EA201700459A1 - Реагенты аминокислотного ацилирования и способы их использования - Google Patents

Реагенты аминокислотного ацилирования и способы их использования

Info

Publication number
EA201700459A1
EA201700459A1 EA201700459A EA201700459A EA201700459A1 EA 201700459 A1 EA201700459 A1 EA 201700459A1 EA 201700459 A EA201700459 A EA 201700459A EA 201700459 A EA201700459 A EA 201700459A EA 201700459 A1 EA201700459 A1 EA 201700459A1
Authority
EA
Eurasian Patent Office
Prior art keywords
reagents
methods
amino acid
acid acylation
acylation
Prior art date
Application number
EA201700459A
Other languages
English (en)
Other versions
EA032630B1 (ru
EA032630B9 (ru
Inventor
Томас Ниттоли
Сринат Тирумалай Райан
Томас П. Маркотан
Нарешкумар Джаин
Original Assignee
Регенерон 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 Регенерон Фармасьютикалз, Инк. filed Critical Регенерон Фармасьютикалз, Инк.
Publication of EA201700459A1 publication Critical patent/EA201700459A1/ru
Publication of EA032630B1 publication Critical patent/EA032630B1/ru
Publication of EA032630B9 publication Critical patent/EA032630B9/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/46—Sulfur atoms
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Заявляются соединения, полезные для дополнения аминокислот до нуклеофилов.
EA201700459A 2015-03-17 2016-03-17 Реагенты аминокислотного ацилирования и способы их использования EA032630B9 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562134065P 2015-03-17 2015-03-17
PCT/US2016/022797 WO2016149464A1 (en) 2015-03-17 2016-03-17 Amino acid acylation reagents and methods of using the same

Publications (3)

Publication Number Publication Date
EA201700459A1 true EA201700459A1 (ru) 2018-04-30
EA032630B1 EA032630B1 (ru) 2019-06-28
EA032630B9 EA032630B9 (ru) 2019-11-27

Family

ID=55661591

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201700459A EA032630B9 (ru) 2015-03-17 2016-03-17 Реагенты аминокислотного ацилирования и способы их использования

Country Status (12)

Country Link
US (1) US10526344B2 (ru)
EP (1) EP3271339B1 (ru)
JP (1) JP6649961B2 (ru)
KR (1) KR20170129769A (ru)
CN (1) CN107750247A (ru)
AU (1) AU2016233227B2 (ru)
CA (1) CA2978182A1 (ru)
EA (1) EA032630B9 (ru)
IL (1) IL254205B (ru)
MX (1) MX2017011820A (ru)
SG (1) SG11201707585UA (ru)
WO (1) WO2016149464A1 (ru)

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US2649458A (en) * 1951-04-30 1953-08-18 Monsanto Chemicals 2-thiono-5-oxazolidones
NL7002228A (ru) * 1970-02-18 1971-08-20
JPS55164686A (en) 1979-06-11 1980-12-22 Takeda Chem Ind Ltd Novel maytansinoid compound and its preparation
US4399163A (en) * 1980-11-05 1983-08-16 Pfizer Inc. Branched amides of L-aspartyl-D-amino acid dipeptides
US4946942A (en) * 1988-03-11 1990-08-07 Bioresearch, Inc. Urethane-protected amino acid-N-carboxyanhydrides
US5663333A (en) 1992-10-22 1997-09-02 The Dupont Merck Pharmaceutical Company Substituted 1,4-diazapine caprolactams useful for treatment of HIV disease
US6083950A (en) 1997-11-13 2000-07-04 Ranbaxy Laboratories Limited 1-(4-arylpiperazin-1-yl)-ω-[n-(α,ω-dicarboximido)]-alka nes useful as uro-selective α1-adrenoceptor blockers
ES2166328B1 (es) * 2000-05-11 2003-09-16 Consejo Superior Investigacion Inhibidores heterociclicos del enzima gsk 3 utiles en el tratamiento de procesos neurodegenerativos e hiperproliferativos
EP1286964B1 (en) 2000-05-11 2007-07-04 Consejo Superior de Investigaciones Cientificas Heterocyclic inhibitors of glycogen synthase kinase gsk-3
DE60102825T2 (de) 2000-07-31 2005-03-31 Brandeis University, Waltham Kinetische racematspaltung chiraler 2- und 3- substituierter carbonsäuren
US6333410B1 (en) 2000-08-18 2001-12-25 Immunogen, Inc. Process for the preparation and purification of thiol-containing maytansinoids
TWI298067B (en) 2002-01-31 2008-06-21 Daiso Co Ltd New optically active compound, method for kinetic resolution of carbonic acid derivatives and catalyst thereof
US7301019B2 (en) * 2005-01-21 2007-11-27 Immunogen, Inc. Method for the preparation of maytansinoid esters
CA2617953C (en) 2005-08-09 2013-12-17 Millennium Pharmaceuticals, Inc. Method of acylating maytansinol with chiral amino acids
NZ574619A (en) 2006-07-18 2012-03-30 Univ Rochester THIADIAZOLIDINEDIONE DERIVATIVES including 4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione (TDZD-8)
ES2544608T3 (es) 2010-11-17 2015-09-02 Genentech, Inc. Conjugados de anticuerpo y de alaninil-maitansinol
HUE055443T2 (hu) * 2012-09-26 2021-11-29 Immunogen Inc Javított eljárások maytansinol acilezéséhez
US9310374B2 (en) 2012-11-16 2016-04-12 Redwood Bioscience, Inc. Hydrazinyl-indole compounds and methods for producing a conjugate
CN103333245B (zh) 2012-12-21 2015-03-18 百奥泰生物科技(广州)有限公司 一种针对细胞受体并抑制癌细胞生长的药物分子及其制备方法和用途
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
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
CN103333246B (zh) 2012-12-21 2015-09-16 百奥泰生物科技(广州)有限公司 一种抗egfr受体的肿瘤生长抑制剂及其制备方法和用途
CN103288957B (zh) 2012-12-21 2015-01-28 百奥泰生物科技(广州)有限公司 一种抑制肿瘤生长的抗体药物衍生物及其制备方法和用途
EP2777714A1 (en) * 2013-03-15 2014-09-17 NBE-Therapeutics LLC Method of producing an immunoligand/payload conjugate by means of a sequence-specific transpeptidase enzyme

Also Published As

Publication number Publication date
JP6649961B2 (ja) 2020-02-19
AU2016233227A1 (en) 2017-09-14
SG11201707585UA (en) 2017-10-30
CN107750247A (zh) 2018-03-02
CA2978182A1 (en) 2016-09-22
WO2016149464A1 (en) 2016-09-22
JP2018510157A (ja) 2018-04-12
KR20170129769A (ko) 2017-11-27
IL254205A0 (en) 2017-10-31
EA032630B1 (ru) 2019-06-28
AU2016233227B2 (en) 2020-03-12
US10526344B2 (en) 2020-01-07
EP3271339A1 (en) 2018-01-24
EP3271339B1 (en) 2021-11-24
MX2017011820A (es) 2018-03-15
US20180237456A1 (en) 2018-08-23
IL254205B (en) 2019-11-28
EA032630B9 (ru) 2019-11-27

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