KR20170137725A - 데스아세톡시투불리신 h 및 이의 유사체 - Google Patents

데스아세톡시투불리신 h 및 이의 유사체 Download PDF

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Publication number
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)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (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 (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
EP3350200A4 (en) 2015-09-18 2019-03-27 Wake Forest University Health Services ANGIOTENSIN (1 7) ANALOGUE AND ASSOCIATED PROCEDURES
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
CN111094233B (zh) 2017-08-09 2024-03-15 戴纳立制药公司 化合物、组合物及方法
PT3676297T (pt) 2017-09-01 2023-08-29 Denali Therapeutics Inc Compostos, composições e métodos
EP3679036A1 (en) 2017-09-08 2020-07-15 Seattle Genetics, Inc. Process for the preparation of tubulysins and intermediates thereof
US11274124B2 (en) 2017-11-29 2022-03-15 William Marsh Rice University Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith
EP3898651A2 (en) 2018-12-21 2021-10-27 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
CA3129609A1 (en) 2019-02-13 2020-08-20 Denali Therapeutics Inc. Eukaryotic initiation factor 2b modulators
MA54959A (fr) 2019-02-13 2021-12-22 Denali Therapeutics Inc Composés, compositions et procédés
EP3814358B1 (en) * 2019-07-11 2025-09-03 Ascentage Pharma (Suzhou) Co., Ltd. Method for preparing 2-indolinospirone compounds and intermediates 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

Family Cites Families (16)

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Publication number Priority date Publication date Assignee Title
WO2004005326A2 (de) 2002-07-09 2004-01-15 Morphochem Aktiengellschaft Fu Tubulysinkonjugate
WO2004005327A1 (de) 2002-07-09 2004-01-15 Morphochem Ag Komb Chemie Neue tubulysinanaloga
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
ES2463693T3 (es) * 2007-05-10 2014-05-29 R & D Biopharmaceuticals Gmbh Derivados de tubulisina
US20110263650A1 (en) 2007-07-20 2011-10-27 Helmholtz-Zentrum Für Infektions-Forschung Gmbh Tubulysin D Analogues
WO2009055562A1 (en) 2007-10-25 2009-04-30 Endocyte, Inc. Tubulysins and processes for preparing
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
MX2013001402A (es) * 2010-08-06 2013-08-29 Endocyte Inc Proceso para preparar tubulisinas.
US20140080175A1 (en) * 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
SI2956173T1 (sl) 2013-02-14 2017-06-30 Bristol-Myers Squibb Company Spojine tubulizina, postopki pridobivanja in uporaba
TW201625662A (zh) 2014-04-11 2016-07-16 麥迪紐有限責任公司 妥布賴森（ｔｕｂｕｌｙｓｉｎ）衍生物

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

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Patent event date: 20170925

Patent event code: PA01051R01D

Comment text: International Patent Application

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PC1203 Withdrawal of no request for examination