KR20170137725A - 데스아세톡시투불리신 h 및 이의 유사체 - Google Patents

데스아세톡시투불리신 h 및 이의 유사체 Download PDF

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KR20170137725A
KR20170137725A KR1020177027116A KR20177027116A KR20170137725A KR 20170137725 A KR20170137725 A KR 20170137725A KR 1020177027116 A KR1020177027116 A KR 1020177027116A KR 20177027116 A KR20177027116 A KR 20177027116A KR 20170137725 A KR20170137725 A KR 20170137725A
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South Korea
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substituted
cycloalkyl
alkyl
groups
alkanediyl
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Korean (ko)
Inventor
키리아코스 씨. 니콜라우
디오노시오스 벌루미스
준 인
로한 에란데
데바시스 만달
필립 클란
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윌리엄 마쉬 라이스 유니버시티
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Publication of KR20170137725A publication Critical patent/KR20170137725A/ko
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    • 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
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K47/6851—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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cell Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020177027116A 2015-02-25 2016-02-25 데스아세톡시투불리신 h 및 이의 유사체 Withdrawn KR20170137725A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562120613P 2015-02-25 2015-02-25
US62/120,613 2015-02-25
US201662275667P 2016-01-06 2016-01-06
US62/275,667 2016-01-06
PCT/US2016/019604 WO2016138288A1 (en) 2015-02-25 2016-02-25 Desacetoxytubulysin h and analogs thereof

Publications (1)

Publication Number Publication Date
KR20170137725A true KR20170137725A (ko) 2017-12-13

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KR1020177027116A Withdrawn KR20170137725A (ko) 2015-02-25 2016-02-25 데스아세톡시투불리신 h 및 이의 유사체

Country Status (22)

Country Link
US (1) US10808007B2 (cg-RX-API-DMAC7.html)
EP (1) EP3261443B1 (cg-RX-API-DMAC7.html)
JP (1) JP2018509404A (cg-RX-API-DMAC7.html)
KR (1) KR20170137725A (cg-RX-API-DMAC7.html)
CN (1) CN107529754A (cg-RX-API-DMAC7.html)
AU (1) AU2016222575A1 (cg-RX-API-DMAC7.html)
BR (1) BR112017018305A2 (cg-RX-API-DMAC7.html)
CA (1) CA2977589A1 (cg-RX-API-DMAC7.html)
CL (1) CL2017002170A1 (cg-RX-API-DMAC7.html)
CO (1) CO2017008600A2 (cg-RX-API-DMAC7.html)
CR (1) CR20170438A (cg-RX-API-DMAC7.html)
DO (1) DOP2017000202A (cg-RX-API-DMAC7.html)
EA (1) EA201791896A1 (cg-RX-API-DMAC7.html)
EC (1) ECSP17057131A (cg-RX-API-DMAC7.html)
GT (1) GT201700190A (cg-RX-API-DMAC7.html)
HK (1) HK1248069A1 (cg-RX-API-DMAC7.html)
IL (1) IL254089A0 (cg-RX-API-DMAC7.html)
MX (1) MX2017011024A (cg-RX-API-DMAC7.html)
PE (1) PE20180355A1 (cg-RX-API-DMAC7.html)
PH (1) PH12017501539A1 (cg-RX-API-DMAC7.html)
SG (1) SG11201706820RA (cg-RX-API-DMAC7.html)
WO (1) WO2016138288A1 (cg-RX-API-DMAC7.html)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10829519B2 (en) 2015-09-18 2020-11-10 Wake Forest University Health Sciences Angiotensin (1-7) analogs and methods relating thereto
CA2914601A1 (en) * 2015-12-11 2017-06-11 Wake Forest University Health Sciences Angiotensin-(1-7) analogs and methods relating thereto
JP2020525513A (ja) * 2017-07-03 2020-08-27 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ 癌および他の疾患を治療するためのａｔｆ４阻害剤としてのｎ−（３−（２−（４−クロロフェノキシ）アセトアミドビシクロ［１．１．１］ペンタン−１−イル）−２−シクロブタン−１−カルボキサミド誘導体および関連化合物
PH12020550028B1 (en) 2017-08-09 2024-05-24 Denali Therapeutics Inc Compounds, compositions and methods
DK3676297T3 (da) 2017-09-01 2023-08-14 Denali Therapeutics Inc Forbindelser, sammensætninger og fremgangsmåder
CN111601803A (zh) 2017-09-08 2020-08-28 西雅图基因公司 微管溶素及其中间体的制备方法
WO2019108685A1 (en) * 2017-11-29 2019-06-06 William March Rice University Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith
MY208067A (en) 2018-12-21 2025-04-11 Regeneron Pharma Tubulysins and protein-tubulysin conjugates
US12091392B2 (en) 2019-02-13 2024-09-17 Denali Therapeutics Inc. Compounds, compositions and methods
KR20210126036A (ko) 2019-02-13 2021-10-19 데날리 테라퓨틱스 인크. 화합물, 조성물 및 방법
TWI750728B (zh) * 2019-07-11 2021-12-21 大陸商蘇州亞盛藥業有限公司 2-吲哚啉螺環酮類化合物的製備方法及其中間體
US11694341B2 (en) 2019-12-23 2023-07-04 Texas Instmments Incorporated Cascaded architecture for disparity and motion prediction with block matching and convolutional neural network (CNN)
CN112645833A (zh) * 2021-01-29 2021-04-13 上海吉奉生物科技有限公司 一种(s)-2,6-二氨基-5-氧己酸的合成方法

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US7776814B2 (en) * 2002-07-09 2010-08-17 R&D-Biopharmaceuticals Gmbh Tubulysin conjugates
DK1523493T3 (da) 2002-07-09 2013-12-02 Alexander Doemling Nye tubulysinanaloge
WO2008106080A2 (en) 2007-02-27 2008-09-04 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Synthesis of desacetoxytubulysin h and analogs thereof
EP2532673A3 (en) 2007-05-10 2014-01-08 R & D Biopharmaceuticals Gmbh Tubulysine derivatives
WO2009012958A2 (en) 2007-07-20 2009-01-29 Helmholtz-Zentrum für Infektionsforschung GmbH Tubulysin d analogues
CN101909441B (zh) * 2007-10-25 2015-05-13 恩多塞特公司 微管蛋白抑制剂及其制备方法
EP2174947A1 (en) 2008-09-25 2010-04-14 Universität des Saarlandes Bioactive pre-tubulysins and use thereof
IT1394860B1 (it) 2009-07-22 2012-07-20 Kemotech S R L Composti farmaceutici
US8394922B2 (en) * 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
EP2322537A1 (en) * 2009-11-12 2011-05-18 R & D Biopharmaceuticals Gmbh Tubulin inhibitors
WO2011069116A1 (en) 2009-12-04 2011-06-09 Endocyte, Inc. Binding ligand linked drug delivery conjugates of tubulysins
EP2409983A1 (en) * 2010-07-19 2012-01-25 Leibniz-Institut für Pflanzenbiochemie (IPB) Tubulysin analogues
JP2013535220A (ja) 2010-08-06 2013-09-12 エンドサイト，インコーポレイテッド ツブリシンを調製するためのプロセス
US20140080175A1 (en) * 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
BR112015019432A2 (pt) 2013-02-14 2017-08-22 Bristol Myers Squibb Co Compostos de tubulisina, métodos de produção e uso
EA032203B1 (ru) 2014-04-11 2019-04-30 МЕДИММЬЮН ЭлЭлСи Производные тубулизина

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Publication number Publication date
CL2017002170A1 (es) 2018-06-08
SG11201706820RA (en) 2017-09-28
MX2017011024A (es) 2017-10-20
WO2016138288A1 (en) 2016-09-01
CA2977589A1 (en) 2016-09-01
EP3261443A1 (en) 2018-01-03
IL254089A0 (en) 2017-10-31
HK1248069A1 (zh) 2018-10-12
CR20170438A (es) 2018-01-30
DOP2017000202A (es) 2017-09-29
PE20180355A1 (es) 2018-02-21
US10808007B2 (en) 2020-10-20
ECSP17057131A (es) 2019-03-29
BR112017018305A2 (pt) 2018-04-17
GT201700190A (es) 2018-11-26
JP2018509404A (ja) 2018-04-05
AU2016222575A1 (en) 2017-09-07
EA201791896A1 (ru) 2018-02-28
EP3261443A4 (en) 2018-09-26
PH12017501539A1 (en) 2018-02-05
US20180127463A1 (en) 2018-05-10
CO2017008600A2 (es) 2018-02-09
EP3261443B1 (en) 2021-04-28
CN107529754A (zh) 2018-01-02

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PA0105 International application

Patent event date: 20170925

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PC1203 Withdrawal of no request for examination