) * 2011-04-05 2020-01-15 Fraunhofer Gesellschaft zur Förderung der Angewand Novel peptides and their use in diagnosis and treatment
US9649385B2 (en) * 2011-09-07 2017-05-16 Prolynx Llc Hydrogels with biodegradable crosslinking
WO2014004639A1 (en) * 2012-06-26 2014-01-03 Sutro Biopharma, Inc. Modified fc proteins comprising site-specific non-natural amino acid residues, conjugates of the same, methods of their preparation and methods of their use
US9018172B2 (en) * 2012-09-26 2015-04-28 Massachusetts Institute Of Technology Modification of peptides via SNAr reactions of thiols with fluorinated aromatics
US9999680B2 (en) * 2013-02-28 2018-06-19 Immunogen, Inc. Conjugates comprising cell-binding agents and maytansinoids as cytotoxic agents
US20160132631A1 (en) * 2013-06-10 2016-05-12 Iogenetics, Llc Bioinformatic processes for determination of peptide binding
CN105451743B (zh) 2013-08-07 2019-11-19 箭头研究公司 用于在活体中递送RNAi触发子至肿瘤细胞的聚偶联物
WO2015038426A1 (en) * 2013-09-13 2015-03-19 Asana Biosciences, Llc Self-immolative linkers containing mandelic acid derivatives, drug-ligand conjugates for targeted therapies and uses thereof

Also Published As

Publication number Publication date
EA036949B1 (ru) 2021-01-19
EP3302516A1 (en) 2018-04-11
BR112017025719A2 (pt) 2018-08-07
US10005815B2 (en) 2018-06-26
TW201716426A (zh) 2017-05-16
TWI732761B (zh) 2021-07-11
JP2018517769A (ja) 2018-07-05
CN107614002A (zh) 2018-01-19
CA2984499A1 (en) 2016-12-08
KR20180010235A (ko) 2018-01-30
US20160347793A1 (en) 2016-12-01
KR102633963B1 (ko) 2024-02-05
ZA201707149B (en) 2019-02-27
EP3302516B1 (en) 2020-12-30
US20180258138A1 (en) 2018-09-13
WO2016196243A1 (en) 2016-12-08
EP3302516A4 (en) 2019-07-31
AU2016270597A1 (en) 2017-11-09
CN107614002B (zh) 2022-01-04
AU2016270597B2 (en) 2022-05-26
IL255999A (en) 2018-01-31
MX2017014638A (es) 2018-01-23
JP6966427B2 (ja) 2021-11-17
SG11201708602XA (en) 2017-12-28

Similar Documents

Publication Publication Date Title
EA201891209A1 (ru) Модуляторы хемокиновых рецепторов
CL2017000654A1 (es) Indazoles sustituidos con bencilo como inhibidores de bub1.
EA201990615A1 (ru) Пирролобензодиазепиновые конъюгаты
EA201890749A1 (ru) ИНГИБИТОРЫ АЦЕТИЛ-КоА-КАРБОКСИЛАЗЫ (ACC) И ИХ ПРИМЕНЕНИЕ
EA201891211A1 (ru) Ингибиторы cxcr2
EA201891024A1 (ru) Соединения-ингибиторы tank-связывающей киназы
EA201591420A1 (ru) Гетероарильные соединения и их применение
CR20170111A (es) Derivados de benzodiazepina citotóxicos
EA201791857A1 (ru) Гемостатическая композиция и гемостатическое средство (варианты)
EA201791029A1 (ru) Антитела против интерлейкина-33 и их применение
EA201591961A1 (ru) Ингибиторы акк и их применение
EA201890895A1 (ru) Мультивалентные и моновалентные мультиспецифические комплексы и их применение
EA201692203A1 (ru) Соединения, ингибирующие tank-связывающую киназу
EA201591728A1 (ru) Гетероциклические соединения и способы их применения
EA201591959A1 (ru) Ингибиторы акк и их применение
EA201591960A1 (ru) Ингибиторы акк и их применение
EA201890247A1 (ru) Ингибиторы дезоксиуридинтрифосфатазы, содержащие гидантоин
EA201400579A1 (ru) Антитела к il-36r
EA201591467A1 (ru) Анти-lag-3 связывающие белки
EA201590993A1 (ru) Гетеродимерные иммуноглобулины
EA201491811A1 (ru) АНТИ-LgR5 АНТИТЕЛА И ИММУНОКОНЪЮГАТЫ
EA201591632A1 (ru) Цитотоксические и антимитотические соединения и способы их применения
EA201591962A1 (ru) Ингибиторы акк и их применение
EA201201016A1 (ru) Антидоты антикоагулянтов
EA201401204A1 (ru) Антитела к il-23p19

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM