HK1248069A1 - 去乙酰氧基微管溶素h及其类似物 - Google Patents

去乙酰氧基微管溶素h及其类似物 Download PDF

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Publication number
HK1248069A1
HK1248069A1 HK18107653.3A HK18107653A HK1248069A1 HK 1248069 A1 HK1248069 A1 HK 1248069A1 HK 18107653 A HK18107653 A HK 18107653A HK 1248069 A1 HK1248069 A1 HK 1248069A1
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HK
Hong Kong
Prior art keywords
present disclosure
analogs
desacetoxytubulysin
provides
compounds disclosed
Prior art date
Application number
HK18107653.3A
Other languages
English (en)
Chinese (zh)
Inventor
Kyriacos C. Nicolaou
Dionosios VOURLOUMIS
Jun Yin
Rohan ERANDE
Debashis MANDAL
Philipp KLAHN
Original Assignee
William Marsh Rice University
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Filing date
Publication date
Application filed by William Marsh Rice University filed Critical William Marsh Rice University
Publication of HK1248069A1 publication Critical patent/HK1248069A1/zh

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    • 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
    • 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
    • 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
    • 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
    • C07D417/14—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

Landscapes

  • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (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)
  • 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)
HK18107653.3A 2015-02-25 2016-02-25 去乙酰氧基微管溶素h及其类似物 HK1248069A1 (zh)

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
HK1248069A1 true HK1248069A1 (zh) 2018-10-12

Family

ID=56789084

Family Applications (1)

Application Number Title Priority Date Filing Date
HK18107653.3A HK1248069A1 (zh) 2015-02-25 2016-02-25 去乙酰氧基微管溶素h及其类似物

Country Status (22)

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

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017049140A2 (en) 2015-09-18 2017-03-23 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
BR112020000122A2 (pt) * 2017-07-03 2020-07-07 Glaxosmithkline Intellectual Property Development Limited derivados da n-(3-(2-(4-clorofenóxi)acetamido)biciclo[1.1.1] pentan-1-il)-2-ciclobutano-1-carboxamida e compostos relacionados como inibidores do atf4 para tratamento contra o câncer e outras doenças
CA3071024A1 (en) 2017-08-09 2019-02-14 Denali Therapeutics Inc. Compounds, compositions and methods
CN111201245B (zh) 2017-09-01 2024-04-05 戴纳立制药公司 化合物、组合物和方法
TW202428569A (zh) * 2017-09-08 2024-07-16 美商思進公司 妥布賴森(tubulysins)及其中間產物之製備方法
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
MA53765B2 (fr) 2018-12-21 2025-04-30 Regeneron Pharmaceuticals, Inc. Tubulysines et conjugués tubulysines-protéines
SG11202108552QA (en) 2019-02-13 2021-09-29 Denali Therapeutics Inc Compounds, compositions and methods
EP3924341A4 (en) 2019-02-13 2022-11-02 Denali Therapeutics Inc. Compounds, compositions and methods
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
AU2003266233A1 (en) 2002-07-09 2004-01-23 Morphochem Aktiengesellschaft Fur Kombinatorische Chemie Novel tubulysin analogues
US20100047841A1 (en) * 2007-02-27 2010-02-25 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Synthesis of desacetoxytubulysin h and analogs thereof
US8980833B2 (en) * 2007-05-10 2015-03-17 R&D-Biopharmaceuticals Gmbh Tubulysine derivatives
EP2181101A2 (en) 2007-07-20 2010-05-05 Helmholtz-Zentrum für Infektionsforschung GmbH Tubulysin d analogues
US9187521B2 (en) * 2007-10-25 2015-11-17 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
AU2011285532B2 (en) 2010-08-06 2015-09-10 Endocyte, Inc. Processes for preparing tubulysins
US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
RS56169B1 (sr) * 2013-02-14 2017-11-30 Bristol Myers Squibb Co Jedinjenja tubulisina, metode pripreme i primena
AU2015243379B2 (en) 2014-04-11 2018-02-01 Medimmune Llc Tubulysin derivatives

Also Published As

Publication number Publication date
EP3261443B1 (en) 2021-04-28
US20180127463A1 (en) 2018-05-10
PE20180355A1 (es) 2018-02-21
PH12017501539A1 (en) 2018-02-05
CN107529754A (zh) 2018-01-02
EA201791896A1 (ru) 2018-02-28
ECSP17057131A (es) 2019-03-29
EP3261443A4 (en) 2018-09-26
AU2016222575A1 (en) 2017-09-07
CA2977589A1 (en) 2016-09-01
MX2017011024A (es) 2017-10-20
JP2018509404A (ja) 2018-04-05
SG11201706820RA (en) 2017-09-28
EP3261443A1 (en) 2018-01-03
WO2016138288A1 (en) 2016-09-01
KR20170137725A (ko) 2017-12-13
CO2017008600A2 (es) 2018-02-09
DOP2017000202A (es) 2017-09-29
GT201700190A (es) 2018-11-26
US10808007B2 (en) 2020-10-20
IL254089A0 (en) 2017-10-31
CR20170438A (es) 2018-01-30
CL2017002170A1 (es) 2018-06-08
BR112017018305A2 (pt) 2018-04-17

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