JP2018509404A - デスアセトキシツブリシンｈおよびその類似体 - Google Patents

デスアセトキシツブリシンｈおよびその類似体 Download PDF

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JP2018509404A
JP2018509404A JP2017545239A JP2017545239A JP2018509404A JP 2018509404 A JP2018509404 A JP 2018509404A JP 2017545239 A JP2017545239 A JP 2017545239A JP 2017545239 A JP2017545239 A JP 2017545239A JP 2018509404 A JP2018509404 A JP 2018509404A
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substituted
cycloalkyl
alkanediyl
groups
alkyl
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JP2018509404A5 (enExample
Inventor
キリアコス シー． ニコラウ
キリアコス シー． ニコラウ
ディノシオス ヴォウロウミス
ディノシオス ヴォウロウミス
ジュン イン
ジュン イン
ローハン エランデ
ローハン エランデ
デバシス マンダル
デバシス マンダル
フィリップ クラン
フィリップ クラン
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William Marsh Rice University
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William Marsh Rice University
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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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cell Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2017545239A 2015-02-25 2016-02-25 デスアセトキシツブリシンｈおよびその類似体 Pending JP2018509404A (ja)

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 (2)

Publication Number Publication Date
JP2018509404A true JP2018509404A (ja) 2018-04-05
JP2018509404A5 JP2018509404A5 (enExample) 2019-04-04

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JP2017545239A Pending JP2018509404A (ja) 2015-02-25 2016-02-25 デスアセトキシツブリシンｈおよびその類似体

Country Status (22)

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

Families Citing this family (13)

* 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
US20210145771A1 (en) * 2017-07-03 2021-05-20 Glaxosmithkline Intellectual Property Development Limited N-(3-(2-(4-chlorophenoxy)acetamido)bicyclo[1.1.1] pentan-1-yl)-2-cyclobutane-1- carboxamide derivatives and related compounds as atf4 inhibitors for treating cancer and other diseases
IL301709B2 (en) 2017-08-09 2025-07-01 Denali Therapeutics Inc Compounds, compositions and methods
EP3676297B1 (en) 2017-09-01 2023-05-17 Denali Therapeutics Inc. Compounds, compositions and methods
EP3679036A1 (en) * 2017-09-08 2020-07-15 Seattle Genetics, Inc. Process for the preparation of tubulysins and intermediates thereof
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
KR20210106467A (ko) 2018-12-21 2021-08-30 리제너론 파마슈티칼스 인코포레이티드 튜불리신 및 단백질-튜불리신 접합체
EP3924341A4 (en) 2019-02-13 2022-11-02 Denali Therapeutics Inc. Compounds, compositions and methods
BR112021015639A2 (pt) 2019-02-13 2021-10-05 Denali Therapeutics Inc. Compostos, composições e métodos
US11787814B2 (en) * 2019-07-11 2023-10-17 Ascentage Pharma (Suzhou) Co., Ltd. Method for preparing 2-indolinospirone compound and intermediate thereof
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

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050239713A1 (en) * 2002-07-09 2005-10-27 R&D-Biopharmaceuticals Am Novel tubulysin analogues
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
WO2008138561A1 (en) * 2007-05-10 2008-11-20 R & D Biopharmaceuticals Gmbh Tubulysine derivatives
JP2011500835A (ja) * 2007-10-25 2011-01-06 エンドサイト，インコーポレイテッド チューブリシン類および調製プロセス
JP2011037846A (ja) * 2009-07-22 2011-02-24 Kemotech Srl 医薬組成物
JP2012503621A (ja) * 2008-09-25 2012-02-09 ユニベルシタート デス サーランデス 生物活性プレチューブリシンおよびその使用
JP2013501055A (ja) * 2009-08-03 2013-01-10 メダレックス インコーポレーティッド 抗増殖性化合物、その抱合体、そのための方法ならびにその使用
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
JP2013536171A (ja) * 2010-07-19 2013-09-19 ライプニッツ−インスティチュート フュア プフランツェンビオケミ チューブリシン類似体
WO2015157594A1 (en) * 2014-04-11 2015-10-15 Medimmune Llc Tubulysin derivatives

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US7776814B2 (en) * 2002-07-09 2010-08-17 R&D-Biopharmaceuticals Gmbh Tubulysin conjugates
US20110263650A1 (en) 2007-07-20 2011-10-27 Helmholtz-Zentrum Für Infektions-Forschung Gmbh Tubulysin D Analogues
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
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US20050239713A1 (en) * 2002-07-09 2005-10-27 R&D-Biopharmaceuticals Am Novel tubulysin analogues
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
WO2008138561A1 (en) * 2007-05-10 2008-11-20 R & D Biopharmaceuticals Gmbh Tubulysine derivatives
JP2011500835A (ja) * 2007-10-25 2011-01-06 エンドサイト，インコーポレイテッド チューブリシン類および調製プロセス
JP2012503621A (ja) * 2008-09-25 2012-02-09 ユニベルシタート デス サーランデス 生物活性プレチューブリシンおよびその使用
JP2011037846A (ja) * 2009-07-22 2011-02-24 Kemotech Srl 医薬組成物
JP2013501055A (ja) * 2009-08-03 2013-01-10 メダレックス インコーポレーティッド 抗増殖性化合物、その抱合体、そのための方法ならびにその使用
JP2013536171A (ja) * 2010-07-19 2013-09-19 ライプニッツ−インスティチュート フュア プフランツェンビオケミ チューブリシン類似体
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
WO2015157594A1 (en) * 2014-04-11 2015-10-15 Medimmune Llc Tubulysin derivatives

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PATTERSON, ANDREW W.; PELTIER, HILLARY M.: "Expedient Synthesis of N-Methyl Tubulysin Analogues with High Cytotoxicity", JOURNAL OF ORGANIC CHEMISTRY, vol. 73(12), JPN6019048759, 2008, US, pages 4362 - 4369, ISSN: 0004330423 *
WANG, ZHIYONG; MCPHERSON, PETER A.: "Structure-activity and high-content imaging analyses of novel tubulysins", CHEMICAL BIOLOGY & DRUG DESIGN, vol. 70(2), JPN6019048760, 2007, pages 75 - 86, ISSN: 0004330424 *

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Publication number Publication date
EA201791896A1 (ru) 2018-02-28
CN107529754A (zh) 2018-01-02
MX2017011024A (es) 2017-10-20
CA2977589A1 (en) 2016-09-01
PE20180355A1 (es) 2018-02-21
EP3261443A4 (en) 2018-09-26
IL254089A0 (en) 2017-10-31
GT201700190A (es) 2018-11-26
US10808007B2 (en) 2020-10-20
DOP2017000202A (es) 2017-09-29
EP3261443B1 (en) 2021-04-28
PH12017501539A1 (en) 2018-02-05
SG11201706820RA (en) 2017-09-28
US20180127463A1 (en) 2018-05-10
HK1248069A1 (zh) 2018-10-12
BR112017018305A2 (pt) 2018-04-17
CL2017002170A1 (es) 2018-06-08
AU2016222575A1 (en) 2017-09-07
CO2017008600A2 (es) 2018-02-09
EP3261443A1 (en) 2018-01-03
ECSP17057131A (es) 2019-03-29
KR20170137725A (ko) 2017-12-13
CR20170438A (es) 2018-01-30
WO2016138288A1 (en) 2016-09-01

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