CL2017002170A1 - Desacetoxitubulisina h y análogos de esta. - Google Patents

Desacetoxitubulisina h y análogos de esta.

Info

Publication number
CL2017002170A1
CL2017002170A1 CL2017002170A CL2017002170A CL2017002170A1 CL 2017002170 A1 CL2017002170 A1 CL 2017002170A1 CL 2017002170 A CL2017002170 A CL 2017002170A CL 2017002170 A CL2017002170 A CL 2017002170A CL 2017002170 A1 CL2017002170 A1 CL 2017002170A1
Authority
CL
Chile
Prior art keywords
deacetoxytubulysin
analogs
tubulisine
pharmaco
understands
Prior art date
Application number
CL2017002170A
Other languages
English (en)
Inventor
Kyriacos C Nicolaou
Dionisios Vourloumis
Jun Yin
Rohan Erande
Debashis Mandal
Philipp Klahn
Original Assignee
Univ Rice William M
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 Univ Rice William M filed Critical Univ Rice William M
Publication of CL2017002170A1 publication Critical patent/CL2017002170A1/es

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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

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)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

<p>COMPUESTOS ANALOGOS DE TUBULISINA; METODO PARA PREPARARLOS; COMPOSICION FARMACEUTICA QUE LOS COMPRENDE; CONJUGADO ANTICUERPO-FARMACO; Y METODO PARA TRATAR EL CANCER.</p>
CL2017002170A 2015-02-25 2017-08-25 Desacetoxitubulisina h y análogos de esta. CL2017002170A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562120613P 2015-02-25 2015-02-25
US201662275667P 2016-01-06 2016-01-06

Publications (1)

Publication Number Publication Date
CL2017002170A1 true CL2017002170A1 (es) 2018-06-08

Family

ID=56789084

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2017002170A CL2017002170A1 (es) 2015-02-25 2017-08-25 Desacetoxitubulisina h y análogos de esta.

Country Status (22)

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

Families Citing this family (11)

* 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 ANALOGUES (1-7) AND ASSOCIATED METHODS
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
IL301709A (en) 2017-08-09 2023-05-01 Denali Therapeutics Inc Compounds, preparations and methods
JP2020533308A (ja) * 2017-09-08 2020-11-19 シアトル ジェネティックス， インコーポレイテッド チューブリシンおよびそれらの中間体の調製のためのプロセス
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
EP3898651A2 (en) 2018-12-21 2021-10-27 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
CR20210426A (es) 2019-02-13 2021-09-30 Denali Therapeutics Inc Compuestos, composiciones y 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

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AU2003266233A1 (en) 2002-07-09 2004-01-23 Morphochem Aktiengesellschaft Fur Kombinatorische Chemie Novel tubulysin analogues
EP1521769B1 (de) * 2002-07-09 2015-09-09 Dömling, Alexander Tubulysinkonjugate
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
CA2703491C (en) * 2007-10-25 2017-06-13 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
CA2807511A1 (en) 2010-08-06 2012-02-09 Endocyte, Inc. Processes for preparing tubulysins
US20140080175A1 (en) * 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
KR102215954B1 (ko) 2013-02-14 2021-02-15 브리스톨-마이어스 스큅 컴퍼니 튜부리신 화합물, 그의 제조 및 사용 방법
KR20160142392A (ko) * 2014-04-11 2016-12-12 메디뮨 엘엘씨 튜부리신 유도체

Also Published As

Publication number Publication date
EP3261443A1 (en) 2018-01-03
EP3261443A4 (en) 2018-09-26
CR20170438A (es) 2018-01-30
IL254089A0 (en) 2017-10-31
CO2017008600A2 (es) 2018-02-09
WO2016138288A1 (en) 2016-09-01
CN107529754A (zh) 2018-01-02
KR20170137725A (ko) 2017-12-13
JP2018509404A (ja) 2018-04-05
BR112017018305A2 (pt) 2018-04-17
US20180127463A1 (en) 2018-05-10
ECSP17057131A (es) 2019-03-29
DOP2017000202A (es) 2017-09-29
US10808007B2 (en) 2020-10-20
PE20180355A1 (es) 2018-02-21
HK1248069A1 (zh) 2018-10-12
EP3261443B1 (en) 2021-04-28
SG11201706820RA (en) 2017-09-28
GT201700190A (es) 2018-11-26
MX2017011024A (es) 2017-10-20
PH12017501539A1 (en) 2018-02-05
EA201791896A1 (ru) 2018-02-28
CA2977589A1 (en) 2016-09-01
AU2016222575A1 (en) 2017-09-07

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